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    • 4. 发明授权
    • Cephaibols: novel antiparasitics from Acremonium tubakii, process for their production, and use thereof
    • 头孢唑醇:来自Acremonium tubakii的新型抗寄生虫药,其生产方法及其用途
    • US07067112B2
    • 2006-06-27
    • US10411144
    • 2003-04-11
    • Laszlo VertesyMichael KurzMatthias SchiellJoachim Hofmann
    • Laszlo VertesyMichael KurzMatthias SchiellJoachim Hofmann
    • A61K49/00A61K38/10C07K7/08
    • C07K7/08A61K38/00
    • 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 Iva; 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-lle-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.
    • 本发明涉及式I化合物<?in-line-formula description =“In-line Formulas”end =“lead”→AcPhe-Aib-Aib-Aib-xw-Leu-y-Aib-Hyp-Gln -z-Hyp-Aib-Pro-R(I)<?in-line-formula description =“In-line Formulas”end =“tail”?>其中R是Phe-ol或Phe-al,w,x ,y和z具有以下含义:a)w是Gly或Ala; x是Aib,y和z是Iva; b)w是Gly; x,y和z是Iva; c)w是Gly; x和z是Aib,y是Iva; d)w是Gly; x,y和z是Aib; 或e)w是Gly; x和y是Aib,z是Iva; AcPhe-Iva-Gln-Aib-Lle-Thr-Aib-Leu-Aib-x-Gln-Aib,或者式II <?in-line-formula description =“In-line Formulas”end =“lead” -Hyp-Aib-Pro-Phe-Ser,(II)<?在线公式描述=“在线公式”end =“tail”?>其中x是Hyp或Pro,它们是由Acremonium tubakii FH 1685 DSM 12774在发酵过程中释放到培养基中,从培养基中分离头孢胆素的方法及其纯化,以及将头孢唑醇用作药物活性化合物,特别是用于控制寄生虫的方法。