Pharmacologically active 2-hydroxy-4-(substituted) phenyl cycloalkanes and derivatives thereof

摘要

Compounds having the formula <IMAGE> <IMAGE> +TR <IMAGE> R1 is hydrogen, benzyl or an ester moiety; Y is -CH(R2'')CH(R2)- or -CH(R3)CH2-; R2'' is hydrogen or methyl; R2 is OH or X-substituted (C1-16) alkyl; R3 is OH, cyano or X-substituted (C1-3) alkyl; X is -OR6, -SR6, -S(O)R6, -S(O)2R6, -NR6R7, -COOR7, -CONR7R8 or oxo; with the proviso that when X is -NR6R7, -COOR7 or -CONR7R8, said group is located on the terminal carbon atom of R2 or R3; R6 is hydrogen, (C1-6) alkyl or acetyl; each of R7 and R8 is hydrogen or (C1-6) alkyl; s is an integer of 1 or 2; with the proviso that when R6 is acetyl, R7 is hydrogen and X is other than S(O)R6 or S(O)2R6; z-w is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain, and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.