JP2019522055A5 - - Google Patents
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- Publication number
- JP2019522055A5 JP2019522055A5 JP2019523154A JP2019523154A JP2019522055A5 JP 2019522055 A5 JP2019522055 A5 JP 2019522055A5 JP 2019523154 A JP2019523154 A JP 2019523154A JP 2019523154 A JP2019523154 A JP 2019523154A JP 2019522055 A5 JP2019522055 A5 JP 2019522055A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- cyclyl
- heterocyclyl
- pharmaceutically acceptable
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims description 32
- 150000001875 compounds Chemical class 0.000 claims description 25
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
- 125000000217 alkyl group Chemical group 0.000 claims description 22
- 229910052736 halogen Inorganic materials 0.000 claims description 22
- 150000002367 halogens Chemical group 0.000 claims description 22
- 239000001257 hydrogen Substances 0.000 claims description 21
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 18
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 5
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 description 37
- 125000000623 heterocyclic group Chemical group 0.000 description 30
- 125000003118 aryl group Chemical group 0.000 description 23
- 125000001072 heteroaryl group Chemical group 0.000 description 18
- 125000004093 cyano group Chemical group *C#N 0.000 description 16
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 14
- 125000001424 substituent group Chemical group 0.000 description 13
- 229940002612 prodrug Drugs 0.000 description 10
- 239000000651 prodrug Substances 0.000 description 10
- 125000003342 alkenyl group Chemical group 0.000 description 9
- 125000000304 alkynyl group Chemical group 0.000 description 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 7
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 7
- -1 -C(O)R 1 Chemical group 0.000 description 3
- 108091008794 FGF receptors Proteins 0.000 description 3
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 description 3
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 description 3
- 230000001404 mediated effect Effects 0.000 description 3
- 206010028980 Neoplasm Diseases 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 229910052799 carbon Inorganic materials 0.000 description 2
- 125000004438 haloalkoxy group Chemical group 0.000 description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 description 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 description 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 description 1
- 229930194542 Keto Natural products 0.000 description 1
- 150000001356 alkyl thiols Chemical group 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 125000000468 ketone group Chemical group 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610550151.3A CN107619388A (zh) | 2016-07-13 | 2016-07-13 | 作为fgfr抑制剂的杂环化合物 |
| CN201610550151.3 | 2016-07-13 | ||
| PCT/CN2017/088038 WO2018010514A1 (zh) | 2016-07-13 | 2017-06-13 | 作为fgfr抑制剂的杂环化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019522055A JP2019522055A (ja) | 2019-08-08 |
| JP2019522055A5 true JP2019522055A5 (enExample) | 2020-07-09 |
| JP6896852B2 JP6896852B2 (ja) | 2021-06-30 |
Family
ID=60951887
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019523154A Expired - Fee Related JP6896852B2 (ja) | 2016-07-13 | 2017-06-13 | Ｆｇｆｒ阻害剤として使用される複素環式化合物 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10590109B2 (enExample) |
| EP (1) | EP3489223A4 (enExample) |
| JP (1) | JP6896852B2 (enExample) |
| KR (1) | KR102386428B1 (enExample) |
| CN (2) | CN107619388A (enExample) |
| AU (1) | AU2017295628B2 (enExample) |
| CA (1) | CA3030070A1 (enExample) |
| MX (1) | MX386089B (enExample) |
| PH (1) | PH12019500036A1 (enExample) |
