135 results about "Radioactive Label" patented technology

The invention relates to the technical field of sensing of magnetic nano photoelectric materials, in particular to a responsive microsphere based on a three-dimensional magnetic photonic crystal and a preparation method and application thereof, and the responsive microsphere is formed by arranging polyhydroxy compound modified magnetic nanoparticles in a spherical polymer into a non-close packing face-centered cubic or body-centered cubic structure. The responsive microsphere based on the three-dimensional magnetic photonic crystal is easy in color distinguishing, has no angle dependence, does not need to depend on a fluorescent dye or a radioactive label, can realize real-time and in-situ monitoring through own optical characteristics, breaks through the bottlenecks of sensitivity and resolution of a traditional sensor, realizes visual detection, simplifies the detection process, and is suitable for mass production. The cost is reduced. According to the responsive microsphere based on the three-dimensional magnetic photonic crystal, the substance diffusion path is shortened through the small size of the responsive microsphere, and the response speed is remarkably increased in combination with the high specific surface area.

The present invention relates to novel, selective compounds with affinity to TDP-43, and to novel, selective radiolabelled TDP-43 ligands which are useful for imaging TDP-43 aggregates, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging TDP-43 aggregates in a tissue or a subject, in vitro or in vivo, and to precursors of said compounds.

The present invention relates to MSLN-specific binding constructs comprising a designed ankyrin repeat domain with binding specificity for MSLN and a chelator capable of bonding to a radionuclide, as well as to such MSLN-specific binding constructs comprising a half-life extending moiety with binding specificity for serum albumin. The invention further relates to methods of producing such radio-labelled MSLN-specific binding constructs, pharmaceutical compositions comprising such constructs, and the use of such constructs or pharmaceutical compositions in methods for treating, imaging or diagnosing diseases, such as cancer.

The present invention provides radiolabeled 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-α]indol-9-yl]pyridin-2(1H)-one derivatives of general formula (I) or salts thereof, as well as precursors of the radioligands of general formulae (II) and (III), processes for their preparation, and intermediates of the processes. The radiolabeled compounds enable visualization and quantification of melanin-concentrating hormone receptor 1 (MCHR1) in various target tissues, including monitoring MCHR1 in such target tissues. The compounds exhibit high binding affinity for MCHR1 and are able to cross the blood-brain barrier, thus facilitating diagnosis of various disease states in human clinical studies.

The present invention provides a pharmaceutical composition comprising a radiolabeled complex comprising a radionuclide and a targeting moiety linked to a chelating moiety, and a stabilizer against radiolytic degradation of a radiolabeled complex comprising para-aminohippuric acid or a pharmaceutically acceptable salt or carboxylic derivative thereof. The pharmaceutical composition of the present invention is characterized by high stability of its radiolabeled complex against radiolytic degradation. The present invention also provides a method for preparing such a pharmaceutical composition, and use of para-aminohippuric acid or a pharmaceutically acceptable salt or carboxylic derivative thereof for the stabilization of the radiolabeled complex of such a pharmaceutical composition.

This invention provides a combination for use in treating cancers that express prostate-specific membrane antigen (PSMA). [Solution] A combination comprising a PD-1 inhibitor, a CTLA-4 inhibitor, and a radiolabeled compound of formula Ia for use in treating PSMA-expressing cancer in the subject. JPEG2026049728000042.jpg45132 The aforementioned combination comprises one or more further anticancer agents, wherein the further anticancer agents are selected from octreotide, lanreotide, vapreotide, pasireotide, satreotide, everolimus, temozolomide, telotristat, sunitinib, sulfatinib, ribociclib, entinostat, and pazopanib.

The present invention relates to novel, selective compounds with affinity to TDP-43, and to novel, selective radiolabelled TDP-43 ligands which are useful for imaging TDP-43 aggregates, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging TDP-43 aggregates in a tissue or a subject, in vitro or in vivo, and to precursors of said compounds.

Disclosed are compositions and methods for the treatment of disease (e.g., cancer) using conjugates comprising a protein-binding moiety (e.g., an antibody or an antigen-binding fragment thereof) and one or more radiolabeled metalloporphyrin complexes. Also disclosed are conjugates that further include one or more chemotherapeutic agents.

Some embodiments relate to imageable radioisotope microspheres. In some embodiments, the imageable microspheres are radiolabeled with an imageable radioisotope. In some embodiments, the imageable radioisotope is directly chemically coupled to the surface of the microsphere matrix. In some embodiments, the imageable microspheres can be used as surrogate particles to predict the distribution of therapeutic microspheres containing radiotherapeutic isotopes.

