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S1P lyase inhibitors for the treatment of cerebral malaria

A technology of lytic enzymes and inhibitors, applied in the field of treatment, compositions useful therefor, treatment and/or prevention of cerebral malaria, which can solve the problem of no future for treatment

Inactive Publication Date: 2011-09-21
LEXICON PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, many adjuvant treatments have been proposed, some of which are promising, but many of these treatments are not promising

Method used

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  • S1P lyase inhibitors for the treatment of cerebral malaria
  • S1P lyase inhibitors for the treatment of cerebral malaria
  • S1P lyase inhibitors for the treatment of cerebral malaria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0130] Various aspects of the present invention can be understood from the following examples, but are not limited to the scope of the following examples.

[0131] Synthesis of (E / Z)-1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)-ethanone oxime

[0132]

[0133] 1-[4-((1R,2S,3R)-1,2,3,4-tetrahydroxy-butyl)-1H-imidazol-2-yl]-ethanone (THI, according to Halweg, K.M. and Büchi , G., J. Org. Chem. 50:1134-1136 (prepared in 1985)) (350mg, 1.52mmol) was suspended in water (10ml). Hydroxylamine hydrochloride (126.8 mg, 1.82 mmol, 1.2 eq.) and sodium acetate (247.3 mg, 3.04 mmol. 2 eq.) were added, and the suspension was stirred at 50°C. The reaction mixture became clear after about 4 hours. Stirring was continued at 50°C for 16 hours. LCMS analysis showed product formation and the absence of starting material. The reaction mixture was brought to room temperature and passed through a fine mesh filter. This solution was used directly to purify the product by pr...

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Abstract

Methods and compositions for treating, managing, and / or preventing cerebral malaria are disclosed.

Description

[0001] This application claims priority to US Provisional Applications 61 / 109,982 and 61 / 109,987, filed October 31, 2008, which applications are hereby incorporated by reference in their entirety. technical field [0002] The present application relates to methods of treating, treating and / or preventing cerebral malaria, and compositions useful therefor. Background technique [0003] cerebral malaria [0004] Malaria kills more than two million people every year, most of them children in Africa. Golenser, J. et al., Int. J. Parasitology 36: 583-593, 583 (2006). Eradication of the disease "has been hampered by the evolution of Plasmodium parasites resistant to existing antimalarial drugs (particularly Plasmodium falciparum, which is the most abundant and dangerous disease-causing species). Ibid. forward. [0005] One of the most serious complications of P. falciparum infection is cerebral malaria (CM), which accounts for approximately 7% of P. falciparum malaria cases. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/417A61K45/06A61P33/06A61K31/422A61K31/4196A61K31/427
CPCA61K45/06A61K31/422A61K31/427A61K31/417A61K31/4196A61P13/00A61P25/04A61P25/08A61P29/00A61P33/06A61P39/06A61P43/00Y02A50/30A61K2300/00
Inventor 菲利普·曼顿·布朗康斯坦斯·安·马乔里·芬尼凯文·查尔斯·凯恩塔马斯·奥拉韦茨斯蒂芬·克里斯·帕帕斯
Owner LEXICON PHARM INC