New Compounds for the Treatment of Acute Pain

Technology Overview

The invention consists of a series of novel compounds for the treatment of acute pain. Current therapeutic approaches for pain management include the use of opioids with which many side effects are known to be associated including tolerance and potential dependence. The present invention serves the development of new therapeutic strategies and new non-opioid drugs for the treatment of pain. The invention describes the development of new compounds with a thiazolo[5,4-d]pyrimidine structure that are found to be A2A adenosine receptor blockers and more potent than those already on the market. Affinity and potency of the compounds were evaluated by receptor binding experiments and cyclic AMP assays. It is evident from these assays that the new compounds have a high affinity (femtomolar order) for the A2A receptor, associated with high potency (picomolar order). In addition, the new derivatives have been tested in widely used and validated animal models of acute pain, such as the writhing and tail immersion tests, and have been found to be similarly or more effective than morphine.

Stage of Development

The Technology Readiness Level (TRL) of the invention is 3.

Benefits

Among the advantages of the technology, it is possible to highlight that two compounds among those patented showed picomolar-order potency in functional tests of cyclic AMP, superior to that of already commercially available A2A receptor blockers, with antinociceptive action equal to or greater than morphine and the reference compound in writhing and tail immersion tests.

Applications

The patented technology is designed for the following fields of application:

1. Treatment of acute pain
2. Treatment of inflammatory processes
3. Treatment of fibrosis
4. Oncological treatments
5. Treatments of neurodegenerative diseases

Opportunity

The patent is available for outright assignment, as well as for exclusive and non-exclusive licensing. Licenses are available for the remaining term of the patent titles.

The Research Group is available for new collaborative and third-party research activities, in-depth technical investigations, scientific advice, also aimed at raising the TRL of the technology.