HUP0105113A2 - Benzoheterociklusos vegyületek és MEK inhibitorokként történő alkalmazásuk és a vegyületeket tartalmazó gyógyászati készítmények - Google Patents

Benzoheterociklusos vegyületek és MEK inhibitorokként történő alkalmazásuk és a vegyületeket tartalmazó gyógyászati készítmények

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Publication number
HUP0105113A2
HUP0105113A2 HU0105113A HUP0105113A HUP0105113A2 HU P0105113 A2 HUP0105113 A2 HU P0105113A2 HU 0105113 A HU0105113 A HU 0105113A HU P0105113 A HUP0105113 A HU P0105113A HU P0105113 A2 HUP0105113 A2 HU P0105113A2
Authority
HU
Hungary
Prior art keywords
alkyl
cycloalkyl
group
phenyl
heterocyclyl
Prior art date
Application number
HU0105113A
Other languages
English (en)
Inventor
Stephen Douglas Barrett
Alexander James Bridges
Haile Tecle
Original Assignee
Warner-Lambert Co.
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Publication date
Application filed by Warner-Lambert Co. filed Critical Warner-Lambert Co.
Publication of HUP0105113A2 publication Critical patent/HUP0105113A2/hu
Publication of HUP0105113A3 publication Critical patent/HUP0105113A3/hu

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    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/12—Radicals substituted by oxygen atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
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    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/18—Benzotriazoles
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
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    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
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    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/14—Thiadiazoles; Hydrogenated thiadiazoles condensed with carbocyclic rings or ring systems

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Heart & Thoracic Surgery (AREA)
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  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)

Abstract

A tal lm ny MEK inhibitorokként proliferatív betegségek kezelésérefelhaszn lható (I) ltal nos képletű vegyületekre - amelyek képletébenW -OR1, -NR2OR1, -NRARB, -NR2NRARB, -O(CH2)2-4NRARB vagy -NR2(CH2)2-4NRARB csoport, R1 hidrogénatom, alkil-, alkenil-, alkinil-,cikloalkil-, fenil-, fenil-alkil-, fenil-alkenil-, fenil-alkinil-,cikloalkil-alkil-, cikloalkil-alkenil-, cikloalkil-alkinil-,heterociklil-, heterociklil-alkil-, heterociklil-alkenil-,heterociklil-alkinil- vagy -(CH2)2-4NRCRD csoport, R2 hidrogénatom,alkil-, fenil-, cikloalkil-, heterociklil vagy heterociklil-metilcsoport, RA jelentése hidrogénatom, alkil-, alkenil-, alkinil-,cikloalkil-, fenil-, cikloalkil-alkil-, cikloalkil-alkenil-,cikloalkil-alkinil-, heterociklil-, heterociklil-alkil-, szulfamoil-fenil-, (szulfamoil-fenil)-alkil-, szulfamoil -alkil-, szulfamoil-cikloalkil-, (szulfamoil-cikloalkil)-alkil- vagy -(CH2)2-4NRCRDcsoport, RB hidrogénatom, alkil-, alkenil-, alkinil-, cikloalkil- vagyfenilcsoport, Q (i), (ii) vagy (iii) ltal nos képletű csoport, R3hidrogén- vagy fluoratom, R4 halogénatom, nitro-, -SO2NRO(CH2)2-4NRERF, -SO2NRERF vagy -(CO)T képletű csoport, T alkil-, cikloalkil-,(RERFN)-(alkil)- -ORF, -NRO (CH2) 2-4-NRERF vagy -NRERF csoport, adottesetben helyettesített 5-6 tagú heterogyűrű, amely heteroatomkéntnitrogén-, kén- vagy oxigénatomot tartalmazhat. R10 és R11hidrogénatom, metilcsoport, halogénatom vagy nitrocsoport, aholvalamennyi fenti szénhidrogén vagy heterociklusos adott esetbenlegfeljebb h romszorosan szubsztitu lt lehet vagy gyógy szatilagelfogadható sóikra és észtereikre vonatkozik. A tal lm ny t rgya tovbb az (I) ltal nos képletű vegyületeket tartalmazó gyógy szatikészítményekre is kiterjed. Ó
HU0105113A 1999-01-13 1999-12-21 Benzoheterocycles and their use as mek inhibitors and pharmaceutical compositions containing the compounds HUP0105113A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11587399P 1999-01-13 1999-01-13
US12255399P 1999-03-02 1999-03-02
PCT/US1999/030483 WO2000042022A1 (en) 1999-01-13 1999-12-21 Benzoheterocycles and their use as mek inhibitors

Publications (2)

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HUP0105113A2 true HUP0105113A2 (hu) 2002-04-29
HUP0105113A3 HUP0105113A3 (en) 2004-11-29

