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Androgen receptor antagonist and preparation method and use thereof

A use, halogen technology, applied in the field of androgen receptor antagonists and their preparation and use, can solve the problems that cannot be treated with prostate patients

Active Publication Date: 2021-02-05
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It should be noted that many antagonists of steroidal corticosteroids have the effect of activating androgen receptors, so they cannot be used in the treatment of prostate patients

Method used

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  • Androgen receptor antagonist and preparation method and use thereof
  • Androgen receptor antagonist and preparation method and use thereof
  • Androgen receptor antagonist and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] The synthesis of compound among the present invention in embodiment 1

[0063] Synthetic scheme one:

[0064]

[0065] Synthesis scheme two:

[0066]

[0067] Synthetic scheme three:

[0068]

[0069] Wherein X is halogen Cl, Br, I, when R 6 , R 6 X can be F when forming a ring with the amino group on the A ring, then the reaction of the A ring and the C ring can be synthesized by a nucleophilic substitution reaction instead. When the B ring is an N-containing heterocycle, such as imidazole, pyrazole, benzimidazole, etc., there is no need to use boronic acid as a substrate, and the nucleophilic substitution reaction or metal-catalyzed coupling reaction is directly connected to the A ring to form a C-N bond.

[0070] The following compounds were prepared:

[0071]

[0072]

[0073] 1. Synthesis of compound SKLB-C4558:

[0074]

[0075] Dissolve NaH (25mg, 0.625mmol) in dry DMF (3ml), cool to 0°C, slowly add compound b (50mg, 0.25mmol), stir for 30mi...

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Abstract

The invention discloses a compound represented by formula (I). The present invention also relates to a pharmaceutical composition containing the compound of formula (I) and the use of the compound in the preparation of androgen receptor antagonist drugs. The compound of the present invention or its pharmaceutical composition can be used to treat prostate cancer, benign prostatic hyperplasia, hirsutism, alopecia, anorexia, breast cancer, acne or male sexual dysfunction.

Description

technical field [0001] The present invention relates to androgen receptor antagonist and its preparation method and use. Background technique [0002] Prostate cancer is an epithelial malignant tumor that occurs in the prostate gland. It is the most common malignant tumor in men in Western countries and the third leading cause of cancer death. In 2012, the incidence rate of prostate cancer in my country's tumor registration areas was 9.92 / 100,000, ranking sixth among male malignant tumors. When the cancer has not metastasized and is in a curable early stage, it can be cured by surgical resection or radiation therapy. Androgen deprivation therapy (ADT) is effective for most patients in a certain period of time, but about 40% of them will develop into castration-resistant prostate cancer (CRPC). [0003] Androgen receptor (AR) plays a very important role in the occurrence and development of prostate cancer. Studies have shown that castration-resistant prostate cancer still d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/04C07D307/52C07D235/06C07D231/12C07D215/12C07D261/08C07D413/12C07D333/20C07D213/36C07D233/56C07D233/61C07D239/26C07D413/04C07D403/04C07C255/58A61K31/277A61K31/4439A61K31/4709A61K31/4184A61K31/351A61K31/415A61K31/422A61K31/4155A61K31/4178A61K31/47A61K31/42A61K31/4164A61K31/505A61K31/381A61K31/44A61K31/4406A61K31/4409A61K31/506A61K31/4725A61P35/00A61P13/08A61P17/00A61P25/00A61P17/14A61P17/10A61P15/10
CPCC07C255/58C07D213/36C07D215/12C07D231/12C07D233/56C07D233/61C07D235/06C07D239/26C07D261/08C07D307/52C07D333/20C07D401/04C07D403/04C07D413/04C07D413/12
Inventor 余江陈元伟
Owner SICHUAN UNIV