ALLEGRETTI, MARCELLO,BERTINI, RICCARDO,BIZZARRI, CINZIA,CESTA, MARIA CANDIDA,COLOTTA, FRANCESCO
申请号：
DK09174797
公开号：
DK2229942T3
申请日:
2002.11.19
申请国别(地区):
DK
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, T 1 in para position or T 2 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)； T 1benzoyloxy, 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 T 2arylmethyl, 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 ind
