C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 239/94 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 403/12 (2006.01)
Patent
CA 2215732
The invention concerns quinazoline derivatives of the formula (I) wherein n is 1, 2 or 3 and each R2 is independently halogeno, trifluoromethyl or (1- 4C)alkyl; R3 is (1-4C)alkoxy; and R1 is di-[(1-4C)alkyl]amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2- 4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2- 4C)alkoxy, imidazol-1-yl-(2-4C)alkoxy, di-[(1-4C)alkoxy-(2-4C)alkoxyl]amino-(2- 4C)alkoxy, thiamorpholino-(2-4C)alkoxy, 1-oxothiamorpholino-(2-4C)alkoxy or 1,1-dioxothiamorpholino-(2-4C)alkoxy, and wherein any of the above-mentioned R1 substituents comprising a CH2 (methylene) group which is not attached to a N or O atom optionally bears on said CH2 group a hydroxy substituent; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.
L'invention concerne des dérivés de quinazoline de formule (I) ou des sels pharmaceutiquement acceptables de ceux-ci. Dans la formule (I), n vaut 1, 2 ou 3 et chaque R?2¿ représente séparément halogéno, trifluorométhyle ou alkyle (1-4C); R?3¿ représente alcoxy (1-4C); et R?1¿ représente di[alkyl(1-4C)]amino-alcoxy(2-4C), pyrrolidin-1-yl-alcoxy(2-4C), pipéridino-alcoxy(2-4C), morpholino-alcoxy(2-4C), pipérazin-1-yl-alcoxy(2-4C), 4-alkylpipérazin(1-4C)-1-yl-alcoxy(2-4C), imidazol-1-yl-alcoxy(2-4C), di[alcoxy(1-4C)-alkyl(2-4C)]amino-alcoxy(2-4C), thiamorpholino-alcoxy(2-4C), 1-oxothiamorpholino-alcoxy(2-4C) ou 1,1-dioxothiamorpholino-alcoxy(2-4C), et dans laquelle les substituants de ¿R?1¿ susmentionnés comprenant un groupe CH¿2?(méthylène) qui n'est pas attaché à un atome N ou O porte éventuellement sur ledit groupe CH¿2? un substituant hydroxy. L'invention porte aussi sur des procédés de préparation desdits composés, des compositions pharmaceutiques les contenant et l'utilisation des propriétés inhibitrices de la tyrosine-kinase réceptrice du composé dans le traitement de maladies prolifératives telles que le cancer.
Astrazeneca Uk Limited
Smart & Biggar
Zeneca Limited
LandOfFree
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