C07B59/00

Macrocycle and composition comprising thereof
11517561 · 2022-12-06 · ·

A macrocycle represented by formula (I) and a pharmaceutical composition comprising the macrocycle, or a crystalline form, pharmaceutically acceptable salt, hydrate or solvent compound, stereoisomer, prodrug, or isotopic variant of the macrocycle. The macrocycle and the composition thereof inhibit a protein kinase.

METHODS AND MATERIALS FOR MAKING PET RADIOTRACERS

Embodiments of the present disclosure provide compositions comprising compounds useful to make radiotracers for positron emission tomography imaging, as well as methods for making and using these compositions.

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.

Deuterated compounds

The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V): ##STR00001##
and salts thereof, wherein R.sup.1, R.sup.2, A, and X.sub.10-X.sub.19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

Compounds, compositions, and methods

The present disclosure relates generally to LRRK2 inhibitors, or a pharmaceutically acceptable salt, deuterated analog, prodrug, tautomer, stereoisomer, or mixture of stereoisomers thereof, and methods of making and using thereof.

Radioactive compound for diagnosis of malignant melanoma and use thereof

The present invention provides a novel radioactive compound for imaging malignant melanoma and a use thereof as a contrast agent for PET imaging.

5-DEUTERO-THIAZOLIDINE-2,4-DIONE COMPOUNDS AND METHODS OF TREATING MEDICAL DISORDERS USING SAME
20220362220 · 2022-11-17 ·

The invention provides deuterium-enriched thiazolidine-2,4-dione compounds (i.e., deuterium-enriched glitazone compounds), enantiopure forms of deuterium-enriched glitazone compounds, pharmaceutical compositions, and methods of treating medical disorders, such as a metabolic disorder, neurological disorder, cancer, or other disorder using deuterium-enriched glitazone compounds, which are preferably in enantiopure form.

AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES

Compounds having the following formula I.

##STR00001##

or a stereoisomer or pharmaceutically-acceptable salt thereof, where R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

SYNTHESIS OF DEUTERATED ALDEHYDES
20220356139 · 2022-11-10 ·

Described are methods for preparing a deuterated aldehyde using N-heterocyclic carbene catalysts in a solvent comprising D.sub.2O. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions without functionality manipulation.