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    Propanobicyclic amine derivatives for CNS disorders
    1.
    发明公开
    Propanobicyclic amine derivatives for CNS disorders 失效
    Propanbicyclische aminderivatefürZNSFunktionsstörungen。

    公开(公告)号：EP0449301A1

    公开(公告)日：1991-10-02

    申请号：EP91105041.7

    申请日：1991-03-28

    申请人： G.D. Searle & Co.

    发明人： Gray, Nancy M. ,  Cheng, Brian K.

    IPC分类号： C07D295/033 ,  C07D295/096 ,  C07C211/38 ,  C07C211/42 ,  A61K31/135 ,  A61K31/495

    CPC分类号： C07D295/088 ,  C07C211/42 ,  C07C2603/78 ,  C07D295/03 ,  C07D295/033

    摘要： Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula


    wherein each of R 1 , R 2 , R 3 , R 4 , Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R 3 and R 4 may be taken together to form oxo;
    wherein each of R 9 , R 10 , R", R 12 , R 13 and R 14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from

    wherein R 15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R 16 and R17 is independently selected from hydrido, hydroxy, alkyl, phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive, with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R 3 , R 4 , ring-position two, ring-position three and ring-position four; or the pharmaceutically-acceptable salts thereof.

    摘要翻译： 描述了某些丙三醇胺化合物用于治疗中枢神经系统疾病如精神病，抽搐，肌张力障碍和脑缺血。 特别感兴趣的化合物具有式CHEM，其中R 1，R 2，R 3，R 4，Y和Z各自独立地选自氢，羟基，烷基，环烷基，环烷基烷基 ，苯烷基，苯基，烷氧基，苯氧基，苯烷氧基，烷氧基烷基，卤素，卤代烷基和羟烷基; 其中R 3和R 4可以一起形成氧代; 其中R 9，R 1，R 1，R 1，R 2，R 3和R 4各自独立地选自 烷基，环烷基，羟基烷基，氟烷基，环烷基烷基，烷氧基烷基，苯烷基和苯基; 其中含氮环杂环部分中的G选自CHEM，其中R 1 5选自氢化，烷基，环烷基，环烷基烷基，苯基，苯烷基，烷氧基烷基和羟烷基; 其中R 1和R 6各自独立地选自氢，羟基，烷基，苯烷基，苯基，烷氧基，氟烷基和氟; 其中m是一个或两个; 其中p是选自0至4的数字（包括端值）; 其中q和r各自独立地选自一至三个，其中q和r之和是三至六的数，包括端值在内; 进一步的条件是含氮环杂环部分必须连接在选自R 3，R 4，环位2，环3位和环4位的一个位置上; 或其药学上可接受的盐。