AU2012202382B2 - STAT3/5 activation inhibitor - Google Patents

Abstract

C:\NRPortb1\DCC\RBR\421lB15_l.DoC-4/23/2012 An object of the present invention is to provide a STAT3/5 activation inhibitor. The present invention provides a STAT3/5 activation inhibitor containing an 5 aromatic compound represented by the general formula or a salt thereof as an active ingredient: Y-A Xi wherein X1 represents a nitrogen atom or a group -CH=, R1 represents a group -Z-R , in which Z represents a group CO-, a group -CH(OH)- or the like, R6 represents a 5-to 15 membered monocyclic, dicyclic or tricyclic saturated or 15 unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group -0-, a group -CO-, a group -CH(OH)-or a lower alkylene group, and A represents a group -NHC0 wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl 25 lower alkyl group or the like.

Description

Australian Patents Act 1990 - Regulation 3.2A ORIGINAL COMPLETE SPECIFICATION STANDARD PATENT Invention Title "STAT3/5 activation inhibitor" The following statement is a full description of this invention, including the best method of performing it known to me/us:- C.\NRPortbl\DCC\RBR\42B115_1.DOC-4/23/2012 1 DESCRIPTION STAT3/5 ACTIVATION INHIBITOR This application is a divisional application of Australian Application No. 2007305511 the specification and drawings of which as originally filed are incorporated herein in their entirety by reference. TECHNICAL FIELD [0001] The present invention relates to a STAT3/5 5 activation inhibitor. BACKGROUND ART [0002] A protein family of STAT (signal transducers and activators of transcription) is one of a DNA binding protein 10 and plays a role in information transmission and transcription activation. At present, the STAT family is known to have 6 different members (STAT 1, STAT 2, STAT 3, STAT 4, STAT 5 and STAT 6) and several iso-forms (STAT la, STAT 1P, STAT 3a, STAT3P, STAT 5a and STAT 5b). The activity 15 of STAT is regulated by stimulation of various cytokines and mitogen. When a cytokine binds to its receptors, Janus protein tyrosine kinase (JAK) associated with the receptors is activated. [0003] 20 STAT 3 has a SH2 (src homology 2) domain capable of recognizing the structure of a specifically phosphorylated tyrosine. It is considered that STAT 3 specifically recognizes the phosphorylated tyrosine 2 within a gpl30 cell region and is conveyed onto gp 130 and tyrosine is phosphorylated by JAK. STAT 3 having phosphorylated tyrosine forms a STAT 3 dimer (homodimer) via its SH2 domain or a dimer (heterodimer) 5 of STAT 3 and STAT1, which moves into a nucleus, and recognizes a specific DNA sequence and binds it. In this way, STAT3 is known to regulate transcription of many genes. [0004] 10 Such in-vivo roles of STAT3/5 are reported in several documents. [0005] For example, Non-Patent Document 1 describes the relationships between activation of STAT 3 and IL 15 6-signaling pathways and between IL-6 and chronic diseases such as Alzheimer's disease, rheumatism, Crohn disease and anemia and cancer associated disease such as cachexia. [0006] 20 Furthermore, Non-Patent Document 2 describes the relationship between STAT 3 activation and Hepatitis C Virus, Non-Patent Document 3 describes the relationship between STAT 3 activation and psoriasis, individually. Moreover, Non-Patent Document 2 sets 25 forth the relationships between STAT 3 and an inflammatory disease and an autoimmune disease, and Non-Patent Document 4 sets forth the relationships between STAT 3 activation and obesity, diabetes, 3 infertility, and thermal dysregulaton, etc., individually. Non-Patent Documents 5 and 6, etc. describe that STAT5 is a critical factor in IgE-induced MC (mast cell) activation, and inflammatory and 5 autoimmune diseases, and describe STAT5's roles in allergies, inflammations, hyperprolactinemia, and malignant tumors. [0007] On the other hand, it is known that an 10 aromatic compound having a collagen production inhibitory action is present (Patent Document 1). However, it has been not yet known that the' aromatic compound described in Patent Document 1 has a STAT3/5 activation inhibitory action. 15 [Patent Document 1] W02006/014012 [Patent Document 21 US2001/0029250 [Non-Patent Document 1] J.Gerontology; MEDICAL SCIENCES 2006, Vol.61A, No.6, 575-584 [Non-Patent Document 2] J. Exp. Med. Vol.196, No.5, 20 2002, 641-653 [Non-Patent Document 3] Nature Medicine Vol.11, No.1, 2005, 43-49 [Non-Patent Document 4] PNAS March 30, 2004, vol.101, no.13, 4661-4666 25 [Non-Patent Document 5] J. Immunology, 2006, 177: 3421-3426, [Non-Patent Document 6] Ann. Rheum. Dis. 2004; 63: 67 71 HMtt0r~lnenvovCn\NKFortbl\UU\K\593369_ 1. UU 4 DISCLOSURE OF THE INVENTION [0008] One or more embodiments of the present invention may provide a STAT3/5 activation inhibitor. 5 [0009] The present inventors repeatedly studied on an aromatic compound described in Patent Document 1. As a result, they found that the compound has a STAT3/5 activation inhibitory action. The present invention has 10 been attained based on such a finding. [0010] In one aspect, the invention provides a method for preventing or treating a symptom or disease associated with activation of STAT3/5 by administering to a patient an 15 effective amount of an aromatic compound represented by the general formula (1) or a salt thereof as an active ingredient: [Formula 1] R X wherein X 1 represents a nitrogen atom, 20 R1 represents a group -Z-R Z represents a group -N(R8) -B-,

R

8 represents a hydrogen atom or a lower alkyl group that may have a lower alkoxy group as a substituent, H \tbr\lItcnvoyen\NRPorlbl\DCC\RBR\6393569_ .DOC 5 B represents a group -CO-, R represents a group [Formula 2] (R/)m 5 R 7 represents a halogen atom or a lower alkyl group that may have a halogen atom as a substituent, m represents an integer of 1 or 2 (when m represents 2, two R 7 s may be identical or different) and

R

2 represents a hydrogen atom, 10 Y represents a group -0- or a group -N(Rs)

R

5 represents a hydrogen atom or a lower alkyl group, A represents a group [Formula 3] p represents 1 or 2, 15 R 3 represents a hydrogen atom, a lower alkoxy group, a halogen atom or a lower alkyl group that may have a halogen atom as a substituent,

R

4 represents a group -(T) 1 -N(R 4 )R, T represents a group -N(R)-B 3 -CO-, a group -B 4 -CO- or a 20 group -CO-, R' represents a hydrogen atom or a lower alkyl group,

B

3 represents a lower alkylene group, 1MDriIrWOvel\NK roDI\ (UU K \3.3. _1. UUL 6

B

4 represents a lower alkylene group that may have a hydroxyl group as a substituent, 1 represents 0 or 1,

R

4 and R 5 , together with the nitrogen atom to which they bind 5 form a heterocyclic group which is a piperidinyl or a piperazinyl group that, on the heterocyclic ring, may be substituted by (28) a phenyl-substituted linear or branched alkyl group that may be substituted by an alkylenedioxy group, wherein the alkylene group is linear or branched and has 1 to 4 10 carbon atoms, on the phenyl ring. [0011] In another aspect, the invention provides a use of a compound or salt thereof as defined in claim 1 in the manufacture or a medicament for preventing or treating a 15 symptom or disease associated with activation of STAT3/5. [0012] - [0048] have been deleted [0049] 20 The aromatic compound (1) or a salt thereof serving as an active ingredient of the STAT3/5 activation inhibitor of the present invention is an aromatic compound (1) or a salt thereof represented by item 1 below and preferably aromatic compounds or salts thereof represented 25 by items 2 to 48. [0050] Item 1: An aromatic compound or a salt thereof Hi:\ crvoven\NRPortbl\DCC\RLURR6393569_ 1 DUL. 7 represented by the general formula: [Formula 15] Ri R 2 Y-A (1) Xi 5 10 15 THE NEXT PAGE IS PAGE 29 20 29 (0051] wherein X, represents a nitrogen atom or a group -CH=, R' represents a group -Z-R 6 , Z represents a group -N (Re) -B-, a group -B-N (R)-, a 5 group -Bo-O-, a group [0052] [Formula 16] -NHC0 [0053] a group -CO-, a group-CH (OH)-, a group -N (R 9 a) -CO-N 10 (RSb) -, a group -N=CH-, a group -N (Rica) -SO 2 - (B 22 a) e-, a lower alkenylene group, a group -NHCO-Bi-, a group NHCO-B 2 -(W)u-, a group -Bo-0-B 1 9 a-, a group (0054] [Formula 17] (CH2)k -N N-(B 2 0 a) d' 0 15 [0055] , a group [0056] [Formula 18] -N N-(B 2 1a)c [0057] 20 -, a group -S0 2 -N(R10b)-, a group -S-, a lower alkynylene 30 group, a lower alkylene group, a group -N(R d)-or a group -CO-NH-Bi 8 a-,

R

8 represents a hydrogen atom, a lower alkyl group that may have a lower alkoxy group as a substituent, a lower 5 alkanoyl group, a lower alkylsulfonyl group or a phenyl lower alkyl group, B represents a group -CO-or a lower alkylene group, Bo represents a lower alkylene group,

B

1 represents a -lower alkenylene group that may have a 10 phenyl group as a substituent,

B

2 represents a lower alkylene group that may be substituted by a group selected from the group consisting of a lower alkoxy group and a phenyl group, R9a represents a hydrogen atom or a lower alkyl group; 15 R represents a hydrogen atom or a lower alkyl group, Rioa represents a hydrogen atom or a lower alkyl group, B22a represents a lower alkylene group or a lower alkenylene group, e represents 0 -or 1, 20 Bisa represents a lower alkylene group, B19, represents a lower alkylene group,

B

20 , represents a lower alkylene group, B21, represents a lower alkylene group, k represents 2 or 3, 25 c represents 0 or 1, d' represents 0 or 1, R10b represents a hydrogen atom or a lower alkyl group, R8d represents a hydrogen atom or a lower alkyl group, 31 W represents an oxygen atom, a group -NH-, or a sulfur atom, u represents 0 or 1,

R

6 represents 5-to 15-membered monocyclic, dicyclic or 5 tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (that may have 1 to 3 substituents, which are selected from the group consisting of an oxo group; a lower alkoxy group that may-have a halogen atom as a 10 substituent; a lower alkyl group that may have a halogen atom as a substituent; a halogen atom; a lower alkylsulfonyl group; a phenyl group that may be substituted by a lower alkyl group that may have a halogen atom on the phenyl ring; a lower alkylthio 15 group, a pyrrolyl group, a benzoyl group; a lower alkanoyl.group; lower alkoxycarbonyl group; and an amino group that may have a group selected from the group consisting of a lower alkyl group and a lower alkanoyl group -as a substituent, on the heterocyclic 20 ring), an adamantly group, a naphthyl group (that may have 1 to 3 groups selected from the group consisting of a lower alkyl group, a halogen atom, and an amino group that may have a group selected from the group consisting of a lower alkyl group and a lower alkanoyl 25 group as a substituent, on the naphthalene ring), an alkyl group that may have a lower alkoxy group as a substituent, a cycloalkyl group that may be substituted by a group selected from the group consisting of an 32 amino substituted lower alkyl group that may have a lower alkyl group and a lower alkyl group that may have a halogen atom as a substituent, on the cycloalkyl ring, a lower alkenyl group that may have a halogen 5 atom as a substituent, a lower alkanoyl group, a benzoyl group (that may have 1 to 3 groups selected from the group consisting of a lower alkyl group that may have a halogen atom and halogen atom, as a substituents, on the phenyl .ring), a halogen atom 10 substituted lower alkyl group, cycloalkyl lower alkyl group or a group [0058] (Formula 19] (R') [0059] 15 RI represents a hydrogen atom, a phenyl group, a carboxy group, a hydroxyl group, a halogen atom, a lower alkyl group that may have a halogen atom as a substituent, a phenoxy group, a lower alkoxy group that may have a halogen atom as a substituent, a lower alkylenedioxy 20 group, an amino group that may have, as a substituent, a group selected from the group consisting of a lower alkyl group, a lower alkanoyl group, a benzoyl group, and a cycloalkyl group, a cyano group, a lower alkanoyl group that may have a halogen atom as a substituent, a 25 lower alkylsulfonyl group, an aminosulfonyl group, a 33 lower alkoxycarbonyl group, a lower alkanoyloxy group, a lower alkoxycarbonyl lower alkyl group or a 5-or 6 membered saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur 5 atoms (that may have an oxo group on the heterocyclic ring), m represents an integer from 1 to 5(when m represents 2 to 5, two to five R's may be identical or different) and

R

2 represents a -hydrogen atom, a halogen atom, or a 10 lower alkyl group, Y represents a group -0-, a group -N(R 5 ) -, a group -CO-, a group -CH(OH)-, a lower alkylene group, a group S(O)n-, or a group -C(=N-OH)-,

R

5 represents a hydrogen atom, a lower alkyl group, a 15 lower alkanoyl group, a benzoyl group, a phenyl lower alkyl group, or a cycloalkyl group, n represents 0, 1, or 2, A represents a group [00601 20 [Formula 20] [00611 or a group [00621 [Formula 21] 34 [0063] p represents 1 or 2,

R

3 represents a hydrogen atom, a lower alkoxy group, a halogen atom, a lower alkyl group that may have a 5 halogen atom as a substituent, a lower alkoxycarbonyl group, a carboxy group, a group -CONR"R , or a cyano group, wherein R" and R1 2 may be identical or different and each represent a hydrogen atom, a lower alkyl group, a 10 cycloalkyl group, or a phenyl group, and R" and R 1 , together with the nitrogen atom to which they bind, may bind to each other, directly or via a nitrogen atom, oxygen atom, or sulfur atom to form a 5-to 7-membered saturated heterocyclic ring, 15 R 4 represents an imidazolyl lower alkyl group, a 1,2,4 triazolyl lower alkyl group, a 1,2,3-triazolyl lower alkyl group, a 1,2,5-triazolyl lower alkyl group, a pyrazolyl lower alkyl group, a pyrimidinyl lower alkyl group that may have an oxo group as a substituent on 20 the pyrimidine ring, a 3,5-dioxoisoxazolidin-4-ylidene lower alkyl group, a 1,2,4-oxadiazolyl lower alkyl group that may have a lower alkyl group as a substituent on the 1,2,4-oxadiazole ring, a thiazolidinyl lower alkyl group that may have an oxo 25 group as a substituent on the thiazolidine ring, a group [0064] 35 [Formula 22] / C N-R1 3 [0065] a group [0066] 5 [Formula 23] R 1 3 a RN-R 1 [00671 or a group -(T)i-N(R )R R1 3 represents a hydrogen atom, a lower alkyl group that may have a halogen atom as a substituent, a lower 10 alkanoyl group that may have a halogen atom as a substituent, a lower alkoxycarbonyl group, a phenyl lower alkyl group that may have a lower alkylenedioxy group as a substituent on the phenyl ring, an imidazolyl lower alkyl group, a lower alkoxycarbonyl 15 lower alkyl group, a carboxy lower alkyl group, a benzoyl group, a morpholino-substituted lower alkanoyl group, a piperazinyl carbonyl lower alkyl group that may be substituted, on the piperazine ring, by a phenyl lower alkyl group that may have a lower alkylenedioxy 20 group as a substituent on the phenyl ring, a piperazinyl lower alkanoyl group that may be substituted, on the piperazine ring, by a phenyl lower alkyl group that may have a lower alkylenedioxy group 36 as a substituent on the phenyl ring, a morpholinocarbonyl-substituted lower alkyl group, or an imidazolyl lower alkanoyl group, R1a represents a hydrogen atom or a hydroxyl group, 5 T represents a lower alkylene group, a group -N(R1) -B 3 CO-, a group -B 1 9 -N (R18) -CO-, a group -B 4 -CO-, a group Q-B 5 -CO-, a group -B 6

-N(R

1 )-B-i-CO-, a group -CO-Bq-, a group -CH(OH)-Bg-, a group -CO-Bio-CO-, a group -CH(OH)

B

11 -CO-, a group -CO-, a group -SO 2 -, or a group -B23a 10 CO-CO-, wherein R1 7 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, a cycloalkylcarbonyl group, a lower alkanoyl group that may have a halogen atom as a substituent, a lower alkenyl group, an amino 15 substituted lower alkanoyl group that may have a lower alkyl group as a substituent, or a lower alkylsulfonyl group,

B

3 represents a lower alkylene group,

B

19 represents a lower alkylene group, 20 R18 represents a hydrogen atom or a lower alkyl group,

B

4 represents a lower alkenylene group or a lower alkylene. group that may have a hydroxyl group as a substituent, Q represents an oxygen atom or a group -S(O)n-(wherein 25 n is the same as described above),

B

5 represents a lower alkylene group,

B

6 represents a lower alkylene group,

R'

9 represents a hydrogen atom or a lower alkanoyl 37 group,

B

7 represents a lower alkylene group, Bg represents a lower alkylene group, B represents a lower alkylene group, 5 B 0 represents a lower alkylene group,

B

11 represents a lower alkylene group, B23a represents a lower alkylene group, 1 represents 0 or 1, R"1 represents a-hydrogen atom or an alkyl group that 10 may have a hydroxyl group as a substituent, R1 5 represents (2) a hydroxyl group-substituted alkyl group, (3) a cycloalkyl group that may have a group selected from the group consisting of a hydroxyl group and a lower alkyl group as a substituent, (4) a phenoxy 15 lower alkyl group, (5) a phenyl group that may be substituted, on the phenyl ring, by 1 to 3 groups selected from the group consisting of a lower alkyl group; a lower alkoxy group that may have a halogen atom as a substituent; a halogen atom; an amino lower 20 alkoxy group that may have a lower alkyl group as a substituent; a hydroxyl group-substituted lower alkyl group; a phenyl lower alkyl group; a lower alkynyl group; an amino group that may have a lower alkylsulfonyl group as a substituent; a lower alkylthio 25 group; a cycloalkyl group; a phenylthio group; an adamantyl group; an anilino group that may have a halogen atom as a substituent on the phenyl ring; a lower alkoxycarbonyl group; a piperazinyl group that 38 may have a lower alkyl group as a substituent on the piperazine ring; a pyrrolidinyl group that may have an oxo group as a substituent on the pyrrolidine ring; a lower alkanoylamino group; a cyano group; and a phenoxy 5 group, (6) a phenoxy group, (7) a phenyl lower alkyl group that may be substituted, on the phenyl ring, by 1 to 3 groups selected from the group consisting of a halogen atom, a lower alkoxy group that may have a halogen atom as -a substituent, and a lower alkyl group, 10 (8) a phenyl lower alkyl group that has a lower alkylenedioxy group as a substituent on the phenyl ring, (10) a lower alkoxycarbonyl-substituted lower alkyl group, (11) a carboxy-substituted lower alkyl group, (12) an amino group that may have a lower 15 alkanoyl group as a substituent, (13) a 1,2,3,4 tetrahydroquinolyl group that may have 1 to 3 groups selected from the group consisting of an oxo group, a lower alkoxy group, and a lower alkylenedioxy group as a substituent(s-) on the tetrahydroquinoline ring, (14) 20 a cycloalkyl lower alkyl group, (15) a piperazinyl lower alkanoyl group that may be substituted, on the piperazine ring, by a phenyl lower alkyl group that may have a lower alkylenedioxy group as a substituent on the phenyl ring, (16) a pyridyl lower alkyl group, (17) 25 an amino group-substituted lower alkyl group that may have a group selected from the group consisting of a lower alkyl group and a lower alkanoyl group as a substituent, (18) a lower alkoxy lower alkyl group, 39 (19) an imidazolyl group, (20) an imidazolyl lower alkyl group, (21) a 1,2,3,4 tetrahydroisoquinolylcarbonyl-substituted lower alkyl group, (22) a piperidinylcarbonyl group that may have a 5 group selected from the group consisting of a lower alkoxycarbonyl group, a phenyl lower alkyl group, and a furyl lower alkyl group as a substituent on the piperidine ring, (23) a thiazolidinyl lower alkanoyl group that may have an oxo group as a substituent on 10 the thiazolidine ring, (24) a piperidinyl group that may be substituted, on the piperidine ring, by a group selected from the group consisting of a lower alkoxycarbonyl group, a phenyl lower alkyl group, a lower alkyl group, a benzoyl group, and a furyl lower 15 alkyl group, (25) a carbonyl lower alkyl group substituted by a group [00681 [Formula 24] -NQQ [0069] 20 , (26) a carbonyl lower alkyl group substituted by a group [0070] (Formula 25] NQQ Hi (R 34 )d 40 [0071] (27) a group -CO-B 2 0 -N(R )R, (26a) a pyrrolidinyl lower alkyl group, (27a) a morpholino lower alkyl group, (28a) a phenyl lower alkenyl group, (29a) an 5 anilinocarbonyl lower alkyl group that may have a lower alkyl group as a substituent on the phenyl ring, (30a) an indolyl group, (31a) a piperazinyl lower alkyl group that may have, as a .substituent on the piperazine ring, a group selected from the group consisting of a lower 10 alkyl group and a phenyl lower alkyl group that may have a lower alkylenedioxy group as a substituent on the phenyl ring, (32a) an amidino lower alkyl group that may have a lower alkyl group as a substituent, (33a) a fluorenyl group, (34a) a carbazolyl group that 15 may have a lower alkyl group as a.substituent on the carbazole ring, (35a) an amidino group that may have a lower alkyl group as a substituent, (36a) a piperazinyl-substituted oxalyl group that may have 1 to 3 groups selected from the group consisting of a phenyl 20 lower alkyl group (that may have 1 to 3 groups selected from the group consisting of a lower alkylenedioxy group and a lower alkoxy group as a substituent(s) on the phenyl ring) and a pyridyl lower alkyl group as a substituent(s) on the piperazine ring, or (37a) a 25 cyano-substituted lower alkyl group,

R

34 represents an oxo group or a phenyl group, d represents an integer from 0 to 3,

B

20 represents a lower alkylene group, 41 36 37 R and R , together with the nitrogen atom to which they bind, may bind to each other, directly or via a nitrogen atom, oxygen atom, or sulfur atom to form a 5 to 7-membered saturated heterocyclic group, wherein, on 5 the heterocyclic ring, 1 to 3 phenyl lower alkyl groups that may have a lower alkylenedioxy group on the phenyl ring, may be present as a substituent(s),

R

4 and R1 5 , together. with the nitrogen atom to which they bind, may bind to each other, directly or via a 10 nitrogen atom, oxygen atom, or sulfur atom to form a 5 to 10-membered saturated or unsaturated heterocyclic ring; or a group [0072] [Formula 261 -NQQ 15 [0073] wherein, on the heterocyclic ring, 1 to 3 substituents may be present -which are selected from the group consisting of (28) a phenyl-substituted lower alkyl group, which has 1 to 2 phenyl groups that may be 20 substituted by 1 to 3 groups on the phenyl ring, selected from the group consisting of a lower alkanoyl group, an amino group that may have a lower alkanoyl group as a substituent, a lower alkoxycarbonyl group, a cyano group, a nitro group, a phenyl group, a halogen 25 atom, a lower alkyl group that may have a halogen atom as a substituent, a lower alkoxy group that may have a 42 halogen atom as a substituent, a phenyl lower alkoxy group, a hydroxyl group, and a lower alkylenedioxy group, and that may have a pyridyl group on the lower alkyl group, (29) a carbamoyl group, (30) a pyridyl 5 lower alkyl group that may have, as a substituent(s) on the pyridine ring, 1 to 3 groups selected from the group consisting of a hydroxyl group and a lower alkyl group that may have.a hydroxyl group as a substituent, (31) a pyrrolyl-lower alkyl group that may have 1 to 3 10 lower alkyl groups as a substituent(s) on the pyrrole ring, (32) a benzoxazolyl lower alkyl group, (33) a benzothiazolyl lower alkyl group, (34) a furyl lower alkyl group, (35) a benzoyl group that may be substituted, on the phenyl ring, by 1 to 3 groups 15 selected from the group consisting of a cyano group, an amino group that may have a lower alkylsulfonyl group as a substituent, a halogen atom, a lower alkoxy group, a lower alkyl group that may have a halogen atom as a substituent, a thiazolidinyl lower alkyl group that may 20 have an oxo group as a substituent on the thiazolidine ring, a thiazolidinylidene lower alkyl group that may have an oxo group as a substituent on the thiazolidine ring, and a lower alkylenedioxy group, (36) a pyrimidinyl group, (37) a pyrazinyl group, (38) a 25 pyridyl group, (39) a lower alkoxycarbonyl group, (40) a thiazolidinyl lower alkanoyl group that may be substituted, on the thiazolidine ring, by a group selected from the group consisting of an oxo group and 43 a group [0074] [Formula 27] Rb [0075] 5 (wherein R' and R each represent a lower alkyl group), (41) a lower alkyl group that may have a group selected from the group .consisting of a hydroxyl group and a halogen atom as a substituent, (42) a lower alkanoyl group that may have a halogen atom as a substituent, 10 (43) a phenyl group that may be substituted, on the phenyl ring, by 1 to 3 groups selected from the group' consisting of a carbamoyl group that may have a group selected from the group consisting of a lower alkoxy lower alkyl group and a lower alkyl group, a lower 15 alkoxycarbonyl group, a carboxy group, a cyano group, a phenyl group, a 'halogen atom, a lower alkyl group that may have a halogen atom as a substituent, a lower alkoxy group that may have a halogen atom as a substituent, a benzoyl group that may have a halogen 20 atom as a substituent on the phenyl ring, a phenyl lower alkyl group that may have a halogen atom as a substituent on the phenyl ring, and a hydroxyl group, (44) a phenyl group that may have a lower alkylenedioxy group as a substituent on the phenyl ring, (45) a 25 naphthyl lower alkyl group, (46) a phenoxy group that 44 may be substituted, on the phenyl ring, by 1 to 3 groups selected from the group consisting of a cyano group, a lower alkyl group that may have a halogen atom as a substituent, and a lower alkoxy group that may 5 have a halogen atom as a substituent, (47) a phenoxy lower alkyl group, (48) a phenyl lower alkoxy group that may be substituted, on the phenyl ring, by 1 to 3 groups selected from the group consisting of a halogen atom, a lower alkyl group that may have a halogen atom 10 as a substituent, and a lower alkoxy group that may have a halogen atom as a substituent, (49) a group (Bi 2 CO) t-N (R 20 ) R 2 1 , (50) a group - (CO) o-Bi,-N (R 2 2 ) R 2 1, (51) a 1,2,3,4-tetrahydronaphthyl-substituted lower alkyl group that may be substituted, on the 1,2,3,4 15 tetrahydronaphthalene ring, by 1 to 5 lower alkyl groups as a substituent(s), (52) a cycloalkyl group that may have a hydroxyl group as a substituent, (53) a piperidinyl group that may be substituted, on the piperidine ring, by 1 to 3 lower alkyl groups as a 20 substituent(s), (54) a quinolyl lower alkyl group, (55) a 1,2,3,4-tetrazolyl lower alkyl group that may have a group selected from the group consisting of a lower alkyl group and a phenyl lower alkyl group as a substituent on the tetrazole ring, (56) a thiazolyl 25 lower alkyl group that may have a phenyl group as a substituent on the thiazole ring, (57) a benzoyl lower alkyl group that may have 1 to 3 groups selected from the group consisting of a lower alkoxy group and a 45 halogen atom as a substituent(s) on the phenyl ring, (58) a piperidinyl lower alkyl group that may have a lower alkyl group as a substituent on the piperidine ring, (59) an imidazolyl group that may have 1 to 3 5 phenyl groups as a substituent(s) on the imidazole ring, (60) a benzimidazolyl group that may have 1 to 3 lower alkyl groups as a substituent(s) on the benzimidazole ring, .(61) a pyridyl lower alkoxy group, (62) a 1,2,3,4-tetrahydroquinolyl lower alkyl group 10 that may have an oxo group as a substituent on the tetrahydroquinoline ring, (63) a 1,3,4-oxadiazolyl lower alkyl group that may have an oxo group as a substituent on the 1,3,4-oxadizole ring, (64) a cycloalkyl lower alkyl group, (65) a tetrahydropyranyl 15 group, (66) a thienyl lower alkyl.group, (67) a' pyrimidinylcarbonyl group that may have an oxo group as a substituent on the pyrimidine ring, (68) a hydroxyl group, (69) a carboxy group, (70) a lower alkoxy lower alkyl group, (71) a lower alkoxy lower alkoxy group, 20 (72) a benzoyloxy group, (73) a lower alkoxycarbonyl lower alkoxy group, (74) a carboxy lower alkoxy group, (75) a phenoxy lower alkanoyl group, (76) a 1,2,3,4 tetrahydroquinolylcarbonyl group that may have an oxo group as a substituent on the tetrahydroquinoline ring, 25 (77) a phenylsulfonyl group, (78) an imidazolyl lower alkanoyl group, (79) an imidazolyl lower alkyl group, (80) a pyridylcarbonyl group, (81) an imidazolylcarbonyl group, (82) a lower alkoxycarbonyl 46 lower alkyl group, (83) a carboxy lower alkyl group, (84) a group -(O-Bis)s-CO-N(R")R , (85) a group -N(R _

CO-B

16 -N (R 29

)R

30 , (86) a group -N(R 3 1 ) -B 1 7-CO-N (R 3 2 )R3, (87) a benzoxazolyl group, (88a) a benzothienyl group, 5 (89a) an oxo group, and (90a) a 1,2,3,4 tetrahydroquinolyl group that may have an oxo group as a substituent on the tetrahydroquinoline ring,

B

12 represents a lower alkylene group, t represents 0 or 1, 10 R 2 0 and R 2 1 may be identical or different and each represent a hydrogen atom; an amino group that may have a lower alkoxycarbonyl group as a substituent; a benzoyl group that may have 1 to 3 lower alkoxy groups as a substituent(s) on the phenyl ring; a lower alkyl 15 group; a lower alkyl group having.1 to 2 phenyl groups that may be substituted, on the phenyl ring, by 1 to 3 groups selected from the group consisting of a lower alkoxycarbonyl group, a cyano group, a nitro group, a phenyl group, a halogen atom, a lower alkyl group that 20 may have a halogen atom as a substituent, a lower alkoxy group that may have a halogen atom as a substituent, and a lower alkylthio group; a phenyl group that may be substituted, on the phenyl ring, by 1 to 3 groups selected from the group consisting of a 25 lower alkoxy group that may have a halogen atom as a substituent and a lower alkyl group that may have a halogen atom as a substituent; a lower alkoxycarbonyl group; a cycloalkyl lower alkyl group; a pyrrolidinyl 47 lower alkyl group that may have 1 to 3 lower alkyl groups that may have a hydroxyl group as a substituent on the pyrrolidine ring; an amino-substituted lower alkyl group that may have a group selected from the 5 group consisting of a phenyl group and a lower alkyl group as a substituent; a 1,2,3,4-tetrahydronaphthyl substituted lower alkyl group that may have 1 to 5 lower alkyl groups as a substituent(s) on the 1,2,3,4 tetrahydronaphthalene ring; a naphthyl lower alkyl 10 group; a pyridyl lower alkyl group; a quinolyl lower alkyl group; a 1,2,3,4-tetrazolyl lower alkyl group that may have 1 to 3 groups selected from the group consisting of a lower alkyl group and a phenyl lower alkyl group as a substituent(s) on the tetrazole ring~; 15 a 1,2,4-triazolyl lower alkyl group; a tetrahydrofuryl lower alkyl group that may have a hydroxyl group as a substituent on the lower alkyl group; a phenoxy lower alkyl group that may have 1 to 3 groups selected from the group consisting of a lower alkyl group and a nitro 20 group as a substituent(s) on the phenyl ring; a phenyl lower alkanoyl group; a lower alkanoyl group that may have a halogen atom as a substituent; an imidazolyl lower alkanoyl group; a lower alkoxycarbonyl lower alkyl group; a pyridyl group; or a carboxy lower alkyl 25 group, or a cycloalkyl group; and R 0 and R , together with the nitrogen atom to which they bind, may bind to each other, directly or via a nitrogen atom, oxygen atom, or sulfur atom to form a 5-to 7-membered 48 saturated heterocyclic ring(wherein, on the heterocyclic ring, 1 to 3 substituents may be present, which are selected from the group consisting of a lower alkyl group, a phenyl group that may have 1 to 3 groups 5 selected from the group consisting of a halogen atom and a lower alkyl group that may have a halogen atom as a substituent(s) on the phenyl ring, and a phenyl lower alkyl group that may have a lower alkylenedioxy group as a substituent on the phenyl ring), 10 o represents 0 or 1,

B

13 represents a lower alkylene group, R and R may be identical or different and each represent a hydrogen atom, a lower alkyl group, a benzoyl group that may have 1 to 3 lower alkoxy groups 15 as a substituent(s) on the phenyl ring, a phenoxy lower alkyl group that may have a lower alkyl group as a substituent on the phenyl ring, a phenyl lower alkyl group, or a phenyl group, or R 22 and R 23 , together with the nitrogen atom to which they bind, may bind to each 20 other, directly or via a nitrogen atom, oxygen atom, or sulfur atom to form a 5-to 7-membered saturated heterocyclic ring (wherein, on the heterocyclic ring, 1 to 3 substituents may be present, which are selected from the group consisting of a lower alkyl group and a 25 phenyl lower alkyl group that may have a lower alkylenedioxy group as a substituent on the phenyl ring),

B

15 represents a lower alkylene group, 49 s represents 0 or 1, R and R may be identical or different and each represent a hydrogen atom, a lower alkyl group, a phenyl lower alkyl group, or an imidazolyl lower alkyl 5 group, and R 2 and R , together with the nitrogen atom to which they bind, may bind to each other, directly or via a nitrogen atom, oxygen atom, or sulfur atom to form a 5-to 7-membered saturated heterocyclic ring, (wherein, on the heterocyclic ring, 1 to 3 phenyl lower 10 alkyl groups that may have a lower alkylenedioxy group as a substituent, may be present on the phenyl ring, as a substituent(s)), R represents a hydrogen atom or a lower alkyl group,

B

16 represents a lower alkylene group, 29 30 15 R and R , together with the nitrogen atom to which they bind, may bind to each other, directly or via a nitrogen atom, oxygen atom, or sulfur atom to form a 5 to 7-membered saturated heterocyclic group, wherein, on the heterocycli-c ring, 1 to 3 substituents may be 20 present, which are selected from the group consisting of a lower alkyl group, a phenyl group, and a phenyl lower alkyl group that may have a lower alkylenedioxy group as a substituent on the phenyl ring,

R

31 represents a hydrogen atom or a lower alkyl group, 25 B 1 represents a lower alkylene group, R 2 and R , together with the nitrogen atom to which they bind, may bind to each other, directly or via a nitrogen atom, oxygen atom, or sulfur atom to form a 5- 50 to 7-membered saturated heterocyclic group, (wherein, on the heterocyclic ring, 1 to 3 substituents may be present, which are selected from the group consisting of a lower alkyl group, a phenyl group, and a phenyl 5 lower alkyl group that may have a lower alkylenedioxy group as a substituent on the phenyl ring). [0076] However, that the aforementioned compound or a salt thereof satisfies the following requirements (i) 10 to (v): [0077 ] (i) when Xi represents a group -CH=, then R 3 represents a hydrogen atom; [0078] 15 (ii) when Xi represents a group -CH=, 1 represents 1, T represents -CO-, and R1 4 represents a hydrogen atom or an alkyl group that may have a hydroxyl group as a substituent, R 5 represents the group (24); 20 [0079] (iii) when X, represents a group -CH=, 1 represents 1, and T represents -N(R 7 ) -B 3 -CO-, R 14 and R , together with the nitrogen atom to which they bind, may bind to each other, directly or via a nitrogen 25 atom, oxygen atom, or sulfur atom to form a 5-to 10 membered saturated or unsaturated heterocyclic ring, wherein, on the heterocyclic ring, 1 to 3 groups of (28) are present as a substituent(s); 5l 0080] (iv) when X 1 represents a nitrogen atom, and 1 represents 0, or when X, represents a nitrogen atom, 1 represents 1, and T represents -CO-or -SO 2 , R1 5 is not a 5 group (5), (7), (19), or (20); and [0081] (v) when R 6 represents, a cycloalkyl group that may have on the cycloalkyl ring, a substituent selected from the group consisting of an amino-substituted lower 10 alkyl group that may have a lower alkyl group and a lower alkyl group that may have a halogen atom as a substituent, R 4 represents a group -(T) 1

-N(R

4 ) R1 5 (wherein T and 1 are the same as described above, and R' and R 15 , together with the nitrogen atom to which 15 they bind, may bind to each other, directly or via a nitrogen atom, oxygen atom, or sulfur atom to form a 5 to 10-membered saturated heterocyclic ring; or R1 4 and

R

15 form a group [0082] 20 [Formula 28] -NQQ [0083] [0084] Item 2: The aromatic compound or a salt 25 thereof according to item 1, comprising a compound selected from the group consisting of the compounds 52 represented by the general formulas (1-1) to (1-7) below or a salt thereof as an active ingredient: [0085] [Formula 29]

R

8 R8 R 8 R6 - R 2 Re R 2 RB R2 R BN R 6 BN RB 0-A A CO-A X x I xl (1-) -(1-2) (1-3) RSXR R 5

R

8 R8R R 6B1 R2

R

6 B1 R2 6B 2 RBN R NRB :,I CH-A Y 3 -A S(0),-A (1-4) (1-5) (1-6) R8

R

6 BN - A

X

1 N-OH (1-7) 5 [0086] wherein Y 3 represents a lower alkylene group. Item 3: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds 10 represented by the general formulas (1-8) to (1-14) below or a salt thereof as an active ingredient: 53 [00871 [Formula 30] R8 R 8

R

8

R

6 NB R 6 NB R 6 NB -A - N-A CO-A x X I R5 X1 (1-8) (1-9) (1-10)

R

8

R

8

R

8 IR 2R 6 B 1RR 6 R

R

6 NBc R R4 R 4BCH-A R4 NB S() -A OH X1x (1-11) (1-12) (1-13) R 8

N>

1 2

X

1 N-OH (1-14) [00881 wherein Y 3 represents a lower alkylene group. 5 Item 4: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-15) to (1-21) below or a salt thereof as an active ingredient: 54 [00891 [Formula 31]

R

6 0-Bo R2 6 -Bo /R R 6 0-Bo 2 -0-A -- N-A -CO-A Xi Xi R 5 X (1-5)(1-16) (1-17)

R

6 0-Bo R2 R 6 0-Bo R2 Rr0-Bo R2 CH-A Ya-A I H X (1-18) (1-19) (1-20)

R

6 0-Bo R 2 -A

X

1 N-OH (1-21) [0090] wherein Y 3 represents a lower alkylene group. 5 Item -5: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-22) to (1-28) below or a salt thereof as an active ingredient: 55 [0091] [Formula 32] RZCONH R 2 CONH R 2 R 6 CONH R2 -0-A N-A CO-A Xt X 1

R

5 X (1-22) (1-23) (1-24) R6 aCONH

R

2 R6 7.

CONH

R

2 R6 CONH

R

2 - CH-A Y3-A S()-A Xi OH Xi XI (1-25) (1-26) (1-27) R6 aCONH R2 -A XI N-OH (1-28) [0092] wherein Y 3 represents a lower alkylene group. 5 Item 6: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-29) to (1-35) below or a salt thereof as an active ingredient: 56 [0093] [Formula 33]

R

6 -CO

R

6 -C R2

R

6 -CO R2 0-AA - -j--CO-A (1-29) (1-30) (1-31)

R

6 -CO R R 6 -C0 R 2

R

6 -CO R2 CH-A r-IY3-A S(0),-A XIN Xi OH X X (1-32) (1-33) (1-34)

R

6 -CO R2 CA XI N-OH (1-35) [0094] wherein Y 3 represents a lower alkylene group. 5 Item 7: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-36) to (1-42) below or a salt thereof as an active ingredient: 57 [0095] [Formula 34] 110 HO HO R -CHl R -CH 2 R"-CH 0 N-0 CO-A xX 1

