AR095781A1 - Inhibidores de proteínas de quinasa - Google Patents
Inhibidores de proteínas de quinasaInfo
- Publication number
- AR095781A1 AR095781A1 ARP140101492A ARP140101492A AR095781A1 AR 095781 A1 AR095781 A1 AR 095781A1 AR P140101492 A ARP140101492 A AR P140101492A AR P140101492 A ARP140101492 A AR P140101492A AR 095781 A1 AR095781 A1 AR 095781A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocyclic ring
- membered heterocyclic
- cycloalkyl
- alkoxy
- Prior art date
Links
- 229940121649 protein inhibitor Drugs 0.000 title 1
- 239000012268 protein inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 20
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical class C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- -1 amino, hydroxy Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Epidemiology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Derivados de benzo[d]imidazol, su uso en la elaboración de un medicamento para el tratamiento del cáncer y composiciones farmacéuticas que los comprenden. Reivindicación 1: Un compuesto de fórmula (1) donde Z¹ es N y Z² es CH o, Z¹ es CH y Z² es N, o Z¹ y Z² es N; Z es CH o N; A es un anillo fenilo o un anillo heterocíclico de 5 - 12 miembros; R¹ es H, alquilo C₁₋₇, cicloalquilo C₃₋₇, cicloalquilo C₃₋₇-alquilo C₁₋₇, alcoxi C₁₋₇, alquilo C₁₋₇carbonilo, amino, hidroxi, hidroxi-alquilo C₁₋₇, halo-alquilo C₁₋₇, alquil C₁₋₇amino-alquilo C₁₋₇, -R¹⁶-C(O)-R¹⁷ o -E-R⁶; R² es H, halógeno o alquilo C₁₋₇; B es un anillo carbocíclico o heterocíclico de 5 - 12 miembros; R³ es H, halógeno, alquilo C₁₋₇, alcoxi C₁₋₇, halo-alquilo C₁₋₇ o halo-alcoxi C₁₋₇; R⁴ es H, halógeno, alquilo C₁₋₇ u oxo; R⁵ es H, -C(O)R⁷, -SO₂R⁸ o un anillo heterocíclico de 5 - 6 miembros opcionalmente sustituido; R⁶ es un anillo heterocíclico de 5 - 6 miembros opcionalmente sustituido; R⁷ es alquilo C₁₋₇, alquenilo C₂₋₇, alcoxi C₁₋₇, alcoxi C₁₋₇-alquilo C₁₋₇, carboxi-alquilo C₁₋₇, alcoxi C₁₋₇carbonilo-alquilo C₁₋₇, alquil C₁₋₇amino-alquilo C₁₋₇, -NH-R¹⁰ o -NH-X¹-R¹¹; R⁸ es alquilo C₁₋₇, alquenilo C₂₋₇, cicloalquilo C₃₋₇, hidroxi-alquilo C₁₋₇, -NR¹³R¹⁴, -NH-X²-R¹⁵, fenilo o un anillo heterocíclico de 5 - 6 miembros opcionalmente sustituido; R¹⁰ es alquilo C₁₋₇ o cicloalquilo C₃₋₇; R¹¹ es fenilo o un anillo heterocíclico de 5 - 6 miembros opcionalmente sustituido; R¹² es H o alquilo C₁₋₇; R¹³ y R¹⁴ son, en forma independiente, H, alquilo C₁₋₇ o cicloalquilo C₃₋₇; R¹⁵ es fenilo o un anillo heterocíclico de 5 - 6 miembros opcionalmente sustituido; R¹⁶ es una unión o un alquilo C₁₋₇; R¹⁷ es alquilo C₁₋₇, alcoxi C₁₋₇, alquil C₁₋₇amino, amino o hidroxi; E es una unión o un alquilo C₁₋₇; X¹ y X² son, en forma independiente, una unión alquilo C₁₋₇; y sales farmacéuticamente aceptables del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN382KO2013 | 2013-04-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR095781A1 true AR095781A1 (es) | 2015-11-11 |
Family
ID=50685938
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140101492A AR095781A1 (es) | 2013-04-04 | 2014-04-04 | Inhibidores de proteínas de quinasa |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US20160031855A1 (es) |
| EP (1) | EP2981533B1 (es) |
| JP (1) | JP6356782B2 (es) |
| KR (1) | KR20150138383A (es) |
