Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1361504 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
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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Authors
Véronique Plantevin Krenitsky, Lisa Nadolny, Mercedes Delgado, Leticia Ayala, Steven S. Clareen, Robert Hilgraf, Ronald Albers, Sayee Hegde, Neil D’Sidocky, John Sapienza, Jonathan Wright, Meg McCarrick, Sogole Bahmanyar, Philip Chamberlain,