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    Synthesis and biological activities of new tricyclic-bis-enones (TBEs)
    6.
    发明授权
    Synthesis and biological activities of new tricyclic-bis-enones (TBEs) 有权
    新型三环双酮（TBE）的合成和生物活性

    公开(公告)号：US08067394B2

    公开(公告)日：2011-11-29

    申请号：US12777120

    申请日：2010-05-10

    申请人： Tadashi Honda ,  Chitra Sundararajan ,  Gordon W. Gribble ,  Michael B. Sporn ,  Karen T. Liby

    发明人： Tadashi Honda ,  Chitra Sundararajan ,  Gordon W. Gribble ,  Michael B. Sporn ,  Karen T. Liby

    IPC分类号： A61K31/695 ,  A61K31/277 ,  A61K31/4164 ,  A61K31/40 ,  A61P35/00 ,  A61P35/02

    CPC分类号： C07F7/0812 ,  C07C49/743 ,  C07C255/47 ,  C07C2603/26 ,  C07D207/337 ,  C07D209/08 ,  C07D233/64 ,  C07D295/145 ,  C07F7/081

    摘要： This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-γ, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.

    摘要翻译： 本发明描述了新型三环双烯衍生物（TBE），如TBE-31，TBE-34，TBE-45和水溶性TBE。 还公开了制备这些化合物的方法。 本发明人证明了这些新型TBE抑制人骨髓瘤细胞增殖的能力，抑制了用干扰素-γ刺激的细胞中诱导iNOS，诱导血红素加氧酶-1（HO-1），诱导CD11b表达 - 白血病分化标记， 抑制白血病细胞增殖，诱导人肺癌细胞凋亡，诱导其他癌细胞凋亡。 预期本发明的TBE可用于治疗和预防许多疾病，包括癌症，神经障碍，炎症和涉及氧化应激的病理学的有用试剂。

    SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW TRICYCLIC-BIS-ENONES (TBES)
    8.
    发明申请
    SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW TRICYCLIC-BIS-ENONES (TBES) 有权
    新TRICYCLIC-BIS-ENONES（TBES）的合成和生物活性

    公开(公告)号：US20110009363A1

    公开(公告)日：2011-01-13

    申请号：US12777120

    申请日：2010-05-10

    申请人： Tadashi Honda ,  Chitra Sundararajan ,  Gordon W. Gribble ,  Michael B. Sporn ,  Karen T. Liby

    发明人： Tadashi Honda ,  Chitra Sundararajan ,  Gordon W. Gribble ,  Michael B. Sporn ,  Karen T. Liby

    IPC分类号： A61K31/695 ,  A61K31/277 ,  A61K31/4164 ,  A61K31/40 ,  A61P35/00 ,  A61P35/02

    CPC分类号： C07F7/0812 ,  C07C49/743 ,  C07C255/47 ,  C07C2603/26 ,  C07D207/337 ,  C07D209/08 ,  C07D233/64 ,  C07D295/145 ,  C07F7/081

    摘要： This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-γ, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.

    摘要翻译： 本发明描述了新型三环双烯衍生物（TBE），如TBE-31，TBE-34，TBE-45和水溶性TBE。 还公开了制备这些化合物的方法。 发明人证明了这些新型TBE抑制人骨髓瘤细胞增殖的能力，抑制了用干扰素-γ刺激的细胞中诱导iNOS，诱导血红素加氧酶-1（HO-1），诱导CD11b表达 - 白血病分化标记， 抑制白血病细胞增殖，诱导人肺癌细胞凋亡，诱导其他癌细胞凋亡。 预期本发明的TBE可用于治疗和预防许多疾病，包括癌症，神经障碍，炎症和涉及氧化应激的病理学的有用试剂。