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Compound for treatment of severe pancreatitis and preparation method thereof

A compound and selected technology, applied in the field of medicine, can solve the problems of poor solubility of emodin and affecting drug efficacy, etc.

Inactive Publication Date: 2017-07-04
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the poor solubility of emodin affects its efficacy

Method used

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  • Compound for treatment of severe pancreatitis and preparation method thereof
  • Compound for treatment of severe pancreatitis and preparation method thereof
  • Compound for treatment of severe pancreatitis and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: 1-{2-(3,7-Dimethyl-5-oxo-5H-thiazolo[3,2-a]pyrimidin-6-yl)-2-oxoethyl)-3 -(pyridin-2-yl)urea (compound 1)

[0040]

[0041] Step 1) Add polyphosphoric acid (20.0 g, 183.0 mmol) into a three-necked flask equipped with a condenser, a thermometer and a nitrogen outlet. The flask was heated to about 70°C to obtain an easily stirred liquid. With stirring, 4-methyl-1,3-thiazol-2-amine (4.0 g, 35.0 mmol) was added in small portions. The temperature of the solution was slowly increased to 78°C while stirring. Then, ethyl acetoacetate (4.9 g, 42.0 mmol) was slowly dropped in through the dropping funnel, and the mixture was heated to 110° C. under nitrogen, and reacted for 6 hours. The reaction mixture was cooled, and water (40 mL) and ethyl acetate (100 mL) were added. The mixture was stirred until all solids were dissolved. Separate the organic layer, extract the aqueous layer with ethyl acetate, and combine the organic layers, and wash the organic layer with...

Embodiment 2

[0047] Example 2: 1-{2-(7-fluoromethyl-3-methyl-5-oxo-5H-oxazolo[3,2-a]pyrimidin-6-yl)-2-oxoethyl base)-3-(quinolin-2-yl)urea (compound 2)

[0048]

[0049] According to the method of Example 1, replace 4-methyl-1,3-thiazol-2-amine with 4-methyl-1,3-oxazol-2-amine, and use 4-fluoro-3-oxobutanoic acid Ethyl acetoacetate was replaced by ethyl acetoacetate, and 1-(pyridin-2-yl)urea was replaced by 1-(quinolin-2-yl)urea to give a light yellow solid with a total yield of 48%, ESI-MS: 410.12 [M +H] + .

Embodiment 3

[0050] Example 3: 1-{2-(7-cyclopropyl-3-methyl-5-oxo-5H-thiazolo[3,2-a]pyrimidin-6-yl)-2-oxoethyl )-3-(piperidin-4-yl)urea (compound 3)

[0051]

[0052] According to the method of Example 1, replace ethyl acetoacetate with ethyl 4-cyclopropyl-3-oxobutanoate, replace 1-(pyridin-2-yl) with 1-(piperidin-4-yl)urea Urea, a light yellow solid was obtained, the total yield was 55%, ESI-MS: 390.15[M+H] + .

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PUM

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Abstract

The invention relates to the field of medicines for treatment of severe pancreatitis, and provides a thiazolopyrimidine or oxazolopyrimidine derivative or a pharmaceutically acceptable salt thereof. In-vivo drug tests show that the compound has significant intestinal barrier function protection effect in the course of severe pancreatitis, and can be used for treating severe pancreatitis. The invention also provides a preparation method of the compound or the pharmaceutically acceptable salt thereof, a pharmaceutical composition, and an application of the compound or the pharmaceutically acceptable salt thereof in preparation of medicines for treatment of severe pancreatitis.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a compound for treating severe pancreatitis and a preparation method thereof. Background technique [0002] Severe pancreatitis is also called acute hemorrhagic necrotizing pancreatitis. The incidence rate accounts for about 10% of all pancreatitis. The mortality rate of severe pancreatitis reported abroad is generally between 30% and 50%, and the domestic report is mostly around 50%. Severe pancreatitis is often complicated by multiple organ failure (MSOF), how to prevent and treat MSOF is an important problem that must be solved in the treatment of severe pancreatitis. Intestinal barrier dysfunction, secondary intestinal flora and endotoxin translocation are important links in triggering systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS) and MSOF. [0003] There are some drugs for treating severe pancreatitis in the prior art. For ex...

Claims

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Application Information

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IPC IPC(8): C07D513/04C07D498/04A61K31/519A61P1/18
Inventor 张瑶崔轮盟杨蕊马晶郑庆霞杨白婧周辉华
Owner MUDANJIANG MEDICAL UNIV