DE60209251T2 - Adenosine a2a receptor antagonisten - Google Patents

Adenosine a2a receptor antagonisten Download PDF

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Publication number
DE60209251T2
DE60209251T2 DE60209251T DE60209251T DE60209251T2 DE 60209251 T2 DE60209251 T2 DE 60209251T2 DE 60209251 T DE60209251 T DE 60209251T DE 60209251 T DE60209251 T DE 60209251T DE 60209251 T2 DE60209251 T2 DE 60209251T2
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DE
Germany
Prior art keywords
alkyl
alkoxy
group
mmol
heteroaryl
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 - Lifetime
Application number
DE60209251T
Other languages
German (de)
English (en)
Other versions
DE60209251D1 (de
Inventor
J. Julius Monmouth Junction MATASI
P. John Ringwood CALDWELL
Deen Lebanon TULSHIAN
S. Lisa Apartment No. 1 Metuchen SILVERMAN
R. Bernard West Orange NEUSTADT
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 DE60209251D1 publication Critical patent/DE60209251D1/de
Application granted granted Critical
Publication of DE60209251T2 publication Critical patent/DE60209251T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime 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
    • C07D487/02—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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/24—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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (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)
DE60209251T 2001-11-30 2002-11-26 Adenosine a2a receptor antagonisten Expired - Lifetime DE60209251T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US33429301P 2001-11-30 2001-11-30
US334293P 2001-11-30
PCT/US2002/038134 WO2003048164A2 (en) 2001-11-30 2002-11-26 Adenosine a2a receptor antagonists

Publications (2)

Publication Number Publication Date
DE60209251D1 DE60209251D1 (de) 2006-04-20
DE60209251T2 true DE60209251T2 (de) 2006-11-09

Family

ID=23306533

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60209251T Expired - Lifetime DE60209251T2 (de) 2001-11-30 2002-11-26 Adenosine a2a receptor antagonisten

Country Status (18)

Country Link
US (1) US7041666B2 (https=)
EP (1) EP1453835B1 (https=)
JP (2) JP4284181B2 (https=)
KR (1) KR20050044607A (https=)
CN (1) CN1596258A (https=)
AR (1) AR038366A1 (https=)
AT (1) ATE317844T1 (https=)
AU (1) AU2002346572A1 (https=)
CA (1) CA2468681C (https=)
DE (1) DE60209251T2 (https=)
ES (1) ES2258164T3 (https=)
HU (1) HUP0402270A3 (https=)
IL (1) IL161572A0 (https=)
MX (1) MXPA04005156A (https=)
PE (1) PE20030739A1 (https=)
TW (1) TW200300686A (https=)
WO (1) WO2003048164A2 (https=)
ZA (1) ZA200404160B (https=)

Families Citing this family (30)

