SPIROCYCLOALKYL-SUBSTITUTED AZETIDINONES USEFUL AS HYPOCHOLESTEROLEMIC AGENTS.

摘要

Novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 is R2 and R3 are independently selected from -CH2-, -CH(lower alkyl)-, -C(di-lower alkyl)-, -CH=CH- and -C(lower alkyl)=CH-; or R1 with R2, or R1 with R3, form -CH=CH- or -CH=C(lower alkyl)-; u and v are independently 0-3, provided both are not zero; R4 is B-(CH2)mC(O)-; m is 0-5; B-(CH2)q-; q is 0-6; B-(CH2)e-Z-(CH2)r; Z is -O-, -C(O)-, phenylene, -N(R8)- or -S(O)0-2-, e and r is 0-5; the sum of e and r is 0-6; B-(C2-C6 alkenylene)-; B'-(C4-C6 alkadienylene)-; B-(CH2)t-Z-(C2-C6 alkenylene)-; t is 0-3; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; B-(CH2)f-V-(CH2)g-; V is cycloalkylene, f is 1-5, g is 0-5; the sum of f and g is 1-6; B-(CH2)t-V-(C2-C6 alkenylene)- or B'-(C2-C6 alkenylene)-V-(CH2)t-; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6, B-(CH2)a-Z-(CH2)b-V-(CH2)d-; a, b and d are 0-6; the sum of a, b and d is 0-6; T-(CH2)s-; T is cycloalkyl, s is 0-6; or R1 and R4 together form B is optionally-substituted phenyl, indanyl, indenyl, naphthyl, tetrahydronaphthyl or optionally substituted-heteroaryl; and R20 and R21 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.