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    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR NECTIN-4
    2.
    发明申请
    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR NECTIN-4 审中-公开

    公开(公告)号：US20190389906A1

    公开(公告)日：2019-12-26

    申请号：US16446901

    申请日：2019-06-20

    Applicant: BicycleTx Limited

    Inventor： Paul Beswick ,  Liuhong Chen ,  Gemma Mudd ,  Peter Park ,  Katerine Van Rietschoten ,  Michael Rigby

    IPC: C07K7/08 ,  A61K47/55 ,  A61K47/65 ,  A61P35/00

    Abstract: The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of Nectin-4. The invention also includes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands and drug conjugates and to the use of said peptide ligands and drug conjugates in preventing, suppressing or treating a disease or disorder mediated by Nectin-4.

    PEPTIDE LIGANDS FOR BINDING TO MT1-MMP
    7.
    发明申请
    PEPTIDE LIGANDS FOR BINDING TO MT1-MMP 审中-公开

    公开(公告)号：US20190389907A1

    公开(公告)日：2019-12-26

    申请号：US16472234

    申请日：2017-12-20

    Applicant: BicycleTx Limited

    Inventor： Daniel Teufel ,  Gemma Mudd ,  Silvia Pavan

    IPC: C07K7/08 ,  G01N33/573 ,  A61K47/64

    Abstract: A peptide ligand specific for MT1-MMP comprising a polypeptide comprising two diaminopropionic acid (Dap) or N-alkyldiaminopropionic acid (N-AlkDap) residues, and a third residue selected from cysteine, Dap or N-AlkDap, separated by at least two loop sequences, and a molecular scaffold, the peptide being linked to the scaffold by covalent alkylamino linkages with the Dap or N-AlkDap residues of the polypeptide and by covalent thioether linkages with the cysteine when the third residue is cysteine, such that two polypeptide loops are formed on the molecular scaffold, wherein the peptide ligand comprises an amino acid sequence of formula (II): -A1-X1-U/O2-X3-X4-G5-A2-E6-D7-F8-Y9-X10-X11-A3- (SEQ ID NO: 1) (II) or a pharmaceutically acceptable salt thereof; wherein: A1, A2, and A3 are independently cysteine, L-2,3-diaminopropionic acid (Dap), N-beta-alkyl-L-2,3-diaminopropionic acid (N-AlkDap), or N-beta-haloalkyl-L-2,3-diaminopropionic acid (N-HAlkDap), provided that at least one of A1, A2, and A3 is Dap, N-AlkDap or N-HAlkDap; X represents any amino acid residue; U represents a polar, uncharged amino acid residue selected from N, C, Q, M, S and T; and O represents a non-polar aliphatic amino acid residue selected from G, A, I, L, P and V.

    Bicyclic peptide ligands specific for P-selectin
    8.
    发明授权
    Bicyclic peptide ligands specific for P-selectin 有权

    公开(公告)号：US12150998B2

    公开(公告)日：2024-11-26

    申请号：US17659934

    申请日：2022-04-20

    Applicant: BicycleTx Limited

    Inventor： Kevin McDonnell ,  Gemma Mudd ,  Michael Skynner ,  Sophie Watcham

    IPC: C07K7/00 ,  A61K47/64 ,  C07K7/06 ,  C07K14/745

    Abstract: The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which bind to P-selectin. The invention also relates to multimeric binding complexes of polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold that are binders of P-selectin. The invention also includes drug conjugates comprising said peptides and complexes, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands, complexes and drug conjugates and the use of said peptide ligands and drug conjugates in preventing, suppressing or treating a disease or disorder mediated by a cell adhesion molecule, such as P-selectin, including vaso-occlusive crisis and sickle cell disease-related conditions, cancer, or COVID-19.

    Peptide derivatives having novel linkage structures
    9.
    发明授权
    Peptide derivatives having novel linkage structures 有权

    公开(公告)号：US11730819B2

    公开(公告)日：2023-08-22

    申请号：US16472242

    申请日：2017-12-20

    Applicant: BicycleTx Limited

    Inventor： Daniel Teufel ,  Gemma Mudd ,  Silvia Pavan

    IPC: A61K47/64 ,  A61K47/65 ,  C07K7/54

    CPC classification number: A61K47/64 ,  A61K47/65 ,  C07K7/54

    Abstract: A compound comprising at least one looped peptide structure attached via at least one alkylamino linkage to a scaffold. Preferably the looped peptide structure is a Bicycle structure comprising two peptide loops attached to the scaffold via two alkylamino linkages and one thioether linkage, one of the linkages being common to both loops. Also provided is a method of making a compound comprising at least one looped peptide structure attached via at least one alkylamino linkages to a scaffold, the method comprising: providing a peptide having at least two residues selected from cysteine, diaminopropionic acid, D-N-Alkyldiaminopropionic acid and β-N-Alkyldiaminopropionic acid, provided that at least one of the residues is diaminopropionic acid, D-N-Alkyldiaminopropionic acid and β-N-Alkyldiaminopropionic acid; providing a scaffold molecule having at least two reactive sites for forming alkylamino or thioether linkages with the said at least two residues; and forming said linkages between the peptide and the scaffold molecule.

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