Substituted quinolymethylen-oxindole analogues as tyrosine kinase inhibitors

US5905149A · kind A · utility

Assignee

• Pharmacia & Upjohn S.p.A. · IT

Inventors

• Carlo Battistini · Milano, IT
• Antonella Ermoli · Romano Banco, IT
• Sergio Vioglio · Cusano Milanino, IT
• Franco Buzzetti · Monza, IT
• Dario Ballinari · San Donato Milanese, IT

Key dates

• Filing date: Jan 29, 1998
• Grant date: May 18, 1999
• Expiry date: Jan 29, 2018

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Quinolylmethylen-oxindole derivatives having general formula (I), wherein R is H or --(CH.sub.2).sub.n --COR.sub.7 group in which n is an integer of 1 to 4 and R.sub.7 is hydroxy, amino, C.sub.1 -C.sub.6 alkoxy or --NR.sub.5 R.sub.6 in which one of R.sub.5 and R.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.5 and R.sub.6 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle or R.sub.7 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 C.sub.1 -C.sub.4 alkyl ester, one or two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are selected from: a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.5 R.sub.6 or --X--(CH.sub.2).sub.m --NHR.sub.8 group; b) --NH--C(.dbd.NH)--NR.sub.5 R.sub.6, --NH--C(.dbd.NH)--NHR.sub.8, --N.dbd.CH--NH.sub.2, --N.dbd.CH--NR.sub.5 R.sub.6 or --N.dbd.CH--NHR.sub.8 group; c) --X--(C.sub.2).sub.n --COR.sub.7 group; d) --COR.sub.a or --COR.sub.9 group; e) --Y--CO--Y'--R.sub.10 group; and f) --NHR.su…