JP2004534733A5 - - Google Patents

Claims (19)

Compounds having formula (I), derivatives thereof, analogs thereof, tautomers thereof, stereoisomers thereof, polymorphs thereof, pharmaceutically acceptable salts thereof, pharmaceutically acceptable solvates thereof:

here,
R ¹ represents a hydrogen atom, halogen, hydroxy, lower alkyl, alkoxy, a substituted or unsubstituted aralkyl group, or forms a bond with the adjacent group R ² ;
R ² represents hydrogen, hydroxy, halogen, lower alkyl, alkoxy, alkanoyl, aroyl, aralkanoyl, substituted or unsubstituted aralkyl, or R ² forms a bond with R ¹ ,
R ³ is selected from a hydrogen atom or an alkyl, cycloalkyl, aryl, alkanoyl, aroyl, aralkyl, heterocyclyl, heteroaryl, heteroaralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl group And when R ³ is substituted, the substituent is halogen, hydroxy, or nitro, or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, aralkoxyalkyl, heterocyclyl. , Heteroaryl, heteroaralkyl, alkanoyl, alkanoyloxy, hydroxyalkyl, amino, acylamino, arylamino, aminoalkyl, aryloxy, a Job aryloxycarbonyl, alkylamino, alkoxyalkyl, alkylthio, thioalkyl groups, selected from a carboxylic acid or a derivative thereof, or sulfonic acid or a substituted or unsubstituted group selected from derivatives thereof, with the proviso, R ⁴ is hydrogen or lower alkyl When it represents a group, R ³ does not represent hydrogen,
R ⁴ can be hydrogen or a substituted or unsubstituted group selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, or heteroaralkyl groups,
Y is oxygen or NR ⁵ (wherein R ⁵ is hydrogen or a substituted or unsubstituted group selected from alkyl, aryl, aralkyl, hydroxyalkyl, alkanoyl, aroyl, aralkanoyl, heterocyclyl, heteroaryl, or heteroaralkyl group. Represents
R ⁴ and R ⁵ together contain a carbon atom, a nitrogen atom, and optionally contain one or more additional heteroatoms selected from oxygen, sulfur or nitrogen. Alternatively, a 6-membered ring structure may be formed,
n is an integer ranging from 1 to 4,
Ar represents a substituted or unsubstituted divalent phenylene, naphthalene, pyridyl, quinolinyl, benzofuryl, dihydrobenzofuryl, benzopyranyl, indolyl, indolinyl, azaindolyl, azaindolinyl, pyrazolyl, benzothiazolyl, or a benzoxazolyl group;
A represents the cyclic structure given below:

(Where
X represents O or S;
R ^6, when attached to a carbon atom, hydrogen, halogen, hydroxy, nitro, cyano, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaryl Aralkyl, heteroaryloxy, heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxy Sicarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, Represents a substituted or unsubstituted group selected from reeloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or a derivative thereof, or sulfonic acid or a derivative thereof, and when R ⁶ is substituted, the substituent is halogen, Hydroxy, nitro, or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, aryloxy, aralkoxy, aralkoxyalkyl, heterocyclyl, heteroaryl, heteroaralkyl, alkanoyl, alkanoyloxy, hydroxyalkyl, amino, acylamino, aryl Amino, aminoalkyl, alkoxycarbonyl, alkylamino, alkoxyalkyl, alkylthio, thioalkyl groups, carboxylic acids or their derivatives, or sulfonic acid groups Ku is selected from a derivative thereof,
R ^6, when attached to a nitrogen atom, hydrogen, hydroxy, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, aryloxy, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, Heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxy From alkyl, aralkoxyalkyl, alkylthio, thioalkyl groups, carboxylic acids or their derivatives, or sulfonic acids or their derivatives Represents a selected substituted or unsubstituted group, and the substituent when R ⁶ is substituted is selected from a halogen, hydroxy, alkanoyl, alkanoyloxy, amino group,
R ⁷ and R ⁸ may be the same or different when bonded to a carbon atom and may be hydrogen, halogen, hydroxy, cyano, nitro, formyl, or alkyl, alkoxy, aryl, aryloxy, aralkyl, Represents a substituted or unsubstituted group selected from aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxyalkyl, thioalkyl, alkylthio groups substituent when R ⁷ and R ⁸ are substituted, halogen, hydroxy, nitro or an alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, aryloxy, aralkoxy, a From substituted or unsubstituted groups selected from alkoxyalkyl, heterocyclyl, heteroaryl, heteroaralkyl, hydroxyalkyl, amino, arylamino, aminoalkyl, alkylamino, alkoxyalkyl, alkylthio, thioalkyl groups, carboxylic acids or sulfonic acids Selected
R ⁷ and R ⁸ when bonded to nitrogen may be the same or different and may be hydrogen, hydroxy, or alkyl, alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, It represents a substituted or unsubstituted group selected from heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, and arylamino groups. When R ⁷ and R ⁸ are substituted, the substituent is fluorine, chlorine Selected from such halogen, hydroxy, alkyl, alkanoyl, alkanoyloxy, or amino groups . Of the compound having the formula (I), its derivatives, its analogs, its tautomers, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates A preparation method comprising:

