Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2‑f][1,2,4]triazine-6-carbonyl)­(propyl)­carba­moyl­oxy)­methyl-2-(4-(phos­pho­no­oxy)­phenyl)­acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor

In search for prodrugs to address the issue of pH-dependent solubility and exposure associated with 1 (BMS-582949), a previously disclosed phase II clinical p38α MAP kinase inhibitor, a structurally novel clinical prodrug, 2 (BMS-751324), featuring a carbamoylmethylene linked promoiety containing hy...

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Veröffentlicht in:	Journal of medicinal chemistry 2015-10, Vol.58 (19), p.7775-7784
Hauptverfasser:	Liu, Chunjian, Lin, James, Hynes, John, Wu, Hong, Wrobleski, Stephen T., Lin, Shuqun, Dhar, T. G. Murali, Vrudhula, Vivekananda M., Sun, Jung-Hui, Chao, Sam, Zhao, Rulin, Wang, Bei, Chen, Bang-Chi, Everlof, Gerry, Gesenberg, Christoph, Zhang, Hongjian, Marathe, Punit H., McIntyre, Kim W., Taylor, Tracy L., Gillooly, Kathleen, Shuster, David J., McKinnon, Murray, Dodd, John H., Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina
Format:	Artikel
Sprache:	eng
Online-Zugang:	Volltext
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