TW202005533A - 包含吲唑之殺蟲混合物 - Google Patents
包含吲唑之殺蟲混合物 Download PDFInfo
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- TW202005533A TW202005533A TW108124649A TW108124649A TW202005533A TW 202005533 A TW202005533 A TW 202005533A TW 108124649 A TW108124649 A TW 108124649A TW 108124649 A TW108124649 A TW 108124649A TW 202005533 A TW202005533 A TW 202005533A
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- 239000000203 mixture Substances 0.000 title claims abstract description 172
- 150000002473 indoazoles Chemical class 0.000 title description 3
- 230000000361 pesticidal effect Effects 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 200
- 241000607479 Yersinia pestis Species 0.000 claims abstract description 119
- 238000000034 method Methods 0.000 claims abstract description 60
- 229940125904 compound 1 Drugs 0.000 claims abstract description 46
- -1 anarinathrin Chemical compound 0.000 claims description 87
- 239000003085 diluting agent Substances 0.000 claims description 39
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- 239000003795 chemical substances by application Substances 0.000 claims description 32
- NYPJDWWKZLNGGM-UHFFFAOYSA-N fenvalerate Aalpha Natural products C=1C=C(Cl)C=CC=1C(C(C)C)C(=O)OC(C#N)C(C=1)=CC=CC=1OC1=CC=CC=C1 NYPJDWWKZLNGGM-UHFFFAOYSA-N 0.000 claims description 28
- 239000004094 surface-active agent Substances 0.000 claims description 27
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- 241000700605 Viruses Species 0.000 claims description 16
- 241000894006 Bacteria Species 0.000 claims description 13
- DVBUIBGJRQBEDP-UHFFFAOYSA-N cyantraniliprole Chemical compound CNC(=O)C1=CC(C#N)=CC(C)=C1NC(=O)C1=CC(Br)=NN1C1=NC=CC=C1Cl DVBUIBGJRQBEDP-UHFFFAOYSA-N 0.000 claims description 13
- WCXDHFDTOYPNIE-RIYZIHGNSA-N (E)-acetamiprid Chemical compound N#C/N=C(\C)N(C)CC1=CC=C(Cl)N=C1 WCXDHFDTOYPNIE-RIYZIHGNSA-N 0.000 claims description 11
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- IBSREHMXUMOFBB-JFUDTMANSA-N 5u8924t11h Chemical compound O1[C@@H](C)[C@H](O)[C@@H](OC)C[C@@H]1O[C@@H]1[C@@H](OC)C[C@H](O[C@@H]2C(=C/C[C@@H]3C[C@@H](C[C@@]4(O3)C=C[C@H](C)[C@@H](C(C)C)O4)OC(=O)[C@@H]3C=C(C)[C@@H](O)[C@H]4OC\C([C@@]34O)=C/C=C/[C@@H]2C)/C)O[C@H]1C.C1=C[C@H](C)[C@@H]([C@@H](C)CC)O[C@]11O[C@H](C\C=C(C)\[C@@H](O[C@@H]2O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C2)[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\2)O)C[C@H]4C1 IBSREHMXUMOFBB-JFUDTMANSA-N 0.000 claims description 10
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- QQODLKZGRKWIFG-QSFXBCCZSA-N cyfluthrin Chemical compound CC1(C)[C@@H](C=C(Cl)Cl)[C@H]1C(=O)O[C@@H](C#N)C1=CC=C(F)C(OC=2C=CC=CC=2)=C1 QQODLKZGRKWIFG-QSFXBCCZSA-N 0.000 claims description 10
- HJUFTIJOISQSKQ-UHFFFAOYSA-N fenoxycarb Chemical compound C1=CC(OCCNC(=O)OCC)=CC=C1OC1=CC=CC=C1 HJUFTIJOISQSKQ-UHFFFAOYSA-N 0.000 claims description 10
- CFRPSFYHXJZSBI-DHZHZOJOSA-N (E)-nitenpyram Chemical compound [O-][N+](=O)/C=C(\NC)N(CC)CC1=CC=C(Cl)N=C1 CFRPSFYHXJZSBI-DHZHZOJOSA-N 0.000 claims description 9
- IQVNEKKDSLOHHK-FNCQTZNRSA-N (E,E)-hydramethylnon Chemical compound N1CC(C)(C)CNC1=NN=C(/C=C/C=1C=CC(=CC=1)C(F)(F)F)\C=C\C1=CC=C(C(F)(F)F)C=C1 IQVNEKKDSLOHHK-FNCQTZNRSA-N 0.000 claims description 9
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- INISTDXBRIBGOC-CGAIIQECSA-N [cyano-(3-phenoxyphenyl)methyl] (2s)-2-[2-chloro-4-(trifluoromethyl)anilino]-3-methylbutanoate Chemical compound N([C@@H](C(C)C)C(=O)OC(C#N)C=1C=C(OC=2C=CC=CC=2)C=CC=1)C1=CC=C(C(F)(F)F)C=C1Cl INISTDXBRIBGOC-CGAIIQECSA-N 0.000 claims description 9
- VEHPJKVTJQSSKL-UHFFFAOYSA-N azadirachtin Natural products O1C2(C)C(C3(C=COC3O3)O)CC3C21C1(C)C(O)C(OCC2(OC(C)=O)C(CC3OC(=O)C(C)=CC)OC(C)=O)C2C32COC(C(=O)OC)(O)C12 VEHPJKVTJQSSKL-UHFFFAOYSA-N 0.000 claims description 9
- FTNJWQUOZFUQQJ-NDAWSKJSSA-N azadirachtin A Chemical compound C([C@@H]([C@]1(C=CO[C@H]1O1)O)[C@]2(C)O3)[C@H]1[C@]23[C@]1(C)[C@H](O)[C@H](OC[C@@]2([C@@H](C[C@@H]3OC(=O)C(\C)=C\C)OC(C)=O)C(=O)OC)[C@@H]2[C@]32CO[C@@](C(=O)OC)(O)[C@@H]12 FTNJWQUOZFUQQJ-NDAWSKJSSA-N 0.000 claims description 9
- FTNJWQUOZFUQQJ-IRYYUVNJSA-N azadirachtin A Natural products C([C@@H]([C@]1(C=CO[C@H]1O1)O)[C@]2(C)O3)[C@H]1[C@]23[C@]1(C)[C@H](O)[C@H](OC[C@@]2([C@@H](C[C@@H]3OC(=O)C(\C)=C/C)OC(C)=O)C(=O)OC)[C@@H]2[C@]32CO[C@@](C(=O)OC)(O)[C@@H]12 FTNJWQUOZFUQQJ-IRYYUVNJSA-N 0.000 claims description 9
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- KAATUXNTWXVJKI-UHFFFAOYSA-N cypermethrin Chemical compound CC1(C)C(C=C(Cl)Cl)C1C(=O)OC(C#N)C1=CC=CC(OC=2C=CC=CC=2)=C1 KAATUXNTWXVJKI-UHFFFAOYSA-N 0.000 claims description 9
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- VJFUPGQZSXIULQ-XIGJTORUSA-N pyrethrin II Chemical compound CC1(C)[C@H](/C=C(\C)C(=O)OC)[C@H]1C(=O)O[C@@H]1C(C)=C(C\C=C/C=C)C(=O)C1 VJFUPGQZSXIULQ-XIGJTORUSA-N 0.000 claims description 9
- DWFZBUWUXWZWKD-UHFFFAOYSA-N pyridaben Chemical compound C1=CC(C(C)(C)C)=CC=C1CSC1=C(Cl)C(=O)N(C(C)(C)C)N=C1 DWFZBUWUXWZWKD-UHFFFAOYSA-N 0.000 claims description 9
- AEHJMNVBLRLZKK-UHFFFAOYSA-N pyridalyl Chemical group N1=CC(C(F)(F)F)=CC=C1OCCCOC1=C(Cl)C=C(OCC=C(Cl)Cl)C=C1Cl AEHJMNVBLRLZKK-UHFFFAOYSA-N 0.000 claims description 9
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- QSOHVSNIQHGFJU-UHFFFAOYSA-L thiosultap disodium Chemical compound [Na+].[Na+].[O-]S(=O)(=O)SCC(N(C)C)CSS([O-])(=O)=O QSOHVSNIQHGFJU-UHFFFAOYSA-L 0.000 claims description 9
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- ZXQYGBMAQZUVMI-RDDWSQKMSA-N (1S)-cis-(alphaR)-cyhalothrin Chemical compound CC1(C)[C@H](\C=C(/Cl)C(F)(F)F)[C@@H]1C(=O)O[C@@H](C#N)C1=CC=CC(OC=2C=CC=CC=2)=C1 ZXQYGBMAQZUVMI-RDDWSQKMSA-N 0.000 claims description 8
- LZTIMERBDGGAJD-SNAWJCMRSA-N (2e)-2-(nitromethylidene)-1,3-thiazinane Chemical compound [O-][N+](=O)\C=C1/NCCCS1 LZTIMERBDGGAJD-SNAWJCMRSA-N 0.000 claims description 8
- PGOOBECODWQEAB-UHFFFAOYSA-N (E)-clothianidin Chemical compound [O-][N+](=O)\N=C(/NC)NCC1=CN=C(Cl)S1 PGOOBECODWQEAB-UHFFFAOYSA-N 0.000 claims description 8
- HOKKPVIRMVDYPB-UVTDQMKNSA-N (Z)-thiacloprid Chemical compound C1=NC(Cl)=CC=C1CN1C(=N/C#N)/SCC1 HOKKPVIRMVDYPB-UVTDQMKNSA-N 0.000 claims description 8
- ZDOOQPFIGYHZFV-UHFFFAOYSA-N 2-ethyl-4-[(4-phenoxyphenoxy)methyl]-1,3-dioxolane Chemical compound O1C(CC)OCC1COC(C=C1)=CC=C1OC1=CC=CC=C1 ZDOOQPFIGYHZFV-UHFFFAOYSA-N 0.000 claims description 8
- ZOCSXAVNDGMNBV-UHFFFAOYSA-N 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile Chemical compound NC1=C(S(=O)C(F)(F)F)C(C#N)=NN1C1=C(Cl)C=C(C(F)(F)F)C=C1Cl ZOCSXAVNDGMNBV-UHFFFAOYSA-N 0.000 claims description 8
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- JFLRKDZMHNBDQS-UCQUSYKYSA-N CC[C@H]1CCC[C@@H]([C@H](C(=O)C2=C[C@H]3[C@@H]4C[C@@H](C[C@H]4C(=C[C@H]3[C@@H]2CC(=O)O1)C)O[C@H]5[C@@H]([C@@H]([C@H]([C@@H](O5)C)OC)OC)OC)C)O[C@H]6CC[C@@H]([C@H](O6)C)N(C)C.CC[C@H]1CCC[C@@H]([C@H](C(=O)C2=C[C@H]3[C@@H]4C[C@@H](C[C@H]4C=C[C@H]3C2CC(=O)O1)O[C@H]5[C@@H]([C@@H]([C@H]([C@@H](O5)C)OC)OC)OC)C)O[C@H]6CC[C@@H]([C@H](O6)C)N(C)C Chemical compound CC[C@H]1CCC[C@@H]([C@H](C(=O)C2=C[C@H]3[C@@H]4C[C@@H](C[C@H]4C(=C[C@H]3[C@@H]2CC(=O)O1)C)O[C@H]5[C@@H]([C@@H]([C@H]([C@@H](O5)C)OC)OC)OC)C)O[C@H]6CC[C@@H]([C@H](O6)C)N(C)C.CC[C@H]1CCC[C@@H]([C@H](C(=O)C2=C[C@H]3[C@@H]4C[C@@H](C[C@H]4C=C[C@H]3C2CC(=O)O1)O[C@H]5[C@@H]([C@@H]([C@H]([C@@H](O5)C)OC)OC)OC)C)O[C@H]6CC[C@@H]([C@H](O6)C)N(C)C JFLRKDZMHNBDQS-UCQUSYKYSA-N 0.000 claims description 8
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- FNELVJVBIYMIMC-UHFFFAOYSA-N Ethiprole Chemical compound N1=C(C#N)C(S(=O)CC)=C(N)N1C1=C(Cl)C=C(C(F)(F)F)C=C1Cl FNELVJVBIYMIMC-UHFFFAOYSA-N 0.000 claims description 8
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- QQODLKZGRKWIFG-RUTXASTPSA-N [(R)-cyano-(4-fluoro-3-phenoxyphenyl)methyl] (1S)-3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropane-1-carboxylate Chemical compound CC1(C)C(C=C(Cl)Cl)[C@@H]1C(=O)O[C@@H](C#N)C1=CC=C(F)C(OC=2C=CC=CC=2)=C1 QQODLKZGRKWIFG-RUTXASTPSA-N 0.000 claims description 8
- KVIZNNVXXNFLMU-AIIUZBJTSA-N [2,3,5,6-tetrafluoro-4-(methoxymethyl)phenyl]methyl (1r,3r)-2,2-dimethyl-3-[(e)-prop-1-enyl]cyclopropane-1-carboxylate Chemical compound FC1=C(F)C(COC)=C(F)C(F)=C1COC(=O)[C@H]1C(C)(C)[C@@H]1\C=C\C KVIZNNVXXNFLMU-AIIUZBJTSA-N 0.000 claims description 8
- ZVQOOHYFBIDMTQ-UHFFFAOYSA-N [methyl(oxido){1-[6-(trifluoromethyl)pyridin-3-yl]ethyl}-lambda(6)-sulfanylidene]cyanamide Chemical compound N#CN=S(C)(=O)C(C)C1=CC=C(C(F)(F)F)N=C1 ZVQOOHYFBIDMTQ-UHFFFAOYSA-N 0.000 claims description 8
- RRZXIRBKKLTSOM-XPNPUAGNSA-N avermectin B1a Chemical compound C1=C[C@H](C)[C@@H]([C@@H](C)CC)O[C@]11O[C@H](C\C=C(C)\[C@@H](O[C@@H]2O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C2)[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\2)O)C[C@H]4C1 RRZXIRBKKLTSOM-XPNPUAGNSA-N 0.000 claims description 8
- OMFRMAHOUUJSGP-IRHGGOMRSA-N bifenthrin Chemical compound C1=CC=C(C=2C=CC=CC=2)C(C)=C1COC(=O)[C@@H]1[C@H](\C=C(/Cl)C(F)(F)F)C1(C)C OMFRMAHOUUJSGP-IRHGGOMRSA-N 0.000 claims description 8
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
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- FJBGIXKIXPUXBY-UHFFFAOYSA-N {2-[3-(4-chlorophenyl)propyl]-2,4,4-trimethyl-1,3-oxazolidin-3-yl}(imidazol-1-yl)methanone Chemical compound C1=CN=CN1C(=O)N1C(C)(C)COC1(C)CCCC1=CC=C(Cl)C=C1 FJBGIXKIXPUXBY-UHFFFAOYSA-N 0.000 description 1
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
- A01N43/50—1,3-Diazoles; Hydrogenated 1,3-diazoles
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
- A01N43/56—1,2-Diazoles; Hydrogenated 1,2-diazoles
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
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- Agronomy & Crop Science (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
所揭示的是化合物1及式2化合物,
Description
本發明關於某些經取代吲唑、其等適用於農藝及非農藝用途之組成物、以及其等在農藝及非農藝環境兩者中防制無脊椎動物害蟲(諸如節肢動物)之方法。
無脊椎動物害蟲之防制對於達成高作物效率而言極為重要。無脊椎動物害蟲對生長中及儲存農藝作物之損害會造成生產力顯著下降,因而導致消費者的成本增加。在林業、溫室作物、觀賞植物、苗圃作物、儲存食物與纖維產物、家畜產物、家用產物、草皮產物、木材產物、及公共衛生與動物健康中,無脊椎動物害蟲之防制亦相當重要。許多產品對於這些用途而言皆為可商購獲得的,但對於更有效、成本更低、毒性更低、對環境更安全、或具有不同作用部位之新穎化合物仍持續有需求。PCT申請案公開案WO 2015/038503 A1揭示相關之吲唑化合物。
本發明亦提供一種組成物,其包含化合物1或式2化合物、或任何前述化合物之組合。
本發明亦提供一種組成物,其包含化合物1或式2化合物、及至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外組分。在一個實施例中,本發明亦提供一種用於防制無脊椎動物害蟲之組成物,其包含化合物1或式2化合物、及至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外組分,該組成物可選地進一步包含至少一種額外生物活性化合物或藥劑。
本發明提供一種防制無脊椎動物害蟲之方法,其包含使該無脊椎動物害蟲或其環境與生物有效量的化合物1或式2化合物(例如,以本文中所述之組成物)接觸。本發明亦關於此種方法,其中使該無脊椎動物害蟲或其環境與包含生物有效量的化合物1或式2化合物、及至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外組分之組成物接觸,該組成物可選地進一步包含生物有效量的至少一種額外生物活性化合物或藥劑。
本發明亦提供一種用於保護種子免受無脊椎動物害蟲侵害之方法,其包含使該種子與生物有效量的化合物1或式2化合物(例如,以本文所述之組成物)接觸。本發明亦關於經處理之種子。
[相關申請案之交互參照]
本申請案主張美國專利臨時申請案第62/698,035號(於2018年7月14日提出申請)及美國臨時專利申請案第62/778,992號(於2018年12月13日提出申請)之優先權。
如本文中所使用,用語「包含(comprises/comprising)」、「包括(includes/including)」、「具有(has/having)」、「含有(contains/containing)」、「特徵在於(characterized by)」、或其等之任何其他變型係意欲涵蓋非排他性的涵括,並且受到任何明示指出之限制所規範。例如,包含要件列表之組成物、混合物、程序、或方法不一定僅限於此等要件,但可以包括未明示列出之要件或者此等組成物、混合物、程序、或方法所固有之其他要件。
連接詞「由......組成(consisting of)」排除未指定之任何要件、步驟、或成分。如果在申請專利範圍中,如此會使申請專利範圍封閉,而不包括除了原本與其相關聯之雜質以外的材料。當該詞「由......組成」出現在申請專利範圍之主體的子句中而非緊接在前言後面時,其只限制該子句中所提出之要件;不將其他要件從整體申請專利範圍排除。
