Allosteric Modulators of CB1 Cannabinoid Receptors

INV-1242

Background

Anorexia nervosa (AN) is a major psychiatric eating disorder associated with substantial morbidity and mortality. Its characteristic symptoms include the refusal to maintain minimally normal body weight, an intense fear of becoming fat, and a disturbed perception of body shape and size. It is also characterized by anhedonia whereby patients experience little pleasure or reward in many aspects of their lives. Pharmacotherapeutic interventions for the treatment of AN are extremely limited, as there is still a lack of understanding of their pathogenesis. The endocannabinoid system has been recently recognized as an important target in both reward processing and feeding behavior.

Technology Overview

This invention is directed to compositions and methods that can be used for the treatment of these disorders while minimizing or eliminating abuse potential and providing higher specificity with reduced side effects. The invention relates to heterocyclic derivatives which are allosteric modulators of cannabinoid receptor 1 (CB1) and are useful for the treatment or prevention of neurological and psychiatric disorders associated with endocannabinoid dysfunction and diseases in which the CB1 subtype of cannabinoid receptor is involved. This is used as a prevention or treatment of such diseases in which cannabinoid receptors are involved such as pain, neuropathic pain, glaucoma, drug addiction, eating disorders (anorexia nervosa; bulimia nervosa; binge-eating disorders) and post-traumatic stress disorders.

Benefits

- Is more site-specific than conventional therapeutic agents
- Works by acting at a site topographically distinct from an orthosteric site
- Has minimal or no abuse potential as compared to conventional agents
- Direct-acting CB1 agonists have been used
- No or minimal abuse potential and higher specificity with reduced side effects

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