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US 4,736,064 AGranted
Prodrugs of antihypercholesterolemic compounds
AssigneeMerck & Co., Inc.
InventorsJohn J. Baldwin, Wasyl Halczenko, George Hartman
Life of this patent
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Abstract
Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## and pharmaceutically acceptable salts thereof are disclosed.
Claims10
A compound represented by the general structural formula (I):
- ##STR19## wherein:
- n is 1 to 6;
- R is selected from a group consisting of:
- ##STR20## wherein:
- m is 1 to 5;
- R.sup.1 is hydrogen or methyl;
- A is ##STR21## in which R.sup.2 is hydrogen or hydroxyl;
- B is ##STR22## in which R.sup.3 is hydrogen or hydroxyl;
- a, b, c and d represent single bonds, one of a, b, c and d represents a double bond or both a and c or both b and d represent double bonds, provided that when a is a double bond, A is ##STR23## and when d is a double bond, B is ##STR24## or ##STR25## wherein:
- E is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;
- R.sup.4 and R.sup.5 are independently C.sub.1-3 alkyl, fluoro, bromo or chloro;
- and
- R.sup.6 is phenyl, benzyloxy, substituted phenyl or substituted benzyloxy in which the phenyl group in each case is substituted with one or more substituents selected from C.sub.1-3 alkyl, hydroxy-C.sub.1-3 alkyl fluoro, bromo or chloro;
- R.sup.7 is hydrogen or C.sub.1-8 alkyl;
- R.sup.9 and R.sup.10 independently are hydrogen or C.sub.1-8 alkyl or when taken together with the nitrogen atom to which they are attached form a heterocycle selected from the group consisting of piperidinyl, pyrrolidinyl, or morpholinyl;
- or a pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.