This invention relates to compounds which have activity as 5-HT1A
agonists and antagonists which may be useful for the treatment of anxiety, depression,
cognitive deficits, and prostate cancer, having the formula
##STR1##
wherein: X is a moiety selected from the group of:
##STR2##
n is selected from the integers 1 through 5; R1 is optionally substituted
aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole;
R2 is H or alkyl; R3 is H, COR5, COOR5,
and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl,
aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl,
wherein the aryl or heteroaryl groups are optionally substituted; R5 and
R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl,
and noradamantyl or R5 and R6 taken together may form a 5-7
membered azacyclic ring, optionally containing an additional heteroatom selected
from O, S, or NR4; when R5 or R6 are chosen from
cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the
1-position with a C1-C3 alkyl group;
or an optical isomer; or a pharmaceutically acceptable salt thereof.