TW200524911A - N-substituted pyrazolyl-amidyl-benzimidazolyl C-KIT inhibitors - Google Patents

N-substituted pyrazolyl-amidyl-benzimidazolyl C-KIT inhibitors Download PDF

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Publication number
TW200524911A
TW200524911A TW093125240A TW93125240A TW200524911A TW 200524911 A TW200524911 A TW 200524911A TW 093125240 A TW093125240 A TW 093125240A TW 93125240 A TW93125240 A TW 93125240A TW 200524911 A TW200524911 A TW 200524911A
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TW
Taiwan
Prior art keywords
alkyl
cancer
compound
pharmaceutically acceptable
acceptable salt
Prior art date
Application number
TW093125240A
Other languages
English (en)
Chinese (zh)
Inventor
Joshua Bolger
Arlindo L Castelhano
Andrew Phillip Crew
Radoslaw Laufer
An-Hu Li
Smith Colin Peter Sambrook
Yingchuan Sun
Original Assignee
Osi Pharm Inc
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 Osi Pharm Inc filed Critical Osi Pharm Inc
Publication of TW200524911A publication Critical patent/TW200524911A/zh

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW093125240A 2003-08-21 2004-08-20 N-substituted pyrazolyl-amidyl-benzimidazolyl C-KIT inhibitors TW200524911A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US49676603P 2003-08-21 2003-08-21

Publications (1)

Publication Number Publication Date
TW200524911A true TW200524911A (en) 2005-08-01

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
TW093125240A TW200524911A (en) 2003-08-21 2004-08-20 N-substituted pyrazolyl-amidyl-benzimidazolyl C-KIT inhibitors

Country Status (19)

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

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1797881B1 (en) 2004-09-17 2009-04-15 Eisai R&D Management Co., Ltd. Medicinal composition with improved stability and reduced gelation properties
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
AU2006309551B2 (en) 2005-11-07 2012-04-19 Eisai R & D Management Co., Ltd. Use of combination of anti-angiogenic substance and c-kit kinase inhibitor
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
ES2556173T3 (es) 2006-05-18 2016-01-13 Eisai R&D Management Co., Ltd. Agente antitumoral para un cáncer de tiroides
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
KR101445892B1 (ko) 2007-01-29 2014-09-29 에자이 알앤드디 매니지먼트 가부시키가이샤 미분화형 위암 치료용 조성물
CN101848895B (zh) 2007-11-09 2013-10-23 卫材R&D管理有限公司 血管新生抑制物质和抗肿瘤性铂络合物的组合使用
EP2400985A2 (en) 2009-02-25 2012-01-04 OSI Pharmaceuticals, LLC Combination of an either an anti-igf-1r antibody or an igf binding protein and a small molecule igf-1r kinase inhibitor
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
US8465912B2 (en) 2009-02-27 2013-06-18 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
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
CA2802644C (en) 2010-06-25 2017-02-21 Eisai R & D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
WO2012121168A1 (ja) * 2011-03-04 2012-09-13 国立大学法人京都大学 キナーゼ阻害剤
RU2580609C2 (ru) 2011-04-18 2016-04-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое терапевтическое средство
EP2702173A1 (en) 2011-04-25 2014-03-05 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
EP3444363B1 (en) 2011-06-03 2020-11-25 Eisai R&D Management Co., Ltd. Biomarkers for prediciting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
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
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
JP6423372B2 (ja) 2013-02-28 2018-11-14 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 強力なｒｏｃｋ１およびｒｏｃｋ２阻害剤としてのフェニルピラゾール誘導体
WO2014185540A1 (en) 2013-05-14 2014-11-20 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
AR096654A1 (es) * 2013-06-20 2016-01-27 Ab Science Derivados de benzimidazol como inhibidores selectivos de proteína quinasa
KR102329681B1 (ko) 2014-08-28 2021-11-23 에자이 알앤드디 매니지먼트 가부시키가이샤 고순도의 퀴놀린 유도체 및 이를 제조하는 방법
KR20250024102A (ko) 2015-02-25 2025-02-18 에자이 알앤드디 매니지먼트 가부시키가이샤 퀴놀린 유도체의 고미 억제 방법
AU2015384801B2 (en) 2015-03-04 2022-01-06 Eisai R&D Management Co., Ltd. Combination of a PD-1 antagonist and a VEGFR/FGFR/RET tyrosine kinase inhibitor for treating cancer
ES2886107T3 (es) 2015-06-16 2021-12-16 Prism Biolab Co Ltd Antineoplásico
SG11201801083UA (en) 2015-08-20 2018-03-28 Eisai R&D Man Co Ltd Tumor therapeutic agent
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
US20200197384A1 (en) 2017-05-16 2020-06-25 Eisai R&D Management Co., Ltd. Treatment of hepatocellular carcinoma
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
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
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use

