| 摘要 |
1-Isoquinolone derivatives and related compounds according to formula (I) wherein, Y is selected from the group consisting of H, OH, lower alkoxy, and halo; X is selected from the group consisting of H, lower alkyl acid, lower alkyl ester, and lower alkyl; and R<1> is selected from the group consisting of H, alkenyl, lower alkyl, lower cycloalkyl, unsubstituted or substituted 3-spiro-1H-indane of structure (II) wherein R<2> is H, OH, lower alkyl, lower alkoxy or halo, and 3-spiro-cycloalkyl of structure (III) wherein n is an integer from zero to six, provided that when R<1> is spiro- X is H, or a pharmaceutically acceptable salt thereof, with the proviso that when R<1> is spiro-, X is H, and when R<1> is H, alkenyl, lower alkyl or lower cycloalkyl substituted at the 3-position of the isoquinolone moiety and X is H or lower alkyl, the (2"-1H--tetrazol-5-yl)biphenyl-4'-ylmethyl group cannot be at the 2(N) position, are useful as angiotensin II receptor antagonists. Also disclosed are methods of synthesis, intermediates, pharmaceutical formulations and methods of treatment. |
