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    • 5. 发明申请
    • New glucocorticoid receptor antagonists for prophylaxis and therapy of glucocorticoid-mediated hypogonadism, of sexual dysfunction and/or infertility
    • 新型糖皮质激素受体拮抗剂用于预防和治疗糖皮质激素介导的性腺机能减退症,性功能障碍和/或不育症
    • US20040180869A1
    • 2004-09-16
    • US10735487
    • 2003-12-12
    • Ulrich BotheGerd SchubertGuenter KaufmannLothar SobekVladimir PatchevAlexander Hillisch
    • A61K031/573
    • A61K31/00A61K31/567A61K31/573C07J1/00
    • The present invention relates to novel glucocorticoid receptor antagonists for producing a drug for the prophylaxis and therapy of glucocorticoid-mediated hypogonadism, sexual dysfunctions and/or infertility. For purposes of the present invention, by nullglucocorticoid receptor antagonistsnull are meant drugs capable of competitively inhibiting the effect of glucocorticoids as a result of better and more selective binding to glucocorticoid receptors The compounds according to the invention or used according to the invention are characterized in that they are significantly more dissociated, namely they bind well to the glucocorticoid receptor and act on the progesterone receptor only to aminor degree compared to 11null-(4-dimethylamino)phenyl-17null-hydroxy-17null-propyn-1-yl-estra-4,9-dien-3-one (RU 38486), a substance of very high activity but low selectivity.
    • 本发明涉及用于生产用于预防和治疗糖皮质激素介导的性腺机能减退症,性功能障碍和/或不育症的药物的新型糖皮质激素受体拮抗剂。 为了本发明的目的,“糖皮质激素受体拮抗剂”是指由于更好和更选择性地结合糖皮质激素受体而能够竞争性地抑制糖皮质激素作用的药物。本发明化合物或根据本发明使用的化合物的特征在于 因为它们明显更多地解离,即它们与糖皮质激素受体很好地结合,并且与11beta-(4-二甲基氨基)苯基-17β-羟基-17α-丙炔-1-基 - 雌二醇相比,仅在孕酮受体上作用于氨基酸 -4,9-二烯-3-酮(RU 38486),其活性非常高但选择性低。