公开(公告)号：US20230330258A1

公开(公告)日：2023-10-19

申请号：US18054018

申请日：2022-11-09

Applicant: Tubulis GmbH ,  Forschungsverbund Berlin e.V.

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

IPC: A61K47/68 ,  C07F9/30

CPC classification number: A61K47/6889 ,  C07F9/30

Abstract: 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：US20250049939A1

公开(公告)日：2025-02-13

申请号：US18717535

申请日：2022-12-12

Applicant: TUBULIS GmbH ,  LUDWIG-MAXIMILIANS-UNIVERSITAET MUENCHEN ,  FORSCHUNGSVERBUND BERLIN E.V. ,  Helmholtz Zentrum Muenchen Deutsches forschungszentrum für Gesundheit und Umwelt (GmbH)

Inventor： Heinrich LEONHARDT ,  Andreas STENGL ,  Maike ROAS ,  Jonathan SCHWACH ,  Karsten SPIEKERMANN ,  Harald POLZER ,  Marina ABLE ,  Jonas HELMA-SMETS ,  Dominik SCHUMACHER ,  Marcus GERLACH ,  Christian Peter Richard HACKENBERGER ,  Marc-André KASPER ,  Irmela JEREMIAS ,  Binje VICK ,  Elisabeth KREMMER

IPC: A61K47/68 ,  A61P35/02 ,  C07K16/28

Abstract: The present invention relates to novel anti-FLT3 antibodies for specifically targeting extracellular domain of FLT3. The present invention further relates to targeting FLT3 by novel antibody-drug-conjugates (ADCs) based on the novel anti-FLT3 antibodies of the present invention, especially in combination with kinase inhibitors, for use in therapy and/or for use in a method of cancer treatment (e.g., acute myeloid leukemia (AML) with or without internal tandem duplication (ITD) mutations in the FLT3 gene (FLT3-ITD)).

公开(公告)号：US20220193251A1

公开(公告)日：2022-06-23

申请号：US17559664

申请日：2021-12-22

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

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

IPC: A61K47/68

Abstract: 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

Applicant: FORSCHUNGSVERBUND BERLIN E.V.

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

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

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

Abstract: 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).