Antitumoral compounds
    1.
    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

    Ecteinascidin analogs for use as antitumour agents
    6.
    发明授权
    Ecteinascidin analogs for use as antitumour agents 有权
    用作抗肿瘤剂的抗坏血酸类抗生素

    公开(公告)号:US07763615B2

    公开(公告)日:2010-07-27

    申请号:US10485536

    申请日:2002-08-06

    CPC分类号: C07D515/22

    摘要: Derivatives of ecteinascidin 736 of general formula (I) wherein the groups R1, R2, R3, R4 and R5 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, C(═O)R′, C(═O)OR′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclic; wherein X is independently selected of OR′, CN, (═O), or H; wherein each of the 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, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein m is 0, 1 or 2; and wherein n is 0, 1, 2, 3, or 4, and their use as antitumoral agent.

    摘要翻译: 基团R 1,R 2,R 3,R 4和R 5各自独立地选自H,OH,OR',SH,SR',SOR',SO 2 R',C的通式(I)的抗坏血酸素736衍生物 (= O)R',C(= O)OR',NO 2,NH 2,NHR',N(R')2,NHC(O)R',CN,卤素,= O,取代或未取代的C 1 -C 25烷基 取代或未取代的C 2 -C 18烯基,取代或未取代的C 2 -C 18炔基,取代或未取代的芳基,取代或未取代的杂环基; 其中X独立地选自OR',CN,(= O)或H; 其中每个R'基团独立地选自H,OH,NO 2,NH 2,SH,CN,卤素,= O,C(= O)H,C(= O)CH 3,CO 2 H, 未取代的C 1 -C 25烷基,取代或未取代的C 2 -C 18烯基,取代或未取代的C 2 -C 18炔基,取代或未取代的芳基; 其中m为0,1或2; 并且其中n为0,1,2,3或4,并且其用作抗肿瘤剂。