Compounds capable of binding to granzyme B and comprising a radioactive moiety, for examples, compounds of Formula (I), and pharmaceutical compositions comprising such. Also provided herein are uses of the compounds and pharmaceutical composition in cancer treatment and/or imaging.

Compounds having the general formula III, or IV ##STR00001##
wherein R.sub.1 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: R.sub.2,4,5,6 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, SR 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 R.sub.1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C.sub.3-C.sub.5 cycloalkyl group, aromatic, and heterocyclic group; and wherein X is C.sub.1-C.sub.4 radiohaloalkyl.

Provided herein are compounds useful for imaging granzyme B. An exemplary compound provided herein is useful as a radiotracer for position emission tomography (PET) and/or single photon emission tomography (SPECT) imaging. Methods of imaging granzyme B, combination therapies, and kits comprising the granzyme B imaging agents are also provided.

The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of PDE10A in mammals. The compound of the present invention is represented by the formula (I): wherein each symbols are as defined in the specification. ##STR00001##

Various compositions and methods for Quasi-Amadori products and derivatives thereof are contemplated in which a halogenated carbohydrate is reacted with a primary amino group of an affinity ligand. In especially preferred aspects, the Quasi-Amadori product is formed from 2-fluorodeoxyglucose and an affinity moiety that preferentially or selectively binds to a neural cell or neural structure. Where contemplated compounds include .sup.18F, PET imaging using compounds presented herein is especially preferred.

This disclosure provides compounds, pharmaceutical compositions, imaging compositions and methods useful for the diagnosis and/or treatment of neurodegenerative diseases. In particular, this disclosure provides compounds, including radiolabeled compounds, compositions, and methods useful for the diagnosis and/or treatment of neurodegenerative diseases associated with a-synuclein aggregation, such as Parkinson's disease, dementia with Lewy bodies, multiple systems atrophy or prodromal REM sleep behavior disorder.

Conjugates are described herein where CCK2R targeting ligands are attached to an active moiety, such as therapeutic agent or an imaging agent, through a linker. The conjugates can be used in the detection, diagnosis, imaging and treatment of cancer.

Compounds of Formula (I) and Formula (II), which are capable of binding to granzyme B. Also provided herein are pharmaceutical compositions comprising such for use in, for example, imaging Granzyme B and/or treating immunoregulatory abnormalities.