Bioreductively-activated prodrugs
    2.
    发明申请
    Bioreductively-activated prodrugs 审中-公开
    生物还原活化的前药

    公开(公告)号:US20090202571A1

    公开(公告)日:2009-08-13

    申请号:US11663495

    申请日:2005-09-26

    摘要: A compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: —Ar is a substituted heteroaryl group bearing at least one nitro or azido group or is a benzoquinone, naphthoquinone or fused heterocyloquinone; -R1 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; -R2 is a glycoside, OH, optionally substituted alkyl, optionally substituted alkoxy, C2-C8 alkenyl, C1-C8 hydroxyalkyl, optionally substituted arylamino, optionally substituted aryl C1-C4 alkylamino or hydroxyalkylamino; and -R3 and R4 are each independently H or halo.

    摘要翻译: 式(1)化合物或其药学上可接受的盐,其中:-Ar为带有至少一个硝基或叠氮基的取代杂芳基,或为苯醌,萘醌或稠合异喹啉醌; -R1是氢,任选取代的烷基,任选取代的烯基,任选取代的炔基,任选取代的环烷基,任选取代的杂环烷基,任选取代的芳基或任选取代的杂芳基; -R2是糖苷,OH,任选取代的烷基,任选取代的烷氧基,C 2 -C 8烯基,C 1 -C 8羟烷基,任选取代的芳基氨基,任选取代的芳基C 1 -C 4烷基氨基或羟烷基氨基; 且R 3和R 4各自独立地为H或卤素。