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    • 4. 发明申请
    • Novel Clerodanes and Methods for Repelling Arthropods
    • 新型克洛膦烷和排斥节肢动物的方法
    • US20100190849A1
    • 2010-07-29
    • US12708726
    • 2010-02-19
    • Charles L. CantrellJerome A. KlunStephen O. Duke
    • Charles L. CantrellJerome A. KlunStephen O. Duke
    • A01N43/20A01N31/04A01N37/00A01P17/00
    • A01N49/00A01N65/00A01N65/22A01N2300/00
    • A method for repelling arthropods involving treating a subject or an object with an arthropod repelling composition containing an arthropod repelling effective amount of at least one clerodane of the formula in which R1 is H, halogen, formyl, a straight chain or branched C1-4 saturated alkyl, a straight chain or branched C2-4 unsaturated alkyl, or an aryl containing 6-10 carbon atoms in the ring skeleton thereof, wherein R1 is unsubstituted or substituted with one or more substituents, which are the same or different, selected from the group consisting of oxo (═O), OR2, CO2R2, and OC(O)R2, wherein R2 is H, a straight chain or branched C1-30 saturated alkyl, a straight chain or branched C2-30 unsaturated alkyl, or an aryl comprising 6-10 carbon atoms in the ring skeleton thereof; wherein R2 is unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, amino, hydroxyl, oxo (═O), thio, cyano and nitro; optionally a carrier, optionally an arthropod repellant, and optionally an insecticide. Preferably the compound is 13,14,15,16-tetranorclerod-3-en-12-al (callicarpenal), 13,14,15,16-tetranorclerod-3-en-12-ol, 13,14,15,16-tetranorclerod-3-en-12-oic acid, β-epoxycallicarpenal, α-epoxycallicarpenal, or mixtures thereof. Also a compound of the above formula. Also an arthropod repellant composition containing an arthropod repelling effective amount of at least one of the compounds of the above formula and a carrier. The present invention does not involve the use of any compound isolated from Callicarpa species other than callicarpenal, intermedeol, or spathulenol.
    • 一种排斥节肢动物的方法,所述节肢动物涉及用节肢动物排斥组合物治疗受试者或物体的方法,所述节肢动物排斥组合物含有节肢动物排斥有效量的至少一种下式的氯化丹烷,其中R 1为H,卤素,甲酰基,直链或支链C 1-4饱和 烷基,直链或支链C 2-4不饱和烷基或其环骨架中含有6-10个碳原子的芳基,其中R1是未取代的或被一个或多个相同或不同的取代基取代,所述取代基选自 由(O)OR 2,CO 2 R 2和OC(O)R 2组成的基团,其中R 2是H,直链或支链C 1-30饱和烷基,直链或支链C 2-30不饱和烷基或芳基 其环骨架中含有6-10个碳原子; 其中R2是未取代的或被一个或多个选自卤素,氨基,羟基,氧代(= O),硫代,氰基和硝基的取代基取代。 任选的载体,任选的节肢动物驱避剂和任选的杀虫剂。 优选地,该化合物是13,14,15,16-四硝基胆甾-3-烯-12-al(愈伤组氨酸),13,14,15,16-四去甲胆甾-3-烯-12-醇,13,14,15,16 抗坏血酸-3-烯-12-酸,和 - 环氧肉桂醛,α-环氧肉桂醛,或其混合物。 也是上述式的化合物。 还有一种节肢动物驱避剂组合物,其含有节肢动物排斥有效量的至少一种上述化合物和载体。 本发明不涉及使用除了卷心菜,中间油或仙客来醇之外的Callicarpa物种分离的任何化合物。
    • 7. 发明授权
    • Methods and compositions for repelling arthropods
    • 用于排斥节肢动物的方法和组合物
    • US06562841B1
    • 2003-05-13
    • US09978154
    • 2001-10-16
    • Jerome A. KlunWalter F. Schmidt
    • Jerome A. KlunWalter F. Schmidt
    • A01N4340
    • A01N43/40G01N33/5085
    • A method for selecting the most effective arthropod repellent from stereoisomers of a compound, involving testing each stereoisomer of the compound for its effectiveness as an arthropod repellent against an arthropod of a particular genus and species, comparing the test results and selecting the most effective arthropod repellent stereoisomer from the stereoisomers of the compound, wherein the compound is a piperidine analog. A composition for repelling arthropods, containing a carrier material and an arthropod repelling effective amount of a stereoisomer of a compound, wherein said stereoisomer is selected by the above method. A method for repelling arthropods (e.g., Aedes aegypti or Aedes albopictus) from a mammal, involving treating the mammal with an arthropod with the above repelling composition (e.g., containing (1S,2′S) stereoisomer of 1-(3-cyclohexen-1-ylcarbonyl)-2-methylpiperidine).
    • 从化合物的立体异构体中选择最有效的节肢动物驱避剂的方法,包括测试化合物的每种立体异构体作为针对特定属和物种的节肢动物的节肢动物驱避剂的有效性,比较测试结果和选择最有效的节肢动物驱避剂 该化合物的立体异构体的立体异构体,其中该化合物是哌啶类似物。 一种用于排斥节肢动物的组合物,其包含载体材料和排斥有效量的化合物的立体异构体的节肢动物,其中所述立体异构体通过上述方法选择。 一种从哺乳动物排斥节肢动物(例如埃及伊蚊或白纹伊蚊)的方法,涉及用上述排斥组合物(例如,含有(1S,2'S)1-(3-环己烯-1-酮)的(1S,2'S)立体异构体的哺乳动物用哺乳动物治疗哺乳动物, 吡啶-2-基羰基)-2-甲基哌啶)。