Abstract: Small molecule radiohalogenated PSMA inhibitors and metal complexes thereof and their use in radioimaging and radiotherapy for treating PSMA-related diseases, including prostate cancer, are disclosed. The combination of small molecule radiohalogenated PSMA inhibitors with a competitive PSMA ligand for reducing off-target accumulation of the radiohalogenated PSMA inhibitor also is disclosed.

Abstract: Theranostic agents incorporating a chelating moiety that can chelate a radioactive metal isotope and a PSMA-targeting moiety are disclosed herein. The theranostic agents, which can be used to treat and/or detect cancers associated with increased PSMA expression, have the formula: and include complexes, anions or salts thereof. R1 includes a chelating moiety; a is 0 or 1; n is an integer from 12 to 21; and R2 includes a prostate specific membrane antigen (PSMA)-targeting moiety. Optionally, the chelating moiety is chelated to a metal atom, where the metal atom is a positron or single photon emitting metal isotope, or an alpha, beta, or Auger emitting metal isotope.

Abstract: A method for treating melanoma or preventing the development of melanoma comprising administration of a composition comprising 64Zne(Asp)2 in a therapeutically effective amount. Such administration may be via injection such as intratumoral and/or intravenous injection and may be once a day or more than once a day. A composition for the treatment of or prevention of melanoma comprising 64Zne(Asp)2 in a therapeutically effective amount. The composition may be a liquid suitable for injection.

Abstract: One aspect of the present invention is directed to triblock peptides comprising a lipid moiety, a peptide block and a zwitterion-like block. Another aspect of the invention is directed to pharmaceutical compositions comprising the triblock peptides of the present in invention arranged in micelles in a pharmaceutically acceptable carrier. In certain embodiments, the pharmaceutical compositions of the present invention are vaccine compositions, which may further comprise an adjuvant. Another aspect of the invention is directed to methods of using the triblock peptides and compositions of the invention to treat a disease or condition.

Abstract: A compound is disclosed that can be used as an anti-inflammatory agent, a cyclooxygenase-2 inhibitor, a therapeutic agent for brain diseases, or a MRI contrast medium. The compound can have the structure represented by chemical formula 1.

Abstract: The present invention relates to a pharmaceutical composition for diagnosing and treating prostate cancer, capable of targeting PSMA, and a compound provided by one aspect of the present invention has a glutamine-urea-lysine compound to which a radioactive metal-coupled chelator is structurally coupled and to which an aryl group that can additionally bind to PSMA protein is coupled. Coupling between the glutamine-urea-lysine compound and the chelator includes a polar spacer so as to serve the role of reducing in vivo nonspecific coupling and exhibit an effect of being rapidly removed from vital organs, but not from prostate cancer. These characteristics lower the radiation exposure, which is caused by a therapeutic radioisotope-coupled compound, to normal tissue and organs, and thus reduce side effects. In addition, a compound that contains a phenyl group having a coupling force with albumin has an increased residence time in the blood, thereby becoming more accumulated in prostate cancer.

Abstract: Complex compounds of transition metals according to formula (1) wherein the M(CO)3+ tricarbonyl-metal core forms a complex with the cyclopentadienyl anion linked to heterocyclic moieties of the benzothiazole, benzimidazole and benzoxazole families. The compounds exhibit high blood-brain barrier permeability and can be used in the diagnosis and/or treatment of diseases of the Central Nervous System.

Abstract: The invention relates to a marking precursor incorporating a chelator or fluorination group for radiolabelling with 44Sc, 47Sc, 55Co, 62Cu, 64Cu, 67Cu, 66Ga, 67Ga, 68Ga, 89Zr, 86Y, 90Y, 90Nb, 99mTc, 111In, 135Sm, 140Pr, 159Gd, 149Tb, 160Tb, 161Tb, 165Er, 166Dy, 166Ho, 175Yb, 177Lu, 186Re, 188Re, 213Bi and 225Ac or with 18F, 131I or 211At, and one or two biological targeting vectors which are coupled to the chelator or fluorinating group via one or more squaric acid groups.

