JP5026076B2 - Ｍｅｋ阻害剤としてのｎ３アルキル化ベンズイミダゾール誘導体 - Google Patents

Ｍｅｋ阻害剤としてのｎ３アルキル化ベンズイミダゾール誘導体 Download PDF

Info

Publication number
JP5026076B2
JP5026076B2 JP2006524761A JP2006524761A JP5026076B2 JP 5026076 B2 JP5026076 B2 JP 5026076B2 JP 2006524761 A JP2006524761 A JP 2006524761A JP 2006524761 A JP2006524761 A JP 2006524761A JP 5026076 B2 JP5026076 B2 JP 5026076B2
Authority
JP
Japan
Prior art keywords
fluoro
bromo
amino
benzo
carboxamide
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
JP2006524761A
Other languages
English (en)
Japanese (ja)
Other versions
JP2007504139A (ja
JP2007504139A5 (enExample
Inventor
ウォレス、エリ、エム．
リシカトス、ジョゼフ、ピー．
マーロー、アリソン、エル．
ハーリー、ブライアン、ティー．
コッチ、ケビン
Original Assignee
アレイ バイオファーマ、インコーポレイテッド
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 アレイ バイオファーマ、インコーポレイテッド filed Critical アレイ バイオファーマ、インコーポレイテッド
Publication of JP2007504139A publication Critical patent/JP2007504139A/ja
Publication of JP2007504139A5 publication Critical patent/JP2007504139A5/ja
Application granted granted Critical
Publication of JP5026076B2 publication Critical patent/JP5026076B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632—Organic additives
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
    • C07F9/65068—Five-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Ceramic Engineering (AREA)
  • Manufacturing & Machinery (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Structural Engineering (AREA)
  • Materials Engineering (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2006524761A 2003-08-29 2004-08-20 Ｍｅｋ阻害剤としてのｎ３アルキル化ベンズイミダゾール誘導体 Expired - Lifetime JP5026076B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10/652,733 US7235537B2 (en) 2002-03-13 2003-08-29 N3 alkylated benzimidazole derivatives as MEK inhibitors
US10/652,733 2003-08-29
PCT/US2004/027199 WO2005023251A1 (en) 2003-08-29 2004-08-20 N3 alkylated benzimidazole derivatives as mek inhibitors

Publications (3)

Publication Number Publication Date
JP2007504139A JP2007504139A (ja) 2007-03-01
JP2007504139A5 JP2007504139A5 (enExample) 2007-09-27
JP5026076B2 true JP5026076B2 (ja) 2012-09-12

Family

ID=34273411

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2006524761A Expired - Lifetime JP5026076B2 (ja) 2003-08-29 2004-08-20 Ｍｅｋ阻害剤としてのｎ３アルキル化ベンズイミダゾール誘導体

Country Status (18)

Country Link
US (2) US7235537B2 (enExample)
EP (1) EP1663210B1 (enExample)
JP (1) JP5026076B2 (enExample)
KR (1) KR20060121853A (enExample)
CN (1) CN1874768A (enExample)
AR (1) AR045738A1 (enExample)
AU (1) AU2004270166A1 (enExample)
BR (1) BRPI0413152A (enExample)
CA (1) CA2537098A1 (enExample)
ES (1) ES2628959T3 (enExample)
IL (1) IL173935A (enExample)
IS (1) IS8384A (enExample)
MX (1) MXPA06002268A (enExample)
NO (1) NO20061432L (enExample)
RU (1) RU2006109600A (enExample)
TW (1) TW200524879A (enExample)
WO (1) WO2005023251A1 (enExample)
ZA (1) ZA200602588B (enExample)

