The present disclosure relates to derivatives of neamine-based aminoglycoside antibacterial drugs modified in position C6′, C2′ and/or C5″. The modifications impart favorable properties regarding activity against ESKAPE pathogens, evasion of resistance traits and increased selectivity, enabling systemic use of the compounds.

The present disclosure relates to derivatives of neamine-based aminoglycoside antibacterial drugs modified in position C6′, C2′ and/or C5″. The modifications impart favorable properties regarding activity against ESKAPE pathogens, evasion of resistance traits and increased selectivity, enabling systemic use of the compounds.

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.

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.

The invention relates to derivatives of apramycin-based aminoglycoside antibacterial drugs modified in positions C5 and/or C6 and O5 and/or O6. The modifications impart favourable properties regarding increased selectivity and retention of activity in the presence of resistance determinants of the AAC(3) class. The invention further relates to said compounds for use in the therapy of bacterial infection by systemic administration, especially in instances where the infection is caused by a pathogen comprising a resistance determinant of the AAC(3) class, in particular AAC(3)-IV.

Provided herein are hyperbranched polyaminoglycosides, where in some embodiments, the hyperbranched polyaminoglycosides are covalently modified to store and release nitric oxide. Some embodiments pertain to methods of making and use of hyperbranched polyaminoglycosides. In some embodiments, the covalently modified hyperbranched polyaminoglycosides may be tailored to release nitric oxide in a controlled manner and are useful for eradication of both gram positive and gram negative bacteria as well as other microbes.

The invention relates to drug development and synthetic chemistry, in particular to the manufacture of biologically active compounds based on naturally occurring molecules. It also relates to novel biologically active compounds, for example aminoglycoside antibiotics, in a substantially pure regioisomeric form. More particularly, the present invention relates to methods for the chemo- or regioselective derivatization of a target compound with multiple reactive groups, some of which may be derivatezed, and other which will not be derivatized.

The invention relates to drug development and synthetic chemistry, in particular to the manufacture of biologically active compounds based on naturally occurring molecules. It also relates to novel biologically active compounds, for example aminoglycoside antibiotics, in a substantially pure regioisomeric form. More particularly, the present invention relates to methods for the chemo- or regioselective derivatization of a target compound with multiple reactive groups, some of which may be derivatezed, and other which will not be derivatized.

This disclosure relates to the incorporation of amphiphilic guanidinylated aminoglycosides (e.g., neomycin) into liposomal assemblies, which contain entrapped therapeutics. The lysosome is responsible for enzymatically breaking down and recycling large biomolecules and aged organelles. While malfunctioned lysosomal enzymes have been established in Lysosomal Storage Disorders (LSDs), recent reports have suggested that defects in lysosomal enzymes (e.g., glucocerebrosidase) are also linked to other chronic ailments, including neurological disorders such as Parkinson's Disease and related disorders.

This disclosure relates to the incorporation of amphiphilic guanidinylated aminoglycosides (e.g., neomycin) into liposomal assemblies, which contain entrapped therapeutics. The lysosome is responsible for enzymatically breaking down and recycling large biomolecules and aged organelles. While malfunctioned lysosomal enzymes have been established in Lysosomal Storage Disorders (LSDs), recent reports have suggested that defects in lysosomal enzymes (e.g., glucocerebrosidase) are also linked to other chronic ailments, including neurological disorders such as Parkinson's Disease and related disorders.