278 results about "Radioactive Label" patented technology

The invention relates to a radionuclide-labeled glucose derivative molecular probe and application thereof, and belongs to the technical field of nuclear medicine. According to the present invention, propargyl glycine is used to synthesize an amino acid skeleton, and the amino acid skeleton reacts with glucose azide to prepare a series of radionuclide-labeled glucose derivative molecular probes, such as [68Ga] Ga-NOTA-SDG, [68Ga] Ga-NOTA-DDG, [68Ga] Ga-NOTA-TDG, [68Ga] Ga-DOTA-SDG, [68Ga] Ga-DOTA-DDG and the like; the glucose derivative molecular probe labeled by the series of radionuclides has the advantages of being simple and rapid in labeling, high in radiolabeling yield and good in stability, can accurately position tumors, has good tumor uptake and lower non-target tissue uptake, and has great application prospects in preparation of broad-spectrum tumor imaging agents.

Methods for treating cancers and precancerous conditions by administering an effective amount of a radiolabeled agent that targets cell surface phosphatidylserine, alone or in combination with other therapies, are provided. The radiolabeled phosphatidylserine targeting agent delivers radiation to cells that externally present phosphatidylserine, such as tumor cells, depleting those cells and neighboring malignant cells to effect overall tumor reduction. Radiation delivered by the radiolabeled phosphatidylserine targeting agent itself increases the cell surface expression of phosphatidylserine, leading to a feed-forward mechanism that drives further accumulation of the phosphatidylserine targeting agent at target lesions to enhance its therapeutic effect.

The present invention belongs to the technical field of radiopharmaceutical chemistry and nuclear medicine diagnosis and treatment and relates to a radiolabeled FAPI complex, a preparation method therefor, and a use thereof. The general structural formula of FAPI capable of realizing radionuclide labeling is as shown below: wherein R is a nitroimidazole group or -COOH; X is a chelating group or a chelating structure chelated with a radionuclide; L1 and L2 are linking groups; and A is an adjusting atom of an FAP-targeting group, and all the A atoms are H atoms or F atoms. The synthesis method for a radionuclide-labeled precursor of the present invention is simple and suitable for various nuclide labels, the labeling method is convenient, and the label has high radiochemical purity and good stability. The radiolabeled FAPI complex shows high affinity and specificity for FAP in a cell experiment and a high tumor uptake and target to non-target ratio in a tumor-bearing mouse, and is a potential FAP-targeting radioactive diagnosis and treatment drug.

The present disclosure relates to stable compositions comprising a radiolabeled compound, and related pharmaceutical compositions and methods of manufacture. Such compositions are useful in both the diagnostic imaging of and the treatment of diseases (e.g., cancer).

The present disclosure provides a compound comprising a radiolabeling moiety, a targeting moiety, and a DNA intercalating agent and complexes thereof For example, the present disclosure provides a compound of Formula I or a pharmaceutically acceptable salt and / or solvate thereof. Methods of making and uses thereof, such as cancer theranostic applications, are also included. (I)

The present invention relates to MOFs for use in imaging and as radiolabeled tracers. More specifically, the present invention provides particles comprising MOFs, optionally at least one targeting moiety, and at least one short-lived radionuclide; compositions comprising the particles; the particles or compositions for use as imaging agents; the particles or compositions for use in methods for diagnosing proliferative diseases; the particles or compositions for use in methods for diagnosing chronic inflammatory diseases; and kits comprising particles comprising MOFs, optionally a targeting moiety, and a short-lived radionuclide cation.

The invention belongs to the technical field of radiopharmaceuticals, and particularly relates to a GPC3 targeted polypeptide probe and application thereof. According to the polypeptide probe targeting GPC3, non-natural functional groups are introduced to modify polypeptide ligands so as to enhance affinity, radiolabeling is carried out, and the polypeptide probe is used for PET molecular imaging diagnosis. The polypeptide probe shows good tumor targeting in vivo, the uptake of tumor tissues is remarkably different from that of normal liver tissues, the background of the normal liver tissues is clear, and a powerful tool and a theoretical basis are provided for noninvasive precise diagnosis of GPC3 positive liver cancer.

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 18F-labeling of unprotected peptides and sugars via thioarylation using a Au(III)-[˜F]fluoroaryl complex is reported. The chemoselective method generates 18F-labeled S-aryl bioconjugates in an aqueous environment in 15 min with high radiochemical yields and displays excellent functional group tolerance. This approach utilizes an air and moisture stable, robust organometallic Au(III) complex and highlights the versatility of designer organometallic reagents as efficient agents for rapid radiolabeling.

A compound comprising a prostate specific membrane antigen (PSMA)-targeting moiety of the following formula (I) or of a salt or a solvate thereof. R1 is —R1aR1b— wherein R1a is absent, —CH2—, —O—, or —S—, and R1b is —CH2— or —CHF—. R2 is —(CH2)3—O—, —(CH2)3—, —(CH2)4—, —CH2—O—(CH2)2—, or —CH2—S—(CH2)2. R3 is ethylene fused to a tricyclic fused ring. L1, L2, L3, L4, L5b L5c, L6 and L7 are linkages (e.g. peptide bonds). Xbr is a branching atom. Rrad is a radiometal chelator. Ralb is an albumin binder. n1, n2, n3, n4, and n5 are integers. When the PSMA-targeting moiety is linked to a radiolabeling group, the compound may be used as an imaging agent or therapeutic agent for PSMA-expressing diseases / conditions.

