DERIVATIVES OF THIAZOLOQUINOLINE, THEIR RACEMATES OR SEPARATE ENANTIOMERS AND PHARMACEUTICALLY ACCEPTABLE HYDRATES OR SALTS AND PHARMACEUTICAL COMPOSITION SHOWING ANTIBACTERIAL ACTIVITY Russian patent published in 1999 - IPC

Abstract RU 2138505 C1

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of thiazoloquinoline of the general formula (I) where R1 - 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; X - direct or branched alkyl with 1-3 carbon atoms or cyclopropyl; Z a residue of formulas (a) , (b) , (c) where R4 means hydrogen atom, hydroxyl, a residue of the formula -NR7R8, hydroxymethyl, a residue of the formula -CH2-NR7R8, carboxyl, methoxycarbonyl or ethoxycarbonyl being R7 means hydrogen atom, alkyl with 1-3 carbon atoms unsubstituted or substituted with hydroxyl, alkoxycarbonyl with 1-4 carbon atoms at an alkoxyl moiety or acyl with 1-3 carbon atoms; R8 means hydrogen atom or methyl; R5 means hydrogen atom, direct or branched alkyl with 1-3 carbon atoms or cyclopropyl; R6 means hydrogen atom or methyl; R3 means hydrogen atom or methyl; R2 means hydrogen atom, methyl or a residue of formulas -CH= CH--COOR2-CH2-CH2-COOR2,-CH2-CO-CH3,-CH2-CH2-CN where R2 means methyl or ethyl; B means -CH2-, oxygen atom or direct bond. Compounds can be in the form of their racemates or separate enantiomers and as their pharmaceutically acceptable hydrates and salts. They can be used as an active component in the pharmaceutical composition showing an antibacterial activity. Invention describes pharmaceutical compositions based on compounds of the formula (I) also. EFFECT: valuable pharmacological property of compounds. 4 cl, 1 tbl, 10 ex

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RU 2 138 505 C1

Authors

Tomas Jehch

Verner Khallenbakh

Tomas Khimmler

Burkkhard Mil'Ke

Klaus-Diter Bremm

Rajner Ehndermann

Frants Pirro

Mikhaehl' Shtegemann

Khejnts-Georg Vettsshtejn

Dates

1999-09-27Published

1995-05-26Filed