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Estratriene derivatives and their uses as 17beta-hydr0xyster0id dehydrogenase inhibitors

A technology of alkyl and nitrile groups, applied in the field of novel estriene-triazole derivatives, can solve the problems such as the inability to reach the level of T castration in men

Inactive Publication Date: 2012-11-28
SOLVAY PHARMA GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, Oefelein et al. reported that long-acting GnRH analogues failed to achieve castration levels of T in males in nearly 20% of cases [Oefelein MG & Cornum R(2000)] 23

Method used

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  • Estratriene derivatives and their uses as 17beta-hydr0xyster0id dehydrogenase inhibitors
  • Estratriene derivatives and their uses as 17beta-hydr0xyster0id dehydrogenase inhibitors
  • Estratriene derivatives and their uses as 17beta-hydr0xyster0id dehydrogenase inhibitors

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[0390] Experimental part

[0391] Examples of the preparation of compounds of the invention are provided in the detailed synthetic procedures below. In the compound tables that follow, the synthesis of individual compounds refers to these exemplary preparative procedures.

[0392] Compounds of formula I can be prepared using the reactions and techniques described in this section. The reactions are performed in solvents appropriate to the reagents and materials employed and suitable for the transformations resulting. Meanwhile, in the synthesis method described below, it should be understood that the selection of all proposed reaction conditions is the standard conditions of the reaction, including the choice of solvent, reaction atmosphere, reaction temperature, experiment duration and post-treatment operation, and the above conditions are easily determined by those skilled in the art. Technicians understand. Those skilled in the art of organic synthesis will appreciate tha...

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Abstract

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 17ss-hydroxysteroid dehydrogenase (17ss-HSD) such as 17ss-HSD type 1, type 2 or type 3 enzyme.

Description

[0001] This application is a divisional case of a patent application with the application number 200780030546.X, the filing date is September 17, 2007, and the invention title is "Estratriene Derivatives and Their Use as 17β-Hydroxysteroid Dehydrogenase Inhibitors" Apply. technical field [0002] The present invention relates to novel estriferases representing inhibitory compounds of 17β-hydroxysteroid dehydrogenase, preferably type 1 (17β-HSD1), type 2 (17β-HSD2) or type 3 (17β-HSD3) 17β-hydroxysteroid dehydrogenase En-triazole derivatives, salts of these compounds, pharmaceutical preparations containing these compounds, and methods for preparing these compounds. Furthermore, the invention relates to the therapeutic use of said estratriene-triazole derivatives, in particular their use in the treatment or prevention of steroid hormone-dependent diseases or disorders, for example where inhibition of 17β-hydroxysteroid dehydrogenase, in particular type I Use of 17[beta]-HSD enz...

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Application Information

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IPC IPC(8): C07J43/00A61K31/58A61P35/00A61P15/00A61P13/00A61P13/08A61P13/02A61P17/10A61P17/08A61P17/14A61P5/24A61P19/10A61P19/02A61P29/00A61P21/04A61P25/28A61P5/14A61P9/00A61P1/04A61P1/00A61P3/10A61P17/06A61P17/00A61P17/02A61P37/02A61P37/06A61P27/12A61P11/06
CPCC07J43/003A61P1/00A61P1/04A61P3/10A61P5/14A61P5/24A61P5/28A61P5/32A61P5/38A61P9/00A61P11/06A61P13/00A61P13/02A61P13/08A61P15/00A61P15/08A61P17/00A61P17/02A61P17/06A61P17/08A61P17/10A61P17/14A61P19/02A61P19/10A61P21/04A61P25/00A61P25/28A61P27/12A61P29/00A61P35/00A61P37/02A61P37/06A61P43/00
Inventor J·梅辛格U·舍恩B·胡森H-H·托勒P·科斯基米耶斯L·卡利奥
Owner SOLVAY PHARMA GMBH
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