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    WATER-SOLUBLE ETOPOSIDE ANALOGS AND METHODS OF USE THEREOF
    3.
    发明申请
    WATER-SOLUBLE ETOPOSIDE ANALOGS AND METHODS OF USE THEREOF 失效
    水溶性ETOPOSIDE ANALOGS及其使用方法

    公开(公告)号：US20070123475A1

    公开(公告)日：2007-05-31

    申请号：US11619304

    申请日：2007-01-03

    Applicant: Kuo-Hsiung Lee ,  Zhiyan Xiao ,  Kenneth Bastow

    Inventor： Kuo-Hsiung Lee ,  Zhiyan Xiao ,  Kenneth Bastow

    IPC: A61K31/7048 ,  A61K31/365 ,  C07D493/02

    CPC classification number: C07D493/04 ,  C07D497/04

    Abstract: Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

    Abstract translation: 具有改善的水溶性的依托泊苷类似物，例如4'-O-脱甲基-4' - （N'，N'-二甲基 - 甘氨酰）-4β-（4“ - 硝基苯胺基）-4-脱氧鬼臼毒素（8）和 描述了4'-O-脱甲基-4' - （N'，N'-二甲基 - 甘氨酰基）-4β-（4“ - 氟苯胺基）-4-脱氧鬼臼毒素（9）以及含有它们的药物制剂 ，其使用方法和中间体及其制备方法。

    Water-soluble etoposide analogs and methods of use thereof
    4.
    发明授权
    Water-soluble etoposide analogs and methods of use thereof 失效
    水溶性依托泊苷类似物及其使用方法

    公开(公告)号：US07176236B2

    公开(公告)日：2007-02-13

    申请号：US10712663

    申请日：2003-11-13

    Applicant: Kuo-Hsiung Lee ,  Zhiyan Xiao ,  Kenneth F. Bastow

    Inventor： Kuo-Hsiung Lee ,  Zhiyan Xiao ,  Kenneth F. Bastow

    IPC: A61K31/335 ,  C07D407/00 ,  C07D307/77

    CPC classification number: C07D493/04 ,  C07D497/04

    Abstract: Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

    Abstract translation: 具有改善的水溶性的依托泊苷类似物，例如4'-O-脱甲基-4' - （N'，N'-二甲基 - 甘氨酰）-4β-（4“ - 硝基苯胺基）-4-脱氧鬼臼毒素（8）和 描述了4'-O-脱甲基-4' - （N'，N'-二甲基 - 甘氨酰基）-4β-（4“ - 氟苯胺基）-4-脱氧鬼臼毒素（9）以及含有它们的药物制剂 ，其使用方法和中间体及其制备方法。

    Covalent conjugates of topoisomerase I and topoisomerase II inhibitors
    6.
    发明授权
    Covalent conjugates of topoisomerase I and topoisomerase II inhibitors 失效
    拓扑异构酶I和拓扑异构酶II抑制剂的共价缀合物

    公开(公告)号：US06420377B1

    公开(公告)日：2002-07-16

    申请号：US09723822

    申请日：2000-11-28

    Applicant: Kuo-Hsiung Lee ,  Yung-Chi Cheng ,  Xin Guo ,  Kenneth F. Bastow ,  Hui-Kang Wang

    Inventor： Kuo-Hsiung Lee ,  Yung-Chi Cheng ,  Xin Guo ,  Kenneth F. Bastow ,  Hui-Kang Wang

    IPC: A61K3144

    CPC classification number: A61K47/55 ,  A61K47/54

    Abstract: The present invention provides covalent conjugates of topoisomerase I and topoisomerase II inhibitors. Such compounds have a structure according to formula I: TI—L—TII  (I) wherein: TI is a topoisomerase I inhibitor such as a camptothecin group; TII is a topoisomerase II inhibitor such as an amsacrine, ellipticine, epipodophyllotoxin, or anthracycline antibiotic group; and L is a linking group. The compounds are useful for inhibiting topoisomerase I and II enzymes, for promoting cellular differentiation, and for treating cancer.

