4-phenylamino-quinazolin-6-yl-amides

Details 4-phenylamino-quinazolin-6-yl-amides 4-phenylamino-quinazolin-6-yl-amides

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 31/517 (2006.01) A61P 35/00 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01)

Patent

CA 2565812

The invention provides quinazoline compounds of the formula: wherein R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) -(CH2)n-morpholino, -(CH2)n-piperidine, -(CH2)n-piperazine, -(CH2)n- piperazine-N(C1-C3 alkyl), -(CH2)n-pyrrolidine, or -(CH2)n imidazole; n is 1 to 4; R4 is -(CH2)m-Het; Het is morpholine,piperidine, piperazine, piperazine- N(C1-C3 alkyl), imidazole,pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N (C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.

La présente invention a trait à des composés de quinazoline de formule (I), dans laquelle: R¿1? est halo; R¿2? est H ou halo; R¿3? est a) alkyle en C¿1?-C¿3?, éventuellement substitué par halo; ou b) -(CH¿2?)¿n?-morpholino, -(CH¿2?)¿n?-pipéridine, -(CH¿2?)¿n?-pipérazine-N(alkyle en C¿1?-C¿3?), -(CH¿2?)¿n?-pyrrolidine, ou -(CH¿2?)¿n?-imidazole; n est 1 à 4; R¿4? est -(CH¿2?)¿m?-Het; Het est morpholine, pipéridine, pipérazine, pipérazine-N(alkyle en C¿1?-C¿3?), imidazole, pyrrolidine, azépane, 3,4-dihydro-2H-pyridine, ou 3,6-dihydro-2H-pyridine, chacun éventuellement substitué par alkyle ou halo, OH, NH¿2?, NH(alkyle en C¿1?-C¿3?) ou N (alkyle en C¿1?-C¿3?)¿2?; m est 1 à 3; et X est O, S ou NH; ou un sel pharmaceutiquement acceptable de ceux-ci, ainsi qu'à des procédés et des composés intermédiaires pour leur fabrication, à des compositions pharmaceutiques utiles et des procédés d'utilisation des composés dans le traitement de maladies proliférantes.

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