TW201741299A - 作為殺蟲劑之經取代咪唑基甲醯胺類 - Google Patents
作為殺蟲劑之經取代咪唑基甲醯胺類 Download PDFInfo
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- TW201741299A TW201741299A TW106104209A TW106104209A TW201741299A TW 201741299 A TW201741299 A TW 201741299A TW 106104209 A TW106104209 A TW 106104209A TW 106104209 A TW106104209 A TW 106104209A TW 201741299 A TW201741299 A TW 201741299A
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- DDVNRFNDOPPVQJ-HQJQHLMTSA-N transfluthrin Chemical compound CC1(C)[C@H](C=C(Cl)Cl)[C@H]1C(=O)OCC1=C(F)C(F)=CC(F)=C1F DDVNRFNDOPPVQJ-HQJQHLMTSA-N 0.000 description 1
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- JWXZLCFGVKMEEK-UHFFFAOYSA-N triarathene Chemical compound C1=CC(Cl)=CC=C1C1=CC(C=2C=CC=CC=2)=C(C=2C=CC=CC=2)S1 JWXZLCFGVKMEEK-UHFFFAOYSA-N 0.000 description 1
- NKNFWVNSBIXGLL-UHFFFAOYSA-N triazamate Chemical compound CCOC(=O)CSC1=NC(C(C)(C)C)=NN1C(=O)N(C)C NKNFWVNSBIXGLL-UHFFFAOYSA-N 0.000 description 1
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- KVSKGMLNBAPGKH-UHFFFAOYSA-N tribromosalicylanilide Chemical compound OC1=C(Br)C=C(Br)C=C1C(=O)NC1=CC=C(Br)C=C1 KVSKGMLNBAPGKH-UHFFFAOYSA-N 0.000 description 1
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- DQJCHOQLCLEDLL-UHFFFAOYSA-N tricyclazole Chemical compound CC1=CC=CC2=C1N1C=NN=C1S2 DQJCHOQLCLEDLL-UHFFFAOYSA-N 0.000 description 1
- ONCZDRURRATYFI-TVJDWZFNSA-N trifloxystrobin Chemical compound CO\N=C(\C(=O)OC)C1=CC=CC=C1CO\N=C(/C)C1=CC=CC(C(F)(F)F)=C1 ONCZDRURRATYFI-TVJDWZFNSA-N 0.000 description 1
- GWBQKPSBYMTNOO-UHFFFAOYSA-N trilithium butan-1-olate Chemical compound [O-]CCCC.[O-]CCCC.[O-]CCCC.[Li+].[Li+].[Li+] GWBQKPSBYMTNOO-UHFFFAOYSA-N 0.000 description 1
- 229960001082 trimethoprim Drugs 0.000 description 1
- IEDVJHCEMCRBQM-UHFFFAOYSA-N trimethoprim Chemical compound COC1=C(OC)C(OC)=CC(CC=2C(=NC(N)=NC=2)N)=C1 IEDVJHCEMCRBQM-UHFFFAOYSA-N 0.000 description 1
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- DBXFMOWZRXXBRN-LWKPJOBUSA-N valifenalate Chemical compound CC(C)OC(=O)N[C@@H](C(C)C)C(=O)NC(CC(=O)OC)C1=CC=C(Cl)C=C1 DBXFMOWZRXXBRN-LWKPJOBUSA-N 0.000 description 1
- LESVOLZBIFDZGS-UHFFFAOYSA-N vamidothion Chemical compound CNC(=O)C(C)SCCSP(=O)(OC)OC LESVOLZBIFDZGS-UHFFFAOYSA-N 0.000 description 1
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- WCJYTPVNMWIZCG-UHFFFAOYSA-N xylylcarb Chemical compound CNC(=O)OC1=CC=C(C)C(C)=C1 WCJYTPVNMWIZCG-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- A01N43/50—1,3-Diazoles; Hydrogenated 1,3-diazoles
-
- 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
-
- 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
- A01N43/64—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
- A01N43/647—Triazoles; Hydrogenated triazoles
- A01N43/653—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- 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
- A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
- A01N43/84—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms six-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,4
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Health & Medical Sciences (AREA)
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- Pest Control & Pesticides (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Tropical Medicine & Parasitology (AREA)
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- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Plural Heterocyclic Compounds (AREA)
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- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
本發明係關於式(I)化合物□其中,Q,V,T,W,Y,L1,L2及A具有說明書中所述定義-及關於其等於控制動物蟲害之用途。
Description
本發明係關於新穎雜環化合物,其等之製備方法及中間體及其等於控制動物蟲害之用途。
WO 2011/009804 A2係說明雜環化合物,特別是,包括可用作為殺昆蟲劑之咪唑基甲醯胺類。然而,咪唑基環直接被胺基基團取代的咪唑基甲醯胺類並未被說明。該列於WO 2011/009804 A2之咪唑基甲醯胺類的殺昆蟲作用相當弱。
現代殺昆蟲劑必須滿足諸多要求,例如關於其作用的程度,持續性及範圍以及可能的用途。毒性問題,保護有益品種及授粉者,環境特性,施用率,與其他活性組成份或調配物輔助劑的合併扮演一角色,合成活性組成份所需努力的問題也是如此;再者,可能會出現抗性,只提一些參數。僅由於所有這些原因,對於新穎作物保護組合物的尋找不被認為完整,且與已知化合物相較,不斷的需要有具備改良特性之新穎化合物,至少在個別方面。
本發明之目的係提供化合物,其在各方面擴大了殺蟲劑之作用譜。
此目的,及未被明確陳述,而可從本文所討論的連接中被辨別或導出
之其他目的,係藉由式(I)化合物之提供來達成
其中(具體例(0))Q 代表氧或硫,V 代表來自包括氫,鹵素,烷基,鹵烷基,烷氧基,鹵烷氧基及氰基之基團,W 代表來自包括氫,鹵素,烷基,鹵烷基,烷氧基,鹵烷氧基及氰基之基團,Y 代表來自包含下列之基團:氫,氰基,可選擇地經取代之烷基、烯基或炔基,可選擇地經取代之環烷基其可選擇地插入雜原子,可選擇地經取代之環烷基烷基其可選擇地插入雜原子,芳基烷基或雜芳基烷基,A 代表來自包含下列之基團:氫,可選擇地經取代之烷基、烯基或炔基及可選擇地經取代之環烷基或環烷基烷基其可選擇地插入雜原子,T 代表氧或一電子對,L1 代表來自包含下列之基團:氫,可選擇地經取代之烷基,烯基,炔基或環烷基並代表基團C(O)R2,C(O)N(R3)(R4),C(O)OR5及SO2R6,L2 代表來自包含下列之基團:氫,N(R3a)(R4a),可選擇地經取代之烷基,烯基,炔基或烷氧基,可選擇地經取代之環烷基或環烷基烷基其可選擇地插入雜原子,及可選擇地經取代之芳基,芳基烷基,雜芳基或雜
芳基烷基,或L1及L2 與其等所連接之氮原子一起,代表可選擇地經取代之具有3至7個環原子之飽和,部份飽和或芳族雜環其可可選擇地插入其他雜原子及/或一個或兩個C=O基團,R2 代表來自包含下列之基團:氫,可選擇地經取代之烷基,烯基或炔基,可選擇地經取代之環烷基,可選擇地經取代之芳基或雜芳基及可選擇地經取代之芳基烷基或雜芳基烷基,R3及R4 各自獨立代表來自包含下列之基團:氫,可選擇地經取代之烷基,烯基或炔基,可選擇地經取代之飽和或不飽和環烷基,環烷基烷基,芳基,雜芳基,芳基烷基或雜芳基烷基,或R3及R4 一起形成可選擇地經取代之三-至七-員脂族環其任意含有氮,硫或氧原子,R3a 代表來自包含下列之基團:氫,可選擇地經取代之烷基,可選擇地經取代之環烷基,芳基,雜芳基,芳基烷基或雜芳基烷基,R4a 代表來自包含下列之基團:氫,可選擇地經取代之烷基,可選擇地經取代之C3-C6-環烷基且代表基團C(O)R2,C(O)OR5及SO2R6,R5 代表可選擇地經取代之烷基,烯基或炔基,可選擇地經取代之環烷基或環烷基烷基,R6 代表來自包括可選擇地經取代之烷基,烯基或炔基,可選擇地經取代之環烷基,環烷基烷基,芳基,芳基烷基,雜芳基或雜芳基烷基之基團,及其鹽類。
於式(I)化合物中之基團之較佳的取代基或範圍係闡述如下。其等之組
合形成較佳範圍(1-1)。
Q 代表氧或硫,V 代表來自包括氫,鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基及氰基之基團,W 代表來自包括氫,鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基及氰基之基團,Y 代表來自包含下列之基團:氫,C1-C6-烷基,C3-C6-烯基或C3-C6-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基,C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,直鏈或分支之C3-C8-環烷基-C1-C4-烷基,彼此獨立可選擇地插入下列者單-或兩次:O,S(O)n,CO或NR4a且彼此獨立可選擇地被下列者所單-至四取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,芳基-C1-C4-烷基或雜芳基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,A 代表來自包含下列之基團:氫,C1-C6-烷基,C3-C6-烯基或C3-C6-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基及C3-C6-環烷基或C3-C8-環烷基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基及C1-C6-烷基,C3-C6-烯基或C3-C6-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基,及直鏈或分支之C3-C8-環烷基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-
烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,T 代表氧或一電子對,L1 代表來自包含下列之基團:氫,C1-C4-烷基,C3-C6-烯基或C3-C6-炔基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基,C3-C6-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基且代表基團C(O)R2,C(O)N(R3)(R4),C(O)OR5及SO2R6,L2 代表來自包含下列之基團:氫,-N(R3a)(R4a),C1-C4-烷基,C3-C6-烯基,C3-C6-炔基或C1-C4-烷氧基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基,直鏈或分支之C3-C8-環烷基或C3-C8-環烷基-C1-C4-烷基,彼此獨立可選擇地插入下列者單-或兩次:O,S(O)n,CO或NR4a且彼此獨立可選擇地被下列者所單-至四取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,芳基,雜芳基,芳基烷基或雜芳基烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,或L1及L2 與N一起代表來自基團U-1至U-36之雜環,
Xb 代表來自包含下列之基團:鹵素,硝基,氰基,C1-C4-烷基,C3-C6-環烷基,C1-C5-鹵素烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基,C3-C6-鹵代環烷基,C1-C4-烷氧基-C1-C4-烷基,氰基-C1-C4-烷基,C3-C6-環烷基-C1-C4-烷基,C2-C6-烯基,C3-C6-炔基,C1-C4-烷基-S(O)n-,
C1-C4-烷基羰基,C1-C6-鹵烷基羰基,C1-C6-烷氧基羰基,C1-C6-烷基胺基羰基,二-(C1-C6)烷基胺基羰基,C1-C6-烷基羰基胺基,芳基及雜芳基,其中該取代基芳基及雜芳基可可選擇地被相同或不同包含下列之取代基所單-或多取代:鹵素,氰基,硝基,C1-C6-烷基,C2-C6-烯基,C2-C6-炔基,C1-C4-烷氧基,C1-C4-鹵烷基,C1-C6-鹵烷氧基及C1-C4-烷基硫基且其中該於U-13,U-14,U-16,U-28及U-35上之環氮原子未被鹵素,硝基,氰基,C1-C4-烷氧基,C1-C4-鹵烷氧基,C1-C4-烷氧基-C1-C4-烷基氧基所取代,R2 代表來自包含下列之基團:氫,C1-C8-烷基,C3-C8-烯基或C3-C8-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基或C1-C4-烷基-S(O)n-,C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,芳基或雜芳基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基及直鏈或分支之芳基-C1-C4-烷基或雜芳基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,R3,R4 彼此獨立代表來自包含下列之基團:氫,C1-C8-烷基,C3-C8-烯基或C3-C8-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基或C1-C4-烷基-S(O)n-,C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,芳基或雜芳基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,
C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基及直鏈或分支之芳基-C1-C4-烷基或雜芳基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,R3a 代表來自包含下列之基團:氫,C1-C8-烷基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,氰基或C1-C4-烷氧基,C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基或C1-C4-烷氧基,芳基或雜芳基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基及直鏈或分支之芳基-C1-C4-烷基或雜芳基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,硝基或氰基,R4a 代表來自包含下列之基團:氫,C1-C4-烷基,彼此獨立可選擇地被下列者所單-至多取代:鹵素或C1-C4-烷氧基,C3-C6-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基或C1-C4-烷氧基且代表基團C(O)R2,C(O)OR5及SO2R6,R5 代表C1-C8-烷基,C3-C8-烯基或C3-C8-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基或C1-C4-烷基-S(O)n-,C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,R6 代表來自包含下列之基團:C1-C8-烷基,C3-C8-烯基或C3-C8-炔
基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基或C1-C4-烷基-S(O)n-,C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,芳基或雜芳基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,m 代表0,1,2或3之數目,n 代表0,1或2之數目,及其鹽類。
列於式(I)化合物中之基團之其他較佳的取代基或範圍係闡述如下。其等之組合形成較佳範圍(1-2),其中Q,V,W,Y,A,T,L1,L2,R2,R3,R4,R3a,R4a,R5,R6,m及n係定義如在較佳範圍(1-1)內之定義,且Xb 代表來自包含下列之基團:鹵素,硝基,氰基,胺基,C1-C4-烷基,C3-C6-環烷基,C1-C5-鹵烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基,C3-C6-鹵代環烷基,C1-C4-烷氧基-C1-C4-烷基,氰基-C1-C4-烷基,C3-C6-環烷基-C1-C4-烷基,C2-C6-烯基,C3-C6-炔基,C1-C4-烷基-S(O)n-,C1-C4-烷基羰基,C1-C6-鹵烷基羰基,C1-C6-烷氧基羰基,C1-C6-烷基胺基羰基,二-(C1-C6)烷基胺基羰基,C1-C6-烷基羰基胺基,芳基及雜芳基,其中之取代基芳基及雜芳基可可選擇地被相同或不同包含下列之取代基所單-至多取代:鹵素,氰基,硝基,C1-C6-烷基,C2-C6-烯基,C2-C6-炔基,C1-C4-烷氧基,C1-C4-鹵烷基,C1-C6-鹵烷氧基及C1-C4-烷基硫代且其中於U-13,U-14,U-16及U-28上之環氮原子未被鹵素,硝基,氰基,
C1-C4-烷氧基,C1-C4-鹵烷氧基,C1-C4-烷氧基-C1-C4-烷基氧基所取代,或Xb 代表C2-C5-碳鏈,其可選擇地含有1個選自包含N,S及O之雜原子,其係連接至兩個相鄰的環位置且其係形成脂族,芳族,雜芳族或雜環,於此情況下m等於2。於式(I)化合物中之基團之特別佳的取代基或範圍係闡述如下。其等之組合形成較佳範圍(2-1)。
Q 代表氧,V 代表來自包含氫,氟,氯,溴,甲基及乙基之基團,W 代表來自包含氫,氟,氯,溴,氰基及甲基之基團,Y 代表來自包含下列之基團:氫,C1-C4-烷基,C3-C4-烯基或C3-C4-炔基,彼此獨立可選擇地被下列者所單-至五取代:氟,氯,溴,甲氧基或乙氧基,且C3-C6-環烷基,彼此獨立可選擇地被下列者所單-至二取代:氟,氯,溴,甲基,乙基,三氟甲基,甲氧基,乙氧基或氰基,A 代表來自包含下列之基團:氫,C1-C6-烷基,C3-C6-烯基或C3-C6-炔基,彼此獨立可選擇地被下列者所單-至五取代:氟,氯,溴,甲氧基,乙氧基或氰基,及C3-C6-環烷基,彼此獨立可選擇地被下列者所單-至二取代:氟,氯,溴,甲基,乙基,三氟甲基,甲氧基,乙氧基或氰基,T 代表一電子對,L1及L2與N一起代表來自基團U-1,U-2,U-3,U-4,U-5,U-6,U-7,U-25,U-26,U-27,U-28,U-29及U-30之雜環,Xb 代表來自包含下列之基團:鹵素,硝基,氰基,C1-C4-烷基,C3-C6-環烷基,C1-C2-鹵烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基,C3-C6-鹵代
環烷基,C1-C4-烷氧基-C1-C4-烷基,C1-C6-烷基硫代,C1-C4-烷氧基羰基,C1-C4-烷基胺基羰基,C1-C6-烷基磺醯基,C1-C6-烷基羰基胺基及苯基,其中苯基可可選擇地被氟,氯,溴,甲基,乙基,二氟甲基,三氟甲基,甲氧基,乙氧基,Me-S(O)n-,Et-S(O)n-,二氟甲氧基,三氟甲氧基,三氟甲基-S(O)n-,二氟乙基-S(O)n-,三氟乙基-S(O)n-,硝基或氰基所單-至三取代,m 代表0,1或2之數目,n 代表0,1或2之數目,及其鹽類。
於式(I)化合物中之基團之其他較佳的取代基或範圍係闡述如下。其等之組合形成較佳範圍(2-2),其中Q,V,W,Y,A,T,L1,L2,m及n係如在較佳範圍(2-1)中所定義,且Xb 代表來自包含下列之基團:鹵素,硝基,氰基,胺基,C1-C4-烷基,C3-C6-環烷基,C1-C2-鹵烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基,C3-C6-鹵代環烷基,C1-C4-烷氧基-C1-C4-烷基,C1-C6-烷基硫代,C1-C4-烷氧基羰基,C1-C4-烷基胺基羰基,C1-C6-烷基磺醯基,C1-C6-烷基羰基胺基及苯基,其中苯基可可選擇地被氟,氯,溴,甲基,乙基,二氟甲基,三氟甲基,甲氧基,乙氧基,Me-S(O)n-,Et-S(O)n-,二氟甲氧基,三氟甲氧基,三氟甲基-S(O)n,二氟乙基-S(O)n-,三氟乙基-S(O)n-,硝基或氰基所單-至三取代,或Xb 代表一C3-C5-碳鏈,其係連接至兩個相鄰的環位置並形成脂族環,於此情況下m等於2。
於式(I)化合物中之基團之非常特別較佳的取代基或範圍係闡述如下。
考慮到甲醯胺基在咪唑基團上的位置,可得到非常特別較佳結構(I-1)。其等之組合形成較佳範圍(3-1)。
考慮到甲醯胺基在咪唑基團上的位置,式(I)提供非常特別較佳的結構式(I-1)。於式(I-1)化合物中之基團中非常特別較佳的取代基或範圍係闡述如下。其等之組合形成較佳範圍(3-2),其中V,W,Y,A,T,L1,L2,m及n係如較佳範圍(3-1)中所定義,且Xb 代表來自包含下列之基團:氟,氯,溴,氰基,胺基,甲基,乙基,正-及異丙基,環丙基,三氟甲基,二氟甲基,三氟乙基,甲氧基,乙氧基,正-及異丙氧基,三氟甲氧基,甲氧基甲基,乙氧基甲基,甲氧基乙基,乙氧基乙基,甲基-S(O)n-,乙基-S(O)n-,甲氧基羰基,乙氧基羰基,甲基胺基羰基,甲基羰基胺基或苯基,其中苯基可可選擇地被氟,氯,溴,甲基,乙基,二氟甲基,三氟甲基,甲氧基,乙氧基,硝基或氰基所單-至三取代,或Xb 代表C3-C5-碳鏈,其係連接至兩個相鄰的環位置並形成脂族環,於此情況下m等於2。
於式(I-1)化合物之基團中之尤其佳的取代基或範圍係闡述如下。其與尤其佳之取代基組合形成較佳範圍(4-1),其中
V 代表氫,W 代表氫,Y 代表來自包含氫,甲基,乙基,烯丙基及炔丙基之基團,A 代表來自包含氫,甲基及乙基之基團,T 代表一電子對,L1及L2 與N一起代表來自基團U-1,U-2,U-3,U-6,U-25,U-26及U-29之雜環,Xb 代表來自包含氟,氯,溴,氰基,甲基,乙基,正-及異丙基,三氟甲基,甲氧基,乙氧基,甲基硫代及苯基之基團,其中苯基可可選擇地被氟,氯,甲基或甲氧基所單-至三取代,m 代表0,1或2之數目,及其鹽類。
於式(I-1)化合物之基團中之尤其佳的取代基或範圍係闡述如下。其與尤其佳之取代基組合形成較佳範圍(4-2),其中V,W,Y,T,L1,L2及m係如較佳範圍(4-1)中所定義,且A 代表來自包含氫,甲基,乙基及環丙基之基團,且Xb 代表來自包含氟,氯,溴,氰基,胺基,甲基,乙基,正-及異丙基,三氟甲基,甲氧基,乙氧基,甲基硫代及苯基之基團,其中苯基可可選擇地被氟,氯,甲基或甲氧基所單-至三取代,或Xb 代表一C3-C4-碳鏈,其係連接至兩個相鄰的環位置並形成脂族環,於此情況下m等於2。
於式(I-1)化合物之基團中之非常特別較佳的取代基或範圍係闡述如下。其等之組合形成較佳範圍(5-1)。
於式(I-1)化合物中之基團之非常特別較佳的取代基或範圍係闡述如下。其等之組合形成較佳範圍(5-2),其中V,W,Y,T,L1,L2及m係定義如較佳範圍(5-1),且A 代表甲基,乙基或環丙基,且Xb 代表來自包含氯,氰基,胺基,甲基,異丙基,三氟甲基,甲基硫代及苯基之基團,或Xb 代表-(CH2)3-,其係連接至兩個相鄰的環位置並形成脂族環,於此情況
下m等於2。
於較佳具體例中,本發明係關於式(I)或式(I-1)化合物,其中基團Q,V,W,Y,A,T及n係定義如較佳範圍(1-1)或較佳範圍(1-2)或較佳範圍(2-1)或較佳範圍(2-2)或較佳範圍(3-1)或較佳範圍(3-2)或較佳範圍(4-1)或較佳範圍(4-2)或較佳範圍(5-1)或較佳範圍(5-2)且L1,L2,Xb,R2,R3,R4,R3a,R4a,R5,R6及m具有於具體例(0)中說明之意義。
