C07D213/79

METHODS OF TREATING ELEVATED PLASMA CHOLESTEROL
20230088095 · 2023-03-23 ·

The present invention relates to compounds of Formula I, pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I increase significantly low density lipoprotein receptor and are useful for preventing and treating of elevated cholesterol.

PROCESS FOR THE PREPARATION OF 5-CHLORO-3-ALKYLSULFANYL-PYRIDINE-2-CARBOXYLIC ACID AMIDES AND CARBOXYLATES

##STR00001##

A process for the preparation of compound of formula (I) is provided: where R.sub.1 and R.sub.2 are as defined in the description.

PROCESS FOR THE PREPARATION OF 5-CHLORO-3-ALKYLSULFANYL-PYRIDINE-2-CARBOXYLIC ACID AMIDES AND CARBOXYLATES

##STR00001##

A process for the preparation of compound of formula (I) is provided: where R.sub.1 and R.sub.2 are as defined in the description.

KETAMINE COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM
20220348544 · 2022-11-03 ·

Disclosed are compounds comprising ketamine (2-(2-chlorophenyl)-2-(methylamino)-cyclohexanone) chemically conjugated to one or more oxoacids, amino acids, polyethylene glycols (PEG or PEO), peptides, phosphates, and/or vitamin compounds, and salts of such compounds. Also disclosed are compositions comprising at least one ketamine compound, or a salt thereof, methods of making such compounds, and methods of using such ketamine compounds and compositions.

KETAMINE COMPOUNDS AND PROCESSES FOR MAKING AND USING THEM
20220348544 · 2022-11-03 ·

Disclosed are compounds comprising ketamine (2-(2-chlorophenyl)-2-(methylamino)-cyclohexanone) chemically conjugated to one or more oxoacids, amino acids, polyethylene glycols (PEG or PEO), peptides, phosphates, and/or vitamin compounds, and salts of such compounds. Also disclosed are compositions comprising at least one ketamine compound, or a salt thereof, methods of making such compounds, and methods of using such ketamine compounds and compositions.

COMPOUNDS AND THEIR USE

The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where A, U, V, W, X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings defined herein. Such compounds are modulators of RXFP1 and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions including heart failure, heart failure with preserved ejection fraction, heart failure with mid-range ejection fraction, heart failure with reduced ejection fraction, chronic kidney disease and acute kidney injury. The specification further relates to compositions comprising such compounds, intermediates useful in processes for preparing such compounds, and processes for preparing such compounds using such intermediates.

Small molecule inhibitors of Ebola and Lassa fever viruses and methods of use

Disclosed herein are compounds having a structure of formula (I), compositions and methods useful for the treatment of a disease or infection, such as a viral infection (e.g., Ebola), cancer and obesity: ##STR00001##
wherein A is N or CR.sup.8; Z is ##STR00002## E is selected from optionally substituted alkyl, cycloalkyl, arylalkyl, cycloalkylalkyl, amino, alkoxy, cycloalkyloxy, and cycloalkylamino; R.sup.1 is selected from optionally substituted aryl and heteroaryl, R.sup.2 and R.sup.3 are independently selected from H, deutero, optionally substituted alkyl, haloalkyl, or R.sup.2 and R.sup.3, together with the carbon to which they are bound, combine to form a carbonyl; and R.sup.8 is selected from H, deutero, halo, hydroxyl, cyano, amino, alkyl, alkoxy, carboxy, alkoxycarbonyl, and aminocarbonyl,
provided that E is not ##STR00003##

NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS

The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

TEAD INHIBITORS AND USES THEREOF

The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

CO-CRYSTALS
20230116520 · 2023-04-13 ·

Co-crystals of itanapraced; methods of preparation of the co-crystals; uses of the co-crystals as APIs; formulations containing the co-crystals; uses of the co-crystals and formulations for prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries; and methods of prevention and treatment of neurodegeneration disorders, infections, dementias, inflammation, and injuries are described.