title: Chloroquine-containing compounds: a patent review (2010 - 2014).
abstract: BACKGROUND
  Chloroquine (CQ) has been well known for its antimalarial effects since World War II. However, it is gradually being phased out from clinical use against malaria due to emergence of CQ-resistant Plasmodium falciparum strains. Besides low cost and tolerability, ongoing research has revealed interesting biochemical properties of CQ that have inspired its repurposing/repositioning in the management of various infectious/noninfectious diseases. Consequently, several novel compounds and compositions based on its scaffold have been studied and patented.
  
  
  METHODS
  In this review, patents describing CQ and its derivatives/compositions over the last 5 years are analyzed. The review highlights the rationale, chemical structures, biological evaluation and potential therapeutic application of CQ, its derivatives and compositions.
  
  
  CONCLUSIONS
  Repurposing efforts have dominantly focused on racemic CQ with no studies exploring the effect of the (R) and (S) enantiomers, which might potentially have additional benefits in other diseases. Additionally, evaluating other similarly acting antimalarials in clinical use and structural analogs could help maximize the intrinsic value of the 4-aminoquinolines. With regard to cancer therapy, successful repurposing of CQ-containing compounds will require linking the mode of action of these antimalarials with the signaling pathways that drive cancer cell proliferation to facilitate the development of a 4-amino-7-chloroquinoline that can be used as a synergistic partner in anticancer combination chemotherapy.
authors.affiliation: a 1 University of Cape Town, Department of Chemistry , Rondebosch 7701, South Africa.
authors.forename: Paul M
authors.initials: PM
authors.lastname: Njaria
authors.forename: John
authors.initials: J
authors.lastname: Okombo
authors.forename: Nicholas M
authors.initials: NM
authors.lastname: Njuguna
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology; D002738:Chloroquine / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D058492:Drug Repositioning; D006801:Humans; D010330:Patents as Topic; D013237:Stereoisomerism
chemical_list: D000962:Antimalarials; D002738:Chloroquine
keywords: Plasmodium falciparum; aminoquinoline; antimalarial; cancer; chloroquine derivatives; hydroxychloroquine; malaria; patent; repositioning; repurposing