4-substituted piperidinecarboxylic acid esters: inhibition of ch

Details 4-substituted piperidinecarboxylic acid esters: inhibition of ch 4-substituted piperidinecarboxylic acid esters: inhibition of ch

1991-12-20

1992-12-08

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514212, 5142278, 5142372, 514316, 514327, 540488, 540524, 544 584, 544129, 546188, 546216, A61K 31445

Patent

active

051698447

ABSTRACT:
Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in inhibition of absorption of cholesterol and thus lowers serum cholesterol levels. Compounds of the formula below: ##STR1## where R.sup.1 is selected from alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or arylalkyl and R.sup.2 is hydrogen or alkyl or --NR.sup.1 R.sup.2 is morpholine, thiomorpholine or 4-substituted or unsubstituted piperidine and R.sup.3, R.sup.4, R.sup.5, R.sup.6 are hydrogen, alkyl, alkoxy, halogen, nitro, cyano, perhaloalkyl, alkanoyloxy, alkoxycarbonyl or hydroxycarbonyl have been shown to inhibit the enzymes CEH and/or ACAT in in vitro tests to inhibit absorption of radio-labeled cholesterol in rats.

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Field, J. Lipid Research, 25, 389 (1984).
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Sumida et al., Plant & Call Physiol. 14, 781-785 (1973).
van den Berg et al., Pestic. Sci. 13, 19-38 (1982).
Derwent Abstract 81-55962-D of Japanese Patent J56071-058.

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