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

Families Citing this family (32)

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JP4574112B2 (ja) * 2000-05-26 2010-11-04 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
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
US7064204B2 (en) * 2002-05-30 2006-06-20 King Pharmacueticals Reserch And Development, Inc. Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use
WO2005044245A1 (en) * 2002-12-19 2005-05-19 Schering Corporation USES OF ADENOSINE A2a RECEPTOR ANTAGONISTS
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
WO2005044819A1 (en) * 2003-10-28 2005-05-19 Schering Corporation Process for preparing substituted 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines
ATE516011T1 (de) * 2003-12-19 2011-07-15 Schering Corp Pharmazeutische zusammensetzungen eines a2a rezeptorantagonisten
EP2258372B8 (en) * 2005-06-07 2012-12-19 Kyowa Hakko Kirin Co., Ltd. A2A antagonists for use in the treatment of motor disorders
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
US7723343B2 (en) 2007-03-30 2010-05-25 King Pharmaceuticals Research And Development, Inc. Adenosine A2A receptor antagonists
WO2009078999A1 (en) 2007-12-17 2009-06-25 Janssen Pharmaceutica N.V. Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of trpv1
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
HRP20141047T1 (hr) 2008-08-01 2015-01-02 Eye Therapies Llc Pripravci za sužavanje krvnih žila i metode njihove uporabe
US12246013B2 (en) 2008-08-01 2025-03-11 Eye Therapies Llc Vasoconstriction compositions and methods of use
EP2379556A1 (en) 2008-12-30 2011-10-26 ArQule, Inc. Substituted 1h-pyrazolo[3,4-d]pyrimidine-6-amine compounds
WO2010114894A1 (en) 2009-03-31 2010-10-07 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
CN113015530A (zh) 2018-11-20 2021-06-22 默沙东公司 取代的氨基三唑并嘧啶和氨基三唑并吡嗪腺苷受体拮抗剂、药物组合物及其用途
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
KR20210097152A (ko) 2018-11-30 2021-08-06 머크 샤프 앤드 돔 코포레이션 아데노신 수용체 길항제로서의 7-, 8- 및 10-치환된 아미노 트리아졸로 퀴나졸린 유도체, 제약 조성물 및 그의 용도
JOP20210117A1 (ar) 2018-11-30 2023-01-30 Merck Sharp & Dohme مشتقات أمينو ترايازولو كوينازولين بها استبدال في الموضع-9 كمضادات مستقبل أدينوزين، تركيبات صيدلانية واستخدامها
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
EP3999513A4 (en) * 2019-07-17 2022-12-21 Teon Therapeutics, Inc. ADENOSIN A2A RECEPTOR ANTAGONISTS AND USES THEREOF
CN112625050B (zh) 2019-07-30 2021-10-01 杭州阿诺生物医药科技有限公司 一种a2a和/或a2b受体抑制剂的制备方法
CN112608316B (zh) 2019-07-30 2022-10-21 厦门宝太生物科技股份有限公司 一种吡唑并三嗪类腺苷受体拮抗剂

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
AU7237294A (en) * 1993-07-27 1995-02-28 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
JP4574112B2 (ja) 2000-05-26 2010-11-04 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
US7064204B2 (en) * 2002-05-30 2006-06-20 King Pharmacueticals Reserch And Development, Inc. Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use
MXPA05011366A (es) * 2003-04-23 2005-11-28 Schering Corp Antagonistas del receptor a2a de 2-alquinil- y 2-alquenil-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidina adenosina.

Also Published As

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

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Effective date: 20131126