150727-24-5

Upstream product

• 20730-58-9 2-(2-Methoxyphenoxy)propanedioic acid diethyl ester 
• 90-05-1 2-methoxy-phenol 
• 150727-23-4 4,6-dichloro-5-(o-methoxyphenoxy)-pyrimidine 
• 202288-08-2 5-(2-methoxy-phenoxy)-1H-pyrimidine-4,6-dione 
• 150726-89-9 (2-methoxyphenoxy)-malonic acid dimethyl ester 
• 150727-22-3 5-(o-methoxyphenoxy)-4,6-dihydroxy-pyrimidine 

Downstream Products

• 150727-21-2 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(3-methoxy-phenoxy)-4-pyrimidinyl]-benzenesulphonamide 
• 346671-52-1 4-tert.-butyl-N-[6-(4-hydroxy-2-butynyloxy)-5-(o-methoxyphenoxy)-4-pyrimidinyl]-benzene sulfonamide 
• 202288-09-3 4-tert-butyl-N-[6-(4-hydroxy-butoxy)-5-(2-methoxy-phenoxy)-pyrimidin-4-yl]-benzenesulfonamide 

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.

6 alkoxy-4-pyrimidinyl bis-sulfonamides

The present invention relates to novel bis-sulfonamides represented, for example, by formula I below and a pure diastereomer, a mixture of diastereomers, a diastereomeric racemate, a mixture of diastereomeric racemates and meso-forms and a pharmaceutically acceptable salt thereof, wherein R1represents aryl; aryl-lower alkyl; aryl-lower alkenyl; heteroaryl; or heteroaryl-lower alkyl; and R2represents lower alkyl; trifluoromethyl; lower alkoxy-lower alkyl; lower alkenyl; lower alkynyl; aryl; aryl-lower alkyl; aryl-lower alkenyl; heterocyclyl; heterocyclyl-lower alkyl; heteroaryl; heteroaryl-lower alkyl; cycloalkyl; or cycloalkyl-lower alkyl. The present invention also relates to a process for manufacturing those compounds, pharmaceutical compositions containing one or more of those compounds as endothelin antagonists, and a method of treating a subject having a disorder involving endothelin with the compounds of the invention.

Synthesis and structure-activity relationships of potent and orally active sulfonamide ETB selective antagonists

The synthesis and structure-activity relationships of a series of N-pyrimidinyl benzenesulfonamides as ETB selective antagonists are described. N-Isoxazolyl benzenesulfonamide 1a, previously reported, was selected as a lead compound, and isosteric replacement of the isoxazole ring of 1a with a pyrimidine ring led to the discovery of the highly potent ETB selective antagonist 6e with oral bioavailability. Modification of the terminal aldehyde group at the 6-position of the pyrimidine ring was investigated, and malonate 15b and acylhydrazone 16f were found to be equipped to aldehyde 6e. Compound 6e showed ETB antagonistic activity on in vivo evaluation. Copyright

SULFONAMIDES

The novel sulfonamides of formula I, STR1 in which the symbols R. sup.1-R 9, R a, R b, X, Y and n have the significance given in the description and salts thereof can be used for the treatment of circulatory disorders, especially hypertension, ischemia, vasopasms and angina pectoris.