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21 条记录 (耗时 0.023 秒)

    Anti-convulsant isoquinolyl-benzamide derivatives
    1.
    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

    Substituted benzamide derivatives and their use as anticonvulsants
    2.
    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。

    Substituted cycloalkylamine derivatives and their use as calcium channel antagonists
    5.
    发明授权
    Substituted cycloalkylamine derivatives and their use as calcium channel antagonists 失效
    取代的环烷基胺衍生物及其作为钙通道拮抗剂的用途

    公开(公告)号：US5817698A

    公开(公告)日：1998-10-06

    申请号：US704585

    申请日：1996-09-20

    申请人： Thomas Henry Brown ,  John David Harling ,  Barry Sidney Orlek

    发明人： Thomas Henry Brown ,  John David Harling ,  Barry Sidney Orlek

    IPC分类号： A61K31/135 ,  A61P9/10 ,  A61P25/00 ,  A61P25/28 ,  A61P43/00 ,  C07C211/35 ,  C07C211/37 ,  C07C217/52 ,  C07C225/20 ,  C07C255/49 ,  C07C323/26 ,  C07C323/30 ,  C07C323/50

    CPC分类号： C07C225/20 ,  C07C217/52 ,  C07C323/26 ,  C07C2101/08

    摘要： A method of treatment of a condition or disease related to the accumulation of calcium in the brain cells of a mammal which comprises administering to a subject in need thereof an effective amount of a compound of formula (I), wherein X is O, S, C.dbd.O or a bond; p and q are independently 0-4; R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkylC.sub.1-4 alkyl; n is 1, 2, 3 or 4; and Ar is phenyl optionally substituted by 1 to 3 substituents selected from; halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-2 alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO.sub.2, amino, mono- or di- alkylamino and Ph(Alk.sup.1).sub.r Y(Alk.sup.2).sub.s -- where Ph is optionally substituted phenyl, Y is a bond, oxygen or a carbonyl group, Alk.sup.1 and Alk.sup.2 are independently C.sub.1-4 alkyl which may be straight or branched and r and s are independently 0 or 1, provided that the length of (Alk.sup.1).sub.r Y(Alk.sup.2).sub.s does not exceed 5 atoms, and pharmaceutically acceptable salts thereof; in the manufacture of a medicament for the treatment of a disorder wherein a calcium channel antagonist is indicated, e.g. ischaemic stroke. Certain novel compounds within formula (I) are also claimed.

    摘要翻译： PCT No.PCT / EP95 / 00964 Sec。 371日期：1996年9月20日 102（e）1996年9月20日PCT PCT 1995年3月14日PCT公布。 公开号WO95 / 26327 日期1995年10月5日式（I）治疗与哺乳动物脑细胞中钙累积相关的病症或疾病的方法，其包括向有需要的受试者施用有效量的化合物 式（I）的化合物，其中X为O，S，C = O或键; p和q独立地为0-4; R 1和R 2各自独立地选自氢，C 1-6烷基，C 3-6环烷基或C 3-6环烷基C 1-4烷基; n为1,2,3或4; 并且Ar是任选被1至3个选自下列的取代基取代的苯基; 卤素，C 1-4烷基，C 1-4烷氧基，C 1-2亚烷基二氧基，三氟甲基，三氟甲氧基，CN，NO 2，氨基，单 - 或二 - 烷基氨基和Ph（Alk 1）rY（Alk 2）s-，其中Ph是任选取代的苯基，Y是 键，氧或羰基，Alk1和Alk2独立地为可以是直链或支链的C 1-4烷基，r和s独立地为0或1，条件是（Alk1）rY（Alk2）s的长度不超过5 原子及其药学上可接受的盐; 在制备用于治疗其中指示钙通道拮抗剂的病症的药物中，例如， 缺血性中风。 还要求公式（I）中的某些新化合物。