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SUNITINIB PRODRUG AND PHARMACEUTICAL COMPOSITION
专利权人:
发明人:
申请号:
EP16742708.7
公开号:
EP3252048A1
申请日:
2016.01.25
申请国别(地区):
EP
年份:
2017
代理人:
摘要:
The present invention provides a Sunitinib prodrug having formula I, wherein R12, R13 are selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4-15 membered heterocyclyl and 5-15 membered heteroaryl R14 is selected from the group consisting of R, OR, SR and N(R)2 and R is selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4-15 membered heterocyclyl, 5-15 membered heteroaryl, hydroxyl C1-C6 alkyl, carboxyl C1-C6 alkyl, C1-C6 alkyl amido and phosphate group. The Sunitinib prodrug of the invention provides better pharmacokinetics and pharmacodynamics, better safety and lower toxicity.
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