JP2019519512A5 - - Google Patents
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- Publication number
- JP2019519512A5 JP2019519512A5 JP2018560780A JP2018560780A JP2019519512A5 JP 2019519512 A5 JP2019519512 A5 JP 2019519512A5 JP 2018560780 A JP2018560780 A JP 2018560780A JP 2018560780 A JP2018560780 A JP 2018560780A JP 2019519512 A5 JP2019519512 A5 JP 2019519512A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- tautomer
- heterocyclyl
- alkyl
- 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
- 150000001875 compounds Chemical class 0.000 claims description 65
- 150000003839 salts Chemical class 0.000 claims description 26
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 239000003623 enhancer Substances 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 24
- 125000000753 cycloalkyl group Chemical group 0.000 claims 22
- 125000000623 heterocyclic group Chemical group 0.000 claims 21
- 125000003118 aryl group Chemical group 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 5
- 238000002360 preparation method Methods 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- -1 acyl halide compound Chemical class 0.000 claims 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 229940125408 FGFR4 inhibitor Drugs 0.000 claims 1
- 102100031734 Fibroblast growth factor 19 Human genes 0.000 claims 1
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 claims 1
- 101000846394 Homo sapiens Fibroblast growth factor 19 Proteins 0.000 claims 1
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 230000003321 amplification Effects 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- 150000007942 carboxylates Chemical group 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical group 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 208000014899 intrahepatic bile duct cancer Diseases 0.000 claims 1
- 201000007450 intrahepatic cholangiocarcinoma Diseases 0.000 claims 1
- 201000005296 lung carcinoma Diseases 0.000 claims 1
- 210000005265 lung cell Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 238000003199 nucleic acid amplification method Methods 0.000 claims 1
- 230000002018 overexpression Effects 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 0 CC(C)N(CC1)CC11CN(*)CC1 Chemical compound CC(C)N(CC1)CC11CN(*)CC1 0.000 description 5
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610341444 | 2016-05-20 | ||
| CN201610341444.0 | 2016-05-20 | ||
| PCT/CN2017/085135 WO2017198221A1 (zh) | 2016-05-20 | 2017-05-19 | 嘧啶类衍生物、其制备方法和其在医药上的用途 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019519512A JP2019519512A (ja) | 2019-07-11 |
| JP2019519512A5 true JP2019519512A5 (enExample) | 2020-01-16 |
| JP6667014B2 JP6667014B2 (ja) | 2020-03-18 |
Family
ID=60324797
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018560780A Active JP6667014B2 (ja) | 2016-05-20 | 2017-05-19 | ピリミジン誘導体、その調製方法および医療での使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (4) | US10654836B2 (enExample) |
| EP (1) | EP3459952B1 (enExample) |
| JP (1) | JP6667014B2 (enExample) |
| CN (1) | CN108884097B (enExample) |
| CA (1) | CA3024532C (enExample) |
| TW (1) | TWI669300B (enExample) |
| WO (1) | WO2017198221A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201602069WA (en) | 2013-10-18 | 2016-04-28 | Eisai R&D Man Co Ltd | Pyrimidine fgfr4 inhibitors |
| CN107660200B (zh) | 2015-04-14 | 2022-01-11 | 卫材R&D管理有限公司 | 结晶fgfr4抑制剂化合物和其用途 |
| JP7372740B2 (ja) | 2016-05-10 | 2023-11-01 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 細胞生存性及び／又は細胞増殖を低減するための薬物の組み合わせ |
| CN108822048A (zh) * | 2018-07-23 | 2018-11-16 | 上海昌肽生物科技有限公司 | 4-(4-乙基-4,7二氮杂螺环[3,3]辛基)-2-硝基苯胺的合成工艺 |
| TWI723480B (zh) | 2018-07-27 | 2021-04-01 | 大陸商北京加科思新藥研發有限公司 | 用作fgfr4抑制劑的稠環衍生物 |
| CN115490670A (zh) * | 2021-06-17 | 2022-12-20 | 浙江海正药业股份有限公司 | Fgfr4选择性抑制剂的盐及其制备方法和用途 |
| CN115504965A (zh) | 2021-06-23 | 2022-12-23 | 浙江海正药业股份有限公司 | 嘧啶类衍生物的晶型及其制备方法 |
| CN116947825B (zh) * | 2022-04-14 | 2025-11-28 | 浙江海正药业股份有限公司 | Fgfr4选择性抑制剂化合物的晶型及其制备方法和用途 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| AR079257A1 (es) * | 2009-12-07 | 2012-01-04 | Novartis Ag | Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas |
| CN102250065B (zh) * | 2011-05-20 | 2015-05-13 | 浙江海正药业股份有限公司 | 取代的三嗪苯脲衍生物及其用途 |
| UA114501C2 (uk) * | 2012-02-28 | 2017-06-26 | Астеллас Фарма Інк. | Азотовмісна ароматична гетероциклічна сполука |
| KR20150037207A (ko) * | 2013-09-30 | 2015-04-08 | 한미약품 주식회사 | Fms 키나아제 저해 활성을 갖는 피리미딘 화합물 |
| SG11201602069WA (en) | 2013-10-18 | 2016-04-28 | Eisai R&D Man Co Ltd | Pyrimidine fgfr4 inhibitors |
| CN105683188B (zh) | 2013-10-25 | 2018-02-09 | 诺华股份有限公司 | 作为fgfr4抑制剂的稠环二环吡啶基衍生物 |
| CN104860891B (zh) * | 2014-02-25 | 2017-06-30 | 上海海雁医药科技有限公司 | 芳氨基嘧啶类化合物及其应用以及由其制备的药物组合物和药用组合物 |
-
2017
- 2017-05-19 TW TW106116657A patent/TWI669300B/zh active
- 2017-05-19 CN CN201780022674.3A patent/CN108884097B/zh active Active
- 2017-05-19 CA CA3024532A patent/CA3024532C/en active Active
- 2017-05-19 JP JP2018560780A patent/JP6667014B2/ja active Active
- 2017-05-19 EP EP17798784.9A patent/EP3459952B1/en active Active
- 2017-05-19 WO PCT/CN2017/085135 patent/WO2017198221A1/zh not_active Ceased
- 2017-05-19 US US16/302,310 patent/US10654836B2/en active Active
-
2020
- 2020-02-25 US US16/800,057 patent/US11001572B2/en active Active
-
2021
- 2021-03-31 US US17/218,380 patent/US11827625B2/en active Active
-
2023
- 2023-09-14 US US18/368,362 patent/US12358898B2/en active Active
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