〔here,
R ¹ together with the adjacent group R ² forms a bond;
R ³ is selected from a hydrogen atom or an alkyl, cycloalkyl, aryl, alkanoyl, aroyl, aralkyl, heterocyclyl, heteroaryl, heteroaralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl group Substituted or unsubstituted, provided that when R ⁴ represents hydrogen or a lower alkyl group, R ³ does not represent hydrogen;
R ⁴ can be hydrogen or a substituted or unsubstituted group selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, or heteroaralkyl groups,
Y represents oxygen,
n is an integer ranging from 1 to 4,
Ar represents a substituted or unsubstituted divalent mono- or fused aromatic or heterocyclic group;
A represents the cyclic structure given below:

(Where
X represents O or S;
R ^6, when attached to a carbon atom, hydrogen, halogen, hydroxy, nitro, cyano, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaryl Aralkyl, heteroaryloxy, heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxy Sicarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, Represents a substituted or unsubstituted group selected from reeloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or a derivative thereof, or sulfonic acid or a derivative thereof;
R ^6, when attached to a nitrogen atom, hydrogen, hydroxy, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, aryloxy, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, Heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxy From alkyl, aralkoxyalkyl, alkylthio, thioalkyl groups, carboxylic acids or their derivatives, or sulfonic acids or their derivatives Represents a selected substituted or unsubstituted group,
R ⁷ and R ⁸ may be the same or different when bonded to a carbon atom and may be hydrogen, halogen, hydroxy, cyano, nitro, formyl, or alkyl, alkoxy, aryl, aryloxy, aralkyl, Represents a substituted or unsubstituted group selected from aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxyalkyl, thioalkyl, alkylthio groups ,
R ⁷ and R ⁸ when bonded to nitrogen may be the same or different and may be hydrogen, hydroxy, or alkyl, alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, A substituted or unsubstituted group selected from heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, and arylamino groups)]
The method
a) Formula (IIIa):
_{A- (CH 2) n -O-} Ar-CHO (IIIa)
(Wherein all symbols are as defined above) are represented by formula (IIIb):

Wherein R ⁹ represents (C ₁ -C ₆ ) alkyl, all other symbols are as defined above, and reacted with a compound of general formula (I) (wherein the symbol Are as defined above) or b) Formula (IIIa):
_{A- (CH 2) n · O} -Ar-CHO (IIIa)
Reacting a compound having the formula (wherein the symbols are all as defined above) with a Wittig reagent to give a compound having the formula (I) (wherein the symbols are all as defined above) Or (c) Formula (IIIc):
A-H (IIIc)
A compound having the formula (IIId): wherein A is as defined above

(Wherein R ¹ and R ² together represent a bond, all other symbols are as defined above, and L ¹ is a leaving group). Producing a compound having the general formula (I), or d) formula (IIIa):
_{A- (CH 2) n · O} -Ar-CHO (IIIa)
(Wherein all symbols are as defined above) are represented by formula (IIIe):

