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Last Updated: May 20, 2024

Claims for Patent: 9,993,491


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Summary for Patent: 9,993,491
Title:Guanine riboswitch binding compounds and their use as antibiotics
Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.
Inventor(s): Mulhbacher; Jerome (Sherbrooke, CA), Lafontaine; Daniel (Sherbrooke, CA), Malouin; Francois (Eastman, CA), Allard; Marianne (Sherbrooke, CA), Marsault; Eric (Sherbrooke, CA)
Assignee: SOCPRA--SCIENCES ET GENIE S.E.C. (Sherbrooke, CA)
Application Number:14/616,164
Patent Claims:1. A method of treating a bacterial infection in a subject, said method comprising administering to said subject a therapeutically effective amount of a non ribosylable ligand of a guanine riboswitch, wherein said subject is infected by the bacterial infection prior to said administration, wherein said bacterial infection is caused by a pathogen bearing the guanine riboswitch, and wherein the guanine riboswitch controls the expression of guaA, wherein said pathogen: a) belongs to the genus Staphylococcus or Clostridium; or b) is Alkaliphilus metalliredigens; Alkaliphilus oremlandii; Bacillus anthracis; Bacillus cereus; Bacillus halodurans; Bacillus thuringiensis; Bacillus weihenstephanensis; Exiguobacterium sibiricum; Geobacillus kaustophilus; Geobacillus thermodenitrificans; Lysinibacillus sphaericus; Oceanobacillus iheyensis; Thermoanaerobacter pseudethanolicus; or Thermoanaerobacter X514, and wherein said non ribosylable ligand of guanine riboswitch is the compound 4-hydroxy-2,5,6-triaminopyrimidine (1.01) or a pharmaceutically acceptable salt, solvate or stereoisomer thereof.

2. The method of claim 1, wherein said subject is a cow or a human.

3. The method of claim 1, wherein said pathogen is Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Clostridium botulinum or Clostridium difficile.

4. The method of claim 1, wherein said infection is a mammary gland infection.

5. The method of claim 1, wherein said pathogen is a pathogen belonging to the genus Staphylococcus or Clostridium and wherein said pathogen is Staphylococcus aureus; Staphylococcus carnosus; Staphylococcus epidermidis; Staphylococcus haemolyticus, Staphylococcus saprophyticus, Clostridium acetobutylicum; Clostridium beijerinckii; Clostridium botulinum; Clostridium difficile; Clostridium novyi; Clostridium perfringens or Clostridium tetani.

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