R

5 X (1-36) (1-37) (1-38) HO HO HO R-CH R2CH -i-CH-A Y (0)-A XI OH X (1-39) (1-40) (1-41) HO

R

6 -CH R2 -A XI N-OH (1-42) [0096] wherein Y 3 represents a lower alkylene group. 5 Item -8: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-43) to (1-49) below or a salt thereof as an active ingredient: 58 [0097] [Formula 35] R9b 9a

R

9 b 9a R9b 9a R -NCON R CONr R Re-NCON R -A -N-A CO-A x~1 xRsX

R

5 (1-43) (1-44) (1-45)

R

9 b 9a 9b 9a R 9C R R-NCON R2 RCON (1-46) (1-47) (1-48)

R

9 b 9a R -NCON 2 Xi N-OH (1-49) [0098] wherein Y 3 represents a lower alkylene group. 5 Item -9: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-50) to (1-56) below or a salt thereof as an active ingredient: 59 [0099] [Formula 361 R-HC=N R2 R 6 -HC=N R2 R 6 -HC=N R2 0--A -AC (1-50) (1-51) (1-52)

R

6 -HC=N R 2

R

6 -HC=N R 6 -HC=N R 2 C--A Y3-A - S(0)-A (1-53) (1-54) (1-55)

R

6 -HC=N 2 C- A X N-OH (1-56) (0100] wherein Y 3 represents a lower alkylene group. 5 Item 10: The aromatic compound or a salt thereof accordi-ng to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-57) to (1-63) below or. a salt thereof as an active ingredient: 60 [0101] [Formula 37] a 1oa Ro 2 1Oa R 2

R-(B

22 .) .- SO 2 N / R6-(B 22 ) e-SO 2 N RR-(B 2 2) .- S0 2 N -0-A -- A CO-A X1 R 5 (1-57) (1-58) (1-59) O 1aa 2 10a

R

6 -(B22.) e-S0 2 N R 2 R -(B 22 o) e-SO 2 N R2R 6 -(B22a) e-SO 2 N R2 --A N Y3-A S(0)-A (1-60) (1-61) (1-62) IOU 2

R

6 - (B22a) eS 2 N R NC-A Xi N-OH (1-63) [01021 wherein Y 3 represents a lower alkylene group. 5 Item 11: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-64) to (1-70) below or a salt thereof as an active ingredient: 61 [0103] [Formula 38] R6-) R2--'R2N-A -2R R6 6_ R5 6 (1-64) (1-65) (1-66)

R

6

-Z

1

R

2 R6_ R 2

R

6 Z R 2 CH-A N Y3-A S(0),-A Xi OH xi (1-67) (1-68) (1-69)

R

6 -Z

R

2 C-A XI N-OH (1-70) [0104] wherein Y 3 represents a lower alkylene group, and Zi 5 represents a lower alkenylene group. Item 12: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-71) to (1-77) 10 below or a salt thereof as an active ingredient: 62 [0105] [Formula 39] Re-BICONH R2 Re-BiCONH 2

R

6 -BICONH R2 0-A -- A xi x xi (1-71) (1-72) (1-73) RB-BiCONH : R R 6 BICONH R2 R 6 -BiCONH R 2 X)- CH A

Y

3 -A N S(0)-A X1 OH xi . (1-74) (1-75) (1-76)

R

6 -BiCONH /R2 C-A Xl N-OH (1-77) [0106] wherein Y 3 represents a lower alkylene group. 5 Item 13: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-78) to (1-84) below or a salt thereof as an active ingredient: 63 [01071 [Formula 40] R -(W)u-B 2 CONH / R 2 R-(W)-B2CONH " RR ()-B2CONH R2 O-A s-A CO-A (1-78) (1-79) (1-80)

R

6 -(W) _.B2CONH 6 R2R6-(W)u-B2CONH R2R6-(W)u-B 2 CONH R2 CH-A Y 3 -A S(0),-A X OH Xi X (1-81) (1-82) (1-83)

R

6 -(W) ,-B 2 CONH R X1 N-OH (1-84) [0108] wherein Y 3 represents a lower alkylene group. 5 Item 14: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-85) to (1-91) below or a salt thereof as an active ingredient: 64 [0109] [Formula 411

R

6

-B

1 g.-Bo R2 R 6 -Bi 9 -0-Bo R2 R 6

-B

19 .- 0-Bo , 2 0-A N-A CO-A -.2 Xi R 5 I (1-85) (1-86) (1-87)

R

6

-B

19 -0-Bo R 2

R

6

-B

1 98 -0-Bo

R

2 R6-B9O--Bo R 2 H-A Y 3 -A S(0)n-A 1 OHX Xi (1-88) (1-89) (1-90)

R

6

-B

1 9 a-0-Bo R 2 -A Xi N-OH *(1-91) [0110] wherein Y 3 represents a lower alkylene group. 5 Item 15: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-92) to (1-98) below or a salt thereof as an active ingredient: 65 [01111 [Formula 42]

(CH

2 ) (CH 2 ) k (CH 2 )k R'- (B 20 ) d-N N R 2

R

6

-(B

20 )d'-N oNR 2 R-(B20)d'-N N R2 Y 0 0-A-A kzX-CO-A X 9 1 5 . (1-92) (1-93) (1-94) 0(C2) k (CH2) k (C2) k R'- (B20) d'-N N R 2 R- (B20) d--N N R 2 Re- (B 20 )d'-N N R CH-A 0 Y 3 -A S(0)n-A XI OH X 1 (1-95) (1-96) (1-97) (CH2)k R'- (B20) d'-N N R 2 0 C-A Xi N-OH represnte16: -9e) rmic comoun o a1salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-99) to (1-105) below or. a salt thereof as an active ingredient: 66 (0113] [Formula 43]

R

6

-(B

21 ae-N N R 6

-(B

21 .) N N R 6

-(B

21 a)c-N N R 2 U 2 R 2 0-A __N-A CO-A X 1 (1-99) (1-100) (1-101)

R

6 - (B 21 ) c-N N R 6 - (8 21 .),7N N R 6 - (B 21 .)e- N N R2 R 2 R2 -y-H-AY3-A S(0)n-A Xi OH Xi (1-102) (1-103) (1-104)

R

6

-(B

2 1ae-N N R2 C-A X1 N-OH (1-105) [0114] wherein Y 3 represents a lower alkylene group. 5 Item '17: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-106) to (1-112) below or a salt thereof as an active ingredient: 67 [0115] [Formula 44] Riob Riob Rlob

R

6 -N-0 2 S R 2

R

6 -N-0 2 S R R6-N-02S

R

2 0-A N-A CO-A x ~X I R 5 I (1-106) (1-107) (1-108) Riob R 1 ab RIOb 6 1 I2 6 2 6 1-2SR R -N-0 2 S - R 6 -N-0 2 S 2 R R 6 -N-0 2 S CH-A -Y3-A S()n-A x O H Xi xi (1-109) (1-110) (1-111) RiOb

R

6 -N-0 2 S Xi N-OH (1-112) [0116] wherein Y 3 represents a lower alkylene group. 5 Item 18: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-113) to (1-119) below or a salt thereof as an active ingredient: 68 [0117] [Formula 451

R

6 -S R 26_ R2 6 R2 0- 6-A -CO-A (1-13)(1-114) (1-115) RS -SCH - A S - Y3- A RS SS (),- A Xi OH Xxi (1-116) (1-117) (1-118) R 6 -S

R

6

-

2 6 %N CA

R

6 _S

R

2 Xl N-OH (1-119) [0118] wherein Y 3 represents a lower alkylene group. 5 Item -19: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-120) to (1-126) below or a salt thereof as an active ingredient: 69 [0119) (Formula 46]

R

6

-Z

2 R2 R 6

-Z

2

R

2

R

6

-Z

2

R

2 0-A -A CO-A xi X 1

R

5 x (1-120) (1-121) (1-122)

R

6 -Z,

R

6 -Z 2 R 2 6 Z R 2 R ZCH- A R ZY 3 - A S(0),- A Xi OH Xi (1-123) (1-124) (1-125)

R

6

-Z

2 ,R

X

1 N-OH (1-126) (0120] wherein Y 3 represents a lower alkylene group, and Z 2 5 represents a lower alkynylene group. Item 20: The aromatic compound or a salt thereof according to item 1, comprising a compound selected. from the group consisting of the compounds represented by the general formulas (1-127) to (1-133) 10 below or a salt thereof as an active ingredient: 70 [0121] [Formula 47]

R

6

-B

1 8a-HNOC 2 R 6 -Bisf-HNOC R 2

R

6 -Bis.-HNOC R2 0-A N-A CO-A xi X1 R 5COA (1-127) (1-128) (1-129) R -Bis-HNOC R2 R 6 -Bis.-HNOC R2 R 6 -Bi,-HNOC R 2 CH-A Y 3 -A S(0).-A X H Xi Xi (1-130) (1-131) (1-132)

R

6 -B8is-HNOC

R

2 XI N-OH (1-133) [0122] wherein Y 3 represents a lower alkylene group. 5 Item 21: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas.(1-134) to (1-140) below or. a salt thereof as an active ingredient: 71 [0123] [Formula 48] R 6 -ZR R 6 - Z 3 R- A RR- Z 3 N A R 2

N

2 O-A A C-N-A x I XI R 5 X1 (1-134) (1-135) (1-136)

R

6

-Z

3 CH -A R 6

-Z

3 R R 6 -Z* ( 2 (1-137) (1-138) (1-139)

R

6

-Z

3

R

2 C-A

X

1 N-OH (1-140) (0124] wherein Y 3 represents a lower alkylene group, and 5 Z 3 represents a-lower alkylene group or a group -N(R8) Item 22: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein Y is a group -0-. 10 [0125] Item 23: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein Y is a group -N(R5) [0126] 72 Item 24: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein Y is a group -CO-, a group -CH(OH)-, a lower alkylene group, a group -S(O)n-, or a group -C(=N-OH)-. 5 [0127] Item 25: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein A is a group [0128] 10 [Formula 49] ) [0129] [0130] Item 26: The aromatic compound or a salt 15 thereof according to any one of items 1 to 21, wherein A is a group [01311 [Formula 50] [0132] 20 (0133] Item 27: The aromatic compound or a salt 73 thereof according to any one of items 1 to 21, wherein

R

4 represents an imidazolyl lower alkyl group, a 1,2,4 triazolyl lower alkyl group, a 1,2,3-triazolyl lower alkyl group, a 1,2,5-triazolyl lower alkyl group, a 5 pyrazolyl lower alkyl group, a pyrimidinyl lower alkyl group that may have an oxo group as a substituent on the pyrimidine ring, a 3,5-dioxoisoxazolidin-4-ylidene lower alkyl group, a 1,2,4-oxadiazolyl lower alkyl group that may have a lower alkyl group as a 10 substituent on the 1,2,4-oxadiazole ring, a thiazolidinyl lower alkyl group that may have an oxo group as a substituent on the thiazolidine ring, a group [0134] 15 [Formula 511

-CN-R

3 [0135] or a group [0136] [Formula. 52] R13a R CN-R1 20 [0137] [01381 74 Item 28: The aromatic compound or a salt thereof according to any one of items 1 to 21, represented by the general formula (1) wherein R 4 represents a group -(T) 1 -N(R")R" (T, R1 4 , and R 15 are 5 the same as defined above) and 1 represents 0. (0139] Item 29: The aromatic compound or a salt thereof according to. any one of items 1 to 21, wherein

R

4 is a group -(T) 1 -N(R1 4 )R15, and 1 is 1. 10 [0140] Item 30: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein

R

4 is a group -(T)i-N(R 4 )R 1, 1 is 1, and T is a group N (R") -B 3 -CO-. 15 (0141] Item 31; The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein

R

4 is a group -(T)i-N(R1 4

)R

15 , 1 is 1, and T is a group Bi 9 -N (R' 8 ) -CO-. 20 [0142] Item 32: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein

R

4 is a group -(T) 1

-N(R

14 )R", 1 is 1, and T is a group B 4 -CO-. 25 [01431 Item 33: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein

R

4 is a group -(T)i-N(R")R 5 , 1 is 1, and T is a group - 75

Q-B

5 -CO-. [0144] Item 34: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein 5 R 4 is a group -(T) 1

-N(R

14 )R", 1 is 1, and T is a group B 6 -N (R'") -B 7 -. [0145] Item 35: .The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein 10 R 4 is a group -(T)i-N(R1 4 )R'R, 1 is 1, and T is a group CO-B 8 -. [01461 Item 36: The aromatic compound or a salt thereof according to any one of Items 1 to 21, wherein 15 R 4 is a group -(T)I-N(R 4 )R", 1 is 1, and T is a group CH (OH) -B 9 -. [0147] Item 37: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein 20 R 4 is a group -(T)i-N(R 14 )R'R, 1 is 1, and T is a group CO-B 1 o-CO-. [0148] Item 38: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein 25 R 4 is a group -(T)i-N(R 4

)R'

5 , 1 is 1, and T is a group CH (OH) -Bu 1 -CO-. [0149] Item 39: The aromatic compound or a salt 76 thereof according to any one of items 1 to 21, wherein

R

4 is a group -(T) 1 -N(R")R", 1 is 1, and T is a group CO-. [0150] 5 Item 40: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein

R

4 is a group -(T) 1

-N(R

1 4 )R", 1 is 1, and T is a group S02-. [0151] 10 Item 41: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein

R

4 is a group -(T)i-N(R")R", 1 is 1, and T is a group B23a-CO-CO [0152] 15 Item 42: The aromatic compound or a salt thereof according to any one of items 1 to 21, wherein

R

4 is a group -(T) 1 -N(R1 4 )R", 1 is 1, and T is a lower alkylene group. [0153] 20 Item 43: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of the compounds represented by the general formulas (1-1), (1-2), (1 8), (1-9), (1-15), (1-16), (1-29), (1-30), (1-43), (1 25 44), (1-57), (1-58), (1-64) and (1-65) or a salt thereof as an active ingredient, wherein Y is a group 0-or a group -N(R5)-, A is a group [0154] [Formula 53] 3) [0155] and

R

4 is a group -(T),-N(R ) R1. 5 [0156] Item 44: The aromatic compound or a salt thereof according to item 43, wherein 1 is 1, and T is a group -N (R 7 ) -B 3 -CO- . [0157] 10 Item 45: The aromatic compound or a salt thereof according to item 43, wherein 1 is 1, and T i's a group -B 4 -CO-. [0158] Item 46: The aromatic compound or a salt 15 thereof according to item 43, wherein 1 is 1, and T is a group -CO-. [0159] Item 47: The aromatic compound or a salt thereof according to item 43, wherein 1 is 0. 20 [0160] Item 48: The aromatic compound or a salt thereof according to item 1, comprising a compound selected from the group consisting of N-[6-(4-{[2-(4 piperonylpiperazin-1-yl)-2-oxoethyl]ethylamino-2 25 methoxyphenoxy)pyridin-3-yl] -3, 4-dichlorobenzamide, N- 78 [6-C4-{ [2-(4-piperorylpiperazin-1-yl)-2 oxoethyl] ethylaminolpheioxy)pyridil-3-yl] -4 trifluoromethylbenzamide, N- [6- (4-{ [2- (4 piperonylpiperazin-1-yl) -2-oxoethyl] ethylamino)-2 5 fluorophenoxy)pyridin-3-yll -4-trifluoromethylbenzamide, N-[6-(4-{ [2-(4-piperonylpiperazin-1-yl)-2 oxoethyllmethylamino}-2-fluorophefloxy)pyridifl 3 -Yl] -4 trifluoromethylbenzamide, N-116-(4-{ [2-(4 piperonylpiperazin-1-yl) -2-oxoethyl]methylamino}-2 10 rnethoxyphenoxy)pyrilif-3-ylI -4 trifluoromethylbenzamide, N-[6-(4-( [2-(4 piperonylpiperazin-1-yl) -2-oxoethyllethylamino)-2 methoxyphenoxy)pyridin-3-yl] -4 trifluoromethylbenzamide, N-[6-(4-{ [2-(4 15 piperonylpiperazin-1-yl) -2-oxoethyl]ethylamino}-2 methylphenoxy)pyridin-3-yl] -3, 4-dichlorobenzamide, N [6-(4-{ [2-(4-piperonylpiper azin-1Yl)-2 oxoethyllmethylamino)-2-methylpheloxy)pyridifl 3 Y-] -4 trifluoromethylbenzamide, N- (6-1 4- [3- (4 20 piperonylpiperazin-1-yl) -3-oxopropyllphenoxy~pyridin-3 yl)-3,4-dichlorobelzelesulfofamide, N-[6-(4-{4-[2-(4 piperonylpiperazin-1-yl) -2-oxoethyllpiperazin-1 y1)phenoxy)pyridin-3-yI-4-trifuoromfethybezamide,

N

[6- (4-{4-[2-(4-piperonylpiperazin-1-yl)-2 25 oxoethyllpiperidin-1-yl~phenoxy)pyridif--lYl] 4 trifluoromethylbenzamide, N-{6-[ (4-{4-[2-(4 piperonylpiperazin-.-yl) -2-oxoethyllpiperidin-1 yl }phenyl) methylamino] pyridin-3-yl) -4- 79 trifluoromethylbenzamide, N- [6- (4-{ 4-[2- (4 benzylpiperazin-1-yl) -2-oxoethyllpipericiin-1-yl}-2 methyiphenoxy) pyridin-3-yl]-4-trifluoromethylbenzamide, N-(6- (4-{4- (2- (4-piperonylpiperazin-1-yl) -2 5 oxoethyllpiperidin-1-yl}-2-methylphenoxy)pyridil-3-yl] 4-trifluoromethylbenzamide, N-[6-C4-{4-112-(4 piperonylpiperazin-1-yl) -2-oxoethyllpipericlin-1-yl}-2 methyiphenoxy) pyridin-3-yl]-3, 4-dichlorobenzamide, N (6- [4- (4-benzylpiperazine-1-.carbonyl) phenoxy] pyridin-3 10 yll-4-trifluorornethylbenzamide; N-{6-14-(4 benzylpiperazine-l-carbonyl) phenoxylpyridin-3-yl )-3,4 dichlorobenzamide, N-[6-({4-[3-(4-piperonylpiperazil yl) -3-oxopropyllphenyllmethylamino)pyridil-3-y1] -4 trifluoromethylbenzamide, N-[6-(4-{ [2-(4 15 piperonylpiperazin-1-yl) -2-oxoethyl] ethylamino) 2 fluorophenoxy)pyridin-3-yl] -3, 4-dichlorobenzamiie, N [6-(4-( (2-(4-piperonylpiperazin-1-Yl) -2 oxoethyllmethylaminol-2-fluorophenoxy)pyridifl3-yl] 3,4-dichlorobezanide, N-(6-(4-1 [2-(4 20 piperonylpiperazin-1-yl) -2-oxoethyl]methylamino}-2 methoxyphenoxy)pyridin-3-yl] -3, 4-dichlorobenzamide, N [6-(4-( [2-(4-piperonylpiperazin-1-yl) -2 oxoethyllmethylamino~phenoxy)'pyridin-3-y1I-3, 4 dichlorobenzamide, 1-(6-(4-[3-(4-piperonylpiperazin-l 25 yl)-3-oxopropyllphenoxylpyridin-3-yl)-3-(3,4 dichlorophenyl)-l-ethylurea, N-(6-{4-[3-(4 piperonylpiperazin-1-yl) -3-oxopropyllphenoxylpyridin-3 yl)-4-trifluoromethylbenzamide, N-[6-(4-( [2-(4- 80 benzylpiperazin-1-yl) -2-oxoethyl]methylamino)-2 methylphenoxy)pyridin-3-yl]-4-trifluoromethylbenzamide, N-[6-(4-{4-[2-(4-benzylpiperazin-1-yl)-2 oxoethyl]piperidin-1-yl }phenoxy) pyridin-3-yl] -3,4 5 dichlorobenzamide, N-(6-(4-[3-(4-piperonylpiperazine-1 carbonyl)piperidin-1-yl]phenoxy}pyridin-3-yl)- 3

,

4 dichlorobenzamide, N-[6-(4-{4-[2-(4-benzylpiperazin-1 yl)-2-oxoethyl]piperidin-1-yl phenoxy)pyridin-3-yl]-4 trifluoromethylbenzamide, N-{6-[(4-{4-[2-(4 10 benzylpiperazin-1-yl) -2-oxoethyl]piperidin-1 yl}phenyl) methylamino] pyridin-3-yl} -4 trifluoromethylbenzamide, N-(6-(4-((2-{4-[4-(4 fluorobenzoyl)phenyl]piperazin-1-yl)-2 oxoethyl)methylamino] -2-methoxyphenoxy}pyridin-3-yl) -4 15 trifluoromethylbenzamide, 2- (4-piperonylpiperazin-1 yl) -N-{3-methyl-4-[5- (4 trifluoromethylphenoxymethyl)pyridin-2-yloxylphenyl}-2 oxoacetamide, N-[6-(4-{[2-(4-piperonylpiperazin-1-yl) 2-oxoethyl]methylamino}-2-methylphenoxy)pyridin-3-yl] 20 2-fluoro-4-trifluoromethylbenzamide, N-[6-(4-{4-[2-(4 piperonylpiperazin-1-yl)-2-oxoethyl]piperidin-1-yl}-2 methoxyphenoxy)pyridin-3-yl]-4-trifluoromethylbenzamide and 4-(3-(3-methyl-4-[5-(4 trifluoromethylbenzoylamino)pyridin-2-yloxy]phenyl}-2 25 oxohexahydropyrimidin-1-yl)benzoic acid ethyl ester, or a salt thereof as an active ingredient. [0161] The aromatic compound or a salt thereof 81 serving as the active ingredient of the present invention is a known compound and described in Patent Document 1. Specific examples of individual groups shown 5 in the general formula (1) are as follows. (0162] Examples of the lower alkenylene group include linear or branched alkenylene groups having 2 to 6 carbon atoms and 1 to 3 double bonds such as 10 vinylene, 1-propenylene, 1-methyl-l-propenylene, 2 methyl-l-propenylene, 2-propehylene, 2-butenylene, 1 butenylene, 3-butenylene, 2-pentenylene, 1-pentenylene, 3-pentenylene, 4-pentenylene, 1,3-butadienylene, 1,3 pentadienylene, 2-penten-4-ynylene, 2-hexenylene, 1 15 hexenylene, 5-hexenylene, 3-hexenylene, 4-hexenylene, 3, 3-dimethyl-l-propenylene, 2-ethyl-l-propenylene, 1,3,5-hexatrienylene, 1,3-hexadienylene, and 1,4 hexadienylene groups. Examples of the lower alkynylene group 20 include linear or branched alkynylene groups having 2 to 6 carbon atoms and 1 to 3 triple bonds such-as ethynylene, 1-propynylene, 1-methyl-l-propynylene, 2 methyl-1-propynylene, 2-propynylene, 2-butynylene, 1 butynylene, 3-butynylene, 2-pentynylene, 1-pentynylene, 25 3-pentynylene, 4-pentynylene, 2-pentyn-4-ynylene, 2 hexynylene, 1-hexynylene, 5-hexynylene, 3-hexynylene, 4-hexynylene, 3, 3-diethyl-l-propynylene, and 2-ethyl-1 propynylene groups.

82 [0163] Examples of the lower alkoxy group include linear or branched alkoxy groups having 1 to 6 carbon atoms such as methoxy, ethoxy, propoxy, isopropoxy, 5 butoxy, tert-butoxyl, pentyloxy, and hexyloxy groups. (0164] Examples of the lower alkyl group include linear or branched alkyl groups having 1 to 6 carbon atoms such as methyl, ethyl, propyl, isopropyl, 2,2 10 dimethylpropyl, 1-ethylpropyl, butyl, isobutyl, tert butyl, isopentyl, pentyl, and hexyl groups. (0165] Examples of the lower alkyl group which may have a lower alkoxy group as a substituent include, in 15 addition to the above described lower alkyl groups, linear or branched alkyl groups having 1 to 6 carbon atoms which may have a linear or branched alkoxy group having 1 to 6 carbon atoms as a substituent such as methoxymethyl, 'l-ethoxyethyl, 2-methoxyethyl, 2 20 propoxyethyl, 3-isopropoxypropyl, 4-butoxybutyl, 5 pentyloxypentyl, 6-hexyloxyhexyl, 1,1-dimethyl-2 methoxyethyl, 2-methyl-3-ethoxypropyl, and 3 methoxypropyl groups. [01661 25 Examples of the lower alkanoyl group include linear or branched alkanoyl groups having 1 to 6 carbon atoms such as formyl, acetyl, propionyl, butyryl, isobutyryl, pentanoyl, tert-butylcarbonyl, and hexanoyl 83 groups. [0167] Examples of the phenyl lower alkyl group include phenylalkyl groups whose alkyl moiety is a 5 linear or branched alkyl group having 1 to 6 carbon atoms such as benzyl, 2-phenylethyl, 1-phenylethyl, 3 phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 6 phenylhexyl, 1,1-dimethyl-2-phenylethyl, and 2-methyl 3-phenylpropyl groups. 10 [0168] Examples of the lower alkylene group include linear or branched alkylene groups having 1 to 6 carbon atoms such as methylene, ethylene, trimethylene, 2 methyltrimethylene,- 2, 2-dimethylethylene, 2,2 15 dimethyltrimethylene, 1-methyltrimethylene, methylmethylene, ethylmethylene, tetramethylene, pentamethylene, and hexamethylene groups. [0169] Examples of the lower alkenylene group which 20 may have a phenyl group as a substituent include linear or branched alkenylene groups, which have 2 to 6 carbon atoms and 1 to 3 double bonds, and which may have a phenyl group as a substituent such as vinylene, 1 propenylene, 1-methyl-1-propenylene, 2-methyl-i 25 propenylene, 2-propenylene, 2-butenylene, 1-butenylene, 3-butenylene, 2-pentenylene, 1-pentenylene, 3 pentenylene, 4-pentenylene, 1,3-butadienylene, 1,3 pentadienylene, 2-pentene-4-ynylene, 2-hexenylene, 1- 84 hexenylene, 5-hexenylene, 3-hexenylene, 4-hexenylene, 3,3-dimethyl-1-propenylene, 2-ethyl-1-propenylene, 1,3,5-hexatrienylene, 1,3-hexadienylene, 1,4 hexadienylene, 1-phenylvinylene, 3-phenyl-1 5 propenylene, 3-phenyl-1-methyl-l-propenylene, 3-phenyl 2-methyl-1-propenylene, 1-phenyl-2-propenylene, 1 phenyl-2-butenylene, 3-phenyl-1-butenylene, 1-phenyl-3 butenylene, 5-phenyl-2-pentenylene, 4-phenyl-1 pentenylene, 2-phenyl-3-pentenylene, 1-phenyl-4 10 pentenylene, 1-phenyl-1, 3-butadienylene, 1-phenyl-1, 3 pentadienylene, 1-phenyl-2-penten-4-ynylene, 1-phenyl 2-hexenylene, 3-phenyl-1-hexenylene, 4-phenyl-5 hexenylene, 6-phenyl-3-hexenylene, 5-phenyl-4 hexenylene, 1-phenyl-3,3-dimethyl-l-propenylene, 1 15 phenyl-2-ethyl--propenylene, 6-phenyl-1, 3,5 hexatrienylene, 1-phenyl-1, 3-hexadienylene, and 2 phenyl-1, 4-hexadienylene groups. [0170] Examples of the lower alkylene group which 20 may be substituted with a group selected from the group consisting of a lower alkoxy group and a phenyl group include,.in addition to the above described lower alkylene groups, linear or branched alkylene groups having 1 to 6 carbon-atoms which may be substituted 25 with 1 or 2 groups selected from the group consisting of a linear or branched alkoxy group having 1 to 6 carbon atoms and a phenyl group such as methoxymethylene, 2-phenylethylene, 3- 85 ethoxytrimethylene, 1-propoxy-2-methyltrimethylene, 1 phenyl-2, 2-dimethylethylene, 3-phenyl-2, 2 dimethyltrimethylene, 2-butoxy-l-methyltrimethylene, phenylmethylmethylene, 2-pentyloxyethylmethylene, 4 5 phenyl-2-hexyloxytetramethylene, 3 phenylpentamethylene, 5-phenylhexamethylene, ethoxymethylene, 1-phenylethylene, 3 phenyltrimethylene, .and 2-phenyl-l-methoxyethylene groups. 10 [0171] Examples of the 5-to 15-membered monocyclic, bicyclic or tricyclic saturated or unsaturated heterocyclic group which has 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms include pyrrolidinyl, 15 piperidinyl, piperazinyl, morpholino, pyridyl, 1,2,5,6 tetrahydropyridyl, 1,2,4-triazolyl, 1,2,3-triazolyl, 1,2,5-triazolyl, thiazolidinyl, 1,2, 3,4-tetrazolyl, thienyl, quinolyl, 1,4-dihydroquinolyl, benzothiazolyl, pyrazyl, pyrimidyl, pyridazyl, 2H-pyrrolyl, pyrrolyl, 20 1,3, 4-oxadiazolyl, tetrahydropyranyl, tetrahydrofuryl, furazanyl, carbostyryl, 3,4-dihydrocarbostyryl, 1,2,3,4-tetrahydroquinolyl, 1,2,3,4 tetrahydroisoquinolyl, indolyl, isoindolyl, indolinyl, benzoimidazolyl, benzooxazolyl, imidazolidinyl, 25 isoquinolyl, quinazolidinyl, quinoxalinyl, cinnolinyl, phthalazinyl, carbazoyl, acridinyl, chromanyl, isoindolinyl, isochromanyl, pyrazolyl, imidazolyl, pyrazolidinyl, phenothiazinyl, benzofuryl, 2,3- 86 dihydrobenzo[b) furyl, benzothienyl, phenoxathiinyl, phenoxazinyl, 4H-chromenyl, 1H-indazolyl, phenazinyl, xanthenyl, thianthrenyl, 2-imidazolinyl, 2-pyrrolinyl, furyl, oxazolyl, isooxazolyl, isooxazolidinyl, 5 thiazolyl, isothiazolyl, pyranyl, 2-thiazolinyl, 2 pyrazolinyl, quinuclidinyl, 1, 4-benzooxadinyl, 3,4 dihydro-2H-1, 4-benzooxadinyl, 3, 4-dihydro-2H-1, 4 benzothiazinyl, 1,4-benzothiazinyl, 1,2,3,4 tetrahydroquinoxalinyl, 1, 3-dithia-2, 4 10 dihydronaphthalenyl, phenanthridinyl, 1,4 dithianaphthalenyl, dibenzfb,e]azepine, and 6,11 dihydro-SH-dibenz [b, e] azepine groups. [01721 Examples of the halogen atom include a 15 fluorine atom, chlorine atom, bromine atom and iodine atom. (0173) Examples of the lower alkoxy group which may have a halogen 'atom as a substituent include linear or 20 branched alkoxy groups having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, tert butoxy, pentyloxy, hexyloxy, trifluoromethoxy, trichloromethoxy, chloromethoxy, bromomethoxy, 25 fluoromethoxy, iodomethoxy, difluoromethoxy, dibromomethoxy, 2-chloroethoxy, 2,2, 2-trifluoroethoxy, 2,2, 2-trichloroethoxy, 3-chloropropoxy, 2,3 dichloropropoxy, 4,4, 4-trichlorobutoxy, 4-fluorobutoxy, 87 5-chloropentyloxy, 3-chloro-2-methylpropoxy, 6 bromohexyloxy, and 5,6-dichlorohexyloxy groups. [0174] Examples of the lower alkyl group which may 5 have a halogen atom as a substituent include, in addition to the above described lower alkyl groups, linear or branched alkyl groups having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents such as trifluoromethyl, trichloromethyl, 10 chloromethyl, bromomethyl, fluoromethyl, iodomethyl, difluoromethyl, dibromomethyl, dichloromethyl, 2 chloroethyl, 2,2,2-trifluoroethyl, 2,2,2 trichloroethyl, 3-chloropropyl, 2,3-dichloropropyl, 4,4,4-trichlorobutyl, 4-fluorobutyl, 5-chloropentyl, 3 15 chloro-2-methylpropyl, 5-bromohexyl, and 5,6 dibromohexyl groups. [01753 Examples of the lower alkylsulfonyl group include linear 'or branched alkylsulfonyl groups having 20 1 to 6 carbon atoms such as methylsulfonyl, ethylsulfonyl, propylsulfonyl, isopropylsulfonyl, butylsulfonyl, tert-butylsulfonyl, pentylsulfonyl, and hexylsulfonyl groups. [0176] 25 Examples of the phenyl group which may be substituted, on the phenyl ring, with a lower alkyl group which may have a halogen atom include phenyl groups which may be substituted, on the phenyl ring, 88 with 1 to 3 linear or branched alkyl groups having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms such as phenyl, 2-methylphenyl, 3-methylphenyl, 4 methylphenyl, 2-ethylphenyl, 3-ethylphenyl, 4 5 ethylphenyl, 4-isopropylphenyl, 3-butylphenyl, 4 pentylphenyl, 4-hexylphenyl, 3,4-dimethylphenyl, 3,4 diethylphenyl, 2,4-dimethylphenyl, 2,5-dimethylphenyl, 2,6-dimethylphenyl, .3,4,5-trimethylphenyl, 2 trifluoromethylphenyl, 3-trifluoromethylphenyl, 4 10 trifluoromethylphenyl, 2-(bromomethyl)phenyl, 3-(2 chloroethyl)phenyl, 4-(2,3-dichloropropyl)phenyl, 4-(4 fluorobutyl)phenyl, 3-(5-chloropentyl)phenyi, 4-(5 bromohexyl)phenyl, 4-(5,6-dibromohexyl)phenyl, 3,4 di(trifluoromethyl)phenyl, 3,4-di(4,4,4 15 trichlorobutyl)phenyl, 2,4-di(3-chloro-2 methylpropyl)phenyl, 2,5-di(3-chloropropyl)phenyl, 2,6 di(2,2,2-trifluoroethyl)phenyl, 3,4,5 tri(trifluoromethyl)phenyl, 4-(2,2,2 trichloroethyl)phenyl, 2-methyl-4 20 trifluoromethylphenyl, and 3-ethyl-4-trichloromethyl groups. [01771 Examples of the lower alkylthio group include linear or branched alkylthio groups having 1 to 6 25 carbon atoms such as methylthio, ethylthio, propylthio, isopropylthio, butylthio, tert-butylthio, pentylthio, and hexylthio groups. [0178] 89 Examples of the amino group which may have a group selected from the group consisting of a lower alkyl group and a lower alkanoyl group as a substituent include amino groups which may have 1 or 2 groups 5 selected from the group consisting of linear or branched alkyl groups having 1 to 6 carbon atoms and linear or branched alkanoyl groups having 1 to 6 carbon atoms as substituents such as amino, methylamino, ethylamino, propylamino, isopropylamino, butylamino, 10 tert-butylamino, pentylamino, hexylamino, dimethylamino, diethylamino, dipropylamino, dibutylamino, dipentylamino, dihexylamino, N-methyl-N ethylamino, N-ethyl-N-propylamino, N-methyl-N butylamino, N-methyl-N-hexylamino, N-acetylamino, N 15 formylamino, N-propionylamino, N-butyrylamino, N isobutyrylamino, N-pentanoylamino, N-tert butylcarbonylamino, N-hexanoylamino, diacetylamino, N acetyl-N-methylamino, and N-acetyl-N-ethylamino groups. [0179] 20 Examples of the naphthyl group which may be substituted on the naphthalene ring with 1 to 3 . substituents selected from the group consisting of a lower alkyl group, a halogen atom, and an amino group which may have a group selected from the group 25 consisting of a lower alkyl group and a lower alkanoyl group include naphthyl groups which may have, on the naphthalene ring, 1 to 3 substituents selected from the group consisting of a linear or branched alkyl group 90 having 1 to 6 carbon atoms, a halogen atom, and an amino group which may have 1 or 2 substituents selected from the group consisting of a linear or branched alkyl group having 1 to 6 carbon atoms and a linear or 5 branched alkanoyl group having 1 to 6 carbon atoms such as (1-or 2-)naphthyl, 1-methyl-(2-, 3-, 4-, 5-, 6-, 7-or 8-)naphthyl, 2-ethyl-(1-, 3-, 4-, 5-, 6-, 7-or 8-)naphthyl, 3-n-propyl-(l-, 2-, 4-, 5-, 6-, 7-or 8-)naphthyl, 4-n-butyl-(l-, 2-, 3-, 5-, 6-, 7-or 10 8-)naphthyl, 4-methyl-(1-, 2-, 3-, 5-, 6-, 7-or 8-)naphthyl, 5-n-pentyl-(l-, 2-, 3-, 4-, 6-, 7-or 8-)naphthyl, 6-n-hexyl-(l-, 2-, 3-, 4-, 5-, 7-or 8-)naphthyl, 1,7-dimethyl-(2-, 3-, 4-, 5-, 6-or 8-)naphthyl, 1,2,8-trimethyl-(3-, 4-, 5-, 6-or 15 7-)naphthyl, 1-dimethylamino-(2-, .3-, 4-, 5-, 6-, 7-or 8-)naphthyl, 2-dimethylamino-(1-, 3-, 4-, 5-, 6-, 7-or 8-)naphthyl, 3-methylamino-(1-, 2-, 4-, 5-, 6-, 7-or 8-)naphthyl, 5-amino-(1-, 2-, 3-, 4-, 6-, 7-or 8-)naphthyl, 5-dimethylamino-(1-, 2-, 3-, 4-, 6-, 7-or 20 8-)naphthyl, 4-(N-methyl-N-ethylamino)-(1-, 2-, 3-, 5-, 6-, 7-or 8-)naphthyl, 1-methyl-2-dimethylamino-(3-, 4-, 5-, 6-, 7-or 8-)naphthyl, 1-chloro-(2-, 3-, 4-, 5-, 6-, 7-or 8-)naphthyl, and 1-acetylamino-(2-, 3-, 4-, 5-, 6-, 7-or 8-)naphthyl groups. 25 (0180] Examples of the alkyl group which may have a lower alkoxy group as a substituent include, in addition to the above described lower alkyl groups 91 which may have a lower alkoxy group as a substituent, linear or branched alkyl groups having 1 to 8 carbon atoms which may have a linear or branched alkoxy group having 1 to 6 carbon atoms as a substituent such as 5 heptyl, 1-ethylpentyl, octyl, 7-methoxyheptyl, 1 ethoxyheptyl, 2-propoxyl-1-ethylpentyl, 3 isopropoxyoctyl, 7-butoxyheptyl, B-pentyloxyoctyl, and 5-hexyloxy-1-ethylpentyl groups. [0181) 10 Examples of the amino substituted lower alkyl group which may have a lower alkyl group include linear or branched alkyl groups having 1 to 6 carbon atoms substituted with an amino group which may have 1 or 2 linear or branched alkyl groups having 1 to 6 carbon 15 atoms such as aminomethyl, 2-aminoethyl, 1-aminoethyl, 3-aminopropyl, 4-aminobutyl, 5-aminopentyl, 6 aminohexyl, 1,1-dimethyl-2-aminoethyl, 2-methyl-3 aminopropyl, methylaminomethyl, 1-ethylaminoethyl, 2 propylaminoethyl, 3-isopropylaminopropyl, 4 20 butylaminobutyl, 5-pentylaminopentyl, 6 hexylaminohexyl, dimethylaminomethyl, 2 diethylaminoethyl, 2-diisopropylaminoethyl, (N-ethyl-N propylamino)methyl, and 2-(N-methyl-N-hexylamino)ethyl groups. 25 [0182]. Examples of the cycloalkyl group include cycloalkyl groups having 3 to 16 carbon atoms such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, 92 cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl, cycloteradecyl, cyclopentadecyl, and cyclohexadecyl groups. 5 [01831 Examples of the cycloalkyl group which may be substituted with a group selected from the group consisting of an amino substituted lower alkyl group which may have a lower alkyl group and a lower alkyl 10 group which may have a halogen atom as a substituent on the cycloalkyl ring include, in addition to the above described cycloalkyl groups, cycloalkyl groups having 3 to 16 carbon atoms which may be substituted, on the cycloalkyl ring, with 1 to 3 groups selected from the 15 group consisting of a linear or branched alkyl group having 1 to 6 carbon atoms substituted with an amino group which may have 1 or 2 linear or branched alkyl groups having 1 to 6 carbon atoms and a linear or branched alkyl 'group having 1 to 6 carbon atoms which 20 may have 1 to 3 halogen atoms as substituents such as 4-dimethylaminomethylcyclohexyl, 2 (aminomethyl) cyclopropyl, 3- (2-aminomethyl)cyclobutyl, 2- (1-aminoethyl) cyclopentyl, 3- (3 aminopropyl)cyclohexyl, 3-(4-aminobutyl)cycloheptyl, 4 25 (5-aminopentyl)cyclooctyl, 4-(6-aminohexyl)cyclohexyl, 2-(1,1-dimethyl-2-aminoethyl)cycloheptyl, 3-(2-methyl 3-aminopropyl)cyclopentyl, 3 (methylaminomethyl)cyclohexyl, 2-(1- 93 ethylaminoethyl) cyclooctyl, 2- (2 propylaminoethyl)cyclohexyl, 3-(3 isopropylaminopropyl)cyclopentyl, 4-(4 butylaminobutyl) cycloheptyl, 2- (5 5 pentylaminopentyl)cyclohexyl, 2- (6 hexylaminohexyl) cyclopentyl, 3 (dimethylaminomethyl)cyclohexyl, 3-[ (N-ethyl-N propylamino)methyl]cycloheptyl, 4-[2-(N-methyl-N hexylamino)ethyl]cyclooctyl, 4 10 dimethylaminomethylcyclononyl, 2 (aminomethyl) cyclodecyl, 3- (2-aminomethyl) cycloundecyl, 2-(l-aminoethyl)cyclododecyl, 3-(3 aminopropyl)cyclotridecyl, 3-(4 aminobutyl) cyclotetradecyl, 4- (5 15 aminopentyl)cyclopentadecyl, 4-(6 aminohexyl) cyclohexadecyl, 2-(1, 1-dimethyl-2 aminoethyl) cyclononyl, 3- (2-methyl-3 aminopropyl)cyclodecyl, 3 (methylaminomethyl) cycloundecyl, 2- (1 20 ethylaminoethyl)cyclododecyl, 2-(2 propylaminoethyl)cyclotridecyl, 3-(3 isopropylaminopropyl) cyclotetradecyl, 4- (4 butylaminobutyl)cyclopentadecyl, 2-(5 pentylaminopentyl)cyclohexadecyl, 2-(6 25 hexylaminohexyl)cyclononyl, 3 (dimethylaminomethyl) cyclododecyl, 3- [(N-ethyl-N propylamino)methyl]cyclodecyl, 4-[2-(N-methyl-N hexylamino) ethyl]cyclohexadecyl, 2,2- 94 dimethylcyclopropyl, and 2-trifluoromethylcyclopropyl groups. [0184] Examples of the lower alkenyl group include 5 linear or branched alkenyl groups having 2 to 6 carbon atoms and 1 to 3 double bonds such as vinyl, 1 propenyl, 1-methyl-l-propenyl, 2-methyl-l-propenyl, 2 propenyl, 2-butenyl,. 1-butenyl, 3-butenyl, 2-pentenyl, 1-pentenyl, 3-pentenyl, 4-pentenyl, 1,3-butadienyl, 10 1,3-pentadienyl, 2-penten-4-ynyl, 2-hexenyl, 1-hexenyl, 5-hexenyl, 3-hexenyl, 4-hexenyl, 3,3-dimethyl-l propenyl, 2-ethyl-1-propenyl, 1,3,5-hexatrienyl, 1,3 hexadienyl, and 1,4-hexadienyl groups. Examples of the lower alkenyl group which may 15 have a halogen atom as a substituent include, in addition to the above described lower alkenyl groups, linear or branched alkenyl groups having 2 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents and which have 1 to 3 double bonds such as 20 3,3,3-trifluoro-l-propenyl, 2-bromovinyl, 3-chloro-l propenyl, 3-iodo-l-methyl-l-propenyl, 3-fluoro-2 methyl-l-propenyl, 2-butenyl, 4,4,3-trichloro-l butenyl, 4,4-difluoro-3-butenyl, 5-fluoro-2-pentenyl, 5,5,3-tribromo-l-pentenyl, 5-chloro-3-pentenyl, 5,5,5 25 trifluoro-4-pentenyl, 4-chloro-1,3-butadienyl, 5 fluoro-1,3-pentadienyl, 5-bromo-2-penten-4-ynyl, 6 fluoro-2-hexenyl, 6,6,5-trifluoro-l-hexenyl, 6-chloro 5-hexenyl, 5-bromo-3-hexenyl, 6-chloro-4-hexenyl, 3,3- 95 dimethyl-2-chloro-1-propenyl, 3-fluoro-2-ethyl-1 propenyl, 6-chloro-1,3,5-hexatrienyl, 6-bromo-1,3 hexadienyl, and 6-fluoro-1,4-hexadienyl groups. Examples of the benzoyl group (which may 5 have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a lower alkyl group which may have a halogen atom as a substituent and a halogen atom) include benzoyl groups (which may have, on the phenyl ring, with 1 to 3 substituents selected from the 10 group consisting of a linear or branched alkyl group having 1 to 6 carbon atoms and which may have 1 to 3 halogen atoms as substituents and a halogen atom) such as benzoyl, 3,4-difluorobenzoyl, 2-fluorobenzoyl, 3 bromobenzoyl, 4-iodobenzoyl, 4-methylbenzoyl, 2 15 methylbenzoyl, 3-methylbenzoyl, 2-ethylbenzoyl, 3 ethylbenzoyl, 4-ethylbenzoyl, 4-isopropylbenzoyl, 3 butylbenzoyl, 4-pentylbenzoyl, 4-hexylbenzoyl, 3,4 dimethylbenzoyl, 3,4-diethylbenzoyl, 2,4 dimethylbenzoyl, 2, 5-dimethylbenzoyl, 2, 6 20 dimethylbenzoyl, 3,4,5-trimethylbenzoyl, 2 trifluoromethylbenzoyl, 3-trifluoromethylbenzoyl, 4 trifluoromethylbenzoyl, 2- (bromomethyl)benzoyl, 3- (2 chloroethyl)benzoyl, 4-(2,3-dichloropropyl)benzoyl, 4 (4-fluorobutyl)benzoyl, 3-(5-chloropentyl)benzoyl, 4 25 (5-bromohexyl)benzoyl, 4- (5, 6-dibromohexyl)benzoyl, 3,4-di(trifluoromethyl)benzoyl, 3,4-di(4,4,4 trichlorobutyl)benzoyl, 2, 4-di (3-chloro-2 methylpropyl)benzoyl, 2, 5-di(3-chloropropyl) benzoyl, 96 2,6-di(2,2,2-trifluoroethyl)benzoyl, 3,4,5 tri(trifluoromethyl)benzoyl, 4-(2,2,2 trichloroethyl)benzoyl, 2-methyl-4 trifluoromethylbenzoyl, 3-ethyl-4 5 trichloromethylbenzoyl, 2-chloro-4 trifluoromethylbenzoyl, 3-ethyl-4-fluorobenzoyl, 3 fluoro-4-trichloromethylbenzoyl, 2-methyl-3 trifluoromethyl-4-trifluoromethylbenzoyl, 3 fluorobenzoyl, 4-fluorobenzoyl, 2-bromobenzoyl, 4 10 bromobenzoyl, 2-iodobenzoyl, 3-iodobenzoyl, 2,3 dibromobenzoyl, 2,4-diiodobenzoyl, 2,5-difluorobenzoyl, 2,6-dichlorobenzoyl, 2,4,6-trichlorobenzoyl, 2,4 difluorobenzoyl, 3,5-difluorobenzoyl, 2,6 difluorobenzoyl, 2-chlorobenzoyl, 3-chlorobenzoyl, 4 15 chlorobenzoyl, 2,3-dichlorobenzoyl, 2,4 dichlorobenzoyl, 2,5-dichlorobenzoyl, 3,4 dichlorobenzoyl, 2,6-dichlorobenzoyl, 3,5 dichlorobenzoyl, 2,4,6-trifluorobenzoyl, and 2,4 difluorobenzoyl groups. 20 Examples of the halogen substituted lower alkyl group include linear or branched alkyl groups having 1. to 6 carbon atoms which have 1 to 3 halogen atoms as substituents such as trifluoromethyl, trichloromethyl, chloromethyl, bromomethyl, 25 fluoromethyl, iodomethyl, difluoromethyl, dibromomethyl, 2-chloroethyl, 2,2,2-trifluoroethyl, 2,2,2-trichloroethyl, 3-chloropropyl, 2,3 dichloropropyl, 4,4,4-trichlorobutyl, 4-fluorobutyl, 5- 97 chloropentyl, 3-chloro-2-methylpropyl, 5-bromohexyl, and 5,6-dibromohexyl groups. [0185] Examples of the lower alkylenedioxy group 5 include linear or branched alkylene groups having 1 to 4 carbon atoms such as methylenedioxy, ethylenedioxy, trimethylenedioxy, and tetramethylenedioxy groups. (0186] Examples of the amino group which may have a 10 substituent selected from the group consisting of a lower alkyl group, a lower alkanoyl group, a benzoyl group and a cycloalkyl group include amino groups which may have 1 or 2 substituents selected from the group consisting of a linear or branched alkyl group having' 1 15 to 6 carbon atoms, a linear or branched alkanoyl group having 1 to 6 carbon atoms, a benzoyl group, and a cycloalkyl group having 3 to 16 carbon atoms such as amino, methylamino, ethylamino, propylamino, isopropylamino,' butylamino, tert-butylamino, 20 pentylamino, hexylamino, dimethylamino, diethylamino, dipropylamino, dibutylamino, dipentylamino, dihexylamino, N-methyl-N-ethylamino, N-ethyl-N propylamino, N-methyl-N-butylamino, N-methyl-N hexylamino, N-methyl-N-acetylamino, N-acetylamino, N 25 formylamino, N-propionylamino, N-butyrylamino, N isobutyrylamino, N-pentanoylamino, N-tert butylcarbonylamino, N-hexanoylamino, N-ethyl-N acetylamino, N-benzoylamino, N-ethyl-N-benzoylamino, N- 98 methyl-N-benzoylamino, N-acetyl-N-benzoylamino, cyclopropylamino, cyclobutylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N methyl-N-cyclohexylamino, N-methyl-N-cyclopentylamino, 5 N-methyl-N-cycloheptylamino, N-cyclohexyl-N acetylamino, N-cyclopentyl-N-benzoylamino, cyclononylamino, cyclodecylamino, cyclododecylamino, cyclotridecylamino, .cyclotetradecylamino, cyclopentadecylamino, N-methyl-N-cyclohexadecylamino, 10 N-methyl-N-cyclononylamino, N-methyl-N-cyclodecylamino, N-cycloundecyl-N-acetylamino, and N-cyclohexadecyl-N benzoyl groups. [0187] Examples of the lower alkanoyl group which' 15 may have a halogen atom as a substituent include, in addition to the above described lower alkanoyl groups, linear or branched alkanoyl groups having 2 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents such as 2,2,2-trifluoroacetyl, 2,2,2 20 trichloroacetyl, 2-chloroacetyl, 2-bromoacetyl, 2 fluoroacetyl, 2-iodoacetyl, 2,2-difluoroacetyl, 2,2 dibromoacetyl, 3,3,3-trifluoropropionyl, 3,3,3 trichloropropionyl, 3-chloropropionyl, 2,3 dichloropropionyl, 4,4,4-trichlorobutyryl, 4 25 fluorobutyryl, 5-chloropentanoyl, 3-chloro-2 methylpropionyl, 6-bromohexanoyl, and 5,6 dibromohexanoyl groups. [0188] 99 Examples of the lower alkoxycarbonyl group include alkoxycarbonyl groups whose alkoxy moiety is a linear or branched alkoxy group having 1 to 6 carbon atoms such as methoxycarbonyl, ethoxycarbonyl, 5 propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, tert-butoxycarbonyl, pentyloxycarbonyl, and hexyloxycarbonyl groups. [0189] Examples of the lower alkanoyloxy group 10 include linear or branched alkanoyloxy groups having 2 to 6 carbon atoms such as acetyloxy, propionyloxy, butyryloxy, isobutyryloxy, pentanoyloxy, tert butylcarbonyloxy, and hexanoyloxy groups. [0190] 15 Examples of the 5-or 6-membered saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms include pyrrolidinyl, piperidinyl, piperazinyl, morpholino, thiomorpholino, pyridyl, 1,2,5, 6-tetrahydropyridyl, 20 thienyl, pyrazyl, pyrimidyl, pyridazyl, pyrrolyl, 2H pyrrolyl, imidazolidinyl, pyrazolyl, imidazolyl, pyrazolidinyl, furazanyl, 2-imidazolinyl, imidazolidinyl, 2-pyrrolinyl, furyl, oxazolyl, isooxazolidinyl, isooxazolyl, thiazolyl, isothiazolyl, 25 pyranyl, 2-pyrazolidinyl, 1,2,4-triazolyl, 1,2,3 triazolyl, 1,2,5-triazolyl, thiazolidinyl, 2 thiazolinyl, 1,2,3,4-tetrazolyl, 1,3,4-oxadiazolyl, tetrahydropyranyl, and tetrahydrofuryl groups.

