245118-94-9Relevant academic research and scientific papers
The discovery of N -[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy] ethoxy]-4-pyrimidinyl]- N ′-propylsulfamide (macitentan), an orally active, potent dual endothelin receptor antagonist
Bolli, Martin H.,Boss, Christoph,Binkert, Christoph,Buchmann, Stephan,Bur, Daniel,Hess, Patrick,Iglarz, Marc,Meyer, Solange,Rein, Josiane,Rey, Markus,Treiber, Alexander,Clozel, Martine,Fischli, Walter,Weller, Thomas
, p. 7849 - 7861 (2012/10/29)
Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy. This led to the discovery of a novel series of alkyl sulfamide substituted pyrimidines. Among these, compound 17 (macitentan, ACT-064992) emerged as particularly interesting as it is a potent inhibitor of ETA with significant affinity for the ET B receptor and shows excellent pharmacokinetic properties and high in vivo efficacy in hypertensive Dahl salt-sensitive rats. Compound 17 successfully completed a long-term phase III clinical trial for pulmonary arterial hypertension.
Agent for prophylaxis or treatment of dysuria
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, (2008/06/13)
A novel agent for prophylaxis or treatment of dysuria, which comprises as an active ingredient a compound of the formula [I]: wherein Ring A is a hydroxy-lower alkyl-substituted phenyl group, Ring B is a lower alkyl-substituted phenyl group, Alk is a lowe
Potent and selective ET-A antagonists. 2. Discovery and evaluation of potent and water soluble N-(6-(2-(Aryloxy)ethoxy)-4-pyrimidinyl) sulfonamide derivatives
Morimoto,Ohashi,Shimadzu,Kushiyama,Kawanishi,Hosaka,Kawase,Yasuda,Kikkawa,Yamauchi-Kohno,Yamada
, p. 3369 - 3377 (2007/10/03)
In the preceding article, we outlined the discovery and structure-activity relationship of a potent and selective ETA receptor antagonist 1 and its related compounds. Metabolites of 1 having potent selective ETA receptor antagonist a
