Thiamine analogues and their use as antibiotics

Simple SummaryContent extracted from patent full text and abstract with AI.

This invention introduces a novel class of antibiotic compounds based on thiamine analogues, particularly triazole thiamine derivatives. These compounds uniquely target bacterial thi-box riboswitches—RNA elements that regulate genes essential for bacterial survival. By binding to and activating these riboswitches, the compounds can inhibit bacterial gene expression and thus treat bacterial infections, including those caused by antibiotic-resistant strains.

Use CasesContent extracted from patent full text and abstract with AI.

• Treatment of bacterial infections in humans or animals, especially those caused by resistant bacteria such as Haemophilus influenzae.
• Development of new antibiotics that function via a novel mode of action, addressing growing antibiotic resistance.
• Prophylactic (preventative) treatment in high-risk environments or patients to reduce incidence of bacterial infections.
• Incorporation into pharmaceutical compositions suitable for oral, topical, injectable, or transdermal drug delivery.
• Use in combination therapies with other antibiotics to enhance antibacterial efficacy or overcome multi-drug resistance.

BenefitsContent extracted from patent full text and abstract with AI.

• Targets a novel bacterial mechanism: thi-box riboswitch regulation, which is not exploited by most current antibiotics, reducing potential for cross-resistance.
• Effective against bacteria that have developed resistance to traditional antibiotics.
• Diverse chemical forms (salts, esters, hydrates) and broad formulation compatibility (oral, topical, parenteral, etc.), enabling flexible drug development and administration.
• Compounds can be used in both treatment and prevention (prophylaxis) of infections, expanding their utility.
• Potential for high selectivity and reduced risk of side effects due to specific targeting of bacterial riboswitches.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present invention relates to compounds according to general formula (I), pharmaceutical compositions comprising compounds according to general formula (I) and the use of the compounds for the treatment of a bacterial infection, particularly for use as an antibiotic.