| abstract |
A derivative of general formula:n wherein Y is -S0 2 - orn n (i) R' and R 2 each represents, same or different, (1) -H, (2) C1-16 alkyl or (3) the formula: -X (R 4 ) n nwherein X is single-bond, -S0 2 -, C1-4 alkylene, C1-4 alkylene substituted by -COOH orn is carbocyclic or heterocyclic ring, n is 1 - 5, R 4 is -H or C1-8 alkyl, C1-14 alkoxy, C1-6 alkylthio, -OH, halogen, -N0 2 or trihalomethyl, the formula: -NR 4 'R 42 wherein R 41 and R 42 each represents halogen or C1-4 alkyl, tetrazole, -SO 3 H or -CH 2 0H, nthe formula:-SO 2 NR 41 R 42 the formula: -Z 41 -COOR 43 wherein Z 41 is single-bond, C1-4 alkylene or C2-4 alkenylene, R 43 is -H, C1-4 alkyl or benzyl, the formula: -CONR 41 R 42 the formula:-COO-Z 42 -COOR 43 wherein Z 42 is C1-4 alkylene, R 43 is -H or C1-4 alkyl, the formula: -COO-Z 42 -CONR 41 R 42 the formula: -OCO-R 45 wherein R 45 is is C1-8 alkyl or p-guanidinophenyl, the formula: -CO-R 46 is wherein R 46 is C1-4 alkyl, the formula: -O-Z 43 -COOR 45 wherein Z 43 is C1-6 alkylene, the formula:n wherein - N -Z 44 -CO is an amino acid residue, R 48 is -H or C1-4 alkyl, R 49 is -OH, C1-4 alkoxy, -NH 2 , 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, whereinn is C3-6 heterocyclic ring, (ii) R', R 2 and N atom bonded to R 1 and R 2 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), R 3 is (1) -H, (2) -OH, (3) C1-6 alkyl, (4) halogen, (5) C1-4 alkoxy or (6) C2-5 acyloxy, m is 1-4, nand 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. |