JP4795237B2 - N−置換ピラゾリル−アミジル−ベンズイミダゾリルc−Kit阻害剤 - Google Patents

N−置換ピラゾリル−アミジル−ベンズイミダゾリルc−Kit阻害剤 Download PDF

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JP4795237B2
JP4795237B2 JP2006523954A JP2006523954A JP4795237B2 JP 4795237 B2 JP4795237 B2 JP 4795237B2 JP 2006523954 A JP2006523954 A JP 2006523954A JP 2006523954 A JP2006523954 A JP 2006523954A JP 4795237 B2 JP4795237 B2 JP 4795237B2
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alkyl
benzimidazole
acid
carboxamide
pharmaceutically acceptable
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Japanese (ja)
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JP2007502820A5 (https=
JP2007502820A (ja
Inventor
ボルジヤー,ジヨシユア
カステラーノ,アルリンド・エル
クルー,アンドリユー・フイリツプ
ローフアー,ラドスロウ
リー,アン−フー
サンブロツク・スミス,コリン・ピーター
スン,インチユアン
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オーエスアイ・フアーマシユーテイカルズ・エル・エル・シー
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    • 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2006523954A 2003-08-21 2004-08-16 N−置換ピラゾリル−アミジル−ベンズイミダゾリルc−Kit阻害剤 Expired - Fee Related JP4795237B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US49676603P 2003-08-21 2003-08-21
US60/496,766 2003-08-21
PCT/US2004/026481 WO2005021537A1 (en) 2003-08-21 2004-08-16 N-substituted pyrazolyl-amidyl-benzimidazolyl c-kit inhibitors

Publications (3)

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JP2007502820A JP2007502820A (ja) 2007-02-15
JP2007502820A5 JP2007502820A5 (https=) 2007-10-04
JP4795237B2 true JP4795237B2 (ja) 2011-10-19

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JP2006523954A Expired - Fee Related JP4795237B2 (ja) 2003-08-21 2004-08-16 N−置換ピラゾリル−アミジル−ベンズイミダゾリルc−Kit阻害剤

Country Status (19)

