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Antibacterial molecules for the treatment of multidrug-resistant and extensively drug-resistant strains of mycobacteria

一种分枝杆菌、结核分枝杆菌的技术，应用在抗细菌药、应用、医药配方等方向，能够解决难以管理依从性、疾病进展危险、限制有效性等问题

Inactive Publication Date: 2011-12-21
POLYMEDIX
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Several anti-infective drugs have been established to combat tuberculosis and other tuberculosis-causing microorganisms; however, the emergence of multidrug-resistant (MDR) and extensively drug-resistant (XDR) organisms has severely limited their effectiveness
The current treatment strategy for active disease is polydrug therapy for 6 to 9 months; adherence to this regimen is difficult to manage, exacerbating the development of drug resistance
In addition, many anti-TB drugs interfere with HIV treatment, which spirals in the risk and severity of disease progression in co-infected individuals

Method used

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  • Antibacterial molecules for the treatment of multidrug-resistant and extensively drug-resistant strains of mycobacteria
  • Antibacterial molecules for the treatment of multidrug-resistant and extensively drug-resistant strains of mycobacteria
  • Antibacterial molecules for the treatment of multidrug-resistant and extensively drug-resistant strains of mycobacteria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0126] Example 1: Sensitivity test to Mycobacterium tuberculosis (H37Rv strain strain) and cytotoxicity test to monkey VERO cells (practical example)

[0127] In order to evaluate the effect of compounds formulas I, II and III on inhibiting the growth of Mycobacterium tuberculosis species, the sensitivity test of some compounds to Mycobacterium tuberculosis (H37Rv strain) and the cytotoxicity test of some compounds to monkey VERO cells were carried out.

[0128] Use the microplate alamar blue assay (MABA) to carry out the antimicrobial screening of anti-tuberculosis mycobacterium H37Rv bacterial strain in BACTEC 12B medium (seeing as people such as Collins, Antimicrobial Agents and Chemotherapy, 1997, 41 (5), 1004- 1009). Compounds were tested in ten 2-fold dilutions to determine IC 90 value (IC 90Values ​​are defined as the concentration effective to reduce fluorescence by 90% relative to the control). The feasibility of the VERO cytotoxicity assay was determined as follow...

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Abstract

The present invention provides methods of inhibiting the growth of Mycobacterium species or treating an animal having a Mycobacterium infection (including multi-drug resistance strains and extensively drug resistant strains) by administering a compound of the invention, a salt thereof, or a composition comprising the same.

Description

technical field [0001] The present invention relates, in part, to methods of treating multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) using antibacterial compounds and compositions. Background technique [0002] Today, tuberculosis (TB) is a highly contagious disease, infecting one-third of the world's population. Eight million new cases are reported each year and 3.1 million people die from the disease each year. TB is the leading cause of death among women, AIDS patients and adolescents in the world. TB has a higher mortality rate than any other single infectious disease. Worldwide, TB is responsible for 30% to 50% of AIDS deaths. Globally, the weighted average population of multi-drug resistant (MDR) TB is estimated at about 5% of all TB cases. Extensively drug-resistant (XDR) TB is more expensive and difficult to treat than MDR-TB and patients with XDR-TB have poorer outcomes. XDR-TB is widespread in 45 countries with a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/58A61K31/50A01N43/60A61K31/495
CPCA61K31/505A61K31/17C07D239/28A61K31/167A01N47/44A61K31/155C07C279/08C07C279/12A61P31/04A61P31/06A01N43/58A61K31/50A01N43/60A61K31/495
Inventor 理查德·W·斯科特刘大慧
Owner POLYMEDIX
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