公开(公告)号：US20240398965A1

公开(公告)日：2024-12-05

申请号：US18698562

申请日：2022-10-06

Applicant: BicycleTx Limited

Inventor： Paul John Beswick ,  Gemma Elizabeth Mudd

IPC: A61K47/64 ,  A61P35/00

Abstract: The present invention relates to drug conjugates comprising two cytotoxic agents conjugated to a peptide ligand. The invention also relates to pharmaceutical compositions comprising said drug conjugates and to the use of said drug conjugates in preventing, suppressing or treating diseases, such as those which may be alleviated by cell death, in particular diseases characterised by defective cell types, proliferative disorders such as cancer and autoimmune disorders such as rheumatoid arthritis.

公开(公告)号：US20240391959A1

公开(公告)日：2024-11-28

申请号：US18610009

申请日：2024-03-19

Applicant: BicycleTx Limited

Inventor： Ellen GOWANS ,  Gemma Elizabeth MUDD ,  Michael RIGBY ,  Punit SETH ,  Michael SKYNNER ,  Steven STANWAY ,  Liudvikas URBONAS ,  Katerine VAN RIETSCHOTEN

IPC: C07K7/64 ,  A61K47/55 ,  A61K47/64 ,  C07K1/107

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.

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.

公开(公告)号：US12049520B2

公开(公告)日：2024-07-30

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

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

CPC classification number: 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：US20240189436A1

公开(公告)日：2024-06-13

申请号：US18499739

申请日：2023-11-01

Applicant: BicycleTx Limited

Inventor： Liuhong CHEN ,  Philip HUXLEY ,  Silvia PAVAN ,  Katerine VAN RIETSCHOTEN

IPC: A61K47/64 ,  A61K38/05 ,  A61K38/10 ,  A61K47/62 ,  A61K47/65 ,  A61P35/00 ,  C07K7/08

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).

公开(公告)号：US20230287047A1

公开(公告)日：2023-09-14

申请号：US17820286

申请日：2022-08-17

Applicant: BicycleTx Limited

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

IPC: C07K7/08 ,  A61K47/65 ,  A61K47/55 ,  A61P35/00 ,  A61K47/64 ,  A61K38/10

CPC classification number: C07K7/08 ,  A61K47/65 ,  A61K47/55 ,  A61P35/00 ,  A61K47/64 ,  A61K38/10 ,  A61K31/40

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：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.

公开(公告)号：US20230233698A1

公开(公告)日：2023-07-27

申请号：US18001374

申请日：2021-06-11

Applicant: BicycleTx Limited

Inventor： Gavin BENNETT ,  Stephen BLAKEMORE ,  Carly CAMPBELL ,  Michael RIGBY

IPC: A61K47/64 ,  C07K16/28 ,  A61K47/65 ,  A61P35/00 ,  G01N33/574

CPC classification number: A61K47/6415 ,  C07K16/2866 ,  A61K47/65 ,  A61P35/00 ,  G01N33/57484

Abstract: The present invention relates to a Bicycle toxin conjugate BT5528, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof, and uses thereof.

公开(公告)号：US20230220008A1

公开(公告)日：2023-07-13

申请号：US18055255

申请日：2022-11-14

Applicant: BicycleTx Limited

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

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

CPC classification number: C07K7/08 ,  C07K17/02 ,  A61K47/59 ,  C07K14/70575 ,  A61K47/66 ,  A61K47/60 ,  C07K2/00 ,  A61K47/64 ,  C07K17/14 ,  C07K7/64 ,  A61P35/00 ,  A61K47/54 ,  C07K2319/00

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. 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：US11696956B2

公开(公告)日：2023-07-11

申请号：US16771186

申请日：2018-12-19

Applicant: BicycleTx Limited

Inventor： Liuhong Chen ,  Philip Huxley ,  Silvia Pavan ,  Katerine Van Rietschoten

IPC: A61K47/64 ,  A61K38/10 ,  C07K7/08 ,  A61P35/00 ,  A61K47/65 ,  A61K38/05 ,  A61K47/62

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).