公开(公告)号：EP0914450A1

公开(公告)日：1999-05-12

申请号：EP97926689.0

申请日：1997-05-20

申请人： SIGNAL PHARMACEUTICALS, INC. ,  UNIVERSITY OF TEXAS SOUTHWESTERN MEDICAL CENTER AT DALLAS

发明人： STEIN, Bernd ,  YANG, Maria, X., H. ,  YOUNG, David B. ,  BARBOSA, Miguel, S. ,  BELARDETTI, Francesco ,  WILK-BLASZCZAK, M., A. ,  COBB, Melanie

IPC分类号： G01N33 ,  C07K16 ,  C12N1 ,  C12N5 ,  C12N9 ,  C12N15 ,  C12P21 ,  A61K38

CPC分类号： C12N9/1205 ,  A61K38/00

摘要： Compositions and methods are provided for the treatment of conditions associated with mitogen-activated protein kinase cascades. In particular, the mitogen-activated protein kinase p38-2, and polypeptide variants thereof that stimulate phosphorylation and activation of substrates such as ATF2, are provided. The polypeptides may be used, for example, to identify antibodies and other agents that inhibit signal transduction via the p38-2 kinase cascade. The polypeptides and agents may be used in a variety of methods, such as in the reduction of pain sensations.

公开(公告)号：EP1163225A1

公开(公告)日：2001-12-19

申请号：EP00921397.6

申请日：2000-03-17

申请人： SIGNAL PHARMACEUTICALS, INC. ,  AXYS PHARMACEUTICALS, INC.

发明人： BHAGWAT, Shripad, S. ,  GAYO, Leah-Fung, M. ,  STEIN, Bernd ,  CHAO, Qi ,  GANGLOFF, Anthony ,  MCKIE, Jeffrey ,  RICE, Ken

IPC分类号： C07D217/18 ,  C07D217/04 ,  C07D217/20 ,  C07D223/16 ,  C07D209/44 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  A61K31/472 ,  A61P35/00

CPC分类号： C07D223/16 ,  C07D209/44 ,  C07D217/04 ,  C07D217/16 ,  C07D217/18 ,  C07D217/20 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04

摘要： Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-β over ER-α. Methods are disclosed for modulating ER-β in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-β. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is 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, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

摘要翻译： 公开了调节雌激素受体（ER）的化合物以及含有该化合物的药物组合物。 在一个具体实施方案中，所述化合物是针对ER-β而非ER-α的选择性调节剂。 公开了调节细胞和/或表达ER-β的组织的方法，包括优先表达ER-β的细胞和/或组织。 更一般地，还公开了用于治疗雌激素相关病症的方法，包括诸如乳腺癌，睾丸癌，骨质疏松症，子宫内膜异位，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动 ，记忆丧失，尿失禁，hairloss，白内障，天然荷尔蒙失衡，以及与环境化学品接触相关的不良生殖效应。