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    TREATMENT OF LEUKEMIA WITH HISTONE DEACETYLASE INHIBITORS
    4.
    发明公开
    TREATMENT OF LEUKEMIA WITH HISTONE DEACETYLASE INHIBITORS 审中-公开
    用组蛋白去乙酰化酶抑制剂治疗白血病

    公开(公告)号：EP3166603A1

    公开(公告)日：2017-05-17

    申请号：EP15818585.0

    申请日：2015-07-06

    申请人： Acetylon Pharmaceuticals, Inc. ,  Tamang, David Lee

    发明人： JONES, Simon S. ,  MIN, Chengyin ,  YANG, Min

    IPC分类号： A61K31/4184 ,  A61K31/706 ,  A61P35/02

    CPC分类号： A61K31/706 ,  A61K31/167 ,  A61K31/4045 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

    摘要： 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.

    摘要翻译： 本文提供了包含HDAC抑制剂和阿扎胞苷的组合，用于治疗有此需要的受试者中的白血病。 本文提供了包含HDAC抑制剂和阿扎胞苷的组合，用于治疗有此需要的受试者中的急性骨髓性白血病。 本文还提供了用于治疗有需要的受试者中的白血病的方法，其包括向受试者施用有效量的上述组合或HDAC抑制剂，以及用于在有需要的受试者中治疗急性骨髓性白血病的方法，所述方法包括施用 给受试者施用有效量的上述组合或HDAC抑制剂。

    TREATMENT OF DISEASES CAUSED BY ABNORMAL LYMPHOCYTE FUNCTION WITH AN HDAC6 INHIBITOR
    5.
    发明公开
    TREATMENT OF DISEASES CAUSED BY ABNORMAL LYMPHOCYTE FUNCTION WITH AN HDAC6 INHIBITOR 审中-公开
    BEHANDLUNG VON DURCH异常LYMPHOZENTENFUNKTION VERURSACHTEN KRANKHEITEN MIT EINEM HDAC6-INHIBITOR

    公开(公告)号：EP3046559A4

    公开(公告)日：2017-03-22

    申请号：EP14845666

    申请日：2014-09-19

    申请人： ACETYLON PHARMACEUTICALS INC ,  EDWARD VIA VIRGINIA COLLEGE OF OSTEOPATHIC MEDICINE ,  VIRGINIA TECH INTELLECTUAL PROPERTIES INC

    发明人： REILLY CHRISTOPHER M ,  GAFOOR ABDUL ,  CAUDELL DAVID L ,  REGNA NICOLE L ,  JARPE MATTHEW

    IPC分类号： A61K31/495 ,  A61P7/00 ,  A61P37/00

    CPC分类号： A61K31/505

    摘要： An HDAC6 inhibitor (a compound of Formula I) is shown to reduce the pathogenesis associated with the B cell mediated autoimmune disease, systemic lupus erythematosus (SLE) Administration of a compound of Formula I attenuated many of the symptoms characteristic of SLE including splenomegaly, abnormal B cell differentiation, an increase in the number double-negative thymic T cells, an increase in the level of auto-antibodies such as anti-dsDNA, immune complex-mediated glomerulonephritis and an increase in inflammatory cytokine production. Treatment with a compound of Formula I also increased the number of the subject's splenic Treg cells while removing circulating auto-antibodies Inhibition of HDAC6 altered bone marrow B cell differentiation by increasing the percentage of cells in the early-stage developmental fractions of both pro- and pre-B cells. These results demonstrate HDAC6 inhibition with a compound of Formula I can treat SLE disease by altering aberrant T and B cell differentiation.

    摘要翻译： 显示出HDAC6抑制剂（式I化合物）可减少与B细胞介导的自身免疫性疾病，系统性红斑狼疮（SLE）相关的发病机制。给予式I化合物的许多症状减轻许多症状，包括脾肿大，异常 B细胞分化，双阴性胸腺T细胞数量增加，自身抗体水平升高，如抗dsDNA，免疫复合物介导的肾小球肾炎和炎症细胞因子产生增加。 用式I化合物的治疗也增加受试者的脾Treg细胞的数量，同时去除循环自身抗体HDAC6的抑制改变骨髓B细胞分化，通过增加前期和后期发育阶段的细胞百分比 前B细胞。 这些结果表明，用式I化合物的HDAC6抑制可以通过改变异常的T和B细胞分化来治疗SLE疾病。

    PYRIMIDINE HYDROXY AMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS
    7.
    发明公开
    PYRIMIDINE HYDROXY AMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS 审中-公开
    吡啶二酮羟基苯甲酸酯

    公开(公告)号：EP3055299A1

    公开(公告)日：2016-08-17

    申请号：EP14852720.3

    申请日：2014-10-09

    申请人： Acetylon Pharmaceuticals, Inc.

    发明人： YANG, Min ,  TAMANG, David, Lee ,  JONES, Simon, Stewart ,  MAZITSCHEK, Ralph ,  VAN DUZER, John, H.

    IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D239/42 ,  A61K31/506 ,  A61P35/00

    CPC分类号： A61K31/506 ,  A61K31/505 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12

    摘要： 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 HDACl, 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 HDACl, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本文提供了化合物，包含这些化合物的药物组合物，以及使用这些化合物治疗或预防与HDAC活性相关的疾病或病症的方法，特别是涉及HDAC1，HDAC2和/或HDAC6的活性的疾病或病症。 本文还提供了抑制神经母细胞瘤细胞迁移，诱导成神经细胞瘤细胞和改变神经母细胞瘤细胞的细胞周期进程的方法，包括向细胞施用治疗有效量的HDAC1，HDAC2和/或HDAC6选择性抑制剂 或其药学上可接受的盐。