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Helicobacter pylori eradicating agent having inhibitory activity on gastric acid secretion

A Helicobacter pylori, general formula technology, applied in the direction of anti-inflammatory agents, antibacterial drugs, organic active ingredients, etc., can solve the problems of unconfirmed effectiveness and difficulty in exerting antibacterial activity, and achieve excellent anti-Helicobacter pylori and gastric acid inhibition secretion effect

Inactive Publication Date: 2009-10-07
LINK GENOMICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its effectiveness could not be confirmed in a H. pylori infection model in gerbils that mirrors H. pylori infection in humans, so development was abandoned
[0007] As mentioned above, although many efforts have been made, triple therapy is still widely used to eradicate Helicobacter pylori
The reason is that proton pump inhibitors such as omeprazole, lansoprazole, rabeprazole, and clarithromycin are extremely unstable to acid, and it is difficult for amoxicillin to exert antibacterial activity under acidic conditions.

Method used

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  • Helicobacter pylori eradicating agent having inhibitory activity on gastric acid secretion
  • Helicobacter pylori eradicating agent having inhibitory activity on gastric acid secretion
  • Helicobacter pylori eradicating agent having inhibitory activity on gastric acid secretion

Examples

Experimental program
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Effect test

Synthetic example 1

[0108] Synthesis Example 1: Preparation of 4-methoxy-2,3-lutidine-1-oxide

[0109] Dilute 41.6g (2.0 equivalents) of 28% sodium methoxide aqueous solution with 200ml of dimethyl sulfoxide, and add dropwise 17.0g of 4-chloro-2,3-lutidine-1-oxide dissolved in di solution after methylsulfoxide (70ml). After reacting at 40° C. to 50° C. for 3 hours, it was left to stand overnight at room temperature. 15ml of water was added to the reaction solution, and concentrated to obtain a black syrupy residue; then, after dissolving in 500ml of water, the aqueous solution was extracted three times with 670ml of chloroform. The extract was dried over anhydrous magnesium sulfate and then concentrated to dryness under reduced pressure to obtain 37.2 g of 4-methoxy-2,3-lutidine-1-oxide.

Synthetic example 2

[0110] Synthesis Example 2: Preparation of 2-acetoxymethyl-3-methyl-4-methoxy-pyridine

[0111] Add 55.0 g (5.0 equivalents) of acetic anhydride to 37.2 g of 4-methoxy-2,3-lutidine-1-oxide, and react at 90°C to 100°C for 3 hours. The concentrated residue obtained after distilling off acetic anhydride was purified with a silica gel column to obtain 15.8 g of oily 2-acetoxymethyl-3-methyl-4-methoxy-pyridine.

Synthetic example 3

[0112] Synthesis Example 3: Preparation of 2-hydroxymethyl-3-methyl-4-methoxy-pyridine

[0113] In 25% aqueous sodium hydroxide solution, 15.8 g of 2-acetoxymethyl-3-methyl-4-methoxy-pyridine was added dropwise, and after reacting at room temperature for 1 hour, it was diluted with toluene, and then the toluene phase was washed with water, After drying over anhydrous magnesium sulfate, it was concentrated to dryness to obtain 5.7 g of oily 2-hydroxymethyl-3-methyl-4-methoxy-pyridine.

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Abstract

The invention provides a compound which is stable in an acid, has an antibacterial effect against a bacterium Helicobacter pylori, can exert a satisfactory level of an antibacterial effect when used singly, does not affect an enteric bacterium, has an antibacterial effect against a bacterium resistant to an antibacterial agent, and has an inhibitory effect on gastric acid secretion; and a pharmaceutical composition comprising the compound. Specifically disclosed are: a compound represented by the general formula (I) or a salt thereof; and a pharmaceutical composition comprising the compound or the salt thereof. (I) wherein R represents a linear alkyl group having 4 to 8 carbon atoms, preferably 5 to 7 carbon atoms.

Description

technical field [0001] The invention relates to a Helicobacter pylori sterilizing agent which has an excellent function of inhibiting gastric acid secretion. Background technique [0002] Gastritis, gastric ulcer, and duodenal ulcer are diseases that are complicated and intertwined with factors such as stress, genetic factors, and living habits. In recent years, Helicobacter pylori (H. pylori), which is one of the main causes of disease, has been attracting attention. Since Warren and Marshall successfully isolated and cultured spiral-shaped bacteria from gastric biopsy specimens in 1983, the relationship between gastritis, gastric ulcer, duodenal ulcer and gastric cancer and the bacteria has been actively studied. As a result, it was reported that the infection rate of Helicobacter pylori was about 83% in chronic gastritis, about 69% in gastric ulcer, about 4% in healthy stomach, and about 69% in duodenal ulcer. It has a high infection rate of about 92%, and about 51% in ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P1/00A61P1/04A61P1/18A61P31/04
CPCC07D401/12A61P1/00A61P1/04A61P1/18A61P29/00A61P31/00A61P31/04A61P35/00A61K31/4439
Inventor 伊藤正春山本雅一
Owner LINK GENOMICS
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