Patent classifications
A61K51/0453
COMPOSITIONS AND METHODS FOR DIAGNOSING VIRAL INFECTIONS INCLUDING COVID-19 AND FOR INFECTION SEVERITY MONITORING AS WELL AS TARGETED DETECTION OF CYTOKINE STORM
Compositions and methods for the diagnosis and treatment of infectious diseases, including for the diagnosis and treatment of Cytokine Storm and Cytokine Release Syndrome. The compositions may include a conjugate of a nucleoside analog, a chelator, and a label for use as imaging and therapeutic agents.
HETEROCYCLIC COMPOUNDS FOR CANCER IMAGING AND TREATMENT AND METHODS FOR THEIR USE
Compounds having a structure of Formula I:
##STR00001##
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.
Highly selective sigma receptor ligands and radioligands as probes in nociceptive processing and the pathphysiological study of memory deficits and cognitive disorders
A method for localizing and quantifying S1R role in nociceptive processing; for providing a guide to providing an analgesic therapy; of using an S1R selective ligand as a biomarker for pathphysiological study of memory deficits and cognitive disorders; or of detecting increased S1R density at the site of nerve injury arising from neuropathic pain comprising using as a probe at least one SR1 selective compound or radioligand of the general formula III′, or IV′: ##STR00001##
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.
Radiopharmaceutical products for diagnosis and therapy of adrenal carcinoma
A radiopharmaceutical composition is disclosed comprising novel iodometomidate derivatives of formula (I) which bind specifically to adrenal enzymes and which exhibit an improved stability. The compounds of formula (I) are suitable for use in a diagnostic imaging method, e.g. for diagnosis of adrenocortical carcinoma. The compounds of formula (I) are further suitable for use in the treatment of adrenocortical carcinoma, by means of radionuclide therapy.
Thioflavin derivatives for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition
This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's disease, familial Alzheimer's disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.
Fluorinated 2-arylbenzo heterocyclic compound with high affinity to Aβ 946; plaques and containing chiral side chain substituent, and preparation method and usage thereof
A fluorinated 2-arylbenzo heterocyclic compound with high affinity to Aβ plaques and containing a chiral side chain substituent, has a general formula (I) as follows: ##STR00001## wherein X is N; Y is S or O; Z is N or CH; R.sub.1 is a 5 or 6-substituent and is ##STR00002##
F is .sup.19F or .sup.18F; R.sub.2 is NHCH.sub.3 or N(CH.sub.3).sub.2. The compound of the present invention has high affinity to Aβ plaques and can be used to make appropriate radioactive nuclide labeling probes for early diagnosis of AD.
RADIOLIGANDS FOR PRETARGETED PET IMAGING AND METHODS OF THEIR THERAPEUTIC USE
Described herein are Tz/TCO-based pretargeting strategies using an Al[.sup.18F]-NOTA-labeled tetrazine radioligand. This imaging strategy enables delineation of cancer at earlier time points compared to other imaging strategies and further decreases the radiation dose to healthy tissues compared to directly labeled antibodies. Al-based .sup.18F imaging of small molecules, such as tetrazine, has not been previously achieved due to the decomposition of tetrazine during radiofluorination. Radiofluorination is advantageous over other radiolabeling methods because, in addition to having a shorter half-life, .sup.18F is more readily available to produce and therefore integrated into hospital workflows.
18F-RADIOLABELED BIOMOLECULES
The application is drawn to .sup.18F-radiolabeled residualizing agents and biomolecules and methods for radiolabeling biomolecules with radioactive fluorine atoms. The biomolecules have an affinity for particular types of cells and may specifically bind a certain cell, such as a cancer cell. Relevant biomolecules include antibodies, monoclonal antibodies, antibody fragments, peptides, other proteins, nanoparticles and aptamers. The application further provides compositions including such labeled biomolecules, as well as methods of using the labeled biomolecules and/or compositions in imaging applications.