| 摘要 |
There is presented benzodiazepine derivatives of the formula <IMAGE> I wherein A is the group <IMAGE> R1 is lower alkyl, R2 and R3 each are hydrogen or lower alkyl, R4 is the group <IMAGE> <IMAGE> +TR <IMAGE> R5 is hydrogen or halogen, R8 is hydrogen or lower alkyl, R9 is lower alkyl or lower alkoxyalkyl, R10 is lower alkyl, R11 is hydrogen, lower alkyl or lower hydroxyalkyl, R12 is hydrogen or lower alkyl and R14 is lower alkyl or aryl, and either R6 is hydrogen or lower alkyl and R7 is lower alkyl or lower hydroxyalkyl or R6 and R7 together with the nitrogen atom are a 3- to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula >N-R13, in which R13 is hydrogen or lower alkyl, and either R6' is hydrogen or lower alkyl and R7' is lower alkyl or R6' and R7' together with the nitrogen atom are a 3- to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula > N-R13', in which R13' is lower alkyl, with the proviso that R4 is the group R6' R7' N-CO-NH-CH(R8)- when A is the group (c), and pharmaceutically acceptable acid addition salts thereof. The compounds exhibit aldosterone-antagonistic properties and are suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension. |
