Cyclic peptides as g-protein-coupled receptor antagonists

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/56 (2006.01) A61K 38/08 (2006.01) A61K 38/12 (2006.01) A61P 9/10 (2006.01) A61P 11/00 (2006.01) A61P 17/00 (2006.01) A61P 37/00 (2006.01) C07K 14/47 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2463675

The invention relates to novel cyclic compounds which have the ability to modulate the activity of G protein-coupled receptors. The compounds preferably act as antagonists. In preferred embodiments, the invention provides cyclic peptidic and peptidomimetic antagonists of C5a receptors, which are active against C5a receptors on polymorphonuclear leukocytes and macrophages. The compounds of the invention are both potent and selective, and are useful in the treatment of a variety of inflammatory conditions.

Cette invention a trait à de nouveaux composés cycliques en mesure de moduler l'activité de récepteurs couplés à la protéine G. Ces composés se comportent, de préférence, en tant qu'antagonistes dudit récepteur. Dans des réalisations préférées, il est traité d'antagonistes peptidiques cycliques et peptidomimétiques des récepteurs de C5a, se montrant actifs à l'encontre des récepteurs de C5a sur des leucocytes polymorphonucléaires et des macrophages. Ces composés, qui sont à la fois puissants et sélectifs, se révèlent des plus utiles pour traiter divers états inflammatoires.

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