CN107108581B - 作为强效rock抑制剂的回接苯甲酰胺衍生物 - Google Patents

作为强效rock抑制剂的回接苯甲酰胺衍生物 Download PDF

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CN107108581B
CN107108581B CN201580044710.7A CN201580044710A CN107108581B CN 107108581 B CN107108581 B CN 107108581B CN 201580044710 A CN201580044710 A CN 201580044710A CN 107108581 B CN107108581 B CN 107108581B
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substituted
methoxy
pyrazol
benzoyl
independently selected
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CN107108581A (zh
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胡子伦
D.F.西特科夫
陈丽芬
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Bristol Myers Squibb Co
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  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201580044710.7A 2014-08-21 2015-08-20 作为强效rock抑制剂的回接苯甲酰胺衍生物 Active CN107108581B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462040044P 2014-08-21 2014-08-21
US62/040044 2014-08-21
PCT/US2015/046032 WO2016028971A1 (en) 2014-08-21 2015-08-20 Tied-back benzamide derivatives as potent rock inhibitors

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CN107108581A CN107108581A (zh) 2017-08-29
CN107108581B true CN107108581B (zh) 2020-06-23

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

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016112236A1 (en) 2015-01-09 2016-07-14 Bristol-Myers Squibb Company Cyclic ureas as inhibitors of rock
WO2016144936A1 (en) 2015-03-09 2016-09-15 Bristol-Myers Squibb Company Lactams as inhibitors of 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
AR107354A1 (es) 2016-01-13 2018-04-18 Bristol Myers Squibb Co Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock
JP6987792B2 (ja) 2016-05-27 2022-01-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Ｒｏｃｋ阻害剤としてのトリアゾロンおよびテトラゾロン
CN110049977B (zh) 2016-07-07 2022-01-18 百时美施贵宝公司 作为强效和选择性rock抑制剂的内酰胺、环状脲和氨基甲酸酯及三唑酮衍生物
ES2821877T3 (es) 2016-07-07 2021-04-28 Bristol Myers Squibb Co Espirolactamas como inhibidores de ROCK
ES2829550T3 (es) 2016-07-07 2021-06-01 Bristol Myers Squibb Co Ureas cíclicas espiro-condensadas como inhibidores de ROCK
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
CA3063616A1 (en) * 2017-06-30 2019-12-06 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
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
JP7206253B2 (ja) 2017-07-12 2023-01-17 ブリストル－マイヤーズ スクイブ カンパニー Ｒｏｃｋ阻害剤としてのフェニルアセトアミド
US12060341B2 (en) 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
JP7313331B2 (ja) 2017-07-12 2023-07-24 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ヘプタニルヒダントイン
KR102680160B1 (ko) 2017-07-12 2024-06-28 브리스톨-마이어스 스큅 컴퍼니 심부전의 치료를 위한 rock의 5원-아미노헤테로사이클 및 5,6- 또는 6,6-원 비시클릭 아미노헤테로시클릭 억제제
WO2019089868A1 (en) 2017-11-03 2019-05-09 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
JP7252417B2 (ja) * 2019-10-18 2023-04-04 メッドシャイン ディスカバリー インコーポレイテッド Ｒｈｏキナーゼ阻害剤としてのベンゾピラゾール化合物の塩形、結晶形及びその製造方法
CN114262322A (zh) * 2020-09-16 2022-04-01 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
WO2023085369A1 (ja) 2021-11-11 2023-05-19 学校法人同志社 角膜内皮細胞の凍結保存製剤およびその製造法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010080357A1 (en) * 2008-12-18 2010-07-15 Boehringer Ingelheim International Gmbh Serotonin 5-ht2b receptor inhibitors
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)

Family Cites Families (64)

