| abstract |
(i) mindestens eines von R 1 und R 2 Wasserstoff ist; (ii) wenn R 3 niederes Acyloxy oder Hydroxy bedeutet, A Gruppe (a), X Wasserstoff, Halogen, Trifluormethyl, Aethyl oder Acetyl und, wenn R 1 die Gruppe -NH(CH 2 )mNR 8 R 9 bedeutet, R' und R 9 je niederes Alkyl bedeuten; (iii) wenn A Gruppe (d) und R 1 die Gruppe -NH(CH 2 )mNR 8 R 9 bedeuten, R' und R 9 je niederes Alkyl bedeuten; und (iv) wenn n 1 bedeutet, R 1 Wasserstoff, niederes Alkyl, niederes Alkoxy, Chlor, Brom oder die Gruppe -CH 2 -CO-R 7 (worin R 7 obige Bedeutung besitzt) und A Gruppe (a) oder (b) bedeuten; nund pharmazeutisch akzeptable Säureadditionssalze davon sind neu und pharmakologisch verwertbar als Anxiolytika und Sedativa. Diese Verbindungen und Salze können nach verschiedenen Methoden ausgehend von teilweise neuen Zwischenprodukten hergestellt werden.Pyrimido-2-benzazepines of the general formula where A is one of the groups R 1 is hydrogen, chlorine, bromine, lower alkyl, the group NR 4 R 5 , the group -CH 2 -CO-R 7 , the group -NH (CH 2 ) m NR 8 R 9 , hydroxy, lower alkoxy, mercapto or lower alkyl mercapto, R 2 hydrogen, amino or di- (lower) alkylamino, R hydrogen, lower acyloxy or hydroxy, X hydrogen, halogen, trifluoromethyl, ethyl, a-hydroxyethyl or acetyl, Y hydrogen or halogen, R 4 and R 5 each hydrogen or lower alkyl or, together with the nitrogen atom, a 5- to 7-membered heterocycle which may contain an oxygen or sulfur atom or the group N-lower alkyl, R 7 is hydrogen, lower alkoxy or NR 8 R 9 , R 6 and R 9 are each hydrogen or lower alkyl, n is 0 or 1 and m is 1 to 7, with the proviso that (i) at least one of R 1 and R 2 is hydrogen; (ii) when R 3 is lower acyloxy or hydroxy, A group (a), X is hydrogen, halogen, trifluoromethyl, ethyl or acetyl and when R 1 is the group -NH (CH 2 ) mNR 8 R 9 , R 'and R 9 each represent lower alkyl; (iii) when A group (d) and R 1 are the group -NH (CH 2 ) mNR 8 R 9 , R 'and R 9 are each lower alkyl; and (iv) when n is 1, R 1 is hydrogen, lower alkyl, lower alkoxy, chlorine, bromine or the group -CH 2 -CO-R 7 (in which R 7 has the above meaning) and A group (a) or (b) mean; and pharmaceutically acceptable acid addition salts thereof are new and pharmacologically useful as anxiolytics and sedatives. These compounds and salts can be prepared using various methods, some of which are new intermediates. |