abstract |
A series of aryl piperazine compounds are effectivenpharmaceuticals for the treatment of conditions related tonor affected by the serotonin 1 A receptor; the compounds arenparticularly effective antagonists at that receptor, and arenparticularly useful for alleviating the symptoms of nicotinenand tobacco withdrawal. The compounds are of the formulan nwhereinn Ar' is a mono or bicyclic aryl or heteroaryl radicalnsubstituted with one to three substituents selected from thengroup consisting of hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy,n(C 1 -C 6 )alkylthio, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl,n(C 1 -C 6 )alkylhalo, (C 3 -C 8 )cycloalkyl, (C 3 -C 8 )cycloalkenyl ornhalo; R 1 is hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy,n(C 1 -C 6 )alkylthio; R 2 is phenyl, naphthyl or (C 3 -C 12 )cycloalkylnsubstituted with one or two substituents selected from thengroup consisting of hydrogen (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy,n(C 1 -C 6 )alkylthio, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl,n(C 1 -C 6 )alkylhalo, (C 3 -C 8 )cycloalkyl, (C 3 -C 8 )cycloalkenyl ornhalo; R 3 is selected from the group consisting of hydrogen,n(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )alkylthio,n(C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, (C 1 -C 6 )alkylhalo,n(C 3 -C 8 )cycloalkyl, (C 3 -C 8 )cycloalkenyl or halo; X is -(C=O)-, -CHOH- or -CH 2 -; nor a pharmaceutically acceptable salt racemate, opticalnisomer or solvate thereof. |