(Wherein R ² represents a hydrogen atom and all other symbols are as defined above) to produce a compound having the formula (I) as defined above, or e) Formula (IIIg):
^{_{A- (CH 2) n -L 1}} (IIIg)
Wherein A and n are as defined above, and L ¹ is a leaving group, a compound having the formula (IIIf):

(Wherein R ¹ and R ² together represent a bond, all other symbols are as defined above) to produce a compound having the formula (I) as defined above. Or f) Formula (IIIh):
_{A- (CH 2) n · OH} (IIIh)
Wherein A and n are as defined above, a compound having the general formula (IIIf):

(Wherein R ¹ and R ² together represent a bond, all other symbols are as defined above) to produce a compound having the formula (I) as defined above. Or g) Formula (IIIi):

A compound having the formula (IIIj): wherein Hal represents halogen and A, Ar and n are as defined above

Reacting with a compound having (wherein R ³ = R ⁴ and as defined above except for hydrogen) to produce a compound having formula (I), and (h) A method comprising converting a compound having formula (I) obtained by any of the methods to a pharmaceutically acceptable salt or pharmaceutically acceptable solvate by conventional methods. Of the compound having the formula (I), its derivatives, its analogs, its tautomers, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates A preparation method comprising:

〔here,
R ¹ represents a hydrogen atom, halogen, hydroxy, lower alkyl, alkoxy, a substituted or unsubstituted aralkyl group,
R ² represents hydrogen, hydroxy, halogen, lower alkyl, alkoxy, alkanoyl, aroyl, aralkanoyl, a substituted or unsubstituted aralkyl group,
R ³ is selected from a hydrogen atom or an alkyl, cycloalkyl, aryl, alkanoyl, aroyl, aralkyl, heterocyclyl, heteroaryl, heteroaralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl group A substituted or unsubstituted group, provided that when R ⁴ represents hydrogen or a lower alkyl group, R ³ does not represent hydrogen;
R ⁴ can be hydrogen or a substituted or unsubstituted group selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, or heteroaralkyl groups,
Y represents oxygen,
n is an integer ranging from 1 to 4,
Ar represents a substituted or unsubstituted divalent mono- or fused aromatic or heterocyclic group;
A represents the cyclic structure given below:

(Where
X represents O or S;
R ^6, when attached to a carbon atom, hydrogen, halogen, hydroxy, nitro, cyano, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaryl Aralkyl, heteroaryloxy, heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxy Sicarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, Represents a substituted or unsubstituted group selected from reeloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or a derivative thereof, or sulfonic acid or a derivative thereof;
R ^6, when attached to a nitrogen atom, hydrogen, hydroxy, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, aryloxy, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, Heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxy From alkyl, aralkoxyalkyl, alkylthio, thioalkyl groups, carboxylic acids or their derivatives, or sulfonic acids or their derivatives Represents a selected substituted or unsubstituted group,
R ⁷ and R ⁸ may be the same or different when bonded to a carbon atom and may be hydrogen, halogen, hydroxy, cyano, nitro, formyl, or alkyl, alkoxy, aryl, aryloxy, aralkyl, Represents a substituted or unsubstituted group selected from aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxyalkyl, thioalkyl, alkylthio groups ,
R ⁷ and R ⁸ when bonded to nitrogen may be the same or different and may be hydrogen, hydroxy, or alkyl, alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, A substituted or unsubstituted group selected from heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, and arylamino groups)]
The above method
a) Formula (IVa):

(This represents a compound of formula (I) wherein R ¹ and R ² together represent a bond, Y represents an oxygen atom, and all other symbols are as defined above)
To obtain a compound having the general formula (I) (wherein R ¹ and R ² each represent a hydrogen atom and all other symbols are as defined above), or b) Formula (IVb):

Wherein R ⁴ is as defined above with the exception of hydrogen, L ³ is a leaving group and all other symbols are as defined above, a compound having the general formula ( IVc):
R ³ OH (IVc)
Wherein R ³ is selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, alkanoyl, aroyl, heterocyclyl, heteroaryl, heteroaralkyl groups Represents a substituted or unsubstituted group)
To produce a compound having the formula (I) as defined above, or c) formula (IIIg):
^{_{A- (CH 2) n -L 1}} (IIIg)
(Wherein L ¹ is a leaving group and A, and n is as defined above)
A compound having the formula (IIIf):

