Biphenyl amide cholesterol ester hydrolase inhibitors

Details Biphenyl amide cholesterol ester hydrolase inhibitors Biphenyl amide cholesterol ester hydrolase inhibitors

1990-09-14

1992-05-12

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

N-c doai

514487, 514490, 560 32, 560115, 560163, A01N, A01N, A61K 3127, C07C26100, C07C26900

Patent

active

051128594

ABSTRACT:
The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## NR.sup.5,--O-- or --S--; where R.sup.3, R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl of gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.

REFERENCES:
patent: 3275512 (1966-09-01), Lemin
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Hosie et al., J. Biol. Chem. 262(1) 260 (1987).
Stout et al., Biochim, Biophys. Acta, 837 6 (1985).
Scofield et al., Biochemistry, 16 (11) 2492 (1977).
Ogawa et al., Chem. Pharm. Bull., 34 (3) 1118 (1986).
Lombardo, Biochim. Biophys. Acta, 700 75 (1982).
Gallo et al., Proc. of the Soc. for Exper. Biol. and Med., 156 277 (1977).
Gallo et al., J. Lipid Res., 25 604 (1984).
Chem. Abstract 19492 (Abstract of Belg. 654,121) (1966).
Sonnet et al., J. Econ. Entomology, 64(6) (1971) 1378.

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