Selective Modulators of PPAR-gamma and Methods for the Use Thereof

Inventors: Ron Evans and Barry Forman
Potential Uses: Cardiovascular, Obesity, Drug Discovery and Development
Use of PPAR-gamma-selective compounds for the treatment of obesity and diabetes.

Because obesity is associated with the development of serious medical conditions, including noninsulin-dependent diabetes mellitus, hypertension, coronary artery disease, hyperlipidemias and certain malignancies, it is important that compounds to control adiposity are identified. The conversion of fibroblasts into cells of the adipose lineage is induced by expression of the orphan nuclear receptor PPAR-gamma. Accordingly, an endogenous PPAR-gamma ligand may be an important regulator of adipogenesis. This invention reveals PPAR-gamma as a drug target and relates to a class of compounds which are capable of selectively modulating processes mediated by PPAR-gamma. The identification of such compounds makes possible the selective intervention in PPAR-gamma mediated pathways, without exerting inadvertent effects on pathways mediated by other PPAR isoforms.