(Wherein all symbols are as defined above)
To produce a compound having formula (I) as defined above, or d) formula (IIIh):
_{A- (CH 2) n -OH (} IIIh)
Wherein A and n are as defined above, a compound having the general formula (IIIf):

(Wherein all symbols are as defined above) to produce a compound having formula (I) as described above,
e) Formula (IVd):

(This represents a compound of formula (I) where R ³ represents a hydrogen atom and all other symbols are as defined above)
A compound having the formula (IVe):
R ³ -L ³ (IVe)
Wherein R ³ is selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, alkanoyl, aroyl, heterocyclyl, heteroaryl, heteroaralkyl groups A substituted or unsubstituted group, and L ³ is a halogen atom)
To produce a compound having formula (I) as defined above, or f) formula (IIIa):
_{A- (CH 2) n · O} -Ar-CHO (IIIa)
(Wherein all symbols are as defined above) are represented by formula (IIIe):

(Wherein R ² represents hydrogen, and all other symbols are as defined above) to obtain a compound having the formula (I) defined above after dehydration and oxidation. Or g) Formula (IIIc):
A-H (IIIc)
A compound having the formula (IIId): wherein A is as defined above

(Wherein L ¹ is a leaving group and all other symbols are as defined above) to produce a compound having the general formula (I) as defined above. Or h) Formula (IVf):

(Wherein all symbols are as defined above)
Or a compound having formula (I) as defined above, or i) formula (IVg):

(Wherein R ⁴ is as defined above except for hydrogen, and all other symbols are as defined above).
A compound having the formula (IVc):
R ³ OH (IVc)
Wherein R ³ is selected from alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, alkanoyl, aroyl, heterocyclyl, heteroaryl, heteroaralkyl groups Represents a substituted or unsubstituted group)
J) to produce a compound having the formula (I), and j) a compound having the formula (I) obtained by any of the above-mentioned methods by a conventional method. Or a method comprising converting to a pharmaceutically acceptable solvate. Of the compound having the formula (I), its derivatives, its analogs, its tautomers, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates A preparation method comprising:

〔here,
R ¹ represents a hydrogen atom, halogen, hydroxy, lower alkyl, alkoxy, a substituted or unsubstituted aralkyl group, or forms a bond with the adjacent group R ² ;
R ² represents hydrogen, hydroxy, halogen, lower alkyl, alkoxy, alkanoyl, aroyl, aralkanoyl, substituted or unsubstituted aralkyl, or R ² forms a bond with R ¹ ,
R ³ is selected from a hydrogen atom or an alkyl, cycloalkyl, aryl, alkanoyl, aroyl, aralkyl, heterocyclyl, heteroaryl, heteroaralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl group Substituted or unsubstituted groups, provided that when R ⁴ represents hydrogen, R ³ does not represent hydrogen;
Y represents oxygen,
n is an integer ranging from 1 to 4,
Ar represents a substituted or unsubstituted divalent mono- or fused aromatic or heterocyclic group;
A represents the cyclic structure given below:

(Where
X represents O or S;
R ^6, when attached to a carbon atom, hydrogen, halogen, hydroxy, nitro, cyano, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaryl Aralkyl, heteroaryloxy, heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxy Sicarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, Represents a substituted or unsubstituted group selected from reeloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or a derivative thereof, or sulfonic acid or a derivative thereof;
R ^6, when attached to a nitrogen atom, hydrogen, hydroxy, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, aryloxy, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, Heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxy From alkyl, aralkoxyalkyl, alkylthio, thioalkyl groups, carboxylic acids or their derivatives, or sulfonic acids or their derivatives Represents a selected substituted or unsubstituted group,
R ⁷ and R ⁸ may be the same or different when bonded to a carbon atom and may be hydrogen, halogen, hydroxy, cyano, nitro, formyl, or alkyl, alkoxy, aryl, aryloxy, aralkyl, Represents a substituted or unsubstituted group selected from aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxyalkyl, thioalkyl, alkylthio groups ,
R ⁷ and R ⁸ when bonded to nitrogen may be the same or different and may be hydrogen, hydroxy, or alkyl, alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, A substituted or unsubstituted group selected from heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, and arylamino groups)]
9. The method according to claim 8, wherein R ⁴ is a substituted or unsubstituted selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, heteroaralkyl groups. Wherein the other symbols are as defined above) and is hydrolyzed by conventional methods. Of the compound having the formula (I), its derivatives, its analogs, its tautomers, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates A preparation method comprising:

