Cyclosporin peptolides having an .alpha.-hydroxycarboxylic acid at position 8
AssigneeSandoz Ltd.
InventorsMichael M. Dreyfuss, Max H. Schreier, Hans Tscherter
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Abstract
Cyclic peptolides having the structure of a cyclosporin in which one amide linkage is replaced by an ester linkage are obtained by fermentation of fungal strains of the genus Cylindrotrichum Bonorden, or by cyclization of a hydroxy-undecapeptide. The cyclic peptolides have immunosuppressive, anti-inflammatory and anti-parasitic properties.
Claims9
A cyclosporin of formula II ##STR13## in which W is MeBmt, 8'-OHMeBmt, or MeBmtH.sub.2,
- X is Sar or Gly,
- Y is MeLeu or Leu,
- Z is Leu, Ile or Val, and
- A is a group of formula III ##STR14## in which R is C.sub.1-4 alkyl.
(Thr).sup.2 (Leu).sup.5 (D-Hiv).sup.8 (Leu).sup.10 -Ciclosporin.
(Thr).sup.2 (D-Hiv).sup.8 (Leu).sup.10 -Ciclosporin.
(Thr).sup.2 (Ile).sup.5 (D-Hiv).sup.8 (Leu).sup.10 -Ciclosporin.
(Thr).sup.2 (Leu).sup.4 (Leu).sup.5 (D-Hiv).sup.8 (Leu).sup.10 -Ciclosporin.
(Thr).sup.2 (Gly).sup.3 (Leu).sup.5 (D-Hiv).sup.8 (Leu).sup.10 -Ciclosporin.
(8'-OH MeBmt).sup.1 (Thr).sup.2 (Leu).sup.5 (D-Hiv).sup.8 (Leu).sup.10 -Ciclosporin.
Dependencies are inferred from the claim text.