,;where R1 is a hydrogen atom or hydroxyl group, R2 is a hydrogen atom or amino group, R3 is a hydrogen atom, halogen atom, hydroxyl group or amino group, R4 is a hydrogen atom, halogen atom or amino group, where R1 and R4 can form a double bound together, R5 is a hydrogen atom or hydroxyl group, R6 is a hydrogen atom, hydroxyl group or amino group, R7 is a hydrogen atom or hydroxyl group, R8 is a hydrogen atom, hydroxyl group or amino group, R9 and R10, each independently, is a hydrogen atom, C1-6alkyl group, amino-C1-6alkyl group, guanidine-C1-6alkyl group, amino-C3-7cycloalkyl group, amino-C3-7cycloalkyl-C1-6alkyl group, amidine group, azetidine group optionally substituted with C1-6alkyl group, glycyl group, sarcozil group, L-alanyl group, D-alanyl group, L-seryl group, D-seryl group, β-alanyl group, L-isoseryl group or D-isoseryl group, and R11 is a hydrogen atom, hydroxyl group or fluorine atom, excluding cases, when (ii) R5, R8, and R11 are hydroxyl groups, R1, R2, R3, R4, R6, R7, R9, and R10 are hydrogen atoms, (iii) R1, R5, R8, and R11 are hydroxyl groups, R2, R3, R4, R6, R7, R9, and R10 are hydrogen atoms, (a) R1 and R4 form a double bound together, R5, R8, and R11 are hydroxyl groups, and R2, R3, R6, R7, R9, and R10 are hydrogen atoms, (b) R1 and R4 form a double bound together, R8 and R11 are hydroxyl groups, and R2, R3, R5, R6, R7, R9, and R10 are hydrogen atoms, (c) R1, R2, R3, R4, R5, R6, R7, R9, and R10 are hydrogen atoms, and R8 and R11 are hydroxyl groups.;EFFECT: obtaining new effective aminoglycoside antibiotic against multidrug-resistant bacteria.;14 cl, 6 tbl, 86 ex"/> NEW EFFECTIVE AMINOGLYCOSIDE ANTIBIOTIC AGAINST MULTIDRUG-RESISTANT BACTERIA
首页> 外国专利> NEW EFFECTIVE AMINOGLYCOSIDE ANTIBIOTIC AGAINST MULTIDRUG-RESISTANT BACTERIA

NEW EFFECTIVE AMINOGLYCOSIDE ANTIBIOTIC AGAINST MULTIDRUG-RESISTANT BACTERIA

机译:针对多药抗性细菌的新有效氨基糖苷类抗生素

摘要

FIELD: pharmaceutics.;SUBSTANCE: present invention relates to a compound represented by the general formula (I), or to its pharmaceutically accepted salt that have antibacterial activity, to a pharmaceutical composition based on them, an antibacterial agent, to use of the claimed compounds and method for preventing or treating bacterial infectious disease. ; ,;where R1 is a hydrogen atom or hydroxyl group, R2 is a hydrogen atom or amino group, R3 is a hydrogen atom, halogen atom, hydroxyl group or amino group, R4 is a hydrogen atom, halogen atom or amino group, where R1 and R4 can form a double bound together, R5 is a hydrogen atom or hydroxyl group, R6 is a hydrogen atom, hydroxyl group or amino group, R7 is a hydrogen atom or hydroxyl group, R8 is a hydrogen atom, hydroxyl group or amino group, R9 and R10, each independently, is a hydrogen atom, C1-6alkyl group, amino-C1-6alkyl group, guanidine-C1-6alkyl group, amino-C3-7cycloalkyl group, amino-C3-7cycloalkyl-C1-6alkyl group, amidine group, azetidine group optionally substituted with C1-6alkyl group, glycyl group, sarcozil group, L-alanyl group, D-alanyl group, L-seryl group, D-seryl group, β-alanyl group, L-isoseryl group or D-isoseryl group, and R11 is a hydrogen atom, hydroxyl group or fluorine atom, excluding cases, when (ii) R5, R8, and R11 are hydroxyl groups, R1, R2, R3, R4, R6, R7, R9, and R10 are hydrogen atoms, (iii) R1, R5, R8, and R11 are hydroxyl groups, R2, R3, R4, R6, R7, R9, and R10 are hydrogen atoms, (a) R1 and R4 form a double bound together, R5, R8, and R11 are hydroxyl groups, and R2, R3, R6, R7, R9, and R10 are hydrogen atoms, (b) R1 and R4 form a double bound together, R8 and R11 are hydroxyl groups, and R2, R3, R5, R6, R7, R9, and R10 are hydrogen atoms, (c) R1, R2, R3, R4, R5, R6, R7, R9, and R10 are hydrogen atoms, and R8 and R11 are hydroxyl groups.;EFFECT: obtaining new effective aminoglycoside antibiotic against multidrug-resistant bacteria.;14 cl, 6 tbl, 86 ex
机译:领域:药剂。物质:本发明涉及通式(I)代表的化合物,或其具有抗菌活性的药学上接受的盐,其基于它们的药物组合物,抗菌剂使用所要求保护的用于预防或治疗细菌传染病的化合物和方法。 ; <图像文件=“00000122.jpg”他=“35”ImgContent =“未定义”ImgFormat =“JPEG”Wi =“107”/>,其中R 1 是氢原子或羟基,R 2 是氢原子或氨基,R 3 是氢原子,卤素原子,羟基或氨基,R 4 是氢原子,卤素原子或氨基,其中R 1 和r 4℃可以形成双束缚,R 5 是氢气原子或羟基,R 6 是氢原子,羟基或氨基,R 7 是氢原子或羟基,R 8 是氢原子,羟基或氨基,R 9 和R 10 ,每个单独地是氢原子,c 1-6 烷基,氨基-C <亚> 1-6 烷基,胍-C <亚烷基>烷基,氨基-c <亚烷基,氨基-C 环烷基组,氨基-C 3-7 环烷基-c 1-6烷基烷基,脒基,吖啶基,任选地被C 1-6 烷基,甘糖基,甲硅基,L-丙基,D-丙基,L-甲基,D-甲基,β-丙酰基,L-异苷基团或D- Isoseryl组,以及R 11 是氢原子,羟基或氟原子,排除案例,当(ii)r 5℃时,R 8℃>和R 11 是羟基,R 1 ,R 2℃,r 3 ,R 4 ,R 6 < / sup>,R 7 ,R 9 ,和R 10 是氢原子,(iii)r 1 ,R 5 ,R 8 和r 11 是羟基,R 2 ,R 3 ,R 4 ,R 6 ,R 7 ,R 9 ,以及R 10 是氢原子,(a)r 1 和R 4 形成双绑定在一起,R 5 ,R 8 和R 11 是羟基,R 2 ,R 3 ,R 6 ,R 7 ,R 9 和r 10 是氢原子,(b)r 1 和r 4 形成双绑定在一起, R 8 和R 11 是羟基,R 2 ,R 3 ,R 5 < / sup>,R 6 ,R 7 ,r 9 ,以及R 10 是氢原子,(c )R 1 ,R 2 ,R 3 ,R 4 ,R 5 ,R 6 ,r 7 ,R 9 和R 10 是氢原子,R 8 和R 11 是羟基。;效果:获得对多药抗性细菌的新有效氨基糖苷类抗生素。; 14 cl,6 tbl,86前

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