A method of identifying cftr-binding compounds useful for...

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) A61K 31/52 (2006.01) A61K 38/17 (2006.01) C07D 473/06 (2006.01) C07K 14/47 (2006.01)

Patent

CA 2205540

The present invention provides a method of identifying CFTR-binding compounds for treating cells having a reduced apical Cl- conductance, such as cystic fibrosis cells. This identification method involves the use of polypeptide I.alpha., which constitutes a portion of the CFTR protein. The present invention also provides a method of treating CF cells by contacting cells having a reduced apical C1- conductance with a therapeutically effective quantity of a compound selected by the present inventive identification method. Preferred compounds for such treatment have little or no affinity for adenosine cell receptors. The present invention provides novel compounds useful in practicing the present inventive method, as well as pharmaceutical compositions containing such compounds.

Technique d'identification des composés liant le régulataire transmembranaire de la mucoviscidose (CFTR) afin de traiter les cellules ayant une conductance apicale réduite des ions Cl?-¿, par exemple les cellules atteintes de mucoviscidose. Cette technique implique l'utilisation du polypeptide I.alpha., qui constitue une partie de la protéine (CFTR). Est également présentée une technique de traitement des cellules atteintes de mucoviscidose consistant à mettre les cellules ayant une conductance apicale réduite des ions Cl?-¿ en contact avec une quantité efficace sur le plan thérapeutique d'un composé choisi au moyen de cette technique d'identification. Les composés privilégiés dans un tel traitement ont peu ou pas d'affinité pour les récepteurs des cellules d'adénosine. Sont présentés de nouveaux composés utiles pour l'application de cette technique, ainsi que des produits pharmaceutiques contenant ces composés.

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