1.
Bioorg Med Chem Lett
; 22(3): 1433-8, 2012 Feb 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-22244937
RESUMEN
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.