除了字面上所揭示者,連接詞「基本上由...組成(consisting essentially of)」係用以界定包括材料、步驟、特徵、組分、或要件的組成物或方法,前提是這些額外材料、步驟、特徵、組分、或要件不會影響所請求發明之基本及新穎特徵。用語「基本上由......組成」居於「包含」與「由......組成」之間的中間地帶。
若申請人已使用開放式用語如「包含」來定義一發明或其一部分,則應輕易瞭解到(除非另有陳述)該描述應解讀為亦使用用語「基本上由......組成」或「由......組成」來描述此一發明。
再者,除非明示相反說明,「或(or)」係指包括性的「或」而非排他性的「或」。例如,下列任一者皆滿足條件A或B:A為真(或存在)且B為偽(或不存在)、A為偽(或不存在)且B為真(或存在)、及A及B兩者皆為真(或存在)。
並且,在本發明之要件或組分前面的不定冠詞「一(a/an)」係意欲就該要件或組件之示例(即,發生)次數而言係非限制性的。因此,「一(a/an)」應理解為包括一個/種或至少一個/種,並且要件或組件之單數字形亦包括複數,除非數目明顯意指單數。
如本揭露中所指稱,用語「無脊椎動物害蟲(invertebrate pest)」包括作為害蟲具有經濟上重要性之節肢動物、腹足動物、線蟲、及蠕蟲。用語「節肢動物(arthropod)」包括昆蟲、蟎、蜘蛛、蠍子、蜈蚣、馬陸、鼠婦(pill bug)、及節足蟲(symphylan)。用語「腹足動物(gastropod)」包括蝸牛、蛞蝓、及其他柄眼目動物(Stylommatophora)。用語「線蟲(nematode)」包括線形動物門(phylum Nematoda)之成員,例如植食性線蟲及蠕蟲線蟲寄生動物。用語「蠕蟲(helminth)」包括所有寄生蟲,諸如蛔蟲(線形動物門)、心絲蟲(線形動物門,胞管腎(Secernentea)綱)、吸蟲(扁形動物門(phylum Platyhelminthes),吸蟲(Tematoda)綱)、棘頭蟲(棘頭動物門(phylum Acanthocephala))、及條蟲(扁形動物門,絛蟲(Cestoda)綱)。
在本發明揭露之上下文中,「無脊椎動物害蟲防制(invertebrate pest control)」意指無脊椎動物害蟲發育之抑制(包括死亡、攝食減少、及/或交配干擾),並且相關表述係以類似方式定義。
用語「農藝(agronomic)」意指田間作物之生產(諸如針對食物及纖維),並且包括玉蜀黍或玉米、大豆與其他豆科植物、稻米、穀物(例如,小麥、燕麥、大麥、黑麥、及稻米)、葉菜類(例如,萵苣、甘藍、及其他芸苔屬作物)、果菜類(例如,番茄、辣椒、茄子、十字花科植物、及瓜類)、馬鈴薯、甘藷、葡萄、棉花、樹果類(例如,梨果、核果、及柑橘)、小型水果(莓果、及櫻桃)、及其他特種作物(例如,芥花、向日葵、及橄欖)。
用語「非農藝(nonagronomic)」意指田間作物以外之應用,諸如園藝作物(例如,非生長於田間之溫室植物、苗圃植物、或觀賞植物)、住宅、農業、商業、及工業結構物、草皮(例如,草皮田地、牧草地、高爾夫球場、草坪、運動場等)、木材產品、積存產物、農林業與植生管理、公共衛生(即,人類)及動物健康(例如,馴養動物如寵物、家畜、及家禽、非馴養動物如野生動物)。
用語「作物生長力(crop vigor)」係指作物植物之生長速率或生物量累積速率。「生長力增加(increase in vigor)」係指相對於未經處理之對照作物植物而言,作物植物之生長或生物量累積有所增加。用語「作物產出(crop yield)」係指在收成作物植物後所獲得之作物物料收益(就數量與品質兩者而言)。「作物產出增加(increase in crop yield)」係指相對於未經處理之對照作物植物而言,作物產出有所增加。
用語「生物有效量(biologically effective amount)」係指生物活性化合物(例如,化合物1或式2化合物)當施用至(即,接觸)待防制之無脊椎動物害蟲或其環境、或施用至植物、生長出該植物之種子、或該植物之所在地(例如,生長介質)以保護該植物免受無脊椎動物害蟲傷害或用於其他所欲效果(例如,增加植物生長力)時,足以產生所欲生物效果之量。
如發明內容中所述之本發明的實施例包括以下所述者。
實施例1. 一種化合物1。
實施例2.一種式2化合物,其中n係0、1、或2
實施例3.一種式2化合物,其中n係0。
實施例4.一種式2化合物,其中n係1。
實施例5.一種式2化合物,其中n係2。
實施例6.一種化合物,其中該化合物係選自N
-[1-(二氟甲基)環丙基]-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺;N
-[1,1-二甲基-2-(甲基硫基)乙基]-7-氟-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺;N
-[1,1-二甲基-2-(甲基亞磺醯基)乙基]-7-氟-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺;及N
-[1,1-二甲基-2-(甲基磺醯基)乙基]-7-氟-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺;或任何前述化合物之組合。
實施例7.一種組成物,其包含化合物1或式2化合物及至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外組分,該組成物可選地進一步包含至少一種額外生物活性化合物或藥劑。
實施例8.一種組成物,其包含化合物1或式2化合物及至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外組分,該組成物可選地進一步包含至少一種額外生物活性化合物或藥劑,其中該至少一種額外生物活性化合物或藥劑係選自於由下列所組成之群組:阿巴汀(abamectin)、毆殺松(acephate)、亞醌蟎(acequinocyl)、亞滅培(acetamiprid)、阿納寧(acrinathrin)、雙丙環蟲脂(afidopyropen)、磺胺蟎酯(amidoflumet)、三亞蹣(amitraz)、阿維菌素(avermectin)、印楝素(azadirachtin)、谷速松(azinphos-methyl)、免扶克(benfuracarb)、免速達(bensultap)、畢芬寧(bifenthrin)、必芬蟎(bifenazate)、雙三氟蟲脲(bistrifluron)、硼酸酯(borate)、布芬淨(buprofezin)、加保利(carbaryl)、加保扶(carbofuran)、培丹(cartap)、殺蟲脒(carzol)、賽速安勃(chlorantraniliprole)、克凡派(chlorfenapyr)、克福隆(chlorfluazuron)、陶斯松(chlorpyrifos)、甲基陶斯松(chlorpyrifos-methyl)、可芬諾(chromafenozide)、克芬蟎(clofentezin)、可尼丁(clothianidin)、氰蟲醯胺(cyantraniliprole)、環溴蟲醯胺(cyclaniliprole)、乙氰菊酯(cycloprothrin)、環氧蟲啶(cycloxaprid)、賽芬蟎(cyflumetofen)、賽扶寧(cyfluthrin)、貝他賽扶寧(beta-cyfluthrin)、賽洛寧(cyhalothrin)、伽瑪賽洛寧(gamma-cyhalothrin)、拉目達賽洛寧(lambda-cyhalothrin)、賽滅寧(cypermethrin)、亞滅寧(alpha-cypermethrin)、傑他賽滅寧(zeta-cypermethrin)、賽滅淨(cyromazine)、第滅寧(deltamethrin)、汰芬隆(diafenthiuron)、大利松(diazinon)、地特靈(dieldrin)、二福隆(diflubenzuron)、四氟甲醚菊酯(dimefluthrin)、殺蟲雙(dimehypo)、大滅松(dimethoate)、達特南(dinotefuran)、苯蟲醚(diofenolan)、因滅汀(emamectin)、安殺番(endosulfan)、益化利(esfenvalerate)、益斯普(ethiprole)、依芬寧(etofenprox)、依殺蟎(etoxazole)、芬佈賜(fenbutatin oxide)、撲滅松(fenitrothion)、芬硫克(fenothiocarb)、芬諾克(fenoxycarb)、芬普寧(fenpropathrin)、芬化利(fenvalerate)、芬普尼(fipronil)、弗美托奎(flometoquin)、氟尼胺(flonicamid)、氟大滅(flubendiamide)、護賽寧(flucythrinate)、嘧蟲胺(flufenerim)、氟芬隆(flufenoxuron)、氟菌蟎酯(flufenoxystrobin)、弗芬梭分(flufensulfone)、氟吡菌醯胺(fluorpyram)、弗皮洛(flupiprole)、氟吡呋喃酮(flupyradifurone)、福化利(fluvalinate)、氟胺氰菊酯(tau-fluvalinate)、大福松(fonophos)、覆滅蟎(formetanate)、福賽絕(fosthiazate)、合芬隆(halofenozide)、右旋七氟甲醚菊酯(heptafluthrin)、六伏隆(hexaflumuron)、合賽多(hexythiazox)、愛美松(hydramethylnon)、益達胺(imidacloprid)、因得克(indoxacarb)、殺蟲皂(insecticidal soaps)、亞芬松(isofenphos)、祿芬隆(lufenuron)、馬拉松(malathion)、氯氟醚菊酯(meperfluthrin)、美氟綜(metaflumizone)、聚乙醛(metaldehyde)、達馬松(methamidophos)、滅大松(methidathion)、滅蟲威(methiodicarb)、納乃得(methomyl)、美賜平(methoprene)、甲氧滴滴梯(methoxychlor)、美特寧(metofluthrin)、亞素靈(monocrotophos)、單福寧(monofluthrin)、滅芬諾(methoxyfenozide)、烯啶蟲胺(nitenpyram)、硝蟲噻嗪(nithiazine)、諾伐隆(novaluron)、諾福隆(noviflumuron)、毆殺滅(oxamyl)、巴拉松(parathion)、甲基巴拉松(parathion-methyl)、百滅寧(permethrin)、福瑞松(phorate)、裕必松(phosalone)、益滅松(phosmet)、福賜米松(phosphamidon)、比加普(pirimicarb)、佈飛松(profenofos)、丙氟菊酯(profluthrin)、毆蟎多(propargite)、丙苯烴菊酯(protrifenbute)、吡氟布米得(pyflubumide)、派滅淨(pymetrozine)、啶吡唑蟲胺(pyrafluprole)、除蟲菊素(pyrethrin)、畢達本(pyridaben)、啶蟲丙醚(pyridalyl)、吡立芙淇納蔥(pyrifluquinazon)、嘧蟎胺(pyriminostrobin)、pyriprole、百利普芬(pyriproxyfen)、魚藤酮(rotenone)、蘭諾定(ryanodine)、矽護芬(silafluofen)、賜諾特(spinetoram)、賜諾殺(spinosad)、賜派芬(spirodiclofen)、賜滅芬(spiromesifen)、賜派滅(spirotetramat)、硫丙磷(sulprofos)、速殺氟(sulfoxaflor)、得芬諾(tebufenozide)、得芬瑞(tebufenpyrad)、得福隆(teflubenzuron)、七氟菊酯(tefluthrin)、托福松(terbufos)、樂本松(tetrachlorvinphos)、治滅寧(tetramethrin)、四氟醚菊酯(tetramethylfluthrin)、賽果培(thiacloprid)、賽速安(thiamethoxam)、硫敵克(thiodicarb)、殺蟲單(thiosultap-sodium)、脫芬瑞(tolfenpyrad)、泰滅寧(tralomethrin)、唑蚜威(triazamate)、三氯松(trichlorfon)、三福隆(triflumuron)、蘇力菌(Bacillus thuringiensis
)之所有品系、昆蟲病原細菌(entomopathogenic bacteria)、核多角體病毒(Nucleo polyhedrosis
viruses)之所有品系、昆蟲病原病毒(entomopathogenic viruses)、及昆蟲病原真菌(entomopathogenic fungi)。
實施例9.一種組成物,其包含化合物1或式2化合物及至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外組分,該組成物可選地進一步包含至少一種額外生物活性化合物或藥劑,其中該至少一種額外生物活性化合物或藥劑係選自於由下列所組成之群組:阿巴汀(abamectin)、亞滅培(acetamiprid)、阿納寧(acrinathrin)、雙丙環蟲脂(afidopyropen)、三亞蹣(amitraz)、阿維菌素(avermectin)、印楝素(azadirachtin)、免扶克(benfuracarb)、免速達(bensultap)、畢芬寧(bifenthrin)、3-溴-1-(3-氯-2-吡啶基)-N
-[4-氰基-2-甲基-6-[(甲基胺基)羰基]苯基]-1H
-吡唑-5-甲醯胺、布芬淨(buprofezin)、加保利(carbaryl)、培丹(cartap)、賽速安勃(chlorantraniliprole)、克凡派(chlorfenapyr)、陶斯松(chlorpyrifos)、可尼丁(clothianidin)、氰蟲醯胺(cyantraniliprole)、環溴蟲醯胺(cyclaniliprole)、乙氰菊酯(cycloprothrin)、賽扶寧(cyfluthrin)、貝他賽扶寧(beta-cyfluthrin)、賽洛寧(cyhalothrin)、拉目達賽洛寧(lambda-cyhalothrin)、伽瑪賽洛寧(gamma-cyhalothrin)、賽滅寧(cypermethrin)、亞滅寧(alpha-cypermethrin)、傑他賽滅寧(zeta-cypermethrin)、賽滅淨(cyromazine)、第滅寧(deltamethrin)、地特靈(dieldrin)、達特南(dinotefuran)、苯蟲醚(diofenolan)、因滅汀(emamectin)、安殺番(endosulfan)、益化利(esfenvalerate)、益斯普(ethiprole)、依芬寧(etofenprox)、依殺蟎(etoxazole)、撲滅松(fenitrothion)、芬硫克(fenothiocarb)、芬諾克(fenoxycarb)、芬化利(fenvalerate)、芬普尼(fipronil)、弗美托奎(flometoquin)、氟尼胺(flonicamid)、氟大滅(flubendiamide)、弗芬梭分(flufensulfone)、氟菌蟎酯(flufenoxystrobin)、氟速芬(fluensulfone)、弗皮洛(flupiprole)、氟吡呋喃酮(flupyradifurone)、福化利(fluvalinate)、覆滅蟎(formetanate)、福賽絕(fosthiazate)、右旋七氟甲醚菊酯(heptafluthrin)、六伏隆(hexaflumuron)、愛美松(hydramethylnon)、益達胺(imidacloprid)、因得克(indoxacarb)、祿芬隆(lufenuron)、氯氟醚菊酯(meperfluthirn)、美氟綜(metaflumizone)、滅蟲威(methiodicarb)、納乃得(methomyl)、美賜平(methoprene)、滅芬諾(methoxyfenozide)、美特寧(metofluthrin)、單福寧(monofluthrin)、烯啶蟲胺(nitenpyram)、硝蟲噻嗪(nithiazine)、諾伐隆(novaluron)、毆殺滅(oxamyl)、吡氟布米得(pyflubumide)、派滅淨(pymetrozine)、除蟲菊素(pyrethrin)、畢達本(pyridaben)、啶蟲丙醚(pyridalyl)、嘧蟎胺(pyriminostrobin)、百利普芬(pyriproxyfen)、蘭諾定(ryanodine)、賜諾特(spinetoram)、賜諾殺(spinosad)、賜派芬(spirodiclofen)、賜滅芬(spiromesifen)、賜派滅(spirotetramat)、速殺氟(sulfoxaflor)、得芬諾(tebufenozide)、治滅寧(tetramethrin)、賽果培(thiacloprid)、賽速安(thiamethoxam)、硫敵克(thiodicarb)、殺蟲單(thiosultap-sodium)、泰滅寧(tralomethrin)、四氟醚菊酯(tetramethylfluthrin)、唑蚜威(triazamate)、三福隆(triflumuron)、蘇力菌(Bacillus thuringiensis
)之所有品系、及核多角體病毒(Nucleo polyhedrosis
viruses)之所有品系。
實施例10.一種防制無脊椎動物害蟲之方法,其包含使該無脊椎動物害蟲或其環境與生物有效量的化合物1或式2化合物接觸。
實施例11.一種經處理之種子,其以該種子處理前之約0.0001至1重量%的量包含化合物1或式2化合物。
值得注意的是,本發明化合物之特徵在於有利的代謝及/或土壤殘留模式,並且展現出防制一系列農藝及非農藝無脊椎動物害蟲之活性。
尤其值得注意的是,由於無脊椎動物害蟲防制範圍及經濟價值之故,藉由防制無脊椎動物害蟲來保護農作物免受無脊椎動物害蟲所造成之損害或傷害係本發明之實施例。因為本發明之化合物在植物中具有有利之易位(translocation)性質或系統性毒性,其亦會保護未與化合物1或式2化合物或包含該化合物之組成物直接接觸之枝葉或其他植物部分。
並且值得注意的是,本發明之實施例係包含下列者之組成物:任何前述實施例、與本文中所述之任何實施例、及其任何組合的化合物,以及至少一種選自由界面活性劑、固體稀釋劑、與液體稀釋劑所組成之群組的額外組分,該等組成物可選地進一步包含至少一種額外生物活性化合物或藥劑。
進一步值得注意的是,本發明之實施例係用於防制無脊椎動物害蟲且包含下列者之組成物:任何前述實施例、與本文中所述之任何實施例、及其任何組合的化合物,以及至少一種選自由界面活性劑、固體稀釋劑、與液體稀釋劑所組成之群組的額外組分,該等組成物可選地進一步包含至少一種額外生物活性化合物或藥劑。本發明之實施例進一步包括用於防制無脊椎動物害蟲之方法,其包含使該無脊椎動物害蟲或其環境與生物有效量的任何前述實施例之化合物(例如,以本文中所述之組成物)接觸。
本發明之實施例亦包括一種組成物,其包含任何前述實施例之化合物,該化合物呈土壤澆灌液體配方之形式。本發明之實施例進一步包括用於防制無脊椎動物害蟲之方法,其包含使該土壤與作為土壤澆灌液之液體組成物接觸,該液體組成物包含生物有效量的任何前述實施例之化合物。
本發明之實施例亦包括一種用於防制無脊椎動物害蟲之噴灑組成物,其包含生物有效量的任何前述實施例之化合物及推進劑。本發明之實施例進一步包括用於防制無脊椎動物害蟲之餌料組成物,其包含生物有效量的任何先前實施例之化合物、一或多種食物材料、可選地引誘劑、及可選地保濕劑。本發明之實施例亦包括一種用於防制無脊椎動物害蟲之裝置,其包含該餌料組成物及經調適以收納該餌料組成物之外殼,其中該外殼具有至少一個開口,該開口之尺寸允許該無脊椎動物害蟲通過該開口,所以該無脊椎動物害蟲可自外殼外部之位置接近該餌料組成物,並且其中該外殼係進一步經調適以被置放在該無脊椎動物害蟲之可能或已知活動所在地或其附近。
本發明實施例亦包括用於保護種子免受無脊椎動物害蟲侵害之方法,其包含使該種子與生物有效量的任何前述實施例之化合物接觸。
本發明實施例亦包括用於保護動物免受無脊椎動物寄生害蟲侵害之方法,其包含向該動物投予殺寄生蟲有效量的任何前述實施例之化合物。
本發明之實施例亦包括用於防制無脊椎動物害蟲之方法,其包含使該無脊椎動物害蟲或其環境與生物有效量的化合物1或式2化合物(例如,以本文中所述之組成物)接觸,前提是該等方法非藉由治療之人體或動物體醫療方法。
本發明亦關於此等方法,其中使該無脊椎動物害蟲或其環境與包含生物有效量的化合物1或式2化合物、及至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外組分之組成物接觸,該組成物可選地進一步包含生物有效量的至少一種額外生物活性化合物或藥劑,前提是該等方法非藉由治療之人體或動物體醫療方法。
化合物1或式2化合物可藉由下列方法及如方案1與2中所述之變化來製備。使用下列縮寫:DMF係N
,N
-二甲基甲醯胺,DCC係N
,N'
-二環己基碳二亞胺,且HATU係1-[雙(二甲基胺基)亞甲基]-1H
-1,2,3-三唑并[4,5-b
]吡啶鎓3-氧六氟-磷酸鹽。
化合物1
可藉由方案1中所示之方法製備自化合物3
。在此方法中,化合物1
係藉由化合物3
之羧基與化合物4
之胺基於醯胺偶合試劑(諸如DCC或HATU)存在下的醯胺鍵形成反應來製備。關於代表性試劑及反應條件,請參見Jones, J.The Chemical Synthesis of Peptides
, International Series of Monographs on Chemistry, Oxford University: Oxford, 1994。
方案1
化合物3(CAS註冊編號2001277-98-9)在所屬技術領域中係已知的。
n係0之式2化合物(化合物2a
)可藉由方案2中所示之方法製備自化合物5
。方案2之方法類似於方案1中針對化合物1之製備所述之方法。在此方法中,式2化合物係藉由化合物5
之羧基與化合物6
之胺基於醯胺偶合試劑(諸如DCC或HATU)存在下的醯胺鍵形成反應來製備。
方案2
n係1或2之式2
化合物(即,各別係亞碸2b
或碸2c
)可藉由硫化物2a
之氧化來製備。各式方法及試劑在將硫化物氧化為亞碸之技術領域中係已知的。此等氧化試劑之實例包括間氯過氧苯甲酸及過碘酸鈉。
會認知到,上述用於製備化合物1或式2化合物之一些試劑及反應條件可能無法與存在於中間物中之某些官能性相容。在這些情況下,將保護/去保護序列或官能基交互轉化結合至合成中將有助於獲得所欲產物。保護基之使用及選擇對於所屬技術領域中具有通常知識者而言將是清楚易知的(參見例如,Greene, T. W.; Wuts, P. G. M.Protective Groups in Organic Synthesis
, 2nd ed.; Wiley: New York, 1991)。所屬技術領域中具有通常知識者將會認知到,在一些情況下,在引入個別方案中所描述之試劑後,可能需要未詳細描述之額外常規合成步驟以完成化合物1或式2化合物之合成。所屬技術領域中具有通常知識者亦將會認知到,可能必須以與所呈現之特定順序所默示者以外的順序來執行以上方案中所繪示之步驟的組合,以製備化合物1或式2化合物。
所屬技術領域中具有通常知識者亦將會認知到,化合物1或式2化合物及本文中所述之中間物可經歷各式親電子、親核、自由基、有機金屬、氧化、及還原反應,以加入取代基或修飾現有取代基。
無需進一步闡述,據信所屬技術領域中具有通常知識者使用前述說明即可最充份利用本發明。因此,將下列合成實例解讀為僅供說明之用,而無論如何不以任何方式限制本揭露。下列合成實例中的步驟說明用於整體合成轉換中之各步驟的程序,並且用於各步驟之起始材料未必要藉由特定製備運行(其程序描述於其他實例或步驟中)來製備。百分比係以重量計,除了層析溶劑混合物或另有指明。層析溶劑混合物之份數及百分比係以體積計,除非另有指明。1
H NMR譜係以偏離四甲基矽烷的低場ppm來記述;「s」意指單峰,「d」意指雙重峰,「t」意指三重峰,「q」意指四重峰,「m」意指多重峰,「dd」意指雙重雙重峰,「dt」意指雙重三重峰,「br s」意指寬單峰。DMF意指N
,N
-二甲基甲醯胺。化合物編號參照索引表A。
合成實例1N
-[1-(二氟甲基)環丙基]-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺(化合物 1
)之製備
步驟A:N
-[1-(二氟甲基)環丙基]-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺之製備
將2-(3-吡啶基)-2H
-吲唑-4-甲酸(100 mg, 0.42 mmol, CAS註冊編號2001277-98-9)、HATU (190 mg, 0.5 mmol)、1-(二氟甲基)環丙胺鹽酸鹽(71 mg, 0.5 mmol)於DMF (2 mL)中之溶液用三乙胺(174 µL, 1.25 mmol)處理。將反應混合物在室溫下攪拌整夜。接著將反應混合物直接經由逆相管柱層析術[C18管柱,用10%-100% MeCN/MeOH(1:1)至水洗提]純化以產出標題化合物,即本發明之化合物(105 mg,76%產率)。1
H NMR (500 MHz, DMSO-d 6
) δ ppm 9.35-9.39 (m, 2H) 9.14 (s, 1H) 8.67-8.68 (m, 1H) 8.55-8.58 (m, 1H) 7.94-7.97 (m, 1H), 7.73-7.75 (m, 1H), 7.63-7.67 (m, 1H), 7.41-7.45 (m, 1H), 6.21 (t, 1H), 1.13-1.17 (m, 2H), 1.02-1.06 (m, 2H).
