329923-33-3

Upstream product

• 150727-72-3 4,6-dichloro-5-(o-methoxyphenoxy)-2-(pyridin-4-yl)-pyrimidine 
• 150728-08-8 5-(o-methoxyphenoxy)-4,6-dihydroxy-2-(pyridin-4-yl)-pyrimidine 
• 6345-27-3 4-amidinopyridine hydrochloride 

Downstream Products

• 346672-35-3 5-isopropyl-N-[6-(4-phenoxy-but-2-ynyloxy)-5-(2-methoxy-phenoxy)-2-pyrid in-4-yl-pyrimidin-4-yl]-2-pyridine sulfonamide 
• 346671-41-8 5-isopropyl-N-[6-(4-hydroxy-2-butynyloxy)-5-(o-methoxyphenoxy)-2-(4-pyridyl)-4-pyrimidinyl]-2-pyridine sulfonamide 
• 290815-27-9 5-isopropyl-pyridine-2-sulfonic acid [6-methoxy-5-(2-methoxy-phenoxy)-2-pyridin-4-yl-pyrimidin-4-yl]-amide 

Relevant academic research and scientific papers

The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists

A series of compounds structurally related to bosentan 1 featuring an unsaturated side chain at position 6 of the core pyrimidine have been studied for their potential to block the ETA and ETB receptor. Incorporation of a 2-butyne-1,4-diol linker bearing a pyridyl carbamoyl moiety led to in vitro highly potent endothelin receptor antagonists (e.g., 70 and 75). The propargyl derivative 26 significantly reduced blood pressure in in vivo model studies with hypertensive salt-sensitive Dahl rats.

Butyne diol derivatives

The present invention relates to novel butyne diol derivatives of the general formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of the general formula I and especially their use as endothelin receptor antagonists.

Heterocyclic sulfonamides

The compounds of formula (I) wherein R1has the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.