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Compound used as CYP11B, CYP17 and/or CYP21 inhibitor

A CYP11B and compound technology, which is applied in the field of compounds as CYP11B, CYP17 and or CYP21 inhibitors, can solve the problems of drug treatment not being a treatment plan, drug deficiency, limitation of CYP11B1 activity and efficacy, etc.

Inactive Publication Date: 2015-09-23
郭明山
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

2. There is still a lack of safe and effective drugs to block the excessive production of cortisol, and drug therapy is not the main treatment option
Although these drugs are clinically significant, efficacy is limited by lack of potency to block CYP11B1 activity

Method used

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  • Compound used as CYP11B, CYP17 and/or CYP21 inhibitor
  • Compound used as CYP11B, CYP17 and/or CYP21 inhibitor
  • Compound used as CYP11B, CYP17 and/or CYP21 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0023] Example 1: Add 6.8 g of ethylene glycol to 34.7 g of D4A in 500 ml of anhydrous ether, cool down to -78 degrees, add 26.7 g of iodotriethylsilane dropwise, and react for 5 h. Cool down to room temperature, add 100ml of water to wash twice, dry over anhydrous sodium sulfate, evaporate the organic solvent under reduced pressure, and about 25g of the product crystallizes from dichloromethane.

[0024]

example 2

[0025] Example 2: Add 14.4 g of 2-mercaptoethylamine hydrochloride to 34.7 g of D4A in 500 ml of anhydrous methanol, and react at 35 degrees for 3.5 hours. Cool down to room temperature, add saturated sodium bicarbonate to raise the pH to about 8, add 100 ml of water to wash twice, dry over anhydrous sodium sulfate, evaporate the organic solvent under reduced pressure, and obtain about 32 g of the product crystallized from dichloromethane.

[0026]

example 3

[0027] Example 3: Add 8.5g of 2-mercaptoethanol to 34.7g of D4A in anhydrous 500ml of ether, fill it with hydrogen chloride gas at 20°C, and react for 0.5h. Saturated sodium bicarbonate was added to raise the pH to about 8, the organic phase was washed twice with 100 ml of water, dried over anhydrous sodium sulfate, the organic solvent was evaporated under reduced pressure, and about 35 g of the product was crystallized from dichloromethane.

[0028]

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PUM

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Abstract

The invention provides a CYP11B, CYP17 and / or CYP21 inhibitor shown in the formula A and applications to treatment of androgen-dependent diseases, illnesses and symptoms. The invention further describes at least one kind of pharmaceutical composition.

Description

technical field [0001] The present invention provides a compound that is an inhibitor of CYP11B, CYP17 and / or CYP21, and it is used for treating androgen-dependent diseases, diseases and conditions through oral or injection route. The invention also describes the synthesis method of the novel compound. technical background [0002] Prostate cancer is a human-specific disease. It is one of the most common malignant tumors in men in Europe and the United States. In the United States, the incidence of prostate cancer ranks first, and the mortality rate is second only to lung cancer. The incidence of prostate cancer in Asian countries such as China, Japan, and India is far lower than that in Europe and the United States, but there is an increasing trend. [0003] In my country, prostate cancer has increased from 1.71 / 100,000 male population in 1993 to 7.9 / 100,000 males, and it is increasing at an annual rate of 10%. With the aging phenomenon of our society becoming more and mo...

Claims

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Application Information

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IPC IPC(8): C07J71/00C07J43/00A61K31/58A61P35/00A61P13/08A61P17/00A61P17/10
CPCC07J43/003
Inventor 郭明山
Owner 郭明山
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