Novel prodrugs for antimicrobial amidines

C - Chemistry – Metallurgy – 07 – D

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C07D 307/54 (2006.01) A61K 31/00 (2006.01) A61K 31/341 (2006.01) A61K 31/357 (2006.01) A61K 31/381 (2006.01) A61K 31/40 (2006.01) C07D 407/14 (2006.01)

Patent

CA 2377902

A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by Formula (I), wherein: X may be O, S, or NR' wherein R' is H or loweralkyl; R1 and R2 may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R5 is represented by a formula selected from the group consisting of: (a) and (b), wherein: X1, X2, and X3 are independently selected from O and S; and R6 and R7 are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.

L'invention concerne des méthodes de traitement d'une infection, qui consistent à administrer une dose efficace au plan thérapeutique d'un composé de formule (I) ou d'un sel de celui-ci, acceptable au plan pharmaceutique,. Dans ladite formule (I), X peut représenter O, S, ou NR', R' représentant H ou alkyle inférieur ; R¿1? et R¿2? peuvent être choisis séparément dans le groupe constitué de H, alkyle inférieur, oxyalkyle, alcoxyalkyle, cycloalkyle, aryle, hydroxyalkyle, aminoalkyle et alkylaminoalkyle; R¿3? et R¿4? sont choisis séparément dans le groupe constitué de H, alkyle inférieur, halogène, oxyalkyle, oxyaryle et oxyarylalkyle ; R¿5? est représenté par une formule choisie dans le groupe constitué de (a) et (b), X¿1?, X¿2?, X¿3? étant choisis séparément parmi O et S ; et R¿6? et R¿7? étant choisis séparément dans le groupe constitué d'alkyle inférieur, aryle, alkylaryle, oxyaryle, un substituant contenant un ester, et oxyalkyle.

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