於較佳具體例中,本發明係關於式(I)或式(I-1)化合物,其中基團Q,V,W,Y,A,T及n係定義如具體例(0)或較佳範圍(2-1)或較佳範圍(2-2)或較佳範圍(3-1)或較佳範圍(3-2)或較佳範圍(4-1)或較佳範圍(4-2)或較佳範圍(5-1)或較佳範圍(5-2)且L1,L2,Xb,R2,R3,R4,R3a,R4a,R5,R6及m具有於較佳範圍(1-1)或(1-2)中說明之意義。
於較佳具體例中,本發明係關於式(I)或式(I-1)化合物,其中基團Q,V,W,Y,A,T及n係定義如具體例(0-1)或具體例(0-2)或較佳範圍(1-1)或較佳範圍(1-2)或較佳範圍(3-1)或較佳範圍(3-2)或較佳範圍(4-1)或較佳範圍(4-2)或較佳範圍(5-1)或較佳範圍(5-2),且L1,L2,Xb及m具有於較佳範圍(2-1)或(2-2)中說明之意義。
於較佳具體例中,本發明係關於式(I)或式(I-1)化合物,其中基團Q,V,W,Y,A,T及n係定義如具體例(0-1)或具體例(0-2)或較佳範圍(1-1)或較佳範圍(1-2)或較佳範圍(2-1)或較佳範圍(2-2)或較佳範圍(4-1)或較佳範圍(4-2)或較佳範圍(5-1)或較佳範圍(5-2)且L1,L2,Xb及m具有於較佳範圍(3-1)或(3-2)中說明之意義。
於較佳具體例中,本發明係關於式(I)或式(I-1)化合物,其中基團Q,V,W,Y,A,T及n係定義如具體例(0-1)或具體例(0-2)或較佳範圍(1-1)或較
佳範圍(1-2)或較佳範圍(2-1)或較佳範圍(2-2)或較佳範圍(3-1)或較佳範圍(3-2)或較佳範圍(5-1)或較佳範圍(5-2)且L1,L2,Xb及m具有於較佳範圍(4-1)或較佳範圍(4-2)中說明之意義。
於較佳具體例中,本發明係關於式(I)或式(I-1)化合物,其中基團Q,V,W,Y,A,T及n係定義如具體例(0-1)或具體例(0-2)或較佳範圍(1-1)或較佳範圍(1-2)或較佳範圍(2-1)或較佳範圍(2-2)或較佳範圍(3-1)或較佳範圍(3-2)或較佳範圍(4-1)或較佳範圍(4-2)且L1,L2,Xb及m具有於較佳範圍(5-1)或較佳範圍(5-2)中說明之意義。
於較佳範圍(1-1)或(1-2)中,除非另有說明,鹵素係選自氟,氯,溴及碘,依次較佳者係來自氟,氯及溴,雜芳基(包含雜芳基之同義詞,包括作為較大單位的一部分,例如雜芳基烷基)係選自包含下列者:呋喃基,噻吩基,吡咯基,吡唑基,咪唑基,1,2,3-三唑-基,1,2,4-三唑基,唑基,異唑基,噻唑基,異噻唑基,1,2,3-二唑基,1,2,4-二唑基,1,3,4-二唑基,1,2,5-二唑基,1,2,3-噻二唑基,1,2,4-噻二唑基,1,3,4-噻二唑基,1,2,5-噻二唑基,吡啶基,嘧啶基,嗒基,吡基,1,2,3-三基,1,2,4-三基,1,3,5-三基,苯并呋喃基,苯并異呋喃基,苯并噻吩基,苯并異噻吩基,吲哚基,異吲哚基,吲唑基,苯并噻唑基,苯并異噻唑基,苯并唑基,苯并異唑基,苯并咪唑基,2,1,3-苯并二唑基,喹啉基,異喹啉基,噌啉基,酞基,喹唑啉基,喹喏啉基,萘啶基,苯并三基,嘌呤基,蝶啶基及吲哚基,雜環基代表一飽和3-,4-,5-或6-員環,其含有1或2個氮原子及/或1個氧原子及/或1個硫原子,但其中2個氮原子不可直接相鄰,例如氮丙啶基,氮雜環丁烷基,唑烷基,亞氮烷基,環氧乙烷基,氧雜環丁烷基,氧雜環戊烷基,烷基,二烷基,噻瑞基(thiiranyl),噻坦基,硫醇基,噻因基(thianyl)及四氫呋喃基。
於較佳範圍(2-1)或(2-2)中,除非另有說明,鹵素代表氟,氯,溴及碘,宜為氟,氯及溴,雜芳基(包括作為較大單位的一部分,如雜芳基烷基)代表吡啶基,嘧啶基,噻唑基,唑基,吡唑基,噻吩基,呋喃基,苄基,吡啶基甲基及噻唑基甲基,且雜環基(包括作為較大單位的一部分,如雜環基烷基)代表一飽和或不飽和3-,4-或5-員環其含有1或2個氮原子及/或1個氧原子及/或1個硫原子,但其中2個氮原子不可直接相鄰,例如1-或2-氮丙啶基,2-環氧乙烷基,2-噻瑞基,1-或2-氮雜環丁烷基,2-或3-氧雜環丁烷基,2-或3-噻坦基,1,3-二氧雜環丁烷-2-基,1-,2-或3-吡咯啶基。
於較佳範圍(3-1)或(3-2)中,除非另有說明,鹵素代表氟,氯,溴及碘,宜為氟,氯及溴,且雜環基(包括作為較大單位的一部分,如雜環基烷基)代表一飽和或不飽和3-或4-員環其含有1或2個氮原子及/或1個氧原子及/或1個硫原子,但其中2個氮原子不可直接相鄰,例如1-或2-氮丙啶基,2-環氧乙烷基,2-噻瑞基,1-或2-氮雜環丁烷基,2-或3-氧雜環丁烷基,2-或3-噻坦基或1,3-二氧雜環丁烷-2-基。經鹵素取代之基團,例如鹵烷基,除非另有說明,為單鹵素化或多鹵素化至最大可能的取代基數目。於多鹵素化之情況時,該鹵素原子可相同或不同。於此情況時,鹵素為氟,氯,溴或碘,尤其是氟,氯或溴。
飽和或不飽和烴基團,如烷基或烯基,如果可能可分別為直鏈或分支之,包括與雜原子合併,如,例如,於烷氧基。
除非另有說明,可選擇地經取代之基團可經單-或多取代,於多取代之情況時其中該取代基可相同或不同。
於式(I)化合物,倘若T代表氧,這些化合物係以N-氧化物呈現。
於式(I)化合物,倘若T代表一電子對,這些化合物係以吡啶呈現。
該基團以一般性名稱或列於較佳區塊之定義或闡釋相應地適用於最終產物及起始物質及中間體。這些基團定義可根據需要而與另一個合併,亦即包括各個較佳範圍之合併。
根據本發明之較佳者係使用式(I)化合物,其含有上述屬較佳意義(較佳範圍(1-1)或(1-2))之組合。
根據本發明之特別較佳者為使用式(I)化合物,其含有上述屬特佳意義(較佳範圍(2-1)或(2-2))之組合。
根據本發明之非常特別較佳者為使用式(I)化合物,其含有非常特別較佳意義(較佳範圍(3-1)或(3-2))之組合。
根據本發明之尤其佳者為使用式(I)化合物,其含有上述屬非常特別較佳意義(較佳範圍(4-1)或(4-2))之組合。
根據本發明更為較佳者為是用式(I)化合物,其含有上述屬非常特別較佳意義(較佳範圍(5-1)或(5-2))之組合。
下文中,有關式(I)化合物之陳述,當然,亦適用於式(I)所包括之式(I-1)化合物。
根據取代基之性質,式(I)化合物於不同組成物中可以是幾何及/或光學活性異構體或相關之異構混合物型式。這些立體異構物為,例如,對映體,非對映立體異構物,阻轉異構物或幾何異構物。本發明因此包括純立體異構物及這些異構物之任何想要的混合物。
本發明亦關於控制動物蟲害之方法,其中式(I)化合物被允許作用於動
物蟲害及/或其等之棲息地。動物蟲害之控制宜於農業和林業方面進行,及於物質保護上。宜於此排除的為人類或動物體之手術或治療性處置的方法及於人類或動物體之診斷方法。
本發明進一步係關於式(I)化合物作為殺蟲劑,特別是作物保護劑之用途。
於本發明之內文中,「殺蟲劑」之詞於各情況中亦總是包含「作物保護劑」之詞。
式(I)化合物,有良好植物耐受性,有利的溫血動物毒性及良好的環境相容性,係適用於保護植物及植物器官以對抗生物及非生物壓力因素,以提高產量,改良收穫物質之品質並控制動物蟲害,尤其是昆蟲,蜘蛛,蠕蟲,尤其是線蟲及軟體動物,其係於農業,於園藝,於動物養殖,於水產培養,於林業,於花園及休閒設施,於儲存產品及物質之保護,及於衛生界遇到。
於本專利申請案內文中,應瞭解「衛生」之詞意指任何及所有以預防疾病為目的之措施,規定及程式,尤其是感染性疾病,且其用於保護人類及動物之健康及/或保護環境及/或保持清潔。根據本發明,此尤其包括清潔,消毒及滅菌之措施,例如紡織品或硬表面,尤其是由玻璃,木頭,水泥,瓷,陶,塑膠或者金屬製成之表面,以確保這些無衛生蟲害及/或其等之分泌物。在這方面,本發明的保護範圍宜排除即將應用於人體或動物體之外科或治療性處理程式,及對人體或動物體進行的診斷程式。
「衛生領域」之詞涵蓋所有區域,技術領域及工業應用,其中這些衛生措施,規定及過程是重要的,例如關於廚房,麵包店,機場,浴室,游泳池,百貨公司,旅社,醫院,攤位,動物飼養等之衛生。
因此應瞭解的是「衛生蟲害」之詞意指一種或多種在衛生領域上存在的動物蟲害問題,尤其是為健康的原因。因此,主要目的是避免,或限制
衛生蟲害的存在及/或在衛生領域接觸這些害蟲到最小程度。其尤其是可經由使用可用來預防感染及抵制現有侵害之殺蟲劑來達成。其亦可使用可防止或減少暴露至蟲害的製劑。衛生蟲害包括,例如,下述生物體。
因此,「衛生保護」之詞涵蓋所有的動作,由此而保持及/或改良這些衛生措施,規定和過程。
式(I)化合物宜被用作為殺蟲劑。其等有效於對抗一般敏感性及抗性品種及對抗發育中之所有或特別階段。上述害蟲包括:節肢動物門(Arthropoda)害蟲,尤其是蜘蛛綱(Arachnida),例如粉蟎(Acarus spp.),如粗腳粉蟎(Acarus siro)、枸杞瘤節蜱(Aceria kuko)、柑橘瘤癭蟎(Aceria sheldoni)、刺皮癭蟎(Aculops spp.)、刺節蜱(Aculus spp.)、福氏刺節蜱(Aculus fockeui)、蘋果銹蜱(Aculus schlechtendali)、長吻蜱(Amblyomma spp.)、山楂葉蟎(Amphitetranychus viennensis)、隱喙蜱(Argas spp.)、頭蜱(Boophilus spp.)、知須蟎(Brevipalpus spp.),如紫紅短須蟎(Brevipalpus phoenicis)、嘉蜱蟎(Bryobia graminum)、苜蓿苔蟎(Bryobia praetiosa)、中美毒蠍(Centruroides spp.)、恙蟎(Chorioptes spp.)、雞皮刺蟎(Dermanyssus gallinae)、屋塵蟎(Dermatophagoides pteronyssinus)、粉塵蟎(Dermatophagoides farina)、革蜱(Dermacenter spp.)、始葉蟎(Eotetranychus spp.),如神澤葉蟎(Eotetranychus hicoriae)、梨葉銹癭蟎(Epitrimerus pyri)、真葉蟎(Eutetranychus spp.),如柑橘褐蜘蛛(Eutetranychus banksi)、銹蜱(Eriophyes spp.),如梨癭蟎(Eriophyes pyri)、傢具蟎蟲(Glycyphagus domesticus)、土蟎(Halotydeus destructor)、半線蟎(Hemitarsonemus spp.),如茶塵蟎(Hemitarsonemus latus)(=多食細蟎(Polyphagotarsonemus latus))、璃眼蜱(Hyalomma spp.)、硬蜱(Ixodes spp.)、寡婦蜘蛛(Latrodectus spp.)、花蛛(Loxosceles spp.)、秋蟲(Neutrombicula autumnalis)、努沙蟲(Nuphersa spp.)、葉蟎(Oligonychus spp.),如咖啡小爪蟎(Oligonychus coffeae)、崗夫拉小爪蟎(Oligonychus coniferarum)、草地小爪蟎
(Oligonychus ilicis)、印度小爪蟎(Oligonychus indicus)、芒果赤葉蟎(Oligonychus mangiferus)、原野小爪蟎(Oligonychus pratensis)、鱷裂褐小爪蟎(Oligonychus punicae)、鱷梨紅小爪蟎(Oligonychus yothersi)、耳殘喙蜱(Ornithodorus spp.)、禽刺蟎(Ornithonyssus spp.)、爪蟎(Panonychus spp.),如柑桔葉蟎(Panonychus citri)(=柑橘瘤葉蟎(Metatetranychus citri))、歐洲葉蟎(Panonychusulmi)(=歐洲葉蟎(Metatetranychus ulmi))、橘銹蟎(Phyllocoptruta oleivora)、多迪吉蟎(Platytetranychus multidigituli)、茶細蟎(Polyphagotarsonemus latus)、癢蟎(Psoroptes spp.)、扇頭蜱(Rhipicephalus spp.)、根蟎(Rhizoglyphus spp.)、蚧蟎(Sarcoptes spp.)、中東金蠍(Scorpio maurus)、細蟎(Steneotarsonemus spp.)、稻細蟎(Steneotarsonemus spinki)、線蟎(Tarsonemus spp.),如亂跗線蟎(Tarsonemus confusus)、仙克萊細蟎(Tarsonemus pallidus)、葉蟎(Tetranychus spp.),如加拿大葉蟎(Tetranychus canadensis)、二斑葉蟎(Tetranychus cinnabarinus)、土耳其斯坦葉蟎(Tetranychus turkestani)、二斑葉蟎(Tetranychus urticae)、阿氏真恙蟎(Trombicula alfreddugesi)、蠍子(Vaejovis spp.)、輻蟎(Vasates lycopersici);唇足綱(Chilopoda),如地蜈蚣(Geophilus spp.)、蚰蜒(Scutigera spp.);彈尾綱或目(Collembola),例如刺棘跳蟲(Onychiurus armatus);綠圓跳蟲(Sminthurus viridis);倍足綱(Diplopoda),例如斑點蟲(Blaniulus guttulatus);昆蟲綱(Insecta),例如蜚蠊目(Blattodea),如東方蠊(Blatta orientalis)、德國姬蠊(Blattella asahinai)、德國小蠊(Blattella germanica)、馬德拉蜚蠊
(Leucophaea maderae)、歐洲缺翅姬蜚蠊(Loboptera decipiens)、家屋斑蠊(Neostylopyga rhombifolia)、蜚蠊(Panchlora spp.)、木蠊(Parcoblatta spp.)、大蠊(Periplaneta spp.),如美洲大蠊(Periplaneta Americana)、澳洲家蠊(Periplaneta australasiae)、蔗蠊(Pycnoscelus surinamensis)、棕帶蜚蠊(Supella longipalpa);鞘翅目(Coleoptera),例如瓜條葉甲(Acalymma vittatum)、菜豆象(Acanthoscelides obtectus)、褐金龜(Adoretus spp.)、小蜂窩甲蟲(Aethina tumida)、葉子甲蟲(Agelastica alni)、叩頭蟲(Agriotes spp.),如具條扣甲(Agriotes linneatus)、小麥金針蟲(Agriotes mancus)、外米擬步行蟲(Alphitobius diaperinus)、馬鈴薯鰓金龜(Amphimallon solstitialis)、傢俱蠹蟲(Anobium punctatum)、星天牛(Anoplophora spp.)、棉鈴象(Anthonomus spp.),如苜蓿葉象甲(Anthonomus grandis)、鰹節蟲(Anthrenus spp.)、象甲(Apion spp.)、甘蔗金龜(Apogonia spp.)、微點蟲(Atomaria spp.),如連瑞金龜(Atomaria linearis)、黑皮蠹(Attagenus spp.)、白樹蠹(Baris caerulescens)、菜豆象(Bruchidius obtectus)、豆象(Bruchus spp.),如豌豆象鼻蟲(Bruchus pisorum)、蠶豆蟲(Bruchus rufimanus)、龜金花蟲(Cassida spp.)、菜豆葉甲(Cerotoma trifurcata)、象鼻蟲(Ceutorrhynchus spp.),如甘藍莢象甲(Ceutorrhynchus assimilis)、甘藍莖象甲(Ceutorrhynchusquadridens)、蕪菁象甲(Ceutorrhynchusrapae)、跳甲(Chaetocnema spp.),如甘薯跳甲(Chaetocnema confinis)、具齒跳甲(Chaetocnema denticulata)、荒地玉米跳甲(Chaetocnema ectypa)、曼迪象鼻蟲(Cleonus mendicus)、金針蟲(Conoderus spp.)、象甲(Cosmopolites spp.),如香蕉蛀基象甲(Cosmopolites sordidus)、紐西蘭草金龜(Costelytra zealandica)、金針蟲(Ctenicera spp.)、象甲(Curculio spp.),如美核桃象甲(Curculio caryae)、大栗象甲(Curculio caryatrypes)、鈍形小象甲
(Curculio obtusus)、栗小象甲(Curculio sayi)、銹扁穀盜(Cryptolestes ferrugineus)、長角扁穀盜(Cryptolestes pusillus)、柳小隱喙象甲(Cryptorhynchus lapathi)、芒果隱喙象甲(Cryptorhynchus mangiferae)、象甲(Cylindrocopturus spp.)、非洲象甲(Cylindrocopturus adspersus)、黃衫枝象甲(Cylindrocopturus furnissi)、黑皮蠹(Dermestes spp.)、葉甲(Diabrotica spp.),如黃瓜條葉甲(Diabrotica balteata)、北方玉米根蟲(Diabrotica barberi)、十一星瓜葉甲(Diabrotica undecimpunctata howardi)、十一星瓜葉甲(Diabrotica undecimpunctata undecimpunctata)、玉米根蟲(Diabrotica virgifera virgifera)、玉米根葉甲(Diabrotica virgifera zeae)、野螟(Dichocrocis spp.)、稻鐵甲蟲(Dicladispa armigera)、阿根廷兜蟲(Diloboderus spp.)、象甲(Epicaerus spp.)、瓢蟲(Epilachna spp.),如南瓜瓢蟲(Epilachna borealis)、墨西哥豆瓢蟲(Epilachna varivestis)、跳甲(Epitrix spp.),如美洲馬鈴薯跳甲(Epitrix cucumeris)、茄跳甲(Epitrix fuscula)、菸草跳甲(Epitrix hirtipennis)、西部馬鈴薯跳甲(Epitrix subcrinita)、塊莖跳甲(Epitrix tuberis)、象甲(Faustinus spp.)、麥珠甲(Gibbium psylloides)、闊角粉甲(Gnathocerus counutus)、菜螟(Hellula undalis)、非洲黑甲蟲(Heteronychus arator)、金龜(Heteronyx spp.)、優佳金龜(Hylamorpha elegans)、家天牛(Hylotrupes bajulus)、苜蓿葉象甲(Hypera postica)、綠鱗象甲(Hypomeces squamosus)、小蠹(Hypothenemus spp.),如咖啡果小蠹(Hypothenemus hampei)、蘋枝小蠹(Hypothenemus obscurus)、波斯小蠹蟲(Hypothenemus pubescens)、康金黑金龜(Lachnosterna consanguinea)、菸草竊蠹(Lasioderma serricorne)、長頭穀盜(Latheticus oryzae)、薪甲(Lathridius spp.)、負泥蟲(Lema spp.)、馬鈴薯甲蟲(Leptinotarsa decemlineata)、潛葉蛾(Leucoptera spp.),如咖啡潛葉蛾(Leucoptera coffeella)、稻象甲(Lissorhoptrus oryzophilus)、莖象甲(Listronotus)(=象甲(Hyperodes spp.))、象甲(Lixus spp.)、守瓜(Luperodes spp.)、葉蟲
(Luperomorpha xanthodera)、粉蠹(Lyctus spp.)、美洲葉甲(Megascelis spp.)、叩甲(Melanotus spp.),如長堅叩甲(Melanotus longulus oregonensis)、花粉甲蟲(Meligethes aeneus)、鰓金龜(Melolontha spp.),如大栗鰓角金龜(Melolontha melolontha)、密朵拉蟲(Migdolus spp.)、天牛(Monochamus spp.)、象甲(Naupactus xanthographus)、郭公蟲(Necrobia spp.)、鞘翅(Neogalerucella spp.)、金黃珠甲(Niptus hololeucus)、犀角金龜(Oryctes rhinoceros)、鋸胸穀盜(Oryzaephilus surinamensis)、稻穀盜(Oryzaphagus oryzae)、象甲(Otiorhynchus spp.),如油橄欖象甲(Otiorhynchus cribricollis)、苜蓿象甲(Otiorhynchus ligustici)、草莓根象甲(Otiorhynchus ovatus)、皺溝象甲(Otiorhynchus rugosostriarus)、縱槽象甲(Otiorhynchus sulcatus)、負泥蟲(Oulema spp.),如橙足負泥蟲(Oulema melanopus)、稻負泥蟲(Oulema oryzae)、銀點花金龜(Oxycetoniajucunda)、耳蝸葉蟲(Phaedon cochleariae)、鰓金龜(Phyllophaga spp.)、海氏金龜(Phyllophaga helleri)、葉蟲(Phyllotreta spp.),如辣根猿葉蟲(Phyllotreta armoraciae)、柔弱黑跳甲(Phyllotreta pusilla)、西部條跳甲(Phyllotreta ramosa)、黃曲條跳甲(Phyllotreta striolata)、日本麗金龜(Popillia japonica)、小象甲(Premnotrypes spp.)、大穀長蠹(Prostephanus truncatus)、小跳甲(Psylliodes spp.),如馬鈴薯跳甲(Psylliodes affinis),油菜蘭跳甲(Psylliodes chrysocephala)、大麻跳甲(Psylliodes punctulata)、珠甲(Ptinus spp.)、黑根瓢蟲(Rhizobius ventralis)、多明尼加豆象(Rhizopertha dominica)、象蟲組(Rhynchophorus spp.)、紅棕象甲(Rhynchophorus ferrugineus)、棕梠象甲(Rhynchophorus palmarum)、雙棘穿孔(Sinoxylon perforans)、穀象(Sitophilus spp.),如穀象(Sitophilus granarius)、羅望子穀象(Sitophilus linearis)、米象(Sitophilus oryzae)、玉米象(Sitophilus zeamais)、穀象(Sphenophorus spp.)、藥材穀盜(Stegobium paniceum)、穀象(Sternechus spp.),如豆莖象(Sternechus paludatus)、大蚊(Symphyletes spp.)、
葉象(Tanymecus spp.),如玉米葉象(Tanymecus dilaticollis)、印度長泥蟲(Tanymecus indicus)、琶塔葉象(Tanymecus palliatus)、黃粉甲(Tenebrio molitor)、幕坦穀盜(Tenebrioides mauretanicus)、粉甲(Tribolium spp.),如黑粉甲(Tribolium audax)、赤擬穀盜(Tribolium castaneum)、雜擬穀盜(Tribolium confusum)、皮蠹(Trogoderma spp.)、象甲(Tychius spp.)、天牛(Xylotrechus spp.)、步甲(Zabrus spp.),如麥步甲(Zabrus tenebrioides);皮蠹目(Dermaptera),例如濱海肥蠼螋(Anisolabis maritime)、歐洲球螋(Forficula auricularia)、紅蠼螋(Labidura riparia);雙翅目(Diptera),例如伊蚊(Aedes spp.),如埃及斑蚊(Aedes aegypti)、白紋伊蚊(Aedes albopictus)、泛水伊蚊(Aedes sticticus)、刺擾伊蚊(Aedes vexans)、潛蠅(Agromyza spp.),如苜蓿斑潛蠅(Agromyza frontella)、玉米斑潛蠅(Agromyza parvicornis)、實蠅(Anastrepha spp.)、瘧蚊(Anopheles spp.),如四斑瘧蚊(Anopheles quadrimaculatus)、甘比亞瘧蚊(Anopheles gambiae)、癭蚊(Asphondylia spp.)、實蠅(Bactrocera spp.),如爪實蠅(Bactrocera cucurbitae)、東方果實蠅(Bactrocera dorsalis)、橄欖果蠅(Bactrocera oleae)、和通蠅(Bibio hortulanus)、紅頭麗蠅(Calliphora erythrocephala)、紅頭麗蠅(Calliphora vicina)、地中海實蠅(Ceratitis capitata)、搖蚊(Chironomus spp.)、金蠅(Chrysomya spp.)、草螟(Chrysops spp.)、雨麻虻(Chrysozona pluvialis)、錐蠅(Cochliomya spp.)、癭蚊(Contarinia spp.),如葡萄花癭蚊(Contarinia johnsoni)、甘藍癭蚊(Contarinia nasturtii)、梨癭蚊(Contarinia pyrivora)、舒氏癭蚊(Contarinia schulzi)、高粱癭蚊(Contarinia sorghicola)、麥黃吸漿蟲(Contarinia tritici)、人皮蠅(Cordylobia anthropophaga)、希維環足搖蚊(Cricotopus sylvestris)、庫蚊(Culex spp.),如尖音庫蚊(Culex pipiens)、致乏
