184779-19-9

Upstream product

• 1878-85-9 (2-methoxyphenoxy)acetic acid 
• 150726-89-9 (2-methoxyphenoxy)-malonic acid dimethyl ester 

Downstream Products

• 1393813-54-1 C₂₅H₂₅BrN₆O₇S 
• 1393813-67-6 N-(6-(2-hydroxyethoxy)-2-methoxy-5-(2-methoxyphenoxy)pyrimidin-4-yl)-N'-benzyl-sulfamide 
• 1393813-66-5 N-(2-chloro-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-N'-benzylsulfamide 
• 1393813-65-4 N-(2,6-dichloro-5-(2-methoxyphenoxy)pyrimidin-4-yl)-N'-benzylsulfamide 

Relevant 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

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.

Sulfonamide derivative and process for preparing the same

Novel sulfonamide derivatives of the formula ?I!: STR1 wherein Ring A and Ring B are substituted or unsubstituted monocyclic, bicyclic or tricyclic hydrocarbon, or substituted or unsubstituted heterocyclic group, Q is single bond, --O--, --S--, --SO--, --