title: Small-molecule endothelin receptor antagonists: a review of patenting activity across therapeutic areas.
abstract: In the field of nonpeptide NCEs with endothelin receptor antagonist activity, a burst in corporate IP filings occurred in the 1990s once the human endothelin system had been characterized, but patent activity has declined in the past decade. Universities have not been active in this area of research to a degree that would have led to many patent applications. While three endothelin receptor antagonists (bosentan, sitaxentan and ambrisentan) are already available for the treatment of pulmonary arterial hypertension, the use of such compounds for the larger therapy areas of heart failure, cancer and nephropathy is still being evaluated in late-stage clinical trials. Marketed and advanced-stage endothelin receptor blockers have remarkably little chemical diversity; thus, the substantially larger chemical space defined by patenting remains to be explored.
authors.affiliation: HM Pharma Consultancy, Wien, Austria. h.mucke@hmpharmacon.com
authors.forename: Hermann A M
authors.initials: HA
authors.lastname: Mucke
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology / Q000627:therapeutic use; D000077300:Bosentan; D015195:Drug Design; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000378:metabolism*; D006801:Humans; D006976:Hypertension, Pulmonary / Q000188:drug therapy / Q000503:physiopathology; D007555:Isoxazoles / Q000494:pharmacology / Q000627:therapeutic use; D010330:Patents as Topic; D010666:Phenylpropionates / Q000494:pharmacology / Q000627:therapeutic use; D011724:Pyridazines / Q000494:pharmacology / Q000627:therapeutic use; D013449:Sulfonamides / Q000494:pharmacology / Q000627:therapeutic use; D013876:Thiophenes / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000959:Antihypertensive Agents; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D007555:Isoxazoles; D010666:Phenylpropionates; D011724:Pyridazines; D013449:Sulfonamides; D013876:Thiophenes; C467894:ambrisentan; C106276:sitaxsentan; D000077300:Bosentan