There are provided fructose-based radiopharmaceuticals, pharmaceutical compositions comprising same, methods for preparing same, and methods of using same for biomedical imaging, particularly nuclear imaging using PET or PET / CT. (Compound 7)

The invention discloses a bisphosphonate radiomarker, and a precursor compound, a preparation method and application thereof, and belongs to the technical field of nuclear medicine. The structure of the precursor compound of the radioactive marker or the salt of the precursor compound is shown as a formula I; the structure of the radioactive marker or the salt thereof is shown as a formula II. The invention also discloses a preparation method of the precursor compound and the radioactive marker. The invention also discloses application of the precursor compound and the radioactive marker in preparation of a bone metastatic tumor targeted tumor imaging agent or / and a tumor therapeutic agent. The radioactive marker disclosed by the invention is relatively high in water solubility, relatively good in-vitro stability at room temperature and high in plasma protein binding rate, relatively high and relatively long-lasting skeleton uptake is shown in imaging and in-vivo distribution in mice, the imaging effect is superior to that of 99mTc-MDP, 68Ga-DOTA-ibandronic acid and 68Ga-labeled dithiophosphoric acid derivatives, and the radioactive marker has a wide application prospect. The compound is an excellent bone developer and a medicine for treating tumor bone metastasis.

Disclosed are compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof. The variables of structural formula (I) are described herein. The compound of the invention can be attached to chelating groups for radionuclide binding and are therefore suitable for radioimaging and / or radiotherapy applications, for example the disclosed compounds can be radiolabeled with a positron emitter such as 18F, 68Ga or 64Cu, and used for positron emission tomography (PET). Alternatively, the compounds can be radiolabeled with an alpha particle emitter such as 223 Ac, a beta particle emitter such as 67Cu or 177Lu, or an Auger electron emitter (e.g. 111In, 67Ga, 99mTc, 195mPt, 125I, 123I and 161Tb) for use as a radiotherapeutic.

This radioactively labeled compound is represented by formula (1). In formula (1), M represents a radioactive metal ion. A represents a chelate moiety coordinated to the radioactive metal ion. B represents a first atomic group having a structure in which ethyleneimine is polymerized. C represents a second atomic group having a molecular weight of 5000 or less and capable of binding to a molecule expressed in a tumor cell. The second atomic group preferably includes a linear or cyclic peptide. The second atomic group also preferably includes 1-50 amino acid residues.

The present invention discloses a method for treating thyroid cancer using a radiolabeled cleavage-type Evans Blue degenerated fibroblast-activating protein inhibitor, said drug having excellent safety and tolerance in patients with thyroid cancer and having a very excellent therapeutic prospect in the treatment of thyroid cancer.

The present application relates to the technical field of sensing of magnetic nano-optoelectronic materials, and particularly relates to a responsive microsphere based on three-dimensional magnetic photonic crystals, a preparation method and application thereof, wherein magnetic nanoparticles modified by a polyhydroxy compound are arranged in a non-close-packed face-centered cubic or body-centered cubic structure in a spherical polymer to form the responsive microsphere. The responsive microsphere based on three-dimensional magnetic photonic crystals has an easily distinguishable color, is not angle-dependent, does not need to rely on fluorescent dyes or radioactive labels, and can realize real-time and in-situ monitoring through its own optical properties, thus breaking through the bottleneck of sensitivity and resolution of traditional sensors, realizing visual detection, simplifying the detection process, and reducing the cost. The responsive microsphere based on three-dimensional magnetic photonic crystals shortens the diffusion path of substances through its small size, and significantly improves the response speed in combination with a high specific surface area.

Radiolabeled anti-MET antibodies and MET×MET bispecific antibodies and their use in immuno-PET imaging are provided herein. Included are methods of detecting the presence of MET proteins in a subject or sample and methods of monitoring efficacy of treatment of a Met expressing tumor.

The present invention relates to fibroblast activation protein (FAP) - based ligands assembled through tetrazine ligation and their use in radiotherapy and imaging. The FAP inhibitor (FAPi) ligand compounds provided herein comprises a FAP targeting moiety, a linker, an IsoF-TCO and a radiolabeled tetrazine. The FAPi targeting compounds are possessing advantageous pharmacokinetic properties and enable quick and efficient modifications of the radiopharmaceuticals allowing a fast renal excretion and reduced liver accumulation.

