title: Therapeutic uses of melatonin and melatonin derivatives: a patent review (2012 - 2014).
abstract: BACKGROUND
  Melatonin is a neurohormone involved in the regulation of circadian rhythms, with potent antioxidant activity. It has a wide functional repertoire, with effects almost on all tissues and organs. It is mainly used as a dietary supplement for sleep regulation and re-synchronization of disrupted circadian rhythms. Melatonin has very low toxicity, but some pharmacokinetic issues, such as limited oral bioavailability and short half-life, limit its tissue availability.
  
  
  METHODS
  Patents and patent applications from 2012 to September 2014 in which melatonin or synthetic analogues are claimed for the prevention or treatment of pathological conditions.
  
  
  CONCLUSIONS
  Melatonin is considered a valuable substance that can be safely administered for the prevention and treatment of many diverse diseases. A major trend in 2012 - 2014 patents is the co-administration of melatonin with other drugs to increase the efficacy of the treatment and reduce side-effects. Two different actions have been combined in hybrid ligands (e.g., melatonin-tamoxifen and melatonin-tacrine derivatives). Further experimental evidence is needed to support the usefulness of these approaches. The number of new melatonin analogues has shown a marked decrease in the past 3 years, with claimed applications mainly as hypnotic or antioxidant agents.
authors.affiliation: Università degli Studi di Parma, Dipartimento di Farmacia , Parco Area delle Scienze 27/A, I-43124 Parma , Italy +39 0521 905061 ; +39 0521 905006 ; silvia.rivara@unipr.it.
authors.forename: Silvia
authors.initials: S
authors.lastname: Rivara
authors.forename: Daniele
authors.initials: D
authors.lastname: Pala
authors.forename: Annalida
authors.initials: A
authors.lastname: Bedini
authors.forename: Gilberto
authors.initials: G
authors.lastname: Spadoni
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001682:Biological Availability; D002940:Circadian Rhythm / Q000502:physiology*; D019587:Dietary Supplements; D006207:Half-Life; D006801:Humans; D006993:Hypnotics and Sedatives / Q000493:pharmacokinetics / Q000627:therapeutic use; D008024:Ligands; D008550:Melatonin / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010330:Patents as Topic; D014018:Tissue Distribution
chemical_list: D000975:Antioxidants; D006993:Hypnotics and Sedatives; D008024:Ligands; D008550:Melatonin
keywords: MT1 receptor; MT2 receptor; TIK-301; agomelatine; antioxidant activity; controlled-release formulation; melatonin; radical scavenger; ramelteon; tasimelteon