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1482932E (pt) * 2002-03-13 2010-01-12 Array Biopharma Inc Derivados de benzimidazole alquilado n3 como inibidores de mek
ES2331246T3 (es) * 2003-07-24 2009-12-28 Warner-Lambert Company Llc Derivados de benzamidazol como inhibidores del mek.
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
US7732616B2 (en) * 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
KR101190912B1 (ko) * 2003-11-19 2012-10-12 어레이 바이오파마 인크. Ｍｅｋ의 헤테로시클릭 억제제 및 그의 사용 방법
US7517994B2 (en) 2003-11-19 2009-04-14 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
BRPI0416852A (pt) * 2003-11-21 2007-02-27 Array Biopharma Inc inibidores da quinase akt
CN102321030A (zh) * 2005-05-18 2012-01-18 阵列生物制药公司 Mek的杂环抑制剂及其使用方法
AU2006302415B2 (en) 2005-10-07 2012-09-13 Exelixis, Inc. Azetidines as MEK inhibitors for the treatment of proliferative diseases
ATE507224T1 (de) 2005-11-15 2011-05-15 Array Biopharma Inc Verfahren und zwischenverbindungen zur herstellung von n4-phenyl-quinazolin-4-amin derivaten
EP1966155A1 (en) * 2005-12-21 2008-09-10 AstraZeneca AB 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
RU2418790C3 (ru) * 2005-12-21 2022-03-14 Астразенека Аб Новая гидросульфатная соль
TWI405756B (zh) 2005-12-21 2013-08-21 Array Biopharma Inc 新穎硫酸氫鹽
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
DK2054418T3 (da) 2006-07-06 2012-02-27 Array Biopharma Inc Dihydrothieno-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
SI2049500T1 (sl) * 2006-07-06 2012-01-31 Array Biopharma Inc Ciklopenta (d) pirimidini kot AKT protein kinazni inhibitorji
CA2656566C (en) 2006-07-06 2014-06-17 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
EP2099796B1 (en) * 2006-11-30 2011-06-01 Genentech, Inc. Aza-indolyl compounds and methods of use
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
EP2170863B1 (en) 2007-07-05 2015-09-02 Array Biopharma, Inc. Pyrimido cyclopentanes useful for the treatment of inflammatory or hyperproliferative diseases
ATE522509T1 (de) * 2007-07-05 2011-09-15 Array Biopharma Inc Pyrimidylcyclopentane als inhibitoren der akt- proteinkinase
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
GB0714384D0 (en) 2007-07-23 2007-09-05 Ucb Pharma Sa theraputic agents
BRPI0815180A2 (pt) * 2007-08-16 2019-09-24 Hoffmann La Roche hindantoinas substituídas
ES2456966T3 (es) 2007-11-12 2014-04-24 Takeda Pharmaceutical Company Limited Inhibidores de MAPK/ERK cinasa
WO2009074827A2 (en) * 2007-12-12 2009-06-18 Astrazeneca Ab Combination comprising a mek inhibitor and an aurora kinase inhibitor 188
BRPI0820696A2 (pt) 2007-12-20 2019-09-24 Hoffmann La Roche hidantoínas substituídas como inibidores de cinase de mek
CN101932565B (zh) * 2008-01-09 2013-06-12 阵列生物制药公司 作为akt蛋白激酶抑制剂的羟基化嘧啶基环戊烷
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
GB0811304D0 (en) 2008-06-19 2008-07-30 Ucb Pharma Sa Therapeutic agents
BRPI0915901A2 (pt) * 2008-07-11 2015-10-27 Novartis Ag combinação de (a) um inibidor de fosfoinositídeo 3-quinase e (b) um modulador da via ras/raf/mek
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
TWI428336B (zh) * 2009-10-12 2014-03-01 Hoffmann La Roche Ｐｉ３ｋ抑制劑及ｍｅｋ抑制劑之組合
WO2011047796A1 (en) 2009-10-21 2011-04-28 Bayer Schering Pharma Aktiengesellschaft Substituted halophenoxybenzamide derivatives
EP2491016A1 (en) 2009-10-21 2012-08-29 Bayer Pharma Aktiengesellschaft Substituted benzosulphonamides
CA2777304A1 (en) 2009-10-21 2011-04-28 Marion Hitchcock Substituted benzosulphonamides
WO2012019113A2 (en) 2010-08-05 2012-02-09 Case Western Reserve University Inhibitors of erk for developmental disorders of neuronal connectivity
SI2624696T1 (sl) 2010-10-06 2017-04-26 Glaxosmithkline Llc Corporation Service Company Benzimidazolni derivati kot inhibitorji pi3-kinaze
JP2013542214A (ja) 2010-10-29 2013-11-21 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 置換フェノキシピリジン類
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
ES2531465T3 (es) 2010-12-23 2015-03-16 Sanofi Derivados de pirimidinona, su preparación y su utilización farmacéutica
CN103857395A (zh) 2011-04-01 2014-06-11 基因泰克公司 Akt抑制剂化合物和阿比特龙的组合及使用方法
US9682082B2 (en) 2011-04-01 2017-06-20 Genentech, Inc. Combinations of AKT and MEK inhibitor compounds, and methods of use
EP2714037B1 (en) 2011-05-25 2016-07-13 Université Paris Descartes Erk inhibitors for use in treating spinal muscular atrophy
US9675595B2 (en) 2011-08-31 2017-06-13 Novartis Ag Synergistic combinations of PI3K- and MEK-inhibitors
CN103204827B (zh) 2012-01-17 2014-12-03 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二唑化合物及其制备方法和用途
CA2865164C (en) 2012-03-14 2021-06-08 Lupin Limited Heterocyclyl compounds as mek inhibitors
AR091876A1 (es) * 2012-07-26 2015-03-04 Novartis Ag Combinaciones farmaceuticas para el tratamiento de enfermedades proliferativas
AU2013328929B2 (en) 2012-10-12 2018-01-04 Exelixis, Inc. Novel process for making compounds for use in the treatment of cancer
PT3702351T (pt) 2012-10-19 2024-01-17 Array Biopharma Inc Formulação contendo um inibidor de mek
EP2934515B1 (en) * 2012-12-20 2018-04-04 Novartis AG A pharmaceutical combination comprising binimetinib
MA44934B1 (fr) * 2013-03-21 2021-11-30 Novartis Ag Therapie de combinaison comprenant un inhibiteur de b-raf et un second inhibiteur
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
WO2016009306A1 (en) 2014-07-15 2016-01-21 Lupin Limited Heterocyclyl compounds as mek inhibitors
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
WO2016035008A1 (en) 2014-09-04 2016-03-10 Lupin Limited Pyridopyrimidine derivatives as mek inhibitors
CN105566225A (zh) * 2015-02-16 2016-05-11 苏州晶云药物科技有限公司 一种口服丝裂原活化蛋白激酶抑制剂的晶型及其制备方法
WO2017033113A1 (en) 2015-08-21 2017-03-02 Acerta Pharma B.V. Therapeutic combinations of a mek inhibitor and a btk inhibitor
PT3463345T (pt) * 2016-06-03 2023-01-06 Array Biopharma Inc Combinações farmacêuticas
CN111646946A (zh) * 2017-11-14 2020-09-11 深圳市塔吉瑞生物医药有限公司 一种取代的苯并咪唑化合物及包含该化合物的组合物
CN111448185A (zh) * 2017-12-07 2020-07-24 哈尔滨珍宝制药有限公司 一种作为fgfr和vegfr抑制剂化合物的盐型、晶型及其制备方法
SMT202400524T1 (it) 2018-09-18 2025-01-14 Hoffmann La Roche Derivati della chinazolina come agenti antitumorali
AU2019407426A1 (en) 2018-12-21 2021-07-22 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
US11447482B1 (en) 2019-02-14 2022-09-20 KUDA Therapeutics, Inc. Imidazopyridine and oxazolopyridine derivatives and analogs thereof, methods of preparation thereof, methods of HIF-2A pathway inhibition, and induction of ferroptosis
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
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN115322105A (zh) * 2021-05-11 2022-11-11 江苏润安制药有限公司 一种合成艾拉莫德关键中间体的方法
EP4346826A4 (en) 2021-05-27 2025-04-30 Mirati Therapeutics, Inc. COMBINATION THERAPIES
WO2022262699A1 (zh) * 2021-06-17 2022-12-22 深圳市塔吉瑞生物医药有限公司 取代的苯并咪唑类化合物及包含该化合物的组合物及其用途
KR20240035820A (ko) 2021-07-09 2024-03-18 플렉시움 인코포레이티드 Ikzf2를 조절하는 아릴 화합물 및 약학 조성물
CN120309621A (zh) 2021-10-20 2025-07-15 豪夫迈·罗氏有限公司 喹唑啉衍生物的结晶形式、其制备、组合物和用途
CN116135839A (zh) * 2021-11-18 2023-05-19 江苏润安制药有限公司 一种阿齐沙坦关键中间体的制备方法
WO2025073765A1 (en) 2023-10-03 2025-04-10 Institut National de la Santé et de la Recherche Médicale Methods of prognosis and treatment of patients suffering from melanoma

