JP7102388B2 - 単環式ヘテロアリール置換化合物 - Google Patents

単環式ヘテロアリール置換化合物 Download PDF

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Publication number
JP7102388B2
JP7102388B2 JP2019501720A JP2019501720A JP7102388B2 JP 7102388 B2 JP7102388 B2 JP 7102388B2 JP 2019501720 A JP2019501720 A JP 2019501720A JP 2019501720 A JP2019501720 A JP 2019501720A JP 7102388 B2 JP7102388 B2 JP 7102388B2
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methylquinoxaline
difluoromethoxy
thiazole
mmol
minutes
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Japanese (ja)
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JP2019521153A (ja
JP2019521153A5 (enExample
Inventor
ジェレミー・エム・リヒター
シャオジュン・ジャン
エルドン・スコット・プリーストリー
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (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)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2019501720A 2016-07-14 2017-07-13 単環式ヘテロアリール置換化合物 Active JP7102388B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662362081P 2016-07-14 2016-07-14
US62/362,081 2016-07-14
PCT/US2017/041873 WO2018013772A1 (en) 2016-07-14 2017-07-13 Monocyclic heteroaryl substituted compounds

Publications (3)

Publication Number Publication Date
JP2019521153A JP2019521153A (ja) 2019-07-25
JP2019521153A5 JP2019521153A5 (enExample) 2020-08-06
JP7102388B2 true JP7102388B2 (ja) 2022-07-19

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JP2019501720A Active JP7102388B2 (ja) 2016-07-14 2017-07-13 単環式ヘテロアリール置換化合物

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US (1) US10815224B2 (enExample)
EP (1) EP3484874B1 (enExample)
JP (1) JP7102388B2 (enExample)
KR (1) KR102492715B1 (enExample)
CN (1) CN109689642B (enExample)
ES (1) ES2805030T3 (enExample)
WO (1) WO2018013772A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2823127T3 (es) 2016-07-14 2021-05-06 Bristol Myers Squibb Co Compuestos tricíclicos de quinolina y azaquinolina sustituidos con heteroarilo como inhibidores de PAR4
CN109689649B (zh) 2016-07-14 2022-07-19 百时美施贵宝公司 经二环杂芳基取代的化合物
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
EP4070733A4 (en) 2019-12-04 2022-11-30 NEC Corporation SYSTEM, METHOD AND COMPUTER PROGRAM FOR DETERMINING ABNORMAL PHYSICAL CONDITIONS
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
CN116041341B (zh) * 2022-11-24 2025-02-28 中国药科大学 一种喹唑啉类par4拮抗剂及其医药应用
KR20250110929A (ko) 2022-12-02 2025-07-21 뉴모라 테라퓨틱스, 인코포레이티드 신경학적 장애를 치료하는 방법

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006508113A (ja) 2002-11-12 2006-03-09 ファイザー・プロダクツ・インク キノリン誘導体

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4567269A (en) * 1982-11-12 1986-01-28 Riker Laboratories, Inc. Intermediates for the preparation of 6,7-dihydro-8-(imidazol-1-yl)-5-methyl-1-oxo-1H,5H-benzo[ij]quinolizine-2-carboxylic acids
US4472406A (en) * 1982-11-12 1984-09-18 Riker Laboratories, Inc. Antimicrobial 6,7-dihydro-8-(imidazol-1-yl)-5-methyl-1-oxo-1H,5H-benzo [ij]quinolizine-2-carboxylic acids and derivatives
US4567186A (en) * 1985-01-14 1986-01-28 Sterling Drug Inc. 5-Heteryl-1,6-naphthyridin-2(1H)-ones, cardiotonic use thereof and intermediates therefor
DE3541722A1 (de) * 1985-11-26 1987-05-27 Basf Ag Chinolinderivate und ihre verwendung zur bekaempfung von unerwuenschtem pflanzenwachstum
EP0224823A3 (de) * 1985-11-26 1988-02-10 BASF Aktiengesellschaft Chinolinderivate und ihre Verwendung zur Bekämpfung von unerwümschtem Pflanzenwachstum
KR900004213A (ko) * 1988-08-12 1990-03-27 최근선 쌍 방향 송수신의 원격 제어 시스템
US5110347A (en) 1990-11-26 1992-05-05 E. I Du Pont De Nemours And Company Substituted fused heterocyclic herbicides
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
US5633218A (en) * 1995-05-24 1997-05-27 E. I. Du Pont De Nemours And Company Herbicidal benzodioxoles and benzodioxanes
US6245760B1 (en) * 1997-05-28 2001-06-12 Aventis Pharmaceuticals Products, Inc Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
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
US6894062B1 (en) * 2002-11-12 2005-05-17 Pfizer Inc. Quinoline derivatives
US20080015193A1 (en) 2006-06-20 2008-01-17 Mendoza Jose S Certain azoles exhibiting ATP-utilizing enzyme inhibitory activity, compositions, and uses thereof
US7592342B2 (en) 2007-05-10 2009-09-22 Smithkline Beecham Corporation Quinoxaline derivatives as PI3 kinase inhibitors
US20120101032A1 (en) 2010-10-22 2012-04-26 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
CN102827073A (zh) * 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN103814020B (zh) * 2011-06-17 2017-07-14 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
US9394297B2 (en) * 2012-02-28 2016-07-19 Amgen Inc. Amides as pim inhibitors
EP2847200B1 (en) 2012-04-26 2017-03-29 Bristol-Myers Squibb Company Imidazothiadiazole derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation
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
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
US9873670B2 (en) 2013-11-22 2018-01-23 University Of Kentucky Research Foundation Arylquinoline and analog compounds and use thereof to treat cancer
ES2929208T3 (es) 2015-02-26 2022-11-25 Univ Montreal Compuestos de imidazotiadiazol como inhibidores de PAR4
WO2017019828A1 (en) 2015-07-30 2017-02-02 Bristol-Myers Squibb Company Aryl substituted bicyclic heteroaryl compounds
ES2823127T3 (es) * 2016-07-14 2021-05-06 Bristol Myers Squibb Co Compuestos tricíclicos de quinolina y azaquinolina sustituidos con heteroarilo como inhibidores de PAR4
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
CN109689649B (zh) * 2016-07-14 2022-07-19 百时美施贵宝公司 经二环杂芳基取代的化合物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006508113A (ja) 2002-11-12 2006-03-09 ファイザー・プロダクツ・インク キノリン誘導体

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ALABASTER, C. T. et al.，2(1H)-QUINOLINONES WITH CARDIAC STIMULANT ACTIVITY. 1. SYNTHESIS AND BIOLOGICAL ACTIVITIES OF (SIX-MEMBERED HETEROARYL)-SUBSTITUTED DERIVATIVES，Journal of Medicinal Chemistry，1988年，Vol.31，No.10，p.2048-2056，http://dx.doi.org/10.1021/jm00118a034
Kuang, Rongze et al.，Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors，Bioorganic & Medicinal Chemistry Letters ，2007年，Vol.17，No.18，p.5150-5154

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US20190248771A1 (en) 2019-08-15
JP2019521153A (ja) 2019-07-25
CN109689642A (zh) 2019-04-26
EP3484874A1 (en) 2019-05-22
CN109689642B (zh) 2022-04-12
WO2018013772A1 (en) 2018-01-18
ES2805030T3 (es) 2021-02-10
US10815224B2 (en) 2020-10-27
EP3484874B1 (en) 2020-04-29
KR102492715B1 (ko) 2023-01-26
KR20190026905A (ko) 2019-03-13

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