Use of symipristone compound for treating AIDS

A compound and AIDS technology, which is applied in the field of preparation of AIDS drugs, cymipristone compounds, can solve the problems of delayed drug resistance, emergence, and inability to fundamentally solve the problem of drug resistance

Inactive Publication Date: 2007-01-24
SHANGHAI THREE ALLIANCE BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because HIV has a high degree of antigenic variability, it is very easy to produce drug resistance, and the use of one of the above drugs alone often leads to treatment failure due to the rapid development of drug resistance
Although the simultaneous use of reverse transcriptase inhibitors and proteolytic enzyme inhibitors (cocktail therapy) can delay the emergence of drug resistance and prolong the life of AIDS patients, it cannot fundamentally solve the problem of drug resistance and completely cure AIDS
Cocktail therapy can produce severe toxic side effects (such as bone marrow suppression and amnesia, etc.) and lead to the emergence of drug-resistant virus strains

Method used

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  • Use of symipristone compound for treating AIDS
  • Use of symipristone compound for treating AIDS
  • Use of symipristone compound for treating AIDS

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: the preparation method of Cymipristone

[0031] Synthetic route of cymipristone:

[0032]

[0033] Epoxy adduct Cymipristone

[0034] (1) Preparation of 4-(N-methyl-N-cyclohexylamino)phenylmagnesium bromide

[0035] In a four-neck flask, put 1.4 grams of magnesium flakes (Mg) and 10 milliliters of anhydrous tetrahydrofuran (THF), without adding iodine or a little iodine, and drop 10.86 grams of 4-bromo-N-methyl- N-cyclohexylaniline (dissolved in 24 milliliters of anhydrous tetrahydrofuran), dropwise, continue to insulate and stir for 1 hour to obtain a tetrahydrofuran solution of 4-(N-methyl-N-cyclohexylamino)phenylmagnesium bromide (to be step addition reaction).

[0036] (2) 3,3-ethylenedioxy-5α, 17β-dihydroxy-11β-[4-(N-methyl-N-cyclohexylamino)phenyl]-17α-(1-propynyl)- Preparation of 9(10)-estrene (adduct)

[0037] In a four-neck bottle, put 5 grams of 3,3-ethylenedioxy-5,10-epoxy-17α-(1-propynyl)-17β-hydroxyl-9(11)-estrene (epoxy matter), 29.1...

Embodiment 2

[0044] Embodiment 2: Determination of human-derived glucocorticoid receptor binding activity

[0045] Purpose of the test: To detect the binding ability of cymipristone to the human glucocorticoid receptor and compare it with Mifepristone which has a similar chemical structure.

[0046] (1) Test method

[0047] The reaction buffer consists of 25mM NaPO 4 , 20mM NaMoO 4 , 10mM KF and 10% Glycerol (pH=7.3), stored at 4°C until use. The stock solution was prepared from CHAPS and DTT and stored at -20°C for future use. Positive drug (Dexamethasone) and test compound solutions were prepared according to a certain concentration gradient, and 2.5 μl was added to each well of a 96-well plate. Take out the required amount of reaction buffer and add it to the stock solution to make the final concentration reach CHAPS 0.25mM and DTT 2mM. Add protease inhibitors (Aprotinin and Leupeptin) to a final concentration of 1 μg / μl and place in an ice bath. After human nuclear receptors GR (...

Embodiment 3

[0052] Example 3: Detection of the binding activity of cymipristone to rat liver cell plasma glucocorticoid receptors Ketone (Mifepristone) for comparison.

[0053] (1) Test method

[0054] Female clean SD rats, weighing 200-250 grams, were fed quantitatively and had free access to water. The breeding temperature is controlled at about 24 degrees Celsius, and the light is 11 hours during the day-13 hours at night. All experimental animals were observed for 1 week before the experiment.

[0055] Bilateral incisions were made under the dorsal rib arch of the rats, and the bilateral adrenal glands of the rats were removed. After the operation, they were fed with normal saline to maintain water and electrolyte balance.

[0056] On the third day after the operation, the animals were sacrificed acutely, and the liver was quickly taken out and placed in ice-cold buffer solution, and the blood was washed as much as possible. Take a certain amount of tissue and add buffer at a rati...

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Abstract

The present invention relates to the use of symipristone compound or its salt or solvolyte in preparing medicine for treating AIDS. Symipristone compound is one new kind of glucocorticoid receptor antagonist. Pharmacological test shows that symipristone compound possesses glucocorticoid resisting activity, powerful affinity to glucocorticoid receptor and function of blocking glucocorticoid receptor. The extracorporeal test proves the obvious growth inhibiting effect of symipristone on AIDS pathogen HIV-1.

Description

field of invention [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to the use of cymipristone compounds in the preparation of drugs for treating AIDS. Background technique [0002] AIDS (Acquired Immuno-deficiency Syndrome, AIDS, acquired immune deficiency syndrome) is one of the major infectious diseases that threaten human health and life in the world today. The pathogen that causes AIDS, that is, Human Immunodeficiency Virus (Human Immunodeficiency Virus, HIV), is divided into two subtypes, HIV-1 and HIV-2. HIV-1 has strong pathogenicity and is the main pathogen causing the global AIDS epidemic; HIV-2 has lower transmission power and pathogenicity than HIV-1, and its incubation period and course of disease are longer, and symptoms are milder. It doesn't even develop into AIDS. HIV-1 infection accounts for the vast majority of AIDS patients, and HIV-2 infection is limited to West Africa. Therefore, current research ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K31/567A61P31/18
CPCA61K31/565A61P31/18
Inventor 王明伟左林应明华
Owner SHANGHAI THREE ALLIANCE BIOTECH
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