Aleglitazar, a new, potent, and balanced dual PPARα/γ agonist for the treatment of type II diabetes

…, A Binggeli, D Blum, M Boehringer, U Grether…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 9 p. 2468 - 2473

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Citation Number: 77

Abstract

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.