ALLEGRETTI, MARCELLO,BERTINI, RICCARDO,BIZZARRI, CINZIA,CESTA, MARIA CANDIDA,COLOTTA, FRANCESCO
申请号：
ES09174797
公开号：
ES2393589T3
申请日:
2002.11.19
申请国别(地区):
ES
年份:
2012
代理人:
摘要：
(R,S)-2-Aryl-propionic acids are useful as inhibitors of interleukin-8 induced human polymorphonucleated neutrophils (PMN) chemotaxis. (R,S)-2-Aryl-propionic acids of formula (I), their single (R) and (S) enantiomers or salts are useful as inhibitors of interleukin-8 (IL-8) induced human polymorphonucleated neutrophils (PMN) chemotaxis. [Image] Ar : phenyl ring (substituted by T in meta position, T1 in para position or T2 in ortho position) T : linear or branched 1-5C alkyl, 2-5C alkenyl, or 2-5C alkynyl (optionally substituted by 1-5C alkoxycarbonyl, optionally substituted phenyl, linear or branched 1-5C hydroxyalkyl or arylhydroxymethyl) T1benzoyloxy, benzoylamino, benzenesulfonyloxy, benzenesulfonylamino, benzenesulfonylmethyl (all optionally substituted), 1-5C acyloxy, 1-5C acylamino, 1-5C sulfonyloxy, 1-5C alkanesulfonylamino, 1-5C alkanesulfonylmethyl, 3-6C cycloalkyl, 2-furyl, 3-tetrahydrofuryl, 2- thiophenyl, 2-tetrahydrothiophenyl or ((1-8C)-alkanoyl, -cycloalkanoyl or -arylalkanoyl)-1-5C-alkylamino (preferably acetyl-N-methyl-amino or pivaloyl-N-ethyl-amino) and T2arylmethyl, aryloxy or acylamino (all optionally substituted by 1-4C alkyl, 1-4C-alkoxy, chlorine, fluorine or trifluoromethyl). The meta linear or branched 1-5C alkyl together with a substituent in ortho or para position and the benzene ring forms optionally saturated or optionally substituted bicyclo aryls. INDEPENDENT CLAIM are included for the following: (1) preparation of (I) and (2) use of (I) in the preparation of a medicament for the treatment of e.g. psoriasis, ulcerative colitis, melanoma and chronic obstructive pulmonary disease (COPD). - ACTIVITY : Antipsoriatic Antiulcer Respiratory-Gen. Antirheumatic Antiarthritic Nephrotropic Vasotropic Antiinflammatory Gastrointestinal-Gen. Cytostatic. - MECHANISM OF ACTION : Interleukin-8 (IL-8) inhibitor GROalpha inhibitor CXCR2 agonist/antagonist. The ability of (R,S) 2-[(3-isopropyl)phenyl]propionic acid (A) to inhibit IL-8 induced chemotaxis
