Abstract: It has been found that the prodrug 1-(butyryloxy)ethyl-5-amino-4-oxopentanoate (AN-233), an oral active conjugate of BA (histone deacetylase inhibitor) and ALA (heme precursor), is useful for the treatment of hemoglobinopathies including but not limited to sickle cell disease and thalassemias. In one embodiment, AN-233 activates ?-globin transcription, induces HbF expression, produces an anti-sickling effect, or combinations thereof when administered to a subject in need thereof.

Abstract: Methods for treating ameliorating, reducing and/or preventing a cutaneous T-cell lymphoma in a subject in need thereof, comprising administration butyroyloxymethyl diethyl phosphate (AN-7) alone or combined with an additional anti-cancer therapy.

Abstract: Disclosed herein is a compound having general Formula I: wherein X, R1 and R2 are as defined herein, for use in methods of treating an inflammatory disease or disorder, treating or preventing anthracycline-induced cardiomyopathy, downregulating interleukin-6, MCP-1, TNF-?, and/or TLR4, and/or upregulating interleukin-10.

Abstract: Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.

Abstract: There are provided conjugates comprising 5-aminolevulinic acid (5-ALA), an aldehyde and a carboxylic acid (e.g., a histone deacetylase inhibitor), compositions comprising same, methods for their preparation and uses thereof for treatment of cancer and anemia, and for inducing erythropoiesis.

Abstract: The present invention provides drug conjugates comprising 5-aminolevulinic acid (ALA), an aldehyde and a carboxylic acid that may function as a histone deacetylase inhibitor (HDACI). These conjugates may serve as co-drugs which release a plurality of active species in vivo. The novel drug conjugates may be used, for the treatment or prevention of cancer in PDT-dependent and/or PDT-independent (nonPDT) treatments, as well as for cosmetic uses. In addition the present invention provides novel uses for both the novel and known compounds. According to some embodiments, the present invention provides drug conjugates (co-drugs) comprising (i) ALA, (ii) an aldehyde and (iii) a carboxylic acid that may function as a histone deacetylase inhibitor (HDACO for the treatment of anemia and/or for the induction of erythropoiesis.

Abstract: Methods and articles of manufacture for use in improving a cognitive function, utilizing a conjugate comprising a first moiety having GABA agonist activity and a second moiety having CNS activity being covalently linked to the first moiety, are disclosed. Also disclosed are methods and articles of manufacture of preventing onset or inhibiting progression of a cognitive impairment or dysfunction utilizing the disclosed conjugate.

Abstract: An acid addition salt of a nortriptyline-GABA conjugate, a novel crystalline form of a fumaric acid addition salt of a nortriptyline-GABA conjugate, and processes of preparing the forgoing are disclosed. Uses of the above-indicated forms of a nortriptyline-GABA conjugate in the treatment of CNS disorders, and in the treatment of pain in particular, are also disclosed. Further disclosed in a large-scale process of preparing a nortriptyline-GABA conjugate.

Abstract: Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.

Abstract: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

Abstract: The present invention provides drug conjugates comprising 5-aminolevulinic acid (ALA), an aldehyde and a carboxylic acid that may function as a histone deacetylase inhibitor (HDACI). These conjugates may serve as co-drugs which release a plurality of active species in vivo. The novel drug conjugates may be used, for the treatment or prevention of cancer in PDT-dependent and/or PDT-independent (nonPDT) treatments, as well as for cosmetic uses. In addition the present invention provides novel uses for both the novel and known compounds. According to some embodiments, the present invention provides drug conjugates (co-drugs) comprising (i) ALA, (ii) an aldehyde and (iii) a carboxylic acid that may function as a histone deacetylase inhibitor (HDACO for the treatment of anemia and/or for the induction of erythropoiesis.

Abstract: An acid addition salt of a nortriptyline-GABA conjugate, a novel crystalline form of a fumaric acid addition salt of a nortriptyline-GABA conjugate, and processes of preparing the forgoing are disclosed. Uses of the above-indicated forms of a nortriptyline-GABA conjugate in the treatment of CNS disorders, and in the treatment of pain in particular, are also disclosed. Further disclosed in a large-scale process of preparing a nortriptyline-GABA conjugate.

Abstract: A novel use of conjugates of psychotropic drugs (e.g., antidepressants or anti-epileptic drugs) and organic acids such as GABA in the treatment of pain is disclosed. A novel GABA conjugate and uses thereof is also disclosed.

Abstract: Novel crystalline form of perphenazine 4-aminobutyrate trimesylate and a process of producing the same are disclosed. The novel crystalline form is characterized by a unique XRPD pattern and a DSC that exhibits an endothermic peak at a relatively high temperature (e.g., higher than 209° C.). Also disclosed are a process of preparing perphenazine 4-aminobutyrate trimesylate by in situ deprotection and salification, in a single-step synthesis, and a highly pure perphenazine 4-aminobutyrate trimesylate obtained thereby. Uses of any of the described perphenazine 4-aminobutyrate trimesylate are also disclosed.

Abstract: A novel use of conjugates of psychotropic drugs (e.g., antidepressants or anti-epileptic drugs) and organic acids such as GABA in the treatment of pain is disclosed. A novel GABA conjugate and uses thereof is also disclosed.

Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.

Abstract: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.

Abstract: Conjugates of a gamma-aminobutyric acid (GABA) compound or a glycine compound and an analgesic drug are disclosed. Further disclosed are pharmaceutical compositions containing these conjugates and uses thereof in the treatment of CNS-associated diseases or disorders, optionally in combination with a psychotropic drug.

Abstract: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.