The present invention are novel amino acid amide compounds of the following general formula which inhibit the enzyme acylcoenzyme A:cholesterol acyltransferase:
wherein R is phenyl or 1- or 2-naphthyl which are unsubstituted or may be substituted; R₁ is hydrogen or a straight or branched alkyl group having from 1 to 6 carbon atoms; R₂ is hydrogen, an aliphatic group, an aromatic group, an aralkyl or diarylalkyl group or R₁ and R₂ form a carbocyclic group; R₃ is hydrogen, an aliphatic group, an aralkyl group wherein the alkyl moiety may contain a carbocyclic entity; R₄ is hydrogen, an aliphatic group, SO₂R₁₄, -C(=S)NHR₁₅, -CO₂R₁₅, -COR₁₈, or -C(=O)NHR₁₅ wherein R₁₄ is morpholino, phenyl or substituted phenyl; R₁₅ is an alkyl group, phenyl or phenylalkyl wherein the phenyl group may be substituted; and R₁₈ is the same is R₁₅ or is halo-substituted alkyl, 9-fluorenylmethylene or pyrrolidino.
本发明是通式如下的新型
氨基酸酰胺化合物,可抑制酰
辅酶 A:
胆固醇酰基转移酶:
其中 R 是
苯基或 1-或 2-
萘基,它们未被取代或可能被取代;R₁ 是
氢或具有 1 至 6 个
碳原子的直链或支链烷基;R₂ 是
氢、
脂肪族基团、芳香族基团、芳烷基或二芳基烷基,或 R₁ 和 R₂ 形成
碳环基团; R₃ 是
氢、
脂肪族基团、芳烷基基团,其中烷基可包含
碳环实体;R₄ 是
氢、
脂肪族基团、SO₂R₁₄、-C(=S)NHR₁₅、-COR₂R₁₅、-COR₁₈ 或 -C(=O)NHR₁₅,其中 R₁₄ 是
吗啉基、
苯基或取代
苯基;R₁₅ 是烷基、
苯基或
苯基烷基,其中
苯基可被取代;以及 R₁₈ 与 R₁₅ 相同,或者是卤代烷基、9-
芴基亚
甲基或
吡咯烷基。