A61K49/12

METAL/RADIOMETAL-LABELED PSMA INHIBITORS FOR PSMA-TARGETED IMAGING AND RADIOTHERAPY

Low-molecular weight gadolinium (Gd)-based MR contrast agents for PSMA-specific T.sub.1-weighted MR imaging are disclosed. The (Gd)-based MR contrast agents exhibit high binding affinity for PSMA and exhibit specific T.sub.1 contrast enhancement at PSMA+ cells. The PSMA-targeted Gd-based MR contrast agents can be used for PSMA-targeted imaging in vivo. .sup.86Y-labeled PSMA-binding ureas also are provided, wherein the PSMA-binding ureas also are suitable for use with other radiotherapeutics.

Cyclodextrin-linked polyvalent ligands for complexation of metal ions

Compounds are described which include polyvalent ligands linked to a cyclodextrin scaffold which exhibit strong binding affinities for lanthanides and favorable characteristics with respect to altering the relaxation time of coordinated water molecules. The compounds are useful as contrast agents in applications such as magnetic resonance imaging. The polyvalent ligands are also useful in applications requiring chelation of metal ions in other applications such as water treatment, sequestration of metal ions and treatment of diseases or conditions caused by exposure to toxic or radioactive metal ions.

RADIOPAQUE MONOMERS, POLYMERS, MICROSPHERES, AND METHODS RELATED THERETO
20220016270 · 2022-01-20 ·

Radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of using the radiopaque monomers, polymers, and microspheres are disclosed herein. Methods of manufacturing radiopaque monomers, polymers, and microspheres are disclosed herein.

FORMULATION OF CONTRAST MEDIA AND PROCESS OF PREPARATION THEREOF

The present disclosure relates to a liquid pharmaceutical formulation comprising a DOSA-derived tetra-chelate of formula (I), in which M is an ion of a paramagnetic metal, preferably a Gd.sup.3+ ion, and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the claims, in a pharmaceutical acceptable solvent. The present disclosure also relates to a method of preparation of said liquid pharmaceutical formulation and to a method of imaging involving said liquid pharmaceutical formulation.

Brush-arm star polymer imaging agents and uses thereof

Disclosed are methods, compositions, reagents, systems, and kits to prepare nitroxide-functionalized brush-arm star polymer organic radical contrast agent (BASP-ORCA) as well as compositions and uses thereof. Various embodiments show that BASP-ORCA display unprecedented per-nitroxide and per-molecule transverse relaxivities for organic radical contrast agents, exceptional stability, high water solubility, low in vitro and in vivo toxicity, and long blood compartment half-life. These materials have the potential to be adopted for tumor imaging using clinical high-field .sup.1H MRI techniques.

FUNCTIONALIZED LIPOSOMES FOR IMAGING MISFOLDED PROTEINS

Phospholipid-polymer-aromatic conjugates comprising binding ligands, liposome compositions including the phospholipid-polymer-aromatic conjugates, and binding ligands having an affinity for misfolded proteins are described. The phospholipid-polymer-aromatic conjugate may be represented by Structural Formula I: PL-AL-HP-X-BL (I). In Formula I, PL is a phospholipid, AL is an aliphatic linkage, HP is hydrophilic polymer, X is a link between the phospholipid-polymer and the binding ligand, and BL is polycyclic aromatic compound that functions as a binding ligand. The liposomal compositions may be useful for the imaging of misfolded and/or aggregated proteins.

MULTIFUNCTIONAL CONTRAST AGENTS, COMPOSITIONS, AND METHODS

Contrast agents, compositions including contrast agents, methods of forming contrast agents, and methods of imaging. Contrast agents may have a desirable solubility in liquids, such as aqueous liquids. Methods of forming contrast agents may include contacting a polymer that includes anhydride functional groups with one or more compounds. Methods of imaging may include administering to patients a contrast agent or composition including a contrast agent.

Polymeric treatment compositions

Polymeric compositions are described comprising a biocompatible polymer including a biodegradable linkage to a visualization agent and a non-physiological solution; wherein the biocompatible polymer is soluble in the non-physiological solution and insoluble in a physiological solution. Methods of forming the solutions and polymers are disclosed as well as methods of therapeutic use.

Polymeric treatment compositions

Polymeric compositions are described comprising a biocompatible polymer including a biodegradable linkage to a visualization agent and a non-physiological solution; wherein the biocompatible polymer is soluble in the non-physiological solution and insoluble in a physiological solution. Methods of forming the solutions and polymers are disclosed as well as methods of therapeutic use.

Targeted protein contrast agents, methods of making, and uses thereof

Provided herein are protein contrast agents and targeted protein contrast agents, formulations thereof, and methods of use, including but not limited to, as a magnetic resonance imaging contrast agent.