Tris carbamic acid esters: inhibitors of cholesterol absorption

Details Tris carbamic acid esters: inhibitors of cholesterol absorption Tris carbamic acid esters: inhibitors of cholesterol absorption

1993-07-21

1999-09-14

Kumar, Shailendra

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514210, 514211, 514212, 5142275, 5142278, 5142282, 5142312, 5142378, 514255, 514256, 514269, 514278, 514307, 514309, 514311, 514312, 514313, 514316, 514317, 514318, 514319, 514320, 514321, 514322, 514323, 514328, 514330, 514365, 514366, 514367, 514372, 514373, 514374, 514375, 514378, 514379, 514396, 514397, 514398, 540466, 540480, 540481, 540482, 540543, 540604, 544 59, 544 60, 544 61, 544 62, 544111, 544298, 544315, 544316, 544319, 544405, 546 16, 546141, 546153, 546157, 546186, 546187, 546188, 546208, 546

Patent

active

059523549

ABSTRACT:
Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.

REFERENCES:
patent: 5112859 (1992-05-01), Commons et al.
patent: 5169844 (1992-12-01), Commons et al.
Hoisie, et al., J. Biol. Chem. 262, 260-264 (1987).
De Vries, et al., J. Med. Chem. 29, 1131 (1986).
Gallo, et al., J. LIpid Research 25, 604-612 (1984).
Gallo, et al., Proc. Soc. Exp. Biol. and Med. 156, 277-281 (1977).
Scofield, et al., Biochemistry 16, 22492-2496 (1977).

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