Novel HMG-CoA reductase inhibitors
AssigneeRorer Pharmaceutical Corporation
InventorsKent W. Neuenschwander, Anthony C. Scotese
Life of this patent
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Abstract
Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids and esters derived therefrom and pharmaceutically acceptable salts thereof. Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.
Claims21
A compound of the formula ##STR21## wherein Y is:
- --CHR--,
- --CHRCHR--,
- --CHRCHRCHR--, or
- --RC.dbd.CR--, wherein R is H or lower alkyl;
- X, X.sub.1 and X.sub.2 are independently:
- H,
- F,
- Cl,
- Br,
- OH,
- CF.sub.3,
- alkyl, or
- alkoxy;
- R.sub.1 is:
- H,
- alkyl,
- substituted alkyl,
- CF.sub.3,
- aryl, or
- substituted aryl;
- m is:
- 0, 1, 2 or 3;
- and
- n is:
- 0 or 1.
Trans-(E)-6-[2-[2-(4-fluoro-3-methylphenyl)-4-phenyl-spiro -[4.4]nona-1,3-dien-1-yl]ethenyl]-3,4,5,6-tetrahydro-2H-pyran-2-one.
Trans-(E)-6-[2-[7,9-di-(4-fluorophenyl)-spiro[4.5]deca-6,8-dien- 6-yl]ethenyl]-3,4,5,6-tetrahydro-2H-pyran-2-one.
Trans-(E)-6-[2-[2-(4-fluorophenyl)-4-(4-hydr oxymethylphenyl)spiro[4.5]deca-1,3-dien-1-yl]ethenyl]-3,4,5,6-tetrahydro-2H -pyran-2-one.
Trans-(E) -6-[2-[5-(4-fluorophenyl)-7-(2-hydroxyprop-2-yl)-spiro[2.4]hepta-4,6-dien-4 -yl]ethenyl]-3,4,5,6-tetrahydro-2H-pyran-2-one.
Trans-(E)-6-[2-[2-(4-fluorophenyl)-4-phenyl -spiro[4.4]nona-1,3-dien-1-yl]ethenyl]-3,4,5,6-tetrahydro-2H-pyran-2-one.
Dependencies are inferred from the claim text.