发明名称 TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES
摘要 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<SUB>2</SUB> 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<SUB>1</SUB> is hydrogen, halogen, alkyl (C<SUB>1-3</SUB>) or alkoxy(C<SUB>1-3</SUB>), CN or CF<SUB>3</SUB>, - R<SUB>2</SUB> is hydrogen or alkyl (C<SUB>1-3</SUB>), R<SUB>3</SUB> is hydrogen or alkyl (C<SUB>1-3</SUB>), - Z is hydrogen or alkyl (C<SUB>1-3</SUB>), alkoxy(C<SUB>1-3</SUB>) or alkylthio(C<SUB>1-3</SUB>), - A is hydrogen or alkyl (C<SUB>1-3</SUB>), or - A and Z together form a saturated or (partly) unsaturated 5 - or 6- membered ring which may be substituted with halogen, alkyl (C<SUB>1-3</SUB>) or phenyl, in which ring Z represents carbon, sulfur of nitrogen .
申请公布号 EP1828168(A2) 申请公布日期 2007.09.05
申请号 EP20050817509 申请日期 2005.12.06
申请人 SOLVAY PHARMACEUTICALS B.V. 发明人 VAN HES, ROELOF;SMID, PIETER;KRUSE, CORNELIS G.;TULP, MARTINUS T. M.
分类号 C07D401/14 主分类号 C07D401/14
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