Abstract: A method for predicting the likelihood of successful treatment of cancer with a topoisomerase inhibitor and/or a DNA damaging agent and/or a DNA methyltransferase inhibitor and/or a HDAC inhibitor comprises the steps of: (a) determining the methylation status of a RecQ helicase family gene in a sample obtained from a subject, wherein if the RecQ helicase family gene is methylated the likelihood of successful treatment is higher than if the RecQ helicase family gene is unmethylated; and/or (b) determining the expression levels of a RecQ helicase family gene in a sample obtained from a subject, wherein a reduced level of expression of the RecQ helicase family gene indicates the likelihood of successful treatment is higher than if the RecQ helicase family gene is expressed at a higher level. Corresponding kits are also useful in predicting the likelihood of successful treatment of cancer. The most preferred RecQ helicase family member is WRN.

Abstract: Methods of determining rate of biosynthesis or breakdown of biological molecules from metabolic derivatives and catabolic products are disclosed herein. In particular, methods of measuring the rates of biosynthesis and breakdown of biological molecules inaccessible or not easily accessible to direct sampling by sampling metabolic derivatives and catabolic products in accessible biological samples are disclosed herein.

Abstract: The present invention provide a method for measuring and assessing the capacity in an individual subject to metabolize a variety of fluorouracil drugs, such as 5-fluorouracil, which are degraded in the pyrimidine metabolic pathway, and a preparation useful for the measurement and assessment. The present invention can be carried out by: administering a preparation for determining pyrimidine metabolic capacity comprising as an active ingredient a pyrimidine compound or pyrimidine metabolic compound that acts as a substrate for a pyrimidine metabolizing enzyme, in which at least one of the carbon, oxygen, and nitrogen atoms is labeled with an isotope; and assessing in vivo pyrimidine metabolic capacity based on the behavior of an excreted metabolite.

Abstract: The present invention relates to novel compounds suitable for or already radiolabelled with 18F, methods of making such compounds and use of such compounds for diagnostic imaging.

Abstract: Methods of making and using labeled macrophages are described.

Abstract: Disclosed herein are novel radiolabeled nucleosides and methods for detecting cellular proliferation in a mammal, the method comprising administrating an effective amount of a radiolabeled nucleoside; the method comprising: a) administering to the mammal a diagnostically effective amount of the nucleoside to the mammal; b) allowing the nucleoside to distribute into the effective tissue; and c) imaging the tissue, wherein an increase in binding of the compound to tissue compared to a normal control level of binding indicates that the mammal is suffering from a disease involving cellular proliferation.

Abstract: The instant invention provides a method for diagnosing an infection in a subject by administering to the subject a compound suitable for imaging which binds to a thymidine kinase present in the infecting organism, and obtaining an image of the subject to determine the presence and location of the compound, wherein a localization of the compound is indicative that the subject has an infection.

Abstract: The invention provides cobalamin compounds linked to a neutron capture therapy target (e.g. Boron-10 or Gadolinium-157), and optionally linked to a detectable moiety, as well as pharmaceutical compositions comprising the compounds, and methods for using the compounds in medical diagnosis and therapy.

Abstract: New diagnostic agents for positron emission tomography (PET) and methods for use of such agents for imaging of human or animal tissue are described, wherein a primary active component of such agents is a radiolabeled halogenated xanthene or halogenated xanthene derivative. Preferably, the radiolabeled halogenated xanthene is radiolabeled Rose Bengal or a functional derivative of Rose Bengal.

Abstract: The present invention refers to novel conjugate molecules and their use or the transport of nano- and macromolecular structures into cells and/or the nucleus. More particularly, the present invention refers to conjugate molecules containing a carrier, preferably thiopyridyl moieties, and a cargo moiety. Thereby, the thiopyridyl moiety is bound to the cargo moiety to act as a carrier, particularly for efficient intracellular and/or intranuclear delivery of drugs, nano-or macromolecular structures, etc. The novel conjugate molecules are provided for the manufacture of a medicament for gene therapy, apoptosis, or for the treatment of diseases such as cancer, autoimmune diseases or infectious diseases.

Abstract: A compound useful for in vivo imaging of organs and tumors is provided of formula: wherein is a cobalamin, is derived from a corrin carboxylic acid group of said cobalamin, Y is a linking group and X is a chelating group, optionally comprising a detectable radionuclide or a paramagnetic metal ion, and n is 1-3.

