(R)-4-(heteroaryl) phenylethyl derivatives and pharmaceutical compositions containing them
AssigneeDompe S.p.A.
InventorsAlessio Moriconi, Andrea Aramini
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Abstract
The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. 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 autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
Claims10
(R)-4-(heteroaryl)phenylpropionic compounds of formula (I):
- and pharmaceutically acceptable salts thereof, wherein
- X is a heteroatom selected from
- S, O and N
- Y is H or a residue selected from the group consisting of:
- halogen, linear or branched C1-C4-alkyl, C2-C4-alkenyl, C1-C4-alkoxy, hydroxy, —COOH, C1-C4-acyloxy, phenoxy, cyano, nitro, —NR2, C1-C4-acylamino, halo-C1-C3-alkyl, benzoyl, linear or branched C1-C8-alkanesulfonate, linear or branched C1-C8-alkanesulfonamides, linear or branched C1-C8-alkyl sulfonylmethyl;
- Z is an heteroaryl ring selected from the group consisting of:
- unsubstituted tetrazole and
- triazole, pyrazole, oxazole, thiazole, isooxazole, isothiazole, thiadiazole and oxadiazole substituted by one hydroxy group and optionally further substituted by one or more goups selected from the group consisting of halogen, linear or branched C1-C4-alkyl, C2-C4-alkenyl, C1-C4-alkylamino, C1-C4-alkoxy, C1-C4-alkylthio, C1-C4-acyloxy, cyano, nitro, NH2, C1-C4-acylamino, halo-C1-C3-alkyl, halo-C1-C3-alkoxy, linear or branched C1-C8-alkanesulfonate and linear or branched C1-C8-alkanesulfonamides.
Dependencies are inferred from the claim text.