| 摘要 |
There are disclosed compounds of the general formula I: <IMAGE> I wherein X is H, NR12R13, OR14, CN, F, Cl, I, Br, perfluoroalkyl, alkyl, alkoxy, alkyl-OH, alkoxyalkyl, -(CH2)nCO2R14, -(CH2)nCONR12R13; Y is NR15, NR18CR16R17, CR16R17NR15; R1 is 5-tetrazolyl, CO2R14, SO3H, NHSO2CH3, NHSO2CF3; R2, R3 is H, alkyl, alkoxy, alkoxyalkyl, alkyl-OH perfluoroalkyl, aralkyl, CN, NO2, SO2R19, -(CH2)nCO2R14, -(CH2)nCONR12R13, OR14, F, Cl, Br, I, NR12R13; R4-R11 is H, F, alkyl, alkoxy, alkoxyalkyl, -OCOR14, alkyl-OH, perfluoroalkyl, aralkyl, aryl, CN, NO2, SO2R19, -(CH2)nCO2R14, -(CH2)nCONR12R13, OH, OR14, -NR12R13, any two geminal groups can be O or CH2; R12, R13 is H, alkyl, aralkyl; R14 is H, alkyl, aralkyl, alkoxyalkyl; R15 is H, alkyl, -(CH2)nCO2R14, alkoxyalkyl, aralkyl, -(CH2)nCONR12R13, OR14, perfluoroalkyl, alkyl-OH, -COR14, -CONR12R13; R16, R17 is H, alkyl, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, CN, NO2, SO2R19, -(CH2)nCO2R14, -(CH2)nCONR12R13; R18 is H, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, OR14, -(CH2)nCO2R14, -(CH2)nCONR12R13, alkyl, -COR14, -CONR12R13; R19 is alkyl, aralkyl; n is 0, 1, 2 or 3; m is 1-5; wherein alkyl is defined as 1-8 carbons, branched or straight chain; perfluoroalkyl is defined as 1-6 carbons; aralkyl is defined as 7-12 carbons or 7-12 carbons substituted with fluorine, bromine or chlorine; aryl is defined as 6-10 carbons or 6-10 carbons substituted with fluorine, bromine or chlorine and the pharmaceutically acceptable salts, solvates and hydrates thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.
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