Spirocycloalkyl-substituted azetidinones useful as hypocholesterolemic agents

Abstract

Novel compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 is ##STR2## R.sub.2 and R.sub.3 are independently selected from --CH.sub.2 --, --CH(lower alkyl)--, --C(di-lower alkyl)--, --CH.dbd.CH-- and --C(lower alkyl).dbd.CH--; or R.sub.1 with R.sub.2, or R.sub.1 with R.sub.3, form --CH.dbd.CH-- or --CH.dbd.C(lower alkyl)--; u and v are independently 0-3, provided both are not zero; R.sub.4 is B--(CH.sub.2).sub.m C(O)--; m is 0-5; B--(CH.sub.2).sub.q --; q is 0-6; B--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r ; Z is --O--, --C(O)--, phenylene, --N(R.sub.8)-- or --S(O).sub.0-2 --, e and r is 0-5; the sum of e and r is 0-6; B--(C.sub.2 -C.sub.6 alkenylene)--; B'--(C.sub.4 -C.sub.6 alkadienylene)--; B--(CH.sub.2).sub.t --Z--(C.sub.2 -C.sub.6 alkenylene)--; t is 0-3; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; B--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --; V is cycloalkylene, f is 1-5, g is 0-5; the sum of f and g is 1-6; B--(CH.sub.2).sub.t --V--(C.sub.2 -C.sub.6 alkenylene)-- or B'--(C.sub.2 -C.sub.6 alkenylene)--V--(CH.sub.2).sub.t --; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6, B--(CH.sub.2).sub.a --Z--(CH.sub.2).sub.b --V--(CH.sub.2).sub.d --; a, b and d are 0-6; the sum of a, b and d is 0-6; T--(CH.sub.2).sub.s --; T is cycloalkyl, s is 0-6; or R.sub.1 and R.sub.4 together form ##STR3## B is optionally-substituted phenyl, indanyl, indenyl, naphthyl, tetrahydronaphthyl or optionally substituted-heteroaryl; and R.sub.20 and R.sub.21 are independently optionally-substituted phenyl, optionally-substituted naphthyl, indanyl, indenyl, tetrahydronaphthyl, benzodioxolyl, optionally-substituted heteroaryl, optionally-substituted benzofused heteroaryl or cyclopropyl, pharmaceutical compositions, the use as hypocholesterolemic agents, processes for preparing, and the use in combination with cholesterol biosynthesis inhibitors to treat or prevent athersclerosis.

Dependencies are inferred from the claim text.