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2,3-Indoledione derivatives, process for their preparation, intermediates, pharmaceutical compositions containing these 2,3-indoledione derivatives and their pharmaceutical use

机译:2,3-吲哚二酮衍生物,其制备方法,中间体,含有这些2,3-吲哚二酮衍生物的药物组合物及其药物用途

摘要

The new compounds of the general formula wherein R is isopropyl or t-butyl, R 1 is hydrogen or lower alkyl and R 2 is lower alkyl or lower aralkyl, and their pharmaceutically acceptable acid addition salts are prepared by reacting a compound of the formula wherein R 3 is hydroxy and R 4 is chlorine or bromine, or R 3 and R 4 together represent an oxygen atom, and R 1 and R 2 have the above meanings, with an amine of formula wherein R has the above significance, if desired, a resulting racemate is separated into the two antipodes and, if desired, converting a resulting compound of formula I into a pharmaceutically acceptable acid addition salt. The compounds of formula I and their aforementioned salts are useful as β-adrenergic blockers and antihypertensive agents.
机译:通式为的新化合物,其中R为异丙基或叔丁基,R 1 为氢或低级烷基,R 2 为低级烷基或低级芳烷基及其药学上可接受的酸加成盐是通过使式的化合物反应制备的,其中R 3 是羟基,R 4是氯或溴,或R 3 和R 4 一起代表一个氧原子,R 1 和R 2 具有上述含义,其中的式为的胺,其中R具有上述含义,如果需要,可将得到的外消旋体分离为两个对映体,如果需要,可将其转化为对映体式I化合物转化为药学上可接受的酸加成盐。式I化合物及其前述盐可用作β-肾上腺素能阻滞剂和抗高血压药。

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