100 [0191] Examples of the 5-to 7-membered saturated heterocyclic ring formed by binding R 1 1 and R1 2 each other, together with nitrogen atoms bound to them, 5 through or not through a nitrogen atom, a sulfur atom or an oxygen atom, include pyrrolidinyl, piperidinyl, piperazinyl, morpholino, thiomorpholino, and homopiperazinyl groups. [01921 10 Examples of the imidazolyl lower alkyl group include imidazolylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (1, 2, 4 or 5-)imidazolylmethyl, 2-[(1, 2, 4 or 5-)imidazolyl]ethyl, 1-[(1, 2, 4 or 15 5-)imidazolyl]ethyl, 3-[(1, 2, 4 or 5-)imidazolyllpropyl, 4-[(1, 2, 4 or 5-)imidazolyl]butyl, 5-[(1, 2, 4 or 5-)imidazolyl]pentyl, 6-[(1, 2, 4 or 5-)imidazolyl]hexyl, 1,1-dimethyl-2-((1, 2, 4 or 20 5-)imidazolyllethyl, and 2-methyl-3-[(1, 2, 4 or 5-)imidazolylipropyl groups. [01931 Examples of the 1,2,4-triazolyl lower alkyl group include 1,2,4-triazolylalkyl groups whose alkyl 25 moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (1, 3 or 5-)1,2,4 triazolylmethyl, 2-[(1, 3 or 5-)1,2,4-triazolyl]ethyl, 1-[(1, 3 or 5-)1,2,4-triazolyl]ethyl, 3-[(1, 3 or 101 5-)1,2,4-triazolyllpropyl, 4-[(1, 3 or 5-)1,2,4 triazolyl]butyl, 5-[(1, 3 or 5-)1,2,4-triazolyl]pentyl, 6-[(1, 3 or 5-)1,2,4-triazolyl]hexyl, 1,1-dimethyl-2 [(1, 3 or 5-)1,2,4-triazolyl]ethyl, and 2-methyl-3-[(1, 5 3 or 5-)1,2,4-triazolyl]propyl groups. [0194] Examples of the 1,2,3-triazolyl lower alkyl group include 1, 2, 3-triazolylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 10 6 carbon atoms .such as (1, 4 or 5-)1,2,3 triazolylmethyl, 2-[(1, 4 or 5-)1,2,3-triazolyl]ethyl, 1-((1, 4 or 5-)1,2,3-triazolyl]ethyl, 3-((1, 4 or 5-)1,2,3-triazolyl]propyl, 4-[(1, 4 or 5-)1,2,3 triazolyl]butyl, 5-[(1, 4 or 5-)1,2,3-triazolyl]pentyl, 15 6-[(1, 4 or 5-)1,2,3-triazolyl]hexyl, 1,1-dimethyl-2 [(1, 4 or 5-)1,2,3-triazolyllethyl, and 2-methyl-3-[(l, 4 or 5-)1,2,3-triazolylpropyl groups. (01951 Examples of the 1,2,5-triazolyl lower alkyl 20 group include 1,2,5-triazolylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (1, 3 or 4-)1,2,5 triazolylmethyl, 2-[(1, 3 or 4-)1,2,5-triazolyl]ethyl, 1-[(1, 3 or 4-)1,2,5-triazolyl]ethyl, 3-((1, 3 or 25 4-)1,2,5-triazolyllpropyl, 4-[(1, 3 or 4-)1,2,5 triazolyl]butyl, 5-[(1, 3 or 4-)1,2,5-triazolyllpentyl, 6-((1, 3 or 4-)1,2,5-triazolyl]hexyl, 1,1-dimethyl-2 ((1, 3 or 4-)1,2,5-triazolyl]ethyl, and 2-methyl-3-[(1, 102 3 or 4-)1,2,5-triazolyllpropyl groups. (0196] Examples of the pyrazolyl lower alkyl group include pyrazolylalkyl groups whose alkyl moiety is a 5 linear or branched alkyl group having 1 to 6 carbon atoms such as (1, 3, 4 or 5-)pyrazolylmethyl, 2-[(1, 3, 4 or 5-)pyrazolyl]ethyl, 1-((1, 3, 4 or 5-)pyrazolyl]ethyl, .3-[(, 3, 4 or 5-)pyrazolyl]propyl, 4-((1, 3, 4 or 5-)pyrazolyl]butyl, 5-[(l, 3, 4 or 10 5-)pyrazolyl]pentyl, 6-[(l, 3, 4 or 5-)pyrazolyl]hexyl, 1,1-dimethyl-2-[(l, 3, 4 or 5-)pyrazolylJethyl, and 2 methyl-3-((1, 3, 4 or 5-)pyrazolyl]propyl groups. [0197] Examples of the pyrimidinyl lower alkyl group 15 which may have an oxo group as a substituent on the pyrimidine ring include pyrimidinylalkyl groups which may have 1 to 3 oxo groups as substituents on the pyrimidine ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as 20 (2, 4, 5 or 6-)pyrimidinylmethyl, 2-[(2, 4, 5 or 6-)pyrimidinyl]ethyl, 1-[(2, 4, 5 or 6-)pyrimidinyllethyl, 3-[(2, 4, 5 or 6-)pyrimidinyl]propyl, 4-[(2, 4, 5 or 6-)pyrimidinyl]butyl, 5-[(2, 4, 5 or 25 6-)pyrimidinyl]pentyl, 6-[(2, 4, 5 or 6-)pyrimidinyl]hexyl, 1,1-dimethyl-2-[(2, 4, 5 or 6-)pyrimidinyl]ethyl, 2-methyl-3-[(2, 4, 5 or 6-)pyrimidinyl]propyl, [(1, 3, 4 or 5-)2,6- 103 dioxopyrimidinyl]methyl, [(1, 3, 4, 5 or 6-)2 oxopyrimidinyllmethyl, [(1, 2, 4 or 5-)6 oxopyrimidinyl]methyl, ((1, 2, 5 or 6-)4 oxopyrimidinylimethyl, [(l, 3, 5 or 6-)2,4 5 dioxopyrimidinyl]methyl, 2-[(4 or 6-)2,5 dioxopyrimidinyllethyl, 1-[(1, 3, 4 or 5-)2,6 dioxopyrimidinyl]ethyl, 3-[(1, 3 or 5-)2,4,6 trioxopyrimidinyl]propyl, 4-[(l, 3, 4 or 5-)2,6 dioxopyrimidinyl]butyl, 5-[(4 or 6-)2,5 10 dioxopyrimidinyl]pentyl, 6-[(1, 3, 5 or 6-)2,4 dioxopyrimidinyl]hexyl, 1,1-dimethyl-[(1, 3, 4 or 5-)2,6-dioxopyrimidinyl]ethyl, and 2-methyl-3-[(1, 3, 4 or 5-)2,6-dioxopyrimidinyl]propyl groups. [0198] 15 Examples of the 3,5-dioxoisoxazolidin-4 ylidene lower alkyl group include 3,5 dioxoisoxazolidin-4-ylidenealkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms -such as 3,5-dioxoisoxazolidin-4 20 ylidenemethyl, 3,5-dioxoisoxazolidin-4-ylideneethyl, 3,5-dioxoisoxazolidin-4-ylidenepropyl, 3,5 dioxoisoxazolidin-4-ylideneisopropyl, 3,5 dioxoisoxazolidin-4-ylidenebutyl, 3,5 dioxoisoxazolidin-4-ylidenepentyl, and 3,5 25 dioxoisoxazolidin-4-ylidenehexyl groups. [0199] Examples of the 1,2,4-oxadiazolyl lower alkyl group which may have a lower alkyl group as a 104 substituent on the 1,2,4-oxadiazol ring include 1,2,4 oxadiazolylalkyl groups which may have a linear or branched alkyl group having 1 to 6 carbon atoms as a substituent on the 1,2,4-oxadiazol ring and whose alkyl 5 moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (3 or 5-)1,2,4 oxadiazolylmethyl, 2-[(3 or 5-)1,2,4-oxadiazolyl]ethyl, 1-[(3 or 5-)1,2,4-oxadiazolyl]ethyl, 3-((3 or 5-)1,2,4 oxadiazolyl]propyl, 4-[(3 or 5-)1,2,4 10 oxadiazolyljbutyl, 5-[(3 or 5-)1,2,4 oxadiazolyl]pentyl, 6-[(3 or 5-)1,2,4 oxadiazolylhexyl, 1,1-dimethyl-2-(3 or 5-)1,2,4 oxadiazolyl]ethyl, 2-methyl---[(3 or 5-)1,2,4 oxadiazolyl]propyl, 5-methyl-3-(1,2,4 15 oxadiazolyl)methyl, 3-ethyl-2-[5-(1,2,4 oxadiazolyl)Jethyl, 1-I3-propyl-5-(l,2,4 oxadiazolyl)]ethyl, 3-[5-butyl-3-(1,2,4 oxadiazolyl)]propyl, 4-[3-pentyl-5-(1,2,4 oxadiazolyl)]bu-tyl, 5-[5-hexyl-3-(1,2,4 20 oxadiazolyl)]pentyl, 6-[3-methyl-5-(1,2,4 oxadiazolyl)]hexyl, 1,1-dimethyl-2-[5-isopropyl-3 (1,2,4-oxadiazolyl)]ethyl, and 2-methyl-3-[3-isobutyl 5-(1,2,4-oxadiazolyl)]propyl groups. [02001 25 Examples of the thiazolydinyl lower alkyl group which may have an oxo group as a substituent on the thiazolydine ring include thiazolydinylalkyl groups which may have 1 to 3 oxo groups as substituents on the 105 thiazolydine ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (2, 3, 4 or 5-)thiazolidinylmethyl, 2-((2, 3, 4 or 5-)thiazolidinyl]ethyl, 1-[(2, 3, 4 or 5 5-)thiazolidinyl]ethyl, 3-[(2, 3, 4 or 5-)thiazolidinyl]propyl, 4-[(2, 3, 4 or 5-)thiazolidinyllbutyl, 5-((2, 3, 4 or 5-)thiazolidinyl]pentyl, 6-[(2, 3, 4 or 5-)thiazolidinyl]hexyl, 1,1-dimethyl-2-[(2, 3, 4 or 10 5-)thiazolidinyl]ethyl, 2-methyl-3-[(2, 3, 4 or 5-)thiazolidinyl]propyl, 2,4-dioxo-5 thiazolidinylmethyl, 2-[2-oxo-(3, 4 or 5-)thiazolidinyl]ethyl, 1-[4-oxo-(2, 3 or 5-)thiazolidinyl]ethyl, 3-[5-oxo-(2, 3 or 15 4-)thiazolidinyl]propyl, 4-[2,5-dioxo-(3 or 4-)thiazolidinyl]butyl, 5-[2,4,5-trioxo-3 thiazolidinyl]pentyl, 6-[4,5-dioxo-(2 or 3-)thiazolidinyl]hexyl, 1,1-dimethyl-2-[2,4-dioxo-(3 or 5-)thiazolidinyl]ethyl, 2-methyl-3-[2,4-dioxo-(3 or 20 5-)thiazolidinyl]propyl, and 3-[2,4-dioxo-(3 or 5-)thiazolidinyl]propyl groups. [02011 Examples of the phenyl lower alkyl group which may have a lower alkylenedioxy group as a 25 substituent on the phenyl ring include, in addition to the above described phenyl lower alkyl groups, phenylalkyl groups which may have a linear or branched alkylenedioxy group having 1 to 4 carbon atoms as a 106 substituent on the phenyl ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as 3,4-methylenedioxybenzyl, 3,4 trimethylenedioxybenzyl, 2-(2,3 5 ethylenedioxyphenyl)ethyl, 1-(3,4 trimethylenedioxyphenyl)ethyl, 3-(2,3 tetramethylenedioxyphenyl)propyl, 4-(3,4 methylenedioxyphenyl)butyl, 5-(2,3 ethylenedioxyphenyl)pentyl, 6-(3,4 10 trimethylenedioxyphenyl)hexyl, 1,1-dimethyl-2-(2,3 methylenedioxyphenyl)ethyl, and 2-methyl-3-(3,4 ethylenedioxyphenyl)propyl groups. [0202] Examples of the lower alkoxycarbonyl lower' 15 alkyl group include alkoxycarbonylalkyl groups whose alkoxy moiety is a linear or branched alkoxy group having 1 to 6 carbon atoms and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as methoxycarbonylmethyl, 20 ethoxycarbonylmethyl, 2-methoxycarbonylethyl, 2 ethoxycarbonylethyl, 1-ethoxycarbonylethyl, 3 methoxycarbonylpropyl, 3-ethoxycarbonylpropyl, 4 ethoxycarbonylbutyl, 5-isopropoxycarbonylpentyl, 6 propoxycarbonylhexyl, 1,1-dimethyl-2 25 butoxycarbonylethyl, 2-methyl-3-tert butoxycarbonylpropyl, 2-pentyloxycarbonylethyl, and hexyloxycarbonylmethyl groups. [0203] 107 Examples of the carboxy lower alkyl group include carboxyalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as carboxymethyl, 2-carboxyethyl, 1 5 carboxyethyl, 3-carboxypropyl, 4-carboxybutyl, 5 carboxypentyl, 6-carboxyhexyl, 1,1-dimethyl-2 carboxyethyl, and 2-methyl-3-carboxypropyl groups. [0204] Examples of the morpholino substituted lower 10 alkanoyl group include morpholino substituted alkanoyl groups whose alkanoyl moiety is a linear or branched alkanoyl group having 2 to 6 carbon atoms such as 2 [(2, 3 or 4-)morpholino]acetyl group, 3-[(2, 3 or 4-)morpholino]propionyl, 2-[(2, 3 or 15 4-)morpholino]propionyl, 4-[(2, 3 or 4-)morpholino]butyryl, 5-[(2, 3 or 4-)morpholino]pentanoyl, 6-[(2, 3 or 4-)morpholino]hexanoyl, 2,2-dimethyl-2-((2, 3 or 4-)morpholino]propionyl, and 2-methyl-3-((2, 3 or 20 4-)morpholino]propionyl groups. [0205] Examples of the piperazinylcarbonyl lower alkyl group which may be substituted on the piperazine ring with a phenyl lower alkyl group which may have a 25 lower alkylenedioxy group as a substituent on the phenyl ring include piperazinylcarbonylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms and which may be substituted 108 on the piperazine ring with 1 to 3 phenylalkyl groups which may have a linear or branched alkylenedioxy group having 1 to 4 carbon atoms as a substituent on the phenyl group and whose alkyl moiety is a linear or 5 branched alkyl group having 1 to 6 carbon atoms such as [(1, 2 or 3-)piperazinyl]carbonylmethyl, 2-[(1, 2 or 3-)piperazinyl]carbonylethyl, 1-[(1, 2 or 3-)piperazinyllcarbo.nylethyl, 3-[(1, 2 or 3-)piperazinyllcarbonylpropyl, 4-[(1, 2 or 10 3-)piperazinyl]carbonylbutyl, 5-[(1, 2 or 3-)piperazinyl]carbonylpentyl, 6-[(1, 2 or 3-)piperazinyl]carbonylhexyl, 1,1-dimethyl-2-[(1, 2 or 3-)piperazinyl]carbonylethyl, 2-methyl-3-[(1, 2 or 3-)piperazinyl]carbonylpropyl, (4-benzyl-1 15 piperazinylcarbonyl)methyl, 2-[4-(2-phenylethyl)-1 piperazinylcarbonyl]ethyl, 1-[4-(3-phenylpropyl)-1 piperazinylcarbonyllethyl, 3-[4-(4-phenylbutyl)-1 piperazinylcarbonyl]propyl, 4-[4-(5-phenylpentyl)-1 piperazinylcarbonyl]butyl, 5-[4-(6-phenylpropyl)-1 20 piperazinylcarbonyllpentyl, 6-(4-benzyl-1 piperazinylcarbonyl)hexyl, 1,1-dimethyl-2-(4-benzyl-1 piperazinylcarbonyl)ethyl, 2-methyl-3-(4-benzyl-1 piperazinylcarbonyl)propyl, (4-(3,4 methylenedioxybenzyl)-1-piperazinylcarbonyl]methyl, 2 25 (4-[2-(2,3-ethylenedioxyphenyl)ethyl]-1 piperazinylcarbonyl)ethyl, 1-{4-[3-(3,4 trimethylenedioxyphenyl)propyl]-1 piperazinylcarbonyl}ethyl, 3-{4-[4-(2,3- 109 tetramethylenedioxyphenyl)butyl)-1 piperazinylcarbonyl)propyl, 4-(4-[5-(3,4 methylenedioxyphenyl)pentyl]-1 piperazinylcarbonylibutyl, 5-{4-[3-(2,3 5 ethylenedioxyphenyl)propyl]-1 piperazinylcarbonyl}pentyl, 6-[4-(3,4 trimethylenedioxybenzyl)-1-piperazinylcarbonyl]hexyl, 1,1-dimethyl-2-[4-(2,3-tetramethylenedioxybenzyl)-1 piperazinylcarbonyl]ethyl, 2-methyl-3-[4-(3,4 10 methylenedioxyb.enzyl)-1-piperazinylcarbonyl]propyl, (3,4-dibenzyl-1-piperazinylcarbonyl)methyl, (3,4,5 tribenzyl-1-piperazinylcarbonyl)methyl, [2,4-di(3,4 methylenedioxybenzyl)-1-piperazinylcarbonyllmethyl, [2,4,6-tri(3,4-methylenedioxybenzyl)-1 15 piperazinylcarbonyl]methyl, and [3-benzyl-4-(3,4 methylenedioxybenzyl)-1-piperazinylcarbonyl]methyl groups. [0206] Examples of the piperazinyl lower alkanoyl 20 group which may be substituted on the piperazine ring with a phenyl lower alkyl group which may have a lower alkylenedioxy group as a substituent on the phenyl ring include piperazinylalkanoyl groups whose alkanoyl moiety is a linear or branched alkanoyl group having 2 25 to 6 carbon atoms and which may be substituted on the piperazine ring with 1 to 3 phenylalkyl groups which may have a linear or branched alkylenedioxy group having 1 to 4 carbon atoms as a substituent on the 110 phenyl ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms, such as 2-[(1, 2 or 3-)piperazinyl]acetyl, 3-[(1, 2 or 3-)piperazinyl]propionyl, 2-[(1, 2 or 5 3-)piperazinyl]propionyl, 4-[(1, 2 or 3-)piperazinyl]butyryl, 5-((l, 2 or 3-)piperazinyl]pentanoyl, 6-[(1, 2 or 3-)piperazinyl]hexanoyl, 2,2-dimethyl-3-[ (1, 2 or 3-)piperazinyl]propionyl, 2-methyl-3-[(1, 2 or 10 3-)piperazinyllpropionyl, 2-(4-benzyl-1 piperazinyl)acetyl, 3-[4-(2-phenylethyl)-1 piperazinylipropionyl, 2-[4-(3-phenylpropyl)-1 piperazinyllpropionyl, 4-[4-(4-phenylbutyl)-1 piperazinyllbutyryl., 5-[4-(5-phenylpentyl)-1 15 piperazinyllpentanoyl, 6-[4-(6-phenylpropyl)-1 piperazinyl]hexanoyl, 6-(4-benzyl-1 piperazinyl)hexanoyl, 2,2-dimethyl-3-(4-benzyl-1 piperazinyl)propionyl, 2-methyl-3-(4-benzyl-1 piperazinyl)propionyl, 2-[4-(3,4-methylenedioxybenzyl) 20 1-piperazinyllacetyl, 3-{4-[2-(2,-3 ethylenedioxyphenyl)ethyl]-1-piperazinyl}propionyl, 2 {4-[3-(3,4-trimethylenedioxyphenyl)propyl]-1 piperazinylipropionyl, 4-{4-[4-(2,3 tetramethylenedioxyphenyl)butyl]-1-piperazinyl)butyryl, 25 5-{4-[5-(3,4-methylenedioxyphenyl)pentyl]-1 piperazinylipentanoyl, 5-{4-(3-(2,3 ethylenedioxyphenyl)propyll-1-piperazinylipentanoyl, 6 [4- (3, 4-trimethylenedioxybenzyl) -l- 111 piperazinyl]hexanoyl, 2,2-dimethyl-3-[4-(2,3 tetramethylenedioxybenzyl)-1-piperazinyl]propionyl, 2 methyl-3-[4-(3,4-methylenedioxybenzyl)-1 piperazinyl]propionyl, 2-(3,4-dibenzyl-l 5 piperazinyl) acetyl, 2- (3,4, 5-tribenzyl-1 piperazinyl)acetyl, 2-[2,4-di(3,4 methylenedioxybenzyl)-1-piperazinyl]acetyl, 2-[2,4,6 tri(3,4-methylenedioxybenzyl)-1-piperazinyl]acetyl, and 2- [3-benzyl-4- (3, 4-methylenedioxybenzyl) -1 10 piperazinyllacetyl groups. [02071 Examples of the morpholinocarbonyl substituted lower alkyl group include morpholinocarbonylalkyl groups whose alkyl moiety is -a 15 linear or branched alkyl group having 1 to 6 carbon atoms such as ((2, 3 or 4-)morpholino]carbonylmethyl, 2-[(2, 3 or 4-)morpholino]carbonylethyl, 1-[(2, 3 or 4-)morpholino]carbonylethyl, 3-[(2, 3 or 4-)morpholino]carbonylpropyl, 4-[ (2, 3 or 20 4-)morpholino]carbonylbutyl, 5-[(2, 3 or 4-)morpholino]carbonylpentyl, 6-[ (2,. 3 or 4-)morpholino]carbonylhexyl, 1,1-dimethyl-2-[(2, 3 or 4-)morpholino]carbonylethyl, and 2-methyl-3-[(2, 3 or 4-)morpholino]carbonylpropyl groups. 25 [0208] Examples of the imidazolyl lower alkanoyl group include imidazolylalkanoyl groups whose alkanoyl moiety is a linear or branched alkanoyl group having 2 112 to 6 carbon atoms such as 2-[(1, 2, 4 or 5-)imidazolyl]acetyl, 3-[(l, 2, 4 or 5-)imidazolyl]propionyl, 2-[(1, 2, 4 or 5-)imidazolyl]propionyl, 4-((1, 2, 4 or 5 5-)imidazolyl]butyryl, 5-[(1, 2, 4 or 5-)imidazolyl]pentanoyl, 6-[(1, 2, 4 or 5-)imidazolylhexanoyl, 2,2-dimethyl-3-[(1, 2, 4 or 5-)imidazolyl]propionyl, and 2-methyl-3-[(l, 2, 4 or 5-)imidazolylipropionyl groups. 10 [02091 Examples of the cycloalkylcarbonyl group include cycloalkylcarbonyl groups whose cycloalkyl moiety is a cycloalkyl group having 3 to 16 carbon atoms such as cyclopropylcarbonyl, cyclobutylcarbonyl, 15 cyclopentylcarbonyl, cyclohexylcarbonyl, cycloheptylcarbonyl, cyclooctylcarbonyl, cyclononylcarbonyl, cyclodecylcarbonyl, cycloundecylcarbonyl, cyclododecylcarbonyl, cyclotridecylcarbonyl, cyclotetradecylcarbonyl, 20 cyclopentadecylcarbonyl, and cyclohexadecylcarbonyl groups. [0210] Examples of the amino substituted lower alkanoyl group which may have a lower alkyl group as a 25 substituent include linear or branched alkanoyl groups having 2 to 6 carbon atoms substituted with an amino group which may have 1 or 2 linear or branched alkyl groups having 1 to 6 carbon atoms as substituents such 113 as aminoacetyl, 2-aminopropionyl, 3-aminopropionyl, 4 aminobutyryl, 5-aminopentanoyl, 6-aminohexanoyl, 2,2 dimethyl-3-aminopropionyl, 2-methyl-3-aminopropionyl, methylaminoacetyl, 2-ethylaminopropionyl, 3 5 propylaminopropionyl, 3-isopropylaminopropionyl, 4 butylaminobutyryl, 5-pentylaminopentanoyl, 6 hexylaminohexanoyl, dimethylaminoacetyl, 3 diisopropylaminopropionyl, (N-ethyl-N propylamino)acetyl, and 2-(N-methyl-N-hexylamino)acetyl 10 groups. [0211] Examples of the lower alkylene group which may have a hydroxyl group as a substituent include, in addition to the above described lower alkylene groups', 15 linear or branched alkylene groups having 1 to 6 carbon atoms which may have 1 to 3 hydroxyl groups as substituents such as 1-hydroxymethylene, 2 hydroxyethylene, 1-hydroxyethylene, 2 hydroxytrimethylene, 3-hydroxytrimethylene, 1 20 hydroxytrimethylene, 3-hydroxy-2-methyltrimethylene, 1 hydroxy-2-methyltrimethylene, 3-hydroxy-2, 2 dimethyltrimethylene, 1-hydroxy-2, 2 dimethyltrimethylene, 3-hydroxy-1-methyltrimethylene, 2-hydroxy-l-methyltrimethylene, 1 25 hydroxymethylmethylene, hydroxymethylmethylene, 2 hydroxymethyltrimethylene, 2-hydroxymethyl-2 methyltrimethylene, (2-hydroxyethyl)methylene, (1 hydroxyethyl)methylene, 4-hydroxytetramethylene, 2- 114 hydroxytetramethylene, 3-hydroxytetramethylene, 1 hydroxytetramethylene, 5-hydroxypentamethylene, 4 hydroxypentamethylene, 3-hydroxypentamethylene, 2 hydroxypentamethylene, 1-hydroxypentamethylene, 6 5 hydroxyhexamethylene, 5-hydroxyhexamethylene, 4 hydroxyhexamethylene, 3-hydroxyhexamethylene, 2 hydroxyhexamethylene, 1-hydroxyhexamethylene, 1,2-. dihydroxytrimethylene, 2,2, 4-trihydroxytetramethylene, 1,2, 6-trihydroxyhexamethylene, and 3,4,5 10 trihydroxypenta.methylene groups. [0212] Examples of the alkyl group which' may have a hydroxyl group as a substituent include, in addition to the above described lower alkyl groups, linear or 15 branched alkyl groups having 1 to16 carbon atoms which may have 1 to 3 hydroxyl groups as substituents such as heptyl, octyl, nonyl, decyl, undecyl, dodecyl, tridecyl, tetradecyl, pentadecyl, 1-methylhexyl, hexadecyl, hydroxymethyl, 2-hydroxyethyl, 1 20 hydroxyethyl, 3-hydroxypropyl, 2,3-dihydroxypropyl, 4 hydroxybutyl, 1, 1-dimethyl-2-hydroxyethyl, 5,5,4 trihydroxypentyl, 5-hydroxypentyl, 6-hydroxyhexyl, 1 hydroxyisopropyl, and 2-methyl-3-hydroxypropyl groups. [0213] 25 Examples of the hydroxyl group substituted alkyl group include linear or branched alkyl groups having 1 to 16 carbon atoms and 1 to 3 hydroxyl groups as substituents such as hydroxymethyl, 2-hydroxyethyl, 115 1-hydroxyethyl, 3-hydroxypropyl, 2, 3-dihydroxypropyl, 4-hydroxybutyl, 1,1-dimethyl-2-hydroxyethyl, 5,5,4 trihydroxypentyl, 5-hydroxypentyl, 6-hydroxyhexyl, 1 hydroxyisopropyl, and 2-methyl-3-hydroxypropyl groups. 5 (0214] Examples of the cycloalkyl group which may have a substituent selected from the group consisting of a hydroxyl group and a lower alkyl group include, in addition to the-above described cycloalkyl groups, 10 cycloalkyl groups having 3 to 16 carbon atoms which may have 1 to 3 substituents selected from the group consisting of a hydroxyl group and a linear' or branched alkyl group having 1 to 6 carbon atoms such as 2 hydroxycyclopropyl, 3-hydroxycyclobutyl, 3 15 hydroxycyclopentyl, 2-hydroxycyclohexyl, 4 hydroxycyclohexyl, 3-hydroxycycloheptyl, 4 hydroxycyclooctyl, 5-hydroxycyclononyl, 3 hydroxycyclodecyl, 4-hydroxycycloundecyl, 5 hydroxycyclododecyl, 6-hydroxycyclotridecyl, 7 20 hydroxycyclotetradecyl, 6-hydroxycyclopentadecyl, 8 hydroxycyclohexadecyl, 2,4-dihydroxycyclohexyl, 2,4,6 trihydroxycyclohexyl, 1-methylcyclopentyl, 2 ethylcyclopropyl, 3-n-propylcyclobutyl, 2-n butylcyclohexyl, 4-n-pentylcycloheptyl, 4-n 25 hexylcyclooctyl, 2, 3-dimethylcyclohexyl, 2,3,4 trimethylcyclohexyl, and 2-methyl-4-hydroxycyclohexyl groups. [0215] 116 Examples of the phenoxy lower alkyl group include phenoxyalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as phenoxymethyl, 2-phenoxyethyl, 1 5 phenoxyethyl, 3-phenoxypropyl, 4-phenoxybutyl, 1,1 dimethyl-2-phenoxyethyl, 5-phenoxypentyl, 6 phenoxyhexyl, 1-phenoxyisopropyl, and 2-methyl-3 phenoxypropyl groups. [0216] 10 Examples of the amino lower alkoxy group which may have a lower alkyl group as a substituent include linear or branched alkoxy groups having 1 to 6 carbon atoms substituted with an amino group which may have 1 or 2 linear or branched alkyl groups having 1 to 15 6 carbon atoms such as aminomethoxy, 2-aminoethoxy, 1 aminoethoxy, 3-aminopropoxy, 4-aminobutoxy, 5 aminopentyloxy, 6-aminohexyloxy, 1, 1-dimethyl-2 aminoethoxy, 2-methyl-3-aminopropoxy, methylaminomethoxy, 1-ethylaminoethoxy, 2 20 propylaminoethoxy, 3-isopropylaminopropoxy, 4 butylaminobutoxy, 5-pentylaminopentyloxy, 6 hexylaminohexyloxy, dimethylaminomethoxy, 2 diethylaminoethoxy, 2-diisopropylaminoethoxy, (N-ethyl N-propylamino)methoxy, and 2-(N-methyl-N 25 hexylamino)ethoxy groups. [0217] Examples of the hydroxyl group substituted lower alkyl group include linear or branched alkyl 117 groups having 1 to 6 carbon atoms which have 1 to 3 hydroxyl groups as substituents such as hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 3-hydroxypropyl, 2,3 dihydroxypropyl, 4-hydroxybutyl, 1,1-dimethyl-2 5 hydroxyethyl, 5,5,4-trihydroxypentyl, 5-hydroxypentyl, 6-hydroxyhexyl, 1-hydroxyisopropyl, and 2-methyl-3 hydroxypropyl groups. [0218] Examples of the amino group which may have a 10 lower alkylsulfonyl as a substituent include amino groups which may have 1 or 2 linear or branched alkylsulfonyl groups having 1 to 6 carbon atoms as substituents such as amino, methylsulfonylamino, ethylsulfonylamino, propylsulfonylamino, 15 isopropylsulfonylamino, butylsulfonylamino, tert butylsulfonylamino, pentylsulfonylamino, hexylsulfonylamino, dimethylsulfonylamino, diethylsulfonylamino, dipropylsulfonylamino, dibutylsulfonylamino, dipentylsulfonylamino, 20 dihexylsulfonylamino, N-methylsulfonyl-N ethylsulfonylamino, N-ethylsulfonyl-N propylsulfonylamino, N-methylsulfonyl-N butylsulfonylamino, and N-methylsulfonyl-N hexylsulfonylamino groups. 25 [0219] Examples of the lower alkynyl group include linear or branched alkynyl groups having 2 to 6 carbon atoms such as ethynyl, 2-propynyl, 2-butynyl, 3- 118 butynyl, 1-methyl-2-propynyl, 2-pentynyl, and 2-hexynyl groups. (0220] Examples of the anilino group which may have 5 a halogen atom as a substituent on the phenyl ring include anilino groups which may have 1 to 3 halogen atoms as substituents on the phenyl ring such as anilino, 2-fluoroanilino, 3-fluoroanilino, 4 fluoroanilino, 2-bromoanilino, 3-bromoanilino, 4 10 bromoanilino, 2-iodoanilino, 3-iodoanilino, 4 iodoanilino, 2,3-dibromoanilino, 2,4-diiodoanilino, 2,5-difluoroanilino, 2,6-dichloroanilino, 2,4,6 trichloroanilino, 2,6-difluoroanilino, 3,5 difluoroanilino, 2,6-difluoroanilino, 2-chloroanilino, 15 3-chloroanilino, 4-chloroanilino, 2,3-dichloroanilino, 2,4-dichloroanilino, 2,5-dichloroanilino, 3,4 dichloroanilino, 2,6-dichloroanilino, 3,5 dichloroanilino, 2,4,6-trifluoroanilino, 2,4 difluoroanilino, and 3,4-difluoroanilino groups. 20 [0221] Examples of the piperazinyl group which may have a lower alkyl group as a substituent on the piperazine ring include piperazinyl groups which may have 1 to 3 linear or branched alkyl groups having 1 to 25 6 carbon atoms as substituents on the piperazine ring such as (1-, 2-or 3-)piperazinyl, 4-methyl-(1-, 2-or 3-)piperazinyl, 2,3-dimethyl-(1-or 5-)piperazinyl, and 2,3,4-trimethyl-(1-, 5-or 6-)piperazinyl groups.

