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US 5,491,152 AGranted
Derivatives of cyclic ethers and sulfides for the treatment of atherosclerosis
AssigneeThe Du Pont Merck Pharmaceutical Company
InventorsRichard G. Wilde, Soo S. Ko, Jeffrey T. Billheimer
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Abstract
The present invention provides compounds of Formula I, ##STR1## or a pharmaceutically acceptable salt forms thereof, which are inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.
Claims15
A compound of Formula I:
- ##STR147## or a pharmaceutically acceptable salt form thereof, wherein:
- A is ##STR148## X is selected from:
- --O--, --S--, --S(.dbd.O)--, and --S(.dbd.O).sub.2 --;
- Y is --C(.dbd.O)--;
- Z is selected from a bond and --(CH.sub.2).sub.p --;
- p is an integer selected from 1-5;
- G is selected from:
- phenyl substituted with 1-3 R.sup.30, and
- naphthyl substituted with 0-3 R.sup.30 ;
- G may also be selected from a heterocylic group selected from:
- ##STR149## each such heterocyclic group being optionally fused to a benzene ring, and each such heterocyclic group and fused benzene ring being substituted with 0-3 R.sup.30 or 0-3 phenyl groups, each phenyl being substituted with 0-3 R.sup.30 ;
- G may also be chosen from the following heterocyclic groups:
- ##STR150## each such heterocyclic group being substituted with 0-3 R.sup.30 or 0-3 phenyl groups, each phenyl being substituted with 0-3 R.sup.30 ;
- R.sup.1 is selected from:
- H,
- C.sub.1 -C.sub.6 alkyl,
- C.sub.3 -C.sub.8 cycloalkyl,
- C.sub.4 -C.sub.9 cycloalkylalkyl,
- benzyl substituted with 0-3 R.sup.30, and
- phenyl substituted with 0-3 R.sup.30 ;
- R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are independently selected from:
- H,
- C.sub.1 -C.sub.13 alkyl,
- C.sub.3 -C.sub.8 cycloalkyl,
- C.sub.3 -C.sub.8 cycloalkyloxy,
- C.sub.4 -C.sub.9 cycloalkylalkyl,
- C.sub.4 -C.sub.9 cycloalkylalkyloxy,
- C.sub.4 -C.sub.12 alkenyl,
- C.sub.4 -C.sub.12 alkenyloxy,
- C.sub.4 -C.sub.12 alkynyl,
- C.sub.4 -C.sub.12 alkynyloxy,
- C.sub.1 -C.sub.10 alkoxy,
- C.sub.2 -C.sub.12 alkoxyalkyl,
- C.sub.2 -C.sub.12 alkoxyalkyloxy,
- C.sub.3 -C.sub.14 alkoxyalkoxyalkyl,
- C.sub.2 -C.sub.10 alkylcarbonyloxy,
- C.sub.1 -C.sub.10 alkylthio,
- C.sub.2 -C.sub.10 alkylthioalkyl,
- C.sub.1 -C.sub.10 haloalkyl,
- aryl-(C.sub.1 -C.sub.5 alkyl)-substituted with 0-3 R.sup.30,
- aryl-(C.sub.1 -C.sub.5 alkyl)oxy substituted with 0-3 R.sup.30,
- aryl substituted with 0-3 R.sup.30, and
- aryloxy substituted with 0-3 R.sup.30 ;
- R.sup.3 and R.sup.4 can also be taken together to form a --(CH.sub.2).sub.q -- bridge;
- q is an integer selected from 1-4;
- R.sup.30 is selected independently from:
- C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.4 -C.sub.9 cycloalkylalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.2 -C.sub.8 dialkylamino, halogen, C.sub.1 -C.sub.6 haloalkyl, and nitro.
44 more elements
Dependencies are inferred from the claim text.