ECSP099436A - Acilaminopirazoles como inhibidores de fgfr - Google Patents
Acilaminopirazoles como inhibidores de fgfrInfo
- Publication number
- ECSP099436A ECSP099436A EC2009009436A ECSP099436A ECSP099436A EC SP099436 A ECSP099436 A EC SP099436A EC 2009009436 A EC2009009436 A EC 2009009436A EC SP099436 A ECSP099436 A EC SP099436A EC SP099436 A ECSP099436 A EC SP099436A
- Authority
- EC
- Ecuador
- Prior art keywords
- acilaminopirazoles
- fgfr inhibitors
- compound
- formula
- fgfr
- Prior art date
Links
- 108091008794 FGF receptors Proteins 0.000 title 1
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
- C07D231/40—Acylated on said nitrogen atom
-
- 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
- A61K31/415—1,2-Diazoles
-
- 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
-
- 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
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87119006P | 2006-12-21 | 2006-12-21 | |
| US98554207P | 2007-11-05 | 2007-11-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP099436A true ECSP099436A (es) | 2009-07-31 |
Family
ID=39536793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2009009436A ECSP099436A (es) | 2006-12-21 | 2009-06-16 | Acilaminopirazoles como inhibidores de fgfr |
Country Status (28)
| Country | Link |
|---|---|
| US (6) | US7737149B2 (en:Method) |
| EP (1) | EP2125748B1 (en:Method) |
| JP (1) | JP5000726B2 (en:Method) |
| KR (1) | KR101467593B1 (en:Method) |
| AR (1) | AR064454A1 (en:Method) |
| AT (1) | ATE510825T1 (en:Method) |
| AU (1) | AU2007336011B2 (en:Method) |
| BR (1) | BRPI0720551A2 (en:Method) |
| CA (1) | CA2672521C (en:Method) |
| CO (1) | CO6210721A2 (en:Method) |
| CY (1) | CY1111721T1 (en:Method) |
| DK (1) | DK2125748T3 (en:Method) |
| EC (1) | ECSP099436A (en:Method) |
| HR (1) | HRP20110520T1 (en:Method) |
| IL (1) | IL199019A (en:Method) |
| MX (1) | MX2009006742A (en:Method) |
| MY (1) | MY146111A (en:Method) |
| NO (1) | NO342176B1 (en:Method) |
| NZ (1) | NZ577209A (en:Method) |
| PE (1) | PE20081532A1 (en:Method) |
| PL (1) | PL2125748T3 (en:Method) |
| PT (1) | PT2125748E (en:Method) |
| RU (1) | RU2458920C2 (en:Method) |
| SA (1) | SA07280734B1 (en:Method) |
| SI (1) | SI2125748T1 (en:Method) |
| TW (1) | TWI434846B (en:Method) |
| UY (1) | UY30819A1 (en:Method) |
| WO (1) | WO2008075068A2 (en:Method) |
Families Citing this family (83)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US8131527B1 (en) | 2006-12-22 | 2012-03-06 | Astex Therapeutics Ltd. | FGFR pharmacophore compounds |
| CA2672213C (en) | 2006-12-22 | 2016-02-16 | Astex Therapeutics Limited | Bicyclic amine derivatives as protein tyrosine kinase inhibitors |
| MX2009006706A (es) | 2006-12-22 | 2009-07-02 | Astex Therapeutics Ltd | Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos. |
| DE102007026341A1 (de) | 2007-06-06 | 2008-12-11 | Merck Patent Gmbh | Benzoxazolonderivate |
| DE102007032507A1 (de) | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
| SA08290520B1 (ar) | 2007-08-22 | 2012-02-22 | استرازينيكا ايه بي | مشتقات سيكلو بروبيل أميد وتركيبات صيدلية تحتوي عليها لعلاج حالة مرضية سببها مستقبلات هيستامين h3 |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| DE102007061963A1 (de) | 2007-12-21 | 2009-06-25 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102008019907A1 (de) | 2008-04-21 | 2009-10-22 | Merck Patent Gmbh | Pyridazinonderivate |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| DE102008028905A1 (de) | 2008-06-18 | 2009-12-24 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate |
