Description:

NEGATIVE ALLOSTERIC MODULATORS OF CB1 CANNABINOID RECEPTOR

INV-14021

INVENTORS:  Ganeshsingh Arjunsingh Thakur, Ritesh B Tichkule, Pushkar Mukund Kulkarni, Abhijit Raghunath Kulkarni

 

Description       

Among cannabinoid receptors, CB1 is the most abundant G-protein coupled receptor present in the brain, and it plays an important role in rewards, learning, memory, motor control and addiction.  Alcohol addiction has been observed to be linked with up/down regulation of CB1 receptor.  Currently available CB1 antagonists, though useful in alcohol addiction treatment, are associated with adverse psychiatric effects.  This invention discloses the development and use of novel class of allosteric compounds that negatively module the response of such endogenous cannabinoids without associated limitations as observed with prior art modulators.

Value Proposition

The allosteric compounds:

•Are synthetic derivatives

•Effectively allow for an affinity modulation, altering association or dissociation rates

•Are associated with a higher subtype selectivity as compared to their orthosteric counterparts

•Are capable of fine tuning the downstream signaling, leading to a functional selectivity

•Provide effective therapeutic benefits with minimal or no side effects

•Are associated with a prolonged duration of action

•Would be commercially useful for the following applications:

oTreatment of metabolic disorders

oTreatment of cardiovascular diseases

oTreatment of substance abuse disorders

oTreatment of neurodegenerative disorders

 

 

Intellectual Property status

Provisional Application 61/868,807

 

License status

Available for license

 

Patent Information:
For Information, Contact:
Mark Saulich
Associate Director of Commercialization
Northeastern University
m.saulich@northeastern.edu
Inventors:
Ganeshsingh Thakur
Ritesh Tichkule
Pushkar Kulkarni
Abhijit Kulkarni
Keywords:
Chemistry
Drug Discovery & Development
Health
Pharmaceutical Composition