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    ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
    2.
    发明公开
    ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 有权
    雄激素受体调节剂和其使用方法

    公开(公告)号：EP1439841A2

    公开(公告)日：2004-07-28

    申请号：EP02778604.5

    申请日：2002-10-15

    申请人： Merck & Co., Inc.

    发明人： COLEMAN, Paul, J. ,  NEILSON, Lou Anne

    IPC分类号： A61K31/55 ,  A61P19/00 ,  C07D223/14 ,  C07D487/00

    CPC分类号： C07D491/04 ,  C07D471/04 ,  C07D491/10

    摘要： Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for antagonizing AR in the prostate of a male patient or in the uterus of a female patient and agonizing AR in bone and/or muscle tissue. These compounds are useful in the treating conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.

    MITOTIC KINESIN INHIBITORS
    5.
    发明公开
    MITOTIC KINESIN INHIBITORS 审中-公开
    MITOTIC KINESIN抑制剂

    公开(公告)号：EP1851213A2

    公开(公告)日：2007-11-07

    申请号：EP06734469.7

    申请日：2006-02-06

    申请人： Merck & Co., Inc.

    发明人： BRESLIN, Michael, J. ,  WHITMAN, David, B. ,  NEILSON, Lou Anne ,  COX, Christopher, D. ,  COLEMAN, Paul, J.

    IPC分类号： C07D405/12 ,  C07D207/50 ,  A61K31/40 ,  A61K31/4025

    CPC分类号： C07D491/052

    摘要： The present invention relates to tricyclic pyrazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

    摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，治疗与KSP驱动蛋白活性有关的病症和用于抑制KSP驱动蛋白的三环吡唑类。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

    ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
    6.
    发明授权
    ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 有权
    雄激素受体调节剂和其使用方法

    公开(公告)号：EP1439841B1

    公开(公告)日：2007-09-19

    申请号：EP02778604.5

    申请日：2002-10-15

    申请人： Merck & Co., Inc.

    发明人： COLEMAN, Paul, J. ,  NEILSON, Lou Anne

    IPC分类号： C07D471/04 ,  C07D491/04 ,  C07D491/10 ,  A61K31/55 ,  A61P19/00

    CPC分类号： C07D491/04 ,  C07D471/04 ,  C07D491/10

    摘要： Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for antagonizing AR in the prostate of a male patient or in the uterus of a female patient and agonizing AR in bone and/or muscle tissue. These compounds are useful in the treating conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.