4-SUBSTITUTED PIPERIDINECARBOXYLIC ACID ESTERS: INHIBITION OF CHOLESTEROL ABSORPTION

摘要

The invention concerns a compound of formula (I) in which R1 is H, C¿1?-C20 alkyl, C3-C20 alkenyl, C3-C8 cycloalkyl, cycloalkylalkyl where the cycloalkyl moiety has from 3 to 8 carbon atoms and the alkyl moiety has from 1 to 6 carbon atoms, phenyl, phenyl substituted by C1-C6 alkyl, C1-C6 alkoxy, halo, nitro, cyano or trifluoromethyl; phenylalkyl where the alkyl moiety has from 1 to 20 carbons, or phenylalkyl where the phenyl group is substituted by C1-C6 alkyl, C1-C6 alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R?2¿ is H or C¿1?-C6 alkyl; or R?1 and R2¿ taken together with the interposed nitrogen forms a heterocyclic group of formula (a) where n is one of the integers 0, 1 or 2; X is -O-, -S-, or (b) and R7 is H, hydroxy, C¿1?-C6 alkyl, C2-C6 alkanoyloxy, C1-C6 hydroxyalkyl, carboxyl, C1-C16 alkoxycarbonyl, phenyl or phenyl substituted with C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 perhaloalkyl, halo, nitro or cyano; R?8¿ is H or C¿1?-C6 alkyl or R?7 and R8¿ taken together with the intervening carbon atom forms a polymethylene ring of 3 to 7 carbon atoms; R9 is H, C¿1?-C6 alkyl or C2-C12 gemdialkyl; and R?3, R4, R5 and R6¿ are H, C¿1-C?6 alkyl, C¿1?-C6 alkoxy, halo, nitro, cyano, C1-C6 perhaloalkyl, C1-C16 alkoxycarbonyl, or carboxyl. The compounds inhibit cholesterol absorption, thus lowering serum cholesterol levels. Pharmaceutical compositions containing the compounds are also covered as are processes for preparing the compounds.