合成實例2N
-[1,1-二甲基-2-(甲基硫基)乙基]-7-氟-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺(化合物 2a
)之製備
步驟A:N
-[1,1-二甲基-2-(甲基硫基)乙基]-7-氟-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺(化合物2a)之製備
將7-氟-2-(3-吡啶基)-2H
-吲唑-4-甲酸(10 g, 39 mmol)、HATU (17.7 g, 47 mmol)、2-甲基-1-甲基氫硫基-丙-2-胺(7 g, 58 mmol)於DMF (100 mL)中之溶液用三乙胺(16 ml, 117 mmol)處理。將反應混合物在室溫下攪拌4小時。將反應混合物用EtOAc (300 mL)稀釋然後用水(6 × 100 mL)洗滌。將有機層分離並在真空中濃縮。將所得粗製固體經由正相層析術(矽膠,以己烷中之70-100% EtOAc洗提)純化,以產出標題化合物,即本發明之化合物(9.9 g, 71%產率)。1
H NMR (500 MHz, DMSO-d 6
) δ ppm 9.37-9.43 (m, 2H), 8.69-8.72 (m, 1H), 8.56-8.60 (m, 1H), 8.00 (s, 1H), 7.64-7.70 (m, 2 H), 7.22-7.27 (m, 1H), 3.11 (s, 2H), 2.09 (s, 3H), 1.47 (s, 6H).
化合物2b(N
-[1,1-二甲基-2-(甲基亞磺醯基)乙基]-7-氟-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺),以及化合物2c(N
-[1,1-二甲基-2-(甲基磺醯基)乙基]-7-氟-2-(3-吡啶基)-2H
-吲唑-4-甲醯胺)可各自經由化合物2a之氧化來製備。
本發明之化合物將通常用作為組成物(即,配方)中之無脊椎動物害蟲防制活性成分,該組成物具有至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外組分,該額外組分作為載劑之用。配方或組成物成分係經選擇以配合活性成分之物理性質、施用模式、及環境因子(諸如土壤類型、濕度、與溫度)。
有用之配方包括液體及固體組成物兩者。液體組成物包括溶液(包括可乳化濃縮物)、懸浮液、乳液(包括微乳液、水包油乳液、可流動濃縮物、及/或懸浮乳液)、及類似者,可將其可選地將其增稠成凝膠。水性液體組成物之一般類型係可溶性濃縮物、懸浮濃縮物、膠囊懸浮液、濃縮乳液、微乳液、水包油乳液、可流動濃縮物、及懸浮乳液。非水性液體組成物之一般類型係可乳化濃縮物、微可乳化濃縮物、可分散濃縮物、及油分散液。
固體組成物之一般類型係塵粉(dust)、粉劑、粒劑、丸劑(pellets)、珠劑(prills)、錠劑(pastilles)、片劑、填充膜(包括種子塗層)、及類似者,其可係水分散性的(「可潤濕的」)或水溶性的。形成自成膜溶液或可流動懸浮液之膜及塗層對於種子處理尤其有用。可將活性成分(微)封裝並進一步形成懸浮液或固體配方;替代地,可將活性成分之整體配方封裝(或「覆塗」)。封裝可控制或延緩活性成分之釋放。可乳化粒劑結合了可乳化濃縮物配方與乾式顆粒配方兩者之優點。高強度組成物主要用作為中間物以用於進一步配製。
可噴灑配方在噴灑前一般會在適當介質中擴展。此等液體及固體配方係經配製以迅速稀釋於噴灑介質(通常為水,但偶爾會是另一種合適介質,像是芳族或石蠟烴或植物油)中。噴灑量可在每公頃約一至數千公升之範圍內,但更一般而言在每公頃約十至數百公升之範圍內。可噴灑配方可與水或另一種合適介質來進行槽式混合,以用於藉由空中或地面施用來進行枝葉處理,或供施用至植物之生長介質。液體及乾式配方可直接計量至滴流灌溉系統中或在栽植期間計量供給至犂溝中。液體及固體配方可施用在作物及其他所欲植生之種子上而作為栽植前之種子處理,以透過系統性吸收來保護發育中的根部及其他地下的植物部分及/或枝葉。
配方一般將包含在下列約略範圍內之有效量的活性成分、稀釋劑、及界面活性劑,其等加總為100重量百分比。
固體稀釋劑包括例如黏土(諸如,膨土、蒙脫土、厄帖浦土與高嶺土)、石膏、纖維素、二氧化鈦、氧化鋅、澱粉、糊精、糖類(例如,乳糖、蔗糖)、二氧化矽、滑石、雲母、矽藻土、尿素、碳酸鈣、碳酸鈉與碳酸氫鈉、及硫酸鈉。一般固體稀釋劑係描述於Watkins et al.,Handbook of Insecticide Dust Diluents and Carriers
, 2nd Ed., Dorland Books, Caldwell, New Jersey。
液體稀釋劑包括例如水、N
,N
-二甲基烷醯胺(例如,N
,N
-二甲基甲醯胺)、檸檬烯、二甲基亞碸、N
-烷基吡咯啶酮(例如,N
-甲基吡咯啶酮)、磷酸烷酯(例如,磷酸三乙酯)、乙二醇、三乙二醇、丙二醇、丙二醇、二丙二醇、聚丙二醇、碳酸丙烯酯、碳酸丁烯酯、石蠟(例如,白礦油、正烷烴、異烷烴)、烷基苯、烷基萘、甘油、甘油三乙酸酯、山梨醇、芳族烴、去芳族化脂族化合物、烷基苯、烷基苯、烷基萘、酮類(諸如,環己酮、2-庚酮、異佛爾酮及4-羥基-4-甲基-2-戊酮)、乙酸酯(諸如,乙酸異戊酯、乙酸己酯、乙酸庚酯、乙酸辛酯、乙酸壬酯、乙酸十三酯、及乙酸異莰酯)、其他酯類(諸如,烷基化乳酸酯、二元酯類烷基與芳基苯甲酸酯)、γ-丁內酯、及醇類(其可為直鏈、支鏈、飽和或不飽和,諸如甲醇、乙醇、正丙醇、異丙醇、正丁醇、異丁醇、正己醇、2-乙基己醇、正辛醇、癸醇、異癸醇、異十八醇、鯨蠟醇、月桂醇、十三醇、油醇、環己醇、四氫呋喃醇、二丙酮醇、甲酚、及苯甲醇。液體稀釋劑亦包括飽和與不飽和脂肪酸之甘油酯(一般而言係C6
–C22
),諸如植物種子與水果油(例如,下列者之油:橄欖、蓖麻、亞麻仁、芝麻、玉米(玉蜀黍)、花生、向日葵、葡萄子、紅花、棉花子、大豆、菜籽、椰子、與棕櫚仁)、動物來源脂肪(例如,牛脂、豬脂、豬油、鱈魚肝油、魚油)、及其混合物。液體稀釋劑亦包括烷基化脂肪酸(例如,甲基化、乙基化、丁基化),其中脂肪酸可藉由水解來自植物和動物來源之甘油酯來獲得,並且可藉由蒸餾來純化。典型液體稀釋劑係描述於Marsden,Solvents Guide
, 2nd Ed., Interscience, New York, 1950。
本發明之固體及液體組成物經常包括一或多種界面活性劑。當添加至液體時,界面活性劑(亦稱為「表面活性劑」)通常會改變、最常為減低液體之表面張力。取決於界面活性劑分子中之親水性及親油性基團的性質,界面活性劑可用作為潤濕劑、分散劑、乳化劑、或消泡劑。
界面活性劑可分類為非離子性、陰離子性、或陽離子性。可用於本組成物之非離子性界面活性劑包括但不限於:醇烷氧基化物(alcohol alkoxylate),諸如基於天然與合成醇(其可為支鏈或直鏈的)及製備自該等醇與環氧乙烷、環氧丙烷、環氧丁烷、或其混合物之醇烷氧基化物;胺乙氧基化物、烷醇醯胺、及乙氧基化烷醇醯胺;烷氧基化三酸甘油酯,諸如乙氧基化大豆油、蓖麻油、及菜籽油;烷基酚烷氧基化物,諸如辛基酚乙氧基化物、壬基酚乙氧基化物、二壬基酚乙氧基化物、及十二基酚乙氧基化物(製備自該等酚及環氧乙烷、環氧丙烷、環氧丁烷、或其混合物);製備自環氧乙烷或環氧丙烷之嵌段聚合物及末端嵌段係製備自環氧丙烷之反向嵌段聚合物;乙氧基化脂肪酸;乙氧基化脂肪酯及油;乙氧基化甲基酯;乙氧基化三苯乙烯酚(包括製備自環氧乙烷、環氧丙烷、環氧丁烷、或其混合物者);脂肪酸酯、甘油酯、基於羊毛脂之衍生物、聚乙氧基化物酯,諸如聚乙氧基化山梨醇酐脂肪酸酯、聚乙氧基化山梨醇脂肪酸酯、及聚乙氧基化甘油脂肪酸酯;其他山梨醇酐衍生物,諸如山梨醇酐酯;聚合界面活性劑,諸如隨機共聚物、嵌段共聚物、醇酸peg(聚乙二醇)樹脂、接枝或梳形聚合物與星形聚合物;聚乙二醇(peg);聚乙二醇脂肪酸酯;基於聚矽氧之界面活性劑;及糖衍生物,諸如蔗糖酯、烷基多醣苷、及烷基多醣。
有用之陰離子性界面活性劑包括但不限於:烷基芳基磺酸及其鹽;羧化醇或烷基酚乙氧基化物;二苯基磺酸鹽衍生物;木質素及木質素衍生物,諸如木質磺酸鹽;馬來酸或琥珀酸或其酐;烯烴磺酸鹽;磷酸酯,諸如醇烷氧基化物之磷酸酯、烷基酚烷氧基化物之磷酸酯、與苯乙烯基酚乙氧基化物之磷酸酯;基於蛋白質之界面活性劑;肌胺酸衍生物;苯乙烯基酚醚硫酸鹽;油及脂肪酸之硫酸鹽與磺酸鹽;乙氧基化烷基酚之硫酸鹽與磺酸鹽;醇之硫酸鹽;乙氧基化醇之硫酸鹽;胺及醯胺之磺酸鹽,諸如N
,N
-烷基牛磺酸鹽;苯、異丙苯、甲苯、二甲苯、及十二基與十三基苯之磺酸鹽;縮合萘之磺酸鹽;萘及烷基萘之磺酸鹽;分餾石油之磺酸鹽;磺琥珀醯胺酸鹽;及磺琥珀酸鹽及其衍生物,例如二烷基磺琥珀酸鹽。
有用之陽離子性界面活性劑包括但不限於:醯胺與乙氧基化醯胺;胺類,諸如N
-烷基丙二胺、三伸丙三胺與二伸丙四胺、及乙氧基化胺、乙氧基化二胺、與丙氧基化胺(製備自該等胺與環氧乙烷、環氧丙烷、環氧丁烷、或其混合物);胺鹽,諸如胺乙酸鹽與二胺鹽;四級銨鹽,諸如四級鹽、乙氧基化四級鹽、與雙四級鹽;及胺氧化物,諸如烷基二甲基胺氧化物與雙-(2-羥乙基)-烷基胺氧化物。
對於本發明組成物亦有用的是非離子性界面活性劑與陰離子性界面活性劑之混合物或非離子性界面活性劑與陽離子性界面活性劑之混合物。非離子性、陰離子性及陽離子性界面活性劑及其建議用途係揭示於各種已公開之參考文獻,包括McCutcheon’s Emulsifiers and Detergents
, annual American and International Editions published by McCutcheon’s Division, The Manufacturing Confectioner Publishing Co.;Sisely and Wood,Encyclopedia of Surface Active Agents
, Chemical Publ.Co., Inc., New York, 1964;及A. S. Davidson and B. Milwidsky,Synthetic Detergents
, Seventh Edition, John Wiley and Sons, New York, 1987。
本發明之組成物亦可含有配方輔助劑及添加劑,其等對於所屬技術領域中具有通常知識者已知為配方助劑(其中一些可視為亦作用為固體稀釋劑、液體稀釋劑、或界面活性劑)。此等配方輔助劑及添加劑可控制:pH(緩衝劑)、處理期間之發泡(抗發泡劑,諸如聚有機矽氧烷)、活性成分之沉降(懸浮劑)、黏度(觸變增稠劑)、在容器中之微生物生長(抗微生物劑)、產物凍結(抗凍劑)、顏色(染料/顏料分散液)、洗除(膜形成劑或黏著劑)、蒸發(蒸發延緩劑)、及其他配方屬性。膜形成劑包括例如聚乙酸乙烯酯、聚乙酸乙烯酯共聚物、聚乙烯吡咯啶酮-乙酸乙烯酯共聚物、聚乙烯醇、聚乙烯醇共聚物、及蠟。配方輔助劑及添加劑之實例包括下列文獻中所列出者:McCutcheon’s Volume 2: Functional Materials
, annual International and North American editions published by McCutcheon’s Division, The Manufacturing Confectioner Publishing Co.;及PCT公開案WO 03/024222。
化合物1或式2化合物及任何其他活性成分一般係藉由將活性成分溶於溶劑中或藉由在液體或乾式稀釋劑中研磨而結合至本案組成物中。溶液(包括可乳化濃縮物)可藉由單純混合成分來製備。如果意欲用作為可乳化濃縮物之液體組成物的溶劑係水不互溶的,則一般會添加乳化劑以在用水稀釋時乳化含活性物之溶劑。具有至多2,000 µm之粒徑的活性成分漿料可使用介質磨機來進行濕磨,以獲得平均直徑低於3 µm之粒子。水性漿料可製成最終懸浮液濃縮物(參見例如,U.S. 3,060,084)或經由噴灑乾燥來進一步處理以形成水分散性粒劑。乾式配方通常需要乾磨程序,其產生在2至10 µm範圍內之平均粒徑。塵粉及粉劑可藉由摻合及通常研磨(諸如用錘磨機或流體能磨機)來製備。粒劑及丸劑可藉由將活性材料噴灑於預成形之顆粒載體上或藉由黏聚技術來製備。參見Browning, 「Agglomeration」,Chemical Engineering
, December 4, 1967, pp 147–48,Perry’s Chemical Engineer’s Handbook
, 4th Ed., McGraw-Hill, New York, 1963, pages 8–57及以下、以及WO 91/13546。丸劑可如U.S. 4,172,714中所述來製備。水分散性及水溶性粒劑可如U.S. 4,144,050、U.S. 3,920,442、及DE 3,246,493中所教示來製備。片劑可如U.S. 5,180,587、U.S. 5,232,701、及U.S. 5,208,030中所教示來製備。膜可如GB 2,095,558及U.S. 3,299,566中所教示來製備。
關於配製技術之進一步資訊,請參見T. S. Woods, 「The Formulator’s Toolbox – Product Forms for Modern Agriculture」 inPesticide Chemistry and Bioscience, The Food–Environment Challenge
, T. Brooks and T. R. Roberts, Eds., Proceedings of the 9th International Congress on Pesticide Chemistry, The Royal Society of Chemistry, Cambridge, 1999, pp. 120–133。亦參見U.S. 3,235,361,第6欄,第16行至第7欄,第19行及實例10至41;U.S. 3,309,192,第5欄,第43行至第7欄,第62行及實例8、12、15、39、41、52、53、58、132、138至140、162至164、166、167、及169至182;U.S. 2,891,855,第3欄,第66行至第5欄,第17行及實例1至4;Klingman,Weed Control as a Science
, John Wiley and Sons, Inc., New York, 1961, pp 81–96;Hance et al.,Weed Control Handbook
, 8th Ed., Blackwell Scientific Publications, Oxford, 1989;及Developments in formulation technology
, PJB Publications, Richmond, UK, 2000。
在下列實例中,所有配方均以習知方式來製備。無需進一步闡述,據信所屬技術領域中具有通常知識者使用前述說明即可最充份利用本發明。因此,下列實例解讀為僅供說明之用,而絕非以任何方式限制本揭露。百分比係以重量計,除非另有指明。
實例A
實例B
實例C
實例D
實例E
實例F
實例G
實例H
實例I
實例J
實例K
實例L
本發明之化合物展現對抗廣泛系列無脊椎動物害蟲之活性。這些害蟲包括棲息於各種環境(諸如例如,植物葉子、根部、土壤、收成作物、或其他糧食、建築結構物、或動物外皮)之無脊椎動物。這些害蟲包括例如攝食枝葉(包括葉子、莖、花、及果實)、種子、木材、紡織纖維、或動物血液或組織,因而對生長中或儲存農藝作物、森林、溫室作物、觀賞植物、苗圃作物、儲存糧食或纖維產物、或房屋或其他結構物或其內容物造成傷害或損害,或對動物健康或公共衛生有害的無脊椎動物。所屬技術領域中具有通常知識者將理解,並非所有化合物對所有害蟲之所有生長階段皆同樣有效。
因此,這些本案化合物及組成物可農藝上用於保護田間作物免受植食性無脊椎動物害蟲侵害,並且亦可非農藝上用於保護其他園藝作物及植物免受植食性無脊椎動物害蟲侵害。此功效包括保護含有藉由遺傳工程(即,基因轉殖)所導入或藉由突變誘發(mutagenesis)所修改之遺傳物質以提供有利性狀的作物及其他植物(即,農藝與非農藝兩者)。此等性狀之實例包括對除草劑之耐性、對植食性害蟲(例如,昆蟲、蟎、蚜蟲、蜘蛛、線蟲、蝸牛、植物病原性真菌、細菌、及病毒)之耐性、改善植物生長、增加對不利生長條件(諸如高溫或低溫、低或高土壤濕度、及高鹽度)之耐受性、增加開花或結果、更大收成產出、更快速成熟、收成產物有更高品質及/或營養價值、或改善收成產物之儲存或處理性質。基因轉殖植物可經修改以表現多種性狀。含有藉由遺傳工程或突變誘發所提供之性狀的植物實例包括表現殺蟲蘇力菌毒素之玉米、棉花、大豆、及馬鈴薯的品種(諸如YIELD GARD®
、KnockOut®
、StarLink®
、Bollgard®
、NuCOTN®
與NewLeaf® 、
INVICTA RR2 PRO™
)、和玉米、棉花、大豆、及菜籽的耐除草劑品種(諸如Roundup Ready®
、Liberty Link®
、IMI®
、STS®
、及Clearfield®
),以及表現N
-乙醯基轉換酶(GAT)以提供對草甘膦(glyphosate)除草劑之耐性的作物,或含有提供對抑制乙醯乳酸合成酶(ALS)之除草劑的耐性之HRA基因的作物。本案化合物及組成物可與藉由遺傳工程所導入或藉由突變誘發所修改之性狀產生協同性交互作用,因此增強該等性狀之表型表現或有效性,或者增加本案化合物及組成物之無脊椎動物害蟲防制有效性。特定而言,本案化合物及組成物可與對無脊椎動物害蟲具有毒性之蛋白質或其他天然產物的表型表現產生協同性作用,從而提供對這些害蟲的大於相加防制。
本發明之組成物亦可選地包含植物營養素,例如包含至少一種選自下列之植物營養素的肥料組成物:氮、磷、鉀、硫、鈣、鎂、鐵、銅、硼、錳、鋅、及鉬。值得注意的是包含至少一種肥料組成物之組成物,該肥料組成物包含至少一種選自下列之植物營養素:氮、磷、鉀、硫、鈣、及鎂。進一步包含至少一種植物營養素的本發明之組成物可呈液體或固體之形式。值得注意的是呈粒劑、小棒、或片劑之固體配方。包含肥料組成物之固體配方可藉由下列方式來製備:將本發明之化合物或組成物與該肥料組成物混合在一起,然後藉由諸如製粒或擠製之方法來製備該配方。替代地,固體配方可藉由下列方式來製備:將本發明之化合物或組成物在揮發性溶劑中的溶液或懸浮液噴灑至先前製備之肥料組成物(其呈尺寸穩定混合物之形式,例如粒劑、小棒或片劑)上然後將溶劑蒸發。
非農藝用途係指在作物植物領域以外之領域中的無脊椎動物害蟲防制。本案化合物及組成物之非農藝用途包括在儲存穀物、豆子、及其他糧食中,以及在紡織品(諸如衣服及地毯)中的無脊椎動物害蟲防制。本案化合物及組成物之非農藝用途亦包括在觀賞植物、森林中、在庭院(連同道路旁及鐵路路權地)中,以及在草皮(諸如草坪、高爾夫球場、及牧草地)上的無脊椎動物害蟲防制。本案化合物及組成物之非農藝用途亦包括在房屋及其他建築物(可由人類及/或夥伴、農場、牧場、動物園、或其他動物所佔有)中的無脊椎動物害蟲防制。本案化合物及組成物之非農藝用途亦包括可破壞木材或建築物中所使用之其他結構材料的害蟲(諸如白蟻)之防制。
本案化合物及組成物之非農藝用途亦包括藉由防制寄生性或傳播感染性疾病之無脊椎動物害蟲來保護人體及動物健康。動物寄生蟲之防制包括防制寄生於宿主動物之身體表面(例如,肩膀、腋窩、腹部、大腿內側部分)的外寄生蟲及寄生於宿主動物之身體內部(例如,胃部、腸子、肺部、靜脈、皮下、淋巴組織)的內寄生蟲。外寄生或疾病傳播害蟲包括例如恙蟲、蜱、蝨、蚊子、蠅、蟎、及蚤。內寄生蟲包括心絲蟲、鉤蟲、及蠕蟲。本發明之化合物及組成物適用於寄生蟲對動物之侵害或感染的系統性及/或非系統性防制。本發明之化合物及組成物特別適用於對抗外寄生或疾病傳播害蟲。本發明之化合物及組成物適用於對抗侵染下列者之之寄生蟲:農業工作動物,諸如牛、綿羊、山羊、馬、豬、驢、駱駝、水牛、兔、母雞、火雞、鴨、鵝、及蜜蜂;寵物動物及家用動物,諸如狗、貓、寵物鳥、及觀賞魚;以及所謂的實驗動物,諸如倉鼠、天竺鼠、大鼠、及小鼠。利用對抗這些寄生蟲,死亡率及效能降低(就肉、奶、羊毛、皮、蛋、蜂蜜等而言)會獲得減少,使得施用包含本發明之化合物的組成物能讓動物管理更加經濟且簡單。
農藝或非農藝無脊椎動物害蟲之實例包括鱗翅目之卵、幼蟲、及成蟲,諸如夜蛾科中之行軍蟲、夜盜蟲、尺蠖、及實夜蛾(例如,粉紅蛀莖蟲(pink stem borer) (Sesamia inferens
Walker)、玉米鑽心蟲(corn stalk borer) (Sesamia nonagrioides
Lefebvre)、南方行軍蟲(southern armyworm) (Spodoptera eridania
Cramer)、秋行軍蟲(fall armyworm) (Spodoptera frugiperda
J. E. Smith)、甜菜行軍蟲(beet armyworm) (Spodoptera exigua
Hübner)、棉樹葉蟲(cotton leafworm) (Spodoptera littoralis
Boisduval)、黃條行軍蟲(yellowstriped armyworm) (Spodoptera ornithogalli
Guenée)、黑色夜盜蟲(black cutworm) (Agrotis ipsilon
Hufnagel)、藜豆毛蟲(velvetbean caterpillar) (Anticarsia gemmatalis
Hübner)、綠色果蟲(green fruitworm) (Lithophane antennata
Walker)、甘藍行軍蟲(cabbage armyworm) (Barathra brassicae
Linnaeus)、大豆尺蠖(soybean looper) (Pseudoplusia includens
Walker)、甘藍尺蠖(cabbage looper) (Trichoplusia ni
Hübner)、菸葉青蟲(tobacco budworm) (Heliothis virescens
