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Pharmaceutical sulphoanilides - vasopressors, vasodepressors, analgesics, bronchodilators, alpha and beta-blocking agents or stimulants etc.

机译:药物磺酰苯胺-升压药,降压药,镇痛药,支气管扩张药,α和β阻滞剂或兴奋剂等。

摘要

Compounds of general formula: and their acid addition and metal salts. X = H, OH, NH2, alkoxy, benzyloxy, halogen, CH3 or R2SO2NH-; R' and R2 = alkyl, phenyl or tolyl; Z =R3 = H, Me; = pyrrolidino, morpholino, piperidino or amino where R4 = H, alkyl or benzyl and R5 = H, alkyl, or aralkyl opt. subst. in the ring by OH, OMe or methylenedioxy, aryloxyalkyl opt. subst. in ring by OH, OMe or methylenedioxy. The alkyl and alkoxy groups have C1-C4. Aralkyl and aryloxyalkyl groups have up to C10. Vasopressors, vasodepressors, analgesics, bronchodilators, alpha- and beta-blocking agents or stimulants, smooth muscle depressants dependent on particular substituents. A specially preferred compound is 3-(2-methylamino-1-hydroxyethyl) methane sulphonanilide which is a moderately long acting adrenergic vasoconstrictor. It is free of cardiac and central side effects found with other phenethanolamines and it is useful to reduce bleeding in surgery, as nasal decongestant and in relief of shock.
机译:通式:的化合物及其酸加成盐和金属盐。 X = H,OH,NH 2,烷氧基,苄氧基,卤素,CH 3或R 2 SO 2 NH-; R 1和R 2 =烷基,苯基或甲苯基; Z = R3 = H,Me; =吡咯烷基,吗啉代,哌啶子基或氨基,其中R 4 = H,烷基或苄基,R 5 = H,烷基或芳烷基。替代在环上由OH,OMe或亚甲基二氧基,芳氧基烷基选择。替代由OH,OMe或亚甲二氧基成环。烷基和烷氧基具有C 1 -C 4。芳烷基和芳氧基烷基基团具有至多C 10。血管升压药,血管降压药,止痛药,支气管扩张药,α和β阻滞剂或兴奋剂,平滑肌抑制剂(取决于特定的取代基)。特别优选的化合物是3-(2-甲基氨基-1-羟乙基)甲烷磺酰苯胺,它是中等长效的肾上腺素能血管收缩剂。它没有其他苯乙醇胺所引起的心脏和中枢副作用,对于减少手术中的出血,鼻充血和减轻电击有用。

著录项

  • 公开/公告号NL7312626A

    专利类型

  • 公开/公告日1973-11-26

    原文格式PDF

  • 申请/专利权人

    申请/专利号NL19730012626

  • 发明设计人

    申请日1973-09-13

  • 分类号C07C143/72;A61K27/00;C07D13/10;C07D27/04;C07D29/34;C07D87/46;A61K27/00B;

  • 国家 NL

  • 入库时间 2022-08-23 06:09:08

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