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Imaging the central nervous system

A central nervous system and in vivo imaging agent technology, applied in the field of purine P2 receptors, can solve the problem of not describing isotopic variants

Inactive Publication Date: 2013-11-20
GE HEALTHCARE LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

these contain 11 C. 18 F. 15 O and 13 Isotopic variants of N have been mentioned to be useful for PET studies of substrate receptor occupancy, although WO2007 / 109154 or WO 2007 / 109192 do not describe how to obtain these isotopic variants

Method used

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  • Imaging the central nervous system
  • Imaging the central nervous system
  • Imaging the central nervous system

Examples

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example

[0108]

[0109]

[0110] Non-radioactive forms of the imaging agents shown in Table I are available in P2X 7 Screening was performed in a receptor function assay. This assay is described in Example 9 and is based on the P2X 7 receptors in P2X 7 Transfected HEK.293 cells rely on the ability of agonists to activate, allowing the dye to penetrate cells to form non-selective pores. A non-selective P2X channel antagonist used as a reference inhibitor for the evaluation of non-radioactive compounds of the invention is pyridoxal-phospho-6-azophenyl-2',4'-disulfonic acid (PPADS), and The assay results are provided in Table I above. A non-radioactive form of the imaging agent of the invention was found to inhibit P2X at 10 μM 7 Function, and generally at a concentration of 100 nM to a similar extent compared to PPADS (reference compound).

[0111] Synthetic routes for obtaining the imaging agents shown in Table I, together with their non-radioactive equivalents, are provided...

Embodiment 9

[0151] Example 9 describes methods for assessing binding P2X 7 Determination of receptors.

[0152] Abbreviations used in the examples

[0153]

Embodiment 1

[0155] Example 1: Synthesis of Non-Radioactive Imaging Agent 2

[0156]

[0157] 3(i) 2-((4-bromophenoxy)methyl)oxirane (5)

[0158] Into an oven-dried round-bottomed 2-neck flask, 4-bromophenol (15 g 86.7 mmol) was added. Potassium carbonate (14.3 g, 1.2 eqv (equivalent)) was added, and the mixture was stirred at room temperature for 10 minutes. Epichlorohydrin (39.8 g, 430 mmol) was added, and the mixture was heated at 120°C for 3 hours. The reaction mass was concentrated under reduced pressure to remove excess epichlorohydrin. Water (100 mL) was added to the reaction mass and extracted with ethyl acetate (4x50 mL). The combined organic layers were dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The crude residue was purified by column chromatography on silica gel using hexane and ethyl acetate as eluents to give the desired product (13.6 g, 69% yield).

[0159] 1 H-NMR: (300MHz, CDCl 3 )δ7.40(d, 2H, J=9Hz), 6.83(d, 2H, J=...

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Abstract

The present invention provides novel compounds which may be used as in vivo imaging agents. The compounds of the invention are useful in a method to image the expression of P2X7 receptors in a subject, as a means to facilitate the diagnosis of a range of disease states.

Description

[0001] This application is a divisional application of the following applications: filing date: February 26, 2009; application number: 200980106791.3 (PCT / EP2009 / 052280); invention title: "imaging of the central nervous system". technical field [0002] The present invention relates to the field of purine P2 receptors. More specifically, the present invention relates to novel purine P2X 7 In vivo imaging agents of receptors, their production and their intermediates. In further detail, the present invention relates to the use of in vivo imaging agents of the present invention in providing for the diagnosis of 7 Use in a method for information of a disease state of receptor expression. Background technique [0003] P2X 7 Receptors are cation-selective ion channels gated directly by extracellular ATP, the only known physiological ligand, and a few pharmacological ATP analogs (North 2002 Physiol. Rev. 82: 1013-1067). ATP release from damaged cells and subsequent localization...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04G21C1/00
CPCA61K51/0455A61P25/00
Inventor P·A·琼斯I·威尔逊V·莫里森-艾夫森C·琼斯J·伍德克拉夫特A·杰克逊D·怀恩
Owner GE HEALTHCARE LTD
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