发明名称 6,7-DIHYDRO-5H-PYRAZOLO[1,2-a]PYRAZOLE-1-ONES (VARIANTS) INHIBITING RELEASE OF INFLAMMATORY CYTOKINES, PHARMACEUTICAL COMPOSITION AND INHIBITION METHOD
摘要 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)jNR9aR9b; (e) -(CH2)OCO2R10; (g) -(CH2)jOCON(R10)2 wherein each radical R8, R9a, R9b and R10 represents independently hydrogen atom, (C1-C4)-alkyl; or R9a and R9b 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
申请公布号 RU2299885(C2) 申请公布日期 2007.05.27
申请号 RU20040111803 申请日期 2002.09.20
申请人 DZE PROKTER EHND GEHMBL KOMPANI 发明人 KLARK MAJKL FILLIP;LOFERSVEJLER MEHTT'JU DZHON;DZUNG DZHEJN FAR-DZHAJN;NEHTCHAS MAJKL DZHORDZH;DE BISVANAT
分类号 C07D487/04;A61K31/407;A61K31/506;A61K31/5377;A61K31/5517;A61P1/04;A61P7/00;A61P9/00;A61P11/00;A61P19/02;A61P29/00;A61P31/04;A61P43/00;C07D491/113;C07D491/20;C07D495/20 主分类号 C07D487/04
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