MEDICINAL COMPOSITIONS FOR PREVENTING OR TREATING DIARRHEA
    22.
    发明公开
    MEDICINAL COMPOSITIONS FOR PREVENTING OR TREATING DIARRHEA 审中-公开
    医疗中心ZUSAMMENSETZUNGEN ZUR PREVENTION ODER BEHANDLUNG DERDIARRHÖ

    公开(公告)号:EP1197214A1

    公开(公告)日:2002-04-17

    申请号:EP00942374.0

    申请日:2000-06-28

    IPC分类号: A61K31/7012 A61P1/12

    摘要: Provided is a pharmaceutical composition for the prevention or treatment of a diarrhea, which comprises as an active ingredient, siastatin B or a siastatin B derivative having a β-glucuronidase inhibitory activity. Siastatin B or the siastatin B derivative is useful as a drug for the prevention or treatment of a diarrhea, which is capable of ameliorating the diarrhea disorders as induced as a side effect when a cancer-bearing patient received the administration of an anticancer chemotherapeutic agent, particularly an anticancer camptothecin derivative acting as a topoisomerase I inhibitor. This composition is effective to prevent or treat such diarrhea as induced by the administration of an anticancer camptothecin derivative to the cancer-bearing patient.

    摘要翻译: 提供了用于预防或治疗腹泻的药物组合物,其包含作为活性成分的具有β-葡糖醛酸糖苷酶抑制活性的西司特汀B或西司他丁B衍生物。 西塔他汀B或西沙星汀B衍生物可用作预防或治疗腹泻的药物,当患有癌症的患者接受抗癌化学治疗剂的施用时,其能够改善作为副作用诱导的腹泻病症, 特别是作为拓扑异构酶I抑制剂的抗癌喜树碱衍生物。 该组合物有效地预防或治疗由向抗癌患者施用抗癌喜树碱衍生物诱导的这种腹泻。

    SIASTATIN B DERIVATIVES HAVING GLYCOSIDASE INHIBITORY ACTIVITIES AND PROCESS FOR PRODUCING THE SAME
    23.
    发明公开
    SIASTATIN B DERIVATIVES HAVING GLYCOSIDASE INHIBITORY ACTIVITIES AND PROCESS FOR PRODUCING THE SAME 有权
    精氨酸衍生物麻醉剂甘氨酸酶INHINBOR-AKTIVITÄTUND EIN VERFAHREN ZUR HERSTELLUNG DERSELBEN

    公开(公告)号:EP1142900A1

    公开(公告)日:2001-10-10

    申请号:EP99961360.7

    申请日:1999-12-24

    CPC分类号: C07H13/04 C07H7/02

    摘要: A compound of the formula (I):
    and a compound of the formula (V):
    as well as a compound of the formula (X):
    which are each a novel siastatin B derivative having a potent inhibitory activity against a glycosidase, are now synthesized by new processes.
    The compound of the formula (I), the compound of the formula (V) and the compound of the formula (X) have a potent enzyme-inhibitory activity to a glycosidase, which is particularly N -acetyl-galactosaminidase, galactosidase, glucosidase and mannosidase.

    摘要翻译: 式(I)的化合物:和式(V)的化合物:以及式(X)的化合物:,它们各自是新的硫酸沙司他滨B衍​​生物,其具有 现在通过新方法合成对糖苷酶的有效抑制活性。 式(I)化合物,式(V)化合物和式(X)化合物对糖苷酶具有有效的酶抑制活性,其特别是N-乙酰基 - 半乳糖苷酶,半乳糖苷酶,葡糖苷酶和 甘露糖苷酶。

    PROCESS FOR PRODUCING D-(CHIRO)-INOSITOL
    24.
    发明授权
    PROCESS FOR PRODUCING D-(CHIRO)-INOSITOL 失效
    VERFAHREN ZUR HERSTELLUNG VON D-CHIRO INOSITOL

    公开(公告)号:EP0712827B1

    公开(公告)日:1999-02-17

    申请号:EP94923085.8

    申请日:1994-08-08

    IPC分类号: C07C35/16 C07C29/10

    摘要: A process for producing D-chiro-inositol which comprises either mixing an aqueous solution of kasugamycin or a salt thereof with a strongly acidic ion-exchange resin (of H type) in a reactor or bringing the aqueous solution into contact with the resin in a column packed therewith, heating the aqueous solution and the resin under normal or applied pressure to effect hydrolysis of kasugamycin to thereby prepare an acidic reaction solution containing D-chiro-inositol, separating the acidic reaction solution from the resin, and recovering D-chiro-inositol from the solution. In this stage, it is possible to obtain efficiently high-purity D-chiro-inositol by passing the acidic reaction solution first through a column packed with a strongly acidic ion-exchange resin (of H type) and then through another column packed with a strongly basic ion-exchange resin (of OH type) to prepare a neutral eluate containing D-chiro-inositol, and concentrating the eluate to effect deposition of D-chiro-inositol crystals.

