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    Sulfated tocopheryl oligosaccharides and antiviral agents including the same as active ingredients
    6.
    发明授权
    Sulfated tocopheryl oligosaccharides and antiviral agents including the same as active ingredients 失效
    硫酸化生育酚低聚糖和包括与活性成分相同的抗病毒剂

    公开(公告)号：US5280111A

    公开(公告)日：1994-01-18

    申请号：US856710

    申请日：1992-03-24

    申请人： Tadao Shoji ,  Naoya Ikushima ,  Kaname Katsuraya ,  Nahoko Takahashi ,  Fusayo Kobayashi ,  Toshiyuki Uryu ,  Takashi Yoshida ,  Naoki Yamamoto ,  Hideki Nakashima

    发明人： Tadao Shoji ,  Naoya Ikushima ,  Kaname Katsuraya ,  Nahoko Takahashi ,  Fusayo Kobayashi ,  Toshiyuki Uryu ,  Takashi Yoshida ,  Naoki Yamamoto ,  Hideki Nakashima

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/12 ,  A61P31/18 ,  C07H17/065 ,  C07H15/20 ,  A61K31/72 ,  C07H11/00 ,  C07H13/02 ,  C07H17/04

    CPC分类号： C07H17/065 ,  A61K31/70

    摘要： The present invention relates to novel tocopheryl oligosaccharides, acylated tocopheryl oligosaccharides, sulfated tocopheryl oligosaccharides, and antiviral agents including the sulfated tocopheryl oligosaccharides as active ingredients. In the tocopheryl oligosaccharide, the hydrogen atom of the hydroxy group at the 1-position in the terminal sugar moiety of an oligosaccharide which consists of 3.about.20 of identical or different repeating monosaccharide units selected from the group consisting of glucose, galactose, mannose, talose, idose, altrose, allose, glucose, xylose, arabinose, rhamnose, fucose, and fructose, which are glycoside-linked, is substituted by a tocopherol group. In the acylated tocopheryl oligosaccharides, each of any hydroxy group of the sugar moiety, other than the hydroxy group at the 1-position in the terminal sugar moiety of the oligosaccharide described above, is protected by an acyl group. The antiviral agents including the sulfated tocopheryl oligosaccharides or the biologically acceptable salt of the same as active ingredients have low toxicities and exhibit improved antiviral action, especially against the Human Immunodeficiency Virus.

    摘要翻译： 本发明涉及新的生育酚低聚糖，酰化生育酚低聚糖，硫酸生育酚寡糖，以及包含硫酸生育酚寡糖作为活性成分的抗病毒剂。 在生育酚低聚糖中，低聚糖的末端糖部分的1位的羟基的氢原子由3〜20个相同或不同的重复单糖单元组成，所述重复单糖单元选自葡萄糖，半乳糖，甘露糖， 与糖生成酚基取代的与糖苷连接的谷氨酸，阿糖，阿卓糖，阿洛糖，葡萄糖，木糖，阿拉伯糖，鼠李糖，岩藻糖和果糖。 在酰化的生育酚低聚糖中，除了上述寡糖的末端糖部分的1位以外的除了羟基以外的糖部分的任何羟基都被酰基保护。 包括硫酸生育酚寡糖或与生物活性成分相同的生物学上可接受的盐的抗病毒剂具有低毒性，并且表现出改善的抗病毒作用，特别是针对人类免疫缺陷病毒。

    Sulfated oligoglycoside acylate and antiviral agent containing the same as active ingredient
    7.
    发明授权
    Sulfated oligoglycoside acylate and antiviral agent containing the same as active ingredient 失效
    硫酸低聚糖苷酰化物和含有与活性成分相同的抗病毒剂

    公开(公告)号：US5459257A

    公开(公告)日：1995-10-17

    申请号：US179623

    申请日：1994-01-07

    申请人： Tadao Shoji ,  Akira Kasai ,  Osamu Misumi ,  Naoya Ikushima ,  Naoki Yamamoto ,  Hideki Nakashima ,  Kazuhiko Inazawa ,  Nahoko Takahashi

    发明人： Tadao Shoji ,  Akira Kasai ,  Osamu Misumi ,  Naoya Ikushima ,  Naoki Yamamoto ,  Hideki Nakashima ,  Kazuhiko Inazawa ,  Nahoko Takahashi

    IPC分类号： C07H15/04 ,  C07H15/203 ,  C07H17/065 ,  C07H13/12 ,  C07H11/00

    CPC分类号： C07H15/203 ,  C07H15/04 ,  C07H17/065

    摘要： A sulfated oligoglycoside acylate comprising monosaccharides of a single or two kinds as the constituents, wherein the hydrogen in the hydroxyl group at the 1-position of a reducing end sugar of the oligosaccharide formed via the glycoside bond of these monosaccharides has been substituted with an aglycon selected from a group consisting of alkyl groups, aromatic alkyl groups, aromatic alkoxy groups and tocopheryl groups; from 12 to 80% of the residual hydroxyl groups have been acylated with an acyl group selected from a group consisting of aliphatic acyl groups and aromatic acyl groups; and 88 to 20% thereof have been sulfated; or a physiologically acceptable salt thereof provided that compounds wherein the aglycon is an alkyl group and the acyl group is an aliphatic acyl group are excluded is disclosed. Further, an antiviral agent, which exerts a long-lasting antiviral action particularly on HIV, containing said compound as an active ingredient is disclosed.

