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Published on: May 15, 2019
Chromanol derivatives--a novel class of CETP inhibitors
Alexandros Vakalopoulos1, Carsten Schmeck, Michael Thutewohl
1Bayer HealthCare AG, Bayer Schering Pharma, Global Drug Discovery, D-42096 Wuppertal, Germany. alexandros.vakalopoulos@bayer.com
Abstract:
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.
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