Loading patent…
OwnerManfred Brockhaus, Heinz Doebeli +4inventors
InventorsManfred Brockhaus, Heinz Doebeli, Fiona Grueninger, Philipp Huguenin, Eric Argirios Kitas, Peter Nelboeck-Hochstetter
Estimating the term…
The present invention relates to an assay for identifying inhibitors of beta-secretases comprising the steps of immobilizing a beta-secretase protein on a solid support, contacting it with a test compound in the presence of a tagged beta-secretase inhibitor, and comparing the extent of binding of the tagged beta-secretase inhibitor in the presence and in the absence of the test compound in order to evaluate if the test compound is an inhibitor of beta-secretases. The present invention also relates to a method of screening for inhibitors of beta-secretases, to novel beta-secretase inhibitors and their use as tagged beta-secretase inhibitors for identification of inhibitors of beta-secetase, to a kit for identifying beta-secretase inhibiotrs as well as to novel beta-secretase inhibitors for use in the treatment of Alzheimer's disease and other cerebrovascular amyloidosis.
A beta-secretase inhibitor of Formula I:Y-P4-P3-P2-P1-P1′-P2′-P3′-P4′-W,
An assay for identifying beta-secretase inhibitors comprising the steps of
A method of screening for compounds capable of inhibiting a beta-secretase activity comprising measuring the binding activities of a tagged beta-secretase inhibitor to a beta-secretase in the presence of a test compound and determining the level of test compound competing with the tagged beta-secretase inhibitor for active-site binding based on the binding activities.
A kit for identifying a beta-secretase inhibitor comprising natural or recombinantly produced beta-secretase polypeptide and a tagged beta-secretase inhibitor.
A kit for use in an assay to identify beta-secretase activity, wherein the assay comprises the steps of
A kit for screening compounds in accordance to a method capable of inhibiting a beta-secretase activity, the method comprises measuring the binding activities of a tagged beta-secretase inhibitor to a beta-secretase in the presence of a test compound and determining the level of test compound competing with the tagged beta-secretase inhibitor for active-site binding based on the binding activities.
An inhibitor of beta-secretase identified by an assay wherein the assay comprises the steps of
An inhibitor of beta-secretase identified by a method of screening compounds capable of inhibiting a beta-secretase activity, the method comprises measuring the binding activities of a tagged beta-secretase inhibitor to a beta-secretase in the presence of a test compound and determining the level of test compound competing with the tagged beta-secretase inhibitor for active-site binding based on the binding activities.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a beta-secretase inhibitor identified by an assay wherein the assay comprises the steps of
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a beta-secretase inhibitor which is identified by a method of screening compounds capable of inhibiting a beta-secretase activity comprising measuring the binding activities of a tagged beta-secretase inhibitor to a beta-secretase in the presence of a test compound and determining the level of test compound competing with the tagged beta-secretase inhibitor for active-site binding based on the binding activities.
A method of treating a patient afflicted or having a predisposition for cerebrovascular amyloidosis comprising administering to the patient a pharmaceutically effective amount of a compound comprising a beta-secretase inhibitor identified by an assay for identifying beta-secretase inhibitors, the assay comprising the steps of
A method of treating a patient afflicted or having a predisposition for cerebrovascular amyloidosis comprising administering to the patient a pharmaceutically effective amount of a compound comprising a beta-secretase inhibitor identified by a method for screening compounds capable of inhibiting a beta-secretase activity, the method comprises measuring the binding activities of a tagged beta-secretase inhibitor to a beta-secretase in the presence of a test compound and determining the level of test compound competing with the tagged beta-secretase inhibitor for active-site binding based on the binding activities.
Dependencies are inferred from the claim text.