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US 4,789,682 AGranted
Antihypercholesterolemic compounds
AssigneeMerck & Co., Inc.
InventorGerald E. Stokker
Life of this patent
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Abstract
Novel antihypercholesterolemic compounds of structure (I) or (II), ##STR1## pharmaceutically acceptable salts, thereof and a novel process for preparing compounds of structure I, are disclosed.
Claims8
A compound of structural formula (I) or (II):
- ##STR12## wherein Z is phenyl, naphthyl, thiophenyl, pyrryl;
- or phenyl, naphthyl, thiophenyl, pyrryl substituted with a group A;
- A is selected from a group consisting of:
- Cl, F, OH,
- C.sub.1-5 alkyl,
- C.sub.1-5 alkyloxy,
- C.sub.2-8 alkanoyloxy,
- C.sub.2-6 alkanolylamino,
- C.sub.1-5 alkyloxycarbonyl,
- phenyl,
- hydroxy-C.sub.1-5 alkyl,
- trifluromethyl-C.sub.2-8 alkanoylamino;
- E is a direct bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --
- R.sub.1, R.sub.2, R.sub.3 are each selected from:
- H, Cl, or F,
- C.sub.1-4 alkyl,
- C.sub.1-4 chloroalkyl or C.sub.1-4 fluoroalkyl,
- phenyl,
- phenyl substituted by Cl or F,
- C.sub.1-4 alkyloxy,
- C.sub.2-8 alkanoyloxy,
- C.sub.2-8 alkanoyloxy-C.sub.1-5 alkyl, and
- OR.sub.4 in which R.sub.4 is
- H,
- C.sub.2-8 alkanoyl,
- benzoyl
- phenyl,
- chlorophenyl or fluorophenyl,
- phenyl-C.sub.1-3 alkyl,
- C.sub.1-8 alkyl,
- C.sub.1-4 chloroalkyl or C.sub.1-4 fluoroalkyl,
- cycloalkyl-C.sub.1-3 alkyl,
- adamantyl-C.sub.1-3 alkyl, or
- substituted phenyl-C.sub.1-3 alkyl
- in which the substituents are selected from:
- chlorine or fluorine,
- C.sub.1-4 alkyloxy,
- C.sub.1-4 alkyl,
- C.sub.1-4 chloroalkyl or
- C.sub.1-4 fluroalkyl.
37 more elements
Dependencies are inferred from the claim text.