Abstract: The present invention provides multifunctional magnetic nanoparticle probe compositions for molecular imaging and monitoring, comprising a nucleic acid or polypeptide probe, a delivery ligand, and a magnetic nanoparticle having a biocompatible coating thereon. The probe compositions may further comprise a fluorescent or luminescent resonance energy transfer moiety. Also provided are compositions comprising two or more such multifunctional magnetic nanoparticle probes for molecular imaging or monitoring. In particular, the nucleic acid or polypeptide probes bind to a target and generate an interaction observable with magnetic resonance imaging (MRI) or optical imaging. The invention thereby provides detectable signals for rapid, specific, and sensitive detection of nucleic acids, polypeptides, and interactions thereof in vivo.

Abstract: The invention relates to new side chain-fluorinated 3?-deoxythymidine derivatives of the general formula I or physiological acceptable esters thereof, wherein R?CH218F; CH18F2; CH2F or CHF2 and Y?H, N3 or Hal. The invention also relates to a simple and efficient method for the preparation of these 3?-deoxythymidines of formula I and to the use of the 18F-containing compounds of formula I or of a pharmaceutical composition comprising these compounds for the diagnosis of tumors in positron emission tomography (PET).

Abstract: The invention discloses the nanoparticles composed of chitosan, poly-glutamic acid, and at least one bioactive agent characterized with a positive surface charge and their enhanced permeability for paracellular drug delivery.

Abstract: The present invention is directed to metal chelating conjugates for use as metallopharmaceutical diagnostics or therapeutic agents. Specifically, conjugates of the present invention include a carrier, a metal coordinating moiety, and a urea linkage chemically linking the metal coordinating moiety to the carrier. The carrier is generally utilized for targeting the conjugate to a biological tissue or organ.

Abstract: Compounds of the formula (I) are disclosed: 18F—(CHR)n(CH2)mCHO ??(I) in which n and m are independently 0 and 1 with at least one of n and m being 1, and R (if present) is a hydrogen atom or a methyl group, subject to the proviso that if n is 1 and R is methyl then m is 0. Synthesis of the compounds is described together with their use in radiolabelling reactions, e.g. for the radiolabelling of peptides to facilitate detection by Positron Emission Tomography (PET) imaging. The preferred compound is [18F]Fluoroacetaldehyde.

Abstract: Described are methods for stabilizing radionuclide-containing compositions against degradation caused by free radicals generated from the radionuclide. Iodide ions stabilize the radionuclide-containing compositions by acting as scavengers to generated free radicals, thus, preventing or lessening degradation therefrom. Among the preferred radionuclide-containing compositions to be stabilized are complexes of a complexing agent with a radionuclide complexed therewith, such as a diagnostic agent having a specific binding peptide linked to a metal ion-complexing moiety which is complexed with a radionuclide, such as technetium-99m (Tc-99m).

Abstract: The present invention relates in part to a method of imaging cardiovascular plaque formation in a mammal comprising administering to the mammal an effective amount of 18F-2-fluorodeoxy-D-glucose and then detecting the 18F-2-fluorodeoxy-D-glucose.

Abstract: The present invention relates to formulations for use in medical or diagnostic procedures comprising a stabilizing agent alone or in combination with an osmotic agent. In one embodiment, the stabilizing agent is a natural hydrocolloid, preferably locust bean gum, and the osmotic agent is a sugar-based compound, preferably mannitol. The present invention also relates to formulations and methods for distending an anatomic segment. The present invention further relates to formulations and methods for delineating an anatomic segment on a diagnostic image, for example. The formulations of the present invention are especially suitable for use with diagnostic imaging procedures including, but not limited to magnetic resonance imaging (MR), computer assisted tomography (CT), and CT-PET (Position emission tomography), as well as other medical and therapeutic uses.

Abstract: Materials and methods are provided for making nanoparticles having a core including metal and/or semiconductor atoms, which core is covalently linked to a plurality of ligands comprising a RNA ligand. The RNA ligands may include siRNA or miRNA. Also provided are uses of these nanoparticles in therapy and diagnosis.

Abstract: It is intended to provide a radioactive diagnostic imaging agent comprising a radioactive halogen-labeled compound as an active ingredient, in which the active ingredient is prevented from radiolysis and its stability is improved. This is achieved by adding a biologically-acceptable sugar or sugar alcohol to the radioactive diagnostic imaging agent in an amount effective to prevent radiolysis. The amount of the sugar or sugar alcohol to be added is preferably 10 (mmol/L)/GBq/mL or more, and more preferably 50 (mmol/L)/GBq/mL or more. The sugar is preferably selected from the group consisting of erythrose, threose, ribose, arabinose, xylose, lyxose, allose, altrose, glucose, mannose, gulose, idose, galactose, talose, erythrulose, ribulose, xylulose, psicose, fructose, sorbose, and tagatose. The sugar alcohol is preferably selected from the group consisting of erythritol, xylitol, sorbitol, and mannitol.

