Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
AssigneeParion Sciences, Inc.
InventorMichael R. Johnson
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Abstract
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.
Claims43
A method for blocking sodium channels in a subject or a cell, the method comprising administering to the subject or cell a compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein Ar is a moiety selected from the group of:
- X is selected from —CH2—, —O—, and —S—;
- n is an integer selected from 0, 1, 2, 3, 4, 5, and 6;
- R is a polyhydroxylated alkyl group having from 3 to 8 carbon atoms;
- R1 is selected from —(CH2)q—Y and —(CH2)q—O—Y;
- q is an integer selected independently in each instance from 1, 2, 3, 4, 5, and 6;
- and
- Y is a phenyl, naphthyl, or pyridyl ring, with each phenyl, naphthyl, or pyridyl ring substituted by 0, 1, 2, or 3 substituents independently selected from halogen, —OH, —CN, —NO2, —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)2, C1-C6 alkyl, C1-C6 alkoxy, and —CF3.
A pharmaceutical composition comprising hypertonic saline and a compound selected from the group consisting of:
- and pharmaceutically acceptable salts thereof.
A pharmaceutical composition comprising an osmolyte and a compound selected from the group consisting of:
- and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.