发明名称 Glutathione-activated anti-tumor prodrugs of 6-mercaptopurine and 6-thioguanine
摘要 The present invention relates to a method for treating a tumor in a tissue of a human or non-human animal, the tumor having an elevated level of glutathione relative to the tissue, the method comprising the steps of administering to the animal a prodrug comprising a thiopurine having a sulfur heteroatom conjugated to an alpha-, beta-unsaturated carbonyl moiety, in combination with a pharmaceutically acceptable carrier, the moiety comprising a double bond having an alpha end and a beta end, the beta end being accessible to glutathione in an addition-elimination reaction, the prodrug lacking an ionizable carboxylic acid group; and observing a reduction in growth of the tumor.
申请公布号 US2004023994(A1) 申请公布日期 2004.02.05
申请号 US20030454443 申请日期 2003.06.04
申请人 ELFARRA ADNAN A.;GUNNARSDOTTIR SJOFN 发明人 ELFARRA ADNAN A.;GUNNARSDOTTIR SJOFN
分类号 A61K31/52;C07D473/24;C07D473/38;(IPC1-7):A61K31/522 主分类号 A61K31/52
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