abstract |
PCT No. PCT/GB90/01030 Sec. 371 Date Oct. 15, 1991 Sec. 102(e) Date Oct. 15, 1991 PCT Filed Jul. 4, 1990 PCT Pub. No. WO91/00280 PCT Pub. Date Jan. 10, 1991.Compounds of either of general formulae (I) and (II), wherein: R1 represents a C1-8 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-8)alkyl, C2-8 alkenyl, or C1-6 alkyl substituted phenyl group; R2 represents a C1-8 alkyl, C2-8 alkenyl, C2-8alkynyl group or a C1-5 alkyl, C2-5 alkenyl or C2-5 alkynyl group substituted with a substituted phenyl group; R3 represents a hydrogen atom or a substituent R4 or M; R4 represents a C1-5 alkyl group, or C1-5 alkyl group substituted with a group chosen from substituted phenyl, dimethylamino and acetylamino; R5 represents a hydrogen atom or a methyl or ethyl group except that when R2 is methyl then R5 is not methyl; M represents a cation capable of forming a pharmaceutically acceptable salt; Q represents C=O or CHOH; and each of a, b, c, and d, is independently a single or double bond except that when a and c are double bonds then b is a single bond; are inhibitors of the enzyme 24 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate limiting enzyme in the biosynthesis of cholesterol in mammals including man, and as such are useful in the treatment of hypercholesterolemia in general and arteriosclerosis, familiar hypercholesterolemia or hyperlipidemia in particular. |