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    Ligands of estrogen receptors α and β, method of their preparation, and pharmaceuticals comprising them
    1.
    发明授权
    Ligands of estrogen receptors α and β, method of their preparation, and pharmaceuticals comprising them 有权
    配体雌激素受体α及其制备方法及其制备方法

    公开(公告)号：US08334280B2

    公开(公告)日：2012-12-18

    申请号：US12990826

    申请日：2009-05-05

    申请人： Petr Novak ,  David Sedlak ,  Petr Bartunek ,  Martin Kotora

    发明人： Petr Novak ,  David Sedlak ,  Petr Bartunek ,  Martin Kotora

    IPC分类号： A61K31/567 ,  A61K31/58 ,  C07J1/00 ,  C07J17/00 ,  C07J43/00

    CPC分类号： C07J1/0088 ,  C07J17/00 ,  C07J43/003

    摘要： The invention relates to novel ligands of the estrogen receptors α and β of general formula II, which are useful as an active substance of pharmaceuticals, for example pharmaceutical compositions useful for hormone replacement therapy, as well as for the treatment of tumors and inflammatory diseases. The invention also relates to a novel preparation method of these ligands comprising cyclotrimerization of ethynylestradiol with the appropriate diyne in an organic solvent. Further, the invention relates to pharmaceuticals comprising the novel compounds according to the invention.

    摘要翻译： 本发明涉及雌激素受体α和bgr的新配体; 通式II，其可用作药物的活性物质，例如可用于激素替代疗法的药物组合物，以及用于治疗肿瘤和炎性疾病。 本发明还涉及这些配体的新型制备方法，其包括在有机溶剂中使炔基雌二醇与合适的二炔环化三聚。 此外，本发明涉及包含根据本发明的新化合物的药物。