| abstract |
(57) [Summary] (Modified) [Object] To provide saccharin derivatives that inhibit the enzymatic activity of proteolytic enzymes, methods for producing them, methods for using them in the treatment of degenerative diseases, and pharmaceutical compositions thereof. [Structure] The following formula I [L is N, O or SO n (where n is 0, 1 or 2), L-R 1 is a leaving group, and H- L-R 1 is their conjugate acid, when L is N, H-L-R 1 has a pKa value of 6 or less, and when L is O, H-L- R 1 has a pKa value of 8 or less, Is SO n , H-LR 1 has a pKa of 5 or less. Has a value, R 2 is alkyl, alkylamino, alkylmethylamino, diethylamino or alkoxy, R 3 is 1 to 3 various substitutions at any or all of the 5-, 6- and 7-positions. A group]. |