Guerbet S.a.

Guerbet

Wake Forest University

Boron Biologicals, Inc.

Guerbert S.a.

Dominique Meyer

Bruno Bonnemain

Michel Schaefer

Christian Simonot

Olivier Rousseaux

Didier Doucet

Marc Port

Dominique Paris

Claire Corot

Soizic Le Greneur

Gael Le Lem

Vincent Barbotin

Maryse Dugast-Zrihen

Bernard F Spielvogel

Jean Lautrou

Myriam Petta

Susan C Jackels

Fatima Z Bennani

Catherine Chambon

Jean-Maxime Nigretto

Michel Guillemot

Anne Bouillot

Nichel Schaefer

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 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.

Metal chelates of substituted polyaminocarboxylic macrocycles and their use in diagnostic imaging

Poly(amino acid) derivatives, which are chelating agents of paramagnetic metal ions, in which at least 3 of the donor nitrogen atoms carry identical or different substituents, of formula

Polyaminated ligands and metal complexes thereof

Iodinated polymers, processes for preparing them and their applications

Metal complexes of polyamino oxides, and their utilization in diagnostic

Biological or synthetic macromolecular polyamine compound. optionally of the dendrimer type, characterized in that it carries at least three radio-opaque iodine-containing derivatives.

Macromolecular polyamine iodine-containing compound, process for its

Polyiodo compounds, their preparation and their use in X-ray radiology

Polyiodinated compounds, their preparation and their use as contrast

Iodinated derivatives, their preparation and their use as contrast

A compound of the following formula II ##STR1## in which R.sub.7, R.sub.8, R'.sub.7, R'.sub.8, collectively, contain 10-24 hydroxyl groups and are selected, independently, from H, (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.10)alkyl substituted with one or more radicals selected from hydroxyl groups, (C.sub.1 -C.sub.3)alkoxy groups and hydroxylated (C.sub.1 -C.sub.3)alkoxy groups, is useful as a contrast agent in diagnostic X-Ray radiography.

Polyiodinated compounds, process for preparing them and diagnostic

The invention relates to ligands having the formula (I), in which X represents a heterocyclic group, together with the process for their preparation. The invention also concerns mono- or polymetallic complexes formed by said ligands with metallic ions selected from lanthanide ions, transition metal ions, barium ion, bismuth ion, lead ion and the radioisotopes 99m.sub.Tc, 111.sub.In, 90.sub.Y, 64.sub.Cu and 169.sub.Yb, as well as salts physiologically acceptable to these complexes. The salts of said complexes can be used as diagnostic and therapeutic agents in magnetic resonance imaging, radiology, in vivo chemical displacement agents and in nuclear medicine.

Diagnostic compositions comprising a complex formed by a nitrogenous

Polyiodinated compounds, process of preparation and contrast agent

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Saint-Maur, France

Dominique Meyer