| 摘要 |
Benzodiazepine derivs. of formula (I) and their stereoisomers and salts are new. Ra = H, 1-4C alkyl, CH2-CHOH-(CH2)m-Z or (CH2)nCORo; m = 0 or 1; Z = 1-4C alkyl, 3-8C cycloalkyl, or aryl or heterocyclyl opt. substd. by 1-4C alkyl, 1-4C alkoxy or halo; n = 1-3; Ro = OR2 or NR2R3; R2, R3 = H or 1-4C alkyl, or NR2R3 is a satd. or unsatd. heterocyclic ring; Rb = Rba or NHRbb; Rba = quinolyl, isoquinolyl, benzimidazolyl, indolyl, or indolyl N-substd. by CO-(1-4C alkyl) or (CH2)nCORo; Rbb = phenyl monosubstd. by halo, 1-3C alkyl or 1-3C alkoxy; X1-X3 = 1-3C alkyl, 1-3C alkoxy, halo or CF3; X4 = H, or is identical to X1, X2 or X3. Also claimed are intermediates of formula (II) (as (I) but with NHCORb replaced by NH2) and their stereoisomers and salts. |
