JP4284181B2 - 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

Info

Publication number
JP4284181B2
JP4284181B2 JP2003549354A JP2003549354A JP4284181B2 JP 4284181 B2 JP4284181 B2 JP 4284181B2 JP 2003549354 A JP2003549354 A JP 2003549354A JP 2003549354 A JP2003549354 A JP 2003549354A JP 4284181 B2 JP4284181 B2 JP 4284181B2
Authority
JP
Japan
Prior art keywords
alkyl
alkoxy
mmol
group
aryl
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
JP2003549354A
Other languages
English (en)
Japanese (ja)
Other versions
JP2005511698A5 (enExample
JP2005511698A (ja
Inventor
ジュリアス ジェイ. マタシ,
ジョン ピー. カルドウェル,
ディーン タルシアン,
リサ エス. シルバーマン,
バーナード アール. ニュースタッド,
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 JP2005511698A publication Critical patent/JP2005511698A/ja
Publication of JP2005511698A5 publication Critical patent/JP2005511698A5/ja
Application granted granted Critical
Publication of JP4284181B2 publication Critical patent/JP4284181B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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)
  • Neurosurgery (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (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)
JP2003549354A 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 JP4284181B2 (ja)

Applications Claiming Priority (2)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2008147394A Division JP2008303217A (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
JP2005511698A JP2005511698A (ja) 2005-04-28
JP2005511698A5 JP2005511698A5 (enExample) 2005-12-22
JP4284181B2 true JP4284181B2 (ja) 2009-06-24

Family

ID=23306533

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2003549354A Expired - Fee Related JP4284181B2 (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
JP2008147394A Pending JP2008303217A (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
JP2008147394A Pending JP2008303217A (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) US7041666B2 (enExample)
EP (1) EP1453835B1 (enExample)
JP (2) JP4284181B2 (enExample)
KR (1) KR20050044607A (enExample)
CN (1) CN1596258A (enExample)
AR (1) AR038366A1 (enExample)
AT (1) ATE317844T1 (enExample)
AU (1) AU2002346572A1 (enExample)
CA (1) CA2468681C (enExample)
DE (1) DE60209251T2 (enExample)
ES (1) ES2258164T3 (enExample)
HU (1) HUP0402270A3 (enExample)
IL (1) IL161572A0 (enExample)
MX (1) MXPA04005156A (enExample)
PE (1) PE20030739A1 (enExample)
TW (1) TW200300686A (enExample)
WO (1) WO2003048164A2 (enExample)
ZA (1) ZA200404160B (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004029056A1 (ja) * 2002-09-24 2004-04-08 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体
WO2005044245A1 (en) 2002-12-19 2005-05-19 Schering Corporation USES OF ADENOSINE A2a RECEPTOR ANTAGONISTS
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
EP1618109A2 (en) * 2003-04-09 2006-01-25 Biogen Idec MA Inc. 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
WO2009003003A2 (en) * 2007-06-25 2008-12-31 Neurogen Corporation Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues
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
EP2357655A4 (en) 2008-11-25 2016-09-07 Nissan Motor CONDUCTIVE ELEMENT AND SOLIDS POLYMER FUEL CELL THEREFOR
WO2010126811A1 (en) * 2009-04-27 2010-11-04 Boehringer Ingelheim International Gmbh Cxcr3 receptor antagonists
US8952004B2 (en) 2010-01-07 2015-02-10 Boehringer Ingelheim International Gmbh CXCR3 receptor antagonists
US9006177B2 (en) * 2010-09-24 2015-04-14 Advinus Therapeutics Limited Fused tricyclic compounds as adenosine receptor antagonist
WO2012127472A1 (en) * 2011-03-22 2012-09-27 Mapi Pharma Ltd. Process and intermediates for the preparation of preladenant and related compounds
PT3611174T (pt) * 2017-04-07 2022-07-07 Medshine Discovery Inc Derivado de [1,2,4]triazolo[1,5-c]pirimidina como inibidor do recetor a2a
WO2019168847A1 (en) * 2018-02-27 2019-09-06 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors
PT3766884T (pt) * 2018-04-28 2022-03-31 Medshine Discovery Inc Forma cristalina e tipo de sal de composto de triazolopirimidina e método de preparação associado
US11168089B2 (en) 2018-05-18 2021-11-09 Incyte Corporation Fused pyrimidine derivatives as A2A / A2B inhibitors
JOP20200342A1 (ar) 2018-07-05 2020-12-30 Incyte Corp مشتقات بيرازين مدمجة كمثبطات a2a/a2b
AR116315A1 (es) * 2018-09-12 2021-04-21 Dizal Jiangsu Pharmaceutical Co Ltd Compuestos de triazolo-pirimidina y usos de los mismos
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
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
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
CR20210336A (es) 2018-12-20 2021-12-06 Incyte Corp Compuestos de imidazopiridazina e imidazopiridina como inhibidores de quinasa-2 de tipo receptor de activina
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
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
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
BR9914040A (pt) * 1998-09-22 2002-01-15 Kyowa Hakko Kogyo Kk Derivados de [1,2,4]triazolo[1,5-c]pirimidina e seu uso, medicamento, antagonista, agente para prevenir ou tratar doenças, bem como processo para prevenção ou tratamento de distúrbios
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
WO2002079204A1 (en) * 2001-03-28 2002-10-10 Kyowa Hakko Kogyo Co., Ltd. 8-thiazolyl[1,2,4]triazolo[1,5-c]pyrimidine derivative
MXPA04005158A (es) 2001-11-30 2004-08-11 Schering Corp Antagonistas receptores de adenosina a2a biciclica de (1.2.4]- triazol.

