534572-68-4Relevant academic research and scientific papers
Novel 17beta-hydroxysteroid dehydrogenase type I inhibitors
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Page/Page column 31, (2010/02/13)
3,15-substituted estrone compounds which act as inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration, as well as the general use of selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.
15Alpha-substituted estradiol carboxylic acid esters as locally active estrogens
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Page/Page column 2; 6; 7; sheet 2, (2010/02/08)
The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 15α-estradiol ester compounds is presented which exhibit excellent biologica
Synthesis and evaluation of B-, C-, and D-ring-substituted estradiol carboxylic acid esters as locally active estrogens
Labaree, David C.,Zhang, Jing-Xin,Harris, Heather A.,O'Connor, Craig,Reynolds, Toni Y.,Hochberg, Richard B.
, p. 1886 - 1904 (2007/10/03)
We have synthesized derivatives of estradiol that are structurally modified to serve as "soft" estrogens and act within a geographically limited area of the body; estrogens without systemic action. We have previously shown with 16α-substituted analogues o
