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公开(公告)号:US20220024982A1
公开(公告)日:2022-01-27
申请号:US17309626
申请日:2019-12-13
Applicant: BicycleTx Limited
Inventor: Liuhong CHEN , Euan RICHARDS , Rachid LANI , Gemma MUDD , Catherine STACE , Daniel TEUFEL , Edward WALKER
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 membrane type 1 metalloprotease (MT1-MMP). The invention also describes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups which have utility in imaging and targeted cancer therapy.
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公开(公告)号:US20200255477A1
公开(公告)日:2020-08-13
申请号:US16636105
申请日:2018-08-03
Applicant: BicycleTx Limited
Inventor: Liuhong Chen , Rachid Lani , Kevin McDonnell , Gemma 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:US20240400616A1
公开(公告)日:2024-12-05
申请号:US18427414
申请日:2024-01-30
Applicant: BicycleTx Limited
Inventor: Paul BESWICK , Liuhong CHEN , Gemma MUDD , Peter PARK , Katerine VAN RIETSCHOTEN , Michael RIGBY
IPC: C07K7/08 , A61K31/40 , A61K31/5375 , A61K38/00 , A61K38/10 , A61K47/55 , A61K47/64 , 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.
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公开(公告)号:US20240336656A1
公开(公告)日:2024-10-10
申请号:US18424386
申请日:2024-01-26
Applicant: BicycleTx Limited
Inventor: Gemma MUDD , Punit Upadhyaya , Kevin McDonnell , Johanna Lahdenranta
IPC: C07K7/08 , A61K9/00 , A61K38/00 , A61K38/12 , A61K47/64 , A61P35/00 , C07K11/02 , C07K14/00 , C07K14/705
CPC classification number: C07K7/08 , A61K9/0019 , A61K38/12 , A61K47/641 , A61P35/00 , C07K11/02 , C07K14/001 , C07K14/70578 , A61K38/00
Abstract: The present invention relates to a heterotandem bicyclic peptide complex which comprises a first peptide ligand, which binds to Nectin-4, conjugated via a linker to two second peptide ligands, which bind to CD137. The invention also relates to the use of said heterotandem bicyclic peptide complex in preventing, suppressing or treating cancer.
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公开(公告)号:US11970553B2
公开(公告)日:2024-04-30
申请号:US17592966
申请日:2022-02-04
Applicant: BicycleTx Limited
Inventor: Gemma Mudd , Punit Upadhyaya , Kevin McDonnell , Johanna Lahdenranta
IPC: C07K7/08 , A61K9/00 , A61K38/12 , A61K47/64 , A61P35/00 , C07K11/02 , C07K14/00 , C07K14/705 , A61K38/00
CPC classification number: C07K7/08 , A61K9/0019 , A61K38/12 , A61K47/641 , A61P35/00 , C07K11/02 , C07K14/001 , C07K14/70578 , A61K38/00
Abstract: The present invention relates to a heterotandem bicyclic peptide complex which comprises a first peptide ligand, which binds to Nectin-4, conjugated via a linker to two second peptide ligands, which bind to CD137. The invention also relates to the use of said heterotandem bicyclic peptide complex in preventing, suppressing or treating cancer.
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公开(公告)号:US11833211B2
公开(公告)日:2023-12-05
申请号:US17934896
申请日:2022-09-23
Applicant: BicycleTx Limited
Inventor: Liuhong Chen , Philip Huxley , Silvia Pavan , Katerine Van Rietschoten
CPC classification number: A61K47/6415 , A61K38/05 , A61K38/10 , A61K47/62 , A61K47/64 , 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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公开(公告)号:US20230340020A1
公开(公告)日:2023-10-26
申请号:US17946380
申请日:2022-09-16
Applicant: BicycleTX Limited
Inventor: Daniel TEUFEL , Gemma MUDD , Silvia PAVAN
IPC: C07K7/08 , A61K47/64 , G01N33/573
CPC classification number: C07K7/08 , A61K47/64 , A61K47/6415 , G01N33/573
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:US20230039677A1
公开(公告)日:2023-02-09
申请号:US17782931
申请日:2020-12-16
Applicant: BicycleTx Limited
Inventor: Paul BESWICK , Gemma MUDD
Abstract: The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of IL-17. 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 IL-17.
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公开(公告)号:US11484602B2
公开(公告)日:2022-11-01
申请号:US16220685
申请日:2018-12-14
Applicant: BicycleTx Limited
Inventor: Liuhong Chen , Philip Huxley , Silvia Pavan , Katerine Van Rietschoten
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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公开(公告)号:US20220339289A1
公开(公告)日:2022-10-27
申请号:US17659934
申请日:2022-04-20
Applicant: BicycleTx Limited
Inventor: Kevin MCDONNELL , Gemma MUDD , Michael SKYNNER , Sophie WATCHAM
IPC: 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.
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