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512 results about "Histone deacetylase inhibitor" patented technology
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Histone deacetylase inhibitors (HDAC inhibitors, HDACi, HDIs) are chemical compounds that inhibit histone deacetylases. HDIs have a long history of use in psychiatry and neurology as mood stabilizers and anti-epileptics. More recently they are being investigated as possible treatments for cancers, parasitic and inflammatory diseases.
Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase
InactiveUS6905669B2Better clinical outcomeReduce dosageBiocideCell receptors/surface-antigens/surface-determinantsCyclic peptideDisease
Compositions and methods are provided for treating diseases associated with aberrant silencing of gene expression such as cancer by reestablishing the gene expression through inhibition of DNA hypomethylation and histone deacetylase. The method comprises: administering to a patient suffering from the disease a therapeutically effective amount of a DNA methylation inhibitor such as a cysteine analog such as decitabine, in combination with an effective amount of histone deacetylase inhibitor such as hydroxamic acid, cyclic peptide, benzamide, butyrate, and depudecin.
Owner:SUPERGEN
Histone deacetylase inhibitors and methods of use thereof
The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
Owner:GEORGETOWN UNIV
Compositions and methods for treatment of cancer
Compositions and methods for treatment of conditions related to the overexpression of EZH2, such as late stage prostate cancer, using a DNA methylation inhibitor and / or a histone deacetylase inhibitor, optionally in combination with an EZH2 antagonist and / or an antineoplastic agent, to specifically target diseases associated with EZH2 over-expression. Further provided are reagents and kits for treatment of EZH2 overexpression.
Owner:SUPERGEN
Histone deacetylase inhibitors and cognitive applications
InactiveUS20060018921A1Enhances long-term passive avoidance memoryImprove long-termBiocideNervous disorderAcetylationPoor memory
The present invention relates to the enhancement of cognition in an individual by delivery of a histone acetylation regulator, such as a histone deacetylase inhibitor. The individual may have normal or poor memory, and the poor memory may be the result of a pathogenic condition or a non-pathogenic condition, such as with normal aging-related impairment. In a specific embodiment, enhancement of cognition occurs in an individual having a mental retardation syndrome.
Owner:BAYLOR COLLEGE OF MEDICINE
Inhibitors of histone deacetylase
InactiveUS7868205B2Strong inhibitory activityBiocideGroup 4/14 element organic compoundsHistone deacetylaseStereochemistry
Owner:METHYLGENE
Composition and method for treating neurological disorders
InactiveUS20050037992A1Effective treatmentBetter clinical outcomeBiocideNervous disorderNervous systemFragile X chromosome
Compositions, kits and methods are provided for treating or preventing neurological disorders associated with aberrant silencing of gene expression by reestablishing the gene expression through inhibition of DNA methylation and / or histone deacetylase. The compositions and methods include administering to a patient suffering from the neurological disorder a therapeutically effective amount of a DNA methylation inhibitor, such as decitabine, preferably in combination with an effective amount of a histone deacetylase inhibitor. The compositions, kits and methods can be used to treat or present neurological disorders such as Lou Gehrig's disease, fragile X syndrome, Parkinson's disease and Alzheimer's disease.
Owner:SUPERGEN
Spirocyclic derivatives as histone deacetylase inhibitors
This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C═R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
Owner:GENEXTRA SPA
Formulation comprising histone deacetylase inhibitors
InactiveUS20070232528A1Inhibition becomes largerInhibit HDAC target enzymesBiocideSenses disorderValproic AcidApoptosis
The present invention relates to an orally available galenics formulation of Valproic Acid or derivatives thereof exhibiting a specific bi-phasic pharmacokinetic profile optimized for maximum inhibition of histone deacetylases in a therapeutic setting. This specific galenics formulation is designed for the treatment of malignant diseases and diseases associated with hypoacetylation of histones or in which induction of hyperacetylation has a beneficial effect, e.g., by induction of differentiation and / or apoptosis. Due to the bi-phasic release pattern the resulting pharmacokinetic profile is able to inhibit HDAC target enzymes most efficiently and to subsequently induce histone hyperacetylation in a rapid as well as a long-lasting fashion. This profile secures the efficient modulation of a desired target gene expression profile which contributes to the therapeutic benefit.
Owner:TOPOTARGET GERMANY AG +1
Therapeutic agent for soft tissue sarcoma
A therapeutic agent for soft tissue sarcoma (particularly synovial sarcoma), contains a histone deacetylase inhibitor (particularly a compound of formula I) as an active ingredient
Owner:ASTELLAS PHARMA INC
Hydroxamates as inhibitors of histone deacetylase
ActiveUS20100317678A1Improve permeabilityProlong the action timeBiocideNervous disorderDiseaseHydroxamic acid
Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers:wherein Q, V and W independently represent —N═ or —C═; B is a divalent radical selected from (B1), (B2), (B3), (B4), (B5) and (B6).wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical; and R is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— or (b) a radical of formula R-L1-Y1—(CH2)z—,
Owner:GLAXOSMITHKLINE INTPROP DEV LTD
Method of using histone deacetylase inhibitors and monitoring biomarkers in combination therapy
ActiveUS20080153877A1Lower Level RequirementsInhibitory activityBiocideMicrobiological testing/measurementPharmaceutical drugBiologic marker
Provided herein are methods for using at least one histone deacetylase inhibitor to decrease cellular DNA repair activity, methods for monitoring the decrease of cellular DNA repair activity using at least one biomarker, methods of treating cancer by using at least one histone deacetylase inhibitor to decrease cellular DNA repair activity in combination therapy, methods of combination therapy where at least one histone deacetylase inhibitor interferes with a DNA repairing mechanism involving RAD51, methods for predicting a induction time period between a first administration of at least one histone deacetylase inhibitor and a second administration of at least one other therapeutic treatment, and pharmaceutical compositions for combination therapy.