庫蚊(Culex quinquefasciatus)、蚊(Culicoides spp.)、蚊(Culiseta spp.)、疽蠅(Cuterebra spp.)、油橄欖實蠅(Dacus oleae)、癭蚊(Dasineura spp.),如雲苔莢癭蚊(Dasineura brassicae)、蠅(Delia spp.),如蔥蠅(Delia antiqua)、麥地種蠅(Delia coarctata)、黃蠅(Delia florilega)、歐洲花蠅(Delia platura)、菜蛆(Delia radicum)、人疽蠅(Dermatobia hominis)、果蠅(Drosophila spp.),如黃猩猩果蠅(Drosphila melanogaster)、鈴木氏果蠅(Drosophila suzukii)、鱗象蟲(Echinocnemus spp.)、實蠅(Euleia heraclei)、廄蠅(Fannia spp.)、胃蠅(Gasterophilus spp.)、采采蠅(Glossina spp.)、麻虻(Haematopota spp.)、水蠅(Hydrellia spp.)、水稻潛葉蠅(Hydrellia griseola)、種蠅(Hylemya spp.)、虱蠅(Hippobosca spp.)、皮蠅(Hypoderma spp.)、潛蠅(Liriomyza spp.),如螺痕潛蠅(Liriomyza brassicae)、南美斑潛蠅(Liriomyza huidobrensis)、蔬菜斑潛蠅(Liriomyza sativae)、綠蠅(Lucilia spp.),如銅綠蠅(Lucilia cuprina)、沙蠅(Lutzomyia spp.)、沼蚊(Mansonia spp.)、家蠅(Musca spp.),如家蠅(Musca domestica)、東方家蠅(Musca domestica vicina)、鼻蠅(Oestrus spp.)、瑞典蠅(Oscinella frit)、跗搖蚊(Paratanytarsus spp.)、小菱帕拉波尼蟲(Paralauterborniella subcincta)、潛葉蠅(Pegomya oder Pegomyia spp.),如甜菜潛葉蠅(Pegomya betae)、波菜潛葉蠅(Pegomya hyoscyami)、懸鉤子花蠅(Pegomya rubivora)、白蛉(Phlebotomus spp.)、草種蠅(Phorbia spp.)、玻璃蠅(Phormia spp.)、酪蠅(Piophila casei)、蘋黑紋蟲(Platyparea poeciloptera)、癭蚊(Prodiplosis spp.)、胡蘿蔔蠅(Psila rosae)、實蠅(Rhagoletis spp.),如櫻桃白帶實蠅(Rhagoletis cingulata)、胡桃實蠅(Rhagoletis completa)、櫻桃黑實蠅(Rhagoletis fausta)、櫻桃細實蠅(Rhagoletis indifferens)、越橘實蠅(Rhagoletis mendax)、蘋果實蠅(Rhagoletis pomonella)、肉蠅(Sarcophaga spp.)、蚋(Simulium spp.),如南方蚋(Simulium meridionale)、螫蠅(Stomoxys spp.)、牛虻(Tabanus spp.)、斑蠅(Tetanops spp.)、大蚊(Tipula spp.),如歐洲大蚊(Tipula
paludosa)、牧場大蚊(Tipula simplex)、番木瓜實蠅(Toxotrypana curvicauda);半翅目(Hemiptera),例如木虱蟲(Acizzia acaciaebaileyanae)、都都木虱(Acizzia dodonaeae)、家庭盲蝽(Acizzia uncatoides)、尖頭蚱蜢(Acrida turrita)、無網長管蚜(Acyrthosipon spp.),如豌豆蚜(Acyrthosiphon pisum)、阿刮尼蟲(Acrogonia spp.)、臭蟲(Aeneolamia spp.)、隆脈木虱(Agonoscena spp.)、刺粉虱(Aleurocanthus spp.)、歐洲甘藍粉虱(Aleyrodes proletella)、甘蔗穴粉虱(Aleurolobus barodensis)、棉絮粉虱(Aleurothrixus floccosus)、榴蓮木虱(Allocaridara malayensis)、葉蟬(Amrasca spp.),如二點小綠葉蟬(Amrasca bigutulla)、馬鈴薯微葉蟬(Amrasca devastans)、薊圓尾蚜(Anuraphis cardui)、圓蚧(Aonidiella spp.),如紅圓蚧(Aonidiella aurantii)、黃圓蚧(Aonidiella citrina)、木瓜腎圓蚧(Aonidiella inornata)、梨瘤蚜(Aphanostigma piri)、蚜(Aphis spp.),如梨綠蚜(Aphis citricola)、豆蚜(Aphis craccivora)、蠶豆蚜(Aphis fabae)、草莓根蚜(Aphis forbesi)、大豆蚜(Aphis glycines)、棉蚜(Aphis gossypii)、長春藤蚜(Aphis hederae)、葡萄蔓蚜(Aphis illinoisensis)、蜜敦蚜(Aphis middletoni)、鼠李馬鈴薯蚜(Aphis nasturtii)、木棉蚜(Aphis nerii)、蘋果蚜(Aphis pomi)、銹線菊蚜(Aphis spiraecola)、莢蒾蚜(Aphis viburniphila)、葡萄浮塵子(Arboridia apicalis)、木虱(Arytainilla spp.)、小圓盾蚧(Aspidiella spp.)、圓蚧(Aspidiotus spp.),如夾竹桃圓蚧(Aspidiotus nerii)、按天蟲(Atanus spp.)、馬鈴薯長鬚蚜(Aulacorthum solani)、煙草粉虱(Bemisia tabaci)、歐美木虱(Blastopsylla occidentalis)、美樂家虱(Boreioglycaspis melaleucae)、光管舌尾蚜(Brachycaudus helichrysi)、山西蚜科(Brachycolus spp.)、菜蚜(Brevicoryne brassicae)、木虱(Cacopsylla spp.),如黔梨木虱(Cacopsylla pyricola)、邊翠飛虱(Calligypona marginata)、毒蜘蛛(Capulinia spp.)、紅尖頭葉蟬(Carneocephala fulgida)、甘蔗棉蚜(Ceratovacuna lanigera)、沫蟬(Cercopidae)、介殼蟲(Ceroplastes spp.)、草莓毛管蚜(Chaetosiphon
fragaefolii)、黃雪盾蚧(Chionaspis tegalensis)、浮塵子(Chlorita onukii)、棉蝗(Chondracris rosea)、蚜蟲(Chromaphisjuglandicola)、茶褐圓蚧(Chrysomphalus aonidum)、柑橘褐圓介殼蟲(Chrysomphalus ficus)、介殼蟲(Cicadulina mbila)、介殼蟲(Coccomytilus halli)、介殼蟲(Coccus spp.),如扁堅介殼蟲(Coccus hesperidum)、長堅介殼蟲(Coccus longulus)、橘灰蚧(Coccus pseudomagnoliarum)、黃綠介殼蟲(Coccus viridis)、葡萄蚜蟲(Cryptomyzus ribis)、蚜蟲(Cryptoneossa spp.)、夜蛾(Ctenarytaina spp.)、夜蛾(Dalbulus spp.)、杜鵑硬殼粉虱(Dialeurodes chittendeni)、柑桔裸粉虱(Dialeurodes citri)、柑橘木虱(Diaphorina citri)、介殼蟲(Diaspis spp.)、麥雙尾(Diuraphis spp.)、實蠅(Doralis spp.)、履綿蚧(Drosicha spp.)、蚜蟲(Dysaphis spp.),如阿皮扶蚜(Dysaphis apiifolia)、車前草蚜(Dysaphis plantaginea),百合西圓尾蚜(Dysaphis tulipae)、嫡粉介殼蟲(Dysmicoccus spp.)、小綠葉蟬(Empoasca spp.),如西部馬鈴薯微葉蟬(Empoasca abrupt)、馬鈴薯姬葉蟬(Empoasca fabae)、蘋果小綠葉蟬(Empoasca maligna)、棉浮塵子(Empoasca solana)、史迪浮塵子(Empoasca stevensi)、綿蚜(Eriosoma spp.),如美國綿蚜(Eriosoma americanum)、蘋果綿蚜(Eriosoma lanigerum)、梨綿蚜(Eriosoma pyricola)、斑葉蟬(Erythroneura spp.)、象甲(Eucalyptolyma spp.)、圓形木蝨(Euphyllura spp.)、葉蜂(Euscelis bilobatus)、介殼蟲(Ferrisia spp.)、盾蚧(Fiorinia spp.)、海洋盾介殼蟲(Furcaspis oceanic)、咖啡粉介殼蟲(Geococcus coffeae)、木虱(Glycaspis spp.)、銀合歡木虱(Heteropsylla cubana)、頰木虱(Heteropsylla spinulosa)、草翅葉蟬(Homalodisca coagulata)、桃粉蚜(Hyalopterus arundinis)、桃粉蚜(Hyalopterus pruni)、介殼蟲(Icerya spp.),如吹綿介殼蟲(Icerya purchasi)、寬突葉蟬(Idiocerus spp.)、綠葉蟬(Idioscopus spp.)、水稻斑飛虱(Laodelphax striatellus)、介殼蟲(Lecanium spp.),如槐介殻蟲(Lecanium corni)(=扁平球堅介殼蟲(Parthenolecanium corni))、介殼蟲
(Lepidosaphes spp.),如榆蠣盾介殼蟲(Lepidosaphes ulmi)、蔬菜偽菜蚜(Lipaphis erysimi)、日本長片盾介殼蟲(Lopholeucaspis japonica)、緣蛾蠟蟬(Lycorma delicatula)、網管蚜(Macrosiphum spp.),如馬鈴薯網管蚜(Macrosiphum euphorbiae)、百合紫斑長管蚜(Macrosiphum lilii)、薔薇長管蚜(Macrosiphum rosae)、番扶長針葉蟬(Macrosteles facifrons)、沫蟬(Mahanarva spp.)、黍蚜(Melanaphis sacchari)、角蟬(Metcalfiella spp.)、普若沙蛾蠟蟬(Metcalfa pruinosa)、麥無網長管蚜(Metopolophium dirhodum)、黑緣平翅斑蚜(Monellia costalis)、平卡蚜蟲(Monelliopsis pecanis)、蚜蟲(Myzus spp.),如瘤額蚜(Myzus ascalonicus)、黑櫻桃蚜(Myzus cerasi)、女貞瘤額(Myzus ligustri)、堇菜瘤蚜(Myzus ornatus)、桃蚜(Myzus persicae)、煙草蚜蟲(Myzus nicotianae)、萵苣蚜(Nasonovia ribisnigri)、粉蝨(Neomaskellia spp.)、黑尾葉蟬(Nephotettix spp.),如黑尾葉蟬(Nephotettix cincticeps)、黑條黑尾葉蟬(Nephotettix nigropictus)、光譜網薊(Nettigoniclla spectra)、褐飛虱(Nilaparvata lugens)、翁密蟲(Oncometopia spp.)、拍長介殼蟲(Orthezia praelonga)、中華稻蝗(Oxya chinensis)、木虱(Pachypsylla spp.)、楊梅粉虱(Parabemisia myricae)、木虱(Paratrioza spp.),如枸杞木虱(Paratrioza cockerelli)、介殼蟲(Parlatoria spp.)、癭綿蚜(Pemphigus spp.),如楊葉癭綿蚜(Pemphigus bursarius)、甜菜多脈癭綿蚜(Pemphigus populivenae)、玉米飛虱(Peregrinus maidis)、飛虱(Perkinsiella spp.)、綿粉蚧(Phenacoccus spp.),如綿粉介殼蟲(Phenacoccus madeirensis)、彩麗蚜(Phloeomyzus passerinii)、指頭蚜(Phorodon humuli)、葡萄根瘤蟲(Phylloxera spp.),如破壞根瘤蚜(Phylloxera devastatrix)、警根瘤蚜(Phylloxera notabilis)、並盾介殼蟲(Pinnaspis aspidistrae)、粉介殼蟲(Planococcus spp.,如柑桔粉介殼蟲(Planococcus citri)、芳香介殼蟲(Prosopidopsylla flava)、厚緣原綿介殼蟲(Protopulvinaria pyriformis)、桑擬白輪盾介殼蟲(Pseudaulacaspis pentagona)、蘭粉介殼蟲
(Pseudococcus spp.),如柑棲粉蚧(Pseudococcus calceolariae)、康氏粉介殼蟲(Pseudococcus comstocki)、長尾粉介殼蟲(Pseudococcus longispinus)、葡萄粉介殼蟲(Pseudococcus maritimus)、白虱(Pseudococcus viburni)、蟲癭(Psyllopsis spp.)、木虱(Psylla spp.),如黃楊木虱(Psylla buxi)、蘋木虱(Psylla mali)、梨木虱(Psylla pyri)、小蜂(Pteromalus spp.)、綿蚧(Pulvinaria spp.)、璐蠟蟬(Pyrilla spp.)、介殼蟲(Quadraspidiotus spp.),如佳藍絲介殼蟲(Quadraspidiotus juglansregiae)、蠣形齒介殼蟲(Quadraspidiotus ostreaeformis)、梨齒介殼蟲(Quadraspidiotus perniciosus)、巨形蟬(Quesada gigas)、介殼蟲(Rastrococcus spp.)、縊管蚜(Rhopalosiphum spp.),如玉米蚜(Rhopalosiphum maidis)、棉蚜(Rhopalosiphum oxyacanthae)、稻麥蚜(Rhopalosiphum padi)、紅腹縊管蚜(Rhopalosiphum rufiabdominale)、盔蚧(Saissetia spp.),如咖啡盔蚧(Saissetia coffeae)、米蘭達盔蚧(Saissetia miranda)、櫻桃花金龜(Saissetia neglecta)、工背硬介殼蟲(Saissetia oleae)、鍬形介殼蟲(Scaphoideus titanus)、麥二叉蚜(Schizaphis graminum)、刺圓盾介殼蟲(Selenaspidus articulatus)、黃偽毛蚜(Sipha flava)、麥長管蚜(Sitobion avenae)、虱(Sogata spp.)、白背飛虱(Sogatella furcifera)、飛虱(Sogatodes spp.)、費納角蟬(Stictocephala festina)、梣粉虱(Siphoninus phillyreae)、馬來西亞虱(Tenalaphara malayensis)、四溝蟲(Tetragonocephela spp.)、核桃黑蚜(Tinocallis caryaefoliae)、廣胸沫蟬(Tomaspis spp.)、二叉蚜(Toxoptera spp.),如橘二岔蚜(Toxoptera aurantii)、橘二叉蚜(Toxoptera citricidus)、溫室白粉虱(Trialeurodes vaporariorum)、木虱(Trioza spp.),如柿木虱(Trioza diospyri)、小蟲蟬(Typhlocyba spp.)、蚧(Unaspis spp.)、葡萄根瘤蚜(Viteus vitifolii)、小綠葉蟬(Zygina spp.);異翅目(Heteroptera),例如蝽象(Aelia spp.)、南瓜緣蝽(Anasa tristis)、小刺蝽(Antestiopsis spp.)、蝽(Boisea spp.)、長蝽(Blissus spp.)、蝽(Calocoris spp.)、
放線盲蝽(Campylomma livida)、長蝽(Cavelerius spp.)、葉蜂(Cimex spp.),如臭蟲(Cimex adjunctus)、熱帶臭蟲(Cimex hemipterus)、溫帶臭蟲(Cimex lectularius)、蝠臭蟲(Cimex pilosellus)、盲蝽(Collaria spp.)、綠淡盲蝽(Creontiades dilutus)、胡椒緣蝽(Dasynus piperis)、福楚蝽(Dichelops furcatus)、厚氏長棒網蝽(Diconocoris hewetti)、紅蝽(Dysdercus spp.)、蝽(Euschistus spp.),如桃蝽(Euschistus heros)、褐臭蝽(Euschistus servus)、三點暗蝽(Euschistus tristigmus)、一點褐蝽(Euschistus variolarius)、菜蝽(Eurydema spp.)、盾蝽(Eurygaster spp.)、褐翅蝽象(Halyomorpha halys)、昔皮堤蟲(Heliopeltis spp.)、奴賀斯蟲(Horcias nobilellus)、緣蝽(Leptocorisa spp.)、稻蛛緣蝽(Leptocorisa varicornis)、薊馬(Leptoglossus occidentalis)、葉腳蝽象(Leptoglossus phyllopus)、盲蝽(Lygocoris spp.),如原麗盲蝽(Lygocoris pabulinus)、盲蝽(Lygus spp.),如依立盲蝽(Lygus elisus)、豆莢盲蝽(Lygus hesperus)、牧草盲蝽(Lygus lineolaris)、鹿黑長蝽(Macropes excavatus)、豆龜蝽(Megacopta cribraria)、盲蝽(Miridae)、金光綠盲蝽(Monalonion atratum)、綠蝽(Nezara spp.),如稻綠蝽(Nezara viridula)、長蝽(Nysius spp.)、盾蝽(Oebalus spp.)、蝽目(Pentomidae)、甜菜擬網蝽(Piesma quadrata)、壁蝽(Piezodorus spp.),如小綠蝽(Piezodorus guildinii)、跳蚤(Psallus spp.)、波斯小爪蟎(Pseudacysta persea)、錐蝽(Rhodnius spp.)、可哥褐盲蝽(Sahlbergella singularis)、栗蝽(Scaptocoris castanea)、稻蝽(Scotinophora spp.)、梨花網蝽(Stephanitis nashi)、蝽(Tibraca spp.)、吸血獵蝽(Triatoma spp.);膜翅目(Hymenoptera),例如切葉蟻(Acromyrmex spp.)、菜葉蜂(Athalia spp.),如菜葉蜂(Athalia rosae)、天蠶蛾(Atta spp.)、大黑蟻(Camponotus spp.)、長黃胡蜂(Dolichovespula spp.)、松葉蜂(Diprion spp.),如鋸角松葉蜂(Diprion similis)、黏葉蜂(Hoplocampa spp.),如櫻實葉蜂(Hoplocampa cookei)、蘋實
葉蜂(Hoplocampa testudinea)、黑蟻(Lasius spp.)、阿根廷蟻(Linepithema (Iridiomyrmex)humile)、廚蟻(Monomorium pharaonis)、褐蟻(Paratrechina spp.)、帕拉黃胡蜂(Paravespula spp.)、蟻(Plagiolepis spp.)、小樹蜂(Sirex spp.)、外引紅火蟻(Solenopsis invicta)、真蟻(Tapinoma spp.)、白足扁琉璃蟻(Technomyrmex albipes)、大樹蜂(Urocerus spp.)、大胡蜂(Vespa spp.),如大胡蜂(Vespa crabro)、小火蟻(Wasmannia auropunctata)、胡蜂(Xeris spp.);等足目(Isopoda),例如球鼠婦(Armadillidium vulgare)、潮蟲(Oniscus asellus)、鼠婦(Porcellio scaber);等翅目(Isoptera),例如白蟻(Coptotermes spp.),如台灣家白蟻(Coptotermes formosanus)、克靡蘭白蟻(Cornitermes cumulans)、乾木白蟻(Cryptotermes spp.)、楹白蟻(Incisitermes spp.)、木白蟻(Kalotermes spp.)、肥胖小白蟻(Microtermes obesi)、象白蟻(Nasutitermes spp.)、白蟻(Odontotermes spp.)、白蚊(Porotermes spp.)、白蟻(Reticulitermes spp.),如黃胸散白蟻(Reticulitermes flavipes)、西方犀白蟻(Reticulitermes hesperus);鱗翅目(Lepidoptera),例如小蠟蛾(Achroia grisella)、桑劍紋夜蛾(Acronicta major)、小捲葉蛾(Adoxophyes spp.),如茶小捲葉蛾(Adoxophyes orana)、白斑煩夜蛾(Aedia leucomelas)、切根蟲(Agrotis spp.),如蕪菁夜蛾(Agrotis segetum)、蔬菜切根蟲(Agrotis ipsilon)、葉蟲(Alabama spp.),如棉樹葉蟲(Alabama argillacea)、柑橘卷葉蛾(Amyelois transitella)、桃芽蛾(Anarsia spp.)、裳夜蛾(Anticarsia spp.),如大豆夜蛾(Anticarsia gemmatalis)、螟(Argyroploce spp.)、夜蛾(Autographa spp.)、甘藍夜盜蟲(Barathra brassicae)、蘋髓尖蛾(Blastodacna atra)、禾弄蝶(Borbo cinnara)、蘇貝稜巢蛾(Bucculatrix
thurberiella)、松樹尺蠖(Bupalus piniarius)、夜蛾(Busseola spp.)、卷蛾(Cacoecia spp.)、茶細蛾(Caloptilia theivora)、紋網捲葉蛾(Capua reticulana)、蘋果蠹蟲(Carpocapsa pomonella)、桃蛀果蛾(Carposina niponensis)、冬日飛蛾(Cheimatobia brumata)、稻螟(Chilo spp.),如七星稻螟(Chilo plejadellus)、二化螟(Chilo suppressalis)、馬利安納彫翅蛾(Choreutis pariana)、卷葉蛾(Choristoneura spp.)、方解石灰夜蛾(Chrysodeixis chalcites)、果蠹蛾(Clysia ambiguella)、瘤野螟(Cnaphalocerus spp.)、稻縱捲葉野螟(Cnaphalocrocis medinalis)、捲葉蛾(Cnephasia spp.)、細蛾(Conopomorpha spp.)、象鼻蟲(Conotrachelus spp.)、夜蛾(Copitarsia spp.)、蠹蛾(Cydia spp.),如豆莢小卷(Cydia nigricana)、蘋果蠹蛾(Cydia pomonella)、達拉可夜蛾(Dalaca noctuides)、螟(Diaphania spp.)、棉鈴蟲(Diparopsis spp.)、蔗螟(Diatraea saccharalis)、金剛鑽(Earias spp.)、苦橙小捲葉蛾(Ecdytolopha aurantium)、小玉米螟(Elasmopalpus lignosellus)、甘蔗鑽心蟲(Eldana saccharina)、粉螟(Ephestia spp.),如菸草粉螟(Ephestia elutella)、地中海粉斑螟(Ephestia kuehniella)、捲葉蛾(Epinotia spp.)、淡棕色蘋果蛾(Epiphyas postvittana)、尺蠖(Erannis spp.)、灰蝶(Erschoviella musculana)、螟(Etiella spp.)、裳蛾(Eudocima spp.)、螟(Eulia spp.)、女貞細卷蛾(Eupoecilia ambiguella)、毛蟲(Euproctis spp.),如黃毒蛾(Euproctis chrysorrhoea)、切根蟲(Euxoa spp.)、夜蛾(Feltia spp.)、大蠟螟(Galleria mellonella)、細蛾(Gracillaria spp.)、食心蟲(Grapholitha spp.),如梨小食心蟲(Grapholita molesta)、蘋小食心蟲(Grapholita prunivora)、捲葉螟(Hedylepta spp.)、棉鈴蟲(Helicoverpa spp.),如番茄夜蛾(Helicoverpa armigera)、玉米穗蟲(Helicoverpa zea)、夜蛾(Heliothis spp.),如美洲菸夜蛾(Heliothis virescens)、褐織夜蛾(Hofmannophila pseudospretella)、斑螟(Homoeosoma spp.)、捲葉蛾(Homona spp.)、櫻桃巢蛾(Hyponomeuta padella)、柿蒂蟲(Kakivoria flavofasciata)、灰蝶(Lampides spp.)、黏蟲
