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    Variolin derivatives and their use as antitumor agents
    2.
    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。

    Variolin derivatives and their use as antitumor agents
    4.
    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。

    Anititumoral ecteinascidin derivatives
    6.
    发明授权
    Anititumoral ecteinascidin derivatives 有权
    抗肿瘤抗坏血酸衍生物

    公开(公告)号：US07919493B2

    公开(公告)日：2011-04-05

    申请号：US11733606

    申请日：2007-04-10

    申请人： Maria Flores ,  Andres Francesh ,  Pilar Gallego ,  Jose Luis Chicharro ,  Maria Zarzuelo ,  Carolina Fernandez ,  Ignacio Manzanares

    发明人： Maria Flores ,  Andres Francesh ,  Pilar Gallego ,  Jose Luis Chicharro ,  Maria Zarzuelo ,  Carolina Fernandez ,  Ignacio Manzanares

    IPC分类号： C07D241/36 ,  A61K31/495 ,  A01N43/60

    CPC分类号： C07D515/22

    摘要： This invention relates to antitumoral ecteinascidin derivatives that contain a fused ecteinascidin five ring system with a 1,4-bridge having the structure of formula (VIa) or (VIb) as described herein and compounds in which the —NH2 or —OH of the 1,4-bridge is derivatized, and related pharmaceutical compositions and methods. Such ecteinascidin derivatives include, but are not limited to, those compounds having formula (XVIIb): in which R1 and R4 together form a group of formula (VIa) or (VIb) as described herein, and R5, R7, R8, R14a, R14b, R15, and R21 are as defined herein.

    摘要翻译： 本发明涉及含有具有如本文所述的结构式（VIa）或（VIb）的1,4桥的融合的ecteinidinidin五环系统的抗肿瘤抗坏血酸衍生物，其中1或2的-NH 2或-OH的化合物 ，4桥衍生化，相关药物组成和方法。 这样的黑皮质素衍生物包括但不限于具有式（XVIIb）的那些化合物：其中R 1和R 4一起形成本文所述的式（VIa）或（VIb）基团，并且R5，R7，R8，R14a， R14b，R15和R21如本文所定义。