KR102468661B1 - Par4 억제제로서의 트리시클릭 헤테로아릴-치환된 퀴놀린 및 아자퀴놀린 화합물 - Google Patents

Par4 억제제로서의 트리시클릭 헤테로아릴-치환된 퀴놀린 및 아자퀴놀린 화합물 Download PDF

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KR102468661B1
KR102468661B1 KR1020197004282A KR20197004282A KR102468661B1 KR 102468661 B1 KR102468661 B1 KR 102468661B1 KR 1020197004282 A KR1020197004282 A KR 1020197004282A KR 20197004282 A KR20197004282 A KR 20197004282A KR 102468661 B1 KR102468661 B1 KR 102468661B1
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methyl
methoxy
methylquinoxalin
thiazol
carbamate
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KR20190026906A (ko
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샤오준 장
엘든 스콧 프리스틀리
오즈 스콧 핼펀
웬 지앙
사무엘 카예 레즈닉
제레미 엠. 리히터
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브리스톨-마이어스 스큅 컴퍼니
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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
    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (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)
KR1020197004282A 2016-07-14 2017-07-13 Par4 억제제로서의 트리시클릭 헤테로아릴-치환된 퀴놀린 및 아자퀴놀린 화합물 Active KR102468661B1 (ko)

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)

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KR20190026906A KR20190026906A (ko) 2019-03-13
KR102468661B1 true KR102468661B1 (ko) 2022-11-17

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US (3) US20190315774A1 (https=)
EP (1) EP3484894B1 (https=)
JP (1) JP6903732B2 (https=)
KR (1) KR102468661B1 (https=)
CN (1) CN109689664B (https=)
ES (1) ES2823127T3 (https=)
WO (1) WO2018013776A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109689664B (zh) 2016-07-14 2022-04-15 百时美施贵宝公司 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
EP3484878B1 (en) 2016-07-14 2020-08-19 Bristol-Myers Squibb Company Bicyclic heteroaryl substituted compounds
CN109689642B (zh) 2016-07-14 2022-04-12 百时美施贵宝公司 经单环杂芳基取代的化合物
KR102494647B1 (ko) 2016-07-14 2023-01-31 브리스톨-마이어스 스큅 컴퍼니 비시클릭 헤테로아릴 치환된 화합물
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013163279A1 (en) 2012-04-26 2013-10-31 Bristol-Myers Squibb Company Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation
WO2013163244A1 (en) 2012-04-26 2013-10-31 Bristol-Myers Squibb Company Imidazothiadiazole derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1164459A (en) * 1980-11-11 1984-03-27 Yung-Hsiung Yang Process for preparing (imidazo¬1,2-a|pyridine- 2-yl)-carbostyril or -3,4-dihydrocarbostyryl derivatives
TW279162B (https=) * 1991-09-26 1996-06-21 Mitsubishi Chem Corp
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
JP2007501189A (ja) 2003-08-01 2007-01-25 ジェネラブス テクノロジーズ，インコーポレイテッド フラビウイルス科に対する二環式イミダゾール誘導体
WO2005113522A1 (en) 2004-05-07 2005-12-01 Janssen Pharmaceutica, N.V. Azole carboxamide inhibitors of bacterial type iii protein secretion systems
US20090054417A1 (en) 2004-07-28 2009-02-26 Irm Llc Compounds and compositions as modulators of steroid hormone nuclear receptors
CN101103026A (zh) 2005-01-14 2008-01-09 健亚生物科技公司 用于治疗病毒感染的吲哚衍生物
US20080015193A1 (en) 2006-06-20 2008-01-17 Mendoza Jose S Certain azoles exhibiting ATP-utilizing enzyme inhibitory activity, compositions, and uses thereof
CN101479249B (zh) 2006-06-29 2012-10-10 霍夫曼-拉罗奇有限公司 苯并咪唑衍生物、其制备方法、它们作为fxr激动剂的用途及含有它们的药物制剂
WO2008073451A2 (en) 2006-12-11 2008-06-19 Sirtris Pharmaceuticals, Inc. Benzoimidazole derivatives as sirtuin (sir) modulating compounds
EA201000915A1 (ru) 2007-11-30 2011-02-28 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Ингибиторы пролилгидроксилазы
ES2586459T3 (es) 2008-05-01 2016-10-14 Glaxosmithkline Llc Quinolinas y análogos relacionados como moduladores de sirtuina
ES2554513T3 (es) 2008-05-23 2015-12-21 Novartis Ag Derivados de quinolinas y quinoxalinas como inhibidores de la proteína tirosina quinasa
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
EP2855489B1 (en) * 2012-04-26 2017-01-04 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
US9598419B1 (en) 2014-06-24 2017-03-21 Universite De Montreal Imidazotriazine and imidazodiazine compounds
US9617279B1 (en) 2014-06-24 2017-04-11 Bristol-Myers Squibb Company Imidazooxadiazole compounds
WO2016134450A1 (en) 2015-02-26 2016-09-01 Université de Montréal Imidazopyridazine and imidazothiadiazole compounds
EP3262052A1 (en) 2015-02-26 2018-01-03 Bristol-Myers Squibb Company Benzothiazole and benzothiophne compounds
CN108137514A (zh) * 2015-07-30 2018-06-08 百时美施贵宝公司 芳基取代的二环杂芳基化合物
EP3484878B1 (en) 2016-07-14 2020-08-19 Bristol-Myers Squibb Company Bicyclic heteroaryl substituted compounds
CN109689664B (zh) 2016-07-14 2022-04-15 百时美施贵宝公司 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
KR102494647B1 (ko) 2016-07-14 2023-01-31 브리스톨-마이어스 스큅 컴퍼니 비시클릭 헤테로아릴 치환된 화합물
CN109689642B (zh) 2016-07-14 2022-04-12 百时美施贵宝公司 经单环杂芳基取代的化合物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013163279A1 (en) 2012-04-26 2013-10-31 Bristol-Myers Squibb Company Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation
WO2013163244A1 (en) 2012-04-26 2013-10-31 Bristol-Myers Squibb Company Imidazothiadiazole derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation

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CN109689664A (zh) 2019-04-26
US12528827B2 (en) 2026-01-20
US20210188877A1 (en) 2021-06-24
ES2823127T3 (es) 2021-05-06
CN109689664B (zh) 2022-04-15
KR20190026906A (ko) 2019-03-13
WO2018013776A1 (en) 2018-01-18
JP2019524732A (ja) 2019-09-05
EP3484894B1 (en) 2020-08-19
US20240309019A1 (en) 2024-09-19
EP3484894A1 (en) 2019-05-22
JP6903732B2 (ja) 2021-07-14
US11932658B2 (en) 2024-03-19
US20190315774A1 (en) 2019-10-17

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