POLSON ANDREW,GUNZNER JANET L.,POLAKIS PAUL,MASTERSON LUKE,SPENCER SUSAN D.,FLYGARE JOHN A.,HOWARD PHILIP WILSON,RAAB HELGA E.,TIBERGHIEN ARNAUD
申请号：
NZ60224111
公开号：
NZ602241A
申请日:
2011.04.15
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
Disclosed herein are conjugates of Formula (AB), (AC), (EB) and (EC), wherein the variables are defined herein, for making conjugates which are pyrrolobenzopdiazepine (PBD) molecules linked via the N10 position to a cell binding agent, such as an antibody. The conjugates may be used for treating proliferative diseases like cancer. Exemplary conjugates include the following: (11S,11aS)-4-((S)-2-((S)-2-(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)-3-methylbutanamido )-5-ureidopentanamido)benzyl 11-hydroxy-7 -methoxy-8-((5-(((S)-7-methoxy-2-methylene-5-oxo-2,3,5,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl)oxy)pentyl)oxy)-2-methylene-5-oxo-2,3,11,11a-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-10(5H)-carboxylate and (MP-PEG8-Val-Ala-PAB-(imp)PBD (11S,11aS)-4-((2S,5S)-37-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-5-isopropyl-2-methyl-4,7,35-trioxo-10,13,16,19,22,25,28,31-octaoxa-3,6,34-triazaheptatriacontanamido )benzyl 11-hydroxy-8-(5-((11S,11aS)-11-hydroxy-10-((4-((10S,13S)-10-isopropyl-13-methyl-8,11-dioxo-2,5-dioxa-9,12-diazatetradecanamido)benzyloxy)carbonyl)-7-methoxy-2-methylene-5-oxo-2,3,5,10,11,11a-hexahydro-pyrrolobenzo[2,1-c][1,4]diazepin-8-yloxy)pentyloxy)-7-methoxy-2-methylene-5-oxo-2,3,11,11a-tetrahydro-pyrrolobenzo[2,1-c][1,4]diazepine-10(5H)-carboxylate).
