利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

18 条记录 (耗时 0.033 秒)

    2'-methylidenepyrimidine nucleoside compounds
    2.
    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
    3.
    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。

    Antineoplastic 5'-diacylglycerylphosphatidyl-2-deoxy-2'-methylenylcytidines and method of making
    4.
    发明授权
    Antineoplastic 5'-diacylglycerylphosphatidyl-2-deoxy-2'-methylenylcytidines and method of making 失效
    抗肿瘤性5'-二酰基甘油基磷脂酰基-2-脱氧-2'-亚甲基胞苷及其制备方法

    公开(公告)号：US5696097A

    公开(公告)日：1997-12-09

    申请号：US525606

    申请日：1995-09-15

    申请人： Akira Matsuda ,  Takuma Sasaki ,  Satoshi Shutou ,  Akihiro Fujii ,  Takashi Ono ,  Shinji Sakata ,  Takanori Miyashita

    发明人： Akira Matsuda ,  Takuma Sasaki ,  Satoshi Shutou ,  Akihiro Fujii ,  Takashi Ono ,  Shinji Sakata ,  Takanori Miyashita

    IPC分类号： C07H19/10 ,  A61K31/70 ,  C07H19/207

    CPC分类号： C07H19/10

    摘要： Novel 2'-methylidenenucleotide compounds of the formula (I) ##STR1## wherein R is a hydrogen or a halogen, R.sup.1 and R.sup.2 are the same or different and each is a fatty acid residue or a hydrocarbon residue, and R.sup.3 and R.sup.4 are the same or different and each is a hydrogen, a halogen or an alkyl; salts thereof; methods for production thereof; and pharmaceutical use thereof. The compounds and salts thereof show an excellent antitumor effect in mammals. More specifically, they show a remarkable activity of inhibiting growth of mouse tumors, cultured human tumor cells, and human tumors transplanted to nude mice, and are useful for the treatment and prevention of recurrence of lung cancer, gastrointestinal cancer, breast cancer, cervical cancer, gynecological cancer, urinological cancer, leukemia, melanoma, lymphogenous metastatic tumor and the like in mammals. They are also useful as antitumor agents since they have an increased bioavailability and low toxicity. In addition, they have the effects of maintaining and enhancing their activities.

    摘要翻译： PCT No.PCT / JP94 / 00427 Sec。 371 1995年9月15日第 102（e）日期1995年9月15日PCT 1994年3月16日PCT公布。 第WO94 / 21659号公报 日期1994年9月29日新颖的式（I）的2'-亚甲基二核苷酸化合物其中R是氢或卤素，R 1和R 2相同或不同，各自为脂肪酸残基或烃 残基，R 3和R 4相同或不同，各自为氢，卤素或烷基; 的盐; 生产方法; 及其药物用途。 其化合物和盐在哺乳动物中表现出优异的抗肿瘤效果。 更具体地说，它们显示了抑制小鼠肿瘤，培养的人肿瘤细胞和移植到裸鼠的人肿瘤生长的显着活性，并且可用于治疗和预防肺癌，胃肠癌，乳腺癌，宫颈癌的复发 ，妇科癌症，尿毒症，白血病，黑素瘤，淋巴瘤转移瘤等。 它们也可用作抗肿瘤剂，因为它们具有增加的生物利用度和低毒性。 此外，它们还具有维护和增强活动的效果。

    Imidazole derivatives and use thereof
    5.
    发明授权
    Imidazole derivatives and use thereof 失效
    咪唑衍生物及其用途

    公开(公告)号：US5126361A

    公开(公告)日：1992-06-30

    申请号：US702210

    申请日：1991-05-15

    申请人： Tohru Ueda ,  Akira Matsuda ,  Noriaki Minakawa ,  Takuma Sasaki ,  Yoshikazu Yanagi

    发明人： Tohru Ueda ,  Akira Matsuda ,  Noriaki Minakawa ,  Takuma Sasaki ,  Yoshikazu Yanagi

    IPC分类号： C07D233/90 ,  C07H19/052

    CPC分类号： C07H19/052 ,  C07D233/90 ,  Y02P20/55

    摘要： Disclosed are imidazole derivatives represented by formula [I]: ##STR1## wherein R is a hydrogen atom or ##STR2## wherein R.sup.2 is a hydrogen atom or a hydroxy protecting group, R.sup.2 protecting either a single hydroxy or two hydroxies together when R.sup.2 is a hydroxy protecting group, and R.sup.3 is a hydrogen atom or OR.sup.2 ; A is CONH.sub.2 or CN; and R.sup.1 is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl.Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position.Furthermore, the compounds have remarkable antitumor activities and therefore can provide novel antitumor agents.

    3′-substituted nucleoside derivative
    10.
    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。