TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES

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 -D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydro...

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Bibliographic Details
Main Authors VAN HES, ROELOF, TULP, MARTINUS T. M, SMID, PIETER, KRUSE, CORNELIS G
Format Patent
LanguageEnglish
French
German
Published 05.09.2007
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary: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 -D2 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: - R1 is hydrogen, halogen, alkyl (C1-3) or alkoxy(C1-3), CN or CF3, - R2 is hydrogen or alkyl (C1-3), R3 is hydrogen or alkyl (C1-3), - Z is hydrogen or alkyl (C1-3), alkoxy(C1-3) or alkylthio(C1-3), - A is hydrogen or alkyl (C1-3), or - A and Z together form a saturated or (partly) unsaturated 5 - or 6- membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen .
Bibliography:Application Number: EP20050817509