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US 5,310,748 AGranted
Imidazoles for the treatment of atherosclerosis
AssigneeThe Du Pont Merck Pharmaceutical Company
InventorsRichard G. Wilde, C. Anne Higley, Jeffrey T. Billheimer, Ruth R. Wexler
Life of this patent
Estimating the term…
Abstract
Disclosed are imidazoles as inhibitors of acylCoA:cholesterol acyltransferase (ACAT), processes for their preparation, pharmaceutical compositions, and their use as antihypercholesterolemics and/or antiatherosclerotics.
Claims9
A compound of the formula:
- ##STR51## or stereosiomers and pharmaceutically acceptable salts thereof wherein:
- X is S(O).sub.p, CH.sub.2 or NR.sup.4 ;
- A is CH.sub.2, O, S, S(O).sub.r or NR.sup.8 ;
- B is [O, S,] or NR.sup.9 ;
- Y is O, S or H.sub.2 ;
- Z is NHR.sup.5, OR.sup.5 or R.sup.5
- R.sup.1, R.sup.2, R.sup.6 and R.sup.7 are selected independently from H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, thienyl, furanyl, or phenyl optionally substituted with 1-3 groups independently selected from C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, CH.sub.3 S(O).sub.t, F, or NR.sup.15 R.sup.16 ;
- R.sup.3 is H, and C.sub.1 -C.sub.6 alkyl, allyl, benzyl, or phenyl, each being optionally substituted with F, Cl, CH.sub.3, OCH.sub.3, or CF.sub.3 ;
- R.sup.5 is C.sub.1 -C.sub.8 alkenyl, C.sub.1 -C.sub.8 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloalkyl, C.sub.7 -C.sub.14 aralkyl, phenyl optionally substituted with 1-3 groups independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.8 branched alkyl, F, Cl, C.sub.1 -C.sub.4 alkoxy, or CN, pyrrolidyl, or imidazolyl;
- R.sup.4, R.sup.8, R.sup.9, R.sup.15, and R.sup.16 are selected independently from H, C.sub.1 -C.sub.8 alkyl, benzyl, or phenyl;
- m is 2-8;
- n is 0-5;
- and
- p, r and t are independently 0-2.
11 more elements
Dependencies are inferred from the claim text.