4-substituted piperidinecarboxylic acid esters: inhibition of cholesterol absorption
US5169844A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 20, 1991 |
| Grant date | Dec 8, 1992 |
| Priority date | — |
| Expiry date | Dec 20, 2011 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D211/46
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.