Abstract: A radioactive material containing chitosan for inhibiting cancer and a preparation method thereof are revealed. The adioactive material containing chitosan is formed by using SOCTA chelating agent to connect chitosan and radionuclides such as 188Re, and Tc-99m etc. The preparation method of the radioactive material containing chitosan includes the steps of: prepare SOCTA-Chitosan compound; and prepare M(radionuclide)-SOCTA-Chitosan compound. By biocompatibility and clotting in alkaline environment of human blood of chitosan, the radioactive material containing chitosan is injected into cancer and staying there for a long time so as to achieve effectively treatment.

Abstract: A method of measuring the efficacy of an anticancer agent in generating abasic (AP) sites in DNA of cancer cells of a subject includes administering to the subject an anticancer agent that generates AP sites in at least one cancer cell and an AP endonuclease inhibitor probe. The AP endonuclease inhibitor probe includes a detection moiety for detecting the probe in the subject. The amount of probe bound to cancer cells of the subject is then measured. The amount of probe bound to cancer cells of the subject is indicative of efficacy of the anticancer agent in generating AP sites in cancer cells of the subject.

Abstract: The present invention relates to an active targeted water-solubility macromolecule polymer, conjugate with interferon and pharmaceutical composition comprising the conjugate. The targeted agent includes, for example, glucose, galatose and the like, as well as their derivates. The conjugate of the present invention is well in water-solubility and have long physiological cycle half-life period, and have specific recognition to pathology organize, improved and increased medication effect of interferon to Hepatitis B, Hepatitis C etc. infectivity sickness and cancer, infect complication etc.

Abstract: The invention relates to Fmoc (9-fluorenyl-methoxycarbonyl)-based polymeric conjugates. These conjugates are useful for extending the in-vivo circulation of protein and peptide drugs.

Abstract: Methods for significantly lowering the carbon-14 content, particularly of DNA and histones in vertebrates, especially humans, to significantly below normal background levels and thereby reduce chromosomal damage using dietary supplements based on low radiocarbon DNA and histone precursors optionally including selected low radiocarbon amino acids, preferably including those which contribute the largest share of histone carbon atoms. Administration of the supplements during the earliest and/or most active growth stages of life is particularly beneficial. Components of the low radiocarbon supplements can be produced using a photobioreactor, an aqueous reaction medium and low radiocarbon carbon dioxide. The photobioreactor can be integrated into a body of water or can comprise a mobile, floating structure. Low radiocarbon by-products of photosynthesis can be recycled for use in non-photosynthetic fermentation processes to increase the yield of desirable supplement components.

Abstract: The present invention relates to a chelating agent of the general formula: (I), wherein m is 0 or 1; X is NR4 or S; Y is SR5, NHR5 or P(R5)2; R1 and R3 are the same or different and are selected from H, alkyl or aryl; R2 is H, COOH, NHR6 or (CH2)nCOOR6; R4 is H, alkyl, aryl, (CH2)nCOOR6 or (CH2)nOR6; R5 is H, alkyl, aryl, (CH2)nCOOR6 or (CH2)nOR6, R6 is H, alkyl or aryl; n is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; and when R1?R3?CH3, R2, R4 and R5 are not all three H. The invention further relates to a method and kit for the preparation of radiolabeled biomolecules while using the chelating agent.

Abstract: The present invention relates to improved chelator conjugates with biological targeting molecules, suitable for forming metal complexes with radiometals. The radiometal complexes, especially with the radiometal 99mTc, are useful as radiopharmaceuticals.

Abstract: The invention relates to a method for improving stability of radiopharmaceutical precursors, and in particular non radiolabelled nucleoside derivatives which are used as precursors for production of radiolabelled nucleoside derivatives for use in in vivo imaging procedures such as positron emission tomography (PET). The invention further includes formulations of radiopharmaceutical precursors, and cassettes for automated synthesis apparatus comprising the same.

Abstract: Radiolabeled tracers for sodium/glucose cotransporters (SGLTs), their synthesis, and their use are provided. The tracers are methyl or ethyl pyranosides having an equatorial hydroxyl group at carbon-2 and a C1 preferred conformation, radio-labeled with 18F, 123I, or 124I, or free hexoses radiolabeled with 18F, 123I, or 124I. Also provided are in vivo and in vitro techniques for using these and other tracers as analytical and diagnostic tools to study glucose transport, in health and disease, and to evaluate therapeutic interventions.

Abstract: Detection methods, assay kits and reagents are provided for detecting pre-cancerous mammary epithelial cell signatures. The disclosed cell signatures comprise a collection of measurements of at least two characteristics of the mammary epithelial cells. Related imaging and diagnostic methods are also disclosed.