Fabricius));來自螟蛾科之蛀蟲、負巢蟲、結網蟲、甜筒蟲、甘藍蟲、雕葉蟲(例如,歐洲甜筒蟲(European corn borer) (Ostrinia nubilalis
Hübner)、臍橙蟲(navel orangeworm) (Amyelois transitella
Walker)、玉米根結網蟲(corn root webworm) (Crambus caliginosellus
Clemens)、草地結網蟲(sod webworms) (Pyralidae:Crambinae
)如草地蟲(Herpetogramma licarsisalis
Walker)、甘蔗蛀莖蟲(sugarcane stem borer) (Chilo infuscatellus
Snellen)、番茄小蛀蟲(tomato small borer) (Neoleucinodes elegantalis
Guenée)、綠色捲葉蟲(green leafroller) (Cnaphalocrocis medinalis
)、葡萄折葉蟲(grape leaffolder) (Desmia funeralis
Hübner)、甜瓜蟲(melon worm) (Diaphania nitidalis
Stoll)、甘藍心蠐螬蟲(cabbage center grub) (Helluala hydralis
Guenée)、黃色蛀莖蟲(yellow stem borer) (Scirpophaga incertulas
Walker)、嫩芽蛀蟲(early shoot borer) (Scirpophaga infuscatellus
Snellen)、白色蛀莖蟲(white stem borer) (Scirpophaga innotata
Walker)、頂芽蛀蟲(top shoot borer) (Scirpophaga nivella
Fabricius)、黑頭稻米蛀蟲(dark-headed rice borer) (Chilo polychrysus
Meyrick)、條紋稻米蛀蟲(striped riceborer) (Chilo suppressalis
Walker)、甘藍簇毛蟲(cabbage cluster caterpillar) (Crocidolomia binotalis
English));捲葉蛾科中之捲葉蟲、芽蟲、種子蟲、及果實蟲(例如,蘋果捲葉蛾(codling moth) (Cydia pomonella
Linnaeus)、葡萄漿果蛾(grape berry moth) (Endopiza viteana
Clemens)、東方果蛾(oriental fruit moth) (Grapholita molesta
Busck)、柑橘偽蘋果捲葉蛾(citrus false codling moth) (Cryptophlebia leucotreta
Meyrick)、柑橘蛀蟲(citrus borer) (Ecdytolopha aurantiana
Lima)、紅帶捲葉蟲(redbanded leafroller) (Argyrotaenia velutinana
Walker)、斜帶捲葉蟲(obliquebanded leafroller) (Choristoneura rosaceana
Harris)、淺棕色蘋果蛾(light brown apple moth) (Epiphyas postvittana
Walker)、歐洲葡萄漿果蛾(European grape berry moth) (Eupoecilia ambiguella
Hübner)、蘋果芽蛾(apple bud moth) (Pandemis pyrusana
Kearfott)、雜食捲葉蟲(omnivorous leafroller) (Platynota stultana
Walsingham)、橫斑果樹捲葉蛾(barred fruit-tree tortrix) (Pandemis cerasana
Hübner)、蘋果棕色捲葉蛾(apple brown tortrix) (Pandemis heparana
Denis & Schiffermüller));及許多其他經濟上重要之鱗翅目(例如,菱紋背蛾(diamondback moth) (Plutella xylostella
Linnaeus)、粉紅夜蛾(pink bollworm) (Pectinophora gossypiella
Saunders)、舞蛾(gypsy moth) (Lymantria dispar
Linnaeus)、桃果實蛀蟲(peach fruit borer) (Carposina niponensis
Walsingham)、桃嫩枝蛀蟲(peach twig borer) (Anarsia lineatella
Zeller)、馬鈴薯塊莖蛾(potato tuberworm) (Phthorimaea operculella
Zeller)、點狀條帶潛葉蟲(spotted teniform leafminer) (Lithocolletis blancardella
Fabricius)、亞洲蘋果潛葉蟲(Asiatic apple leafminer) (Lithocolletis ringoniella
Matsumura)、稻米折葉蟲(rice leaffolder) (Lerodea eufala
Edwards)、蘋果潛葉蟲(apple leafminer) (Leucoptera scitella
Zeller));蜚蠊目之卵、若蟲、及成蟲,包括來自姬蠊科及蜚蠊科之蟑螂(例如,東方蟑螂(oriental cockroach) (Blatta orientalis
Linnaeus)、亞洲蟑螂(Asian cockroach) (Blatella asahinai
Mizukubo)、德國蟑螂(German cockroach) (Blattella germanica
Linnaeus)、棕帶蟑螂(brownbanded cockroach) (Supella longipalpa
Fabricius)、美洲蟑螂(American cockroach) (Periplaneta americana
Linnaeus)、棕色蟑螂(brown cockroach) (Periplaneta brunnea
Burmeister)、馬德拉蟑螂(Madeira cockroach) (Leucophaea maderae
Fabricius))、光滑棕色蟑螂(smoky brown cockroach) (Periplaneta fuliginosa
Service)、澳洲蟑螂(Australian Cockroach) (Periplaneta australasiae
Fabr.)、龍蝦蟑螂(lobster cockroach) (Nauphoeta cinerea
Olivier)、及光滑蟑螂(smooth cockroach) (Symploce pallens
Stephens));鞘翅目之食葉、食果、食根、食種子、與食泡狀組織幼蟲及成蟲,包括來自長角象鼻蟲科(Anthribidae)、豆象蟲科、及象鼻蟲科之象鼻蟲(例如,棉鈴象鼻蟲(boll weevil) (Anthonomus grandis
Boheman)、稻米水象鼻蟲(rice water weevil) (Lissorhoptrus oryzophilus
Kuschel)、穀倉象鼻蟲(granary weevil) (Sitophilus granarius
Linnaeus)、稻米象鼻蟲(rice weevil) (Sitophilus oryzae
Linnaeus))、一年生藍草象鼻蟲(annual bluegrass weevil) (Listronotus maculicollis
Dietz)、藍草穀象(bluegrass billbug) (Sphenophorus parvulus
Gyllenhal)、獵食穀象(hunting billbug) (Sphenophorus venatus vestitus
)、丹佛穀象(Denver billbug) (Sphenophorus cicatristriatus
Fahraeus));金花蟲科中之蚤甲蟲、胡瓜甲蟲、根蟲、葉甲蟲、馬鈴薯甲蟲、及潛葉蟲(例如,科羅拉多馬鈴薯甲蟲(Colorado potato beetle) (Leptinotarsa decemlineata
Say)、西方玉米根蟲(western corn rootworm) (Diabrotica virgifera virgifera
LeConte));來自金龜子科之金龜子及其他甲蟲(例如,日本甲蟲(Japanese beetle) (Popillia japonica
Newman)、東方甲蟲(oriental beetle) (Anomala orientalis
Waterhouse、Exomala orientalis
(Waterhouse) Baraud)、北方假面金龜子(northern masked chafer) (Cyclocephala borealis
Arrow)、南方假面金龜子(southern masked chafer) (Cyclocephala immaculata
Olivier orC. lurida
Bland)、糞甲蟲及白蠐螬(dung beetle and white grub) (Aphodius spp.)、黑色草皮草蜉金龜(black turfgrass ataenius) (Ataenius spretulus
Haldeman)、綠色六月甲蟲(green June beetle) (Cotinis nitida
Linnaeus)、亞洲花園甲蟲(Asiatic garden beetle) (Maladera castanea
Arrow)、五月/六月甲蟲(May/June beetles) (Phyllophaga
spp.)及歐洲金龜子(European chafer) (Rhizotrogus majalis
Razoumowsky));來自鰹節蟲科之地毯甲蟲;來自叩頭蟲科之線蟲;來自木蠹蟲科之樹皮甲蟲及來自偽步行蟲科之麵粉甲蟲。
此外,農藝及非農藝害蟲包括革翅目之卵、成蟲、及幼蟲,包括來自蠼螋科之蠼螋(例如,歐洲蠼螋(European earwig) (Forficula auricularia
Linnaeus)、黑色蠼螋(black earwig) (Chelisoches morio
Fabricius));半翅目及同翅目之卵、未成熟體、成蟲、及若蟲,諸如來自盲椿象科之盲蝽、來自蟬科之蟬、來自葉蟬科之葉蟬(例如,Empoasca
spp.)、來自床蝨科之床蝨(例如,Cimex lectularius
Linnaeus)、來自蠟蟬科與稻蝨科之蠟蟬、來自角蟬科之角蟬、來自木蝨科之木蝨、來自粉蝨科之粉蝨、來自蚜蟲科之蚜蟲、來自瘤蚜科之瘤蚜、粉介殼蟲科之粉介殼蟲、來自介殼蟲科、圓介殼蟲科、及碩介殼蟲科之介殼蟲、來自網蝽科之網蝽、來自蝽科之蝽、來自長椿象科之長椿(例如,毛長椿象(hairy chinch bug) (Blissus leucopterus hirtus
Montandon)及南方長椿象(southern chinch bug) (Blissus insularis
Barber))及其他長蝽、來自吹沫蟲科之泡沫蟲、來自緣蝽科之南瓜椿象、及來自星椿象科之紅椿象與棉椿象。
農藝及非農藝害蟲亦包括:蟎蜱目(蟎)之卵、幼蟲、若蟲、及成蟲,諸如葉壁蝨科中之葉蟎及紅蟎(例如,歐洲紅蟎(European red mite) (Panonychus ulmi
Koch)、二點葉蟎(two spotted spider mite) (Tetranychus urticae
Koch)、丹尼爾蟎(McDaniel mite) (Tetranychus mcdanieli
McGregor));偽葉蟎科中之扁蟎(例如,柑橘扁蟎(citrus flat mite) (Brevipalpus lewisi
McGregor));蟲癭壁蝨科中之鏽蟎與芽蟎及其他食葉蟎以及對人體及動物健康具有重要性之蟎,即表皮蟎科中之塵蟎、面皰壁蝨蟲科中之濾泡蟎、食甜蟎科中之穀物蟎;真壁蝨科中之蜱,常稱為硬蜱(例如,鹿蜱(deer tick) (Ixodes scapularis
Say)、澳洲麻痺蜱(Australian paralysis tick) (Ixodes holocyclus
Neumann)、美洲狗蜱(American dog tick) (Dermacentor variabilis
Say)、孤星蜱(lone star tick) (Amblyomma americanum
Linnaeus))及軟蜱科中之蜱,常稱為軟蜱(例如,回歸熱蜱(relapsing fever tick) (Ornithodoros turicata
)、常見雞蜱(common fowl tick) (Argas radiatus
));慅蟎科、蒲蟎科、及疥癬蟲科中之疥癬蟎及搔癢蟎;直翅目之卵、成蟲、及未成熟體,包括蚱蜢、蝗蟲、及蟋蟀(例如,遷移性蚱蜢(migratory grasshoppers)(例如,Melanoplus sanguinipes
Fabricius、M. differentialis
Thomas)、美洲蚱蜢(American grasshoppers)(例如,Schistocerca americana
Drury)、沙漠蝗蟲(desert locust) (Schistocerca gregaria
Forskal)、遷移性蝗蟲(migratory locust) (Locusta migratoria
Linnaeus)、灌木蝗蟲(bush locust) (Zonocerus
spp.)、家蟋蟀(house cricket) (Acheta domesticus
Linnaeus)、螻蛄(mole crickets)(例如,黃褐螻蛄(tawny mole cricket) (Scapteriscus vicinus
Scudder)及南方螻蛄(southern mole cricket) (Scapteriscus borellii
Giglio-Tos));雙翅目之卵、成蟲、及未成熟體,包括斑潛蠅(leafminers)(例如,蔬菜斑潛蠅(Liriomyza
spp.),諸如蛇形蔬菜斑潛蠅(serpentine vegetable leafminer) (Liriomyza sativae
Blanchard))、糠蚊(midges)、果蠅(fruit flies)(果蠅科)、黃潛蠅(frit flies)(例如,Oscinella frit
Linnaeus)、泥土蛆(soil maggots)、家蠅(house flies)(例如,Musca domestica
Linnaeus)、小家蠅(lesser house flies)(例如,Fannia canicularis
Linnaeus、F. femoralis
Stein)、廄蠅(stable flies)(例如,Stomoxys calcitrans
Linnaeus)、秋家蠅(face flies)、角蠅(horn flies)、麗蠅(blow flies)(例如,Chrysomya
spp.、Phormia
spp.)、及其他家蠅(muscoid fly)害蟲、馬蠅(horse flies)(例如,Tabanus
spp.)、膚蠅(bot flies)(例如,Gastrophilus
spp.、Oestrus
spp.)、牛蠐螬(cattle grubs)(例如,Hypoderma
spp.)、鹿蠅(deer flies)(例如,Chrysops
spp.)、綿羊蠅(keds)(例如,Melophagus ovinus
Linnaeus)及其他短角亞目、蚊子(mosquitoes)(例如,Aedes
spp.、Anopheles
spp.、Culex
spp.)、黑蠅(black flies)(例如,Prosimulium
spp.、Simulium
spp.)、蠓(biting midges)、白蛉(sand flies)、黑翅蕈蚋(sciarids)、及其他長角亞目(Nematocera);櫻翅目之卵、成蟲、及未成熟體,包括洋葱薊馬(onion thrips) (Thrips tabaci
Lindeman)、花薊馬(flower thrips) (Frankliniella
spp.)、及其他食葉薊馬;膜翅目之昆蟲害蟲,包括蟻科之蟻,包括佛羅里達木蟻(Florida carpenter ant) (Camponotus floridanus
Buckley)、紅木蟻(red carpenter ant) (Camponotus ferrugineus
Fabricius)、黑木蟻(black carpenter ant) (Camponotus pennsylvanicus
De Geer)、白腳蟻(white-footed ant) (Technomyrmex albipes
fr. Smith)、大頭蟻(big headed ants) (Pheidole
sp.)、黑頭慌蟻(ghost ant) (Tapinoma melanocephalum
Fabricius);法老蟻(Pharaoh ant) (Monomorium pharaonis
Linnaeus)、小火蟻(little fire ant) (Wasmannia auropunctata
Roger)、火蟻(fire ant) (Solenopsis geminata
Fabricius)、入侵紅火蟻(red imported fire ant) (Solenopsis invicta
Buren)、阿根廷蟻(Argentine ant) (Iridomyrmex humilis
Mayr)、瘋蟻(crazy ant) (Paratrechina longicornis
Latreille)、鋪道蟻(pavement ant) (Tetramorium caespitum
Linnaeus)、玉米田蟻(cornfield ant) (Lasius alienus
Förster)、及臭家蟻(odorous house ant) (Tapinoma sessile
Say)。其他膜翅目包括蜂(包括木蜂(carpenter bees)、大黃蜂(hornets)、黃胡蜂(yellow jackets)、土蜂(wasps)、及鋸蜂(sawflies) (Neodiprion
spp.;Cephus
spp.);等翅目之昆蟲害蟲,包括白蟻科(例如,Macrotermes
sp.、Odontotermes obesus
Rambur)、木白蟻科(Kalotermitidae)(例如,Cryptotermes
sp.)、及鼻白蟻科(Rhinotermitidae)(例如,Reticulitermes
sp.、Coptotermes
sp.、Heterotermes tenuis
Hagen)之白蟻、東方地下白蟻(eastern subterranean termite) (Reticulitermes flavipes
Kollar)、西方地下白蟻(western subterranean termite) (Reticulitermes hesperus
Banks)、台灣地下白蟻(Formosan subterranean termite)(Coptotermes formosanus
Shiraki)、西印度乾木白蟻(West Indian drywood termite) (Incisitermes immigrans
Snyder)、粉蠹白蟻(powder post termite) (Cryptotermes brevis
Walker)、乾木白蟻(drywood termite) (Incisitermes snyderi
Light)、西南方地下白蟻(southeastern subterranean termite) (Reticulitermes virginicus
Banks)、西方乾木白蟻(western drywood termite) (Incisitermes minor
Hagen)、樹木白蟻(arboreal termites)(諸如Nasutitermes
sp.)及具有經濟重要性之其他白蟻;櫻尾目之昆蟲害蟲,諸如衣魚(silverfish) (Lepisma saccharina
Linnaeus)及斑衣魚(firebrat) (Thermobia domestica
Packard);食毛目之昆蟲害蟲並且包括頭虱(head louse) (Pediculus humanus capitis
De Geer)、體虱(body louse) (Pediculus humanus
Linnaeus)、雞體虱(chicken body louse) (Menacanthus stramineus
Nitszch)、狗咬蝨(dog biting louse) (Trichodectes canis
De Geer)、絨虱(fluff louse) (Goniocotes gallinae
De Geer)、綿羊體虱(sheep body louse) (Bovicola ovis
Schrank)、短鼻牛虱(short-nosed cattle louse) (Haematopinus eurysternus
Nitzsch)、長鼻牛虱(long-nosed cattle louse) (Linognathus vituli
Linnaeus)及攻擊人體與動物之其他吸血與咀嚼寄生虱;蚤目之昆蟲害蟲,包括東方鼠蚤(oriental rat flea) (Xenopsylla cheopis
Rothschild)、貓蚤(cat flea) (Ctenocephalides felis
