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Benzimidazole derivative containing alkoxyl oxygen alkyl substituted pyridine-tetrahydrochysene isoxazole

An alkyl and ethoxy technology, applied in the field of medicine, can solve the problems of large individual differences in pharmacokinetics, slow onset time, affecting drug efficacy and pharmacokinetic parameters, 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

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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  • Benzimidazole derivative containing alkoxyl oxygen alkyl substituted pyridine-tetrahydrochysene isoxazole
  • Benzimidazole derivative containing alkoxyl oxygen alkyl substituted pyridine-tetrahydrochysene isoxazole
  • Benzimidazole derivative containing alkoxyl oxygen alkyl substituted pyridine-tetrahydrochysene isoxazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] The preparation of embodiment 1 2-mercapto-benzimidazole

[0103] 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, after the reaction is complete, cool 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

[0104] Example 2 Preparation of 2-mercapto-5-methoxy-benzimidazole

[0105] 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

[0106] Example 3 Preparation of 2-mercapto-5-difluoromethoxy-benzimidazole

[0107] 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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PUM

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Abstract

The invention belongs to the pharmaceutical technical field and specifically relates to benzoglioxaline derivatives which are shown in general formula (I) and contain naphthyridine tetrahydrochysene isoxazole substituted by alcoxyl alkyl, pharmaceutically acceptable salts and isomers thereof, wherein, 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 invention belongs to the technical field of medicine, and in particular relates to benzimidazole derivatives containing alkoxyalkyl-substituted pyrido-tetrahydroisoxazoles, pharmaceutically acceptable salts and isomers thereof, and the preparation methods of these compounds, including The pharmaceutical composition of these compounds, and the application of these compounds in the preparation of medicines for treating and / or preventing peptic ulcer. 2. Background technology [0002] Diseases of the digestive system are one of common frequently-occurring diseases, and the incidence of ulcer disease accounts for about 10% to 12% of the total population. The initial treatment is mainly to use antacids (such as sodium bicarbonate, aluminum hydroxide, etc.) to neutralize gastric acid to relieve symptoms. After the 1970s, with the H 2 The discovery of gastric acid secretion inhibitors such as receptor blockers and proton pump inhibitors has created a...

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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