Human leukocyte elastase inhibitors and methods of producing...

Details Human leukocyte elastase inhibitors and methods of producing... Human leukocyte elastase inhibitors and methods of producing...

C - Chemistry, Metallurgy

07

K

167/233, 260/312

C07K 5/062 (2006.01) A61K 38/06 (2006.01) C07D 207/16 (2006.01) C07K 5/06 (2006.01) C07K 5/068 (2006.01) C07K 5/083 (2006.01) C07K 5/09 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2001629

HUMAN LEUKOYTE ELASTASE INHIBITORS AND METHODS OF PRODUCING AND USING SAME ABSTRACT OF THE DISCLOSURE Compounds selected from the group consisting of a compound of the formula Image (I) and a compound of the formula Image (II) wherein x is 1 or 2, Y is carbobenzoxy or benzoyl, and XR is Image 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- 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.

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