AU2013370977B2 - Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with A2A antagonist properties - Google Patents
Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with A2A antagonist properties Download PDFInfo
- Publication number
- AU2013370977B2 AU2013370977B2 AU2013370977A AU2013370977A AU2013370977B2 AU 2013370977 B2 AU2013370977 B2 AU 2013370977B2 AU 2013370977 A AU2013370977 A AU 2013370977A AU 2013370977 A AU2013370977 A AU 2013370977A AU 2013370977 B2 AU2013370977 B2 AU 2013370977B2
- Authority
- AU
- Australia
- Prior art keywords
- triazolo
- quinazolin
- amine
- methoxy
- 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.)
- Ceased
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P25/14—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Hydrogenated Pyridines (AREA)
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 |
| AUPCT/CN2012/087865 | 2012-12-28 | ||
| AUPCT/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 (2)
| Publication Number | Publication Date |
|---|---|
| AU2013370977A1 AU2013370977A1 (en) | 2015-07-09 |
| AU2013370977B2 true AU2013370977B2 (en) | 2017-12-14 |
Family
ID=51019745
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2013370977A Ceased AU2013370977B2 (en) | 2012-12-28 | 2013-12-20 | Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with A2A antagonist properties |
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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001099264A1 (en) * | 2000-06-20 | 2001-12-27 | Rees, Alexander, Ellison | Electrical drive line |
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| 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 |
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| 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 |
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| 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 |
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| 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
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001099264A1 (en) * | 2000-06-20 | 2001-12-27 | Rees, Alexander, Ellison | Electrical drive line |
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| FGA | Letters patent sealed or granted (standard patent) | ||
| HB | Alteration of name in register |
Owner name: MERCK SHARP & DOHME LLC Free format text: FORMER NAME(S): MERCK SHARP & DOHME CORP. |
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| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |