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. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label 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, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen.

Abstract: The present method for determining the efficacy of therapy in the treatment of amyloidosis involves administering to a patient in need thereof a compound of formula (I) or Formula (II) or structures 1-45 and imaging the patient. After said imaging, at least one anti-amyloid agent is administered to said patient. Then, an effective amount of a compound of formula (I) or Formula (II) or structures 1-45 is administered to the patient and the patient is imaged again. Finally, baseline levels of amyloid deposition in the patient before treatment with the anti-amyloid agent are compared with levels of amyloid deposition in the patient following treatment with the anti-amyloid agent.

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 the provision of compounds, methods for producing them, and their use for imaging and quantification of aggregates of ?-amyloid peptides in vivo. In a preferred aspect of the invention, a tracer is administered to humans and displays enrichment in body parts that are containing aggregates of amyloid peptides. Tracers of the invention can be used for non-invasive depiction and quantification of aggregates of ?-amyloid peptides in humans affected with diseases that are characterized in the generation of such aggregates.

Abstract: Methods and systems for labeling synthesis of phosgen by UV light are provided. Methods of synthesizing labeled compounds useful as PET tracers from labeled phosgen are also provided. The resultant carbon-isotope labeled compounds are useful as radio-pharmaceuticals, especially for use in Positron Emission Tomography. Associated kits for PET studies are also provided.

Abstract: Provided herein are thalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.

Abstract: The present invention is directed to radiolabeled pyrimidinone compounds of general structural formula I which are useful as radiotracers for quantitative imaging of PDE10 in mammals.

Abstract: Methods and reagents for photo-initiated carbonylation with carbon-isotope labeled carbon monoxide using weakly nucleophilic amines and alkyl/aryl iodides are provided. The resultant carbon-isotope labeled amides are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.

Abstract: The present invention provides methods of using optimal PET tracers for diagnosing head and neck cancer. Non-invasive methods for assessing tumor perfusion and oxidative metabolism for in vivo imaging with PET tracers that are suitable for uses in radiation therapy (RT) in head and neck cancer and evaluation of salivary gland function are provided. A pharmaceutical comprising the PET tracer and a kit for the preparation of the pharmaceutical are provided as well.

Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an alkene or alkyne dienohile.

Abstract: The present invention relates to methods for the detection of myelin and a quantitative measurement of its local concentration in a sample using a benzofuran compound or its radioisotope derivatives. In one embodiment a method of myelin detection comprises identifying a subject at risk of or diagnosed with a myelin-associated neuropathy, parenterally administering to the subject the benzofuran compound, or a derivative of the compound, and determining myelination in the subject by detecting binding in the sample. In one embodiment, the invention provides a method of imaging myelinated tissue in a surgical field of mammalian tissue comprising the steps of contacting the surgical site with the benzofuran compound or a radioisotope derivative of the compound, and detecting binding in the surgical site.

Abstract: Disclosed are compositions and methods useful for targeting and internalizing molecules into cells of interest and for penetration by molecules of tissues of interest. The compositions and methods are based on peptide sequences, such as truncated CAR peptides, that are selectively internalized by a cell, penetrate tissue, or both. The disclosed internalization and tissue penetration is useful for delivering therapeutic and detectable agents to cells and tissues of interest.

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: Bipiperidinyl compounds and salts thereof are disclosed. The compounds include high affinity ligands for ?1 receptors. Some compounds are also highly selective for ?1 receptor compared to ?2 receptor. Compounds can comprise radioisotopes, including 18F or 11C. Radiolabeled compounds can be used as probes for imaging distribution of ?1 receptor in a subject such as a human using positron emission tomography (PET) scanning.

Abstract: The present invention relates to methods for the detection of myelin and a quantitative measurement of its local concentration in a sample using a benzofuran compound or its radioisotope derivatives. In one embodiment a method of myelin detection comprises identifying a subject at risk of or diagnosed with a myelin-associated neuropathy, parenterally administering to the subject the benzofuran compound, or a derivative of the compound, and determining myelination in the subject by detecting binding in the sample. In one embodiment, the invention provides a method of imaging myelinated tissue in a surgical field of mammalian tissue comprising the steps of contacting the surgical site with the benzofuran compound or a radioisotope derivative of the compound, and detecting binding in the surgical site.

