- ENDOPARASITIC DEPSIPEPTIDES
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The present invention provides cyclic depsipeptides of Formula (1), stereoisomers thereof, and veterinary acceptable salts thereof (1) wherein each of R1, R2, R3, R4, L1, and L2, are as defined herein. The present invention also contemplates compositions and methods of treatment as an endoparasiticide with a Formula (1) compound.
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- ENDOPARASITIC DEPSIPEPTIDES
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The present invention provides cyclic depsipeptides of Formula (1), stereoisomers thereof, and veterinary acceptable salts thereof wherein each of R1, R2, R3, R4, L1, and L2 are as defined herein. The present invention also contemplates compositions, methods of treatment, and uses as a medicament to treat an animal for an endoparasitic infection with a Formula (1 ) compound.
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- METHOD FOR THE SYNTHESIS OF CYCLIC DEPSIPEPTIDES
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The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, from the open form.
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Page/Page column 59
(2019/05/30)
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- ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS
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The present invention provides cyclic depsipeptide compounds of formula (I) wherein the stereochemical configuration of at least one carbon atom bearing the groups Cy1, Cy2, R1, R2, R3, R4, Ra and Rb is inverted compared with the naturally occurring cyclic depsipeptide PF1022A. The invention also provides compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.
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Page/Page column 279
(2018/06/06)
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- ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS
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The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals, including humans. The compounds and compositions may be used for combating parasites in or on animals including mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in animals, including birds and mammals.
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Page/Page column 331
(2017/07/14)
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- ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS
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The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.
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Page/Page column 258; 259
(2016/12/07)
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- Segment solid-phase total synthesis of the anthelmintic cyclooctadepsipeptides PF1022A and emodepside
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Cyclodepsipeptides of the enniation, PF1022 and verticilide families represent a diverse class of highly interesting natural products with respect to their manifold biological activities. However, until now, no practicable solid-phase syntheses of these compounds have been accomplished, probably due to the problematic combination of N-methyl amino acids and hydroxycarboxylic acids. We report herein an efficient synthesis of the anthelmintic PF1022A and its commercial analogue emodepside on Kaiser and Wang resins. Our protocol provides the basis for the solid-phase synthesis of cyclodepsipeptide libraries with a high probability of anthelmintic, antibacterial or insecticidal activity.
- Scherkenbeck, Juergen,Luettenberg, Sebastian,Ludwig, Monika,Bruecher, Karin,Kotthaus, Andreas
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experimental part
p. 1546 - 1553
(2012/04/23)
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