(Laphygma spp.)、人厭蠹蛾(Laspeyresia molesta)、茄蛀螟(Leucinodes orbonalis)、蜚蠊(Leucoptera spp.),如咖啡一點潛蛾(Leucoptera Coffeella)、細蛾(Lithocolletis spp.),如布卡拉細蛾(Lithocolletis blancardella)、綠果夜蛾(Lithophane antennata)、小捲蛾(Lobesia spp.),如葡萄小捲蛾(Lobesia botrana)、豆白緣切根蟲(Loxagrotis albicosta)、毒蛾(Lymantria spp.),如舞毒蛾(Lymantria dispar)、潛葉蛾(Lyonetia spp.),如窄翹潛葉蛾(Lyonetia clerkella)、天幕毛蟲(Malacosoma neustria)、豇豆莢螟(Maruca testulalis)、甘藍夜蛾(Mamestra brassicae)、稻褐眼蝶(Melanitis leda)、夜蛾(Mocis spp.)、歐唯拉穀蛾(Monopis obviella)、東方黏蟲(Mythimna separata)、軟木長角蛾(Nemapogon cloacellus)、水螟(Nymphula spp.)、蛾(Oiketicus spp.)、野螟(Omphisa spp.)、尺蠖(Operophtera spp.)、螟(Oria spp.)、織葉螟(Orthaga spp.)、螟(Ostrinia spp.),如歐洲玉米螟(Ostrinia nubilalis)、火燄夜蛾(Panolis flammea)、弄蝶(Parnara spp.)、鈴蟲(Pectinophora spp.),如紅鈴蟲(Pectinophora gossypiella)、潛葉蠅(Perileucoptera spp.)、麥蛾(Phthorimaea spp.),如麝香草麥蛾(Phthorimaea operculella)、橘細潛蛾(Phyllocnistis citrella)、潛蠅蛾(Phyllonorycter spp.),如潛葉蟲(Phyllonorycter blancardella)、山楂潛葉蛾(Phyllonorycter crataegella)、粉蝶(Pieris spp.),如菜粉蝶(Pieris rapae)、稻縱捲葉螟(Platynota stultana)、印度穀螟(Plodia interpunctella)、夜蛾(Plusia spp.)、小菜蛾(Plutella xylostella)(=小菜蛾(Plutella maculipennis))、巢蛾(Prays spp.)、黏蟲(Prodenia spp.)、蛾(Protoparce spp.)、黏蟲(Pseudaletia spp.),如一點黏蟲(Pseudaletia unipuncta)、大豆夜蛾(Pseudoplusia includens)、玉米螟(Pyrausta nubilalis)、努悠螟(Rachiplusia nu)、三化螟(Schoenobius spp.),如二化螟(Schoenobius bipunctifer)、白螟(Scirpophaga spp.),如水稻螟蛾(Scirpophaga innotata)、希佳蛾(Scotia segetum)、夜蛾(Sesamia spp.),如大螟(Sesamia inferens)、捲葉蛾(Sparganothis spp.)、夜蛾(Spodoptera spp.),如亞
熱帶黏蟲(Spodoptera eradiana)、甜菜夜蛾(Spodoptera exigua)、草地黏蟲(Spodoptera fiugiperda)、西部黃條黏蟲(Spodoptera praefica)、展足蛾(Stathmopoda spp.)、蛾(Stenoma spp.)、花生鬚峭麥蛾(Stomopteryx subsecivella)、透翅蛾(Synanthedon spp.)、索崴拉蛾(Tecia solanivora)、帶蛾(Thaumetopoea spp.)、金美夜蛾(Thermesia gemmatalis)、卡希拉衣蛾(Tinea cloacella)、網衣蛾(Tinea pellionella)、袋衣蛾(Tineola bisselliella),捲葉蛾(Tortrix spp.)、毛氈衣蛾(Trichophaga tapetzella)、夜蛾(Trichoplusia spp.),如粉紋夜蛾(Trichoplusia ni)、三化螟(Tryporyza incertulas)、番茄斑潛蠅(Tuta absoluta)、蝴蝶(Virachola spp.);直翅目(Orthoptera)或跳躍目(Saltatoria),例如家蟋蟀(Acheta domesticus)、螻蛄(Dichroplus spp.)、螻蛄(Gryllotalpa spp.),如歐洲螻蛄(Gryllotalpa gryllotalpa)、蔗蝗(Hieroglyphus spp.)、飛蝗(Locusta spp.),如東亞飛蝗(Locusta migratoria)、負蝗(Melanoplus spp.),如赤地蚱蜢(Melanoplus devastator)、烏蘇裡擬寰螽(Paratlanticus ussuriensis)、沙漠蝗蟲(Schistocerca gregaria);毛虱目(Phthiraptera),例如虱(Damalinia spp.)、盲虱(Haematopinus spp.)、長顎虱(Linognathus spp.)、虱(Pediculus spp.)、葡萄根瘤蚜(Phylloxera vastatrix)、陰虱(Phthirus pubis)、羽虱(Trichodectes spp.);囓蟲目(Psocoptera),例如書虱(Lepinotus spp.)、書虱(Liposcelis spp.);蚤目(Siphonaptera),例如蚤(Ceratophyllus spp.)、櫛頭蚤(Ctenocephalides spp.),如狗櫛頭蚤(Ctenocephalides canis)、貓櫛頭蚤(Ctenocephalides felis)、人蚤(Pulex irritans)、穿皮潛蚤(Tunga penetrans)、東方鼠蚤(Xenopsylla
cheopis);纓翅目(Thysanoptera),例如栗薊馬(Anaphothrips obscurus)、稻薊馬(Baliothrips biformis)、非洲梯胸薊馬(Chaetanaphothrips leeuweni)、葡萄薊馬(Drepanothrips reuteri)、黃花薊馬(Enneothrips flavens)、薊馬(Frankliniella spp.),如菸草褐薊馬(Frankliniella fusca)、苜蓿薊馬(Frankliniella occidentalis)、梳缺花薊馬(Frankliniella schultzei)、花薊馬(Frankliniella tritici)、樾櫸薊馬(Frankliniella vaccinii)、玉米薊馬(Frankliniella williamsi)、薊馬(Haplothrips spp.)、薊馬(Heliothrips spp.)、溫室條薊馬(Hercinothrips femoralis)、卡薊馬(Kakothrips spp.)、腹鉤薊馬(Rhipiphorothrips cruentatus)、薊馬(Scirtothrips spp.)、豆蔻薊馬(Taeniothrips cardamomi)、薊馬(Thrips spp.),如南黃薊馬(Thrips palmi)、蒜之蔥薊馬(Thrips tabaci);衣魚目(Zygentoma)(=纓尾目(Thysanura)),例如櫛頭衣魚(Ctenolepisma spp.)、西洋衣魚(Lepisma saccharina)、獅子魚衣魚(Lepismodes inquilinus)、斑衣魚(Thermobia domestica);綜合綱(Symphyla),例如蚰蜒(Scutigerella spp.),如蜜曲拉蚰蜒(Scutigerella immaculate);體動物門(Mollusca)蟲害,例如雙殼綱(Bivalvia),如殻菜蚧(Dreissena spp.);以及腹足綱(Gastropoda),例如蛞蝓(Arion spp.),如黑蛞蝓(Arion ater rufus)、雙臍螺(Biomphalaria spp.)、水泡螺(Bulinus spp.)、灰蛞蝓(Deroceras spp.),如田灰蛞蝓(Deroceras laeve)、土蝸(Galba spp.)、淩螺(Lymnaea spp.)、釘螺
(Oncomelania spp.)、福壽螺(Pomacea spp.)、蝸牛(Succinea spp.);植物蟲害線蟲門(Nematoda),亦即植物-寄生線蟲,特別是野外墊刃(Aglenchus spp.),如農家野外墊刃(Aglenchus agricola)、腫癭線蟲(Anguina spp.),如小麥粒癭線蟲(Anguina tritici)、葉芽線蟲(Aphelenchoides spp.),如花生滑刃線蟲(Aphelenchoides arachidis)、葉芽線蟲(Aphelenchoides fragariae)、刺線蟲(Belonolaimus spp.),如萵苣刺線蟲(Belonolaimus gracilis)、草坪刺線蟲(Belonolaimus longicaudatus)、諾頓刺線蟲(Belonolaimus nortoni)、線蟲(Bursaphelenchus spp.),如菊花滑刃線蟲(Bursaphelenchus cocophilus)、獨尾草松材線蟲(Bursaphelenchus eremus)、松樹松材線蟲(Bursaphelenchus xylophilus)、壞死線蟲(Cacopaurus spp.),如波斯壞死線蟲(Cacopaurus pestis)、環紋線蟲(Criconemella spp.),如彎曲小環線蟲(Criconemella curvata)、刻線小環線蟲(Criconemella onoensis)、裝飾小環線蟲(Criconemella ornata)、美洲山核桃環線蟲(Criconemella rusium)、薄葉小環線蟲(Criconemella xenoplax)(=環腐線蟲(Mesocriconema xenoplax))、環紋線蟲(Criconemoides spp.),如弗尼亞小環線蟲(Criconemoides ferniae)、刻線輪線蟲(Criconemoides onoense)、裝飾輪線蟲(Criconemoides omatum)、莖線蟲(Ditylenchus spp.),如莖線蟲(Ditylenchus dipsaci)、錐線蟲(Dolichodorus spp.)、囊線蟲(Globodera spp.),如馬鈴薯白線蟲(Globodera pallida)、黃金線蟲(Globodera rostochiensis)、螺旋線蟲(Helicotylenchus spp.),如雙宮螺旋線蟲(Helicotylenchus dihystera)、鞘線蟲(Hemicriconemoides spp.)、鞘線蟲(Hemicycliophora spp.)、禾穀孢囊線蟲(Heterodera spp.),如禾穀孢囊線蟲(Heterodera avenae)、大豆孢囊線蟲(Heterodera glycines)、甜菜胞囊線蟲(Heterodera schachtii)、水稻穿根線蟲(Hirschmaniella spp.)、紐帶線蟲(Hoplolaimus spp.)、針線蟲(Longidorus spp.),如非洲長針線蟲(Longidorus
africanus)、抗南方根結線蟲(Meloidogyne spp.),如哥倫比亞根結線蟲(Meloidogyne chitwoodi)、偽根結線蟲(Meloidogyne fallax)、北方根結線蟲(Meloidogyne hapla)、苦瓜根瘤線蟲(Meloidogyne incognita)、瓢線蟲(Meloinema spp.)、假根瘤線蟲(Nacobbus spp.)、擬莖線蟲(Neotylenchus spp.)、擬長針線蟲(Paralongidorus spp.)、擬滑刃線蟲(Paraphelenchus spp.)、擬針線蟲(Paratrichodorus spp.),如微小擬毛刺線蟲(Paratrichodorus minor)、根腐線蟲(Paratylenchus spp.)、根腐線蟲(Pratylenchus spp.),如穿刺短體根腐線蟲(Pratylenchus penetrans)、假賀初蟲(Pseudohalenchus spp.)、平滑線蟲(Psilenchus spp.)、斑皮線蟲(Punctodera spp.)、五溝線蟲(Quinisulcius spp.)、穿孔線蟲(Radopholus spp.),如穿孔線蟲(Radopholus citrophilus)、穿孔線蟲(Radopholus similis)、腎形線蟲(Rotylenchulus spp.)、螺旋線蟲(Rotylenchus spp.).、螺旋線蟲(Scutellonema spp.)、根瘤線蟲(Subanguina spp.)、殘根線蟲(Trichodorus spp.),如鈍毛刺線蟲(Trichodorus obtusus)、原始毛刺線蟲(Trichodorus primitivus)、矮化線蟲(Tylenchorhynchus spp.),如飾環矮化線蟲(Tylenchorhynchus annulatus)、鴕形線蟲(Tylenchulus spp.),如半穿刺線蟲(Tylenchulus semipenetrans)、劍線蟲(Xiphinema spp.),如劍線蟲(Xiphinema index)。
式(I)化合物視情況,於特定濃度或施用率,亦可用作為除草劑,安全劑,生長調節劑或植物特性改良劑,作為殺微生物劑或殺配子劑,例如作為殺真菌劑,抗真菌劑,殺菌劑,殺病毒劑(包括抗類病毒劑)或作為對抗MLO(似支原體有機體)及RLO(似立克次體有機體)之試劑。其等,視情況,亦可用作為合成其他活性組成份之中間體或先質。
本發明進一步係關於製劑及由其等製備作為殺蟲劑之用途,例如澆淋,
滴灌及噴霧液,包括至少一種式(I)化合物。可選擇地,該使用型式包括其他可改良作用之殺蟲劑及/或佐劑,如滲透劑,如植物油,例如菜籽油,葵花籽油,礦物油,例如石蠟油,植物脂肪酸之烷基酯類,例如菜籽油甲基酯或黃豆油甲基酯,或烷醇烷氧基類及/或散播劑,例如烷基矽氧烷及/或鹽類,例如有機或無機銨或鏻鹽,例如硫酸銨或磷酸氫二銨及/或保持促進子,例如二辛基磺基琥珀酸酯或羥丙基瓜爾膠聚合物及/或保濕劑,例如甘油及/或肥料,例如含有銨-,鉀-或磷之肥料。
習用製劑為,例如,水溶性液體(SL),乳液濃縮物(EC),於水中之乳液(EW),懸浮濃縮物(SC,SE,FS,OD),水可分散顆粒(WG),顆粒(GR)及膠囊濃縮物(CS);此等及進一步可能之製劑型式係說明於,例如,Crop Life International and in Pesticide Specifications,Manual on development and use of FAO and WHO specifications for pesticides,FAO Plant Production and Protection Papers-173,prepared by the FAO/WHO Joint Meeting on Pesticide Specifications,2004,ISBN:9251048576。該製劑,除了一個或多個式(I)化合物,可任意含有其他農化活性化合物。
較佳之製劑或使用型式包括輔助劑,例如擴充劑,溶劑,自發性促進劑,載體,乳化劑,分散劑,霜凍防護劑,殺生物劑,增稠劑及/或其他輔助劑,例如佐劑。於本文中佐劑為一組份,其可加強該製劑之生物功效而其組份自身並未具有任何生物效果。佐劑之實例為可促進保持、散佈、黏附至葉面或穿透之試劑。
這些製劑係依已知方式製備,例如藉由將式(I)化合物與輔助劑,例如擴充劑,溶劑及/或固態載體及/或其他輔助劑,例如表面活性劑摻合。該製劑係於適當設備製造或於施用之前或於施用期間製作。
所使用之輔助劑可為適用來賦予特殊性能,如特別的物理,技術及/或生物特點,至式(I)化合物之製劑,或至由這些製劑製得之使用型式(例如立
即可用之殺害蟲劑如噴灑液或種子敷料產品)的物質。
適當的擴充劑為,例如水、極性及非極性有機化學液體,例如來自芳族及非芳族烴類者(如石蠟,烷基苯,烷基萘,氯苯),醇類及多元醇(其,如果適當,亦可被取代,醚化及/或酯化),酮類(如丙酮,環己酮),酯類(包括脂肪及油)及(聚)醚類,未經取代及經取代之胺類,醯胺類,內醯胺類(如N-烷基吡咯烷酮)及內酯類,碸類及亞碸類(如二甲亞碸)。
如果所使用之擴充劑為水,其亦可使用,例如有機溶劑作為輔助溶劑。有用之液態溶劑主要為:芳族,如二甲苯,甲苯或烷基萘,氯化芳族或氯化脂族烴類,如氯苯,氯乙烯或二氯甲烷,脂族烴類,如環己烷或石蠟,例如例如礦物油餾份,礦物油及植物油,醇類,如丁醇或乙二醇及其等之醚類及酯類,酮類,如丙酮,甲基乙基酮,甲基異丁基酮或環己酮,強極性溶劑,如二甲基甲醯胺及二甲亞碸,以及水。
理論上,其可使用所有適當的溶劑。適當溶劑之實例芳族烴類,例如二甲苯,甲苯或烷基萘,氯化芳香族或脂族烴類,例如氯苯,氯乙烯或二氯甲烷,脂族烴類,例如環己烷,石蠟,礦物油餾份,礦物油及植物油,醇類,例如甲醇,乙醇,異丙醇,丁醇或乙二醇及其等之醚類及酯類,酮類,例如丙酮,甲基乙基酮,甲基異丁基酮或環己酮,強極性溶劑,例如二甲亞碸,及水。
理論上,其亦可使用所有適當的載體。有用之載體尤其是包括,例如,銨鹽及研碎之天然礦物質,如高嶺土,礬土,滑石,白堊,石英,綠坡縷石,蒙脫土或矽藻土,以及磨細的合成岩石,如高度分散的二氧化矽,氧化鋁和天然或合成的矽酸鹽,樹脂,蠟及/或固態肥料。同樣可使用此等載體之混合物。顆粒中有用之載體包括:例如粉碎及分級的天然岩石如方解石,大理石,浮石,海泡石,白雲石,及無機和有機粗粉之合成顆粒,以及有機物質之顆粒如木屑,紙,椰子殼,玉米穗軸及菸草稈。
亦可使用液化之氣態擴充劑或溶劑。尤其適當的擴充劑或載體為那些於周遭溫度及於大氣壓時為氣態者,例如氣溶膠推進劑,如鹵化烴類,以及丁烷,丙烷,氮及二氧化碳。
具有離子或非離子特性之乳化劑及/或泡沫形成劑,分散劑或潤濕劑,或這些表面活性劑之混合物之實例為:聚丙烯酸之鹽類,木質素磺酸之鹽類,苯酚磺酸或萘磺酸之鹽類,環氧乙烷與脂肪醇或與脂肪酸或與脂肪胺,與經取代之苯酚(宜為烷基苯酚或芳基苯酚)之縮聚物,磺基琥珀酸酯之鹽類,牛磺酸衍生物(宜為烷基牛磺酸酯),聚乙氧基化之醇類或苯酚之磷酸酯類,多元醇之脂肪酸酯類,及包含硫酸鹽,磺酸鹽及磷酸鹽之化合物的衍生物,例如烷基芳基聚乙二醇醚,烷基磺酸酯,烷基硫酸酯,芳基磺酸酯,蛋白水解產物,木質素亞硫酸鹽廢液及甲基纖維素。如果式(I)化合物中之一個及/或惰性載體中之一個不溶於水且當施用係發生在水中時,表面活性劑之存在是有利的。
可存在於製劑及由其衍生之使用型式中的其他輔助劑包括染料,如無機顏料,例如氧化鐵,氧化鈦及普魯士藍,及有機染料,如茜素染料,偶氮染料及金屬酞花青染料,及營養素及微量營養素,如鐵,錳,硼,銅,鈷,鉬和鋅之鹽。
其他可存在的組份可為穩定劑,如冷穩定劑,防腐劑,抗氧化劑,光穩定劑,或其他改良化學及/或物理穩定性之試劑。亦可存在有泡沫形成劑或消泡劑。
此外,製劑及由其衍生之使用型式亦可包括,標貼,如羧基甲基纖維素及天然及合成聚合物,以粉末,顆粒或乳膠型式,如阿拉伯樹膠,聚乙烯醇及聚乙烯基醋酸酯,或其他天然磷脂,如腦磷脂和卵磷脂及合成磷脂,作為額外輔助劑。其他可能的輔助劑為礦物油和植物油。
如果適當,其仍可能有其他輔助劑存在於製劑及由其衍生之使用型式
中。此等添加物之實例包括香料,保護性膠體,粘合劑,黏著劑,增稠劑,觸變劑,滲透劑,保持促進劑,穩定劑,螯合劑,絡合劑,保濕劑,散佈劑。通常,式(I)化合物可與任何習用於製劑目的之固體或液體添加物合併。
有用之保持促進劑包括所有可降低動態表面張力之物質,例如二辛基磺基琥珀酸酯,或提高黏彈性,例如羥基丙基瓜爾膠聚合物。
於本發明內文中,適當的穿透劑為所有通常使用來改良農化活性組成份穿透至植物之能力的那些物質。於本文中,穿透劑係藉由其等由(通常為水溶液)施用液及/或由噴灑塗層穿透至植物表皮且因而提高活性組成份於表皮之流動性的能力來定義。該說明於文獻之方法(Baur et al.,1997,Pesticide Science 51,131-152)可用來確定其特徵。實例包括醇烷氧酸酯如椰子油脂肪酸乙氧酸酯(10)或異十三烷基乙氧酸酯(12),脂肪酸酯類,例如菜籽油甲基酯或黃豆油甲基酯,脂肪胺烷氧酸酯,例如牛脂胺乙氧酸酯(15),或銨及/或鏻鹽,例如硫酸銨或磷酸氫二銨。
該製劑宜為含有介於0.00000001%及98%重量之式(I)化合物,更宜為介於0.01%及95%重量之式(I)化合物,最宜為介於0.5%及90%重量之式(I)化合物,以製劑之重量計。
由製劑製得之使用型式(特別是殺蟲劑)之式(I)化合物的含量可在大範圍內變化。於使用型式之式(I)化合物的濃度典型的可為0.00000001%及95%重量間之式(I)化合物,宜為0.00001%及1%重量間,以使用型式之重量計。施用係依適用於使用型式之習用方式來完成。
式(I)化合物亦可使用於含有一種或多種適當之殺真菌劑,殺菌劑,殺蟎蟲劑,殺軟體動物劑,殺線蟲劑,殺昆蟲劑,微生物製品,有益生物,除草劑,肥料,驅鳥劑,植物滋補品,消毒劑,安全劑,化學資訊素及/或
植物生長調節劑之混合物中,以便因此,例如,擴大作用範圍,延長作用期間,提高作用速率,防止排斥或防止抗性進化。此外,此等型式之活性組成份合併物可改良植物生長及/或對非生物因素,例如高溫或低溫,對乾旱或提高水份含量或土壤鹽分之耐受。其亦可改良開花及結實表現,優化發芽能力及根部生長,便於收穫及提高產量,影響成熟度,提高收穫產品質量及/或營養價值,延長儲存壽命及/或提高收穫產品的加工性。
此外,式(I)化合物可存在於含有其他活性化合物或化學資訊素,如引誘劑及/或驅鳥劑及/或植物啟動劑及/或生長調節劑及/或肥料之混合物中。同樣的,式(I)化合物可用來改良植物特性,例如收穫物質之生長,產量及品質。
於根據本發明之特別具體例中,式(I)化合物係呈製劑之型式或呈由此等製劑製得之使用型式於含有其他化合物之混合物中,宜為那些說明於下者。
如果下述化合物之一可以各種互變異構型式出現,即便於各情況中沒有明確提及,這些型式亦包括在內。所有提及之混合的組份,視情況可以,亦可與適當的鹼或酸形成鹽類,如果其等根據其官能基團而能如此。
於本文中以其等之通用名稱指明之活性組成份係說明於例如「The Pesticide Manual」,16th ed.,British Crop Protection Council 2012,或可由網路中(如http://www.alanwood.net/Pesticides)搜尋。分類係在提交本專利申請時根據適用的IRAC Mode of Action Classification Scheme。
(1)乙醯膽鹼酯酶(AChE)抑制劑,例如胺基甲酸酯,如棉鈴威(alanycarb)、涕滅威(aldicarb)、惡蟲威(bendiocarb)、丙硫克百威(benfuracarb)、丁克威(butocarboxim)、丁氧基克威(butoxycarboxim)、甲萘威(carbaryl)、克百威
(carbofuran)、丁硫克百威(carbosulfan)、乙硫苯威(ethiofencarb)、仲丁威(fenobucarb)、甲坦內(formetanate)、呋線威(furathiocarb)、異丙威(isoprocarb)、滅蟲威(methiocarb)、滅多威(methomyl)、速滅威(metolcarb)、殺線威(oxamyl)、抗蚜威(pirimicarb)、殘殺威(propoxur)、硫雙威(thiodicarb)、硫芬濃(thiofanox)、三唑脈(triazamate)、三甲卡(trimethacarb)、XMC及二甲苯卡(xylylcarb);或有機磷酸鹽,如乙醯甲胺磷(acephate)、甲基吡啶磷(azamethiphos)、保棉磷-乙基(azinphos-ethyl)、保棉磷-甲基(azinphos-methyl)、硫線磷(cadusafos)、氯氧磷(chlorethoxyfos)、毒蟲畏(chlorfenvinphos)、氯密磷(chlormephos)、毒死蜱-甲基(chlorpyrifos-methyl)、蠅毒磷(coumaphos)、殺螟腈(cyanophos)、內吸磷-S-甲基(demeton-S-methyl)、二嗪磷(diazinon)、敵敵畏/DDVP(dichlorvos/DDVP)、百治磷(dicrotophos)、樂果(dimethoate)、二甲基威磷(dimethylvinphos)、乙拌磷(disulfoton)、EPN、乙硫磷(ethion)、滅線磷(ethoprophos)、奉磷爾(famphur)、苯線磷(fenamiphos)、殺螟硫磷(fenitrothion)、倍硫磷(fenthion)、噻唑磷(fosthiazate)、庚烯磷(heptenophos)、密塞扶(imicyafos)、異柳磷(isofenphos)、異丙基O-(甲氧基胺基硫代磷醯)水楊酸鹽、異唑磷(isoxathion)、馬拉硫磷(malathion)、敉卡敗(mecarbam)、甲胺磷(methamidophos)、殺撲磷(methidathion)、速滅磷(mevinphos)、久效磷(monocrotophos)、二溴磷(naled)、氧化樂果(omethoate)、碸吸磷-甲基(oxydemeton-methyl)、對硫磷-甲基(parathion-methyl)、稻豐散(phenthoate)、甲拌磷(phorate)、伏殺硫磷(phosalone)、亞胺硫磷(phosmet)、磷胺(phosphamidon)、辛硫磷(phoxim)、嘧啶磷-甲基(pirimiphos-methyl)、丙溴磷(profenofos)、強敵(propetamphos)、丙硫磷(prothiofos)、皮克扶(pyraclofos)、噠嗪硫磷(pyridaphenthion)、喹硫磷(quinalphos)、治螟磷(sulfotep)、特皮風(tebupirimfos)、雙硫磷(temephos)、特丁硫磷(terbufos)、殺蟲威(tetrachlorvinphos)、甲基乙(thiometon)、三唑磷(triazophos)、三卡封(triclorfon)
及維督辛(vamidothion)。
(2)GABA-閘氯道阻斷劑,例如環二烯類-有機氯,如氯丹(chlordane)及硫丹(endosulfan)或苯基吡唑(fiproles),如乙蟲腈(ethiprole)及氟蟲腈(fipronil)。
(3)鈉道調節劑,例如擬除蟲菊酯(pyrethroids),如氟酯菊酯(acrinathrin)、烯丙菊酯(allethrin)、d-順式-反式烯丙菊酯、d-反式烯丙菊酯、聯苯菊酯(bifenthrin)、生物烯丙菊酯(bioallethrin),生物烯丙菊酯S-環戊烯基異構物、生物苄呋菊酯(bioresmethrin)、乙氰菊酯(cycloprothrin)、氟氯氰菊酯(cyfluthrin),β-氟氯氰菊酯,氯氟氰菊酯(cyhalothrin),λ-氯氟氰菊酯、γ-氯氟氰菊酯、氯氰菊酯(cypermethrin),α-氯氰菊酯、β-氯氰菊酯、θ-氯氰菊酯、ζ-氯氰菊酯、苯氰菊酯(cyphenothrin)[(1R)-反式異構物]、溴氰菊酯(deltamethrin)、烯炔菊酯(empenthrin)[(EZ)-(1R)異構物]、順式氰戊菊酯(esfenvalerate)、醚菊酯(etofenprox)、甲氰菊酯(fenpropathrin)、氰戊菊酯(fenvalerate)、氟氰戊菊酯(flucythrinate)、氟氯苯菊酯(flumethrin)、tau-氟胺氰菊酯(tau-fluvalinate)、哈芬普(halfenprox)、嘧普辛(imiprothrin)、卡丹辛(kadethrin)、猛氟辛(momfluorothrin)、氯苯醚菊酯(permethrin)、醚菊酯(phenothrin)[(1R)-反式異構物]、丙炔菊酯(prallethrin)、除蟲菊酯(除蟲菊素)(pyrethrins(pyrethrum))、苄呋菊酯(resmethrin)、氟矽菊酯(silafluofen)、七氟菊酯(tefluthrin)、胺菊酯(tetramethrin)、胺菊酯[(1R)異構物]、四溴菊酯(tralomethrin)及菊酯(transfluthrin)或DDT或甲氧氯(methoxychlor)。
(4)菸鹼乙醯基膽鹼受體(nAChR)競爭調節劑,例如新菸鹼類殺蟲劑(neonicotinoids),如啶蟲脒(acetamiprid)、噻蟲胺(clothianidin)、呋蟲胺(dinotefuran)、吡蟲啉(imidacloprid)、烯啶蟲胺(nitenpyram)、噻蟲啉(thiacloprid)及噻蟲嗪(thiamethoxam)或尼古丁或硫負夆(sulfoxaflor)或氟吡喃酮(flupyradifurone)。
