Substituted tetralylmethylen-oxindole analogues as tyrosine kinase inhibitors

摘要

PCT No. PCT/EP97/02672 Sec. 371 Date Jan. 12, 1998 Sec. 102(e) Date Jan. 12, 1998 PCT Filed May 15, 1997 PCT Pub. No. WO97/45409 PCT Pub. Date Dec. 4, 1997A tetralylmethylene-2-oxindole derivative having the following formula (I) wherein one or two of R, R1, R2 and R3 the said two being the same or different, are selected from: a) -X-(CH2)m-NH2, -X-(CH2)m-NR4R5 or -X-(CH2)m-NHR6, in which X is -O-, -S- or -NH-, m is an integer of 2 to 4, one of R4 and R5 is hydrogen or C1-C6 alkyl and the other is C1-C6 alkyl or R4 and R5 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle, and R6 is C2-C6 alkanoyl or a C-terminally linked peptidyl residue containing from 1 to 3 aminoacids wherein the terminal amino group is either free or protected or in an alkylated form to provide a -NR4R5 group in which R4 and R5 are as defined above.