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    • 3. 发明授权
    • Benzoylurea compounds, and insecticidal and acaricidal compositions
comprising same
    • 苯甲酰脲化合物和包含它们的杀虫和杀螨组合物
    • US4656193A
    • 1987-04-07
    • US778433
    • 1985-09-20
    • Marius S. BrouwerArnoldus C. GrosscurtRoelof van Hes
    • Marius S. BrouwerArnoldus C. GrosscurtRoelof van Hes
    • A01N47/34A01P7/04C07C273/18C07C275/54C07C127/22
    • A01N47/34
    • The invention relates to new benzoylurea compounds of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of halogen and alkyl and haloalkyl having 1-4 carbon atoms,R.sub.2 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of chlorine, methyl and trifluoromethyl, andR.sub.3 is a hydrogen atom or represents 1-3 alkyl and/or alkenyl groups each having 1-6 and/or 2-6 carbon atoms respectively,or wherein R.sub.3 together with the cyclohexyl ring to which it is attached forms a bi- or polycyclic hydrocarbyl group having 8-14 carbon atoms and, if desired, substituted with 1-3 alkyl groups each 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 the control of insects and/or mites in a dosage from 1 to 5000 g of active substance per hectare.
    • 本发明涉及通式为“IMAGE”的新的苯甲酰脲化合物,其中R 1是氢原子或代表1或2个选自卤素和具有1-4个碳原子的烷基和卤代烷基的取代基,R 2是氢 原子或表示1或2个选自氯,甲基和三氟甲基的取代基,R3为氢原子或表示1-3个分别具有1-6个碳原子和/或2-6个碳原子的烷基和/或烯基基团 或其中R 3与其所连接的环己基环一起形成具有8-14个碳原子的双或多环烃基,如果需要,由1-3个分别具有1-4个碳原子的烷基取代。 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。
    • 5. 发明授权
    • Benzoylurea compounds, and insecticidal and acaricidal compositions
comprising same
    • 苯甲酰脲化合物和包含它们的杀虫和杀螨组合物
    • US4783485A
    • 1988-11-08
    • US912169
    • 1986-09-26
    • Marius S. BrouwerArnoldus C. GrosscurtRoelof Van Hes
    • Marius S. BrouwerArnoldus C. GrosscurtRoelof Van Hes
    • A01N47/34A01N47/36C07D213/75C07C127/22
    • C07D213/75A01N47/34A01N47/36
    • The invention relates to new benzoylurea compounds having insecticidal and acaricidal activity, of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom or represents 1 or 2 halogen atoms;Ar is a para-phenylene group or a para-pyridylene group, which groups may be substituted with 1 or 2 substituents selected from the group consisting of chlorine, methyl and trifluoromethyl;B is an oxygen atom or represents a group having the formula ##STR2## wherein R.sub.2 is a hydrogen atom or an alkyl group having 1-4 carbon atoms; andR is a cycloalkyl group or a cycloalkenyl group having 6-12 carbon atoms, which groups may be substituted with 1-3 substituents selected from the group consisting of alkyl and alkenyl having 1-6 carbon atoms, or whereinR is a bi- or polycyclic, saturated or unsaturated, hydrocarbyl group, having 8-14 carbon atoms and, if desired, substituted with 1-3 substituents selected from the group consisting of alkyl and alkenyl having 1-6 carbon atoms;with the proviso, that,if Ar is a whether or not substituted para-phenylene group, andR is a whether or not substituted cyclohexyl-group, or a saturated bi- or polycyclic hydrocarbyl group having 8-14 carbon atoms, then B does not represent an oxygen atom.
    • 本发明涉及具有杀虫和杀螨活性的新的苯甲酰脲化合物,通式为其中R 1为氢原子或表示1或2个卤原子的通式(Ⅰ) Ar是对亚苯基或对 - 亚吡啶基,该基团可以被1或2个选自氯,甲基和三氟甲基的取代基取代; B是氧原子,或表示具有式“IMAGE”的基团,其中R2是氢原子或具有1-4个碳原子的烷基; 并且R是具有6-12个碳原子的环烷基或环烯基,该基团可以被选自具有1-6个碳原子的烷基和烯基的1-3个取代基取代,或其中R是双 - 或具有8-14个碳原子的多环,饱和或不饱和的烃基,如果需要,被1-3个选自具有1-6个碳原子的烷基和烯基的取代基取代; 条件是,如果Ar是否为取代的对亚苯基,R为无取代的环己基,还是具有8-14个碳原子的饱和双环或多环烃基,则B为 不代表氧原子。
    • 7. 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
    • US4665235A
    • 1987-05-12
    • US572143
    • 1984-01-19
    • Marius S. BrouwerArnoldus C. Grosscurt
    • Marius S. BrouwerArnoldus C. Grosscurt
    • A61K31/17A01N47/34A01P7/02A61P35/00C07C275/54C07C127/22
    • C07C275/54A01N47/34
    • 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 trifluormethyl,R.sub.4 is a hydrogen atom or represents 1-3 substituents which are selected from the group consisting of halogen, and alkyl, alkoxy, haloalkyl and haloalkoxy, having 1-4 carbon atoms,X is N or CH,n is 0 or 1, andR.sub.5 is a hydrogen atom, an alkyl group having 1-6 carbon atoms, an alkenyl group having 2-6 carbon atoms, or a cycloalkyl group having 3-6 carbon atoms, with the proviso, that, if n is 0 and R.sub.5 is a hydrogen atom, R.sub.3 is a hydrogen atom.The compounds have an insecticidal and acaricidal activity. After having been processed to compositions, the compounds may be used for the control of insects and/or mites in a dosage of 1 to 5000 grams of active substance per hectare. In addition the compounds have an antitumor 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是氢原子或表示1-3个选自卤素和具有1-4个碳原子的烷基,烷氧基,卤代烷基和卤代烷氧基的取代基,X是N或CH,n 是0或1,R5是氢原子,具有1-6个碳原子的烷基,具有2-6个碳原子的烯基或具有3-6个碳原子的环烷基,条件是如果 n为0,R5为氢原子,R3为氢原子。 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。
