Abstract: Disclosed are mGluR4 positive allosteric modulator ligands of general formula (I) and radiolabeled derivates, their use as therapeutic agents for the treatment of central nervous system disorders modulated by mGluR4 and as ligands for the labeling and diagnostic imaging of mGluR4 in mammals.

Abstract: Presented is a method for assessing dopamine transporter levels in a selected area of a subject's central nervous system by SPECT imaging comprising administering an injection of a labeled dopamine transporter ligand at approximately the time the subject is positioned for SPECT imaging and initiating a SPECT acquisition for a duration of about 30 minutes commencing at about 15 minutes after administration of labeled dopamine transporter ligand; and assessing, based on said SPECT acquisition, the amount of labeled dopamine transporter ligand that is bound to dopamine transporter.

Abstract: The present invention provides an immunostimulatory complex specifically adapted to act as adjuvant and as a peptide immunogen stabilizer. The immunostimulatory complex comprises a CpG oligonucleotide and a biologically active peptide immunogen. The immunostimulatory complex is particulate and can efficiently present peptide immunogens to the cells of the immune system to produce an immune response. The immunostimulatory complex may be formulated as a suspension for parenteral administration. The immunostimulatory complex may also be formulated in the form of w/o-emulsions, as a suspension in combination with a mineral salt suspension or with an in-situ gelling polymer for the efficient delivery of an immunogen to the cells of the immune system of a subject following parenteral administration, to produce an immune response which may also be a protective immune response.

Abstract: Disclosed are a curcumin derivative or a salt thereof, which contains a fluorine atom, represented by formula (I): (wherein R1a and R1b are each independently a hydrogen atom, alkyl, acetyl, or methoxycarbonyl; R2s are each independently a fluorine atom, CHF2—, CF3—, CHF2O—, or CF3O—; R3s are each independently a hydrogen atom or a fluorine atom; A is alkyl, cyano, carboxyl, alkoxycarbonyl, or R4—(CH2)m—; R4 is hydroxy, carboxy, cyano, acetyloxy, alkoxycarbonyl, alkoxyalkoxy, hydroxyalkoxy, or CONR5R6; R5 and R6 are each independently a hydrogen atom or alkyl; and m is an integer from 1 to 5), and a diagnostic imaging agent for diagnosing a disease in which an amyloid ? peptide aggregate accumulates, the diagnostic imaging agent containing a compound having a 1,3-dicarbonyl structure, wherein the compound exists in a keto form and an enol form, and the keto form and the enol form have different affinities, respectively, to the amyloid ? peptide aggregate.

Abstract: The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).

Abstract: Use of benzimidazole-derived compounds of formula (I) according to the following structure, wherein x is a heteroatom selected from N, S, O, P, SO, SO2 and SO3, preferably from N, S and SO3 and most preferably from N and SO3; n may be 0 or 1, R1 is a group selected from formula (II) and formula (III) and R2 is a group selected from H and formula (IV) since the aforesaid serves for the production of a formulation used as a specific marker in the case of neurodegenerative diseases and tau pathologies.

Abstract: The present invention relates to complexes comprising one or more markers and one or more biomolecules for use as a contrast agent in positron emission tomography based imaging. The complexes according to the present invention preferably accumulate in a target compartment, such as the kidney. The present invention further relates to methods for generating the complexes and methods for using the complexes such as for evaluation of different aspects of kidney functionality e.g. for calculation of total and/or regional glomerular filtration rate in the kidney without the need for sampling blood or urine.

Abstract: The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

Abstract: Heterofunctional segment-poly(ethylene glycol) polymers, conjugates of these molecules with therapeutic and/or imaging agents, and methods for their use are disclosed. The heterofunctional segment-poly(ethylene glycol) polymers are useful as drug delivery conjugates, i.e., the heterofunctional segment-poly(ethylene glycol) polymers can be covalently attached to therapeutic agents (e.g., pharmaceutically active agents) and serve as delivery vehicles for the therapeutic agents. The heterofunctional segment-poly(ethylene glycol) polymers are also useful as imaging agent conjugates, i.e. the heterofunctional segment-poly(ethylene glycol) polymers can be covalently attached to imaging agents (e.g., tracers, imaging atoms, and imaging molecules) and serve as delivery vehicles for the imaging agents. Also disclosed are methods for treating a subject by administering to the subject an effective amount of the polymers conjugated to a therapeutic agent, an imaging agent, or a mixture thereof.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic central moiety containing urea or urethane functions allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic central moiety containing hydroxyl groups allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to methods employing such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract: The present invention is directed to compounds which are conjugates of two non-toxic natural products, noscapine (and various noscapine analogs) and folic acid (and various folic acid analogs), where the folic acid is conjugated to noscapine or the noscapine analog at the 9-position on the isoquinoline ring on the noscapine framework. Pharmaceutical compositions including the compounds, and methods of treating various tumors using the compounds and compositions, are also disclosed. The conjugates are particularly useful for treating cancers which overexpress the Folate Receptor ? (FRa) receptor.

