WO2003068776A1 - [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES - Google Patents

[1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES Download PDF

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Publication number
WO2003068776A1
WO2003068776A1 PCT/JP2003/001565 JP0301565W WO03068776A1 WO 2003068776 A1 WO2003068776 A1 WO 2003068776A1 JP 0301565 W JP0301565 W JP 0301565W WO 03068776 A1 WO03068776 A1 WO 03068776A1
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WIPO (PCT)
Prior art keywords
optionally substituted
triazolo
pyrimidine derivatives
adenosine
receptor
Prior art date
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PCT/JP2003/001565
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French (fr)
Japanese (ja)
Inventor
Hironori Imma
Tomokazu Watanabe
Shizuo Shiozaki
Tomoyuki Kanda
Yoshihisa Kuwana
Junichi Shimada
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Kyowa Hakko Kogyo Co., Ltd.
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Publication date
Application filed by Kyowa Hakko Kogyo Co., Ltd. filed Critical Kyowa Hakko Kogyo Co., Ltd.
Priority to AU2003211993A priority Critical patent/AU2003211993A1/en
Priority to JP2003567903A priority patent/JPWO2003068776A1/en
Publication of WO2003068776A1 publication Critical patent/WO2003068776A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Emergency Medicine (AREA)
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  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

[1,2,4]Triazolo[1,5-c]pyrimidine derivatives represented by the following general formula (I) or pharmacologically acceptable salts thereof which show an adenosine A2A receptor antagonism and are useful in treating and/or preventing various diseases caused by the hyperfunction of the adenosine A2A receptor: (I) wherein R1 represents optionally substituted aryl or optionally substituted heteroaryl; R2 represents hydrogen, halogeno, optionally substituted lower alkyl, optionally substituted aryl or optionally substituted heteroaryl; and R3 represents a group of any of the following formulae (A), (B) and (C).
PCT/JP2003/001565 2002-02-15 2003-02-14 [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES WO2003068776A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2003211993A AU2003211993A1 (en) 2002-02-15 2003-02-14 (1,2,4)TRIAZOLO(1,5-c)PYRIMIDINE DERIVATIVES
JP2003567903A JPWO2003068776A1 (en) 2002-02-15 2003-02-14 [1,2,4] Triazolo [1,5-c] pyrimidine derivatives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2002-37819 2002-02-15
JP2002037819 2002-02-15

Publications (1)

Publication Number Publication Date
WO2003068776A1 true WO2003068776A1 (en) 2003-08-21

Family

ID=27678133

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2003/001565 WO2003068776A1 (en) 2002-02-15 2003-02-14 [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES

Country Status (3)

Country Link
JP (1) JPWO2003068776A1 (en)
AU (1) AU2003211993A1 (en)
WO (1) WO2003068776A1 (en)

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004029056A1 (en) * 2002-09-24 2004-04-08 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]-TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVE
WO2004092173A3 (en) * 2003-04-09 2004-12-09 Biogen Idec Inc A2a adenosine receptor antagonists
US7285550B2 (en) 2003-04-09 2007-10-23 Biogen Idec Ma Inc. Triazolotriazines and pyrazolotriazines and methods of making and using the same
US7517874B2 (en) 2007-06-21 2009-04-14 Cara Therapeutics, Inc. Substituted imidazo[1,5-a][1,4]diazepines and imidazo[1,5-a]pyrazines as cannabinoid receptor agonists for the treatment of pain
US7674791B2 (en) 2003-04-09 2010-03-09 Biogen Idec Ma Inc. Triazolopyrazines and methods of making and using the same
US8071766B2 (en) 2008-02-01 2011-12-06 Takeda Pharmaceutical Company Limited HSP90 inhibitors
US8859538B2 (en) 2007-06-21 2014-10-14 Cara Therapeutics, Inc. Uses of substituted imidazoheterocycles
CN107922437A (en) * 2015-09-09 2018-04-17 豪夫迈·罗氏有限公司 Bridging piperidine derivative
WO2018166493A1 (en) * 2017-03-16 2018-09-20 江苏恒瑞医药股份有限公司 Heteroaryl[4,3-c]pyrimidine-5-amine derivative, preparation method therefor, and medical uses thereof
WO2020106558A1 (en) 2018-11-20 2020-05-28 Merck Sharp & Dohme Corp. Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
US11161850B2 (en) 2018-07-05 2021-11-02 Incyte Corporation Fused pyrazine derivatives as A2A / A2B inhibitors
US11168089B2 (en) 2018-05-18 2021-11-09 Incyte Corporation Fused pyrimidine derivatives as A2A / A2B inhibitors
US11390624B2 (en) 2019-01-29 2022-07-19 Incyte Corporation Pyrazolopyridines and triazolopyridines as A2A / A2B inhibitors
WO2022224180A1 (en) * 2021-04-23 2022-10-27 Chong Kun Dang Pharmaceutical Corp. Compound as adenosine a2a receptor antagonist and pharmaceutical composition comprising same
US11673894B2 (en) 2018-02-27 2023-06-13 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors
RU2802866C2 (en) * 2018-09-12 2023-09-05 Дизал (Цзянсу) Фармасьютикал Ко., Лтд. Triazolo-pyrimidine compounds and their use

