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Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8. doi: 10.1016/j.bmcl.2011.12.027. Epub 2011 Dec 10.

Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.

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Celgene Corporation, 4550 Towne Centre Court, San Diego, CA 92121, USA.


In this Letter we describe the discovery of potent, selective, and orally active aminopurine JNK inhibitors. Improving the physico-chemical properties as well as increasing the potency and selectivity of a subseries with rat plasma exposure, led to the identification of four structurally diverse inhibitors. Differentiation based on PK profiles in multiple species as well as activity in a chronic efficacy model led to the identification of 1 (CC-930) as a development candidate, which is currently in Phase II clinical trial for IPF.

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