Patent Evaluation: Novel 5-bisaminomethylene-1,3-dioxane-4,6-diones as ACAT-inhibitors

Summary

Novelty: Novel 5-bisaminomethylene-1,3-dioxane-4,6-diones are disclosed. These compounds are said to be ACAT inhibitors which possess antioxidant properties.

Biology: In vitro ACAT inhibition was determined (IC₅₀ = 0.044 μM, 99% inhibition at a concentration of 26 μM). In vivo studies were undertaken on rats in order to establish inhibition of cholesterol absorption and percentage decrease of cholesterol in plasma (a 20 mg/kg dose induced a 62% decrease).

Chemistry: 5-[[[4-(Dimethylamino)phenyl]amino][(1-hexylheptyl)[[4-(2-methylpropyl)phenyl]-methyl]-amino]methylene]-2,2-dimethyl-1,3-dioxane-4,6-dione is one of seventy-seven specifically claimed compounds.

Structure: