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.

Disclosed is a method for production of an ester obtained from a reaction between at least one alcohol having at least one hydroxyl group, such as a diol, and at least one linear of branched C3-C20 monocarboxylic acid, said reaction being performed in presence of at least one azeotropic solvent and optionally at least one antioxidant. Said method comprises the steps of (a) charging said alcohol, said monocarboxylic acid, and said azeotropic solvent and optionally said antioxidant to a reactor, (b) subjecting said alcohol and said carboxylic acid to esterification under reflux, (c) removing azeotropic solvent and unreacted carboxylic acid from yielded reaction mixture, (d) steam stripping off residual unreacted carboxylic acid, (e) neutralising yielded reaction product with an aqueous base, (f) separating water and organic phases, (g) recovering said organic phase and evaporating residual water, and (h) filtering off said antioxidant and possible remaining salts in yielded reaction product. The method is preferably performed in at least one reactor equipped with reflux, at least one vacuum pump, evaporation/distillation, steam stripping and decantation, and at least one filtration unit and optionally at least one coalescer filtre.

Disclosed is a method for production of an ester obtained from a reaction between at least one alcohol having at least one hydroxyl group, such as a diol, and at least one linear of branched C3-C20 monocarboxylic acid, said reaction being performed in presence of at least one azeotropic solvent and optionally at least one antioxidant. Said method comprises the steps of (a) charging said alcohol, said monocarboxylic acid, and said azeotropic solvent and optionally said antioxidant to a reactor, (b) subjecting said alcohol and said carboxylic acid to esterification under reflux, (c) removing azeotropic solvent and unreacted carboxylic acid from yielded reaction mixture, (d) steam stripping off residual unreacted carboxylic acid, (e) neutralising yielded reaction product with an aqueous base, (f) separating water and organic phases, (g) recovering said organic phase and evaporating residual water, and (h) filtering off said antioxidant and possible remaining salts in yielded reaction product. The method is preferably performed in at least one reactor equipped with reflux, at least one vacuum pump, evaporation/distillation, steam stripping and decantation, and at least one filtration unit and optionally at least one coalescer filtre.

Compounds having a structure of Formula I

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Compounds having a structure of Formula I

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Disclosed are hydroquinone compounds, preparation methods therefor, and uses thereof in anti-tumor or immunomodulation. The structural formula of the hydroquinone compounds are shown by formula I, ##STR00001##
wherein X is CO or CH.sub.2; Y is NH, O or absent; R is a substituted or unsubstituted alkyl group having at least one carbon atom, a substituted or unsubstituted cycloalkyl group having at least three carbon atoms, a substituted or unsubstituted alkenyl group or alkynyl group having at least two carbon atoms; and a substituted or unsubstituted aryl group or heteroaryl group containing at least four carbon atoms. The compounds provided slowly release 2-tert-butyl-4-methoxyphenol in vivo and maintain stable plasma concentration of 2-tert-butyl-4-methoxyphenol (T=1224 h). The compounds provided by the present invention protect the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, avoid environmental oxidation and increase the environmental stability of drugs containing the compounds.

Disclosed are hydroquinone compounds, preparation methods therefor, and uses thereof in anti-tumor or immunomodulation. The structural formula of the hydroquinone compounds are shown by formula I, ##STR00001##
wherein X is CO or CH.sub.2; Y is NH, O or absent; R is a substituted or unsubstituted alkyl group having at least one carbon atom, a substituted or unsubstituted cycloalkyl group having at least three carbon atoms, a substituted or unsubstituted alkenyl group or alkynyl group having at least two carbon atoms; and a substituted or unsubstituted aryl group or heteroaryl group containing at least four carbon atoms. The compounds provided slowly release 2-tert-butyl-4-methoxyphenol in vivo and maintain stable plasma concentration of 2-tert-butyl-4-methoxyphenol (T=1224 h). The compounds provided by the present invention protect the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, avoid environmental oxidation and increase the environmental stability of drugs containing the compounds.

This invention is directed to, inter alia, compounds, methods, systems, and compositions for the maintenance, enhancement, and expansion of hematopoietic stem cells derived from one or more sources of CD34+ cells. Sources of CD34+ cells include bone marrow, cord blood, mobilized peripheral blood, and non-mobilized peripheral blood. Also provided herein are compounds of Formula I

##STR00001##

which are useful in maintaining, enhancing, and expanding of hematopoietic stem cells.

The present disclosure discloses prodrugs of gamma-hydroxybutyric acid as well as compositions and uses thereof.