| CN (1) | CN105073733B (es) |
| AR (1) | AR095781A1 (es) |
| AU (1) | AU2014246961B2 (es) |
| BR (1) | BR112015025413A2 (es) |
| CA (1) | CA2907855A1 (es) |
| CL (1) | CL2015002932A1 (es) |
| CY (1) | CY1120306T1 (es) |
| DK (1) | DK2981533T3 (es) |
| EA (1) | EA031076B1 (es) |
| ES (1) | ES2658183T3 (es) |
| HR (1) | HRP20180382T1 (es) |
| HU (1) | HUE036692T2 (es) |
| LT (1) | LT2981533T (es) |
| MA (1) | MA38454B1 (es) |
| MX (1) | MX2015013776A (es) |
| MY (1) | MY184528A (es) |
| NO (1) | NO2981533T3 (es) |
| NZ (1) | NZ713410A (es) |
| PE (1) | PE20160115A1 (es) |
| PH (1) | PH12015502284A1 (es) |
| PL (1) | PL2981533T3 (es) |
| PT (1) | PT2981533T (es) |
| RS (1) | RS56942B1 (es) |
| SA (1) | SA515361260B1 (es) |
| SG (1) | SG11201508125XA (es) |
| SI (1) | SI2981533T1 (es) |
| TW (1) | TWI628176B (es) |
| UA (1) | UA115176C2 (es) |
| WO (1) | WO2014162039A1 (es) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| ES2984771T3 (es) | 2012-06-13 | 2024-10-31 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| US9951047B2 (en) | 2014-08-18 | 2018-04-24 | Eisai R&D Management Co., Ltd. | Salt of monocyclic pyridine derivative and crystal thereof |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| EA038045B1 (ru) | 2015-02-20 | 2021-06-28 | Инсайт Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| EP3275442B1 (en) | 2015-03-25 | 2021-07-28 | National Cancer Center | Therapeutic agent for bile duct cancer |
| WO2017104739A1 (ja) | 2015-12-17 | 2017-06-22 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 乳がん治療剤 |
| US10487863B2 (en) * | 2017-02-17 | 2019-11-26 | Ford Global Technologies, Llc | Castellated joint for improved adhesive coverage when using mechanical fixings and adhesive in one joint |
| CN109963854B (zh) | 2017-03-16 | 2022-04-12 | 江苏恒瑞医药股份有限公司 | 杂芳基并[4,3-c]嘧啶-5-胺类衍生物、其制备方法及其在医药上的应用 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| BR112020017922A2 (pt) | 2018-03-28 | 2020-12-22 | Eisai R&D Management Co., Ltd. | Agente terapêutico para carcinoma hepatocelular |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| US11174257B2 (en) | 2018-05-04 | 2021-11-16 | Incyte Corporation | Salts of an FGFR inhibitor |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
| CA3141424C (en) | 2019-06-14 | 2023-11-07 | Zhengxia CHEN | Fused ring compound as fgfr and vegfr dual inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021018047A1 (zh) | 2019-07-26 | 2021-02-04 | 南京明德新药研发有限公司 | 作为fgfr和vegfr双重抑制剂的吡啶衍生物 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| PH12022550892A1 (en) | 2019-10-14 | 2023-05-03 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| 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 |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| AU2022213682C1 (en) * | 2021-01-26 | 2025-04-17 | Cgenetech (Suzhou, China) Co., Ltd | Crystal form of methylpyrazole-substituted pyridoimidazole compound and preparation method therefor |
| KR102655210B1 (ko) * | 2021-03-26 | 2024-04-08 | 주식회사 스탠다임 | 아데노신 a2a 수용체 길항제 및 이의 용도 |
| JP2024513575A (ja) | 2021-04-12 | 2024-03-26 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法 |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2376957A1 (en) * | 1999-06-30 | 2001-01-04 | Merck & Co., Inc. | Src kinase inhibitor compounds |
