C07B59/00

Microfluidic cassette for synthesizing a radio-tracer and method of synthesizing a radio-tracer with such a cassette
11471850 · 2022-10-18 · ·

The present application concerns a microfluidic cassette for synthesizing a radiotracer including a microfluidic circuit in a support card that includes at least one intake for supply by a vial, at least one isotope port, at least one reaction chamber, at least one mixing chamber, at least one formulation chamber, and at least one connection for a syringe, linked together by capillaries. Also disclosed is a method for synthesizing a radiotracer in such a cassette.

Deuterated N,N-dimethyltryptamine compounds

Compounds, compositions, methods, and uses are described for therapeutic deuterated N,N-dimethyltryptamine compounds (e.g., a single compound or a plurality of deuterated N,N-dimethyltryptamine compounds) such as N,N-dimethyltryptamine compounds, α-protio, α-deutero-N,N-dimethyltryptamine compounds, α,α-dideutero-N,N-dimethyltryptamine compounds, and pharmaceutically acceptable salts of these compounds. The deuterated N,N-dimethyltryptamine compound may have an increased half-life compared with the half-life of undeuterated N,N-dimethyltryptamine. For example, a deuterated N,N-dimethyltryptamine compound may be used in therapy and have a Formula (I): ##STR00001## wherein: the ratio of deuterium:protium in the compound is greater than that found naturally in hydrogen; each R.sup.1 is independently selected from H and D; R.sup.2 is selected from CH.sub.3 and CD.sub.3; R.sup.3 is selected from CH.sub.3 and CD.sub.3; each .sup.yH is independently selected from H and D, or a pharmaceutically acceptable salt thereof.

METHODS AND SYSTEMS THAT NORMALIZE IMAGES, GENERATE QUANTITATIVE ENHANCEMENT MAPS, AND GENERATE SYNTHETICALLY ENHANCED IMAGES
20230123208 · 2023-04-20 · ·

The current document is directed to digital-image-normalization methods and systems that generate accurate intensity mappings between the intensities in two digital images. The intensity mapping generated from two digital images is used to normalize or adjust the intensities in one image in order to produce a pair of normalized digital images to which various types of change-detection methodologies can be applied in order to extract differential data. Accurate intensity mappings facilitate accurate and robust normalization of sets of multiple digital images which, in turn, facilitates many additional types of operations carried out on sets of multiple normalized digital images, including change detection, quantitative enhancement, synthetic enhancement, and additional types of digital-image processing, including processing to remove artifacts and noise from digital images.

CASSETTE FOR STABILISED RADIOLABELLING REACTION

The present invention provides a method for the synthesis of an injectable composition comprising a [.sup.18F]-labelled pyridaben derivative that is advantageous over prior methods. In particular, the method of the present invention comprises a method of radiosynthesis that permits a more facile purification using solid phase extraction (SPE).

Targeted Radiopharmaceutical for Tumor and Its Use in the Imaging-guided Combination Therapy of Targeted Radiotherapy and Immunotherapy
20230117927 · 2023-04-20 ·

A pharmacological composition contains a complex having a structurally modified RGD polypeptide a radionuclide. This pharmacological composition is useful for diagnosis or treatment of the integrin αvβ3-positive tumors. The pharmacological composition may further contain an immunotherapeutic medicament and an optional nanoantibody molecular imaging probe. Treatment with a PD-L1 blockade after the targeted radioactive therapy can archive the optimal synergic efficacy. Moreover, with administration of PD-1 or PD-L1 nanoantibody molecular imaging probe, expression of PD-1 or PD-L1 in the tumor after targeted radiotherapy can be observed.

ELUENT SOLUTION

The present invention provides a novel method for the preparation of .sup.18F-fluoride (.sup.18F) for use in radiofluorination reactions. The method of the invention finds use especially in the preparation of .sup.18F-labelled positron emission tomography (PET) tracers. The method of the invention is particularly advantageous where bulk solutions are prepared and stored in prefilled vials rather than being freshly prepared on the day of synthesis. Also provided by the present invention is a radiofluorination reaction which comprises the method of the invention, as well as a cassette for use in carrying out the method of the invention and/or the radiofluorination method of the invention on an automated radiosynthesis apparatus.

ELUENT SOLUTION

The present invention provides a novel method for the preparation of .sup.18F-fluoride (.sup.18F) for use in radiofluorination reactions. The method of the invention finds use especially in the preparation of .sup.18F-labelled positron emission tomography (PET) tracers. The method of the invention is particularly advantageous where bulk solutions are prepared and stored in prefilled vials rather than being freshly prepared on the day of synthesis. Also provided by the present invention is a radiofluorination reaction which comprises the method of the invention, as well as a cassette for use in carrying out the method of the invention and/or the radiofluorination method of the invention on an automated radiosynthesis apparatus.

METHODS OF MANUFACTURING BENZOQUINOLINE COMPOUNDS
20230060294 · 2023-03-02 ·

The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof.

##STR00001##

COMPOSITIONS AND METHODS FOR PREPARING REGIO- AND STEREOSELECTIVE ALICYCLIC ALKENE ISOTOPOLOGUES AND STEREOISOTOPOMERS

A method for preparing isotopologues and/or stereoisotopomers of cyclic and heterocyclic alkenes and dienes is described. The method provides regio- and/or stereospecific addition of hydrogen, deuterium, tritium and a variety of other substituents to arenes, heteroarenes, and alicyclic compounds that have multiple carbon-carbon double bonds, thereby providing discrete isotopologues and stereoisotopomers of cyclic and heterocyclic alkenes and dienes with high isotopic purity and in high enantiomeric excess. Also described are isotopologues and stereoisotopomers of cyclic and heterocyclic alkenes and dienes, such as isotopologues and stereoisotopomers of cyclohexene and tetrahydropyridine, as well as products thereof, such as isotopologues and stereoisotopomers of piperidines and piperidine-containing compounds, such as methylphenidate. In addition, a method of determining the absolute configuration of stereoisotopomers of cyclohexenes is described.

Method of synthesizing .SUP.18.F radiolabeled biomolecular agents

A method for preparing .sup.18F radiolabeled biomolecules and agents for .sup.18F-PET imaging is disclosed herein. A perfluoroaryl-conjugated target tracer is synthesized and purified with temperature and solvent conditions that are mild for the tracer molecule. The purified perfluoroaryl-conjugated target tracer is then labeled with .sup.18F using .sup.18F salts within a short reaction time, and with temperature and solvent conditions that are mild for the tracer molecule. The method provides a quick and convenient process that maintains the biological activities of the target molecules. The radio-labeled biomolecules may be used as contrast agents for Positron Emission Tomography (PET).