The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Jul. 03, 1990
Filed:
Sep. 19, 1988
Norman B Javitt, New York, NY (US);
Stephen R Wilson, Chatham, NJ (US);
New York University, New York, NY (US);
Abstract
This invention relates to cholesterol synthesis and to the accumulation and regulation of cholesterol levels in body tissue. More specifically, the invention provides that the compound 26-aminocholesterol, ##STR1## and analogs and derivatives thereof, exhibit biological activity as a potent inhibitor of cholesterol synthesis and/or cholesterol accumulation in body tissue. The compounds strongly inhibit of the enzyme HMGCoA reductase and low density lipoprotein accumulation by non-hepatic cells. Surprisingly, it has been discovered that 26-aminocholesterol is selective for fibroblast (plasma) cells, and has little or no effect on hepato (liver) cells. Therapeutic compounds according to the invention include substituted or unsubstituted sterols of the formula: ##STR2## wherein the carbon atoms at positions 5 and 6 of the sterol are one of saturated and unsaturated, R.sub.1 is one of a 3-hydroxyl group and a 3-keto group, R.sub.2 is one of a hydroxyl group and a keto group, and wherein at least one of R.sub.3, R.sub.4 and R.sub.5 is an amino group and the others are each selected from the group consisting of hydrogen and an amino group.