N-benzylindole modulators of PPARG
US9051265B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 6, 2012 |
| Grant date | Jun 9, 2015 |
| Priority date | — |
| Expiry date | Jun 6, 2032 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D419/12
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), and 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. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal 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.