TW201444798A - 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物 - Google Patents

作爲強效rock1及rock2抑制劑之苯基吡唑衍生物 Download PDF

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TW201444798A
TW201444798A TW103106886A TW103106886A TW201444798A TW 201444798 A TW201444798 A TW 201444798A TW 103106886 A TW103106886 A TW 103106886A TW 103106886 A TW103106886 A TW 103106886A TW 201444798 A TW201444798 A TW 201444798A
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彌米L 關
胡子倫
王彩蘭
彼得W 克勞斯
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必治妥美雅史谷比公司
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    • 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
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    • C07D513/04Ortho-condensed systems

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  • Neurology (AREA)
  • Urology & Nephrology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW103106886A 2013-02-28 2014-02-27 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物 TW201444798A (zh)

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US201361770508P 2013-02-28 2013-02-28

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US (2) US9458110B2 (OSRAM)
EP (1) EP2961745B1 (OSRAM)
JP (1) JP6423371B2 (OSRAM)
CN (1) CN105358547B (OSRAM)
AR (1) AR094929A1 (OSRAM)
ES (1) ES2624664T3 (OSRAM)
TW (1) TW201444798A (OSRAM)
WO (1) WO2014134388A1 (OSRAM)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6423372B2 (ja) 2013-02-28 2018-11-14 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
US9902702B2 (en) 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
JP6633618B2 (ja) 2014-08-21 2020-01-22 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
TW201630899A (zh) * 2015-01-09 2016-09-01 必治妥美雅史谷比公司 作為rock抑制劑的環狀脲類
ES2730112T3 (es) * 2015-03-09 2019-11-08 Bristol Myers Squibb Co Lactamas como inhibidores de ROCK
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
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
WO2018036414A1 (zh) * 2016-08-23 2018-03-01 北京诺诚健华医药科技有限公司 稠杂环类衍生物、其制备方法及其在医学上的应用
IL266150B2 (en) * 2016-10-24 2023-12-01 Translational Drug Dev Llc 3-substituted benzamide derivatives as kinase inhibitors
KR102511441B1 (ko) * 2016-11-30 2023-03-16 브리스톨-마이어스 스큅 컴퍼니 트리시클릭 Rho 키나제 억제제
US11046683B2 (en) 2016-12-15 2021-06-29 Ono Pharmaceutical Co., Ltd. Activator of TREK (TWIK RElated K+ channels) channels
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
ES2878054T3 (es) 2017-07-12 2021-11-18 Bristol Myers Squibb Co Espiroheptanil hidantoínas como inhibidores de ROCK
CN110869361B (zh) 2017-07-12 2023-06-02 百时美施贵宝公司 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
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
US11306081B2 (en) 2017-07-12 2022-04-19 Bristol-Myers Squibb Company Phenylacetamides as inhibitors of rock
US12060341B2 (en) 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
JP7114594B2 (ja) 2017-07-28 2022-08-08 武田薬品工業株式会社 複素環化合物
WO2019089868A1 (en) 2017-11-03 2019-05-09 Bristol-Myers Squibb Company Diazaspiro rock inhibitors
CA3092749A1 (en) * 2018-03-23 2019-09-26 Fochon Pharmaceuticals, Ltd. Deuterated compounds as rock inhibitors
WO2019201297A1 (zh) 2018-04-18 2019-10-24 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
EP3784226B1 (en) * 2018-04-24 2024-08-14 Translational Drug Development Llc Pyrazole-phenylamide derivatives as inhibitors of the rho-associated protein kinase rock1 and rock2 for the treatment of cancer
CN109020977B (zh) * 2018-10-26 2020-11-13 安庆奇创药业有限公司 一种Acalabrutinib的制备方法
JP2021050161A (ja) 2019-09-25 2021-04-01 武田薬品工業株式会社 複素環化合物及びその用途
WO2021073592A1 (zh) 2019-10-18 2021-04-22 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
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

Family Cites Families (192)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ246593A (en) 1992-02-05 1997-07-27 Boehringer Ingelheim Int Amidine derivatives; their preparation and medicaments containing them
ATE219766T1 (de) 1993-04-07 2002-07-15 Otsuka Pharma Co Ltd N-acylierte 4-aminopiperidin derivate als aktive bestandteile von peripher gefässerweiternden wikstoffen
HUT74450A (en) 1993-12-27 1996-12-30 Eisai Co Ltd Anthranilic acid derivative and pharmaceutical compns. contg. such compds.
