JP6633618B2 - 強力なｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体 - Google Patents

強力なｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体 Download PDF

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JP6633618B2
JP6633618B2 JP2017510314A JP2017510314A JP6633618B2 JP 6633618 B2 JP6633618 B2 JP 6633618B2 JP 2017510314 A JP2017510314 A JP 2017510314A JP 2017510314 A JP2017510314 A JP 2017510314A JP 6633618 B2 JP6633618 B2 JP 6633618B2
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substituted
alkyl
methoxy
pyrazol
benzoyl
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JP2017524026A5 (https=
JP2017524026A (ja
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ジルン・フー
ドリー・エフ・シトコフ
ミミ・エル・クワン
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Bristol Myers Squibb Co
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • 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
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2017510314A 2014-08-21 2015-08-20 強力なｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体 Active JP6633618B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462040044P 2014-08-21 2014-08-21
US62/040,044 2014-08-21
PCT/US2015/046032 WO2016028971A1 (en) 2014-08-21 2015-08-20 Tied-back benzamide derivatives as potent rock inhibitors

Publications (3)

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JP2017524026A JP2017524026A (ja) 2017-08-24
JP2017524026A5 JP2017524026A5 (https=) 2018-09-27
JP6633618B2 true JP6633618B2 (ja) 2020-01-22

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US (1) US10112939B2 (https=)
EP (1) EP3183248B1 (https=)
JP (1) JP6633618B2 (https=)
CN (1) CN107108581B (https=)
ES (1) ES2838573T3 (https=)
WO (1) WO2016028971A1 (https=)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10123993B2 (en) 2015-01-09 2018-11-13 Bristol-Myers Squibb Company Cyclic ureas as inhibitors of rock
ES2730112T3 (es) 2015-03-09 2019-11-08 Bristol Myers Squibb Co Lactamas como inhibidores de ROCK
CN106924254A (zh) * 2015-12-31 2017-07-07 中国医学科学院药物研究所 黄连碱在制备预防和/或治疗系统性红斑狼疮及其并发症药物中的应用
TWI730032B (zh) 2016-01-13 2021-06-11 美商必治妥美雅史谷比公司 作為ｒｏｃｋ抑制劑之螺庚烷水楊酸醯胺及相關化合物
WO2017205709A1 (en) 2016-05-27 2017-11-30 Bristol-Myers Squibb Company Triazolones and tetrazolones as inhibitors of rock
ES2829550T3 (es) 2016-07-07 2021-06-01 Bristol Myers Squibb Co Ureas cíclicas espiro-condensadas como inhibidores de ROCK
JP7113810B2 (ja) 2016-07-07 2022-08-05 ブリストル－マイヤーズ スクイブ カンパニー Ｒｏｃｋ阻害剤としてのスピロラクタム
JP6903731B2 (ja) 2016-07-07 2021-07-14 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 強力で選択的なｒｏｃｋ阻害剤としてのラクタム、環状尿素、およびカルバメート、およびトリアゾロン誘導体
KR102511441B1 (ko) 2016-11-30 2023-03-16 브리스톨-마이어스 스큅 컴퍼니 트리시클릭 Rho 키나제 억제제
CN108203433B (zh) * 2016-12-16 2020-07-03 成都先导药物开发股份有限公司 一种rock抑制剂及其应用
CN110582489B (zh) * 2017-06-30 2023-10-27 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
US11306081B2 (en) 2017-07-12 2022-04-19 Bristol-Myers Squibb Company Phenylacetamides as inhibitors of rock
JP7234201B2 (ja) 2017-07-12 2023-03-07 ブリストル－マイヤーズ スクイブ カンパニー 心不全の治療のためのｒｏｃｋの５員アミノヘテロ環および５，６－または６，６員二環式アミノヘテロ環の阻害剤
US11447487B2 (en) 2017-07-12 2022-09-20 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as rock inhibitors
US12060341B2 (en) 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
TW201908293A (zh) 2017-07-12 2019-03-01 美商必治妥美雅史谷比公司 作為rock抑制劑之5員及雙環雜環醯胺
EP3704121B1 (en) 2017-11-03 2022-12-21 Bristol-Myers Squibb Company Diazaspiro rock inhibitors
WO2019201297A1 (zh) 2018-04-18 2019-10-24 南京明德新药研发有限公司 作为rho激酶抑制剂的苯并吡唑类化合物
US11702400B2 (en) 2019-10-18 2023-07-18 Medshine Discovery Inc. Salt types, crystal forms, and preparation methods for benzopyrazole compounds as RHO kinase inhibitors
CN114262322B (zh) * 2020-09-16 2026-01-06 中国科学院上海有机化学研究所 一类细胞程序性坏死抑制剂及其制备方法和用途
WO2022100614A1 (zh) * 2020-11-11 2022-05-19 南京明德新药研发有限公司 苯并脲环衍生物及其制备方法和应用
EP4431596A4 (en) 2021-11-11 2026-01-14 The Doshisha CRYOCONSERVATION PREPARATION FOR CORNIAL ENDOTHELIAL CELLS AND PROCESS FOR PRODUCING SAID CRYOCONSERVATION PREPARATION

