A61K51/0491

RADIOLABELED MOEM TYPE OLIGONUCLEOTIDES AND PROCESS FOR THEIR PREPARATION

The invention comprises radiolabeled MOEM type oligonucleotide of the formula (I), (I) wherein n, X.sup.1, X.sup.2, the linker (1), the linker (2), Q* and the receptor targeting moiety are as defined (I) the description. The radiolabeled oligonucleotides of the formula (I) can be used for the determination of the biodistribution and pharmacokinetics of the oligonucleotide in the tissue or body fluid.

##STR00001##

Positron Emission Tomography Guided Delivery of Mitochondral Complex I Inhibitors
20220347323 · 2022-11-03 ·

A method for detecting or ruling out non-small cell lung cancer (NS-CLC) in a patient comprises: (a) administering to a patient a detectable amount of a compound of formula (I): Formula (I) wherein the compound is targeted to any NSCLC tumor in the patient; and (b) acquiring an image to detect the presence or absence of any NSCLC tumor in the patient, wherein at least one of the atoms in formula (I) is replaced with .sup.11C, .sup.13N, .sup.15O, .sup.18F, .sup.34mCI, .sup.38K, .sup.45Ti, .sup.51Mn, .sup.52Mn, .sup.52Fe, .sup.55Co, .sup.60CU, .sup.61Cu, .sup.62Cu, .sup.64Cu, .sup.66Ga, .sup.68Ga, .sup.71As, .sup.72As, .sup.74As, .sup.75Br, .sup.75Br, .sup.76Br, .sup.82Rb, .sup.86Y, .sup.89Zr, .sup.90Nb, .sup.94mTc, .sup.110mIn, .sup.118Sb, .sup.120I, .sup.121I, .sup.122I, and .sup.124I.

##STR00001##

NANOPARTICLES FOR USE IN THE TREATMENT AND DIAGNOSIS OF CNS DISORDERS
20230090223 · 2023-03-23 ·

A nanoparticle comprising chemically modified heparin, wherein the heparin has been chemically modified by attaching hydrophobic moieties to functional groups of the heparin, said functional groups being selected from hydroxy groups and carboxy groups, for use in the treatment or diagnosis of a brain disorder.

PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) LIGANDS COMPRISING AN AMYLASE CLEAVABLE LINKER

In particular, the present invention relates to a PSMA binding ligand comprising an oligosaccharide building block which comprises a bond being cleavable by alpha-amylase.

Typically, this PSMA binding ligand further comprises a PSMA binding motif Q and a chelator residue A, wherein the PSMA binding motif Q and the chelator residue A are preferably linked via at least one linker L.sup.AQ comprising the oligosaccharide building block, the PSMA binding ligand thus preferably having the structure (I)


A-L.sup.AQ-Q

or a pharmaceutically acceptable salt or solvate thereof.

.SUP.99m.Tc-labeled isonitrile-containing glucose derivative and preparation method and use thereof

A .sup.99mTc-labeled isonitrile-containing glucose derivative having the general formula [.sup.99mTc-(CNDG).sub.6].sup.+, preparation method and use thereof is disclosed herein. The derivative is centered on .sup.99mTc.sup.+, and the carbon atom of the isonitrile in CNDG coordinates with .sup.99mTc(I) to form a hexacoordinated complex [.sup.99mTc-(CNDG).sub.6].sup.+. The [.sup.99mTc-(CNDG).sub.6].sup.+ derivative was obtained by the synthesis of the ligand CNDG and the preparation of the lyophilized CNDG kit. The derivative of this disclosure has good stability, simple preparation, high uptake and good retention at a tumor site, and high tumor/non-target ratio, and it is a novel .sup.99mTc-labeled isonitrile-containing glucose derivative with excellent performance for tumor imaging. The derivative of this disclosure is advantageous for popularization and application.

PSMA-binding agents and uses thereof

The present invention provides novel compounds that are useful as radiopharmaceuticals, imaging agents and for treatment of cancer.

SYSTEMS AND METHODS FOR IMAGE RECONSTRUCTION
20230069017 · 2023-03-02 · ·

The present disclosure is related to systems and methods for image reconstruction. The method may include obtaining at least one positron emission tomography (PET) image of a subject. The at least one PET image may be generated based on PET data acquired during an examination period. In the examination period, the subject may be injected with a tracer. The method may also include determining, based on the at least one PET image, an input function that reflects a concentration change of the tracer in the subject during the examination period. The method may further include generating a parametric image based on the input function and the at least one PET image according to a non-linear parametric estimation algorithm. The parametric image may reflect a kinetic parameter of the tracer in the subject.

Deuterium-Stabilised Ribonucleic Acid (RNA) Molecules Displaying Increased Resistance to Thermal and Enzymatic Hydrolysis, Aqueous Compositions Comprising Stabilised RNA Molecules and Methods for Making Same
20230109802 · 2023-04-13 · ·

The invention relates to the field of RNA stabilisation, and more particularly to the use of deuterium oxide (D.sub.2O) during storage and/or synthesis of RNA molecules. Described herein are deuterium-stabilised ribonucleic acid (RNA) molecules that display an increased resistance to thermal and enzymatic hydrolysis. Also described are aqueous compositions comprising stabilized RNA molecules and methods for making same. The invention is particularly useful for in the manufacture of RNA-based therapeutics, such as mRNA vaccines, to render them less sensitive to temperature fluctuations.

Modified peptide nucleic acid compositions

The present disclosure relates to compounds useful for the detection or modulation of target nucleic acids, including DNA and RNA. The present disclosure further relates to methods for treatment of trinucleotide repeat disorders, which can include administration of oligonucleotide analogues that can bind pathogenic nucleotide repeats in DNA or RNA.

THERANOSTIC SYSTEM FOR DIRECTED DIFFUSION OF THERAPEUTIC AND IMAGING AGENTS TO CANCER CELLS
20230144838 · 2023-05-11 ·

The invention relates to a multifunctional system stable in a physiological medium, which includes in the same platform an anti-carcinogenic molecule, an imaging agent and a directing molecule that interacts specifically with cancer-cell membrane receptors, the system allowing pathological tissue imaging and pharmacological action to be carried out jointly with high specificity. The intratumoral administration of the system facilitates selective diffusion to cancer cells and minimises the disadvantages of chemotherapy.