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HU0105113A HUP0105113A3 (en) 1999-01-13 1999-12-21 Benzoheterocycles and their use as mek inhibitors and pharmaceutical compositions containing the compounds

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US (1) US6469004B1 (hu)
EP (1) EP1144385B1 (hu)
JP (1) JP4621355B2 (hu)
KR (1) KR20020002370A (hu)
CN (1) CN1177830C (hu)
AP (1) AP2001002224A0 (hu)
AT (1) ATE302193T1 (hu)
AU (1) AU2203700A (hu)
BG (1) BG105800A (hu)
BR (1) BR9916904A (hu)
CA (1) CA2355470C (hu)
CZ (1) CZ20012498A3 (hu)
DE (1) DE69926800T2 (hu)
EA (1) EA200100772A1 (hu)
EE (1) EE200100373A (hu)
ES (1) ES2247859T3 (hu)
GE (1) GEP20032922B (hu)
HK (1) HK1041697A1 (hu)
HR (1) HRP20010524A2 (hu)
HU (1) HUP0105113A3 (hu)
ID (1) ID30439A (hu)
IL (1) IL144214A0 (hu)
IS (1) IS5976A (hu)
MA (1) MA26771A1 (hu)
NO (1) NO20013452D0 (hu)
NZ (1) NZ513433A (hu)
OA (1) OA11746A (hu)
SK (1) SK9832001A3 (hu)
TR (1) TR200102030T2 (hu)
WO (1) WO2000042022A1 (hu)
YU (1) YU49401A (hu)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010068738A1 (en) 2008-12-10 2010-06-17 Dana-Farber Cancer Institute, Inc. Mek mutations conferring resistance to mek inhibitors
WO2011106298A1 (en) 2010-02-25 2011-09-01 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
WO2013169858A1 (en) 2012-05-08 2013-11-14 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002534380A (ja) * 1999-01-07 2002-10-15 ワーナー−ランバート・カンパニー Ｍｅｋ阻害剤による喘息の治療
US7030119B1 (en) 1999-07-16 2006-04-18 Warner-Lambert Company Method for treating chronic pain using MEK inhibitors
WO2001005390A2 (en) * 1999-07-16 2001-01-25 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
EP1339702A1 (en) 2000-03-15 2003-09-03 Warner-Lambert Company 5-amide substituted diarylamines as mek inhibitors
ES2461854T3 (es) * 2000-07-19 2014-05-21 Warner-Lambert Company Llc Ésteres oxigenados de ácidos 4-yodofenilamino-benzhidroxámicos
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
SI2130537T1 (sl) 2002-03-13 2013-01-31 Array Biopharma, Inc. N3-alkilirani derivati benzimidazola kot inhibitorji mek
CN1652792A (zh) * 2002-03-13 2005-08-10 阵列生物制药公司 作为mek抑制剂的n3烷基化苯并咪唑衍生物
US20050004186A1 (en) * 2002-12-20 2005-01-06 Pfizer Inc MEK inhibiting compounds
US20050049276A1 (en) * 2003-07-23 2005-03-03 Warner-Lambert Company, Llc Imidazopyridines and triazolopyridines
MXPA06000921A (es) 2003-07-24 2006-03-30 Warner Lambert Co Derivados de benzamidazoles como inhibidores de mek.
US7452895B2 (en) 2003-08-14 2008-11-18 Array Biopharma Inc. Quinazoline analogs as receptor tyrosine kinase inhibitors
US7501427B2 (en) 2003-08-14 2009-03-10 Array Biopharma, Inc. Quinazoline analogs as receptor tyrosine kinase inhibitors
US7538120B2 (en) 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
US7144907B2 (en) 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
US8084645B2 (en) 2003-09-19 2011-12-27 Chugai Seiyaku Kabushiki Kaisha 4-phenylamino-benzaldoxime derivatives and uses thereof as mitogen-activated protein kinase kinase (MEK) inhibitors
WO2005028447A1 (en) 2003-09-22 2005-03-31 S*Bio Pte Ltd Benzimidazole derivates: preparation and pharmaceutical applications
BRPI0415710A (pt) * 2003-10-21 2006-12-19 Warner Lambert Co formas polimórficas de n-[(r)-2,3-dihidróxi-propóxi]-3,4-diflúor-2-(2-flúor-4-io dofenilamino)-benzamida
US7732616B2 (en) * 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
US7517994B2 (en) * 2003-11-19 2009-04-14 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
WO2005051302A2 (en) 2003-11-19 2005-06-09 Array Biopharma Inc. Bicyclic inhibitors of mek and methods of use thereof
NZ547327A (en) 2003-11-21 2009-08-28 Array Biopharma Inc AKT protein kinase inhibitors
AU2004297235A1 (en) 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
JP2007513967A (ja) * 2003-12-11 2007-05-31 セラヴァンス， インコーポレーテッド 変異レセプターチロシンキナーゼが駆動する細胞増殖性疾患の処置において使用するための組成物
