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115 条记录 (耗时 0.029 秒)

    3′-substituted nucleoside derivative
    52.
    再颁专利
    3′-substituted nucleoside derivative 有权
    3'-取代核苷衍生物

    公开(公告)号：USRE38090E1

    公开(公告)日：2003-04-22

    申请号：US09584171

    申请日：2000-05-26

    申请人： Akira Matsuda ,  Takuma Sasaki

    发明人： Akira Matsuda ,  Takuma Sasaki

    IPC分类号： A61K3170

    CPC分类号： C07H19/06 ,  C07H19/04 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  Y02P20/55

    摘要： The invention relates to a 3′-substituted nucleoside derivative represented by the following general formula (1): wherein B means a nucleic acid base which may have a substituent, Z represents a lower alkynyl or lower alkenyl group which may be substituted by a group represented by the formula: in which Ra, Rb and Rc are individually a lower alkyl group or a phenyl group, or an oxiranyl group which may have at least one lower alkyl group, R1 and R2 individually represent H or an ester-forming residue capable of easily leaving in a living body, and R3 is H, a mono- or polyphosphoric acid residue, or an ester-forming residue capable of easily leaving in a living body, with the proviso that the sugar moiety is ribose, or a pharmaceutically acceptable salt thereof. The 3′-substituted nucleoside derivative according to the invention has an excellent antitumor activity and is hence useful for treatment for and prevention of cancers.

    摘要翻译： 本发明涉及由以下通式（1）表示的3'-取代核苷衍生物：其中B表示可具有取代基的核酸碱基，Z表示可被基团取代的低级炔基或低级烯基 由下式表示：其中Ra，Rb和Rc分别为低级烷基或苯基，或可具有至少一个低级烷基的环氧乙烷基，R 1和R 2分别表示H或成酯残基 容易地离开生物体，R3是H，单磷酸或多磷酸残基或能够容易地在活体中离开的酯形成残基，条件是糖部分是核糖或药学上可接受的 的盐。 根据本发明的3'-取代的核苷衍生物具有优异的抗肿瘤活性，因此可用于治疗和预防癌症。

    3'-substituted nucleoside derivatives
    54.
    发明授权
    3'-substituted nucleoside derivatives 失效
    3'-取代核苷衍生物

    公开(公告)号：US5763418A

    公开(公告)日：1998-06-09

    申请号：US693161

    申请日：1996-08-13

    申请人： Akira Matsuda ,  Sasaki Takuma

    发明人： Akira Matsuda ,  Sasaki Takuma

    IPC分类号： A61K31/7052 ,  A61P35/00 ,  C07H19/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  A61K31/70

    CPC分类号： C07H19/06 ,  C07H19/04 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  Y02P20/55

    摘要： The invention relates to a 3'-substituted nucleoside derivative represented by the following general formula (1): ##STR1## wherein B means a nucleic acid base which may have a substituent, Z represents a lower alkynyl or lower alkenyl group which may be substituted by a group represented by the formula: ##STR2## in which R.sup.a, R.sup.b and R.sup.c are individually a lower alkyl group or a phenyl group, or an oxiranyl group which may have at least one lower alkyl group, R.sup.1 and R.sup.2 individually represent H or an ester-forming residue capable of easily leaving in a living body, and R.sup.3 is H, a mono- or polyphosphoric acid residue, or an ester-forming residue capable of easily leaving in a living body, with the proviso that the sugar moiety is ribose, or a pharmaceutically acceptable salt thereof. The 3'-substituted nucleoside derivative according to the invention has an excellent antitumor activity and is hence useful for treatment for and prevention of cancers.

    摘要翻译： PCT No.PCT / JP95 / 02554 Sec。 371日期：1996年8月13日 102（e）日期1996年8月13日PCT 1995年12月13日PCT PCT。 WO96 / 18636 PCT公开号 日期：1996年6月20日本发明涉及由以下通式（1）表示的3'-取代核苷衍生物：其中B表示可具有取代基的核酸碱基，Z表示低级炔基 或低级链烯基，其可以被下式表示的基团取代：其中Ra，Rb和Rc分别是低级烷基或苯基，或可以具有至少一个的环氧乙烷基 低级烷基，R 1和R 2分别表示H或能够容易地在活体中离开的成酯残基，R3是H，单磷酸或多磷酸残基或能容易地离开的酯形成残基 活体，条件是糖部分是核糖，或其药学上可接受的盐。 根据本发明的3'-取代的核苷衍生物具有优异的抗肿瘤活性，因此可用于治疗和预防癌症。

