C07D249/06

ANTIBACTERIAL AND ANTIFUNGAL PLEUROMUTILIN CONJUGATES
20230219964 · 2023-07-13 ·

Compounds of formula (1) comprising a pleuromutilin backbone with a triazole based side-group at C22 are provided. The compounds can be used for treatment of bacterial infections and fungal infections. Importantly, infections caused by multidrug-resistant bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA) may be treated effectively.

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ACLY inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

COMPOUNDS USEFUL FOR TREATING LIVER DISEASES
20230008367 · 2023-01-12 · ·

This invention provides compounds of Formulae (A) and (B) and pharmaceutically acceptable salts, solvates, esters, amides, and prodrugs thereof, including 2-(4-(3-hydroxy-3-(4-(methylthio)phenyl)prop-1-en-1-yl)-2,6-dimethylphenoxy)-2-methylpropanoic acid (“Compound I”), 3-(4-((1-hydroxy-2-methylpropan-2-yl)oxy)-3,5-dimethylphenyl)-1-(4-(methylthio)phenyl)prop-2-en-1-one (“Compound II”) and 3-(4-((1-hydroxy-2-methylpropan-2-yl)oxy)-3,5-dimethylphenyl)-1-(4-(methylthio)phenyl)prop-2-en-1-ol (“Compound III”), and pharmaceutically acceptable salts, solvates, esters, amides, and prodrugs thereof. The invention further provides pharmaceutical compositions comprising a compound of Formulae (A) and (B) or a pharmaceutically acceptable salt, solvate, ester, amide, or prodrug thereof, including Compound I, Compound II, or Compound III, or a pharmaceutically acceptable salt, solvate, ester, amide, or prodrug thereof, and a pharmaceutically acceptable carrier or vehicle. The compounds and compositions disclosed herein are useful for treating or preventing liver disease such as liver fibrosis, fatty liver disease, non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH).

Triazole N-linked carbamoyl cyclohexyl acids as LPA antagonists

The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Triazole N-linked carbamoyl cyclohexyl acids as LPA antagonists

The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

LPA RECEPTOR ANTAGONISTS AND USES THEREOF

The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non-alcoholic steatohepatitis (NASH), interstitial lung disease (ILD), or chronic kidney disease (CKD).

Antifreezing coolant composition not including glycol

Disclosed is an antifreezing coolant composition, which does not include glycol but includes environmentally friendly materials, such as a carboxylic acid salt, an anthranilamide compound, a corrosion inhibitor and a triazole compound. The antifreezing coolant composition may form a thin film on the metal surface in cooling systems for vehicles to thereby exhibit high corrosion resistance at low and high temperatures, superior antifreezing performance at low temperatures, and superior cooling performance at high temperatures.

Antifreezing coolant composition not including glycol

Disclosed is an antifreezing coolant composition, which does not include glycol but includes environmentally friendly materials, such as a carboxylic acid salt, an anthranilamide compound, a corrosion inhibitor and a triazole compound. The antifreezing coolant composition may form a thin film on the metal surface in cooling systems for vehicles to thereby exhibit high corrosion resistance at low and high temperatures, superior antifreezing performance at low temperatures, and superior cooling performance at high temperatures.

TREATMENT OF MALARIA USING HISTONE DEACETYLASE (HDAC) INHIBITORS

The present invention provides methods for treating malaria. The methods of the present invention comprise administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising aN-hydroxy-4-((4-(4-(pyrrolidin-1-ylmethyl)phenyl)-1H-1,2,3-triazol-1-yl)methyl)benzamide.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, are featured (Formula A) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

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