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5750545A (en) * 1993-07-23 1998-05-12 The Green Cross Corporation Triazole derivative and pharmaceutical use thereof
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
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
NZ501277A (en) 1997-07-01 2002-12-20 Warner Lambert Co -2(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
US6821963B2 (en) * 1997-07-01 2004-11-23 Warner-Lambert Company 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors
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
WO1999001426A1 (en) 1997-07-01 1999-01-14 Warner-Lambert Company 4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as mek inhibitors
US6506798B1 (en) * 1997-07-01 2003-01-14 Warner-Lambert Company 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors
HUP0104933A3 (en) 1999-01-07 2003-12-29 Warner Lambert Co Antiviral method using mek inhibitors
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
EE200100374A (et) 1999-01-13 2002-12-16 Warner-Lambert Company 1-heterotsükliga asendatud diarüülamiinid
CA2348236A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors
JP2002534446A (ja) 1999-01-13 2002-10-15 ワーナー−ランバート・カンパニー ４′ヘテロアリールジアリールアミン
WO2000042002A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors
CA2349832A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Benzenesulfonamide derivatives and their use as mek inhibitors
EP1144385B1 (en) * 1999-01-13 2005-08-17 Warner-Lambert Company Llc Benzoheterocycles and their use as mek inhibitors
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
HUP0202623A3 (en) 1999-07-16 2003-03-28 Warner Lambert Co Method for treating chronic pain using mek inhibitors
US7030119B1 (en) * 1999-07-16 2006-04-18 Warner-Lambert Company Method for treating chronic pain using MEK inhibitors
CN1358095A (zh) 1999-07-16 2002-07-10 沃尼尔·朗伯公司 使用mek抑制剂治疗慢性疼痛的方法
AU5912500A (en) 1999-07-16 2001-02-05 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
MXPA02008103A (es) 2000-03-15 2002-11-29 Warner Lambert Co Diarilaminas sustituidas con 5-amida como inhibidores mek.
EP1339702A1 (en) * 2000-03-15 2003-09-03 Warner-Lambert Company 5-amide substituted diarylamines as mek inhibitors
OA12333A (en) 2000-07-19 2004-04-06 Warner Lambert Co Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids.
AP2001002249A0 (en) 2000-08-25 2001-09-30 Warner Lambert Co Process for making N-ARYL-ANTHRANILIC acids and their derivatives.
EP1337524A1 (en) 2000-11-02 2003-08-27 AstraZeneca AB Substituted quinolines as antitumor agents
US20040039208A1 (en) * 2001-07-20 2004-02-26 Chen Michael Huai Gu Process for making n-aryl-anthranilic acids and their derivatives
PT1482932E (pt) * 2002-03-13 2010-01-12 Array Biopharma Inc Derivados de benzimidazole alquilado n3 como inibidores de mek
AU2003220202A1 (en) * 2002-03-13 2003-09-29 Array Biopharma, Inc N3 alkylated benzimidazole derivatives as mek inhibitors
ES2331246T3 (es) * 2003-07-24 2009-12-28 Warner-Lambert Company Llc Derivados de benzamidazol como inhibidores del mek.

