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Compound containing alcoxyl acetyl dihydrogen isoxazole-pyridine

A compound, ethyl technology, applied in the field of medicine, can solve problems affecting drug efficacy and pharmacokinetic parameters, insufficient drug effect, slow onset time, etc.

Active Publication Date: 2009-07-29
SHANDONG XUANZHU PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, this type of drug has a slow onset time and is not strong enough. It takes several doses (and a few days later) to achieve the maximum acid-suppressing effect, and it may not be able to stably suppress acid for 24 hours. The time of taking the drug and eating may affect the drug. Pharmacokinetic parameters, individual differences in pharmacokinetics, and significant interactions with other drugs

Method used

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  • Compound containing alcoxyl acetyl dihydrogen isoxazole-pyridine
  • Compound containing alcoxyl acetyl dihydrogen isoxazole-pyridine
  • Compound containing alcoxyl acetyl dihydrogen isoxazole-pyridine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0103] The preparation of embodiment 1 2-mercapto-benzimidazole

[0104] Put 6.5g (60mmol) of phthalic diamine into the reaction flask, add 200ml of 95% ethanol solution, then add 12.8g (80mmol) of potassium ethoxysulfonate, heat and reflux at 80°C for 4h. To room temperature, pour the reaction solution into 200ml of ice water, stir evenly, adjust the pH to 3-4 with 4N hydrochloric acid, precipitate a solid, filter, wash with water until neutral, and vacuum-dry the filter cake to obtain 7.2g of the product, yield: 79.7% .

Embodiment 2

[0105] Example 2 Preparation of 2-mercapto-5-methoxy-benzimidazole

[0106] Preparation method Referring to Example 1, 8.3 g (60 mmol) of 4-methoxy o-phenylenediamine and 12.8 g (80 mmol) of potassium ethoxysulfonate were added to obtain 8.2 g of the product, yield: 75.4%.

Embodiment 3

[0107] Example 3 Preparation of 2-mercapto-5-difluoromethoxy-benzimidazole

[0108] Preparation method Referring to Example 1, 10.4 g (60 mmol) of 4-difluoromethoxy o-phenylenediamine and 12.8 g (80 mmol) of potassium ethoxysulfonate were added to obtain 9.5 g of the product, yield: 73.5%.

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Abstract

The invention belongs to the pharmaceutical technical field and specifically relates to dihydro isoxazole pyridine derivatives which are shown in general formula (I) and contain alcoxyl acetyl, pharmaceutically acceptable salts and isomers thereof, wherein, R, R, R and R are defined as in the specification. The invention also relates to preparation methods of the compounds, drug compositions containing the compounds and the application of the compounds in preparing drugs for preventing and / or treating digestive ulcer.

Description

1. Technical field [0001] The present invention belongs to the technical field of medicine, and specifically relates to alkoxyacetyl dihydroisoxazolopyridine compounds, pharmaceutically acceptable salts and isomers thereof, preparation methods of these compounds, pharmaceutical compositions containing these compounds, And the application of these compounds in the preparation of medicines for treating and / or preventing peptic ulcer. 2. Background technology [0002] Peptic ulcers are caused by ulceration of the gastrointestinal mucosa. These ulcers expose the bottom layer of the lining of the digestive tract to the acidic secretions of the stomach and pepsin. Cell autolysis occurs when there is an imbalance between the intestinal control). It is generally believed that peptic ulcer is caused by this autolysis. [0003] Peptic ulcer is one of the common frequently-occurring diseases, and the incidence of ulcer disease accounts for about 10% to 12% of the total population. ...

Claims

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Application Information

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IPC IPC(8): C07D498/04A61K31/437A61P1/04
Inventor 黄振华
Owner SHANDONG XUANZHU PHARMA TECH CO LTD
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