Aralkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds

Abstract

The present invention relates to a compound of the following formula or a pharmaceutically acceptable salt thereof, a composition comprising the compound or a pharmaceutically acceptable salt thereof, a method for preparing the compound or a pharmaceutically acceptable salt thereof, and the use of the compound or a pharmaceutically acceptable salt thereof Its pharmaceutically acceptable salts are used to promote hydration of mucosal surfaces and treatments for diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema and pneumonia.

Description

technical field [0001] The present invention relates to novel aralkyl-substituted and aryloxyalkyl-substituted compounds (including in particular 3,5-diamino-6-chloro-N-(N-(4 -(4-(2-(aralkyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)formamidoyl)pyrazine-2-carboxamide and related compounds) and pharmaceutically acceptable salts thereof, compositions comprising said compounds and pharmaceutically acceptable salts thereof, methods of treatment and uses of said compounds and pharmaceutically acceptable salts thereof, and methods for preparing said compounds and pharmaceutically acceptable salts thereof salt method. Background technique [0002] The mucosal surfaces at the interface between the environment and the body have evolved a variety of "innate defense behaviors, i.e. protective mechanisms. The main form of these innate defenses is the cleaning of these surfaces with fluids. Generally speaking, the amount of fluid layer on the mucosal surface reflects the Th...

AI Technical Summary

Problems solved by technology

However, given the limited weight of drug that can be inhaled into the lungs; (2) rapid absorption, and thus exhibit an undesirably short half-life on mucosal surfaces; and (3) free dissociation from ENaC, these compounds are relatively weak effect

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