Country Link
EP (1) EP1664032B1 (https=)
JP (1) JP4795237B2 (https=)
KR (1) KR20060115346A (https=)
CN (1) CN1839130A (https=)
AP (1) AP2006003553A0 (https=)
AR (1) AR045389A1 (https=)
AT (1) ATE413395T1 (https=)
AU (1) AU2004268948A1 (https=)
BR (1) BRPI0413785A (https=)
CA (1) CA2536151A1 (https=)
DE (1) DE602004017623D1 (https=)
IL (1) IL173616A0 (https=)
IS (1) IS8320A (https=)
MX (1) MXPA06002017A (https=)
NO (1) NO20060665L (https=)
RU (1) RU2006108791A (https=)
TW (1) TW200524911A (https=)
UA (1) UA84712C2 (https=)
WO (1) WO2005021537A1 (https=)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005283422C1 (en) 2004-09-17 2017-02-02 Eisai R & D Management Co., Ltd. Medicinal composition
WO2007015578A1 (ja) 2005-08-02 2007-02-08 Eisai R & D Management Co., Ltd. 血管新生阻害物質の効果を検定する方法
CN101316590B (zh) 2005-11-07 2011-08-03 卫材R&D管理有限公司 血管生成抑制剂和c-kit激酶抑制剂的组合使用
JP5583346B2 (ja) * 2006-01-18 2014-09-03 エルジー ハウスホールド アンド ヘルスケア リミテッド c−Kit活性阻害剤、及び、肌美白剤
TW200740776A (en) * 2006-02-06 2007-11-01 Osi Pharm Inc N-phenylbenzotriazolyl c-kit inhibitors
RU2448708C3 (ru) * 2006-05-18 2017-09-28 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое средство против рака щитовидной железы
CN101511793B (zh) 2006-08-28 2011-08-03 卫材R&D管理有限公司 针对未分化型胃癌的抗肿瘤剂
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
CN101600694A (zh) 2007-01-29 2009-12-09 卫材R&D管理有限公司 未分化型胃癌治疗用组合物
KR101513326B1 (ko) 2007-11-09 2015-04-17 에자이 알앤드디 매니지먼트 가부시키가이샤 혈관 신생 저해 물질과 항종양성 백금 착물의 병용
WO2010099139A2 (en) 2009-02-25 2010-09-02 Osi Pharmaceuticals, Inc. Combination anti-cancer therapy
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
EP2401614A1 (en) 2009-02-27 2012-01-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
JP2012519282A (ja) 2009-02-27 2012-08-23 オーエスアイ・ファーマシューティカルズ,エルエルシー 間葉様腫瘍細胞またはその生成を阻害する薬剤を同定するための方法
DK2468281T3 (en) 2009-08-19 2016-03-21 Eisai R&D Man Co Ltd Quinolinderivatholdig pharmaceutical composition
WO2011162343A1 (ja) 2010-06-25 2011-12-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 キナーゼ阻害作用を有する化合物の併用による抗腫瘍剤
JPWO2012121168A1 (ja) * 2011-03-04 2014-07-17 国立大学法人京都大学 キナーゼ阻害剤
CN103402519B (zh) 2011-04-18 2015-11-25 卫材R&D管理有限公司 肿瘤治疗剂
EP2702173A1 (en) 2011-04-25 2014-03-05 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
JP6038128B2 (ja) 2011-06-03 2016-12-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 レンバチニブ化合物に対する甲状腺癌対象及び腎臓癌対象の反応性を予測及び評価するためのバイオマーカー
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
US20140179712A1 (en) 2012-12-21 2014-06-26 Astrazeneca Ab Pharmaceutical formulation of n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2h-pyrazol-3-yl]-4-[(3r,5s)-3,5-dimethylpiperazin-1-yl]benzamide
AU2013364953A1 (en) 2012-12-21 2015-04-30 Eisai R&D Management Co., Ltd. Amorphous form of quinoline derivative, and method for producing same
WO2014134391A1 (en) 2013-02-28 2014-09-04 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
EP2997377B1 (en) 2013-05-14 2018-07-18 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
TW201534597A (zh) 2013-06-20 2015-09-16 Ab Science 作為選擇性蛋白質激酶抑制劑之苯并咪唑衍生物
PT3524595T (pt) 2014-08-28 2022-09-19 Eisai R&D Man Co Ltd Derivado de quinolina altamente puro e método para produção do mesmo
AU2016224583B2 (en) 2015-02-25 2021-06-03 Eisai R&D Management Co., Ltd. Method for suppressing bitterness of quinoline derivative
KR102662228B1 (ko) 2015-03-04 2024-05-02 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
BR112017027227B1 (pt) 2015-06-16 2023-12-12 Eisai R&D Management Co., Ltd Agente anti-câncer
JP6553726B2 (ja) 2015-08-20 2019-07-31 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療剤
JP6581320B2 (ja) 2017-02-08 2019-09-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療用医薬組成物
EP3624800A4 (en) 2017-05-16 2021-02-17 Eisai R&D Management Co., Ltd. TREATMENT OF HEPATOCELLULAR CARCINOMA
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) 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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6218388B1 (en) * 1997-08-20 2001-04-17 Warner-Lambert Company Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation
US6348032B1 (en) * 1998-11-23 2002-02-19 Cell Pathways, Inc. Method of inhibiting neoplastic cells with benzimidazole derivatives
WO2002072090A1 (en) * 2001-03-12 2002-09-19 Avanir Pharmaceuticals Benzimidazole compounds for modulating ige and inhibiting cellular proliferation

