Aleglitazar, a new, potent, and balanced dual PPARα/γ agonist for the treatment of type II diabetes
Design, synthesis, and SAR of novel α-alkoxy-β-arylpropionic acids as potent and balanced PPARαγ coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical development. Its X-ray structure in complex with both receptors as well as its high efficacy in animal models of T2D and dyslipidemia are also presented.
Benardeau, Agnes,Benz, Joerg,Binggeli, Alfred,Blum, Denise,Boehringer, Markus,Grether, Uwe,Hilpert, Hans,Kuhn, Bernd,Maerki, Hans Peter,Meyer, Markus,Puentener, Kurt,Raab, Susanne,Ruf, Armin,Schlatter, Daniel,Mohr, Peter
experimental part
p. 2468 - 2473
(2010/03/24)
Oxazole derivatives
The present invention relates to novel oxazole compounds which act as PPARα and PPARγ agonists and are accordingly useful for the treatment of diseases modulated by PPARα and PPARγ such as diabetes.
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(2008/06/13)
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