New 4-(alkyl, alkenyl or alkynyl)-cyclohexylamine derivatives, are ORL1 receptor ligands useful e.g. for treating anxiety, depression, epilepsy, senile dementia, withdrawal symptoms or especially pain

摘要

1-Substituted 4-(omega-substituted alkyl, alkenyl or alkynyl)-cyclohexylamine derivatives (I) are new. Cyclohexylamine derivatives of formula (I), optionally in the form of racemates, pure stereoisomers (especially enantiomers or diastereomers) or their mixtures in all proportions, including free bases, free acids, salts (specifically acid or base addition salt) or solvates (specifically hydrates), are new. ----- = optional bond; R1, R2 = H, Alk, Cyc, Ar, Het, -Q1-Ar, -Q1-Cyc' or -Q1-Het; or NR1R2 = morpholino, 4-(R6)-piperazino, azetidino, pyrrolidino, piperidino or homopiperidino; Alk = optionally unsaturated, optionally mono- or polysubstituted 1-8C alkyl; Cyc = optionally unsaturated, optionally mono- or polysubstituted 3-8C cycloalkyl; Cyc' = optionally mono- or polysubstituted 3-8C cycloalkyl; Ar = optionally mono- or polysubstituted aryl; Het = optionally mono- or polysubstituted heteroaryl; Q1 = 1-3C alkylene; R6 = as for R1; R3 = Alk, Cyc, Ar, Het, -Q2-Ar, -Q2-Cyc' or -Q2-Het ; Q2 = optionally unsaturated, optionally substituted 1-4C alkylene; R4 = H or optionally protected hydroxy; n = 0 or 1; R5 = Cyc', Ar, Het, -CH2R12, -(CH2)2R12 or -(CH2)3R12; R12 = Cyc', Ar or Het. Independent claims are also included for the preparation of (I).