Owner:PHARMACYCLICS
Promotion of adoptosis in cancer cells by co-administration of cyclin dependent kinase inhibitiors and cellular differentiation agents
The invention provides compositions and methods for promoting apoptosis of cancer cells, and methods for treating cancer. The compositions comprise cyclin dependent kinase inhibitor and an agent that induces cellular differentiation. The methods of promoting apoptosis of cancer cells involve the co-administration to the cancer cells of a cyclin dependent kinase inhibitor and an agent that induces cell differentiation. The method for treating cancer involves the co-administration of a cyclin dependent kinase inhibitor and an agent that induces cellular differentiation to a patient. Examples of cyclin dependent kinase inhibitors include histone deacetylase inhibitors, protein kinase C activators, retinoids, and Vitamin D3.
Owner:VIRGINIA COMMONWEALTH UNIV
Method for increasing therapeutic gain in radiotherapy and chemotherapy
InactiveUS20050272644A1Inhibit tumor growthReduced radiation-induced normal tissue fibrosisBiocideAntipyreticAbnormal tissue growthTumor therapy
The present invention provides compositions and methods for increasing therapeutic gain in radiotherapy and chemotherapy for proliferating malignant or nonmalignant disease to produce high probability of tumor control with low frequency of sequelae of therapy by administering a therapeutically effective amount of a histone deacetylase inhibitor. The compounds are capable of simultaneously stimulating the epithelium regrowth, inhibiting the fibroblast proliferation, decreasing the collagen deposit, suppressing the fibrogenic growth factor, subsiding the proinflammatory cytokine and modulating the expression of cell cycle genes, tumor suppressors and oncogenes, and are useful to increase the therapeutic gain in radiotherapy and chemotherapy, which results in decrease of skin swelling and inflammation, promotion of epithelium healing in mucosa and dermis, decrease of xerostomia, prevention / reduction of severity of plantar-palmar syndrome, prevention of tissue fibrosis, ulceration, necrosis and tumorigenesis, and increase of tumor growth inhibition and tumor therapy effectiveness.
Owner:SUNNY PHARMTECH
3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors
ActiveUS20160222028A1Useful in treatmentOrganic active ingredientsNervous disorderDiseaseHydroxamic acid
![3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors](https://images-eureka.patsnap.com/patent_img/b31837b1-af5c-47fc-b00f-34bbda87ea97/US20160222028A1-20160804-C00001.PNG "3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors")
![3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors](https://images-eureka.patsnap.com/patent_img/b31837b1-af5c-47fc-b00f-34bbda87ea97/US20160222028A1-20160804-C00002.PNG "3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors")
![3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors](https://images-eureka.patsnap.com/patent_img/b31837b1-af5c-47fc-b00f-34bbda87ea97/US20160222028A1-20160804-C00003.PNG "3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors")
Owner:VALO HEALTH INC
![3-alkyl bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors](https://images-eureka.patsnap.com/patent_img/386a7737-e24b-423f-80c4-039885e4580e/US20160221972A1-20160804-C00001.PNG "3-alkyl bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors")
![3-alkyl bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors](https://images-eureka.patsnap.com/patent_img/386a7737-e24b-423f-80c4-039885e4580e/US20160221972A1-20160804-C00002.PNG "3-alkyl bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors")
![3-alkyl bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors](https://images-eureka.patsnap.com/patent_img/386a7737-e24b-423f-80c4-039885e4580e/US20160221972A1-20160804-C00003.PNG "3-alkyl bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors")
Inhibitors of Histone Deacetylase
ActiveUS20140080802A1Increasing synaptic densityIncreasing synaptic plasticityAntibacterial agentsBiocideDiseaseFungal disease
The present invention relates to compounds of formula (I):or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and / or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders / impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
Owner:THE BROAD INST INC +2
Spirocyclic derivatives as histone deacetylase inhibitors
This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C═R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
Owner:GENEXTRA SPA
Histone deacelylase inhibitors in diagnosis and treatment of thyroid neoplasms
InactiveUS20040132643A1Increase count rateAdequate imagingBiocideRadioactive preparation carriersLymphatic SpreadRadioactive iodine therapy
Disclosed herein are novel approaches to thyroid cancer therapy. These approaches include methods to enhance thyroid specific gene expression, for example methods to enhance expression of thyroglobulin and / or the Na<+> / I<-> symporter in thyroid cancer cells. Enhanced expression of thyroid-specific genes promotes cellular differentiation and reduces biologically aggressive behavior such as invasion and metastasis. In addition, enhanced expression of thyroglobulin and / or the Na<+> / I<31 > symporter increases the ability of thyroid cancer cells to concentrate iodine or iodide, thereby making the cells more susceptible to radioactive iodine therapy. Also disclosed herein are methods for detecting thyroid neoplasms in a subject, by administering a therapeutically effective amount of a histone deacetylase inhibitor, administering a detectable agent whose uptake or concentration in thyroid cells is increased by administration of the histone deacetylase inhibitor, and detecting the detectable agent.
