TW201307319A - Insecticidal compounds - Google Patents
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本發明係關於具有殺蟲活性的新穎三唑衍生物及製備它們之方法與中間體,含其之殺蟲、殺蟎、殺線蟲或殺軟體動物組成物,及使用其對抗與控制昆蟲、蟎、線蟲或軟體動物有害生物的方法。 The present invention relates to a novel triazole derivative having insecticidal activity and a method and an intermediate thereof for preparing the same, comprising an insecticidal, acaricidal, nematicidal or molluscicidal composition thereof, and using the same for controlling and controlling insects and cockroaches , a method of nematode or mollusc pests.
因此,本發明提供式(I)的化合物
式(I)的化合物可能以不同的空間異構體、光學異構體(鏡像異構體及/或非鏡像異構體)或互變異構體形式存在。本發明包括所有這類的異構體和互變異構體及其各種比例混合物,以及同位素形式,例如氘化化合物。 The compounds of formula (I) may exist in different spatial isomers, optical isomers (Spiegelmer and/or non-Spiegelmer) or tautomeric forms. The present invention includes all such isomers and tautomers, as well as mixtures thereof in various ratios, as well as isotopic forms such as deuterated compounds.
除非另有說明,否則作為單獨部分或另一基團之一部分(例如,烷氧基、烷基羰基或烷氧羰基)的烷基可呈直鏈或支鏈,較佳可能包含1至6個碳原子,更佳1至4個,最佳1至3個。烷基的實例包括甲基、乙基、正丙基、異丙基、正丁基、第二丁基、異丁基和第三丁基。 Unless otherwise stated, an alkyl group as a single moiety or as part of another group (eg, alkoxy, alkylcarbonyl or alkoxycarbonyl) may be straight or branched, preferably containing from 1 to 6 More preferably 1 to 4 carbon atoms, most preferably 1 to 3. Examples of the alkyl group include a methyl group, an ethyl group, a n-propyl group, an isopropyl group, a n-butyl group, a second butyl group, an isobutyl group, and a tert-butyl group.
除非另有說明,否則作為單獨部分或另一取代基之一部分的烯基與炔基,可採直鏈或支鏈,且較佳可含有2至6個碳原子,較佳2至4個,更佳2至3個,而且在適當情況下,可採(E)或(Z)組態。實例包括乙烯基、烯丙基、炔丙 基。 Unless otherwise stated, alkenyl and alkynyl as part of a single moiety or another substituent may be straight or branched, and preferably may contain from 2 to 6 carbon atoms, preferably from 2 to 4. More preferably 2 to 3, and where appropriate, an (E) or (Z) configuration is available. Examples include vinyl, allyl, propargyl base.
鹵素係指氟、氯、溴或碘。 Halogen means fluorine, chlorine, bromine or iodine.
鹵烷基可能包含一個或多個相同或相異的鹵原子,並包括,舉例來說,三氟甲基、氯二氟甲基、2,2,2-三氟乙基或2,2-二氟乙基。全氟烷基是能以氟原子完全取代的烷基,且包括,舉例來說,三氟甲基、五氟乙基和七氟丙-2-基。 A haloalkyl group may contain one or more of the same or different halo atoms and includes, for example, trifluoromethyl, chlorodifluoromethyl, 2,2,2-trifluoroethyl or 2,2- Difluoroethyl. The perfluoroalkyl group is an alkyl group which can be completely substituted with a fluorine atom, and includes, for example, a trifluoromethyl group, a pentafluoroethyl group, and a heptafluoroprop-2-yl group.
鹵烯基和鹵炔基可能包含一個或多個相同或相異的鹵原子,並包括,舉例來說,2,2-二氟乙烯基、1,2-二氯-2-氟乙烯基或1氯丙-2-炔-1-基。 The haloalkenyl and haloalkynyl groups may contain one or more of the same or different halo atoms and include, for example, 2,2-difluorovinyl, 1,2-dichloro-2-fluorovinyl or 1 chloroprop-2-yn-1-yl.
除非另有說明,環烷基可能是單環或雙環,可選擇性地由一個或多個C1-C6烷基取代,且較佳包含3至8個碳原子,更佳3至6個碳原子。環烷基的實例包括環丙基、1-甲基環丙基、2-甲基環丙基、環丁基、環戊基和環己基。 Unless otherwise stated, a cycloalkyl group may be monocyclic or bicyclic, optionally substituted by one or more C 1 -C 6 alkyl groups, and preferably contains from 3 to 8 carbon atoms, more preferably from 3 to 6 carbon atom. Examples of the cycloalkyl group include a cyclopropyl group, a 1-methylcyclopropyl group, a 2-methylcyclopropyl group, a cyclobutyl group, a cyclopentyl group, and a cyclohexyl group.
鹵環烷基可能包含一個或多個相同或相異的鹵原子,並包括,舉例來說,2,2-二氯環丙基、2,2-二氯-1-甲基環丙基和2-氯基-4-氟環己基。 Halocycloalkyl groups may contain one or more identical or different halogen atoms and include, for example, 2,2-dichlorocyclopropyl, 2,2-dichloro-1-methylcyclopropyl, and 2-Chloro-4-fluorocyclohexyl.
芳基包括苯基、萘基、蔥基、茚基、菲基和聯苯,較佳為苯基。 The aryl group includes a phenyl group, a naphthyl group, an onion group, an anthracenyl group, a phenanthryl group and a biphenyl group, preferably a phenyl group.
雜芳基係指單環、雙環或三環芳香烴,包含3至14個,較佳為5至10個,更佳為6至8個環原子,包括1至6個,較佳為1至4個獨立選自氮、氧和硫之雜原子。實例包括呋喃基、噻吩基、吡咯基、咪唑基、吡唑基、噻唑基、異噻唑基、唑基、異唑基、二唑基、噻二唑基、三唑基、四唑基、吡啶基、嗒基、嘧啶基、吡基、三 基、四基、吲哚基、苯並噻吩基、苯並呋喃基、苯並咪唑基、苯並噻二唑基、吲唑基、苯並三唑基、苯並噻唑基、苯並唑基、喹啉基、異喹啉基、酞基、喹啉基、喹唑啉基、啉基和萘啶基。 Heteroaryl means a monocyclic, bicyclic or tricyclic aromatic hydrocarbon containing from 3 to 14, preferably from 5 to 10, more preferably from 6 to 8 ring atoms, including from 1 to 6, preferably from 1 to Four heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur. Examples include furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, Azolyl, different Azolyl, Diazolyl, thiadiazolyl, triazolyl, tetrazolyl, pyridyl, anthracene Base, pyrimidinyl, pyridyl Base, three Base, four Base, fluorenyl, benzothienyl, benzofuranyl, benzimidazolyl, benzothiadiazolyl, oxazolyl, benzotriazolyl, benzothiazolyl, benzo Azyl, quinolinyl, isoquinolinyl, anthracene Base Lolinyl, quinazolinyl, Andolinyl and naphthyridinyl.
雜環基(如同此處所使用的)包括雜芳基,此外可能是一個飽和或部分不飽和的環烴,包含3至10個環原子,其中高至4個是選自氮、氧和硫的雜原子,且可選擇性地由獨立選自鹵素、硝基、氰基、烷基、烷氧基的一個或多個基團取代。非芳香雜環基的實例是環氧乙烷基、四氫吖唉基(azetidinyl)、四氫呋喃基、噻基、吡咯啶基、吡咯啉基、咪唑啶基、咪唑啉基、環丁碸基、二基、二氫吡喃基、四氫吡喃基、哌啶基、吡唑啉基、吡唑啶基、二烷基、嗎啉基、二噻烷基、硫代嗎啉基、哌基、氮呯基、氧雜吖庚因基(oxazepinyl)、硫氮呯基(thiazepinyl)、噻唑啉基和二氮雜環庚基(diazapanyl)。 Heterocyclyl (as used herein) includes heteroaryl, and may also be a saturated or partially unsaturated cyclic hydrocarbon containing from 3 to 10 ring atoms, up to four of which are selected from the group consisting of nitrogen, oxygen and sulfur. A heteroatom, and optionally substituted with one or more groups independently selected from halo, nitro, cyano, alkyl, alkoxy. Examples of non-aromatic heterocyclic groups are oxiranyl, azetidinyl, tetrahydrofuranyl, thio Base, pyrrolidinyl, pyrrolinyl, imidazolidinyl, imidazolinyl, cyclobutenyl, di , dihydropyranyl, tetrahydropyranyl, piperidinyl, pyrazolinyl, pyrazolyl, di Alkyl, morpholinyl, dithiaalkyl, thiomorpholinyl, piperidine a base, a nitrogen sulfhydryl group, an oxazepinyl group, a thiazepinyl group, a thiazolinyl group, and a diazapyl group.
A1、A2、A3、A4、R1、R2、R3、G1、X、Q1、Q2、R5、R6、R7的較佳值係,以任何組合,如下所述。 Preferred values of A 1 , A 2 , A 3 , A 4 , R 1 , R 2 , R 3 , G 1 , X, Q 1 , Q 2 , R 5 , R 6 , R 7 are, in any combination, As described below.
A1較佳為C-X。 A 1 is preferably CX.
A2較佳為C-X。 A 2 is preferably CX.
A3較佳為C-X。 A 3 is preferably CX.
A4較佳為C-X。 A 4 is preferably CX.
X較佳為氫、鹵素、氰基、甲基、三氟甲基或甲氧基。更佳的是,X為氫、氟基、氯基、氰基、三氟甲基或甲氧基。甚至更佳的是,X為氫、氟基、氰基或甲氧基。最佳的是, X為氫、氟基或氰基。 X is preferably hydrogen, halogen, cyano, methyl, trifluoromethyl or methoxy. More preferably, X is hydrogen, fluoro, chloro, cyano, trifluoromethyl or methoxy. Even more preferably, X is hydrogen, fluoro, cyano or methoxy. Best of all, X is hydrogen, a fluorine group or a cyano group.
較佳的是,A1、A2、A3和A4為C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且A2和A3較佳為CH;A1和A4為C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且更佳的是,各X皆獨立選自氫、氟基、氰基和甲氧基。甚至更佳的是,A1、A2、A3和A4為C-X,且各X皆獨立選自氫、氟基、氰基和甲氧基。最佳的是,A1為CH、C-CN、C-Cl或C-F;A2、A3和A4為CH或者A1、A2和A3為CH且A4為CH、C-OCH3或C-F。最佳的是,A1為CH、C-CN、C-Cl或C-F;A2、A3和A4為CH。進一步最佳的是A1、A2和A3為CH,且A4為CH、C-OCH3或C-F。 Preferably, A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and methoxy, and A 2 and A 3 is preferably CH; A 1 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and methoxy, and more preferably, each X is independent. It is selected from the group consisting of hydrogen, fluorine, cyano and methoxy. Even more preferably, A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy. Most preferably, A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH or A 1 , A 2 and A 3 are CH and A 4 is CH, C-OCH 3 or CF. Most preferably, A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH. Further preferably, A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF.
G1較佳為氧。 G 1 is preferably oxygen.
R1較佳為氫、甲基、乙基或乙醯基。更佳的是,R1為氫、甲基或乙基。最佳的是,R1為氫。 R 1 is preferably hydrogen, methyl, ethyl or ethyl fluorenyl. More preferably, R 1 is hydrogen, methyl or ethyl. Most preferably, R 1 is hydrogen.
R2較佳為氫、甲基、三氟甲基或鹵素。更佳的是,R2為氫、三氟甲基或鹵素。甚至更佳的是,R2為氫或鹵素。最佳的是,R2為氫。 R 2 is preferably hydrogen, methyl, trifluoromethyl or halogen. More preferably, R 2 is hydrogen, trifluoromethyl or halogen. Even more preferably, R 2 is hydrogen or halogen. Most preferably, R 2 is hydrogen.
Q1較佳為芳基或雜芳基;各自選擇性地由一至五個獨立選自氰基、硝基、羥基、溴基、氯基、氟基、甲基、三氟甲基、甲氧基、三氟甲氧基、甲硫基、甲亞磺醯基、甲磺醯基和苯基的取代基取代。 Q 1 is preferably an aryl or heteroaryl group; each of which is optionally independently selected from one to five selected from the group consisting of cyano, nitro, hydroxy, bromo, chloro, fluoro, methyl, trifluoromethyl, methoxy Substituent substitution of a group, a trifluoromethoxy group, a methylthio group, a sulfinyl group, a methanesulfonyl group, and a phenyl group.
更佳的是,Q1為苯基、吡啶基、呋喃基、噻吩基、吡唑基或1,2,3-噻二唑基;各自選擇性地由一至四個獨立選自 氰基、硝基、羥基、溴基、氯基、氟基、甲基、三氟甲基、甲氧基、三氟甲氧基、甲硫基、甲亞磺醯基、甲磺醯基和苯基的取代基取代。 More preferably, Q 1 is phenyl, pyridyl, furyl, thienyl, pyrazolyl or 1,2,3-thiadiazolyl; each of which is optionally independently selected from one to four selected from the group consisting of cyano and nitrate Substituents of hydroxy, bromo, bromo, chloro, fluoro, methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylthio, sulfinyl, methylsulfonyl and phenyl groups Substituted.
甚至更佳的是,Q1為苯基、吡啶基或吡唑基;各自選擇性地由一至四個獨立選自氰基、硝基、羥基、溴基、氯基、氟基、甲基、乙基、三氟甲基、甲氧基、三氟甲氧基、甲硫基、甲亞磺醯基、甲磺醯基和苯基的取代基取代。 Even more preferably, Q 1 is phenyl, pyridyl or pyrazolyl; each optionally one to four independently selected from the group consisting of cyano, nitro, hydroxy, bromo, chloro, fluoro, methyl, Substituent substitution of ethyl, trifluoromethyl, methoxy, trifluoromethoxy, methylthio, sulfinyl, methanesulfonyl and phenyl.
最佳的是,Q1為苯基或吡啶基;各自選擇性地由一個、兩個或三個獨立選自氰基、硝基、氯基、氟基、甲基、乙基、三氟甲基、甲氧基和三氟甲氧基的取代基取代。 Most preferably, Q 1 is phenyl or pyridyl; each of which is optionally selected from one, two or three independently from cyano, nitro, chloro, fluoro, methyl, ethyl, trifluoromethyl Substituent substitution of a methoxy group and a trifluoromethoxy group.
在另一較佳具體實例中,Q1為C1-C8烷基或由一至五個R4取代的C1-C8烷基、C2-C8烯基或由一至五個R4取代的C2-C8烯基、C2-C8炔基或由一至五個R4取代的C2-C8炔基、C3-C10環烷基或由一至五個R4取代的C3-C10環烷基,且各R4獨立的為鹵素、氰基、硝基、羥基、C1-C8烷氧基、C1-C8鹵烷氧基、C1-C8烷硫基、C1-C8鹵烷硫基、C1-C8烷基亞磺醯基、C1-C8鹵烷基亞磺醯基、C1-C8烷基磺醯基、C1-C8鹵烷基磺醯基、C1-C8烷基羰基、C1-C8烷氧基羰基、芳基或被一個至五個R3取代的芳基、或雜環基或被一個至五個R3取代的雜環基,且R3具有上下文中所賦與的意義。 In another preferred specific example, Q 1 is C 1 -C 8 alkyl or by one to five R 4 is a substituted C 1 -C 8 alkyl, C 2 -C 8 alkenyl group or by one to five R 4 substituted C 2 -C 8 alkenyl, C 2 -C 8 alkynyl group, or, C 3 -C 10 cycloalkyl or substituted by one to five R 4 is a substituted C 2 -C 8 alkynyl group by one to five R 4 C 3 -C 10 cycloalkyl, and each R 4 is independently halogen, cyano, nitro, hydroxy, C 1 -C 8 alkoxy, C 1 -C 8 haloalkoxy, C 1 -C 8 alkylthio, C 1 -C 8 haloalkylthio, C 1 -C 8 alkylsulfinyl, C 1 -C 8 haloalkylsulfinyl, C 1 -C 8 alkylsulfonyl , C 1 -C 8 haloalkylsulfonyl, C 1 -C 8 alkylcarbonyl, C 1 -C 8 alkoxycarbonyl, aryl or aryl substituted by one to five R 3 or a heterocyclic ring A group or a heterocyclic group substituted by one to five R 3 , and R 3 has the meaning imparted in the context.
在另一更佳具體實例中,Q1為C1-C4烷基或由一至五個R4取代的C1-C4烷基、C2-C8烯基或由一至五個R4取代的C2-C8烯基、C2-C8炔基或由一至五個R4取代的C2-C8炔基、C3-C6環烷基或由一至五個R4取代的C3-C6環烷基,且 各R4獨立的為鹵素、氰基、硝基、羥基、C1-C4烷氧基、C1-C4鹵烷氧基、C1-C4烷硫基、C1-C4鹵烷硫基、C1或者芳基或由一至五個R3取代的芳基,或是雜環基或由一個至五個R3取代的雜環基;且R3具有上下文中所賦與的意義,或R3較佳為H或鹵素。 In another particular example, more preferably, Q 1 is C 1 -C 4 alkyl, or substituted by one to five R 4 C 1 -C 4 alkyl, C 2 -C 8 alkenyl group or by one to five R 4 substituted C 2 -C 8 alkenyl, C 2 -C 8 alkynyl group or substituted by one to five R 4 C 2 -C 8 alkynyl, C 3 -C 6 cycloalkyl, or substituted by one to five R 4 C 3 -C 6 cycloalkyl, and each R 4 is independently halogen, cyano, nitro, hydroxy, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, C 1 -C a 4 -alkylthio group, a C 1 -C 4 haloalkylthio group, a C 1 or aryl group or an aryl group substituted by one to five R 3 or a heterocyclic group or a heterocyclic group substituted by one to five R 3 And R 3 has the meaning given in the context, or R 3 is preferably H or halogen.
在另一甚至更佳具體實例中,Q1為C1-C4烷基或由一至五個R4取代的C1-C4烷基、C2-C8烯基或由一個至五個R4取代的C2-C8烯基、C2-C8炔基或由一至五個R4取代的C2-C8炔基、C3-C6環烷基或由一至五個R4取代的C3-C6環烷基,且各R4獨立的為鹵素、氰基、硝基、羥基、C1-C4烷氧基、C1-C4鹵烷氧基,或者芳基或由一至五個R3取代的芳基,或是雜環基或由一至五個R3取代的雜環基;且R3具有上下文中所賦與的意義,或R3較佳為H或鹵素。 In another even more preferred embodiment, Q 1 is C 1 -C 4 alkyl or C 1 -C 4 alkyl, C 2 -C 8 alkenyl substituted by one to five R 4 or from one to five R 4 is a substituted C 2 -C 8 alkenyl, C 2 -C 8 alkynyl group or substituted by one to five R 4 C 2 -C 8 alkynyl, C 3 -C 6 cycloalkyl, or by one to five R a 4- substituted C 3 -C 6 cycloalkyl group, and each R 4 is independently halogen, cyano, nitro, hydroxy, C 1 -C 4 alkoxy, C 1 -C 4 haloalkoxy, or aryl a aryl group substituted by one to five R 3 or a heterocyclic group or a heterocyclic group substituted by one to five R 3 ; and R 3 has the meaning given in the context, or R 3 is preferably H Or halogen.
Q1較佳實例包括(2,6-二氯苯基)-甲基、(4-甲氧基苯基)-甲基、(E)-2-異丁氧基乙烯基、1-(4-氯苯基)-2-甲基-丙烷-1-基、1-(4-氯苯基)-5-三氟甲基-1H-吡唑-4-基、1-(4-氯苯基)環戊基、1-(4-氟苯基)-5-甲基-1H-吡唑-4-基、1-甲基-1H-苯並三唑-5-基、1-甲基-3-第三丁基-1H-吡唑-5-基、1-甲基-3-三氟甲基-4-氯-1H-吡唑-5-基、1-甲基苯並三唑-5-基、1-苯基-5-丙基-1H-吡唑-4-基、1-苯基-5-三氟甲基-1H-吡唑-4-基、1-苯乙基、1-第三丁基-5-甲基-1H-咪唑-4-基、2,3-二氟基-苯基、2,4-二氟基-苯基、2,4,6-三甲基苯基、2,4-二氯苯基、2,6-二氯基-苯基、2,1,3-苯並二唑-5-基、2,2,3,3,4,4,4-七氟丁烷基、2,2,3,3-四氟基-1-甲基-環丁烷 基、2,3-二氟基-苯基、2,4,6-三氟基-苯基、2,4-二氟基-苯基、2,4-二甲基-1,1,3-三氧-2,3-二氫-1H-1 λ *6*-苯並[d]異噻唑-5-基、2,5-二甲基-呋喃-3-基、2,5-二甲基吡唑-3-基、2,6-二氯-4-吡啶基、2-氯基-3-吡啶基、2-氯基-4-氰基-苯基、2-氯基-4-甲磺醯基-苯基、2-氯-6-甲氧基-4-吡啶基、2-氯基-苯基、2-氯噻唑-5-基、2-乙基己基、2-氟基-4-三氟甲基-苯基、2-氟基-5-氯基-苯基、2-氟基-5-三氟甲基-苯基、2-氟基-苯基、2-異丙磺醯苯基、2-甲氧基-苯基、2-甲基-4-氰基-苯基、2-甲基-4-氟基-苯基、2-甲基-4-硝基-苯基、2-甲基乙基、2-甲基-苯基、2-甲磺醯乙基、2-苯噻唑-4-基、2-苯基-噻唑-4-基、2-吡啶基、2-噻吩甲基、2-三氟甲氧基-苯基、2-三氟甲基-4-氟苯基、2-三氟甲基-苯基、3-(2-氯基-苯基)-5-甲基-異唑-4基、3,5-二氟苯基、3,5-二甲基-異唑-4-基、3-氯基-2,2-二甲基-丙烷基、3-氯基-4-(異丙磺醯基)-噻吩-2-基、3-氯基-4-異丙磺醯基-噻吩-2-基、3-氯基-5-三氟甲基-2-吡啶基、3-氯基-苯並[b]噻吩-2-基、3-氯噻吩-2-基、3-氯基-噻吩-2-基、3-吡啶基、3-吡啶基-N-氧化物、3-三氟甲基-4-氟基-苯基、3-三氟甲苯基、4-(氯甲基)苯基、4-氰基-2-甲基-苯基、4-氰基-苯基、4-氟-2-氯基-苯基、4-氟苄基、4-氟基-苯基、4-甲基-[1,2,3]噻二唑、4-甲基-[1,2,3]噻二唑基、4-甲基-苯基、4-甲磺醯苯基、4-硝基-2-氯基-苯基、4-硝基-苯基、4-吡啶基、4-吡啶-N-氧化物、4-第三丁基苯基、4-三氟甲氧基-苯基、4-三氟甲基-苯基、5-氯基-1-甲基-1H-吡唑-4-基、5-氯基-3-吡啶基、5-甲基-2-苯基-2H-[1,2,3]三 唑-4-基、5-甲基-2-三氟甲基-呋喃-3-基、5-甲基-3-(2-氯基-5-氟基-苯基)-異唑-4-基、5-甲基-3-苯基-異唑-4-基、5-甲異唑-3-基、5-甲基-異唑-3-基、6-(三氟甲基)萘-3-基、6-氯基-3-吡啶基、6-氯吡啶-3-基、6-三氟甲基-3-吡啶基、苯並[b]噻吩-2-基、苯並[c]噻吩-1-基、苄基、3-丁烯基、丁烷基、環丁基、環己基、環丙基、乙烯基、氟甲基、呋喃基、異唑-5-基、甲氧基甲基、甲基丙酸-3-基、萘-1-基、苯基、苯乙基、喹啉-2-基、喹啉-2-基、第三丁基、噻吩-2-基、噻吩-2-基和三氯甲基。 Preferred examples of Q 1 include (2,6-dichlorophenyl)-methyl, (4-methoxyphenyl)-methyl, (E)-2-isobutoxyvinyl, 1-(4 -Chlorophenyl)-2-methyl-propan-1-yl, 1-(4-chlorophenyl)-5-trifluoromethyl-1H-pyrazol-4-yl, 1-(4-chlorobenzene Cyclopentyl, 1-(4-fluorophenyl)-5-methyl-1H-pyrazol-4-yl, 1-methyl-1H-benzotriazol-5-yl, 1-methyl 3-tert-butyl-1H-pyrazol-5-yl, 1-methyl-3-trifluoromethyl-4-chloro-1H-pyrazole-5-yl, 1-methylbenzotriazole -5-yl, 1-phenyl-5-propyl-1H-pyrazol-4-yl, 1-phenyl-5-trifluoromethyl-1H-pyrazol-4-yl, 1-phenylethyl , 1-tert-butyl-5-methyl-1H-imidazol-4-yl, 2,3-difluoro-phenyl, 2,4-difluoro-phenyl, 2,4,6-tri Methylphenyl, 2,4-dichlorophenyl, 2,6-dichloro-phenyl, 2,1,3-benzo Diazol-5-yl, 2,2,3,3,4,4,4-heptafluorobutane, 2,2,3,3-tetrafluoro-1-methyl-cyclobutane, 2 ,3-difluoro-phenyl, 2,4,6-trifluoro-phenyl, 2,4-difluoro-phenyl, 2,4-dimethyl-1,1,3-trioxy -2,3-dihydro-1H-1 λ * 6 * -benzo[d]isothiazol-5-yl, 2,5-dimethyl-furan-3-yl, 2,5-dimethylpyridyl Zyrid-3-yl, 2,6-dichloro-4-pyridyl, 2-chloro-3-pyridyl, 2-chloro-4-cyano-phenyl, 2-chloro-4-methylsulfonate Mercapto-phenyl, 2-chloro-6-methoxy-4-pyridyl, 2-chloro-phenyl, 2-chlorothiazol-5-yl, 2-ethylhexyl, 2-fluoro-4 -trifluoromethyl-phenyl, 2-fluoro-5-chloro-phenyl, 2-fluoro-5-trifluoromethyl-phenyl, 2-fluoro-phenyl, 2-isopropylsulfonate Phenylphenyl, 2-methoxy-phenyl, 2-methyl-4-cyano-phenyl, 2-methyl-4-fluoro-phenyl, 2-methyl-4-nitro-benzene Base, 2-methylethyl, 2-methyl-phenyl, 2-methylsulfonylethyl, 2-phenylthiazol-4-yl, 2-phenyl-thiazol-4-yl, 2-pyridyl, 2-thienylmethyl, 2-trifluoromethoxy-phenyl, 2-trifluoromethyl-4-fluorophenyl, 2-trifluoromethyl-phenyl, 3-(2-chloro-phenyl )-5-methyl-iso Zin-4-yl, 3,5-difluorophenyl, 3,5-dimethyl-iso Zin-4-yl, 3-chloro-2,2-dimethyl-propane, 3-chloro-4-(isopropylsulfonyl)-thiophen-2-yl, 3-chloro-4- Isopropyl sulfonyl-thiophen-2-yl, 3-chloro-5-trifluoromethyl-2-pyridyl, 3-chloro-benzo[b]thiophen-2-yl, 3-chlorothiophene- 2-yl, 3-chloro-thiophen-2-yl, 3-pyridyl, 3-pyridyl-N-oxide, 3-trifluoromethyl-4-fluoro-phenyl, 3-trifluorotoluene , 4-(chloromethyl)phenyl, 4-cyano-2-methyl-phenyl, 4-cyano-phenyl, 4-fluoro-2-chloro-phenyl, 4-fluorobenzyl , 4-fluoro-phenyl, 4-methyl-[1,2,3]thiadiazole, 4-methyl-[1,2,3]thiadiazolyl, 4-methyl-phenyl, 4-methanesulfonyl phenyl, 4-nitro-2-chloro-phenyl, 4-nitro-phenyl, 4-pyridyl, 4-pyridine-N-oxide, 4-tert-butylbenzene , 4-trifluoromethoxy-phenyl, 4-trifluoromethyl-phenyl, 5-chloro-1-methyl-1H-pyrazol-4-yl, 5-chloro-3-pyridine , 5-methyl-2-phenyl-2H-[1,2,3]triazol-4-yl, 5-methyl-2-trifluoromethyl-furan-3-yl, 5-methyl -3-(2-chloro-5-fluoro-phenyl)-iso Zin-4-yl, 5-methyl-3-phenyl-iso Zin-4-yl, 5-methyl Zyrid-3-yl, 5-methyl-iso Zyridin-3-yl, 6-(trifluoromethyl)naphthalen-3-yl, 6-chloro-3-pyridyl, 6-chloropyridin-3-yl, 6-trifluoromethyl-3-pyridyl , benzo[b]thiophen-2-yl, benzo[c]thiophen-1-yl, benzyl, 3-butenyl, butane, cyclobutyl, cyclohexyl, cyclopropyl, vinyl, Fluoromethyl, furyl, iso Zyrid-5-yl, methoxymethyl, methylpropion-3-yl, naphthalen-1-yl, phenyl, phenethyl, quinolin-2-yl, quin Andros-2-yl, tert-butyl, thiophen-2-yl, thiophen-2-yl and trichloromethyl.
Q1另一較佳實例包括(2,6-二氯苯基)-甲基、(4-甲氧苯基)-甲基、(E)-2-異丁氧基乙烯基、1-(4-氯苯基)-2-甲基-丙烷-1-基、1-(4-氯苯基)環戊基、1-苯乙基、2,2,3,3,4,4,4-七氟丁烷基、2,2,3,3-四氟-1-甲基-環丁烷基、2-乙基己基、2-甲基乙基、3-氯基-2,2-二甲基-丙烷基、3-三氟甲基苄基、4-氟苄基、3-丁烯基、丁烷基、環丁基、環己基、環丙基、乙烯基、氟甲基、甲氧基甲基、甲基丙酸-3-基、苯乙基、第三丁基和三氯甲基。 Another preferred example of Q 1 includes (2,6-dichlorophenyl)-methyl, (4-methoxyphenyl)-methyl, (E)-2-isobutoxyvinyl, 1-( 4-chlorophenyl)-2-methyl-propan-1-yl, 1-(4-chlorophenyl)cyclopentyl, 1-phenylethyl, 2,2,3,3,4,4,4 -heptafluorobutane, 2,2,3,3-tetrafluoro-1-methyl-cyclobutane, 2-ethylhexyl, 2-methylethyl, 3-chloro-2,2- Dimethyl-propane, 3-trifluoromethylbenzyl, 4-fluorobenzyl, 3-butenyl, butane, cyclobutyl, cyclohexyl, cyclopropyl, vinyl, fluoromethyl, Methoxymethyl, methylpropionic acid-3-yl, phenethyl, tert-butyl and trichloromethyl.
Q1另一較佳實例包括1-(4-氯苯基)-5-三氟甲基-1H-吡唑-4-基、1-(4-氟苯基)-5-甲基-1H-吡唑-4-基、1-甲基-1H-苯並三唑-5-基、1-甲基-3-第三丁基-1H-吡唑-5-基、1-甲基-3-三氟甲基-4-氯基-1H-吡唑-5-基、1-甲基苯並三唑-5-基、1-苯基-5-丙基-1H-吡唑-4-基、1-苯基-5-三氟甲基-1H-吡唑-4-基、1-第三丁基-5-甲基-1H-咪唑-4-基、2,4,6-三甲基苯基、2,4-二氯苯基、2,6-二氯基-苯基、2,1,3-苯並二唑-5- 基、2,3-二氟基-苯基、2,3-二氟基-苯基、2,4,6-三氟基-苯基、2,4-二氟基-苯基、2,4-二氟基-苯基、2,4-二甲基-1,1,3-三氧-2,3-二氫-1H-1 λ *6*-苯並[d]異噻唑-5-基、2,5-二甲基-呋喃-3-基、2,5-二甲吡唑-3-基、2,6-二氯基-4-吡啶基、2-氯基-3-吡啶基、2-氯基-4-氰基-苯基、2-氯基-4-甲磺醯基-苯基、2-氯基-6-甲氧基-4-吡啶基、2-氯基-苯基、2-氯噻唑-5-基、2-氟基-4-三氟甲基-苯基、2-氟基-5-氯基-苯基、2-氟基-5-三氟甲基-苯基、2-氟基-苯基、2-異丙磺醯苯基、2-甲氧基-苯基、2-甲基-4-氰基-苯基、2-甲基-4-氟基-苯基、2-甲基-4-硝基-苯基、2-甲基-苯基、2-甲磺醯乙基、2-苯噻唑-4-基、2-苯基-噻唑-4-基、2-吡啶基、2-噻吩甲基、2-三氟甲氧基-苯基、2-三氟甲基-4-氟苯基、2-三氟甲基-苯基、3-(2-氯基-苯基)-5-甲基-異唑-4-基、3,5-二氟苯基、3,5-二甲基-異唑-4-基、3-氯基-4-(異丙磺醯基)-噻吩-2-基、3-氯基-4-異丙磺醯基-噻吩-2-基、3-氯基-5-三氟甲基-2-吡啶基、3-氯基-苯並[b]噻吩-2-基、3-氯噻吩-2-基、3-氯基-噻吩-2-基、3-吡啶基、3-吡啶基-N-氧化物、3-三氟甲基-4-氟基-苯基、4-(氯甲基)苯基、4-氰基-2-甲基-苯基、4-氰基-苯基、4-氟基-2-氯基-苯基、4-氟基-苯基、4-甲基-[1,2,3]噻二唑、4-甲基-[1,2,3]噻二唑基、4-甲基-苯基、4-甲磺醯基苯基、4-硝基-2-氯基-苯基、4-硝基-苯基、4-吡啶基、4-吡啶-N-氧化物、4-第三丁基苯基、4-三氟甲氧基-苯基、4-三氟甲基-苯基、5-氯基-1-甲基-1H-吡唑-4-基、5-氯基-3-吡啶基、5-甲基-2-苯基-2H-[1,2,3]三唑-4-基、5-甲基-2-三 氟甲基-呋喃-3-基、5-甲基-3-(2-氯基-5-氟苯基)-異唑-4-基、5-甲基-3-苯基-異唑-4-基、5-甲基異唑-3-基、5-甲基異唑-3-基、6-(三氟甲基)萘-3-基、6-氯基-3-吡啶基、6-氯吡啶-3-基、6-三氟甲基-3-吡啶基、苯並[b]噻吩-2-基、苯並[c]噻吩-1-基、苄基、呋喃基、異唑-5-基、萘-1-基、苯基、喹啉-2-基、喹啉-2-基、噻吩-2-基和噻吩-2-基。 Another preferred example of Q 1 includes 1-(4-chlorophenyl)-5-trifluoromethyl-1H-pyrazol-4-yl, 1-(4-fluorophenyl)-5-methyl-1H -pyrazol-4-yl, 1-methyl-1H-benzotriazol-5-yl, 1-methyl-3-t-butyl-1H-pyrazole-5-yl, 1-methyl- 3-trifluoromethyl-4-chloro-1H-pyrazol-5-yl, 1-methylbenzotriazol-5-yl, 1-phenyl-5-propyl-1H-pyrazole-4 -yl, 1-phenyl-5-trifluoromethyl-1H-pyrazol-4-yl, 1-tert-butyl-5-methyl-1H-imidazol-4-yl, 2,4,6- Trimethylphenyl, 2,4-dichlorophenyl, 2,6-dichloro-phenyl, 2,1,3-benzo Azul-5-yl, 2,3-difluoro-phenyl, 2,3-difluoro-phenyl, 2,4,6-trifluoro-phenyl, 2,4-difluoro- Phenyl, 2,4-difluoro-phenyl, 2,4-dimethyl-1,1,3-trioxo-2,3-dihydro-1H-1 λ * 6 * -benzo[d Isothiazol-5-yl, 2,5-dimethyl-furan-3-yl, 2,5-dipyrazol-3-yl, 2,6-dichloro-4-pyridyl, 2- Chloro-3-pyridyl, 2-chloro-4-cyano-phenyl, 2-chloro-4-methylsulfonyl-phenyl, 2-chloro-6-methoxy-4-pyridine , 2-chloro-phenyl, 2-chlorothiazol-5-yl, 2-fluoro-4-trifluoromethyl-phenyl, 2-fluoro-5-chloro-phenyl, 2-fluoro 5--5-trifluoromethyl-phenyl, 2-fluoro-phenyl, 2-isopropylsulfonylphenyl, 2-methoxy-phenyl, 2-methyl-4-cyano-phenyl , 2-methyl-4-fluoro-phenyl, 2-methyl-4-nitro-phenyl, 2-methyl-phenyl, 2-methylsulfonylethyl, 2-phenylthiazole-4- , 2-phenyl-thiazol-4-yl, 2-pyridyl, 2-thienylmethyl, 2-trifluoromethoxy-phenyl, 2-trifluoromethyl-4-fluorophenyl, 2- Trifluoromethyl-phenyl, 3-(2-chloro-phenyl)-5-methyl-iso Zin-4-yl, 3,5-difluorophenyl, 3,5-dimethyl-iso Zin-4-yl, 3-chloro-4-(isopropylsulfonyl)-thiophen-2-yl, 3-chloro-4-isopropylsulfonyl-thiophen-2-yl, 3-chloro -5-trifluoromethyl-2-pyridyl, 3-chloro-benzo[b]thiophen-2-yl, 3-chlorothiophen-2-yl, 3-chloro-thiophen-2-yl, 3 -pyridyl, 3-pyridyl-N-oxide, 3-trifluoromethyl-4-fluoro-phenyl, 4-(chloromethyl)phenyl, 4-cyano-2-methyl-benzene Base, 4-cyano-phenyl, 4-fluoro-2-chloro-phenyl, 4-fluoro-phenyl, 4-methyl-[1,2,3]thiadiazole, 4-methyl -[1,2,3]thiadiazolyl, 4-methyl-phenyl, 4-methylsulfonylphenyl, 4-nitro-2-chloro-phenyl, 4-nitro-benzene , 4-pyridyl, 4-pyridine-N-oxide, 4-tert-butylphenyl, 4-trifluoromethoxy-phenyl, 4-trifluoromethyl-phenyl, 5-chloro 1-methyl-1H-pyrazol-4-yl, 5-chloro-3-pyridyl, 5-methyl-2-phenyl-2H-[1,2,3]triazol-4-yl , 5-methyl-2-trifluoromethyl-furan-3-yl, 5-methyl-3-(2-chloro-5-fluorophenyl)-iso Zin-4-yl, 5-methyl-3-phenyl-iso Zin-4-yl, 5-methyliso Zyrom-3-yl, 5-methyliso Zyridin-3-yl, 6-(trifluoromethyl)naphthalen-3-yl, 6-chloro-3-pyridyl, 6-chloropyridin-3-yl, 6-trifluoromethyl-3-pyridyl Benzo[b]thiophen-2-yl, benzo[c]thiophen-1-yl, benzyl, furyl, iso Zyrid-5-yl, naphthalen-1-yl, phenyl, quinolin-2-yl, quin Andros-2-yl, thiophen-2-yl and thiophen-2-yl.
Q1另一較佳實例包括苯基、5-溴呋喃-2-基、2-甲氧基苯基、2-溴苯基、2-甲基苯基、5-溴吡啶-3-基、3-甲基吡啶-2-基、2-氯基-4-氟苯基、4-甲基-1,2,3-噻二唑-5-基、3-氯基-2-氟苯基、4-硝基苯基、5-氯基-2-氟苯基、3-氯基-2-甲基苯基、1,2,3-噻二唑-4-基、2-氯基-4-硝基苯基、噻吩-2-基、2-氯基-5-硝基苯基、2-(三氟甲氧基)苯基、2氯苯基、4-(三氟甲氧基)苯基、3氯苯基、2-(三氟甲基)苯基、2-氯吡啶-3-基、4-(三氟甲基)苯基、2-氯吡啶-4-基、2-甲基-4-氰苯基、6-氯吡啶-3-基、2,4,6三氟苯基、5-氯噻吩-2-基、2,6-二氟苯基、3-氯-5-(三氟甲基)吡啶-2-基、2,6-二氟基-4-氰基苯基、4-氰基-2-氟苯基、2-氯-6-氟苯基、4-氰基苯基、2-甲基-3-硝基苯基、2-甲基-4-硝基苯基、2,5二氯苯基、3-甲基-4-硝基苯基、2,3-二氟苯基、2-氯基-4-氰基苯基、1,3-二甲基-1H-吡唑-5-基、2-氟基-4-氰基苯基、2-氟苯基、4-甲基噻吩基、4-氟苯基、1-甲基-3-(三氟甲基)吡唑-4-基、2-氟吡啶-3-基、4-吡啶基、2-氟基-3-(三氟甲基)苯基、1,3-二甲基吡唑-4-基、2-氟基-5-(三氟甲基)-苯基、4-甲基苯基、4-氟基-3-(三氟甲基)苯基、4-氟基-2-甲基苯基、呋喃-2-基 和2,4-二氟苯基、環丙基、苄基。 Another preferred example of Q 1 includes phenyl, 5-bromofuran-2-yl, 2-methoxyphenyl, 2-bromophenyl, 2-methylphenyl, 5-bromopyridin-3-yl, 3-methylpyridin-2-yl, 2-chloro-4-fluorophenyl, 4-methyl-1,2,3-thiadiazol-5-yl, 3-chloro-2-fluorophenyl 4-nitrophenyl, 5-chloro-2-fluorophenyl, 3-chloro-2-methylphenyl, 1,2,3-thiadiazol-4-yl, 2-chloro- 4-nitrophenyl, thiophen-2-yl, 2-chloro-5-nitrophenyl, 2-(trifluoromethoxy)phenyl, 2-chlorophenyl, 4-(trifluoromethoxy) Phenyl, 3-chlorophenyl, 2-(trifluoromethyl)phenyl, 2-chloropyridin-3-yl, 4-(trifluoromethyl)phenyl, 2-chloropyridin-4-yl, 2 -methyl-4-cyanophenyl, 6-chloropyridin-3-yl, 2,4,6-trifluorophenyl, 5-chlorothiophen-2-yl, 2,6-difluorophenyl, 3-chloro -5-(trifluoromethyl)pyridin-2-yl, 2,6-difluoro-4-cyanophenyl, 4-cyano-2-fluorophenyl, 2-chloro-6-fluorophenyl 4-cyanophenyl, 2-methyl-3-nitrophenyl, 2-methyl-4-nitrophenyl, 2,5-dichlorophenyl, 3-methyl-4-nitrobenzene Base, 2,3-difluorophenyl, 2-chloro-4-cyanophenyl, 1,3-dimethyl-1H-pyrazol-5-yl, 2-fluoro-4-cyanobenzene Base, 2-fluorophenyl 4-methylthienyl, 4-fluorophenyl, 1-methyl-3-(trifluoromethyl)pyrazol-4-yl, 2-fluoropyridin-3-yl, 4-pyridyl, 2-fluoro 3-(trifluoromethyl)phenyl, 1,3-dimethylpyrazol-4-yl, 2-fluoro-5-(trifluoromethyl)-phenyl, 4-methylphenyl , 4-fluoro-3-(trifluoromethyl)phenyl, 4-fluoro-2-methylphenyl, furan-2-yl and 2,4-difluorophenyl, cyclopropyl, benzyl .
在另一較佳具體實例中,Q2為式(II)的一部分,其中取代基R5、R6和R7具有以下含義:R7和R6獨立的為氫、氰基、鹵素、C1-C6烷基、C1-C6全氟烷基、C1-C6全氟烷硫基、C1-C6全氟烷基亞磺醯基或C1-C6-全氟烷基磺醯基,較佳為獨立的C1-C4全氟烷基、C1-C4全氟烷硫基、C1-C4-全氟烷基亞磺醯基或C1-C4-全氟烷基磺醯基,甚至更佳為獨立的C1-C4-全氟烷基、C1-C4-全氟烷硫基或C1-C4-全氟烷基磺醯基,最佳為獨立的三氟甲基或全氟乙基或三氟甲硫基或全氟乙硫基或三氟甲磺醯基或全氟乙磺醯基。 In another preferred embodiment, Q 2 is a moiety of formula (II) wherein the substituents R 5 , R 6 and R 7 have the following meanings: R 7 and R 6 are independently hydrogen, cyano, halogen, C 1- C 6 alkyl, C 1 -C 6 perfluoroalkyl, C 1 -C 6 perfluoroalkylthio, C 1 -C 6 perfluoroalkylsulfinyl or C 1 -C 6 -perfluoro Alkylsulfonyl, preferably independently C 1 -C 4 perfluoroalkyl, C 1 -C 4 perfluoroalkylthio, C 1 -C 4 -perfluoroalkylsulfinyl or C 1 - C 4 -perfluoroalkylsulfonyl, even more preferably independently C 1 -C 4 -perfluoroalkyl, C 1 -C 4 -perfluoroalkylthio or C 1 -C 4 -perfluoroalkyl The sulfonyl group is preferably an independently trifluoromethyl or perfluoroethyl or trifluoromethylthio group or a perfluoroethylthio group or a trifluoromethanesulfonyl group or a perfluoroethanesulfonyl group.
更佳的是,R7和R6為獨立的氰基、鹵素、C1-C6烷基、C1-C6-全氟烷基,較佳獨立的為C1-C6-全氟烷基,甚至更佳獨立的為三氟甲基或全氟乙基。 More preferably, R 7 and R 6 are independently cyano, halogen, C 1 -C 6 alkyl, C 1 -C 6 -perfluoroalkyl, preferably independently C 1 -C 6 -perfluoro Alkyl groups, even more preferably independently, are trifluoromethyl or perfluoroethyl.
甚至更佳的是,R7和R6獨立的為鹵素、C1-C6全氟烷基。 Even more preferably, R 7 and R 6 are independently halogen, C 1 -C 6 perfluoroalkyl.
最佳的是,R6為三氟甲基。 Most preferably, R 6 is a trifluoromethyl group.
最佳的是,R7為全氟乙基。 Most preferably, R 7 is a perfluoroethyl group.
較佳的是,R5為氫、C1-C6鹵烷基、C1-C6烷基、C2-C6烯基、C2-C6炔基、苯基或由一至五個可相同或相異的R10取代基取代的苯基、吡啶基或由一至五個可相同或相異的R10取代基取代的吡啶基。 Preferably, R 5 is hydrogen, C 1 -C 6 haloalkyl, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, phenyl or from one to five It may be the same or different substituents R 10 phenyl, pyridyl, or may be by one to five identical or different substituents R 10 pyridyl.
更佳的是,R5為氫、C1-C6鹵烷基、C1-C6烷基,甚至更佳的是,R5為C1-C6烷基,較佳是C1-C4烷基;在另一較佳具體實例中,Q2為式(II)的一部分,其中取 代基R5、R6和R7具有以下含義:R7和R6獨立的為氰基、鹵素、C1-C6烷基、C1-C6全氟烷基、C1-C6全氟烷硫基、C1-C6全氟烷基亞磺醯基或C1-C6-全氟烷基磺醯基;且R5是C1-C6鹵烷基或C1-C6烷基;甚至更佳的是,R5為C1-C6烷基,較佳為C1-C4烷基;在一較佳具體實例中,Q2為2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基 More preferably, R 5 is hydrogen, C 1 -C 6 haloalkyl, C 1 -C 6 alkyl, and even more preferably, R 5 is C 1 -C 6 alkyl, preferably C 1 - C 4 alkyl; in another preferred embodiment, Q 2 is a part of formula (II), wherein the substituents R 5 , R 6 and R 7 have the following meanings: R 7 and R 6 are independently cyano, Halogen, C 1 -C 6 alkyl, C 1 -C 6 perfluoroalkyl, C 1 -C 6 perfluoroalkylthio, C 1 -C 6 perfluoroalkylsulfinyl or C 1 -C 6 a perfluoroalkylsulfonyl group; and R 5 is a C 1 -C 6 haloalkyl group or a C 1 -C 6 alkyl group; even more preferably, R 5 is a C 1 -C 6 alkyl group, preferably C 1 -C 4 alkyl; in a preferred embodiment, Q 2 is 2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl
較佳具體實例(E1)在式(I)化合物中的取代基具有以下含義:R1為氫、甲基、乙基或乙醯基;R2為氫、甲基、三氟甲基或鹵素;G1為氧;Q1為芳基或雜芳基;各自選擇性地由一至五個獨立選自氰基、硝基、羥基、溴基、氯基、氟基、甲基、三氟甲基、甲氧基、三氟甲氧基、甲硫基、甲亞磺醯基、甲磺醯基和苯基的取代基取代;Q2為一個具有式(II)的部分
較佳具體實例(E5)在式(I)化合物中的取代基具有以下含義:R1為氫、甲基、乙基或乙醯基;R2為氫、甲基、三氟甲基或鹵素;G1為氧;Q1為C1-C4烷基或由一至五個R4取代的C1-C4烷基、C2-C8烯基或由一個至五個R4取代的C2-C8烯基、C2-C8炔基或由一至五個R4取代的C2-C8炔基、C3-C6環烷基或由一至五個R4取代的C3-C6環烷基,且各R4獨立的為鹵素、氰基、硝基、羥基、C1-C4烷氧基、C1-C4鹵烷氧基,或者芳基或由一至五個R3取代的芳基,或是雜環基或由一至五個R3取代的雜環基;且R3具有上下文中所賦與的意義,或較佳是R3為H或鹵素;Q2為一個具有式(II)的部分
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且其他取代基具有如在具體實例(E1)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and Oxygen, and other substituents have the meaning as in the specific example (E1)
較佳具體實例是式(I)的化合物,其中A2和A3都是CH;A1和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且更佳的是各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E1)的意義 A preferred embodiment is a compound of formula (I) wherein A 2 and A 3 are both CH; A 1 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl And methoxy, and more preferably each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and the other substituents have the meaning as in the specific example (E1)
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E1)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and other substituents Has the meaning as in the specific example (E1)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F,且A2、A3和A4是CH,或A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E1)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF, and A 2 , A 3 and A 4 are CH, or A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the meaning as in the specific example (E1)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F;A2、A3和A4是CH甲氧基,且其他取代基具有如在具體實例(E1)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH methoxy groups, and the other substituents are as specific The meaning of the instance (E1)
較佳具體實例是式(I)的化合物,其中A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E1)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have as in specific example (E1) significance
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且其他取代基具有如在具體實例(E2)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and Oxygen, and other substituents have the meaning as in the specific example (E2)
較佳具體實例是式(I)的化合物,其中A2和A3都是CH;A1和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且更佳的是各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E2)的意義 A preferred embodiment is a compound of formula (I) wherein A 2 and A 3 are both CH; A1 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl And methoxy, and more preferably each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and the other substituents have the meaning as in the specific example (E2)
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E2)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and other substituents Has the meaning as in the specific example (E2)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F,且A2、A3和A4是CH,或A1、A2和A3是CH, 且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E2)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF, and A 2 , A 3 and A 4 are CH, or A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the meaning as in the specific example (E2)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F;A2、A3和A4是CH甲氧基,且其他取代基具有如在具體實例(E2)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH methoxy groups, and the other substituents are as specific The meaning of the instance (E2)
較佳具體實例是式(I)的化合物,其中A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E2)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have as in specific example (E2) significance
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且其他取代基具有如在具體實例(E3)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and Oxygen, and other substituents have the meaning as in the specific example (E3)
較佳具體實例是式(I)的化合物,其中A2和A3都是CH;Al和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且更佳的是各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E3)的意義 A preferred embodiment is a compound of formula (I) wherein A 2 and A 3 are both CH; Al and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl And methoxy, and more preferably each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and the other substituents have the meaning as in the specific example (E3)
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E3)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and other substituents Has the meaning as in the specific example (E3)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F,且A2、A3和A4是CH,或A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E3)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF, and A 2 , A 3 and A 4 are CH, or A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the meaning as in the specific example (E3)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F;A2、A3和A4是CH甲氧基,且其他取代基具有如在具體實例(E3)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH methoxy groups, and the other substituents are as specific The meaning of the instance (E3)
較佳具體實例是式(I)的化合物,其中A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E3)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have as in specific example (E3) significance
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且其他取代基具有如在具體實例(E4)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and Oxygen, and other substituents have the meaning as in the specific example (E4)
較佳具體實例是式(I)的化合物,其中A2和A3都是CH;A1和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且更佳的是各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E4)的意義 A preferred embodiment is a compound of formula (I) wherein A 2 and A 3 are both CH; A1 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl And methoxy, and more preferably each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and the other substituents have the meaning as in the specific example (E4)
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E4)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and other substituents Has the meaning as in the specific example (E4)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F,且A2、A3和A4是CH,或A1、A2和A2是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E4)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF, and A 2 , A 3 and A 4 are CH, or A 1 , A 2 and A 2 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the meaning as in the specific example (E4)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F;A2、A3和A4是CH甲氧基,且其他取代基具 有如在具體實例(E4)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH methoxy groups, and the other substituents are as specific The meaning of the instance (E4)
較佳具體實例是式(I)的化合物,其中A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E4)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the specific example (E4) significance
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且其他取代基具有如在具體實例(E5)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and Oxygen, and other substituents have the meaning as in the specific example (E5)
較佳具體實例是式(I)的化合物,其中A2和A3都是CH;A1和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且更佳的是各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E5)的意義 A preferred embodiment is a compound of formula (I) wherein A 2 and A 3 are both CH; A 1 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl And methoxy, and more preferably each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and the other substituents have the meaning as in the specific example (E5)
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E5)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and other substituents Has the meaning as in the specific example (E5)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F,且A2、A3和A4是CH,或A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E5)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF, and A 2 , A 3 and A 4 are CH, or A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the meaning as in the specific example (E5)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F;A2、A3和A4是CH甲氧基,且其他取代基具有如在具體實例(E5)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH methoxy groups, and the other substituents are as specific The meaning of the instance (E5)
較佳具體實例是式(I)的化合物,其中A1、A2和A3是 CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E5)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have as in specific example (E5) significance
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且其他取代基具有如在具體實例(E6)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and Oxygen, and other substituents have the meaning as in the specific example (E6)
較佳具體實例是式(I)的化合物,其中A2和A3都是CH;A1和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且更佳的是各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E6)的意義 A preferred embodiment is a compound of formula (I) wherein A 2 and A 3 are both CH; A 1 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl And methoxy, and more preferably each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and the other substituents have the meaning as in the specific example (E6)
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E6)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and other substituents Has the meaning as in the specific example (E6)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F,且A2、A3和A4是CH,或A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E6)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF, and A 2 , A 3 and A 4 are CH, or A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the meaning as in the specific example (E6)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F;A2、A3和A4是CH甲氧基,且其他取代基具有如在具體實例(E6)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH methoxy groups, and the other substituents are as specific The meaning of the instance (E6)
較佳具體實例是式(I)的化合物,其中A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E6)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have as in specific example (E6) significance
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且其他取代基具有如在具體實例(E7)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and Oxygen, and other substituents have the meaning as in the specific example (E7)
較佳具體實例是式(I)的化合物,其中A2和A3都是CH;A1和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且更佳的是各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E7)的意義 A preferred embodiment is a compound of formula (I) wherein A 2 and A 3 are both CH; A 1 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl And methoxy, and more preferably each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and the other substituents have the meaning as in the specific example (E7)
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E7)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and other substituents Has the meaning as in the specific example (E7)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F,且A2、A3和A4是CH,或A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E7)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF, and A 2 , A 3 and A 4 are CH, or A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the meaning as in the specific example (E7)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F;A2、A3和A4是CH甲氧基,且其他取代基具有如在具體實例(E7)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH methoxy groups, and the other substituents are as specific The meaning of the instance (E7)
較佳具體實例是式(I)的化合物,其中A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E7)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the specific example (E7) significance
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三 氟甲基和甲氧基,且其他取代基具有如在具體實例(E8)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl and Oxygen, and other substituents have the meaning as in the specific example (E8)
較佳具體實例是式(I)的化合物,其中A2和A3都是CH;A1和A4是C-X,且各X皆獨立選自氫、鹵素、氰基、甲基、三氟甲基和甲氧基,且更佳的是各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E8)的意義 A preferred embodiment is a compound of formula (I) wherein A 2 and A 3 are both CH; A 1 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, halogen, cyano, methyl, trifluoromethyl And methoxy, and more preferably each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and the other substituents have the meaning as in the specific example (E8)
較佳具體實例是式(I)的化合物,其中A1、A2、A3和A4是C-X,且各X皆獨立選自氫、氟基、氰基和甲氧基,且其他取代基具有如在具體實例(E8)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CX, and each X is independently selected from the group consisting of hydrogen, fluoro, cyano and methoxy, and other substituents Has the meaning as in the specific example (E8)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F,且A2、A3和A4是CH,或A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E8)的意義 A preferred embodiment is a compound of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF, and A 2 , A 3 and A 4 are CH, or A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have the meaning as in the specific example (E8)
較佳具體實例是式(I)的化合物,其中A1是CH、C-CN、C-Cl或C-F;A2、A3和A4是CH甲氧基,且其他取代基具有如在具體實例(E8)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 is CH, C-CN, C-Cl or CF; A 2 , A 3 and A 4 are CH methoxy groups, and the other substituents are as specific The meaning of the instance (E8)
較佳具體實例是式(I)的化合物,其中A1、A2和A3是CH,且A4是CH、C-OCH3或C-F,且其他取代基具有如在具體實例(E8)的意義 Preferred specific examples are compounds of formula (I) wherein A 1 , A 2 and A 3 are CH, and A 4 is CH, C-OCH 3 or CF, and the other substituents have as in specific example (E8) significance
較佳具體實例(Ea)是式(I)的化合物,其中A1是C-CN,且A2、A3和A4是CH。 A preferred embodiment (Ea) is a compound of formula (I) wherein A 1 is C-CN and A 2 , A 3 and A 4 are CH.
較佳具體實例(Eb)是式(I)的化合物,其中A4是C-F,且A1、A2和A3是CH。 A preferred embodiment (Eb) is a compound of formula (I) wherein A 4 is CF and A 1 , A 2 and A 3 are CH.
較佳具體實例(Ec)是式(I)的化合物,其中A4是C-OMe,且A1、A2和A3是CH。 A preferred embodiment (Ec) is a compound of formula (I) wherein A 4 is C-OMe and A 1 , A 2 and A 3 are CH.
較佳具體實例(Ed)是式(I)的化合物,其中A1、A2、A3和A4是CH。 A preferred embodiment (Ed) is a compound of formula (I) wherein A 1 , A 2 , A 3 and A 4 are CH.
較佳具體實例(Ee)是式(I)的化合物,其中A1是C-Cl,且A2、A3和A4是CH。 A preferred embodiment (Ee) is a compound of formula (I) wherein A 1 is C-Cl and A 2 , A 3 and A 4 are CH.
較佳具體實例(Ef)是式(I)的化合物,其中A1是C-F,且A2、A3和A4是CH。 A preferred embodiment (Ef) is a compound of formula (I) wherein A 1 is CF and A 2 , A 3 and A 4 are CH.
較佳具體實例(Eg)是式(I)的化合物,其中A1是C-CF3,且A2、A3和A4是CH。 A preferred embodiment (Eg) is a compound of formula (I) wherein A 1 is C-CF 3 and A 2 , A 3 and A 4 are CH.
較佳具體實例(Eh)是式(I)的化合物,其中A4是N,A1、A2和A3是CH。 A preferred embodiment (Eh) is a compound of formula (I) wherein A 4 is N and A 1 , A 2 and A 3 are CH.
較佳具體實例(Ei)是式(I)的化合物,其中A4是N,A1是CN,A2和A3是CH。 A preferred embodiment (Ei) is a compound of formula (I) wherein A 4 is N, A 1 is CN, and A 2 and A 3 are CH.
較佳具體實例(Ej)是式(I)的化合物,其中A4是N,A1是F,A2和A3是CH。 A preferred embodiment (Ej) is a compound of formula (I) wherein A 4 is N, A 1 is F, and A 2 and A 3 are CH.
較佳具體實例(Ea1)是式(I)的化合物,其中A1是C-CN,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E1)中所賦與之意義。 A preferred embodiment (Ea1) is a compound of the formula (I) wherein A 1 is C-CN, and A 2 , A 3 and A 4 are CH, and the other substituents have the same as those given in the specific example (E1) The meaning.
較佳具體實例(Eb1)是式(I)的化合物,其中A4是C-F,且A1、A2和A3是CH,且其他取代基具有如同具體實例(E1)中所賦與之意義。 A preferred embodiment (Eb1) is a compound of formula (I) wherein A 4 is CF, and A 1 , A 2 and A 3 are CH, and the other substituents have the meaning as given in the specific example (E1) .
較佳具體實例(Ec1)是式(I)的化合物,其中A4是C-OMe,A1、A2和A3是CH,且其他取代基具有如同具體 實例(E1)中所賦與之意義。 A preferred embodiment (Ec1) is a compound of formula (I) wherein A 4 is C-OMe, A 1 , A 2 and A 3 are CH, and the other substituents are as given in specific example (E1) significance.
較佳具體實例(Ed1)是式(I)的化合物,其中A1、A2、A3和A4是CH,且其他取代基具有如同具體實例(E1)中所賦與之意義。 A preferred embodiment (Ed1) is a compound of the formula (I) wherein A 1 , A 2 , A 3 and A 4 are CH, and the other substituents have the meanings as given in the specific example (E1).
較佳具體實例(Ee1)是式(I)的化合物,其中A1是C-Cl,A2、A3和A4是CH,且其他取代基具有如同具體實例(E1)中所賦與之意義。 A preferred embodiment (Ee1) is a compound of the formula (I) wherein A 1 is C-Cl, A 2 , A 3 and A 4 are CH, and the other substituents have the same as those given in the specific example (E1) significance.
較佳具體實例(Ef1)是式(I)的化合物,其中A1是C-F,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E1)中所賦與之意義。 A preferred embodiment (Ef1) is a compound of formula (I) wherein A 1 is CF, and A 2 , A 3 and A 4 are CH, and the other substituents have the meaning as given in the specific example (E1) .
較佳具體實例(Eg1)是式(I)的化合物,其中A1是C-CF3,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E1)中所賦與之意義。 A preferred embodiment (Eg1) is a compound of the formula (I) wherein A 1 is C-CF 3 and A 2 , A 3 and A 4 are CH, and the other substituents have the same as those exemplified in the specific example (E1) With meaning.
較佳具體實例(Eh1)是式(I)的化合物,其中A4是N,A1、A2和A3是CH,且其他取代基具有如同具體實例(E1)中所賦與之意義。 A preferred embodiment (Eh1) is a compound of the formula (I) wherein A 4 is N, A 1 , A 2 and A 3 are CH, and the other substituents have the meanings as given in the specific example (E1).
較佳具體實例(Ei1)是式(I)的化合物,其中A4是N,A1是CN,A2和A3是CH,且其他取代基具有如同具體實例(E1)中所賦與之意義。 A preferred embodiment (Ei1) is a compound of the formula (I) wherein A 4 is N, A 1 is CN, A 2 and A 3 are CH, and the other substituents are as given in the specific example (E1) significance.
較佳具體實例(Ej1)是式(I)的化合物,其中A4是N,A1是F,A2和A3是CH,且其他取代基具有如同具體實例(E1)中所賦與之意義。 A preferred embodiment (Ej1) is a compound of formula (I) wherein A 4 is N, A 1 is F, A 2 and A 3 are CH, and the other substituents are as given in specific example (E1) significance.
較佳具體實例(Ea2)是式(I)的化合物,其中A1是C-CN,且A2、A3和A4是CH,且其他取代基具有如同具體 實例(E2)中所賦與之意義。 A preferred embodiment (Ea2) is a compound of formula (I) wherein A 1 is C-CN, and A 2 , A 3 and A 4 are CH, and the other substituents are as given in specific example (E2) The meaning.
較佳具體實例(Eb2)是式(I)的化合物,其中A4是C-F,且A1、A2和A3是CH,且其他取代基具有如同具體實例(E2)中所賦與之意義。 A preferred embodiment (Eb2) is a compound of formula (I) wherein A 4 is CF, and A 1 , A 2 and A 3 are CH, and the other substituents have the meaning as given in the specific example (E2) .
較佳具體實例(Ec2)是式(I)的化合物,其中A4是C-OMe,A1、A2和A3是CH,且其他取代基具有如同具體實例(E2)中所賦與之意義。 A preferred embodiment (Ec2) is a compound of formula (I) wherein A 4 is C-OMe, A 1 , A 2 and A 3 are CH, and the other substituents are as given in specific example (E2) significance.
較佳具體實例(Ed2)是式(I)的化合物,其中A1、A2、A3和A4是CH,且其他取代基具有如同具體實例(E2)中所賦與之意義。 A preferred embodiment (Ed2) is a compound of the formula (I) wherein A 1 , A 2 , A 3 and A 4 are CH, and the other substituents have the meanings as given in the specific example (E2).
較佳具體實例(Ee2)是式(I)的化合物,其中A1是C-Cl,A2、A3和A4是CH,且其他取代基具有如同具體實例(E2)中所賦與之意義。 A preferred embodiment (Ee2) is a compound of formula (I) wherein A 1 is C-Cl, A 2 , A 3 and A 4 are CH, and the other substituents are as given in specific example (E2) significance.
較佳具體實例(Ef2)是式(If)的化合物,其中A1是C-F,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E2)中所賦與之意義。 A preferred embodiment (Ef2) is a compound of the formula (If) wherein A 1 is CF, and A 2 , A 3 and A 4 are CH, and the other substituents have the meaning as given in the specific example (E2) .
較佳具體實例(Eg2)是式(I)的化合物,其中A1是C-CF3,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E2)中所賦與之意義。 A preferred embodiment (Eg2) is a compound of formula (I) wherein A 1 is C-CF 3 and A 2 , A 3 and A 4 are CH, and the other substituents have the same as those given in the specific example (E2) With meaning.
較佳具體實例(Eh2)是式(I)的化合物,其中A4是N,A1、A2和A3是CH,且其他取代基具有如同具體實例(E2)中所賦與之意義。 A preferred embodiment (Eh2) is a compound of formula (I) wherein A 4 is N, A 1 , A 2 and A 3 are CH, and the other substituents have the meanings as given in the specific example (E2).
較佳具體實例(Ei2)是式(I)的化合物,其中A4是N,A1是CN,A2和A3是CH,且其他取代基具有如同具體實例(E2) 中所賦與之意義。 A preferred embodiment (Ei2) is a compound of formula (I) wherein A 4 is N, A 1 is CN, A 2 and A 3 are CH, and the other substituents are as given in specific example (E2) significance.
較佳具體實例(Ej2)是式(I)的化合物,其中A4是N,A1是F,A2和A3是CH,且其他取代基具有如同具體實例(E2)中所賦與之意義。 A preferred embodiment (Ej2) is a compound of formula (I) wherein A 4 is N, A 1 is F, A 2 and A 3 are CH, and the other substituents are as given in specific example (E2) significance.
較佳具體實例(Ea3)是式(I)的化合物,其中A1是C-CN,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E3)中所賦與之意義。 A preferred embodiment (Ea3) is a compound of formula (I) wherein A 1 is C-CN, and A 2 , A 3 and A 4 are CH, and the other substituents are as given in the specific example (E3) The meaning.
較佳具體實例(Eb3)是式(I)的化合物,其中A4是C-F,且A1、A2和A3是CH,且其他取代基具有如同具體實例(E3)中所賦與之意義。 A preferred embodiment (Eb3) is a compound of formula (I) wherein A 4 is CF, and A 1 , A 2 and A 3 are CH, and the other substituents have the meaning as given in the specific example (E3) .
較佳具體實例(Ec3)是式(I)的化合物,其中A4是C-OMe,A1、A2和A3是CH,且其他取代基具有如同具體實例(E3)中所賦與之意義。 A preferred embodiment (Ec3) is a compound of the formula (I) wherein A 4 is C-OMe, A 1 , A 2 and A 3 are CH, and the other substituents have the same as those given in the specific example (E3) significance.
較佳具體實例(Ed33)是式(I)的化合物,其中A1、A2、A3和A4是CH,且其他取代基具有如同具體實例(E3)中所賦與之意義。 A preferred embodiment (Ed33) is a compound of the formula (I) wherein A 1 , A 2 , A 3 and A 4 are CH, and the other substituents have the meanings as given in the specific example (E3).
較佳具體實例(Ee3)是式(I)的化合物,其中A1是C-Cl,A2、A3和A4是CH,且其他取代基具有如同具體實例(E3)中所賦與之意義。 A preferred embodiment (Ee3) is a compound of the formula (I) wherein A 1 is C-Cl, A 2 , A 3 and A 4 are CH, and the other substituents have the same as those given in the specific example (E3) significance.
較佳具體實例(Ef3)是式(I)的化合物,其中A1是C-F,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E3)中所賦與之意義。 A preferred embodiment (Ef3) is a compound of formula (I) wherein A 1 is CF, and A 2 , A 3 and A 4 are CH, and the other substituents have the meaning as given in the specific example (E3) .
較佳具體實例(Eg3)是式(I)的化合物,其中A1是C-CF3,且A2、A3和A4是CH,且其他取代基具有如同具 體實例(E3)中所賦與之意義。 A preferred embodiment (Eg3) is a compound of formula (I) wherein A 1 is C-CF 3 and A 2 , A 3 and A 4 are CH, and the other substituents have the same as those given in the specific example (E3) With meaning.
較佳具體實例(Eh3)是式(I)的化合物,其中A4是N,A1、A2和A3是CH,且其他取代基具有如同具體實例(E3)中所賦與之意義。 A preferred embodiment (Eh3) is a compound of the formula (I) wherein A 4 is N, A 1 , A 2 and A 3 are CH, and the other substituents have the meanings as given in the specific example (E3).
較佳具體實例(Ei3)是式(I)的化合物,其中A4是N,A1是CN,A2和A3是CH,且其他取代基具有如同具體實例(E3)中所賦與之意義。 A preferred embodiment (Ei3) is a compound of formula (I) wherein A 4 is N, A 1 is CN, A 2 and A 3 are CH, and the other substituents are as given in specific example (E3) significance.
較佳具體實例(Ej3)是式(I)的化合物,其中A4是N,A1是F,A2和A3是CH,且其他取代基具有如同具體實例(E3)中所賦與之意義。 A preferred embodiment (Ej3) is a compound of formula (I) wherein A 4 is N, A 1 is F, A 2 and A 3 are CH, and the other substituents are as given in specific example (E3) significance.
較佳具體實例(Ea4)是式(I)的化合物,其中A1是C-CN,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E4)中所賦與之意義。 A preferred embodiment (Ea4) is a compound of formula (I) wherein A 1 is C-CN, and A 2 , A 3 and A 4 are CH, and the other substituents have the same as those given in the specific example (E4) The meaning.
較佳具體實例(Eb4)是式(I)的化合物,其中A4是C-F,且A1、A2和A3是CH,且其他取代基具有如同具體實例(E4)中所賦與之意義。 A preferred embodiment (Eb4) is a compound of formula (I) wherein A 4 is CF, and A 1 , A 2 and A 3 are CH, and the other substituents have the meaning as given in the specific example (E4) .
較佳具體實例(Ec4)是式(I)的化合物,其中A4是C-OMe,A1、A2和A3是CH,且其他取代基具有如同具體實例(E4)中所賦與之意義。 A preferred embodiment (Ec4) is a compound of the formula (I) wherein A 4 is C-OMe, A 1 , A 2 and A 3 are CH, and the other substituents have the same as those given in the specific example (E4) significance.
較佳具體實例(Ed4)是式(I)的化合物,其中A1、A2、A3和A4是CH,且其他取代基具有如同具體實例(E4)中所賦與之意義。 A preferred embodiment (Ed4) is a compound of the formula (I) wherein A 1 , A 2 , A 3 and A 4 are CH, and the other substituents have the meanings as given in the specific example (E4).
較佳具體實例(Ee4)是式(I)的化合物,其中A1是C-Cl,A2、A3和A4是CH,且其他取代基具有如同具體實例(E4) 中所賦與之意義。 A preferred embodiment (Ee4) is a compound of formula (I) wherein A 1 is C-Cl, A 2 , A 3 and A 4 are CH, and the other substituents are as given in specific example (E4) significance.
較佳具體實例(Ef4)是式(I)的化合物,其中A1是C-F,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E4)中所賦與之意義。 A preferred embodiment (Ef4) is a compound of formula (I) wherein A 1 is CF, and A 2 , A 3 and A 4 are CH, and the other substituents have the meaning as given in the specific example (E4) .
較佳具體實例(Eg4)是式(I)的化合物,其中A1是C-CF3,且A2、A3和A4是CH,且其他取代基具有如同具體實例(E4)中所賦與之意義。 A preferred embodiment (Eg4) is a compound of formula (I) wherein A 1 is C-CF 3 and A 2 , A 3 and A 4 are CH, and the other substituents have the same as those given in the specific example (E4) With meaning.
較佳具體實例(Eh4)是式(I)的化合物,其中A4是N,A1、A2和A3是CH,且其他取代基具有如同具體實例(E4)中所賦與之意義。 A preferred embodiment (Eh4) is a compound of formula (I) wherein A 4 is N, A 1 , A 2 and A 3 are CH, and the other substituents have the meanings as given in the specific example (E4).
較佳具體實例(Ei4)是式(I)的化合物,其中A4是N,A1是CN,A2和A3是CH,且其他取代基具有如同具體實例(E4)中所賦與之意義。 A preferred embodiment (Ei4) is a compound of formula (I) wherein A 4 is N, A 1 is CN, A 2 and A 3 are CH, and the other substituents are as given in specific example (E4) significance.
較佳具體實例(Ej4)是式(I)的化合物,其中A4是N,A1是F,A2和A3是CH,且其他取代基具有如同具體實例(E4)中所賦與之意義。 A preferred embodiment (Ej4) is a compound of formula (I) wherein A 4 is N, A 1 is F, A 2 and A 3 are CH, and the other substituents are as given in specific example (E4) significance.
式(III)的中間體化合物形成本發明的另一態樣
其中A1、A2、A3、A4、R2和Q2係如關於式(I)之定義;或其鹽類。A1、A2、A3、A4、R2和Q2較佳與式(I)化合物相應的取代基之較佳情況相同。 Wherein A 1 , A 2 , A 3 , A 4 , R 2 and Q 2 are as defined for formula (I); or a salt thereof. A 1 , A 2 , A 3 , A 4 , R 2 and Q 2 are preferably the same as those of the corresponding substituents of the compound of the formula (I).
