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31 条记录 (耗时 0.031 秒)

    Fluorocytidine derivatives
    1.
    发明授权
    Fluorocytidine derivatives 失效
    氟胞嘧啶衍生物

    公开(公告)号：US4966891A

    公开(公告)日：1990-10-30

    申请号：US268437

    申请日：1988-11-08

    申请人： Morio Fujiu ,  Hideo Ishitsuka ,  Masanori Miwa ,  Isao Umeda ,  Kazuteru Yokose

    发明人： Morio Fujiu ,  Hideo Ishitsuka ,  Masanori Miwa ,  Isao Umeda ,  Kazuteru Yokose

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61P35/00 ,  C07H19/06 ,  C07H19/067

    CPC分类号： C07H19/06

    摘要： The novel 5'-deoxy-5-fluorocytidine derivatives of formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen or an easily hydrolyzable radical under physiological conditions, with the proviso that, at least one or R.sup.1, R.sup.2 and R.sup.3 is an easily hydrolyzable radical under physiological conditions,as well as hydrates of solvates of these compounds have antitumor properties. They can be prepared from compounds of formula I, wherein R.sup.1 is hydrogen or an amino-protecting radical and R.sup.2 and R.sup.3 are hydrogen or a hydroxy-protecting radical or taken together are a cyclic hydroxy-protecting radical.

    摘要翻译： 式（Ⅰ）的新的5'-脱氧-5-氟胞苷衍生物，其中R 1，R 2和R 3在生理条件下为氢或易水解的基团，条件是至少一个或R 1，R 2和R 3 在生理条件下是易水解的基团，以及这些化合物的溶剂合物的水合物具有抗肿瘤性质。 它们可以由式I化合物制备，其中R 1是氢或氨基保护基，并且R 2和R 3是氢或羟基保护基或一起是环状羟基保护基。

    N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine compounds, compositions and methods of using same
    2.
    发明授权
    N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine compounds, compositions and methods of using same 失效
    N4-（取代氧羰基）-5'-脱氧-5-氟胞苷化合物，组合物及其使用方法

    公开(公告)号：US5472949A

    公开(公告)日：1995-12-05

    申请号：US167392

    申请日：1993-12-14

    申请人： Motohiro Arasaki ,  Hideo Ishitsuka ,  Isami Kuruma ,  Masanori Miwa ,  Chikako Murasaki ,  Nobuo Shimma ,  Isao Umeda

    发明人： Motohiro Arasaki ,  Hideo Ishitsuka ,  Isami Kuruma ,  Masanori Miwa ,  Chikako Murasaki ,  Nobuo Shimma ,  Isao Umeda

    IPC分类号： A61K31/70 ,  A61K31/305 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61P35/00 ,  C07D239/00 ,  C07H19/06

    CPC分类号： C07H19/06 ,  Y02P20/55

    摘要： The invention relates to N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives which are useful as an agent for treating tumors, pharmaceutical compositions including the same, a method of treating tumors and a method of preparing N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives for treating tumors.Compounds of formula (I), ##STR1## wherein R.sup.1 is a saturated or unsaturated, straight or branched hydrocarbon radical wherein the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven, or is a radical of the formula --(CH.sub.2)n--.sup.Y wherein Y is a cyclohexyl radical, a C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical and wherein when Y is a cyclohexyl radical n is an integer from 0 to 4, and when Y is C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical n is an integer from 2 to 4, and R.sup.2 is a hydrogen atom or a radical easily hydrolyzable under physiological conditions,or a hydrate or solvate thereof. Compounds of formula (I) are useful in the treatment of tumors.

