Method for inhibiting or disrupting biofilm formation, or reducing biofilm

A method for inhibiting or disrupting biofilm formation, or reducing biofilm, in an individual in need thereof, comprising administering to said individual a therapeutically effective amount of a compound of formula I:

• wherein
• R1 is —CR6R7—, wherein R6 and R7 each independently is H, halogen, —COR8, —COOR8, —OCOOR8, —OCON(R8)2, —CN, —NO2, —SR8, —OR8, —N(R8)2, —CON(R8)2, —SO2R8, —SO3H, —S(═O)R8, or (C1-C8)alkyl optionally substituted by one or more groups each independently selected from the group consisting of —COR8, —COOR8, —OCOOR8, —OCON(R8)2, —CN, —NO2, —SR8, —OR8, —N(R8)2, —CON(R8)2, —SO2R8, —SO3H, —S(═O)R8, —N+(R′)3 and —P+(R′)3, wherein R′ each independently is H, (C1-C6)alkyl, phenyl, benzyl, or heterocyclyl, or two R's together with the N atom to which they are attached form a 3-7 membered saturated ring, optionally containing one or more heteroatoms selected from the group consisting of O, S and N and optionally further substituted at the additional N atom;
• R2 and R3 each independently is H, halogen, or (C1-C8)alkyl optionally substituted by one or more groups each independently selected from the group consisting of halogen, —COR8, —COOR8, —OCOOR8, —OCON(R8)2, —CN, —NO2, —SR8, —OR8, —N(R8)2, —CON(R8)2, —SO2R8, —SO3H, —S(═O)R8, —N+(R′)3 and —P+(R′)3, wherein R′ each independently is H, (C1-C6)alkyl, phenyl, benzyl, or heterocyclyl, or two R's together with the N atom to which they are attached form a 3-7 membered saturated ring, optionally containing one or more heteroatoms selected from the group consisting of O, S and N and optionally further substituted at the additional N atom;
• R4 and R5 each independently is selected from the group consisting of (C1-C10)alkylene, (C2-C10)alkenylene, and (C2-C10)alkynylene, optionally substituted by one or more groups each independently selected from the group consisting of halogen, —COR8, —COOR8, —OCOOR8, —OCON(R8)2, —CN, —NO2, —SR8, —OR8, —N(R8)2, —CON(R8)2, —SO2R8, —SO3H, —S(═O)R8, (C6-C10)aryl, (C1-C4)alkylene-(C6-C10)aryl, heteroaryl, and (C1-C4)alkylene-heteroaryl, and further optionally interrupted by one or more identical or different heteroatoms selected from the group consisting of S, O and N, or by one or more groups each independently selected from the group consisting of —NH—CO—, —CO—NH—, —N(C1-C8alkyl)-, —N(C6-C10aryl)-, (C6-C10)arylenediyl, and heteroarylenediyl;
• R8 each independently is H or (C1-C8)alkyl;
• Y each independently is (i) a cation derived from a nitrogen-containing group and selected from the group consisting of an ammonium [—N+(R′)3], hydrazinium [—N+(R′)2—N(R′)2], ammoniumoxy [—N+(R′)2→O], iminium [—N+(R′)2═C<], amidinium [—N+(R′)2—C(R′)═NR′], and guanidinium [—N+(R′)2—C(═NR′)—N(R′)2];
• (ii) a cation derived from a nitrogen-containing mono- or polycyclic heteroaromatic group and selected from the group consisting of pyrazolium, imidazolium, oxazolium, thiazolium, pyridinium, pyrimidinium, quinolinium, isoquinolinium, 1,2,4-triazinium, 1,3,5-triazinium, and purinium, optionally substituted by one or more groups each independently selected from the group consisting of halogen, (C1-C6)alkyl, —COH, —COOH, —OCOOH, —OCONH2, —CN, —NO2, —SH, —OH, —NH2, —CONH2, —SO3H, —SO2H, and —S(═O)H;
• or (iii) a cation derived from an onium group not containing nitrogen and selected from the group consisting of phosphonium [—P+(R′)3], arsonium [—As+(R′)3], oxonium [—O+(R′)2], sulfonium [—S+(R′)2], selenonium [—Se+(R′)2], telluronium [—Te+(R′)2], stibonium [—Sb+(R′)3], and bismuthonium [—Bi+(R′)3];
• wherein R′ each independently is H, (C1-C6)alkyl, phenyl, benzyl, or heterocyclyl, or two R's in the ammonium, hydrazinium, ammoniumoxy, iminium, amidinium or guanidinium groups, together with the N atom to which they are attached, form a 3-7 membered saturated ring, optionally containing one or more heteroatoms selected from the group consisting of 0, S and N and optionally further substituted at the additional N atom;
• X is a counter anion;
• and
• n is an integer of 5-11.