JP2011500544A5 - - Google Patents
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- JP2011500544A5 JP2011500544A5 JP2010528478A JP2010528478A JP2011500544A5 JP 2011500544 A5 JP2011500544 A5 JP 2011500544A5 JP 2010528478 A JP2010528478 A JP 2010528478A JP 2010528478 A JP2010528478 A JP 2010528478A JP 2011500544 A5 JP2011500544 A5 JP 2011500544A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- nitrogen
- heterocyclic
- cycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 62
- 150000001875 compounds Chemical class 0.000 claims description 62
- 125000000217 alkyl group Chemical group 0.000 claims description 50
- 229910052757 nitrogen Inorganic materials 0.000 claims description 40
- 125000000623 heterocyclic group Chemical group 0.000 claims description 32
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 20
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 20
- 125000003545 alkoxy group Chemical group 0.000 claims description 20
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 239000001257 hydrogen Substances 0.000 claims description 20
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 18
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 16
- 150000002431 hydrogen Chemical class 0.000 claims description 16
- 229910052736 halogen Inorganic materials 0.000 claims description 15
- 150000002367 halogens Chemical class 0.000 claims description 15
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 125000004122 cyclic group Chemical group 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
- 125000002837 carbocyclic group Chemical group 0.000 claims description 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 230000002265 prevention Effects 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 239000012453 solvate Substances 0.000 claims description 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 3
- -1 C 1-6 alkanol Chemical group 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 2
- 125000006553 (C3-C8) cycloalkenyl group Chemical group 0.000 claims description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 description 6
- 201000010099 disease Diseases 0.000 description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
- 125000005843 halogen group Chemical group 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 238000004519 manufacturing process Methods 0.000 description 4
- 238000011282 treatment Methods 0.000 description 4
- 108091008794 FGF receptors Proteins 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 230000001404 mediated effect Effects 0.000 description 3
- 150000001408 amides Chemical class 0.000 description 2
- PFKFTWBEEFSNDU-UHFFFAOYSA-N carbonyldiimidazole Chemical compound C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 description 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 description 2
- 150000001204 N-oxides Chemical class 0.000 description 1
- 150000001299 aldehydes Chemical class 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 150000001733 carboxylic acid esters Chemical class 0.000 description 1
- 150000004820 halides Chemical class 0.000 description 1
- 239000012948 isocyanate Substances 0.000 description 1
- 150000002513 isocyanates Chemical class 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97955507P | 2007-10-12 | 2007-10-12 | |
| GBGB0720041.3A GB0720041D0 (en) | 2007-10-12 | 2007-10-12 | New Compounds |
| US60/979,555 | 2007-10-12 | ||
| GB0720041.3 | 2007-10-12 | ||
| US6117808P | 2008-06-13 | 2008-06-13 | |
| US61/061,178 | 2008-06-13 | ||
| PCT/GB2008/003418 WO2009047506A1 (en) | 2007-10-12 | 2008-10-10 | Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011500544A JP2011500544A (ja) | 2011-01-06 |
| JP2011500544A5 true JP2011500544A5 (enExample) | 2011-10-20 |
| JP5497648B2 JP5497648B2 (ja) | 2014-05-21 |
Family
ID=38788133
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010528478A Expired - Fee Related JP5497648B2 (ja) | 2007-10-12 | 2008-10-10 | タンパク質チロシンキナーゼインヒビターとしての二環式ヘテロ環式化合物 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US8076354B2 (enExample) |
| EP (1) | EP2197880B1 (enExample) |
| JP (1) | JP5497648B2 (enExample) |
| AU (1) | AU2008309418B2 (enExample) |
| CA (1) | CA2701865C (enExample) |
| CY (1) | CY1117139T1 (enExample) |
| DK (1) | DK2197880T3 (enExample) |
| ES (1) | ES2559685T3 (enExample) |
| GB (1) | GB0720041D0 (enExample) |
| HR (1) | HRP20160002T1 (enExample) |
| HU (1) | HUE026275T2 (enExample) |
| ME (1) | ME02373B (enExample) |
| PL (1) | PL2197880T3 (enExample) |
| PT (1) | PT2197880E (enExample) |
| RS (1) | RS54518B1 (enExample) |
| SI (1) | SI2197880T1 (enExample) |
