Patent classifications
A61K51/0459
DESIGN AND DEVELOPMENT OF NEUROKININ-1 RECEPTOR-BINDING AGENT DELIVERY CONJUGATES
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.
Ligands for imaging cardiac innervation
Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release thereby reducing side effects, improved quantitative data, and/or high affinity for VMAT over prior radiotracers. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.
Contrast agents for myocardial perfusion imaging
The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.
18F-labelled folates
The present invention is directed towards new .sup.18F-folate radiopharmaceuticals, wherein the fluorine-18 is covalently linked to the aminobenzoyl moiety, which connects the condensed pyrimidine heterocycle to the amino acid portion within folate structures, as well as their precursors and their non-radioactive references, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
RADIOHALIDE-LABELED TARGETED DIAGNOSTICS AND THERAPEUTICS
Disclosed are chemical entities of formula (I) wherein R.sub.1, R.sub.2 and n are defined herein, and methods of use thereof. These chemical entities are radiative emitters and are useful, e.g., as therapeutic agents for the treatment of, or as diagnostic (e.g., imaging) agents for cancers, e.g., cancers in which PARP1 is overexpressed.
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COMPOSITIONS, IMAGING, AND THERAPEUTIC METHODS TARGETING FOLATE RECEPTOR 1 (FOLR1)
The present application provides stable heterobiligands made up of peptide-based FOLR1 ligands and folate (the ligand of FOLR1) and methods of use of the heterobiligands as detection, imaging, diagnostic, and therapeutic agents. The application further provides methods of manufacturing FOLR1 heterobiligands, capture agents, and imaging agents.
Imaging Agents and Methods of Use
A composition comprises a conjugate of the formula targeting component-linker-imaging component. In an embodiment, the targeting component is a VLA-4 antagonist. In an embodiment, the targeting component is a LFA-1 antagonist. In an embodiment, the linker includes chain of 2 to 20 atoms containing any combination of —CH.sub.2—, —CH═CH—, —C(O)—, —NH—, —S—, —S(O)—, —O—, —C(O)O— or —S(O).sub.2—; or a polyethylene glycol chain, wherein said chain of 2-20 atoms or polyethylene glycol chain are attached to the targeting and imaging components through ether, amide, sulfonamide, urea, thiourea, or triazole functional groups. In an embodiment, the imaging component is a metal chelator complexed with a metal ion or isotope thereof.
HETEROCYCLIC COMPOUNDS AND IMAGING AGENTS FOR IMAGING HUNTINGTIN PROTEIN
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.
COMPOSITIONS AND METHODS FOR MEASURING OXIDATIVE STRESS
The present disclosure provides for imaging agents and methods of making and using the same. The imaging agent comprises a luminol component comprising a luminol moiety or functional analogue thereof; a chelator; a linker group bonding or complexing the luminol component to the chelator; and a radiolabel component bound to the chelator. The imaging agent described herein is capable of monitoring, targeting, or imaging oxidative stress, reactive oxygen species (ROS), superoxide generation, or hydrogen peroxide generation, mediating pathophysiology of different disease states.
PROBES FOR IMAGING HUNTINGTIN PROTEIN
Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
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