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##

Disclosed are compounds, compositions, systems, and methods useful for treating disease (such as cancer and tumors), or binding, detecting, and affecting compounds, compositions, cells, tissues, and organs, where the compounds, compositions, systems, and methods include or involve toxic compounds and where the toxic effect of the compounds, compositions, systems, and methods is reduced by providing a cleavage site to facilitate separation of the toxic component from other components of the compound, composition, or system. Preferably the system is a composition delivery system comprising or using a composition as disclosed herein. In some forms, the cleavage of the composition delivers a therapeutic agent and avoids organ damage by the composition.

The invention provides 3-deuterium-enriched 3-(5-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same, such as in the treatment of cancer, an immune-related disease, or an inflammatory disease.

The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

The invention relates to methods and compositions for the selection of patients for therapy with an anti-inflammatory drug. More particularly, the invention relates to compositions comprising folate-imaging agent conjugates for the selection of patients for therapy with an anti-inflammatory drug, and methods and uses therefor.

Compounds having formula I, ##STR00001##
or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.

The invention relates to a radioactive I-labeled Larotrectinib compound and a preparation method and application thereof, including a radioactive I-labeled Larotrectinib compound having the following structural formula and its analogs:

##STR00001## where R.sub.1 and R.sub.2 are respectively H, F, Cl, Br, .sup.123I, .sup.124I, .sup.125I, .sup.130I or .sup.131I, and at least one of R.sub.1 and R.sub.2 is a radioactive iodine element. The invention provides a preparation method of a radioiodinated pyrazolo[1,5-a]pyrimidine compound base. Radioiodinated pyrazolo[1,5-a]pyrimidine compounds with long half-life and different ray energy can be used for PET tomography and clinical diagnostic research of SPECT. Moreover, the high-energy radioiodinated pyrazolo[1,5-a]pyrimidine can act as a TrK receptor ligand to inhibit the activity of TRK and kill tumor cells; and due to high-energy I-131 ray energy carried, the radioiodinated pyrazolo[1,5-a]pyrimidine can coordinate to shoot tumor cells and thus achieve an accurate radiotherapy effect.

Provided herein are certain compounds and imaging agents useful for detecting a disease or condition associated with protein aggregation, compositions thereof, and methods of their use.

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.

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 linker 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.