AR096788A1 - Compuestos tricíclicos de carboxamida como inhibidores potentes de rock - Google Patents

Compuestos tricíclicos de carboxamida como inhibidores potentes de rock

Info

Publication number
AR096788A1
AR096788A1 ARP140102466A ARP140102466A AR096788A1 AR 096788 A1 AR096788 A1 AR 096788A1 AR P140102466 A ARP140102466 A AR P140102466A AR P140102466 A ARP140102466 A AR P140102466A AR 096788 A1 AR096788 A1 AR 096788A1
Authority
AR
Argentina
Prior art keywords
substituted
independently selected
nrara
alkyl
chrd
Prior art date
Application number
ARP140102466A
Other languages
English (en)
Spanish (es)
Inventor
Patil Sharanabasappa
Wang Cailan
L Quan Mimi
Hu Zilun
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 AR096788A1 publication Critical patent/AR096788A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10Drugs 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • AIDS & HIV (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Molecular Biology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
ARP140102466A 2013-07-02 2014-07-01 Compuestos tricíclicos de carboxamida como inhibidores potentes de rock AR096788A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361842098P 2013-07-02 2013-07-02

Publications (1)

Publication Number Publication Date
AR096788A1 true AR096788A1 (es) 2016-02-03

Family

ID=51211901

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140102466A AR096788A1 (es) 2013-07-02 2014-07-01 Compuestos tricíclicos de carboxamida como inhibidores potentes de rock

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 (41)