(5)菸鹼乙醯基膽鹼受體(nAChR)變構調節劑,例如多殺菌素(spinosyns),
如乙基多殺菌素(spinetoram)及多殺菌素(spinosad)。
(6)穀胺酸-閘氯道(GluCl)變構調節劑,例如阿維菌素/米爾倍黴素(avermectins/milbemycins),如阿維菌素(abamectin)、甲胺基阿維菌素苯甲酸鹽(emamectin benzoate)、滅幼寶(lepimectin)及米爾貝林(milbemectin)。
(7)保幼激素模仿劑,例如,保幼激素類似物,如烯蟲乙酯(hydroprene)、克皮尼(kinoprene)及烯蟲酯(methoprene)或苯氧威(fenoxycarb)或吡丙醚(pyriproxyfen)。
(8)多項非特異性(多位點)抑制劑,例如鹵代烷,如甲基溴及其他烷基鹵化物;或氯吡辛(chloropicrin)或硫醯氟或硼砂(borax)或吐酒石(tartar emetic)或異氰酸甲酯生成劑,如重氮甲(diazomet)及威百畝(metam)。
(9)弦音器調節劑,如吡蚜酮(pymetrozine)或氟啶蟲醯胺(flonicamide)。
(10)蟎蟲生長抑制劑,例如四蟎嗪(clofentezine)、噻蟎酮(hexythiazox)及氟蟎嗪(diflovidazin)或依殺蟎(etoxazole)。
(11)昆蟲腸膜之微生物干擾素,例如蘇雲金芽孢桿菌以色列亞種(Bacillus thuringiensis subspecies israelensis)、球形芽孢桿菌(Bacillus sphaericus)、蘇雲金芽孢桿菌蘇力菌亞種(Bacillus thuringiensis subspecies aizawai)、蘇雲金芽孢桿菌庫爾斯克亞種(Bacillus thuringiensis subspecies kurstaki)、蘇雲金芽孢桿菌擬步行亞種(Bacillus thuringiensis subspecies tenebrionis)及BT植物蛋白質:Cry1Ab,Cry1Ac,Cry1Fa,Cry1A.105,Cry2Ab,VIP3A,mCry3A,Cry3Ab,Cry3Bb,Cry34Ab1/35Ab1。
(12)線粒體ATP合成酶抑制劑,如ATP干擾素,例如丁醚脲(diafenthiuron)或有機錫化合物,如三唑錫(azocyclotin)、三環錫(cyhexatin)及苯丁錫(fenbutatin oxide)或克蟎特(propargite)或三氯殺蟎碸(tetradifon)。
(13)經由質子梯度而破壞氧化磷酸化的解偶合劑,例如溴蟲腈(chlorfenapyr)、DNOC及氟蟲胺(sulfluramid)。
(14)菸鹼乙醯基膽鹼受體道阻斷劑,例如殺蟲磺(bensultap)、殺螟丹鹽酸鹽(cartap hydrochloride)、殺蟲環(thiocyclam)、及硫甦坦-鈉(thiosultap-sodium)。
(15)幾丁質生合成抑制劑,0型,例如必三福隆(bistrifluron)、抑太保(chlorfluazuron)、除蟲脲(diflubenzuron)、福環隆(flucycloxuron)、氟蟲脲(flufenoxuron)、氟鈴脲(hexaflumuron)、虱蟎脲(lufenuron)、氟醯脲(novaluron)、氟蟲腈(noviflumuron)、伏蟲隆(teflubenzuron)及殺鈴脲(triflumuron)。
(16)幾丁質生合成抑制劑,1型,例如噻嗪酮(buprofezin)。
(17)蛻皮抑制劑(尤其是於雙翅目之情況時),例如環丙氨嗪(cyromazine)。
(18)蛻皮激素受體激動劑,例如氯邁芬尼(chromafenozide)、特丁苯醯肼(halofenozide)、甲氧蟲醯肼(methoxyfenozide)及雙苯醯肼(tebufenozide)。
(19)章魚胺能激動劑,例如雙甲脒(amitraz)。
(20)線粒體絡合物III電子傳遞抑制劑,例如伏蟻腙(hydramethylnon)或滅蟎醌(acequinocyl)或嘧蟎酯(fluacrypyrim)。
(21)線粒體絡合物I電子傳遞抑制劑,例如METI殺蟎蟲劑,如喹蟎醚(fenazaquin)、唑蟎酯(fenpyroximate)、吡密芬(pyrimidifen)、噠蟎靈(pyridaben)、吡蟎胺(tebufenpyrad)及噠芬吡(tolfenpyrad)或魚藤酮(rotenone)(Derris)。
(22)電壓-閘鈉道阻斷劑,例如茚蟲威或氰氟蟲腙(metaflumizone)。
(23)乙醯CoA羧基酶抑制劑,例如季酮酸及四密酸(tetramic acid)衍生物,如螺蟎酯(spirodiclofen)、螺甲蟎酯(spiromesifen)及螺蟲乙酯(spirotetramat)。
(24)線粒體絡合物IV電子傳遞抑制劑,例如膦類,如磷化鋁、磷化鈣、膦及磷化鋅,或氰化物、氰化鈣、氰化鉀及氰化鈉。
(25)線粒體絡合物II電子傳遞抑制劑,例如β-酮腈衍生物,如腈吡蟎酯(cyenopyrafen)及丁氟蟎酯(cyflumetofen)及苯胺基甲醯(carboxanilide),例如吡蟲啉(pyflubumide)。
(28)蘭尼鹼受體調節劑,例如二醯胺類,如氯蟲苯甲醯胺(chlorantraniliprole),
欣立普(cyantraniliprole)及氟蟲醯胺(flubendiamide),其他活性組成份,例如阿芬平(afidopyropen)、阿福拉納(afoxolaner)、印楝素(azadirachtin)、硫線磷(benclothiaz)、苯蟎特(苯并ximate)、聯苯肼酯(bifenazate)、布洛苯胺(broflanilide)、溴蟎酯(bromopropylate)、滅蟎猛(chinomethionat)、氯普瑞烯(chloroprallethrin)、冰晶石(cryolite)、環拉利吡(cyclaniliprole)、環螺普(cycloxaprid)、沙利度胺(cyhalodiamide)、二氯滿汰(dicloromezotiaz)、三氯殺蟎醇(dicofol)、ε-甲氧苄氟菊酯(epsilon metofluthrin)、ε-猛呋炫(epsilon momfluthrin)、呋滅困(flometoquin)、氟因(fluazaindolizine)、氟碸(fluensulfone)、氟芬柔(flufenerim)、氟蟲腈(flufenoxystrobin)、氟吡蟲(flufiprole)、氟己芳(fluhexafon)、氟吡菌醯胺(fluopyram)、氟嵐尼(fluralaner)、氟殺甲醯(fluxametamide)、呋喃醯肼(fufenozide)、戊吡蟲胍(guadipyr)、七氟菊酯(heptafluthrin)、吡蟲啉(imidaclothiz)、異菌脲(iprodione)、κ聯苯菊酯(kappa bifenthrin)、κ七氟菊酯(kappa tefluthrin)、羅嵐尼(lotilaner)、氯氟醚菊酯(meperfluthrin)、呱蟲啶(paichongding)、三氟甲吡醚(pyridalyl)、吡啶喹唑啉(pyrifluquinazon)、嘧菌酯(pyr亞胺基strobin)、螺雙溴芬(spirobudiclofen)、四氫卟吩(tetramethylfluthrin)、四硝基吡咯(tetraniliprole)、四氯蟲醯胺(tetrachlorantraniliprole)、汰線芬(tioxazafen)、硫代肟(thiofluoximate)、三氟苯嘧啶(triflumezopyrim)及碘甲烷;其他根據堅強芽孢桿菌(Bacillus firmus)(I-1582,BioNeem,Votivo),以及下列化合物之製劑:1-{2-氟-4-甲基-5-[(2,2,2-三氟乙基)亞磺醯基]苯基}-3-(三氟甲基)-1H-1,2,4-三唑-5-胺(已知於WO2006/043635)(CAS 885026-50-6),{1'-[(2E)-3-(4-氯苯基)丙-2-烯-1-基]-5-氟螺[吲哚-3,4'-六氫吡啶]-1(2H)-基}(2-氯吡啶-4-基)甲酮(已知於WO2003/106457)(CAS 637360-23-7),2-氯-N-[2-{1-[(2E)-3-(4-氯苯基)丙-2-烯-1-基]六氫吡啶-4-基}-4-(三氟甲基)苯基]異菸醯胺(已知於WO2006/003494)(CAS 872999-66-1),3-(4-氯-2,6-二甲基苯基)-4-羥基-8-甲
氧基-1,8-二氮雜螺[4.5]癸-3-烯-2-酮(已知於WO 2010052161)(CAS 1225292-17-0),3-(4-氯-2,6-二甲基苯基)-8-甲氧基-2-酮基-1,8-二氮雜螺[4.5]癸-3-烯-4-基乙基碳酸酯(已知於EP 2647626)(CAS-1440516-42-6),4-(丁-2-炔-1-基氧基)-6-(3,5-二甲基六氫吡啶-1-基)-5-氟嘧啶(已知於WO2004/099160)(CAS 792914-58-0),PF1364(已知於JP2010/018586)(CAS Reg.No.1204776-60-2),N-[(2E)-1-[(6-氯吡啶-3-基)甲基]吡啶-2(1H)-亞基]-2,2,2-三氟乙醯胺(已知於WO2012/029672)(CAS 1363400-41-2),(3E)-3-[1-[(6-氯-3-吡啶基)甲基]-2-吡啶亞基]-1,1,1-三氟丙-2-酮(已知於WO2013/144213)(CAS 1461743-15-6),N-[3-(苄基胺基甲醯基)-4-氯苯基]-1-甲基-3-(五氟乙基)-4-(三氟甲基)-1H-吡唑-5-甲醯胺(已知於WO2010/051926)(CAS 1226889-14-0),5-溴-4-氯-N-[4-氯-2-甲基-6-(甲基胺基甲醯基)苯基]-2-(3-氯-2-吡啶基)吡唑-3-甲醯胺(已知於CN103232431)(CAS 1449220-44-3),4-[5-(3,5-二氯苯基)-4,5-二氫-5-(三氟甲基)-3-異唑基]-2-甲基-N-(順式-1-氧撐-3-噻坦基)苯醯胺,4-[5-(3,5-二氯苯基)-4,5-二氫-5-(三氟甲基)-3-異唑基]-2-甲基-N-(反式-1-氧撐-3-噻坦基)苯醯胺及4-[(5S)-5-(3,5-二氯苯基)-4,5-二氫-5-(三氟甲基)-3-異唑基]-2-甲基-N-(順式-1-氧撐-3-噻坦基)苯醯胺(已知於WO 2013/050317 A1)(CAS 1332628-83-7),N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)亞磺醯基]丙醯胺,(+)-N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)亞磺醯基]丙醯胺及(-)-N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)亞磺醯基]丙醯胺(已知於WO 2013/162715 A2,WO 2013/162716 A2,US 2014/0213448 A1)(CAS 1477923-37-7),5-[[(2E)-3-氯-2-丙烯-1-基]胺基]-1-[2,6-二氯-4-(三氟甲基)苯基]-4-[(三氟甲基)亞磺醯基]-1H-吡唑-3-甲腈(已知於CN 101337937 A)(CAS 1105672-77-2),3-溴-N-[4-氯-2-甲基-6-[(甲基胺基)硫酮基甲基]苯基]-1-(3-
氯-2-吡啶基)-1H-吡唑-5-甲醯胺,(Liudaibenjiaxuanan,已知於CN 103109816 A)(CAS 1232543-85-9);N-[4-氯-2-[[(1,1-二甲基乙基)胺基]羰基]-6-甲基苯基]-1-(3-氯-2-吡啶基)-3-(氟甲氧基)-1H-吡唑-5-甲醯胺(已知於WO 2012/034403 A1)(CAS 1268277-22-0),N-[2-(5-胺基-1,3,4-噻二唑-2-基)-4-氯-6-甲基苯基]-3-溴-1-(3-氯-2-吡啶基)-1H-吡唑-5-甲醯胺(已知於WO 2011/085575 A1)(CAS 1233882-22-8),4-[3-[2,6-二氯-4-[(3,3-二氯-2-丙烯-1-基)氧基]苯氧基]丙氧基]-2-甲氧基-6-(三氟甲基)嘧啶(已知於CN 101337940 A)(CAS 1108184-52-6);(2E)-及2(Z)-2-[2-(4-氰基苯基)-1-[3-(三氟甲基)苯基]乙亞基]-N-[4-(二氟甲氧基)苯基]肼甲醯胺(已知於CN 101715774 A)(CAS 1232543-85-9);環丙烷羧酸3-(2,2-二氯乙烯基)-2,2-二甲基-4-(1H-苯并咪唑-2-基)苯基酯(已知於CN 103524422 A)(CAS 1542271-46-4);(4aS)-7-氯-2,5-二氫-2-[[(甲氧基羰基)[4-[(三氟甲基)硫基]苯基]胺基]羰基]茚并[1,2-e][1,3,4]二-4a(3H)-羧酸甲酯(已知於CN 102391261 A)(CAS 1370358-69-2);6-去氧-3-O-乙基-2,4-二-O-甲基-1-[N-[4-[1-[4-(1,1,2,2,2-五氟乙氧基)苯基]-1H-1,2,4-三唑-3-基]苯基]胺基甲酸基]-α-L-甘露吡喃糖(已知於US 2014/0275503 A1)(CAS 1181213-14-8);8-(2-環丙基甲氧基-4-三氟甲基苯氧基)-3-(6-三氟甲基嗒-3-基)-3-氮雜二環[3.2.1]辛烷(CAS 1253850-56-4),(8-反)-8-(2-環丙基甲氧基-4-三氟甲基苯氧基)-3-(6-三氟甲基嗒-3-基)-3-氮雜二環[3.2.1]辛烷(CAS 933798-27-7),(8-順)-8-(2-環丙基甲氧基-4-三氟甲基苯氧基)-3-(6-三氟甲基嗒-3-基)-3-氮雜二環[3.2.1]辛烷(已知於WO 2007040280 A1,WO 2007040282 A1)(CAS 934001-66-8)及N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)硫基]丙醯胺(已知於WO 2015/058021 A1,WO 2015/058028 A1)(CAS 1477919-27-9)。
以其等之通用名稱指明之活性化合物為已知且係說明於,例如,「Pesticide Manual」(16th Ed.British Crop Protection Council)或可於網路搜尋(例如:http://www.alanwood.net/pesticides)。
所有於(1)至(15)類中所提及之混合的組份,視情況可以,亦可與適當的鹼或酸形成鹽類,如果其等根據其官能基團而能如此。所有於(1)至(15)類中提及之殺真菌性混合的組份,視情況可以,可包括互變異構型式。
1)麥角甾醇生合成抑制劑,例如(1.001)環唑醇(cyproconazole),(1.002)苯醚甲環唑(difenoconazole),(1.003)氧氟康唑(epoxiconazole),(1.004)環醯菌胺(fenhexamid),(1.005)苯銹啶(fenpropidin),(1.006)丁苯嗎啉(fenpropimorph),(1.007)胺苯吡菌酮(fenpyrazamine),(1.008)氟喹唑(fluquinconazole),(1.009)粉唑醇(flutriafol),(1.010)抑黴唑(imazalil),(1.011)硫酸抑黴唑(imazalil sulfate),(1.012)益康唑(ipconazole),(1.013)葉菌唑(metconazole),(1.014)腈菌唑(myclobutanil),(1.015)多效唑(paclobutrazol),(1.016)丙氯靈(prochloraz),(1.017)丙環唑(propiconazole),(1.018)丙硫菌唑(prothioconazole),(1.019)啶菌唑(pyrisoxazole),(1.020)螺環菌胺(spiroxamine),(1.021)戊唑醇(tebuconazole),(1.022)四氟唑(tetraconazole),(1.023)三唑醇(triadimenol),(1.024)克啉菌(tridemorph),(1.025)戊叉唑菌(triticonazole),(1.026)(1R,2S,5S)-5-(4-氯苄基)-2-(氯甲基)-2-甲基-1-(1H-1,2,4-三唑-1-基甲基)環戊醇,(1.027)(1S,2R,5R)-5-(4-氯苄基)-2-(氯甲基)-2-甲基-1-(1H-1,2,4-三唑-1-基甲基)環戊醇,(1.028)(2R)-2-(1-氯環丙基)-4-[(1R)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇(1.029)(2R)-2-(1-氯環丙基)-4-[(1S)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇,(1.030)(2R)-2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇,(1.031)(2S)-2-(1-氯環丙基)-4-[(1R)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇,(1.032)(2S)-2-(1-氯環丙基)-4-[(1S)-2,2-二氯環丙
基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇,(1.033)(2S)-2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇,(1.034)(R)-[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-1,2-唑-4-基](吡啶-3-基)甲醇,(1.035)(S)-[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-1,2-唑-4-基](吡啶-3-基)甲醇,(1.036)[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-1,2-唑-4-基](吡啶-3-基)甲醇,(1.037)1-({(2R,4S)-2-[2-氯-4-(4-氯苯氧基)苯基]-4-甲基-1,3-二茂烷-2-基}甲基)-1H-1,2,4-三唑,(1.038)1-({(2S,4S)-2-[2-氯-4-(4-氯苯氧基)苯基]-4-甲基-1,3-二茂烷-2-基}甲基)-1H-1,2,4-三唑,(1.039)1-{[3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑-5-基硫基氰酸鹽,(1.040)1-{[rel(2R,3R)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑-5-基硫基氰酸鹽,(1.041)1-{[rel(2R,3S)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑-5-基硫基氰酸鹽,(1.042)2-[(2R,4R,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.043)2-[(2R,4R,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.044)2-[(2R,4S,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.045)2-[(2R,4S,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.046)2-[(2S,4R,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.047)2-[(2S,4R,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.048)2-[(2S,4S,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.049)2-[(2S,4S,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.050)2-[1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.051)2-[2-氯-4-(2,4-二氯苯氧基)苯基]-1-(1H-1,2,4-三唑-1-
基)丙-2-醇,(1.052)2-[2-氯-4-(4-氯苯氧基)苯基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇,(1.053)2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇,(1.054)2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)戊-2-醇,(1.055)2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇,(1.056)2-{[3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.057)2-{[rel(2R,3R)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.058)2-{[rel(2R,3S)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-2,4-二氫-3H-1,2,4-三唑-3-硫酮,(1.059)5-(4-氯苄基)-2-(氯甲基)-2-甲基-1-(1H-1,2,4-三唑-1-基甲基)環戊醇,(1.060)5-(烯丙基硫烷基)-1-{[3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑,(1.061)5-(烯丙基硫烷基)-1-{[rel(2R,3R)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑,(1.062)5-(烯丙基硫烷基)-1-{[rel(2R,3S)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑,(1.063)N'-(2,5-二甲基-4-{[3-(1,1,2,2-四氟乙氧基)苯基]硫烷基}苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.064)N'-(2,5-二甲基-4-{[3-(2,2,2-三氟乙氧基)苯基]硫烷基}苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.065)N'-(2,5-二甲基-4-{[3-(2,2,3,3-四氟丙氧基)苯基]硫烷基}苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.066)N'-(2,5-二甲基-4-{[3-(五氟乙氧基)苯基]硫烷基}苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.067)N'-(2,5-二甲基-4-{3-[(1,1,2,2-四氟乙基)硫烷基]苯氧基}苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.068)N'-(2,5-二甲基-4-{3-[(2,2,2-三氟乙基)硫烷基]苯氧基}苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.069)N'-(2,5-二甲基-4-{3-[(2,2,3,3-四氟丙基)硫烷基]苯氧基}苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.070)N'-(2,5-二甲基-4-{3-[(五氟乙基)硫烷基]苯氧基}苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.071)N'-(2,5-二甲基-4-苯氧基苯基)-N-乙基-N-甲基亞
胺基甲醯胺,(1.072)N'-(4-{[3-(二氟甲氧基)苯基]硫烷基}-2,5-二甲基苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.073)N'-(4-{3-[(二氟甲基)硫烷基]苯氧基}-2,5-二甲基苯基)-N-乙基-N-甲基亞胺基甲醯胺,(1.074)N'-[5-溴-6-(2,3-二氫-1H-茚-2-基氧基)-2-甲基吡啶-3-基]-N-乙基-N-甲基亞胺基甲醯胺,(1.075)N'-{4-[(4,5-二氯-1,3-噻唑-2-基)氧基]-2,5-二甲基苯基}-N-乙基-N-甲基亞胺基甲醯胺,(1.076)N'-{5-溴-6-[(1R)-1-(3,5-二氟苯基)乙氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基亞胺基甲醯胺,(1.077)N'-{5-溴-6-[(1S)-1-(3,5-二氟苯基)乙氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基亞胺基甲醯胺,(1.078)N'-{5-溴-6-[(順式-4-異丙基環己基)氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基亞胺基甲醯胺,(1.079)N'-{5-溴-6-[(反式-4-異丙基環己基)氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基亞胺基甲醯胺,(1.080)N'-{5-溴-6-[1-(3,5-二氟苯基)乙氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基亞胺基甲醯胺。
2)於絡合物I或II中之呼吸道抑制劑,例如(2.001)苯并烯氟菌唑(benzovindiflupyr),(2.002)聯苯吡菌胺(bixafen),(2.003)啶醯菌胺(boscalid),(2.004)萎銹靈(carboxin),(2.005)扶吡藍(fluopyram),(2.006)氟醯胺(flutolanil),(2.007)扶吡塞(fluxapyroxad),(2.008)扶吡塞(furametpyr),(2.009)異紛邁(isofetamid),(2.010)異皮姆(isopyrazam)((抗差向異構對映體1R,4S,9S)),(2.011)異皮姆(抗差向異構對映體1S,4R,9R),(2.012)異皮姆(抗差向異構外消旋物1RS,4SR,9SR),(2.013)異皮姆(順-差向異構外消旋物1RS,4SR,9RS及抗差向異構外消旋物1RS,4SR,9SR之混合物),(2.014)異皮姆(順-差向異構對映體1R,4S,9R),(2.015)異皮姆(順-差向異構對映體1S,4R,9S),(2.016)異皮姆(順-差向異構外消旋物1RS,4SR,9RS),(2.017)盼扶芬(penflufen),(2.018)吡噻菌胺(penthiopyrad),(2.019)吡福密芬(pydiflumetofen),(2.020)吡福(pyraziflumid),(2.021)環丙沙星(sedaxane),(2.022)1,3-二甲基-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-甲醯胺,
