Antibacterial agents comprising conjugates of glycopeptides...

Details Antibacterial agents comprising conjugates of glycopeptides... Antibacterial agents comprising conjugates of glycopeptides...

C - Chemistry, Metallurgy

07

K

C07K 9/00 (2006.01) A61K 47/48 (2006.01) A61P 31/04 (2006.01) C07K 7/08 (2006.01) C07K 14/195 (2006.01) C07K 14/435 (2006.01) C07K 14/46 (2006.01) C07K 14/47 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2426012

The invention concerns agents with anti-bacterial activity and methods and intermediates for their production. The present invention further concerns the use of such agents for the treatment of bacterial infections in animals, including man. The agents are derivatives of vancomycin-type antibiotics, of structure: V-L-W-X; wherein V is a glycopeptide moiety which inhibits peptidoglycan biosynthesis in bacteria; L is a linking group; W is a peptidic membrane-associating element such as an element based on naturally-occurring animal or bacterial peptide antibiotics; and X is hydrogen or a membrane- insertive element.

L'invention concerne des agents présentant une activité antibactérienne et des procédés et intermédiaires pour leur production. La présente invention concerne également l'utilisation de tels agents pour le traitement d'infections bactériennes chez les animaux, y compris chez l'homme. Ces agents sont des dérivés d'antibiotiques de type vancomycine, de structure: V-L-W-X; où V représente un groupe glycopeptide qui inhibe la biosynthèse de la muréine dans les bactéries; L représente un groupe de liaison; W représente un élément peptidique d'association membranaire tel qu'un élément à base d'antibiotiques peptidiques naturels d'origine animale ou bactérienne; et X représente un hydrogène ou un élément d'insertion membranaire.

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