Antimicrobial compounds

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/08 (2006.01) A61P 17/00 (2006.01) A61P 31/04 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2738974

The present invention relates to a compound of formula (I) AA-AA-AA-R1-R2 (I) wherein, in any order, 2 of said AA (amino acid) moieties are cationic amino acids and 1 of said AA is an amino acid with a lipophilic R group, the R group having 14-27 non-hydrogen atoms; R1 is a N atom, which may be substituted by a branched or unbranched C1-C10 alkyl or aryl group, which group may incorporate up to 2 heteroatoms selected from N, O and S; and R2 is an aliphatic moiety having 2-20 non-hydrogen atoms, said moiety being linear, branched or cyclic. The invention further relates to formulations containing these compounds, solid supports having these compounds attached thereto, the use of these compounds in therapy, particularly as antimicrobial, anti-tumour or anti-biofilm agents and non- therapeutic uses of these compounds, particularly their use in inhibiting biofilm formation or removing a biofilm.

La présente invention concerne un composé de formule (I) AA-AA-AA-R1-R2  (I) dans laquelle deux desdits groupements d'acides aminés AA sont, dans n'importe quel ordre, des acides aminés cationiques et l'un desdits acides aminés AA est un acide aminé renfermant un groupe R lipophile, le groupe R possédant de 14 à 27 atomes différents de l'hydrogène; R1 est un atome d'azote qui peut être remplacé par un groupe alkyle ou aryle C1-C10, ramifié ou non, lequel groupe peut contenir jusqu'à 2 hétéroatomes sélectionnés parmi N, O et S; et R 2  est un groupement aliphatique possédant de 2 à 20 atomes différents de l'hydrogène, ledit groupement étant linéaire, ramifié ou cyclique. L'invention concerne également des formulations contenant ces composés, des supports solides auxquels sont fixés ces composés, l'utilisation thérapeutique de ces composés, en particulier en tant quagents antimicrobiens, anticancéreux ou anti-biofilm, et des utilisations non thérapeutiques de ces composés, notamment leur utilisation dans la prévention de la formation de biofilm ou dans la suppression d'un biofilm.

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