The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of ()-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of ()-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of ()-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of ()-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

The present invention relates to methods and strategies for extracting nitrosylated and/or nitrated derivatives and analogs from Myriciaria dubia fruit and for synthesizing the same. The ascorbic acid derivatives and analogs have the chemical structure of:

##STR00001##

where R.sub.1 is O, ONO, ONO.sub.2, or NH.sub.2; R.sub.2 is OH, ONO, ONO.sub.2, or NH.sub.2; R.sub.3 is OH, ONO, ONO.sub.2. The extraction method comprises freeze-drying the Myriciaria dubia fruit, mixing the freeze-dried powder with a solvent and separating and drying the supernatant. The synthetic method comprises derivatizing an ascorbic acid via nitrosylation and/or nitration in a buffered ascorbic acid solution, reducing zero or more nitro groups to an amine group, and purifying the ascorbic acid analog.

The present invention relates to methods and strategies for extracting nitrosylated and/or nitrated derivatives and analogs from Myriciaria dubia fruit and for synthesizing the same. The ascorbic acid derivatives and analogs have the chemical structure of:

##STR00001##

where R.sub.1 is O, ONO, ONO.sub.2, or NH.sub.2; R.sub.2 is OH, ONO, ONO.sub.2, or NH.sub.2; R.sub.3 is OH, ONO, ONO.sub.2. The extraction method comprises freeze-drying the Myriciaria dubia fruit, mixing the freeze-dried powder with a solvent and separating and drying the supernatant. The synthetic method comprises derivatizing an ascorbic acid via nitrosylation and/or nitration in a buffered ascorbic acid solution, reducing zero or more nitro groups to an amine group, and purifying the ascorbic acid analog.

Provided are compounds of Formula III that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided. ##STR00001##

Provided are compounds of Formula III that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided. ##STR00001##

The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

The present invention relates to an optically active axially chiral -allenic alcohol, a synthesis method and use thereof. The invention relates to a method of preparing a highly optically active chiral -allenic alcohol by using propargyl alcohol, aldehyde and chiral ,-diphenyl-L-prolinol under the protection of tert-butyldimethylsilyl with an accelerant zinc bromide. The axially chiral -allenic alcohol has the structural formula (I). The method of the present invention has the following advantages: the synthesis route is short, operations are simple, raw materials are readily available, separation and purification are convenient, the substrate has high universality, the total yield is high, and enantioselectivity and diastereoselectivity are high. The highly optically active axially chiral -allenic alcohol synthesized by the method of the present invention can conveniently synthesize 2,5-dihydrofuran compounds having central chirality and complete chirality, and at the same time can further synthesize axially chiral allenic amine and allenic malonic ester compounds having complete chirality. ##STR00001##

The present invention relates to an optically active axially chiral -allenic alcohol, a synthesis method and use thereof. The invention relates to a method of preparing a highly optically active chiral -allenic alcohol by using propargyl alcohol, aldehyde and chiral ,-diphenyl-L-prolinol under the protection of tert-butyldimethylsilyl with an accelerant zinc bromide. The axially chiral -allenic alcohol has the structural formula (I). The method of the present invention has the following advantages: the synthesis route is short, operations are simple, raw materials are readily available, separation and purification are convenient, the substrate has high universality, the total yield is high, and enantioselectivity and diastereoselectivity are high. The highly optically active axially chiral -allenic alcohol synthesized by the method of the present invention can conveniently synthesize 2,5-dihydrofuran compounds having central chirality and complete chirality, and at the same time can further synthesize axially chiral allenic amine and allenic malonic ester compounds having complete chirality. ##STR00001##

The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of ()-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of ()-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of ()-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of ()-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.