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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 9586928 B1

PDFFull Text
Date of Patent:
Mar. 07, 2017

Filed:

May. 16, 2012

Modulators of the nuclear hormone receptor ror

Applicants:

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

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

Youseung Shin, Dublin, OH (US);

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

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

Brent R. Lyda, Jupiter, FL (US);

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

Naresh Kumar, Indianapolis, IN (US);

Thomas Burris, Palm Beach Gardens, FL (US);

Inventors:

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

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

Youseung Shin, Dublin, OH (US);

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

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

Brent R. Lyda, Jupiter, FL (US);

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

Naresh Kumar, Indianapolis, IN (US);

Thomas Burris, Palm Beach Gardens, FL (US);

Assignee:

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

Attorneys:

Geoffrey K. Cooper

Thomas Fitting

Primary Examiner:

Emily Bernhardt

Int. Cl.
CPC ...
C07D 213/74 (2006.01); C07D 213/36 (2006.01); C07D 295/096 (2006.01); C07D 295/185 (2006.01); C07D 295/195 (2006.01); C07D 295/26 (2006.01); C07D 277/64 (2006.01); C07D 207/09 (2006.01); C07D 211/22 (2006.01); C07D 233/61 (2006.01); C07D 317/50 (2006.01); C07D 213/82 (2006.01); C07D 215/12 (2006.01); C07D 317/58 (2006.01); C07D 319/20 (2006.01); C07D 333/20 (2006.01); C07D 333/34 (2006.01); C07D 401/12 (2006.01); C07D 277/28 (2006.01); C07D 209/14 (2006.01); C07D 295/205 (2006.01); C07D 295/215 (2006.01); C07D 213/61 (2006.01); C07D 213/64 (2006.01); C07D 307/24 (2006.01); A61K 31/495 (2006.01); A61K 31/496 (2006.01); A61K 31/5375 (2006.01); A61K 31/5377 (2006.01); A61K 45/06 (2006.01);
U.S. Cl.
CPC ...
C07D 317/50 (2013.01); A61K 31/495 (2013.01); A61K 31/496 (2013.01); A61K 31/5375 (2013.01); A61K 31/5377 (2013.01); A61K 45/06 (2013.01); C07D 207/09 (2013.01); C07D 209/14 (2013.01); C07D 211/22 (2013.01); C07D 213/36 (2013.01); C07D 213/61 (2013.01); C07D 213/64 (2013.01); C07D 213/74 (2013.01); C07D 213/82 (2013.01); C07D 215/12 (2013.01); C07D 233/61 (2013.01); C07D 277/28 (2013.01); C07D 277/64 (2013.01); C07D 295/096 (2013.01); C07D 295/185 (2013.01); C07D 295/205 (2013.01); C07D 295/215 (2013.01); C07D 295/26 (2013.01); C07D 307/24 (2013.01); C07D 317/58 (2013.01); C07D 319/20 (2013.01); C07D 333/20 (2013.01); C07D 333/34 (2013.01); C07D 401/12 (2013.01);
Abstract

The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα, RORβ, or RORγ, of formula with the variable atoms as defined herein and Rcomprising a hydroxyl- or alkoxyl-substituted fluoroalkyl group. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.

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