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    Avermectin derivatives
    6.
    发明授权
    Avermectin derivatives 有权
    阿维菌素衍生物

    公开(公告)号：US06605595B1

    公开(公告)日：2003-08-12

    申请号：US09890824

    申请日：2002-02-11

    申请人： Satoshi Omura ,  Toshiaki Sunazuka ,  Andreas Turberg ,  Georg von Samson-Himmelstjerna ,  Olaf Hansen ,  Achim Harder

    发明人： Satoshi Omura ,  Toshiaki Sunazuka ,  Andreas Turberg ,  Georg von Samson-Himmelstjerna ,  Olaf Hansen ,  Achim Harder

    IPC分类号： A01N4304

    CPC分类号： C07H17/08 ,  A61K31/7048

    摘要： Avermectin derivatives represented by the general formula (I) or salts thereof: wherein —X----Y— represents —CH═CH—, —CH2—C(═O)—, —CH2—CH2—, or —CH2—CH(R13)—; for example, 1) when —X----Y— represents —CH═CH—, R1 represents (R11)(R12)C [wherein R11 represents a substituted or unsubstituted lower alkyl group; a formyl group; a lower alkoxylcarbonyl group etc.; and R12 represents a hydrogen atom or a lower alkyl group]; when the bond between R2 and a carbon atom at the 5-position is a single bond, R2 represents a hydroxyl group or a tri(lower alkyl)silyloxy group; or R2 forms a carbonyl group or a hydroxime group together with the carbon atom at the 5-position; 2) when —X----Y— represents —CH2—C(═O)—, R1 represents (R11a)(R12a)C [wherein R11a represents a lower alkoxycarbonyl group, or —COOCH2CH═CH2; and R12a represents a hydrogen atom]; and R2 represents a hydroxyl group or a tri(lower alkyl)silyloxy group.

    摘要翻译： 由通式（I）表示的阿维菌素衍生物或其盐：其中-X-Y-表示-CH = CH-，-CH 2 -C（= O） - ， - CH 2 -CH 2 - 或-CH 2 - CH（R 13） - ; 例如，1）当-X ----Y-表示-CH = CH-时，R1表示（R11）（R12）C [其中R11表示取代或未取代的低级烷基; 甲酰基; 低级烷氧基羰基等; R12表示氢原子或低级烷基]。 当R 2与5位的碳原子之间的键是单键时，R 2表示羟基或三（低级烷基）甲硅烷氧基; 或R 2与5-位上的碳原子一起形成羰基或羟基基团; 2）当-X ----Y-表示-CH2-C（= O） - 时，R1表示（R11a）（R12a）C [其中R11a表示低级烷氧基羰基或-COOCH2CH = CH2; R12a表示氢原子]; 并且R 2表示羟基或三（低级烷基）甲硅烷氧基。

    Octacyclodepsipeptides having an endoparasiticidal action
    7.
    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：US06369028B1

    公开(公告)日：2002-04-09

    申请号：US08246029

    申请日：1994-05-19

    申请人： Jürgen Scherkenbeck ,  Peter Jeschke ,  Hans-Georg Lerchen ,  Hermann Hagemann ,  Achim Harder ,  Norbert Mencke ,  Andrew Plant

    发明人： Jürgen Scherkenbeck ,  Peter Jeschke ,  Hans-Georg Lerchen ,  Hermann Hagemann ,  Achim Harder ,  Norbert Mencke ,  Andrew Plant

    IPC分类号： A61K3800

    CPC分类号： C07D273/00 ,  C07C235/12 ,  C07C235/34

    摘要： 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.

    摘要翻译： 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。

    Substituted 1,2,4-oxadiazole derivatives
    10.
    发明授权
    Substituted 1,2,4-oxadiazole derivatives 失效
    取代的1,2,4-恶二唑衍生物

    公开(公告)号：US5371231A

    公开(公告)日：1994-12-06

    申请号：US57584

    申请日：1993-05-05

    申请人： Peter Jeschke ,  Werner Lindner ,  Achim Harder ,  Norbert Mencke ,  Axel Haberkorn

    发明人： Peter Jeschke ,  Werner Lindner ,  Achim Harder ,  Norbert Mencke ,  Axel Haberkorn

    IPC分类号： A61K31/41 ,  A01N43/82 ,  A01N43/836 ,  A61K31/4245 ,  A61P33/00 ,  A61P33/10 ,  C07D271/06

    CPC分类号： C07D271/06 ,  A01N43/82

    摘要： The present invention relates to new substituted 1,2,4-oxadiazole derivatives of the formula (I) and to their stereoisomers ##STR1## in which formula R.sup.4 represents OH, SH, halogenoalkoxy, halogenoalkylthio, halogenoalkylsulphinyl, halogenoalkylsulphonyl, aryloxy, aralkoxy, arylthio, aralkylthio, alkylenedioxy, halogenoalkylenedioxy, amino, alkylamino, dialkylamino, acylamino, carbamoyl, alkylsulphinyl, alkylsulphonyl, arylsuphinyl, arylsulphonyl, sulphonylamino, alkoxycarbonyl, alkylcarbonyl, alkylcarbonyloxy, alkoxyalkyl, alkoxyalkoxy or hydroxyalkoxy, where in the event that at least one of the radicals R.sup.2 or R.sup.3 is other than hydrogen, R.sup.4 additionally represents halogen, alkyl, halogenoalkyl, alkoxy or thioalkyl, where, in the event that R.sup.1 represents optionally substituted C.sub.1-8 -alkyl, R.sup.4 additionally represents alkoxy,processes for their preparation, and their use as endoparasiticides.

    摘要翻译： 本发明涉及式（I）的新的取代的1,2,4-恶二唑衍生物及其立体异构体，其中式R4代表OH，SH，卤代烷氧基，卤代烷硫基，卤代烷基亚磺酰基，卤代烷基磺酰基，芳氧基， 芳烷氧基，芳硫基，芳烷硫基，亚烷基二氧基，卤代亚烷基二氧基，氨基，烷基氨基，二烷基氨基，酰基氨基，氨基甲酰基，烷基亚磺酰基，烷基磺酰基，芳基亚乙基，芳基磺酰基，磺酰基氨基，烷氧基羰基，烷基羰基，烷基羰基氧基，烷氧基烷基，烷氧基烷氧基或羟基烷氧基，其中在至少一个 基团R2或R3不是氢，R4另外表示卤素，烷基，卤代烷基，烷氧基或硫代烷基，其中，在R 1表示任选取代的C 1-8 - 烷基的情况下，R 4另外表示烷氧基，其制备方法， 并将其用作内寄生物杀灭剂。