C07C217/22

Histone acetyltransferase modulators and uses thereof

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

Histone acetyltransferase modulators and uses thereof

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

UV CURED BENZOPHENONE TERMINATED QUATERNARY AMMONIUM ANTIMICROBIALS FOR SURFACES

The invention relates to benzophenone-terminated quaternary ammonium compounds, processes for preparing benzophenone-terminated quaternary ammonium compounds, environmentally friendly antimicrobial formulations of said quaternary ammonium compounds and their use as durable antimicrobial surface coatings for surfaces.

UV CURED BENZOPHENONE TERMINATED QUATERNARY AMMONIUM ANTIMICROBIALS FOR SURFACES

The invention relates to benzophenone-terminated quaternary ammonium compounds, processes for preparing benzophenone-terminated quaternary ammonium compounds, environmentally friendly antimicrobial formulations of said quaternary ammonium compounds and their use as durable antimicrobial surface coatings for surfaces.

PROCESS FOR THE PREPARATION OF 2,7-DIHYDROXY-9-FLUORENONE USEFUL FOR THE SYNTHESIS OF TILORONE AND ITS SALTS

Methods involving preparation of building blocks of 2,7-dihydroxy-9-fluorenone toward the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of tilorone, and an efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts are developed. The methods involve oxygenation of fluorene, nitration of fluorenone, followed by reduction and diazotization toward the formation of 2,7-dihydroxy-9-fluorenone, which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]-9-fluorenone-dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The synthesis method has relatively simple operation, mild reaction conditions, high yield, and simple process with yields of 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. Therefore, the research of its synthetic method being with a wide range of applications from the drug development and material synthesis point of view.

PROCESS FOR THE PREPARATION OF 2,7-DIHYDROXY-9-FLUORENONE USEFUL FOR THE SYNTHESIS OF TILORONE AND ITS SALTS

Methods involving preparation of building blocks of 2,7-dihydroxy-9-fluorenone toward the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of tilorone, and an efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts are developed. The methods involve oxygenation of fluorene, nitration of fluorenone, followed by reduction and diazotization toward the formation of 2,7-dihydroxy-9-fluorenone, which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]-9-fluorenone-dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The synthesis method has relatively simple operation, mild reaction conditions, high yield, and simple process with yields of 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. Therefore, the research of its synthetic method being with a wide range of applications from the drug development and material synthesis point of view.

ATX MODULATING AGENTS

Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.

COMPOSITIONS OF (Z)-ENDOXIFEN AND METHODS OF ENRICHMENT THEREOF

Described herein are methods of making (Z)-endoxifen, a salt thereof, crystalline forms of endoxifen, and compositions comprising them. Also described herein are crystalline forms of (Z)-endoxifen. A method of making (Z)-endoxifen may include one or more enrichment steps to enrich the amount of (Z)-endoxifen present in a composition. Enrichment may include one or more steps of crystallization, recrystallization, or fractional recrystallization to reduce the level of one or more impurities in the composition. These methods may be industrially scalable. Also described herein are compositions enriched for (Z)-endoxifen produced by the methods described herein.

COMPOSITIONS OF (Z)-ENDOXIFEN AND METHODS OF ENRICHMENT THEREOF

Described herein are methods of making (Z)-endoxifen, a salt thereof, crystalline forms of endoxifen, and compositions comprising them. Also described herein are crystalline forms of (Z)-endoxifen. A method of making (Z)-endoxifen may include one or more enrichment steps to enrich the amount of (Z)-endoxifen present in a composition. Enrichment may include one or more steps of crystallization, recrystallization, or fractional recrystallization to reduce the level of one or more impurities in the composition. These methods may be industrially scalable. Also described herein are compositions enriched for (Z)-endoxifen produced by the methods described herein.

HISTONE ACETYLTRANSFERASE MODULATORS AND USES THEREOF

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.