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    • 64. 发明申请
    • ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF
    • 雌激素受体配体及其使用方法
    • WO2013043304A1
    • 2013-03-28
    • PCT/US2012/052141
    • 2012-08-23
    • GTX, INC.DALTON, JamesSTEINER, Mitchell, S.COSS, Christopher, C.
    • DALTON, JamesSTEINER, Mitchell, S.COSS, Christopher, C.
    • A01N37/18A61K31/165
    • A61K31/137A61K31/167
    • The present invention relates to methods for reducing testosterone levels by reduction of luteinizing hormone (LH) or independent of LH levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate (5) cancer, castration resistant prostate cancer (CRPC), metastatic castration resistant prostate cancer (mCRPC) and palliative treatment of prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC) and metastatic castration resistant prostate cancer (mCRPC), and methods of reducing high or increasing PSA levels and/or increasing SHBG levels in a subject suffering from prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC) and metastatic (10) castration resistant prostate cancer (mCRPC). The compounds of this invention suppress free or total testosterone levels despite castrate levels secondary to ADT and reduce high or increasing PSA levels.
    • 本发明涉及通过降低男性受试者的黄体生成素(LH)或LH水平而降低睾酮水平的方法以及治疗,抑制,降低发病率,降低严重程度或抑制前列腺癌,晚期前列腺( 5)癌症,阉割抗性前列腺癌(CRPC),转移性阉割抗性前列腺癌(mCRPC)和姑息治疗前列腺癌,晚期前列腺癌,去势抗性前列腺癌(CRPC)和转移性阉割抗性前列腺癌(mCRPC) 在前列腺癌,晚期前列腺癌,阉割抗性前列腺癌(CRPC)和转移性(10)抗阉割前列腺癌(mCRPC)的受试者中降低PSA水平升高和/或增加SHBG水平。 本发明的化合物尽管阉割水平继发于ADT并降低高水平或增加PSA水平,但抑制游离或总睾丸激素水平。