COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA-2-ADRENERGIC RECEPTOR AGONIST ACTIVITY

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to a series of compounds selected from a group consisting of 4-(((R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)butyl-1-(4-((3-((S)-phenyl((((R)-quinuclidin-3-yloxy)carbonyl)amino)methyl)phenoxy)methyl)benzoyl)piperidine-4-carboxylate; (S)-4-(((R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)butyl-2-(4-((3-((S)-phenyl((((R)-quinuclidin-3-yloxy)carbonyl)amino)methyl)phenoxy)methyl)benzamido)propanoate; (S)-4-(((R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)butyl-3-methyl-2-(4-((3-((S)-phenyl((((R)-quinuclidin-3-yloxy)carbonyl)amino)methyl)phenoxy)methyl)benzamido) butanoate; (S)-4-(((R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)butyl-4-methyl-2-(4-((3-((S)-phenyl((((R)-quinuclidin-3-yloxy)carbonyl)amino)methyl)phenoxy)methyl)benzamido)pentanoate; 4-(((R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)butyl-2-methyl-2-(4-((3-((S)-phenyl((((R)-quinuclidin-3-yloxy)carbonyl)amino)methyl)phenoxy)methyl)benzamido)propanoate; (S)-4-(((R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)butyl-3-cyclohexyl-2-(4-((3-((S)-phenyl((((R)-quinuclidin-3-yloxy)carbonyl)amino)methyl)phenoxy)methyl)benzamido)propanoate and so on, which have the action of both a muscarinic receptor antagonist and beta 2-adrenergic receptor agonist.;EFFECT: invention also relates to a pharmaceutical composition, the use of said compounds to prepare a medicament for the prevention and/or treatment of bronchial obstructive or inflammatory diseases, a combination thereof with other active ingredients and an apparatus comprising said pharmaceutical composition.;6 cl, 18 ex