JP6434968B2 - Ｒｏｃｋ阻害剤としての三環式ピリド−カルボキサミド誘導体 - Google Patents

Ｒｏｃｋ阻害剤としての三環式ピリド−カルボキサミド誘導体 Download PDF

Info

Publication number
JP6434968B2
JP6434968B2 JP2016524303A JP2016524303A JP6434968B2 JP 6434968 B2 JP6434968 B2 JP 6434968B2 JP 2016524303 A JP2016524303 A JP 2016524303A JP 2016524303 A JP2016524303 A JP 2016524303A JP 6434968 B2 JP6434968 B2 JP 6434968B2
Authority
JP
Japan
Prior art keywords
substituted
carboxamide
pyridine
chromeno
alkyl
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.)
Expired - Fee Related
Application number
JP2016524303A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016523922A5 (enExample
JP2016523922A (ja
Inventor
ミミ・エル・クワン
ジルン・フー
ワン・カイラン
シャラナバサッパ・パティル
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 JP2016523922A publication Critical patent/JP2016523922A/ja
Publication of JP2016523922A5 publication Critical patent/JP2016523922A5/ja
Application granted granted Critical
Publication of JP6434968B2 publication Critical patent/JP6434968B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • 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
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10—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
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
JP2016524303A 2013-07-02 2014-07-01 Ｒｏｃｋ阻害剤としての三環式ピリド−カルボキサミド誘導体 Expired - Fee Related JP6434968B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361842098P 2013-07-02 2013-07-02
US61/842,098 2013-07-02
PCT/US2014/044988 WO2015002915A1 (en) 2013-07-02 2014-07-01 Tricyclic pyri do-carboxam i d e derivatives as rock inhibitors

Publications (3)

Publication Number Publication Date
JP2016523922A JP2016523922A (ja) 2016-08-12
JP2016523922A5 JP2016523922A5 (enExample) 2017-08-10
JP6434968B2 true JP6434968B2 (ja) 2018-12-05

Family

ID=51211901

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016524303A Expired - Fee Related JP6434968B2 (ja) 2013-07-02 2014-07-01 Ｒｏｃｋ阻害剤としての三環式ピリド−カルボキサミド誘導体

Country Status (8)

