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Tyrosine kinase inhibitor and medicinal application thereof in treating malignant tumor

A technology for malignant tumors and medicinal salts, applied in the field of tyrosine kinase inhibitor compounds, can solve problems such as liver toxicity and side effects of imatinib, and achieve the effects of less side effects, less dosage, and reduced oxidative metabolism

Inactive Publication Date: 2011-05-04
苏州康益明华生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, imatinib has side effects and has been shown to cause hepatotoxicity, as evidenced by elevated liver enzymes (ammoniatransferase, alkaline phosphatase)

Method used

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  • Tyrosine kinase inhibitor and medicinal application thereof in treating malignant tumor
  • Tyrosine kinase inhibitor and medicinal application thereof in treating malignant tumor
  • Tyrosine kinase inhibitor and medicinal application thereof in treating malignant tumor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] A tyrosine kinase inhibitor, the chemical name is: 1-trideuteromethyl-4-(4-(4-methyl-3-(4-(pyridine-3-ester) pyrimidine-2-ester amine) )phenylaminocarbonyl)-dideuteriobenzyl)-2,2,3,3,5,5,6,6-octadeutero-1-oxo-piperazine-6-methyl-N-1 -(4-(Pyridine-3-ester)pyrimidine-2-ester)benzene-1,3-diamine. Its structural formula is as follows:

[0018]

[0019] Above-mentioned compound can be prepared by following steps:

[0020] (1) At room temperature, add potassium carbonate to the stirred mixture of 2,6-piperazinedione, deuterium oxide and deuterated methanol, stir for 18 hours, concentrate to dryness, and dissolve the residue in ethyl acetate , washed successively with dilute hydrochloric acid (1M), saturated sodium bicarbonate solution, water and saturated brine, dried over anhydrous sodium sulfate, filtered and concentrated to obtain 3,3,5,5-tetradeuterium-2,6-piperazine di ketone.

[0021] (2), at room temperature, add deuterated methyl iodide to the stirred mixture o...

Embodiment 2

[0034] According to the tyrosine kinase inhibitor of this embodiment, the chemical name is: 4-((4-methoxy)-2,2,3,3,5,5,6,6-octadeutero-piperazine -1-ester)-dideuteromethyl)-N-(4-methyl-3-(4-(pyridine-3-ester)pyrimidine-2-esteramine)phenyl)benzamide. Its structural formula is as follows:

[0035]

[0036] Above-mentioned compound can be prepared by following steps:

[0037] (1), add m-chloroperoxybenzoic acid in the stirred mixed liquid of 4-trideuteromethyl-3,3,5,5-tetradeuterium-2,6-piperazinedione and dichloromethane, stir After the reaction, it was concentrated to dryness. The residue was dissolved in ethyl acetate and washed successively with dilute hydrochloric acid (1M), saturated sodium bicarbonate solution, water and saturated brine. Dry over anhydrous sodium sulfate, filter, and concentrate to give 4-hydroxy-3,3,5,5-tetradeuterium-2,6-piperazinedione (Intermediate 2-1).

[0038] (2) At room temperature, add methyl iodide to the stirred mixture of intermediate 2...

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Abstract

The invention relates to compounds capable of serving as tyrosine kinase inhibitors and medicinal application thereof in treating malignant tumor. Compared with the prior art, the oxidative metabolism of the compounds provided by the invention is reduced, and the medicinal power performance is improved; and moreover, the compounds have the advantages of less dosage and small side effects.

Description

technical field [0001] The invention relates to a tyrosine kinase inhibitor compound and its drug application in treating malignant tumors. Background technique [0002] Protein tyrosine kinase (PTK) activates downstream signaling proteins through phosphorylation, thereby regulating cellular responses. When signaling proteins are overactive, they cause abnormal cell growth and differentiation. Therefore, abnormal regulation of tyrosine kinases is closely related to the invasion and poor prognosis of many tumors, and is an important feature of malignant tumors. Tumor angiogenesis is the process of tumor forming new blood vessels on the original blood vessels, which plays a very important role in the growth, development and metastasis of tumors. The signals that promote angiogenesis are transduced through related tyrosine kinases on the surface of vascular endothelial cells. Therefore, blocking related signal transduction can effectively inhibit tumor angiogenesis, thereby ...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/506A61P35/00
Inventor 朱惠霖殷建明
Owner 苏州康益明华生物医药科技有限公司
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