Patent classifications
A61K51/0455
MACROCYCLIC COMPLEXES OF RADIONUCLIDES AND THEIR USE IN 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 Formulas (I), or a pharmaceutically acceptable salt thereof (IA), or a pharmaceutically acceptable salt thereof (II), 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.
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RADIOLABELLED AND NONRADIOLABELLED PEGYLATED COMPOUNDS AND USES THEREOF
The disclosure provides compounds for detecting neurodegeneration and/or identifying and monitoring the progression of inflammation in neurodegenerative diseases. The disclosure further provides compounds that inhibit the activity of monoamine oxidases, and uses thereof.
NOVEL DEUTERIUM SUBSTITUTED POSITRON EMISSION TOMOGRAPHY (PET) IMAGING AGENTS AND THEIR PHARMACOLOGICAL APPLICATION
The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.
Half-Curcuminoids as Amyloid-Beta PET Imaging Agents
Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.
FIBROBLAST ACTIVATION PROTEIN (FAP) TARGETED IMAGING AND THERAPY IN FIBROSIS
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.
MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 4
The present application provides picolinamide compounds that can be used as allosteric positron emission tomography (“PET”) imaging probes. Methods of using these compounds for treating a neurodegenerative disease are also provided.
TAU PET IMAGING LIGANDS
The present invention relates to novel, selective radiolabelled tau ligands which are useful for imaging and quantifying tau aggregates, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue or a subject, in vitro or in vivo, and to precursors of said compounds.
RADIOLABELLED COMPOUND OF A QUATERNARY AMMONIUM SALT OF A POLYCYCLIC AROMATIC AMINE AND METHODS OF MANUFACTURING AND DIAGNOSTIC USE THEREOF
The disclosure relates to a radioisotope-labelled compound having a structure according to formula I, wherein a wavy line indicates a single bond between a non-nodal carbon atom of a polycyclic aromatic system and an R.sup.1 substituent selected from a hydrogen; a halogen; a hydroxy; a protected hydroxy; a C.sub.1-4 alkoxy; a nitro group; an amino group; an amino group having 1 hydrogen replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogens replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogen atoms replaced with C.sub.2-5 alkylene to form a heterocyclic ring; a chain C.sub.1-6 carbon group; a chain C.sub.1-6 carbon group having a substituent selected from a halogen, carboxyl, a formyl, and a C.sub.1-4 alkanesulfonic; a phenyl group; a phenyl group having 1-5 substituents independently selected from halogens, a chain C.sub.1-6 carbon, a halogenated chain C.sub.1-6 carbon substituent, a hydroxy, a protected hydroxy, a C.sub.1-4 alkoxy, and an amino group having 1-2 atoms of hydrogen replaced with C.sub.1-6 alkyl; wherein R.sup.2 is a chain aliphatic substituent having: a total of 1-16 carbon atoms, an atom of .sup.18F fluorine radioisotope replacing a hydrogen atom at one of the carbon atoms, and a —CH.sub.2 fragment as a terminal member of a chain, wherein the chain connects to one of a hydrogen, a phenyl group, and a phenyl group having 1-3 substituents selected from halogens and C.sub.1-6 alkyl, and wherein if the chain contains at least 2 carbon atoms and there is a bivalent link between the chain carbon atoms, then the bivalent link is selected from the group consisting of an oxygen atom —O—, a sulfur atom —S—, and a C.sub.3-6 cycloalkylene; wherein R.sup.3 and R.sup.4 are combined to form a bivalent butadienyl-1,3 substituent whose terminal carbon atoms are linked to adjacent non-nodal carbon atoms of a B ring to form an aromatic C ring fused with an A and B ring system, having R.sup.1 substituents at non-nodal carbon atoms; wherein n is an integer of 9; wherein X.sup.− is a pharmaceutically acceptable counter ion selected from: an anion of a mono-basic inorganic acid, a mononegative anion of a multi-basic inorganic acid, an anion of an alkane carboxylic acid, an anion of an aliphatic sulfonic acid, an anion of an aromatic sulfonic acid, an anion of an acidic amino acid, a hydrate thereof, and a solvate thereof.
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SYSTEMS AND METHODS FOR PLATFORM AGNOSTIC WHOLE BODY IMAGE SEGMENTATION
Presented herein are systems and methods that provide for automated analysis of three-dimensional (3D) medical images of a subject in order to automatically identify specific 3D volumes within the 3D images that correspond to specific anatomical regions (e.g., organs and/or tissue). Notably, the image analysis approaches described herein are not limited to a single particular organ or portion of the body. Instead, they are robust and widely applicable, providing for consistent, efficient, and accurate detection of anatomical regions, including soft tissue organs, in the entire body. In certain embodiments, the accurate identification of one or more such volumes is used to automatically determine quantitative metrics that represent uptake of radiopharmaceuticals in particular organs and/or tissue regions. These uptake metrics can be used to assess disease state in a subject, determine a prognosis for a subject, and/or determine efficacy of a treatment modality.
18F - TAGGED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) AND THEIR USE AS IMAGING AGENTS FOR PROSTATE CANCER
The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer.