S1P receptor agonists for the treatement of cerebral malaria

A technology of receptor agonists and uses, applied in the direction of antibodies, anti-toxins, anti-inflammatory agents, etc., can solve problems such as no future for treatment

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

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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 receptor agonists for the treatement of cerebral malaria
  • S1P receptor agonists for the treatement of cerebral malaria
  • S1P receptor agonists for the treatement of cerebral malaria

Examples

Experimental program
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Embodiment

[0114] Aspects of the invention can be understood from the following examples, which are not intended to limit the scope of the invention.

[0115] Measuring S1P receptor binding affinity

[0116] The binding affinity of an S1P receptor agonist for an individual human S1P receptor can be determined using well known assays. For example, the human S1P receptor S1P can be used 1 , S1P 2 , S1P 3 , S1P 4 and S1P 5 , by quantifying the induction of GTP [γ- 35 S] to test compounds. A suitable assay technique is SPA (scintillation proximity based assay). Briefly, compounds dissolved in DMSO were serially diluted and prepared in 50 mM Hepes, 100 mM NaCl, 10 mM MgCl 2 , 10μM GDP, 0.1% defatted BSA and 0.2nM GTP[γ- 35 S1P receptor expressing membrane protein (10-20 μg / well) immobilized with SPA-beads (Amersham-Pharmacia) in the presence of S] 1200 Ci / mmol). Unbound GTP[γ- 35 S]. Quantification of membrane-bound GTP [γ- 35 S] Fluorescence induced by SPA beads. Calculate EC u...

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Abstract

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

Description

[0001] This application claims priority to US Provisional Application 61 / 109,991, filed October 31, 2008, and US Provisional Application 61 / 229,970, filed July 30, 2009, the entire contents of which are incorporated herein by reference. 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 approximat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P33/06A61K45/06A61K31/13
CPCA61K39/395A61K31/13A61K9/7061A61K9/0014A61K45/06A61P13/00A61P25/08A61P29/00A61P33/06A61P39/06A61P43/00Y02A50/30A61K2300/00
Inventor 马科斯·巴拉赫康斯坦斯·安·马乔里·芬尼凯文·查尔斯·凯恩塔马斯·奥拉韦茨
Owner LEXICON PHARM INC
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