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

Info

Publication number
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
Authority
JP
Japan
Prior art keywords
substituted
alkyl
methoxy
pyrazol
benzoyl
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
JP2017510314A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017524026A (ja
JP2017524026A5 (enExample
Inventor
ジルン・フー
ドリー・エフ・シトコフ
ミミ・エル・クワン
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 JP2017524026A publication Critical patent/JP2017524026A/ja
Publication of JP2017524026A5 publication Critical patent/JP2017524026A5/ja
Application granted granted Critical
Publication of JP6633618B2 publication Critical patent/JP6633618B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • C07D403/12—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • 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
    • C07D413/14—Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (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)

Publication Number Publication Date
JP2017524026A JP2017524026A (ja) 2017-08-24
JP2017524026A5 JP2017524026A5 (enExample) 2018-09-27
JP6633618B2 true JP6633618B2 (ja) 2020-01-22

Family

ID=54011128

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2017510314A Active JP6633618B2 (ja) 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

Country Status (6)

Country Link
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
ES2815681T3 (es) 2015-01-09 2021-03-30 Bristol Myers Squibb Co Ureas cíclicas como inhibidores de ROCK
TW201706265A (zh) 2015-03-09 2017-02-16 必治妥美雅史谷比公司 做為Ｒｈｏ激酶（ＲＯＣＫ）抑制劑之內醯胺
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
UY37073A (es) 2016-01-13 2017-07-31 Bristol-Myers Squibb Company Una Corporación Del Estado De Delaware Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock, y las composiciones que los contienen
US10562887B2 (en) 2016-05-27 2020-02-18 Bristol-Myers Squibb Company Triazolones and tetrazolones as inhibitors of ROCK
US10787450B2 (en) 2016-07-07 2020-09-29 Bristol-Myers Squibb Company Spiro-fused cyclic ureas as inhibitors of rock
KR102491994B1 (ko) 2016-07-07 2023-01-25 브리스톨-마이어스 스큅 컴퍼니 Rock의 억제제로서의 스피로락탐
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
US10654860B2 (en) 2016-11-30 2020-05-19 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
US11390609B2 (en) * 2017-06-30 2022-07-19 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
EP3652164B1 (en) 2017-07-12 2023-06-21 Bristol-Myers Squibb Company Phenylacetamides as inhibitors of rock
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
ES2894128T3 (es) 2017-07-12 2022-02-11 Bristol Myers Squibb Co Inhibidores aminoheterocíclicos de cinco miembros y aminoheterocíclicos bicíclicos de 5,6 o 6,6 miembros de ROCK para el tratamiento de la insuficiencia cardíaca
WO2019089868A1 (en) 2017-11-03 2019-05-09 Bristol-Myers Squibb Company Diazaspiro rock inhibitors
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
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
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
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

