Patent classifications
C07C35/52
FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF
The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof:
##STR00001##
wherein each symbol is as defined in the specification.
Modulators of liver receptor homologue 1 (LRH-1) and uses
This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.
MODULATORS OF LIVER RECEPTOR HOMOLOGUE 1 (LRH-1) AND USES
This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.
CARBAMATE DERIVATIVE COMPOUNDS, PROCESSES FOR PREPARING THEM AND THEIR USES
The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a carbamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention CNS disorders comprising administering a carbamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of CNS disorders.
METHOD FOR PREPARING 3-CHLOROBICYCLO[3.2.1]-3-OCTEN-2-OL
Disclosed is a method for preparing 3-chlorobicyclo[3.2.1]-3-octen-2-ol, which belongs to the field of pharmaceutical technology. The method for preparing 3-chlorobicyclo[3.2.1]-3-octen-2-ol can be achieved by any of the following reaction routes: Reaction route I: 3,4-dichlorobicyclo[3.2.1]-2-octene is esterified in the presence of a carboxylate, and hydrolyzed in a strong base to obtain 3-chlorobicyclo[3.2.1]-3-octen-2-ol; Reaction route II: in the presence of an inorganic salt of strong base and weak acid, 3,4-dichlorobicyclo[3.2.1]-2-octene is reacted in a solvent to obtain 3-chlorobicyclo[3.2.1]-3-octen-2-ol. The present application can result in decreased formation of polymers and impurities, more obvious layering, and improved purification efficiency.
METHOD FOR PREPARING 3-CHLOROBICYCLO[3.2.1]-3-OCTEN-2-OL
Disclosed is a method for preparing 3-chlorobicyclo[3.2.1]-3-octen-2-ol, which belongs to the field of pharmaceutical technology. The method for preparing 3-chlorobicyclo[3.2.1]-3-octen-2-ol can be achieved by any of the following reaction routes: Reaction route I: 3,4-dichlorobicyclo[3.2.1]-2-octene is esterified in the presence of a carboxylate, and hydrolyzed in a strong base to obtain 3-chlorobicyclo[3.2.1]-3-octen-2-ol; Reaction route II: in the presence of an inorganic salt of strong base and weak acid, 3,4-dichlorobicyclo[3.2.1]-2-octene is reacted in a solvent to obtain 3-chlorobicyclo[3.2.1]-3-octen-2-ol. The present application can result in decreased formation of polymers and impurities, more obvious layering, and improved purification efficiency.
Modulators of liver receptor homologue 1 (LRH-1) and uses
This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.
Process of preparing 3-fluoro-5(((1R,2AR)-3,3,4,4-tetrafluoro-1,2A-dihydroxy-2,2A,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)-oxy)benzonitrile
Disclosed herein are processes for preparing certain intermediates useful in the synthesis of 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)oxy)benzonitrile or a pharmaceutically acceptable salt thereof.
Process of preparing 3-fluoro-5(((1R,2AR)-3,3,4,4-tetrafluoro-1,2A-dihydroxy-2,2A,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)-oxy)benzonitrile
Disclosed herein are processes for preparing certain intermediates useful in the synthesis of 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)oxy)benzonitrile or a pharmaceutically acceptable salt thereof.
MODULATORS OF LIVER RECEPTOR HOMOLOGUE 1 (LRH-1) AND USES
This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.