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US 5,474,993 AGranted
Lactam inhibitors of cholesterol esterase
AssigneeSterling Winthrop Inc.
InventorsByron Rubin, Kenneth C. Mattes, Terrence C. Mungal
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Abstract
The present invention is related to compounds which inhibit pancreatic cholesterol esterase. The compounds have the formula: ##STR1## wherein R.sup.1 is H or C.sub.1-6 alkyl; R.sup.2 is H or C.sub.1-6 alkyl; R.sup.3 is H or C.sub.1-6 alkyl; X is CHR.sup.6, S or O; R.sup.6 is H or C.sub.1-6 alkyl; R.sup.4 is a hydrophobic moiety; and pharmaceutically acceptable salts thereof.
Claims12
A compound of the formula:
- ##STR13## wherein R.sub.1 is H or C.sub.1-3 alkyl;
- R.sub.2 is H or C.sub.1-3 alkyl;
- R.sub.3 is H or C.sub.1-3 alkyl;
- Y is a chemical bond ##STR14## wherein R.sub.5 is C.sub.1-3 alkyl;
- Z is C.sub.1-6 alkyl, C.sub.3-8 cyclo alkyl, phenyl phenyl C.sub.1-6 alkyl, phenyloxy C.sub.1-6 alkyl, bicyclic aryl, fused cyclo C.sub.3-8 alkyl phenyl, fused phenyl cyclo C.sub.3-8 alkyl, tricyclic aryl, phenoxyphenyl, or ##STR15## wherein each Z.sup.1 is phenyl or bicyclic aryl, and wherein any of the ring structures can be mono- or di-substituted with
- C.sub.1-3 alkyl or C.sub.3-8 cyclo alkyl;
- and a pharmaceutically acceptable salt thereof.
4 more elements
Dependencies are inferred from the claim text.