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Use of an antibacterial agent for the treatment of an epithelial-related condition

一种用途、病况的技术，应用在抗细菌剂用于治疗上皮相关病况的用途领域

Active Publication Date: 2016-01-06
SIGNUM BIOSCIENCES INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the emergence of bacterial resistance to commonly used antibiotics poses an increasing challenge to the treatment, prevention and containment of epithelial-associated conditions caused or aggravated by bacteria

Method used

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  • Use of an antibacterial agent for the treatment of an epithelial-related condition
  • Use of an antibacterial agent for the treatment of an epithelial-related condition
  • Use of an antibacterial agent for the treatment of an epithelial-related condition

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0354]

[0355] (4-((R)-1-carboxy-2-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienylthio)ethylamino)- Synthesis of 4-oxobutanoic acid) (Compound B): To a solution of S-trans,trans-farnesyl-L-cysteine ​​(500 mg, 1.54 mmol) in THF was added the first copies of K 2 CO 3 (2 mmol) and the resulting solution was cooled to 5°C while stirring vigorously. To this stirred solution was added succinic anhydride (308 mg, 3.1 mmol) dropwise while utilizing another portion of K 2 CO 3 (4 mmol) to maintain the pH at 9.0-10.0. The mixture was stirred at room temperature for 2 h, HPLC analysis showed the reaction was complete. The pH of the reaction mixture was then adjusted to 2.0 by adding 2N HCl solution. The acidic solution was extracted 3 times with 10 mL of ethyl acetate. The combined organic extracts were washed with water, brine and washed with Na 2 SO 4 Drying and removal of solvent on a rotary evaporator afforded crude compound B, which was further purified by preparative HP...

example 2

[0357]

[0358] ((E)-4-((R)-1-carboxy-2-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienylthio)ethyl Synthesis of S-trans,trans-farnesyl-L-cysteine ​​(500mg, 1.54mmol) in THF and the first part of K 2 CO 3 (3 mmol) was cooled to 5°C. To this stirred solution was added maleic anhydride (302mg, 3.07mmol) portionwise while utilizing another portion of K 2 CO 3 (3 mmol) to maintain the pH at 9.0-10.0. The mixture was stirred at room temperature for 3 h, HPLC analysis showed the reaction was complete. The pH of the reaction mixture was then adjusted to 2.0 by adding 2N HCl solution. The acidic solution was extracted 3 times with 15 mL of ethyl acetate. The combined organic extracts were washed with water, brine and washed with Na 2 SO 4 Drying and then concentration afforded crude Compound A, which was further purified by preparative HPLC (552 mg, 85%) to yield Compound A. 1 H-NMR (500MHz, CD 3 OD): δ1.50 (bs, 6H), 1.57 (s, 3H), 1.59 (s, 3H), 1.85-2.10 (m, 8H), 2.68 (dd, ...

example 3

[0360]

[0361] ((R)-2-((S)-2-Acetamido-3-hydroxypropionylamino)-3-((2E,6E)-3,7,11-trimethyldodeca-2,6, 10-trienylthio)propionic acid) and ((R)-2-((R)-2-acetylamino-3-hydroxypropionylamino)-3-((2E,6E)-3,7, 11-Trimethyldodeca-2,6,10-trienylthio)propionic acid)) Synthesis of a mixture (compound D): In a 100 mL round bottom flask, N-acetyl-L-serine ( 1.0mmol), coupling reagent (520mgPBOP or 380mgHATU, 1mmol) and N, N-diisopropyl-ethylamine (650mg, 5mmol) were mixed in CH 2 Cl 2 (10mL). The reaction mixture was stirred at room temperature for 30 minutes. S-trans,trans-farnesyl-L-cysteine ​​(325 mg, 1 mmol) was added to the reaction mixture and stirred overnight at room temperature. CH removal by rotary evaporation 2 Cl 2 . The resulting residue was dissolved in ethyl acetate (50 mL). use NH 4 Cl saturated solution (50mL) washed the organic solution, washed with Na 2 SO 4 Dried and concentrated to obtain a crude mixture. The crude mixture was purified by preparative ...

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Abstract

Disclosed herein are methods of inactivating and / or decolonizing bacteria on a surface. The present invention also discloses methods of treating epithelial conditions caused or aggravated by bacteria, such as acne vulgaris, in an individual in need thereof. The invention additionally discloses compounds and compositions of the invention which exhibit antibacterial and / or anti-inflammatory effects.

Description

[0001] Related Application Cross Reference [0002] This application claims priority to US Provisional Application Serial No. 61 / 260,401, filed November 12, 2009, the entire contents of which are incorporated herein by reference. technical field Background technique [0003] Dermatologists are well aware of the difficulties associated with the treatment of conditions associated with bacterial colonization of mammalian epithelium. This is especially true in the context of skin and wound antimicrobials, where the most effective treatment of epithelial conditions caused or aggravated by bacterial colonization often involves the use of topical antibacterial agents. However, the emergence of bacterial resistance to commonly used antibiotics poses an increasing challenge to the treatment, prevention and containment of epithelial-related conditions caused or aggravated by bacteria. There is a clear and urgent need in the industry for novel and cost-effective methods for the effec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/165A61P17/10
CPCA61K31/165A61K31/198A61K31/341A61K31/381A61K31/4045A61K31/5375A61K38/05A61P1/02A61P1/04A61P9/00A61P11/00A61P11/02A61P11/14A61P13/00A61P13/02A61P15/00A61P15/02A61P17/00A61P17/02A61P17/04A61P17/06A61P17/08A61P17/10A61P21/00A61P27/02A61P27/16A61P29/00A61P31/00A61P31/04A61P31/06A61P35/00A61P37/08Y02A50/30A61K9/0014A61K9/007
Inventor 杰弗里·B·斯托克马克斯韦尔·斯托克
Owner SIGNUM BIOSCIENCES INC
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