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33 条记录 (耗时 0.052 秒)

    Substituted pyrimidoindoles and diazepinoindoles useful as hypoglycaemics
    23.
    发明授权
    Substituted pyrimidoindoles and diazepinoindoles useful as hypoglycaemics 失效
    用作低血糖的取代的嘧啶并吲哚和二氮茚啶醇

    公开(公告)号：US4783455A

    公开(公告)日：1988-11-08

    申请号：US53444

    申请日：1987-05-22

    申请人： Ian A. Cliffe

    发明人： Ian A. Cliffe

    IPC分类号： C07D487/04 ,  A61K31/505 ,  A61K31/55

    CPC分类号： C07D487/04

    摘要： Compounds of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl or a mono- or bicyclic aryl or heteroaryl radical, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino, X represents--CH.sub.2 CR.sup.3 R.sup.4 CH.sub.2 --or --(CH.sub.2).sub.4 --where R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached represent a 5, 6 or 7 membered carbocyclic ring and R.sup.5 represents acyl and R.sup.6 represents hydrogen or R.sup.5 and R.sup.6 each independently represent hydrogen or lower alkyl, are useful as hypoglycaemics.

    摘要翻译： 式（I）化合物及其药学上可接受的酸加成盐，其中R表示低级烷基或单环或双环芳基或杂芳基，可以相同或不同的R 1和R 2各自表示氢， 羟基，低级烷基，低级烷氧基，卤素（低级）烷基，卤素，氨基或单或二（低级）烷基氨基，X代表-CH 2 CR 3 R 4 CH 2 - 或 - （CH 2）4 - ，其中R 3和R 4各自独立地表示氢或低级烷基 或R 3和R 4与它们所连接的碳原子一起表示5,6或7元的碳环，R 5表示酰基，R 6表示氢或R 5和R 6各自独立地表示氢或低级烷基，可用作低血糖症。

    Nitriles
    24.
    发明授权
    Nitriles 失效
    腈类

    公开(公告)号：US4760158A

    公开(公告)日：1988-07-26

    申请号：US23329

    申请日：1987-03-09

    申请人： Ian A. Cliffe ,  Richard S. Todd

    发明人： Ian A. Cliffe ,  Richard S. Todd

    IPC分类号： C07C255/45 ,  C07D211/62 ,  C07C121/46

    CPC分类号： C07C255/00 ,  C07D211/62

    摘要： Novel 3-halo-2,2-disubstituted propanenitriles of formula ##STR1## wherein Z represents bromo or chloro and A, together with the carbon atom to which it is attached, represents a 5,6 or 7 membered saturated carbocyclic or heterocyclic ring, are useful as intermediates for preparing substituted pyrimido[1,2-a]indoles. The intermediates can be prepared by a novel process which comprises condensing a 2,2-disubstituted ethanenitrile with a dihalomethane in the presence of a non-nucleophilic strong base.

    摘要翻译： 其中Z代表溴或氯并且A与它所连接的碳原子一起表示5,6或7元饱和的碳环或杂环的新的3-卤代-2-二取代的丙烯腈， 可用作制备取代的嘧啶并[1,2-a]吲哚的中间体。 中间体可以通过一种新方法制备，其包括在非亲核性强碱存在下将2,2-二取代的乙腈与二卤代甲烷缩合。

    Piperazine derivatives as 5-HT receptors antagonists
    26.
    发明授权
    Piperazine derivatives as 5-HT receptors antagonists 失效
    哌嗪衍生物作为5-HT受体拮抗剂

    公开(公告)号：US5532242A

    公开(公告)日：1996-07-02

    申请号：US256330

    申请日：1994-07-07

    申请人： Ian A. Cliffe

    发明人： Ian A. Cliffe

    IPC分类号： C07D295/12 ,  A61K31/495 ,  A61P3/04 ,  A61P9/12 ,  A61P25/00 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D295/13 ,  A61K31/505 ,  C07D295/15 ,  C07D401/04

    CPC分类号： C07D295/13 ,  C07C2101/14

    摘要： ##STR1## This invention concerns compounds of formula (I) where A is an alkylene chain of 2 to 5 carbon atoms optionally substituted by one or more lower alkyl groups, R represents hydrogen or one or two same or different lower alkyl groups, R
    1 is a monocyclic aryl or heteroaryl radical, R
    2 is a mono or bicyclic aryl radical and R
    3 is cycloalkyl. The compounds of the invention are useful as antidepressant, antianxiety, or hypotensive agents; or for regulating the sleep/wake cycle, feeding behavior and/or sexual function; and for treating cognition disorders.

