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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 9051265 B1

PDFFull Text
Date of Patent:
Jun. 09, 2015

Filed:

Jun. 06, 2012

N-benzylindole modulators of pparg

Applicants:

Theodore Mark Kamenecka, Palm Beach Gardens, FL (US);

Patrick R. Griffin, Jupiter, FL (US);

Marcel Koenig, Palm Beach Gardens, FL (US);

Alice Asteian, Jupiter, FL (US);

Anne-laure Blayo, Jupiter, FL (US);

Yuanjun He, Palm Beach Gardens, FL (US);

Youseung Shin, Jupiter, FL (US);

Inventors:

Theodore Mark Kamenecka, Palm Beach Gardens, FL (US);

Patrick R. Griffin, Jupiter, FL (US);

Marcel Koenig, Palm Beach Gardens, FL (US);

Alice Asteian, Jupiter, FL (US);

Anne-Laure Blayo, Jupiter, FL (US);

Yuanjun He, Palm Beach Gardens, FL (US);

Youseung Shin, Jupiter, FL (US);

Assignee:

The Scripps Research Institute, La Jolla, CA (US);

Attorneys:

Geoffrey K. Cooper

Thomas Fitting

Primary Examiner:

Michael Barker

Assistant Examiner:

Po-Chih Chen

Int. Cl.
CPC ...
C07D 209/08 (2006.01); C07D 405/12 (2006.01); C07D 409/12 (2006.01); C07D 401/06 (2006.01); C07D 403/12 (2006.01); C07D 413/12 (2006.01); A61K 31/4439 (2006.01); A61K 31/497 (2006.01); A61K 31/41 (2006.01); A61K 31/4245 (2006.01); C07D 209/42 (2006.01); C07D 209/04 (2006.01); C07D 413/10 (2006.01); C07D 419/12 (2006.01); A61K 31/404 (2006.01);
U.S. Cl.
CPC ...
C07D 209/42 (2013.01); C07D 209/04 (2013.01); C07D 413/10 (2013.01); C07D 419/12 (2013.01); A61K 31/404 (2013.01); C07D 401/06 (2013.01); C07D 403/12 (2013.01); C07D 405/12 (2013.01); C07D 409/12 (2013.01);
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.

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