Antitumoral compounds
    16.
    发明授权

    公开(公告)号:US07138547B2

    公开(公告)日:2006-11-21

    申请号:US10297352

    申请日:2001-06-06

    摘要: New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form ═O; Y is NR1, OR1, PR1, SR1, or halogen, wherein the number of substituents R1 is selected to suit the valency and each R1 is independently selected of H, OH, C(═O)R′, P(═O)R′R″, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups Z may together form ═O; z is 0 to 25; y is to 0 to 20; R2 is H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, S(═O)2R′, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 Alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl; R3 is H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, S(═O)2R′, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl; each of the R′, R″ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C1–C18 alkoxy, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynl, substituted or unsubstituted aryl; there may be one or more unsaturations in the hydrocarbon backbone defined by the chain (II) and salts thereof; with the exception of a C16–C24 2-amino-3-hydroxyalkane or a C16–C24 2-amino-3-hydroxyalkene

    Variolin derivatives and their use as antitumor agents
    20.
    发明授权
    Variolin derivatives and their use as antitumor agents 失效
    异喹啉衍生物及其作为抗肿瘤剂的用途

    公开(公告)号:US07772241B2

    公开(公告)日:2010-08-10

    申请号:US12349813

    申请日:2009-01-07

    IPC分类号: A61K31/519 C07D473/00

    摘要: Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, NHSO2R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.

    摘要翻译: 提供了式(5)的衍生物,其中由X2,R1,R2,R3,R6,R7和R12定义的取代基各自独立地选自H,OH,OR',SH,SR' ,SOR',SO2R',NO2,NH2,NHR',N(R')2,NHCOR',NHSO2R',CN,卤素,= O,C(= O)H,C(= O)R' ,CO 2 R',羧基烷基,C 1 -C 12烷基,C 2 -C 12烯基,C 2 -C 12炔基,取代或未取代的芳基,取代或未取代的芳烷基和取代或未取代的杂芳族; 其中每个R'基团独立地选自H,OH,SH,NO 2,NH 2,CN,卤素,= O,C(= O)H,C(= O)CH 3,CO 2 H,CO 2 CH 3, C 1 -C 12烷基,C 2 -C 12烯基,C 2 -C 12炔基,芳基,芳烷基和杂芳族; 其中R 1和R 2,R 2和R 3,R 3和R 12,R 12和R 6,或R 6和R 7的这些基团可以连接成碳环或杂环系。