C07B59/00

Metal Tricarbonyl Complexes Comprising Substituted Iminodiactic Acid Ligands and Uses as Radioisotope Tracers
20220306663 · 2022-09-29 ·

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 .sup.99mTc or Re. In certain embodiments, the ligands are substituted with a fluorine, a fluorine-18(F.sup.18) radioisotope, or other radionuclide.

RADIOLIGANDS FOR IMAGING THE ID01 ENZYME

The present invention relates to radiolabeled IDO1 inhibitors or pharmaceutically acceptable salts thereof which are useful for the quantitative imaging of IDO enzymes in mammals.

MODULATOR OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR, PHARMACEUTICAL COMPOSITIONS, METHODS OF TREATMENT, AND PROCESS FOR MAKING THE MODULATOR

Compounds of Formula I:

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pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.

PROCESS FOR PREPARING ENANTIOMERICALLY ENRICHED JAK INHIBITORS

Improved processes and intermediates for preparing ruxolitinib and deuterated analogs of ruxolitinib are disclosed.

CARBOXYLIC ACID COMPOUND, METHOD FOR PREPARATION THEREOF, AND USE THEREOF
20170233376 · 2017-08-17 ·

The present invention relates to the technical field of medicine, and specifically relates to the carboxylic acid compound represented by the chemical formula I or chemical formula II, and a pharmaceutically acceptable salt, a prodrug, and a solvate thereof, and a method for preparation thereof, as well as a pharmaceutical composition containing the described substances, and a use thereof.

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CXCR4 Receptor Antagonists

The compounds of formula (I) are antagonists of the CXCR4 receptor

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Wherein R.sup.1, X, Y and R.sup.2 are as defined in the claims.

METHOD FOR CHIRAL RESOLUTION AND DEVICE THEREFOR
20170226027 · 2017-08-10 ·

The present invention relates to method for chiral resolution of chiral species contained in a liquid placed in a cell formed by an inner wall and an outer wall surrounding the inner wall over at least a portion of the inner wall, each of the outer and inner walls being a solid of revolution about a longitudinal axis, the outer and inner walls being coaxial to one another, the method comprising: rotating the outer wall in one direction of rotation with respect to the inner wall for generating a Taylor-Couette flow within the liquid; collecting at least one of the chiral species.

The present invention also relates to a device therefor.

METAL OXIDE CATALYZED RADIOFLUORINATION

Inter alia, the first titania-catalyzed [.sup.18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [.sup.18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.

METAL OXIDE CATALYZED RADIOFLUORINATION

Inter alia, the first titania-catalyzed [.sup.18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [.sup.18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.

Benzoquinoline Inhibitors of Vesicular Monoamine Transporter 2
20220267317 · 2022-08-25 ·

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

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