The present invention provides a novel compound of the formula: methods of making this compound, methods of using this compound for pretargeted imaging, and preparations of such formulations.

##STR00001##

The present disclosure relates to compositions and methods of carbonic anhydrase IX inhibitors. The present disclosure also relates to targeting conjugates of carbonic anhydrase IX inhibitors. The present disclosure also relates to the use of targeting conjugates of carbonic anhydrase IX inhibitors in methods of treating disease and for imaging of disease.

The tumor stroma, which accounts for a large part of the tumor mass, represents an attractive target for the delivery of diagnostic and therapeutic compounds. Here, the focus is notably on a subpopulation of stromal cells, known as cancer-associated fibroblasts, which are present in more than 90% of epithelial carcinomas, including pancreatic, colon, and breast cancer. Cancer-associated fibroblasts feature high expression of FAP, which is not detectable in adult normal tissue but is associated with a poor prognosis in cancer patients. The present invention provides small-molecule radiopharmaceutical and imaging agents based on a FAP-specific inhibitor.

A method for producing an .sup.225Ac solution includes a step (I) of irradiating a .sup.226Ra target with particles to generate two or more actinium radioisotopes (Ac) including at least .sup.225Ac, a step (II) of dissolving the .sup.226Ra target after the aforementioned step to obtain a solution (1), a step (III) of separating .sup.226Ra and Ac contained in the solution (1) to obtain a solution (2), a step (IV) of allowing Ac contained in the solution (2) other than .sup.225Ac to decay to obtain a solution (3), and a step (V) of separating Ra and Ac contained in the solution (3) to obtain a solution (4). The solution (4) is used to produce a medicine that contains, as an active ingredient, a conjugate between a chelating agent that has formed a complex with .sup.225Ac, and a targeting agent.

Kits for the preparation, synthesis, and delivery of compositions comprising a conjugate of a nucleoside analog, a chelator, and a label for use as imaging and therapeutic agents. The kits, as well as methods for their use, may be used in diagnosing, treating, or monitoring the progression of infectious diseases and/or symptoms or complications resulting from infection.

A compound comprising a prostate specific membrane antigen (PSMA)-targeting moiety of the following formula or of a salt or a solvate thereof. R.sup.0 is O or S. Each of R.sup.1a, R.sup.1b and R.sup.1c may be —CO.sub.2H, —SO.sub.2H, —SO.sub.3H, —PO.sub.2H, or —PO.sub.3H.sub.2, for example. R.sup.2 may be methylene or a derivative thereof, propylene or a derivative thereof, or a derivative of ethylene, optionally substituted. R.sup.3 is a linker. When the PSMA-targeting moiety is linked to a radiolabeling group, the compound may be used as an imaging agent or therapeutic agent for PSMA-expressing diseases/conditions. ##STR00001##

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging and therapeutic agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

The present disclosure provides compositions and methods for the detection, and treatment of cancer. Specifically, the compositions of the present technology include multimodal fluorine-cyanine-DOTA-hapten compositions that may be complexed with a radioisotope (e.g., .sup.175Lu). Also disclosed herein are methods of using the fluorine-cyanine-DOTA-hapten compositions of the present technology in diagnostic imaging as well as pretargeted radioimmunotherapy.

The present invention relates to combinations for use and methods of treating cancers that express prostate specific membrane antigen (PSMA). In particular, the invention provides novel therapies based on the combination of a PSMA therapeutic agent, such as radiolabeled Compound I, and immuno-oncology (I-O) therapeutic agents, wherein said I-O therapeutic agents are selected from the group consisting of LAG-3 inhibitors, TIM-3 inhibitors, GITR agonists, TGF-β inhibitors, IL15/IL-15RA complex, PD-1 inhibitors, PD-L1 inhibitors, and CTLA-4 inhibitors.

Excessive deposition of extracellular matrix is a hallmark of Idiopathic pulmonary fibrosis (IPF), it is advantageous to target the cells and the mechanisms associated with this process. By targeting myofibroblasts (specialized contractile fibroblasts) that are key for the development of IPF with drugs conjugated with fibroblast activation protein (FAP). this technology helps minimize the production of extracellular matrix in the lungs and provides a new treatment option for patients diagnosed with IPF.