119 [0222] Examples of the pyrrolidinyl group which may have an oxo group as a substituent on the pyrrolidine ring include pyrrolidinyl groups which may have 1 or 2 5 oxo groups as substituents on the pyrrolidine ring such as (1-, 2-or 3-)pyrrolidinyl, 2-oxo-(1-, 3-, 4-or 5-)pyrrolidinyl, 3-oxo-(1-, 2-, 4-or 5-)pyrrolidinyl, 2,3-dioxo-(1-, 4-or 5-)pyrrolidinyl, and 2,5-dioxo (1-, 3-or 4-)pyrrolidinyl groups. 10 Examples of the lower alkanoyl amino group include linear or branched alkanoyl amino groups having 2 to 6 carbon atoms which have 1 to 3 halogen atoms as substituents such as acetyl amino, propionyl amino, butyryl amino, pentanoyl amino, 2-methylpropionyl 15 amino, and hexanoyl amino groups. [0223] Examples of the phenyl group which may be substituted on the phenyl ring with 1 to 3 groups selected from the group consisting of a lower alkyl 20 group; a lower alkoxy group which may have a halogen atom as a substituent; a halogen atom; an amino lower alkoxy group which may have a lower alkyl group as a substituent; a hydroxyl group substituted lower alkyl group; a phenyl lower alkyl group; a lower alkynyl 25 group; an amino group which may have a lower alkylsulfonyl group as a substituent; a lower alkylthio group; a cycloalkyl group; a phenylthio group; an adamantyl group; an anilino group which may have a 120 halogen atom as a substituent on the phenyl ring; a lower alkoxycarbonyl group; a piperazinyl group which may have a lower alkyl group as a substituent on the piperazine ring; a lower alkanoylamino group; a cyano 5 group; a pyrrolidinyl group which may have an oxo group as a substituent on the pyrrolidine ring; and a phenoxy group include phenyl groups which may be substituted on the phenyl ring with 1 to 3 groups selected from the group consisting of a linear or branched alkyl group 10 having 1 to 6 carbon atoms; a linear or branched alkoxy group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms; a halogen atom; an aminoalkoxy group whose alkoxy moiety is a linear or branched alkoxy group having 1 to 6 carbon atoms and which may have I 15 or 2 linear or branched alkyl groups having 1 to 6 carbon atom as substituents; a linear or branched alkyl group having 1 to 6 carbon atoms and 1 to 3 hydroxyl groups as substituents; a phenylalkyl group whose alkyl moiety is a linear or branched alkyl group having 1 to 20 6 carbon atoms; a linear or branched alkynyl group having 2 to 6 carbon atoms; an amino group which may have 1 or 2 linear or branched alkylsulfonyl groups having 1 to 6 carbon atoms as substituents; a linear or branched alkylthio group having 1 to 6 carbon atoms; a 25 cycloalkyl group having 3 to 16 carbon atoms; a phenylthio group; an adamantyl group; an anilino group which may have 1 to 3 halogen atoms as substituents on the phenyl ring; an alkoxycarbonyl group whose akloxy 121 moiety is a linear or branched alkoxy group having 1 to 6 carbon atoms; an amino group which may have 1 or 2 linear or branched alkanoyl groups having 2 to 6 carbon atoms; a cyano group; a piperazinyl group which may 5 have 1 to 3 linear or branched alkyl groups having 1 to 6 carbon atoms as substituents on the piperazine ring; a pyrrolidinyl group which may have 1 or 2 oxo groups as substituents on the pyrrolidine ring; and a phenoxy group such as phenyl, 2-methylphenyl, 3-methylphenyl, 10 4-methylphenyl, 2-ethylphenyl, 3-ethylphenyl, 4 ethylphenyl, 2-isopropylphenyl, 4-isopropylphenyl, 3 butylphenyl, 4-pentylphenyl, 4-hexylphenyl,' 3,4 dimethylphenyl, 3, 4-diethylphenyl, 2, 4-dimethylphenyl, 2, 5-dimethylphenyl, 2, 6-dimethylphenyl, 3,4,5 15 trimethylphenyl, 2-methoxyphenyl, 3-methoxyphenyl, 4 methoxyphenyl, 2-ethoxyphenyl, 3-ethoxyphenyl, 4 ethoxyphenyl, 4-isopropoxyphenyl, 3-butoxyphenyl, 4 pentyloxyphenyl, 4-hexyloxyphenyl, 3, 4-dimethoxyphenyl, 3,4-diethoxyphenyl, 2,4-dimethoxyphenyl, 2,5 20 dimethoxyphenyl, 2, 6-dimethoxyphenyl, 3,4,5 trimethoxyphenyl, 2-trifluoromethoxyphenyl, 3 trifluoromethoxyphenyl, 4-trifluoromethoxyphenyl, 2 (bromomethoxy)phenyl, 3- (2-chloroethoxy)phenyl, 4- (2,3 dichloropropoxy)phenyl, 4-(4-fluorobutoxy)phenyl, 3-(5 25 chloropentyloxy)phenyl, 4-(5-bromohexyloxy)phenyl, 4 (5, 6-dibromohexyloxy) phenyl, 3,4 di(trifluoromethoxy)phenyl, 3,4-di(4,4,4 trichlorobutoxy)phenyl, 2,4-di(3-chloro-2- 122 methoxypropyl)phenyl, 2,5-di(3-chloropropoxy)phenyl, 2,6-di(2,2,2-trifluoroethoxy)phenyl, 3,4,5 tri(trifluoromethoxy)phenyl, 4-(2,2,2 trichloroethoxy)phenyl, 2-methyl-4 5 trifluoromethoxyphenyl, 3-ethyl-4 trichloromethoxyphenyl, 2-methoxy-4 trifluoromethoxyphenyl, 3-ethoxy-4 trichloromethoxyphenyl, 2-methyl-3-trifluoromethoxy-4 trifluoromethoxyphenyl, 2-phenoxyphenyl, 3 10 phenoxyphenyl, 4-phenoxyphenyl, 2,3-diphenoxyphenyl, 3,4-diphenoxyphenyl, 2,6-diphenoxyphenyl, 3,4,5 triphenoxyphenyl, 2-methyl-4-phenoxyphenyl, 3-ethyl-4 phenoxyphenyl, 2-methoxy-4-phenoxyphenyl, 3-ethoxy-4 phenoxyphenyl, 2-methyl-3-phenoxy-4 15 trifluoromethoxyphenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2,3-dichlorophenyl, 2,4-dichlorophenyl, 2,5-dichlorophenyl, 3,4-dichlorophenyl, 2,6 dichlorophenyl, 3,5-dichlorophenyl, 2,4,6 trichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 4 20 fluorophenyl, 2,5-difluorophenyl, 2,4-difluorophenyl, 3,4-difluorophenyl, 3,5-difluorophenyl, 2,6 difluorophenyl, 2,4,6-tritluorophenyl, 2-bromophenyl, 3-bromophenyl, 4-bromophenyl, 2-iodophenyl, 3 iodophenyl, 4-iodophenyl, 2,3-dibromophenyl, 2,4 25 diiodophenyl, 4-methylthiophenyl, 4-cyclohexylphenyl, 4-chloro-2-anilinophenyl, 2-(4-chloro anilino)-5-ethoxy carbonylphenyl, 4-[2-(N,N-diethylamino)ethoxy]phenyl, 4-(4-methyl-1-piperazinyl)phenyl, 4-(2-oxo-1- 123 pyrrolidinyl)phenyl, 4-methylsulfonylaminophenyl, 4-(2 hydroxyethyl)phenyl, 4-benzylphenyl, 4-ethynylphenyl, 4-phenylthiophenyl, 4-(1-adamantyl)phenyl, 5 acetylamino-2-chlorophenyl, 2-propanoylaminophenyl, 3 5 cyanophenyl, 2-cyanophenyl, 4-cyanophenyl, 3,4 dicyanophenyl, and 3,4,5-tricyanophenyl groups. [0224] Examples of the phenyl lower alkyl group which may be substituted on the phenyl ring with 1 to 3 10 groups selected from the group consisting of a halogen atom, a lower alkoxy group which may have a halogen atom as a substituent, and a lower alkyl group include, in addition to the above described phenyl lower alkyl groups, phenylalkyl groups whose alkyl moiety is a 15 linear or branched alkyl group having 1 to 6 carbon atoms and which may be substituted on the phenyl ring with 1 to 3 groups selected from the group consisting of a halogen atom, a linear or branched alkoxy group having 1 to 6 carbon atoms which may have 1 to 3 20 halogen atoms as substituents, and a linear or branched alkyl group having 1 to 6 carbon atoms such as 4 fluorobenzyl, 2-chlorobenzyl, 3-chlorobenzyl, 4 chlorobenzyl, 2-(2-fluorophenyl)ethyl, 2-(4 fluorophenyl)ethyl, 2-(4-chlorophenyl)ethyl, 3,4 25 dibromobenzyl, 3,4-diiodobenzyl, 2,4-difluorobenzyl, 2,5-dichlorobenzyl, 2,6-dichlorobenzyl, 3,4,5 trifluorobenzyl, 3-(4-chlorophenyl)propyl, 1-(2 bromophenyl)ethyl, 4-(3-fluorophenyl)butyl, 5-(4- 124 iodophenyl)pentyl, 6-(4-chlorophenyl)hexyl, 1,1 dimethyl-2-(3-fluorophenyl)ethyl, 2-methyl-3-(4 chlorophenyl)propyl, 2-methylbenzyl, 2-(3 methylphenyl)ethyl, 3-(4-methylphenyl)propyl, 1-(2 5 ethylphenyl)ethyl, 4-(3-ethylphenyl)butyl, 5-(4 ethylphenyl)pentyl, 6-(4-isopropylphenyl)hexyl, 1,1 dimethyl-2-(3-butylphenyl)ethyl, 2-methyl-3-(4 pentylphenyl)propyl, 4-hexylbenzyl, 3,4-dimethylbenzyl, 3,4-diethylbenzyl, 2,4-dimethylbenzyl, 2,5 10 dimethylbenzyl, 2,6-dimethylbenzyl, 3,4,5 trimethylbenzyl, 2-methoxybenzyl, 2-(2 methoxyphenyl)ethyl, 2-(3-methoxyphenyl)ethyl, 2-(4 methoxyphenyl)ethyl, 4-methoxybenzyl, 1-(2 ethoxyphenyl).ethyl,. 3-(3-ethoxyphenyl)propyl, 4-(4 15 ethoxyphenyl)butyl, 5-(4-isopropoxyphenyl)pentyl, 6-(3 butoxyphenyl)hexyl, 1,1-dimethyl-2-(4 pentyloxyphenyl)ethyl, 2-methyl-3-(4 hexyloxyphenyl)propyl, 3,4-dimethoxybenzyl, 3,4 diethoxybenzyl, 2,4-dimethoxybenzyl, 2,5 20 dimethoxybenzyl, 2,6-dimethoxybenzyl, 3,4,5 trimethoxybenzyl, 2-trifluoromethoxybenzyl, 3 trifluoromethoxybenzyl, 4-trifluoromethoxybenzyl, 2-[2 (bromomethoxy)phenyllethyl, 1-[3-(2 chloroethoxy)phenyl]ethyl, 3-[4-(2,3 25 dichloropropoxy)phenyl]propyl, 4-[4-(4 fluorobutoxy)phenyl]butyl, 5-[3-(5 chloropentyloxy)phenyllpentyl, 6-[4-(5 bromohexyloxy)phenyl]hexyl, 1,1-dimethyl-2-[4-(5,6- 125 dibromohexyloxy)phenyllethyl, 3,4 di(trifluoromethoxy)benzyl, 3,4-di(4,4,4 trichlorobutoxy)benzyl, 2,4-di(3-chloro-2 methoxypropyl)benzyl, 2,5-di(3-chloropropoxy)benzyl, 5 2,6-di(2,2,2-trifluoroethoxy)benzyl, 3,4,5 tri(trifluoromethoxy)benzyl, 4-(2,2,2 trichloroethoxy)benzyl, 2-methyl-4 trifluoromethoxybenzyl, 3-ethyl-4 .trichloromethoxybenzyl, 2-methoxy-4 10 trifluoromethoxybenzyl, 3-ethoxy-4 trichloromethoxybenzyl, 2-methyl-3-trifluoromethoxy-4 trifluoromethoxybenzyl, 2-chloro-3-methylbenzyl, 4 fluoro-2-trifluoromethoxybenzyl, and 3-chloro-2-methyl 4-methoxybenzyl groups. 15 [0225] Examples of the phenyl lower alkyl group which has a lower alkylenedioxy group as a substituent on the phenyl ring include phenylalkyl groups which have a linear or branched alkylenedioxy group having 1 20 to 4 carbon atoms as a substituent on the phenyl ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as 3,4 methylenedioxybenzyl, 3,4-trimethylenedioxybenzyl, 2 (2,3-ethylenedioxyphenyl)ethyl, 1-(3,4 25 trimethylenedioxyphenyl)ethyl, 3-(2,3 tetramethylenedioxyphenyl)propyl, 4-(3,4 methylenedioxyphenyl)butyl, 5-(2,3 ethylenedioxyphenyl)pentyl, 6-(3,4- 126 trimethylenedioxyphenyl) hexyl, 1, 1-dimethyl-2- (2,3 metylenedioxyphenyl)ethyl, and 2-methyl-3-(3,4 ethylenedioxyphenyl)propyl groups. [02261 5 Examples of the amino group which may have a lower alkanoyl group as a substituent include amino groups which may have a linear or branched alkanoyl group having 1 to 6 carbon atoms as a substituent such as amino, N-acetylamino, N-formylamino, N 10 propionylamino, N-butyrylamino; N-isobutyrylamino, N pentanoylamino, N-tert-butylcarbonylamino, and N hexanoylamino groups. [0227] Examples of the 1,2,3,4-tetrahydroquinolyl 15 group which may have, on the tetrahydroquinoline ring, 1 to 3 substituents selected from the group consisting of an oxo group, a lower alkoxy group, and a lower alkylenedioxy group include 1,2,3,4-tetrahydroquinolyl groups which may have, on the tetrahydroquinoline ring, 20 1 to 3 substituents selected from the group consisting of an oxo group, a linear or branched alkoxy group having 1 to 6 carbon atoms, and a linear or branched alkylenedioxy group having 1 to 4 carbon atoms such as (1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl, 25 2-oxo-(l, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroquinolyl, 2-oxo-6,7-methylenedioxy-(1, 3, 4, 5 or 8-)1,2,3,4-tetrahydroquinolyl, 4-oxo-(l, 2, 3, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl, 2,4-dioxo-(l, 3, 127 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl, 2,4-dioxo 6,7-methylenedioxy-(1, 3, 5 or 8-)1,2,3,4 tetrahydroquinolyl, 5,6-ethylenedioxy-(1, 2, 3, 4, 7 or 8-)1,2,3,4-tetrahydroquinolyl, 7,8-trimethylenedioxy 5 (1, 2, 3, 4, 5 or 6-)1,2,3,4-tetrahydroquinolyl, 6,7 tetramethylenedioxy-(1, 2, 3, 4, 5 or 8-)1,2,3,4 tetrahydroquinolyl, 5-methoxy-2-oxo-(1, 3, 4, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl, and 2-oxo-6,7 ethylenedioxy-(l, 3, 4, 5 or 8-)1,2,3,4 10 tetrahydroquinolyl groups. [0228] Examples of the cycloalkyl lower alkyl group include cycloalkylalkyl groups having 3 to 16 carbon atoms whose alkyl moiety is a linear or branched alkyl 15 group having 1 to 6 carbon atoms such as cyclopropylmethyl, cyclohexylmethyl, 2 cyclopropylethyl, 1-cyclobutylethyl, 3 cyclopentylpropyl, 4-cyclohexylbutyl, 5 cycloheptylpentyl, 6-cyclooctylhexyl, 1,1-dimethyl-2 20 cyclononylethyl, 2-methyl-3-cyclodecylpropyl, cycloundecylmethyl, 2-cyclododecylethyl, 1 cyclotridecylethyl, 3-cyclotetradecylpropyl, 4 cyclopentadecylbutyl, and 5-cyclohexadecylpentyl groups. 25 [0229] Examples of the pyridyl lower alkyl group include pyridylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon 128 atoms such as (2, 3 or 4-)pyridylmethyl, 2-[(2, 3 or 4-)pyridyl]ethyl, 1-[(2, 3 or 4-)pyridyl]ethyl, 3-[(2, 3 or 4-)pyridyl]propyl, 4-[(2, 3 or 4-)pyridyl]butyl, 1,1-dimethyl-2-[(2, 3 or 4-)pyridyl]ethyl, 5-[(2, 3 or 5 4-)pyridyl]pentyl, 6-[(2, 3 or 4-)pyridyl]hexyl, 1-[(2, 3 or 4-)pyridyllisopropyl, and 2-methyl-3-[(2, 3 or 4-)pyridyl propyl groups. [0230] Examples of the amino group substituted lower 10 alkyl group which may have a substituent selected from the group consisting of a lower alkyl group and a lower alkanoyl group include linear or branched alkyl groups having 1 to 6 carbon atoms and an amino group which may have 1 or 2 substituents selected from the group 15 consisting of a linear or branched alkyl group having 1 to 6 carbon atoms and a linear or branched alkanoyl group having 1 to 6 carbon atoms such as aminomethyl, 2-aminoethyl, 1-aminoethyl, 3-aminopropyl, 4 aminobutyl, 5-aminopentyl, 6-aminohexyl, 1,1-dimethyl 20 2-aminoethyl, 2-methyl-3-aminopropyl, methylaminomethyl, 1-ethylaminoethyl, 2 propylaminoethyl, 3-isopropylaminopropyl, 4 butylaminobutyl, 5-pentylaminopentyl, 6 hexylaminohexyl, dimethylaminomethyl, 2 25 diisopropylaminoethyl, (N-ethyl-N-propylamino)methyl, 2-(N,N-dimethylamino)ethyl, 2-(N-methyl-N-hexylamino) ethyl, formylaminomethyl, acetylaminomethyl, 1 propionylaminoethyl, 2-acetylaminoethyl, 3- 129 butyrylaminopropyl, 4-pentanoylaminobutyl, 5 hexanoylaminopentyl, 6-acetylaminohexyl, N-methyl-N acetylaminomethyl, 2-(N-ethyl-N-propanoylamino)ethyl, (N-ethyl-N-butyrylamino)methyl, 2-(N-methyl-N 5 hexanoylamino)ethyl, and 3-(N,N-dimethylamino)propyl groups. [0231] Examples of the lower alkoxy lower alkyl group include linear or branched alkyl groups having 1 10 to 6 carbon atoms which have a linear or branched alkoxy group having 1 to 6 carbon atoms, as a substituent such as methoxymethyl, 1-ethoxyethyl, 2 methoxyethyl, 2-propoxyethyl, 3-isopropoxypropyl, 4 butoxybutyl, 5-pentyloxypentyl, 6-hexyloxyhexyl, 1,1 15 dimethyl-2-methoxyethyl, 2-methyl-3-ethoxypropyl, and 3-methoxypropyl groups. [0232] Examples of the 1,2,3,4 tetrahydroisoquinolylcarbonyl substituted lower alkyl 20 group include 1,2,3, 4-tetrahydroisoquinolylcarbonyl alkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroisoquinolylcarbonylmethyl, 2-((1, 2, 3, 4, 5, 25 6, 7 or 8-)1,2,3,4-tetrahydroisoquinolylcarbonyllethyl, 1-[((l, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroisoquinolylcarbonyl)ethyl, 3-[(l, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4- 130 tetrahydroisoquinolylcarbonyl]propyl, 4-[(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroisoquinolylcarbonyl]butyl, 1,1-dimethyl-2 [(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 5 tetrahydroisoquinolylcarbonyl]ethyl, 5-[(1, 2, 3, 4, 5, 6, 7 or 8-) 1,2,3,4 tetrahydroisoquinolylcarbonyl]pentyl, 6-[(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroisoquinolylcarbonyllhexyl, 1-[(1, 2, 3, 4, 5, 10 6, 7 or 8-)1,2,.3,4 tetrahydroisoquinolylcarbonyllisopropyl, and 2-methyl 3-[(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroisoquinolylcarbonyllpropyl groups. [0233] 15 Examples of the piperidinylcarbonyl group which may have, on the piperidine ring, a substituent selected from the group consisting of a lower alkoxycarbonyl group, a phenyl lower alkyl group, and a furyl lower alkyl group include piperidinylcarbonyl 20 groups which may have, on the piperidine ring, 1 to 3 substituents selected from the group consisting of an alkoxycarbonyl group whose alkoxy moiety is a linear or branched alkoxy group having 1 to 6 carbon atoms, a phenylalkyl group whose alkyl moiety is a linear or 25 branched alkyl group having 1 to 6 carbon atoms, and a furylalkyl group whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (1, 2, 3 or 4-)piperidinylcarbonyl, 1-benzyl-(2, 3 or 131 4-)piperidinylcarbonyl, 1-(2 or 3-)furylmethyl-(2, 3 or 4-)piperidinylcarbonyl, 1-(2-phenylethyl)-(2, 3 or 4-)piperidinylcarbonyl, 1-12-[(1 or 2-)furyl]ethyl}-(2, 3 or 4-)piperidinylcarbonyl, 1-(1-phenylethyl)-(2, 3 or 5 4-)piperidinylcarbonyl, 1-{3-((1 or 2-)furyl]propyl]} (2, 3 or 4-)piperidinylcarbonyl, 1-(3-phenylpropyl)-(2, 3 or 4-)piperidinylcarbonyl, 1-(1-[(1 or 2-)furyl]ethyl]}-(2,. 3 or 4-)pfperidinylcarbonyl, 1-(4 phenylbutyl)-(2, 3 or 4-)piperidinylcarbonyl, 1-{4-[(1 10 or 2-)furyl]butyl]}-(2, 3 or 4-)piperidinylcarbonyl, 1 (5-phenylpentyl)-(2, 3 or 4-)piperidinylcarbonyl, 1-{5 [(1 or 2-)furyl]pentyl]}-(2, 3 or 4-)piperidinylcarbonyl, 1-(6-phenylhexyl)-(2, 3 or 4-)piperidinylcarbonyl, 1-16-[(1 or 2-)furyl]hexyl]} 15 (2, 3 or 4-)piperidinylcarbonyl, 1,2-dibenzyl-(3, 4, 5 or 6-)piperidinylcarbonyl, 1,3-di(1 or 2-)furylmethyl (2, 4, 5 or 6-)piperidinylcarbonyl, 1,3,5-tribenzyl-(2, 4 or 6-)piperidinylcarbonyl, 1,2,6-tri(1 or 2-)furylmethyl-(3, 4 or 5-)piperidinylcarbonyl, 1 20 benzyl-3-(1 or 2-)furylmethyl-(2, 4, 5 or 6-)piperidinylcarbonyl, 1-{1-[(1 or.2-)furyl]ethyll (2, 3 or 4-)piperidinylcarbonyl, 1-methoxycarbonyl-(2, 3 or 4-)piperidinylcarbonyl, 1-ethoxycarbonyl-(2, 3 or 4-)piperidinylcarbonyl, 1-propoxycarbonyl-(2, 3 or 25 4-)piperidinylcarbonyl, 1-butoxycarbonyl-(2, 3 or 4-)piperidinylcarbonyl, 1-tert-butoxycarbonyl-(2, 3 or 4-)piperidinylcarbonyl, 1-pentyloxycarbonyl-(2, 3 or 4-)piperidinylcarbonyl, 1-hexyloxycarbonyl-(2, 3 or 132 4-)piperidinylcarbonyl, 1,2-dimethoxycarbonyl-(3, 4, 5 or 6-)piperidinylcarbonyl, 1,2,6-triethoxycarbonyl-(3, 4 or 5-)piperidinylcarbonyl, 1-(1 or 2-)furylmethyl-3 tert-butoxycarbonyl-(3, 4, 5 or 6-)piperidinylcarbonyl, 5 1-benzyl-2-methoxycarbonyl-(2, 4, 5 or 6-)piperidinylcarbonyl, and 1-(1 or 2-)furylmethyl-2,4 dimethoxycarbonyl-(3, 5 or 6-)piperidinylcarbonyl groups. [02341 10 Examples of the thiazolidinyl lower alkanoyl group which may have an oxo group as a substituent on the thiazolidine ring include thiazolidinylalkanoyl groups which may have 1 to 3 oxo groups as substituents on the thiazolidine ring and whose alkanoyl moiety is' a 15 linear or branched alkanoyl group .having 2 to 6 'carbon atoms such as 2-[(2, 3, 4 or 5-)thiazolidinyllacetyl, 3-[(2, 3, 4 or 5-)thiazolidinyl]propionyl, 2-[(2, 3, 4 or 5-)thiazolidinyl]propionyl, 4-((2, 3, 4 or 5-)thiazolidinyl]butyryl, 5-[(2, 3, 4 or 5-)1,2,4 20 thiazolidinyl]pentanoyl, 6-[(2, 3, 4 or 5-)thiazolidinyl]hexanoyl, 2,2-dimethyl-3-[(2, 3, 4 or 5-)thiazolidinyl]propionyl, 2-methyl-3-[(2, 3, 4 or 5-)thiazolidinyl]propionyl, 2,*4-dioxo-(3 or 5-)thiazolidinylacetyl, 3-[2-oxo-(3, 4 or 25 5-)thiazolidinyl]propionyl, 2-[4-oxo-(2, 3 or 5-)thiazolidinyllpropionyl, 4-[5-oxo-(2, 3 or 4-)thiazolidinyl]butyryl, 5-[2,5-dioxo-(3 or 4-)thiazolidinyl]pentanoyl, 6-[2,4,5-trioxo-3- 133 thiazolidinyl ]hexanoyl, 2- [4, 5-dioxo- (2 or 3-)thiazolidinyl) acetyl, 2,2-dimethyl-3-(2,4-dioxo-(3 or 5-)thiazolidinyllpropionyl, and 2-methyl-3-[2,4 dioxo-(3 or 5-)thiazolidinyl]propionyl groups. 5 [0235] Examples of the piperidinyl group which may be substituted on the piperidine ring with a group selected from the group consisting of a lower alkoxycarbonyl group, a phenyl lower alkyl group, a 10 lower alkyl group, a benzoyl group and a furyl lower alkyl group include piperidinyl groups which may be substituted on the piperidine ring with 1 to 3 groups selected from the group consisting of an alkoxycarbonyl group whose 'alkoxy moiety is a linear or branched 15 alkoxy group having 1 to 6 carbon atoms, a phenylalkyl group whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms, a linear or branched alkyl group having 1 to 6 carbon atoms, a benzoyl group, and a furylalkyl group whose alkyl moiety is a 20 linear or branched alkyl group having 1 to 6 carbon atoms such as (1, 2, 3 or 4-)piperidinyl, 1-benzyl-(2, 3 or 4-)piperidinyl, 1-(2 or 3-)furylmethyl-(2, 3 or 4-)piperidinyl, 1-(2-phenylethyl)-(2, 3 or 4-)piperidinyl, 1-12-[(1 or 2-)furyl]ethyl}-(2, 3 or 25 4-)piperidinyl, 1-(1-phenylethyl)-(2, 3 or 4-)piperidinyl, 1-{3-[(l or 2-)furyllpropyl]}-(2, 3 or 4-)piperidinyl, 1-(3-phenylpropyl)-(2, 3 or 4-)piperidinyl, 1-{1-[(1 or 2-)furyl]ethyl]}-(2, 3 or 134 4-)piperidinyl, 1-(4-phenylbutyl)-(2, 3 or 4-)piperidinyl, 1-{4-[(l or 2-)furyllbutyl])-(2, 3 or 4-)piperidinyl, 1-C5-phenylpentyl)-(2, 3 or 4-)piperidinyl, 1-{5-[(1 or 2-)furyllpentyl}--(2, 3 or 5 4-)piperidinyl, 1-(6-phenylhexyl)-(2, 3 or 4-)piperidinyl, 1-16-[I(l or 2-)furyl]hexyl]}-(2, 3 or 4-)piperidinyl, 1,2-dibenzyl-(3,. 4, 5 or 6-)piperidinyl, 1,3-di(1 or 2-)furylmethyl-(2, 4, 5 or 6-)piperidinyl, -1,3,5-tribenzyl-(2, 4 or 10 6-)piperidinyl, 1,2,6-tri(1 or 2-)furylmethyl-(3, 4 or 5-)piperidinyl, 1-benzyl-3-C1 or 2-)furylmethyl-(2, 4, 5 or 6-)piperidinyl, 1-{1-[(1 or 2-)furyljethylfl-(2, 3 or 4-)piperidinyl, 1-benzoyl-C2, 3 or 4-)piperidinyl, 1,2-dibenzoyl-(3, 4, 5 or 6-)piperidinyl, 1,3,5 15 tribenzoyl-(2, 4 or 6-)piperidinyl, 1-methyl-(2,' 3 or 4-)piperidinyl, 1-ethyl-(2, 3 or 4-)piperidinyl, 1 propyl-(2, 3 or 4-)piperidinyl, 1-isopropyl-(2, 3 or 4-)piperidinyl, 1-butyl-(2, 3 or 4-)piperidinyl, 1 isobutyl-(2, 3 or 4-)piperidinyl, 1-tert-butyl-(2, 3 or 20 4-)pipericiinyl, 1-pentyl-(2, 3 or 4-)piperidinyl, 1 hexyl-(2, 3 or 4-)piperidinyl, 1,2-dimethyl-(3, 4, 5 or 6-)piperidiiyl, 1,2, 6-trimethyl-(3, 4 or 5-)piperidinyl, 1-methyl-3-benzyl-C3, 4, 5 or 6-)piperidinyl, 1-benzoyl-2-methyl-(2, 4, 5 or 25 6-)piperidinyl, 1-(l or 2-)furylmethyl-2,4-dimethyl-(3, 5 or 6-)piperidinyl, 1-methoxycarbonyl-(2, 3 or 4-)piperidinyl, 1-ethoxycarbonyl-(2, 3 or 4-)piperidinyl, 1-propoxycarbonyl-(2, 3 or 135 4-)piperidinyl, 1-butoxycarbonyl-(2, 3 or 4-)piperidinyl, 1-tert-butoxycarbonyl-(2, 3 or 4-)piperidinyl, 1-pentyloxycarbonyl-(2, 3 or 4-)piperidinyl, 1-hexyloxycarbonyl-(2, 3 or 5 4-)piperidinyl, 1,2-dimethoxycarbonyl-(3, 4, 5 or 6-)piperidinyl, 1,2,6-triethoxycarbonyl-(3, 4 or 5-)piperidinyl, 1-methyl-3-tert-butoxycarbonyl-(3, 4, 5 or 6-)piperidinyl, 1-benzoyl-2-methoxycarbonyl-(2, 4, 5 or 6-)piperidinyl, 1-(1 or 2-)furylmethyl-2,4 10 dimethoxycarbonyl-(3, 5 or 6-)piperidinyl, and 1 benzyl-2,4-dimethoxycarbonyl-(3, 5 or 6-)piperidinyl groups. [0236] Examples of the carbonyl lower alkyl group 15 substituted with a group: (0237] [Formula 54] -NW [0238] (hereinafter called "A group") include A group 20 substituted carbonylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as A group substituted carbonylmethyl, 2-A group substituted carbonylethyl, 1-A group substituted carbonylethyl, 3-A group substituted carbonylpropyl, 4 25 A group substituted carbonylbutyl, 1,1-dimethyl-2-A 136 group substituted carbonylethyl, 5-A group substituted carbonylpentyl, 6-A group substituted carbonylhexyl, 1 A group substituted carbonylisopropyl, and 2-methyl-3-A group substituted carbonylpropyl groups. 5 [0239] Examples of the carbonyl lower alkyl group substituted with a group: [0240] [Formula 55] NQQ ii( 3 4 X 10 (0241] wherein R3 4 is an oxo group or a phenyl group, and d is an integer of 0 to 3 (hereinafter called "B group"), include B group substituted carbonylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 15 1 to 6 carbon atoms such as B group substituted carbonylmethyl,- 2-B group substituted carbonylethyl, 1 B group substituted carbonylethyl, 3-B group substituted carbonylpropyl, 4-B group substituted carbonylbutyl, 1,1-dimethyl-2-B group substituted 20 carbonylethyl, 5-B group substituted carbonylpentyl, 6 B group substituted carbonylhexyl, 1-B group substituted carbonylisopropyl, and 2-methyl-3-B group substituted carbonylpropyl groups. (0242] 25 Examples of the pyrrolidinyl lower alkyl 137 group include pyrrolidinylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (1-, 2-, or 3-)pyrrolidinylmethyl, 2-[(1-, 2-, or 5 3-)pyrrolidinyl)ethyl, 1-[(1-, 2-, or 3-)pyrrolidinyl]ethyl, 3-[(1-, 2-, or 3-)pyrrolidinyl]propyl, 4-[(1-, 2-, or 3-)pyrrolidinyl]butyl, 5-[(1-, 2-, or 3-)pyrrolidinyllpentyl, 6-[(1-, 2-, or 10 3-)pyrrolidinyl]hexyl, 1,1-dimethyl-2-[(1-, 2-, or 3-)pyrrolidinyl]ethyl, and 2-methyl-3-[(1l-, 2-, or 3-)pyrrolidinyl]propyl groups. [0243] Examples of the morpholino lower alkyl group 15 include morpholinoalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (2-, 3-or 4-)morpholinomethyl, 2-[(2-, 3 or 4-)morpholino]ethyl, 1-[(2-, 3-or 4-)morpholino]ethyl, 3-[(2-, 3-or 20 4-)morpholino]propyl, 4-[(2-, 3-or 4-)morpholino]butyl, 5-[(2-, 3-or 4-)morph.olino]pentyl, 6-[(2-, 3-or 4-)morpholinolhexyl, 1,1-dimethyl-2-[(2-, 3-or 4-)morpholino]ethyl, and 2-methyl-3-[(2-, 3-or 25 4-)morpholino]propyl groups. [0244] Examples of the phenyl lower alkenyl group include phenylalkenyl groups whose alkenyl moiety is a 138 linear or branched alkenyl group having 2 to 6 carbon atoms and which have 1 to 3 double bonds such as styryl, 3-phenyl-2-propenyl group (trivial name: cinnamyl group), 4-phenyl-2-butenyl, 4-phenyl-3 5 butenyl, 5-phenyl-4-pentenyl, 5-phenyl-3-pentenyl, 6 phenyl-5-hexenyl, 6-phenyl-4-hexenyl, 6-phenyl-3 hexenyl, 4-phenyl-1,3-butadienyl, and 6-phenyl-1,3,5 hexatrienyl groups. [0245) 10 Examples of the anilinocarbonyl lower alkyl group which may have a lower alkyl group as a substituent on the phenyl ring include anilinocarbonylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon 15 atoms and which may have 1 to 3 linear or branched alkyl groups having 1 to 6 carbon atoms as substituents on the phenyl ring such as anilinocarbonylmethyl, 2 anilinocarbonylethyl, 1-anilinocarbonylethyl, 3 anilinocarbonyl-propyl, 4-anilinocarbonylbutyl, 5 20 anilinocarbonylpentyl, 6-anilinocarbonylhexyl, 1,1 dimethyl-2-anilinocarbonylethyl, 2-methyl-3 anilinocarbonylpropyl, (4-methylanilinocarbonyl)methyl, 2-(3-methylanilinocarbonyl)ethyl, 3-(4 methylanilinocarbonyl)propyl, 1-(2 25 ethylanilinocarbonyl)ethyl, 4-(3 ethylanilinocarbonyl)butyl, 5-(4 ethylanilinocarbonyl)pentyl, 6-(4 isopropylanilinocarbonyl)hexyl, 1,1-dimethyl-2-(3- 139 butylanilinocarbonyl)ethyl, 2-methyl-3-(4 pentylanilinocarbonyl)propyl, 4 hexylanilinocarbonylmethyl, 3,4 dimethylanilinocarbonylmethyl, 3,4 5 diethylanilinocarbonylmethyl, 2,4 dimethylanilinocarbonylmethyl, 2,5 dimethylanilinocarbonylmethyl, 2,6 dimethylanilinocarbonylmethyl, and 3,4,5 trimethylanilinocarbonylmethyl groups. 10 [0246] Examples of the piperazinyl lower alkyl group which may have, on the piperazine ring, a substituent selected from the group consisting of a lower alkyl group and a phenyl lower alkyl group which may have a 15 lower alkylenedioxy group as a substituent on the phenyl ring include piperazinylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms and which may have, on the piperazine ring, 1 to 3 substituents selected from the group 20 consisting of a linear or branched alkyl group having 1 to 6 carbon atoms and a phenylalkyl group which may have a linear or branched alkylenedioxy group having 1 to 4 carbon atoms as a substituent on the phenyl ring and whose alkyl moiety is a linear or branched alkyl 25 group having 1 to 6 carbon atoms such as [(1-, 2-or 3-)piperazinyllmethyl, 2-[(1-, 2-or 3-)piperazinyl]ethyl, 1-[ (1-, 2-or 3-)piperazinyl]ethyl, 3-[ (1-, 2-or 140 3-)piperazinyljpropyl, 4-[(l-, 2-or 3-)piperazinyl]butyl, 5-((1-, 2-or 3-)piperazinyl]pentyl, 6-[(1-, 2-or 3-)piperazinyl]hexyl, 1,1-dimethyl-2-[(l-, 2-or 5 3-)piperazinyl]ethyl, 2-methyl-3-[(1-, 2-or 3-)piperazinyl]propyl, [1-methyl-(2-, 3-or 4-)piperazinyllmethyl, 2-[l-ethyl-(2-, 3-or 4-)piperazinyl]ethyl, 1-[4-propyl-(1-, 2-or 3-)piperazinyllethyl, 3-[3-isopropyl-(1-, 2-, 4-, 5-or 10 6-)piperazinyl]propyl, 4-[2-butyl-(1-, 3-, 4-, 5-or 6-)piperazinyljbutyl, 5-[l-isobutyl-(2-, 3-or 4-)piperazinyl]pentyl, 3-[4-methyl-(1-, 2-or 3-)piperazinyljpropyl, 6-[1-tert-butyl-(2-, 3-or 4-)piperazinyllhexyl, 1,1-dimethyl-2-[4-pentyl-(l-, 2 15 or 3-)piperazinyllethyl, [1,2-dimethyl-(3-, 4-, 5-or 6-)piperazinyllmethyl, [1,2,6-trimethyl-(3-, 4-or 5-)piperazinyl]methyl, and 2-[4-(3,4 methylenedioxybenzyl)-(1-, 2-or 3-)piperazinyl]ethyl groups. 