A61K49/101

LUMINESCENT PARTICLES BASED ON RARE EARTH ELEMENTS AND USE THEREOF AS A DIAGNOSTIC AGENT

The present invention concerns a luminescent particle comprising a nanoparticle of formula


A.sub.1xLn.sub.xVO.sub.4(1y)(PO.sub.4).sub.y (I)

in which A is selected from yttrium (Y), gadolinium (Gd), lanthanum (La), and mixtures thereof; Ln is selected from europium (Eu), dysprosium (Dy), samarium (Sm), neodymium (Nd), erbium (Er), ytterbium (Yb), and mixtures thereof; 0<x<1; and 0<y<1; characterized in that the nanoparticle on its surface has tetraalkylammonium cations in an amount such that said nanoparticle has a zeta potential, , of less than or equal to 28 mV in an aqueous medium with a pH5, more particularly with a pH5.5, and with an ionic conductivity >100 S.cm.sup.1.

It also concerns a method for preparing such luminescent particles, a colloidal suspension of these particles, and the use thereof as a diagnostic agent, and also a diagnostic kit comprising such luminescent particles.

Solvent-free gadolinium contrast agents

Disclosed herein are complexes of gadolinium metal, ligand and meglumine that are substantially free of non-aqueous solvents. In particular, solvent-free complexes of 1) gadopentetate dimeglumine and 2) gadoterate meglumine are disclosed and methods of their preparation are disclosed. In addition, methods are disclosed for purifying reactants, monitoring and controlling pH, quantifying the free gadolinium content, quantifying the concentration of gadolinium-ligand complex in aqueous solution, and procedures for producing a drug product in one step. The one step process eliminates the need to dry the gadolinium-ligand complex, which is typically highly hygroscopic. The one step process includes purification steps that do not require the use of non-aqueous solvents.

NITROGEN-CONTAINING MACROCYCLIC CONJUGATES AS RADIOPHARMACEUTICALS

The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

PREPARATION OF A SOLID FORM OF GADOBENATE DIMEGLUMINE

The present invention relates to a process for the preparation of a solid form of the gadobenate dimeglumine compound that comprises obtaining a solution of the said compound in a suitable solvent A wherein the amount by weight of the water optionally present in the solution is at most equal to or lower than the amount by weight of the gadobenate dimeglumine comprised in the solution and adding the obtained solution to an organic solvent B, acting as an appropriate antisolvent and favoring the formation of a solid form of the gadobenate dimeglumine that can be collected by filtration.

SYSTEM AND METHOD FOR DYNAMIC MULTIPLE CONTRAST ENHANCED, MAGNETIC RESONANCE FINGERPRINTING (DMCE-MRF)

The present disclosure provides a method of DDCE-MRF. The method can include: a) introducing two or more contrast agents to a region of interest (ROI) of a subject, the two or more contrast agents having different relaxivities; b) measuring a T1 relaxation time and a T2 relaxation time for locations within the ROI using magnetic resonance fingerprinting (MRF); c) determining, using equations that relate the different relaxivities, the T1 relaxation time, the T2 relaxation time, and concentrations of the two or more contrast agents, the concentrations of the two or more contrast agents for each of the locations within the ROI; and d) producing an image depicting the ROI based, at least in part, on the concentrations of the two or more contrast agents.

Nitrogen-containing macrocyclic conjugates as radiopharmaceuticals

The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

FORMATION AND USES OF EUROPIUM
20200023082 · 2020-01-23 ·

An MRI contrast composition includes a liposome and a europium metal complex disposed within the liposome. The europium metal complex includes a europium metal ion and a multi-dentate ligand selected from the group consisting of cryptands and thiacryptands and one or more counter-ions that balances a charge of the europium metal ion and the multi-dentate ligand, the europium metal ion being switchable between a 2+ and 3+ oxidation state. The contrast composition advantageously provides an oxidation-responsive dual-mode contrast agent because it would enhance either T.sub.1-weighted images or CEST images depending on the oxidation state of Eu.

MELANOCORTIN 1 RECEPTOR LIGANDS AND METHODS OF USE

The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.

Nitrogen-containing macrocyclic conjugates as radiopharmaceuticals

The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

SOLVENT-FREE GADOLINIUM CONTRAST AGENTS
20190365933 · 2019-12-05 ·

Disclosed herein are complexes of gadolinium metal, ligand and meglumine that are substantially free of non-aqueous solvents. In particular, solvent-free complexes of 1) gadopentetate dimeglumine and 2) gadoterate meglumine are disclosed and methods of their preparation are disclosed. In addition, methods are disclosed for purifying reactants, monitoring and controlling pH, quantifying the free gadolinium content, quantifying the concentration of gadolinium-ligand complex in aqueous solution, and procedures for producing a drug product in one step. The one step process eliminates the need to dry the gadolinium-ligand complex, which is typically highly hygroscopic. The one step process includes purification steps that do not require the use of non-aqueous solvents.