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Bioorg Med Chem Lett. 2003 Sep 15;13(18):3097-100.

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

Author information

1
Aventis Pharmaceuticals, Route 202/206, Brigdewater, NJ 08807, USA.

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.

PMID:
12941342
DOI:
10.1016/s0960-894x(03)00655-3
[Indexed for MEDLINE]

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