Inhibitors of neurotrypsin and determination thereof

Details Inhibitors of neurotrypsin and determination thereof Inhibitors of neurotrypsin and determination thereof

C - Chemistry, Metallurgy

07

C

C07C 311/47 (2006.01) A61K 31/63 (2006.01) A61P 25/18 (2006.01)

Patent

CA 2600791

The invention relates to a method for determining whether a compound is a neurotrypsin inhibitor, characterized in that the compound is incubated together with neurotrypsin, a variant thereof or a fragment comprising the protease domain and with a protein or peptide comprising agrin, a variant thereof or a fragment comprising the - or the - cleavage site of agrin, in an aqueous buffer solution, and the amount of cleavage of agrin is measured. Additionally, the invention relates to inhibitors of neurotrypsin found by this method, in particular to compounds of formula (1) wherein Hal1 and Hal2 are fluorine, chlorine or bromine, and the use of such inhibitors for the treatment and/or prophylaxis of diseases caused by deficiency of synapses, for example skeletal muscle atrophy, schizophrenia, and cognitive disturbance.

L'invention concerne un procédé qui permet de déterminer si un composé est un inhibiteur de la neurotrypsine, caractérisé en ce que ce composé est incubé avec la neurotrypsine, un variant ou un fragment de celle-ci comprenant le domaine protéasique, ainsi qu'avec une protéine ou un peptide qui comprend de l'agrine, un variant ou un fragment comprenant l'agrine ou le site de clivage de l'agrine, dans une solution tampon, le degré de clivage de l'agrine étant alors mesuré. Par ailleurs, l'invention concerne des inhibiteurs de la neurotrypsine, en particulier des composés représentés par la formule (1) dans laquelle Hal1 et Hal2 représentent fluor, chlore ou brome, ainsi que l'utilisation de ces inhibiteurs dans le traitement et/ou la prophylaxie de maladies déclenchées par le manque de synapses, telles que l'atrophie du muscle squelettique, la schizophrénie et la distorsion cognitive.

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