Benzimidazole derivative containing isoxazole-pyridine

A compound and isomer technology, applied in the application field of benzimidazole derivatives and drugs, can solve the problems of affecting drug efficacy and pharmacokinetic parameters, insufficient drug effect, large individual differences in pharmacokinetics, 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

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 new era of peptic ulcer treatment. These drugs have the characteristics of quick effect and high ulcer healing rate, which greatly reduces the surgical operation rate
However, the onset time of these drugs is slow, and the drug effect is not strong enough. It takes several doses (that is, a few days) 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 effect of the drug. Pharmacokinetic parameters, individual differences in pharmacokinetics, and significant interactions with other drugs
[0004] Patent WO1997000875 discloses a compound with the following structure, although the acid suppression effect has been improved, but it has not reached a satisfactory level

Method used

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  • Benzimidazole derivative containing isoxazole-pyridine
  • Benzimidazole derivative containing isoxazole-pyridine
  • Benzimidazole derivative containing isoxazole-pyridine

Examples

Experimental program
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Effect test

Embodiment 1

[0104] The preparation of embodiment 1 2-mercapto-benzimidazole

[0105] 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, and heat to reflux at 80°C for 4h. After the reaction was completed, 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. Rate: 79.7%.

Embodiment 2

[0106] Example 2 Preparation of 2-mercapto-5-methoxy-benzimidazole

[0107] 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 cast. 8.2 g of the product was obtained, yield: 75.4%.

Embodiment 3

[0108] Example 3 Preparation of 2-mercapto-5-difluoromethoxy-benzimidazole

[0109] 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 injected. 9.5 g of the product was obtained, yield: 73.5%.

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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 isoxazole pyridine, 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 invention belongs to the technical field of medicine, and in particular relates to benzimidazole derivatives containing isoxazolopyridine, pharmaceutically acceptable salts and isomers thereof, methods for preparing 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] 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 new era of peptic ulcer treatment. These drugs ...

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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