Specific topoisomerase inhibitor, antibody drug conjugate and preparation method of antibody drug conjugate

The invention discloses a specific topoisomerase inhibitor, an antibody drug conjugate and a preparation method of the antibody drug conjugate, and belongs to the technical field of medicinal chemistry. The inhibitor compound A or a tautomer, a mesomer, a raceme, an enantiomer, a diastereoisomer, or...

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Hauptverfasser: WANG FANGDAO, WANG DONG, WANG MENG
Format: Patent
Sprache:chi ; eng
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Beschreibung
Zusammenfassung:The invention discloses a specific topoisomerase inhibitor, an antibody drug conjugate and a preparation method of the antibody drug conjugate, and belongs to the technical field of medicinal chemistry. The inhibitor compound A or a tautomer, a mesomer, a raceme, an enantiomer, a diastereoisomer, or a mixture form thereof, or a pharmaceutically acceptable salt thereof, the structure of the compound A is the structure of the compound A, and the compound A can be further prepared into an antibody drug conjugate; the antibody drug conjugate provided by the invention has good solubility and druggability, and no precipitate is generated in the coupling process; aDC shows obvious in-vivo anti-tumor activity, and compared with a control sample, the ADC can show obviously stronger anti-tumor activity. 本发明公开了特异性拓扑异构酶抑制剂和可用于抗体药物偶联物及其制备方法,属于药物化学技术领域。所述抑制剂化合物A或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式,或其可药用的盐,化合物A结构为该化合物还可进一步制备得到抗体药物偶联物;本发明抗体药物偶联物具有很好溶解性和成药性,偶联过程不发生沉淀;ADC表现出明显体内抗肿瘤活性,与对照样品相比可以显示出显著更强抗肿瘤活性。