20 [0247] Examples of the amidino lower alkyl group which may have a lower alkyl group as a substituent include amidinoalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon 25 atoms and which may have 1 or 2 linear or branched alkyl groups having 1 to 6 carbon atoms such as amidinomethyl, 2-amidinoethyl, 1-amidinoethyl, 3 amidinopropyl, 4-amidinobutyl, 5-amidinopentyl, 6- 141 amidinohexyl, 1, 1-dimethyl-2-amidinoethyl, 2-methyl-3 amidinopropyl, N,N-dimethylamidinomethyl, 2-(N,N dimethylamidino)ethyl, 1-(N-methylamidino)ethyl, 3-(N ethylamidino)propyl, 4-(N-n-propylamidino)propyl, 5-(N 5 n-pentylamidino)pentyl, 6- (N-n-hexylamidino) hexyl, and (N-methyl-N-ethylamidino)methyl groups. [0248] Examples of the carbazolyl group which may have a lower alkyl group as a substituent on the 10 carbazole ring include carbazolyl groups which may have 1 to 3 linear or branched alkyl groups having 1 to 6 carbon atoms as substituents on the carbazole ring such as (1-, 2-, 3-or 4-)carbazolyl, 9-methyl-(1-, 2-, 3-or 4-)carbazolyl, 9-ethyl-(1-, 2-, 3-or 4-)carbazolyl, 1 15 ethyl-(2-, 3-, 4-, 5-, 6-, 7-, 8-or 9-)carbazolyl, 2-n propyl-(i-, 3-, 4-, 5-, 6-, 8-or 9-)carbazolyl, 3-n butyl-(1-, 2-, 4-, 5-, 6-, 7-, 8-or 9-)carbazolyl, 4-n pentyl-(1-, 2-, 3-, 5-, 6-, 7-, 8-or 9-)carbazolyl, -5-n-hexyl-(1-, 2-, 3-, 4-, 6-, 7-, 8-or 20 9-)carbazolyl, 6,9-dimethyl-(1-, 2-, 3-, 4-, 5-, 7-or 8-)carbazolyl, and 1,7,8-trityl-(2-, 3-, 4-, 5-, 6-, 7-, 8-or 9-)carbazolyl groups. [0249] Examples of the amidino group which may have 25 a lower alkyl group as a substituent include amidino groups which may have 1 or 2 linear or branched alkyl groups having 1 to 6 carbon atoms as substituents such as amidino, N,N-dimethylamidino, N-methylamidino, N- 142 ethylamidino, N-n-propylamidino, N-n-butylamidino, N-n pentylamidino, N-n-hexylamidino, N,N-diethylamidino, and N-methyl-N-ethylamidino groups. Examples of the phenyl lower alkyl group 5 (which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a lower alkylenedioxy group and a lower alkoxy group), include, in addition to the above described phenyl lower alkyl groups, phenylalkyl groups whose alkyl 10 moiety is a linear or branched alkyl group having 1 to 6 carbon atoms (and which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a linear or branched alkylenedioxy group having 1 to 4 carbon atoms and a linear or branched alkoxy group 15 having 1 to 6 carbon atoms) such as 3,4 methylenedioxybenzyl, 3,4-trimethylenedioxybenzyl, 2 (2,3-ethylenedioxyphenyl)ethyl, 1-(3,4 trimethylenedioxyphenyl)ethyl, 3-(2,3 tetramethylenedioxyphenyl)propyl, 4-(3,4 20 methylenedioxyphenyl)butyl, 5-(2,3 ethylenedioxyphenyl)pentyl, 6-(3,4 trimethylenedioxyphenyl)hexyl, 1,1-dimethyl-2-(2,3 methylenedioxyphenyl)ethyl, 2"methyl-3-(3,4 ethylenedioxyphenyl)propyl, 2-methoxybenzyl, 2-(2 25 methoxyphenyl)ethyl, 2-(3-methoxyphenyl)ethyl, 2-(4 methoxyphenyl)ethyl, 4-methoxybenzyl, 1-(2 ethoxyphenyl)ethyl, 3-(3-ethoxyphenyl)propyl, 4-(4 ethoxyphenyl)butyl, 5-(4-isopropoxyphenyl)pentyl, 6-(3- 143 butoxyphenyl)hexyl, 1,1-dimethyl-2-(4 pentyloxyphenyl)ethyl, 2-methyl-3-(4 hexyloxyphenyl)propyl, 3,4-dimethoxybenzyl, 3,4 diethoxybenzyl, 2,4-dimethoxybenzyl, 2,5 5 dimethoxybenzyl, 2,6-dimethoxybenzyl, and 3,4,5 trimethoxybenzyl groups. [0250] Examples of the piperazinyl substituted oxalyl group which may have, on the piperazine ring, 1 10 to 3 substituents selected from the group consisting of a phenyl lower alkyl group (which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a lower alkylenedioxy group and a lower alkoxy group) and a pyridyl lower alkyl group 15 include piperazinyl substituted oxalyl groups which may have, on the piperazine ring, 1 to 3 substituents selected from the group consisting of a phenylalkyl group whose alkyl moiety is a linear or branched alkyl group having 1 -to 6 carbon atoms (and which may have, 20 on the phenyl ring, 1 to 3 substituents selected from the group consisting of a linear or branched alkylenedioxy group having 1 to 4 carbon atoms and a linear or branched alkoxy group having 1 to 6 carbon atoms) and a pyridylalkyl group whose alkyl moiety is a 25 linear or branched alkyl group having 1 to 6 carbon atoms such as 4-(3,4-methylenedioxybenzyl)-(1-, 2-or 3-)piperazinyloxalyl, 4-(2-, 3-or 4-pyridylmethyl) (1-, 2-or 3-)piperazinyloxalyl, 4-(3,4- 144 dimethoxybenzyl)-(1-, 2-or 3-)piperazinyloxalyl, 4 (2, 3-methylenedioxybenzyl) -(1-, 2-or 3-)piperazinyloxalyl, 4-(3,4-ethylenedioxybenzyl)-(1-, 2-or 3-)piperazinyloxalyl, 4-[2-(2-, 3-or 4 5 pyridyl)ethyl]-(1-, 2-or 3-)piperazinyloxalyl, 4-[3 (2-, 3-or 4-pyridyl)propyl-(1-, 2-or 3-)piperazinyloxalyl, 2,4-bis(2-, 3-or 4 pyridylmethyl)-(l-, .2-or 3-)piperazinyloxalyl, 2-(3,4 methylenedioxybenzyl)-4-(2-,. 3-or 4-pyridylmethyl) 10 (1-, 2-or 3-)piperazinyloxalyl, and 2,3,4-tri(2-, 3-or 4-pyridylmethyl)-(1-, 2-or 3-)piperazinyloxalyl groups. [0251] Examples of the cyano substituted lower alkyl group include cyanoalkyl groups whose alkyl moiety is a 15 linear or branched alkyl group having 1 to 6 carbon atoms such as cyanomethyl, 2-cyanoethyl, 1-cyanoethyl, 3-cyanopropyl, 4-cyanobutyl, 5-cyanopentyl, 6 cyanohexyl, 1,1-dimethyl-2-cyanoethyl, and 2-methyl-3 cyanopropyl groups. 20 (0252] Examples of the 5-to 7-membered saturated heterocyclic ring formed by binding R3 and R3 each other, together with nitrogen atoms bound to them, through or not through a nitrogen atom, an oxygen atom, 25 or a sulfur atom include pyrrolidinyl, piperidinyl, piperazinyl, morpholino, thiomorpholino, and homopiperazinyl groups. [0253] 145 Examples of the 5-to 10-membered saturated or unsaturated heterocyclic ring formed by binding R 14 and R1 5 each other, together with nitrogen atoms bound to them, through or not through a nitrogen atom, an oxygen 5 atom, or a sulfur atom include 1,2,3,4,5,6 hexahydropyrimidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholino, thiomorpholino, homopiperazinyl, homopiperidinyl, thiazolidinyl, 1,2,5,6-tetrahydropyridyl, pyrrolyl, pyrazolyl, 10 imidazolyl, 2-pyrrolinyl, 2-imidazolinyl, imidazolidinyl, 2-pyrazolinyl, pyrazolidinyl, 1,2 dihydropyridyl, 1,2-dihydroquinolyl, 1,2,3,4 tetrahydroquinolyl, 1,2,3,4-tetrahydroisoquinolyl, 1,2 dihydroisoquinolyl, indolyl, isoindolyl, indolinyl, 15 isoindolinyl, 3,4-dihydro-2H-1,4-benzooxazinyl, 3,4 dihydro-2H-1,4-benzothiazolidinyl, 1,4-benzothiazinyl, 1,2,3,4-tetrahydroquinoxalinyl, 1,2,3,4 tetrahydrocinnolinyl, 1,2,3,4-tetrahydrophthalazinyl, 1,2,3,4-tetrahydroquinazolinyl, 1,2 20 dihydroquinoxalinyl, 3,4-dihydroquinoxalinyl, 1,4 dihydroquinoxalinyl, 1,2-dihydrocinnolinyl, 1,2 dihydrophthalazinyl, 3,4-dihydrophthalazinyl, 1,2 dihydroquinazolinyl, 3,4-dihydroquinazolinyl, indazolyl, indazolinyl, 6-azabicyclo[3,2,1]octyl, 3 25 aza-spiro[5,5)undecyl, and thiazolidinyl groups. Preferably, R' and R , together with the nitrogen atom to which they bind, bind to each other, directly or via a nitrogen atom to form a 6-membered saturated 146 heterocyclic group. Most preferably, they include piperidinyl and piperazinyl groups. [0254] Examples of the phenyl lower alkoxy group 5 include phenylalkoxy groups whose alkoxy moiety is a linear or branched alkoxy group having 1 to 6 carbon atoms such as benzyloxy, 2-phenylethoxy, 1 phenylethoxy, 3-phenylpropoxy, 4-phenylbutoxy, 5 phenylpentyloxy, 6-phenylhexyloxy, 1,1-dimethyl-2 10 phenylethoxy, and 2-methyl-3-phenylpropoxy groups. [0255] Examples of the phenyl substituted lower alkyl group which has 1 or 2 phenyl groups which may be substituted on the phenyl ring with 1 to 3 substituents 15 selected from the group consisting of a lower alkanoyl group, an amino group which may have a lower alkanoyl group as a substituent, a lower alkoxycarbonyl group, a cyano group, a nitro group, a phenyl group, a halogen atom, a lower alkyl group which may have a halogen atom 20 as a substituent, a lower alkoxy group which may have a halogen atom as a substituent, a phenyl lower alkoxy group, a hydroxyl group, and a lower alkylenedioxy groups; and which may have a pyridyl group on the lower alkyl group include in addition to the above described 25 phenyl lower alkyl groups, phenyl substituted alkyl groups which have 1 or 2 phenyls which may be substituted on the phenyl ring with 1 to 3 substituents selected from the group consisting of a linear or 147 branched alkanoyl group having 1 to 6 carbon atoms, an amino group which may have 1 or 2 linear or branched alkanoyl groups having 1 to 6 carbon atoms as substituents, an alkoxycarbonyl group whose akloxy 5 moiety is a linear or branched alkoxy group having I to 6 carbon atoms, a cyano group, a nitro group, a phenyl group, a halogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents, a linear or branched 10 alkoxy group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents, a phenylalkoxy groups whose alkoxy moiety is a linear or branched alkoxy group having 1 to 6 carbon atoms, a hydroxy group, and a linear or branched alkylenedioxy group 15 having 1 to 4 carbon atoms; which.may have a pyridyl group on the alkyl group, and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms, such as 1-phenyl-1-(2, 3 or 4-)pyridyl methyl, 1,1-diphenylmet-hyl, 1,1-di(4-fluorophenyl)methyl, 1 20 phenyl-1-(4-methoxyphenyl)methyl, 3,4 methylenedioxybenzyl, 3, 4-ethylenedioxybenzyl, 3, 4 trimethylenedioxybenzyl, 2,5-difluorobenzyl, 2,4 difluorobenzyl, 3,4-difluorobenzyl, 3,5-difluorobenzyl, 2,6-difluorobenzyl, 3-trifluoromethylbenzyl, 2 25 trifluoromethylbenzyl, 4-trifluoromethylbenzyl, 3,4 dimethoxybenzyl, 3, 5-dimethoxybenzyl, 2-chlorobenzyl, 3-chlorobenzyl, 4-chlorobenzyl, 2-methylbenzyl, 3 methylbenzyl, 4-methylbenzyl, 3, 4-dimethylbenzyl, 2,3- 148 dimethylbenzyl, 2-methoxybenzyl, 3-methoxybenzyl, 4 cyanobenzyl, 2-cyanobenzyl, 3-cyanobenzyl, 4 methoxybenzyl, 2,3-dichlorobenzyl, 2,4-dichlorobenzyl, 2, 5-dichlorobenzyl, 3, 4-dichlorobenzyl, 2,6 5 dichlorobenzyl, 4-fluorobenzyl, 3-fluorobenzyl, 2 fluorobenzyl, 4-nitrobenzyl, 3-nitrobenzyl, 2 nitrobenzyl, 3-trifluoromethoxybenzyl, 4 trifluoromethoxybenzyl, 2-trifluoromethoxybenzyl, 4 methoxycarbonylbenzyl, 3-methoxycarbonylbenzyl, 4-tert 10 butylbenzyl, 4-ethylbenzyl, 4-isopropylbenzyl, 4 methoxy-3-chlorobenzyl, 2-(4-methoxyphenyl)ethyl, 2-(4 fluorophenyl)ethyl, 2-(4-chlorophenyl)ethyl, 2-(3 methoxyphenyl)ethyl, 2-(4-methylphenyl)ethyl, 4 phenylbenzyl, 3, 3-diphenylpropyl, 3-methyl-4 15 nitrobenzyl, 4-(4-methoxyphenyl)butyl, 2-(4 methylphenyl) ethyl, 4-tert-butoxycarbonylbenzyl, 3 -chloro-6-methoxybenzyl, 4-acetylaminobenzyl, 4-nitro-3 methylbenzyl, 4-hydroxybenzyl, 3-hydroxybenzyl, 2 hydroxybenzyl, 4-tert-butyrylbenzyl, 4-benzyloxybenzyl, 20 4-pivaloylbenzyl, 2-(4-acetylphenyl)ethyl, 1-(3 propionylphenyl)ethyl, 3-(2-butyrylphenyl)propyl, 4-(4 pentanoylphenyl)butyl, 5-(3-hexanoylphenyl)pentyl, 6 (2,4-diacetylphenyl)hexyl, 1,1-dimethyl-2-(2,4,6 triacetylphenyl)ethyl, 2-methyl-3-(3,4 25 diacetylphenyl)propyl, 2-(4-aminophenyl)ethyl, 1-(3 propionylaminophenyl) ethyl, 3- (2 butyrylaminophenyl)propyl, 4-(4 pentanoylamino)phenylbutyl, 5- 149 (hexanoylaminophenyl)pentyl, 6-(N-acetyl-N propionylaminophenyl)hexyl, 1,1-dimethyl-2-(3,4 diaminophenyl)ethyl, 2-methyl-3-(3,4,5 triacetylaminophenyl)propyl, 2-(2 5 ethoxycarbonylphenyl)ethyl, 1-(3 propoxycarbonylphenyl)ethyl, 3-(4 pentyloxycarbonylphenyl)propyl, 4-(3 hexyloxycarbonylphenyl)butyl, 5-(3,4 dimethoxycarbonylphenyl)pentyl, 6-(3,4,5 10 triethoxycarbonylphenyl)hexyl, 1,1-dimethyl-2-(4 butoxycarbonylphenyl)ethyl, 2-methyl-3-(4 methoxycarbonylphenyl)propyl, 2-(2-cyanophenyl)ethyl, 1-(3-cyanophenyl)ethyl, 3-(4-cyanophenyl)propyl, 4-(2 cyanophenyl)butyl, 5-(3-cyanophenyl)pentyl, 6-(4 15 cyanophenyl)hexyl, 1,1-dimethyl-2-(2,4 dicyanophenyl)ethyl, 2-methyl-3-(2,4,6 tricyanophenyl)propyl, 2-(2-nitrophenyl)ethyl, 1-(3 nitrophenyl)ethyl, 3-(4-nitrophenyl)propyl, 4-(2 nitrophenyl)butyl, 5-(3-nitrophenyl)pentyl, 6-(4 20 nitrophenyl)hexyl, 1,1-dimethyl-2-(2,4 dinitrophenyl)ethyl, 2-methyl-3-(2,4,6 trinitrophenyl)propyl, 2-(2-phenylphenyl)ethyl, 1-(3 phenylphenyl)ethyl, 3-(4-phenylphenyl)propyl, 4-(2 phenylphenyl)butyl, 5-(3-phenylphenyl)pentyl, 6-(4 25 phenylphenyl)hexyl, 1,1-dimethyl-2-(2,4 diphenylphenyl)ethyl, 2-methyl-3-(2,4,6 triphenylphenyl)propyl, 2-(2-fluorophenyl)ethyl, 1-(3 bromophenyl)ethyl, 3-(4-iodophenyl)propyl, 4-(2- 150 bromophenyl)butyl, 5-(3-chlorophenyl)pentyl, 6-(4 bromophenyl)hexyl, 1,1-dimethyl-2-(2, 4 dichlorophenyl)ethyl, 2-methyl-3-(2,4,6 trifluorophenyl)propyl, 2-(2-ethylphenyl)ethyl, 1-(3 5 propylphenyl)ethyl, 3-(4-butylphenyl)propyl, 4-(2 pentylphenyl)butyl, 5-(3-hexylphenyl)pentyl, 6-(4 trifluoromethylphenyl)hexyl, 1,1-dimethyl-2-(2,4 dimethylphenyl)ethyl., 2-methyl-3-(2,4,6 tri(trifluoromethyl)phenyllpropyl, 2-(2 10 ethoxyphenyl)ethyl, 1-(3-propoxyphenyl)ethyl, 3-(4 butoxyphenyl)propyl, 4-(2-pentyloxyphenyl)butyl, 5-(3 hexyloxyphenyl)pentyl, 6-(4 trifluoromethoxyphenyl)hexyl, 1,1-dimethyl-2-(2,4 dimethoxyphenyl)ethyl, 2-methyl-3-[2,4,6 15 tri(trifluoromethoxy)phenyl]propyl, 2-(2 benzyloxyphenyl)ethyl, 1-[3-(2 phenylethoxy)phenyl]ethyl, 3-[4-(3 phenylpropoxy)phenyllpropyl, 4-[2-(4 phenylbutoxy)phenyl]butyl, 5-[3-(5 20 phenylpentyloxy)phenyllpentyl, 6-[4-(6 phenylhexyloxy)phenyl]hexyl, 1,1-dimethyl-2-(2,4 dibenzyloxyphenyl)ethyl, 2-methyl-3-(2, 4,6 tribenzyloxyphenyl)propyl, 2-(2-hydroxyphenyl)ethyl, 1 (3-hydroxyphenyl)ethyl, 3-(4-hydroxyphenyl)propyl, 4 25 (2-hydroxyphenyl)butyl, 5-(3-hydroxyphenyl)pentyl, 6 (4-hydroxyphenyl)hexyl, 1,1-dimethyl-2-(2,4 dihydroxyphenyl)ethyl, 2-methyl-3-(2, 4,6 trihydroxyphenyl)propyl, 2-(3,4- 151 methylenedioxyphenyl)ethyl, 1-(2,3 ethylenedioxyphenyl)ethyl, 3-(3,4 trimethylenedioxyphenyl)propyl, 4-(3,4 tetramethylenedioxyphenyl)butyl, 5-(3,4 5 methylenedioxyphenyl)pentyl, 6-(3,4 ethylenedioxyphenyl)hexyl, 1,1-dimethyl-2-(3,4 methylenedioxy)ethyl, and 2-methyl-3-(3,4 methylenedioxyphenyl)propyl groups. Preferably, they include phenyl substituted lower alkyl groups which may 10 be substituted on the phenyl ring with group(s), as substituent(s), selected from the group consisting of a lowe-r alkanoyl group, an amino group which may have a lower alkanoyl group as a substituent, a lower alkoxycarbonyl group, a cyano group, a nitro group, a' 15 phenyl group, a halogen atom, a lower alkyl group which may have a halogen atom as a substituent, a lower alkoxy group which may have a halogen atom as a substituent, a phenyl lower alkoxy group, a hydroxyl group, and a lower alkylenedioxy groups. 20 [0256] Examples of the pyridyl lower alkyl group which may have, on the pyridine ring, 1 to 3 substituents selected from the group consisting of a hydroxyl group and a lower alkyl group which may have a 25 hydroxyl group as a substituent include, in addition to the above described pyridyl lower alkyl groups, pyridylalkyl groups which may have, on the pyridine ring, 1 to 3 substituents selected from the group 152 consisting of a hydroxy group and a linear or branched alkyl group having 1 to 6 carbon atoms which may have 1 to 3 hydroxy groups as substituents, and whose alkyl moiety is a linear or branched alkyl group having 1 to 5 6 carbon atoms such as [2-methyl-(3, 4, 5 or 6-)pyridyl]methyl, [2-methyl-3-hydroxy-5-hydroxy methyl-(4 or 6-)pyridyllmethyl, 2-[3-ethyl-(2, 4, 5 or 6-)pyridyl]ethyl, 1-[4-propyl-(2, 3, 5 or 6-)pyridyl]ethyl, 3-[2-butyl-(3, 4, 5 or 10 6-)pyridyl]propyl, 4-[3-pentyl-(2, 4, 5 or 6-)pyridyl]butyl, 1,1-dimethyl-2-[4-hexyl-(2, 3, 5 or 6-)pyridyl]ethyl, 5-[2,3-dimethyl-(4, 5 or 6-)pyridyl]pentyl, 6-[2,4,6-trimethyl-(3 or 5-)pyridyllhexyl, 1-[2-hydroxy-(2, 3, 5 or 15 6-)pyridyl]isopropyl, 2-methyl-3-(3-hydroxy-(2, 4, 5 or 6-)pyridyl]propyl, [2-hydroxy-(3, 4, 5 or 6-)pyridyl]methyl, 2-[3-hydroxy-(2, 4, 5 or 6-)pyridyl]ethyl, 1-[4-hydroxy-(2, 3, 5 or 6-)pyridyl]ethyl, 3-[2-hydroxy-(3, 4, 5 or 20 6-)pyridyl]propyl, 4-[3-hydroxy-(2, 4, 5 or 6-)pyridyl]butyl, 1,1-dimethyl-2-[4-hydroxy-(2, 3, 5 or 6-)pyridyllethyl, 5-[2,3-dihydroxy-(4, 5 or 6-)pyridyl]pentyl, 6-[2,4,6-trihydroxy-(3 or 5-)pyridyl]hexyl, [2-hydroxymethyl-(3, 4, 5 or 25 6-)pyridyllmethyl, 2-[3-(2-hydroxyethyl)-(2, 4, 5 or 6-)pyridyl]ethyl, 1-[4-(3-hydroxypropyl)-(2, 3, 5 or 6-)pyridyllethyl, 3-(2-(4-hydroxybutyl)-(3, 4, 5 or 6-)pyridyllpropyl, 4-[3-(5-hydroxypentyl)-(2, 4, 5 or 153 6-)pyridyl]butyl, 1,1-dimethyl-2-(4-(6-hydroxyhexyl) (2, 3, 5 or 6-)pyridyl]ethyl, 5-[2,3-di(hydroxymethyl) (4, 5 or 6-)pyridyl]pentyl, 6-[2,4,6 tri(hydroxymethyl)-(3 or 5-)pyridyllhexyl, 1-(2 5 hydroxymethyl-(2, 3, 5 or 6-)pyridyl]isopropyl, 2 methyl-3-[3-(2,3-dihydroxypropyl)-(2, 4, 5 or 6-)pyridyl]propyl, [2-methyl-3-(2,2,4-trihydroxybutyl) (4, 5 or 6-)pyridyl]methyl, and [2-methyl-5 hydroxymethyl-(3, 4 or 6-)pyridyllmethyl groups. 10 [02571 Examples of the pyrrolyl lower alkyl group which may have 1 to 3 lower alkyl groups as substituents on the pyrrole ring include pyrrolylalkyl groups which may have 1 to 3 linear or branched alkyl 15 groups having 1 to 6 carbon atoms on the pyrrole ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as [(1, 2 or 3-)pyrrolyl]methyl, 2-[(1, 2 or 3-)pyrrolyl]ethyl, 1 [(1, 2 or 3-)pyrrolyl]ethyl, 3-[(l, 2 or 20 3-)pyrrolyllpropyl, 4-[(1, 2 or 3-)pyrrolyllbutyl, 5 [(1, 2 or 3-)pyrrolyl]pentyl, 6-(l, 2 or 3-)pyrrolyllhexyl, 1,1-dimethyl-2-[(1, 2 or 3-)pyrrolyljethyl, 2-methyl-3-[(1, 2 or 3-)pyrrolyl]propyl, [1-methyl-(2 or 3-)pyrrolyllmethyl, 25 2-[2-ethyl-(l, 3, 4 or 5-)pyrrolyl]ethyl, 1-[3-propyl (1, 2, 4 or 5-)pyrrolyl]ethyl, 3-[l-butyl-(2, 3 or 4-)pyrrolyl]propyl, 4-[2-pentyl-(l, 3, 4 or 5-)pyrrolyl]butyl, 5-[3-hexyl-(l, 2, 4 or 154 5-)pyrrolyl]pentyl, 6-[1,2-dimethyl-(3, 4 or 5-)pyrrolyl]hexyl, 1,1-dimethyl-2-(1,2,3-trimethyl-(4 or 5-)pyrrolyl]ethyl, and 2-methyl-3-[1-ethyl-2-methyl (3, 4 or 5-)pyrrolyl]propyl groups. 5 [0258] Examples of the benzoxazolyl lower alkyl group include benzoxazolylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as [(2, 4, 5, 6 or 10 7-)benzooxazolyl]methyl, 2-[(2, 4, 5, 6 or 7-)benzooxazolyl]ethyl, 1-((2, 4, 5, 6 or 7-)benzooxazolyl]ethyl, 3-[(2, 4, 5, 6 or 7-)benzooxazolyl]propyl, 4-[(2, 4, 5, 6 or 7-)benzooxazolyl]butyl, 5-[(2, 4, 5, 6 or 15 7-)benzooxazolyllpentyl, 6-[(2, 4, 5, 6 or 7-)benzooxazolyl]hexyl, 1,1-dimethyl-2-[(2, 4, 5, 6 or 7-)benzooxazolyl]ethyl, and 2-methyl-3-[(2, 4, 5, 6 or 7-)benzooxazolyl]propyl groups. 10259] 20 Examples of the benzothiazolyl lower alkyl group include benzothiazolylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as [(2, 4; 5, 6 or 7-)benzothiazolyl]methyl, 2-[(2, 4, 5, 6 or 25 7-)benzothiazolyl)ethyl, 1-[(2, 4, 5, 6 or 7-)benzothiazolyl]ethyl, 3-[(2, 4, 5, 6 or 7-)benzothiazolyllpropyl, 4-[(2, 4, 5, 6 or 7-)benzothiazolyl]butyl, 5-[(2, 4, 5, 6 or 155 7-)benzothiazolyl]pentyl, 6-[(2, 4, 5, 6 or 7-)benzothiazolyl]hexyl, 1,1-dimethyl-2-[(2, 4, 5, 6 or 7-)benzothiazolyl]ethyl, and 2-methyl-3[-((2, 4, 5, 6 or 7-)benzothiazolyl]propyl groups. 5 [0260] Examples of the furyl lower alkyl group include furylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as [(2 or 3-)furyl]methyl, 2-[(2 or 10 3-)furyl]ethyl, 1-[(2 or 3-)furyl]ethyl, 3-[(2 or 3-)furyl]propyl, 4-[(2 or 3-)furyl]butyl, 5-[(2 or 3-)furyl]pentyl, 6-[(2 or 3-)furyl]hexyl, 1,1-dimethyl 2-[(2 or 3-)furyl]ethyl, and 2-methyl-3-[(2 or 3-)furyljpropyl groups. 15 [0261] Examples of the thiazolidinyl lower alkyl group which may have an oxo group as a substituent on the thiazolidine ring include thiazolidinylalkyl groups which may have -1 to 3 oxo groups as substituents on the 20 thiazolidine ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (2, 3, 4 or 5-)thiazolidinylmethyl, 2-[(2, 3, 4 or 5-)thiazolidinyl]ethyl, 1-[(2) 3, 4 or 5-)thiazolidinyl]ethyl, 3-[(2, 3, 4 or 25 5-)thiazolidinyl]propyl, 4-[(2, 3, 4 or 5-)thiazolidinyl]butyl, 5-((2, 3, 4 or 5-)thiazolidinyl]pentyl, 6-[(2, 3, 4 or 5-)thiazolidinyl]hexyl, 1,1-dimethyl-2-[(2, 3, 4 or 156 5-)thiazolidinyl]ethyl, 2-methyl-3-[(2, 3, 4 or 5-)thiazolidinyl]propyl, [2,4-dioxo-(3 or 5-)thiazolidinyl]methyl, 2-[2-oxo-(3, 4 or 5-)thiazolidinyl]ethyl, 1-[4-oxo-(2, 3 or 5 5-)thiazolidinyl]ethyl, 3-(2-oxo-(3, 4 or 5-)thiazolidinyllpropyl, 4-[5-oxo-(2, 3 or 4-)thiazolidinyl]butyl, 5-[2,5-dioxo-(3 or 4-)thiazolidinyl]pentyl, 6-[2,4,5-trioxo-3 thiazolidinyl]hexyl, 1-[4,5-dioxo-(2 or 10 3-)thiazolidinyl]ethyl, 2-[4,5-dioxo-(2-or 3-)thiazolidinyl]ethyl, 1,1-dimethyl-2-[2,4-dioxo-(3 or 5-)thiazolidinyl]ethyl, and 2-methyl-3-[2,4-dioxo-(3 or 5-)thiazolidinyl]propyl groups. [0262] 15 Examples of the thiazolidinylidene lower alkyl group which may have an oxo group as a substituent on the thiazolidine ring include thiazolidinylidenealkyl groups which may have 1 to 3 oxo groups as substituents on the thiazolidine ring and 20 whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (2, 4 or 5-)thiazolidinylidenemethyl, (2, 4 or 5-)thiazolidinylideneethyl, (2, 4 or 5-)thiazolidinylidenepropyl, (2, 4 or 25 5-)thiazolidinylideneisopropyl, (2, 4 or 5-)thiazolidinylidenebutyl, (2, 4 or 5-)thiazolidinylidenepentyl, (2, 4 or 5-)thiazolidinylidenehexyl, 4,5-dioxo-2- 157 thiazolidinylidenemethyl, 2,5-dioxo-4 thiazolidinylidenemethyl, 2,4-dioxo-5 thiazolidinylidenemethyl, 4-oxo-(2 or 5-)thiazolidinylideneethyl, 5-oxo-(2 or 5 4-)thiazolidinylidenepropyl, and 2-oxo-(4 or 5-)thiazolidinylidenebutyl groups. [0263] Examples of the benzoyl group which may be substituted on the phenyl ring with 1 to 3 groups 10 selected from the group consisting of a cyano group, an amino group which may have a lower alkylsulfonyl group as a substituent, a halogen atom, a lower alkoxy group, a lower alkyl group which may have a halogen atom as a substituent, a thiazolidinyl lower alkyl group which* 15 may have an oxo group as a substituent on the thiazolidine ring, a thiazolidinylidene lower alkyl group which may have an oxo group as a substituent on the thiazolidine ring, and a lower alkylenedioxy group include benzoyl groups which may be substituted on the 20 phenyl ring with 1 to 3 groups selected from the group consisting of a cyano group; an amino group which may have 1 or 2 linear or branched alkylsulfonyl groups having 1 to 6 carbon atoms as substituents; a halogen atom; a linear or branched alkoxy group having 1 to 6 25 carbon atoms; a linear or branched alkyl group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents; a thiazolidinylalkyl group which may have 1 to 3 oxo groups as substituents on the 158 thiazolidine ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms; a thiazolidinylidenealkyl group which may have 1 to 3 oxo groups as substituents on the thiazolidine ring and 5 whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms; and a linear or branched alkylenedioxy group having 1 to 4 carbon atoms such as benzoyl, 4-cyanobenzoyl, 3, 4-methylenedioxybenzoyl, 2 aminobenzoyl, 3-aminobenzoyl, 4-aminobenzoyl, 3,4 10 diaminobenzoyl, 2,4,6-triaminobenzoyl, 4 methoxybenzoyl, 4-trifluoromethylbenzoyl, 4 chlorobenzoyl, 3, 4-difluorobenzoyl, 2-fluorobenzoyl, 3 bromobenzoyl, 4-iodobenzoyl, 3,4-dimethoxybenzoyl, 4 fluorobenzoyl, 3-cyanobenzoyl, 2-cyanobenzoyl, 2,3 15 dicyanobenzoyl, 3,4, 5-tricyanobenzoyl, 4-methylbenzoyl, 4-(2,4-dioxothiazolidinylmethyl)benzoyl, 4-(2,4 dioxothiazolidinylidenemethyl) benzoyl, 2-methylbenzoyl, 3-methylbenzoyl, 2-ethylbenzoyl, 3-ethylbenzoyl, 4 ethylbenzoyl, 4--isopropylbenzoyl, 3-butylbenzoyl, 4 20 pentylbenzoyl, 4-hexylbenzoyl, 3,4-dimethylbenzoyl, 3, 4-diethylbenzoyl, 2, 4-dimethylbenzoyl, 2,5 dimethylbenzoyl, 2,6-dimethylbenzoyl, 3,4,5 trimethylbenzoyl, 2-methoxybenzoyl, 3-methoxybenzoyl, 2-ethoxybenzoyl, 3-ethoxybenzoyl, 4-ethoxybenzoyl, 4 25 isopropoxybenzoyl, 3-butoxybenzoyl, 4-pentyloxybenzoyl, 4-hexyloxybenzoyl, 3, 4-diethoxybenzoyl, 2,4 dimethoxybenzoyl, 2,5-dimethoxybenzoyl, 2,6 dimethoxybenzoyl, 3, 4, 5-trimethoxybenzoyl, 2- 159 trifluoromethylbenzoyl, 3-trifluoromethylbenzoyl, 4 trifluoromethylbenzoyl, 2-(bromomethyl)benzoyl, 3-12 chloroethyl)benzoyl, 4-(2,3-dichloropropyl)benzoyl, 4 (4-fluorobutyl)benzoyl, 3-(5-chloropentyl)benzoyl, 4 5 (5-bromohexyl)benzoyl, 4-(5, 6-dibromohexyl)benzoyl, 3,4-di(trifluoromethyl)benzoyl, 3,4-di(4,4,4 trichlorobutyl)benzoyl, 2,4-di (3-chloro-2 methylpropyl)benzoyl, 2, 5-di (3-chloropropyl)benzoyl, 2,6-di(2,2,2-triffluoroethyl).benzoyl, 3,4,5 10 tri(trifluoromethyl)benzoyl, 4-(2,2,2 trichloroethyl)benzoyl, 2-methyl-4 trifluoromethylbenzoyl, 3-ethyl-4 trichloromethylbenzoyl, 2-methoxy-4 trifluoromethylbenzoyl, 3-ethyl-4-fluorobenzoyl, 3 15 ethoxy-4-trichloromethylbenzoyl, 2-rnethyl-3 trifluoroniethyl-4-trifluoromethylbelzoyl, 3 fluorobenzoyl, 4-f luorobenzoyl, 2-bromobenzoyl, 4 bromobenzoy., 2-iodobenzoyl, 3-iodobenzoyl, 2,3 dibromobenzoyl, 2, 4-diioclobenzoyl, 2, 5-difluorobenzoyl, 20 2,6-dichlorobenzoyl, 2,4,6-trichlorobenzoyl, 2,4 difluorobeizoyl, 3, 4-difluorobenzoyl,' 3,5 difluorobenzoyl, 2, 6-difluorobentoyl, 2-chlorobenzoyl, 3-chlorobenzoyl, 4-chlorobenzoyl, 2, 3-dichlorobenzoyl, 2,4-dichlorobenzoyl, 2,5-ciichlorobenzoyl, 3,4 25 dichlorobenzoyl, 2,6-dichiorobeizoyl, 3,5 dichlorobenzoyl, 2,4,6-trifluorobenzoyl, 2,4 difluorobenzoyl, 3, 4-difluorobenzoyl, 3,4 methylenedioxybenzoyl, 3, 4-trimethylenedioxybenzoyl, 160 2, 3-ethylenedioxybenzoyl, 3, 4-trimethylenedioxybenzoyl, 2,3-tetramethylenedioxybenzoyl, 2,3 methylenedioxybenzoyl, 3,4-ethylenedioxybenzoyl, and 2 methanesulfonylaminobenzoyl groups. 5 [0264] Examples of the thiazolidinyl lower alkanoyl group which may be substituted on the thiazolidine ring with a group selected from the group consisting of an oxo group and a-group of the formula: 10 [0265] [Formula 56] Ra Rb [0266] wherein Ra and Rb each represent a lower alkyl group, include thiazolidinylalkanoyl groups which may be 15 substituted on the thiazolidine ring with 1 to 3 substituents selected from the group consisting of an oxo group and a group of the formula: [0267] [Formula 57] Rb 20 [0268] wherein R' and Rb each represent a linear or branched alkyl group having 1 to 6 carbon atoms, and whose 161 alkanoyl moiety is a linear or branched alkanoyl group having 2 to 6 carbon atoms such as 2-[(2, 3, 4 or 5-)thiazolidinyl]acetyl, 3-[(2, 3, 4 or 5-)thiazolidinyl]propionyl, 2-[(2, 3, 4 or 5 5-)thiazolidinyllpropionyl, 4-[(2, 3, 4 or 5-)thiazolidinyl]butyryl, 5-[(2, 3, 4 or 5-)thiazolidinyl]pentanoyl, 6-((2, 3, 4 or 5-)thiazolidinyllhexanoyl, 2,2-dimethyl-3-[(2, 3, 4 or 5-)thiazolidinyllpropionyl, 2-methyl-3-[(2, 3, 4 or 10 5-)thiazolidinyl]propionyl, [2,4-dioxo-(3 or 5-)thiazolidinyllacetyl, 3-[2-oxo-(3, 4 or 5-)thiazolidinyl]propionyl, 2-[4-oxo-(2, 3 or 5-)thiazolidinyl]propionyl, 4-[5-oxo-(2, 3 or 4-)thiazolidinyl]butyryl, 5-[2,5-dioxo-(3 or 15 4-)thiazolidinyl]pentanoyl, 6-[2,4,5-trioxo-3 thiazolidinyl]hexanoyl, 2-[4,5-dioxo-(2 or 3-)thiazolidinyl]acetyl, 2,2-dimethyl-3-[2,4-dioxo-(3 or 5-)thiazolidinyl]propionyl, 2-methyl-3-[2,4-dioxo-(3 or 5-)thiazolidinyl]propionyl, 2-[4-oxo-2 20 isopropylidenehydrazono-(3 or 5-)thiazolidinyl]acetyl, 2-(2-oxo-5-isopropylidenehydrazono-(3 or 4-)thiazolidinyllacetyl, 2-[2,4 di(isopropylidenehydrazono)-(3 or 5-)thiazolidinyl]acetyl, 3-[2-methylidenehydrazono-(3, 25 4 or 5-)thiazolidinyllpropionyl, 2-[4 ethylidenehydrazono-(2, 3 or 5-)thiazolidinyllpropionyl, 4-[5-propylidenehydrazono (2, 3 or 4-)thiazolidinyl]butyryl, 5-[2,5- 162 di(isopropylidenehydrazono)-(3 or 4-)thiazolidinyl]pentanoyl, 6-[2,4,5 tri(isopropylidenehydrazono)-3-thiazolidinyl]hexanoyl, 2-[4,5-di(isopropylidenehydrazono)-(2 or 5 3-)thiazolidinyl]acetyl, 2,2-dimethyl-3-[ 4 butylidenehydrazono(2, 3 or 5-)thiazolidinyl]propionyl, 2-methyl-3-[5-pentylidene-(2, 3 or 4-)thiazolidinyl]propionyl, and 2 (hexylidenehydrazono)-(3, 4 or 5-)thiazolidinylacetyl 10 groups. [02691 Examples of the lower alkyl group which may have a substituent selected from the group consisting of a hydroxyl group and a halogen atom include, in 15 addition to the above described lower alkyl groups, linear or branched alkyl groups having 1 to 6 carbon atoms which may have 1 to 3 substituents selected from the group consisting of a hydroxy group and a halogen atom such as hydroxymethyl, 2-hydroxyethyl, 1 20 hydroxyethyl, 3-hydroxypropyl, 2,3-dihydroxypropyl, 4 hydroxybutyl, 1,1-dimethyl-2-hydroxyethyl, 5,5,4 trihydroxypentyl, 5-hydroxypentyl, 6-hydroxyhexyl, 1 hydroxyisopropyl, 2-methyl-3-hydroxypropyl, trifluoromethyl, trichloromethyl, chloromethyl, 25 bromomethyl, fluoromethyl, iodomethyl, difluoromethyl, dibromomethyl, 2-chloroethyl, 2,2, 2-trifluoroethyl, 2,2, 2-trichloroethyl, 3-chloropropyl, 2,3 dichloropropyl, 4,4,4-trichlorobutyl, 4-fluorobutyl, 5- 163 chloropentyl, 3-chloro-2-methylpropyl, 5-bromohexyl, 5,6-dibromohexyl, 2-hydroxy-3-fluoropropyl, and 2,2 dichloro-3-hydroxybutyl groups. Examples of the carbamoyl group which may 5 have a group selected from the group consisting of a lower alkoxy lower alkyl group and a lower alkyl group include carbamoyl groups which may have 1 or 2 groups selected from the group consisting of a linear or branched alkyl group having .1 to 6 carbon atoms and 10 which has a linear or branched alkoxy group having 1 to 6 carbon atoms and a linear or branched alkyl group having 1 to 6 carbon atoms such as carbamoyl, N-(2 methoxyethyl)carbamoyl, methylcarbamoyl, ethylcarbamoyl, propylcarbamoyl, isopropylcarbamoyl, 15 butylcarbamoyl, tert-butylcarbamoyl, pentylcarbamoyl, hexylcarbamoyl, dimethylcarbamoyl, diethylcarbamoyl, dipropylcarbamoyl, dibutylcarbamoyl, dipentylcarbamoyl, dihexylcarbamoyl, N-methyl-N-ethylcarbamoyl, N-ethyl-N propylcarbamoyl, N-methyl-N-butylcarbamoyl, N-methyl-N 20 hexylcarbamoyl, N-(methoxymethyl)carbamoyl, N-(3 propoxypropyl)carbamoyl, N-(4-butoxybutyl)carbamoyl,

