Patent classifications
A61K51/0455
Targeted, metal-catalyzed fluorination of complex compounds with fluoride ion via decarboxylation
Methods of preparing fluorinated compounds by carboxylative fluorination using fluoride are contained herein. Fluorinated compounds are provided. Methods of using fluorinated compounds are contained herein.
USE OF FLUORINATED DERIVATIVES OF 4-AMINOPYRIDINE IN THERAPEUTICS AND MEDICAL IMAGING
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.
Radiolabeled Pharmaceuticals and Methods of Making and Using Same
In one aspect, the invention comprises compounds that bind to the synaptic vesicle protein SV2A and that can be useful as radiotracers for positron emission tomography. In another aspect, the invention comprises methods of imaging the brain, measuring synaptic density or diagnosing neurological diseases such as Alzheimer's disease, psychiatric disorders such as depression, and metabolic disorders such as diabetes comprising detecting the compounds of the invention by positron emission tomography (PET).
RADIOLABELLED MGL PET LIGANDS
The present invention relates to novel, selective, radiolabelled compound having monoacylglycerol lipase (MGL) affinity which are useful for imaging and quantifying MGL receptor expression, distribution and enzyme occupancy in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
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.
Imaging and radiotherapeutics agents targeting fibroblast-activation protein-alpha (FAP-alpha)
Imaging and radiotherapeutics agents targeting fibroblast-activation protein-? (FAP-?) and their use in imaging and treating FAP-? related diseases and disorders are disclosed.
COMPOUNDS FOR TAU PROTEIN DEGRADATION
Provided herein are bifunctional compounds that bind tau protein and/or promote targeted ubiquitination for the degradation of tau protein. In particular, provided are compounds that can bind tau protein, a protein whose aggregation is implicated in a variety of neurodegenerative disease (e.g., tauopathies), and can promote its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon), which can ubiquitinate tau protein, marking it for proteasomal degradation. Also provided are radiolabeled forms of the bifunctional compounds, pharmaceutical compositions comprising the bifunctional compounds, methods of detecting and/or diagnosing neurological disorders, methods of detecting and/or diagnosing pathological aggregation of tau protein (e.g., in the central nervous system), methods of treating and/or preventing neurological disorders, and methods of promoting the degradation of tau protein by E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.
Solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates and their use as precursors for therapeutic and/or diagnostic agents
The disclosure provides methods for the solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates. The disclosure also relates to key intermediates of this process and methods for their preparation such as a method of preparing a compound of formula (V). Also disclosed are use of the conjugates as precursors for therapeutic and/or diagnostic agents, including treating and diagnosing prostate cancer.
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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.
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.