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    • 85. 发明授权
    • Benzoylurea compounds, and pesticidal and pharmaceutical compositions
comprising same
    • 苯甲酰脲化合物,以及包含其的杀虫剂和药物组合物
    • US4550202A
    • 1985-10-29
    • US572145
    • 1984-01-19
    • Marius S. BrouwerArnoldus C. Grosscurt
    • Marius S. BrouwerArnoldus C. Grosscurt
    • A61K31/17A01N47/34A01P7/02C07C67/00C07C239/00C07C251/50C07C275/54C07C325/00C07C335/26C07D213/53C07C157/12C07C127/22
    • C07D213/53A01N47/34C07C275/54
    • The invention relates to new benzoylurea compounds of the general formula ##STR1## wherein R.sub.1 is a halogen atom,R.sub.2 is a hydrogen atom or a halogen atom,R.sub.3 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of chlorine, methyl and trifluoromethyl,R.sub.4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a cycloalkyl group having 3-6 carbon atoms,R.sub.5 is a hydrogen atom or an alkyl group having 1-4 carbon atoms, andA is a phenyl group or a heteroaryl group having 1 or 2 nitrogen atoms, which groups may be substituted with 1-3 substituents which are selected from the group consisting of halogen, and alkyl, alkoxy, haloalkyl and haloalkoxy having 1-4 carbon atoms.The compounds have an insecticidal and acaricidal activity. After having been processed to compositions, the compounds may be used for control of insects and/or mites in a dosage from 1 to 5000 g of active substance per hectare. In addition the compounds have an anti-tumor activity and may be used in pharmaceutical compositions.
    • 本发明涉及通式为“IMAGE”的新的苯甲酰脲化合物,其中R 1为卤素原子,R 2为氢原子或卤素原子,R 3为氢原子或表示1或2个选自以下的取代基: 氯,甲基和三氟甲基,R4是氢原子,具有1-6个碳原子的烷基或具有3-6个碳原子的环烷基,R5是氢原子或具有1-4个碳原子的烷基,A 是具有1或2个氮原子的苯基或杂芳基,该基团可以被选自卤素和具有1-4个碳原子的烷基,烷氧基,卤代烷基和卤代烷氧基的1-3个取代基取代。 这些化合物具有杀虫和杀螨活性。 经处理成组合物后,化合物可用于以每公顷1至5000克活性物质的剂量控制昆虫和/或螨虫。 此外,化合物具有抗肿瘤活性并可用于药物组合物。
    • 86. 发明授权
    • 2,5-Dihalogenobenzoyl-(thio)urea insecticides
    • 2,5-二卤代苯甲酰 - (硫)脲类杀虫剂
    • US4533676A
    • 1985-08-06
    • US487799
    • 1983-04-22
    • Wilhelm SirrenbergErich KlaukeIngeborg Hammann
    • Wilhelm SirrenbergErich KlaukeIngeborg Hammann
    • A01N47/34C07C67/00C07C275/54C07C309/66C07C313/00C07C317/42C07C323/19C07C323/20C07C323/44C07C325/00C07C335/26C07D317/46C07D319/08C07D319/20C07C127/22
    • C07D319/08A01N47/34C07C275/54C07C309/66C07C317/42C07C323/19C07C323/20C07C323/44C07D317/46C07D319/20
    • A 2,5-dihalogenobenzoyl-(thio)urea of the formula ##STR1## in which X represents sulphur or oxygen,X.sup.1 and X.sup.2 are identical or different and represent fluorine, chlorine, bromine or iodine,R.sup.1 represents hydrogen, halogen, or optionally substituted radicals from the series comprising alkyl, alkoxy and alkylthio,R.sup.2 represents hydrogen, halogen, cyano, nitro or optionally substituted radicals from the series comprising alkyl, alkylthio, alkylsulphonyl, alkoxy, aryloxy, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl and alkoxycarbonylalkylthio,R.sup.1 and R.sup.2 together represent an optionally substituted alkylenedioxy radical or represent --CF.sub.2 --O--CF.sub.2 --O--,R.sup.3 represents hydrogen, halogen, or an optionally substituted alkyl, alkoxy or aryloxy radical, andR.sup.4 represents hydrogen, halogen, or optionally substituted radicals from the series comprising alkyl, alkylthio and alkoxy, with the exception of those cases in which X represents oxygen, X.sup.1 and X.sup.2 represent chlorine and (a) R.sup.1 represents chlorine, R.sup.2 represents OCF.sub.2 CHFCL and R.sup.3 and R.sup.4 represent hydrogen, or (b) R.sup.1 represents chlorine, R.sup.2 represents OCF.sub.3 and R.sup.3 and R.sup.4 represent hydrogen, or (c) R.sup.2 represents OCF.sub.3 and R.sup.1, R.sup.3 and R.sup.4 represent hydrogen, which possesses insecticidal activity.
    • 其中X表示硫或氧,X1和X2的式“IMAGE”的2,5-二卤代苯甲酰基(硫代)脲相同或不同,表示氟,氯,溴或碘,R1表示氢,卤素或任选地 取代基包括烷基,烷氧基和烷硫基,R2代表氢,卤素,氰基,硝基或任选取代的基团,其中包括烷基,烷硫基,烷基磺酰基,烷氧基,芳氧基,烷基羰基,烷氧基羰基,烷氧基羰基烷基和烷氧羰基烷硫基,R1和R2 一起代表任选取代的亚烷基二氧基或代表-CF2-O-CF2-O-,R3代表氢,卤素或任选取代的烷基,烷氧基或芳氧基,R4代表氢,卤素或任选取代的基团 包括烷基,烷硫基和烷氧基,除了其中X表示氧,X1和X2表示氯的那些情况,(a)R1代表氯 R表示OCF2CHFCL,R3和R4表示氢,或(b)R1表示氯,R2表示OCF3,R3和R4表示氢,或(c)R2表示OCF3,R1,R3和R4表示氢,具有杀虫活性 。