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
US5696122A (en) * 1993-09-03 1997-12-09 Smithkline Beecham P.L.C. Indole and indoline derivatives as 5HT1D receptor antagonists
EP0724580A1 (en) * 1993-10-19 1996-08-07 Smithkline Beecham Plc Benzanilide derivatives as 5ht-1d receptor antagonists
WO2000006085A2 (en) * 1998-07-28 2000-02-10 Smithkline Beecham Corporation Compounds and methods
AU5196399A (en) 1998-08-11 2000-03-06 Daiichi Pharmaceutical Co., Ltd. Novel sulfonyl derivatives
JP3722700B2 (ja) * 1999-05-04 2005-11-30 シェーリング コーポレイション Ｃｃｒ５アンタゴニストとして有用なピペラジン誘導体
WO2001070673A2 (en) 2000-03-17 2001-09-27 Bristol-Myers Squibb Pharma Company CYCLIC β-AMINO ACID DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEASES AND TNF-$g(a)
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
IL160990A0 (en) 2001-10-01 2004-08-31 Bristol Myers Squibb Co Spiro-hydantoin compounds useful as anti-inflammatory agents
EP2033953A1 (en) * 2002-02-15 2009-03-11 Glaxo Group Limited Vanilloid receptor modulators
TWI319387B (en) * 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
AU2003252715B2 (en) * 2002-07-30 2009-06-04 Banyu Pharmaceutical Co., Ltd. Antagonist of melanin-concentrating hormone receptor comprising benzimidazole derivative as active ingredient
EP1569646A2 (en) 2002-12-13 2005-09-07 Smithkline Beecham Corporation Piperidine derivatives as ccr5 antagonists
AU2003299797A1 (en) * 2002-12-19 2004-07-14 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
MXPA05009063A (es) 2003-02-26 2005-12-12 Sugen Inc Compuestos de aminoheteroarilo como inhibidores de proteina cinasa.
EP1599475A2 (en) 2003-03-06 2005-11-30 Eisai Co., Ltd. Jnk inhibitors
WO2005074643A2 (en) 2004-01-30 2005-08-18 Smithkline Beecham Corporation Benzamide compounds useful as rock inhibitors
ES2337376T3 (es) * 2004-04-01 2010-04-23 Eli Lilly And Company Agentes receptores de la histamina h3, preparacion y usos terapeuticos.
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
EP2354139A1 (en) * 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
CA2613522A1 (en) 2005-06-27 2007-01-04 Exelixis, Inc. Imidazole based lxr modulators
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
KR101404360B1 (ko) 2006-09-05 2014-06-09 교와 핫꼬 기린 가부시키가이샤 이미다졸 유도체
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
CA2685106A1 (en) 2007-04-25 2008-11-06 Exelixis, Inc. 6-phenylpyrimidinones as pim modulators
AU2008285718A1 (en) 2007-08-07 2009-02-12 F. Hoffmann-La Roche Ag Pyrrolidine aryl-ether as NK3 receptor antagonists
CN103896831A (zh) * 2007-08-27 2014-07-02 Abbvie德国有限责任两合公司 4-(4-吡啶基)-苯甲酰胺及其作为rock活性调节剂的应用
CA2707445A1 (en) 2007-11-30 2009-06-11 Biota Scientific Management Pty Ltd Tetrahydro-isoquinoline ppat inhibitors as antibacterial agents
US8470816B2 (en) * 2007-12-03 2013-06-25 Takeda Pharmaceutical Company Limited 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
CA2730116A1 (en) 2008-07-08 2010-01-14 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
CN102177136A (zh) 2008-10-09 2011-09-07 弗·哈夫曼-拉罗切有限公司 吡咯烷n-苄基衍生物
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
SG173114A1 (en) 2009-01-30 2011-08-29 Hoffmann La Roche 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.
JP5624560B2 (ja) * 2009-05-28 2014-11-12 大塚製薬株式会社 ストレス性疾患の治療のための複素環化合物
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
NO2513053T3 (enExample) 2009-12-18 2018-03-03
UY33199A (es) 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.
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
US9302989B2 (en) 2010-11-15 2016-04-05 Abbvie Inc. NAMPT and rock inhibitors
PH12014500308A1 (en) * 2011-08-09 2021-06-02 Takeda Pharmaceuticals Co Cyclopropaneamine compound
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
IN2014MN02562A (enExample) 2012-06-27 2015-07-24 4Sc Discovery Gmbh
NZ729443A (en) * 2012-07-03 2017-11-24 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
US9815820B2 (en) 2012-10-05 2017-11-14 Kadmon Corporation, Llc Rho kinase inhibitors
LT3486245T (lt) * 2012-12-07 2021-08-25 Vertex Pharmaceuticals Incorporated 2-amino-n-(piperidin-1-il-piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamidas, kaip atr kinazės inhibitorius
US9221767B2 (en) 2013-01-18 2015-12-29 Bristol-Myers Squibb Company Substituted phthalazinones 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
US9828345B2 (en) 2013-02-28 2017-11-28 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors

Also Published As

Publication number Publication date
EP3183248A1 (en) 2017-06-28
CN107108581B (zh) 2020-06-23
US20170226105A1 (en) 2017-08-10
WO2016028971A1 (en) 2016-02-25
JP2017524026A (ja) 2017-08-24
ES2838573T3 (es) 2021-07-02
US10112939B2 (en) 2018-10-30
EP3183248B1 (en) 2020-11-11
CN107108581A (zh) 2017-08-29

Similar Documents

Publication Publication Date Title
JP6633618B2 (ja) 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
US11884661B2 (en) 3-substituted propionic acids as αV integrin inhibitors
JP6423372B2 (ja) 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
JP6423371B2 (ja) 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
KR102644889B1 (ko) Rock 억제제로서의 스피로헵타닐 히단토인
CN109153663B (zh) 作为rock抑制剂的三唑酮类化合物和四唑酮类化合物
JP6488239B2 (ja) Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン
KR102680160B1 (ko) 심부전의 치료를 위한 rock의 5원-아미노헤테로사이클 및 5,6- 또는 6,6-원 비시클릭 아미노헤테로시클릭 억제제
JP2019520398A (ja) Ｒｏｃｋ阻害剤としてのスピロラクタム
HK40009959A (en) 3-substituted propionic acids as alpha v integrin inhibitors
HK40009959B (en) 3-substituted propionic acids as alpha v integrin inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180817

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180817

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20190509

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190528

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190821

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190903

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20191126

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20191210

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20191212

R150 Certificate of patent or registration of utility model

Ref document number: 6633618

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250