Use of new and known amine compounds for stimulating neuronal activity for treating e.g. Alzheimer's and Parkinson's disease, neuralgias and multiple sclerosis

摘要

Use of new and known amine compounds (I) is claimed for stimulating neuronal activity. Use of new and known amine compounds (I) and their salts is claimed for stimulating neuronal activity. X = S, SO, SO2, NH, or NR5; Y = SO2, COCO, CONH, CSNH, COCOO, COCONH, COO, or SO2NH, CO or a bond; R1 = H, Ar, or 1-7C alkyl, 2-7C alkenyl, 3-7C cycloalkyl, or 5-7C cycloalkenyl (all optionally substituted by Ar or E); R2 = 1-6C alkyl (optionally substituted by phenyl or halophenyl); R3 = 1-6C alkyl, 2-6C alkenyl, 3-7C cycloalkyl, 5-7C cycloalkenyl, or cyclohexylmethyl (all optionally substituted by 1 or 2 Ar), or NR2R3 = 5-7 membered heterocyclyl (optionally substituted by 1-4C alkyl or hydroxy); R4, R5 = Ar, 1-9C alkyl, haloalkyl, or 2-9C alkenyl (all optionally substituted by 1 or 2 Ar, 3-7C cycloalkyl, or 5-7C cycloalkenyl); Ar = 6-12C mono- or bi- cyclic aryl or partially hydrogenated aryl (optionally containing 1-4 N, S or O heteroatoms and optionally substituted by 1-3 E) and E = halo, OH, nitro, cyano, CF3, OCF3, amino, phenyl, methylenedioxy, phenoxy, benzyloxy, 1-4C alkyl or 1-4C alkoxy. An Independent claim is included for new compounds (I), provided that: (a) when Y is SO2, R1 is not H; (b) Y is not CO or a bond; (c) when X = NR5 and YR1 = tosyl, then R2-R5 are not all methyl; (d) when X = SO, Y = CONH, R1 and R2 = benzyl, and R3 = vinyl, then R4 is not n-butyl; (e) when X = NR5 and YR1 = tosyl, and NR2R3 together = 6-7 membered saturated azacyclyl, R4 and R5 are not both n-propyl and (f) when X = NR5, Y = CSNH, R1 = p-tolyl, and R3 = phenyl, then R2, R4 and R5 are not all methyl. Independent claims are included for the preparation of (I).