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    Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites
    1.
    发明专利
    Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 未知

    公开(公告)号：ZA200704155B

    公开(公告)日：2008-08-27

    申请号：ZA200704155

    申请日：2007-05-22

    Applicant: SOLVAY PHARM BV

    Inventor： ROELOF VAN HES ,  KRUSE CORNELIS G ,  PIETER SMID ,  TULP MARTINUS TH M

    IPC: A61K20090101 ,  A61P20090101 ,  C07D20090101

    Abstract: The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine -D 2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin -4-yl indoles of the formula (I) and tautomers, stereoisomers, prodrugs, N -oxides, pharmacologically acceptable salts, hydrates and solvates thereof , wherein: - R 1 is hydrogen, halogen, alkyl (C 1-3 ) or alkoxy(C 1-3 ), CN or CF 3 , - R 2 is hydrogen or alkyl (C 1-3 ), R 3 is hydrogen or alkyl (C 1-3 ), - Z is hydrogen or alkyl (C 1-3 ), alkoxy(C 1-3 ) or alkylthio(C 1-3 ), - A is hydrogen or alkyl (C 1-3 ), or - A and Z together form a saturated or (partly) unsaturated 5 - or 6- membered ring which may be substituted with halogen, alkyl (C 1-3 ) or phenyl, in which ring Z represents carbon, sulfur of nitrogen .

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