Aromatic di-keto derivatives, processes for their production and their use as a pharmaceutical
    3.
    发明授权
    Aromatic di-keto derivatives, processes for their production and their use as a pharmaceutical 有权
    芳香族二酮衍生物,其制备方法及其作为药物的用途

    公开(公告)号:US06380257B1

    公开(公告)日:2002-04-30

    申请号:US09694790

    申请日:2000-10-24

    IPC分类号: A61K3119

    CPC分类号: C07C65/40 C07D307/20

    摘要: The present invention relates to new aromatic di-keto derivatives and to their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents. The derivatives are glucose-6-phosphate translocase inhibitors and can be used in the treatment of diabetes mellitus. The present invention further relates to a process for the production of the derivatives, to the use of the derivatives and their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents as pharmaceuticals, in particular to their use in the treatment of diabetes mellitus, and to pharmaceutical compositions comprising the derivatives, pharmaceutically acceptable salts, esters, ethers or other chemical equivalents thereof.

    摘要翻译: 本发明涉及新的芳族二酮衍生物及其药学上可接受的盐,酯,醚和其它化学等价物。 衍生物为葡萄糖-6-磷酸转位酶抑制剂,可用于治疗糖尿病。 本发明还涉及衍生物的制备方法,衍生物及其药学上可接受的盐,酯,醚和其它化学等价物作为药物的用途,特别是其用于治疗糖尿病的方法,以及 涉及包含衍生物,药学上可接受的盐,酯,醚或其它化学等价物的药物组合物。

    Cephaibols: novel antiparasitics from Acremonium tubakii process for their production, and use thereof
    4.
    发明授权
    Cephaibols: novel antiparasitics from Acremonium tubakii process for their production, and use thereof 有权
    Cephaibols:来自Acremonium tubakii方法的新型抗寄生虫药物的生产及其用途

    公开(公告)号:US06582949B1

    公开(公告)日:2003-06-24

    申请号:US09563505

    申请日:2000-05-03

    IPC分类号: C07K708

    CPC分类号: C07K7/08 A61K38/00

    摘要: The invention relates to compounds of the formula I AcPhe-Aib-Aib-Aib-x-w-Leu-y-Aib-Hyp-Gln-z-Hyp-Aib-Pro-R  (I) in which R is Phe-ol or Phe-al and w, x, y, and z have the following meanings: a) w is Gly or Ala; x is Aib and y and z are Iva; b) w is Gly; x, y and z are va; c) w is Gly; x and z are Aib and y is Iva; d) w is Gly; x, y and z are Aib; or e) w is Gly; x and y are Aib and z is Iva; or of the formula II AcPhe-Iva-Gln-Aib-Ile-Thr-Aib-Leu-Aib-x-Gln-Aib-Hyp-Aib-Pro-Phe-Ser  (II), wherein x is Hyp or Pro, which are synthesized by Acremonium tubakii FH 1685 DSM 12774 during fermentation and released into the culture medium, a process for the isolation of the cephaibols from the culture medium, and their purification, and the use of the cephaibols as pharmacologically active compounds, in particular for the control of parasites.

    摘要翻译: 本发明涉及式Iin化合物,其中R为Phe-ol或Phe-al,w,x,y和z具有以下含义:a)w为Gly或Ala; x是Aib,y和z是Iva; b)w是Gly; x,y和z是va; c)w是Gly; x和z是Aib,y是Iva; d)w是Gly; x,y和z是Aib; 矿石)w是Gly; x和y是Aib,z是Iva;或者其中X是Hyp或Pro的式II,其在发酵过程中被Acremonium tubakii FH 1685 DSM 12774合成并释放到培养基中,从头孢曲松 培养基和它们的纯化,以及将头孢吡肟作为药理学活性化合物的用途,特别是用于控制寄生虫。