title: Artemisinin derivatives: a patent review (2006 - present).
abstract: BACKGROUND
  The isolation of artemisinin from an ancient Chinese remedy in the early 1970s heralded the beginning of a new era in antimalarial drug therapy culminating in artemisinin-based combination therapies currently being the mainstay of malaria treatment worldwide. Ongoing research on this compound and its derivatives has revealed its potential use in treating other infectious and noninfectious diseases.
  
  
  METHODS
  This review provides a summary of patents published globally from January 2006 to June 2012 covering promising artemisinin derivatives and artemisinin-based drug combinations developed for use in various therapeutic areas.
  
  
  CONCLUSIONS
  The diversity of semi-synthetic artemisinin derivatives has been limited to the same design strategy of modifying the artemisinin molecule at the same positions due to inherent synthetic challenges. To address this, future endeavors should include: the use of biotransformation strategies to modify other positions in the sesquiterpene ring while retaining the endoperoxide bridge; the design and synthesis of synthetic ozonides based on the pharmacophoric endoperoxide motif and drug repositioning approaches to artemisinin-based combination therapy. A better understanding of the mechanism of action of artemisinin derivatives and their biomolecular targets may provide an invaluable tool for the development of derivatives with a wider array of activity and greater clinical utility than currently appreciated.
authors.affiliation: Department of Chemistry & Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Private Bag X3, Rondebosch 7701, South Africa.
authors.forename: Nicholas M
authors.initials: NM
authors.lastname: Njuguna
authors.forename: Dennis S B
authors.initials: DS
authors.lastname: Ongarora
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000494:pharmacology*; D037621:Artemisinins / Q000138:chemical synthesis / Q000494:pharmacology*; D055808:Drug Discovery; D006801:Humans; D015394:Molecular Structure; D010330:Patents as Topic; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D037621:Artemisinins; C031327:artemisinin