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37 条记录 (耗时 0.032 秒)

    COMPOUNDS AND METHODS FOR MODULATION OF ESTROGEN RECEPTORS
    21.
    发明公开
    COMPOUNDS AND METHODS FOR MODULATION OF ESTROGEN RECEPTORS 有权
    化合物和方法具有调节雌激素受体

    公开(公告)号：EP1246814A2

    公开(公告)日：2002-10-09

    申请号：EP00990966.4

    申请日：2000-12-29

    申请人： SIGNAL PHARMACEUTICALS, INC.

    发明人： BHAGWAT, Shripad, S. ,  MCKIE, Jeffrey, A. ,  KHAMMUNGKHUNE, Sak

    IPC分类号： C07D311/16 ,  C07D405/12 ,  A61K31/32 ,  A61P35/00

    CPC分类号： C07D405/12 ,  C07D311/16

    摘要： Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having formula (I), as well as pharmaceutical compositions containing the same wherein R1, R2, R3, n and p are as defined here. In a specific embodiment, the compounds are selective modulators for ER-β over ER-α. Methods are also disclosed for modulating ER-β in cells and/or tissues expressing the same, including cells and/or tissues that preferentially express ER-β. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

    Indazole compounds and methods of use thereof as protein kinase inhibitors
    26.
    发明公开
    Indazole compounds and methods of use thereof as protein kinase inhibitors 审中-公开
    Indazolverbindungen und Verwendungsverfahren davon als Proteinkinasehemmer

    公开(公告)号：EP2065383A1

    公开(公告)日：2009-06-03

    申请号：EP08022584.0

    申请日：2004-11-19

    申请人： SIGNAL PHARMACEUTICALS, INC.

    发明人： Bhagwat, Shripad, S. ,  Satoh, Yoshitaka ,  Sakata, Steven, T. ,  Buhr, Chris, A. ,  Albers, Ronald ,  Sapienza, John ,  Plantevin, Veronique ,  Chao, Qi ,  Sahasrabudhe, Kiran ,  Stengone, Rachel ,  Narla, Rama, K.

    IPC分类号： C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  A61K31/416 ,  A61K31/4196

    CPC分类号： C07D403/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

    摘要： This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases. Thus, the invention encompasses orally active molecules as well as parenterally active molecules which can be used at lower doses or serum concentrations for treating diseses or disorders associated with protein kinase signal transduction.

    摘要翻译： 本发明涉及吲唑化合物或其药学上可接受的盐，溶剂化物和水合物。 吲唑化合物可用于治疗或预防对抑制，调节或调节激酶（例如炎症性疾病，异常血管生成及其相关疾病，癌症，动脉粥样硬化，心血管疾病）的各种疾病和病症 肾脏疾病，自身免疫性疾病，黄斑变性，疾病相关性消耗，石棉相关病症，肺动脉高压，糖尿病，肥胖症，疼痛等。 因此，还公开了治疗或预防这些疾病和病症的方法，以及包含一种或多种吲唑化合物的药物组合物。 本发明部分地基于发现关于蛋白激酶调节具有强力活性的新一类5-三唑基取代的吲唑分子。 因此，本发明包括口服活性分子以及肠胃外活性分子，其可以以较低剂量或血清浓度使用，用于治疗与蛋白激酶信号转导相关的疾病或障碍。

    COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER, COMPOSITIONS THEREOF AND METHODS THEREWITH
    28.
    发明公开
    COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER, COMPOSITIONS THEREOF AND METHODS THEREWITH 审中-公开
    用于癌症的治疗中有用链接，THEREOF组合物和程序

    公开(公告)号：EP1551388A2

    公开(公告)日：2005-07-13

    申请号：EP03760389.1

    申请日：2003-06-17

    申请人： Signal Pharmaceuticals, Inc.

    发明人： MCKENNA, Jeffrey ,  MERCURIO, Frank ,  PLANTEVIN, Veronique ,  XIE, Weilin

    IPC分类号： A61K31/35

    CPC分类号： A61K31/351 ,  A61K31/135 ,  A61K31/4025

    摘要： The present invention generally relates to compounds and compositions useful for the modulation of ligase activity. The invention further relates to Compounds of the Invention, compositions thereof, and methods for treating or preventing cancer, a neoplastic disorder, acute or chronic renal failure, an inflammatory disorder, an immune disorder, a cardiovascular disease, an effect of aging or an infectious disease comprising administering an effective amount of a Compound of the Invention. The invention further relates to the use of a Compound of the Invention as a preservative of a cell, blood, tissue or an organ or as an agent to modulate stem cells.