OXAZOLE TETRACYCLINE DERIVATIVES Russian patent published in 2011 - IPC C07D263/52 C07C237/26 A61K31/423 A61P31/04 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula (I), its tautomers and pharmaceutically acceptable salts. In formula X is chosen from hydrogen, -NR¹¹ R¹², A" is a group chosen from: and R¹¹ and R¹² are independently chosen from alkyl with 1-6 carbon atoms; Y represents hydrogen; R is chosen from alkyl containing 1 to 6 carbon atoms which can have optionally independently 1-2 substitutes representing halogen, alkenyl with 2-6 carbon atoms which optionally independently contain 1-2 substitutes chosen from phenyl, optionally substituted by alkoxy with 1 to 6 carbon atoms, halogen, heteroaryl with 5 atoms of a ring containing 1 heteroatom; -CH₂NR¹R²; aryl with 6 carbon atoms which optionally contains 1-3 substitutes independently chosen from halogen, cyano, hydroxy, alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms, benzyloxy, di(alkyl with 1-6 carbon atoms)amino, and methylene dioxy; heteroaryl with 5 or 6 ring atoms containing 1-2 heteroatoms which can be identical or different and are independently chosen from nitrogen, oxygen, sulphur, optionally containing 1 substitute representing -CH₂OCOCH₃; benzofuranyl and benzothienyl; or a group consisting of -SR³; R¹ and R² are independently H or alkyl with 1-6 carbon atoms, or R¹ and R² together with nitrogen atom whereto each of them is bound, form a 5- or 6-members saturated ring containing one heteroatom N; R³ is chosen from -CH₂-phenyl optionally substituted by halogen; CH₂(CO)OCH₂phenyl; provided X is NR¹¹R¹², and R¹¹ is hydrogen, then R¹² is methyl, ethyl, n-propyl, n-butyl, 1-methylethyl, 1-methylpropyl, 2-methylpropyl or 1,1-dimethylethyl; and provided R¹¹ is methyl or ethyl, then R¹² is methyl, ethyl, n-propyl, 1-methylethyl, n-propyl, 1- methylpropyl or 2- methylpropyl.

EFFECT: preparation of a pharmaceutical composition exhibiting antimicrobial activity, containing a compound of the invention, development of a method of treating or controlling a bacterial infections and a method of producing the chemical compound of formula:

28 cl, 8 tbl, 2 dwg, 49 ex