N

(4-ethoxybutyl)carbamoyl, N-(5 pentyloxypentyl)carbamoyl, N-(5 methoxypentyl)carbamoyl, N-(6-hexyloxyhexyl)carbamoyl, 25 di(2-methoxyethyl)carbamoyl, N-(2-methoxyethyl)-N methylcarbamoyl, and N-(2-methoxyethyl)-N ethylcarbamoyl groups. [0270] 164 Examples of the phenyl group which may be substituted on the phenyl ring with 1 to 3 groups selected from the group consisting of a carbamoyl group which may have a group selected from the group 5 consisting of a lower alkoxy lower alkyl group and a lower alkyl group, a lower alkoxycarbonyl group, a carboxy group, a cyano group, a phenyl group, a halogen atom, a lower alkyl.group which may have a halogen atom as a substituent, a lower alkoxy group which may have a 10 halogen atom as a substituent, a benzoyl group which may have a halogen atom as a substituent on the phenyl ring, a phenyl lower alkyl group which may have a halogen atom as a substituent on the phenyl ring, and a hydroxyl group include phenyl groups which may be 15 substituted on the phenyl ring with 1 to 3 groups selected from the group consisting of a carbamoyl group which may have 1 or 2 groups selected from the group consisting of an alkoxyalkyl group whose alkoxy moiety is a linear or branched alkoxy group having 1 to 6 20 carbon atoms and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms and a linear or branched alkyl group having 1 to 6 carbon atoms; an alkoxycarbonyl group whose akloxy moiety is a linear or branched alkoxy group having 1 to 6 carbon 25 atoms; a carboxy group; a cyano group; a phenyl group; a halogen atom; a linear or branched alkyl group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents; a linear or branched alkoxy group 165 having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents; a benzoyl group which may have 1 to 3 halogen atoms as substituents on the phenyl ring; a phenylalkyl group which may have 1 to 3 5 halogen atoms as substituents on the phenyl ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms, and a hydroxyl group such as phenyl, 2-methylphenyl, 3-methylphenyl, 4 methylphenyl, 2-ethylphenyl, 3-ethylphenyl, 4 10 ethylphenyl, 4-isopropylphenyl, 3-butylphenyl, 4 pentylphenyl, 4-hexylphenyl, 3,4-dimethylphenyl, 3,4 diethylphenyl, 2,4-dimethylphenyl, 2,3-dimethylphenyl, 2,5-dimethylphenyl, 2,6-dimethylphenyl, 3,4,5 trimethylphenyl, 2-methoxyphenyl, 3-methoxyphenyl, 4-' 15 methoxyphenyl, 2-ethoxyphenyl, 3-ethoxyphenyl, 4 ethoxyphenyl, 4-isopropoxyphenyl, 3-butoxyphenyl, 4 pentyloxyphenyl, 4-hexyloxyphenyl, 3,4-dimethoxyphenyl, 3,4-diethoxyphenyl, 2,4-dimethoxyphenyl, 2,5 dimethoxyphenyl-, 2,6-dimethoxyphenyl, 3,4,5 20 trimethoxyphenyl, 2-trifluoromethoxyphenyl, 3 trifluoromethoxyphenyl, 4-trifluoromethoxyphenyl, 2 (bromomethoxy)phenyl, 3-(2-chloroethoxy)phenyl, 4-(2,3 dichloropropoxy)phenyl, 4-(4-fluorobutoxy)phenyl, 3-(5 chloropentyloxy)phenyl, 4-(5-bromohexyloxy)phenyl, 4 25 (5,6-dibromohexyloxy)phenyl, 3,4 di(trifluoromethoxy)phenyl, 3,4-di(4,4,4 trichlorobutoxy)phenyl, 2,4-di(3-chloro-2 methoxypropyl)phenyl, 2,5-di(3-chloropropoxy)phenyl, 166 2,6-di(2,2,2-trifluoroethoxy)phenyl, 3,4,5 tri(trifluoromethoxy)phenyl, 4-(2,2,2 trichloroethoxy)phenyl, 2-methyl-4 trifluoromethoxyphenyl, 3-ethyl-4 5 trichloromethoxyphenyl, 2-methoxy-4 trifluoromethoxyphenyl, 3-ethoxy-4 trichloromethoxyphenyl, 2-trifluoromethylphenyl, 3 trifluoromethylphenyl, 4-trifluoromethylphenyl, 2 (bromomethyl)phenyl, 3- (2-chloroethyl)phenyl, 4- (2,3 10 dichloropropyl) phenyl, 4- (4-fluorobutyl)phenyl, 3- (5 chloropentyl)phenyl, 4- (5-bromohexyl)phenyl, 4- (5,6 dibromohexyl)phenyl, 3,4-di(trifluoromethyl)phenyl, 3,4-di(4,4,4-trichlorobutyl)phenyl, 2,4-di(3-chloro-2 methylpropyl)phenyl, 2, 5-di (3-chloropropyl)phenyl, 2,*6 15 di(2,2,2-trifluoroethyl)phenyl, 3,4,5 tri(trifluoromethyl)phenyl, 4-(2,2,2 trichloroethyl) phenyl, 2-methyl-4 trifluoromethylphenyl, 3-ethyl-4-trichloromethylphenyl, 2-methoxycarbonylphenyl, 3-methoxycarbonylphenyl, 4 20 methoxycarbonylphenyl, 2-ethoxycarbonylphenyl, 3 ethoxycarbonylphenyl, 4-ethoxycarbonylphenyl, 4 isopropoxycarbonylphenyl, 3-butoxycarbonylphenyl, 4 tert-butoxycarbonylphenyl, 4-pentyloxycarbonylphenyl, 4-hexyloxycarbonylphenyl, 3,4-dimethoxycarbonylphenyl, 25 3, 4-diethoxycarbonylphenyl, 2,4 dimethoxycarbonylphenyl, 2,5-diethoxycarbonylphenyl, 2,6-dimethoxycarbonylphenyl, 3,4,5 triethoxycarbonylphenyl, 2-cyanophenyl, 3-cyanophenyl, 167 4-cyanophenyl, 3,4-dicyanophenyl, 3,5-dicyanophenyl, 2,4-dicyanophenyl, 2,5-dicyanophenyl, 2,6 dicyanophenyl, 3,4,5-tricyanophenyl, 2-phenylphenyl, 3 phenylphenyl, 4-phenylphenyl, 3,4-diphenylphenyl, 3,5 5 diphenylphenyl, 2,4-diphenylphenyl, 2,5-diphenylphenyl, 2,6-diphenylphenyl, 3,4,5-triphenylphenyl, 2 chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2,3 dichlorophenyl, 2,4-dichlorophenyl, 2,5-dichlorophenyl, 3,4-dichlorophenyl, 2,6-dichlorophenyl, 3,5 10 dichlorophenyl, 2,4,6-trichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 2,5-difluorophenyl, 2,4-difluorophenyl, 3,4-difluorophenyl, 3,5 difluorophenyl, 2,6-difluorophenyl, 2,4,6 trifluorophenyl, 2-bromophenyl, 3-bromophenyl, 4 15 bromophenyl, 2-iodophenyl, 3-iodophenyl, 4-iodophenyl, 2,3-dibromophenyl, 2,4-diiodophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3,4-dihydroxyphenyl, 3,5-dihydroxyphenyl, 2,4-dihydroxyphenyl, 2,5 dihydroxyphenyl, 2,6-dihydroxyphenyl, 3,4,5 20 trihydroxyphenyl, 3-benzylphenyl, 2-(2 phenylethyl)phenyl, 4-(1-phenylethyl)phenyl, 2-(3 phenylpropyl)phenyl, 3-(4-phenylbutyl)phenyl, 4-(5 phenylpentyl)phenyl, 2-(6-phenylhexyl)phenyl, 4-(1,1 dimethyl-2-phenylethyl)phenyl, 3-(2-methyl-3 25 phenylpropyl)phenyl, 2-(4-fluorobenzyl)phenyl, 2 methyl-5-chlorophenyl, 2-methoxy-5-chlorophenyl, 4-(4 fluorobenzoyl)phenyl, 4-(4-fluorobenzyl)phenyl, 3-(2 chlorobenzyl)phenyl, 4-(3-chlorobenzyl)phenyl, 2-(4- 168 chlorobenzyl)phenyl, 3-[2-(4-fluorophenyl)ethyl]phenyl, 4-[2-(4-chlorophenyl)ethyllphenyl, 2-(3,4 dibromobenzyl)phenyl, 3-(3,4-diiodobenzyl)phenyl, 4 (2,4-difluorobenzyl)phenyl, 2-(2,5 5 dichlorobenzyl)phenyl, 3-(2,6-dichlorobenzyl)phenyl, 4 (3,4,5-trifluorobenzyl)phenyl, 2-[3-(4 chlorophenyl)propyl]phenyl, 3-[1-(2 bromophenyl)ethyllphenyl, 4-[4-(3 fluorophenyl)butyl]phenyl, 2-[5-(4 10 iodophenyl)pentyl]phenyl, 3-[6-(4 chlorophenyl)hexyl]phenyl, 2-[1,1-dimethyl-2-(3 fluorophenyl)ethyllphenyl, 4-(2-methyl-3-(4 chlorophenyl)propyl]phenyl, 2,4-dibenzylphenyl, 2,4,6 tribenzylphenyl, 2-chloro-4-cyanophenyl, 3-hydroxy-4 15 phenylphenyl, 3-ethoxycarbonyl-2-benzoylphenyl, 2 benzyl-4-methyl-6-methoxyphenyl, 4-[ (2 methoxyethyl)carbamoyl]phenyl, 3- (N-ethyl-N isopropylcarbamoyl)phenyl, 4-dimethylcarbamoylphenyl, 2-carboxyphenyl, 3-carboxyphenyl, and 4-carboxyphenyl 20 groups. [0271] Examples of the phenyl group which has a lower alkylenedioxy group as a substituent on the phenyl ring include phenyl groups which has a linear or 25 branched alkylenedioxy group having 1 to 4 carbon atom as a substituent on the phenyl ring such as 3,4 methylenedioxyphenyl, 3, 4-trimethylenedioxyphenyl, 2,3 ethylenedioxyphenyl, 2, 3-tetramethylenedioxyphenyl, 169 2, 3-methylenedioxyphenyl, 3, 4-ethylenedioxyphenyl, and 2, 3-trimethylenedioxyphenyl groups. [0272] Examples of the naphthyl lower alkyl group 5 include naphthylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (1 or 2-)naphthylmethyl, 2-[(1 or 2-)naphthyllethyl, l-[(1 or 2-)naphthyl]ethyl, 3-[(l or 2-)naphthyl]propyl, 4-[(( or 2-)naphthyl]butyl, 5-[(1 10 or 2-)naphthyl].pentyl, 6-[(1 or 2-)naphthyl]hexyl, 1,1 dimethyl-2-[(1 or 2-)naphthyl]ethyl, and 2-methyl-3-[(l or 2-)naphthyllpropyl groups. [0273] Examples -of the phenoxy group which may be 15 substituted on the phenyl ring with 1 to 3 groups selected from the group consisting of a cyano group, a lower alkyl group which may have a halogen atom as a substituent, and a lower alkoxy group which may have a halogen atom as, a substituent include phenoxy groups 20 which may be substituted on the phenyl group with 1 to 3 groups selected from the group consisting of a cyano group, a linear or branched alkyl group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents, and a linear or branched alkoxy group 25 having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents such as phenoxy, 2 methylphenoxy, 3-methylphenyl, 4-methylphenoxy, 2 ethylphenoxy, 3-ethylphenoxy, 4-ethylphenoxy, 4- 170 isopropylphenoxy, 3-butylphenoxy, 4-pentylphenoxy, 4 hexylphenoxy, 3,4-dimethylphenoxy, 3,4-diethylphenoxy, 2,4-dimethylphenoxy, 2,5-dimethylphenoxy, 2,6 dimethylphenoxy, 3,4,5-trimethylphenoxy, 2 5 methoxyphenoxy, 3-methoxyphenoxy, 4-methoxyphenoxy, 2 ethoxyphenoxy, 3-ethoxyphenoxy, 4-ethoxyphenoxy, 4 isopropoxyphenoxy, 3-butoxyphenoxy, 4-pentyloxyphenoxy, 4-hexyloxyphenoxy, 3.,4-dimethoxyphenoxy, 3,4 diethoxyphenoxy,- 2,4-dimethoxyphenoxy, 2,5 10 dimethoxyphenoxy, 2,6-dimethoxyphenoxy, 3,4,5 trimethoxyphenoxy, 2-trifluoromethoxyphenoxy, 3 trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy, 2 (bromomethoxy)phenoxy, 3-(2-chloroethoxy)phenoxy, 4 (2,3-dichloropropoxy)phenoxy, 4-(4 15 fluorobutoxy)phenoxy, 3-(5-chloropentyloxy)phenoxy, 4 (5-bromohexylOxy)phenoxy, 4-(5,6 dibromohexyloxy)phenoxy, 3,4 di(trifluoromethoxy)phenoxy, 3,4-di(4,4,4 trichlorobutoxy)phenoxy, 2,4-di(3-chloro-2 20 methoxypropyl)phenoxy, 2,5-di(3-chloropropoxy)phenoxy, 2,6-di(2,2,2-trifluoroethoxy)phenoxy, 3,4,5 tri(trifluoromethoxy)phenoxy, 4-(2,2,2 trichloroethoxy)phenoxy, 2-methyl-4 trifluoromethoxyphenoxy, 3-ethyl-4 25 trichloromethoxyphenoxy, 2-methoxy-4 trifluoromethoxyphenoxy, 3-ethoxy-4 trichloromethoxyphenoxy, 2-trifluoromethylphenoxy, 3 trifluoromethylphenoxy, 4-trifluoromethylphenoxy, 2- 171 (bromomethyl)phenoxy, 3-(2-chloroethyl)phenoxy, 4-(2,3 dichloropropyl)phenoxy, 4-(4-fluorobutyl)phenoxy, 3-(5 chloropentyl)phenoxy, 4-(5-bromohexyl)phenoxy, 4-(5,6 dibromohexyl)phenoxy, 3,4-di(trifluoromethyl)phenoxy, 5 3,4-di(4,4,4-trichlorobutyl)phenoxy, 2,4-di(3-chloro-2 methylpropyl)phenoxy, 2,5-di(3-chloropropyl)phenoxy, 2,6-di(2,2,2-trifluoroethyl)phenoxy, 3,4,5 tri(trifluoromethyl).phenoxy, 4-(2,2,2 trichloroethyl)phenoxy, 2-methyl-4 10 trifluoromethylphenoxy, 3-ethyl-4 trichloromethylphenoxy, 2-cyanophenoxy, 3-cyanophenoxy, 4-cyanophenoxy, 3,4-dicyanophenoxy, 3,5-dicyanophenoxy, 2,3-dicyanophenoxy, 2,4-dicyanophenoxy, 2,5 dicyanophenoxy, 2,6-dicyanophenoxy, 3,4,5 15 tricyanophenoxy, 2-cyano-4-methylphenoxy, 3-cyano-4 methoxyphenoxy, 3-cyano-5-trifluoromethylphenoxy, and 4-cyano-3-trifluoromethoxyphenoxy groups. [0274) Examples of the phenyl lower alkoxy group 20 which may be substituted on the phenyl ring with 1 to 3 groups selected from the group consisting of a halogen atom, a lower alkyl group which may have a halogen atom as a substituent, and a lower alkoxy group which may have a halogen atom as a substituent include, in 25 addition to the above described phenyl lower alkoxy groups, phenylalkoxy groups which may be substituted on the phenyl ring with 1 to 3 groups selected from the group consisting of a halogen atom, a linear or 172 branched alkyl group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents, and a linear or branched alkoxy group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as 5 substituents, and whose alkoxy moiety is a linear or branched alkoxy group having 1 to 6 carbon atoms such as 2,5-difluorobenzyloxy, 2,4-difluorobenzyloxy, 3,4 difluorobenzyloxy, 3, 5-difluorobenzyloxy, 2,6 difluorobenzyloxy, 3-trifluoromethylbenzyloxy, 2 10 trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy, 3, 4-dimethoxybenzyloxy, 3, 5-dimethoxybenzyloxy, 2 chlorobenzyloxy, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 2-methylbenzyloxy, 3-methylbenzyloxy, 4 methylbenzyloxy, 3, 4-dimethylbenzyloxy, 2,3 15 dimethylbenzyloxy, 2-methoxybenzyloxy, 3 methoxybenzyloxy, 4-methoxybenzyloxy, 2,3 dichlorobenzyloxy, 2,4-dichlorobenzyloxy, 2,5 dichlorobenzyloxy, 3,4-dichlorobenzyloxy, 2,6 dichlorobenzyloxy, 4-fluorobenzyloxy, 3 20 fluorobenzyloxy, 2-fluorobenzyloxy, 3 trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 2-trifluoromethoxybenzyloxy, 4-tert-butylbenzyloxy, 4 ethylbenzyloxy, 4-isopropylbenzyloxy, 4-methoxy-3 chlorobenzyloxy, 2- (4-methoxyphenyl) ethoxy, 2- (4 25 fluorophenyl)ethoxy, 2-(4-chlorophenyl)ethoxy, 2-(3 methoxyphenyl)ethoxy, 2-(4-methylphenyl)ethoxy, 3 methyl-4-chlorobenzyloxy, 4- (4-methoxyphenyl)butoxy, 2 (4-methylphenyl) ethoxy, 4-tert-butoxybenzyloxy, 3- 173 chloro-6-methoxybenzyloxy, 4-methoxy-3-methylbenzyloxy, 2-(2-fluorophenyl)ethoxy, 1-(3-bromophenyl)ethoxy, 3 (4-iodophenyl)propoxy, 4-(2-bromophenyl)butoxy, 5-(3 chlorophenyl)pentyloxy, 6-(4-bromophenyl)hexyloxy, 1,1 5 dimethyl-2-(2,4-dichlorophenyl)ethoxy, 2-methyl-3 (2,4,6-trifluorophenyl)propoxy, 2-(2 ethylphenyl)ethoxy, 1-(3-propylphenyl)ethoxy, 3-(4 butylphenyl)propoxy,. 4-(2-pentylphenyl)butoxy, 5-(3 hexylphenyl)pentyloxy, 6-(4 10 trifluoromethylphenyl)hexyloxy, 1,1-dimethyl-2-(2,4 dimethylphenyl)ethoxy, 2-methyl-3-[2,4,6 tri(trifluoromethyl)phenyl]propoxy, 2-(2 ethoxyphenyl)ethoxy, 1-(3-propoxyphenyl)ethoxy, 3-(4 butoxyphenyl)propoxy, 4-(2-pentyloxyphenyl)butoxy, 5 15 (3-hexyloxyphenyl)pentyloxy, 6-(4 trifluoromethoxyphenyl)hexyloxy, 1,1-dimethyl-2-(2,4 dimethoxyphenyl)ethoxy, and 2-methyl-3-[2,4,6 tri(trifluoromethoxy)phenyl]propoxy groups. (0275] 20 Examples of the 1,2,3,4-tetrahydronaphthyl substituted lower alkyl group which may have 1 to 5 lower alkyl groups as substituents on the 1,2,3,4 tetrahydronaphthalene ring include 1,2,3,4 tetrahydronaphthyl substituted alkyl groups which may 25 have 1 to 5 linear or branched alkyl groups having 1 to 6 carbon atoms as substituents on the 1,2,3,4 tetrahydronaphthalene ring, and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon 174 atoms such as (1, 2, 5 or 6-)1,2,3,4 tetrahydronaphthylmethyl, 2-[(1, 2, 5 or 6-)1,2,3,4 tetrahydronaphthyl]ethyl, 1-[(1, 2, 5 or 6-)1,2,3,4 tetrahydronaphthyl]ethyl, 3-[(1, 2, 5 or 6-)1,2,3,4 5 tetrahydronaphthyl]propyl, 4-[(1, 2, 5 or 6-)1,2,3,4 tetrahydronaphthyl]butyl, 5-((1, 2, 5 or 6-)1,2,3,4 tetrahydronaphthyl]pentyl, 6-[(1, 2, 5 or 6-)1,2,3,4 tetrahydronaphthyl]hexyl, 1,1-dimethyl-2-[(1, 2, 5 or 6-)1,2,3,4-tetrahydronaphthyl]ethyl, 2-methyl-3-[(1, 2, 10 5 or 6-)1,2,3,4-tetrahydronaphthyl]propyl, 1,1,4,4 tetramethyl(2, 3, 5 or 6-)1,2,3,4 tetrahydronaphthylmethyl, 1,1,4,4,5-pentamethyl(2, 3, 6, 7 or 8-)1,2,3,4-tetrahydronaphthylmethyl, 1,4,4 trimethyl(2, 3, 5, 6, 7 or 8-)1,2,3,4 15 tetrahydronaphthylmethyl, 5,6-dimethyl(2, 3, 7 or 8-)1,2,3,4-tetrahydronaphthylmethyl, 2-[1-methyl-(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4-tetrahydronaphthyllethyl, 1-[2-ethyl-(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydronaphthyl]ethyl, 3-[3-propyl-(1, 2, 3, 4, 5, 20 6, 7 or 8-)1,2,3,4-tetrahydronaphthyl]propyl, 4-[(4 butyl-(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydronaphthyl]butyl, 5-[5-pentyl-(1, 2, 3, 4, 6, 7 or 8-)1,2,3,4-tetrahydronaphthyl]pentyl, 6-[6-hexyl-(1, 2, 3, 4, 5, 7 or 8-)1,2,3,4-tetrahydronaphthyl)hexyl, 25 1,1-dimethyl-2-[1,7-dimethyl-(1, 2, 3, 4, 5, 6 or 8-)1,2,3,4-tetrahydronaphthyllethyl, and 2-methyl-3 [1,1,4-trimethyl-(2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydronaphthyl)propyl groups.

