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    Benzodiazepine compounds and their use as pharmaceuticals
    1.
    发明授权
    Benzodiazepine compounds and their use as pharmaceuticals 失效
    苯二氮卓类化合物及其作为药物的用途

    公开(公告)号：US4977150A

    公开(公告)日：1990-12-11

    申请号：US390029

    申请日：1989-08-04

    申请人： Jiban Kumar Chakrabarti ,  Terrence M. Hotten

    发明人： Jiban Kumar Chakrabarti ,  Terrence M. Hotten

    IPC分类号： C07D277/20 ,  A61K31/00 ,  A61K31/55 ,  A61P25/18 ,  A61P25/20 ,  C07D277/56 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D277/56

    摘要： Pharmaceutical thiazolo-[1,5]benzodiazepines of the formula ##STR1## in which R.sup.1, R.sup.2 , R.sup.3 and R.sup.4 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, benzyl or ZO-C.sub.2-6 alkyl wherein Z is hydrogen or an acyl group, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio; and in which ##STR3## represents a thiazole ring selected from ##STR4## and acid addition salts thereof. The compounds have cental nervous system activity.

    Halogenated amino methyl adamantane derivatives
    5.
    发明授权
    Halogenated amino methyl adamantane derivatives 失效
    卤代氨基甲基金刚烷衍生物

    公开(公告)号：US4061774A

    公开(公告)日：1977-12-06

    申请号：US566502

    申请日：1975-04-09

    申请人： Jiban Kumar Chakrabarti ,  Terrence Michael Hotten ,  David Edward Tupper

    发明人： Jiban Kumar Chakrabarti ,  Terrence Michael Hotten ,  David Edward Tupper

    IPC分类号： C07D295/096 ,  C07D303/06 ,  A61K31/13 ,  C07C87/40

    CPC分类号： C07D295/096 ,  C07D303/06

    摘要： Novel 2-substituted-1-methylamino adamantanes of formula: ##STR1## where X is hydroxyl or halogeno, and R.sup.1, R.sup.2 and R.sup.3 are hydrogen or C.sub.1-4 alkyl or R.sup.2 and R.sup.3 together with the nitrogen form a heterocyclic ring, having anti-Parkinsonian activity, pharmaceutical formulations containing the active adamantanes and novel 4-protoadamantane spiro oxirane and 1,2-difunctionalized intermediates useful in the preparation of the final products of the invention.

    摘要翻译： 新颖的2-取代-1-甲基氨基金刚烷，其结构式如下：其中X是羟基或卤素，R 1，R 2和R 3是氢或C 1-4烷基，或者R 2和R 3与氮一起形成杂环， 帕金森病活性，含有活性金刚烷的药物制剂和新的4-原金刚烷螺环氧乙烷和可用于制备本发明最终产物的1,2-二官能化中间体。