Technology Listings


7,8-Dihydroxyflavone Derivatives for Treating Neurological and Neurodegenerative Diseases

Application

Family of small molecule 7,8-dihydroxyflavones that act as TrkB agonists, including a prodrug, for treating a number of neurological conditions and diseases.

Key Benefits
  • Has antidepressant-like properties, improves cognitive function, and promotes neuronal survival in animal models of neurological diseases.
  • Whereas current anti-depressant and anti-anxiety medications take 1-2 months to take effect, and frequently produce very harsh side effects, 7,8-dihydroxyflavone is a potent anti-depressant that demonstrates therapeutic efficacy within a few days.
  • Substantial patent portfolio with large number of protected derivatives.
  • May be effective against several neurological disease indications.
Market Summary

Brain-derived neurotrophic factor (BDNF), a ligand that activates the TrkB receptor, is of interest as a therapeutic target due to its neuroprotective properties. Treatment with BDNF, however, is not an option due to poor efficiency, bioavailability, adverse side effects, and inability to cross the blood brain barrier. Because dysregulation of BDNF and TrkB receptor activation is implicated in a variety of neurological diseases, the impact of a TrkB agonist could prove to be quite profound. Some disorders that may benefit from this therapeutic include Parkinson’s disease, Alzheimer’s disease, stroke, Rett Syndrome, Huntington’s disease, Amyolateral Sclerosis, glaucoma, macular degeneration, anxiety, and depression.

Technical Summary

Researchers at Emory have identified a TrkB agonist, 7,8-dihydroxyflavone (7,8-DHF), that has improved activity, bioavailability, and fewer deleterious side effects. Moreover, Dr. Ye and colleagues are doing further structure activity relationships assays to identify additional modifications that could further improve upon this small molecule therapeutic. Treatment with 7,8-DHF improves Parkinsonian symptoms in animal models, reduces anxiety, increases synaptic plasticity, and promotes neuronal survival. Through a structure-activity relationship study, a derivative of 7,8-DHF was found to have higher and more prolonged TrkB agonistic activity than 7,8-DHF in vitro. There is currently a lead compound which has anti-apoptotic activity.

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Developmental Stage

This small molecule program has a lead candidate and additional work is ongoing.

Patent Information
App Type Country Serial No. Patent No. File Date Issued Date Expire Date
Nationalized PCT - United States United States 13/055,861 7/23/2009    
Nationalized PCT - Foreign Canada 2,731,849   7/23/2009   7/23/2029
Nationalized PCT - Foreign EP 09801005.1   7/23/2009   7/23/2029
Nationalized PCT - Foreign China 200980134395.1   7/23/2009   7/23/2029
Nationalized PCT - Foreign India 1201/DELNP/2011   7/23/2009   2/18/2011
Nationalized PCT - Foreign Canada 2,801,415   6/8/2011    
Nationalized PCT - Foreign China 201180027364.3 ZL201180027364.3 6/8/2011 1/27/2016 6/7/2031
Nationalized PCT - Foreign EP 11793086.7   6/8/2011    
Nationalized PCT - United States United States 13/643,769 9,029,561 6/8/2011 5/12/2015 7/3/2031
Nationalized PCT - Foreign Australia 2011264917 2011264917 6/8/2011 11/19/2015  
Nationalized PCT - Foreign China 2013800385775   7/25/2013   7/25/2033
Nationalized PCT - Foreign EP 13822110.6   7/25/2013   7/25/2033
Nationalized PCT - United States United States 14/410,756 9,593,125 12/23/2014 3/14/2017  
Divisional United States 14/639,343 9,504,674 3/5/2015 11/29/2016 6/8/2031
Divisional China 201610018368.X   1/12/2016    
Divisional China 201610243176.9   4/18/2016    
Divisional United States 15/416,964 1/26/2017    
Tech ID: NCS.01
Published: 10/18/2016
Category
Therapeutics

Contact
Cliff Michaels
Assistant Director
Emory University
404-727-3890
ccmicha@emory.edu

Inventor(s)
Keqiang Ye

Keywords
Neuroscience/Pain
Small Molecule