发明名称 DERIVATIVES OF THIAZOLOQUINOLINE, THEIR RACEMATES OR SEPARATE ENANTIOMERS AND PHARMACEUTICALLY ACCEPTABLE HYDRATES OR SALTS AND PHARMACEUTICAL COMPOSITION SHOWING ANTIBACTERIAL ACTIVITY
摘要 FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of thiazoloquinoline of the general formula (I) <EMI ID=0.577 HE=36 WI=36 TI=CHI> where R - 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) <EMI ID=0.578 HE=27 WI=27 TI=CHI>, (b) <EMI ID=0.579 HE=27 WI=27 TI=CHI>, (c) <EMI ID=0.580 HE=27 WI=27 TI=CHI> where R means hydrogen atom, hydroxyl, a residue of the formula -NR<SP>7</SP>R , hydroxymethyl, a residue of the formula -CH<SB>2</SB>-NR<SP>7</SP>R , carboxyl, methoxycarbonyl or ethoxycarbonyl being R 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; R means hydrogen atom or methyl; R means hydrogen atom, direct or branched alkyl with 1-3 carbon atoms or cyclopropyl; R means hydrogen atom or methyl; R means hydrogen atom or methyl; R means hydrogen atom, methyl or a residue of formulas -CH= CH--COOR<SP>2</SP>-CH<SB>2</SB>-CH<SB>2</SB>-COOR<SP>2</SP>,-CH<SB>2</SB>-CO-CH<SB>3</SB>,-CH<SB>2</SB>-CH<SB>2</SB>-CN where R means methyl or ethyl; B means -CH<SB>2</SB>-, 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
申请公布号 RU2138505(C1) 申请公布日期 1999.09.27
申请号 RU19950108319 申请日期 1995.05.26
申请人 BAJER AG 发明人 TOMAS JEHCH;VERNER KHALLENBAKH;TOMAS KHIMMLER;BURKKHARD MIL'KE;KLAUS-DITER BREMM;RAJNER EHNDERMANN;FRANTS PIRRO;MIKHAEHL' SHTEGEMANN;KHEJNTS-GEORG VETTSSHTEJN
分类号 A61K31/4738;A61K31/495;A61P31/04;C07D513/16;(IPC1-7):C07D513/16;A61K31/50 主分类号 A61K31/4738
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