Bouche)、狗蚤(dog flea) (Ctenocephalides canis
Curtis)、母雞蚤(hen flea) (Ceratophyllus gallinae
Schrank)、吸著蚤(sticktight flea) (Echidnophaga gallinacea
Westwood)、人蚤(human flea) (Pulex irritans
Linnaeus)及侵襲哺乳動物與鳥類之其他蚤。所涵蓋之額外節肢動物害蟲包括:真蜘蛛目中之蜘蛛,諸如棕色隱居蜘蛛(brown recluse spider) (Loxosceles reclusa
Gertsch & Mulaik)與黑色窗蜘蛛(black widow spider) (Latrodectus mactans
Fabricius),以及蚰蜒目中之蜈蚣,諸如家蜈蚣(house centipede) (Scutigera coleoptrata
Linnaeus)。
儲存穀物之無脊椎動物害蟲的實例包括大穀物蛀蟲(larger grain borer) (Prostephanus truncatus
)、小穀物蛀蟲(lesser grain borer) (Rhyzopertha dominica
)、稻米象鼻蟲((rice weevil) (Stiophilus oryzae
)、玉蜀黍象鼻蟲(maize weevil) (Stiophilus zeamais
)、豇豆象鼻蟲(cowpea weevil) (Callosobruchus maculatus
)、紅麵粉甲蟲(red flour beetle)) (Tribolium castaneum
)、穀倉象鼻蟲(granary weevil) (Stiophilus granarius
)、印度榖蛾(Indian meal moth) (Plodia interpunctella
)、地中海麵粉甲蟲(Mediterranean flour beetle) (Ephestia kuhniella
)、及扁或鏽穀物甲蟲(flat or rusty grain beetle) (Cryptolestis ferrugineus
)。
本發明之化合物可對於線蟲綱(Nematoda)、絛蟲綱(Cestoda)、吸蟲綱(Trematoda)、及棘頭動物門(Acanthocephala)之成員具有活性,包括圓線蟲目(Strongylida)、蛔蟲目(Ascaridida)、尖尾線蟲目(Oxyurida)、小桿圓蟲目(Rhabditida)、司比路目(Spirurida)、及埃諾甫目(Enoplida)之經濟上重要成員,諸如但不限於經濟上重要的農業害蟲(即,Meloidogyne
屬中之根瘤線蟲、Pratylenchus
屬中之根腐線蟲、Trichodorus屬中之殘根線蟲等)及動物與人體健康害蟲(即,所有經濟上重要的吸蟲、條蟲、及蛔蟲,諸如馬中之Strongylus vulgaris
、狗中之Toxocara canis
、綿羊中之Haemonchus contortus
、狗中之Dirofilaria immitis
Leidy、馬中之Anoplocephala perfoliata
、反芻動物中之Fasciola hepatica
Linnaeus等)。
本發明之化合物可具有對抗下列者中之害蟲的活性:鱗翅目(例如,Alabama argillacea
Hübner(棉葉蟲)、Archips argyrospila
Walker(果樹捲葉蟲)、A. rosana
Linnaeus(歐洲捲葉蟲)與其他Archips
物種、Chilo suppressalis
Walker(稻米蛀莖蟲)、Cnaphalocrosis medinalis
Guenée(稻米捲葉蟲)、Crambus caliginosellus
Clemens(玉米根結網蟲)、Crambus teterrellus
Zincken(藍草結網蟲)、Cydia pomonella
Linnaeus(蘋果捲葉蛾)、Earias insulana
Boisduval(刺夜蛾)、Earias vittella
Fabricius(斑點夜蛾)、Helicoverpa armigera
Hübner(美洲夜蛾)、Helicoverpa zea
Boddie(玉米穗蟲)、Heliothis virescens
Fabricius(菸葉青蟲)、Herpetogramma licarsisalis
Walker(草皮結網蟲)、Lobesia botrana
Denis & Schiffermüller(葡萄漿果蛾)、Pectinophora gossypiella
Saunders(粉紅夜蛾)、Phyllocnistis citrella
Stainton(柑橘潛葉蟲)、Pieris brassicae
Linnaeus(大白蝶)、Pieris rapae
Linnaeus(小白蝶)、Plutella xylostella
Linnaeus(菱紋背蛾)、Spodoptera exigua
Hübner(甜菜行軍蟲)、Spodoptera litura
Fabricius(菸葉夜盜蟲、簇毛蟲)、Spodoptera frugiperda
J. E. Smith(秋行軍蟲)、Trichoplusia ni
Hübner(甘藍尺蠖)、及Tuta absoluta
Meyrick(番茄潛葉蟲))。
本發明之化合物對於包括下列者的來自同翅目之成員具有明顯活性:Acyrthosiphon pisum
Harris(豌豆蚜蟲)、Aphis craccivora
Koch(豇豆蚜蟲)、Aphis fabae
Scopoli(黑豆蚜蟲)、Aphis gossypii
Glover(棉蚜蟲、瓜蚜蟲)、Aphis pomi
De Geer(蘋果蚜蟲)、Aphis spiraecola
Patch(繡線菊蚜蟲)、Aulacorthum solani
Kaltenbach(毛地黃蚜蟲)、Chaetosiphon fragaefolii
Cockerell(草莓蚜蟲)、Diuraphis noxia
Kurdjumov/Mordvilko(俄羅斯小麥蚜蟲)、Dysaphis plantaginea
Paaserini(玫瑰蘋果蚜蟲)、Eriosoma lanigerum
Hausmann(絨毛蘋果蚜蟲)、Hyalopterus pruni
Geoffroy(粉質梅蚜蟲)、Lipaphis erysimi
Kaltenbach(蕪菁蚜蟲)、Metopolophium dirrhodum
Walker(穀物蚜蟲)、Macrosiphum euphorbiae
Thomas(馬鈴薯蚜蟲)、Myzus persicae
Sulzer(桃子-馬鈴薯蚜蟲、綠桃蚜)、Nasonovia ribisnigri
Mosley(萵苣蚜蟲)、Pemphigus
spp.(根蚜蟲及癭蚜蟲)、Rhopalosiphum maidis
Fitch(玉米葉蚜蟲)、Rhopalosiphum padi
Linnaeus(稠梨-燕麥蚜蟲)、Schizaphis graminum
Rondani(綠蟲(greenbug))、Sitobion avenae
Fabricius(英國穀物蚜蟲)、Therioaphis maculata
Buckton(斑點苜蓿蚜蟲)、Toxoptera aurantii
Boyer de Fonscolombe(黑色柑橘蚜蟲)、andToxoptera citricida
Kirkaldy(棕色柑橘蚜蟲);Adelges
spp.(球蚜(adelgids));Phylloxera devastatrix
Pergande(胡桃瘤蚜);Bemisia tabaci
Gennadius(菸葉粉蝨、甘藷粉蝨)、Bemisia argentifolii
Bellows & Perring(銀葉粉蝨)、Dialeurodes citri
Ashmead(柑橘粉蝨)、及Trialeurodes vaporariorum
Westwood(溫室粉蝨);Empoasca fabae
Harris(馬鈴薯葉蟬)、Laodelphax striatellus
Fallen(小棕色蠟蟬)、Macrolestes quadrilineatus
Forbes(紫菀葉蟬)、Nephotettix cinticeps
Uhler(綠葉蟬)、Nephotettix nigropictus
Stål(稻米葉蟬)、Nilaparvata lugens
Stål(棕色蠟蟬)、Peregrinus maidis
Ashmead(玉米蠟蟬)、Sogatella furcifera
Horvath(白背蠟蟬)、Sogatodes orizicola
Muir(稻蝨)、Typhlocyba pomaria
McAtee白蘋果葉蟬、Erythroneoura
spp.(葡萄葉蟬);Magicidada septendecim
Linnaeus(週期蟬(periodical cicada));Icerya purchasi
Maskell(吹綿介殼蟲(cottony cushion scale))、Quadraspidiotus perniciosus
Comstock(聖約瑟介殼(San Jose scale));Planococcus citri
Risso(柑橘粉介殼蟲);Pseudococcus
spp.(其他粉介殼蟲複合體);Cacopsylla pyricola
Foerster(梨木蝨)、Trioza diospyri
Ashmead(柿木蝨)。
本發明之化合物亦對於包括下列者的來自半翅目之成員具有活性:Acrosternum hilare
Say(綠蝽)、Anasa tristis
De Geer(南瓜椿象)、Blissus leucopterus leucopterus
Say(長椿象)、Cimex lectularius
Linnaeus(床蝨)Corythuca gossypii
Fabricius(棉網蝽)、Cyrtopeltis modesta
Distant(番茄椿象)、Dysdercus suturellus
Herrich-Schäffer(棉椿象)、Euchistus servus
Say(棕色蝽)、Euchistus variolarius
Palisot de Beauvois(單點蝽)、Graptosthetus
spp.(種子椿象之複合體)、Halymorpha halys
Stål(茶翅蝽(brown marmorated stink bug))、Leptoglossus corculus
Say(葉足松種子椿象(leaf-footed pine seed bug))、Lygus lineolaris
Palisot de Beauvois(牧草盲蝽(tarnished plant bug))、Nezara viridula
Linnaeus(南方綠蝽)、Oebalus pugnax
Fabricius(稻米綠蝽)、Oncopeltus fasciatus
Dallas(大蘿摩椿象(large milkweed bug))、Pseudatomoscelis seriatus
Reuter(棉盲蝽(cotton fleahopper))。本發明之化合物所防制的其他昆蟲目包括櫻翅目(例如,Frankliniella occidentalis
Pergande(西方花薊馬)、Scirthothrips citri
Moulton(柑橘薊馬)、Sericothrips variabilis
Beach(大豆薊馬)、及Thrips tabaci
Lindeman(洋葱薊馬);及鞘翅目(例如,Leptinotarsa decemlineata
Say(科羅拉多馬鈴薯甲蟲)、Epilachna varivestis
Mulsant(墨西哥豆甲蟲)及Agriotes
、Athous
、或Limonius
屬之線蟲)。
請注意,有些當代分類系統會將同翅目作為半翅目內之亞目。
值得注意的是本發明之化合物用於防制西方花薊馬(Frankliniella occidentalis
)之用途。值得注意的是本發明之化合物用於防制馬鈴薯葉蟬(Empoasca fabae
)之用途。值得注意的是本發明之化合物用於防制棉瓜蚜蟲(Aphis gossypii
)之用途。值得注意的是本發明之化合物用於防制綠桃蚜(Myzus persicae
)之用途。值得注意的是本發明之化合物用於防制甘藷粉蝨(Bemisia tabaci
)之用途。
本發明之化合物亦可用於增加作物植物之生長力。此方法包含使作物植物(例如,枝葉、花、果實、或根部)或生長出該作物植物之種子以達到所欲之植物生長力效果(即,生物有效量)的量與化合物1或式2化合物接觸。一般而言,化合物1或式2化合物係以經配製組成物來施用。雖然化合物1或式2化合物經常直接施用至作物植物或其種子,其亦可施用至該作物植物之所在地,亦即該作物植物之環境,尤其是該環境之足夠接近部分,以讓化合物1或式2化合物能夠遷移至該作物植物。與此方法相關之所在地最常包含生長介質(即,提供營養素給植物的介質),一般係該植物所生長之土壤。因此,增加作物植物生長力之作物植物處理包含使該作物植物、生長出該作物植物之種子、或該作物植物之所在地與生物有效量的化合物1或式2化合物接觸。
作物生長力增加可導致下列觀察到效果中之一或多者:(a)最佳作物建立(establishment),如藉由優良之種子發芽、作物萌發、及作物挺立所顯示;(b)增進作物生長,如藉由快速且強健之葉子生長(例如,藉由葉面積指數來測量)、植物高度、分蘖數量(例如,針對稻米)、作物之根質量與營養體整體乾重所顯示;(c)改善作物產出,如藉由開花時間、開花持續期間、花數量、總生質累積(即,產出數量)及/或果實或穀物等級產物可銷售性(即,產出品質)所顯示;(d)增進作物承受或防止植物疾病感染及節肢動物、線蟲、或軟體動物害蟲侵害之能力;以及(e)增加作物承受環境逆境(諸如暴露於熱極端條件、次最佳濕氣、或植物毒性(phytotoxic)化學物質)之能力。
本發明之化合物可藉由殺死或以其他方式防止植食性無脊椎動物害蟲在植物環境中之攝食來增加經處理植物之生長力(相較於未經處理植物)。在沒有對植食性無脊椎動物害蟲之此防制的情況下,害蟲會藉由食用植物組織或汁液(sap)、或傳播植物病原體(諸如病毒)來減少植物生長力。即使在沒有植食性無脊椎動物害蟲的情況下,本發明之化合物可藉由修改植物代謝來增加植物生長力。大致上,如果植物係生長在非理想環境(即,包含一或多個不利於該植物達成其在理想環境中所會展現之完整遺傳潛力之方面的環境)中,用本發明之化合物處理該植物將會最顯著增加作物植物之生長力。
值得注意的是一種用於增加作物植物之生長的方法,其中該作物植物係生長在包含植食性無脊椎動物害蟲之環境中。亦值得注意的是一種用於增加作物植物之生長力的方法,其中該作物植物係生長在不包含植食性無脊椎動物害蟲的環境中。亦值得注意的是一種用於增加作物植物之生長的方法,其中該作物植物係生長在包含低於支持該作物植物之生長的理想量之水分量的環境中。值得注意的是一種用於增加作物植物之生長力的方法,其中該作物係稻米。亦值得注意的是一種用於增加作物植物之生長力的方法,其中該作物係玉蜀黍(玉米)。亦值得注意的是一種用於增加作物植物之生長力的方法,其中該作物係大豆。
本發明之化合物亦可與一或多種包括下列之其他生物活性化合物或藥劑混合:殺蟲劑、殺真菌劑、殺線蟲劑、殺菌劑、除草劑、除草劑、除草劑安全劑、生長調控劑(諸如昆蟲蛻皮抑制劑及生根刺激劑)、化學消毒劑、半化學物、驅除劑、引誘劑、費洛蒙、進食刺激劑、其他生物活性化合物或昆蟲病原細菌、病毒、或真菌,以形成提供範圍更加廣泛之農藝與非農藝功效的多組分殺蟲劑。因此,本發明亦關於一種組成物,其包含生物有效量的化合物1或式2化合物、至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外成分、及至少一種額外生物活性化合物或藥劑。對於本發明之混合物而言,可將其他生物活性化合物或藥劑與本案化合物(包括化合物1或式2化合物)一起配製以形成預混物,或者可將其他生物活性化合物或藥劑與本案化合物(包括化合物1或式2化合物)分開配製,並且在施用前將兩種配方組合在一起(例如,在噴灑槽中),或者替代地接續施用。
可與本發明之化合物配製之此等生物活性化合物或藥劑的實例係殺蟲劑,諸如阿巴汀(abamectin)、毆殺松(acephate)、亞醌蟎(acequinocyl)、亞滅培(acetamiprid)、阿納寧(acrinathrin)、雙丙環蟲脂(afidopyropen)([(3S
,4R
,4aR
,6S
,6aS
,12R
,12aS
,12bS
)-3-[(環丙羰基)氧基]-1,3,4,4a,5,6,6a,12,12a,12b-十氫-6,12-二羥基-4,6a,12b-三甲基-11-側氧基-9-(3-吡啶基)-2H
,11H
-萘并[2,1-b
]哌喃并[3,4-e
]哌喃-4-基]甲基環丙烷甲酸酯)、磺胺蟎酯(amidoflumet)、三亞蹣(amitraz)、阿維菌素(avermectin)、印楝素(azadirachtin)、谷速松(azinphos-methyl)、免扶克(benfuracarb)、免速達(bensultap)、畢芬寧(bifenthrin)、必芬蟎(bifenazate)、雙三氟蟲脲(bistrifluron)、硼酸酯(borate)、布芬淨(buprofezin)、cadusafos、加保利(carbaryl)、加保扶(carbofuran)、培丹(cartap)、殺蟲脒(carzol)、賽速安勃(chlorantraniliprole)、克凡派(chlorfenapyr)、克福隆(chlorfluazuron)、陶斯松(chlorpyrifos)、陶斯松(chlorpyrifos)、甲基陶斯松(chlorpyrifos-methyl)、可芬諾(chromafenozide)、克芬蟎(clofentezin)、可尼丁(clothianidin)、氰蟲醯胺(cyantraniliprole)(3-溴-1-(3-氯-2-吡啶基)-N
-[4-氰基-2-甲基-6-[(甲基胺基)羰基]苯基]-1H
-吡唑-5-甲醯胺)、環溴蟲醯胺(cyclaniliprole)(3-溴-N
-[2-溴-4-氯-6-[[(1-環丙基乙基)胺基]羰基]苯基]-1-(3-氯-2-吡啶基)-1H
-吡唑-5-甲醯胺)、氰菊酯(cycloprothrin)、環氧蟲啶(cycloxaprid)((5S
,8R
)-1-[(6-氯-3-吡啶基)甲基]-2,3,5,6,7,8-六氫-9-硝基-5,8-環氧基-1H
-咪唑并[1,2-a
]氮呯)賽芬蟎(cyflumetofen)、賽扶寧(cyfluthrin)、貝他賽扶寧(beta-cyfluthrin)、賽洛寧(cyhalothrin)、伽瑪賽洛寧(gamma-cyhalothrin)、拉目達賽洛寧(lambda-cyhalothrin)、賽滅寧(cypermethrin)、亞滅寧(alpha-cypermethrin)、傑他賽滅寧(zeta-cypermethrin)、賽滅淨(cyromazine)、第滅寧(deltamethrin)、汰芬隆(diafenthiuron)、大利松(diazinon)、地特靈(dieldrin)、二福隆(diflubenzuron)、四氟甲醚菊酯(dimefluthrin)、殺蟲雙(dimehypo)、大滅松(dimethoate)、達特南(dinotefuran)、苯蟲醚(diofenolan)、因滅汀(emamectin)、安殺番(endosulfan)、益化利(esfenvalerate)、益斯普(ethiprole)、依芬寧(etofenprox)、依殺蟎(etoxazole)、芬佈賜(fenbutatin oxide)、撲滅松(fenitrothion)、芬硫克(fenothiocarb)、芬諾克(fenoxycarb)、芬普寧(fenpropathrin)、芬化利(fenvalerate)、芬普尼(fipronil)、弗美托奎(flometoquin)(2-乙基-3,7-二甲基-6-[4-(三氟甲氧基)苯氧基]-4-喹啉基甲基碳酸酯)、氟尼胺(flonicamid)、氟大滅(flubendiamide)、護賽寧(flucythrinate)、嘧蟲胺(flufenerim)、氟芬隆(flufenoxuron)、氟菌蟎酯(flufenoxystrobin)((αE
)-2-[[2-氯-4-(三氟甲基)苯氧基]甲基]-α-(甲氧基亞甲基)苯乙酸甲酯)、弗芬梭分(flufensulfone)(5-氯-2-[(3,4,4-三氟-3-丁烯-1-基)磺醯基]噻唑)、fluhexafon、氟吡菌醯胺(fluopyram)、弗皮洛(flupiprole)(1-[2,6-二氯-4-(三氟甲基)苯基]-5-[(2-甲基-2-丙烯-1-基)胺基]-4-[(三氟甲基)亞磺醯基]-1H
-吡唑-3-腈)、氟吡呋喃酮(flupyradifurone) (4-[[(6-氯-3-吡啶基)甲基](2,2-二氟乙基)胺基]-2(5H
)-呋喃酮)、福化利(fluvalinate)、氟胺氰菊酯(tau-fluvalinate)、大福松(fonophos)、覆滅蟎(formetanate)、福賽絕(fosthiazate)、合芬隆(halofenozide)、右旋七氟甲醚菊酯(heptafluthrin)([2,3,5,6-四氟-4-(甲氧基甲基)苯基]甲基2,2-二甲基-3-[(1Z
)-3,3,3-三氟-1-丙烯-1-基]環丙烷甲酸酯)、六伏隆(hexaflumuron)、合賽多(hexythiazox)、愛美松(hydramethylnon)、益達胺(imidacloprid)、因得克(indoxacarb)、殺蟲皂(insecticidal soaps)、亞芬松(isofenphos)、祿芬隆(lufenuron)、馬拉松(malathion)、氯氟醚菊酯(meperfluthrin)([2,3,5,6-四氟-4-(甲氧基甲基)苯基]甲基(1R
