Patent classifications
C07K7/52
NOVEL lNHIBITORS OF THE ENZYME ACTIVATED FACTOR XII (FXIIA)
The present invention relates to a bicyclic inhibitor of the coagulation enzyme activated factor XII (FXIIa) comprising or consisting of the peptide) (X.sup.1)(X.sup.2)(X.sup.3).sub.n(X.sup.4)RL(X.sup.5)(X.sup.6).sub.m(X.sup.7)(X.sup.9).sub.l(X.sup.10)(X.sup.11)(X.sup.12)(X.sup.13)(X.sup.14).sub.k(X.sup.15)(X.sup.16), wherein (X.sup.1) is present or absent and, if present, is an amino acid; (X.sup.2) is an amino acid with a side chain; (X.sup.3) is an amino acid and n is between 0 and 3, preferably 0 or 1 and most preferably 0; (X.sup.4) is an aliphatic L-amino acid or a cyclic L-amino acid, preferably L, P or an aromatic L-amino acid, and most preferably an aromatic L-amino acid; (X.sup.5) is an amino acid; (X.sup.6) is an amino acid and m is between 0 and 3, preferably 0 or 1 and most preferably 0; (X.sup.7) is an amino acid with a side chain; (X.sup.9) is an amino acid and l is between 0 and 3, preferably 0 or 1 and most preferably 0; (X.sup.10) is an amino acid; (X.sup.11) is an amino acid, preferably Q; (X.sup.12) is a hydrophobic L-amino acid, preferably an aliphatic L-amino acid, and is most preferably L; (X.sup.13) is an amino acid; (X.sup.14) is an amino acid and k is between 0 and 3, preferably 0 or 1 and most preferably 0, (X.sup.15) is an amino acid with a side chain; and (X.sup.16) is present or absent and, if present, is an amino acid; and wherein the side chains of (X.sup.2), (X.sup.7) and (X.sup.15) are connected via a connecting molecule, said connecting molecule having at least three functional groups, each functional group forming a covalent bond with one of the side chains of (X.sup.2), (X.sup.7) and (X.sup.15).
NOVEL lNHIBITORS OF THE ENZYME ACTIVATED FACTOR XII (FXIIA)
The present invention relates to a bicyclic inhibitor of the coagulation enzyme activated factor XII (FXIIa) comprising or consisting of the peptide) (X.sup.1)(X.sup.2)(X.sup.3).sub.n(X.sup.4)RL(X.sup.5)(X.sup.6).sub.m(X.sup.7)(X.sup.9).sub.l(X.sup.10)(X.sup.11)(X.sup.12)(X.sup.13)(X.sup.14).sub.k(X.sup.15)(X.sup.16), wherein (X.sup.1) is present or absent and, if present, is an amino acid; (X.sup.2) is an amino acid with a side chain; (X.sup.3) is an amino acid and n is between 0 and 3, preferably 0 or 1 and most preferably 0; (X.sup.4) is an aliphatic L-amino acid or a cyclic L-amino acid, preferably L, P or an aromatic L-amino acid, and most preferably an aromatic L-amino acid; (X.sup.5) is an amino acid; (X.sup.6) is an amino acid and m is between 0 and 3, preferably 0 or 1 and most preferably 0; (X.sup.7) is an amino acid with a side chain; (X.sup.9) is an amino acid and l is between 0 and 3, preferably 0 or 1 and most preferably 0; (X.sup.10) is an amino acid; (X.sup.11) is an amino acid, preferably Q; (X.sup.12) is a hydrophobic L-amino acid, preferably an aliphatic L-amino acid, and is most preferably L; (X.sup.13) is an amino acid; (X.sup.14) is an amino acid and k is between 0 and 3, preferably 0 or 1 and most preferably 0, (X.sup.15) is an amino acid with a side chain; and (X.sup.16) is present or absent and, if present, is an amino acid; and wherein the side chains of (X.sup.2), (X.sup.7) and (X.sup.15) are connected via a connecting molecule, said connecting molecule having at least three functional groups, each functional group forming a covalent bond with one of the side chains of (X.sup.2), (X.sup.7) and (X.sup.15).
Botulinum neurotoxin-specific capture agents, compositions, and methods of using and making
The present application provides stable peptide-based Botulinum neurotoxin (BoNT) serotype A capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing BoNT serotype A capture agents using iterative on-bead in situ click chemistry.
Botulinum neurotoxin-specific capture agents, compositions, and methods of using and making
The present application provides stable peptide-based Botulinum neurotoxin (BoNT) serotype A capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing BoNT serotype A capture agents using iterative on-bead in situ click chemistry.
Immunomodulators
The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
Immunomodulators
The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
BOTULINUM NEUROTOXIN-SPECIFIC CAPTURE AGENTS, COMPOSITIONS, AND METHODS OF USING AND MAKING
The present application provides stable peptide-based Botulinum neurotoxin (BoNT) serotype A capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing BoNT serotype A capture agents using iterative on-bead in situ click chemistry.
BOTULINUM NEUROTOXIN-SPECIFIC CAPTURE AGENTS, COMPOSITIONS, AND METHODS OF USING AND MAKING
The present application provides stable peptide-based Botulinum neurotoxin (BoNT) serotype A capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing BoNT serotype A capture agents using iterative on-bead in situ click chemistry.
METHOD OF DETECTING AUTO-ANTIBODIES FROM PATIENTS SUFFERING FROM RHEUMATOID ARTHRITIS, A PEPTIDE AND ASSAY KIT
Peptides useful in determining the presence of autoantibodies in patients suffering from rheumatoid arthritis are disclosed.
METHOD OF DETECTING AUTO-ANTIBODIES FROM PATIENTS SUFFERING FROM RHEUMATOID ARTHRITIS, A PEPTIDE AND ASSAY KIT
Peptides useful in determining the presence of autoantibodies in patients suffering from rheumatoid arthritis are disclosed.