首页> 外国专利> PROCESS FOR PRODUCING MONO- AND BIS-QUATERNARY AMMONIUM-DERIVATIVES OF 2-BETA,16-BETA-DIAMINO-5-ALPHA-ANDROSTANES

PROCESS FOR PRODUCING MONO- AND BIS-QUATERNARY AMMONIUM-DERIVATIVES OF 2-BETA,16-BETA-DIAMINO-5-ALPHA-ANDROSTANES

机译:制备2-BETA,16-BETA-DIAMINO-5-α-雄激素的单价和BIS季铵衍生物的方法

摘要

This invention relates to novel mono- and bisquaternary ammonium derivatives of 5 alpha -androstanes having the formula: IMAGE wherein: R1=H or alkyl (1-4 C); R2 and R3 each are alkyl (1-4 C) or form together with the N-atom a piperidino, pyrrolidino or morpholino group; R4=O or H( beta OR5) and R5=H or acyl derived from an organic carboxylic acid having 1-18, preferably 1-6 carbon atoms; the quaternarizing group being a saturated or unsaturated aliphatic hydrocarbon group having 1-4 carbon atoms the anion being halide; and acid addition salts of the monoquaternary compounds; and to pharmaceutical preparations containing one or more of said androstane compounds as active constituent. The compounds according to the invention are non-depolarizing neuromuscular blocking agents having very quick onset and recovery characteristics, a short duration of action and a favorable dissociation between muscle blocking and vagal blocking effects.
机译:本发明涉及新的5种α-雄烷酮的单和双季铵衍生物,其分子式为:式中:R 1 = H或烷基(1-4C);和R 2和R 3各自为烷基(1-4 C)或与N原子一起形成哌啶子基,吡咯烷基或吗啉代基团; R 4 = O或H(βOR 5),R 5 = H或衍生自具有1-18个,优选1-6个碳原子的有机羧酸的酰基;季铵化基团是具有1-4个碳原子的饱和或不饱和脂族烃基,阴离子是卤素。一元化合物的酸加成盐;以及含有一种或多种所述雄甾烷化合物作为活性成分的药物制剂。根据本发明的化合物是非去极化神经肌肉阻滞剂,其具有非常快速的发作和恢复特性,短的作用持续时间以及在肌肉阻滞和迷走神经阻滞作用之间有利的解离。

著录项

  • 公开/公告号HU186074B

    专利类型

  • 公开/公告日1985-05-28

    原文格式PDF

  • 申请/专利权人 AKZO NVNL;

    申请/专利号HU19820001917

  • 申请日1982-06-14

  • 分类号C07J43/00;

  • 国家 HU

  • 入库时间 2022-08-22 08:15:47

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