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water soluble derivative of 1 - (2 - hydroxyethyl) - 2 - methyl - 5 - nitro imidazole therapeutic activity, process for its preparation and related pharmaceutical compositions

机译:1-(2-羟乙基)-2-甲基-5-硝基咪唑的水溶性衍生物的治疗活性,其制备方法及相关药物组合物

摘要

The N-(5-carboxy-5-aminopentan)-carbonic ester of 1-(2-hydroxyethyl)-2-methyl-5-nitro-imidazole is perfectly soluble in water and shows relevant trichomonacide activity. The process for the preparation of the compound of the invention comprises reacting 1-(2-hydroxyethyl)-2-methyl-5-nitro imidazole with an alkyl- or phenyl-chlorocarbonate and hydrolizing the resulting carbonic ester, after isolation, in a water-alcohol medium with lysine hydrochloride. The invention relates furthermore to the pharmaceutical compositions, containing the derivative according to the invention, in form suitable for the several administration routes, in combination with the usual excipients and additives.
机译:1-(2-羟乙基)-2-甲基-5-硝基-咪唑的N-(5-羧基-5-氨基戊烷)-碳酸酯完全溶于水,并显示出相关的滴虫酰胺活性。制备本发明化合物的方法包括使1-(2-羟乙基)-2-甲基-5-硝基咪唑与烷基-或苯基-氯代碳酸酯反应,并在分离后在水中将所得碳酸酯水解。 -含赖氨酸盐酸盐的酒精培养基。本发明还涉及含有本发明衍生物的药物组合物,其形式适合于几种给药途径,并与常规的赋形剂和添加剂结合。

著录项

  • 公开/公告号IT1194283B

    专利类型

  • 公开/公告日1988-09-14

    原文格式PDF

  • 申请/专利权人 PIETRO ISNARDI & C. SPA.;

    申请/专利号IT19830021704

  • 发明设计人 REINER ALBERTO;

    申请日1983-06-21

  • 分类号A61K;

  • 国家 IT

  • 入库时间 2022-08-22 06:58:14

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