Class / Patent application number | Description | Number of patent applications / Date published |
514575000 | Hydroxamic acid or salt thereof | 32 |
20080249179 | Methods of treating cancer with HDAC inhibitors - 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. | 10-09-2008 |
20090012175 | Methods of treating cancer with HDAC inhibitors - The present invention provides methods of treating cancers, chemoprevention, 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. | 01-08-2009 |
20090137679 | ZN2+Chelating Motif-Tethered Short-Chain Fatty Acids as a Novel Class of Histone Deacetylase Inhibitors | 05-28-2009 |
20100168242 | 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. | 07-01-2010 |
20100210729 | Methods of inducing terminal differentiation - 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. | 08-19-2010 |
20100286279 | Methods of Synthesis of Certain Hydroxamic Acid Compounds - The present invention pertains to the general field of chemical synthesis, and more particularly to methods for the synthesis of certain hydroxamic acid compounds, and in particular, (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as PXD101 and Belinostat®, comprising, for example, the steps of: (SAF) sulfonamide formation; (PUR | 11-11-2010 |
20100298439 | DERIVATIVES OF ARYLSULFONAMIDO-SUBSTITUTED HYDROXAMIC ACID AS MATRIX METALLOPROTEINASES INHIBITORS - Described herein are derivatives of arylsulfonamido-substituted hydroxamic acid of formula (I) having good solubility in water and inhibitory activity of matrix metalloproteinases, useful for the preparation of pharmaceutical compositions for the treatment of diseases associated to a pathologic activity and/or an over-expression of metalloproteinases, and of cosmetic preparations having anti-ageing properties in particular for hair and skin. | 11-25-2010 |
20110124731 | Treatment Of Neurodegenerative Diseases And Cancer Of The Brain Using Histone Deacetylase Inhibitors - The present application is directed to a method of treating diseases of the central nervous system (CNS) comprising administering to a individual in need of treatment a therapeutically effective amount of an inhibitor of histone deacetylase. In particular embodiments, the CNS disease is a neurodegenerative disease. In further embodiments, the neurogenerative disease is an inherited neurodegenerative disease, such as those inherited neurodegenerative diseases which are polyglutamine expansion diseases. The individual can be a mammal such as a primate or human. | 05-26-2011 |
20110263712 | PROCESS FOR THE PREPARATION OF VORINOSTAT - The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient vorinostat. In particular it relates to a process for preparing vorinostat substantially free from impurities, involving suberic acid, aniline and hydroxylamine as starting materials. | 10-27-2011 |
20110269838 | NOVEL PROCESSES AND PURE POLYMORPHS - The present invention relates to crystalline forms of the active pharmaceutical ingredient vorinostat, processes for their preparation and their use in pharmaceutical compositions. | 11-03-2011 |
20110281950 | COMPOSITIONS AND METHODS FOR REDUCING PROLIFERATION AND VIABILITY OF LYMPHOBLASTOID CELLS - Pharmaceutical compositions including an HDAC inhibitor and a pharmaceutically acceptable carrier wherein the HDAC inhibitor is present in an amount sufficient to achieve a plasma concentration from about 100 nM to about 2 uM and methods of treatment using the same. Pharmaceutical compositions including an HDAC inhibitor and a pharmaceutically acceptable carrier wherein the HDAC inhibitor is present in an amount from 0.1 mg to 100 mg. Pharmaceutical compositions including an HDAC inhibitor and a pharmaceutically acceptable carrier, wherein the concentration of the HDAC inhibitor is sufficient to decrease the relative viability of lymphoblastoid cells by at least about 50 percent and/or is sufficient to decrease the proliferation of lymphoblastoid cells by at least about 60 percent and/or is sufficient to decrease the relative viability of peripheral blood mononuclear cells by less than about 50 percent and methods of treatment using the same. | 11-17-2011 |
20110288177 | Methods for Preventing or Reducing Colon Carcinogenesis - The present invention is directed in part to methods of preventing or reducing colon carcinogenesis comprising administering to a patient at risk of colorectal cancer, a pharmaceutical preparation comprising a chemopreventive agent disclosed herein. | 11-24-2011 |
20110313044 | Polymorphs of Suberoylanilide Hydroxamic Acid - The present invention is directed to a novel form of suberoylanilide hydroxamic acid and the processes for its preparation. | 12-22-2011 |
20110313045 | HISTONE DEACETYLASES, AND USES RELATED THERETO - The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo. | 12-22-2011 |
20110319493 | HISTONE DEACETYLASES, AND USES RELATED THERETO - The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo. | 12-29-2011 |
20120004309 | Hydroxamic Acid Derivatives, Preparation and Therapeutic Uses Thereof - Disclosed are amino alkyl/aryl hydroxamic acid compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for degenerative diseases in mammal. | 01-05-2012 |
20130018103 | BIFUNCTIONAL HISTONE DEACETYLASE INHIBITORS - In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention. | 01-17-2013 |
20130165520 | Hybrid Molecule Having Mixed Retinoic Acid Receptor Agonism and Histone Deacetylase Inhibitory Properties - Hybrid molecules comprising a retinoic acid receptor agonist moiety and a histone deacetylase inhibitor (HDAC) moiety are disclosed. Hybrid molecule 3 (6-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)naphthalene-2-hydroxamic acid) was proven to posses HDAC activity while maintaining RAR agonist activity. Hybrid molecule 3 and pharmaceutical compositions thereof can be used in the treatment of breast cancer, leukemia, non-small cell lung cancer, colon cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and cancer of the CNS. | 06-27-2013 |
20130331455 | DEACETYLASE INHIBITORS AND USES THEREOF - The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds. | 12-12-2013 |
