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Novel compositions magnetic particles covered with gem-bisphosphonate derivatives

A technology of magnetic particles and compositions, which is applied in the direction of drug combinations, compounds of Group 5/15 elements of the periodic table, nano-medicines, etc., and can solve problems such as difficult control of annexin grafting

Inactive Publication Date: 2006-03-08
GUERBET SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0023] Finally, annexin grafting is difficult to control

Method used

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  • Novel compositions magnetic particles covered with gem-bisphosphonate derivatives
  • Novel compositions magnetic particles covered with gem-bisphosphonate derivatives
  • Novel compositions magnetic particles covered with gem-bisphosphonate derivatives

Examples

Experimental program
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Effect test

preparation example Construction

[0335] Preparation method of particles

[0336] According to another aspect of the present invention, the object of the present invention is a method for preparing acidic magnetic particles (p), in which at least 90% of the protonation sites are covered by one or several geminal diphosphonic acids of the same or different general formula (1). The ester compound is complexed, and the group X may be coupled with at least one biological vehicle. The method includes contacting an acidic solution of iron compound-based acidic magnetic particles (p) with a sufficient amount of a compound of the general formula (1) as described above, The resulting complex particles are recovered.

[0337] According to another aspect of the present invention, the target is a preparation method of a magnetic nano-scale particle composition complexed by compound (1) and covered with a biological medium, which successively includes the following steps:

[0338] i) contacting an acidic solution of acidic ma...

Embodiment 1

[0463] Example 1: Preparation of compound A:

[0464]

[0465] 1) Diethyl-1-[ethoxyphosphoryl] vinyl phosphonate

[0466] Under heating conditions, 13g (0.433mol) of paraformaldehyde and 10mL (0.097mol) of diethylamine were dissolved in 250mL of methanol. Then add 24g (8.67×10 -2 mol) Diethyl[ethoxy(propyl)phosphoryl]methylphosphonate. The mixture was refluxed for 24h. The reaction medium is concentrated under vacuum. The concentrate was treated twice with 250 mL of toluene and then concentrated under vacuum.

[0467] The obtained oil was dissolved in 125 mL of toluene. Add 0.14 g of p-toluenesulfinic acid. The mixture was refluxed for 24 h with a Dean-Stark trap, and then concentrated to dryness under vacuum.

[0468] The product was extracted with 500 mL of dichloromethane and then washed twice with 250 mL of water. Use MgSO 4 The organic phase was dried and concentrated under vacuum.

[0469] The crude product was purified on 625 g Merck Geduran silica gel (40-63 μm). Elutio...

Embodiment 2～7

[0488] Examples 2-7: Preparation of biological media

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Abstract

The invention relates to a composition comprising acid magnetic particles (p) based on an iron compound, the acid magnetic particles (p) being complexed by one or more gem-bisphosphonate compounds, of formula I X-L-CH(PO3H2)2 (I) in which L represents an organic group connecting the X group to the gem-bisphosphonate group -CH(PO3H2)2; X represents a chemical group capable of reacting with a biovector; all or some of the X groups of the particles optionally being coupled to a biovector. The invention relates also to a process for the preparation of the compositions and their use, in particular as contrast products for Magnetic Resonance Imaging (MRI).

Description

Technical field [0001] The present invention relates to a magnetic particle composition covered by a molecule. On the one hand, this molecule contains a geminal bisphosphonate group bonded to the surface of the particle, and on the other hand, it contains a covalent bond with a so-called biological vehicle. The active group bound to the target entity. The invention also relates to its preparation method and its use, especially its use as a contrast compound for MRI. Background technique [0002] MRI can observe the internal organs of living organisms, so it becomes a powerful guide and assistant in diagnosis, treatment and surgery. [0003] The use of contrast compounds helps to improve the resolution of images obtained by this technique and the accuracy of diagnosis. [0004] Therefore, when there are various magnetic fragments, such as paramagnetic, ferromagnetic or superparamagnetic fragments, in the environment of the organ to be tested, this contrast effect can be enhanced. ...

Claims

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Application Information

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IPC IPC(8): A61K49/18C07F9/38A61P9/00A61P29/00A61P35/00
CPCB82Y5/00A61K49/1842A61P29/00A61P35/00A61P9/00
Inventor M·波尔C·科罗I·雷纳尔O·卢梭
Owner GUERBET SA
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