C07B59/002

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.

Deuterated compounds as inhibitors of the BCL6 BTB domain protein-protein interaction and/or as BCL6 degraders

The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB and/or by degrading BCL6, such as cancer.

Deuterated analogs of elacridar

The present invention relates to efflux inhibitor compounds, compositions, and methods of using the same. More specifically, the instant invention comprises deuterated analogs of elacridar with superior pharmacokinetic properties such that it is now possible to facilitate accumulation and distribution of therapeutic agents to effective levels in cells or compartments protected by efflux transporter proteins such as Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP). Such transporter protected compartments include brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, stem cells, and solid tumors. In other embodiments, the present invention comprises methods of using the instant deuterated analogs.

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.

DIACYLGLYERCOL KINASE MODULATING COMPOUNDS

The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.

Radiolabeled Darapladib and analogs thereof and their use as imaging compounds

The present inventors have developed new radiolabeled Darapladib and analogs thereof which can be used for the specific detection of vulnerable atherosclerotic plaques by targeting lipoprotein-associated phospholipase A2 (Lp-PLA2) which is a biomarker of choice concerning inflammation and atherosclerosis progression. Thus, the present invention relates to radiolabeled Darapladib and analogs thereof and their use as imaging compounds.

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.

METHOD FOR PRODUCING AROMATIC ASTATINE COMPOUND

This method for producing an aromatic astatine compound comprises reacting an aromatic iodonium ylide with astatine to produce an aromatic astatine compound.

PLURALITY OF HOST MATERIALS AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME
20220356193 · 2022-11-10 ·

The present disclosure relates to a plurality of host materials comprising at least one first host compound and at least one second host compound, and an organic electroluminescent device comprising the same. By comprising a specific combination of the compounds wherein the first host compound is represented by formula 1 and the second host compound is represented by formula 2, it is possible to provide an organic electroluminescent device having improved driving voltage, luminous efficiency, power efficiency and/or lifetime property.