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2-arylthiazole derivative and medicinal salt and application thereof

A technology of arylthiazole and derivatives, applied in the field of 2-arylthiazole derivatives, can solve the problems affecting the bioavailability of febuxostat, etc., achieve high effective bioavailability, less side effects, and reduce the concentration of uric acid

Inactive Publication Date: 2012-08-22
苏州波锐生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, febuxostat will undergo severe oxidative metabolism (the main metabolites are 67M-1, 67M-2, 67M-4) and acyl glucuronidation metabolism (22% to 44%) in the human body, thus affecting the effect of febuxostat. Sutent Bioavailability

Method used

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  • 2-arylthiazole derivative and medicinal salt and application thereof
  • 2-arylthiazole derivative and medicinal salt and application thereof
  • 2-arylthiazole derivative and medicinal salt and application thereof

Examples

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Embodiment 1

[0029] The present embodiment provides a compound represented by formula (II):

[0030]

Embodiment 2

[0032] The present embodiment provides a compound represented by formula (III):

[0033]

Embodiment 3

[0035] The present embodiment provides a compound represented by formula (IV):

[0036]

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Abstract

The invention relates to a novel 2-arylthiazole derivative and medicinal salts thereof, and an application in the preparation of medicaments for preventing and / or treating gout. The compound of the invention is an ideal selective xanthine oxidoreductase inhibitor, is applicable to the treatment and prevention of various indications associated with uric acid synthesis in the body, and is especially applicable to the treatment of gout. The compound has reduced oxidative metabolism and acyl glucuronidation metabolism, reduced first-pass effect, higher effective bioavailability, and less side effect due to its low using amount.

Description

technical field [0001] The present invention relates to 2-arylthiazole derivatives, their pharmaceutically acceptable salts and their use in the preparation of medicaments for preventing and / or treating gout. Background technique [0002] Gout, also known as metabolic arthritis, is a kind of sudden inflammation caused by the accumulation of uric acid in the body due to purine metabolism disorder, which leads to the deposition of urate crystals in joints and surrounding tissues. Acute arthritis. When the uric acid concentration in the blood reaches saturation, it can eventually induce the release of uric acid crystals accumulated in soft tissues such as joint membranes or tendons, causing the body's immune system to become allergic and cause inflammation. [0003] Gout is a global metabolic disease, and its prevalence is affected by various factors such as economic development, environment, eating habits, race, genetics, medical level, and diagnostic criteria. The prevalenc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/56C07D417/12A61K31/427A61K31/426A61P19/06
Inventor 殷建明朱惠霖
Owner 苏州波锐生物医药科技有限公司
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