Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

Abstract: The present disclosure encompasses embodiments of a novel near-infrared-emitting molecular fluorophore and probes incorporating said fluorophore advantageous for in vitro and in vivo research studies. The fluorophore is robust, photostable, and possesses functionalities for easy bioorthogonal conjugation (e.g., click chemistry, hydrazone formation, Diels Alder, Staudinger ligation, etc.). It is biocompatible and emits at 711 nm in aqueous conditions. These fluorophores may be used to fluorescently tag biological molecules or structures of interest, or used as optical reporters (i.e., activatable molecular probes, fluorescent dyes) for specific biomarkers/analytes as they can be switched from “off” to “on.” This fluorophore is useful for cellular assays and preclinical small animal imaging as the near-infrared emission is highly penetrating, and the photophysical properties are outstanding. As such, the properties of this class of fluorophores could easily be translated for use in clinical applications.

Abstract: The present invention relates to a curcumin derivative, a method for producing same, and a photo-acoustic imaging agent comprising the curcumin derivative for detecting beta-amyloid plaque. The curcumin derivative, expressed by chemical formula 1, according to the present invention exhibits superb selective bonding with beta-amyloid, thereby allowing beta-amyloid to be detected by means of an optical or photo-acoustic imaging methods, and, particularly, the curcumin derivative can highly effectively detect photo-acoustic signals with almost no noise by reacting to irradiation of light having a particular wavelength range, and thus can be useful as a composition for detecting beta-amyloid and for diagnosing diseases caused by excessive production of beta-amyloid.

Abstract: Among the various aspects of the present disclosure is the provision of compositions and methods for imaging and treating subjects with amyloidosis or multiple myeloma with or without amyloidosis.

Abstract: This document relates to compounds useful for targeting PARP1. Also provided herein are methods for using such compounds to detect and image cancer cells.

Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.

Abstract: This disclosure relates to compositions comprising substituted iminodiacetic acid ligands and metal tricarbonyl complexes containing the ligands and derivatives thereof. In certain embodiments, the metal tricarbonyl complexes are used as radioisotope tracers such as renal tracers. In certain embodiments, the metal complexes comprise 99mTc or Re. In certain embodiments, the ligands are substituted with a fluorine, a fluorine-18 (F18) radioisotope, or other radionuclide.

Abstract: The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof. wherein: R1 and R2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R3 is hydrogen or halogen; ring A is a benzene ring or a pyridine ring; ring B is selected from the group consisting of the following formulas (i), (ii), (iii), and (iv): in the formula (ii), Ra is alkyl; R4 and R5 are each separately selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl; and ??[Formula 3] represents a double bond or a triple bond. The above compound can be used as a molecular probe for imaging tau proteins that accumulate in the brain.

Abstract: The present invention relates to novel 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabelled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron-emission tomography (PET).

Abstract: The invention relates to products and methods that provide increased yields of certain radiopharmaceuticals.

Abstract: The present invention is directed to a novel compound of Formula 1 wherein the radiolabeled compound of Formula 1 is capable of being used as a radiotracer in PET imaging of a targeted localized tissue and targeted radionuclide therapy of one or more conditions that may be regulated or normalized via inhibition of transporter such as Pgp, BCRP or MRP I. The novel compounds of Formula 1 can also be used as substrates for binding with one or more ABC transporters. In particular, the present invention aids in diagnosis and therapeutic treatment of MDR disorders in all forms of cancers and neurological disorders of the central nervous system. The present invention further provides methods of preparation of compounds of Formula 1 and novel intermediates used in the preparation of compounds of Formula 1.

Abstract: Radioactive hydrogels for the delivery of localized radiotherapy, methods of making the radioactive hydrogels, and methods of using the radioactive hydrogels are disclosed. A radioisotope may be conjugated to a high molecular weight molecule, which may be encapsulated in a microparticle, where the microparticle is then dispersed within a hydrogel. The radioactive hydrogel may prevent leakage of the radioisotope to provide radiotherapy to a surgical margin while minimizing damage to surrounding normal tissue.

Abstract: The present invention relates to a hydroxamic acid-based contrast agent containing an isotope of fluorine, which comprises a compound having a structure of Formula (III): wherein R1 represents radioactive fluorine-18 (18F) or isotope fluorine-19 (19F), and R2 represents hydroxyamine —(NH)OH. The hydroxamic acid-based contrast agent containing an isotope of fluorine provided in the present invention has the capability of selectively inhibiting histone deacetylase (HDAC) subtypes 8/6/3, and specifically targets to the focus of spinocerebellar ataxia with over-activation of HDAC. By labeling with the radioisotope fluorine-18, a positron emission tomography (PET) image is obtained with the hydroxamic acid-based contrast agent containing radioisotope fluorine-18, whereby spinocerebellar ataxia is effectively detected.

Abstract: This present application relates to fluorescent tetrazine-containing compounds consisting of a single pi-system. For example, a compound of Formula (I): or a salt thereof, wherein: F is a fluorophore, L is a conjugated linker, and Tz is a substituted or unsubstituted tetrazine; wherein the linker bridges the Tz and F moieties in a single conjugated pi-system. Also provided herein are methods of using the compounds provided herein for biomedical imaging.

Abstract: The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue and decreased renal uptake in kidney, evidencing favorable pharmacokinetics of compounds of the present invention. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are also useful for initiating therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.

Abstract: Provided herein are monoacylglycerol lipase (MGLL) occupancy probes comprising a MGLL inhibitor containing a positron emission tomography (PET) tracer radionuclide. Also provided are methods of assessing MGLL enzyme occupancy of a MGLL inhibitor using the radiolabeled occupancy probes described herein.

Abstract: Selective chelation of bismuth radionuclide ions from a mixture including actinium radionuclide ions involves exposing a ligand to an aqueous solution that includes bismuth radionuclide ions and actinium radionuclide ions under conditions whereby the bismuth radionuclide ions selectively chelate to the ligand for form cationic complexes of the bismuth radionuclide ions. and separating the cationic complexes of the bismuth radionuclide ions from the actinium radionuclide ions. The ligands have a structure based on a 12-membered cyclen ring and may include pendant functional groups that can be derivatized with biological targeting vectors for targeted alpha therapy.

Abstract: 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 demyelinating diseases, and/or in vivo imaging of the central nervous system, and to diagnose and/or assess the progression of MS or other diseases.

Abstract: A Diels-Alder adduct of a trans-cyclooctene with a tetrazine is provided, wherein the adduct bears a substituent labeled with a radionuclide. A method of producing a PET or other image of an organ in an animal or human includes forming the Diels-Alder adduct in the animal or human. Trans-cyclooctenes and tetrazines suitable for preparing the adducts are provided.

Abstract: 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.