发明名称 OMEGA-AMINOALKYLAMIDES OF R-2-ARYL-PROPIONIC ACIDS AS INHIBITORS OF THE CHEMOTAXIS OF POLYMORPHONUCLEATE AND MONONUCLEATE CELLS
摘要 (R) -2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (Leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomer s of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of he chemataxis of neutrophils and monocites induced by t he C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Select ed compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of nutrophils and monocytes and the IL-8-induced chemotaxis of PM N leukocytes. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, rheumatoid arthritis and in the preventi on and the treatment of injury caused by ischemia and reperfusion.
申请公布号 CA2435687(A1) 申请公布日期 2002.09.06
申请号 CA20022435687 申请日期 2002.02.25
申请人 DOMPE S.P.A. 发明人 CESTA, MARIA CANDIDA;BERDINI, VALERIO;BIZZARRI, CINZIA;DI CIOCCIO, VITO;COLOTTA, FRANCESCO;CASELLI, GIANFRANCO;ALLEGRETTI, MARCELLO;GANDOLFI, CARMELO;BERTINI, RICCARDO
分类号 C07D295/12;A61K31/165;A61K31/198;A61K31/439;A61K31/445;A61K31/4453;A61K31/5375;A61K31/5377;A61P1/04;A61P9/10;A61P11/00;A61P13/12;A61P17/02;A61P17/06;A61P19/02;A61P19/04;A61P29/00;A61P37/06;A61P43/00;C07C231/02;C07C231/16;C07C233/40;C07C233/44;C07C233/51;C07C235/34;C07C235/70;C07C237/22;C07C279/12;C07C281/16;C07D211/58;C07D233/24;C07D233/46;C07D295/13;C07D295/14;C07D451/04 主分类号 C07D295/12
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