CN109689664B - 作为par4抑制剂的三环杂芳基取代的喹啉和氮杂喹啉化合物 - Google Patents
作为par4抑制剂的三环杂芳基取代的喹啉和氮杂喹啉化合物 Download PDFInfo
- Publication number
- CN109689664B CN109689664B CN201780056459.5A CN201780056459A CN109689664B CN 109689664 B CN109689664 B CN 109689664B CN 201780056459 A CN201780056459 A CN 201780056459A CN 109689664 B CN109689664 B CN 109689664B
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- CN
- China
- Prior art keywords
- thiazol
- methoxy
- methylquinoxalin
- methyl
- benzo
- Prior art date
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Classifications
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- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, 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 three hetero rings
- C07D515/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662362121P | 2016-07-14 | 2016-07-14 | |
| US62/362,121 | 2016-07-14 | ||
| PCT/US2017/041880 WO2018013776A1 (en) | 2016-07-14 | 2017-07-13 | Tricyclic heteroaryl-substituted quinoline and azaquinoline compounds as par4 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109689664A CN109689664A (zh) | 2019-04-26 |
| CN109689664B true CN109689664B (zh) | 2022-04-15 |
Family
ID=59384259
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780056459.5A Active CN109689664B (zh) | 2016-07-14 | 2017-07-13 | 作为par4抑制剂的三环杂芳基取代的喹啉和氮杂喹啉化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US20190315774A1 (enExample) |
| EP (1) | EP3484894B1 (enExample) |
| JP (1) | JP6903732B2 (enExample) |
| KR (1) | KR102468661B1 (enExample) |
| CN (1) | CN109689664B (enExample) |
| ES (1) | ES2823127T3 (enExample) |
| WO (1) | WO2018013776A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3484874B1 (en) | 2016-07-14 | 2020-04-29 | Bristol-Myers Squibb Company | Monocyclic heteroaryl substituted compounds |
| EP3484881B1 (en) | 2016-07-14 | 2020-04-29 | Bristol-Myers Squibb Company | Bicyclic heteroaryl substituted compounds |
| JP7058256B2 (ja) | 2016-07-14 | 2022-04-21 | ブリストル-マイヤーズ スクイブ カンパニー | 二環式ヘテロアリール置換化合物 |
| CN111440146B (zh) * | 2020-05-15 | 2022-10-21 | 中国药科大学 | 一种具有par4拮抗活性的苯并三嗪类化合物及其应用 |
| CN117285527A (zh) * | 2023-09-25 | 2023-12-26 | 中国药科大学 | 一种噌啉类par4拮抗剂及其医药应用 |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1982001706A1 (en) * | 1980-11-11 | 1982-05-27 | Tominaga Michiaki | Carbostyril compounds,composition containing same,and process for their preparation |
| EP0534443A1 (en) * | 1991-09-26 | 1993-03-31 | Mitsubishi Chemical Corporation | 3,6-Disubstituted pyridazine derivatives |
| WO2013163241A1 (en) * | 2012-04-26 | 2013-10-31 | Bristol-Myers Squibb Company | Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
| WO2015077550A1 (en) * | 2013-11-22 | 2015-05-28 | University Of Kentucky Research Foundation | Arylquinoline and analog compounds and use thereof to treat cancer |
| WO2017019828A1 (en) * | 2015-07-30 | 2017-02-02 | Bristol-Myers Squibb Company | Aryl substituted bicyclic heteroaryl compounds |
| WO2018013770A1 (en) * | 2016-07-14 | 2018-01-18 | Bristol-Myers Squibb Company | Bicyclic heteroaryl substituted compounds |
| WO2018013774A1 (en) * | 2016-07-14 | 2018-01-18 | Bristol-Myers Squibb Company | Bicyclic heteroaryl substituted compounds |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2928079B2 (ja) | 1994-02-14 | 1999-07-28 | 永信薬品工業股▲ふん▼有限公司 | 1−(置換ベンジル)−3−(置換アリール)縮合ピラゾール類、その製造法及びその用途 |
| US6166041A (en) | 1995-10-11 | 2000-12-26 | Euro-Celtique, S.A. | 2-heteroaryl and 2-heterocyclic benzoxazoles as PDE IV inhibitors for the treatment of asthma |
| US6387942B2 (en) * | 2000-06-19 | 2002-05-14 | Yung Shin Pharmaceutical Ind. Co. Ltd | Method of treating disorders related to protease-activated receptors-induced cell activation |
| EP1348701A1 (en) | 2002-03-28 | 2003-10-01 | Warner-Lambert Company LLC | (2,4-disubstituted-thiazol-5-yl) amine compounds as PDE7 inhibitors |
| US7511145B2 (en) | 2003-08-01 | 2009-03-31 | Genelabs Technologies, Inc. | Bicyclic heteroaryl derivatives |
| WO2005113522A1 (en) | 2004-05-07 | 2005-12-01 | Janssen Pharmaceutica, N.V. | Azole carboxamide inhibitors of bacterial type iii protein secretion systems |
| JP2008508314A (ja) | 2004-07-28 | 2008-03-21 | アイアールエム・リミテッド・ライアビリティ・カンパニー | ステロイドホルモン核内受容体のモジュレーターとしての化合物および組成物 |
| AU2006204917A1 (en) | 2005-01-14 | 2006-07-20 | Smithkline Beecham Corporation | Indole derivatives for treating viral infections |
| WO2007149395A2 (en) | 2006-06-20 | 2007-12-27 | Amphora Discovery Corporation | 2,5-substituted oxazole derivatives as protein kinase inhibitors for the treatment of cancer |