    摘要翻译: 一种生产D-手性肌醇的方法,其包括在反应器中混合春日霉素或其盐与强酸性离子交换树脂(H +型)的水溶液或使水溶液与 树脂在正常或施加压力下加热水溶液和树脂以实现春雷霉素的水解,从而制备含有D-手性肌醇的酸性反应溶液,将酸性反应溶液与树脂分离,并回收D - 双 - 肌醇溶液。 在这个阶段,通过使酸性反应溶液首先通过填充有强酸性离子交换树脂(H +型)的柱然后通过另一个柱子,可以有效地获得高纯度D-手性肌醇 填充强碱性离子交换树脂(OH - 型)以制备含有D-手性肌醇的中性洗脱液,并浓缩洗脱液以实现D-手性肌醇晶体的沉积。

    3,4'-DIDEOXYMYCAMINOSYLTYLONOLIDE DERIVATIVE AND PRODUCTION THEREOF
    25.
    发明公开
    3,4'-DIDEOXYMYCAMINOSYLTYLONOLIDE DERIVATIVE AND PRODUCTION THEREOF 失效
    3,4'-二脱氧氨基甲酰基烟酰胺衍生物及其生产

    公开(公告)号:EP0627443A1

    公开(公告)日:1994-12-07

    申请号:EP93901539.2

    申请日:1993-01-12

    IPC分类号: C07H17/08

    CPC分类号: C07H17/08

    摘要: A compound represented by general formula (1) which is useful for producing 3,4'-dideoxymycaminosyltylonolide useful as an antibacterial substance. In the said formula, A represents optionally protected carbonyl; B represents optionally protected formyl; R¹ represents optionally protected hydroxy; R² represents hydrogen or acyl; W represents hydrogen, hydroxy, lower alkanoyloxy or substituted sulfonyloxy; Y represents hydrogen, halogen, hydroxy or substituted sulfonyloxy; and symbol --- represents either a double or a single bond.

    摘要翻译: 由通式(1)表示的化合物,其可用于制备可用作抗菌物质的3,4'-二脱氧碳霉糖基太乐内酯。 在所述式中,A表示任选被保护的羰基; B代表任选保护的甲酰基; R 1代表任选保护的羟基; R 2代表氢或酰基; W代表氢,羟基,低级烷酰氧基或取代的磺酰氧基; Y代表氢,卤素,羟基或取代的磺酰氧基; 符号---代表双键或单键。

    4-O-(AMINOGLYCOSYL)- OR 4,6-DI-O-(AMINOGLYCOSYL)-2,5-DIDEOXY-5,5-DIFLUOROSTREPTAMINE DERIVATIVE AND PRODUCTION THEREOF
    26.
    发明公开
    4-O-(AMINOGLYCOSYL)- OR 4,6-DI-O-(AMINOGLYCOSYL)-2,5-DIDEOXY-5,5-DIFLUOROSTREPTAMINE DERIVATIVE AND PRODUCTION THEREOF 失效
    4-(氨基甲酰基)-ODER 4,6-DI-O-(氨基甲酰基)-2,5-二脱氧-5,5-二脱氧嘧啶脱乙酰壳多糖在SEINE HERSTELLUNG。

    公开(公告)号:EP0546179A1

    公开(公告)日:1993-06-16

    申请号:EP91914768.6

    申请日:1991-08-22

    摘要: The invention provides 5-deoxy-5,5-difluoro derivatives of aminoglycoside antibiotics of neamine, kanamycin A, kanamycin B, gentamicin and seldomycin, each synthesized as a novel compound, and also 1-N-(a-hydroxy- m-aminoalkanoyl) derivatives synthesized from the newly obtained 5-deoxy-5,5-difluorokanamycins A and B and analogs thereof. The 5-deoxy-5,5-difluoro derivatives thus obtained have antibacterial activities superior or substantially equivalent to those of the amino-glycoside antibiotics from which they are derived and further have a remarkably improved median lethal dose (LD so ) when intravenously administered to mice and a remarkably reduced toxicity on mammals.

    摘要翻译: 本发明提供了作为新化合物合成的神经胺,卡那霉素A,卡那霉素B,庆大霉素和青少霉素的氨基糖苷类抗生素的5-脱氧-5,5-二氟衍生物,还提供了1-N-(α-羟基-ω-氨基烷酰基 )衍生物,其新合成的5-脱氧-5,5-二氟吗啉霉素A和B及其类似物合成。 由此获得的5-脱氧-5,5-二氟衍生物具有优于或基本上等同于其衍生的氨基 - 糖苷抗生素的抗菌活性,并且当向小鼠静脉内施用时还具有显着改善的中位数致死量(LD 50) 并且对哺乳动物的毒性显着降低。