Abstract: The present invention provides a method of promoting neuron growth and development by contacting cells with a peptide amphiphile molecule in an aqueous solution in the presence of a metal ion. According to the method, the peptide amphiphile forms a cylindrical micellar nanofiber composed of beta-sheets, which promote neuron growth and development.

Abstract: A radioactive mixture and a manufacturing method thereof are disclosed. The radioactive mixture (188Re-MN/Lipiodol mixture) is formed by chelating reaction of MN series compounds that are amine-amide-disulfide amine quadric-dentate chelate ligands with TcO4?/or ReO4?, and then dissolved in Lipiodol. Moreover, the 99mTc/or 188Re of the TcO4?/or ReO4? avoids bone marrow injuries caused by free 90Y. By the feature of the Lipiodol that stays in liver tumors for a long period, the radioactive mixture is applied to treat liver cancers by injection so that injuries caused by surgical operations can be prevented. 188Re-MN/Lipiodol is used for liver cancer, breast cancer or other solid tumors treatment. Re-188 MN or Re-188 MN/Lipiodol can be mixed with anticancer drugs, hydrogel, liposome, micelle or other nano-particles to form the multifunctional therapeutic modality.

Abstract: Compounds of formula (I), wherein X, Z, A, B, D, E, R1-R4 and m are as defined in the claims, exhibit alpha2C antagonistic activity and are thus useful as alpha2 antagonists.

Abstract: The present invention relates to nuclear medicine using fluorescent silica nanoparticle and detecting method of optical dual imaging, and more particularly to radioisotope labeled fluorescent silica nanoparticles which are used for PET (positron emission tomography) and fluorescence detecting, and detecting method of PET and fluorescent dual imaging using thereof. Functionalized silica nanoparticles of this invention have promising potential as a role for organic lymphatic tracer in biomedical imaging such as pre- and intra-operative surgical guidance.

Abstract: Tetrapyrollic photosensitizers and imaging agent compounds having A, B, C, and D rings and having a reduced B ring and an oxidized D ring. The compounds preferably have a purity of at least 95 percent and preferably have a fused system connected at an unsaturated carbon atom of the C ring nearest the D ring and at the unsaturated carbon atom between the C and D rings. The invention also includes a method of making the compounds at over 95 percent yield by starting with a B and D ring oxidized tetrapyrollic compound and dissolving it in a halogenated hydrocarbon solvent and treating it with sufficient nitroalkane solution of FeCl3.6H2O to oxidize the D ring and separating the resulting organic layer and drying.

Abstract: Formula (I) compounds are described where the groups are as defined here below, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumours.

Abstract: Methods and compositions for treating sepsis using cell membrane-permeant peptide conjugate covalent compounds having target cell specificity are provided.

Abstract: Disclosed are novel conjugates that include fluorinated carbohydrate molecules and methods for synthesizing the conjugates. The fluorinated carbohydrate molecule may include a radioisotope. The method of synthesizing the conjugate is useful for labeling selected molecules, and the conjugates may be useful in diagnostic or therapeutic methods. Particularly, the conjugates may be useful in diagnostic or therapeutic kits.

Abstract: The present invention relates to simultaneous tracking or imaging followed by hyperthermia therapy for cancer and other diseases associated with altered metabolic enzymes. In particular, the invention relates to a novel class of therapeutic nanomaterial which selectively target and kill tumor cells.

Abstract: This invention relates to compounds (benzothiazoles) suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging.

Abstract: The present invention relates to fluorescent silica nanoparticles for detecting lymph node and identification method of lymph node using thereof. The functionalized silica nanoparticles containing fluorescent dye of this invention have a promising potential for sentinel node detection in the surgical field through fluorescent imaging.

Abstract: Disclosed are mGluR4 positive allosteric modulator ligands of general formula (I) and radiolabeled derivates, their use as therapeutic agents for the treatment of central nervous system disorders modulated by mGluR4 and as ligands for the labeling and diagnostic imaging of mGluR4 in mammals.