TWI361066B (en) 2004-07-26 2012-04-01 Chugai Pharmaceutical Co Ltd 5-substituted-2-phenylamino benzamides as mek inhibitors
AU2005293384A1 (en) * 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as B Raf inhibitors
DK1802579T3 (da) 2004-10-20 2014-01-20 Merck Serono Sa Derivater af 3-arylaminopyridin
CA2608201C (en) 2005-05-18 2013-12-31 Array Biopharma Inc. Heterocyclic inhibitors of mek and methods of use thereof
KR20140000721A (ko) 2005-06-23 2014-01-03 어레이 바이오파마 인크. 벤즈이미다졸 화합물의 제조 방법
HUE043172T2 (hu) 2005-06-23 2019-08-28 Array Biopharma Inc SNAr eljárás benzimidazol-származékok elõállítására
US8101799B2 (en) 2005-07-21 2012-01-24 Ardea Biosciences Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK
EP1934174B1 (en) * 2005-10-07 2011-04-06 Exelixis, Inc. Azetidines as mek inhibitors for the treatment of proliferative diseases
ZA200804498B (en) 2005-11-15 2009-07-29 Array Biopharma Inc N4-phenyl-quinazoline-4 -amine derivatives and related compounds as ERBB type I receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
US20090239936A1 (en) 2006-05-15 2009-09-24 Yoshikazu Sugimoto Prophylactic and Therapeutic Agent for Cancer
WO2008006039A1 (en) 2006-07-06 2008-01-10 Array Biopharma Inc. Dihydrothieno pyrimidines as akt protein kinase inhibitors
NZ573979A (en) 2006-07-06 2012-02-24 Array Biopharma Inc Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
CA2656566C (en) 2006-07-06 2014-06-17 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
JP5448818B2 (ja) * 2006-08-21 2014-03-19 ジェネンテック， インコーポレイテッド アザベンゾフラニル化合物および使用方法
WO2008024724A1 (en) * 2006-08-21 2008-02-28 Genentech, Inc. Aza-benzothiophenyl compounds and methods of use
RU2444524C2 (ru) * 2006-08-21 2012-03-10 Дженентек, Инк. Азабензотиофенильные соединения и способы применения
ZA200901009B (en) * 2006-08-21 2010-05-26 Genentech Inc Aza-benzothiophenyl compounds and methods of use
WO2008076415A1 (en) 2006-12-14 2008-06-26 Exelixis, Inc. Methods of using mek inhibitors
JO2985B1 (ar) 2006-12-20 2016-09-05 Takeda Pharmaceuticals Co مثبطات كينازmapk/erk
US20080312307A1 (en) * 2007-05-25 2008-12-18 Takeda Pharmaceutical Company Limited Mapk/erk kinase inhibitors
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
MX2009014013A (es) 2007-07-05 2010-01-28 Array Biopharma Inc Pirimidil ciclopentanos como inhibidores de la proteina cinasa akt.
BRPI0813999A2 (pt) 2007-07-05 2019-10-01 Array Biopharma Inc ciclopentanos de pirimidil como inibidores de akt proteína cinase
PE20131210A1 (es) 2007-12-19 2013-10-31 Genentech Inc Derivados de 5-anilinoimidazopiridina como inhibidores de mek
NZ586720A (en) 2008-01-09 2012-11-30 Array Biopharma Inc Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
EP2247578B1 (en) 2008-01-09 2013-05-22 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
NZ591498A (en) 2008-08-04 2012-09-28 Merck Patent Gmbh Novel phenylamino isonicotinamide compounds
JP5746630B2 (ja) 2008-11-10 2015-07-08 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 置換スルホンアミドフェノキシベンズアミド
US20120263714A1 (en) 2009-10-21 2012-10-18 Bayer Intellectual Property Gmbh Substituted halophenoxybenzamide derivatives
WO2011047795A1 (en) 2009-10-21 2011-04-28 Bayer Schering Pharma Aktiengesellschaft Substituted benzosulphonamides
US8962606B2 (en) 2009-10-21 2015-02-24 Bayer Intellectual Property Gmbh Substituted benzosulphonamides
BR112012022801B8 (pt) 2010-03-09 2019-10-29 Dana Farber Cancer Inst Inc método de identificar um indivíduo que tem câncer que é provável beneficiar-se do tratamento com uma terapia de combinação com um inibidor de raf e um segundo inibidor e uso de um inibidor de raf e um segundo inibidor para a fabricação de um medicamento para tratar câncer
US8541596B2 (en) 2010-04-21 2013-09-24 Probiodrug Ag Inhibitors
