| 摘要 |
<p>Cpds. of formula (I) and their salts are new: X = CO and Y = NH; or X = NH and Y = CO; Z = CH2, O, S or NR3 and Ra is not present; R3 = H, 1-6C alkyl, 3-7C alkenyl-methyl, or phenyl or phenyl (1-4C) alkyl opt. ring substd. by 1 or 2 of halo, CF3, 1-6C alkoxy and 1-6C alkyl; or Z = CH or N and Ra is as defined for R3 above; R6 is present when X-Y-R2 is attached at the phenyl ring and = H, halo, CF3, OH, 1-6C alkoxy or 1-6C alkyl; R1 = H, halo, CF3, 1-6C alkyl, 1-6C alkoxy, 1-6C alkylthio, 1-7C acyl, 1-7C acylamino, 1-6C alkylsulphonylamino, N-(1-6C alkylsulphonyl)-N-(1-4C)alkylamino, 1-6C alkylsulphinyl, OH, NO2, or NH2, amino-carbonyl, -sulphonyl or -sulphonylamino or N-(aminosulphonyl)-(1-4C)alkylamino opt. N-substd. by 1 or 2 of 1-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl (1-4C) alkyl, phenyl and phenyl (1-4C)alkyl, or opt. N-disubstd. by 4-5C polymethylene; R2 = a gp. of formula (a)-(c): n = 2 or 3; p and q each = 1-3; R4 or R5 = 1-7C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl (1-2C)alkyl or (CH2)tR6; t = 1 or 2; R6 = thienyl, pyrrolyl or furyl (all opt. substd. by 1 or 2 of 1-6C alkyl, 1-6C alkoxy, CF3 and halo) or phenyl (opt. substd. by 1 or 2 of 1-4C alkoxy, CF3, halo, NO2, COOH, esterified carboxy and 1-4C alkyl opt. substd. by OH, 1-4C alkoxy, COOH, esterified carboxy or in vivo hydrolysable acyloxy). Intermediates Xof formula (VII) are also new: R'2 = a gp. of formula (d) or (e).</p> |
