26-aminocholesterol and derivatives and analogs thereof in the r

Details 26-aminocholesterol and derivatives and analogs thereof in the r 26-aminocholesterol and derivatives and analogs thereof in the r

1988-09-19

1990-07-03

Lipovsky, Joseph A.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514182, A61K 3156

Patent

active

049391348

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.

REFERENCES:
patent: 3156619 (1964-11-01), Bertin et al.
patent: 3271250 (1966-09-01), Kaazawa et al.
patent: 3291690 (1966-12-01), Bertin et al.
patent: 3839565 (1974-10-01), Saltzman
patent: 4427668 (1984-01-01), Javitt
CA 98:103618k (1983).
CA 94:27444a (1981).
CA 82:13692v (1975).
CA 79:144832b (1973).
CA 110:5143y (1988).
CA 91:141094z (1979).

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