Abstract: Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modified at either the N-terminal or the C-terminal end or at both termini, a carbohydrate unit and a chelator or prosthetic group to provide a complexation of a radioisotope binding or holding the radioisotope. The sst- or SSTR-receptor binding peptidic ligands may also contain one or more multifunctional linker units optionally coupling the peptide, and/or the sugar moiety and/or the chelator and/or the prosthetic group. Upon administering the ligand to a mammal through the blood system the ligand provides improved availability, clearance kinetics, sst-receptor targeting and internalization over the non-carbohydrated ligands.

Abstract: This disclosure relates to compositions for delivering agents to a subject, and in particular, to compositions for delivery of therapeutic agents or diagnostic agents in the presence or absence of targeting moieties. In part, this disclosure relates to compositions comprising a hydrophobic group with a first end and a second end, a first metal binding domain linked to the hydrophobic group, a metal ion capable of being chelated to the first metal binding domain, and an agent linked to a second metal binding domain capable of chelating to the metal ion.

Abstract: The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.

Abstract: The present invention discloses composites which generally comprise a polymeric matrix and a hydrophobic organic compound which is associated with a radioisotope.

Abstract: The invention provides immunomodulatory compounds and methods for immunomodulation of cells and individuals using the immunomodulatory compounds.

Abstract: The present invention discloses a method for the enzyme-mediated, site-specific, in-vivo precipitation of a water soluble molecule in an animal. The enzyme is either unique to tumor cells, or is produced within a specific site (e.g., tumor) at concentrations that are higher than that in normal tissues. Alternatively, the enzyme is conjugated to a targeting moiety such as an antibody or a receptor-binding molecule.

Abstract: The invention relates to molecules for treatment and diagnosis of tumors and malignancies, comprising a tumor seeking biomolecule, which is coupled to an intercalating moiety, which is capable of complexing a metal, which metal is preferably a radioactive metal, to the use of these molecules and to therapeutic and diagnostic compositions containing them.

Abstract: A2A agonists of formula (I) is provided, wherein R1, R2, R4, R5, X, Y, Z, n, p, and q are as described herein. Also provided are compositions comprising and methods of using compounds of formula (I).

Abstract: The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.

Abstract: There is disclosed a process for producing an amide compound, which process is characterized in that a compound having an amino group are reacted with a polyaminopolycarboxylic acid anhydride in the presence of the polyaminopolycarboxylic acid.

Abstract: Methods for simultaneously detecting dementia or cognitive impairment, such as Alzheimer's Disease (AD), Parkinson's Disease (PD), Lewy Body Dementia (LBD) and Vascular Dementia (VaD) in a patient using dual or multiple radiopharmaceutical probes are provided herein.

Abstract: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

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

Abstract: The methods and compositions of the invention are based on the preferential utilization of fructose by cancer cells. This invention relates to compositions, methods and kits utilizing fructose and other monosaccharides for the treatment of cancer. This invention also relates to methods and kits for using compositions to mimic or corrupt metabolic pathways of fructose and/or signal transduction pathways related to cancer cells for the treatment of cancer.

Abstract: The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.

Abstract: Disclosed herein are methods for treating a mammal harboring a solid tumor which expresses higher levels of High Affinity Laminin Receptors (LAMR) than normal cells of the same lineage comprising systematically administering to a mammal in need of such treatment a therapeutically effective amount of a Replication Competent (RC) Sindbis virus vector, wherein said vector encodes a suicide gene.

Abstract: A detection agent, including a polymerized liposome, a lectin, and an imaging agent, can be administered to an animal for the detection of polyps in the lower gastrointestinal tract.

Abstract: The present invention provides a 13C-labeled oligosaccharide or polysaccharide or a salt thereof excluding U—13C-maltose, 13C-starch, 1-13C-maltotetraose and 1-13C-amylose; a derivative of the 13C-labeled oligosaccharide or polysaccharide or salt thereof; a 13C-labeled inclusion complex or a salt thereof, which comprises a cyclodextrin or a modified derivative thereof as a host molecule; a 13C- or 14C-labeled fluorescein ester compound or a salt thereof; and a diagnostic agents for pancreatic exocrine function comprising these compounds 13C- or 14C-labeled.

Abstract: Described herein are methods for detecting a bacteria in a subject and methods for detecting, imaging or diagnosing a site, disease, disorder or condition in a subject using bacteria. The methods can be used in conjunction with methods for treating a disease, disorder or condition. Such sites, diseases and disorders include sites of cellular proliferation, such as tumors, tumor tissues, metastases, areas of inflammation, immunoprivileged sites or tissues, wounds and infections. Further described are bacteria for use in the methods and compositions, combinations and kits, including diagnostic and pharmaceutical compositions, containing a bacterium. Bacteria described herein include those that bind, sequester or accumulate radiolabeled compounds by expression of an endogenous gene product that binds to the radiolabeled compound. Additional imaging and therapeutic agents and methods also are described.

