New substituted 4-aminocyclohexanol derivatives, are ORL1 receptor ligands useful e.g. for treating anxiety, depression, epilepsy, Alzheimer's disease, cardiovascular disease or especially pain

摘要

1,4-Disubstituted 4-aminocyclohexanol derivatives (I) are new. Aminocyclohexanol derivatives of formula (I) (including racemates and pure stereoisomers (specifically enantiomers or diastereomers) or their mixtures) and their salts (specifically hydrochlorides) and solvates (specifically hydrates) are new. R1, R2, R5 = H, alkyl or cycloalkyl (both optionally unsaturated and optionally substituted), Ar or -Q-Cyc; or NR1R2 = morpholino, 4-(R5)-piperazino, azetidino, pyrrolidino, piperidino or homopiperidino; Ar = aryl or heteroaryl (both optionally substituted); Q = 1-3C alkylene; Cyc = optionally substituted cycloalkyl or Ar; R3 = alkyl or cycloalkyl (both optionally unsaturated and optionally substituted), Ar or -Q'-Cyc; Q' = optionally unsaturated, optionally substituted 1-4C alkylene; R4 = Cyc, -CHR6(CH2)nR7, -C(Y)(CH2)nR7 or -R8-L-R9; n = 0-3; Y = O, S or H2; R6 = H, or 1-7C alkyl or 1-6C alkoxycarbonyl (both optionally unsaturated and optionally substituted); R7 = H or Cyc; R8 = Ar; L = CONH, NHCO, COO, OCO, O, S or SO2; and R9 = Ar; provided that: alkyl moieties have 1-8C and cycloalkyl moieties 3-8C unless specified otherwise; and R1 and R2 are not both H. An Independent claim is also included for the preparation of (I).