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    • 3. 发明申请
    • WATER SOLUBLE DERIVATIVES OF CAMPTOTHECIN AND THEIR USE AS ANTITUMOR AGENTS
    • 卡莫司汀的水溶性衍生物及其作为抗菌剂的用途
    • WO1994025466A1
    • 1994-11-10
    • PCT/US1994004681
    • 1994-04-28
    • GLAXO, INC.BESTERMAN, Jeffrey, MarkEVANS, Michael, GlennLUZZIO, Michael, JosephMYERS, Peter, Leslie
    • GLAXO, INC.
    • C07D491/22
    • C07D317/66C07D319/18
    • The present invention relates to water soluble, camptothecin derivatives of formula (I), wherein: n represents the integer 1 or 2; and i) R represents: hydrogen, lower alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, amino lower alkyl, lower alkylamino lower alkyl, amino lower alkyl, lower alkoxy lower alkyl or (CH2)tAr wherein: t is 0 to 5 and Ar represents phenyl, furyl, pyridyl, N-methylpyrrolyl, imidazolyl; or phenyl, furyl, pyridyl, N-methylpyrrolyl, imidazolyl, with one or more substituents independently selected from hydroxy, methoxy, halogen, and amino; and R represents: diphenylmethyl or (CH2)tAr; or ii) R1 and R2 taken together with the linking nitrogen represent: N-tetrahydroquinolyl or N-tetrahydroisoquinolyl; and the pharmaceutically acceptable salts and solvates thereof, their use in the treatment of tumors and methods of their preparation.
    • 本发明涉及式(I)的水溶性喜树碱衍生物,其中:n表示整数1或2; 和(i)R 1表示:氢,低级烷基,(C 3-7)环烷基,(C 3-7)环烷基低级烷基,低级烯基,羟基低级烷基,氨基低级烷基,低级烷基氨基低级烷基,氨基低级烷基, 低级烷氧基低级烷基或(CH2)tAr其中:t为0至5,Ar表示苯基,呋喃基,吡啶基,N-甲基吡咯基,咪唑基; 或苯基,呋喃基,吡啶基,N-甲基吡咯基,咪唑基,其中一个或多个取代基独立地选自羟基,甲氧基,卤素和氨基; 和R 2代表:二苯基甲基或(CH 2)t Ar; 或ii)R 1和R 2与连接氮一起代表:N-四氢喹啉基或N-四氢异喹啉基; 及其药学上可接受的盐和溶剂合物,它们在治疗肿瘤中的用途及其制备方法。