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: 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 a cyclooctene or cyclooctyne.

Abstract: The present invention relates to cell targeting conjugates and in particular, but not exclusively, to methods of their use in selectively eliminating and in selectively imaging target cells. The invention also relates to processes for production of the conjugates and to intermediate compounds that may be used in production of a specific class of cell targeting conjugates. In one embodiment there is provided a cell targeting conjugate comprising the following components that are covalently conjugated via a linker that is degradable within the target cells: i) a DNA minor groove binding ligand incorporating an effective Auger electron-emitting and/or gamma-emitting and/or positron-emitting atom or photoactive moiety; ii) a target cell specific protein or peptide that is capable of internalization by target cells.

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: 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 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: 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 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: Provided is radiolabeled ammonium salts and uses thereof as myocardial perfusion agents in molecular imaging.

Abstract: The present invention relates to in vivo imaging and radiotherapeutic methods and agents which target the enzyme aldehyde dehydrogenase (ALDH) and that are suitable for the in vivo imaging of tumours and treatment of cancer.

Abstract: The present invention provides a method for the synthesis of radioiodinated compounds which is advantageous over prior art methods. Using a hydrazine or an aminoxy in place of a primary amine for indirect radioiodination facilitates a much quicker reaction thus reducing reaction time and increasing the yield. In addition, where there are primary amines in the molecule to be radioiodinated, such as the N-terminus of a peptide or lysine residues, reaction at the hydrazine or aminoxy is greatly favoured.

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: 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: 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 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: Compounds useful for the early diagnosis of malignant tumors, multiple sclerosis, and especially Alzheimer's Disease and related dementias; especially compounds of Formula (I) wherein R1 is selected from the group consisting of hydrogen, cyano, fluoro, iodo, alkyl, and aryl; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; X is selected from the group consisting of CH2, CH2O, oxygen, OCH2, CH2S, SCH2, NH, N-alkyl, and N-aryl; Y is an optional spacer group, absent or selected from the group consisting of oxygen, sulfur, NH, N-alkyl, and N-aryl; and Z is selected from the group consisting of alkyl substituted with cyano, fluoro, or iodo and aryl substituted with cyano, fluoro, or iodo. In a preferred embodiment, R1 and R2 are hydrogen, X is CH2O, Y is absent, and Z is phenyl substituted with fluoro, cyano, or iodo. In some embodiments, Z is more specifically 18F-phenyl or 123I-phenyl or 131I-phenyl. Other compounds are also provided.

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: Provided is a pharmaceutical composition comprising radioiodinated N-(2-(diethylamino)ethyl)-4-(4-fluorobenzamido)-5-iodo-2-methoxybenzamide of Formula I. The pharmaceutical composition provides a stable formulation for both storing and administering to patients having melanoma. Also provided is a novel method of iodinating the precursor compound.

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: 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: Disclosed are A3 adenosine receptor antagonists and/or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs.

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: This invention relates to a method of imaging amyloid deposits and to diphenyl-heteroaryl compounds, and methods of making radiolabeled diphenyl-heteroaryl 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: 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: A compound of formula (I) wherein, X and Y independently bind TSPO, wherein X and Y are the same or different; and L is a linker that links X to Y; or a salt or solvate thereof. For preference, X and Y may be (II) or (III). The compounds may be radiolabeled with a radioisotope. Also methods for diagnosing or treating TSPO related disorders such as neurodegenerative disorder, inflammation or anxiety, eg. Alzheimer's disease, Parkinson's disease, Huntington's disease, multiple sclerosis, multiple system atrophy, epilepsy, encephalopathy, stroke, brain tumour, anxiety, stress, emotional disturbances or cognitive impairment, glioblastoma, ischemic stroke, herpes encephalitis, HIV, amyotrophic lateral sclerosis, corticobasal degeneration, cancer, depression, an auto-immune disease and an infectious disease.

Abstract: The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[18F]fluorocyclobutyl-1-carboxylic acid (2-[18F]FACBC) and 1-amino-2-[18F]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC).

Abstract: The invention features compositions and methods for treating or alleviating a symptom of cancer. The compositions and methods of the invention direct supra-lethal doses of radiation, called Hot-Spots, to virtually all cancer cell types.

