Quinazoline derivatives, process for their preparation,...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/78 (2006.01) A61K 31/505 (2006.01) A61P 35/00 (2006.01) C07D 239/82 (2006.01)

Patent

CA 2586602

The invention relates to quinazoline derivatives of formula (I), in which R1, X and A have the meanings as indicated, or to a pharmaceutically acceptable salt thereof, e.g. (formula II). Such compounds are useful as modulators, in particular inhibitors, of the mitotic kinesin Eg5. i.e. the human protein (also called KSP), the Xenopus laevis homologue, further homologues from other species as well as allelic variants and functionally related proteins. The invention also relates to processes for their preparation, pharmaceutical compositions comprising said quinazoline derivatives, and the use of said quinazoline derivatives, in particular for treating diseases such as cancer.

L'invention concerne des dérivés de quinazoline représentés par la formule (I), dans laquelle R1, X et A sont tels que représentés dans le descriptif, ou un sel pharmaceutiquement acceptable de ceux-ci, par exemple (formule II). Ces composés sont utilisés comme modulateurs, en particulier comme inhibiteurs, de la kinésine mitotique Eg5, à savoir la protéine humaine (également appelée KSP), l'homologue de Xenopus laevis, d'autres homologues provenant d'autres espèces ainsi que des variants alléliques et des protéines fonctionnellement apparentées. Par ailleurs, l'invention concerne des procédés de préparation de ces dérivés de quinazoline, des compositions pharmaceutiques contenant ces dérivés de quinazoline, ainsi que l'utilisation de ces dérivés de quinazoline, en particulier pour traiter des maladies telles que le cancer.

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