公开(公告)号：US20230330258A1

公开(公告)日：2023-10-19

申请号：US18054018

申请日：2022-11-09

申请人： Tubulis GmbH ,  Forschungsverbund Berlin e.V.

发明人： Christian HACKENBERGER ,  Marc-André KASPER ,  Philipp OCHTROP ,  Jahaziel JAHZERAH ,  Paul MACHUI ,  Dominik SCHUMACHER ,  Jonas HELMA-SMETS ,  Isabelle MAI

IPC分类号： A61K47/68 ,  C07F9/30

CPC分类号： A61K47/6889 ,  C07F9/30

摘要： The present invention relates to a conjugate having the formula (I):





wherein a receptor binding molecule (RBM) is connected with a drug moiety (D). The present invention also relates to intermediates for producing the same, methods of preparing the same, pharmaceutical compositions comprising the same, as well as uses thereof.

公开(公告)号：US20220193251A1

公开(公告)日：2022-06-23

申请号：US17559664

申请日：2021-12-22

申请人： Ludwig-Maximilians-Universitaet Muenchen ,  Forschungsverbund Berlin e.V.

发明人： Heinrich LEONHARDT ,  Jonas HELMA-SMETS ,  Dominik SCHUMACHER ,  Marcus GERLACH ,  Christian PR HACKENBERGER ,  Marc-André KASPER

IPC分类号： A61K47/68

摘要： The present invention relates to an antibody-drug conjugate (ADC) comprising: (a) Brentuximab, wherein Brentuximab comprises at the C-terminus of the light chains, the heavy chains or all of the heavy and light chains of the Brentuximab a recognition sequence for tubulin tyrosine ligase and a non-natural amino acid; and (b) at least one drug moiety; wherein a drug moiety is coupled to each of the non-natural amino acids via a linker. The present invention further relates to methods of producing same, pharmaceutical compositions comprising same as well as uses thereof.

公开(公告)号：US20240350655A1

公开(公告)日：2024-10-24

申请号：US18556602

申请日：2022-04-22

申请人： FORSCHUNGSVERBUND BERLIN E.V.

发明人： Christian Ewald STIEGER ,  Christian Peter Richard HACKENBERGER ,  Marc-André KASPER ,  Philipp OCHTROP

IPC分类号： A61K47/68 ,  A61K47/54 ,  C07F9/32 ,  C07F9/6518 ,  C07F9/6524 ,  C07F9/653 ,  C07F9/6558 ,  C07F9/6561

CPC分类号： A61K47/6851 ,  A61K47/548 ,  A61K47/68031 ,  C07F9/3217 ,  C07F9/6518 ,  C07F9/6524 ,  C07F9/65324 ,  C07F9/65583 ,  C07F9/65586 ,  C07F9/6561

摘要： Disclosed are novel conjugates and methods for the preparation thereof. One of the methods for the preparation of a conjugate comprises a step of: acting a compound of formula (I), with a thiol-containing molecule of formula (II), wherein represents an amino acid, a peptide, a protein, an antibody, a nucleotide, an oligonucleotide, a saccharide, a polysaccharide, a polymer, a small molecule, an optionally substituted C1-C8-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5- or 6-membered heterocyclic system; resulting in a compound of formula (III).