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Antibody coupled drug intermediates with maleimide connector, and synthesis method thereof

An antibody-conjugated drug-maleimide technology, which is applied in peptide preparation methods, antibody mimics/scaffolds, chemical instruments and methods, etc., can solve problems such as poor water solubility

Inactive Publication Date: 2020-08-07
LEVENA SUZHOU BIOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Another object of the present invention is to solve the problem of poor water solubility of ADC drugs, and provide a structure in which amino acid terminals are connected with hydrophilic polyethylene glycol chains, which can effectively improve the water solubility of ADC drugs

Method used

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  • Antibody coupled drug intermediates with maleimide connector, and synthesis method thereof
  • Antibody coupled drug intermediates with maleimide connector, and synthesis method thereof
  • Antibody coupled drug intermediates with maleimide connector, and synthesis method thereof

Examples

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Embodiment Construction

[0086] As used herein, commonly used abbreviations have their conventional meanings in the art.

[0087]

[0088]

[0089]

[0090] Having a maleimide linker means having a maleimide group.

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Abstract

The invention relates to the field of organic synthesis, and especially relates to a series of antibody coupled drug intermediates with a maleimide connector, and a synthesis method thereof. The intermediates are provided with the maleimide connector and can be rapidly subjected to a Michael addition reaction with sulfydryl groups on an antibody, antibody coupling is achieved, and cytotoxin is connected to the antibody.

Description

technical field [0001] The present invention relates to the field of organic synthesis, in particular to a series of antibody-drug coupling drug intermediates and synthesis methods thereof. Background technique [0002] Antibody drug conjugate (ADC) is a new type of anti-tumor drug. Its principle is to link cytotoxins to antibodies, recognize specific antigens on the surface of cancer cells through antibodies, and enter cancer cells through endocytosis. Cells, so as to transport cytotoxins to the target, to achieve the purpose of targeted treatment of malignant tumors. Compared with traditional small-molecule anti-tumor drugs, ADC is more specific and effective because it can rely on the target recognition of antibodies and the high activity of toxins. [0003] ADCs consist of three distinct components, namely antibodies, linkers and cytotoxins. The antibody achieves targeting, and the linker ensures the stability of the ADC during blood transport, and after reaching the t...

Claims

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Application Information

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IPC IPC(8): C07K5/062C07K5/103C07K1/00C07D491/22
CPCC07D491/22C07K5/06052C07K5/1008C07K2319/00
Inventor 许喆李海泓王威威戚文科王相明孔令配郭茂君李辉
Owner LEVENA SUZHOU BIOPHARMA CO LTD
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