PE20011047A1 - Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas - Google Patents

Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas

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Publication number
PE20011047A1
PE20011047A1 PE2001000042A PE2001000042A PE20011047A1 PE 20011047 A1 PE20011047 A1 PE 20011047A1 PE 2001000042 A PE2001000042 A PE 2001000042A PE 2001000042 A PE2001000042 A PE 2001000042A PE 20011047 A1 PE20011047 A1 PE 20011047A1
Authority
PE
Peru
Prior art keywords
heteroaryl
proteinkinases
inhibit
compound
alkyl
Prior art date
Application number
PE2001000042A
Other languages
English (en)
Inventor
Steven Lee Bender
Dilip Bhumralkar
Michael Raymond Collins
Stephan James Cripps
Michael David Varney
Lei Jia
Mitchell David Nambu
Cynthia Louise Palmer
Zhengwei Peng
Judith Gail Deal
Original Assignee
Agouron Pharma
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 Agouron Pharma filed Critical Agouron Pharma
Publication of PE20011047A1 publication Critical patent/PE20011047A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30Oxygen atoms
    • 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
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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
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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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    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic 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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38Nitrogen atoms
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    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
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    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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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    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D401/06Heterocyclic 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 only aliphatic carbon atoms
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    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • C07D487/04Ortho-condensed systems

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES UNA FRACCION DEL GRUPO a; DONDE Z ES CH, NH; Q ES UNA FRACCION DE MANERA QUE R1 ES UN HETEROARILO; X ES CH2, O, S, NH; Y ES CH2, O, S CON LA CONDICION QUE POR LO MENOS UNO DE X E Y ES CH2 O QUE X E Y JUNTOS FORMEN UN CICLOROPILO; R2 Y R3 SON H, METILO HALOGENO, TRIFLUOROMETILO, CIANO; R4 ES O=C-NH-R5, -NH-(CO)-R6; DONDE R5 ES UN ARILO HETEROARILO, CICLOALQUILO HETEROCICLOALQUILO, O-R7, NR8R9, ALQUILO C1-C8, ENTRE OTROS; R6 ES ARILO , HETEROARILO, ENTRE OTROS; R7 ES ALQUILO, CICLOALQUILO, HETEROCICLOALQUILO, ARILO, ENTRE OTROS; R8 ES H, ALQUILO; R9 ES ALQUILO, ARILO, HETEROARILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. LOS COMPUESTOS DE FORMULA I REGULAN O INHIBEN LA ACTIVIDAD DE LAS PROTEINQUINASAS Y SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES ASOCIADAS A CRECIMIENTO TUMORAL, PROLIFERACION CELULAR O ANGIOGENESIS
PE2001000042A 2000-01-21 2001-01-17 Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas PE20011047A1 (es)

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US (2) US6635641B2 (es)
EP (1) EP1252146A1 (es)
JP (1) JP2003529558A (es)
AR (1) AR029222A1 (es)
AU (1) AU2001234484A1 (es)
BR (1) BR0108025A (es)
CA (1) CA2394703A1 (es)
CO (1) CO5280047A1 (es)
GT (1) GT200100014A (es)
HN (1) HN2001000008A (es)
MX (1) MXPA02007102A (es)
PA (1) PA8510201A1 (es)
PE (1) PE20011047A1 (es)
WO (1) WO2001053274A1 (es)

Families Citing this family (103)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1147214B1 (en) 1999-01-13 2011-01-05 The Research Foundation Of State University Of New York A novel method for designing protein kinase inhibitors
