发明名称 Compounds for binding to ERα/βand GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof
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 ER&bgr;). 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 endometritis, 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 disorders 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.
申请公布号 US7875721(B2) 申请公布日期 2011.01.25
申请号 US20060497751 申请日期 2006.08.02
申请人 STC.UNM 发明人 PROSSNITZ ERIC R.;TKATCHENKO SERGEY E.;REVANKAR CHETANA M.;SKLAR LARRY A.;ARTERBURN JEFFREY B.;CIMINO DANIEL F.;OPREA TUDOR I.;BOLOGA CRISTIAN-GEORGE;EDWARDS BRUCE S.;KISELYOV ALEXANDER;YOUNG SUSAN M.
分类号 A61K31/435;C07D221/06 主分类号 A61K31/435
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