公开(公告)号：EP1641535A2

公开(公告)日：2006-04-05

申请号：EP04777135.7

申请日：2004-06-25

申请人： Merck & Co., Inc.

发明人： DANKULICH, William, P. ,  KAUFMAN, Mildred, L. ,  MEISSNER, Robert, S. ,  MITCHELL, Helen, J.

IPC分类号： A61P19/00 ,  A61K31/56 ,  A61K31/58 ,  C07D221/18 ,  C07D221/22 ,  C07D239/02 ,  C07D241/00 ,  C07D241/36 ,  C07D401/00 ,  C07D413/00

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. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore 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, cancer cachexia, Alzheimer’s disease, muscular dystrophies, cognitive impairment, decreased libido, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

公开(公告)号：EP1660184A2

公开(公告)日：2006-05-31

申请号：EP04777129.0

申请日：2004-06-25

申请人： Merck & Co., Inc.

发明人： DANKULICH, William, P. ,  KAUFMAN, Mildred, L. ,  MEISSNER, Robert, S. ,  MITCHELL, Helen, J.

IPC分类号： A61P19/00 ,  A61K31/56 ,  A61K31/58 ,  C07D221/18 ,  C07D221/22 ,  C07D239/02 ,  C07D241/00

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.

公开(公告)号：EP1663228A1

公开(公告)日：2006-06-07

申请号：EP04783033.6

申请日：2004-09-02

申请人： Merck & Co., Inc.

发明人： KAUFMAN, Mildred, L. ,  MEISSNER, Robert, S. ,  MITCHELL, Helen, J.

IPC分类号： A61K31/473 ,  C07D221/18 ,  C07D417/04 ,  C07D401/04 ,  C07D413/04

CPC分类号： C07J73/005 ,  C07D401/04 ,  C07D417/04 ,  C07D417/14

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.