Country Link
US (1) US9914740B2 (enExample)
EP (1) EP3016951B1 (enExample)
JP (1) JP6434968B2 (enExample)
CN (1) CN105492444B (enExample)
AR (1) AR096788A1 (enExample)
ES (1) ES2633987T3 (enExample)
TW (1) TW201506024A (enExample)
WO (1) WO2015002915A1 (enExample)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2958924B1 (en) 2013-02-22 2016-12-28 Bristol-Myers Squibb Company 5h-chromeno[3,4-c]pyridines as inhibitors of adaptor associated kinase 1 (aak1)
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
WO2015002926A1 (en) 2013-07-02 2015-01-08 Bristol-Myers Squibb Company Tricyclic pyrido-carboxamide derivatives as rock inhibitors
JP6434968B2 (ja) 2013-07-02 2018-12-05 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｒｏｃｋ阻害剤としての三環式ピリド−カルボキサミド誘導体
CN105979950A (zh) 2013-10-11 2016-09-28 百时美施贵宝公司 吡咯并三嗪激酶抑制剂
US9902702B2 (en) 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
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
EP3292124B1 (en) 2015-04-10 2019-05-22 Bristol-Myers Squibb Company 6h-isochromeno[3,4-c]pyridines and benzo[c][1,7]naphthyridin-6-(5h)-ones as adaptor associated kinase 1 (aak1) inhibitors
CN107709314A (zh) 2015-06-11 2018-02-16 巴斯利尔药物国际股份公司 外排泵抑制剂及其治疗性用途
AU2016313263B2 (en) * 2015-08-26 2021-02-04 Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Condensed tricyclic compounds as protein kinase inhibitors
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
WO2017156071A1 (en) 2016-03-09 2017-09-14 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
WO2017205709A1 (en) 2016-05-27 2017-11-30 Bristol-Myers Squibb Company Triazolones and tetrazolones as inhibitors of rock
AU2017292646A1 (en) 2016-07-05 2019-02-07 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
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
ES2821877T3 (es) 2016-07-07 2021-04-28 Bristol Myers Squibb Co Espirolactamas como inhibidores de 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
US10934261B2 (en) 2016-09-28 2021-03-02 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
EP3548468B1 (en) 2016-11-30 2020-09-16 Bristol-Myers Squibb Company Tricyclic rho kinase inhibitors
JP6906105B2 (ja) * 2017-06-16 2021-07-21 成都先導薬物開発股▲ふん▼有限公司Ｈｉｔｇｅｎ Ｌｔｄ． Ｒｏｃｋを阻害する化合物及びその使用
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
WO2019014300A1 (en) 2017-07-12 2019-01-17 Bristol-Myers Squibb Company PHENYLACETAMIDES 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
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
ES2937039T3 (es) 2017-11-03 2023-03-23 Bristol Myers Squibb Co Inhibidores diazaespiro de ROCK
WO2019180627A1 (en) * 2018-03-21 2019-09-26 Piramal Enterprises Limited AN IMPROVED ASYMMETRIC SYNTHESIS OF alpha-(DIARYLMETHYL) ALKYL AMINES
CN108299429B (zh) * 2018-04-09 2021-10-08 中南大学 一类八氢苯并萘啶化合物及其制备方法和应用
CN110283119A (zh) * 2018-04-20 2019-09-27 长沙理工大学 一种合成全碳基取代吡啶衍生物的方法
CN110759923B (zh) * 2018-07-26 2022-08-30 上海医药工业研究院有限公司 嘧啶并吡咯并哒嗪衍生物、其中间体、制备方法、药物组合物和用途
AU2021228285A1 (en) * 2020-02-28 2022-09-29 Remix Therapeutics Inc. Compounds and methods for modulating splicing
CN115697968B (zh) * 2020-05-28 2024-03-29 杭州中美华东制药有限公司 (s)-2-氨基-3-(4-(2,3-二甲基吡啶-4-基)苯基丙酸甲酯及其盐的制备方法
CN112010853A (zh) * 2020-09-01 2020-12-01 成都大学 一种食品中杂环胺风险物质norharman及类似物的合成方法
CA3195150A1 (en) 2020-10-08 2022-04-14 Sven Weiler Benzo[h]quinazolin-4-amine and thieno[3,2-h]quinazolin-4-amine derivatives for the treatment of cancer
US20240400584A1 (en) * 2021-08-30 2024-12-05 Remix Therapeutics Inc. Compounds and methods for modulating splicing
CA3238227A1 (en) 2021-11-11 2023-05-19 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation
CN114544851B (zh) * 2022-02-22 2023-12-15 苏州正济医药研究有限公司 一种测定邻氯苯甘氨酸甲酯酒石酸盐及杂质的分析方法
CN117105779A (zh) * 2023-07-18 2023-11-24 河南师范大学 一种5-溴-2-甲酰基苯甲酸甲酯的制备方法
CN117263934A (zh) * 2023-08-16 2023-12-22 上海凌凯医药科技有限公司 一种5H-苯并[c][1,6]萘啶-6-酮类衍生物的制备方法
CN119874716B (zh) * 2025-03-27 2025-07-15 上海隆盛化工有限公司 1-氯-6,8-二氟-7-异丙基苯并呋喃并[2,3-c]吡啶及其合成方法和应用

