861930-46-3Relevant academic research and scientific papers
Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety
Richardson, Timothy I.,Frank, Scott A.,Wang, Minmin,Clarke, Christian A.,Jones, Scott A.,Ying, Bai-Ping,Kohlman, Dan T.,Wallace, Owen B.,Shepherd, Timothy A.,Dally, Robert D.,Palkowitz, Alan D.,Geiser, Andrew G.,Bryant, Henry U.,Henck, Judith W.,Cohen, Ilene R.,Rudmann, Daniel G.,McCann, Denis J.,Coutant, David E.,Oldham, Samuel W.,Hummel, Conrad W.,Fong, Kin C.,Hinklin, Ronald,Lewis, George,Tian, Hongqi,Dodge, Jeffrey A.
, p. 3544 - 3549 (2008/02/07)
Structure-activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting brain exposure and were guided by computational properties. Compounds with limited impact on the HPO axis were selected using serum estrogen levels as a biomarker for ovarian stimulation.
SELECTIVE ESTROGEN RECEPTOR MODULATORS FOR THE TREATMENT OF VASOMOTOR SYMPTOMS
-
Page/Page column 26, (2008/06/13)
The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats
Hummel, Conrad W.,Geiser, Andrew G.,Bryant, Henry U.,Cohen, Ilene R.,Dally, Robert D.,Fong, Kin Chiu,Frank, Scott A.,Hinklin, Ronald,Jones, Scott A.,Lewis, George,McCann, Denis J.,Rudmann, Daniel G.,Shepherd, Timothy A.,Tian, Hongqi,Wallace, Owen B.,Wang, Minmin,Wang, Yong,Dodge, Jeffrey A.
, p. 6772 - 6775 (2007/10/03)
The design of a novel selective estrogen receptor modulator (SERM) for the potential treatment of uterine leiomyoma is described. 16 (LY2066948-HCl) binds with high affinity to estrogen receptors α and β (ERα and ERβ, respectively) and is a potent uterine
