6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as...

Details 6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as... 6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as...

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/505 (2006.01) A61P 35/00 (2006.01) C07D 231/00 (2006.01) C07D 239/00 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2345809

The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

La présente invention concerne la synthèse d'une nouvelle classe de pyrazolo[3,4-d]pyrimidin-4-ones correspondant à la formule (I) et représentés en variante par le tautomère (II): Ces composés sont des inhibiteurs puissants de la classe d'enzymes connues sous le nom de kinases dépendantes des cyclines. L'invention se rapporte aux unités catalytiques de kinases dépendantes des cyclines 1-8 et à leurs sous-unités régulatrices connues sous le nom de cyclines A-H, K, N et T. L'invention concerne aussi un nouveau procédé pour traiter le cancer ou d'autres maladies proliférantes par l'administration d'une quantité thérapeutiquement efficace d'un de ces composés ou d'un de leurs sels pharmaceutiquement acceptables. En variante, on peut traiter le cancer ou d'autres maladies proliférantes par l'administration d'une combinaison thérapeutiquement efficace d'un des composés de l'invention et d'un ou de plusieurs agents anticancéreux ou antiproliférants connus.

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