C07J51/00

STEROL ANALOGS AND USES THEREOF
20220402965 · 2022-12-22 ·

The invention relates to compositions and methods for the preparation, manufacture, and therapeutic use of compositions comprising mRNA and a lipid nanoparticle comprising a compound of the invention and an ionizable lipid.

METHOD FOR PREPARING ALKENYL AMINOBORANES AND THEIR DERIVATIVES, AND USES THEREOF
20220396591 · 2022-12-15 ·

Disclosed is a method for preparing alkenyl aminoboranes and their derivatives, and uses thereof. The method for preparing alkenyl aminoboranes includes contacting, preferably in a single synthesis step, a terminal alkyne, an aminoborane and a catalyst chosen from Schwartz's reagent (Cp2ZrHCl), dicyclohexylborane (HBCy), diisopinocamphenylborane (HBipc2) and 9-Borabicyclo(3.3.1)nonane (9-BBN).

NMDAR INHIBITING AGENTS AND GABAAR POTENTIATING AGENTS AND USES THEREOF
20220396597 · 2022-12-15 · ·

N-methyl-d-aspartate receptors (NMDAR) and/or potentiating y-aminobutyric acid receptors (GABAAR) agents and uses thereof are described. Uses of these agents include methods of treating or preventing various psychiatric diseases, disorders, or conditions and methods of treating or preventing alcohol use disorder in a subject in need thereof.

Fluorinated bile acid derivatives

The invention relates to compounds of general formula (I): ##STR00001##
wherein R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.5, Y and R.sup.7 are as defined herein are selective agonists at the FXR receptor and are useful for the treatment or prevention of diseases and conditions including nonalcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; biliary atresia; cholestatic liver disease; hepatitis C infection; alcoholic liver disease; fibrosis; and liver damage arising from fibrosis.

3.ALPHA.-HYDROXY-17.BETA.-AMIDE NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF
20220372067 · 2022-11-24 ·

Provided herein is a compound of Formula (I) or pharmaceutically acceptable salt thereof, wherein R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.6, R.sup.7, R.sup.11a, R.sup.11b, R.sup.16, R.sup.17, R.sup.3, R.sup.5, R.sup.19 and R.sup.X are defined herein and wherein R.sup.Y represents optionally substituted heteroaryl. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

##STR00001##

ISOTOPICALLY LABELED BILE ACID DERIVATIVES

The present application relates to isotopically labeled compounds of Formula I and methods of preparation and use thereof

##STR00001##

Compositions and methods for sulfation of carbohydrates

In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

BILE ACID DERIVATIVE SALT, CRYSTAL STRUCTURE THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF
20230054001 · 2023-02-23 · ·

The present invention provides a salt of a bile acid derivative, a crystal form thereof, a preparation method therefor and use thereof. The salt of a bile acid derivative, the crystal form thereof and a composition thereof provided by the present invention can improve cholestasis, reduce portal pressure, and improve liver function, and can be used for preparing medicaments for treating or alleviating chronic liver diseases, metabolic diseases, portal hypertension and related diseases.

Polyethylene glycol-conjugated glucocorticoid prodrugs and compositions and methods thereof

Polyethylene glycol (PEG)-conjugated glucocorticoid prodrugs, methods of preparation, and use for the treatment of diseases and disorders are disclosed. In particular, PEG-conjugated dexamethasone compounds and methods of using them for treating inflammatory and autoimmune diseases, including but not limited to lupus, are disclosed.

OXYSTEROLS AND METHODS OF USE THEREOF

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

##STR00001##