title: Phosphodiesterase 10A inhibitors: a 2009 - 2012 patent update.
abstract: BACKGROUND
  Inhibitors of the phosphodiesterase enzyme PDE10A have been the target for extensive investigations and huge drug discovery research efforts during the recent years. Although PDE10A with its 13 years history is a relatively newly discovered target, it has been paradigmatic for the new generation of 'high efficiency drug discovery'. Several companies now have clinical programs aiming at validating the clinical potential of PDE10A inhibitors. The majority of companies have been focusing on the treatment of schizophrenia since preclinical evidence suggests that a PDE10A inhibitor could provide antipsychotic, pro-cognitive and negative symptom efficacy.
  
  
  METHODS
  This article highlights and reviews research advances published in the patent literature since mid-2009 until mid-2012. The article is supplemented with selected publications from the scientific literature, emphasizing the possible involvement of PDE10A inhibitors in the treatment of schizophrenia.
  
  
  CONCLUSIONS
  Several compounds from various companies are currently undergoing clinical testing, dominated by compounds in clinical Phase I. Focus is mainly on CNS diseases and schizophrenia is the leading target indication.
authors.affiliation: Discovery Chemistry & DMPK, H. Lundbeck A/S, Valby, Denmark. jke@lundbeck.com
authors.forename: Jan
authors.initials: J
authors.lastname: Kehler
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology; D002493:Central Nervous System Diseases / Q000188:drug therapy / Q000503:physiopathology; D003071:Cognition / Q000187:drug effects; D015195:Drug Design; D006801:Humans; D010330:Patents as Topic; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology*; D010727:Phosphoric Diester Hydrolases / Q000187:drug effects*; D012559:Schizophrenia / Q000188:drug therapy / Q000503:physiopathology
chemical_list: D014150:Antipsychotic Agents; D010726:Phosphodiesterase Inhibitors; C119843:PDE10A protein, human; D010727:Phosphoric Diester Hydrolases