Tag: phosphodiesterase

Company News: biocrea and Boehringer Ingelheim Conclude Asset Purchase Agreement

biocrea today announced the completion of an asset purchase and licensing deal with Boehringer Ingelheim. Under the terms of the agreement, biocrea will receive an undisclosed payment and will transfer the exclusive global rights for certain research programs originating from its phosphodiesterase (PDE) platform to Boehringer Ingelheim. This includes biocrea´s PDE2 inhibitors and its most advanced compound BCA909.
“This transaction marks a key milestone in the evolution of biocrea, which was created only about a year ago,” said Tom Kronbach, CEO of biocrea. ”Importantly, this deal demonstrates our ability to identify and validate disease-relevant novel mechanisms of action for which we create high-quality drug candidates. The proceeds from this agreement will allow us to implement our strategy to build a sustainable company over the next several years.”

Company News: biocrea and Pfizer Jointly Presented Details on Novel PDE10 Inhibitors at the 241st ACS National Meeting & Exposition

– Novel treatment opportunities for CNS diseases –

biocrea, a biopharmaceutical company focusing on novel treatments for disorders of the central nervous system (CNS), today reported details on the design and synthesis of novel, brain-penetrating phosphodiesterase-10 (PDE10) inhibitors developed in collaboration with Pfizer Inc. (NYSE: PFE). The data were featured in joint presentations[1] with Pfizer at the recent 241st ACS National Meeting & Exposition, an event organized by the American Chemical Society (ACS).

The data demonstrated that the scientists at Pfizer and biocrea were able to eliminate undesired activity on adenosine receptors and to considerably improve the compounds´ physicochemical properties and potency. The team had started with initial high-throughput hits characterized by low potency and selectivity. Further lead optimization led to a number of compounds with very robust activity in a range of preclinical models of anti-psychotic efficacy. Moreover, these PDE10 inhibitors produced low levels of catalepsy, suggesting a minimal risk for the induction of side-effects involving the extrapyramidal system (EPS), the most common adverse reaction observed with anti-psychotic drugs.

Phosphodiesterases (PDEs) have been identified as key regulators of intracellular cyclic nucleotide levels in the brain. Mechanistically, PDE10 inhibition has two major benefits, mimicking, (1) the effects of antagonists of the dopamine-2 receptor, the current standard treatment for psychosis, and (2) the effects of agonists of dopamine-1 receptors, which may decrease the side-effect liabilities while contributing to a pro-cognitive profile.

 


[1] Malamas M et al., 241st ACS National Meeting & Exposition Abstract 65 – Imidazo[1,5-a]quinoxalines as selective PDE10A inhibitors for the treatment of schizophrenia, http://redir.ec/Qr3C; Malamas, M. et al., 241st ACS National Meeting & Exposition Abstract 66 – Benzo[e]imidazo[5,1-c][1,2,4]triazines as selective PDE10A inhibitors for the treatment of schizophrenia, http://redir.ec/pl1Q


Company News: biocrea acquires CNS pipeline and PDE inhibitor platform from Biotie

In a management-buyout, biocrea GmbH is taking over  the CNS pipeline and phosphodiesterase enzyme (PDE) inhibitor platform from Finnish Biotie Therapies Corp.

The company currently has a pipeline of three PDE inhibitors at research and preclinical stages, which will be advanced into clinical development by 2012. The compounds have already demonstrated efficacy in preclinical animal models for schizophrenia, memory impairment, depression and anxiety.

biocrea is based in Radebeul near Dresden, Germany, and will be led by Dr. Tom Kronbach, former CSO of Biotie.

More details can be found soon at biocrea’s website.