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Crystal form of androgen receptor inhibitor and preparation method of crystal form

A technology of crystal formation and crystallization, which is applied in organic chemical methods, pharmaceutical formulations, organic active ingredients, etc., can solve the problem that anti-androgen therapy is no longer effective

Active Publication Date: 2019-06-21
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, castration surgery has a certain timeliness. Many patients undergo a transition from androgen-dependent to androgen-independent for a period of time after castration. They are no longer effective for anti-androgen therapy and develop androgen-independent Prostate cancer (androgen independent prostate cancer, AIPC), and the occurrence of AlPC is still related to the activation of AR signaling pathway in PCa cells

Method used

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  • Crystal form of androgen receptor inhibitor and preparation method of crystal form
  • Crystal form of androgen receptor inhibitor and preparation method of crystal form
  • Crystal form of androgen receptor inhibitor and preparation method of crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Weigh 150 mg of the I crystal form of the compound represented by the formula (I) (prepared according to the method disclosed in WO2017041622) and put it into a reaction flask, add 6 ml of ethanol to dissolve, then add 30 ml of petroleum ether, leave it at room temperature for 30 min, and filter to obtain the formula (I ) of the B crystal form of the compound shown. Its X-ray diffraction pattern is shown in figure 1 , whose DSC spectrum is shown in Figure 8 , and its characteristic peak positions are shown in the table below:

[0099] Table 1. Characteristic peaks of crystal form B

[0100]

Embodiment 2

[0102] Weigh 150 mg of the crystal form I of the compound represented by the formula (I) and put it into a reaction flask, add 0.5 ml of dioxane to dissolve it, then add 5 ml of n-hexane, let it stand at room temperature for 6 hours, and filter to obtain the compound represented by the formula (I) C crystal form. Its X-ray diffraction pattern is shown in figure 2 , whose DSC spectrum is shown in Figure 9 , and its characteristic peak positions are shown in the table below:

[0103] Table 2. Characteristic peaks of crystal form C

[0104]

[0105]

Embodiment 3

[0107] Weigh 150 mg of crystal form I of the compound represented by formula (I) into a reaction flask, add 0.5 ml of acetonitrile to dissolve, then add 5 ml of water, let stand at room temperature for 1 hour, and filter to obtain crystal D of the compound represented by formula (I) type. Its X-ray diffraction pattern is shown in image 3 , whose DSC spectrum is shown in Figure 10 , and its characteristic peak positions are shown in the table below:

[0108] Table 3. Characteristic peaks of crystal form D

[0109]

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Abstract

The invention relates to a crystal form of an androgen receptor inhibitor and a preparation method of the crystal form, in particular to a crystal form of the androgen receptor inhibitor shown in a formula (I) and a preparation method of the crystal form. The crystal form has good stability and can be better used for clinical treatment.

Description

technical field [0001] The invention relates to a new crystal form of an androgen receptor inhibitor and a preparation method thereof. Background technique [0002] Prostate cancer (PCa) is a malignant tumor occurring in male prostate tissue, which is the result of abnormal and disordered growth of prostate acinar cells. The differentiation and growth of normal prostate epithelial cells and the development of prostate cancer depend on androgen, and androgen is mainly synthesized in the testis, accounting for about 80-90%. Synthetic androgen enters the cell and binds to the androgen receptor (AR), causing heat shock protein (HSP) to dissociate from AR and allowing AR to enter the nucleus, activating multiple downstream genes, including prostate-specific antigen (PSA) . Early prostate cancer is sensitive to male hormones, and orchiectomy (castration) can significantly inhibit the development of prostate cancer. However, castration surgery has a certain timeliness. Many pati...

Claims

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Application Information

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IPC IPC(8): C07D233/86A61K31/4166A61P35/00
CPCC07D233/86A61P35/00C07B2200/13
Inventor 周先强王立坤杜振兴
Owner JIANGSU HENGRUI MEDICINE CO LTD
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