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Compound serving as inhibitor for CYP11B, CYP17 and CYP21

A compound and composition technology, applied in the field of compounds as inhibitors of CYP11B, CYP17, and CYP21, can solve problems such as potency blocking, CYP11B1 activity potency limitation, etc.

Inactive Publication Date: 2017-01-04
郭明山
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these drugs are clinically significant, efficacy is limited by lack of potency to block CYP11B1 activity

Method used

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  • Compound serving as inhibitor for CYP11B, CYP17 and CYP21
  • Compound serving as inhibitor for CYP11B, CYP17 and CYP21
  • Compound serving as inhibitor for CYP11B, CYP17 and CYP21

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0028] Example 1: Put 3.62g of SM in diethyl ether, add 2.2g of triethylamine, 1.2g of ethoxyformyl chloride, and react at room temperature for 2h. Add 50ml of EA, add 10ml of water to wash twice, dry the organic phase with anhydrous sodium sulfate, evaporate the organic solvent under reduced pressure, and obtain about 3.5g of the product crystallized from dichloromethane.

[0029]

example 2

[0030] Example 2: Put 3.62g SM in tetrahydrofuran, add 5.0g iron powder, add dropwise 0.95g acetyl chloride, and react at room temperature for 5h. Add 50ml of EA, add 10ml of water to wash twice, dry the organic phase with anhydrous sodium sulfate, evaporate the organic solvent under reduced pressure, and obtain about 2.7g of product crystallized from dichloromethane.

[0031]

example 3

[0032] Example 3: Add 0.95 g of acetyl chloride to 3.62 g of SM in ether, react at room temperature for 2 h, and filter. 50ml EA was added to the mother liquor, 10ml water was added to wash twice, the organic phase was dried over anhydrous sodium sulfate, and the organic solvent was evaporated under reduced pressure, and about 2.7g of the product was crystallized from dichloromethane.

[0033]

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PUM

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Abstract

The invention provides an inhibitor for CYP11B, CYP17 and / or CYP21 as shown in a formula A. The inhibitor is used for treating androgen dependent diseases and symptoms.

Description

technical field [0001] The present invention provides a compound as an inhibitor of CYP11B, CYP17, and CYP21, which is administered orally or by injection for the treatment of androgen-dependent diseases, disorders, and conditions. Synthetic methods for this compound are also described herein. [0002] technical background [0003] 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. [0004] 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 mor...

Claims

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Application Information

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IPC IPC(8): C07J43/00A61K31/58A61P35/00A61P13/08A61P17/10A61P17/14A61P17/00A61P15/00
Inventor 郭明山
Owner 郭明山
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