RU2300528C2 - N3-алкилированные бензимидазольные производные в качестве ингибиторов мек - Google Patents

N3-алкилированные бензимидазольные производные в качестве ингибиторов мек Download PDF

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Publication number
RU2300528C2
RU2300528C2 RU2004127925/04A RU2004127925A RU2300528C2 RU 2300528 C2 RU2300528 C2 RU 2300528C2 RU 2004127925/04 A RU2004127925/04 A RU 2004127925/04A RU 2004127925 A RU2004127925 A RU 2004127925A RU 2300528 C2 RU2300528 C2 RU 2300528C2
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RU
Russia
Prior art keywords
alkyl
cycloalkyl
trifluoromethyl
halogen
difluoromethoxy
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RU2004127925/04A
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English (en)
Russian (ru)
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RU2004127925A (ru
Inventor
Эли М. УОЛЛЕС (US)
Эли М. Уоллес
Джозеф П. ЛИССИКЭЙТОС (US)
Джозеф П. ЛИССИКЭЙТОС
Брайан Т. ХЕРЛИ (US)
Брайан Т. ХЕРЛИ
Элисон Л. МАРЛОУ (US)
Элисон Л. МАРЛОУ
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Эррэй Биофарма, Инк.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
RU2004127925/04A 2002-03-13 2003-03-13 N3-алкилированные бензимидазольные производные в качестве ингибиторов мек RU2300528C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36416402P 2002-03-13 2002-03-13
US60/364,164 2002-03-13

Publications (2)

Publication Number Publication Date
RU2004127925A RU2004127925A (ru) 2005-05-27
RU2300528C2 true RU2300528C2 (ru) 2007-06-10

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Country Status (18)

Country Link
US (2) US20030216460A1 (OSRAM)
EP (1) EP1482944A4 (OSRAM)
JP (1) JP2005526076A (OSRAM)
KR (1) KR20040098013A (OSRAM)
CN (1) CN1652792A (OSRAM)
AR (1) AR038972A1 (OSRAM)
AU (1) AU2003220202A1 (OSRAM)
CA (1) CA2478534A1 (OSRAM)
CO (1) CO5611145A2 (OSRAM)
DO (1) DOP2003000614A (OSRAM)
IL (1) IL163996A0 (OSRAM)
MX (1) MXPA04008894A (OSRAM)
PA (1) PA8569201A1 (OSRAM)
PL (1) PL378635A1 (OSRAM)
RU (1) RU2300528C2 (OSRAM)
TW (1) TW200406203A (OSRAM)
UA (1) UA76837C2 (OSRAM)
WO (1) WO2003077855A2 (OSRAM)

Cited By (7)

* Cited by examiner, † Cited by third party
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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
RU2441004C1 (ru) * 2007-12-19 2012-01-27 Дженентек, Инк. 5-анилиноимидазопиридины и способы их применения
RU2483069C2 (ru) * 2007-12-21 2013-05-27 Дженентек, Инк. Азаиндолизины и способы их применения
RU2495028C2 (ru) * 2008-07-01 2013-10-10 Дженентек, Инк. Изоиндолоны и способы их применения
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
US11078540B2 (en) 2010-03-09 2021-08-03 Dana-Farber Cancer Institute, Inc. Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy

