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    Variolin derivatives and their use as antitumor agents
    1.
    发明申请
    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：US20060235223A1

    公开(公告)日：2006-10-19

    申请号：US10483525

    申请日：2002-07-11

    申请人： Modesto Remuiñan ,  Juan Gonzalez ,  Carlos Pozo ,  Carmen Cuevas ,  Simon Munt ,  Regan Anderson ,  Andres Francesh ,  Jonathan Morris ,  Ignacio Manzanares

    发明人： Modesto Remuiñan ,  Juan Gonzalez ,  Carlos Pozo ,  Carmen Cuevas ,  Simon Munt ,  Regan Anderson ,  Andres Francesh ,  Jonathan Morris ,  Ignacio Manzanares

    IPC分类号： C07D487/14

    CPC分类号： C07D213/64 ,  C07D213/78 ,  C07D239/38 ,  C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D471/06 ,  C07D471/14

    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, N02, NH2, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups 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）的异喹啉衍生物，其中由X 2，R 1，R 2，R 2， R 3，R 6，R 7和R 12各自独立地选自H，OH，OR' ，SH，SR'，SOR'，SO 2 R'，NO 2，NH 2，NHR'，N（R' （O）H，C（-O）R'，CO 2（OR 2）2，NHCOR'，NHSO 2 R'，CN，卤素， H，CO 2 R'，羧基烷基，C 1 -C 12烷基，C 2 -C 12烷基，C 1 -C 12烷基， C 12 - 12链烯基，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，N，O，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链烯基，C 2 -C 12烷基，C 1 -C 12烷基， 炔基，芳基，芳烷基和杂芳基; 其中基团R 1和R 2，R 2和R 3，R 3， R 12和R 12，R 12和R 6，或R 6和R 12， 7可以连接到碳环或杂环系中。

    Variolin derivatives and their use as antitumor agents
    3.
    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

    申请人： Modesto Remuinan ,  Juan Jose Gonzalez ,  Carlos Del Pozo ,  Andres Francesh ,  Carmen Cuevas ,  Simon Munt ,  Ignacio Manzanares ,  Regan James Anderson ,  Jonathan Charles Morris

    发明人： Modesto Remuinan ,  Juan Jose Gonzalez ,  Carlos Del Pozo ,  Andres Francesh ,  Carmen Cuevas ,  Simon Munt ,  Ignacio Manzanares ,  Regan James Anderson ,  Jonathan Charles Morris

    IPC分类号： A61K31/519 ,  C07D473/00

    CPC分类号： C07D213/64 ,  C07D213/78 ,  C07D239/38 ,  C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D471/06 ,  C07D471/14

    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。

    Ecteinascidin analogs for use as antitumour agents
    7.
    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

    申请人： Pilar Gallego ,  Carmen Cuevas ,  Simon Munt ,  Ignacio Manzanares ,  Valentin Martinez

    发明人： Pilar Gallego ,  Carmen Cuevas ,  Simon Munt ,  Ignacio Manzanares ,  Valentin Martinez

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D487/00 ,  C07D491/00 ,  C07D513/00

    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。