HUMAN LEUKOCYTE ELASTASE INHIBITORS AND METHODS OF PRODUCING AND USING SAME

摘要

Compounds selected from the group consisting of a compound of formula (I), and a compound of formula (II), wherein x is 1 or 2, Y is carbobenzoxy or benzoyl, and XR is (III) have use as elastase enzyme inhibitors. Particularly potent are the L-proline diastereomers. Elastase enzyme inhibitory compositions comprise a carrier and an elastase enzyme inhibiting amount of the compounds of the invention. A method of selectively inhibiting the enzyme elastase in an animal or a human in need of such treatment comprises administering to the animal or human an enzyme elastase inhibiting amount of one of the compounds of the invention or a composition thereof. A method of reducing corneal scarring or fibroblast proliferation comprises applying to an area of a subject's eye afflicted with the condition a corneal scar- or fibroblast proliferation-reducing amount of a free or polymer-bound HLE inhibitory agent under conditions and for a period of time effective to attain the desired effect. A method of reducing neovascularization of corneal scar tissue comprises applying to an area of a subject's eye afflicted with the condition a neovascularization-inhibitory amount of a free or polymer-bound HLE inhibitory agent under conditions and for a period of time effective to attain the desired effect.