A kind of β-cytidine nucleoside-5'-arginine triphosphate derivative ester and its preparation method and application

A technology of arginine triphosphate and cytidine nucleoside, which is applied to the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., and can solve problems such as mental disorders, family and social burdens, and difficulties in treatment and care

Active Publication Date: 2011-12-07
HAINAN HUALON PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

These patients not only suffer from limb paralysis and language dysfunction, but also have mental abnormalities. Treatment and care are difficult, and they impose a heavy burden on families and society.

Method used

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  • A kind of β-cytidine nucleoside-5'-arginine triphosphate derivative ester and its preparation method and application
  • A kind of β-cytidine nucleoside-5'-arginine triphosphate derivative ester and its preparation method and application
  • A kind of β-cytidine nucleoside-5'-arginine triphosphate derivative ester and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The ultraviolet analysis of embodiment 1-beta-cytidine-5'-arginine triphosphate

[0043] Adopt ultraviolet-visible spectrophotometry to analyze and measure the above-mentioned compounds, take compound 1 to prepare the test solution, and there is maximum absorption at the wavelength of 280 ± 2nm;

[0044] Table 1: Maximum absorption wavelength position and absorbance ratio range:

[0045]

[0046] Take compound 2 to prepare the test solution, which has maximum absorption at the wavelength of 250 ± 2nm;

[0047] Table 2: Maximum absorption wavelength position and absorbance ratio range:

[0048]

[0049]

Embodiment 2

[0050] The HPLC analysis of embodiment 2-beta-cytidine-5'-arginine triphosphate:

[0051] The detection wavelength is 280nm, the mobile phase is 0.02mol / L phosphate buffer: methanol (75:25), the number of theoretical plates is not less than 2000, the resolution is greater than 1.5, the flow rate is 1.0ml / mim, and the running time is 20 minutes , the injection volume was 10 μl / time, and each operation was equilibrated at intervals of 10 minutes.

[0052] Table 1: Retention times of Compound 1

[0053]

[0054]The detection wavelength of the ultraviolet detector is 272nm, the chromatographic column adopts C18, 3.9×150mmID, the particle size of 4μm, with 0.02mol / L phosphate buffer: methanol (75:25) as the mobile phase, the number of theoretical plates is not less than 2000, the resolution is greater than 1.5, the flow rate is 1.00ml / mim, the running time is 35 minutes, the injection volume is 10μl / time, the column temperature is controlled at 25°C, and the interval between ea...

Embodiment 3

[0057] Example 3-Pharmacology of β-cytidine-5'-arginine triphosphate

[0058] β-cytidine nucleoside-5'-arginine triphosphate can promote the synthesis and metabolism of phospholipids, fats, nucleic acids and proteins in cells, regulate the synthesis and reconstruction of cell biofilm structures, enhance the activity and regeneration of vascular cells and Repair ability, improve cell resistance to damage, promote the substance and energy metabolism of nerve cells, support the survival of neurons, delay the aging of nerve cells and hardening of blood vessels, and can pass through the blood-brain barrier and directly enter the nerve cells, affecting the respiratory chain, Improve brain cell ischemia and hypoxia.

[0059] It is used to treat nervous system diseases and vascular sclerosis caused by various reasons. Cytidine-5”-cytidine triphosphate, which participates in the synthesis and construction of the body’s membrane structure, can be catabolized into cytidine monophosphate ...

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Abstract

The invention belongs to the field of pharmaceutical chemistry and specially relates to a gamma-cytidine-5 '-triphosphoarginine derivative ester, the preparation method and the application for the same. The invention also provides a preparation method of the gamma-cytidine-5 '-triphosphoarginine derivative ester, and functions of the gamma-cytidine-5 '-triphosphoarginine derivative ester in reversion of an acute cerebral infarction-caused disease process that brain cells are transformed from an ischemia state to a necrosis state, and treatment and improvement of brain cells.

Description

【Technical field】 [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a β-cytidine-5'-arginine triphosphate; the invention also provides a synthesis method of this type of compound and its role in the treatment of acute cerebral infarction-induced reversal The pathological process of brain cells from ischemia to necrosis can be used to treat and improve the function of brain cells. 【Background technique】 [0002] The compounds of the present invention relate to the main diseases as follows; [0003] 1. Ischemic brain disease [0004] Cerebrovascular diseases are brain diseases caused by various cerebrovascular diseases. According to the pathological nature, it can be divided into ischemic stroke and hemorrhagic stroke. The former is also called cerebral infarction. In addition, vascular dementia (VD) and vascular mild cognitive impairment (VaMCI) also belong to cerebrovascular stroke. category of disease. [0005] Acute cerebral...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/10C07H1/00A61K31/7064A61P9/00A61P9/10A61P25/28
Inventor 宁辉
Owner HAINAN HUALON PHARM
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