〔here,
R ¹ represents a hydrogen atom, halogen, hydroxy, lower alkyl, alkoxy, a substituted or unsubstituted aralkyl group, or forms a bond with the adjacent group R ² ;
R ² represents hydrogen, hydroxy, halogen, lower alkyl, alkoxy, alkanoyl, aroyl, aralkanoyl, substituted or unsubstituted aralkyl, or R ² forms a bond with R ¹ ,
R ³ is selected from a hydrogen atom or an alkyl, cycloalkyl, aryl, alkanoyl, aroyl, aralkyl, heterocyclyl, heteroaryl, heteroaralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl group Substituted or unsubstituted groups, provided that when R ⁴ represents hydrogen, R ³ does not represent hydrogen;
Y represents oxygen,
n is an integer ranging from 1 to 4,
Ar represents a substituted or unsubstituted divalent mono- or fused aromatic or heterocyclic group;
A represents the cyclic structure given below:

(Where
X represents O or S;
R ^6, when attached to a carbon atom, hydrogen, halogen, hydroxy, nitro, cyano, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaryl Aralkyl, heteroaryloxy, heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxy Sicarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, Represents a substituted or unsubstituted group selected from reeloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or a derivative thereof, or sulfonic acid or a derivative thereof;
R ^6, when attached to a nitrogen atom, hydrogen, hydroxy, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, aryloxy, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, Heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxy From alkyl, aralkoxyalkyl, alkylthio, thioalkyl groups, carboxylic acids or their derivatives, or sulfonic acids or their derivatives Represents a selected substituted or unsubstituted group,
R ⁷ and R ⁸ may be the same or different when bonded to a carbon atom and may be hydrogen, halogen, hydroxy, cyano, nitro, formyl, or alkyl, alkoxy, aryl, aryloxy, aralkyl, Represents a substituted or unsubstituted group selected from aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxyalkyl, thioalkyl, alkylthio groups ,
R ⁷ and R ⁸ when bonded to nitrogen may be the same or different and may be hydrogen, hydroxy, or alkyl, alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, A substituted or unsubstituted group selected from heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, and arylamino groups)]
10. The method according to claim 9, wherein R ⁴ is a substituted or unsubstituted selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, heteroaralkyl groups. Wherein the other symbols are as defined above) and is hydrolyzed by conventional methods. Of the compound having the formula (I), its derivatives, its analogs, its tautomers, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates A preparation method comprising:

〔here,
R ¹ represents a hydrogen atom, halogen, hydroxy, lower alkyl, alkoxy, a substituted or unsubstituted aralkyl group, or forms a bond with the adjacent group R ² ;
R ² represents hydrogen, hydroxy, halogen, lower alkyl, alkoxy, alkanoyl, aroyl, aralkanoyl, substituted or unsubstituted aralkyl, or R ² forms a bond with R ¹ ,
R ³ is selected from a hydrogen atom or an alkyl, cycloalkyl, aryl, alkanoyl, aroyl, aralkyl, heterocyclyl, heteroaryl, heteroaralkyl, alkoxyalkyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl group A substituted or unsubstituted group, provided that when R ⁴ represents hydrogen or a lower alkyl group, R ³ does not represent hydrogen;
R ⁴ can be hydrogen or a substituted or unsubstituted group selected from alkyl, cycloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, or heteroaralkyl groups,
Y represents NR ⁵ (wherein R ⁵ represents hydrogen or a substituted or unsubstituted group selected from alkyl, aryl, aralkyl, hydroxyalkyl, alkanoyl, aroyl, aralkanoyl, heterocyclyl, heteroaryl, or heteroaralkyl group. )
R ⁴ and R ⁵ together contain a carbon atom, a nitrogen atom, and optionally contain one or more additional heteroatoms selected from oxygen, sulfur or nitrogen. Alternatively, a 6-membered ring structure may be formed,
n is an integer ranging from 1 to 4,
Ar represents a substituted or unsubstituted divalent mono- or fused aromatic or heterocyclic group;
A is the cyclic structure given below:

