CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE

• Main Authors: XU YIFANG, YANG CHENGYU, LIN CHEN, XU JUN, ZHU HAIFENG, ZHAO ROBERT YONGXIN, GAI SHUN, YE HANGBO, YE ZHICANG, WANG CHUNYAN, GAO SHUIHONG, XIE HONGSHENG, GUO HUIHUI, YANG QINGLIANG, CHAO MINJUN, SU QINGYU, YANG YANLEI, HUANG YUANYUAN, ZHAO LINYAO, PENG JIE, ZUO XIAOTAO, LI WENJUN, ZHOU XIAOMAI, JIA JUNXIANG, GUO ZHIXIANG, CAI XIANG, TONG QIANQIAN
• Format: Patent
• Language: English; Korean
• Published: 08.10.2021
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

화학식 (I)에 나타낸 바와 같은 비스-링커(이중-링커)를 사용한 세포독성 분자 대 세포-결합 분자의 접합이 제공된다. 본 발명은 세포독성 약물 분자 대 세포-결합제의 접합체를 특별한 방식으로 제조하는 비스-링키지 방법을 제공한다. 본 발명은 또한 암, 또는 자가면역 질환, 또는 감염성 질환의 치료를 위한 접합체의 응용에 관한 것이다. A conjugation of a cytotoxic drug to a cell-binding molecule with a bis-linker (dual-linker) as shown in Formula (I). Bis-linkage methods of making a conjugate of a cytotoxic drug/molecule to a cell-binding agent in a specific manner are also described, as well as application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease.wherein "" is an optional bond; X, Y, Z1, and Z2 are a functional group; m1 and n are a integer; L1 and L2 are a linker.