852814-92-7Relevant academic research and scientific papers
The discovery of equipotent PPARα/γ dual activators
Martres, Paul,Faucher, Nicolas,Laroze, Alain,Pineau, Olivier,Fouchet, Marie Helene,Potvain, Florent,Grillot, Didier,Beneton, Veronique
supporting information; experimental part, p. 6251 - 6254 (2009/07/18)
We report the design and synthesis of equipotent PPARα/γ dual agonists starting from selective PPAR alpha agonist 1. In vivo data for 7 in the Zucker fa/fa rat are presented.
Development of a scalable synthesis of GSK183390A, a PPAR α/γ agonist
Oh, Lynette M.,Wang, Huan,Shilcrat, Susan C.,Hermann, Robert E.,Patience, Daniel B.,Spoors, P. Grant,Sisko, Joseph
, p. 1032 - 1042 (2012/12/30)
A scalable synthesis of GSK183390A, a PPAR α/γ agonist, is described. This synthesis is highlighted by (1) a regioselective formal 1,3-dipolar cycloaddition reaction between an enamine and a nitrile inline dipole to form a 1,3,5-trisubstmited pyrazole and (2) a regioselective amidomethylation of an o-cresol derivative using 2-chloro-JV- hydroxymethylacetamide.
SUBSTITUTED PYRAZOLES AS PPAR AGONISTS
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Page/Page column 159, (2010/02/12)
A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof (I) wherein: p is O or 1; q is O or 1; R1 and R2 are independently H or C1-3 alkyl; R3 and R4 are independently H, C1-6 alkyl, -OC1-6 alkyl, halogen, OH, C2-6 alkenyl or CF3; R5 is H, C1-6 alkyl (optionally substituted by one or more halogens, -COphenyl, OC1-6 alkyl, phenyl morpholino or C2-6 alkenyl. R6 is C1-6 alkyl, halogen, -OCH2 phenyl, phenyl (optionally substituted by C1-3 alkiyl), morpholino, pyrrolidino, piperidino, thiophenyl, furanyl pyridinyl or -OC2-6 alkenyl. These compounds activate the alpha and gamma subtypes fo the hppar receptor and are useful e.g. in the treatment of diabetes, dyslipidemia or syndrome X.
