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    Avermectin derivatives
    5.
    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。

    Nematicidal pyrazoles
    8.
    发明授权
    Nematicidal pyrazoles 失效
    杀线虫剂

    公开(公告)号：US06310049B1

    公开(公告)日：2001-10-30

    申请号：US09762365

    申请日：2001-04-05

    申请人： Katsuaki Wada ,  Takuya Gomibuchi ,  Yuichi Otsu ,  Katsuhiko Shibuya ,  Takahisa Abe ,  Wolfram Andersch ,  Achim Harder ,  Peter Lösel

    发明人： Katsuaki Wada ,  Takuya Gomibuchi ,  Yuichi Otsu ,  Katsuhiko Shibuya ,  Takahisa Abe ,  Wolfram Andersch ,  Achim Harder ,  Peter Lösel

    IPC分类号： A61K314155

    CPC分类号： C07D409/04 ,  A01N43/56 ,  A01N47/16 ,  A01N47/38 ,  C07D333/16 ,  C07D333/22

    摘要： Novel pyrazoles of formula (1) wherein R1 represents halogen, C1-6 alkyl, C1-5 haloalkyl, C2-6 alkoxy, C1-4 alkylthio, C2-5 alkenyloxy, C3-5 alkynyloxy, C2-6 (total carbon number) alkoxyalkyl, C2-6 (total carbon number) alkylthioalkyl, C1-5 haloalkoxy, C2-6 (total carbon number) alkoxyalkoxy, hydroxy or optionally substituted phenyl, R2 represents hydrogen, halogen, C1-5 alkyl, C2-6 (total carbon number) alkoxyalkyl, C2-6 (total carbon number) alkylthioalkyl, C2-6 (total carbon number) alkylsulfinylalkyl, C2-6 (total carbon number alkylsulfonylalkyl or C1-5 haloalkyl, R3 represents hydrogen, C1-5 alkyl, —COR4, COOR5, CH(OR6)2 or CH2Si(R7)3, R4 represents C1-10 alkyl, C1-6 haloalkyl, C2-6 alkenyl, optionally substituted C3-6 cycloalkyl, C2-6 (total carbon number) alkoxyalkyl, C2-6 (total carbon number alkylthioalkyl, optionally substituted phenyl, C1-6 haloalkyl, alkylamino, di-(C1-6 alkyl)amino or optionally substituted phenylamino, R5 represents C1-7 alkyl, R6 and R7 represent C1-6 alkyl, and n is 1, 2 or 3, and when n is 2 or 3, the corresponding number (n) of R1 radicals may be the same or different, processes for preparing these compounds and their use as nematicides and anthelmintics.

    摘要翻译： 式（1）的新型吡唑其中R1表示卤素，C1-6烷基，C1-5卤代烷基，C2-6烷氧基，C1-4烷硫基，C2-5烯氧基，C3-5炔氧基，C2-6（总碳数） 烷氧基烷基，C 2-6（总碳数）烷硫基烷基，C 1-5卤代烷氧基，C 2-6（总碳数）烷氧基烷氧基，羟基或任选取代的苯基，R 2表示氢，卤素，C 1-5烷基，C 2-6 数量）烷氧基烷基，C2-6（总碳数）烷硫基烷基，C2-6（总碳数）烷基亚磺酰基烷基，C2-6（总碳数烷基磺酰基烷基或C1-5卤代烷基，R3表示氢，C1-5烷基，-COR4， COOR 5，CH（OR 6）2或CH 2 Si（R 7）3，R 4表示C 1-10烷基，C 1-6卤代烷基，C 2-6烯基，任选取代的C 3-6环烷基，C 2-6（总碳数）烷氧基烷基， 6（总碳数烷基硫代烷基，任选取代的苯基，C 1-6卤代烷基，烷基氨基，二 - （C 1-6烷基）氨基或任选取代的苯基氨基，R 5表示C 1-7烷基，R 6和R 7表示C 1-6 kyl，n为1,2或3，当n为2或3时，R1基团的相应数目（n）可以相同或不同，制备这些化合物的方法及其作为杀线虫剂和驱肠虫剂的用途。