式(IIIb)的中間體化合物形成本發明的另一態樣
其中A1、A2、A3、A4、R2和Q2係如關於式(I)之定義;或其鹽類。A1、A2、A3、A4、R2和Q2較佳與式(I)化合物相應的取代基之較佳情況相同。 Wherein A 1 , A 2 , A 3 , A 4 , R 2 and Q 2 are as defined for formula (I); or a salt thereof. A 1 , A 2 , A 3 , A 4 , R 2 and Q 2 are preferably the same as those of the corresponding substituents of the compound of the formula (I).
在一較佳具體實例中,本發明提供式(III)的化合物,其中A1、A2、A3和A4是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(III)的化合物,其中A1是C-CN;A2、A3和A4是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(III)的化合物,其中A1是C-F;A2、A3和A4是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(III)的化合物,其中A1是C-Cl;A2、A3和A4是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(III)的化合物,其中A4是C-F;A2、A3和A1是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(III)的化合物,其中A4是C-OMe;A2、A3和A1是CH;R2是氫;Q2是式 (II)的一部分;在另一較佳具體實例中,本發明提供式(III)的化合物,其中A4是N;A2、A3和A1是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(III)的化合物,其中A4是N;A1是CN,A2和A3是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(III)的化合物,其中A4是N;A1是F,A2和A3是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A1是C-CF3;A2、A3和A4是CH;R2是氫;Q2是式(II)的一部分;在一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A1、A2、A3和A4是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A1是C-CN;A2、A3和A4是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A1是C-F;A2、A3和A4是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A1是C-Cl;A2、A3和A4是CH;R2是氫;Q2是 式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A4是C-F;A2、A3和A1是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A4是C-OMe;A2、A3和A1是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A4是N;A2、A3和A1是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A4是N;A1是CN,A2和A3是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A4是N;A1是F,A2和A3是CH;R2是氫;Q2是式(II)的一部分;在另一較佳具體實例中,本發明提供式(IIIb)的化合物,其中A1是C-CF3;A2、A3和A4是CH;R2是氫;Q2是式(II)的一部分; In a preferred embodiment, the invention provides a compound of formula (III) wherein A 1 , A 2 , A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is part of formula (II); In a preferred embodiment, the invention provides a compound of formula (III) wherein A 1 is C-CN; A 2 , A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is part of formula (II) In another preferred embodiment, the invention provides a compound of formula (III) wherein A 1 is CF; A 2 , A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is formula (II) In a further preferred embodiment, the invention provides a compound of formula (III) wherein A 1 is C-Cl; A 2 , A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is formula ( Part of II); in another preferred embodiment, the invention provides a compound of formula (III) wherein A 4 is CF; A 2 , A 3 and A 1 are CH; R 2 is hydrogen; Q 2 is a formula a portion of (II); in another preferred embodiment, the invention provides a compound of formula (III), wherein A 4 is C-OMe; A 2 , A 3 and A 1 are CH; R 2 is hydrogen; 2 is a part of formula (II); in another preferred embodiment, the invention provides a compound of formula (III), wherein A 4 is N; 2 , A 3 and A 1 are CH; R 2 is hydrogen; Q 2 is a part of formula (II); in another preferred embodiment, the invention provides a compound of formula (III), wherein A 4 is N; A 1 is CN, A 2 and A 3 are CH; R 2 is hydrogen; Q 2 is a part of formula (II); in another preferred embodiment, the invention provides a compound of formula (III), wherein A 4 Is N; A 1 is F, A 2 and A 3 are CH; R 2 is hydrogen; Q 2 is a part of formula (II); in another preferred embodiment, the invention provides a compound of formula (IIIb), Wherein A 1 is C-CF3; A 2 , A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is a part of formula (II); in a preferred embodiment, the invention provides formula (IIIb) a compound wherein A 1 , A 2 , A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is a part of formula (II); in another preferred embodiment, the invention provides a compound of formula (IIIb) Wherein A 1 is C-CN; A 2 , A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is a part of formula (II); and in another preferred embodiment, the invention provides formula (IIIb) a compound wherein A 1 is CF; A 2 , A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is a part of formula (II); In one embodiment, the invention provides a compound of formula (IIIb) wherein A 1 is C-Cl; A 2 , A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is part of formula (II); In a preferred embodiment, the invention provides a compound of formula (IIIb) wherein A 4 is CF; A 2 , A 3 and A 1 are CH; R 2 is hydrogen; Q 2 is part of formula (II); In another preferred embodiment, the invention provides a compound of formula (IIIb) wherein A 4 is C-OMe; A 2 , A 3 and A 1 are CH; R 2 is hydrogen; Q 2 is formula (II) In a further preferred embodiment, the invention provides a compound of formula (IIIb) wherein A 4 is N; A 2 , A 3 and A 1 are CH; R 2 is hydrogen; Q 2 is formula (II) a portion; in another preferred embodiment, the invention provides a compound of formula (IIIb) wherein A 4 is N; A 1 is CN, A 2 and A 3 are CH; R 2 is hydrogen; Q 2 is a portion of (II); in another preferred embodiment, the invention provides a compound of formula (IIIb) wherein A 4 is N; A 1 is F, A 2 and A 3 are CH; R 2 is hydrogen; 2 is a part of formula (II); and in another preferred embodiment, the present invention provides a compound of formula (IIIb), wherein a 1 is C-CF3 A 2, A 3 and A 4 are CH; R 2 is hydrogen; Q 2 is a part of formula (II); and
表1: Table 1:
根據式(I),表1提供式(Ia)的47種化合物,其中A1是C-CN,A2、A3和A4是C-H,且Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1則具有表1所列 的值。 According to formula (I), Table 1 provides 47 compounds of formula (Ia) wherein A 1 is C-CN, A 2 , A 3 and A 4 are CH, and Q 2 is 2-methyl-5-pentafluoro Ethyl-4-trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in Table 1.
表2: Table 2:
根據式(I),表2提供式(Ib)的47種化合物,其中A4是C-F,A1、A2和A3是C-H,且Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1則具有表1所列的值。 According to formula (I), Table 2 provides 47 compounds of formula (Ib) wherein A 4 is CF, A 1 , A 2 and A 3 are CH, and Q 2 is 2-methyl-5-pentafluoroethyl -4-Trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in Table 1.
表3: table 3:
根據式(I),表3提供式(Ic)的47種化合物,其中A4是C-OMe,A1、A2和A3是C-H,且Q2是2-甲基-5-五氟乙基 -4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1則具有表1所列的值。 According to formula (I), Table 3 provides 47 compounds of formula (Ic) wherein A 4 is C-OMe, A 1 , A 2 and A 3 are CH, and Q 2 is 2-methyl-5-pentafluoro Ethyl-4-trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in Table 1.
表4: Table 4:
根據式(I),表4提供式(Id)的47種化合物,其中A1、A2、A3和A4是C-H,且Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1具有以下表中所列的值。 According to formula (I), Table 4 provides 47 compounds of formula (Id) wherein A 1 , A 2 , A 3 and A 4 are CH and Q 2 is 2-methyl-5-pentafluoroethyl-4 -Trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in the following table.
表5: table 5:
根據式(I),表5提供式(Ie)的47種化合物,其中A1是C-Cl,A2、A3和A4是C-H,且Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1則具有表1所列的值。 According to formula (I), Table 5 provides 47 compounds of formula (Ie) wherein A 1 is C-Cl, A 2 , A 3 and A 4 are CH, and Q 2 is 2-methyl-5-pentafluoro Ethyl-4-trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in Table 1.
表6: Table 6:
根據式(I),表6提供式(If)的47種化合物,其中A1是C-F,A2、A3和A4是C-H,且Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1則具有表1所列的值。 According to formula (I), Table 6 provides 47 compounds of formula (If) wherein A 1 is CF, A 2 , A 3 and A 4 are CH, and Q 2 is 2-methyl-5-pentafluoroethyl -4-Trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in Table 1.
表7: Table 7:
根據式(I),表7提供的式(Ig)的47種化合物,其中A1是C-CF3,A2、A3和A4是C-H,且Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1則具有表1 所列的值。 According to formula (I), there are 47 compounds of formula (Ig) provided in Table 7, wherein A 1 is C-CF 3 , A 2 , A 3 and A 4 are CH, and Q 2 is 2-methyl-5- Pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in Table 1.
表8: Table 8:
根據式(I),表8提供式(Ih)的47種化合物,其中A4是N,A1、A2和A3是C-H,且Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1則具有表1所列的值。 According to formula (I), Table 8 provides 47 compounds of formula (Ih) wherein A 4 is N, A 1 , A 2 and A 3 are CH, and Q 2 is 2-methyl-5-pentafluoroethyl -4-Trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in Table 1.
表9: Table 9:
根據式(I),表9提供式(Ii)的47種化合物,其中A4是N,A1是CN,A2和A3是C-H,且Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1則具有表1所列的值。 According to formula (I), Table 9 provides 47 compounds of formula (Ii) wherein A 4 is N, A 1 is CN, A 2 and A 3 are CH, and Q 2 is 2-methyl-5-pentafluoro Ethyl-4-trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in Table 1.
表10: Table 10:
根據式(I),表10提供式(Ij)的47種化合物,其中A4是N,A1是F,A2和A3是C-H,且Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且Q1則具有表1所列的值。 According to formula (I), Table 10 provides 47 compounds of formula (Ij) wherein A 4 is N, A 1 is F, A 2 and A 3 are CH, and Q 2 is 2-methyl-5-pentafluoro Ethyl-4-trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and Q 1 has the values listed in Table 1.
表11: Table 11:
表11提供式(IIIb)的9種化合物,其中Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且A1、A2、A3和A4則具有下表中所列的值。 Table 11 provides nine compounds of formula (IIIb) wherein Q 2 is 2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and A 1 , A 2 , A 3 and A 4 have the values listed in the table below.
表12: Table 12:
表12提供式(III)的9種化合物,其中Q2是2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基,R2是H,且A1、A2、A3和A4則具有下表中所列的值。 Table 12 provides nine compounds of formula (III) wherein Q 2 is 2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl, R 2 is H, and A 1 , A 2 , A 3 and A 4 have the values listed in the table below.
本發明之化合物可藉由下列方法製造。 The compound of the present invention can be produced by the following method.
(1)式(I)的化合物(其中G1是氧)可在銅或銅催化劑(如硫酸銅或碘化亞銅)存在下,及視需要在如N-乙基二異丙胺之鹼存在下,於溶劑或溶劑混合物(如第三丁醇、水)存在下,藉由使式(V)化合物與疊氮衍生物(Q2-N3)反應而製備。在Cu(II)催化劑的情況下,可使用如抗壞血酸鈉的還原劑。在Cu(0)催化劑的情況下,可使用如胺鹽的氧化劑。(範例請參閱:《Angewandte Chemie,International Edition》(德國應用化學國際版),2009年,第48卷第27期,頁4900-4908與引用的參考資料;《Angewandte Chemie,International Edition》,2008年,第47卷,頁2182-2184和參考文獻引證;《Chem.Eur.J.》(歐洲化學期刊),2006年,頁51-68與引用的參考資料。 (1) A compound of formula (I) wherein G 1 is oxygen may be present in the presence of a copper or copper catalyst such as copper sulfate or cuprous iodide, and optionally in a base such as N-ethyldiisopropylamine. It is prepared by reacting a compound of the formula (V) with an azide derivative (Q 2 -N 3 ) in the presence of a solvent or a solvent mixture such as tert-butanol or water. In the case of a Cu(II) catalyst, a reducing agent such as sodium ascorbate can be used. In the case of a Cu(0) catalyst, an oxidizing agent such as an amine salt can be used. (See, for example, Angewandte Chemie, International Edition, 2009, Vol. 48, No. 27, pp. 4900-4908 and references cited; Angewandte Chemie, International Edition, 2008 , vol. 47, pp. 2182-2184 and references cited; Chem. Eur. J. (European Chemical Journal), 2006, pp. 51-68 and references cited.
(2)式(V)的化合物(其中G1是氧)可在如DCC(N,N'-二環己基碳二亞胺)、EDC(1乙基-3-[3-二甲基胺基-丙基]碳二亞 胺鹽酸鹽)或BOP-Cl(雙(2-側氧基-3-唑啶基)膦醯氯)之偶合試劑的存在下,在如吡啶、三乙胺、4-(二甲胺基)吡啶或二異丙基乙基胺等鹼的存在下,以及視需要在如羥基苯並三唑等親核性催化劑的存在下,藉由以式(IV)的化合物(其中R是OH)使式(VI)化合物醯化而製備。視需要地,當R是Cl時,該醯化反應可在鹼性條件下(例如存在吡啶、三乙胺、4-(二甲胺基)-吡啶或二異丙基乙基胺),再次視需要在親核性催化劑存在下進行。或者,亦可在含有機溶劑(較佳為乙酸乙酯)及水性溶劑(較佳為碳酸氫鈉溶液)的二相系統中進行此類反應。視需要地,當R為C1-C6烷氧基時,可藉由將酯類(IV)與胺類(VI)一起加熱來製備醯胺。 (2) A compound of the formula (V) wherein G 1 is oxygen may be, for example, DCC (N,N'-dicyclohexylcarbodiimide), EDC (1 ethyl-3-[3-dimethylamine) Propyl-propyl]carbodiimide hydrochloride) or BOP-Cl (bis(2-trioxy-3-) In the presence of a coupling reagent such as pyridine, triethylamine, 4-(dimethylamino)pyridine or diisopropylethylamine, and optionally in the presence of a coupling reagent such as pyridyl)phosphine chloride It is prepared by deuteration of a compound of formula (VI) by a compound of formula (IV) wherein R is OH in the presence of a nucleophilic catalyst such as hydroxybenzotriazole. Optionally, when R is Cl, the deuteration reaction can be carried out under basic conditions (for example, in the presence of pyridine, triethylamine, 4-(dimethylamino)-pyridine or diisopropylethylamine), again It is carried out in the presence of a nucleophilic catalyst as needed. Alternatively, such a reaction can be carried out in a two-phase system containing an organic solvent (preferably ethyl acetate) and an aqueous solvent (preferably sodium hydrogencarbonate solution). Optionally, when R is a C 1 -C 6 alkoxy group, the decylamine can be prepared by heating the ester (IV) together with the amine (VI).
(3)式(VI)的化合物(其中R1是C1-C6烷基)可藉由還原胺化反應(使用醛或酮及如硼氫氰化鈉的還原劑與胺反應),從式(VI)的化合物(其中R1是H)製備。或者,烷化作用也可藉由,視需要在鹼的存在下,以如鹵烷之烷化劑處理胺類而達成。 (3) A compound of the formula (VI) wherein R 1 is a C 1 -C 6 alkyl group can be reacted by a reductive amination reaction (using an aldehyde or a ketone and a reducing agent such as sodium borohydride to react with an amine) The compound of formula (VI) wherein R 1 is H is prepared. Alternatively, alkylation can also be achieved by treating the amine with an alkylating agent such as a halogenated alkane in the presence of a base, if desired.
(4)式(I)的化合物(其中G1是氧)也可藉由使式(III)的化合物與如第(2)項中所描述的式(IV)之化合物反應而製備。 (4) A compound of the formula (I) wherein G 1 is oxygen can also be produced by reacting a compound of the formula (III) with a compound of the formula (IV) as described in the item (2).
(5)式(III)的化合物可利用如(1)中所描述的相同條件從 式(VI)的化合物製備。 (5) The compound of the formula (III) can be obtained from the same conditions as described in (1) Preparation of a compound of formula (VI).
(6)式(VI)的化合物(其中R1是H)可藉由還原式(VIII)的硝基化合物而製備,例如在酸性環境下以氯化錫處理或藉由金屬(例如鐵)催化的氫化作用。 (6) A compound of the formula (VI) wherein R 1 is H can be produced by reducing a nitro compound of the formula (VIII), for example, by treatment with tin chloride in an acidic environment or by a metal (for example, iron). Hydrogenation.
(7)式(III)的化合物(其中R1是H)可藉由第(6)項所述方法,藉由還原式(IIIb)的硝基化合物而製備。 (7) A compound of the formula (III) wherein R 1 is H can be produced by reducing the nitro compound of the formula (IIIb) by the method described in the item (6).
(8)式(IIIb)的化合物可從式(VIII)的化合物,藉由與疊氮衍生物Q2-N3反應而製備,其係利用第(1)項中所述的相同條件。 (8) A compound of the formula (IIIb) can be produced from a compound of the formula (VIII) by reacting with an azide derivative Q 2 -N 3 using the same conditions as described in the item (1).
(9)式(I)的化合物(其中G1為硫)可藉由將式(I)的化合物(其中的G1為氧),以一種如Lawesson試劑或五硫化二磷此類的硫轉移試劑處理製備。 (9) A compound of the formula (I) wherein G 1 is sulfur can be prepared by treating a compound of the formula (I) wherein G 1 is oxygen, by a sulfur transfer reagent such as Lawesson's reagent or phosphorus pentasulfide. .
(10)式(III)的化合物可從式(VI)的化合物(其中P是 適合的保護基)製備,其係利用第(1)項中所述的相同條件,,,然後在標準條件下移除保護基P。 (10) A compound of formula (III) can be obtained from a compound of formula (VI) wherein P is A suitable protecting group is prepared by the same conditions as described in item (1), and then the protecting group P is removed under standard conditions.
(11)式(VIII)的化合物可從式(IX)的化合物(其中A1、A2、A3和A4各自獨立為C-LG或C-H,且LG是脫離基,例如氟或氯),藉由與如脂族醇和氰化鈉的親核試劑反應而製備。 (11) A compound of the formula (VIII) may be a compound of the formula (IX) wherein A 1 , A 2 , A 3 and A 4 are each independently C-LG or CH, and LG is a leaving group such as fluorine or chlorine. Prepared by reaction with a nucleophile such as an aliphatic alcohol and sodium cyanide.
(12)式(IIIb)的化合物(其中A1、A2、A3和A4如同對式(I)的化合物之描述),可從式(IIIb)的化合物(其中A1、A2、A3和A4各自獨立為C-LG或C-H,且LG是脫離基,例如氟或氯),藉由與如脂族醇和氰化鈉的親核劑反應而製備。 (12) a compound of the formula (IIIb) (wherein A 1 , A 2 , A 3 and A 4 are as described for the compound of the formula (I)), which may be a compound of the formula (IIIb) (wherein A 1 , A 2 , A 3 and A 4 are each independently C-LG or CH, and LG is a leaving group such as fluorine or chlorine), which is prepared by reaction with a nucleophile such as an aliphatic alcohol and sodium cyanide.
14)式(VII)的化合物(其中Q2如同對式(I)的化合物之描述),也可藉由使式(I1)的化合物與亞硝酸鈉反應,之後加入疊氮化鈉而製備。範例請參閱:《Diazo Chemistry I:Aromatic and Heteroaromatic Compounds》(重氮基化學I:芳香和雜芳族化合物)。Zollinger,H.德國(1994年),380頁。出版公司:(VCH,Weinheim,德國)與引用的參考資料。 14) A compound of the formula (VII) wherein Q 2 is as described for the compound of the formula (I) can also be produced by reacting a compound of the formula (I1) with sodium nitrite, followed by sodium azide. See, for example, "Diazo Chemistry I: Aromatic and Heteroaromatic Compounds" (diazo-based chemistry I: aromatic and heteroaromatic compounds) . Zollinger, H. Germany (1994), 380 pages. Publishing company: (VCH, Weinheim, Germany) with referenced references.
15)式(II)的化合物(其中R5是甲基,R7是全氟乙基,且R6是三氟甲基),可從式(IIa)的化合物(其中LG是鹵素),如氟化物或氯化物,藉由與如疊氮化鈉的疊氮鹽類反應而製成。 15) a compound of formula (II) wherein R 5 is methyl, R 7 is perfluoroethyl, and R 6 is trifluoromethyl, which may be from a compound of formula (IIa) wherein LG is a halogen, such as fluoride or Chloride is prepared by reaction with an azide salt such as sodium azide.
16)或者,式(NH2Q2)的化合物不是已知就是可按照熟習此項技術者已知的方法製成。 16) Alternatively, the compound of formula (NH2Q2) is not known or can be prepared by methods known to those skilled in the art.
17)式(VIII)和(VI)的化合物不是已知就是可按照熟習此項技術者已知的方法製成。 17) The compounds of formula (VIII) and (VI) are not known or can be made by methods known to those skilled in the art.
具有式(I)的化合物可用於對抗和控制蟲害的侵擾,如鳞翅目(Lepidoptera)、雙翅目(Diptera)、半翅目(Hemiptera)、纓翅目(Thysanoptera)、直翅目(Orthoptera)、網翅目(Dictyoptera)、鞘翅目(Coleoptera)、蚤目(Siphonaptera)、膜翅目(Hymenoptera)和等翅目(Isoptera)等有害生物,以及其他的無脊椎有害生物,例如蟎、線蟲及軟體動物有害生物等。以下將昆蟲、蟎、線蟲及軟體動物有害生物統稱為有害生物。這些可利用本化合物發明對抗和控制的有害生物包括:涉及農業(涵意包括種植有關食物和纖維性產品的作物)、園藝、畜牧、寵物、林業與植蔬原料產品(例如水果、縠物及木材)之儲藏者;涉及毀損人造結構和傳播人畜疾病者;以及騷擾性有害生物(例如蒼蠅)。 Compounds of formula (I) are useful for combating and controlling pest infestation, such as Lepidoptera, Diptera, Hemiptera, Thysanoptera, Orthoptera ), pests such as Dictyoptera, Coleoptera, Siphonaptera, Hymenoptera, and Isoptera, and other invertebrate pests such as ticks and nematodes And mollusc pests, etc. Insects, mites, nematodes, and mollusc pests are collectively referred to as pests. These pests that can be used to combat and control using this compound include: agriculture (which includes crops for growing food and fiber products), horticulture, livestock, pets, forestry and vegetable raw materials (eg fruits, booties and A warehousing of wood; involved in the destruction of man-made structures and the spread of human and animal diseases; and harassing pests (such as flies).
具式(I)的化合物可控制之有害生物種類實例包括:桃蚜(Myzus persicae)、棉蚜(Aphis gossypii)、黑豆蚜(Aphis fabae)、盲蝽種(Lygus spp.)、盲蝽種(Dysdercus spp.)、蠟蟬(Nilaparvata lugens)、葉蟬(Nephotettixc incticeps)、稻綠蝽屬(Nezara spp.)、蝽象種(Euschistus spp.)、蛛緣蝽象種(Leptocorisa spp.)、西方花薊馬(Frankliniella occidentalis)、薊馬種(Thrips spp.)、科羅拉多馬鈴薯甲蟲(Leptinotarsa decemlineata)、棉鈴象鼻蟲(Anthonomus grandis)、介殼蟲種(Aonidiella spp.)、粉虱種(Trialeurodes spp.)、粉虱(Bemisia tabaci)、歐洲玉米螟(Ostrinia nubilalis)、棉樹葉蟲(Spodoptera littoralis)、菸夜蛾(Heliothis virescens)、棉鈴蟲(Helicoverpa armigera)、棉鈴蟲(Helicoverpa zea)、棉卷葉螟(Sylepta derogata)、粉蝶(Pieris brassicae)、小菜蛾(Plutella xylostella)、夜盜蟲(Agrotis spp.)、稻條螟(Chilo suppressalis)、飛蝗(Locusta migratoria)、蝗蟲(Chortiocetes terminifera)、根蟲種(Diabrotica spp.)、歐洲葉蟎(Panonychus ulmi)、柑桔葉蟎(Panonychus citri)、二點葉蟎(Tetranychus urticae)、赤葉蟎(Tetranychus cinnabarinus)、柑桔銹蟎(Phyllocoptruta oleivora)、茶細蟎(Polyphagotarsonemus latus)、葡萄短須蟎種(Brevipalpus spp.)、牛蜱(Boophilus microplus)、美國犬壁虱(Dermacentor variabilis)、貓蚤(Ctenocephalides felis)、潛葉蟲種(Liriomyza spp.)、家蠅(Musca domestica)、埃及斑蚊(Aedes aegypti)、瘧蚊屬(Anopheles spp.)、家蚊屬(Culex spp.)、綠蠅種(Lucillia spp.)德國蟑螂(Blattella germanica)、美國蟑螂(Periplaneta americana)、東方蟑螂(Blatta orientalis)、澳白蟻科的白蟻(例如澳白蟻種(Mastotermes spp.))、木白蟻科的白蟻(例如新白蟻種(Neotermes spp.))、鼻白蟻科的白蟻(例如家白蟻(Coptotermes formosanus)、黃肢散白蟻(Reticulitermes flavipes)、R.speratu、R.virginicus、R.hesperus和R.santonensis),以及白蟻科的白蟻(例如黃球白蟻 (Globitermes sulfureus))、火蟻(Solenopsis geminata)、法老家蟻(Monomorium pharaonis)、毛虱種(Damalinia spp.)及咬虱與吸吮虱種(Linognathus spp.)、根瘤線蟲種(Meloidogyne spp.)、黃金線蟲種(Globodera spp.)及胞囊線蟲種(Heterodera spp.)、根腐線蟲種(Pratylenchus spp.)、香蕉穿孔線蟲種(Rhodopholus spp.)、柑橘線蟲種(Tylenchulus spp.)、撚轉胃蟲(Haemonchus contortus)、醋線蟲(Caenorhabditis elegans)、消化道線蟲種(Trichostrongylus spp.)及蛞蝓(Deroceras reticulatum)。 Examples of pest species that can be controlled by compounds of formula (I) include: Myzus persicae , Aphis gossypii , Aphis fabae , Lygus spp., and blind mites ( Dysdercus spp.), Nilaparvata lugens , Nephotettixc incticeps , Nezara spp., Euschistus spp., Leptocorisa spp., Western Frankliniella occidentalis , Thrips spp., Leptinotarsa decemlineata , Anthonomus grandis , Aonidiella spp., Trialeurodes spp. ), Bemisia tabaci , Ostrinia nubilalis , Spodoptera littoralis , Heliothis virescens , Helicoverpa armigera , Helicoverpa zea , cotton leaf Sylepta derogata , Pieris brassicae , Plutella xylostella , Agrotis spp., Chilo suppressalis , Locusta migratoria , Chortiocetes terminifera , Diabrotica spp., Panonychus ulmi , Panonychus citri , Tetranychus urticae , Tetranychus cinnabarinus , mandarin Phyllocoptruta oleivora , Polyphagotarsonemus latus , Brevipalpus spp., Boophilus microplus , Dermacentor variabilis , Ctenocephalides felis , Liriomyza spp., Musca domestica , Aedes aegypti , Anopheles spp., Culex spp., Lucillia spp. ) German cockroach ( Blattella germanica ), American cockroach ( Periplaneta americana ), Oriental cockroach ( Blatta orientalis ), termites of the family Ants (such as Mastotermes spp.), termites of the wood termite family (eg new termite species ( Neotermes spp.)), termites of the family Termidae (eg Coptotermes formosanus , Reticulitermes flavipes , R. speratu , R. virginicus , R .hesperus and R. santonensis ), and termites of the termite family (eg, Globitermes sulfureus ), fire ants ( Solenopsis geminata ), primordial ants ( Monmorium pharaonis ), mites ( Dalalinia spp.) and biting Linognathus spp., Meloidogyne spp., Globodera spp. and Heterodera spp., root rot nematode ( Pratylushus spp.), banana perforated nematode Species ( Rhoodopholus spp.), Tylenchulus spp., Haemonchus contortus , Caenorhabditis elegans , Trichostrongylus spp., and Deroceras reticulatum .
因此,本發明提供一種對抗和控制昆蟲、蟎、線蟲或軟體動物的方法,其包含將殺蟲、殺蟎、殺線蟲或殺軟體動物有效量的式(I)化合物,或含有式(I)化合物的組成物,施於有害生物、其所在之處(最好是植物)或容易受有害生物侵害的植物或植物繁殖物質上。具有式(I)的化合物較佳可用於對抗昆蟲、蟎或線蟲。 Accordingly, the present invention provides a method of combating and controlling insects, mites, nematodes or molluscs comprising an effective amount of a compound of formula (I), or a formula (I), which is insecticidal, acaricidal, nematicidal or molluscicidal. A composition of a compound applied to a pest, where it is (preferably a plant) or a plant or plant propagation material that is susceptible to pests. The compounds of formula (I) are preferably used against insects, mites or nematodes.
蟎,例如棉紅蜘蛛(Tetranychus cinnabarinus)、二點葉蹣(Tetranychus urticae)、柑橘葉蹣(Panonychus citri)、柑橘鏽壁虱(Aculops pelekassi)、跗線蟎屬(Tarsonemus spp.)。 螨, such as cotton red spider ( Tetranychus cinnabarinus ), Tetranychus urticae , Panonychus citri , Aculops pelekassi , Tarsonemus spp.
線蟲,例如根瘤線蟲(Meloidogyne incognita)、松材線蟲(Bursaphelenchus lignicolus Mamiya et Kiyohara)、葉芽線蟲(Aphelenchoides besseyi)、大豆胞囊線蟲(Heterodera glycines)、根腐線蟲(Pratylenchus spp.)等線蟲。 Nematodes, such as Meloidogyne incognita , Bursaphelenchus lignicolus Mamiya et Kiyohara , Aphelenchoides besseyi , Heterodera glycines , and Pratylenchus spp.
此外,這些化合物亦可用於控制動物有害生物,特別是農業、園藝、獸醫場所、森林、花園及休閒設施、保護 儲藏的產品與物資及衛生場所出現昆蟲、蛛形綱動物、蠕蟲、線蟲及軟體動物。其可作為植物保護劑。它們可有效於對抗通常敏感和耐藥性物種及對抗所有或部分生長階段。 In addition, these compounds can also be used to control animal pests, especially in agriculture, horticulture, veterinary establishments, forests, gardens and leisure facilities, and protection. Insects, arachnids, worms, nematodes and mollusks appear in stored products and materials and in sanitary settings. It can be used as a plant protection agent. They are effective against common sensitive and resistant species and against all or part of the growth phase.
這些有害生物尤其包括: These pests include, inter alia:
屬虱目(Anoplura(Phthiraptera))者,例如毛虱種(Damalinia spp.)、血虱種(Haematopinus spp.)、長顎虱種(Linognathus spp.)、虱種(Pediculus spp.)、嚙毛虱屬(Trichodectes spp.)。 Of the order Anoplura ( Phthiraptera ), such as the genus Damalinia spp., Haematopinus spp., Linognathus spp., Pediculus spp., Pteridium ( Trichodectes spp.).
屬蛛形綱(Arachnida)者,例如粗腳粉蟎(Acarus siro)、橘蚜癭蟎(Aceria sheldoni)、刺皮節蜱種(Aculops spp.)、刺節蜱種(Aculus spp.)、鈍眼蜱屬(Amblyomma spp.)、銳緣蜱屬(Argas spp.)、牛蜱屬(Boophilus spp.)、葡萄短須蟎種(Brevipalpus spp.)、苜蓿紅蜘蛛(Bryobia praetiosa)、皮蟎種(Chorioptes spp.)、雞皮剌蟎(Dermanyssus gallinae)、葉蟎種(Eotetranychus spp.)、梨上癭蟎(Epitrimerus pyri)、葉蟎種(Eutetranychus spp.)、鏽蜱種(Eriophyes spp.)、塵蟎種(Hemitarsonemus spp.)、璃眼蜱屬(Hyalomma spp.)、硬蜱屬(Ixodes spp.)、黑寡婦蜘蛛(Latrodectus mactans)、Metatetranychus spp.、葉蟎種(Oligonychus spp.)、鈍緣蜱種(Ornithodoros spp.)、葉蟎種(Panonychus spp.)、柑桔銹蟎(Phyllocoptruta oleivora)、茶細蟎(Polyphagotarsonemus latus)、癢蟎屬(Psoroptes spp.)、扇頭蜱種(Rhipicephalus spp.)、根蟎種(Rhizoglyphus spp.)、疥蟎種(Sarcoptes spp.)、 中東金蠍(Scorpio maurus)、Stenotarsonemus spp.、跗線蟎屬(Tarsonemus spp.)、四爪蟎屬(Tetranychus spp.)、Vasates lycopersici。 Arachnida , such as Acarus siro , Aceria sheldoni , Aculops spp., Aculus spp., blunt Amblyomma spp., Argas spp., Boophilus spp., Brevipalpus spp., Bryobia praetiosa , Piedia ( Chorioptes spp.), Dermanyssus gallinae , Eotetranychus spp., Epitrimerus pyri , Eutetranychus spp., Eriophyes spp. Hemitarsonemus spp., Hyalomma spp., Ixodes spp., Latrodectus mactans , Metatetranychus spp., Oligonychus spp., blunt Ornithodoros spp., Panonychus spp., Phyllocoptruta oleivora , Polyphagotarsonemus latus , Psoroptes spp., Rhipicephalus spp.), root mite species (Rhizoglyphus spp.), scabies mite species (Sarcoptes spp.), Middle East Scorpion (Scorpio maurus), Stenotarsonemus spp. , Tetranychus spp tarsal (Tarsonemus spp.), The genus Tetranychus (Tetranychus spp.), Vasates lycopersici .
屬雙殼綱(Bivalva)者,例如似殼菜蛤種(Dreissena spp.)。 It belongs to the class of Bivalva , for example, Dreissena spp.
屬唇足綱(Chilopoda)者,例如地蜈蚣種(Geophilus spp.)、蚰蜓種(Scutigera spp.)。 Genus Chilopoda (Chilopoda) are, for example, Geophilus species (Geophilus spp.), Scorpionfish dragonfly species (Scutigera spp.).
屬鞘翅目(Coleoptera)者,例如大豆象(Acanthoscehdes obtectus)、褐金龜種(Adoretus spp.)、赤楊葉甲(Agelastica alni)、叩頭蟲種(Agriotes spp.)、粉吹金龜子(Amphimallon solstitialis)、家具竊蟲(Anobium punctatum)、天牛種(Anoplophora spp.)、Anthonomus spp.、鰹節蟲(Anthrenus)、甘蔗金龜(Apogonia spp.)、金花蟲(Atomaria)、毛皮蠹(Attagenus)、菜豆象(Bruchidius obtectus)、菜豆象(Bruchus)、象甲(Ceuthorhynchus)、Cleonus mendicus、金針蟲(Conoderus spp.)、象甲(Cosmopolites)、紐西蘭金龜種(Costelytra zealandica)、象鼻蟲(Cureulio spp.)、楊幹象(Cryptorhynchus lapathi)、皮蠹(Dermestes)、玉米根蟲(Diabrotica)、瓢蟲(Epilachna)、煙草鑽孔蟲(Faustinus cubae)、弧背標本蟲(Gibbium psylloides)、非洲獨角仙(Heteronychus arator)、Hylamorpha elegans、家天牛(Hylotrupes bajulus)、目蓿葉象甲(Hypera postica)、小蠹蟲(Hypothenemus)、Lachnosterna consanguinea、科羅拉多金花蟲(Leptinotarsa decemlineata)、水稻水象鼻蟲 (Lissorhoptrus oryzophilus)、象鼻蟲(Lixus)、長蠹蟲(Lyctus spp.)、油菜露尾甲(Meligethes aeneus)、台灣吹粉金龜(Melolontha melolontha)、Migdolus spp.、天牛(Monochamus spp.)、象甲(Naupactus xanthographus)、金黃蛛甲(Niptus hololeucus)、犀角金龜(Oryctes rhinoceros)、鋸胸粉扁蟲(Oryzaephilus surinamensis)、黑耳喙象甲(Otiorrhynchus sulcatus)、小青花金龜(Oxycetonia jucunda)、辣根猿葉甲(Phaedon cochleariae)、鰓角金龜屬(Phyllophaga spp.)、日本金龜子(Popillia japonica)、馬鈴薯象(Premnotrypes)、油菜蘭跳甲(Psylliodes chrysocephala)、蛛甲(Ptinus spp.)、黑根瓢蟲(Rhizobius ventralis)、穀蠹(Rhizopertha dominica)、穀象(Sitophilus)、穀喙甲(Sphenophorus)、象甲(Sternechus)、Symphyletes spp.、麵包蟲(Tenebrio molitor)、穀盜蟲(Tribolium spp.)、皮蠹(Trogoderma spp.)、象甲(Tychius spp.)、虎天牛(Xylotrechus spp.)、步甲(Zabrus spp.)。 Genus Coleoptera (Coleoptera) by, for example, soybean like (Acanthoscehdes obtectus), brown beetle species (Adoretus spp.), Alder leaf beetle (Agelastica alni), beetle species (Agriotes spp.), Powder blowing chafer (Amphimallon solstitialis), furniture Anobium punctatum , Anoplophora spp., Anthonomus spp., Anthrenus , Apogonia spp., Atomaria , Attagenus , and peas Bruchidius obtectus ), Bruchus , Ceuthorhynchus , Cleonus mendicus , Conoderus spp., Cosmopolites , Costelytra zealandica , and Cureulio spp. ), Yang Ganxiang ( Cryptorhynchus lapathi ), Dermestes , Diabrotica , Epilachna , Faustinus cubae , Gibbium psylloides , African unicorn Heteronychus arator , Hylamorpha elegans , Hylotrupes bajulus , Hypera postica , Hypothenemus , Lachnost Erna consanguinea , Leptinotarsa decemlineata , Lissorhoptrus oryzophilus , Lyxus, Lyctus spp., Meligethes aeneus , Taiwanese tortoise ( Melolontha melolontha ), Migdolus spp., Monochamus spp., Naupactus xanthographus , Niptus hololeucus , Oryctes rhinoceros , Oryzaephilus surinamensis , black Otiorrhynchus sulcatus , Oxycetonia jucunda , Phaedon cochleariae , Phyllophaga spp., Popillia japonica , Premnotrypes , Psylliodes chrysocephala , Ptinus spp., Rhizobius ventralis , Rhizopertha dominica , Sitophilus , Sphenophorus , Sternechus ), Symphyletes spp., Tenebrio molitor , Tribolium spp., Trogoderma Spp .), Tychius spp., Xylotrechus spp., Zabrus spp.
屬彈尾綱(Collembola)者,例如Onychiurus armatus。 Is a member of the Collembola, such as Onychiurus armatus.
屬革翅目(Dermaptera)者,例如蠼螋(Forficula auricularia)。 It belongs to the genus Dermaptera, such as Forficula auricularia.
屬倍足綱(Diplopoda)者,例如千足蟲(Blaniulus guttulatus)。 A person of the genus Diplopoda, such as the genus Blancoi guttulatus.
屬雙翅目(Diptera)者,例如豹腳蚊屬(Aedes spp.)、瘧蚊屬(Anopheles spp.)、果蠅(Bibio hortulanus)、紅頭麗蠅(Calliphora erythrocephala)、地中海果實蠅(Ceratitis capitata)、金蠅種(Chrysomyia spp.)、軟體動物旋蠅屬(Cochliomyia spp.)、人皮蠅(Cordylobia anthropophaga)、家蚊屬(Culex spp.)、黃蠅屬(Cuterebra spp.)、油橄欖實蠅(Dacus oleae)、人膚蠅(Dermatobia hominis)、果蠅屬(Drosophila spp.)、廁蠅屬(Fannia spp.)、胃蠅屬(Gastrophilus spp.)、黑蠅屬(Hylemyia spp.)、虱蠅屬(Hyppobosca spp.)、皮蠅種(Hypoderma spp.)、斑潛蠅屬(Liriomyza spp.)、綠蠅種(Lucilia spp.)、蠅屬(Musca spp.)、稻綠蝽屬(Nezara spp.)、鼻蠅種(Oestrus spp.)、麥桿蠅(Oscinella frit)、菠菜潛葉蠅(Pegomyia hyoscyami)、草種蠅(Phorbia)、螫蠅屬(Stomoxys spp.)、馬蠅種(Tabanus spp.)、Tannia spp.、歐洲大蚊(Tipula paludosa)、汙蠅種(Wohlfahrtia spp.)。 Diptera (Diptera), such as Aedes spp., Anopheles spp., Bibio hortulanus, Calliphora erythrocephala, Ceratitis Capitata), Chrysomyia spp., Cochliomyia spp., Cordylobia anthropophaga, Culex spp., Cuterebra spp., olive oil Fruit fly (Dacus oleae), Dermatobia hominis, Drosophila spp., Fannia spp., Gastrophilus spp., Hylemyia spp. , Hypoposca spp., Hypoderma spp., Liriomyza spp., Lucilia spp., Musca spp., indica (Nezara spp.), Oestrus spp., Oscinella frit, Pegomyia hyoscyami, Phorbia, Stomoxys spp., horsefly (Tabanus spp.), Tannia spp., Tipula paludosa, Wohlfahrtia spp.
屬腹足綱(Gastropoda)者,例如Arion spp.種、扁捲軟體動物種(Biomphalaria spp.)、水泡軟體動物種(Bulinus spp.)、Deroceras spp.、土蝸種(Galba spp.)、椎實軟體動物種(Lymnaea spp.)、釘軟體動物種(Oncomelania spp.)、錐實蝸牛種(Succinea spp.) Gastropoda, such as Arion spp., Biomphalaria spp., Bulinus spp., Deroceras spp., Galba spp., Vertebral Lymnaea spp., Oncomelania spp., Succinea spp.
屬蠕蟲(helminths)者,例如十二指腸鉤蟲(Ancylostoma duodenale)、錫蘭鉤蟲(Ancylostoma ceylanicum)、巴西鉤蟲(Acylostoma braziliensis)、鉤蟲屬(Ancylostoma spp.)、蛔蟲(Ascaris lubricoides)、蛔蟲屬(Ascaris spp.)、馬來絲蟲(Brugia malayi)、帝汶絲蟲(Brugia timori)、反芻獸鉤蟲屬(Bunostomum spp.)、夏伯特線蟲種(Chabertia spp.)、肝吸蟲種(Clonorchis spp.)、古柏線蟲種(Cooperia spp.)、槍狀肝吸 蟲種(Dicrocoelium spp.)、絲狀網尾線蟲(Dictyocaulus filaria)、廣節裂頭絛蟲(Diphyllobothrium latum)、幾內亞蠕蟲(Dracunculus medinensis)、顆粒包生絛蟲(Echinococcus granulosus)、多房性包生絛蟲(Echinococcus multilocularis)、蟯蟲(Enterobius vermicularis)、片形吸蟲種(Faciola spp.)、血矛線蟲種(Haemonchus spp.)、異刺屬(Heterakis spp.)、微小絛蟲(Hymenolepis nana)、豬圓形線蟲屬(Hyostrongulus spp.)、羅阿絲蟲(Loa Loa)、細頸線蟲屬(Nematodirus spp.)、有齒食道口線蟲種(Oesophagostomum spp.)、後睾吸蟲屬(Opisthorchis spp.)、蟠尾絲蟲(Onchocerca volvulus)、胃線蟲屬(Ostertagia spp.)、並殖吸蟲屬(Paragonimus spp.)、人血吸蟲種(Schistosomen spp.)、福氏桿線蟲(Strongyloides fuelleborni)、糞小桿線蟲種(Strongyloides stercoralis spp.)、桿線蟲(Stronyloides)、絛蟲(Taenia saginata)、豬肉絛蟲(Taenia solium)、旋毛蟲(Trichinella spiralis)、鄉土旋毛蟲(Trichinella nativa)、布氏旋毛蟲(Trichinella britovi)、納氏旋毛蟲(Trichinella nelsoni)、偽旋毛蟲(Trichinella pseudopsiralis)、毛圓線蟲種(Trichostrongulus spp.)、鞭蟲(Trichuris trichuria)、班氏絲蟲(Wuchereria bancrofti)。 Genus helminths, such as Ancylostoma duodenale, Ancylostoma ceylanicum, Acylostoma braziliensis, Ancylostoma spp., Ascaris lubricoides, Ascaris spp .), Brugia malayi, Brugia timori, Bunostomum spp., Chabertia spp., Clonorchis spp. ), Coopereria spp., gun-like liver suction Dicrocoelium spp., Dictyocaulus filaria, Diphyllobothrium latum, Dracunculus medinensis, Echinococcus granulosus, multi-atrial Echinococcus multilocularis, Enterobius vermicularis, Faciola spp., Haemonchus spp., Heterakis spp., Hymenolepis nana, Hyostrongulus spp., Loa Loa, Nematodirus spp., Oesophagostomum spp., Opshorchis spp .), Onchocerca volvulus, Ostertagia spp., Paragonimus spp., Schistosomen spp., Strongyloides fuelleborni, Strongyloides stercoralis spp., Stronyloides, Taenia saginata, Taenia solium, Trichinella spiralis, Trichinella nativa, Trichinella britovi, Trichinella nelsoni, Trichinella pseudopsiralis, Trichostrongulus spp., Trichuris trichuria, Wuchereria bancrofti .
也可進一步控制如艾美球蟲(Eimeria)此類之原生動物。 Protozoa such as Eimeria can also be further controlled.
屬異翅亞目(Heteroptera)者,例如瓜緣蝽(Anasa tristis)、Antestiopsis spp.、Blissus spp.、Calocoris spp.、Campylomma livida、Cavelerius spp.、臭蟲屬(Cimex spp.)、 綠盲蝽(Creontiades dilutus)、Dasynus piperis、Dichelops furcatus、Diconocoris hewetti、Dysdercus spp.、Euschistus spp.、Eurygaster spp.、角盲蝽種(Heliopeltis spp.)、Horcias nobilellus、稻緣蝽種(Leptocorisa spp.)、葉足緣蝽(Leptoglossus phyllopus)、草盲蝽種(Lygus spp.)、Macropes excavatus、盲蝽(Miridae)、稻綠蝽屬(Nezara spp.)、稻蝽種(Oebalus spp.)、蝽象(Pentomidae)、蝽象(Piesma quadrata)、壁蝽種(Piezodorus spp.)、棉跳盲蝽(Psallus seriatus)、Pseudacysta persea、長紅獵蝽種(Rhodnius spp.)、可可褐盲蝽(Sahlbergella singularis)、Scotinophora spp.、梨冠網蝽(Stephanitis nashi)、Tibraca spp.、椎蝽種(Triatoma spp.)。 Of the genus Heteroptera, such as Anasa tristis, Antestiopsis spp., Blissus spp., Calocoris spp., Campylomma livida, Caverierius spp., Cimex spp. Creeoniades dilutus, Dasynus piperis, Dichelops furcatus, Diconocoris hewetti, Dysdercus spp., Euschistus spp., Eurygaster spp., Heliopeltis spp., Horcias nobilellus, Leptocorisa spp. ), Leptoglossus phyllopus, Lygus spp., Macropes excavatus, Miridae, Nezara spp., Oebalus spp., 蝽Pentomidae, Piesema quadrata, Piezodorus spp., Psallus seriatus, Pseudacysta persea, Rhodnius spp., Coco brown scorpion (Sahlbergella) Singularis), Scotinophora spp., Stephanitis nashi, Tibraca spp., Triatoma spp.
屬同翅目(Homoptera)者,例如Acyrthosipon spp.、巴西稻褐飛虱種(Aeneolamia spp.)、Agonoscena spp.、Aleurodes spp.、甘蔗穴粉虱(Aleurolobus barodensis)、Aleurothrixus spp.、Amrasca spp.、Anuraphis cardui、Aonidiella spp.、梨瘤蚜(Aphanostigma piri)、Aphis spp.、Arboridia apicalis、Aspidiella spp.、薄圓盾介殼蟲屬(Aspidiotus spp.)、Atanus spp.、馬鈴薯蚜(Aulacorthum solani)、伯粉虱屬(Bemisia spp.)、光管舌尾蚜(Brachycaudus helichrysii)、Brachycolus spp.、甘藍蚜(Brevicoryne brassicae)、Calligypona marginata、紅頭大葉蟬(Carneocephala fulgida)、甘蔗綿蚜(Ceratovacuna lanigera)、沬蟬(Cercopidae)、Ceroplastes spp.、草莓毛管蚜(Chaetosiphon fragaefolii)、Chionaspis tegalensis、Chlorita onukii、胡桃黑斑蚜(Chromaphis juglandicola)、茶褐圓蚧(Chrysomphalus ficus)、Cicadulina mbila、Coccomytilus halli、介殼蟲種(Coccus spp.)、茶藨隱瘤額蚜(Cryptomyzus ribis)、Dalbulus spp.、粉虱種(Dialeurodes spp.)、木虱種(Diaphorina spp.)、盾蚧屬(Diaspis spp.)、Doralis spp.、草履介殼蟲種(Drosicha spp.)、西圓尾蚜屬(Dysaphis spp.)、粉蚧種(Dysmicoccus spp.)、葉蟬種(Empoasca spp.)、Eriosoma spp.、Erythroneura spp.、Euscelis bilobatus、咖啡荒粉蚧(Geococcus coffeae)、褐透翅尖頭葉蟬(Homalodisca coagulata)、桃大尾蚜(Hyalopterus arundinis)、Icerya spp.、扁喙葉蟬屬(Idiocerus spp.)、Idioscopus spp.、灰飛虱(Laodelphax striatellus)、Lecanium spp.、Lepidosaphes spp.、蘿蔔蚜(Lipaphis erysimi)、Macrosiphum spp.、Mahanarva fimbriolata、高粱蚜(Melanaphis sacchari)、Metcalfiella spp.、麥無網長管蚜(Metopolophium dirhodum)、黑緣平翅斑蚜(Monellia costalis)、Monelliopsis pecanis、Myzus spp.、萵苣蚜(Nasonovia ribisnigri)、Nephotettix spp.、褐飛虱(Nilaparvata lugens)、Oncometopia spp.、Orthezia praelonga、Parabemisia myricae、Paratrioza spp.、Parlatoria spp.、癭綿蚜屬(Pemphigus spp.)、玉米花翅飛虱(Peregrinus maidis)、綿粉蚧屬(Phenacoccus spp.)、Phloeomyzus passerinii、蛇麻疣額蚜(Phorodon humuli)、葡萄根瘤蚜屬(Phylloxera spp.)、柑桔並盾蚧(Pinnaspis aspidistrae)、臀紋粉蚧屬(Planococcus spp.)、梨形原綿蠟蚧 (Protopulvinaria pyriformis)、桑白盾蚧(Pseudaulacaspis pentagona)、Pseudococcus spp.、木虱種(Psylla spp)、Pteromalus spp.、Pyrilla spp.、Quadraspidiotus spp、Quesada gigas、Rastrococcus spp.、縊管蚜屬(Rhopalosiphum spp.)、Saissetia spp.、葡萄帶葉蟬種(Scaphoides titanus)、麥二叉蚜(Schizaphis graminum)、刺盾蚧(Selenaspidus articulatus)、長唇基飛虱屬(Sogata spp.)、白背飛虱(Sogatella furcifera)、飛虱屬(Sogatodes spp.)、Stictocephala festina、Tenalaphara malayensis、胡桃黑蚜(Tinocallis caryaefoliae)、Tomaspis spp.、Toxoptera spp.、溫室白粉虱(Trialeurodes vaporariorum)、Trioza spp.、翻斤斗葉跳蟲種(Typhlocyba spp.)、矢尖蚧屬(Unaspis spp.)、葡萄根瘤蚜(Viteus vitifolii)。 Homoptera, such as Acyrthosipon spp., Aeneolamia spp., Agonoscena spp., Aleurodes spp., Aleurolobus barodensis, Aleurothrixus spp., Amrasca spp. Anuraphis cardui, Aonidiella spp., Aphanostigma piri, Aphis spp., Arboridia apicalis, Aspidiella spp., Aspidiotus spp., Atanus spp., Aulacorthum solani, Bemisia spp., Brachycaudus helichrysii, Brachycolus spp., Brevicoryne brassicae, Calligypona marginata, Carneocephala fulgida, Ceratovacuna lanigera, Cercopidae, Ceroplastes spp., Chaetosiphon fragaefolii, Chionaspis tegalensis, Chlorita Onukii, Chromaphis juglandicola, Chrysomphalus ficus, Cicadulina mbila, Coccomytilus halli, Coccus spp., Cryptomyzus ribis, Dalbulus spp. Dialeurodes spp., Diaphorina spp., Diaspis spp., Doralis spp., Drosicha spp., Dysaphis spp. , Dysmicoccus spp., Empoasca spp., Eriosoma spp., Erythroneura spp., Euceleli bilobatus, Geococcus coffeae, Homalodisca coagulata , Hyalopterus arundinis, Icerya spp., Idiocerus spp., Idioscopus spp., Laodelphax striatellus, Lecanium spp., Lepidosaphes spp., Lipaphis erysimi ), Macrosiphum spp., Mahanarva fimbriolata, Melanaphis sacchari, Metcalfiella spp., Metopolophium dirhodum, Monellia costalis, Monelliopsis pecanis, Myzus spp. Lettuce (Nasonovia ribisnigri), Nephotettix spp., Nilaparvata lugens, Oncometopia spp., Orthezia praelonga, Parabemisia myricae, Paratrioza spp., Parlatoria spp., Pemphigus spp., corn flower wing Peregrinus maidis, Phenacoccus spp., Phloeomyzus passerinii, Phorodon humuli, Phylloxera spp., Pinnaspis aspidistrae, Planococcus spp., pear-shaped original wax mites (Protopulvinaria pyriformis), Pseudaulacaspis pentagona, Pseudococcus spp., Psylla spp, Pteromalus spp., Pyrilla spp., Quadrazipiotus spp, Quesada gigas, Rastrococcus spp., Rhopalosip Spp.), Saissetia spp., Scaphoides titanus, Schizaphis graminum, Selenaspidus articulatus, Sogata spp., white back fly Sogatella furcifera, Sogatodes spp., Stictocephala festina, Tenalaphara malayensis, Tinocallis caryaefoliae, Tomaspis spp., Toxoptera spp., Trialeurodes vaporariorum, Trioza spp. Typhlocyba spp., Unaspis spp., Viteus vitifolii.
屬膜翅目(Hymenoptera)者,例如鋸蜂種(Diprion spp.)、李實蜂種(Hoplocampa spp.)、毛蟻種(Lasius spp.)、小黃家蟻(Monomorium pharaonis)、胡蜂種(Vespa spp.)。 Of the order Hymenoptera, such as Diprion spp., Hoplocampa spp., Lasius spp., Monomorium pharaonis, Vespa species Vespa spp.).
屬等足目(Isopoda)者,例如鼠婦(Armadillidium vulgare)、壁潮蟲(Oniscus asellus)、Porcellio scaber。 Isopoda, such as Armadillidium vulgare, Oniscus asellus, Porcellio scaber.
屬白蟻目(Isoptera)者,例如散白蟻種(Reticulitermes spp.)、土白蟻屬(Odontotermes spp.)。 Isoptera, such as Reticulitermes spp., Odontotermes spp.
屬鱗翅目(Lepidoptera)者,例如桑劍紋夜蛾(Acronicta major)、白斑煩夜蛾(Aedia leucomelas)、夜盜蟲種(Agrotis spp.)、棉葉波紋夜蛾(Alabama argillacea)、幹煞夜蛾屬(Anticarsia spp.)、甘藍夜蛾幼蟲(Barathra brassicae)、 Bucculatrix thurberiella、松尺蠖(Bupalus piniarius)、Cacoecia podana、Capua reticulana、蘋果蠹蛾(Carpocapsa pomonella)、Cheimatobia brumata、螟屬(Chilo spp.)、雲杉色卷蛾(Choristoneura fumiferana)、Clysia ambiguella、Cnaphalocerus spp.、埃及鑽夜蛾(Earias insulana)、地中海粉螟(Ephestia kuehniella)、黃毒蛾(Euproctis chrysorrhoea)、切夜蛾屬(Euxoa spp.)、Feltia spp.、蠟螟(Galleria mellonella)、鈴夜蛾屬(Helicoverpa spp.)、實夜蛾屬(Heliothis spp.)、褐織蛾(Hofmannophila pseudospretella)、茶長卷蛾(Homona magnanima)、食果巢蛾(Hyponomeuta padella)、蔥蘭夜蛾種(Laphygma spp.)、Lithocolletis blancardella、綠果夜蛾(Lithophane antennata)、豆白緣切根蟲(Loxagrotis albicosta)、毒蛾屬(Lymantria spp.)、天幕毛蟲(Malacosoma neustria)、甘藍夜蛾(Mamestra brassicae)、Mocis repanda、黏蟲(Mythimna separata)、Oria spp.、水稻負泥蟲(Oulema oryzae)、對小菜蛾(Panolis flammea)、棉紅鈴蟲(Pectinophora gossypiella)、柑橘潛葉蛾(Phyllocnistis citrella)、馬醉木屬(Pieris spp.)、小菜蛾(Plutella xylostella)、Prodenia spp.、擬黏夜蛾屬(Pseudaletia spp.)、大豆夜蛾(Pseudoplusia includens)、歐洲玉蜀黍螟(Pyrausta nubilalis)、灰翅夜蛾屬(Spodoptera spp.)、Thermesia gemmatalis、帶殼衣蛾(Tinea pellionella)、衣蛾(Tineola bisselliella)、櫟綠卷蛾(Tortrix viridana)、粉紋夜蛾種(Trichoplusia spp.)。 Lepidoptera, such as Acronicta major, Aedia leucomelas, Agrotis spp., Alabama argillacea, cognac Anticarsia spp., Barathra brassicae, Bucculatrix thurberiella, Bupalus piniarius, Cacoecia podana, Capua reticulana, Carpocapsa pomonella, Cheimatobia brumata, Chilo spp., Choristoneura fumiferana, Clysia ambiguella, Cnaphalocerus spp , Earias insulana, Ephestia kuehniella, Euproctis chrysorrhoea, Euxoa spp., Feltia spp., Galleria mellonella, Bombyx mori Genus (Helicoverpa spp.), Heliothis spp., Hofmannophila pseudospretella, Homona magnanima, Hyponomeuta padella, and Lyphygma spp .), Lithocolletis blancardella, Lithophea antennata, Loxalactis albicosta, Lymantria spp., Malacosoma neustria, Mazestra brassicae, Mocis Repanda, Mythimna separata, Oria spp., Oulema oryzae, Panolis flammea, cotton red bollworm (Pectinop) Hora gossypiella), Phyllocnistis citrella, Pieris spp., Plutella xylostella, Prodenia spp., Pseudaletia spp., Pseudoplusia includens , European mackerel (Pyrausta nubilalis), Spodoptera spp., Thermesia gemmatalis, Tinea pellionella, Tineola bisselliella, Tortrix viridana, pink Trichoplusia spp.
屬直翅目(Orthoptera)者,例如家蟋蟀(Acheta domesticus)、東方蜚蠊(Blatta orientalis)、德國蟑螂(Blattella germanica、螻蛄種(Gryllotalpa spp.)、馬德拉蜚蠊(Leucophaea maderae)、飛蝗屬(Locusta spp.)、黑蝗屬(Melanoplus spp.)、美洲蟑螂(Periplaneta americana)、沙漠蝗蟲(Schistocerca gregaria)。 Orthoptera, such as Acheta domesticus, Blatta orientalis, Blattella germanica, Gryllotalpa spp., Leucophaea maderae, planthopper Genus (Locusta spp.), Melanoplus spp., Periplaneta americana, and Desert locust (Schistocerca gregaria).
屬蚤目(Siphonaptera)者,例如角葉屬(Ceratophyllus spp.)、印度鼠蚤(Xenopsylla cheopis)。 It belongs to the genus Siphonaptera, such as Ceratophyllus spp., Xenopsylla cheopis.
屬綜合綱(Symphyla)者,例如白松蟲(Scutigerella immaculata)。 It belongs to the general class (Symphyla), such as the white cutworm (Scutigerella immaculata).
屬纓翅目(Thysanoptera)者,例如稻薊馬(Baliothrips biformis)、Enneothrips flavens、Frankliniella spp.、Heliothrips spp.、溫室條薊馬(Hercinothrips femoralis)、Kakothrips spp.、腹鉤薊馬(Rhipiphorothrips cruentatus)、跳薊馬屬(Scirtothrips spp.)、Taeniothrips cardamoni、薊馬屬(Thrips spp.)。 Of the order Thysanoptera, such as Balithrips biformis, Enneothrips flavens, Frankliniella spp., Heliothrips spp., Hercinothrips femoralis, Kakothrips spp., Rhipiphorothrips cruentatus , Scirthothrips spp., Taeniothrips cardamoni, Thrips spp.
屬纓尾亞目(Thysanura),例如衣魚(Lepisma saccharina)。 It belongs to the order of Thysanura, such as Lepisma saccharina.
寄生植物線蟲(phytoparasitic nematodes)包括鰻屬(Anguina spp)、滑刃線蟲屬(Aphelenchoides spp.)、刺線蟲屬(Belonoaimus spp.)、傘滑刃屬線蟲(Bursaphelenchus spp.)、續斷雙墊刃線蟲(Ditylenchus dipsaci)、黃金線蟲種(Globodera spp.)、軟體動物旋屬線蟲種(Heliocotylenchus spp.)、異皮線蟲屬(Heterodera spp.)、長針線蟲種(Longidorus spp.)、根結線蟲種(Meloidogyne spp.)、短體線蟲種(Pratylenchus spp.)、香蕉穿孔線蟲(Radopholus similis)、盤旋線蟲屬(Rotylenchus spp.)、毛刺線蟲種(Trichodorus spp.)、矮化線蟲種(Tylenchorhynchus spp.)、柑桔線蟲種(Tylenchulus spp.)、柑桔根線蟲(Tylenchulus semipenetrans)、劍線蟲屬(Xiphinema spp.)。 The phytoparasitic nematodes include Anguina spp, Aphelenchoides spp., Belonoaimus spp., Bursaphelenchus spp., and double-sided cutting edges. Ditylenchus dipsaci, Globodera spp., Heliocotylenchus spp., Heterodera spp., Long needles Spp.), Meloidogyne spp., Pratylenchus spp., Radopholus similis, Rotylenchus spp., Trichodorus spp. Tylenchorhynchus spp., Tylenchulus spp., Tylenchulus semipenetrans, Xiphinema spp.
此外,在獸醫學領域,本發明的新穎化合物可有效地用於對抗各種不同有害的動物寄生性有害生物(內寄生物及外寄生物),例如昆蟲和蠕蟲。 Furthermore, in the field of veterinary medicine, the novel compounds of the present invention are effective for combating various different harmful animal parasitic pests (endoparasites and ectoparasites) such as insects and helminths.
此類動物寄生性有害生物的實例包括以下所述之有害生物。 Examples of such animal parasitic pests include the pests described below.
昆蟲的實例包括胃蠅屬(Gasterophilus spp.)、螫蠅屬(Stomoxys spp.)、嚙毛虱屬(Trichodectes spp.)、長紅獵蝽種(Rhodnius spp.)、狗蚤(Ctenocephalides canis)、溫帶臭蟲(Cimx lecturius)、貓蚤(Ctenocephalides felis)、銅綠蠅(Lucilia cuprina)及其他類似昆蟲。 Examples of insects include Gasterophilus spp., Stomoxys spp., Trichodectes spp., Rhodnius spp., Ctenocephalides canis, temperate zone Cimx lecturius, Ctenocephalides felis, Lucilia cuprina and other similar insects.
蟎的實例包括鈍緣蜱種(Ornithodoros spp.)、硬蜱屬(Ixodes spp.)、牛蜱屬(Boophilus spp.)等等。 Examples of cockroaches include Ornithodoros spp., Ixodes spp., Boophilus spp., and the like.
在獸醫領域上(例如在獸醫學領域上),根據本發明之活性化合物可有效對抗動物寄生物,且對外寄生物或內寄生物。 In the veterinary field (for example in the field of veterinary medicine), the active compounds according to the invention are effective against animal parasites, as well as ectoparasites or endoparasites.
內寄生物一詞特別包含蠕蟲,如絛蟲、線蟲或吸蟲,以及雙孢子球蟲等原生動物。 The term endoparasite specifically includes helminths such as aphids, nematodes or trematodes, and protozoa such as bisporus coccidia.
外寄生物通常最好是節肢動物,尤其是像飛蠅(叮咬及舔食)、寄生蠅殂、虱子、頭虱、鳥虱、跳蚤及其他類似的昆蟲;或如壁虱(例如硬蜱或軟蜱)的疥蟲,或如癢蟎、秋蟎、鳥蟎及其他類似的小虱。 The ectoparasites are usually arthropods, especially like flies (biting and foraging), parasitic maggots, scorpions, head lice, guanines, fleas and other similar insects; or such as ticks (such as hard crickets or Soft mites, such as itch, autumn owl, guanine and other similar mites.
這些寄生物包括: These parasites include:
屬虱目(Anoplura)者,例如血虱種(Haematopinus spp.)、長顎虱種(Linognathus spp.)、虱種(Pediculus spp.)、陰虱屬(Phthirus spp.)、盲虱屬(Solenopotes spp.);以下為特別的例子:棘顎虱(Linognathus setosus)、犢顎虱(Linognathus vituli)、綿羊顎虱(Linognathus ovillus)、Linognathus oviformis、羊足顎虱(Linognathus pedalis)、窄面顎虱(Linognathus stenopsis)、Haematopinus asini macrocephalus、牛血虱(Haematopinus eurysternus)、豬血虱(Haematopinus suis)、頭虱(Pediculus humanus capitis)、體虱(Pediculus humanus corporis)、Phylloera vastatrix、陰虱(Phthirus pubis)、小藍牛虱(Solenopotes capillatus);屬食毛目(Mallophagida)且屬鈍角亞目(Amblycera)及絲角亞目(Ischnocerina)者,例如Trimenopon spp.、雞虱(Menopon spp.)、鴨虱(Trinoton spp.)、牛羽虱屬(Bovicola spp.)、Werneckiella spp.、Lepikentron spp.、Damalina spp.、嚙毛虱屬(Trichodectes spp.)、貓虱屬(Felicola spp.);以下為特別的例子:牛虱(Bovicola bovis)、綿羊虱(Bovicola ovis)、Bovicola limbata、Damalina bovis、犬齧毛虱(Trichodectes canis)、貓羽虱(Felicola subrostratus)、Bovicola caprae、 Lepikentron ovis、咬虱(Werneckiella equi);屬雙翅目(Diptera)且屬長角亞目(Nematocerina)及短角亞目(Brachycerina)者,例如豹腳蚊屬(Aedes spp.)、瘧蚊屬(Anopheles spp.)、家蚊屬(Culex spp.)、黑蠅種(Simulium spp.)、真蚋屬(Eusimulium spp.)、白蛉種(Phlebotomus spp.)、羅蛉屬(Lutzomyia spp.)、庫蠓種(Culicoides spp.)、斑虻屬(Chrysops spp.)、短蚋屬(Odagmia spp.)、Wilhelmia spp.、瘤虻屬(Hybomitra spp.)、黃虻屬(Atylotus spp.)、虻蟲種(Tabanus spp.)、麻虻種(Haematopota spp.)、Philipomyia spp.、Braula spp.、蠅屬(Musca spp.)、Hydrotaea spp.、螫蠅屬(Stomoxys spp.)、黑角蠅(Haematobia spp.)、Morellia spp.、廁蠅(Fannia spp.)、舌蠅屬(Glossina spp.)、綠頭蒼蠅種(Calliphora spp.)、綠蠅種(Lucilia spp.)、金蠅種(Chrysomyia spp.)、汙蠅種(Wohlfahrtia spp.)、麻蠅種(Sarcophaga spp.)、鼻蠅種(Oestrus spp.)、皮蠅種(Hypoderma spp.)、胃蠅屬(Gasterophilus spp.)、馬虱蠅種(Hippobosca spp.)、羊虱蠅屬(Lipoptena spp.)、蜱蠅屬(Melophagus spp.)、鼻狂蠅屬(Rhinoestrus spp.)、大蚊種(Tipula spp.);以下為特別的例子:埃及伊蚊(Aedes aegypti)、白紋伊蚊(Stegomyia albopicta(Aedes albopictus))、帶喙伊蚊(Aedes taeniorhynchus)、岡比亞按蚊(Anopheles gambiae)、五斑按蚊(Anopheles maculipennis)、紅頭麗蠅(Calliphora erythrocephala)、Chrysozona pluvialis、熱帶家蚊(Culex quinquefasciatus)、尖音庫蚊(Culex pipiens)、跗斑庫蚊 (Culex tarsalis)、夏廁蠅(Fannia canicularis)、肉麻蠅(Sarcophaga carnaria)、廄螫蠅(Stomoxys calcitrans)、歐洲大蚊(Tipula paludosa)、銅綠蠅(Lucilia cuprina)、絲光綠蠅(Lucilia sericata)、爬蚋(Simulium reptans)、巴浦白蛉(Phlebotomus papatasi)、長鬚白蛉(Phlebotomus longipalpis)、Odagmia ornata、Wilhelmia equina、Boophthora erythrocephala、吵擾虻(Tabanus bromius)、Tabanus spodopterus、abanus atratus、Tabanus sudeticus、Hybomitra ciurea、盲斑虻(Chrysops caecutiens)、黃緣斑虻(Chrysops relictus)、Haematopota pluvialis、Haematopota italica、秋家蠅(Musca autumnalis)、家蠅(Musca domestica)、真角蠅(Haematobia irritans irritans)、水牛蠅(Haematobia irritans exigua)、牛血蠅(Haematobia stimulans)、頭蠅(Hydrotaea irritans)、白斑齒股蠅(Hydrotaea albipuncta)、Chrysomya chloropyga、蛆症金蠅(Chrysomya bezziana)、羊狂蠅(Oestrus ovis)、牛蠅(Hypoderma bovis)、紋皮蠅(Hypoderma lineatum)、山羊牛蠅(Przhevalskiana silenus)、人膚蠅(Dermatobia hominis)、羊蜱蠅(Melophagus ovinus)、Lipoptena capreoli、鹿虱蠅(Lipoptena cervi)、Hippobosca variegata、馬虱蠅(Hippobosca equina)、腸胃蠅(Gasterophilus intestinalis)、赤尾胃蠅(Gasterophilus haemorroidalis)、Gasterophilus inermis、鼻胃蠅(Gasterophilus nasalis)、黑角胃蠅(Gasterophilus nigricornis)、黑腹胃蠅(Gasterophilus pecorum)、蜂虱(Braula coeca);屬蚤目(Siphonapterida)者,例如蚤屬(Pulex spp.)、櫛頭蚤屬(Ctenocephalides spp.)、潛蚤屬(Tunga spp.)、客蚤屬(Xenopsylla spp.)、角葉屬(Ceratophyllus spp.);以下為特別的例子:狗蚤(Ctenocephalides canis)、貓蚤(Ctenocephalides felis)、人蚤(Pulex irritans)、穿皮潛蚤(Tunga penetrans)、印度鼠蚤(Xenopsylla cheopis);屬Heteropterida者,例如,臭蟲屬(Cimex spp.)、錐蝽屬(Triatoma spp.)、長紅獵蝽種(Rhodnius spp.)、錐蝽屬(Panstrongylus spp.) Of the order Anoplura, such as Haematopinus spp., Linognathus spp., Pediculus spp., Phthirus spp., Solenopotes Spp.); The following are special examples: Linognathus setosus, Linognathus vituli, Linognathus ovillus, Linognathus oviformis, Linognathus pedalis, Narrow-faced 颚虱(Linognathus stenopsis), Haematopinus asini macrocephalus, Haematopinus eurysternus, Haematopinus suis, Pediculus humanus capitis, Pediculus humanus corporis, Phylloera vastatrix, Phthirus pubis , Solenopotes capillatus; belonging to Mallophagida and belonging to Amblycera and Ischnocerina, such as Trimenopon spp., Menopon spp., duck plague (Trinoton spp.), Bovicola spp., Werneckiella spp., Lepikentron spp., Damalina spp., Trichodectes spp., Felicola spp.; example: Bovicola bovis, Bovicola ovis, Bovicola limbata, Damalina bovis, Trichodectes canis, Felicola subrostratus, Bovicola caprae, Lepikentron ovis, Werneckiella equi; belonging to the genus Diptera and belonging to the genus Nematocerina and Brachycerina, such as the genus Aedes spp. (Anopheles spp.), Culex spp., Simulium spp., Eusimulium spp., Phlebotomus spp., Lutzomyia spp. , Culicoides spp., Chrysops spp., Odagmia spp., Wilhelmia spp., Hybomitra spp., Atylotus spp. Tabanus spp., Haematopota spp., Philipomyia spp., Braula spp., Musca spp., Hydrotaea spp., Stomoxys spp., Black horn flies (Haematobia spp.), Morellia spp., Fannia spp., Glossina spp., Calliphora spp., Lucilia spp., Golden fly species Chrysomyia spp.), Wohlfahrtia spp., Sarcophaga spp., Oestrus spp., Hypoderma spp., Gasterophilus spp., horse虱fly species (Hippobosca spp.) , Lipoptena spp., Melophagus spp., Rhinoestrus spp., Tipula spp.; the following is a special case: Aedes aegypti (Aedes Aegypti), Aedes albopicta (Aedes albopictus), Aedes taeniorhynchus, Anopheles gambiae, Anopheles maculipennis, Calliphora erythrocephala, Chrysozona pluvialis, Culex quinquefasciatus, Culex pipiens, Culex pipiens (Culex tarsalis), Fannia canicularis, Sarcophaga carnaria, Stomoxys calcitrans, Tipula paludosa, Lucilia cuprina, Lucilia sericata , Mumulium reptans, Phlebotomus papatasi, Phlebotomus longipalpis, Odagmia ornata, Wilhelmia equina, Boophthora erythrocephala, Tabanus bromius, Tabanus spodopterus, abanus atratus, Tabanus Sudeticus, Hybomitra ciurea, Chrysops caecutiens, Chrysops relictus, Haematopota pluvialis, Haematopota italica, Musca autumnalis, Musca domestica, Haematobia irritans irritans ), Haematobia irritans exigua, Haematobia stimulans, Hydrotaea irritans, Hydrotaea albipuncta, Chrysomya chloropyga, Chrysomya bezziana, Sheep flies Oestrus ovis), Hypoderma bovis, Hypoderma lineatum, Goat cattle fly (Przhe) Valskiana silenus), Dermatobia hominis, Melophagus ovinus, Lipoptena capreoli, Lipoptena cervi, Hippobosca variegata, Hippotosca equina, Gasterophilus intestinalis, red tail Gasterophilus haemorroidalis, Gasterophilus inermis, Gasterophilus nasalis, Gasterophilus nigricornis, Gasterophilus pecorum, Braula Coeca); belonging to the genus Siphonapterida, such as Pulex spp., Ctenocephalides spp., Tunga spp., Xenopsylla spp., horn Genus (Ceratophyllus spp.); the following are special examples: Ctenocephalides canis, Ctenocephalides felis, Pulex irritans, Tunga penetrans, Xenopsylla cheopis Of the genus Heteropterida, for example, Cimex spp., Triatoma spp., Rhodnius spp., Panstrongylus spp.