WO2001024796A1 (en) * 1999-10-01 2001-04-12 Smithkline Beecham Corporation 1,2,4-triazole derivatives, composition, process of making and methods of use
DE10021246A1 (de) * 2000-04-25 2001-10-31 Schering Ag Substituierte Benzoesäureamide und deren Verwendung als Arzneimittel
CA2462442A1 (en) * 2001-10-12 2003-04-24 Warner-Lambert Company Llc Alkyne matrix metalloproteinase inhibitors
CA2464214C (en) * 2001-10-22 2011-02-08 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors, methods for designing them, and methods of using them
US7005445B2 (en) 2001-10-22 2006-02-28 The Research Foundation Of State University Of New York Protein kinase and phosphatase inhibitors and methods for designing them
AU2002353147A1 (en) * 2001-12-13 2003-06-30 Abbott Laboratories 3-(phenyl-alkoxy)-5-(phenyl)-pyridine derivatives and related compounds as kinase inhibitors for the treatment of cancer
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
JP2005538975A (ja) * 2002-07-03 2005-12-22 アステックス テクノロジー リミテッド p38MAPキナーゼ阻害薬としての3−(ヘテロ)アリールメトキシピリジン類およびそれらの類縁体
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
AU2003250701A1 (en) 2002-07-31 2004-02-16 Wayne R. Danter Protein tyrosine kinase inhibitors
WO2004033446A1 (en) * 2002-10-09 2004-04-22 Danter Wayne R Protein tyrosine kinase inhibitors
CN1506359A (zh) * 2002-12-05 2004-06-23 �й�ҽѧ��ѧԺҩ���о��� 新的香豆素酰胺衍生物及其制法和其药物组合物与用途
EP2397462A3 (en) * 2003-01-14 2012-04-04 Cytokinetics, Inc. Compounds, compositions and methods of treatment for heart failure
AP2114A (en) * 2003-02-26 2010-03-04 Sugen Inc Aminoheteroaryl compounds as protein kinase inhibitors
US7078419B2 (en) 2003-03-10 2006-07-18 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
EP1618133A1 (en) * 2003-04-17 2006-01-25 Pfizer Inc. Crystal structure of vegfrkd: ligand complexes and methods of use thereof
CN1816529A (zh) 2003-05-01 2006-08-09 布里斯托尔-迈尔斯.斯奎布公司 用作激酶抑制剂的芳基取代的吡唑-酰胺化合物
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
KR101204247B1 (ko) 2003-07-22 2012-11-22 아스텍스 테라퓨틱스 리미티드 3,4-이치환된 1h-피라졸 화합물 및 그의 시클린 의존성키나제 (cdk) 및 글리코겐 합성효소 키나제-3(gsk-3) 조정제로서 용도
US20050182061A1 (en) * 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
DE102004009238A1 (de) * 2004-02-26 2005-09-08 Merck Patent Gmbh Arylamid-Derivate
US7297817B2 (en) * 2004-04-13 2007-11-20 Cephalon France Thio-substituted arylmethanesulfinyl derivatives
JPWO2005108370A1 (ja) * 2004-04-16 2008-03-21 味の素株式会社 ベンゼン化合物
KR101276136B1 (ko) 2004-06-17 2013-06-18 싸이토키네틱스, 인코포레이티드 화합물, 조성물 및 방법
US7776869B2 (en) * 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
US7947682B2 (en) * 2004-12-29 2011-05-24 University Of Southern California Substituted N′-pyrrolo[1,2-a]quinoxalin-4-yl-hydrazides as anti-cancer agents
EP2395000A1 (en) 2004-12-30 2011-12-14 Astex Therapeutics Limited Benzimidazole compounds that modulate the activity of CDK, GSK and aurora kinases
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
CA2594477C (en) 2005-01-21 2016-07-12 Astex Therapeutics Limited Pharmaceutical compounds
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
EP1845974A1 (en) 2005-01-21 2007-10-24 Astex Therapeutics Limited Pharmaceutical compounds
DE602006018590D1 (de) 2005-03-29 2011-01-13 Icos Corp Heteroarylharnstoffderivate zur hemmung von chk1
WO2006110477A2 (en) * 2005-04-07 2006-10-19 Astrum Therapeutics Pty. Ltd. Compounds to treat amyloidosis and prevent death of beta-cells in type 2 diabetes mellitus
EP1879884B1 (en) * 2005-05-03 2010-08-25 Ranbaxy Laboratories Limited Azole-based phosphodiesterase inhibitors
GT200600207A (es) * 2005-06-09 2007-01-15 Novartis Ag Proceso para la síntesis de compuestos orgánicos
AU2013205820B2 (en) * 2005-06-09 2015-11-26 Novartis Ag Process for the synthesis of organic compounds
MY146795A (en) * 2005-06-09 2012-09-28 Novartis Ag Process for the synthesis of organic compounds
