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：US20240269313A1

公开(公告)日：2024-08-15

申请号：US18394303

申请日：2023-12-22

申请人： Tubulis GmbH

发明人： Marc-André KASPER ,  Philipp OCHTROP ,  Anil Pandurang JAGTAP ,  Swetlana WUNDER ,  Simon VOGT ,  Dominik SCHUMACHER ,  Jonas HELMA-SMETS

IPC分类号： A61K47/68 ,  A61K47/54 ,  A61P35/00

CPC分类号： A61K47/6889 ,  A61K47/548 ,  A61K47/68031 ,  A61K47/68033 ,  A61K47/68035 ,  A61K47/68037 ,  A61K47/6809 ,  A61K47/6851 ,  A61P35/00

摘要： The present invention relates to a conjugate having the formula (1):




wherein a receptor binding molecule (RBM) is connected with a drug moiety (D), the conjugate comprising a phosphorus(V) moiety. 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：US20230158154A1

公开(公告)日：2023-05-25

申请号：US18054063

申请日：2022-11-09

申请人： Tubulis GmbH

发明人： Marc-André KASPER ,  Paul MACHUI ,  Isabelle MAI ,  Annette VOGL ,  Saskia SCHMITT ,  Dominik SCHUMACHER ,  Jonas HELMA-SMETS

IPC分类号： A61K47/54 ,  A61K31/4745 ,  A61K47/68

CPC分类号： A61K47/545 ,  A61K31/4745 ,  A61K47/6803

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




wherein a receptor binding molecule (RBM) is connected with a camptothecin moiety (C). 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.