Amides, useful in the inhibition of il-8-induced chemotaxis...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 233/51 (2006.01) A61K 31/165 (2006.01) A61K 31/395 (2006.01) C07C 233/11 (2006.01) C07C 233/22 (2006.01) C07C 233/52 (2006.01) C07C 235/34 (2006.01) C07C 235/78 (2006.01) C07C 237/20 (2006.01) C07C 271/64 (2006.01) C07D 213/75 (2006.01) C07D 239/42 (2006.01) C07D 241/20 (2006.01) C07K 5/06 (2006.01) C07K 5/062 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2396937

N-(2-aryl-propionyl)-amides of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of N-(2-aryl-propionyl)amides of formula (I) for use in the inhibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.

L'invention concerne des N-(2-aryl-propionyl)-amides représentés par la formule (I). L'invention concerne également leur procédé de préparation et leurs préparations pharmaceutiques. Les amides de l'invention sont utilisés dans la prévention et le traitement des lésions tissulaires dues au recrutement exacerbé de neutrophiles polymorphonucléaires (leucocytes PMN) sur les sites inflammatoires. L'invention concerne, en particulier, les énantiomères R des N-(2-aryl-propionyl)amides représentés par la formule (I), utilisés dans l'inhibition de la chimiotaxie des neutrophiles associée à l'IL-8. Les composés de l'invention sont utilisés dans le traitement du psoriasis, de la rectocolite hémorragique, de la glomérulonéphrite, de l'insuffisance respiratoire aiguë, de la fibrose idiopathique, et de la polyarthrite rhumatoïde.

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