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    Method of designing molecular structure of enzyme inhibitor
    2.
    发明申请
    Method of designing molecular structure of enzyme inhibitor 审中-公开
    酶抑制剂分子结构设计方法

    公开(公告)号：US20040093169A1

    公开(公告)日：2004-05-13

    申请号：US10448871

    申请日：2003-05-29

    申请人： TOYO SUISAN KAISHA, LTD.

    发明人： Yoshiyuki Mizushina ,  Kengo Sakaguchi ,  Fumio Sugawara

    IPC分类号： G06F019/00 ,  G01N033/48 ,  G06G007/48 ,  A01N037/18 ,  A01N043/04

    CPC分类号： C07B61/00 ,  G16B15/00 ,  G16B20/00

    摘要： A method of designing a molecular structure of an inhibitor of a target enzyme by analyzing, in the tertiary structure of a first enzyme, a geometric configuration formed by amino acids to which an inhibitor on the first enzyme is to bind. The method comprises (1) a step of determining the amino acid group of the first enzyme to which the inhibitor is to bind, (2) a step of determining the geometric configuration of the amino acid group of the step (1), (3) a step of searching for an amino acid group having a geometric configuration similar to that of the step (2), in the target enzyme, and (4) a step of searching weather or not (i) the amino acids constituting the amino acid group are present at the surface of the target enzyme, and (ii) the amino acids have been conserved in different species by comparison with an enzyme derived from an organism of different types from the organism from which the target enzyme is derived. When the requirements are satisfied, it is assumed that the geometric configuration formed by amino acids to which the inhibitor of the first enzyme is to bind, is also present in the target enzyme, then the molecular structure of an inhibitor of the target enzyme is designed.

    摘要翻译： 通过在第一酶的三级结构中分析由第一种酶上的抑制剂结合的氨基酸形成的几何构型，来设计靶酶抑制剂的分子结构的方法。 该方法包括：（1）确定抑制剂结合的第一酶的氨基酸基团的步骤，（2）确定步骤（1）的氨基酸组的几何构型的步骤，（3） ）在目标酶中搜索具有类似于步骤（2）的几何构型的氨基酸基团的步骤，和（4）搜寻天气的步骤（i）构成氨基酸的氨基酸 基团存在于目标酶的表面，并且（ii）通过与源自来自靶酶的生物体的不同类型的生物体的酶进行比较，（II）氨基酸已被保守在不同的物种中。 当满足要求时，假定由第一酶的抑制剂所结合的氨基酸形成的几何构型也存在于靶酶中，则设计靶酶抑制剂的分子结构 。

    Method for treating cancer
    6.
    发明申请
    Method for treating cancer 失效
    癌症治疗方法

    公开(公告)号：US20040067893A1

    公开(公告)日：2004-04-08

    申请号：US10678193

    申请日：2003-10-02

    申请人： TOYO SUISAN KAISHA, LTD.

    发明人： Takayuki Yamazaki ,  Fumio Sugawara ,  Keisuke Ohta ,  Kazuyoshi Masaki ,  Kotaro Nakayama ,  Kengo Sakaguchi ,  Noriyuki Sato ,  Hiroeki Sahara ,  Tatsuya Fujita

    IPC分类号： A61K031/70

    CPC分类号： A61K31/70 ,  A61K31/7032 ,  C07H15/06

    摘要： A method for treating a cancer. The cancer excluding an adenocarcinoma and being epithelioma, glioma, sarcoma, melanoma, lymphoma or leukemia; or the cancer is an adenocarcinoma cancer excluding colon cancer, lung cancer and gastric cancer. The method comprises administering to a subject in need thereof and suffering from cancer, a pharmaceutically effective amount of at least one sulfoquinovosylacylglycerol compound represented by formula (1): 1 wherein R101 represents an acyl residue of an unsaturated fatty acid and R102 represents a hydrogen atom and/or at least one pharmaceutically acceptable salt thereof.

    摘要翻译： 一种治疗癌症的方法。 不包括腺癌并且是上皮瘤，神经胶质瘤，肉瘤，黑素瘤，淋巴瘤或白血病的癌症; 或癌症是排除结肠癌，肺癌和胃癌的腺癌。 该方法包括向有需要的受试者和患有癌症的药物有效量的至少一种由式（1）表示的磺基秋水诺酰基甘油化合物：其中R 101表示不饱和脂肪酸的酰基残基，R 102表示氢原子， /或其至少一种药学上可接受的盐。

    Novel sulfoquinovosylacylglycerol derivative, and use thereof as medicaments
    7.
    发明申请
    Novel sulfoquinovosylacylglycerol derivative, and use thereof as medicaments 失效
    新型磺基秋水仙酰基甘油衍生物及其作为药物的用途

    公开(公告)号：US20020052327A1

    公开(公告)日：2002-05-02

    申请号：US09949907

    申请日：2001-09-10

    申请人： TOYO SUISAN KAISHA, LTD.

    发明人： Takayuki Yamazaki ,  Fumio Sugawara ,  Keisuke Ohta ,  Kazuyoshi Masaki ,  Kotaro Nakayama ,  Kengo Sakaguchi ,  Noriyuki Sato ,  Hiroeki Sahara ,  Tatsuya Fujita

    IPC分类号： A61K031/70 ,  C07H015/00

    CPC分类号： C07H15/04 ,  A61K31/7032 ,  C07H13/00

    摘要： A method for immunosuppression in a subject comprising administering to the subject in need thereof, a pharmaceutically effective amount of at least one sulfoquinovosylacylglycerol derivative represented by General formula (1-1): 1 wherein R101 represents an acyl residue of a higher fatty acid, and R102 represents a hydrogen atom or an acyl residue of a higher fatty acid; and a pharmaceutically acceptable salt thereof. Of the sulfoquinovosylacylglycerol derivatives, null-sulfoquinovosylacylglycerols are novel compounds. The present invention also relates to pharmaceutical composition comprising a pharmaceutically effective amount of the null-sulfoquinovosylacylglycerols and/or its pharmaceutically acceptable salt; and a pharmaceutically acceptable excipient. The pharmaceutical composition may be used as an immunosuppressive agent, anticancer agent and DNA polymerase null inhibitor.

    摘要翻译： 一种受试者的免疫抑制方法，包括向有需要的受试者施用药学上有效量的通式（1-1）表示的至少一种磺基秋水仙酰基甘油衍生物：其中，R 101表示高级脂肪酸的酰基残基，R 102 表示氢原子或高级脂肪酸的酰基残基; 及其药学上可接受的盐。 在磺基奎诺糖基酰基甘油衍生物中，β-磺基奎诺乙酰基酰基甘油是新化合物。 本发明还涉及药物组合物，其包含药学上有效量的β-磺基奎诺乙酰基酰基甘油和/或其药学上可接受的盐; 和药学上可接受的赋形剂。 药物组合物可以用作免疫抑制剂，抗癌剂和DNA聚合酶α抑制剂。