Bayer HealthCare AG, Bayer Schering Pharma, Global Drug Discovery, D-42096 Wuppertal, Germany.
Bioorg Med Chem Lett. 2011 Jan 1;21(1):488-91. doi: 10.1016/j.bmcl.2010.10.110. Epub 2010 Oct 26.
Based on our former development candidate BAY 38-1315, optimization efforts led to the discovery of a novel chemical class of orally active cholesteryl ester transfer protein (CETP) inhibitors. The chromanol derivative 19b is a highly potent CETP inhibitor with favorable pharmacokinetic properties suitable for clinical studies. Chemical process optimization furnished a robust synthesis for a kilogram-scale process.
基于我们之前的开发候选物 BAY 38-1315，优化工作导致发现了一类新型的具有口服活性的胆固醇酯转移蛋白（CETP）抑制剂。色满醇衍生物 19b 是一种高效的 CETP 抑制剂，具有适合临床研究的良好药代动力学特性。通过化学工艺优化，实现了公斤级规模的稳定合成。