屬蜚蠊目(Blattarida)者,例如東方蜚蠊(Blatta orientalis)、美洲蟑螂(Periplaneta americana)、德國小蠊(Blattela germanica)、夏柏拉蟑螂屬(Supella spp.)(例如棕帶蜚蠊(Suppella longipalpa));屬蜱蟎亞綱(Acari(Acarina))且屬變異(Meta-)及中氣亞目(Mesostigmata)者,例如銳緣蜱屬(Argas spp.)、Ornithodorus spp.、耳蜱屬(Otobius spp.)、硬蜱屬(Ixodes spp.)、鈍眼蜱屬(Amblyomma spp.)、扇頭蜱(牛蜱)屬(Rhipicephalus(Boophilus)spp.)、矩頭蟬屬(Dermacentor spp.)、血蜱屬(Haemophysalis spp.)、璃眼蜱屬(Hyalomma spp.)、皮刺蟎屬(Dermanyssus spp.)、扇頭蜱屬(Rhipicephalus spp.)(多宿主壁虱的原始屬)、禽刺蟎屬(Ornithonyssus spp.)、肺刺蟎(Pneumonyssus spp.)、耳蟎屬(Raillietia spp)、肺刺蟎(Pneumonyssus spp.)、胸孔蟎屬(Sternostoma spp.)、瓦蟎(Varroa spp.)、蟎屬(Acarapis spp.);以下為特別的例 子:波斯銳緣蜱(Argas persicus)、鴿銳緣蜱(Argas reflexus)、Ornithodorus moubata、耳殘喙蜱(Otobius megnini)、微小牛蜱(Rhipicephalus(Boophilus)microplus)、脫色扇頭蜱(Rhipicephalus(Boophilus)decoloratus)、Rhipicephalus(Boophilus)annulatus、Rhipicephalus(Boophilus)calceratus、小亞璃眼蜱(Hyalomma anatolicum)、埃及璃眼蜱(Hyalomma aegypticum)、邊緣璃眼蜱(Hyalomma marginatum)、Hyalomma transiens、外翻扇頭蜱(Rhipicephalus evertsi)、菎子硬蜱(Ixodes ricinus)、六角形硬蜱(Ixodes hexagonus)、犬硬蜱(Ixodes canisuga)、多毛硬蜱(Ixodes pilosus)、淺紅硬蜱(Ixodes rubicundus)、肩突硬蜱(Ixodes scapularis)、全環硬蜱(Ixodes holocyclus)、嗜群血蜱(Haemaphysalis concinna)、刻點血蜱(Haemaphysalis punctata)、Haemaphysalis cinnabarina、鼠耳血蜱(Haemaphysalis otophila)、犬血蜱(Haemaphysalis leachi)、Haemaphysalis longicorni、邊緣革蜱(Dermacentor marginatus)、網紋革蜱(Dermacentor reticulatus)、花紋革蜱(Dermacentor pictus)、白紋革蜱(Dermacentor albipictus)、落磯山革蜱(Dermacentor andersoni)、美洲狗蜱(Dermacentor variabilis)、Hyalomma mauritanicum、棕色犬壁虱(Rhipicephalus sanguineus)、囊狀扇頭蜱(Rhipicephalus bursa)、具尾扇頭蜱(Rhipicephalus appendiculatus)、好望角扇頭蜱(Rhipicephalus capensis)、圖蘭扇頭蜱(Rhipicephalus turanicus)、贊比西扇頭蜱(Rhipicephalus zambeziensis)、美 洲鈍眼蜱(Amblyomma americanum)、彩飾鈍眼蜱(Amblyomma variegatum)、斑點鈍眼蜱(Amblyomma maculatum)、希伯來鈍眼蜱(Amblyomma hebraeum)、卡延鈍眼蜱(Amblyomma cajennense)、雞皮刺蟎(Dermanyssus gallinae)、囊形刺脂蟎(Ornithonyssus bursa)、北方刺脂蟎(Ornithonyssus sylviarum)、雅氏瓦蟎(Varroa jacobsoni);屬輻蟎亞目(Actinedida(Prostigmata))及粉蟎目(Acaridida(Astigmata))者,例如蟎屬(Acarapis spp.)、Cheyletiella spp.、Ornithocheyletia spp.、Myobia spp.、Psorergates spp.、蠕形蟎屬(Demodex spp.)、恙蟎屬(Trombicula spp.)、Listrophorus spp.、壁虱屬(Acarus spp.)、食酪蟎屬(Tyrophagus spp.)、嗜木蟎屬(Caloglyphus spp.)、Hypodectes spp.、Pterolichus spp.、癢蟎屬(Psoroptes spp.)、皮蟎屬(Chorioptes spp.)、耳蟎屬(Otodectes spp.)、疥蟎屬(Sarcoptes spp.)、耳蟎屬(Notoedres spp.)、鳥疥蟎屬(Knemidocoptes spp.)、胞蟎屬(Cytodites spp.)、雞雛蟎屬(Laminosioptes spp.);以下為特別的例子:牙氏姬螫蟎(Cheyletiella yasguri)、布氏姬螫蟎(Cheyletiella blakei)、犬脂蟎(Demodex canis)、牛脂蟎(Demodex bovis)、綿羊脂蟎(Demodex ovis)、山羊蠕形蟎(Demodex caprae)、馬脂蟎(Demodex equi)、Demodex caballi、Demodex suis、秋收恙蟎(Neotrombicula autumnalis)、Neotrombicula desaleri、Neoschongastia xerothermobia、紅恙蟎(Trombicula akamushi)、犬耳蟎(Otodectes cynotis)、貓耳蟎(Notoedres cati)、Sarcoptis canis、牛疥蟎(Sarcoptes bovis)、羊疥蟎(Sarcoptes ovis)、Sarcoptes rupicaprae(S.caprae)、馬疥蟎(Sarcoptes equi)、豬疥蟎(Sarcoptes suis)、綿羊癢蟎(Psoroptes ovis)、兔癢蟎(Psoroptes cuniculi)、馬癢蟎(Psoroptes equi)、牛足蟎(Chorioptes bovis)、羊生疥蟎(Psoergates ovis)、Pneumonyssoidic mange、犬鼻疥蟲(Pneumonyssoides caninum)、氣管蟎(Acarapis woodi)。 Of the genus Blattarida, such as Blatta orientalis, Periplaneta americana, Blattela germanica, Supella spp. (eg brown belt 蜚蠊 ( Suppella longipalpa)); belonging to Acari (Acarina) and belonging to the mutated (Meta-) and mesostigmata, such as Argas spp., Ornithodorus spp., deafness Genus (Otobius spp.), Ixodes spp., Amblyomma spp., Rhipicephalus (Boophilus spp.), Dermacentor spp .), Haemophysalis spp., Hyalomma spp., Dermanyssus spp., Rhipicephalus spp. (original genus of multi-hosted ticks) , Ornithonyssus spp., Pneumonyssus spp., Raillietia spp, Pneumonyssus spp., Sternostoma spp., Corrugated (Sternostoma spp.) Varroa spp.), Acarapis spp.; the following are special cases Son: Argas persicus, Argas reflexus, Ornithodorus moubata, Otobius megnini, Rhipicephalus (Boophilus microplus), Rhipicephalus (Rhipicephalus) Boophilus) decoloratus), Rhipicephalus (Boophilus) annuulas, Rhipicephalus (Boophilus) calceratus, Hyalomama anatolicum, Hyalomma aegypticum, Hyalomma marginatum, Hyalomma transiens, valgus Rhipicephalus evertsi, Ixodes ricinus, Ixodes hexagonus, Ixodes canisuga, Ixodes pilosus, Ixodes rubicundus , Ixodes scapularis, Ixodes holocyclus, Haemaphysalis concinna, Haemaphysalis punctata, Haemaphysalis cinnabarina, Haemaphysalis otophila, dogs Bloody (Haemaphysalis leachi), Haemaphysalis longicorni, Dermacentor marginatus, Dermacentor reticulatus, flowers Dermacentor pictus, Dermacentor albipictus, Dermacentor andersoni, Dermacentor variabilis, Hyalomma mauritanicum, Rhipicephalus sanguineus, capsular fan Rhipicephalus bursa, Rhipicephalus appendiculatus, Rhipicephalus capensis, Rhipicephalus turanicus, Rhipicephalus zambeziensis, beauty Amblyomma americanum, Amblyomma variegatum, Amblyomma maculatum, Amblyomma hebraeum, Amblyomma cajennense, chicken prick Dermanyssus gallinae, Ornithonyssus bursa, Ornithonyssus sylviarum, Varroa jacobsoni, Actinedida (Prostigmata) and pink mites (Actinedida (Prostigmata)) Acaridida (Astigmata)), such as Acarapis spp., Cheyletiella spp., Ornithocheyletia spp., Myobia spp., Psorergates spp., Demodex spp., Trombula spp. , Listrophorus spp., Acarus spp., Tyrophagus spp., Caloglyphus spp., Hypodectes spp., Pterolichus spp., Psoroptes spp. , Choriopteres spp., Otodectes spp., Sarcoptes spp., Notoedres spp., Knemidocoptes spp., Cymbidium (Cytodites spp.), larvae (Laminosioptes spp.); the following are special Son: Cheyletiella yasguri, Cheyletiella blakei, Demodex canis, Demodex bovis, Demodex ovis, Goat Demodex Demodex caprae), Demodem equi, Demodex caballi, Demodex suis, Neocrombicula autumnalis, Neotrombicula desaleri, Neoschongastia xerothermobia, Trombula akamushi, Otodectes cynotis, cat ears Notoedres cati, Sarcoptis Canis, Sarcoptes bovis, Sarcoptes ovis, Sarcoptes rupicaprae (S. caprae), Sarcoptes equi, Sarcoptes suis, Psoroptes ovis, Psoroptes cuniculi, Psoroptes equi, Chorioptes bovis, Psoergates ovis, Pneumonyssoidic mange, Pneumonyssoides caninum, Acarapis woodi ).
根據本發明之活性化合物亦適用於控制會攻擊動物的節肢動物、蠕蟲及原生動物。 The active compounds according to the invention are also suitable for controlling arthropods, helminths and protozoa which attack animals.
這些動物包括農業牲畜,如牛、綿羊、山羊、馬、豬、騾、駱駝、水牛、兔、雞、火雞、鴨、鵝、養殖魚類及蜜蜂。 These animals include agricultural livestock such as cattle, sheep, goats, horses, pigs, donkeys, camels, buffalo, rabbits, chickens, turkeys, ducks, geese, farmed fish and bees.
此外,這些動物包括馴養動物,例如狗、貓、籠鳥、觀賞魚,以及已知的實驗性動物,例如倉鼠、天竺鼠、野鼠及家鼠。 In addition, these animals include domesticated animals such as dogs, cats, cage birds, ornamental fish, and known experimental animals such as hamsters, guinea pigs, voles and house mice.
藉由控制這些節肢動物、蠕蟲及/或原生動物達成減少死亡和提升成效(針對肉、牛奶、毛、皮、蛋、蜂蜜及其他類似製品)及宿主動物之健康。如此,經由利用根據本發明的活性化合物,可使得飼養動物的工作更為經濟而簡單。 By controlling these arthropods, worms and/or protozoa to achieve reduced death and improved effectiveness (for meat, milk, hair, skin, eggs, honey and other similar products) and the health of the host animal. Thus, by using the active compound according to the invention, the work of raising animals can be made more economical and simple.
例如,預防或中斷寄生物吸取宿主的血液可能是所欲的。 For example, preventing or interrupting parasites from drawing the host's blood may be desirable.
同時,對寄生物進行控制可有助於預防傳播傳染源。 At the same time, controlling parasites can help prevent the spread of infectious agents.
此處使用的「控制」一詞,係有關於獸醫領域,表示活性化合物有效於將已感染此類寄生物之動物之各自寄生 物的發生率降至無害的程度。 The term "control" as used herein relates to the veterinary field and indicates that the active compound is effective against the respective parasitic animals that have been infected with such parasites. The incidence of the object has dropped to a level that is harmless.
更精確地說,此處使用的「控制」一詞表示此活性化合物係有效於殺死各自的寄生物,抑制其生長或抑制其增殖。一般而言,在使用來治療動物時,根據本發明的活性化合物可直接施用。 More precisely, the term "control" as used herein means that the active compound is effective in killing the respective parasites, inhibiting their growth or inhibiting their proliferation. In general, the active compounds according to the invention may be administered directly when used to treat animals.
較佳將這些化合物呈醫藥組成物施用,其可含有此技術領域已知的醫藥上可接受之賦形劑及/或輔助劑。 These compounds are preferably administered as a pharmaceutical composition which may contain pharmaceutically acceptable excipients and/or adjuvants known in the art.
在獸醫領域和動物飼養方面,主要是使用已知的方式來施用(例如投予)活性化合物,以諸如藥片、膠囊、藥水、灌藥水(drenches)、顆粒、藥膏、大丸藥(boluses)、灌食法及栓劑的形式,進行經腸給藥;非口服給藥,例如注射(肌肉內、皮下、靜脈、腹膜內等等)、植入投藥;鼻腔投藥;以諸如藥浴或浸漬、噴灑、澆潑與滴劑、洗滌、佈撒的方式藉由真皮投藥,以及使用含活性化合物的成型製品(例如項圈(collars)、耳標、尾標、肢體縛帶(limb bands)、韁繩(halters)、標示裝置等等)來輔助投藥。 In the veterinary field and in the field of animal husbandry, active compounds are mainly administered (for example, by administration) in a known manner, such as tablets, capsules, syrups, drenches, granules, ointments, boluses, irrigation. In the form of food and suppository, enteral administration; parenteral administration, such as injection (intramuscular, subcutaneous, intravenous, intraperitoneal, etc.), implantation; nasal administration; such as medicated bath or dipping, spraying, Pouring and dropping, washing, spreading, by dermal administration, and using molded articles containing active compounds (such as collars, ear tags, tails, limb bands, halters) , marking devices, etc.) to assist in the administration of drugs.
活性化合物可調配為洗髮精,或作為可用於氣溶膠(aerosols)、未加壓噴(unpressurized sprays)(如泵式噴霧)和霧化器噴霧(atomizer sprays)的合適調配物。 The active compound can be formulated as a shampoo or as a suitable formulation for use in aerosols, unpressurized sprays such as pump sprays, and atomizer sprays.
用於牲畜、家禽、家畜及此類動物時,可將本發明活性化合物以調配物(例如粉劑、可溼性粉劑[「WP」]、乳劑、乳化濃縮物[「EC」]、流體(flowable)、均相溶液及水懸浮濃縮物[「SC」])施用,其含有1至80%(按重量計)的量的活性化合物,係直接使用或在稀釋後(如100至10 000倍的 稀釋率)使用,或用於化學浴。 For use in livestock, poultry, livestock and such animals, the active compounds of the invention may be formulated (for example, powders, wettable powders ["WP"], emulsions, emulsified concentrates ("EC"), fluids (flowable) , a homogeneous solution and an aqueous suspension concentrate ["SC")), which contains from 1 to 80% by weight of the active compound, either directly or after dilution (eg 100 to 10,000 times) Dilution rate) used, or used in chemical baths.
用於獸醫領域時,根據本發明的活性化合物可與合適的增效劑或其他活性化合物(例如殺蟎劑、殺蟲劑、驅蟲劑和抗原生動物試劑)組合使用。 When used in the veterinary art, the active compounds according to the invention can be used in combination with suitable synergists or other active compounds, for example acaricides, insecticides, insect repellents and antiprotozoal agents.
在本發明中,包含所有這些具殺蟲作用對抗有害生物物質均以殺蟲劑表示。 In the present invention, all of these insecticidal agents against harmful biological substances are represented by insecticides.
作為殺蟲劑使用時,本發明中的活性化合物可利用習知的調配物形式來備製。 When used as an insecticide, the active compound of the present invention can be prepared by using a conventional formulation form.
調配物形式的實例包括溶液、乳劑、可溼性粉劑、水可分散粒劑、懸浮液、粉劑、發泡劑、藥膏、藥片、粒劑、氣溶膠、已滲入活性化合物的天然與合成材料、微膠囊、種子塗佈劑(seed coating agents)、配合燃燒器具使用的調配物(例如煙燻盒、罐子、線圈或其他此類的燃燒器具)、ULV(冷霧、暖霧)等等的形式。 Examples of formulation forms include solutions, emulsions, wettable powders, water-dispersible granules, suspensions, powders, foaming agents, ointments, tablets, granules, aerosols, natural and synthetic materials which have been infiltrated into the active compound, Microcapsules, seed coating agents, formulations used in conjunction with combustion appliances (eg, smoke boxes, cans, coils, or other such burners), ULV (cold fog, warm fog), etc. .
這些調配物可使用本身已知的方法製作。 These formulations can be made using methods known per se.
例如,可混合活性化合物與顯影劑(即水性稀釋劑或載體;液化氣體稀釋劑或載體;固態稀釋劑或載體),並選擇性混入界面活性劑(即乳化劑及/或分散劑及/或發泡劑),藉此製造調配物。 For example, the active compound may be mixed with a developer (ie, an aqueous diluent or carrier; a liquefied gas diluent or carrier; a solid diluent or carrier), and optionally mixed with a surfactant (ie, an emulsifier and/or dispersant and/or A blowing agent) whereby a formulation is made.
例如,若要以水作為顯影劑,可使用有機溶劑作為輔助溶劑。 For example, if water is to be used as the developer, an organic solvent can be used as an auxiliary solvent.
水性稀釋劑或載體的實例包括芳香烴(例如二甲苯、甲苯、烷基萘及其類似物)、氯化芳烴或氯化脂族烴(例如氯苯、氯乙烯、二氯甲烷)、脂肪羥(如環己烷)、石蠟(例如礦 物油餾分)、醇類(例如丁醇,乙二醇及其乙醚與酯類及類似物)、酮類(例如丙酮、甲基乙基酮、甲基異丁基酮、環己酮及類似物)、強極性溶劑(例如二甲基甲醯胺、二甲亞碸及類似物),以及水及類似物。液化氣體稀釋劑或載體可以是在常溫常壓下為氣態之物,例如丁烷、丙烷、氮氣、二氧化碳及鹵化烴等推噴劑(aerosol propellants)。固體稀釋劑的實例包括粉狀天然礦物質(例如高嶺土、黏土、滑石、白堊、石英,厄帖浦土、蒙脫土、矽藻土及類似物)、粉狀合成礦物質(例如高度分散的矽酸、礬土、矽酸鹽及類似物)及類似物。顆粒的固體載體包括粉狀和篩過的岩石(例如方解石、大理石、浮石、海泡石、白雲石及類似物)、有機和無機粉末的合成顆粒、細顆粒的有機材料(例如鋸屑、椰子殼、玉米棒、菸草稈及類似物)及類似物。乳化劑及/或發泡劑的實例包括非離子和陰離子乳化劑[例如聚氧乙烯脂肪酸酯、聚氧乙烯脂肪酸醇醚(例如烷基芳基聚乙二醇醚)、烷基磺酸鹽、烷基硫酸鹽、芳基磺酸酯及類似物]、白蛋白水解產物及類似物。分散劑之實例包括木質素亞硫酸鹽廢液和甲基纖維素。 Examples of aqueous diluents or carriers include aromatic hydrocarbons (e.g., xylene, toluene, alkylnaphthalene, and the like), chlorinated aromatic hydrocarbons or chlorinated aliphatic hydrocarbons (e.g., chlorobenzene, vinyl chloride, methylene chloride), aliphatic hydroxy groups. (such as cyclohexane), paraffin (such as mine Oil fraction), alcohols (such as butanol, ethylene glycol and its ethers and esters and analogs), ketones (such as acetone, methyl ethyl ketone, methyl isobutyl ketone, cyclohexanone and the like) , strong polar solvents (such as dimethylformamide, dimethyl hydrazine and the like), as well as water and the like. The liquefied gas diluent or carrier may be a gaseous substance such as butane, propane, nitrogen, carbon dioxide, and a halogenated hydrocarbon, which is gaseous at normal temperature and pressure. Examples of solid diluents include powdered natural minerals (e.g., kaolin, clay, talc, chalk, quartz, erectite, montmorillonite, diatomaceous earth, and the like), powdered synthetic minerals (e.g., highly dispersed Capric acid, alumina, citrate and the like) and the like. Solid carriers of particles include powdered and sieved rocks (such as calcite, marble, pumice, sepiolite, dolomite and the like), synthetic particles of organic and inorganic powders, fine-grained organic materials (eg sawdust, coconut shells) , corn cobs, tobacco stalks and the like) and the like. Examples of emulsifiers and/or blowing agents include nonionic and anionic emulsifiers [e.g., polyoxyethylene fatty acid esters, polyoxyethylene fatty acid alcohol ethers (e.g., alkyl aryl polyglycol ethers), alkyl sulfonates , alkyl sulfates, aryl sulfonates and the like], albumin hydrolysates and the like. Examples of the dispersing agent include lignin sulfite waste liquid and methyl cellulose.
也可在調配物(粉劑、粒劑、乳劑)中使用固色劑(fixing agent),而固色劑的實例包括羧甲基纖維素、天然及合成的聚合物(例如阿拉伯樹膠、聚乙烯醇、聚醋酸乙烯酯及類似物)及類似物。也可使用著色劑,其實例包括無機色素(例如氧化鐡、氧化鈦、普魯士藍及類似物)、有機染料(例如茜素染料、偶氮染料或金屬酞菁染料),以及微量元素(例如鐵 鹽、錳鹽、硼鹽、銅鹽、鈷鹽、鉬鹽和鋅鹽)。一般而言,調配物可包含活性化合物含量範圍從0.1至95%(按重量計),較佳從0.5至90%(按重量計)。根據本發明的化合物也能作為混合物,與其他活性化合物(例如殺蟲劑、毒餌、殺菌劑、殺蟎劑、殺線蟲劑、殺真菌劑、生長調節劑、除草劑及類似物)以其具商業用處之調配物形式共存,並以從這些調配物來製備的應用形式共存。 Fixing agents can also be used in formulations (powders, granules, emulsions), and examples of fixing agents include carboxymethylcellulose, natural and synthetic polymers (eg, gum arabic, polyvinyl alcohol). , polyvinyl acetate and the like) and the like. Colorants may also be used, examples of which include inorganic pigments (such as cerium oxide, titanium oxide, Prussian blue, and the like), organic dyes (such as alizarin dyes, azo dyes or metal phthalocyanine dyes), and trace elements (such as iron). Salt, manganese salt, boron salt, copper salt, cobalt salt, molybdenum salt and zinc salt). In general, the formulations may contain the active compound in an amount ranging from 0.1 to 95% by weight, preferably from 0.5 to 90% by weight. The compounds according to the invention can also be used as mixtures with other active compounds (for example insecticides, baits, bactericides, acaricides, nematicides, fungicides, growth regulators, herbicides and the like) Commercial formulations are coexisting and coexist in the form of application prepared from these formulations.
根據本發明且以具商業用處之應用形式存在的化合物,其含量足以存在極大的差異。 The compounds according to the invention and which are present in commercial applications are present in an amount sufficient to vary greatly.
在實際應用上,根據本發明之化合物的濃度範圍,可從像是0.0000001至100%(按重量計),最好是從0.00001至1%(按重量計)。 In practical applications, the concentration range of the compound according to the present invention may range from 0.0000001 to 100% by weight, preferably from 0.00001 to 1% by weight.
可藉由適合應用形式的習知方法,來使用根據本發明的化合物。 The compounds according to the invention can be used by conventional methods suitable for the application form.
當用於抑制衛生性有害生物和涉及所儲藏產品之有害生物時,本發明之活性化合物可有效穩定石灰材料上的鹼,而在木材和土壤上也有優異的殘餘效應。本發明之化合物在以下方面可具備良好的特性:施用量、殘留調配物、選擇性、毒性、生產方法、高活性、控制範圍廣泛性、安全性、耐藥生物(例如對有機磷劑及/或胺基甲酸酯劑具有抗藥性之有害生物)的控制。 When used to inhibit hygienic pests and pests involved in stored products, the active compounds of the present invention are effective in stabilizing alkali on lime materials and have excellent residual effects on wood and soil. The compounds of the present invention may possess good characteristics in terms of application rate, residual formulation, selectivity, toxicity, production method, high activity, wide range of control, safety, and resistant organisms (for example, organophosphorus agents and/or Or the control of a drug-resistant pest of a urethane agent.
以下將描述更多本發明之具體實例。 More specific examples of the invention will be described below.
具有式(I)的化合物可用於對抗和控制蟲害的侵擾,如鳞翅目、雙翅目、半翅目、纓翅目、直翅目、網翅目、鞘 翅目、蚤目、膜翅目和等翅目等有害生物,以及其他的無脊椎有害生物,例如蟎、線蟲及軟體動物有害生物等。以下將昆蟲、蟎、線蟲及軟體動物有害生物統稱為有害生物。這些可利用本化合物發明對抗和控制的有害生物包括:涉及農業(涵意包括種植有關食物和纖維性產品的作物)、園藝、畜牧、伴侶(companion)動物、林業與植蔬原料產品(例如水果、縠物及木材)之儲藏者;涉及毀損人造結構和傳播人畜疾病者;以及騷擾性有害生物(例如蒼蠅)。 Compounds of formula (I) are useful for combating and controlling pest infestation, such as Lepidoptera, Diptera, Hemiptera, Thysanoptera, Orthoptera, Nettle, Sheath Pests such as Hymenoptera, Hymenoptera, Hymenoptera, and Isoptera, and other invertebrate pests such as ticks, nematodes, and mollusc pests. Insects, mites, nematodes, and mollusc pests are collectively referred to as pests. These pests that can be used to combat and control using this compound include: agriculture (meaning crops that include food and fiber products), horticulture, livestock, companion animals, forestry and vegetable raw materials (such as fruits) Warehousing of sputum, timber and wood; involved in the destruction of man-made structures and the spread of human and animal diseases; and harassing pests (such as flies).
例如,本發明的化合物可用於草皮、觀賞植物(例如花卉、灌木、闊葉樹或如針葉樹等常綠植物),以及為樹注射、蟲害管理等。 For example, the compounds of the present invention can be used for turf, ornamental plants (e.g., flowers, shrubs, broadleaf trees, or evergreen plants such as conifers), as well as for tree injection, pest management, and the like.
本發明的化合物可用於控制動物居家有害生物,其中包括:螞蟻、臭蟲(成蟲)、蜜蜂、甲蟲、梣葉槭蝽(Boxelder Bugs)、木匠蜂、地毯甲蟲、蜈蚣、煙草甲蟲、三葉草蟎、蟑螂、扁擬縠盜(Confused Flour Beetle)、蟋蟀、蠼螋(Earwigs)、家衣魚(Firebrats)、跳蚤、蒼蠅、擬縠盜(Lesser Grain Borers)、千足蟲、蚊子、赤擬穀盜、稻象鼻蟲(Rice Weevils)、鋸胸穀盜、衣魚(Silverfish)、蛜蛾(Sowbugs)、蜘蛛、白蟻、壁虱、黃蜂、蟑螂、蟋蟀、蒼蠅、小甲蟲(如擬步甲蟲、隱蔽甲蟲和食腐甲蟲肉)、蚊子、潮蟲、蝎子、蜘蛛、葉蟎(二點葉蟎、無爪小爪蟎)。 The compounds of the present invention are useful for controlling animal home pests, including: ants, bed bugs (adults), bees, beetles, boxelder Bugs, carpenter bees, carpet beetles, cockroaches, tobacco beetles, clover cockroaches, cockroaches Confused Flour Beetle, Earwigs, Firebrats, Fleas, Flies, Lesser Grain Borers, Millipedes, Mosquitoes, Red Valley Pirates, Rice Rice Weevils, Sawgrass, Silverfish, Sowbugs, Spiders, Termites, Ticks, Wasps, Storks, Storks, Flies, Small Beetles (Pseudo-Beetles, Concealed Beetles) And scavenger beetle), mosquitoes, worms, scorpions, spiders, spider mites (two-pointed spider mites, non-clawed scorpion scorpions).
本發明之化合物可用於控制觀賞植物性有害生物,其中包括:螞蟻(包括外來火蟻)、斜紋夜蛾(Armyworms)、杜鵑花毛蟲(Azalea caterpillar)、蚜蟲、邂債蛾(Bagworms)、 黑藤象鼻蟲(Black vine weevils)(成蟲)、梣葉槭蝽(Boxelder bugs)、食心蟲(Budworms)、加州橡木蟲(California oakworm)、尺蠼(Cankerworms)、蟑螂、蟋蟀、夜盜蟲、東方天幕毛蟲、榆葉甲(Elm leaf beetles)、歐洲鋸蜂(European sawflies)、秋幕毛蟲(Fall webworms)、跳甲(Flea beetles)、森林天幕毛蟲、舞毒蛾幼蟲(Gypsy moth larvae)、日本甲蟲(成蟲)、六月甲蟲(成蟲)、網蝽(Lace bugs)、食葉性毛蟲、葉蟬(Leafhoppers)、斑潛蠅(成蟲)、捲葉蛾(Leaf rollers)、雕葉蟲(Leaf skeletonizers)、糠蚊(Midges)、蚊子、夾竹桃蛾幼蟲(Oleander moth larvae)、潮蟲(Pillbugs)、松葉蜂(Pine sawflies)、杉切梢小蠹(Pine shoot beetles)、松梢蛾(Pinetip moths)、盲蝽(Plant bugs)、根象鼻蟲(Root weevils)、葉蜂(Sawflies)、介殼蟲(Scale insects)(爬蟲)、蜘蛛、沬蟬(Spittlebugs)、條紋甲蟲、條紋橡樹蟲、薊馬、Tip moth、毒蛾幼蟲(Tussock moth larvae)、黃蜂、茶細蟎(Broadmites)、褐軟蚧(Brown softscales)、紅圓蚧(California redscales)(爬蟲)、苜蓿紅蜘蛛(Clover mites)、粉蚧(Mealybugs)、松梢蚧(Pineneedlescales)(爬蟲)、葉蟎(Spider mites)、粉虱(Whiteflies)。 The compounds of the present invention are useful for controlling ornamental plant pests, including: ants (including exotic fire ants), armyworms, Azalea caterpillar, aphids, and bagworms. Black vine weevils (adults), Boxelder bugs, Budworms, California oakworms, Cankerworms, crickets, crickets, night worms, Oriental sky caterpillar, Elm leaf beetles, European sawflies, Fall webworms, Flea beetles, forest caterpillars, Gypsy moth larvae, Japan Beetle (adult), June beetle (adult), Lace bugs, leaf-feeding caterpillar, Leafhoppers, Liriomyza (adult), Leaf rollers, Leaf skeletonizers , Midges, mosquitoes, Oleander moth larvae, Pillbugs, Pine sawflies, Pine shoot beetles, Pinetip moths, Plant bugs, Root weevils, Sawflies, Scale insects (reptiles), spiders, Spittlebugs, striped beetles, striped oak worms, thrips, Tip moth, Tussock moth larvae, wasp, tea fine (Broadmite) s), Brown softscales, California redscales (reptiles), Clover mites, Mealybugs, Pineneedles (reptiles), spider mites (Spider) Mites), whiteflies.
本發明之化合物可用於控制草皮之有害生物,其中包括:螞蟻(包括外來火蟻)、斜紋夜蛾、蜈蚣、蟋蟀、夜盜蟲、蠼螋、跳蚤(成蟲)、草蜢、日本甲蟲(成蟲)、千足蟲、蟎蟲、蚊子(成蟲)、潮蟲、草地螟、蛜蛾、壁虱(包括傳播萊姆病的物種)、Bluegrass billbug(成蟲)、黑金龜子(成蟲)、恙蟎、 跳蚤(成蟲)、蠐螬(Grubs)(抑制)、象鼻蟲(Hyperodes weevils)(成蟲)、螻蛄(Mole Crickets)(蛹和年輕成蟲)、螻蛄(成熟成蟲)、麥虱(Chinch Bugs)。 The compounds of the present invention can be used to control pests of turf, including: ants (including exotic fire ants), Spodoptera litura, ticks, ticks, night larvae, crickets, fleas (adults), grass mites, Japanese beetles (adults) ), millipedes, mites, mosquitoes (adults), tide worms, grasshoppers, moths, ticks (including species that spread Lyme disease), Bluegrass billbug (adults), black chafers (adults), cockroaches, Fleas (adults), Grubs (inhibition), Hyodes weevils (adults), Mole Crickets (scorpion and young adults), ticks (mature adults), and Chinch Bugs.
具式(I)的化合物可控制之有害生物種類實例包括:桃蚜(Myzus persicae)、棉蚜(Aphis gossypii)、黑豆蚜(Aphis fabae)、盲蝽種(Lygus spp.)、盲蝽種(Dysdercus spp.)、蠟蟬(Nilaparvata lugens)、葉蟬(Nephotettixc incticeps)、稻綠蝽屬(Nezara spp.)、蝽象種(Euschistus spp.)、蛛緣蝽象種(Leptocorisa spp.)、西方花薊馬(Frankliniella occidentalis)、薊馬種(Thrips spp.)、科羅拉多馬鈴薯甲蟲(Leptinotarsa decemlineata)、棉鈴象鼻蟲(Anthonomus grandis)、介殼蟲種(Aonidiella spp.)、粉虱種(Trialeurodes spp.)、粉虱(Bemisia tabaci)、歐洲玉米螟(Ostrinia nubilalis)、棉樹葉蟲(Spodoptera littoralis)、菸夜蛾(Heliothis virescens)、棉鈴蟲(Helicoverpa armigera)、棉鈴蟲(Helicoverpa zea)、棉卷葉螟(Sylepta derogata)、粉蝶(Pieris brassicae)、小菜蛾(Plutella xylostella)、夜盜蟲(Agrotis spp.)、稻條螟(Chilo suppressalis)、飛蝗(Locusta migratoria)、蝗蟲(Chortiocetes terminifera)、根蟲種(Diabrotica spp.)、歐洲葉蟎(Panonychus ulmi)、柑桔葉蟎(Panonychus citri)、二點葉蟎(Tetranychus urticae)、赤葉蟎(Tetranychus cinnabarinus)、柑桔銹蟎(Phyllocoptruta oleivora)、茶細蟎(Polyphagotarsonemus latus)、葡萄短須蟎種(Brevipalpus spp.)、牛蜱(Boophilus microplus)、美國 犬壁虱(Dermacentor variabilis)、貓蚤(Ctenocephalides felis)、潛葉蟲種(Liriomyza spp.)、家蠅(Musca domestica)、埃及斑蚊(Aedes aegypti)、瘧蚊屬(Anopheles spp.)、家蚊屬(Culex spp.)、綠蠅種(Lucillia spp.)德國蟑螂(Blattella germanica)、美國蟑螂(Periplaneta americana)、東方蟑螂(Blatta orientalis)、澳白蟻科的白蟻(例如澳白蟻種(Mastotermes spp.))、木白蟻科的白蟻(例如新白蟻種(Neotermes spp.))、鼻白蟻科的白蟻(例如家白蟻(Coptotermes formosanus)、黃肢散白蟻(Reticulitermes flavipes)、R.speratu、R.virginicus、R.hesperus和R.santonensis),以及白蟻科的白蟻(例如黃球白蟻(Globitermes sulfureus))、火蟻(Solenopsis geminata)、法老家蟻(Monomorium pharaonis)、毛虱種(Damalinia spp.)及咬虱與吸吮虱種(Linognathus spp.)、根瘤線蟲種(Meloidogyne spp.)、黃金線蟲種(Globodera spp.)及胞囊線蟲種(Heterodera spp.)、根腐線蟲種(Pratylenchus spp.)、香蕉穿孔線蟲種(Rhodopholus spp.)、柑橘線蟲種(Tylenchulus spp.)、撚轉胃蟲(Haemonchus contortus)、醋線蟲(Caenorhabditis elegans)、消化道線蟲種(Trichostrongylus spp.)及蛞蝓(Deroceras reticulatum)。 Examples of pest species that can be controlled by compounds of formula (I) include: Myzus persicae , Aphis gossypii , Aphis fabae , Lygus spp., and blind mites ( Dysdercus spp.), Nilaparvata lugens , Nephotettixc incticeps , Nezara spp., Euschistus spp., Leptocorisa spp., Western Frankliniella occidentalis , Thrips spp., Leptinotarsa decemlineata , Anthonomus grandis , Aonidiella spp., Trialeurodes spp. ), Bemisia tabaci , Ostrinia nubilalis , Spodoptera littoralis , Heliothis virescens , Helicoverpa armigera , Helicoverpa zea , cotton leaf Sylepta derogata , Pieris brassicae , Plutella xylostella , Agrotis spp., Chilo suppressalis , Locusta migratoria , Chortiocetes terminifera , Diabrotica spp., Panonychus ulmi , Panonychus citri , Tetranychus urticae , Tetranychus cinnabarinus , mandarin Phyllocoptruta oleivora , Polyphagotarsonemus latus , Brevipalpus spp., Boophilus microplus , Dermacentor variabilis , Ctenocephalides felis , Liriomyza spp., Musca domestica , Aedes aegypti , Anopheles spp., Culex spp., Lucillia spp. ) German cockroach ( Blattella germanica ), American cockroach ( Periplaneta americana ), Oriental cockroach ( Blatta orientalis ), termites of the family Ants (such as Mastotermes spp.), termites of the wood termite family (eg new termite species ( Neotermes spp.)), termites of the family Termidae (eg Coptotermes formosanus , Reticulitermes flavipes , R. speratu , R. virginicus , R .hesperus and R. santonensis ), and termites of the termite family (eg, Globitermes sulfureus ), fire ants ( Solenopsis geminata ), primordial ants ( Monmorium pharaonis ), mites ( Dalalinia spp.) and biting Linognathus spp., Meloidogyne spp., Globodera spp. and Heterodera spp., root rot nematode ( Pratylushus spp.), banana perforated nematode Species ( Rhoodopholus spp.), Tylenchulus spp., Haemonchus contortus , Caenorhabditis elegans , Trichostrongylus spp., and Deroceras reticulatum .
本發明的化合物可用於控制在各類植物上的有害生物,這些植物包括大豆(例如,在某些情況下施用10-70克/公頃)、玉米(例如,在某些情況下施用10-70克/公頃)、甘蔗(例如,在某些情況下施用20-200克/公頃)、苜蓿(例 如,在某些情況下施用10-70克/公頃)、芸苔屬植物(brassicas)(例如,在某些情況下施用10-50克/公頃)、油菜(例如菜籽)(例如,在某些情況下施用20-70克/公頃)、馬鈴薯(包括甘薯)(例如,在某些情況下施用10-70克/公頃)、棉花(例如,在某些情況下施用10-70克/公頃)、稻米(例如,在某些情況下施用10-70克/公頃)、咖啡(例如,在某些情況下施用30-150克/公頃)、柑橘(例如,在某些情況下施用60-200克/公頃)、杏仁(例如,在某些情況下施用40-180克/公頃)、果菜類蔬菜(例如,番茄、胡椒、辣椒、茄子、小黃瓜、南瓜等)(例如,在某些情況下施用10-80克/公頃)、茶(例如,在某些情況下施用20-150克/公頃)、鱗莖類蔬菜(例如,洋蔥、韭蔥等)(例如,在某些情況下施用30-90克/公頃)、葡萄(例如,在某些情況下施用30-180克/公頃)、仁果類水果(例如,蘋果、梨子等)(例如,在某些情況下施用30-180克/公頃)、核果(例如,梨、李子等)(例如,在某些情況下施用30-180克/公頃)。 The compounds of the present invention are useful for controlling pests on a variety of plants, including soybeans (e.g., 10-70 grams per hectare in some cases), corn (e.g., in some cases 10-70) G/ha), sugar cane (for example, 20-200 g/ha in some cases), 苜蓿 (example) For example, in some cases 10-70 g/ha), Brassica (for example, 10-50 g/ha in some cases), canola (eg rapeseed) (for example, in In some cases 20-70 g/ha), potatoes (including sweet potatoes) (for example, 10-70 g/ha in some cases), cotton (for example, in some cases 10-70 g/ Haha), rice (for example, 10-70 g/ha in some cases), coffee (for example, 30-150 g/ha in some cases), citrus (for example, 60 in some cases) -200 g/ha), almonds (for example, 40-180 g/ha in some cases), fruits and vegetables (for example, tomatoes, peppers, peppers, eggplants, cucumbers, pumpkins, etc.) (for example, at some In some cases 10-80 g/ha), tea (for example, 20-150 g/ha in some cases), bulbous vegetables (eg, onions, leeks, etc.) (for example, in some cases Applying 30-90 g/ha), grapes (for example, 30-180 g/ha in some cases), pome fruit (eg, apples, pears, etc.) (eg, in some cases Use 30-180 g/ha), stone fruit (eg, pear, plum, etc.) (eg, 30-180 g/ha in some cases).
本發明的化合物可用於大豆,以控制諸如南美玉米苗斑螟(Elasmopalpus lignosellus)、阿根廷兜蟲(Diloboderus abderus)、南美葉甲(Diabrotica speciosa)、Sternechus subsignatus、蟻科(Formicidae)、小地老虎(Agrotis ypsilon)、筒馬陸種(Julus spp.)、黎豆夜蛾(Anticarsia gemmatalis)、Megascelis spp.、Procornitermes spp.、蛄螻科(Gryllotalpidae)、稻綠蝽(Nezara viridula)、壁蝽屬(Piezodorus spp.)、Acrosternum spp.、Neomegalotomus spp.、 豆葉甲(Cerotoma trifurcata)、日本金龜子(Popillia japonica)、Edessa spp.、Liogenys fuscus、Euchistus heros、鑽心蟲(stalk borer)、Scaptocoris castanea、鰓角金龜屬(Phyllophaga spp.)、大豆夜蛾(Pseudoplusia includens)、灰翅夜蛾屬(Spodoptera spp.)、菸草粉虱(Bemisia tabaci)、叩頭蟲種(Agriotes spp.)。本發明的化合物較佳用於大豆,以控制阿根廷兜蟲(Diloboderus abderus)、南美葉甲(Diabrotica speciosa)、稻綠蝽(Nezara viridula)、壁蝽種(Piezodorus spp.)、Acrosternum spp.、豆葉甲(Cerotoma trifurcata)、日本金龜子(Popillia japonica)、Euchistus heros、鰓角金龜屬(Phyllophaga spp.)、叩頭蟲種(Agriotes spp.)。 Compounds of the invention may be used in soy, such as to control the South American Maize seedlings Oligochroa (Elasmopalpus lignosellus), Argentina pocket insects (Diloboderus abderus), Diabrotica South America (Diabrotica speciosa), Sternechus subsignatus, Formicidae (Formicidae), black cutworm ( Agrotis ypsilon ), Julus spp., Anticarsia gemmatalis , Megascelis spp., Procornitermes spp., Gryllotalpidae , Nezara viridula , Piezodorus Spp .), Acrosternum spp., Neomegalotomus spp., Cerotoma trifurcata , Japanese cock ( Papiillia japonica ), Edessa spp., Liogenys fuscus , Euchistus heros , stalk borer, Scaptocoris castanea , horned tortoise Genus ( Phyllophaga spp.), Pseudoplusia includens , Spodoptera spp., Bemisia tabaci , Agriotes spp. The compounds of the present invention are preferably used in soybeans to control Diloboderus abderus , Diabrotica speciosa , Nezara viridula , Piezodorus spp., Acrosternum spp., beans. Cerotoma trifurcata , Japanese poplar ( Popillia japonica ), Euchistus heros , Phyllophaga spp., Agriotes spp.
本發明的化合物可用於玉米,以控制Euchistus heros、Dichelops furcatus、阿根廷兜蟲(Diloboderus abderus)、南美玉米苗斑螟(Elasmopalpus lignosellus)、草地貪夜蛾(Spodoptera frugiperda)、稻綠蝽(Nezara viridula)、豆葉甲(Cerotoma trifurcata)、日本金龜子(Popillia japonica)、小地老虎(Agrotis ypsilon)、南美葉甲(Diabrotica speciosa)、異翅亞目、Procornitermes spp.、Scaptocoris castanea、蟻科(Formicidae)、筒馬陸種(Julus spp.)、玉米黃翅葉蟬(Dalbulus maidis)、玉米根葉甲(Diabrotica virgifera)、Mocis latipes、菸草粉虱(Bemisia tabaci)、實夜蛾屬(heliothis spp.)、四爪蟎屬(Tetranychus spp.)、薊馬屬(Thrips spp.)、鰓角金龜屬(Phyllophaga spp.)、類盾臭蟲種(Scaptocoris spp.)、Liogenys fuscus、灰翅夜蛾屬(Spodoptera spp.)、桿野螟屬(Ostrinia spp.)、蛀莖夜蛾屬(Sesamia spp.)、叩頭蟲種(Agriotes spp.)。本發明物之化合物較佳用於玉米,以控制Euchistus heros、Dichelops furcatus、阿根廷兜蟲(Diloboderus abderus)、稻綠蝽(Nezara viridula)、豆葉甲(Cerotoma trifurcata)、日本金龜子(Popillia japonica)、南美葉甲(Diabrotica speciosa)、玉米根葉甲(Diabrotica virgifera)、四爪蟎屬(Tetranychus spp.)、薊馬屬(Thrips spp.)、鰓角金龜屬(Phyllophaga spp.)、類盾臭蟲種(Scaptocoris spp.)、叩頭蟲種(Agriotes spp.)。 The compounds of the present invention can be used in corn to control Euchitus heros , Dichelops furcatus , Diloboderus abderus , Elasmopalpus lignosellus , Spodoptera frugiperda , Nezara viridula , bean leaf beetle (Cerotoma trifurcata), Japan chafer (Popillia japonica), black cutworm (Agrotis ypsilon), the South American leaf beetle (Diabrotica speciosa), Heteroptera, Procornitermes spp., Scaptocoris castanea, Formicidae (Formicidae), Julus spp., Dalbulus maidis , Diabrotica virgifera , Mocis latipes , Bemisia tabaci , heliothis spp., four Tetranychus spp., Thrips spp., Phyllophaga spp., Scaptocoris spp., Liogenys fuscus , Spodoptera spp. ), Ostrinia spp., Sesamia spp., Agriotes spp. The compounds of the present invention are preferably used in corn to control Euchitus heros , Dichelops furcatus , Diloboderus abderus , Nezara viridula , Cerotoma trifurcata , Popillia japonica , Diabrotica speciosa , Diabrotica virgifera , Tetranychus spp., Thrips spp., Phyllophaga spp., Shield-like bug species ( Scaptocoris spp.), Agriotes spp.
本發明的化合物可用於甘蔗,以控制穀喙甲屬(Sphenophorus spp.)、白蟻、泡沫蟲種(Mahanarva spp.)等。本發明的化合物較佳用於甘蔗,以控制白蟻、泡沫蟲種(Mahanarva spp.)。 The compounds of the present invention are useful in sugar cane to control Sphenophorus spp., termites, Mahanarva spp., and the like. The compounds of the invention are preferably used in sugar cane to control termites, Mahanarva spp.
本發明的化合物可用於紫花苜蓿,以控制諸如埃及苜蓿象甲(Hypera brunneipennis)、苜蓿象鼻蟲(Hypera postica)、苜蓿毛蟲(Colias eurytheme)、Collops spp.、Empoasca solana、跳甲(Epitrix)、大眼長蝽屬(Geocoris spp.)、豆莢盲蝽(Lygus hesperus)、牧草盲蝽(Lygus lineolaris)、Spissistilus spp、灰翅夜蛾屬(Spodoptera spp.)、粉紋夜蛾(Trichoplusia ni)。本發明的化合物較佳用於紫花苜蓿,以控制埃及苜蓿象甲(Hypera brunneipennis)、苜蓿象鼻蟲(Hypera postica)、Empoasca solana、跳甲(Epitrix)、豆莢盲蝽(Lygus hesperus)、牧草盲蝽(Lygus lineolaris)、粉紋 夜蛾(Trichoplusia ni)。 The compounds of the invention can be used in alfalfa to control, for example, Hypera brunneipennis , Hypera postica , Colias eurytheme , Collops spp., Empoasca solana, Epitrix , Geocoris spp., Lygus hesperus , Lygus lineolaris , Spissistilus spp, Spodoptera spp., Trichoplusia ni . The compounds of the present invention are preferably used in alfalfa to control Hypera brunneipennis , Hypera postica , Empoasca solana , Epitrix , Lygus hesperus , and pasture blindness. Lygus lineolaris , Trichoplusia ni .
本發明的化合物可用於芸苔屬植物,以控制諸如小菜蛾(Plutella xylostella)、馬醉木屬(Pieris spp.)、甘藍夜蛾屬(Mamestra spp.)、Plusia spp.、粉紋夜蛾(Trichoplusia ni)、條跳甲屬(Phyllotreta spp.)、灰翅夜蛾屬(Spodoptera spp.)、Empoasca solana、薊馬屬(Thrips spp.)、灰翅夜蛾屬(Spodoptera spp.)、地種蠅屬(Delia spp.)。本發明的化合物最適合用於芸苔屬植物,以控制小菜蛾(Plutella xylostella)、馬醉木屬(Pieris spp.)、Plusia spp.、粉紋夜蛾(Trichoplusia ni)、條跳甲屬(Phyllotreta spp.)、薊馬屬(Thrips spp.)。 The compounds of the present invention can be used in Brassica plants to control, for example, Plutella xylostella , Pieris spp., Mamestra spp., Plusia spp., Trichoplusia ni ), Phyllotreta spp., Spodoptera spp., Empoasca solana , Thrips spp., Spodoptera spp., Spodoptera spp. ( Delia spp.). The compounds of the present invention are most suitable for use in Brassica plants to control Plutella xylostella , Pieris spp., Plusia spp., Trichoplusia ni , Phyllotreta spp. ), Thrips spp.
本發明的化合物可用於如芥花等芸苔,以控制諸如露尾甲屬(Meligethes spp.)、Ceutorhynchus napi、裸蛛甲(Psylloides spp.)。 The compounds of the present invention are useful in canola such as canola to control, for example, Meligethes spp., Ceutorhynchus napi , Psylloides spp.
本發明的化合物可用於馬鈴薯(包括甘薯),以控制諸如葉蟬種(Empoasca spp.)、馬鈴薯葉甲屬(Leptinotarsa spp.)、南美葉甲(Diabrotica speciosa)、枸杞蛀果蛾屬(Phthorimaea spp.)、Paratrioza spp.、鰓金龜(Maladera matrida)、叩頭蟲種(Agriotes spp.)。本發明的化合物較佳用於馬鈴薯(包括甘薯),以控制葉蟬種(Empoasca spp.)、馬鈴薯葉甲屬(Leptinotarsa spp.)、南美葉甲(Diabrotica speciosa)、枸杞蛀果蛾屬(Phthorimaea spp.)、Paratrioza spp.、叩頭蟲種(Agriotes spp.)。 The compounds of the present invention are useful in potato (including sweet potato) to control, for example, the genus Empoasca spp., the genus Leptinotarsa spp., the genus Diabrotica speciosa , and the genus Phthorimaea spp. .), Paratrioza spp., Maladera matrida , Agriotes spp. Preferred compounds of the invention for potato (including sweet), to control the species leafhopper (Empoasca spp.), Colorado potato beetle genus (Leptinotarsa spp.), Leaf beetle America (Diabrotica speciosa), the genus wolfberry fruit moth (Phthorimaea Spp .), Paratrioza spp., Agriotes spp.
本發明的化合物可用於棉花,以控制諸如棉鈴象鼻蟲 (Anthonomus grandis)、棉紅鈴蟲屬(Pectinophora spp.)、實夜蛾屬(Heliothis spp.)、灰翅夜蛾屬(Spodoptera spp.)、四爪蟎屬(Tetranychus spp.)、葉蟬種(Empoasca spp.)、薊馬屬(Thrips spp.)、菸草粉虱(Bemisia tabaci)、草盲蝽種(Lygus spp.)、鰓角金龜屬(Phyllophaga spp.)、類盾臭蟲種(Scaptocoris spp.)。本發明的化合物較佳用於棉花,以控制棉鈴象鼻蟲(Anthonomus grandis)、四爪蟎屬(Tetranychus spp.)、葉蟬種(Empoasca spp.)、薊馬屬(Thrips spp.)、草盲蝽種(Lygus spp.)、鰓角金龜屬(phyllophaga spp.)、類盾臭蟲種(Scaptocoris spp.)。 The compounds of the present invention are useful in cotton to control, for example, Anthonomus grandis , Pectinophora spp., Heliothis spp., Spodoptera spp. ), Tetranychus spp., Empoasca spp., Thrips spp., Bemisia tabaci , Lygus spp., horns Phyllophaga spp., Scaptocoris spp. Compounds of the invention preferred for cotton, to control the cotton boll weevil (Anthonomus grandis), the genus Tetranychus (Tetranychus spp.), Species leafhopper (Empoasca spp.), Thrips (Thrips spp.), Oxalyl seed bugs (Lygus spp.), the genus gill angle beetle (phyllophaga spp.), species of class shield bug (Scaptocoris spp.).
本發明的化合物可用於水稻,以控制諸如稻緣蝽種(Leptocorisa spp.)、Cnaphalocrosis spp.、螟屬(Chilo spp.)、草螟蛾屬(Scirpophaga spp.)、Lissorhoptrus spp.、美洲稻盾(Oebalus pugnax)。本發明的化合物較佳用於水稻,以控制稻緣蝽種(Leptocorisa spp.)、Lissorhoptrus spp.、美洲稻盾(Oebalus pugnax)。 The compounds of the present invention can be used in rice to control such as Leptocorisa spp., Cnaphalocrosis spp., Chilo spp., Scirpophaga spp., Lissorhoptrus spp. ( Oebalus pugnax ). The compounds of the present invention are preferably used in rice to control Leptocorisa spp., Lissorhoptrus spp., and Oebalus pugnax .
本發明的化合物可用於咖啡,以控制諸如咖啡果小蠹(Hypothenemus Hampei)、咖啡潛葉蛾(Perileucoptera Coffeella)、四爪蟎屬(Tetranychus spp.)。本發明的化合物可用於咖啡,以控制咖啡果小蠹(Hypothenemus Hampei)、咖啡潛葉蛾(Perileucoptera Coffeella)。 The compounds of the present invention are useful in coffee to control, for example, Hypothenemus Hampei , Perileucoptera Coffeella , Tetranychus spp. The compounds of the present invention are useful in coffee to control Hypothenemus Hampei , Perileucoptera Coffeella .
本發明的化合物可用於柑橘,以控制諸如柑桔葉蟎(Panonychus citri)、柑桔銹蟎(Phyllocoptruta oleivora)、葡萄短須蟎種(Brevipalpus spp.)、木虱(Diaphorina citri)、跳 薊馬屬(Scirtothrips spp.)、薊馬屬(Thrips spp.)、矢尖蚧屬(Unaspis spp.)、地中海果實蠅(Cerstitis capitata)、潛葉蛾屬(Phyllocnistis spp.)。本發明的化合物較佳用於柑橘,以控制柑桔葉蟎(Panonychus citri)、柑桔銹蟎(Phyllocoptruta oleivora)、葡萄短鬚蟎(Brevipalpus spp.)、柑橘木虱(Diaphorina citri)、跳薊馬屬(Scirtothrips spp.)、薊馬屬(Thrips spp.)、Phyllocnistis spp.。 The compounds of the present invention can be used in citrus to control, for example, Panonychus citri , citrus rust ( Phyllocoptruta oleivora ), Brevipalpus spp., Diaphorina citri , flea horse Genus ( Scirtothrips spp.), Thrips spp., Unaspis spp., Cerstitis capitata , Phyllocnistis spp. The compounds of the present invention are preferably used in citrus to control Panonychus citri , citrus rust ( Philyllocoptruta oleivora ), Brevipalpus spp., Diaphorina citri , flea Scirtothrips spp., Thrips spp., Phyllocnistis spp.
本發明的化合物可用於杏仁,以控制諸如臍橙螟(Amyelois transitella)、四爪蟎屬(etranychus spp.)。 The compounds of the invention are useful in almonds to control, for example, Amyelois transitella , etranychus spp.
本發明的化合物可用於果菜類蔬菜,其中包括番茄、胡椒、辣椒、茄子、小黃瓜、南瓜等,以控制薊馬屬(Thrips spp.)、四爪蟎屬(Tetranychus spp.)、茶細蟎屬(Polyphagotarsonemus spp.)、刺皮節蜱屬(Aculops spp.)、葉蟬種(Empoasca spp.)、灰翅夜蛾屬(Spodoptera spp.)、實夜蛾屬(heliothis spp.)、斑潛蠅(Tuta absoluta)、斑潛蠅種(Liriomyza spp.)、菸草粉虱(Bemisia tabaci)、粉虱屬(Trialeurodes spp.)、Paratrioza spp.、西方花薊馬(Frankliniella occidentalis、Frankliniella spp.、Anthonomus spp.、條跳甲屬(Phyllotreta spp.)、Amrasca spp.、瓢蟲屬(Epilachna spp.)、Halyomorpha spp.、跳薊馬屬(Scirtothrips spp.)、螟蛾屬(Leucinodes spp.)、Neoleucinodes spp.。本發明的化合物較佳用於果菜類蔬菜,其中包括番茄、胡椒、辣椒、茄子、小黃瓜、南瓜等,以控制諸如薊馬屬(Thrips spp.)、四爪蟎屬(Tetranychus spp.)、茶細蟎屬 (Polyphagotarsonemus spp.)、刺皮節蜱屬(Aculops spp.)、葉蟬種(Empoasca spp.)、灰翅夜蛾屬(Spodoptera spp.)、實夜蛾屬(heliothis spp.)、斑潛蠅(Tuta absoluta)、斑潛蠅種(Liriomyza spp.)、Paratrioza spp.、西方花薊馬(Frankliniella occidentalis)、Frankliniella spp.、Amrasca spp.、跳薊馬屬(Scirtothrips spp.)、螟蛾屬(Leucinodes spp.)、Neoleucinodes spp.。 The compound of the present invention can be used for fruits and vegetables, including tomatoes, peppers, peppers, eggplants, cucumbers, pumpkins, etc., to control Thrips spp., Tetranychus spp., tea fines. Genus ( Polyphagotarsonemus spp.), Aculops spp., Empoasca spp., Spodoptera spp., heliothis spp. flies (Tuta absoluta), species of leafminer (Liriomyza spp.), silverleaf whitefly (Bemisia tabaci), is a whitefly (Trialeurodes spp.), Paratrioza spp ., western flower thrips (Frankliniella occidentalis, Frankliniella spp., Anthonomus Spp ., Phyllotreta spp., Amrasca spp., Epilachna spp., Halyomorpha spp., Scirtothrips spp., Leucinodes spp., Neoleucinodes The compound of the present invention is preferably used for fruits and vegetables, including tomatoes, peppers, peppers, eggplants, gherkins, pumpkins, etc., to control, for example, Thrips spp., Tetraychus spp .), Tea genus ( Polyphago) Tarsonemus spp.), Aculops spp., Empoasca spp., Spodoptera spp., heliothis spp., Liriomyza spp. Tuta absoluta), species of leafminer (Liriomyza spp.), Paratrioza spp ., western flower thrips (Frankliniella occidentalis), Frankliniella spp. , Amrasca spp., thrips jump (Scirtothrips spp.), Minge genus (Leucinodes Spp .), Neoleucinodes spp.
本發明的化合物可用於茶類,以控制諸如白盾蚧屬(Pseudaulacaspis spp.)、葉蟬種(Empoasca spp.)、跳薊馬屬(Scirtothrips spp.)、茶細蛾(Caloptilia theivora)。本發明的化合物較佳用於茶類,以控制葉蟬種(Empoasca spp.)、跳薊馬屬(Scirtothrips spp.)。 The compounds of the present invention can be used in teas to control, for example, Pseudaulacaspis spp., Empoasca spp., Scirtothrips spp., Caloptilia theivora . The compounds of the invention are preferably used in teas to control the genus Empoasca spp., Scirtothrips spp.
本發明的化合物可用於鱗莖類蔬菜(包括洋蔥、韭蔥等),以控制諸如薊馬屬(Thrips spp.)、灰翅夜蛾屬(Spodoptera spp.)、實夜蛾屬(Heliothis spp.)。本發明的化合物較佳用於鱗莖類蔬菜(包括洋蔥、韭蔥等),以控制薊馬屬(Thrips spp.)。 The compounds of the present invention are useful for bulbous vegetables (including onions, leeks, etc.) to control, for example, Thrips spp., Spodoptera spp., Heliothis spp. . The compounds of the invention are preferably used in bulbous vegetables (including onions, leeks, etc.) to control Thrips spp.
本發明的化合物可用於葡萄,以控制諸如葉蟬種(Empoasca spp.)、花翅小卷蛾屬(Lobesia spp.)、Frankliniella spp.、薊馬屬(Thrips spp.)、四爪蟎屬(Tetranychus spp.)、腹鉤薊馬(Rhipiphorothrips Cruentatus)、Eotetranychus Willamettei、葡萄園葉蟬(Erythroneura Elegantula)、Scaphoides spp.。本發明的化合物較佳用於葡萄,以控制Frankliniella spp.、薊馬屬(Thrips spp.)、四爪蟎屬 (Tetranychus spp.)、腹鉤薊馬(Rhipiphorothrips Cruentatus)、Scaphoides spp.。 Compounds of the invention can be used in grapes, such as to control the species leafhopper (Empoasca spp.), Flowers genus wings pomonella (Lobesia spp.), Frankliniella spp ., Thrips (Thrips spp.), Tetranychus genus ( Tetranychus spp.), Rhipiphorothrips Cruentatus , Eotetranychus Willamettei , Erythroneura Elegantula , Scaphoides spp. The compounds of the invention are preferably used in grapes to control Frankliniella spp., Thrips spp., Tetranychus spp., Rhipiphorothrips Cruentatus , Scaphoides spp.
本發明的化合物可用於仁果類水果(包括蘋果、梨子等),以控制諸如Cacopsylla spp.、木虱種(Psylla spp.)、蘋果全爪蟎(Panonychus ulmi)、蘋果蠢蛾(Cydia pomonella)。本發明的化合物較佳用於仁果類水果(包括蘋果、梨子等),以控制Cacopsylla spp.、木虱種(Psylla spp.)、蘋果全爪蟎(Panonychus ulmi)。 The compounds of the present invention can be used in pome fruits (including apples, pears, etc.) to control such as Cacopsylla spp., Psylla spp., Panonychus ulmi , Cydia pomonella . . The compounds of the present invention are preferably used in pome fruit (including apples, pears, etc.) to control Cacopsylla spp., Psylla spp., and Panonychus ulmi .
本發明的化合物可用於核果類,以控制諸如梨小食心蟲(Grapholita molesta)、跳薊馬屬(Scirtothrips spp.)、薊馬屬(Thrips spp.)、Frankliniella spp.、四爪蟎屬(Tetranychus spp.)。本發明之化合物較佳用於核果,以控制跳薊馬屬(Scirtothrips spp.)、薊馬屬(Thrips spp.)、Frankliniella spp.、四爪蟎屬(Tetranychus spp.)。因此,本發明可提供一種對抗及/或控制動物性有害生物的方法,如無脊椎動物性有害生物,該方法包括將殺有害生物有效量的式(I)化合物,施用於有害生物、其所在之處或易受有害生物侵害之植物。尤其,本發明提供一種對抗及/或控制昆蟲、蟎、線蟲或軟體動物的方法,亦即將殺蟲、殺蟎、殺線蟲或殺軟體動物有效量的式(I)化合物,或含有式(I)化合物的組成物,施於有害生物、其所在之處(較佳為植物)或容易受有害生物侵害的植物上。式(I)化合物較佳用來對抗昆蟲、蟎或線蟲。 The compounds of the present invention can be used in stone fruits to control, for example, Grapholita molesta , Scirtothrips spp., Thrips spp., Frankliniella spp., Tetraychus spp .). The compounds of the invention are preferably used in stone fruit to control Scirtothrips spp., Thrips spp., Frankliniella spp., Tetranychus spp. Accordingly, the present invention may provide a method of combating and/or controlling an animal pest, such as an invertebrate pest, the method comprising applying a pesticidally effective amount of a compound of formula (I) to a pest, where Or a plant that is susceptible to pests. In particular, the present invention provides a method of combating and/or controlling insects, mites, nematodes or molluscs, i.e., an insecticidally, acaricidal, nematicidally or molluscicially effective amount of a compound of formula (I), or a formula (I) A composition of a compound applied to a pest, where it is (preferably a plant) or a plant susceptible to pests. The compounds of formula (I) are preferably used against insects, mites or nematodes.
此處使用的「植物」一詞包括幼苗、灌木及樹木。應 瞭解,作物亦包括已藉由習知培育方法或基因工程技術而對除草劑或各類除草劑(如ALS抑制劑、GS抑制劑、EPSPS抑制劑、PPO抑制劑與HPPD抑制劑)具耐藥性之作物。已經有通過習知方法育種並對咪唑啉酮(如甲氧咪草煙(imazamox))產生耐藥性之作物實例,名為Clearfield®夏季油菜(芥花)。在市場上,已經有通過基因工程方法而對除草劑產生耐藥性的農作物實例,包括如針對草甘膦和草銨膦具有耐藥性的市售玉米品種,產品名稱為RoundupReady®和LibertyLink®。 The term "plant" as used herein includes seedlings, shrubs and trees. should Understand that crops also include resistance to herbicides or various herbicides (eg ALS inhibitors, GS inhibitors, EPSPS inhibitors, PPO inhibitors and HPPD inhibitors) by conventional breeding methods or genetic engineering techniques. Sex crops. There have been examples of crops that have been bred by conventional methods and are resistant to imidazolinones such as imazamox, known as Clearfield® summer rape (canola). In the market, there are already examples of crops that are resistant to herbicides by genetic engineering methods, including commercially available corn varieties that are resistant to glyphosate and glufosinate, under the product names RoundupReady® and LibertyLink®. .
所謂的作物,也可以是那些已藉由基因工程技術而對有害生物具抗性的作物,例如Bt玉米(可抗歐洲玉米螟)、Bt棉花(可抗棉鈴象鼻蟲)及Bt馬鈴薯(可抗科羅拉多甲蟲)。Bt玉米的例子有NK®牌Bt 176玉米混種(Syngenta Seeds)。基因轉殖植物的例子有KnockOut®(玉米)、Yield Gard®(玉米)、NuCOTIN33B®(棉花)、Bollgard®(棉花)、NewLeaf®(馬鈴薯)、NatureGard®及Protexcta,這些植物有一個或更多個基因編碼了殺蟲抵抗性,並釋出一種或更多種毒性。因此,植物性作物或種子材料能同時抵抗除草劑和昆蟲啃食(疊加型(stacked)基因轉殖事件)。例如,種子能釋出一種可殺蟲的Cry3蛋白質,同時能耐受草甘膦。 The so-called crops can also be those that have been resistant to pests by genetic engineering techniques, such as Bt corn (resistant to European corn borer), Bt cotton (resistant to cotton boll weevil) and Bt potato (can Anti-Colorado beetle). An example of Bt corn is the NK® brand Bt 176 Corn Mix (Syngenta Seeds). Examples of genetically modified plants are KnockOut® (corn), Yield Gard® (corn), NuCOTIN 33B® (cotton), Bollgard® (cotton), NewLeaf® (potato), NatureGard® and Protexcta, one or more of these plants. The genes encode insecticidal resistance and release one or more toxicities. Therefore, plant crops or seed materials can simultaneously resist herbicides and insect foraging (stacked gene transfer events). For example, seeds can release a pesticidal Cry3 protein while being tolerant to glyphosate.
作物也應被理解為那些藉由習知培育方法或基因工程技術而取得的作物,以及那些含有所謂輸出性狀(如更佳的儲存穩定性、更高的營養價值及更好的滋味)的作物。 Crops should also be understood as crops obtained by conventional breeding methods or genetic engineering techniques, as well as crops containing so-called export traits such as better storage stability, higher nutritional value and better taste. .
為了將式(I)化合物作為殺蟲劑、殺蟎劑、殺線蟲或殺 軟體動物劑,以施用於有害生物、其所在之處或易受有害生物侵害之植物,通常會將式(I)的化合物配製成納入了以下項目的組成物:除了式(I)化合物本身,合適的惰性稀釋劑或載體,及選擇性納入表面活性劑(SFA)。SFA這種化學品,能夠降低界面張力而藉此引發其他特性(例如分散性、乳化性及濕性)產生變化,以修正某個界面(例如液體/固體、液體/空氣或液體/液體界面)的特性。所有組成物(固體和液體調配物)較佳包含(按重量計)0.0001至95%,更佳1至85%,例如5至60%的式(I)化合物。此組成物一般用於控制有害生物,而式(I)化合物的施用率是從每公頃0.1公克至10公斤,較佳每公頃1公克至6公斤,更佳為每公頃1公克至1公斤。 In order to use the compound of formula (I) as an insecticide, acaricide, nematicide or kill A mollusc agent, which is applied to a pest, where it is located, or susceptible to pests, typically formulating a compound of formula (I) into a composition incorporating the following: in addition to the compound of formula (I) itself A suitable inert diluent or carrier, and optionally a surfactant (SFA). SFA, a chemical that reduces interfacial tension and thereby induces changes in other properties (such as dispersibility, emulsifying, and wet) to modify an interface (eg, liquid/solid, liquid/air or liquid/liquid interface) Characteristics. All compositions (solid and liquid formulations) preferably comprise (by weight) from 0.0001 to 95%, more preferably from 1 to 85%, for example from 5 to 60%, of the compound of formula (I). The composition is generally used for controlling pests, and the application rate of the compound of the formula (I) is from 0.1 to 10 kg per hectare, preferably from 1 to 6 kg per hectare, more preferably from 1 to 1 kg per hectare.
若用於種子敷料(seed dressing),式(I)化合物的施用率一般每公斤種子是從0.0001公克至10公克(例如0.001公克或0.05公克),較佳0.005公克至10公克,更佳為0.005公克至4公克。 If used in seed dressing, the application rate of the compound of formula (I) is generally from 0.0001 g to 10 g (e.g., 0.001 g or 0.05 g) per kg of seed, preferably from 0.005 g to 10 g, more preferably 0.005. Gram to 4 grams.
本發明另一態樣提供一種包含殺有害生物有效量的式(I)化合物之組成物,尤其是包含殺蟲、殺蟎、殺線蟲或殺軟體動物有效量的式(I)化合物以及其合適的載體或稀釋劑的殺蟲、殺蟎、殺線蟲或殺軟體動物之組成物。此組成物較佳為殺蟲、殺蟎、殺線蟲或殺軟體動物組成物。 Another aspect of the invention provides a composition comprising a pesticidally effective amount of a compound of formula (I), especially an insectic, acaricidal, nematicidally or molluscicidal effective amount of a compound of formula (I) and suitable A carrier or diluent for the composition of insecticidal, acaricidal, nematicidal or molluscicidal animals. Preferably, the composition is a pesticidal, acaricidal, nematicidal or molluscicidal composition.
此組成物可從一些調配物類型中選擇,其中包括粉劑(DP)、可溶性粉劑(SP)、水溶性粒劑(SG)、水分散粒劑(WG)、可溼性粉劑(WP)、粒劑(GR)(緩慢或快速釋放)、可 溶性濃縮物(SL)、油溶性液劑(OL)、超低容量液劑(UL)、乳化濃縮物(EC)、可分散濃縮物(DC)、乳劑(水包油(EW)和油包水(EO))、微乳劑(ME)、懸浮液濃縮物(SC)、氣溶膠、霧化/煙霧調配物、膠囊懸浮液(CS)和種子處理調配物。在任何實例中選擇的調配物類型將視特定的設想目的而定,以及式(I)化合物之物理、化學與生物特性而定。 The composition can be selected from a number of formulation types including powder (DP), soluble powder (SP), water soluble granules (SG), water dispersible granules (WG), wettable powders (WP), granules. Agent (GR) (slow or fast release), available Soluble concentrate (SL), oil soluble liquid (OL), ultra low volume liquid (UL), emulsified concentrate (EC), dispersible concentrate (DC), emulsion (water in oil (EW) and oil package Water (EO)), microemulsion (ME), suspension concentrate (SC), aerosol, nebulization/smoke formulation, capsule suspension (CS) and seed treatment formulations. The type of formulation selected in any of the examples will depend on the particular intended purpose, as well as the physical, chemical, and biological properties of the compound of formula (I).
可藉由以下方式備製粉劑(DP):將式(I)化合物與一種或多種固體稀釋劑(例如天然黏土、高嶺土、葉蠟石、膨潤土、礬土、蒙脫土,矽藻土、白堊、矽藻土、磷酸鈣、碳酸鈣、碳酸鎂、硫、石灰,麵粉,滑石和其他有機與無機固體載體)混合,並機械式地將此混合物磨成細粉。 A powder (DP) can be prepared by reacting a compound of formula (I) with one or more solid diluents (eg, natural clay, kaolin, pyrophyllite, bentonite, alumina, montmorillonite, diatomaceous earth, chalk). Mixing diatomaceous earth, calcium phosphate, calcium carbonate, magnesium carbonate, sulfur, lime, flour, talc and other organic and inorganic solid carriers, and mechanically grinding the mixture into a fine powder.
可藉由將式(I)化合物與一個或多個可溶於水的無機鹽(例如碳酸氫鈉、碳酸鈉或硫酸鎂)混合,或和一個或多個水溶性有機固體(例如多醣)混合,以及選擇性地與一個或多個潤濕劑混合、與一個或多個分散劑混合,或與潤濕劑和分散劑的混合物來混合以改善水分散性/溶解性,來製備可溶性粉劑(SP)。接著再將此混合物磨成細粉。亦可將類似的組成物製成粒狀以形成水溶性粒劑(SG)。 By mixing a compound of formula (I) with one or more water-soluble inorganic salts such as sodium bicarbonate, sodium carbonate or magnesium sulfate, or with one or more water-soluble organic solids such as polysaccharides Preparing a soluble powder by selectively mixing with one or more wetting agents, mixing with one or more dispersing agents, or mixing with a mixture of wetting agents and dispersing agents to improve water dispersibility/solubility ( SP). This mixture is then ground to a fine powder. Similar compositions can also be granulated to form water soluble granules (SG).
