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Compound for treating prostatic cancers, preparation method therefor and use of compound

A technology for prostate cancer and compounds, which is applied in the directions of steroids, medical preparations containing active ingredients, organic chemistry, etc., can solve problems such as drug treatment not being a treatment plan, drug deficiency, and limitation of CYP11B1 activity and efficacy.

Inactive Publication Date: 2017-10-03
李成凤
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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 for treating prostatic cancers, preparation method therefor and use of compound
  • Compound for treating prostatic cancers, preparation method therefor and use of compound
  • Compound for treating prostatic cancers, preparation method therefor and use of compound

Examples

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Embodiment Construction

[0018] The present invention will be described in detail below in conjunction with the examples. The examples of the present invention are only used to illustrate the technical solutions of the present invention, and do not limit the essence of the present invention.

[0019] Put 3.6g of Formula B in 20ml of dichloromethane, add 1.3g of triethylamine, dropwise add 1.8g of acetyl chloride at room temperature, react for 1h, after the reaction is complete, wash twice with 10ml of water, dry over anhydrous sodium sulfate, and concentrate to obtain the product 4.0 g.

[0020]

[0021] Put 3.6g of formula B in 20ml of dichloromethane, add 1.9g of N-Boc glycine, add 1.1g of thionyl chloride dropwise at zero degree, react for 1h, then react for 2h at room temperature, after concentration, add 20ml of methanol, add 2ml of 1N hydrochloric acid , refluxed for 1h, cooled to room temperature, added 20ml of water, adjusted the pH to about 8 with a saturated sodium bicarbonate solution, f...

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Abstract

The invention provides use of a compound represented by a formula A shown in the description in the treatment of androgen-dependent diseases, disease symptoms and diagnostic signs. The invention further provides a synthesis method for the compound.

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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Patent Type & Authority Applications(China)
IPC IPC(8): C07J43/00A61K31/58A61P35/00A61P13/08A61P17/10A61P17/14A61P15/08A61P5/28A61P17/00
CPCC07J43/003
Inventor 李成凤
Owner 李成凤