The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.

##STR00001##

Novel .sup.18F-labelled tetrazines are provided which are highly reactive to be effective in vivo, suitable for pretargeted positron emission tomography (PET) and accessible in radiochemical yields (RCYs) which allow access to .sup.18F-labeled tetrazines for clinical applications. The .sup.18F-labelled tetrazines are developed using a Cu-mediated click indirect labelling approach. Only a subset of compounds appeared to be suitable for clinical pretargeted imaging strategies, and a particular compound which includes the use of an .sup.18F-labelled azide synthon having an azide structure with glucose as the linker and a triazole moiety within the linker, appears to be highly suited for clinical pretargeted imaging purposes.

The present disclosure provides radiolabeled compounds of the formula: (I) and (II), as well as precursor compounds of the formula: (VII) wherein the variables are defined herein. The present disclosure also provides radiopharmaceutical compositions comprising the radiolabeled compounds disclosed herein as well as precursor compositions comprising the precursor compounds disclosed herein. The present disclosure further provides methods of imaging using the radiolabeled compounds and/or radiopharmaceutical compositions of the present disclosure as well as kits for the preparation of the radiolabeled compounds and radiopharmaceutical compositions disclosed herein.

##STR00001##

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”) where the compounds are represented by the following:

##STR00001## or a pharmaceutically acceptable salt thereof,

##STR00002## or a pharmaceutically acceptable salt thereof,

##STR00003## or a pharmaceutically acceptable salt thereof,
wherein M.sup.1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.

Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”) where the compounds are represented by the following: ##STR00001## or a pharmaceutically acceptable salt thereof, ##STR00002## or a pharmaceutically acceptable salt thereof, ##STR00003## or a pharmaceutically acceptable salt thereof,
wherein M.sup.1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.

Fluoridated organofluoroborates comprising at least one .sup.18F atom and precursors thereto, for use in PET scanning.

Provided are a compound represented by the following formula (1): ##STR00001##
wherein X.sub.1 represents a hydrogen atom or a halogen atom, X.sub.2 represents a fluorine atom or a nitrile group, and X.sub.3 represents a radioactive halogen atom, or a salt thereof, and a medicament including the same.

Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

Neurokinin-1 (NK-1) receptor-binding agent delivery conjugates, compositions comprising NK-1 receptor-binding agent delivery conjugates, and methods for making and administering NK-1 receptor-binding agent delivery conjugates are provided. A conjugate may include an NK-1 receptor-binding moiety, a tinker group containing at least one linker selected from the group of a releasable linker and a spacer linker, and an active agent linked to the linker group. The active agent may be selected from the group of fluorophore-containing compounds, radionuclide-containing compounds, and therapeutic agents for treatment of tumor cells characterized by over-expression of the NK-1 receptor.