title: Fatty acid amide hydrolase inhibitors: a patent review (2009-2014).
abstract: BACKGROUND
  Fatty acid amide hydrolase (FAAH) is a key enzyme responsible for the degradation of the endocannabinoid anandamide. FAAH inactivation is emerging as a strategy to treat several CNS and peripheral diseases, including inflammation and pain. The search for effective FAAH inhibitors has thus become a key focus in present drug discovery.
  
  
  METHODS
  Patents and patent applications published from 2009 to 2014 in which novel chemical classes are claimed to inhibit FAAH.
  
  
  CONCLUSIONS
  FAAH is a promising target for treating many disease conditions including pain, inflammation and mood disorders. In the last few years, remarkable efforts have been made to develop new FAAH inhibitors (either reversible and irreversible) characterized by excellent potency and selectivity, to complete the arsenal of tools for modulating FAAH activity. The failure of PF-04457845 in a Phase II study on osteoarthritis pain has not flattened the interest in FAAH inhibitors. New clinical trials on 'classical' FAAH inhibitors are now ongoing, and new strategies based on compounds with peculiar in vivo distribution (e.g., peripheral) or with multiple pharmacological activities (e.g., FAAH and COX) are under investigation and could boost the therapeutic potential of this class in the next future.
authors.affiliation: a 1 Università degli Studi di Parma, Dipartimento di Farmacia , Parco Area delle Scienze 27/A, Parma, Italy.
authors.forename: Alessio
authors.initials: A
authors.lastname: Lodola
authors.affiliation: b 2 Università degli Studi di Parma, Dipartimento di Farmacia , Parco Area delle Scienze 27/A, Parma, Italy.
authors.forename: Riccardo
authors.initials: R
authors.lastname: Castelli
authors.affiliation: c 3 Università degli Studi di Parma, Dipartimento di Farmacia , Parco Area delle Scienze 27/A, Parma, Italy +39 0521 905059 ; +39 0521 905006 ; marco.mor@unipr.it.
authors.forename: Marco
authors.initials: M
authors.lastname: Mor
authors.affiliation: a 1 Università degli Studi di Parma, Dipartimento di Farmacia , Parco Area delle Scienze 27/A, Parma, Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Rivara
mesh_terms: D000581:Amidohydrolases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D001095:Arachidonic Acids / Q000378:metabolism; D002493:Central Nervous System Diseases / Q000188:drug therapy / Q000201:enzymology; D015195:Drug Design; D063388:Endocannabinoids / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000201:enzymology; D010146:Pain / Q000188:drug therapy / Q000201:enzymology; D010330:Patents as Topic; D053284:Polyunsaturated Alkamides / Q000378:metabolism; D000099252:Fatty Acid Amide Hydrolases
chemical_list: D000581:Amidohydrolases; D001095:Arachidonic Acids; D063388:Endocannabinoids; D004791:Enzyme Inhibitors; D053284:Polyunsaturated Alkamides; D000099252:Fatty Acid Amide Hydrolases; C078814:anandamide
keywords: PF-04457845; URB597; endocannabinoid system; fatty acid amide hydrolase; fatty acid ethanolamides