公开(公告)号：US20230086865A1

公开(公告)日：2023-03-23

申请号：US17802382

申请日：2021-02-26

Applicant: BicycleTx Limited

Inventor： Matthew BALMFORD ,  Paul BESWICK ,  Mike DAWSON ,  Rachel DODS ,  Catherine ROWLAND ,  Michael SKYNNER ,  Katerine VANRIETSCHOTEN ,  James WAGSTAFF

IPC: A61K47/64 ,  C07K7/64 ,  C07K7/08 ,  C07K14/195

Abstract: The present invention relates to a 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 bicyclic peptides of the invention are conjugated to a carrier peptide in order to greatly enhance the bacterial cell killing activity. More particularly, the invention describes peptides which are high affinity binders of penicillin-binding proteins (PBPs), such as PBP3 and PBP3a. The invention also includes pharmaceutical compositions comprising said conjugates and to the use of said conjugates in suppressing or treating a disease or disorder mediated by bacterial infection or for providing prophylaxis to a subject at risk of infection.

公开(公告)号：US11542304B2

公开(公告)日：2023-01-03

申请号：US17080021

申请日：2020-10-26

Applicant: BicycleTx Limited

Inventor： Liuhong Chen ,  Rachid Lani ,  Kevin Mcdonnell ,  Gemma Mudd ,  Peter U. Park ,  Punit Upadhyaya

IPC: C07K7/08 ,  C07K7/64 ,  C07K2/00 ,  A61K47/64 ,  A61K47/66 ,  A61P35/00 ,  C07K17/02 ,  A61K47/60 ,  C07K17/14 ,  A61K47/59 ,  C07K14/705 ,  A61K47/54

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. 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.

公开(公告)号：US11261214B2

公开(公告)日：2022-03-01

申请号：US16636105

申请日：2018-08-03

Applicant: BicycleTx Limited

Inventor： Liuhong Chen ,  Rachid Lani ,  Kevin McDonnell ,  Gemma Mudd ,  Peter Park

IPC: C07K7/64 ,  A61K47/64 ,  A61K38/00

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 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.

公开(公告)号：US20210299210A2

公开(公告)日：2021-09-30

申请号：US16372692

申请日：2019-04-02

Applicant: BicycleTx Limited

Inventor： Nicholas Keen ,  Kevin McDonnell ,  Peter Park ,  Punit Upadhyaya

IPC: A61K38/12 ,  C07K7/08 ,  C07K7/06 ,  C07K7/50 ,  A61P35/00

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.

公开(公告)号：US20210269480A1

公开(公告)日：2021-09-02

申请号：US17252038

申请日：2019-06-21

Applicant: BicycleTx Limited

Inventor： Paul BESWICK ,  Liuhong CHEN ,  Gemma Elizabeth MUDD ,  Peter PARK ,  Katerine VAN RIETSCHOTEN ,  Michael RIGBY

IPC: C07K7/08 ,  A61K47/64 ,  A61K38/10 ,  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.

公开(公告)号：US20210147485A1

公开(公告)日：2021-05-20

申请号：US17254464

申请日：2019-06-18

Applicant: BicycleTx Limited

Inventor： Daniel TEUFEL ,  Gemma MUDD ,  Silvia PAVAN

IPC: C07K7/08 ,  A61K47/64

Abstract: A peptide ligand specific for integrin αvβ3 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 a formed on the molecular scaffold. Also provided are drug conjugates comprising the peptide ligands conjugated to one or more effector groups and pharmaceutical compositions comprising the conjugates.

公开(公告)号：US20210101937A1

公开(公告)日：2021-04-08

申请号：US17062662

申请日：2020-10-05

Applicant: BicycleTx Limited

Inventor： Gemma MUDD ,  Punit Upadhyaya ,  Kevin McDonnell

IPC: C07K11/02

Abstract: The present invention relates to heterotandem bicyclic peptide complexes which comprise a first peptide ligand, which binds to a component present on a cancer cell, conjugated via a linker to a second peptide ligand, which binds to a component present on an immune cell. The invention also relates to the use of said heterotandem bicyclic peptide complexes in preventing, suppressing or treating cancer.

公开(公告)号：US20210040154A1

公开(公告)日：2021-02-11

申请号：US16941614

申请日：2020-07-29

Applicant: BicycleTx Limited

Inventor： Gemma MUDD ,  Punit UPADHYAYA ,  Kevin MCDONNELL ,  Johanna LAHDENRANTA

IPC: C07K7/08 ,  A61P35/00

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.

公开(公告)号：US10857196B2

公开(公告)日：2020-12-08

申请号：US15964599

申请日：2018-04-27

Applicant: BicycleTx Limited

Inventor： Paul John Beswick ,  Gabriela Ivanova-Berndt ,  Gemma Elizabeth Mudd ,  Silvia Pavan ,  Michael Skynner ,  Daniel Paul Teufel ,  Katerine Van Rietschoten

IPC: A61K38/00 ,  A61P35/00 ,  A61K47/10 ,  A61K38/12 ,  C12N9/64 ,  C07K7/08 ,  C12N9/88 ,  C07K7/64 ,  A61K47/62 ,  A61K38/10

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.