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    • 3. 发明授权
      US06277861B1 Anti-convulsant isoquinolyl-benzamide derivatives 失效
    • Anti-convulsant isoquinolyl-benzamide derivatives
    • 抗惊厥异喹啉基 - 苯甲酰胺衍生物
    • US06277861B1
    • 2001-08-21
    • US09381369
    • 1999-12-21
    • John David Harling , Barry Sidney Orlek , Mervyn Thompson
    • John David Harling , Barry Sidney Orlek , Mervyn Thompson
    • A61K3147
    • C07D217/04
    • Compounds of formula (I) and pharmaceutically acceptable salts thereof, where R1 is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), C1-6alkenyl, C1-6alkynyl, C1-6alkylCO—, formyl, CF3CO— or C1-6alkylSO2—; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, CF3O—, CF3S—, CF3CO—, trifluoromethyldiazirinyl, C 1-6?alkyl, 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 C1-4alkyl, 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 and unsubstituted or substituted by —OH or ═O; and the two R3 groups and the two R4 groups are each independently hydrogen or C1-6alkyl or the two R3 groups and/or the two R4 groups together form a C3-6spiroalkyl group provided that at least one R3 and R4 group is not hydrogen, are useful in the treatment and prophylaxis of epilepsy and other disorders.
    • 式（I）化合物及其药学上可接受的盐，其中R 1为氢，C 1-6烷基（任选被羟基或C 1-4烷氧基取代），C 1-6烯基，C 1-6炔基，C 1-6烷基CO-，甲酰基，CF 3 CO-或C 1 烷基SO2-; 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-，三氟甲基二氮丙烯基，C 1-6烷基，C 1-6烯基，C 1-6炔基，C 1-6全氟烷基， C 1-6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-， -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且未被取代或被-OH或= O取代的碳环; 并且两个R 3基团和两个R 4基团各自独立地为氢或C 1-6烷基，或者两个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和R 4
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 4. 发明授权
      US06245778B1 1,6-naphthyridine anti-convulsants 失效
    • 1,6-naphthyridine anti-convulsants
    • 1,6-萘啶抗惊厥药
    • US06245778B1
    • 2001-06-12
    • US09424399
    • 1999-11-23
    • Michael Stewart Hadley , John David Harling , Frank Peter Harrington , Mervyn Thompson , Robert William Ward
    • Michael Stewart Hadley , John David Harling , Frank Peter Harrington , Mervyn Thompson , Robert William Ward
    • A61K314375
    • C07D471/04
    • Compounds of formula (I) and pharmaceutically acceptable salts thereof: where R1 is hydrogen, C1-6 alkyl optionally substituted by hydroxy or C1-4alkoxy, or C1-6 alkylphenyl; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, C1-6 alkylO-, C1-6 alkylS-, C1-6 alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl, CF3, CF3O, CF3CO—, C1-6alkylCO-, C3-6cycloalkylCO-, C3-6cycloalkyl-C1-4alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, or —NR3R4 where R3 is hydrogen or C1-4 alkyl, and R4 is hydrogen, C1-4alkyl, —CHO, —CO2C1-4alkyl or —COC1-4alkyl; or two R2 groups form a saturated carbocyclic ring optionally interrupted by oxygen; and X is selected from hydrogen, halogen, cyano, alkyl and alkoxy; are useful in the treatment and prophylaxis of inter alia epilepsy.
    • 式（I）化合物及其药学上可接受的盐：其中R 1是氢，任选被羟基或C 1-4烷氧基取代的C 1-6烷基或C 1-6烷基苯基; R 2是氢或至多三个选自卤素，NO 2，CN的取代基 ，N 3，C 1-6烷基，C 1-6烷基，C 1-6烷基，C 3-6环烷基，C 3-6环烷基-C 1-4烷基 - ，C 1-6烯基，C 1-6炔基，CF 3，CF 3 O，CF 3 CO-， C 3-6烷基CO-，C 3-6环烷基CO-，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 - 或-NR 3 R 4，其中R 3是氢或C 1-4烷基，R 4是氢， 4个烷基，-CHO，-CO 2 C 1-4烷基或-COC 1-4烷基;或两个R 2基团形成任选被氧中断的饱和碳环; X选自氢，卤素，氰基，烷基和烷氧基;可用于处理和 特别是癫痫预防。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 6. 发明授权
      US06410555B1 Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity 失效
    • Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity
    • 具有抗惊厥活性的四氢萘并吡喃基甲酰胺
    • US06410555B1
    • 2002-06-25
    • US09719335
    • 2001-02-16
    • John David Harling , Frank Peter Harrington , Mervyn Thompson
    • John David Harling , Frank Peter Harrington , Mervyn Thompson
    • A61K31435
    • C07D471/04 , C07D471/10
    • 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.
    • 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
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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