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7 alpha-substituted 11 alpha-hydroxysteroids and its microbiological production method

A technique of steroids and pharmacology, applied in the field of 7α-substituted 11α-hydroxy steroids and their microbiological preparation

Inactive Publication Date: 2007-03-07
SCHERING AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, reference is also made to Shibahara et al., Biochim. Biophys. Acta, 202 (1970), 172-179 in the introduction of the specification, which reports that microbial 11α-hydroxylation in steroids may be unpredictable

Method used

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  • 7 alpha-substituted 11 alpha-hydroxysteroids and its microbiological production method
  • 7 alpha-substituted 11 alpha-hydroxysteroids and its microbiological production method
  • 7 alpha-substituted 11 alpha-hydroxysteroids and its microbiological production method

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Experimental program
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Embodiment 1

[0124]

[0125] The inclined bacillus culture of Gnomonia cingulata bacterial strain (CBS 15226) was inoculated in a container containing 3% by weight of glucose, 1% by weight of corn steep liquor, 0.2% by weight of NaNO 3 , 0.1 wt% KH 2 PO 4 , 0.2 wt% K 2 HPO 4 , 0.05% by weight KCl, 0.05% by weight MgSO 4 ·7H 2 O and 0.002 wt% FeSO 4 ·7H 2 O (pH 6.0) in 1000 ml of nutrient solution autoclaved at 121° C. for 30 minutes in a 2-liter Erlenmeyer flask at 28° C. on a rotary shaker at 165 rpm for 72 hours. After such preculture, it was inoculated in a 20 liter fermenter covered with 19 liters of sterile medium having the same final composition as the preculture described above. In addition, another 1.0 ml of silicone oil and 1.0 ml of synperonic (oxoalcoholethoxylate) were added to reduce foaming. After a 12-hour growth period at an overpressure of 0.7 bar at a temperature of 28°C, aeration at 20 l / min, stirring at 250 rpm and addition of 4.0 g of 17β-hydroxy-7α-methyle...

Embodiment 2

[0127]

[0128] The Incline bacillus culture of Glomerella cingulata strain (IFO 6425) was inoculated in a container containing 3% by weight of glucose, 1% by weight of corn steep liquor, 0.2% by weight of NaNO 3 , 0.1 wt% KH 2 PO 4 , 0.2 wt% K 2 HPO 4 , 0.05% by weight KCl, 0.05% by weight MgSO 4 ·7H 2 O and 0.002 wt% FeSO 4 ·7H 2 O (pH 6.0) in 1000 ml of nutrient solution autoclaved at 121° C. for 30 minutes in a 2-liter Erlenmeyer flask at 28° C. on a rotary shaker at 165 rpm for 72 hours. After such preculture, it was inoculated in a 20 liter fermenter covered with 19 liters of sterile medium having the same final composition as the preculture described above. In addition, another 1.0ml of silicone oil and 1.0ml of synperonic were added to reduce foaming. After a 12-hour growth period at an overpressure of 0.7 bar at a temperature of 28°C, aeration at 10 l / min, stirring at 350 rpm and addition of 2.0 g of 17β-hydroxy-7α-methylestr-4-en-3-one 30ml of DMF solutio...

Embodiment 3

[0131]

[0132] The culture of Aspergillus ochraceae (CBS 13252) was inoculated in a culture chamber containing 3% by weight of glucose, 1% by weight of corn steep liquor, 0.2% by weight of NaNO 3 , 0.1 wt% KH 2 PO 4 , 0.2 wt% K 2 HPO 4 , 0.05% by weight KCl, 0.05% by weight MgSO 4 ·7H 2 O and 0.002 wt% FeSO 4 ·7H 2 O (pH 6.0) in 500 ml of nutrient solution autoclaved at 121° C. for 30 minutes in a 2 L Erlenmeyer flask, shaken at 28° C. on a rotary shaker at 165 rpm for 72 hours. After such preculture, it was reinoculated in a 10-liter fermentor covered with 9.5 liters of sterile medium having the same final composition as the preculture described above. In addition, another 0.5ml of silicone oil and 0.5ml of synperonic were added to reduce foaming. After a 6-hour growth period at an overpressure of 0.7 bar and a temperature of 28°C, aeration at 5 liters / min, stirring at 350 rpm and addition of 1.0 g of 7α-methylestr-4-ene-3,17-dione 15ml DMF solution. Continue to...

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Abstract

Disclosed is a new synthetic pathway for the production of precursors for the production of compounds having general formula (8,10,12). During said synthesis, compounds of general formal (4,B) are produced in a microbiological reaction. The meanings of radicals R<7>, R<10>, R<11>, R<13>, R<17> and R<17'> and group U-V-W-X-Y-Z are defined in the patent claims.

Description

[0001] This application is a divisional application of the invention patent application No. 03817696.3 (PCT / EP2003 / 008111) entitled "Microbiological method for preparing 7α-substituted 11α-hydroxy steroids" filed on July 24, 2003. technical field [0002] The present invention relates to a microbial process for the preparation of 7α-substituted 11α-hydroxy steroids and to 7α,17α-substituted 11β-halogen steroids which can be prepared therefrom, to a process for the preparation of the latter compounds and to their use as well as to compounds comprising these pharmaceutical preparations. Furthermore, the present invention relates to other 7α-substituted 11β-halogen steroids, namely 7α-substituted estro-1,3,5(10)-tri alkene. Background technique [0003] Androgens, especially testosterone, are used to treat andropause symptoms and for male genital development and male birth control. In addition, these hormones also have some anabolic active ingredients that promote, for exampl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00C07J3/00C07J5/00C07J7/00C07J9/00C07J11/00C07J31/00C07J41/00C12P33/10C12P33/16A61K31/56A61P15/12A61P15/16
CPCC12P33/10C07J41/00C12P33/16C07J3/00C07J11/00C07J1/00C07J5/00C07J1/0051C07J7/00C07J9/00C07J31/00
Inventor 路德维希·措恩罗尔夫·博尔曼诺贝特·加卢斯赫尔曼·金策尔汉斯-彼得·穆恩赖因哈德·努贝迈尔
Owner SCHERING AG
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