Stable protein kinase activator, preparation method thereof and use

A protein kinase and activator technology, applied in the field of medicine, to achieve the effect of easy storage and transportation, and stable storage

Inactive Publication Date: 2010-07-21
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The current published literature only reports some salts of cyclic adenosine monophosphate. So far, there is no published literature at home and abroad for angina pectoris, heart failure, myocardial infarction, myocarditis, arrhythmia and cardiogenic shock, improving rheumatic N

Method used

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  • Stable protein kinase activator, preparation method thereof and use
  • Stable protein kinase activator, preparation method thereof and use
  • Stable protein kinase activator, preparation method thereof and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Example 1 Preparation of magnesium salt 8 hydrate of cyclic adenosine monophosphate In a 250ml three-necked flask, add cyclic adenosine monophosphate 0.1mol, water 100ml, stir, add 0.05mol magnesium oxide, stir at 20~60°C for 30~ Dissolve for 90 minutes, filter, add 1 to 5 times the amount of acetone to precipitate the solid, cool to -10 to 15°C, place it for 1 to 24 hours, filter, dry the solid at about 50°C for 2 to 4 hours to obtain off-white crystals Decomposition at 227°C (uncorrected), HPLC: cyclic adenosine monophosphate content 39.86%, water content measured by Karl Fischer method is 17.57%, thermal analysis: platform weight loss is about 17.16% (see attached figure 1 ), which is within the error range with the sample containing 8 crystal waters (theoretical value 17.48%). Elemental analysis theoretical value: C 29.12%, H4.64%, N16.98% P7.51%, Mg 2.95%; measured value: C 29.33%, H4.52%, N17.11% P7.67%, Mg 3.23 %.

Embodiment 2

[0073] Example 2 Preparation of cyclic adenosine monophosphate calcium salt 3.5 hydrate In a 250ml three-necked flask, add 0.1mol of purified cyclic adenosine monophosphate, 100ml of water, stir, add 0.05mol of calcium hydroxide or calcium oxide, 20 Stir for 30 to 90 minutes at ~60°C to dissolve, filter, add 1 to 5 times the amount of absolute ethanol and isopropanol (1:1), cool to -10 to 15°C, and place for 1 to 24 hours. The solid was precipitated, filtered, and dried at about 50°C for 4-6 hours to obtain 19.2 grams of off-white solid, melting point: 223°C decomposition (ELECTROTHERMAL MELTING POINT APPARATUS, uncorrected), infrared spectrum: the moisture content was 8.52% as determined by the Karl Fischer method, and the thermal Analysis: The weight loss of the platform is about 8.4%, which is within the error range with the result of the sample containing 3.5 crystal waters (theoretical value 8.30%); elemental analysis theoretical value: C 31.63%, H3.85%, N18.44% P8.16 %, ...

Embodiment 3

[0074]Example 3 Preparation of cyclic adenosine monophosphate meglumine monohydrate Put 10 g of purified cyclic adenosine monophosphate and equimolar meglumine into a reaction flask, add 200 ml of water, stir, and control the temperature between 10 and 60 ° C. For 10-120 minutes, add 1% of the total amount of the solution to the activated carbon and stir for half an hour to filter, then filter with a 0.22-micron microporous membrane or filter with an ultrafiltration membrane with a molecular weight cut-off of 6,000-30,000, and freeze it until -70~-30℃, keep it for about 24 hours, raise the temperature to about 20℃, dry it in vacuum, and then dry it at 20~30℃ for about 3~6 hours to get off-white crystalline powder, easily soluble in water, melting point: 67~ 71. ℃ (ELECTROTHERMAL MELTING POINT APPARATUS, uncorrected); HPLC: cyclic adenosine monophosphate content is 60.79%, ESI: m / z: 523; moisture (Karl Fischer method): 3.51%, thermal analysis: weight loss on the platform is abou...

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Abstract

The invention relates to a novel stable protein kinase activator adenosine cyclophosphate salt derivate, which has high storage stability and preparation performance and can be used in the preparation of medicaments for treating or preventing the following human and animal diseases such as stenocardia, cardiac failure, myocardial infarction, myocarditis, arrhythmia, cardiogenicshock, acute leukemia, nerve system diseases, respiratory system diseases, senile chronic bronchitis, hepatitis, psoriasis and the like and relieving the symptoms, such as cardiopalmus, shortness of breath, chest distress and the like of rheumatic heart disease.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to provide a novel and stable protein kinase activator-cyclic adenosine monophosphate hydrate and its preparation and application. Background technique [0002] The current published literature only reports certain salts of cyclic adenosine monophosphate. So far, there is no published literature at home and abroad for angina pectoris, heart failure, myocardial infarction, myocarditis, arrhythmia and cardiogenic shock, improving rheumatic Novel and stable protein kinase activator for symptoms such as heart palpitations, shortness of breath, chest tightness, acute leukemia, nervous system diseases, respiratory system diseases, hepatitis and psoriasis - cyclic adenosine monophosphate hydrate and its preparation method and uses. Contents of the invention [0003] What the present invention relates to is reported to be used for angina pectoris, heart failure, myocardial infarction, m...

Claims

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Application Information

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IPC IPC(8): C07H19/213C07H1/00A61K31/7076A61P9/10A61P9/04A61P9/06A61P9/00A61P35/02A61P25/00A61P11/00A61P1/16A61P17/06
CPCA61K31/7076C07H19/213A61P1/16A61P9/00A61P9/04A61P9/06A61P9/10A61P11/00A61P17/06A61P19/02A61P25/00A61P35/02
Inventor 刘力
Owner 刘力
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