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.

Abstract: Tin-117m somatostatin analogues or antagonist are used to treat tumors and symptoms associated with these tumors which express somatostatin receptors, such as gastroenteropancreatic neuroendocrine tumors. The tin-117m somatostatin receptor binding compounds can be administered at a dosage which is effectively apoptotic and not necrotic. Also, if desired, it can be administered at a dose that is necrotic and/or induces necrosis, but only to cells within 290 microns of the tin-117m atom. A novel somatostatin analogue is also disclosed, as well as novel methods to produce the tin labeled analogues and antagonists.

Abstract: In a preferred aspect, organic coating compositions, particularly antireflective coating compositions for use with an overcoated photoresist, are provided that comprise 1) one or more glycidyl groups; and 2) one or more aromatic groups that each comprises two or more substituents that comprise hydroxy, thiol and/or amine moieties. Catechol-containing polymers and methods for producing same also are provided.

Abstract: Disclosed are compositions and methods for mitigating a tolerance effect from ingestion of cannabis-based medicines in human subjects, for example, subjects having an increased risk of unresponsiveness to one or more therapeutic agents such as, for example, antidepressants and antianxiety drugs. In some methods, the human subjects have been previously treated with one or more therapeutic agents such as, for example, antidepressants and antianxiety drugs, and have developed at least partial tolerance to the one or more therapeutic agents.

Abstract: Provided is a method for producing flutemetamol including the steps of: reacting a precursor compound represented by a predetermined general formula with a radioactive fluoride to obtain a 18F labeling compound represented by a predetermined general formula; allowing a strong base to act on the reaction mixture of the above step containing the precursor compound and the 18F labeling compound; after the above step, purifying the 18F labeling compound using a reverse phase solid phase extraction cartridge; and removing a protective group to obtain [18F]flutemetamol.

Abstract: The present invention provides a multifunctional 2-D and 3-D matrix for propagation of stem cells. In particular, a chitosan-based biomaterial scaffold is engineered to promote CNS regeneration from primitive neural precursors by stabilizing a recombinant protein, fibroblast growth factor to preserve the cardinal properties of stem cells. The matrix, is further modified by the addition of either the extracellular matrix protein fibronectin or the small peptide RGD or IKVAV. A method to manufacture an injectable multifunctional microsphere scaffold is also disclosed that is suitable as a vehicle for cell transplantation to repair traumatic brain injuries.

Abstract: Multifunctional chelators, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.

Abstract: Disclosed herein are a multivalent saccharide complex, a radioactive multivalent saccharide complex contrast agent and use thereof. The multivalent saccharide complex has a chelator, a linker, and glucose, and is configured to diagnose and evaluate the therapeutic effect of cancers.

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 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 complexes comprising a PSMA targeting compound linked to a radionuclide, such as 212Pb or 227Th. 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: A method of analyzing biological data containing expression values of a plurality of polypeptides in the blood of a subject. The method comprises: calculating a distance between a segment of a curved line and an axis defined by a direction, the distance being calculated at a point over the curved line defined by a coordinate along the direction. The method further comprises correlating the distance to the presence of, absence of, or likelihood that the subject has, a bacterial infection. The coordinate is defined by a combination of the expression values, wherein at least 90% of the segment is between a lower bound line and an upper bound line.

Abstract: A method for performing an imaging scan of a subject includes positioning a narrow field-of-view camera at a first imaging position to acquire a first set of imaging information of a first object of interest, positioning the narrow field-of-view camera at a second imaging position to acquire a second set of imaging information of a second object of interest, determining emission counts for the first and second sets of imaging information, and utilizing the determined emission counts to generate a value that indicates a probability of a successful medical procedure being performed on the subject.

Abstract: Synthesis and characterization of starch based pH-responsive nanoparticles for controlled drug delivery are described. Polymethacrylic acid grafted starch (PMAA-g-St) nanoparticles with various molar ratio of starch to MAA were synthesized by a new one-pot method that enabled simultaneous grafting of PMAA and nanoparticle formation in an aqueous medium. NMR data showed that polysorbate 80 was polymerized into the graft polymer. Nanoparticles were relatively spherical with narrow size distribution and porous surface morphology and exhibited pH-dependent swelling in physiological pH range. The particle size and magnitude of volume phase transition were dependent on PMAA content and formulation parameters such as surfactant levels, cross-linker amount, and total monomer concentration. The results showed that the new pH-responsive nanoparticles possessed useful properties for controlled drug delivery.

Abstract: Somatostatin derivative compounds of general formula (I) that may be readily labelled with the isotope fluorine-18 and that have affinity and selectivity for cellular somatostatin receptors are provided. The labelled compounds are useful clinically as radioactive tracers in various in vivo imaging applications (for example, using positron emission tomography (PET) and related techniques) to detect somatostatin-expressing cells and tissues, including tumors, or as therapeutic agents.