    Abstract translation: 本发明提供拓扑异构酶I和拓扑异构酶II抑制剂的共价缀合物。 这样的化合物具有式I的结构：其中：TI是拓扑异构酶I抑制剂，如喜树碱基; TII是拓扑异构酶II抑制剂，如amsacrine，玫瑰树碱，表鬼臼毒素或蒽环类抗生素组; 和L是连接基团。该化合物可用于抑制拓扑异构酶I和II酶，促进细胞分化和治疗癌症。

    Covalent conjugates of topoisomerase I and topoisomerase II inhibitors
    7.
    发明授权
    Covalent conjugates of topoisomerase I and topoisomerase II inhibitors 失效
    拓扑异构酶I和拓扑异构酶II抑制剂的共价缀合物

    公开(公告)号：US06207673B1

    公开(公告)日：2001-03-27

    申请号：US08815890

    申请日：1997-03-12

    Applicant: Kuo-Hsiung Lee ,  Yung-Chi Cheng ,  Xin Guo ,  Kenneth F. Bastow ,  Hui-Kang Wang

    Inventor： Kuo-Hsiung Lee ,  Yung-Chi Cheng ,  Xin Guo ,  Kenneth F. Bastow ,  Hui-Kang Wang

    IPC: A61K3144

    CPC classification number: A61K47/55 ,  A61K47/54

    Abstract: The present invention provides covalent conjugates of topoisomerase I and topoisomerase II inhibitors. Such compounds have a structure according to formula I: TI—L—TII  (I) wherein: TI is a topoisomerase I inhibitor such as a camptothecin group; TII is a topoisomerase II inhibitor such as an amsacrine, ellipticine, epipodophyllotoxin, or anthracycline antibiotic group; and L is a linking group. The compounds are useful for inhibiting topoisomerase I and II enzymes, for promoting cellular differentiation, and for treating cancer.

    Abstract translation: 本发明提供拓扑异构酶I和拓扑异构酶II抑制剂的共价缀合物。 这样的化合物具有式I的结构：其中：TI是拓扑异构酶I抑制剂，如喜树碱基; TII是拓扑异构酶II抑制剂，如amsacrine，玫瑰树碱，表鬼臼毒素或蒽环类抗生素组; 和L是连接基团。该化合物可用于抑制拓扑异构酶I和II酶，促进细胞分化和治疗癌症。

    Naphthoquinone antitumor compound and method
    9.
    发明授权
    Naphthoquinone antitumor compound and method 失效
    萘醌类抗肿瘤化合物及方法

    公开(公告)号：US5789431A

    公开(公告)日：1998-08-04

    申请号：US601114

    申请日：1996-02-16

    Applicant: Kuo-Hsiung Lee ,  Sheng-Chu Kuo ,  Toshiro Ibuka

    Inventor： Kuo-Hsiung Lee ,  Sheng-Chu Kuo ,  Toshiro Ibuka

    IPC: C07C233/32 ,  C07C233/42 ,  C07C233/43 ,  C07C233/44 ,  C07C233/76 ,  C07D235/02 ,  A61K31/415

    CPC classification number: C07D235/02 ,  C07C233/32 ,  C07C233/42 ,  C07C233/43 ,  C07C233/44 ,  C07C233/76 ,  C07C2102/10

    Abstract: The invention provides 1,4-naphthoquinone compounds and a method for inhibiting tumor cell growth in a subject by administering such compounds. The compounds are represented by the structures: ##STR1## where R.sub.1 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX where m is 2 or 3 and X is H, methyl, or ethyl; R.sub.2 is halo or NHY, where Y is hydrogen, lower alkyl, halogenated lower alkyl, hydroxylated lower alkyl, lower dialkylaminoalkyl, phenyl, benzyl, or phenethyl; R.sub.3 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX, where m and X are as defined for R.sub.1 above; and R.sub.4 is hydrogen, lower alkyl, lower aminoalkyl, halogenated lower alkyl, phenyl, benzyl, or phenethyl.

    Abstract translation: 本发明提供1,4-萘醌化合物和通过施用这些化合物来抑制受试者的肿瘤细胞生长的方法。 化合物由以下结构表示：其中R 1是低级烷基，卤代低级烷基，苯基，苄基，苯乙基或 - （CH 2）m COOX，其中m是2或3，以及 X是H，甲基或乙基; R2是卤素或NHY，其中Y是氢，低级烷基，卤代低级烷基，羟基化的低级烷基，低级二烷基氨基烷基，苯基，苄基或苯乙基; R3是低级烷基，卤代低级烷基，苯基，苄基，苯乙基或 - （CH2）mCOOX，其中m和X如上述R1所定义; 和R4是氢，低级烷基，低级氨基烷基，卤代低级烷基，苯基，苄基或苯乙基。

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