Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof

摘要

Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula <IMAGE> wherein: L is -O-, -S-, -SO- or -SO2-; m and n are each independently 0 or 1; R1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl 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 each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.