NOVEL 2-SACCHARINYLMETHYL ARYL CARBOXYLATES USEFUL AS PROTEOLYTIC ENZYME INHIBITORS AND COMPOSITIONS AND METHOD OF USE THEREFOR

摘要

26299-18 Disclosed are novel 2-saccharinylmethylaryl carbonates of the formula: (wherein Ar is phenyl, naphthyl or anthryl or such a group substituted one to three substituents such as alkyl, alkoxy, amino, halogen, hydroxy etc.; R4 is such as hydrogen, halogen, alkyl, cyano, amino, alkoxy, alkoxy carbonyl or phenyl; and R5 is hydrogen or substituent such as halogen, cyano, nitro, amino, etc. or R5 is a 5- or 6-membered saturated ring fused to the saccharin), similar compounds of the formula: (wherein R4a is hydrogen, alkyl or phenyl; R6 is hydrogen or primary alkyl; or R4a and R6 together form spirocyclopropyl; R7 is hydrogen or alkoxy; and Ar is as defined above) and of the formula: 26299-18 (wherein A is methylene, ethylene or dimethylmethylene and Ar is as defined above), useful in the treatment of degenerative diseases.