(2.023)1,3-二甲基-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-甲醯胺,(2.024)1,3-二甲基-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-甲醯胺,(2.025)1-甲基-3-(三氟甲基)-N-[2'-(三氟甲基)bi苯基-2-基]-1H-吡唑-4-甲醯胺,(2.026)2-氟-6-(三氟甲基)-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)苯醯胺,(2.027)3-(二氟甲基)-1-甲基-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-甲醯胺,(2.028)3-(二氟甲基)-1-甲基-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-甲醯胺,(2.029)3-(二氟甲基)-1-甲基-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-甲醯胺,(2.030)3-(二氟甲基)-N-(7-氟-1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1-甲基-1H-吡唑-4-甲醯胺,(2.031)3-(二氟甲基)-N-[(3R)-7-氟-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1-甲基-1H-吡唑-4-甲醯胺,(2.032)3-(二氟甲基)-N-[(3S)-7-氟-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1-甲基-1H-吡唑-4-甲醯胺,(2.033)5,8-二氟-N-[2-(2-氟-4-{[4-(三氟甲基)吡啶-2-基]氧基}苯基)乙基]喹唑啉-4-胺,(2.034)N-(2-環戊基-5-氟苄基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.035)N-(2-第三丁基-5-甲基苄基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.036)N-(2-第三丁基苄基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.037)N-(5-氯-2-乙基苄基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.038)N-(5-氯-2-異丙基苄基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.039)N-[(1R,4S)-9-(二氯亞甲基)-1,2,3,4-四氫-1,4-甲撐萘-5-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-甲醯胺,(2.040)N-[(1S,4R)-9-(二氯亞甲基)-1,2,3,4-四氫-1,4-甲撐萘-5-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-甲醯胺,(2.041)N-[1-(2,4-二氯苯基)-1-甲氧基丙-2-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-甲醯胺,(2.042)N-[2-氯-6-(三氟甲基)苄基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.043)N-[3-氯-2-氟-6-(三氟甲基)苄基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-
甲醯胺,(2.044)N-[5-氯-2-(三氟甲基)苄基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.045)N-環丙基-3-(二氟甲基)-5-氟-1-甲基-N-[5-甲基-2-(三氟甲基)苄基]-1H-吡唑-4-甲醯胺,(2.046)N-環丙基-3-(二氟甲基)-5-氟-N-(2-氟-6-異丙基苄基)-1-甲基-1H-吡唑-4-甲醯胺,(2.047)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基-5-甲基苄基)-1-甲基-1H-吡唑-4-甲醯胺,(2.048)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基苄基)-1-甲基-1H-吡唑-4-碳硫代醯胺,(2.049)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基苄基)-1-甲基-1H-吡唑-4-甲醯胺,(2.050)N-環丙基-3-(二氟甲基)-5-氟-N-(5-氟-2-異丙基苄基)-1-甲基-1H-吡唑-4-甲醯胺,(2.051)N-環丙基-3-(二氟甲基)-N-(2-乙基-4,5-二甲基苄基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.052)N-環丙基-3-(二氟甲基)-N-(2-乙基-5-氟苄基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.053)N-環丙基-3-(二氟甲基)-N-(2-乙基-5-甲基苄基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.054)N-環丙基-N-(2-環丙基-5-氟苄基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.055)N-環丙基-N-(2-環丙基-5-甲基苄基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺,(2.056)N-環丙基-N-(2-環丙基苄基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-甲醯胺。
3)於絡合物III中之呼吸道抑制劑,例如(3.001)艾美脫賓(ametoctradin),(3.002)艾蜜讓(amisulbrom),(3.003)嘧菌酯(azoxystrobin),(3.004)康甲氧基脫賓(coumethoxystrobin),(3.005)康氧脫賓(coumoxystrobin),(3.006)氰霜胺(cyazofamid),(3.007)二氧脫賓(dimoxystrobin),(3.008)烯肟菌酯(enoxastrobin),(3.009)唑菌酮(famoxadon),(3.010)咪唑菌酮(fenamidon),(3.011)氟蟲腈(flufenoxystrobin),(3.012)氟嘧菌酯(fluoxastrobin),(3.013)醚菌酯-甲基(kresoxim-methyl),(3.014)美托黴素(metominostrobin),(3.015)肟醚菌胺(orysastrobin),(3.016)啶氧菌酯(picoxystrobin),(3.017)唑菌胺酯(pyraclostrobin),(3.018)唑菌胺酯(pyrametostrobin),(3.019)吡肟菌酯
(pyraoxystrobin),(3.020)肟菌酯(trifloxystrobin),(3.021)(2E)-2-{2-[({[(1E)-1-(3-{[(E)-1-氟-2-苯基乙烯基]氧基}苯基)乙亞基]胺基}氧基)甲基]苯基}-2-(甲氧基亞胺基)-N-甲基乙醯胺,(3.022)(2E,3Z)-5-{[1-(4-氯苯基)-1H-吡唑-3-基]氧基}-2-(甲氧基亞胺基)-N,3-二甲基戊-3-烯醯胺,(3.023)(2R)-2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺,(3.024)(2S)-2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺,(3.025)(3S,6S,7R,8R)-8-苄基-3-[({3-[(異丁醯氧基)甲氧基]-4-甲氧基吡啶-2-基}羰基)胺基]-6-甲基-4,9-二酮基-1,5-二喃-7-基2-甲基丙酸酯,(3.026)2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺,(3.027)N-(3-乙基-3,5,5-三甲基環己基)-3-甲醯胺-2-羥基苯醯胺,(3.028)(2E,3Z)-5-{[1-(4-氯-2-氟苯基)-1H-吡唑-3-基]氧基}-2-(甲氧基亞胺基)-N,3-二甲基戊-3-烯醯胺。
4)有絲分裂及細胞分裂抑制劑,例如(4.001)多菌靈(carbendazim),(4.002)乙黴威(diethofencarb),(4.003)噻唑菌胺(ethaboxam),(4.004)扶吡克靈(fluopicolid),(4.005)戊菌隆(pencycuron),(4.006)噻菌靈(thiabendazole),(4.007)硫菌靈-甲基(thiophanate-methyl),(4.008)苯醯菌胺(zoxamide),(4.009)3-氯-4-(2,6-二氟苯基)-6-甲基-5-苯基嗒,(4.010)3-氯-5-(4-氯苯基)-4-(2,6-二氟苯基)-6-甲基嗒,(4.011)3-氯-5-(6-氯吡啶-3-基)-6-甲基-4-(2,4,6-三氟苯基)嗒,(4.012)4-(2-溴-4-氟苯基)-N-(2,6-二氟苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.013)4-(2-溴-4-氟苯基)-N-(2-溴-6-氟苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.014)4-(2-溴-4-氟苯基)-N-(2-溴苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.015)4-(2-溴-4-氟苯基)-N-(2-氯-6-氟苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.016)4-(2-溴-4-氟苯基)-N-(2-氯苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.017)4-(2-溴-4-氟苯基)-N-(2-氟苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.018)4-(2-氯-4-氟苯基)-N-(2,6-二氟苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.019)4-(2-氯-4-氟苯
基)-N-(2-氯-6-氟苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.020)4-(2-氯-4-氟苯基)-N-(2-氯苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.021)4-(2-氯-4-氟苯基)-N-(2-氟苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.022)4-(4-氯苯基)-5-(2,6-二氟苯基)-3,6-二甲基嗒,(4.023)N-(2-溴-6-氟苯基)-4-(2-氯-4-氟苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.024)N-(2-溴苯基)-4-(2-氯-4-氟苯基)-1,3-二甲基-1H-吡唑-5-胺,(4.025)N-(4-氯-2,6-二氟苯基)-4-(2-氯-4-氟苯基)-1,3-二甲基-1H-吡唑-5-胺。
5)具有多位點活性能力之化合物,例如(5.001)波爾多(Bordeaux)混合物,(5.002)敵菌丹(captafol),(5.003)克菌丹(captan),(5.004)百菌清(chlorthalonil),(5.005)氫氧化銅(5.006)環烷酸銅,(5.007)氧化銅,(5.008)氧氯化銅,(5.009)硫酸銅(2+),(5.010)二氰蒽醌(dithianon),(5.011)多果定(dodin),(5.012)滅菌丹(folpet),(5.013)代森錳鋅(mancozeb),(5.014)代森錳(maneb),(5.015)代森聯(metiram),(5.016)代森聯鋅(zinc metiram),(5.017)羥基喹啉銅(copper oxine),(5.018)丙森鋅(propineb),(5.019)硫及硫製劑,包括多硫化鈣,(5.020)福美雙(thiram),(5.021)代森鋅(zineb),(5.022)福美鋅(ziram)。
6)能觸發宿主防禦之化合物,例如(6.001)噻二唑素-S-甲基(acibenzolar-S-methyl),(6.002)異噻菌胺(isotianil),(6.003)噻菌靈(probenazole),(6.004)噻醯菌胺(tiadinil)。
7)胺基酸及/或蛋白質生合成抑制劑,例如(7.001)嘧菌環胺(cyprodinil),(7.002)春日黴素(kasugamycin),(7.003)春日黴素氫氯酸水合物,(7.004)土黴素(oxytetracycline),(7.005)二甲嘧菌胺(pyrimethanil),(7.006)3-(5-氟-3,3,4,4-四甲基-3,4-二氫異喹啉-1-基)喹啉。
(8)ATP生產抑制劑,例如(8.001)矽噻菌胺(silthiofam)。
9)細胞壁合成抑制劑,例如(9.001)苯噻菌胺(benthiavalicarb),(9.002)烯
醯嗎啉(dimethomorph),(9.003)氟嗎啉(flumorph),(9.004)異丙菌胺(iprovalicarb),(9.005)雙炔醯菌胺(mandipropamid),(9.006)丁吡嗎啉(pyrimorph),(9.007)霜黴滅(valifenalate),(9.008)(2E)-3-(4-第三丁基苯基)-3-(2-氯吡啶-4-基)-1-(嗎福啉-4-基)丙-2-烯-1-酮,(9.009)(2Z)-3-(4-第三丁基苯基)-3-(2-氯吡啶-4-基)-1-(嗎福啉-4-基)丙-2-烯-1-酮。
10)脂質及膜合成抑制劑,例如(10.001)霜黴威(propamocarb),(10.002)霜黴威鹽酸鹽,(10.003)立枯磷-甲基(tolclofos-methyl)。
11)黑色素生合成抑制劑,例如(11.001)三環唑(tricyclazole),(11.002)2,2,2-三氟乙基{3-甲基-1-[(4-甲基苯甲醯)胺基]丁-2-基}胺基甲酸酯。
12)核酸合成抑制劑,例如(12.001)苯霜靈(benalaxyl),(12.002)苯霜靈-M(精苯霜靈(kiralaxyl)),(12.003)甲霜靈(metalaxyl),(12.004)甲霜靈-M(精甲霜靈(mefenoxam))。
13)信號傳導抑制劑,例如(13.001)咯菌腈(fludioxonil),(13.002)撲海因(iprodione),(13.003)速克靈(procymidone),(13.004)丙氯靈(proquinazid),(13.005)喹氧靈(quinoxyfen),(13.006)乙烯菌核利(vinclozolin)。
14)可充當解偶劑之化合物,例如(14.001)氟啶胺(fluazinam),(14.002)敵蟎普(meptyldinocap)。
15)其他化合物,例如(15.001)脫落酸,(15.002)苯并噻唑,(15.003)必撲辛(bethoxazin),(15.004)辣椒素(capsimycin),(15.005)香旱芹酮(carvone),(15.006)滅蟎猛(chinomethionat),(15.007)硫雜靈(cufraneb),(15.008)環氟菌胺(cytlufenamid),(15.009)清菌脲(cymoxanil),(15.010)環丙磺醯胺(cyprosulfamide),(15.011)扶丁尼(flutianil),(15.012)三乙膦酸鋁(fosetyl-aluminium),(15.013)三乙膦酸鈣(fosetyl-calcium),(15.014)三乙膦酸鈉(fosetyl-sodium),(15.015)異硫基氰酸甲酯,(15.016)苯菌酮(metrafenon),(15.017)米多黴素(mildiomycin),(15.018)納他黴素
(natamycin),(15.019)二甲基二硫代胺基甲酸鎳,(15.020)硝基噻-異丙基(nitrothal-isopropyl),(15.021)阨幕卡(oxamocarb),(15.022)氟噻唑吡乙酮(oxathiapiprolin),(15.023)奧施康定(oxyfenthiin),(15.024)五氯苯酚及鹽類,(15.025)膦酸及其鹽類,(15.026)霜黴威-扶提雷(propamocarb-fosetylate),(15.027)螺甲蟎酯(pyriofenone(氯芬酮(chlazafenone)))(15.028)雙炔醯菌胺(tebufloquin),(15.029)葉枯酞(tecloftalam),(15.030)菌胺(tolnifanide),(15.031)1-(4-{4-[(5R)-5-(2,6-二氟苯基)-4,5-二氫-1,2-唑-3-基]-1,3-噻唑-2-基}六氫吡啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮,(15.032)1-(4-{4-[(5S)-5-(2,6-二氟苯基)-4,5-二氫-1,2-唑-3-基]-1,3-噻唑-2-基}六氫吡啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮,(15.033)2-(6-苄基吡啶-2-基)喹唑啉,(15.034)2,6-二甲基-1H,5H-[1,4]二噻因(dithiino)[2,3-c:5,6-c']二吡咯-1,3,5,7(2H,6H)-四酮,(15.035)2-[3,5-聯(二氟甲基)-1H-吡唑-1-基]-1-[4-(4-{5-[2-(丙-2-炔-1-基氧基)苯基]-4,5-二氫-1,2-唑-3-基}-1,3-噻唑-2-基)六氫吡啶-1-基]乙酮,(15.036)2-[3,5-聯(二氟甲基)-1H-吡唑-1-基]-1-[4-(4-{5-[2-氯-6-(丙-2-炔-1-基氧基)苯基]-4,5-二氫-1,2-唑-3-基}-1,3-噻唑-2-基)六氫吡啶-1-基]乙酮,(15.037)2-[3,5-聯(二氟甲基)-1H-吡唑-1-基]-1-[4-(4-{5-[2-氟-6-(丙-2-炔-1-基氧基)苯基]-4,5-二氫-1,2-唑-3-基}-1,3-噻唑-2-基)六氫吡啶-1-基]乙酮,(15.038)2-[6-(3-氟-4-甲氧基苯基)-5-甲基吡啶-2-基]喹唑啉,(15.039)2-{(5R)-3-[2-(1-{[3,5-聯(二氟甲基)-1H-吡唑-1-基]乙醯}六氫吡啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-唑-5-基}-3-氯苯基甲烷磺酸酯,(15.040)2-{(5S)-3-[2-(1-{[3,5-聯(二氟甲基)-1H-吡唑-1-基]乙醯}六氫吡啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-唑-5-基}-3-氯苯基甲烷磺酸酯,(15.041)2-{2-[(7,8-二氟-2-甲基喹啉-3-基)氧基]-6-氟苯基}丙-2-醇,(15.042)2-{2-氟-6-[(8-氟-2-甲基喹啉-3-基)氧基]苯基}丙-2-醇,(15.043)2-{3-[2-(1-{[3,5-聯(二氟甲基)-1H-吡唑-1-基]乙醯}六氫吡啶-4-基)-1,3-噻唑
-4-基]-4,5-二氫-1,2-唑-5-基}-3-氯苯基甲烷磺酸酯,(15.044)2-{3-[2-(1-{[3,5-聯(二氟甲基)-1H-吡唑-1-基]乙醯}六氫吡啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-唑-5-基}苯基甲烷磺酸酯,(15.045)2-苯基苯酚及其鹽類,(15.046)3-(4,4,5-三氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉,(15.047)3-(4,4-二氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉,(15.048)4-胺基-5-氟嘧啶-2-醇(互變異構型式:4-胺基-5-氟嘧啶-2(1H)-酮),(15.049)4-酮基-4-[(2-苯基乙基)胺基]丁酸,(15.050)5-胺基-1,3,4-噻二唑-2-硫醇,(15.051)5-氯-N'-苯基-N'-(丙-2-炔-1-基)噻吩2-硫磷(sulphono)醯肼,(15.052)5-氟-2-[(4-氟苄基)氧基]嘧啶-4-胺,(15.053)5-氟-2-[(4-甲基苄基)氧基]嘧啶-4-胺,(15.054)9-氟-2,2-二甲基-5-(喹啉-3-基)-2,3-二氫-1,4-苯并氧雜吖庚因,(15.055){6-[({[(Z)-(1-甲基-1H-四唑-5-基)(苯基)亞甲基]胺基}氧基)甲基]吡啶-2-基}胺基甲酸丁-3-炔-1-基酯,(15.056)(2Z)-3-胺基-2-氰基-3-苯基丙烯酸乙酯,(15.057)吩-1-羧酸,(15.058)3,4,5-三羥基苯甲酸丙酯,(15.059)喹啉-8-醇,(15.060)喹啉-8-醇硫酸酯(2:1),(15.061){6-[({[(1-甲基-1H-四唑-5-基)(苯基)亞甲基]胺基}氧基)甲基]吡啶-2-基}胺基甲酸第三丁酯。
式(I)化合物可與生物性殺害蟲劑合併。
生物性殺害蟲劑尤其是包括細菌、真菌、酵母菌、植物萃出物及由微生物所形成之產物,包括蛋白質及次級代謝產物。
生物性殺害蟲劑包括細菌,如形成孢子的細菌、根克隆的細菌及用作為生物性殺昆蟲劑,殺真菌劑或殺線蟲劑的細菌。
此等細菌,其係使用或可用作為生物性殺害蟲劑,之實例為:解澱粉芽孢桿菌(Bacillus amyloliquefaciens)、菌株FZB42(DSM 231179)、或蠟狀芽孢桿菌(Bacillus cereus),尤其是蠟狀芽孢桿菌菌株CNCM I-1562
或堅強芽孢桿菌(Bacillus firmus)、菌株I-1582(登錄編號CNCM I-1582)或短小芽孢桿菌(Bacillus pumilus),尤其是菌株GB34(登錄編號ATCC 700814)及菌株QST2808(登錄編號NRRL B-30087)、或枯草芽孢桿菌(Bacillus subtilis),尤其是菌株GB03(登錄編號ATCC SD-1397)、或枯草芽孢桿菌菌株QST713(登錄編號NRRL B-21661)或枯草芽孢桿菌菌株OST 30002(登錄編號NRRL B-50421)、蘇雲金芽孢桿菌(Bacillus thuringiensis),尤其是蘇雲金芽孢桿菌以色列亞種(血清型H-14)、菌株AM65-52(登錄編號ATCC 1276)、或蘇雲金芽孢桿菌蘇力菌亞種,尤其是菌株ABTS-1857(SD-1372)、或蘇雲金芽孢桿菌庫爾斯克亞種菌株HD-1、或蘇雲金芽孢桿菌擬步行亞種菌株NB 176(SD-5428)、穿刺巴氏桿菌(Pasteuria penetrans)、巴氏桿菌(Pasteuria spp.)(腎形線蟲(Rotylenchulus reniform)線蟲)-PR3(登錄編號ATCC SD-5834)、細黃鏈黴(Streptomyces microflavus)菌株AQ6121(=QRD 31.013,NRRL B-50550)、鮮黃鏈黴(Streptomyces galbus)菌株AQ 6047(登錄編號NRRL 30232)。
真菌及酵母菌,其係使用或可用作為生物殺害蟲劑,之實例為:白殭菌(Beauveria bassiana),特別是菌株ATCC 74040、盾殼黴(Coniothyrium minitans),特別是菌株CON/M/91-8(登錄編號DSM-9660)、蚧黴屬(Lecanicillium spp.),特別是菌株HRO LEC 12、蠟蚧輪枝菌(Lecanicillium lecanii),(以前稱為蠟蚧輪枝(Verticillium lecanii)),特別是菌株KV01、金龜子綠僵菌(Metarhizium anisopliae),特別是菌株F52(DSM3884/ATCC 90448)、梅奇腐病菌(Metschnikowia fructicola),特別是菌株NRRL Y-30752、玫煙色擬青黴菌(Paecilomyces fumosoroseus)(新:玫煙色棒束孢(Isaria fumosorosea)),特別是菌株IFPC 200613、或菌株Apopka 97(登錄編號ATCC 20874)、淡紫擬青黴(Paecilomyces lilacinus),特別是淡紫擬青黴(P.lilacinus)菌株251(AGAL 89/030550)、大孢籃狀菌(Talaromyces flavus),特別是菌株
V117b、深綠木黴(Trichoderma atroviride),特別是菌株SC1(登錄編號CBS 122089)、哈茨木黴(Trichoderma harzianum),特別是哈茨木黴rifai T39(登錄編號CNCM I-952)。
用作為或可用作為生物殺害蟲劑之病毒的實例為:茶小卷葉蛾(Adoxophyes orana)(夏日果實捲葉蛾summer fruit tortrix))顆粒體病毒(GV)、蘋果蠹蛾(Cydia pomonella)(蠹蛾(codling moth))顆粒體病毒(GV)、棉鈴實夜蛾(Helicoverpa armigera)(棉花螟蛉(cotton bollworm))核型多角體病毒(NPV)、甜菜夜蛾(Spodoptera exigua)(甜菜夜蛾)mNPV、草地黏蟲(Spodoptera frugiperda)(草地夜蛾(fall armyworm))mNPV、斜紋夜蛾(Spodoptera littoralis)(非洲棉花葉蟲(African cotton leafworm))NPV。
