648906-10-9Relevant articles and documents
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity
Qin, Zhihui,Kastrati, Irida,Chandrasena, R. Esala P.,Liu, Hong,Yao, Ping,Petukhov, Pavel A.,Bolton, Judy L.,Thatcher, Gregory R. J.
, p. 2682 - 2692 (2008/02/07)
The regulation of estrogenic and antiestrogenic effects of selective estrogen receptor modulators (SERMs) is thought to underlie their clinical use. Most SERMs are polyaromatic phenols susceptible to oxidative metabolism to quinoids, which are proposed to
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 CONTAINING A PHENYLSULFONYL GROUP
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Page/Page column 81, (2008/06/13)
The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.