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Antimalarial and anti-babesiosis agent and pharmaceutical compositions contg. same

A composition and medicine technology, applied in the application field in the preparation of antimalarial medicines, can solve the problems of increased cost, indecision in treatment and the like

Inactive Publication Date: 2007-09-19
沃贝克股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In-dwelling treatments with insecticides have many disadvantages (resistance, hesitation or increased cost of these treatments, no effect in grasslands) and practically effective pyrethroid-impregnated nets have certain drawbacks in use

Method used

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  • Antimalarial and anti-babesiosis agent and pharmaceutical compositions contg. same
  • Antimalarial and anti-babesiosis agent and pharmaceutical compositions contg. same
  • Antimalarial and anti-babesiosis agent and pharmaceutical compositions contg. same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] Example 1: N,N'-dimethyl-N,N'-diethyl-N,N'-dipropyl-1,14-tetradecanediammonium, dibromide

[0093] 35.6 g (0.1 mol) of 1,14-dibromotetradecane and 11.1 g of N-ethyl-N-methyl-1-propylamine were added to 200 ml of ethanol. Reflux for 8 hours until the reaction is complete, followed by thin-layer chromatography on silica gel plates in a solvent system such as propanol / pyridine / acetic acid / water. The solution was then evaporated and the residue was recrystallized from an isopropanol / ethyl acetate mixture. The title derivative is obtained in the form of crystals, m.p. = 185 / 190°C.

[0094] No commercially available α-ω dibromo derivatives can be synthesized from lower dibromoalkane derivatives with 4 carbon atoms by malonic acid synthesis. As an example, the synthesis of 1,14-dibromotetradecane (a, b, c and d) from dibromodecane will be described below:

[0095] a) Synthesis of ethyl 2,13-diethoxycarbonyl-1,14-tetradecanedioate

[0096] 1 gram atom of sodium (23 g) was d...

Embodiment 2

[0104] Example 2: N,N'-dimethyl-N,N'-diethyl-N,N'-dipropyl-1,15-pentadecanediammonium, dibromide, m.p.=230°C.

Embodiment 3

[0105] Example 3: N,N'-dimethyl-N,N'-diethyl-N,N'-dipropyl-1,16-hexadecanediammonium, dibromide, m.p.=232°C.

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PUM

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Abstract

The invention concerns pharmaceutical compositions with antimalaria and antibabesiosis activity, the active substances of these compositions and their use for formulating antimalaria drugs.

Description

field of invention [0001] The present invention relates to pharmaceutical compositions with antimalarial activity and antibabesia activity, active components of these compositions and their use in the preparation of antimalarial drugs. Background of the invention [0002] Malaria remains the most important parasitic disease in the tropics. Due to practical environmental factors, the disease is one of the most powerful constraints on the development of vast areas. Any resident there who is infected with the disease multiple times a year (up to 1000 in the Congo) from birth to death is likely to survive due to immunity from the infection during the first 5 years of his life. It is during this period, especially between 6 months and 2 years, that the large number of deaths from malaria is difficult to estimate. [0003] Nearly two billion people, often the poorest (often the poorest), now live in areas of high incidence and are threatened by malaria; often helplessly, they su...

Claims

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Application Information

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IPC IPC(8): C07D295/02A61K31/14A61K31/40A61K31/445A61P33/02C07D295/12A61K31/4025A61K31/4545A61K31/5377A61P33/06C07C211/63C07C215/90C07C217/08C07D207/08C07D211/22C07D295/13
CPCC07D211/22C07D295/13C07C217/08A61K31/4025C07C211/63A61K31/4545C07C215/90C07D207/08A61K31/5377A61K31/40A61K31/14A61P33/02A61P33/06Y02A50/30
Inventor H·维尔M·卡拉斯M-L·安司林L·吉拉尔
Owner 沃贝克股份有限公司
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