EP0508425A1 — Bicyclic amides as inhibitors of acyl-coenzyme a: cholesterol acyl transferase

USPTO Abstract

Novel bicyclic amides of the formula wherein Ar¹ and Ar² are phenyl, R²-substituted phenyl, heteroaryl or R²-substituted heteroaryl, wherein R² is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;    X, Y and Z are -CH₂-, -CH(alkyl)-, -C(alkyl)₂-, -NH-, -N(alkyl)-, -O- or SO r , wherein r is 0, 1 or 2, and m, n and p are 0 or 1;    R¹ is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain -O-, -SO r , phenylene, R²-substituted phenylene, heteroarylene or R²-substituted heteroarylene groups; an interrupted alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain of 4 to 25 carbon atoms, interrupted by one or more -NH-, -C(O)- or -N(lower alkyl)- groups; an interrupted alkyl chain of 4 to 25 carbon atoms substituted by one or more phenyl, R²-substituted phenyl, heteroaryl or R²-substituted heteroaryl groups; a diphenylamino group; a di-(R²-substituted phenyl)amino group; a diheteroarylamino group; or a di-(R²-substituted heteroaryl)amino group;    or a pharmaceutically acceptable salt thereof, useful in the treatment of artherosclerosis are disclosed.