Abstract: Copper-catalyzed radiofluorination of iodonium salts, iodonium salts, and compounds obtained by copper-catalyzed radiofluorination of iodonium salts are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.

Abstract: The invention provides an antibody or fragment thereof that specifically binds to human endothelial vascular cell adhesion molecule-1 (VCAM-1), wherein the antibody or fragment thereof binds to the extracellular domain of VCAM-1, and wherein the antibody or fragment thereof binds to VCAM-1 when expressed on endothelial cells, wherein the antibody or fragment thereof is a human or humanized antibody, or fragment thereof.

Abstract: Disclosed herein are globular nanostructures having a hydrodynamic diameter (Dh) of 8-100 nm comprising a central part and a peripheral part, wherein said central part has a calculated diameter (Dc) of 6-90 nm and said peripheral part has an estimated thickness (Tp) so that Dh=Dc+2Tp, wherein said central part comprises: (i) a crosslinked polymeric framework comprising monomer residues wherein at least 30% by number of the monomer residues have crosslinked thereby forming the crosslinked polymeric framework and/or (ii) a branched polymeric framework comprising monomer residues wherein the number of branch points is at least 30% of the number of monomer residues, wherein said central part comprises chelating groups of which at least 4 allow chelation of at least one multiply charged cation, wherein said chelating groups are independently selected from the group consisting of —COOR1, —P?O(OR1)(OR2), and —S(?O)2OR1, wherein R1 and R2 are independently selected from the group consisting of a negative charge, H, a

Abstract: The present disclosure relates generally to a mucoadhesive nanoparticle delivery system. The nanoparticles are formed from amphiphilic macromolecules conjugated to a mucosal targeting moiety in such a manner that the surface of the nanoparticle is coated with the targeting moiety. The surface density of the targeting moiety can be tuned for adjustable targeting of the nanoparticles to a mucosal site without substantially compromising the stability of the particles. The particles were found to have high loading efficiency and sustained release properties at the mucosal site. The present disclosure also relates to polymers and macromolecules useful in the preparation of the mucoadhesive nanoparticles, as well as compositions, methods, commercial packages, kits and uses related thereto.

Abstract: The present invention relates to a biopolymer and a cell-harvesting scaffold comprising same, as well as the associated cell-harvesting method that allows said harvesting to be performed in a simple and effective manner by reducing the culture temperature. The present invention also relates to a method for synthesizing said biopolymer.

Abstract: Nanoparticles for a selective, two stage delivery to tumors have been developed. The nanoparticles are initially sized so that they preferentially accumulate in the tumor tissue as a result of leakage through the defective vascular in the solid tumors. Once in the tumor tissue, the nanoparticles are cleaved hydrolytically and/or by enzymatic cleavage over time to release smaller nanoparticles carrying therapeutic, prophylactic or diagnostic agents into the necrotic interior of the tumors. This provides a simple, elegant and highly effective means of delivery drug selectively not just to tumors generally, but, more importantly, into the poorly vascularized necrotic interiors which drugs are normally unable to penetrate. The nanoparticles have a number of advantages: less toxicity due to selective accumulation only in the tumors; access into the poorly vascularized necrotic interiors of the tumor; and sustained release over a period of time within the tumor.

Abstract: Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.

Abstract: The present invention relates to a novel delivery system for delivering therapeutic agents into living cells, and more particularly, to novel chemical moieties that are designed capable of targeting and/or penetrating cells or other targets of interest and further capable of binding therapeutic agents to be delivered to these cells, and to delivery systems containing same.

Abstract: A magnetic anti-counterfeit label and identification system thereof, wherein the magnetic anti-counterfeit label comprises a substrate, a magnetic ink layer, an opaque layer and a protective coating. The magnetic ink layer covers the substrate. The opaque layer covers the magnetic ink layer in order to visually hide the characters, bar code, and other patterns which are printed using magnetic ink. Additionally the protective coating is composed of a polymer or a metal layer, which covers opaque layer. This identification system comprises a magnetic sensor for sensing the magnitude of the magnetic field emitted by the magnetic anti-counterfeit label, a permanent magnet or an electromagnet for magnetizing the magnetic anti-counterfeit label, a digital processing circuit that is electrically connected to the magnetic sensor, and a frame that is used to hold the magnetic sensor and the digital processing circuit. The digital processing circuit outputs a code corresponding to the magnetic anti-counterfeit label.

Abstract: Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.

Abstract: There is provided a lysine oligomer derivative, wherein an ?-amino group and a carboxyl group of lysines are linked via a peptide bond, and a group capable of generating or absorbing electromagnetic wave is bonded to a C-terminal carboxyl group, an N-terminal amino group and/or an ?-amino group. This lysine oligomer derivative has the characteristic of specifically accumulating in the cartilage matrix and can generate or absorb an electromagnetic wave, and is, therefore, useful as a cartilage tissue marker.