GB9500580D0 (en) 1995-01-12 1995-03-01 Merck Sharp & Dohme Therapeutic agents
US5763618A (en) 1995-05-12 1998-06-09 Konica Corporation Manufacturing method of sulfides
DE19545878A1 (de) 1995-12-08 1997-06-12 Basf Ag Pyridylcarbamate, Verfahren und Zwischenprodukte zu ihrer Herstellung und ihre Verwendung
DK0892780T3 (da) 1996-02-22 2003-03-03 Bristol Myers Squibb Pharma Co m-Amidinophenylanaloger som faktor Xa-inhibitorer
EP0891343A1 (en) 1996-04-03 1999-01-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6020357A (en) 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
US6187797B1 (en) 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
WO1998028269A1 (en) 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
WO1998028282A2 (en) 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
EA200000048A1 (ru) 1997-06-19 2000-08-28 Дюпон Фармасьютикалз Компани ИНГИБИТОРЫ ФАКТОРА Ха, СОДЕРЖАЩИЕ ГРУППУ С НЕЙТРАЛЬНОЙ P1-СПЕЦИФИЧНОСТЬЮ
US6339099B1 (en) 1997-06-20 2002-01-15 Dupont Pharmaceuticals Company Guanidine mimics as factor Xa inhibitors
EP1000062B1 (en) 1997-07-30 2004-09-22 Wyeth Tricyclic vasopressin agonists
US6511974B1 (en) 1997-07-30 2003-01-28 Wyeth Tricyclic vasopressin agonists
AU8592598A (en) 1997-07-30 1999-02-22 Wyeth Tricyclic vasopressin agonists
AU3665199A (en) 1998-04-29 1999-11-16 Vertex Pharmaceuticals Incorporated Inhibitors of impdh enzyme
US6121271A (en) 1998-05-12 2000-09-19 American Home Products Corporation Naphtho[2,3-B]heteroar-4-yl derivatives
WO1999058522A1 (en) 1998-05-12 1999-11-18 American Home Products Corporation Naphtho[2,3-b]heteroar-4-yl derivatives
JP2000109465A (ja) 1998-08-05 2000-04-18 Nippon Soda Co Ltd フェニルピラゾ―ル化合物、製法及び抗高脂血症薬
AU1707700A (en) 1998-10-29 2000-05-22 Bristol-Myers Squibb Company Novel inhibitors of impdh enzyme
WO2000029399A1 (en) 1998-11-12 2000-05-25 Boehringer Ingelheim (Canada) Ltd. Antiherpes compounds
CN1347415A (zh) 1999-02-04 2002-05-01 美国家用产品公司 三环吡啶n-氧化物血管升压素激动剂
JP2000256358A (ja) 1999-03-10 2000-09-19 Yamanouchi Pharmaceut Co Ltd ピラゾール誘導体
ATE368037T1 (de) 1999-04-28 2007-08-15 Sanofi Aventis Deutschland Di-aryl-säurederivate als ppar rezeptor liganden
CN1391476A (zh) 1999-09-27 2003-01-15 美国氰胺公司 血管升压素激动剂制剂和方法
ES2293980T3 (es) 2000-01-13 2008-04-01 Amgen Inc. Agentes antibacterianos.
