Phosphoinositide 3-kinase inhibitor compounds and methods of...

C - Chemistry – Metallurgy – 07 – D

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C07D 491/048 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2671845

Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. Formula (Ic) and (Id).

La présente invention concerne des composés de formules Ia à Id où X représente S ou O, mor représente un groupe morpholine, et R3 représente un groupe hétéroaryle monocyclique, et y compris les stéréoisomères, les isomères géométriques, les tautomères, les solvates, les métabolites et les sels pharmaceutiquement acceptables de ceux-ci. Lesdits composés sont utiles pour moduler l'activité de kinases lipidiques comprenant la PI3K, et pour traiter des maladies telles que le cancer provoqué par les kinases lipidiques. L'invention concerne également des procédés d'utilisation des composés de formules Ia à Id pour le diagnostic in vitro, in situ, et in vivo, la prévention ou le traitement de telles maladies dans les cellules de mammifères, ou les conditions pathologiques associées. Formules (Ic) et (Id).

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