Cholesterol ester hydrolase inhibitors

Details Cholesterol ester hydrolase inhibitors Cholesterol ester hydrolase inhibitors

1993-05-13

1995-02-21

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

N-c doai

514529, 514550, 560 20, 560 23, 560 24, 560 29, 560 30, 560 31, 560 32, 560 33, 560115, 560117, 560118, 560120, 560121, 560123, 560124, 560133, A61K 31325, C07C27102, C07C27140

Patent

active

053915712

ABSTRACT:
The compounds of the formula: ##STR1## in which R.sup.1 is alkyl of 4 or more carbon atoms, cycloalkyl, 1-adamantyl, 2-adamantyl, 3-noradamantyl, 3-methyl-1-adamantyl, 1-fluorenyl, 9-fluorenyl, cycloalkylalkyl, phenyl, substituted phenyl, alkyl, alkoxy, halo, nitro, cyano or trifluoromethyl, phenylalkyl or substituted phenylalkyl, where the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R.sup.2 is hydrogen, alkyl or R.sup.1 taken with R.sup.2 and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula: ##STR2## wherein ##STR3## in which R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; useful as inhibitors of cholesterol ester hydrolase.

REFERENCES:
patent: 4163861 (1979-08-01), Illuminati et al.
Chemical Abstract, vol. 95, #168777u, 1981.
Foldes et al, Experimental Therap. 457-468, 1958.
Bhat et al., Biochem. Biophys. Res. Commun., 109, 486 (1982).
Gallo et al., J. Lipid Research, 25, 604 (1984).
Hosie et al., J. Biol. Chem. 262, 260 (1987).
Stout et al., Biochem. Biophys. Acta, 837, 6 (1985).
Field, J. Lipid Research, 25, 389 (1984).
Cayen et al., J. Lipid Research, 20, 162 (1979).
Foldes et al., J. Pharmacol. Exptl. Therap. 122, 457-464 (1958).
Sumida et al., Plant & Cell Physiol. 14, 781-785 (1973).
van den Berg et al., Pestic. Sci. 13, 29-38 (1982).
Derwent Abstract 81-55962-D of Japanese Patent J56071-058, 1981.

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