Amides of r-2-(aminoaryl)-propionic acids for use in the...

C - Chemistry – Metallurgy – 07 – D

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C07D 295/155 (2006.01) A61K 31/47 (2006.01) A61P 17/06 (2006.01) C07D 207/20 (2006.01) C07D 209/18 (2006.01) C07D 213/75 (2006.01) C07D 215/12 (2006.01) C07D 215/38 (2006.01) C07D 239/42 (2006.01) C07D 241/20 (2006.01) C07D 277/46 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2420585

N-(2-aminoaryl-propionyl)-amides of formula (1) 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 2-(aminoaryl)-propionyl amides of formula (1) 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 porte sur des N-(2-aminoaryl-propionyl)-amides de formule (1), leur procédé d'obtention et des préparations pharmaceutiques les utilisant. Lesdits amides servent à la prévention et au traitement de lésions tissulaires dues à l'accumulation exacerbée de neutrophiles polymorphonucléaires (leucocytes PMN) dans les sites inflammatoires. L'invention porte en particulier sur les énantiomères R des 2-/aminoaryl)-propionyl amides de formule (1) inhibant la chimiotaxie des neutrophiles induite par l'IL-8. Lesdits composés servent au traitement du psoriasis, de la colite ulcéreuse, de la néphrite glomérulaire, de l'insuffisance respiratoire aiguë, de la fibrose idiopathique et de l'arthrite rhumatoïde.

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