1706-60-1Relevant academic research and scientific papers
Synthesis of the PPARβ/δ-selective agonist GW501516 and C4-thiazole-substituted analogs
Pereira, Raquel,Gaudon, Claudine,Iglesias, Beatriz,Germain, Pierre,Gronemeyer, Hinrich,De Lera, Angel R.
, p. 49 - 54 (2007/10/03)
Sequential, position-selective, Pd-catalyzed cross-coupling reactions of 2,4-dibromo-5-hydroxymethylthiazole provided the scaffold for the synthesis of GW501516, the most potent PPARβ/δ agonist yet described, and equally selective analogs at the thiazole-
Insights into the mechanism of the site-selective sequential palladium-catalyzed cross-coupling reactions of dibromothiophenes/ dibromothiazoles and arylboronic acids. Synthesis of PPARβ/δ agonists
Pereira, Raquel,Furst, Audrey,Iglesias, Beatriz,Germain, Pierre,Gronemeyer, Hinrich,De Lera, Angel R.
, p. 4514 - 4525 (2008/09/19)
A reactivity study, aided by NMR spectroscopy, allowed a mechanistic rationale to be postulated for the palladium-catalyzed regioselective coupling of arylboronic acid (and arylstannane where feasible) at the position next to the sulfur atom in functional
Compounds that modulate PPAR activity and methods of preparation
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, (2008/06/13)
This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.
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.
Compounds that modulate PPAR activity and methods for their preparation
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Page 84, (2010/02/05)
This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disipidemia, hypercholesteremia, obesity, eating disorders, hyperglycemia, atherosclerosis, hypertriglyceridemia, hyperinsulinemia and diabetes in a mammal as well as methods of supressing appetite and modulating leptin levels in a mammal. The present invention also discloses methods for making the disclosed compounds.
