AR061867A1 - Derivados de (4,5') bipirimidil 6,4' - diamina como inhibidores de proteinquinasa - Google Patents
Derivados de (4,5') bipirimidil 6,4' - diamina como inhibidores de proteinquinasaInfo
- Publication number
- AR061867A1 AR061867A1 ARP070103061A ARP070103061A AR061867A1 AR 061867 A1 AR061867 A1 AR 061867A1 AR P070103061 A ARP070103061 A AR P070103061A AR P070103061 A ARP070103061 A AR P070103061A AR 061867 A1 AR061867 A1 AR 061867A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- unsaturated
- monocyclic
- independently selected
- hydrogen
- Prior art date
Links
Classifications
-
- 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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Composiciones farmacéuticas que comprenden estos compuestos, y métodos para utilizar tales compuestos con el fin de tratar o prevenir enfermedades o trastornos asociados con una actividad anormal o mal regulada de la cinasa, en particular enfermedades o trastornos que involucren una activacion anormal de la cinasa FGFR3. utiles para proliferacion celular, enfermedades autoinmunes e inflamatorias. Reivindicacion 1: Un compuesto de la formula 1: en donde: Y es N y Z es CH, o bien Z es N e Y es CH; R1 es alcoxilo C1-4; R2 se selecciona a partir de ciano, alcoxilo C1-4, -C(O)NR7R8, -NR7C(O)R8, -NR7S(O)2R8, -S(O)2NR7R8, -NR7R8, -C(O)OR8, -OC(O)R8, -C(O)NR7OR8, y un anillo monocíclico saturado, insaturado, o parcialmente saturado, que contiene de 5 a 7 miembros del anillo seleccionados a partir de C, O, N y S; en donde R7 se selecciona a partir de hidrogeno y alquilo C1-4; y R8 se selecciona a partir de hidrogeno, alquilo C1-4, y cicloalquilo C3-12, o es fenilo que está insustituido o sustituido por uno o más sustituyentes seleccionados a partir de alquilo C1-4, halo-alquilo C1-4, y (pirrolidino, piperidino, piperazino o 4-alquilo C1-4-piperazino)-alquilo C1-4; o R1 y R2 son independientemente H cuando Y es N y Z es CH; R3 se selecciona a partir de H, halogeno, alquilo C1-4, y alcoxilo C1-4; R4a se selecciona a partir de halogeno y alquilo C1-4; R4b se selecciona a partir de H y alquilo C1-4; R5 es H y alquilo C1-4; R6 se selecciona a partir de H, -X1R9 y - X1NR10R11; en donde cada X1 se selecciona independientemente a partir de un enlace y alquileno C1-4; R9 se selecciona a partir de arilo C6-10, un anillo monocíclico que contiene de 5 a 7 miembros del anillo seleccionados a partir de C, O, N y S, y un sistema de anillo bicíclico puenteado o fusionado que contiene de 8 a 14 miembros seleccionados a partir de C, O, N y S; en donde estos anillos monocíclicos y bicíclicos puenteados o fusionados de R9 pueden estar saturados, insaturados, o parcialmente insaturados; R10 y R11 se seleccionan independientemente a partir de H y alquilo C1-4, en donde el arilo de los anillos monocíclicos o bicíclicos de R9 puede estar opcionalmente sustituido con un grupo seleccionado a partir de alquilo C1-4, -X2R12, y -OX2NR13R14; en donde cada X2 se selecciona independientemente a partir de un enlace y alquileno C1-4; R13 y R14 se seleccionan independientemente a partir de hidrogeno y alquilo C1-4; R12 se selecciona a partir de un anillo monocíclico que contiene de 5 a 7 miembros del anillo seleccionados a partir de C, O, N y S opcionalmente sustituido con hasta 3 grupos seleccionados a partir de alquilo C1-4, -X3C(O)NR15R16, -X3OR16, -X3C(O)X3OR15, -X3C(O)R15 y -X3NR15R16; en donde el anillo monocíclico de R12 puede estar saturado, insaturado, o parcialmente insaturado; en donde cada X3 se selecciona independientemente a partir de un enlace y alquileno C1-4; cada R15 y R16 se selecciona independientemente a partir de hidrogeno y alquilo C1-4; en donde cualesquiera sustituyentes de alquilo de R9 pueden estar opcionalmente sustituidos con hasta 3 grupos hidroxilo; un derivado de N-oxido, un isomero individual, una mezcla de isomeros, y/o una sal farmacéuticamente aceptable del mismo, incluyendo un solvato, respectivamente.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US83049206P | 2006-07-12 | 2006-07-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR061867A1 true AR061867A1 (es) | 2008-09-24 |