可藉由將式(I)化合物與一種或多種固體稀釋劑或載體、一種或多種濕潤劑(以及較佳一種或多種分散劑)混合,並選擇性加入一種或多種懸浮液以促進於液體中的分散性,來備製可溼性粉劑(WP)。接著再將此混合物磨成細粉。亦可將類似的組成物製成粒狀以形成水分散粒劑(WG)。 By promoting the compound of formula (I) with one or more solid diluents or carriers, one or more wetting agents (and preferably one or more dispersing agents), and optionally one or more suspensions to facilitate in the liquid Dispersion to prepare wettable powder (WP). This mixture is then ground to a fine powder. Similar compositions can also be granulated to form a water dispersible granule (WG).
可利用兩種方式來形成粒劑(GR):將式(I)化合物與一 種或多種粉狀固體稀釋劑或載體,或來自預製之空白顆粒的混合物製成粒狀(藉著在多孔顆粒材料(例如浮石、厄帖浦土、漂白土、矽藻土或碎玉米棒)中吸收式(I)化合物(或其溶劑,在適合的試劑中吸收),來製成粒狀);或是在硬核材料(例如沙、矽酸鹽、礦物碳酸鹽、硫酸鹽或磷酸鹽)上吸收式(I)化合物(或其溶劑,在適合的試劑中吸收),並在必要時加以乾燥。通常用於輔助吸收或吸收的試劑,包括溶劑(例如脂族和芳香族石油溶劑、醇、醚、酮和酯)和黏著劑(例如聚醋酸乙烯酯、聚乙烯醇、糊精、糖和植物油)。粒劑中亦可包含一種或多種其他的添加劑(例如乳化劑、濕潤劑或分散劑)。 There are two ways to form a granule (GR): a compound of formula (I) a mixture of one or more powdered solid diluents or carriers, or from preformed blanks, in the form of granules (by means of porous particulate material (eg, pumice, erectite, bleaching earth, diatomaceous earth or ground corn cob) Intermediate absorption of a compound of formula (I) (or a solvent thereof, which is absorbed in a suitable reagent) to form a granule); or in a hard core material such as sand, citrate, mineral carbonate, sulfate or phosphate The compound of formula (I) (or its solvent, absorbed in a suitable reagent) is absorbed and dried if necessary. Reagents commonly used to aid absorption or absorption, including solvents (eg, aliphatic and aromatic petroleum solvents, alcohols, ethers, ketones, and esters) and adhesives (eg, polyvinyl acetate, polyvinyl alcohol, dextrin, sugar, and vegetable oils) ). One or more other additives (such as emulsifiers, wetting agents or dispersing agents) may also be included in the granules.
可利用將式(I)化合物溶於水或有機溶劑(例如酮、醇或乙二醇醚)的方式,來製備可分散濃縮物(DC)。這些溶液可包含表面活性劑(例如藉以改善水稀釋性或防止在噴霧罐中結晶)。 Dispersible concentrates (DC) can be prepared by dissolving the compound of formula (I) in water or an organic solvent such as a ketone, alcohol or glycol ether. These solutions may contain surfactants (for example to improve water dilution or to prevent crystallization in a spray can).
可藉由將式(I)化合物溶於有機溶劑(可選擇性包含一種或多種濕潤劑、一種或多種乳化劑或前述製劑的混合物),來製備乳化濃縮物(EC)或水包油型乳液(EW)。適合用於EC的有機溶劑包括芳香烴(例如烷基苯或烷基萘,例示於SOLVESSO 100、SOLVESSO 150和SOLVESSO 200;SOLVESSO是註冊商標)、酮類(例如環己酮或甲基環己酮)和醇類(如苯甲醇、糠醇或丁醇)、N-烷基吡咯啶酮(如N-甲基吡咯啶酮或N-辛基吡咯啶酮)、脂肪酸的二甲基醯胺(如C8-C10脂肪酸二甲基醯胺)和氯烴。EC產品於加水後,自 然便可乳化而產生具有足夠穩定性之乳劑,因而能藉由適當的設備噴灑。EW的製備包括取得液體形式的式(I)化合物(如果它在環境溫度下並非液體,則它可能會在一個合理的溫度下融化,一般是低於70℃),或是溶液形式的式(I)化合物(藉由將之溶解在適當的溶劑當中),然後在高剪切力下,將產生的液體或溶液在含有一個或多個SFAs的水中乳化,以製造乳劑。適用於EWs的溶劑包括植物油、氯烴(如氯苯)、芳香族溶劑(如烷基苯或烷基萘)及其他適當且水溶性低之有機溶劑。 An emulsified concentrate (EC) or an oil-in-water emulsion can be prepared by dissolving a compound of formula (I) in an organic solvent, optionally comprising one or more wetting agents, one or more emulsifiers or a mixture of the foregoing. (EW). Organic solvents suitable for use in EC include aromatic hydrocarbons (e.g., alkylbenzenes or alkylnaphthalenes, exemplified in SOLVESSO 100, SOLVESSO 150, and SOLVESSO 200; SOLVESSO is a registered trademark), ketones (e.g., cyclohexanone or methylcyclohexanone). And alcohols (such as benzyl alcohol, decyl or butanol), N-alkylpyrrolidone (such as N-methylpyrrolidone or N-octylpyrrolidone), fatty acid dimethyl decylamine (such as C8-C10 fatty acid dimethyl decylamine) and chlorocarbons. EC products after adding water, since It can then be emulsified to produce an emulsion of sufficient stability to be sprayed by suitable equipment. Preparation of EW involves obtaining a compound of formula (I) in liquid form (if it is not liquid at ambient temperature, it may melt at a reasonable temperature, typically below 70 ° C), or in the form of a solution ( I) The compound (by dissolving it in a suitable solvent) and then emulsifying the resulting liquid or solution in water containing one or more SFAs under high shear to produce an emulsion. Suitable solvents for EWs include vegetable oils, chlorocarbons (such as chlorobenzene), aromatic solvents (such as alkylbenzenes or alkylnaphthalenes), and other suitable and water-soluble organic solvents.
可利用將水與一種或多種含一種或多種SFA的摻合物混合的方式,自然產生一種具熱力穩定性的等向液體調配物,藉以製備微乳劑(ME)。式(I)化合物最初的形態為水或溶劑/SFA摻合物。適用於MEs的溶劑包括以上描述用於ECs或EWs之溶劑。ME可為水包油或油包水系統(可由傳導性測量來判定存在何種系統),也可適合用來在相同的調配物中混合水溶性與油溶性殺有害生物劑。ME適合在水中稀釋,包括繼續保持微乳劑的形式或形成習知的水包油乳劑。 Microemulsions (ME) can be prepared by naturally producing a thermally stable, isotropic liquid formulation by mixing water with one or more blends containing one or more SFAs. The initial form of the compound of formula (I) is water or a solvent/SFA blend. Solvents suitable for use in MEs include the solvents described above for ECs or EWs. The ME can be an oil-in-water or water-in-oil system (which can be determined by conductivity measurements to determine which system is present), and can also be adapted to mix water-soluble and oil-soluble pesticides in the same formulation. ME is suitable for dilution in water, including continuing to maintain the form of a microemulsion or forming a conventional oil-in-water emulsion.
懸浮液濃縮物(SC)可包含式(I)化合物微細不溶固體顆粒的水性或非水性懸浮液。可在適當的介質中,利用球磨或珠磨方式來研磨式(I)化合物(可選擇性使用一種或多種分散劑)以製備SC,藉以製成細粒狀的化合物懸浮液。組成物中可含一種或多種的濕潤劑,並可加入一種懸浮液以降低顆粒沉澱的速率。或者,可對式(I)化合物進行乾磨並加入 含有前述試劑的水中,製成所欲的最終產品。 The suspension concentrate (SC) may comprise an aqueous or non-aqueous suspension of finely insoluble solid particles of the compound of formula (I). The compound of formula (I) (optionally using one or more dispersing agents) can be milled in a suitable medium by ball milling or bead milling to prepare SC, whereby a suspension of the finely divided compound can be prepared. The composition may contain one or more wetting agents and a suspension may be added to reduce the rate of particle precipitation. Alternatively, the compound of formula (I) can be dry milled and added The water containing the aforementioned reagent is used to make the desired final product.
氣溶膠調配物包含式(I)化合物及合適的推進劑(例如正丁烷)。也可在一個合適的介質(例如水或是正丙醇等水溶性液體)中溶解或分散式(I)的化合物,以提供使用於非加壓之手致動式噴淋泵的組成物。 Aerosol formulations comprise a compound of formula (I) and a suitable propellant (e.g., n-butane). The compound of formula (I) may also be dissolved or dispersed in a suitable medium (e.g., water or a water soluble liquid such as n-propanol) to provide a composition for use in a non-pressurized hand-actuated spray pump.
式(I)化合物可在乾燥狀態下與煙火混合物混合,以形成一種適合在密閉空間中產生含此化合物的煙霧之組成物。 The compound of formula (I) can be mixed with the pyrotechnic mixture in a dry state to form a composition suitable for producing a fumes containing the compound in a confined space.
能以類似製備EW調配物的方式來製備膠囊懸浮液(CS),但是附加一個額外的聚合階段,藉此獲得油滴的水分散,其中,每個油滴是用聚合外殼來封裝,並含有式(I)的化合物,及選擇性地包含一個載體或稀釋劑。聚合外殼可利用界面聚縮合反應或凝聚程序來製成。組成物可提供式(I)化合物的控釋(controlled release)效果,並可用於種子處理。式(I)化合物亦能配製於可生物降解的聚合物基體,以提供化合物緩慢,受控制的釋放。 The capsule suspension (CS) can be prepared in a similar manner to the preparation of the EW formulation, but with the addition of an additional polymerization stage whereby water dispersion of the oil droplets is obtained, wherein each oil droplet is encapsulated with a polymeric outer shell and contains a compound of formula (I), and optionally a carrier or diluent. The polymeric shell can be made using an interfacial polycondensation reaction or a coacervation procedure. The composition provides a controlled release effect of the compound of formula (I) and can be used for seed treatment. The compound of formula (I) can also be formulated in a biodegradable polymer matrix to provide a slow, controlled release of the compound.
組成物中可包含一種或多種添加劑,以增進組成物的生物表現性(例如藉由改善濕性、保留性或表面分布性;處理之表面的抗雨性;或式(I)化合物的攝取性和移動性來增進)。此類添加劑包括表面活性劑、基於某些礦物油或天然植物油(如大豆及油菜籽油)等油類的噴霧添加劑,以及其與其他生物性強化佐劑(可幫助或更改式(I)化合物作用之成分)的摻合物。 One or more additives may be included in the composition to enhance the bio-exhibition of the composition (e.g., by improving wettability, retention or surface distribution; the rain resistance of the treated surface; or the uptake of the compound of formula (I) And mobility to improve). Such additives include surfactants, spray additives based on certain mineral oils or natural vegetable oils (such as soybean and rapeseed oil), and other bio-enhancing adjuvants that can help or modify compounds of formula (I). Blend of the component of action.
式(I)化合物亦可配製為種子處理的調配物,例如粉末 組成物,包括用於乾式種子處理(DS)的粉末、水溶性粉劑(SS)或用於泥水處理的水分散性粉劑(WS),或是液體組成物,包括懸浮濃縮物(FS)、溶劑(LS)或膠囊懸浮液(CS)。DS、SS、WS、FS及LS組成物的製備方法,分別與上述DP、SP、WP、SC和DC組成物的製備方法非常類似。用於處理種子的組成物,可包括用於幫助組成物附著於種子的試劑(例如礦物油或成膜阻隔物)。 The compound of formula (I) may also be formulated as a seed treatment formulation, such as a powder Compositions, including powders for dry seed treatment (DS), water-soluble powders (SS) or water-dispersible powders (WS) for mud water treatment, or liquid compositions, including suspension concentrates (FS), solvents (LS) or capsule suspension (CS). The preparation methods of the DS, SS, WS, FS and LS compositions are very similar to the preparation methods of the above DP, SP, WP, SC and DC compositions, respectively. The composition for treating the seed may include an agent (e.g., mineral oil or film-forming barrier) for assisting in the attachment of the composition to the seed.
濕潤劑、分散劑及乳化劑可為陽離子、陰離子、兩性或非離子類型的表面SFA。 The humectant, dispersant and emulsifier can be cationic, anionic, amphoteric or nonionic surface SFA.
陽離子類型之適合的SFAs,包括四級銨化合物(例如溴化十六烷基三甲基銨)、咪唑啉類及胺鹽類。 Suitable SFAs of the cationic type include quaternary ammonium compounds such as cetyltrimethylammonium bromide, imidazolines and amine salts.
適合的陰離子SFAs包括脂肪酸的鹼金屬鹽、硫酸之脂族單酯的鹽(例如十二烷基硫酸鈉)、磺化芳香族化合物的鹽(例如十二烷基苯磺酸鈉、十二烷基苯磺酸鈣、萘磺酸丁脂,以及二異丙基萘磺酸鈉及三異丙基萘磺酸鈉之混合物)、醚硫酸鹽、醇醚硫酸鹽(例如月桂基聚醚-3硫酸鈉)、醚羧酸鹽(例如月桂基聚醚-3羧酸鈉)、磷酸鹽酯(一個或多個脂肪醇與磷酸(主要為單酯)或五氧化二磷(主要是二酯)反應下之產物,例如月桂醇與四磷酸反應;此外,這些產物可乙氧基化)、磺化琥珀醯胺酸鹽、石蠟或烯屬磺酸酯、胺基乙磺酸鹽和木素磺化鹽。 Suitable anionic SFAs include alkali metal salts of fatty acids, salts of aliphatic monoesters of sulfuric acid (for example sodium lauryl sulfate), salts of sulfonated aromatic compounds (for example sodium dodecylbenzene sulfonate, dodecane) Calcium benzenesulfonate, naphthalene sulfonate, and a mixture of sodium diisopropylnaphthalenesulfonate and sodium triisopropylnaphthalenesulfonate, ether sulfate, alcohol ether sulfate (eg, lauryl polyether-3) Sodium sulphate), ether carboxylates (eg sodium lauryl polyether-3 carboxylate), phosphate esters (one or more fatty alcohols with phosphoric acid (mainly monoesters) or phosphorus pentoxide (mainly diesters) Products under reaction, such as lauryl alcohol and tetraphosphoric acid; in addition, these products can be ethoxylated), sulfonated amber amide, paraffin or olefin sulfonate, aminoethanesulfonate and lignin Salt.
兩性類型之適合的SFA包括甜菜鹼、丙酸鹽及甘胺酸鹽。 Suitable SFAs of the amphoteric type include betaines, propionates and glycinates.
非離子類型之合適的SFA包括環氧烷烴的縮合產物, 如環氧乙烷、環氧丙烷、環氧丁烷,或其與脂肪醇(如油醇或十六醇)或烷基酚(如辛基苯酚、壬基苯酚或辛基甲酚)的混合物;由長鏈脂肪酸或己糖醇酐取得的偏酯;上述偏酯與環氧乙烷的縮合產物;嵌段聚合物(包括環氧乙烷和環氧丙烷);烷醇醯胺;單酯(例如脂肪酸聚乙二醇酯);氧化胺(例如十二烷基二甲基氧化胺);和卵磷脂。 Suitable SFAs of the nonionic type include condensation products of alkylene oxides, Such as ethylene oxide, propylene oxide, butylene oxide, or a mixture thereof with a fatty alcohol (such as oleyl alcohol or cetyl alcohol) or an alkyl phenol (such as octylphenol, nonylphenol or octyl cresol) a partial ester obtained from a long-chain fatty acid or hexitol anhydride; a condensation product of the above partial ester with ethylene oxide; a block polymer (including ethylene oxide and propylene oxide); an alkanolamine; a monoester (eg fatty acid polyethylene glycol esters); amine oxides (eg dodecyl dimethyl amine oxide); and lecithin.
適合的懸浮劑包括親水膠體(如多醣體、聚乙烯吡咯啶酮或羧甲基纖維素鈉)及膨脹性黏土(如膨潤土或厄帖浦土(attapulgite))。 Suitable suspending agents include hydrophilic colloids (such as polysaccharides, polyvinylpyrrolidone or sodium carboxymethylcellulose) and swelling clays (such as bentonite or attapulgite).
可使用任何已知的殺有害生物化合物施用方法,來施用式(I)化合物。舉例來說,不論它是否製成調配物,都可直接應用在有害生物或有害生物的所在之處(例如有害生物的棲息地、或是容易受到有害生物侵襲之成長中的植物)或是應用在植物的任何部分,包括葉子、莖、枝條或根,或在種植種子之前應用於種子上,或應用在當中具有成長中的植物、或準備在其內種植植物的其他媒介(例如根部週遭的土壤、一般土壤、稻田水或水耕栽培系統),或是可在土壤或水性環境中,將它噴上、撒上、以浸泡方式來應用、當作乳膏或藥膏調配物來應用、以蒸汽方式應用,或是藉由分配或加入組成物的方式來應用(例如顆粒組成物或包在水溶性袋中的組成物)。 The compound of formula (I) can be administered using any known method of administering a pesticidal compound. For example, whether it is formulated or not, it can be applied directly to where pests or pests are located (such as habitats of pests or growing plants that are susceptible to pests) or applications. Apply to any part of the plant, including leaves, stems, shoots or roots, or to the seed before planting it, or to plants that have grown up, or other medium in which plants are to be planted (eg, around the roots) Soil, general soil, paddy water or hydroponic cultivation system, or it can be sprayed, sprinkled, applied by immersion in a soil or aqueous environment, applied as a cream or ointment, Steam application, either by dispensing or adding a composition (eg, a particulate composition or a composition encapsulated in a water soluble bag).
式(I)化合物亦可注入植物內,或使用電動噴霧技術或其他少量性方法噴於植物上,或使用土地或空中灌溉系統來施用。 The compounds of formula (I) may also be injected into plants or sprayed onto plants using electrodynamic spraying techniques or other minor methods, or applied using land or aerial irrigation systems.
當作水性製劑(如水溶液或分散液)來使用的組成物,通常是以含有高比例活性成分的濃縮物(濃縮物在使用前先加入水中)形式來供應。這些可含DCs、SCs、ECs、EWs、MEs、SGs、SPs、WPs、WGs及CSs的濃縮物,通常要能承受長時間的儲藏,並在這樣長時間儲藏後仍能加入水以形成水性製劑,而且這些調劑能在一段充分的時間內保持同質,以便供習知噴霧設備來施用。視其用途而定,此類的水性製劑可含有不同含量的式(I)化合物(例如從0.0001至10%(按重量計))。 Compositions for use as aqueous preparations (e.g., aqueous solutions or dispersions) are typically supplied as a concentrate containing a high proportion of active ingredient (the concentrate is added to the water prior to use). These concentrates, which can contain DCs, SCs, ECs, EWs, MEs, SGs, SPs, WPs, WGs, and CSs, are typically capable of withstanding long-term storage and can be added to form aqueous formulations after such long-term storage. And these agents can remain homogenous for a sufficient period of time for application by conventional spray equipment. Depending on the use, such aqueous preparations may contain varying amounts of the compound of formula (I) (for example from 0.0001 to 10% by weight).
式(I)的化合物可與肥料(例如含氮、鉀或磷的肥料)一起用於混合物裡。合適的調配物類型包括肥料顆粒。式(I)化合物在混合物中的含量,較佳高達此化合物重量的25%。 The compound of formula (I) can be used in a mixture with a fertilizer such as a fertilizer containing nitrogen, potassium or phosphorus. Suitable formulation types include fertilizer granules. The content of the compound of the formula (I) in the mixture is preferably up to 25% by weight of the compound.
因此,本發明還提供了包含肥料和式(I)化合物的肥料組成物。 Accordingly, the present invention also provides a fertilizer composition comprising a fertilizer and a compound of formula (I).
本發明之組成物可包含其他具有生物活性的化合物,例如微量營養素或具以下活性的化合物:殺真菌活性,或植物生長調節、除草、殺蟲、殺線蟲或殺蟎活性。 The compositions of the present invention may comprise other biologically active compounds, such as micronutrients or compounds having the following activity: fungicidal activity, or plant growth regulating, herbicidal, insecticidal, nematicidal or acaricidal activity.
式(I)的化合物可以是組成物的唯一活性成分,或是它可以在適當的情況下,與一個或多個額外的活性成分(例如殺有害生物劑(如殺蟲劑、殺真菌劑或除草劑,或是增效劑或植物生長調節劑等等))混合。額外的活性成分可提供效力譜更廣泛、或在有害生物所在之處更具持久效力的組成物;增效或補充式(I)化合物的活性(例如藉由增加效果的速度或藉由克服抵抗性的方式);或是協助克服或預防對個別 的成分發展出抗性。特定之額外活性成分將視預期的組成物效用而定。 The compound of formula (I) may be the sole active ingredient of the composition, or it may, where appropriate, be combined with one or more additional active ingredients (eg pesticides such as insecticides, fungicides or Herbicide, or synergist or plant growth regulator, etc.)) mixed. Additional active ingredients may provide a composition having a broader spectrum of efficacy, or a more durable effect where the pest is present; synergizing or supplementing the activity of the compound of formula (I) (eg, by increasing the rate of effect or by overcoming resistance) Sexual approach); or assist in overcoming or preventing individual The ingredients develop resistance. The particular additional active ingredient will depend on the intended utility of the composition.
本發明物之化合物也有益於動物健康領域,例如它們可用來防制寄生的無脊椎有害生物,更適合用來防制動物體內或身上之寄生的無脊椎有害生物。有害生物的例子包括線蟲、吸蟲、絛蟲、飛蠅、蟎、壁虱、虱子、跳蚤、蝽象及蛆。動物可以是非人動物,例如與農業相關之動物,例如牛、豬、綿羊、山羊、馬或騾,或狗或貓等伴侶動物。 The compounds of the present invention are also useful in the field of animal health, for example, they can be used to prevent parasitic invertebrate pests, and are more suitable for preventing invertebrate pests in or on parasitic objects. Examples of pests include nematodes, flukes, mites, flies, cockroaches, ticks, lice, fleas, ticks, and ticks. The animal may be a non-human animal, such as an animal associated with agriculture, such as a cow, pig, sheep, goat, horse or donkey, or a companion animal such as a dog or cat.
在另一態樣中,本發明中的一種化合物能用於治療處理方法之中。 In another aspect, a compound of the invention can be used in a therapeutic treatment.
在另一態樣中,本發明涉及一種控制動物體內外寄生的無脊椎有害生物之方法,其中包括投予殺有害生物有效量的本發明化合物。舉例來說,此給藥方式可為口服給藥、非口服給藥或外部給藥,例如動物身體表面。在另一態樣中,本發明涉及一種控制動物體內外寄生的無脊椎有害生物之化合物。在另一態樣中,本發明涉及使用本發明的化合物,製造控制動物體內外寄生的無脊椎有害生物之試劑的用途。 In another aspect, the invention relates to a method of controlling an invertebrate pest that is parasitic in and out of an animal, comprising administering a pesticidally effective amount of a compound of the invention. For example, the mode of administration can be oral, parenteral or external, such as the surface of an animal's body. In another aspect, the invention relates to a compound that controls an invertebrate pest that is parasitic in and out of an animal. In another aspect, the invention relates to the use of a compound of the invention for the manufacture of an agent for controlling invertebrate pests in vivo and in vitro.
在另一態樣中,本發明涉及一種控制寄生的無脊椎有害生物之方法,其中包含將殺有害生物有效量的本發明之化合物施於動物所棲息的環境中。 In another aspect, the invention relates to a method of controlling parasitic invertebrate pests comprising administering a pesticidally effective amount of a compound of the invention to an environment in which the animal is inhabited.
在另一態樣中,本發明涉及保護動物不受寄生的無脊椎有害生物侵擾之方法,其中包含將殺有害生物有效量的本發明之化合物施於動物上。在另一態樣中,本發明涉及 一種用於保護動物不受寄生的無脊椎有害生物侵擾的化合物。在另一態樣中,本發明涉及使用本發明的化合物,製造用於保護動物不受寄生的無脊椎有害生物侵擾之試劑的用途。 In another aspect, the invention relates to a method of protecting an animal from parasitic invertebrate pests comprising administering a pesticidally effective amount of a compound of the invention to an animal. In another aspect, the invention relates to A compound used to protect animals from parasitic invertebrate pests. In another aspect, the invention relates to the use of a compound of the invention for the manufacture of an agent for protecting an animal from parasitic invertebrate pests.
在另一態樣中,本發明提供為受寄生的無脊椎有害生物所苦的動物進行治療的方法,其中包含將殺有害生物有效量的本發明之化合物施於動物上。在另一態樣中,本發明涉及一種化合物能用於治療受寄生的無脊椎有害生物所苦的動物。在另一態樣中,本發明涉及了使用本發明的化合物來製造試劑,以用於處理受寄生的無脊椎有害生物所苦的動物的用途。 In another aspect, the invention provides a method of treating an animal suffering from a parasitic invertebrate pest comprising administering a pesticidally effective amount of a compound of the invention to an animal. In another aspect, the invention relates to a compound that can be used to treat an animal suffering from a parasitic invertebrate pest. In another aspect, the invention relates to the use of a compound of the invention to manufacture an agent for use in treating an animal suffering from a parasitic invertebrate pest.
在另一態樣中,本發明提供一種醫藥組成物,包括本發明的一個化合物與一個適用於醫藥的賦形劑。 In another aspect, the invention provides a pharmaceutical composition comprising a compound of the invention and an excipient suitable for use in medicine.
本發明的化合物得以單獨使用,也可以和一種或多種其他的生物活性成分組合使用。 The compounds of the invention may be used alone or in combination with one or more other biologically active ingredients.
在另一態樣中,本發明提供了一種組合產物,包含了殺有害生物有效量的A組分與殺有害生物有效量的B組分。其中,A組分是本發明的一個化合物,而B組分則是如下所述的一個化合物。 In another aspect, the invention provides a combination product comprising a pesticidally effective amount of component A and a pesticidally effective amount of component B. Among them, the A component is a compound of the present invention, and the B component is a compound as described below.
本發明的化合物可與驅蟲劑組合使用。這樣的驅蟲劑包括選自大環內酯類化合物的化合物,諸如:伊維菌素(ivermectin)、阿凡曼菌素(avermectin)、阿巴汀(abamectin)、因滅汀(emamectin)、埃普利諾菌素(eprinomectin)、得拉滅克汀(doramectin)、色拉菌素 (selamectin)、莫斯達汀(moxidectin)、奈馬克丁(nemadectin)與米爾比霉素(milbemycin)衍生物,如EP-357460、EP-444964與EP-594291中所述。其他驅蟲劑則包括半合成和生物合成的阿凡曼菌素/米爾比霉素衍生物,例如那些描述於US-5015630、WO-9415944和WO-9522552的衍生物。其他驅蟲劑還包括苯並咪唑類,例如:阿苯達唑(albendazole)、堪苯達唑(cambendazole)、芬苯達唑(fenbendazole)、氟苯達唑(flubendazole)、甲苯咪唑(mebendazole)、奧芬達唑(oxfendazole)、奧苯達唑(oxibendazole)、帕苯達唑(parbendazole)、以及本類別的其他成員。其他驅蟲劑包括咪唑並噻唑和四氫嘧啶,例如:四咪唑(tetramisole)、左旋咪唑(levamisole)、噻嘧啶波(pyrantel pamoate)、奥克太生(oxantel)或莫侖太(morantel)。其他驅蟲劑包括殺吸蟲劑(flukicide)(例如三氯苯達唑(triclabendazole)和氯舒隆(clorsulon)),以及殺條蟲劑(cestocides),例如吡喹酮(praziquantel)和依西太爾(epsiprantel)。 The compounds of the invention may be used in combination with an insect repellent. Such insect repellents include compounds selected from macrolide compounds, such as: ivermectin, avermectin, abamectin, emamectin, Eprinomectin, doramectin, serracin (selamectin), moxidectin, nemadectin and milbemycin derivatives, as described in EP-357460, EP-444964 and EP-594291. Other insect repellents include semi-synthetic and biosynthetic avermectin/milbimycin derivatives such as those described in US-5015630, WO-9415944 and WO-9522552. Other insect repellents also include benzimidazoles such as albendazole, cambendazole, fenbendazole, flubendazole, mebendazole , oxfendazole, oxibendazole, parbendazole, and other members of this class. Other insect repellents include imidazothiazole and tetrahydropyrimidine, for example: tetramisole, levamisole, pyrantel pamoate, oxantel or morantel. Other insect repellents include flukicides (such as triclabendazole and clorsulon), as well as cestocides such as praziquantel and Isey. Tyr (epsiprantel).
本發明的化合物可與以下項目組合使用:驅蟲劑paraherquamide/marcfortine種類的衍生物和類似物,以及抗寄生物的唑啉,例如那些揭露於US-5478855、US-4639771和DE-19520936的唑啉。 The compounds of the invention may be used in combination with the derivatives and analogues of the insect repellent paraherquamide/marcfortine species, as well as antiparasitic Oxazolines, such as those disclosed in US-5478855, US-4639771, and DE-19520936 Oxazoline.
本發明的化合物可與以下項目組合使用:二側氧嗎啉抗寄生物試劑(如WO-9615121中所述)之一般類的衍生物和類似物,以及驅蟲活性環狀縮肽,例如那些描述於 WO-9611945、WO-9319053、WO-9325543、EP-626375、EP-382173、WO-9419334、EP-382173和EP-503538的縮肽。 The compounds of the present invention can be used in combination with the following general derivatives and analogs of the two-side oxymorpholine antiparasitic agent (as described in WO-9615121), as well as anthelmintic active cyclic depsipeptides, such as those Described in The peptides of WO-9611945, WO-9319053, WO-9325543, EP-626375, EP-382173, WO-9419334, EP-382173 and EP-503538.
本發明的化合物可與其他的殺體外寄生物劑組合使用,如芬普尼(fipronil);菊酯類農藥(pyrethroids);有機磷酸酯;昆蟲生長調節劑,例如祿芬隆(lufenuron);蛻皮激素激動劑(ecdysone agonists),例如得芬諾(tebufenozide)及類似物;新菸鹼(neonicotinoids),例如益達胺(imidacloprid)及類似物。 The compounds of the invention may be used in combination with other ectoparasites, such as fipronil; pyrethroids; organophosphates; insect growth regulators such as lufenuron; Ecdysone agonists, such as tebufenozide and analogs; neonicotinoids, such as imidacloprid and the like.
本發明的化合物可與萜烯類生物鹼組合使用,例如那些描述於國際專利申請出版物編號WO95/19363或WO04/72086的萜類生物鹼,尤其是揭露於其中的化合物。 The compounds of the present invention can be used in combination with terpenoid alkaloids, such as those described in International Patent Application Publication No. WO 95/19363 or WO 04/72086, especially the compounds disclosed therein.
對於此類可和本發明之化合物組合使用的生物活性化合物,其他範例包括但不限於下列各項: Other examples of such biologically active compounds that can be used in combination with the compounds of the invention include, but are not limited to, the following:
有機磷酸酯類:歐殺松(acephate)、亞滅松(azamethiphos)、乙基谷速松(azinphos-ethyl)、甲基谷速松(azinphos-methyl)、溴磷松(bromophos)、乙基溴磷松(bromophos-ethyl)、硫線磷(cadusafos)、氯氧磷(chlorethoxyphos)、陶斯松(chlorpyrifos)、克芬松(chlorfenvinphos)、氯甲硫磷(chlormephos)、滅賜松(demeton)、滅賜松-S-甲基(demeton-S-methyl)、碸吸磷(demeton-S-methyl sulphone)、得拉松(dialifos)、大利松(diazinon)、二氯松(dichlorvos)、百治磷(dicrotophos)、大滅松(dimethoate)、二硫松(disulfoton)、愛殺松(ethion)、普伏松(ethoprophos)、益多松(etrimfos)、胺磺磷(famphur)、 芬滅松(fenamiphos)、撲滅松(fenitrothion)、繁福松(fensulfothion)、芬殺松(fenthion)、flupyrazofos、大福松(fonofos)、福木松(formothion)、福賽絕(fosthiazate)、飛達松(heptenophos)、依殺松(isazofos)、異拌磷(isothioate)、加福松(isoxathion)、馬拉松(malathion)、蟲蟎畏(methacrifos)、達馬松(methamidophos)、滅大松(methidathion)、甲基-巴拉松、美文松(mevinphos)、亞速靈(monocrotophos)、乃力松(naled)、歐滅松(omethoate)、滅多松(oxydemeton-methyl)、對氧磷(paraoxon)、巴拉松(parathion)、甲基-巴拉松(parathion-methyl)、賽達松(phenthoate)、裕必松(phosalone)、硫環磷(phosfolan)、福賜卡(phosphocarb)、益滅松(phosmet)、福賜米松(phosphamidon)、福瑞松(phorate)、巴賽松(phoxim)、亞特松(pirimiphos)、亞特松-甲基(pirimiphos-methyl)、佈飛松(profenofos)、丙蟲磷(propaphos)、胺丙畏(propetamphos)、丙硫磷(prothiofos)、白克松(pyraclofos)、必芬松(pyridaphenthion)、拜裕松(quinalphos)、硫丙磷(sulprofos)、亞培松(temephos)、托福松(terbufos)、特布松(tebupirimfos)、殺蟲畏(tetrachlorvinphos)、二甲硫吸磷(thimeton)、三落松(triazophos)、三氯松(trichlorfon)、繁米松(vamidothion)。 Organophosphates: acephate, azamethiphos, azinphos-ethyl, azinphos-methyl, bromophos, ethyl Bromophos-ethyl, cadusafos, chlorethoxyphos, chlorpyrifos, chlorfenvinphos, chlormephos, demeton, Demeton-S-methyl, demeton-S-methyl sulphone, dialifos, diazinon, dichlorvos, Baizhi Dicrotophos, dimethoate, disulfoton, ethion, ethoprophos, etrimfos, famphur, Fenamiphos, fenitrothion, fensulfothion, fenthion, flupyrazofos, fonofos, formothion, fosthiazate, feida Heptophophos, isazofos, isothioate, isoxathion, malathion, mecaprifos, methamidophos, methidathion, Methyl-balazon, mevinphos, monocrotophos, naled, omethoate, oxydemeton-methyl, paraoxon, bar Parathion, parathion-methyl, phenthoate, phosalone, phosfolan, phosphocarb, yishen ( Phosmet), phosphamidon, phorate, phoxim, pirimiphos, pirimiphos-methyl, profenofos, chlorpyrifos Propaphos, propetamphos, prothiofos, pyraclofos, pyridaphenthion Quinaphos, sulprofos, temephos, terbufos, tebupirimfos, tetrachlorvinphos, thimeton, Triazophos, trichlorfon, vamidothion.
胺基甲酸酯類:棉鈴威(alanycarb)、得滅克(aldicarb)、2-sec-butylphenyl methylcarbamate、丙硫克百威(benfuracarb)、西維因(carbaryl)、克百威(carbofuran)、 丁硫克百威(carbosulfan)、除線威(cloethocarb)、殺蟲丹(ethiofencarb)、苯氧威(fenoxycarb)、fenthiocarb、呋線威(furathiocarb)、HCN-801、滅必蝨(isoprocarb)、茚蟲威(indoxacarb)、滅蟲威(methiocarb)、滅多威(methomyl)、5-methyl-m-cumenylbutyryl(methyl)carbamate、殺線威(oxamyl)、抗蚜威(pirimicarb)、殘殺威(propoxur)、硫雙威(thiodicarb)、久效威(thiofanox)、唑蚜威(triazamate)、UC-51717。 Carbamates: alanycarb, aldicarb, 2-sec-butylphenyl methylcarbamate, benfuracarb, carbaryl, carbofuran, Carbosulfan, cloethocarb, ethiofencarb, fenoxycarb, fenthiocarb, furathiocarb, HCN-801, isoprocarb, Indoxacarb, metiocarb, methomyl, 5-methyl-m-cumenylbutyryl(methyl)carbamate, oxamyl, pirimicarb, propoxur ), thiodicarb, thiofanox, triazamate, UC-51717.
菊酯類農藥:acrinathin、烯丙菊酯(allethrin)、alphametrin、5-苯甲基-3-呋喃甲基(E)-(1 R)-順-2,2-二甲基-3-(2-側氧基噻-3-亞基甲基)環丙烷羧酸酯、聯苯菊酯(bifenthrin)、β-氟氯氰菊酯(beta-cyfluthrin)、氟氯氰菊酯(cyfluthrin)、a-氯氰菊酯(a-cypermethrin)、高效氯氰菊酯(beta-cypermethrin)、生物烯丙菊酯(bioallethrin)、bioallethrin((S)-cyclopentylisomer)、生物滅蟲菊(bioresmethrin)、聯苯菊酯(bifenthrin)、NCI-85193、乙氰菊酯(cycloprothrin)、氯氟氰菊酯(cyhalothrin)、cythithrin、苯醚氰菊酯(cyphenothrin)、溴氰菊酯(deltamethrin)、右旋烯炔菊酯(empenthrin)、D-氰戊菊酯(esfenvalerate)、醚菊酯(ethofenprox)、芬氟司林(fenfluthrin)、甲氰菊酯(fenpropathrin)、氰戊菊酯(fenvalerate)、氟氰菊酯(flucythrinate)、氟氯苯菊酯(flumethrin)、氟胺氰菊酯(fluvalinate)(D異構物)、炔咪菊酯(imiprothrin)、氯氟氰菊酯(cyhalothrin)、高效氯氟 氰菊酯(lambda-cyhalothrin)、氯菊酯(permethrin)、苯醚菊酯(phenothrin)、炔丙菊脂(prallethrin)、除蟲菊酯(pyrethrins)(天然產品)、苄呋菊酯(resmethrin)、胺菊酯(tetramethrin)、四氟苯菊酯(transfluthrin)、高效反式氯氰菊酯(theta-cypermethrin)、氟矽菊酯(silafluofen)、t-fluvalinate、七氟菊酯(tefluthrin)、四溴菊酯(tralomethrin)、Z-氯氰菊酯(Zeta-cypermethrin)。 Pyrethroid pesticides: acrinathin, allethrin, alphametrin, 5-benzyl-3-furanyl(E)-(1 R)-cis-2,2-dimethyl-3-( 2-sided oxythiophene -3-ylidenemethyl)cyclopropanecarboxylate, bifenthrin, beta-cyfluthrin, cyfluthrin, a-cypermethrin, beta-cypermethrin Beta-cypermethrin), bioallethrin, bioallethrin ((S)-cyclopentylisomer), bioresmethrin, bifenthrin, NCI-85193, cycloprothrin , cyhalothrin, cythithrin, cyphenothrin, deltamethrin, empenthrin, esfenvalerate, ether Ethyl ester (ethofenprox), fenfluthrin (fenfluthrin), fenpropathrin, fenvalerate, flucythrinate, flumethrin, fluocyanine Fluvalinate (D isomer), imiprothrin, cyhalothrin, lambda-cyhalothrin, permethrin, phenyl ether Phenophane, prallethrin, pyrethrins (natural product), fenfenyl ( Resmethrin), tetramethrin, transfluthrin, theta-cypermethrin, silafluofen, t-fluvalinate, tefluthrin, tetra Tralomethrin, Zeta-cypermethrin.
節肢動物生長調節劑:a)幾丁質合成抑制劑:苯甲醯脲類(benzoylureas):定蟲脲(chlorfluazuron)、除蟲脲(diflubenzuron)、氟佐隆(fluazuron)、氟蟎脲(flucycloxuron)、氟蟲脲(flufenoxuron)、氟鈴脲(hexaflumuron)、祿芬隆、雙苯氟脲(novaluron)、伏蟲隆(teflubenzuron)、殺鈴脲(triflumuron)、撲虱靈(buprofezin)、苯蟲醚(diofenolan)、噻蟎酮(hexythiazox)、依殺蟎(etoxazole)、氯苯那敏(chlorfentazine);b)蛻皮激素拮抗劑(ecdysone antagonists):氯蟲醯肼(halofenozide)、甲氧蟲醯肼(methoxyfenozide)、得芬諾(tebufenozide);c)保幼激素類似物(juvenoids):吡丙醚(pyriproxyfen)、烯蟲酯(methoprene)(包括S-烯蟲酯)、苯氧威(fenoxycarb);d)脂質生物合成抑制劑:螺蟎酯(spirodiclofen)。 Arthropod growth regulators: a) Chitin synthesis inhibitors: benzoylureas: chlorfluazuron, diflubenzuron, fluzuron, flucycloxuron ), flufenoxuron, hexaflumuron, velfenone, novaluron, teflubenzuron, triflumuron, buprofezin, benzene Diofenolan, hexythiazox, etoxazole, chlorfentazine; b) ecdysone antagonists: halofenozide, methoxy worm Methoxy (methoxyfenozide), tebufenozide; c) juvenoids: pyriproxyfen, methoprene (including S-methoprene), phenoxy Fenoxycarb); d) Lipid biosynthesis inhibitor: spirodiclofen.
其他的抗寄生物劑:亞醌蟎(acequinocyl)、雙甲脒(amitraz)、AKD-1022、ANS-118、印楝素(azadirachtin)、蘇雲金芽孢桿菌(Bacillus thuringiensis)、殺蟲磺 (bensultap)、必芬蟎(bifenazate)、樂殺蟎(binapacryl)、溴蟎酯(bromopropylate)、BTG-504、BTG-505、毒殺芬(camphechlor)、殺螟丹(cartap)、乙酯殺蟎醇(chlorobenzilate)、殺蟲脒(chlordimeform)、溴蟲腈(chlorfenapyr)、環蟲醯肼(chromafenozide)、可尼丁(clothianidine)、滅蠅胺(cyromazine)、diacloden、丁醚脲(diafenthiuron)、DBI-3204、二活菌素(dinactin)、二羥基甲基二羥基吡咯啶、敵蟎通(dinobuton)、敵蟎普(dinocap)、硫丹(endosulfan)、乙蟲腈(ethiprole)、醚菊酯(ethofenprox)、喹蟎醚(fenazaquin)、氟蟎(flumite)、MTI-800、唑蟎酯(fenpyroximate)、嘧蟎酯(fluacrypyrim)、氟苯亞胺噻唑(flubenzimine)、flubrocythrinate、flufenzine、三氟醚菊酯(flufenprox)、fluproxyfen、halofenprox、氟蟻腙(hydramethylnon)、IKI-220、kanemite、NC-196、neem guard、nidinorterfuran、烯啶蟲胺(nitenpyram)、SD-35651、WL-108477、pirydaryl、克蟎特(propargite)、protrifenbute、pymethrozine、噠蟎靈(pyridaben)、畢汰芬(pyrimidifen)、NC-1111、R-195、RH-0345、RH-2485、RYI-210、S-1283、S-1833、SI-8601、氟矽菊酯(silafluofen)、silomadine、多殺菌素(spinosad)、吡蟎胺(tebufenpyrad)、四氯殺蟎碸(tetradifon)、四抗菌素(tetranactin)、噻蟲啉(thiacloprid)、殺蟲環(thiocyclam)、噻蟲(thiamethoxam)、唑蟲醯胺(tolfenpyrad)、唑蚜威 (triazamate)、triethoxyspinosyn、三活菌素(trinactin)、verbutin、vertalec、YI-5301。 Other antiparasitic agents: acequinocyl, amitraz, AKD-1022, ANS-118, azadirachtin, Bacillus thuringiensis, bensultap , bifenazate, binapacryl, bromopropylate, BTG-504, BTG-505, camphechlor, cartap, ethyl chlorobenzilate ), chlordimeform, chlorfenapyr, chromafenozide, clothianidine, cyromazine, diacloden, diafenthiuron, DBI-3204 , dinactin, dihydroxymethyldihydroxypyrrolidine, dinobuton, dinocap, endosulfan, ethiprole, ethiprofen (ethofenprox) ), quinacline (fenazaquin), fluoroquinone (flumite), MTI-800, fenpyroximate, fluacrypyrim, flubenzimine, flubrocythrinate, flufenzine, flufenprox, fluproxyfen, halofenprox, flu Hydramethylnon, IKI-220, kanemite, NC-196, neem guard, nidinorterfuran, nitenpyram, SD-35651, WL-108477, pirydaryl, propargite, protrifenbute, pymethrozine, 哒Pyridaben, pyrimidifen, NC-1111, R-195, RH-0345, RH-2485, RYI-210, S-1283, S-1833, SI-8601, flumethrin Silafluofen), silomadine, spinosad, tebufenpyrad, tetradifon, tetranactin, thiacloprid, thiocyclam, worm (thiamethoxam), tolfenpyrad, triazamate, triethoxyspinosyn, trinactin, verbutin, vertalec, YI-5301.
殺真菌劑:阿昔貝拉(acibenzolar)、aldimorph、ampropylfos、andoprim、氮康唑(azaconazole)、嘧菌酯(azoxystrobin)、苯霜靈(benalaxyl)、苯菌靈(benomyl)、雙丙胺膦(bialaphos)、灰瘟素(blasticidin-S)、波爾多液(Bordeaux mixture)、糠菌唑(bromuconazole)、乙嘧酚磺酸酯(bupirimate)、加普胺(carpropamid)、敵菌丹(captafol)、克菌丹(captan)、多菌靈(carbendazim)、chlorfenazole、氯苯甲醚(chloroneb)、三氯硝基甲烷(chloropicrin)、百菌清(chlorothalonil)、乙菌利(chlozolinate)、氧氯化銅(copper oxychloride)、銅鹽、環氟菌胺(cyflufenamid)、霜脲氰(cymoxanil)、環唑醇(cyproconazole)、嘧菌環胺(cyprodinil)、酯菌胺(cyprofuram)、RH-7281、diclocymet、diclobutrazole、噠菌酮(diclomezine)、氯硝胺(dicloran)、醚唑(difenoconazole)、RP-407213、烯醯嗎啉(dimethomorph)、domoxystrobin、烯唑醇(diniconazole)、烯唑醇-M(diniconazole-M)、多果定(dodine)、敵瘟磷(edifenphos)、氟環唑(epoxiconazole)、唑菌酮(famoxadone)、fenamidone、氯苯嘧啶醇(fenarimol)、腈苯唑(fenbuconazole)、fencaramid、拌種咯(fenpiclonil)、苯鏽啶(fenpropidin)、丁苯嗎啉(fenpropimorph)、薯瘟錫(fentin acetate)、氟啶胺(fluazinam)、咯菌腈 (fludioxonil)、flumetover、flumorf/flumorlin、毒菌錫(fentin hydroxide)、氟嘧菌酯(fluoxastrobin)、氟喹唑(fluquinconazole)、氟矽唑(flusilazole)、福多寧(flutolanil)、粉唑醇(flutriafol)、殺菌丹(folpet)、三乙膦酸鋁(fosetyl-aluminium)、呋霜靈(furalaxyl)、furametapyr、己唑醇(hexaconazole)、種菌唑(ipconazole)、異稻瘟淨(iprobenfos)、異菌脲(iprodione)、稻瘟靈(isoprothiolane)、春雷霉素(kasugamycin)、醚菌酯(krsoxim-methyl)、代森錳鋅(mancozeb)、代森錳(maneb)、精甲霜靈(mefenoxam)、滅銹胺(mepronil)、甲霜靈(metalaxyl)、葉菌唑(metconazole)、苯氧菌胺(metominostrobin)/fenominostrobin、metafenone、腈菌唑(myclobutanil)、甲胂鐵銨(neo-asozin)、nicobifen、orysastrobin、霜靈(oxadixyl)、戊菌唑(penconazole)、戊菌隆(pencycuron)、噻菌靈(probenazole)、咪鮮胺(prochloraz)、霜黴威(propamocarb)、propioconazole、proquinazid、丙硫菌唑(prothioconazole)、啶斑肟(pyrifenox)、吡唑醚菌酯(pyraclostrobin)、嘧黴胺(pyrimethanil)、咯喹酮(pyroquilon)、喹氧靈(quinoxyfen)、螺環菌胺(spiroxamine)、硫、戊唑醇(tebuconazole)、四氟醚唑(tetrconazole)、噻菌靈(thiabendazole)、噻呋醯胺(thifluzamide)、甲基硫菌靈(thiophanate-methyl)、福美雙(thiram)、tiadinil、三唑酮(triadimefon)、三唑醇 (triadimenol)、三環唑(tricyclazole)、肟菌酯(trifloxystrobin)、滅菌唑(triticonazole)、井岡黴素(validamycin)、vinclozin。 Fungicides: acibenzolar, aldimorph, ampropylfos, andoprim, azaconazole, azoxystrobin, benaraxyl, benomyl, dipropylphosphine ( Bialaphos), blasticidin-S, Bordeaux mixture, bromuconazole, bupirimate, carpropamid, captafol, Captan, carbendazim, chlorfenazole, chloroneb, chloropicrin, chlorothalonil, chlozolinate, oxychlorination Copper oxychloride, copper salt, cyflufenamid, cymoxanil, cyproconazole, cyprodinil, cyprofuram, RH-7281, Diclocymet, diclobutrazole, diclomezine, dicloran, Difenoconazole, RP-407213, dimethomorph, domoxystrobin, diniconazole, diniconazole-M, dodine, edifenphos ), epoxiconazole, Famoxadone, fenamidone, fenarimol, fenbuconazole, fencaramid, fenpiclonil, fenpropidin, fenpropimorph, yam Fetin acetate, fluazinam, fludioxonil, flumetover, flumorf/flumorlin, fentin hydroxide, fluoxastrobin, fluquinconazole, fluoride Flusilazole, fluolanil, flurifaol, folpet, fosetyl-aluminium, furalaxyl, furametapyr, hexaconazole Hexaconazole), ipconazole, iprobenfos, iprodione, isoprothiolane, kasugamycin, krsoxim-methyl, mancozeb Mancozeb, maneb, mefenoxam, mepronil, metalaxyl, metconazole, metominostrobin/fenominostrobin , metafenone, myclobutanil, neo-asozin, nicofigen orysastrobin, Oxedixyl, penconazole, pencycuron, probenazole, prochloraz, propamocarb, propioconazole, proquinazid, prothioconazole Prothioconazole), pyrifenox, pyraclostrobin, pyrimethanil, pyroquilon, quinoxyfen, spiroxamine, sulfur, Tebuconazole, tetrconazole, thiabendazole, thifluzamide, thiophanate-methyl, thiram, tiadinil, three Triadimefon, triadimenol, tricyclazole, trifloxystrobin, triticonazole, validamycin, vinclozin.
生物製劑:Bacillus thuingiensis ssp.aizawai、kurstaki、蘇雲金芽孢桿菌(Bacillus thuringiensis)δ-內毒素類、桿狀病毒、昆蟲病原細菌、病毒與真菌。 Biologics: Bacillus thuingiensis ssp.aizawai, kurstaki, Bacillus thuringiensis delta-endotoxin, baculovirus, entomopathogenic bacteria, viruses and fungi.
殺菌劑:金黴素、土黴素、鏈黴素。 Bactericide: chlortetracycline, oxytetracycline, streptomycin.
其他生物製劑:恩氟沙星(enrofloxacin)、非班太(febantel)、青霉素G二乙胺基乙酯(penethamate)、moloxicam、頭孢胺芐(cefalexin)、卡那黴素(kanamycin)、匹克苯丹(pimobendan)、鹽酸克倫特羅(clenbuterol)、奧美拉唑(omeprazole)、硫姆林(tiamulin)、貝那普利(benazepril)、pyriprole、頭孢喹諾(cefquinome)、氟苯尼考(florfenicol)、乙基醯胺(buserelin)、cefovecin、泰拉黴素(tulathromycin)、ceftiour、卡洛芬(carprofen)、氰氟蟲腙(metaflumizone)、praziquarantel、三氯苯達唑(triclabendazole)。 Other biological agents: enrofloxacin, febantel, penicillin G diethylamine ethyl ester (penethamate), moloxicam, cefalexin, kanamycin, gram benzene Pimobendan, clenbuterol, omeprazole, tiamulin, benazepril, pyriprol, cefquinome, florfenicol (florfenicol), ethyl acetamide (bererelin), cefovecin, tulathromycin, ceftiour, carprofen, metaflumizone, praziquarantel, triclabendazole.
當本發明的化合物與其他活性成分組合使用時,最好與下列(其中,「Tx」係指式(I)之化合物,尤其是指選自表1至表120的化合物,該化合物可與特定的活性成分產生協同增效的效果)各項組合使用。益達胺+Tx、恩氟沙星+Tx、吡喹酮+Tx、雙羥萘酸噻嘧啶+Tx、非班太+Tx、青霉素G二乙胺基乙酯+Tx、moloxicam+Tx、頭孢胺芐+Tx、卡那黴素+Tx、匹克苯丹+Tx、鹽酸克倫特羅+Tx、 芬普尼+Tx、伊維菌素+Tx、奧美拉唑+Tx、硫姆林+Tx、貝那普利+Tx、米爾比霉素+Tx、滅蠅胺+Tx、噻蟲+Tx、pyriprole+Tx、溴氰菊酯+Tx、頭孢喹諾+Tx、氟苯尼考+Tx、乙基醯胺+Tx、cefovecin+Tx、泰拉黴素+Tx、ceftiour+Tx、色拉菌素+Tx、卡洛芬+Tx、氰氟蟲腙+Tx、莫斯達汀+Tx、烯蟲酯(包括S-烯蟲酯)+Tx、氯舒隆+Tx、噻嘧啶+Tx、雙甲脒+Tx、三氯苯達唑+Tx、阿凡曼菌素+Tx、阿巴汀+Tx、因滅汀+Tx、埃普利諾菌素+Tx、得拉滅克汀+Tx、色拉菌素+Tx、奈馬克丁+Tx、阿苯達唑+Tx、堪苯達唑+Tx、芬苯達唑+Tx、氟苯咪唑+Tx、甲苯咪唑+Tx、奧芬達唑+Tx、奧苯達唑+Tx、帕苯達唑+Tx、四咪唑+Tx、左旋咪唑+Tx、噻嘧啶波+Tx、奥克太生+Tx、莫侖太+Tx、三氯苯達唑+Tx、依西太爾+Tx、芬普尼+Tx、祿芬隆+Tx、蛻皮激素+Tx或得芬諾+Tx;更佳地是,恩氟沙星+Tx、吡喹酮+Tx、雙羥萘酸噻嘧啶+Tx、非班太+Tx、青霉素G二乙胺基乙酯+Tx、moloxicam+Tx、頭孢胺芐+Tx、卡那黴素+Tx、匹克苯丹+Tx、鹽酸克倫特羅+Tx、奧美拉唑+Tx、硫姆林+Tx、貝那普利+Tx、pyriprole+Tx、頭孢喹諾+Tx、氟苯尼考+Tx、乙基醯胺+Tx、cefovecin+Tx、泰拉黴素+Tx、ceftiour+Tx、色拉菌素+Tx、卡洛芬+Tx、莫斯達汀+Tx、氯舒隆+Tx、噻嘧啶+Tx、埃普利諾菌素+Tx、得拉滅克汀+Tx、色拉菌素+Tx、奈馬克丁+Tx、阿苯達唑+Tx、堪苯達 唑+Tx、芬苯達唑+Tx、氟苯咪唑+Tx、甲苯咪唑+Tx、奧芬達唑+Tx、奧苯達唑+Tx、帕苯達唑+Tx、四咪唑+Tx、左旋咪唑+Tx、噻嘧啶波+Tx、奥克太生+Tx、莫侖太+Tx、三氯苯達唑+Tx、依西太爾+Tx、祿芬隆+Tx或蛻皮激素+Tx;甚至更佳地是,恩氟沙星+Tx、吡喹酮+Tx、雙羥萘酸噻嘧啶+Tx、非班太+Tx、青霉素G二乙胺基乙酯+Tx、moloxicam+Tx、頭孢胺芐+Tx、卡那黴素+Tx、匹克苯丹+Tx、鹽酸克倫特羅+Tx、奧美拉唑+Tx、硫姆林+Tx、貝那普利+Tx、pyriprole+Tx、頭孢喹諾+Tx、氟苯尼考+Tx、乙基醯胺+Tx、cefovecin+Tx、泰拉黴素+Tx、ceftiour+Tx、色拉菌素+Tx、卡洛芬+Tx、莫斯達汀+Tx、氯舒隆+Tx或噻嘧啶+Tx。 When the compound of the present invention is used in combination with other active ingredients, it is preferably the same as the following (wherein "Tx" means a compound of the formula (I), especially a compound selected from Tables 1 to 120, which is specific to the compound The active ingredients produce synergistic effects) in combination. Yidaamine + Tx, enfloxacin + Tx, praziquantel + Tx, pyrantel p-hydroxypyrimidine + Tx, non-ban Tai + Tx, penicillin G diethylaminoethyl ester + Tx, moloxicam + Tx, cephalosporin Azide + Tx, kanamycin + Tx, Phenbenzidine + Tx, Clenbuterol + Tx, Fenpney + Tx, Ivermectin + Tx, Omeprazole + Tx, Sulm Tx, benazepril + Tx, milbemycin + Tx, chlortetracycline + Tx, worm +Tx, pyriprol+Tx, deltamethrin+Tx, cefquinome+Tx, florfenicol+Tx, ethylguanamine+Tx, cefovecin+Tx, taramycin+Tx, ceftiour+Tx, salad菌素+Tx, carprofen+Tx, cyanofluorfen+Tx, mosastatin+Tx, methoprene (including S-methoprene)+Tx, clorsulon+Tx, pyriazine+Tx, Amitraz + Tx, tricbendazole + Tx, avermectin + Tx, abatatin + Tx, indomethacin + Tx, eplenomycin + Tx, dermaquinin + Tx , serramycin + Tx, nemadacin + Tx, albendazole + Tx, candidazole + Tx, fenbendazole + Tx, fluorobenzazole + Tx, mebendazole + Tx, oxfendazole + Tx, opiateazole + Tx, pabendazole + Tx, tetraimidazole + Tx, levamisole + Tx, pyrithione + Tx, okexon + Tx, molena + Tx, tricbendazole +Tx, ezetine + Tx, Fenpney + Tx, Lucendron + Tx, ecdysone + Tx or Defenol + Tx; more preferably, Enfloxacin + Tx, Praziquantel + Tx , pyrantel p-hydroxypyrimidine + Tx, non-ban Tai + Tx, penicillin G diethylaminoethyl ester + Tx, moloxicam + Tx, cephalexin + Tx, kanamycin + Tx, pectin / Tx, Clenbuterol + Tx, omeprazole +Tx, thiolamin + Tx, benazepril + Tx, pyriprol + Tx, cefquinome + Tx, florfenicol + Tx, ethyl decylamine + Tx, cefovecin + Tx, taramycin + Tx , ceftiour+Tx, serramycin + Tx, carprofen + Tx, mustardatin + Tx, clorsulon + Tx, pyriazine + Tx, eplenomycin + Tx, dermametine + Tx, serramycin + Tx, nemadacin + Tx, albendazole + Tx, candidazole + Tx, fenbendazole + Tx, fluorobenzazole + Tx, mebendazole + Tx, oxfendazole +Tx, albendazole + Tx, pabendazole + Tx, tetraimidazole + Tx, levamisole + Tx, pyrimidine wave + Tx, okexon + Tx, molena + Tx, trichlorobenzene Oxazole + Tx, Ecetaxel + Tx, Lucendron + Tx or ecdysone + Tx; even more preferably, Enfloxacin + Tx, praziquantel + Tx, pyrantel p-hydroxypyrimidine + Tx, Non-ban Tai + Tx, penicillin G diethylaminoethyl ester + Tx, moloxicam + Tx, cephalexin + Tx, kanamycin + Tx, pectidine / Tx, clenbuterol + Tx, Ogilvy Carbazole + Tx, thiolam + Tx, benazepril + Tx, pyriprol + Tx, cefquinome + Tx, florfenicol + Tx, ethyl decylamine + Tx, cefovecin + Tx, tyranomycin +Tx, ceftiou r+Tx, serramycin + Tx, carprofen + Tx, mustardatin + Tx, clorsulon + Tx or pyrantel + Tx.
比例的例子包括100:1至1:6000、50:1至1:50、20:1至1:20,尤其是從10:1至1:10、5:1至1:5、2:1至1:2、4:1至2:1、1:1,或5:1、5:2、5:3、5:4、4:1、4:2或4:3,或3:1、3:2、2:1、1:5、2:5、3:5、4:5、1:4、2:4、3:4、1:3、2:3或1:2,或1:600、1:300、1:150、1:35、2:35、4:35、1:75、2:75或4:75,或1:6000、1:3000、1:1500、1:350、2:350、4:350、1:750、2:750或4:750。而我們知道這些混合比例一方面要按照重量比,一方面也要按照莫耳比。 Examples of ratios include 100:1 to 1:6000, 50:1 to 1:50, 20:1 to 1:20, especially from 10:1 to 1:10, 5:1 to 1:5, 2:1 To 1:2, 4:1 to 2:1, 1:1, or 5:1, 5:2, 5:3, 5:4, 4:1, 4:2 or 4:3, or 3:1 , 3:2, 2:1, 1:5, 2:5, 3:5, 4:5, 1:4, 2:4, 3:4, 1:3, 2:3 or 1:2, or 1:600, 1:300, 1:150, 1:35, 2:35, 4:35, 1:75, 2:75 or 4:75, or 1:6000, 1:3000, 1:1500, 1 : 350, 2:350, 4:350, 1:750, 2:750 or 4:750. And we know that these mixing ratios should be based on the weight ratio on the one hand and Moerby on the other.
特別要注意這種組合情況:額外活性成分的作用點與式I化合物不同。在某些實例當中,若組合至少一種具有類似控制範圍、但作用點不同的寄生的無脊椎有害生物控制 活性成分,對耐抗性的管理尤其有利。因此,本發明的化合產物可包含殺有害生物有效量的式I化合物,以及殺有害生物有效量的具有類似控制範圍、但作用點不同的至少一種另外寄生的無脊椎有害生物控制活性成分。 Particular attention should be paid to this combination: the point of action of the additional active ingredient is different from that of the compound of formula I. In some instances, if at least one parasitic invertebrate pest control with similar control range but different points of action is combined The active ingredient is particularly advantageous for the management of resistance. Thus, the compound of the invention may comprise a pesticidally effective amount of a compound of formula I, as well as a pesticidally effective amount of at least one additional parasitic invertebrate pest controlling active ingredient having a similar range of control but different points of action.
熟悉該項技術領域者認定,因為在環境和生理條件下,化合物的鹽與其相應的非鹽形式相稱,鹽形式與非鹽形式具有相同的生物效用。 Those skilled in the art recognize that because under the environmental and physiological conditions, the salt of the compound is commensurate with its corresponding non-salt form, the salt form has the same biological utility as the non-salt form.
因此,本發明之各式各樣的化合物鹽(以及與本發明的活性成分組合使用的活性成分),若用來控制無脊椎有害生物和動物寄生物,可能會很有用。鹽包括含無機酸或有機酸的酸性加成鹽類,例如氫溴酸、鹽酸、硝酸、磷酸、硫酸、乙酸、丁酸、富馬酸、乳酸、馬來酸、丙二酸、草酸、丙酸、水楊酸、酒石酸、4-甲苯磺酸或戊酸。本發明的化合物亦包括N-氧化物。因此,本發明包括本發明的化合物(包括N-氧化物及其鹽)和一個額外的活性成分(包括N-氧化物及其鹽)的組合。 Thus, the various compound salts of the present invention (and the active ingredients used in combination with the active ingredients of the present invention) may be useful if used to control invertebrate pests and animal parasites. Salts include acidic addition salts containing inorganic or organic acids such as hydrobromic acid, hydrochloric acid, nitric acid, phosphoric acid, sulfuric acid, acetic acid, butyric acid, fumaric acid, lactic acid, maleic acid, malonic acid, oxalic acid, and sodium. Acid, salicylic acid, tartaric acid, 4-toluenesulfonic acid or valeric acid. The compounds of the invention also include N-oxides. Accordingly, the invention includes combinations of the compounds of the invention (including N-oxides and salts thereof) and an additional active ingredient, including N-oxides and salts thereof.
使用於動物健康的組成物,也可包含調配物輔助劑和添加劑,即熟悉該項技術領域者所熟知的調配物助劑(其中一些可被視為亦作為固體稀釋劑、液體稀釋劑或界面活性劑)。這樣的調配物輔助劑和添加劑可控制:pH值(緩衝劑)、在處理過程中發泡(聚有機矽氧烷等消泡劑)、活性成分(懸浮劑)沉澱、粘度(觸變性增稠劑)、容器內微生物的生長(抗微生物劑)、產品凍結(防凍劑)、顏色(染料/顏料分散劑)、洗滌劑(成膜劑或粘附物)、蒸發(蒸發遲滯劑)和其他調配 物屬性。成膜劑的例子包括聚醋酸乙烯酯、聚醋酸乙烯酯共聚物、聚乙烯吡咯啶酮-聚醋酸乙烯酯共聚物、聚乙烯醇、聚乙烯醇共聚物和蠟。調配物輔助劑和添加劑的例子包括McCutcheon第2卷所列的輔助劑和添加劑:由《製造糕點出版公司》(The Manufacturing Confectioner Publishing Co.)的McCutcheon's部門出版的《功能材料》(Functional Materials,一年一度的國際版與北美版);與PCT出版品WO 03/024222。 Compositions useful for animal health may also contain formulation adjuvants and additives, i.e., formulation auxiliaries well known to those skilled in the art (some of which may be considered as solid diluents, liquid diluents or interfaces). Active agent). Such formulation adjuvants and additives can be controlled: pH (buffer), foaming during processing (defoamer such as polyorganosiloxane), precipitation of active ingredient (suspension), viscosity (thixotropy thickening) Agent), growth of microorganisms in the container (antimicrobial agent), product freezing (antifreeze), color (dye/pigment dispersant), detergent (film former or adherent), evaporation (evaporation retarder) and others Provisioning Property attribute. Examples of the film former include polyvinyl acetate, polyvinyl acetate copolymer, polyvinylpyrrolidone-polyvinyl acetate copolymer, polyvinyl alcohol, polyvinyl alcohol copolymer, and wax. Examples of formulation adjuvants and additives include the adjuvants and additives listed in McCutcheon Volume 2: "Functional Materials" published by McCutcheon's division of The Manufacturing Confectioner Publishing Co. Annual International and North American editions; and PCT publication WO 03/024222.
可以在不搭配佐劑的情況下,應用本發明的化合物,但最常用的應用將是一種包含以下各項的調配物:一個或多個含合適載體、稀釋劑與界面活性劑的活性成分,並可能與食物組合使用,視預期的最終用途而定。其中一個應用方法涉及了噴灑水分散劑或組合產品的精製油溶液。含有以下成分的組成物,通常能強化化合物的功效:噴淋油、濃縮噴淋油、展固劑、佐劑、其他溶劑與像是胡椒基丁氧化物(piperonyl butoxide)等增效劑。對於這類的噴灑物,可藉由幫浦或從加壓的容器(如加壓式氣霧噴灑罐)釋放噴灑物,從多種噴灑容器來噴灑,如罐子、瓶子或其他容器。此類的噴灑組成物可具有多種的形式,例如:噴灑、濕霧、泡沫、煙狀或霧氣。因此,此類的噴灑組成物能進一步包含推進劑、發泡劑等等(若情況所需)。應注意的是一種噴灑組成物,它包含了殺有害生物有效量的本發明之化合物與載體。此種噴灑組成物之具體實例,包含了殺有害生物有效量的本發明之化合物與推進劑。代表性推進劑包括但不 限於甲烷、乙烷、丙烷、丁烷、異丁烷、丁烯、戊烷、異戊烷、新戊烷、戊烯、氫氟碳化合物、氯氟碳化合物、二甲醚,及前述的混合物。應注意的是一種噴灑組成物(和一種使用此類從噴灑容器施配之噴灑組成物的方法),它用於控制起碼一種選自以下生物群的寄生的無脊椎有害生物:蚊子、黑蠅、廄螫蠅、鹿蠅、馬蠅、黃蜂、小黃蜂、大黃蜂、壁虱、蜘蛛、螞蟻、蚋及類似物(包括個別控制或組合控制)。 The compounds of the invention may be employed without the use of an adjuvant, but the most common application would be a formulation comprising one or more active ingredients containing a suitable carrier, diluent and surfactant, It may be combined with food, depending on the intended end use. One of the application methods involves spraying a water dispersant or a refined oil solution of a combination product. Compositions containing the following ingredients generally enhance the efficacy of the compound: spray oil, concentrated spray oil, spreading agents, adjuvants, other solvents and synergists such as piperonyl butoxide. For such sprays, the spray can be sprayed from a variety of spray containers, such as cans, bottles or other containers, by means of a pump or from a pressurized container such as a pressurized aerosol spray can. Such spray compositions can take a variety of forms such as, for example, spraying, wet mist, foam, smoke or mist. Thus, such spray compositions can further comprise propellants, blowing agents, and the like, if desired. It should be noted that a spray composition comprising a pesticidally effective amount of a compound of the invention and a carrier. Specific examples of such spray compositions comprise a pesticidally effective amount of a compound of the invention and a propellant. Representative propellants include but not Limited to methane, ethane, propane, butane, isobutane, butene, pentane, isopentane, neopentane, pentene, hydrofluorocarbon, chlorofluorocarbon, dimethyl ether, and mixtures thereof . It should be noted that a spray composition (and a method of using such a spray composition dispensed from a spray container) is used to control at least one parasitic invertebrate pest selected from the group consisting of: mosquitoes, black flies , fly, deer fly, horsefly, wasp, wasp, bumblebee, tick, spider, ant, cockroach and the like (including individual control or combination control).
動物寄生物之控制,包括了控制寄生於宿主動物身體表面(例如肩膀、腋窩、腹部、大腿內側)的外部寄生物,還有寄生於宿主動物身體內部(例如胃、腸子、肺部、血管、皮下、淋巴組織)的內部寄生物。外部寄生物或傳播疾病的有害生物包括像是:恙蟎、壁虱、虱子、蚊子、飛蠅、蟎與跳蚤。內部寄生物包括心絲蟲、鉤蟲與蠕蟲。本發明之化合物,在對抗外部寄生有害生物上可特別適用。在動物的寄生物侵擾或傳染方面,本發明之化合物可適合為此提供系統性及/或非系統性控制。 Control of animal parasites, including controlling external parasites that are parasitic on the surface of the host animal (eg, shoulders, armpits, abdomen, inner thighs), as well as parasitic inside the body of the host animal (eg, stomach, intestines, lungs, blood vessels, Internal parasites of subcutaneous, lymphoid tissue. External parasites or pests that transmit diseases include: ticks, ticks, scorpions, mosquitoes, flies, crickets and fleas. Internal parasites include heartworm, hookworms and worms. The compounds of the invention are particularly useful in combating external parasitic pests. The compounds of the invention may be suitable for providing systemic and/or non-systemic control for this in terms of animal parasite infestation or infection.
本發明之化合物可適用於對抗侵擾動物個體(包括野生動物、家畜與務農役用動物)之寄生的無脊椎有害生物。家畜這個名詞指的是(一隻或多隻)馴養之動物,而且特別養在農業環境之中以便協助生產如食物或纖維等農產品,或提供畜力;家畜的例子包括牛、綿羊、山羊、馬、豬、驢、駱駝、水牛、兔、母雞、火雞、鴨與鵝(例如養來供應肉食、乳汁、奶油、蛋、毛皮、皮、羽毛及/或羊毛)。藉由對抗寄 生物,可降低致死率與產能下降之情形(在肉食、乳汁、羊毛、外皮、蛋等方面)。如此,只要使用本發明之化合物,就能在動物畜牧方面更輕鬆、更經濟。 The compounds of the present invention are useful for combating parasitic invertebrate pests that invade animal individuals, including wild animals, livestock and farm animals. The term livestock refers to (one or more) domesticated animals, and is particularly raised in an agricultural environment to assist in the production of agricultural products such as food or fiber, or to provide animal power; examples of livestock include cattle, sheep, goats, and horses. , pigs, crickets, camels, buffalo, rabbits, hens, turkeys, ducks and geese (for example, feeding meat, milk, butter, eggs, fur, leather, feathers and/or wool). By confronting Biology can reduce the rate of death and productivity (in meat, milk, wool, skin, eggs, etc.). Thus, as long as the compound of the present invention is used, it is easier and more economical in animal husbandry.
本發明之化合物可適用於對抗會侵害伴侶動物與寵物(例如貓、狗、寵物鳥和觀賞魚)、研究與實驗動物(例如倉鼠、天竺鼠、野鼠與家鼠),還有動物園、野生棲息地及/或馬戲團的飼養動物。 The compounds of the present invention are useful for combating companion animals and pets (eg, cats, dogs, pet birds, and ornamental fish), research and experimental animals (such as hamsters, guinea pigs, voles and house mice), as well as zoos, wild habitats, and / or circus breeding animals.
在本發明的具體實例中,動物較佳是脊椎動物,更佳是哺乳動物、鳥類或魚類。在特別的具體實例中,動物個體為哺乳動物(包括類人猿,例如人類)。其他哺乳類個體包括靈長類(例如猴子)、牛類(例如牛畜或乳牛)、豬類(例如食用豬或豬)、羊類(例如山羊或綿羊)、馬類(例如馬)、犬科(例如狗)、貓科(例如家貓)、駱駝、鹿、驢、水牛、羚羊、兔與嚙齒類(例如天竺鼠、松鼠、野鼠、家鼠、沙鼠與倉鼠)。鳥類包括鴨科(天鵝、鴨與鵝)、鳩鴿科(例如鴿子)、雉科(例如山鶉、松雞與火雞)、Thesienidae(例如家雞)、鸚鵡類(例如長尾鸚鵡、金剛鸚鵡與鸚鵡)、獵禽與平胸鳥類(例如鴕鳥)。 In a particular embodiment of the invention, the animal is preferably a vertebrate, more preferably a mammal, bird or fish. In a particular embodiment, the animal individual is a mammal (including apes such as humans). Other mammalian individuals include primates (such as monkeys), cattle (such as cattle or cows), pigs (such as pigs or pigs), sheep (such as goats or sheep), horses (such as horses), and dogs. (eg dogs), cats (eg domestic cats), camels, deer, lynxes, buffaloes, antelopes, rabbits and rodents (eg guinea pigs, squirrels, voles, house mice, gerbils and hamsters). Birds include ducks (swan, ducks and geese), pigeons (eg pigeons), cockroaches (eg hawthorn, grouse and turkey), Thesienidae (eg chickens), parrots (eg long-tailed parrots, macaws) With parrots, hunting birds and flat-chested birds (such as ostriches).