* 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)
US9828345B2 (en) 2013-02-28 2017-11-28 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent ROCK1 and ROCK2 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
CN105518005B (zh) 2013-07-02 2018-07-20 百时美施贵宝公司 作为rock抑制剂的三环吡啶-甲酰胺衍生物
TW201506024A (zh) 2013-07-02 2015-02-16 必治妥美雅史谷比公司 作為有效rock抑制劑的三環甲醯胺衍生物
US9737542B2 (en) 2013-10-11 2017-08-22 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US9902702B2 (en) 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
US10123993B2 (en) 2015-01-09 2018-11-13 Bristol-Myers Squibb Company Cyclic ureas as inhibitors of rock
EP3268360B1 (en) 2015-03-09 2019-04-24 Bristol-Myers Squibb Company Lactams as inhibitors of rock
US10174044B2 (en) 2015-04-10 2019-01-08 Bristol-Myers Squibb Company Fused pyridines as kinase inhibitors
KR20180011843A (ko) 2015-06-11 2018-02-02 바실리어 파마슈티카 인터내셔널 리미티드 유출-펌프 억제제 및 이의 치료적 용도
EP3341376B1 (en) * 2015-08-26 2020-12-23 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
US10590084B2 (en) 2016-03-09 2020-03-17 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
EP3464262B1 (en) 2016-05-27 2020-02-26 Bristol-Myers Squibb Company Triazolones and tetrazolones as inhibitors of rock
US11292801B2 (en) 2016-07-05 2022-04-05 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
US10730858B2 (en) 2016-07-07 2020-08-04 Bristol-Myers Squibb Company Lactam, cyclic urea and carbamate, and triazolone derivatives as potent and selective rock inhibitors
EP3523294A4 (en) 2016-09-28 2021-01-13 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
US10654860B2 (en) 2016-11-30 2020-05-19 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
EP3652167B1 (en) 2017-07-12 2021-06-02 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
US11306081B2 (en) 2017-07-12 2022-04-19 Bristol-Myers Squibb Company Phenylacetamides as inhibitors of rock
US11192891B2 (en) 2017-11-03 2021-12-07 Bristol-Myers Squibb Company Diazaspiro ROCK inhibitors
JP2021523092A (ja) * 2018-03-21 2021-09-02 ピラマル・ファーマ・リミテッドPiramal Pharma Limited アルファ−(ジアリールメチル)アルキルアミンの改良された不斉合成
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
MX2022010681A (es) * 2020-02-28 2023-03-21 Remix Therapeutics Inc Compuestos y metodos para modular el empalme.
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
WO2023034833A1 (en) * 2021-08-30 2023-03-09 Remix Therapeutics Inc. Compounds and methods for modulating splicing
AU2022385051A1 (en) 2021-11-11 2024-06-20 Actualeyes Inc. 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
HU168776B (enExample) 1973-11-09 1976-07-28
HU168036B (enExample) 1973-11-09 1976-02-28
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
CN1065242C (zh) 1995-05-26 2001-05-02 拜尔公司 吡啶基-噻唑
US6187797B1 (en) 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
EP0946528B1 (en) 1996-12-23 2003-04-09 Bristol-Myers Squibb Pharma Company OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
ATE257703T1 (de) 1997-10-27 2004-01-15 Takeda Chemical Industries Ltd 1,3-thiazole als adenosine a3 rezeptor antagonisten zur behandlung von asthma, allergien und diabetes
AU3702699A (en) 1998-04-08 1999-11-01 Bayer Aktiengesellschaft Substituted oxazolyle and thiazolyl uracil herbicides
EP1207155A4 (en) 1999-07-26 2005-01-12 Shionogi & Co DRUG COMPOSITIONS HAVING AGONIST THROMBOPOIETINE ACTIVITY
KR100826817B1 (ko) * 2000-03-15 2008-05-02 사노피-아벤티스 도이칠란트 게엠베하 치환된 베타-카볼린
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
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
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
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
CA2436739A1 (en) 2000-12-26 2002-07-04 Takeda Chemical Industries, Ltd. Combination agent
WO2002062775A1 (en) 2001-02-02 2002-08-15 Yamanouchi Pharmaceutical Co., Ltd. 2-acylaminothiazole derivative or its salt
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
WO2002076957A1 (en) 2001-03-23 2002-10-03 Nippon Chemiphar Co.,Ltd. Activator for peroxisome proliferator-activated receptor
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
WO2002100433A1 (fr) 2001-06-11 2002-12-19 Takeda Chemical Industries, Ltd. Compositions medicinales
GB0123589D0 (en) 2001-10-01 2001-11-21 Syngenta Participations Ag Organic compounds
US7163952B2 (en) 2001-12-03 2007-01-16 Japan Tobacco Inc. Azole compound and medicinal use thereof
CN1319967C (zh) 2002-01-18 2007-06-06 安斯泰来制药有限公司 2-酰基氨基噻唑衍生物或其盐
WO2003062215A1 (en) 2002-01-25 2003-07-31 Kylix Pharmaceuticals B.V. 4(hetero-) aryl substituted (thia-/oxa-/pyra) zoles for inhibition of tie-2
CA2484233A1 (en) 2002-05-13 2003-11-27 Eli Lilly And Company Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes
PL375442A1 (en) 2002-07-18 2005-11-28 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
MXPA05001592A (es) 2002-08-09 2005-05-05 Astrazeneca Ab Oxadiazoles como moduladores de receptor-5 de glutamato metabotropico.
AU2003265395A1 (en) 2002-08-14 2004-03-03 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
NZ540161A (en) 2002-10-30 2008-03-28 Vertex Pharma 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
ES2328819T3 (es) 2003-04-07 2009-11-18 Pharmacyclics, Inc. Hidroxamatos como agentes terapeuticos.
WO2004094375A2 (en) 2003-04-16 2004-11-04 Memory Pharmaceuticals Corporation 4 - (3,4 - disubstituted phenyl) - pyrrolidin-2-one compounds as 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
WO2005026137A2 (en) 2003-09-06 2005-03-24 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
TWI336697B (en) 2003-09-19 2011-02-01 Solvay Pharm Bv Thiazole derivatives as cannabinoid receptor modulators
MXPA06004657A (es) 2003-10-28 2006-06-27 Pharmacia Corp Combinaciones que comprenden un inhibidor de hsp90 y un inhibidor de fosfodiesterasa para tratar o prevenir la neoplasia.
WO2005044194A2 (en) 2003-10-28 2005-05-19 Pharmacia Corporation TREATMENT OR PREVENTION OF NEOPLASIA BY USE OF AN Hsp90 INHIBITOR
EP1713775A4 (en) 2004-01-30 2009-08-12 Smithkline Beecham Corp CHEMICAL COMPOUNDS
ES2631362T3 (es) 2004-01-30 2017-08-30 Vertex Pharmaceuticals Incorporated Moduladores de transportadores de casete de unión a ATP
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
MY148488A (en) 2004-02-18 2013-04-30 Astrazeneca Ab Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
JPWO2005077900A1 (ja) 2004-02-18 2007-10-18 杏林製薬株式会社 ビシクロアミド誘導体
US7259155B2 (en) 2004-05-05 2007-08-21 Otsuka Pharmaceutical Factory, Inc. Phosphonic diester derivatives
JP3928086B2 (ja) 2005-03-29 2007-06-13 塩野義製薬株式会社 3−プロペニルセフェム誘導体
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.
WO2006122011A2 (en) 2005-05-09 2006-11-16 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
BRPI0615524A2 (pt) * 2005-07-11 2010-04-06 Devgen Nv derivados da amida como inibidores da quinase
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
EP1983980A4 (en) 2006-01-25 2010-05-05 Synta Pharmaceuticals Corp THIAZOL AND THIADIAZOL COMPOUNDS FOR USES IN RELATION TO INFLAMMATION AND IMMUNITY
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
JP5448164B2 (ja) 2006-07-28 2014-03-19 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 Cb2受容体を変調する化合物
MX2009002888A (es) 2006-09-25 2009-03-31 Boehringer Ingelheim Int Compuestos que modulan el receptor cb2.
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
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
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.
EP2203429A1 (en) 2007-10-31 2010-07-07 Nissan Chemical Industries, Ltd. Pyridazinone derivatives and use thereof as p2x7 receptor inhibitors
JP5492092B2 (ja) 2007-11-07 2014-05-14 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 Cb2受容体を調節する化合物
WO2009067607A2 (en) 2007-11-20 2009-05-28 Memory Pharmaceuticals Corporation Combinations of pde4 inhibitors and antipsychotics for the treatment of psychotic disorders
WO2009081222A1 (en) 2007-12-21 2009-07-02 Glenmark Pharmaceuticals, S.A. Substituted tricyclic pyridine or pyrimidine vanilloid receptor ligands
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
ES2655305T3 (es) 2008-02-08 2018-02-19 Shiseido Company, Ltd. Agente para blanqueamiento de la piel
WO2009114552A1 (en) 2008-03-10 2009-09-17 The Board Of Trustees Of The Leland Stanford Junior University Heteroaryl compounds, compositions, and methods of use in cancer treatment
US20120108614A1 (en) 2008-05-14 2012-05-03 Chong Jayhong A 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
WO2010029300A1 (en) 2008-09-12 2010-03-18 Biolipox Ab 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
ES2490867T3 (es) * 2008-12-19 2014-09-04 Bristol-Myers Squibb Company Inhibidores de carbazol y carbolina quinasas
NZ593135A (en) 2008-12-19 2013-04-26 Novartis Ag Isoxazoline derivatives and their use as pesticide
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
JP2012529518A (ja) 2009-06-09 2012-11-22 アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー ヘッジホッグシグナル伝達のピリジル−トリアジン阻害剤
HRP20160551T8 (hr) 2009-08-25 2016-11-18 Abraxis Bioscience, Llc Kombinirana terapija s pripravcima nanočestica taksana i hedgehog inhibitora
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
MX2012006913A (es) 2009-12-18 2012-08-23 Activesite Pharmaceuticals Inc Profarmacos de inhibidores de calicreina plasmatica.
JP5766690B2 (ja) 2010-04-12 2015-08-19 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
EP2582668B1 (en) * 2010-06-16 2016-01-13 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
EP2630144B1 (en) * 2010-10-19 2016-09-07 Boehringer Ingelheim International GmbH Rho kinase inhibitors
JP2015513557A (ja) * 2012-03-09 2015-05-14 レクシコン ファーマシューティカルズ インコーポレイテッド 疼痛の治療に対するアダプター関連キナーゼ1の阻害
US8703953B2 (en) 2012-03-09 2014-04-22 Bristol-Myers Squibb Company Aryl ether-base kinase inhibitors
TW201506024A (zh) 2013-07-02 2015-02-16 必治妥美雅史谷比公司 作為有效rock抑制劑的三環甲醯胺衍生物
CN105518005B (zh) 2013-07-02 2018-07-20 百时美施贵宝公司 作为rock抑制剂的三环吡啶-甲酰胺衍生物