,3S
)-3-(2,2-二氯乙烯基)-2,2-二甲基環丙烷甲酸酯)、美氟綜(metaflumizone)、聚乙醛(metaldehyde)、達馬松(methamidophos)、滅大松(methidathion)、滅蟲威(methiodicarb)、納乃得(methomyl)、美賜平(methoprene)、甲氧滴滴梯(methoxychlor)、美特寧(metofluthrin)、滅芬諾(methoxyfenozide)、美特寧(metofluthrin)、亞素靈(monocrotophos)、monofluorothrin([2,3,5,6-四氟-4-(甲氧基甲基)苯基]甲基3-(2-氰基-1-丙烯-1-基)-2,2-二甲基環丙烯甲酸酯)、尼古丁(nicotine)、烯啶蟲胺(nitenpyram)、硝蟲噻嗪(nithiazine)、諾伐隆(novaluron)、諾福隆(noviflumuron)、毆殺滅(oxamyl)、巴拉松(parathion)、甲基巴拉松(parathion-methyl)、百滅寧(permethrin)、福瑞松(phorate)、裕必松(phosalone)、益滅松(phosmet)、福賜米松(phosphamidon)、比加普(pirimicarb)、佈飛松(profenofos)、丙氟菊酯(profluthrin)、毆蟎多(propargite)、丙苯烴菊酯(protrifenbute)、吡氟布米得(pyflubumide)(1,3,5-三甲基-N
-(2-甲基-1-側氧基丙基)-N
-[3-(2-甲基丙基)-4-[2,2,2-三氟-1-甲氧基-1-(三氟甲基)乙基]苯基]-1H
-吡唑-4-甲醯胺)、派滅淨(pymetrozine)、啶吡唑蟲胺(pyrafluprole)、除蟲菊素(pyrethrin)、畢達本(pyridaben)、啶蟲丙醚(pyridalyl)、吡立芙淇納蔥(pyrifluquinazon)、嘧蟎胺(pyriminostrobin)((αE
)-2-[[[2-[(2,4-二氯苯基)胺基]-6-(三氟甲基)-4-嘧啶基]氧基]甲基]-α-(甲氧基亞甲基)苯乙酸甲酯)、pyriprole、百利普芬(pyriproxyfen)、魚藤酮(rotenone)、蘭諾定(ryanodine)、矽護芬(silafluofen)、賜諾特(spinetoram)、賜諾殺(spinosad)、賜派芬(spirodiclofen)、賜滅芬(spiromesifen)、賜派滅(spirotetramat)、硫丙磷(sulprofos)、速殺氟(sulfoxaflor)(N
-[甲氧基氧橋[1-[6-(三氟甲基)-3-吡啶基]乙基]-λ4
-伸氧硫基]氰胺)、得芬諾(tebufenozide)、得芬瑞(tebufenpyrad)、得福隆(teflubenzuron)、七氟菊酯(tefluthrin)、托福松(terbufos)、樂本松(tetrachlorvinphos)、治滅寧(tetramethrin)、四氟醚菊酯(tetramethylfluthrin)([2,3,5,6-四氟-4-(甲氧基甲基)苯基]甲基2,2,3,3-四甲基環丙烷甲酸酯)、tetraniliprole、賽果培(thiacloprid)、賽速安(thiamethoxam)、硫敵克(thiodicarb)、殺蟲單(thiosultap-sodium)、tioxazafen(3-苯基-5-(2-噻吩基)-1,2,4-二唑)、脫芬瑞(tolfenpyrad)、泰滅寧(tralomethrin)、唑蚜威(triazamate)、三氯松(trichlorfon)、三氟滅吡林(triflumezopyrim)(2,4-二側氧基-1-(5-嘧啶基甲基)-3-[3-(三氟甲基)苯基]-2H
-吡啶并[1,2-a
]嘧啶鎓內鹽)、泰滅寧(tralomethrin)、唑蚜威(triazamate)、三氯松(trichlorfon)、三福隆(triflumuron)、蘇力菌德他內毒素、昆蟲病原細菌、昆蟲病原病毒、及昆蟲病原真菌。
值得注意的是諸如下列之殺蟲劑:阿巴汀(abamectin)、亞滅培(acetamiprid)、阿納寧(acrinathrin)、雙丙環蟲脂(afidopyropen)、三亞蹣(amitraz)、阿維菌素(avermectin)、印楝素(azadirachtin)、免扶克(benfuracarb)、免速達(bensultap)、畢芬寧(bifenthrin)、布芬淨(buprofezin)、cadusafos、加保利(carbaryl)、培丹(cartap)、賽速安勃(chlorantraniliprole)、克凡派(chlorfenapyr)、克福隆(chlorfluazuron)、陶斯松(chlorpyrifos)、可尼丁(clothianidin)、氰蟲醯胺(cyantraniliprole)、環溴蟲醯胺(cyclaniliprole)、乙氰菊酯(cycloprothrin)、賽扶寧(cyfluthrin)、貝他賽扶寧(beta-cyfluthrin)、賽洛寧(cyhalothrin)、伽瑪賽洛寧(gamma-cyhalothrin)、拉目達賽洛寧(lambda-cyhalothrin)、賽滅寧(cypermethrin)、亞滅寧(alpha-cypermethrin)、傑他賽滅寧(zeta-cypermethrin)、賽滅淨(cyromazine)、第滅寧(deltamethrin)、地特靈(dieldrin)、達特南(dinotefuran)、苯蟲醚(diofenolan)、因滅汀(emamectin)、安殺番(endosulfan)、益化利(esfenvalerate)、益斯普(ethiprole)、依芬寧(etofenprox)、依殺蟎(etoxazole)、撲滅松(fenitrothion)、芬硫克(fenothiocarb)、芬諾克(fenoxycarb)、芬化利(fenvalerate)、芬普尼(fipronil)、弗美托奎(flometoquin)、氟尼胺(flonicamid)、氟大滅(flubendiamide)、氟芬隆(flufenoxuron)、氟菌蟎酯(flufenoxystrobin)、弗芬梭分(flufensulfone)、弗皮洛(flupiprole)、氟吡呋喃酮(flupyradifurone)、福化利(fluvalinate)、覆滅蟎(formetanate)、福賽絕(fosthiazate)、右旋七氟甲醚菊酯(heptafluthrin)、六伏隆(hexaflumuron)、愛美松(hydramethylnon)、益達胺(imidacloprid)、因得克(indoxacarb)、祿芬隆(lufenuron)、氯氟醚菊酯(meperfluthrin)、美氟綜(metaflumizone)、滅蟲威(methiodicarb)、納乃得(methomyl)、美賜平(methoprene)、滅芬諾(methoxyfenozide)、美特寧(metofluthrin)、單福寧(monofluthrin)、烯啶蟲胺(nitenpyram)、硝蟲噻嗪(nithiazine)、諾伐隆(novaluron)、毆殺滅(oxamyl)、吡氟布米得(pyflubumide)、派滅淨(pymetrozine)、除蟲菊素(pyrethrin)、畢達本(pyridaben)、啶蟲丙醚(pyridalyl)、嘧蟎胺(pyriminostrobin)、百利普芬(pyriproxyfen)、蘭諾定(ryanodine)、賜諾特(spinetoram)、賜諾殺(spinosad)、賜派芬(spirodiclofen)、賜滅芬(spiromesifen)、賜派滅(spirotetramat)、速殺氟(sulfoxaflor)、得芬諾(tebufenozide)、治滅寧(tetramethrin)、四氟醚菊酯(tetramethylfluthrin)、賽果培(thiacloprid)、賽速安(thiamethoxam)、硫敵克(thiodicarb)、殺蟲單(thiosultap-sodium)、泰滅寧(tralomethrin)、唑蚜威(triazamate)、三氟滅吡林(triflumezopyrim)、三福隆(triflumuron)、蘇力菌德他內毒素、蘇力菌之所有品系、及核多角體病毒之所有品系。
用於與本發明之化合物混合的生物藥劑之一個實施例包括昆蟲病原細菌(諸如蘇力菌)與經封裝之蘇力菌德他內毒素(諸如以CellCap®
程序所製備之MVP®
與MVPII®
生物殺蟲劑,CellCap®
、MVP®
、及MVPII®
皆為Mycogen Corporation, Indianapolis, Indiana, USA之商標);昆蟲病原真菌真菌,諸如青蕈真菌(green muscardine fungus);及昆蟲病原(天然發生或基因改造的皆是)病毒,包括桿狀病毒、核多角體病毒(NPV, nucleopolyhedro virus)(諸如Helicoverpa zea
核多角體病毒(HzNPV)、Anagrapha falcifera
核多角體病毒(AfNPV));及顆粒增殖病毒(GV, granulosis virus)(諸如Cydia pomonella
顆粒增殖病毒(CpGV))。
用於與本發明之化合物混合的生物藥劑之一個實施例包括下列者其中之一或其組合:(i)下列者之細菌:放射菌屬(Actinomycetes
)、農桿菌屬(Agrobacterium
)、關節桿菌屬(Arthrobacter
)、產鹼桿菌屬(Alcaligenes
)、金桿菌屬(Aureobacterium
)、固氮菌屬(Azobacter
)、芽孢桿菌屬(Bacillus
)、拜葉林克氏菌屬(Beijerinckia
)、慢生根瘤菌屬(Bradyrhizobium
)、短芽孢桿菌屬(Brevibacillus
)、伯克氏菌屬(Burkholderia
)、產色細菌屬(Chromobacterium
)、芽胞梭菌屬(Clostridium
)、棒桿菌屬(Clavibacter)
、叢毛單胞菌屬(Comamonas
)、棒狀桿菌屬(Corynebacterium
)、短小桿菌屬(Curtobacterium
)、腸桿菌屬(Enterobacter
)、黃質細菌屬(Flavobacterium
)、葡萄桿菌屬(Gluconobacter
)、噬氫菌屬(Hydrogenophaga
)、克留氏菌屬(Klebsiella
)、甲基桿菌屬(Methylobacterium
)、類芽孢桿菌屬(Paenibacillus
)、巴斯德氏菌屬(Pasteuria
)、光桿菌屬(Photorhabdus
)、葉桿菌屬(Phyllobacterium
)、假單胞菌屬(Pseudomonas
)、根瘤菌屬(Rhizobium
)、鋸桿菌屬(Serratia
)、鞘脂桿菌屬(Sphingobacterium
)、寡養單胞菌屬(Stenotrophomonas
)、鏈黴菌屬(Streptomyces
)、貪食菌屬(Variovorax
)、或嗜線蟲桿菌屬(Xenorhabdus
),例如芽孢枯草桿菌(Bacillus amyloliquefaciens
)、仙人掌桿菌(Bacillus cereus
)、堅強桿菌(Bacillus firmus
)、地衣桿菌(Bacillus licheniformis
)、短小桿菌(Bacillus pumilus
)、圓形桿菌(Bacillus sphaericus
)、枯草桿菌(Bacillus subtilis
)、蘇力菌(Bacillus thuringiensis
)、慢生大豆根瘤菌(Bradyrhizobium japonicum)
、Chromobacterium subtsugae
、撤銷巴斯德氏菌(Pasteuria nishizawae
)、穿透巴斯德氏菌(Pasteuria penetrans)
、Pasteuria usage
、螢光假單胞菌(Pseudomonas fluorescens
)、及利迪鏈黴菌(Streptomyces lydicus
);(ii)真菌,諸如青蕈真菌;(iii)病毒,包括桿狀病毒、核多角體病毒,諸如Helicoverpa zea
核多角體病毒、Anagrapha falcifera
核多角體病毒;顆粒增殖病毒,諸如Cydia pomonella
顆粒增殖病毒。
尤其值得注意的是具有下列條件之組合:其他無脊椎動物害蟲防制活性成分屬於不同於化合物1或式2化合物之化學類別或具有不同於化合物1或式2化合物之作用部位。在某些實例中,與至少一種具有相似防制範圍但不同作用部位之其他無脊椎動物害蟲防制活性成分的組合將尤其有利於抗性管理。因此,本發明之組成物可進一步包含生物有效量的至少一種具有相似防制範圍但屬於不同化學類別或具有不同作用部位之其他無脊椎動物害蟲防制活性成分。這些額外的生物活性化合物或藥劑包括但不限於乙醯膽鹼酯酶(AChE)抑制劑,諸如胺甲酸酯類納乃得(methomyl)、毆殺滅(oxamyl)、硫敵克(thiodicarb)、唑蚜威(triazamate)及有機磷酸酯類陶斯松(chlorpyrifos);GABA閘控氯離子通道拮抗劑,諸如環二烯類地特靈(dieldrin)與安殺番(endosulfan)、及苯基吡唑類益斯普(ethiprole)與芬普尼(fipronil);鈉通道調節劑,諸如類除蟲菊素類(pyrethroids)畢芬寧(bifenthrin)、賽扶寧(cyfluthrin)、貝他賽扶寧(beta
-cyfluthrin)、賽洛寧(cyhalothrin)、拉目達賽洛寧(lambda
-cyhalothrin)、賽滅寧(cypermethrin)、第滅寧(deltamethrin)、四氟甲醚菊酯(dimefluthrin)、益化利(esfenvalerate)、美特寧(metofluthrin)、與丙氟菊酯(profluthrin);尼古丁乙醯膽鹼受體(nAChR)促效劑,諸如類尼古丁類(neonicotinoids)亞滅培(acetamiprid)、可尼丁(clothianidin)、達特南(dinotefuran)、益達胺(imidacloprid)、烯啶蟲胺(nitenpyram)、硝蟲噻嗪(nithiazine)、賽果培(thiacloprid)、及賽速安(thiamethoxam)、與速殺氟(sulfoxaflor);尼古丁乙醯膽鹼受體(nAChR)別位活化劑,諸如賜諾司類(spinosyns)賜諾特(spinetoram)及賜諾殺(spinosad);氯離子通道活化劑,諸如阿維菌素類(avermectins)阿巴汀(abamectin)及因滅汀(emamectin);保幼激素模擬物,諸如苯蟲醚(diofenolan)、美賜平(methoprene)、芬諾克(fenoxycarb)、及百利普芬(pyriproxyfen);選擇性同翅目昆蟲(homopteran)進食阻斷劑,諸如派滅淨(pymetrozine)及氟尼胺(flonicamid);蟎生長抑制劑,諸如依殺蟎(etoxazole);粒線體ATP合成酶之抑制劑,諸如毆蟎多(propargite);經由破壞質子梯度之氧化磷酸化的去偶合劑(ucouplers),諸如克凡派(chlorfenapyr);尼古丁乙醯膽鹼受體(nAChR)通道阻斷劑,諸如沙蠶毒素類似物培丹(cartap);幾丁質生物合成之抑制劑,諸如苯甲醯脲氟芬隆(flufenoxuron)、六伏隆(hexaflumuron)、祿芬隆(lufenuron)、諾伐隆(novaluron)、諾福隆(noviflumuron)、及三福隆(triflumuron)、與布芬淨(buprofezin);雙翅類昆蟲蛻皮干擾劑,諸如賽滅淨(cyromazine);蛻皮激素受體促效劑,諸如二醯基肼類(diacylhydrazines)滅芬諾(methoxyfenozide)及得芬諾(tebufenozide);章魚胺受體促效劑,諸如三亞蹣(amitraz);粒線體複合體III電子傳輸抑制劑,諸如愛美松(hydramethylnon);粒線體複合體I電子傳輸抑制劑,諸如畢達本(pyridaben);電壓依賴性鈉離子通道阻斷劑,諸如因得克(indoxacarb);乙醯CoA羧基酶之抑制劑,諸如特窗酸類(tetronic acids)及帖唑咪酸類(tetramic acids)賜派芬(spirodiclofen)、賜滅芬(spiromesifen)、及賜派滅(spirotetramat);粒線體錯合物II電子傳輸抑制劑,諸如ß-酮腈類賽派芬(cyenopyrafen)及賽芬蟎(cyflumetofen);蘭諾定(ryanodine)受體調節劑,諸如鄰胺苯甲酸二醯胺賽速安勃(chlorantraniliprole)、氰蟲醯胺(cyantraniliprole)、與氰蟲醯胺(cyantraniliprole),及二醯胺類諸如氟大滅(flubendiamide),以及蘭諾定(ryanodine)受體配體,諸如蘭諾定(ryanodine);負責生物活性之目標部位係未知的或未特徵化之化合物,諸如印楝素(azadirachtin)、必芬蟎(bifenazate)、啶蟲丙醚(pyridalyl)、吡立芙淇納蔥(pyrifluquinazon)、及三氟滅吡林(triflumezopyrim);昆蟲中腸膜之微生物干擾劑,諸如蘇力菌與其生產之德他內毒素及圓形桿菌(Bacillus sphaericus
);及生物劑,包括核多角體病毒(NPV)及其他天然發生或基因改造之殺蟲病毒。
可與本發明之化合物配製之此等生物活性化合物或藥劑的進一步實例係:殺真菌劑,諸如阿拉酸式苯-S-甲基(acibenzolar-S-methyl)、aldimorph、滅脫定(ametoctradin)、安美速(amisulbrom)、敵菌靈(anilazine)、氧環唑(azaconazole)、亞托敏(azoxystrobin)、本達樂(benalaxyl)(包括本達樂-M))、麥鏽靈(benodanil)、免賴得(benomyl)、苯噻菌胺(benthiavalicarb)(包括苯噻菌胺-異丙基)、苯并烯氟菌唑(benzovindiflupyr)、苯噻唑嗪(bethoxazin)、百蟎克(binapacryl)、聯苯(biphenyl)、比多農((bitertanol)、聯苯吡菌胺(bixafen)、保米黴素(blasticidin-S)、白克列(boscalid)、溴克座(bromuconazole)、布瑞莫(bupirimate)、得滅多(buthiobate)、萎鏽靈(carboxin)、加普胺(carpropamid)、四氯丹(captafol)、蓋普丹(captan)、貝芬替(carbendazim)、地茂散(chloroneb)、四氯異苯腈(chlorothalonil)、克氯得(chlozolinate)、氫氧化銅(copper hydroxide)、氧氯化銅(copper oxychloride)、硫酸銅(copper sulfate)、丁香菌酯(coumoxystrobin)、賽座滅(cyazofamid)、賽福芬胺(cyflufenamid)、克絕(cymoxanil)、環克座(cyproconazole)、賽普洛(cyprodinil)、益發靈(dichlofluanid)、雙氯氰菌胺(diclocymet)、達滅淨(diclomezine)、大克爛(dicloran)、乙霉威(diethofencarb)、待克利(difenoconazole)、二氟林(diflumetorim)、二甲嘧酚(dimethirimol)、達滅芬(dimethomorph)、醚菌胺(dimoxystrobin)、達克利(diniconazole)(包括達克利-M)、白粉克(dinocap)、腈硫醌(dithianon)、二硫戊環類(dithiolanes)、十二環嗎啉(dodemorph)、多寧(dodine)、益康唑(econazole)、乙環唑(etaconazole)、護粒松(edifenphos)、烯肟菌酯(enoxastrobin)(亦稱為enestroburin)、依普座(epoxiconazole)、噻唑菌胺(ethaboxam)、依瑞莫(ethirimol)、依得利(etridiazole)、凡殺同(famoxadone)、咪唑菌酮(fenamidone)、烯肟菌胺(fenaminstrobin)、芬瑞莫(fenarimol)、芬克座(fenbuconazole)、甲呋醯胺(fenfuram)、環醯菌胺(fenhexamide)、芬諾尼(fenoxanil)、拌種咯(fenpiclonil)、苯鏽啶(fenpropidin)、芬普福(fenpropimorph)、fenpyrazamine、三苯醋錫(fentin acetate)、三苯羥錫(fentin hydroxide)、富爾邦(ferbam)、富米綜(ferimzone)、flometoquin、扶吉胺(fluazinam)、護汰寧(fludioxonil)、氟菌蟎酯(flufenoxystrobin)、氟嗎啉(flumorph)、氟比來(fluopicolide)、氟派瑞(fluorpyram)、氟嘧菌酯(fluoxastrobin)、氟喹唑(fluquinconazole)、護矽得(flusilazole)、氟硫滅(flusulfamide)、氟噻唑菌腈(flutianil)、福多寧(flutolanil)、護汰芬(flutriafol)、氟克殺(fluxapyroxad)、福爾培(folpet)、熱必斯(fthalide)(亦稱為phthalide)、麥穗寧(fuberidazole)、呋霜靈(furalaxyl)、福拉比(furametpyr)、菲克利(hexaconazole)、殺紋寧(hymexazole)、克熱淨(guazatine)、依滅列(imazalil)、易胺座(imibenconazole)、克熱淨烷苯磺酸鹽(iminoctadine albesilate)、克熱淨三乙酸鹽(iminoctadine