Also Published As

Publication number Publication date
US20030212080A1 (en) 2003-11-13
WO2003048164A2 (en) 2003-06-12
ATE317844T1 (de) 2006-03-15
HUP0402270A3 (en) 2008-09-29
AR038366A1 (es) 2005-01-12
WO2003048164A3 (en) 2003-10-16
TW200300686A (en) 2003-06-16
KR20050044607A (ko) 2005-05-12
CN1596258A (zh) 2005-03-16
JP2005511698A (ja) 2005-04-28
PE20030739A1 (es) 2003-08-28
DE60209251D1 (de) 2006-04-20
US7041666B2 (en) 2006-05-09
EP1453835B1 (en) 2006-02-15
AU2002346572A1 (en) 2003-06-17
JP2008303217A (ja) 2008-12-18
CA2468681A1 (en) 2003-06-12
ZA200404160B (en) 2005-04-08
HUP0402270A2 (hu) 2005-02-28
EP1453835A2 (en) 2004-09-08
IL161572A0 (en) 2004-09-27
HK1064100A1 (en) 2005-01-21
MXPA04005156A (es) 2004-08-11
ES2258164T3 (es) 2006-08-16
CA2468681C (en) 2011-01-25
DE60209251T2 (de) 2006-11-09

Similar Documents

Publication Publication Date Title
JP4284181B2 (ja) アデノシンA2aレセプターアンタゴニスト
JP4938348B2 (ja) アデノシンa2aレセプターアンタゴニスト
JP4284182B2 (ja) アデノシンA2aレセプターアンタゴニスト
JP4429724B2 (ja) [1,2,4]−トリアゾール二環式アデノシンA2aレセプタアンタゴニスト
HK1064100B (en) Adenosine a 2a receptor antagonists
HK1108882B (en) Pyrazolo[1,5-a]pyrimidine adenosine a2a receptor antagonists
HK1063780B (en) Adenosine a2a receptor antagonists
HK1108882A1 (en) Pyrazolo[1,5-a]pyrimidine adenosine a2a receptor antagonists

Legal Events

Date Code Title Description
A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20071204

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20071206

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20080303

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20080310

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20080403

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20080410

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20080501

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20080512

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20080604

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20090316

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20090323

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120327

Year of fee payment: 3

LAPS Cancellation because of no payment of annual fees