US2022226486A1PendingUtilityA1
Synthetic compound
Est. expiryMay 24, 2036(~9.8 yrs left)· nominal 20-yr term from priority
A61K 39/39A61K 47/60A61P 3/00C07K 14/705A61P 31/04C07K 16/2842A61P 35/00A61K 47/6811A61P 31/12A61P 37/06A61K 47/64C07K 7/06C07K 5/1013A61K 38/08A61K 47/6849A61P 25/00
47
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Claims
Abstract
The present invention relates to a synthetic compound comprising at least one effector moiety and at least one binder moiety, wherein the effector moiety is associated to the binder moiety, and wherein further the effector moiety comprises a N-formyl methionine peptide which comprises an isoleucine residue.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A synthetic compound comprising at least one effector moiety and at least one binder moiety,
wherein the effector moiety is associated to the binder moiety, and wherein further the effector moiety comprises a N-formyl methionine peptide which comprises an isoleucine residue.
2 . The synthetic compound according to any of the aforementioned claims, in which compound the N-formyl methionine residue is located N-terminally.
3 . The compound according to claim 1 , wherein the effector moiety is associated to the binder moiety either
directly, and/or via a linker.
4 . The synthetic compound according to any of the aforementioned claims, in which compound the N-formyl methionine peptide comprises, in addition to the at least one isoleucine residue, at least one residue selected from the group consisting of leucine, phenylalanine, valine and/or threonine.
5 . The synthetic compound according to any of the aforementioned claims, in which compound the N-formyl methionine peptide comprises, in addition to the at least one isoleucine residue,
at least one phenylalanine residue and at least one leucin residue, or at least one phenylalanine residue, at least one leucin residue and at least one selected from a threonine residue and/or a valine residue.
6 . The synthetic compound according to any of the aforementioned claims, in which compound the N-formyl methionine residue is followed, in direction N->C, by
a first block comprising one or two isoleucine residues, and a second block comprising a phenylalanine residue and a leucin in any order relative to one another, wherein the two blocks can be positioned in any order relative to one another, and are either linked directly or via a peptide sequence comprising up to two amino acid residues.
7 . The synthetic compound according to any of the aforementioned claims, in which compound the effector moiety comprises, in addition to the N-formyl methionine residue, at least one of the sequence motifs selected from the group consisting of
IFL LFII, IVTLF. LFIIK, and/or IFTLF.
8 . The synthetic compound according to any of the aforementioned claims, in which compound the effector moiety comprises at least one peptide sequence selected from the group consisting of fMIFL (SEQ ID No 3), fMLFII (SEQ ID No 4) and/or fMIVTLF (SEQ ID No 5), fMLFIIK (SEQ ID No 6) and fMIFTLF (SEQ ID No 7).
9 . The synthetic compound according to any of the aforementioned claims, in which compound the binder moiety is at least one selected from the group consisting of
a peptide or peptidomimetic an antibody, or a fragment or derivative thereof a receptor molecule, or a fragment or derivative thereof an antibody mimetic, or a fragment or derivative thereof, and/or an aptamer.
10 . The synthetic compound according to any of the aforementioned claims, in which compound the binder moiety targets α3 integrin or αvβ6 integrin, or a subdomain or epitope thereof.
11 . The synthetic compound according to any of the aforementioned claims, in which compound the linker comprises polyethylene glycol.
12 . The synthetic compound according to claim 6 , in which compound the linker comprises one or more polyethylene glycol molecules of between 40 and ≥15 monomers in length.
13 . The synthetic compound according to claim 6 or 7 , in which compound the polyethylene glycol linker is bound to the effector moiety by means of one or more amino acid side chain groups.
14 . The synthetic compound according to any of the aforementioned claims, wherein at least two moieties selected from an effector moiety, a binder moiety, agonist are linked to one another by means of click chemistry.
15 . A pharmaceutical formulation comprising the synthetic compound according to any of the aformentioned claims, and physiologically acceptable excipients.
16 . Use of the synthetic compound according to the any of the aformentioned claims, or the formulation according to claim 12 , for the treatment of a human or animal subject.
17 . Use according to claim 13 , wherein said use relates to the treatment of at least one disease selected from the group consisting of:
Neoplastic diseases Autoimmune diseases Neuropathological disease, Metabolic diseases and/or Infectious diseases.Join the waitlist — get patent alerts
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