(Where
X represents O or S;
R ^6, when attached to a carbon atom, hydrogen, halogen, hydroxy, nitro, cyano, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaryl Aralkyl, heteroaryloxy, heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, acylamino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxy Sicarbonyl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, alkylthio, thioalkyl, alkoxycarbonylamino, Represents a substituted or unsubstituted group selected from reeloxycarbonylamino, aralkoxycarbonylamino, carboxylic acid or a derivative thereof, or sulfonic acid or a derivative thereof;
R ^6, when attached to a nitrogen atom, hydrogen, hydroxy, formyl or alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aralkyl, aryloxy, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, Heteroaralkoxy, alkanoyl, aroyl, alkanoyloxy, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, alkoxyalkyl, aryloxy From alkyl, aralkoxyalkyl, alkylthio, thioalkyl groups, carboxylic acids or their derivatives, or sulfonic acids or their derivatives Represents a selected substituted or unsubstituted group,
R ⁷ and R ⁸ may be the same or different when bonded to a carbon atom and may be hydrogen, halogen, hydroxy, cyano, nitro, formyl, or alkyl, alkoxy, aryl, aryloxy, aralkyl, Represents a substituted or unsubstituted group selected from aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino, arylamino, aralkylamino, aminoalkyl, alkoxyalkyl, thioalkyl, alkylthio groups ,
R ⁷ and R ⁸ when bonded to nitrogen may be the same or different and may be hydrogen, hydroxy, or alkyl, alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, A substituted or unsubstituted group selected from the group consisting of heteroaralkyl, hydroxyalkyl, amino, monoalkylamino, dialkylamino and arylamino)
Represents))]
The method
a) Formula (I) (wherein the symbols are all as defined above, Y represents oxygen or YR ⁴ represents a halogen atom or COYR ⁴ represents a mixed anhydride group) Reacting with a suitable amine having the formula NHR ⁴ R ⁵ , wherein R ⁴ and R ⁵ are as defined above, and if desired,
b) A method comprising converting the compound having formula (I) obtained above into a pharmaceutically acceptable salt or pharmaceutically acceptable solvate by conventional methods. 2. The compound of claim 1, selected from the group consisting of:
(±) 2-ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidine- 6-yl) ethoxy] phenyl] ethyl propanoate,
(+) 2-Ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidine- 6-yl) ethoxy] phenyl] ethyl propanoate,
(−) 2-Ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidine- 6-yl) ethoxy] phenyl] ethyl propanoate,
(±) 2-ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidine- 6-yl) ethoxy] phenyl] propanoic acid or a salt thereof,
(+) 2-Ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidine- 6-yl) ethoxy] phenyl] propanoic acid or a salt thereof,
(−) 2-Ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidine- 6-yl) ethoxy] phenyl] propanoic acid or a salt thereof,
(±) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoate,
(+) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoate,
(−) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoate,
(±) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or a salt thereof,
(+) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or a salt thereof,
(−) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or a salt thereof,
(±) 2-Ethoxy-3- [4- [2- (1-methyl-7-oxo-3-propyl-5-trifluoromethyl-6,7-dihydro-1H-pyrazolo [4,3-d] Pyrimidin-6-yl) ethoxy] phenyl] ethyl propanoate,
(+) 2-Ethoxy-3- [4- [2- (1-methyl-7-oxo-3-propyl-5-trifluoromethyl-6,7-dihydro-1H-pyrazolo [4,3-d] Pyrimidin-6-yl) ethoxy] phenyl] ethyl propanoate,
(−) 2-Ethoxy-3- [4- [2- (1-methyl-7-oxo-3-propyl-5-trifluoromethyl-6,7-dihydro-1H-pyrazolo [4,3-d] Pyrimidin-6-yl) ethoxy] phenyl] ethyl propanoate,
(±) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] ethyl 2-ethoxypropanoate,
(+) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] ethyl 2-ethoxypropanoate,
(−) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] ethyl 2-ethoxypropanoate,
(±) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-ethoxypropanoic acid or a salt thereof,
(+) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-ethoxypropanoic acid or a salt thereof,
(−) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-ethoxypropanoic acid or a salt thereof,
(±) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid ethyl ester,
(+) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid ethyl ester,
(−) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid ethyl ester,
(±) 3- [4- [2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid ethyl ester,
(+) 3- [4- [2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid ethyl ester,
