Polyol modified aminoglycoside-lipid conjugates
AssigneeUniversity of Manitoba
InventorsFrank Schweizer, Smritilekha Bera, George Zhanel
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Abstract
In some aspects, the present invention provides aminoglycoside derivatives thereof that exhibit antibacterial activity. In some aspects, the aminoglycoside derivatives comprise compounds consisting of (a) an ammoglycoside group and (b) at least one hydrophobic carbamate and alkoxy group to the primary or secondary hydroxy position of the aminolvcoside group and salts thereof. Additionally, methods of treating and preventing bacterial infections using the aminoglycoside derivatives are also provided
Claims27
1-32. (canceled)
An aminoglycoside derivative comprising:
- (a) an aminoglycoside group;
- and
- (b) at least one carbamate group or alkoxy group attached to a primary or secondary hydroxy position of the aminoglycoside group;
- or a salt thereof.
An aminoglycoside derivative defined as:
- wherein
- each R1 and each R2 are each independently:
- H, C(NH)NH2, —C(O)(NH2), alkyl(C≦18), alkenyl(C≦18), aryl(C≦18), aralkyl(C≦18), heteroaryl(C≦18), heteroaralkyl(C≦18), acyl(C≦18), or substituted versions thereof, provided that not all R1 and R2 are H;
- or pharmaceutically-acceptable salts thereof.
An aminoglycoside derivative defined as:
- wherein
- each R1 and each R2 are each independently:
- H, C(NH)NH2, C(O)(NH2), alkyl(C≦18), alkenyl(C≦18), alkynyl(C≦18), aryl(C≦18), aralkyl(C≦18), heteroaryl(C≦18), heteroaralkyl(C≦18), acyl(C≦18), or substituted versions thereof, provided that not all R1 and R2 are H;
- or pharmaceutically-acceptable salts thereof.
An aminoglycoside derivative defined as:
- wherein
- each R1 is H, —C(NH)NH2, —C(O)(NH2), alkyl(C≦18), alkynyl(C≦18), aralkyl(C≦18), heteroaryl(C≦18), heteroaralkyl(C≦18), acyl(C≦18), or substituted versions thereof;
- or pharmaceutically-acceptable salts thereof.
An aminoglycoside derivative defined as:
- wherein
- each R1 and each R2 are each independently:
- H, C(NH)NH2, —C(O)(NH2), alkyl(C≦18), alkenyl(C≦18), alkynyl(C≦18), aryl(C≦18), aralkyl(C≦18), heteroaryl(C≦18), heteroaralkyl(C≦18), acyl(C≦18), or substituted versions thereof, provided that not all R1 and R2 are H;
- or pharmaceutically-acceptable salts thereof.
58-73. (canceled)
Dependencies are inferred from the claim text.