Di-substituted maleic amide linker for antibody drug conjugating and preparation method and use thereof
US10987430B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Nov 24, 2017 |
| Grant date | Apr 27, 2021 |
| Priority date | — |
| Expiry date | Nov 24, 2037 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K7/02
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.