Tezosentan Actelion

S. De Servi

Research output: Contribution to journalArticlepeer-review


Novel sulfonamides are claimed which are endothelin receptor inhibitors. They are potentially useful for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischemia, vasospasm and angina pectoris. Processes by which there compounds may be synthesized are claimed. Six compounds were shown to inhibit the binding of endothelin to recombinant endothelin receptors. Data are presented in one table. IC50 values ranged from 1 to 6 nM, the former being exhibited by the specified compound. These six compounds also inhibited endothelin-induced contractions in isolated rat aorta rings. Six processes by which these compounds may be synthesized are described. 75 Compounds are exemplified by syntheses, including the specified compound, 2-[6-(1,3-benzodioxol-5-ylsulfonylamino)-5-(2-methoxyphenoxy)-2-2-1H-(tetrazol-5 -yl)-pyri-din-4-yl)-pyrimidin-4-yloxy]-ethylpyridin-2-yl-carbam-ate, which is one of 82 compounds specifically claimed.

Original languageEnglish
Pages (from-to)400-402
Number of pages3
JournalCurrent Opinion in Cardiovascular, Pulmonary and Renal Investigational Drugs
Issue number4
Publication statusPublished - 2000

ASJC Scopus subject areas

  • Pharmacology


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