Family Cites Families (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU168036B (enExample) 1973-11-09 1976-02-28
HU168776B (enExample) 1973-11-09 1976-07-28
CA1098910A (en) 1978-06-15 1981-04-07 Robert N. Schut 3-amino-2-(5-fluoro and 5-methoxy-1h-indol-3-yl) propanoic acid derivatives
JPS57116067A (en) 1981-01-12 1982-07-19 Sankyo Kagaku Kk Novel 8-quinolinesulfonyl derivative, its synthesis and use
DE3703435A1 (de) 1987-02-05 1988-08-18 Thomae Gmbh Dr K Neue thiazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
IE68593B1 (en) 1989-12-06 1996-06-26 Sanofi Sa Heterocyclic substituted acylaminothiazoles their preparation and pharmaceutical compositions containing them
WO1996037493A1 (de) 1995-05-26 1996-11-28 Bayer Aktiengesellschaft Pyridyl-thiazole und deren verwendung zum schutz von pflanzen gegen befall durch mikroorganismen
CA2276034A1 (en) 1996-12-23 1998-07-02 Mimi Lifen Quan Oxygen or sulfur containing 5-membered heteroaromatics as factor xa inhibitors
US6187797B1 (en) 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
JPH11193281A (ja) 1997-10-27 1999-07-21 Takeda Chem Ind Ltd アデノシンａ３受容体拮抗剤およびチアゾール化合物
WO1999052906A1 (de) 1998-04-08 1999-10-21 Bayer Aktiengesellschaft Substituierte oxazolyl- und thiazolyl-uracil herbizide
KR20020069183A (ko) 1999-07-26 2002-08-29 시오노기세이야쿠가부시키가이샤 트롬보포이에틴 작동성을 나타내는 의약 조성물
CA2402549A1 (en) * 2000-03-15 2001-09-20 Aventis Pharma Deutschland Gmbh Substituted beta-carbolines
EP1268477B1 (en) * 2000-03-15 2010-04-21 Sanofi-Aventis Deutschland GmbH Substituted beta-carbolines with ikb-kinase inhibiting activity
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
JP2002053566A (ja) 2000-08-11 2002-02-19 Japan Tobacco Inc チアゾール化合物及びその医薬用途
JP4790969B2 (ja) 2000-08-11 2011-10-12 日本ケミファ株式会社 ペルオキシソーム増殖剤応答性受容体δの活性化剤
US20020173507A1 (en) 2000-08-15 2002-11-21 Vincent Santora Urea compounds and methods of uses
US20020103192A1 (en) 2000-10-26 2002-08-01 Curtin Michael L. Inhibitors of histone deacetylase
WO2002051442A1 (en) 2000-12-26 2002-07-04 Takeda Chemical Industries, Ltd. Concomitant drugs
JPWO2002062775A1 (ja) 2001-02-02 2004-06-10 山之内製薬株式会社 ２−アシルアミノチアゾール誘導体又はその塩
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
US20020177594A1 (en) 2001-03-14 2002-11-28 Curtin Michael L. Inhibitors of histone deacetylase
JP4157381B2 (ja) 2001-03-23 2008-10-01 日本ケミファ株式会社 ペルオキシソーム増殖剤応答性受容体の活性化剤
JPWO2002087589A1 (ja) 2001-04-26 2004-08-12 第一製薬株式会社 薬剤排出ポンプ阻害薬
EP1402900A1 (en) 2001-06-11 2004-03-31 Takeda Chemical Industries, Ltd. Medicinal compositions
GB0123589D0 (en) 2001-10-01 2001-11-21 Syngenta Participations Ag Organic compounds
WO2003048140A1 (en) 2001-12-03 2003-06-12 Japan Tobacco Inc. Azole compound and medicinal use thereof
PT1466912E (pt) 2002-01-18 2013-06-28 Astellas Pharma Inc Derivado de 2-aciloaminotiazol ou seu sal
EP1467981A1 (en) 2002-01-25 2004-10-20 Kylix Pharmaceuticals B.V. 4(hetero-) aryl substituted (thia-/oxa-/pyra) zoles for inhibition of tie-2
US7229987B2 (en) 2002-05-13 2007-06-12 Eli Lilly And Company Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes
JP2006508042A (ja) 2002-07-18 2006-03-09 ブリストル−マイヤーズ　スクイブ　カンパニー グルココルチコイド受容体の修飾物質および方法
CN1691944A (zh) 2002-08-09 2005-11-02 阿斯利康(瑞典)有限公司 作为代谢型谷氨酸受体－5调节剂的噁二唑
WO2004016592A1 (en) 2002-08-14 2004-02-26 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
AU2003288956A1 (en) 2002-10-30 2004-06-07 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases
GB0230087D0 (en) 2002-12-24 2003-01-29 Astrazeneca Ab Therapeutic agents
GB0302672D0 (en) 2003-02-06 2003-03-12 Astrazeneca Ab Pharmaceutical formulations
