Sulphonamine compounds and methods of making and using same
US-9221787-B2 · Dec 29, 2015 · US
US9051265B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9051265-B2 |
| Application number | US-201213490342-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 6, 2012 |
| Priority date | Jun 6, 2011 |
| Publication date | Jun 9, 2015 |
| Grant date | Jun 9, 2015 |
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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.
Opening claim text (preview).
What is claimed is: 1. A non-agonist peroxisome proliferator active receptor gamma (PPARG) modulatory compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: R is H, (C 1 -C 6 )alkyl, (C 3 -C 9 )cycloalkyl, or (C 1 -C 6 )haloalkyl; R′ is independently H, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, or (C 3 -C 9 )cycloalkyl; each X is independentl…
Human Necessities · mapped topic
Human Necessities · mapped topic
Human Necessities · mapped topic
Chemistry & Metallurgy · mapped topic
Human Necessities · mapped topic
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