JP2016504363A5 - - Google Patents
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- Publication number
- JP2016504363A5 JP2016504363A5 JP2015550682A JP2015550682A JP2016504363A5 JP 2016504363 A5 JP2016504363 A5 JP 2016504363A5 JP 2015550682 A JP2015550682 A JP 2015550682A JP 2015550682 A JP2015550682 A JP 2015550682A JP 2016504363 A5 JP2016504363 A5 JP 2016504363A5
- Authority
- JP
- Japan
- Prior art keywords
- triazolo
- amine
- methoxy
- quinazoline
- ethyl
- 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
- 0 *(*1)**2C1CNCC2 Chemical compound *(*1)**2C1CNCC2 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2012/087865 WO2014101120A1 (en) | 2012-12-28 | 2012-12-28 | Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties |
| CNPCT/CN2012/087865 | 2012-12-28 | ||
| CNPCT/CN2013/076853 | 2013-06-06 | ||
| PCT/CN2013/076853 WO2014101373A1 (en) | 2012-12-28 | 2013-06-06 | Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds for treatment of central nervous system disorder |
| PCT/US2013/076781 WO2014105666A1 (en) | 2012-12-28 | 2013-12-20 | Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016504363A JP2016504363A (ja) | 2016-02-12 |
| JP2016504363A5 true JP2016504363A5 (enExample) | 2017-01-12 |
| JP6306049B2 JP6306049B2 (ja) | 2018-04-04 |
Family
ID=51019745
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015550682A Expired - Fee Related JP6306049B2 (ja) | 2012-12-28 | 2013-12-20 | Ａ２ａアンタゴニスト特性を有するヘテロビシクロ−置換−［１，２，４］トリアゾロ［１，５−ｃ］キナゾリン−５−アミン化合物 |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US9708347B2 (enExample) |
| EP (1) | EP2945632B1 (enExample) |
| JP (1) | JP6306049B2 (enExample) |
| KR (1) | KR102165113B1 (enExample) |
| AU (1) | AU2013370977B2 (enExample) |
| BR (1) | BR112015015468B8 (enExample) |
| CA (1) | CA2896056C (enExample) |
| CY (1) | CY1120258T1 (enExample) |
| DK (1) | DK2945632T3 (enExample) |
| ES (1) | ES2667477T3 (enExample) |
| HR (1) | HRP20180678T1 (enExample) |
| HU (1) | HUE037950T2 (enExample) |
| LT (1) | LT2945632T (enExample) |
| ME (1) | ME03034B (enExample) |
| MX (1) | MX370017B (enExample) |
| NO (1) | NO2945632T3 (enExample) |
| PL (1) | PL2945632T3 (enExample) |
| PT (1) | PT2945632T (enExample) |
| RS (1) | RS57162B1 (enExample) |
| RU (2) | RU2018136104A (enExample) |
| SI (1) | SI2945632T1 (enExample) |
| WO (3) | WO2014101120A1 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10138212B2 (en) | 2015-02-06 | 2018-11-27 | Merck Sharp & Dohme Corp. | Aminoquinazoline compounds as A2A antagonist |
| EP3307067B1 (en) * | 2015-06-11 | 2022-11-02 | Merck Sharp & Dohme LLC | Aminopyrazine compounds with a2a antagonist properties |
| WO2017008205A1 (en) | 2015-07-10 | 2017-01-19 | Merck Sharp & Dohme Corp. | Substituted aminoquinazoline compounds as a2a antagonist |
| WO2017034990A1 (en) | 2015-08-21 | 2017-03-02 | Portola Pharmaceuticals, Inc. | Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate pcsk9 protein activity |
| EP3337497B1 (en) | 2015-08-21 | 2023-07-12 | SRX Cardio, LLC | Composition and methods of use of novel phenylalanine small organic compounds to directly modulate pcsk9 protein activity |
| HK1257102A1 (zh) | 2015-08-21 | 2019-10-11 | Portola Pharmaceuticals, Inc. | 苯基哌嗪前蛋白转化酶枯草杆菌蛋白酶/kexin9型(pcsk9)调节剂及其应用 |
| WO2017107089A1 (en) | 2015-12-23 | 2017-06-29 | Merck Sharp & Dohme Corp. | 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor |
| ES2789756T3 (es) | 2015-12-23 | 2020-10-26 | Merck Sharp & Dohme | Moduladores alostéricos de 6,7-dihidro-5H-pirrolo[3,4-b]piridin-5-ona del receptor de acetilcolina muscarínico M4 |
| WO2017107087A1 (en) * | 2015-12-23 | 2017-06-29 | Merck Sharp & Dohme Corp. | 6, 7-dihydro-5h-pyrrolo [3, 4-b] pyridin-5-oneallosteric modulators of the m4 muscarinic acetylcholine receptor |
