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 (enExample
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
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    • 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
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    • 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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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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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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    • C07D401/14—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)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (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 (enExample) 2018-09-27
JP6633618B2 true JP6633618B2 (ja) 2020-01-22

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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
JP6779214B2 (ja) 2015-01-09 2020-11-04 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｒｏｃｋ阻害剤としての環状ウレア
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
EP3481816B1 (en) 2016-07-07 2020-06-24 Bristol-Myers Squibb Company Lactam, cyclic urea and carbamate, and triazolone derivatives as potent and selective rock inhibitors
ES2821877T3 (es) 2016-07-07 2021-04-28 Bristol Myers Squibb Co Espirolactamas como inhibidores de ROCK
JP7155102B2 (ja) 2016-07-07 2022-10-18 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縮合環尿素
EP3548468B1 (en) 2016-11-30 2020-09-16 Bristol-Myers Squibb Company Tricyclic rho kinase inhibitors
WO2018108156A1 (zh) * 2016-12-16 2018-06-21 成都先导药物开发有限公司 Rock抑制剂及其应用
JP7311228B2 (ja) * 2017-06-30 2023-07-19 ベイジン タイド ファーマシューティカル カンパニー リミテッド Ｒｈｏ－関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
CN110914257B (zh) 2017-07-12 2023-05-26 百时美施贵宝公司 作为rock抑制剂的螺庚基乙内酰脲
US12060341B2 (en) 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
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
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
WO2019014300A1 (en) 2017-07-12 2019-01-17 Bristol-Myers Squibb Company PHENYLACETAMIDES AS ROCK INHIBITORS
ES2937039T3 (es) 2017-11-03 2023-03-23 Bristol Myers Squibb Co Inhibidores diazaespiro de ROCK
CN112020496B (zh) 2018-04-18 2023-04-28 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
CN114555561B (zh) * 2019-10-18 2023-08-11 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的盐型、晶型及其制备方法
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
CN116438175B (zh) * 2020-11-11 2025-07-22 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
CA3238227A1 (en) 2021-11-11 2023-05-19 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation 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
EP0716650B1 (en) * 1993-09-03 1999-03-24 Smithkline Beecham Plc Indole and indoline derivatives as 5ht1d receptor antagonists
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
US6399656B1 (en) * 1998-07-28 2002-06-04 Smithkline Beecham Corporation Compounds and methods
EP1104754A1 (en) 1998-08-11 2001-06-06 Daiichi Pharmaceutical Co., Ltd. Novel sulfonyl derivatives
SK286641B6 (sk) * 1999-05-04 2009-03-05 Schering Corporation Piperazínové deriváty užitočné ako CCR5 antagonisty, farmaceutické prípravky s ich obsahom a ich použitie
IL151552A0 (en) * 2000-03-17 2003-04-10 Bristol Myers Squibb Pharma Co Cyclic beta-amino acid derivatives as inhibitors of matrix metalloproteases and tnf-alpha
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
DE60234264D1 (de) 2001-10-01 2009-12-17 Bristol Myers Squibb Co Spiro-hydantoin-verbindungen, die sich als entzündungshemmende mittel eignen
ATE416168T1 (de) 2002-02-15 2008-12-15 Glaxo Group Ltd Modulatoren des vanilloidrezeptors
TWI319387B (en) 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
EP1553089B1 (en) * 2002-07-30 2009-09-30 Banyu Pharmaceutical Co., Ltd. Antagonist of melanin-concentrating hormone receptor comprising benzimidazole derivative as active ingredient
CN1744899A (zh) 2002-12-13 2006-03-08 史密丝克莱恩比彻姆公司 作为ccr5拮抗剂的哌啶衍生物
US20060100245A1 (en) * 2002-12-19 2006-05-11 Neurogen Corporation Substituted biphenyl-4-carboxylic acid arylamide analogues
