Treatment of CNS disorders with 4,5,6,7-tetrahydro-1H-imidazo (4,5-)-pyridines and analogs

Claim 1

A compound of the formula: ##STR15## or a pharmaceutically acceptable salt thereof; wherein (1) R 1 is: (a) H, (b) halo, (c) C 1 -C 6 alkyl, or C 3 -C 6 alkenyl or alkynyl, (d) R 14 --(CH 2 ) x --wherein x is one, two, three, four or five, and R 14 is C 3 -C 8 cycloalky,, naphthyl, [heteroaryl,] 2-, 3-, or 4-pyridyl; 1-, 2-, or 4-imidazolyl; 1-, 2-, 3-, 4-, 5-, 6-or 7-indolyl; 2-,or 3-pyraxolyl, phenyl unsubstituted or substituted with from one through five substituents comprising C 1 -C 4 alkyl, halo, trifluoromethyl, hydroxy, C 1 -C 4 akloxy, lower acyloxy, amino, N-lower monoalkylamino, N,N-lower dialkylamino, lower thioalkyl, lower alkylsulfonyl, nitro or --NHCOR 10 wherein R 10 is lower alkyl, phenyl unsubstituted or substituted with lower alkyl, or --NHR 11 wherein R 11 is H or C 1 -C 4 alkyl, (e) ##STR16## wherein R 14 is independently as defined above, or (f) R 14 --CH(OH)--wherein R 14 is independently as defined above; (2) R 2 is (a) --(CH 2 ) x OR 7 wherein R 7 is H, C 1 -C 4 aklyl, C 1 -C 4 acyl, C 3 --C 6 cycloalkyl, phenyl, or bensyl, (b) --(CH 2 ) x NR 7 R 8 wherein R 7 is independently as defined above and R 8 is H, C 1 -C 4 alkyl, phenyl, benzyl, or C 1 -C 4 acyl, (c) --(CH 2 ) x OC 5 H 11 , (d) --CHO (e) --CN, (f) --COOR 9 wherein R 9 is hydrogen, C 1 -C 4 alkyl or benzyl; unsubstituted or substituted with from one through five substituents, comprising alkyl, halo, trifluoromethyl, amino, N-lower monoaklylamino, N,N-lower dialkylamino, lower thioaklyl, lower alkylsulfonyul, OH, or C 1 -C 4 alkoxy, or nitro. (iii) --(CH=CR 12 )--R 16 , is hydrogen or lower alkyl and R 16 is (a) alkyl of from four to twenty carbons, inclusive, ##STR17## (b) wherein y, R 14 and R 15 are, independently, as defined above, and (iv) R 14 (CH 2 ) y R 14 and R 12 are, independently, as defined above, (v) R 14 --(CH 2 ) y --O--wherein y and R 14 are independently as defined above, (vi) ##STR18## wherein R 14 , R 15 , and y are independently as defined above, (d) SO 2 R 5 wherein R 5 is, independently, as defined above; (4) R 4 is --CO 2 H, --NHSO 2 CF 3 , or ##STR19##