Abstract: The present invention relates to methods for the detection and therapy of active atheromatous plaques, and in particular vulnerable plaques, whereby immune modulators are used to increase the uptake of diagnostic or therapeutic compositions by the inflammatory cells associated with such plaques.

Abstract: The present invention is directed to bioconjugates of complexes represented by the formula: wherein R, R?, R1, R?1, R2, R?2, R3, R?3, R4, R?4, R5, R?5, R6, R?6, R7, R?7, R8, R?8, R9, R?9, M, X, Y, Z and n are defined herein for use as contrast agents in diagnostic imaging.

Abstract: A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.

Abstract: Diagnostic and therapeutic compositions in the form of complexes for enhancing transmembrane transport of a diagnostic or therapeutic agent and methods for their use. The complexes contain the ?, ?, or bis isomers of folate receptor-binding analogs of folate, a metal chelated by a ligand, and in one embodiment, a chemotherapeutic agent.

Abstract: The present invention relates to a radionuclide-chitosan complex solution and its preparation method, and more particularly to the radionuclide-chitosan complex solution having a viscosity of 300˜2,400 cps, comprising an aqueous chitosan solution or a freeze-dried chitosan labeled with a radionuclide. The radionuclide-chitosan complex solution according to the present invention has a stable gelation state at a target region when injected into the body while maintaining a labeling yield of radioisotope to chitosan above 99%. Side effects may be minimized and treatment efficiency may be increased when injected to a patient.

Abstract: Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

Abstract: The invention provides a novel class of xanthene dyes, some of which are functionalized to allow their coupling to conjugation partners of interest, e.g. biomolecules, drugs, toxins and the like. Also provided are conjugates of the dyes, methods of preparing and using the dyes and their conjugates and kits including the dyes and their conjugates.

Abstract: A nutritional supplement includes a first formulation including minerals: chromium polynicotinate, magnesium glycinate, manganese sulfate, selenium, vanadyl sulfate, zinc gluconate, copper gluconate, iodine, and boron; and vitamins: vitamins C, B1, B2, B3, B6, and B12, biotin, alpha-lipoic acid, and folic acid. The second formulation, packaged separately from the first, includes essential fatty acids: walnut oil, flax seed oil, safflower oil, sesame seed oil, and pumpkin seed oil; and vitamins: vitamin E and vitamin Q-10. A method for improving metabolic function includes consuming the first and second formulation. A method of formulating a composition for improving metabolic function includes packaging together the first formulation and packaging together and separately from the first formulation the second formulation. A method for assisting a patient to improve metabolic function includes prescribing the first formulation and the second formulation to be taken separately from the first formulation.

Abstract: Positron emitting compounds and methods of their production are provided. The compounds have the formula: (F)m G (R)n wherein each R is a group comprising at least one carbon, nitrogen, phosphorus or sulfur atom and G is joined to R through said carbon, nitrogen, phosphorus or sulfur atom; G is silicon or boron; m is 2 to 5 and n is 1 to 3 with m+n=3 to 6 when G is silicon; m is 1 to 3 and n is 1 to 3 with m+n=3 to 4 when G is boron; and wherein the compound further comprises one or more counterions when the above formula is charged; and wherein at least one F is 18 F.

Abstract: The present invention provides novel imaging agents for clinical diagnosis of injuries and diseases, in the form of a radionuclide in spatial proximity to a substantially pure stereoisomer of a fatty acid analog. The invention also provides methods for using the novel imaging agents, and kits containing one or more of the novel imaging agents of the invention.

Abstract: Novel compositions and methods are provided for identifying agents which affect chromosomal stability and aging.

Abstract: The invention discloses the nanoparticles composed of chitosan, poly-?-glutamic acid, and at least one bioactive agent characterized with a positive surface charge and their enhanced permeability for paracellular drug delivery.

Abstract: Disclosed are methods for manufacturing radiohalogen-labeled steroids, nucleosides, nucleotides and proteins, for example, pyrimidines and proteins. Methods according to the example embodiments specific to pyrimidines includes dissolving a halogenated pyrimidine to obtain an initial solution, adding bis(tributyltin) and triphenylphosphine palladium to produce a catalyzed solution, heating the catalyzed solution under conditions sufficient to induce a reaction that produces an intermediate solution including a stannylated pyrimidine compound, removing substantially all of the first solvent from the intermediate solution to obtain an intermediate composition, purifying the resulting solution to obtain a purified composition including a stannylated pyrimidine, reacting the stannylated pyrimidine compound with a radiohalogen in a buffered reaction mixture to produce the radiohalogenated pyrimidine, adding an antioxidant and extracting the radiohalogenated pyrimidine from the reaction mixture.

