Reversible cysteine protease inhibitors

Details Reversible cysteine protease inhibitors Reversible cysteine protease inhibitors

C - Chemistry, Metallurgy

07

K

C07K 4/00 (2006.01) A61K 31/18 (2006.01) A61K 31/27 (2006.01) A61K 31/33 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/5375 (2006.01) A61K 31/5377 (2006.01) A61K 31/675 (2006.01) A61K 38/03 (2006.01) A61K 38/04 (2006.01) C07C 311/15 (2006.01) C07C 311/18 (2006.01) C07D 241/04 (2006.01) C07D 295/215 (2006.01) C07D 295/26 (2006.01) C07D 401/06 (2006.01) C07D 403/06 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01) C07F 9/6509 (2006.01) C07F 9/6533 (2006.01) C07K 5/00 (2006.01) C07K 5/04 (2

Patent

CA 2222972

A reversible cysteine protease inhibitor comprising two N-substituents linked via an ethylenediamine or a substituted ethylenediamine, wherein the dissociation constant for inhibition, K1, of a protease with the inhibitor, is no greater than about 100 µM, and wherein said N-substituents are selected from the group consisting of acyl, acylpeptidyl, alkyloxycarbonyl, alkyloxycarbonyl peptidyl, sulfonyl, sulfonyl peptidyl, peptidyl, sulfamoyl, sulfamoyl peptidyl, sulfinyl, sulfinyl peptidyl, carbamoyl, and carbamoyl peptidyl.

Cette invention concerne un inhibiteur réversible de cystéine protéase comportant deux substituants portés par des atomes d'azote et liés par l'intermédiaire d'une éthylènediamine ou d'une éthylènediamine substituée, la constante de dissociation K¿1? qui permet l'inhibition d'une protéase par un inhibiteur n'étant pas supérieure à 100µm environ, et lesdits substituants portés par l'azote étant sélectionnés dans le groupe constitué d'acyle, acyl peptidyle, alkyloxycarbonyle, alkoxycarbonyl peptidyle, sulfonyle, sulfonyl peptidyle, peptidyle, sulfamyle, sulfamyl peptidyle, sulfinyle, sulfinyl peptidyle, carbamyle et carbamyl peptidyle.

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