- METHODS OF USE AND PHARMACEUTICAL COMBINATIONS COMPRISING HISTONE DEACETYLASE INHIBITORS AND JAK 1 2 INHIBITORS
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The disclosure relates to pharmaceutical combinations comprising an HDAC6 selective inhibitor and a JAK1/2 inhibitor for the treatment of a cancer, such as a hematological cancer, in a subject in need thereof. Also provided herein are methods for treating a cancer in a subject in need thereof, comprising administering to the subject an effective amount of an HDAC6 selective inhibitor and a JAK1/2 inhibitor.
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Page/Page column 27-29
(2019/06/17)
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- PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND EPOTHILONE AND METHODS OF USE THEREOF
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The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) an epothilone, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.
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Page/Page column 28; 29
(2018/05/24)
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- PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND A PROGRAMMED DEATH-LIGAND 1 (PD-L1) INHIBITOR AND METHODS OF USE THEREOF
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The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) a programmed death ligand 1 (PD-L1) inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.
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Page/Page column 31
(2018/06/12)
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- PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND A BCL-2 INHIBITOR AND METHODS OF USE THEREOF
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The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) a BCL-2 inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.
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Page/Page column 30
(2018/05/24)
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- PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND AN AURORA KINASE INHIBITOR AND METHODS OF USE THEREOF
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The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) an aurora kinase inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.
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Page/Page column 33
(2018/05/24)
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- PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND A CD38 INHIBITOR AND METHODS OF USE THEREOF
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The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase inhibitor and (b) a CD38 inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.
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Page/Page column 28; 29
(2018/06/12)
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- USE OF HDAC6 INHIBITORS FOR PREVENTING AND TREATING RENAL CYSTOGENESIS, RENAL CELL CARCINOMA, AND RENAL CILIOPATHIES
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The present disclosure is directed to the use of HDAC6 inhibitors for the treatment of renal diseases and disorders, including ciliopathy, Von Hippel-Lindau (VHL) disease, renal cystogenesis, renal cell carcinoma, and Tuberous Sclerosis Complex (TSC), and the like. In some embodiments, the HDAC6 inhibitor is a direct inhibitor of HDAC6. In a further embodiment, the HDAC6 signaling inhibitor is ACY-1215 or a pharmaceutically acceptable salt thereof. In some embodiments, the HDAC6 inhibitor is combined with an AURKA inhibitor.
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Page/Page column 31; 30
(2018/09/26)
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- Biomarkers to identify patients that will respond to treatment and treating such patients
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The invention relates to methods for using biomarkers to identify cancer patients that will or are likely to respond to treatment. Specifically, the invention relates to the use of one or more of three association studies of cancer types, gene mutations, or gene expression levels in order to identify cancer patients that will or are likely to respond to treatment with a histone deacetylase (HDAC) inhibitor, alone or in combination with another cancer treatment. The methods may, optionally, further include treating such patient with an HDAC inhibitor, alone or in combination with another cancer treatment.
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- HDAC INHIBITORS FOR THE TREATMENT OF DIABETIC PERIPHERAL NEUROPATHY
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The invention relates to HDAC inhibitors for use in the treatment of diabetic peripheral neuropathy in a subject in need thereof. Also provided herein are methods for treating diabetic peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor.
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Paragraph 0125; 0130
(2017/06/23)
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- HDAC INHIBITORS, ALONE OR IN COMBINATION WITH BTK INHIBITORS, FOR TREATING CHRONIC LYMPHOCYTIC LEUKEMIA
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Disclosed are histone deacetylase (HDAC) inhibitors, or combinations comprising an HDAC inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of chronic lymphocytic leukemia in a subject in need thereof. Also provided herein are methods for treating chronic lymphocytic leukemia in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a BTK inhibitor. Other related methods are disclosed.
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Page/Page column 44; 45
(2017/11/15)
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- METHODS OF USE AND PHARMACEUTICAL COMBINATIONS OF HDAC INHIBITORS WITH BET INHIBITORS
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The disclosure relates to pharmaceutical combinations comprising an HDAC6 selective inhibitor and a BET inhibitor for the treatment of cancer in a subject in need thereof. Also provided herein are methods for treating cancer in a subject in need thereof, comprising administering to the subject an effective amount of an HDAC6 selective inhibitor and a BET inhibitor.
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Page/Page column 34; 35
(2018/01/17)
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- INCREASING EXPRESSION OF INTERFERON REGULATED GENES WITH COMBINATONS OF HISTONE DEACETYLASE INHIBITORS AND IMMUNOMODULATORY DRUGS
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Provided herein is a combination comprising an HDAC inhibitor and an IMiD for increasing interferon regulated gene expression or decreasing c-MYC gene expression in a cancer cell or tumor in a subject in need thereof. Increasing interferon regulated gene expression may result in increased recognition of tumors by innate or adaptive immune system and an increase in programmed cell death (apoptosis) gene expression, increasing apoptosis in cancer cells and tumors. The cells can be multiple myeloma cells or diffuse large B-cell lymphoma cells. Also provided are methods for treating myelodysplastic syndromes/acute myeloid leukemia (MDS/AML) or pathogen infections in a subject in need thereof comprising administering to the subject an effective amount of HDAC inhibitor and an IMiD. The HDAC inhibitor can be an HDAC6-selective inhibitor.