175 (0276] Examples of the piperidinyl group which may have 1 to 3 lower alkyl groups as substituents on the piperidine ring include piperidinyl group which may 5 have 1 to 3 linear or branched alkyl groups having 1 to 6 carbon atoms as substituents on the piperidine ring such as (1, 2, 3 or 4-)piperidinyl, 1-methyl-(2, 3 or 4-)piperidinyl, 1-ethyl-(2, 3 or 4-)piperidinyl, 1 propyl-(2, 3 or-4-)piperidinyl, 1-isopropyl-(2, 3 or 10 4-)piperidinyl, 1-butyl-(2, 3 or 4-)piperidinyl, 1 isobutyl-(2, 3 or 4-)piperidinyl, 1-tert-butyl-(2, 3 or 4-)piperidinyl, 1-pentyl-(2, 3 or 4-)piperidinyl, 1 hexyl-(2, 3 or 4-)piperidinyl, 1,2-dimethyl-(3, 4, 5 or 6-)piperidinyl, and 1,2,6-trimethyl-(3, 4 or 15 5-)piperidinyl groups. [0277] Examples of the quinolyl lower alkyl group include quinolylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon 20 atoms such as (2, 3, 4, 5, 6, 7 or 8-)quinolylmethyl, 2-[(2, 3, 4, 5, 6, 7 or 8-)quinolyl]ethyl, 1-[(2, 3, 4, 5, 6, 7 or 8-)quinolyl]ethyl, 3-((2, 3, 4, 5, 6, 7 or 8-)quinolyllpropyl, 4-[(2, 3,'4, 5, 6, 7 or 8-) quinolylibutyl, 5-[(2, 3, 4, 5, 6, 7 or 8-) 25 quinolyllpentyl, and 6-[(2, 3, 4, 5, 6, 7 or 8-) quinolyl)hexyl groups. (0278] Examples of the 1,2,3,4-tetrazolyl lower 176 alkyl group which may have, on the tetrazole ring, a substituent selected from the group consisting of a lower alkyl group and a phenyl lower alkyl group include 1,2,3,4-tetrazolylalkyl groups whose alkyl 5 moiety is a linear or branched alkyl group having 1 to 6 carbon atoms and which may have, on the tetrazole ring, a substituent selected from the. group consisting of a linear or branched alkyl group having 1 to 6 carbon atoms and a phenyl alkyl group whose alkyl 10 moiety is a linear or branched alkyl group having 1 to 6'carbon atoms, such as [(1 or 5-)1,2,3,4 tetrazolylimethyl, 2-[(1 or 5-)1,2,3,4 tetrazolyl]ethyl, 1-[(1 or 5-)1,2,3,4-tetrazolyl]ethyl, 3-[(l or 5-)1,2,3,4-tetrazolyllpropyl, 4-[(1 or 15 5-)1,2,3,4-tetrazolyl]butyl, 5-[(1 or 5-)1,2,3,4 tetrazolyl]pentyl, 6-[(1 or 5-)1,2,3,4 tetrazolyllhexyl, 5-[1-methyl-5-(1,2,3,4 tetrazolyl)]pentyl, 6-[1-methyl-5-(1,2,3,4 tetrazolyl)]hexyl, 5-methyl-1-(1,2,3,4 20 tetrazolyl)methyl, 2-[5-ethyl-1-(1,2,3,4 tetrazolyl]hexyl, 1,1-dimethyl-2-[(l or 5-)1,2,3,4 tetrazolyl)Jethyl, 2-methyl-3-[(1 or 5-)1,2,3,4 tetrazolyl]propyl, [1-methyl-5-(1,2,3,4 tetrazolyl)]methyl, [1-ethyl-5-(1,2,3,4 25 tetrazolyl)]methyl, 2-[1-propyl-5-(1,2,3,4 tetrazolyl)]ethyl, 1-[1-butyl-5-(1,2,3,4 tetrazolyl)]ethyl, 3-[1-pentyl-5-(1,2,3,4 tetrazolyl)]propyl, 3-[5-propyl-l-(1,2,3,4- 177 tetrazolyl)]propyl, 4-[5-butyl-1-(1,2,3,4 tetrazolyl)]butyl, 5-[5-pentyl-1-(1,2,3,4 tetrazolyl)]pentyl, 6-[5-hexyl-1-(1,2,3,4 tetrazolyl) ]hexyl, [1-ethyl-5-(1,2,3,4 5 tetrazolyl) ]methyl, [1-benzyl-5--(1,2,3,4 tetrazolyl) Imethyl, 1-[(2-phenylethyl)-5-(1,2,3,4 tetrazolyl)]methyl, 2-[1-(3-phenylpropyl)-5-(1,2,3,4 tetrazolyl))ethyl, 1-[1-(4-phenylbutyl)-5-(1,2,3,4 tetrazolyl) ]ethyl, 3-[1-(5-phenylpentyl)-5-(1,2,3,4 10 tetrazolyl)]propyl, 4-[1-(6-phenylhexyl)-5-(1,2,3,4 tetrazolyl)]butyl, 5-[1-(1,1-dimethyl-2-phenylethyl)-5 (1,2,3,4-tetrazolyl) ]methyl, 6-[1-(2-methyl-3 phenylpropyl)-5-(1,2,3,4-tetrazolyl)]hexyl, 5-benzyl-1 (1,2,3,4-tetrazolyl)methyl, 2-[5-(1-phenylethyl)-1 15 (1,2,3,4-tetrazolyl) ]ethyl, 3-(5-(3-phenylpropyl)-1 (1,2,3,4-tetrazolyl)lpropyl, 4-[5-(4-phenylbutyl)-l (1,2,3,4-tetrazolyl) Jbutyl, 5-[5-(5-phenylpentyl)-1 (1,2,3,4-tetrazolyl) ]pentyl, and 6-[5-(6-phenylhexyl) 1-(1,2,3,4-tetrazolyl) ]hexyl groups. 20 [0279] Examples of the thiazolyl lower alkyl group which may have a phenyl group as a substituent on the thiazole ring include thiazolylalkyl groups which may have 1 or 2 phenyl groups as substituents on the 25 thiazole ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as [(2, 4 or 5-)thiazolyl]methyl, 2-[(2, 4 or 5-)thiazolyl]ethyl, 1-[(2, 4 or 5-)thiazolyl]ethyl, 3- 178 [(2, 4 or 5-)thiazolyl]propyl, 4-[(2, 4 or 5-)thiazolyl]butyl, 5-[(2, 4 or 5-)thiazolyl]pentyl, 6 [(2, 4 or 5-)thiazolyl]hexyl, 1,1-dimethyl-2-[(2, 4 or 5-)thiazolyl]ethyl, 2-methyl-3-[(2, 4 or 5 5-)thiazolyl]propyl, [2-phenyl-(4 or 5-)thiazolyl]methyl, 2-(4-phenyl-(2 or 5-)thiazolyl]ethyl, 1-[5-phenyl-(2 or 4-)thiazolyl]ethyl, 3-[2-phenyl-(2 or 5-)thiazolyl]propyl, 4-(2,4-diphenyl-5-thiazolyl)butyl, 10 5-(2,5-diphenyl-4-thiazolyl)pentyl, 6-(4,5-diphenyl-2 thiazolyl)hexyl, 1,1-dimethyl-2-[2-phenyl-(4 or 5-)thiazolyl]ethyl, 2-methyl-3-[4-phenyl-(2 or 5-)thiazolyl]propyl, [4-phenyl-(2 or 5-)thiazolyl]methyl, (5-phenyl-(2 or 15 4-)thiazolyl]methyl, (2,4-diphenyl-5-thiazolyl)methyl, (2,5-diphenyl-4-thiazolyl)methyl, and (4,5-diphenyl-2 thiazolyl)methyl groups. [0280] Examples of the benzoyl lower alkyl group 20 which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a lower alkoxy group and a halogen atom include benzoylalkyl groups which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a linear or 25 branched alkoxy group having 1 to 6 carbon atoms and a halogen atom and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as benzoylmethyl, 2-benzoylethyl, 1-benzoylethyl, 3- 179 benzoylpropyl, 4-benzoylbutyl, 5-benzoylpentyl, 6 benzoylhexyl, 1,1-dimethyl-2-benzoylethyl, 2-methyl-3 benzoylpropyl, 4-fluorobenzoylmethyl, 2 chlorobenzoylmethyl, 3-chlorobenzoylmethyl, 4 5 chlorobenzoylmethyl, 2-(4-fluorobenzoyl)ethyl, 2-(4 chlorobenzoyl)ethyl, 3,4-dibromobenzoylmethyl, 3,4 diiodobenzoylmethyl, 2,4-difluorobenzoylmethyl, 2,5 dichlorobenzoylmethyl, 2,6-dichlorobenzoylmethyl, 3,4,5-trifluorobenzoylmethyl, 3-(4 10 chlorobenzoyl)propyl, 1-(2-bromobenzoyl)ethyl, 4-(3 fluorobenzoyl)butyl, 5-(4-iodobenzoyl)pentyl, 6-(4 chlorobenzoyl)hexyl, 1,1-dimethyl-2-(3 fluorobenzoyl)ethyl, 2-methyl-3-(4 chlorobenzoyl)propyl, 2-methoxybenzoylmethyl, 2-(3 15 methoxybenzoyl)ethyl, 2-(4-methoxybenzoyl)ethyl, 4 methoxybenzoylmethyl, 1-(2-ethoxybenzoyl)ethyl, 3-(3 ethoxybenzoyl)propyl, 4-(4-ethoxybenzoyl)butyl, 5-(4 isopropoxybenzoyl)pentyl, 6-(3-butoxybenzoyl)hexyl, 1,1-dimethyl-2--(4-pentyloxybenzoyl)ethyl, 2-methyl-3 20 (4-hexyloxybenzoyl)propyl, 3,4-dimethoxybenzoylmethyl, 3,4-diethoxybenzoylmethyl, 2,4-dimethoxybenzoylmethyl, 2,5-dimethoxybenzoylmethyl, 2,6-dimethoxybenzoylmethyl, 3,4,5-trimethoxybenzoylmethyl, 2-chloro-4 methoxybenzoylmethyl, and 3-fluoro-5 25 ethoxybenzoylmethyl groups. [0281] Examples of the piperidinyl lower alkyl group which may have a lower alkyl group as a substituent on 180 the piperidine ring include piperidinylalkyl groups which may have 1 to 3 linear or branched alkyl groups having 1 to 6 carbon atoms as substituents on the piperidine ring and whose alkyl moiety is a linear or 5 branched alkyl group having 1 to 6 carbon atoms such as [(1, 2, 3 or 4-)piperidinyl]methyl, 2-[(1, 2, 3 or 4-)piperidinyllethyl, 1-[(1, 2, 3 or 4-)piperidinyl]ethyl, 3-[(1, 2, 3 or 4-)piperidinyl]propyl, 4-[(1, 2, 3 or 10 4-)piperidinyl.butyl, 5-[(1, 2, 3 or 4-)piperidinyl]pentyl, 6-[(1, 2, 3 or 4-)piperidinyl]hexyl, 1,1-dimethyl-2-[(1, 2, 3 or 4-)piperidinyl]ethyl, 2-methyl-3-H(l, 2, 3 or 4-)piperidinyl]propyl, [1-methyl-(2, 3 or 15 4-)piperidinyl]methyl, 2-[l-ethyl-(2, 3 or 4-)piperidinyllethyl, 1-[4-propyl-(1, 2 or 3-)piperidinyl]ethyl, 3-(3-isopropyl-(1, 2, 4, 5 or 6-)piperidinyl]propyl, 4-[2-butyl-(1, 3, 4, 5 or 6-)piperidinyl]butyl, 5-[1-isobutyl-(2, 3 or 20 4-)piperidinyl]pentyl, 6-[1-tert-butyl-(2, 3 or 4-)piperidinyl]hexyl, 1,1-dimethyl-2-[4-pentyl-(1, 2 or 3-)piperidinyl]ethyl, 2-methyl-3-[l-hexyl-(2, 3 or 4-)piperidinyl]propyl, [1,2-dimethyl-(3, 4, 5 or 6-)piperidinyl]methyl, and (1,2,6-trimethyl-(3, 4 or 25 5-)piperidinyl]methyl groups. [0282] Examples of the imidazolyl group which may have 1 to 3 phenyl groups as substituents on the 181 imidazole ring include imidazolyl groups which may have 1 to 3 phenyl groups as substituents on the imidazole ring such as (1, 2, 4 or 5-)imidazolyl, 1-phenyl-(2, 4 or 5-)imidazolyl, 2-phenyl-(1, 4 or 5-)imidazolyl, 4 5 phenyl-(1, 2 or 5-)imidazolyl, 5-phenyl-(1, 2 or 4-)imidazolyl, 1,2-diphenyl-(4 or 5-)imidazolyl, 2,4 diphenyl-(1 or 5-)imidazolyl, 4,5-diphenyl-(1 or 2-)imidazolyl, 2,5-diphenyl-(1 or 4-)imidazolyl, and 2,4,5-triphenyl-1-imidazolyl groups. 10 [02831 Examples of the benzimidazolyl group which may have 1 to 3 lower alkyl groups as substituents on the benzimidazole ring include benzimidazolyl group which may have 1 to 3 linear or branched alkyl groups 15 having 1 to 6 carbon atoms as substituents on the benzimidazole ring such as (1, 2, 4, 5, 6 or 7-)benzimidazolyl, 1-methyl-(2, 4, 5, 6 or 7-)benzimidazolyl, 2-ethyl-(1, 4, 5, 6 or 7-)benzimidazolyl, 4-propyl-(l, 2, 5, 6 or 20 7-)benzimidazolyl, 5-butyl-(1, 2, 4, 6 or 7-)benzimidazolyl, 6-pentyl-(1, 2, 4, 5 or 7-)benzimidazolyl, 7-hexyl-(1, 2, 4, 5 or 6-)benzimidazolyl, 1-ethyl-(2, 4, 5, 6 or 7-)benzimidazolyllhexyl, 1-butyl-(2, 4, 5, 6 or 25 7-)benzimidazolyl, 1-isopropyl-(1, 2, 4, 5, 6 or 7-)benzimidazolyl, 1,2-dimethyl-(4, 5, 6 or 7-)benzimidazolyl, 1-methyl-4-ethyl-(2, 5, 6 or 7-)benzimidazolyl, 1-propyl-5-methyl-(2, 4, 6 or 182 7-)benzimidazolyl, and 1,2,5-trimethyl-(2, 4, 5, 6 or 7-)benzimidazolyl groups. [0284] Examples of the pyridyl lower alkoxy group 5 include pyridylalkoxy groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (2, 3 or 4-)pyridylmethoxy, 2-[(2, 3 or 4-)pyridyl]ethoxy, 1-[(2, 3 or 4-)pyridyllethoxy, 3 [(2, 3 or 4-)pyridyllpropoxy, 4-[(2, 3 or 10 4-)pyridyl]butoxy, 1-1-dimethyl-2-[(2, 3 or 4-)pyridyllethoxy, 5-[(2, 3 or 4-)pyridyl]pentyloxy, 6 [(2, 3 or 4-)pyridyl]hexyloxy, 1-[(2, 3 or 4-)pyridyl]isopropoxy, and 2-methyl-3-[ (2, 3 or 4-)pyridyl]propoxy groups. 15 [0285] Examples of the 1,2,3,4-tetrahydroquinolyl lower alkyl group which may have an oxo group as a substituent on the tetrahydroquinoline ring include 1,2,3,4-tetrahydroquinolylalkyl groups which may have 1 20 or 2 oxo groups as substituents on the tetrahydroquinoline ring and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as (1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroquinolylmethyl, 2-[(1, 2, 3, 4, 5, 6, 7 or 25 8-)1,2,3,4-tetrahydroquinolyl]ethyl, 1-[(l, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]ethyl, 3-[(l, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]propyl, 4-[ (1, 2, 3, 4, 5, 6, 7 or 8-) 1,2,3,4- 183 tetrahydroquinolyl]butyl, 5-[(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]pentyl, 6-[(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]hexyl, 1,1 dimethyl-2-[(1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 5 tetrahydroquinolyllethyl, 2-methyl-3-((1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]propyl, [2-oxo (1, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroquinolyllmethyl, [4-oxo-(1, 2, 3, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyllmethyl, [2,4-dioxo-(1, 3, 10 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]methyl, 2-[2 oxo-(1, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroquinolyl]ethyl, 3-[4-oxo-(1, 2, 3, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]propyl, 4-[2,4-dioxo-(1, 3, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]butyl, 5 15 [2-oxo-(1, 3, 4, 5, 6, 7 or 8-) 1,2,3,4 tetrahydroquinolyllpentyl, and 6-[4-oxo-(1, 2, 3, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]hexyl groups. (0286] Examples of the 1,3,4-oxadiazolyl lower alkyl 20 group which may have an oxo group as a substituent on the 1,3,4-oxadiazole ring include 1,3,4 oxadiazolylalkyl groups which may have an oxo group as a substituent on the 1,3,4-oxadiazole ring and whose alkyl moiety is a linear or branched alkyl group having 25 1 to 6 carbon atoms such as (2 or 5-)1,3,4 oxadiazolylmethyl, 2-[(2 or 5-)1,3,4-oxadiazolyl]ethyl, 1-[(2 or 5-)1,3,4-oxadiazolyl]ethyl, 3-[(2 or 5-)1,3,4 oxadiazolyl]propyl, 4-[(2 or 5-)1,3,4- 184 oxadiazolyl)butyl, 5-[(2 or 5-)1,3,4 oxadiazolylipentyl, 6-[(2 or 5-)1,3,4 oxadiazolyllhexyl, 1,1-dimethyl-2-[(2 or 5-)1,3,4 oxadiazolyl]ethyl, 2-methyl-3-[(2 or 5-)1,3,4 5 oxadiazolyl]propyl, 2-oxo-[(3 or 5-)1,3,4 oxadiazolyl]methyl, 5-oxo-[(2 or 3-)1,3,4 oxadiazolyl]methyl, 2-[2-oxo-(3 .or 5-) (1,3,4 oxadiazolyl)]ethyl,.1-[5-oxo-(2 or 3-)1,3,4 oxadiazolyl]ethyl, 3-[(2 or 5-)1,3,4 10 oxadiazolyllpropyl, 4-[2-oxo(3 or 5-)1,3,4 oxadiazolylibutyl, 5-[5-oxo(2 or 3-)1,3,4 oxadiazolyl]pentyl, 6-[2-oxo(3 or 5-)1,3,4 oxadiazolyllhexyl, 1,1-dimethyl-2-[5-oxo(2 or 3-)1,3,4 oxadiazolyll ethyl, and 2-methyl-3-[2-oxo(3 or 5-)1,3,'4 15 oxadiazolyllpropyl groups. [0287] Examples of the thienyl lower alkyl group include thienylalkyl groups whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon 20 atoms such as (2 or 3-)thienylmethyl, 2-[(2 or 3-)thienyl]ethyl, 1-[(2 or 3-)thienyl]ethyl, 3-[(2 or 3-)thienyl]propyl, 4-[(2 or 3-)thienyl]butyl, 5-[(2 or 3-)thienyl]pentyl, 6-[(2 or 3-)thienyl]hexyl, 1,1 dimethyl-2-[ (2 or 3-)thienyllethyl, and 2-methyl-3-[ (2 25 or 3-)thienyl]propyl groups. [0288] Examples of the pyrimidinylcarbonyl group which may have an oxo group as a substituent on the 185 pyrimidine ring include pyrimidinylcarbonyl groups which may have 1 to 3 oxo groups as substituents on the pyrimidine ring such as (2, 3, 4 or 6-)pyrimidinylcarbonyl, 2,6-dioxo-(l, 3, 4 or 5 5-)pyrimidinylcarbonyl, 2-oxo-(1, 3, 4, 5 or 6-)pyrimidinylcarbonyl, 6-oxo-(l, 2, 3, 4 or 5-)pyrimidinylcarbonyl, 4-oxo-(1, 2, 3, 5 or 6-)pyrimidinylcarbonyl, 2,4-dioxo-(1, 3, 4 or 6-)pyrimidinylcarbonyl, and 2,4,6-trioxo-(1, 3 or 10 5-)pyrimidinylcarbonyl groups. (0289] Examples of the lower alkoxy lower alkoxy group include linear or branched alkoxy groups having 1 to 6 carbon atoms which may have a linear or branched 15 alkoxy group having 1 to 6 carbon .atoms as a substituent such as methoxymethoxy, 1-ethoxyethoxy, 2 methoxyethoxy, 2-propoxyethoxy, 3-isopropoxypropoxy, 4 butoxybutoxy, 5-pentyloxypentyloxy, 6-hexyloxyhexyloxy, 1,1-dimethyl-2-methoxyethoxy, 2-methyl-3-ethoxypropoxy, 20 and 3-methoxypropoxy groups. [0290] Examples of the lower alkoxycarbonyl lower alkoxy group include alkoxycarbonylalkoxy groups whose two alkoxy moieties are linear or branched alkoxy 25 groups having 1 to 6 carbon atoms such as methoxycarbonylmethoxy, ethoxycarbonylmethoxy, 2 methoxycarbonylethoxy, 2-ethoxycarbonylethoxy, 1 ethoxycarbonylethoxy, 3-methoxycarbonylpropoxy, 3- 186 ethoxycarbonylpropoxy, 4-ethoxycarbonylbutoxy, 5 isopropoxycarbonylpentyloxy, 6-propoxycarbonylhexyloxy, 1,1-dimethyl-2-butoxycarbonylethoxy, 2-methyl-3-tert butoxycarbonylpropoxy, 2-pentyloxycarbonylethoxy, and 5 hexyloxycarbonylmethoxy groups. [0291] Examples of the carboxy lower alkoxy group include carboxyalkoxy groups whose alkoxy moiety is a linear or branched alkoxy group having 1 to 6 carbon 10 atoms such as carboxymethoxy, 2-carboxyethoxy, 1 carboxyethoxy, 3-carboxypropoxy, 4-carboxybutoxy, 5 carboxypentyloxy, 6-carboxyhexyloxy, 1,1-dimethyl-2 carboxyethoxy, and 2-methyl-3-carboxypropoxy groups. [0292] 15 Examples of the phenoxy lower alkanoyl group include phenoxyalkanoyl groups whose alkanoyl moiety is a linear or branched alkanoyl group having 2 to 6 carbon atoms such as 2-phenoxyacetyl, 3 phenoxypropionyl, 2-phenoxypropionyl, 4-phenoxybutyryl, 20 5-phenoxypentanoyl, 6-phenoxyhexanoyl, 2, 2-dimethyl-2 phenoxypropionyl, and 2-methyl-3-phenoxypropionyl groups. [0293] Examples of the 1,2,3,4 2-5 tetrahydroquinolylcarbonyl group which may have an oxo group as a substituent on the tetrahydroquinoline ring include 1,2,3, 4-tetrahydroquinolylcarbonyl groups which may have 1 or 2 oxo groups as substituents on the 187 tetrahydroquinoline ring such as [(1, 3, 4, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl]carbonyl, (2-oxo-(1, 3, 4, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolylcarbonyl, [4-oxo-(1, 2, 3, 5, 6, 7 or 8-)1,2,3,4 5 tetrahydroquinolyl]carbonyl, and [2,4-dioxo-(1, 3, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyllcarbonyl groups. [02941 Examples of the 1,2,3,4-tetrahydroquinolyl group which may-have an oxo .group as a substituent on 10 the tetrahydroquinoline ring include 1,2,3,4 tetrahydroquinolyl groups which may have 1 or 2 oxo groups as substituents on the tetrahydroquinoline ring such as (1, 2, 3, 4, 5, 6, 7 or 8-)1,2,3,4 tetrahydroquinolyl, 2-oxo-(1, 3, 4, 5, 6, 7 or 15 8-)1,2,3,4-tetrahydroquinolyl, 4.-oxo-(1, 2, 3, 5, 6, 7 or 8-)1,2,3,4-tetrahydroquinolyl, and 2,4-dioxo-(1, 3, 5, 6, 7 or B-)1,2,3,4-tetrahydroquinolyl groups. [0295] Examples of the amino group which may have a 20 lower alkoxycarbonyl group as a substituent include amino groups which may have an alkoxycarbonyl group whose akloxy moiety is a linear or branched alkoxy group having 1 to 6 carbon atoms such as amino, methoxycarbonylamino, ethoxycarbonylamino, 25 propoxycarbonylamino, isopropoxycarbonylamino, butoxycarbonylamino, tert-butoxycarbonylamino, pentyloxycarbonylamino, and hexyloxycarbonylamino groups.

188 [0296) Examples of the benzoyl group which may have 1 to 3 lower alkoxy groups as substituents on the phenyl ring include benzoyl groups which may have 1 to 5 3 linear or branched alkoxy groups having 1 to 6 carbon atoms as substituents on the phenyl ring such as benzoyl, 2-methoxybenzoyl, 3-methoxybenzoyl, 4 methoxybenzoyl, 2-ethoxybenzoyl, 3-ethoxybenzoyl, 4 ethoxybenzoyl, 4-isopropoxybenzoyl, 3-butoxybenzoyl, 4 10 pentyloxybenzoyl, 4-hexyloxybenzoyl, 3,4 dimethoxybenzoyl, 3,4-diethoxybenzoyl, 2,4 dimethoxybenzoyl, 2,5-dimethoxybenzoyl, 2,6 dimethoxybenzoyl, and 3,4,5-trimethoxybenzoyl groups. [0297] 15 Examples of the lower alkyl group which have 1 or 2 phenyls which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a lower alkoxycarbonyl group, a cyano group, a nitro group, a phenyl- group, a halogen atom, a lower alkyl 20 group which may have a halogen atom as a substituent, a lower alkoxy group which may have a halogen atom as a substituent, and a lower alkylthio group include, in addition to the above described phenyl lower alkyl groups, linear or branched alkyl groups which have 1 to 25 6 carbon atoms and 1 to 2 phenyls which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of an alkoxycarbonyl group whose akloxy moiety is a linear or branched alkoxy group 189 having 1 to 6 carbon atoms, a cyano group, a nitro group, a phenyl group, a halogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents, a linear 5 or branched alkoxy group having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms as substituents, and a linear or branched alkylthio group having 1 to 6 carbon atoms such as 1,1-diphenylmethyl, 1,1-di(4 fluorophenyl)methyl, 1-phenyl-1-(4 10 methoxyphenyl)methyl, 3,3-diphenylpropyl, 2,5 difluorobenzyl, 2,4-difluorobenzyl, 3,4-difluorobenzyl, 3,5-difluorobenzyl, 2,6-difluorobenzyl, 3 trifluoromethylbenzyl, 2-trifluoromethylbenzyl, 4 trifluoromethylbenzyl, 3,4-dimethoxybenzyl, 3,5 15 dimethoxybenzyl, 2-chlorobenzyl, 3-chlorobenzyl, 4 chlorobenzyl, 2-methylbenzyl, 3-methylbenzyl, 4 methylbenzyl, 3,4-dimethylbenzyl, 2,3-dimethylbenzyl, 2-methoxybenzyl, 3-methoxybenzyl, 4-cyanobenzyl, 2 cyanobenzyl, 3-cyanobenzyl, 4-methoxybenzyl, 2,3 20 dichlorobenzyl, 2,4-dichlorobenzyl, 2,5-dichlorobenzyl, 3,4-dichlorobenzyl, 2,6-dichlorobenzyl, 4-fluorobenzyl, 3-fluorobenzyl, 2-fluorobenzyl, 4-nitrobenzyl, 3 nitrobenzyl, 2-nitrobenzyl, 3 trifluoromethoxybenzyl, 4-trifluoromethoxybenzyl, 2-trifluoromethoxybenzyl, 4 25 methoxycarbonylbenzyl, 3-methoxycarbonylbenzyl, 4-tert butylbenzyl, 4-ethylbenzyl, 4-isopropylbenzyl, 4 methoxy-3-chlorobenzyl, 2-(4-methoxyphenyl)ethyl, 2-(4 fluorophenyl)ethyl, 2-(4-chlorophenyl)ethyl, 2-(3- 190 methoxyphenyl)ethyl, 2-(4-methylphenyl)ethyl, 4 phenylbenzyl, 3,3-diphenylpropyl, 3-methyl-4 nitrobenzyl, 4-(4-methoxyphenyl)butyl, 2-(4 methylphenyl)ethyl, 4-tert-butoxycarbonylbenzyl, 3 5 chloro-6-methoxybenzyl, 4-nitro-3-methylbenzyl, 4-tert butyrylbenzyl, 2-(2-ethoxycarbonylphenyl)ethyl, 1-(3 propoxycarbonylphenyl)ethyl, 3-(4 pentyloxycarbonylphenyl)propyl, 4-(3 hexyloxycarbonylphenyl)butyl, 5-(3,4 10 dimethoxycarbonylphenyl)pentyl, 6-(3,4,5 diethoxycarbonylphenyl)hexyl, 1,1-dimethyl-2-(4 butoxycarbonylphenyl)ethyl, 2-methyl-3-(4 methoxycarbonylphenyl)propyl, 2-(2-cyanophenyl)ethyl, 1-(3-cyanophenyl)ethyl, 3-(4-cyanophenyl)propyl, 4-(2 15 cyanophenyl)butyl, 5-(3-cyanophenyl)pentyl, 6-(4 cyanophenyl)hexyl, -1,1-dimethyl-2-(2,4 dicyanophenyl)ethyl, 2-methyl-3-(2,4,6 tricyanophenyl)propyl, 2-(2-nitrophenyl)ethyl, 1-(3 nitrophenyl)ethyl, 3-(4-nitrophenyl)propyl, 4-(2 20 nitrophenyl)butyl, 5-(3-nitrophenyl)pentyl, 6-(4 nitrophenyl)hexyl, 1,1-dimethyl-2-(2,4 dinitrophenyl)ethyl, 2-methyl-3-(2,4,6 trinitrophenyl)propyl, 2-(2-phenylphenyl)ethyl, 1-(3 phenylphenyl)ethyl, 3-(4-phenylphenyl)propyl, 4-(2 25 phenylphenyl)butyl, 5-(3-phenylphenyl)pentyl, 6-(4 phenylphenyl)hexyl, 1,1-dimethyl-2-(2,4 diphenylphenyl)ethyl, 2-methyl-3-(2,4,6 triphenylphenyl)propyl, 2-(2-fluorophenyl)ethyl, 1-(3- 191 bromophenyl)ethyl, 3-(4-iodophenyl)propyl, 4-(2 bromophenyl)butyl, 5-(3-chlorophenyl)pentyl, 6-(4 bromophenyl)hexyl, 1,1-dimethyl-2-(2,4 dichlorophenyl)ethyl, 2-methyl-3-(2,4,6 5 trifluorophenyl)propyl, 2-(2-ethylphenyl)ethyl, 1-(3 propylphenyl)ethyl, 3-(4-butylphenyl)propyl, 4-(2 pentylphenyl)butyl, 5-(3-hexylphenyl)pentyl, 6-(4 trifluoromethylphenyl)hexyl, 1,1-dimethyl-2-(2,4 dimethylphenyl)ethyl, 2-methyl-3-(2,4,6 10 tri(trifluoromethyl)phenyl]propyl, 2-(2 ethoxyphenyl)ethyl, 1-(3-propoxyphenyl)ethyl, 3-(4 butoxyphenyl)propyl, 4-(2-pentyloxyphenyl)butyl, 5-(3 hexyloxyphenyl)pentyl, 6-(4 trifluoromethoxyphenyl)hexyl, 1,1-dimethyl-2-(2,4 15 dimethoxyphenyl)ethyl, 2-methyl-3-[2,4,6 tri(trifluoromethoxy)phenylipropyl, 2-methylthiobenzyl, 3-methylthiobenzyl, 4-methylthiobenzyl, 3,4 dimethylthiobenzyl, 2,3-dimethylthiobenzyl, 2-(2 ethylthiophenyl-)ethyl, 2-(4-methylthiophenyl)ethyl, 1 20 (3-propylthiophenyl)ethyl, 3-(4-butylthiophenyl)propyl, 4-(2-pentylthiophenyl)butyl, 5-(3 hexylthiophenyl)pentyl, 6-(4-methylthiophenyl)hexyl, 1,1-dimethyl-2-(2,4-dimethylthiophenyl)ethyl, 2-methyl 3-[2,4,6-trimethylthiophenyl]propyl, 2-methyl-4 25 cyanobenzyl, 3-ethoxy-4-ethoxycarbonylbenzyl, 4-phenyl 3-nitrobenzyl, 3-fluoro-4-methoxybenzyl, 4 trifluoromethyl-3-cyanobenzyl, and 3-trifluoromethoxy 3-fluorobenzyl groups.

192 [02981 Examples of the phenyl group which may have, on the phenyl ring, 1 to 3 groups selected from the group consisting of a lower alkoxy group which may have 5 aihalogen atom as a substituent and a lower alkyl group which may have a halogen atom as a substituent include phenyl groups which may have, on the phenyl ring, 1 to 3 groups selected from the group consisting of a linear or branched alkoxy group having 1 to 6 carbon atoms 10 which may have 1 to 3 halogen atoms as substituents and a linear or branched alkyl group having 1 to 6 carbon atoms and which may have 1 to 3 halogen atoms as substituents such as phenyl, 2-methylphenyl, 3 methylphenyl, 4-methylphenyl, 2-ethylphenyl, 3 15 ethylphenyl, 4-ethylphenyl, 4-isopropylphenyl, 3 butylphenyl, 4-pentylphenyl, 4-hexylphenyl, 3,4 dimethylphenyl, 3,4-diethylphenyl, 2,4-dimethylphenyl, 2,5-dimethylphenyl, 2,6-dimethylphenyl, 3,4,5 trimethylphenyl, 2-methoxyphenyl, 3-methoxyphenyl, 4 20 methoxyphenyl, 2-ethoxyphenyl, 3-ethoxyphenyl, 4 ethoxyphenyl, 4-isopropoxyphenyl, 3-butoxyphenyl, 4 pentyloxyphenyl, 4-hexyloxyphenyl, 3,4-dimethoxyphenyl, 3,4-diethoxyphenyl, 2,4-dimethoxyphenyl, 2,5 dimethoxyphenyl, 2,6-dimethoxyphenyl, 3,4,5 25 trimethoxyphenyl, 2-trifluoromethoxyphenyl, 3 trifluoromethoxyphenyl, 4-trifluoromethoxyphenyl, 2 (bromomethoxy)phenyl, 3-(2-chloroethoxy)phenyl, 4-(2,3 dichloropropoxy)phenyl, 4-(4-fluorobutoxy)phenyl, 3-(5- 193 chloropentyloxy)phenyl, 4-(5-bromohexyloxy)phenyl, 4 (5,6-dibromohexyloxy)phenyl, 3,4 di(trifluoromethoxy)phenyl, 3,4-di(4,4,4 trichlorobutoxy)phenyl, 2,4-di(3-chloro-2 5 methoxypropyl)phenyl, 2,5-di(3-chloropropoxy)phenyl, 2,6-di(2,2,2-trifluoroethoxy)phenyl, 3,4,5 tri(trifluoromethoxy)phenyl, 4-(2,2,2 trichloroethoxy)phenyl, 2-methyl-4 trifluoromethoxyphenyl, 3-ethyl-4 10 trichloromethoxyphenyl, 2-methoxy-4 trifluoromethoxyphenyl, 3-ethoxy-4 trichloromethoxyphenyl, 2-trifluoromethylphenyl, 3 trifluoromethylphenyl, 4-trifluoromethylphenyl, 2 (bromomethyl)phenyl, 3-(2-chloroethyl)phenyl, 4-(2,3 15 dichloropropyl)phenyl, 4-(4-fluorobutyl)phenyl, 3-(5 chloropentyl)phenyl, 4-(5-bromohexyl)phenyl, 4-(5,6 dibromohexyl)phenyl, 3,4-di(trifluoromethyl)phenyl, 3,4-di(4,4,4-trichlorobutyl)phenyl, 2,4-di(3-chloro-2 methylpropyl)phenyl, 2,5-di(3-chloropropyl)phenyl, 2,6 20 di(2,2,2-trifluoroethyl)phenyl, 3,4,5 tri(trifluoromethyl)phenyl, 4-(2,2,2 trichloroethyl)phenyl, 2-methyl-4 trifluoromethylphenyl, and 3-ethyl-4 trichloromethylphenyl groups. 25 [02991 Examples of the pyrrolidinyl lower alkyl group which may have, on the pyrrolidine ring, 1 to 3 lower alkyl groups which may have a hydroxyl group as a 194 substituent include pyrrolidinylalkyl groups which may have, on the pyrrolidine ring, 1 to 3 linear or branched alkyl groups having 1 to 6 carbon atoms which may have 1 to 3 hydroxyl groups as substituents and 5 whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as [(1, 2 or 3-)pyrrolidinyl]methyl, 2-[(l, 2 or 3-)pyrrolidinyllethyl, 1-[(1, 2 or 3-)pyrrolidinyllethyl, 3-[(1, 2 or 10 3-)pyrrolidinyl]propyl, 4-[(1, 2 or 3-)pyrrolidinyl]butyl, 5-[(1, 2 or 3-)pyrrolidinyl]pentyl, 6-[(1, 2 or 3-)pyrrolidinyl]hexyl, 1,1-dimethyl-2-[(1, 2 or 3-)pyrrolidinyl]ethyl, 2-methyl-3-[(l, 2 or 15 3-)pyrrolidinyl]propyl, [1-methyl-(2 or 3-)pyrrolidinyl]methyl, 2-(2-ethyl-(1, 3, 4 or 5-)pyrrolidinyl]ethyl, 1-[3-propyl-(1, 2, 4 or 5-)pyrrolidinyl]ethyl, 3-[1-butyl-(2 or 3-)pyrrolidinyl-]propyl, 4-[2-pentyl-(1, 3, 4 or 20 5-)pyrrolidinyl]butyl, 5-(3-hexyl-(1, 2, 4 or 5-)pyrrolidinyllpentyl, 6-[1,2-dimethyl-(3, 4 or 5-)pyrrolidinyl]hexyl, 1,1-dimethyl-2-[1,2,3-trimethyl (4 or 5-)pyrrolidinyl~ethyl, 2-methyl-3-[1-ethyl-2 methyl-(3, 4 or 5-)pyrrolidinyllpropyl, [1-(2 25 hydroxyethyl)-(2 or 3-)pyrrolidinyllmethyl, [2 hydroxymethyl-(1, 3, 4 or 5-)pyrrolidinyl]methyl, 2-[2 hydroxymethyl-(l, 3, 4 or 5-)pyrrolidinyl]ethyl, 1-[3 (3-hydroxypropyl)-(1, 2, 4 or 5-)pyrrolidinyl]ethyl, 3- 195 [1-(4-hydroxybutyl)-(2 or 3-)pyrrolidinyllpropyl, 4-[2 (5-hydroxypentyl)-(1, 3, 4 or 5-)pyrrolidinyl]butyl, 5 [3-(6-hydroxyhexyl)-(l, 2, 4 or 5-)pyrrolidinyl]pentyl, 6-[1,2-dihydroxymethyl-(3, 4 or 5-)pyrrolidinylJhexyl, 5 1, 1-dimethyl-2-(1,2,3-trihydroxymethyl-(4 or 5-)pyrrolidinyl]ethyl, 2-methyl-3-[2-(1,2 hydroxyethyl)-(1, 3, 4 or 5-)pyrrolidinyl]propyl, and [2-(2,3,4-trihydroxybutyl)-(1, 3, 4 or 5-)pyrrolidinyllmethyl groups. 10 [0300] Examples of the amino substituted lower alkyl group which may have a substituent selected from the group consisting of a phenyl group and a lower alkyl group include linear or branched alkyl groups having I 15 to 6 carbon atoms substituted with an amino group which may have 1 or 2 substituents selected from the group consisting of a phenyl group and a linear or branched alkyl group having 1 to 6 carbon atoms such as aminomethyl, 2-aminomethyl, 1-aminoethyl, 3 20 aminopropyl, 4-aminobutyl, 5-aminopentyl, 6-aminohexyl, 1, 1-dimethyl-2-aminoethyl, N,N-diethyl-2-aminoethyl, 2 methyl-3-aminopropyl, methylaminomethyl, 1 ethylaminoethyl, 2-propylaminoethyl, 3 isopropylaminopropyl, 4-butylaminobutyl, 5 25 pentylaminopentyl, 6-hexylaminohexyl, dimethylaminomethyl, 2-diisopropylaminoethyl, (N-ethyl N-propylamino)methyl, 2-(N-methyl-N-hexylamino)ethyl, phenylaminomethyl, 1-phenylaminoethyl, 2- 196 phenylaminoethyl, 3-phenylaminopropyl, 4 phenylaminobutyl, 5-phenylaminopentyl, 6 phenylaminohexyl, N-methyl-N-phenylaminomethyl, 2-(N ethyl-N-phenylamino)ethyl, (N-ethyl-N 5 phenylamino)methyl, and 2-(N-methyl-N-phenylamino)ethyl groups. [0301] Examples of the tetrahydrofuryl lower alkyl group which may-have a hydroxyl group as a substituent 10 on the lower alkyl group include tetrahydrofurylalkyl groups which may have a hydroxyl group as a substituent on the lower alkyl group and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 carbon atoms such as [(2 or 3-)tetrahydrofuryl]methyl, 2-[(2 15 or 3-)tetrahydrofuryl]ethyl, 1-[(2 or 3-)tetrahydrofuryl]ethyl, 3-[(2 or 3-)tetrahydrofuryl]propyl, 4-[(2 or 3-)tetrahydrofuryl]butyl, 5-[(2 or 3-)tetrahydrofu-ryl]pentyl, 6-[(2 or 20 3-)tetrahydrofuryl]hexyl, 1,1-dimethyl-2-[(2 or 3-)tetrahydrofuryllethyl, 2-methyl-3-[(2 or 3-)tetrahydrofuryl]propyl, 1-hydroxy-l-[(2 or 3-)tetrahydrofuryl]methyl, 2-hydroxy-2-[(2 or 3-)tetrahydrofuryl]ethyl, 2-hydroxy-1-[(2 or 25 3-)tetrahydrofuryl]ethyl, 3-hydroxy-3-[(2 or 3-)tetrahydrofuryl]propyl, 4-hydroxy-4-[(2 or 3-)tetrahydrofuryllbutyl, 5-hydroxy-5-[(2 or 3-)tetrahydrofuryl]pentyl, 6-hydroxy-6-[(2 or 197 3-)tetrahydrofuryllhexyl, 2-hydroxy-1,1-dimethyl-2-[(2 or 3-)tetrahydrofuryl]ethyl, and 3-hydroxy-2-methyl-3 ((2 or 3-)tetrahydrofuryl]propyl groups. [0302] 5 Examples of the phenoxy lower alkyl group which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a lower alkyl group and a nitro group include, in addition to the above described -phenoxy lower alkyl groups, 10 phenoxyalkyl groups which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a linear or branched alkyl group having 1 to 6 carbon atoms and a nitro group and whose alkyl moiety is a linear or branched alkyl group having 1 to 6 15 carbon atoms such as 2-methylphenoxymethyl, 3 methylphenoxymethyl, 4-methylphenoxymethyl, 3,4 dimethylphenoxymethyl, 2,3-dimethylphenoxymethyl, 3,4,5-trimethylphenoxymethyl, 2-(2-ethylphenoxy)ethyl, 2-(3-methylphenoxy)ethyl, 2-(4-methylphenoxy)ethyl, 1 20 (3-propylphenoxy)ethyl, 3-(4-butylphenoxy)propyl, 4-(2 pentylphenoxy)butyl, 5-(3-hexylphenoxy)pentyl, 6-(4 methylphenoxy)hexyl, 1,1-dimethyl-2-(2, 4 dimethylphenoxy)ethyl, 2-methyl-3-(2,4,6 trimethylphenoxy)propyl, 2-(4-nitro-3 25 methylphenoxy)ethyl, 4-nitrophenoxymethyl, 3 nitrophenoxymethyl, 2-nitrophenoxymethyl, 2-(2 nitrophenoxy)ethyl, 2-(4-nitrophenoxy)ethyl, 1-(3 nitrophenoxy)ethyl, 3-(4-nitrophenoxy)propyl, 4-(2- 198 nitrophenoxy)butyl, 5-(3-nitrophenoxy)pentyl, 6-(4 nitrophenoxy)hexyl, 1,1-dimethyl-2-(2,4 dinitrophenoxy)ethyl, and 2-methyl-3-(2,4,6 trinitrophenoxy)propyl groups. 5 [0303) Examples of the phenyl lower alkanoyl group include phenylalkanoyl groups whose alkanoyl moiety is a linear or branched alkanoyl group having 2 to 6 carbon atoms such as 2-phenylacetyl, 3-phenylpropionyl, 10 2-phenylpropionyl, 4-phenylbutyryl, 5-phenylpentanoyl, 6-phenylhexanoyl, 2,2-dimethyl-3-phenylpropionyl, and 2-methyl-3-phenylpropionyl groups. Examples of the phenyl group which may have, on the phenyl ring, 1 to 3 substituents selected from 15 the group consisting of a halogen atom and a lower alkyl group which may have a halogen atom include phenyl groups which may have, on the phenyl ring, 1 to 3 substituents selected from the group consisting of a halogen atom and a linear or branched alkyl group 20 having 1 to 6 carbon atoms which may have 1 to 3 halogen atoms such as phenyl, 3,4-difluorophenyl, 2 fluorophenyl, 3-bromophenyl, 4-iodophenyl, 4 methylphenyl, 2-methylphenyl, 3-methylphenyl, 2 ethylphenyl, 3-ethylphenyl, 4-ethylphenyl, 4 25 isopropylphenyl, 3-butylphenyl, 4-pentylphenyl, 4 hexylphenyl, 3,4-dimethylphenyl, 3,4-diethylphenyl, 2,4-dimethylphenyl, 2,5-dimethylphenyl, 2,6 dimethylphenyl, 3,4,5-trimethylphenyl, 2- 199 trifluoromethylphenyl, 3-trifluoromethylphenyl, 4 trifluoromethylphenyl, 2-(bromomethyl)phenyl, 3-(2 chloroethyl)phenyl, 4-(2,3-dichloropropyl)phenyl, 4-(4 fluorobutyl)phenyl, 3-(5-chloropentyl)phenyl, 4-(5 5 bromohexyl)phenyl, 4-(5,6-dibromohexyl)phenyl, 3,4 di(trifluoromethyl)phenyl, 3,4-di(4,4,4 trichlorobutyl)phenyl, 2,4-di(3-chloro-2 methylpropyl)phenyl,. 2,5-di(3-chloropropyl)phenyl, 2,6 di(2,2,2-trifluoroethyl)phenyl, 3,4,5 10 tri(trifluoromethyl)phenyl, 4-(2,2,2 trichloroethyl)phenyl, 2-methyl-4 trifluoromethylphenyl, 3-ethyl-4-trichloromethylphenyl, 2-chloro-4-trifluoromethylphenyl, 3-ethyl-4 fluorophenyl, 3-fluoro-4-trichloromethylphenyl, 2 15 methyl-3-trifluoromethyl-4-trifluoromethylphenyl, 3 fluorophenyl, 4-fluorophenyl, 2-bromophenyl, 4 bromophenyl, 2-iodophenyl, 3-iodophenyl, 2,3 dibromophenyl, 2,4-diiodophenyl, 2,5-difluorophenyl, 2,6-dichlorophenyl, 2,4,6-trichlorophenyl, 2,4 20 difluorophenyl, 3,5-difluorophenyl, 2,6-difluorophenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2,3 dichlorophenyl, 2,4-dichlorophenyl, 2,5-dichlorophenyl, 3,4-dichlorophenyl, 2,6-dichlorophenyl, 3,5 dichlorophenyl, 2,4,6-trifluorophenyl, and 2,4 25 difluorophenyl groups. [0304] Examples of the 5-to 7-membered saturated heterocyclic group formed by mutually binding R 20 and 200 21 22 23 26 27 29 3 23 R , R and R, R and R , R and R 3 or R 3 and R 3 together with the nitrogen atoms bound to them, through or not through a nitrogen atom, an oxygen atom or a sulfur atom, include pyrrolidinyl, piperidinyl, 5 piperazinyl, morpholino, thiomorpholino, and homopiperazinyl groups. [0305] Examples of the phenoxy lower alkyl group which may have, -on the phenyl ring, a lower alkyl group 10 as a substituent include, in addition to the above described phenoxy lower alkyl groups, phenoxyalkyl groups which may have, on the phenyl ring, 1 to 3 linear or branched alkyl groups having 1 to 6 carbon atoms as substituents and whose alkyl moiety is a 15 linear or branched alkyl group having 1 to 6 carbon atoms such as 2-methylphenoxymethyl, 3 methylphenoxymethyl, 4-methylphenoxymethyl, 3,4 dimethylphenoxymethyl, 2, 3-dimethylphenoxymethyl, 3,4, 5-trimethylphenoxymethyl, 2-(2-ethylphenoxy)ethyl, 20 2- (4-methylphenoxy)ethyl, 1- (3-propylphenoxy) ethyl, 3 (4-butylphenoxy)propyl, 4- (2-pentylphenoxy)butyl, 5- (3 hexylphenoxy)pentyl, 6-(4-methylphenoxy)hexyl, 1,1 dimethyl-2- (2, 4-dimethylphenoxy) ethyl, and 2-methyl-3 (2,4,6-trimethylphenoxy)propyl groups. 25 A compound represented by the general formula (1) or a salt thereof is more preferred, wherein

X

1 represents a nitrogen atom or a group -CH=, R' represents a group -Z-Rs, 201 Z represents a group -N (R )-B-, a group -B-N (R') -, a group -Bo-0- or a group -N (R 9 a) -CO-N- (R 9 b) -, R represents a hydrogen atom, a lower alkyl group that may have a lower alkoxy group as a substituent, a lower 5 alkanoyl group, a lower alkylsulfonyl group or a phenyl lower alkyl group, B represents a group -CO- or a lower alkylene group,

B

0 represents a lower alkylene group, R9a represents a-hydrogen atom or a lower alkyl group, 10 R represents a hydrogen atom or a lower alkyl group,

R

6 represents a group (Formula 58] (R7) RI represents a halogen atom or a lower alkyl group that may have a halogen atom as a substituent,. 15 m represents an integer of 1 or 2 (when m represents 2, two R7s may be identical or different) and R2 represents a hydrogen atom, a halogen atom, or a lower alkyl group, Y represents a group -0-, or a group -N(R 5 )-, 20 R 5 represents a hydrogen atom, or a lower alkyl group, A represents a group (Formula 59]

(R

202 p represents 1 or 2,

R

3 represents a hydrogen atom, a lower alkoxy group, a halogen atom, or a lower alkyl group that may have a halogen atom as a substituent, 5 R 4 represents a group - (T) 1-N (R") R5, T represents a group -N(R 17