US6660885B2 (en) 2000-03-13 2003-12-09 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
MY138097A (en) 2000-03-22 2009-04-30 Du Pont Insecticidal anthranilamides
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
DE10063008A1 (de) 2000-12-16 2002-06-20 Merck Patent Gmbh Carbonsäureamidderivate
AU2002248432A1 (en) 2001-02-14 2002-08-28 Sankyo Company, Limited Oxazole derivatives, their preparation and their use as cytokine inhibitors
CA2437840A1 (en) 2001-03-05 2002-09-12 E.I. Du Pont De Nemours Heterocyclic diamide invertebrate pest control agents
DE10110749A1 (de) 2001-03-07 2002-09-12 Bayer Ag Substituierte Aminodicarbonsäurederivate
DE10111842A1 (de) 2001-03-13 2002-09-19 Boehringer Ingelheim Pharma Antithrombotische Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel
WO2002076959A1 (en) 2001-03-23 2002-10-03 Takeda Chemical Industries, Ltd. Five-membered heterocyclic alkanoic acid derivative
CA2447475A1 (en) 2001-05-25 2002-12-05 Chu-Biao Xue Hydantion derivatives as inhibitors of matrix metalloproteinases
DE10130374A1 (de) 2001-06-23 2003-01-02 Boehringer Ingelheim Pharma Substituierte N-Acyl-anilinderivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2003002561A1 (en) 2001-06-28 2003-01-09 Smithkline Beecham P.L.C. N-aroyl cyclic amine derivatives as orexin receptor antagonists
GB0115862D0 (en) 2001-06-28 2001-08-22 Smithkline Beecham Plc Compounds
WO2003004474A1 (en) 2001-07-06 2003-01-16 Syngenta Participations Ag Pesticidally active aminoacetonitriles
MXPA04001088A (es) 2001-08-03 2004-05-20 Vertex Pharma Derivados de pirazol como inhibidores de cinasa y uso de los mismos.
GB0124463D0 (en) 2001-10-11 2001-12-05 Smithkline Beecham Plc Compounds
SE0103644D0 (sv) 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic isoquinoline compounds
US6984735B2 (en) 2001-12-03 2006-01-10 Wyeth Process for making an aldehyde
WO2003079986A2 (en) 2002-03-18 2003-10-02 Bristol-Myers Squibb Company Uracil derivatives as inhibitors of tnf-alpha converting enzyme (tace) and matrix metalloproteinases
CA2479928A1 (en) 2002-03-28 2003-10-09 Neurogen Corporation Substituted biaryl amides as c5a receptor modulators
WO2004000788A1 (en) 2002-06-19 2003-12-31 Bristol-Myers Squibb Company Ureido-substituted aniline compounds useful as serine protease inhibitors
US20040044041A1 (en) 2002-08-06 2004-03-04 Kuduk Scott D. 2-(Biarylalkyl)amino-3-(cyanoalkanoylamino)pyridine derivatives
WO2004016592A1 (en) 2002-08-14 2004-02-26 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
US7041693B2 (en) 2002-10-04 2006-05-09 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
US20040082641A1 (en) 2002-10-28 2004-04-29 Rytved Klaus Asger Use of glycogen phosphorylase inhibitors for treatment of cardiovascular diseases
CA2505361A1 (en) 2002-11-11 2004-05-27 Bayer Healthcare Ag Phenyl or heteroaryl amino alkane derivatives as ip receptor antagonist
JP2004161716A (ja) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Jnk阻害剤
WO2004071426A2 (en) 2003-02-11 2004-08-26 Kemia Inc. Compounds for the treatment of viral infection
DE10306250A1 (de) 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
