342 results about "Radioactive Label" patented technology

The invention provides a compound DOTA-HX2-DZ and application thereof, and belongs to the technical field of biological medicine. According to the invention, the molecular structure of DZ-HX2-DOTA is optimized, and a special connexon is designed and adopted, so that the problem of limited anti-tumor curative effect caused by poorer stability, fat solubility, tumor residence time and other properties of a radiolabeled drug in the prior art is solved. The compound provided by the invention can significantly reduce the risk of label removal of radioactive metal ions in an in-vivo environment, and ensures that the compound stably plays a role at a targeted part; the compound has excellent molecular lipid solubility, can penetrate cell membranes and vascular barriers more easily, improves the bioavailability of drugs, prolongs the in-vivo circulation time, prolongs the tumor residence time, and further improves the treatment efficiency. The DZ-HX2-DOTA disclosed by the invention has broad-spectrum tumor targeting property, and can be used for diagnosing and treating various types of malignant tumors.

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.

It is an object of the present invention to provide drugs that bind specifically to FAPα, are effective in the treatment and diagnosis of tumors or cancers expressing FAPα, for example, in the treatment and diagnosis of solid cancers such as pancreatic cancer, sarcoma, esophageal cancer, lung cancer, breast cancer, prostate cancer, head and neck cancer, ovarian cancer, colon cancer, neuroendocrine tumor, thyroid cancer, uterine cancer, liver cancer and the like (particularly, pancreatic cancer), and have a lower risk of prolonged side effects. The present invention provides a conjugate comprising a radioactive moiety comprising an aryl group substituted with a radionuclide selected from 211At, 210At, 131I, 125I, 124I, 123I, 77Br and 76Br, and a bioactive moiety having an affinity for fibroblast activation protein α (FAPα).

The invention discloses a class of radiopharmaceutical labeled precursors targeting prostate specific membrane antigens, the structure of the radiopharmaceutical labeled precursors is shown as the following: # imgabs0 #, a precursor reagent RESCA-PSMA-1802 targeting prostate specific membrane antigens is synthesized for the first time, the reagent can be labeled by using an 18F-Al method to prepare a positron imaging agent 18FAl-RESCA-PSMA-1802, and the reagent can be used for preparing the prostate specific membrane antigens. The polymer has good stability and biological activity in vivo and in vitro, has good targeting property on prostate cancer cells, can reflect tumor recurrence or metastasis conditions, and is very suitable for PET imaging.

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 invention provides a preparation method of Al18F tracer integrated freeze-dried powder, a kit and application thereof, and the preparation method comprises the following steps: dissolving 1-10 mg of a precursor by using deionized water, adding a pH buffer solution with the concentration of 0.2-0.5 M and an AlCl3 solution with the concentration of 10 mM, with the ratio of the amount of substance of AlCl3 to the amount of substance of the precursor being 0.8-1.0, then continuously adding a stabilizer solution with the concentration of 0.5 M and 1-4 mg of an excipient, and uniformly stirring to obtain the Al18F tracer integrated freeze-dried powder. And finally, adding deionized water to enable the concentration of the precursor to be 0.5-1.0 mM, uniformly mixing the solution, sub-packaging the solution into 1.5 mL cryopreservation tubes or 2 mL penicillin bottles according to a certain volume, and then putting the cryopreservation tubes or the penicillin bottles into a vacuum freeze dryer to remove water at a low temperature to obtain powder or freeze-dried cakes, and the container is a freeze-dried powder / cake storage container and is used for storing the freeze-dried powder / cakes. Meanwhile, the reaction container is also used during radioactive labeling.

The invention discloses a radioactive labeling method of [18F] trifluoromethyl terminal olefin in the technical field of organic synthesis, under the condition of room temperature, 3, 3-difluoroallyl sulfosalt is used as a precursor, [18F] KF / K222 or [18F] TBAF is used as a fluorinating reagent, acetonitrile is used as a solvent, very high radiochemical yield can be obtained within 30 seconds, the tolerance of functional groups is excellent, and the method is suitable for industrial production. The specific reaction formula is as follows: # imgabs0 #. The method provides a simple and efficient way for producing the [18F] trifluoromethylated terminal olefin compound, so that the [18F] trifluoromethylated terminal olefin compound can be applied to positron emission tomography imaging. According to the method for preparing the 3, 3-difluoroallyl sulfur salt compound, the raw materials are easy to obtain, the cost is low, the operation is simple and convenient, safety and controllability are realized, and the radiation yield of the obtained product is high.

