JP2016535000A5 - - Google Patents
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- JP2016535000A5 JP2016535000A5 JP2016523266A JP2016523266A JP2016535000A5 JP 2016535000 A5 JP2016535000 A5 JP 2016535000A5 JP 2016523266 A JP2016523266 A JP 2016523266A JP 2016523266 A JP2016523266 A JP 2016523266A JP 2016535000 A5 JP2016535000 A5 JP 2016535000A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- pharmaceutically acceptable
- acceptable salt
- pharmaceutical composition
- 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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- 238000000034 method Methods 0.000 claims description 5
- -1 methoxyethyl Chemical group 0.000 claims 29
- 125000000217 alkyl group Chemical group 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 22
- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 16
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 102100031734 Fibroblast growth factor 19 Human genes 0.000 claims 8
- 101000846394 Homo sapiens Fibroblast growth factor 19 Proteins 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 239000012472 biological sample Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 claims 1
- 125000006479 2-pyridyl methyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims 1
- DGYIJVNZSDYBOE-UHFFFAOYSA-N [CH2]C1=CC=NC=C1 Chemical group [CH2]C1=CC=NC=C1 DGYIJVNZSDYBOE-UHFFFAOYSA-N 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- MBWRLLRCTIYXDW-UHFFFAOYSA-N N-[2-[[6-[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl-methylamino]pyrimidin-4-yl]amino]-5-(4-ethylpiperazin-1-yl)phenyl]prop-2-enamide Chemical compound ClC1=C(C(=C(C=C1OC)OC)Cl)NC(N(C)C1=CC(=NC=N1)NC1=C(C=C(C=C1)N1CCN(CC1)CC)NC(C=C)=O)=O MBWRLLRCTIYXDW-UHFFFAOYSA-N 0.000 description 1
- XGVXKJKTISMIOW-ZDUSSCGKSA-N simurosertib Chemical compound N1N=CC(C=2SC=3C(=O)NC(=NC=3C=2)[C@H]2N3CCC(CC3)C2)=C1C XGVXKJKTISMIOW-ZDUSSCGKSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361892881P | 2013-10-18 | 2013-10-18 | |
| US61/892,881 | 2013-10-18 | ||
| PCT/US2014/060857 WO2015057938A1 (en) | 2013-10-18 | 2014-10-16 | Pyrimidine fgfr4 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017088732A Division JP2017160233A (ja) | 2013-10-18 | 2017-04-27 | ピリミジンｆｇｆｒ４阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016535000A JP2016535000A (ja) | 2016-11-10 |
| JP2016535000A5 true JP2016535000A5 (OSRAM) | 2017-04-27 |
| JP6139788B2 JP6139788B2 (ja) | 2017-05-31 |
Family
ID=51842899
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016523266A Active JP6139788B2 (ja) | 2013-10-18 | 2014-10-16 | ピリミジンｆｇｆｒ４阻害剤 |
| JP2017088732A Pending JP2017160233A (ja) | 2013-10-18 | 2017-04-27 | ピリミジンｆｇｆｒ４阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017088732A Pending JP2017160233A (ja) | 2013-10-18 | 2017-04-27 | ピリミジンｆｇｆｒ４阻害剤 |
Country Status (33)
| Country | Link |
|---|---|
| US (4) | US9434697B2 (OSRAM) |
| EP (2) | EP3057943B1 (OSRAM) |
| JP (2) | JP6139788B2 (OSRAM) |
| KR (1) | KR101826015B1 (OSRAM) |
| CN (2) | CN105899490B (OSRAM) |
| AR (1) | AR098048A1 (OSRAM) |
| AU (2) | AU2014337291B9 (OSRAM) |
| BR (1) | BR112016008110B1 (OSRAM) |
| CA (1) | CA2924206C (OSRAM) |
| CL (1) | CL2016000918A1 (OSRAM) |
| CY (1) | CY1121129T1 (OSRAM) |
| DK (1) | DK3057943T3 (OSRAM) |
| ES (1) | ES2679521T3 (OSRAM) |
| HR (1) | HRP20181129T1 (OSRAM) |
| HU (1) | HUE039268T2 (OSRAM) |
| IL (1) | IL244373B (OSRAM) |
| JO (1) | JO3515B1 (OSRAM) |
| LT (1) | LT3057943T (OSRAM) |
| MX (1) | MX378288B (OSRAM) |
| MY (1) | MY184733A (OSRAM) |
| NZ (1) | NZ717559A (OSRAM) |
| PE (1) | PE20160679A1 (OSRAM) |
| PH (1) | PH12016500676B1 (OSRAM) |
| PL (1) | PL3057943T3 (OSRAM) |
| PT (1) | PT3057943T (OSRAM) |
| RS (1) | RS57444B1 (OSRAM) |
| RU (1) | RU2715708C2 (OSRAM) |
| SG (1) | SG11201602069WA (OSRAM) |
| SI (1) | SI3057943T1 (OSRAM) |
| SM (1) | SMT201800379T1 (OSRAM) |
| TW (1) | TWI597268B (OSRAM) |
| UA (1) | UA116920C2 (OSRAM) |
| WO (2) | WO2015057963A1 (OSRAM) |
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| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| UA125503C2 (uk) | 2012-06-13 | 2022-04-13 | Інсайт Холдинґс Корпорейшн | Заміщені трициклічні сполуки як інгібітори fgfr |
| RU2679130C2 (ru) | 2012-07-11 | 2019-02-06 | Блюпринт Медсинс Корпорейшн | Ингибиторы рецептора фактора роста фибробластов |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| SG11201507478VA (en) | 2013-03-15 | 2015-10-29 | Celgene Avilomics Res Inc | Heteroaryl compounds and uses thereof |
| MY181020A (en) | 2013-03-15 | 2020-12-16 | Sanofi Sa | Heteroaryl compounds and uses thereof |
| AR095464A1 (es) | 2013-03-15 | 2015-10-21 | Celgene Avilomics Res Inc | Compuestos de heteroarilo y usos de los mismos |
| MY181497A (en) | 2013-04-19 | 2020-12-23 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2015057963A1 (en) * | 2013-10-18 | 2015-04-23 | Eisai R&D Management Co., Ltd. | Fgfr4 inhibitors |
| AU2014338549B2 (en) | 2013-10-25 | 2017-05-25 | Novartis Ag | Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors |
| EP3060560A1 (en) | 2013-10-25 | 2016-08-31 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| ES2756748T3 (es) | 2014-10-03 | 2020-04-27 | Novartis Ag | Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CR20170390A (es) | 2015-02-20 | 2017-10-23 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de fgfr |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles 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 |
| WO2016164703A1 (en) * | 2015-04-09 | 2016-10-13 | Eisai R & D Management Co., Ltd. | Fgfr4 inhibitors |
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| EP3325469A4 (en) * | 2015-07-20 | 2019-01-23 | Dana Farber Cancer Institute, Inc. | NOVEL PYRIMIDINS AS EGFR INHIBITORS AND METHOD FOR THE DISEASE TREATMENT THEREWITH |
| CN105418441A (zh) * | 2015-12-22 | 2016-03-23 | 中国工程物理研究院化工材料研究所 | 2,3-二氯-4-羟基苯胺的制备方法 |
| US10934311B2 (en) | 2016-01-08 | 2021-03-02 | Hangzhou Innogate Pharma Co., Ltd. | Heterocyclic compound used as FGFR inhibitor |
| 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 |
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