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

被引：181

作者：

He, W ^{[1
]}

Myers, MR ^{[1
]}

Hanney, B ^{[1
]}

Spada, AP ^{[1
]}

Bilder, G ^{[1
]}

Galzcinski, H ^{[1
]}

Amin, D ^{[1
]}

Needle, S ^{[1
]}

Page, K ^{[1
]}

Jayyosi, Z ^{[1
]}

Perrone, MH ^{[1
]}

机构：

[1] Aventis Pharmaceut, Bridgewater, NJ 08807 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(03)00655-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3097 / 3100

页数：4

共 11 条

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