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 |
WO2006061373(A3) |
申请公布日期 |
2006.09.21 |
申请号 |
WO2005EP56501 |
申请日期 |
2005.12.06 |
申请人 |
SOLVAY PHARMACEUTICALS B.V.;VAN HES, ROELOF;SMID, PIETER;KRUSE, CORNELIS, G.;TULP, MARTINUS, TH., M. |
发明人 |
VAN HES, ROELOF;SMID, PIETER;KRUSE, CORNELIS, G.;TULP, MARTINUS, TH., M. |
分类号 |
C07D401/14;A61K31/519;A61P25/00;C07D471/04;C07D487/04;C07D513/04 |
主分类号 |
C07D401/14 |
代理机构 |
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地址 |
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