JP2007502820A5 - - Google Patents
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- Publication number
- JP2007502820A5 JP2007502820A5 JP2006523954A JP2006523954A JP2007502820A5 JP 2007502820 A5 JP2007502820 A5 JP 2007502820A5 JP 2006523954 A JP2006523954 A JP 2006523954A JP 2006523954 A JP2006523954 A JP 2006523954A JP 2007502820 A5 JP2007502820 A5 JP 2007502820A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cancer
- benzimidazole
- carboxamide
- pharmaceutically acceptable
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 150000001204 N-oxides Chemical class 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000011780 sodium chloride Substances 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 230000003463 hyperproliferative Effects 0.000 claims 7
- 239000002246 antineoplastic agent Substances 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- -1 3,5-dimethoxyphenyl Chemical group 0.000 claims 2
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 201000009030 carcinoma Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- UPQTXQWNEOLBOJ-UHFFFAOYSA-N 1-(3-fluorophenyl)-N-(2-methyl-5-phenylpyrazol-3-yl)benzimidazole-5-carboxamide Chemical compound CN1N=C(C=2C=CC=CC=2)C=C1NC(=O)C(C=C1N=C2)=CC=C1N2C1=CC=CC(F)=C1 UPQTXQWNEOLBOJ-UHFFFAOYSA-N 0.000 claims 1
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 208000002517 Adenoid Cystic Carcinoma Diseases 0.000 claims 1
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 206010024324 Leukaemias Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000008968 Lymphoma, Large-Cell, Anaplastic Diseases 0.000 claims 1
- 206010025650 Malignant melanoma Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000587 Small Cell Lung Carcinoma Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 201000003076 angiosarcoma Diseases 0.000 claims 1
- 230000001772 anti-angiogenic Effects 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 201000011231 colorectal cancer Diseases 0.000 claims 1
- 230000001472 cytotoxic Effects 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002496 gastric Effects 0.000 claims 1
- 230000002147 killing Effects 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 201000001514 prostate carcinoma Diseases 0.000 claims 1
- 201000007416 salivary gland adenoid cystic carcinoma Diseases 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005161 thyroid carcinoma Diseases 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
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)
Publication Number | Publication Date |
---|---|
JP2007502820A JP2007502820A (ja) | 2007-02-15 |
JP2007502820A5 true JP2007502820A5 (US07585860-20090908-C00112.png) | 2007-10-04 |
JP4795237B2 JP4795237B2 (ja) | 2011-10-19 |
Family
ID=34272512
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
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)
Families Citing this family (33)
Publication number | Priority date | Publication date | Assignee | Title |
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JP4834553B2 (ja) | 2004-09-17 | 2011-12-14 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 医薬組成物 |
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 |
JPWO2007052849A1 (ja) | 2005-11-07 | 2009-04-30 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 血管新生阻害物質とc−kitキナーゼ阻害物質との併用 |
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 |
CA2652442C (en) | 2006-05-18 | 2014-12-09 | Eisai R & D Management Co., Ltd. | Antitumor agent for thyroid cancer |
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 |
CA2676796C (en) | 2007-01-29 | 2016-02-23 | Eisai R & D Management Co., Ltd. | Composition for treatment of undifferentiated gastric cancer |
KR101513326B1 (ko) | 2007-11-09 | 2015-04-17 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 혈관 신생 저해 물질과 항종양성 백금 착물의 병용 |
JP2012518657A (ja) | 2009-02-25 | 2012-08-16 | オーエスアイ・ファーマシューティカルズ,エルエルシー | 併用抗癌治療 |
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 |
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 |
JP2014519813A (ja) | 2011-04-25 | 2014-08-21 | オーエスアイ・ファーマシューティカルズ,エルエルシー | 癌薬剤発見、診断、および治療におけるemt遺伝子シグネチャーの使用 |
EP2714937B1 (en) | 2011-06-03 | 2018-11-14 | Eisai R&D Management Co., Ltd. | Biomarkers for predicting 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 |
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 |
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 |
SG11201509278XA (en) | 2013-05-14 | 2015-12-30 | Eisai R&D Man 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 |
IL302218B1 (en) | 2014-08-28 | 2024-06-01 | Eisai R&D Man Co Ltd | Methods for the production of lanvotinib and its derivatives in a high degree of purity |
DK3263106T3 (da) | 2015-02-25 | 2024-01-08 | Eisai R&D Man Co Ltd | Fremgangsmåde til undertrykkelse af bitterhed af quinolinderivat |
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 |
EP3311841B1 (en) | 2015-06-16 | 2021-07-28 | PRISM BioLab Co., Ltd. | Anticancer agent |
BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
AU2020378630A1 (en) | 2019-11-08 | 2022-05-26 | INSERM (Institut 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 |
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-
2004
- 2004-08-16 DE DE602004017623T patent/DE602004017623D1/de active Active
- 2004-08-16 WO PCT/US2004/026481 patent/WO2005021537A1/en active Application Filing
- 2004-08-16 JP JP2006523954A patent/JP4795237B2/ja not_active Expired - Fee Related
- 2004-08-16 CN CNA2004800239977A patent/CN1839130A/zh active Pending
- 2004-08-16 CA CA002536151A patent/CA2536151A1/en not_active Abandoned
- 2004-08-16 RU RU2006108791/04A patent/RU2006108791A/ru not_active Application Discontinuation
- 2004-08-16 UA UAA200602943A patent/UA84712C2/ru unknown
- 2004-08-16 BR BRPI0413785-0A patent/BRPI0413785A/pt not_active IP Right Cessation
- 2004-08-16 AU AU2004268948A patent/AU2004268948A1/en not_active Abandoned
- 2004-08-16 AP AP2006003553A patent/AP2006003553A0/xx unknown
- 2004-08-16 KR KR1020067003094A patent/KR20060115346A/ko not_active Application Discontinuation
- 2004-08-16 AT AT04781203T patent/ATE413395T1/de not_active IP Right Cessation
- 2004-08-16 EP EP04781203A patent/EP1664032B1/en active Active
- 2004-08-16 MX MXPA06002017A patent/MXPA06002017A/es unknown
- 2004-08-20 AR ARP040103010A patent/AR045389A1/es not_active Application Discontinuation
- 2004-08-20 TW TW093125240A patent/TW200524911A/zh unknown
-
2006
- 2006-02-08 IL IL173616A patent/IL173616A0/en unknown
- 2006-02-10 NO NO20060665A patent/NO20060665L/no not_active Application Discontinuation
- 2006-02-21 IS IS8320A patent/IS8320A/is unknown