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    Sordarin derivatives
    5.
    发明授权
    Sordarin derivatives 失效
    Sordarin衍生物

    公开(公告)号：US6136853A

    公开(公告)日：2000-10-24

    申请号：US284123

    申请日：1999-03-06

    申请人： James M. Balkovec ,  Bruno Tse

    发明人： James M. Balkovec ,  Bruno Tse

    IPC分类号： A01N45/00 ,  A01N63/04 ,  C07H15/20 ,  A01N37/34

    CPC分类号： C07H15/20 ,  A01N45/00 ,  A01N63/04

    摘要： PURPOSE: To produce a novel antibiotic substance zofimarin having antimicrobial activity against fungi and obtain an antimicrobial agent containing the antibiotic substance zofimarin as an active constituent, by cultivating a microorganism, belonging to the genus Zopfiella and capable of producing the zofimarin.CONSTITUTION: An ascomycete belonging to the genus Zopfiella, e.g. Zopfiella marina; is cultivated. The cultivation is carried out according to general fungi, but artifical seawater is used in place of tap water in a liquid culture medium. A carbon source, nitrogen source, inorganic salt, etc., are added, and a defoaming agent is suitably used to carry out the cultivation at 20-30.degree. C. by the spinner culture method with aeration. After completing the cultivation, microbial cells are removed, and the resultant product in the supernatant liquid or filtrate is extracted and purified to afford the aimed zofimarin. The above-mentioned antibiotic substance is neutral colorless oily substance exhibiting the following properties; Soluble in methanol, ethanol and acetone and slightly soluble in water. Positive to the color reaction with iodine and sulfuric acid, etc., and expressed by the formula.

    摘要翻译： PCT No.PCT / US97 / 18047 Sec。 371日期1999年3月6日 102（e）1999年3月6日PCT PCT 1997年10月3日PCT公布。 公开号WO98 / 15178 日期：1998年04月16日目的：生产具有抗真菌抗微生物活性的新型抗生素唑夫胺，通过培养属于佐布氏菌属的Zopfiella属的微生物，得到含有抗生素唑菲林作为活性成分的抗微生物剂， 。 构成：属于Zopfiella属的子囊菌纲，例如 Zopfiella码头 耕种 根据一般真菌进行培养，但在液体培养基中使用人造海水代替自来水。 添加碳源，氮源，无机盐等，适当地使用消泡剂，通过旋风培养法在20-30℃进行培养。 完成培养后，除去微生物细胞，提取和纯化上清液或滤液中的所得产物，得到目标唑非那嗪。 上述抗生素是中性无色油状物质，具有以下特性; 溶于甲醇，乙醇和丙酮，微溶于水。 与碘和硫酸等颜色反应呈正相，并用式表示。

    Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders
    10.
    发明授权
    Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders 失效
    用于治疗癌症，代谢疾病和皮肤病症的治疗剂

    公开(公告)号：US07572816B2

    公开(公告)日：2009-08-11

    申请号：US10514383

    申请日：2004-07-21

    申请人： Bruno Tse ,  Sepehr Sarshar

    发明人： Bruno Tse ,  Sepehr Sarshar

    IPC分类号： A61K31/47 ,  A61K31/425 ,  A61K31/415 ,  C07D295/00 ,  C07D207/00 ,  C07D401/00 ,  C07D233/00 ,  C07D277/00 ,  C07D409/00 ,  C07D403/00 ,  C07D239/02 ,  C07D215/02 ,  C07D271/00 ,  C07D285/02 ,  C07D257/04 ,  C07D487/00

    CPC分类号： C07D233/72 ,  C07D277/34

    摘要： The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals

    摘要翻译： 本发明涉及具有其中R 1，R 2，R 3，R 4，R 5和m如本文所定义的结构的化合物。 本发明的化合物是用于治疗哺乳动物受试者的癌症，代谢疾病和皮肤病症的新型治疗剂。 这些化合物也是基因表达的有用调节剂。 它们通过干扰某些细胞信号转导级联发挥其活性。 因此，本发明的化合物也可用于调节由各种激素或细胞因子控制或调节的细胞分化和细胞周期过程。 特别地，本发明涉及诱导癌细胞凋亡的化合物，因此可用于治疗或预防癌症，包括晚期癌症和癌前细胞。 本发明还公开了哺乳动物疾病的药物组合物和治疗方法