4-aminopyrimidine-5-one

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/12 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) C07D 239/48 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 413/14 (2006.01)

Patent

CA 2512915

Novel 4-aminopyrimidine-5-one derivatives of the formula (I) wherein R1 and R2 are as defined in the specification, are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds, their use for treating or controlling cancer, to a process of their preparation and to intermediates useful in their preparation.

La présente invention a trait à de nouveaux dérivés de 4-aminopyrimidine-5-one de formule (I), dans laquelle R?1¿ et R?2¿ sont tels que définis dans la description. Ces composés sont inhibiteurs de la kinase dépendante des cyclines, notamment de la kinase 4 dépendante des cyclines (Cdk4). Ces composés et leurs sels et esters pharmaceutiquement acceptables présentent une activité antiproliférative et sont utiles dans le traitement ou le contrôle du cancer, en particulier des tumeurs solides. La présente invention a également trait à des compositions pharmaceutiques contenant de tels composés, leur utilisation pour le traitement et le contrôle du cancer, à leur procédé de préparation et à des intermédiaires utiles dans leur préparation.

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