ATE384526T1 (de) 2003-04-14 2008-02-15 Inst For Pharm Discovery Inc N-(((((1,3-thiazol-2- yl)amino)carbonyl)phenyl)sulphonyl)phenylalanin derivate und verwandte verbindungen zur behandlung von diabetes
WO2005000813A1 (en) 2003-05-30 2005-01-06 Imclone Systems Incorporated Heteroarylamino-phenylketone derivatives and their use as kinase inhibitors
AU2004260758B2 (en) 2003-08-01 2007-06-07 Nippon Soda Co., Ltd. Phenylazole compounds, production process, and antioxidants
CA2536151A1 (en) 2003-08-21 2005-03-10 Osi Pharmaceuticals, Inc. N-substituted pyrazolyl-amidyl-benzimidazolyl c-kit inhibitors
US7485658B2 (en) 2003-08-21 2009-02-03 Osi Pharmaceuticals, Inc. N-substituted pyrazolyl-amidyl-benzimidazolyl c-Kit inhibitors
AU2004268621C1 (en) 2003-08-29 2011-08-18 Exelixis, Inc. c-Kit modulators and methods of use
WO2005023809A1 (en) 2003-09-10 2005-03-17 Virochem Pharma Inc. Spiro compounds and methods for the modulation of chemokine receptor activity
US7211671B2 (en) 2003-10-01 2007-05-01 Bristol Myers Squibb Company Substituted 1,3-dihydro-imidazol-2-one and 1,3-dihydro-imidazol-2-thione derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
DE602004021011D1 (de) 2003-10-08 2009-06-18 Lilly Co Eli Pyrrol- und pyrazolderivate als potentiatoren von glutamatrezeptoren
WO2005039494A2 (en) 2003-10-21 2005-05-06 Message Pharmaceuticals, Inc. Inhibitors of rnase p proteins as antibacterial compounds
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
EP1574502A1 (en) 2004-03-08 2005-09-14 Novartis AG Use of pyrimidine compounds in the preparation of parasiticides
WO2006028963A2 (en) 2004-09-03 2006-03-16 Celgene Corporation Substituted heterocyclic compounds and uses thereof
TW200630327A (en) 2004-10-28 2006-09-01 Inst For Pharm Discovery Inc Substituted phenylalkanoic acids
AU2005319455A1 (en) 2004-12-21 2006-06-29 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors
US8329703B2 (en) 2005-02-15 2012-12-11 Xtl Biopharmaceuticals Ltd. Pyrazole compounds
EP1863756A1 (en) 2005-03-24 2007-12-12 Janssen Pharmaceutica N.V. Biaryl derived amide modulators of vanilloid vr1 receptor
NZ564916A (en) 2005-06-27 2011-03-31 Exelixis Inc Imidazole based LXR modulators
FR2887548B1 (fr) 2005-06-27 2007-09-21 Sanofi Aventis Sa Derives de 4,5-diarylpyrrole, leur preparation et leur application en therapeutique
FR2888237B1 (fr) 2005-07-08 2007-08-31 Sanofi Aventis Sa Derives de n-[(4,5-diphenylpyrimidin-2-yl)methyl] amine, leur preparation et leur application en therapeutique
AR057450A1 (es) 2005-07-12 2007-12-05 Sanofi Aventis Derivados de n-[(1,2-difenil-1h-imidazol-4- il)metil]amina su preparacion y su aplicacion en terapeutica
US20090221547A1 (en) 2005-08-23 2009-09-03 Irm Llc Immunosuppressant Compounds and Compositions
US7906652B2 (en) 2005-11-28 2011-03-15 Merck Sharp & Dohme Corp. Heterocycle-substituted 3-alkyl azetidine derivatives
FR2894579B1 (fr) 2005-12-12 2008-01-18 Sanofi Aventis Sa Derives diaryltriazolmethylamine, leur preparation et leur application en therapeutique.
FR2894578B1 (fr) 2005-12-12 2008-02-01 Sanofi Aventis Sa Derives heterocycliques, leur preparation et leur application en therapeutique.