    2'-methylidenepyrimidine nucleoside compounds
    55.
    发明授权
    2'-methylidenepyrimidine nucleoside compounds 失效
    2'-亚甲基嘧啶核苷化合物

    公开(公告)号：US5705630A

    公开(公告)日：1998-01-06

    申请号：US818656

    申请日：1992-01-07

    申请人： Tohru Ueda ,  Takuma Sasaki ,  Akira Matsuda ,  Keiji Yamagami ,  Akihiro Fujii

    发明人： Tohru Ueda ,  Takuma Sasaki ,  Akira Matsuda ,  Keiji Yamagami ,  Akihiro Fujii

    IPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/073

    CPC分类号： C07H19/06 ,  C07H19/10

    摘要： 2'-Methylidenepyrimidine nucleoside compounds of the general formula: ##STR1## wherein R.sup.1 stands for amino or hydroxy group; R.sup.2 stands for a halogen or a lower alkyl when R.sup.1 is amino or R.sup.2 stands for an alkyl having 2 to 4 carbon atoms, an alkynyl having 2 to 4 carbon atoms or a haloalkyl when R.sup.1 is hydroxy group; and R.sup.3 stands for hydrogen or a phosphoric acid residue, or salts thereof, anticancer compositions containing one or more of these compounds and methods for production of these compounds. Said compounds and salts thereof exhibit noticeable antitumor activities and are useful as anticancer agents.

    摘要翻译： 2'-亚甲基嘧啶核苷化合物，其通式如下：其中R1代表氨基或羟基; 当R 1为氨基或R 2表示具有2至4个碳原子的烷基，具有2至4个碳原子的炔基或R 1为羟基时的卤代烷基时，R 2表示卤素或低级烷基; R3表示氢或磷酸残基或其盐，含有这些化合物中的一种或多种的抗癌组合物及其制备方法。 所述化合物及其盐具有显着的抗肿瘤活性，可用作抗癌剂。

    2'methylidenepyrimidine nucleoside compounds, their use and method for production thereof
    59.
    发明授权
    2'methylidenepyrimidine nucleoside compounds, their use and method for production thereof 失效
    二亚甲基嘧啶核苷化合物，其用途及其制备方法

    公开(公告)号：US5401726A

    公开(公告)日：1995-03-28

    申请号：US44039

    申请日：1993-04-08

    申请人： Tohru Ueda ,  Takuma Sasaki ,  Akira Matsuda ,  Keiji Yamagami ,  Akihiro Fujii

    发明人： Tohru Ueda ,  Takuma Sasaki ,  Akira Matsuda ,  Keiji Yamagami ,  Akihiro Fujii

    IPC分类号： C07H19/06 ,  C07H19/10 ,  A61K31/70

    CPC分类号： C07H19/06 ,  C07H19/10

    摘要： 2'-Methylidenepyrimidine nucleoside compounds of the general formula: ##STR1## wherein R.sup.1 stands for amino or hydroxy group; R.sup.2 stands for a halogen or a lower alkyl when R.sup.1 is amino or R.sup.2 stands for an alkyl having 2 to 4 carbon atoms, an alkynyl having 2 to 4 carbon atoms or a haloalkyl when R.sup.1 is hydroxy group; and R.sup.3 stands for hydrogen or a phosphoric acid residue, or salts thereof, compositions containing one or more of these compounds and methods for production of these compounds are disclosed.Said compounds and salts thereof exhibit noticeable antitumor activities.

    摘要翻译： 2'-亚甲基嘧啶核苷化合物，其通式如下：其中R1代表氨基或羟基; 当R 1为氨基或R 2表示具有2至4个碳原子的烷基，具有2至4个碳原子的炔基或R 1为羟基时的卤代烷基时，R 2表示卤素或低级烷基; R3代表氢或磷酸残基，或其盐，含有这些化合物中的一种或多种的组合物和这些化合物的制备方法。 所述化合物及其盐具有显着的抗肿瘤活性。