2004 Enzyme inhibiting activity

Enzyme inhibiting activityX 0220 Potent Quinoxaline-Based Inhibitors of PDGF Receptor Tyrosine Kinase Activity.

Part 2. The Synthesis and Biological Activities of RPR127963 an Orally Bioavail-able Inhibitor. — The highly optimized PDGF-R tyrosine kinase inhibitor (I) exhibits and excellent pharmacokinetic profile in several species and demonstrates efficacy in an animal model of restenosis. The oral activity of (I) at a relatively low dose and a chronic administration represents a major improvement over the prototype RPR101511. — (HE*, W.; et al.; Bioorg. Med. Chem. Lett. 13 (2003) 18, 3097-3100; Aventis Pharm., Bridgewater, NJ 08807, USA; Eng.) — H. Hoennerscheid

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