- (1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3 -b)indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A Potent and Highly Selective Cathepsin K Inhibitor for the Treatment of Osteoarthritis
[作者:DOSSETTER ALEXANDER G; BEELEY HOWARD; BOWYER JONATHAN; COOK CALUM R; CRAWFORD JAMES J; FINLAYSON JONATHAN E; HERON NICOLA M; HEYES CHRISTINE; HIGHTON ADRIAN J; HUDSON JULIAN A; JESTEL ANJA; KENNY PETER W; KRAPP STEPHAN; MARTIN SCOTT; MACFAUL PHILIP A; MCGUIRE THOMAS M; GUTIERREZ PABLO MORENTIN; MORLEY ANDREW D; MORRIS JEFFREY J; PAGE KEN M; RIBEIRO LYN ROSENBRIER; SAWNEY HELEN; STEINBACHER STEFAN; SMITH CAROLINE; VICKERS MADELEINE,期刊:Journal of Medicinal Chemistry, 页码:6363-6374 , 文章类型: Article,,卷期:2012年55-14]
- Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. Synthesis of compounds with reduced molecular complexity, s...
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