A61K51/0491

99mTc-LABELED ISONITRILE-CONTAINING GLUCOSE DERIVITIVE 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 the present invention 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 the present invention this disclosure is advantageous for popularization and application.

POLYMERIC CORE-SHELL PARTICLES
20210228750 · 2021-07-29 ·

A nanoparticle having a lipidic core, wherein the nanoparticle is linked via first polymeric linkers to a glucose molecules, and is further linked via second polymeric linkers to chelating agents, and wherein a weight ratio of the chelating agents to the nanoparticle is 1:20 to 1:80, respectively, is disclosed. Uses of the nanoparticle, particularly for imaging a tumor in a mammal, are further disclosed.

THERAPEUTIC, RADIOLABELED NANOPARTICLES AND METHODS OF USE THEREOF

Provided herein are therapeutic nanoparticles including a radiolabel, a chelator that is covalently linked to the therapeutic nanoparticle and to the radiolabel, and a nucleic acid molecule that is covalently linked to the therapeutic nanoparticle. The therapeutic nanoparticle has a diameter between about 10 nanometers (nm) to about 30 nm, and the therapeutic nanoparticle is magnetic. Also provided are pharmaceutical compositions containing these therapeutic nanoparticles. Also provided herein are methods of decreasing cancer cell invasion or metastasis in a subject having a cancer and methods of treating a metastatic cancer in a lymph node in a subject that require the administration of these therapeutic nanoparticles to a subject. Also provided herein are methods of detecting, diagnosing, and/or monitoring a metastatic cancer tissue in a subject. Also provided herein are methods of preparing these therapeutic nanoparticles.

Compounds and Methods of Making Compounds

Embodiments of the present disclosure provide for compounds and methods of making compounds such as those shown in FIG. 1.1A and 1.1B having formula 2, 3, 4, 5, 11, and 12 and formula 2′, 4′, and 11′, as well as uses for the compounds for imaging, and the like.

SYSTEMS, METHODS AND DEVICES FOR PRODUCING, MANUFACTURING AND CONTROL OF RADIOPHARMACEUTICALS

Systems, methods, and devices for generating radionuclides for use in production of radiopharmaceuticals; synthesizing the radionuclides generated and removing any unwanted products; measuring the quantity and activity level of the synthesized radionuclides; distributively delivering the radionuclides in appropriate quantities to modular cassette synthesis units in a modular cassette subsystem for contemporaneous/parallel production of radiopharmaceutical output and that allow reuse and/or quick, safe, and disposable replacement of portions of the subsystem; delivering non-radionuclide components to the modular cassette synthesis units as part of production of radiopharmaceutical output; measuring the quantity and activity level of each stream of radiopharmaceutical output; purifying the radiopharmaceutical output; dispensing individual doses in sterile vial(s); automatically producing labeling and dose related information; performing automated quality control on extracted samples of produced radiopharmaceutical output; and providing software and hardware controls for overall and sub-portion operation for optional remote data collection, communication, and/or control.

PURINE AND PYRIMIDINE NUCLEOTIDES AS ECTO-5'-NUCLEOTIDASE INHIBITORS

Disclosed is a compound of formula (I), wherein Q, U, T, A, a, b, c, and n are as defined herein. Also disclosed are methods of inhibiting ecto-5′-nucleotidase, inhibiting suppression of an antitumor immune response, inhibiting tumor growth of a cancerous tumor, inhibiting metastasis of cancer in a mammal afflicted with cancer, synergistically enhancing a response of a mammal afflicted with cancer undergoing treatment with an immunotherapeutic anti-cancer agent, potentiating an activity of an inhibitor of nicotinamide phosphoribosyltransferase in a mammal undergoing treatment of a mammal with the inhibitor, and treating preeclampsia in a mammal in need thereof, comprising administering to an animal an effective amount of a compound of formula (I).

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COMPLEX POLYSACCHARIDE-BOUND RADIOISOTOPE CHELATES AND METHODS OF TREATING MALIGNANCIES THEREWITH
20210283280 · 2021-09-16 ·

The invention provides a compound having the following structure:


D-DT-R,

wherein D is a dextran molecule or a charged dextran molecule having a molecular weight between about 50,000 and about 110,000 Daltons, DT is dodecane tetra-acetic acid (DOTA) or a conjugate base thereof, and R is a radioactive isotope. The invention also provides a method for treating body cavity cancer in a patient afflicted therewith, comprising administering an effective amount of a dextran-dodecane tetraacetic acid-radioactive isotope compound in a pharmaceutically effective vehicle.

COMPOSITIONS AND RELATED METHODS FOR BLOCKING OFF-TARGET LOCALIZATION OF MANNOSYLATED DEXTRANS AND OTHER CD206 LIGANDS
20210145989 · 2021-05-20 ·

Disclosed is a method for increase target specificity of a mannosylated dextran therapeutic or diagnostic compound by administering at least a blocking composition comprising a backbone and one or more CD206 targeting moieties attached thereto; administering an effective amount of the mannosylated dextran therapeutic or diagnostic compound comprising a dextran backbone and one or more CD206 targeting moieties and one or more therapeutic agents attached thereto. In exemplary implementations, the molecular mass of the blocking composition backbone is at least about two times larger than the molecular mass of the mannosylated dextran backbone compound.

CIRCULATING TUMOR CELL DIAGNOSTICS FOR LUNG CANCER

The present invention provides methods for diagnosing lung cancer in a subject comprising (a) generating circulating tumor cell (CTC) data from a blood sample obtained from the subject based on a direct analysis comprising immunofluorescent staining and morphological characteristics of nucleated cells in the sample, wherein CTCs are identified in context of surrounding nucleated cells based on a combination of the immunofluorescent staining and morphological characteristics; (b) obtaining clinical data for the subject; (c) combining the CTC data with the clinical data to diagnose lung cancer in the subject.

.SUP.18.F-saccharide-folates

The present invention is directed towards new .sup.18F-folate radiopharmaceuticals, wherein the .sup.18F isotope is linked via a prosthetic group, more specifically via a prosthetic group having a saccharide group, such as a cyclic mono- or oligosaccharide, preferably based on a pyranoside or furanoside, which is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.