US20090042926A1 (en) 2005-12-20 2009-02-12 Jason Imbriglio Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment
EP1962830B1 (en) 2005-12-23 2013-03-27 GlaxoSmithKline LLC Azaindole inhibitors of aurora kinases
US20070265256A1 (en) 2006-02-21 2007-11-15 Arrington Mark P Phosphodiesterase 10 inhibitors
AU2012200157B2 (en) 2006-05-25 2014-08-21 Synta Pharmaceuticals Corp. Method for treating proliferative disorders associated with protooncogene products
WO2007146230A2 (en) 2006-06-14 2007-12-21 Merck & Co., Inc. Non-nucleoside reverse transcriptase inhibitors
US9108948B2 (en) 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
BRPI0713946A2 (pt) 2006-06-29 2012-12-04 Hoffmann La Roche compostos, composições farmacêuticas que os compreendem, método para o tratamento terapêutico e/ou profilático de enfermidades que são moduladas por agonistas de fxr, e uso dos compostos
EP2041116A1 (de) 2006-07-07 2009-04-01 Boehringer Ingelheim International GmbH Phenyl substituierte heteroaryl-derivate und deren verwendung als antitumormittel
WO2008016643A2 (en) 2006-08-01 2008-02-07 Cytokinetics, Incorporated Certain chemical entities, compositions, and methods
FR2904827B1 (fr) 2006-08-11 2008-09-19 Sanofi Aventis Sa Derives de 5,6-bisaryl-2-pyridine-carboxamide, leur preparation et leur application en therapeutique comme antiganistes des recepteurs a l'urotensine ii
EP2064213A1 (en) 2006-09-06 2009-06-03 F. Hoffmann-La Roche AG Heteroaryl derivatives as protein kinase inhibitors
WO2008057246A2 (en) 2006-10-26 2008-05-15 Synta Pharmaceuticals Corp. Method for treating inflammatory disorders
WO2008064317A1 (en) 2006-11-22 2008-05-29 University Of Medicine And Dentistry Of New Jersey Lipophilic opioid receptor active compounds
WO2008064318A2 (en) 2006-11-22 2008-05-29 University Of Medicine And Dentistry Of New Jersey Peripheral opioid receptor active compounds
WO2008064310A2 (en) 2006-11-22 2008-05-29 University Of Medicine And Dentistry Of New Jersey Mixed opioid receptor active compounds
ES2366980T3 (es) 2006-12-19 2011-10-27 F. Hoffmann-La Roche Ag Derivados de heteroaril-pirrolidinil- y - piperidinil-cetona.
CA2674237C (en) 2006-12-28 2015-11-24 Rigel Pharmaceuticals, Inc. N-substituted-heterocycloalkyloxybenzamide compounds and methods of use
FR2911136B1 (fr) 2007-01-05 2009-02-20 Sanofi Aventis Sa Derives de n-(4-cyano-1h-pyrazol-3-yl)methylamine substitues leur preparation et leur application en therapeutique.
AU2008205642B2 (en) 2007-01-12 2013-06-06 Msd K.K. Spirochromanon derivatives
TW200838516A (en) 2007-01-31 2008-10-01 Merck & Co Inc Substituted pyrano[2,3-B]pyridine derivatives as cannabinoid-1 receptor modulators
JP2008195655A (ja) 2007-02-14 2008-08-28 Kitasato Institute 糖尿病白内障の治療剤
WO2008137102A2 (en) 2007-05-04 2008-11-13 Torreypines Therapeutics, Inc. Methods of modulating amyloid beta and compounds useful therefor
EP1992625A1 (en) 2007-05-16 2008-11-19 Sanofi-Aventis Arylamide pyrimidone compounds
KR20100016617A (ko) 2007-05-18 2010-02-12 바이엘 쉐링 파마 악티엔게젤샤프트 과증식성 장애 및 혈관형성 관련 질환의 치료에 유용한 저산소증 유도성 인자 (hif)의 억제제
HRP20120240T1 (hr) 2007-05-23 2012-04-30 Merck Sharp & Dohme Corp. Piridil piperidin antagonisti receptora za oreksin
AR066834A1 (es) 2007-06-06 2009-09-16 Janssen Pharmaceutica Nv Espirobenzoazepanos como antagonistas de vasopresina, composiciones farmaceuticas que los contienen, proceso de preparacion y usos para el tratamiento de afecciones cardiacas, renales y del sistema nervioso central.
