Inhibitors of fatty acid amide hydrolase

Details Inhibitors of fatty acid amide hydrolase Inhibitors of fatty acid amide hydrolase

C - Chemistry, Metallurgy

07

D

C07D 417/04 (2006.01) A61K 31/421 (2006.01) A61K 31/422 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61P 25/00 (2006.01) C07D 263/30 (2006.01) C07D 263/32 (2006.01) C07D 263/34 (2006.01) C07D 263/56 (2006.01) C07D 271/10 (2006.01) C07D 277/20 (2006.01) C07D 277/24 (2006.01) C07D 277/64 (2006.01) C07D 285/12 (2006.01) C07D 413/04 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2501575

Improved competitive inhibitors of FAAH employ an .alpha.-keto heterocyclic pharmacophore and a binding subunit having a -unsaturation. The .alpha.-keto heterocyclic pharmacophore and a binding subunit are attached to one another, preferably by a hydrocarbon chain. The improvement lies in the use of a heterocyclic pharmacophore selected from oxazoles, oxadiazoles, thiazoles, and thiadiazoles that have alkyl or aryl substituents at their 4 and/or 5 positions. The improved competitive inhibitors of FAAH display enhanced activity over conventional competitive inhibitors of FAAH.

L'invention concerne des inhibiteurs améliorés de FAAH utilisant un pharmacophore hétérocyclique .alpha.-keto et une sous-unité de liaison présentant une insaturation -. Le pharmacophore hétérocyclique .alpha.-keto et la sous-unité de liaison? ¿sont reliés, de préférence par une chaîne d'hydrocarbone. L'invention est caractérisée en ce que le pharmacophore hétérocyclique est sélectionné dans le groupe comprenant des oxazoles, oxadiazoles, thiazoles et thiadiazoles, lesquels ont des substituants alkyle ou aryle en position 4 et/ou 5. Les inhibiteurs améliorés de FAAH selon l'invention développent une plus grande activité que les inhibiteurs de FAAH classiques.

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