    摘要翻译： PCT No.PCT / GB92 / 02399 Sec。 371日期：1994年7月7日 102（e）日期1994年7月7日PCT提交1992年12月24日PCT公布。 公开号WO93 / 14076 （I）本发明涉及式（I）化合物，其中A是任选被一个或多个低级烷基取代的2至5个碳原子的亚烷基链，R表示氢或一个或多个 两个相同或不同的低级烷基，R 1是单环芳基或杂芳基，R 2是单或双环芳基，R 3是环烷基。 本发明的化合物可用作抗抑郁药，抗焦虑剂或降压药剂; 或用于调节睡眠/唤醒周期，进食行为和/或性功能; 并用于治疗认知障碍。

    Azabicyclic derivatives
    28.
    发明授权
    Azabicyclic derivatives 失效
    化学衍生物

    公开(公告)号：US5204470A

    公开(公告)日：1993-04-20

    申请号：US756648

    申请日：1991-09-09

    申请人： Ian A. Cliffe

    发明人： Ian A. Cliffe

    IPC分类号： C07D451/02

    CPC分类号： C07D451/02

    摘要： Azabicyclic compounds of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, ##STR2## is an optionally substituted heteroaryl group containing at least one hetero atom X; n is 2, 3 or 4; m is 1 or 2; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.3-5 -alkenyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl-C.sub.1-2 alkyl or aryl- or heteroaryl-C.sub.1-2 -alkyl; and the --(CH.sub.2).sub.m ##STR3## moiety is ortho to the hetero atom X. The compounds exhibit activity as 5-HT.sub.3 -antagonists and can be used, inter alia, for the treatment of neuropsychiatric disorders.

    摘要翻译： 公开了式（I）的叠氮化合物及其药学上可接受的酸加成盐。 在该式中，是含有至少一个杂原子X的任选取代的杂芳基; n为2,3或4; m为1或2; R 1是氢，C 1-6烷基，C 3-5烯基，C 3-6环烷基，C 3-6环烷基-C 1-2烷基或芳基 - 或杂芳基-C 1-2 - 烷基; 并且 - （CH 2）m部分是杂原子X的邻位。化合物表现出作为5-HT 3拮抗剂的活性，并且可以特别用于治疗神经精神障碍。

    Tertiary alkyl functionalized piperazine derivatives
    30.
    发明授权
    Tertiary alkyl functionalized piperazine derivatives 失效
    叔烷基官能化哌嗪衍生物

    公开(公告)号：US4988814A

    公开(公告)日：1991-01-29

    申请号：US428148

    申请日：1989-10-27

    申请人： Magid A. Abou-Gharbia ,  John P. Yardley ,  Ian A. Cliffe

    发明人： Magid A. Abou-Gharbia ,  John P. Yardley ,  Ian A. Cliffe

    IPC分类号： C07D239/42 ,  C07D295/13 ,  C07D295/15

    CPC分类号： C07D295/13 ,  C07D239/42 ,  C07D295/15

    摘要： Compounds of the formula: ##STR1## in which R.sup.1 is alkyl; R.sup.2 and R.sup.3 are alkyl or taken together they are polymethylene, R.sup.2 and R.sup.3 complete a 5-norbornen-2-yl moiety; X is --CO.sub.2 --, --OCO--, --OCO.sub.2 --, --N(R.sup.7)CO--, --NHNHCO--, --ON(R.sup.7)CO--, --CON(R.sup.7)--, --N(R.sup.7)CO.sub.2 --, --OCON(R.sup.7)-- or --N(R.sup.7)CON(R.sup.8)--, wherein R.sup.7 and R.sup.8 are, independently, hydrogen, alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are halo, alkyl alkoxy, cyano, nitro or perhalomethyl; R.sup.4 is hydrogen or alkyl; R.sup.5 is hydrogen, alkyl, hydroxyalkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are hydroxy, halo, alkyl alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; R.sup.6 is phenyl, benzyl, 2-, 3-, or 4-pyridinyl, 2-pyrimidinyl or 2-pyrazinyl any of which may be substituted by one or more hydroxy, halo, alkyl alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; n is one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof, with the proviso that when X is --CON(R.sup.7)-- and R.sup.7 is alkyl, R.sup.6 is other than 2-pyrimidinyl, and when X is --CO.sub.2 -- and R.sup.1, R.sup.2 and R.sup.3 are methyl and n is 1, R.sup.6 is other than 3,5-di(trifluoromethyl)phenyl are antidepressant and/or anxiolytic agents.