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    Piperazine derivatives, their preparation and uses in therapy
    12.
    发明授权
    Piperazine derivatives, their preparation and uses in therapy 失效

    公开(公告)号：US07109201B2

    公开(公告)日：2006-09-19

    申请号：US10471433

    申请日：2002-03-11

    申请人： Mervyn Thompson ,  Paul Adrian Wyman

    发明人： Mervyn Thompson ,  Paul Adrian Wyman

    IPC分类号： A61K31/496 ,  C07D403/04 ,  C07D401/14

    CPC分类号： C07D401/10 ,  C07D209/08

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: in which Ra is a group of formula (i) wherein P2 is phenyl, naphthyl, heteroaryl or a 5 to 7 membered heterocyclic ring; P3 is phenyl, naphthyl or heteroaryl; R1 is NR4COR5, NR4SO2R5, CH2NR4SO2R5, CH2NR4COR5 or CH2NR4CO2R5 where R4 and R5 are independently hydrogen or C1-6alkyl; R2 and R3 are independently halogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkoxy, COC1-6alkyl, haloC1-6alkyl, cyano or NR6R7 where R6 and R7 are independently hydrogen or C1-6alkyl; b and c are independently 0, 1, 2 or 3; Y is a single bond, CH2 or NH; W is —(CR9R10)t—where t is 2, 3 or 4 and R9 and R10 are independently hydrogen or C1-6alkyl or W is a group CH═CH; Rb is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, COC1-6alkyl, cyano or C1-6alkoxy; and Rc is hydrogen or C1-6alkyl. Processes for preparation of the compounds and their uses in therapy, particularly depression, are also disclosed.

    Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity
    16.
    发明授权
    Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity 失效
    具有抗惊厥活性的四氢萘并吡喃基甲酰胺

    公开(公告)号：US06410555B1

    公开(公告)日：2002-06-25

    申请号：US09719335

    申请日：2001-02-16

    申请人： John David Harling ,  Frank Peter Harrington ,  Mervyn Thompson

    发明人： John David Harling ,  Frank Peter Harrington ,  Mervyn Thompson

    IPC分类号： A61K31435

    CPC分类号： C07D471/04 ,  C07D471/10

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts and solvates: where R1 is hydrogen, C1-6alkyl (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—, CF3SO2—, CF3CO—, C1-6alkyl, C1-6alkenyl, C1-6alkynyl, C1-6perfluoroalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkyl, 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 C1-4alkyl, 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, optionally interrupted by O or NH; R3 groups and R4 groups are each independently hydrogen or C1-6alkyl and/or the two R3 groups and/or the two R4 groups together form a C3-6spiroalkyl 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.

    摘要翻译： 式（I）化合物及其药学上可接受的盐和溶剂化物：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; R2是氢或最多三个选自卤素，NO 2，CN，N 3，CF 3 O-，CF 3 S-，CF 3 SO 2 - ，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，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 ，（C 1-4烷基）2 NSO 2 - ，（C 1-4烷基）NHSO 2 - ，（C 1-4烷基）2 NCO - ，（C 1-4烷基），C 1-4烷基 ）NHCO-或CONH 2; 或-NR5R6，其中R5是氢或C1-4烷基，R6是氢，C1-4烷基，甲酰基，-CO2C1-4烷基或-COC1-4烷基; 或两个R 2基团一起形成饱和或不饱和的碳环，任选被O或NH中断; 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基团和/或两个R 4基团一起形成C 3-6螺环烷基，条件是至少一个R 3或R 4基团不是氢; X选自氢，卤素，氰基，烷基和烷氧基