| 摘要 |
Biphenyl derivatives of cyclobutene-1,2-dione of formula 1 are angiotensin II antagonists and are useful for the treatment of hypertension and congestive heart failure <IMAGE> 1 wherein: Y is O, NR7, NCOR7; or R5 and Y taken together represent a linking chain of N=CR8N; or R5 and Y taken together represent a linking chain of (CR9R10)nCON where n=1,2,3,4, or 5; X is N, CR7; Z is N, CR7; R1 is H, alkyl, benzyl, alkoxyalkyl, phenyl; R2 is H, alkyl, benzyl, alkoxyalkyl, phenyl, alkoxy, alkyl-OH, perfluoroalkyl, F, Cl, Br, I, NR7R8; R3 is H, alkyl, benzyl, alkoxyalkyl, phenyl, alkoxy, alkyl-OH, perfluoroalkyl, F, Cl, Br, I, NR7R8; R4 is H, NR7R8, OR1, CN, F, Cl, I, Br, perfluoroalkyl, alkyl, phenyl, alkoxy, alkyl-OH, alkoxyalkyl, -(CH2)nCO2R1, -(CH2)nCONR7R8 where n=1, 2, 3, 4, or 5; R5, R6 is independently chosen from H, alkyl, benzyl, alkoxyalkyl, phenyl, F, Cl, NR7R8; or R5 and R6 taken together represent a linking chain of CR9R10 of up to 6 linking members; or R5 and R6 taken together represent a repeating linking chain of (R9C=CR10) up to 2 repeating units; R7 is H, alkyl, phenyl, benzyl; R8 is H, alkyl, phenyl, benzyl; R9 is chosen from H, alkyl, benzyl, alkoxyalkyl, phenyl, halogen, OR1, NR7R8; R10 is chosen from H, alkyl, benzyl, alkoxyalkyl, phenyl, halogen, OR1, NR7R8; wherein alkyl contains 1-8 branched or straight chain carbon atoms or the pharmaceutically acceptable sets thereof.
|
