- 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 208
(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 302
(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 189; 190
(2016/12/07)
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- BENZIIMIDAZOLE AND IMIDAZOPYRIDINE DERIVATIVES AS SODIUM CHANNEL MODULATORS
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The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Nav1.8 modulators of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7. X and Y are as defined in the description. Nav1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.
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Page/Page column 159; 160
(2013/08/15)
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- VERSATILE AND STEREOSPECIFIC SYNTHESIS OF GAMMA,DELTA -UNSATURATED AMINO ACIDS BY WITTIG REACTION
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The present invention relates to γ,δ-unsaturated a-amino acids of general formula (I). The present invention also provides a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. The present invention also relates to intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I).
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Page/Page column 35; 36
(2013/03/28)
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- Synthesis of β-(S-methyl)thioaspartic acid and derivatives
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β-(S-Methyl)thioaspartic acid occurs as a posttranslational modification at position 88 in Escherichia coli ribosomal protein S12, a position that is a mutational hotspot resulting in both antibiotic-resistant and antibiotic-sensitive phenotypes. Critical
- Heredia-Moya, Jorge,Kirk, Kenneth L.
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p. 5908 - 5913
(2008/12/21)
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- Bodipy-VAD-Fmk, a useful tool to study yeast peptide N-glycanase activity
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In this paper the development of a fluorescent activity based probe, Bodipy-VAD-Fmk, for visualization of yeast peptide N-glycanase is described. The activity based probe is used to assess the efficacy of known and new chitobiose-based electrophilic traps to bind yeast peptide N-glycanase. The Royal Society of Chemistry.
- Witte, Martin D.,Descals, Carlos V.,De Lavoir, Sebastiaan V. P.,Florea, Bogdan I.,Van Der Marel, Gijsbert A.,Overkleeft, Herman S.
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p. 3690 - 3697
(2008/10/09)
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- Synthesis, characterization and cytolytic activity of α-helical amphiphilic peptide nanostructures containing crown ethers
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Many natural α-helical amphiphilic peptides are known to have lytic activity toward different cells. Herein, we describe the synthesis and the characterization of synthetic α-helical amphiphilic peptide nanostructures containing crown ethers, as well as t
- Boudreault, Pierre-Luc,Voyer, Normand
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p. 1459 - 1465
(2008/02/08)
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- Structure-activity study of L-amino acid-based N-type calcium channel blockers
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Synthesis and structure-activity relationship (SAR) study of L-amino acid-based N-type calcium channel blockers are described. The compounds synthesized were evaluated for inhibitory activity against both N-type and L-type calcium channels focusing on sel
- Seko, Takuya,Kato, Masashi,Kohno, Hiroshi,Ono, Shizuka,Hashimura, Kazuya,Takimizu, Hideyuki,Nakai, Katsuhiko,Maegawa, Hitoshi,Katsube, Nobuo,Toda, Masaaki
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p. 1901 - 1913
(2007/10/03)
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- INHIBITORS OF THROMBOSIS
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This invention relates to peptide aldehyde analogs that inhibit the thrombin or Factor Xa. The compounds are thought useful for preventing or treating conditions in mammal characterized by abnormal thrombosis.
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