| 摘要 |
FIELD: medicine. SUBSTANCE: claimed invention describes 1-(2- fluorocyclopropyl)chinolon- and naphthyridoncarboxylic acid derivatives of general formula (I):wherein Ris hydrogen, alkyl having 1-3 carbon atoms which may be substituted by hydroxy group; alkoxycarbonyl having-1-4 carbon atoms, acetyl which may be substituted by halogen, or (5-methyl-2-oxo-1,3-dioxol-4-yl) methyl; Ris hydrogen, alkyl having 1-3 carbon atoms which may be substituted by hydroxy, methoxy, amino, methylamino or dimethylamino group, (5-methyl-2-oxo-1,3-dioxol-4-yl) methyl, acetoxymethyl or pyvaloyloxymethyl; n is 0 or 1; Xis halogen or nitro group, Xis hydrogen, halogen, amino group or methyl; A is N, C-H, C-F, C-Cl, P-Br, C-CF, C-OCH, C-OCHF, C-CHor C-C=CH, or isomeric mixtures or individual isomers thereof and pharmaceutically acceptable hydrates and salts thereof. The claimed invention also describes pharmaceutical composition having antibiotic activity and containing of least one pharmaceutically acceptable carrier and one active agent based on chinolon- and naphthyrydon-carboxylic acid derivatives. The active agent is at least one compound of general formula (I):wherein Ris hydrogen, alkyl having 1-3 carbon atoms which may be substituted by hydroxy group; alkoxycarbonyl having 1-4 carbon atoms, acetyl which may be substituted by halogen or (5-methyl- 2-oxo-1,3-dioxol-4-yl) methyl; Ris hydrogen alkyl having 1-3 carbon atoms which may be substituted by hydroxy, methoxy, amino, methylamino or dimethylamino group, (5-methyl-2-oxo-1,3-dioxol-4-yl) methyl, acetoxymethyl or pyraloyloxymethyl, n or 1; Xis halogen or nitro group, Xis hydrogen, halogen, amino group or methyl A is N, C-H, C-F, C-Cl, C-Br, C-CF, C-OCH, C-OCHF, C-CHor C-C=CH, mixture of isomers thereof or individual isomers or pharmaceutically acceptable hydrate or salt thereof in effective amount. EFFECT: improved properties of the pharmaceutical composition. |
