862129-71-3

Usage

Uses

Used in Pharmaceutical Industry:
(+/-)-2-(4-methanesulfonyl-cyclohex-1-enyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane is used as a reactant for the preparation of piperidine derivatives. These derivatives act as selective estrogen receptor modulators (SERMs) and have potential applications in the treatment of uterine fibroids. (+/-)-2-(4-methanesulfonyl-cyclohex-1-enyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane's reactivity and stability make it a valuable component in the synthesis of these therapeutic agents.

Upstream product

• 862129-73-5 (+/-)-trifluoro-methanesulfonic acid 4-methanesulfonyl-cyclohex-1-enyl ester 
• 73183-34-3 bis(pinacol)diborane 
• 862129-72-4 4-(methylsulfonyl)cyclohexan-1-one 

Downstream Products

• 862129-75-7 (+/-)-1-(2-{4-[2-(4-methanesulfonyl-cyclohex-1-enyl)-6-methoxy-naphthalen-1-yloxy]-phenoxy}-ethyl)-piperidine 
• 862130-05-0 6-(4-methanesulfonyl-cyclohexyl)-5-[4-(2-piperidin-1-yl-ethoxy)-phenoxy]-naphthalen-2-ol 
• 862129-77-9 (+/-)-6-(4-methanesulfonyl-cyclohex-1-enyl)-5-[4-(2-piperidin-1-yl-ethoxy)-phenoxy]-naphthalen-2-ol 

Relevant academic research and scientific papers

Structure-activity relationships of SERMs optimized for uterine antagonism and ovarian safety

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

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 uterine leiomyoma.