Evaluation of WO2012037204 and WO2012037226: Exelixis' selective PI3Kδ inhibitors; the basis of a US$251 million deal

Abstract

Two applications each claim compounds described as selective PI3Kδ inhibitors. The first claims 2-amino-3-substituted-8-methylquinoline derivatives. The second, more substantial, application claims a broad range of cyclic amine derivatives of 6-aminopurines. These are the first patent applications from Exelixis relating to its PI3Kδ inhibitor program despite its disclosure of the biological profile of its lead inhibitor XL-499 in late 2010.

Keywords::

• inflammation
• leukemia
• leukocyte
• lymphoma
• PI3Kδ inhibitor
• XL-499