首页> 外国专利> Novel bis- and mono-quaternary ammonium derivatives of 2-beta, 16-beta-dipiperidino-5-alpha-androstanes, processes for their preparation and pharmaceutical preparations

Novel bis- and mono-quaternary ammonium derivatives of 2-beta, 16-beta-dipiperidino-5-alpha-androstanes, processes for their preparation and pharmaceutical preparations

机译:2-beta,16-beta-dipiperidino-5-alpha-androstanes的新型双季铵盐和单季铵盐衍生物,其制备方法和药物制剂

摘要

The invention relates to novel bisquaternary ammonium derivatives of 2 beta ,16 beta -dipiperidino-5 alpha -androstanes having the formula: IMAGE wherein IMAGE R2=CH3, C2H5 or CH2CH=CH2; R3=CH3, C2H5 or CH2CH=CH2, with the proviso that R2 and R3 are not CH3 simultaneously; R4=O or H( beta OR5), wherein R5=H or aliphatic carbacyl (1-6 C); and X=a halogen atom, to processes for their preparation and to pharmaceutical preparations. The invention also relates to novel 16-monoquaternary analogs as intermediates. The compounds possess neuromuscular blocking activity.
机译:本发明涉及具有以下化学式的2β,16β-二哌啶子基-5α-雄烷二酮的新型双季铵衍生物,其中:[IMAGE] R2 = CH3,C2H5或CH2CH = CH2; R3 = CH3,C2H5或CH2CH = CH2,条件是R2和R3不是同时为CH3; R 4 = O或H(βOR 5),其中R 5 = H或脂族碳酰基(1-6 C); X =卤素原子,涉及其制备方法和药物制剂。本发明还涉及作为中间体的新颖的16-单季类似物。该化合物具有神经肌肉阻断活性。

著录项

  • 公开/公告号EP0032261B1

    专利类型

  • 公开/公告日1983-09-28

    原文格式PDF

  • 申请/专利权人 AKZO N.V.;

    申请/专利号EP19800201186

  • 发明设计人 KELDER JAN DR.;

    申请日1980-12-09

  • 分类号C07J43/00;A61K31/58;

  • 国家 EP

  • 入库时间 2022-08-22 10:34:07

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