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PROTEASOME INHIBITORS
专利权人:
MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WISSENSCHAFTEN E.V.
发明人:
CHARI, ASHWIN,STARK, HOLGER,SCHRADER, JIL,HENNEBERG, FABIAN
申请号:
CA3026564
公开号:
CA3026564A1
申请日:
2017.06.06
申请国别(地区):
CA
年份:
2017
代理人:
摘要:
The present invention relates to a compound of formula (I), wherein X is C=0, C=S or B-OH Y is an electrophile and Z is a leaving group, or Y--Z is an electrophile R1 comprises or consists of (a) (i) a first group binding to a proteolytic site of a proteasome, said first group being bound to X and (ii) optionally a second group enhancing delivery or (b) a group binding between subunits ß1 and ß2 of a proteasome R2 and R3 are independently selected from H, methyl, methoxy, ethyl, ethenyl, ethinyl and cyano, wherein methyl and ethyl may be substituted with OH or halogen.
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