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    Hemisynthetic Method and New Compounds
    1.
    发明申请
    Hemisynthetic Method and New Compounds 有权
    半合成方法和新化合物

    公开(公告)号：US20080045713A1

    公开(公告)日：2008-02-21

    申请号：US11774890

    申请日：2007-07-09

    申请人： Carmen Cuevas ,  Marta Perez ,  Andres Francesch ,  Carolina Fernandez ,  Jose Chicharro ,  Pilar Gallego ,  Maria Zarzuelo ,  Fernando Calle ,  Ignacio Manzanares

    发明人： Carmen Cuevas ,  Marta Perez ,  Andres Francesch ,  Carolina Fernandez ,  Jose Chicharro ,  Pilar Gallego ,  Maria Zarzuelo ,  Fernando Calle ,  Ignacio Manzanares

    IPC分类号： C07D471/08 ,  C07D491/147

    CPC分类号： C07D471/18 ,  C07D471/22 ,  C07D491/22 ,  C07D515/22 ,  Y02P20/55

    摘要： Methods are provided for preparing a compound with a fused ring structure of formula (XIV) which comprises one or more reactions starting from a 21-cyano compound of formula (XVI) where typically; R1 is an amidomethylene group or an aryloxymethylene group; R5 and R8 are independently chosen from —H, —OH or —OCOCH2OH, or R5 and R8 are both keto and the ring A is a p-benzoquinone ring; R14a and R14b are both —H ozone is —H and the other is —OH, —OCH3 or —OCH2CH3, or R14a and R14b together form a keto group; and R15 and R18 are independently chosen from —H or —OH, or R5 and R8 are both keto and the ring A is a p-benzoquinone ring. In modified starting materials, the 21-cyano group can be replaced by other groups introduced using nucleophilic reagents.

    摘要翻译： 提供了制备具有式（XIV）的稠环结构的化合物的方法，其包含一个或多个由式（XVI）的21-氰基化合物开始的反应，其中通常; R 1是酰亚胺基或芳氧基亚甲基; R 5和R 8独立地选自-H，-OH或-OCOCH 2 OH，或R 5 O >和R 8均为酮，环A为对苯醌环; R 14a和R 14b都是-H臭氧是-H，另一个是-OH，-OCH 3或-OCH 3 2 3，或R 14a和R 14b共同形成酮基; R 15和R 18独立地选自-H或-OH，或R 5和R 8， 都是酮基，环A是对苯醌环。 在改性原料中，21-氰基可以被其它使用亲核试剂引入的基团所取代。

    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。