AR045389A1 - Inhibidores del c-kit con estructura de pirazolil-amidil-benzoimidazolilo n-sustituido - Google Patents
Inhibidores del c-kit con estructura de pirazolil-amidil-benzoimidazolilo n-sustituidoInfo
- Publication number
- AR045389A1 AR045389A1 ARP040103010A ARP040103010A AR045389A1 AR 045389 A1 AR045389 A1 AR 045389A1 AR P040103010 A ARP040103010 A AR P040103010A AR P040103010 A ARP040103010 A AR P040103010A AR 045389 A1 AR045389 A1 AR 045389A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cyclyl
- optionally substituted
- heterocyclyl
- alkoxy
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 18
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 125000004122 cyclic group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- -1 N-substituted pyrazolyl-amidyl-benzoimidazolyl structure Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 abstract 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
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)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US49676603P | 2003-08-21 | 2003-08-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045389A1 true AR045389A1 (es) | 2005-10-26 |
Family
ID=34272512
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040103010A AR045389A1 (es) | 2003-08-21 | 2004-08-20 | Inhibidores del c-kit con estructura de pirazolil-amidil-benzoimidazolilo n-sustituido |
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)
| 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 |
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| 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 |
-
2004
- 2004-08-16 AU AU2004268948A patent/AU2004268948A1/en not_active Abandoned
- 2004-08-16 MX MXPA06002017A patent/MXPA06002017A/es unknown
- 2004-08-16 AT AT04781203T patent/ATE413395T1/de not_active IP Right Cessation
- 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 RU RU2006108791/04A patent/RU2006108791A/ru not_active Application Discontinuation
- 2004-08-16 AP AP2006003553A patent/AP2006003553A0/xx unknown
- 2004-08-16 CN CNA2004800239977A patent/CN1839130A/zh active Pending
- 2004-08-16 CA CA002536151A patent/CA2536151A1/en not_active Abandoned
- 2004-08-16 KR KR1020067003094A patent/KR20060115346A/ko not_active Withdrawn
- 2004-08-16 EP EP04781203A patent/EP1664032B1/en not_active Expired - Lifetime
- 2004-08-16 JP JP2006523954A patent/JP4795237B2/ja not_active Expired - Fee Related
- 2004-08-16 DE DE602004017623T patent/DE602004017623D1/de not_active Expired - Lifetime
- 2004-08-16 WO PCT/US2004/026481 patent/WO2005021537A1/en not_active Ceased
- 2004-08-20 TW TW093125240A patent/TW200524911A/zh unknown
- 2004-08-20 AR ARP040103010A patent/AR045389A1/es not_active Application Discontinuation
-
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
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 |
| TW200524911A (en) | 2005-08-01 |
| WO2005021537A1 (en) | 2005-03-10 |
| JP2007502820A (ja) | 2007-02-15 |
| IS8320A (is) | 2006-02-21 |
| DE602004017623D1 (de) | 2008-12-18 |
| 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 |
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