.alpha.- (1,3- or 1, 2- dicarbonylenol ether methyl ketones as cysteine protease inhibitors
AssigneePrototek, Inc.
InventorsMary P. Zimmerman, Robert E. Smith, Mark Becker
Life of this patent
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AssigneePrototek, Inc.
InventorsMary P. Zimmerman, Robert E. Smith, Mark Becker
Estimating the term…
Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a .beta.-dicarbonyl enol ether leaving group.
Cathepsin or calpain inhibitors of the formula:
Protease inhibitors of the formula:
Dependencies are inferred from the claim text.