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21 条记录 (耗时 0.028 秒)

    FLUORINATED 4-AZASTEROIDS AS ANDROGEN RECEPTOR MODULATORS
    1.
    发明公开
    FLUORINATED 4-AZASTEROIDS AS ANDROGEN RECEPTOR MODULATORS 审中-公开
    氟化4- azasteroids ALS雄激素受体调节剂

    公开(公告)号：EP1742631A1

    公开(公告)日：2007-01-17

    申请号：EP05738680.7

    申请日：2005-04-22

    申请人： Merck & Co., Inc.

    发明人： MEISSNER, Robert, S. ,  PERKINS, James, J.

    IPC分类号： A61K31/473 ,  A61K31/437 ,  C07D401/12 ,  C07D401/14

    CPC分类号： C07J73/005

    摘要： Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer’s disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

    17-HYDROXY-4-AZA-ANDROSTAN-3-ONES AS ANDROGEN RECEPTOR MODULATORS
    3.
    发明公开
    17-HYDROXY-4-AZA-ANDROSTAN-3-ONES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
    17-羟基-4-亚氨基 - 安息替康-3-ONE ALS和去甲肾上腺素调节剂

    公开(公告)号：EP1467739A2

    公开(公告)日：2004-10-20

    申请号：EP03715925.8

    申请日：2003-01-10

    申请人： Merck & Co., Inc.

    发明人： DANKULICH, William, P. ,  MEISSNER, Robert, S. ,  MITCHELL, Helen, J. ,  PERKINS, James, J.

    IPC分类号： A61K31/56

    CPC分类号： C07J73/005 ,  A61K31/473 ,  A61K31/58 ,  A61K45/06 ,  A61K2300/00

    摘要： Compounds of structural formula I as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue. These compounds are useful in the treatment of 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, obesity, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.

    N-(PYRIDIN-3-YL)-2-PHENYLBUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS
    5.
    发明公开
    N-(PYRIDIN-3-YL)-2-PHENYLBUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
    N-（吡啶-3-基）-2-苯基丁酰胺和恶二唑酮

    公开(公告)号：EP1807076A1

    公开(公告)日：2007-07-18

    申请号：EP05851360.7

    申请日：2005-10-25

    申请人： Merck & Co., Inc.

    发明人： KIM, Yuntae ,  CLOSE, Joshua ,  DUGGAN, Mark, E. ,  HANNEY, Barbara ,  MEISSNER, Robert, S. ,  MUSSELMAN, Jeffrey ,  PERKINS, James, J. ,  WANG, Jiabing

    IPC分类号： A61K31/44 ,  C07D213/02

    CPC分类号： C07D213/64 ,  A61K31/44 ,  C07D213/74

    摘要： Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer’s disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

    ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
    8.
    发明公开
    ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 有权
    雄激素受体调节和使用方法

    公开(公告)号：EP1622567A2

    公开(公告)日：2006-02-08

    申请号：EP04751257.9

    申请日：2004-05-03

    申请人： Merck & Co., Inc.

    发明人： MEISSNER, Robert, S. ,  PERKINS, James, J.

    IPC分类号： A61K6/00

    CPC分类号： A61K31/58 ,  C07J73/005

    摘要： Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of 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, post-menopausal symptoms in women, female sexual dysfunction, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal 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.

    INTEGRIN RECEPTOR ANTAGONISTS
    9.
    发明公开
    INTEGRIN RECEPTOR ANTAGONISTS 有权
    整合素受体拮抗剂

    公开(公告)号：EP1044001A1

    公开(公告)日：2000-10-18

    申请号：EP98963893.7

    申请日：1998-12-14

    申请人： MERCK & CO., INC.

    发明人： DUGGAN, Mark, E. ,  PERKINS, James, J. ,  MEISSNER, Robert, S.

    IPC分类号： A61K31/495 ,  A61K31/445 ,  C07D417/14 ,  C07D401/14

    CPC分类号： C07D471/04 ,  A61K41/00 ,  A61K45/06

    摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αξβ3, αξβ5, and/or αξβ6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.

    摘要翻译： 本发明涉及化合物及其衍生物，它们的合成及其作为整联蛋白受体拮抗剂的用途。 更具体地说，本发明化合物是整联蛋白受体αξβ3，αξβ5和/或αξβ6的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松症，抑制血管再狭窄，糖尿病性视网膜病，黄斑变性，血管生成，动脉粥样硬化 ，炎症，伤口愈合，病毒性疾病，肿瘤生长和转移。