C-4" POSITION SUBSTITUTED MACROLIDE DERIVATIVE Russian patent published in 2016 - IPC C07H17/08 A61K31/7048 A61P31/04 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) and pharmaceutically acceptable salts thereof

where Me denotes a methyl group, R¹ is a hydrogen atom, C_1-6alkyl group (C_1-6alkyl group can be substituted with one substitute selected from hydroxy group, C_1-6alkoxy group, diC_1-6alkylamino group and group, presented by formula -NR⁷⁸COR⁷⁹ or formula -NR⁸⁰SO₂R⁸¹, where R⁷⁸ and R⁸⁰ represent a hydrogen atom and R⁷⁹ and R⁸¹, which can be identical or different, denote a hydrogen atom or C_1-6alkyl group) or C_1-6alkylsulphonyl group, R² represents a hydrogen atom, 4-8-member saturated heterocyclic group with one heteroatom selected from nitrogen atoms (saturated heterocyclic group can be substituted with one substitute selected from phenyl C_1-6alkyl group and C_1-6alkyl group), C_1-6alkanoyl group (C_1-6alkanoyl group can be substituted with an amino group or diC_1-6alkylamino group) or C_1-6alkyl group which can be substituted with 1-3 substitutes selected from a group of substitutes 1, or R¹ and R² may be combined together with a nitrogen atom to which they are bonded to form a 4-8-member saturated nitrogen-containing heterocyclic group, which can additionally contain 1 heteroatom selected from a nitrogen atom (saturated nitrogen-containing heterocyclic group can be substituted with 1 substitute selected from hydroxy group, amino group, diC_1-6alkylamino group and C_1-6alkyl group (C_1-6alkyl group can be substituted with diC_1-6alkylamino group)). Values of other substitutes are given in patent claim. Invention also relates to a medicinal agent as a macrolide antibiotic for prevention and/or therapeutic treatment of various microbial infectious diseases, containing disclosed compound as an active ingredient, and to a compound of formula (VIII).

EFFECT: technical result is obtaining novel compounds having strong antibacterial activity.

20 cl, 22 tbl, 576 ex