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 invention belongs to the field of tumor drugs, and discloses a radioactive hydrogel based on crosslinking of sodium alginate and metal ions and a preparation method and application thereof.The preparation method of the radioactive hydrogel comprises the following steps that lutetium chloride and metal ions are mixed, and a metal ion mixed solution is obtained; doping 177Lu radioactive isotope into the obtained metal ion mixed solution to obtain a metal ion cross-linking agent; and injecting a metal ion cross-linking agent into the sodium alginate solution under a vortex condition, centrifuging, and discarding the supernatant to obtain the radioactive hydrogel. The radioactive hydrogel (177Lu-RH) provided by the invention has good in-tumor colonization capability, can be directly injected into a tumor to realize local radiotherapy, has good radioactive stability, and can be stably retained at a tumor part for more than 120 hours, so that the stability of radioactive labeling in a treatment process is ensured.

Disclosed is a compound 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 225 Ac, a beta particle emitter such as 67Cu or 177Lu, or an Auger electron emitter (e.g. 111In, 67Ga, 99mTc, 195mPt, 125I and 123I). The compounds can also be attached to a cytotoxic agent for targeted delivery of the cytotoxic agent to tumors, for example conjugated to gemcitabine or doxycycline, or a venom. Likewise, the compounds can be conjugated to compounds having physiological effects, such as TLR agonists to stimulate the immune response of a recipient.

The present disclosure relates to compounds, pharmaceutical compositions, and methods of using the compounds and compositions to image reactive oxygen and nitrogen species (RONS). The disclosed compounds and pharmaceutical compositions can also be useful in treating diseases or disorders due to oxidative stress or otherwise based on RONS pathophysiology such as, for example, neurological diseases, cancer, cardiovascular diseases, and ischemia reperfusion injury (IRI). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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 relates to a radiolabeled FAPI complex as well as a preparation method and application thereof, and belongs to the technical field of radiopharmaceutical chemistry and nuclear medicine diagnosis and treatment. The structural general formula of the FAPI capable of being subjected to radionuclide labeling is as follows: # imgabs0 #, wherein R is a nitroimidazole group or-COOH; x is a chelating group or a chelating structure of a chelating radionuclide; l1 and L2 are linking groups; a is a regulating atom of an FAP targeting group, and A is an H atom or an F atom. The synthesis method of the radionuclide labeling precursor is simple and suitable for labeling of various nuclides, the labeling method is convenient and fast, and the radiochemical purity of the label is high, and the stability is good; the radiolabeled FAPI complex shows high affinity and specificity with FAP in cell experiments, shows high tumor uptake and target-to-non-target ratio in tumor-bearing mice, and is a potential FAP targeted radioactive diagnosis and treatment drug.

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, Me2 Thz, 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 invention relates to a new therapeutic radiopharmaceutical as an inhibitor of prostate-specific membrane antigen (iPSMA), wherein 1,4,7,10-tetraazacyclododecane-N, N′, N″, N″″ -tetraacetic acid (DOTA) bonded to the heterocyclic molecule hydrazinonicotinamide (HYNIC), generates a rigid chemical structure that minimises the number of conformers and intramolecular hydrogen bonds, thereby producing a favourable spatial orientation of the active site (Lys(Nal)—NH—CO—NH-Glu) in the molecule, for biological recognition by the PSMA protein. The new DOTA-HYNIC-iPSMA radiopharmaceutical accumulates, with high affinity in vivo, in tumours that overexpress the PSMA protein, acting as a radiotherapeutic or radiodiagnostic agent. The purpose of the invention is to provide a new specific radiopharmaceutical (molecular target radiopharmaceutical) for the detection and treatment of tumours with PSMA overexpression. Radiolabelling of the new molecule is demonstrated with lutetium-177, actinium-225, terbium-161, gallium-67 or gallium-68 isotopes.

The invention relates to a compound targeting prostate specific membrane antigen as well as a preparation method and application thereof. The compound provided by the invention has a wide application prospect in the aspects of diagnosis and treatment of diseases with high expression of prostate specific membrane antigen (PSMA). The preparation method of the compound provided by the invention has the advantages of simplicity, high efficiency and short preparation time, the marking condition of radiolabeling is simple, and the radiochemical yield is high.

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.