title: AT1 antagonists: a patent review (2008 - 2012).
abstract: BACKGROUND
  For two decades a class of pharmaceutical molecules with proved beneficial therapeutic properties, especially in hypertension, has been introduced in the market aiming to specifically prevent the detrimental effects of the peptide hormone Angiotensin II at the AT1 receptor. The prototype of this class was losartan and based on its structure, several drugs were launched and also called 'Sartans'. New structural features on these molecules can provide multi-target properties in the RAS or other systems. New methodologies were developed for the treatment of hypertension utilizing either AT1 antagonists alone or as cocktails.
  
  
  METHODS
  In this review article, authors aim to cover information provided by patents of the years 2008 - 2012. The rationale of writing this review article is to cover the most important patents which can forward the field with new important discoveries.
  
  
  CONCLUSIONS
  From the patent investigation it is clear that new areas on the subject are still offered for new discoveries. New structural features can be still considered in the synthetic compounds that can advance the knowledge and beneficial effects on diseases related to Angiotensin II and AT1 receptor. There is era also for new formulations (i.e., cyclodextrins, polymers and liposomes). The multitarget approach can be further strengthened and more combinations can be sought in the rational drug design for seeking cocktails. Furthermore, the revealing of the complexity of the RAS offers new avenues for novel targets and this must not be overlooked.
authors: University of Athens, Department of Chemistry , Panepistimiopolis Zografou 15771, Athens , Greece tmavrom@chem.uoa.gr.
authors: Thomas
authors: T
authors: Mavromoustakos
authors: George
authors: G
authors: Agelis
authors: Serdar
authors: S
authors: Durdagi
mesh_terms: D047228:Angiotensin II Type 1 Receptor Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D002626:Chemistry, Pharmaceutical; D004338:Drug Combinations; D055808:Drug Discovery; D006801:Humans; D006973:Hypertension / Q000188:drug therapy / Q000503:physiopathology; D008958:Models, Molecular; D010080:Oxazoles / Q000494:pharmacology; D010330:Patents as Topic; D012084:Renin-Angiotensin System / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D047228:Angiotensin II Type 1 Receptor Blockers; D004338:Drug Combinations; D010080:Oxazoles