Abstract: The present invention relates to a ligand-SIF A-chelator conjugate, comprising, within in a single molecule three separate moieties: (a) one or more ligands which are capable of binding to a disease-relevant target molecule, (b) a silicon-fluoride acceptor (SIFA) moiety which comprises a covalent bond between a silicon atom and a fluorine atom, and (c) one or more chelating groups, optionally containing a chelated nonradioactive or radioactive cation.
Type:
Grant
Filed:
June 24, 2022
Date of Patent:
August 19, 2025
Assignees:
Technische Universität München, Technische Universität München—Klinikum Rechts der Isar
Inventors:
Alexander Josef Wurzer, Hans-Jürgen Wester, Matthias Johannes Eiber
Abstract: The present invention relates to novel, selective, radiolabelled compound having monoacylglycerol lipase (MGL) affinity which are useful for imaging and quantifying MGL receptor expression, distribution and enzyme occupancy in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
Type:
Grant
Filed:
December 1, 2023
Date of Patent:
August 12, 2025
Assignee:
Janssen Pharmaceutica NV
Inventors:
Gang Chen, Chaofeng Huang, Jimmy T. Liang
Abstract: Rigidified pentadentate chelating agents of Formulae (I) and (II), which are useful for the [Al18F]2+ labelling of biomolecules are provided. The rigidified pentadentate chelating agents are used to form coordination complexes with [Al18F]2+, which are particularly advantageous for use as tracers in molecular imaging techniques.
Type:
Grant
Filed:
March 17, 2020
Date of Patent:
August 5, 2025
Assignee:
UNIVERSITÀ DEGLI STUDI DEL PIEMONTE ORIENTALE “A. AVOGADRO”
Abstract: The present invention provides in certain embodiments a carcinoma-targeting conjugate comprising Formula I: T-L-X wherein T is a SSTR2 targeting ligand, L is a linker, and X is a chelator, for the therapeutic treatment of cancer, and methods of use thereof.
Type:
Grant
Filed:
July 12, 2024
Date of Patent:
June 24, 2025
Assignee:
UNIVERSITY OF IOWA RESEARCH FOUNDATION
Inventors:
Dongyoul Lee, Michael K. Schultz, Mengshi Li, Nicholas Baumhover, F. Christopher Pigge
Abstract: The present disclosure relates to a pharmaceutical composition comprising 177Lu-PSMA I&T and methods of administering the same. The administration of the composition results in a low absorbed radiation dose per gram of tissue in a human patient's body, including the kidneys, gastrointestinal tract, left colon, liver, rectum, red marrow, spleen, lacrimal glands, and salivary glands.
Type:
Grant
Filed:
July 31, 2024
Date of Patent:
June 10, 2025
Assignee:
Curium US LLC
Inventors:
Jarno Jalomäki, Salla Seppänen, Amanda Donovan, Jessica Salem, Allan Casciola, Anthony Vaughn
Abstract: The present invention relates to complexes comprising a prostate-specific membrane antigen (PSMA) targeting compound linked to a radionuclide, such as 212Pb or 227Th, through a TCMC or DOTA chelating moiety. These compounds, and pharmaceutical compositions comprising them, can be used for medical applications. These applications include the treatment of prostate cancer, and the complexes allow for dual targeting of cancers.
Abstract: The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue via 18F-labeled peptide ligands disclosed herein.
Abstract: The invention relates to compounds according to Formula (I): wherein A is —As(OH)2 or an arsenoxide equivalent group; each of R1, R2, R3 and R4 is independently selected from H, X, OH, NH2, CO, SCN, —CH2NH, —NHCOCH3, —NHCOCH2X or NO, and X is a halogen; R5 is —NHCH2COOH, OH or OR6, wherein R6 is a C1-5 straight or branched alkyl group; and Z is a radioisotope with a half-life of less than 4 days, or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof, uses of said compounds, and methods of preparing said compounds. The invention also relates to diagnostic methods utilizing said compounds.
Type:
Grant
Filed:
August 18, 2023
Date of Patent:
May 13, 2025
Assignees:
CENTENARY INSTITUTE OF CANCER MEDICINE AND CELL BIOLOGY, UNIVERSITY OF SYDNEY
Abstract: The present invention relates to compounds of general formula (I) for chromatographic separation of rare earth elements and/or s-, p-, d-metals, as well as to the method of the separation of rare earth elements.
Type:
Grant
Filed:
November 30, 2018
Date of Patent:
April 8, 2025
Assignee:
USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR. V.V.I.
Abstract: HPLC-based quality control systems to perform quality control testing on a radiopharmaceutical solution shortly after synthesis. An HPLC-based quality control system makes efficient use of sample volume and is compatible with a variety of radioisotopes and radiopharmaceutical compounds. In several embodiments, the automated nature of an HPLC-based quality control system allows for quality control tests to be conducted quickly and with minimal impact on user workflow. When used as part of an integrated PET biomarker radiopharmaceutical production system, the present general inventive concept permits a manufacturer to produce product and conduct quality control tests with lower per dose costs.
Type:
Grant
Filed:
April 13, 2012
Date of Patent:
February 25, 2025
Assignee:
Best ABT, Inc.
Inventors:
Ronald Nutt, Anthony M. Giamis, Aaron McFarland
Abstract: 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.
Abstract: The present invention relates to a method for conditioning reversed phase SPE cartridges that provides certain advantages compared with known such methods. The method of the invention finds particular use in the automated synthesis of radiolabeled compounds where SPE is used for example in the purification steps.