(−) 3- [4- [2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid ethyl ester,
(±) 3- [4- [2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(+) 3- [4- [2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(−) 3- [4- [2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(±) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid ethyl ester,
(+) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid ethyl ester,
(−) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid ethyl ester,
(±) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(+) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(−) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(±) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoate,
(+) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoate,
(−) 3- [4- [2- (3,5-dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoate,
(±) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or a salt thereof,
(+) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or a salt thereof,
(−) 3- [4- [2- (3,5-dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or a salt thereof,
(±) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(+) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(−) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(±) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid ethyl ester,
(+) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid ethyl ester,
(−) 3- [4- [2- (3,5-dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid ethyl ester,
(±) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(+) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid, or a salt thereof,
(−) 3- [4- [2- (3,5-dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid, or a salt thereof,
[2R, N (1S)]-2-ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4 3-d] pyrimidin-6-yl) ethoxy] phenyl] -N- (2-hydroxy-1-phenylethyl) propanamide, and [2S, N (1S)]-2-ethoxy-3- [4- [ 2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] phenyl] -N- (2 -Hydroxy-1-phenylethyl) propanamide.   The pharmaceutically acceptable salt is Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt. 2. The compound of claim 1 selected from. 8. The compound of claim 7 , selected from the group consisting of the following shells:
(±) 2-ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidine- 6-yl) ethoxy] phenyl] propanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(+) 2-Ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidine- 6-yl) ethoxy] phenyl] propanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(−) 2-Ethoxy-3- [4- [2- (5-ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidine- 6-yl) ethoxy] phenyl] propanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(±) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(+) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(−) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(±) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-ethoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(+) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-ethoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(−) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-ethoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(±) 3- [4- [2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(+) 3- [4- [2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(−) 3- [4- [2- (5-Ethyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(±) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(+) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(−) 3- [4- [2- (1,5-Dimethyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(±) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(+) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(−) 3- [4- [2- (3,5-dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-ethoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(±) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(+) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(−) 3- [4- [2- (5-Benzyl-1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) Ethoxy] phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, Or aluminum salt,
(±) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum salt,
(+) 3- [4- [2- (3,5-Dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl) ethoxy] Phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline salt, ammonium salt, substituted ammonium salt, or aluminum A salt, and (−) 3- [4- [2- (3,5-dipropyl-1-methyl-7-oxo-6,7-dihydro-1H-pyrazolo [4,3-d] pyrimidin-6-yl ) Ethoxy] phenyl] -2-phenoxypropanoic acid or its Li salt, Na salt, K salt, Ca salt, Mg salt, lysine salt, arginine salt, guanidine salt, diethanolamine salt, choline Salt, ammonium salt, substituted ammonium salt, or aluminum salt. Formula (I) according to claim 1:

