DORONINA, SVETLANA O.,SENTER, PETER D.,TOKI, BRIAN E.,EBENS, ALLEN J.,KLINE, TONI BETH,POLAKIS, PAUL,SLIWKOWSKI, MARK X.,SPENCER, SUSAN D.
申请号：
ES12157783
公开号：
ES2534185T3
申请日:
2004.11.05
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
An antibody-drug conjugate having the formula: ** ** Formula or a pharmaceutically acceptable salt or solvate thereof, wherein: Ab is an antibody, R17 is C1-C10 alkylene, C3-C8- -carbociclo , -O- (C1-C8) -, -arylene-, -C1-C10-arylene, -arylene- C1-C10 alkylene, C1-C10 alkylene (C3-C8 carbocycle) -, - ( C3-C8 carbocycle) -C1-C10-, -heterocycle 3 -C 8, -C1-C10 alkylene- (C3-C8 heterocycle) -, - (C3 C8 heterocycle) -C1-C10 alkylene-, - (CH2CH2O) r-, or - (CH2CH2O) r-CH2- r is an integer ranging from 1 to 10 p ranges from 1 to about 20, and DF is a Drug unit having the formula: ** ** Formula wherein, independently for each position: R2 is selected from H and C1-C8 alkyl R3 is selected from H, C1-C8 alkyl, C3-C8 carbocycle, aryl, alkaryl C1-C8, C1-C8 alkyl- (C3-C8 carbocycle), C3-C8 heterocycle and C1-C8 alkyl- (C3 heterocycle C8) R4 is selected from H, C1-C8 alkyl, C3-C8 carbocycle, aryl, alkaryl C1-C8, C1-C8 alkyl- (C3-C8 carbocycle), C3-C8 heterocycle and C1-C8 alkyl- (C3 heterocycle C8) R5 is selected from H and methyl or: R4 and R5 together form a carbocyclic ring and have the formula - (CRaRb) n- wherein Ra and Rb are independently selected from H, C1-C8 alkyl and C3-C8 carbocycle and n is selected from 2, 3, 4, 5 and 6 R6 is selected from H and C1-C8 alkyl R7 is selected from H, C1-C8 alkyl, C3-C8 carbocycle, aryl, alkaryl C1-C8, C1-C8 alkyl- (C3-C8 carbocycle), C3-C8 heterocycle and C1-C8 alkyl- (C3 heterocycle C8) each R8 is independently selected from H, OH, C1-C8 alkyl, C3-C8 carbocycle and O- (C1-C8) R9 is selected from H and C1-C8 alkyl R10 is selected from aryl and C3-C8 heterocycle Z is O, S, NH or NR12, where R12 is C1 to C8-alkyl R11 is selected from -H, C1-C20 aryl, C3-C8 heterocycle, alkyl - (R13O) m-R14 or - (R13O) m-CH (R15) 2 m is an integer ranging from 1 to 1000 R13 is C2-C8 alkyl R14 is H or C1-C8 alkyl each occurrence of R15 is independently H, COOH, - (CH2) nN (R16) 2, - (CH2) n-SO3H, or - (CH2) n-SO3-C1-C8 each occurrence of R16 is independent
