QUINOLONE DERIVATIVES OR ITS PHARMACEUTICALLY ACCEPTABLE SALT Russian patent published in 2012 - IPC C07D215/22 C07D215/56 C07D401/04 C07D401/12 C07D401/14 C07D405/04 C07D405/12 C07D405/14 C07D409/12 C07D409/14 C07D407/04 C07D407/12 C07D407/14 A61K31/4709 A61K31/519 A61K31/5377 A61K31/662 A61K31/683 A61K31/695 A61P7/02 A61P9/00 A61P9/04 A61P9/10 A61P43/00 

FIELD: chemistry.

SUBSTANCE: present invention is related to new quinolone derivatives of general formula (I) where R¹: C_3-6cycloalkyl or lower alkylene C_3-6cycloalkyl, R²: -H or halogen, R³: -H, halogen, -OR⁰ or -O-(lower alkylene)-phenyl, R⁰: are the same or different from each other, and each represents -H or lower alkyl, R⁴: lower alkyl, halogen(lower alkyl), lower alkyleneC_3-6cycloalkyl, C_3-7cycloalkyl or a heterocyclic group, where cycloalkyl and the heterocyclic group specified in R⁴ can be respectively substituted, R⁵: -NO₂, -CN, -L-R^a, -C(O)R⁰, -O-R^b, -N(R⁶)₂, lower alkylene-N(R⁶)(R^c), -N(R⁶)C(O)-R^d, lower alkylene-N(R⁶)C(O)-R^d, lower alkylene-N(R⁰)C(O)O-(lower alkyl), -N(R⁰)C(O)N(R⁰)-R^e, lower alkylene-N(R⁰)C(O)N(R⁰)-R^e, -N(R⁰)S(O)₂N(R⁰)C(O)-R^d, -CH=NOH, C₃-₆cycloalkyl, (2,4-dioxo-1,3-thiazolidin-5-yliden)methyl or (4-oxo-2-tioxo-1,3-thiazolidin-5-yliden)methyl where cycloalkyl specified in R⁵ can be respectively substituted, R⁶: H, lower alkyl, lower alkylene-CO₂R⁰ or lower alkylene-P(O)((OP^p)₂, where lower alkylene specified in R⁶ can be substituted, L: lower alkylene or lower alkenylene which can be respectively substituted, R^a: -OR⁰, -O-(lower alkylene)-phenyl, -O-(lower alkylene)-CO₂R⁰, -CO₂R⁰, -C(O)NHOH, -C(O)N(R⁶)₂, -C(O)N(R⁰)-S(O)₂-(lower alkyl), -C(O)N(R⁰)-S(O)₂-phenyl, -C(O)N(R⁰)-S(O)₂-(heterocyclic group), -NH₂OH, -OC(O)R⁰, -OC(O)-(halogen(lower alkyl)), -P(O)(OR^p)₂, phenyl or the heterocyclic group where phenyl or the heterocyclic group specified in R^a can be substituted, R^p: R⁰, lower alkylene-OC(O)-(lower alkyl), lower alkylene-OC(O)-C_3-6cycloalkyl, lower alkylene-OC(O)O-(lower alkyl), R^b: H, lower alkylene-R^ba or lower alkenylene-R^ba where lower alkylene or lower alkenylene specified in R^b can be substituted, R^ba: -OR⁰, -CO₂R⁰, -C(O)N(R⁰)₂, -C(O)N(R⁰)-S(O)₂-(lower alkyl), -C(O)N(R⁰)-S(O)₂-[phenyl, -C(NH₂)-NOH, -C(NH₂)=NO-C(O)-(lower alkylene)-C(O)R⁰, -CO₂-(lower alkylene)-phenyl, -P(O)(OR^p)₂, -C(O)R⁰, -C(O)-phenyl, C_3-6cycloalkyl, phenyl or the heterocyclic group where phenyl and the heterocyclic group specified in R^ba can be substituted, R^c: H, lower alkylene-OR⁰, lower alkylene-CO₂R⁰, lower alkylene-P(O)((OP^p)₂, phenyl where lower alkylene and phenyl are specified in R^d can be substituted, R^d: C_1-7-alkyl, lower alkenyl, halogen(lower alkyl), lower alkylene-R^da, lower alkylenylene-R^da, C_3-6cycloalkyl, phenyl, naphthyl or the heterocyclic group, where lower alkylene, cycloalkyl, phenyl, naphthyl and the heterocyclic group specified in R^d can be substituted, R^da: -CN, -OR⁰, -O-(lower alkylene)-CO₂R⁰, -O-naphthyl, -CO₂R⁰, -CO₂-(lower alkylene)-N(R⁰)₂, -P(O)(OR^p)₂, -N(R⁶)₂, -C(O)N(R⁰)-phenyl, -C(O)N(R⁰)-(lower alkylene which can be used by -CO₂R⁰)-phenyl, -N(R⁰)C(O)-phenyl, -N(R⁰)C(O)-OR⁰, -N(R⁰)C(O)-O-(lower alkylene)-phenyl, -N(R⁰)S(O)₂-phenyl, C_3-6cycloalkyl, phenyl, naphthyl or the heterocyclic group, where phenyl, naphthyl and heterocyclic group specified in R^a can be substituted, R^e: lower alkylene-CO₂R⁰, phenyl, -S(O)₂-phenyl or -S(O)₂-(heterocyclic group), where phenyl and the heterocyclic group specified in R^e can be substituted, X: CH, A: C(R⁷), R⁷: -H, or R⁴ and R⁷ together can form lower alkylene, where the substituted groups have the substituted specified in cl.1, and provided 7-(cyclohexylamino)-1-ethyl-6-fluor-4-oxo-1,4-dohydroquinoline-3-carbonitryl is excluded. Also, the invention refers to a pharmaceutical composition based on a compound of formula (I) and application of formula (I) for preparing a thrombocyte aggregation inhibitor or a P2Y12 inhibitor.

EFFECT: there are produced new quinol-4-one derivatives showing effective biological properties.

11 cl, 83 tbl, 71 ex