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Sulfhydryl benzimidazole derivative containing dihydrofuran-pyridine

A technology of alkyl and methyl, applied in the direction of medical preparations containing active ingredients, organic chemistry, drug combination, etc., can solve the problem of large individual differences in pharmacokinetics, affecting drug efficacy and pharmacokinetic parameters, and onset of effect Slow time etc.

Inactive 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, 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

Method used

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Examples

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Effect test

Embodiment 1

[0106] The preparation of embodiment 1 2-mercapto-benzimidazole

[0107] 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

[0108] Example 2 Preparation of 2-mercapto-5-methoxy-benzimidazole

[0109] 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

[0110] Example 3 Preparation of 2-mercapto-5-difluoromethoxy-benzimidazole

[0111] 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 hydrosulphonyl benzoglioxaline derivatives which are shown in general formula (I) and contain dihydrofuran 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 present invention belongs to the technical field of medicine, and specifically relates to mercaptobenzimidazole derivatives containing dihydrofuropyridine, its isomers and pharmaceutically acceptable salts 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] 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 t...

Claims

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Application Information

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IPC IPC(8): C07D491/04A61K31/4353A61P1/04
Inventor 黄振华
Owner SHANDONG XUANZHU PHARMA TECH CO LTD
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