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: The invention provides, inter alia, methods for treating cancer, compositions for treating cancer, and methods and compositions for diagnosing and/or detecting cancer. In particular, the present invention provides compositions and methods for treating, diagnosing and detecting cancers associated with AMIGO-2 overexpression.

Abstract: Differential expression of nucleic acids in the brains of subjects suffering from late-onset depression has been demonstrated. The invention provides methods useful in the determination of late-onset depression. Also provided by the present invention is a screening method for the identification of compounds for treatment, prevention or diagnosis of late-onset depression.

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: Synthetic peptidomimetic derivatives and phenyl group derivatives of Fenretinide (4-HPR) are disclosed, as are their uses as therapeutic, diagnostic and imaging agents for cancer and other diseases.

Abstract: The invention features a class of 2-nitroimidazole compounds with a secondary basic nitrogen atom and a linker bearing one or more therapeutic agents, cytotoxic agents, detectable labels, or chelating groups. In particular, the invention provides 2-nitroimidazole compounds containing a cluster of boron atoms for use in boron neutron capture therapy (BNCT). The 2-nitroimidazole compounds can be used to treat hypoxic conditions, including, e.g., cancer, inflammation, and ischemia. The weakly basic 2-nitroimidazole compounds target to hypoxic tissue and provide increased tissue concentration overall.

Abstract: This invention relates to vitamin-mitomycin conjugates, to a method of using the conjugates to selectively eliminate a population of pathogenic cells in a host animal harboring the pathogenic cells, and to a method of preparation of the conjugates. The conjugate is of the general formula B-L-X wherein the group B is a vitamin, or an analog or a derivative thereof, that binds to a surface accessible vitamin receptor that is uniquely expressed, overexpressed, or preferentially expressed by a population of pathogenic cells, wherein the group L comprises a cleavable linker, and wherein the group X comprises a mitomycin compound, or an analog or a derivative thereof. An additional therapeutic agent, such as a chemotherapeutic agent, can be administered in combination with the conjugate.

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: 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: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.

Abstract: A compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4) alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6) alkenyl group or a group of formula (y): wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.

Abstract: Renal extraction fraction (EF) is determined through use of computed tomography (CT) measurements of arterial blood before and after injection of a radiographic contrast agent into the blood and CT measurements of renal vein blood after injection of the radiographic contrast agent.

Abstract: Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.

Abstract: A method of single photon emission computed tomography (SPECT) using dual-isotopes of [99mTc]TRODAT-1 and [123I]ADAM is provided. Through SPECT, anomalies in dopamine and serotonin system are diagnosed with their photos in one examination. Thus, cost and labor for two examinations are saved and uses of SPECT are reduced.

Abstract: The present invention concerns a therapeutically labeled napthodianthrone or phenanthro[1,10,9,8-opqra]perylene-7,14-dione compound, which comprises a chemical element or an isotope that has an unstable nucleus and emits radiation during its decay to a stable form sufficient to destroy neighboring cells or tissues for use in a targeted radiotherapy to enhance curability of a warm-blooded animal that has been subjected to a necrosis-inducing antitumor therapy. A particular advantage of present invention is that viable rim resistant to a necrosis-inducing antitumor therapy such as vascular targeting agent (VTA) can be supplemented by one single or repeated doses of a therapeutically radiolabeled small molecule necrosis-avid chemical compound treatment to enhance the curability.

Abstract: A precursor of molecular probe for imaging of pancreatic islets is provided. A polypeptide represented by any one of the following formulae (1) to (4), or a polypeptide having a homology with the foregoing polypeptide. *-DLSK*?QMEEEAVRLFIEWLK*?NGGPSSGAPPPSK-NH2 (1) ?*-LSK*?QMEEEAVRLFIEWLK*?NGGPSSGAPPPSK-NH2 (2) ??*-SK*?QMEEEAVRLFIEWLK*?NGGPSSGAPPPSK-NH2 (3) ???*-K*?QMEEEAVRLFIEWLK*?NGGPSSGAPPPSK-NH2, (4) wherein *- indicates that an ?-amino group at an N-terminus is protected by a protecting group or modified with a modifying group having no electric charge; K* indicates that an amino group of a side chain of a lysine is protected by a protecting group; and —NH2 indicates that a carboxyl group at a C-terminus is amidated.

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: 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: 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: A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of readionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; Q is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; Y is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; R? is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.