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Chromanol derivatives emerge as a novel class of orally active CETP inhibitors suitable for clinical development (Bioorg Med Chem Lett 2011)

Original title: Chromanol derivatives--a novel class of CETP inhibitors

Bioorg Med Chem Lett · · 4

Vakalopoulos A, Schmeck C, Thutewohl M, Li V, Bischoff H, Lustig K, Weber O, Paulsen H, Elias H

Building on the earlier development candidate BAY 38-1315, optimisation work led to the discovery of chromanol derivatives as a novel chemical class of orally active CETP inhibitors. The lead compound, chromanol derivative 19b, is a highly potent CETP inhibitor with pharmacokinetic properties favourable for clinical studies. Chemical process optimisation also produced a robust, scalable synthesis suitable for kilogram-scale production.

Read the paper (DOI)PubMed

Original 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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Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.