| abstract |
This invention relates to compounds which have activity as 5-HT 1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula n nwherein: X is a moiety selected from the group of:n n nn is selected from the integers 1 through 5; R 1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R 2 is H or alkyl; R 3 is H, COR 5 , COOR 5 , and CONR 5 R 6 ; R 4 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; R 5 and R 6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R 5 and R 6 taken together may form a 5–7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR 4 ; when R 5 or R 6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the 1-position with a C 1 –C 3 alkyl group;n nor an optical isomer; or a pharmaceutically acceptable salt thereof. |