DE10306250A1 (de) 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
PT2476667E (pt) 2003-02-26 2014-09-18 Sugen Inc Compostos de aminoheteroarilo como inibidores da proteína quinase
US7432375B2 (en) 2003-03-06 2008-10-07 Eisai R & D Management Co., Ltd. JNK inhibitors
JP2007519754A (ja) * 2004-01-30 2007-07-19 スミスクライン ビーチャム コーポレーション 化合物
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
JP2008545660A (ja) * 2005-05-20 2008-12-18 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
KR101363278B1 (ko) 2005-06-27 2014-02-21 엑셀리시스 페이턴트 컴퍼니 엘엘씨 이미다졸계 ｌｘｒ 변조제
GB0514812D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
WO2007084667A2 (en) * 2006-01-19 2007-07-26 Osi Pharmaceutical, 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
CA2662112A1 (en) 2006-09-05 2008-03-13 Kyowa Hakko Kirin Co., Ltd. Imidazole derivatives and their use as cannabinoid type 2 (cb2) receptor modulators
EP2526948A1 (en) 2006-09-20 2012-11-28 Aerie Pharmaceuticals, Inc. 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
US8242129B2 (en) 2007-04-25 2012-08-14 Exelixis, Inc. 6-phenylpyrimidinones as PIM modulators
JP2010535733A (ja) 2007-08-07 2010-11-25 エフ．ホフマン−ラ ロシュ アーゲー Ｎｋ３受容体アンタゴニストとしてのピロリジンアリールエーテル
US8445686B2 (en) * 2007-08-27 2013-05-21 Abbvie Inc. 4-(4-pyridinyl)-benzamides and their use as rock activity modulators
CN102007101A (zh) 2007-11-30 2011-04-06 生物区科学管理控股有限公司 作为抗菌剂的四氢-异喹啉ppat抑制剂
WO2009072643A1 (en) 2007-12-03 2009-06-11 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound and use thereof
KR20110010781A (ko) 2008-06-16 2011-02-07 에프. 호프만-라 로슈 아게 Ｎｋ2 수용체 길항제로서의 피롤리딘 유도체
US20110118262A1 (en) 2008-07-08 2011-05-19 Boehringer Ingelheim International Gmbh Pyrrolidinyl and Piperidinyl Compounds Useful as NHE-1 Inhibitiors
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
CA2738870A1 (en) 2008-10-09 2010-04-15 F. Hoffmann-La Roche Ag Pyrrolidine n-benzyl derivatives
US8367679B2 (en) * 2008-12-09 2013-02-05 Merck Sharp & Dohme Corp. Biaryl carboxamides
EP2379524A1 (en) * 2008-12-18 2011-10-26 Boehringer Ingelheim International GmbH Serotonin 5-ht2b receptor inhibitors
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.
TW201109327A (en) 2009-05-28 2011-03-16 Otsuka Pharma Co Ltd Heterocyclic compound
TW201103904A (en) * 2009-06-11 2011-02-01 Hoffmann La Roche Janus kinase inhibitor compounds and methods
EP3406613A1 (en) 2009-10-16 2018-11-28 Melinta Therapeutics, Inc. Antimicrobial compounds and methods of making and using the same
NO2513053T3 (enExample) 2009-12-18 2018-03-03
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
SG10202010119TA (en) 2010-11-15 2020-11-27 Abbvie Inc NAMPT And Rock Inhibitors
BR112014002939A2 (pt) 2011-08-09 2017-03-01 Takeda Pharmaceuticals Co composto, medicamento, método para profilaxia ou tratamento de doença, a doença sendo esquizofrenia, alzheimer, parkinson ou huntington, uso do composto, e, método para inibir o lsd1
EP2838534A4 (en) 2012-04-12 2015-11-11 Univ Leland Stanford Junior SUBSTITUTED BENZAMIDES AND USES THEREOF
WO2013153539A1 (en) * 2012-04-13 2013-10-17 Glenmark Pharmaceuticals S.A. Tricyclic compounds as tec kinase inhibitors
CA2877589C (en) 2012-06-27 2019-11-26 4Sc Ag Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and cns disorders
KR102071095B1 (ko) * 2012-07-03 2020-01-29 3-브이 바이오사이언시스, 인코포레이티드 지질 합성의 헤테로사이클릭 조절인자
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
RS63503B1 (sr) 2012-10-05 2022-09-30 Kadmon Corporation Llc Inhibitori rho kinaze
LT3418281T (lt) * 2012-12-07 2021-01-11 Vertex Pharmaceuticals Inc. Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui
ES2684776T3 (es) 2013-01-18 2018-10-04 Bristol-Myers Squibb Company Ftalazinonas e isoquinolinonas como inhibidores de ROCK
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
EP2961746B1 (en) 2013-02-28 2018-01-03 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors

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CN107108581A (zh) 2017-08-29
US10112939B2 (en) 2018-10-30
CN107108581B (zh) 2020-06-23
US20170226105A1 (en) 2017-08-10
EP3183248B1 (en) 2020-11-11
JP2017524026A (ja) 2017-08-24

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