JP2005511699A5 - - Google Patents
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- Publication number
- JP2005511699A5 JP2005511699A5 JP2003549355A JP2003549355A JP2005511699A5 JP 2005511699 A5 JP2005511699 A5 JP 2005511699A5 JP 2003549355 A JP2003549355 A JP 2003549355A JP 2003549355 A JP2003549355 A JP 2003549355A JP 2005511699 A5 JP2005511699 A5 JP 2005511699A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- substituents
- aryl
- halogen
- alkyl
- 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.)
- Granted
Links
- -1 1 - thienyl - Chemical class 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
- 125000004442 acylamino group Chemical group 0.000 claims 2
- 125000004423 acyloxy group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000003725 azepanyl group Chemical group 0.000 claims 2
- 125000004472 dialkylaminosulfonyl group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000001462 1-pyrrolyl group Chemical group [*]N1C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000005083 alkoxyalkoxy group Chemical group 0.000 claims 1
- 125000004422 alkyl sulphonamide group Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
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 true JP2005511699A5 (https=) | 2005-12-22 |
| JP4284182B2 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 (https=) |
| EP (1) | EP1448565B1 (https=) |
| JP (2) | JP4284182B2 (https=) |
| KR (1) | KR20050044593A (https=) |
| CN (1) | CN1692116A (https=) |
| AR (1) | AR037680A1 (https=) |
| AT (1) | ATE453647T1 (https=) |
| AU (1) | AU2002346503A1 (https=) |
| CA (1) | CA2468649C (https=) |
| DE (1) | DE60234951D1 (https=) |
| ES (1) | ES2336435T3 (https=) |
| HU (1) | HUP0402018A3 (https=) |
| IL (1) | IL161716A0 (https=) |
| MX (1) | MXPA04005209A (https=) |
| PE (1) | PE20030665A1 (https=) |
| TW (1) | TW200306837A (https=) |
| WO (1) | WO2003048165A1 (https=) |
| ZA (1) | ZA200404161B (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1283839T1 (https=) * | 2000-05-26 | 2005-08-31 | Schering Corp | |
| 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 |
| IL160133A0 (en) * | 2002-05-30 | 2004-06-20 | King Pharmaceuticals Res & Dev | Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use |
| 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 |
| 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 |
| CN1898246B (zh) * | 2003-10-28 | 2010-10-27 | 先灵公司 | 制备取代的5-氨基-吡唑并[4，3-e]-1，2，4-三唑并[1，5-c]嘧啶的方法 |
| WO2005060981A2 (en) * | 2003-12-19 | 2005-07-07 | Schering Corporation | Pharmaceutical compositions |
| EP1902716A4 (en) * | 2005-06-07 | 2009-05-13 | Kyowa Hakko Kirin Co Ltd | PROPHYLACTIC AND / OR THERAPEUTIC AGENT FOR MOTOR TROUBLESHOOTING |
| 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 |
| WO2009078999A1 (en) | 2007-12-17 | 2009-06-25 | Janssen Pharmaceutica N.V. | Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of trpv1 |
| 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 |
| 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 |
| WO2010078430A1 (en) | 2008-12-30 | 2010-07-08 | Arqule, Inc. | Substituted 1h-pyrazolo[3,4-d]pyrimidine-6-amine compounds |
| TW201100427A (en) | 2009-03-31 | 2011-01-01 | 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| CN114667287A (zh) * | 2019-07-17 | 2022-06-24 | 泰昂治疗公司 | 腺苷a2a受体拮抗剂及其用途 |
| CN112592346B (zh) | 2019-07-30 | 2022-04-26 | 厦门宝太生物科技股份有限公司 | 一种a2a和/或a2b抑制剂中间体的制备方法 |
| CN111825698B (zh) | 2019-07-30 | 2021-10-15 | 杭州阿诺生物医药科技有限公司 | 腺苷受体拮抗剂 |
Family Cites Families (9)
| 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 |
| 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 |
| 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 |
| SI1283839T1 (https=) * | 2000-05-26 | 2005-08-31 | Schering Corp | |
| IL160133A0 (en) * | 2002-05-30 | 2004-06-20 | King Pharmaceuticals Res & Dev | Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use |
| CL2004000847A1 (es) * | 2003-04-23 | 2005-03-11 | Schering Corp | Compuestos derivados de 2-alquinil o 2-alquenil-5amino-pirazolo-[4,3-e]-1,2,4-triazolo[1,5-]pirimidina; composicion farmaceutica, y uso en el tratamiento de enfermedades del sistema nervioso central o un accidente cerebrovascular tal como depresion, |
-
2002
- 2002-11-26 CA CA002468649A patent/CA2468649C/en not_active Expired - Fee Related
- 2002-11-26 ES ES02784568T patent/ES2336435T3/es not_active Expired - Lifetime
- 2002-11-26 MX MXPA04005209A patent/MXPA04005209A/es active IP Right Grant
- 2002-11-26 EP EP02784568A patent/EP1448565B1/en not_active Expired - Lifetime
- 2002-11-26 DE DE60234951T patent/DE60234951D1/de not_active Expired - Lifetime
- 2002-11-26 AT AT02784568T patent/ATE453647T1/de not_active IP Right Cessation
- 2002-11-26 JP JP2003549355A patent/JP4284182B2/ja not_active Expired - Fee Related
- 2002-11-26 AU AU2002346503A patent/AU2002346503A1/en not_active Abandoned
- 2002-11-26 IL IL16171602A patent/IL161716A0/xx unknown
- 2002-11-26 KR KR1020047007876A patent/KR20050044593A/ko not_active Withdrawn
- 2002-11-26 WO PCT/US2002/037710 patent/WO2003048165A1/en not_active Ceased
- 2002-11-26 HU HU0402018A patent/HUP0402018A3/hu unknown
- 2002-11-26 CN CNA02823782XA patent/CN1692116A/zh active Pending
- 2002-11-26 US US10/304,931 patent/US6916811B2/en not_active Expired - Lifetime
- 2002-11-27 AR ARP020104561A patent/AR037680A1/es unknown
- 2002-11-27 TW TW091134471A patent/TW200306837A/zh unknown
- 2002-11-27 PE PE2002001143A patent/PE20030665A1/es not_active Application Discontinuation
-
2004
- 2004-05-27 ZA ZA200404161A patent/ZA200404161B/en unknown
-
2008
- 2008-06-04 JP JP2008147306A patent/JP2008260776A/ja active Pending
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