亦包括者為細菌及真菌,其係「接種」至植物或植物部份或植物器官且其,憑藉其特殊的性質,促進植物生長及植物健康。實例包括:土壤桿菌屬(Agrobacterium spp.)、莖瘤固氮根瘤菌(Azorhizobium caulinodans)、固氮螺菌屬(Azospirillum spp.)、固氮菌屬(Azotobacter spp.),慢生根瘤菌屬(Bradyrhizobium spp.),伯克氏菌屬(Burkholderia spp.),尤其是洋蔥伯克氏菌(Burkholderia cepacia)(以前稱為洋蔥假單胞菌(Pseudomonas cepacia))、瘤壁孢菌屬(Gigaspora spp.)、或大單孢子(Gigaspora monosporum)、球囊菌屬(Glomus spp.)、蠟蘑菌屬(Laccaria spp.)、布氏乳酸桿菌(Lactobacillus buchneri)、對球囊菌屬(Paraglomus spp.)、彩色豆馬勃(Pisolithus tinctorus)、假單孢菌屬(Pseudomonas spp.)、根瘤菌屬(Rhizobium spp.),尤其是三葉草根瘤菌(Rhizobium trifolii)、根鬚腹菌屬(Rhizopogon spp.)、硬皮馬勃屬(Scleroderma spp.)、黏蓋菌屬(Suillus spp.)、鏈黴菌屬(Streptomyces spp.)。
植物萃出物及由微生物所形成之產物的實例,包括蛋白質及次級代謝產物,其係用作為或可用作為生物性殺害蟲劑:
蒜(Allium sativum)、艾蒿苦艾(Artemisia absinthium)、印楝素(azadirachtin)、Biokeeper WP,黑醋栗(Cassia nigricans)、苦皮藤(Celastrus angulatus)、臭杏(Chenopodium anthelminticum)、甲殼素(chitin)、Armour-Zen、綿馬(Dryopteris filix-mas)、問荊草(Equisetum arvense)、Fortune Aza、Fungastop、Heads Up(藜屬藜皂素萃出物)、除蟲菊/除蟲菊酯(pyrethrum/pyrethrins)、蘇林南苦木(Quassia amara)、櫟木(Quercus)、皂樹(Quillaja)、雷佳裡(Regalia)、「Requiem TM殺蟲劑」、魚藤酮(rotenone)、ryania/蘭尼鹼、紫花苜蓿(Symphytum officinale)、菊蒿屬大麥(Tanacetum vulgare)、麝香草酚(thymol)、Triact 70、TriCon、旱金蓮(Tropaeulum majus)、大蕁麻(Urtica dioica)、嚏根草鹼(Veratrin)、槲寄生(Viscum album)、十字花科(Brassicaceae)萃出物、尤其是油菜粉末或芥末粉末。
式(I)化合物可與安全劑合併,例如解草酮(benoxacor)、喹氧(-草酯)(cloquintocet(-mexyl))、解草胺腈(cyometrinil)、環丙磺醯胺(cyprosulfamide)、二氯丙烯胺(dichlormid)、解草唑(-乙基)(fenchlorazole(-ethyl))、解草啶(fenclorim)、解草胺(flurazole)、氟草肟(fluxofenim)、解草唑(furilazole)、雙苯唑酸(-乙基)(isoxadifen(-ethyl))、吡唑解(-二乙基)(mefenpyr (-diethyl))、萘酸酐、解草腈(oxabetrinil)、2-甲氧基-N-({4-[(甲基胺基甲醯基)胺基]苯基}磺醯基)苯醯胺(CAS 129531-12-0)、4-(二氯乙醯)-1--4-氮雜螺[4.5]癸烷(CAS 71526-07-3)、2,2,5-三甲基-3-(二氯乙醯)-1,3-唑烷(CAS 52836-31-4)。
應瞭解於本文中植物意指所有植物及植物群,如想要及不想要的野生
植物或作物植物(包括天然生成的作物植物),例如穀類(小麥、稻、小黑麥、大麥、裸麥、燕麥)、玉蜀黍、黃豆、馬鈴薯、糖用甜菜、甘蔗、蕃茄、燈籠椒、黃瓜、瓜、胡蘿蔔、西瓜、洋蔥、萵苣、菠菜、韭菜、豆類、甘藍(如捲心菜)及其他蔬菜種類、棉花、菸草、油菜、以及果實植物(為蘋果、梨子、柑橘類及葡萄果實)。作物植物可為可藉由傳統選育及最優化方法或藉由生物技術及基因工程方法或這些方法合併而得到之植物,其包括轉基因植物且包括被植物育種者權利所保護及未保護之植物栽培種。應瞭解植物意指所有的發展階段,如種子,幼苗,年輕(不成熟)植物,直至並包括成熟植物。應瞭解植物部份意指所有植物地上和地下之部份及器官,如芽、葉、花及根,實例為葉、針葉、稈、莖、花、果實體、果實及種子,以及塊莖、根及根莖。植物部份亦包括收穫之植物或收穫之植物部份及無性及生殖繁殖物質,例如扡插、塊莖、根莖、插枝及種子。
根據本發明用式(I)化合物來處理植物及植物部份係直接進行或藉由將該化合物以習用處理方法作用於其等之環境區,棲息地或其儲存區域,例如以浸漬、噴灑、蒸發、霧化、散佈、塗佈、注射、及,於繁殖物質之情況,尤其是於種子之情況時,亦藉由施用一個或多個塗敷。
如上提及,其可根據本發明處理所有植物及其部份。於較佳具體例中,係處理野生植物品種及植物栽培種,或那些藉由傳統生物育種法,如雜交或原生質體融合,及其部份而得到者。於其他較佳具體例中,係處理藉由基因工程的方法得到之轉基因植物及植物栽培種,如果適當係與傳統方法合併(轉基因生物),及其部份。「部份」或「植物的部份」或「植物部份」之詞已說明如上。特佳者為根據本發明處理之各別市售栽培種之植物或那些正在使用者。應瞭解植物栽培種意指植物,其具有新特性(「特徵」)且其係藉由傳統育種,藉由突變或藉由重組DNA技術得到者。其等可為栽培種,變種,生物型或基因型。
即將根據本發明處理之較佳的轉基因植物或植物栽培種(其等係藉由基因工程得到)包括所有,經由基因改造,接受賦予特別有利的有用特性(「特徵」)到這些植物之基因物質的植物。此等特性之實例為植物生長較佳,對高溫或低溫的耐受性提高,對乾旱或對水含量或土壤鹽分含量之耐受性提高,開花表現提高,較易收成,加速熟成,收成產量較高,收穫產物之品質較高及/或營養價值較高,收穫產品之儲存期較長及/或加工性較佳。此等特性之其他及特別強調的實例為提高植物對抗動物及微生物害蟲,如對抗昆蟲,蜘蛛,線蟲,蟎蟲,蛞蝓和蝸牛,例如,由於在植物中形成之毒性,特別是那些於植物中由蘇雲金芽孢桿菌所產生之基因物質(例如藉由基因CryIA(a)、CryIA(b)、CryIA(c)、CryIIA、CryIIIA、CryIIIB2、Cry9c、Cry2Ab、Cry3Bb及CryIF以及其組合),而亦提高植物對抗植物病原性真菌,細菌及/或病毒之抗性,其係,例如,藉由系統性所需之抗性(SAR),系統蛋白,植物防禦素,激發子及抗性基因及相對應表現蛋白質及毒性造成,以及提高植物對於特定除草活性化合物,例如咪唑啉酮,磺醯脲,甘磷散或膦基三辛(例如「PAT」基因)之耐受性。所討論之傳授想要特性(「特徵」)的基因亦可於基因轉殖植物相互合併而發生。轉基因植物實例包括重要作物植物,如穀類(小麥、稻、小黑麥、大麥、裸麥、燕麥)、玉蜀黍、黃豆、馬鈴薯、糖用甜菜、甘蔗、蕃茄、豌豆及其他型式之蔬菜、棉花、菸草、油菜以及果實植物(為蘋果、梨子、柑橘類及葡萄果實),特別強調的是玉蜀黍、黃豆、小麥、稻、馬鈴薯、棉花、甘蔗、菸草及油菜。特別強調的特性(「特徵」)為提高植物對於昆蟲、蜘蛛、線蟲及蛞蝓和蝸牛的抗性。
用式(I)化合物處理植物及植物部份係直接作用或藉由作用於其等之環境區,棲息地或儲存區域,其係藉由習用處理方法,例如藉由浸漬、噴灑、噴霧、灌水、蒸發、噴粉、霧化、散播、起泡、塗佈、蔓延、注射、灑水(淋灑)、滴灌水及,於繁殖物質之情況時,特別是於種子之情況時,進一步藉由乾燥種子處理,液體種子處理,泥漿處理,藉由覆皮,藉由包埋以一層或多層等。其進一步可藉由超低體積方法施用式(I)化合物,或將使用型式或式(I)化合物本身注射至土壤中。
較佳之直接植物處理為葉面施用,亦即式(I)化合物係施用至葉面,於此情況下,處理頻率及施用率應根據被問題蟲害感染之程度來調整。
於系統活性化合物之情況時,式(I)化合物亦係經由根系進入植物。然後將植物藉由將式(I)化合物作用於植物之棲息地而處理。此之完成係,例如,藉由淋灑,或藉由摻合至土壤或營養液,意指該植物之基底(如土壤或水培系統)係用液體型式之式(I)化合物來浸漬,或藉由土壤施用,意指將本發明之式(I)化合物以固體型式(如以顆粒型式)引至該植物之基底。於水稻作物之情況時,此亦可藉由將式(I)化合物以固體施用型式(例如呈顆粒)計量加至水淹之稻田而完成。
藉由處理植物種子而控制動物蟲害早已知曉且為不斷改善的主題。然而,處理種子造成一系列始終不能以令人滿意之方式解決的問題。因此,最好能開發方法來保護種子及發芽植物,以免除,或至少能大大減少,於儲存期間,播種後或植物發芽後額外施用殺蟲劑。另外亦想要優化所使用之活性組成份的量,以便對於種子及發芽植物提供最優保護而免受動物蟲害攻擊,但所使用之活性組成份不會傷害植物本身。特別的,處理種子之方法亦需考慮到抗蟲害或對蟲害耐受之轉基因植物原本之殺昆蟲或殺線蟲
特性,以便用最小殺害蟲劑的開銷達到對於種子及發芽植物之最優保護。
本發明因此亦特別關於,將種子用式(I)化合物之一處理以保護種子及發芽植物免於蟲害攻擊之方法。本發明因此亦特別關於,將種子用式(I)化合物之一處理以保護種子及發芽植物免於蟲害攻擊之方法,其中,該種子係同時於一個操作中或順序的用式(I)化合物及一摻合之組份處理。其亦包括一方法,其中,該種子係於不同時間用式(I)化合物及一摻合之組份處理。
本發明同樣係關於式(I)化合物於處理種子以保護種子及所長成之植物免於動物蟲害之用途。
本發明進一步係關於種子,其係用本發明之式(I)化合物處理以保護而免於動物蟲害。本發明亦關於種子,其係同時用式(I)化合物及摻合之組份處理。本發明進一步係關於種子,其係於不同時間用式(I)化合物及摻合之組份處理。於種子之情況時,其係於不同時間用式(I)化合物及摻合之組份處理,該個別物質可存在於種子之不同層中。於此情況時,該包括式(I)化合物及摻合之組份的各層可任意藉由中間層來分離。本發明亦關於種子,其中,式(I)化合物及摻合之組份係以作為塗層之部份來施用或作為另一層或除了一塗層外之其他層。
本發明進一步係關於種子,其,於用式(I)化合物處理後,係進行薄膜塗敷過程以防止於種子之灰塵磨耗。
式(I)化合物之系統性作用的有利優點之一為,不僅保護種子本身亦保護由其長成之植物,使其於出苗後,可免於動物蟲害。依此方式,可以省略於播種之時立即或不久後處理作物。
進一步之優點是用式(I)化合物處理種子,可促進經處理種子之發芽和出苗。
同樣的,式(I)合物尤其是用於轉基因種子亦被認為是有利的。
再者,式(I)化合物可與信號技術組成物合併使用,其可藉由共生而產
生較佳之克隆化,例如,根瘤菌(rhizobia),菌根(mycorrhizae)及/或內生細菌或真菌,及/或最優化之氮固定。
式(I)化合物適用於保護任何植物品種之種子,其係用於農業,於溫室,於森林或於園藝。更特別的,這包括穀物之種子(例如小麥、大麥、裸麥、粟及燕麥)、玉蜀黍、棉花、黃豆、稻、馬鈴薯、向日葵、咖啡、菸草、油菜花、油菜、甜菜(例如糖用甜菜及飼料甜菜)、花生、蔬菜(例如蕃茄、黃瓜、大豆、十字花科蔬菜、洋蔥及萵苣)、果實植物、草坪及觀賞植物。特別重要的是處理穀物種子(如小麥、大麥、裸麥及燕麥)、玉蜀黍、玉米、黃豆、棉花、油菜籽、油菜、蔬菜及稻子。
如上所提及,用式(I)化合物處理轉基因種子亦屬特別重要。這涉及到植物種子,其通常含有至少一種特別是控制具有殺昆蟲及/或殺線蟲特性之聚肽表現的異源性基因。該於轉基因種子之異源性基因可源自微生物,如芽孢桿菌(Bacillus)、根瘤菌(Rhizobium)、假單胞菌(Pseudomonas)、沙雷氏菌(Serratia)、木黴菌(Trichoderma)、環腐菌(Clavibacter)、球囊黴菌(Glomus)或黏地黴菌(Gliocladium)。本發明特別適用來處理含有至少一種源自異源性基因芽孢桿菌之轉基因種子。該異源性基因更宜為源自蘇雲金芽孢桿菌(Bacillus thuringiensis)。
於本發明內文中,式(I)化合物係施用至種子。該種子宜在其中,係足夠穩定使在處理過程中沒有損傷之狀態中處理。通常,該種子係於收成及播種期間任何時間處理。通常使用之種子係已由植物分離出來並去掉穗軸,殼,秸稈,外殼,毛或果實之果肉。例如,其可使用業經收穫,清潔並乾燥至可允許儲存之水分含量之種子。或者,其亦可使用於乾燥後用,例如,水處理且然後,例如藉由倒掉而再次乾燥之種子。於稻米種子之情況時,其亦可使用已經浸泡在例如水中直至其達到水稻胚胎(「雞胸階段(pigeon breast stag)」)之某一階段的種子,此導致對萌芽的刺激及更均勻的出芽。
通常,於處理種子時,必須確保施用至種子之式(I)化合物及/或其他添加物之量係經選擇使得種子之發芽不受損且由其所長成之植物也不損壞。這個於某些施用率時表現出植物毒性作用之活性組成份的情況時特別必須確保。
通常,式(I)化合物係以適當的製劑施用至種子。適當的製劑及處理種子方法係精於此方面技藝者所已知。
式(I)化合物可轉換為習用種子敷料製劑,如溶液、乳液、懸浮液、粉末、泡沫、漿液或其他種子之塗敷組成物,以及ULV製劑。
這些製劑係依已知方式來製造,藉由將式(I)化合物與習用添加劑,例如習用擴充劑以及溶劑或稀釋劑、染料、潤濕劑、分散劑、乳化劑、消泡劑、防腐劑、第二增稠劑、粘合劑、赤黴素以及水摻合。
可存在於種子敷料製劑中可根據本發明使用之染料為所有習用於此目的之染料。其亦可使用任一微溶於水之顏料,或溶於水之染料。實例包括已知名稱為Rhodamine B、C.I.Pigment Red 112及C.I.溶劑Red 1的染料。
可出現於根據本發明使用之種子敷料製劑中之有用潤濕劑為所有可促進潤濕之物質且其係傳統上使用於活性農化組成份製劑。較佳為使用烷基萘磺酸鹽,如二異丙基或二異丁基萘磺酸鹽。
可根據本發明使用之可存在於種子敷料製劑中之適當的分散劑及/或乳化劑為所有傳統上用於製劑之活性農化組成份之非離子性,陰離子性及陽離子性分散劑。較佳為使用非離子性或陰離子性分散劑或非離子性或陰離子性分散劑之混合物。適當的非離子性分散劑尤其是包括環氧乙烷/環氧丙烷阻斷聚合物,烷基苯酚聚乙二醇醚類及三苯乙烯苯酚聚乙二醇醚類,及其磷酸化或硫酸化衍生物。適當的陰離子性分散劑尤其是木質素磺酸鹽,聚丙烯酸鹽及芳基磺酸鹽-甲醛縮合物。
可根據本發明使用之可存在於種子敷料製劑中之消泡劑為所有傳統上
用於製劑之活性農化組成份之泡沫抑制物質。較佳為使用矽膠消泡劑及硬脂酸鎂。
可根據本發明使用之可存在於種子敷料製劑中之防腐劑為所有為此目的使用於農化組成物之物質。實例包括二氯吩及苯甲醇半縮甲醛。
可根據本發明使用之可存在於種子敷料製劑中之第二增稠劑為所有為此目的使用於農化組成物之物質。較佳之實例包括纖維素衍生物,丙烯酸衍生物,黃原膠,改性粘土及細碎的二氧化矽。
可根據本發明使用之可存在於種子敷料製劑中之粘合劑為所有有用於種子敷料產物之習用粘合劑。較佳之實例包括聚乙烯基吡咯烷酮,聚乙烯基醋酸酯,聚乙烯醇及纖基乙酸鈉。
可根據本發明使用之可存在於種子敷料製劑中之赤黴素宜為赤黴素A1,A3(=赤黴酸),A4及A7;特別佳為使用赤黴酸。該赤黴素為已知(參見R.Wegler「Chemie der Pflanzenschutz- and Schädlingsbekämpfungsmittel」,vol.2,Springer Verlag,1970,pp.401-412)。
可根據本發明使用之種子敷料製劑可用來處理不同種子之野生品種,無論是直接於用水稀釋之前或之後。例如,該濃縮物或可由其等藉由用水稀釋可得之製劑可用來塗敷穀物,如小麥、大麥、裸麥、燕麥、及小黑麥之種子,以及玉蜀黍、稻、油菜、豌豆、豆子、棉花、向日葵、黃豆及甜菜之種子,或不同蔬菜種子之野生品種。可根據本發明使用之種子敷料製劑,或其稀釋使用型式,亦可用來塗敷轉基因植物之種子。
以可根據本發明使用之種子敷料製劑來處理種子,或由其等藉由添加水所製成之使用型式,所有可習慣的使用於種子敷料之摻合單元係有用的。特別的,種子敷料之過程係將種子逐批或於連續操作而置入摻合器中,加入特別想要量之種子敷料製劑,無論是如此或是先用水稀釋後,並摻合直到該製劑均勻的分佈在種子上。如果適當,接著進行乾燥過程。
可根據本發明使用之種子敷料製劑的施用率可在一相當大的範圍內變化。其係由製劑中式(I)化合物的特別含量及由種子來引導。每公斤種子,式(I)化合物的施用率通常係介於0.001及50g,宜為每公斤種子介於0.01及15g。
於動物健康區塊上,亦即在獸藥領域上,式(I)化合物係對於動物寄生蟲具有活性,特別是體外寄生蟲或體內寄生蟲。「體內寄生蟲」之詞尤其是包括蠕蟲及原生動物,如球蟲。體外寄生蟲典型的且宜為節肢動物,尤其是昆蟲或蟎蟲。
在獸藥領域內,該具備有利溫血動物毒性之式(I)化合物適用於控制在畜牧業之動物選育及動物養殖,選育動物,動物園動物,實驗室動物,實驗動物及家養動物時出現的寄生蟲。其等對於對抗寄生蟲發育之所有或特定階段具有活性。
農畜包括,例如,哺乳類,如羊、山羊、馬、驢、駱駝、水牛、兔子、馴鹿、小鹿且尤其是黃牛及豬;或家禽如火雞、鴨、鵝且尤其是雞;或魚或甲殼類動物,例如於水產養殖;或,視情況可以,昆蟲如蜜蜂。
家養動物包括,例如,哺乳類,如倉鼠、豚鼠、大鼠、小鼠、龍貓、雪貂、且特別為狗、貓、圏養的鳥、爬蟲類、兩棲類或觀賞魚。
於特別具體例中,式(I)化合物係給藥至哺乳類。
於其他特別具體例中,式(I)化合物係給藥至鳥類,即圏養的鳥或特別為家禽。
式(I)化合物於控制動物寄生蟲之用途係為了減少或預防疾病,死亡病例及產能降低(於肉、奶、毛、皮、蛋、蜜等之情況時),使得更經濟且動物飼養更簡單且可以實現更好的動物安康。
關於動物健康方面,「控制」或「可控制」之詞意指式(I)化合物可有效的將特定寄生蟲於感染該寄生蟲之動物身上之發病率降低至無害的程度。更具體言,於本發明內文中,「控制」意指式(I)化合物可殺死各別的寄生蟲,抑制其生長,或抑制其繁殖。
節肢動物包括,例如,但非侷限於,虱目(Anoplurida),例如,盲虱(Haematopinus spp.)、長顎虱(Linognathus spp.)、虱(Pediculus spp.)、陰虱(Phthirus spp.)及管虱(Solenopotes spp.);食毛目(Mallophagida)及鈍角亞目(Amblycerina)及細角亞目(Ischnocerina),例如,牛羽虱(Bovicola spp.)、畜虱(Damalina spp.)、貓羽虱(Felicola spp.);盤羊羽虱(Lepikentron spp.)、短角鳥虱(Menopon spp.)、嚼毛虱(Trichodectes spp.)、毛鳥虱(Trimenopon spp.)、鵝巨毛虱(Trinoton spp.)、馬羽虱(Werneckiella spp.);雙翅目(Diptera)及長角亞目(Nematocerina)及短角亞目(Brachycerina),例如,伊蚊(Aedes spp.)、瘧蚊(Anopheles spp.)、黃虻(Atylotus spp.)、蜂蠅(Braula spp.)、麗蠅(Calliphora spp.)、金蠅(Chrysomyia spp.)、草螟(Chrysops spp.)、庫蚊(Culex spp.)、庫蠓(Culicoides spp.)、真蚋(Eusimulium spp.)、廁蠅(Fannia spp.)、胃蠅(Gasterophilus spp.)、采采蠅(Glossina spp.)、血蠅(Haematobia spp.)、麻虻(Haematopota spp.)、虱蠅(Hippobosca spp.)、瘤虻(Hybomitra spp.)、齒股蠅(Hydrotaea spp.)、皮蠅(Hypoderma spp.)、鹿虱蠅(Lipoptena spp.)、綠蠅(Lucilia spp.)、沙蠅(Lutzomyia spp.)、蜱蠅(Melophagus spp.)、莫蠅(Morellia spp.)、家蠅(Musca spp.)、短蚋(Odagmia spp.)、狂蠅(Oestrus spp.)、蠅(Philipomyia spp.)、白蛉(Phlebotomus spp.)、鼻狂蠅(Rhinoestrus spp.)、肉蠅(Sarcophaga spp.)、水牛蚋(Simulium spp.)、螫蠅(Stomoxys spp.)、牛虻
(Tabanus spp.)。大蚊(Tipula spp.)、維蚋(Wilhelmia spp.)、汙蠅(Wohlfahrtia spp.);蚤目(Siphonapterida),例如,毛列蚤(Ceratophyllus spp.)、櫛頭蚤(Ctenocephalides spp.)、跳蚤(Pulex spp.)、潛蚤(Tunga spp.)、鼠蚤(Xenopsylla spp.);異翅亞目(Heteropterida),例如,葉蜂(Cimex spp.)、金圓錐椿(Panstrongylus spp.)、臭蟲(Rhodnius spp.)、吸血獵椿(Triatoma spp.);以及來自蜚蠊目(Blattarida)之討厭和衛生蟲害。
此外,於節肢動物之情況時,應當藉由實例提及但不限於以下蜱蟎:蜱蟎亞綱(Acari)(蜱蟎亞綱(Acarina))及後氣門亞目(Metastigmata),例如軟蜱科(Argasidae)如隱喙蜱(Argas spp.)、鈍喙蜱(Ornithodorus spp.)、喙蜱(Otobius spp.)、硬蜱科(Ixodidae)如花蜱(Amblyomma spp.)、革蜱(Dermacentor spp.)、血蜱(Haemaphysalis spp.)、眼蜱(Hyalomma spp.)、硬蜱(Ixodes spp.)、扇頭蜱(Rhipicephalus spp.(消色牛蜱(Boophilus))、扇頭蜱(Rhipicephalus spp.(原始多宿主蜱屬));中氣門蟎目(Mesostigmata)如皮刺蟎(Dermanyssus spp.)、禽刺蟎(Ornithonyssus spp.)、肺刺蟎(Pneumonyssus spp.)、耳恙蟲(Raillietia spp.)、氣囊蟎(Sternostoma spp.)、熱厲蟎(Tropilaelaps spp.)、瓦蟎(Varroa spp.);輻蟎亞目(Actinedida)(前氣門亞目(Prostigmata)),例如,氣管蟎(Acarapis spp.)、姬螯蟎(Cheyletiella spp.)、蠕形蟎(Demodex spp.)、持鏟蟎(Listrophorus spp.)、鼷鼠跳蟎(Myobia spp.)、紐楚必克蟲(Neotrombicula spp.)、蟎(Ornithocheyletia spp.)、瘡蟎(Psorergates spp.),恙蟎(Trombicula spp.);及粉蟎亞目(Acaridida)(無氣門亞目(Astigmata)),例如,毛囊蟲(Acarus spp.)、木嗜蟎(Caloglyphus spp.)、足蟎(Chorioptes spp.)、蜱蟎(Cytodites spp.)、皮頸下蟎
(Hypodectes spp.)、鱗疥蟎(Knemidocoptes spp.)、雞雛蟎(Laminosioptes spp.)、節蟎(Notoedres spp.)、耳蟎(Otodectes spp.)、癢蟎(Psoroptes spp.)、翼蟎(Pterolichus spp.)、疥蟎(Sarcoptes spp.)、粗腳粉蟎(Trixacarus spp.)、酪食蟎(Tyrophagus spp.)。
寄生原生動物之實例包括,但非侷限於:鞭毛綱(Mastigophora)(鞭毛蟲綱(Flagellata)),如:
後滴門(Metamonada):雙滴蟲目(Diplomonadida),例如梨形鞭毛蟲(Giardia spp.)、旋核六鞭毛蟲(Spironucleus spp.)。
副基體綱(Parabasala):毛滴蟲目(Trichomonadida),例如組織滴蟲(Histomonas spp.)、人五毛滴蟲(Pentatrichomonas spp.)、巴氏四毛滴蟲(Tetratrichomonas spp.)、腸道鞭毛滴蟲(Trichomonas spp.)、三腸道鞭毛滴蟲(Tritrichomonas spp.)。
眼蟲門(Euglenozoa):錐體蟲目(Trypanosomatida),例如利什曼原蟲(Leishmania spp.)、瘧原蟲(Trypanosoma spp.)。
肉鞭蟲(Sarcomastigophora)(根足蟲(Rhizopoda))如內阿米巴蟲(Entamoebidae),例如內阿米巴蟲(Entamoeba spp.)、中蟲科(Centramoebidae),例如棘阿米巴原蟲(Acanthamoeba sp.)、裸阿米巴原蟲(Euamoebidae),如哈曼拉蟲(Hartmanella spp.)。
囊泡蟲(Alveolata)如頂複合器門(Apicomplexa)(孢子蟲綱(Sporozoa)):如隱孢子蟲(Cryptosporidium spp.);艾美球蟲目(Eimeriida),例如,貝斯諾孢子
蟲(Besnoitia spp.)、等孢子蟲(Cystoisospora spp.)、艾美球蟲(Eimeria spp.)、哈蒙球蟲(Hammondia spp.)、等孢球蟲(Isospora spp.)、新孢子蟲(Neospora spp.)、肉孢子蟲(Sarcocystis spp.)、弓形蟲(Toxoplasma spp.);阿黛爾球蟲目(Adeleida),例如,肝簇蟲(Hepatozoon spp.)、克雷伯氏蟲(Klossiella spp.);血孢子蟲目(Haemosporida),例如,白細胞原蟲(Leucocytozoon spp.)、瘧原蟲(Plasmodium spp.);漿漿蟲目(Piroplasmida),例如,巴貝斯蟲(Babesia spp.)、纖毛蟲(Ciliophora spp.)、奇汝蟲(Echinozoon spp.)、泰勒蟲(Theileria spp.);威並菲蟲目(Vesibuliferida),例如,大腸纖毛蟲(Balantidium spp.)、波斯通貝蟲(Buxtonella spp.)。
微孢子蟲(Microspora)如腦孢子蟲(Encephalitozoon spp.)、腸球菌(Enterocytozoon spp.)、球形蟲(Globidium spp.)、豬鼻蟲(Nosema spp.),以及,例如,黏體蟲(Myxozoa spp.)。
人類或動物致病性之蠕蟲包括,例如,棘頭蟲(Acanthocephala)、線蟲(Nematoden)、蛇形蟲(Pentastoma)及扁形動物(Platyhelminthes)(如單殖吸蟲(Monogenea)、縧蟲(cestodes)及吸蟲(trematodes))。
闡釋之蠕蟲包括,但非侷限於:
單殖吸蟲(Monogenea):例如:指環蟲(Dactylogyrus spp.)、三代蟲(Gyrodactylus spp.)、小盤吸蟲(Microbothrium spp.)、多盤吸蟲(Polystoma spp.)、楚發蟲(Troglecephalus spp.);
縧蟲(Cestodes):假葉目(Pseudophyllidea),例如:槽頭蟲(Bothridium spp.)、裂頭蟲(Diphyllobothrium spp.)、複殖孔縧蟲(Diplogonoporus spp.)、艾呦蟲(Ichthyobothrium spp.)、舌狀縧蟲(Ligula spp.)、頭裂畸胎蟲(Schistocephalus spp.)、疊宮縧蟲(Spirometra spp.)。
