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Salts of benzimidazole compounds, their use and synthetic preparation

AnthelminticsAnti-cancer agentsBenzimidazolesChiral separationWater solubility

Introduction

Pharmaceuticals salts drugs with benzimidazole structure already on the market that have better chemical-physical and pharmacokinetic characteristics than the starting products that can be used in anthelmintic and anti-tumor therapy.

Technical features

Production, through a simple and economical synthetic procedure, of water-soluble salts of the sulfoxides of the chiral drugs listed in the title both in the form of racemic mixture and in enantiopure form. Products having the characteristics of the salts of the proposed invention do not exist in the chemical literature. An innovative feature of the salts object of the invention relates to the fact that they can be solubilized in water. This characteristic allows the administration of the drug, as well as by oral route, also by parenteral route, providing a greater bioavailability and the achievement of optimal therapeutic levels at lower doses than those foreseen for the non-salified forms. The synthetic strategy for the preparation of the salts of the invention provides for a single and simple salification step in which the nitrogen atom of the imidazole nucleus with acidic characteristics is de-protonated by a base capable of releasing a cation A+n = Li+, Na+, K+, Mg+2 and Ca+2. Contrary to the unsalified forms, the saline forms with A+n = Li+, Na+, K+ are soluble in water.

Possible Applications

  • Systemic Cancer Treatment;
  • Veterinary field, new water-soluble formulations of anthelmintic drugs allow to adopt simpler methods of administration;
  • Treatment and prevention of parasitic diseases that develop in farm animals, pets and humans.

Advantages

  • Possible parenteral administration in addition to the oral route;
  • Greater bioavailability;
  • Achievement of optimal therapeutic levels at lower doses than those foreseen for the unsalified forms.