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    Antitumoral ecteinascidin derivatives
    1.
    发明授权
    Antitumoral ecteinascidin derivatives 有权
    抗肿瘤抗坏血酸衍生物

    公开(公告)号：US07202361B2

    公开(公告)日：2007-04-10

    申请号：US10240963

    申请日：2001-04-12

    申请人： Maria Flores ,  Andrés Francesch ,  Pilar Gallego ,  José Luis Chicharro ,  Maria Zarzuelo ,  Carolina Fernández ,  Ignacio Manzanares

    发明人： Maria Flores ,  Andrés Francesch ,  Pilar Gallego ,  José Luis Chicharro ,  Maria Zarzuelo ,  Carolina Fernández ,  Ignacio Manzanares

    IPC分类号： C07D515/22 ,  A61K31/395 ,  A61P35/00

    CPC分类号： C07D515/22

    摘要： This invention relates to compounds of the formula: wherein: the substituent groups defined by R1, R2 are each independently selected of H, C(═O)R′, C1–C18 alkyl, C2–C18 alkenyl, C2–C18 alkynyl, or aryl; 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; or C1–C18 alkyl, C2–C18 alkenyl, C2–C18 alkynyl, or aryl, each of which, independently, may be substituted with one or more substituents selected from the group consisting of halogen, cyano, hydroxy, nitro, azido; alkanoyl, carboxamido, alkyl, alkenyl, alkynyl, aryloxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, aminoalkyl, carbocylic aryl having 6 or more carbons, and aralkyl; X2 is OX1 or N(X1)2 wherein each X1 is independently H, C(═O)R′ where R′ is as defined, C1–C18 alkyl, C2–C18 alkenyl, C2–C18 alkynyl, aryl, alkoxy, heterocyclyl, or two X1 groups together form a cyclic substituent on the nitrogen atom, or X1 is SO2CH3 when X2 is OX1, or N(X1)2 is NHCOalkylCOOH, Nilbiotin, NH(aa)y where aa is amino acid acyl andy is 1, 2 or 3 optionally with a amide terminal group, protected NHCOCH(NH2)CH2SH, NHCOalkenylaryl substituted with CF3, or m-methoxycarbonylbenzoylNH; wherein N(X1)2 is not NH2; X3 is selected of OR1 where R1 is as defined, CN, (═O), or H; X4 is—H or C1–C18 alkyl; and X5 is selected of H, or R1 where R1 is as defined; provided that the compound is not ecteinascidin 583 or 597, which are useful for treating tumors.

    摘要翻译： 本发明涉及下式的化合物：其中：R 1，R 2定义的取代基各自独立地选自H，C（.dbd.O）R'，C C 18 -C 18烷基，C 2 -C 18烯基，C 2 -C 18炔基或芳基; 每个R'基团独立地选自H; 哦; NO2; NH2; SH; CN; 卤素; .dbd.O; C（.dbd.O）H; C（.dbd.O）CH 3; CO 2， 或C 1 -C 18烷基，C 2 -C 18烯基，C 2 -C 18炔基或芳基，其各自独立地可以被 一个或多个选自卤素，氰基，羟基，硝基，叠氮基的取代基; 烷酰基，甲酰氨基，烷基，烯基，炔基，芳氧基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，氨基烷基，具有6个或更多个碳的碳环芳基和芳烷基; X 2是OX 1或N（X 1）2，其中每个X 1独立地是H，C（.dbd.O）R'，其中R'如所定义 ，C 1 -C 18烷基，C 2 -C 18烯基，C 2 -C 18炔基，芳基，烷氧基，杂环基或两个X 1 一起在氮原子上形成环状取代基，或当X 2为O X 1或N（X 1）时，X 1为SO 2 CH 3。 sub.2是NHCO烷基COOH，NHBiotin，NH（aa），其中aa是氨基酸酰基，Y是1,2或3，任选具有酰胺末端基，保护的NHCOCH（NH 2）CH 2。 2S，被CF 3取代的NHCO烯基芳基或间甲氧基羰基苯甲酰基NH; 其中N（X 1）2不是NH 2; X 3选自OR.sub.1其中R 1如定义，CN，（.dbd.O）或H; X 4是-H或C 1 -C 18烷基; 并且X 5选自H或R 1，其中R 1如定义; 条件是该化合物不是用于治疗肿瘤的角叉菜胶583或597。