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Novel pyridine-imidazole derivative

A technology of pyridine and lutidine, which is applied in the field of medicine, can solve the problems of large individual differences in pharmacokinetics, slow onset time, influence on drug efficacy and pharmacokinetic parameters, 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

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Example 1 Preparation of 2-mercapto-5-methoxy-6-chloro-imidazo[4,5-b]pyridine

[0107] Put 10.4g (60mmol) of 2,3-diamino-5-chloro-6-methoxypyridine into the reaction flask, add 200ml of 95% ethanol solution, and then add 12.8g (80mmol) of potassium ethoxysulfonate , Heated to 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 to 4 with 4N hydrochloric acid, precipitate a solid, filter, wash with water until neutral, and vacuum-dry the filter cake to obtain 9.5g of the product. Rate: 73.2%.

Embodiment 2

[0108] Example 2 Preparation of 2-mercapto-5-methoxy-6-fluoro-imidazo[4,5-b]pyridine

[0109] Preparation method Referring to Example 1, 9.4 g (60 mmol) of 2,3-diamino-5-fluoro-6-methoxypyridine and 12.8 g (80 mmol) of potassium ethoxysulfonate were administered. 9.1 g of the product was obtained, yield: 76.0%.

Embodiment 3

[0110] Example 3 Preparation of 2-mercapto-5-methoxy-6-bromo-imidazo[4,5-b]pyridine

[0111] Preparation method Referring to Example 1, 13.1 g (60 mmol) of 2,3-diamino-5-bromo-6-methoxypyridine and 12.8 g (80 mmol) of potassium ethoxysulfonate were administered. 10.9 g of the product was obtained, yield: 69.8%.

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Abstract

The invention belongs to the pharmaceutical technical field and specifically relates to new naphthyridine imidazole derivatives which are shown in general formula (I), acceptable salts in pharmacy and isomers thereof, wherein, R, 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 new pyridoimidazole derivatives, pharmaceutically acceptable salts and isomers thereof, preparation methods of these compounds, pharmaceutical compositions containing these compounds, and preparation of these compounds for preventing And / or the application in the medicine of treating 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 have the charact...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/437A61P1/04
Inventor 黄振华
Owner SHANDONG XUANZHU PHARMA TECH CO LTD
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