Invention Grant
- Patent Title: Modulators of the nuclear hormone receptor ROR
- Patent Title (中): 核激素受体ROR的调节剂
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Application No.: US14118116Application Date: 2012-05-16
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Publication No.: US09586928B2Publication Date: 2017-03-07
- Inventor: Theodore Mark Kamenecka , Patrick R. Griffin , Youseung Shin , Yuanjun He , Anne-Laure Blayo , Brent R. Lyda , Marcel Koenig , Naresh Kumar , Thomas Burris
- Applicant: Theodore Mark Kamenecka , Patrick R. Griffin , Youseung Shin , Yuanjun He , Anne-Laure Blayo , Brent R. Lyda , Marcel Koenig , Naresh Kumar , Thomas Burris
- Applicant Address: US CA La Jolla
- Assignee: The Scripps Research Institute
- Current Assignee: The Scripps Research Institute
- Current Assignee Address: US CA La Jolla
- Agent Geoffrey K. Cooper; Thomas Fitting
- International Application: PCT/US2012/038119 WO 20120516
- International Announcement: WO2012/158784 WO 20121122
- Main IPC: C07D213/74
- IPC: C07D213/74 ; C07D213/36 ; C07D295/096 ; C07D295/185 ; C07D295/195 ; C07D295/26 ; C07D277/64 ; C07D207/09 ; C07D211/22 ; C07D233/61 ; C07D317/50 ; C07D213/82 ; C07D215/12 ; C07D317/58 ; C07D319/20 ; C07D333/20 ; C07D333/34 ; C07D401/12 ; C07D277/28 ; C07D209/14 ; C07D295/205 ; C07D295/215 ; C07D213/61 ; C07D213/64 ; C07D307/24 ; A61K31/495 ; A61K31/496 ; A61K31/5375 ; A61K31/5377 ; A61K45/06

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 R1 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.
Public/Granted literature
- US20140187554A1 MODULATORS OF THE NUCLEAR HORMONE RECEPTOR ROR Public/Granted day:2014-07-03
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