Abstract: Briefly described, embodiments of this disclosure include compounds as described herein, labeled compounds as described herein, pharmaceutical composition including compounds described herein, methods of imaging, method of forming a compound as described herein, and the like. In particular, embodiments of the disclosure include a series of triamino-pyridine derivatives and labeled triamino-pyridine derivatives, methods of synthesizing these compounds, intermediate compounds, methods of treatment using these compounds, methods of imaging, diagnosing, localizing, monitoring, and/or assessing a condition (e.g., corticotropin releasing factor type-1 (CRF1)) and/or related biological events, using triamino-pyridine derivatives, and the like. In addition, the present disclosure includes compositions (e.g., labeled triamino-pyridine derivatives that are ligands for the CRF1 receptor) used in and methods relating to non-invasive imaging (e.g., positron emission tomography (PET) imaging or SPECT imaging).

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: 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: Positron Emission Tomography (PET) tracers such as D-[methyl-11C]-Deprenyl (DDE) and [11C]-GR205171 (GLD), methods for and methods of preparing biological mechanisms that identify treatment targets in connection with Whiplash-Associated Disorder (WAD) are provided. Associated kits for the evaluation of the biological mechanisms are also provided.

Abstract: The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. Formula (E) wherein X, Y and L are independently nondirectionally selected from —C(R1)(R2)—, —C(R3)?, —N(R4)—, —N?, —N+(R5)?, —O— and —S—; M and Z are independently nondirectionally selected from formula (I) and formula (II).

Abstract: A new and improved method for extending the half life of pharmaceutical compounds for use in diagnostic imaging or therapy uses a novel linker to attach a diagnostic or therapeutic moiety to a targeting peptide or another diagnostic or therapeutic moiety. The resulting compound may have the general formula M-N—O—P-Q, wherein M is the diagnostic or therapeutic moiety, N—O—P is the linker of the present invention, and Q is the targeting peptide. In another embodiment the compounds may have the formula M-N—O—P-M, wherein M is independently a diagnostic or therapeutic moiety and N—O—P is the linker of the invention. Methods for imaging or treating a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods for radiotherapy of a patient using the compounds are further provided, as are methods for preparing a radiotherapeutic agent from the compounds.

Abstract: Compounds having the general formula III?, or IV? wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y is S; Z can be either H, O, S, S—R or NR where R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic, and heterocycli

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: The present application is directed to radiolabeled cyclic polyazapeptides, pharmaceutical compositions comprising radiolabeled cyclic polyazapeptides, and methods of using the radiolabeled cyclic polyazapeptides. Such polyazapeptides can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).

Abstract: The invention relates to compounds of formula I, their synthesis and their use, in particular for detecting amyloid deposits in a patient.

Abstract: Compositions, methods of making, and methods of using nanoclusters in which the nanoclusters comprise a plurality of nanoparticles having a core of nanoparticles arranged such that the surfaces of the nanoparticles contact adjacent nanoparticles, the nanoparticles comprise an active ingredient, and the nanocluster has a mass median aerodynamic diameter of from about 0.25 ?m to about 20 ?m.

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: Translocator protein (TSPO) targeting compounds are described. Methods of making the compounds, and uses of the compounds for imaging are also described.

Abstract: The present invention provides curcumin-derived near infrared (NIR) imaging probes. Upon interacting with amyloid ? aggregates, these probes undergo a range of changes, qualifying them as “smart” probes. The inventors have demonstrated that probes of the invention have the capacity to monitor the progression of Alzheimer's disease in an in vivo animal model. In addition, the present invention encompasses probes useful as PET imaging agents, MRI imaging agents and multimodal imaging agents, as well as related methods of detecting and imaging amyloid ? aggregates and plaques.

Abstract: Disclosed herein are compounds of Formula (I), or a pharmaceutically acceptable salt, ester, amide, thereof; and methods of modulating the activity of a cannabinoid CB2 receptor comprising contacting a compound of Formula I with the cannabinoid CB2 receptor. Also disclosed are methods of imaging of a tissue by positron emission tomography, the method comprising administering to the subject a compound of Formula I, wherein the compound comprises a radioisotope. Also disclosed are methods of measuring the relative concentration of cannabinoid CB2 receptors in tissue of a subject, by using a compound of Formula I which comprises a radioisotope. In addition, method of diagnosing a disorder in a subject are disclosed.

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: A molecular probe for labeling myelin includes a fluorescent trans-stilbene derivative.

