发明名称 Substituted quinazolines as angiotensin II antagonists
摘要 There are disclosed compounds of the general formula I: <IMAGE> I wherein A is -CR7=CR8-; Z is -CR7=CR8-; X is H, NR 9R10, OR11, CN, F, Cl, I, Br, perfluoroalkyl, alkyl,alkoxy, alkyl-OH, alkoxyalkyl, -(CH2)nCO2R11,-(CH2)nCONR9R10; Y is NR13,NR13CR12R14, CR12R14NR13; R1 is 5-tetrazolyl, CO2R11,SO3H, NHSO2CH3, NHSO2CF3; R2,R3,R4,R7R8 is H, alkyl, alkoxy, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, CN, NO2, SO2R13, -(CH2)nCO2R11,-(CH2)nCONR9R10, OR11,F,Cl,Br,I,NR9R10; R5 is alkyl, alkoxy, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, H, -CN, NO2, SO2R13,-(CH2)nCO2R11, -(CH2)nCONR9R10, -OH,OR11,F,Cl,Br,I,NR9R10; R9,R10 is H, alkyl, alkoxyalkyl,alkyl-OH, perfluoroalkyl, aralkyl; R11 is H, alkyl, aralkyl, alkoxyalkyl; R12,R14 is H, alkyl, alkoxy, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, CN, NO2, SO2R13, -(CH2)nCO2R11, -(CH2)nCONR9R10; R13 is H, OR11, alkyl, perfluoroalkyl, aralkyl, -(CH2)nCO2R11,-(CH2)nCONR9R10; 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 and the phamaceutically 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.
申请公布号 US5187168(A) 申请公布日期 1993.02.16
申请号 US19910782850 申请日期 1991.10.24
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 PRIMEAU, JOHN L.;GARRICK, LLOYD M.
分类号 C07D239/74;A61K31/505;A61K31/517;A61P3/06;A61P9/00;A61P9/12;C07D239/78;C07D239/80;C07D239/94;C07D239/95;C07D403/12;C07D405/12;C07D409/12;C07D491/052;C07D495/04 主分类号 C07D239/74
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