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6087380A (en) 1949-11-24 2000-07-11 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, the preparations and the use thereof as pharmaceutical compositions
GB8610980D0 (en) 1986-05-06 1986-06-11 Ici America Inc Heterocyclic fused tricyclic compounds
US5814651A (en) 1992-12-02 1998-09-29 Pfizer Inc. Catechol diethers as selective PDEIV inhibitors
JP2829788B2 (ja) 1994-02-10 1998-12-02 ファイザー インク. ベンゾジアゼピン受容体部位アゴニスト及びアンタゴニストとしての5−ヘテロアリールインドール誘導体
US5563143A (en) 1994-09-21 1996-10-08 Pfizer Inc. Catechol diether compounds as inhibitors of TNF release
WO1997012613A1 (en) 1995-10-05 1997-04-10 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US5972980A (en) 1995-10-05 1999-10-26 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US6001866A (en) 1995-10-05 1999-12-14 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US6548524B2 (en) 1996-10-16 2003-04-15 American Cyanamid Company Preparation and use of ortho-sulfonamido bicyclic heteroaryl hydroxamic acids as matrix metalloproteinase and TACE inhibitors
EP0846689B1 (en) 1996-12-09 2004-01-14 Pfizer Inc. Benzimidazole compounds
US6414008B1 (en) 1997-04-29 2002-07-02 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, the preparation thereof, and their use as pharmaceutical compositions
IL133575A0 (en) 1997-06-27 2001-04-30 Fujisawa Pharmaceutical Co Sulfonamide compounds, a method for producing same and pharmaceutical compositions containing same
US6162804A (en) 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
US6465484B1 (en) 1997-09-26 2002-10-15 Merck & Co., Inc. Angiogenesis inhibitors
WO2000012089A1 (en) 1998-08-31 2000-03-09 Merck & Co., Inc. Novel angiogenesis inhibitors
CN1311778A (zh) 1998-07-28 2001-09-05 日本农药株式会社 稠杂环二羧酸二酰胺衍生物或其盐,应用上述物质的除草剂及其使用方法
US6326379B1 (en) 1998-09-16 2001-12-04 Bristol-Myers Squibb Co. Fused pyridine inhibitors of cGMP phosphodiesterase
US6329383B1 (en) 1999-01-25 2001-12-11 Pharmacia Ab 2-amino-5-pyrimidine acetic acid compounds
WO2000059888A1 (en) 1999-04-02 2000-10-12 Neurogen Corporation N-benzimidazolylmethyl- and n-indolylmethyl-benzamides and their use as crf modulators
CO5190696A1 (es) 1999-06-16 2002-08-29 Smithkline Beecham Corp Antagonistas de los receptores il-8
AU6762400A (en) 1999-08-12 2001-03-13 Cor Therapeutics, Inc. Inhibitors of factor xa
DE19939463A1 (de) 1999-08-20 2001-02-22 Boehringer Ingelheim Pharma Aminocarbonyl-substituierte Benzimidazolderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
EP1085372B1 (en) 1999-09-13 2004-12-22 Eastman Kodak Company Photographic material having improved color reproduction
WO2001021634A1 (en) 1999-09-21 2001-03-29 Lion Bioscience Ag Benzimidazole derivatives and combinatorial libraries thereof
US6316474B1 (en) 1999-10-29 2001-11-13 Merck & Co., Inc. 2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists
US20020072530A1 (en) 2000-02-01 2002-06-13 Bing-Yan Zhu Indole and benzimidazole inhibitors of factor Xa
US20020019395A1 (en) 2000-02-01 2002-02-14 Bing-Yan Zhu Indalone and benzimidazolone inhibitors of factor Xa
US7087632B2 (en) 2001-03-05 2006-08-08 Transtech Pharma, Inc. Benzimidazole derivatives as therapeutic agents
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
AU2002216314A1 (en) 2000-10-12 2002-04-22 Scott A Henderson Heterocyclic angiogenesis inhibitors
MXPA03005152A (es) 2000-12-11 2004-10-14 Tularik Inc Antogonista de cxcr3.
GB0102109D0 (en) 2001-01-26 2001-03-14 Syngenta Ltd Chemical process
US20030009034A1 (en) 2001-03-22 2003-01-09 Neil Wishart Transition metal mediated process

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6218388B1 (en) * 1997-08-20 2001-04-17 Warner-Lambert Company Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation
US6348032B1 (en) * 1998-11-23 2002-02-19 Cell Pathways, Inc. Method of inhibiting neoplastic cells with benzimidazole derivatives
WO2002072090A1 (en) * 2001-03-12 2002-09-19 Avanir Pharmaceuticals Benzimidazole compounds for modulating ige and inhibiting cellular proliferation

Also Published As

Publication number Publication date
KR20060115346A (ko) 2006-11-08
AP2006003553A0 (en) 2006-04-30
MXPA06002017A (es) 2006-05-31
DE602004017623D1 (de) 2008-12-18
UA84712C2 (en) 2008-11-25
WO2005021537A1 (en) 2005-03-10
IS8320A (is) 2006-02-21
EP1664032B1 (en) 2008-11-05
EP1664032A1 (en) 2006-06-07
ATE413395T1 (de) 2008-11-15
IL173616A0 (en) 2006-07-05
BRPI0413785A (pt) 2006-11-07
AR045389A1 (es) 2005-10-26
NO20060665L (no) 2006-05-16
RU2006108791A (ru) 2006-07-27
CN1839130A (zh) 2006-09-27
AU2004268948A1 (en) 2005-03-10
CA2536151A1 (en) 2005-03-10
JP2007502820A (ja) 2007-02-15
TW200524911A (en) 2005-08-01

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