WO2004071509A1 (ja) 2003-02-12 2004-08-26 Nippon Chemiphar Co., Ltd. オリゴデンドロサイト分化促進剤
PT1611088E (pt) 2003-04-07 2009-09-24 Pharmacyclics Inc Hidroxamatos como agentes terapêuticos
US7696198B2 (en) 2003-04-16 2010-04-13 Memory Pharmaceuticals Corporation Phosphodiesterase 4 inhibitors
CN100545161C (zh) 2003-08-15 2009-09-30 中国科学院上海药物研究所 一类杂环衍生物、制备方法及其用途
US7351727B2 (en) 2003-09-02 2008-04-01 Bristol-Myers Squibb Company Inhibitors of 15-lipoxygenase
US7973169B2 (en) 2003-09-06 2011-07-05 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
AR045651A1 (es) 2003-09-19 2005-11-02 Solvay Pharm Bv Derivados de tiazol como moduladores del receptor de cannabinoide
EP1682143A2 (en) 2003-10-28 2006-07-26 Pharmacia Corporation Combinations comprising an hsp90 inhibitor and a phophodiesterase inhibitor for treating or preventing neoplasia
WO2005044194A2 (en) 2003-10-28 2005-05-19 Pharmacia Corporation TREATMENT OR PREVENTION OF NEOPLASIA BY USE OF AN Hsp90 INHIBITOR
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
BRPI0507278A (pt) 2004-01-30 2007-06-26 Vertex Pharma moduladores dos transportadores do cassete de ligação ao atp
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
AU2005212073B2 (en) 2004-02-18 2010-07-08 Kyorin Pharmaceutical Co., Ltd. Bicyclic amide derivatives
MY148488A (en) 2004-02-18 2013-04-30 Astrazeneca Ab Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
US7259155B2 (en) 2004-05-05 2007-08-21 Otsuka Pharmaceutical Factory, Inc. Phosphonic diester derivatives
TW200637559A (en) 2005-03-29 2006-11-01 Shionogi & Co 3-propenylcefem derivative
FR2885129B1 (fr) 2005-04-29 2007-06-15 Proskelia Sas Nouveaux derives de l'ureee substituee parun thiazole ou benzothiazole, leur procede de preparation, leur application a titre de medicaments, les compositions pharmaceutiques les renfermant et utilisation.
AU2006244203B2 (en) 2005-05-09 2012-05-03 Achillion Pharmaceuticals, Inc. Thiazole compounds and methods of use
US7655446B2 (en) 2005-06-28 2010-02-02 Vertex Pharmaceuticals Incorporated Crystal structure of Rho-kinase I kinase domain complexes and binding pockets thereof
JP2009505948A (ja) * 2005-07-11 2009-02-12 デブジェン エヌブイ キナーゼ阻害剤としてのアミド誘導体
EP1962892A4 (en) 2005-11-22 2011-10-12 Univ South Florida INHIBITION OF CELL PROLIFERATION
WO2007075896A2 (en) 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors
JP2009524677A (ja) 2006-01-25 2009-07-02 シンタ ファーマシューティカルズ コーポレーション 炎症および免疫関連使用用のチアゾールおよびチアジアゾール化合物
WO2007116106A1 (es) 2006-04-12 2007-10-18 Palobiofarma, S.L. Nuevos compuestos como antagonistas de los receptores a1 de adenosina
EP2032562B1 (en) 2006-05-12 2010-08-25 Vertex Pharmaceuticals Incorporated Selective inhibitors of rock protein kinase and uses thereof
WO2008014199A2 (en) 2006-07-28 2008-01-31 Boehringer Ingelheim International Gmbh Sulfonyl compounds which modulate the cb2 receptor
KR20090069318A (ko) 2006-09-25 2009-06-30 베링거 인겔하임 인터내셔날 게엠베하 Ｃｂ2 수용체를 조절하는 화합물
TW200831081A (en) 2006-12-25 2008-08-01 Kyorin Seiyaku Kk Glucokinase activator
WO2008124000A2 (en) 2007-04-02 2008-10-16 Ligand Pharmaceuticals Incorporated Thiazole derivatives as androgen receptor modulator compounds
GB0706793D0 (en) 2007-04-05 2007-05-16 Evotec Ag Compounds
WO2009002933A1 (en) 2007-06-22 2008-12-31 Hydra Biosciences, Inc. Methods and compositions for treating disorders
US8445686B2 (en) 2007-08-27 2013-05-21 Abbvie Inc. 4-(4-pyridinyl)-benzamides and their use as rock activity modulators
WO2009026701A1 (en) 2007-08-29 2009-03-05 Methylgene Inc. Sirtuin inhibitors
ES2331220B1 (es) 2007-10-02 2010-09-23 Palobiofarma, S.L. Nuevos compuestos como antagonistas de los receptores a1 de adenosina.
