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    • 71. 发明申请
    • 18-Membered Nitrobenzyl- and Aminobenzyl-Substituted Cyclohexadepsipeptides for Controlling Endoparasites and a Process for Their Preparation
    • 用于控制内寄生虫的18位硝基苄基 - 和氨基苄基取代的环己二肽及其制备方法
    • US20080026990A1
    • 2008-01-31
    • US10582555
    • 2004-12-07
    • Peter JeschkeAchim Harder
    • Peter JeschkeAchim Harder
    • A61K38/12A61P33/00C07K7/56
    • C07K11/02A61K38/00C07D273/00
    • The invention relates to cyclic depsipeptides, especially 18-membered cyclohexadepsipeptides of general formula (I) and the salts thereof, wherein R1 represents nitrobenzyl or R′R″N-benzyl—wherein R′ and R″ independently represent hydrogen, optionally substituted C1-C4-alkyl, formyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxycarbonyl, or hydroxy-C1-C2-alkyl-sulfonyl-C1-C2-alkyl, or, together with the nitrogen atom to which they are bound, R′ and R″ form an optionally substituted monocyclic or polycyclic, optionally bridged and/or spirocyclic, saturated or unsaturated heterocycle containing between one and three other heteroatoms from the group of nitrogen, oxygen and sulphur, or R′ and R″ together form C3-C5-alkylene monocarbonyl or an optionally susbtituted diacyl radical of a C4-C6-dicarboxylic acid—and R2, R3 and R4 independently represent C1-C4-alkyl. The invention also relates to the optical isomers and racemates of said cyclic depsipeptides, to a method for the production thereof, and to the use of the same for controlling endoparasites.
    • 本发明涉及环状缩肽,特别是通式(I)的18元环己缩肽和其盐,其中R 1表示硝基苄基或R'R''N-苄基,其中R'和R “独立地表示氢,任选取代的C 1 -C 4 - 烷基,甲酰基,C 1 -C 4 - 烷氧基-C 1 -C 4 - 亚烷基,C 1 -C 4 - 烷氧基羰基或羟基(C 1 -C 4) -C 1 -C 2 - 烷基 - 磺酰基-C 1 -C 2 - 烷基,或一起 与其结合的氮原子一起形成任选取代的单环或多环,任选桥连和/或螺环,饱和或不饱和的杂环,其含有一个和三个其它杂原子,来自氮,氧和 硫或R'和R“一起形成C 3 -C 5 - 亚烷基一羰基或任选被取代的C 4 - 亚烷基二酰基, -C 6 - 二羧酸 - 且R 2,R 3和R 4独立地表示C 1 -C 4 烷基。 本发明还涉及所述环状缩酚酸酯的光学异构体和外消旋体,其制备方法及其用于控制​​内寄生虫的用途。
    • 79. 发明授权
    • Use of substituted 1,2,4-oxadiazole derivatives for combating
endoparasites, new substituted 1,2,4-oxadiazole derivatives, and
processes for their preparation
    • 使用取代的1,2,4-恶二唑衍生物对抗内寄生虫,新的取代的1,2,4-恶二唑衍生物及其制备方法
    • US5428047A
    • 1995-06-27
    • US124909
    • 1993-09-21
    • Peter JeschkeWerner LindnerAchim HarderNorbert Mencke
    • Peter JeschkeWerner LindnerAchim HarderNorbert Mencke
    • A01N43/82A01N43/836A61K31/41A61K31/4245A61P33/00A61P33/10C07D271/06C07D413/06
    • C07D271/06A01N43/82A61K31/41
    • The present invention relates to the use of substituted 1,2,4-oxadiazole derivatives of the general formula I ##STR1## in which R.sup.1 represents hydrogen, alkyl which is optionally substituted by halogen, alkoxy, hydroxyl, amino, alkylamino, dialkylamino, cycloalkylamino as well as cycloalkyl, optionally substituted aryl or hetaryl,R.sup.2 represents hydrogen and alkyl,X represents O, S, SO, SO.sub.2 and N-R.sup.3,R.sup.3 represents hydrogen, alkyl, alkylcarbonyl or halogenoalkylcarbonylR.sup.4 represents identical or different radicals from the series comprising hydrogen, halogen, cyano, nitro, isothiocyanato, amino, aminoacyl, alkylamino, dialkylamino, trialkylammonium halide, sulphonylamino, hydroxyl, mercapto, alkyl, aralkyl, halogenoalkyl, alkoxy, aralkoxy, halogenoalkoxy, aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl, alkylthio, halogenoalkylthio, alkylsulphinyl, halogenoalkylsulphinyl, alkylsulphonyl, halogenoalkylsulphonyl, alkoxycarbonyl, alkylcarbonyl, alkylcarbonyloxy, alkoxyalkyl, alkoxyalkoxy, hydroxyalkoxy, hetarylmethyleneoxy,for combating endoparasites in medicine and veterinary medicine, and new compounds of the formula (I) and their preparation.
    • 本发明涉及通式Ⅰ的取代的1,2,4-恶二唑衍生物(Ⅰ),其中R1代表氢,任选被卤素,烷氧基,羟基,氨基,烷基氨基, 二烷基氨基,环烷基氨基以及环烷基,任选取代的芳基或杂芳基,R 2表示氢和烷基,X表示O,S,SO,SO 2和N-R 3,R 3表示氢,烷基,烷基羰基或卤代烷基羰基R 4表示相同或不同的基团, 氨基,氨基酰基,烷基氨基,二烷基氨基,三烷基卤化铵,磺酰基氨基,羟基,巯基,烷基,芳烷基,卤代烷基,烷氧基,芳烷氧基,卤代烷氧基,芳基,芳氧基,芳硫基,芳基亚磺酰基, 芳基磺酰基,烷硫基,卤代烷硫基,烷基亚磺酰基,卤代烷基亚磺酰基,烷基磺酰基,卤代烷基磺酰基,烷氧基羰基,烷基羰基,烷基羰基氧基,烷氧基烷基,烷氧基 烷氧基,羟基烷氧基,杂芳基亚甲氧基,用于对抗医药和兽药中的内寄生虫,以及式(I)的新化合物及其制备。