Neurodegenerative disorders (ND) accounts the vast majority of age related dementias characterized by progressive cognitive decline of higher mental functions. The research devoted to this field uncovered a pathomechanism of complex multietiology which cannot be addressed by hitting one target.
Motivated by currently available treatment against ND involving the inhibitors of acetylcholinesterase (AChE) and N-methyl-D-aspartate receptor (NMDAR), administered also in combination, we developed dually-acting compounds based on 1,2,3,4-tetrahydro-9-aminoacridine (tacrine) structure and confirmed their neuropsychopharmacological and drug-like properties for potential therapeutic use.
Only a few compounds have been established for the treatment of Alzheimer’s disease. For instance, FDA and EMEA have approved three cholinesterase inhibitors, one NMDA-receptor antagonist – memantine and one disease-modifying immunotherapy – aducanumab, for Alzheimer’s disease (AD). Here we offer a combination of both effect in a single molecule. To date there are many other drugs undergoing clinical trials in AD, having various mechanism of action (vaccines against amyloid beta, against Tau protein, antiinflammation drugs) but none of them seems to reach the registration in a short term.
Novel molecules represent a new way how to cope with the multiple pathogenic factors of ND. Based on our observations, we suppose that these compounds are able to hit additional targets relevant to ND and thus succeed in overcoming the multifactorial pathogenesis. While tacrine (approved for AD treatment in 1993) was withdrawn from the market due to its hepatotoxicity and other side effects in 2013, our compounds were prepared to avoid this hepatotoxic effect as we demonstrated in in vitro studies. Since these compounds have also been found acting as GluN2B selective NMDAR antagonists, they are therefore believed to hold strong therapeutic potential in the treatment of other disorders – e.g. ischemic damage, chronic pain and depression.
Authors would like to thank the grant of Ministry of Education, Youth and Sports of the Czech Republic (project ERDF no. CZ.02.1.01/0.0/0.0/18_069/0010054).
1. https://pubmed.ncbi.nlm.nih.gov/33892271/
2. https://www.sciencedirect.com/science/article/abs/pii/S0006295221000563?dgcid=rss_sd_all
3. https://www.tandfonline.com/doi/abs/10.1080/01480545.2019.1566350?journalCode=idct20&
Technology is owned by University Hospital Hradec Králové together with Institute of Physiology CAS, National Institute of Mental Health and Institute of Experimental Medicine CAS. We are currently seeking for development or commercial partner or licensing. Two Czech patents309 225 and 309 262 were granted. PCT application CZ/2022/050004was submitted. Technology is going through in vitro validation.
Intellectual property status
Granted Patent
Patent number : 309 225 & 309 262
Patent already applied for
Patent application number : CZ/2022/050004
Where : PCT
Current development status
Others
In vitro validation
Desired business relationship
Patent licensing
Technology development
University Hospital Hradec Králové is now one of the largest medical facilities not only in Eastern Bohemia but also throughout the Czech Republic. It is a state-of-the-art facility spanning a wide range of medical fields and serves as a catchment center for approximately 1,000,000 inhabitants from all over the Czech Republic.
More than 41,000 patients are hospitalized every year at the hospital’s 39 workplaces, which include 24 departments and over 1370 beds, with approximately 715,000 outpatients treated annually. The most complex surgical procedures are performed and modern diagnostic and treatment technologies are used. This makes University Hospital Hradec Králové comparable with similar hospitals in Europe.
University Hospital is an important research and educational institution closely connected with the Faculty of Medicine in Hradec Králové.
Create your free account to connect with University Hospital Hradec Králové and thousands of other innovative organizations and professionals worldwide
Send a request for information
to University Hospital Hradec Králové
Technology Offers on Innoget are directly posted
and managed by its members as well as evaluation of requests for information. Innoget is the trusted open innovation and science network aimed at directly connect industry needs with professionals online.
Need help requesting additional information or have questions regarding this Technology Offer?
Contact Innoget support
