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    Tetrahydro-benzo(e) isoindolines
    6.
    发明公开
    Tetrahydro-benzo(e) isoindolines 失效
    四氢 - 苯并（e）异吲哚啉

    公开(公告)号：EP0095666A3

    公开(公告)日：1985-01-16

    申请号：EP83104932

    申请日：1983-05-19

    申请人： ABBOTT LABORATORIES

    发明人： DeBernardis, John Francis ,  Kerkman, Daniel Joseph ,  McClellan, William John

    IPC分类号： C07D209/62 ,  C07D405/06 ,  C07D209/66 ,  C07C121/48 ,  A61K31/40 ,  C07C121/75

    CPC分类号： C07D405/06 ,  C07C255/00 ,  C07D209/62 ,  C07D209/66

    摘要： DisGosed herein are tetrahydro-benzo [e] isoindolines useful in the treatment of hypertension, which are represented by the formula
    wherein R, R,, and R 2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, benzyloxy, benzoyloxy, thiomethyl, halo, or
    wherein R. and R 5 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula
    wherein R 6 is loweralkyl of 1 to 4 carbon atoms; or R and R,, or R, and R 2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R, or R 2 must be other than hydrogen; and R 3 is hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula
    wherein m is 0, 1 or 2, p is 0 or 1, R 7 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R 8 and R 9 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1. to 4 carbon atoms, or halo, or R, and R 9 can be taken together to form a methylendioxy or ethylenedioxy bridge; or 1,4-benzodioxan.

    摘要翻译： 本发明公开了用于治疗高血压的四氢 - 苯并[e]异吲哚啉，其由下式表示：其中R 1，R 2和R 2独立地选自氢，羟基，1至3个碳原子的低级烷氧基，1的低级链烯氧基 苄氧基，苯甲酰氧基，硫代甲基，卤素，或者其中R和R 5独立地选自氢，1-4个碳原子的低级π-酰氨基或下式的磺酰基：其中R 6为1-4个碳原子的低级烷基; 或R 1和R 2或R 1和R 2可一起形成亚甲二氧基或亚乙二氧基桥; 条件是R 1，R 2或R 2中的至少一个必须不是氢; 和R3是氢; 具有1至4个碳原子的低级烷基; 卤素取代的1至4个碳原子的低级烷基; 其中m为0,1或2，p为0或1，R 7为氢或1-4个碳原子的低级烷基，R 8和R 9独立地选自氢，羟基，甲氧基，1-4低级烷基 碳原子或卤素，或R 1和R 9可一起形成亚甲基二氧基或亚乙基二氧桥; 或1,4-苯并二恶烷。

    CYCLIC PRODRUGS OF DUOCARMYCIN ANALOGS
    10.
    发明公开
    CYCLIC PRODRUGS OF DUOCARMYCIN ANALOGS 有权
    循环前体药物OFF卡霉素类似物

    公开(公告)号：EP2830614A1

    公开(公告)日：2015-02-04

    申请号：EP13769317.2

    申请日：2013-03-26

    申请人： The Scripps Research Institute

    发明人： BOGER, Dale L.

    IPC分类号： A61K31/27

    CPC分类号： C07D498/06 ,  A61K45/06 ,  C07D209/62

    摘要： The invention provides prodrugs of DNA-reactive analogs of duocarmycin and CC-1065 anticancer agents, wherein a cyclic prodrug form, such as carbamate, thionocarbamate, or carbamimidate, can be hydrolyzed by the patient
    in vivo to yield a respective bioactive agent comprising a DNA-alkylating moiety and a binding/targeting moiety. The DNA-reactive moiety is a γ-spirocyclohexenone fused to a heterocyclyl group which can be produced by endogenous hydrolysis of a cyclic carbamate prodrug of the invention. The cyclic carbamate prodrug produces no residual byproduct during activation
    in vivo . Methods of synthesis and biological methods and data are also provided.