JP4284182B2 - アデノシンＡ２ａレセプターアンタゴニスト - Google Patents

アデノシンＡ２ａレセプターアンタゴニスト Download PDF

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Publication number
JP4284182B2
JP4284182B2 JP2003549355A JP2003549355A JP4284182B2 JP 4284182 B2 JP4284182 B2 JP 4284182B2 JP 2003549355 A JP2003549355 A JP 2003549355A JP 2003549355 A JP2003549355 A JP 2003549355A JP 4284182 B2 JP4284182 B2 JP 4284182B2
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JP
Japan
Prior art keywords
group
alkyl
compound
alkoxy
compounds
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
JP2003549355A
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English (en)
Japanese (ja)
Other versions
JP2005511699A (ja
JP2005511699A5 (enExample
Inventor
クレイグ ディー． ボイル，
サミュエル チャカラマニル，
ウィリアム ジェイ． グリーンリー，
ウンメッシュ ジー． シャー，
ヤン シャー，
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 & Dohme LLC
Original Assignee
Schering Corp
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Publication date
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Publication of JP2005511699A publication Critical patent/JP2005511699A/ja
Publication of JP2005511699A5 publication Critical patent/JP2005511699A5/ja
Application granted granted Critical
Publication of JP4284182B2 publication Critical patent/JP4284182B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (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)
JP2003549355A 2001-11-30 2002-11-26 アデノシンＡ２ａレセプターアンタゴニスト Expired - Fee Related JP4284182B2 (ja)

Applications Claiming Priority (2)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2008147306A Division JP2008260776A (ja) 2001-11-30 2008-06-04 アデノシンＡ２ａレセプターアンタゴニスト

Publications (3)

Publication Number Publication Date
JP2005511699A JP2005511699A (ja) 2005-04-28
JP2005511699A5 JP2005511699A5 (enExample) 2005-12-22
JP4284182B2 true JP4284182B2 (ja) 2009-06-24

Family

ID=23306779

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2003549355A Expired - Fee Related JP4284182B2 (ja) 2001-11-30 2002-11-26 アデノシンＡ２ａレセプターアンタゴニスト
JP2008147306A Pending JP2008260776A (ja) 2001-11-30 2008-06-04 アデノシンＡ２ａレセプターアンタゴニスト

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2008147306A Pending JP2008260776A (ja) 2001-11-30 2008-06-04 アデノシンＡ２ａレセプターアンタゴニスト

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1283839E (pt) * 2000-05-26 2005-08-31 Schering Corp Antagonistas do receptor a2a da adenosina
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
MXPA04000908A (es) * 2002-05-30 2004-03-26 King Pharmaceuticals Res & Dev Compuestos farmaceuticamente activos que tienen estructura de anillo de pirazolotriazolopirimidina triciclica y metodos de uso.
MXPA05006790A (es) 2002-12-19 2005-09-08 Schering Corp Usos de antagonistas del receptor adenosina a2a.
US7816353B2 (en) * 2003-10-24 2010-10-19 Exelixis, Inc. P70S6 kinase modulators and method of use
DK1678182T3 (da) * 2003-10-28 2007-06-04 Schering Corp Fremgangsmåde til fremstilling af substituerede 5-amino-pyrazolo[4,3-E]-1,2,4-triazolo-[1,5-C]pyrimidiner
CA2550071A1 (en) * 2003-12-19 2005-07-07 Schering Corporation Pharmaceutical compositions
JPWO2006132275A1 (ja) * 2005-06-07 2009-01-08 協和醗酵工業株式会社 運動障害の予防および／または治療剤
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
JP5562865B2 (ja) 2007-12-17 2014-07-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｔｒｐｖ１のイミダゾロ−、オキサゾロ−、及びチアゾロピリミジン・モジュレーター
US20100203165A1 (en) 2008-08-01 2010-08-12 Gerald Horn Compositions and methods for treatment of disorders or conditions of the eye
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
US8952011B2 (en) 2008-08-01 2015-02-10 Eye Therapies Llc Compositions and methods for the treatment of nasal conditions
TW201036614A (en) 2008-12-30 2010-10-16 Arqule Inc Substituted 1H-pyrazolo[3,4-d]pyrimidine-6-amine compounds
EP2414361A1 (en) 2009-03-31 2012-02-08 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
CA2782872A1 (en) * 2009-12-17 2011-06-23 Alpha Synergy Development, Inc. 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
US12414952B2 (en) 2018-11-20 2025-09-16 Merck Sharp & Dohme Llc Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
JP2022507734A (ja) 2018-11-20 2022-01-18 メルク・シャープ・アンド・ドーム・コーポレーション 置換アミノトリアゾロピリミジン及びアミノトリアゾロピラジンアデノシン受容体アンタゴニスト、医薬組成物及びそれらの使用
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
AR117164A1 (es) 2018-11-30 2021-07-14 Merck Sharp & Dohme Derivados de amino-triazoloquinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmacéuticas y su uso para el tratamiento de diversos tipos de cáncer
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
WO2021011670A1 (en) * 2019-07-17 2021-01-21 Teon Therapeutics, Inc. Adenosine a2a receptor antagonists and uses thereof
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
CN112592354B (zh) 2019-07-30 2022-05-27 厦门宝太生物科技股份有限公司 一种异噁唑并嘧啶类杂环化合物的制备方法

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
US5565460A (en) * 1993-07-27 1996-10-15 Kyowa Hakko Koygo Co., Ltd. Therapeutic purine agents 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
US6921825B2 (en) * 1998-09-16 2005-07-26 King Pharmaceuticuals Research & Development, Inc. Adenosine A3 receptor modulators
US6448253B1 (en) * 1998-09-16 2002-09-10 King Pharmaceuticals Research And Development, Inc. Adenosine A3 receptor modulators
PT1283839E (pt) * 2000-05-26 2005-08-31 Schering Corp Antagonistas do receptor a2a da adenosina
MXPA04000908A (es) * 2002-05-30 2004-03-26 King Pharmaceuticals Res & Dev Compuestos farmaceuticamente activos que tienen estructura de anillo de pirazolotriazolopirimidina triciclica y metodos de uso.
EP1622912B1 (en) * 2003-04-23 2009-05-27 Schering Corporation 2-alkynyl-and 2-alkenyl-pyrazolo- [4,3-e ] -1,2,4-triazolo- [1,5-c] -pyrimidine adenosine a2a receptor antagonists

Also Published As

Publication number Publication date
EP1448565B1 (en) 2009-12-30
HK1063780A1 (en) 2005-01-14
ATE453647T1 (de) 2010-01-15
HUP0402018A3 (en) 2008-06-30
AR037680A1 (es) 2004-12-01
JP2008260776A (ja) 2008-10-30
DE60234951D1 (de) 2010-02-11
US6916811B2 (en) 2005-07-12
WO2003048165A1 (en) 2003-06-12
CA2468649A1 (en) 2003-06-12
HUP0402018A2 (hu) 2005-02-28
CN1692116A (zh) 2005-11-02
ES2336435T3 (es) 2010-04-13
ZA200404161B (en) 2005-11-30
TW200306837A (en) 2003-12-01
PE20030665A1 (es) 2003-08-08
US20030212059A1 (en) 2003-11-13
EP1448565A1 (en) 2004-08-25
KR20050044593A (ko) 2005-05-12
JP2005511699A (ja) 2005-04-28
IL161716A0 (en) 2004-09-27
CA2468649C (en) 2009-03-10
MXPA04005209A (es) 2004-08-19
AU2002346503A1 (en) 2003-06-17

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