A61K51/0455

8-HYDROXYQUINOLINE DERIVATIVES AS DIAGNOSTIC AND THERAPEUTIC AGENTS
20210024468 · 2021-01-28 ·

The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single-photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.

USE OF FLUORINATED DERIVATIVES OF 4-AMINOPYRIDINE IN THERAPEUTICS AND MEDICAL IMAGING
20210017133 · 2021-01-21 ·

The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including their use to diagnose and/or assess traumatic brain injury and use to treat dymeylinating diseases, and/or in vivo imaging of the central neverous system, and to diagnose and/or assess the progression of MS or other diseases.

IN VIVO IMAGING OF MATRIX METALLOPROTEINASES IN LUNG DISEASE

The present invention provides a method of imaging a subject's lung which comprises contacting the subject's lung with a matrix metalloproteinase inhibitor labeled with a radioisotope under conditions such that the inhibitor binds to matrix metalloproteinase in the lung, and then imaging the radiolabeled inhibitor bound to matrix metalloproteinase in the subject's lung.

The invention also provides Ro 32-3555 labeled with a radioisotope.

18/19F-labelled compounds which target the prostate specific membrane antigen

This disclosure relates to novel compounds comprising a zwitterionic trifluoroborate prosthetic group which target prostate-specific membrane antigen (PSMA), e.g. in prostate cancer. The compounds have Formula I, wherein each R1 is an anionic group, L is a linker and R2B-F3 is N(R.sup.3).sub.2CH.sub.2BF.sub.3, a pyridinium group substituted with BF.sub.3 or methyl BF.sub.3, or an azole group substituted with methyl BF3. Methods and uses of imaging and treating PSMA-expressing cancers are also disclosed. ##STR00001##

Compounds for imaging Tau protein aggregates

The present invention relates to novel compounds of the formula (I) ##STR00001##
that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.

TIME-VARYING KINETIC MODELING OF HIGH TEMPORAL-RESOLUTION DYNAMIC PET DATA FOR MULTIPARAMETRIC IMAGING
20200367846 · 2020-11-26 ·

Systems and methods are disclosed for quantifying blood flow using time-varying kinetic modeling of high temporal-resolution dynamic positron emission tomography (PET) data. A single tracer is introduced into the body. A first set of images is acquired, via PET, of at least a portion of the body at a plurality of predetermined time intervals. Based on the first set of images, an intensity of the tracer in the at least the portion of the body is determined as a function of time. The intensity of the tracer as a function of time is modeled using a time-varying kinetic model. Based on the model, the blood flow through the at least the portion of the body is quantified. Additional images may be acquired and used to quantify additional parameter(s), such as glucose metabolism, amyloid load, etc., with the single tracer.

COMPOSITIONS OF SPHINGOSINE-1-PHOSPHATE RECEPTOR 2 (S1PR2) BINDING AGENTS AND USES THEREOF
20200369626 · 2020-11-26 · ·

Described are compounds for the binding of S1PR2, and imaging agents and pharmaceutical compositions including said compounds. Also described are methods employing the compounds, imaging agents, and pharmaceutical compositions. These methods include imaging and/or treatment of diseases associated with S1PR2.

SCAFFOLDS AND MULTIFUNCTIONAL INTERMEDIATES FOR IMAGING PSMA AND CANCER THERAPY

Carbamate and beta-amino acid urea-based scaffolds that have high binding affinity to PSMA are disclosed. These scaffolds can be radiolabeled and used for imaging cells and tumors that express PSMA or for cancer radiotherapy. These compounds also can comprise a fluorescent dye and be used for imaging cells and tumors that express PSMA or for photodynamic therapy.

Compounds for imaging Tau protein aggregates

The present invention relates to novel compounds of the formula (II) ##STR00001##
that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.

PSMA-BASED MOLECULAR-GENETIC REPORTER SYSTEM

Methods, reporter gene constructs, and kits for using prostate-specific membrane antigen (PSMA) as an imaging reporter to image a variety of cells and tissues are provided.