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Steroid derivatives

A technology of drugs and compounds, applied in the field of steroid derivatives, to achieve the effect of reducing side effects and blocking stimulation

Inactive Publication Date: 2005-11-02
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, through clinical research, it has been found that although the side effects of this drug are far less than a series of steroidal compounds such as tamoxifen, tamoxifen, and medroxyprogesterone, there are still some unwanted clinical side effects, such as vaginal bleeding, body odor changes, and sleepwalking. State, gastrointestinal reactions, 2.5% of patients discontinued the drug due to side effects during clinical treatment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1) Preparation of 17-β-propionyloxy-7α-[9-(dimethyl-tert-butylsiloxy)nonyl]-estr-4-en-3-one

[0036]In a 500 ml reaction flask, drop magnesium chips (2.84 grams) and THF (40 milliliters), add dropwise a mixed solution of bromosilyl ether (41 grams) and THF (140 milliliters) under stirring, and react at room temperature for 3 About an hour until the action of magnesium shavings is complete. Cool to internal temperature -30°C, add cuprous chloride (1 g), stir for 5 minutes, then add dropwise the mixed solution of intermediate (II) (9.2 g) and THF (50 ml), after dropping, keep warm - React at 35°C for 1 hour. After the reaction, add 100 ml of glacial acetic acid to the reaction solution. After stirring completely, add diethyl ether (300 ml) and water (200 ml), separate layers, and reverse the aqueous layer with diethyl ether (100 ml*2). Extracted, combined organic layers, washed with water (100 ml), brine (100 ml*2) successively, dried, filtered and concentrated to dryne...

Embodiment 2

[0048] The compound of the present invention and fulvestrant have been done drug effect contrast research, by experiment, have drawn following data and conclusion:

[0049] group

dosage

(mg / piece)

way

number of animals

d0 dn

weight

(gram)

d0 dn

TV

x±SD

d0 dn

RTV

x±SD

T / C

(%)

Fulvestrant

NS

S.C.

6 4

20 20

66±11 133±34

2.1±0.5

Example 1

5

S.C.

53

22 22

62±11 98±20

1.7±0.5

79.3

Example 1

3

S.C.

64

20 20

39±21 76±9

1.9±0.7

90.0

[0050] d0: The time of drug administration in separate cages

[0051] dn: the time when the actual therapeutic effect is the best, this experiment is 28 days after the first administration

[0052] TV: tumor volume

[0053] RTV: relative tumor volume (V n / V 0 )

[0054] T / C: Anti-tumor activity e...

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PUM

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Abstract

The invention relates to the compound and its salt in formula(ó±), wherein R1 represents linear or branched chain alkane with one to four carbon atoms, or halogenated linear or branched chain alkane; and bittern atoms mean fluorine atom, chlorine atom, bromine atom and iodine atom. Such compound is provided with therapeutic activity in breast cancer.

Description

technical field [0001] The invention relates to a steroid derivative, and the obtained product can be used as medicine for treating female breast cancer. Background technique [0002] Breast cancer is one of the major diseases seriously affecting women's health worldwide. Once breast cancer is formed, it is a systemic disease. Cancer cells continue to fall off from the primary tumor and enter the blood and lymph circulation. Even in the early stage, there may be micrometastases in the body. Even after surgical resection, the 5-year and 10-year survival rates of breast cancer patients are only 64% and 46%. [0003] At present, the reported drugs for the treatment of breast cancer mainly focus on three aspects: chemotherapy drugs, endocrine therapy drugs, and immune drugs. Among them, endocrine therapy drugs play an important role in the drug treatment of breast cancer through anti-estrogen and other effects, and it has been reported that they can reduce the annual mortality...

Claims

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Application Information

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IPC IPC(8): A61K31/565A61P5/30A61P35/00C07J31/00C07J63/00
CPCC07J31/00A61P5/30A61P35/00
Inventor 钟慧娟吕爱峰
Owner JIANGSU HANSOH PHARMA CO LTD
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