Abstract: Small molecule radiohalogenated PSMA inhibitors and metal complexes thereof and their use in radioimaging and radiotherapy for treating PSMA-related diseases, including prostate cancer, are disclosed. The combination of small molecule radiohalogenated PSMA inhibitors with a competitive PSMA ligand for reducing off target accumulation of the radiohalogenated PSMA inhibitor also is disclosed.

Abstract: This invention resides in using metal complex-activated particles to bind molecules, polymers and other particles to each other, so as to produce multifunctional conjugates having controlled ratios of two or more different molecules.

Abstract: The present invention relates to a conjugated compound comprising a marker M pharmaceutically acceptable, and a peptide or pseudo-peptide P having at most 30 amino acid residues and able to bind the Low-Density Lipoprotein Receptor (LDLR) and to its use in a method of labelling and/or detecting and/or treating cancerous cells in a subject by administration of the conjugated compound to the subject an analysis of the presence and/or the amount of marker.

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.

Abstract: Provided herein is a one-step method for chelating actinium-225 to a construct comprising a chelator linked to a bio-molecule, such as, an antibody or monoclonal antibody, via a bifunctional ligand in, for example, a 3-arm configuration. Also provided are methods for increasing the radiochemical yield of an actinium-225-chelant-biomolecule complex and for producing a high specific activity actinium-225 complex. The chelation is performed at a physiological temperature, about 37° C. Also provided are high specific activity actinium-225 complexes, that is, actinium-225 chelated to the chelator-biomolecule construct and pharmaceutical compositions thereof. Further provided are methods of treating a neoplastic disease or disorder with the actinium-225 complexes.

Abstract: The present application provides methods of functionalizing an organ or tissue of a mammal by administering a nutrient (e.g., peracetylated N-azido galactosamine Ac4GalNAz) to the mammal or by culturing an organ or tissue in a bioreactor containing such nutrient. The present application also provides methods of selectively functionalizing extracellular matrix (ECM) of an organ or tissue of a mammal by administering a nutrient (e.g., peracetylated N-azido galactosamine Ac4GalNAz) to the mammal. In some aspects, the present application provides a decellularized scaffold of a mammalian organ or tissue comprising an extracellular matrix, wherein the extracellular matrix of the decellularized scaffold is functionalized with a chemical group that is reactive in a bioorthogonal chemical reaction, such as an azide chemical group. The present application also provides biological prosthetic mesh and mammalian organs and tissues for transplantation prepared according to the methods of the application.

Abstract: Disclosed are a method of measuring concentration distribution of boron for boron neutron capture therapy (BNCT) using magnetic resonance imaging (MRI) alone and a treatment planning method for BNCT. The methods include (a) acquiring an anatomical image of a patient and measuring a boron concentration from magnetic resonance (MR) data, (b) extracting a boron concentration change prediction parameter of the patient and predicting the concentration over time, (c) calculating and verifying a boron distribution prediction value estimated by boron imaging and spectral analysis, and (d) deriving an optimal time for BNCT based on the verified results.

Abstract: Disclosed herein is a method for coupling a first compound having the formula (I) with a second compound that contains a carbonyl group. Also disclosed herein are compounds that can be formed by this method, and uses for such compounds.

Abstract: Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer are disclosed.

Abstract: In general, the patent herein is a radioactive chemical which attaches to the virus and releases radiation which kills the virus. Specifically, the chemical is an alpha-ketoamide designed to attach to the virus. However, instead of 2 bromine atoms, Iodine-131 is at the location of where the bromine atoms would have been. Iodine-131 is a radioactive element which releases ionizing radiation. The virus with which this radioactive chemical is designed for is the COVID-19 coronavirus, although the patent is for any virus. Since, modifications can be made in chemical structure and radioactive chemical species, the patent is for any and all chemicals which contain any type of radioactive element to kill or disrupt any type of virus.

