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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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)

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

Cited By (7)

* 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
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
WO2005009975A2 (en) 2003-07-24 2005-02-03 Warner-Lambert Company Llc Benzimidazole derivatives as mek inhibitors
US7144907B2 (en) 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
US7538120B2 (en) 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
TWI349664B (en) 2003-09-22 2011-10-01 S Bio Pte Ltd Benzimidazole derivatives: preparation and pharmaceutical applications
JP4768628B2 (ja) * 2003-11-19 2011-09-07 アレイ バイオファーマ、インコーポレイテッド Mekの二環系阻害剤及びその使用方法
US7517994B2 (en) * 2003-11-19 2009-04-14 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
US7732616B2 (en) 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
AU2004293026B2 (en) * 2003-11-21 2012-01-19 Array Biopharma Inc. AKT protein kinase inhibitors
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PT1802579E (pt) 2004-10-20 2014-02-17 Merck Serono Sa Derivados da 3-arilaminopiridina
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
EP1967516B1 (en) 2005-05-18 2009-11-04 Array Biopharma, Inc. 4-(phenylamino)-6-oxo-1,6-dihydropyridazine-3-carboxamide derivatives as MEK inhibitors for the treatment of hyperproliferative diseases
US8039637B2 (en) 2005-06-23 2011-10-18 Array Biopharma Inc. Process for preparing benzimidazole compounds
US8101799B2 (en) 2005-07-21 2012-01-24 Ardea Biosciences Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK
HRP20110498T1 (hr) 2005-10-07 2011-08-31 Exelixis Azetidini kao inhibitori mek za liječenje proliferativnih bolesti
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
WO2008006025A1 (en) 2006-07-06 2008-01-10 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
SI2054418T1 (sl) 2006-07-06 2012-02-29 Array Biopharma Inc Dihidrotieno pirimidini kot AKT protein kinazni inhibitorji
DK2049500T3 (da) 2006-07-06 2011-12-12 Array Biopharma Inc Cyclopenta [d]-pyrimidiner som AKT-proteinkinase-inhibitorer
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
CN101583616B (zh) * 2006-08-21 2012-05-30 健泰科生物技术公司 氮杂苯并噻吩基化合物及使用方法
JP5349306B2 (ja) 2006-08-21 2013-11-20 ジェネンテック, インコーポレイテッド アザベンゾチオフェニル化合物および使用方法
CA2660546A1 (en) * 2006-08-21 2008-02-28 Genentech, Inc. Aza-benzofuranyl compounds and methods of use
JP5311673B2 (ja) 2006-12-14 2013-10-09 エグゼリクシス, インコーポレイテッド Mek阻害剤の使用方法
JO2985B1 (ar) 2006-12-20 2016-09-05 Takeda Pharmaceuticals Co مثبطات كينازmapk/erk
WO2008157179A2 (en) 2007-06-12 2008-12-24 Genentech, Inc. N-substituted azaindoles and methods of use
CN101801955B (zh) 2007-07-05 2013-05-08 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
KR20150091196A (ko) 2007-07-05 2015-08-07 어레이 바이오파마 인크. Akt 단백질 키나제 억제제로서의 피리미딜 시클로펜탄
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
GB0714384D0 (en) 2007-07-23 2007-09-05 Ucb Pharma Sa theraputic agents
US8022057B2 (en) 2007-11-12 2011-09-20 Takeda Pharmaceutical Company Limited MAPK/ERK kinase inhibitors
CA2704125A1 (en) 2007-12-19 2009-07-09 Genentech, Inc. 8-anilinoimidazopyridines and their use as anti-cancer and/or anti-inflammatory agents
US8486963B2 (en) 2007-12-21 2013-07-16 Genentech, Inc. Azaindolizines and methods of use
KR101624752B1 (ko) * 2008-01-09 2016-05-26 어레이 바이오파마 인크. Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄
CA2711699A1 (en) * 2008-01-09 2009-07-16 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
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HUE027223T2 (en) 2008-08-04 2016-08-29 Merck Patent Gmbh New Phenylamino Isonicotinamide Compounds
EP2346818B1 (en) 2008-11-10 2012-12-05 Bayer Intellectual Property GmbH Substituted sulphonamido phenoxybenzamides
EP2491014A1 (en) 2009-10-21 2012-08-29 Bayer Pharma Aktiengesellschaft Substituted halophenoxybenzamide derivatives
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KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
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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
PL378635A1 (pl) 2006-05-15
AR038972A1 (es) 2005-02-02
DOP2003000614A (es) 2009-09-30
MXPA04008894A (es) 2005-06-20
PA8569201A1 (es) 2004-05-21
IL163996A0 (en) 2005-12-18
TW200406203A (en) 2004-05-01
JP2005526076A (ja) 2005-09-02
WO2003077855A2 (en) 2003-09-25
WO2003077855A3 (en) 2004-03-04
US20030216460A1 (en) 2003-11-20
CN1652792A (zh) 2005-08-10
CO5611145A2 (es) 2006-02-28
US20060106225A1 (en) 2006-05-18
CA2478534A1 (en) 2003-09-25
KR20040098013A (ko) 2004-11-18
AU2003220202A1 (en) 2003-09-29
RU2004127925A (ru) 2005-05-27
EP1482944A4 (en) 2006-04-19
EP1482944A2 (en) 2004-12-08

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