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C-aryl glucoside SGLT2 inhibitors
专利权人:
BRISTOL-MYERS SQUIBB CO
发明人:
SHER PHILIP M,WASHBURN WILLIAM N,MENG WEI,WU GANG,ELLSWORTH BRUCE A
申请号:
NO20070149
公开号:
NO332798B1
申请日:
2007.01.09
申请国别(地区):
NO
年份:
2013
代理人:
摘要:
SGLT2 inhibiting compounds are provided having the formulawhereR1, R2, and R2a are independently hydrogen, OH, OR5, lower alkyl, CF3, OCHF2, OCF3, SR5i or halogen, or two of R1, R2 and R2a together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle;R3 and R4 are independently hydrogen, OH, OR5a, OAryl, OCH2Aryl, lower alkyl, cycloalkyl, CF3, -OCHF2, -OCF3, halogen, -CN, -CO2R5b, -CO2H, -COR6b, -CH(OH)R6c, -CH(OR5h)R6d, -CONR6R6a, -NHCOR5c, -NHSO2R5d, -NHSO2Aryl, Aryl, -SR5e, -SOR5f, -SO2R5g, -SO2Aryl, or a five, six or seven membered heterocycle, or R3 and R4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle;R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h and R5i are independently lower alkyl;R6, R6a, R6b, R6c and R6d are independently hydrogen, alkyl,aryl, alkylaryl or cycloalkyl, or R6 and R6a together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle;A is O, S, NH, or (CH2)n where n is 0-3.A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.Det beskrives SGLT2-inhibitorforbindelser med formelen hvor R1, R2 og R2a uavhengig er hydrogen, OH, OR5, lavere alkyl, CF3, OCHF2, OCF3, SR5' eller halogen, eller to av R1, R2 og R2a sammen med karbonatomene som de er tilknyttet, kan danne en annelert fem-, seks- eller syv-leddet karbocyklisk eller heterocyklisk ring; R3 og R4 er uavhengig hydrogen, OH, OR5a, OAryl, OCH2Aryl, lavere alkyl, cykloalkyl, CF3, -OCHF2, -OCF3l halogen, -CN, -CO2R5b, -CO2H, -COR6b, -CH(OH)R6c, -CH^R^R*1, -CONR6R6a, -NHCOR5c, -NHSOgR501, -NHSO2Aryl, Aryl, -SR5e, -SOR5f, -SO2R5g, -SO2Aryl, eller en fem-, seks- eller syv-leddet heterocyklisk ring, eller hvor R3 og R4 sammen med karbonatomene som de er tilk
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