Abstract: The invention relates to a family of cyanine dyes which fluoresce in the far red and near infra red wavelengths of the spectrum and preferably possess lipophilic side chains. The dyes of the invention are soluble in commercially available membrane staining vehicles, are useful as probes for rapidly staining lipophilic structures such as membranes in cells or isolated from cells, and are well retained therein. Methods of using the dyes to detect stained cells both in vivo and in vitro are also disclosed.

Abstract: The invention provides a labeling composition for an intraocular tissue of a living individual, which specifically labels the intraocular tissue without need of an invasive operation such as exposure of an ocular tissue or injection of a staining agent into the ocular tissue or a nerve tissue linking to the ocular tissue, a method of noninvasively labeling an intraocular tissue of a living individual, and a screening method using the labeling composition for the intraocular tissues. The composition contains a compound capable of labeling at least a photoreceptor cell layer of a retina, wherein the compound is a staining compound having a particular structure as a partial structure thereof.

Abstract: The present invention provides an in vivo imaging method that facilitates the diagnosis of Parkinson's disease (PD) at an early stage. Early diagnosis is particularly advantageous as neuroprotective treatment can be applied to healthy neural cells to delay or even prevent the onset of debilitating clinical symptoms.

Abstract: The present invention relates generally to chelation compounds, radionuclide metal chelate compounds, i.e., complexes, and radiolabeled targeting moieties, i.e., conjugates, formed therefrom, and methods of using these compounds, complexes and conjugates for diagnostic and therapeutic purposes. This invention is more particularly related to aryl bidentate isonitrile metal complexes generated by a chemical interaction of a metal salt oxide or weak complex of the metal with aryl isonitrile bidentate ligands.

Abstract: The invention provides compounds that comprise a 4?-thio nucleoside that is a derivative of 4?-thiothymidine or 4?-thio-2?-deoxyuridine comprising a positron or single photon emitting radioisotope or corresponding non-radioactive isotope attached via a triazole link to the N-3 position. Methods for preparing such compounds and uses of the compounds in medicine are also provided.

Abstract: Provided herein are methods for imaging an optically labeled target cell implanted in vivo using a reporter construct that encodes an enzyme that is not endogenous to the target cell. The disclosed methods include the steps of: (a) introducing target cell transformed with non-endogenous enzyme into a mammalian subject; (b) contacting the transformed target cell with a cell-permeable soluble fluorescent dye; and (c) observing a fluorescent signal generated by the target cell present in the mammalian subject. In some embodiments, the non-endogenous enzyme comprises a nitroreductase. In some embodiments, the methods may also include the step of tracking the fluorescent target cells in the mammalian subject over time.

Abstract: The invention provides an insulin-like growth factor-1 (IGF-1) receptor ligand carrying a therapeutic radionuclide for treatment of cancer is provided. A method of treating cancer using the IGF-1 receptor ligand carrying a therapeutic radionuclide is also provided. An anti-cancer therapeutic agent containing an IGF-1 receptor ligand linked to a toxin is also provided, as are methods of using the toxin conjugates for treatment of cancer.

Abstract: The present invention provides an integral source material, the integral source material has at least one nuclide that is an integral source material having at least one nuclide that is activatable by exposure to radiation, the nuclide is a chemically bound constituent of a polymer of the integral source material, wherein the integral source material is configured before activation to provide a device.

Abstract: The present invention relates to a method of producing radiolabelled gallium complexes that could be used as diagnostic agents, e.g. for positron emission tomography (PET) imaging.

Abstract: The invention relates to compositions and methods for treating diseases. In particular aspects, the invention relates to administering a combination of a disintegrin with a microtubule stabilizing agent useful for treatment of cancer.

Abstract: This invention relates to articles of manufacture containing liquid compositions of hypohalous acid or hypohalous acid salt for deactivating allergens and preventing diseases on hard surfaces, soft surfaces and in the air. The articles of manufacture contain usage instructions with health claims. This invention also includes methods of instructing the public and promoting the use of these compositions.

Abstract: Stabilized radiopharmaceutical formulations are disclosed. Methods of making and using stabilized radiopharmaceutical formulations are also disclosed. The invention relates to stabilizers that improve the radiostability of radiotherapeutic and radiodiagnostic compounds, and formulations containing them. In particular, it relates to stabilizers useful in the preparation and stabilization of targeted radiodiagnostic and radiotherapeutic compounds, and, in a preferred embodiment, to the preparation and stabilization of radiodiagnostic and radiotherapeutic compounds that are targeted to the Gastrin Releasing Peptide Receptor (GRP-Receptor).