EP2002838A1 (de) 2007-06-13 2008-12-17 Bayer Schering Pharma AG Verwendung von Aryl/Hetarylamid-Derivaten als Modulatoren des EP2-Rezeptors
CA2690460A1 (en) 2007-06-15 2008-12-18 Markus Nett Method for producing difluoromethyl-substituted pyrazole compounds
US20100240657A1 (en) 2007-07-02 2010-09-23 Boehringer Ingelheim International Gmbh Chemical compounds
WO2009015208A1 (en) 2007-07-23 2009-01-29 Replidyne, Inc. Antibacterial amide and sulfonamide substituted heterocyclic urea compounds
EP2190466A4 (en) 2007-08-10 2011-12-21 Burnham Inst Medical Research Tissue-specific alkaline phosphatase (TNAP) activators and their use
EP2193119B1 (en) 2007-08-27 2014-01-01 Abbvie Deutschland GmbH & Co. KG 4-(4-pyridinyl)-benzamides and their use as rock activity modulators
WO2009036051A1 (en) 2007-09-10 2009-03-19 Curis, Inc. Bcl-2 inhibitors containing a zinc binding moiety
TW200920357A (en) 2007-09-10 2009-05-16 Curis Inc HSP90 inhibitors containing a zinc binding moiety
KR20090033583A (ko) 2007-10-01 2009-04-06 주식회사 엘지생명과학 글라이신 아릴 아마이드를 포함하는 신규한베타-세크리타제 저해용 화합물
WO2009052065A1 (en) 2007-10-17 2009-04-23 Sanofi-Aventis Substituted n-phenyl-bipyrrolidine carboxamides and therapeutic use thereof
TWI440638B (zh) 2007-10-30 2014-06-11 Otsuka Pharma Co Ltd 雜環化合物及其藥學組成物
US20100280049A1 (en) 2007-11-06 2010-11-04 Amira Pharmaceuticals, Inc. Antagonists of pgd2 receptors
WO2009076352A1 (en) 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
CA2709879A1 (en) * 2007-12-19 2009-06-25 The Scripps Research Institute Anilides and analogs as rho kinase inhibitors
JP2011507848A (ja) 2007-12-21 2011-03-10 ザ スクリプス リサーチ インスティチュート Rhoキナーゼインヒビターとしてのベンゾピランおよびアナログ
CN101538245B (zh) 2008-03-18 2011-02-16 中国科学院上海药物研究所 一类哒嗪酮类化合物及其制备方法和制备药物的用途
TW201000107A (en) 2008-04-09 2010-01-01 Infinity Pharmaceuticals Inc Inhibitors of fatty acid amide hydrolase
EP2269993B1 (en) 2008-04-23 2013-02-27 Kyowa Hakko Kirin Co., Ltd. 2-aminoquinazoline derivative
JP2011523633A (ja) 2008-05-08 2011-08-18 ブリストル−マイヤーズ スクイブ カンパニー 2−アリールグリシンアミド誘導体
CN101597278B (zh) 2008-06-04 2013-04-17 中国中化股份有限公司 酰胺类化合物及其制备与应用
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8623238B2 (en) 2008-06-27 2014-01-07 Transitions Optical, Inc. Mesogenic stabilizers
NZ589843A (en) 2008-06-27 2012-12-21 Avila Therapeutics Inc Pyrimidine heteroaryl compounds and uses thereof as protein kinase inhibitors
WO2010036316A1 (en) 2008-09-24 2010-04-01 Yangbo Feng Urea and carbamate compounds and analogs as kinase inhibitors
CA2739303A1 (en) 2008-10-01 2010-04-08 Synta Pharmaceuticals Corp. Compounds for inflammation and immune-related uses
WO2010040274A1 (zh) 2008-10-10 2010-04-15 中国人民解放军军事医学科学院毒物药物研究所 新型多巴胺d3受体配体,其制备方法及其医药用途
EP2375904B1 (en) 2008-12-09 2014-05-28 Merck Sharp & Dohme Corp. Biaryl carboxamides
US8609696B2 (en) 2008-12-18 2013-12-17 Boehringer Ingelheim International Gmbh Serotonin 5-HT2B receptor inhibitors
WO2010075290A1 (en) 2008-12-22 2010-07-01 President And Fellows Of Harvard College Unsaturated heterocyclic inhibitors of necroptosis
WO2010093849A2 (en) 2009-02-13 2010-08-19 Amgen Inc. Phenylalanine amide derivatives useful for treating insulin-related diseases and conditions
