N-biphenylmethylindole modulators of PPARG
US8957093B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 6, 2012 |
| Grant date | Feb 17, 2015 |
| Priority date | — |
| Expiry date | Jun 6, 2032 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D493/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit kinase-mediated, e.g., 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, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.