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

A hydroxyl and alkyl technology, applied in the field of new estratriene-triazole derivatives, can solve the problem of not being able to reach the level of T castration in men

Inactive Publication Date: 2012-09-12
SOLVAY PHARMA GMBH
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  • Abstract
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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

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

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Embodiment Construction

[0273] definition

[0274] The following terms are used to describe the various components of the chemical compositions used in the present invention. The terms are defined as follows:

[0275] As used herein, the terms "comprises" and "including" are used herein in their open-ended, non-limiting sense.

[0276] The term "compound" is to be understood herein to encompass any and all isomers (such as enantiomers, stereoisomers, diastereomers, rotamers and tautomers), racemates or any mixture of isomers, prodrugs and any pharmaceutically acceptable salts of said compounds, unless the formula describing the compound clearly shows a particular stereochemistry.

[0277] When the plural form is used for compounds, salts, etc., it is also used to refer to a single compound, salt, etc.

[0278]The term "17β-hydroxysteroid dehydrogenase type I" or simply "17β-HSD1" is used for the enzyme EC 1.1.1.62, and reduces estrone (E1) to the biologically active estrogen, estradiol (E2) .

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

Description

technical field [0001] 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 enzymes and / or steroid hormone-dependent diseases or disorders requiring regulation of endogenous 17[beta]-estradiol and / or testosterone concentrations. Background technique [0002] The publications and other materials used herein to illustrate the background of the inventio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J43/00A61K31/58A61P35/00A61P13/00A61P5/32
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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