Lytix Biopharma As

Peptide Patents As

Amicoat As

Oystein Rekdal

John Sigurd Svendsen

Wenche Stensen

John Sigurd Mjoen Svendsen

Liv Marie Eike

Ketil Camilio

Laurence Zitvogel

Takahiro Yamazaki

Baldur Sveinbjornsson

Jon Amund Eriksen

Bengt Erik Haug

Frederick Alan Leeson

Istvan Marko

Merete Linchausen Skar

Baldur Sveinbjörnsson

Ketil André Camilio

Johannes Eksteen

Bengt Erick Haug

Trond Flaegstad

Stig Olov Engqvist

Morten Böhmer Ström

The present invention provides a compound, preferably a peptide, having the following characteristics:

Immune checkpoint inhibitor combinations

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-tumour 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 present invention provides a compound, preferably a peptide, having the following characteristics: a) consisting of 9 amino acids in a linear arrangement; b) of those 9 amino acids, 5 are cationic and 4 have a lipophilic R group; c) at least one of said 9 amino acids is a non-genetically coded amino acid (e.g. a modified derivative of a genetically coded amino acid); and optionally d) the lipophilic and cationic residues are arranged such that there are no more than two of either type of residue adjacent to one another; and further optionally e) the molecule comprises two pairs of adjacent cationic amino acids and one or two pairs of adjacent lipophilic residues; for use in the treatment of a tumour by combined, sequential or separate administration with a cytotoxic chemotherapeutic agent that inhibits immune tolerance, wherein the chemotherapeutic agent is administered at a sub-cytotoxic dose. The present invention further provides pharmaceutical packs or compositions comprising these active agents and methods of treating a tumour comprising administration of these active agents.

Chemotherapeutic combinations of cationic antimicrobial peptides and chemotherapeutics

The present invention provides a compound, preferably a peptide, having the following characteristics: a) consisting of 9 amino acids in a linear arrangement; b) of those 9 amino acids, 5 are cationic and 4 have a lipophilic R group; c) at least one of said 9 amino acids is a non-genetically coded amino acid (e.g. a modified derivative of a genetically coded amino acid); and optionally d) the lipophilic and cationic residues are arranged such that there are no more than two of either type of residue adjacent to one another; and further optionally e) the molecule comprises two pairs of adjacent cationic amino acids and one or two pairs of adjacent lipophilic residues; for use in the treatment of a tumour by combined, sequential or separate administration with an immune checkpoint inhibitor. The present invention further provides pharmaceutical packs or compositions comprising these active agents and methods of treating a tumour comprising administration of these active agents. Also provided are the peptidic compounds as defined above for use in the destabilisation of a mitochondrial membrane, and a peptidic compound as defined above and an immunotherapeutic agent as a combined preparation for separate, simultaneous or sequential use in treating tumours.

The present invention relates to peptides or peptide like molecules and their uses in therapy, in particular as anti-tumor agents.

Nonapeptide with anti-tumour activity

The present invention relates to a method of improving the resistance of a peptide or peptidomimetic to degradation by trypsin which comprises incorporating into said peptide or peptidomimetic a C-terminal capping group of formula (I): X&#x2014;Y&#x2014;Z (I) wherein X is 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; Y represents a group selected from &#x2014;R&#x2014;R&#x2014;, &#x2014;R&#x2014;R&#x2014;R,- and &#x2014;R&#x2014;R&#x2014;R&#x2014; wherein Ris C, O, S or N, and Ris C; each of Rand R, may be substituted by C-Calkyl groups or unsubstituted; and Z is a group comprising 1 to 3 cyclic groups each of 5 or 6 non-hydrogen atoms, 2 or more of the cyclic groups may be fused and one or more of the cyclic groups may be substituted; the Z. moiety incorporates a maximum of 15 non-hydrogen atoms; and wherein the bond between Y and Z is a covalent bond between Ror Rof Y and a non-hydrogen atom of one of the cyclic groups of Z.

Methods of peptide modification

The present invention relates to a compound of formula (I) AA-AA-AA-X&#x2014;Y&#x2014;Z 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; X is 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; Y represents a group selected from &#x2014;R&#x2014;R&#x2014;, &#x2014;R&#x2014;R&#x2014;R&#x2014; and &#x2014;R&#x2014;R&#x2014;R&#x2014; wherein Ris C, O, S or N, and Ris C; each of Rand Rmay be substituted by C-Calkyl groups or unsubstituted; and Z is a group comprising 1 to 3 cyclic groups each of 5 or 6 non-hydrogen atoms, 2 or more of the cyclic groups may be fused and one or more of the cyclic groups may be substituted; the Z moiety incorporates a maximum of 15 non-hydrogen atoms; and wherein the bond between Y and Z is a covalent bond between Ror Rof Y and a non-hydrogen atom of one of the cyclic groups of Z. The invention further relates to formulations containing these compounds and their uses in therapy, particularly as antimicrobial or antitumoural agents.

Growing community of inventors

Billingstad, Norway

Oystein Rekdal