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 | ||
| 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 |
| CNPCT/CN2013/076853 | 2013-06-06 | ||
| 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 (show.php) | 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 (show.php) |
| EP (1) | EP2945632B1 (show.php) |
| JP (1) | JP6306049B2 (show.php) |
| KR (1) | KR102165113B1 (show.php) |
| AU (1) | AU2013370977B2 (show.php) |
| BR (1) | BR112015015468B8 (show.php) |
| CA (1) | CA2896056C (show.php) |
| CY (1) | CY1120258T1 (show.php) |
| DK (1) | DK2945632T3 (show.php) |
| ES (1) | ES2667477T3 (show.php) |
| HR (1) | HRP20180678T1 (show.php) |
| HU (1) | HUE037950T2 (show.php) |
| LT (1) | LT2945632T (show.php) |
| ME (1) | ME03034B (show.php) |
| MX (1) | MX370017B (show.php) |
| NO (1) | NO2945632T3 (show.php) |
| PL (1) | PL2945632T3 (show.php) |
| PT (1) | PT2945632T (show.php) |
| RS (1) | RS57162B1 (show.php) |
| RU (2) | RU2671628C2 (show.php) |
| SI (1) | SI2945632T1 (show.php) |
| WO (3) | WO2014101120A1 (show.php) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3253390B1 (en) * | 2015-02-06 | 2022-04-13 | Merck Sharp & Dohme Corp. | Aminoquinazoline compounds as a2a antagonist |
| US10688082B2 (en) | 2015-06-11 | 2020-06-23 | Merck Sharp & Dohme Corp. | Aminopyrazine compounds with A2A antagonist properties |
| WO2017008205A1 (en) * | 2015-07-10 | 2017-01-19 | Merck Sharp & Dohme Corp. | Substituted aminoquinazoline compounds as a2a antagonist |
| US10821106B2 (en) | 2015-08-21 | 2020-11-03 | Srx Cardio, Llc | Composition and methods of use of novel phenylalanine small organic compounds to directly modulate PCSK9 protein activity |
| EP3337564A4 (en) * | 2015-08-21 | 2019-01-23 | Portola Pharmaceuticals, Inc. | COMPOSITION AND METHOD FOR THE USE OF TETRAHYDROISOCHINOLINE SMALL MOLECULES FOR THE BINDING AND MODULATION OF PCSK9 PROTEIN ACTIVITY |
| WO2017034997A1 (en) | 2015-08-21 | 2017-03-02 | Portola Pharmaceuticals, Inc. | Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (pcsk9) modulators and their use |
| 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 |
| 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 |
| US10329289B2 (en) | 2015-12-23 | 2019-06-25 | Merck Sharp & Dohme Corp. | 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric 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 |
| US11014904B2 (en) | 2017-01-13 | 2021-05-25 | Jiangsu Hengrui Medicine Co., Ltd. | 1,2,4-triazine-3-amine derivative, preparation method therefor, and use thereof in medicine |
| SG11201907909TA (en) | 2017-02-27 | 2019-09-27 | Betta Pharmaceuticals Co Ltd | Fgfr inhibitor and application thereof |
| UA125592C2 (uk) | 2017-03-16 | 2022-04-27 | Джянгсу Хенгруй Медісін Ко., Лтд. | ПОХІДНА ГЕТЕРОАРИЛ[4,3-c]ПІРИМІДИН-5-АМІНУ, СПОСІБ ЇЇ ОТРИМАННЯ ТА ЇЇ МЕДИЧНІ ЗАСТОСУВАННЯ |
| ES2927086T3 (es) | 2017-09-28 | 2022-11-02 | Cstone Pharmaceuticals Suzhou Co Ltd | Derivado de anillo condensado como inhibidor del receptor A2A |
| EP3723754A4 (en) | 2017-12-13 | 2021-05-19 | Merck Sharp & Dohme Corp. | IMIDAZO [1,2-C] QUINAZOLINE-5-AMINE COMPOUNDS WITH PROPERTIES OF A2A ANTAGONIST |
| US20210032253A1 (en) | 2018-02-06 | 2021-02-04 | Jiangsu Hengrui Medicine Co., Ltd. | Pyrazolo[1,5-a][1,3,5]triazine-2-amine derivative, preparation method therefor and medical use thereof |
| EP3883576B1 (en) | 2018-11-20 | 2025-12-17 | Merck Sharp & Dohme LLC | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| MA55142A (fr) | 2018-11-20 | 2022-02-23 | Merck Sharp & Dohme | Amino-triazolopyrimidine et amino-triazolopyrazine substitués antagoniste du récepteur de l'adénosine, compositions pharmaceutiques et leur utilisation |
| CA3120331A1 (en) | 2018-11-30 | 2020-06-04 | Merck Sharp & Dohme Corp. | 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use |
