Vertex inhibitors of Aurora-2, glycogen synthase kinase-3 and Src kinase

Abstract

Four patent applications from Vertex have recently been published relating to inhibitors of protein kinases. The compounds described in this invention are claimed as inhibitors of Aurora-2, glycogen synthase kinase-3 (GSK-3), and Src protein kinases. The applications are highly homologous, in that an identical set of five core templates are described as especially preferred in each of the four applications. The compounds are differentiated from one another by the substituent off of the 4-amino position of the core template. A series of 30 – 40 representative compounds are provided for each application but none are described as especially preferred and no biological data are provided for any of these representative compounds. These recent publications signal a continued interest by Vertex in pan-inhibitors of Aurora-2, GSK-3 and Src.

• Aurora-2
• glycogen synthase kinase-3 (GSK-3)
• kinase inhibitor
• quinazoline
• Src
• Vertex