triacetate)、iodicarb、種菌唑(ipconazole)、噻吩酰菌酮(isofetamid)、丙基喜樂松(iprobenfos)、依普同(iprodione)、丙森鋅(iprovalicarb)、亞賜圃(isoprothiolane)、亞派占(isopyrazam)、亞汰尼(isotianil)、嘉賜黴素(kasugamycin)、克收欣(kresoxim-methyl)、鋅錳乃浦(mancozeb)、曼普胺(mandipropamid)、mandestrobin、錳乃浦(maneb)、mapanipyrin、滅普寧(mepronil)、硝苯菌酯(meptyldinocap)、滅達樂(metalaxyl)(包括右滅達樂(metalaxyl-M)/mefenoxam)、滅特座(metconazole)、滅速克(methasulfocarb)、免得爛(metiram)、苯氧菌胺(metominostrobin)、滅芬農(metrafenone)、邁克尼(myclobutanil)、萘替芬(naftitine)、新阿蘇仁(neo-asozin)(甲烷胂酸鐵)、尼瑞莫(nuarimol)、辛噻酮(octhilinone)、呋醯胺(ofurace)、肟醚菌胺(orysastrobin)、毆殺斯(oxadixyl)、氟噻唑吡乙酮(oxathiapiprolin)、歐索林酸(oxolinic acid)、噁咪唑(oxpoconazole)、嘉保信(oxycarboxin)、土黴素(oxytetracycline)、平克座(penconazole)、賓克隆(pencycuron)、平氟芬(penflufen)、吡噻菌胺(penthiopyrad)、稻痕酯(perfurazoate)、磷酸(phosphorous acid)(包括其鹽,例如福賽得(fosetyl-aluminm))、啶氧菌酯(picoxystrobin)、粉病靈(piperalin)、保粒黴素(polyoxin)、撲殺熱(probenazole)、撲克拉(prochloraz)、撲滅寧(procymidone)、普拔克(propamocarb)、普克利(propiconazole)、甲基鋅乃浦(propineb)、普快淨(proquinazid)、硫菌威(prothiocarb)、丙硫菌唑(prothioconazole)、百克敏(pyraclostrobin)、唑胺菌酯(pyrametostrobin)、唑菌酯(pyraoxystrobin)、白粉松(pyrazophos)、pyribencarb、pyributacarb、比芬諾(pyrifenox)、苯啶菌酮(pyriofenone)、perisoxazole、派美尼(pyrimethanil)、比芬諾(pyrifenox)、硝吡咯菌素(pyrrolnitrin)、百快隆(pyroquilon)、唑喹菌酮(quinconazole)、quinmethionate、快諾芬(quinoxyfen)、五氯硝苯(quintozene)、矽噻菌胺(silthiofam)、氟唑環菌胺(sedaxane)、矽氟唑(simeconazole)、螺環菌胺(spiroxamine)、鏈黴素(streptomycin)、硫(sulfur)、得克利(tebuconazole)、tebufloquin、葉枯酞(teclofthalam)、克枯爛(tecloftalam)、四氯硝基苯(tecnazene)、特比萘芬(terbinafine)、四克利(tetraconazole)、腐絕(thiabendazole)、賽氟滅(thifluzamide)、多保淨(thiophanate)、甲基多保淨(thiophanate-methyl)、得恩地(thiram)、噻醯菌胺(tiadinil)、脫克松(tolclofos-methyl)、三氟甲氧威(tolprocarb)、甲基益發靈(tolyfluanid)、三泰芬(triadimefon)、三泰隆(triadimenol)、嘧菌醇(triarimol)、咪唑嗪(triazoxide)、硫酸三銅(tribasic copper sulfate)、氯啶菌酯(triclopyricarb)、三得芬(tridemorph)、三氟敏(trifloxystrobin)、賽福座(triflumizole)、三嗎福胺三環唑(trimoprhamide tricyclazole)、三氟敏(trifloxystrobin)、賽福寧(triforine)、滅菌唑(triticonazole)、單克素(uniconazole)、維利黴素(validamycin)、纈菌胺(valifenalate)(亦稱為valifenal)、免克寧(vinclozolin)、鋅乃浦(zineb)、福美鋅(ziram)、座賽胺(zoxamide)、及1-[4-[4-[5-(2,6-二氟苯基)-4,5-二氫-3-異唑基]-2-噻唑基]-1-哌啶基]-2-[5-甲基-3-(三氟甲基)-1H
-吡唑-1-基]乙酮;殺線蟲劑,諸如氟吡菌醯胺(fluopyram)、賜派滅(spirotetramat)、硫敵克(thiodicarb)、福賽絕(fosthiazate)、阿巴汀(abamectin)、依普同(iprodione)、氟速芬(fluensulfone)、二硫化二甲基、tioxazafen、1,3-二氯丙烯(1,3-D)、斯美地(metam)(鈉及鉀)、邁隆(dazomet)、氯化苦(chloropicrin)、芬滅松(fenamiphos)、普伏松(ethoprophos)、硫線磷(cadusaphos)、托福松(terbufos)、imicyafos、毆殺滅(oxamyl)、加保扶(carbofuran)、tioxazafen、堅強桿菌(Bacillus firmus
)、及撤銷巴斯德氏菌(Pasteuria nishizawae
);殺菌劑,諸如鏈黴素(streptomycin);殺蟎劑,諸如三亞蹣(amitraz)、蟎離丹(chinomethionat)、克氯苯(chlorobenzilate)、錫蟎丹(cyhexatin)、大克蟎(dicofol)、氯蟎(dienochlor)、依殺蟎(etoxazole)、芬殺蟎(fenazaquin)、芬佈賜(fenbutatin oxide)、芬普寧(fenpropathrin)、芬普蟎(fenpyroximate)、合賽多(hexythiazox)、毆蟎多(propargite)、畢達本(pyridaben)、及得芬瑞(tebufenpyrad)。
在某些情況下,本發明之化合物與其他生物活性(尤其是無脊椎動物害蟲防制)化合物或藥劑(即,活性成分)之組合可導致大於相加(即,協同)效果。減少活性成分在環境中釋放的量,同時確保有效害蟲防制一直是理想的。當無脊椎動物害蟲防制活性成分之協同作用發生在給出農藝上令人滿意之無脊椎動物害蟲防制水準的施用率下時,此等組合可有利於減少作物生產成本及降低環境負擔。
本發明之化合物及其組成物可施用至經過基因轉形以表現對無脊椎動物害蟲有毒之蛋白質(諸如,蘇力菌德他內毒素)的植物。此種施用可提供更廣泛範圍之植物保護,並且有利於抗性管理。外源性施用之本發明無脊椎動物害蟲防制化合物的效果可能會與該表現之毒素蛋白質產生協同作用。
這些農業用保護劑(即,殺蟲劑、殺真菌劑、殺線蟲劑、殺蟎劑、除草劑、及生物藥劑)的一般參考文獻包括The Pesticide Manual, 13th Edition
, C.D. S. Tomlin, Ed., British Crop Protection Council, Farnham, Surrey, U.K., 2003及The BioPesticide Manual
,2nd Edition
, L. G. Copping, Ed., British Crop Protection Council, Farnham, Surrey, U.K., 2001。
無脊椎動物害蟲在農藝及非農藝應用中係藉由下列方式來防制:將一或多種本發明之化合物(一般呈組成物之形式)以生物有效量施用至害蟲之環境(包括農藝及/或非農藝侵害所在地)、施用至欲保護之區域、或直接施用至欲防制之害蟲。
因此,本發明包含一種用於在農藝及/或非農藝應用中防制無脊椎動物害蟲之方法,其包含使該無脊椎動物害蟲或其環境與生物有效量的本發明之一或多種化合物接觸,或者與包含至少一種此化合物之組成物或包含至少一種此化合物及生物有效量的至少一種額外生物活性化合物或藥劑之組成物接觸。包含本發明之化合物及生物有效量的至少一種額外生物活性化合物或藥劑之合適組成物實例包括顆粒組成物,其中該額外活性化合物係存在於與本發明之化合物相同的顆粒上,或存在於與本發明化合物不同之顆粒上。
為了達成與本發明之化合物或組成物接觸以保護田間作物免受無脊椎動物害蟲侵害,該化合物或組成物一般係在栽植前施用至該作物之種子、施用至作物植物之枝葉(例如,葉子、莖、花、果實)、或在栽植作物之前或之後施用至土壤或其他生長介質。
接觸方法之一個實施例係藉由噴灑。替代地,包含本發明之化合物的顆粒組成物可施用至植物枝葉或土壤。藉由使植物與包含本發明之化合物的組成物(以液體配方之土壤澆灌液施用、以顆粒配方施用至土壤、以苗箱處理或移植物之浸泡液施用)接觸,本發明之化合物亦可透過植物吸收來有效遞送。值得注意的是呈土壤澆灌液體配方形式的本發明之組成物。亦值得注意的是一種防制無脊椎動物害蟲之方法,其包含使該無脊椎動物害蟲或其環境與生物有效量的本發明之化合物接觸,或與包含生物有效量的本發明之化合物的組成物接觸。值得進一步注意的是此方法中之環境係土壤,並且該組成物係以土壤澆灌配方施用至該土壤。進一步值得注意的是本發明之化合物係藉由局部施用至侵害所在地而亦為有效的。其他接觸方法包括藉由直接及殘餘噴灑、空中噴灑、凝膠、種子塗層、微封裝、系統性吸收、餌料、耳標、藥丸、噴霧器、燻蒸劑、氣霧劑、塵粉、及許多其他方法來施用本發明之化合物或組成物。接觸方法之一個實施例係包含本發明之化合物或組成物的尺寸穩定肥料粒劑、棒劑、或片劑。本發明之化合物亦可浸透至用於製造無脊椎動物防制裝置(例如,昆蟲網)之材料中。
本發明之化合物可用於處理所有植物、植物部分、及種子。植物及種子品種與栽培品種可藉由習知繁殖及育種方法或藉由遺傳工程方法來獲得。基因改造植物或種子(基因轉殖植物或種子)係異種基因(轉殖基因)已穩定結合至該植物之基因組或種子之基因組者。藉由轉殖基因在植物基因組中之特定位置來定義的轉殖基因稱為轉形或基因轉殖事件。
根據本發明可處理之基因改造植物及種子栽培品種包括抵抗一或多種生物逆境(害蟲如線蟲、昆蟲、蟎、真菌等)或非生物逆境(乾旱、寒冷溫度、土壤鹽度等)者,或者含有其他所欲之特性者。植物及種子可經基因改造以展現例如下列性狀:耐除草劑性、抗昆蟲性、油特性(oil profile)受到修改、或耐乾旱性。
用本發明化合物處理基因改造植物及種子可導致超過相加或協同效果。舉例而言,施用率減少、活性範圍增廣、對生物/非生物逆境之耐性增加、或儲存穩定性增強可能大於預期來自本發明之化合物的施用對基因改造植物及種子的單純相加效果。
本發明之化合物亦可用於種子處理以保護種子免受無脊椎動物害蟲侵害。在本揭露及申請專利範圍之上下文中,處理種子意指使該種子與生物有效量的本發明之化合物接觸,而本發明之化合物一般係配製成本發明之組成物。此種子處理會保護種子免受無脊椎土壤害蟲侵害,並且通常亦可保護與從發芽種子發育出之幼苗的土壤接觸之根部及其他植物部分。種子處理亦可藉由本發明化合物或第二活性成分在發育中植物內之易位而提供枝葉保護。種子處理可應用於所有類型的種子,包括經基因轉殖以表現特種性狀之植物將由之發芽者。代表性實例包括表現對無脊椎動物害蟲有毒之蛋白質(諸如如蘇力菌毒素)或表現抗除草劑性(諸如草甘膦乙醯基轉換酶,其提供對草甘膦之抗性)者。用本發明之化合物進行種子處理亦可增加由該種子生長之植物的生長力。
種子處理之一種方法係藉由在播撒種子之前用本發明之化合物(即,以經配製組成物)噴灑種子或灑在種子上。針對種子處理而調配之組成物通常包含成膜劑或黏著劑。因此,本發明之種子塗佈組成物一般包含生物有效量的化合物1或式2化合物,以及成膜劑或黏著劑。可藉由將可流動懸浮濃縮物直接噴灑至種子滾動床中,然後乾燥種子來塗佈種子。替代地,可將其他配方類型(諸如濕粉劑、溶液、懸浮乳液、可乳化濃縮物、及水中之乳液)噴灑在種子上。此程序尤其可用於施加膜塗層在種子上。所屬技術領域中具有通常知識者可獲得各種塗佈機器及程序。合適的程序包括列於P. Kosters et al.,Seed Treatment: Progress and Prospects
, 1994 BCPC Mongraph No. 57中,及其中所列出之參考文獻中者。
化合物1或式2化合物及其組成物(無論是單獨還是與其他殺蟲劑、殺線蟲劑、及殺真菌劑組合)對於包括但不限於下列者之作物的種子處理尤其有用:玉蜀黍或玉米、大豆、棉花、穀物(例如,小麥、燕麥、大麥、黑麥、及稻米)、馬鈴薯、蔬菜、和油菜籽。
可與化合物1或式2化合物配製以提供可用於種子處理之其他殺蟲劑包括阿巴汀(abamectin)、亞滅培(acetamiprid)、阿納寧(acrinathrin)、三亞蹣(amitraz)、阿維菌素(avermectin)、印楝素(azadirachtin)、免速達(bensultap)、畢芬寧(bifenthrin)、布芬淨(buprofezin)、cadusafos、加保利(carbaryl)、加保扶(carbofuran)、培丹(cartap)、賽速安勃(chlorantraniliprole)、克凡派(chlorfenapyr)、克福隆(chlorfluazuron)、陶斯松(chlorpyrifos)、可尼丁(clothianidin)、氰蟲醯胺(cyantraniliprole)、賽扶寧(cyfluthrin)、貝他賽扶寧(beta-cyfluthrin)、賽洛寧(cyhalothrin)、伽瑪賽洛寧(gamma-cyhalothrin)、拉目達賽洛寧(lambda-cyhalothrin)、賽滅寧(cypermethrin)、亞滅寧(alpha-cypermethrin)、傑他賽滅寧(zeta-cypermethrin)、賽滅淨(cyromazine)、第滅寧(deltamethrin)、地特靈(dieldrin)、達特南(dinotefuran)、苯蟲醚(diofenolan)、因滅汀(emamectin)、安殺番(endosulfan)、益化利(esfenvalerate)、益斯普(ethiprole)、依芬寧(etofenprox)、依殺蟎(etoxazole)、芬硫克(fenothiocarb)、芬諾克(fenoxycarb)、芬化利(fenvalerate)、芬普尼(fipronil)、氟尼胺(flonicamid)、氟大滅(flubendiamide)、氟芬隆(flufenoxuron)、福化利(fluvalinate)、覆滅蟎(formetanate)、福賽絕(fosthiazate)、六伏隆(hexaflumuron)、愛美松(hydramethylnon)、益達胺(imidacloprid)、因得克(indoxacarb)、祿芬隆(lufenuron)、美氟綜(metaflumizone)、滅賜克(methiocarb)、納乃得(methomyl)、美賜平(methoprene)、滅芬諾(methoxyfenozide)、烯啶蟲胺(nitenpyram)、硝蟲噻嗪(nithiazine)、諾伐隆(novaluron)、毆殺滅(oxamyl)、派滅淨(pymetrozine)、除蟲菊素(pyrethrin)、畢達本(pyridaben)、啶蟲丙醚(pyridalyl)、嘧蟎胺(pyriminostrobin)、百利普芬(pyriproxyfen)、蘭諾定(ryanodine)、賜諾特(spinetoram)、賜諾殺(spinosad)、賜派芬(spirodiclofen)、賜滅芬(spiromesifen)、賜派滅(spirotetramat)、速殺氟(sulfoxaflor)、得芬諾(tebufenozide)、治滅寧(tetramethrin)、賽果培(thiacloprid)、賽速安(thiamethoxam)、硫敵克(thiodicarb)、殺蟲單(thiosultap-sodium)、泰滅寧(tralomethrin)、唑蚜威(triazamate)、三福隆(triflumuron)、蘇力菌德他內毒素、蘇力菌之所有品系、及核多角體病毒之所有品系。
可與化合物1或式2化合物配製以提供可用於種子處理之其他殺真菌劑包括安美速(amisulbrom)、亞托敏(azoxystrobin)、白克列(boscalid)、貝芬替(carbendazim)、萎鏽靈(carboxin)、克絕(cymoxanil)、環克座(cyproconazole)、待克利(difenoconazole)、達滅芬(dimethomorph)、扶吉胺(fluazinam)、護汰寧(fludioxonil)、氟喹唑(fluquinconazole)、氟比來(fluopicolide)氟嘧菌酯(fluoxastrobin)、護汰芬(flutriafol)、氟克殺(fluxapyroxad)、種菌唑(ipconazole)、依普同(iprodione)、滅達樂(metalaxyl)、mefenoxam、滅特座(metconazole)、邁克尼(myclobutanil)、巴克素(paclobutrazole)、平氟芬(penflufen)、啶氧菌酯(picoxystrobin)、丙硫菌唑(prothioconazole)、百克敏(pyraclostrobin)、氟唑環菌胺(sedaxane)、矽噻菌胺(silthiofam)、得克利(tebuconazole)、腐絕(thiabendazole)、甲基多保淨(thiophanate-methyl)、得恩地(thiram)、三氟敏(trifloxystrobin)、及滅菌唑(triticonazole)。
包含可用於種子處理之化合物1或式2化合物的組成物可進一步包含具有提供保護以免受植物病原真菌或細菌及/或土生動物(諸如線蟲)之有害影響的能力之細菌及真菌。展現殺線蟲性質之細菌可包括但不限於堅強桿菌(Bacillus firmus
)、仙人掌桿菌(Bacillus cereus
)、枯草桿菌(Bacillius subtiliis
)、及穿透巴斯德氏菌(Pasteuria penetrans
)。合適堅強桿菌(Bacillus firmus
)菌株係菌株CNCM I-1582 (GB-126),其可商購為BioNem™
。合適仙人掌桿菌(Bacillus cereus
)菌株係菌株NCMM I-1592。這兩種桿菌(Bacillus
)菌株係揭示於US 6,406,690。展現殺線蟲活性之其他合適細菌係B. amyloliquefaciens
IN937a及B. subtilis
菌株GB03。展現殺真菌性質之細菌可包括但不限於B. pumilus
菌株GB34。展現殺線蟲性質之真菌物種可包括但不限於Myrothecium verrucaria
、Paecilomyces lilacinus
、及Purpureocillium lilacinum
。
種子處理亦可包括一或多種天然來源之殺線蟲劑,諸如稱為harpin之誘導子蛋白(elicitor protein),其係分離自某些細菌性植物病原,諸如Erwinia amylovora
。實例係Harpin-N-Tek種子處理技術,其可獲得為N-Hibit™
Gold CST。
種子處理亦可包括一或多個豆科根部結瘤細菌(legume-root nodulating bacteria)物種,諸如微共生固氮細菌Bradyrhizobium japonicum
。這些接種劑可選地可包括一或多種脂質-幾丁質寡醣(LCO),其等係在豆科根部上之瘤形成起始期間由根瘤細菌所生產的結瘤(Nod)因子。例如,Optimize®品牌種子處理技術納入LCO Promoter Technology™
並結合接種劑。
種子處理亦可包括一或多種異黃酮,其可增加由菌根菌所致之根部移生程度。菌根菌藉由增強營養素(諸如水、硫酸鹽、硝酸鹽、磷酸鹽、及金屬)之根部吸收來改善植物生長。異構酮之實例包括但不限於金雀異黃酮、雞豆黃素A (biochanin
A)、芒柄花黃素(formononetin)、大豆黃酮(daidzein)、黃豆黃素(glycitein)、柑果苷素(hesperetin)、柚苷配基(naringenin)、及紅車軸草素(pratensein)。芒柄花黃素可獲得為菌根接種劑產品(諸如PHC Colonize® AG)中之活性成分。
種子處理亦可包括一或多種植物活化劑,其在接觸病原體後會誘發植物中之系統性獲得抗性。引發此等保護機制之植物活化劑的實例係阿拉酸式苯-S-甲基(acibenzolar-S
-methyl)。
經處理種子一般以每100 kg種子約0.1 g至1 kg(即,處理前種子之約0.0001至1重量%)的量包含本發明之化合物。配製用於種子處理之可流動懸浮液一般包含約0.5至約70%的活性成分、約0.5至約30%的成膜黏著劑、約0.5至約20%的分散劑、0至約5%的增稠劑、0至約5%的顏料及/或染料、0至約2%的消泡劑、0%至約1%的防腐劑、及0至約75%的揮發性液體稀釋劑。
本發明之化合物可結合入至餌料組成物中,該餌料組成物係由無脊椎動物害蟲所食用或在諸如陷阱、餌料台、及類似者之裝置中所使用。此種餌料組成物可呈粒劑之形式,其包含(a)活性成分,即生物有效量的化合物1或式2化合物(b)一或多種食物材料;可選地(c)引誘劑、及可選地(d)一或多種保濕劑。值得注意的是包含介於下列者之間的粒劑或餌料組成物:約0.001至5%活性成分、約40至99%食物材料及/或引誘劑;以及可選地約0.05至10%保濕劑,其在極低施用率下(尤其是在藉由攝食而非直接接觸而致死之活性成分劑量下)對於防制土壤無脊椎動物害蟲係有效的。一些食物材料可同時作用為食物來源及引誘劑。食物材料包括碳水化合物、蛋白質、及脂質。食物材料之實例係蔬菜粉、糖、澱粉、動物脂肪、植物油、酵母萃取物、及乳固形物。引誘劑之實例為氣味劑及增味劑,諸如水果或植物萃取物、香料、或其他動物或植物組分、費洛蒙、或已知可引誘目標無脊椎動物害蟲之其他藥劑。保濕劑(即,水分保持劑)之實例係二醇及其他多元醇、甘油、及山梨醇。值得注意的是一種餌料組成物(及一種利用此種餌料組成物之方法),其用以控制至少一種選自由螞蟻、白蟻、及蟑螂所組成之群組的無脊椎動物害蟲。用於防制無脊椎動物害蟲之裝置可包含本案餌料組成物及經調適以收納該餌料組成物之外殼,其中該外殼具有至少一個開口,該開口之尺寸允許該無脊椎動物害蟲通過該開口,所以該無脊椎動物害蟲可自外殼外部之位置接近該餌料組成物,並且其中該外殼係進一步經調適以被置放在該無脊椎動物害蟲之可能或已知活動所在地或其附近。