Family Cites Families (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0259559A (ja) 1988-08-23 1990-02-28 Mitsubishi Kasei Corp ピリドン誘導体又はその塩類
GB9119932D0 (en) * 1991-09-18 1991-10-30 Glaxo Group Ltd Chemical compounds
WO1995006637A1 (en) 1993-09-03 1995-03-09 Smithkline Beecham Plc Indole and indoline derivatives as 5ht1d receptor antagonists
WO1995011243A1 (en) 1993-10-19 1995-04-27 Smithkline Beecham Plc Benzanilide derivatives as 5ht-1d receptor antagonists
CA2338697A1 (en) * 1998-07-28 2000-02-10 Smithkline Beecham Corporation Compounds and methods
US6747023B1 (en) 1998-08-11 2004-06-08 Daiichi Pharmaceutical Co., Ltd. Sulfonyl derivatives
CA2371583C (en) * 1999-05-04 2005-09-13 Schering Corporation Piperazine derivatives useful as ccr5 antagonists
JP2003528072A (ja) 2000-03-17 2003-09-24 ブリストル−マイヤーズ スクイブ ファーマ カンパニー マトリックスメタロプロテアーゼおよびＴＮＦ−αの阻害剤としての環状β−アミノ酸誘導体
GB2361003A (en) 2000-04-07 2001-10-10 Astrazeneca Ab Novel compounds
US20020045613A1 (en) 2000-04-27 2002-04-18 Heinz Pauls 1-aroyl-piperidinyl benzamidines
TWI243164B (en) * 2001-02-13 2005-11-11 Aventis Pharma Gmbh Acylated indanyl amines and their use as pharmaceuticals
CA2462112A1 (en) 2001-10-01 2003-04-10 Bristol-Myers Squibb Company Spiro-hydantoin compounds useful as anti-inflammatory agents
ES2316777T3 (es) 2002-02-15 2009-04-16 Glaxo Group Limited Moduladores de receptores vainilloides.
TWI319387B (en) * 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
CA2494102A1 (en) * 2002-07-30 2004-02-05 Banyu Pharmaceutical Co., Ltd. Antagonist of melanin-concentrating hormone receptor comprising benzimidazole derivative as active ingredient
BR0317230A (pt) 2002-12-13 2005-10-25 Smithkline Beecham Corp Composto, composição, métodos de antagonizar uma atividade do receptor de quimiocina ccr-5, e de tratar uma infecção viral em um paciente, e, uso de um composto
WO2004056774A2 (en) * 2002-12-19 2004-07-08 Neurogen Corporation Substituted biphenyl-4-carboxylic acid arylamide analogues as capsaicin receptor modulators
DE10306250A1 (de) * 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CA2517256C (en) 2003-02-26 2013-04-30 Sugen, Inc. Aminoheteroaryl compounds as protein kinase inhibitors
JP4787150B2 (ja) 2003-03-06 2011-10-05 エーザイ・アール・アンド・ディー・マネジメント株式会社 Ｊｎｋ阻害剤
WO2005074643A2 (en) * 2004-01-30 2005-08-18 Smithkline Beecham Corporation Benzamide compounds useful as rock inhibitors
SI1735278T1 (sl) * 2004-04-01 2010-05-31 Lilly Co Eli Agenti histamin h receptorja priprava in terapevtska uporaba
WO2006123725A1 (ja) 2005-05-19 2006-11-23 Astellas Pharma Inc. ピロリジン誘導体またはその塩
WO2006127587A1 (en) 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
US8703805B2 (en) 2005-06-27 2014-04-22 Exelixis Patent Company Llc Modulators of LXR
GB0514812D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
US20070208053A1 (en) 2006-01-19 2007-09-06 Arnold Lee D Fused heterobicyclic kinase inhibitors
TW200808751A (en) 2006-04-13 2008-02-16 Astrazeneca Ab New compounds
US7601716B2 (en) 2006-05-01 2009-10-13 Cephalon, Inc. Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors
AU2007292155B2 (en) 2006-09-05 2012-11-01 Kyowa Kirin Co., Ltd. Imidazole derivative
WO2008036540A2 (en) 2006-09-20 2008-03-27 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
CL2007003874A1 (es) 2007-01-03 2008-05-16 Boehringer Ingelheim Int Compuestos derivados de benzamida; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar enfermedades cardiovasculares, hipertension, aterosclerosis, reestenosis, ictus, insuficiencia cardiaca, lesion isquemica, hipertensio
EP2074103A1 (en) 2007-04-25 2009-07-01 Exelixis, Inc. 6-phenylpyrimidinones as pim modulators
BRPI0815658A2 (pt) 2007-08-07 2015-02-18 Hoffmann La Roche Aril-éter pirrolidina como antagonistas do receptor nk3
US8445686B2 (en) * 2007-08-27 2013-05-21 Abbvie Inc. 4-(4-pyridinyl)-benzamides and their use as rock activity modulators
