Abstract: The present disclosure addresses this need by providing crystalline fine particle forms of PRX-3140 potassium salt, methods for preparation and the treatment for Alzheimer's disease (AD) and other dementias affecting the cholinergic and/or serotonergic systems including post-traumatic stress disorder (PTSD). In certain aspects, the present disclosure provides novel methods of preparing the compound of Formula I thereof, or PRX-3140 potassium salts, crystalline fine particle forms of PRX-3140 potassium salt, and compositions comprising them. In certain aspects, the present disclosure provides novel crystalline fine particle form of PRX-3140 potassium salt which may provide advantages including improved bioavailability and stability relative to other crystalline or amorphous forms. In other aspects, the present disclosure provides oral dosage forms of crystalline fine particle form of PRX-3140 potassium salt and excipients with improved stability.

Abstract: The present disclosure addresses this need by providing crystalline fine particle forms of PRX-3140 potassium salt, methods for preparation and the treatment for Alzheimer's disease (AD) and other dementias affecting the cholinergic and/or serotonergic systems including post-traumatic stress disorder (PTSD). In certain aspects, the present disclosure provides novel methods of preparing the compound of Formula I thereof, or PRX-3140 potassium salts, crystalline fine particle forms of PRX-3140 potassium salt, and compositions comprising them. In certain aspects, the present disclosure provides novel crystalline fine particle form of PRX-3140 potassium salt which may provide advantages including improved bioavailability and stability relative to other crystalline or amorphous forms. In other aspects, the present disclosure provides oral dosage forms of crystalline fine particle form of PRX-3140 potassium salt and excipients with improved stability.

Abstract: The present disclosure addresses this need by providing crystalline fine particle forms of PRX-3140 potassium salt, methods for preparation and the treatment for Alzheimer's disease (AD) and other dementias affecting the cholinergic and/or serotonergic systems including post-traumatic stress disorder (PTSD). In certain aspects, the present disclosure provides novel methods of preparing the compound of Formula I thereof, or PRX-3140 potassium salts, crystalline fine particle forms of PRX-3140 potassium salt, and compositions comprising them. In certain aspects, the present disclosure provides novel crystalline fine particle form of PRX-3140 potassium salt which may provide advantages including improved bioavailability and stability relative to other crystalline or amorphous forms. In other aspects, the present disclosure provides oral dosage forms of crystalline fine particle form of PRX-3140 potassium salt and excipients with improved stability.

Abstract: Methods for stereoselective synthesis and manufacturing of 2?-deoxynucleosides, such as 2?-ribonucleosides, are disclosed. In some embodiments, the 2?-deoxynucleoside is a ?-anomer of a 2?-deoxynucleoside having a 3? ? hydroxyl, 4? ? hydroxymethyl configuration. Nonlimiting examples of compounds prepared by the disclosed methods include 4?-thio-2?-deoxycytidine (T-dCyd) and 5-aza-4?-thio-2?-deoxycytidine (5-aza-T-dCyd; aza-T-dCyd; aza-T-dC).

Abstract: Methods for stereoselective synthesis and manufacturing of 2?-deoxynucleosides, such as 2?-ribonucleosides, are disclosed. In some embodiments, the 2?-deoxynucleoside is a ?-anomer of a 2?-deoxynucleoside having a 3? ? hydroxyl, 4? ? hydroxymethyl configuration. Nonlimiting examples of compounds prepared by the disclosed methods include 4?-thio-2?-deoxycytidine (T-dCyd) and 5-aza-4?-thio-2?-deoxycytidine (5-aza-T-dCyd; aza-T-dCyd; aza-T-dC).