Family
ID=38617203
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070103061A AR061867A1 (es) | 2006-07-12 | 2007-07-10 | Derivados de (4,5') bipirimidil 6,4' - diamina como inhibidores de proteinquinasa |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8026243B2 (es) |
| EP (1) | EP2044036B1 (es) |
| JP (1) | JP2009543798A (es) |
| KR (1) | KR20090029832A (es) |
| CN (1) | CN101511798B (es) |
| AR (1) | AR061867A1 (es) |
| AT (1) | ATE508119T1 (es) |
| AU (1) | AU2007272646A1 (es) |
| BR (1) | BRPI0714291A2 (es) |
| CA (1) | CA2657381A1 (es) |
| CL (1) | CL2007002017A1 (es) |
| DE (1) | DE602007014374D1 (es) |
| ES (1) | ES2367666T3 (es) |
| MX (1) | MX2009000429A (es) |
| PE (1) | PE20080548A1 (es) |
| PL (1) | PL2044036T3 (es) |
| PT (1) | PT2044036E (es) |
| RU (1) | RU2009104340A (es) |
| TW (1) | TW200811134A (es) |
| UY (1) | UY30477A1 (es) |
| WO (1) | WO2008008747A1 (es) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2114941B1 (en) | 2006-12-22 | 2015-03-25 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| CA2672213C (en) | 2006-12-22 | 2016-02-16 | Astex Therapeutics Limited | Bicyclic amine derivatives as protein tyrosine kinase inhibitors |
| US8131527B1 (en) | 2006-12-22 | 2012-03-06 | Astex Therapeutics Ltd. | FGFR pharmacophore compounds |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| EP2308866A1 (de) | 2009-10-09 | 2011-04-13 | Bayer CropScience AG | Phenylpyri(mi)dinylpyrazole und ihre Verwendung als Fungizide |
| BR112012018358A2 (pt) | 2009-12-21 | 2016-08-09 | Bayer Cropscience Ag | tienilpiri(mi)dinilazol e seu uso para controlar fungos fitopatogênicos |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| WO2012175513A1 (en) | 2011-06-20 | 2012-12-27 | Bayer Intellectual Property Gmbh | Thienylpyri(mi)dinylpyrazole |
| MX355016B (es) | 2011-10-06 | 2018-04-02 | Bayer Ip Gmbh | Heterociclilpiri(mi)dinilpirazoles como fungicidas. |
| IN2014CN02475A (es) | 2011-10-06 | 2015-06-19 | Bayer Ip Gmbh | |
| ES2860299T3 (es) | 2012-04-24 | 2021-10-04 | Vertex Pharma | Inhibidores de DNA-PK |
| SMT202000673T1 (it) | 2012-06-13 | 2021-01-05 | Incyte Holdings Corp | Composti triciclici sostituiti come inibitori di fgfr |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| EA031631B1 (ru) * | 2012-09-27 | 2019-01-31 | Чугаи Сеияку Кабушики Каиша | Способ лечения или предупреждения злокачественного новообразования, способ отбора пациента, способ тестирования предрасположенности к злокачественному новообразованию у субъекта, гибридный полипептид и его применения |
| 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 |
| BR112015021888B1 (pt) | 2013-03-12 | 2022-08-09 | Vertex Pharmaceuticals Incorporated | Inibidores de dna-pk, seus usos e composição farmacêutica |
| SG11201508328PA (en) | 2013-04-19 | 2015-11-27 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| PL3057953T3 (pl) | 2013-10-17 | 2019-01-31 | Vertex Pharmaceuticals Incorporated | Kokryształy (S)-N-metylo-8-(1-((2'-metylo-[4,5'-bipirymidyn]-6-ylo)amino)propan-2-ylo)chinolino-4-karboksyamidu i ich deuterowane pochodne jako inhibitory DNA-PK |
| CA2956270C (en) | 2014-08-18 | 2022-08-09 | 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 |
| UA121669C2 (uk) | 2015-02-20 | 2020-07-10 | Інсайт Корпорейшн | Біциклічні гетероцикли як інгібітори fgfr |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| KR20190062485A (ko) | 2016-09-27 | 2019-06-05 | 버텍스 파마슈티칼스 인코포레이티드 | Dna-손상제 및 dna-pk 저해제의 조합을 사용한 암 치료 방법 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| KR102613433B1 (ko) * | 2017-10-11 | 2023-12-13 | 주식회사 대웅제약 | 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물 |
| CA3091153A1 (en) | 2018-03-28 | 2019-10-03 | Eisai R&D Management Co., Ltd. | Therapeutic agent for hepatocellular carcinoma |
