Description:

Background
A novel class of compounds containing indole functionality has been found to have robust positive allosteric modulator (PAM) activity at the CB1 cannabinoid receptor. GAT1102 is a representative compound from this class shown to be effective in lowering intraocular pressure in the animal model with potential utility in treating glaucoma.

 

Technology Overview
A structurally novel class of compounds containing N-aryl indole moiety and an additional carboxylate functionality has been found to act as a CB1 PAM.

This class of compounds are structurally novel from the previously disclosed 2-phenylindole class of CB1 PAMs and are more druggable. A representative compound from this scaffold, GAT1102, was shown to be effective in reducing intraocular pressure in the animal models with potential utility in treating glaucoma.

 

Benefits

  • The modifications from the original 2‑phenylindole class of PAMs makes this template more druggable and provides opportunities to be administered as a prodrug.
  • The animal data make a compelling case for the utility of GAT1102 for reduced increased intraocular pressure associated with glaucoma. Based on previous findings with GAT211, a CB1 PAM, the researchers strongly believe that the class of compounds disclosed in this patent application will be useful for treating several other disorders mediated through CB1 receptor.

 

Applications

  • Neuropathic pain treatment
  • Treatment of Post-traumatic stress disorder (PTSD)
  • Treatment of glaucoma, epilepsy and neurodegenerative disorders such as Alzheimer’s (AD), Parkinson’s (PD), Huntington’s diseases (HD)

 

Opportunity

  • License
  • Partnering
  • Research Collaboration
Patent Information:
For Information, Contact:
Mark Saulich
Associate Director of Commercialization
Northeastern University
m.saulich@northeastern.edu
Inventors:
Ganeshsingh Thakur
Pushkar Kulkarni
Keywords:
Cancer
Chemistry
Drug Discovery & Development
Drugs
Therapeutic