US Patent 7560570 Inhibitors of fatty acid amide hydrolase
Patent 7560570 was granted and assigned to the scripps research institute on July, 2009 by the United States Patent and Trademark Office.
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Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having Ki's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an α-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other π-unsaturation corresponding to the arachidonyl Δ8,9/Δ11,12 and/or oleyl Δ9,10 positions. A preferred α-keto heterocylic head group is α-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).
US Patent 07560570 Inhibitors of fatty acid amide hydrolase US Patent 7560570 Inhibitors of fatty acid amide hydrolase
US Patent 07560570 Inhibitors of fatty acid amide hydrolase
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