The invention relates to quinazoline derivatives of formula (I) (wherein:
R.sup.1 represents hydrogen or methoxy; R.sup.2 represents methoxy,
ethoxy, 2-methoxyethoxy, 3-methoxypropoxy, 2-ethoxyethoxy,
trifluoromethoxy, 2,2,2-trifluoroethoxy, 2-hydroxyethoxy,
3-hydroxypropoxy, 2-(N,N-dimethylamino)ethoxy,
3-(N,N-dimethylamino)propoxy, 2-morpholinoethoxy, 3-morpholinopropoxy,
4-morpholinobutoxy, 2-piperidinoethoxy, 3-piperidinopropoxy,
4-piperidinobutoxy, 2-(piperazin-1-yl)ethoxy, 3-(piperazin-1-yl)propoxy,
4-(piperazin-1-yl)butoxy, 2-(4-methylpiperazin-1-yl)ethoxy,
3-(4methylpiperazin-1-yl)propoxy or 4-(4-methylpiperazin-1-yl)butoxy; the
phenyl group bearing (R.sup.3).sub.2 is selected from:
2-fluoro-5-hydroxyphenyl, 4-bromo-2-fluorophenyl, 2,4-difluorophenyl,
4-chloro-2-fluorophenyl, 2-fluoro-4-methylphenyl,
2-fluoro-4-methoxyphenyl, 4-bromo-3-hydroxyphenyl,
4-fluoro-3-hydroxyphenyl, 4-chloro-3-hydroxyphenyl,
3-hydroxy-4-methylphenyl, 3-hydroxy-4-methoxyphenyl and
4-cyano-2-fluorophenyl); and salts thereof, processes for their
preparation and pharmaceutical compositions containing a compound of
formula (I) or a pharmaceutically acceptable salt thereof as active
ingredient The compounds of formula (I) and the 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
##STR1##
L'invention concerne des dérivés de quinazoline de la formule (i) (où : R.sup.1 représente l'hydrogène ou méthoxy ; R.sup.2 représente méthoxy, l'ethoxy, le 2-methoxyethoxy, le 3-methoxypropoxy, le 2-ethoxyethoxy, le trifluoromethoxy, le 2,2,2-trifluoroethoxy, le 2-hydroxyethoxy, le 3-hydroxypropoxy, le 2-(N, le N-dimethylamino)ethoxy, le 3-(N, le N-dimethylamino)propoxy, le 2-morpholinoethoxy, le 3-morpholinopropoxy, le 4-morpholinobutoxy, le 2-piperidinoethoxy, le 3-piperidinopropoxy, le 4-piperidinobutoxy, le 2-(piperazin-1-yl)ethoxy, le 3-(piperazin-1-yl)propoxy, le 4-(piperazin-1-yl)butoxy, le 2-(4-methylpiperazin-1-yl)ethoxy, le 3-(4methylpiperazin-1-yl)propoxy ou le 4-(4-methylpiperazin-1-yl)butoxy ; le roulement de groupe phényle (R.sup.3).sub.2 est choisi à partir : 2-fluoro-5-hydroxyphenyl, 4-bromo-2-fluorophenyl, 2,4-difluorophenyl, 4-chloro-2-fluorophenyl, 2-fluoro-4-methylphenyl, 2-fluoro-4-methoxyphenyl, 4-bromo-3-hydroxyphenyl, 4-fluoro-3-hydroxyphenyl, 4-chloro-3-hydroxyphenyl, 3-hydroxy-4-methylphenyl, 3-hydroxy-4-methoxyphenyl et 4-cyano-2-fluorophenyl) ; et les sels en, les processus pour leur préparation et compositions pharmaceutiques contenant un composé de la formule (i) ou un sel pharmaceutiquement acceptable en en tant que substance active les composés de la formule (i) et les sels pharmaceutiquement acceptables empêchent en les effets de VEGF, une propriété de valeur dans le traitement d'un certain nombre d'états de la maladie comprenant le cancer et le ## du ## STR1 de rhumatisme articulaire