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FUNCTIONALIZED MORPHOLINYL ANTHRACYCLINE DERIVATIVES
专利权人:
发明人:
BERIA ITALO,CARUSO MICHELE,LUPI VITTORIA
申请号:
IN201747018902
公开号:
IN201747018902A
申请日:
2017.05.30
申请国别(地区):
IN
年份:
2017
代理人:
摘要:
The present invention relates to new functionalized morpholinyl anthracycline derivatives which have cytotoxic activity and are useful in treating diseases such as cancer cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them. The invention also relates to the use of these derivatives in the preparation of conjugates. The morpholinyl anthracycline derivatives are of the formula Ant L W Z RM (I) wherein RM is null or a reactive moiety Z is null or a peptidic non peptidic or hybrid peptidic and non peptidic linker W is null or a self immolative system comprising one or more self immolative groups L is null or a conditionally cleavable moiety Ant is an anthracycline moiety selected from the formulas (II) (III) (IV) and (V) wherein the wavy line indicates the attachment to the conditionally cleavable moiety L or to the self immolative system W or to the linker Z or to the reactive moiety RM provided that at least one of L W Z and RM is not null R is halogen or NR4R5 R2 is OR6 NR7R8 or an optionally substituted group selected from straight or branched CCalkyl NR7R8 CCalkyl and R60 CCalkyl R4 and R5 are independently hydrogen a monosubstituted benzyl a disubstituted benzyl or an optionally substituted group selected from straight or branched C Calkyl NR7R8 C Calkyl R60 C Calkyl R7R8N C Calkylcarbonyl R60 C Calkylcarbonyl R7R8N C Calkoxycarbonyl and R60 C Calkoxycarbonyl or R4 and R5 taken together with the nitrogen atom to which they are bound form a heterocyclyl substituted with R4 wherein R4 is hydrogen or a group selected from straight or branched C Calkyl and NR7R8 C Calkyl R15 is null or an optionally substituted bivalent group selected from NR7 C Calkyl O C Calkyl NR7 C Calkylcarbonyl O C Calkylcarbonyl NR7 C Calk
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中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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