发明名称 BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS
摘要 This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain.
申请公布号 US2014296245(A1) 申请公布日期 2014.10.02
申请号 US201214355552 申请日期 2012.10.30
申请人 XENON PHARMACEUTICALS INC. 发明人 Sun Shaoyi;Zenova Alla Yurevna;Chafeev Mikhail;Jia Qi;Zhang Zaihui;Oballa Renata Marcella
分类号 C07D417/12;C07D285/08;C07D257/06;C07D277/52;C07D261/14;C07D239/42;C07D285/135 主分类号 C07D417/12
代理机构 代理人
主权项 1. A compound of formula (I): wherein: k is 0, 1, 2, 3 or 4; m is 0, 1 or 2; n is 0, 1, 2, 3, 4 or 5; q is 0, 1, 2, 3, 4, 5 or 6; A is —O— or —S—; is aryl or N-heteroaryl; R1 is —O—, —C(R9)2—, —N(R10)—, —N(R11)- or —S(O)t (where t is 0, 1 or 2); R2 is C(R9) or N; R3 is hydrogen, alkyl, haloalkyl, optionally substituted aryl or optionally substituted aralkyl; or R3 is a direct bond to R4; R4 is H, optionally substituted alkyl, optionally substituted heterocyclyl, optionally substituted heteroaryl, optionally substituted cycloalkyl, haloalkyl, —C(O)R10, —C(O)N(R10)2 or —C(═NCN)N(R10)2; or R3 and R4, together with the nitrogen to which they are both attached, form an optionally substituted N-heterocyclyl or optionally substituted N-heteroaryl; each R5 and each R6 are independently hydrogen, alkyl, halo, haloalkyl, nitro, cyano, —OR10, —S(O)R10 (where t is 0, 1 or 2), —C(O)OR10, —C(O)R10 or —C(O)N(R10)2; each R7 is independently hydrogen, alkyl, halo, haloalkyl, —OR10, —S(O)tR10 (where t is 0, 1 or 2), —C(O)OR10, —C(O)R10 or —C(O)N(R10)2; or any two R7's on the same carbon may form an oxo and the other R7's are independently hydrogen, alkyl, halo, haloalkyl, —OR10, —S(O)tR10 (where t is 0, 1 or 2), —C(O)OR10, —C(O)R10 or —C(O)N(R10)2; or any two R7's on different carbons may form an optionally substituted straight or branched alkylene chain optionally containing one or more heteroatoms, and the other R7's, if present, are independently hydrogen, alkyl, halo, haloalkyl, —OR10, —S(O)tR10 (where t is 0, 1 or 2), —C(O)OR10, —C(O)R10 or —C(O)N(R10)2, R8 is a direct bond or an optionally substituted straight or branched alkylene chain; each R9 is independently hydrogen, alkyl, halo, haloalkyl, —OR4, —N(R10)2, —N(R11)2, —S(O)tR10 (where t is 0, 1 or 2), —C(O)OR10, —C(O)R10 or —C(O)N(R10)2; each R10 is independently hydrogen, alkyl, haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl; and each R11 is independently —C(O)R10; —C(O)OR10, —C(O)N(R10)2, —S(O)pR10 (where p is 1 or 2) or —S(O)PN(R10)2 (where p is 1 or 2); as individual stereoisomers, enantiomers or tautomers thereof or mixtures thereof; or as pharmaceutically acceptable salts, solvates or prodrugs thereof.
地址 Burnaby CA US