1. Academic Validation
  2. Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes

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

  • Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73. doi: 10.1016/j.bmcl.2009.03.036.
Agnes Bénardeau 1 Jörg Benz Alfred Binggeli Denise Blum Markus Boehringer Uwe Grether Hans Hilpert Bernd Kuhn Hans Peter Märki Markus Meyer Kurt Püntener Susanne Raab Armin Ruf Daniel Schlatter Peter Mohr
Affiliations

Affiliation

  • 1 F. Hoffmann-La Roche Ltd, Pharma Research, CH-4070 Basel, Switzerland.
Abstract

Design, synthesis, and SAR of novel alpha-alkoxy-beta-arylpropionic acids as potent and balanced PPARalphagamma 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.

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