发明名称 OXAZOLE TETRACYCLINE DERIVATIVES
摘要 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
申请公布号 RU2415844(C2) 申请公布日期 2011.04.10
申请号 RU20060118367 申请日期 2004.12.07
申请人 VAJET 发明人 SAM FAIK-EHNG;KHOU DAVID BRAJAN;KHOPPER DARRIN UILL'JAM;VERA MEHTT'JU DUGLAS;SABATINI DZHOSHUA DZHEJMS
分类号 A61K31/423;A61K31/65;A61P31/04;C07C237/26;C07D263/52;C07D413/04;C07D413/06;C07D417/04 主分类号 A61K31/423
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