Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1990-07-30
1992-10-06
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514618, 514619, 514620, 514621, 514622, 514626, 514255, 5142382, 514414, 514419, 514378, 514374, 514399, 514463, 514385, 564164, 564165, 564167, 564166, 564194, 544165, 544400, A61K 3118, A61K 31165
Patent
active
051532263
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.
REFERENCES:
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patent: 4310429 (1982-01-01), Lai
patent: 4500662 (1985-02-01), Lai
patent: 4639468 (1987-01-01), Roncucci et al.
patent: 4891058 (1990-01-01), Wee
patent: 4944796 (1990-07-01), Wee
patent: 4987153 (1991-01-01), Kay et al.
Chucholowski Alexander W.
Creswell Mark W.
Roark William H.
Sircar Ila
Newtson Ruth H.
Raymond Richard L.
Russell Mark W.
Warner-Lambert & Company
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