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Tyrosine kinase inhibitor and application thereof

A tyrosine kinase and inhibitor technology, applied in the field of tyrosine kinase inhibitors, can solve the problem of genotoxic impurities

Pending Publication Date: 2021-10-29
成都蓝蜻蜓生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So many side effects may also be related to too many genotoxic impurities of lenvatinib

Method used

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  • Tyrosine kinase inhibitor and application thereof
  • Tyrosine kinase inhibitor and application thereof
  • Tyrosine kinase inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The preparation of compound (two), such as figure 1 shown in;

[0041] Wherein: compound 3 is synthesized as;

[0042] Add 900ml of DMSO into a 3L reaction flask, then add 64g of KOH, vacuumize, replace with nitrogen once, and keep adding 98.9g of compound 1 into the reaction flask under nitrogen.

[0043] Rinse wall material with 100ml DMSO. Cool the reaction liquid to 20-25°C, add water dropwise to the reaction bottle (dropping time is 10-15 minutes), (the reaction is slightly exothermic) and control the temperature to be less than 40°C.

[0044] After the water is added dropwise, keep stirring until the system changes from reddish brown to dark black (about 0.5-1h), and continue stirring for 10-15 minutes after the system changes color.

[0045] Add 100g of compound 2 to the reaction flask at one time, raise the temperature to 90°C, stir for 2 hours, cool down to 55°C, add 500ml of acetone and 1000ml of water to the reaction solution dropwise, keep warm at 50 to 5...

Embodiment 2

[0060] The preparation of compound (three):

[0061] The preparation process refers to the synthesis of compound (2) in Example 1; compound (3) can be prepared by replacing amantadine hydrochloride with memantine hydrochloride.

[0062] MS: m / z (ES): 549.2, 550.2 [M+1].

[0063] 1H NMR:

[0064] (400MHz,d6-DMSO):8.67(d,2H),8.27(d,1H),8.00(s,1H),7.86(s,1H),7.75(s,1H),7.51(s,1H), 7.47(d,1H),7.18~7.21(dd,1H),6.90(s,1H),6.51(d,1H),4.03(s,3H),2.10(s,1H),1.78(s,2H) ,1.60(s,4H),1.35(d,2H),1.28(d,2H),1.12(s,2H),0.83(s,6H).

Embodiment 3

[0066] Compound (two) preparation of hydrochloride:

[0067] Weigh 10 g of compound (2), add 300 ml of ethanol to dissolve it, add dropwise 10 ml of 15% hydrogen chloride ethanol solution, after the drop is completed, stir at room temperature for 2 hours, filter, wash the filter cake with ethanol, and dry in vacuo to obtain about 9 g of white solid.

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PUM

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Abstract

The invention discloses a tyrosine kinase inhibitor and application thereof. The structure of the tyrosine kinase inhibitor compound or pharmaceutically acceptable salt is as shown in formula (I); in the formula (I), R1, R3 and R4 are independently hydrogen, substituted or unsubstituted C1-4 alkyl, the substitution is substituted by at least one of the following groups: halogen, nitro, amino, cyano and phenyl, R2 is independently hydrogen, halogen, nitro, cyano, substituted or unsubstituted C1-2 alkyl, and substituted or unsubstituted C1-2 alkoxy, and the substitution is substituted by at least one of the following groups: halogen, nitro and phenyl; the tyrosine kinase inhibitor compound or the pharmaceutically acceptable salt exists in the form of a pharmaceutical composition in the practical application process, and the pharmaceutical composition further comprises a pharmaceutically acceptable carrier and / or auxiliary materials. The tyrosine kinase inhibitor and the application thereof can be used for preventing and treating tyrosine kinase mediated diseases, including thyroid cancer, renal cell carcinoma, liver cancer and the like, mainly HCC.

Description

technical field [0001] The invention relates to the technical field of medicines, and more to a tyrosine kinase inhibitor and its application in the prevention and treatment of tyrosine kinase-mediated diseases, specifically a tyrosine kinase inhibitor and its application. Background technique [0002] Liver cancer is the sixth leading cause of cancer worldwide and the fourth most common cause of cancer death. China is a big country with liver cancer. According to statistics, there are about 700,000 new liver cancer patients in the world every year, and China accounts for about half of them, about 360,000. [0003] Hepatocellular carcinoma (HCC) accounts for 75%-85% of all primary liver cancers, and it is a solid tumor with high vascular dependence. During the occurrence of HCC, abnormalities of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) can upregulate the RAS / MAPK pathway downstream, leading to increased angiogen...

Claims

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Application Information

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IPC IPC(8): C07D215/48A61K31/47A61P35/00
CPCC07D215/48A61P35/00
Inventor 王俊凯李雪徐燕戈丹妮石杨斌朱绪成韩光戚鑫
Owner 成都蓝蜻蜓生物技术有限公司
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