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EGFR (epidermal growth factor receptor) inhibitor and medical application thereof

A pharmaceutical and prodrug technology, applied in the field of EGFR inhibitors and their medical applications, can solve the problems of drug resistance and poor selectivity of EGFR inhibitors

Active Publication Date: 2019-06-21
WUHAN DENUOMEI BIOLOGY MEDICINE TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the second-generation inhibitors have solved the problem of drug resistance to a certain extent, due to their high inhibition of wild-type EGFR, side effects such as diarrhea and rash
[0006] In order to solve the defects of existing EGFR inhibitor drug resistance and poor selectivity, it is still necessary to develop more safer and more effective EGFR inhibitor drugs to achieve better tumor treatment effects and better meet clinical needs and market needs

Method used

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  • EGFR (epidermal growth factor receptor) inhibitor and medical application thereof
  • EGFR (epidermal growth factor receptor) inhibitor and medical application thereof
  • EGFR (epidermal growth factor receptor) inhibitor and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] The preparation of embodiment 1 compound I-a

[0073]

[0074] Compound shown in formula I-a-1 (1.69g, 5.77mmol) was dissolved in 80mL isopropanol, to which was added compound shown in formula 2 (840mg, 5.77mmol) and p-toluenesulfonic acid (993mg, 5.77mmol), and The mixture was stirred and reacted at 70°C for 6 hours. After the reaction was detected by TLC, the solvent was evaporated under reduced pressure, and the residual solid was dispersed in 200 mL of ethyl acetate, washed with saturated aqueous sodium bicarbonate, water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure The crude product was obtained, and the compound represented by formula I-a was separated by column chromatography (yield 811 mg, yield 35%, HPLC purity 99.8%).

[0075] m / z:403(M+H) + .

Embodiment 2

[0076] The preparation of embodiment 2 compound I-b

[0077]

[0078] The preparation method of compound I-b was experimented in a manner similar to Example 1, except that the starting material was changed to compound I-b-1. Purification by silica gel chromatography gave the compound represented by formula I-b (yield 59%, HPLC purity 99.4%).

[0079] m / z:430(M+H) + .

Embodiment 3

[0080] The preparation of embodiment 3 compound I-c

[0081]

[0082] The preparation method of compound I-c was experimented in a manner similar to that of Example 1, except that the starting material was changed to compound I-c-1. Purification by silica gel chromatography gave the compound represented by formula I-c (yield 55%, HPLC purity 99.0%).

[0083] m / z:442(M+H) + .

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PUM

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Abstract

The invention discloses an EGFR (epidermal growth factor receptor) inhibitor and medical application thereof. The compound is a compound as shown in a formula I, pharmaceutically acceptable salt or prodrug. The compound can be applied to preparation of medicines for treating and / or preventing cancer.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and relates to an EGFR inhibitor and its medical use. Background technique [0002] Malignant tumor is a common and frequently-occurring disease that seriously threatens human health. It is caused by abnormal proliferation of cells in the human body. Lung cancer, gastrointestinal cancer and liver cancer are the most common tumors in men, accounting for more than 70% of all cases (lung cancer 23%, gastric cancer 15.2%, liver cancer 13.57%, esophageal cancer 10.46%, colorectal cancer 9.39%), while breast cancer, Lung cancer, gastrointestinal cancer and liver cancer are the most common tumors in women, accounting for more than 60% of all cases (breast cancer 16.97%, lung cancer 14.85%, colorectal cancer 9.68%, gastric cancer 8.53%, liver cancer 6.17%). With the aging population in China, the prevalence of cancer is bound to increase. In addition, environmental pollution has also increased the p...

Claims

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Application Information

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IPC IPC(8): C07D403/04C07D401/04A61K31/517A61P35/00
Inventor 邱启裕全欣鑫
Owner WUHAN DENUOMEI BIOLOGY MEDICINE TECH
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