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

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

Info

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
Authority
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

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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

ID=34272512

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 (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE428421T1 (de) 2004-09-17 2009-05-15 Eisai R&D Man Co Ltd Medizinische zusammensetzung mit verbesserter stabilität und reduzierten gelierungseigenschaften
JP4989476B2 (ja) 2005-08-02 2012-08-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 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
WO2007083904A1 (en) * 2006-01-18 2007-07-26 Lg Household & Health Care Ltd. C-kit activation inhibitor, skin whitening compound and composition for skin whitening containing the same
TW200740776A (en) * 2006-02-06 2007-11-01 Osi Pharm Inc N-phenylbenzotriazolyl c-kit inhibitors
CN104706637A (zh) * 2006-05-18 2015-06-17 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
WO2008026748A1 (en) 2006-08-28 2008-03-06 Eisai R & D Management Co., Ltd. Antitumor agent for undifferentiated gastric cancer
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
CA2676796C (en) 2007-01-29 2016-02-23 Eisai R & D Management Co., Ltd. Composition for treatment of undifferentiated gastric cancer
US8952035B2 (en) 2007-11-09 2015-02-10 Eisai R&D Management Co., Ltd. Combination of anti-angiogenic substance and anti-tumor platinum complex
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
WO2010099364A2 (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
WO2010099363A1 (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
MY162940A (en) 2009-08-19 2017-07-31 Eisai R&D Man Co Ltd Quinoline derivative-containing pharmaceutical composition
CN102958523B (zh) 2010-06-25 2014-11-19 卫材R&D管理有限公司 使用具有激酶抑制作用的组合的抗肿瘤剂
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
WO2012149014A1 (en) 2011-04-25 2012-11-01 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
KR20150098605A (ko) 2012-12-21 2015-08-28 에자이 알앤드디 매니지먼트 가부시키가이샤 퀴놀린 유도체의 비정질 형태 및 그의 제조방법
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
CN105102448B (zh) 2013-02-28 2018-03-06 百时美施贵宝公司 作为rock1和rock2抑制剂的苯基吡唑衍生物
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
NZ714049A (en) 2013-05-14 2020-05-29 Eisai R&D Man 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
LT3263106T (lt) 2015-02-25 2024-01-10 Eisai R&D Management Co., Ltd. Chinolino darinių kartumo sumažinimo būdas
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
MX373231B (es) 2015-06-16 2020-05-08 Eisai R&D Man Co Ltd Agente anticancerigeno.
US12220398B2 (en) 2015-08-20 2025-02-11 Eisai R&D Management Co., Ltd. Tumor therapeutic agent
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
RU2019134940A (ru) 2017-05-16 2021-06-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Лечение гепатоцеллюлярной карциномы
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
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
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
US6001866A (en) 1995-10-05 1999-12-14 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
AU6966696A (en) 1995-10-05 1997-04-28 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
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
DK0846689T3 (da) 1996-12-09 2004-04-19 Pfizer Benzimidazolforbindelser
US6414008B1 (en) 1997-04-29 2002-07-02 Boehringer Ingelheim Pharma Kg Disubstituted bicyclic heterocycles, the preparation thereof, and their use as pharmaceutical compositions
AU745081B2 (en) 1997-06-27 2002-03-14 Fujisawa Pharmaceutical Co., Ltd. Sulfonamide compounds and medicinal use thereof
US5990146A (en) 1997-08-20 1999-11-23 Warner-Lambert Company Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation
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
US6444617B1 (en) 1998-07-28 2002-09-03 Nihon Nohyaku Co., Ltd. Fused-heterocycle dicarboxylic acid diamide derivatives or salts thereof, herbicide and usage thereof
CA2341409A1 (en) 1998-08-31 2000-03-09 Merck And Co., Inc. Novel angiogenesis inhibitors
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
EP1214330A1 (en) 1999-09-21 2002-06-19 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
AU2002216314A1 (en) 2000-10-12 2002-04-22 Scott A Henderson Heterocyclic angiogenesis inhibitors
NZ526622A (en) 2000-12-11 2006-07-28 Amgen Sf Llc CXCR3 antagonists
GB0102109D0 (en) 2001-01-26 2001-03-14 Syngenta Ltd Chemical process
CN1235583C (zh) 2001-03-05 2006-01-11 特兰斯泰克制药公司 用作治疗剂的苯并咪唑衍生物
CZ20032691A3 (en) * 2001-03-12 2004-04-14 Avanir Pharmaceuticals Benzimidazole compounds for modulating ige and inhibiting cellular proliferation
US20030009034A1 (en) 2001-03-22 2003-01-09 Neil Wishart Transition metal mediated process

Also Published As

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

Similar Documents

Publication Publication Date Title
TW200524911A (en) N-substituted pyrazolyl-amidyl-benzimidazolyl C-KIT inhibitors
US7485658B2 (en) N-substituted pyrazolyl-amidyl-benzimidazolyl c-Kit inhibitors
US10858359B2 (en) Heterocyclic ring derivatives useful as SHP2 inhibitors
KR101812390B1 (ko) 키나제 억제제로서의 치환된 트리시클릭 벤즈이미다졸
AU2006233535B2 (en) (LH-indol-7-YL)-( (pyrimidin-2 -YL-amino) methanone derivatives and related compounds as IGF-RL inhibitors for treating cancer
AU2005299384B2 (en) (2-carboxamido)(3-amino) thiophene compounds
US20070232669A1 (en) N-phenylbenzotriazolyl c-kit inhibitors
CN101848908B (zh) 激酶抑制剂的组合物及其在治疗癌症和其它与激酶相关的疾病中的用途
US7767673B2 (en) N-substituted imidazopyridine c-Kit inhibitors
TWI697490B (zh) 用於作為shp2抑制劑之新穎雜環衍生物
CA2512608C (en) (2-carboxamido)(3-amino) thiophene compounds
KR20070029246A (ko) Parp 저해제로서의 프탈아진 유도체
MXPA06002019A (es) Imidazopiridinas n3 sustituidas inhibidoras de c_kit.
AU2010333083B2 (en) 3-(indolyl)- or 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
WO2001064680A1 (en) Myt1 kinase inhibitors
CN113840823B (zh) 显示癌细胞生长抑制效果的新型杂环取代的嘧啶衍生物,以及包含其的药物组合物
WO2006034075A1 (en) (hydrazido) (amino) thiophene compounds
CN100471841C (zh) (2-甲酰胺基)(3-氨基)噻吩化合物
ES2371928T3 (es) Nuevos aza-heterociclos que actúan como inhibidores de la quinasa.
NZ757707B2 (en) Compounds and compositions for treating hematological disorders