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MERCAPTOMETHYL-OCTAHYDRO-OXO-PYRIDAZINO(1,2-A)(1,2)DIAZEPINE-,DIAZOCINE-AND(1,2,5)TRIAZEPINECARBOXYLIC ACID DERIVATIVES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND CERTAIN INTERMEDIATES THEREFOR
MERCAPTOMETHYL-OCTAHYDRO-OXO-PYRIDAZINO(1,2-A)(1,2)DIAZEPINE-,DIAZOCINE-AND(1,2,5)TRIAZEPINECARBOXYLIC ACID DERIVATIVES,THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND CERTAIN INTERMEDIATES THEREFOR
Compounds of the formula IMAGE I wherein R1 is hydrogen, alkanoyl or aroyl; R2 is hydrogen or alkyl; R3 is hydrogen or aryl; R4 and R5 each are hydrogen or R4 and R5 taken together are oxo; and Y is -CH2-, -CH2CH2-or -N(R6)-in which R6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is -N(R6)-, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described. The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
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机译：式 I的化合物，其中R1为氢，烷酰基或芳酰基; R 2是氢或烷基; R3是氢或芳基; R 4和R 5各自为氢或R 4和R 5一起为氧代;并且Y是-CH 2-，-CH 2 CH 2-或-N（R 6）-，其中R 6是氢，烷基或芳烷基，以及当R 2是氢时其与碱的可药用盐，以及当Y是氢时，其与酸的可药用盐。描述了具有抗高血压活性并且可以以药物制剂形式用作药物的-N（R6）-。式I化合物包含至少一个不对称碳原子。因此，本发明不仅包括这些化合物的光学均一形式，而且包括各种非对映异构体外消旋体和不同非对映异构体外消旋体的混合物。
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