EP1910297B1 (en) 2005-07-11 2016-05-25 Aerie Pharmaceuticals, Inc. Isoquinoline compounds
US7538223B2 (en) 2005-08-04 2009-05-26 Cytokinetics, Inc. Compounds, compositions and methods
TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
US7825120B2 (en) * 2005-12-15 2010-11-02 Cytokinetics, Inc. Certain substituted ((piperazin-1-ylmethyl)benzyl)ureas
US20070161617A1 (en) 2005-12-15 2007-07-12 Morgan Bradley P Certain chemical entities, compositions and methods
WO2007078815A2 (en) 2005-12-16 2007-07-12 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
JP5178526B2 (ja) 2005-12-19 2013-04-10 サイトキネティクス・インコーポレーテッド 化合物、組成物および方法
AU2006331673B2 (en) * 2005-12-23 2013-02-28 Ariad Pharmaceuticals, Inc. Bicyclic heteroaryl compounds
CA2635760C (en) * 2005-12-28 2014-07-15 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US7671221B2 (en) 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
EA200870515A1 (ru) 2006-05-08 2009-06-30 Ариад Фармасьютикалз, Инк. Моноциклические гетероарильные соединения
WO2007133560A2 (en) * 2006-05-08 2007-11-22 Ariad Pharmaceuticals, Inc. Acetylenic heteroaryl compounds
US7838542B2 (en) 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade
ES2729424T3 (es) 2006-09-20 2019-11-04 Aerie Pharmaceuticals Inc Inhibidores de Rho cinasa
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
PT2848610T (pt) * 2006-11-15 2017-11-14 Ym Biosciences Australia Pty Inibidores da atividade de quinases
AU2013273769B2 (en) * 2006-11-15 2016-05-12 Ym Biosciences Australia Pty Ltd Inhibitors of Kinase Activity
CN101627027B (zh) * 2007-01-05 2013-06-19 百时美施贵宝公司 氨基吡唑激酶抑制剂
US8455513B2 (en) 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8034815B2 (en) 2007-01-11 2011-10-11 Critical Outcome Technologies, Inc. Compounds and method for treatment of cancer
EP2070929A1 (en) * 2007-12-11 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
EP2225226B1 (en) 2007-12-26 2016-08-17 Critical Outcome Technologies, Inc. Compounds and their use in a method for treatment of cancer
US8513287B2 (en) 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
US8455514B2 (en) 2008-01-17 2013-06-04 Aerie Pharmaceuticals, Inc. 6-and 7-amino isoquinoline compounds and methods for making and using the same
WO2009100536A1 (en) * 2008-02-15 2009-08-20 Methylgene Inc. Inhibitors of kinase activity with 1,2-di-cyclyl substituted alkyne structures
AU2009261683A1 (en) * 2008-06-19 2009-12-23 Astrazeneca Ab Pyrazole compounds 436
EP2318406B1 (en) 2008-07-17 2016-01-27 Critical Outcome Technologies, Inc. Thiosemicarbazone inhibitor compounds and cancer treatment methods
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
JP5424187B2 (ja) * 2008-08-27 2014-02-26 学校法人 関西大学 アシルアミノフェニル基を有する抗がん剤
AU2009305624A1 (en) * 2008-10-17 2010-04-22 Exelixis, Inc. Sphingosine-1-phosphate receptor antagonists
US8846664B2 (en) 2008-11-12 2014-09-30 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
CA2760562C (en) 2009-05-01 2016-07-19 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
CA2999435A1 (en) 2010-04-01 2011-10-06 Critical Outcome Technologies Inc. Compounds and method for treatment of hiv
WO2012112567A1 (en) * 2011-02-15 2012-08-23 Georgetown University Small molecule inhibitors of agbl2
WO2013022766A1 (en) 2011-08-05 2013-02-14 Flynn Gary A Preparation and methods of use for ortho-aryl 5- membered heteroaryl-carboxamide containing multi-targeted kinase inhibitors
CN103664924B (zh) * 2012-09-18 2015-12-02 江西天新药业有限公司 3-[(4-氨基-2-甲基-5-嘧啶基)甲基]-5-(2-氯乙基)-4-甲基噻唑的制备方法
CA3167093A1 (en) 2012-12-12 2014-06-12 Ariad Pharmaceuticals, Inc. Crystalline form c of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride
US9815815B2 (en) 2013-01-10 2017-11-14 Pulmokine, Inc. Non-selective kinase inhibitors
JP5934658B2 (ja) * 2013-01-29 2016-06-15 Jxエネルギー株式会社 イミド−ウレア化合物及びその製造方法、グリース用増ちょう剤並びにグリース組成物