Abstract: The present invention relates to a ligand-SIFA-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.

Abstract: The subject matter disclosed herein relates generally to cancer therapy and to anti-cancer compounds and imaging agents. More specifically, the subject matter disclosed herein relates to agents that target MC1R and their use in the treatment of cancer. Methods of screening for MC1R targeted agents are also disclosed.

Abstract: The present invention relates to methods of treating female reproductive tract irritation (such as pain and pruritus) or/and inflammation.

Abstract: This disclosure relates to compositions comprising substituted iminodiacetic acid ligands and metal tricarbonyl complexes containing the ligands and derivatives thereof. In certain embodiments, the metal tricarbonyl complexes are used as radioisotope tracers such as renal tracers. In certain embodiments, the metal complexes comprise 99mTc or Re. In certain embodiments, the ligands are substituted with a fluorine, a fluorine-18(F18) radioisotope, or other radionuclide.

Abstract: The invention relates to a method for preparing a polymer scaffold that comprises the steps of providing a piece of a fabric of filaments of a first biodegradable or biocompatible polymer, applying a coating of a second polymer to said arrangement of filaments, and stretching the piece along its axis of longitudinal extension, thereby obtaining an aligned microfibrillar scaffold. The invention further relates to a method for providing an artificial tissue, and to a microfibrillar scaffold of aligned filaments obtained by the method of the invention.

Abstract: Compositions and methods for assessing gut function are disclosed. They are designed to provide accurate, rapid, point-of-care or in-community assessment of enteric dysfunction.

Abstract: Provided are methods for multiple administrations of cells for adoptive cell therapy, and for administering cells to subjects having received prior administrations, and compositions and articles of manufacture for use in the methods. The cells generally express recombinant molecules such as recombinant receptors, e.g., chimeric antigen receptors (CARs) and/or other transgenic receptors. The methods can involve administering cells expressing a first or prior receptor(s) and cells expressing a second or subsequent receptor(s), the second or subsequent receptor(s) being distinct from the first, and which generally do not express the first receptor, and/or administering the cells expressing the second receptor to a subject having received the first administration.

Abstract: Disclosed are compositions and methods relating to prostate cancer. In particular, disclosed are bivalent targeting ligands that specifically bind prostate specific membrane antigen and gastrin-releasing peptide receptor. Bivalent binding agents disclosed herein can be used to image a tissue in a subject in need thereof and to diagnose prostate cancer in a subject in need thereof. Bivalent binding agents disclosed herein can be used to treat prostate cancer in a subject in need thereof.

Abstract: The present disclosure provides certain angular tricyclic compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: Provided herein are compositions and methods for treating or preventing metabolic disorders. In particular, provided herein are compositions, methods, and uses of Cyclin-dependent Kinase 6 (CDK6) inhibitors for treating and preventing metabolic diseases (e.g., type II diabetes, obesity, metabolic syndrome, elevated blood pressure, cardiovascular diseases, elevated fasting plasma glucose, and high serum triglycerides).

Abstract: Compositions comprising polymers comprising one or more ketal, monothioketal, and/or thioketal bonds are provided, as well as related methods and kits. In some embodiments, a polymer may comprise one or more repeat units comprising one or more ketal, monothioketal, and/or thioketal bonds and a precursor of a pharmaceutically active agent. The precursor of the pharmaceutically active agent may be located in the backbone or may be a pendant group. The polymer may degrade in certain environments (e.g., aqueous environments, acidic environments, in vivo, etc.) to produce the pharmaceutically active agent and other biocompatible degradation products, such as certain ketones, alcohols, and/or thiols. Regardless of the location of the precursor of the pharmaceutically active agent in the repeat unit(s), the polymer may have a prolonged degradation time and/or release of the pharmaceutically active agent in certain environments.

