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US 5,981,595 AGranted
Sulfonyl urea and carbamate ACAT inhibitors
AssigneeWarner-Lambert Company
InventorsJoseph Armand Picard, William Howard Roark, Bruce David Roth
Life of this patent
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Abstract
A pharmaceutically useful compound which lowers blood cholesterol levels having the formula ##STR1## wherein X is oxygen or --NH--; Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; R.sub.1 is hydrogen, lower alkyl or benzyl; and R.sub.2 is a straight or branched alkyl group having from 5 to 17 carbon atoms which may be substituted on the 1-carbon position with methyl, ethyl, phenyl, or substituted phenyl, or a cycloalkyl group having from 3 to 8 carbon atoms.
Claims8
A compound of the formula wherein X is --NH--;
- wherein Ar is
- (a) phenyl which is substituted by
- 2,6 -bis(methylethyl),
- 2,4,6-trimethoxy, or from one to three substituents selected from:
- hydroxy,
- nitro,
- --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.3 R.sub.4 wherein m is zero or one, and each of R.sub.3 and R.sub.4 is hydrogen or a straight or branched alkyl group having 1 to 4 carbon atoms;
- or
- (b) 1- or 2-naphthyl which is unsubstituted or substituted with one to three substituents selected from:
- alkyl having from 1 to 4 carbon atoms and which is straight or branched,
- alkoxy having from 1 to 3 carbon atoms and which is straight or branched,
- hydroxy,
- fluorine,
- chlorine,
- bromine,
- nitro,
- cyano,
- trifluoromethyl,
- --COOH,
- --COOalkyl wherein alkyl has from 1 to 4 carbon atoms and is straight or branched,
- --(CH.sub.2).sub.m NR.sub.3 R.sub.4 wherein m, R.sub.3, and R.sub.4 have the meanings defined above;
- wherein R.sub.1 is hydrogen, lower alkyl having from 1 to 4 carbon atoms or benzyl;
- wherein R.sub.2 is ##STR25## wherein each of R.sub.5 and R.sub.6 is hydrogen, methyl or ethyl, or R.sub.5 and R.sub.6 together with the carbon atom to which they are attached form a cyclic group having from 3 to 8 carbon atoms;
- and R.sub.7 is a straight or branched alkyl group having from 4 to 16 carbon atoms;
- and pharmaceutically acceptable salts thereof.
24 more elements
Dependencies are inferred from the claim text.