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    HISTONE DEACETYLASE INHIBITORS
    9.
    发明申请
    HISTONE DEACETYLASE INHIBITORS 有权
    HISTONE脱乙酰酶抑制剂

    公开(公告)号：US20150038581A1

    公开(公告)日：2015-02-05

    申请号：US14198764

    申请日：2014-03-06

    申请人： James Elliot Bradner ,  Ralph Mazitschek

    发明人： James Elliot Bradner ,  Ralph Mazitschek

    IPC分类号： C07C259/06

    CPC分类号： A61K31/231 ,  A61K9/0014 ,  A61K31/165 ,  A61K31/337 ,  C07C235/78 ,  C07C259/06 ,  C07D319/06 ,  C07D413/12

    摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.

    摘要翻译： 鉴于需要开发新的治疗剂，本发明提供了新的组蛋白脱乙酰酶抑制剂。 这些化合物包括酯键，使它们对酯酶的失活敏感。 因此，这些化合物特别可用于治疗皮肤病。 当化合物达到血流时，酯酶或具有酯酶活性的酶将化合物切割成具有大大降低的活性的生物活性片段或片段。理想地，这些降解产物表现出短的血清和/或全身半衰期并被快速消除。 这些化合物及其药物组合物例如特别可用于治疗皮肤T细胞淋巴瘤，神经纤维瘤病，牛皮癣，脱发，皮肤色素沉着和皮炎。 本发明还提供了制备本发明化合物及其中间体的方法。

    Histone deacetylase and tubulin deacetylase inhibitors
    10.
    发明授权
    Histone deacetylase and tubulin deacetylase inhibitors 有权
    组蛋白脱乙酰酶和微管蛋白脱乙酰酶抑制剂

    公开(公告)号：US08304451B2

    公开(公告)日：2012-11-06

    申请号：US12299430

    申请日：2007-05-02

    申请人： Ralph Mazitschek ,  Nicholas Paul Kwiatkowski ,  James Elliot Bradner

    发明人： Ralph Mazitschek ,  Nicholas Paul Kwiatkowski ,  James Elliot Bradner

    IPC分类号： A61K31/357 ,  C07D407/12

    CPC分类号： C07D413/12 ,  C07D319/06 ,  C07D405/12 ,  C07D417/12

    摘要： In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel inhibitors of histone deacetylases, tubulin deacetylases, and/or aggresome inhibitors, and pharmaceutically acceptable salts and derivatives thereof. The inventive compounds fall into two classes—“isotubacin” class and “isoisotubacin” class—all of which include a 1,3-dioxane core. The present invention further provides methods for treating disorders regulated by histone deacetylase activity, tubulin deacetylase activity, and/or the aggresome (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, protein degradation disorders, protein deposition disorders, 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.

    摘要翻译： 鉴于需要开发新的治疗剂及其有效的合成方法，本发明提供组蛋白脱乙酰酶，微管蛋白脱乙酰酶和/或聚集抑制剂的新型抑制剂及其药学上可接受的盐和衍生物。 本发明的化合物分为两类：异豆豆素类和异倍他宁类，其中全部包括1,3-二恶烷核。 本发明还提供了用于治疗由组蛋白脱乙酰酶活性，微管蛋白脱乙酰酶活性和/或聚集体（例如增殖性疾病，癌症，炎性疾病，原生动物感染，蛋白质降解紊乱，蛋白质沉积病症等）调节的病症的方法，其包括 向有需要的受试者施用治疗有效量的本发明化合物。 本发明还提供了制备本发明化合物的方法。