Patent Evaluation: Uses of Verbenone and Verbenone cyclodextrin complexes as anti-elastase drugs

Summary

Novelty: The use of the terpene derivative verbenone, (1S)-(-)-4,6,6-trimethylbicyclo-[3.1.1]hept-3-ene-2-one, in the treatment of pulmonary emphysema is disclosed. Verbenone is claimed to be an elastase inhibitor.

Biology: Elastase inhibitory activity of verbenone was determined in vitro using neutrophilic polymorphonuclear cells from heparinised peripheral blood. Inhibition of elastase release was 83–96% for verbenone concentrations of 10pM-1 mM (greatest inhibition at 0.1 nM).

Chemistry: The synthesis of verbenone itself is not given but the preparation of three verbenone cyclodextrin complexes are detailed. Verbenone and verbenone cyclodextrin complexes are specifically claimed.