20140045943 | Hydroxamic Acid Derivatives, Preparation and Therapeutic Uses Thereof - Disclosed are amino alkyl/aryl hydroxamic acid compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for degenerative diseases in mammal. | 02-13-2014 |
20140051760 | Hybrid Molecule Having Mixed Retinoic Acid Receptor Agonism and Histone Deacetylase Inhibitory Properties - Hybrid molecules comprising a retinoic acid receptor agonist moiety and a histone deacetylase inhibitor (HDAC) moiety are disclosed. Hybrid molecule 3 (6-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)naphthalene-2-hydroxamic acid) was proven to posses HDAC activity while maintaining RAR agonist activity. Hybrid molecule 3 and pharmaceutical compositions thereof can be used in the treatment of breast cancer, leukemia, non-small cell lung cancer, colon cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and cancer of the CNS. | 02-20-2014 |
20140107211 | USE OF HDAC AND/OR DNMT INHIBITORS FOR TREATMENT OF ISCHEMIC INJURY - The present invention provides methods of ameliorating or reducing the extent of ischemic injury, reperfusion injury, and myocardial infarction, by administering an inhibitor of histone deacetylase enzyme (HDAC) or an inhibitor of DNA methyltransferase enzyme (DNMT). | 04-17-2014 |
20140142189 | METHIONINE ANALOGS AND METHODS OF USING SAME - Provided are methionine analogs which may be useful for inhibiting protein synthesis, inhibiting microbial growth and/or treating infectious diseases. In some instances, the analogs exhibit bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and/or antiviral properties. Also provided are methods of treatment and methods of preparation, as well as kits and unit dosages. | 05-22-2014 |
20140179787 | METHOD OF TREATING SPINAL CORD INJURY COMPRISING ADMINISTERING METAL CHELATORS TO THE UPPER ONE-THIRD OF THE NASAL CAVITY - Methods for treating the animal central nervous system against the effects of spinal cord injury, including associated cognitive, behavioral and physical impairments. Effective amounts of therapeutic agents are administered to the upper third of the patient's nasal cavity to bypass the blood-brain barrier and access the central nervous system directly to avoid unwanted and potentially lethal side effects. Therapeutic agents include those substances that interact with iron and/or copper such as iron chelators, copper chelators, and antioxidants. A particular example of a therapeutic agent is the iron chelator deferoxamine (DFO). | 06-26-2014 |
20140179788 | METHOD OF PRE-TREATING PATIENTS FOR STROKE COMPRISING ADMINISTERING METAL CHELATORS TO THE UPPER ONE-THIRD OF THE NASAL CAVITY - Methods for preconditioning and/or providing neuroprotection to the animal central nervous system against the effects of stoke, including associated cognitive, behavioral and physical impairments. Initially, a patient at risk for stroke is identified. Effective amounts of therapeutic agents are administered to the upper third of the at-risk patient's nasal cavity to bypass the blood-brain barrier and access the central nervous system directly to avoid unwanted and potentially lethal side effects. Therapeutic agents include those substances that interact with iron and/or copper such as iron chelators, copper chelators, and antioxidants. A particular example of a therapeutic agent is the iron chelator deferoxamine (DFO). | 06-26-2014 |
20140213655 | METHOD OF TREATING STROKE COMPRISING ADMINISTERING METAL CHELATORS TO THE UPPER ONE-THIRD OF THE NASAL CAVITY - Methods for treating the animal central nervous system against the effects of stoke, including associated cognitive, behavioral and physical impairments. Effective amounts of therapeutic agents are administered to the upper third of the stroke patient's nasal cavity to bypass the blood-brain barrier and access the central nervous system directly to avoid unwanted and potentially lethal side effects. Therapeutic agents include those substances that interact with iron and/or copper such as iron chelators, copper chelators, and antioxidants. A particular example of a therapeutic agent is the iron chelator deferoxamine (DFO). | 07-31-2014 |
20150018424 | PROCESS FOR THE PREPARATION OF VORINOSTAT - The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient vorinostat. In particular it relates to a process for preparing vorinostat substantially free from impurities. | 01-15-2015 |
20150148421 | Preservatives for Cosmetic, Toiletry and Pharmaceutical Compositions - A composition for and methods of preserving a topical cosmetic, toiletry or pharmaceutical formulation against microbiological contamination or growth are described in which the compositions used herein include at least one hydroxamic acid, salt or complex thereof, and the methods include addition of an effective amount of such compounds to a cosmetic, toiletry or pharmaceutical formulation. Compositions further including alkanediols and/or solubilizing agents in blends with hydroxamic acid are also described. | 05-28-2015 |
20150329481 | METHIONINE ANALOGS AND METHODS OF USING SAME - Provided are methionine analogs which may be useful for inhibiting protein synthesis, inhibiting microbial growth and/or treating infectious diseases. In some instances, the analogs exhibit bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and/or antiviral properties. Also provided are methods of treatment and methods of preparation, as well as kits and unit dosages. | 11-19-2015 |
20160045463 | USE OF METALLOPROTEASE INHIBITORS IN THE TREATMENT OF POLYCYSTIC LIVER DISEASES - The present invention comprises the use of metalloprotease inhibitors for the treatment of polycystic liver diseases (PLDs). The invention particularly describes the use of Marimastat as the preferred metalloprotease inhibitor for the treatment of PLDs. Treatment with Marimastat is able to inhibit liver cystogenesis by blocking metalloproteolytic hyperactivity of polycystic cholangiocytes. | 02-18-2016 |
20160199323 | CANCER TREATMENT | 07-14-2016 |
20160199324 | MULTIPLE MYELOMA TREATMENT | 07-14-2016 |