| CA2376951A1 (en) * | 1999-06-30 | 2001-01-04 | Peter J. Sinclair | Src kinase inhibitor compounds |
| AU2004268949A1 (en) * | 2003-08-21 | 2005-03-10 | Osi Pharmaceuticals, Inc. | N-substituted benzimidazolyl C-kit inhibitors |
| KR20090064602A (ko) * | 2006-10-16 | 2009-06-19 | 노파르티스 아게 | 단백질 키나제 억제제로서 유용한 페닐아세트아미드 |
| US8513276B2 (en) * | 2006-12-22 | 2013-08-20 | Astex Therapeutics Limited | Imidazo[1,2-a]pyridine compounds for use in treating cancer |
| HRP20150642T1 (hr) * | 2006-12-22 | 2015-08-14 | Astex Therapeutics Limited | BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a |
| GB0906472D0 (en) * | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| CN102216300B (zh) * | 2009-09-30 | 2014-10-22 | 贝达药业股份有限公司 | 作为蛋白激酶抑制剂的化合物和组合物 |
| UA111382C2 (uk) * | 2011-10-10 | 2016-04-25 | Оріон Корпорейшн | Інгібітори протеїнкінази |
-
2014
- 2014-04-02 TW TW103112259A patent/TWI628176B/zh not_active IP Right Cessation
- 2014-04-03 EP EP14722686.4A patent/EP2981533B1/en active Active
- 2014-04-03 RS RS20180257A patent/RS56942B1/sr unknown
- 2014-04-03 MX MX2015013776A patent/MX2015013776A/es unknown
- 2014-04-03 SI SI201430589T patent/SI2981533T1/en unknown
- 2014-04-03 CN CN201480019409.6A patent/CN105073733B/zh not_active Expired - Fee Related
- 2014-04-03 NO NO14722686A patent/NO2981533T3/no unknown
- 2014-04-03 UA UAA201510726A patent/UA115176C2/uk unknown
- 2014-04-03 DK DK14722686.4T patent/DK2981533T3/en active
- 2014-04-03 PL PL14722686T patent/PL2981533T3/pl unknown
- 2014-04-03 PE PE2015002104A patent/PE20160115A1/es not_active Application Discontinuation
- 2014-04-03 BR BR112015025413A patent/BR112015025413A2/pt not_active Application Discontinuation
- 2014-04-03 AU AU2014246961A patent/AU2014246961B2/en not_active Ceased
- 2014-04-03 WO PCT/FI2014/000003 patent/WO2014162039A1/en not_active Ceased
- 2014-04-03 HU HUE14722686A patent/HUE036692T2/hu unknown
- 2014-04-03 MY MYPI2015703505A patent/MY184528A/en unknown
- 2014-04-03 CA CA2907855A patent/CA2907855A1/en not_active Abandoned
- 2014-04-03 PT PT147226864T patent/PT2981533T/pt unknown
- 2014-04-03 SG SG11201508125XA patent/SG11201508125XA/en unknown
- 2014-04-03 EA EA201591913A patent/EA031076B1/ru not_active IP Right Cessation
- 2014-04-03 JP JP2016505869A patent/JP6356782B2/ja not_active Expired - Fee Related
- 2014-04-03 NZ NZ713410A patent/NZ713410A/en not_active IP Right Cessation
- 2014-04-03 KR KR1020157031629A patent/KR20150138383A/ko not_active Withdrawn
- 2014-04-03 MA MA38454A patent/MA38454B1/fr unknown
- 2014-04-03 ES ES14722686.4T patent/ES2658183T3/es active Active
- 2014-04-03 LT LTEP14722686.4T patent/LT2981533T/lt unknown
- 2014-04-03 HR HRP20180382TT patent/HRP20180382T1/hr unknown
- 2014-04-03 US US14/782,020 patent/US20160031855A1/en not_active Abandoned
- 2014-04-04 AR ARP140101492A patent/AR095781A1/es unknown
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2015
- 2015-10-01 PH PH12015502284A patent/PH12015502284A1/en unknown
- 2015-10-02 CL CL2015002932A patent/CL2015002932A1/es unknown
- 2015-10-04 SA SA515361260A patent/SA515361260B1/ar unknown
-
2018
- 2018-02-21 CY CY20181100204T patent/CY1120306T1/el unknown
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