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998042711A1 (en) * 1997-03-24 1998-10-01 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES
WO2000017201A1 (en) * 1998-09-22 2000-03-30 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998042711A1 (en) * 1997-03-24 1998-10-01 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES
WO2000017201A1 (en) * 1998-09-22 2000-03-30 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES

Cited By (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004029056A1 (en) * 2002-09-24 2004-04-08 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]-TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVE
WO2004092173A3 (en) * 2003-04-09 2004-12-09 Biogen Idec Inc A2a adenosine receptor antagonists
US7285550B2 (en) 2003-04-09 2007-10-23 Biogen Idec Ma Inc. Triazolotriazines and pyrazolotriazines and methods of making and using the same
US7674791B2 (en) 2003-04-09 2010-03-09 Biogen Idec Ma Inc. Triazolopyrazines and methods of making and using the same
US7834014B2 (en) 2003-04-09 2010-11-16 Biogen Idec Ma Inc. A2a adenosine receptor antagonists
US7517874B2 (en) 2007-06-21 2009-04-14 Cara Therapeutics, Inc. Substituted imidazo[1,5-a][1,4]diazepines and imidazo[1,5-a]pyrazines as cannabinoid receptor agonists for the treatment of pain
US8431565B2 (en) 2007-06-21 2013-04-30 Cara Therapeutics, Inc. Substituted imidazoheterocycles
US8859538B2 (en) 2007-06-21 2014-10-14 Cara Therapeutics, Inc. Uses of substituted imidazoheterocycles
US8071766B2 (en) 2008-02-01 2011-12-06 Takeda Pharmaceutical Company Limited HSP90 inhibitors
US8618290B2 (en) 2008-02-01 2013-12-31 Takeda Pharmaceutical Company Limited HSP90 inhibitors
CN107922437A (en) * 2015-09-09 2018-04-17 豪夫迈·罗氏有限公司 Bridging piperidine derivative
JP7111733B2 (en) 2017-03-16 2022-08-02 江蘇恒瑞医薬股▲ふん▼有限公司 Heteroaryl[4,3-c]pyrimidin-5-amine derivatives, methods for their preparation, and pharmaceutical uses thereof
TWI772386B (en) * 2017-03-16 2022-08-01 大陸商江蘇恆瑞醫藥股份有限公司 Heteroaryl fused [4,3-c]pyrimidin-5-amine derivative, a preparation method therefor, and a pharmaceutical use thereof
WO2018166493A1 (en) * 2017-03-16 2018-09-20 江苏恒瑞医药股份有限公司 Heteroaryl[4,3-c]pyrimidine-5-amine derivative, preparation method therefor, and medical uses thereof
JP2020510012A (en) * 2017-03-16 2020-04-02 江蘇恒瑞医薬股▲ふん▼有限公司 Heteroaryl [4,3-c] pyrimidin-5-amine derivatives, methods for their preparation and use of their medicaments
US11312705B2 (en) 2017-03-16 2022-04-26 Jiangsu Hengrui Medicine Co., Ltd. Heteroaryl[4,3-C]pyrimidine-5-amine derivative, preparation method therefor, and medical uses thereof
RU2764655C2 (en) * 2017-03-16 2022-01-19 Цзянсу Хэнжуй Медицин Ко., Лтд. HETEROARYL[4,3-c]PYRIMIDINE-5-AMINE DERIVATIVE, ITS PREPARATION METHOD AND ITS MEDICAL APPLICATIONS
US11673894B2 (en) 2018-02-27 2023-06-13 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors
US11168089B2 (en) 2018-05-18 2021-11-09 Incyte Corporation Fused pyrimidine derivatives as A2A / A2B inhibitors
US11873304B2 (en) 2018-05-18 2024-01-16 Incyte Corporation Fused pyrimidine derivatives as A2A/A2B inhibitors
US11161850B2 (en) 2018-07-05 2021-11-02 Incyte Corporation Fused pyrazine derivatives as A2A / A2B inhibitors
RU2802866C2 (en) * 2018-09-12 2023-09-05 Дизал (Цзянсу) Фармасьютикал Ко., Лтд. Triazolo-pyrimidine compounds and their use
RU2802866C9 (en) * 2018-09-12 2023-10-16 Дизал (Цзянсу) Фармасьютикал Ко., Лтд. Triazolo-pyrimidine compounds and their use
EP3883575A4 (en) * 2018-11-20 2022-06-15 Merck Sharp & Dohme Corp. Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
WO2020106558A1 (en) 2018-11-20 2020-05-28 Merck Sharp & Dohme Corp. Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
US11390624B2 (en) 2019-01-29 2022-07-19 Incyte Corporation Pyrazolopyridines and triazolopyridines as A2A / A2B inhibitors
US11884665B2 (en) 2019-01-29 2024-01-30 Incyte Corporation Pyrazolopyridines and triazolopyridines as A2A / A2B inhibitors
WO2022224180A1 (en) * 2021-04-23 2022-10-27 Chong Kun Dang Pharmaceutical Corp. Compound as adenosine a2a receptor antagonist and pharmaceutical composition comprising same
US11999740B2 (en) 2021-10-13 2024-06-04 Incyte Corporation Fused pyrazine derivatives as A2A / A2B inhibitors

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AU2003211993A1 (en) 2003-09-04

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