TAN-1511, its derivatives, production and use thereof
    1.
    发明授权
    TAN-1511, its derivatives, production and use thereof 失效
    TAN-1511,其衍生物,生产和使用

    公开(公告)号:US5478809A

    公开(公告)日:1995-12-26

    申请号:US174365

    申请日:1993-12-28

    摘要: A compound of the formula: ##STR1## wherein each R.sup.1, R.sup.2 and R.sup.3 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: 下式的化合物:其中每个R 1,R 2和R 3是脂族酰基,X是由1至5个氨基酸残基组成的氨基酸序列,其含有至少一个酸性氨基酸残基,n是整数 为0〜4,条件是当n为0时,X在其N-末端具有谷氨酰 - 甘氨酰,当n为1或2时,酸性氨基酸残基为除D-谷氨酰以外的酸性氨基酸残基或盐 其具有显着改善造血作用的活性,并且可用作具有白细胞增加活性的免疫刺激剂。

    Xanthene derivatives, their production and use
    4.
    发明授权
    Xanthene derivatives, their production and use 失效
    呫吨衍生物,其生产和使用

    公开(公告)号:US06221637B1

    公开(公告)日:2001-04-24

    申请号:US08812946

    申请日:1997-03-04

    IPC分类号: C12P1702

    摘要: Xanthene compounds represented by the formula: wherein R1 is a carboxyl group which may be esterified or amidated; R2 is a hydrogen atom, a hydroxyl group, or a hydrocarbon group which may be substituted; R3 and R4 are the same or different and are a hydroxyl group which may be substituted; R5 and R6 are a hydrogen atom or a halogen atom; R7 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, R2 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: 由下式表示的呫吨化合物:其中R1是可被酯化或酰胺化的羧基; R2是氢原子,羟基或可被取代的烃基; R3和R4相同或不同,为可被取代的羟基; R5和R6是氢原子或卤素原子; R7是氢原子,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,R2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依赖性的活化 T细胞,抑制T细胞的IL-2产生,作为免疫调节剂,例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,糖尿病等的药物组合物。

    Physiologically active substance TAN-931, its derivatives, their
production and use
    6.
    发明授权
    Physiologically active substance TAN-931, its derivatives, their production and use 失效
    生理活性物质TAN-931,其衍生物,其生产和使用

    公开(公告)号:US5196564A

    公开(公告)日:1993-03-23

    申请号:US661115

    申请日:1991-02-27

    摘要: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is esterified carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or alkyl; A is formyl, 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 R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.

    摘要翻译: 式(I)的新化合物:其中R1是酯化羧基; R2,R3和R4相同或不同,为氢或烷基; A是甲酰基,羟基亚氨基甲基或羧基; 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,以及可产生青霉素的青霉菌 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)。