发明名称 C-ARYLGLUCOSIDE INHIBITORS OF SGLT-2
摘要 FIELD: organic chemistry, biochemistry, medicine. ^ SUBSTANCE: invention proposes compounds inhibiting activity of enzyme SGLT-2 of the formula (I) ^ wherein R1, R2 and R2a mean independently hydrogen atom, hydroxyl (OH), OR5, alkyl, CF3, -OCHF2, -OCF3, CR5i or halogen atom, or two radicals among R1, R2 and R2a in common with adjacent carbon atoms can form annelated 5-membered heterocycle; R3 and R4 mean independently hydrogen atom, OH, OR5, O-aryl, OCH2-aryl, alkyl, cycloalkyl, CF3, -OCHF2, -OCF3, halogen atom, -CN, -CO2R5b, - CO2H, -CONR6R6a, -NHCOR5c, -NHSO2R5d, -NHSO2-aryl, aryl, -SR5c, -SOR5f, -SO2R5g, -SO2-aryl, or 5-, 6- or 7-membered carbocycle or heterocycle; R5, R5a, R5b, R5c, R5d, R5e, R5f, RR5g, R5h and R5i means independently alkyl; R6, R6a, R6b, R6c and R6d mean independently hydrogen atom, alkyl, aryl, alkylaryl or cycloalkyl, or R6 and R6a in common with adjacent nitrogen atoms form annelated 5-, 6- or 7-membered heterocycle; A means oxygen (O), sulfur (S) atom, NH or (CH2)n wherein n = 0-3. Also, invention proposes a method for treatment of diabetes mellitus and related diseases by using the above described compound in doses inhibiting activity of SGLT-2 taken as a single substance or in combination with other therapeutic agents. ^ EFFECT: valuable medicinal and biochemical properties of inhibitors. ^ 19 cl, 2 tbl, 82 ex
申请公布号 RU2262507(C2) 申请公布日期 2005.10.20
申请号 RU20020109477 申请日期 2000.10.02
申请人 发明人 ILLSUORT BRJUS;UOSHBURN UILL'JAM N.;SHER FILIP M.;VU GANG;MENG VEJ
分类号 C07D309/10;A61K31/351;A61K31/41;A61K31/433;A61K31/70;A61K31/7032;A61K31/7034;A61K45/00;A61K45/06;A61P3/04;A61P3/06;A61P3/10;A61P9/10;A61P9/12;A61P17/02;A61P27/02;A61P43/00;C07C43/225;C07C45/46;C07C49/84;C07D405/06;C07D417/06;C07H7/04;C07H15/203 主分类号 C07D309/10
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