Abstract: This invention provides a class of dual mode imaging tracer capable of acting both as a fluorescent imaging tracer and a positron emission tomography imaging tracer. Tracers in accordance with this invention generally have a fluorescent core with a boron-fluoride element embedded therein. Exemplary embodiments of the tracer include 18F-labeled BODIPY compounds and derivative thereof. Also provided are tracer kits containing a sterile formulation of a BODIPY dye either in a radio-labeled or pre-labeled state, and methods for imaging heart perfusion using the 18F-labeled dual mode tracers.

Abstract: The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

Abstract: The present invention relates to a peptide thiourea derivative, a pharmaceutically acceptable salt thereof, a radioisotope labeled compound comprising the same, and a pharmaceutical composition for treating or diagnosing prostate cancer comprising the same as an active ingredient. The peptide thiourea derivative of the present invention is excellent in stability in human serum when it is administered in vivo and not only binds well to PSMA expressed in prostate cancer but also inhibits excellently PSMA at a low concentration. Besides, the derivative of the invention has a high water-solubility and can be excreted through the kidney not through the bile passage so that a clear image of the tumor region of prostate cancer can be obtained. Therefore, the derivative of the present invention can be effectively used as a pharmaceutical composition for treating and diagnosing prostate cancer.

Abstract: The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: (A) at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; and (C) at least one dye moiety; wherein said compound has a molecular weight of not more than 5 kDa. Further, the invention refers to a method for producing such compound and to the in vivo and in vitro uses thereof.

Abstract: The invention relates to a method for treating PSMA expressing cancers, wherein the method comprises administering to patient in need thereof an effective amount of one or more Ac-225-radiopharmaceuticals, wherein the effective amount of said one or more Ac-225-radiopharmaceuticals is administered as a dosage of from 25 kBq to 400 kBq/kg of body weight of said patient or wherein the effective amount of said one or more Ac-225-radiopharmaceuticals is administered as a unitary dosage of from 3 MBq to 30 MBq to said patient.

Abstract: The invention provides a method for preparing a technetium-99m tricarbonyl intermediate. The method comprises reacting a manganese carbonyl compound used as a carbon monoxide source with pertechnetate and water to obtain the technetium-99m tricarbonyl intermediate. The method for preparing a technetium-99m tricarbonyl intermediate in an embodiment of the invention can complete the preparation of the intermediate at atmospheric pressure and room temperature. The method is easy to operate, uses easily obtained raw materials, has a high labeling yield, and can be used to prepare various types of technetium tricarbonyl labeled probes.

Abstract: Methods for isolating Pb and/or Pb isotopes from various sources are provided. Compositions comprising Pb and/or Pb isotopes free of certain amounts of various contaminants are also provided.

Abstract: PAMAM dendrimer based CEST imaging agents, pharmaceutical compositions comprising the same and methods of uses thereof are disclosed.

Abstract: The present invention relates to an 18F-labelled compound, and a use thereof. The compound selectively binds to a prostate-specific membrane antigen (PSMA), and enables the acquisition of clear prostate cancer images in a short time when used in positron emission tomography (PET).

Abstract: The present invention relates to novel compounds of the formula (II) that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.

Abstract: Systems and methods for magnetic resonance imaging (“MRI”) of multiple different nuclear spin species using the same radio frequency (“RF”) coil are described. Generally, multiple different nuclear spin species are imaged using the same RF coil by using an MRI system whose magnetic field can be rapidly ramped between a number of different, and arbitrary, magnetic field strengths. The magnetic field of this MRI system can be ramped to different values in reasonable amounts of time (e.g., in a time frame that is feasible within an imaging study).

