title: Novel 1H-1,2,3-, 2H-1,2,3-, 1H-1,2,4- and 4H-1,2,4-triazole derivatives: a patent review (2008 - 2011).
abstract: BACKGROUND
  The triazoles represent a class of five-membered heterocyclic compounds of great importance for the preparation of new drugs with diverse biological activities because they may present several structural variations with the same numbers of carbon and nitrogen atoms. Due to the success of various triazoles that entered the pharmaceutical market and are still being used in medicines, many companies and research groups have shown interest in developing new methods of synthesis and biological evaluation of potential uses for these compounds. In this review, the authors explored aspects of patents for the 1H-1,2,3-, 2H-1,2,3-, 1H-1,2,4- and 4H-1,2,4-triazole families, including prototypes being considered in clinical studies between 2008 and 2011.
  
  
  METHODS
  The triazoles have been studied for over a century as an important class of heterocyclic compounds and still attract considerable attention due to their broad range of biological activities. More recently, there has been considerable interest in the development of novel triazoles with anti-inflammatory, antiplatelet, antimicrobial, antimycobacterial, antitumoral and antiviral properties and activity against several neglected diseases. This review emphasizes recent perspective and advances in the therapeutically active 1H-1,2,3-, 2H-1,2,3-, 1H-1,2,4- and 4H-1,2,4-triazole derivative patents between 2008 and 2011, covering the development of new chemical entities and new pharmaceuticals. Many studies have focused on these compounds as target structures and evaluated them in several biological targets.
  
  
  CONCLUSIONS
  The preparation of 1H-1,2,3-, 2H-1,2,3-, 1H-1,2,4- and 4H-1,2,4-triazole derivatives brings to light several issues. There is a need to find new, more efficient preparations for these triazoles that take into consideration current issues in green chemistry, energy saving and sustainability. New diseases are discovered and new viruses and bacteria continue to challenge mankind, so it is imperative to find new prototypes for these new diseases. Of great urgency is finding prototypes against bacteria that continue to increase resistance and for neglected diseases that affect a large part of humanity, especially the poor and vulnerable.
authors.affiliation: Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, 24020-150 Niterói, RJ, Brazil. cegvito@vm.uff.br
authors.forename: Vitor F
authors.initials: VF
authors.lastname: Ferreira
authors.forename: David R
authors.initials: DR
authors.lastname: da Rocha
authors.forename: Fernando C
authors.initials: FC
authors.lastname: da Silva
authors.forename: Patrícia G
authors.initials: PG
authors.lastname: Ferreira
authors.forename: Núbia A
authors.initials: NA
authors.lastname: Boechat
authors.forename: Jorge L
authors.initials: JL
authors.lastname: Magalhães
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D004345:Drug Industry / Q000706:statistics & numerical data; D006801:Humans; D010330:Patents as Topic / Q000706:statistics & numerical data; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D014230:Triazoles