C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 233/00 (2006.01) A61K 31/185 (2006.01) A61P 11/00 (2006.01) C07D 211/14 (2006.01) C07D 213/74 (2006.01)
Patent
CA 2592608
Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of lnterleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo- oxygenase inhibition activity and are particularly useful in the treatment of neutrophil- dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
L'invention porte sur des métabolites de 2-(R)-4-isobutylarylpropionamides et sur des préparations pharmaceutiques les contenant. Lesdits composés, qui s'avèrent inhiber l'activation chimiotactique des neutrophiles (leucocytes PMN) induite par l'interaction de l'interleukine-8 (IL-8) avec les récepteurs membranaires CXCR1 et CXCR2, peuvent servir à prévenir et traiter des pathologies dues à ladite activation. Ces métabolites, qui n'affectent pas l'inhibition de la cyclooxygénase, se montrent particulièrement utiles dans le traitement de pathologies dépendant des neutrophiles, telles que le psoriasis, la colite ulcérative, les mélanomes, la BPCO, la pemphigoïde bulleuse, l'arthrite rhumatoïde, la fibrose idiopathique, la glomérulonéphrite, et pour prévenir et traiter les dommages dus à l'ischémie et à la reperfusion.
Allegretti Marcello
Bertini Riccardo
Bizzarri Cinzia
Colotta Francesco
Mosca Marco
Dompe Pha.r.ma. S.p.a.
Kirby Eades Gale Baker
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