IP Library Granted Patent US 9,586,928
Granted Patent B2
US 9,586,928 · App. 14/118,116 · Granted Mar 7, 2017

Modulators of the nuclear hormone receptor ROR

Inventors: Theodore Mark Kamenecka (Palm Beach Gardens, FL); Patrick R. Griffin (Jupiter, FL); Youseung Shin (Dublin, OH); Yuanjun He (Palm Beach Gardens, FL); Anne-Laure Blayo (Jupiter, FL); Brent R. Lyda (Jupiter, FL); Marcel Koenig (Palm Beach Gardens, FL); Naresh Kumar (Indianapolis, IN); Thomas Burris (Palm Beach Gardens, FL)
Assignee: The Scripps Research Institute
C07D317/50A61K31/495A61K31/496A61K31/5375A61K31/5377A61K45/06C07D207/09C07D209/14C07D211/22C07D213/36C07D213/61C07D213/64C07D213/74C07D213/82C07D215/12C07D233/61C07D277/28C07D277/64C07D295/096C07D295/185C07D295/205C07D295/215C07D295/26C07D307/24C07D317/58C07D319/20C07D333/20C07D333/34C07D401/12
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Quick Facts
Patent No.
US 9,586,928
App. No.
14/118,116
Granted
Mar 7, 2017
Kind
B2
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 R 1 comprising 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.

Claims (1)

1. A compound wherein the compound is any of the following, or a pharmaceutically acceptable salt thereof:

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 16, 2022
From: THE SCRIPPS RESEARCH INSTITUTE
To: UNIVERSITY OF FLORIDA BOARD OF TRUSTEES
Reel/Frame 061201/0563 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 16, 2022
From: UNIVERSITY OF FLORIDA BOARD OF TRUSTEES
To: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INCORPORATED
Reel/Frame 061201/0624 →
CONFIRMATORY LICENSE Recorded Oct 7, 2015
From: SCRIPPS RESEARCH INSTITUTE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 036816/0995 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 4, 2014
From: KAMENECKA, THEODORE MARK; GRIFFIN, PATRICK R.; SHIN, YOUSEUNG; HE, YUANJUN; BLAYO, ANNE-LAURE; LYDA, BRENT R.; KOENIG, MARCEL; KUMAR, NARESH; BURRIS, THOMAS
To: THE SCRIPPS RESEARCH INSTITUTE
Reel/Frame 032347/0587 →
Continuity (2)
Provisional Application 61486459 · May 16, 2011
Related Publication 20140187554A1 · Jul 3, 2014