Novel TRPV-1 derivates for treament of chronic pain

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Chronic neuropathic pain is complex, not well understood, and is usually accompanied by tissue injury. Nerve fibers may be injured, damaged, or dysfunctional. This pain has a detrimental effect on the quality of life of individuals afflicted with neuropathy. Sometimes they are unable to work or even perform simple daily tasks.

The costs associated with neuropathic pain around the world totaled ~$1.8 Billion in 2010 and is projected to grow at a 10% CAGR. There are several vanilloid receptors, both agonists and antagonists, in various phases of clinical trials. Today, there are at least seven drugs in clinical trials now and more drugs in a pre-clinical state from various manufacturers.

This invention details preparation, identification, and in vitro studies of novel thiadiazol and chalcone derivative antagonists for treatment of chronic pain in diseases in which the TRPV-1 receptor is overactivated. These new derivatives are potent, have a distinct binding site, and have an IC50 in the nanomolar range that exceeds or is comparable to other potent antagonists and vanilloid derivatives currently undergoing testing. UdeC is seeking a commercial partner for further testing and enhancing the potential value of these compounds.

Areas of application:
– Neuropathic Pain.
– Novel drug molecules.

Miguel Zárraga Olavarría
Department of Chemistry
Faculty of Chemistry

Intellectual Property:

Patent pending CL201202133


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