Abstract: The present invention pertains to a novel liposome-based contrast agent that is for suppressing absorption in the reticuloendothelial system and for tumor-specific delivery of a radiolabeled substance. More specifically, the present invention pertains to: a liposome contrast agent containing a lipid and a compound of chemical formula 1, which is a radiolabeled substance, the liposome contrast agent being characterized in that the lipid is composed of (a) cholesterol, (b) 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), and (c) 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N [methoxy(polyethylene glycol)-2000] (DSPE-PEG2000); and a cancer diagnostic composition containing the liposome contrast agent as an active ingredient.

Abstract: Provided are a compound represented by the following formula (1): wherein X1 represents a hydrogen atom or a halogen atom, X2 represents a fluorine atom or a nitrile group, and X3 represents a radioactive halogen atom, or a salt thereof, and a medicament including the same.

Abstract: Provided are macrocyclic compounds having a macrocyclic core which has at least one macrocyclic donor and at least one pendant group which has at least one donor group. The macrocyclic compounds can be complexed to Fe(II) and Ni(II). The macrocyclic compounds can be used in imaging methods. For example, the compounds can be used MRI paraCEST contrast agents.

Abstract: Readily available hydrophilic and small organofluorine moieties were condensed via “click chemistry” to generate nonionic hydrophilic fluorinated molecules with unique 19F MR signatures. These were used to fabricate stable liposome formulations for imaging various tissue types. This approach was tailored to exploit the broad spectrum of organic 19F molecular species and to generate probes with distinct 19F MRI signatures for simultaneous assessment of multiple molecular targets within the same target volume.

Abstract: Provided herein are compounds useful for binding to one or more histone deacetylase enzymes (HDACs). The present application further provides radiolabeled compounds useful as a radiotracer for position emission tomography imaging of HDAC. Methods for prepared unlabeled and labeled compounds, diagnostic methods, and methods of treating diseases associated HDAC are also provided.

Abstract: The present invention relates to conjugates including a chelating moiety of a metal complex thereof and a therapeutic or targeting moiety, methods for their production, and uses thereof.

Abstract: Berberine or its derivatives are used in the preparation of myocardial perfusion imaging agents It has been verified using in vitro investigations, in vivo biodistribution, and small animal PET dynamic imaging, etc., that 18F-labeled berberine derivatives can specifically accumulate in cardiomyocytes or heart tissues, and has good distribution properties of targetting heart muscle in living animals, together with high contrast values of heart v.s. peripheral tissue (liver, lung, blood, muscle, bone, etc.).

Abstract: The present invention relates to a method of labelling biological molecules with 18F, via attachment to fluorine to a macrocyclic metal complex of a non-radioactive metal, where the metal complex is conjugated to the biological molecule. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.

Abstract: An automated radiopharmaceutical production and quality control system includes a particle accelerator, a radiopharmaceutical micro-synthesis subsystem, and quality control subsystem. The micro-accelerator of the improved biomarker generator is optimized for producing radioisotopes useful in synthesizing radiopharmaceuticals in quantities on the order of multiple unit doses, allowing for significant reductions in size, power requirements, and weight when compared to conventional radiopharmaceutical cyclotrons. The radiopharmaceutical micro-synthesis subsystem encompasses a small volume chemical synthesis system comprising a microreactor and/or a microfluidic chip and optimized for synthesizing the radiopharmaceutical in small quantities, allowing for significant reductions in processing time and in the quantity of radioisotope required. The automated quality control subsystem is used to test the composition and characteristics of the radiopharmaceutical to ensure that it is safe to inject.

Abstract: The concentration of an administered compound, such as a drug (D), in an organ or a bodily fluid, such as blood, is determined directly through detecting the drug (D) or its metabolites (DM) in sweat. The concentration may be determined indirectly by administering the drug (D) together with one or more tracer compounds (T, T2) or metabolites thereof (TM, T2M) or by detecting concentrations and trends of other analytes present in the body that react to the presence of the drug (D). By determining tracer concentration in sweat, the concentration of the drug (D) in blood or an organ can be determined. The tracer (T, T2) is a compound selected for ease of detection in sweat, known metabolic and solubility profiles that correspond to those of the drug (D), and safety of use. A smart transdermal delivery patch (300) is used to administer a dosage of drug to a wearer in coordination with at least one sweat sensor (324) reading conveying information about the wearer.

Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.

Abstract: A method of labelling biological molecules with 18F, via attachment of fluorine to a metal complex, where the metal complex is conjugated to the biological molecule. The invention highlights the incorporation of hydrogen bonding (H-bonding) into the metal complex scaffold, and how this can be utilised to improve the kinetics of fluoride incorporation. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.

Abstract: The present invention relates to 18F-labeled compounds suitable for positron emission tomography (PET) imaging. The invention further relates to the use of these compounds for carrying out PET scans, imaging the indoleamine 2,3-dioxygenase, pathway, predicting the responsiveness of a subject with a solid tumor to therapies including immunotherapy such as PD-1/PD-L1 inhibition, and determining whether a solid tumor in a subject contains tumor-infiltrating immune cells.

Abstract: The present invention provides a system for evaporating a radioactive fluid, a method for the synthesis of a radiolabelled compound including this system, and a cassette for the synthesis of a radiolabelled compound comprising this system. The present invention provides advantages over known methods for evaporation of a radioactive fluid as it reduces drastically the amount of radioactive gaseous chemicals that are released in the hot cell. It is gentler and more secure compared to the known process and provides access to radiosyntheic processes that may not been acceptable for safety reasons related to release of volatile radioactive gases during evaporation. In addition, the process yields are higher because the radioactive volatiles are labelled intermediate species.

Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.

Abstract: The present invention provides a composition comprising anti-1-amino-3-18F-fluorocyclobutyl-1-carboxylic acid (18F-FACBC) having an improved impurity profile compared with previous such compositions. Also provided is a method to obtain said composition.

Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.

Abstract: The present invention relates to novel, radiolabeled mGluR2/3 ligands, selective versus other mGlu receptors which are useful for imaging and quantifying the metabotropic glutamate receptor mGlu2 and 3 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.

Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.

Abstract: The present invention relates to novel, radiolabelled mGluR2/3 ligands, selective 5 versus other mGlu receptors, which are useful for imaging and quantifying the metabotropic glutamate receptors mGlu2 and 3 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or 10 in vivo and to precursors of said compounds.