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185 条记录 (耗时 0.037 秒)

    17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS
    161.
    发明公开
    17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
    17-乙酰氨基-4- AZASTEROIDDERIVATE ALS雄激素受体调节

    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.

    MONOCYCLIC DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS
    165.
    发明公开
    MONOCYCLIC DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
    单衍生物作为抑制剂基质金属蛋白酶

    公开(公告)号：EP1537098A1

    公开(公告)日：2005-06-08

    申请号：EP03784414.9

    申请日：2003-08-03

    申请人： Warner-Lambert Company LLC

    发明人： PICARD, Joseph A.Pfizer Global Research & Develop

    IPC分类号： C07D401/04 ,  C07D241/18 ,  C07D403/14 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  A61K31/495 ,  A61P9/00 ,  A61P19/00 ,  A61P29/00 ,  C07D257/00 ,  C07D241/00 ,  C07D263/00 ,  C07D233/00

    CPC分类号： C07D241/24 ,  C07D231/12 ,  C07D233/56 ,  C07D237/14 ,  C07D237/24 ,  C07D241/18 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14

    摘要： This invention provides compounds defined by Formula (I) or a pharmaceutically acceptable salt thereof, wherein R', Q, D, V', m, and R2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula (I), or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula (I), or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.