JP5688918B2 (ja) 2009-04-28 2015-03-25 大塚製薬株式会社 医薬組成物
WO2010129848A2 (en) 2009-05-08 2010-11-11 Takeda Pharmaceutical Company Limited 2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxamides
CA2765053C (en) 2009-06-09 2015-08-18 California Capital Equity, Llc Isoquinoline, quinoline, and quinazoline derivatives as inhibitors of hedgehog signaling
TW201103904A (en) * 2009-06-11 2011-02-01 Hoffmann La Roche Janus kinase inhibitor compounds and methods
CA2773561A1 (en) 2009-09-14 2011-03-17 Phusis Therapeutics Inc. Pharmaceutical compositions and formulations including inhibitors of the pleckstrin homology domain and methods for using same
US20110082098A1 (en) 2009-09-30 2011-04-07 University Of Kansas Novobiocin analogues and treatment of polycystic kidney disease
US8377970B2 (en) 2009-10-08 2013-02-19 Rhizen Pharmaceuticals Sa Modulators of calcium release-activated calcium channel
US8993612B2 (en) 2009-10-08 2015-03-31 Rhizen Pharmaceuticals Sa Modulators of calcium release-activated calcium channel and methods for treatment of non-small cell lung cancer
US20120225900A1 (en) 2009-11-10 2012-09-06 Pfizer Inc. N2-pyrazolospiroketone acetyl-coa carboxylase inhibitors
CU24077B1 (es) 2009-11-10 2015-03-30 Pfizer DERIVADOS DE N1-PIRAZOLOESPIROCETONA ÚTILES COMO INHIBIDORES DE ACETIL-CoA CARBOXILASA
US8394858B2 (en) 2009-12-03 2013-03-12 Novartis Ag Cyclohexane derivatives and uses thereof
ES2655091T3 (es) 2009-12-18 2018-02-16 Ogeda Sa Derivados del ácido pirrolidíncarboxílico como agonistas del receptor 43 acoplado a proteína G (GPR43), composición farmacéutica y métodos para su uso en el tratamiento de trastornos metabólicos
JP2013047188A (ja) 2009-12-24 2013-03-07 Nippon Chemiphar Co Ltd Gpr119作動薬
KR101781663B1 (ko) 2010-01-13 2017-09-25 템페로 파마슈티칼즈, 인크. 히스톤 데아세틸라제 효소를 억제하기 위한 화합물 및 이를 제조하는 방법
WO2011088031A1 (en) 2010-01-13 2011-07-21 Glaxosmithkline Llc Compounds and methods
AU2011205485B2 (en) 2010-01-13 2014-09-25 Glaxosmithkline Llc Compounds and methods
CN102971304A (zh) 2010-02-01 2013-03-13 日本化学医药株式会社 Gpr119激动剂
EP2535059A4 (en) 2010-02-10 2014-03-12 Public Univ Corp Yokohama City USE OF A MSIN3B BINDING COMPOUND FOR SPECIFIC BINDING TO THE NEURONIC RESTRICTIVE SILENCER FACTOR (NRSF)
WO2011106632A1 (en) 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
US8354410B2 (en) 2010-03-11 2013-01-15 Bristol-Meyers Squibb Company Compounds for the treatment of hepatitis C
JP2013522192A (ja) 2010-03-11 2013-06-13 ブリストル−マイヤーズ スクイブ カンパニー C型肝炎の処置のための化合物
WO2011140425A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
WO2011156557A2 (en) 2010-06-11 2011-12-15 Thomas James B Compounds active at the neurotensin receptor
US8697911B2 (en) 2010-07-07 2014-04-15 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
US9079880B2 (en) 2010-07-07 2015-07-14 Boehringer Ingelheim International Gmbh Rho kinase inhibitors
BR112013003864B1 (pt) 2010-08-20 2021-08-31 Hutchison Medipharma Limited Compostos de pirrolpirimidina, composição e uso dos mesmos
WO2012040444A2 (en) 2010-09-24 2012-03-29 Bristol-Myers Squibb Company Treatment of patients with incipient alzheimer's disease