| US20190119236A1 (en) | 2016-02-23 | 2019-04-25 | Portola Pharmaceuticals, Inc. | Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9) |
| WO2018112843A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
| WO2018112842A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor |
| TW201827422A (zh) | 2017-01-13 | 2018-08-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | １，２，４－三嗪－３－胺類衍生物、其製備方法及其在醫藥上的應用 |
| CN110382499B (zh) | 2017-02-27 | 2023-01-03 | 贝达药业股份有限公司 | Fgfr抑制剂及其应用 |
| WO2018166493A1 (zh) | 2017-03-16 | 2018-09-20 | 江苏恒瑞医药股份有限公司 | 杂芳基并[4，3-c]嘧啶-5-胺类衍生物、其制备方法及其在医药上的应用 |
| AU2018341781B2 (en) | 2017-09-28 | 2023-03-30 | Cstone Pharmaceuticals | Fused ring derivative as A2A receptor inhibitor |
| US11498923B2 (en) | 2017-12-13 | 2022-11-15 | Merck Sharp & Dohme Llc | Substituted imidazo[1,2-c]quinazolines as A2A antagonists |
| JP2021512959A (ja) | 2018-02-06 | 2021-05-20 | 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司Ｊｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．， Ｌｔｄ． | ピラゾロ［１，５−ａ］［１，３，５］トリアジン−２−アミン誘導体、その製造法、およびその医薬用途 |
| WO2020106558A1 (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 |
| 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 |
| 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 |
| CR20210271A (es) | 2018-11-30 | 2021-07-14 | Merck Sharp & Dohme | Derivados de amino triazolo quinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmacéuticas y su uso |
| CN113727999A (zh) | 2019-01-11 | 2021-11-30 | 奥默罗斯公司 | 用于治疗癌症的方法和组合物 |
| AR117844A1 (es) | 2019-01-22 | 2021-09-01 | Merck Patent Gmbh | Derivados de tiazolopiridina como antagonistas del receptor de adenosina |
| CA3102364A1 (en) | 2019-03-26 | 2020-10-01 | Novel Pharma Inc. | Long-acting fatty acid-conjugated gnrh derivatives and pharmaceutical compositions containing same |
| PE20231066A1 (es) | 2020-02-07 | 2023-07-17 | Gasherbrum Bio Inc | Agonistas heterociclicos de glp-1 |
| US20240076297A1 (en) * | 2020-07-24 | 2024-03-07 | Merck Sharp & Dohme Llc | Adenosine a2a and a2b receptor dual antagonists for immuno-oncology |
| EP4185296A4 (en) * | 2020-07-24 | 2025-03-05 | Merck Sharp & Dohme LLC | DUAL ADENOSINE A2A RECEPTOR AND A2B RECEPTOR ANTAGONISTS FOR IMMUNO-ONCOLOGY |
| JP7858636B2 (ja) | 2020-09-10 | 2026-05-14 | ガシャーブラム・バイオ・インコーポレイテッド | ヘテロ環ｇｌｐ－１アゴニスト |
| CN112159411A (zh) * | 2020-10-15 | 2021-01-01 | 南京工业大学 | 一种三氟甲基取代嘧啶并[1,3]二氮杂*化合物及其制备方法 |
| US12115154B2 (en) | 2020-12-16 | 2024-10-15 | Srx Cardio, Llc | Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) |
| KR20250004779A (ko) | 2022-04-13 | 2025-01-08 | 길리애드 사이언시즈, 인코포레이티드 | Trop-2 발현 암을 치료하기 위한 병용 요법 |
| IL322686A (en) | 2023-02-16 | 2025-10-01 | Gasherbrum Bio Inc | Heterocyclic glp-1 agonists |
| WO2025137640A1 (en) | 2023-12-22 | 2025-06-26 | Gilead Sciences, Inc. | Azaspiro wrn inhibitors |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4713383A (en) * | 1984-10-01 | 1987-12-15 | Ciba-Geigy Corporation | Triazoloquinazoline compounds, and their methods of preparation, pharmaceutical compositions, and uses |
| EP0181282A1 (de) * | 1984-10-01 | 1986-05-14 | Ciba-Geigy Ag | Triazolochinazolinverbindungen |
| 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 |
| ATE208199T1 (de) | 1993-07-27 | 2001-11-15 | Kyowa Hakko Kogyo Kk | Arzneimittel gegen parkinsonsche krankheit |
| WO1995035107A1 (en) * | 1994-06-20 | 1995-12-28 | Smithkline Beecham Corporation | Endothelin receptor antagonists |
| US5571775A (en) | 1994-07-11 | 1996-11-05 | Dowelanco | N-aryl[1,2,4]triazolo[1,5-a]pyridine-2-sulfonamide herbicides |
| 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 |
| US5929106A (en) * | 1997-10-27 | 1999-07-27 | Smithkline Beecham Corporation | Endothelin receptor antagonists |
| SI1283839T1 (enExample) * | 2000-05-26 | 2005-08-31 | Schering Corp | |
