Patent · US Expired

Acat inhibitors for treating hypocholesterolemia

US5153226A · kind A · utility

19Cited by
7References
1Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJul 30, 1990
Grant dateOct 6, 1992
Priority date
Expiry dateJul 30, 2010

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C2603/18
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention are novel amino acid amide compounds of the following general formula which inhibit the enzyme acylcoenzyme A:cholesterol acyltransferase: ##STR1## wherein R is phenyl or 1- or 2-naphthyl which are unsubstituted or may be substituted; R.sub.1 is hydrogen or a straight or branched alkyl group having from 1 to 6 carbon atoms; R.sub.2 is hydrogen, an aliphatic group, an aromatic group, an aralkyl or diarylalkyl group or R.sub.1 and R.sub.2 form a carbocyclic group; R.sub.3 is hydrogen, an aliphatic group, an aralkyl group wherein the alkyl moiety may contain a carbocyclic entity; R.sub.4 is hydrogen, an aliphatic group, SO.sub.2 R.sub.14, --C(.dbd.S)NHR.sub.15, --CO.sub.2 R.sub.15, --COR.sub.18, or --C(.dbd.O)NHR.sub.15 wherein R.sub.14 is morpholino, phenyl or substituted phenyl; R.sub.15 is an alkyl group, phenyl or phenylalkyl wherein the phenyl group may be substituted; and R.sub.18 is the same is R.sub.15 or is halo-substituted alkyl, 9-fluoroenylmethylene or pyrrolidino.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.