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69 results about "Suberoylanilide Hydroxamic Acid" patented technology
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Vorinostat (rINN) also known as suberanilohydroxamic acid (suberoyl+anilide+hydroxamic acid abbreviated as SAHA) is a member of a larger class of compounds that inhibit histone deacetylases (HDAC). Histone deacetylase inhibitors (HDI) have a broad spectrum of epigenetic activities.
Methods of treating cancer with hdac inhibitors
InactiveUS20070060614A1Better pharmacokinetic profileImprove bioavailabilityBiocideAnimal repellantsDosing regimenOncology
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.
Owner:MERCK HDAC RESEARCH LLC +1
Methods of treating cancer with HDAC inhibitors
InactiveUS20060276547A1Better pharmacokinetic profileImprove bioavailabilityBiocideCyclic peptide ingredientsDosing regimenIn 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.
Owner:MERCK HDAC RESEARCH LLC +1
Histone Deacetylase Inhibitor Prodrugs
InactiveUS20090023786A1Increased aqueous solubilityImprove permeabilityBiocideNervous disorderAbnormal tissue growthHydroxamic acid
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.
Owner:MERCK HDAC RESEARCH LLC
Methods of treating cancer with HDAC inhibitors
InactiveUS20080249179A1Better pharmacokinetic profileImprove bioavailabilityBiocideOrganic chemistryDosing regimenIn vivo
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.
Owner:MERCK HDAC RESEARCH LLC +1
Methods of using SAHA and Bortezomib for treating cancer
The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Bortezomib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.
Owner:MERCK & CO INC
Use of thioredoxin measurements for diagnostics and treatments
InactiveUS20050288227A1Increase doseLower Level RequirementsPeptide/protein ingredientsMicrobiological testing/measurementPeripheral blood mononuclear cellAutoimmune condition
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.
Owner:SLOAN KETTERING INST FOR CANCER RES
Methods of treating mesothelioma with suberoylanilide hydroxamic acid
InactiveUS7148257B2Simple processPotent inhibitor of histone deacetylaseBiocideOrganic chemistryMesotheliomaCancer research
Owner:MERCK HDAC RESEARCH LLC +1
Hydroxamic acid compound, and preparation method and application thereof
InactiveCN103159646AMild reaction conditionsFew stepsOrganic chemistryRespiratory disorderDiseaseHydroxamic acid
The invention relates to the application areas of organic chemistry, pharmaceutical chemistry and medicine, and particularly discloses hydroxamic acid. The hydroxamic acid compound has a structure shown in Formula I, wherein R is selected from a substituted benzene ring, a heterocyclic ring, a substituted heterocyclic ring, a benzoheterocyclic ring or a substituted benzoheterocyclic ring, wherein the substitution refers to that 1-n hydrogen atoms on the benzene ring, heterocyclic ring or benzoheterocyclic ring are substituted by the following groups: halogen, amino, hydroxy, nitro, cyano, alkoxy, aminoalkyl, alkylamino, sulfoalkyl, perfluoroalkyl, perfluoroalkoxy, amido or alkoxycarbonyl. According to the invention, the hydroxamic acid compound achieves the purpose of treating neoplastic diseases by regulating histone deacetylase; the hydroxamic acid compound has anti-proliferation effect on tumor cells, influences cell cycle arrest and induces cell apoptosis; and above all, the anti-proliferation effect on lung cancer cell strains is obviously improved in comparison with the effect of a positive control drug SAHA (suberoylanilide hydroxamic acid).
Owner:GUANGDONG PHARMA UNIV
Methods of treating cancer with HDAC inhibitors
InactiveUS20080227862A1Better pharmacokinetic profileImprove bioavailabilityBiocideOrganic chemistryDosing regimenIn vivo
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.
Owner:MERCK HDAC RESEARCH LLC
Polymorphs of suberoylanilide hydroxamic acid
The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and / or apoptosis of neoplastic cells, and / or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective 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 also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.
Owner:MERCK HDAC RESEARCH LLC
Methods of using saha and bortezomib for treating multiple myeloma
InactiveUS20100113392A1Additive and synergistic therapeutic effectBiocideBoron compound active ingredientsAnticarcinogenHDAC inhibitor
The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Bortezomib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.
