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Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds

A compound, alkoxyl technology, applied in metabolic diseases, drug combinations, skin diseases, etc., can solve problems such as limited weight, weak effect, short half-life, etc.

Active Publication Date: 2015-09-30
PARION SCI DURHAM NC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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  • Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
  • Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
  • Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds

Examples

Experimental program
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Embodiment approach

[0063]

[0064] where, in each case,

[0065] n is an integer selected from 1, 2, 3, 4, 5 and 6;

[0066] R is for -CH 2 -(CHOH) r -CH 2 OH, wherein r is an integer selected from 1, 2, 3, 4, 5 or 6; and

[0067] R 1 selected from -(CH 2 ) q -Y or -(CH 2 ) q -O-Y;

[0068]q is an integer independently selected in each instance from 1, 2, 3, 4, 5 or 6;

[0069] Y is a phenyl, naphthyl or pyridyl ring, wherein each phenyl, naphthyl or pyridyl ring is substituted with 0, 1, 2 or 3 substituents independently selected from: halogen, -OH, -CN , -NO 2 , -NH 2 , -NH(C 1 -C 6 Alkyl), -N(C 1 -C 6 alkyl) 2 、C 1 -C 6 Alkyl, C 1 -C 6 Alkoxy and -CF 3 .

[0070] In each of the above described embodiments for formulas (III), (IV), (V) and (VI) or pharmaceutically acceptable salts thereof, there is yet another embodiment wherein:

[0071] n is an integer selected from 2, 3 and 4;

[0072] R is CH 2 -(CHOH) r -CH 2 OH, wherein r is an integer selected from 1, 2, 3...

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Abstract

The invention discloses an arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds. The present invention relates to the compound of the formula or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of 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 defenses', protection mechanisms. The main form of these innate defenses is cleaning these surfaces with liquids. In general, the amount of fluid layer on a mucosal surface reflects the balance between epithelial flu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/20A61K31/4965A61P11/12
CPCC07D241/20C07D241/34A61P1/00A61P1/02A61P1/04A61P1/10A61P11/00A61P11/02A61P11/06A61P11/08A61P11/12A61P11/14A61P15/02A61P17/00A61P17/16A61P25/02A61P27/02A61P27/16A61P29/00A61P3/12A61P31/00A61P31/04A61P31/12A61P31/16A61P37/06A61P43/00
Inventor 迈克尔·R·约翰逊
Owner PARION SCI DURHAM NC
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