WO2012055953A1 (en) 2010-10-29 2012-05-03 Bayer Pharma Aktiengesellschaft Substituted phenoxypyridines
CN102020651B (zh) 2010-11-02 2012-07-18 北京赛林泰医药技术有限公司 6-芳基氨基吡啶酮甲酰胺mek抑制剂
KR20140022053A (ko) 2011-04-01 2014-02-21 제넨테크, 인크. Akt 및 mek 억제제 화합물의 조합물, 및 사용 방법
SG194045A1 (en) 2011-04-01 2013-11-29 Genentech Inc Combinations of akt inhibitor compounds and abiraterone, and methods of use
ES2597052T3 (es) 2011-05-25 2017-01-13 Université Paris Descartes Inhibidores de ERK para su uso en el tratamiento de atrofia muscular espinal
ES2396764B1 (es) 2011-11-02 2013-12-19 Universidad Autónoma de Madrid FÁRMACOS INHIBIDORES DE p38 Y APLICACIONES.
CN103204825B (zh) 2012-01-17 2015-03-04 上海科州药物研发有限公司 作为蛋白激酶抑制剂的苯并噻唑化合物及其制备方法和用途
MX2014014097A (es) 2012-05-31 2015-04-13 Bayer Pharma AG Biomarcadores para determinar la respuesta eficaz de tratamientos en pacientes de carcinoma hepatocelular (chc).
BR112015008113B1 (pt) 2012-10-12 2022-05-24 Exelixis, Inc. Novo processo para preparar compostos para uso no tratamento de câncer
DK2909182T3 (da) * 2012-10-19 2020-02-17 Array Biopharma Inc Fremstilling af og formulering omfattende en mek-inhibitor
EP3043822A1 (en) 2013-09-11 2016-07-20 The J. David Gladstone Institutes, A Testamentary Trust Established under The Will of J. David Gladstone Compositions for preparing cardiomyocytes
CA2935804A1 (en) 2014-01-14 2015-07-23 Dana-Farber Cancer Institute, Inc. Compositions and methods for identification, assessment, prevention, and treatment of melanoma using pd-l1 isoforms
CN104774188B (zh) * 2014-01-15 2019-10-11 江苏恒瑞医药股份有限公司 苯并杂环类或苯并杂芳环类衍生物、其制备方法及其在医药上的应用
CN105384754B (zh) * 2014-09-02 2018-04-20 上海科州药物研发有限公司 作为蛋白激酶抑制剂的杂环类化合物及其制备方法和用途
AU2015328411C1 (en) 2014-10-06 2022-03-03 Dana-Farber Cancer Institute, Inc. Angiopoietin-2 biomarkers predictive of anti-immune checkpoint response
MA41866A (fr) 2015-03-31 2018-02-06 Massachusetts Gen Hospital Molécules à auto-assemblage pour l'administration ciblée de médicaments
WO2017033113A1 (en) 2015-08-21 2017-03-02 Acerta Pharma B.V. Therapeutic combinations of a mek inhibitor and a btk inhibitor
AU2016370846B2 (en) * 2015-12-18 2022-08-25 Ignyta, Inc. Combinations for the treatment of cancer
AR108257A1 (es) 2016-05-02 2018-08-01 Mei Pharma Inc Formas polimórficas de 3-[2-butil-1-(2-dietilamino-etil)-1h-bencimidazol-5-il]-n-hidroxi-acrilamida y usos de las mismas
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
EP4073102A4 (en) 2019-12-12 2024-05-08 Ting Therapeutics LLC COMPOSITIONS AND METHODS FOR PREVENTION AND TREATMENT OF HEARING LOSS
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN114478447A (zh) * 2020-11-13 2022-05-13 江苏恒瑞医药股份有限公司 苯并含氧环类衍生物、其制备方法及其在医药上的应用
TW202342018A (zh) 2022-03-04 2023-11-01 美商奇奈特生物製藥公司 Mek激酶抑制劑

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5525625A (en) 1995-01-24 1996-06-11 Warner-Lambert Company 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders
US6251943B1 (en) * 1997-02-28 2001-06-26 Warner-Lambert Company Method of treating or preventing septic shock by administering a MEK inhibitor
CN1163475C (zh) 1997-07-01 2004-08-25 沃尼尔·朗伯公司 4-溴或4-碘苯基氨基苯氧肟酸衍生物及其作为mek抑制剂的用途
US6310060B1 (en) 1998-06-24 2001-10-30 Warner-Lambert Company 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
JP2000204079A (ja) * 1999-01-13 2000-07-25 Warner Lambert Co ジアリ―ルアミン

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010068738A1 (en) 2008-12-10 2010-06-17 Dana-Farber Cancer Institute, Inc. Mek mutations conferring resistance to mek inhibitors
WO2011106298A1 (en) 2010-02-25 2011-09-01 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
EP3028699A1 (en) 2010-02-25 2016-06-08 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
WO2013169858A1 (en) 2012-05-08 2013-11-14 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy

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