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Use of an aureolysin inhibitor for the treatment of inflammatory skin conditions characterised by colonisation with staphylococcus aureus

A technology of metalloprotease and staphylococcus, which is applied in the direction of skin diseases, antibacterial drugs, organic active ingredients, etc., and can solve the problems of no effect, no limited cutting, etc.

Inactive Publication Date: 2009-01-28
SERENTIS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Thus, they indirectly indicate that MMPs cleave CD154, but they do not define which metalloprotease cleaves CD154
The specification al

Method used

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  • Use of an aureolysin inhibitor for the treatment of inflammatory skin conditions characterised by colonisation with staphylococcus aureus
  • Use of an aureolysin inhibitor for the treatment of inflammatory skin conditions characterised by colonisation with staphylococcus aureus
  • Use of an aureolysin inhibitor for the treatment of inflammatory skin conditions characterised by colonisation with staphylococcus aureus

Examples

Experimental program
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Embodiment

[0096] Synthetic example

[0097] 1. Synthesis of compounds 11 and 12

[0098] Two interchangeable synthetic routes were used to generate compounds 11 and 12. The first is, for example, the synthesis of compound 11 from (R)-2-(2-methoxy-2-oxyethyl)-4-methylpentanoic acid. The second is, for example, the synthesis of compound 12 from L-leucine. The first route can be used to synthesize compound 12 by using (S)-2-(2-methoxy-2-oxyethyl)-4-methylvaleric acid, and the second route can be used to synthesize compound 12 by using D-leucine instead of Compound 11 was synthesized from L-leucine.

[0099] A.(R)-N1-((S)-3,3-Dimethyl-1-(methylamino)-1-oxobutan-2-yl)-N4-hydroxy-2-isobutyl Synthesis of Succinamide (Compound 11)

[0100] i) (R)-2-(2-Methoxy-2-oxoethyl)-4-methylpentanoic acid (0.5g, 2.4mmol), DCC (1.2eq, 0.61g) and HOBT were stirred at room temperature (1.02eq, 0.34g) in dichloromethane (5ml) for 10 minutes. (S)-2-Amino-N,3,3-trimethylbutanamide (1.1 eq, 0.39 g) was add...

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Abstract

There is provided, inter alia, a method for the treatment or prevention of an inflammatory skin condition which is characterised by colonisation with Staphylococcus aureus, comprising the topical administration of an aureolysin inhibitor.

Description

technical field [0001] The present invention relates to the treatment of inflammatory skin diseases characterized by Staphylococcus aureus colonization. Background technique [0002] Atopic dermatitis (AD), sometimes called eczema, is a chronic relapsing disease characterized by itching, erythema, dry skin, and inflammation. [0003] Although excessive T cell activation in response to antigen stimulation and overstimulation of T cells by atopic Langerhans cells are considered important factors, the pathogenesis of AD is not fully understood. The level of IgE production is closely related to the severity of the disease, and although allergen-specific IgE can be observed in many patients, it is unclear whether this finding marks sensitization to a specific allergen. [0004] The prevalence of the disease varies widely, but is estimated to be as high as 20% of children in some Western countries. AD is common in families with a history of atopic disease (asthma, allergic rhini...

Claims

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Application Information

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IPC IPC(8): C07C259/06A61K31/00A61K31/4035A61K31/16A61K31/4402A61K31/7056G01N33/50G01N33/68A61P17/00A61P31/04
Inventor 盖伊·蒂莫西·莱顿史蒂芬·鲁珀特·钱德勒
Owner SERENTIS LTD