title: Novel calcium sensing receptor ligands: a patent survey.
abstract: BACKGROUND
  In the parathyroid gland, the calcium sensing receptor responds to small changes in circulating levels of Ca(2+), and consequently stimulates or inhibits the secretion of parathyroid hormone (PTH). Thus, ligands potentiating the action of calcium (calcimimetics) lead to decreased PTH secretion and can thus be useful for the treatment of hyperparathyroidism. On the other hand, ligands which antagonize the action of calcium (calcilytics) stimulate PTH secretion, favoring bone tissue regeneration.
  
  
  METHODS
  This review first discusses the rapid development of calcimimetics (only one of which has been approved for the treatment of hyperparathyroidism) followed by that of calcilytics (none of which has as yet been approved for the treatment of osteoporosis). Peer-reviewed articles generated by these patents are also surveyed.
  
  
  CONCLUSIONS
  The rapid progress in developing a clinically approved calcimimetic has not been matched by an identical success in finding an orally available calcilytic useful for the treatment of osteoporosis. However, the growing importance of osteoporosis as a debilitating disease is a stimulating factor in discovering such compounds.
authors.affiliation: Institut de Chimie des Substances Naturelles, UPR 2301, CNRS, Avenue de la Terrasse, 91198 Gif-sur-Yvette, France. robert.dodd@icsn.cnrs-gif.fr
authors.forename: Lionel
authors.initials: L
authors.lastname: Kiefer
authors.forename: Simon
authors.initials: S
authors.lastname: Leiris
authors.forename: Robert H
authors.initials: RH
authors.lastname: Dodd
mesh_terms: D000818:Animals; D057966:Calcimimetic Agents / Q000627:therapeutic use; D006801:Humans; D006961:Hyperparathyroidism / Q000188:drug therapy; D008024:Ligands; D009281:Naphthalenes / Q000627:therapeutic use; D010024:Osteoporosis / Q000188:drug therapy; D010330:Patents as Topic; D044169:Receptors, Calcium-Sensing / Q000037:antagonists & inhibitors / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship
chemical_list: D057966:Calcimimetic Agents; D008024:Ligands; C436740:N-(2-hydroxy-3-(2-cyano-3-chlorophenoxy)propyl)-1,1-dimethyl-2-(2-nephthyl)ethylamine; D009281:Naphthalenes; D044169:Receptors, Calcium-Sensing