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Thiazole derivatives

A drug and composition technology, applied in the direction of drug combination, metabolic disease, anti-drug, etc.

Inactive Publication Date: 2005-07-13
AVON PROD INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method has so far been of limited value in splitting AGE crosslinks formed in skin collagen (Yang 2000)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] This example describes the efficacy of the compounds of the present invention in inhibiting the formation of AGEs.

[0057] When incubated at 37°C, a control tube containing protein and sugar formed a gel with little or no residual liquid. This gel is a symbol of the large amount of cross-linking associated with saccharification. On the contrary, a treatment tube, which contains all the contents of the control tube plus the AGE inhibitor 2-amino-4,5-dimethylthiazole HCl, remains liquid, indicating 2-amino-4,5-dimethyl Thiazole HCl is an effective AGE inhibitor.

Embodiment 2

[0059] This example uses a sandwich enzyme-linked immunosorbent assay to illustrate the effect of the compound of the present invention in cleaving the cross-linked bonds associated with AGEs.

[0060]The mixture of protein and sugar is incubated to form cross-links representing AGEs and placed in a multi-well plate. The plates are then treated with 2-amino-4,5-dimethylthiazole HCl or buffer. After treatment, the plates are rinsed to remove any free protein released by the rupture of the cross-links. An antibody that reacts with the protein is then added to the plate to provide a quantitative level of protein in the plate.

[0061] The plate treated with 2-amino-4,5-dimethylthiazole HCl has less antibody bound to the plate than the control plate, indicating that 2-amino-4,5-dimethylthiazole HCl effectively splits Crosslinks related to saccharification.

Embodiment 3

[0063] This example describes the effect of the compounds of the present invention in inhibiting glucose oxidase.

[0064] In order to test the efficacy of 2-amino-4,5-dimethylthiazole HCl in inhibiting glucose oxidase, a commercially available glucose oxidase kit was used. The test showed that, compared with the control sample, in the sample containing 2-amino-4,5-dimethylthiazole HCl, H 2 O 2 The production of serotonin was reduced by more than 60%, indicating that 2-amino-4,5-dimethylthiazole HCl effectively inhibited glucose oxidase.

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PUM

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Abstract

Disclosed are methods of improving the appearance of skin by topical administration of thiazole derivatives that inhibit the formation of advanced glycation end products, cleave crosslinks associated with advanced glycation end products, and inhibit the function of glucose oxidase . Cosmetic and pharmaceutical compositions comprising said thiazole derivatives are also disclosed.

Description

Invention field [0001] The present invention generally relates to compositions and methods for improving the texture and elasticity of the skin. More specifically, the present invention relates to the application of thiazole derivatives in inhibiting the formation of advanced glycation end products, breaking the cross-linking bonds associated with advanced glycation end products, and inhibiting the function of glucose oxidase. Background of the invention [0002] The deterioration of skin appearance and texture with age is partly due to the accumulation of abnormal collagen and elastin in the skin. Due to the presence of advanced glycation end products ("AGEs"), these abnormal proteins have impaired functions. AGEs are cross-linked protein structures that change the chemical and mechanical properties of proteins such as collagen and elastin. The increase in age-related AGEs is related to the rigidity of skin fibers, leading to the deterioration of skin tone...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/20A61K8/49A61K31/426A61P3/10A61P9/10A61P17/00A61P19/02A61P25/00A61P25/28A61P29/00A61P39/02A61P43/00A61Q19/08C07D277/34C07D277/40C07D277/44C07D277/54C07D277/56
CPCA61K8/49A61K31/426A61Q19/08A61P3/10A61P9/10A61P13/12A61P17/00A61P19/02A61P25/00A61P25/28A61P29/00A61P39/00A61P39/02A61P43/00
Inventor M·D·海因斯B·C·琼斯
Owner AVON PROD INC
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