受本發明之化合物處理或保護的鳥類,也能是與商業或非商業養鳥活動有關的鳥類。這些包括鴨科,例如天鵝、鵝與鴨;鳩鴿科,例如鴿子與家鴿;雉科,例如山鶉、松雞與火雞;Thesienidae,例如家雞;與鸚鵡類,例如為了作為寵物或供人收藏而飼養的長尾鸚鵡、金剛鸚鵡與鸚鵡及類似物。 Birds treated or protected by the compounds of the invention can also be birds associated with commercial or non-commercial bird breeding activities. These include ducks such as swans, geese and ducks; pigeons such as pigeons and domestic pigeons; cockroaches such as hawthorn, grouse and turkey; Thesienidae, such as domestic chickens; and parrots, for example for pets or Long-tailed parrots, macaws and parrots and the like that are kept for collection.
針對本發明之目的,「魚」一詞應被理解為包括但不限於Teleosti類的魚種,也就是硬骨魚。鮭形目(這也包括鮭科)及鱸形目(這也包括棘臀魚科)兩者都包含於Teleosti類之中。可能的魚類接受者包括鮭科、鮨科、鯛科、慈鯛科、太陽魚科及類似物。 For the purposes of the present invention, the term "fish" is to be understood to include, but is not limited to, the Teleosti species, that is, the bony fish. Both the scorpion (which also includes the scorpion) and the scorpion (which also includes the scorpionfish) are included in the Teleosti class. Possible fish recipients include the genus Polygonaceae, Polygonaceae, Polygonaceae, Cichlidae, Sunfish and the like.
亦仔細考量過其他可從發明的方法獲益之動物,包括有袋動物(例如袋鼠)、爬蟲類(例如飼養烏龜),還有其他具重要經濟價值的家畜類,而發明的方法能安全有效地為這些動物處理或預防寄生物傳染或侵擾的問題。 Other animals that can benefit from the invented method, including marsupials (such as kangaroos), reptiles (such as turtles), and other livestock with important economic value, have been carefully considered, and the method of invention is safe and effective. The problem of treating or preventing parasitic infections or infestation for these animals.
因替欲保護的動物提供殺有害生物有效量的本發明化合物,而加以控制的寄生的無脊椎有害生物例子包括:外寄生物(節肢動物、蟎等等)與內寄生物(蠕蟲,例如線蟲、吸蟲、絛蟲、寄生棘頭蟲等等)。 Examples of parasitic invertebrate pests that are controlled by providing a pesticidally effective amount of a compound of the invention to an animal to be protected include: ectoparasites (arthropods, ticks, etc.) and endoparasites (worms, eg, Nematodes, trematodes, mites, parasitic echinoderms, etc.).
之所以染上通常被描述為蠕蟲病的某個疾病或一組疾病,是因為動物宿主感染到稱為蠕蟲的寄生物。「蠕蟲」一詞的意義包括了線蟲、吸蟲、絛蟲及寄生棘頭蟲。蠕蟲病在家畜(如豬、綿羊、馬、牛、山羊、狗、貓與家禽)之間,構成了一個普遍且嚴重的經濟問題。 The reason why a disease or a group of diseases that are usually described as helminthiasis is caused is because the animal host is infected with a parasite called a worm. The meaning of the term "worm" includes nematodes, flukes, mites, and parasitic echinococcosis. Worm disease poses a widespread and serious economic problem between livestock (such as pigs, sheep, horses, cattle, goats, dogs, cats and poultry).
在蠕蟲之中,被描述為線蟲的一群寄生物會廣泛地散佈,有時候會在許多種動物之間造成嚴重的傳染問題。 Among the worms, a group of parasites described as nematodes are widely distributed, sometimes causing serious infection problems among many species of animals.
若在仔細考量後,打算用本發明之化合物來對付線蟲,這些線蟲包括但不限於下列屬:棘唇(Acanthocheilonema)、貓圓線蟲(Aelurostrongylus)、鉤蟲(Ancylostoma)、管口線蟲(Angiostrongylus)、雞蛔蟲 (Ascaridia)、蛔蟲(Ascaris)、布魯格絲蟲(Brugia)、反芻獸鉤蟲(Bunostomum)、毛細線蟲(Capillaria)、夏伯特線蟲(Chabertia)、古柏線蟲(Cooperia)、環體線蟲(Crenosoma)、網尾線蟲(Dictyocaulus)、澎結線蟲(Dioctophyme)、棘唇線蟲(Dipetalonema)、裂頭線蟲(Diphyllobothrium)、絲蟲(Dirofilaria)、龍線屬(Dracunculus)、蟯蟲(Enterobius)、類絲蟲(Filaroides)、血矛線蟲(Haemonchus)、異刺屬(Heterakis)、兔唇蛔(Lagochilascaris)、羅阿絲蟲(Loa)、曼森線蟲(Mansonella)、繆勒線蟲(Muellerius)、板口線蟲(Necator)、細頸線蟲(Nematodirus)、有齒食道口線蟲(Oesophagostomum)、胃線蟲(Ostertagia)、尖尾線蟲(Oxyuris)、副絲蟲(Parafilaria)、副蛔蟲(Parascaris)、泡翼蟲(Physaloptera)、原圓線蟲(Protostrongylus)、腹腔絲蟲(Setaria)、旋尾線蟲(Spirocerca)、冠絲蟲(Stephanofilaria)、糞桿線蟲(Strongyloides)、圓線蟲(Strongylus)、吸吮線蟲(Thelazia)、弓蛔線蟲(Toxascaris)、弓蛔蟲(Toxocara)、旋毛蟲(Trichinella)、毛線屬(Trichonema)、毛圓線蟲(Trichostrongylus)、鞭蟲(Trichuris)、鉤蟲(Uncinaria)與吳策線蟲(Wuchereria)。 If considered carefully, the compounds of the present invention are intended to be used against the nematodes, including but not limited to the following genera: Acanthocheilonema , Aelurostrongylus , Ancylostoma , Angiostrongylus , chicken roundworms (Ascaridia), roundworm (Ascaris), Bruce mercerizing worm (Brugia), ruminants hookworms (Bunostomum), capillariasis (Capillaria), Shadbolt nematodes (Chabertia), Cooper nematode (Cooperia), ring Nematodes ( Cernosoma ), Dictyocaulus , Dioctophyme , Dipetalonema , Diphyllobothrium , Heartworm (Dirofilaria), Long line genus (Dracunculus), pinworms (Enterobius), filarial class (Filaroides), Haemonchus (Haemonchus), Heterakis genus (Heterakis), roundworm lip (Lagochilascaris), L. loa ( Loa ), Mansonella , Muellerius , Necator , Nematodirus , Oesophagostomum , Ostertagia , Nematodes ( Oxyuris ), Parafilaria , Parascaris , Physaloptera , Protostrongylus , Setaria , Spirocerca , and Stephanofilaria ), fecal nematode (Strongyloides), nematodes (Strongylus), sucking nematodes (Thelazia), bow roundworm C. elegans (Toxascaris), bow roundworm (Toxocara), Trichinella spiralis (Trichinella), wool genus (Trichonema), hair nematodes ( Trichostrongylus ), Trichuris , Uncinaria , and Wuchereria .
上述最常見的動物傳染性線蟲屬為血矛線蟲(Haemonchus)、毛圓線蟲(Trichostrongylus)、胃線蟲(Ostertagia)、細頸線蟲(Nematodirus)、古柏線蟲(Cooperia)、蛔蟲(Ascaris)、反芻獸鉤蟲(Bunostomum)、有齒食道口線蟲(Oesophagostomum)、夏伯特線蟲 (Chabertia)、鞭蟲(Trichuris)、圓線蟲(Strongylus)、毛線屬(Trichonema)、網尾線蟲(Dictyocaulus)、毛細線蟲(Capillaria)、異刺屬(Heterakis)、弓蛔蟲(Toxocara)、雞蛔蟲(Ascaridia)、尖尾線蟲(Oxyuris)、鉤蟲(Ancylostoma)、鉤蟲(Uncinaria)、弓蛔線蟲(Toxascaris)與副蛔蟲(Parascaris)。其中,某些如細頸線蟲(Nematodirus)、古柏線蟲(Cooperia)與有齒食道口線蟲(Oesophagostomum)的主要攻擊部位為腸道,而其他如血矛線蟲(Haemonchus)與胃線蟲(Ostertagia)更普遍存在於胃部,而其他如網尾線蟲(Dictyocaulus)及類似物則出現於肺部。還有其他寄生物會位於其他組織裡,如心臟與血管、皮下和淋巴組織及類似物。 Above the most common zoonotic nematode genera Haemonchus (Haemonchus), hair round worm (Trichostrongylus), stomach nematodes (Ostertagia), narrow neck and nematodes (Nematodirus), Cooper nematode (Cooperia), roundworm (Ascaris), ruminants Bunostomum , Oesophagostomum , Chabertia , Trichuris , Strongylus , Trichonema , Dictyocaulus , Capillary nematode ( Capillaria ), Heterakis , Toxocara , Ascaridia , Oxyuris , Ancylostoma , Uncinaria , Toxascaris and Parasitic Locust ( Parascaris ). Wherein some of such Nematodirus (Nematodirus), Cooper nematode (Cooperia) with the toothed Oesophagostomum (Oesophagostomum) portion of the main attack the intestinal tract while others, such as Haemonchus (Haemonchus) and Ostertagia (Ostertagia) It is more common in the stomach, while others such as Dictyocaulus and the like appear in the lungs. There are other parasites that can be found in other tissues, such as heart and blood vessels, subcutaneous and lymphoid tissues, and the like.
若在仔細考量後,打算用本發明及發明的方法來對付吸蟲,這些吸蟲包括但不限於下列屬:Alaria、片吸蟲(Fasciola)、侏形吸蟲(Nanophyetus)、後睪吸蟲(Opisthorchis)、並殖吸蟲(Paragonimus)與血吸蟲(Schistosoma)。 If carefully considered, the invention and the method of the invention are intended to combat trematode, including but not limited to the following genus: Alaria , Fasciola , Nanophyetus , and trematode (Opisthorchis), Paragonimus (Paragonimus) and schistosomes (Schistosoma).
若在仔細考量後,打算用本發明及發明的方法來對付絛蟲,這些絛蟲包括但不限於下列屬:裂頭線蟲(Diphyllobothrium)、復孔蟲(Diplydium)、迭宮絛蟲(Spirometra)與絛蟲(Taenia)。 If considered carefully, the present invention and the method of the invention are intended to deal with aphids , including but not limited to the following genera: Diphyllobothrium , Diplydium , Spirometra and aphids ( Taenia ).
人類胃腸道最常見的寄生物屬為 The most common parasitic genus in the human gastrointestinal tract is
鉤蟲(Ancylostoma)、板口線蟲(Necator)、蛔蟲(Ascaris)、Strongy hides、旋毛蟲(Trichinella)、毛細線蟲 (Capillaria)、鞭蟲(Trichuris)與蟯蟲(Enterobius)。其他具重要醫學價值、發現於胃腸道以外之血液或其他組織與器官的寄生物屬,為絲蟲,例如吳策線蟲(Wuchereria)、布魯格線蟲(Brugia)、盤尾屬(Onchocerca)與羅阿絲蟲(Loa),以及龍線屬(Dracunculus)和腸外階段之腸蠕蟲-糞桿線蟲(Strongyloides)與旋毛蟲(Trichinella)。 Hookworms (Ancylostoma), spinigerum plate (Necator), roundworm (Ascaris), Strongy hides, Trichinella spiralis (Trichinella), capillariasis (Capillaria), whipworms (Trichuris) with pinworms (Enterobius). Other parasitic genus of blood or other tissues and organs found to be of great medical value outside the gastrointestinal tract, such as Wuchereria , Brugia , Onchocerca , and intestinal worms L. loa (Loa), and Long line genus (dracunculus) and parenteral stage - the fecal nematode (Strongyloides) and Trichinella spiralis (Trichinella).
其他數種蠕蟲屬與種為熟悉此技術者所知,同時也需仔細考量以本發明之化合物來對付它們。這些全都極詳盡地列舉於《Textbook of Veterinary Clinical Parasitology》(獸醫臨床寄生物學教材)(編者:E.J.L.Soulsby,由位於賓州費城的F.A.Davis Co.出版)第1卷的「Helminths」(蠕蟲)部分中;《Helminths,Arthropods,& Protozoa》(家畜的蠕蟲、節肢動物與原生動物)(《Monnig's Veterinary Helminthology and Entomology》((Monnig的獸醫蠕蟲學與昆蟲學)第6版。編者:E.J.L.Soulsby,由位於馬里蘭州巴爾的摩的Williams and Wilkins Co.出版)。 Several other genus genus and species are known to those skilled in the art, and it is also necessary to carefully consider the compounds of the present invention to deal with them. These are all very detailed in the "Textbook of Veterinary Clinical Parasitology" (Editor: EJLSoulsby, published by FADavis Co., Philadelphia, PA), Volume 1, "Helminths" (Worms) Partial; "Helminths, Arthropods, & Protozoa" (worms, arthropods and protozoa in livestock) (Monnig's Veterinary Helminthology and Entomology) (6th edition of Monnig's Veterinary Wormology and Entomology). EJLSoulsby, published by Williams and Wilkins Co., Baltimore, Maryland).
本發明的化合物亦可有效對抗數種動物外寄生物(例如:哺乳類與鳥類之節肢動物外寄生物)。 The compounds of the invention are also effective against several animal ectoparasites (e.g., arthropod ectoparasites of mammals and birds).
昆蟲與蟎類有害生物的例子包括咬蟲(如飛蠅與蚊子)、蟎、壁虱、虱子、跳蚤、蝽象、寄生蛆及類似物。 Examples of insects and mites pests include biting insects (such as flies and mosquitoes), mites, ticks, scorpions, fleas, mites, parasitic mites, and the like.
成蟲飛蠅的例子包括角蠅(Haematobia irritans)、馬蠅(Tabanus spp.)、廄螫蠅(Stomoxys calcitrans)、黑蠅(Simulium spp.)、鹿蠅(Chrysops spp.)、虱蠅(Melophagus ovinus)還有舌蠅(Glossina spp.)。寄生蠅蛆的例子包括膚蠅(Oestrus ovis 與Cuterebra spp.)、麗蠅(或Phaenicia spp.)、軟體動物旋蛆(Cochliomyia hominivorax)、牛皮蠅幼蟲(Hypoderma spp.)、羊毛蟲及馬類的胃蠅(Gastrophilus)。蚊子的例子包括家蚊屬(Culex spp.)、瘧蚊屬(Anopheles spp.)與豹腳蚊屬(Aedes spp.)。 Examples of adult fly flies include Haematobia irritans , Tabanus spp., Stomoxys calcitrans , Simulium spp., Chrysops spp., Melophagus ovinus ) There is also the Glossina spp. Examples of parasitic maggots include the fly ( Oestrus ovis and Cuterebra spp.), the fly (or Phaenicia spp.), the mollusk ( Cochliomyia hominivorax ), the larvae ( Hypoderma spp.), the woolworm and the horse. Gastrophilus . Examples of mosquitoes include Culex spp., Anopheles spp., and Aedes spp.
蟎包括Mesostigmalphatalpha spp.,例如mesostigmatids,像是雞蟎(Dermalphanyssus galphallinalphae);癢蟎或痂蟎,像是疥蟎科(Sarcoptidae spp.),以Salpharcoptes scalphabiei為例;疥蟎,像是癢蟎科(Psoroptidae spp.),包括牛足蟎(Chorioptes bovis)與綿羊癢蟎(Psoroptes ovis);恙蟎,例如恙蟎科(Trombiculidae spp.),以北美恙蟎的阿氏真恙蟎(Trombicula alfreddugesi)為例。 螨 includes Mesostigmalphatalpha spp., such as mesostigmatids , such as Dermalphanyssus galphallinalphae ; itch or sputum , such as Sarcoptidae spp., with Salpharcoptes scalphabiei as an example; 疥螨, like itch ( Psoroptidae spp), including bovine foot mites (Chorioptes bovis) and sheep itch mite (Psoroptes ovis);.. chiggers, for example TROMBICULIDAE (Trombiculidae spp), North American chiggers Ah's really chiggers (Trombicula alfreddugesi) is example.
壁虱的例子包括軟蜱,其中包括隱喙蜱科(Argasidae spp.),以Argalphas spp.與鈍緣蜱種(Ornithodoros spp.)為例;硬蜱,包括硬蜱科(Ixodidae spp.),以Rhipicephalphalus sanguineus、美國狗蜱(Dermacentor variabilis)、落磯山革蜱(Dermacentor andersoni)、美洲鈍眼蜱(Amblyomma americanum)、肩突硬蜱(Ixodes scapularis)及其他扇頭蜱屬(Rhipicephalus spp.)為例。(包括之前的牛蜱(Boophilus)屬)。 Examples of ticks include soft palate , including Argasidae spp., Argalphas spp. and Ornithodoros spp.; hard palate , including Ixodidae spp. Rhipicephalphalus sanguineus , Dermacentor variabilis , Dermacentor andersoni , Amblyomma americanum , Ixodes scapularis , and other Rhipicephalus spp. example. (including the previous genus Boophilus ).
虱子的例子包括吸虱,像是雞虱屬(Menopon spp.) Examples of scorpions include sucking, like the genus Menopon spp.
與牛羽虱屬(Bovicola spp.);咬虱,例如血虱種(Haematopinus spp.)、長顎虱種(Linognathus spp.)與盲虱屬(Solenopotes spp.)。 And Bovicola spp.; biting, such as Haematopinus spp., Linognathus spp. and Solenopotes spp.
跳蚤的例子包括櫛頭蚤屬(Ctenocephalides spp.),像是狗蚤(Ctenocephalides canis)與貓蚤(Ctenocephalides felis);客蚤屬(Xenopsylla spp.),例如東方鼠蚤(Xenopsylla cheopis);還有蚤屬(Pulex spp.),例如人蚤(Pulex irritans)。 Examples of fleas include Ctenocephalides spp., such as Ctenocephalides canis and Ctenocephalides felis ; Xenopsylla spp., such as Xenopsylla cheopis ; Pulex spp., such as Pulex irritans .
蝽象的例子包括臭蟲科(Cimicidae)或例如常見的溫帶臭蟲(Cimex lectularius);錐獵蝽亞科(Triatominae spp.),包括俗稱為接吻蟲的錐蝽,以長紅獵蝽(Rhodnius prolixus)與錐蝽屬(Triatoma spp.)為例。 Examples of artifacts include Cimicidae or, for example, the common temperate bed bug ( Cimex lectularius ); Triatominae spp., including the common genus known as the kissing worm, Rhodnius prolixus Take the example of Triatoma spp.
一般來說,飛蠅、跳蚤、虱子、蚊子、蚋、蟎、壁虱與蠕蟲,會對畜產業及伴侶動物產業造成巨大的損失。節肢動物寄生物也對人類造成困擾,也會成為人類和動物之致病生物的傳染媒介。 In general, flies, fleas, scorpions, mosquitoes, crickets, crickets, ticks and worms can cause huge losses to the livestock industry and the companion animal industry. Arthropod parasites also cause problems for humans and become vectors for pathogenic organisms of humans and animals.
其他數種寄生的無脊椎有害生物,為熟悉此技術者所知,同時也需仔細考量以本發明之化合物來對付它們。這些全都詳盡地列舉於《Medical and Veterinary Entomology》(醫學與獸醫昆蟲學)(編者:D.S.Kettle,由位於紐約與多倫多的John Wiley AND Sons出版);《Control of Arthropod Pests of Livestock:A Review of Technology》(技術之審查:牲畜節肢動物有害生物控制)(編者:R.O.Drummand、J.E.George與S.E.Kunz,由位於佛州Boca Raton的CRC Press公司出版)。 Several other parasitic invertebrate pests are known to those skilled in the art, and the compounds of the present invention need to be carefully considered to deal with them. These are all detailed in the Medical and Veterinary Entomology (editor: DSKettle, published by John Wiley AND Sons in New York and Toronto); Control of Arthropod Pests of Livestock: A Review of Technology (Technical Review: Animal Arthropod Pest Control) (Editors: RODrummand, JEGeorge and SEKunz, published by CRC Press, Inc., Boca Raton, FL).
本發明亦提供了控制有害生物的方法(例如蚊子與其他疾病傳染媒介;可另外參考http://www.who.int/malaria/vector_control/irs/en/)。在一個 具體實例中,控制有害生物的方法包含了藉由刷、滾、噴灑、散佈或浸入的方式,將本發明之組成物用於目標有害生物、其所在之處、物體表面或基質上。舉例來說,對於將室內滯留噴霧(IRS)應用於物體(如牆壁、天花板或地板)表面,本發明的方法已仔細考量到此一用途。在另一個具體實例中,根據仔細的考量,也可將此種組成物用於基質上,例如以網製品、衣服、寢具、窗簾與帳篷之形式存在(或可用於製造這些產品)的不織布或布料材質。 The invention also provides methods of controlling pests (e.g., mosquitoes and other disease vectors; additional reference may be made to http://www.who.int/malaria/vector_control/irs/en/). in a In a specific example, the method of controlling a pest comprises applying the composition of the present invention to a target pest, where it is located, the surface of the object, or a substrate by brushing, rolling, spraying, spreading or immersing. For example, for applying an indoor residual spray (IRS) to an object (such as a wall, ceiling or floor) surface, the method of the present invention has been carefully considered for this purpose. In another embodiment, such compositions may also be applied to a substrate, such as in the form of mesh products, clothing, bedding, curtains, and tents (or may be used to make these products), depending on careful considerations. Or cloth material.
在一個具體實例中,控制此類有害生物的方法包含了將殺有害生物有效量的本發明之組成物,施用於目標有害生物上、其所在之處、物體表面或基質上,以在表面或基質上提供有效的殘效殺蟲活性。可藉由刷、滾、噴灑、散佈或浸入本發明之殺蟲組成物,來進行此類的應用。舉例來說,對於將室內滯留噴霧(IRS)應用於物體(如牆壁、天花板或地板)表面,本發明的方法已仔細考量到此一用途,以便在表面上提供有效的殘效殺蟲活性。在另一個具體實例中,根據仔細的考量,也可將此種組成物用於基質上,例如以網製品、衣服、寢具、窗簾與帳篷之形式存在(或可用於製造這些產品)的布料材質,以對有害生物進行殘效控制。 In one embodiment, a method of controlling such pests comprises applying a pesticidally effective amount of a composition of the invention to a target pest, where it is located, on a surface or substrate of the object, on a surface or Provides effective residual insecticidal activity on the substrate. Such applications can be carried out by brushing, rolling, spraying, spreading or dipping into the insecticidal compositions of the present invention. For example, for applying an indoor residual spray (IRS) to an object (such as a wall, ceiling or floor) surface, the method of the present invention has been carefully considered for such use to provide effective residual pesticidal activity on the surface. In another embodiment, such a composition may also be applied to a substrate, such as in the form of a web product, clothing, bedding, curtains, and tents (or may be used to make these products), depending on careful considerations. Material to control residual pests.
要處理的基質(包括不織布、布料或網製品)可由天然纖維製成,如棉花、酒椰葉、黃麻、亞麻、劍麻、粗麻布、羊毛,或合成纖維,如聚醯胺、聚酯、聚丙烯、聚丙烯腈及類似物。聚酯則特別合適。織物的處理方法係自以下來源而得知,如《Handbuch Textilveredlung:Band 1:Ausrü stung,Band 2:Farbgebung,Band 3:Beschichtung,Band 4:Umwelttechnik》(第1卷:設備、第2卷:顏色、第3卷:塗層、第4卷:環境科技);出版社:Deutscher Fachverlag;版本:15.;修訂版本:2006年4月17日;ISBN-10:3866410123;ISBN-13:978-3866410121,尤其請參閱Band 1:Ausrütung(第1卷:設備)第27-198頁,特別是第118頁;或是WO2008151984、WO2003034823、US5631072、WO200564072、WO2006128870、EP1724392、WO2005064072、WO2005113886或WO2007090739。 The substrate to be treated (including non-woven fabrics, cloth or net products) can be made of natural fibers such as cotton, raffia, jute, linen, sisal, burlap, wool, or synthetic fibers such as polyamide or polyester. , polypropylene, polyacrylonitrile and the like. Polyester is particularly suitable. The processing method of the fabric is known from the following sources, such as "Handbuch Textilveredlung: Band 1: Ausrü Stung, Band 2: Farbgebung, Band 3: Beschichtung, Band 4: Umwelttechnik (Vol. 1: Equipment, Volume 2: Color, Volume 3: Coatings, Volume 4: Environmental Technology); Publisher: Deutscher Fachverlag ;Version: 15.; Revised: April 17, 2006; ISBN-10: 3866410123; ISBN-13: 978-3866410121, see, in particular, Band 1: Ausrütung (Vol. 1: Equipment), pp. 27-198. In particular, page 118; or WO2008151984, WO2003034823, US5631072, WO200564072, WO2006128870, EP1724392, WO2005064072, WO2005113886 or WO2007090739.
本發明的化合物亦可能有效對抗外寄生物,包括:諸如角蠅(Haematobia(Lyperosia)irritans)、黑蠅種(Simulium spp.)、采采蠅種(Glossina spp.)頭蠅(Hydrotaea irritans)、面蠅(Musca autumnalis)、家蠅(Musca domestica)、汗蠅(Morellia simplex)、馬蠅種(Tabanus spp.)、牛蠅(Hypoderma bovis)、紋皮蠅(Hypoderma lineatum)、絲光綠蠅(Lucilia sericata)、銅綠蠅(Lucilia cuprina)、綠頭蒼蠅種(Calliphora spp.)、原伏蠅種(Protophormia spp.)、羊狂蠅(Oestrus ovis)、庫蠓種(Culicoides spp.)、馬虱蠅(Hippobosca equine)、馬腸胃蠅(Gastrophilus intestinalis)、赤尾胃蠅(Gastrophilus haemorrhoidalis)與鼻胃蠅(Gastrophilus nasalis)等蒼蠅;諸如牛毛虱(Bovicola(Damalinia)bovis)、馬毛虱(Bovicola equi)、驢血虱(Haematopinus asini)、貓羽虱(Felicola subrostratus)、狗虱(Heterodoxus spiniger)、棘顎虱(Lignonathus setosus)與犬囓毛虱(Trichodectes canis)等虱 子;諸如羊蜱蠅(Melophagus ovinus)等蠅類,以及諸如癢蟎種(Psoroptes spp.)、疥癬蟎(Sarcoptes scabei)、牛足蟎(Chorioptes bovis)、馬蠕形蟎(Demodex equi)、姬螯蟎種(Cheyletiella spp.)、貓耳蟎(Notoedres cati)、羌蟎種(Trombicula spp.)與耳蟎(Otodectes cyanotis)等蟎類。 The compounds of the invention may also be effective against ectoparasites, including, for example, Haematobia (Lyperosia) irritans , Simulium spp., Glossina spp., Hydrotaea irritans , Musca autumnalis , Musca domestica , Morellia simplex , Tabanus spp., Hypoderma bovis , Hypoderma lineatum , Lucilia Sericata ), Lucilia cuprina , Calliphora spp., Protophormia spp., Oestrus ovis , Culicoides spp., horsefly ( Hippobosca equine ), Gastrophilus intestinalis , Gastrophilus haemorrhoidalis and Gastrophilus nasalis ; such as Bovicola (Damalinia bovis ), Bovicola equi , 驴 Hazeltopinus asini , Felicola subrostratus , Heterodoxus spiniger , Lignonathus setosus , and Trichodectes canis ; Such as flies such as Melophagus ovinus , and such as Psoroptes spp., Sarcoptes scabei , Chorioptes bovis , Demodex equi , and Alfalfa Species such as Cheyletiella spp., Notoedres cati , Trombicula spp. and Otodectes cyanotis .
本發明的治療是藉由習知療法,例如以藥片、膠囊、藥水、灌藥、藥粒、藥膏、藥丸、灌食術、或栓劑等形式的經腸給藥療法;或是藉由例如以注射(包括肌肉注射、皮下注射、靜脈注射、腹腔內注射)等非口服給藥療法或是注射充填方式;或是藉由鼻腔給藥療法。 The treatment of the present invention is by enteral administration in the form of a conventional therapy, for example, in the form of a tablet, a capsule, a syrup, a drug, a granule, an ointment, a pill, a medicinal herb, or a suppository; or by, for example, Non-oral administration or injection filling methods such as intramuscular injection, subcutaneous injection, intravenous injection, intraperitoneal injection; or intranasal administration.
當組合額外的生物活性成分施用本發明的化合物時,可個別用藥,例如作為個別的組成物。在這種情況下,生物活性成分得予以同時或相繼用藥。或者,生物活性成分也可作為一個組成物的構成成分。 When the additional biologically active ingredient is administered in combination with a compound of the invention, it can be administered individually, for example as an individual composition. In this case, the biologically active ingredients may be administered simultaneously or sequentially. Alternatively, the bioactive ingredient can also be used as a constituent of a composition.
本發明的化合物得以受控制的釋放形式進行用藥,例如以皮下或口服給藥的緩慢釋放形式。 The compounds of the invention are administered in a controlled release form, for example in a slow release form for subcutaneous or oral administration.
一般而言,根據本發明的殺有害生物組成物包括一個本發明的化合物,可選擇性地組合一個額外的生物活性成分、或N-氧化物或其鹽類,以及包含與想要的給藥途徑相關而選取的賦形劑與輔助劑的一個或多個醫藥或獸醫用藥可接受的載體(例如:口服給藥或諸如注射等的非口服給藥)並與標準作法一致。此外,根據與組成物中的一個或多個活性成分的相容性,包括與pH值及含水量有關的穩定度等等之類的考量,而選擇一個合適的載體。因此,本發明的 化合物可保護動物遠離寄生的無脊椎有害生物,這點是值得注意的,其包含殺寄生物有效量的本發明之化合物,且選擇性地組合一個額外的生物活性成分,以及至少一個載體。 In general, the pesticidal composition according to the invention comprises a compound of the invention which can be optionally combined with an additional biologically active ingredient, or an N-oxide or a salt thereof, and with the desired administration. One or more pharmaceutically or veterinary acceptable carriers (e.g., for oral administration or parenteral administration such as injection) of the excipients and adjuvants selected in connection with the route are consistent with standard practice. In addition, a suitable carrier is selected based on considerations such as compatibility with one or more active ingredients in the composition, including stability in relation to pH and water content, and the like. Therefore, the present invention It is worth noting that the compound protects the animal from parasitic invertebrate pests, comprising a parasiticidally effective amount of a compound of the invention, and optionally combining an additional bioactive ingredient, and at least one carrier.
針對包括靜脈注射、肌肉注射、皮下注射等等的非口服給藥,本發明的化合物能於油性或水性媒介物中以懸浮液、溶劑或乳劑的形式製成用藥,且能包含懸浮劑、穩定劑和/或分散劑等等的附加劑。 For parenteral administration including intravenous, intramuscular, subcutaneous injection and the like, the compound of the present invention can be formulated as a suspension, a solvent or an emulsion in an oily or aqueous vehicle, and can contain a suspending agent and be stable. Additives for agents and/or dispersants and the like.
本發明的化合物亦能針對一次性注射或持續靜脈滴注而製成用藥。注射的藥品成分包括活性成分的水溶性形式之水性溶液(例如:活性化合鹽),最好是以含有其他賦形劑或輔助劑、且與生理相容的緩衝劑,這是眾人皆知的醫藥調配物技巧。此外,可以用親脂性媒介物備製活性化合物的懸浮液。合適的親脂性媒介物包括芝麻油之類的脂肪油,或油酸乙酯與三酸甘油酯等等的合成脂肪酸酯,或是脂質體等等的材料。 The compounds of the invention can also be formulated for either single injection or continuous intravenous drip. The pharmaceutical ingredient to be injected comprises an aqueous solution (for example, an active compound salt) in a water-soluble form of the active ingredient, preferably a physiologically compatible buffer containing other excipients or adjuvants, which is well known. Medical formula tips. In addition, suspensions of the active compounds can be prepared with lipophilic vehicles. Suitable lipophilic vehicles include fatty oils such as sesame oil, or synthetic fatty acid esters of ethyl oleate and triglycerides, or materials such as liposomes and the like.
水性注射懸浮液可能包含會增加懸浮液黏稠度的物質,例如羧甲基纖維素鈉、山梨糖醇、或是葡聚糖。注射液的調配物可能以單位劑量形式呈現,例如:裝在安瓿內或是裝在多劑量容器內。或者,在使用之前,活性成分可能為粉末形式,以與合適的媒介物組合,例如:無菌無致熱物的水。 Aqueous injection suspensions may contain materials which increase the viscosity of the suspension, such as sodium carboxymethylcellulose, sorbitol, or dextran. The formulation of the injectable solution may be presented in unit dosage form, for example, in an ampoule or in a multi-dose container. Alternatively, prior to use, the active ingredient may be in powder form for combination with a suitable vehicle, for example, sterile non-pyrogenic water.
除了前述調配物之外,本發明的化合物亦可能以長效製劑形式製成調配物。這樣的長效調配物的給藥方式可能 採注射充填(例如,經皮下或是肌肉)的方式或是採肌肉注射或皮下注射的方式。 In addition to the formulations described above, the compounds of the invention may also be formulated in the form of a depot preparation. Such long-acting formulations may be administered in a manner Injection (eg, subcutaneous or intramuscular) or intramuscular or subcutaneous injection.
本發明的化合物可針對此給藥途徑製成調配物,搭配合適的聚合物材料或是疏水性材料(例如,在含有醫藥用可接受油脂的乳劑中),或搭配離子交換樹脂,或是作為微溶衍生物,例如,但不限於,微溶鹽等。 The compounds of the present invention can be formulated for this route of administration, with suitable polymeric materials or hydrophobic materials (for example, in emulsions containing pharmaceutically acceptable oils and fats), or with ion exchange resins, or as A slightly soluble derivative such as, but not limited to, a sparingly soluble salt or the like.
針對吸入式給藥方式,本發明的化合物可利用加壓包或是噴霧器,以及合適的推進劑(例如,但不限於,二氯二氟甲烷、三氯氟甲烷、二氯四氟乙烷或是二氧化碳),以噴霧形式傳遞。就加壓式的氣溶膠而言,可藉由提供活栓傳送經儀表計量的容量來控制劑量單位。 For inhaled administration, the compounds of the invention may utilize a pressurized pack or nebulizer, as well as suitable propellants (such as, but not limited to, dichlorodifluoromethane, trichlorofluoromethane, dichlorotetrafluoroethane or It is carbon dioxide) and is delivered as a spray. In the case of a pressurized aerosol, the dosage unit can be controlled by providing a stopcock to deliver a metered volume.
舉例來說,使用於吸入器或吹藥器的凝膠膠囊和藥筒可以用含有化合物與諸如乳糖或澱粉等之類合適粉底的粉末混合物製成調配物。 For example, gel capsules and cartridges for use in an inhaler or insufflator can be formulated with a powder mixture containing a compound and a suitable foundation such as lactose or starch.
本發明的化合物可具有良好的藥物動力與藥物效力性質,提供自口服給藥與攝取的全身性可用性。因此,經由所要保護的動物攝取之後,本發明的化合物於血流中達殺寄生物的有效濃度時,即可保護接受治療的動物免於遭到諸如跳蚤、壁虱和虱子之類的吸血有害生物叮咬。因此,值得注意的是以口服給藥保護動物遠離無脊椎寄生有害生物的組成物(亦即,除了內含達殺寄生物有效濃度之本發明化合物之外,尚包含一個或多個選自適合的口服給藥與餵養濃縮物載體的結合劑或填充料的載體)。 The compounds of the invention may have good pharmacokinetic and pharmaceutical efficacy properties, providing systemic availability from oral administration and ingestion. Thus, upon ingestion of the animal to be protected, the compound of the invention, when in the bloodstream reaches an effective concentration of parasiticidal, protects the treated animal from blood-sucking such as fleas, ticks and lice. Biological bites. Therefore, it is worth noting that the composition for protecting the animal from the invertebrate parasitic pest by oral administration (ie, in addition to the compound of the present invention containing an effective concentration of the parasiticidal, further comprises one or more selected from suitable Oral administration to a carrier or a carrier for feeding a concentrate carrier).
針對溶劑(最即可使用的吸收形式)、乳劑、懸浮液、藥 膏、凝膠劑、膠囊、藥片、大丸藥、粉劑、粒劑、瘤胃滯留與飼料/水/舔塊等等形式的口服給藥,能以已知在此技術方面適合於口服給藥組成物的粘合劑/填充料,例如糖與糖衍生物(例如乳糖、蔗糖、甘露醇、山梨糖醇)、澱粉(例如玉米澱粉、小麥澱粉、米澱粉、馬鈴薯澱粉)、纖維素及衍生物(例如甲基纖維素、羧甲基纖維素、乙羥纖維)、蛋白質衍生物(例如玉蜀黍蛋白質、明膠),以及合成聚合物(例如聚乙烯醇、聚乙烯吡咯啶酮)等等。如果需要的話,可以加入潤滑油(例如硬脂酸鎂)、崩解劑(例如交聯聚乙烯吡咯啶酮、瓊脂、褐藻酸)和染料或顏料。藥膏和凝膠往往還含有黏合劑(例如洋槐、褐藻酸、膨潤土、纖維素、黃原膠、膠體矽酸鋁鎂),以幫助組成物保持與口腔接觸且不易被彈出。 For solvents (the most usable form of absorption), emulsions, suspensions, medicines Oral administration in the form of a cream, a gel, a capsule, a tablet, a bolus, a powder, a granule, a rumen retention, and a feed/water/clam block, etc., can be suitably formulated for oral administration in the art. Binders/fillers such as sugars and sugar derivatives (eg lactose, sucrose, mannitol, sorbitol), starch (eg corn starch, wheat starch, rice starch, potato starch), cellulose and derivatives ( For example, methyl cellulose, carboxymethyl cellulose, hydroxy fiber), protein derivatives (such as maize protein, gelatin), and synthetic polymers (such as polyvinyl alcohol, polyvinylpyrrolidone) and the like. If necessary, a lubricating oil (for example, magnesium stearate), a disintegrating agent (for example, crosslinked polyvinylpyrrolidone, agar, alginic acid), and a dye or pigment may be added. Ointments and gels often also contain binders (eg, artichoke, alginic acid, bentonite, cellulose, xanthan gum, colloidal aluminum magnesium citrate) to help keep the composition in contact with the oral cavity and are not easily ejected.
在具體實例中,將本發明的組成物配製成可咀嚼及/或可食用的產品(例如可嚼性治療食品或食用藥片)。很理想的一點是,受保護的動物會青睞這類產品的滋味、質地及/或香氣,而更容易服下本發明的化合物。 In a specific example, the compositions of the present invention are formulated into chewable and/or edible products (e.g., chewable therapeutic foods or edible tablets). Ideally, protected animals will appreciate the taste, texture and/or aroma of such products, and will more readily take the compounds of the present invention.
如果殺寄生物組成物的形式是濃縮飼料的話,則一般會從高效性的飼料、飼料穀物或濃縮蛋白質當中選擇載體。 If the form of the parasiticidal composition is a concentrated feed, the carrier is generally selected from high-efficiency feeds, feed grains or concentrated proteins.
除了殺寄生物活性成分之外,這種含有濃縮飼料的組成物還能夠含有促進動物健康或生長、提高屠宰動物的肉質或對畜牧業有用的添加物。 In addition to the parasiticidally active ingredient, such concentrated feed compositions can also contain additives that promote the health or growth of the animal, increase the meat quality of the slaughtered animal, or are useful for the livestock industry.
這些添加物可以包括如維他命、抗生素、化學療法、抑菌劑、阻止黴菌生長劑、抑制球蟲劑和激素。 These additives may include, for example, vitamins, antibiotics, chemotherapy, bacteriostats, mold growth inhibitors, coccidiostats, and hormones.
也能利用可可油或其他甘油脂之類的習知栓劑基,在 栓劑或保留灌腸等之類的直腸組成物中配製本發明的化合物。 It is also possible to use a conventional suppository base such as cocoa butter or other glycerides. The compounds of the invention are formulated in rectal compositions such as suppositories or retention enemas and the like.
本發明所用之方法的調配物可包括抗氧化劑,例如BHT(二丁基羥基甲苯)。抗氧化劑的劑量一般是在0.1-5%(wt/vol)。有些調配物需要增溶劑,例如油酸,以便溶解活性劑,特別是如果包括多殺菌素的話。使用於這些澆潑調配物的常見擴展劑包括肉荳蔻酸異丙酯、棕櫚酸異丙酯、飽和C12-C18脂肪醇的辛酸/癸酸酯、油酸、油烯基酯、油酸乙酯、三酸甘油酯、矽油和二丙二醇甲醚。本發明所用之方法的澆潑調配物係根據已知的技術來製備。以澆潑的方法做為溶液時,係將驅蟲劑/殺蟲劑與載體或媒介物混合,如果需要的話,還可用熱和攪拌的方式混合。可以將輔助成分或附加成分添加至活性劑與載體的混合物,或是也可以在添加載體之前,將它們先與活性劑混合。乳劑或懸浮液形式的澆潑調配物,也是使用已知技術做類似的製備。 Formulations of the methods used in the present invention may include an antioxidant such as BHT (dibutylhydroxytoluene). The dose of the antioxidant is generally from 0.1 to 5% (wt/vol). Some formulations require a solubilizing agent, such as oleic acid, to solubilize the active agent, especially if spinosyn is included. These pour-on formulations used in the composition of common spreading agents include isopropyl myristate, isopropyl palmitate, C 12 -C 18 saturated fatty alcohols caprylic / capric acid esters, oleic acid, oleyl oleate, Ethyl ester, triglyceride, eucalyptus oil and dipropylene glycol methyl ether. The pour-on formulations of the methods used in the present invention are prepared according to known techniques. When the method of pouring is used as a solution, the insect repellent/insecticide is mixed with a carrier or a vehicle, and if necessary, it may be mixed by heat and stirring. The auxiliary ingredients or additional ingredients may be added to the mixture of the active agent and the carrier, or they may be first mixed with the active agent before the carrier is added. Pour-on formulations in the form of emulsions or suspensions are also prepared analogously using known techniques.
可以運用相對疏水性藥物化合物的其他輸送系統。脂質體和乳劑是眾所周知的疏水性藥物輸送載具或載體例子。此外,如果有需要的話,也可以使用諸如二甲亞碸之類的有機溶劑。 Other delivery systems that are relatively hydrophobic drug compounds can be employed. Liposomes and emulsions are well known examples of hydrophobic drug delivery vehicles or carriers. In addition, an organic solvent such as dimethyl hydrazine can also be used if necessary.
要應用多少比例才能有效控制寄生的無脊椎有害生物(例如「殺有害生物有效量」),將取決於多種因素,例如欲控制之寄生無脊椎有害生物的種類、有害生物的生命週期、生命階段、其大小、位置、一年裡的時間點、宿主作物或動物、攝食行為、交配行為、環境濕度、溫度等等。 技巧熟練的人可以很容易地判定需要多少殺有害生物有效量,才能達到想要的寄生的無脊椎有害生物控制程度。 How much proportion should be applied to effectively control parasitic invertebrate pests (such as "killing pest effective amount"), depending on various factors, such as the type of parasitic invertebrate pest to be controlled, the life cycle of the pest, and the life stage , its size, location, time of year, host crop or animal, feeding behavior, mating behavior, environmental humidity, temperature, etc. Skilled people can easily determine how much pesticidal effective amount is needed to achieve the desired parasitic invertebrate pest control.
一般來說,在獸醫用途方面,會以殺有害生物有效量來提供本發明的化合物,讓動物(特別是恆溫動物)不被寄生的無脊椎有害生物所侵擾。 In general, in veterinary use, the compounds of the invention are provided in a pesticidally effective amount to render the animal (especially warm-blooded animals) infested by parasitic invertebrate pests.
殺有害生物有效量是指達到顯著效果所需的活性成分量,以減少目標寄生的無脊椎有害生物的出現率或活動。技巧熟練的人將會明瞭殺有害生物有效量會因多種因素而有所不同,如各種對本發明的方法有用的化合物和組成物、想要的殺蟲效果和持續時間、目標的寄生的無脊椎有害生物種類、受保護的動物、應用的模式等等,並且可藉由簡單的實驗來判定達到特定結果所需的量。 The pesticidal effective amount refers to the amount of active ingredient required to achieve a significant effect to reduce the incidence or activity of the target parasitic invertebrate pest. Skilled people will understand that the effective amount of pesticidal agents will vary depending on a variety of factors, such as the various compounds and compositions useful for the methods of the invention, the desired insecticidal effect and duration, and the parasitic invertebrate of the target. Species of pests, protected animals, patterns of application, etc., and the amount required to achieve a particular result can be determined by simple experimentation.
針對動物的口服或非口服給藥,本發明的組成物每隔一段適當時間所投予的劑量,一般是從0.01毫克/公斤左右到100毫克/公斤左右,而且最好是動物體重的0.01毫克/公斤左右到30毫克/公斤左右。 For oral or parenteral administration of the animal, the dose of the composition of the present invention administered at an appropriate time is generally from about 0.01 mg/kg to about 100 mg/kg, and preferably 0.01 mg of the animal's body weight. / kg or so to 30 mg / kg or so.
為動物供給本發明之組成物的適當間隔時間,是從每天左右到每年左右。值得注意的是每週左右到每隔6個月左右這個給藥間隔時間,而每月給藥間隔時間(亦即每個月為動物供給化合物一次)則特別值得注意。 The appropriate interval for supplying the compositions of the present invention to animals is from about daily to about yearly. It is worth noting that this dosing interval is from about every week to about every other month, and that the monthly dosing interval (that is, once a month for the animal to supply the compound) is particularly noteworthy.
本發明亦提供了控制有害生物的方法(例如蚊子與其他疾病傳染媒介)。在一個具體實例中,控制有害生物的方法包含了藉由刷、滾、噴灑、散佈或浸入的方式,將本發明之組成物施用於目標有害生物、其所在之處、物體表面或 基質上。舉例來說,對於將室內滯留噴霧(IRS)應用於物體(如牆壁、天花板或地板)表面,本發明的方法已仔細考量到此一用途。在另一個具體實例中,根據仔細的考量,也可將此種組成物用於基質上,例如以網製品、衣服、寢具、窗簾與帳篷之形式存在(或可用於製造這些產品)的不織布或布料材質。 The invention also provides methods of controlling pests (e.g., mosquitoes and other disease vectors). In one embodiment, the method of controlling a pest comprises applying the composition of the present invention to a target pest, where it is located, the surface of the object, or by brushing, rolling, spraying, spreading or immersing. On the substrate. For example, for applying an indoor residual spray (IRS) to an object (such as a wall, ceiling or floor) surface, the method of the present invention has been carefully considered for this purpose. In another embodiment, such compositions may also be applied to a substrate, such as in the form of mesh products, clothing, bedding, curtains, and tents (or may be used to make these products), depending on careful considerations. Or cloth material.
在一個具體實例中,控制此類有害生物的方法包含了將殺有害生物有效量之本發明組成物施用於目標有害生物上、其所在之處、物體表面或基質上,以在表面或基質上提供有效的殘效殺有害生物活性。可藉由刷、滾、噴灑、散佈或浸入本發明之殺有害生物組成物,來進行此類的應用。舉例來說,對於將室內滯留噴霧(IRS)應用於物體(如牆壁、天花板或地板)表面,本發明的方法已仔細考量到此一用途,以便在表面上提供有效的殘效殺有害生物活性。在另一個具體實例中,根據仔細的考量,也可將此種組成物用於基質上,例如以網製品、衣服、寢具、窗簾與帳篷之形式存在(或可用於製造這些產品)的布料材質,以對有害生物進行殘效控制。 In one embodiment, a method of controlling such pests comprises applying a pesticidally effective amount of a composition of the invention to a target pest, where it is located, on a surface or substrate of the object, on a surface or substrate. Provides effective residual pesticidal activity. Such applications can be carried out by brushing, rolling, spraying, spreading or immersing in the pesticidal composition of the present invention. For example, for applying an indoor residual spray (IRS) to an object (such as a wall, ceiling or floor) surface, the method of the present invention has been carefully considered for such use to provide effective residual pesticidal activity on the surface. In another embodiment, such a composition may also be applied to a substrate, such as in the form of a web product, clothing, bedding, curtains, and tents (or may be used to make these products), depending on careful considerations. Material to control residual pests.
要處理的基質(包括不織布、布料或網製品)可由天然纖維製成,如棉花、酒椰葉、黃麻、亞麻、劍麻、粗麻布、羊毛,或合成纖維,如聚醯胺、聚酯、聚丙烯、聚丙烯腈等等。聚酯則特別合適。織物的處理方法係自以下來源而得知,如《Handbuch Textilveredlung:Band 1:Ausrütung,Band 2:Farbgebung,Band 3:Beschichtung,Band 4:Umwelttechnik》 (第1卷:設備、第2卷:顏色、第3卷:塗層、第4卷:環境科技);出版社:Deutscher Fachverlag;版本:15.;修訂版本:2006年4月17日;ISBN-10:3866410123;ISBN-13:978-3866410121,尤其請參閱Band 1:Ausr ung(第1卷:設備)第27-198頁,特別是第118頁;或是WO2008151984、WO2003034823、US5631072、WO200564072、WO2006128870、EP1724392、WO2005064072、WO2005113886或WO2007090739。 The substrate to be treated (including non-woven fabrics, cloth or net products) can be made of natural fibers such as cotton, raffia, jute, linen, sisal, burlap, wool, or synthetic fibers such as polyamide or polyester. , polypropylene, polyacrylonitrile and so on. Polyester is particularly suitable. The processing method of the fabric is known from the following sources, such as "Handbuch Textilveredlung: Band 1: Ausrütung, Band 2: Farbgebung, Band 3: Beschichtung, Band 4: Umwelttechnik" (Volume 1: Equipment, Volume 2: Color, Volume 3: Coatings, Volume 4: Environmental Technology); Publisher: Deutscher Fachverlag; Version: 15.; Revision: April 17, 2006; ISBN -10:3866410123; ISBN-13: 978-3866410121, in particular, see Band 1: Ausr ung (Vol. 1: Equipment) on pages 27-198, especially page 118; or WO2008151984, WO2003034823, US5631072, WO200564072, WO2006128870, EP1724392, WO2005064072, WO2005113886 or WO2007090739.
此處使用的「植物」一詞包括幼苗、灌木及樹木。 The term "plant" as used herein includes seedlings, shrubs and trees.
「作物」一詞應被理解為也包括具有以下特點的作物植物:使用重組DNA技術加以轉換,而且轉換到能夠合成一個或多個選擇性起作用的毒素,例如已知是來自像產毒細菌(特別是屬於內孢子形桿菌的細菌)的毒素。 The term "crop" should be understood to also include crop plants that are transformed using recombinant DNA techniques and converted to be capable of synthesizing one or more selectively acting toxins, for example from bacteria-producing bacteria. Toxins (especially bacteria belonging to the genus Neisseria).
舉例來說,可以由這些基因轉殖植物釋出的毒素包括來自蠟樣芽胞桿菌或乳化菌的殺蟲蛋白質;或是來自蘇雲金芽孢桿菌(如δ-內毒素)的殺蟲蛋白質,例如Cry1Ab、Cry1Ac、Cry1F、Cry1Fa2、Cry2Ab、Cry3A、Cry3Bb1或Cry9C;或例如VIP1、VIP2、VIP3或Vip3A等等的營養性(vegetative)殺蟲蛋白(VIP);或細菌移生線蟲(如發光光狀桿菌(Photorhabdus luminescens)、嗜線蟲致病桿菌(Xenorhabdus nematophilus)之類的發光桿菌(Photorhabdus spp.)或異桿菌(Xenorhabdusspp.))的殺蟲蛋白質;用動物製成的毒素,如蠍毒素、蛛形綱動物毒素、黃蜂毒素和其他昆蟲特定神經毒素;由菌類植物所產生的毒素,如鏈黴菌 毒素;植物凝集素,例如豌豆凝集素、大麥凝集素或雪花蓮凝集素;白芍提取物凝聚素;蛋白酶抑制劑,例如胰蛋白酶抑制劑、絲胺酸蛋白酶抑制劑、patatin、胱抑素、木瓜蛋白酶抑制劑;核糖體失活蛋白(RIP),例如蓖麻毒素、玉米-RIP、相思豆毒蛋白、絲瓜素、皂草素或異株腹瀉毒蛋白);類固醇代謝酶,例如3-羥類固醇氧化酶、蛻皮激素UDP糖基轉移酶、膽固醇氧化酶、蛻皮抑制劑、HMG-COA還原酶、離子通道阻滯劑,例如鈉或鈣通道、保幼激素酯酶、利尿激素受體、二苯乙烯合酶,聯苯甲基合酶,幾丁質酶和葡聚醣酶的阻滯劑。 For example, toxins that can be released from these genetically transgenic plants include insecticidal proteins from Bacillus cereus or emulsified bacteria; or insecticidal proteins from Bacillus thuringiensis (such as delta-endotoxin), such as Cry1Ab, Cry1Ac, Cry1F, Cry1Fa2, Cry2Ab, Cry3A, Cry3Bb1 or Cry9C; or a vegetative insecticidal protein (VIP) such as VIP1, VIP2, VIP3 or Vip3A; or a bacterial-borne nematode (such as a luminescent photobacterium) Photoinhabdus luminescens), insecticidal proteins of Photorhabdus spp. or Xenorhabdusspp., such as Xenorhabdus nematophilus; toxins made from animals, such as scorpion toxin, arachnid Animal toxins, wasp toxins and other insect-specific neurotoxins; toxins produced by fungi, such as Streptomyces Toxin; plant lectin, such as pea lectin, barley lectin or snowdrop lectin; white peony extract lectin; protease inhibitors such as trypsin inhibitor, serine protease inhibitor, patatin, cystatin, Papain inhibitor; ribosome inactivating protein (RIP), such as ricin, corn-RIP, acacia, loofah, saporin or diarrhea protein; steroid metabolism enzymes such as 3-hydroxyl Steroid oxidase, ecdysone UDP glycosyltransferase, cholesterol oxidase, ecdysone inhibitor, HMG-COA reductase, ion channel blocker, such as sodium or calcium channel, juvenile hormone esterase, diuretic hormone receptor, two Styryl synthase, biphenyl methyl synthase, chitinase and glucanase blockers.
在本發明中,有些部分應被理解為δ-內毒素,例如Cry1Ab、Cry1Ac、Cry1F、Cry1Fa2、Cry2Ab、Cry3A、Cry3Bb1或Cry9C,或營養性殺蟲蛋白(VIP),例如Vip1、Vip2、Vip3或Vip3A,特別還有混合毒素、截斷毒素和改造毒素。藉著這些蛋白質不同結構域的新組合,以重新組合的方式產生混合毒素(範例請參看:WO02/15701)。截斷毒素則為人所知,例如被截斷的Cry1Ab。而在改造毒素方面,自然發生毒素的一個或多個胺基酸會被取代。在這種胺基酸取代的情況中,最好是將非天然存在的蛋白酶識別序列插入毒素中。舉例來說,像是在Cry3A055方面,將組織蛋白酶-G-識別序列插入Cry3A毒素中(參看WO 03/018810)。 In the present invention, some portions are to be understood as delta-endotoxins, such as Cry1Ab, Cry1Ac, Cry1F, Cry1Fa2, Cry2Ab, Cry3A, Cry3Bb1 or Cry9C, or nutritive insecticidal proteins (VIP), such as Vip1, Vip2, Vip3 or Vip3A, especially mixed toxins, truncated toxins and engineered toxins. Hybrid toxins are produced in a recombination manner by a new combination of different domains of these proteins (see, for example, WO02/15701). Truncated toxins are known, such as the truncated Cry1Ab. In the modification of toxins, one or more amino acids of naturally occurring toxins are replaced. In the case of such amino acid substitution, it is preferred to insert a non-naturally occurring protease recognition sequence into the toxin. For example, as in the case of Cry3A055, a cathepsin-G-recognition sequence is inserted into the Cry3A toxin (see WO 03/018810).
在EP-A-0 374 753、WO 93/07278、WO 95/34656、EP-A-0 427 529、EP-A-451 878和WO 03/052073等等中,已揭露這種能夠合成此類毒素的毒素或基因轉殖植物例子。 It has been disclosed in EP-A-0 374 753, WO 93/07278, WO 95/34656, EP-A-0 427 529, EP-A-451 878 and WO 03/052073, etc. Examples of toxins or gene transfer plants of toxins.
熟悉該項技術領域者通常都知道這種基因轉殖植物的製備過程,而且在例如上述提到的出版品當中皆已描述這些過程。CryI型去氧核糖核酸及其製備事宜,則可從WO 95/34656、EP-A-0 367 474、EP-A-0 401 979和WO 90/13651等來得知。 The preparation of such genetically transformed plants is generally known to those skilled in the art, and these processes have been described, for example, in the publications mentioned above. CryI-type deoxyribonucleic acid and its preparation are known from WO 95/34656, EP-A-0 367 474, EP-A-0 401 979 and WO 90/13651.
包含在基因轉殖植物當中的毒素,會為植物賦予對有害昆蟲的耐受性。這種昆蟲可出現在任何昆蟲分類群當中,但特別常被歸類在甲蟲(鞘翅目)、雙翅蟲(雙翅目)和蝴蝶(鱗翅目)方面。 Toxins contained in genetically transformed plants impart tolerance to harmful insects to plants. This insect can occur in any insect taxonomic group, but is often classified as a beetle (Coleoptera), a double-winged worm (Diptera), and a butterfly (Lepidoptera).
有一種或多種基因編碼了殺蟲抵抗性、並釋出一種或多種毒素的基因轉殖植物,不僅為人所知,而且其中有些是市售品。這類植物的例子有:YieldGard®(釋出Cry1Ab毒素之玉米品種);YieldGard Rootworm®(釋出Cry3Bb1毒素之玉米品種);YieldGard Plus®(釋出Cry1Ab和Cry3Bb1毒素之玉米品種);Starlink®(釋出Cry9C毒素之玉米品種);Herculex I®(釋出Cry1Fa2毒素和草丁膦N-乙醯轉移酶酵素(PAT)以達草胺磷除草劑耐受性之玉米品種);NuCOTN 33B®(釋出Cry1Ac毒素之棉花品種);Bollgard I®(釋出Cry1Ac毒素之棉花品種);Bollgard II®(釋出Cry1Ac和Cry2Ab毒素之棉花品種);VipCot®(釋出Vip3A和Cry1Ab毒素之棉花品種);NewLeaf®(釋出Cry3A毒素之馬鈴薯品種);NatureGard®、Agrisure® GT Advantage(GA21草甘磷耐受性特徵)、Agrisure® CB Advantage(Bt11玉米螟蟲(CB)特徵)和Protecta®。 Gene-transgenic plants that have one or more genes that encode insecticidal resistance and release one or more toxins are not only known, but some of them are commercially available. Examples of such plants are: YieldGard® (a corn variety that releases Cry1Ab toxin); YieldGard Rootworm® (a corn variety that releases Cry3Bb1 toxin); YieldGard Plus® (a corn variety that releases Cry1Ab and Cry3Bb1 toxin); Starlink® ( Released Cry9C toxin maize variety); Herculex I® (released Cry1Fa2 toxin and glufosinate N-acetyltransferase enzyme (PAT) to chlorhexidine herbicide tolerance maize variety); NuCOTN 33B® ( Cotton varieties that release Cry1Ac toxin); Bollgard I® (cotton varieties that release Cry1Ac toxin); Bollgard II® (cotton varieties that release Cry1Ac and Cry2Ab toxins); VipCot® (cotton varieties that release Vip3A and Cry1Ab toxins) NewLeaf® (released Cry3A toxin potato variety); NatureGard®, Agrisure® GT Advantage (G21 glyphosate tolerance), Agrisure® CB Advantage (Bt11 corn borer (CB) characteristics) and Protecta®.
更多這類基因轉殖作物的例子還有: More examples of such genetically modified crops are:
1. Bt11玉米(出自Syngenta Seeds SAS公司,地址:Chemin de l'Hobit 27,F-31 790 St.Sauveur,France;註冊編號:C/FR/96/05/10)。經過基因改造的Zea mays玉米,藉著以基因轉殖的方式釋出截斷的Cry1Ab毒素,已能抵抗歐洲玉米螟蟲(Ostrinia nubilalis和Sesamia nonagrioides)的侵襲。Bt11玉米亦藉著基因轉殖的方式來釋出PAT酵素,以達到對草胺磷除草劑的耐受性。 1. Bt11 corn (from Syngenta Seeds SAS, Chemin de l'Hobit 27, F-31 790 St. Sauveur, France; registration number: C/FR/96/05/10). The genetically engineered Zea mays corn has been able to resist the invasion of the European corn borer ( Serrinia nubilalis and Sesamia nonagrioides ) by releasing the truncated Cry1Ab toxin by gene transfer. Bt11 corn also releases PAT enzyme by gene transfer to achieve tolerance to glufosinate herbicides.
2. Bt176玉米(出自Syngenta Seeds SAS公司,地址:Chemin de l'Hobit 27,F-31 790 St.Sauveur,France;註冊編號:C/FR/96/05/10)。經過基因改造的Zea mays玉米,藉著以基因轉殖的方式釋出Cry1Ab毒素,已能抵抗歐洲玉米螟蟲(Ostrinia nubilalis和Sesamia nonagrioides)的侵襲。Bt176玉米亦藉著基因轉殖的方式來釋出PAT酵素,以達到對草胺磷除草劑的耐受性。 2. Bt176 corn (from Syngenta Seeds SAS, Chemin de l'Hobit 27, F-31 790 St. Sauveur, France; registration number: C/FR/96/05/10). The genetically engineered Zea mays corn has been able to resist the invasion of the European corn borer ( Serrinia nubilalis and Sesamia nonagrioides ) by releasing the Cry1Ab toxin by gene transfer. Bt176 corn also releases PAT enzyme by gene transfer to achieve tolerance to glufosinate herbicides.
3. MIR604玉米(出自Syngenta Seeds SAS公司,地址:Chemin de l'Hobit 27,F-31 790 St.Sauveur,France,註冊編號:C/FR/96/05/10)。此玉米藉著以基因轉殖的方式釋出改造的Cry3A毒素,而已能抵抗昆蟲侵害。這種毒素是經由插入組織蛋白酶-G蛋白酶識別序列來改造的Cry3A055。這種基因轉殖玉米植物的製備資訊,在WO 03/018810中已有說明。 3. MIR604 corn (from Syngenta Seeds SAS, Chemin de l'Hobit 27, F-31 790 St. Sauveur, France, registration number: C/FR/96/05/10). This corn has been able to resist insect damage by releasing the engineered Cry3A toxin by gene transfer. This toxin is a Cry3A055 engineered by insertion of a cathepsin-G protease recognition sequence. Information on the preparation of such genetically transformed maize plants is described in WO 03/018810.
4. MON 863玉米(出自Monsanto Europe S.A.公司,地址:270-272 Avenue de Tervuren,B-1150 Brussels,Belgium,註 冊編號:C/DE/02/9)。MON 863釋出了Cry3Bb1毒素並對某些鞘翅目昆蟲具有耐受性。 4. MON 863 corn (from Monsanto Europe SA, 270-272 Avenue de Tervuren, B-1150 Brussels, Belgium, registration number: C/DE/02/9). MON 863 releases the Cry3Bb1 toxin and is resistant to certain coleopteran insects.
5. IPC 531棉花(出自Monsanto Europe S.A.公司,地址:270-272 Avenue de Tervuren,B-1150 Brussels,Belgium,註冊編號:C/ES/96/02)。 5. IPC 531 cotton (from Monsanto Europe SA, 270-272 Avenue de Tervuren, B-1150 Brussels, Belgium, registration number: C/ES/96/02).
6. 1507玉米(出自Pioneer Overseas Corporation公司,地址:Avenue Tedesco,7 B-1160 Brussels,Belgium,註冊編號:C/NL/00/10)。此基因改造玉米旨在釋出Cry1F蛋白質,以達到對某些鱗翅目昆蟲的耐受性,並旨在表達PAT蛋白質,以達到對草胺磷除草劑的耐受性。 6. 1507 Corn (from Pioneer Overseas Corporation, Address: Avenue Tedesco, 7 B-1160 Brussels, Belgium, registration number: C/NL/00/10). This genetically engineered maize is designed to release the Cry1F protein to achieve tolerance to certain lepidopteran insects and to express PAT proteins to achieve tolerance to glufosinate herbicides.
7. NK603×MON 810玉米(出自Monsanto Europe S.A.公司,地址:270-272 Avenue de Tervuren,B 1150 Brussels,Belgium,註冊編號:C/GB/02/M3/03)。此玉米包括藉由將基因改造的NK603和MON810進行雜交,所習知培育出的雜交玉米品種。NK603×MON 810玉米藉著基因轉殖的方式,釋出了從農桿菌種(Agrobacterium spp.)CP4菌株所獲得的蛋白質CP4 EPSPS,該蛋白質能賦予對Roundup®除草劑(含有草甘磷)的耐受性,並表達了從蘇雲金芽孢桿菌亞種(Bacillus thuringiensis subsp.)kurstaki所獲得的Cry1Ab毒素,其可帶來對某些鱗翅目生物(包括歐洲玉米螟蟲在內)的耐受性。所謂的作物,也可以是那些已藉由基因工程技術而對有害生物具抗性的作物,其中包括Bt玉米(可抗歐洲玉米螟)、Bt棉花(可抗棉鈴象鼻蟲)及Bt馬鈴薯(可抗科羅拉多甲蟲)。Bt玉米的例子有NK牌Bt 176 玉米混種(Syngenta Seeds)。基因轉殖植物的例子有KnockOut®(玉米)、Yield Gard®(玉米)、NuCOTIN33B®(棉花)、Bollgard®(棉花)、NewLeaf®(馬鈴薯)、NatureGard®及Protexcta,這些植物有一個或更多個基因編碼了殺蟲抵抗性,並釋出一種或更多種毒性。 7. NK603 x MON 810 corn (from Monsanto Europe SA, address: 270-272 Avenue de Tervuren, B 1150 Brussels, Belgium, registration number: C/GB/02/M3/03). This maize includes hybrid corn varieties that have been conventionally developed by hybridizing genetically engineered NK603 and MON810. NK603×MON 810 maize released the protein CP4 EPSPS obtained from the Agrobacterium spp. CP4 strain by gene transfer, which confers on Roundup® herbicide (containing glyphosate). Tolerance, and expression of the Cry1Ab toxin obtained from Bacillus thuringiensis subsp . kurstaki , which confers tolerance to certain lepidopteran organisms, including European corn borers. The so-called crops can also be those that have been resistant to pests by genetic engineering techniques, including Bt corn (which is resistant to European corn borer), Bt cotton (resistant to cotton boll weevil) and Bt potato ( Resistant to Colorado beetles). An example of Bt corn is the NK brand Bt 176 Corn Mix (Syngenta Seeds). Examples of genetically modified plants are KnockOut® (corn), Yield Gard® (corn), NuCOTIN 33B® (cotton), Bollgard® (cotton), NewLeaf® (potato), NatureGard® and Protexcta, one or more of these plants. The genes encode insecticidal resistance and release one or more toxicities.
植物性作物或其種子材料能同時抵抗除草劑和昆蟲啃食(疊加型(stacked)基因轉殖事件)。例如,種子能釋出一種可殺蟲的Cry3蛋白質,同時能耐受草甘膦。 Plant crops or their seed materials are resistant to both herbicides and insect foraging (stacked gene transfer events). For example, seeds can release a pesticidal Cry3 protein while being tolerant to glyphosate.
作物也應被理解為那些藉由習知培育方法或基因工程技術而取得的作物,以及那些含有所謂輸出性狀(如更佳的儲存穩定性、更高的營養價值及更好的滋味)的作物。 Crops should also be understood as crops obtained by conventional breeding methods or genetic engineering techniques, as well as crops containing so-called export traits such as better storage stability, higher nutritional value and better taste. .
為了將式(I)化合物作為殺蟲劑、殺蟎劑、殺線蟲或殺軟體動物劑,以施用於有害生物、其所在之處或易受有害生物侵害之植物,通常會將式(I)的化合物配製成納入了以下項目的組成物:式(I)化合物本身,以及合適的惰性稀釋劑或載體,並選擇性納入表面活性劑(SFA)。SFA這種化學品,能夠降低界面張力而藉此引發其他特性(例如分散性、乳化性及濕性)產生變化,以更改某個界面(例如液體/固體、液體/空氣或液體/液體表面)的特性。所有組成物(固體和液體調配物)較佳包含(按重量計)0.0001至95%,更佳1至85%,例如5至60%的式(I)化合物。此組成物一般用於控制有害生物,而式(I)化合物的施用率是從每公頃0.1公克至10公斤,較佳每公頃1公克至6公斤,更佳為每公頃1公克至1公斤。 In order to use a compound of formula (I) as an insecticide, acaricide, nematicidal or molluscicide for application to a pest, where it is or susceptible to pests, formula (I) will generally be used. The compounds are formulated into a composition incorporating the compound of formula (I) itself, together with a suitable inert diluent or carrier, and optionally incorporating a surfactant (SFA). SFA, a chemical that reduces interfacial tension and thereby induces changes in other properties (such as dispersibility, emulsifying, and wet) to alter an interface (such as liquid/solid, liquid/air or liquid/liquid surfaces) Characteristics. All compositions (solid and liquid formulations) preferably comprise (by weight) from 0.0001 to 95%, more preferably from 1 to 85%, for example from 5 to 60%, of the compound of formula (I). The composition is generally used for controlling pests, and the application rate of the compound of the formula (I) is from 0.1 to 10 kg per hectare, preferably from 1 to 6 kg per hectare, more preferably from 1 to 1 kg per hectare.
若用於種子敷料(seed dressing),式(I)化合物的施用率一般每公斤種子是從0.0001公克至10公克(例如0.001公克或0.05公克),較佳0.005公克至10公克,更佳為0.005公克至4公克。 If used in seed dressing, the application rate of the compound of formula (I) is generally from 0.0001 g to 10 g (e.g., 0.001 g or 0.05 g) per kg of seed, preferably from 0.005 g to 10 g, more preferably 0.005. Gram to 4 grams.
本發明另一態樣提供一種包含殺有害生物有效量的式(I)化合物之組成物,尤其是包含殺蟲、殺蟎、殺線蟲或殺軟體動物有效量的式(I)化合物以及其合適的載體或稀釋劑的殺蟲、殺蟎、殺線蟲或殺軟體動物之組成物。此組成物較佳為殺蟲、殺蟎、殺線蟲或殺軟體動物組成物。 Another aspect of the invention provides a composition comprising a pesticidally effective amount of a compound of formula (I), especially an insectic, acaricidal, nematicidally or molluscicidal effective amount of a compound of formula (I) and suitable A carrier or diluent for the composition of insecticidal, acaricidal, nematicidal or molluscicidal animals. Preferably, the composition is a pesticidal, acaricidal, nematicidal or molluscicidal composition.
此組成物可從一些調配物類型中選擇,其中包括粉劑(DP)、可溶性粉劑(SP)、水溶性粒劑(SG)、水分散粒劑(WG)、可溼性粉劑(WP)、粒劑(GR)(緩慢或快速釋放)、可溶性濃縮物(SL)、油溶性液劑(OL)、超低容量液劑(UL)、乳化濃縮物(EC)、可分散濃縮物(DC)、乳劑(水包油(EW)和油包水(EO))、微乳劑(ME)、懸浮液濃縮物(SC)、氣溶膠、霧化/煙霧調配物、膠囊懸浮液(CS)和種子處理調配物。在任何實例中選擇的調配物類型將視特定的設想目的而定,以及式(I)化合物之物理、化學與生物特性而定。 The composition can be selected from a number of formulation types including powder (DP), soluble powder (SP), water soluble granules (SG), water dispersible granules (WG), wettable powders (WP), granules. Agent (GR) (slow or rapid release), soluble concentrate (SL), oil soluble liquid (OL), ultra low volume liquid (UL), emulsified concentrate (EC), dispersible concentrate (DC), Emulsions (oil-in-water (EW) and water-in-oil (EO)), microemulsions (ME), suspension concentrates (SC), aerosols, atomization/smoke formulations, capsule suspensions (CS) and seed treatment Formulation. The type of formulation selected in any of the examples will depend on the particular intended purpose, as well as the physical, chemical, and biological properties of the compound of formula (I).
可藉由以下方式備製粉劑(DP):將式(I)化合物與一種或多種固體稀釋劑(例如天然黏土、高嶺土、葉蠟石、膨潤土、礬土、蒙脫土,矽藻土、白堊、矽藻土、磷酸鈣、碳酸鈣、碳酸鎂、硫、石灰,麵粉,滑石和其他有機與無機固體載體)混合,並機械式地將此混合物磨成細粉。 A powder (DP) can be prepared by reacting a compound of formula (I) with one or more solid diluents (eg, natural clay, kaolin, pyrophyllite, bentonite, alumina, montmorillonite, diatomaceous earth, chalk). Mixing diatomaceous earth, calcium phosphate, calcium carbonate, magnesium carbonate, sulfur, lime, flour, talc and other organic and inorganic solid carriers, and mechanically grinding the mixture into a fine powder.
可藉由將式(I)化合物與一個或多個可溶於水的無機鹽 (例如碳酸氫鈉、碳酸鈉或硫酸鎂)混合,或和一個或多個水溶性有機固體(例如多醣)混合,以及選擇性地與一個或多個潤濕劑混合、與一個或多個分散劑混合,或與潤濕劑和分散劑的混合物來混合以改善水分散性/溶解性,來製備可溶性粉劑(SP)。接著再將此混合物磨成細粉。亦可將類似的組成物製成粒狀以形成水溶性粒劑(SG)。 By reacting a compound of formula (I) with one or more water-soluble inorganic salts (for example, sodium bicarbonate, sodium carbonate or magnesium sulfate), or mixed with one or more water-soluble organic solids (such as polysaccharides), and optionally mixed with one or more wetting agents, dispersed with one or more The soluble powder (SP) is prepared by mixing or mixing with a mixture of a wetting agent and a dispersing agent to improve water dispersibility/solubility. This mixture is then ground to a fine powder. Similar compositions can also be granulated to form water soluble granules (SG).
可藉由將式(I)化合物與一種或多種固體稀釋劑或載體、一種或多種濕潤劑(以及較佳一種或多種分散劑)混合,並選擇性加入一種或多種懸浮液以促進於液體中的分散性,來備製可溼性粉劑(WP)。接著再將此混合物磨成細粉。亦可將類似的組成物製成粒狀以形成水分散粒劑(WG)。 By promoting the compound of formula (I) with one or more solid diluents or carriers, one or more wetting agents (and preferably one or more dispersing agents), and optionally one or more suspensions to facilitate in the liquid Dispersion to prepare wettable powder (WP). This mixture is then ground to a fine powder. Similar compositions can also be granulated to form a water dispersible granule (WG).
