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    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR PD-L1
    5.
    发明申请
    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR PD-L1 有权

    公开(公告)号：US20220306689A9

    公开(公告)日：2022-09-29

    申请号：US17044868

    申请日：2019-12-23

    申请人： BicycleTx Limited

    发明人： Liuhong CHEN ,  James COOKE ,  Kevin MCDONNELL ,  Gemma MUDD ,  Katerine VAN RIETSCHOTEN ,  Punit UPADHYAYA

    IPC分类号： C07K7/08 ,  A61K47/64

    摘要： The present invention relates to polypeptides which are covalently bound to non-aromatic 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 PD-L1. 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 PD-L1.

    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR PD-L1
    6.
    发明申请
    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR PD-L1 有权

    公开(公告)号：US20220088207A1

    公开(公告)日：2022-03-24

    申请号：US17416562

    申请日：2019-12-23

    申请人： BicycleTx Limited

    发明人： Liuhong CHEN ,  James COOKE ,  Kevin MCDONNELL ,  Gemma MUDD ,  Katerine VAN RIETSCHOTEN ,  Punit UPADHYAYA

    IPC分类号： A61K47/64 ,  C07K7/64

    摘要： The present invention relates to polypeptides which are covalently bound to aromatic 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 PD-L1. 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 PD-L1.

    MULTIMERIC BICYCLIC PEPTIDE LIGANDS
    7.
    发明申请
    MULTIMERIC BICYCLIC PEPTIDE LIGANDS 有权

    公开(公告)号：US20210101933A1

    公开(公告)日：2021-04-08

    申请号：US17080021

    申请日：2020-10-26

    申请人： BicycleTx Limited

    发明人： Liuhong CHEN ,  Rachid LANI ,  Kevin MCDONNELL ,  Gemma MUDD ,  Peter U. PARK ,  Punit UPADHYAYA

    IPC分类号： C07K7/08 ,  A61K47/59 ,  A61K47/60 ,  A61K47/64 ,  A61K47/66 ,  A61P35/00 ,  C07K7/64 ,  C07K14/705 ,  C07K17/02 ,  C07K17/14 ,  C07K2/00

    摘要： The present invention relates to multimers of polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. The invention also describes the multimerization of polypeptides through various chemical linkers and hinges of various lengths and rigidity using different sites of attachments within polypeptides. In particular, the invention describes multimers of peptides which are high affinity binders and activators of CD137. 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 CD137.

    MODIFIED MULTIMERIC BICYCLIC PEPTIDE LIGANDS
    8.
    发明申请
    MODIFIED MULTIMERIC BICYCLIC PEPTIDE LIGANDS 有权

    公开(公告)号：US20220275053A1

    公开(公告)日：2022-09-01

    申请号：US17630754

    申请日：2020-08-13

    申请人： BicycleTx Limited

    发明人： Punit UPADHYAYA ,  Gemma Elizabeth MUDD ,  Kevin MCDONNELL

    IPC分类号： C07K14/705 ,  A61K47/64 ,  C07K7/06 ,  A61P35/00

    摘要： The present invention relates to multimers of polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold, characterised in that said multimeric binding complex additionally comprises a modifier group conjugated thereto. The invention also describes the multimerization of polypeptides through various chemical linkers and hinges of various lengths and rigidity using different sites of attachments within polypeptides. In particular, the invention describes multimers of peptides which are high affinity binders and activators of CD137. The invention also includes drug conjugates comprising said multimeric binding complexes, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said multimeric binding complexes and drug conjugates and to the use of said multimeric binding complexes and drug conjugates in preventing, suppressing or treating a disease or disorder mediated by CD137 and to the use in an analytical method (i.e. as a tracer or a tag).

    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR EPHA2
    9.
    发明申请
    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR EPHA2 有权

    公开(公告)号：US20220257784A1

    公开(公告)日：2022-08-18

    申请号：US17630314

    申请日：2020-07-30

    申请人： BicycleTx Limited

    发明人： Punit UPADHYAYA ,  Johanna LAHDENRANTA ,  Gemma MUDD ,  Kevin MCDONNELL

    IPC分类号： A61K47/64 ,  C07K14/00 ,  C07K11/02

    摘要： The present invention relates to polypeptides which are covalently bound to non-aromatic 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 the Eph receptor tyrosine kinase A2 (EphA2). The invention also relates to pharmaceutical compositions comprising said peptide ligands and to the use of said peptide ligands in preventing, suppressing or treating a disease or disorder characterised by overexpression of EphA2 in diseased tissue (such as a tumour).

    PEPTIDE LIGANDS FOR BINDING TO PSMA
    10.
    发明申请
    PEPTIDE LIGANDS FOR BINDING TO PSMA 有权

    公开(公告)号：US20220194983A1

    公开(公告)日：2022-06-23

    申请号：US17254339

    申请日：2019-06-19

    申请人： BicycleTx Limited

    发明人： Daniel TEUFEL ,  Gemma MUDD ,  Silvia PAVAN ,  Kevin MCDONNELL ,  Punit UPADHYAYA

    IPC分类号： C07K7/08 ,  A61K47/64 ,  A61P35/00

    摘要： A peptide ligand specific for prostate specific membrane antigen (PSMA) comprising a polypeptide comprising three residues selected from cysteine, L-2,3-diaminopropionic acid (Dap), N-beta-alkyl-L-2,3-diaminopropionic acid (N-AlkDap) and N-beta-haloalkyl-L-2,3-diaminopropionic acid (N-HAlkDap), with the proviso that at least one of said three residues is selected from Dap, N-AlkDap or N-HAlkDap, the said three residues being 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 or N-HAlkDap residues of the polypeptide and by thioether linkages with the cysteine residues of the polypeptide when the said three residues include cysteine, such that two polypeptide loops are formed on the molecular scaffold.