WO2014121883A1 (en) * 2013-02-07 2014-08-14 Merck Patent Gmbh Substituted acetylene derivatives and their use as positive allosteric modulators of mglur4
CN105263494A (zh) 2013-03-15 2016-01-20 爱瑞制药公司 联合治疗
CA2926793C (en) 2013-10-11 2022-11-22 Lawrence S. ZISMAN Spray-dry formulations for treating pulmonary arterial hypertension
EP3068758B1 (en) 2013-11-15 2021-09-08 The Wistar Institute Of Anatomy And Biology Ebna1 inhibitors and their method of use
EA032355B1 (ru) * 2013-12-24 2019-05-31 Онкотартис, Инк. Бензамидные и никотинамидные соединения и способы их применения
WO2015143654A1 (en) * 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
CN106146391A (zh) * 2015-04-15 2016-11-23 中国科学院上海药物研究所 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途
JP6771491B2 (ja) 2015-05-14 2020-10-21 ザ ウィスター インスティテュート オブ アナトミー アンド バイオロジー Ebna1阻害剤およびその使用方法
US9951019B2 (en) * 2015-06-26 2018-04-24 Regents Of The University Of Minnesota Therapeutic compounds
US9643927B1 (en) 2015-11-17 2017-05-09 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
US10550087B2 (en) 2015-11-17 2020-02-04 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
BR112019003945A2 (pt) 2016-08-31 2019-05-21 Aerie Pharmaceuticals, Inc. composições oftálmicas
WO2018068739A1 (zh) * 2016-10-13 2018-04-19 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白激酶活性的炔基杂环类化合物
BR112019008622A2 (pt) 2016-10-27 2019-07-09 Pulmokine Inc método para tratar uma condição
CN110506037A (zh) 2017-03-31 2019-11-26 爱瑞制药公司 芳基环丙基-氨基-异喹啉酰胺化合物
CN112543634A (zh) 2018-05-17 2021-03-23 威斯达研究所 Ebna1抑制剂晶体形式及其制备和使用方法
US20210246120A1 (en) * 2018-08-24 2021-08-12 Biomedical Research Foundation Of The Academy Of Athens (Brfaa) Method of preparation and use of phosphoinositide 3-kinase inhibitors in treating cancer
WO2020056345A1 (en) 2018-09-14 2020-03-19 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
EP3936192A4 (en) 2019-03-06 2022-11-16 Daiichi Sankyo Company, Limited PYRROLOPYRAZOL DERIVATIVES
WO2020206583A1 (en) * 2019-04-08 2020-10-15 Qilu Regor Therapeutics Inc. Kinase inhibitors and uses thereof
JP2022537833A (ja) * 2019-06-24 2022-08-30 ベネボレントエーアイ バイオ リミティド 新規化合物と方法
CA3147407A1 (en) * 2019-07-25 2021-01-28 Curadev Pharma Pvt. Ltd. Small molecule inhibitors of acetyl coenzyme a synthetase short chain 2 (acss2)
AU2020320195A1 (en) * 2019-07-30 2022-03-10 Nurix Therapeutics, Inc. Urea, amide, and substituted heteroaryl compounds for Cbl-b inhibition
CN113754541A (zh) * 2020-06-02 2021-12-07 深圳湾实验室 靶向eb病毒核抗原蛋白的小分子抑制剂、制备方法及其应用
US11629143B2 (en) 2020-10-01 2023-04-18 Vibliome Therapeutics, Llc HipK4 inhibitors and uses thereof

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH575397A5 (es) 1971-11-09 1976-05-14 Basf Ag
DE3148291A1 (de) * 1981-12-05 1983-06-09 Basf Ag, 6700 Ludwigshafen Harnstoffderivate, verfahren zu ihrer herstellung und ihre verwendung zur bekaempfung unerwuenschten pflanzenwuchses
IE58870B1 (en) * 1985-03-08 1993-11-17 Leo Pharm Prod Ltd Pyridine derivatives
JPH083564B2 (ja) 1986-07-25 1996-01-17 三菱化学株式会社 偏光フィルム
US5612360A (en) 1992-06-03 1997-03-18 Eli Lilly And Company Angiotensin II antagonists
WO1994014780A1 (en) 1992-12-18 1994-07-07 The Wellcome Foundation Limited Pyrimidine, pyridine, pteridinone and indazole derivatives as enzyme inhibitors
US5625031A (en) 1994-02-08 1997-04-29 Bristol-Myers Squibb Company Peptide inhibitors of the p33cdk2 and p34cdc2 cell cycle regulatory kinases and human papillomavirus E7 oncoprotein
US5631156A (en) 1994-06-21 1997-05-20 The University Of Michigan DNA encoding and 18 KD CDK6 inhibiting protein
DE69532817T2 (de) 1994-11-10 2005-01-13 Millenium Pharmaceuticals, Inc., Cambridge Verwendung von pyrazole verbindungen zur behandlung von glomerulonephritis, krebs, atherosklerose oder restenose
TR199700749T1 (xx) 1995-02-02 1998-02-21 Smithkline Beecham P.L.C. 5-HT resept�r antagonisti olarak indole t�revleri.
