کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1361504 981465 2012 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor
چکیده انگلیسی

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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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 3, 1 February 2012, Pages 1433–1438
نویسندگان
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