JP5423679B2 (ja) 2007-10-31 2014-02-19 日産化学工業株式会社 ピリダジノン化合物及びｐ２ｘ７受容体阻害剤
EP2217565B1 (en) 2007-11-07 2013-05-22 Boehringer Ingelheim International GmbH Compounds which modulate the cb2 receptor
WO2009067607A2 (en) 2007-11-20 2009-05-28 Memory Pharmaceuticals Corporation Combinations of pde4 inhibitors and antipsychotics for the treatment of psychotic disorders
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009081222A1 (en) 2007-12-21 2009-07-02 Glenmark Pharmaceuticals, S.A. Substituted tricyclic pyridine or pyrimidine vanilloid receptor ligands
EP2250999B1 (en) 2008-02-08 2016-04-13 Shiseido Company, Ltd. Skin whitening agent and external preparation for the skin
US20110105436A1 (en) 2008-03-10 2011-05-05 Auckland Uniservices Limited Heteroaryl compounds, compositions, and methods of use in cancer treatment
WO2009140519A1 (en) 2008-05-14 2009-11-19 Hydra Biosciences, Inc. Compounds and compositions for treating chemical warfare agent-induced injuries
WO2010028193A1 (en) 2008-09-03 2010-03-11 Repligen Corporation Compounds including pimelic acid derivatives as hdac inhibitors
US20100063085A1 (en) * 2008-09-11 2010-03-11 University Court Of The University Of Dundee Method of treating learning impairment in down's syndrome subjects
US20110294853A1 (en) 2008-09-12 2011-12-01 Benjamin Pelcman Bis Aromatic Compounds for Use in the Treatment of Inflammation
WO2010036821A1 (en) 2008-09-24 2010-04-01 Hydra Biosciences, Inc. Methods and compositions for treating respiratory disorders
AR074790A1 (es) 2008-12-19 2011-02-09 Novartis Ag Derivados de isooxazol sustituidos, composiciones farmaceuticas y para el control de parasitos que los comprenden y su uso en metodos para controlar parasitos en y sobre animales de sangre caliente.
EP2370407B1 (en) * 2008-12-19 2014-06-18 Bristol-Myers Squibb Company Carbazole and carboline kinase inhibitors
CN102264737A (zh) 2008-12-23 2011-11-30 雅培制药有限公司 抗病毒化合物
JP2012051804A (ja) * 2008-12-26 2012-03-15 Kyoto Univ Ｅｇ５阻害剤
UA103918C2 (en) 2009-03-02 2013-12-10 Айерем Элелси N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators
US8362249B2 (en) 2009-04-27 2013-01-29 Boehringer Ingelheim International Gmbh CXCR3 receptor antagonists
CN102573487A (zh) 2009-06-09 2012-07-11 加利福尼亚资本权益有限责任公司 Hedgehog信号传导的吡啶基-三嗪抑制剂
BR112012004149A2 (pt) 2009-08-25 2016-03-22 Abraxis Bioscience Llc terapia de combinação com composições de nanopartículas de taxano e inibidores de hedgehog
JP5856064B2 (ja) * 2009-11-17 2016-02-09 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 治療特性を有する１，４−ベンゾジアゼピン−２，５−ジオンおよび関連化合物
US8609866B2 (en) 2009-12-18 2013-12-17 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
WO2011129095A1 (ja) 2010-04-12 2011-10-20 塩野義製薬株式会社 インテグラーゼ阻害活性を有するピリドン誘導体
US9221808B2 (en) 2010-04-16 2015-12-29 H. Lee Moffitt Cancer Center And Research Institute, Inc. Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinase (ROCK) and methods of use
US8685969B2 (en) * 2010-06-16 2014-04-01 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
US9000154B2 (en) * 2010-10-19 2015-04-07 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
US8703953B2 (en) 2012-03-09 2014-04-22 Bristol-Myers Squibb Company Aryl ether-base kinase inhibitors
HK1199814A1 (en) * 2012-03-09 2015-07-24 Lexicon Pharmaceuticals, Inc. Inhibition of adaptor associated kinase 1 for the treatment of pain
WO2015002926A1 (en) 2013-07-02 2015-01-08 Bristol-Myers Squibb Company Tricyclic pyrido-carboxamide derivatives as rock inhibitors
JP6434968B2 (ja) 2013-07-02 2018-12-05 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｒｏｃｋ阻害剤としての三環式ピリド−カルボキサミド誘導体

