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)
- 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)
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 (OSRAM) |
| JP (1) | JP4795237B2 (OSRAM) |
| KR (1) | KR20060115346A (OSRAM) |
| CN (1) | CN1839130A (OSRAM) |
| AP (1) | AP2006003553A0 (OSRAM) |
| AR (1) | AR045389A1 (OSRAM) |
| AT (1) | ATE413395T1 (OSRAM) |
| AU (1) | AU2004268948A1 (OSRAM) |
| BR (1) | BRPI0413785A (OSRAM) |
| CA (1) | CA2536151A1 (OSRAM) |
| DE (1) | DE602004017623D1 (OSRAM) |
| IL (1) | IL173616A0 (OSRAM) |
| IS (1) | IS8320A (OSRAM) |
| MX (1) | MXPA06002017A (OSRAM) |
| NO (1) | NO20060665L (OSRAM) |
| RU (1) | RU2006108791A (OSRAM) |
| TW (1) | TW200524911A (OSRAM) |
| UA (1) | UA84712C2 (OSRAM) |
| WO (1) | WO2005021537A1 (OSRAM) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006030826A1 (ja) | 2004-09-17 | 2006-03-23 | Eisai R & D Management Co., Ltd. | 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 |
| WO2007052849A1 (ja) | 2005-11-07 | 2007-05-10 | Eisai R & D Management Co., Ltd. | 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 |
| KR101472600B1 (ko) | 2006-08-28 | 2014-12-15 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 미분화형 위암에 대한 항종양제 |
| 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 |
| WO2009060945A1 (ja) | 2007-11-09 | 2009-05-14 | Eisai R & D Management Co., Ltd. | 血管新生阻害物質と抗腫瘍性白金錯体との併用 |
| 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 |
| JP2012519281A (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 |
| 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 |
| 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 |
| 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 |
| CA2828946C (en) | 2011-04-18 | 2016-06-21 | Eisai R&D Management Co., Ltd. | Therapeutic agent for tumor |
| EP2702173A1 (en) | 2011-04-25 | 2014-03-05 | OSI Pharmaceuticals, LLC | Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment |
| US9945862B2 (en) | 2011-06-03 | 2018-04-17 | 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 |
| MX2015004979A (es) | 2012-12-21 | 2015-07-17 | Eisai R&D Man Co Ltd | Forma amorfa de derivado de quinolina y metodo para su produccion. |
| 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 |
| 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 |
| 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 |
| IL302218B2 (en) | 2014-08-28 | 2024-10-01 | Eisai R&D Man Co Ltd | Methods for manufacturing high-purity lenvatinib and its derivatives |
| JP6792546B2 (ja) | 2015-02-25 | 2020-11-25 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | キノリン誘導体の苦味抑制方法 |
| 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 |
| CN108135894B (zh) | 2015-08-20 | 2021-02-19 | 卫材R&D管理有限公司 | 肿瘤治疗剂 |
| RU2750539C2 (ru) | 2017-02-08 | 2021-06-29 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Фармацевтическая композиция для лечения опухоли |
| AU2018269996A1 (en) | 2017-05-16 | 2019-11-21 | 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 |
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| 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 |
| AU685881B2 (en) | 1994-02-10 | 1998-01-29 | Pfizer Inc. | 5-heteroarylindole derivatives as benzodiazepine receptor site agonists and antagonists |
| 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 |
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| WO1997012613A1 (en) | 1995-10-05 | 1997-04-10 | 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 |
| ES2212054T3 (es) | 1996-12-09 | 2004-07-16 | Pfizer Inc. | Compuestos de bencimidazol. |
| US6414008B1 (en) | 1997-04-29 | 2002-07-02 | Boehringer Ingelheim Pharma Kg | Disubstituted bicyclic heterocycles, the preparation thereof, and their use as pharmaceutical compositions |
| EP0995742A4 (en) | 1997-06-27 | 2004-08-25 | Fujisawa Pharmaceutical Co | SULPHONAMIDE COMPOUNDS AND THEIR MEDICAL USE |
| US5990146A (en) | 1997-08-20 | 1999-11-23 | Warner-Lambert Company | Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation |
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| US6162804A (en) | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| WO2000012089A1 (en) | 1998-08-31 | 2000-03-09 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| KR20010079546A (ko) | 1998-07-28 | 2001-08-22 | 무라타 도시카즈 | 융합 헤테로환 디카르복실산 디아미드 유도체 또는 그의염, 제초제 및 그의 용도 |
| US6326379B1 (en) | 1998-09-16 | 2001-12-04 | Bristol-Myers Squibb Co. | Fused pyridine inhibitors of cGMP phosphodiesterase |
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| 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 |
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| US20020072530A1 (en) | 2000-02-01 | 2002-06-13 | Bing-Yan Zhu | Indole and benzimidazole inhibitors of factor Xa |
| EP1263754A1 (en) | 2000-02-01 | 2002-12-11 | Millennium Pharmaceuticals, 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 |
| BR0116096A (pt) | 2000-12-11 | 2005-10-18 | Tularik Inc | Composto, composição farmacêutica, e, métodos para tratar uma condição ou doença inflamatória ou imune em um paciente, para tratar uma condição ou doença mediada por cxcr3 em um paciente, e para a modulação da função de cxcr3 em uma célula |
| GB0102109D0 (en) | 2001-01-26 | 2001-03-14 | Syngenta Ltd | Chemical process |
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| ES2291455T3 (es) | 2001-03-12 | 2008-03-01 | Avanir Pharmaceuticals | Compuestos de bencimidazol para modular ige e inhibir la proliferacion celular. |
| US20030009034A1 (en) | 2001-03-22 | 2003-01-09 | Neil Wishart | Transition metal mediated process |
-
2004
- 2004-08-16 EP EP04781203A patent/EP1664032B1/en not_active Expired - Lifetime
- 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 CA CA002536151A patent/CA2536151A1/en not_active Abandoned
- 2004-08-16 DE DE602004017623T patent/DE602004017623D1/de not_active Expired - Lifetime
- 2004-08-16 AT AT04781203T patent/ATE413395T1/de not_active IP Right Cessation
- 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 MX MXPA06002017A patent/MXPA06002017A/es unknown
- 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 UA UAA200602943A patent/UA84712C2/ru unknown
- 2004-08-16 KR KR1020067003094A patent/KR20060115346A/ko not_active Withdrawn
- 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 |
|---|---|
| AP2006003553A0 (en) | 2006-04-30 |
| MXPA06002017A (es) | 2006-05-31 |
| IS8320A (is) | 2006-02-21 |
| AU2004268948A1 (en) | 2005-03-10 |
| CN1839130A (zh) | 2006-09-27 |
| CA2536151A1 (en) | 2005-03-10 |
| IL173616A0 (en) | 2006-07-05 |
| TW200524911A (en) | 2005-08-01 |
| JP2007502820A (ja) | 2007-02-15 |
| JP4795237B2 (ja) | 2011-10-19 |
| UA84712C2 (en) | 2008-11-25 |
| EP1664032A1 (en) | 2006-06-07 |
| DE602004017623D1 (de) | 2008-12-18 |
| WO2005021537A1 (en) | 2005-03-10 |
| BRPI0413785A (pt) | 2006-11-07 |
| KR20060115346A (ko) | 2006-11-08 |
| RU2006108791A (ru) | 2006-07-27 |
| EP1664032B1 (en) | 2008-11-05 |
| ATE413395T1 (de) | 2008-11-15 |
| NO20060665L (no) | 2006-05-16 |
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