534572-92-4Relevant academic research and scientific papers
Homo- and heterogeneous Ru-based metathesis catalysts in cross-metathesis of 15-allylestrone-towards 17β-hydroxysteroid dehydrogenase type 1 inhibitors
Kirschning, Andreas,Harmrolfs, Kirsten,Mennecke, Klaas,Messinger, Josef,Sch?n, Uwe,Grela, Karol
, p. 3019 - 3022 (2008/09/20)
The cross-metathesis of allylestrone with acrylic acid derivatives using homogeneous and heterogenized Ru-catalysts was evaluated for the synthesis of a new 17β-hydroxysteroid dehydrogenase type 1 inhibitor. Hoveyda-type catalyst containing an additional diethylamino group turned out to be comparably active as homogeneous Grubbs II catalyst after immobilization on an acidic ion exchange resin which greatly facilitated workup.
THERAPEUTICALLY ACTIVE TRIAZOLES AND THEIR USE
-
Page/Page column 58, (2008/06/13)
This invention relates to novel estratrien-triazoles of general formula (I) useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17beta-hydroxysteroid dehydrogenase (17beta-HSD) such as 17beta-HSD type 1, type 2 or type 3 enzyme.
Therapeutically Active Triazoles and Their Use
-
Page/Page column 26, (2008/12/06)
Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17β-HSD) such as 17β-HSD type 1, type 2 or type 3 enzyme.
17SS-HSD1 and STS inhibitors
-
Page/Page column 94, (2010/11/25)
The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration.
15Alpha-substituted estradiol carboxylic acid esters as locally active estrogens
-
Page/Page column 2; 10; sheet 4, (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
