| 摘要 |
Pyrrolo (3,4-d) benzazepine derivs. (I) and their acid addn. salts where A is a group of formula (Ia) are new: A is a group of formula (Ia), (Ib), (Ic), (Id) or (Ie); R1 is H, lower alkyl 3-7C alkenyl, 3-7C alkynyl, CH2OH or -CO-R11; R11 is H, OH, alkoxy, NH2 or mono- or di (lower) alkyl imino; R3 is H, lower alkyl, 3-7C alkenyl, 3-7C alkynyl, CH2OH or -CO-R111; R111 is H, OH, trihalomethyl, alkoxy, NH2 or mono- or di(lower alkyl)amino; R2 is H, lower alkyl, 3-7C alkenyl, 3-7C alkynyl, -COO (lower alkyl), a 2-7C carboxylic acid residue or ester or amide thereof, hydroxy-(2-7C alkyl), or amino- or mono- or di(lower alkyl)amino (2-7C alkyl); R5 is H, F, Cl or Br; R6 is F, Cl or Br; R95 is lower alkyl; and Z is the anion of an acid. Provisos are that (a) when one of R1 and R3 is hydroxymethyl, -CO-R11 or -CO-R111 then the other of R1 and R3 is H, lower alkyl, 3-7C alkenyl or 3-7C alkynyl and R2 is H, (b) when R4 is acyloxy, then R1 and R3 are H, lower alkyl, 3-7C alkenyl or 3-7C alkynyl and R2 is -CO-(lower alkoxy), (c) when R4 is OH then R1 and R3 are H, lower alkyl, 3-7C alkynyl or 3-7C alkenyl and R2 is H, (d) when R4 is unbranched lower alkoxy, then R1 and R3 are H, lower alkyl 3-7C alkenyl or 3-7C alkynyl, (e) when A is a group (Ib), (Ic), (Id) or (Ie), then R4 is H and (f) when A is a group (Ib) or (Ie), then R2 is other than amino- or mono- or di- (lower alkyl) amino- (2-7C alkyl)). Also new and claimed are intermediates to (I) and their precursors (I) have sedative and anxiolytic activity. |