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: A peptide for diagnosing, preventing and treating atherosclerosis, and a use thereof, comprising an amino acid sequence as set forth in SEQ ID NO: 1 or SEQ ID NO: 2, and a use thereof. The peptide effectively targets atherosclerotic plaques, and binds to IL-4R to thereby exhibit antagonistic effects on IL-4-mediated signaling of cellular inflammatory reaction and survival reaction. The peptide of the present invention can be used for diagnosis of atherosclerosis, prevention and treatment of IL-4-induced inflammatory reaction and prevention and treatment of atherosclerosis which is primarily caused by the inflammatory reaction, as well as for prevention or treatment of atherosclerosis via conjugation with an anti-atherosclerotic drug.

Abstract: The present invention relates to indolyl-pyhdazinyl-diazabicyclononane derivatives in their labelled and unlabelled form. Furthermore, the present invention relates to the use of said derivatives in their labelled or unlabelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).

Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.

Abstract: This invention pertains to methods, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.

Abstract: Disclosed is a kit for use in the production of a molecular probe for PET drug screening for the purpose of producing a compound containing a short-lived radionuclide for PET applications. Specifically disclosed is a kit comprising a compound represented by the formula (I), (II) or (III) or a salt thereof. In the formulae, X1, X2, X3, X4, X5 and X6 are as defined in the description.

Abstract: The present invention relates to compounds having the general formula: Y-L-BFR-X wherein BFR is a bridged fused ring system; Y is a targeting group; L is optionally present and is a linker for coupling Y to BFR; and X is halogen (e.g., radiohalogen) or a functional group for labelling.

Abstract: The present invention relates to a method of radiolabelling carbon nanotubes, to the radiolabelled carbon nanotubes that can be obtained by implementing this method, and to applications thereof.

Abstract: Racemic mixtures and enantiomerically pure forms of novel 1-[(2?-substituted)-piperazin-1?-yl]-isoquinolines are norepinephrine (NE) transporter (NET) inhibitor compounds. Compounds of the invention are considered therapeutic agents for central nervous system (CNS) diseases and disorders, without limitation, including neurodegeneration, anxiety, depression, attention deficit disorders, drug dependency, and post traumatic stress disorder. Examples of the chemical syntheses of the compounds of the invention are provided. The isoquinoline compounds of the invention competitively bind at NET at nanomolar concentrations. The isoquinoline agents of the invention bind selectively to NET over other competitive transporter targets and receptor binding sites, including those of serotonin and dopamine, amongst others. The chemical syntheses of the invention are suitable for labeling with radionuclide atoms.

Abstract: The present invention provides novel compounds which may be used as in vivo imaging agents. The compounds of the invention are useful in a method to image the expression of P2X7 receptors in a subject, as a means to facilitate the diagnosis of a range of disease states.

Abstract: One aspect of the invention relates to novel complexes of technetium (Tc) with various heteroaromatic ligands, e.g., pyridyl and imidazolyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to novel pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the technetium complexes are also described. Another aspect of the invention relates to novel pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

Abstract: The present invention relates to radiopharmaceuticals and in particular to a radiopharmaceutical composition comprising a compound of Formula (I): and polysorbate as an excipient. The radiopharmaceutical composition of the invention reduces problems encountered with prior art compositions comprising the same class of compounds. Also provided by the invention is a method for the preparation of the radiopharmaceutical composition of the invention as well as particular uses of the radiopharmaceutical composition.

Abstract: The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.

Abstract: The present invention relates, generally to a method of determining and assessing cytochrome P450 2D6 isoenzyme (CYP2D6)-related metabolic capacity in an individual mammalian subject via a breath assay, by determining the relative amount of 13CO2 exhaled by a the subject upon intravenous or oral administration of a 13C-labeled CYP2D6 substrate compound. The present invention is useful as an in vivo phenotype assay for evaluating CYP2D6-related activity using the metabolite 13CO2 in expired breath and to determine the optimal dosage and timing of administration of CYP2D6 substrate compound.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's disease, familial Alzheimer's disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.

Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.

Abstract: Disclosed relates to an ionic liquid type crown ether derivative, expressed by Chemical Formula 1 below, for isolating metal ions, a method for preparing the same and a method for isolating selectively the metal ions using the cycle size of the same. The present invention can provide the ionic liquid type crown ether and isolate metal ions including radioactive isotopes efficiently using the same. Furthermore, the prevent invention provides crown ether valuably used as a recyclable and environment-friendly isolating medium by preparing crown ether of ionic liquid type. wherein m, n, X? and R are identical with those in the description.