There is provided peptidic compounds of Formula I, A or B(Rradn6-[linker]-RL-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-ψ-Xaa9-NH2). Xaa1 is D-Phe, Cpa, D-Cpa, Nal, D-Nal, 2-Nal, or D-2-Nal; Xaa2 is Asn, Gln, Hse, Cit or His. Xaa3 is Trp, Bta, Trp(Me), Trp(7-Me), Trp(6-Me), Trp(5-Me), Trp(4-Me), Trp(2-Me), Trp(7-F), Trp(6-F), Trp(5-F), Trp(4-F), Trp(5-OH), or αMe-Trp. Xaa4 is Ala or Ser. Xaa5 is Val, Cpg, or Tle. Xaa6 is Gly, NMe-Gly, or D-Ala. Xaa7 is His or NMe-His. Xaa8 is Leu or Phe. Xaa9-NH2 is a C-terminally amidated amino acid residue selected from Pro, 4-oxa-L-Pro, Me2Thz, or Thz. ψ represents a peptide bond or reduced peptide bond joining Xaa8 to Xaa9. Rradn6 is 1-5 radiolabeling groups. There is also provided the use of such compounds as imaging agents or therapeutic agents.

The present invention provides a probe compound for labeling a cysteine protease based on activity. The compound targets the protease through a specific targeting element. The compound also includes a detectable element, such as a fluorescent label, a radioactive label, or a chelator. In some cases, the compound also includes a quenching element that is released upon reaction with the protease. The present invention also provides compositions comprising the compound, as well as methods of using the compound, such as labeling a protease in an animal and visualizing a tumor in an animal.

The present invention relates to MOFs for use in imaging and as radiolabeled tracers. More particularly, the invention provides a particle comprising a MOF, optionally at least one targeting moiety and at least one short-lived radionuclide; a composition comprising said particle; said particle or composition for use as an imaging agent; said particle or composition for use in a method for the diagnosis of a proliferative disease; said particle or composition for use in a method for the diagnosis of a chronic inflammatory disease; and a kit comprising a particle comprising a MOF, an optional targeting moiety, and a short-lived radionuclide cation.

Radiolabeled anti-PD-L1 antibodies and their use in immuno-PET imaging are provided herein. Included are methods of detecting the presence of PD-L1 proteins in a patient or sample.

The present invention relates to radiolabeled gemtuzumab ozogamicin antibodies and humanized versions conjugated with the radionuclide astatine 211 The antibody conjugates are used in radiotherapy for the treatment of urothelial cancer, including bladder cancer.

A labeled cell targeting agent for in vivo imaging of a subject is disclosed. The labeled cell targeting includes, for example, a radiolabel or a paramagnetic ion or compound or a labeling agent-binding moiety; and a polypeptide comprising an IL13 or mIL13 amino acid sequence that binds IL13Rα2 and optionally a PE cytotoxin amino acid sequence. Methods of preparing and using the agent also are provided. The labeled cell targeting agent may be used in a method of in vivo imaging, wherein the method comprises administering the labeled therapeutic agent to a subject such that a cell of the subject becomes labeled for in vivo imaging, wherein the cell may be an IL13Rα2-expressing cell, such as a diffuse midline glioma cell or a glioblastoma cell.

Disclosed in the present invention are a radiolabeled compound of a risedronic acid derivative, and a precursor compound thereof, and a preparation method therefor and the use, which belong to the technical field of nuclear medicine. Provided in the present invention are a precursor compound of a radiolabeled compound of a risedronic acid derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and a radiolabeled compound of a risedronic acid derivative as shown in formula (II) or a pharmaceutically acceptable salt thereof. In the present invention, risedronic acid is creatively combined with a chelating agent to obtain NOTA-risedronic acid and DOTA-risedronic acid, and then a radionuclide is used for labelling. The radiolabeled product of the present invention has a relatively high water solubility, good in-vitro stability at room temperature, and a high plasma protein binding rate, and exhibits a relatively high and prolonged bone uptake in terms of imaging and in vivo distribution in mice; and compared to 68Ga-DOTA-ibandronic acid, the uptake of the compound of the present invention at the lesion site is twice as high.

The present disclosure provides for imaging agents and methods of making and using the same. The imaging agent comprises a luminol component comprising a luminol moiety or functional analogue thereof; a chelator; a linker group bonding or complexing the luminol component to the chelator; and a radiolabel component bound to the chelator. The imaging agent described herein is capable of monitoring, targeting, or imaging oxidative stress, reactive oxygen species (ROS), superoxide generation, or hydrogen peroxide generation, mediating pathophysiology of different disease states.