| FI3788047T3 (fi) | 2018-05-04 | 2024-11-02 | Incyte Corp | Fgft-estäjän kiinteitä muotoja ja menetelmiä niiden valmistamiseksi |
| MX2020011639A (es) | 2018-05-04 | 2021-02-15 | Incyte Corp | Sales de un inhibidor de receptores de factor de crecimiento de fibroblastos (fgfr). |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| KR102133595B1 (ko) | 2019-05-31 | 2020-07-13 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| KR102112336B1 (ko) | 2019-08-12 | 2020-05-18 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JOP20220083A1 (ar) | 2019-10-14 | 2023-01-30 | Incyte Corp | حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| PE20221504A1 (es) | 2019-12-04 | 2022-09-30 | Incyte Corp | Derivados de un inhibidor de fgfr |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| JP2024522189A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式ヘテロ環 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9924862D0 (en) | 1999-10-20 | 1999-12-22 | Celltech Therapeutics Ltd | Chemical compounds |
| BRPI0410348A (pt) | 2003-05-14 | 2006-05-30 | Torreypines Therapeutics Inc | compostos e usos dos mesmos na modulação de amilóide-beta |
| CN100412066C (zh) | 2003-09-30 | 2008-08-20 | Irm责任有限公司 | 用作蛋白激酶抑制剂的化合物和组合物 |
| AU2005245386B2 (en) | 2004-05-07 | 2008-11-27 | Amgen Inc. | Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer |
| RU2008135690A (ru) | 2006-02-06 | 2010-03-20 | Айрм Ллк (Bm) | Соединения и композиции в качестве ингибиторов протеинкиназы |
-
2007
- 2007-07-04 TW TW096124311A patent/TW200811134A/zh unknown
- 2007-07-10 CA CA002657381A patent/CA2657381A1/en not_active Abandoned
- 2007-07-10 RU RU2009104340/04A patent/RU2009104340A/ru not_active Application Discontinuation
- 2007-07-10 DE DE602007014374T patent/DE602007014374D1/de active Active
- 2007-07-10 CN CN2007800337140A patent/CN101511798B/zh not_active Expired - Fee Related
- 2007-07-10 JP JP2009519623A patent/JP2009543798A/ja active Pending
- 2007-07-10 WO PCT/US2007/073111 patent/WO2008008747A1/en active Application Filing
- 2007-07-10 PE PE2007000885A patent/PE20080548A1/es not_active Application Discontinuation
- 2007-07-10 PT PT07812739T patent/PT2044036E/pt unknown
- 2007-07-10 AT AT07812739T patent/ATE508119T1/de active
- 2007-07-10 ES ES07812739T patent/ES2367666T3/es active Active
- 2007-07-10 AR ARP070103061A patent/AR061867A1/es unknown
- 2007-07-10 BR BRPI0714291-9A2A patent/BRPI0714291A2/pt not_active Application Discontinuation
- 2007-07-10 PL PL07812739T patent/PL2044036T3/pl unknown
- 2007-07-10 KR KR1020097002815A patent/KR20090029832A/ko not_active Application Discontinuation
- 2007-07-10 US US12/373,441 patent/US8026243B2/en not_active Expired - Fee Related
- 2007-07-10 EP EP07812739A patent/EP2044036B1/en not_active Not-in-force
- 2007-07-10 AU AU2007272646A patent/AU2007272646A1/en not_active Abandoned
- 2007-07-10 MX MX2009000429A patent/MX2009000429A/es not_active Application Discontinuation
- 2007-07-11 UY UY30477A patent/UY30477A1/es not_active Application Discontinuation
- 2007-07-11 CL CL200702017A patent/CL2007002017A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PT2044036E (pt) | 2011-08-23 |
| JP2009543798A (ja) | 2009-12-10 |
| AU2007272646A1 (en) | 2008-01-17 |
| CL2007002017A1 (es) | 2008-06-13 |
| US8026243B2 (en) | 2011-09-27 |
| EP2044036B1 (en) | 2011-05-04 |
| US20100234376A1 (en) | 2010-09-16 |
| UY30477A1 (es) | 2009-04-30 |
| PE20080548A1 (es) | 2008-06-24 |
| WO2008008747A1 (en) | 2008-01-17 |
| PL2044036T3 (pl) | 2011-09-30 |
| CN101511798A (zh) | 2009-08-19 |
| TW200811134A (en) | 2008-03-01 |
| CN101511798B (zh) | 2011-11-02 |
| ATE508119T1 (de) | 2011-05-15 |
| KR20090029832A (ko) | 2009-03-23 |
| MX2009000429A (es) | 2009-01-29 |
| RU2009104340A (ru) | 2010-08-20 |
| BRPI0714291A2 (pt) | 2014-10-21 |
| CA2657381A1 (en) | 2008-01-17 |
| ES2367666T3 (es) | 2011-11-07 |
| EP2044036A1 (en) | 2009-04-08 |
| DE602007014374D1 (de) | 2011-06-16 |
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