title: T-type calcium channels inhibitors: a patent review.
abstract: BACKGROUND
  T-type calcium channels are transmembrane proteins that regulate calcium entry in the cell in a voltage-dependent manner. Intracellular calcium levels are the key to many physiological processes, ranging from neuron firing to cardiac pacemaking. Inhibition of T-type calcium channels is heralded as a potential treatment to peripheral and CNS disorders, including hypertension, heart failure, sleep, epilepsy, drug addiction and neuropathic pain.
  
  
  METHODS
  A comprehensive summary of patent literature disclosing T-type calcium channels inhibitors is provided.
  
  
  RESULTS
  In all, 46 patent applications including 15 chemical structure classes are reviewed. Available in vitro, in vivo and clinical results are also discussed.
  
  
  CONCLUSIONS
  Several selective T-type calcium channels inhibitors with demonstrated in vitro and in vivo effects, including one Phase I clinical candidate, are now available. While future clinical results will be paramount to assess target validity in patients, these novel inhibitors represent excellent tools to further investigate the role of T-type channels in pathophysiological conditions.
authors.affiliation: AstraZeneca R&D, Lead Generation, SE-431 83 Mölndal, Sweden. fabrizio.giordanetto@astrazeneca.com
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Giordanetto
authors.forename: Laurent
authors.initials: L
authors.lastname: Knerr
authors.forename: Andreas
authors.initials: A
authors.lastname: Wållberg
mesh_terms: D000818:Animals; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D020747:Calcium Channels, T-Type / Q000187:drug effects* / Q000378:metabolism; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D010330:Patents as Topic
chemical_list: D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D002118:Calcium