| abstract |
Quinolylmethylen-oxindole derivatives having general formula (I), wherein R is H or -(CH2)n-COR7 group in which n is an integer of 1 to 4 and R7 is hydroxy, amino, C1-C6 alkoxy or -NR5R6 in which one of R5 and R6 is hydrogen or C1-C6 alkyl and the other is C1-C6 alkyl or R5 and R6 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle or R7 is a N-terminally linked peptidyl residue containing from 1 to 3 aminoacids in which the terminal carboxyl group may be present as such, as amide, as alkali metal salt or as a C1-C4 alkyl ester; one or two of R1, R2, R3 and R4, which may be the same or different, are selected from: a) -X-(CH2)m-NH2, -X-(CH2)m-NR5R6 or -X-(CH2)m-NHR8 group; b)-NH-C(=NH)-NR5R6, -NH-C(=NH)-NHR8, -N=CH-NH2, -N=CH-NR5R6 or -N=CH-NHR8 group; c) -X-(CH2)n-COR7 group; d) -CORa or -COR9 group; e) -Y-CO-Y'-R10 group; and f) -NHR8 or -NHR11 group and the pharmaceutically acceptable salts thereof, are tyrosine kinase inhibitors. |