Patent classifications
C07C323/22
PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND
A process for the preparation of a polyunsaturated thiol comprising: (1) reacting a polyunsaturated alcohol in the presence of a compound of formula R.sub.2—SO.sub.2Hal wherein R.sub.2 is a C.sub.1-20 hydrocarbyl group, such an C.sub.1-10 alkyl group, to form a polyunsaturated sulphonyl ester; (2) converting the polyunsaturated sulphonyl ester to a polyunsaturated thioester by reacting with an anion of formula .sup.−SC(═O)R.sub.4 wherein R.sub.4 is a C.sub.1-20 hydrocarbyl group; (3) converting the polyunsaturated thioester to form a polyunsaturated thiol optionally in the presence of an antioxidant, e.g. using a metal carbonate. (4) reacting said polyunsaturated thiol with a compound (LG)R.sup.3COX wherein X is an electron withdrawing group and R.sup.3 is an alkylene group carrying a leaving group (LG), such as LG-CH.sub.2— forming
##STR00001## where X is an electron withdrawing group and LG is a leaving group; optionally in the presence of an antioxidant, so as to form a polyunsaturated ketone compound.
COMPOUNDS USEFUL FOR TREATING LIVER DISEASES
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).
COMPOUNDS USEFUL FOR TREATING LIVER DISEASES
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).
POLYETHYLENE GLYCOL DERIVATIVE AND USE THEREOF
Polyethylene glycol derivatives of the following formula I and uses thereof are disclosed. A method for manufacturing the polyethylene glycol derivatives is also disclosed.
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POLYETHYLENE GLYCOL DERIVATIVE AND USE THEREOF
Polyethylene glycol derivatives of the following formula I and uses thereof are disclosed. A method for manufacturing the polyethylene glycol derivatives is also disclosed.
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Benzamide or benzamine compounds useful as anticancer agents for the treatment of human cancers
The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not affect normally dividing cells.
Benzamide or benzamine compounds useful as anticancer agents for the treatment of human cancers
The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not affect normally dividing cells.
COMPOUNDS WITH ANTIMICROBIAL ACTIVITY
Provided herein are compounds useful in the treatment of bacterial infections, pharmaceuticals comprising the same, and methods of use and preparation thereof.
Compounds Useful for Treating Liver Diseases
This invention provides compounds, for example, of Formulae (A)-(H) and (J)-(AA) and pharmaceutically acceptable salts, solvates, esters, amides, and prodrugs thereof. The invention further provides pharmaceutical compositions comprising a compound of the invention, and a pharmaceutically acceptable carrier or vehicle. The compounds and compositions disclosed herein are useful for treating or preventing various diseases and conditions, for example liver disease such as liver fibrosis, fatty liver disease, non-alcoholic fatty liver disease (NAFLD) or non-alcoholic steatohepatitis (NASH), and kidney diseases such as acute kidney injury (AKI).
SULFUR AND AMIDE TROPOLONE INHIBITORS OF NUCLEOTIDYL TRANSFERASES AND USES THEREFOR
The present disclosure provides inhibitors of microorganisms including viruses and fungi of the formula (I) or (II) wherein the variables are defined herein. Also provided are methods of treatment using these agents in the treatment of infections of microorganisms such as viruses and fungi.
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