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：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).

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.