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Page/Page column 48; 50
(2017/09/08)
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- TREATMENT OF LEUKEMIA WITH HISTONE DEACETYLASE INHIBITORS
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Provided herein are combinations comprising an HDAC inhibitor and azacitidine for the treatment of leukemia in a subject in need thereof. Provided herein are combinations comprising an HDAC inhibitor and azacitidine for the treatment of acute myelogenous leukemia in a subject in need thereof. Also provided herein are methods for treating leukemia in a subject in need thereof, comprising administering to the subject an effective amount of the above combination or an HDAC inhibitor, as well as methods for treating acute myelogenous leukemia in a subject in need thereof, comprising administering to the subject an effective amount of the above combination or an HDAC inhibitor.
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Page/Page column 39
(2016/01/25)
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- COMBINATIONS OF HISTONE DEACETYLASE INHIBITORS AND BENDAMUSTINE FOR USE IN THE TREATMENT OF LYMPHOMA
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The invention relates to pharmaceutical combinations comprising an HDAC inhibitor and bendamustine; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions for treating lymphoma in a subject in need thereof.
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Page/Page column 28
(2016/06/28)
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- METHODS OF MAKING PROTEIN DEACETYLASE INHIBITORS
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The present invention relates to methods and intermediates useful for the synthesis of protein deacetylase inhibitors.
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Paragraph 0138; 0143
(2016/12/22)
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- CRYSTALLINE FORMS OF A HISTONE DEACETYLASE INHIBITOR
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This disclosure provides solid forms of 2-((2-chlorophenyl)(phenyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide, and methods of manufacturing and using these forms.
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Page/Page column 20; 21
(2016/12/26)
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- HISTONE DEACETYLASE 6 (HDAC6) BIOMARKERS IN MULTIPLE MYELOMA
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The invention relates to histone deacetylase (HDAC) biomarkers in multiple myeloma. Specifically, the biomarkers are drug specific, histone deacetylase (HDAC) or HDAC6 biomarker RNAs for multiple myeloma. The invention also relates to a kit for determining the treatment efficiency of a HDAC6 inhibitor, and a kit for identifying a histone deacetylase 6 (HDAC6) inhibitor. The invention further relates to a method for monitoring treatment efficiency of an HDAC inhibitor in a subject.
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Page/Page column
(2015/07/02)
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- COMBINATIONS OF HISTONE DEACETYLASE INHIBITORS AND EITHER HER2 INHIBITORS OR PI3K INHIBITORS
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The invention relates to combinations comprising an HDAC inhibitor and a Her2 inhibitor for the treatrent of breast cancer in a subject in need thereof. The invention also relates to combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of breast cancer in a subject in need thereof. Also provided herein are methods for treating breast cancer in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations. Further provided are methods for inhibiting migration and/or invasion of a breast cancer cell in a subject by administering to the subject a HDAC6 specific inhibitor.
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Paragraph 0237
(2015/04/15)
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- PYRIMIDINE HYDROXY AMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS
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Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.
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Paragraph 0406
(2015/04/21)
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- COMBINATIONS OF HISTONE DEACETYLASE INHIBITORS AND IMMUNOMODULATORY DRUGS
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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.
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Paragraph 0396-0397
(2015/04/21)
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- HDAC INHIBITORS, ALONE OR IN COMBINATION WITH BTK INHIBITORS, FOR TREATING NONHODGKIN'S LYMPHOMA
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The invention relates to HDAC inhibitors, or combinations comprising an HDAC inhibitor and a BTK inhibitor for the treatment of non-hodgkin's lymphoma in a subject in need thereof. Also provided herein are methods for treating non-hodgkin's lymphoma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a BTK inhibitor.
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Paragraph 0203
(2015/04/21)
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- HDAC Inhibitors, Alone Or In Combination With PI3K Inhibitors, For Treating Non-Hodgkin's Lymphoma
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The invention relates to HDAC inhibitors, or combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of non-hodgkin's lymphoma in a subject in need thereof. Also provided herein are methods for treating non-hodgkin's lymphoma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a PI3K inhibitor.
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Paragraph 0217
(2015/04/21)
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- COMBINATIONS OF HISTONE DEACETYLASE INHIBITORS AND IMMUNOMODULATORY DRUGS
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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.
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Paragraph 0254-0255
(2015/06/10)
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- TREATMENT OF POLYCYSTIC DISEASES WITH AN HDAC6 INHIBITOR
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An HDAC6-specific inhibitor (i.e., a compound of Formula I or II) is shown to reduce the pathogenesis associated with polycystic disease. Administration of an HDAC6-specific inhibitor attenuated many of the symptoms characteristic of polycystic liver disease including cyst formation, cyst growth and cholangiocyte proliferation. Treatment with a HDAC6-specific inhibitor also increased the amount of bile duct acetylated tubulin and β-catenin phosphorylation and/or acetylation while reducing bile duct β-catenin synthesis. These results demonstrate that HDAC6 is overexpressed in cystic cholangiocytes and that its pharmacological inhibition reduces cholangiocyte proliferation and cyst growth.
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Paragraph 0158-0159
(2015/05/05)
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- HISTONE DEACETYLASE 6 SELECTIVE INHIBITORS FOR THE TREATMENT OF BONE DISEASE
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This invention relates to methods for treating bone disease associated with osteoclast activation using HDAC6 selective inhibitors, e.g., small molecule inhibitors such as reverse amide compounds.
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- REVERSE AMIDE COMPOUNDS AS PROTEIN DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF
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The present invention relates to novel "reverse amide" compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
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