    摘要翻译： 一种包含单一或两种单糖作为组分的硫酸化寡糖苷酰化物，其中通过这些单糖的糖苷键形成的寡糖的还原性末端糖在1位羟基中的氢被aglycon取代 选自烷基，芳族烷基，芳族烷氧基和生育酚基; 残余羟基的12至80％已经用选自脂族酰基和芳族酰基的酰基酰化; 88％〜20％已被硫酸化; 或其生理学上可接受的盐，其中排除了糖苷配基是烷基和酰基是脂族酰基的化合物。 此外，公开了以含有所述化合物作为有效成分的对HIV特别施加长效抗病毒作用的抗病毒剂。

    Oligosaccharide aromatic glycoside and sulfate thereof
    8.
    发明授权
    Oligosaccharide aromatic glycoside and sulfate thereof 失效
    寡糖芳香糖苷及其硫酸盐

    公开(公告)号：US5498602A

    公开(公告)日：1996-03-12

    申请号：US944077

    申请日：1992-09-11

    申请人： Tadao Shoji ,  Nahoko Takahashi ,  Naoya Ikushima ,  Toshiyuki Uryu ,  Takashi Yoshida ,  Naoki Yamamoto ,  Hideki Nakashima ,  Kaname Katsuraya ,  Koichiro Adachi ,  Fusayo Kataoka

    发明人： Tadao Shoji ,  Nahoko Takahashi ,  Naoya Ikushima ,  Toshiyuki Uryu ,  Takashi Yoshida ,  Naoki Yamamoto ,  Hideki Nakashima ,  Kaname Katsuraya ,  Koichiro Adachi ,  Fusayo Kataoka

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61P31/12 ,  A61P31/18 ,  C07H15/203 ,  C08B37/00 ,  C07G3/00 ,  C07H11/00

    CPC分类号： C07H15/203 ,  C08B37/006

    摘要： Oligosaccharide aromatic glycoside sulfates and physiologically acceptable salts thereof, are disclosed. Further, antiviral agents having these sulfate compounds as the active components, and particularly an antiviral agent, wherein the virus is one which causes AIDS (Acquired Immune Deficiency Syndrome), are disclosed. The active components or the glycoside sulfates, and the salts thereof, are characterized by an oligosaccharide aromatic glycoside sulfate in which the hydrogen of the position-1 hydroxyl group of the terminal sugar of an oligosaccharide is substituted with a specified formula having an alkyl group consisting of 1 to 18 carbons, an oxygen or no oxygen, and an allylene group. The number of constituent monosaccharides in the oligosaccharide portion is preferably within a range of 2 to 20. Further, 10% or more of the remaining hydroxyl groups of the sugar subunits are subjected to sulfated esterification. In addition the antiviral agent exhibits low toxicity and is useful in the treatment of AIDS. Furthermore, an oligosaccharide is also disclosed as described above with the exception that it is the hydrogen atom of the position 1 hydrogen group at the terminal sugar residue which is substituted with the specified formula, also described above. However, in addition the remaining hydroxyl groups of the sugar portion of this oligosaccharide are protected by acyl groups or are present in an unprotected form. Also disclosed is a method for the production of an oligosaccharide aromatic glycoside sulfate synthesized by sulfation using a sulfating agent.

    摘要翻译： 公开了寡糖芳香糖苷硫酸盐及其生理上可接受的盐。 此外，公开了具有这些硫酸盐化合物作为活性成分的抗病毒剂，特别是其中病毒是引起AIDS（获得性免疫缺陷综合征）的抗病毒剂。 活性成分或糖苷硫酸盐及其盐的特征在于寡糖芳香糖苷硫酸盐，其中寡糖末端糖的位置1羟基的氢被具有烷基的特定式所取代， 1至18个碳，氧或无氧，以及烯丙基。 寡糖部分中的构成单糖的数量优选在2〜20的范围内。此外，将糖亚基的剩余羟基的10％以上进行硫酸化酯化。 此外，抗病毒剂的毒性低，可用于治疗艾滋病。 此外，还公开了如上所述的寡糖，不同之处在于它是上述也被指定式取代的末端糖残基上的1位氢原子的氢原子。 然而，此外，该寡糖的糖部分的剩余羟基由酰基保护或以未保护的形式存在。 还公开了通过使用硫酸化剂硫酸化合成的寡糖芳香族糖苷硫酸盐的制造方法。