Octacyclodepsipeptides having an endoparasiticidal action
    95.
    发明授权
    Octacyclodepsipeptides having an endoparasiticidal action 失效
    具有内寄生性杀伤作用的Octacyclodepsipeptide

    公开(公告)号:US5717063A

    公开(公告)日:1998-02-10

    申请号:US456148

    申请日:1995-05-31

    CPC classification number: C07D273/00 C07K11/02 A61K38/00

    Abstract: The present invention relates to compounds of the general formula (I) ##STR1## in which R.sup.1 and R.sup.12 represent the same or different radicals selected from the group of C.sub.2-9 -alkyl, C.sub.1-8 -halogeno-alkyl, C.sub.3-6 -cycloalkyl, aralkyl or aryl, R.sup.3 to R.sup.10 represent the same or different radicals selected from the group of hydrogen, C.sub.1-5 -alkyl which may optionally be substituted by hydroxyl, alkoxy, carboxyl, carboxamide, imidazolyl, indolyl, guanidino, thio- or thioalkyl, and represent aryl, alkylaryl or heteroarylmethyl which are optionally substituted by halogen, hydroxyl, alkyl, alkoxy, nitro or a --NR.sup.13 R.sup.14 group in which R.sup.13 or R.sup.14 independently from each other represent hydrogen or alkyl or together with the adjoining nitrogen atom form a 5, 6 or 7-membered ring which is optionally interrupted by O, S or N and which is optionally substituted by C.sub.1-4 -alkyl, R.sup.2 and R.sup.11 represent the same of different radicals selected from the group of C.sub.1-4 -alkyl, and stereoisomers thereof, to processes for their preparation and to their use as endoparasiticides.

    Abstract translation: 本发明涉及通式(I)的化合物,其中R 1和R 12表示相同或不同的选自C 2-9 - 烷基,C 1-8 - 卤代烷基,C 3 - -6-环烷基,芳烷基或芳基,R 3至R 10表示相同或不同的选自氢,可任选被羟基,烷氧基,羧基,羧酰胺,咪唑基,吲哚基,胍基, 硫代或硫代烷基,并且表示任选被卤素,羟基,烷基,烷氧基,硝基或-NR 13 R 14基团取代的芳基,烷基芳基或杂芳基甲基,其中R 13或R 14彼此独立地表示氢或烷基或与相邻的氮 原子形成5,6或7-元环,其任选地被O,S或N中断,并且其任选被C 1-4 - 烷基取代,R 2和R 11表示与选自C 1-4的不同基团相同的基团 - 烷基和它们的立体异构体 继承人的准备和用作内寄生虫病药物。

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