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 (cg-RX-API-DMAC7.html) | 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)
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016126570A1 (en) * | 2015-02-06 | 2016-08-11 | 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 |
| HK1260897A1 (zh) | 2015-08-21 | 2019-12-27 | Portola Pharmaceuticals, Inc. | 使用四氢异喹啉小分子来结合并调节pcsk9的蛋白活性的组合物和方法 |
| WO2017034997A1 (en) | 2015-08-21 | 2017-03-02 | Portola Pharmaceuticals, Inc. | Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (pcsk9) modulators and their use |
| HK1257100A1 (zh) | 2015-08-21 | 2019-10-11 | Portola Pharmaceuticals, Inc. | 使用新型苯丙胺酸小分子有机化合物来直接调节pcsk9的蛋白活性的组合物和方法 |
| 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 |
| 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 |
| TW201726675A (zh) | 2015-12-23 | 2017-08-01 | 默沙東藥廠 | M4毒蕈鹼乙醯膽鹼受體之異位調節劑6,7-二氫-5h-吡咯并[3,4-b]吡啶-5-酮 |
| WO2017147328A1 (en) | 2016-02-23 | 2017-08-31 | 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 |
| JP2020506885A (ja) | 2017-01-13 | 2020-03-05 | 江蘇恒瑞医薬股▲ふん▼有限公司 | 1,2,4−トリアジン−3−アミン誘導体、その製造方法、および医薬におけるその使用 |
| RU2745035C1 (ru) | 2017-02-27 | 2021-03-18 | Бетта Фармасьютикалз Ко., Лтд. | Ингибитор fgfr и его применение |
| KR20190129851A (ko) | 2017-03-16 | 2019-11-20 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 헤테로아릴[4,3-c]피리미딘-5-아민 유도체, 이의 제조 방법 및 이의 의학적 용도 |
| MX383975B (es) | 2017-09-28 | 2025-03-14 | Cstone Pharmaceuticals Suzhou Co Ltd | Derivado de anillo fusionado como inhibidor del receptor a2a |
| WO2019118313A1 (en) | 2017-12-13 | 2019-06-20 | Merck Sharp & Dohme Corp. | Imidazo [1,2-c] quinazolin-5-amine compounds with a2a antagonist properties |
| CN111511745B (zh) | 2018-02-06 | 2022-05-27 | 江苏恒瑞医药股份有限公司 | 吡唑并[1,5-a][1,3,5]三嗪-2-胺类衍生物、其制备方法及其应用 |
| US12414952B2 (en) | 2018-11-20 | 2025-09-16 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| US12466831B2 (en) | 2018-11-20 | 2025-11-11 | Merck Sharp & Dohme Llc | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| EP3886988A1 (en) | 2018-11-30 | 2021-10-06 | Merck Sharp & Dohme Corp. | 9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| 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 |
| AU2020205753B2 (en) | 2019-01-11 | 2025-05-29 | Omeros Corporation | Methods and compositions for treating cancer |
| AR117844A1 (es) | 2019-01-22 | 2021-09-01 | Merck Patent Gmbh | Derivados de tiazolopiridina como antagonistas del receptor de adenosina |
| ES2944511T3 (es) | 2019-03-26 | 2023-06-21 | Novel Pharma Inc | Derivado de GnRH que se une a ácido graso de acción prolongada y composición farmacéutica que comprende el mismo |
| PH12022552056A1 (en) | 2020-02-07 | 2024-02-12 | Gasherbrum Bio Inc | Heterocyclic glp-1 agonists |
| EP4185296A4 (en) * | 2020-07-24 | 2025-03-05 | Merck Sharp & Dohme LLC | DUAL ADENOSINE A2A RECEPTOR AND A2B RECEPTOR ANTAGONISTS FOR IMMUNO-ONCOLOGY |
| WO2022020552A1 (en) * | 2020-07-24 | 2022-01-27 | Merck Sharp & Dohme Corp. | Adenosine a2a and a2b receptor dual antagonists for immuno-oncology |
| 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) |
| WO2023201267A1 (en) | 2022-04-13 | 2023-10-19 | Gilead Sciences, Inc. | Combination therapy for treating trop-2 expressing cancers |
| EP4665730A1 (en) | 2023-02-16 | 2025-12-24 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| US20250230168A1 (en) | 2023-12-22 | 2025-07-17 | 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 |
| US5736564A (en) | 1994-06-20 | 1998-04-07 | 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 |
| PE20020062A1 (es) * | 2000-05-26 | 2002-02-02 | Schering Corp | 5-AMINO-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA COMO ANTAGONISTAS RECEPTORES DE ADENOSINA A2a |
| EP1293029A1 (en) * | 2000-06-20 | 2003-03-19 | Alexander Ellison Rees | 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 |
| US20060135508A1 (en) | 2002-07-25 | 2006-06-22 | Manuela Villa | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| BR0317436A (pt) * | 2002-12-19 | 2005-11-16 | Schering Corp | Usos de antagonistas do receptor a2a de adenosina |
| WO2004092173A2 (en) * | 2003-04-09 | 2004-10-28 | Biogen Idec Ma Inc. | A2a adenosine receptor antagonists |
| ATE432282T1 (de) * | 2003-04-23 | 2009-06-15 | Schering Corp | 2-alkinyl- und 2-alkenyl-pyrazolo-ä4,3-eü -1,2,4- triazolo-ä1,5-cü -pyrimidinadenosin a2a rezeptorantagonisten |
| 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 |
| ES2339502T3 (es) | 2006-06-26 | 2010-05-20 | Schering Corporation | Antagonistas del receptor a2a de adenisina. |
| WO2009032754A2 (en) * | 2007-08-31 | 2009-03-12 | 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 LT LTEP13866588.0T patent/LT2945632T/lt unknown
- 2013-12-20 CA CA2896056A patent/CA2896056C/en active Active
- 2013-12-20 PL PL13866588T patent/PL2945632T3/pl unknown
- 2013-12-20 NO NO13866588A patent/NO2945632T3/no unknown
- 2013-12-20 DK DK13866588.0T patent/DK2945632T3/en active
- 2013-12-20 PT PT138665880T patent/PT2945632T/pt unknown
- 2013-12-20 HR HRP20180678TT patent/HRP20180678T1/hr unknown
- 2013-12-20 KR KR1020157020147A patent/KR102165113B1/ko not_active Expired - Fee Related
- 2013-12-20 RS RS20180410A patent/RS57162B1/sr unknown
- 2013-12-20 SI SI201330980T patent/SI2945632T1/en unknown
- 2013-12-20 ES ES13866588.0T patent/ES2667477T3/es active Active
- 2013-12-20 US US14/655,648 patent/US9708347B2/en active Active
- 2013-12-20 ME MEP-2018-97A patent/ME03034B/me unknown
- 2013-12-20 BR BR112015015468A patent/BR112015015468B8/pt not_active IP Right Cessation
- 2013-12-20 JP JP2015550682A patent/JP6306049B2/ja not_active Expired - Fee Related
- 2013-12-20 RU RU2018136104A patent/RU2018136104A/ru unknown
- 2013-12-20 EP EP13866588.0A patent/EP2945632B1/en active Active
- 2013-12-20 HU HUE13866588A patent/HUE037950T2/hu unknown
- 2013-12-20 AU AU2013370977A patent/AU2013370977B2/en not_active Ceased
- 2013-12-20 WO PCT/US2013/076781 patent/WO2014105666A1/en not_active Ceased
- 2013-12-20 RU RU2015131148A patent/RU2671628C2/ru active
- 2013-12-20 MX MX2015008481A patent/MX370017B/es active IP Right Grant
-
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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