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Gemcitabine derivatives, producing methods thereof and the use as prodrugs
专利权人:
发明人:
WU, I CHIH,吴逸之,吳逸之
申请号:
TW103116551
公开号:
TWI569800B
申请日:
2014.05.09
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
The present invention relates to Gemcitabine derivatives according to formula I: and pharmaceutically acceptable salts thereof. For compounds of formula I, R1 and R2 are independently selected from the group consisting of H, -C(=O)-(CH2)2-aryl, and -C(=O)-(CH2)n-C(=O)-NH-aryl. The subscript n is from 2 to 6. R3 is selected from the group consisting of H and -C(=O)-O-R4 and R4 is selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, arylalkyl, substituted arylalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl and substituted heteroalkyl. Compounds are provided wherein at least one of R1 and R2 is other than H. Pharmaceutical compositions and methods for the treatment of cancer are also provided.本發明係關於一種具有下式I之吉西他濱(Gemcitabine)衍生物,及其醫藥上可接受之鹽類其中R1及R2獨立地係選自由H、-C(=O)-(CH2)2-芳基及C(=O)-(CH2)n-C(=O)-NH-芳基組成之組群,其條件為R1及R2其中至少一者不為氫。n代表2至6之數字。R3係選自由H及-C(=O)-O-R4組成之組群;且R4係選自由烷基、經取代之烷基、烯基、經取代之烯基、炔基、經取代之炔基、芳基烷基、經取代之芳基烷基、環雜烷基、經取代之環雜烷基、雜烷基及經取代之雜烷基組成之組群。本發明亦關於包含該等吉西他濱衍生物之醫藥組成物,特別是用於治療癌症之醫藥組成物。
来源网站:
中国工程科技知识中心
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