首页> 外国专利> TETRAHYDROPYRIDIN-4-IL INDOLES WITH A COMBINATION OF PROPERTIES-RELATIONSHIPS FOR D2 DOPAMINE RECEPTORS D2 AND SEROTONIN REVERSION CENTERS

TETRAHYDROPYRIDIN-4-IL INDOLES WITH A COMBINATION OF PROPERTIES-RELATIONSHIPS FOR D2 DOPAMINE RECEPTORS D2 AND SEROTONIN REVERSION CENTERS

机译:D2多巴胺受体D2和5-羟色胺活性中心结合特性关系的四氢吲哚-4-IL吲哚

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 -DSUB2/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: - RSUB1/SUB is hydrogen, halogen, alkyl (CSUB1-3/SUB) or alkoxy(CSUB1-3/SUB), CN or CFSUB3/SUB, - RSUB2/SUB is hydrogen or alkyl (CSUB1-3/SUB), RSUB3/SUB is hydrogen or alkyl (CSUB1-3/SUB), - Z is hydrogen or alkyl (CSUB1-3/SUB), alkoxy(CSUB1-3/SUB) or alkylthio(CSUB1-3/SUB), - A is hydrogen or alkyl (CSUB1-3/SUB), or - A and Z together form a saturated or (partly) unsaturated 5 - or 6- membered ring which may be substituted with halogen, alkyl (CSUB1-3/SUB) or phenyl, in which ring Z represents carbon, sulfur of nitrogen .
机译:本发明涉及一组具有双重作用方式的新的四氢吡啶并-4-基吲哚类:5-羟色胺再摄取抑制和对多巴胺-D 2 受体的亲和力,涉及制备这些化合物和方法的方法。用于合成所述四氢吡啶-4-基吲哚的新型中间体。本发明还涉及本文公开的化合物在制备产生有益作用的药物中的用途。本发明涉及式(I)的新颖的四氢吡啶并-4-基吲哚及其互变异构体,立体异构体,前药,N-氧化物,其药理学上可接受的盐,水合物和溶剂化物,其中:-R 1 为氢,卤素,烷基(C 1-3 )或烷氧基(C 1-3 ),CN或CF 3 ,-R 2 是氢或烷基(C 1-3 ),R 3 是氢或烷基(C 1-3 ) ,-Z是氢或烷基(C 1-3 ),烷氧基(C 1-3 )或烷硫基(C 1-3 ) ,-A是氢或烷基(C 1-3 ),或-A和Z一起形成可被卤素,烷基取代的饱和或(部分)不饱和的5-或6-元环(C 1-3 )或苯基,其中环Z表示碳,氮的硫。

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