| RU (1) | RU2742485C2 (enExample) |
| SG (2) | SG11201900298RA (enExample) |
| WO (1) | WO2018010514A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11312701B2 (en) | 2017-08-04 | 2022-04-26 | Abbisko Therapeutics Co., Ltd | Formylpyridine derivative having FGFR4 inhibitory activity, preparation method therefor and use thereof |
| BR112020003725A2 (pt) | 2017-10-06 | 2020-11-03 | Forma Therapeutics, Inc. | inibição da peptidase 30 específica de ubiquitina |
| CN108129471A (zh) * | 2018-03-20 | 2018-06-08 | 韩邦森 | 一种噻唑取代嘧啶类化合物的合成工艺 |
| CN112513036B (zh) | 2018-05-17 | 2024-05-24 | 福马治疗有限公司 | 用作泛素特异性肽酶30抑制剂的稠合双环化合物 |
| CA3110113A1 (en) | 2018-10-05 | 2020-04-09 | Forma Therapeutics, Inc. | Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors |
| 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 |
| CN111039874B (zh) * | 2019-12-13 | 2022-11-04 | 南开大学 | 一种2-胺基-4-甲基嘧啶化合物的零废水制备方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2340605C2 (ru) * | 2002-06-27 | 2008-12-10 | Ново Нордиск А/С | Арилкарбонильные производные в качестве терапевтических средств |
| CN1508130A (zh) * | 2002-12-18 | 2004-06-30 | 中国科学院大连化学物理研究所 | N-苯基-n’-嘧啶基取代脲类衍生物的合成方法 |
| FR2850652B1 (fr) | 2003-01-31 | 2008-05-30 | Aventis Pharma Sa | Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases |
| EP1761520B1 (en) * | 2004-06-23 | 2008-07-09 | Eli Lilly And Company | Kinase inhibitors |
| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| FR2889526B1 (fr) * | 2005-08-04 | 2012-02-17 | Aventis Pharma Sa | 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation |
| EP1790342A1 (de) | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| WO2007059341A2 (en) * | 2005-11-16 | 2007-05-24 | Sgx Pharmaceuticals, Inc. | Pyrazolothiazole protein kinase modulators |
| JP5249776B2 (ja) | 2005-12-02 | 2013-07-31 | バイエル・ヘルスケア・エルエルシー | 過剰増殖性疾患および血管新生と関連する疾患を処置するために有用な置換された４−アミノ−ピロロトリアジン誘導体 |
| FR2908409B1 (fr) | 2006-11-10 | 2009-01-09 | Sanofi Aventis Sa | Pyrazoles substituees,compositions les contenant,procede de fabrication et utilisation |
| FR2947546B1 (fr) * | 2009-07-03 | 2011-07-01 | Sanofi Aventis | Derives de pyrazoles, leur preparation et leur application en therapeutique |
| WO2013024427A1 (en) * | 2011-08-16 | 2013-02-21 | Glenmark Pharmaceuticals S.A. | Novel urea derivatives as tec kinase inhibitors and uses thereof |
| AP2016009156A0 (en) * | 2013-10-25 | 2016-04-30 | Novartis Ag | Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
| RU2017134379A (ru) * | 2015-03-25 | 2019-04-03 | Новартис Аг | Формилированные n-гетероциклические производные в качестве ингибиторов fgfr4 |
| US9802917B2 (en) | 2015-03-25 | 2017-10-31 | Novartis Ag | Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide |
-
2016
- 2016-07-13 CN CN201610550151.3A patent/CN107619388A/zh active Pending
-
2017
- 2017-06-13 SG SG11201900298RA patent/SG11201900298RA/en unknown
- 2017-06-13 KR KR1020197004058A patent/KR102386428B1/ko active Active
- 2017-06-13 WO PCT/CN2017/088038 patent/WO2018010514A1/zh not_active Ceased
- 2017-06-13 CA CA3030070A patent/CA3030070A1/en active Pending
- 2017-06-13 CN CN201780002825.9A patent/CN108349896B/zh active Active
- 2017-06-13 MX MX2019000451A patent/MX386089B/es unknown
- 2017-06-13 JP JP2019523154A patent/JP6896852B2/ja not_active Expired - Fee Related
- 2017-06-13 SG SG10202013038VA patent/SG10202013038VA/en unknown
- 2017-06-13 AU AU2017295628A patent/AU2017295628B2/en not_active Ceased
- 2017-06-13 RU RU2019100164A patent/RU2742485C2/ru active
- 2017-06-13 EP EP17826852.0A patent/EP3489223A4/en not_active Withdrawn
-
2019
- 2019-01-04 PH PH12019500036A patent/PH12019500036A1/en unknown
- 2019-01-11 US US16/246,236 patent/US10590109B2/en not_active Expired - Fee Related
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