Also Published As

Publication number Publication date
US20160152628A1 (en) 2016-06-02
TW201506024A (zh) 2015-02-16
WO2015002915A1 (en) 2015-01-08
CN105492444B (zh) 2018-09-07
CN105492444A (zh) 2016-04-13
EP3016951B1 (en) 2017-05-31
ES2633987T3 (es) 2017-09-26
JP6434968B2 (ja) 2018-12-05
EP3016951A1 (en) 2016-05-11
US9914740B2 (en) 2018-03-13
JP2016523922A (ja) 2016-08-12

Similar Documents

Publication Publication Date Title
AR096788A1 (es) Compuestos tricíclicos de carboxamida como inhibidores potentes de rock
AR094929A1 (es) Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
AR103990A1 (es) Ureas cíclicas como inhibidoras de rock
AR098414A1 (es) PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e
AR104884A1 (es) Compuestos de 4-hidroxi-3-(heteroaril)piridin-2-ona como agonistas de apj
AR129635A2 (es) Moduladores de tetrahidropiridopirazina de gpr6
AR100059A1 (es) Compuestos útiles como inmunomoduladores
AR099379A1 (es) Compuestos tricíclicos como agentes antineoplásicos
AR103232A1 (es) ANTAGONISTAS DE TGFbR
AR107061A1 (es) Heteroarilhidroxipirimidinonas como agonistas del receptor de apj
AR099228A1 (es) Inhibidores macrocíclicos de fxia que tienen grupos heterocíclicos
AR088423A1 (es) Ligadores p1 ciclicos como inhibidores del factor xia
AR102177A1 (es) Compuestos de heteroarilo como inhibidores de btk y usos de los mismos
AR106948A1 (es) Agonistas del receptor de apelina y método de uso
AR092349A1 (es) Imidazotriazincarbonitrilos utiles como inhibidores de quinasa
AR104176A1 (es) Inhibidores de ido (indolamina-2,3-dioxigenasa)
AR091981A1 (es) Dihidropiridona p1 como inhibidores del factor xia
AR107973A1 (es) 6-hidroxi-4-oxo-1,4-dihidropirimidin-5-carboxamidas como agonista de apj
AR096684A1 (es) Compuestos para tratar atrofia muscular espinal
AR100809A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR111983A1 (es) ANILLOS 6 - 5 FUSIONADOS COMO INHIBIDORES DE C5a
AR100807A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR104555A1 (es) SULFONAS TRICÍCLICAS COMO MODULARES DE RORg
AR090557A1 (es) DERIVADOS IMIDAZOLICOS AGONISTAS ADRENERGICOS a2
AR113811A1 (es) Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos

Legal Events

Date Code Title Description
FB Suspension of granting procedure