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    • 64. 发明授权
    • Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity
    • 具有抗惊厥活性的四氢萘并吡喃基甲酰胺
    • US06762192B2
    • 2004-07-13
    • US10154997
    • 2002-05-23
    • John David HarlingFrank Peter HarringtonMervyn Thompson
    • John David HarlingFrank Peter HarringtonMervyn Thompson
    • A61K3144
    • C07D471/04C07D471/10
    • Compounds of formula (I) and pharmaceutically acceptable salts and solvates: where R1 is hydrogen, C1-6 alkyl (optionally substituted by hydroxy or C1-4alkoxy), phenyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, CF3O—, CF3S—, CF3CO—, 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 —NR5R6 where R5 is hydrogen or C1-4 alkyl, and R6 is hydrogen, C1-4alkyl, formyl, —CO2C1-4alkyl or —COC1-4alkyl; or two R2 groups together form a carbocyclic ring that is saturated or unsaturated. R3 groups and R4 groups are each independently hydrogen or C1-6 alkyl and/or the two R3 groups and/or the two R4 groups together form a C3-6 spiroalkyl group, provided that at least one R3 or R4 group is not hydrogen; and X is selected from hydrogen, halogen, cyano, alkyl and alkoxy, are useful in the treatment and prophylaxis of epilepsy, migraine, and other disorders.
    • 式(I)化合物及其药学上可接受的盐和溶剂合物:其中R 1是氢,C 1-6烷基(任选被羟基或C 1-4烷氧基取代),苯基-C 1-4烷基 - ,C 1-6烯基,C 1-6炔基 R 2是氢或至多三个选自卤素,NO 2,CN,N 3,CF 3 O-,CF 3 S-,CF 3 CO-,C 1-6烷基,C 1-6烯基,C 1-6炔基,C 1-6全氟烷基,C 3-6环烷基 ,C 3-6环烷基-C 1-4烷基 - ,C 1-6烷基O-,C 1-6烷基CO-,C 3-6环烷基O - ,C 3-6环烷基CO-,C 3-6环烷基-C 1-4烷基O - ,C 3-6环烷基-C 1-4烷基CO-,苯基, 苯氧基,苄氧基,苯甲酰基,苯基-C 1-4烷基 - ,C 1-6烷基-S-,C 1-6烷基SO 2 - ,(C 1-4烷基)2NSO 2 - ,(C 1-4烷基)NHSO 2 - ,(C 1-4烷基)2 CO-,(C1- 4烷基)NHCO-或CONH 2;或-NR 5 R 6,其中R 5是氢或C 1-4烷基,R 6是氢,C 1-4烷基,甲酰基,-CO 2 C 1-4烷基或-COC 1 1-4烷基或两个R 2基团一起形成饱和或不饱和的碳环.R 3基团和R 4基团各自独立地为氢或C 1-6烷基和/或两个R 3基团。 格罗 和/或两个R 4基团一起形成C 3-6螺烷基,条件是至少一个R 3或R 4基团不是氢; 和X选自氢,卤素,氰基,烷基和烷氧基,可用于治疗和预防癫痫,偏头痛和其他疾病。