Also Published As

Publication number Publication date
US9914740B2 (en) 2018-03-13
TW201506024A (zh) 2015-02-16
WO2015002915A1 (en) 2015-01-08
CN105492444A (zh) 2016-04-13
CN105492444B (zh) 2018-09-07
AR096788A1 (es) 2016-02-03
ES2633987T3 (es) 2017-09-26
EP3016951B1 (en) 2017-05-31
EP3016951A1 (en) 2016-05-11
JP2016523922A (ja) 2016-08-12
US20160152628A1 (en) 2016-06-02

Similar Documents

Publication Publication Date Title
KR102680164B1 (ko) Rock 억제제로서의 페닐아세트아미드
JP7225317B2 (ja) 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
JP7155102B2 (ja) Ｒｏｃｋ阻害剤としてのスピロ縮合環尿素
JP6622378B2 (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
JP6522602B2 (ja) Ｒｏｃｋ阻害剤としての三環式ピリド−カルボキサミド誘導体
EP3016951B1 (en) Tricyclic pyrido-carboxamide derivatives as rock inhibitors
KR102725741B1 (ko) Rock의 억제제로서의 스피로헵탄 살리실아미드 및 관련 화합물
KR102716960B1 (ko) 디아자스피로 rock 억제제
KR102506327B1 (ko) αV 인테그린 길항제로서의 인다졸 유도체
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
CN107406426B (zh) 作为rock抑制剂的环状脲类
JP2019517475A (ja) Ｒｏｃｋ阻害剤としてのトリアゾロンおよびテトラゾロン

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160324

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20160219

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170630

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20170630

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180724

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181019

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: 20181106

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20181109

R150 Certificate of patent or registration of utility model

Ref document number: 6434968

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

LAPS Cancellation because of no payment of annual fees