Aza-indole derivatives useful as modulators of FAAH

A compound, CH2 technology, applied in the direction of active ingredients of heterocyclic compounds, anti-toxic agents, anti-inflammatory agents, etc.

Inactive Publication Date: 2013-02-06
MERCK & CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thus, inhibition of FAAH activity in vivo results in reductions in body fat, body weight, caloric intake, and hepatic triglyceride levels

Method used

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  • Aza-indole derivatives useful as modulators of FAAH
  • Aza-indole derivatives useful as modulators of FAAH
  • Aza-indole derivatives useful as modulators of FAAH

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Experimental program
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Effect test

preparation example Construction

[0473] Preparation of lysates and microsomes

[0474] CHO cells expressing FAAH were used to prepare crude cell lysates or microsomal fractions. To harvest the cells, decant the tissue culture medium slowly and replace the monolayer with Ca-free ++ Mg ++ The cells were washed three times with PBS and recovered after 15 min in enzyme-free dissociation medium (Millipore Corp, Billerica, MA). Cells were harvested by centrifugation at 2000 rpm for 15 min, and the cell pellet was resuspended with 50 mM HEPES (pH 7.4) containing 1 mM EDTA and the protease inhibitors aprotinin (1 mg / ml) and leupeptin (100 μM). hanging. Cell lysates were recovered after sonicating the suspension at 4°C and centrifuging at 12,000xg (14,600rpm, SS34 rotor) for 20 min at 4°C to form cell debris, nuclei, peroxisomes, lysosomes, and mitochondria crude pellets; supernatants or cell lysates were used for FAAH enzyme assays. In some cases, FAAH-enriched microsomal fractions were prepared by further cen...

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PUM

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Abstract

The present invention is directed to certain Aza-Indole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application Serial No. 61 / 331,974, filed May 6, 2010. Background of the invention [0003] The present application discloses compounds that inhibit the activity of fatty acid amide hydrolase (FAAH), compositions comprising the compounds, and methods of using the same. Compounds disclosed herein that are fatty acid amide hydrolase (FAAH) inhibitors are useful in the treatment of diseases, conditions or disorders that would benefit from inhibition of fatty acid amide hydrolase and an increase in endogenous fatty acid amides. [0004] Fatty acid amide hydrolase (FAAH) is abundantly expressed throughout the CNS (Freund et al., Physiol. Rev. 2003; 83:1017-1066) and in surrounding tissues such as, for example, pancreas, brain, kidney, skeletal muscle, placenta and Liver (Giang, D. K. et al., Proc. Natl. Acad. Sci. U.S.A. 1997, 94, 2238-2242; Cravatt et al., Proc. Natl. Acad....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/555A61K31/40
CPCC07D519/00C07D471/04A61P1/04A61P1/08A61P1/12A61P1/16A61P13/02A61P13/10A61P15/06A61P19/02A61P19/08A61P21/02A61P25/00A61P25/04A61P25/06A61P25/08A61P25/14A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P25/30A61P25/32A61P27/02A61P27/06A61P29/00A61P3/00A61P3/04A61P31/04A61P31/12A61P35/00A61P3/06A61P39/02A61P43/00A61P9/10A61P9/12
Inventor A.M.瓦尔吉P.G.南特梅特K.P.穆尔R.A.斯托尔L.瓦萨洛C.克里特索拉斯
Owner MERCK & CO INC
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