169547-22-2

Upstream product

• 7524-52-9 (S)-tryptophan methyl ester hydrochloride 
• 2592-95-2 benzotriazol-1-ol 
• 1892-57-5 N-(3-dimethylaminopropyl)-N-ethylcarbodiimide 
• 184698-56-4 N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5-isoxazolyl)-phenyl]-alanine 
• 184698-55-3 N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5-isoxazolyl)-phenyl]-alanine ethyl ester 
• 184698-53-1 3-[4-(5-isoxazolyl)-phenyl]-alanine ethyl ester 
• 184698-54-2 N-(3,5-dimethylbenzoyl)-3-[4-(5-isoxazolyl)-phenyl]-alanine ethyl ester 
• 169547-50-6 5-(4-bromomethyl-phenyl)-isoxazole 
• 122-00-9 para-methylacetophenone 
• 7064-35-9 5-(4-methylphenyl)isoxazole 
• 499-06-9 3,5-dimethylbenzoic acid 

Downstream Products

• 169545-68-0 [N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5-isoxazolyl)-phenyl]-(D)-alanyl]-(L)-tryptophane 

Relevant academic research and scientific papers

Discovery of IRL 3461: A novel and potent endothelin antagonist with balanced ET(A)/ET(B) affinity

IRL 3461, N-butanesulfonyl-[N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5- isoxazolyl)-phenyl]-alanyl]-(L)-valineamide, a potent and bifunctional (ET(A) + ET(B)) [Ki(ET(A))=1.8 nM, Ki(ET(B))=1.2 nM] antagonist was discovered by structural modification of IRL 2500, an ET(B) selective antagonist. IRL 3461 was found to be stable on incubation with human, rat, mouse, and guinea pig plasmas.

Antagonists of endothelin receptors

The present invention provides novel compounds having pharmacological properties represented by the general formula I STR1 processes for the manufacture, pharmaceutical compositions and the use of the compounds of formula I and salts thereof.