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Composition, synthesis and application of hydantoin derivatives

A technology of hydantoin and derivatives, which is applied in the composition of hydantoin derivatives and its medical application, and can solve the problems that the research and development of prostate cancer drugs cannot be carried out accurately.

Inactive Publication Date: 2012-07-04
陈德桂
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although many biotechnology companies and major pharmaceutical companies in the world have drug research and development programs targeting the androgen receptor, the mechanisms that cause anti-androgen therapy-resistant prostate cancer have not been discovered until recently, so anti-androgen Drug development in therapy-resistant prostate cancer can't be done accurately

Method used

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  • Composition, synthesis and application of hydantoin derivatives
  • Composition, synthesis and application of hydantoin derivatives
  • Composition, synthesis and application of hydantoin derivatives

Examples

Experimental program
Comparison scheme
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Embodiment Construction

[0052] Compound CD1

[0053] 4-[3-(6-cyano-5-trifluoromethylpyridin-3-yl)-5,5-dimethyl-4-oxo-2-thioimidazolidin-1-yl]-benzene Butanamide

[0054]

[0055] 5-Amino-2-cyano-3-(trifluoromethyl)pyridine (10 g) dissolved in 18 mL THF was slowly added to an aqueous solution (120 mL) containing 5 mL thiophosgene at room temperature After stirring for 50 minutes, it was extracted with dichloromethane (100 ml three times), the organic phase was washed with salt, and washed with anhydrous Na 2 SO 4 Drying, concentration under reduced pressure, passing through a silica gel column, and eluting with PE-EA (20:1) gave white solid compound 1A (5-isothiocyanate-2-cyano-3-(trifluoromethyl)pyridine, 10 gram).

[0056] Combine p-aminophenylbutyric acid (2 g), acetone cyanohydrin (16 ml) and MgSO 4 (6g) was heated to 80°C, stirred for 24 hours, added 50 ml of ethyl acetate and water for extraction after room temperature, and the organic phase was passed over MgSO 4 , concentrated under r...

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Abstract

The invention discloses medicinal composition, synthesis process and medical application of hydantoin derivatives. The compounds have an effect of inhibiting an androgen receptor, and can be used for treating prostatic cancer and other diseases and physiologic derangement related with androgen receptor activity.

Description

technical field [0001] The invention belongs to the field of medicine, and more specifically, the invention relates to the composition and medical application of hydantoin derivatives. Background technique [0002] Prostate cancer is a common disease in men over the age of 50. In recent years, the incidence of prostate cancer has shown a rapid increase. In western countries, its incidence rate ranks first among male malignant tumors, and its death rate also ranks second. In my country, during the ten years from 1991 to 2001, the incidence of prostate cancer in Shanghai increased from 2.7 cases / 100,000 to 12.7 / 100,000; during the same period, the incidence of the disease in Changchun also increased by 4.7 times; The incidence of prostate cancer in men over the age of 50 is 1.28%. Obviously, prostate cancer has constituted a major disease that endangers the health of modern people. [0003] For a small number of in situ prostate cancer detected early, nearly 70% of the pati...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/4439A61P35/00A61P13/08A61P5/26A61P15/14
Inventor 陈德桂
Owner 陈德桂
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