A novel set of azepine compounds were designed and synthesized as small-molecule inhibitors of JAK2.  Further optimization of the azepine lead led to the discovery of INCB016562, an orally bioavailable and JAK2 selective inhibitor.   Treatment with once daily doses of INCB016562 in a MPLW515L-dependent murine model of essential thrombocytosis (ET) and primary myelofibrosis (PMF) demonstrated normalized white blood cell counts and platelet counts while improving myelofibrosis and survival compared to vehicle controls.

Azepine inhibitors of JAK2

244th National Meeting (2012)

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