Neuroactive 3.alpha.-hydroxy-steroids of the androstane and pregnane series
    7.
    发明公开
    Neuroactive 3.alpha.-hydroxy-steroids of the androstane and pregnane series 失效
    Neuroaktive 3.alpha.-Androstan und-Pseudan Steroide

    公开(公告)号:EP1288220A2

    公开(公告)日:2003-03-05

    申请号:EP02025321.7

    申请日:1996-06-06

    摘要: The invention relates to a 3α-hydroxy, 17-(un)substituted derivatives of the androstane series and 3α-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at the recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having general structural formula (I), wherein R, R 1 , R 2 , R 3 ,R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are further defined herein and the dotted lines are single or double bonds. The structure includes androstanes pregnanes (R 4 = methyl), 19-norandrostanes, and norpregnanes (R 4 =H).

    摘要翻译: 本发明涉及雄甾烷基系列的3α-羟基,17-(未)取代的衍生物和孕烷系列的3α-羟基,21-取代衍生物。 这些衍生物能够在最近识别的GRC位点起作用,从而以减轻压力,焦虑,失眠,舒适于GRC活性剂(如抑郁症)和癫痫发作活动的情绪障碍的方式调节脑兴奋性。 本发明的类固醇衍生物是具有通式结构式(I)的那些,其中R,R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8,R 9和R 10在本文中进一步定义,虚线是单或双 债券。 该结构包括雄甾烷孕烷(R 4 =甲基),19-去雄孕烷和诺孕烷(R4 = H)。