A61K51/0463

Alpha-synuclein ligands

The present invention generally relates to various compounds that are useful as -synuclein ligands. The invention further relates to methods of using these compounds and their radiolabeled analogs for the detection of synucleinopathies, including Parkinson's disease (PD).

Imaging of glycogen synthase kinase 3

Provided herein are radiolabelled compounds useful for imaging GSK-3 kinase. An exemplary radiolabelled compound provided herein is useful as a radiotracer for imaging GSK-3 kinase using PET imaging. Methods for preparing the radiolabelled compounds and diagnostic methods using the radiolabelled compounds are also provided.

SMALL MOLECULES FOR DUAL FUNCTION POSITRON EMISSION TOMOGRAPHY (PET) AND CELL SUICIDE SWITCHES
20190070321 · 2019-03-07 ·

The present invention includes an engineered cell comprising a chimeric antigen receptor (CAR) further comprising a nucleic acid molecule comprising a suicide gene comprising a ligand binding domain and a suicide domain wherein the ligand binding domain is capable of binding to radiolabeled tracer or a small molecule suicide switch. This invention also includes methods for inducing apoptosis of an engineered cell, methods for assessing the efficacy or toxicity of an adoptive cell therapy in a subject, methods for detecting the quantity of engineered T cells in a subject, methods for monitoring an immunotherapy treatment in a subject and methods of imaging engineered T cells in a subject. In some embodiments, the imaging is performed via Positron Emission Topography (PET). This invention further includes a chemical inducer of dimerization (CID), wherein the CID is a Bis-Trimethoprim (Bis-TMP).

Imaging of Glycogen Synthase Kinase 3
20180370949 · 2018-12-27 ·

Provided herein are radiolabelled compounds useful for imaging GSK-3 kinase. An exemplary radiolabelled compound provided herein is useful as a radiotracer for imaging GSK-3 kinase using PET imaging. Methods for preparing the radiolabelled compounds and diagnostic methods using the radiolabelled compounds are also provided.

HETEROCYCLIC COMPOUNDS FOR CANCER IMAGING AND TREATMENT AND METHODS FOR THEIR USE

Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, X, n.sup.1, n.sup.2, and n.sup.3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

##STR00001##

Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (PSMA) where the compounds are represented by the following: ##STR00001## or a pharmaceutical y acceptable salt thereof, ##STR00002## or a pharmaceutically acceptable salt thereof, ##STR00003## or a pharmaceutically acceptable salt thereof,
wherein M.sup.1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.

1,4-disubstituted 1,2,3-triazoles, methods for preparing same, and diagnostic and therapeutic uses thereof

A compound having the following general formula (I): ##STR00001##
wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.

Methylsulfonamide Derivatives and Uses Related Thereto
20180228924 · 2018-08-16 ·

This disclosure relates to methylsulfonamide derivatives and uses as imaging agents and other uses related to CXCR4 inhibition. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein, derivatives, or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for imaging to study CXCR4 related conditions.

Nuclear medicine diagnostic imaging agent

Provided is a radioactive labeled compound capable of detecting a secondary mutation of an epidermal growth factor receptor, where the compound is represented by Formula (1) or a pharmaceutically acceptable salt thereof, where Y, L.sub.1, R.sub.1 and R.sub.2 are as defined. ##STR00001##

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.