Also Published As

Publication number Publication date
TW200524879A (en) 2005-08-01
US7235537B2 (en) 2007-06-26
ZA200602588B (en) 2008-07-30
EP1663210A1 (en) 2006-06-07
KR20060121853A (ko) 2006-11-29
MXPA06002268A (es) 2006-05-31
ES2628959T3 (es) 2017-08-04
US20040116710A1 (en) 2004-06-17
EP1663210B1 (en) 2017-04-19
IS8384A (is) 2006-03-29
IL173935A (en) 2015-08-31
US20070299063A1 (en) 2007-12-27
NO20061432L (no) 2006-08-25
BRPI0413152A (pt) 2006-10-03
CA2537098A1 (en) 2005-03-17
JP2007504139A (ja) 2007-03-01
EP1663210A4 (en) 2009-04-22
AU2004270166A1 (en) 2005-03-17
US7842816B2 (en) 2010-11-30
IL173935A0 (en) 2006-07-05
CN1874768A (zh) 2006-12-06
AR045738A1 (es) 2005-11-09
RU2006109600A (ru) 2007-10-10
WO2005023251A1 (en) 2005-03-17

Similar Documents

Publication Publication Date Title
JP5026076B2 (ja) Ｍｅｋ阻害剤としてのｎ３アルキル化ベンズイミダゾール誘導体
JP5102642B2 (ja) Ｍｅｋ阻害剤としてのｎ３アルキル化ベンズイミダゾール誘導体
JP2005526076A (ja) Ｍｅｋ阻害剤としてのｎ３アルキル化ベンズイミダゾール誘導体
HK1153139B (en) N3 alkylated benzimidazole derivatives as mek inhibitors
HK1141976B (en) N3 alkylated benzimidazole derivatives as mek inhibitors
HK1070823B (en) N3 alkylated benzimidazole derivatives as mek inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20070807

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20070807

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20101210

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20110310

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20110317

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20110408

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20110415

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110510

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20111115

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20120208

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20120215

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20120314

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20120322

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20120413

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20120420

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120507

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20120601

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20120620

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20150629

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Ref document number: 5026076

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313114

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

EXPY Cancellation because of completion of term