发明名称 Anthracycline prodrugs, method for preparation as well as their use in selective chemotherapy
摘要 Anthracycline derivatives are disclosed which are coupled to an enzymatically cleavable N-phenyl-O-glycosyl carbamate spacer group, which derivatives are represented by the formula <IMAGE> 1 R1 = H, OH, OMe R2 = H, OH R3 = H, CX3, NO2, CN, X, Y, OY, NHY, S(O2)Y, C(O)Y, C(O)OY R4 = CH2OH, C(O)O-Z+ X = halogen Y = C1C3 alkyl, aryl Z = H, LI, Na, K as well as the acid addition salts thereof. Further the synthesis of these derivatives and their use, alone or in combination with enzymes or antibody enzyme conjugates are disclosed.
申请公布号 US5710135(A) 申请公布日期 1998.01.20
申请号 US19960652940 申请日期 1996.05.24
申请人 PHARMACHEMIE B.V. 发明人 LEENDERS, RUBEN G. G.;DAMEN, ERIC W. P.;SCHEEREN, JOHAN WILHELM;HAISMA, HIDDE J.;HOUBA, PIETER H. J.;DE VOS, DICK
分类号 A61K31/70;A61K31/7028;A61K31/7034;A61K31/704;A61K39/395;A61P35/00;C07F7/18;C07H15/203;C07H15/252;(IPC1-7):A61K31/70;C07H15/24 主分类号 A61K31/70
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