Abstract: A hypoxia contrast medium including nitroimidazole-amino acid chelate with a positively charged radioactive nuclide, a preparation method and use thereof. The contrast medium can be used in imaging cerebral thrombosis, tumors or other diseases such as ulceration, thrombosis, and so on.

Abstract: MRI contrast agents that employ paramagnetic agents and chemical exchange saturation transfer (paraCEST) and which are coupled to targeted particulate delivery vehicles provide sufficient concentration of the paraCEST contrast agents to obtain useful images of target tissues or organs. In addition, the image contrast may be switched on or off with a presaturation radio frequency pulse, avoiding the necessity obtaining pre-injection and post-injection images.

Abstract: An improved linker which lacks chiral centers between a hydrophobic anchor for coupling to lipid-based particles and a targeting agent has suitable hydrophobic/hydrophilic properties for use in vivo.

Abstract: The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled by the described methods. Preferably, the F-18 may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other embodiments, the F-18 labeled moiety may comprise a targetable construct used in combination with a bispecific or multispecific antibody to target F-18 to a disease-associated antigen, such as a tumor-associated antigen. The F-18 labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET imaging analysis.

Abstract: The invention relates to a method of identifying/monitoring active atherosclerotic plaques associated with blood vessel walls wherein the plaques comprise activated macrophages having accessible binding sites for a ligand. The method comprises the steps of administering to a patient being evaluated for atherosclerosis an effective amount of a composition comprising a conjugate of a ligand and a chromophore capable of emitting light under predetermined conditions, allowing sufficient time for the ligand conjugate to bind to the activated macrophages, subjecting the blood vessels to the predetermined conditions using a catheter-based device, and identifying active plaques by detecting light emitted by the chromophore using a catheter-based device or by using an external imaging technique. The invention also relates to a similar method wherein a chemical moiety capable of emitting radiation is conjugated to the ligand.

Abstract: The invention provides compounds such as chelating agents useful in chelating metal ions, particularly radionuclides, to provide metal ion complexes. The invention also provides methods of using the compounds and complexes of the invention, such as in therapeutic and diagnostic applications.

Abstract: There is provided a central nervous system labelling composition for intranasal administration for the purpose of labelling the central nervous system from the olfactory epithelium by way of the olfactory bulb and by means of intranasal administration. Additionally, there is provided a method of non-invasively labelling the central nervous system by way of an administration route that entails little transferability to the entire body. Furthermore, there is provided a screening method using a central nervous system labelling composition for intranasal administration.

Abstract: A generic structure for the peptides of the present invention includes A-X-B-C, where C is a cargo moiety, the B portion includes basic amino acids, X is a cleavable linker sequence, and the A portion includes acidic amino acids. The intact structure is not significantly taken up by cells; however, upon extracellular cleavage of X, the B-C portion is taken up, delivering the cargo to targeted cells. Cargo may be, for example, a contrast agent for diagnostic imaging, a chemotherapeutic drug, or a radiation-sensitizer for therapy. X may be cleaved extracellularly or intracellularly. The molecules of the present invention may be linear, cyclic, branched, or have a mixed structure.

Abstract: The invention relates to a compound of formula (I): wherein P1, P2, P3, and P4 are each independently hydrogen or a protecting group; and n is an integer of from 2 to 20 and to the use of such compounds for the synthesis of 18F-FDG.

Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.

Abstract: Described are amphiphilic polymers that are provided with chelating moieties. The amphiphilic polymers are block copolymers comprising a hydrophilic block and a hydrophobic block, with the chelating moieties linked to the end-group of the hydrophilic block. The disclosed polymers are capable of self-assembly into structures such as micelles and polymersomes. With suitable metals present in the form of coordination complexes with 5 the chelating moieties, the chelating amphiphilic polymers of the invention are suitable for use in various imaging techniques requiring metal labeling, such as MRI (T 1/T 2 weighted contrast agents or CEST contrast agents) SPECT, PET or Spectral CT.

Abstract: The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): R*-L2-N3 (II) or, a compound of formula (III) with a compound of formula (IV) in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.

Abstract: Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.

Abstract: A composition for oral radionuclide chelation therapy comprises a DTPA chelate selected from Zn-DTPA and Ca-DTPA and a permeation enhancer that preferentially increases jejunal uptake of the DTPA chelate. The composition has a DTPA chelate bioavailability of at least 10% of the chelate when orally administered to a mammal.