| BRPI0914233A2 (pt) * | 2008-06-19 | 2015-11-03 | Astrazeneca Ab | composto, uso de um composto, métodos para produzir um efeito inibidor de fgfr e para produzir um efeito anticâncer em um animal de sangue quente, composição farmacêutica, e, método para tratar uma doença |
| DK2361250T3 (da) | 2008-12-22 | 2013-11-04 | Merck Patent Gmbh | Nye polymorfe former af 6-(1-methyl-1h-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2h-pyridazin-3-on-dihydrogenphosphat og fremgangsmåder til fremstilling deraf |
| TW201039825A (en) | 2009-02-20 | 2010-11-16 | Astrazeneca Ab | Cyclopropyl amide derivatives 983 |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| JO2860B1 (en) * | 2009-05-07 | 2015-03-15 | ايلي ليلي اند كومباني | Phenylendazolyl compounds |
| WO2011102795A1 (en) | 2010-02-18 | 2011-08-25 | Astrazeneca Ab | New crystalline form of a cyclopropyl benzamide derivative |
| CN103096893B (zh) | 2010-06-04 | 2016-05-04 | 阿尔巴尼分子研究公司 | 甘氨酸转运体-1抑制剂、其制备方法及其用途 |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| US9255072B2 (en) | 2011-03-04 | 2016-02-09 | National Health Rsearch Institutes | Pyrazole compounds and thiazole compounds as protein kinases inhibitors |
| BR112014018868B1 (pt) | 2012-02-28 | 2021-02-09 | Astellas Pharma Inc. | composto heterocíclico aromático contendo nitrogênio, composição farmacêutica compreendendo dito composto e uso do mesmo |
| PT2824181T (pt) | 2012-03-08 | 2018-12-20 | Astellas Pharma Inc | Novo produto de fusão de fgfr3 |
| JPWO2013161871A1 (ja) * | 2012-04-25 | 2015-12-24 | 興和株式会社 | Ｔｌｒ阻害作用を有するチオフェン誘導体 |
| CN107652289B (zh) | 2012-06-13 | 2020-07-21 | 因塞特控股公司 | 作为fgfr抑制剂的取代的三环化合物 |
| WO2014002922A1 (ja) * | 2012-06-26 | 2014-01-03 | アステラス製薬株式会社 | 抗癌剤の併用による癌治療方法 |
| US20150203589A1 (en) | 2012-07-24 | 2015-07-23 | The Trustees Of Columbia University In The City Of New York | Fusion proteins and methods thereof |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| 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 |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| WO2014138364A2 (en) | 2013-03-06 | 2014-09-12 | Genentech, Inc. | Methods of treating and preventing cancer drug resistance |
| PL403149A1 (pl) * | 2013-03-14 | 2014-09-15 | Celon Pharma Spółka Akcyjna | Nowe związki pochodne pirazolilobenzo[d]imidazolu |
| CA2907152A1 (en) | 2013-03-15 | 2014-09-25 | The Trustees Of Columbia University In The City Of New York | Fusion proteins and methods thereof |
| KR102350704B1 (ko) | 2013-03-15 | 2022-01-13 | 셀젠 카르 엘엘씨 | 헤테로아릴 화합물 및 이의 용도 |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| CN111793068A (zh) | 2013-03-15 | 2020-10-20 | 西建卡尔有限责任公司 | 杂芳基化合物和其用途 |
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| AR096393A1 (es) * | 2013-05-23 | 2015-12-30 | Bayer Cropscience Ag | Compuestos heterocíclicos pesticidas |
| WO2015053407A1 (ja) | 2013-10-08 | 2015-04-16 | 第一三共株式会社 | 抗ｆｇｆｒ２抗体と他剤の組合せ |
| US20230190750A1 (en) | 2014-06-13 | 2023-06-22 | Genentech, Inc. | Methods of treating and preventing cancer drug resistance |
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| JP6445684B2 (ja) * | 2014-08-19 | 2018-12-26 | シャンハイ ハイヘ ファーマシューティカル カンパニー リミテッドＳｈａｎｇｈａｉ Ｈａｉｈｅ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｃｏ．， Ｌｔｄ． | Ｆｇｆｒキナーゼ阻害剤としてのインダゾール系化合物およびその製造と使用 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2016105517A1 (en) | 2014-12-23 | 2016-06-30 | The Trustees Of Columbia University In The City Of New York | Fusion proteins and methods thereof |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| PE20171514A1 (es) | 2015-02-20 | 2017-10-20 | Incyte Corp | Heterociclos biciclicos como inhibidores de fgfr |
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