Guerbet

Universitë De Bordeaux

Université De Bordeaux 1

Marc Port

Claire Corot

Dominique Meyer

Olivier Rousseaux

Bruno Bonnemain

Vincent Barbotin

Thierry Gautheret

Christian Simonot

Caroline Robic

Fernando Leal Calderon

Anne Petit

Robert Muller

Carmen Burtea

Christelle Medina

Samy Chadel

Monique Sabatou

Isabelle Raynal

Irène Guilbert

Jean Sébastien Raynaud

The present invention relates to a liquid pharmaceutical composition including a complex of formula (I), in which M is an ion of a paramagnetic metal and R1 to R3, X1 to X3 and K1 to K12 are such as defined in claim, said composition also including a calcium complex of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid. The invention also relates to the preparation method thereof and to an imaging method involving said composition.

Contrast medium formulation and related preparation method

The invention relates to a process for preparing a liquid pharmaceutical formulation containing a complex of macrocyclic chelate with a lanthanide and a mol/mol amount of free macrocyclic chelate of between 0.002% and 0.4%, advantageously between 0.02% and 0.3% and very advantageously between 0.025% and 0.25%, the macrocyclic chelate advantageously being chosen from DOTA, NOTA, DOTAGA, D03A, BT-D03A, HP-D03A and PCTA, and is preferably DOTA, the said process comprising the following successive steps: b) preparation of a liquid pharmaceutical composition containing, firstly, the complex of macrocyclic chelate with a lanthanide, and, secondly, free macrocyclic chelate and/or free lanthanide; c) measurement in the pharmaceutical formulation obtained in step b) of the concentration of free macrocyclic chelate Cchl and/or of free lanthanide Ciani; d) adjustment of Cchl and/or of Ciani so as to obtain Cchl=Ct chi and Ciani=0, wherein Ct chi is the target concentration of free macrocyclic chelate in the final liquid pharmaceutical formulation.

Process for preparing a pharmaceutical formulation of contrast agents

The present invention relates to a method for preparing a pharmaceutical formulation of lanthanide chelate in powder form, wherein the powder constitutes a mol/mol excess of free chelate of between 0.002 and 0.4%.

Method for preparing a pharmaceutical formulation of lanthanide chelate in powder form

The present invention relates to an oil-in-water nanoemulsion composition for MRI, comprising:

Chelate nanoemulsion for MRI

The invention relates to a process for preparing a liquid pharmaceutical formulation containing a complex of macrocyclic chelate with a lanthanide and a mol/mol amount of free macrocyclic chelate of between 0.002% and 0.4%, advantageously between 0.02% and 0.3% and very advantageously between 0.025% and 0.25%, the macrocyclic chelate advantageously being chosen from DOTA, NOTA, DOTAGA, DO3A, BT-DO3A, HP-DO3A and PCTA, and is preferably DOTA, the said process comprising the following successive steps: b) preparation of a liquid pharmaceutical composition containing, firstly, the complex of macrocyclic chelate with a lanthanide, and, secondly, free macrocyclic chelate and/or free lanthanide; c) measurement in the pharmaceutical formulation obtained in step b) of the concentration of free macrocyclic chelate C ch1 and/or of free lanthanide C lan1; d) adjustment of C ch1 and/or of C lan1 so as to obtain C ch1=C tch1 and C lan1=0, wherein C t ch1 is the target concentration of free macrocyclic chelate in the final liquid pharmaceutical formulation.

The invention relates to a process for preparing a liquid pharmaceutical formulation containing a complex of macrocyclic chelate with a lanthanide and a mol/mol amount of free macrocyclic chelate of between 0.002% and 0.4%, advantageously between 0.02% and 0.3% and very advantageously between 0.025% and 0.25%, the macrocyclic chelate advantageously being chosen from DOTA, NOTA, DOTAGA, DO3A, BT-DO3A, HP-DO3A and PCTA, and is preferably DOTA, the said process comprising the following successive steps: b) preparation of a liquid pharmaceutical composition containing, firstly, the complex of macrocyclic chelate with a lanthanide, and, secondly, free macrocyclic chelate and/or free lanthanide; c) measurement in the pharmaceutical formulation obtained in step b) of the concentration of free macrocyclic chelate Cand/or of free lanthanide C; d) adjustment of Cand/or of Cso as to obtain C=Cand C=0, wherein Cis the target concentration of free macrocyclic chelate in the final liquid pharmaceutical formulation.

The present invention relates to a compound comprising, firstly a component for targeting at least one chemokine receptor and, secondly, a detection component capable of being identified by a medical imaging method.

Diagnostic compounds for targeting a chemokine receptors

The present invention concerns a Ga68 complex of formula FOLATE-(LINKER)i-NOTA-Gain which:

Complex folate-NOTA-Ga68

The invention concerns compounds comprising a biological target recognizing part, coupled to a signal part capable of complexing gallium. The invention also concerns methods for obtaining said compounds, screening methods capable of selecting such compounds for chemical synthesis thereof and their diagnostic applications, in particular in PET, PET/IRM, PET CT imaging.

Compounds comprising a biological target recognizing part, coupled to a signal part capable of complexing gallium

A novel method for preparing nanoparticles for medical imaging, including a metal core, an organic stabilizing layer containing gem-bisphosphonate compounds and at least one hydrophilic biodistribution ligand.

Method for preparing nanoparticles covered with a gem-bisphosphonate stabilizing layer coupled to hydrophilic distribution ligands

The present invention relates to a compound of the following general formula (I): Signal-Linker-Peptide (I) in which Signal is a signal entity; Linker, is absent or is a chemical bond, and Peptide is a peptide having a VCAM-targeting peptide and pharmaceutically acceptable salts thereof. The VCAM-targeting peptide may be X10-X11-X12-X13-X14-X15-X16-X17-X18 (SEQ ID No. 4) with X10 chosen from cysteine and methionine; X11 chosen from methionine and cysteine; X12 chosen from lysine, arginine and alanine; X13 chosen from threonine and serine; X14 chosen from aspartic acid and glutamic acid; X15 chosen from threonine and serine; X16 chosen from arginine, alanine and lysine; X17 chosen from leucine, isoleucine and valine; X18 chosen from cysteine and methionine; preferably, the peptide CMKTDTRLC (SEQ ID No. 5).

Compounds for the diagnosis of diseases associated with VCAM expression

The invention relates to chelate compounds which can be used in MRI, the chelates being intended to be conveyed by lipophilic transporters, such as lipid nanoparticles or liposomes. The invention also relates to compounds comprising, in association, these chelates and these transporters, if appropriate connected via chemical bonding groups, and to their use in diagnostic imaging, it being possible for this association additionally to comprise biological targeting markers, denoted biovectors.

Lipophilic chelates and their use in imaging

The present invention relates to a compound of formula (II) chosen from (IIa) and (IIb) or of formula (VI) chosen from (VIa) and (VIb) of following general formulae: in which: It also relates to a complex of these compounds with a paramagnetic metal or a radionuclide and their use in diagnostic methods.

Compounds comprising short aminoalcohol chains and metal complexes for medical imaging

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(POH)&#x2003;&#x2003;(I)in which:

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Deuil la Barre, France

Marc Port