Patent Evaluation: Iminodicarbonic acid ester ACAT inhibitors

Summary

Novelty: Imino and thiocarbonyl compounds are disclosed which have ACAT inhibitory properties. These may have utility in the treatment of atherosclerosis.

Biology: The ability of the compounds to inhibit ACAT was measured in vitro according to Field and Salone (Biochemica et Biophysica (1982) 712: 557–570). IC₅₀ values were in the range 0.017–10.37 μM. An in vivo test using male Spague-Dawley rats produced reductions in blood cholesterol levels by 4mg/dL to 70mg/dL.

Chemistry: The compounds were synthesised using standard techniques. Thirty-three compounds are specifically claimed. Iminodicarbonic acid, 2,6-bis(1-methylethyl)phenyl-1-methyltridecyl ester is a preferred compound.