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86 条记录 (耗时 0.031 秒)

    1,6-naphthyridine anti-convulsants
    2.
    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。

    Substituted benzamide derivatives and pharmaceutical compositions containing them
    3.
    发明授权
    Substituted benzamide derivatives and pharmaceutical compositions containing them 失效
    取代的苯甲酰胺衍生物和含有它们的药物组合物

    公开(公告)号：US06395759B1

    公开(公告)日：2002-05-28

    申请号：US09319124

    申请日：1999-06-01

    申请人： Mervyn Thompson ,  Antonio Kuok Keong Vong ,  Robert William Ward

    发明人： Mervyn Thompson ,  Antonio Kuok Keong Vong ,  Robert William Ward

    IPC分类号： A61K31445

    CPC分类号： C07D211/26 ,  C07D207/09

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, where G is a methylene or ethylene linkage; R1 is hydrogen, C1-6alkylO—; R2 is hydrogen, halogen, CN, N3, trifluoromethyldiazirinyl, CF3, CF3O—, CF3S—, CF3CO—, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO—, C1-6alkylCO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4-alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl and substituted benzoyl, phenyl-C1-4alkyl-, C1-6alkylSO2—, (C1-4alkyl)2NSO2— or (C1-4alkyl)NHSO2—; R3 is hydrogen, halogen, CN, N3, trifluoromethyldiazirinyl, C1-6alkylO—, C1-6alkylS—, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl, CF3CO—, C1-6alkylCO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, or —NR5R6 where R5 is hydrogen or C1-4alkyl; and R6 is hydrogen, C1-4alkyl, —CHO, —CO2C1-4alkyl or —COC1-4alkyl; R4 is hydrogen, C1-6alkyl, C1-6alkenyl, or C1-6alkynyl, are useful in the prevention and treatment of anxiety, mania, depression disorders associated with a subarachnoid haemorrhage or neural shock, the effects associated with withdrawal from substances of abuse such as cocaine, nicotine, alcohol and benzodiazepines, disorders treatable and/or preventable with anti-convulsive agents, such as epilepsy including post-traumatic epilepsy, Parkinson's disease, psychosis, migraine, etc.

    摘要翻译： 式（I）化合物及其药学上可接受的盐，其中G是亚甲基或亚乙烯键; R1是氢，C1-6烷基， R2是氢，卤素，CN，N3，三氟甲基二氮丙烯基，CF3，CF3O-，CF3S-，CF3CO-，C1-6烷基，C3-6环烷基，C3-6环烷基C1-4烷基 - ，C1-6烷基， - C1-6烷基， 苯基，苯甲酰基，苯基-C 1-4烷基，C 1-6烷基SO 2 - ，（C 1-4烷基）2 NSO 2 - 或（C 1 -C 4烷基） 4烷基）NHSO 2 - ; R 3是氢，卤素，CN，N 3，三氟甲基二氮嗪基，C 1-6烷基O - ，C 1-6烷基-S-，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 CO-， 苯基，苯氧基，苄氧基，苯甲酰基，苯基-C 1-4烷基 - 或-NR 5 R 6，其中R 5是氢或C 1-4烷基; R 3是C 1-4烷基， 并且R 6是氢，C 1-4烷基，-CHO，-CO 2 C 1-4烷基或-COC 1-4烷基; R4是氢，C1-6烷基，C1-6链烯基或C1-6炔基，可用于预防和治疗与蛛网膜下腔出血或神经性休克相关的焦虑，躁狂症，抑郁症，与滥用物质相关的作用 可卡因，尼古丁，酒精和苯并二氮杂，可用抗惊厥药治疗和/或预防的疾病，如癫痫，包括创伤后癫痫，帕金森病，精神病，偏头痛等。

    Derivatives of 4-(2-aminoethyl)phenoxymethyl-phosphonic and -phosphinic acid and pharmaceutical and veterinary uses therefor
    4.
    发明授权
    Derivatives of 4-(2-aminoethyl)phenoxymethyl-phosphonic and -phosphinic acid and pharmaceutical and veterinary uses therefor 失效
    4-（2-氨基乙基）苯氧基甲基 - 膦酸和次膦酸的衍生物及其药用和兽用用途

    公开(公告)号：US5726165A

    公开(公告)日：1998-03-10

    申请号：US465486

    申请日：1995-06-05

    申请人： Lee James Beeley ,  Mervyn Thompson ,  David Kenneth Dean ,  Nikesh Rasiklal Kotecha ,  John Michael Berge ,  Robert William Ward

    发明人： Lee James Beeley ,  Mervyn Thompson ,  David Kenneth Dean ,  Nikesh Rasiklal Kotecha ,  John Michael Berge ,  Robert William Ward

    IPC分类号： C07C217/34 ,  C07D317/46 ,  C07F9/30 ,  C07F9/32 ,  C07F9/40 ,  A61K31/665 ,  A61K31/66 ,  C07F9/665

    CPC分类号： C07F9/3211 ,  C07C217/34 ,  C07D317/46 ,  C07F9/301 ,  C07F9/303 ,  C07F9/3223 ,  C07F9/4006 ,  C07C2101/14

    摘要： A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, or solvate thereof, wherein, R.sup.o represents an aryl group, optionally substituted; X represents O or S; R.sup.1 and R.sup.1a each independently represents hydrogen or an alkyl group; R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b): ##STR2## wherein R.sup.4 represent hydrogen, alkyl, hydroxyalkyl, arylalkyl, aralkyloxyalkyl or cycloalkyl and R.sup.5 represent hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, arylalkoxyalkyloxy, cycloalkyloxy, hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, arylalkyloxyalkyl or R.sup.5 together with OR.sup.4 represents O(CH.sub.2).sub.n O wherein n is 2, 3 or 4; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.2 represents a moiety of formula (c): ##STR3## or an ester or amide thereof; a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.

    摘要翻译： 式（I）的化合物：其中，R 1表示任选被取代的芳基;（I）化合物或其药学上可接受的盐或其溶剂合物， X表示O或S; R 1和R 1a各自独立地表示氢或烷基; R 2表示OCH 2 CO 2 H或其酯或酰胺，或R 2表示式（b）的部分：其中R 4表示氢，烷基，羟烷基，芳烷基，芳烷氧基烷基或环烷基，R 5表示羟基，烷氧基，芳基烷氧基 ，羟烷基氧基，烷氧基烷氧基，芳基烷氧基烷氧基，环烷氧基，氢，烷基，取代烷基，环烷基，芳基，芳基烷基，芳基烷氧基烷基或R5与OR4一起表示O（CH2）nO，其中n为2,3或4; 并且R 3表示氢，卤素，烷基或烷氧基，或者R 3与R 2一起表示式（c）的部分：（c）或其酯或酰胺; 含有这种化合物的药物组合物，制备这种化合物的方法以及这种化合物在医药中的用途。

    Piperazine derivatives, their preparation and uses in therapy
    10.
    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.