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Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K |
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| Authors: | Barrett David G Catalano John G Deaton David N Long Stacey T Miller Larry R Tavares Francis X Wells-Knecht Kevin J Wright Lois L Zhou Hui-Qiang Q |
| Affiliation: | Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. |
| Abstract: | An orally available series of ketoamide-based inhibitors of cathepsin K has been identified. Starting from a potent inhibitor with poor oral bioavailability, modifications to P1 and P1' elements led to enhancements in solubility and permeability. These improvements resulted in orally available cathepsin K inhibitors. |
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