公开(公告)号：US08487100B2

公开(公告)日：2013-07-16

申请号：US12967871

申请日：2010-12-14

申请人： Eric R Prossnitz ,  Sergey E Tkatchenko ,  Chetana M Revankar ,  Larry A Sklar ,  Jeffrey B Arterburn ,  Daniel F Cimino ,  Tudor I Oprea ,  Cristian-George Bologa ,  Bruce S Edwards ,  Alexandor Kiselyov ,  Susan M Young

发明人： Eric R Prossnitz ,  Sergey E Tkatchenko ,  Chetana M Revankar ,  Larry A Sklar ,  Jeffrey B Arterburn ,  Daniel F Cimino ,  Tudor I Oprea ,  Cristian-George Bologa ,  Bruce S Edwards ,  Alexandor Kiselyov ,  Susan M Young

IPC分类号： A61K31/4375 ,  C07D221/06

CPC分类号： C07D221/16 ,  C07D405/04 ,  C07D405/14

摘要： The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ERα and ERβ). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors. Diseases which are mediated through one or more of these receptors include cancer (particularly breast, reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometreitis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disoders such as Parkinson's disease and Alzheimer's disease, as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.

摘要翻译： 本发明在分子生物学/药理学领域，并提供调节GPR30以及经典雌激素受体α和β（ERα和ERβ）的作用的化合物。 这些化合物可以用作一种或多种所公开的雌激素受体的激动剂和/或拮抗剂。 通过这些受体中的一种或多种介导的疾病包括癌症（特别是乳腺，生殖和其他激素依赖性癌症，白血病，结肠癌，前列腺癌），生殖（泌尿 - 泌尿）包括子宫内膜炎，前列腺炎，多囊卵巢综合征，膀胱 控制，激素相关疾病，听觉障碍，心血管疾病，包括潮热和大量出汗，高血压，中风，肥胖，骨质疏松症，血液病，血管疾病或诸如静脉血栓形成，动脉粥样硬化等疾病，以及许多其他疾病和中枢和 周围神经系统，包括抑郁症，失眠，焦虑，多发性硬化，神经病变，神经变性解码器如帕金森病和阿尔茨海默病，以及炎性肠病，克罗恩病，腹腔（腹腔）疾病和肠道相关疾病。 用于预防或减少性交后怀孕的可能性的避孕指示是本发明的另一方面。