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PL401638A1 (pl) * 2002-03-13 2013-05-27 Array Biopharma Inc. N3 alkilowane pochodne benzimidazolu jako inhibitory MEK
ES2331246T3 (es) * 2003-07-24 2009-12-28 Warner-Lambert Company Llc Derivados de benzamidazol como inhibidores del mek.
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
US7781595B2 (en) 2003-09-22 2010-08-24 S*Bio Pte Ltd. Benzimidazole derivatives: preparation and pharmaceutical applications
US7732616B2 (en) * 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
ATE495155T1 (de) * 2003-11-19 2011-01-15 Array Biopharma Inc Heterocyclische inhibitoren von mek
US7517994B2 (en) * 2003-11-19 2009-04-14 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
NZ547327A (en) * 2003-11-21 2009-08-28 Array Biopharma Inc AKT protein kinase inhibitors
WO2005058341A2 (en) * 2003-12-11 2005-06-30 Theravance, Inc. Compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases
CA2582247C (en) 2004-10-20 2014-02-11 Applied Research Systems Ars Holding N.V. 3-arylamino pyridine derivatives
AU2005311451A1 (en) * 2004-12-01 2006-06-08 Merck Serono Sa [1,2,4]triazolo[4,3-a]pyridine derivatives for the treatment of hyperproliferative diseases
TW201238952A (en) 2005-05-18 2012-10-01 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
US8101799B2 (en) 2005-07-21 2012-01-24 Ardea Biosciences Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK
ATE504565T1 (de) * 2005-10-07 2011-04-15 Exelixis Inc Azetidine als mek-inhibitoren bei der behandlung proliferativer erkrankungen
US20090030058A1 (en) * 2005-12-21 2009-01-29 Mohammed Pervez Tosylate salt of 6- (4-br0m0-2-chl0r0phenylamin0) -7-fluoro-n- (2-hydroxyethoxy) -3-methyl-3h-benzimi dazole- 5 - carboxamide , mek inhibitor useful in the treatment of cancer
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
CA2656618C (en) 2006-07-06 2014-08-26 Array Biopharma Inc. Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
ATE532789T1 (de) 2006-07-06 2011-11-15 Array Biopharma Inc Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
CN101511842B (zh) 2006-07-06 2012-10-31 阵列生物制药公司 作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶
ZA200901009B (en) * 2006-08-21 2010-05-26 Genentech Inc Aza-benzothiophenyl compounds and methods of use
KR101475088B1 (ko) * 2006-08-21 2014-12-23 제넨테크, 인크. 아자-벤조티오페닐 화합물 및 사용 방법
MX2009001878A (es) * 2006-08-21 2009-03-03 Genentech Inc Compuestos de aza-benzofuranilo y metodos de uso.
CN105106199A (zh) 2006-12-14 2015-12-02 埃克塞利希斯股份有限公司 使用mek抑制剂的方法
JO2985B1 (ar) 2006-12-20 2016-09-05 Takeda Pharmaceuticals Co مثبطات كينازmapk/erk
US8258152B2 (en) 2007-06-12 2012-09-04 Genentech, Inc. N-substituted azaindoles and methods of use
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
WO2009006567A2 (en) 2007-07-05 2009-01-08 Array Biopharma Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors
SI2173723T1 (sl) * 2007-07-05 2011-12-30 Array Biopharma Inc Pirimidil ciklopentani kot inhibitorji AKT-protein-kinaze
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
GB0714384D0 (en) 2007-07-23 2007-09-05 Ucb Pharma Sa theraputic agents
WO2009064675A1 (en) 2007-11-12 2009-05-22 Takeda Pharmaceutical Company Limited Mapk/erk kinase inhibitors
CN101903387B (zh) 2007-12-19 2014-05-21 健泰科生物技术公司 8-苯氨基咪唑并吡啶和它们在制备抗癌剂和/或抗炎剂中的用途
JP5710269B2 (ja) 2007-12-21 2015-04-30 ジェネンテック, インコーポレイテッド アザインドリジン類と使用方法
WO2009089453A1 (en) * 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
NZ586346A (en) * 2008-01-09 2012-02-24 Array Biopharma Inc Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
WO2009093008A1 (en) 2008-01-21 2009-07-30 Ucb Pharma S.A. Thieno-pyridine derivatives as mek inhibitors
GB0811304D0 (en) 2008-06-19 2008-07-30 Ucb Pharma Sa Therapeutic agents
US8841462B2 (en) 2008-07-01 2014-09-23 Robert A. Heald Bicyclic heterocycles as MEK kinase inhibitors
MX2011001127A (es) 2008-08-04 2011-03-21 Merck Patent Gmbh Compuestos novedosos de fenilamino-isonicotinamida.
CA2742945A1 (en) 2008-11-10 2010-05-14 Bayer Schering Pharma Aktiengesellschaft Substituted sulphonamido phenoxybenzamides
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JP2013508320A (ja) 2009-10-21 2013-03-07 バイエル・ファルマ・アクチェンゲゼルシャフト 置換されたハロフェノキシベンズアミド誘導体
CA2777304A1 (en) 2009-10-21 2011-04-28 Marion Hitchcock Substituted benzosulphonamides
MA34591B1 (fr) 2010-10-06 2013-10-02 Glaxosmithkline Llc Dérivés de benzimidazole utilisés comme inhibiteurs de pi3 kinase
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JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
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Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2441004C1 (ru) * 2007-12-19 2012-01-27 Дженентек, Инк. 5-анилиноимидазопиридины и способы их применения
RU2483069C2 (ru) * 2007-12-21 2013-05-27 Дженентек, Инк. Азаиндолизины и способы их применения
RU2495028C2 (ru) * 2008-07-01 2013-10-10 Дженентек, Инк. Изоиндолоны и способы их применения
WO2010068738A1 (en) 2008-12-10 2010-06-17 Dana-Farber Cancer Institute, Inc. Mek mutations conferring resistance to mek inhibitors
US9084781B2 (en) 2008-12-10 2015-07-21 Novartis Ag 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
US8637246B2 (en) 2010-02-25 2014-01-28 Dana-Farber Cancer Institute, Inc. BRAF mutations conferring resistance to BRAF inhibitors
US9279144B2 (en) 2010-02-25 2016-03-08 Dana-Farber Cancer Institute, Inc. Screening method for BRAF inhibitors
EP3028699A1 (en) 2010-02-25 2016-06-08 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
US11078540B2 (en) 2010-03-09 2021-08-03 Dana-Farber Cancer Institute, Inc. Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy
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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Publication number Publication date
UA76837C2 (uk) 2006-09-15
KR20040098013A (ko) 2004-11-18
US20030216460A1 (en) 2003-11-20
CO5611145A2 (es) 2006-02-28
EP1482944A4 (en) 2006-04-19
AU2003220202A1 (en) 2003-09-29
WO2003077855A3 (en) 2004-03-04
RU2004127925A (ru) 2005-05-27
TW200406203A (en) 2004-05-01
US20060106225A1 (en) 2006-05-18
MXPA04008894A (es) 2005-06-20
AR038972A1 (es) 2005-02-02
CN1652792A (zh) 2005-08-10
IL163996A0 (en) 2005-12-18
CA2478534A1 (en) 2003-09-25
PA8569201A1 (es) 2004-05-21
WO2003077855A2 (en) 2003-09-25
PL378635A1 (pl) 2006-05-15
DOP2003000614A (es) 2009-09-30
EP1482944A2 (en) 2004-12-08
JP2005526076A (ja) 2005-09-02

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