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    (Oxo-)xanthene derivatives, their preparation and their use as immunomodulators
    1.
    发明公开
    (Oxo-)xanthene derivatives, their preparation and their use as immunomodulators 失效
    （Oxo-）Xanthen Derivate，deren Herstellung und deren Verwendung als Immunmodulatoren

    公开(公告)号：EP0795554A3

    公开(公告)日：1998-01-28

    申请号：EP97301438.4

    申请日：1997-03-04

    申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.

    发明人： Hida, Tsuneaki ,  Hattori, Masahiko ,  Kurokawa, Tsutomu ,  Nakanishi, Atsushi

    IPC分类号： C07D311/86 ,  C07D311/82 ,  A61K31/35 ,  C07D405/12 ,  A61K31/41 ,  C07D407/12 ,  A61K31/44 ,  C07D409/04 ,  A61K31/38 ,  C07D407/04 ,  C12P17/06 ,  C12N1/15

    CPC分类号： C07D405/12 ,  C07D311/82 ,  C07D311/86 ,  C07D407/04 ,  C07D409/04 ,  C07K14/70521

    摘要： Xanthene derivatives represented by the general formula:
    wherein R 1 is a carboxyl group which may be esterified or amidated; R 2 is a hydrogen atom, a hydroxyl group, or a hydrocarbon group which may be substituted; R 3 and R 4 are the same or different and are a hydroxyl group which may be substituted; R 5 and R 6 are a hydrogen atom or a halogen atom; R 7 is a hydrogen atom, a nitro group, a halogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, or an acyl group which may be substituted; n is an integer of 0 to 2; and Y is an oxygen atom or two hydrogen atoms; and when n is 0, R 2 may be a group represented by the formula:
    wherein the symbols have the same meanings as defined above, or a salt thereof inhibit a binding of B7-1 to CD28, prevent the B7-1-dependent activation of T cells and inhibit IL-2 production from T cells, thus being used as an immunomodulator such as a graft rejection inhibitor or a pharmaceutical composition for therapeutic treatment of allergy, rheumatoid arthritis, autoimmune disease, nephritis, diabetes mellitus and so on.

    摘要翻译： 由以下通式表示的呫吨衍生物：其中R 1是可被酯化或酰胺化的羧基; R 2是氢原子，羟基或可被取代的烃基; R 3和R 4相同或不同，为可被取代的羟基; R 5和R 6是氢原子或卤素原子; R 7为氢原子，硝基，卤素原子，可被取代的烃基，可被取代的杂环基或可被取代的酰基; n为0〜2的整数， Y是氧原子或两个氢原子; 当n为0时，R 2可以是由下式表示的基团：其中符号具有与上述相同的含义，或其盐抑制B7-1与CD28的结合，防止B7 -1依赖性激活T细胞并抑制T细胞的IL-2产生，因此被用作免疫调节剂如移植排斥抑制剂或用于治疗过敏，类风湿性关节炎，自身免疫性疾病，肾炎，糖尿病的药物组合物 等等; 以及能够产生一些根据式（I）的化合物的微生物霉菌（Aspergillus terreus）的FL-67283菌株; 以及用于筛选具有抑制或增强CD28与B7-1或其盐的结合活性的化合物的方法，其包括比较（1）当CHO（CHO）时获得的CD28和B7-1-Ig之间的结合量 含有CD28的细胞或其细胞膜级分与可溶性B7-1-Ig接触，（2）当含有CD28或其细胞膜级分的CHO细胞接触时获得的CD28和B7-1-Ig之间的结合量 可溶性B7-1-Ig和试验化合物; 和由CD28-CHO-11（FERM BP-5431）表示的CHO细胞，由B7-1-CHO-22（FERM BP-5430）表示的CHO细胞或由sB7-1-Ig-CHO- 20（FERM BP-5432）。

    TAN-1511, its derivatives, production and use thereof
    4.
    发明公开
    TAN-1511, its derivatives, production and use thereof 失效
    TAN-1511，Derivate，Herstellung und Verwendung。

    公开(公告)号：EP0604945A1

    公开(公告)日：1994-07-06

    申请号：EP93120952.2

    申请日：1993-12-27

    申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.

