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    SEROTONIN TRANSPORTER (SERT) INHIBITORS
    3.
    发明公开
    SEROTONIN TRANSPORTER (SERT) INHIBITORS 有权
    羟色胺转运抑制剂（SERT）

    公开(公告)号：EP1957450A1

    公开(公告)日：2008-08-20

    申请号：EP06819656.7

    申请日：2006-11-22

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： GRUNDSCHOBER, Christophe ,  HOFFMANN, Torsten ,  KOBLET, Andreas ,  SCHNIDER, Patrick

    IPC分类号： C07D207/08 ,  C07D207/09 ,  A61K31/40

    CPC分类号： C07D207/08 ,  C07D207/09

    摘要： The present invention relates to cis- derivatives of formula (I) wherein R1 is hydrogen, halogen or lower alkyl; R2/R3 are independently from each other hydrogen, halogen, CN, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; X is -O- or -N(R)-; R is hydrogen or lower alkyl; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.

    SPIRO-PIPERIDINE DERIVATIVES
    5.
    发明公开
    SPIRO-PIPERIDINE DERIVATIVES 有权
    SPIRO-PIPERIDINE衍生物

    公开(公告)号：EP2099799A1

    公开(公告)日：2009-09-16

    申请号：EP07847384.0

    申请日：2007-11-27

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： BISSANTZ, Caterina ,  GRUNDSCHOBER, Christophe ,  MASCIADRI, Raffaello ,  RATNI, Hasane ,  ROGERS-EVANS, Mark ,  SCHNIDER, Patrick

    IPC分类号： C07D471/10 ,  C07D498/10 ,  A61K31/438 ,  A61P9/02

    CPC分类号： C07D471/10 ,  C07D498/10

    摘要： Present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general Formula (I) wherein R1 to R11 and X are as defined in the description.

    摘要翻译： 本发明涉及作为V1a受体拮抗剂的新吲哚-2-基 - 羰基 - 螺 - 哌啶衍生物，它们的制造方法，含有它们的药物组合物以及它们作为药物的用途。 本发明的活性化合物可用于预防和/或治疗焦虑症和抑郁症以及其他疾病。 本发明化合物具有通式（I），其中R 1至R 11和X如说明书中所定义。

    SEROTONIN TRANSPORTER (SERT) INHIBITORS
    6.
    发明授权
    SEROTONIN TRANSPORTER (SERT) INHIBITORS 有权
    羟色胺转运抑制剂（SERT）

    公开(公告)号：EP1957450B1

    公开(公告)日：2009-06-24

    申请号：EP06819656.7

    申请日：2006-11-22

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： GRUNDSCHOBER, Christophe ,  HOFFMANN, Torsten ,  KOBLET, Andreas ,  SCHNIDER, Patrick

    IPC分类号： C07D207/08 ,  C07D207/09 ,  A61K31/40

    CPC分类号： C07D207/08 ,  C07D207/09

    摘要： The present invention relates to cis- derivatives of formula (I) wherein R1 is hydrogen, halogen or lower alkyl; R2/R3 are independently from each other hydrogen, halogen, CN, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; X is -O- or -N(R)-; R is hydrogen or lower alkyl; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.