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Chromanol derivatives—A novel class of CETP inhibitors

✍ Scribed by Alexandros Vakalopoulos; Carsten Schmeck; Michael Thutewohl; Volkhart Li; Hilmar Bischoff; Klemens Lustig; Olaf Weber; Holger Paulsen; Harry Elias


Book ID
104005060
Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
305 KB
Volume
21
Category
Article
ISSN
0960-894X

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✦ Synopsis


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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