| abstract |
A derivative of general formula: wherein Y is -SO2- or , (i) R1 and R2 each represents, same or different, (1) -H, (2) C1-16 alkyl or (3) the formula: wherein X is single-bond, -SO2-, C1-4 alkylene, C1-4 alkylene substituted by -COOH or , is carbocyclic or heterocyclic ring, n is 1 ~ 5, R4 is -H or C1-8 alkyl, C1-14 alkoxy, C1-6 alkylthio, -OH, halogen, -NO2 or trihalomethyl, the formula: -NR41R42 wherein R41 and R42 each represents halogen or C1-4 alkyl, tetrazole, -SO3H or -CH2OH, the formula:-SO2NR41R42 the formula: -Z41-COOR43 wherein Z41 is single-bond, C1-4 alkylene or C2-4 alkenylene, R43 is -H, C1-4 alkyl or benzyl, the formula: -CONR41R42 the formula:-COO-Z42-COOR43 wherein Z42 is C1-4 alkylene, R43 is -H or C1-4 alkyl, the formula: -COO-Z42-CONR41R42 the formula: -OCO-R45 wherein R45 is C1-8 alkyl or p-guanidinophenyl, the formula: -CO-R46 wherein R46 is C1-4 alkyl, the formula: -O-Z43-COOR45 wherein Z43 is C1-6 alkylene, the formula: wherein is an amino acid residue, R48 is -H or C1-4 alkyl, R49 is -OH, C1-4 alkoxy, -NH2, amino substituted by one or two C1-4 alkyl, carbamoylmethoxy or carbamoylmethoxy substituted by one or two C1-4 alkyl at N atom of carbamoyl, wherein is C3-6 heterocyclic ring, (ii) R1, R2 and N atom bonded to R1 and R2 together represents heterocyclic ring containing at least a N atom(s) and substituted by -COOH or unsubstituted heterocyclic ring containing at least a N atom(s), R3 is (1) -H, (2) -OH, (3) C1-6 alkyl, (4) halogen, (5) C1-4 alkoxy or (6) C2-5 acyloxy, m is 1-4, and non-toxic salts thereof which possess inhibitory activity on elastase, and are therefore useful for treating and/or preventing pulmonary emphysema, atherosclerosis and rheumatoid arthritis. |