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
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)
Abstract
La presente se refiere a inhibidores del c-kit con estructura de pirazolil-amidil-benzoimidazolilo N-sustituido, composiciones farmacéuticas que los comprenden y usos. Reivindicación 1: un compuesto representado por la fórmula (1) o una sal o N-óxido farmacéuticamente aceptable del mismo, en donde R11 es F, Cl, alquilo C0-8, alcoxi C0-8, o -N(alquilo C0-8)(alquilo C0-8); R51 es fenilo, opcionalmente sustituido con 1-5 sustituyentes independientes; halógeno, NR34R35, -NR34COR35, -NR34C(O)OR35, -NR34SO2R35, -OR34, -SR34, -SO2R34, -SO2NR34R35, -C(O)OR34, -CO2H, -CONR34R35, alquilo C0-8, alquenilo C2-8, alquinilo C2-8, CN, CF3, NO2, oxo, ciclilo o heterociclilo; r52 es halógeno, CF3, -CN, alquilo C0-8, alcoxi C0-8, -COOH, o -N(alquil C0-8)(alquiloC0-8); X es un grupo ciclilo o heterociclilo, opcionalmente sustituido con 1-4 sustituyentes independientes: F, Cl. CF3, -CN, alquilo C0-8, alcoxi C0-8, -COOH, o -N(alquil C0-8)(alquilo C0-8); R34 y R35 son independientemente alquilo C0-8 opcionalmente sustituido con un sustituyentes heterociclilo u OH; -alquilo C0-8-cicloalquilo C3-8, CF3, -alquilo C0-8-O-alquilo C0-8, -alquilo C0-8-N(alquilo C08-)(alquiloC0-8), -alquilo C0-8-s(O)0-2-alquilo C0-8; o heterociclilo opcionalmente sustituido con alquilo C0-8, ciclilo o sustituyente ciclilo sustituido.
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 (es) |
JP (1) | JP4795237B2 (es) |
KR (1) | KR20060115346A (es) |
CN (1) | CN1839130A (es) |
AP (1) | AP2006003553A0 (es) |
AR (1) | AR045389A1 (es) |
AT (1) | ATE413395T1 (es) |
AU (1) | AU2004268948A1 (es) |
BR (1) | BRPI0413785A (es) |
CA (1) | CA2536151A1 (es) |
DE (1) | DE602004017623D1 (es) |
IL (1) | IL173616A0 (es) |
IS (1) | IS8320A (es) |
MX (1) | MXPA06002017A (es) |
NO (1) | NO20060665L (es) |
RU (1) | RU2006108791A (es) |
TW (1) | TW200524911A (es) |
UA (1) | UA84712C2 (es) |
WO (1) | WO2005021537A1 (es) |
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KR20070053205A (ko) | 2004-09-17 | 2007-05-23 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 의약 조성물 |
EP1925676A4 (en) | 2005-08-02 | 2010-11-10 | Eisai R&D Man Co Ltd | TEST METHOD FOR THE EFFECT OF A VASCULARIZATION INHIBITOR |
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 |
EP2036557B1 (en) | 2006-05-18 | 2015-10-21 | Eisai R&D Management Co., Ltd. | Antitumor agent for thyroid cancer |
WO2008026748A1 (fr) | 2006-08-28 | 2008-03-06 | Eisai R & D Management Co., Ltd. | Agent antitumoral pour cancer gastrique non différencié |
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 |
US8962655B2 (en) | 2007-01-29 | 2015-02-24 | Eisai R&D Management Co., Ltd. | Composition for treatment of undifferentiated gastric cancer |
AU2008325608B2 (en) | 2007-11-09 | 2013-03-14 | Eisai R & D Management Co., Ltd. | Combination of anti-angiogenic substance and anti-tumor platinum complex |
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 |
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 |
US8642834B2 (en) | 2009-02-27 | 2014-02-04 | OSI Pharmaceuticals, LLC | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
ES2573515T3 (es) | 2010-06-25 | 2016-06-08 | Eisai R&D Management Co., Ltd. | Agente antitumoral que emplea compuestos con efecto inhibitorio de cinasas combinados |
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 |
ES2705950T3 (es) | 2011-06-03 | 2019-03-27 | Eisai R&D Man Co Ltd | Biomarcadores para predecir y valorar la capacidad de respuesta de sujetos con cáncer de tiroides y de riñón a compuestos de lenvatinib |
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 |
EP2937337A4 (en) | 2012-12-21 | 2016-06-22 | Eisai R&D Man Co Ltd | AMORPHIC FORM OF CHINOLINE DERIVATIVES AND METHOD FOR THE PRODUCTION THEREOF |
AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
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 |
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 |
AR096654A1 (es) | 2013-06-20 | 2016-01-27 | Ab Science | Derivados de benzimidazol como inhibidores selectivos de proteína quinasa |
TWI721954B (zh) | 2014-08-28 | 2021-03-21 | 日商衛材R&D企管股份有限公司 | 高純度喹啉衍生物及其生產方法 |
RU2017128583A (ru) | 2015-02-25 | 2019-03-25 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Способ ослабления горечи хинолинового производного |
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AU2016279474B2 (en) | 2015-06-16 | 2021-09-09 | Eisai R&D Management Co., Ltd. | Anticancer agent |
US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | 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 AU AU2004268948A patent/AU2004268948A1/en not_active Abandoned
- 2004-08-16 CA CA002536151A patent/CA2536151A1/en not_active Abandoned
- 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 KR KR1020067003094A patent/KR20060115346A/ko not_active Application Discontinuation
- 2004-08-16 MX MXPA06002017A patent/MXPA06002017A/es unknown
- 2004-08-16 BR BRPI0413785-0A patent/BRPI0413785A/pt not_active IP Right Cessation
- 2004-08-16 AT AT04781203T patent/ATE413395T1/de not_active IP Right Cessation
- 2004-08-16 WO PCT/US2004/026481 patent/WO2005021537A1/en active Application Filing
- 2004-08-16 UA UAA200602943A patent/UA84712C2/ru unknown
- 2004-08-16 RU RU2006108791/04A patent/RU2006108791A/ru not_active Application Discontinuation
- 2004-08-16 EP EP04781203A patent/EP1664032B1/en active Active
- 2004-08-16 AP AP2006003553A patent/AP2006003553A0/xx unknown
- 2004-08-16 DE DE602004017623T patent/DE602004017623D1/de active Active
- 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
Also Published As
Publication number | Publication date |
---|---|
CN1839130A (zh) | 2006-09-27 |
EP1664032B1 (en) | 2008-11-05 |
AU2004268948A1 (en) | 2005-03-10 |
WO2005021537A1 (en) | 2005-03-10 |
JP2007502820A (ja) | 2007-02-15 |
DE602004017623D1 (de) | 2008-12-18 |
RU2006108791A (ru) | 2006-07-27 |
EP1664032A1 (en) | 2006-06-07 |
NO20060665L (no) | 2006-05-16 |
TW200524911A (en) | 2005-08-01 |
UA84712C2 (en) | 2008-11-25 |
ATE413395T1 (de) | 2008-11-15 |
IS8320A (is) | 2006-02-21 |
MXPA06002017A (es) | 2006-05-31 |
BRPI0413785A (pt) | 2006-11-07 |
KR20060115346A (ko) | 2006-11-08 |
CA2536151A1 (en) | 2005-03-10 |
JP4795237B2 (ja) | 2011-10-19 |
AP2006003553A0 (en) | 2006-04-30 |
IL173616A0 (en) | 2006-07-05 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA | Abandonment or withdrawal |