2-substituted saccharin derivative proteolytic enzyme...

Details 2-substituted saccharin derivative proteolytic enzyme... 2-substituted saccharin derivative proteolytic enzyme...

C - Chemistry, Metallurgy

07

D

C07D 275/06 (2006.01) A61K 31/425 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/695 (2006.01) C07D 417/02 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 513/04 (2006.01) C07F 7/10 (2006.01) C07F 9/6541 (2006.01)

Patent

CA 2079822

D.N. 7464D/55381 ABSTRACT Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytie enzymes are useful in the treatment of degenerative diseases and have the formula Image wherein: L is -O-, -S-, -SO- or -S02-; m and n are each independently 0 or 1; R1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heteroeyelyl or, when L is -O- and n is 1, cycloheptatrienon-2-yl or, when L is -S- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is -SO2- and n is 1, lower-alkyl or trifluoromethyl; R2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; and R3 and R4 are eaeh hydrogen or various substituents and processes for preparation and pharmaeeutical compositions and method of use thereof are disclosed.

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