A61K51/0455

POSITRON EMISSION TOMOGRAPHY RADIOTRACER FOR DISEASES ASSOCIATED WITH TRANSLOCATOR PROTEIN OVEREXPRESSION, TRANSLOCATOR PROTEIN-TARGETING LIGAND FOR FLUORESCENCE IMAGING-GUIDED SURGERY AND PHOTODYNAMIC THERAPY, AND PRODUCTION METHODS THEREFOR

Disclosed is a method for producing a fluorine-18-labeled, translocator protein overexpression-targeting PET radiotracer including: preparing a fluorine-18 reaction solution; producing a ((4-(6,8-dichloro-3-(2-(dipropylamino)-2-oxoethyl)imidazo[1,2-a]pyridin-2-yl)phenyl) (aryl)iodonium) anion precursor as an iodonium salt precursor; producing a 2-(6,8-dichloro-2-(4-(4,4,5,6-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)imidazo[1,2-a]pyridin-3-yl-N,N-dipropylacetamide precursor as a boron ester precursor; producing an iodonium salt precursor reaction solution; preparing a boron ester precursor reaction solution; and producing a radiotracer composition containing a fluorine-18-labeled radiotracer by reacting the iodonium salt or boron ester precursor reaction solution with the fluorine-18-labeled reaction solution. The use of the fluorine-18-labeled PET radiotracer makes it possible to diagnose patients with various brain diseases and tumors by obtaining new images of neuroinflammation, stroke and tumors associated with translocator protein overexpression through PET. In addition, by virtue of the long half-life of fluorine 18, the PET radiotracer can provide brain neuroinflammation and tumor imaging diagnostics to a larger number of patients compared to conventional carbon-11 tracers.

NOVEL RADIOMETAL-BINDING COMPOUNDS FOR DIAGNOSIS OR TREATMENT OF PROSTATE SPECIFIC MEMBRANE ANTIGEN-EXPRESSING CANCER

This application relates to compounds of Formula (I-a) or Formula (I-b), or is salts or solvates thereof. R.sup.1 is (CH.sub.2).sub.5CH.sub.3 or comprises 2-4 fused benzene rings. R.sup.2 is I, Br, F, Cl, H, OH, OCH.sub.3, NH.sub.2, NO.sub.2 or CH.sub.3. R.sup.3 is a peptide-bonded glycine, aspartate or glutamate or is glutamate peptide bonded through C.sub.delta. L is CH.sub.2NH, (CH.sub.2).sub.2NH, (CH.sub.2).sub.3NH, or (CH.sub.2).sub.4NH. R.sup.4 is a radiometal chelator optionally bound by a radiometal. Variable n is 1-3. The compounds may be useful for imaging prostate specific membrane antigen (PSMA)-expressing tissues or for treating PSMA-expressing diseases (e.g. cancer).

USE OF BERBERINE OR DERIVATIVE THEREOF IN PREPARING MYOCARDIAL PERFUSION IMAGING AGENT

Berberine or its derivatives are used in the preparation of myocardial perfusion imaging agents It has been verified using in vitro investigations, in vivo biodistribution, and small animal PET dynamic imaging, etc., that .sup.18F-labeled berberine derivatives can specifically accumulate in cardiomyocytes or heart tissues, and has good distribution properties of targetting heart muscle in living animals, together with high contrast values of heart v.s. peripheral tissue (liver, lung, blood, muscle, bone, etc.).

IMAGING AND RADIOTHERAPEUTICS AGENTS TARGETING FIBROBLAST-ACTIVATION PROTEIN-ALPHA (FAP-ALPHA)

Imaging and radiotherapeutics agents targeting fibroblast-activation protein- (FAP-) and their use in imaging and treating FAP- related diseases and disorders are disclosed.

RADIOPHARMACEUTICAL SYNTHESIS METHODS

The invention relates to products and methods that provide increased yields of certain radiopharmaceuticals.

PSMA inhibitor derivatives for labelling with 99mTc via HYNIC, a radiopharmaceutical kit, radiopharmaceutical preparations and their use in prostate cancer diagnostics

The subject matter of the invention is PSMA inhibitor-HYNIC derivatives of PSMA-L.sub.1-L.sub.2-HYNIC formula, aromatic and aliphatic hydrazone derivatives, a radiopharmaceutical kit for 99mTc isotope labelling, radiopharmaceutical preparation and its application for prostate cancer and its metastasis diagnostics.

COPPER-CONTAINING COMPLEX AND USES THEREOF
20200297878 · 2020-09-24 · ·

Complexes comprising a coordinated Cu(II) ion are described herein, which are capable of binding to an extracellular portion of Ctr1 such that the complex with the Cu(II) ion is transported through the Ctr1. The complexes may comprise a Cu(II) ion coordinated to a ligand and to a peptide, wherein the peptide is released upon contact of the complex with an extracellular portion of Ctr1, thereby forming a second complex comprising the ligand, the copper ion and the extracellular portion of Ctr1. Further described herein are uses and methods utilizing the complex, in imaging, in radiation therapy, and for determining a redox state of cells.

8-hydroxyquinoline derivatives as diagnostic and therapeutic agents

The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single-photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.

PSMA-BINDING AGENTS AND USES THEREOF
20200282083 · 2020-09-10 ·

Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.

Probes for imaging huntingtin protein

Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use. ##STR00001##