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US 2020/0048308 A1Published application
Influenza virus neutralizing compounds
AssigneeJanssen Vaccines & Prevention B.V.
InventorsJaroslaw JURASZEK, Maria VAN DONGEN, Boerries BRANDENBURG
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel compounds, in particular peptidic macrocyclic peptides, that are capable of binding to and/or neutralizing influenza viruses, in particular influenza A viruses comprising HA of the H1 subtype 1, and to pharmaceutical compositions comprising such compounds. The invention also relates to the use of the peptidomimetic 5 compounds in the diagnosis, prophylaxis and/or treatment of influenza virus infections.
Claims16
A compound comprising the sequence:
- CapN-Tyr-X1-Asp-Pro-X2-Gly-X3-X4-Gly-X5-[Met/Nlu]-CapC,
- wherein CapN and CapC each are an amino acid sequence comprising from 0-10 residues;
- X1 is any charged, hydrophilic or polar L or D-amino acid, as well as any non-canonical hydrophilic, charged or polar L or D amino-acid;
- X2 is a hydrophobic, aliphatic or aromatic, canonical or non-canonical amino acid, provided that X2 is not proline;
- X3 is a small or medium aliphatic or hydrophobic L-amino acid;
- X4 is a small aliphatic or hydrophobic L-amino acid;
- and
- X5 is any polar or charged L- or D-amino acid,
- and wherein the compound is capable of specifically binding to hemagglutinin (HA) of an influenza A virus strain comprising HA of the H1 subtype.
6 more elements
A compound selected from the group consisting of:
- Suc-Cys-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Cys-NH2, which is cyclized through a cysteine bridge (SEQ ID NO:
- 1);
- Suc-Cys-Tyr-Arg-Asp-Pro-Leu-Gly-Val-Ala-Gly-Glu-Met-Cys-NH2, which is cyclized through a cysteine bridge (SEQ ID NO:
- 2);
- Suc-Cys-Tyr-Arg-Asp-Pro-Ph5-Gly-Val-Abu-Gly-Glu-Met-Cys-NH2, which is cyclized through a cysteine bridge (SEQ ID NO:
- 3);
- Suc-Cys-Tyr-Arg-Asp-Pro-Leu-Gly-Val-Ala-Gly-Glu-Nlu-Cys-NH2, which is cyclized through a cysteine bridge (SEQ ID NO:
- 4);
- Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-Gly, which is cyclized through a head-to-tail linkage (SEQ ID NO:
- 5);
- Suc-Cys-Leu-Tyr-Arg-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-Cys-NH2, which is cyclized through a cysteine bridge (SEQ ID NO:
- 6);
- Suc-Cys-Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-Cys-NH2, which is cyclized through a cysteine bridge (SEQ ID NO:
- 7);
- Pro-Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-D-Pro, which is cyclized through a head-to-tail linkage (SEQ ID NO:
- 8);
- Gly-Leu-Tyr-Glu-Asp-Pro-Ph5-Gly-Val-Abu-Gly-Gly-Met-Gly-D-Pro, which is cyclized through a head-to-tail linkage (SEQ ID NO:
- 9);
- Gly-Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-D-Pro, which is cyclized through a head-to-tail linkage (SEQ ID NO:
- 10);
- Suc-Cys-Leu-Tyr-Arg-Asp-Pro-Leu-Gly-Val-Ala-Gly-Glu-Met-Gly-Cys-NH2, which is cyclized through a cysteine bridge (SEQ ID NO:
- 11);
- Suc-Val-Ser-Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-Val-Tyr-NH2 (SEQ ID NO:
- 12);
- Suc-Val-Ser-Leu-Tyr-Arg-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-Val-Tyr-NH2 (SEQ ID NO:
- 13);
- D-Pro-Ser-Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-Val-Pro, which is cyclized through a head-to-tail linkage (SEQ ID NO:
- 14);
- Suc-Val-Ser-Leu-Tyr-Arg-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Nlu-Gly-Val-Tyr-NH2 (SEQ ID NO:
- 15);
- D-Pro-Ser-Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-Val-Gly, which is cyclized through a head-to-tail linkage (SEQ ID NO:
- 16);
- Suc-Val-Ser-Leu-Tyr-Arg-Asp-Pro-Ph5-Gly-Val-Abu-Gly-Glu-Met-Gly-Val-Tyr-NH2 (SEQ ID NO:
- 17);
- Suc-Val-Ser-Leu-Tyr-Arg-Asp-Pro-Leu-Gly-Val-Ala-Gly-Glu-Met-Gly-Val-Tyr-NH2 (SEQ ID NO:
- 18);
- Pro-Val-Ser-Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-Val-Tyr-D-Pro, which is cyclized through a head-to-tail linkage (SEQ ID NO:
- 19);
- Gly-Val-Ser-Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly-Val-Tyr-D-Pro, which is cyclized through a head-to-tail linkage (SEQ ID NO:
- 20);
- Leu-Tyr-Glu-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Gly, which is cyclized through a head-to-tail linkage (SEQ ID NO:
- 21);
- and
- Cys-Tyr-Arg-Asp-Pro-Leu-Gly-Val-Ala-Gly-Gly-Met-Cys, which is cyclized through a cysteine bridge (SEQ ID NO:
- 22).
42 more elements
(canceled)
Dependencies are inferred from the claim text.