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    Substituted benzamide derivatives and pharmaceutical compositions containing them
    84.
    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
    85.
    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。

    9H-pyrido[2,B-8]indole-3-carboxylic acid ester compounds having useful pharmaceutical activity
    86.
    发明授权
    9H-pyrido[2,B-8]indole-3-carboxylic acid ester compounds having useful pharmaceutical activity 失效
    具有有用的药学活性的9H-吡啶并[2，B-8]吲哚-3-羧酸酯化合物

    公开(公告)号：US4952584A

    公开(公告)日：1990-08-28

    申请号：US307068

    申请日：1989-02-06

    申请人： Mervyn Thompson ,  Ian T. Forbes

    发明人： Mervyn Thompson ,  Ian T. Forbes

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-4 alkyl wherein the phenyl moiety is optionally substituted by one or more C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, halo, trifluoromethyl, nitro, amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.2-7 alkanoyl, cyano, carbamoyl or carboxy groups; R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylthio, hydroxy, C.sub.2-7 alkanoyl, chloro, fluoro, trifluoromethyl, nitro, amino optionally substituted by one or two C.sub.1-6 alkyl groups or by C.sub.2-7 alkanoyl, cyano, carbamoyl and carboxy, and phenyl, phenyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkoxy in which any phenyl moiety is optionally substituted by any of these groups; R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-C.sub.1-4 alkyl, C.sub.2-6 alkenyl, C.sub.1-7 alkanoyl, C.sub.1-6 alkylsulphonyl, di-(C.sub.1-6 alkyl)amino C.sub.1-6 alkyl, 3-oxobutyl, 3-hydroxybutyl, phenyl, phenyl C.sub.1-4 alkyl, benzoyl, phenyl C.sub.2-7 alkanoyl or benzenesulphonyl any of which phenyl moieties are optionally substituted by one or two halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3, amino or carboxy, or R.sub.5 and R.sub.6 together are C.sub.2-6 polymethylene optionally interrupted by oxygen or NR.sub.9 wherein R.sub.9 is hydrogen or C.sub.1-6 alkyl optionally substituted by hydroxy; R.sub.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; and --CO.sub.2 R.sub.8 is a pharmaceutically acceptable ester group, processes for its preparation and its use for the treatment or prophylaxis of anxiety or depression.

    摘要翻译： 式（I）化合物或其药学上可接受的盐：其中：R 1是氢，C 1-6烷基，苯基或苯基C 1-4烷基，其中苯基部分任选地被一个或多个C 1 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，羟基，C 2-7烷酰基，卤素，三氟甲基，硝基，任选被一个或两个C 1-6烷基取代的氨基或C 2-7烷酰基，氰基，氨基甲酰基或 羧基; R2，R3和R4独立地选自氢，C1-6烷基，C1-6烷氧基，C1-6烷氧基羰基，C1-6烷硫基，羟基，C2-7烷酰基，氯，氟，三氟甲基，硝基，任选被 一个或两个C 1-6烷基或C 2-7烷酰基，氰基，氨基甲酰基和羧基，以及苯基，苯基C 1-4烷基或苯基C 1-4烷氧基，其中任何苯基部分任选被这些基团任意取代; R 5和R 6独立地选自氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基-C 1-4烷基，C 2-6烯基，C 1-7烷酰基，C 1-6烷基磺酰基，二 - （C 1-6） 烷基）氨基C 1-6烷基，3-氧代丁基，3-羟基丁基，苯基，苯基C 1-4烷基，苯甲酰基，苯基C 2-7烷酰基或苯磺酰基任何苯基部分任选被一个或两个卤素取代，C 1-6 烷基，C 1-6烷氧基，CF 3，氨基或羧基，或R 5和R 6一起是任选被氧或NR 9中断的C 2-6多亚甲基，其中R 9是氢或任选被羟基取代的C 1-6烷基; R 7是氢，C 1-6烷基，C 3-6环烷基，C 3-6环烷基-C 1-4烷基，C 2-6烯基或C 2-6炔基; 和-CO 2 R 8是药学上可接受的酯基，其制备方法及其用于治疗或预防焦虑或抑郁症的用途。