发明名称 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
摘要 FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of pyridobenzoxadiazine carboxylic acid of the general formula (I) <EMI ID=0.572 HE=36 WI=36 TI=CHI> where R - hydrogen atom, alkyl with 1-4 carbon atoms unsubstituted or substituted with hydroxyl or halogen atom; R is independent of R and means hydrogen atom or methyl; R - hydrogen atom or alkyl with 1-4 carbon atoms; 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 - hydrogen or halogen atom; Z - residues of formulas (a) <EMI ID=0.573 HE=27 WI=27 TI=CHI>, (b) <EMI ID=0.574 HE=27 WI=30 TI=CHI>, (c) <EMI ID=0.575 HE=27 WI=27 TI=CHI> where R - hydrogen atom, methyl or residues of formulas -CH=CH-CO<SB>2</SB>R<SP>5</SP>,-CH<SB>2</SB>-CH<SB>2</SB>CO<SB>2</SB>R -CN where <EMI ID=0.576 HE=9 WI=45 TI=CHI> means methyl or ethyl; R - hydrogen atom or methyl; R - hydrogen atom, hydroxyl, hydroxymethyl, carboxyl, methoxycarbonyl, ethoxycarbonyl, groups NR<SP>10</SP>R<SP>11</SP>,-CH<SB>2</SB>-NR<SP>10</SP>R where R 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; R - hydrogen atom or methyl; R - hydrogen atom , direct or branched alkyl with 1-3 carbon atoms or cyclopropyl; R - hydrogen atom or methyl; B - the group -CH<SB>2</SB>-, 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
申请公布号 RU2138504(C1) 申请公布日期 1999.09.27
申请号 RU19950107150 申请日期 1995.05.10
申请人 BAJER AG 发明人 TOMAS JEHTSH;BURKKHARD MIL'KE;UVE PETERZEN;TOMAS SHENKE;KLAUS-DITER BREMM;RAJNER EHNDERMANN;KARL-GEORG METTSGER;MARTIN SHEER;MIKHAEHL' SHTEGEMANN;KHAJNTS-GEORG VETTSSHTAJN
分类号 A61K9/00;A61K31/535;A61K31/5395;A61P31/04;C07D498/06;(IPC1-7):C07D498/06 主分类号 A61K9/00
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