Abstract: A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.

Abstract: Cyclic amidinium containing compounds and their methods of preparation are described. Compositions containing these compounds facilitate delivery of biologically active polymers to cells in vitro and in vivo.

Abstract: Radiolabeled conjugates are disclosed which have a component that is effective to target tumor cells, which cells selectively take up and degrade the conjugate, thereby delivering to the tumor cell nucleus a radioisotope capable of being incorporated into the nuclear material, so as to produce a cytotoxic effect and/or to render the cell detectable by radioimaging.

Abstract: A method of simply and quickly determining ?-ray releasing nuclides having long half-life without carrying out a chemical separation is provided. By inputting a data of pulses incident to an ?-ray detector in a computer, obtaining time distribution of the incident pulses by using a very short time measuring timer and plotting, and fitting the linear originated in a random event corresponding to the background and the non-linear originated in the correlated events of parent nuclides-progenies by using the least squares method, the whole generating probability P (t) from the parent nuclide to the progeny thereof is obtained. By subtracting the random events portion from the P(t), the correlated events portion is extracted. The radioactivity per unit can be obtained by dividing the extracted correlated events portion by the measured time, the amount of the supplied sample and the counting efficiency.

Abstract: Diagnostic and therapeutic compositions in the form of complexes for enhancing transmembrane transport of a diagnostic or therapeutic agent and methods for their use. The complexes contain the ?, ?, or bis isomers of folate receptor-binding analogs of folate, a metal chelated by a ligand, and in one embodiment, a chemotherapeutic agent.

Abstract: The invention provides detectably labeled cobalamin derivatives which are useful for medical treatment and diagnosis.

Abstract: The invention provides compounds having increased or reduced immunostimulatory effect, said compounds comprising a CpG dinucleotide and an immunomodulatory moiety wherein the increased or reduced immunomodulatory effect is relative to a similar compound lacking the immunomodulatorv moiety.

Abstract: A compound useful for in vivo imaging of organs and tumors is provided of formula: wherein is a cobalamin, is derived from a corrin carboxylic acid group of said cobalamin, Y is a linking group and X is a chelating group, optionally comprising a detectable radionuclide or a paramagnetic metal ion, and n is 1–3.

Abstract: This invention provides compounds containing a 2-deoxy-2-amino-?-D-glucopyranose (glucosamine) glycosidically linked to a cyclic aminoalkyl (aglycon) group. The invention further provides methods for inducing an immune response using the compounds of the present invention in the presence or absence of an antigen. In addition, methods for treating disease with the compounds of the present invention with or without an antigen are also provided in this invention.

Abstract: The invention relates to compounds and methods for targeting radionuclide-based imaging agents to cells having receptors for a vitamin, or vitamin receptor binding derivative or analog thereof, by using such a vitamin as the targeting ligand for the imaging agent. The invention provides a compound of the formula for use in such methods. In the compound, V is a vitamin that is a substrate for receptor-mediated transmembrane transport in vivo, or a vitamin receptor binding derivative or analog thereof, L is a divalent linker, R is a side chain of an amino acid, M is a cation of a radionuclide, n is 1 or 0, K is 1 or 0, and the compound can be in a pharmaceutically acceptable carrier therefor. The vitamin-based compounds can be used to target radionuclides to cells, such as a variety of tumor cell types, for use in diagnostic imaging of the targeted cells.

Abstract: An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1–8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

Abstract: The invention provides methods for modulating the immune response caused by CpG dinucleotide-containing compounds. The methods according to the invention enables both decreasing the immunostimulatory effect for antisense applications, as well as increasing the immunostimulatory effect for immunotherapy applications.

Abstract: Radiolabeled annexin and modified annexin conjugates useful for imaging vascular thrombi are described. Methods for making and using such radiolabeled annexin conjugates are also provided.

Abstract: The invention provides methods for modulating the immune response caused by CpG dinucleotide-containing compounds. The methods according to the invention enables both decreasing the immunostimulatory effect for antisense applications, as well as increasing the immunostimulatory effect for immunotherapy applications.

Abstract: An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1–8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

Abstract: A process for stabilizing a sensitive substance; (a) plating a sensitive substance onto a solid carrier under a controlled atmosphere to reduce loss of the sensitive substance; (b) encapsulating the plated material under controlled atmosphere and airflow to reduce volatilization during the process and stabilize the sensitive substance.