biocrea announces novel treatment opportunities for CNS diseases

Company has filed US patent on novel, brain-penetrating PDE2 and PDE10 inhibitors

16-Feb-2011 - Germany

biocrea announced it has filed a patent application covering its brain-penetrating inhibitors of phosphodiesterases. These compounds constitute a new generation of promising drug candidates to address several CNS disorders that are currently lacking effective treatment options.

“Phosphodiesterases, or PDEs, are key regulators of brain signaling. Recently, PDEs have also been associated with a number of CNS diseases, and inhibiting certain PDEs in the brain bears great therapeutic potential for indications such as schizophrenia, depression, anxiety or movement disorders,” said Dr. Martin Gunthorpe, CSO of biocrea. “However, a lot of opportunities are still unexplored so far. Most attempts have failed to develop small molecule PDE inhibitors that easily penetrate the brain and act with sufficient specificity and efficacy. biocrea has pioneered the development of PDE2 and PDE10 inhibitors that overcome these limitations. Therefore, our compounds open an exciting avenue for novel treatment options for severe diseases of the central nervous system.”

biocrea has submitted a patent application to the U.S. Patent Office (USPTO) covering compounds and uses of its proprietary PDE2 and PDE10 inhibitors.

While the inhibitors of PDE10 show excellent potential for the treatment of schizophrenia, Huntington’s disease and Tourette’s syndrome, the PDE2 inhibitors cover a whole spectrum of new biological activities and treatment opportunities. “As an example,” Gunthorpe said, “we have demonstrated in animal models that these compounds are able to significantly improve cognitive deficits and have therapeutic potential to treat depression and anxiety.”

Moreover, biocrea’s brain-penetrating PDE2 inhibitors show promise for the treatment of drug-induced movement disorders. “This constitutes a completely novel therapeutic approach for this indication, a common side effect of anti-psychotic medications,” Gunthorpe added.

biocrea’s patent application also comprises dual inhibitors of PDE2 and PDE10 as the combination of both modes of action in one molecule results in synergistic biological effects.

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