| AU2001274287A1 (en) * | 2000-06-20 | 2002-01-02 | Nour Eddin Ajan Alhadid | Electrical drive line |
| US6358964B1 (en) * | 2000-07-26 | 2002-03-19 | King Pharmaceuticals Research And Development, Inc. | Adenosine, A3 receptor modulators |
| GB0100624D0 (en) * | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds VII |
| EP1527074A1 (en) * | 2002-07-25 | 2005-05-04 | Pharmacia Italia S.p.A. | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| AU2003304527B2 (en) * | 2002-12-19 | 2010-09-09 | Merck Sharp & Dohme Corp. | Uses of adenosine A2a receptor antagonists |
| DE602004018637D1 (de) * | 2003-04-09 | 2009-02-05 | Biogen Idec Inc | A2a-adenosinrezeptorantagonisten |
| 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 |
| PE20070521A1 (es) * | 2005-09-23 | 2007-07-13 | Schering Corp | 7-[2-[4-(6-FLUORO-3-METIL-1,2-BENCISOXAZOL-5-IL)-1-PIPERAZINIL]ETIL]-2-(1-PROPINIL)-7H-PIRAZOL-[4,3-E]-[1,2,4]-TRIAZOL-[1,5-C]-PIRIMIDIN-5-AMINA COMO ANTAGONISTA DEL RECEPTOR DE ADENOSINA A2a |
| ATE457988T1 (de) | 2006-06-26 | 2010-03-15 | Schering Corp | A2a-adenosin-rezeptor-antagonisten |
| US20090062253A1 (en) | 2007-08-31 | 2009-03-05 | Kalypsys, Inc. | Heterocyclodiazepine cannabinoid receptor modulators for treatment of disease |
| EP2210891A1 (en) * | 2009-01-26 | 2010-07-28 | Domain Therapeutics | New adenosine receptor ligands and uses thereof |
| EP2509983B1 (en) * | 2009-11-16 | 2014-09-17 | Merck Sharp & Dohme Corp. | FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY |
| WO2012135084A1 (en) * | 2011-03-31 | 2012-10-04 | Merck Sharp & Dohme Corp. | METABOLITES OF 2-(FURAN-2-YL)-7-(2-(4-(4-(2-METHOXYETHOXY)PHENYL)PIPERAZIN-1-YL)ETHYL)-7H-PYRAZOLO[4,3-e][1,2,4]TRIAZOLO[1,5-c]PYRIMIDIN-5-AMINE AND THEIR UTILITY AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| WO2014101113A1 (en) | 2012-12-28 | 2014-07-03 | Merck Sharp & Dohme Corp. | Piperazine-substituted 7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties |
-
2012
- 2012-12-28 WO PCT/CN2012/087865 patent/WO2014101120A1/en not_active Ceased
-
2013
- 2013-06-06 WO PCT/CN2013/076853 patent/WO2014101373A1/en not_active Ceased
- 2013-12-20 RS RS20180410A patent/RS57162B1/sr unknown
- 2013-12-20 KR KR1020157020147A patent/KR102165113B1/ko not_active Expired - Fee Related
- 2013-12-20 LT LTEP13866588.0T patent/LT2945632T/lt unknown
- 2013-12-20 JP JP2015550682A patent/JP6306049B2/ja not_active Expired - Fee Related
- 2013-12-20 WO PCT/US2013/076781 patent/WO2014105666A1/en not_active Ceased
- 2013-12-20 EP EP13866588.0A patent/EP2945632B1/en active Active
- 2013-12-20 NO NO13866588A patent/NO2945632T3/no unknown
- 2013-12-20 CA CA2896056A patent/CA2896056C/en active Active
- 2013-12-20 DK DK13866588.0T patent/DK2945632T3/en active
- 2013-12-20 HR HRP20180678TT patent/HRP20180678T1/hr unknown
- 2013-12-20 AU AU2013370977A patent/AU2013370977B2/en not_active Ceased
- 2013-12-20 MX MX2015008481A patent/MX370017B/es active IP Right Grant
- 2013-12-20 RU RU2018136104A patent/RU2018136104A/ru unknown
- 2013-12-20 PL PL13866588T patent/PL2945632T3/pl unknown
- 2013-12-20 US US14/655,648 patent/US9708347B2/en active Active
- 2013-12-20 RU RU2015131148A patent/RU2671628C2/ru active
- 2013-12-20 BR BR112015015468A patent/BR112015015468B8/pt not_active IP Right Cessation
- 2013-12-20 SI SI201330980T patent/SI2945632T1/en unknown
- 2013-12-20 ES ES13866588.0T patent/ES2667477T3/es active Active
- 2013-12-20 HU HUE13866588A patent/HUE037950T2/hu unknown
- 2013-12-20 PT PT138665880T patent/PT2945632T/pt unknown
- 2013-12-20 ME MEP-2018-97A patent/ME03034B/me unknown
-
2017
- 2017-02-02 US US15/423,238 patent/US10011615B2/en active Active
-
2018
- 2018-05-04 CY CY20181100472T patent/CY1120258T1/el unknown
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