Reduced FK228 and use thereof
The present invention relates to reduced FK228 of the formula (I)wherein R1 and R2 are the same or different and each is a hydrogen atom or a thiol-protecting group, or a salt thereof, and a histone deacetylase inhibitor containing this compound, an expression potentiator and a reactivation promoter of a transgene, and pharmaceutical agents containing them as active ingredients. The reduced FK228 or a salt thereof has a strong histone deacetylase inhibitory activity and this compound can be used for the prophylaxis or treatment of various diseases, in which histone deacetylation is involved, and for the gene therapy of such diseases.
Owner:ASTELLAS PHARMA INC
HDAC inhibitors and therapeutic methods using the same
ActiveUS9249087B2High sensitivityDegree of isoform selectivity for an HDACIOrganic active ingredientsOrganic chemistryAutoimmune diseaseMalaria
Owner:THE CHILDRENS HOSPITAL OF PHILADELPHIA +1
Benzimidazole derivates: preparation and pharmaceutical applications
InactiveUS20070043043A1Low toxicityPotent anti-proliferative activityBiocideSenses disorderBenzimidazole derivativeDisease cause
The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).
Owner:MEI PHARM INC
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
Combinations of histone deacetylase inhibitors and immunomodulatory drugs
The invention relates to combinations comprising an HDAC inhibitor and an immunomodulatory drug for the treatment of multiple myeloma in a subject in need thereof. The combinations may, optionally, further comprise an anti-inflammatory agent, such as dexamethasone. Also provided herein are methods for treating multiple myeloma in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations.
Owner:DANA FARBER CANCER INST INC +1
Combinations of histone deacetylase inhibitors and immunomodulatory drugs
ActiveUS20150150871A1Achieve effectOrganic active ingredientsPharmaceutical non-active ingredientsImmunomodulatory drugLymphoid Tumor
The invention relates to combinations comprising an HDAC inhibitor and an immunomodulatory drug for the treatment of lymphoma in a subject in need thereof. Also provided herein are methods for treating lymphoma in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations.
Owner:ACETYLON PHARMA
Histone deacetylase inhibitors of novel benzamide derivatives with potent differentiation and anti-proliferation activity
ActiveUS7244751B2Effective againstConvenient treatmentBiocideOrganic chemistryProliferation activityPsoriasis
The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g. cancer and psoriasis
Owner:SHENZHEN CHIPSCREEN BIOSCIENCES CO LTD
Medicinal use of histone deacetylase inhibitor and method of evaluating antitumor effect thereof
A therapeutic agent for prostate cancer and malignant lymphoma containing FK228 or a salt thereof as an active ingredient, and a method for evaluating an antitumor effect of a histone deacetylase inhibitor which includes at least a step of treating a test cell with a histone deacetylase inhibitor, a step of measuring change in the expression amount of a specific gene in the test cell before and, after the treatment with the inhibitor, comparing the both expression amounts.
Owner:ASTELLAS PHARMA INC
Naphthamide Derivatives As Multi-Target Protein Kinase Inhibitors and Histone Deacetylase Inhibitors
ActiveUS20100298358A1Highly effective against hematologicalBiocideNervous disorderAutoimmune conditionPTK Inhibitors
Isolated compounds of formula I:and stereoisomers, enantiomers, diastereomers, and pharmaceutically acceptable salts thereof are described, as well as processes for production, and methods of use of these compounds and compositions thereof for the treatment of diseases associated with abnormal protein kinase activities and / or abnormal histone deacetylase activities including, for example, inflammatory diseases, autoimmune diseases, cancer, neurological and neurodegenerative diseases, cardiovascular diseases, metabolic disease, allergies and asthma and / or hormone-related diseases.
Owner:SHENZHEN CHIPSCREEN BIOSCIENCES CO LTD
Antitumor agent
ActiveUS20050187149A1Improve anti-tumor effectEliminate side effectsBiocideOrganic active ingredientsCross-linkMetabolite
An antitumor agent containing, in combination, at least one kind of antitumor agent selected from the group consisting of an antitumor agent that forms a cross-link with DNA and shows an antitumor effect, an antimetabolite antitumor agent and a taxane antitumor agent, and a histone deacetylase inhibitor. According to the present invention, an antitumor agent causing reduced side effects and having a superior antitumor activity can be provided.
Owner:ASTELLAS PHARMA INC
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