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Novel prodrug of steroid CYP 17 inhibitor as well as application and preparation method thereof

A drug and pharmaceutical technology, applied in the field of new drug precursors, can solve the problems of stimulating tumor growth, unable to inhibit androgen, etc., and achieve the effect of good application prospect and good anti-tumor activity

Active Publication Date: 2014-09-03
广州艾格生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In men with prostate cancer, the hormone testosterone stimulates tumor growth. Castration therapy, including drugs or surgery, can reduce testosterone production or block the effects of testosterone, but this treatment does not suppress androgen production elsewhere in the body , prostate cancer can continue to grow

Method used

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  • Novel prodrug of steroid CYP 17 inhibitor as well as application and preparation method thereof
  • Novel prodrug of steroid CYP 17 inhibitor as well as application and preparation method thereof
  • Novel prodrug of steroid CYP 17 inhibitor as well as application and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Synthesis of Compound (Abiraterone Ethyl Carbonate)

[0049]

[0050] Add 0.3 g of the raw material abiraterone into a 10 ml single-port reaction flask, then inject 1.0 ml of dichloromethane and 0.5 ml of pyridine, stir at room temperature for 10 min, then add dropwise 0.19 g of ethyl chloroformate diluted with 1.0 ml of dichloromethane at room temperature, Reaction at room temperature for 3h. After the reaction was finished, the reaction solution was concentrated to dryness, 10ml of ethyl acetate and 10ml of water were added to the concentrate, shaken and extracted, the organic phase was separated and washed twice with water, each 10ml. Take the organic phase and dry it with anhydrous sodium sulfate for 5 hours, filter and concentrate the filtrate to dryness to obtain a white solid, which is beaten and washed with a mixed solution of ethyl acetate / petroleum ether=1 / 5, finally filtered, and dried under reduced pressure and vacuum 0.2 g of abiraterone ethyl carbonate...

Embodiment 2

[0054] The preparation of embodiment 2 Abiraterone ethyl carbonate sheet

[0055]

[0056] After uniformly mixing the above-mentioned raw materials and auxiliary materials, it is wet granulated according to the conventional method, dried and pressed into tablets.

Embodiment 3

[0057] The preparation of embodiment 3 Abiraterone ethyl carbonate injection

[0058]

[0059] Take sodium chloride, stir and dissolve with water for injection, then add abiraterone ethyl carbonate, continue stirring to dissolve completely, adjust the pH value to 4-8 with hydrochloric acid / sodium hydroxide, add water for injection to the total amount, filter until clear, Potting, sterilization, that is.

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Abstract

The invention discloses a precursor compound of a novel abiraterone drug, wherein the precursor compound provides improved oral bioavailability and drug dynamic characteristic. The drug is an irreversible inhibitor of human body CYP17 enzyme, can be used for treating urogenital system or androgen-associated cancers, diseases or sickness, for example, human prostate cancer, breast cancer and prostatic hyperplasia.

Description

technical field [0001] The present invention provides a novel drug prodrug of abiraterone, a cholesterol CYP17 enzyme inhibitor, which is used for treating cancers, diseases or diseases related to genitourinary system or androgen, including castration-resistant prostate cancer. The invention also describes the synthesis method of the novel compound. Background technique [0002] Prostate cancer is the most common malignant tumor worldwide, and its incidence increases with age. The current aging population trend has led to a rapid increase in the number of patients with prostate cancer, which, after lung cancer, is the most common form of cancer in men and the second leading cause of death in American men. About 218,000 men in the United States are diagnosed with prostate cancer each year, and 32,000 die from it, according to the American Cancer Society. [0003] In my country, prostate cancer used to be a relatively rare disease, but the incidence of the disease has also b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J43/00A61K31/58A61P35/00A61P13/00A61P13/08A61P15/00
Inventor 张现涛谭斌何盛江于江月
Owner 广州艾格生物科技有限公司
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