Fused 1-(2,6-dichloro-4-trifluoromethylphenyl)-pyrazoles, the synthesis thereof and the use thereof as pesticides
    3.
    发明授权
    Fused 1-(2,6-dichloro-4-trifluoromethylphenyl)-pyrazoles, the synthesis thereof and the use thereof as pesticides 有权
    熔融的1-(2,6-二氯-4-三氟甲基苯基) - 吡唑,其合成及其作为农药的用途

    公开(公告)号:US06545033B1

    公开(公告)日:2003-04-08

    申请号:US09680275

    申请日:2000-10-06

    IPC分类号: A61K31416

    摘要: The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I: or a salt thereof, where R1 is amino, hydrogen, alkyl, hydroxy, halo, alkoxy, alkylamino, dialkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, trifluoroalkylsulfinyl, trifluoroalkylsulfonyl, hydroxy, amino, trifluoromethyl, acetylamino, —OSO2R2, —OS(O)R2, —OC(O)R2, —OC(O)NHR2, or —NHC(O)NHR2 where R2 is C1-4 alkyl or optionally substituted aryl; X, Y and Z are each independently (CH)n, (CR3R4)n, S, S(O), or SO2, wherein n is 1-2, R3 and R4 are defined herein; Q is N or C—R6, wherein R6 is fluoro, chloro, bromo, or iodo; R5 is halo, C1-C6 alkyl, C1-C4 alkenyl, C1-C4 alkoxy, C1-C4 alkylamino, C1-C4 dialkylamino, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 trifluoroalkylsulfinyl, C1-C4 trifluoroalkylsulfonyl, hydroxy, amino, or trifluoromethyl; and with the proviso that only one of X, Y and Z can be S, S(O) or SO2.

    摘要翻译: 本发明涉及新颖的吡唑衍生物及其作为杀虫剂的用途。 吡唑衍生物具有式I或其盐,其中R 1是氨基,氢,烷基,羟基,卤素,烷氧基,烷基氨基,二烷基氨基,烷硫基,烷基亚磺酰基,烷基磺酰基,三氟烷基亚磺酰基,三氟烷基磺酰基,羟基,氨基,三氟甲基,乙酰氨基, ,-OS(O)R 2,-OC(O)R 2,-OC(O)NHR 2或-NHC(O)NHR 2,其中R 2为C 1-4烷基或任选取代的芳基; X,Y和Z各自独立地为 CH)n,(CR 3 R 4)n,S,S(O)或SO 2,其中n为1-2,R 3和R 4如本文所定义; Q为N或C-R6,其中R6为氟,氯,溴, 或碘; R5是卤素,C1-C6烷基,C1-C4链烯基,C1-C4烷氧基,C1-C4烷基氨基,C1-C4二烷基氨基,C1-C4烷硫基,C1-C4烷基亚磺酰基,C1-C4烷基磺酰基,C1-C4 三氟烷基亚磺酰基,C 1 -C 4三氟烷基磺酰基,羟基,氨基或三氟甲基; 并且条件是X,Y和Z中只有一个可以是S,S(O)或SO 2。

    Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands
    4.
    发明授权
    Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands 有权
    放射性标记的1-芳基吡唑,其合成及其作为害虫GABA受体配体的用途

    公开(公告)号:US06409988B1

    公开(公告)日:2002-06-25

    申请号:US09606051

    申请日:2000-06-29

    IPC分类号: A61K5100

    摘要: The present invention is directed to radiolabeled compounds of Formula I: or salts thereof, where R1 represents R8, R8O, R8SO2, R8SO or R8S in which R8 is tritiated or deuterated methyl; X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond; R2 is hydrogen or amino; and R3-R7 are defined in the specification. The invention is also directed to methods of using such compounds for demonstrating specific insect GABA receptors, qualitatively screening for compounds acting on an insect GABA receptor or quantitatively assaying concentrations of a compound acting on an insect GABA receptor.

    摘要翻译: 本发明涉及放射性标记的式I化合物或其盐,其中R 1表示R8,R8O,R8SO2,R8SO或R8S,其中R8为氚化或氘代甲基; X为卤素,氰基,C1-6烷氧基羰基,C2-6 炔基,任选取代的C 6-14芳基或经由碳 - 碳键与噻唑连接的任选取代的5至7元杂芳环; R 2是氢或氨基; 本发明还涉及使用这些化合物来证明特异性昆虫GABA受体的方法,定性筛选作用于昆虫GABA受体的化合物或定量测定作用于昆虫GABA受体的化合物的浓度 。