69 results about "Suberoylanilide Hydroxamic Acid" patented technology

The present invention relates to methods of treating cancers, e.g., mesothelioma or lymphoma. More specifically, the present invention relates to methods of treating mesothelioma or diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

The present invention relates to methods of treating cancers, e.g., lymphoma. More specifically, the present invention relates to methods of treating diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

The present invention is directed to prodrugs of hydroxamic acid based histone deacetylase (HDAC) inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The prodrugs are acylated derivatives having increased aqueous solubility and cellular permeability as compared with the free hydroxamic acid, and are useful for inhibiting HDACs, and for selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the prodrugs of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The prodrugs of the invention are also useful in the prevention and treatment of thioredoxin (TRX)-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

The invention relates to methods for monitoring patient response to histone deacetylase inhibitors (e.g., suberoylanilide hydroxamic acid (SAHA)) or other therapeutic agents by measuring the level of thioredoxin in body fluids, tissues, and/or cells, such as peripheral blood mononuclear cells, plasma, or serum. The invention also relates to methods of monitoring and/or assisting with the diagnosis of a wide variety of thioredoxin-related diseases and conditions, such as inflammatory diseases, allergic diseases, autoimmune diseases, diseases associated with oxidative stress or diseases characterized by cellular hyperproliferation.

The present invention relates to methods of treating cancers, e.g., leukemia. More specifically, the present invention relates to methods of treating acute and chronic leukemias including Acute Lymphocytic Leukemia (ALL), Acute Myeloid Leukemia (AML), Chronic Lymphocytic leukemia (CLL), Chronic myeloid leukemia (CML) and Hairy Cell Leukemia, by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

The present invention relates to methods of treating cancers, e.g., mesothelioma or lymphoma. More specifically, the present invention relates to methods of treating mesothelioma or diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.

A pharmaceutical composition for induction therapy which has a hypomethylating agent and a histone deacetylase inhibitor (“HDAC inhibitor”); wherein the hypomethylating agent is a DNA and histone methylation inhibitor such as cladribine and the HDAC inhibitor is, for example, entinostat, panobinostat, vorinostat, and/or romedepsin; further wherein the hypomethylating agent and the HDAC inhibitor are combined in formulations for various administrations including e.g., a continuous delivery system such as a transdermal patch of at least one reservoir or a plurality of reservoirs, oral, a fixed-dose oral combination, intravenous, and combinations thereof. This pharmaceutical composition for induction therapy is used with a monoclonal antibody in the treatment of various cancers, sarcomas, and other malignancies.

The invention discloses applications of vorinostat in aspect of drugs for treating autoimmune diseases. The experiment result disclosed by the invention shows that due to the vorinostat, the morbidity of the experimental autoimmune encephalomyelitis of mice is reudced, and also the average score, the highest score and the total score of clinical marks are reduced; spinal cord inflammatory cell infiltration and spinal cord demyelination can be alleviated; the weight percent of a cell Th1 related to IFN (Interferon)-gamma secretion and a cell Th17 cell related to IL-17A secretion accounting for positive T cells CD4 in the spleen can be reduced. Therefore the invention relates to the preparation of the drug for inhibiting the experimental autoimmune encephalomyelitis of an animal model, and the drug is expected to treat the diseases related to multiple sclerosis, ophthalmoneuromyelitis, acute disseminated encephalomyelitis and the like.

A composite medicine for treating B-cell leucoma is prepared from rituximab and suberoylanilide hydroxamic acid (SAHA). Its advantages are obvious synergistic effect, high curative effect and low cost.

The invention discloses a method for preparing an anticancer drug--Vorinostat. The method comprises the following steps: 1) subjecting a hydrophilic substrate and octanedioic acid to contacting and carrying out self-assembling so as to obtain an octanedioic acid-substrate self-assembled film; 2) in the presence of 1,3-dicyclohexylcarbodiimide, subjecting the octanedioic acid-substrate self-assembled film to contacting with aniline in THF, after a reaction is completed, adding a 4M HCl solution and carrying out a reaction under stirring, and carrying out extraction with dichloromethane so as to obtain octanedioic acid monoanilide; and 3) subjecting octanedioic acid monoanilide and hydroxylamine hydrochloride to a reaction so as to obtain Vorinostat. The preparation method for Vorinostat provided by the invention provides a novel synthetic route for Vorinostat. By adopting the method for preparing Vorinostat provided by the invention, mild conditions and good selectivity are achieved; the time of the reaction, specifically the time of the aniline amidation reaction, is greatly reduced; meanwhile, the yield of Vorinostat is greatly improved.

The invention discloses a marigold pollen differential medium and a differentiation culture method. The medium comprises KNO3, NH4NO3, KH2PO4.H2O, MgSO4.7H2O, CaCl2.2H2O, MnSO4.4H2O, ZnSO4.7H2O, H3BO3, KI, Na2MoO4.2H2O, CuSO4.5H2O, CoCl2.6H2O, ferrous glycine, inositol, thiamine hydrochloride, pyridoxine hydrochloride, niacin, threonine, asparagine, retinol, an air-plant herb extraction solution,6-BA, NAA, abscisic acid, vorinostat, 5-aminolevulinic acid, maltose, betaine and agar. By means of culture using the medium and the method, the plant differentiation rate of 70% or above can be obtained, and a certain technical support is provided for establishment of a marigold pollen high-efficiency culture system.