Type:
Grant
Filed:
December 21, 2017
Date of Patent:
January 28, 2025
Assignee:
GE HEALTHCARE LIMITED
Inventors:
Nicolas Verbrugge, Xavier Y. A. Franci, Natthawadee Thawinwisan
Abstract: The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein: R1 and R2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R3 is hydrogen or halogen; ring A is a benzene ring or a pyridine ring; ring B is selected from the group consisting of the following formulas (i), (ii), (iii), and (iv): in the formula (ii), Ra is alkyl; R4 and R5 are each separately selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl; and represents a double bond or a triple bond. The above compound can be used as a molecular probe for imaging tau proteins that accumulate in the brain.
Type:
Grant
Filed:
May 8, 2023
Date of Patent:
January 14, 2025
Assignee:
National Institutes for Quantum and Radiological Science and Technology
Abstract: A mannose derivative is an isonitrile-containing mannose derivative of formula (I), including different linking groups X: A radioactive preparation is provided, including a radiolabeled compound formed by radiolabeling the mannose derivative with a radionuclide. An application of the radioactive preparation in the diagnosis and treatment of tumors is also provided.
Type:
Grant
Filed:
November 17, 2023
Date of Patent:
December 10, 2024
Assignee:
Beijing Normal University
Inventors:
Junbo Zhang, Qing Ruan, Guangxing Yin, Xuebin Wang, Zhanbin Zhang, Zhigang Tang, Jie Lu
Abstract: An F-18 labeled chiral pure derivative of hydroxyfuran, a preparation method and use thereof were provided. (4R, 5R)[18F]FAA provided by the present disclosure is a chiral pure radioactive compound, and three other chiral pure [18F]FAA structural formulae are also provided by the present disclosure. The present disclosure provides a chiral pure radioactive probe (4R, 5R)[18F]FAA, which shows unique tumor diagnostic efficiency and similar distribution to AA, and can be used for early diagnosis of tumors, pathological studies, assessment of disease progression, and evaluation for efficacy.
Type:
Grant
Filed:
May 25, 2023
Date of Patent:
December 10, 2024
Assignee:
The First Affiliated Hospital of Sun Yat-sen University
Inventors:
Zhihao Zha, Xiangsong Zhang, Renbo Wu, Jianbo Liu
Abstract: Radioisotope-labeled small molecule activity-based probes that target the cancer associated serine hydrolase neutral cholesterol ester hydrolase 1 (NCEH1) are described. The probes can undergo a reaction with the NCEH1, resulting in covalent bonding of a portion of the probe molecule to the NCEH1. Also described are methods of labeling NCEH1 in biological samples, such as cells or tissue, and methods of visualizing tumors using the radioisotope-labeled NCEH1 probes as tracer compounds, either alone or in combination with assessing the efficacy of a cancer treatment or potential cancer treatment.
Abstract: The invention provides a compound of formula (I), and salts, solvates and radiolabelled forms thereof, together with complexes of the compound of formula (I) with TSPO, and methods for forming such complexes, and methods for detecting the compound of formula (I), such as in complex with TSPO.
Type:
Grant
Filed:
June 21, 2019
Date of Patent:
October 29, 2024
Assignees:
The University Court of the University of Glasgow, The University Court of the University of Edinburgh
Inventors:
Andrew Sutherland, Sally Pimlott, Adriana Tavares, Christoph Lucatelli
Abstract: A method of performing a chelating reaction comprising contacting a divalent metal with a compound of Formula (I): or a salt thereof wherein: each of R1-R4 is independently selected from the group consisting of CH2COORa and CH2C(?O)NHRa; each of R5-R12 is independently selected from the group consisting of H and -L-X; each Ra is independently selected from the group consisting of H and -L-X; each L is independently selected from the group consisting of absent and a linking group; and each X is a biological agent; and wherein the contacting occurs at a temperature below about 40° C. to form a chelated composition.
Type:
Grant
Filed:
April 25, 2019
Date of Patent:
October 29, 2024
Assignee:
UNIVERSITY OF IOWA RESEARCH FOUNDATION
Inventors:
Michael K. Schultz, Christopher Pigge, Mengshi Li, Moustafa Gabr, Edwin Sagastume
Abstract: The present disclosure is generally related to methods, systems and devices for direct production of a radioisotope-based cancer treatment pharmaceutical directly from a corresponding non-radioactive drug molecule precursor by irradiating the non-radioactive drug molecule precursor using neutrons produced by an electronic neutron generator array or other neutron generator sources.
Type:
Grant
Filed:
February 4, 2022
Date of Patent:
September 17, 2024
Assignee:
Westinghouse Electric Company LLC
Inventors:
Michael D. Heibel, James Boyle, Kris Paserba
Abstract: The present disclosure relates to radiolabeled compounds and methods of uses for diagnosis, monitoring, and treatment of various degenerative neurological disorders, neuropsychiatric disorders, brain injuries, vascular diseases, and cancers. Radiolabled compounds for imaging of microtubules or microtubules and other targets using positron-emission tomography (PET) are specifically disclosed.
Type:
Grant
Filed:
October 30, 2018
Date of Patent:
August 6, 2024
Assignee:
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
Inventors:
Dileep Kumar, J. John Mann, Akiva Mintz, Kiran Kumar Solingapuram Sai