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

Info

Publication number
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
Authority
CN
China
Prior art keywords
substituted
methoxy
pyrazol
benzoyl
independently selected
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201580044710.7A
Other languages
English (en)
Chinese (zh)
Other versions
CN107108581A (zh
Inventor
胡子伦
D.F.西特科夫
陈丽芬
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN107108581A publication Critical patent/CN107108581A/zh
Application granted granted Critical
Publication of CN107108581B publication Critical patent/CN107108581B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • 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)
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

Publications (2)

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

Family

ID=54011128

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580044710.7A Active CN107108581B (zh) 2014-08-21 2015-08-20 作为强效rock抑制剂的回接苯甲酰胺衍生物

Country Status (6)

Country Link
US (1) US10112939B2 (OSRAM)
EP (1) EP3183248B1 (OSRAM)
JP (1) JP6633618B2 (OSRAM)
CN (1) CN107108581B (OSRAM)
ES (1) ES2838573T3 (OSRAM)
WO (1) WO2016028971A1 (OSRAM)

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
US10112929B2 (en) 2015-03-09 2018-10-30 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
WO2017205709A1 (en) 2016-05-27 2017-11-30 Bristol-Myers Squibb Company Triazolones and tetrazolones as inhibitors of rock
WO2018009625A1 (en) 2016-07-07 2018-01-11 Bristol-Myers Squibb Company Spirolactams as inhibitors of 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
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
ES2829400T3 (es) 2016-11-30 2021-05-31 Bristol Myers Squibb Co Inhibidores tricíclicos de Rho cinasa
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
US12060341B2 (en) 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
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
WO2019014300A1 (en) 2017-07-12 2019-01-17 Bristol-Myers Squibb Company PHENYLACETAMIDES AS ROCK INHIBITORS
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
CN111278825B (zh) 2017-11-03 2023-05-02 百时美施贵宝公司 二氮杂螺rock抑制剂
EP3782987B1 (en) 2018-04-18 2025-04-02 Medshine Discovery Inc. Benzopyrazole compound used as rho kinase inhibitor
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
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
US20250000083A1 (en) 2021-11-11 2025-01-02 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation

