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Inhibitors of fatty acid amide hydrolase

A composition and compound technology, applied in the direction of anti-inflammatory agents, non-central analgesics, allergic diseases, etc., can solve the problem of unexplored therapeutic efficacy of FAAH inhibitors, lack of target selectivity, biological activity and/or bioavailability Degree and other issues

Inactive Publication Date: 2011-05-04
INFINITY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, current FAAH inhibitors lack the target selectivity, bioactivity, and / or bioavailability required for in vivo studies and therapeutic use
Thus, to date, the therapeutic efficacy of FAAH inhibitors has remained largely unexplored

Method used

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  • Inhibitors of fatty acid amide hydrolase
  • Inhibitors of fatty acid amide hydrolase
  • Inhibitors of fatty acid amide hydrolase

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0763] Provided formulations of the pharmaceutically acceptable compositions described herein can be prepared by any method known or hereafter developed in the art of pharmacology. In general, such methods of preparation comprise the steps of bringing into association the active ingredient with the carrier and / or one or more other auxiliary ingredients, and then, if necessary and / or desired, shaping and / or packaging the product in the desired unit. or in multiple dose units.

[0764] The pharmaceutically acceptable compositions of the invention may be prepared, packaged and / or sold in bulk, as a single unit dose and / or as a plurality of single unit doses. As used herein, a "unit dose" is a discrete quantity of a pharmaceutically acceptable composition containing a predetermined quantity of active ingredient. The amount of active ingredient is usually equal to the dose of active ingredient to be administered to the individual and / or a convenient fraction of such a dose (eg, on...

example 1

[0921]

[0922] 3-Fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid (470mg, 1.77mmol) and 2-amino Acetophenone hydrochloride (318 mg, 1.89 mmol) was dissolved in 10 mL of anhydrous dichloromethane. HOBt (286 mg, 2.12 mmol) and EDC (406 mg, 2.12 mmol) were added, followed by triethylamine (741 μL, 5.30 mmol). The reaction was stirred at room temperature for 12 h, after which time it was transferred to a separatory funnel using excess dichloromethane and added with 0.5M citric acid (2x75 mL) and saturated NaHCO 3 (2x75 mL) wash. Then the organic layer was treated with MgSO 4 Drying, filtration and concentration afforded the desired ketoamide (680 mg) in quantitative yield as a yellow solid, which was used directly in the subsequent step to form the oxazole.

[0923] The crude ketoamide (100 mg, 0.261 mmol) was dissolved in 2 mL of concentrated H 2 SO 4 middle. The reaction solution first turned bright orange, followed by the formation of a brown solid. ...

example 2

[0925]

[0926] Oxazole 2 was prepared using the conditions described for Example 1. [M-H] - = 264.1 m / z. Activity: B

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Abstract

The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof.

Description

Background technique [0001] Fatty acid amide hydrolase (FAAH), also known as oleamide hydrolase and anandamide amidohydrolase, is a membrane that degrades fatty acid primary amides and ethanolamides (including oleamide and anandamide) Intrinsic protein. FAAH degrades neuromodulatory fatty acid amides at their sites of action and is intimately involved in their regulation. [0002] FAAH has been shown to be involved in numerous biological processes, and inhibition of FAAH has been shown to be effective in the treatment of a variety of pathologies. For example, inhibition of FAAH has been shown to be useful in the treatment of chronic pain, acute pain, neuropathic pain, anxiety, depression, feeding behavior, movement disorders, glaucoma, neuroprotection, and cardiovascular disease. However, current FAAH inhibitors lack the target selectivity, biological activity and / or bioavailability required for in vivo studies and therapeutic use. Thus, to date, the therapeutic efficacy of...

Claims

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Application Information

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IPC IPC(8): A61K31/69A61P29/00A61P43/00
CPCA61K31/69A61P1/00A61P1/02A61P1/12A61P11/06A61P13/12A61P17/00A61P17/02A61P17/04A61P17/06A61P19/02A61P19/10A61P21/00A61P21/04A61P25/00A61P25/04A61P25/06A61P25/16A61P25/20A61P25/22A61P25/24A61P25/28A61P27/02A61P27/06A61P29/00A61P3/04A61P37/02A61P37/06A61P43/00A61P5/14A61P7/06A61P9/00A61P9/10A61P3/10C07F5/02C07F5/025
Inventor 马克·L·本克阿尔弗雷多·C·卡斯特罗凯瑟琳·A·埃文斯路易·格勒涅尔迈克尔·J·格罗根刘涛丹尼尔·A·斯奈德托马斯·T·帝比茨
Owner INFINITY PHARMA
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