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US 5,510,379 AGranted
Sulfonate ACAT inhibitors
AssigneeWarner-Lambert Company
InventorsHelen T. Lee, Joseph A. Picard, Drago R. Sliskovic
Life of this patent
Estimating the term…
Abstract
.beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
Claims13
A compound of Formula I ##STR32## wherein R.sub.1 is selected from (a) phenyl substituted with from 1 to 3 substituents selected from
- C.sub.1 -C.sub.4 alkyl,
- C.sub.1 -C.sub.4 alkoxy,
- C.sub.1 -C.sub.4 alkylthio,
- hydroxy,
- halo,
- nitro,
- cyano,
- trifluoromethyl,
- -COOH,
- -COOalkyl wherein alkyl has from 1 to 4 carbon atoms and which is straight or branched,
- -(CH.sub.2).sub.m NR.sub.x R.sub.y wherein m is 0 or 1, and each of R.sub.x and
- R.sub.y is independently hydrogen or C.sub.1 -C.sub.4 alkyl;
- R.sub.3 and R.sub.4 independently are C.sub.3 -C.sub.6 cycloalkyl, hydroxy-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, 1- or 2-naphthyl, or phenyl or naphthyl substituted with from 1 to 3 substituents selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, halo, nitro, cyano, trifiuoromethyl, phenyl, or C.sub.3 -C.sub.8 cycloalkyl;
- or R.sub.3 and R.sub.4 taken together with the carbon to which they are attached complete a C.sub.3 -C.sub.8 carbocyclic ring;
- Y is -NR.sub.2 -, wherein R.sub.2 is hydrogen C.sub.1 -C.sub.4 alkyl, phenyl, C.sub.1 -C.sub.4 alkylphenyl, wherein the phenyl may be substituted with 1, 2, or 3 groups selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, hydroxy, halo, nitro, cyano, trifluoromethyl, and COOH;
- R.sub.6 is phenyl substituted with from 1 to 3 substituents selected from:
- C.sub.1 -C.sub.4 alkyl,
- C.sub.1 -C.sub.4 alkoxy,
- C.sub.1 -C.sub.4 alkylthio,
- phenyl,
- hydroxy,
- halo,
- nitro,
- cyano,
- trifluoromethyl,
- -COOH,
- -COOalkyl wherein alkyl has from 1 to 4 carbon atoms and which is straight or branched, and
- -(CH.sub.2).sub.m NR.sub.x R.sub.y wherein m is 0 or 1, and each of R.sub.x and R.sub.y is hydrogen or a straight chain alkyl group having 1 to 4 carbon atoms.
25 more elements
Dependencies are inferred from the claim text.