C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 309/65 (2006.01) A61K 31/165 (2006.01) A61K 31/18 (2006.01) A61P 9/10 (2006.01) C07C 233/76 (2006.01) C07C 311/03 (2006.01) C07C 311/21 (2006.01) C07D 213/70 (2006.01) C07D 213/76 (2006.01) C07D 277/42 (2006.01) C07D 295/10 (2006.01) C07D 295/14 (2006.01) C07D 307/52 (2006.01) C07D 307/68 (2006.01) C07D 333/34 (2006.01)
Patent
CA 2629935
The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
La présente invention concerne des dérivés (R)-arylalkylaminés sélectionnés. Ces composés présentent un effet inhibiteur puissant surprenant sur la chimiotaxie des PMN humains induite par le C5a. Les composés de l'invention n'ont absolument aucune activité d'inhibition de la CXCL8. Lesdits composés sont utiles dans le traitement de pathologies dépendantes de l'activation chimiotactique de neutrophiles et de monocytes induite par la fraction C5a du complément. En particulier, les composés de l'invention sont utiles dans le traitement de la sepsie, du psoriasis, de la polyarthrite rhumatoïde, de la recto-colite hémorragique, du syndrome de détresse respiratoire aiguë, d'une fibrose idiopathique, de la glomérulonéphrite et dans la prévention et le traitement de plaies provoquées par l'ischémie et la reperfusion.
Allegretti Marcello
Aramini Andrea
Beccari Andrea
Bertini Riccardo
Cesta Maria Candida
Allegretti Marcello
Aramini Andrea
Beccari Andrea
Bertini Riccardo
Cesta Maria Candida
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