Owner:UNIV OF MARYLAND
Methods of using saha and bortezomib for treating cancer
Owner:MERCK SHARP & DOHME CORP
Polymorphs of suberoylanilide hydroxamic acid
ActiveUS20080228005A1Easy to followOrganic chemistry methodsCyclic peptide ingredientsDosing regimenApoptosis
Owner:MERCK HDAC RESEARCH LLC
Formulations of suberoylanilide hydroxamic acid and methods for producing same
ActiveCN101080223AAntineoplastic agentsAnhydride/acid/halide active ingredientsSolubilityActive component
The present invention provides a medicine composition or crystal composition which is provided with specific solubility characters, which includes octanedioyl aniline hydroxamic acids or its medicinal salt or hydrated compound as the active component. The invention also provides a method for preparing the crystal composition or medicine composition. The invention also provides a composition which is provided with specific particle size distribution.
Owner:MERCK SHARP & DOHME BV
Methods of treating cancer with HDAC inhibitors
InactiveCN1870985ATotal daily dose highInhibit deacetylase activityAnhydride/acid/halide active ingredientsDosing regimenBlood level
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.
Owner:MERCK HDAC RESEARCH LLC +1
Formulations Of Suberoylanilide Hydroxamic Acid And Methods For Producing Same
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.
Owner:MERCK SHARP & DOHME LLC
Histone deacetylase inhibitor and preparation method and application thereof
InactiveCN103845315APrevent proliferationInduced differentiationOrganic compound preparationCarboxylic acid amides preparationAbnormal tissue growthCancer cell
The invention discloses a histone deacetylase inhibitor and a preparation method and application thereof. The histone deacetylase inhibitor comprises a hydroxamic acid compound and a benzamide compound and is a novel compound which shows activity for inhibiting histone deacetylase and also shows a good inhibiting activity for in-vitro histone deacetylase; HDACs (Histone Deacetylases) are closely related with the growth and development of cancer. The histone deacetylase inhibitor is characterized in that the activity of the HDACs can be inhibited to effectively inhibit the proliferation of cancer cells and introduce the cancer cells to differentiate and reach apoptosis, so as to realize the purpose of treating tumor. The experiment result shows that the prepared histone deacetylase inhibitor is able to inhibit the growth of tumor cells; some of the compounds show the equivalent inhabitation for tumor cells as positive SAHA (Suberoylanilide Hydroxamic Acid), which proves that the prepared histone deacetylase inhibitor can be used for preparing antineoplastic drugs.
Owner:XI AN JIAOTONG UNIV
Composition for activating latent HIV virus and application thereof
ActiveCN109620954AFully activatedHigh induction activationAntiviralsAntibody ingredientsSide effectValproic Acid
The invention relates to the field of medicine, in particular to a composition for activating an HIV latent virus and application thereof. The composition consists of a monoclonal antibody drug, a histone deacetylase inhibitor and a PKC activator, wherein the monoclonal antibody drug is selected from an anti-human CD3 monoclonal antibody and an anti-human CD28 monoclonal antibody, the histone deacetylase inhibitor is selected from at least one of vorinostat and valproic acid, and a PKC activator is 12-deoxyphorbol-13-acetic acid (Prostratin). The main obstacle to cure the HIV is that the HIV establishes a hidden 'reservoir' of viruses in the body at the very early stage of infection. The composition has the effect of significantly activating latent HIV-infected CD4+ T cells, can activate the HIV latent virus simultaneously at the cellular level, the chromatin level and the HIV-specific transcription factor level, can fully activate the HIV pre-virus in the resting CD4+ T cells withoutsignificant cytotoxic side effects and is a necessary way to HIV functional healing.
Owner:WUHAN UNIV OF SCI & TECH
Histone deacetylase inhibitor prodrugs
InactiveUS8227636B2Good cell permeabilityPrevent proliferationBiocideNervous disorderAbnormal tissue growthHydroxamic acid
Owner:MERCK HDAC RESEARCH LLC
Method of using SAHA and Erlotinib for treating cancer
InactiveCN101300015ACarbohydrate active ingredientsAnhydride/acid/halide active ingredientsErlotinibHDAC inhibitor
The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Erlotinib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.
Owner:MERCK & CO INC +1
Pharmaceutical composition containing a hypomethylating agent and a histone deacetylase inhibitor
InactiveUS20110129521A1Good curative effectBiocideCarbohydrate active ingredientsTransdermal patchHistone methylation
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.