| BRPI0713946A2 (pt) | 2006-06-29 | 2012-12-04 | Hoffmann La Roche | compostos, composições farmacêuticas que os compreendem, método para o tratamento terapêutico e/ou profilático de enfermidades que são moduladas por agonistas de fxr, e uso dos compostos |
| WO2008073451A2 (en) | 2006-12-11 | 2008-06-19 | Sirtris Pharmaceuticals, Inc. | Benzoimidazole derivatives as sirtuin (sir) modulating compounds |
| EP2227770A4 (en) | 2007-11-30 | 2011-11-09 | Glaxosmithkline Llc | PROLYLHYDROXYLASEINHIBITOREN |
| CA2723135A1 (en) | 2008-05-01 | 2009-11-05 | Sirtris Pharmaceuticals, Inc. | Quenolines and related analogs as sirtuin modulators |
| EP2282995B1 (en) | 2008-05-23 | 2015-08-26 | Novartis AG | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
| AU2009274023A1 (en) | 2008-07-23 | 2010-01-28 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| US20130072473A1 (en) | 2011-05-09 | 2013-03-21 | Proteostasis Therapeutics, Inc. | Compounds for treating protein folding disorders |
| TW201348226A (zh) | 2012-02-28 | 2013-12-01 | Amgen Inc | 作為pim抑制劑之醯胺 |
| JP6073464B2 (ja) | 2012-04-26 | 2017-02-01 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 血小板凝集を治療するためのプロテアーゼ活性化受容体4(par4)阻害剤としてのイミダゾチアジアゾールおよびイミダゾピラジン誘導体 |
| BR112014026493A2 (pt) | 2012-04-26 | 2017-06-27 | Bristol Myers Squibb Co | derivados de imidazotiadiazol como inibidores do receptor ativado por protease 4 (par4) para tratar a agregação de plaqueta |
| US9617279B1 (en) | 2014-06-24 | 2017-04-11 | Bristol-Myers Squibb Company | Imidazooxadiazole compounds |
| US9598419B1 (en) | 2014-06-24 | 2017-03-21 | Universite De Montreal | Imidazotriazine and imidazodiazine compounds |
| EP3262052A1 (en) | 2015-02-26 | 2018-01-03 | Bristol-Myers Squibb Company | Benzothiazole and benzothiophne compounds |
| EP3262053B1 (en) | 2015-02-26 | 2022-10-05 | Université de Montréal | Imidazothiadiazole compounds as par4-inhibitors |
| EP3484874B1 (en) | 2016-07-14 | 2020-04-29 | Bristol-Myers Squibb Company | Monocyclic heteroaryl substituted compounds |
-
2017
- 2017-07-13 US US16/317,258 patent/US20190315774A1/en not_active Abandoned
- 2017-07-13 WO PCT/US2017/041880 patent/WO2018013776A1/en not_active Ceased
- 2017-07-13 JP JP2019501630A patent/JP6903732B2/ja active Active
- 2017-07-13 EP EP17742926.3A patent/EP3484894B1/en active Active
- 2017-07-13 KR KR1020197004282A patent/KR102468661B1/ko active Active
- 2017-07-13 ES ES17742926T patent/ES2823127T3/es active Active
- 2017-07-13 CN CN201780056459.5A patent/CN109689664B/zh active Active
-
2021
- 2021-01-06 US US17/142,288 patent/US11932658B2/en active Active
-
2023
- 2023-12-06 US US18/530,405 patent/US20240309019A1/en active Pending
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1982001706A1 (en) * | 1980-11-11 | 1982-05-27 | Tominaga Michiaki | Carbostyril compounds,composition containing same,and process for their preparation |
| EP0534443A1 (en) * | 1991-09-26 | 1993-03-31 | Mitsubishi Chemical Corporation | 3,6-Disubstituted pyridazine derivatives |
| WO2013163241A1 (en) * | 2012-04-26 | 2013-10-31 | Bristol-Myers Squibb Company | Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
| WO2015077550A1 (en) * | 2013-11-22 | 2015-05-28 | University Of Kentucky Research Foundation | Arylquinoline and analog compounds and use thereof to treat cancer |
| WO2017019828A1 (en) * | 2015-07-30 | 2017-02-02 | Bristol-Myers Squibb Company | Aryl substituted bicyclic heteroaryl compounds |
| WO2018013770A1 (en) * | 2016-07-14 | 2018-01-18 | Bristol-Myers Squibb Company | Bicyclic heteroaryl substituted compounds |
| WO2018013774A1 (en) * | 2016-07-14 | 2018-01-18 | Bristol-Myers Squibb Company | Bicyclic heteroaryl substituted compounds |
Non-Patent Citations (2)
| Title |
|---|
| Studies on the Chemical constituents of Rutaceous Plants.XXXVI.Synthesis of Ethyl Isodecarine;HISASHI ISHII et al.;《Chem. Phem. Bull》;19771231;第514-519页 * |
| Substituted indoles as selective protease activated receptor 4 (PAR-4)antagonists: Discovery and SAR of ML354;Wandong Wen et al.;《Bioorganic & Medicinal Chemistry Letters》;20140815;第4708-4713页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20190315774A1 (en) | 2019-10-17 |
| JP6903732B2 (ja) | 2021-07-14 |
| KR102468661B1 (ko) | 2022-11-17 |
| EP3484894B1 (en) | 2020-08-19 |
| EP3484894A1 (en) | 2019-05-22 |
| KR20190026906A (ko) | 2019-03-13 |
| ES2823127T3 (es) | 2021-05-06 |
| US20240309019A1 (en) | 2024-09-19 |
| CN109689664A (zh) | 2019-04-26 |
| US20210188877A1 (en) | 2021-06-24 |
| WO2018013776A1 (en) | 2018-01-18 |
| JP2019524732A (ja) | 2019-09-05 |
| US11932658B2 (en) | 2024-03-19 |
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