Patent Evaluation: Novel Pyridone Reverse Transcriptase Inhibitors for the Treatment of HIV Infection

Summary

Novelty: A group of pyridones are claimed as reverse transcriptase inhibitors; they are related to those claimed in AM4930.

Biology: Biological data include methodology and general statements to the effect that the preferred group of compounds inhibit RT with IC₅₀ values in the 7–30 nM range and in a cell culture assay have CIC₉₅ between 6 and 100 nM.

Chemistry: There is extensive synthetic detail with ninety two examples. Thirty-two examples are specifically claimed, one of which is 3-[[(4,7-dichlorobenzoxazol-2-yl)methyl]amino]-5-ethyl-6-methyl-2-(1H)-pyridone.