Alpha-ketoheterocycles and methods of making and using

Patent metadata

Field	Value
Publication number	US-9504675-B2
Application number	US-201213983369-A
Country	US
Kind code	B2
Filing date	Feb 3, 2012
Priority date	Feb 4, 2011
Publication date	Nov 29, 2016
Grant date	Nov 29, 2016

Abstract

Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones.

First claim

What is claimed is:

1. A compound of formula (I)

wherein:
R 2 is hydrogen, halo, haloalkyl, nitrile, C(O)OR′, C(O)N(R′) 2 , aryl, or heteroaryl, wherein the aryl or heteroaryl is optionally mono- or independently multisubstituted with J;
X is CH 2 or CH 2 Ch 2;
Y is CH or N;
R 1 is selected from the group consisting of H, aryl, —Z-aryl, heteroaryl, and —Z-het…

Assignees

• Boger Dale L
• Scripps Research Inst

Inventors

• Boger Dale L

Classifications

• A61P43/00

  Human Necessities · mapped topic

• A61K31/421 Primary

  Human Necessities · mapped topic

• A61P29/00

  Human Necessities · mapped topic

• C07D263/34

  Chemistry & Metallurgy · mapped topic

• C07D271/10

  Chemistry & Metallurgy · mapped topic