Antihypercholesterolemic compounds
AssigneeMerck & Co., Inc.
InventorsWilliam F. Hoffman, Robert L. Smith, Alvin K. Willard
Life of this patent
Estimating the term…
Abstract
6(R)-[2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen)-polyhydronaphthyl-1')-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H- pyran-2-ones are prepared by acylation of the corresponding 8'-hydroxy compounds. The products are strong inhibitors of the biosynthesis of cholesterol.
Claims9
A compound of the formula:
- ##STR81## wherein R' is H or CH.sub.3 ;
- R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl,
- the dotted lines at X, Y and Z represent possible double bonds, said double bonds, when any are present, being either X and Z in combination or X, Y or Z alone;
- or
- the corresponding dihydroxy acid of the formula:
- ##STR82## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester or .alpha.-monoglyceride of said acid.
A pharmaceutical antihypercholesterolemic composition comprising a pharmaceutical carrier and an antihypercholesterolemic effective amount of a compound of structural formula:
- ##STR83## in which R' is H, or CH.sub.3 ;
- R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl,
- the dotted lines at X, Y and Z represent possible double bonds, said double bonds, when any are present, being either X and Z in combination or X, Y or Z alone;
- or
- the corresponding dihydroxy acid of the formula:
- ##STR84## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester or .alpha.-monoglyceride of said acid.
A method of treating hypercholesterolemia in a patient in need of such treatment which comprises administration of an antihyperchloesterolemic effective amount of a compound of structural formula:
- ##STR85## wherein R' is H or CH.sub.3 ;
- R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl,
- the dotted lines at X, Y and Z represent possible double bonds, said double bonds, when any are present, being either X and Z in combination or X, Y or Z alone;
- or
- the corresponding dihydroxy acid of the formula:
- ##STR86## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester or .alpha.-monoglyceride of said acid.
Dependencies are inferred from the claim text.