Novel Inhibitors of N-Acylethanolamine-Hydrolyzing Acid Amidase (NAAA)

Tech ID: 18747 / UC Case 2007-532-0

Background

Ethanoloamides of long-chain fatty acids, termed N-acylethanolamines (NAEs) have been reported to have a variety of biological activities. NAEs are a substrate of N-acylethanolamine-hydrolyzing acid amidase (NAAA) that catalytically hydrolyze NAEs to ethanolamine and the corresponding fatty acid. The catalytic activity of NAAA is distinct from that of fatty acid amide hydrolase (FAAH) and NAAA exhibits a preference for N-palmitoylethanolamine (PEA) over other NAEs. PEA has anti-inflammatory, anti-nociceptive, immunosuppressive, neuroprotective and also anti-oxidant activity. These characteristics make NAAA an excellent therapeutic target for discovery of novel compounds to treat pain, inflammation, and other conditions that may benefit from modulating the levels of endogenous fatty-acid ethanolamides, particularly PEA.

Technology Description

Current analgesic and anti-inflammatory agents produce side effects, limited efficacy and there remains an unmet need for new therapeutics for pain and inflammatory disorders. UC Irvine investigators have discovered a new class of compounds that inhibit N-acylethanolamine-hydrolyzing acid amidase (NAAA). Several novel NAAA inhibitors showed submicromolar activity in vitro enzymatic assays. Potent and selective compounds were further evaluated for anti-inflammatory effects in animal models. An increase in PEA levels, modulation of the immune cell infiltrate, and a reduction in inflammation were demonstrated. NAAA inhibitors will be useful to alleviate conditions associated with a reduced concentration of N-palmitoylethanolamine (PEA), such as pain and inflammation, and neurodegenerative disorders.

Applications

Various NAAA inhibitors were identified that will be useful in the treatment of conditions associated with reduced levels of endogenous ethanolamides. NAAA inhibitors represent therapeutic agents for the treatment of inflammatory diseases (rheumatoid arthritis, osteoarthritis, asthma, psoriasis), pain, metabolic diseases, and neurodegenerative diseases such as Alzheimer's Disease.

Patent Status

Country Type Number Dated Case
United States Of America Issued Patent 9,908,848 03/06/2018 2011-056
Japan Issued Patent 6266528 01/05/2018 2011-057
Australia Issued Patent 2012340519 01/03/2018 2011-057
Austria Issued Patent 2782567 03/22/2017 2011-057
Germany Issued Patent 2782567 03/22/2017 2011-057
France Issued Patent 2782567 03/22/2017 2011-057
United Kingdom Issued Patent 2782567 03/22/2017 2011-057
Italy Issued Patent 2782567 03/22/2017 2011-057
Monaco Issued Patent 2782567 03/22/2017 2011-057
Turkey Issued Patent 2782567 03/22/2017 2011-057
United States Of America Issued Patent 9,353,075 05/31/2016 2011-057
Austria Issued Patent 2200564 05/04/2016 2007-532
Switzerland Issued Patent 02200564 05/04/2016 2007-532
Germany Issued Patent 2200564 05/04/2016 2007-532
Denmark Issued Patent 2200564 05/04/2016 2007-532
European Patent Office Issued Patent 2200564 05/04/2016 2007-532
Spain Issued Patent 2200564 05/04/2016 2007-532
France Issued Patent 2200564 05/04/2016 2007-532
United Kingdom Issued Patent 2200564 05/04/2016 2007-532
Ireland Issued Patent 2200564 05/04/2016 2007-532
Italy Issued Patent 2200564 05/04/2016 2007-532
Luxembourg Issued Patent 2200564 05/04/2016 2007-532
Monaco Issued Patent 2200564 05/04/2016 2007-532
Netherlands (Holland) Issued Patent 2200564 05/04/2016 2007-532
Norway Issued Patent 2200564 05/04/2016 2007-532
Sweden Issued Patent 2200564 05/04/2016 2007-532
United States Of America Issued Patent 9,321,743 04/26/2016 2007-532
China Issued Patent 200880111269.X 06/10/2015 2007-532
Australia Issued Patent 2008310628 12/18/2014 2007-532
Japan Issued Patent 5526362 04/25/2014 2007-532
New Zealand Issued Patent 582970 08/08/2011 2007-532
United States Of America Published Application 20160256432 09/08/2016 2007-532
United States Of America Published Application 20160068482 03/10/2016 2013-109
United States Of America Published Application 20100311711 12/09/2010 2007-532
Canada Published Application 2011-057
 

Additional Patents Pending

Contact

Learn About UC TechAlerts - Save Searches and receive new technology matches

Other Information

Categorized As

  • AN INTEGRAL PART OF
  • Institute for Innovation Logo
  • Institute for Innovation Logo

University of California, Irvine Invention Transfer Group
5141 California Avenue, Suite 200, Irvine,CA 92697-7700
Tel: 949.824.2683 | Fax: 949.824.3880
www.ota.uci.edu | ota@uci.edu

© 2009 - 2018, The Regents of the University of California
Terms of use | Privacy Notice