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US 4,902,709 AGranted
Novel 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 (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 alkanoylamino, 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 fluroalkyl, phenyl, phenyl substituted by Cl or F, C.sub.1-4 alkyloxy. C.sub.2-8 alkanoyloxy C.sub.2-8 -Balkanoyloxy-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 flurophenyl, phenyl-C.sub.1-3 alkyl, C.sub.1-8 alkyl, C.sub.1-4 chloroalkyl or C.sub.1-4 fluroalkyl, 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;
- R.sub.5 is hydrogen, C.sub.1-5 alkyl or C.sub.1-5 alkyl substituted with a member of the group consisting of phenyl, dimethylamino, or acetylamino;
- and
- a pharmaceutically acceptable salt of the compound (II) in which R.sub.5 is hydrogen.
8 more elements
Dependencies are inferred from the claim text.