Owner:NIMBLE EPITECH
Method for promoting Chinese cabbage microspore embryogeny and direct seedling development
InactiveCN105028203APromote productionHigh seedling rate directlyPlant tissue cultureHorticulture methodsSporeMicrometer
The invention provides a method for promoting Chinese cabbage microspore embryogeny and direct seedling development so as to solve the problems that in an existing dissociative microspore culture technology, the microspore embryogeny rate is low, the direct seedling development rate is low, and the culture period is long. Histone histone deacetylase inhibitor-suberoylanilide hydroxamic acid (SAHA) is added to an induction medium NLN to increase the Chinese cabbage microspore embryogeny rate and the direct seedling development rate. In the NLN induction medium with SAHA of 0.025 micrometer to 0.10 micrometer added, the Chinese cabbage microspore embryogeny rate is increased by 1.42-4.35 times, and the direct seedling development rate is increased by 1.11-1.50 times.
Owner:SHENYANG AGRI UNIV
Applications of vorinostat in aspect of drugs for treating autoimmune diseases and inflammatory diseases
InactiveCN102793693AReduce infiltrationReduce morbidityOrganic active ingredientsSenses disorderImmunologic disordersAutoimmune responses
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.
Owner:TIANJIN MEDICAL UNIV
Medicinal composition for treating B cell lymph tumour
InactiveCN1824307AInduce apoptosisInhibition of growth and proliferationAntibody ingredientsAmine active ingredientsCurative effectCell growth
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.
Owner:RUIJIN HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
Combination of roscovitine and a hdca inhibitor to treat proliferative diseases
A first aspect of the invention relates to a combination comprising roscovitine, or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor selected from sodium butyrate, or a prodrug thereof, suberoylanilide hydroxamic acid (SAHA), sodium valproate and trichostatin A (TSA). A second aspect of the invention relates to a pharmaceutical product comprising roscovitine, or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor selected from sodium butyrate, or a prodrug thereof, suberoylanilide hydroxamic acid (SAHA), sodium valproate and trichostatin A (TSA) as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method for treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering roscovitine, or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor selected from sodium butyrate, or a prodrug thereof, suberoylanilide hydroxamic acid (SAHA), sodium valproate and trichostatin A (TSA) to a subject.
Owner:CYCLACEL
Vorinostat solid preparation
The invention discloses a Vorinostat solid preparation which is prepared from bulk drug Vorinostat and pharmaceutical adjuvant, wherein the pharmaceutical adjuvant comprises a filling agent, a disintegrating agent and a lubricating agent. The Vorinostat solid preparation is characterized in that the weight ratio of the Vorinostat to the filling agent is 1:0.9-4.5, the weight ratio of the Vorinostat to the disintegrating agent is 1:0.0834-0.4170, and the weight ratio of the Vorinostat to the lubricating agent is 1:0.0166-0.0830. The invention determines the doses of the disintegrating agent, the filling agent and the lubricating agent in the prescription of the Vorinostat solid preparation by creative experiments, and the dissolution of the Vorinostat solid preparation reaches more than 80% in 45 minutes.
Owner:PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
Method for preparing anticancer drug--Vorinostat
InactiveCN106187818AHigh yieldMild conditionsOrganic compound preparationCarboxylic acid amides preparationHydroxylamine HydrochlorideAniline
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.
Owner:THE AFFILIATED HOSPITAL OF QINGDAO UNIV
Marigold pollen differential medium and differentiation culture method
ActiveCN110547200AImproved growth and development characteristicsPromote differentiationHorticulture methodsPlant tissue cultureBetaineVitamin A Retinol
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.
Owner:济南易通城市建设集团股份有限公司
Preparation method and preparation of vorinostat I crystal form large grains
ActiveCN102643214AGood dissolution effectHigh commercial application valueOrganic active ingredientsOrganic chemistryMedicineCutaneous T-cell lymphoma
The invention provides a preparation method of vorinostat I crystal form large grains as a medicament for treating cutaneous T cell lymphoma and a preparation prepared from vorinostat obtained by the preparation method. The preparation method can crystallize in place once, is simple, effective and suitable for large-scale industrial production and further has greater commercial application value. The obtained preparation is good in dissolution effect.
Owner:杭州容立医药科技有限公司
Methods and compositions for promoting wound healing with decreased scar formation after glaucoma filtration surgery
InactiveUS20180369172A1Long-term and stable effectivenessHigh densityOrganic active ingredientsSenses disorderWound healingGlaucoma
Disclosed is a method of promoting wound healing with reduced scarring after glaucoma filtration surgery in a mammalian subject in need thereof, which involve the use of a HDAC inhibitor (HDACi), such as, but not limited to, suberoylanilide hydroxamic acid (SAHA).
Owner:U S GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS
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