title: Chromanol derivatives--a novel class of CETP inhibitors.
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.
authors.affiliation: Bayer HealthCare AG, Bayer Schering Pharma, Global Drug Discovery, D-42096 Wuppertal, Germany. alexandros.vakalopoulos@bayer.com
authors.forename: Alexandros
authors.initials: A
authors.lastname: Vakalopoulos
authors.forename: Carsten
authors.initials: C
authors.lastname: Schmeck
authors.forename: Michael
authors.initials: M
authors.lastname: Thutewohl
authors.forename: Volkhart
authors.initials: V
authors.lastname: Li
authors.forename: Hilmar
authors.initials: H
authors.lastname: Bischoff
authors.forename: Klemens
authors.initials: K
authors.lastname: Lustig
authors.forename: Olaf
authors.initials: O
authors.lastname: Weber
authors.forename: Holger
authors.initials: H
authors.lastname: Paulsen
authors.forename: Harry
authors.initials: H
authors.lastname: Elias
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008076:Cholesterol, HDL / Q000378:metabolism; D002839:Chromans / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D004285:Dogs; D006801:Humans; D051379:Mice; D008822:Mice, Transgenic; D051381:Rats; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship
chemical_list: D001578:Benzopyrans; D053480:Cholesterol Ester Transfer Proteins; D008076:Cholesterol, HDL; D002839:Chromans; D013141:Spiro Compounds; C029141:2,2,5,7,8-pentamethyl-1-hydroxychroman