AU2008334075A1 (en) 2007-11-30 2009-06-11 Biota Scientific Management Pty Ltd Tetrahydro-isoquinoline PPAT inhibitors as antibacterial agents
TW200930713A (en) * 2007-12-03 2009-07-16 Takeda Pharmaceutical Nitrogen-containing heterocyclic compound and use thereof
CN102066321A (zh) 2008-06-16 2011-05-18 弗·哈夫曼-拉罗切有限公司 作为nk2受体拮抗剂的吡咯烷衍生物
JP2011527677A (ja) 2008-07-08 2011-11-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｎｈｅ−１阻害剤として有用なピロリジニル及びピペリジニル化合物
CA2735204C (en) 2008-08-25 2017-06-20 Boehringer Ingelheim International Gmbh Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use
EP2331500A1 (en) 2008-10-09 2011-06-15 F. Hoffmann-La Roche AG Pyrrolidine n-benzyl derivatives
WO2010077624A1 (en) 2008-12-09 2010-07-08 Merck Sharp & Dohme Corp. Biaryl carboxamides
JP2012512877A (ja) * 2008-12-18 2012-06-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング セロトニン５−ｈｔ２ｂ受容体阻害剤
CA2747961C (en) 2009-01-30 2016-11-08 F. Hoffmann-La Roche Ag Piperidine derivatives as nk3 receptor antagonists
US8324250B2 (en) 2009-03-19 2012-12-04 Hoffmann-La Roche Inc. Piperidine derivatives as NK3 receptor antagonists
AR076332A1 (es) 2009-04-21 2011-06-01 Boehringer Ingelheim Int Derivados heterociclicos de 5-alquinil-piridinas, composiciones farmaceuticas que los comprenden y uso de los mismos para el tratamiento y/o prevencion del cancer, procesos inflamatorios, autoinmunes, y/o infecciones.
AR076928A1 (es) 2009-05-28 2011-07-20 Otsuka Pharma Co Ltd Derivados de 3h-pirido[4, 3-d]pirimidin-4-ona, un metodo para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la manufactura de un medicamento para el tratamiento o prevencion de enfermedades relacionadas con el estres.
AR077033A1 (es) * 2009-06-11 2011-07-27 Hoffmann La Roche Compuestos inhibidores de las quinasas de janus y su uso en el tratamiento de enfermedades inmunologicas
EA201270566A1 (ru) 2009-10-16 2012-11-30 Риб-Экс Фармасьютикалз, Инк. Противомикробные соединения и способы их получения и применения
WO2011073376A1 (en) * 2009-12-18 2011-06-23 Euroscreen S.A. Pyrrolidine or thiazolidine carboxylic acid derivatives, pharmaceutical composition and methods for use in treating metabolic disordersas as agonists of g- protein coupled receptor 43 (gpr43)
US8633183B2 (en) 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
US8507535B2 (en) 2010-07-07 2013-08-13 Hoffmann-La Roche Inc. Methyl-pyrrolidine ether derivatives
US9079880B2 (en) 2010-07-07 2015-07-14 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
AU2011329233A1 (en) 2010-11-15 2013-05-23 Abbvie Deutschland Gmbh & Co Kg NAMPT and ROCK inhibitors
KR20140052018A (ko) 2011-08-09 2014-05-02 다케다 야쿠힌 고교 가부시키가이샤 시클로프로판아민 화합물
US9296732B2 (en) 2012-04-12 2016-03-29 The Board Of Trustees Of The Leland Stanford Junior University Substituted benzamides and their uses
WO2013153539A1 (en) 2012-04-13 2013-10-17 Glenmark Pharmaceuticals S.A. Tricyclic compounds as tec kinase inhibitors
AU2013283318B2 (en) 2012-06-27 2017-11-23 4Sc Ag Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and CNS disorders
NZ703162A (en) * 2012-07-03 2017-05-26 3-V Biosciences Inc Heterocyclic modulators of lipid synthesis
EP2687528A1 (en) * 2012-07-17 2014-01-22 Ares Trading S.A. Fused triazole derivatives as gamma secretase modulators
CN103664878A (zh) 2012-09-12 2014-03-26 山东亨利医药科技有限责任公司 杂芳环及其衍生物类酪氨酸激酶抑制剂
CN113620933A (zh) 2012-10-05 2021-11-09 卡德门企业有限公司 Rho激酶抑制剂
SI2941432T1 (en) * 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
JP6488239B2 (ja) 2013-01-18 2019-03-20 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
WO2014134391A1 (en) 2013-02-28 2014-09-04 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors

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CN107108581A (zh) 2017-08-29
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