CA2468649C - Adenosine a2a receptor antagonists - Google Patents

Adenosine a2a receptor antagonists Download PDF

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Publication number
CA2468649C
CA2468649C CA002468649A CA2468649A CA2468649C CA 2468649 C CA2468649 C CA 2468649C CA 002468649 A CA002468649 A CA 002468649A CA 2468649 A CA2468649 A CA 2468649A CA 2468649 C CA2468649 C CA 2468649C
Authority
CA
Canada
Prior art keywords
disease
group
alkyl
alkoxy
hydrogen
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CA002468649A
Other languages
English (en)
French (fr)
Other versions
CA2468649A1 (en
Inventor
Craig D. Boyle
Samuel Chackalamannil
William J. Greenlee
Unmesh G. Shah
Yan Xia
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of CA2468649A1 publication Critical patent/CA2468649A1/en
Application granted granted Critical
Publication of CA2468649C publication Critical patent/CA2468649C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Veterinary Medicine (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA002468649A 2001-11-30 2002-11-26 Adenosine a2a receptor antagonists Expired - Fee Related CA2468649C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US33434201P 2001-11-30 2001-11-30
US60/334,342 2001-11-30
PCT/US2002/037710 WO2003048165A1 (en) 2001-11-30 2002-11-26 ADENOSINE A2a RECEPTOR ANTAGONISTS

Publications (2)

Publication Number Publication Date
CA2468649A1 CA2468649A1 (en) 2003-06-12
CA2468649C true CA2468649C (en) 2009-03-10

Family

ID=23306779

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002468649A Expired - Fee Related CA2468649C (en) 2001-11-30 2002-11-26 Adenosine a2a receptor antagonists

Country Status (18)

Country Link
US (1) US6916811B2 (https=)
EP (1) EP1448565B1 (https=)
JP (2) JP4284182B2 (https=)
KR (1) KR20050044593A (https=)
CN (1) CN1692116A (https=)
AR (1) AR037680A1 (https=)
AT (1) ATE453647T1 (https=)
AU (1) AU2002346503A1 (https=)
CA (1) CA2468649C (https=)
DE (1) DE60234951D1 (https=)
ES (1) ES2336435T3 (https=)
HU (1) HUP0402018A3 (https=)
IL (1) IL161716A0 (https=)
MX (1) MXPA04005209A (https=)
PE (1) PE20030665A1 (https=)
TW (1) TW200306837A (https=)
WO (1) WO2003048165A1 (https=)
ZA (1) ZA200404161B (https=)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1283839T1 (https=) * 2000-05-26 2005-08-31 Schering Corp
US6964288B2 (en) * 2001-07-06 2005-11-15 Ksaria Corporation Apparatus and method for automated preparation of an optical fiber
JP4545437B2 (ja) 2001-10-15 2010-09-15 シェーリング コーポレイション アデノシンａ２ａ受容体アンタゴニストとしてのイミダゾ（４，３−ｅ）−１，２，４−トリアゾロ（１，５−ｃ）ピリミジン
IL160133A0 (en) * 2002-05-30 2004-06-20 King Pharmaceuticals Res & Dev Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use
JP2006514697A (ja) * 2002-12-19 2006-05-11 シェーリング　コーポレイション アデノシンＡ２ａレセプターアンタゴニストの使用
JP4800216B2 (ja) * 2003-10-24 2011-10-26 エグゼリクシス， インコーポレイテッド ｐ７０Ｓ６キナーゼモジュレーターおよび使用方法
CN1898246B (zh) * 2003-10-28 2010-10-27 先灵公司 制备取代的5-氨基-吡唑并[4，3-e]-1，2，4-三唑并[1，5-c]嘧啶的方法
WO2005060981A2 (en) * 2003-12-19 2005-07-07 Schering Corporation Pharmaceutical compositions
EP1902716A4 (en) * 2005-06-07 2009-05-13 Kyowa Hakko Kirin Co Ltd PROPHYLACTIC AND / OR THERAPEUTIC AGENT FOR MOTOR TROUBLESHOOTING
ES2273599B1 (es) 2005-10-14 2008-06-01 Universidad De Barcelona Compuestos para el tratamiento de la fibrilacion auricular.
PE20080145A1 (es) * 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv Tetrahidro-pirimidoazepinas como moduladores de trpv1
US7691869B2 (en) 2007-03-30 2010-04-06 King Pharmaceuticals Research And Development, Inc. Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine A2A receptor activity
WO2009078999A1 (en) 2007-12-17 2009-06-25 Janssen Pharmaceutica N.V. Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of trpv1
US12246013B2 (en) 2008-08-01 2025-03-11 Eye Therapies Llc Vasoconstriction compositions and methods of use
US20100028266A1 (en) 2008-08-01 2010-02-04 Alpha Synergy Development. Inc. Composition and methods for treating allergic response
US20100203165A1 (en) 2008-08-01 2010-08-12 Gerald Horn Compositions and methods for treatment of disorders or conditions of the eye
US8952011B2 (en) 2008-08-01 2015-02-10 Eye Therapies Llc Compositions and methods for the treatment of nasal conditions
WO2010078430A1 (en) 2008-12-30 2010-07-08 Arqule, Inc. Substituted 1h-pyrazolo[3,4-d]pyrimidine-6-amine compounds
TW201100427A (en) 2009-03-31 2011-01-01 Arqule Inc Substituted heterocyclic compounds
US8987270B2 (en) 2009-07-27 2015-03-24 Eye Therapies Llc Formulations of selective alpha-2 agonists and methods of use thereof
US20110152271A1 (en) * 2009-12-17 2011-06-23 Gerald Horn Compositions and methods for ophthalmic delivery of nasal decongestants
US8445526B2 (en) 2011-02-03 2013-05-21 Glaucoma & Nasal Therapies Llc Compositions and methods for treatment of glaucoma
US8999938B2 (en) 2013-06-21 2015-04-07 Gnt Llc Ophthalmic lipophilic drug delivery vehicle formulations
CN110742893B (zh) * 2018-07-23 2024-04-05 百济神州(北京)生物科技有限公司 A2a受体拮抗剂治疗癌症的方法
WO2020106560A1 (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
KR20210093964A (ko) 2018-11-20 2021-07-28 머크 샤프 앤드 돔 코포레이션 치환된 아미노 트리아졸로피리미딘 및 아미노 트리아졸로피라진 아데노신 수용체 길항제, 제약 조성물 및 그의 용도
TW202039496A (zh) 2018-11-30 2020-11-01 美商默沙東藥廠 做為腺苷受體拮抗劑之9-經取代胺基三唑喹唑啉衍生物、醫藥組合物及其用途
JP2022511778A (ja) 2018-11-30 2022-02-01 メルク・シャープ・アンド・ドーム・コーポレーション アデノシン受容体拮抗薬としての７－、８－及び１０－置換されたアミノトリアゾロキナゾリン誘導体、医薬組成物及びそれらの使用
DE102019116986A1 (de) 2019-06-24 2020-12-24 Helmholtz-Zentrum Dresden-Rossendorf E. V. Deuterierte 7-(3-(4-(2-([18F]Fluor)ethoxy)phenyl)propyl)-2-(furan-2-yl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amin-Derivate
CN114667287A (zh) * 2019-07-17 2022-06-24 泰昂治疗公司 腺苷a2a受体拮抗剂及其用途
CN112592346B (zh) 2019-07-30 2022-04-26 厦门宝太生物科技股份有限公司 一种a2a和/或a2b抑制剂中间体的制备方法
CN111825698B (zh) 2019-07-30 2021-10-15 杭州阿诺生物医药科技有限公司 腺苷受体拮抗剂

