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
scheme or table
p. 2468 - 2473
(2010/03/24)
Process for the production of chiral propionic acid derivatives
The present invention is concerned with a novel process for the preparation of compounds of formula I comprising catalytic asymmetric hydrogenation of a compound of formula (II) in the presence of a catalyst comprising ruthenium and a chiral diphosphine ligand or comprising rhodium and a chiral diphosphine ligand, wherein R1, R2, R3 and R4 are as defined in the specification and claims. The compounds of formula I and the corresponding salts and/or esters are pharmaceutically active substances.
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Page/Page column 13-14
(2010/02/11)
Novel process for the preparation of the insulin sensitizer
A novel process for the preparation of compounds of formula I and optionally converting a compound of formula I into a pharmaceutically acceptable salt is disclosed. The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharma
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Page 6
(2010/02/10)
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