LU, JUI MEI,吕瑞梅,呂瑞梅,CHANG, MAY HUA,张美华,張美華,HWANG, JENN TSANG,黄振仓,黃振倉,CHENG, PING FU,郑平福,鄭平福,CHANG, LI WEN,张瓈文,張瓈文,KO, YI JU,柯怡如,柯怡如,HUNG, CHI Y,洪集英,洪集英,LIU, CHUN MIN,刘俊旻,劉俊旻,FAN, CHIA YU,范佳玉,范佳玉
申请号：
TW106144499
公开号：
TW201822820A
申请日:
2017.12.15
申请国别(地区):
TW
年份:
2018
代理人:
摘要：
A linker-drug represented by formula (I) is provided. In formula (I), C is a conjugating linker L is a linker unit D is a drug unit and m is an integer ranging from 1 to 4. The structure of the conjugator is represented by formula (II). In formula (II), X is a leaving group, both of R1 and R2 are single bond or -NH- Z is aryl, substituted aryl, heteroaryl, substituted heteroaryl, linear alkyl, cycloalkyl, heterocycloalkyl, or a combination thereof. The wave line of formula (II) indicates the covalent attachment site to L. An antibody-drug conjugate (ADC) employing the above linker-drug is also provided.C-(L-D)m (I)本揭露提供一種如化學式(I)所示之連接子藥物。於化學式(I)中,C為一接合連接子,L為一連接子單元,D為一藥物單元,且m為從1至4之整數。接合連接子的結構如化學式(II)所示。於化學式(II)中,X為一離去基,R1和R2同時為一單鍵或-NH-,Z為芳基、經取代的芳基、雜芳基、經取代的雜芳基、直鏈烷基、環烷基、雜環烷基、或前述之組合物。化學式(II)中的波浪線表示與L的共價連接位。本揭露也提供一種抗體藥物複合物(ADC)。C-(L-D)m (I)
