Patent Evaluation: Substituted Pyrroles as Protein Kinase C Inhibitors

Summary

Novelty: Substituted pyrrole compounds, which are proposed to be protein kinase C inhibitors, are disclosed. They are claimed to be potentially useful for the treatment of a wide range of conditions including inflammatory, immunological, cardiovascular and pulmonary disorders. Potential use for the treatment of diabetic complications and AIDS is also claimed.

Biology: Data relating to a protein kinase C inhibition assay are presented. Test compounds had IC₅₀ values in the range 7–40 nM.

Chemistry: Trans-3-[2,3,3a,4,11,11a-hexahydro-2-methyl-1H-pyrrolo[3′,4′,4,5]pyrido[1,2a] indol-10-yl]-4-(1-methyl-3-indolyl)-1H-pyrrole-2,5-dione is one of three compounds specifically claimed. Preparative details using standard techniques are presented.