Conjugates of sodium channel blockers and methods of using...

C - Chemistry – Metallurgy – 07 – D

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C07D 241/26 (2006.01) A61K 31/495 (2006.01) A61K 31/70 (2006.01) A61P 11/12 (2006.01) C07D 401/12 (2006.01) C07H 19/10 (2006.01) C07H 19/207 (2006.01)

Patent

CA 2378181

Compounds of the general formula P1-L-P2; wherein "P1" is a pyrazinoylguanidine sodium channel blocker, "L" is a linking group, and "P2" is either (i) a pyrazinoylguanidine sodium channel blocker or (ii) a P2Y2 receptor agonist, are disclosed. Pharmaceutical formulations containing the same and methods of use thereof to hydrate mucosal surfaces such as airway mucosal surfaces are also disclosed.

Cette invention a trait à des composés correspondant à la formule générale P¿1?-L-P¿2? dans laquelle P¿1? représente un bloqueur de canal sodique à base de pyrazinoylguanidine, L représente un groupe de liaison et P¿2? représente, soit un bloqueur de canal sodique à base de pyrazinoylguanidine, soit un agoniste du récepteur de P2Y¿2?. Elle concerne également des formulations pharmaceutiques contenant ces composés et leurs méthodes d'utilisation afin d'hydrater des muqueuses telles que celles des voies aériennes.

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