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EP1544200A1 (en) * 2002-09-24 2005-06-22 Kyowa Hakko Kogyo Co., Ltd. 1,2,4 -TRIAZOLO 1,5-c PYRIMIDINE DERIVATIVE
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
US20060106040A1 (en) 2002-12-19 2006-05-18 Michael Grzelak Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
US20070010522A1 (en) * 2003-04-09 2007-01-11 Chi Vu Triazolo[1,5-c]pyrimidines and pyrazolo[1,5-c]pyrimidines useful as a2a adenosine 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
AR050926A1 (es) * 2004-09-03 2006-12-06 Astrazeneca Ab Derivados de benzamida como inhibidores de la histonadesacetilasa(hdac)
WO2006129626A1 (ja) * 2005-05-30 2006-12-07 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]トリアゾロ[1,5-c]ピリミジン誘導体の製造法
ES2273599B1 (es) 2005-10-14 2008-06-01 Universidad De Barcelona Compuestos para el tratamiento de la fibrilacion auricular.
US8835631B2 (en) 2007-05-24 2014-09-16 Mitsubishi Tanabe Pharma Corporation Therapeutic agent for cerebral infarction
JP2010531364A (ja) * 2007-06-25 2010-09-24 ニューロジェン・コーポレーション ピペラジニルオキソアルキルテトラヒドロ−β−カルボリンおよび関連類似体
US20100093756A1 (en) * 2008-10-13 2010-04-15 Berbay J Kent HETEROARYL SUBSTITUTED THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS
US20100093764A1 (en) * 2008-10-13 2010-04-15 Devraj Chakravarty AMINES AND SULFOXIDES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS
KR101211338B1 (ko) 2008-11-25 2012-12-11 닛산 지도우샤 가부시키가이샤 도전 부재 및 이것을 사용한 고체 고분자형 연료 전지
EP2424840B1 (en) * 2009-04-27 2014-08-06 Boehringer Ingelheim International GmbH Cxcr3 receptor antagonists
US8952004B2 (en) 2010-01-07 2015-02-10 Boehringer Ingelheim International Gmbh CXCR3 receptor antagonists
CN103261202B (zh) * 2010-09-24 2016-01-20 阿迪维纳斯疗法有限公司 作为腺苷受体拮抗剂的稠合三环化合物
WO2012127472A1 (en) * 2011-03-22 2012-09-27 Mapi Pharma Ltd. Process and intermediates for the preparation of preladenant and related compounds
PL3611174T3 (pl) * 2017-04-07 2022-08-08 Medshine Discovery Inc. Pochodne [1,2,4]triazolo[1,5-c]pirymidyny jako inhibitor receptora a2a
BR122023024273A2 (pt) * 2018-02-27 2024-02-20 Incyte Corporation Compostos imidazopirimidinas e triazolopirimidinas, seus usos, método para inibir uma atividade de um receptor de adenosina e composição farmacêutica dos mesmos
CN112105617B (zh) * 2018-04-28 2022-04-05 南京明德新药研发有限公司 一种三唑并嘧啶类化合物的晶型、盐型及其制备方法
WO2019222677A1 (en) * 2018-05-18 2019-11-21 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
GEP20237548B (en) 2018-07-05 2023-10-10 Incyte Corp Fused pyrazine derivatives as a2a /a2b inhibitors
AR116315A1 (es) * 2018-09-12 2021-04-21 Dizal Jiangsu Pharmaceutical Co Ltd Compuestos de triazolo-pirimidina y usos de los mismos
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
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
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
CA3124088A1 (en) 2018-12-20 2020-06-25 Incyte Corporation Imidazopyridazine and imidazopyridine compounds as inhibitors of activin receptor-like kinase-2
WO2020128036A1 (en) * 2018-12-21 2020-06-25 Ryvu Therapeutics S.A. Modulators of the adenosine a2a receptor
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU622330B2 (en) 1989-06-23 1992-04-02 Takeda Chemical Industries Ltd. Condensed heterocyclic compounds having a nitrogen atom in the bridgehead for use as fungicides
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
JP4195729B2 (ja) * 1997-03-24 2008-12-10 協和醗酵工業株式会社 ［１，２，４］トリアゾロ［１，５−ｃ］ピリミジン誘導体
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
IL142128A0 (en) * 1998-09-22 2002-03-10 Kyowa Hakko Kogyo Kk [1,2,4] triazolo [1,5-c] pyrimidine derivatives
SI1283839T1 (https=) 2000-05-26 2005-08-31 Schering Corp
JPWO2002079204A1 (ja) * 2001-03-28 2004-07-22 協和醗酵工業株式会社 ８−チアゾリル［１，２，４］トリアゾロ［１，５−ｃ］ピリミジン誘導体
ES2283625T3 (es) 2001-11-30 2007-11-01 Schering Corporation Antagonistas del receptopr a2a de adenosina de (1,2,4)-triazol biciclicos.

Also Published As

Publication number Publication date
CA2468681C (en) 2011-01-25
AR038366A1 (es) 2005-01-12
TW200300686A (en) 2003-06-16
IL161572A0 (en) 2004-09-27
US20030212080A1 (en) 2003-11-13
ES2258164T3 (es) 2006-08-16
EP1453835B1 (en) 2006-02-15
JP4284181B2 (ja) 2009-06-24
US7041666B2 (en) 2006-05-09
KR20050044607A (ko) 2005-05-12
EP1453835A2 (en) 2004-09-08
HUP0402270A3 (en) 2008-09-29
ATE317844T1 (de) 2006-03-15
DE60209251D1 (de) 2006-04-20
JP2005511698A (ja) 2005-04-28
CA2468681A1 (en) 2003-06-12
ZA200404160B (en) 2005-04-08
WO2003048164A3 (en) 2003-10-16
JP2008303217A (ja) 2008-12-18
WO2003048164A2 (en) 2003-06-12
AU2002346572A1 (en) 2003-06-17
HUP0402270A2 (hu) 2005-02-28
PE20030739A1 (es) 2003-08-28
CN1596258A (zh) 2005-03-16
MXPA04005156A (es) 2004-08-11
HK1064100A1 (en) 2005-01-21

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