Novel anandamide amidase inhibitors as analgesic agents

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 207/46 (2006.01) A61K 31/185 (2006.01) A61K 31/22 (2006.01) A61K 31/255 (2006.01) A61K 31/33 (2006.01) A61K 31/40 (2006.01) A61K 31/4015 (2006.01) C07C 259/06 (2006.01) C07D 401/06 (2006.01) C07D 403/06 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2255620

Disclosed is a method of inhibiting anandamide amidase in an individual or animal and novel inhibitors of anandamide amidase. Compounds of the invention are represented by Structural Formula (I): R-X-Y (I) wherein R is selected from the group consisting of a methyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, and an optionally substituted heterocyclic group; X is an optionally substituted straight chain hydrocarbyl group containing from 10-24 carbon atoms if R is a methyl group, and from 4-18 carbon atoms if R is an optionally substituted aryl group, an optionally substituted heteroaryl group, or an optionally substituted heterocyclic group; and Y is a moiety capable of irreversibly binding to a nucleophilic group at the active site of an amidase enzyme.

L'invention décrit un procédé d'inhibition d'anandamide amidase chez un individu ou un animal, ainsi que de nouveaux inhibiteurs d'anandamide amidase. Le procédé décrit et les nouveaux composés peuvent être utilisés afin d'atténuer la douleur chez un individu ou un animal souffrant, réduire les nausées chez un individu traité par chimiothérapie, par exemple une chimiothérapie contre le cancer, supprimer l'appétit chez un individu, réduire la pression intraoculaire d'un individu ou d'un animal souffrant d'un glaucome, et supprimer le système immunitaire chez un individu à qui on a transplanté un organe.

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