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 PDFInfo
- 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
Links
- 0 Cc1c(*)c2nc(*)n[n]2c([N+])n1 Chemical compound Cc1c(*)c2nc(*)n[n]2c([N+])n1 0.000 description 4
- SCMLXSJOWWOSME-UHFFFAOYSA-N CC(C1)=C(C=C(c2cccc(N3CCNCC3)c2)N=C2N)N2N=C1c1ccc[o]1 Chemical compound CC(C1)=C(C=C(c2cccc(N3CCNCC3)c2)N=C2N)N2N=C1c1ccc[o]1 SCMLXSJOWWOSME-UHFFFAOYSA-N 0.000 description 1
- AFVPOSGGZWXGCK-ARJAWSKDSA-N CC/C=C\CC(N)N(CC1)CCN1c(c(F)c1)ccc1F Chemical compound CC/C=C\CC(N)N(CC1)CCN1c(c(F)c1)ccc1F AFVPOSGGZWXGCK-ARJAWSKDSA-N 0.000 description 1
- KFEZLCUGHDUQIW-UHFFFAOYSA-N CCC(N(CC1)CCN1C(C)N(C)C(c1ccc[o]1)N(C)NC(N)=N)=O Chemical compound CCC(N(CC1)CCN1C(C)N(C)C(c1ccc[o]1)N(C)NC(N)=N)=O KFEZLCUGHDUQIW-UHFFFAOYSA-N 0.000 description 1
- KYQCRBDECYASKY-UHFFFAOYSA-N N#Cc1cc(CN(CC2)CCN2c(ccc(F)c2)c2F)ccc1 Chemical compound N#Cc1cc(CN(CC2)CCN2c(ccc(F)c2)c2F)ccc1 KYQCRBDECYASKY-UHFFFAOYSA-N 0.000 description 1
- PCOFIIVWHXIDGT-UHFFFAOYSA-N N#Cc1cc(CO)ccc1 Chemical compound N#Cc1cc(CO)ccc1 PCOFIIVWHXIDGT-UHFFFAOYSA-N 0.000 description 1
- WRXVOTDGLNPNND-UHFFFAOYSA-N N#Cc1cccc(CCl)c1 Chemical compound N#Cc1cccc(CCl)c1 WRXVOTDGLNPNND-UHFFFAOYSA-N 0.000 description 1
- FYGCFFIHTQDABY-UHFFFAOYSA-N Nc1nc(-c2cc(N3CCN(Cc4ccccc4)CC3)ccc2)cc2nc(-c3ccc[o]3)n[n]12 Chemical compound Nc1nc(-c2cc(N3CCN(Cc4ccccc4)CC3)ccc2)cc2nc(-c3ccc[o]3)n[n]12 FYGCFFIHTQDABY-UHFFFAOYSA-N 0.000 description 1
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)
- 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)
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)
| 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)
| 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. |
-
2002
- 2002-11-25 PE PE2002001128A patent/PE20030739A1/es not_active Application Discontinuation
- 2002-11-25 AR ARP020104528A patent/AR038366A1/es unknown
- 2002-11-25 TW TW091134178A patent/TW200300686A/zh unknown
- 2002-11-26 CA CA2468681A patent/CA2468681C/en not_active Expired - Fee Related
- 2002-11-26 HU HU0402270A patent/HUP0402270A3/hu unknown
- 2002-11-26 WO PCT/US2002/038134 patent/WO2003048164A2/en not_active Ceased
- 2002-11-26 MX MXPA04005156A patent/MXPA04005156A/es active IP Right Grant
- 2002-11-26 AU AU2002346572A patent/AU2002346572A1/en not_active Abandoned
- 2002-11-26 AT AT02784641T patent/ATE317844T1/de not_active IP Right Cessation
- 2002-11-26 EP EP02784641A patent/EP1453835B1/en not_active Expired - Lifetime
- 2002-11-26 ES ES02784641T patent/ES2258164T3/es not_active Expired - Lifetime
- 2002-11-26 KR KR1020047008031A patent/KR20050044607A/ko not_active Withdrawn
- 2002-11-26 IL IL16157202A patent/IL161572A0/xx unknown
- 2002-11-26 DE DE60209251T patent/DE60209251T2/de not_active Expired - Lifetime
- 2002-11-26 US US10/304,504 patent/US7041666B2/en not_active Expired - Lifetime
- 2002-11-26 CN CNA028239229A patent/CN1596258A/zh active Pending
- 2002-11-26 JP JP2003549354A patent/JP4284181B2/ja not_active Expired - Fee Related
-
2004
- 2004-05-27 ZA ZA200404160A patent/ZA200404160B/en unknown
-
2008
- 2008-06-04 JP JP2008147394A patent/JP2008303217A/ja active Pending
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 |
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