    摘要翻译： 本发明涉及可用作治疗肿瘤的药物的N4-（取代 - 氧代羰基）-5'-脱氧-5-氟胞苷衍生物，包含其的药物组合物，治疗肿瘤的方法和制备N4-（ 取代氧羰基）-5'-脱氧-5-氟胞苷衍生物用于治疗肿瘤。 式（I）化合物，其中R1是饱和或不饱和的直链或支链烃基，其中该烃基的最长直链中的碳原子数范围为3-7，或者是 基团 - （CH 2）n Y其中Y是环己基，C 1 -C 4烷氧基或苯基，并且其中当Y是环己基时，n是0-4的整数，当Y是C 1 -C 4 烷氧基或苯基n是2〜4的整数，R2是氢原子或在生理条件下易水解的基团，或其水合物或溶剂合物。 式（I）化合物可用于治疗肿瘤。

    Water-insoluble medicine
    6.
    发明授权
    Water-insoluble medicine 失效
    水不溶性药

    公开(公告)号：US08399024B2

    公开(公告)日：2013-03-19

    申请号：US12879413

    申请日：2010-09-10

    申请人： Hiroyuki Kato ,  Isao Umeda ,  Kazuo Watanabe ,  Kazuya Hirata ,  Akio Ishiguro ,  Tetsu Go

    发明人： Hiroyuki Kato ,  Isao Umeda ,  Kazuo Watanabe ,  Kazuya Hirata ,  Akio Ishiguro ,  Tetsu Go

    IPC分类号： A61K9/14 ,  A61K31/44 ,  A61K9/127 ,  C21C1/00

    CPC分类号： A61K9/146 ,  A61K9/5161 ,  A61K31/44

    摘要： A method of producing water-insoluble anti-cancer drug in the form of particulates, the method including preparing a water-insoluble anti-cancer drug having at least one multiple bond in the structure, and irradiating said water-insoluble anti-cancer drug with a laser beam having a wavelength of a low absorption portion in the vicinity of the foot of an absorption curve on the long wavelength side within the absorption band until said water-insoluble anti-cancer drug is formed into particulates having an average particle diameter of 50 to 200 nm.

    摘要翻译： 一种以微粒形式生产不溶于水的抗癌药物的方法，该方法包括制备结构中具有至少一个多重键的水不溶性抗癌药物，并将所述水不溶性抗癌药物与 在吸收带内的长波长侧的吸收曲线的脚附近具有低吸收部分的波长的激光束，直到所述水不溶性抗癌药物形成具有平均粒径为50微米的颗粒 至200nm。

    Preventive or Therapeutic Agents for Pancreatic Cancer, Ovarian Cancer, or Liver Cancer Comprising a Novel Water-Soluble Prodrug
    9.
    发明申请
    Preventive or Therapeutic Agents for Pancreatic Cancer, Ovarian Cancer, or Liver Cancer Comprising a Novel Water-Soluble Prodrug 审中-公开
    包含新型水溶性前体药物的胰腺癌，卵巢癌或肝癌的预防或治疗剂

    公开(公告)号：US20090118271A1

    公开(公告)日：2009-05-07

    申请号：US12083831

    申请日：2006-10-19

    申请人： Isao Umeda ,  Jun Ohwada ,  Sawako Ozawa ,  Mika Endo ,  Masako Ura

    发明人： Isao Umeda ,  Jun Ohwada ,  Sawako Ozawa ,  Mika Endo ,  Masako Ura

    IPC分类号： A61K31/5377 ,  C07D491/22 ,  A61K31/519 ,  A61P35/00 ,  A61K31/4375

    CPC分类号： C07D491/22 ,  A61K31/519

    摘要： Preventive or therapeutic agents for pancreatic cancer, ovarian cancer, or liver cancer of the present invention comprise a water-soluble prodrug represented by formula 1 described below, or a pharmaceutically acceptable salt, or a hydrate or solvate of the prodrug or pharmaceutically acceptable salt, (wherein, R1 represents a hydrogen atom, or a C1-C6 alkyl group; W represents a divalent group comprising a tertiary amino group or a divalent group comprising a sulfonyl group, and Y represents a residue of a compound represented by Y—OH comprising an alcoholic hydroxyl group, wherein said Y—OH is a camptothecin, a taxane, or an anticancer nucleotide).

    摘要翻译： 本发明的胰腺癌，卵巢癌或肝癌的预防或治疗剂包含由下述式1表示的水溶性前药或其前药或药学上可接受的盐的药学上可接受的盐或水合物或溶剂合物， （其中，R1表示氢原子或C1-C6烷基; W表示包含叔氨基或包含磺酰基的二价基团的二价基团，Y表示由Y-OH表示的化合物的残基，包括 醇羟基，其中所述Y-OH是喜树碱，紫杉烷或抗癌核苷酸）。