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1264901B1 (it) 1993-06-29 1996-10-17 Schering Plough S P A Analoghi eterociclici di 1,2,4-triazolo(15-c)pirimidine ad attivita' antagonista per il recettore a2 dell'adenosina
EP0666079B1 (en) * 1993-07-27 2001-11-07 Kyowa Hakko Kogyo Co., Ltd. Remedy for parkinson's disease
IT1277392B1 (it) * 1995-07-28 1997-11-10 Schering Plough S P A Analoghi eterociclici di 1,2,4-triazolo(1,5-c]pirimidine ad attivita' antagonista per il recettore a2a dell'adenosina
IT1291372B1 (it) 1997-05-21 1999-01-07 Schering Plough S P A Uso di analoghi eterociclici di 1,2,4-triazolo (1,5-c) pirimidine per la preparazione di medicamenti utili per il trattamento delle malattie
US6448253B1 (en) * 1998-09-16 2002-09-10 King Pharmaceuticals Research And Development, Inc. Adenosine A3 receptor modulators
US6921825B2 (en) * 1998-09-16 2005-07-26 King Pharmaceuticuals Research & Development, Inc. Adenosine A3 receptor modulators
SI1283839T1 (https=) * 2000-05-26 2005-08-31 Schering Corp
IL160133A0 (en) * 2002-05-30 2004-06-20 King Pharmaceuticals Res & Dev Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use
CL2004000847A1 (es) * 2003-04-23 2005-03-11 Schering Corp Compuestos derivados de 2-alquinil o 2-alquenil-5amino-pirazolo-[4,3-e]-1,2,4-triazolo[1,5-]pirimidina; composicion farmaceutica, y uso en el tratamiento de enfermedades del sistema nervioso central o un accidente cerebrovascular tal como depresion,

Also Published As

Publication number Publication date
MXPA04005209A (es) 2004-08-19
US6916811B2 (en) 2005-07-12
HUP0402018A2 (hu) 2005-02-28
JP4284182B2 (ja) 2009-06-24
JP2005511699A (ja) 2005-04-28
TW200306837A (en) 2003-12-01
ZA200404161B (en) 2005-11-30
CN1692116A (zh) 2005-11-02
EP1448565A1 (en) 2004-08-25
HK1063780A1 (en) 2005-01-14
DE60234951D1 (de) 2010-02-11
AU2002346503A1 (en) 2003-06-17
AR037680A1 (es) 2004-12-01
ATE453647T1 (de) 2010-01-15
EP1448565B1 (en) 2009-12-30
PE20030665A1 (es) 2003-08-08
ES2336435T3 (es) 2010-04-13
HUP0402018A3 (en) 2008-06-30
KR20050044593A (ko) 2005-05-12
JP2008260776A (ja) 2008-10-30
IL161716A0 (en) 2004-09-27
WO2003048165A1 (en) 2003-06-12
US20030212059A1 (en) 2003-11-13
CA2468649A1 (en) 2003-06-12

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Effective date: 20131126