| WO (1) | WO2009047506A1 (enExample) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2009006706A (es) | 2006-12-22 | 2009-07-02 | Astex Therapeutics Ltd | Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos. |
| MX2009006704A (es) * | 2006-12-22 | 2009-06-30 | Astex Therapeutics Ltd | Derivados de amina triciclicos como inhibidores de proteina de tirosina cinasa. |
| 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 |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| 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 |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| US9611267B2 (en) | 2012-06-13 | 2017-04-04 | Incyte Holdings Corporation | Substituted tricyclic compounds as FGFR inhibitors |
| 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 |
| FR3000746A1 (fr) | 2013-01-04 | 2014-07-11 | Centre Nat Rech Scient | Peptide pour son utilisation dans le traitement des neuronopathies motrices |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| TWI649318B (zh) | 2013-04-19 | 2019-02-01 | 英塞特控股公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| BR112017002268B1 (pt) | 2014-08-18 | 2022-11-08 | Eisai R&D Management Co., Ltd | Sal de derivado de piridina monocíclica e cristal do mesmo |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| 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 |
| RU2712222C2 (ru) | 2015-03-25 | 2020-01-27 | Нэшнл Кэнсер Сентер | Терапевтическое средство против рака желчных протоков |
| WO2017049498A1 (zh) * | 2015-09-23 | 2017-03-30 | 前湾医药科技（深圳）有限公司 | 一种咪唑并吡啶类化合物与在制备pi3k抑制剂中的应用 |
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| US11780848B2 (en) | 2015-10-16 | 2023-10-10 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof |
| KR20250010141A (ko) | 2015-10-16 | 2025-01-20 | 애브비 인코포레이티드 | (3S,4R)-3-에틸-4-(3H-이미다조[1,2-a]피롤로[2,3-e]-피라진-8-일)-N-(2,2,2-트리플루오로에틸)피롤리딘-1-카복스아미드및 이의 고체상 형태의 제조 방법 |
| US12365689B2 (en) | 2015-10-16 | 2025-07-22 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11365198B2 (en) | 2015-10-16 | 2022-06-21 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| 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 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CN111225915B (zh) * | 2017-10-18 | 2023-03-07 | 朱比兰特埃皮帕德有限公司 | 作为pad抑制剂的咪唑并吡啶化合物 |
| JOP20200073A1 (ar) | 2017-10-24 | 2020-04-29 | Bayer Pharma AG | مركبات أميد إيميدازوبيريدين تحمل بدائل واستخداماتها |
| BR112020017922A2 (pt) | 2018-03-28 | 2020-12-22 | Eisai R&D Management Co., Ltd. | Agente terapêutico para carcinoma hepatocelular |
| TW201946630A (zh) | 2018-05-04 | 2019-12-16 | 美商英塞特公司 | Fgfr抑制劑之鹽 |
| ES2991427T3 (es) | 2018-05-04 | 2024-12-03 | Incyte Corp | Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| WO2020216669A1 (de) | 2019-04-23 | 2020-10-29 | Bayer Aktiengesellschaft | Phenylsubstituierte imidazopyridinamide und ihre verwendung |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CN114072402B (zh) * | 2019-07-26 | 2023-12-26 | 盛世泰科生物医药技术(苏州)股份有限公司 | 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 |
| GEAP202415945A (en) | 2019-10-14 | 2024-04-25 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4286382A4 (en) * | 2021-01-26 | 2025-01-08 | CGeneTech (Suzhou, China) Co., Ltd. | CRYSTAL FORM OF A METHYLPYRAZOLE-SUBSTITUTED PYRIDOIMIDAZOLE COMPOUND AND METHOD FOR PREPARING THE SAME |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| AR126101A1 (es) | 2021-06-09 | 2023-09-13 | Incyte Corp | Heterociclos tricíclicos como inhibidores de fgfr |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2025140656A1 (en) * | 2023-12-30 | 2025-07-03 | Fujian Haixi Pharmaceuticals Co., Ltd. | Heteroaryl compounds as multi-target protein kinase inhibitors |
| WO2025140655A1 (en) * | 2023-12-30 | 2025-07-03 | Fujian Haixi Pharmaceuticals Co., Ltd. | Heteroaryl compounds as multi-target protein kinase inhibitors |
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-
2007
- 2007-10-12 GB GBGB0720041.3A patent/GB0720041D0/en not_active Ceased
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2008
- 2008-10-10 US US12/682,508 patent/US8076354B2/en active Active
- 2008-10-10 SI SI200831563T patent/SI2197880T1/sl unknown
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- 2008-10-10 PL PL08806556T patent/PL2197880T3/pl unknown
- 2008-10-10 WO PCT/GB2008/003418 patent/WO2009047506A1/en not_active Ceased
- 2008-10-10 AU AU2008309418A patent/AU2008309418B2/en not_active Ceased
- 2008-10-10 PT PT88065560T patent/PT2197880E/pt unknown
- 2008-10-10 ME MEP-2016-3A patent/ME02373B/me unknown
- 2008-10-10 DK DK08806556.0T patent/DK2197880T3/en active
- 2008-10-10 ES ES08806556.0T patent/ES2559685T3/es active Active
- 2008-10-10 JP JP2010528478A patent/JP5497648B2/ja not_active Expired - Fee Related
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