6,7-DIHYDRO-5H-PYRAZOLO[1,2-a]PYRAZOLE-1-ONES (VARIANTS) INHIBITING RELEASE OF INFLAMMATORY CYTOKINES, PHARMACEUTICAL COMPOSITION AND INHIBITION METHOD Russian patent published in 2007 - IPC C07D487/04 A61K31/407 A61P29/00 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compounds of the formula (I): possessing properties of inhibitor of inflammatory cytokines release from cells. In compound of the formula (I) R is chosen from: (a) fragment of the formula -OR³ wherein R³ is chosen from group consisting of phenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 2,6-difluorophenyl, 2-cyanophenyl, 3-cyanophenyl, 2-trifluoromethylphenyl, 4-trifluoromethylphenyl, 2-methylphenyl, 4-methylphenyl, 2,4-dimethylphenyl, 3-N-acetylaminophenyl, 2-methoxyphenyl, 4-methoxyphenyl and 3-benzo[1,3]dioxol-5-yl; (b) fragment of the formula: wherein R⁶ is chosen from group consisting of hydrogen atom, methyl, ethyl, vinyl, cyclopropyl, cyclohexyl, methoxymethyl, methoxyethyl, 1-hydroxy-1-methylethyl, carboxy-group, 4-fluorophenyl, 2-aminophenyl, 2-methylphenyl, 4-methylphenyl, 4-methoxyphenyl, 4-(propanesulfonyl)phenyl, 3-benzo[1,3]dioxol-5-yl, pyridine-2-yl, pyridine-3-yl, or (c) fragment of the formula: wherein R⁶ is chosen from group consisting of hydrogen atom, methyl, ethyl, vinyl, cyclopropyl, cyclohexyl, methoxymethyl, methoxyethyl, 1-hydroxy-1-methylethyl, carboxy-group, phenyl, 4-fluorophenyl, 2-aminophenyl, 2-methylphenyl, 4-methylphenyl, 4-methoxyphenyl, 4-(propanesulfonyl)phenyl, 3-benzo[1,3]dioxol-5-yl, pyridine-2-yl, pyridine-3-yl; each radical R² is chosen independently from group consisting of (a) hydrogen atom; (b) -(CH₂)_jO(CH₂)_nR⁸; (c) -(CH₂)_jNR^9aR^9b; (e) -(CH₂)OCO₂R¹⁰; (g) -(CH₂)_jOCON(R¹⁰)₂ wherein each radical R⁸, R^9a, R^9b and R¹⁰ represents independently hydrogen atom, (C₁-C₄)-alkyl; or R^9a and R^9b can form in common 5-6-membered heterocyclic ring comprising 1-2 heteroatoms chosen from nitrogen and/or oxygen atoms; or two radicals R¹⁰ can form in common 5-6-membered heterocyclic ring comprising 1-2 heteroatoms chosen from nitrogen and/or oxygen atoms; j represents index 0; n represents index 0. Also, invention relates to a pharmaceutical composition and a method for inhibition.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

15 cl, 2 sch, 8 tbl, 13 ex