4-SUBSTITUTED PIPERIDINE ANALOGS AND THEIR USE AS SUBTYPE SELECTIVE NMDA RECEPTOR ANTAGONISTS

摘要

4-Substituted piperidine analogues of formula (I) and their salts are new. Ar1, Ar2 = aryl or heteroaryl, both optionally substituted by H, OH, alkyl, halo, NO2, aryl, aralkyl, amino, haloalkyl, NHAc, NHSO2Me, N(SO2Me)2, CONHalkyl, SO2NH2, alkylguanidine, lower alkylamino or lower alkoxy; z = single or double bond; X = (CHR2)m, O, S or NR3; R2 = H, OH, lower alkoxy or 1-6C alkyl; m = 0-2; R3 = H or 1-6C alkyl; provided that when z = a double bond then X = (CHR2)m; R1 = H or OH; n = 0-2; Q = CH=CH or -C?=C-; R4 = H or OH when z = a single bond; provided that (i) when n = 0 then z is double and R4 is absent; (ii) when n = 1 or 2 and Q = -C?=C- and z is double or R4 = OH then Ar1 = halo-aryl; and (iii) when R4 = OH then R2 is not OH or lower alkoxy. Also claimed are compounds of formulae (II)-(VII) and their salts; with the proviso that: in (II) and (III), when Q = -C?=C- then Ar1 = haloaryl. X1 = O or S. Compounds of formula (VIII) are also new.