DOROSKI MATTHEW DAVID,MADERNA ANDREAS,O&rsquo,DONNELL CHRISTOPHER JOHN,SUBRAMANYAM CHAKRAPANI,VETELINO BETH COOPER,DUSHIN RUSSELL GEORGE,GRAZIANI EDMUND IDRIS,STROP PAVEL,O&rsquoDONNELL CHRISTOPHER JOHN
申请号：
NZ62447012
公开号：
NZ624470A
申请日:
2012.11.07
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
The disclosure relates to cytotoxic pentapeptides of general formula I. The disclosure also relates to antibody drug conjugates and their use in treating cancer. Example compounds include: 2-methylalanyl-N-[(3R,4S,5S)-l-{ (2S)-2-[(lR,2R)-3-({ (1S)-1-[(7S)-bicyclo[4.2.0]octa-1,3,5-trien-7-yl]-2-methoxy-2-oxoethyl} amino)-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl} -3-methoxy-S-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide 2-methylalanyl-N-[(3R,4S,5S)-1-{ (2S)-2-[(lR,2R)-3-({ (1S)-l-[(7R)-bicyclo[4.2.0]octa-1,3,5trien-7-yl]-2-methoxy-2-oxoethyl} amino)-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl} -3-methoxy-S-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide 2-methylalanyl-N-{ (3R,4S,5S)-1-[(2S)-2-{ (3R,4R,7S,12S)-7-benzyl-14-[3-chloro-4-(propan-2-yloxy)phenyl]-4-methyl-12-[4-(8-methylimidazo[1,2-a]pyridin-2-yl)benzyl]-5,8,14-trioxo-2,9-dioxa-6,13-diazatetradecan-3-yl} pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl} -N-methyl-L-valinamide