可利用兩種方式來形成粒劑(GR):將式(I)化合物與一種或多種粉狀固體稀釋劑或載體,或來自預製之空白顆粒的混合物製成粒狀(藉著在多孔顆粒材料(例如浮石、厄帖浦土、漂白土、矽藻土或碎玉米棒)中吸收式(I)化合物(或其溶劑,在適合的試劑中吸收),來製成粒狀);或是在硬核材料(例如沙、矽酸鹽、礦物碳酸鹽、硫酸鹽或磷酸鹽)上吸收式(I)化合物(或其溶劑,在適合的試劑中吸收),並在必要時加以乾燥。通常用於輔助吸收或吸收的試劑,包括溶劑(例如脂族和芳香族石油溶劑、醇、醚、酮和酯)和黏著劑(例如聚醋酸乙烯酯、聚乙烯醇、糊精、糖和植物油)。粒劑中亦可包含一種或多種其他的添加劑(例如乳化劑、濕潤劑或分散劑)。 Granulation (GR) can be formed in two ways: by granulating a mixture of a compound of formula (I) with one or more powdered solid diluents or carriers, or from preformed blank particles (by means of porous particulate material) Absorbing a compound of formula (I) (or a solvent thereof, which is absorbed in a suitable reagent) to form a granule (for example, in pumice, erbium, smectite, diatomaceous earth or ground corn cob); The compound of formula (I) (or its solvent, absorbed in a suitable reagent) is absorbed on a hard core material such as sand, citrate, mineral carbonate, sulfate or phosphate and dried if necessary. Reagents commonly used to aid absorption or absorption, including solvents (eg, aliphatic and aromatic petroleum solvents, alcohols, ethers, ketones, and esters) and adhesives (eg, polyvinyl acetate, polyvinyl alcohol, dextrin, sugar, and vegetable oils) ). One or more other additives (such as emulsifiers, wetting agents or dispersing agents) may also be included in the granules.
可利用將式(I)化合物溶於水或有機溶劑(例如酮、醇或 乙二醇醚)的方式,來製備可分散濃縮物(DC)。這些溶液可包含表面活性劑(例如藉以改善水稀釋性或防止在噴霧罐中結晶)。 The compound of formula (I) can be dissolved in water or an organic solvent (such as a ketone, an alcohol or A glycol ether) is used to prepare a dispersible concentrate (DC). These solutions may contain surfactants (for example to improve water dilution or to prevent crystallization in a spray can).
可藉由將式(I)化合物溶於有機溶劑(可選擇性包含一種或多種濕潤劑、一種或多種乳化劑或前述製劑的混合物),來製備乳化濃縮物(EC)或水包油型乳液(EW)。適合用於EC的有機溶劑包括芳香烴(例如烷基苯或烷基萘,例示於SOLVESSO 100、SOLVESSO 150和SOLVESSO 200;SOLVESSO是註冊商標)、酮類(例如環己酮或甲基環己酮)和醇類(如苯甲醇、糠醇或丁醇)、N-烷基吡咯啶酮(如N-甲基吡咯啶酮或N-辛基吡咯啶酮)、脂肪酸的二甲基醯胺(如C8-C10脂肪酸二甲基醯胺)和氯烴。EC產品於加水後,自然便可乳化而產生具有足夠穩定性之乳劑,因而能藉由適當的設備噴灑。EW的製備包括取得液體形式的式(I)化合物(如果它在環境溫度下並非液體,則它可能會在一個合理的溫度下融化,一般是低於70℃),或是溶液形式的式(I)化合物(藉由將之溶解在適當的溶劑當中),然後在高剪切力下,將產生的液體或溶液在含有一個或多個SFAs的水中乳化,以製造乳劑。適用於EWs的溶劑包括植物油、氯烴(如氯苯)、芳香族溶劑(如烷基苯或烷基萘)及其他適當且水溶性低之有機溶劑。 An emulsified concentrate (EC) or an oil-in-water emulsion can be prepared by dissolving a compound of formula (I) in an organic solvent, optionally comprising one or more wetting agents, one or more emulsifiers or a mixture of the foregoing. (EW). Organic solvents suitable for use in EC include aromatic hydrocarbons (e.g., alkylbenzenes or alkylnaphthalenes, exemplified in SOLVESSO 100, SOLVESSO 150, and SOLVESSO 200; SOLVESSO is a registered trademark), ketones (e.g., cyclohexanone or methylcyclohexanone). And alcohols (such as benzyl alcohol, decyl or butanol), N -alkylpyrrolidone (such as N -methylpyrrolidone or N -octylpyrrolidone), fatty acid dimethyl decylamine (such as C 8 -C 10 fatty acid dimethyl decylamine) and chlorocarbons. Once the EC product is added with water, it is naturally emulsified to produce an emulsion with sufficient stability and can be sprayed by suitable equipment. Preparation of EW involves obtaining a compound of formula (I) in liquid form (if it is not liquid at ambient temperature, it may melt at a reasonable temperature, typically below 70 ° C), or in the form of a solution ( I) The compound (by dissolving it in a suitable solvent) and then emulsifying the resulting liquid or solution in water containing one or more SFAs under high shear to produce an emulsion. Suitable solvents for EWs include vegetable oils, chlorocarbons (such as chlorobenzene), aromatic solvents (such as alkylbenzenes or alkylnaphthalenes), and other suitable and water-soluble organic solvents.
可利用將水與一種或多種含一種或多種SFA的摻合物混合的方式,自然產生一種具熱力穩定性的等向液體調配物,藉以製備微乳劑(ME)。式(I)化合物最初的形態為水或 溶劑/SFA摻合物。適用於MEs的溶劑包括以上描述用於ECs或EWs之溶劑。ME可為水包油或油包水系統(可由傳導性測量來判定存在何種系統),也可適合用來在相同的調配物中混合水溶性與油溶性殺有害生物劑。ME適合在水中稀釋,包括繼續保持微乳劑的形式或形成習知的水包油乳劑。 Microemulsions (ME) can be prepared by naturally producing a thermally stable, isotropic liquid formulation by mixing water with one or more blends containing one or more SFAs. The initial form of the compound of formula (I) is water or Solvent/SFA blend. Solvents suitable for use in MEs include the solvents described above for ECs or EWs. The ME can be an oil-in-water or water-in-oil system (which can be determined by conductivity measurements to determine which system is present), and can also be adapted to mix water-soluble and oil-soluble pesticides in the same formulation. ME is suitable for dilution in water, including continuing to maintain the form of a microemulsion or forming a conventional oil-in-water emulsion.
懸浮液濃縮物(SC)可包含式(I)化合物微細不溶固體顆粒的水性或非水性懸浮液。可在適當的介質中,利用球磨或珠磨方式來研磨式(I)化合物(可選擇性使用一種或多種分散劑)以製備SC,藉以製成細粒狀的化合物懸浮液。組成物中可含一種或多種的濕潤劑,並可加入一種懸浮液以降低顆粒沉澱的速率。或者,可對式(I)化合物進行乾磨並加入含有前述試劑的水中,製成所欲的最終產品。 The suspension concentrate (SC) may comprise an aqueous or non-aqueous suspension of finely insoluble solid particles of the compound of formula (I). The compound of formula (I) (optionally using one or more dispersing agents) can be milled in a suitable medium by ball milling or bead milling to prepare SC, whereby a suspension of the finely divided compound can be prepared. The composition may contain one or more wetting agents and a suspension may be added to reduce the rate of particle precipitation. Alternatively, the compound of formula (I) can be dry milled and added to water containing the aforementioned reagents to form the desired end product.
氣溶膠調配物包含式(I)化合物及合適的推進劑(例如正丁烷)。也可在一個合適的介質(例如水或是正丙醇等水溶性液體)中溶解或分散式(I)的化合物,以提供使用於非加壓之手致動式噴淋泵的組成物。 Aerosol formulations comprise a compound of formula (I) and a suitable propellant (e.g., n-butane). The compound of formula (I) may also be dissolved or dispersed in a suitable medium (e.g., water or a water soluble liquid such as n-propanol) to provide a composition for use in a non-pressurized hand-actuated spray pump.
式(I)化合物可在乾燥狀態下與煙火混合物混合,以形成一種適合在密閉空間中產生含此化合物的煙霧之組成物。 The compound of formula (I) can be mixed with the pyrotechnic mixture in a dry state to form a composition suitable for producing a fumes containing the compound in a confined space.
能以類似製備EW調配物的方式來製備膠囊懸浮液(CS),但是附加一個額外的聚合階段,藉此獲得油滴的水分散,其中,每個油滴是用聚合外殼來封裝,並含有式(I)的化合物,及選擇性地包含一個載體或稀釋劑。聚合外殼可 利用界面聚縮合反應或凝聚程序來製成。組成物可提供式(I)化合物的控釋(controlled release)效果,並可用於種子處理。式(I)化合物亦能配製於可生物降解的聚合物基體,以提供化合物緩慢,受控制的釋放。 The capsule suspension (CS) can be prepared in a similar manner to the preparation of the EW formulation, but with the addition of an additional polymerization stage whereby water dispersion of the oil droplets is obtained, wherein each oil droplet is encapsulated with a polymeric outer shell and contains a compound of formula (I), and optionally a carrier or diluent. Polymeric shell It is made by an interfacial polycondensation reaction or a coagulation procedure. The composition provides a controlled release effect of the compound of formula (I) and can be used for seed treatment. The compound of formula (I) can also be formulated in a biodegradable polymer matrix to provide a slow, controlled release of the compound.
組成物中可包含一種或多種添加劑,以增進組成物的生物表現性(例如藉由改善濕性、保留性或表面分布性;處理之表面的抗雨性;或式(I)化合物的攝取性和移動性來增進)。此類添加劑包括表面活性劑、基於某些礦物油或天然植物油(如大豆及油菜籽油)等油類的噴霧添加劑,以及其與其他生物性強化佐劑(可幫助或更改式(I)化合物作用之成分)的摻合物。 One or more additives may be included in the composition to enhance the bio-exhibition of the composition (e.g., by improving wettability, retention or surface distribution; the rain resistance of the treated surface; or the uptake of the compound of formula (I) And mobility to improve). Such additives include surfactants, spray additives based on certain mineral oils or natural vegetable oils (such as soybean and rapeseed oil), and other bio-enhancing adjuvants that can help or modify compounds of formula (I). Blend of the component of action.
式(I)化合物亦可配製為種子處理的調配物,例如粉末組成物,包括用於乾式種子處理(DS)的粉末、水溶性粉劑(SS)或用於泥水處理的水分散性粉劑(WS),或是液體組成物,包括懸浮濃縮物(FS)、溶劑(LS)或膠囊懸浮液(CS)。DS、SS、WS、FS及LS組成物的製備方法,分別與上述DP、SP、WP、SC和DC組成物的製備方法非常類似。用於處理種子的組成物,可包括用於幫助組成物附著於種子的試劑(例如礦物油或成膜阻隔物)。 The compounds of formula (I) may also be formulated as seed treatment formulations, such as powder compositions, including powders for dry seed treatment (DS), water soluble powders (SS) or water dispersible powders for mud water treatment (WS). ), or a liquid composition, including a suspension concentrate (FS), a solvent (LS) or a capsule suspension (CS). The preparation methods of the DS, SS, WS, FS and LS compositions are very similar to the preparation methods of the above DP, SP, WP, SC and DC compositions, respectively. The composition for treating the seed may include an agent (e.g., mineral oil or film-forming barrier) for assisting in the attachment of the composition to the seed.
濕潤劑、分散劑及乳化劑可為陽離子、陰離子、兩性或非離子類型的表面SFA。 The humectant, dispersant and emulsifier can be cationic, anionic, amphoteric or nonionic surface SFA.
陽離子類型之適合的SFAs,包括四級銨化合物(例如溴化十六烷基三甲基銨)、咪唑啉類及胺鹽類。 Suitable SFAs of the cationic type include quaternary ammonium compounds such as cetyltrimethylammonium bromide, imidazolines and amine salts.
適合的陰離子SFAs包括脂肪酸的鹼金屬鹽、硫酸之脂 族單酯的鹽(例如十二烷基硫酸鈉)、磺化芳香族化合物的鹽(例如十二烷基苯磺酸鈉、十二烷基苯磺酸鈣、萘磺酸丁脂,以及二異丙基萘磺酸鈉及三異丙基萘磺酸鈉之混合物)、醚硫酸鹽、醇醚硫酸鹽(例如月桂基聚醚-3硫酸鈉)、醚羧酸鹽(例如月桂基聚醚-3羧酸鈉)、磷酸鹽酯(一個或多個脂肪醇與磷酸(主要為單酯)或五氧化二磷(主要是二酯)反應下之產物,例如月桂醇與四磷酸反應;此外,這些產物可乙氧基化)、磺化琥珀醯胺酸鹽、石蠟或烯屬磺酸酯、胺基乙磺酸鹽和木素磺化鹽。 Suitable anionic SFAs include alkali metal salts of fatty acids, lipids of sulfuric acid a salt of a monoester (for example, sodium lauryl sulfate), a salt of a sulfonated aromatic compound (for example, sodium dodecylbenzenesulfonate, calcium dodecylbenzenesulfonate, butylene naphthalenesulfonate, and two a mixture of sodium isopropyl naphthalene sulfonate and sodium triisopropyl naphthalene sulfonate), an ether sulfate, an alcohol ether sulfate (for example, sodium laureth-3 sulfate), an ether carboxylate (for example, a lauryl polyether) -3 sodium carboxylate), a phosphate ester (product of the reaction of one or more fatty alcohols with phosphoric acid (mainly monoester) or phosphorus pentoxide (mainly diester), such as lauryl alcohol and tetraphosphoric acid; These products may be ethoxylated), sulfonated amber phthalates, paraffin or olefin sulfonates, aminoethanesulfonates and lignosulfonates.
兩性類型之適合的SFA包括甜菜鹼、丙酸鹽及甘胺酸鹽。 Suitable SFAs of the amphoteric type include betaines, propionates and glycinates.
非離子類型之合適的SFA包括環氧烷烴的縮合產物,如環氧乙烷、環氧丙烷、環氧丁烷,或其與脂肪醇(如油醇或十六醇)或烷基酚(如辛基苯酚、壬基苯酚或辛基甲酚)的混合物;由長鏈脂肪酸或己糖醇酐取得的偏酯;上述偏酯與環氧乙烷的縮合產物;嵌段聚合物(包括環氧乙烷和環氧丙烷);烷醇醯胺;單酯(例如脂肪酸聚乙二醇酯);氧化胺(例如十二烷基二甲基氧化胺);和卵磷脂。 Suitable SFAs of the nonionic type include condensation products of alkylene oxides such as ethylene oxide, propylene oxide, butylene oxide, or their association with fatty alcohols such as oleyl alcohol or cetyl alcohol or alkylphenols (eg a mixture of octylphenol, nonylphenol or octylcresol; a partial ester obtained from a long chain fatty acid or hexitol anhydride; a condensation product of the above partial ester with ethylene oxide; a block polymer (including an epoxy) Ethane and propylene oxide; alkanolamine; monoester (e.g., fatty acid polyethylene glycol ester); amine oxide (e.g., dodecyldimethylamine oxide); and lecithin.
適合的懸浮劑包括親水膠體(如多醣體、聚乙烯吡咯啶酮或羧甲基纖維素鈉)及膨脹性黏土(如膨潤土或厄帖浦土(attapulgite))。 Suitable suspending agents include hydrophilic colloids (such as polysaccharides, polyvinylpyrrolidone or sodium carboxymethylcellulose) and swelling clays (such as bentonite or attapulgite).
可使用任何已知的殺有害生物化合物施用方法,來施用式(I)化合物。舉例來說,不論它是否製成調配物,都可直接應用在有害生物或有害生物的所在之處(例如有害生物 的棲息地、或是容易受到有害生物侵襲之成長中的植物)或是應用在植物的任何部分,包括葉子、莖、枝條或根,或在種植種子之前應用於種子上,或應用在當中具有成長中的植物、或準備在其內種植植物的其他媒介(例如根部週遭的土壤、一般土壤、稻田水或水耕栽培系統),或是可在土壤或水性環境中,將它噴上、撒上、以浸泡方式來應用、當作乳膏或藥膏調配物來應用、以蒸汽方式應用,或是藉由分配或加入組成物的方式來應用(例如顆粒組成物或包在水溶性袋中的組成物)。 The compound of formula (I) can be administered using any known method of administering a pesticidal compound. For example, whether it is formulated or not, it can be applied directly to where pests or pests are located (eg pests) a habitat, or a growing plant that is susceptible to pests) or applied to any part of the plant, including leaves, stems, shoots or roots, or applied to the seed prior to planting the seed, or Growing plants, or other mediums in which plants are to be planted (such as soil around the roots, soil, rice fields, or hydroponic systems), or spray or sprinkle them in soil or in an aqueous environment. Applied in a soaking manner, applied as a cream or ointment formulation, applied as a vapor, or applied by dispensing or adding a composition (eg, a particulate composition or encapsulated in a water soluble pouch) Composition)).
式(I)化合物亦可注入植物內,或使用電動噴霧技術或其他少量性方法噴於植物上,或使用土地或空中灌溉系統來施用。 The compounds of formula (I) may also be injected into plants or sprayed onto plants using electrodynamic spraying techniques or other minor methods, or applied using land or aerial irrigation systems.
當作水性製劑(如水溶液或分散液)來使用的組成物,通常是以含有高比例活性成分的濃縮物(濃縮物在使用前先加入水中)形式來供應。這些可含DCs、SCs、ECs、EWs、MEs、SGs、SPs、WPs、WGs及CSs的濃縮物,通常要能承受長時間的儲藏,並在這樣長時間儲藏後仍能加入水以形成水性製劑,而且這些調劑能在一段充分的時間內保持同質,以便供習知噴霧設備來施用。視其用途而定,此類的水性製劑可含有不同含量的式(I)化合物(例如從0.0001至10%(按重量計))。 Compositions for use as aqueous preparations (e.g., aqueous solutions or dispersions) are typically supplied as a concentrate containing a high proportion of active ingredient (the concentrate is added to the water prior to use). These concentrates, which can contain DCs, SCs, ECs, EWs, MEs, SGs, SPs, WPs, WGs, and CSs, are typically capable of withstanding long-term storage and can be added to form aqueous formulations after such long-term storage. And these agents can remain homogenous for a sufficient period of time for application by conventional spray equipment. Depending on the use, such aqueous preparations may contain varying amounts of the compound of formula (I) (for example from 0.0001 to 10% by weight).
式(I)的化合物可與肥料(例如含氮、鉀或磷的肥料)一起用於混合物裡。合適的調配物類型包括肥料顆粒。式(I)化合物在混合物中的含量,較佳高達此化合物重量的25%。 The compound of formula (I) can be used in a mixture with a fertilizer such as a fertilizer containing nitrogen, potassium or phosphorus. Suitable formulation types include fertilizer granules. The content of the compound of the formula (I) in the mixture is preferably up to 25% by weight of the compound.
因此,本發明還提供了包含肥料和式(I)化合物的肥料組成物。本發明之組成物可包含其他具有生物活性的化合物,例如微量營養素或具以下活性的化合物:殺真菌活性,或植物生長調節、除草、殺蟲、殺線蟲或殺蟎活性。 Accordingly, the present invention also provides a fertilizer composition comprising a fertilizer and a compound of formula (I). The compositions of the present invention may comprise other biologically active compounds, such as micronutrients or compounds having the following activity: fungicidal activity, or plant growth regulating, herbicidal, insecticidal, nematicidal or acaricidal activity.
式I的化合物(以下以「TX」一詞簡稱之,意指由式I的化合物所圍繞的化合物,或更佳的是,「TX」一詞指的是選自表1到12、A、B與C的化合物)可以是組成物的唯一活性成分,或是它可以在適當的情況下,與一個或多個額外的活性成分混合,如殺有害生物劑(昆蟲、蟎、軟體動物和線蟲殺蟲劑)、殺真菌劑、增效劑、除草劑、安全劑或植物生長調節劑等等。根據本發明,組成物的活性可因此大大擴大,並有令人驚訝的優點(這也可以廣義地稱為增效活性)。額外的活性成分可以:提供效力譜更廣泛、或在有害生物所在之處更具持久效力的組成物;藉由減少植物藥害的方式,提供更具植物/作物耐受性的組成物;提供能在昆蟲不同發展階段中控制昆蟲的組成物;增效或補充TX的活性(例如藉由增加效果的速度或藉由克服抵抗性的方式);或是協助克服或預防對個別的成分發展出抗性。特定之額外活性成分將視預期的組成物效用而定。合適殺有害生物劑的例子包括以下各項:a)菊酯類農藥,例如氯菊酯、氯氰菊酯、氰戊菊酯、S-氰戊菊酯、溴氰菊酯、氯氟氰菊酯(特別是三氟氯氰菊酯)、聯苯菊酯、甲氰菊酯、氟氯氰菊酯、七氟菊酯、魚安全菊酯類農藥(例如醚菊酯)、天然除蟲菊酯、胺菊酯、s-生 物烯丙菊酯、芬氟司林、炔丙菊脂或5-苯甲基-3-呋喃甲基-(E)-(1R,3S)-2、2-二甲基-3-(2-側氧基噻-3-亞基甲基)環丙烷羧酸酯;b)有機磷酸酯,例如佈飛松、硫丙磷、歐殺松、甲基-巴拉松、甲基谷速松、滅賜松-s-甲基、飛達松、甲基二硫松、芬滅松、亞速靈、佈飛松、三落松、達馬松、大滅松、福賜米松、馬拉松、陶斯松、裕必松、托福松、繁福松、大福松、福瑞松、巴賽松、亞特松-甲基、乙基嘧啶磷、撲滅松、福賽絕或大利松;c)胺基甲酸酯類(包括芳基胺基甲酸酯),例如抗蚜威、唑蚜威、除線威、克百威、呋線威、殺蟲丹、得滅克、硫雜呋喃酮、丁硫克百威、蟲威、仲丁威、殘殺威、滅多威或殺線威;d)苯甲醯脲,例如除蟲脲、殺鈴脲、氟鈴脲、氟蟲脲或定蟲脲;e)有機錫化合物,例如三環錫、苯丁錫或三唑錫;f)吡唑,例如吡蟎胺和唑蟎酯;g)大環內酯類,諸如阿凡曼菌素或米爾比霉素等等,例如阿巴汀、因滅汀苯甲酸鹽、伊維菌素、米爾比霉素,或多殺菌素、賜諾特或印楝素;h)激素或費洛蒙;i)有機氯化合物,諸如硫丹、六氯化苯、DDT、氯丹或狄氏劑;j)脒類,例如殺蟲脒或雙甲脒; k)燻蒸劑,例如三氯硝基甲烷、二氯丙烷、溴甲烷或威百畝;l)新菸鹼類化合物,例如益達胺、噻蟲啉、啶蟲脒、噻蟲胺、烯啶蟲胺、呋蟲胺或噻蟲;m)二芳甲醯基肼類,例如得芬諾、環蟲醯肼或甲氧蟲醯肼;n)二苯基醚類,例如苯蟲醚或吡丙醚;o)茚蟲威;p)溴蟲腈;q)吡蚜酮或pyrifluquinazon;r)螺蟲乙酯、螺蟎酯或螺甲蟎酯;s)氟蟲醯胺、氯蟲醯胺或氰蟲醯胺;t)cyenopyrafen或丁氟蟎酯;或u)氟啶蟲胺腈。 A compound of formula I (hereinafter abbreviated by the term "TX", meaning a compound surrounded by a compound of formula I, or more preferably, the term "TX" is selected from Tables 1 to 12, A, The compound of B and C) may be the sole active ingredient of the composition, or it may be mixed with one or more additional active ingredients, such as pesticides (insects, mites, mollusks and nematodes, where appropriate). Insecticides), fungicides, synergists, herbicides, safeners or plant growth regulators, and the like. According to the invention, the activity of the composition can thus be greatly expanded and has surprising advantages (this can also be referred to broadly as synergistic activity). Additional active ingredients may: provide a composition with a broader spectrum of efficacy, or a more durable effect where the pest is, and provide a more plant/crop tolerant composition by reducing the phytotoxicity of the plant; Controls the composition of insects at different stages of development of insects; synergistically or complements the activity of TX (eg by increasing the rate of effect or by overcoming resistance); or assisting in overcoming or preventing the development of individual components Resistance. The particular additional active ingredient will depend on the intended utility of the composition. Examples of suitable pesticidal agents include the following: a) pyrethroid pesticides such as permethrin, cypermethrin, fenvalerate, S-fenvalerate, deltamethrin, cyhalothrin (especially Is cyhalothrin, bifenthrin, fenpropathrin, cyfluthrin, tefluthrin, fish safe pyrethroid pesticides (such as efenthrin), natural pyrethrins, methrin, s-bio Allylmethrin, fenfluralin, propargyl or 5-benzyl-3-furanmethyl-( E )-(1R,3S)-2,2-dimethyl-3-(2- Side oxythiophene -3-ylidenemethyl)cyclopropanecarboxylate; b) organophosphates such as bufson, thiopropylphosphonium, acesulfame, methyl-barlaxon, methyl tamarind, and chlorhexidine-s -Methyl, Fedasone, Methyl Disulfoxide, Penfensone, Azovin, Bufson, Sanluosong, Damasson, Dasongsong, Fusemisone, Marathon, Taosson, Yubisong, TOEFL Pine, Fanfusong, Dafusong, Furyson, Bassson, Yateson-methyl, ethylpyrimidine, chlorpheniramine, forsythia or russula; c) urethanes (including arylamines) Formate), for example, anti-carbocarb, zodicon, de-line, carbofuran, furosemide, insecticidal, dexamethasone, thiafuranone, butyl thiocarbamate, Insecticide, Zhongdingwei, propoxur, methomyl or chlorpyrifos; d) benzalazine, such as diflubenzuron, triflumuron, hexaflumuron, flubenzuron or chlorfenapyr; e) organotin compounds , for example, tricyclotin, phenbutyltin or triazole tin; f) pyrazoles, such as pyridoxamine and oxazolidine; g) macrolides, such as avermectin or mirabimycin, etc. For example, abatatin, indomethacin, ivermectin, milbemycin, or spinosyn, sinote or azadirachtin; h) hormone or pheromone; i) organochlorine compounds, Such as endosulfan, hexachlorobenzene, DDT, chlordane or dieldrin; j) terpenoids such as insecticidal or amitraz; k) fumigants such as trichloronitromethane, dichloropropane, methyl bromide or Weibaimu; l) neonicotinoids, such as edetamine, thiacloprid, acetamiprid, clothianidin, nitenpyram, dinotefuran or worm m) diarylmethionyl hydrazines, such as fenfenolone, cyclosporin or methoxypterin; n) diphenyl ethers, such as behenil or pyriproxy; o) indoxacarb; p) chlorfenapyr; q) pymetrozine or pyrifluquinazon; r) spirotetramat, spironolactone or spiromethyl ester; s) flufenamide, chlorhexidine or cyanamide; t) cyenopyrafen Or butaflurane; or u) flonicamidonitrile.
除了上面列出的主要化學級殺有害生物劑之外,如果適合意欲的組成物效用,尚可將具有特定目標的其他殺有害生物劑運用在組成物中。舉例來說,可運用適用於特定作物的選擇性殺蟲劑,例如適用於稻米的螟蟲專用殺蟲劑(例如培丹)或跳蟲專用殺蟲劑(例如撲虱靈)。或者,也可將專用於特定昆蟲種類/階段的殺蟲劑或殺蟎劑納入組成物中(例如殺蟎卵殺幼蟲劑,諸如四蟎、氟苯亞胺噻唑、噻蟎酮或四氯殺蟎碸等等;殺蟎劑,諸如三氯殺蟎醇或克蟎特等等;殺蟎劑,諸如:溴蟎酯或乙酯殺蟎醇等等;或生長調節劑,諸如氟蟻腙、殺蠅胺、烯蟲酯、定蟲脲或除蟲脲)。 In addition to the primary chemical grade pesticides listed above, other pesticidal agents with specific objectives can be utilized in the composition if they are suitable for the intended composition. For example, selective insecticides suitable for a particular crop can be utilized, such as a locust-specific insecticide (such as Pedan) or a hopper-specific insecticide (such as chlorpyrifos) suitable for rice. Alternatively, insecticides or acaricides specific to a particular insect species/stage may also be incorporated into the composition (eg, mites and larvae, such as four mites). , fluorobenzimidazole, thiazolone or tetrachlorocrine, etc.; acaricides such as dicofol or ketone, etc.; acaricides such as bromo oxime ester or ethyl ester sterol; Growth regulators, such as fluoroantimony, chlorfenapyr, methacrylate, chlorfenapyr or diflubenzuron.
式I化合物與活性成分之下列混合物是較佳的,其中,較佳的是,「TX」一詞係指式I化合物所涵蓋的化合物,或較佳的是,「TX」一詞係指選自表1到12、A、B與C的化合物:一種佐劑,其係選自由石油(別名)(628)+TX所組成之物質群組,一種殺蟎劑,是從由下列所組成的物質群中選出:1,1-二-(4-氯苯基)-2-乙氧基乙醇(國際純化學暨應用化學聯合會(IUPAC)名稱)(910)+TX、2,4-二氯苯基苯磺酸(IUPAC/化學摘要名稱)(1059)+TX、2-氟-N-甲基-N-1-萘乙醯胺(IUPAC名稱)(1295)+TX、4-氯苯基苯基碸(IUPAC名稱)(981)+TX、阿巴汀(1)+TX、亞醌蟎(3)+TX、乙醯蟲腈[CCN]+TX、氟酯菊酯(9)+TX、得滅克(16)+TX、氧得滅克(863)、α-氯氰菊酯(202)+TX、賽果(870)+TX、磺胺蟎酯[CCN]+TX、醯胺硫酯(872)+TX、胺吸磷(875)+TX、酸式草酸胺吸磷(875)+TX、雙甲脒(24)+TX、殺蟎特(881)+TX、三氧化二砷(882)+TX、AVI 382(化合物碼)+TX、AZ 60541(化合物碼)+TX、乙基谷速松(44)+TX、甲基谷速松(45)+TX、偶氮苯(IUPAC名稱)(888)+TX、三唑錫(46)+TX、偶氮磷(889)+TX、苯菌靈(62)+TX、苯磷(別名)[CCN]+TX、苯蟎特(71)+TX、苯甲酸芐酯(IUPAC名稱)[CCN]+TX、必芬蟎(74)+TX、聯苯菊酯(76)+TX、樂殺蟎(907)+TX、溴滅菊 酯(別名)+TX、溴殺烯(918)+TX、溴磷松(920)+TX、乙基溴磷松(921)+TX、溴蟎酯(94)+TX、撲虱靈(99)+TX、丁酮威(103)TX、丁酮碸威(104)+TX、丁基達蟎靈(別名)+TX、石硫合劑(IUPAC名稱)(111)+TX、毒殺芬(941)+TX、氯滅殺威(943)+TX、西維因(115)+TX、克百威(118)+TX、三硫磷(947)+TX、CGA 50’439(開發碼)(125)+TX、滅蟎猛(126)+TX、氯殺蟎(959)+TX、殺蟲脒(964)+TX、殺蟲脒鹽酸鹽(964)+TX、溴蟲腈(130)+TX、殺蟎醇(968)+TX、殺蟎酯(970)+TX、敵蟎丹(971)+TX、克芬松(131)+TX、乙酯殺蟎醇(975)+TX、滅蟎醚(977)+TX、螟蛉畏(978)+TX、丙酯殺蟎醇(983)+TX、陶斯松(145)+TX、甲基陶斯松(146)+TX、氯甲硫磷(994)+TX、瓜菊酯I(696)+TX、瓜菊酯II(696)+TX、瓜菊酯類(696)+TX、四蟎(158)+TX、氯氰碘柳胺(別名)[CCN]+TX、蠅毒磷(174)+TX、克羅米通(別名)[CCN]+TX、丁烯磷(1010)+TX、硫雜靈殺菌劑(1013)+TX、果蟲磷(1020)+TX、丁氟蟎酯(CAS註冊編號:編號:400882-07-7)+TX、氯氟氰菊酯(196)+TX、三環錫(199)+TX、氯氰菊酯(201)TX、DCPM(1032)+TX、DDT(219)+TX、田樂磷(1037)+TX、田樂磷-O(1037)+TX、田樂磷-S(1037)+TX、滅賜松(1038)+TX、甲基滅賜松(224)+TX、滅賜松-O(1038)+TX、甲基異滅賜松(224)+TX、滅賜松-S(1038)+TX、滅賜松-S-甲基(224)+TX、碸吸磷(1039)+TX、丁醚脲(226)+TX、得 拉松(1042)+TX、大利松(227)+TX、抑菌靈(230)+TX、二氯松(236)+TX、二克膦(別名)+TX、三氯殺蟎醇(242)+TX、百治磷(243)+TX、得氯蟎(1071)+TX、甲氟磷(1081)、大滅松(262)+TX、二活菌素(別名)(653)+TX、消蟎酚(1089)+TX、代奈-代克新(1089)+TX、敵蟎通(269)+TX、敵蟎普(270)+TX、敵蟎普-4[CCN]+TX、敵蟎普-6[CCN]+TX、鄰敵蟎消(1090)+TX、硝戊酯(1092)+TX、硝辛酯殺蟎劑(1097)+TX、硝丁酯(1098)+TX、二磷(1102)+TX、二苯碸(IUPAC名稱)(1103)+TX、雙硫崙(別名)[CCN]+TX、二硫松(278)+TX、DNOC(282)+TX、dofenapyn(1113)+TX、得拉滅克汀(別名)[CCN]+TX、硫丹(294)+TX、因毒磷(1121)+TX、EPN(297)+TX、埃普利諾菌素(別名)[CCN]+TX、愛殺松(309)+TX、益硫磷(1134)+TX、依殺蟎(320)+TX、益多松(1142)+TX、抗蟎唑(1147)+TX、喹蟎醚(328)+TX、苯丁錫(330)+TX、芬硫克(337)+TX、甲氰菊酯(342)+TX、吡蟎胺(別名)+TX、唑蟎酯(345)+TX、除蟎酯(1157)+TX、芳氟胺(1161)+TX、氰戊菊酯(349)+TX、芬普尼(354)+TX、嘧蟎酯(360)+TX、氟佐隆(1166)+TX、氟苯亞胺噻唑(1167)+TX、氟蟎脲(366)+TX、氟氰菊酯(367)+TX、聯氟蟎(1169)+TX、氟蟲脲(370)+TX、氟氯苯菊酯(372)+TX、氟殺蟎(1174)+TX、氟胺氰菊酯(1184)+TX、FMC 1137(開發碼)(1185)+TX、伐蟲脒(405)+TX、伐蟲脒鹽酸鹽(405)+TX、福木松 (1192)+TX、甲脒(1193)+TX、林丹(430)+TX、果綠定(1205)+TX、合芬寧(424)+TX、飛達松(432)+TX、十六烷基環丙烷甲酸酯(IUPAC/化學摘要名稱)(1216)+TX、噻蟎酮(441)+TX、碘甲烷(IUPAC名稱)(542)+TX、水胺硫磷(別名)(473)+TX、異丙醇O-(甲氧基胺基硫代磷醯)水楊酸(IUPAC名稱)(473)+TX、伊維菌素(別名)[CCN]+TX、茉莉菊酯I(696)+TX、茉莉菊酯II(696)+TX、碘硫磷(1248)+TX、立氯化苯(430)+TX、祿芬隆(490)+TX、馬拉松(492)+TX、特蟎腈(1254)+TX、滅蚜磷(502)+TX、二噻磷(1261)+TX、二甲噻蒽(別名)[CCN]+TX、蟲蟎畏(1266)+TX、達馬松(527)+TX、滅大松(529)+TX、滅蟲威(530)+TX、滅多威(531)+TX、溴甲烷(537)+TX、速滅威(550)+TX、美文松(556)+TX、自克威(1290)+TX、密滅汀(557)+TX、米爾比霉素肟化物(別名)[CCN]+TX、丙胺氟(1293)+TX、亞速靈(561)+TX、茂果(1300)+TX、莫斯達汀(別名)[CCN]+TX、乃力松(567)+TX、NC-184(化合物碼)+TX、NC-512(化合物碼)+TX、尼氟利地(1309)+TX、尼柯霉素(別名)[CCN]+TX、戊氰威(1313)+TX、戊氰威1:1氯化鋅綜合物(1313)+TX、NNI-0101(化合物碼)+TX、NNI-0250(化合物碼)+TX歐滅松(594)+TX、殺線威(602)+TX、異滅多松(1324)+TX、碸拌磷(1325)+TX、pp'-DDT(219)+TX、巴拉松(615)+TX、氯菊酯(626)+TX、石油油料(別名)(628)+TX、芬硫磷(1330)+TX、 賽達松(631)+TX、福瑞松(636)+TX、裕必松(637)+TX、硫環磷(1338)+TX、益滅松(638)+TX、福賜米松(639)+TX、巴賽松(642)+TX、亞特松-甲基(652)+TX、多氯萜烯類(習知名稱)(1347)+TX、多萘菌素(別名)(653)+TX、丙氯醇(1350)+TX、佈飛松(662)+TX、蜱虱威(1354)+TX、克蟎特(671)+TX、烯蟲磷(673)+TX、殘殺威(678)+TX、乙福賽絕(1360)+TX、發果(1362)+TX、除蟲菊酯I(696)+TX、除蟲菊酯II(696)+TX、除蟲菊酯(696)+TX、噠蟎靈(699)+TX、必芬松(701)+TX、畢汰芬(706)+TX、嘧啶磷(1370)+TX、拜裕松(711)+TX、拜裕松(1381)+TX、R-1492(開發碼)(1382)+TX、RA-17(開發碼)(1383)+TX、魚藤酮(722)+TX、八甲磷(1389)+TX、硫線磷(別名)+TX、色拉菌素(別名)[CCN]+TX、SI-0009(化合物碼)+TX、蘇果(1402)+TX、螺蟎酯(738)+TX、螺甲蟎酯(739)+TX、SSI-121(開發碼)(1404)+TX、舒非崙(別名)[CCN]+TX、氟蟲胺(750)+TX、治螟磷(753)+TX、硫(754)+TX、SZI-121(開發碼)(757)+TX、氟胺氰菊酯(398)+TX、吡蟎胺(763)+TX、TEPP(1417)+TX、第三丁威(別名)+TX、殺蟲畏(777)+TX、四氯殺蟎碸(786)+TX、四抗菌素(別名)(653)+TX、殺蟎好(1425)+TX、硫芬諾(別名)+TX、抗蟲威(1431)+TX、久效威(800)+TX、甲基二硫松(801)+TX、克殺蟎(1436)+TX、蘇力菌素(別名)[CCN]+TX、福賜米松(1441)+TX、苯蟎噻(1443) +TX、三落松(820)+TX、唑呀威(別名)+TX、三氯松(824)+TX、三氯丙氧磷(1455)+TX、三活菌素(別名)(653)+TX、繁米松(847)+TX、維尼普唑[CCN]和YI-5302(化合物碼)+TX、一種殺藻劑,是從由下列所組成的物質群中選出:苯沙[CCN]+TX、二辛酸銅(IUPAC名稱)(170)+TX、硫酸銅(172)+TX、噻布三[CCN]+TX、二氯萘醌(1052)+TX、二羥二氯二苯甲烷(232)+TX、草多索(295)+TX、三苯錫(347)+TX、熟石灰[CCN]+TX、代森鈉(566)+TX、莫克草(714)+TX、醌萍胺(1379)+TX、西瑪津(730)+TX、三苯基醋酸錫(IUPAC名稱)(347)和三苯基氫氧化錫(IUPAC名稱)(347)+TX、一種驅蟲藥,是從由下列所組成的物質群中選出:阿巴汀(1)+TX、育畜磷(1011)+TX、得拉滅克汀(別名)[CCN]+TX、因滅汀(291)+TX、甲維鹽(291)+TX、埃普利諾菌素(別名)[CCN]+TX、伊維菌素(別名)[CCN]+TX、米爾比霉素肟化物(別名)[CCN]+TX、莫斯達汀(別名)[CCN]+TX、哌[CCN]+TX、色拉菌素(別名)[CCN]+TX、多殺菌素(737)和甲基托布津(1435)+TX、一種殺鳥劑,是從由下列所組成的物質群中選出:氯醛糖(127)+TX、異狄氏劑(1122)+TX、芬殺松(346)+TX、吡啶-4-胺(IUPAC名稱)(23)和馬錢子鹼(745)+TX、一種殺菌劑,是從由下列所組成的物質群中選出:1- 羥-1氫-吡啶-2-硫酮(IUPAC名稱)(1222)+TX、4-(喹啉-2-胺基)苯磺醯胺(IUPAC名稱)(748)+TX、8-羥基喹啉硫酸鹽(446)+TX、溴硝醇(97)+TX、二辛酸銅(IUPAC名稱)(170)+TX、氫氧化銅(IUPAC名稱)(169)+TX、甲酚[CCN]+TX、二氯芬(232)+TX、雙硫氧吡啶(1105)+TX、多地辛(1112)+TX、敵克松(1144)+TX、甲醛(404)+TX、汞加芬(別名)[CCN]+TX、春雷霉素(483)+TX、春雷黴素鹽酸鹽水合物(483)+TX、二甲胺基二硫代甲酸鎳(IUPAC名稱)(1308)+TX、硝基吡啶(580)+TX、辛異噻啉酮(590)+TX、喹酸(606)+TX、土黴素(611)+TX、羥基喹啉硫酸氫鉀鹽(446)+TX、噻菌靈(658)+TX、鏈黴素(744)+TX、鏈黴素硫酸鹽(744)+TX、克桔爛(766)+TX和硫柳汞(別名)[CCN]+TX、一種生物製劑,是從由下列所組成的物質群中選出:棉褐帶卷蛾(Adoxophyes orana GV)(別名)(12)+TX、放射形土壤桿菌(Agrobacterium ra二obacter)(別名)(13)+TX、鈍綏蟎種(Amblyseius spp.)(別名)(19)+TX、芹菜夜蛾(Anagrapha falcifera NPV)(別名)(28)+TX、纓翅纓小蜂屬(Anagrus atomus)(別名)(29)+TX、苜蓿蚜小蜂(Aphelinus abdominalis)(別名)(33)+TX、蚜科爾曼(Aphidius colemani)(別名)(34)+TX、食蚜癭蚊(Aphidoletes aphidimyza)(別名)(35)+TX、草地貪夜蛾(Autographa californica NPV)(別名)(38)+TX、強固芽胞桿菌(Bacillus firmus)(別名)(48)+TX、球形芽孢桿菌 (Bacillus sphaericus Neide)(學名)(49)+TX、蘇雲金芽孢桿菌(Bacillus thuringiensis Berliner)(學名)(51)+TX、蘇力菌鮎澤亞種(Bacillus thuringiensis subsp.Aizawai)(學名)(51)+TX、蘇雲金芽孢桿菌以色列亞種(Bacillus thuringiensis subsp.israelensis)(學名)(51)+TX、蘇雲金芽孢桿菌日本亞種(Bacillus thuringiensis subsp.japonensis)(學名)(51)+TX、蘇雲金芽孢桿菌kurstaki亞種(Bacillus thuringiensis subsp.kurstaki)(學名)(51)+TX、蘇雲金芽孢桿菌tenebrionis亞種(Bacillus thuringiensis subsp.tenebrionis)(學名)(51)+TX、白殭菌(Beauveria bassiana)(別名)(53)+TX、布氏白殭菌(Beauveria brongniartii)(別名)(54)+TX、普通草蛉(Chrysoperla carnea)(別名)(151)+TX、孟氏隱唇瓢蟲(Cryptolaemus montrouzieri)(別名)(178)+TX、蘋果蠢蛾顆粒體病毒(Cydia pomonella GV)(別名)(191)+TX、西伯利亞離顎繭蜂(Dacnusa sibirica)(別名)(212)+TX、豌豆潛蠅姬小蜂(Diglyphus isaea)(別名)(254)+TX、麗蚜小蜂(Encarsia formosa)(學名)(293)+TX、漿角蚜小蜂(Eretmocerus eremicus)(別名)(300)+TX、美洲棉鈴蟲(Helicoverpa zea NPV)(別名)(431)+TX、異小杆線蟲屬(Heterorhabditis bacteriophora)與H.megidis(別名)(433)+TX、聚長足瓢蟲(Hippodamia convergens)(別名)(442)+TX、寄生桔柑粉介殼蟲(Leptomastix dactylopii)(別名)(488)+TX、捕食性蝽象(Macrolophus caliginosus)(別名)(491)+TX、甘藍夜 蛾(Mamestra brassicae NPV)(別名)(494)+TX、Metaphycus helvolus(別名)(522)+TX、金龜子綠僵菌(Metarhizium anisopliae var.acridum)(學名)(523)+TX、綠殭菌(Metarhizium anisopliae var.anisopliae)(學名)(523)+TX、歐洲松銹鋸角葉蜂(Neodiprion sertifer NPV)和紅頭松葉蜂(N.lecontei NPV)(別名)(575)+TX、小花蝽種(Orius spp.)(別名)(596)+TX、玫煙色擬青黴(Paecilomyces fumosoroseus)(別名)(613)+TX、智利捕植蟍(Phytoseiulus persimilis)(別名)(644)+TX、Spodoptera exigua multicapsid核多角體病毒(學名)(741)+TX、Steinernema bibionis(別名)(742)+TX、小卷蛾斯氏線蟲(Steinernema carpocapsae)(別名)(742)+TX、夜蛾斯氏線蟲(Steinernema feltiae)(別名)(742)+TX、Steinernema glaseri(別名)(742)+TX、Steinernema riobrave(別名)(742)+TX、Steinernema riobravis(別名)(742)+TX、螻蛄斯氏線蟲(Steinernema scapterisci)(別名)(742)+TX、斯氏線蟲(Steinernema spp.)(別名)(742)+TX、赤眼蜂種(Trichogramma spp.)(別名)(826)+TX、西方盲走蟎(Typhlodromus occidentalis)(別名)(844)和蠟蚧輪枝菌(Verticillium lecanii)(別名)(848)+TX、一種土壤滅菌劑,是從由下列所組成的物質群中選出:碘甲烷(IUPAC名稱)(542)和溴甲烷(537)+TX、一種化學滅菌劑,是從由下列所組成的物質群中選出:唑磷[CCN]+TX、雙(氮丙啶)甲胺基磷硫化物(別 名)[CCN]+TX、白消安(別名)[CCN]+TX、除蟲脲(250)+TX、dimatif(別名)[CCN]+TX、六甲嘧胺[CCN]+TX、六甲磷[CCN]+TX、甲基涕巴[CCN]+TX、甲硫涕巴[CCN]+TX、甲基不育特[CCN]+TX、雙硫膦啉[CCN]+TX、氟幼脲(別名)[CCN]+TX、涕巴[CCN]+TX、硫代六甲磷(別名)[CCN]+TX、塞替派(別名)[CCN]+TX、不孕津(別名)[CCN]和尿烷亞胺(別名)[CCN]+TX、一種昆蟲費洛蒙,是從由下列所組成的物質群中選出:含(E)-dec-5-en-1-ol的(E)-dec-5-en-1-yl acetate(IUPAC名稱)(222)+TX、(E)-十三-4-烷烯-1-酸(IUPAC名稱)(829)+TX、(E)-6-甲基-2-庚烯-4醇(IUPAC名稱)(541)+TX、(E,Z)-十四烷-4,10-二烯-1-乙酸酯(IUPAC名稱)(779)+TX、(Z)-十二烯-7-醇-1-醋酸酯(IUPAC名稱)(285)+TX、(Z)-十六碳-11-烯醛(IUPAC名稱)(436)+TX、(Z)-十六烯-11-醇-1-乙酸酯(IUPAC名稱)(437)+TX、(Z)-hexadec-13-en-11-yn-1-yl acetate(IUPAC名稱)(438)+TX、(Z)-icos-13-en-10-one(IUPAC名稱)(448)+TX、(Z)-十四碳-7-烯-1-醛(IUPAC名稱)(782)+TX、(Z)-十四碳-9-烯-1-醇(IUPAC名稱)(783)+TX、(Z)-十四碳-9-烯-1-乙酸酯(IUPAC名稱)(784)+TX、(7E,9Z)-十二二烯-7,9-醇-1-乙酸酯(IUPAC名稱)(283)+TX、(9Z,11E)-十四烷-9,11-二烯-1-乙酸酯(IUPAC名稱)(780)+TX、(9Z,12E)-十四烷-9,12-二烯-乙酸酯(IUPAC名稱)(781)+TX、14-甲基十八碳-1-烯(IUPAC名稱)(545)+TX、含 4-methylnonan-5-one的4-methylnonan-5-ol(IUPAC名稱)(544)+TX、α-多紋素(別名)[CCN]+TX、brevicomin(別名)[CCN]+TX、codlelure(別名)[CCN]+TX、十二碳二烯醇(別名)(167)+TX、瓜實蠅性誘劑(別名)(179)+TX、雌舞毒蛾引誘劑(277)+TX、十二烷-8-烯-1-基乙酸酯(IUPAC名稱)(286)+TX、十二烷-9-烯-1-基乙酸酯(IUPAC名稱)(287)+TX、十二烷-8+TX、10-二烯-1-基乙酸酯(IUPAC名稱)(284)+TX、穀蠢引誘劑2號(別名)[CCN]+TX、乙基4-辛酸甲酯(IUPAC名稱)(317)+TX、丁子香酚(別名)[CCN]+TX、南部松小蠹誘劑(別名)[CCN]+TX、棉紅鈴蟲性誘劑(別名)(420)+TX、誘殺烯混劑(421)+TX、誘殺烯混劑I(別名)(421)+TX、誘殺烯混劑II(別名)(421)+TX、誘殺烯混劑III(別名)(421)+TX、誘殺烯混劑IV(別名)(421)+TX、紅鈴誘烯[CCN]+TX、齒小蠹二烯醇(別名)[CCN]+TX、齒小蠹烯醇(別名)[CCN]+TX、金龜子性誘劑(別名)(481)+TX、三甲基二氧三環壬烷(別名)[CCN]+TX、夜蛾誘劑(別名)[CCN]+TX、誘尺蛾酯(別名)[CCN]+TX、誘殺酯[CCN]+TX、四癸二烯酸(別名)[CCN]+TX、誘蟲醚(別名)(540)+TX、家蠅引誘劑(563)+TX、十八碳-2,13-二烯-1-乙酸(IUPAC名稱)(588)+TX、十八碳-3,13-二烯-1-乙酸(IUPAC名稱)(589)+TX、奧弗拉路(別名)[CCN]+TX、奧立他路(別名)(317)+TX、四癸烯基乙酸酯(別名)[CCN]+TX、地中海果蠅引誘劑[CCN]+TX、索地丁(別 名)(736)+TX、食菌甲誘醇(別名)[CCN]+TX、十四碳-11-烯-1-乙酸酯(IUPAC名稱)(785)+TX、地中海實蠅性誘劑(839)+TX、地中海實蠅性誘劑A(別名)(839)+TX、地中海實蠅性誘劑B1(別名)(839)+TX、地中海實蠅性誘劑B2(別名)(839)+TX、地中海實蠅性誘劑C(別名)(839)和創克科(別名)[CCN]+TX、一種昆蟲忌避劑,是從由下列所組成的物質群中選出:避蟲醇(IUPAC名稱)(591)+TX、丁基三甲苯基化氧(933)+TX、丁氧基(聚丙二醇)(936)+TX、己二酸二丁酯(IUPAC名稱)(1046)+TX、鄰苯二甲酸二丁酯(1047)+TX,丁二酸二丁酯(IUPAC名稱)(1048)+TX、二乙莖甲苯醯胺[CCN]+TX、驅蚊靈[CCN]+TX、鄰苯二甲酸二甲酯[CCN]+TX、乙基二醇(1137)+TX、二乙胺乙苯巴比妥[CCN]+TX、喹啉羧酯(1276)+TX、甲基新癸醯胺[CCN]+TX、草胺酸鹽[CCN]和派卡瑞丁[CCN]+TX、一種殺蟲劑,是從由下列所組成的物質群中選出:1-二氯-1-硝基乙烷(IUPAC/化學摘要名稱)(1058)+TX、1,1-二氯-2,2-二(4-乙苯基)乙烷(IUPAC名稱)(1056)+TX、1,2-二氯丙烷(IUPAC/化學摘要名稱)(1062)+TX、1,2-二氯丙烷with 1,3-二氯丙烯(IUPAC名稱)(1063)+TX、1-溴-2-氯乙烷(IUPAC/化學摘要名稱)(916)+TX、2,2,2-三氯-1-(3,4-二氯苯基)乙酸乙酯(IUPAC名稱)(1451)+TX、2,2-二氯乙烯基二甲基酯2-乙基亞硫醯基乙基磷酸甲酯(IUPAC名稱)(1066)+TX、2-(1,3-二 thiolan-2-yl)phenyl二methylcarbamate(IUPAC/化學摘要名稱)(1109)+TX、2-(2-丁氧基乙氧基)乙基硫氰酸酯(IUPAC/化學摘要名稱)(935)+TX、2-(4,5-dimethyl-1,3-dioxolan-2-yl)phenyl methylcarbamate(IUPAC/化學摘要名稱)(1084)+TX、2-(4-胺-3,5-二甲苯氧基)乙醇(IUPAC名稱)(986)+TX、2-氯乙烯磷酸二乙酯(IUPAC名稱)(984)+TX、2-咪唑啉酮(IUPAC名稱)(1225)+TX、2-異戊醯基-1,3-二酮(IUPAC名稱)(1246)+TX、2-methyl(prop-2-ynyl)aminophenyl methylcarbamate(IUPAC名稱)(1284)+TX、2-thiocyanatoethyl laurate(IUPAC名稱)(1433)+TX、3-溴-1-氯-1-丙烯(IUPAC名稱)(917)+TX、3-methyl-1-phenylpyrazol-5-yl dimethyl carbamate(IUPAC名稱)(1283)+TX、4-甲基(丙-2-炔)胺-3,5-二甲苯基胺基甲酸甲酯(IUPAC名稱)(1285)+TX、5,5-dimethyl-3-oxocyclohex-1-enyl dimethylcarbamate(IUPAC名稱)(1085)+TX、阿巴汀(1)+TX、歐殺松(2)+TX、啶蟲脒(4)+TX、家蠅磷(別名)[CCN]+TX、乙醯蟲腈[CCN]+TX、氟丙菊酯(9)+TX、丙烯腈(IUPAC名稱)(861)+TX、棉鈴威(15)+TX、得滅克(16)+TX、氧得滅克(863)+TX、艾氏劑(864)+TX、烯丙菊酯(17)+TX、阿洛胺菌素(別名)[CCN]+TX、除害威(866)+TX、á-氯氰菊酯(202)+TX、á-蛻皮激素(別名)[CCN]+TX、磷化鋁(640)+TX、賽果(870)+TX、醯胺硫酯(872)+TX、滅害威(873)+TX、胺吸磷(875)+TX、酸式草酸胺 吸磷(875)+TX、雙甲脒(24)+TX、新菸鹼(877)+TX、乙基撲殺磷(883)+TX、AVI 382(化合物碼)+TX、AZ60541(化合物碼)+TX、印楝素(別名)(41)+TX、亞滅松(42)+TX、乙基谷速松(44)+TX、甲基谷速松(48)+TX、偶氮磷(889)+TX、蘇雲金芽孢桿菌(Bacillus thuringiensis)δ-內毒素類(別名)(52)+TX、氟矽酸鋇(別名)[CCN]+TX、多硫化鋇(IUPAC/化學摘要名稱)(892)+TX、胡椒除蟲菊[CCN]+TX、拜耳22/190(開發碼)(893)+TX、拜耳22408(開發碼)(894)+TX、蟲威(58)+TX、丙硫克百威(60)+TX、殺蟲磺(66)+TX、â-氟氯氰菊酯(194)+TX、高效氯氰菊酯(203)+TX、聯苯菊酯(76)+TX、生物烯丙菊酯(78)+TX、丙戊烯丙菊酯S-環戊烯基異構體(別名)(79)+TX、bioethanomethrin[CCN]+TX、生物氯菊酯(908)+TX、生物殺蟲菊(80)+TX、雙(2-氯乙基)醚(IUPAC名稱)(909)+TX、雙三氟蟲脲(83)+TX、硼砂(86)+TX、溴殺菊酯(別名)+TX、甲基溴苯烯磷(914)+TX、溴殺烯(918)+TX、溴滴滴涕(別名)[CCN]+TX、溴磷松(920)+TX、乙基溴磷松(921)+TX、丁苯胺酯(924)+TX、撲虱靈(99)+TX、丁苯甲胺酯(926)+TX、脫甲基丁嘧啶膦(927)+TX、丁酮威(103)+TX、丁酯磷(932)+TX、丁酮碸威(104)+TX、丁基達蟎靈(別名)+TX、硫線磷(109)+TX、砷酸鈣[CCN]+TX、氰化鈣(444)+TX、石硫合劑(IUPAC名稱)(111)+TX、毒殺芬(941)+TX、氯殺殺威(943)+TX、西維因(115)+TX、克百威 (118)+TX、二硫化碳(IUPAC/化學摘要名稱)(945)+TX、四氯化碳(IUPAC名稱)(946)+TX、三硫磷(947)+TX、丁硫克百威(119)+TX、殺螟丹(123)+TX、殺螟丹鹽酸鹽(123)+TX、瑟瓦定(別名)(725)+TX、冰片丹(960)+TX、氯丹(128)+TX、十氯酮(963)+TX、殺蟲脒(964)+TX、殺蟲脒鹽酸鹽(964)+TX、氯氧磷(129)+TX、溴蟲腈(130)+TX、克芬松(131)+TX、定蟲脲(132)+TX、氯甲硫磷(136)+TX、氯仿[CCN]+TX、三氯硝基甲烷(141)+TX、氯腈肟磷(989)+TX、殺蟲吡啶(990)+TX、陶斯松(145)+TX、甲基陶斯松(146)+TX、氯甲硫磷(994)+TX、環蟲醯肼(150)+TX、瓜菊酯I(696)+TX、瓜菊酯II(696)+TX、瓜菊酯類(696)+TX、cis-resmethrin(別名)+TX、cismethrin(80)+TX、功夫菊酯(別名)+TX、除線威(999)+TX、氯氰碘柳胺(別名)[CCN]+TX、噻蟲胺(165)+TX、乙醯亞砷酸銅[CCN]+TX、砷酸銅[CCN]+TX、銅油酸[CCN]+TX、蠅毒磷(174)+TX、畜蟲磷(1006)+TX、克羅米通(別名)[CCN]+TX、丁烯磷(1010)+TX、育畜磷(1011)+TX、冰晶石(別名)(177)+TX、CS 708(開發碼)(1012)+TX、苯腈磷(1019)+TX、殺螟腈(184)+TX、果蟲磷(1020)+TX、環蟲菊[CCN]+TX、乙氰菊酯(188)+TX、氟氯氰菊酯(193)+TX、氯氟氰菊酯(196)+TX、氯氰菊酯(201)+TX、苯醚氰菊酯(206)+TX、殺蠅胺(209)+TX、賽殺磷(別名)[CCN]+TX、香芹烯(別名)[CCN]+TX、右旋胺菊酯(別名)(788) +TX、DAEP(1031)+TX、棉隆(216)+TX、DDT(219)+TX、加保扶(1034)+TX、溴氰菊酯(223)+TX、田樂磷(1037)+TX、田樂磷-O(1037)+TX、田樂磷-S(1037)+TX、滅賜松(1038)+TX、甲基滅賜松(224)+TX、滅賜松-O(1038)+TX、甲基異滅賜松(224)+TX、滅賜松-S-甲基(1038)+TX、滅賜松-S-甲基(224)+TX、碸吸磷(1039)+TX、丁醚脲(226)+TX、得拉松(1042)+TX、二胺磷(1044)+TX、大利松(227)+TX、異氯硫磷(1050)+TX、除線磷(1051)+TX、二氯松(236)+TX、二克膦(別名)+TX、dicresyl(別名)[CCN]+TX、百治磷(243)+TX、環蟲腈(244)+TX、狄氏劑(1070)+TX、二乙基5-甲基-3-吡唑磷酸鹽(IUPAC名稱)(1076)+TX、除蟲脲(250)+TX、二羥丙茶鹼(別名)[CCN]+TX、四氟甲醚菊酯[CCN]+TX、甲氟磷(1081)+TX、地麥威(1085)+TX、大滅松(262)+TX、芐菊酯(1083)+TX、甲基克芬松(265)+TX、敵蠅威(1086)+TX、消蟎酚(1089)+TX、代奈-代克新(1089)+TX、硝丙酚(1093)+TX、戊硝酚(1094)+TX、地樂酚(1095)+TX、呋蟲胺(271)+TX、苯蟲醚(1099)+TX、蔬果磷(1100)+TX、二氧威(1101)+TX、二磷(1102)+TX、二硫松(278)+TX、代西羅膦(1108)+TX、DNOC(282)+TX、得拉滅克汀(別名)[CCN]+TX、DSP(1115)+TX、脫皮甾酮(別名)[CCN]+TX、EI 1642(開發碼)(1118)+TX、甲維鹽(291)+TX、因滅汀苯甲酸鹽(291)+TX、EMPC(1120)+TX、右旋烯炔菊酯(292)+ TX、硫丹(294)+TX、因毒磷(1121)+TX、異狄氏劑(1122)+TX、EPBP(1123)+TX、EPN(297)+TX、保幼醚(1124)+TX、埃普利諾(別名)[CCN]+TX、S-氰戊菊酯(302)+TX、依他膦(別名)[CCN]+TX、殺蟲丹(308)+TX、愛殺松(309)+TX、乙蟲腈(310)+TX、益硫磷(1134)+TX、普伏松(312)+TX、甲酸乙酯(IUPAC名稱)[CCN]+TX、ethyl-DDD(別名)(1056)+TX、二溴乙烯(316)+TX、二氯乙烷(化學名稱)(1136)+TX、環氧乙烷[CCN]+TX、醚菊酯(319)+TX、益多松(1142)+TX、EXD(1143)+TX、胺磺磷(323)+TX、芬滅松(326)+TX、抗蟎唑(1147)+TX、皮蠅硫磷(1148)+TX、二乙基苯酚甲基胺基甲酸酯(1149)+TX、芬氟司林(1150)+TX、撲滅松(335)+TX、仲丁威(336)+TX、芬諾沙利(1153)+TX、苯氧威(340)+TX、吡氯氰菊酯(1155)+TX、甲氰菊酯(342)+TX、吡蟎胺(別名)+TX、繁福松(1158)+TX、芬殺松(346)+TX、乙基芬殺松[CCN]+TX、氰戊菊酯(349)+TX、芬普尼(354)+TX、氟啶蟲醯胺(358)+TX、氟蟲醯胺(CAS.註冊編號:272451-65-7)+TX、flucofuron(1168)+TX、氟蟎脲(366)+TX、氟氰菊酯(367)+TX、聯氟蟎(1169)+TX、嘧蟲胺[CCN]+TX、氟蟲脲(370)+TX、三氟醚菊酯(1171)+TX、氟氯苯菊酯(372)+TX、氟胺氰菊酯(1184)+TX、FMC 1137(開發碼)(1185)+TX、大福松(1191)+TX、伐蟲脒(405)+TX、伐蟲脒鹽酸鹽(405)+TX、福木松(1192)+TX、甲脒(1193)+TX、丁噻吩磷 (1194)+TX、福司吡酯(1195)+TX、福賽絕(408)+TX、伐線丹(1196)+TX、呋線威(412)+TX、糠醛菊酯(1200)+TX、超高效三氟氯氰菊酯(197)+TX、林丹(430)+TX、雙胍鹽(422)+TX、雙胍辛乙酸鹽(422)+TX、GY-81(開發碼)(423)+TX、合芬寧(424)+TX、氯蟲醯肼(425)+TX、HCH(430)+TX、HEOD(1070)+TX、七氯(1211)+TX、飛達松(432)+TX、速殺硫磷[CCN]+TX、氟鈴脲(439)+TX、HHDN(864)+TX、氟蟻腙(443)+TX、氰化氫(444)+TX、烯蟲乙酯(445)+TX、hyquincarb(1223)+TX、益達胺(458)+TX、炔咪菊酯(460)+TX、茚蟲威(465)+TX、碘甲烷(IUPAC名稱)(542)+TX、IPSP(1229)+TX、依殺松(1231)+TX、碳氯靈(1232)+TX、水胺硫磷(別名)(473)+TX、異艾氏劑(1235)+TX、異柳磷(1236)+TX、異蘭(1237)+TX、滅必蝨(472)+TX、異丙醇O-(甲氧基胺基硫代磷醯)水楊酸鹽(IUPAC名稱)(473)+TX、稻瘟靈(474)+TX、異拌磷(1244)+TX、加福松(480)+TX、伊維菌素(別名)[CCN]+TX、茉莉菊酯I(696)+TX、茉莉菊酯II(696)+TX、碘硫磷(1248)+TX、保幼激素I(別名)[CCN]+TX、保幼激素II(別名)[CCN]+TX、保幼激素III(別名)[CCN]+TX、克來範(1249)+TX、丙諾保幼素(484)+TX、高效氯氟氰菊酯(198)+TX、砷酸鉛[CCN]+TX、lepimectin(CCN)+TX、對溴磷(1250)+TX、立氯化苯(430)+TX、lirimfos(1251)+TX、祿芬隆(490)+TX、福賽絕(1253)+TX、m-枯烯 基胺基甲酸甲酯(IUPAC名稱)(1014)+TX、磷化鎂(IUPAC名稱)(640)+TX、馬拉松(492)+TX、特蟎腈(1254)+TX、疊氮磷(1255)+TX、殺蚜磷(502)+TX、甲基殺蚜磷(1258)+TX、殺蚜松(1260)+TX、二噻磷(1261)+TX、氯化亞汞(513)+TX、mesulfenfos(1263)+TX、氰氟蟲腙(CCN)+TX、威百畝(519)+TX、metam-potassium(別名)(519)+TX、威是畝(519)+TX、蟲蟎畏(1266)+TX、達馬松(527)+TX、甲磺醯氟(IUPAC/化學摘要名稱)(1268)+TX、滅大松(529)+TX、殺蟲威(530)+TX、殺蟲乙烯磷(1273)+TX、殺多威(531)+TX、烯蟲酯(532)+TX、喹啉羧酯(1276)+TX、甲醚菊酯(別名)(533)+TX、甲氧氯(534)+TX、甲氧蟲醯肼(535)+TX、溴甲烷(537)+TX、異硫氰酸甲酯(543)+TX、三氯乙烷(別名)[CCN]+TX、二氯甲烷[CCN]+TX、甲氧苄氟菊酯[CCN]+TX、速殺威(550)+TX、蟲酮(1288)+TX、美文松(556)+TX、自克威(1290)+TX、密殺汀(557)+TX、米爾比霉素肟化物(別名)[CCN]+TX、丙胺氟(1293)+TX、殺蟻靈(1294)+TX、亞速靈(561)+TX、茂果(1300)+TX、莫斯達汀(別名)[CCN]+TX、萘酞磷(別名)[CCN]+TX、乃力松(567)+TX、萘(IUPAC/化學摘要名稱)(1303)+TX、NC-170(開發碼)(1306)+TX、NC-184(化合物碼)+TX、尼古丁(578)+TX、硫酸菸鹼(578)+TX、尼氟利地(1309)+TX、烯啶蟲胺(579)+TX、噻(1311)+TX、戊氰威(1313)+TX、 戊氰威1:1氯化鋅綜合物(1313)+TX、NNI-0101(化合物碼)+TX、NNI-0250(化合物碼)+TX、去甲菸鹼(習知名稱)(1319)+TX、雙苯氟脲(585)+TX、多氟脲(586)+TX、O-5-二氯-4-靛酚-O-乙基硫代磷酸酯(IUPAC名稱)(1057)+TX、O,O-diethyl O-4-methyl-2-oxo-2H-chromen-7-yl phosphorothioate(IUPAC名稱)(1074)+TX、O,O-diethyl O-6-methyl-2-propylpyrimidin-4-yl phosphorothioate(IUPAC名稱)(1075)+TX、O,O,O',O'-四丙基二硫代焦磷酸鹽(IUPAC名稱)(1424)+TX、油酸(IUPAC名稱)(593)+TX、歐滅松(594)+TX、殺線威(602)+TX、滅多松(609)+TX、異滅多松(1324)+TX、碸拌磷(1325)+TX、pp'-DDT(219)+TX、對二氯苯[CCN]+TX、巴拉松(615)+TX、甲基-巴拉松(616)+TX、氟幼脲(別名)[CCN]+TX、五氯苯酚(623)+TX、月桂酸五氯苯酯(IUPAC名稱)(623)+TX、氯菊酯(626)+TX、石油油料(別名)(628)+TX、PH 60-38(開發碼)(1328)+TX、芬硫磷(1330)+TX、苯醚菊酯(630)+TX、賽達松(631)+TX、福瑞松(636)+TX、裕必松(637)+TX、硫環磷(1338)+TX、益滅松(638)+TX、對氯硫磷(1339)+TX、福賜米松(639)+TX、磷化氫(IUPAC名稱)(640)+TX、巴賽松(642)+TX、甲基巴賽松(1340)+TX、pirimetaphos(1344)+TX、抗蚜威(651)+TX、乙基嘧啶磷(1345)+TX、亞特松-甲基(652)+TX、polychlorodicyclopentadiene isomers (IUPAC名稱)(1346)+TX、多氯萜烯類(習知名稱)(1347)+TX、亞砷酸鉀[CCN]+TX、硫氰酸鉀[CCN]+TX、炔丙菊脂(655)+TX、早熟素I(別名)[CCN]+TX、早熟素II(別名)[CCN]+TX、早熟素III(別名)[CCN]+TX、primidophos(1349)+TX、佈飛松(662)+TX、丙氟菊酯[CCN]+TX、蜱虱威(1354)+TX、猛殺威(1355)+TX、丙蟲磷(1356)+TX、烯蟲磷(673)+TX、殘殺威(678)+TX、乙福賽絕(1360)+TX、丙硫磷(686)+TX、發果(1362)+TX、protrifenbute[CCN]+TX、吡蚜酮(688)+TX、白克松(689)+TX、定菌磷(693)+TX、pyresmethrin(1367)+TX、除蟲菊酯I(696)+TX、除蟲菊酯II(696)+TX、除蟲菊酯(696)+TX、噠蟎靈(699)+TX、二氯丙烯(700)+TX、必芬松(701)+TX、畢汰芬(706)+TX、嘧啶磷(1370)+TX、吡丙醚(708)+TX、苦木科植物(別名)[CCN]+TX、拜裕松(711)+TX、拜裕松-甲基(1376)+TX、quinothion(1380)+TX、拜裕松(1381)+TX、R-1492(開發碼)(1382)+TX、雷複尼特(別名)[CCN]+TX、苄呋菊酯(719)+TX、魚藤酮(722)+TX、RU 15525(開發碼)(723)+TX、RU 25475(開發碼)(1386)+TX、魚尼丁(別名)(1387)+TX、利阿諾定(習知名稱)(1387)+TX、沙巴藜蘆(別名)(725)+TX、八甲磷(1389)+TX、硫線磷(別名)+TX、色拉菌素(別名)[CCN]+TX、SI-0009(化合物碼)+TX、SI-0205(化合物碼)+TX、SI-0404(化合物碼)+TX、SI-0405(化合物碼)+TX、氟矽菊酯(728)+TX、SN 72129(開發碼)(1397)+TX、亞砷酸鈉[CCN]+TX、氰化鈉(444)+TX、氟化鈉(IUPAC/化學摘要名稱)(1399)+TX、六氟合矽酸鈉(1400)+TX、五氯酚鈉(623)+TX、硒酸鈉(IUPAC名稱)(1401)+TX、硫氰酸鈉[CCN]+TX、蘇果(1402)+TX、多殺菌素(737)+TX、軟體動物甲蟎酯(739)+TX、軟體動物蟲乙酯(CCN)+TX、sulcofuron(746)+TX、sulcofuron-sodium(746)+TX、氟蟲胺(750)+TX、治螟磷(753)+TX、硫醯氟(756)+TX、硫丙磷(1408)+TX、焦油(別名)(758)+TX、氟胺氰菊酯(398)+TX、噻蟎威(1412)+TX、TDE(1414)+TX、得芬諾(762)+TX、吡蟎胺(763)+TX、特布松(764)+TX、伏蟲隆(768)+TX、七氟菊酯(769)+TX、亞培松(770)+TX、TEPP(1417)+TX、環戊烯丙菊酯(1418)+TX、第三丁威(別名)+TX、托福松(773)+TX、四氯乙烷[CCN]+TX、殺蟲畏(777)+TX、胺菊酯(787)+TX、高效反式氯氰菊酯(204)+TX、噻蟲啉(791)+TX、硫芬諾(別名)+TX、噻蟲(792)+TX、thicrofos(1428)+TX、抗蟲威(1431)+TX、殺蟲環(798)+TX、硫賜安(798)+TX、硫雙威(799)+TX、久效威(800)+TX、甲基二硫松(801)+TX、硫磷(1434)+TX、thiosultap(803)+TX、thiosultap-sodium(803)+TX、蘇力菌素(別名)[CCN]+TX、唑蟲醯胺(809)+TX、四溴菊酯(812)+TX、四氟苯菊酯(813)+TX、transpermethrin(1440)+TX、福賜米松(1441)+TX、唑蚜威(818)+TX、三落松(820)+TX、 唑呀威(別名)+TX、三氯松(824)+TX、trichlormetaphos-3(別名)[CCN]+TX、壤蟲磷(1452)+TX、三氯丙氧磷(1455)+TX、殺鈴脲(835)+TX、混殺威(840)+TX、烯蟲硫酯(1459)+TX、繁米松(847)+TX、維尼普唑[CCN]+TX、藜蘆定(別名)(725)+TX、藜蘆鹼類(別名)(725)+TX、XMC(853)+TX、滅殺威(854)+TX、YI-5302(化合物碼)+TX、Z-氯氰菊酯(205)+TX、zetamethrin(別名)+TX、磷化鋅(640)+TX、zolaprofos(1469)與ZXI 8901(開發碼)(858)+TX、氰蟲醯胺[736994-63-19]+TX、氯蟲醯胺[500008-45-7]+TX、cyenopyrafen[560121-52-0]+TX、丁氟蟎酯[400882-07-7]+TX、pyrifluquinazon[337458-27-2]+TX、賜諾特[187166-40-1+187166-15-0]+TX、軟體動物蟲乙酯[203313-25-1]+TX、氟啶蟲胺腈[946578-00-3]+TX、丁烯芬普尼[704886-18-0]+TX、氯氟醚菊酯[915288-13-0]+TX、四氟醚菊酯[84937-88-2]+TX、一種殺軟體動物劑,是從由下列所組成的物質群中選出:丁蝸錫(IUPAC名稱)(913)+TX、溴乙醯胺[CCN]+TX、砷酸鈣[CCN]+TX、除線威(999)+TX、乙醯亞砷酸銅[CCN]+TX、硫酸銅(172)+TX、三苯錫(347)+TX、磷酸鐵(IUPAC名稱)(352)+TX、四聚乙醛(518)+TX、滅蟲威(530)+TX、氯硝柳胺(576)+TX、耐克軟體動物乙醇胺鹽(576)+TX、五氯苯酚(623)+TX、五氯酚鈉(623)+TX、噻蟎威(1412)+TX、硫雙威(799)+TX、三 丁基氧化錫(913)+TX、蝸軟體動物淨(1454)+TX、混殺威(840)+TX、三苯基醋酸錫(IUPAC名稱)(347)和三苯基氫氧化錫(IUPAC名稱)(347)+TX、pyriprole[394730-71-3]+TX、一種殺線蟲劑,是從由下列所組成的物質群中選出:AKD-3088(化合物碼)+TX、1,2-二溴-3-氯丙烷(IUPAC/化學摘要名稱)(1045)+TX、1,2-二氯丙烷(IUPAC/化學摘要名稱)(1062)+TX、1,2-二氯丙烷含1,3-二氯丙烯(IUPAC名稱)(1063)+TX、1,3-二氯丙烯(233)+TX、3,4-dichlorotetrahydrothiophene 1,1-dioxide(IUPAC/化學摘要名稱)(1065)+TX、3-(4-氯苯)-5-甲基羅丹寧(IUPAC名稱)(980)+TX、5-methyl-6-thioxo-1,3,5-thiadiazinan-3-ylacetic acid(IUPAC名稱)(1286)+TX、6-異戊烯胺基嘌呤(別名)(210)+TX、阿巴汀(1)+TX、乙醯蟲腈[CCN]+TX、棉鈴威(15)+TX、得滅克(16)+TX、氧得滅克(863)+TX、AZ 60541(化合物碼)+TX、benclothiaz[CCN]+TX、苯菌靈(62)+TX、丁基達蟎靈(別名)+TX、硫線磷(109)+TX、克百威(118)+TX、二硫化碳(945)+TX、丁硫克百威(119)+TX、三氯硝基甲烷(141)+TX、陶斯松(145)+TX、除線威(999)+TX、細胞分裂素(別名)(210)+TX、棉隆(216)+TX、DBCP(1045)+TX、DCIP(218)+TX、二胺磷(1044)+TX、除線磷(1051)+TX、二克膦(別名)+TX、大滅松(262)+TX、得拉滅克汀(別名)[CCN]+TX、甲維鹽(291)+TX、 因滅汀苯甲酸鹽(291)+TX、埃普利諾菌素(別名)[CCN]+TX、普伏松(312)+TX、二溴乙烯(316)+TX、芬滅松(326)+TX、吡蟎胺(別名)+TX、繁福松(1158)+TX、福賽絕(408)+TX、伐線丹(1196)+TX、糠醛(別名)[CCN]+TX、GY-81(開發碼)(423)+TX、速殺硫磷[CCN]+TX、碘甲烷(IUPAC名稱)(542)+TX、isamidofos(1230)+TX、依殺松(1231)+TX、伊維菌素(別名)[CCN]+TX、呋喃甲基腺嘌呤(別名)(210)+TX、甲基滅蚜磷(1258)+TX、威百畝(519)+TX、metam-potassium(別名)(519)+TX、威是畝(519)+TX、溴甲烷(537)+TX、異硫氰酸甲酯(543)+TX、米爾比霉素肟化物(別名)[CCN]+TX、莫斯達汀(別名)[CCN]+TX、疣孢漆斑(真)菌(Myrothecium verrucaria)組成物(別名)(565)+TX、NC-184(化合物碼)+TX、殺線威(602)+TX、福瑞松(636)+TX、福賜米松(639)+TX、福賜卡[CCN]+TX、硫線磷(別名)+TX、色拉菌素(別名)[CCN]+TX、多殺菌素(737)+TX、第三丁威(別名)+TX、托福松(773)+TX、四氯噻吩(IUPAC/化學摘要名稱)(1422)+TX、硫芬諾(別名)+TX、硫磷(1434)+TX、三落松(820)+TX、唑呀威(別名)+TX、二甲苯酚[CCN]+TX、YI-5302(化合物碼)和玉米素(別名)(210)+TX、fluensulfone[318290-98-1]+TX、硝化抑制劑,是從由下列所組成的物質群中選出:乙基黃原酸鉀[CCN]和硝基吡啶(580)+TX、 一種植物活化劑,是從由下列所組成的物質群選出:阿昔貝拉(6)+TX、阿拉酸式苯-S-甲基(6)+TX、噻菌靈(658)和虎杖(Reynoutria sachalinensis)提取物(別名)(720)+TX、一種殺鼠劑,是從由下列所組成的物質群中選出:2-異戊醯基-1,3-茚二酮(IUPAC名稱)(1246)+TX、4-(喹啉-2-胺基)苯磺醯胺(IUPAC名稱)(748)+TX、alpha-chlorohydrin[CCN]+TX、磷化鋁(640)+TX、安妥(880)+TX、三氧化二砷(882)+TX、碳酸鋇(891)+TX、雙鼠脲(912)+TX、大隆(89)+TX、溴敵隆(91)+TX、溴鼠胺(92)+TX、氰化鈣(444)+TX、氯醛糖(127)+TX、氯鼠酮(140)+TX、維生素D3(別名)(850)+TX、氯殺鼠靈(1004)+TX、克滅鼠(1005)+TX、殺鼠迷(175)+TX、鼠立死(1009)+TX、鼠得克(246)+TX、噻鼠靈(249)+TX、敵鼠(273)+TX、鈣化醇(301)+TX、氟鼠靈(357)+TX、氟乙醯胺(379)+TX、氟鼠啶(1183)+TX、flupropadine hydrochloride(1183)+TX、林丹(430)+TX、HCH(430)+TX、氰化氫(444)+TX、碘甲烷(IUPAC名稱)(542)+TX、立氯化苯(430)+TX、磷化鎂(IUPAC名稱)(640)+TX、溴甲烷(537)+TX、鼠特靈(1318)+TX、毒鼠磷(1336)+TX、磷化氫(IUPAC名稱)(640)+TX、磷[CCN]+TX、殺鼠酮(1341)+TX、亞砷酸鉀[CCN]+TX、滅鼠優(1371)+TX、紅海蔥苷(1390)+TX、亞砷酸鈉[CCN]+TX、氰化鈉(444)+TX、氟乙酸鈉(735)+ TX、馬錢子鹼(745)+TX、硫酸鉈[CCN]+TX、殺鼠靈(851)和磷化鋅(640)+TX、一種增效劑,是從由下列所組成的物質群中選出:2-(2-butoxyethoxy)ethyl piperonylate(IUPAC名稱)(934)+TX、5-(1,3-benzodioxol-5-yl)-3-hexylcyclohex-2-enone(IUPAC名稱)(903)+TX、金合歡醇與橙花第三醇(別名)(324)+TX、MB-599(開發碼)(498)+TX、MGK 264(開發碼)(296)+TX、向日葵基丁醇(649)+TX、增效醛(1343)+TX、丙基異構體(1358)+TX、S421(開發碼)(724)+TX、增效菊(1393)+TX、麻油酚(1394)與亞碸(1406)+TX、一種獸用驅避劑,是從由下列所組成的物質群中選出:蒽醌(32)+TX、氯醛糖(127)+TX、環烷酸銅[CCN]+TX、氧氯化銅(171)+TX、大利松(227)+TX、雙環戊二烯(化學名稱)(1069)+TX、雙胍鹽(422)+TX、雙胍辛乙酸鹽(422)+TX、滅蟲威(530)+TX、吡啶-4-胺(IUPAC名稱)(23)+TX、福美雙(804)+TX、混殺威(840)+TX、環烷酸鋅[CCN]和二甲胺荒酸鋅(856)+TX、一種殺病毒劑,是從由馬南(別名)[CCN]和病毒唑(別名)[CCN]+TX所組成的物質群中選出、一種傷口保護劑,是從由下列所組成的物質群中選出:氧化汞(512)+TX、辛異噻啉酮(590)和甲基硫菌靈(802)+TX,和生物活性化合物,是從由下列所組成的物質群中選 出:氮康唑(60207-31-0]+TX、雙苯三唑醇[70585-36-3]+TX、糠菌唑[116255-48-2]+TX、環唑醇[94361-06-5]+TX、醚唑[119446-68-3]+TX、烯唑醇[83657-24-3]+TX、氟環唑[106325-08-0]+TX、腈苯唑[114369-43-6]+TX、氟喹唑[136426-54-5]+TX、氟矽唑[85509-19-9]+TX、粉唑醇[76674-21-0]+TX、己唑醇[79983-71-4]+TX、抑黴唑[35554-44-0]+TX、亞胺唑[86598-92-7]+TX、種菌唑[125225-28-7]+TX、葉菌唑[125116-23-6]+TX、腈菌唑[88671-89-0]+TX、稻瘟酯[101903-30-4]+TX、戊菌唑[66246-88-6]+TX、丙硫菌唑[178928-70-6]+TX、啶斑肟[88283-41-4]+TX、咪鮮胺[67747-09-5]+TX、丙環唑[60207-90-1]+TX、矽氟唑[149508-90-7]+TX、戊唑醇[107534-96-3]+TX、四氟醚唑[112281-77-3]+TX、三唑酮[43121-43-3]+TX、三唑醇[55219-65-3]+TX、氟菌唑[99387-89-0]+TX、滅菌唑[131983-72-7]+TX、環丙嘧啶醇[12771-68-5]+TX、氯苯嘧啶醇[60168-88-9]+TX、氟苯嘧啶醇[63284-71-9]+TX、乙嘧酚磺酸酯[41483-43-6]+TX、二甲嘧酚[5221-53-4]+TX、乙嘧酚[23947-60-6]+TX、嗎菌靈[1593-77-7]+TX、苯鏽啶[67306-00-7]+TX、丁苯嗎啉[67564-91-4]+TX、軟體動物環菌胺[118134-30-8]+TX、十三嗎啉[81412-43-3]+TX、嘧菌環胺[121552-61-2]+TX、嘧菌胺[110235-47-7]+TX、嘧黴胺[53112-28-0]+TX、拌種咯[74738-17-3]+TX、咯菌腈[131341-86-1]+TX、苯霜靈 [71626-11-4]+TX、呋霜靈[57646-30-7]+TX、甲霜靈[57837-19-1]+TX、R甲霜靈[70630-17-0]+TX、呋醯胺[58810-48-3]+TX、霜靈[77732-09-3]+TX、苯菌靈[17804-35-2]+TX、多菌靈[10605-21-7]+TX、咪菌威[62732-91-6]+TX、麥穗寧[3878-19-1]+TX、噻菌靈[148-79-8]+TX、乙菌利[84332-86-5]+TX、菌核利[24201-58-9]+TX、異菌脲[36734-19-7]+TX、myclozoline[54864-61-8]+TX、腐霉利[32809-16-8]+TX、乙烯菌核利[50471-44-8]+TX、啶醯菌胺[188425-85-6]+TX、萎銹靈[5234-68-4]+TX、甲呋醯胺[24691-80-3]+TX、福多寧[66332-96-5]+TX、滅銹胺[55814-41-0]+TX、氧化萎銹靈[5259-88-1]+TX、吡噻菌胺[183675-82-3]+TX、噻呋醯胺[130000-40-7]+TX、雙胍鹽[108173-90-6]+TX、多果定[2439-10-3][112-65-2](游離鹼)+TX、雙胍辛胺[13516-27-3]+TX、嘧菌酯[131860-33-8]+TX、醚菌胺[149961-52-4]+TX、烯肟菌酯{Proc.BCPC,Int.Congr.,Glasgow,2003,1,93}+TX、氟嘧菌酯[361377-29-9]+TX、醚菌酯[143390-89-0]+TX、苯氧菌胺[133408-50-1]+TX、肟菌酯[141517-21-7]+TX、orysastrobin[248593-16-0]+TX、啶氧菌酯[117428-22-5]+TX、吡唑醚菌酯[175013-18-0]+TX、福美鐵[14484-64-1]+TX、代森錳鋅[8018-01-7]+TX、代森錳[12427-38-2]+TX、代森聯[9006-42-2]+TX、丙森鋅[12071-83-9]+TX、福美雙[137-26-8]+TX、代森鋅 [12122-67-7]+TX、二甲胺荒酸鋅[137-30-4]+TX、敵菌丹[2425-06-1]+TX、克菌丹[133-06-2]+TX、抑菌靈[1085-98-9]+TX、氟氯菌核利[41205-21-4]+TX、滅菌丹[133-07-3]+TX、甲苯氟磺胺[731-27-1]+TX、波爾多液[8011-63-0]+TX、氫氧化銅[20427-59-2]+TX、copperoxychlorid[1332-40-7]+TX、coppersulfat[7758-98-7]+TX、copperoxid[1317-39-1]+TX、代森錳銅[53988-93-5]+TX、喹啉銅[10380-28-6]+TX、敵蟎普[131-72-6]+TX、酞菌酯[10552-74-6]+TX、敵瘟磷[17109-49-8]+TX、異稻瘟淨[26087-47-8]+TX、稻瘟靈[50512-35-1]+TX、氯瘟磷[36519-00-3]+TX、定菌磷[13457-18-6]+TX、甲基立枯磷[57018-04-9]+TX、阿拉酸式苯-S-甲基[135158-54-2]+TX、敵菌靈[101-05-3]+TX、benthiavalicarb[413615-35-7]+TX、灰瘟素[2079-00-7]+TX、滅蟎猛[2439-01-2]+TX、氯苯甲醚[2675-77-6]+TX、百菌清[1897-45-6]+TX、環氟菌胺[180409-60-3]+TX、霜脲氰[57966-95-7]+TX、二氯萘醌[117-80-6]+TX、diclocymet[139920-32-4]+TX、噠菌酮[62865-36-5]+TX、氯硝胺[99-30-9]+TX、乙黴威[87130-20-9]+TX、烯醯嗎啉[110488-70-5]+TX、SYP LI90(氟嗎啉)[211867-47-9]+TX、二氰蒽醌[3347-22-6]+TX、噻唑菌胺[162650-77-3]+TX、土菌靈[2593-15-9]+TX、唑菌酮[131807-57-3]+TX、fenamidone[161326-34-7]+TX、氰菌胺[115852-48-7]+TX、三苯錫[668-34-8]+ TX、嘧菌腙[89269-64-7]+TX、氟啶胺[79622-59-6]+TX、氟啶醯菌胺[239110-15-7]+TX、磺菌胺[106917-52-6]+TX、fenhexamid[126833-17-8]+TX、三乙膦酸鋁[39148-24-8]+TX、霉靈[10004-44-1]+TX、纈黴威[140923-17-7]+TX、IKF 916(氰霜唑)[120116-88-3]+TX、春雷黴素[6980-18-3]+TX、磺菌威[66952-49-6]+TX、metrafenone[220899-03-6]+TX、戊菌隆[66063-05-6]+TX、四氯苯酞[27355-22-2]+TX、多氧菌素[11113-80-7]+TX、噻菌靈[27605-76-1]+TX、霜黴威[25606-41-1]+TX、proquinazid[189278-12-4]+TX、咯喹酮[57369-32-1]+TX、喹氧靈[124495-18-7]+TX、五氯硝基苯[82-68-8]+TX、硫磺[7704-34-9]+TX、tiadinil[223580-51-6]+TX、咪唑[72459-58-6]+TX、三環唑[41814-78-2]+TX、胺靈[26644-46-2]+TX、井岡黴素[37248-47-8]+TX、醯菌胺(RH7281)[156052-68-5]+TX、雙炔醯菌胺[374726-62-2]+TX、isopyrazam[881685-58-1]+TX、sedaxane[874967-67-6]+TX、3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid(9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-napht halen-5-yl)-amide(揭露於WO 2007/048556)+TX、3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid[2-(2,4-dichlorophenyl)-2-methoxy-1-methyl-ethyl]-amide(揭露於WO 2008/148570)+TX、1-[4-[4-[(5S)5-(2,6-difluorophenyl)-4,5-dihydro-1,2-oxazol- 3-yl]-1,3-thiazol-2-yl]piperidin-1-yl]-2-[5-methyl-3-(trifluo romethyl)-1H-pyrazol-1-yl]ethanone+TX、1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-1,2-oxazol-3-yl]-1,3-thiazol-2-yl]piperidin-1-yl]-2-[5-methyl-3-(trifluorom ethyl)-1H-pyrazol-1-yl]ethanone[1003318-67-9](兩者皆揭露於WO 2010/123791、WO 2008/013925、WO 2008/013622和WO 2011/051243第20頁)+TX,和3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid(3',4',5'-trifluoro-biphenyl-2-yl)-amide(揭露於WO 2006/087343)+TX、S)-[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-異唑-4-基]-吡啶-3-基甲醇+TX、3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-異唑-4-基]-吡啶-3-基甲醇+TX和3-二氟甲基-1-甲基-1H-吡唑-4-羧酸(3',4',5'-五氟聯苯-2-基)-醯胺(揭露於WO 2006/087343)+TX、3-(二氟甲基)-N-甲氧基-1-甲基-N-[1-甲基-2-(2,4,6-三氯苯基)乙基]-1H-吡唑-4-甲醯胺+TX,TX的混合物配對物也可以是酯類或鹽類的形式,如《The Pesticide Manual》(殺蟲劑手冊,2000年第12版(BCPC))中所提及。 