Modified polybicyclic peptide ligands

• Main Authors: MUDD GEMMA, MCDONNELL KEVIN, VUBOTYE PATRICK
• Format: Patent
• Language: Chinese; English
• Published: 22.07.2022
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to a multimer of a polypeptide covalently bound to a molecular scaffold such that two or more peptide rings are present oppositely between the connection points of the scaffold, characterized in that the multimer binding complex additionally comprises a modifying group coupled thereto. Polymerization of a polypeptide using different connection points within the polypeptide through various chemical joints and hinges of different lengths and rigidities is also described. In particular, the present invention describes peptide multimers that are high affinity conjugates and activators of CD137. The invention also includes drug conjugates comprising the multimeric binding complexes coupled to one or more effector groups and/or functional groups, pharmaceutical compositions comprising the multimeric binding complexes and drug conjugates, and to the use of the multimeric binding complexes and drug conjugates in the prevention, inhibition or treatment of CD137 mediated diseases or disord