1083287-06-2Relevant academic research and scientific papers
BENZOPIPERAZINE DERIVATIVES AS CETP INHIBITORS
-
Page/Page column 38, (2013/03/26)
Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
Synthesis and discovery of 2,3-dihydro-3,8-diphenylbenzo[1,4]oxazines as a novel class of potent cholesteryl ester transfer protein inhibitors
Wang, Aihua,Prouty, Catherine P.,Pelton, Patricia D.,Yong, Maria,Demarest, Keith T.,Murray, William V.,Kuo, Gee-Hong
scheme or table, p. 1432 - 1435 (2010/07/06)
2,3-Dihydro-3,8-diphenylbenzo[1,4]oxazines were identified as a new class of potent cholesteryl ester transfer protein inhibitors. The most potent compound 6a (IC50 = 26 nM) possessed a favorable pharmacokinetic profile with good oral bioavailability in rat (F = 53%) and long human liver microsome stability (t1/2 = 62 min). It increased HDL-C in human CETP transgenic mice and high-fat fed hamsters. The structure and activity relationship of this series will be described in this Letter.
