Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents

Abstract

Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein:Arand Arare aryl or R-substituted aryl;Aris aryl or R-substituted aryl;X, Y and Z are —CH—, —CH(lower alkyl)— or —C(dilower alkyl)—;R and Rare —OR, —O(CO)R, —O(CO)ORor —O(CO)NRR;Rand Rare H or lower alkyl;q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5;Ris selected from lower alkyl, R, —CF, —CN, —NOand halogen Ris selected from —OR, —O(CO)R, —O(CO)OR, —O(CH)OR, —O(CO)NRR, —NRR, —NR(CO)R, —NR(CO)OR, —NR(CO)NRR, —NRSOR, —COOR, —CONRR, —COR, —SONRR, S(O)R, —O(CH)—COOR, —O(CH)CONR, —(lower alkylene)COORand —CH═CH—COOR;R, Rand Rare H, lower alkyl or aryl-substituted IcRis lower alkyl, aryl or aryl-substituted lower alkyl;are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.