A61K51/0453

DEUTERATED AND TRITIATED N-(4,5-DIMETHYLTHIAZOLO-2(3H)-YLIDEN)-2,2,3,3-TETRAMETHYLCYCLOPROPANE-1-CARBOXAMIDE DERIVATIVES AND THE USE THEREOF

Compounds of general formula I

##STR00001##

X.sup.1 is a CD.sub.2 group or a CT.sub.2 group; X.sup.2 is oxygen or a group (CZ.sup.1Z.sup.2).sub.n, wherein Z.sup.1 and Z.sup.2 on each occurrence independently each are hydrogen, deuterium, or tritium and n is an integer from 1 to 12; X.sup.3 is a CD.sub.2 group or a CT.sub.2 group; and R is selected from the group consisting of hydroxy, -NO.sub.2, halogen, a diazonium ion, a diazonium salt, a trialkylammonium ion, a trialkylammonium salt, a dialkoxyarene, a sulphoxide, a boronic acid, a boronic acid ester, an organotin compound, an iodonium ion, an iodonium salt, an iodonium ylide, and a sulphonate.

PSMA-TARGETING COMPOUNDS AND USES THEREOF
20230348405 · 2023-11-02 ·

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

Radioligands for myelin

A radioligand for labeling myelin includes a fluorescent trans-stilbene derivative.

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. Methods of using the compounds to image cardiac innervation are also provided. 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.

PSMA-TARGETING COMPOUNDS AND USES THEREOF
20220259161 · 2022-08-18 ·

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

Selective ligands for tau aggregates

The invention provides compounds of formula (I) and compositions comprising compounds of formula (I). The invention further provides uses of the compounds of formula (I) and compositions comprising compounds of formula (I), including the use of such compounds for the detection of tau deposits, and the use of such compounds and compositions as diagnostic agents in the diagnosis or monitoring of the progression of a disease or disorder such as Alzheimer's disease or corticobasal degeneration, or for the prevention or treatment of a disease or disorder such as Alzheimer's disease or corticobasal degeneration. ##STR00001##

Method for removing acetaldehyde

A method for removing or controlling or quantifying the presence of aldehydes, in particular acetaldehyde, is described. Such a method is useful in prolonging the shelf life of a pharmaceutical product.

Method for labeling radioisotope radiolabeling compound and kit comprising the same for labeling radioisotope

The present disclosure relates to a method for labeling a radioisotope, a radiolabeling compound, a kit including the same, and a method for labeling a radioisotope, including: providing a diaminophenyl compound represented by Chemical Formula I below and including a biomolecule, a fluorescent dye or a nanoparticle compound bound thereto; and reacting the diaminophenyl compound and a radioisotope-labeled aldehyde compound represented by Chemical Formula II below at room temperature; and a related technology: ##STR00001## in Chemical Formula I, A is CH.sub.2 or O; a is 0 or an integer of 1 to 10; X is CH.sub.2 or —CONH—; Y is CH.sub.2 or ##STR00002##  and Z is the biomolecule, the fluorescent dye or the nanoparticle compound, ##STR00003## in Chemical Formula II, b is 0 or an integer of 1 to 10; and L is CH.sub.2 or —CONH—; and Q is ##STR00004## M, M′ and M″ in Q are radioisotopes.

SUBSTITUTED ORGANOFLUOROBORATES AS IMAGING AGENTS
20220062445 · 2022-03-03 ·

Fluoridated organofluoroborates comprising at least one .sup.18F atom and precursors thereto, for use in PET scanning.

MILD AND SITE-SELECTIVE 18F-LABELING OF SMALL MOLECULES AND/OR BIOMOLECULES VIA A THIOL-REACTIVE SYNTHON

Site-selective conjugation to biomolecules via thiol-based chemistry is superior to the unselective modification of lysine residues, which produce a mixed product and can potentially interfere with binding affinity of the biomolecule. However, in physiological environments, the maleimide-thiol conjugation product which is the current gold-standard for site-selective thiol-conjugation can be susceptible to hydrolysis or a retro-Michael reaction via exchange with reactive thiols such as those in albumin or glutathione residues yet the degradation is relatively slow. Therefore, for in vivo studies, the maleimide-thiol conjugation proposes instability issues. The compositions and methods disclosed herein provide an alternative thiol-based linkage, one that overcomes the instability issues with conventional reagents and methods. The compositions and methods disclosed herein are useful in various contexts, for example, for .sup.18F-labeling of peptides/proteins in the preparation of positron emission tomography (PET) probes.