A novel set of macrocyclic compounds were designed and synthesized and were found to be very potent inhibitors of a number of kinases including janus kinases (JAKs).  The macrocycles are based on a diaminopyrimidine scaffold that was constrained to maximize binding affinity.  The goal of maintaining or increasing biological activity in a locked conformation was achieved by varying the type of linker and the length of the linker.  The discovery and SAR of these macrocycles will be described.

Macrocyclic inhibitors of JAK

244th National Meeting (2012)

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