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
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 3, 1 February 2012, Pages 1433–1438
نویسندگان
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,