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AssigneeHelmholtz-Zentrum FüR Infektionsforschung GmbH
InventorsDuy-Khiet Ho, Brigitta Loretz, Claus-Michael Lehr
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The present invention relates to conjugates of aminoglycosides and terpenoids, in particular sesquiterpenoids. Furthermore, the present invention relates to nano-assemblies formed by the inventive conjugates and to a method for producing the conjugates and/or the nano-assemblies. The present invention also relates to the inventive conjugates and nano-assemblies for use in therapy, in particular for use in the treatment of infectious diseases. Particularly preferred embodiments of the present invention relate to farnesylated aminoglycosides and nano-assemblies thereof, in which farnesol and its derivatives do not only function as carrier for the aminoglycosides but do themselves have pharmaceutical activity upon cleavage of the conjugate, in particular quorum sensing inhibitory activity.
A conjugate comprising an aminoglycoside moiety and at least one terpenyl moiety, wherein the terpenyl moiety has at most 20 carbon atoms, and wherein the aminoglycoside moiety and the terpenyl moiety are linked via a pH-sensitive link that is not stable at a pH<5.0, wherein the term “not stable” indicates that at least 80% of the aminoglycoside is released from the conjugate after incubation at pH<5.0 for at most at 8 hours at a temperature of 37° C.
Dependencies are inferred from the claim text.