公开(公告)号：US20240300900A1

公开(公告)日：2024-09-12

申请号：US18660802

申请日：2024-05-10

Applicant: Roche Diagnostics Operations, Inc.

Inventor： Frank Bergmann ,  Dieter Heindl ,  Nils Winter

IPC: C07D225/08 ,  A61K47/54 ,  A61K49/00 ,  A61K51/04

CPC classification number: C07D225/08 ,  A61K47/545 ,  A61K49/0052 ,  A61K51/044

Abstract: The invention relates in a first aspect to an azadibenzocyclooctyne derivative according to formula (I) or a salt thereof having specific substituents at the benzo rings of the DIBAC structure and having specific substituents connected to the nitrogen atom of the DIBAC structure. A second aspect of the invention is directed to a conjugate of formula (II), wherein a substituent R6 is connected to the N atom of the 8 membered ring of the DIBAC structure via a linker structure —C(═O)-[L]n-Z—. A third aspect of the invention relates to a method for the modification of a target molecule, wherein a conjugate according to the second aspect is reacted with a target molecule comprising a 1,3-dipole group or a 1,3-(hetero)diene group. In a fourth aspect, the invention is directed to the use of the conjugate according to the second aspect for bioorthogonal labeling and/or modification of a target molecule. A fifth aspect of the invention relates to a modified target molecule comprising the reaction product of a conjugate according to the second aspect and a target molecule comprising a 1,3-dipole group or a 1,3-(hetero)diene group, obtained or obtainable from the method of the third aspect. In a sixth aspect, the invention is related to a kit comprising a modified target molecule according to the fifth aspect as detector reagent and a suitable capture reagent.