* 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
DE69417427T2 (de) * 1993-09-03 1999-11-25 Smithkline Beecham P.L.C., Brentford Indol- und indolin-derivate als 5ht1d rezeptor antagonisten
JPH09503773A (ja) 1993-10-19 1997-04-15 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー ５ｈｔ−１ｄレセプター拮抗剤用のベンズアニリド誘導体
WO2000006085A2 (en) * 1998-07-28 2000-02-10 Smithkline Beecham Corporation Compounds and methods
EP1104754A1 (en) 1998-08-11 2001-06-06 Daiichi Pharmaceutical Co., Ltd. Novel sulfonyl derivatives
CZ20013940A3 (cs) * 1999-05-04 2002-04-17 Schering Corporation Piperazinové deriváty uľitečné jako CCR5 antagonisté
MXPA02009020A (es) * 2000-03-17 2003-02-12 Du Pont Pharm Co Derivados de beta-aminoacidos ciclicos como inhibidores de las metaloproteasas de matriz y factor de necrosis de tumor alfa.
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
BR0213025A (pt) 2001-10-01 2004-10-05 Bristol Myers Squibb Co Compostos de espiro-hidantoìna úteis como agentes antiinflamatórios
JP2005526723A (ja) 2002-02-15 2005-09-08 グラクソ　グループ　リミテッド バニロイド受容体モジュレーター
TWI319387B (en) * 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
DE60329513D1 (de) 2002-07-30 2009-11-12 Banyu Pharma Co Ltd Antagonist des melanin-concentrating-hormone-rezeptors, enthaltend ein benzimidazolderivat als wirkstoff
EP1569646A2 (en) 2002-12-13 2005-09-07 Smithkline Beecham Corporation Piperidine derivatives as ccr5 antagonists
CA2510471A1 (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
AU2004215428B2 (en) 2003-02-26 2009-08-27 Sugen LLC 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
EP1713775A4 (en) * 2004-01-30 2009-08-12 Smithkline Beecham Corp CHEMICAL COMPOUNDS
CA2561628C (en) * 2004-04-01 2012-05-08 Eli Lilly And Company Histamine h3 receptor agents, preparation and therapeutic uses
EP1882684B1 (en) 2005-05-19 2014-12-10 Astellas Pharma Inc. Pyrrolidine derivative or salt thereof
ES2380795T3 (es) * 2005-05-20 2012-05-18 Vertex Pharmaceuticals, Inc. Pirrolopiridinas útiles como inhibidores de proteínas quinasas
US8569352B2 (en) 2005-06-27 2013-10-29 Exelixis Patent Company Llc Imidazole based LXR modulators
GB0514812D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
EP1979353A2 (en) * 2006-01-19 2008-10-15 OSI Pharmaceuticals, Inc. 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
PT2090570E (pt) 2006-09-05 2011-12-29 Kyowa Hakko Kirin Co Ltd Derivado de imidazole
CA2664335C (en) 2006-09-20 2014-12-02 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
CA2685106A1 (en) 2007-04-25 2008-11-06 Exelixis, Inc. 6-phenylpyrimidinones as pim modulators
ES2367464T3 (es) 2007-08-07 2011-11-03 F. Hoffmann-La Roche Ag Pirrolidina-aril-éteres como antagonistas de receptor de nk3.
EP2193119B1 (en) 2007-08-27 2014-01-01 Abbvie Deutschland GmbH & Co. KG 4-(4-pyridinyl)-benzamides and their use as rock activity modulators
CA2707445A1 (en) 2007-11-30 2009-06-11 Biota Scientific Management Pty Ltd Tetrahydro-isoquinoline ppat inhibitors as antibacterial agents
PE20091093A1 (es) 2007-12-03 2009-08-25 Takeda Pharmaceutical Compuesto heterociclico que contiene nitrogeno y su uso
MX2010013311A (es) 2008-06-16 2010-12-21 Hoffmann La Roche Derivados de pirrolidina como antagonistas del receptor de nk2.
US20110118262A1 (en) 2008-07-08 2011-05-19 Boehringer Ingelheim International Gmbh Pyrrolidinyl and Piperidinyl Compounds Useful as NHE-1 Inhibitiors
US8609690B2 (en) 2008-08-25 2013-12-17 Boehringer Ingelheim International Gmbh Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use
MX2011003312A (es) 2008-10-09 2011-04-26 Hoffmann La Roche Derivados de pirrolidina n-bencilo.
US8367679B2 (en) * 2008-12-09 2013-02-05 Merck Sharp & Dohme Corp. Biaryl carboxamides
EP2391615B1 (en) 2009-01-30 2013-01-16 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.
WO2010137738A1 (en) 2009-05-28 2010-12-02 Otsuka Pharmaceutical Co., Ltd. Heterocyclic compounds for the treatment of stress-related conditions
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
DK2488525T3 (en) 2009-10-16 2018-08-06 Melinta Therapeutics Inc ANTIMICROBIAL COMPOUNDS AND PROCEDURES FOR PREPARING AND USING THEREOF
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
UY33726A (es) 2010-11-15 2012-06-29 Abbott Lab Inhibidores de nampt y rock
UA114406C2 (uk) * 2011-08-09 2017-06-12 Такеда Фармасьютікал Компані Лімітед Похідні циклопропанаміну як інгібітори lsd1
SG11201406518XA (en) 2012-04-12 2014-11-27 Univ Leland Stanford Junior Substituted benzamides and their uses
WO2013153539A1 (en) 2012-04-13 2013-10-17 Glenmark Pharmaceuticals S.A. Tricyclic compounds as tec kinase inhibitors
EA029718B1 (ru) 2012-06-27 2018-05-31 4-Эс-Си Дискавери Гмбх Бифтордиоксалан-аминобензимидазольные ингибиторы киназы для лечения рака, аутоиммунного воспаления и нарушений цнс
JP6109934B2 (ja) * 2012-07-03 2017-04-05 ３−ブイ・バイオサイエンシーズ・インコーポレイテッド３−Ｖ Ｂｉｏｓｃｉｅｎｃｅｓ，Ｉｎｃ． 脂質合成の複素環モジュレーター
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
EP4116293A3 (en) 2012-10-05 2023-03-29 Kadmon Corporation, LLC Rho kinase inhibitors
PL3808749T3 (pl) * 2012-12-07 2023-07-10 Vertex Pharmaceuticals Incorporated Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych
CA2898440A1 (en) 2013-01-18 2014-07-24 Bristol-Myers Squibb Company Phthalazinones and isoquinolinones as rock inhibitors
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
JP6423372B2 (ja) 2013-02-28 2018-11-14 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 強力なｒｏｃｋ１およびｒｏｃｋ２阻害剤としてのフェニルピラゾール誘導体

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010080357A1 (en) * 2008-12-18 2010-07-15 Boehringer Ingelheim International Gmbh Serotonin 5-ht2b receptor inhibitors
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)

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
REGISTRY[Online];Columbus,Ohio,US;《REGISTRY》;20120130;1354720-58-3,1354719-49-5 *

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EP3183248A1 (en) 2017-06-28
US10112939B2 (en) 2018-10-30
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