Family Cites Families (36)

* 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
CA2183084A1 (en) 1994-02-10 1995-08-17 John Eugene Macor 5-heteroarylindole derivatives
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
DE69727199T2 (de) 1996-12-09 2004-11-18 Pfizer Inc. Benzimidazol-Verbindungen
US6414008B1 (en) 1997-04-29 2002-07-02 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, the preparation thereof, and their use as pharmaceutical compositions
BR9810456A (pt) 1997-06-27 2001-09-25 Fujisawa Pharmaceutical Co Composto de sulfonamida, método para sua obtenção e seu uso farmacêutico
US5990146A (en) 1997-08-20 1999-11-23 Warner-Lambert Company Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation
WO2000012089A1 (en) 1998-08-31 2000-03-09 Merck & Co., Inc. Novel angiogenesis inhibitors
US6465484B1 (en) 1997-09-26 2002-10-15 Merck & Co., Inc. Angiogenesis inhibitors
US6162804A (en) 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase 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
US6348032B1 (en) * 1998-11-23 2002-02-19 Cell Pathways, Inc. Method of inhibiting neoplastic cells with benzimidazole derivatives
US6329383B1 (en) 1999-01-25 2001-12-11 Pharmacia Ab 2-amino-5-pyrimidine acetic acid compounds
CA2369553A1 (en) 1999-04-02 2000-10-12 Raymond F. Horvath 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
US6534535B1 (en) 1999-08-12 2003-03-18 Millennium Pharmaceuticals, 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
EP1255750A1 (en) 2000-02-01 2002-11-13 Millenium Pharmaceuticals, Inc. INDOLE AND BENZIMIDAZOLE INHIBITORS OF FACTOR Xa
WO2001057019A1 (en) 2000-02-01 2001-08-09 Cor Therapeutics, Inc. INDALONE AND BENZIMIDAZOLONE INHIBITORS OF FACTOR Xa
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
US20020128232A1 (en) 2000-10-12 2002-09-12 Henderson Scott A. Heterocyclic angiogenesis inhibitors
KR100883184B1 (ko) 2000-12-11 2009-02-12 암젠 인코포레이션 Ｃｘｃｒ3 길항제
GB0102109D0 (en) 2001-01-26 2001-03-14 Syngenta Ltd Chemical process
JP2004523565A (ja) 2001-03-05 2004-08-05 トランス　テック　ファーマ，インコーポレイテッド 治療因子としてのベンゾイミダゾール誘導体
JP2004528304A (ja) * 2001-03-12 2004-09-16 アバニール・ファーマシューティカルズ ＩｇＥを調節し、細胞増殖を阻害するためのベンゾイミダゾール化合物
WO2002076960A1 (en) 2001-03-22 2002-10-03 Abbott Gmbh & Co. Kg Transition metal mediated process

Also Published As

Publication number Publication date
JP2007502820A (ja) 2007-02-15
AR045389A1 (es) 2005-10-26
RU2006108791A (ru) 2006-07-27
UA84712C2 (en) 2008-11-25
NO20060665L (no) 2006-05-16
BRPI0413785A (pt) 2006-11-07
JP4795237B2 (ja) 2011-10-19
DE602004017623D1 (de) 2008-12-18
AU2004268948A1 (en) 2005-03-10
CA2536151A1 (en) 2005-03-10
WO2005021537A1 (en) 2005-03-10
AP2006003553A0 (en) 2006-04-30
KR20060115346A (ko) 2006-11-08
IS8320A (is) 2006-02-21
MXPA06002017A (es) 2006-05-31
IL173616A0 (en) 2006-07-05
ATE413395T1 (de) 2008-11-15
EP1664032A1 (en) 2006-06-07
CN1839130A (zh) 2006-09-27
EP1664032B1 (en) 2008-11-05

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