Ultupharma Ab

Joakim Bjerketorp

Jolanta Levenfors

Anders Broberg

Bengt Guss

Bo Öberg

Christina Nord

Christer Sahlberg

Pierre Andersson

Bo Oberg

The present invention relates to novel compounds, which presents a peptide structure and an unexpected antibacterial effect even against certain multiresistant bacteria. The compounds may be cyclic peptides, sometimes depsipeptides, or non-ring-closed peptides, as defined by Formula (I). Further, the invention relates to the medical use of the herein claimed compounds, a method for the production of the compounds as well as a method of treatment including the compounds. In addition, the invention relates to a pharmaceutical preparation comprising one or more of the herein described and claimed compounds combined with suitable carrier(s) and/or adjuvant(s). Finally, the invention is the use of one or more of the claimed compounds in a method for decolonization of a surface of Gram-positive and/or Gram-negative bacteria.

Peptide compounds

The invention relates to compounds of Formula I, wherein the variables are as defined in the claims, which are useful in the treatment and/or prevention of bacterial infections in a subject. The invention further relates to the use of a compound of Formula I in the manufacture of a medicament, and medical devices when used in a method of treating or preventing a bacterial infection in a subject, and related aspects.

Compounds and methods of treating bacterial infections

The present invention relates to a composition comprising a first compound which is a nucleoside analogue capable of inhibiting a bacterial colonisation or infection of a subject; a second compound which is capable of decreasing mitochondrial toxicity of said nucleoside analogue and surprisingly enhance the antibacterial effect of the combination; and a third compound capable of decreasing the concentration in bacteria of nucleosides and/or nucleotides known to compete with nucleoside analogues. The first compound may be AZT, FdUrd, 5-fluorouracil, BrdUrd, IdUrd, didanosine or gemcitabine; the second compound may be uridine or a uridine-comprising compound; and the third compound may be trimethoprim or a compound comprising trimethoprim, such as trimethoprim-sulfa.

Method of treating bacterial infections

The present invention relates to a composition comprising a first compound which is a nucleoside analogue capable of inhibiting a bacterial colonisation or infection of a subject; a second compound which is capable of decreasing mitochondrial toxicity of said nucleoside analogue and surprisingly enhance the antibacterial effect of the combination; and a third compound capable of decreasing the concentration in bacteria of nucleosides and/or nucleotides known to compete with nucleoside analogues. The first compound may be AZT, FdUrd, 5-fluorouracil, BrdUrd, IdUrd, didanosine or gemcitabine; the second compound may be uridine or a uridine-comprising compound; and the third compound may be iclaprim; trimethoprim; or a compound comprising trimethoprim, such as trimethoprim-sulfa.

The invention relates to compounds of Formula (I), wherein the variables are as defined in the claims, which are useful in the treatment and/or prevention of bacterial infections in a subject. The invention further relates to the use of a compound of Formula (I) in the manufacture of a medicament, and medical devices when used in a method of treating or preventing a bacterial infection in a subject, and related aspects. 

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Uppsala, Sweden

Joakim Bjerketorp