N-biphenylmethylbenzimidazole modulators of PPARG
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United States of America Patent
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Apr 12, 2016
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May 21, 2015
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Nov 20, 2012
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Nov 22, 2011
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Abstract
The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
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