The invention relates to a method of preparing an [.sup.18F] radio-labelled compound, wherein the water content is controlled. Controlling the water content and the origin of the water within the reaction process has a significant effect on both the yield and the purity of the product of the radio-labelling process.

In various embodiments, the invention provides a radiotracer comprising a positron emitting atom bound to a deoxy sugar moiety. The radiotracer is reversible bound to a caging moiety that prevents or retards tissue uptake of the radiotracer while the caging moiety is in place. An exemplary caging moiety is acid labile and is cleaved upon uptake of the radiotracer by tissue with an acidic pH.

Methods are provided for the prognosis, diagnosis and treatment of various pathological states, including cancer, chemotherapy resistance and dementia associated with Alzheimer's disease. The methods provided herein are based on the discovery that various proteins with a high level of sialylation are shown herein to be associated with disease states, such as, cancer, chemotherapy resistance and dementia associated with Alzheimer's disease. Such methods provide a lysosomal exocytosis activity profile comprising one or more values representing lysosomal exocytosis activity. Also provided herein, is the discovery that low lysosomal sialidase activity is associated with various pathological states. Thus, the methods also provide a lysosomal sialidase activity profile, comprising one or more values representing lysosomal sialidase activity. A lysosomal sialidase activity profile is one example of a lysosomal exocytosis activity profile.

A method for preparing a precursor of gene expression probe is revealed. First prepare 2-deoxy-2-fluoro-3,5-di-O-benzoyl--D-arabinofuranosyl bromide and 2,4-bis-O-(trimethylsilyl)-5-bromouracil respectively. Then use 2-deoxy-2-fluoro-3,5-di-O-benzoyl--D-arabinofuranosyl bromide and 2,4-bis-O-(trimethylsilyl)-5-bromouracil to perform a coupling reaction and get a 1-(3,5-di-O-benzoyl-2-deoxy-2-fluoro--D-arabinofuranosyl)-5-bromouracil. Next use 1-(3,5-di-O-benzoyl-2-deoxy-2-fluoro--D-arabinofuranosyl)-5-bromouracil generated and hexabutylditin to perform a substitution reaction in an anhydrous 1,4-dioxane solution and get 1-(3,5-di-O-benzoyl-2-deoxy-2-fluoro--D-arabinofuranosyl)-5-tributylstannyl)uracil. At last carry out debenzoylation of 1-(3,5-di-O-benzoyl-2-deoxy-2-fluoro--D-arabinofuranosyl)-5-tributylstannyl)uracil to get 5-tributylstannyl-1-(2-deoxy-2-fluoro--D-arabinofuranosyl)uracil (FSAU), a precursor of gene expression probe.

Inter alia, the first titania-catalyzed [.sup.18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [.sup.18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.

A mannose derivative is an isonitrile-containing mannose derivative of formula (I), including different linking groups X: ##STR00001##
A radioactive preparation is provided, including a radiolabeled compound formed by radiolabeling the mannose derivative with a radionuclide. An application of the radioactive preparation in the diagnosis and treatment of tumors is also provided.

The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals.

The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.

The invention relates to a method for the preparation of radiochemical compounds using a device having at least a reaction module, a dosing module, and a storage module, wherein the reaction module has at least one reaction vessel having a closable opening through which substances needed for the preparation of a predetermined radiochemical compound can be introduced into the reaction vessel of the reaction module and through which the prepared radiochemical compound can be removed from the reaction vessel of the reaction module; the dosing module has at least one pipetting head which can be moved relative to the storage module and the reaction module and in x, y, and z directions and also has at least one dosing unit; and at least one reservoir for one of the substances needed for the preparation of the respective radiochemical compound is formed in the storage module. Substances needed for the preparation of the respective radiochemical compound are introduced into the reaction vessel of the reaction module by means of dosing units, wherein the dosing units can be moved via a pipetting head in x, y directions or in x, y, and z directions.

The present invention relates to a method for synthesizing a radiopharmaceutical using a cartridge, which makes it possible to carry out several steps of reaction required for synthesizing a radiopharmaceutical in the cartridge filled with a polymer. A method for synthesizing a radiopharmaceutical according to the present invention enables each step's reaction to be carried out with the solution confined in the cartridge so as not to flow out, thus being simplified compared to the conventional methods for synthesizing radiopharmaceuticals, and expediting the synthesis thereof.