Pyrazolopyrimidines as pi3k lipid kinase inhibitors

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01)

Patent

CA 2664378

The invention relates to novel - at least 3,5-disubstituted - pyrazolo[1,5-a]pyrimidines of the formula (I), wherein the symbols R1 to R4 are as defined in the specification, tautomers thereof or N-oxides thereof, or (preferably pharmaceutically acceptable) salts thereof, or hydrates or solvates thereof, as well as to related embodiments. The compounds are useful inter alia as protein kinase inhibitors, and thus e.g. useful in the treatment of diseases that respond to an inhibition of kinases of the PI3-kinase-related protein kinase family, especially lipid kinases and/or PI3 kinase (PI3K) and/or mTOR and/or DNA protein kinase and/or ATM and/or ATR and/or hSMG-1.

Cette invention concerne de nouvelles pyrazolo[1,5-a]pyrimidines au moins 3,5-disubstituées représentées par la formule (I) dans laquelle les symboles R1 à R4 sont tels que définis dans la description, ou des tautomères, des N-oxydes, des sels (de préférence pharmaceutiquement acceptables), des hydrates ou des solvates de celles-ci, ainsi que des modes de réalisation associés. Ces composés sont notamment utilisés comme inhibiteurs de protéines kinases et peuvent de ce fait servir à traiter des maladies sensibles à une inhibition de kinases de la famille des protéines kinases associées à la Pl3 kinase, en particulier de lipides kinases et/ou de la kinase Pl3 (Pl3K) et/ou de la voie mTOR et/ou de la protéine kinase dépendante de l'ADN et/ou de la kinase ATM et/ou de la kinase ATR et/ou de la protéine hSMG-1.

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