And a pharmaceutical composition comprising a pharmaceutically acceptable carrier, diluent, excipient, or solvent. 11. A pharmaceutical composition according to claim 10 in the form of a tablet, capsule, powder, syrup, solution or suspension. Prevent hyperlipidemia, hypercholesterolemia, hyperglycemia, osteoporosis, obesity, glucose intolerance, leptin resistance, insulin resistance, or diseases where insulin resistance is a fundamental pathophysiological mechanism Or a method of treatment comprising administering a compound having formula (I) as defined in claim 1 or a pharmaceutical composition according to claims 10 and 11 to a patient in need thereof. Method. 13. The method of claim 12 , wherein the disease is type II diabetes, impaired glucose tolerance, dyslipidaemia, syndrome X related disorders (eg, hypertension, obesity, atherosclerosis). , Hyperlipidemia, coronary artery disease and other cardiovascular disorders), certain renal diseases (including glomerulonephritis, glomerulosclerosis, nephrotic syndrome, hypertensive nephrosclerosis, retinopathy, nephropathy) Disorders related to endothelial cell activation, psoriasis, polycystic ovary syndrome (PCOS) to improve cognitive function in dementia, as well as diabetic complications, osteoporosis, inflammatory bowel disease, myotonicity A method useful as an aldose reductase inhibitor for treating dystrophies, pancreatitis, arteriosclerosis, xanthomas and cancer. Hyperlipidemia, hypercholesterolemia, hyperglycemia, osteoporosis, obesity, impaired glucose tolerance, atherosclerosis, leptin resistance, insulin resistance, or insulin resistance is the basic pathophysiological mechanism An agent for preventing or treating a disease which is: an effective amount of a compound having formula (I) according to claim 1, or a compound according to claim 7 or 9 , or claims 10 and 11 . A medicament comprising administering a pharmaceutical composition as described. Said disease is type II diabetes, impaired glucose tolerance, dyslipidemia, syndrome X related disorders (eg hypertension, obesity, insulin resistance, coronary artery disease and other cardiovascular disorders), certain Kidney disease (including glomerulonephritis, glomerulosclerosis, nephrotic syndrome, hypertensive nephrosclerosis, retinopathy, nephropathy), disorders related to endothelial cell activation, psoriasis, polycystic ovary syndrome (PCOS), dementia, diabetic complications, osteoporosis, inflammatory bowel diseases, myotonic dystrophy, pancreatitis, arteriosclerosis, as xanthoma, eating disorders, or a cancer, or inflammatory agents, according to claim 14 Drugs. A compound according to claim 1, which is an agent for reducing plasma glucose, triglycerides, total cholesterol, LDL, VLDL, or free fatty acids or increasing HDL in plasma, having an effective amount of formula (I). Or a compound comprising a compound according to claim 7 or 9 , or a pharmaceutical composition according to claims 10 and 11 . Hyperlipidemia, hypercholesterolemia, hyperglycemia, osteoporosis, obesity, impaired glucose tolerance, atherosclerosis, leptin resistance, insulin resistance, or insulin resistance is the basic pathophysiological mechanism A drug for preventing or treating a disease which is a compound having the formula (I) according to claim 1, or a compound according to claim 7 or 9 , or a pharmaceutical according to claims 10 and 11. And an agent comprising an HMG CoA reductase inhibitor or fibrate or nicotinic acid or cholestyramine or colestipol or probucol. Said disease is type II diabetes, impaired glucose tolerance, dyslipidemia, syndrome X related disorders (eg hypertension, obesity, insulin resistance, coronary artery disease and other cardiovascular disorders), certain Kidney disease (including glomerulonephritis, glomerulosclerosis, nephrotic syndrome, hypertensive nephrosclerosis, retinopathy, nephropathy), disorders related to endothelial cell activation, psoriasis, polycystic ovary syndrome (PCOS), dementia, diabetic complications, osteoporosis, inflammatory bowel diseases, myotonic dystrophy, pancreatitis, arteriosclerosis, as xanthoma, eating disorders, or a cancer, or inflammatory agents, according to claim 17 Drugs. A compound for reducing plasma glucose, triglycerides, total cholesterol, LDL, VLDL, or free fatty acids or increasing HDL in plasma, comprising a compound having formula (I) according to claim 1, or claim A compound comprising the compound according to claim 7 or 9 , or the pharmaceutical composition according to claims 10 and 11 , and an HMG CoA reductase inhibitor or fibrate or nicotinic acid or cholestyramine or colestipol or probucol.