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Title:
HYDROPHOBICALLY ENHANCED AMINOGLYCOSIDES
Document Type and Number:
WIPO Patent Application WO/2010/004433
Kind Code:
A3
Abstract:
Hydrophobically enhanced aminoglycosides have been prepared and shown to be effective antibacterial agents. These agents may be used in the treatment or prevention of various bacterial infections. Methods of preparing these agents also permit facile synthetic access. Formula (I).

Inventors:
BERA SMRITILEHHA (CA)
ZHANEL GEORGE G (CA)
SCHWEIZER FRANK (CA)
Application Number:
PCT/IB2009/006651
Publication Date:
April 08, 2010
Filing Date:
July 09, 2009
Export Citation:
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Assignee:
UNIV MANITOBA (CA)
BERA SMRITILEHHA (CA)
ZHANEL GEORGE G (CA)
SCHWEIZER FRANK (CA)
International Classes:
C07H13/12; A61K31/702; A61K31/7028; A61K31/7036; A61K47/48; A61P31/04; C07H15/12
Domestic Patent References:
WO2003066648A12003-08-14
WO2008040792A22008-04-10
Foreign References:
CA2687689A12009-03-26
US20030054556A12003-03-20
Other References:
BERA ET AL.: "Design, synthesis, and antibacterial activities of neomycin-lipid conjugates: polycationic lipids with potent gram-positive activity", J. MED. CHEM., vol. 51, 2008, pages 6160 - 6164, XP008123388
ZHANG ET AL.: "''Surprising alteration of antibacterial activity of 5''-modified neomycin against resistant bacteria''", J. MED. CHEM., vol. 51, 2008, pages 7563 - 7573, XP008142322
SAINLOS ET AL.: "Kanamycin A-derived cationic lipids as vectors for gene transfection", CHEMBIOCHEM, vol. 6, 2005, pages 1023 - 1033, XP002479876
SAINLOS ET AL.: "Aminoglycoside-derived cationic lipids for gene transfection: synthesis of Kanamycin A derivatives", EUR. J. ORG. CHEM., 2003, pages 2764 - 2774, XP008142324
LI ET AL.: "Investigation of the regioselectivity for the Staudinger reaction and its application for the synthesis of aminoglycosides with N1 modification", J. ORG. CHEM., vol. 72, 2007, pages 4055 - 4066, XP008142327
See also references of EP 2318422A4
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