发明名称 SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS
摘要 This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
申请公布号 US2015291623(A1) 申请公布日期 2015.10.15
申请号 US201414542367 申请日期 2014.11.14
申请人 Xenon Pharmaceuticals Inc. 发明人 Chafeev Mikhail;Chowdhury Sultan;Fraser Lauren;Fu Jianmin;Langille Jonathan;Liu Shifeng;Sun Jianyu;Sun Shaoyi;Sviridov Serguei;Wood Mark;Zenova Alla Yurevna;Jia Qi;Cadieux Jean-Jacques Alexandre;Gauthier Simon J.;Douglas Amy Frances;Hsieh Tom;Chakka Nagasree;Cikojevic Zoran
分类号 C07D513/20;C07D519/00;C07D491/22;C07D491/20;C07D498/20 主分类号 C07D513/20
代理机构 代理人
主权项 1. A compound of formula (II): wherein: each R3a is hydrogen or fluoro; R3 is hydrogen, methyl, 3-(trifluoromethyl)pyridin-2-yl]methyl, 2,5-dimethyl-1-(1-methylethyl)-1H-pyrrol-3-yl]methyl, (3-isopropylisoxazol-5-yl)methyl, (4-bromo-2-thienyl)methyl, 1-benzofuran-2-ylmethyl, [2-methyl-5-(trifluoromethyl)-1,3-oxazol-4-yl]methyl, [5-(4-chlorophenyl)-2-(trifluoromethyl)furan-3-yl]methyl, [5-chloro-1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl, 5-methoxypyridin-3-yl, 4-bromobenzyl, [(2S)-5-oxopyrrolidin-2-yl]methyl, tert-butoxycarbonyl, cyanomethyl, [5-(trifluoromethyl)-2-furyl]methyl, (5-chloro-2-thienyl)methyl, (3-chlorothiophen-2-yl)methyl, [3-(2,6-dichlorophenyl)-5-methylisoxazol-4-yl]methyl, {2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-4-yl}methyl, (5-phenyl-1,3,4-oxadiazol-2-yl)methyl, [5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl]methyl, [1,3]oxazolo[4,5-b]pyridin-2-ylmethyl, (2-isopropyl-1,3-thiazol-5-yl)methyl, (2-isopropyl-1,3-oxazol-5-yl)methyl, 3-(tert-butoxycarbonylamino)-3-(cyclopropyl)propyl, 4-(methylsulfanyl)benzyl, 2-cyanoethyl, (2-bromo-1,3-thiazol-5-yl)methyl, [2-amino-4-(trifluoromethyl)-1,3-thiazol-5-yl]methyl, (2-amino-1,3-thiazol-4-yl)methyl, (5-chlorothiophen-2-yl)methyl, [2-(1-methylethyl)-1,3-thiazol-4-yl]methyl, (5-chloro-1,2,4-thiadiazol-3-yl)methyl, (5-chloro-1,2,4-thiadiazol-3-yl)methyl, 4-methoxybenzyl, (2S)-1,4-dioxan-2-ylmethyl, (2-chloro-1,3-thiazol-5-yl)methyl, [2-(dimethylamino)-1,3-thiazol-5-yl]methyl, (2-morpholin-4-yl-1,3-thiazol-5-yl)methyl, (2-piperidin-1-yl-1,3-thiazol-5-yl)methyl, (2-methoxy-1,3-thiazol-5-yl)methyl, 2-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]ethyl, [5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]methyl, (5-cyclopropyl-1,2,4-oxadiazol-3-yl)methyl, [5-(difluoromethyl)-1,2,4-oxadiazol-3-yl]methyl, (5-tert-butyl-1,2,4-oxadiazol-3-yl)methyl, [5-(1-methylethyl)-1,2,4-oxadiazol-3-yl]methyl, (4-methylpiperazin-1-yl)methyl, (3-methyl-2-oxo-1,3-oxazolidin-5-yl)methyl, 2-(1-(methylethyl)aminocarbonylpiperidin-3yl)ethyl, (4-cyanothien-2-yl)methyl, [5-trifluoromethyl-4-(methyl)aminocarbonylfuran-2-yl]methyl, (5-trifluoromethyl-4-aminocarbonylfuran-2-yl)methyl, [5-trifluoromethyl-4-(dimethyl)aminocarbonylfuran-2-yl]methyl, [4-(cyclopropyl)aminocarbonyl-1,3-oxazol-2-yl]methyl, (2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)methyl, or [4-(methylethyl)aminocarbonyl-1,3-oxazol-2-yl]methyl; and each R4 is independently hydrogen, chloro, bromo, trifluoromethyl, cyano, 6-(dimethylamino)pyridin-3-yl, tetrahydrofuran-3-yl or furan-3-yl; as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof.
地址 Burnaby CA US