| 摘要 |
<p>Biphenyl-2-carboxylic acid-tetrahydro-isoquinolin-6-yl amide derivs. of formula (I) and their salts are new. X = CH2, CO, CS or SO2; Y = a direct link, 2-10C aliphatic hydrocarbylene (opt. substd. by OH, 1-10C alkoxy, 1-10C acyl, 1-10C acyloxy or 6-10C aryl), NH or O; provided that is X = CH2, then Y is a direct link; Z = (i) H, halo or CN, (ii) OH, 1-10C alkoxy, 1-10C alkylthio, 1-10C acyl, thiophenylcarbonyl or 1-10C alkoxycarbonyl, (iii) 1-10C alkylamino, di(1-10C)alkylamino, 6-10C aryl(1 10C)alkylamino, provided that Y is not O or NH, (iv) vinyl, 6-10C aryl, 3-8C cycloalkyl opt. benz-fused, 7-10C polycycloalkyl, 4-8C cycloalkenyl, 7-10C polycycloalkenyl, (v) 6-10C aryloxy, 6-10C arylthio, 6-10C aryl(1-10C)alkoxy, 6-10C aryl(1-10C)alkylthio, 3-8C cycloalkoxy or 4-8C cycloalkenyloxy, (vi) monocyclic or fused polycyclic radical contg. 5-14 ring atoms, including 1-4 ring heteroatoms selected from O, N and S, the individual rings being satd., partially unsatd. or aromatic; provided that (a) if X is CH2, Z is H or one of (iv) or (vi); and (b) when Z contains 1 or more rings, they are opt. substd. by 1-4 halo, OH, CN, NO2, oxo, thioxo, aminosulphonyl, Ph, phenoxy, phenylthio, halophenylthio, benzyl, benzyloxy, 1-10C alkyl(1-10C)alkoxy, 1-10C alkoxycarbonyl, 1-10C alkylthio, 1-10C alkylamino, 1-10C alkylaminocarbonyl, di(1-10C)alkylamino, di(1-10C)alkylaminocarbonyl, di(1-10C)alkylamino(1-10C)alkoxy, 1-3C perfluoroalkyl, 1-3C perfluoroalkoxy, 1-10C acyl, 1-10C acyloxy, 1-10C acyloxy(1-10C)alkyl and pyrrolidinyl.</p> |
