Carbamate inhibitors of cholesterol esterase and their use as hy

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

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Details

560134, 560136, 558234, 558235, A61K 3122

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active

050666746

ABSTRACT:
Certain carbamate esters are used as inhibitors as cholesterol esterase and function as hypolipidemic and hypocaloric agents. The invention also relates to a method of decreasing the absorption of dietary cholesterol and fats through the wall of the intestinal tract.

REFERENCES:
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patent: 4095034 (1978-06-01), Mangold et al.
patent: 4381195 (1983-04-01), Hyzak
patent: 4786652 (1988-11-01), Venuti
Hosie, Lynn et al., "p-Nitrophenyl and Cholesteryl-N-Alkyl Carbamates as Inhibitors of Cholesterol Esterase", Journal of Biological Chemistry, vol. 262, No. 1, Jan. 5, 1987, pp. 260-264.
Bat, Santhoor G. et al., "The Role of Cholesteryl Ester Hydrolysis and Synthesis in Cholesterol Transport Across Rat Intestinal Mucosal Membrane a New Concept", Biochem. & Biophys. Res. Comm., vol. 109, No. 2, 1982, pp. 486-492.
Gallo, Linda L. et al., "Cholesterol Absorption in Rat Intestine: Role of Cholesterol Esterase and Acyl Coenzyme A: Cholesterol Acyltransferase", Journal. of Lipid Research, vol. 25, 1984, pp. 604-612.
Watt, Shirley M. et al.,. "The Effect of Pancreatic Diversion on Lymphatic Absorption and Esterification of Cholesterol in the Rat", Journal of Lipid Research, vol. 22, 1982, pp. 157-165.
Sutton, Larry D. et al., "Phenyl-n-Butylborinic Acid is a Potent Transition State Analog Inhibitor of Lipolytic Enzymes", Biochem & Biophys. Res. Comm., vol. 134, No. 1, 1986, pp. 386-392.

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