Piperazines as antimalarial agents

A technology of piperazine and compounds, applied in the field of preparation of these compounds, can solve problems such as the rapid spread of drug resistance and threats to malaria endemic areas

Active Publication Date: 2012-09-12
IDORSIA PHARM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, resistance to many currently available antimalarial drugs is spreading rapidly and threatening people in malaria-endemic areas

Method used

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  • Piperazines as antimalarial agents
  • Piperazines as antimalarial agents
  • Piperazines as antimalarial agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0136] Compounds of formula I according to the invention may be prepared according to the procedures described herein, in particular as described in the Examples section.

[0137] In general, all chemical transformations can be carried out according to well-known standard methods as described in literature sources or as described in the following procedures.

[0138] except R 1 Yes - NCH 3 (CH 2 CH 2 OH) The preparation method of the compound of formula I except the compound:

[0139]

[0140] plan 1

[0141] Boc-Phe- OH 1 is coupled with benzylpiperazine derivative 2 to obtain intermediate 3. Alternatively, Cbz-Phe-OH can also be used in the initial peptide coupling step to obtain 3. Boc-deprotection is usually achieved by reacting 3 with HCl in 4N dioxane (using DCM as solvent), while Cbz-deprotection is achieved by hydrogenation in MeOH with a Pd / C catalyst to obtain the amine intermediate Body 4. Reductive amination of free amine 4 with aldehyde 5 in MeOH at re...

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PUM

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Abstract

The invention relates to piperazine derivatives of Formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.

Description

technical field [0001] The present invention relates to a novel compound of formula I. The present invention also relates to related aspects, which include processes for the preparation of these compounds, pharmaceutical compositions containing one or more compounds of formula I and especially as a method for the treatment or prevention of malaria infection or the treatment or prevention of other protozoal diseases (such as sleeping sickness, South American Use of a medicament for Chagas disease, Amoeba, Piroplasmosis, Trichomoniasis, Toxoplasmosis, Leishmaniasis. Background technique [0002] Many serious diseases affecting humans and domestic and livestock animals are caused by protozoal organisms (e.g., kinetoplastida, apicomplexa, anaerobic protozoa, microsporidia and Caused by Plasmodium. The most clinically relevant of these diseases is malaria. [0003] Malaria is the most serious and complex health problem affecting humanity in the 21st century. The disease affec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/56C07D213/64C07D295/185A61K31/495A61K31/496A61P33/02A61P33/06
CPCC07D213/56C07D213/64C07D295/185A61P33/00A61P33/02A61P33/06A61P43/00Y02A50/30C07D403/12C07D403/14A61K31/496
Inventor 哈米德·艾萨维克里斯托夫·博斯奥利弗·科尔米伯夫比比安·海德曼罗曼·西格里斯特
Owner IDORSIA PHARM LTD
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