Novel Allosteric Modulators of CB1 Cannabinoid Receptor

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.

 

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 our 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 animal model with potential utility in treating glaucoma.

 

- 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 our previous findings with GAT211, a CB1 PAM, we strongly believe that the class of compounds disclosed in this patent application will be useful for treating several other disorders mediated through CB1 receptor. 

 

- 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)

 

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