Polyol modified aminoglycoside-lipid conjugates
AssigneeUniversity of Manitoba
InventorsFrank Schweizer, Smritilekha Bera, George Zhanel
Life of this patent
Estimating the term…
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.
Claims11
An aminoglycoside derivative of the following formula:
- wherein
- each R1 is H and each R2 is:
- C(O)NHC6H5, C(O)NH-p-C6H4Cl, C(O)NHC6H13, C(O)NH-p-C6H4N(Me)2, CH2-p-C6H4Cl, CH2-p-C6H4C(CH3)4, or CH3;
- or pharmaceutically-acceptable salts thereof.
An aminoglycoside derivative of the following formula:
- wherein
- each R1 is H and each R2 is:
- C(O)NHC6H5, C(O)NHC6H13, C(O)NH-p-C6H4N(Me)2, CH2C6H5, CH2-p-C6H4Cl, or CH3;
- or pharmaceutically-acceptable salts thereof.
An aminoglycoside derivative of the following formula:
- wherein
- each R1 is H, C(NH)NH2, C(O)(NH2), alkyl(C≦18), substituted alkyl(C≦18), alkenyl(C≦18), substituted alkenyl(C≦18), alkynyl(C≦18), substituted alkynyl(C≦18), aryl(C≦18), substituted aryl(C≦18), aralkyl(C≦18), substituted aralkyl(C≦18), heteroaryl(C≦18), substituted heteroaryl(C≦18), heteroaralkyl(C≦18), substituted heteroaralkyl(C≦18), acyl(C≦18), substituted acyl(C≦18);
- or pharmaceutically-acceptable salts thereof.
An aminoglycoside derivative of the following formula:
- wherein
- each R1 and each R2 are each independently:
- H, C(NH)NH2, C(O)(NH2), alkyl(C≦18), substituted alkyl(C≦18), alkenyl(C≦18), substituted alkenyl(C≦18), alkynyl(C≦18), substituted alkynyl(C≦18), aryl(C≦18), substituted aryl(C≦18), aralkyl(C≦18), substituted aralkyl(C≦18), heteroaryl(C≦18), substituted heteroaryl(C≦18), heteroaralkyl(C≦18), substituted heteroaralkyl(C≦18), acyl(C≦18), substituted acyl(C≦18), provided that not all R1 and R2 are H;
- or pharmaceutically-acceptable salts thereof.
Dependencies are inferred from the claim text.