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2-(substituted methylidene)-N-3-piperidin-1-ylpropylhydrazine carboximidamides useful as antiparasitics

机译:用作抗寄生虫药的2-(取代的亚甲基)-N- [3- [哌啶-1-基]丙基]肼碳亚胺

摘要

The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.
机译:本发明涉及由宿主中的入侵生物引起的疾病的治疗,其方法是首先确定宿主与入侵生物之间的酶促差异,然后对宿主施用药学有效量的颠覆性底物以用于不同的入侵酶。生物体,不同酶的作用导致的结果与酶的预期结果和功能相反,导致酶的衰弱或死亡。特别地,通过施用药学有效的抗寄生虫量的竞争性产毒素的锥虫对硫磷还原酶来治疗由运动型体质引起的寄生虫病,包括锥虫和利什曼原虫,例如非洲昏睡病,查加斯病,东方疮和黑热病。治疗方法及其组合物含有竞争性产锥虫硫醚还原酶的产毒底物。公开了许多化合物和相应的组合物。

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