DERIVATIVES OF PYRIDINALKYL-AMINOALKYL-1H-INDOLE INHIBITING RECEPTORS 5-HT AND RECAPTURE OF SEROTONIN WHICH CAN BE USED AS ANTIDEPRESSANT AND ANXIOLYTIC

摘要

The invention relates to a compound of formula I (see formula I)in which X denotes (see formula II); Y denotes H or A'; R1 denotes CN or F;R2 denotes H, A, Hal, OH, OA, SA, COOH, COOA', CHO, COA', SO2A', NH2, NHA,NA2, CH2NA2, NHCOA, NHCOAr, NHCOOA, NHSO2A, NHSO2Ar, CH2NHSO2A,NHCONH2, NHCONHA, NHCONA2, NHCONHAr, CONH2, CONHA, CONA2,SO2NH2, SO2NHA, SO2NA2, CH2SO2NH2, CH2SO2NHA, CH2SO2NA2, [C(R4R4')]p CN,[C(R4R4')]p CF3, [C(R4R4')]p COR4, [C(R4R4')]p Ar, -O-[C(R4R4')]p Ar or[C(R4R4')]p Het;R3 denotes H, A, [C(R4R4')]p Ar or [C(R4R4')]p Het, Hal or CN; R2 and R3together alsodenote -CH=CH-CH=CH-, -CH=CH-CH2-CH2- or -CH2-CH2-CH=CH-, in which 1 or 2CH and/or CH2 units may be replaced by N and/or 1, 2, 3 or 4 H atoms may besubstituted by other radicals; R4, R4' each, independently of one another,denote H, A,OH, OA, NH2, NHA, NA2 or NHCOOA'; Ar denotes substituted or unsubstitutedphenyl, naphthyl or biphenyl; Het denotes a substituted or unsubstituted, mono-orbicyclic saturated, unsaturated or aromatic heterocycle; A denotes unbranchedorbranched alkyl having 1-10 C atoms, in which one or two CH2 groups may bereplaced by -CH=CH- groups and/or 1-7 H atoms may also be replaced by F and/orCl; A' denotes alkyl having 1 to 6 C atoms or benzyl; Hal denotes F, Cl, Br orI;m denotes 2, 3, 4, 5 or 6; n denotes 1, 2, 3 or 4; o denotes 0, 1 or 2; and pdenotes 0,1, 2, 3, 4, 5 or 6; or a pharmaceutically usable salt, solvate or stereoisomerthereof,or a mixture thereof in any ratio. Said compound exhibits a high affinity withrespectto the receptors 5-HT1A and a partial affinity with respect to the receptors 5-HT1D.The compound inhibits the recapture of serotonin, exhibits agonistic andantagonisticproperties with respect to said serotonin and can be used as antidepressantandanxiolitic and for curing a neurogenerative disorder.