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WO2004048352A3 - 2-cyanopyrrolidines and their analogues as dpp-iv inhibitors - Google Patents

2-cyanopyrrolidines and their analogues as dpp-iv inhibitors Download PDF

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Publication number
WO2004048352A3
WO2004048352A3 PCT/JP2003/015061 JP0315061W WO2004048352A3 WO 2004048352 A3 WO2004048352 A3 WO 2004048352A3 JP 0315061 W JP0315061 W JP 0315061W WO 2004048352 A3 WO2004048352 A3 WO 2004048352A3
Authority
WO
WIPO (PCT)
Prior art keywords
dpp
cyanopyrrolidines
analogues
inhibitors
formula
Prior art date
Application number
PCT/JP2003/015061
Other languages
French (fr)
Other versions
WO2004048352A2 (en
Inventor
Ichiro Shima
Toshio Kurosaki
Original Assignee
Fujisawa Pharmaceutical Co
Ichiro Shima
Toshio Kurosaki
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Fujisawa Pharmaceutical Co, Ichiro Shima, Toshio Kurosaki filed Critical Fujisawa Pharmaceutical Co
Priority to AU2003283832A priority Critical patent/AU2003283832A1/en
Publication of WO2004048352A2 publication Critical patent/WO2004048352A2/en
Publication of WO2004048352A3 publication Critical patent/WO2004048352A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

A compound of the formula (I) or a pharmaceutically acceptable s alt thereof: [wherein X is CH2, O or S, R1 is the moiety represented by the formula (II), etc.: [wherein R3 is lower alkyl, etc., m is integer of 1 to 3], R2 is hydrogen, etc.]. Compouund of formula (I) inhibits DPP-IV activity. They are therefore useful in the treatment of conditions mediated by DPP-IV, such as NIDDM.
PCT/JP2003/015061 2002-11-27 2003-11-26 2-cyanopyrrolidines and their analogues as dpp-iv inhibitors WO2004048352A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003283832A AU2003283832A1 (en) 2002-11-27 2003-11-26 2-cyanopyrrolidines and their analogues as dpp-iv inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
AU2002952946A AU2002952946A0 (en) 2002-11-27 2002-11-27 Dpp-iv inhibitor
AU2002-952946 2002-11-27

Publications (2)

Publication Number Publication Date
WO2004048352A2 WO2004048352A2 (en) 2004-06-10
WO2004048352A3 true WO2004048352A3 (en) 2004-07-08

Family

ID=29741559

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2003/015061 WO2004048352A2 (en) 2002-11-27 2003-11-26 2-cyanopyrrolidines and their analogues as dpp-iv inhibitors

Country Status (2)

Country Link
AU (1) AU2002952946A0 (en)
WO (1) WO2004048352A2 (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7842707B2 (en) 2004-07-23 2010-11-30 Nuada, Llc Peptidase inhibitors
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007035629A2 (en) 2005-09-16 2007-03-29 Takeda Pharmaceutical Company Limited Process for the preparation of pyrimidinedione derivatives
GB0526291D0 (en) 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EA200802054A1 (en) 2006-04-12 2009-04-28 Пробиодруг Аг ENZYME INHIBITORS
JP5379692B2 (en) 2006-11-09 2013-12-25 プロビオドルグ エージー 3-Hydroxy-1,5-dihydro-pyrrol-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcers, cancer and other diseases
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
JP5523107B2 (en) 2006-11-30 2014-06-18 プロビオドルグ エージー Novel inhibitors of glutaminyl cyclase
DK2142514T3 (en) 2007-04-18 2015-03-23 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
KR20190016601A (en) * 2008-08-06 2019-02-18 베링거 인겔하임 인터내셔날 게엠베하 Treatment for diabetes in patients inappropriate for metformin therapy
EA022007B1 (en) 2009-09-11 2015-10-30 Пробиодруг Аг Heterocylcic derivatives as inhibitors of glutaminyl cyclase
JP6026284B2 (en) 2010-03-03 2016-11-16 プロビオドルグ エージー Inhibitors of glutaminyl cyclase
US8269019B2 (en) 2010-03-10 2012-09-18 Probiodrug Ag Inhibitors
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
ES2570167T3 (en) 2011-03-16 2016-05-17 Probiodrug Ag Benzimidazole derivatives as glutaminyl cyclase inhibitors
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
JP6307989B2 (en) * 2014-04-02 2018-04-11 住友化学株式会社 Salt, acid generator, resist composition, and method for producing resist pattern
ES2812698T3 (en) 2017-09-29 2021-03-18 Probiodrug Ag Glutaminyl cyclase inhibitors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0419683A1 (en) * 1989-04-13 1991-04-03 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
WO2001096295A2 (en) * 2000-06-13 2001-12-20 Novartis Ag 2-cyanopyrrolidine derivatives and their use as medicaments
WO2002076450A1 (en) * 2001-03-27 2002-10-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2002083109A1 (en) * 2001-04-11 2002-10-24 Ferring Bv Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase iv

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0419683A1 (en) * 1989-04-13 1991-04-03 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
WO2001096295A2 (en) * 2000-06-13 2001-12-20 Novartis Ag 2-cyanopyrrolidine derivatives and their use as medicaments
WO2002076450A1 (en) * 2001-03-27 2002-10-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2002083109A1 (en) * 2001-04-11 2002-10-24 Ferring Bv Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase iv

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
NOVARTIS A G: "NOVEL N-SUBSTITUTED-2-CYANOPYRROLIDINES AS POTENT INHIBITORS OF DIPEPTIDYL PEPTIDASE IV IN THE TREATMENT OF NON-INSULIN-DEPENDENT DIABETES MELLITUS", EXPERT OPINION ON THERAPEUTIC PATENTS, ASHLEY PUBLICATIONS, GB, vol. 10, no. 12, December 2000 (2000-12-01), pages 1937 - 1942, XP001019155, ISSN: 1354-3776 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7842707B2 (en) 2004-07-23 2010-11-30 Nuada, Llc Peptidase inhibitors
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors

Also Published As

Publication number Publication date
WO2004048352A2 (en) 2004-06-10
AU2002952946A0 (en) 2002-12-12

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