The following mixtures of the compound of the formula I with the active ingredient are preferred. Preferably, the term "TX" refers to a compound encompassed by the compound of the formula I or, preferably, the term "TX" is used. Compounds from Tables 1 to 12, A, B and C: an adjuvant selected from the group consisting of petroleum (alias) (628) + TX, an acaricide consisting of the following Selected from the group of substances: 1,1-di-(4-chlorophenyl)-2-ethoxyethanol (name of the International Union of Pure and Applied Chemistry (IUPAC)) (910) + TX, 2, 4- Chlorophenylbenzenesulfonic acid (IUPAC/Chemical abstract name) (1059) + TX, 2-fluoro-N-methyl-N-1-naphthylacetamide (IUPAC name) (1295) + TX, 4-chlorobenzene Phenyl phenyl hydrazine (IUPAC name) (981) + TX, abatin (1) + TX, hydrazine (3) + TX, acetamipridonitrile [CCN] + TX, flumethrin (9) + TX, get gram (16) + TX, oxydike (863), alpha cypermethrin (202) + TX, match (870) + TX, sulfamate [CCN] + TX, guanamine thioester ( 872) + TX, amine phosphorus (875) + TX, acid oxalate amine phosphorus (875) + TX, amitraz (24) + TX, chlorpyrifos (881) + TX, arsenic trioxide (882) + TX , AVI 382 (compound code) + TX, AZ 60541 (chemical Code) +TX, Ethyl tacrolimus (44) + TX, methyl tacrolimus (45) + TX, azobenzene (IUPAC name) (888) + TX, triazolyl (46) + TX, Azophos (889)+TX, benomyl (62)+TX, benzene Phosphorus (alias) [CCN]+TX, benzophenone (71)+TX, benzyl benzoate (IUPAC name) [CCN]+TX, Bifendrazin (74)+TX, bifenthrin (76)+ TX, lysine (907) + TX, bromomethrin (alias) + TX, bromo (918) + TX, bromo pine (920) + TX, ethyl bromide (921) + TX, Bromodecyl ester (94) + TX, chlorpyrifos (99) + TX, butanone (103) TX, butanone oxime (104) + TX, butyl daprost (alias) + TX, stone sulphur mixture (IUPAC name) (111)+TX, toxaphene (941)+TX, chlorhexazone (943)+TX, carbaryl (115)+TX, carbofuran (118)+TX, trithion ( 947) +TX, CGA 50'439 (development code) (125) + TX, cockroach (126) + TX, chlorpyrifos (959) + TX, insecticidal 964 (964) + TX, insecticidal strontium salt Acid salt (964) + TX, chlorfenapyr (130) + TX, sterol (968) + TX, decyl ester (970) + TX, diazepam (971) + TX, kefensone (131) +TX, ethyl ester sterol (975) + TX, decyl ether (977) + TX, 螟蛉 (978) + TX, propyl ester sterol (983) + TX, Taosson (145) + TX, A Chitosson (146)+TX, chloromethylphosphonium (994)+TX, fenvalerate I(696)+TX, methyrin II (696)+TX, fenvalerate (696)+TX, tetraterpenoid (158) + TX, cyanoguanidin (alias) [CCN] + TX, fly poison phosphorus (174) + TX, clomiphene (alias) [CCN] + TX, butene phosphorus (1010) + TX , thiabendazole fungicide (1013) + TX, fruit insect phosphorus (1020) + TX, butafluorodecyl ester (CAS registration number: number 400882-07-7) + TX, cyhalothrin (196) + TX, tricyclotin (199)+TX, cypermethrin (201) TX, DCPM (1032)+TX, DDT(219)+TX, Tianle phosphorus (1037)+TX, Tianle phosphorus-O(1037)+TX , Tianle Phosphorus-S(1037)+TX, Zengsongsong (1038)+TX, methyl chlorhexidine (224)+TX, chlorhexidine-O(1038)+TX, methylisomethasone ( 224)+TX, Descendants-S(1038)+TX, Descendants-S-methyl (224)+TX, sputum phosphorus (1039)+TX, dibutyl ether urea (226)+TX, derla Pine (1042) + TX, Da Lisong (227) + TX, bacteriostatic (230) + TX, diclofen (236) + TX, di-propyl phosphine (alias) + TX, dicofol (242) + TX, hundred Treatment of phosphorus (243) + TX, dechlorination (1071) + TX, mefphosphate (1081), dassam (262) + TX, bisectin (alias) (653) + TX, decylphenol ( 1089)+TX, Dyna-Dikexin (1089)+TX, enemy 螨通(269)+TX, enemy 螨普(270)+TX, enemy 螨普-4[CCN]+TX, enemy 螨普- 6[CCN]+TX, neighboring enemy annihilation (1090)+TX, penemene ester (1092)+TX Octyl nitrate acaricides (1097) + TX, butyl nitrate (1098) + TX, two Phosphorus (1102) + TX, diphenyl hydrazine (IUPAC name) (1103) + TX, disulfiram (alias) [CCN] + TX, disulfoxide (278) + TX, DNOC (282) + TX, dofenapyn ( 1113) +TX, dermametine (alias) [CCN] + TX, endosulfan (294) + TX, toxic phosphorus (1121) + TX, EPN (297) + TX, eplenomycin ( Alias) [CCN]+TX, Aizusong (309)+TX, Yishen (1134)+TX, 螨(320)+TX, Yidusong(1142)+TX, anti-carbazole (1147) +TX, quinacridone (328)+TX, phenbutyltin (330)+TX, fenthiophene (337)+TX, fenpropathrin (342)+TX, pyridoxamine (alias)+TX, azole Decyl ester (345) + TX, decyl ester (1157) + TX, aryl fluoroamine (1161) + TX, fenvalerate (349) + TX, Fenpney (354) + TX, pyrimidine (360 +TX, fluzolone (1166) + TX, fluoroaniline thiazole (1167) + TX, fluoroquinone urea (366) + TX, cyfluthrin (367) + TX, fluorinated hydrazine (1169) + TX, flubendiamide (370) + TX, flumethrin (372) + TX, fluocyanine (1174) + TX, fluvalinate (1184) + TX, FMC 1137 (development code) (1185 ) +TX, worm (405) + TX, worm + (405) + TX, Fu Musong (1192) + TX, hyperthyroidism (1193) + TX, lindane (430) + TX, fruit Green Ding (1205)+TX, Hefening (424)+TX, Feidasong (432)+TX, Ten Alkylcyclopropanecarboxylate (IUPAC/Chemical Abstract Name) (1216) + TX, thiazolone (441) + TX, methyl iodide (IUPAC name) (542) + TX, acesulfame (alias) (473 +TX, isopropanol O-(methoxyaminothiophosphonium)salicylic acid (IUPAC name) (473)+TX, ivermectin (alias) [CCN]+TX, jasperate I (696)+TX, Jasmine II (696)+TX, iodophos (1248)+TX, chlorinated benzene (430)+TX, Lufenlong (490)+TX, marathon (492)+TX , special nitrile (1254) + TX, bismuth phosphorus (502) + TX, dithia phosphorus (1261) + TX, dimethyl thiazide (alias) [CCN] + TX, insect phobia (1266) + TX, Damason (527)+TX, dexamethasone (529)+TX, chlorpyrifos (530)+TX, methomyl (531)+TX, methyl bromide (537)+TX, acetonide (550)+TX, Meiwensong (556)+TX, Ziwei (1290)+TX, Mistidine (557)+TX, Milbymycin Telluride (alias)[CCN]+TX, propylamine fluoride (1293)+TX, Speeding (561)+TX, Maoguo (1300)+TX, Mosdatin (alias)[CCN]+TX, Nai Lisong (567)+TX, NC-184 (compound code)+TX, NC- 512 (compound code) + TX, Niflulily (1309) + TX, nicotimycin (alias) [CCN] + TX, pentamidine (1313) + TX, pentamidine 1:1 zinc chloride synthesis Object (1313)+ TX, NNI-0101 (compound code) + TX, NNI-0250 (compound code) + TX Oujiesong (594) + TX, killing line (602) + TX, isobaric (1324) + TX, mixing Phosphorus (1325) + TX, pp'-DDT (219) + TX, Barlason (615) + TX, permethrin (626) + TX, petroleum oil (alias) (628) + TX, fenthion ( 1330) +TX, Sedasson (631) + TX, Fresson (636) + TX, Yubisson (637) + TX, sulfur cyclophosphine (1338) + TX, Yisong (638) + TX, Fu Misesong (639) + TX, Bassson (642) + TX, Yatesson - methyl (652) + TX, polychlorinated terpenes (known name) (1347) + TX, polynacromycin ( Alias) (653) + TX, chlorinated alcohol (1350) + TX, Bufson (662) + TX, Converse (1354) + TX, Kruth (671) + TX, chlorpyrifos (673) + TX, chlorpyrifos (678) + TX, Blessing (1360) + TX, fruit (1362) + TX, pyrethrin I (696) + TX, pyrethrin II (696) + TX, Pyrethrin (696)+TX, Qiling (699)+TX, Bifendon (701)+TX, Pidifen (706)+TX, pyrimidine phosphorus (1370)+TX, Baiyusong (711) ) +TX, Bai Yusong (1381) + TX, R-1492 (development code) (1382) + TX, RA-17 (development code) (1383) + TX, rotenone (722) + TX, octadecyl ( 1389) +TX, sulphur phosphorus (alias) + TX, serracin (alias) [CCN ]+TX, SI-0009 (compound code) + TX, Suguo (1402) + TX, spiro-ester (738) + TX, spironolactone (739) + TX, SSI-121 (development code) (1404) +TX, Shufeilun (alias) [CCN]+TX, sulfluramid (750)+TX, guanidine phosphorus (753)+TX, sulfur (754)+TX, SZI-121 (development code) (757 +TX, fluvalinate (398) + TX, pyridoxamine (763) + TX, TEPP (1417) + TX, third Dingwei (alias) + TX, insecticidal (777) + TX, Tetrachlorine (786) + TX, four antibiotics (alias) (653) + TX, killing good (1425) + TX, thiophene (alias) + TX, insect-resistant (1431) + TX, long Weiwei (800)+TX, methyl disulfoxide (801)+TX, chlorpyrifos (1436)+TX, sulindac (alias)[CCN]+TX, bismamisone (1441)+TX, Benzoquinone (1443) + TX, trilopine (820) + TX, oxazide (alias) + TX, triclosan (824) + TX, phosphorus oxychloride (1455) + TX, three live bacteria (alias) (653)+TX, sylvestre (847)+TX, fenidazole [CCN] and YI-5302 (compound code)+TX, an algicide, from a group of substances consisting of Selected: Benzene [CCN]+TX, copper dioctoate (IUPAC name) (170)+TX, copper sulfate (172)+TX, thiobenzene [CCN]+TX, dichloronaphthylquinone (1052)+TX, dihydroxydichlorodiphenylmethane (232)+TX, cadmium (295)+TX, triphenyltin (347)+TX, slaked lime [CCN ]+TX, Dyson sodium (566)+TX, Mokgrass (714)+TX, indigoamine (1379)+TX, simazine (730)+TX, triphenyltin acetate (IUPAC name) 347) and triphenyltin hydroxide (IUPAC name) (347) + TX, an anthelmintic, selected from the group consisting of: abatatin (1) + TX, breeding livestock phosphorus (1011 ) +TX, dermathistine (alias) [CCN]+TX, indomethacin (291)+TX, gamma salt (291)+TX, eplenomycin (alias)[CCN]+TX , ivermectin (alias) [CCN]+TX, milbemycin oxime (alias) [CCN]+TX, mosstatin (alias) [CCN]+TX, piperazine [CCN]+TX, serramycin (alias) [CCN]+TX, spinosyn (737) and methyl thiophanate (1435)+TX, a bird killing agent, from a group of substances consisting of Selected: chloralose (127) + TX, endrin (1122) + TX, fumicide (346) + TX, pyridin-4-amine (IUPAC name) (23) and strychnine (745) +TX, a fungicide, is selected from the group consisting of 1-hydroxy-1 hydrogen-pyridine-2-thione (IUPAC name) (1222) + TX, 4-(quinoline Oxalin-2-amino)benzenesulfonamide (IUPAC name) (748)+TX, 8-hydroxyquinoline sulfate (446)+TX, bronopol (97)+TX, copper dioctoate (IUPAC name) (170)+TX, copper hydroxide (IUPAC name) (169)+TX, cresol [CCN]+TX, diclofen (232)+TX, dithiopyridinium (1105)+TX, and doxine ( 1112) +TX, dikesone (1144) + TX, formaldehyde (404) + TX, mercury plus fen (alias) [CCN] + TX, chunleimycin (483) + TX, chunleimycin hydrochloride hydrate ( 483) +TX, nickel dimethylaminodithioate (IUPAC name) (1308) + TX, nitropyridine (580) + TX, octyl isothiophenone (590) + TX, Quinoic acid (606)+TX, oxytetracycline (611)+TX, hydroxyquinoline potassium hydrogensulfate (446)+TX, thiabendazole (658)+TX, streptomycin (744)+TX, streptavidin Sulfate (744) + TX, gram gram (766) + TX and thimerosal (alias) [CCN] + TX, a biological preparation, selected from the group consisting of: cotton brown moth ( Adoxophyes orana GV) (alias) (12) + TX, Agrobacterium radiotypes ( Agrobacterium ra two obacter ) (alias) (13) + TX, blunt species ( Amblyseius Spp.) (alias) (19) + TX, celery night moth ( Anagrapha falcifera NPV) (alias) (28) + TX, pteridophyte Anagrus atomus ) (alias) (29) + TX, 苜蓿蚜 bee ( Aphelinus abdominalis ) (alias) (33) + TX, 蚜 Coleman ( Aphidius colemani ) (alias) (34) + TX, 蚜瘿 mosquito ( Aphidoletes aphidimyza ) (alias) (35) + TX, Spodoptera frugiperda ( Autographa californica NPV) (alias) (38) + TX, Bacillus lentus ( Bacillus firmus ) (alias) (48) + TX, Bacillus sphaericus ( Bacillus sphaericus Neide) (49)+TX, Bacillus thuringiensis ( Bacillus thuringiensis Berliner) (scientific name) (51) + TX, Su Li bacteria Bacillus thuringiensis Subsp. Aizawai ) (scientific name) (51) + TX, Bacillus thuringiensis subspecies of Israel ( Bacillus thuringiensis Subsp. Israelensis ) (scientific name) (51) + TX, Bacillus thuringiensis subsp. Bacillus thuringiensis Subsp. Japonensis ) (scientific name) (51) + TX, Bacillus thuringiensis Kurstaki subspecies( Bacillus thuringiensis Subsp. Kurstaki ) (scientific name) (51) + TX, Bacillus thuringiensis Tenebrionis subspecies( Bacillus thuringiensis Subsp. Tenebrionis ) (scientific name) (51) + TX, Beauveria bassiana ( Beauveria bassiana ) (alias) (53) + TX, Beauveria bassiana ( Beauveria brongniartii ) (alias) (54) + TX, ordinary grasshopper ( Chrysoperla carnea ) (alias) (151) + TX, Meng's hidden ladybug ( Cryptolaemus montrouzieri ) (alias) (178) + TX, apple stupid moth granulosis virus ( Cydia pomonella GV) (alias) (191) + TX, Siberian bee Dacnusa sibirica ) (alias) (212) + TX, peas Diglyphus isaea ) (alias) (254) + TX, Li Wei wasp ( Encarsia formosa ) (scientific name) (293) + TX, scorpion horned bee ( Eretmocerus eremicus ) (alias) (300) + TX, American cotton bollworm ( Helicoverpa zea NPV) (alias) (431) + TX, Heterodera Heterorhabditis bacteriophora )versus H.megidis (alias) (433) + TX, poly-legged ladybug ( Hippodamia convergens ) (alias) (442) + TX, parasitic tangerine powder scale insects ( Leptomastix dactylopii ) (alias) (488) + TX, predatory artifacts ( Macrolophus caliginosus ) (alias) (491) + TX, Cabbage Mamestra brassicae NPV) (alias) (494) + TX, Metaphycus helvolus (alias) (522)+TX, Metarhizium anisopliae ( Metarhizium anisopliae Var. Acridum ) (scientific name) (523) + TX, Metarhizium ( Metarhizium anisopliae Var. Anisopliae ) (scientific name) (523) + TX, European pine rust sawdust bee ( Neodiprion sertifer NPV) and red-headed pine bee ( N.lecontei NPV) (alias) (575) + TX, small flower species ( Orius Spp.) (alias) (596) + TX, Paecilomyces fuliginea ( Paecilomyces fumosoroseus ) (alias) (613) + TX, Chilean plantation 蟍 ( Phytoseiulus persimilis ) (alias) (644) + TX, Spodoptera exigua Multicapsid nuclear polyhedrosis virus (scientific name) (741) + TX, Steinernema bibionis (alias) (742) + TX, M. elegans ( Steinernema carpocapsae ) (alias) (742) + TX, Spodoptera frugiperda ( Steinernema feltiae ) (alias) (742) + TX, Steinernema glaseri (alias) (742) + TX, Steinernema riobrave (alias) (742) + TX, Steinernema riobravis (alias) (742) + TX, M. elegans ( Steinernema scapterisci ) (alias) (742) + TX, Streptomyces elegans ( Steinernema Spp.) (alias) (742) + TX, Trichogram bee ( Trichogramma Spp.) (alias) (826) + TX, Western blind walk ( Typhlodromus occidentalis ) (alias) (844) and Verticillium lecanii ( Verticillium lecanii (alias) (848) + TX, a soil sterilant, selected from the group consisting of methyl iodide (IUPAC name) (542) and methyl bromide (537) + TX, a chemical sterilant, Selected from a group consisting of: oxazophos [CCN]+TX, bis(aziridine)methylaminophosphorus sulfide (alias) [CCN]+TX, busulfan (alias) [CCN]+TX, diflubenzuron (250)+TX, dimatif ( Alias) [CCN]+TX, hexamethylene amide [CCN]+TX, hexamethylphosphorus [CCN]+TX, methyl hydrazine [CCN]+TX, methylthiocarbamate [CCN]+TX, methyl sterility [CCN]+TX, bisphosphonazoline [CCN]+TX, fluorojumolone (alias) [CCN]+TX, 涕ba[CCN]+TX, thiohexamethylphosphorus (alias)[CCN]+TX, stopper Substitute (alias) [CCN]+TX, infertility (alias) [CCN] and urethane imine (alias) [CCN]+TX, an insect pheromones, from a group of substances consisting of Selected: (E)-dec-5-en-1-yl acetate containing (E)-dec-5-en-1-ol (IUPAC name) (222) + TX, (E) - Thirteen-4- Alken-1-carboxylic acid (IUPAC name) (829) + TX, (E)-6-methyl-2-hepten-4-ol (IUPAC name) (541) + TX, (E, Z) - fourteen Alkane-4,10-diene-1-acetate (IUPAC name) (779) + TX, (Z)-dodecene-7-ol-1-acetate (IUPAC name) (285) + TX, (Z)-hexadecyl-11-enyl aldehyde (IUPAC name) (436) + TX, (Z)-hexadecen-11-ol-1-acetate (IUPAC name) (437) + TX, ( Z)-hexadec-13-en-11-yn-1-yl acetate (IUPAC name) (438)+TX, (Z)-icos-13-en-10-one (IUPAC name) (4 48) +TX, (Z)-tetradec-7-en-1-yl (IUPAC name) (782) + TX, (Z)-tetradec-9-en-1-ol (IUPAC name) ( 783) +TX, (Z)-tetradec-9-ene-1-acetate (IUPAC name) (784) + TX, (7E, 9Z)-dodecene-7,9-olol-1 - acetate (IUPAC name) (283) + TX, (9Z, 11E) - tetradecane-9,11-diene-1-acetate (IUPAC name) (780) + TX, (9Z, 12E )-tetradecane-9,12-diene-acetate (IUPAC name) (781)+TX, 14-methyloctadec-1-ene (IUPAC name) (545)+TX, 4- Methylnonan-5-one 4-methylnonan-5-ol (IUPAC name) (544) + TX, α-polymorph (alias) [CCN] + TX, brevicomin (alias) [CCN] + TX, codlelure (alias )[CCN]+TX, dodecadienol (alias) (167)+TX, melon fly attractant (alias) (179)+TX, female gypsy moth attractant (277)+TX, twelve Alkan-8-en-1-yl acetate (IUPAC name) (286) + TX, dodecane-9-en-1-yl acetate (IUPAC name) (287) + TX, dodecane - 8+TX, 10-dien-1-yl acetate (IUPAC name) (284)+TX, Stupid attractant No. 2 (alias) [CCN]+TX, ethyl 4-octanoic acid methyl ester (IUPAC name )(317)+TX, eugenol (alias) [CCN]+TX, southern pine scorpion attractant (alias) [CCN]+TX, cotton red bell Insect attractant (alias) (420) + TX, decoy olefin mixture (421) + TX, decoy olefin mixture I (alias) (421) + TX, decoy olefin mixture II (alias) (421) + TX , decoy olefin mixture III (alias) (421) + TX, decoy olefin mixture IV (alias) (421) + TX, red bell entangled [CCN] + TX, dentate decyl alcohol (alias) [CCN ]+TX, dentate decyl alcohol (alias) [CCN]+TX, scarab attractant (alias) (481)+TX, trimethyldioxytricyclodecane (alias) [CCN]+TX, night Moth attractant (alias) [CCN]+TX, lure moth (alias) [CCN]+TX, decoy ester [CCN]+TX, tetradecadienoic acid (alias) [CCN]+TX, insecticidal ether (alias) (540)+TX, Musca domestica attractant (563)+TX, octadecene-2,13-diene-1-acetic acid (IUPAC name) (588)+TX, octadecene-3,13 -Diene-1-acetic acid (IUPAC name) (589) + TX, Ovra Road (alias) [CCN] + TX, Oritas Road (alias) (317) + TX, tetradecenyl acetate (alias) [CCN]+TX, Mediterranean fruit fly attractant [CCN]+TX, soddine (alias) (736)+TX, bacteriocin (alias) [CCN]+TX, fourteen carbon- 11-ene-1-acetate (IUPAC name) (785)+TX, Mediterranean fruit fly attractant (839)+TX, Mediterranean fruit fly attractant A (alias) (839)+TX, Mediterranean Sex attractant B1 (alias) (839) + TX, Mediterranean fruit fly attractant B2 (alias) (839) + TX, Mediterranean fruit fly attractant C (alias) (839) and Chuangke (alias) [ CCN]+TX, an insect repellent, is selected from the group consisting of: insecticidal alcohol (IUPAC name) (591) + TX, butyl trimethylated oxygen (933) + TX, butoxy (Polypropylene glycol) (936) + TX, dibutyl adipate (IUPAC name) (1046) + TX, dibutyl phthalate (1047) + TX, dibutyl succinate (IUPAC name) (1048)+TX, di-ethyl stem toluidine amine [CCN]+TX, mosquito repellent [CCN]+TX, dimethyl phthalate [CCN]+TX, ethyl diol (1137)+TX, Diethylamine, ethidium, barbital [CCN] + TX, quinoline carboxylate (1276) + TX, methyl neodecylamine [CCN] + TX, oxalate [CCN] and picarein [CCN] ]+TX, an insecticide, is selected from the group consisting of 1-dichloro-1-nitroethane (IUPAC/Chemical Abstract Name) (1058)+TX, 1,1-II Chloro-2,2-bis(4-ethylphenyl)ethane (IUPAC name) (1056)+TX, 1,2-dichloropropane (IUPAC/Chemical Abstract Name) (1062)+TX, 1,2- Dichloropropane with 1,3-dichloropropene (IUPAC name) (1063) + TX, 1-bromo-2-chloro Alkane (IUPAC / Chemical Abstract Name) (916) + TX, 2,2,2-trichloro-1-(3,4-dichlorophenyl)acetate (IUPAC name) (1451) + TX, 2, 2-Dichlorovinyl dimethyl ester 2-ethylsulfinylethyl phosphate methyl ester (IUPAC name) (1066) + TX, 2-(1,3-dithiolan-2-yl)phenyl dimethylcarbamate (IUPAC / Chemical Abstract Name) (1109) + TX, 2-(2-butoxyethoxy)ethyl thiocyanate (IUPAC / Chemical Abstract Name) (935) + TX, 2- (4, 5 -dimethyl-1,3-dioxolan-2-yl)phenyl methylcarbamate (IUPAC/Chemical Abstract Name) (1084) + TX, 2-(4-amine-3,5-xylyleneoxy)ethanol (IUPAC name) ( 986) +TX, 2-chloroethylene diethyl phosphate (IUPAC name) (984) + TX, 2-imidazolidinone (IUPAC name) (1225) + TX, 2-isopentyl-1,3- Ketone (IUPAC name) (1246) + TX, 2-methyl (prop-2-ynyl) aminophenyl methylcarbamate (IUPAC name) (1284) + TX, 2-thiocyanatoethyl laurate (IUPAC name) (1433) + TX, 3-bromo 1-chloro-1-propene (IUPAC name) (917) + TX, 3-methyl-1-phenylpyrazol-5-yl dimethyl carbamate (IUPAC name) (1283) + TX, 4-methyl (prop-2- Alkyne) Amine-3,5-dimethylphenylaminocarbamate (IUPAC name) (1285)+TX, 5,5-dimethyl-3- Oxocyclohex-1-enyl dimethylcarbamate (IUPAC name) (1085) + TX, abatatin (1) + TX, chlorfenapyr (2) + TX, acetamiprid (4) + TX, housefly phosphorus (alias) [ CCN]+TX, acetaminophen [CCN]+TX, flumethrin (9)+TX, acrylonitrile (IUPAC name) (861)+TX, cotton ring (15)+TX, get gram (16 ) +TX, Oxygen (863) + TX, Aldrin (864) + TX, allylmethrin (17) + TX, alemsin (alias) [CCN] + TX, disinfection (866) + TX, á-cypermethrin (202) + TX, á-ecdysone (alias) [CCN] + TX, aluminum phosphide (640) + TX, match (870) + TX, guanamine thioester ( 872)+TX, chlorpyrifos (873)+TX, amine phosphorus (875)+TX, acid oxalate amine (875)+TX, amitraz (24)+TX, neonicotinoid (877) +TX, ethyl chlorpyrifos (883) + TX, AVI 382 (compound code) + TX, AZ60541 (compound code) + TX, azadirachtin (alias) (41) + TX, sub-desin (42) + TX , Ethyl tamarind (44) + TX, methyl tacrolimus (48) + TX, azo (889) + TX, Bacillus thuringiensis δ - endotoxin (alias) (52) +TX, bismuth fluoroantimonate (alias) [CCN]+TX, bismuth polysulfide (IUPAC/chemical abstract name) (892)+TX, pepper pyrethrum [CCN]+TX, Bayer 22/190 (development code) (893) + TX, Bayer 22408 (development code) (894) + TX, Insect (58)+TX, propylthiocarbamate (60)+TX, insecticidal sulfonate (66)+TX, â-cyfluthrin (194)+TX, beta-cypermethrin (203)+TX, bifenthrin (76) + TX, bio-methrin (78) + TX, propyl methrin S-cyclopentenyl isomer (alias) (79) + TX, bioethanomethrin [CCN] + TX, biological chlorine Pyrethroid (908) + TX, bio-insecticide (80) + TX, bis (2-chloroethyl) ether (IUPAC name) (909) + TX, bistrifluoroidazolium (83) + TX, borax ( 86) +TX, bromostat (alias) + TX, methyl bromide (914) + TX, bromo (918) + TX, bromine DDT (alias) [CCN] + TX, bromo pine (920)+TX, ethyl bromide (921)+TX, butylanilide (924)+TX, chlorpyrifos (99)+TX, butyl methacrylate (926)+TX, demethylated Pyrimidine phosphine (927)+TX, butanone (103)+TX, butyl phosphate (932)+TX, butanone oxime (104)+TX, butyldaprofen (alias)+TX, sulphur phosphorus (109) + TX, calcium arsenate [CCN] + TX, calcium cyanide (444) + TX, stone sulfur mixture (IUPAC name) (111) + TX, toxaphene (941) + TX, chlorpyrifos ( 943) +TX, carbaryl (115) + TX, carbofuran (118) + TX, carbon disulfide (IUPAC / chemical abstract name) (945) + TX, carbon tetrachloride (IUPAC name) (946) + TX ,three Phosphorus (947) + TX, butyl thiocarbazone (119) + TX, chlorpyrifos (123) + TX, chlorpyrifos hydrochloride (123) + TX, sivadine (alias) (725) + TX, Borneol Dan (960)+TX, Chlordane (128)+TX, Chlordecone (963)+TX, Insecticidal (964)+TX, Insecticidal Hydrochloride (964)+TX, Oxychloride Phosphorus (129)+TX, chlorfenapyr (130)+TX, kefensone (131)+TX, chlorfenapyr (132)+TX, chloromethylphosphonium (136)+TX, chloroform [CCN]+TX , Trichloronitromethane (141) + TX, chloronitrile phosphine (989) + TX, insecticidal pyridine (990) + TX, Dossson (145) + TX, methyl tausson (146) + TX, chloromethyl sulfide Phosphorus (994)+TX, Cyclosporin (150)+TX, fenvalerate I(696)+TX, methyrin II (696)+TX, fenvalerate (696)+TX, cis-resmethrin (alias) +TX, cismethrin (80) + TX, cyhalothrin (alias) + TX, in addition to line (999) + TX, cyanoguanidine (alias) [CCN] + TX, clothianidin (165 ) +TX, acetonitrile copper arsenate [CCN] + TX, copper arsenate [CCN] + TX, copper oleic acid [CCN] + TX, fly poison phosphorus (174) + TX, livestock phosphorus (1006) + TX, Cromiton (alias) [CCN]+TX, butene phosphorus (1010)+TX, breeding livestock phosphorus (1011)+TX, cryolite (alias) (177)+TX, CS 708 (development code) (1012)+TX, benzonitrile phosphorus (1019)+TX, acaricidal nitrile (18 4) +TX, fruit worm phosphorus (1020) + TX, ringworm chrysanthemum [CCN] + TX, fenpropathrin (188) + TX, cyfluthrin (193) + TX, cyhalothrin (196) + TX, cypermethrin (201) + TX, cyprofen (206) + TX, chlorfenapyr (209) + TX, chlorpyrifos (alias) [CCN] + TX, celery (alias) [CCN] +TX, dextromethrin (alias) (788) + TX, DAEP (1031) + TX, cotton (216) + TX, DDT (219) + TX, plus Bao Fu (1034) + TX, bromide Pyrethroid (223)+TX, Tianle Phosphorus (1037)+TX, Tianle Phosphorus-O(1037)+TX, Tianle Phosphorus-S(1037)+TX, Cecidate (1038)+TX, Methyl Dexamesone (224)+TX, Descendants-O(1038)+TX, methylisomethasone (224)+TX, chlorhexidine-S-methyl (1038)+TX, cecissin- S-methyl (224)+TX, sputum phosphorus (1039)+TX, dibutyl ether urea (226)+TX, derasson (1042)+TX, diamine phosphorus (1044)+TX, dansson (227 ) +TX, isothiophos (1050) + TX, dephosphorization (1051) + TX, diclofen (236) + TX, dipropyl phosphine (alias) + TX, dicresyl (alias) [CCN] + TX , Baizhi phosphorus (243) + TX, cyclosporin (244) + TX, dieldrin (1070) + TX, diethyl 5-methyl-3-pyrazole phosphate (IUPAC name) (1076) + TX, diflubenzuron (250) + TX, dihydroxypropyl theophylline (alias) [CCN] + TX, tetrafluoro Ethyl cholate [CCN] + TX, mefphosphate (1081) + TX, dime (1085) + TX, dass (262) + TX, fenthrin (1083) + TX, methyl kefensone (265)+TX, Diptera (1086)+TX, decylphenol (1089)+TX, Daina-Dikexin (1089)+TX, nitrophenol (1093)+TX, pentophenol (1094) ) +TX, dinol (1095) + TX, dinotefuran (271) + TX, benzophenone (1099) + TX, fruit and vegetable phosphorus (1100) + TX, dioxin (1101) + TX, two Phosphorus (1102)+TX, disulfiramone (278)+TX, desithrolide (1108)+TX, DNOC(282)+TX, dermametin (alias)[CCN]+TX, DSP(1115 ) +TX, ecdysterone (alias) [CCN] + TX, EI 1642 (development code) (1118) + TX, gamma salt (291) + TX, statin benzoate (291) + TX, EMPC(1120)+TX, dextromethrin (292)+ TX, endosulfan (294)+TX, toxic phosphorus (1121)+TX, endrin (1122)+TX, EPBP (1123) +TX, EPN(297)+TX, juvenile ether (1124)+TX, Epleno (alias) [CCN]+TX, S-fenvalerate (302)+TX, italabine (alias) [CCN]+TX, insecticidal (308)+TX, Aibo (309)+TX, ethiprole (310)+TX, dithizone (1134)+TX, Pfsson (312)+TX Ethyl formate (IUPAC name) [CCN]+TX, ethyl-DDD (alias) (1056)+TX, dibromoethylene (316)+TX, dichloroethane (chemical name) (1136)+TX, ring Oxyethane [CCN]+TX, etofenproxate (319)+TX, prednisone (1142)+TX, EXD(1143)+TX, sulfaphos (323)+TX, fentansone (326)+ TX, anti-carbazole (1147) + TX, picophos (1148) + TX, diethyl phenol methyl urethane (1149) + TX, fenfluramine (1150) + TX, chlorfen (335)+TX, Zhongdingwei (336)+TX, Fenofali (1153) +TX, phenoxycarb (340) + TX, beta-cypermethrin (1155) + TX, fenpropathrin (342) + TX, pyridoxamine (alias) + TX, Fanfusong (1158) + TX, fumicide (346)+TX, ethylfensonate [CCN]+TX, fenvalerate (349)+TX, fentanyl (354)+TX, fluramide (358)+TX, flubendivir Amine (CAS. Registration No.: 272451-65-7) + TX, flucofuron (1168) + TX, fluoroquinone urea (366) + TX, cyfluthrin (367) + TX, fluorinated hydrazine (1169) + TX , pyrimethanil [CCN] + TX, flubendiamide (370) + TX, trimethrin (1171) + TX, flumethrin (372) + TX, fluvalinate (1184) + TX, FMC 1137 (development code) (1185) + TX, Dafusong (1191) + TX, worm (405) + TX, worms (405) + TX, Fu Musong (1192) + TX, formazan (1193) + TX, butyl thiophene (1194) + TX, formazin (1195) + TX, forsythia (408) + TX, selebrane (1196) + TX, furosemide ( 412) +TX, furfural (1200) + TX, super efficient cyhalothrin (197) + TX, lindane (430) + TX, biguanide salt (422) + TX, biguanide acetate (422) + TX, GY-81 (development code) (423) + TX, fenfenine (424) + TX, chlorantranil (425) + TX, HCH (430) + TX, HEOD (1070) + TX, heptachlor (1211 ) +TX, Feidasong (432) +TX, chlorpyrifos [CCN]+TX, hexaflumuron (439)+TX, HHDN(864)+TX, fluoroantimony (443)+TX, hydrogen cyanide (444)+TX, enebene B Ester (445) + TX, hyquincarb (1223) + TX, idadine (458) + TX, methadin (460) + TX, indoxacarb (465) + TX, methyl iodide (IUPAC name) (542 ) +TX, IPSP (1229) + TX, chlorpyrifos (1231) + TX, carbochlorin (1232) + TX, acesulfame (alias) (473) + TX, isoprene (1235) + TX, Isophosphorus (1236)+TX, Ilan (1237)+TX, chlorhexidine (472)+TX, isopropanol O-(methoxyaminothiophosphonium)salicylate (IUPAC) Name) (473)+TX, Indigo (474)+TX, Heterophosphorus (1244)+TX, Jiafusong (480)+TX, Ivermectin (alias) [CCN]+TX, Jasmine I(696)+TX, jasperate II (696)+TX, iodophos (1248)+TX, juvenile hormone I (alias)[CCN]+TX, juvenile hormone II (alias)[CCN]+ TX, juvenile hormone III (alias) [CCN]+TX, Klevan (1249)+TX, protosan (484)+TX, lambda-cyhalothrin (198)+TX, lead arsenate [CCN]+TX, lepimectin(CCN)+TX, p-bromophosphorus (1250)+TX, chlorinated benzene (430)+TX, lirimfos(1251)+TX, Lufenlong(490)+TX, Fusai Absolutely (1253)+TX, m Methyl cumylaminocarbamate (IUPAC name) (1014) + TX, magnesium phosphide (IUPAC name) (640) + TX, marathon (492) + TX, terpene nitrile (1254) + TX, azide Phosphorus (1255)+TX, chlorpyrifos (502)+TX, methyl acaricidal (1258)+TX, chlorpyrifos (1260)+TX, dithiaphos (1261)+TX, mercuric chloride ( 513) +TX, mesulfenfos (1263) + TX, cyanofluorfen (CCN) + TX, Weibaimu (519) + TX, metam-potassium (alias) (519) + TX, Wei is mu (519) + TX, worms (1266) + TX, damasson (527) + TX, methotrexate fluoride (IUPAC / chemical abstract name) (1268) + TX, dexamethasone (529) + TX, insecticide (530 +TX, insecticidal ethylene phosphorus (1273) + TX, chlordane (531) + TX, methoprene (532) + TX, quinoline carboxylate (1276) + TX, pyrethrin (alias) ( 533) +TX, methoxychlor (534) + TX, methoxy worm (535) + TX, methyl bromide (537) + TX, methyl isothiocyanate (543) + TX, trichloroethane (alias )[CCN]+TX, dichloromethane [CCN]+TX, trimethoprim [CCN]+TX, quick kill (550)+TX, Insectone (1288)+TX, Meiwensong (556)+TX, self-kewei (1290)+TX, chlorhexidine (557)+TX, milbemycin oxime (alias)[CCN]+TX, propylamine fluoride (1293)+TX, anthill (1294)+TX, yawrin (561)+TX, Maoguo (1300)+TX, mosstatin (alias)[CCN]+TX, naphthoquinone phosphorus (alias )[CCN]+TX, Nai Lisong (567)+TX, naphthalene (IUPAC/Chemical Abstract Name) (1303)+TX, NC-170 (development code) (1306)+TX, NC-184 (compound code) +TX, nicotine (578) + TX, nicotine sulfate (578) + TX, nifluli (1309) + TX, nitenpyram (579) + TX, thiazide (1311)+TX, pentanyl (1313)+TX, pentanyl 1:1 zinc chloride complex (1313)+TX, NNI-0101 (compound code)+TX, NNI-0250 (compound code)+ TX, nornicotine (known name) (1319) + TX, diphenylfluorourea (585) + TX, polyfluoro urea (586) + TX, O -5-dichloro-4-indophenol- O -ethyl phosphorothioate (IUPAC name) (1057) + TX, O, O -diethyl O -4-methyl-2-oxo-2 H -chromen-7-yl phosphorothioate (IUPAC name) (1074) + TX, O, O -diethyl O -6-methyl-2-propylpyrimidin-4-yl phosphorothioate (IUPAC name) (1075) + TX, O, O, O ', O '-Tetrapropyl dithio pyrophosphate (IUPAC name) (1424) + TX, oleic acid (IUPAC name) (593) + TX, eugenium (594) + TX, kill line (602) + TX , edrosone (609)+TX, acetonide (1324)+TX, phloem (1325)+TX, pp'-DDT(219)+TX, p-dichlorobenzene [CCN]+TX, balason (615) + TX, methyl-balazon (616) + TX, fluoro-urea (alias) [CCN] + TX, pentachlorophenol (623) + TX, pentachlorophenyl laurate (IUPAC name) ( 623) +TX, permethrin (626) + TX, petroleum oil (alias) (628) + TX, PH 60-38 (development code) (1328) + TX, fenthion (1330) + TX, phenyl ether Pyrethroid (630)+TX, Sedasson (631)+TX, Fresson (636)+TX, Yubisson (637)+TX, sulfur cyclophosphine (1338)+TX, Yisongsong (638)+ TX, p-chlorosulfate (1339) + TX, bismamisone (639) + TX, phosphine (IUPAC name) (640) + TX, Paceson (642) + TX, methyl bassason (1340 ) +TX, pirimetaphos (1344) + TX, anti-River (651) + TX, ethyl pyrimidine (1345) + TX, atesson-methyl (652) + TX, polychlorodicyclopentadiene isomers (IUPAC name) (1346 +TX, polychlorinated terpenes (known name) (1347) + TX, potassium arsenite [CCN] + TX, potassium thiocyanate [CCN] + TX, acetyl methionine (655) + TX, Mature I (alias) [CCN]+TX, presenilin II (alias) [CCN]+TX, presenilin III (alias) [CCN]+TX, primidophos (1349)+TX, Bufeisong (662)+TX , fenfluthrin [CCN] + TX, Converse (1354) + TX, chlorpyrifos (1355) + TX, chlorpyrifos (1356) + TX, methionem (673) + TX, propoxur ( 678) +TX, Bifford (1360) + TX, propionate (686) + TX, hair (1362) + TX, protrifenbute [CCN] + TX, pymetrozine (688) + TX, Bai Kesong ( 689)+TX, fixed bacteria phosphorus (693)+TX, pyresmethrin (1367)+TX, pyrethrin I (696)+TX, pyrethrin II (696)+TX, pyrethrin (696) +TX, 哒螨灵(699)+TX, dichloropropene (700)+TX, bifensone (701)+TX, piroxicam (706)+TX, pyrimidine phosphorus (1370)+TX, pyriproxyfen (708)+TX, Bitterwood (alias)[CCN]+TX, Baiyusong (711)+TX, Baiyusong-Methyl (1376)+TX, quinothion(1380)+TX, Baiyusong (1381) + TX, R-1492 (development code) (1382) + TX, Rafanet (alias) [CCN] + TX, fenfenyl (719) + TX, rotenone (722) + TX, RU 15525 (development code) (723) + TX, RU 25475 (development code) (1386) + TX, fish nitin (alias) (1387) + TX, L'Alan (known name) (1387) + TX, Sabah gourd (alias) (725)+TX, octaphosphorus (1389)+TX, sulphur phosphorus (alias)+TX, serramycin (alias)[CCN]+TX, SI-0009 (compound code)+TX, SI-0205 ( Compound code) + TX, SI-0404 (compound code) + TX, SI-0405 (compound code) + TX, flumethrin (728) + TX, SN 72129 (development code) (1397) + TX, arsenic Sodium [CCN] + TX, sodium cyanide (444) + TX, sodium fluoride (IUPAC / chemical abstract name) (1399) + TX, sodium hexafluoroantimonate (1400) + TX, sodium pentachlorophenol ( 623) + TX, sodium selenate (IUPAC name) (1401) + TX, sodium thiocyanate [CCN] + TX, Suguo (1402) + TX, spinosyn (737) + TX, mollusc methyl ester (739)+TX, molluscicidal ethyl ester (CCN)+TX, sulcofuron(746)+TX, sulcofuron-sodium(746)+TX, flubendiamide (750)+TX, guanidine phosphorus (753)+TX , sulphur fluoride (756) + TX, thiopropyl phosphorus (1408) + TX, tar (alias) (758) + TX, fluvalinate (398) + TX, thiazide (1412) + TX, TDE (1414) + TX, Defeno (762) + TX, pyridoxamine (763) + TX, Tebson (764) + TX, Fumaron (768) + TX, tefluthrin (769) + TX, Apexon (770) + TX, TEPP (1417) + TX, cyclopentimeryl (1418) + TX, third butyl (alias) + TX, tofosson (773) + TX, tetrachloro Ethane [CC N]+TX, insecticidal (777)+TX, methrin (787)+TX, high-efficiency transcypermethrin (204)+TX, thiacloprid (791)+TX, thiophene (alias)+TX Bug (792)+TX, thicrofos (1428)+TX, insect-resistant (1431)+TX, insecticidal ring (798)+TX, thiophanate (798)+TX, thiodicarb (799)+TX, long Weiwei (800)+TX, methyl disulfoxide (801)+TX, sulfur (1434) + TX, thiosultap (803) + TX, thiosultap-sodium (803) + TX, sulindac (alias) [CCN] + TX, oxazolamide (809) + TX, tetramethrin ( 812) +TX, tetrafluthrin (813) + TX, transpermethrin (1440) + TX, fetamethasone (1441) + TX, oxazolidine (818) + TX, triple-loose (820) + TX, Oxime (alias) + TX, triclosan (824) + TX, trichlormetaphos-3 (alias) [CCN] + TX, soil phosphorus (1452) + TX, phosphorus oxychloride (1455) + TX, Killing chlorinated urea (835) + TX, chlorpyrifos (840) + TX, enedisulfonyl ester (1459) + TX, sylvestris (847) + TX, fenidazole [CCN] + TX, cucurbitine (alias (725)+TX, cucurbitine (alias) (725)+TX, XMC(853)+TX, chlorpyrifos (854)+TX, YI-5302 (compound code)+TX, Z-cypermethrin 205) +TX, zetamethrin (alias) + TX, zinc phosphide (640) + TX, zolaprofos (1469) and ZXI 8901 (development code) (858) + TX, cyanamide [736994-63-19] + TX, chlorantamine [500008-45-7] + TX, cyenopyrafen [560121-52-0] + TX, butylated fluoro ester [400882-07-7] + TX, pyrifluquinazon [337458-27-2] + TX, Cinot [187166-40-1+187166-15-0]+TX, molluscicidal ethyl ester [203313-25-1]+TX, fluramide nitrile [946578-00-3]+TX , butenphene [704886-18-0] + TX, fenfluthrin [915288-13-0] + TX, tetrafluthrin [84937-88-2] + TX, a mollusc The agent is selected from the group consisting of: Ding Woxi (IUPAC name) (913) + TX, bromoacetamide [CCN] + TX, calcium arsenate [CCN] + TX, in addition to line ( 999)+TX, acetonitrile copper arsenate [CCN]+TX, copper sulfate (172)+TX, triphenyltin (347)+TX, iron phosphate (IUPAC name) (352)+TX, tetraacetaldehyde (518) + TX, chlorfenapyr (530) + TX, niclosamide (576) + TX, Nike mollusk ethanolamine salt (576) + TX, pentachlorophenol (623) + TX, sodium pentachlorophenol ( 623) +TX, thiazide (1412) + TX, thiodicarb (799) + TX, tributyltin oxide (913) + TX, snail mollusc net (1454) + TX, mixed killing (840) +TX, triphenyltin acetate (IUPAC name) (347) and triphenyltin hydroxide (IUPAC name) (347) + TX, pyriprol [394730-71-3] + TX, a nematicide, is from Selected from the following group of substances: AKD-3088 (compound code) + TX, 1,2-dibromo-3-chloropropane (IUPAC / chemical abstract name) (1045) + TX, 1,2-dichloro Propane (IUPAC / Chemical Abstract Name) (1062) + TX, 1,2-dichloropropane contains 1,3-two Propylene (IUPAC name) (1063) + TX, 1,3-dichloropropene (233) + TX, 3,4-dichlorotetrahydrothiophene 1, 1-dioxide (IUPAC / chemical abstract name) (1065) + TX, 3- ( 4-chlorophenyl)-5-methylrhodanin (IUPAC name) (980)+TX, 5-methyl-6-thioxo-1,3,5-thiadiazinan-3-ylacetic acid (IUPAC name) (1286)+ TX, 6-isopentenylaminopurine (alias) (210)+TX, abatatin (1)+TX, acetaminophen [CCN]+TX, cotton bollworm (15)+TX, derkeke ( 16) +TX, Oxygen (863) + TX, AZ 60541 (compound code) + TX, benclothiaz [CCN] + TX, benomyl (62) + TX, butyl daprofen (alias) + TX , sulphur phosphorus (109) + TX, carbofuran (118) + TX, carbon disulfide (945) + TX, butyl thiocarbazone (119) + TX, trichloronitromethane (141) + TX, Taosson ( 145) +TX, in addition to line (999) + TX, cytokinin (alias) (210) + TX, cotton (216) + TX, DBCP (1045) + TX, DCIP (218) + TX, diamine Phosphorus (1044)+TX, dephosphorization (1051)+TX, dipropylphosphine (alias)+TX, Dasongsong (262)+TX, dermametin (alias)[CCN]+TX, Avi Salt (291)+TX, Incomgent benzoate (291)+TX, Eplenomycin (alias) [CCN]+TX, Pfsson (312)+TX, Dibromoethylene (316) +TX, fentansone (326) + TX, pyridoxamine (alias) + TX, Fanfusong (1158) + TX, Fusai (408) + TX, scutellaria (1196) + TX, furfural (alias )[CCN]+TX, GY-81(development code)(423)+TX, chlorpyrifos [CCN]+TX, iodomethane (IUPAC name) (542)+TX, isamidofos(1230)+TX, Killing pine (1231) + TX, ivermectin (alias) [CCN] + TX, furan methyl adenine (alias) (210) + TX, methyl quinone phosphorus (1258) + TX, Weibaimu ( 519) +TX, metam-potassium (alias) (519) + TX, Wei is mu (519) + TX, methyl bromide (537) + TX, methyl isothiocyanate (543) + TX, mirabimycin Compound (alias) [CCN]+TX, Mustardin (alias) [CCN]+TX, Myrothecium verrucaria composition (alias) (565)+TX, NC-184 ( Compound code) +TX, kill line (602) + TX, Fresson (636) + TX, Fetish miso (639) + TX, Fusika [CCN] + TX, sulfur phosphorus (alias) + TX, Serramycin (alias) [CCN]+TX, spinosyn (737)+TX, third butyl (alias)+TX, tofusone (773)+TX, tetrachlorothiophene (IUPAC/chemical abstract name) 1422) +TX, thiophene (alias) + TX, thiophosphorus (1434)+TX, three-loose (820)+TX, oxazide (alias)+TX, xylenol [CCN]+TX, YI-5302 (compound code) and zeatin (alias) (210)+ TX, flensulfone [318290-98-1]+TX, nitrification inhibitor, is selected from the group consisting of potassium ethyl xanthate [CCN] and nitropyridine (580) + TX, a plant The activator is selected from the group consisting of: axibella (6) + TX, arsenic benzene-S-methyl (6) + TX, thiabendazole (658) and knotweed ( Reynoutria sachalinensis Extract (alias) (720) + TX, a rodenticide, is selected from the group consisting of 2-isoamyl-1,3-indanedione (IUPAC name) (1246) +TX, 4-(quin Oxalin-2-amino) benzenesulfonamide (IUPAC name) (748) + TX, alpha-chlorohydrin [CCN] + TX, aluminum phosphide (640) + TX, ant (880) + TX, arsenic trioxide (882) +TX, cesium carbonate (891) + TX, double mouse urea (912) + TX, Dalong (89) + TX, bromadiolone (91) + TX, bromine murine (92) + TX, calcium cyanide ( 444) +TX, chloralose (127) + TX, chlorflumente (140) + TX, vitamin D3 (alias) (850) + TX, chlortetracycline (1004) + TX, gram-killing mouse (1005) +TX, rodent killer (175) + TX, rat death (1009) + TX, mouse gram (246) + TX, timolone (249) + TX, enemy mouse (273) + TX, calcified alcohol ( 301) +TX, flurazepam (357) + TX, fluridamide (379) + TX, flurazepam (1183) + TX, flupropadine hydrochloride (1183) + TX, lindane (430) + TX, HCH ( 430) +TX, hydrogen cyanide (444) + TX, methyl iodide (IUPAC name) (542) + TX, chlorinated benzene (430) + TX, magnesium phosphide (IUPAC name) (640) + TX, methyl bromide (537)+TX, murine Trane (1318)+TX, tetramine (1336)+TX, phosphine (IUPAC name) (640)+TX, phosphorus [CCN]+TX, murmurone (1341) +TX, potassium arsenite [CCN]+TX, rodent control (1371)+TX, red squid (1390)+TX, sodium arsenite [CCN]+TX, sodium cyanide (444)+TX, Sodium fluoroacetate (735) + TX, horse Subbase (745) + TX, barium sulfate [CCN] + TX, warfarin (851) and zinc phosphide (640) + TX, a synergist, is selected from the group consisting of: 2 -(2-butoxyethoxy)ethyl piperonylate (IUPAC name) (934)+TX, 5-(1,3-benzodioxol-5-yl)-3-hexylcyclohex-2-enone (IUPAC name) (903)+TX, gold Acacia and Neroli third alcohol (alias) (324) + TX, MB-599 (development code) (498) + TX, MGK 264 (development code) (296) + TX, sunflower butanol (649) + TX, synergistic aldehyde (1343) + TX, propyl isomer (1358) + TX, S421 (development code) (724) + TX, synergistic chrysanthemum (1393) + TX, sesame oil (1394) and Aachen (1406) + TX, a veterinary repellent, is selected from the group consisting of 蒽醌(32)+TX, chloralose (127)+TX, copper naphthenate [CCN]+ TX, copper oxychloride (171) + TX, dansson (227) + TX, dicyclopentadiene (chemical name) (1069) + TX, biguanide salt (422) + TX, biguanide acetate (422) + TX, chlorfenapyr (530) + TX, pyridin-4-amine (IUPAC name) (23) + TX, thiram (804) + TX, chlorpyrifos (840) + TX, zinc naphthenate [CCN] And dimethylamine zincate (856) + TX, a viricide, is from Manan (alias) [CCN] and A wound protectant selected from the group consisting of oxazolyl (alias) [CCN]+TX is selected from the group consisting of oxidized mercury (512) + TX and octyl isothiophenone (590). And thiophanate-methyl (802) + TX, and biologically active compounds, are selected from the group consisting of: Nitroconazole (60207-31-0) + TX, dibenzotriazole alcohol [70585] -36-3]+TX, carbendazole [116255-48-2]+TX, cyproconazole [94361-06-5]+TX, Etherazole [119446-68-3]+TX, diniconazole [83657-24-3]+TX, epoxiconazole [106325-08-0]+TX, nitrile azole [114369-43-6]+TX Fluoroquinazole [136426-54-5]+TX, flucarbazole [85509-19-9]+TX, fluconazole [76674-21-0]+TX, hexaconazole [79983-71-4] +TX, imazalil [35554-44-0]+TX, imidazole [86598-92-7]+TX, inocastazole [125225-28-7]+TX, mexazole [125116-23-6 ]+TX, myclobutanil [88671-89-0]+TX, rice glutamate [101903-30-4]+TX, penconazole [66246-88-6]+TX, prothioconazole [178928- 70-6]+TX, pyridine plaque [88283-41-4]+TX, prochloraz [67747-09-5]+TX, propiconazole [60207-90-1]+TX, guanidazole [ 149508-90-7]+TX, tebuconazole [107534-96-3]+TX, tetrafluoroetherazole [112281-77-3]+TX, triazolone [43121-43-3]+TX, three Oxazol [55219-65-3]+TX, fluconazole [99387-89-0]+TX, sterilized azole [131983-72-7]+TX, cyprodinol [12771-68-5]+TX , chloropyrimidinol [60168-88-9]+TX, fluoropyrimidinol [63284-71-9]+TX, acetaminophen sulfonate [41483-43-6]+TX, dipyridamole [ 5221-53-4]+TX, acetaminophen [23947-60-6]+TX, carbendazim [1593-77-7]+TX, fenpropidin [67306-00-7]+TX, butylbenzene Morpholine [67564-91-4]+TX, soft body Cyclosporin [118134-30-8]+TX, tridemorpholine [81412-43-3]+TX, cyprodinil [121552-61-2]+TX, azoxystrobin [110235-47- 7]+TX, pyrimethanil [53112-28-0]+TX, seed dressing [74738-17-3]+TX, fluke nitrile [131341-86-1]+TX, benzophene [71626- 11-4]+TX, furosemide [57646-30-7]+TX, metalaxyl [57837-19-1]+TX, R metalaxyl [70630-17-0]+TX, furosemide [58810-48-3]+TX, 霜灵[77732-09-3]+TX, benomyl [17804-35-2]+TX, carbendazim [10605-21-7]+TX, imiprozil [62732-91-6]+TX , Mai Suining [3878-19-1]+TX, thiabendazole [148-79-8]+TX, ethyl bacillus [84332-86-5]+TX, sclerotia [24201-58-9] +TX, iprodione [36734-19-7]+TX, myclozoline[54864-61-8]+TX, procymidone [32809-16-8]+TX, vinyl nucleus [50471-44-8 ] +TX, pyridine amide [188425-85-6] + TX, rust rust [5234-68-4] + TX, mezylamine [24691-80-3] + TX, Fudonin [66332] -96-5]+TX, rust-eliminating amine [55814-41-0]+TX, oxidized rust rust [5259-88-1]+TX, pirfenidazole [183675-82-3]+TX, thiophene Furosemide [130000-40-7]+TX, biguanide salt [108173-90-6]+TX, Duoguoding [2439-10-3][112-65-2](free base)+TX, biguanide Octamine [13516-27-3] + TX, azoxystrobin [131860-33-8] + TX, ether myramine [149961-52-4] + TX, enestrobin {Proc. BCPC, Int. Congr .,Glasgow,2003,1,93}+TX, fluoxastrobin [361377-29-9]+TX, oxystrobin [143390-89-0]+TX, phenoxystrobin [133408-50-1 ] +TX, trifloxystrobin [141517-21-7] + TX, orysastrobin [248593-16-0] + TX, picoxystrobin [117428-22-5] + TX, pyraclostrobin [175013- 18-0]+TX, Fami Iron [14484-64-1]+TX, Mancozeb [8018-01-7]+TX, Mansen Manganese [12427-38-2]+TX, Daisenlian [9006-42-2]+TX , Bensen zinc [12071-83-9] + TX, Fumei double [137-26-8] + TX, Daisen zinc [12122-67-7] + TX, dimethyl amine zinc hydride [137-30- 4]+TX, dichlorpyrifos [2425-06-1]+TX, captan[133-06-2]+TX, bacteriostatic [1085-98-9]+TX, chlorochlorin nuclear [ 41205-21-4]+TX, sterilized Dan [133-07-3]+TX, toluene sulfonamide [731-27-1]+TX, Bordeaux mixture [8011-63-0]+TX, copper hydroxide [ 20427-59-2]+TX, copperoxychlorid[1332-40-7]+TX, coppersulfat[7758-98-7]+TX, copperoxid[1317-39-1]+TX, mancozeb [53988-93] -5]+TX, quinoline copper [10380-28-6]+TX, enemies [131-72-6]+TX, trifloxystrobin [10552-74-6]+TX, enemies phosphorus [17109] -49-8]+TX, 瘟 瘟 [ [26087-47-8]+TX, 瘟 瘟 [50512-35-1]+TX, chlorpyrifos [36519-00-3]+TX, bacterium Phosphorus [13457-18-6]+TX, methyl chlorpyrifos [57018-04-9]+TX, arsenic acid benzene-S-methyl [135158-54-2]+TX, carbendazim [101] -05-3]+TX, benthiavalicarb[413615-35-7]+TX, ash sputum [2079-00-7]+TX, sputum sputum [2439-01-2]+TX, chloroanisole [ 2675-77-6]+TX, bacteria [1897-45-6]+TX, cycloflufenamide [180409-60-3]+TX, cymoxanil [57966-95-7]+TX, dichloronaphthylquinone [117-80-6]+TX ,dicocymet[139920-32-4]+TX, chlorfenone [62865-36-5]+TX, chloramine [99-30-9]+TX, carbendazim [87130-20-9]+TX , olefin morpholine [110488-70-5] + TX, SYP LI90 (fluoromorpholine) [211867-47-9] + TX, dicyanoquinone [3347-22-6] + TX, thiazolam [ 162650-77-3]+TX, soil fungus [2593-15-9]+TX, Izamidone [131807-57-3]+TX, fenamidone [161326-34-7]+TX, cyanamide [115852-48-7]+TX, triphenyltin [668-34-8]+ TX, Azoxystrobin [89269-64-7]+TX, fluazinam [79622-59-6]+TX, fluroxypyramine [239110-15-7]+TX, sulfamethamine [106917-52-6 ]+TX, fenhexamid[126833-17-8]+TX, aluminum triethylphosphonate [39148-24-8]+TX, Mold [10004-44-1]+TX, 缬Mulberry [140923-17-7]+TX, IKF 916 (cyanosin) [120116-88-3]+TX, chunleimycin [6980-18- 3]+TX, sulfonamide [66952-49-6]+TX, metrafenone[220899-03-6]+TX, pentosan[66063-05-6]+TX, tetrachlorobenzoquinone [27355-22 -2]+TX, polyoxin [11113-80-7]+TX, thiabendazole [27605-76-1]+TX, downy mildew [25606-41-1]+TX, proquinazid[189278- 12-4]+TX, praziquantel [57369-32-1]+TX, quinoxaline [124495-18-7]+TX, pentachloronitrobenzene [82-68-8]+TX, sulfur [ 7704-34-9]+TX, tiadinil[223580-51-6]+TX, imidazole [72459-58-6]+TX, tricyclazole [41814-78-2]+TX, Amine [26644-46-2]+TX, Jinggangmycin[37248-47-8]+TX, guanosamine (RH7281)[156052-68-5]+TX, diacetylergicillin [374726-62 -2]+TX, isopyrazam[881685-58-1]+TX, sedaxane[874967-67-6]+TX, 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid(9-dichloromethylene-1 , 2,3,4-tetrahydro-1,4-methano-napht halen-5-yl)-amide (disclosed in WO 2007/048556) + TX, 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic Acid[2-(2,4-dichlorophenyl)-2-methoxy-1-methyl-ethyl]-amide (disclosed in WO 2008/148570) + TX, 1-[4-[4-[(5S)5-( 2,6-difluorophenyl)-4,5-dihydro-1,2-oxazol- 3-yl]-1,3-thiazol-2-yl]piperidin-1-yl]-2-[5-methyl-3- (trifluo romethyl)-1H-pyrazol-1-yl]ethanone+TX, 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-1,2-oxazol-3- Yl]-1,3-thiazol-2-yl]piperidin-1-yl]-2-[5-methyl-3-(trifluorom ethyl)-1H-pyrazol-1-yl]ethanone[1003318-67-9] (both are disclosed in WO 2010/123791, WO 2008/013925, WO 2008/013622 and WO 2011/051243, page 20) + TX, and 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid ( 3',4',5'-trifluoro-biphenyl-2-yl) -amide (disclosed in WO 2006/087343) + TX, S)-[3-(4-chloro-2-fluorophenyl)-5-(2,4-difluorophenyl)-iso Zin-4-yl]-pyridin-3-ylmethanol+TX, 3-(4-chloro-2-fluorophenyl)-5-(2,4-difluorophenyl)-iso Zin-4-yl]-pyridin-3-ylmethanol+TX and 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (3',4',5'-pentafluoro Benz-2-yl)-guanamine (disclosed in WO 2006/087343) + TX, 3-(difluoromethyl)-N-methoxy-1-methyl-N-[1-methyl-2- The mixture of (2,4,6-trichlorophenyl)ethyl]-1H-pyrazole-4-carboxamide + TX, TX may also be in the form of an ester or a salt, such as "The Pesticide Manual" (Insecticide Manual, 12th Edition, 2000 (BCPC)).
