PYRIMIDINE GYRASE AND TOPOISOMERASE IV INHIBITORS Russian patent published in 2017 - IPC C07D405/14 C07F9/6558 A61K31/506 A61P31/04 

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, which having gyrase MIC and topoisomerase IV inhibiting properties and can be used for treating bacterial infections, mediated by one or more bacteria from Streptococcus pneumoniae, Staphylococcus epidermidis, Enterococcus faecalis, Staphylococcus aureus, Clostridium difficile, Moraxella catarrhalis, Neisseria gonorrhoeae, Neisseria meningitidis, Mycobacterium avium complex, Mycobacterium abscessus, Mycobacterium kansasii, Mycobacterium ulcerans, Chlamydophila pneumoniae, Chlamydia trachomatis, Haemophilus influenzae, Streptococcus pyogenes or β-haemolytic streptococci. Infections are infections of lower and upper airway, ear infections, pleuropulmonary and bronchial infections, infections of urinary tract, intraabdominal infections, cardiovascular infections, blood poisoning, sepsis, bacteriaemia, CNS infections, skin and soft tissue infection, gastro-intestinal infections, infections affecting bones and joints, genital infections, eye infections or granulomatous infections, uncomplicated skin and skin structure infections (uSSSI), catheter infections, pharyngitis, sinusitis, etc. In formula (I)

R is hydrogen or fluorine; X is hydrogen, -PO(OH)₂, -PO(OH)O^-M⁺, -PO(O^-)₂⋅2M⁺ or -PO(O^-)₂⋅D²⁺; M⁺ is a pharmaceutically acceptable univalent cation, such as Li⁺, Na⁺, K⁺, N-methyl-D-glucamine and N(R⁹)₄⁺, where each R⁹ is independently hydrogen or C₁-C₄ alkyl group; D²⁺ is a pharmaceutically acceptable divalent cation, such as Mg²⁺, Ca⁺² and Ba²⁺.

EFFECT: novel compounds.

21 cl, 2 dwg, 27 tbl, 39 ex