3,5-diamino-6-chloro-N-(N-(4-phenylbutyl)carbamimidoyl) pyrazine-2-carboxamide compounds

摘要

The present invention relates compounds of the formula:;
or pharmaceutically acceptable salts thereof, useful as sodium channel blockers, 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 cystic fibrosis, chronic obstructive pulmonary disease, asthma, bronchiectasis, acute and chronic bronchitis, emphysema, and pneumonia.

主权项

1. A compound of the formula: wherein Ar is a moiety selected from the group of: X is selected from —CH2—, —O—, or —S—; R1 and R2 are independently selected from H and C1-C6 alkyl; or R1 and R2 together with the nitrogen atom to which they are bound form a 5-membered or 6-membered heterocyclic ring optionally containing one additional ring heteroatom selected from N or O; R3 is an alkyl group having from 3 to 8 carbon atoms or a polyhydroxylated alkyl group having from 3 to 8 carbon atoms; R4 is a polyhydroxylated alkyl group having from 3 to 8 carbon atoms; and R5 is selected from H or C1-C3 alkyl; or a pharmaceutically acceptable salt thereof.