SUNITINIB PRODRUG AND PHARMACEUTICAL COMPOSITION

    公开(公告)号:EP3252048A4

    公开(公告)日:2018-07-18

    申请号:EP16742708

    申请日:2016-01-25

    发明人: WANG ZHONG LI QING

    摘要: The present invention provides a Sunitinib prodrug having formula I, wherein R 12 , R 13 are selected from the group consisting of H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, C 6 -C 10 aryl, 4-15 membered heterocyclyl and 5-15 membered heteroaryl; R 14 is selected from the group consisting of R', OR', SR' and N(R') 2 ; and R' is selected from the group consisting of H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, C 6 -C 10 aryl, 4-15 membered heterocyclyl, 5-15 membered heteroaryl, hydroxyl C 1 -C 6 alkyl, carboxyl C 1 -C 6 alkyl, C 1 -C 6 alkyl amido and phosphate group. The Sunitinib prodrug of the invention provides better pharmacokinetics and pharmacodynamics, better safety and lower toxicity.