Description:
 
Background
The present application relates to the synthetic derivatives which are negative allosteric modulators of the cannabinoid 1 (CB1) receptor and are useful in the treatment of several diseases including neuropathic pain, cancer, obesity as well as neuropathic pain and inflammation. This application is also directed towards the synthesis of the covalent probes for the allosteric site of the CB1 receptors which will help map the binding site through LAPS (Ligand Assisted Protein Structure) approach followed by Mass Spectrometry studies. 
 
Technology Overview
The covalent probes proposed can be useful for mapping CB1 allosteric sites as well as used for treatment of CB1 mediated disorders. 
Useful information like understanding important amino acid residue/s which are responsible for binding as well as altering functional response of both allosteric modulator as well as orthosteric ligand. Information like binding mode, kinetics of binding and dissociation, mechanism of action can be obtained using these modulators. 
One of our compounds has shown more than 250% binding at allosteric site than its normal counterpart. 
These compounds may also be useful as covalent drugs for treatment of CB1 mediated diseases. 
 
Benefits
- Molecules can be used as diagnostic tools and also for analytical purposes in CB1 allosterism 
- Helps in treatment of neuropathic pain and inflammation
- Targets allosteric sites
- Has high specificity for allosteric sites
 
Applications
- Neuopathic diseases
- Pharmaceuticals
- Allosteric Therapeutics
- Mapping Allosteric sites
- Treatment of CB! mediated disorders
 
Opportunity
- Research Collaboration
- partnering
- License
 
Patent Information:
For Information, Contact:
Mark Saulich
Associate Director of Commercialization
Northeastern University
m.saulich@northeastern.edu
Inventors:
Ganeshsingh Thakur
Pushkar Kulkarni
Abhijit Kulkarni
Ritesh Tichkule
Keywords:
Chemistry
Drug Discovery & Development
Health
Pharmaceutical Composition