Lytix Biopharma As

Lytix Biopharma

Universitetet I Tromsø—norges Arktiske Universit

Universitetet I Tromsø—norges Arktiske Universitet

Øystein Rekdal

John Sigurd Svendsen

Wenche Stensen

Baldur Sveinbjørnsson

Morten Bøhmer Strøm

Bengt Erik Haug

Istvan Marko

Merete Linchausen Skar

Frederick Alan Leeson

Jon Amund Eriksen

Liv Marie Eike

Lars Vorland

Stig Olov Magnus Engqvist

Ketil Camilio

Liv Tone Eliassen

Gerd Berge

Johannes Eksteen

Mari Wikman

Terese Solstad

Nannan Yang

Trond Flægstad

John Sigurd Mjøen Svendsen

The present invention provides a peptide which: (i) consists of 10 to 16 amino acids; (ii) has at least 8 cationic amino acids with either (a) a side chain comprising a guanidinium group, or (b) a side chain comprising an amino group, of which no more than 7 are consecutive; and (iii) has 2 or 3 tryptophan residues which are not both, or not all, consecutive, said peptide optionally in the form of a salt, ester or amide, or a peptidomimetic of said peptide. The invention further relates to pharmaceutical compositions containing these compounds, the use of these compounds in therapy, particularly as anti-tumor (e.g. anti-lymphoma) agents and non-therapeutic uses of these compounds.

Anti-lymphoma peptides

The present invention relates to a compound of formula (I) AA-AA-AA-R&#x2014;R(I) wherein, in any order, 2 of said AA (amino acid) moieties are cationic amino acids and 1 of said AA is an amino acid with a lipophilic R group, the R group having 14-27 non-hydrogen atoms; Ris a N atom, which may be substituted by a branched or unbranched C-Calkyl or aryl group, which group may incorporate up to 2 heteroatoms selected from N, O and S; and Ris an aliphatic moiety having 2-20 non-hydrogen atoms, said moiety being linear, branched or cyclic. The invention further relates to formulations containing these compounds, solid supports having these compounds attached thereto, the use of these compounds in therapy, particularly as antimicrobial, anti-tumor or anti-biofilm agents and non-therapeutic uses of these compounds, particularly their use in inhibiting biofilm formation or removing a biofilm.

Antimicrobial compounds

The invention provides a method of treating tumors by adminstering to a human or animal patient an effective amount of a molecule of 2 to 4 amino acids or equivalent subunits in length, which incorporates a bulky and lipophilic group comprising at least 13 non-hydrogen atoms and containing no more than 2 polar functional groups, in which the bulky and lipophilic group incorporates one or more closed rings of 5 or more non-hydrogen atoms, and in which the molecule further has at least two more cationic than anionic moieties.

Method of treating tumors

The present invention provides a cytotoxic 7 to 25 mer peptide with three or more cationic residues which has one or more non-genetic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them and their use as medicaments, particularly as antibacterions or antitumoral agents. In a preferred aspect, the invention provides the use of said peptides in a method of inducing adaptive immunity against tumor growth or establishment in a subject, as well as the use of other lytic agents in a method of inducing adaptive immunity in a subject.

Inhibition of tumor growth

The present invention relates to a peptide or peptidomimetic for use in the treatment of a biofilm-associated infection in a subject, wherein said peptide or peptidomimetic a) carries a net positive charge, &#x2014;b) is 1 to 6 amino acids in length or is an equivalently sized peptidomimetic; and c) is amphipathic in nature, having one or more lipophilic groups, one of said lipophilic groups comprising at least 7 non-hydrogen atoms.

Treatment of biofilms

Inhibition of tumour growth

The present invention provides a cytotoxic 7 to 25-mer peptide with three or more cationic residues which has one or more non-generic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them, and their use as medicaments, particularly as antibacterial or antitumor agents.

Bioactive peptides

The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilizing microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics.

Antimicrobial compounds and formulations

The present invention provides a cytotoxic 7 to 25-mer peptide with three or more catonic residues which has one or more non-genetic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them, and their use as medicaments, particularly as antibacterial or antitumor agents.

The present invention relates to a method of producing a bioactive peptide, wherein the peptide is 7 to 25 amino acids in length, has at least 3 cationic amino acids and is capable of forming an amphipathic &#x3b1;-helix, which method comprises identification of a cationic sector and division of the remaining part of the peptide into three further sectors which are substantially equal in size, and incorporation of at least 60% of the bulk and lipophilicity provided by the amino acid R groups into the sectors flanking the cationic sector; and to uses of the peptides produced thereby in therapy, particularly in the treatment of benign or malignant tumours.

Growing community of inventors

Tomasjord, Norway

Øystein Rekdal