N-benzylindole modulators of PPARG

US9051265B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9051265-B2
Application numberUS-201213490342-A
CountryUS
Kind codeB2
Filing dateJun 6, 2012
Priority dateJun 6, 2011
Publication dateJun 9, 2015
Grant dateJun 9, 2015

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  2. Abstract

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Abstract

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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.

First claim

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…

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What does patent US9051265B2 cover?
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…
Who is the assignee on this patent?
Kamenecka Theodore Mark, Griffin Patrick R, Koenig Marcel, and 5 more
What technology area does this patent fall under?
Primary CPC classification C07D209/42. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Jun 09 2015 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).