| Abstract: | The invention relates to quinazoline derivatives of formula (1) ##STR1## wherein m is an integer from 1 to 2; R.sup.1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-3 alkylthio, or --NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6, which may be the same or different, each represents hydrogen or C.sub.1-3 alkyl); R.sup.2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R.sup.3 represents hydroxy, halogeno, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-3 alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X.sup.1 represents --O--, --CH.sub.2 --, --S--, --SO--, --SO.sub.2 --, --NR.sup.7 CO--, --CONR.sup.8 --, --SO.sub.2 NR.sup.9 --, --NR.sup.10 SO.sub.2 -- or --NR.sup.11 -- (wherein R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 each independently represents hydrogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxyC.sub.2-3 alkyl); R.sup.4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis. |
| Inventor(s): | Thomas; Andrew Peter (Macclesfield, GB), Johnstone; Craig (Macclesfield, GB), Clayton; Edward (Macclesfield, GB), Stokes; Elaine Sophie Elizabeth (Macclesfield, GB), Lohmann; Jean-Jacques Marcel (Reims Cedex, FR), Hennequin; Laurent Francois Andre (Reims Cedex, FR) |