本發明之一個實施例關於一種用於防制無脊椎動物害蟲之方法,其包含將本發明之殺蟲劑組成物(與界面活性劑、固體稀釋劑、及液體稀釋劑配製之化合物1或式2化合物,或者化合物1或式2化合物與至少一種其他殺蟲劑之經配製混合物)用水稀釋,並且可選地添加佐劑以形成經稀釋組成物,然後使該無脊椎動物害蟲或其環境與有效量的該經稀釋組成物接觸。
雖然藉由用水稀釋足夠濃度之本案殺蟲組成物所形成的噴灑組成物可提供足以防制無脊椎動物害蟲之效力,但亦可將分開配製之佐劑產品添加至噴灑槽混合物。這些額外佐劑通常稱為「噴灑佐劑」或「槽混佐劑」,並且包括混合在噴灑槽中的任何物質以改善殺蟲劑之效能或改變噴灑混合物之物理性質。佐劑可係界面活性劑、乳化劑、石油基作物油、作物衍生之種子油、酸化劑、緩衝劑、增稠劑、或消泡劑。佐劑係用來增強效力(例如,生物可利用性、黏著性、滲透、覆蓋均勻性、及保護耐久性)、或最小化或消除與不相容性、起泡、漂移、蒸發、揮發、及降解相關聯的噴灑施用問題。為獲得最佳效能,針對活性成分、配方及目標(例如,作物、昆蟲害蟲)之性質來選擇佐劑。
在噴灑佐劑中,包括作物油、作物油濃縮物、植物油濃縮物、及甲基化種子油濃縮物之油最常用來改善殺蟲劑之效力,此可能是藉由促進更均勻且一致之噴灑沉積所致。在油或其他水不互溶液體可能會有造成植物毒性之顧慮的情況下,製備自本發明之組成物的噴灑組成物通常將不含有油基噴灑佐劑。然而,在油基噴灑佐劑所造成之植物毒性商業上不明顯的情況下,製備自本發明之組成物的噴灑組成物亦可含有油基噴灑佐劑,其可能會進一步增加無脊椎動物害蟲之防制,以及耐雨性(rainfastness)。
標示為「作物油」之產品一般含有95至98%石蠟或石油腦基石油油,以及1至2%的一或多種作用為乳化劑之界面活性劑。標示為「作物油濃縮物」之產品一般由80至85%的可乳化石油基油及15至20%之非離子性界面活性劑所組成。正確標示為「植物油濃縮物」之產品一般由80至85%的植物油(即,種子或果實油,最常來自棉花、亞麻子、大豆、或向日葵)及15至20%的非離子性界面活性劑所組成。佐劑效能可藉由將植物油更換為脂肪酸甲酯(一般衍生自植物油)來改善。甲基化種子油濃縮物之實例包括MSO®
Concentrate (UAP-Loveland Products, Inc.)及Premium MSO Methylated Spray Oil (Helena Chemical Company)。
添加至噴灑混合物之佐劑的量通常不超過約2.5體積%,並且更一般而言該量係約0.1至約1體積%。添加佐劑至噴灑混合物之施用率一般介於每公頃1至5 L之間。噴灑佐劑之代表性實例包括:Adigor®
(Syngenta)在液體烴中之47%甲基化菜籽油、Silwet®
(Helena Chemical Company)聚環氧烷改質之七甲基三矽氧烷、及Assist®
(BASF)在83%石蠟基礦物油中之17%界面活性劑摻合物。
本發明之化合物可在無其他佐劑的情況下施用,但最常施用的將是包含一或多種活性成分及取決於所預期的最終用途具有合適載劑、稀釋劑、與界面活性劑之配方,並且可能與食物組合。一種施用方法涉及噴灑本發明之化合物的水分散液或精製油溶液。與噴霧油、噴霧油濃縮物、展布黏著劑、佐劑、其他溶劑、及協力劑(諸如向日葵基丁氧化物(piperonyl butoxide))組合經常會增強化合物效力。針對非農藝用途,此等噴灑劑可藉由泵而自噴灑容器(諸如,桶子、瓶子、或其他容器)施用,或藉由自加壓容器(例如,加壓氣霧劑噴灑桶)將其釋出而施用。此等噴灑組成物可採用各種形式,例如,噴灑劑、水霧、泡沫、煙氣、或霧氣。因此,此等噴灑組成物可視情況需要進一步包含推進劑、發泡劑等。值得注意的是包含生物有效量的本發明之化合物或組成物及載劑之噴灑組成物。此噴灑組成物之一個實施例包含生物有效量的本發明之化合物或組成物及推進劑。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、氫氟碳化物、戊烷、氫氟碳化物、氯氟碳化物、二甲基醚、及上述者之混合物。值得注意的是一種用以防制至少一種選自由下列所所組成之群組的無脊椎動物害蟲之噴灑組成物(及一種利用此種噴灑組成物施配自噴灑容器之方法):蚊子、黑蠅、廄蠅、鹿蠅、馬蠅、胡蜂、黃胡蜂、大黃蜂、蜘蛛、螞蟻、蚋、及類似者,包括個別或組合。
下列測試顯示本發明之化合物對特定害蟲的防制效力。「防制效力」代表無脊椎動物害蟲發育之抑制(包括死亡)而造成攝食顯著減少。然而,該等化合物所提供之害蟲防制保護不限於這些物種。
本發明之生物實例
用於測試A至D之配方及噴灑方法
測試化合物係使用含有10%丙酮、90%水、及300 ppm X-77® Spreader Lo-Foam Formula非離子性界面活性劑(Loveland Industries, Inc. Greeley, Colorado, USA)之溶液來配製,該界面活性劑含有烷基芳基聚氧乙烯、游離脂肪酸、二醇、及異丙醇。將經配製之化合物透過具有1/8 JJ定製本體之SUJ2噴霧器噴嘴(Spraying Systems Co. Wheaton, Illinois, USA)來施用於1 mL的液體中,該噴嘴位在各測試單元之頂部上方1.27 cm(0.5吋)。將測試化合物以所指示之比率噴灑,並且將各測試重複三次。
測試A
為了評估經由接觸及/或系統性方式對綠桃蚜(Myzus persicae
(Sulzer))之防制,測試單元係由小開口容器與其內之12至15天齡蘿蔔植物所組成。此係藉由在一片自培養植物切下之葉子上(切葉法)放置30至40隻蚜蟲(在測試植物的一片葉子上)來預侵害。蚜蟲會隨著葉片乾掉而移至測試植物上。在預侵害後,用一層砂覆蓋測試單元之土壤。
配製測試化合物並以250及/或50 ppm噴灑。在噴灑完經配製之測試化合物後,讓各測試單元乾燥1小時,然後將黑色網蓋放在頂部。將測試單元在生長室中在19至21℃及50至70%相對濕度下保持6天。接著目視評估各測試單元的昆蟲死亡率。
在250 ppm下測試之化合物中,下列化合物導致至少80%死亡率:1及2a。
在50 ppm下測試之化合物中,下列化合物導致至少80%死亡率:1、2a、2b、及2c。
測試B
為了評估經由接觸及/或系統性方式對棉瓜蚜蟲(Aphis gossypii
(Glover))之防制,測試單元係由小開口容器與其內之6至7天齡棉花植物所組成。此係根據切葉法用30至40隻昆蟲在一片葉子上預侵害,然從用一層砂覆蓋測試單元之土壤。
配製測試化合物並以250及/或50 ppm噴灑。在噴灑後,將測試單元在生長室中在19℃及70%相對濕度下維持6天。接著目視評估各測試單元的昆蟲死亡率。
在50 ppm下測試之化合物中,下列化合物導致至少80%死亡率:1、2a、2b、及2c。
測試C
為了評估經由接觸及/或系統性方式對甘藷粉蝨(Bemisia tabaci
(Gennadius))之防制,測試單元係由小開口容器與其內之12至14天齡棉花植物所組成。在噴灑施用前,將兩個子葉自植物移除,留下用於檢定之一個真葉。讓成體粉蝨在植物上下蛋,然後將其自測試單元移除。將用至少15個蛋侵染之棉花植物送交測試以進行噴灑。
配製測試化合物並以250及/或50 ppm噴灑。在噴灑後,讓測試單元乾燥1小時。接著將圓筒移除,然後將測試單元拿到生長室並且在28℃及50至70%相對濕度下保持13天。接著目視評估各測試單元的昆蟲死亡率。
在250 ppm下測試之化合物中,下列導致至少50%死亡率:1及2b。
在50 ppm下測試之化合物中,下列導致至少50%死亡率:1。
測試D
為了評估經由接觸及/或系統性方式對西方花薊馬(Frankliniellla occidentalis
(Pergande))之防制,測試單元係由小開口容器與其內之5至7天齡Soleil豆植物所組成。
配製測試化合物並以250及/或50 ppm噴灑。在噴灑後,讓測試單元乾燥1小時,接著將22至27隻成體薊馬添加至各單元。將黑色網蓋放在頂部,然後將測試單元在25℃及45至55%相對濕度下保持6天。
在250 ppm下測試之化合物中,下列化合物提供極佳至優良程度之防制效力水準(30%或更低之植物損傷及/或100%死亡率):1、2a、及2b。
在50 ppm下測試之化合物中,下列化合物提供極佳至優良程度之防制效力水準(30%或更低之植物損傷及/或100%死亡率):1、2a、及2b。
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Claims (11)
- 如請求項1之化合物1。
- 如請求項1之式2化合物,其中n係0。
- 如請求項1之式2化合物,其中n係1。
- 如請求項1之式2化合物,其中n係2。
- 如請求項1之化合物,其中該化合物係選自N -[1-(二氟甲基)環丙基]-2-(3-吡啶基)-2H -吲唑-4-甲醯胺、N -[1,1-二甲基-2-(甲基硫基)乙基]-7-氟-2-(3-吡啶基)-2H -吲唑-4-甲醯胺、N -[1,1-二甲基-2-(甲基亞磺醯基)乙基]-7-氟-2-(3-吡啶基)-2H -吲唑-4-甲醯胺、及N -[1,1-二甲基-2-(甲基磺醯基)乙基]-7-氟-2-(3-吡啶基)-2H -吲唑-4-甲醯胺;或任何前述化合物之組合。
- 一種組成物,其包含請求項1之化合物及至少一種選自由界面活性劑、固體稀釋劑、及液體稀釋劑所組成之群組的額外組分,該組成物可選地進一步包含至少一種額外生物活性化合物或藥劑。
- 如請求項7之組成物,其中該至少一種額外生物活性化合物或藥劑係選自於由下列所組成之群組:阿巴汀(abamectin)、毆殺松(acephate)、亞醌蟎(acequinocyl)、亞滅培(acetamiprid)、阿納寧(acrinathrin)、雙丙環蟲脂(afidopyropen)、磺胺蟎酯(amidoflumet)、三亞蹣(amitraz)、阿維菌素(avermectin)、印楝素(azadirachtin)、谷速松(azinphos-methyl)、免扶克(benfuracarb)、免速達(bensultap)、畢芬寧(bifenthrin)、必芬蟎(bifenazate)、雙三氟蟲脲(bistrifluron)、硼酸酯(borate)、布芬淨(buprofezin)、加保利(carbaryl)、加保扶(carbofuran)、培丹(cartap)、殺蟲脒(carzol)、賽速安勃(chlorantraniliprole)、克凡派(chlorfenapyr)、克福隆(chlorfluazuron)、陶斯松(chlorpyrifos)、甲基陶斯松(chlorpyrifos-methyl)、可芬諾(chromafenozide)、克芬蟎(clofentezin)、可尼丁(clothianidin)、氰蟲醯胺(cyantraniliprole)、環溴蟲醯胺(cyclaniliprole)、乙氰菊酯(cycloprothrin)、環氧蟲啶(cycloxaprid)、賽芬蟎(cyflumetofen)、賽扶寧(cyfluthrin)、貝他賽扶寧(beta-cyfluthrin)、賽洛寧(cyhalothrin)、伽瑪賽洛寧(gamma-cyhalothrin)、拉目達賽洛寧(lambda-cyhalothrin)、賽滅寧(cypermethrin)、亞滅寧(alpha-cypermethrin)、傑他賽滅寧(zeta-cypermethrin)、賽滅淨(cyromazine)、第滅寧(deltamethrin)、汰芬隆(diafenthiuron)、大利松(diazinon)、地特靈(dieldrin)、二福隆(diflubenzuron)、四氟甲醚菊酯(dimefluthrin)、殺蟲雙(dimehypo)、大滅松(dimethoate)、達特南(dinotefuran)、苯蟲醚(diofenolan)、因滅汀(emamectin)、安殺番(endosulfan)、益化利(esfenvalerate)、益斯普(ethiprole)、依芬寧(etofenprox)、依殺蟎(etoxazole)、芬佈賜(fenbutatin oxide)、撲滅松(fenitrothion)、芬硫克(fenothiocarb)、芬諾克(fenoxycarb)、芬普寧(fenpropathrin)、芬化利(fenvalerate)、芬普尼(fipronil)、弗美托奎(flometoquin)、氟尼胺(flonicamid)、氟大滅(flubendiamide)、護賽寧(flucythrinate)、嘧蟲胺(flufenerim)、氟芬隆(flufenoxuron)、氟菌蟎酯(flufenoxystrobin)、弗芬梭分(flufensulfone)、氟吡菌醯胺(fluorpyram)、弗皮洛(flupiprole)、氟吡呋喃酮(flupyradifurone)、福化利(fluvalinate)、氟胺氰菊酯(tau-fluvalinate)、大福松(fonophos)、覆滅蟎(formetanate)、福賽絕(fosthiazate)、合芬隆(halofenozide)、右旋七氟甲醚菊酯(heptafluthrin)、六伏隆(hexaflumuron)、合賽多(hexythiazox)、愛美松(hydramethylnon)、益達胺(imidacloprid)、因得克(indoxacarb)、殺蟲皂(insecticidal soaps)、亞芬松(isofenphos)、祿芬隆(lufenuron)、馬拉松(malathion)、氯氟醚菊酯(meperfluthrin)、美氟綜(metaflumizone)、聚乙醛(metaldehyde)、達馬松(methamidophos)、滅大松(methidathion)、滅蟲威(methiodicarb)、納乃得(methomyl)、美賜平(methoprene)、甲氧滴滴梯(methoxychlor)、美特寧(metofluthrin)、亞素靈(monocrotophos)、單福寧(monofluthrin)、滅芬諾(methoxyfenozide)、烯啶蟲胺(nitenpyram)、硝蟲噻嗪(nithiazine)、諾伐隆(novaluron)、諾福隆(noviflumuron)、毆殺滅(oxamyl)、巴拉松(parathion)、甲基巴拉松(parathion-methyl)、百滅寧(permethrin)、福瑞松(phorate)、裕必松(phosalone)、益滅松(phosmet)、福賜米松(phosphamidon)、比加普(pirimicarb)、佈飛松(profenofos)、丙氟菊酯(profluthrin)、毆蟎多(propargite)、丙苯烴菊酯(protrifenbute)、吡氟布米得(pyflubumide)、派滅淨(pymetrozine)、啶吡唑蟲胺(pyrafluprole)、除蟲菊素(pyrethrin)、畢達本(pyridaben)、啶蟲丙醚(pyridalyl)、吡立芙淇納蔥(pyrifluquinazon)、嘧蟎胺(pyriminostrobin)、pyriprole、百利普芬(pyriproxyfen)、魚藤酮(rotenone)、蘭諾定(ryanodine)、矽護芬(silafluofen)、賜諾特(spinetoram)、賜諾殺(spinosad)、賜派芬(spirodiclofen)、賜滅芬(spiromesifen)、賜派滅(spirotetramat)、硫丙磷(sulprofos)、速殺氟(sulfoxaflor)、得芬諾(tebufenozide)、得芬瑞(tebufenpyrad)、得福隆(teflubenzuron)、七氟菊酯(tefluthrin)、托福松(terbufos)、樂本松(tetrachlorvinphos)、治滅寧(tetramethrin)、四氟醚菊酯(tetramethylfluthrin)、賽果培(thiacloprid)、賽速安(thiamethoxam)、硫敵克(thiodicarb)、殺蟲單(thiosultap-sodium)、脫芬瑞(tolfenpyrad)、泰滅寧(tralomethrin)、唑蚜威(triazamate)、三氯松(trichlorfon)、三福隆(triflumuron)、蘇力菌(Bacillus thuringiensis )之所有品系、昆蟲病原細菌(entomopathogenic bacteria)、核多角體病毒(Nucleo polyhedrosis viruses)之所有品系、昆蟲病原病毒(entomopathogenic viruses)、及昆蟲病原真菌(entomopathogenic fungi)。
- 如請求項7之組成物,其中該至少一種額外生物活性化合物或藥劑係選自於由下列所組成之群組:阿巴汀(abamectin)、亞滅培(acetamiprid)、阿納寧(acrinathrin)、雙丙環蟲脂(afidopyropen)、三亞蹣(amitraz)、阿維菌素(avermectin)、印楝素(azadirachtin)、免扶克(benfuracarb)、免速達(bensultap)、畢芬寧(bifenthrin)、3-溴-1-(3-氯-2-吡啶基)-N -[4-氰基-2-甲基-6-[(甲基胺基)羰基]苯基]-1H -吡唑-5-甲醯胺、布芬淨(buprofezin)、加保利(carbaryl)、培丹(cartap)、賽速安勃(chlorantraniliprole)、克凡派(chlorfenapyr)、陶斯松(chlorpyrifos)、可尼丁(clothianidin)、氰蟲醯胺(cyantraniliprole)、環溴蟲醯胺(cyclaniliprole)、乙氰菊酯(cycloprothrin)、賽扶寧(cyfluthrin)、貝他賽扶寧(beta-cyfluthrin)、賽洛寧(cyhalothrin)、拉目達賽洛寧(lambda-cyhalothrin)、伽瑪賽洛寧(gamma-cyhalothrin)、賽滅寧(cypermethrin)、亞滅寧(alpha-cypermethrin)、傑他賽滅寧(zeta-cypermethrin)、賽滅淨(cyromazine)、第滅寧(deltamethrin)、地特靈(dieldrin)、達特南(dinotefuran)、苯蟲醚(diofenolan)、因滅汀(emamectin)、安殺番(endosulfan)、益化利(esfenvalerate)、益斯普(ethiprole)、依芬寧(etofenprox)、依殺蟎(etoxazole)、撲滅松(fenitrothion)、芬硫克(fenothiocarb)、芬諾克(fenoxycarb)、芬化利(fenvalerate)、芬普尼(fipronil)、弗美托奎(flometoquin)、氟尼胺(flonicamid)、氟大滅(flubendiamide)、氟芬隆(flufenoxuron)、氟菌蟎酯(flufenoxystrobin)、弗芬梭分(flufensulfone)、弗皮洛(flupiprole)、氟吡呋喃酮(flupyradifurone)、福化利(fluvalinate)、覆滅蟎(formetanate)、福賽絕(fosthiazate)、右旋七氟甲醚菊酯(heptafluthrin)、六伏隆(hexaflumuron)、愛美松(hydramethylnon)、益達胺(imidacloprid)、因得克(indoxacarb)、祿芬隆(lufenuron)、氯氟醚菊酯(meperfluthirn)、美氟綜(metaflumizone)、滅蟲威(methiodicarb)、納乃得(methomyl)、美賜平(methoprene)、滅芬諾(methoxyfenozide)、美特寧(metofluthrin)、單福寧(monofluthrin)、烯啶蟲胺(nitenpyram)、硝蟲噻嗪(nithiazine)、諾伐隆(novaluron)、毆殺滅(oxamyl)、吡氟布米得(pyflubumide)、派滅淨(pymetrozine)、除蟲菊素(pyrethrin)、畢達本(pyridaben)、啶蟲丙醚(pyridalyl)、嘧蟎胺(pyriminostrobin)、百利普芬(pyriproxyfen)、蘭諾定(ryanodine)、賜諾特(spinetoram)、賜諾殺(spinosad)、賜派芬(spirodiclofen)、賜滅芬(spiromesifen)、賜派滅(spirotetramat)、速殺氟(sulfoxaflor)、得芬諾(tebufenozide)、治滅寧(tetramethrin)、賽果培(thiacloprid)、賽速安(thiamethoxam)、硫敵克(thiodicarb)、殺蟲單(thiosultap-sodium)、泰滅寧(tralomethrin)、四氟醚菊酯(tetramethylfluthrin)、唑蚜威(triazamate)、三福隆(triflumuron)、蘇力菌(Bacillus thuringiensis )之所有品系、及核多角體病毒(Nucleo polyhedrosis viruses)之所有品系。
- 一種防制無脊椎動物害蟲之方法,其包含使該無脊椎動物害蟲或其環境與生物有效量的如請求項1之化合物接觸。
- 一種經處理之種子,其以該種子處理前之約0.0001至1重量%的量包含如請求項1之化合物。
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