)-B

3 -CO-, a group -B 4 -CO-, or a group -CO-, R1 7 represents a hydrogen atom, or a lower alkyl group,

B

3 represents a -lower alkylene group, 10 B 4 represents a lower alkenylene group or a lower alkylene group that may have a hydroxyl group as a substituent, 1 represents 0 or 1,

R

14 represents a hydrogen atom or an alkyl group that' 15 may have a hydroxyl group as a substituent,

R

15 represents (36a) a piperazinyl-substituted oxalyl group that may have 1 to 3 groups selected from the group consisting of a phenyl lower alkyl group (that may have 1 to 3 groups selected from the group 20 consisting of a lower alkylenedioxy group and a lower alkoxy group as a substituent(s) on the phenyl ring) and a py.ridyl lower alkyl group as a substituent(s) on the piperazine ring,

R

4 and R1 5 , together with the nitrogen atom to which 25 they bind, form a heterocyclic group which is piperidinyl or piperazinyl group, wherein the heterocyclic ring may be substituted by a group selected from the group consisting of (28) a 203 phenyl-substituted lower alkyl group that may be substituted by a group, on the phenyl ring, selected from the group consisting of a lower alkanoyl group, an amino group that may have a lower alkanoyl group as a 5 substituent, a lower alkoxycarbonyl group, a cyano group, a nitro group, a phenyl group, a halogen atom, a lower alkyl group that may have a halogen atom as a substituent, a lower alkoxy group that may have a halogen atom as a substituent, a phenyl lower alkoxy 10 group, a hydroxyl group, and a lower alkylenedioxy group (49) a group -(Bi 2 CO)t-N(R )R , or (84) a group (0-B 5 ) s-CO-N (R 2 ) R 2 ,

B

12 represents a lower alkylene group, t represents 0 or 1, 15 R 2 and R , together with the nitrogen atom to which they bind, form a saturated heterocyclic group which is piperidinyl or piperazinyl group that, on the heterocyclic ring, may be substituted by a phenyl lower alkyl group that may have a lower alkylenedioxy group 20 as a substituent on the phenyl ring,

B

15 represents a lower alkylene group, s represents 0 or 1, R and R may be identical or different and each represent a hydrogen atom, a lower alkyl group, a 25 phenyl lower alkyl group, or an imidazolyl lower alkyl group, and R 2 and R , together with the nitrogen atom to which they bind, may bind to each other, directly or via a nitrogen atom, oxygen atom, or sulfur atom to 204 form a 5- to 7-membered saturated heterocyclic ring, (wherein the heterocyclic ring may be substituted by 1 to 3 phenyl lower alkyl groups that may have a lower alkylenedioxy group on the phenyl ring). 5 For example, a compound represented by the general formula (1) or a salt thereof is further more preferred, wherein Xi represents a nitrogen atom, R represents a group -Z-R , 10 Z represents a group -N(R 8 )-B-, Re represents a hydrogen atom, or a lower alkyl group that may have a lower alkoxy group as a substituent, B represents a group -CO-,

R

6 represents a group 15 [Formula 60]

R

7 represents a halogen atom or a lower alkyl group that may have a halogen atom as a substituent, m represents an integer of 1 or 2 (when m represents 2, two R 7 s may be identical or different) and 20 R 2 represents a hydrogen atom' Y represents a group -0-, or a group -N(R5)-,

R

5 represents a hydrogen atom, or a lower alkyl group, A represents a group 205 [Formula 61] p :represents 1 or 2,

R

3 represents a hydrogen atom, a lower alkoxy group, a halogen atom, or a lower alkyl group that may have a 5 halogen atom as a substituent,

R

4 represents a -group -(T),-N(R1)R5, T represents a group -N (R") -B 3 -CO-, a group -B 4 -CO-, or a group -CO-, R1 7 represents a hydrogen atom, or a lower alkyl group, 10 B 3 represents a lower alkylene group,

B

4 represents a lower alkylene group that may have a hydroxyl group as a substituent, 1 represents 0 or 1,

R

4 and R1 5 , together with the nitrogen atom to which 15 they bind, form a heterocyclic group which is piperidinyl or piperazinyl group that, on the heterocyclic ring, may be substututed by (28) a phenyl substituted lower alkyl group that may be substituted by a lower alkylenedioxy group on the phenyl ring. 20 Another more preferred example is a compound represented by the general formula (1) or a salt thereof, wherein

X

1 represents a nitrogen atom, R' represents a group -Z-Rs 25 Z represents a group -N (R8) -B-, 206 R8 represents a hydrogen atom, or a lower alkyl group that may have a lower alkoxy group as a substituent, B represents a group -CO-,

R

6 represents a group 5 [Formula 62] (R7~ R represents a halogen atom. or a lower alkyl group that may have a halogen atom as a substituent, m represents an integer of 1 or 2 (when m represents 2, two R7s may be identical or different) and 10 R 2 represents a hydrogen atom, Y represents a group -0-, or a group -N(R 5 )-,

R

5 represents a hydrogen atom, or a lower alkyl group, A represents a group [Formula 63]

(R

3 15 p represents 1 or 2,

R

3 represents a hydrogen atom, a lower alkoxy group, a halogen atom, or a lower alkyl group that may have a halogen atom as a substituent,

R

4 represents a group -(T)1-N(R")R1, 20 R 7 represents a hydrogen atom, or a lower alkyl group,

B

3 represents a lower alkylene group,

B

4 represents a lower alkylene group that may have a 207 hydroxyl group as a substituent, 1 represents 0,

R

14 and R1 5 , together with the nitrogen atom to which they bind, form a heterocyclic group which is .5 piperidinyl or piperazinyl group wherein, on the heterocyclic ring, one substituent may be present which is selected from the group consisting of (49) a group -(B 12 CO)t-N(R2 )R , and (84) a group 21 27 (0-Bi) s-CO-N (R ) R 10 B 12 represents a lower alkylene group, t represents 0 or 1,

R

20 and R 2 , together with the nitrogen atom to which they bind, form a saturated heterocyclic group which is piperazine or piperidine 15 wherein, on the heterocyclic ring, one substituent may be present which is a phenyl lower alkyl group that may have a lower alkylenedioxy group as a substituent on the phenyl ring,

B

15 represents a lower alkylene group, 20 s represents 0 or 1,

R

2 and R , together with the nitrogen atom to which they bind, bind to each other, directly or via an oxygen atom or nitrogen atom to form a 6-membered saturated heterocyclic ring (wherein the heterocyclic 25 ring may be substituted by 1 to 3 phenyl lower alkyl groups that may have a lower alkylenedioxy group as a substituent on the phenyl ring). [0306] 208 The aromatic compound (1) or a salt thereof contained in the STAT3/5 activation inhibitor of the present invention includes a stereoisomer, optical isomer and solvate (hydrate, ethanolate, etc.). 5 [0307] Of the aromatic compounds (1), a'compound having a basic group may be easily reacted with a conventional pharmacologically acceptable acid to form a salt. Examples of such acid include mineral acids 10 such as hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, and phosphoric acid, and organic acids such as methanesulfonic acid, p-toluenesulfonic acid, acetic acid, citric acid, tartaric acid, maleic acid, fumaric acid, malonic acid, and lactic acid. 15 (0308] Of the aromatic compounds (1), a compound having an acidic group may be easily reacted with a conventional pharmacologically acceptable basic compound to form a salt. Examples of such a salt 20 include a sodium salt, a potassium salt, and a calcium salt. [0309]. The aromatic compound (1) or a salt thereof can be prepared in the same manner as in W02006/014012. 25 [0310] Next, a medical formulation containing the aromatic compound (1) or a salt thereof as an active ingredient will be described.

209 [0311] The medical formulation is obtained by formulating the aromatic compound (1) or a salt thereof in the form of pharmaceutical preparation, and more 5 specifically, prepared using a diluent or an excipient such as a filler, expander, binder, moistener, disintegrator, surfactant, or lubricant. [0312] The form of such a medicinal formulation may 10 be chosen from various forms depending upon the therapeutic purpose, and typical forms include tablets, pills, powders, liquids, suspensions, emulsions, granules, capsules, suppositories, and injections (liquids, suspensions). 15 [0313] The carrier to be used in forming tablets may be chosen widely from conventionally known ones. Examples of the carrier include excipients such as lactose, saccha-rose, sodium chloride, glucose, urea, 20 starch, calcium carbonate, kaolin, and crystalline cellulose, binders such as water, ethanol, propanol, simple syrup, a glucose solution, a starch solution, a gelatin solution, carboxymethylcellulose, shellac, methylcellulose, potassium phosphate, and 25 polyvinylpyrrolidone, disintegrators such as dried starch, sodium arginate, agar powder, laminaran powder, sodium bicarbonate, calcium carbonate, polyoxyethylene sorbitan fatty acid ester, sodium lauryl sulfate, 210 stearic acid monoglyceride, starch, and lactose, anti disintegrators such as saccharose, stearine, cacao butter, and hydrogenated oil, absorbefacients such as quartenary ammonium base and sodium lauryl sulfate, 5 wetting agents such as glycerol and starch, adsorbents such as starch, lactose, kaolin, bentonite, and colloidal silicate, and lubricants such as purified talc, stearate, boric acid powder, and polyethylene glycol. 10 (0314] Further, tablets may be coated in a conventional manner as needed. Examples of' coated tablets include sugar-coated tablets, gelatin-coated tablets, enteric-coated tablets, film-coated tablets, 15 or double or multi-layered tablets. [03151 The carriers to be used in forming pills may be chosen widely from the conventionally known ones. Examples of the carrier include excipients such as 20 glucose, lactose, starch, cacao butter, hydrogenated vegetable oil, kaolin, and talc, binders such as gum arabic powder, tragacanth powder, gelatin, and ethanol, and disintegrators such as laminaran and agar. [0316] 25 The carriers to be used in forming suppositories may be chosen widely from the conventionally known ones. Examples of the carrier include polyethylene glycol, cacao butter, higher 211 alcohols, esters of higher alcohols, gelatin, and semi synthetic glycerides. [0317] When liquid, emulsion and suspension are 5 prepared as injection preparations, they are preferably sterilized and controlled to be isotonic with the blood. Diluents to be used in forming these liquid, emulsion and suspension preparations may be chosen widely from the -conventionally known ones. Examples of 10 the diluents include water, ethanol, propylene glycol, ethoxylated isostearyl alcohol, polyoxylated isostearyl alcohol, and polyoxyethylene sorbitan fatty acid ester. In this case, the medical formulations may contain sodium chloride, glucose or glycerol in a sufficient 15 amount to prepare isotonic solutions. Also, conventional solubilizers, buffers, analgesics, and the like, and, as necessary, coloring agents, preservatives, spices, flavors, sweets and the like, or other pharmaceuticals may be contained. 20 [0318] Although the amount of the aromatic compound (1) or a salt thereof contained in a medical formulation is not particularly limited and may be appropriately selected from a wide range of compounds. 25 It is preferable that the aromatic compound (1) or a salt thereof is contained in an amount of 1 to 70 wt% in a medical formulation. [0319] 212 The method for administrating a medical formulation according to the present invention is not particularly limited. The medical formulation can be administered by a method determined depending upon the 5 form of medical formulation, patient's age, sex, severity of the disease and other conditions. For example, tablets, pills, liquids, suspensions, emulsions, granules and capsules are administered orally. The injection formulations are administered 10 singly or by mixing with a conventional fluid replacement such as a glucose solution or amino acid solution, intravenously or, as necessary, singly administered intramuscularly, intradermally, subcutaneously or intraperitoneally. Suppositories a-re 15 administered into the rectum. [0320] The dosage for the above mentioned medical formulation may be chosen appropriately depending upon the usage, patient's age, sex and severity of the 20 disease and other conditions. Typically, 0.001 to 100 mg per kg (body weight) per day, preferably 0.001 to 50 mg per kg (body weight) per day, is administered once or in several times a day. [0321] 25 Since the above described dosage varies depending upon various conditions, the dosage may be smaller than the lower limit of the range described above or larger than the upper limit of the range 213 described above. [03221 The aromatic compound (1) or a salt thereof in the present invention has a STAT3/5 activation 5 inhibitory action and useful as a STAT3/5 activation inhibitor. (0323] The aromatic compound (1) or a salt thereof has a STAT3 activation inhibitory action and therefore 10 useful as a medicinal drug for preventing or treating autoimmune disease, diabetes, infection, central disease, cancer-associated disease or psoriasis. [0324] Examples of the autoimmune disease include 15 autoimmune blood dyscrasia (for example, hemolytic anemia, aplastic anemia and idiopathy thrombocytopenia), rheumatism, systemic lupus erythematosus, polychondritis, scleroderma, Wegener's granulomatosis,, dermatomyositis, chronic active 20 hepatitis, severe myasthenic, Stevens-Johnson syndrome, idiopathic sprue, inflammatory bowel disease (for example,. ulcerative colitis and Crohn disease), endocrine ophthalmopathy, Graves' disease, sarcoidosis, multiple sclerosis, primary biliary cirrhosis, 25 juvenile-onset diabetes (Type I diabetes), uveitis (front and rear uveitis), keratoconjunctivitis sicca, vernal keratoconjunctivitis, psoriatic arthritis, glomerulonephritis (with and without a nephrosis 214 symptom, such as idiopathic nephrotic syndrome or minimal-change nephropathy). [0325] As the central disease, Alzheimer's disease 5 may be mentioned. [03261 As the cancer-associated disease, cachexia may be mentioned. [0327) 10 As the infection, infection with hepatitis C virus (HCV) and infection with Kaposi's sarcoma associated herpes virus (KSHV) may be mentioned. Further, the compound of the present invention has a STAT5 activation inhibitory action and 15 is useful as STATS activation inhibitor, specifically as preventive or treating agent for autoimmune diseases, allergies, inflammations, hyperprolactinemia and the like as mentioned above. [03281 20 In the present invention, the aromatic compound (1) or a salt thereof may be used in combination with another STAT3 activation inhibitor, STAT3 activity inhibitor, immunosuppressive agent, antiphlogistic, therapeutic agent for diabetes, 25 therapeutic agent for infectious disease, therapeutic agent for central disease, therapeutic agent for cancer-associated, therapeutic agent for psoriasis, antitumor agent, and fibrosis suppressive agent.

215 [03291 The patents, patent applications and literatures cited in the present invention are incorporated herein by reference. 5 [Example 1] [0330] Effect of test compound on the amount of STAT3 activated in nucleus of Hep G2 cells after stimulation with IL-6 10 1) Culture After Hep G2 cells are washed with PBS (-) twice, they are washed once with trypsin/EDTA solution and detached using trypsin/EDTA solution. The cells are centrifuged and suspended in a medium supplemented 15 with antibiotics (MEM medium (10% FBS + antibiotic (100 U/mL penicillin + 100 pg/mL streptomycin)). After the number of cells is counted, the cells are seeded on 12 well plates at a density of 1.2 x 105 cells/lmL per well. 20 Two days after seeding, the culture medium is replaced with 1 mL of antibiotic-free culture medium (MEM medium (10%FBS)). 2) Addition of test compound Two days after medium replacement, a test 25 compound is added so as to obtain concentrations of 0, 1, 10 and 100 nM. Three hours after addition of the test compound, IL-6 (Code No. KTS102S manufactured by 216 Kamakura Techno Science Inc.) is added at a final concentration 0 or 500 ng/mL. Five minutes after addition of IL-6, extraction is performed by use of a Nuclear Extraction 5 Kit (Code No. 40410 manufactured by Active Motif Inc.) 3) Extraction of nuclear fraction The supernatant of the cells is removed by suction. The cells are washed with 1 mL of ice-cold phosphatase inhibitor-containing PBS (hereinafter, 10 PBS/phosphatase inhibitor) and the supernatant of the cells is again removed by suction. The cells are collected with a cell scraper in 0.6 mL of ice-cold PBS/phosphatase inhibitors and divided into ice-cold 1.5 mL microtubes. 15 After the microtube is centrifuged at 4*C and a rate of 400 x g for 5 minutes, the supernatant is removed. The cells are resuspended in 0.2 mL of hypotonic buffer by pipetting up and down several times 20 and kept on ice for 15 minutes. To this suspension, 10 pL .of a detergent is added and vortexed for 10 seconds. After centrifugation is performed at 4*C and a rate of 20,400 x g for 30 seconds, the supernatant is removed. 25 To the resultant cells, 50 pL of Complete Lysis Buffer is added. The suspension is pipetted, vortexed for 10 seconds and shaken on ice for 30 minutes.

217 After vortexed for 30 seconds, the suspension is centrifuged at 4 0 C and a rate of 20,400 x g for 10 minutes. The supernatant is divided into ice-cold 1.5 5 mL microtubes and stored at -80 0 C. 4) DNA binding is measured by use of TransAM STAT3 Kit (Code No. 45196 manufactured by Active Motif Inc.) To each of the wells of an ELISA plate, 30 iL 10 of Complete Binding Buffer and 20 pL of a sample (extracted from a nucleus) are added. A positive control: 10 p.l of Hep G2 nuclear extract (2.5 mg/mL) is diluted with 40 pxL of Complete Lysis Buffer (10 pg/20 pL) . Dilutions were prepared -at 15 5, 2.5, 1.25, 0.625 and 0.313 g/20 pL by sequential half-fold dilution, and 20 pL of dilutions is added to each well. Blank well: 20 p±L of Complete Lysis Buffer is added. 20 After the plate is sealed, the plate is gently shaken at room temperature for one hour, followed by washing with 200 pL of washing buffer three times. 100 pL of a STAT3 antibody is added and the 25 plate is sealed. Thereafter, the plate is gently shaken at room temperature. One hour later, the plate is washed with 200 pL of washing buffer three times. After washing, 100 pL of an HRP-conjugated antibody is 218 added. The plate is sealed, gently shaken at room temperature for one hour, followed by washing with 200 pL of washing buffer four times. After that, 100 pL of developing solution 5 returned to room temperature is added, and the plate is incubated for 2 to 10 minutes protected from light. After color development is confirmed, 100 pL of stop solution is added and absorbance at 450 nm and 630 nm is determined within 5 minutes. 10 5) The results of test compounds listed in Table 1 below are shown in Table 2.

219 (0331] [Table 1] -Test compounds R2 XiY-A Test compound No. RR 2 X, -Y-A ( )* _________ (Ex. 582) H H- N (a~' 109) Es0H4 2 H- N (Ex. 1039) H .3 4 0 F 3 C H - N 09 (Ex. 322) Fa0H 4 F H- N (Ex 1503) F3~ X 0 5 F H- Cii (*x 1049) H nme H- N (E. 940)OI = 7 FC - "3 H- N (Ex. 2228) 8 H- N (Ex. 1202) *: )Numerical value within the parentheses is the number of Example in WO 2006/014012 220 [0332] [Table 2] *Results Test compound No. IC 50 (nM) 1 < 150 2 < 150 3 < 150 4 < 150 5 < 150 6 < 150 7 < 150 8 < 150 (Example 2] (0333] Effect of test compound on suppressing phosphorylation of STAT3 5 (1) Cells Seeding of cells After Hep G2 cells are washed with PBS (-) twice, they are washed and removed by trypsin/EDTA and further removed by trypsin/EDTA. The cells are 10 centrifuged and suspended in a medium supplemented with antibiotics (MEM medium (10% FBS + antibiotic (100 U/mL penicillin + 100 pg/mL streptomycin))). After the number of cells is counted, the cells are seeded in a 6-well plate in a rate of 2.4 x 10 5 /2mL per well.

221 Two days later, the medium supplemented with antibiotics is replaced with a medium supplemented with no antibiotics (MEM medium (10%FBS)). Treatment of cells with medicinal drug 5 Two days after medium replacement, a test compound is added so as to obtain concentrations of 0, 1, 10 and 100 nM. Three hours after addition of the test compound, IL-6 (Code No. KTS102S manufactured by 10 Kamakura Techno Science Inc.) is added so as to obtain a concentration 100 ng/mL. Recovery of cells Five minutes after addition of IL-6, the cells are washed with cooled PBS (-) twice, and peeled 15 off from the plate by a scraper. The cells are collected in a 1.5 mL microtube by use of PBS (-). The cells collected in the 1.5 mL microtube are centrifuged and the supernatant is removed. The cells collected in the 1.5 mL microtube are cryopreserved in a cryogenic 20 refrigerator until use. Lysis treatment To the frozen cells, RIPA buffer is added. The frozen cells are suspended by use of 1 mL syringe with a 26G x 1/2 injection needle and the suspension 25 solution is allowed to stand still in ice water for 30 to 60 minutes. The cell suspension solution is centrifuged and the supernatant (cell lysate) is transferred to a new tube. The cell lysate collected 222 in the tube is cryopreserved in a cryogenic refrigerator until use. Measurement of protein concentration The amount of protein of each cell lysate is 5 measured in accordance with the protocol attached to a BCA protein assay reagent set. (2) Western blotting analysis - PAGE (Electrophoresis) After-the protein amount of each cell lysate 10 is set at the same value, denature treatment is performed under reduced conditions. After the samples and a molecular marker are applied to polyacrylamide gel, electrophoresis is performed. - Blotting 15 After completion of electrophoresis, the gel is equilibrated with the solution to be used in transferring. The proteins developed on the polyacrylamide gel are transferred onto a PVDF (polyvinylidene 20 difluoride) film by a semidry type transferring apparatus. - Blocking/washing After the PVDF film is washed, it is soaked in blocking buffer (5% BSA) to perform blocking. 25 - Primary antibody (Phospho-STAT3 (Ser 727) Antibody or Phospho-STAT3 (Tyr 705) Antibody) Blocked PVDF film is reacted with the primary antibody.

223 Secondary antibody (Anti-rabbit-IgG HRP-linked Antibody) /washing After washed, the PVDF film is reacted with the HRP labeled antibody. 5 - Detection of Color emission by ECL After the PVDF film is washed, color is allowed to emit by use of ECL Western Blotting Detection Reagents and fluorescence is detected by LAS 3000. 10 - According to the aforementioned method, the effect of the test compound on surppressing phosphorylation of STAT3 is measured. (Example 3) [0334] 15 Effect of test compound on prolactin-induced STAT5 activation in 22Rvl cells 1) Culture After 22Rvl cells cryopreserved are subcultured at -least twice, they are subjected to a 20 test. After culture until subconfluency, the cells are washed with D-PBS (-). Thereafter, they are detached using trypsin/EDTA solution and suspended in a medium (RPMI-1640 medium (10% FBS + antibiotics (100 U/mL penicillin + 100 pig/mL streptomycin)). The cell 25 suspension solution is centrifuged at 150 x g, for 5 minutes at 20 to 25 0 C. The supernatant is removed and the pellet is resuspended in the medium. An aliquot of the cell suspension solution is taken and dead cells 224 are stained with trypan blue. The number of viable cells is counted by a hemocytometer. A cell suspension solution is prepared so as to contain 2 x 105 cells/mL, and cells are seeded in a 12 well-plate in a rate of 2 5 x:105 cells/mL per well. Cells are cultured in a CO 2 incubator (5% C0 2 , 37 0 C). 2) Addition of test compound Two days after seeding, a test compound is added so as to obtain concentrations of 0 and 1000 nM. 10 Three hours after addition of the test compound, recombinant human prolactin (rhPRL, R&D systems Inc.) is added so as to obtain a concentration of 0 or 250 ng/mL. 3) Extraction of cytoplasmic fraction 15 Fifteen minutes after addition of prolactin, extraction is performed by a Nuclear Extract Kit (Code No. 40410 manufactured by Active Motif Inc.). At 15 minutes after the addition of prolactin, the supernatant is removed and prolactin-stimlation is 20 immediately stopped by adding 1 ml of ice-cold PBS/phosphatase inhibitor. After aspirating 1mL of ice-cold PBS/phosphatase inhibitor, 0.6 mL of ice-cold PBS/phosphatase inhibitor is added and centrifuged at 200 x g, for 5 minutes at 4 0 C. 25 After the supernatant is removed, 0.2 mL of hypotonic buffer is added and suspended. After the suspension is kept on ice for 15 minutes, 10 pL of a detergent is added. After the solution is further 225 stirred, it is centrifuged at 14,000 x g, for one minute at 4 0 C. The resultant supernatant (cytoplasmic fraction) is divided to three ice-cold 96-well plates, and stored in a freezer of -80 0 C. 5 4) Measurement of activated STAT5 Measurement is performed by use of reagents attached to TransAMTMSTAT family kit. To describe more specifically, to each of the wells of an ELISA plate of the TransAMTMSTAT family kit, 30 pL of Complete Binding 10 Buffer is added, and thereafter, 20 p.L of the cytoplasmic fraction is added. As a sample for calibration curve, 12 pL of a cell nuclear fraction reference sample (Nb2 nuclear fraction (prolactin stimulated, 2.5 4g/pL)) attached to the TransATM STAT 15 family kit is diluted with 48 pL of Complete Lysis Buffer (to 10 pg/20 pL), and further serially diluted in half to prepare diluted solutions of 5, 2.5, 1.25, 0.625, 0.313, and 0.156 pg/20 ;AL. 20 p.1 of each of the dilution solution is added to well. As a blank, 20 p.L 20 of Complete Lysis Buffer is added. After addition of a sample, the plate is sealed and gently shaken at room temperature for one hour. After that, the plate is washed with 200 pL of wash buffer three times. Next, 100 p.L of STAT5B antibody is added, sealed and 25 incubated at room temperature without agitation. One hour later, the plate is washed with 200 pL of wash buffer three times. 100 pL of a Horseradish Peroxidase (HRP)-conjugated antibody is added, sealed and 226 incubated at room temperature without agitation. One hour later, the plate is washed with 200 p.L of wash buffer four times and 100 pL of a developing solution is added. The plate is incubated for 2 to 10 minutes 5 protected from light. After color development is confirmed, 100 lL of a stop solution is added. Immediately after, absorbance at 450 nm (measurement wavelength) and 630 nm (reference wavelength) is determined using a plate reader. 10 The amount of phosphorylated STAT5B dimer is estimated based on a calibration curve. Further, a ratio (T/C %) of the amount of phosphorylated STAT5B dimer in the presence of each medicinal drug relative to that in the absence of a medicinal drug is 15 calculated. The results of test compounds listed in Table 1 are shown in Table 3. [0335] [Table 3] Test compound No. T/C % Object (DMSO) 0 100 1 1000 nM <30 2 1000 nM <30 3 1000 nM <30 4 1000 nM <30 5 1000 nM <30 6 1000 nM <30 7 1000 nM <30 8 1000 nM <30 227 [0336] [Example 4] Effect of test compound on dextran sulfate sodium (DSS) induced colitis model 5 1. Induction of colitis by OSS After female mice C57BL/6J Jms Slc are preliminarily raised for a week, the mice are grouped based on the body weight (BW) of the mice at the grouping day and in accordance with stratified random 10 sampling. DSS (Lot No, 4556J, MP Biomedicals) is dissolved in Otsuka distilled water to prepare a 4% DSS solution. Mice are allowed to drink the 4% DSS solution freely for 7 days from the following day (Day 15 2) after initiation of administration to induce colitis. 2. Administration of test compound and solvent Based on the body weight before administration of the DSS solution (Day 1) and the most 20 recent body weight after administration of the DSS solution, each administration solution is orally administered in a dose of 10 mL/kg once a day. The dose of the test compound is 300 mg/kg. An administration solution is prepared by 25 suspending a test compound in a 5% gum arabic solution so as to contain the test compound in a concentration of 30 mg/mL. 3. Autopsy 228 Autopsy is performed at Day 8. 4. Collection of blood After blood is collected from the abdominal posterior vena cava under anaesthesia with diethyl 5 ether, it is immediately transferred to a BD Microtainers (Nippon Becton, Dickinson and Company), mixed by overturning the Micro-Tina and allowed to stand still in ice. The Micro-Tina is centrifuged by use of a refrigerated centrifuge (HITACHI CF9RX, T3S51 10 rotor) at 4*C and 2,150 x g for 20 minutes to obtain heparin plasma. The plasma dispensed is cryopreserved in a freezer (-80*C) until use in measurement. 5. Collection of organ After the abdominal posterior vena cava is 15 cut under anaesthesia with diethyl ether to kill a mouse by blood letting, the spleen is excised out. The weight of the spleen is measured by an electronic force balance. And, the large intestine was immediately removed for measurement of intestinal length and 20 evaluation of intestinal shortening. 6. Measurement Items Body weight Body weight is measured at Day 1 (day of grouping), 3, 5, 7 and 8 (day of autopsy) by an 25 electronic force balance. Based on the body weight of Day 1 (day of grouping) and Day 8 (day of autopsy), a body weight change is calculated.

229 Spleen weight The wet weight of the spleen is measured by an electronic force balance. In addition, from the measurement results of 5 spleen weight, a ratio (T/C %) of the spleen weight relative to an average spleen weight of a control group and a spleen weight gain inhibition ratio (IR %) are calculated. Intestinal length 10 The length of the large intestine is measured by a scale. In addition, from the measurement results of intestinal length, a ratio (T/C%) of the intestinal length relative to an average intestinal length of a 15 control group and an intestinal shortening inhibition ratio (IR%) are calculated. The results of test compounds are shown in Table 4. [Table 4] Spleen weight gain inhibition Test compound No. ratio IR (%) 9 >40 (Example 305 of W02006/014012) 10 >40 (Example 1105 of W2006/014012) 11 >40 (Example 1503 of W02006/014012) H:\,br\InlInoven\NRPortbI\DCC\RBR\6393569_lI.DOC 230 The reference in this specification to any prior publication (or information derived from it), or to any matter which is known, is not, and should not be taken as an acknowledgment or admission or any form of suggestion that that 5 prior publication (or information derived from it) or known matter forms part of the common general knowledge in the field of endeavour to which this specification relates. Throughout this specification and the claims which follow, 10 unless the context requires otherwise, the word "comprise", and variations such as "comprises" and "comprising", will be understood to imply the inclusion of a stated integer or step or group of integers or steps but not the exclusion of any other integer or step or group of integers or steps. 15

Claims (9)

1. A method for preventing or treating a symptom or disease associated with activation of STAT3/5 by 5 administering to a patient an effective amount of an aromatic compound represented by the general formula (1) or a salt thereof as an active ingredient: R1 [Formula 1] wherein X, represents a nitrogen atom, 10 R 1 represents a group -Z-R , Z represents a group -N(R8)-B R represents a hydrogen atom or a lower alkyl group that may have a lower alkoxy group as a substituent, B represents a group -CO-, 15 R' represents a group [Formula 2] R 7 represents a halogen atom or a lower alkyl group that may have a halogen atom as a substituent, 20 m represents an integer of 1 or 2 (when m represents 2, two R 7 s may be identical or different) and R 2 represents a hydrogen atom, 232 Y represents a group -0-- or a group -N(R5) R 5 represents a hydrogen atom or a lower alkyl group, A represents a group [Formula 3] 5 p represents 1 or 2, R 3 represents a hydrogen atom, a lower alkoxy group, a halogen atom or a lower alkyl group that may have a halogen atom as a substituent, R 4 represents a group -(T)i-N(R 4 ) R 5 , 10 T represents a group -N(R1 7 )-B 3 -CO-, a group -B 4 -CO- or a group -co-, R1 7 represents a hydrogen atom or a lower alkyl group, B 3 represents a lower alkylene group, 15 B 4 represents a lower alkylene group that may have a hydroxyl group as a substituent, 1 represents 0 or 1, R 4 and R1 5 , together with the nitrogen atom to which they bind form a heterocyclic group which is a piperidinyl or a 20 piperazinyl group that, on the heterocyclic ring, may be substituted by (28) a phenyl-substituted linear or branched alkyl group that may be substituted by an alkylenedioxy group, wherein the alkylene group is linear or branched and has 1 to 4 carbon atoms, on the phenyl ring. 25 233

2. The method according to claim, wherein the compound is selected from the group consisting of N- [6- (4- { [2- (4-piperonylpiperazin-1 -yl) - 2-oxoethyl] ethylamino} - 2 methoxyphenoxy) pyridin- 3 -yl ] - 3, 4 - dichlorobenzamide, N- [6- (4 5 { [2- (4-piperonylpiperazin-1-yl) - 2 - oxoethyl] ethylamino} phenoxy) pyridin-3-yl] -4-trif luoromethylbenzamide, N- [6- (4-{ [2 (4 -piperonylpiperazin-1- yl) - 2 - oxoethyll ethylamino} -2 f luorophenoxy) pyridin-3 -yl] -4 - trif luoromethylbenzamide, N- [6 (4 -{ [2- (4 -piperonylpiperazin-1-yl) -2-oxoethyl] methylamino} -2 10 fluorophenoxy) pyridin-3 -yl] -4 -trifluoromethylbenzamide, N- [6 (4- { [2- (4 -piperonylpiperazin-1-yl) -2-oxoethyl] methylamino} -2 methoxyphenoxy) pyridin-3 -yl] -4 -trif luoromethylbenzamide, N- [6 (4- { [2- (4-piperonylpiperazin- 1-yl) - 2 -oxoethyl] ethylamino} -2 methoxyphenoxy) pyridin-3 -yl] -4 -trif luorome thylbenzamide, N- [6 15 (4- { [2- (4-piperonylpiperazin- 1-yl) - 2-oxoethyl] ethylamino} -2 methylphenoxy) pyridin-3-yl] -3, 4-dichlorobenzamide, N- [6- (4 {[2- (4 -piperonylpiperazin-1-yl) -2-oxoethyl] methylamino} -2 methylphenoxy)pyridin-3-yl] -4-trifluoromethylbenzamide, N-{6 [4- (4-benzylpiperazine-l-carbonyl) phenoxy] pyridin-3-yl} -4 20 trifluoromethylbenzamide, N-{6-[4-(4-benzylpiperazine-1 carbonyl)phenoxy]pyridin-3-yl}-3,4-dichlorobenzamide, N- [6 ({4-[3-(4-piperonylpiperazin-1-yl)-3 oxopropyl] phenyl}methylamino) pyridin-3-yl] -4 trifluoromethylbenzamide, N- [6- (4-{ [2- (4-piperonylpiperazin-l 25 yl) -2-oxoethyl] ethylamino}-2-fluorophenoxy)pyridin-3-yl] -3,4 dichlorobenzamide, N- [6- (4-{ [2- (4-piperonylpiperazin-1-yl) -2 oxoethyl] methylamino}-2-fluorophenoxy) pyridin-3-yl] -3,4- 234 dichlorobenzamide, N- [6- (4-{ [2- (4-piperonylpiperazin-1-yl) -2 oxoethyl]methylamino}-2 -methoxyphenoxy) pyridin-3 -yl] -3,4 dichlorobenzamide, N- [6- (4- { [2- (4-piperonylpiperazin-1-yl) -2 oxoethyl]methylamino}phenoxy) pyridin-3 -yl] -3,4 5 dichlorobenzamide, N- (6-{4- [3- (4-piperonylpiperazin-1-yl) -3 oxopropyl] phenoxy} pyridin-3 -yl) -4 - trifluoromethylbenzamide, N [6- (4-{ [2- (4-benzylpiperazin-1-yl) - 2 -oxoethyl]methylamino} -2 methylphenoxy) pyridin-3-yl] -4-trifluoromethylbenzamide, N- [6 (4-{ [2- (4 -piperonylpiperazin-1-yl) -2- oxoethyl] methylamino} -2 10 methylphenoxy)pyridin-3-yl]-2-fluoro-4 trifluoromethylbenzamide, and salts thereof, as the active ingredient.

3. The method according to claim 1 or claim 2, 15 wherein the symptom or disease associated with activation of STAT3 is an autoimmune disease, diabetes, infection, central disease, cancer-associated disease or psoriasis.

4. The method according to claim 1 or claim 2, 20 wherein the symptom or disease associated with activation of STAT5 is an autoimmune disease, allergy or hyperprolactinemia.

5. Use of a compound or salt thereof as defined in claim 1 25 in the manufacture or a medicament for preventing or treating a symptom or disease associated with activation of STAT3/5. 235

6. The use according to claim 5 wherein the compound is selected from the group consisting of N- [6- (4- { [2- (4-piperonylpiperazin-1-yl) -2-oxoethyl] ethylamino)-2 5 methoxyphenoxy)pyridin-3-yl] -3,4-dichlorobenzamide, N- [6-(4 { [2- (4-piperonylpiperazin-1-yl) -2 -oxoethyl] ethylamino} phenoxy)pyridin-3-yl] -4-trifluoromethylbenzamide, N- [6- (4-{ [2 (4 -piperonylpiperazin- 1-yl) -2- oxoethyl] ethylamino} -2 fluorophenoxy) pyridin-3-yl] -4-trifluoromethylbenzamide, N- [6 10 (4-{ [2- (4-piperonylpiperazin-1-yl) -2-oxoethyl] methylamino} -2 fluorophenoxy) pyridin-3-yll -4-trifluoromethylbenzamide, N- [6 (4-{ [2- (4 -piperonylpiperazin-1-yl) -2-oxoethyl] methylamino} -2 methoxyphenoxy) pyridin-3 -yl] -4 -trif luoromethylbenzamide, N- [6 (4-{ [2- (4-piperonylpiperazin-1-yl) -2 -oxoethyll ethylamino} -2 15 methoxyphenoxy) pyridin-3 -yl] -4 -trif luoromethylbenzamide, N- [6 (4-{ [2- (4-piperonylpiperazin-1-yl) -2-oxoethyl] ethylamino}-2 methylphenoxy) pyridin- 3 -yl] -3, 4 - dichlorobenzamide, N- [6- (4 {[2- (4 -piperonylpiperazin-1-yl) -2-oxoethyl] methylamino} -2 methylphenoxy) pyridin-3-yl] -4-trifluoromethylbenzamide, N-{6 20 [4- (4-benzylpiperazine-l-carbonyl) phenoxy]pyridin-3-yl} -4 trifluoromethylbenzamide, N-{6- [4- (4-benzylpiperazine-1 carbonyl) phenoxy] pyridin-3-yl}-3 , 4 - dichlorobenzamide, N- [6 ({4-[3-(4-piperonylpiperazin-1-yl)-3 oxopropyl] phenyl}methylamino)pyridin-3-yl] -4 25 trifluoromethylbenzamide, N- [6- (4-{ [2- (4-piperonylpiperazin-l yl) -2-oxoethyl] ethylamino}-2-fluorophenoxy)pyridin-3-yl] -3,4 dichlorobenzamide, N- [6- (4-{ [2- (4-piperonylpiperazin-1-yl) -2- 236 oxoethyl Imethylamino}-2-fluorophenoxy) pyridin-3 -yl] -3,4 dichlorobenzamide, N- [6- (4-{ [2- (4-piperonylpiperazin-1-yl) -2 oxoethyl]methylamino)-2-methoxyphenoxy) pyridin-3 -yl] -3,4 dichlorobenzamide, N- [6- (4- { [2- (4-piperonylpiperazin-1-yl) -2 5 oxoethyll methylamino}phenoxy) pyridin-3 -yl] -3,4 dichlorobenzamide, N- (6-{4- [3- (4-piperonylpiperazin-1-yl) -3 oxopropyl I phenoxy} pyridin-3 -yl) -4 - trifluoromethylbenzamide, N [6- (4-{ [2- (4-benzylpiperazin-1-yl) -2-oxoethyl]methylamino}l-2 methylphenoxy)pyridin-3-yl] -4-trifluoromethylbenzamide, N- [6 10 (4- { [2- (4 -piperonylpiperazin-1-yl) - 2 - oxoethyl] methylamino} -2 methylphenoxy)pyridin-3-yl]-2-fluoro-4 trifluoromethylbenzamide, and salts thereof, as the active ingredient. 15

7. The use according to claim 5 or claim 6, wherein the symptom or disease associated with activation of STAT3 is an autoimmune disease, diabetes, infection, central disease, cancer-associated disease or psoriasis. 20

8. The use according to claim 5 or claim 6, wherein the symptom or disease associated with activation of STAT5 is an autoimmune disease, allergy or hyperprolactinemia.

9. A method according to claim 1 or a use according to claim 25 5 substantially as hereinbefore described with reference to the Examples and/or Figures