Patent classifications
C07D209/18
Carbocyanines for G-quadruplex DNA stabilization and telomerase inhibition
Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.
Carbocyanines for G-quadruplex DNA stabilization and telomerase inhibition
Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.
INHIBITORS OF APOL1 AND METHODS OF USING SAME
The disclosure provides at least one entity chosen from compounds of Formula (I)
##STR00001##
pharmaceutically acceptable salts thereof, solvates of any of the foregoing, and deuterated derivatives of any of the foregoing, compositions comprising the same, and methods of using the same, including use in treating APOL1 mediated kidney disease.
INHIBITORS OF APOL1 AND METHODS OF USING SAME
The disclosure provides at least one entity chosen from compounds of Formula (I)
##STR00001##
pharmaceutically acceptable salts thereof, solvates of any of the foregoing, and deuterated derivatives of any of the foregoing, compositions comprising the same, and methods of using the same, including use in treating APOL1 mediated kidney disease.
DRG-MDM2-1 FOR USE AS A NOVEL MOUSE DOUBLE MINUTE 2 (MDM2) INHIBITOR
The invention relates to compound shown with formula (I) or a pharmaceutically acceptable derivative thereof for use as a novel inhibitor of MDM2 activity.
##STR00001##
DRG-MDM2-1 FOR USE AS A NOVEL MOUSE DOUBLE MINUTE 2 (MDM2) INHIBITOR
The invention relates to compound shown with formula (I) or a pharmaceutically acceptable derivative thereof for use as a novel inhibitor of MDM2 activity.
##STR00001##
METHOD FOR PURIFYING INDOLE-3-LACTIC ACID FROM LACTOBACILLUS PLANTARUM FERMENTATION SUPERNATANT
The present invention discloses a method for purifying indole-3-lactic acid from a Lactobacillus plantarum fermentation supernatant, using a fermentation supernatant of Lactobacillus plantarum ZJ316 with a deposit number CCTCC NO: M 208077, including the following steps: adsorbing the fermentation supernatant with a macroporous resin XAD-16 first, then performing elution, collecting an eluate corresponding to 50% methanol with a pH of 7, and concentrating the eluate to obtain a concentrate; performing separation on the concentrate through dextrangel G25 to obtain a G25-2 fraction; and purifying the G25-2 fraction by reversed-phase high performance liquid chromatography, and concentrating the collected eluate to obtain the indole-3-lactic acid. The indole-3-lactic acid obtained in the present invention has a purity of 99.00%, and has broad-spectrum antibacterial activity.
METHOD FOR PURIFYING INDOLE-3-LACTIC ACID FROM LACTOBACILLUS PLANTARUM FERMENTATION SUPERNATANT
The present invention discloses a method for purifying indole-3-lactic acid from a Lactobacillus plantarum fermentation supernatant, using a fermentation supernatant of Lactobacillus plantarum ZJ316 with a deposit number CCTCC NO: M 208077, including the following steps: adsorbing the fermentation supernatant with a macroporous resin XAD-16 first, then performing elution, collecting an eluate corresponding to 50% methanol with a pH of 7, and concentrating the eluate to obtain a concentrate; performing separation on the concentrate through dextrangel G25 to obtain a G25-2 fraction; and purifying the G25-2 fraction by reversed-phase high performance liquid chromatography, and concentrating the collected eluate to obtain the indole-3-lactic acid. The indole-3-lactic acid obtained in the present invention has a purity of 99.00%, and has broad-spectrum antibacterial activity.
NUCLEAR RECEPTOR MODULATORS
The invention provides compounds of Formula (I)
##STR00001##
pharmaceutically acceptable salts, thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological conditions.
NUCLEAR RECEPTOR MODULATORS
The invention provides compounds of Formula (I)
##STR00001##
pharmaceutically acceptable salts, thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological conditions.