Tocotrienol analogs in the treatment of hypercholesterolemia and hyperlipidemia
AssigneeBristol-Myers Squibb Company
InventorBradley C. Pearce
Life of this patent
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Abstract
This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.
Claims29
A method of treating hypercholesterolemia and hyperlipidemia which comprises administering to a patient in need of such treatment an effective amount of a method of the formula (II) ##STR41## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent hydrogen, C.sub.1 -C.sub.5 lower alkyl, halogen, COCH.sub.3, CH.sub.2 OH,CH.sub.2 CH.sub.2 OH, OH or OMe;
- R.sup.5 represents hydrogen or methyl;
- Y represents hydrogen or a hydrogen bond donating group, selected from the group consisting of NHSO.sub.2 Me, NHCO.sub.2 Me, NH.sub.2, CH.sub.2 OH, B(OH).sub.2, CONH.sub.2, SO.sub.2 NH.sub.2, or OH, with the proviso that Y is not hydrogen when R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are all hydrogen;
- X represents oxygen, sulfur, NH, N (C.sub.1 -C.sub.5 lower alkyl), N(acyl), CH.sub.2, CO, SO, SO.sub.2 ;
- n.sub.1 is 1 or 2;
- and
- n.sub.2 is 1 or 2;
- or nontoxic pharmaceutically acceptable acid addition salts, hydrate, solvate or metal salts thereof.
Dependencies are inferred from the claim text.