Abstract: This invention relates to compositions, methods utilizing fructose and other monosaccharides for the diagnosis of cancer. Cancer cells have shown a higher level of fructose utilization as compared to glucose. Further, cancer cells have shown a preferential use of fructose for nucleic acid synthesis. The present invention takes advantage of these features and provides for fructose or fructose-based compositions for the diagnosis of cancer using imaging techniques such as positron emission tomography.

Abstract: An composition in a method for noninvasively monitoring the expression of therapeutic transgene delivered ex vivo and in vivo for the treatment of diseases includes the step of quantitatively imaging a reporter gene expression which is coupled to a therapeutic gene on a plasmid vector to infer levels, location, or duration of the therapeutic gene expression in the targeted tissues or organs. The reporter gene is imaged using a radiopharmaceutical for scintigraphic imaging of the gene expression interactions with the reporter gene, namely positron emission tomography, gamma camera or single-photon emission computed tomography. The genes are delivered with a liposome encapsulated reporter-therapeutic linked transgene vector with balanced reporter/therapeutic transgene expression. A transgene composition includes the reporter gene linked to the therapeutic gene or genes incorporated in and delivered by a liposome encapsulated reporter-therapeutic linked transgene vector.

Abstract: The present invention relates to an universal method for the large scale production of high-purity carrier free or non carrier added radioisotopes by applying a number of “unit operations” which are derived from physics and material science and hitherto not used for isotope production. A required number of said unit operations is combined, selected and optimised individually for each radioisotope production scheme. The use of said unit operations allows a batch wise operation or a fully automated continuous production scheme. The radioisotopes produced by the inventive method are especially suitable for producing radioisotope-labelled bioconjugates as well as particles, in particular nanoparticles and microparticles.

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 substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Abstract: Aminoalkyl glucosaminide phosphate (AGP) compounds that are adjuvants and immunoeffectors are described and claimed. The compounds have a 2-deoxy-2-amino glucose in glycosidic linkage with an aminoalkyl (aglycon) group. Compounds are phosphorylated at the 4 or 6 carbon on the glucosaminide ring and comprise three 3-alkanoyloxyalkanoyl residues. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

Abstract: A method for preparing a radioactive surface source for radiotherapy is disclosed. The method comprises: (a) providing a structure having a surface; (b) positioning the structure in a flux of at least one radionuclide so as to collect atoms of the at least one radionuclide on or beneath the surface; and (c) treating the surface such that the atoms are intercalated into the surface but allowed to recoil out of the surface upon radioactive decay. In various exemplary embodiments of the invention the method further comprises coating the surface by at least one layer of polymeric material, such that the atoms are collected into the polymeric material.

Abstract: An agent, composition and method for the treatment, prophylaxis and/or diagnosis of proliferative disorders, which is highly and efficiently absorbed at the site of abnormal cellular proliferation is disclosed.

Abstract: The invention provides improved nucleic acid ligands with enhanced stability that inhibit coagulation and improved modulators of the nucleic acids to provide ideal modulators of coagulation. These improved nucleic acids and modulators are particularly useful for inhibiting coagulation in a host undergoing a therapeutic regime such as surgery or coronary artery bypass.

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

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: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologs. The compounds may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350 to 1300 nm, the exact range being dependent upon the particular dye. The use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluoresence tumor imaging, detection and therapy.

Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.

Abstract: A compound of the formula (I) wherein the variables are defined herein. Methods of dye-labeling biomolecules with the compound of formula (I) and dye-labeled biomolecules are also provided.

Abstract: This invention relates to novel nucleotide-based compounds, methods of making radiolabeled compounds and use of such compounds for diagnostic imaging. Provided are compounds according to Formula (I) A-B-L-C, wherein A stands for an aptamer, B is absent or stands for a bridging structure, L is a linker, and C is a metal ion chelator. All substituents are defined in detail in the description. Preferred embodiments of said compounds bind to Tenascin-C.

Abstract: This invention provides compounds containing a 2-deoxy-2-amino-?-D-glucopyranose (glucosamine) glycosidically linked to an 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 present invention relates to a 2-nitroimidazole derivative, a diagnostic pharmaceutical composition which contains such 2-nitroimidazole derivative, the use of the 2-nitroimidazole derivative for the detection of hypoxic biological tissue as well a method for the detection of hypoxic biological tissue by the use of the 2-nitroimidazole derivative.

Abstract: The invention provides an immunostimulatory nucleic acid. In certain embodiments according to this aspect of the invention, the sequence of the immunostimulatory oligonucleotide and/or immunomer is at least partially self-complementary.

Abstract: The invention provides an immunostimulatory nucleic acid. In certain embodiments according to this aspect of the invention, the sequence of the immunostimulatory oligonucleotide and/or immunomer is at least partially self-complementary.

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: The present invention is directed to metal chelating conjugates for use as metallopharmaceutical diagnostic or therapeutic agents. Specifically, conjugates of the present invention include one or more carriers, a linker, and a metal coordinating moiety comprising a substituted phenyl, pyridyl, or pyrimidyl derivative.