公开(公告)号：EP0506048A1

公开(公告)日：1992-09-30

申请号：EP92105212.2

申请日：1992-03-26

申请人： DAINIPPON INK AND CHEMICALS, INC.

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

IPC分类号： C07H17/065 ,  A61K31/70

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 ∼ 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，以及包含硫酸化生育酚寡糖作为活性成分的抗病毒剂。 在生育酚低聚糖中，寡糖的末端糖部分的1位的羟基的氢原子由3个相同或不同的重复单糖单元组成，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糖，偶氮，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，并表现出改善的抗病毒作用，特别是针对人类免疫缺陷病毒。

公开(公告)号：EP0606882A1

公开(公告)日：1994-07-20

申请号：EP94100286.7

申请日：1994-01-11

申请人： DAINIPPON INK AND CHEMICALS, INC.

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

IPC分类号： C07H17/065 ,  C07H15/203 ,  C07H15/04 ,  C08B37/00 ,  A61K31/70

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低聚糖苷酰化物，其中通过这些单糖的糖苷键形成的寡糖在还原性末端糖的1位上的羟基中的氢被糖苷配基取代 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; 或其生理上可接受的盐，其中排除了其中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抗HIV病毒作用，特别是HIV的长效抗病毒作用。

公开(公告)号：EP0532026A3

公开(公告)日：1993-10-06

申请号：EP92115574.3

申请日：1992-09-11

申请人： DAINIPPON INK AND CHEMICALS, INC.

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

IPC分类号： C07H15/203 ,  A61K31/70 ,  C08B37/00 ,  A61K31/72

CPC分类号： C07H15/203 ,  C08B37/006

摘要： A oligosaccharide aromatic glycoside sulfate or a physiologically acceptable salt of the same which is formed from same or different monosaccharides bonded by glycoside bonds, wherein the hydrogen atom in the hydroxyl group at the position-1 carbon atom at the terminal of the oligosaccharide is substituted with a group represented by Formula (I):
        - Y - (O) n - R   (I)
(in the formula, R represents an alkyl group having 1-18 carbon atoms, n is 0 or 1, O represents an oxygen atom, and Y represents an allylene group) and at least 10% of the remaining hydroxyl groups of the sugar subunits have been subjected to sulfated esterification; an anti-viral agent containing this oligosaccharide aromatic glycoside sulfate or physiologically acceptable salt of the same as an active component; and a oligosaccharide aromatic glycoside which functions as a production intermediate are disclosed. The anti-viral agent exhibits low toxicity and superior anti-viral activity, and is especially effective against viruses which are known to cause AIDS.

公开(公告)号：EP0532026A2

公开(公告)日：1993-03-17

申请号：EP92115574.3

申请日：1992-09-11

申请人： DAINIPPON INK AND CHEMICALS, INC.

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

IPC分类号： C07H15/203 ,  A61K31/70 ,  C08B37/00 ,  A61K31/72

CPC分类号： C07H15/203 ,  C08B37/006

摘要： A oligosaccharide aromatic glycoside sulfate or a physiologically acceptable salt of the same which is formed from same or different monosaccharides bonded by glycoside bonds, wherein the hydrogen atom in the hydroxyl group at the position-1 carbon atom at the terminal of the oligosaccharide is substituted with a group represented by Formula (I):



        - Y - (O) n - R   (I)



(in the formula, R represents an alkyl group having 1-18 carbon atoms, n is 0 or 1, O represents an oxygen atom, and Y represents an allylene group) and at least 10% of the remaining hydroxyl groups of the sugar subunits have been subjected to sulfated esterification; an anti-viral agent containing this oligosaccharide aromatic glycoside sulfate or physiologically acceptable salt of the same as an active component; and a oligosaccharide aromatic glycoside which functions as a production intermediate are disclosed. The anti-viral agent exhibits low toxicity and superior anti-viral activity, and is especially effective against viruses which are known to cause AIDS.

摘要翻译： 由通过糖苷键键合的相同或不同的单糖形成的寡糖芳香糖苷硫酸盐或其生理学上可接受的盐，其中寡糖末端的位置-1个碳原子上的羟基中的氢原子被 式（I）表示的基团：-Y - （O）n -R（I>（式中，R表示碳原子数1〜18的烷基，n表示0或1，O表示氧原子， Y表示烯丙基），并且将糖亚基的剩余羟基中的至少10％进行硫酸酯化反应，含有该寡糖芳香族糖苷硫酸盐的抗病毒剂或与活性成分相同的生理学上可接受的盐 ;和作为生产中间体发挥作用的寡糖芳香糖苷，抗病毒剂具有低毒性和优良的抗病毒活性，特别有效对抗 已知导致艾滋病的病毒。