DERIVATIVES OF PYRIDOBENZOXADIAZINE CARBOXYLIC ACID, MIXTURE OF THEIR ISOMERS OR SEPARATE ISOMERS, THEIR PHARMACEUTICALLY USED HYDRATES AND SALTS AND PHARMACEUTICAL COMPOSITION SHOWING ANTIBACTERIAL ACTIVITY ON THEREOF Russian patent published in 1999 - IPC

Abstract RU 2138504 C1

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of pyridobenzoxadiazine carboxylic acid of the general formula (I) where R1 - hydrogen atom, alkyl with 1-4 carbon atoms unsubstituted or substituted with hydroxyl or halogen atom; R2 is independent of R1 and means hydrogen atom or methyl; R3 - hydrogen atom or alkyl with 1-4 carbon atoms; R4 - hydrogen atom, alkyl with 1-4 carbon atoms unsubstituted or substituted with hydroxyl, methoxyl, amino-, methylamino- or dimethylamino-group or (5-methyl-2-oxo-1,3-dioxol-4-yl)- -methyl; X1 - hydrogen or halogen atom; Z - residues of formulas (a) , (b) , (c) where R5 - hydrogen atom, methyl or residues of formulas -CH=CH-CO2R5,-CH2-CH2CO2R5-CN where R5′-CH2-CO-CH3-CH2-CH2 means methyl or ethyl; R6 - hydrogen atom or methyl; R7 - hydrogen atom, hydroxyl, hydroxymethyl, carboxyl, methoxycarbonyl, ethoxycarbonyl, groups NR10R11,-CH2-NR10R11 where R10 means hydrogen atom, alkyl with 1-3 carbon atoms, alkoxycarbonyl with 1-4 carbon atoms at an alkoxyl moiety, acyl with 1-3 carbon atoms unsubstituted or substituted with hydroxyl; R11 - hydrogen atom or methyl; R8 - hydrogen atom , direct or branched alkyl with 1-3 carbon atoms or cyclopropyl; R9 - hydrogen atom or methyl; B - the group -CH2-, oxygen atom or direct bond, a mixture of their isomers or separate isomers, their pharmaceutically used hydrates and salts that can be an active component of the pharmaceutical composition showing an antibacterial activity. Invention describes pharmaceutical compositions based on compounds of the formula (I) also. EFFECT: valuable pharmacological property of compositions. 4 cl, 35 ex

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RU 2 138 504 C1

Authors

Tomas Jehtsh

Burkkhard Mil'Ke

Uve Peterzen

Tomas Shenke

Klaus-Diter Bremm

Rajner Ehndermann

Karl-Georg Mettsger

Martin Sheer

Mikhaehl' Shtegemann

Khajnts-Georg Vettsshtajn

Dates

1999-09-27Published

1995-05-10Filed