Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors
This letter describes the discovery and SAR optimization of tetrazoyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m exhibited robust HDL-c increase in hCETP/hApoA1 double transgenic model and favorable pharmacokinetic properties.
Escribano, Ana,Mateo, Ana I.,Martin De La Nava, Eva M.,Mayhugh, Daniel R.,Cockerham, Sandra L.,Beyer, Thomas P.,Schmidt, Robert J.,Cao, Guoqing,Zhang, Youyan,Jones, Timothy M.,Borel, Anthony G.,Sweetana, Stephanie A.,Cannady, Ellen A.,Mantlo, Nathan B.
scheme or table
p. 3671 - 3675
(2012/07/16)
Asymmetric synthesis of the cholesteryl ester transfer protein inhibitor torcetrapib
Previously our group reported synthetic efforts used to synthesize kilogram quantities of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, 1, via a mid-stage resolution. This account describes research conducted to develop an asymmetri
Damon, David B.,Dugger, Robert W.,Hubbs, Stephen E.,Scott, Jill M.,Scott, Robert W.
p. 472 - 480
(2012/12/22)
Intermediates of CETP inhibitors
This invention relates to intermediates useful in the preparation of CETP inhibitors and methods of preparation thereof.
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(2008/06/13)
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