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
US5696122A (en) * 1993-09-03 1997-12-09 Smithkline Beecham P.L.C. 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
CA2338697A1 (en) * 1998-07-28 2000-02-10 Smithkline Beecham Corporation Compounds and methods
CA2340100A1 (en) 1998-08-11 2000-02-24 Daiichi Pharmaceutical Co., Ltd. Novel sulfonyl derivatives
ES2244437T3 (es) 1999-05-04 2005-12-16 Schering Corporation Derivados de piperazina utiles como antagonistas de ccr5.
HUP0300850A2 (hu) 2000-03-17 2003-07-28 Bristol-Myers Squibb Pharma Company Gyűrűs béta-aminosav-származékok mint mátrix metalloproteázok és a TNF-alfa inhibitorok és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
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
CN1596253A (zh) 2001-10-01 2005-03-16 布里斯托尔-迈尔斯斯奎布公司 用作抗炎药的螺-乙内酰脲化合物
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
US7541477B2 (en) * 2002-07-30 2009-06-02 Banyu Pharmaceutical Co., Ltd. Antagonists to melanin-concentrating hormone receptor comprising benzimidazole derivative as active ingredient
CA2509711A1 (en) 2002-12-13 2004-07-01 Smithkline Beecham Corporation Piperidine derivatives as ccr5 antagonists
EP1575918A2 (en) * 2002-12-19 2005-09-21 Neurogen Corporation Substituted biaryl-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
WO2004076412A2 (en) 2003-02-26 2004-09-10 Sugen, Inc. Aminoheteroaryl compounds as protein kinase inhibitors
US7432375B2 (en) 2003-03-06 2008-10-07 Eisai R & D Management Co., Ltd. JNK inhibitors
EP1713775A4 (en) * 2004-01-30 2009-08-12 Smithkline Beecham Corp CHEMICAL COMPOUNDS
ATE454372T1 (de) * 2004-04-01 2010-01-15 Lilly Co Eli Am histamin-h3-rezeptor wirksame mittel, herstellung und therapeutische anwendungen
PL1882684T3 (pl) 2005-05-19 2015-08-31 Astellas Pharma Inc Pochodna pirolidyny albo jej sól
US8921376B2 (en) 2005-05-20 2014-12-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
WO2007002559A1 (en) 2005-06-27 2007-01-04 Exelixis, Inc. Pyrazole based lxr modulators
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
TWI386405B (zh) 2006-09-05 2013-02-21 咪唑衍生物
ES2729424T3 (es) 2006-09-20 2019-11-04 Aerie Pharmaceuticals Inc Inhibidores de Rho cinasa
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
JP2010525062A (ja) 2007-04-25 2010-07-22 エグゼリクシス, インコーポレイテッド Pimモジュレーターとしてのピリミジノン類
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
ES2453950T3 (es) * 2007-08-27 2014-04-09 AbbVie Deutschland GmbH & Co. KG 4-(4-Piridinil)-benzamidas y su uso como moduladores de la actividad de ROCK
JP2011518109A (ja) 2007-11-30 2011-06-23 ビオタ サイエンティフィック マネージメント ピーティーワイ リミテッド 抗菌剤としてのテトラヒドロ−イソキノリンppat阻害剤
AR069526A1 (es) * 2007-12-03 2010-01-27 Takeda Pharmaceutical Compuesto heterociclico que contiene nitrogeno y su uso
WO2009153179A1 (en) 2008-06-16 2009-12-23 F. Hoffmann-La Roche Ag Pyrrolidine derivatives as nk2 receptor antagonists
EP2321274A1 (en) 2008-07-08 2011-05-18 Boehringer Ingelheim International GmbH Pyrrolidinyl and piperidinyl compounds useful as nhe-1 inhibitors
EP2318403B1 (en) 2008-08-25 2015-12-23 Boehringer Ingelheim International GmbH Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use
WO2010040663A1 (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
AU2010209825A1 (en) 2009-01-30 2011-08-11 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.
US9206173B2 (en) * 2009-05-28 2015-12-08 Otsuka Pharmaceutical Co., Ltd. Heterocyclic compounds for the treatment of stress-related conditions
TW201103904A (en) * 2009-06-11 2011-02-01 Hoffmann La Roche Janus kinase inhibitor compounds and methods
WO2011047319A2 (en) 2009-10-16 2011-04-21 Rib-X Pharmaceuticals, Inc. Antimicrobial compounds and methods of making and using the same
US8633183B2 (en) 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
US9079880B2 (en) 2010-07-07 2015-07-14 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
US8507535B2 (en) 2010-07-07 2013-08-13 Hoffmann-La Roche Inc. Methyl-pyrrolidine ether derivatives
PE20140913A1 (es) 2010-11-15 2014-08-22 Abbvie Inc Inhibidores de nampt y rock
JP6111195B2 (ja) * 2011-08-09 2017-04-05 武田薬品工業株式会社 シクロプロパンアミン化合物
CA2873701A1 (en) 2012-04-12 2013-10-17 Auckland Uniservices Limited Substituted benzamides and their uses
WO2013153539A1 (en) * 2012-04-13 2013-10-17 Glenmark Pharmaceuticals S.A. Tricyclic compounds as tec kinase inhibitors
JP6272846B2 (ja) 2012-06-27 2018-01-31 4エスツェー ディスカバリー ゲゼルシャフト ミット ベシュレンクテル ハフツング 癌、自己免疫性炎症及びcns疾患の処置のためのビフルオロジオキサラン−アミノ−ベンゾイミダゾールキナーゼ阻害剤
BR112015000106B1 (pt) * 2012-07-03 2022-02-22 Sagimet Biosciences Inc Moduladores heterocíclicos de síntese de lipídio, composição farmacêutica e uso dos referidos moduladores
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
CA2926478C (en) 2012-10-05 2022-05-24 Kadmon Corporation, Llc Rho kinase inhibitors
TR201807740T4 (tr) * 2012-12-07 2018-06-21 Vertex Pharma ATR kinaz inhibitörü olarak 2-amino-6-fluoro-n-(5-fluoro-4-(4-(4-(oksetan-3-il)piperazin-1-karbonil)piperidin-1-il)piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamid.
US9926282B2 (en) 2013-01-18 2018-03-27 Bristol-Myers Squibb Company Phthalazinones and isoquinolinones as rock inhibitors
TW201444798A (zh) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物
US9828345B2 (en) 2013-02-28 2017-11-28 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors

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 *

Also Published As

Publication number Publication date
JP6633618B2 (ja) 2020-01-22
US20170226105A1 (en) 2017-08-10
EP3183248A1 (en) 2017-06-28
ES2838573T3 (es) 2021-07-02
CN107108581A (zh) 2017-08-29
EP3183248B1 (en) 2020-11-11
WO2016028971A1 (en) 2016-02-25
JP2017524026A (ja) 2017-08-24
US10112939B2 (en) 2018-10-30

Similar Documents

Publication Publication Date Title
CN107108581B (zh) 作为强效rock抑制剂的回接苯甲酰胺衍生物
CN105073741B (zh) 作为rock抑制剂的酞嗪酮及异喹啉酮
CN105102448B (zh) 作为rock1和rock2抑制剂的苯基吡唑衍生物
CN109153663B (zh) 作为rock抑制剂的三唑酮类化合物和四唑酮类化合物
CN105358547B (zh) 作为rock1和rock2抑制剂的苯基吡唑衍生物
US11884661B2 (en) 3-substituted propionic acids as αV integrin inhibitors
EP3538526B1 (en) Cyclobutane- and azetidine-containing mono and spirocyclic compounds as alpha v integrin inhibitors
CN105492444B (zh) 作为rock抑制剂的三环吡啶-甲酰胺衍生物
CN107406426B (zh) 作为rock抑制剂的环状脲类
CN105518005B (zh) 作为rock抑制剂的三环吡啶-甲酰胺衍生物
CN110869361A (zh) 用于治疗心力衰竭的rock的五元氨基杂环和5,6元或6,6元双环氨基杂环抑制剂
EP3475289A1 (en) Macrocyclic inhibitors of myeloperoxidase
HK40009959B (en) 3-substituted propionic acids as alpha v integrin inhibitors
HK40009959A (en) 3-substituted propionic acids as alpha v integrin inhibitors

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant