Cephaibols: novel antiparasitics from Acremonium tubakii process for their production, and use thereof

US6582949B1 · kind B1 · utility

Assignee

• Aventis Pharma Deutschland GmbH · DE

Inventors

• Laszlo Vertesy · Eppstein, DE
• Michael Kurz · Neustadt, DE
• Matthias Schiell · Brechen, DE
• Joachim Hofmann · Bad Camberg, DE

Key dates

• Filing date: May 3, 2000
• Grant date: Jun 24, 2003
• Expiry date: May 3, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to compounds of the formula IAcPhe-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; ore) w is Gly; x and y are Aib and z is Iva;or of the formula IIAcPhe-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.