An intraoral tomosynthesis imaging apparatus having an intraoral detector coupled to a frame or radio-opaque marker attached to its radiation facing surface without any frame attached, wherein the frame defines a target aperture for an incident radiation beam. An enclosure seats against the target aperture and houses at least one x-ray source configured to emit a radiation beam from each of a plurality of focal points within the enclosure A collimator is disposed to form a collimated radiation beam and direct the collimated beam through the target aperture and to the detector. A geometric calibration phantom having a plurality of radio-opaque markers is disposed in the path of the collimated beam. This arrangement is modified to operate as a regular intraoral imaging device by accommodating a high-power central source at the same or different distances as other sources from the detector and displacing the phantom from the field of view.

The present invention relates to triglyceride analogs labeled with radioisotopes, or salts thereof, for positron emission tomography (PET) or single-photon emission computed tomography (SPECT) imaging. In addition, the present invention relates to compositions comprising the radiolabeled triglyceride analog, or a salt thereof, and methods for preparing the same. Further, methods of imaging using the radiolabeled triglyceride analog and uses of the radiolabeled triglyceride analog are disclosed herein. The invention also relates to an intermediate triglyceride analog for synthesis of the radiolabeled triglyceride analog.

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 application provides a synthetic process for production of lipoxin B4 and analogues thereof, which is modular and scalable, thus permitting synthesis of large quantities of LXB4 and analogues thereof, including radiolabeled analogues. Also provided are intermediate compounds that are useful in the synthetic process for production of lipoxin B4 and analogues thereof.

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 relates to radio- and fluorescence-labeled compounds, as well as their use as Diagnostics for Detecting Ecto-5′-Nucleotidase (CD73). The invention is further directed to a pharmaceutical composition comprising said compounds as well as to the compounds and the pharmaceutical composition for use in a method of diagnosis of a disease associated with increased or decreased CD73-expression as well as in the treatment of a disease associated with increased CD73-expression.

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.

To provide a method of synthesizing 2-(3{1-carboxy-5-[(6-[18F]fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-pentanedioic acid ([18F]DCFPyL), which is a radiotracer for prostate-specific membrane antigen (PSMA) PET imaging for prostate cancer.SOLUTION: A synthesis method comprises the following steps: (i) radiofluorinating a DCFPyL precursor comprising ester moiety-protecting groups to form a radiofluorinated DCPFPyL precursor; (ii) deprotecting the ester moiety-protecting groups of the radiofluorinated DCPFPyL precursor of the step (i) with phosphoric acid to form [18F]DCFPyL in a reaction mixture; and (iii) purifying the [18F]DCFPyL from the reaction mixture of the step (ii) to provide [18F]DCFPyL.SELECTED DRAWING: Figure 5

According to the pyridazinone derivative and the < 18 > F radiomarker thereof, the pyridazinone derivative and the < 18 > F radiomarker thereof have good hydrophilicity and metabolic pathway and can reduce uptake of non-target organs such as liver and the like, so that a better imaging effect is obtained; and mild and efficient direct 18F labeling can be carried out on drug molecules through a leaving group mediated nucleophilic substitution reaction, so that large-scale clinical popularization is facilitated. Animal experiment results show that the < 18 > F-labeled pyridazinone derivative provided by the invention has better in-vitro stability, heart-to-liver ratio, heart-blood ratio and heart-lung ratio than reported molecular probes, is high in myocardial uptake and rapid in metabolism in small animal bodies, is obvious in myocardial defect display, and can be used for preparing the < 18 > F-labeled pyridazinone derivative. The kit has a wide application prospect in diagnosis of diseases such as coronary heart disease with abnormal mitochondrial function as a marker.

The present invention relates to a kit for radiolabelling a targeting agent with gallium-68. The present invention also relates to the use of said kit for radiolabelling a targeting agent, a method for radiolabelling a targeting agent with gallium-68 using said kit, said kit and a method of preparation.

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.

Improved methods of radiolabeling antibodies using click chemistry are described. Also described are pharmaceutical compositions and uses related to the radiolabeled antibodies produced by the methods.

Radiolabeled liposomes can be used in the treatment of cancer. These local therapies can be used to treat cancers including, but not limited to, leptomeningeal metastases. In an embodiment, radiolabeled liposomes comprising (186Re) obisbemeda can be administered to a patient through an Ommaya reservoir. The therapies can include imaging the radiolabeled liposome concomitant or subsequent to administration.

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.

Disclosed are radiopharmaceuticals with high stability and radiolabeling efficiency obtained by attaching a radionuclide to a pharmaceutical part with high stability that is obtained by attaching a chelating agent to a pharmaceutical specific to the receptors present in the tumor area, the radiopharmaceuticals enabling the imaging and / or the destruction of the cancer cells. Also disclosed is are a method for obtaining the radiopharmaceuticals and to a kit including the radiopharmaceuticals. The radiopharmaceuticals basically include at least one radionuclide, which enables the imaging and / or the destruction of the cancer cells, at least one pharmaceutical part, which includes at least one pharmaceutical agent targeting the receptor that causes the growth of the cancer cells, and at least one chelating agent enabling at least one radionuclide to be attached to the pharmaceutical agent.