6-(HYDRONAPHTYL-1-ETHYL)-4-HYDROXY-3,4,5,6-TETRAHYDRO-2H-PYRAN-2-ONES AND THE CORRESPONDING HYDROXY ACIDS

摘要

Compounds of either of general formulae (I) and (II), wherein: R<1> represents a C1-8 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-8)alkyl, C2-8 alkenyl, or C1-6 alkyl substituted phenyl group; R<2> represents a C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl group or a C1-5 alkyl, C2-5 alkenyl, or C2-5 alkynyl group substituted with a substituted phenyl group; R<3> represents a hydrogen atom or a substituent R<4> or M; R<4> represents a C1-5 alkyl group, or a C1-5 alkyl group substituted with a group chosen from substituted phenyl, dimethylamino and acetylamino; R<5> represents a hydrogen atom or a methyl or ethyl group, except that when R<2> is methyl then R<5> 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 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 hypercholesterolaemia in general and arteriosclerosis, familiar hypercholesterolaemia or hyperlipidaemia in particular.