Triterpene derivatives cholesterol acyltransferase inhibitors an

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

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Details

514559, 560173, 562508, C07C22900, C07C 6200, A61K 31215, A61K 3119

Patent

active

049871510

ABSTRACT:
The present invention provides a purified compound of the structure; ##STR1## wherein R may be palmitoyl or steroyl. The invention also provides compositions comprising an admixture of the foregoing palmitate and stearate esters.
The invention also provides a compound of the structure: ##STR2## The invention further provides pharmaceutical compositions including the aforementioned compounds and compositions and methods of inhibiting the acyl CoA: cholesterol acyltransferase catalyzed conversion of cholesterol to cholesteryl esters.

REFERENCES:
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L. L. Gallo, et al., (1987), J. Lipid Res.; 28:381 (Exhibit 3).
B. Middleton et al., (1987), Drugs, 33 (Sup. 2): 75-79 (Exhibit 4).
J. L. Kelly et al., (1988), Biochimica Et Biophysica Acta, 960:83-90 (Exhibit 5).
E. E. Largis, et al., (1989), J. Lipid Res.; 30:681-690 (Exhibit 6).
S. B. Clark et al., (1984), J. Lipid Res.; 25:148-159 (Exhibit 7).
J. G. Heider et al., (1983), J. Lipid Res.; 24:1127-34 (Exhibit 8).
S. A. Schaffer, et al., (1986), Atherosclerosis VII; 633-636 (Exhibit 9).
I. Tabas et al., (1986), J. Biol. Chem.; 261:3147-3155 (Exhibit 10).
Nozakli et al. J. Chem Soc. Chem Commun. 1982 pp. 1048-1051.

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