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Sphingosine-1 -phosphate receptor agonist and antagonist compounds

A compound, C1-C20 technology, applied in animal repellents, biocides, plant growth regulators, etc., can solve problems such as separation and identification limitations

Inactive Publication Date: 2009-12-23
ABBOTT LAB INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Isolation and identification of S1P analogs with potent agonist or antagonist activity at S1P receptors has been limited

Method used

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  • Sphingosine-1 -phosphate receptor agonist and antagonist compounds
  • Sphingosine-1 -phosphate receptor agonist and antagonist compounds
  • Sphingosine-1 -phosphate receptor agonist and antagonist compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0442] Compounds of the present invention were synthesized and their activities were assayed as described below.

[0443] S1P receptor GTPγS assay

[0444] Performed with scintillation proximity assay (SPA) and filter method[ 35 S] GTPyS binding assay. Both methods are advantageously performed in 96-well plates using overexpressed S1P 1 , S1P 2 , S1P 3 , S1P 4 or S1P 5 Membranes of Stable or Transient CHO Human Cell Lines. Compound stocks were prepared at 10 mM in DMSO and serially diluted in 100% DMSO. Compounds were transferred into 96-well plates to give a final concentration of 1% DMSO for all assays (1 ul for 100 ul assay volume). Frozen membranes were thawed and diluted in assay buffer containing 20 mM HEPES pH 7.4, 0.1% fatty acid free BSA, 100 mM NaCl, 5 mM MgCl 2 and 10 μM GDP. For the SPA assay, the membrane was premixed with WGA-SPA beads to give a final concentration of 5ug membrane and 500ug beads per well. For filtration assays, membranes were added di...

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PUM

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Abstract

The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of US Provisional Application Serial No. 60 / 876,288, filed December 21, 2006, and US Provisional Application Serial No. 60 / 876,318, filed December 21, 2006, the contents of which are incorporated herein. Background of the invention [0003] Sphingosine-1-phosphate (S1P) is part of the sphingomyelin biosynthesis pathway and is known to affect a variety of biological processes. S1P is formed by phosphorylation of sphingosine by sphingosine kinases (SK1 and SK2), and is degraded by cleavage of sphingosine lyase to form palmaldehyde and phosphoethanolamine or dephosphorylated by phospholipid phosphatase. It occurs at high levels (~500nM) in serum and can be found in most tissues. It is synthesized by a variety of cells in response to several stimuli, including cytokines, growth factors, and G protein-coupled receptor (GPCR) ligands. The GPCR that binds S1P (currently known as the S1P re...

Claims

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Application Information

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IPC IPC(8): A01N43/50A61K31/415
CPCY02A50/30
Inventor G·A·华勒斯E·C·布尔格K·P·库赛克S·R·菲斯-史坦塞尔T·D·高登A·D·何伯森M·E·海斯G·K·安塞尔P·葛隆沙德
Owner ABBOTT LAB INC
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