Invention Grant
- Patent Title: N-biphenylmethylbenzimidazole modulators of PPARG
- Patent Title (中): PPARG的N-联苯甲基苯并咪唑调节剂
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Application No.: US13811965Application Date: 2012-11-20
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Publication No.: US09309227B2Publication Date: 2016-04-12
- Inventor: Theodore Mark Kamenecka , Patrick R. Griffin , Amy S. Ripka , Jeffrey O. Saunders
- Applicant: The Scripps Research Institute , Ember Therapeutics, Inc.
- Applicant Address: US CA La Jolla US MA Boston
- Assignee: The Scripps Research Institute,Ember Therapeutics, Inc.
- Current Assignee: The Scripps Research Institute,Ember Therapeutics, Inc.
- Current Assignee Address: US CA La Jolla US MA Boston
- Agency: Schwegman Lundberg & Woessner, P.A.
- International Application: PCT/US2012/066135 WO 20121120
- International Announcement: WO2013/078240 WO 20130530
- Main IPC: C07D235/08
- IPC: C07D235/08 ; C07D403/10 ; C07D235/06 ; C07D401/06 ; C07D401/10 ; A61K31/4184 ; A61K31/4439 ; A61K45/06
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.
Public/Granted literature
- US20150141464A1 N-BIPHENYLMETHYLBENZIMIDAZOLE MODULATORS OF PPARG Public/Granted day:2015-05-21
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