Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable …

…, B Hanney, AP Spada, G Bilder, H Galzcinski…

Index: He, Wei; Myers, Michael R.; Hanney, Barbara; Spada, Alfred P.; Bilder, Glenda; Galzcinski, Helen; Amin, Dilip; Needle, Saul; Page, Ken; Jayyosi, Zaid; Perrone, Mark H. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 18 p. 3097 - 3100

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Citation Number: 153

Abstract

RPR127963 demonstrates an excellent pharmacokinetic profile in several species and was found to be efficacious in the prevention of restenosis in a Yucatan mini-pig model upon oral administration of 1–5 mg/kg. The in vitro selectivity profile and SAR of the highly optimized PDGF-R tyrosine kinase inhibitor are highlighted.