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 |
|---|---|---|---|
| CN201610550151.3 | 2016-07-13 | ||
| CN201610550151.3A CN107619388A (zh) | 2016-07-13 | 2016-07-13 | 作为fgfr抑制剂的杂环化合物 |
| 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 (https=) | 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 (https=) |
| EP (1) | EP3489223A4 (https=) |
| JP (1) | JP6896852B2 (https=) |
| KR (1) | KR102386428B1 (https=) |
| CN (2) | CN107619388A (https=) |
| AU (1) | AU2017295628B2 (https=) |
| CA (1) | CA3030070A1 (https=) |
| MX (1) | MX386089B (https=) |
| PH (1) | PH12019500036A1 (https=) |
| RU (1) | RU2742485C2 (https=) |
| SG (2) | SG10202013038VA (https=) |
| WO (1) | WO2018010514A1 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3663285B1 (en) * | 2017-08-04 | 2024-01-24 | Abbisko Therapeutics Co., Ltd. | Formylpyridine derivative having fgfr4 inhibitory activity, preparation method therefor and use thereof |
| AU2018346597B2 (en) | 2017-10-06 | 2023-07-13 | Forma Therapeutics, Inc. | Inhibiting Ubiquitin Specific Peptidase 30 |
| 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 |
| JP7449242B2 (ja) | 2018-05-17 | 2024-03-13 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的ペプチダーゼ３０（ｕｓｐ３０）阻害剤として有用な縮合二環化合物 |
| JP7530889B2 (ja) | 2018-10-05 | 2024-08-08 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的プロテアーゼ３０（ｕｓｐ３０）阻害剤として作用する縮合ピロリン |
| EA202192575A1 (ru) | 2019-03-21 | 2022-01-14 | Онксео | Соединения dbait в сочетании с ингибиторами киназ для лечения рака |
| 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 |
| 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 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (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 |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
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 |
| PT1761520E (pt) * | 2004-06-23 | 2008-09-15 | Lilly Co Eli | Inibidores de quinase |
| 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 |
| EP1966222A2 (en) * | 2005-11-16 | 2008-09-10 | SGX Pharmaceuticals, Inc. | Pyrazolothiazole protein kinase modulators |
| WO2007064931A2 (en) | 2005-12-02 | 2007-06-07 | Bayer Healthcare Llc | Substituted 4-amino-pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis |
| 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 |
| TN2016000115A1 (en) * | 2013-10-25 | 2017-07-05 | Novartis Ag | Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors. |
| 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 |
| AU2016238436A1 (en) * | 2015-03-25 | 2017-08-17 | Novartis Ag | Formylated N-heterocyclic derivatives as FGFR4 inhibitors |
-
2016
- 2016-07-13 CN CN201610550151.3A patent/CN107619388A/zh active Pending
-
2017
- 2017-06-13 CN CN201780002825.9A patent/CN108349896B/zh active Active
- 2017-06-13 RU RU2019100164A patent/RU2742485C2/ru active
- 2017-06-13 KR KR1020197004058A patent/KR102386428B1/ko not_active Expired - Fee Related
- 2017-06-13 CA CA3030070A patent/CA3030070A1/en active Pending
- 2017-06-13 SG SG10202013038VA patent/SG10202013038VA/en unknown
- 2017-06-13 MX MX2019000451A patent/MX386089B/es unknown
- 2017-06-13 AU AU2017295628A patent/AU2017295628B2/en not_active Ceased
- 2017-06-13 EP EP17826852.0A patent/EP3489223A4/en not_active Withdrawn
- 2017-06-13 WO PCT/CN2017/088038 patent/WO2018010514A1/zh not_active Ceased
- 2017-06-13 SG SG11201900298RA patent/SG11201900298RA/en unknown
- 2017-06-13 JP JP2019523154A patent/JP6896852B2/ja not_active Expired - Fee Related
-
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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