A61K49/106

COMPLEX OF GADOLINIUM AND A CHELATING LIGAND DERIVED OF A DIASTEREOISOMERICALLY ENRICHED PCTA AND SYNTHESIS METHOD

The present invention relates to a complex of formula (II) constituted of at least 80% of a diastereoisomeric excess comprising a mixture of isomers II-RRR and II-SSS of formulae:

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The present invention also relates to a process for preparing said complex of formula (II), and also to two synthetic intermediates.

FORMULATION OF CONTRAST MEDIA AND PROCESS OF PREPARATION THEREOF

The present disclosure relates to a liquid pharmaceutical formulation comprising a DOSA-derived tetra-chelate of formula (I), in which M is an ion of a paramagnetic metal, preferably a Gd.sup.3+ ion, and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the claims, in a pharmaceutical acceptable solvent. The present disclosure also relates to a method of preparation of said liquid pharmaceutical formulation and to a method of imaging involving said liquid pharmaceutical formulation.

Formation and uses of europium
11185599 · 2021-11-30 · ·

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.

Metal complex formulations

The present invention relates to a method of preparation of formulations of lanthanide metal complexes of macrocyclic chelators which further comprise a small excess of free chelator. The method uses a solid phase-bound scavenger chelator to remove excess lanthanide metal ions, prior to the addition of a defined excess chelator. Also provided is a method of preparation of MRI contrast agents, together with solid-phase bound chelator meglumine salts useful in the methods.

Imaging Agents

This invention relates to compounds of formula I or Ia: (I) (Ia). Y is EuK, —EuAF, —EuPG, -L-EuE; Z is a chelating moiety; and the other substituents are as defined herein. Also provided are formulations comprising such a compound, as well as methods of imaging or methods for the treatment of cancer comprising use of such a compound or formulation.

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Nanoparticles

The invention provides a (drug-containing) lipid nanoparticle with: (i) at least one phospholipid; (ii) at least one lysolipid; and (iii) at least one phospholipid comprising a hydrophilic polymer; and (iv) at least one structural lipid of formula (I) which has the following general structure: ##STR00001## wherein R and R′ are long hydrocarbyl hydrophobic chains, Y is a linker element, and PHG is a polar head group described as large according to its van der Waals radius, and which is different from the phospholipid (i). The lipid nanoparticle can release a drug (or API) from within the lipid nanoparticle as a result of focused ultrasound (FUS) applied continuously, at least twice, to a desired part of the body to induce hyperthermia (an increase in temperature). FUS is applied after the lipid nanoparticle containing the drug has been administered to the live subject, and causes controlled release of the drug at the desired site of the body. Ultrasound is then halted, and the site of interest allowed to cool. Ultrasound is then applied again. Lipid nanoparticles can be labelled (for MRI, NIRF imaging), enabling real time monitoring of the drug in the human body. Imaging information can be used to direct and guide the nature of the FUS applied to the site of interest.

Modified biotin, streptavidin mutant, and usage of them

An object of this invention is to provide a streptavidin mutant reduced in affinity to the naturally-occurring biotin, and to provide a modified biotin which shows a high affinity to such streptavidin mutant reduced in affinity to the naturally-occurring biotin. This invention can provide a compound composed of a dimer of modified biotin, a streptavidin mutant, angsd usage of them.

METHOD FOR MULTIMODAL TISSUE IMAGING BASED ON RESONANCE RAMAN EFFECT ON METAL BASED MRI CONTRAST AGENTS AND METHOD FOR IONIZING LASER PLUMES THROUGH ATMOSPHERIC PRESSURE CHEMICAL IONIZATION
20230329558 · 2023-10-19 ·

Disclosed herein is a method for multimodal imaging during a medical procedure using magnetic resonance imaging (MRI) and Raman optical imaging which involves administering an MRI imaging contrast agent that a chemical structure having charge-transfer electronic transitions. The tissue is imaged using and MRI device and the tissue is illuminated with excitation light that has spectral components that are approximately tuned close to one of the charge-transfer electronic transitions thereby producing enhanced Raman optical signals which are analyzed to produce Raman imaging data followed by registering the MRI and Raman imaging data. The present disclosure also provides a method for ionizing laser plumes through atmospheric pressure chemical ionization.

FORMULATIONS AND KITS FOR RADIOTHERAPY AND DIAGNOSTIC IMAGING
20230330276 · 2023-10-19 ·

Aqueous formulations and kits of radiopharmaceutical compounds of general Formula (II) protected from radiolysis with stabilisers, such as L-methionine and gentisic acid, are disclosed, wherein the compounds are based on sarcophagine ligands coordinated to a radioisotope, such as 64-copper, and linked to a tetrazine group for reaction with tumour targeting antibodies having functional reactive groups such as trans-cyclooctene, processes of preparing said radioligand formulations, and uses thereof for radioimaging, diagnosing and treating cancer.

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COMPOUND AND MRI CONTRAST AGENT CONTAINING SAME
20230330272 · 2023-10-19 ·

The present invention relates to a novel compound and an MRI contrast agent containing same. The compound according to the present invention can minimize MRI contrast agent side effects caused by the release of gadolinium ions within the body, on the basis of the outstanding kinetic stability, and can be very usefully employed as an MRI contrast agent for diagnosing liver diseases, owing to the superior level of contrast enhancement for the liver in an MRI image of the body in comparison with other organs.