发明名称 SUBSTITUTED ISOQUINOLINE DERIVATIVES AND THEIR USE AS ANTICONVULSANTS
摘要 Compounds of formula (I) and pharmaceutically acceptable salts thereof; where Q is a monocyclic or bicyclic aryl or heteroaryl ring, R<1> is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), C1-6alkenyl, C1-6alkynyl, C1-6alkylCO-, formyl, CF3CO- or C1-6alkylSO2-, R<2> is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, CF3O-, CF3S-, CF3CO-, trifluoromethyldiazirinyl, C1-6alkyl, C1-6alkenyl, C1-6alkynyl, C1-6perfluoroalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO-, C1-6alkylCO-, C3-6cycloalkylO-, C3-6cycloalkylCO-, C3-6cycloalkyl-C1-4alkylO-, C3-6cycloalkyl-C1-4alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, C1-6alkylS-, C1-6alkylSO2-, (C1-4alkyl)2NSO2-, (C1-4alkyl)NHSO2-, (C1-4alkyl)2NCO-, (C1-4alkyl)NHCO- or CONH2; or -NR<3>R<4> where R<3> is hydroven or C1-4alkyl, and R<4> is hydrogen, C1-4alkyl, formyl, -CO2C1-4alkyl or -COC1-4alkyl; or two R<2> groups together form a carbocyclic ring that is saturated or unsaturated and unsubstituted or substituted by -OH or =O; and X is hydrogen, halogen, C1-6alkoxy, C1-6alkyl, amino or trifluoroacetylamino, but when X is hydrogen excluding compounds in which R<2> is 2-alkoxy and when X is hydrogen excluding the compounds N-(7-iodo-2-methyl-1,2,3,4-tetrahydroisoquinolin-5-yl) -5-benzoyl-2-methoxybenzamide, N-(7-iodo-1,2,3,4-tetrahydroisoquinolin-5-yl) -5-benzoyl-2-methoxybenzamide, N-(5-iodo-1,2,3,4-tetrahydroisoquinolin-7-yl) -5-benzoyl-2-methoxybenzamide, N-(5-iodo-1,2,3,4-tetrahydroisoquinolin-7-yl) -2-methoxy-4-trifluoromethyldiazirinylbenzamide, N-(5-iodo-1,2,3,4-tetrahydroisoquinolin-7-yl) -2-methoxy-5-trifluoromethyldiazirinylbenzamide, N-(7-iodo-1,2,3,4,-tetrahydroisoquinolin-5-yl) -2-methoxy-5-trifluoromethyldiazirinylbenzamide et N-(8-fluoro-2-methyl-1,2,3,4-tetrahydroisoquinolin-5-yl) -4-t-butyl-2-methoxybenzamide, are useful inter alia in the treatment and prophylaxis of epilepsy.
申请公布号 WO9841508(A1) 申请公布日期 1998.09.24
申请号 WO1998GB00782 申请日期 1998.03.16
申请人 SMITHKLINE BEECHAM PLC;THOMPSON, MERVYN;WARD, ROBERT, WILLIAM;EDWARDS, PETER, DAVID 发明人 THOMPSON, MERVYN;WARD, ROBERT, WILLIAM;EDWARDS, PETER, DAVID
分类号 A61P25/04;A61K31/472;A61K31/4725;A61P3/10;A61P21/00;A61P21/02;A61P25/06;A61P25/08;A61P25/16;A61P25/18;A61P25/20;A61P25/22;A61P25/24;A61P25/28;A61P25/30;C07D217/02;C07D217/04;C07D217/06;C07D401/12;C07D405/12;C07D409/12;C07D413/12;C07D417/12;(IPC1-7):C07D217/04;A61K31/47 主分类号 A61P25/04
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