EP0731385B1 (en) * 1995-03-09 2003-08-27 Agfa-Gevaert New photographic useful group releasing system
EP0817630A4 (en) 1995-03-29 1999-01-27 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
WO1997003967A1 (en) 1995-07-22 1997-02-06 Rhone-Poulenc Rorer Limited Substituted aromatic compounds and their pharmaceutical use
US5705499A (en) * 1995-10-06 1998-01-06 Boehringer Ingelheim Pharmaceuticals, Inc. 8-arylalkyl- and 8-arylheteroalkyl-5,11-dihydro-6H-dipyrido 3,2-B:2',3'-e! 1!diazepines and their use in the treatment of HIV-1 infection
US5733920A (en) 1995-10-31 1998-03-31 Mitotix, Inc. Inhibitors of cyclin dependent kinases
US6495526B2 (en) 1996-01-23 2002-12-17 Gpc Biotech, Inc. Inhibitors of cell-cycle progression and uses related thereto
US6514971B1 (en) 1996-03-15 2003-02-04 Zeneca Limited Cinnoline derivatives and use as medicine
US5849733A (en) 1996-05-10 1998-12-15 Bristol-Myers Squibb Co. 2-thio or 2-oxo flavopiridol analogs
US5821243A (en) 1996-07-22 1998-10-13 Viropharma Incorporated Compounds compositions and methods for treating influenza
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
EP0964864B1 (en) 1997-02-05 2008-04-09 Warner-Lambert Company LLC Pyrido 2,3-d pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
WO1998038168A1 (en) 1997-02-27 1998-09-03 Tanabe Seiyaku Co., Ltd. Isoquinolinone derivatives, process for preparing the same, and their use as phosphodiesterase inhibitors
EP1017394B1 (en) 1997-07-12 2005-12-07 Cancer Research Technology Limited Cyclin dependent kinase inhibiting purine derivatives
FR2767827A1 (fr) 1997-09-03 1999-02-26 Adir Nouveaux derives de l'indole et de l'indazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
JP2001518501A (ja) 1997-10-06 2001-10-16 ビーエーエスエフ アクチェンゲゼルシャフト インデノ[1,2−c]−、ナフト[1,2−c]−およびベンゾ[6,7]シクロへプタ[1,2−c]ピラゾール誘導体
ID24372A (id) 1997-10-27 2000-07-13 Agouron Pharma SENYAWA-SENYAWA 4-AMINO-TIAZOL-2-IL SEBAGAI PENGHAMBAT-PENGHAMBAT CDKs
JP2001521926A (ja) 1997-11-04 2001-11-13 ファイザー・プロダクツ・インク 治療上活性の化合物におけるカテコールのインダゾール生物学的等価物置換
US6040321A (en) 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US6479487B1 (en) 1998-02-26 2002-11-12 Aventis Pharmaceuticals Inc. 6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines
JP2002504553A (ja) 1998-02-26 2002-02-12 アベンティス・ファーマスーティカルズ・インコーポレイテツド 6,9−ジ置換2−[トランス−(4−アミノシクロヘキシル)アミノ]プリン
AU739403B2 (en) 1998-02-27 2001-10-11 Pfizer Products Inc. N-((substituted five-membered di- or triaza diunsaturated ring)carbonyl) guanidine derivatives for the treatment of ischemia
WO1999059959A1 (en) * 1998-05-15 1999-11-25 Astrazeneca Ab Benzamide derivatives for the treatment of diseases mediated by cytokines

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