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    • 41. 发明授权
    • Octacyclodepsipeptides having an endoparasiticidal action
    • 具有内寄生性杀伤作用的Octacyclodepsipeptide
    • US06369028B1
    • 2002-04-09
    • US08246029
    • 1994-05-19
    • Jürgen ScherkenbeckPeter JeschkeHans-Georg LerchenHermann HagemannAchim HarderNorbert MenckeAndrew Plant
    • Jürgen ScherkenbeckPeter JeschkeHans-Georg LerchenHermann HagemannAchim HarderNorbert MenckeAndrew Plant
    • A61K3800
    • C07D273/00C07C235/12C07C235/34
    • The present invention relates to compounds of the general formula (I) in which R1, R2, R11 and R12 represent the same or different radicals selected from the group of C1-8-alkyl, C1-8-halogenoalkyl, C3-6-cycloalkyl, aralkyl or aryl, R3, R5, R7, R9, represent the same or different radicals selected from the group of hydrogen or straight-chain C1-5-alkyl or branched C4-7-alkyl which may optionally be substituted by hydroxyl, C1-4-alkoxy, carboxyl  carboxamide,  imidazolyl, indolyl, guanidino, —SH or C1-4-alkylthio, and furthermore represents aryl, aralkyl or heteroarylmethyl which may be substituted by halogen, hydroxyl, C1-4-alkyl, C1-4-alkoxy, nitro or a —NR13R14 group in which R13 and R14 independently from each other represent hydrogen or alkyl or together with the adjoining nitrogen atom forms a 5, 6 or 7-membered ring which is optionally interrupted by O, S or N and which is optionally C1-4-alkyl substituted, R4, R6, R8, R10 represent the same or different radicals selected from the group of hydrogen, straight-chain C1-5-alkyl and represents isopropyl, sec.-butyl, t-butyl, C2-6-alkenyl, C3-7-cycloalkyl, which may optionally be substituted by hydroxyl, C1-4-alkoxy, carboxyl, carboxamide, imidazolyl, indolyl, guanidino, SH or C1-4-alkylthio and represent aryl, aralkyl or heteroarylmethyl which may be substituted by halogen, hydroxyl, C1-4-alkyl, C1-4-alkoxy, and stereoisomers thereof, to processes for their preparation and to their use as endoparasiticides.
    • 本发明涉及通式(I)的化合物,其中R 1,R 2,R 11和R 12表示相同或不同的选自C 1-8 - 烷基,C 1-8 - 卤代烷基,C 3-6 - 环烷基, 芳烷基或芳基,R 3,R 5,R 7,R 9表示相同或不同的选自氢或直链C 1-5烷基或支链C 4-7 - 烷基的基团,其可任选被羟基,C 1-4 烷氧基,羧基羧酰胺,咪唑基,吲哚基,胍基,-SH或C 1-4 - 烷硫基,此外表示可被卤素,羟基,C 1-4 - 烷基,C 1-4 - 烷氧基,硝基取代的芳基,芳烷基或杂芳基甲基 或-NR 13 R 14基团,其中R 13和R 14彼此独立地表示氢或烷基或与相邻的氮原子一起形成可选地被O,S或N中断的5,6或7-元环,并且其任选地为C1 R 4,R 6,R 8,R 10表示选自该基团的相同或不同的基团 的氢,直链C1-5 - 烷基,代表异丙基,仲丁基,叔丁基,C 2-6 - 烯基,C 3-7 - 环烷基,其可任选被羟基,C 1-4 - 烷氧基, 羧基,羧酰胺,咪唑基,吲哚基,胍基,SH或C 1-4 - 烷硫基,代表可被卤素,羟基,C 1-4 - 烷基,C 1-4 - 烷氧基及其立体异构体取代的芳基,芳烷基或杂芳基甲基, 其制备方法及其作为内寄生物杀虫剂的用途。
    • 44. 发明授权
    • Octacyclodepsipeptides having an endoparasiticidal action
    • 具有内寄生性杀伤作用的Octacyclodepsipeptide
    • US06468966B1
    • 2002-10-22
    • US08246022
    • 1994-05-19
    • Jürgen ScherkenbeckPeter JeschkeHans-Georg LerchenHermann HagemannAchim HarderNorbert MenckeAndrew Plant
    • Jürgen ScherkenbeckPeter JeschkeHans-Georg LerchenHermann HagemannAchim HarderNorbert MenckeAndrew Plant
    • A61K3800
    • C07D273/00A61K38/00C07K11/02
    • The present invention relates to compounds of the general formula (I) in which R1 and R12 represent the same or different radicals selected from the group of C2-9-alkyl, C1-8-halogen-alkyl, C3-6-cycloalkyl, aralkyl or aryl, R3 to R10 represent the same or different radicals selected from the group of hydrogen, C1-5-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 —NR13R14 group in which R13 or R14 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 C1-4-alkyl, R2 and R11 represent the same of different radicals selected from the group of C1-4-alkyl, and stereoisomers thereof, to processes for their preparation and to their use as endoparasiticides.
    • 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 - 卤素 - 烷基,C 3-6 - 环烷基,芳烷基或 芳基,R 3至R 10表示选自氢,可任选被羟基,烷氧基,羧基,羧酰胺,咪唑基,吲哚基,胍基,硫代或硫代烷基取代的C 1-5 - 烷基的相同或不同的基团,并且表示 芳基,烷基芳基或杂芳基甲基,其任选被卤素,羟基,烷基,烷氧基,硝基或-NR 13 R 14基团取代,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一起形成5,6或 任选地被O,S或N中断并且任选被C 1-4 - 烷基取代的R 7和R 11代表与选自C 1-4 - 烷基及其立体异构体的不同基团相同的7-元环, 进行准备a 并将其用作内寄生物杀虫剂。