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    Anti-convulsant isoquinolyl-benzamide derivatives
    2.
    发明授权
    Anti-convulsant isoquinolyl-benzamide derivatives 失效
    抗惊厥异喹啉基 - 苯甲酰胺衍生物

    公开(公告)号：US06277861B1

    公开(公告)日：2001-08-21

    申请号：US09381369

    申请日：1999-12-21

    申请人： John David Harling ,  Barry Sidney Orlek ,  Mervyn Thompson

    发明人： John David Harling ,  Barry Sidney Orlek ,  Mervyn Thompson

    IPC分类号： A61K3147

    CPC分类号： C07D217/04

    摘要： 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.

    摘要翻译： 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

    1,6-naphthyridine anti-convulsants
    3.
    发明授权
    1,6-naphthyridine anti-convulsants 失效
    1,6-萘啶抗惊厥药

    公开(公告)号：US06245778B1

    公开(公告)日：2001-06-12

    申请号：US09424399

    申请日：1999-11-23

    申请人： Michael Stewart Hadley ,  John David Harling ,  Frank Peter Harrington ,  Mervyn Thompson ,  Robert William Ward

    发明人： Michael Stewart Hadley ,  John David Harling ,  Frank Peter Harrington ,  Mervyn Thompson ,  Robert William Ward

    IPC分类号： A61K314375

    CPC分类号： C07D471/04

    摘要： 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.

    摘要翻译： 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。

    Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity
    4.
    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

    Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity
    6.
    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：US06762192B2

    公开(公告)日：2004-07-13

    申请号：US10154997

    申请日：2002-05-23

    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： A61K3144

    CPC分类号： C07D471/04 ,  C07D471/10

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts and solvates: where R1 is hydrogen, C1-6 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.

    摘要翻译： 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。

    Substituted benzamide derivatives and their use as anticonvulsants
    7.
    发明授权
    Substituted benzamide derivatives and their use as anticonvulsants 失效
    取代的苯甲酰胺衍生物及其作为抗惊厥药的用途

    公开(公告)号：US6110934A

    公开(公告)日：2000-08-29

    申请号：US202524

    申请日：1998-12-16

    申请人： John David Harling ,  Barry Sidney Orlek ,  Mervyn Thompson

    发明人： John David Harling ,  Barry Sidney Orlek ,  Mervyn Thompson

    IPC分类号： A61K31/472 ,  C07D209/44 ,  C07D217/04 ,  C07D223/16 ,  C07D401/12 ,  A61K31/47

    CPC分类号： C07D223/16 ,  A61K31/472 ,  C07D209/44 ,  C07D217/04 ,  C07D401/12

    摘要： This invention relates to substituted benzamido-heterocyclic compounds of general formula (I) having an alkoxy substituent at the C2 position of the benzamido group and various substituents at positions C4 and C5, being optionally substituted on the N atom of the heterocyclic system, and where the unsaturated ring of the heterocyclic system is a 5,6, 7 or 8-membered ring. Also to the use of these compounds as anticonvulsants in certain medical conditions, and to processes for making them.

    摘要翻译： PCT No.PCT / EP97 / 03131 Sec。 371日期1998年12月16日第 102（e）日期1998年12月16日PCT提交1997年6月13日PCT公布。 出版物WO97 / 48683 日期1997年12月24日本发明涉及通式（I）的取代苯甲酰氨基 - 杂环化合物，其在苯甲酰氨基的C2位具有烷氧基取代基和C4和C5位的各种取代基，任选在 并且其中杂环体系的不饱和环是5,6,7或8元环。 还涉及在某些医疗条件下使用这些化合物作为抗惊厥药，以及制备它们的方法。