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公开(公告)号:US11453703B2
公开(公告)日:2022-09-27
申请号:US16372692
申请日:2019-04-02
Applicant: BicycleTX Limited
Inventor: Nicholas Keen , Kevin McDonnell , Peter Park , Punit Upadhyaya , Gemma Mudd
IPC: C07K14/00 , A61K38/12 , C07K7/08 , A61P35/00 , C07K7/50 , A61K38/00 , C07K7/06 , C07K14/705 , C07K14/715 , C07K17/08
Abstract: The present invention relates to heterotandem bicyclic peptide complexes which comprise a first peptide ligand, which binds to a component present on an immune cell, conjugated via a linker to a second peptide ligand, which binds to a component present on a cancer cell. The invention also relates to the use of said heterotandem bicyclic peptide complexes in preventing, suppressing or treating cancer.
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公开(公告)号:US20220275053A1
公开(公告)日:2022-09-01
申请号:US17630754
申请日:2020-08-13
Applicant: BicycleTx Limited
Inventor: Punit UPADHYAYA , Gemma Elizabeth MUDD , Kevin MCDONNELL
IPC: C07K14/705 , A61K47/64 , C07K7/06 , A61P35/00
Abstract: 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).
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公开(公告)号:US20220257784A1
公开(公告)日:2022-08-18
申请号:US17630314
申请日:2020-07-30
Applicant: BicycleTx Limited
Inventor: Punit UPADHYAYA , Johanna LAHDENRANTA , Gemma MUDD , Kevin MCDONNELL
Abstract: 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).
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公开(公告)号:US20220213145A1
公开(公告)日:2022-07-07
申请号:US17648560
申请日:2022-01-21
Applicant: BicycleTx Limited
Inventor: Liuhong CHEN , Rachid LANI , Kevin MCDONNELL , Gemma Elizabeth MUDD , Peter PARK
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 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.
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公开(公告)号:US20220194988A1
公开(公告)日:2022-06-23
申请号:US17454665
申请日:2021-11-12
Applicant: BicycleTx Limited
Inventor: Ellen GOWANS , Gemma Elizabeth MUDD , Michael RIGBY , Punit SETH , Michael SKYNNER , Steven STANWAY , Liudvikas URBONAS , Katerine VAN RIETSCHOTEN
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 TfR1. The invention also relates to multimeric binding complexes which comprise at least two of said bicyclic peptide ligands. The invention also includes pharmaceutical compositions comprising said peptide ligands and multimeric binding complexes and the use of said peptide ligands, and multimeric binding complexes and pharmaceutical compositions in preventing, suppressing or treating a disease or disorder through TfR1 mediated delivery of a therapeutic agent.
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公开(公告)号:US20220194983A1
公开(公告)日:2022-06-23
申请号:US17254339
申请日:2019-06-19
Applicant: BicycleTx Limited
Inventor: Daniel TEUFEL , Gemma MUDD , Silvia PAVAN , Kevin MCDONNELL , Punit UPADHYAYA
Abstract: 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.
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公开(公告)号:US20220064221A1
公开(公告)日:2022-03-03
申请号:US17422935
申请日:2020-01-15
Applicant: BicycleTx Limited
Inventor: Rachid LANI , Catherine STACE , Daniel TEUFEL , Edward WALKER
Abstract: 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 integrin αvβ3. 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 integrin αvβ3.
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公开(公告)号:US20210147484A1
公开(公告)日:2021-05-20
申请号:US17082075
申请日:2020-10-28
Applicant: BicycleTx Limited
Inventor: Paul BESWICK , Gemma Elizabeth Mudd , Kevin McDonnell , Gabriela Ivanova-Berndt , Katerine Van Rietschoten , David Witty , Michael Skynner
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
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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.
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公开(公告)号:US20190184025A1
公开(公告)日:2019-06-20
申请号:US16220685
申请日:2018-12-14
Applicant: BicycleTx Limited
Inventor: Liuhong Chen , Philip Huxley , Silvia Pavan , Katerine Van Rietschoten
CPC classification number: A61K47/6415 , A61K38/05 , A61K38/10 , A61K47/62 , A61K47/65 , A61P35/00 , C07K7/08
Abstract: 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 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 characterised by overexpression of EphA2 in diseased tissue (such as a tumour).
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