Substituted polyamines as inhibitors of bacterial efflux pumps
AssigneeParatek Pharmaceuticals, Inc.
InventorsMark L. Nelson, Michael N. Alekshun
Life of this patent
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Abstract
Disclosed are methods of treating bacterial infections including those caused by multidrug resistant bacteria using polyamine efflux pump inhibiting compounds, including for example N-benzylated polyazaalkanes, N-benzylated polyaminoalkanes, or mixed N-benzylated poly(aza/amino)alkanes, optionally in combination with other drugs such as antibiotics, as well as pharmaceutical compositions thereof.
Claims20
An inhibitor of an efflux pump for treating an infection caused by a microbe in a subject consisting of a polyazaalkane, polyaminoalkane, or mixed poly(aza/amino)alkane, any carbon atom of which may be hydroxyl, amino, or oxo substituted, and wherein said inhibitor contains at least two nitrogen atoms that are bonded to a lipophilic group, wherein said inhibitor inhibits efflux pump activity.
(canceled)
A method for treating a microbial infection in an animal, comprising administering to an animal suffering from said infection an efflux pump inhibitor in an amount sufficient to reduce efflux pump activity, wherein said inhibitor is a polyazaalkane, polyaminoalkane, or mixed poly(azdamino)alkane, any carbon atom of which may be hydroxyl, amino, or oxo substituted, and wherein said inhibitor contains at least two nitrogen atoms that are bonded to a lipophilic group, such that infection is inhibited.
(canceled)
A method of enhancing the antimicrobial activity of an antimicrobial agent against a microbe, comprising contacting said microbe with said antimicrobial agent and an efflux pump inhibitor in an amount effective to inhibit an efflux pump in said microbe, wherein said inhibitor is a polyazaalkane, polyaminoalkane, or mixed poly(aza/amino)alkane, any carbon atom of which may be hydroxyl, amino, or oxo substituted, and wherein said inhibitor contains at least two nitrogen atoms that are bonded to a lipophilic group, such that said activity is enhanced.
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Dependencies are inferred from the claim text.