title: Transient receptor potential vanilloid type 1 antagonists: a patent review (2011 - 2014).
abstract: BACKGROUND
  Transient receptor potential vanilloid type 1 (TRPV1) is a nonselective cation channel that can be activated by noxious heat, low pH and vanilloid compounds such as capsaicin. Since TRPV1 acts as an integrator of painful stimuli, TRPV1 antagonists can be used as promising therapeutics for new types of analgesics.
  
  
  METHODS
  This review article covers the patents that claim TRPV1 antagonists and were published during 2011 - 2014. The patent evaluation is organized according to the applicant companies, and the representative chemical entities with important in vitro and in vivo data are summarized.
  
  
  CONCLUSIONS
  Many pharmaceutical companies showed promising results in the discovery of potent small molecule TRPV1 antagonists, and recently, a number of small molecule TRPV1 antagonists have been advanced into clinical trials. Unfortunately, several candidate molecules showed critical side effects such as hyperthermia and impaired noxious heat sensation in humans, leading to their withdrawal from clinical trials. Some TRPV1 antagonists patented in recent years (2011 - 2014) overcame these undesirable side effects, making the development of TRPV1 antagonists much more promising.
authors: Ewha Womans University, National Leading Research Laboratory of Molecular Modeling and Drug Design, College of Pharmacy, Graduate School of Pharmaceutical Sciences, and Global Top 5 Research Program , Seoul 120-750 , Korea +82 2 3277 4503 ; +82 2 3277 2851 ; sunchoi@ewha.ac.kr.
authors: Yoonji
authors: Y
authors: Lee
authors: Sunhye
authors: S
authors: Hong
authors: Minghua
authors: M
authors: Cui
authors: Pankaz K
authors: PK
authors: Sharma
authors: Jeewoo
authors: J
authors: Lee
authors: Sun
authors: S
authors: Choi
mesh_terms: D000700:Analgesics / Q000009:adverse effects / Q000494:pharmacology*; D000818:Animals; D002986:Clinical Trials as Topic; D015195:Drug Design; D006801:Humans; D010330:Patents as Topic; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors*
chemical_list: D000700:Analgesics; D050916:TRPV Cation Channels; C494482:TRPV1 protein, human
keywords: TRPV1; TRPV1 antagonist; VR1; VR1 antagonist; capsaicin; transient receptor potential; vanilloid