APPLICATION OF CHIRAL ARYLKETONES FOR NEUTROPHIL-DEPENDENT INFLAMMATORY DISEASES Russian patent published in 2009 - IPC A61K31/12 A61K31/121 A61P29/00 

Abstract RU 2345759 C2

FIELD: medicine; pharmacology.

SUBSTANCE: compounds can be applied as medical products for treating the diseases associated with PMN chemotaxis caused with IL-8, including psoriasis, rheumatoid arthritis, and ulcerative colitis, and for treating the damages caused by ischemia and reperfusion. In formula , Ar represents phenyl optionally substituted with one to three substitutes which can be the same or differ from each other, chosen of: halogen, C1-C4-alkyl, C1-C4-alkoxy, hydroxy, C1-C4-acyloxy, phenoxy, cyano, nitro, amino, C1-C4-acylamino, halogen-C1-C3-alkyl, halogen-C1-C3-alkoxy, benzoyl; or Ar represents 4-thienoylphenyl, 4-(1-oxo-2-isoindolynil)phenyl, 3-chlorine-4-(2,5-dihydro-1H-pyrrole-1-yl)phenyl, 6-methoxy-β-naphthyl, 1-hydroxyphenyl-1-methyl; or Ar represents group of formula III where A represents benzyl, phenoxy, benzoyl, benzoyloxym, 1- hydroxyphenyl-1-methyl; B represents hydroxy, C1-C4-acyloxy or group of formula -O-C(=S)-N(CH3)2, or -S-C(=O)-N(CH3)2; Ra and Rb are independently chosen from the group including hydrogen, linear or branched C1-C6-alkyl, phenyl, α- or β-naphthyl, 2,3,4-pyridyl, C1-C4-alkylphenyl, C1-C4-alkyl (α- or β-naphthyl), C1-C4-alkyl (2,3,4-pyridyl), cyano (-CN), carboxamide, carboxyl or carboxy esters of formula CO2R" wherein R" represents residue linear or branched aliphatic C1-C6-alcohol, phosphonate PO(OR")2, where R" has specified values, or formula of group X-(CH2)n-Z, where X represents C, SO or SO2 group; Z represents hydrogen, tert-butyl, isopropyl, CO2R", CN, phenyl, α- or β-naphthyl, 2,3,4-pyridyl, C3-C6-cycloalkyl, NH-BOC, NH2; n is equal to zero or integer within 1 to 3; or Ra and Rb together with carbon atom whereto attached form cyclic residue 2,2-disubstituted 4,6-dioxo-1,3-dioxanyl of formula, II where R' represents methyl or ethyl, or two groups R' form cyclohexane or cyclopentane ring.

EFFECT: higher efficiency of treatment.

7 cl, 15 ex

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RU 2 345 759 C2

Authors

Allegretti Marchello

Bertini Rikkardo

Chesta Marija Kandida

Bitstsarri Chintsija

Kolotta Franchesko

Dates

2009-02-10Published

2003-12-09Filed