A61K51/082

Method for labeling radioisotope radiolabeling compound and kit comprising the same for labeling radioisotope

The present disclosure relates to a method for labeling a radioisotope, a radiolabeling compound, a kit including the same, and a method for labeling a radioisotope, including: providing a diaminophenyl compound represented by Chemical Formula I below and including a biomolecule, a fluorescent dye or a nanoparticle compound bound thereto; and reacting the diaminophenyl compound and a radioisotope-labeled aldehyde compound represented by Chemical Formula II below at room temperature; and a related technology: ##STR00001## in Chemical Formula I, A is CH.sub.2 or O; a is 0 or an integer of 1 to 10; X is CH.sub.2 or —CONH—; Y is CH.sub.2 or ##STR00002##  and Z is the biomolecule, the fluorescent dye or the nanoparticle compound, ##STR00003## in Chemical Formula II, b is 0 or an integer of 1 to 10; and L is CH.sub.2 or —CONH—; and Q is ##STR00004## M, M′ and M″ in Q are radioisotopes.

SUBSTITUTED ORGANOFLUOROBORATES AS IMAGING AGENTS
20220062445 · 2022-03-03 ·

Fluoridated organofluoroborates comprising at least one .sup.18F atom and precursors thereto, for use in PET scanning.

METHOD FOR EXTRACTION AND PURIFICATION OF 68GA

Disclosed herein are methods preparing a purified, carrier-free 68Ga solution. Tire present disclosure also provides systems for preparing a purified, carrier-free 68Ga solution. The present disclosure also provides compositions comprising the purified, carrier-free 68Ga solutions disclosed herein. Also provided are methods of administering compositions of the present disclosure to a patient in need thereof, for example, for imaging a disease or disorder, such as cancer.

Radiofluorination method

The present invention relates to a method of labelling biological molecules with .sup.18F, via attachment to fluorine to a macrocyclic metal complex of a non-radioactive metal, where the metal complex is conjugated to the biological molecule. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.

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.

BI-TERMINAL PEGYLATED INTEGRIN-BINDING PEPTIDES AND METHODS OF USE THEREOF

The present invention provides bi-terminal PEGylated peptide conjugates that target an integrin such as α.sub.vβ.sub.6 integrin. In particular embodiments, the peptide conjugates of the present invention further comprise a biological agent such as an imaging agent or a therapeutic agent, e.g., covalently attached to one of the PEG moieties. The peptide conjugates of the present invention are particularly useful for imaging a tumor, organ, or tissue and for treating integrin-mediated diseases and disorders such as cancer, inflammatory diseases, autoimmune diseases, chronic fibrosis, chronic obstructive pulmonary disease (COPD), lung emphysema, and chronic wounding skin disease. Compositions and kits containing the peptide conjugates of the present invention find utility in a wide range of applications including, e.g., in vivo imaging and immunotherapy.

METHODS AND KITS FOR PREPARING RADIONUCLIDE COMPLEXES
20210138094 · 2021-05-13 ·

A method for preparing a complex comprising a radioisotope of gallium for use in radiotherapy or in a medical imaging procedure, said method comprising adding a gallium radioisotope solution obtained directly from a gallium radionuclide generator to a composition comprising a pharmaceutically acceptable buffer and optionally also a pharmaceutically acceptable basic reagent, in amounts sufficient to increase the pH to a level in the range of 3 to 8, wherein the composition further comprises a chelator that is able to chelate radioactive gallium within said pH range and at moderate temperature, said chelator being optionally linked to a biological targeting agent. Kits and compositions for use in the method are also described and claimed.

Chemical conjugates of Evans Blue derivatives and their use as radiotherapy and imaging agents

The present invention is directed to a compound of Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula III wherein the definitions of R.sub.1-R.sub.12 and L.sub.1-L.sub.4 are provided in the disclosure, wherein R.sub.13 is a chelating group comprising .sup.177Lu, and wherein R.sub.14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

RADIOPHARMACEUTICAL COMPOSITIONS
20210060189 · 2021-03-04 ·

The present invention relates to .sup.99mTc-maraciclatide radiopharmaceutical compositions, which are stabilised with a radioprotectant. Also described are kits for the preparation of the radiopharmaceutical compositions, as well as methods of preparing such compositions from the kit. The invention also includes methods of imaging the mammalian body using the radiopharmaceutical compositions.

Modified cyclopentapeptides and uses thereof

The present invention, among others, relates to a compound having a structure according to formula (I) or a pharmaceutically acceptable salt thereof, wherein Xaa.sup.1 are the iodo-substituted or methyl-substituted amino acids D- and L-Tyr, iodo-substituted or methyl- substituted D- and L-homotyrosine, iodo-substituted or methyl-substituted D- and L-Phe, iodo-substituted or methyl-substituted D- and L-p-OH-phenylglycine, and iodo-substituted or methyl-substituted D- or L-Trp, Xaa.sup.2 to Xaa.sup.4 are independently of each other, an optionally N-alkylated natural or unnatural amino acid, R is H or methyl, L is a linker moiety, Ar is a spacer comprising an aromatic moiety, and D comprises, preferably is i) a combination of an organic complexation agent and a radioactive or a detectable label; or ii) a radioactive or a detectable label, an organic complexation agent or an active substance, said active substance particularly being selected from cytotoxic agents, lipids, sugars, sugar conjugates, sugar derivatives, proteins and combinations thereof.