    • 8. 发明授权
    • Sulphonyl compounds, method of preparing the new compounds, as well as
aphicidal compositions on the basis of the new compounds
    • US4379157A
    • 1983-04-05
    • US226533
    • 1981-01-19
    • Roelof van HesArnoldus C. GrosscurtWouter Balk
    • Roelof van HesArnoldus C. GrosscurtWouter Balk
    • C07D275/04A01N41/06A01N43/36A01N43/40A01N43/80C07C67/00C07C301/00C07C303/38C07C303/40C07C311/16C07D275/06
    • C07D275/06A01N41/06A01N43/80
    • The invention relates to new sulphonyl compounds of the general formula ##STR1## wherein X is a halogen atom, a phenoxy group, or an alkyl group or alkoxy group having 1-4 carbon atoms and substituted, if desired, with halogen;R.sub.1 is a cyano group, andR.sub.2 is an amino group which, if desired, may be substituted with halogen, with one or two alkenyl groups or alkynyl groups having 2-6 carbon atoms or with one or two alkyl groups having 1-6 carbon atoms, which alkyl groups, together with the nitrogen atom to which they are bound, may form a saturated heterocyclic ring, which ring may also contain a second hetero atom selected from the group consisting of nitrogen, oxygen and sulphur, or which alkyl groups may be substituted with an alkoxy group, having 1-4 carbon atoms, or with a dialkylamino group having 2-6 carbon atoms the alkyl groups of which, together with the nitrogen atom to which they are bound, may form a saturated heterocyclic ring;or whereinR.sub.1 and R.sub.2 together form a S,S-dialkylsulphoximido group the alkyl groups of which comprise 1-4 carbon atoms, or a 1-amino-2-azavinylene group, of which the amino group is substituted, if desired, with a cycloalkylcarbamoyl group having 4-8 carbon atoms, an alkylcarbamoyl group having 2-5 carbon atoms, a dialkylamino group the alkyl group of which comprise 1-4 carbon atoms, or an alkyl group having 1-4 carbon atoms which alkyl group may be substituted with a hydroxy group or one or more halogen atoms;or whereinR.sub.1 and R.sub.2 together form a 1-imino-2-azaethylene group of which the ring nitrogen is substituted with an alkyl group or alkenyl group having 1-4 carbon atoms, and of which the imino group may be substituted with a substituted or non-substituted phenylcarbamoyl group,having aphicidal activity. After having been processed to compositions, the compounds may be used for the control of aphids in agriculture, horticulture and forestry in a dosage from 20 to 5,000 g of active substance per hectare.
    • 9. 发明授权
    • Composition active against mites, whitefly and thrips, pharmaceutical
composition, and new benzoylurea compounds
    • 对螨虫,粉虱和蓟马有活性的组合物,药物组合物和新的苯甲酰脲化合物
    • US4567295A
    • 1986-01-28
    • US572144
    • 1984-01-19
    • Marius S. BrouwerArnoldus C. Grosscurt
    • Marius S. BrouwerArnoldus C. Grosscurt
    • A61K31/17A01N47/34A61P35/00C07C275/54C07C323/44
    • A01N47/34C07C275/54C07C323/44
    • The invention relates to a composition active against mites, whitefly and thrips, which comprises, in addition to a liquid or solid inert carrier material, a benzoylurea compound of the general formula ##STR1## wherein R.sub.1 is hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of chlorine, methyl and trifluoromethyl,R.sub.2 is an alkyl group having 2-4 carbon atoms or a cycloalkyl group having 3 or 4 carbon atoms,R.sub.3 is a hydrogen atom or represents 1-3 substituents which are selected from the group consisting of halogen, and alkyl, alkoxy, haloalkyl and haloalkoxy having 1-4 carbon atoms,R.sub.4 and R.sub.5 are both fluorine atoms, or whereinR.sub.4 is a chlorine atom and R.sub.5 is a hydrogen atom, andX is an oxygen or sulphur atom.The composition may be used in a dosage of 10 to 5000 g of active substance per hectare.The invention further relates to pharmaceutical compositions comprising the above compounds. Finally the invention relates to new benzoylurea compounds and to the preparation thereof.
    • 本发明涉及对螨虫,粉虱和蓟马有活性的组合物,其除液体或固体惰性载体材料之外还包含通式为“IMAGE”的苯甲酰脲化合物,其中R 1是氢原子或表示1或2个取代基, 选自氯,甲基和三氟甲基,R2是具有2-4个碳原子的烷基或具有3或4个碳原子的环烷基,R3是氢原子或表示1-3个选自 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,R4和R5都是氟原子,或者其中R4是氯原子,R5是氢原子,X是氧或硫 原子。 组合物可以以每公顷10-5000克活性物质的剂量使用。 本发明还涉及包含上述化合物的药物组合物。 最后,本发明涉及新的苯甲酰脲化合物及其制备方法。
    • 10. 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。