NEW EFFECTIVE AMINOGLYCOSIDE ANTIBIOTIC AGAINST MULTIDRUG-RESISTANT BACTERIA Russian patent published in 2021 - IPC C07H15/12 C07H15/234 A61K31/7036 A61P31/04 

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.

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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, C_1-6alkyl group, amino-C_1-6alkyl group, guanidine-C_1-6alkyl group, amino-C_3-7cycloalkyl group, amino-C_3-7cycloalkyl-C_1-6alkyl group, amidine group, azetidine group optionally substituted with C_1-6alkyl 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