Bicyclic pyrimidine pi3k inhibitor compounds selective for...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 9/00 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) C07D 491/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2761445

Formula (I) ((Ia) and (Ib)) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

L'invention porte sur des composés de Formule (I) ((Ia) et(Ib)), où (i) X1 représente N et X2 représente S, (ii) X1 représente CR7 et X2 représente S, (iii) X1 représente N et X2 représente NR2, ou (iv) X1 représente CR7 et X2 représente O, comprenant des stéréo-isomères, des tautomères, des métabolites et des sels pharmaceutiquement acceptables de ceux-ci, lesquels composés sont utiles pour inhiber l'isoforme delta de PI3K, et pour traiter des troubles à médiation par des lipides kinases, tels qu'une inflammation, une maladie immunologique et un cancer. L'invention porte sur des procédés d'utilisation des composés de Formule (I) pour un diagnostic in vitro, in situ et in vivo, une prévention ou un traitement de tels troubles dans des cellules de mammifère, ou des états pathologiques associés.

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