WO2012051117A2 (en) 2010-10-11 2012-04-19 The Board Of Trustees Of The Leland Stanford Junior University Substituted benzamides and their uses
CN102451178A (zh) 2010-10-29 2012-05-16 中国科学院上海药物研究所 二氢呋喃-2-酮类化合物在制备抗糖尿病及糖脂代谢药物中的用途
US20120129843A1 (en) 2010-11-18 2012-05-24 Yan Zhang Pyridyl-thiazolyl inhibitors of pro-matrix metalloproteinase activation
CN103328492A (zh) 2010-11-22 2013-09-25 阿勒根公司 作为受体调节剂具有疗效的新型化合物
EP2457900A1 (en) 2010-11-25 2012-05-30 Almirall, S.A. New pyrazole derivatives having CRTh2 antagonistic behaviour
WO2012074068A1 (ja) 2010-12-01 2012-06-07 日産化学工業株式会社 ピラゾール化合物による造血幹細胞の製造方法
RU2583430C2 (ru) 2010-12-01 2016-05-10 Ниссан Кемикал Индастриз, Лтд. Пиразольные соединения, обладающие терапевтическим эффектом на множественную миелому
CA2820817A1 (en) 2010-12-07 2012-06-14 Amira Pharmaceuticals, Inc. Lysophosphatidic acid receptor antagonists and uses thereof
GB201021104D0 (en) 2010-12-13 2011-01-26 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
RU2634900C2 (ru) 2011-02-02 2017-11-08 Вертекс Фармасьютикалз Инкорпорейтед Спироциклические пирролопиразин(пиперидин)амиды в качестве модуляторов ионных каналов
GB201104267D0 (en) 2011-03-14 2011-04-27 Cancer Rec Tech Ltd Pyrrolopyridineamino derivatives
BR112013024907A2 (pt) 2011-03-28 2016-12-20 Mei Pharma Inc composto, composição farmacêutica, método para o tratamento, prevenção ou atenuação de um ou mais sintomas de um distúrbio, doença ou condição mediada por pi3k em um sujeito, método para modular a atividade enzimática de pi3k
WO2012135697A2 (en) 2011-03-30 2012-10-04 H. Lee Moffitt Cancer Center & Research Institute Inc. Novel rho kinase inhibitors and methods of use
GB201107223D0 (en) 2011-04-29 2011-06-15 Amakem Nv Novel rock inhibitors
AP3308A (en) 2011-05-26 2015-06-30 Tfchem Family of aryl, heteroaryl, O-aryl and O-heteroaryl carbasugars
EP2714688B1 (en) 2011-05-26 2016-02-24 Daiichi Sankyo Company, Limited Heterocyclic compounds as protein kinase inhibitors
US8686184B2 (en) 2011-05-31 2014-04-01 Theravance, Inc. Neprilysin inhibitors
MX2014000374A (es) 2011-07-12 2014-03-21 Hoffmann La Roche Compuesto de aminometil quinolona.
WO2013018526A1 (ja) 2011-07-29 2013-02-07 日本ゼオン株式会社 光学異方体の波長分散調整方法及び重合性組成物
WO2013067248A1 (en) 2011-11-04 2013-05-10 Vertex Pharmaceuticals Incorporated Benzoxazines as modulators of ion channels
BR112015003376A8 (pt) 2012-08-23 2018-01-23 Alios Biopharma Inc composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica e usos de quantidade eficiente de composto ou sal farmaceuticamente aceitável do mesmo ou composição farmacêutica
WO2014079850A1 (en) * 2012-11-23 2014-05-30 F. Hoffmann-La Roche Ag Substituted heterocyclic derivatives
JP6488239B2 (ja) 2013-01-18 2019-03-20 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのフタラジノンおよびイソキノリノン
JP6423372B2 (ja) 2013-02-28 2018-11-14 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
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
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
KR101861942B1 (ko) 2014-01-20 2018-06-29 에프. 호프만-라 로슈 아게 신경 발생을 자극할 수 있는 n-페닐-락탐 유도체 및 이의 신경 장애 치료에서의 용도

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