583883-82-3Relevant articles and documents
BENZOAZEPIN-OXY-ACETIC ACID DERIVATIVES AS PPAR-DELTA AGONISTS USED FOR THE INCREASE OF HDL-C, LOWER LDL-C AND LOWER CHOLESTEROL
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Page/Page column 43-44, (2008/06/13)
The invention is directed to compounds of Formula (I) useful as PPAR agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, diabetes, nephropathy, neuropathy, retinopathy, polycystic ovary syndr
Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ) - Synthesis and biological activity
Sznaidman, Marcos L.,Haffner, Curt D.,Maloney, Patrick R.,Fivush, Adam,Chao, Esther,Goreham, Donna,Sierra, Michael L.,LeGrumelec, Christelle,Xu, H. Eric,Montana, Valerie G.,Lambert, Millard H.,Willson, Timothy M.,Oliver Jr., William R.,Sternbach, Daniel D.
, p. 1517 - 1521 (2007/10/03)
We report the synthesis and biological activity of a new series of small molecule agonists of the human Peroxisome Proliferator-Activated Receptor δ (PPARδ). Several hits were identified from our original libraries containing lipophilic carboxylic acids. Optimization of these hits by structure-guided design led to 7k (GW501516) and 7l (GW0742), which shows an EC50 of 1.1 nM against PPARδ with 1000-fold selectivity over the other human subtypes.