Abstract: In various aspects, embodiments of the present invention are directed to a series of multivalent dendrons containing a bioactive peptide domain and surface-binding catechol domains. In some embodiments, these multivalent dendrons were obtained through solid phase synthesis and have a strong binding affinity to metal oxide surfaces such as, TiO2, ZrO2, CeO2, and Fe3O4, SiO2, as well as other inorganic surfaces such as hydroxyapatite, silver, fluorapatite, calcium carbonate and gold. These catechol-bearing dendrons provide a fast and efficient method to functionalize a wide range of inorganic materials with bioactive peptides and have the potential to be used in coating orthopaedic implants and fixation devices.

Abstract: The present invention relates to 99mTc-maraciclatide radiopharmaceutical compositions, which are stabilised with a radioprotectant. Also described are kits for the preparation of the radiopharmaceutical compositions, as well methods of preparing such compositions from the kit. The invention also includes methods of imaging the mammalian body using the radiopharmaceutical compositions.

Abstract: The invention provides a novel trifunctional targeting construct and related compositions and methods that are useful in therapeutic, diagnostic (including imaging) of various biological and/or pathological conditions and diseases such as cancers and diabetes. The trifunctional targeting construct of the invention provides enhanced clearing step and reduced non-specific background via complete clearance of undesired antibody conjugates.

Abstract: The present invention is directed to novel non-invasive diagnostic took to dispose numerous disease states and/or conditions. The presets invention, represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these disease states. The novel imaging probe is capable of detecting infected cells, as well tissue. The methods described herein are able to diagnose, treat and/or monitor the therapy of numerous diseases and conditions including atherosclerosis, atherothrombosis, cerebral vascular disease, cerebral ischemia, cerebral infarct and meningitis as well as pneumonitis, pericarditis, multiple sclerosis, lupus erythematosus and pancreatitis, among others.

Abstract: Methods for adjusting the solubility of a botanical oil in water, along with the resulting modified botanical oil and related products (e.g., treatment compositions, wipes, absorbent articles, etc.) are provided. In one embodiment, the method includes reacting the botanical oil to form a reactive product (e.g., having a hydroxyl group); and attaching a hydrophilic end group (e.g., a carboxylic acid, a carboxylic acid salt, a sugar, etc.) on the reactive product to form a modified botanical oil. The modified botanical oil generally, in most embodiments, has a greater solubility in water than the botanical oil (e.g., a solubility in water of about 10 grams per 100 grams of water or greater, such as completely soluble in water). The botanical oil includes, in one particular embodiment, an essential oil, such as those essential oil that include at least one terpene compound.

Abstract: The present invention relates to compounds according to Formula I and Formula IV. These compounds display very good binding affinities to the PSMA binding sites. They can be labeled with [68Ga]GaCl3 with high yields and excellent radiochemical purity. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula IV, or a pharmaceutically acceptable salt thereof.

Abstract: Among the various aspects of the present disclosure is the provision of compositions and methods for imaging and treating subjects with amyloidosis or multiple myeloma with or without amyloidosis.

Abstract: Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.

Abstract: This disclosure relates to compositions comprising substituted iminodiacetic acid ligands and metal tricarbonyl complexes containing the ligands and derivatives thereof. In certain embodiments, the metal tricarbonyl complexes are used as radioisotope tracers such as renal tracers. In certain embodiments, the metal complexes comprise 99mTc or Re. In certain embodiments, the ligands are substituted with a fluorine, a fluorine-18 (F18) radioisotope, or other radionuclide.

Abstract: The present invention concerns a positron emission tomography (PET) contrast agent or imaging tracer comprising a red blood cell (RBC) internally labeled with 2-deoxy-2-(18F)fluoro-D-glucose (FDG); a method of preparing RBCs of a human or non-human animal for PET, comprising labeling RBCs in vitro with FDG to produce FDG-labeled RBCs; a method for in vivo imaging of RBCs using PET, comprising: introducing RBCs internally labeled with FDG (FDG-RBCs) into the circulatory system of a human or non-human animal subject in vivo; and PET imaging the introduced FDG-RBCs in the subject; a composition useful for labeling RBCs, and a kit for labeling RBCs.