    发明人： Tanida, Seiichi ,  Hida, Tsuneaki ,  Wakimasu, Mitsuhiro

    IPC分类号： C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K7/06 ,  A61K37/02

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/0606 ,  C07K5/081 ,  C07K5/1013

    摘要： A compound of the formula:

    wherein each R¹, R² and R³ is an aliphatic acyl group, X is an amino acid sequence consisting of 1 to 5 amino acid residues which contain at least one acidic amino acid residue, n is an integer of 0 to 4, provided that when n is 0, X has glutamyl-glycyl at its N-terminal and when n is 1 or 2, the acidic amino acid residue is an acidic amino acid residue other than D-glutamyl, or a salt thereof has an activity of remarkably improving anhematopoiesis and is useful as an immuno-stimulating agent having a leukocyte-increasing activity.

    摘要翻译： 下式化合物：其中R 1，R 2和R 3各自为脂族酰基，X为1至5个氨基酸残基的氨基酸序列，其含有至少一个 酸性氨基酸残基，n为0〜4的整数，条件是当n为0时，X在其N-末端具有谷氨酰基 - 甘氨酰，当n为1或2时，酸性氨基酸残基为酸性氨基酸残基 除了D-谷氨酰，或其盐具有显着改善致血细胞生成的活性，并且可用作具有白细胞增加活性的免疫刺激剂。

    Physiologically active substance tan-931, its derivatives, their production and use
    7.
    发明公开
    Physiologically active substance tan-931, its derivatives, their production and use 失效
    Physiologisch aktive Substanz tan-931，ihre Derivate，ihre Herstellung und Verwendung。

    公开(公告)号：EP0342665A2

    公开(公告)日：1989-11-23

    申请号：EP89108926.0

    申请日：1989-05-18

    申请人： Takeda Chemical Industries, Ltd.

    发明人： Kanamaru, Tsuneo ,  Hida, Tsuneaki ,  Muroi,, Masayuki

    IPC分类号： C07C65/42 ,  A61K31/19 ,  A61K31/235 ,  C07D265/30

    CPC分类号： C07D295/192 ,  C07C65/40 ,  C07C65/42 ,  C07C235/84 ,  C07D313/12

    摘要： A novel compound of the formula (I):
    wherein R₁ is optionally esterified or amidated carboxyl; R₂, R₃ and R₄ are the same or different and are hydrogen or alkyl; A is fcrmyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R₁ is carboxyl, R₂, R₃ and R₄ are hydrogen and X is formyl are also disclosed.

    摘要翻译： 式（I）的新型化合物：其中R 1任选被酯化或酰胺化的羧基; R2，R3和R4相同或不同，为氢或烷基; A是fcrmyl，羟基亚氨基甲基或羧基; 并且X是氢或卤素或其盐，其可用作芳香酶抑制剂或其生产的中间体。 制备式（I）化合物的方法和含有作为活性成分的式（I）化合物的芳香酶抑制剂的方法，其中A是甲酰基，X是氢，或其盐，以及能产生青霉素的青霉菌（Penicillium funiculosum） 还公开了其中R 1是羧基，R 2，R 3和R 4是氢并且X是甲酰基的化合物（I）。

    Derivatives of 6,7-Dihydroxy-4-thiaheptonic acid and their use
    10.
    发明公开
    Derivatives of 6,7-Dihydroxy-4-thiaheptonic acid and their use 失效
    衍生自6,7-二羟基-4-thiaheptansäureund deren Verwendung。

    公开(公告)号：EP0638588A1

    公开(公告)日：1995-02-15

    申请号：EP94111469.6

    申请日：1994-07-22

    申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.

    发明人： Hida, Tsuneaki ,  Tanida, Seiichi ,  Harada, Setsuo ,  Yukishige, Koichi

    IPC分类号： C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K7/06

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/1021 ,  C07K7/02 ,  Y02P20/55

    摘要： A compound of the formula:

    wherein each of R¹ and R² is hydrogen or an aliphatic acyl group, each of R³ and R⁴ is hydrogen or a protecting group, X is an amino acid sequence consisting of 1 to 10 amino acid residues which may be protected, Y is an amino acid sequence consisting of 1 to 5 amino acids residues which may be protected, bounding at a terminal carboxyl group, or a salt thereof has an activity of remarkably improving hematopoietic disorder and is useful as an immuno-stimulating agent or an agent for treating thrombocytopenia.

    摘要翻译： 下式化合物：其中R 1和R 2各自为氢或脂族酰基，R 3和R 4各自为氢或保护基，X为 由1〜10个可被保护的氨基酸残基组成的氨基酸序列，Y是由可被保护的1〜5个氨基酸残基组成的氨基酸序列，其末端羧基被界定，或其盐具有活性 显着改善造血障碍，可用作免疫刺激剂或治疗血小板减少症的药剂。