Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), 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.
Type:
Grant
Filed:
November 20, 2012
Date of Patent:
April 12, 2016
Assignees:
The Scripps Research Institute, Ember Therapeutics, Inc.
Inventors:
Theodore Mark Kamenecka, Patrick R. Griffin, Amy S. Ripka, Jeffrey O. Saunders
Abstract: Beige cells that contain a reporter gene are disclosed herein. Such cells can be used to identify therapeutic agents for treatment of obesity and its associated disorders, such as diabetes.