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    Sulfated oligoglycoside acylate and antiviral agent containing the same as active ingredient
    1.
    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。

    Quinolinone derivative, method for preparing the same, and anti-allergic agent
    3.
    发明授权
    Quinolinone derivative, method for preparing the same, and anti-allergic agent 有权
    喹啉酮衍生物，其制备方法和抗过敏剂

    公开(公告)号：US6136822A

    公开(公告)日：2000-10-24

    申请号：US201662

    申请日：1998-12-01

    申请人： Hidetsugu Takagaki ,  Shinobu Yamaguchi ,  Masayoshi Abe ,  Mitsuru Sakai ,  Osamu Misumi

    发明人： Hidetsugu Takagaki ,  Shinobu Yamaguchi ,  Masayoshi Abe ,  Mitsuru Sakai ,  Osamu Misumi

    IPC分类号： C07D215/22 ,  A61K31/00 ,  A61K31/47 ,  A61K31/4704 ,  A61P37/00 ,  A61P37/08 ,  C07C235/16 ,  C07D215/38 ,  C07D215/40 ,  C07D215/48 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D215/16 ,  C07D215/20 ,  C07D215/36

    CPC分类号： C07D215/22 ,  C07C235/16 ,  C07D215/38 ,  C07D215/40 ,  C07D215/48 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06

    摘要： The present invention relates to a simple method for preparing a quinolinone derivative, which is effective as a medicine, e.g., as an agent for treating allergic diseases and the like; novel amide derivatives effective as an intermediate in the method; novel quinolinone derivatives obtained according to the method; and an anti-allergic agent containing a quinolinone derivative and/or physiological salt of the same as the active ingredients. The quinolinone derivative is expressed by the following general formula (II); and the method is characterized in that an amide derivative, expressed by the following formula (I), is reacted with a basic agent, followed by intramolecular ring formation: ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkyl group containing a hydroxyl group an alkenyl group, or an aryl group; R.sub.2 represents an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; R.sub.3 represents a reactive carboxyl group; and R.sub.4 to R.sub.7 represent, respectively and independently, a hydrogen atom; a hydroxyl group; an alkyl group; an alkoxy group; an alkenyl group; an alkenyloxy group; an aryl group; an aryloxy group; an aralkyloxy group; a R.sub.8 R.sub.9 N group wherein R.sub.8 and R.sub.9 represent, respectively and independently, a hydrogen atom, an alkyl group, an alkenyl group an aralkyl group, or an acyl group; a nitro group; or a R.sub.10 OOC group wherein R.sub.10 represents a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; ##STR2## wherein R.sub.1, R.sub.2 and R.sub.4 to R.sub.7 represent, respectively, the same constituents as described in formula (I).

    摘要翻译： 本发明涉及一种制备喹啉酮衍生物的简单方法，其作为药物是有效的，例如用作治疗过敏性疾病等的药剂; 在该方法中作为中间体有效的新型酰胺衍生物; 按照该方法得到的新型喹啉酮衍生物; 以及含有与活性成分相同的喹啉酮衍生物和/或其生理盐的抗过敏剂。 喹啉酮衍生物由以下通式（II）表示; 该方法的特征在于将由下式（I）表示的酰胺衍生物与碱性试剂反应，然后分子内环形成：其中R 1表示氢原子，烷基，含有羟基的烷基 烯基或芳基; R2表示烷基，烯基，芳基或芳烷基; R3代表活性羧基; 和R 4至R 7分别独立地表示氢原子; 羟基; 烷基; 烷氧基 烯基; 烯氧基; 芳基; 芳氧基; 芳烷氧基; R8R9N基，其中R8和R9分别独立地表示氢原子，烷基，烯基，芳烷基或酰基; 硝基; 或R10OOC基，其中R10表示氢原子，烷基，烯基，芳基或芳烷基; 其中R1，R2和R4至R7分别表示与式（I）中所述相同的组分。

    Quinolinone derivative, method for preparing the same, and anti-allergic agent
    5.
    发明授权
    Quinolinone derivative, method for preparing the same, and anti-allergic agent 有权
    喹啉酮衍生物，其制备方法和抗过敏剂

    公开(公告)号：US06271416B1

    公开(公告)日：2001-08-07

    申请号：US09595909

    申请日：2000-06-20

    申请人： Hidetsugu Takagaki ,  Shinobu Yamaguchi ,  Masayoshi Abe ,  Mitsuru Sakai ,  Osamu Misumi

    发明人： Hidetsugu Takagaki ,  Shinobu Yamaguchi ,  Masayoshi Abe ,  Mitsuru Sakai ,  Osamu Misumi

    IPC分类号： C07C22900

    CPC分类号： C07D215/22 ,  C07C235/16 ,  C07D215/38 ,  C07D215/40 ,  C07D215/48 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06

    摘要： The present invention relates to a simple method for preparing a quinolinone derivative, which is effective as a medicine, e.g., as an agent for treating allergic diseases and the like; novel amide derivatives effective as an intermediate in the method, novel quinolinone derivatives obtained according to the method; and an anti-allergic agent containing a quinolinone derivative and/or physiological salt of the same as the active ingredients. The quinolinone derivative is expressed by the following general formula (II); and the method is characterized in that an amide derivative, expressed by the following general formula (I), is reacted with a basic agent, followed by intramolecular ring formation: General Formula (I) [wherein, R1 represents a hydrogen atom, an alkyl group, an alkyl group containing a hydroxyl group, an alkenyl group, or an aryl group; R2 represents an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; R3 represents a reactive carboxyl group; and R4 to R7 represent, respectively and independently, a hydrogen atom, a hydroxyl group, an alkyl group, an alkoxy group, an alkenyl group, an alkenyloxy group, an aryl group, an aryloxy group, an aralkyloxy group, a R8R9N group (wherein, R8 and R9 represent, respectively and independently, a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, or an acyl group), a nitro group, or a R10OOC group (wherein, R10 represents a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, or an aralkyl group)]. General Formula (II) [wherein, R1, R2 and R4 to R7 represent, respectively, the same constituents as described in general formula (I)].

    摘要翻译： 本发明涉及一种制备喹啉酮衍生物的简单方法，其作为药物是有效的，例如用作治疗过敏性疾病等的药剂; 该方法中作为中间体有效的新型酰胺衍生物，按照该方法得到的新型喹啉酮衍生物; 以及含有与活性成分相同的喹啉酮衍生物和/或其生理盐的抗过敏剂。 喹啉酮衍生物由以下通式（II）表示; 该方法的特征在于将由以下通式（I）表示的酰胺衍生物与碱性试剂反应，然后分子内环形成：通式（I）[其中，R 1表示氢原子，烷基 基团，含有羟基，烯基或芳基的烷基; R2表示烷基，烯基，芳基或芳烷基; R3代表活性羧基; R 4〜R 7分别独立地表示氢原子，羟基，烷基，烷氧基，烯基，烯氧基，芳基，芳氧基，芳烷氧基，R8R9N基（ 其中，R8和R9分别独立地表示氢原子，烷基，烯基，芳烷基或酰基），硝基或R10OOC基（其中，R10表示氢原子， 烷基，烯基，芳基或芳烷基）]通式（II）[其中，R1，R2和R4至R7分别表示与通式（I）中所述相同的组分] 。