| CN113329791A (zh) | 2018-11-30 | 2021-08-31 | 默沙东公司 | 作为腺苷受体拮抗剂的9-取代的氨基三唑并喹唑啉衍生物、药物组合物及其用途 |
| BR112021012685A2 (pt) | 2019-01-11 | 2021-12-28 | Omeros Corp | Métodos para tratar câncer, para aumentar o nível de citocinas th1 nas células mononucleares de sangue periférico humanas, para realçar uma resposta imune antitumoral e para estimular e/ou amplificar uma resposta imune em um sujeito mamífero sofrendo de ou em risco de desenvolver câncer ou metástase de câncer, e, composição farmacêutica |
| AR117844A1 (es) | 2019-01-22 | 2021-09-01 | Merck Patent Gmbh | Derivados de tiazolopiridina como antagonistas del receptor de adenosina |
| AU2019437315B2 (en) | 2019-03-26 | 2022-10-06 | Novel Pharma Inc. | Long-acting fatty acid-binding GnRH derivative and pharmaceutical composition comprising same |
| MX2022009524A (es) | 2020-02-07 | 2023-01-11 | Gasherbrum Bio Inc | Agonistas heterociclicos de glp-1. |
| EP4185296A4 (en) * | 2020-07-24 | 2025-03-05 | Merck Sharp & Dohme LLC | DUAL ADENOSINE A2A RECEPTOR AND A2B RECEPTOR ANTAGONISTS FOR IMMUNO-ONCOLOGY |
| EP4185297A4 (en) * | 2020-07-24 | 2024-08-28 | Merck Sharp & Dohme LLC | 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 |
| WO2024169952A1 (en) | 2023-02-16 | 2024-08-22 | 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 |
| WO1995003806A1 (en) * | 1993-07-27 | 1995-02-09 | Kyowa Hakko Kogyo Co., Ltd. | Remedy for parkinson's disease |
| 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 |
| WO2001092264A1 (en) | 2000-05-26 | 2001-12-06 | Schering Corporation | Adenosine a2a receptor antagonists |
| WO2001099264A1 (en) * | 2000-06-20 | 2001-12-27 | Rees, Alexander, Ellison | 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 |
| TWI331036B (en) * | 2002-12-19 | 2010-10-01 | Schering Corp | Adenosine a2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| ATE418555T1 (de) * | 2003-04-09 | 2009-01-15 | Biogen Idec Inc | A2a-adenosinrezeptorantagonisten |
| CA2522813C (en) * | 2003-04-23 | 2009-09-08 | 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 |
| JP2010509189A (ja) | 2006-06-26 | 2010-03-25 | 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 |
| 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 |
| WO2011060207A1 (en) * | 2009-11-16 | 2011-05-19 | Schering Corporation | 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 EP EP13866588.0A patent/EP2945632B1/en active Active
- 2013-12-20 PL PL13866588T patent/PL2945632T3/pl unknown
- 2013-12-20 US US14/655,648 patent/US9708347B2/en active Active
- 2013-12-20 BR BR112015015468A patent/BR112015015468B8/pt not_active IP Right Cessation
- 2013-12-20 RS RS20180410A patent/RS57162B1/sr unknown
- 2013-12-20 RU RU2015131148A patent/RU2671628C2/ru active
- 2013-12-20 DK DK13866588.0T patent/DK2945632T3/en active
- 2013-12-20 ME MEP-2018-97A patent/ME03034B/me unknown
- 2013-12-20 AU AU2013370977A patent/AU2013370977B2/en not_active Ceased
- 2013-12-20 KR KR1020157020147A patent/KR102165113B1/ko not_active Expired - Fee Related
- 2013-12-20 JP JP2015550682A patent/JP6306049B2/ja not_active Expired - Fee Related
- 2013-12-20 PT PT138665880T patent/PT2945632T/pt unknown
- 2013-12-20 HU HUE13866588A patent/HUE037950T2/hu unknown
- 2013-12-20 SI SI201330980T patent/SI2945632T1/en unknown
- 2013-12-20 LT LTEP13866588.0T patent/LT2945632T/lt unknown
- 2013-12-20 HR HRP20180678TT patent/HRP20180678T1/hr unknown
- 2013-12-20 RU RU2018136104A patent/RU2018136104A/ru unknown
- 2013-12-20 CA CA2896056A patent/CA2896056C/en active Active
- 2013-12-20 MX MX2015008481A patent/MX370017B/es active IP Right Grant
- 2013-12-20 WO PCT/US2013/076781 patent/WO2014105666A1/en not_active Ceased
- 2013-12-20 NO NO13866588A patent/NO2945632T3/no unknown
- 2013-12-20 ES ES13866588.0T patent/ES2667477T3/es active Active
-
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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