在上列各種要與TX混合的活性成分中,式I之化合物較佳為表1到12、A、B、C與D的化合物;更佳且甚至更佳的是,選自表1到12、A和B的化合物;化合物TX選自表A,或化合物TX選自表B,或化合物TX選自表C,或化合物TX選自表D,且最佳的是化合物TX選自A1、 A3、A4、A5、A6、A8、A9、A10、A11、A13、A15、A16、A17、A22、A23、A25、A28、A30、A31、A32、A33至A36、A38至A40、A45至A51、A76、A56、A59、A77、A80、A82、A84、A85、A86、A87、A90、A91、A93、A94、A99、A101、A104、A105、A106、A111、A112、A115、A120、A122、A124、A126、A128、A129、A131、A132、133、A134、A135、A136、A137、A138、A143、A144、A145、B1、B2、B3、B4、B5、B6、B7、B8、B9和B10,或化合物TX選自A1、A2、A3、A4、A5、A8、A9、A10、A11、A13、A14、A15、A16、A17、A19、A20、A22、A23、A25、A30、A31、A32、A33、A34、A36、A37、A38、A39、A40、A41、A42、A45、A46、A47、A48、A49、A50、A51、A76、A56、A57、A59、A61、A65、A68、A69、A72、A82、A86、A90、A101、A112、A115、A126、A128、A129、A130、A131、A132、133、A134、A135、A136、A137、A138、A139、A140、A142、A143、A144、A145、A146、A147、A149、A151、A157、A158、A159、A167、A168、A178、A180、A181、A182、A183、A184、A186、A187、A188、A189、A190、A192、A195、A196、A197、A198、A199、B1、B2、B3、B4、B5、B6、B7、B8、B9和B10,或化合物TX選自A1、A3、A4、A5、A6、A10、A12、A13、A15、A22、A23、A25、A28、A31、A32、A33、A34、A35、A36、A38、A39、A40、A41、A42、A45、A46、A48、A49、A50、A51、A76、A56、A57、A59、A61、A79、A80、A83、A84、A86、A87、A90、A91、 A93、A94、A95、A104、A106、A111、A112、A123、A126、A128、A129、A130、A131、A132、133、A134、A135、A136、A137、A138、A142、A143、A144、A145、A146、A151、A157、A159、A163、A168、A178、A181、A182、A183、A184、A188、A189、A192、A195、A197、A199、B1、B2、B3、B4、B5、B6、B7、B8、B9和B10,或化合物TX選自A1、A2、A3、A4、A5、A6、A10、A11、A12、A23、A30、A32、A33、A34、A35、A38、A39、A40、A42、A45、A46、A48、A49、A51、A76、A56、A57、A59、A61、A65、A68、A69、A80、A81、A82、A84、A87、A93、A101、A106、A109、A112、A115、A124、A126、A128、A129、A131、A132、133、A134、A135、A136、A137、A138、A143、A144、A145、A146、A151、A157、A158、A159、A168、A175、A178、A180、A181、A182、A183、A184、A188、A189、A190、A191、A192、A195、A197、A198、A199、B1、B2、B3、B4、B5、B6、B7、B8和B9,或化合物TX選自A1、A3、A4、A5、A6、A31、A45、A46、A48、A49、A76、A80、A81、A82、A86、A90、A100、A101、A109、A110、A115、A124、A126、A128、A129、A132、A136、A143、A144、A145、B3、B4、B5、B6、B7、B9和B10,或A6或化合物TX選自A4、A5、A10、A11、A23、A25、A33、A34、A36、A40、A42、A45、A46、A48、A49、A50、A56、A80、A82、A84、A86、A94、A100、A101、A111、A112、A124、A126、A128、A132、A134、A137、A143、A168、B1、B2、B3、 B4、B5、B6和B9,或化合物TX選自A46、A128、A132、A135、A137、B1、B2、B3、B4、B5、B9和B10。 In the above various active ingredients to be mixed with TX, the compound of formula I is preferably a compound of Tables 1 to 12, A, B, C and D; more preferably and even more preferably, selected from Tables 1 to 12. a compound of A, B; compound TX is selected from Table A, or compound TX is selected from Table B, or compound TX is selected from Table C, or compound TX is selected from Table D, and it is preferred that compound TX is selected from A1. A3, A4, A5, A6, A8, A9, A10, A11, A13, A15, A16, A17, A22, A23, A25, A28, A30, A31, A32, A33 to A36, A38 to A40, A45 to A51, A76, A56, A59, A77, A80, A82, A84, A85, A86, A87, A90, A91, A93, A94, A99, A101, A104, A105, A106, A111, A112, A115, A120, A122, A124, A126, A128, A129, A131, A132, 133, A134, A135, A136, A137, A138, A143, A144, A145, B1, B2, B3, B4, B5, B6, B7, B8, B9 and B10, or a compound TX is selected from the group consisting of A1, A2, A3, A4, A5, A8, A9, A10, A11, A13, A14, A15, A16, A17, A19, A20, A22, A23, A25, A30, A31, A32, A33, A34 , A36, A37, A38, A39, A40, A41, A42, A45, A46, A47, A48, A49, A50, A51, A76, A56, A57, A59, A61, A65, A68, A69, A72, A82, A86 , A90, A101, A112, A115, A126, A128, A129, A130, A131, A132, 133, A134, A135, A136, A137, A138, A139, A140, A142, A143, A144, A145, A146, A147, A149 , A151, A157, A158, A159, A167, A168, A178, A180, A181, A182 A183, A184, A186, A187, A188, A189, A190, A192, A195, A196, A197, A198, A199, B1, B2, B3, B4, B5, B6, B7, B8, B9 and B10, or compound TX From A1, A3, A4, A5, A6, A10, A12, A13, A15, A22, A23, A25, A28, A31, A32, A33, A34, A35, A36, A38, A39, A40, A41, A42, A45 , A46, A48, A49, A50, A51, A76, A56, A57, A59, A61, A79, A80, A83, A84, A86, A87, A90, A91, A93, A94, A95, A104, A106, A111, A112, A123, A126, A128, A129, A130, A131, A132, 133, A134, A135, A136, A137, A138, A142, A143, A144, A145, A146, A151, A157, A159, A163, A168, A178, A181, A182, A183, A184, A188, A189, A192, A195, A197, A199, B1, B2, B3, B4, B5, B6, B7, B8, B9 and B10, or compound TX is selected from the group consisting of A1, A2, A3, A4, A5, A6, A10, A11, A12, A23, A30, A32, A33, A34, A35, A38, A39, A40, A42, A45, A46, A48 , A49, A51, A76, A56, A57, A59, A61, A65, A68, A69, A80, A81, A82, A84, A87, A93, A101, A106, A109, A112, A115, A124, A126, A128, A129 , A131, A132, 133, A134, A135, A136, A137, A138, A143, A144, A145, A146, A151, A157, A158, A159, A168, A175, A178, A180, A181, A182, A183, A184, A188 , A189, A190, A191, A192, A195, A197, A198, A199, B1, B2, B3, B4, B5, B6, B7, B8 and B9, or the compound TX is selected from the group consisting of A1, A3, A4, A5, A6, A31, A45, A46, A48, A49, A76, A80 A81, A82, A86, A90, A100, A101, A109, A110, A115, A124, A126, A128, A129, A132, A136, A143, A144, A145, B3, B4, B5, B6, B7, B9 and B10, Or A6 or compound TX is selected from the group consisting of A4, A5, A10, A11, A23, A25, A33, A34, A36, A40, A42, A45, A46, A48, A49, A50, A56, A80, A82, A84, A86, A94 , A100, A101, A111, A112, A124, A126, A128, A132, A134, A137, A143, A168, B1, B2, B3, B4, B5, B6 and B9, or compound TX are selected from the group consisting of A46, A128, A132, A135, A137, B1, B2, B3, B4, B5, B9 and B10.
在上述式I化合物(特別是選自該表1到12、A、B、C與D之化合物)與其他殺蟲劑、殺真菌劑、除草劑、安全劑、佐劑及類似物之混合物中,該混合比例可在極大範圍內變化,且(較佳是100:1至1:6000,特別是50:1至1:50,更特別是20:1至1:20,甚至更特別是10:1至1:10。該等比例被理解為,一方面包含重量比,另方面也包含莫耳比。 In a mixture of the above compounds of formula I (particularly selected from the compounds of Tables 1 to 12, A, B, C and D) with other insecticides, fungicides, herbicides, safeners, adjuvants and the like The mixing ratio can vary over a wide range and (preferably from 100:1 to 1:6000, especially from 50:1 to 1:50, more particularly from 20:1 to 1:20, even more particularly 10) : 1 to 1: 10. These ratios are understood to include, on the one hand, a weight ratio and, in addition, a molar ratio.
該等混合物可有利地被使用在上述調配物中(在此情況下,「活性成分」係和TX與混合配對物的各混合物相關)。 These mixtures can advantageously be used in the above formulations (in this case, the "active ingredient" system and TX are associated with each mixture of the mixed partners).
一些混合物可包含具有顯著不同的物理、化學或生物性質的活性成分,以致他們不會輕易成為相同的習知調配物類型。在這些情況下,可以製備其他調配物類型。舉例來說,當一種活性成分是不溶於水的固體,而另一者是不溶於水的液體,仍然可能將各活性成分分散在相同的連續水相中,其係藉由將固體活性成分分散作為懸浮液(使用類似SC的製備),而將液體活性成分分散作為乳劑(使用類似EW的製備)。所產生的組成物為懸浮乳劑(SE)調配物。 Some mixtures may contain active ingredients that have significantly different physical, chemical or biological properties such that they do not readily become the same type of conventional formulation. In these cases, other formulation types can be prepared. For example, when one active ingredient is a water-insoluble solid and the other is a water-insoluble liquid, it is still possible to disperse the active ingredients in the same continuous aqueous phase by dispersing the solid active ingredients. As a suspension (using a preparation similar to SC), the liquid active ingredient was dispersed as an emulsion (using a preparation similar to EW). The resulting composition is a suspension emulsion (SE) formulation.
可將包含選自表1到12、A、B與C的TX,與上述一或多種活性成分的混合物應用於(例如)單一「預拌」形式中,應用於由單一活性成分要素之個別調配物所構成的組合噴霧混合物(如「桶混合物」(tank-mix))中,以及當以連續方式使用時,應用於單一活性成分的組合應用中,亦即,在合理的短期間(如幾小時或幾天)一個接一個地應用。施用選自表 1到12、A、B與C的式I化合物及上述的活性成分的順序對本發明物的作用來說並不重要。 A mixture comprising TX selected from Tables 1 to 12, A, B and C, and a mixture of one or more of the above active ingredients may be applied, for example, to a single "premixed" form for individual blending of single active ingredient elements. a combination spray mixture of materials (such as a "tank-mix"), and when used in a continuous manner, in a combined application of a single active ingredient, that is, in a reasonable short period of time (eg, Hours or days) apply one by one. Application selected from the table The order of the compounds of formula I from 1 to 12, A, B and C and the above-mentioned active ingredients is not critical to the action of the invention.
式(I)化合物可與土壤、泥炭或其他生根媒介物等混合,以保護植物免於種子傳播、土壤傳播或是葉面真菌疾病侵襲。 The compound of formula (I) can be mixed with soil, peat or other rooting agents to protect the plant from seed, soil or foliar fungal diseases.
適合用於組成物的增效劑的例子包括增效醚(piperonyl butoxide)、增效菊(sesamex)、增效散(safroxan)和十二基咪唑。 Examples of synergists suitable for use in the composition include piperonyl butoxide, sesamex, safroxan, and dodecyl imidazole.
適合納入組成物的除草劑與植物生長調節劑,將視預定目標和所需的效果而定。 Herbicides and plant growth regulators suitable for inclusion in the composition will depend on the intended purpose and desired effect.
敵稗(porpanil)是可納入稻選擇性除草劑之中的一個例子。而PIXTM是可用於棉花的植物生長調節劑例子。 Porpanil is an example of a herbicide that can be incorporated into rice. And PIX TM is available for cotton plant growth regulator examples.
一些混合物可包含具有顯著不同的物理、化學或生物性質的活性成分,以致他們不會輕易成為相同的習知調配物類型。在這些情況下,可以製備其他調配物類型。舉例來說,當一種活性成分是不溶於水的固體,而另一者是不溶於水的液體,仍然可能將各活性成分分散在相同的連續水相中,其係藉由將固體活性成分分散作為懸浮液(使用類似SC的製備),而將液體活性成分分散作為乳劑(使用類似EW的製備)。所產生的組成物為懸浮乳劑(SE)調配物。 Some mixtures may contain active ingredients that have significantly different physical, chemical or biological properties such that they do not readily become the same type of conventional formulation. In these cases, other formulation types can be prepared. For example, when one active ingredient is a water-insoluble solid and the other is a water-insoluble liquid, it is still possible to disperse the active ingredients in the same continuous aqueous phase by dispersing the solid active ingredients. As a suspension (using a preparation similar to SC), the liquid active ingredient was dispersed as an emulsion (using a preparation similar to EW). The resulting composition is a suspension emulsion (SE) formulation.
中間體I1:5-疊氮基-1-甲基-3-五氟乙基-4-三氟甲基-1H-吡唑 Intermediate I1: 5-azido-1-methyl-3-pentafluoroethyl-4-trifluoromethyl-1H-pyrazole
將5-氟基-1-甲基-3-五氟乙基-4-三氟甲基-1H-吡唑(根據《Russian Chemical Bulletin》(俄羅斯化學通報),1990年,39,N° 11,2338頁,2g;7mmol製備)加至DMSO(10ml)和疊氮化鈉(0.5g;7.7mmol)的混合物中加至混合物(保存於室溫下)中。在室溫下攪拌該混合物一整夜。在反應完成之後,加入水(100mL)與二乙醚(100mL)的混合物。分離了相,並使用二乙醚萃取水相二次。未經額外的純化使用此化合物。 5-Fluoro-1-methyl-3-pentafluoroethyl-4-trifluoromethyl-1H-pyrazole (according to "Russian Chemical Bulletin", 1990, 39, N° 11 , 2338 pages, 2 g; 7 mmol preparation) was added to a mixture of DMSO (10 ml) and sodium azide (0.5 g; 7.7 mmol) and added to the mixture (preserved at room temperature). The mixture was stirred overnight at room temperature. After the reaction was completed, a mixture of water (100 mL) and diethyl ether (100 mL) was added. The phases were separated and the aqueous phase was extracted twice with diethyl ether. This compound was used without additional purification.
中間體I2:D1:3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺 Intermediate I2: D1: 3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3] Triazol-4-yl]-aniline
乙炔基苯胺(市售)和5-疊氮基-1-甲基-3-五氟乙基-4-三氟甲基-1H-吡唑(中間體I1,0.81g,2.6mmol)皆懸浮於水和t-BuOH(15mL)的混合物中。將抗壞血酸鈉(0.300ml 1M水溶液,新製備)添加至混合物中,接著添加五水硫酸銅 (0.017g)。將所產生的非勻相混合物大力攪拌96小時。用水稀釋反應混合物,並以乙酸乙酯萃取產物。用鹽水清洗有機相,並以硫酸鎂乾燥並蒸發。殘基經由矽膠管柱層析法(iHEX/EtOAc=3:1)提供想要的產物3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D1)。1HNMR(400MHz,CDCl3):8.01(s,1H)、7.32-7.19(m,2H)、6.75(dd,1H)、3.39(s,3H)、3.81(s,2H)ppm。 Ethynyl aniline (commercially available) and 5-azido-1-methyl-3-pentafluoroethyl-4-trifluoromethyl-1H-pyrazole (intermediate I1, 0.81 g, 2.6 mmol) were suspended In a mixture of water and t-BuOH (15 mL). Sodium ascorbate (0.300 ml of a 1 M aqueous solution, freshly prepared) was added to the mixture followed by copper sulfate pentahydrate (0.017 g). The resulting heterogeneous mixture was vigorously stirred for 96 hours. The reaction mixture was diluted with water and the product was extracted with ethyl acetate. The organic phase was washed with brine and dried over magnesium sulfate and evaporated. The desired product 3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-) was obtained from EtOAc EtOAc (EtOAc) Pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenylamine (Compound D1). 1 H NMR (400 MHz, CDCl 3 ): 8.01 (s, 1H), 7.32-7.19 (m, 2H), 6.75 (dd, 1H), 3.39 (s, 3H), 3.81 (s, 2H) ppm.
2-氟基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D4)藉由使用3-乙炔基-2-氟基-苯胺作為起始原料的相同方法而製備。 2-fluoro-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]tri Zizo-4-yl]-aniline (Compound D4) was prepared by the same method using 3-ethynyl-2-fluoro-aniline as a starting material.
1HNMR(400MHz,CDCl3):8.26(d,1H)、7.73(t,1H)、7.14(t,1H)、6.88(t,1H)、3.89(s,3H)、3.87(bs,2H)ppm。 1 H NMR (400 MHz, CDCl 3 ): 8.26 (d, 1H), 7.73 (t, 1H), 7.14 (t, 1H), 6.88 (t, 1H), 3.89 (s, 3H), 3.87 (bs, 2H) Ppm.
中間體I3:4-乙炔基-2-硝基-苄腈 Intermediate I3: 4-ethynyl-2-nitro-benzonitrile
將含有25mL的4-溴基-2-硝基苄腈(110.1mmol)、25.2ml的乙炔基三甲基矽烷(178.4mmol)、0.49g的醋酸鈀(2.2mmol)和1.16g的三苯基膦(4.4mmol)的無水三乙胺溶液(300mL)快速地加熱,在氬中回流整夜。將混合物冷卻,並通過過濾分離三乙胺氫溴酸鹽的結晶狀白色固體。將深棕色濾液濃 縮,與250mL的碳酸氫鈉水溶液混合,並以二氯甲烷(3x100ml)萃取。結合有機餾分,以硫酸鎂乾燥,並濃縮以產生油,使其在200ml的THF中溶解,並以300ml的甲醇和450mg的碳酸鉀處理。將混合物攪拌一小時並濃縮。將濃縮的溶液與250mL的碳酸氫鈉水溶液混合,並以乙酸乙酯(3x100ml)萃取。結合有機餾分,以硫酸鎂乾燥,並在真空中濃縮,以環己烷/乙酸乙酯(95:5)進行層析法處理,產生4-乙炔基-2-硝基-苄腈(7.3g,39%的產率)。1HNMR(400MHz,CDCl3):8.40(s,1H)、7.89(s,2H)、3.5(s,1H)ppm。 Will contain 25 mL of 4-bromo-2-nitrobenzonitrile (110.1 mmol), 25.2 ml of ethynyltrimethylnonane (178.4 mmol), 0.49 g of palladium acetate (2.2 mmol) and 1.16 g of triphenyl. A solution of phosphine (4.4 mmol) in dry triethylamine (300 mL) was quickly heated and refluxed in EtOAc overnight. The mixture was cooled and the crystalline white solid of triethylamine hydrobromide was isolated by filtration. The dark brown filtrate was concentrated, taken up in water (250 mL) aqueous The organic fraction was combined, dried over magnesium sulfate and concentrated to give an oil, which was dissolved in 200 ml of THF and treated with 300 ml of methanol and 450 mg of potassium carbonate. The mixture was stirred for one hour and concentrated. The concentrated solution was mixed with 250 mL of aqueous sodium bicarbonate and extracted with ethyl acetate (3×100 mL). The combined organic extracts were dried with MgSO4, EtOAcjjjjjjjjjjjjjjjjjjjjjj , 39% yield). 1 H NMR (400 MHz, CDCl 3 ): 8.40 (s, 1H), 7.89 (s, 2H), 3.5 (s, 1H) ppm.
中間體I4:C1:4-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-2-硝基-苄腈 Intermediate I4: C1: 4-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3] Triazol-4-yl]-2-nitro-benzonitrile
4-乙炔基-2-硝基-苄腈(1.20g,1.07mmol)和5-疊氮基-1-甲基-3-五氟乙基-4-三氟甲基-1H-吡唑(中間體I1,2.15g,7.0mmol)皆懸浮於水和t-BuOH(1:1,30mL)的混合物中。將抗壞血酸鈉(0.3ml,1M溶液於水中,新製備)添加至混合物中,接著添加五水硫酸銅(0.017g)。在室溫下將所產生的非勻相混合物大力攪拌96小時。用水稀釋反應混合物,並用冰浴予以冷卻。將沉澱的橙色產物予以過濾和乾燥。殘基 經由矽膠管柱層析法(乙酸乙酯:環己烷1:3)提供想要的產物(化合物C1)(1.3g,40%的產率)。1HNMR(400MHz,CDCl3):8.82(s,1H)、8.41(d,1H)、8.33(s,1H)、8.07(d,1H)、3.92(s,3H)ppm。 4-ethynyl-2-nitro-benzonitrile (1.20 g, 1.07 mmol) and 5-azido-1-methyl-3-pentafluoroethyl-4-trifluoromethyl-1H-pyrazole ( Intermediate I1, 2.15 g, 7.0 mmol) were suspended in a mixture of water and t-BuOH (1:1, 30 mL). Sodium ascorbate (0.3 ml, 1 M solution in water, freshly prepared) was added to the mixture followed by copper sulfate pentahydrate (0.017 g). The resulting heterogeneous mixture was vigorously stirred at room temperature for 96 hours. The reaction mixture was diluted with water and cooled with an ice bath. The precipitated orange product was filtered and dried. The residue was purified by column chromatography (ethyl acetate: hexanes: 1:3) to give the desired product (Compound C1) (1.3 g, 40% yield). 1 H NMR (400 MHz, CDCl 3 ): 8.82 (s, 1H), 8.41 (d, 1H), 8.33 (s, 1H), 8.07 (d, 1H), 3.92 (s, 3H) ppm.
使用1-氯-4-乙炔基-2-硝基-苯(可用萘)做為起始原料的相同方法來製備4-(4-氯-3-硝基-苯基)-1-[2-甲基-5-(1,1,2,2,2-五氟乙基)-4-(三氟甲基)吡唑-3-基]三唑。 4-(4-Chloro-3-nitro-phenyl)-1-[2] was prepared in the same manner using 1-chloro-4-ethynyl-2-nitro-benzene (naphthalene) as a starting material. -Methyl-5-(1,1,2,2,2-pentafluoroethyl)-4-(trifluoromethyl)pyrazol-3-yl]triazole.
1HNMR(400MHz,CDCl3):8.40(d,1H)、8.23(s,1H)、8.10(dd,1H)、7.71(d,1H)、3.81(s,3H)ppm。 1 H NMR (400 MHz, CDCl 3 ): 8.40 (d, 1H), 8.23 (s, 1H), 8.10 (dd, 1H), 7.71 (d, 1H), 3.81 (s, 3H) ppm.
中間體I5:D2:2-胺基-4-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苄腈 Intermediate I5: D2: 2-Amino-4-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1 , 2,3]triazol-4-yl]-benzonitrile
將水性氫氧化鈉(0.1M)(12.5ml)、亞硫酸氫鈉(82%,2.98g,14.0mmol)和四丁基溴化銨(「TBAB」)(0.09g,0.3mmol)添加至含有4-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-2-硝基-苄腈(中間體I5)(1.35g,2.8mmol)的四氫呋喃(37.5ml)溶液中。在室溫下攪拌反應混合物2小時。添加水(100mL)和乙酸乙酯(100mL)的混合物。 分離水相與有機相。用乙酸乙酯萃取水相兩次。結合的有機萃取物經由硫酸鈉乾燥並濃縮。在矽膠上過濾純化殘基以取得2-胺基-4-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苄腈(化合物D2)(1.22g,96%的產率)。1HNMR(400MHz,CDCl3):8.12(s,1H)、7.52(d,1H)、7.41(s,1H)、7.19(d,1H)、4.58(sb,2H)、3.88(s,3H)ppm。 Aqueous sodium hydroxide (0.1 M) (12.5 ml), sodium hydrogen sulfite (82%, 2.98 g, 14.0 mmol) and tetrabutylammonium bromide ("TBAB") (0.09 g, 0.3 mmol) were added to the 4-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl a solution of 2-nitro-benzonitrile (Intermediate I5) (1.35 g, 2.8 mmol) in tetrahydrofurane (37.5 mL). The reaction mixture was stirred at room temperature for 2 hours. A mixture of water (100 mL) and ethyl acetate (100 mL) was added. The aqueous phase and the organic phase are separated. The aqueous phase was extracted twice with ethyl acetate. The combined organic extracts were dried over sodium sulfate and concentrated. The residue was purified by filtration on silica gel to give 2-amino-4-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H -[1,2,3]Triazol-4-yl]-benzonitrile (Compound D2) (1.22 g, 96% yield). 1 H NMR (400 MHz, CDCl 3 ): 8.12 (s, 1H), 7.52 (d, 1H), 7.41 (s, 1H), 7.19 (d, 1H), 4.58 (sb, 2H), 3.88 (s, 3H) Ppm.
使用4-(2-甲氧基-3-硝苯基)-1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑做為起始原料的相同方法來製備表D的2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D5)。1HNMR(400MHz,CDCl3):8.4(s,1H)、7.68(d,1H)、7.11(t,1H)、6.83(t,1H)、3.92(bs,2H+3H)、3.71(s,3H)ppm。 4-(2-Methoxy-3-nitrophenyl)-1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H was used. -[1,2,3]triazole as the starting material for the preparation of 2-methoxy-3-[1-(2-methyl-5-pentafluoroethyl-4-III) of Table D Fluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenylamine (Compound D5). 1 H NMR (400 MHz, CDCl 3 ): 8.4 (s, 1H), 7.68 (d, 1H), 7.11 (t, 1H), 6.83 (t, 1H), 3.92 (bs, 2H+3H), 3.71 (s, 3H) ppm.
中間體I6:D3:2-氯-5-[1-[2-甲基-5-(1,1,2,2,2-五氟乙基)-4-(三氟甲基)吡唑-3-基]三唑-4-基]苯胺 Intermediate I6: D3: 2-chloro-5-[1-[2-methyl-5-(1,1,2,2,2-pentafluoroethyl)-4-(trifluoromethyl)pyrazole -3-yl]triazol-4-yl]aniline
在環境溫度下,將氯化錫(1.5g,6.6mmol)添加至含有4-(4-氯-3-硝基-苯基)-1-[2-甲基-5-(1,1,2,2,2-五氟乙 基)-4-(三氟甲基)吡唑-3-基]三唑(範例I4)(0.90g,1.8mmol)的異丙醇(6ml)溶液中。將混合物冷卻至0℃,並慢慢添加濃縮的鹽酸水(1.5ml)。於80℃下攪拌反應混合物2小時。蒸發總量三分之一的異丙醇。將水(100ml)添加至濃縮的混合物,並添加水性氫氧化鈉(30%),以將pH值調整到8至9。並用乙酸乙酯萃取水相三次(3x200ml)。結合的有機萃取物經由硫酸鈉乾燥,並進行了濃縮。在矽土上用管柱層析法純化殘基(沖提液:環己烷/乙酸乙酯2:1到1:1)以取得2-氯-5-[1-[2-甲基-5-(1,1,2,2,2-五氟乙基)-4-(三氟甲基)吡唑-3-基]三唑-4-基]苯胺(化合物D3)(0.67 g,79%的產率)。 Tin chloride (1.5 g, 6.6 mmol) was added to contain 4-(4-chloro-3-nitro-phenyl)-1-[2-methyl-5-(1,1, at ambient temperature 2,2,2-pentafluoroethyl A solution of 4-(trifluoromethyl)pyrazol-3-yl]triazole (Example I4) (0.90 g, 1.8 mmol) in isopropyl alcohol (6 mL). The mixture was cooled to 0 ° C and concentrated aqueous hydrochloric acid (1.5 mL) was slowly added. The reaction mixture was stirred at 80 ° C for 2 hours. Evaporate a third of the total amount of isopropanol. Water (100 ml) was added to the concentrated mixture, and aqueous sodium hydroxide (30%) was added to adjust the pH to 8 to 9. The aqueous phase was extracted three times with ethyl acetate (3 x 200 mL). The combined organic extracts were dried over sodium sulfate and concentrated. The residue was purified by column chromatography on silica (eluent: cyclohexane / ethyl acetate 2:1 to 1:1) to give 2-chloro-5-[1-[2-methyl- 5-(1,1,2,2,2-pentafluoroethyl)-4-(trifluoromethyl)pyrazol-3-yl]triazol-4-yl]phenylamine (Compound D3) (0.67 g, 79% yield).
1HNMR(400MHz,CDCl3):8.01(s,1H)、7.40(d,1H)、7.35(d,1H)、7.14(dd,1H)、4.23(bs,2H)、3.87(s,3H)ppm。 1 H NMR (400 MHz, CDCl 3 ): 8.01 (s, 1H), 7.40 (d, 1H), 7.35 (d, 1H), 7.14 (dd, 1H), 4.23 (bs, 2H), 3.87 (s, 3H) Ppm.
範例I 7.1:D6:乙基-{2-氟-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-胺 Example I 7.1: D6: ethyl-{2-fluoro-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H -[1,2,3]triazol-4-yl]-phenyl}-amine
將2-氟-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D4)(0.200g, 0.45mmol)溶解於甲醇(8ml)中,並添加乙醛(0.027ml,0.47mmol)和乙酸(0.03ml,0.54mmol)。接著以小量方式添加硼氫氰化物(0.0368g,0.585mmol)。在室溫下攪拌反應混合物1.2小時。用碳酸氫鈉水溶液稀釋混合物,並以乙酸乙酯萃取水層兩次。將結合的有機層由硫酸鈉乾燥,並過濾和濃縮。利用層析法純化了殘基(沖提液:環己烷/乙酸乙酯)以取得乙基-{2-氟-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-胺(化合物D6)(0.170g,80%)。 2-Fluoro-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3] Zin-4-yl]-aniline (Compound D4) (0.200 g, 0.45 mmol) was dissolved in methanol (8 ml) and acetaldehyde (0.027 ml, 0.47 mmol) and acetic acid (0.03 ml, 0.54 mmol). Boron hydrocyanide (0.0368 g, 0.585 mmol) was then added in small amounts. The reaction mixture was stirred at room temperature for 1.2 hours. The mixture was diluted with aqueous sodium bicarbonate and the aqueous layer was extracted twice with ethyl acetate. The combined organic layers were dried over sodium sulfate and filtered and concentrated. The residue was purified by chromatography (eluent: cyclohexane / ethyl acetate) to give ethyl-{2-fluoro-3-[1-(2-methyl-5-pentafluoroethyl-4) -Trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenyl}-amine (Compound D6) (0.170 g, 80%).
1HNMR(400MHz,CDCl3):8.21(d,1H)、7.72(t,1H)、7.19(t,1H)、6.29(t,1H)、3.93(bs,1H)、3.88(s,3H)、3.27(q,2H)、1.34(t,3H)ppm。 1 H NMR (400 MHz, CDCl 3 ): 8.21 (d, 1H), 7.72 (t, 1H), 7.19 (t, 1H), 6.29 (t, 1H), 3.93 (bs, 1H), 3.88 (s, 3H) , 3.27 (q, 2H), 1.34 (t, 3H) ppm.
使用2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D5)做為起始原料並將含甲醛的水(~37.3質量%)當做試劑的類似方法製備表D的{2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)1H[1,2,3]三唑-4-基]-苯基}-甲胺(化合物D7): Using 2-methoxy-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3 [2-methoxy-3-[Table D] is prepared by a similar method using triazol-4-yl]-aniline (Compound D5) as a starting material and using formaldehyde-containing water (~37.33% by mass) as a reagent. 1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)1H[1,2,3]triazol-4-yl]-phenyl} -Methylamine (Compound D7):
1HNMR(400MHz,CDCl3):8.48(s,1H)、7.61(dd,1H)、7.22(t,1H)、6.73(dd,1H)、4.32(bs,1H)、3.92(s,3H)、3.68(s,3H)、2.92(s,3H)ppm。 1 H NMR (400 MHz, CDCl 3 ): 8.48 (s, 1H), 7.61 (dd, 1H), 7.22 (t, 1H), 6.73 (dd, 1H), 4.32 (bs, 1H), 3.92 (s, 3H) , 3.68 (s, 3H), 2.92 (s, 3H) ppm.
實施例P1:4-氰-N-{2-氰-5-[1-(2-甲基-5-五氟乙基-4-三氟 甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-2-甲基-苯甲醯胺(化合物A1) Example P1: 4-cyano-N-{2-cyano-5-[1-(2-methyl-5-pentafluoroethyl-4-trifluoro Methyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenyl}-2-methyl-benzamide (Compound A1)
依次將2-甲基-4-氰基苯甲醯氯(0.1g,0.5mmol,2eq.)和吡啶(0.064Ml,0.8eq)添加至含有2-胺基-4-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苄腈(化合物D2)的四氫呋喃(5mL)溶液中。於室溫下攪拌混合物一整夜。接著,將該混合物溶解於乙酸乙酯與水的混合物中。分離有機層與水層,接著用乙酸乙酯萃取水相兩次。結合有機相並以硫酸鈉乾燥,且溶劑在真空中蒸發。用管柱層析法純化殘基(環己烷:乙酸乙酯:3:1)以取得4-氰-N-{2-氰-5-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-2-甲基-苯甲醯胺(化合物A1)(0.1g,63%的產率)。1HNMR(400MHz,CDCl3):9.05(s,1H)、8.30(s,1H)、8.03(s,1H)、7.97(d,1H)、7.81(d,1H)、7.70(d,1H)、7.64(m,2H)、3.89(s,3H)、2.60(s,3H)ppm。 2-Methyl-4-cyanobenzamide chloride (0.1 g, 0.5 mmol, 2 eq.) and pyridine (0.064 Ml, 0.8 eq) were added to 2-amino-4-[1-(2- Methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-benzonitrile (Compound D2) In a solution of tetrahydrofuran (5 mL). The mixture was stirred at room temperature overnight. Next, the mixture was dissolved in a mixture of ethyl acetate and water. The organic layer and the aqueous layer were separated, then the aqueous phase was extracted twice with ethyl acetate. The organic phase was combined and dried over sodium sulfate, and the solvent was evaporated in vacuo. The residue was purified by column chromatography (cyclohexane:ethyl acetate: 3:1) to afford 4-cyan-N-{2-cyan-5-[1-(2-methyl-5-pentafluoro Ethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenyl}-2-methyl-benzamide (Compound A1) (0.1 g, 63% yield). 1 H NMR (400 MHz, CDCl 3 ): 9.05 (s, 1H), 8.30 (s, 1H), 8.03 (s, 1H), 7.97 (d, 1H), 7.81 (d, 1H), 7.70 (d, 1H) , 7.64 (m, 2H), 3.89 (s, 3H), 2.60 (s, 3H) ppm.
使用2-胺基-4-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苄腈(化合物D2)或3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物C1)或2-氯-5-[1-[2- 甲基-5-(1,1,2,2,2-五氟乙基)-4-(三氟甲基)吡唑-3-基]三唑-4-基]苯胺(化合物D3)或2-氟-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D4)或2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D5)或乙基-{2-氟-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-胺(化合物D6)或{2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)1H[1,2,3]三唑-4-基]-苯基}-甲胺(化合物D7)做為起始原料的相同或類似方法來製備表A中的A2至A6與A76、A126至A131、133至141以及表B中的B1至B8的化合物。 2-Amino-4-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3] was used. Triazol-4-yl]-benzonitrile (Compound D2) or 3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)- 1H-[1,2,3]triazol-4-yl]-phenylamine (Compound C1) or 2-Chloro-5-[1-[2- Methyl-5-(1,1,2,2,2-pentafluoroethyl)-4-(trifluoromethyl)pyrazol-3-yl]triazol-4-yl]phenylamine (Compound D3) or 2-fluoro-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazole 4-yl]-aniline (Compound D4) or 2-methoxy-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazole-3- -1H-[1,2,3]triazol-4-yl]-phenylamine (Compound D5) or Ethyl-{2-Fluoro-3-[1-(2-methyl-5-pentafluoroethyl) Benzyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenyl}-amine (Compound D6) or {2-A Oxy-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)1H[1,2,3]triazole-4- Preparation of A2 to A6 and A76, A126 to A131, 133 to 141, and B1 to B8 in Table B in Table A by the same or similar method using as a starting material. compound of.
實施例P2:將胺基苯甲醯胺平行醯化的一般方法 Example P2: General Method for Parallel Deuteration of Aminobenzamide
藉由在甲苯(15.6ml)中溶解胺基苯甲醯胺(0.78mmol)(例如在表A化合物A7實例中的3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D1),來製備A溶液。藉由在甲苯(8ml)中溶解醯氯(1.0mol)(例如在表A編號A7化合物實例中的2-氟-苯甲醯氯),來製備B溶液。 Aminobenzamide (0.78 mmol) was dissolved in toluene (15.6 ml) (for example, 3-[1-(2-methyl-5-pentafluoroethyl-4-) in the compound A7 example of Table A Trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenylamine (Compound D1) to prepare solution A in toluene (8 ml) The B solution was prepared by dissolving ruthenium chloride (1.0 mol) (for example, 2-fluoro-benzimid chloride in the example of the compound of Table A No. A7).
將A溶液(0.6ml,30μmol)放在孔盤的孔中,並依次添加 了B溶液(0.3ml,36μmol)與二異丙基乙基胺(Hunig's Base)(30μl,150μmol)。於70℃下攪拌混合物一整夜。使用乙腈(0.6ml)與N,N-二甲基乙醯胺(0.2ml)的混合物稀釋混合物,接著用HPLC純化,以取得想要的化合物,例如:2-氟-N-{3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-苯甲醯胺(化合物A7)。 Place the A solution (0.6ml, 30μmol) in the well of the well plate and add it in order. Solution B (0.3 ml, 36 μmol) and diisopropylethylamine (Hunig's Base) (30 μl, 150 μmol). The mixture was stirred at 70 ° C overnight. The mixture was diluted with a mixture of acetonitrile (0.6 ml) and N,N-dimethylacetamide (0.2 ml), followed by purification by HPLC to give the desired compound, for example: 2-fluoro-N-{3-[ 1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-benzene Benzoyl-benzamide (Compound A7).
這種一般方法或類似的方法是用來製備表A的一些化合物(化合物編號A7至A75、A77至A125與A146至A200),其使用2-胺基-4-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苄腈(化合物D2)或3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D1)或2-氯-5-[1-[2-甲基-5-(五氟乙基1)-4-(三氟甲基)吡唑-3-基]三唑-4-基]苯胺(化合物D3)或2-氟-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D4)做為起始原料。 This general method or a similar method is used to prepare some of the compounds of Table A (Compound Nos. A7 to A75, A77 to A125 and A146 to A200) using 2-amino-4-[1-(2-methyl) 5-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-benzonitrile (Compound D2) or 3 -[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl] -aniline (compound D1) or 2-chloro-5-[1-[2-methyl-5-(pentafluoroethyl 1)-4-(trifluoromethyl)pyrazol-3-yl]triazole- 4-yl]aniline (compound D3) or 2-fluoro-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H -[1,2,3]Triazol-4-yl]-phenylamine (Compound D4) was used as a starting material.
實施例P3:N-{2-氟-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-1-氧基-異菸鹼醯胺(化合物A132) Example P3: N -{2-Fluoro-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1 ,2,3]triazol-4-yl]-phenyl}-1-oxy-isonicotinamide (Compound A132)
將N-{2-氟-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-異菸鹼醯胺(化合物A128)(0.050g,0.1125mmol)溶解於二氯甲烷(2ml)中,並添加3-氯過氧苯甲酸(0.0261g,0.1463mmol)。在室溫下攪拌4小時之後,用二氯甲烷稀釋混合物,並添加氫氧化鈉水溶液。分離相,使用鹽水清洗有機相,並由硫酸鈉乾燥、過濾並濃縮以取得純化合物A132(50mg,79%的產率)。熔點227-229℃。1H-NMR(400MHz,CDCl3):8.44(t,1H)、8.22(d,2H)、8.17(d,1H)、8.09(t,1H)、7.97(bs,1H)、7.71(d,2H)、7.32(t,1H)、3.82(s,3H)ppm。 N-{2-Fluoro-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2, 3] Triazol-4-yl]-phenyl}-isonicotinamine amide (Compound A128) (0.050 g, 0.1125 mmol) was dissolved in dichloromethane (2 ml) and 3-chloroperoxybenzoic acid was added ( 0.0261 g, 0.1463 mmol). After stirring at room temperature for 4 hours, the mixture was diluted with dichloromethane, and aqueous sodium hydroxide solution was added. The phases were separated, EtOAc (EtOAc m.) Melting point 227-229 ° C. 1 H-NMR (400MHz, CDCl 3): 8.44 (t, 1H), 8.22 (d, 2H), 8.17 (d, 1H), 8.09 (t, 1H), 7.97 (bs, 1H), 7.71 (d, 2H), 7.32 (t, 1H), 3.82 (s, 3H) ppm.
用相同的方法製備了表A的化合物A142至A143和表B的化合物B9至B10。 Compounds A142 to A143 of Table A and Compounds B9 to B10 of Table B were prepared in the same manner.
實施例P4:2,4,6-三氟-N-{2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-苯甲醯胺(化合物A144) Example P4: 2,4,6-Trifluoro-N-{2-methoxy-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyridyl) Zyrid-3-yl)-1H-[1,2,3]triazol-4-yl]-phenyl}-benzamide (Compound A144)
將1-乙基-3-(3-二甲基胺基丙基)碳二亞胺鹽酸鹽(EDCI,0.0429g,0.217mol)、1-羥基-7-偶氮苯並三唑(HOAT,0.0301g,0.217mol)、三乙胺(0.056ml,0.394mmol)和2,4,6-三氟苯甲酸(39mg,0.217mmol)添加於含有2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯胺(化合物D5)(0.09g,0.197mmol)的二氯甲烷(4mL)的溶液中。於室溫下攪拌混合物一整夜(19小時)。接著,用二氯甲烷稀釋混合物,並添加碳酸氫鈉。分離有機層與水層,接著用氫氧化鈉水溶液萃取有機相。藉由硫酸鈉乾澡有機相並過濾,且溶劑在真空中蒸發。使用管柱層析法(環己烷:乙酸乙酯)純化殘基,以取得2,4,6-三氟-N-{2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-苯甲醯胺(化合物A144)(0.038g,32%的產率)。1HNMR(400MHz,CDCl3):8.49(dd,1H)、8.28(s,1H)、8.19(bs,1H)、7.98(dd,1H)、7.29(t,1H)、6.75(t,2H)、3.87(s,3H)、3.63(s,3H)ppm。 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDCI, 0.0429 g, 0.217 mol), 1-hydroxy-7-azobenzotriazole (HOAT) , 0.0301 g, 0.217 mol), triethylamine (0.056 ml, 0.394 mmol) and 2,4,6-trifluorobenzoic acid (39 mg, 0.217 mmol) were added to 2-methoxy-3-[1-( 2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenylamine (Compound D5 (0.09 g, 0.197 mmol) in dichloromethane (4 mL). The mixture was stirred at room temperature overnight (19 hours). Next, the mixture was diluted with dichloromethane and sodium hydrogencarbonate was added. The organic layer and the aqueous layer were separated, and then the organic phase was extracted with aqueous sodium hydroxide. The organic phase was dried by sodium sulfate and filtered, and the solvent was evaporated in vacuo. The residue was purified by column chromatography (cyclohexane: ethyl acetate) to give 2,4,6-trifluoro-N-{2-methoxy-3-[1-(2-methyl- 5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenyl}-benzamide ( Compound A144) (0.038 g, 32% yield). 1 H NMR (400 MHz, CDCl 3 ): 8.49 (dd, 1H), 8.28 (s, 1H), 8.19 (bs, 1H), 7.78 (dd, 1H), 7.29 (t, 1H), 6.75 (t, 2H) , 3.87 (s, 3H), 3.63 (s, 3H) ppm.
用相同的方法製備了表A的化合物A145和A201。 Compounds A145 and A201 of Table A were prepared in the same manner.
實施例P5:2,4,6-三氟-N-{2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4- 基]-苯基}-N-甲基-苯甲醯胺(化合物B11) Example P5: 2,4,6-Trifluoro-N-{2-methoxy-3-[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyridyl) Zyrid-3-yl)-1H-[1,2,3]triazole-4- Base]-phenyl}-N-methyl-benzamide (Compound B11)
將三乙胺(0.060ml,0.425mmol)、2,4,6-三氟苯甲酸(46mg,0.255mmol)和BOP-Cl(0.167g,0.638mmol)添加至含有{2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)1H[1,2,3]三唑-4-基]-苯基}-甲胺(化合物D7)(0.1g,213mmol)的1,2-二氯乙烷(3mL)的溶液中。在回流下攪拌混合物15小時。接著,用二氯甲烷稀釋混合物,並添加碳酸氫鈉。分離有機層與水層,接著用鹽水萃取有機相。藉由硫酸鈉乾燥有機相並過濾,且溶劑在真空中蒸發。用管柱層析法(環己烷:乙酸乙酯)純化殘基,以取得2,4,6-三氟-N-{2-甲氧基-3-[1-(2-甲基-5-五氟乙基-4-三氟甲基-2H-吡唑-3-基)-1H-[1,2,3]三唑-4-基]-苯基}-N-甲基-苯甲醯胺(化合物B11)(0.045g,34%的產率)。 Triethylamine (0.060 ml, 0.425 mmol), 2,4,6-trifluorobenzoic acid (46 mg, 0.255 mmol) and BOP-Cl (0.167 g, 0.638 mmol) were added to contain {2-methoxy-3 -[1-(2-methyl-5-pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)1H[1,2,3]triazol-4-yl]-benzene A solution of methylamine-methylamine (Compound D7) (0.1 g, 213 mmol) in 1,2-dichloroethane (3 mL). The mixture was stirred under reflux for 15 hours. Next, the mixture was diluted with dichloromethane and sodium hydrogencarbonate was added. The organic layer and the aqueous layer were separated, and then the organic phase was extracted with brine. The organic phase was dried over sodium sulfate and filtered, and the solvent evaporated in vacuo. The residue was purified by column chromatography (cyclohexane: ethyl acetate) to give 2,4,6-trifluoro-N-{2-methoxy-3-[1-(2-methyl- 5-Pentafluoroethyl-4-trifluoromethyl-2H-pyrazol-3-yl)-1H-[1,2,3]triazol-4-yl]-phenyl}-N-methyl- Benzamide (Compound B11) (0.045 g, 34% yield).
1HNMR(400MHz,CDCl3):8.20(d,1H)、8.17(s,1H)、7.45(d,1H)、6.82(t,1H)、6.52(bs,1H)、6.38(bs,1H)、3.90(s,3H)、3.78(s,3H)、3.58(s,3H)ppm。此外,範圍包含旋轉異構體的峰值。 1 H NMR (400 MHz, CDCl 3 ): 8.20 (d, 1H), 8.17 (s, 1H), 7.45 (d, 1H), 6.82 (t, 1H), 6.52 (bs, 1H), 6.38 (bs, 1H) , 3.90 (s, 3H), 3.78 (s, 3H), 3.58 (s, 3H) ppm. In addition, the range contains the peaks of the rotamer.
方法A:Method A:
適用化合物A1至A7、C1、D1和D2的LC-MS方法(正或負): LC-MS method (positive or negative) for compounds A1 to A7, C1, D1 and D2:
美商沃特斯(Waters)的ZQ質譜儀(單一四極質譜儀) American Waters ZQ mass spectrometer (single quadrupole mass spectrometer)
儀器參數: Instrument parameters:
離子化方法:電噴灑 Ionization method: electric spraying
極性:正離子 Polarity: positive ion
毛細管(kV)3.00,進樣錐(V)30.00,提取器(V)2.00,來源溫度(℃)100,脫溶劑氣溫度(℃)250,進樣錐氣體流速(L/Hr)50,脫溶劑氣體流速(L/Hr)400 Capillary (kV) 3.00, injection cone (V) 30.00, extractor (V) 2.00, source temperature (°C) 100, desolvation gas temperature (°C) 250, injection cone gas flow rate (L/Hr) 50, off Solvent gas flow rate (L/Hr) 400
質量範圍:100至900Da Quality range: 100 to 900Da
安捷倫(Agilent)公司的HP 1100 HPLC:溶劑除氣劑、四元泵(ZCQ)/二元泵、加熱柱箱和二極管陣列檢測器。 Agilent's HP 1100 HPLC: solvent deaerator, quaternary pump (ZCQ) / binary pump, heated oven and diode array detector.
管柱:費諾美Gemini C18,3mm,30x3mm,溫度:60℃ Column: Fernome Gemini C18, 3mm, 30x3mm, temperature: 60 ° C
DAD波長範圍(nm):200至500 DAD wavelength range (nm): 200 to 500
溶劑梯度: Solvent gradient:
A=水+0.05%HCOOH A=water+0.05%HCOOH
B=乙腈/甲醇(4:1,v:v)+0.04%HCOOH B = acetonitrile / methanol (4:1, v: v) + 0.04% HCOOH
B方法:Method B:
適用化合物A7至A75、A77至A125以及A146至A200的LC-MS方法(正): LC-MS method for the application of compounds A7 to A75, A77 to A125 and A146 to A200 (positive):
美商沃特斯(Waters)的ACQUITY SQD質譜儀(單一四極質譜儀) American Waters ACQUITY SQD Mass Spectrometer (Single Quadrupole Mass Spectrometer)
離子化方法:電噴灑,極性:正離子,毛細管(kV)3.00,進樣錐(V)20.00,提取器(V)3.00,來源溫度(℃)150,脫溶劑氣溫度(℃)400,進樣錐氣體流速(L/Hr)60,脫溶劑氣體流速(L/Hr)700 Ionization method: electrospray, polarity: positive ion, capillary (kV) 3.00, injection cone (V) 20.00, extractor (V) 3.00, source temperature (°C) 150, desolvation gas temperature (°C) 400, into Cone gas flow rate (L/Hr) 60, desolvation gas flow rate (L/Hr) 700
質量範圍:100至800Da,DAD波長範圍(nm):210至400 Mass range: 100 to 800 Da, DAD wavelength range (nm): 210 to 400
美商沃特斯(Waters)ACQUITY UPLC方法與下列HPLC梯度條件 American Waters ACQUITY UPLC Method with the following HPLC Gradient Conditions
(A溶劑:水/甲醇9:1,0.1%甲酸與B溶劑:乙腈,0.1%甲酸) (A solvent: water/methanol 9:1, 0.1% formic acid and B solvent: acetonitrile, 0.1% formic acid)
管柱類型:美商沃特斯(Waters)ACQUITY UPLC HSS T3;管柱長:30mm;管柱內徑:2.1mm;顆粒尺寸:1.8微 米;溫度:60℃。 Column type: American Waters ACQUITY UPLC HSS T3; column length: 30mm; column inner diameter: 2.1mm; particle size: 1.8 micro Rice; temperature: 60 ° C.
C方法:C method:
適用化合物A126至A139、A141至A145、B1至B11、C2至C3、D3至D7的LC-MS方法(正/負): LC-MS method (positive/negative) for the compounds A126 to A139, A141 to A145, B1 to B11, C2 to C3, D3 to D7:
美商沃特斯(Waters)的ZQ質譜儀(單一四極質譜儀) American Waters ZQ mass spectrometer (single quadrupole mass spectrometer)
儀器參數:離子化方法:電噴灑,極性:正離子與負離子 Instrument parameters: ionization method: electrospray, polarity: positive and negative ions
毛細管:3.00kV,進樣錐:30.00V,提取器:2.00V,來源溫度:100℃,脫溶劑氣溫度:250℃,進樣錐氣體流速:50L/Hr,脫溶劑氣體流速:400L/Hr,質量範圍:100至900Da Capillary: 3.00kV, injection cone: 30.00V, extractor: 2.00V, source temperature: 100 ° C, desolvation gas temperature: 250 ° C, injection cone gas flow rate: 50 L / Hr, desolvation gas flow rate: 400 L / Hr , mass range: 100 to 900Da
安捷倫(Agilent)公司的HP 1100 HPLC: Agilent's HP 1100 HPLC:
溶劑除氣劑、二元泵、加熱柱箱和二極管陣列檢測器。管柱:費諾美Gemini C18,3mm,30x3 mm,溫度:60℃,DAD波長範圍(nm):210至500 Solvent degassing agent, binary pump, heating oven and diode array detector. Column: Fernome Gemini C18, 3mm, 30x3 mm, temperature: 60 ° C, DAD wavelength range (nm): 210 to 500
溶劑梯度: Solvent gradient:
A=H2O+5%MeOH+0.05%HCOOH A=H2O+5% MeOH+0.05%HCOOH
B=乙腈+0.05%HCOOH B = acetonitrile + 0.05% HCOOH
D方法:D method:
適用化合物A140和A143的LC-MS方法(正/負): LC-MS method (positive/negative) for compounds A140 and A143:
美商沃特斯(Waters)的SQD質譜儀(單一四極質譜儀) American Waters SQD mass spectrometer (single quadrupole mass spectrometer)
儀器參數:離子化方法:電噴灑,極性:正離子與負離子,毛細管:3.00kV,進樣錐:30.00V,提取器:2.00V,來源溫度:150℃,脫溶劑氣溫度:250℃,進樣錐氣體流速:0L/Hr,脫溶劑氣體流速:650L/Hr,質量範圍:100至900Da Instrument parameters: ionization method: electric spraying, polarity: positive ion and negative ion, capillary: 3.00kV, injection cone: 30.00V, extractor: 2.00V, source temperature: 150 °C, desolvation gas temperature: 250 °C, advance Cone gas flow rate: 0L/Hr, desolvation gas flow rate: 650L/Hr, mass range: 100 to 900Da
美商沃特斯(Waters)的Acquity UPLC: Acquity UPLC from Waters:
二元泵、加熱柱箱和二極管陣列檢測器。 Binary pump, heated oven and diode array detector.
溶劑除氣劑、二元泵、加熱柱箱和二極管陣列檢測器。 Solvent degassing agent, binary pump, heating oven and diode array detector.
管柱:費諾美Gemini C18,3 mm,30 x 2 mm,溫度:60℃ Column: Fernome Gemini C18, 3 mm, 30 x 2 mm, temperature: 60 ° C
DAD波長範圍(nm):210至500 DAD wavelength range (nm): 210 to 500
溶劑梯度: Solvent gradient:
A=H2O+5%MeOH+0.05%HCOOH A=H2O+5% MeOH+0.05%HCOOH
B=乙腈+0.05%HCOOH B = acetonitrile + 0.05% HCOOH
此項說明式(I)之化合物的殺蟲特性測試的執行方式如下: This method of demonstrating the insecticidal properties of the compounds of formula (I) is carried out as follows:
埃及棉樹葉蟲(Spodoptera littoralis): Egyptian cotton leaf worm ( Spodoptera littoralis ):
將棉葉碟放置在24孔微量滴定盤裡的瓊脂上,並以200 ppm的施用率,用測試溶液噴灑。乾燥之後,以5 L1幼蟲感染葉碟。在處理3天(DAT)後,針對死亡率、攝食行為和生長調節情形,檢查樣本。 The cotton leaf disc was placed on agar in a 24-well microtiter plate and sprayed with the test solution at an application rate of 200 ppm. After drying, the leaf discs were infected with 5 L1 larvae. After 3 days of treatment (DAT), samples were examined for mortality, feeding behavior, and growth regulation.
下列化合物對埃及棉樹葉蟲(Spodoptera littoralis)產生至少80%的控制:A1、A3、A4、A5、A6、A8、A9、A10、A11、A13、A15、A16、A17、A22、A23、A25、A28、A30、A31、A32、A33至A36、A38至A40、A45至A51、A76、A56、A59、A77、A80、A82、A84、A85、A86、A87、A90、A91、A93、A94、A99、A101、A104、A105、A106、A111、A112、A115、A120、A122、A124、A126、A128、A129、A131、A132、133、A134、A135、A136、A137、A138、A143、A144、A145、B1、B2、B3、B4、B5、B6、B7、B8、B9、B10。 The following compounds produce at least 80% control of the Egyptian cotton leaf worm ( Sodoptera littoralis ): A1, A3, A4, A5, A6, A8, A9, A10, A11, A13, A15, A16, A17, A22, A23, A25, A28, A30, A31, A32, A33 to A36, A38 to A40, A45 to A51, A76, A56, A59, A77, A80, A82, A84, A85, A86, A87, A90, A91, A93, A94, A99, A101, A104, A105, A106, A111, A112, A115, A120, A122, A124, A126, A128, A129, A131, A132, 133, A134, A135, A136, A137, A138, A143, A144, A145, B1 B2, B3, B4, B5, B6, B7, B8, B9, B10.
菸夜蛾(Heliothis virescens):Heliothis virescens:
將蛋(蛋齡:0至24小時)放置在24孔微量滴定盤裡的人工飼料上,並利用移液管吸取的方式,以200ppm的施用率在蛋上施用測試溶液(孔中的濃度為18pm)。經過4天的 孵化期之後,針對蛋的死亡率、幼蟲的死亡率和生長調節情形,檢查樣本。 The eggs (aged age: 0 to 24 hours) were placed on the artificial feed in a 24-well microtiter plate, and the test solution was applied to the eggs at a rate of 200 ppm using a pipette suction method (the concentration in the well was 18pm). After 4 days After the incubation period, the samples were examined for egg mortality, larval mortality, and growth regulation.
下列化合物對菸夜蛾(Heliothis virescens)產生至少80%的控制:A1、A2、A3、A4、A5、A8、A9、A10、A11、A13、A14、A15、A16、A17、A19、A20、A22、A23、A25、A30、A31、A32、A33、A34、A36、A37、A38、A39、A40、A41、A42、A45、A46、A47、A48、A49、A50、A51、A76、A56、A57、A59、A61、A65、A68、A69、A72、A82、A86、A90、A101、A112、A115、A126、A128、A129、A130、A131、A132、133、A134、A135、A136、A137、A138、A139、A140、A142、A143、A144、A145、A146、A147、A149、A151、A157、A158、A159、A167、A168、A178、A180、A181、A182、A183、A184、A186、A187、A188、A189、A190、A192、A195、A196、A197、A198、A199、B1、B2、B3、B4、B5、B6、B7、B8、B9、B10。 The following compounds produce at least 80% control of Heliothis virescens: A1, A2, A3, A4, A5, A8, A9, A10, A11, A13, A14, A15, A16, A17, A19, A20, A22 , A23, A25, A30, A31, A32, A33, A34, A36, A37, A38, A39, A40, A41, A42, A45, A46, A47, A48, A49, A50, A51, A76, A56, A57, A59 , A61, A65, A68, A69, A72, A82, A86, A90, A101, A112, A115, A126, A128, A129, A130, A131, A132, 133, A134, A135, A136, A137, A138, A139, A140 , A142, A143, A144, A145, A146, A147, A149, A151, A157, A158, A159, A167, A168, A178, A180, A181, A182, A183, A184, A186, A187, A188, A189, A190, A192 , A195, A196, A197, A198, A199, B1, B2, B3, B4, B5, B6, B7, B8, B9, B10.
小菜蛾(Plutella xylostella):Plutella xylostella:
用移液器吸取的方式,在含有人工飼料的24孔微量滴定盤(MTP)裡,以200ppm的施用率來施用測試溶液(孔中的濃度為18ppm)。乾燥之後,L2幼蟲寄生於MTP上(每孔7至12隻)。經過6天的孵化期之後,針對幼蟲死亡率和生長調節情形,檢查樣本。 The test solution (concentration in the well was 18 ppm) was applied at a rate of 200 ppm in a 24-well microtiter plate (MTP) containing artificial feed by pipetting. After drying, the L2 larvae were parasitic on the MTP (7 to 12 per well). After a 6-day incubation period, samples were examined for larval mortality and growth regulation.
下列化合物對小菜蛾(Plutella xylostella)產生至少80%的控制:A1、A3、A4、A5、A6、A10、A12、A13、A15、 A22、A23、A25、A28、A31、A32、A33、A34、A35、A36、A38、A39、A40、A41、A42、A45、A46、A48、A49、A50、A51、A76、A56、A57、A59、A61、A79、A80、A83、A84、A86、A87、A90、A91、A93、A94、A95、A104、A106、A111、A112、A123、A126、A128、A129、A130、A131、A132、133、A134、A135、A136、A137、A138、A142、A143、A144、A145、A146、A151、A157、A159、A163、A168、A178、A181、A182、A183、A184、A188、A189、A192、A195、A197、A199、B1、B2、B3、B4、B5、B6、B7、B8、B9、B10。 The following compounds produce at least 80% control of Plutella xylostella: A1, A3, A4, A5, A6, A10, A12, A13, A15, A22, A23, A25, A28, A31, A32, A33, A34, A35, A36, A38, A39, A40, A41, A42, A45, A46, A48, A49, A50, A51, A76, A56, A57, A59, A61, A79, A80, A83, A84, A86, A87, A90, A91, A93, A94, A95, A104, A106, A111, A112, A123, A126, A128, A129, A130, A131, A132, 133, A134, A135, A136, A137, A138, A142, A143, A144, A145, A146, A151, A157, A159, A163, A168, A178, A181, A182, A183, A184, A188, A189, A192, A195, A197, A199, B1, B2, B3, B4, B5, B6, B7, B8, B9, B10.
玉米根蟲(Diabrotica balteata):Corn rootworm (Diabrotica balteata):
用移液器吸取的方式,在含有人工飼料的24孔微量滴定盤(MTP)裡,以200ppm的施用率來施用測試溶液(孔中的濃度為18 ppm)。乾燥之後,L2幼蟲寄生於MTP上(每孔6至10隻)。經過5天的孵化期之後,針對幼蟲死亡率和生長調節情形,檢查樣本。 The test solution (concentration in the well was 18 ppm) was applied at a rate of 200 ppm in a 24-well microtiter plate (MTP) containing artificial diet by pipetting. After drying, the L2 larvae are parasitic on the MTP (6 to 10 per well). After a 5-day incubation period, the samples were examined for larval mortality and growth regulation.
下列化合物對玉米根蟲(Diabrotica balteata)產生至少80%的控制:A1、A2、A3、A4、A5、A6、A10、A11、A12、A23、A30、A32、A33、A34、A35、A38、A39、A40、A42、A45、A46、A48、A49、A51、A76、A56、A57、A59、A61、A65、A68、A69、A80、A81、A82、A84、A87、A93、A101、A106、A109、A112、A115、A124、A126、A128、A129、A131、A132、133、A134、A135、A136、A137、A138、A143、 A144、A145、A146、A151、A157、A158、A159、A168、A175、A178、A180、A181、A182、A183、A184、A188、A189、A190、A191、A192、A195、A197、A198、A199、B1、B2、B3、B4、B5、B6、B7、B8、B9。 The following compounds produce at least 80% control of the corn rootworm (Diabrotica balteata): A1, A2, A3, A4, A5, A6, A10, A11, A12, A23, A30, A32, A33, A34, A35, A38, A39 , A40, A42, A45, A46, A48, A49, A51, A76, A56, A57, A59, A61, A65, A68, A69, A80, A81, A82, A84, A87, A93, A101, A106, A109, A112 , A115, A124, A126, A128, A129, A131, A132, 133, A134, A135, A136, A137, A138, A143, A144, A145, A146, A151, A157, A158, A159, A168, A175, A178, A180, A181, A182, A183, A184, A188, A189, A190, A191, A192, A195, A197, A198, A199, B1 B2, B3, B4, B5, B6, B7, B8, B9.
二點葉蟎(Tetranychus urticae):Tetranychus urticae:
以200ppm的施用率,在24孔微量滴定盤裡以測試溶液噴灑瓊脂上的豆葉碟。乾燥之後,葉碟寄生了不同蟲齡的蟎群。8天後,針對蛋的死亡率、幼蟲死亡率和成蟲死亡率,檢查了這些碟。 The bean leaf dish on the agar was sprayed with the test solution in a 24-well microtiter plate at an application rate of 200 ppm. After drying, the leaf discs parasitize the cockroaches of different ages. After 8 days, these dishes were examined for egg mortality, larval mortality, and adult mortality.
下列化合物對二點葉蟎(Tetranychus urticae)產生至少80%的控制:A1、A3、A4、A5、A6、A31、A45、A46、A48、A49、A76、A80、A81、A82、A86、A90、A100、A101、A109、A110、A115、A124、A126、A128、A129、A132、A136、A143、A144、A145、B3、B4、B5、B6、B7、B9、B10。 The following compounds produce at least 80% control of Tetranychus urticae: A1, A3, A4, A5, A6, A31, A45, A46, A48, A49, A76, A80, A81, A82, A86, A90, A100, A101, A109, A110, A115, A124, A126, A128, A129, A132, A136, A143, A144, A145, B3, B4, B5, B6, B7, B9, B10.
蔥薊馬(Thrips tabaci):Thrips tabaci:
將向日葵葉碟放置在24孔微量滴定盤裡的瓊脂上,並以200ppm的施用率,用測試溶液噴灑。乾燥之後,葉碟寄生了不同蟲齡的蚜蟲群。經過7天的孵化期之後,針對死亡率檢查樣本。 The sunflower leaf discs were placed on agar in a 24-well microtiter plate and sprayed with the test solution at an application rate of 200 ppm. After drying, the leaf discs parasitize the locust swarms of different ages. After a 7-day incubation period, the samples were examined for mortality.
下列化合物對蔥薊馬(Thrips tabaci)產生至少80%的控制:A4、A5、A10、A11、A23、A25、A33、A34、A36、 A40、A42、A45、A46、A48、A49、A50、A56、A80、A82、A84、A86、A94、A100、A101、A111、A112、A124、A126、A128、A132、A134、A137、A143、A168、B1、B2、B3、B4、B5、B6、B9。 The following compounds produce at least 80% control of Thrips tabaci: A4, A5, A10, A11, A23, A25, A33, A34, A36, A40, A42, A45, A46, A48, A49, A50, A56, A80, A82, A84, A86, A94, A100, A101, A111, A112, A124, A126, A128, A132, A134, A137, A143, A168, B1, B2, B3, B4, B5, B6, B9.
桃蚜(Myzus persicae):Myzus persicae:
將向日葵葉碟放置在24孔微量滴定盤裡的瓊脂上,並以200ppm的施用率,用測試溶液噴灑。乾燥之後,葉碟寄生了不同蟲齡的蚜蟲群。經過6天的孵化期之後,針對死亡率檢查樣本。 The sunflower leaf discs were placed on agar in a 24-well microtiter plate and sprayed with the test solution at an application rate of 200 ppm. After drying, the leaf discs parasitize the locust swarms of different ages. After a 6-day incubation period, the samples were examined for mortality.
下列化合物對桃蚜(Myzus persicae)產生至少80%的控制:A46、A128、A132、A135、A137、B1、B2、B3、B4、B5、B9、B10。 The following compounds produced at least 80% control of Myzus persicae: A46, A128, A132, A135, A137, B1, B2, B3, B4, B5, B9, B10.
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| CN111925363A (en) * | 2019-05-13 | 2020-11-13 | 东莞市东阳光农药研发有限公司 | 4-amino furan-2 (5H) ketone derivative and preparation method and application thereof |
| CN116918808A (en) * | 2022-03-30 | 2023-10-24 | 沈阳恩柽研究院有限公司 | Application of fatty diacid ester compound |
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| CN111925363A (en) * | 2019-05-13 | 2020-11-13 | 东莞市东阳光农药研发有限公司 | 4-amino furan-2 (5H) ketone derivative and preparation method and application thereof |
| CN111925363B (en) * | 2019-05-13 | 2024-01-16 | 东莞市东阳光农药研发有限公司 | 4-aminofuran-2 (5H) ketone derivative and preparation method and application thereof |
| CN116918808A (en) * | 2022-03-30 | 2023-10-24 | 沈阳恩柽研究院有限公司 | Application of fatty diacid ester compound |
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