99450-00-7Relevant articles and documents
Benzoyl 2-methyl indoles as selective PPARγ modulators
Acton III, John J.,Black, Regina M.,Jones, A. Brian,Moller, David E.,Colwell, Lawrence,Doebber, Thomas W.,MacNaul, Karen L.,Berger, Joel,Wood, Harold B.
, p. 357 - 362 (2005)
A series of selective PPARγ modulators (SPPARγMs) and their development from hPPARγ active screening leads 1 and 2 is described. SPPARγM 24 displayed robust anti-diabetic activity with an improved therapeutic window in comparison to a PPARγ full agonist in a rodent efficacy model. Routine screening for human PPAR ligands yielded compounds 1 and 2, both of which were sub-micromolar hPPARγ agonists. Synthetic modifications of these leads led to a series of potent substituted 3-benzyl-2-methyl indoles, a subset of which were noted to be selective PPARγ modulators (SPPARγMs). SPPARγM 24 displayed robust anti-diabetic activity with an improved therapeutic window in comparison to a PPARγ full agonist in a rodent efficacy model.
Orally effective inotropic compounds
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, (2008/06/13)
A method for increasing cardiac contractility in a warm-blooded animal suffering from acutely depressed cardiac contractility which comprises administering to said animal an effective amount of a compound of the formula STR1 wherein R is hydrogen or isobu