圓葉目(Cyclophyllida),例如:安得拉縧蟲(Andyra spp.)、裸頭縧蟲(Anoplocephala spp.)、無卵黃腺縧蟲(Avitellina spp.)、伯特縧蟲(Bertiella spp.)、裸頭縧蟲(Cittotaenia spp.)、代凡縧蟲(Davainea spp.)、雙睪縧蟲(Diorchis spp.)、複殖器縧蟲(Diplopylidium spp.)、複孔縧蟲(Dipylidium spp.)、棘球縧蟲(Echinococcus spp.)、棘球縧蟲(Echinocotyle spp.)、瘍棘殼絳蟲(Echinolepis spp.)、泡尾縧蟲(Hydatigera spp.)、膜殼縧蟲(Hymenolepis spp.)、喬伊縧蟲(Joyeuxiella spp.)、中殖孔縧蟲(Mesocestoides spp.)、莫尼茨縧蟲(Moniezia spp.)、副裸頭絳蟲(Paranoplocephala spp.)、瑞裂縧蟲(Raillietina spp.)、斯泰勒縧蟲(Stilesia spp.)、牛帶縧蟲(Taenia spp.)、裸頭科曲子宮(Thysaniezia spp.)、遂體蟲(Thysanosoma spp.)。
吸蟲(Trematodes):複殖綱(Digenea),例如:澳血吸蟲(Austrobilharzia spp.)、短咽吸蟲(Brachylaima spp.)、杯殖吸蟲(Calicophoron spp.)、下彎吸蟲(Catatropis spp.)、肝吸蟲(Clonorchis spp.)、表孔吸蟲(Collyriclum spp.)、殖盤吸蟲(Cotylophoron spp.)、環腔吸蟲(Cyclocoelum spp.)、雙腔吸蟲(Dicrocoelium spp.)、雙層層孔蟲(Diplostomum spp.)、棘隙吸蟲(Echinochasmus spp.)、棘緣吸蟲(Echinoparyphium spp.)、棘口吸蟲(Echinostoma spp.)、闊盤吸蟲(Eurytrema spp.)、片形吸蟲(Fasciola spp.)、擬片形吸蟲(Fasciolides spp.)、薑片吸蟲(Fasciolopsis spp.)、菲策吸蟲(Fischoederius spp.)、食羊胃吸蟲(Gastrothylacus spp.)、巨畢吸蟲(Gigantobilharzia spp.)、巨盤吸蟲(Gigantocotyle spp.)、異形吸蟲(Heterophyes spp.)、低頸吸蟲(Hypoderaeum spp.)、彩蚴吸蟲(Leucochloridium spp.)、後殖吸蟲(Metagonimus spp.)、次睪吸蟲(Metorchis spp.)、短身吸蟲(Nanophyetus spp.)、背孔吸蟲(Notocotylus spp.)、後睪吸蟲(Opisthorchis spp.)、鳥畢吸蟲
(Ornithobilharzia spp.)、並殖吸蟲(Paragonimus spp.)、同盤吸蟲(Paramphistomum spp.)、斜睪吸蟲(P1agiorchis spp.)、雙穴吸蟲(Posthodiplostomum spp.)、前殖吸蟲(Prosthogonimus spp.)、血吸蟲(Schistosoma spp.)、毛畢吸蟲(Trichobilharzia spp.)、隱孔吸蟲(Troglotrema spp.)、盲腸吸蟲(Typhlocoelum spp.)。
線蟲(Nematodes):毛形亞目(Trichinellida),例如:毛細線蟲(Capillaria spp.)、旋毛蟲(Trichinella spp.)、似毛體線蟲(Trichomosoides spp.)、毛首線蟲(Trichuris spp.)。
墊刃線蟲(Tylenchida),例如:微線線蟲(Micronema spp.)、擬糞桿線蟲(Parastrangyloides spp.)、小桿線蟲(Strongyloides spp.)。
小桿亞綱(Rhabditida),例如:貓圓線蟲(Aelurostrongylus spp.)、裂口線蟲(Amidostomum spp.)、鉤蟲(Ancylostoma spp.)、管圓線蟲(Angiostrongylus spp.)、波久蟲(Bronchonema spp.)、仰口線蟲(Bunostomum spp.)、線蟲(Chabertia spp.)、古柏線蟲(Cooperia spp.)、可皮芮蟲(Cooperioides spp.)、齒體線蟲(Crenosoma spp.)、盅口線蟲(Cyathostomum spp.)、環可瑟蟲(Cyclococercus spp.)、環齒口鉤蟲(Cyclodontostomum spp.)、環線蟲(Cylicocyclus spp)、杯冠線蟲(Cylicostephanus spp.)、柱咽蟲(Cylindropharynx spp.)、囊尾線蟲(Cystocaulus spp.)、綱尾線蟲(Dictyocaulus spp.)、馴鹿圓絲蟲(Elaphostrongylus spp.)、類絲蟲(Filaroides spp.)、球頭蟲(Globocephalus spp.)、格拉斯線蟲(Graphidium spp.)、盅口輻首蟲(Gyalocephalus spp.)、血矛線蟲(Haemonchus spp.)、多形螺旋線蟲(Heligmosomoides spp.)、賀絲狀蟲(Hyostrongylus spp.)、毛圓科馬線蟲(Marshallagia spp.)、後圓線蟲
(Metastrongylus spp.)、毛細線蟲(Muellerius spp.)、板口線蟲(Necator spp.)、細頸線蟲(Nematodirus spp.)、新原線蟲(Neostrongylus spp.、鼠鉤口線蟲(Nippostrongylus spp.)、毛圓科劍形蟲(Obeliscoides spp.)、食道齒蟲(Oesophagodontus spp.)、結節線蟲(Oesophagostomum spp.)、盤頭線蟲(Ollulanus spp.);圓蟲(Ornithostrongylus spp.)、奧斯勒絲蟲(Oslerus spp.)、奧斯特線蟲(Ostertagia spp.)、副古柏線蟲(Paracooperia spp.)、副齒體線蟲(Paracrenosoma spp.)、副類絲蟲(Parafilaroides spp.)、擬馬鹿圓線蟲(Parelaphostrongylus spp.)、卡氏肺尾線蟲(Pneumocaulus spp.)、肺原蟲(Pneumostrongylus spp.)、盆口蟲(Poteriostomum spp.)、原圓線蟲(Protostrongylus spp.)、史可客蟲(Spicocaulus spp.)、冠線蟲(Stephanurus spp.)、圓線蟲(Strongylus spp.)、比翼線蟲(Syngamus spp.)、背板線蟲(Teladorsagia spp.)、背板線蟲(Teladorsagia spp.)、毛圓線蟲(Trichostrongylus spp.)、三齒線蟲(Triodontophorus spp.)、灰桿線蟲(Troglostrongylus spp.)、鈎蟲(Uncinaria spp.)。
旋尾目(Spirurida),例如:棘唇線蟲(Acanthocheilonema spp.)、單線蟲(Anisakis spp.)、禽蛔蟲(Ascaridia spp.);蛔蟲(Ascaris spp.)、胃蟲(Ascarops spp.)、無刺線蟲(Aspiculuris spp.)、蛔蟲(Baylisascaris spp.)、布氏絲蟲(Brugia spp.)、喜皮拉蟲(Cercopithifilaria spp.)、毛體蟲(Crassicauda spp.)、唇棘線蟲(Dipetalonema spp.)、惡絲蟲(Dirofilaria spp.)、龍絲蟲(Dracunculus spp.)、龍線蟲(Draschia spp.)、蟯蟲(Enterobius spp.)、絲蟲(Filaria spp.)、顎口線蟲(Gnathostoma spp.)、筒線蟲(Gongylonema spp.)、柔線蟲(Habronema spp.)、盲腸蟲(Heterakis spp.);光絲蟲(Litomosoides spp.)、羅阿絲蟲(Loa spp.)、盤尾絲蟲(Onchocerca spp.)、蟯蟲(Oxyuris spp.)、付柔線蟲(Parabronema spp.)、副絲蟲(Parafilaria spp.)、副蛔蟲(Parascaris spp.)、尖尾科栓尾線蟲(Passalurus
spp.)、泡翼線蟲(Physaloptera spp.)、蟯蟲(Probstmayria spp.)、假絲蟲(Pseudofilaria spp.)、腹腔絲蟲(Setaria spp.)、(Skjrabinema spp.)、旋尾線蟲(Spirocerca spp.)、冠絲蟲(Stephanofilaria spp.)、絲股蟲(Strongyluris spp.)、管狀科管狀線蟲(Syphacia spp.)、吸吮線蟲(Thelazia spp.)、弓蛔線蟲(Toxascaris spp.)、弓蛔蟲(Toxocara spp.)、班氏線蟲(Wuchereria spp.)。
棘頭蟲綱(Acanthocephala):少棘目(Oligacanthorhynchida),例如:巨吻棘頭線蟲(Macracanthorhynchus spp.)、棘頭蟲前睪線蟲(Prosthenorchis spp.);念珠目(Moniliformida),例如:念珠棘蟲(Moniliformis spp.)。
多形目(Polymorphida),例如:尖刺細頸線蟲(Filicollis spp.);棘吻目(Echinorhynchida),例如棘頭線蟲(Acanthocephalus spp.)、棘吻線蟲(Echinorhynchus spp.)、利多海楚蟲(Leptorhynchoides spp.)。
舌形蟲(Pentastoma):舌狀蟲目(Porocephalida),例如,舌形蟲(Linguatula spp.)。
在獸醫領域及於動物照護上,式(I)化合物係藉由技藝通常已知之方法給藥,如以適當製劑型式經由腸,腸胃外,皮膚或經鼻途徑。給藥可為預防性,代謝性或治療性。
因此,本發明一個具體例係指式(I)化合物作為醫藥品之用途。
另一方面係關於式(I)化合物作為抗體內寄生蟲劑之用途。
本發明另一特定方面係關於式(I)化合物作為抗體內寄生蟲劑之用途,尤其是作為殺線蟲劑,殺扁形動物劑,殺棘頭蟲劑或殺舌形蟲劑之用途。
本發明另一特定方面係關於式(I)化合物作為抗原生動物劑之用途。
另一方面係關於式(I)化合物作為抗寄生蟲劑之用途,尤其是殺節肢動
物劑,特別是殺蟲劑或殺蟎劑。
本發明另一方面為包含有效量之至少一種式(I)化合物及至少一種下列者之獸醫用藥製劑:製藥上可接受的賦形劑(如固態或液態稀釋劑),製藥上可接受的輔助劑(如表面活性劑),尤其是製藥上可接受之習用於獸醫用藥製劑的賦形劑及/或製藥上可接受之習用於獸醫用藥製劑的輔助劑。
本發明一相關方面為製備本文中說明之獸醫用藥製劑的方法,其包括將至少一種式(I)化合物與製藥上可接受之賦形劑及/或輔助劑,尤其是與製藥上可接受之習用於獸醫用藥製劑的賦形劑及/或習用於獸醫用藥製劑的輔助劑摻合的步驟。
本發明其他特別方面為選自殺外寄生蟲和殺體內寄生蟲製劑之獸醫用藥製劑,尤其是選自驅蟲,抗原生動物及殺節肢動物製劑者,最特別為選自殺線蟲,殺扁形動物,殺棘頭蟲,殺舌形蟲,殺昆蟲及殺蟎蟲製劑,根據上述方面,及其製備方法。
其他方面係關於治療寄生蟲感染之方法,尤其是藉由選自本文提及之體外寄生蟲及體內寄生蟲之寄生蟲所引起的感染,其係藉由於動物中使用有效量之式(I)化合物,尤其是有需要之非人動物。
其他方面係關於治療寄生蟲感染之方法,尤其是藉由選自本文提及之體外寄生蟲及體內寄生蟲之寄生蟲所引起的感染,其係藉由使用如本文中於動物所定義之獸醫用藥製劑,尤其是有需要之非人動物。
其他方面係關於使用式(I)化合物來治療寄生蟲感染,尤其是藉由選自本文提及之體外寄生蟲及體內寄生蟲之寄生蟲,於動物,尤其是非人動物所引起的感染。
在動物健康或獸醫用藥之內文中,「治療」之詞係指預防性,代謝性及治療性處理。
於特別的具體例中,以此方式,含至少一種式(I)化合物與其他活性化
合物之混合物,尤其是含有內及外殺寄生蟲劑,係為獸醫用藥領域而提供。
於動物健康領域中,「混合物」非僅意指兩種(或多種)不同活性組成份,於一般製劑中配製並相應地一起使用,亦關於包含各別活性組成份之製劑的產物。因此,當使用多於兩種活性組成份時,所有的活性組成份於一般製劑中配製或所有的活性組成份可於各別之製劑中配製;同樣可以想到的混合形式為,其中一些活性組成份係一起配製而一些活性組成份係各別配製。各別之製劑允許分別或連續使用所討論的活性組成份。
於本文中以其等之「通用名稱」指明之活性化合物為已知且係說明於,例如,「Pesticide Manual」(參見上文)或可由網路中(e.g.:http://www.alanwood.net/pesticides)搜尋。
作為摻合組份之來自體外寄生蟲劑之說明性活性組成份,沒有任何將此構成限制之意圖,包括詳列於上之殺昆蟲劑及殺蟎蟲劑。其他有用之活性組成份係根據上述分類依照目前之IRAC Mode of Action Classification Scheme而列出:(1)乙醯膽鹼酯酶(AChE)抑制劑;(2)GABA-閘氯道阻斷劑;(3)鈉道調節劑;(4)菸鹼乙醯基膽鹼受體(nAChR)競爭調節劑;(5)菸鹼乙醯基膽鹼受體(nAChR)變構調節劑;(6)穀胺酸-閘氯道(GluCl)變構調節劑;(7)保幼激素模擬物;(8)多種非特異性(多位點)抑制劑;(9)弦音器調節劑;(10)蟎蟲生長抑制劑;(12)線粒體ATP合成酶抑制劑,如ATP干擾素;(13)經由質子梯度之破壞的氧化磷酸化之解偶合劑;(14)菸鹼乙醯膽鹼受體通道阻斷劑;(15)幾丁質生合成抑制劑,0型;(16)幾丁質生合成抑制劑,1型;(17)蛻皮抑制劑(尤其是於雙翅目);(18)蛻皮激素受體激動劑;(19)章魚胺受體激動劑;(21)線粒體絡合物I電子傳遞抑制劑;(25)線粒體絡合物II電子傳遞抑制劑;(20)線粒體絡合物III電子傳遞抑制劑;(22)電壓-依賴鈉道阻斷劑;(23)乙醯CoA羧基酶抑制劑;(28)尼丁受體調節劑;
具有未知或非特異性作用機制之活性組成份,如氟硝二苯胺(fentrifanil),嘧醯蟲胺(fenoxacrim),環戊烯(cycloprene),乙酯殺蟎醇(chlorobenzilate),殺蟲脒(chlordimeform),噻唑蟎(flubenzimin),地昔尼爾(dicyclanil),阿米多芬(amidoflumet),滅蟎猛(quinomethionat),苯蟎噻(triarathene),克噻並(clothiazoben),殺蟎好(tetrasul),油酸鉀,石油,惡蟲酮(metoxadiazone),古帕(gossyplur),氟非那嗪(flutenzine),溴蟎酯(brompropylate),冰晶石(cryolite);其他種類之化合物,例如畜蟲威(butacarb),敵蠅威(dimetilan),除線威(cloethocarb),磷蟲威(phosphocarb),嘧啶磷-乙基(pirimiphos-ethyl),對硫磷-乙基(parathion-ethyl),蟲蟎畏(methacrifos),(異丙基o-水楊酸酯),敵百蟲(trichlorfon),海羅松(sulprofos),丙蟲磷(propaphos),硫線磷(sebufos),巰氧吡啶鋅(pyridathion),發果(prothoate),除線磷(dichlofenthion),內吸磷-S-甲基碸(demeton-S-methyl sulfone),氯唑磷(isazofos),苯腈磷(cyanofenphos),氯亞胺硫磷(dialifos),三硫磷(carbophenothion),奧硫呋(autathiofos),芳紛呋-甲基(aromfenvinfos-methyl),乙基穀硫磷(azinphos-ethyl),毒死蜱-乙基(chlorpyrifos-ethyl),丁苯硫磷(fosmethilan),丙胺磷(iodofenphos),蔬果磷(dioxabenzofos),安果(formothion),地蟲磷(fonofos),吡氟硫磷(flupyrazofos),豐索磷(fensulfothion),乙嘧硫磷(etrimfos);有機氯化合物,例如毒殺芬(camphechlor),林丹(lindane),七氯(heptachlor);或苯基吡唑,如乙醯蟲腈(acetoprole),否氟撲(pyrafluprole),吡內咯(pyriprole),凡尼撲(vaniliprole),斯撲尼(sisapronil);或異唑烷,如殺羅尼(sarolaner),阿福拉納(afoxolaner),露來尼(lotilaner),服婪尼(fluralaner);
擬除蟲菊酯,如(順式-,反式-)美特寧(metofluthrin),撲扶寧(profluthrin),三氟醚菊酯(flufenprox),溴氟菊酯(flubrocythrinate),苄蟎醚(fubfenprox),芬氟司林(fenfluthrin),撲芬彬(protrifenbut),百滅寧(pyresmethrin),(RU15525),環戊烯丙菊酯(terallethrin),順式-苄呋菊酯(resmethrin),害扶辛(heptafluthrin),生物d-t-戊環苄呋菊酯(bioethanomethrin),生物氯菊酯(biopermethrin),氯吡氰菊酯(fenpyrithrin),順式-氯氰菊酯(cypermethrin),順式-百滅寧(permethrin),剋星(clocythrin),氯氟氰菊酯(λ-)(cyhalothrin(lambda-)),氯烯炔菊酯(chlovaporthrin),或鹵化之烴化合物(HCHs),新菸鹼類殺蟲劑(neonicotinoids),如噻嗪類(nithiazine);二克米汰(dicloromezotiaz),三氟苯嘧啶(triflumezopyrim);大環內酯類,如奈馬克丁(nemadectin),伊維菌素(ivermectin),拉替菌素(latidectin),摩西菌素(moxidectin),沙拉菌素(selamectin),埃普利諾菌素(eprinomectin),朵拉菌素(doramectin),甲胺基阿維菌素苯甲酸鹽(emamectin benzoate);米爾倍黴素肟(milbemycin oxime);烯蟲硫酯(triprene),保幼醚(epofenonane),二苯丙醚(diofenolan);生物製品,賀爾蒙或資訊素,例如天然產物,如蘇力菌素(thuringiensin),十二碳二烯醇(codlemone)或印楝組份;二硝基苯酚,如敵蟎普(dinocap),消蟎通(dinobuton),樂殺蟎(binapacryl);
苯甲醯脲,如氟佐隆(fluazuron),氟幼脲(penfluron),脒衍生物,如殺螟蟎(chlormebuform),甲基異丙苯基吡咯(cymiazole),二甲苯胺脒(demiditraz),蜂窩瓦蟎殺蟎蟲劑,例如有機酸,如甲酸,草酸。
作為摻合組份之來自體內寄生蟲劑之說明性活性組成份,包括但非侷限於,活性驅蟲組成份及活性抗原生動物組成份。
該活性驅蟲化合物包括但非侷限於下列活性殺線蟲,殺白蟻及/或殺細胞化合物:大環內酯類,例如:埃普利諾菌素(eprinomectin),阿維菌素(abamectin),奈馬克丁(nemadectin),摩西菌素(moxidectin),朵拉菌素(doramectin),沙拉菌素(selamectin),雷皮菌素(lepimectin),拉替菌素(latidectin),密滅汀(milbemectin),伊維菌素(ivermectin),艾瑪菌素(emamectin),米爾貝黴素(milbemycin);苯并咪唑及原苯并咪唑類,例如:丙氧苯唑(oxibendazole),甲苯咪唑(mebendazole),三氯苯咪唑(triclabendazole),托布津(thiophanate),氟苯達唑(parbendazole),奧吩達唑(oxfendazole),奈托比胺(netobimin),苯硫噠唑(fenbendazole),非班太(febantel),噻苯咪唑(thiabendazole),環苯達唑(cyclobendazole),堪苯達唑(cambendazole),阿苯達唑亞碸(albendazole sulfoxide),阿苯達唑(albendazole),氟苯達唑(flubendazole);縮肽類,宜為環縮肽類,尤其是24-員環縮肽類,例如:艾莫德斯(emodepside),PF1022A;
四氫嘧啶類,例如:噻烯氫嘧啶(morantel),抗蟲靈(pyrantel),酚嘧啶(oxantel);咪唑并噻唑類,例如:丁咪唑(butamisole),左旋咪唑(levamisole),驅蟲淨(tetramisole);胺基苯基脒類,例如:阿米登太(amidantel),脫醯基阿米替丁(deacylated amidantel)(dAMD),三苯雙脒(tribendimidine);胺基乙腈類,例如:莫內太爾碸(monepantel);副荷坤醯胺類(Paraherquamides),例如:副荷坤醯胺(paraherquamide),得曲恩特(derquantel);水楊酸苯胺類,例如:三溴水楊胺(tribromsalan),溴氟硝柳胺(bromoxanide),溴替尼特(brotianide),氯碘醯胺(clioxanide),氯氰碘柳胺(closantel),滅絲靈(niclosamide),羥氯水楊醯苯胺(oxyclozanide),碘醚柳胺(rafoxanide);經取代之苯酚類,例如:硝羥碘苄腈(nitroxynil),硫雙二氯酚(bithionol),二碘硝基酚(disophenol),六氯酚(hexachlorophen),聯硝氯酚(niclofolan),聯硝氯酚(meniclopholan);有機磷殺蟲劑類,例如:敵百蟲(trichlorfon),萘鹵福(naphthalofos),敵敵畏(dichlorvos)/DDVP,育畜磷(crufomate),蠅毒磷(coumaphos),皮蟲鱗
(haloxon);六氫吡酮/喹啉類,例如:吡喹酮(praziquantel),依西太爾(epsiprantel);六氫吡類,例如:六氫吡,羥(hydroxyzine);四環素類,例如:四環素,氯四環素(chlorotetracycline),四環黴素(doxycycline),羥四環素(oxytetracycline),羅利環素(rolitetracycline);其他各類,例如:西萘脒(bunamidine),尼立達唑(niridazole),雷瑣侖太(resorantel),勿鹵酊(omphalotin),奧替普拉(oltipraz),硝硫氰酯(nitroscanate),硝羥碘苄腈(nitroxynil),奧沙尼喹(oxamniquin),脈拉殺(mirasan),鹽酸盧甘宋(miracil),魯坎松((lucanthon),海恩酮(hycanthon),舒喘靈(hetolin),吐根堿(emetin),乙胺嗪(diethylcarbamazine),二氯芬(dicholophen),地芬尼太(diamfenetide),氯硝西泮(clonazepam),酚乙銨(bephenium),硝硫氰胺(amoscamate),氯舒隆(clorsulon)。
活性抗原生動物組成份,包括但非侷限於下列活性組成份:三類,例如:地克珠利(diclazuril),帕托珠利(ponazuril),來曲珠利(letrazuril),甲苯二嗪酮(toltrazuril);聚醚離子載體類,例如:莫能菌素(monensin),鹽黴素(salinomycin),馬杜黴素(maduramicin),甲基鹽黴素(narasin);大環內酯類,例如:米爾倍黴素(milbemycin),紅黴素(erythromycin);喹諾酮類,例如:恩諾沙星(enrofloxacin),比多沙星(pradofloxacin);奎寧類,例如:氯喹(chloroquin);嘧啶類,例如:乙胺嘧啶(pyrimethamine);磺醯類,例如:磺胺喹喔啉(sulfaquinoxaline),甲氧苄啶(trimethoprim),磺
胺氯吡(sulfaclozin);硫胺類,例如:安普羅利(amprolium);林可醯胺類,例如:克林黴素(clindamycin);碳醯替苯胺類,例如:依咪多卡(imidocarb);硝基呋喃類,例如:硝呋莫司(nifurtimox);喹唑啉酮生物鹼類,例如:鹵夫酮(halofuginone);其他各類,例如:奧沙尼喹(oxamniquin),巴龍黴素(paromomycin);疫苗類或來自微生物的抗原類,例如:狗焦蟲(Babesia canis rossi),雞艾美球蟲(Eimeria tenella),早熟艾美球蟲(Eimeria praecox),毒害艾美球蟲(Eimeria necatrix),和緩艾美球蟲(Eimeria mitis),巨型艾美球蟲(Eimeria maxima),深色艾美球蟲(Eimeria brunette),堆型艾美球蟲(Eimeria acervulina),(Babesia canis vogeli),嬰兒利什曼原蟲(Leishmania infantum),犬巴貝斯原蟲(Babesia canis canis),牛肺線蟲(Dictyocaulus viviparous)。
所有提及之混合的組份,視情況可以,亦可與適當的鹼或酸形成鹽類,如果其等根據其官能基團而能如此。
式(I)化合物亦可用來控制媒介。於本發明內文中,媒介為節肢動物,尤其是能夠將病原體,例如,病毒,蠕蟲,單細胞生物及細菌,由儲存體(植物,動物,人類等)傳介至一寄主之昆蟲或蜘蛛。該病原體可機械式的傳介(例如沙眼係由無刺蠅)至寄主或於注入後(例如瘧原蟲係由蚊子)傳介至寄主。
媒介及其等所傳介之疾病或病原體的實例為:1)蚊子-瘧蚊:瘧疾,絲蟲病;-庫蚊:日本腦炎,絲蟲病,其他病毒性疾病,其他蠕蟲的傳播;
-伊蚊:黃熱病,登革熱,其他病毒性疾病,絲蟲病;-蚋:蠕蟲的傳介,尤其是盤尾絲蟲;-毛蠓(Psychodidae):利甚曼病(leishmaniasis)的傳介;2)蝨子:皮膚感染,流行性斑疹傷寒;3)跳蚤:鼠疫,地方性斑疹傷寒,縧蟲;4)蠅:昏睡病(錐蟲病);霍亂,其他細菌性疾病;5)蟎蟲:壁虱病,流行性斑疹傷寒,立克次痘疹,土拉菌病,聖路易士腦炎,蜱傳腦炎(TBE),克裡米亞-剛果出血熱,疏螺旋體病;6)蜱:包柔螺旋體病,如伯氏疏螺旋體(Borrelia bungdorferi sensu lato.),杜通氏螺旋體(Borrelia duttoni),蜱傳腦炎,Q熱病(貝氏柯克斯體(Coxiella bumetii)),巴貝斯蟲(babesioses)(犬巴貝斯蟲(Babesia canis canis)),艾利希體(ehrlichiosis)。
於本發明內文中,媒介之實例為昆蟲,例如蚜蟲,蒼蠅,葉蟬或薊馬,其可將植物病毒傳遞至植物。其他可傳遞植物病毒之媒介為紅蜘蛛,虱,甲蟲及線蟲。
於本發明內文中,其他媒介之實例為昆蟲及蜘蛛,如蚊子,尤其是屬名為下列者:伊蚊(Aedes),瘧蚊(Anopheles),例如甘比亞瘧蚊(A.gambiae),阿拉伯按蚊(A.arabiensis),不吉按蚊(A.funestus),大劣按蚊(A.dirus)(瘧疾)及庫蚊(Culex),毛蠓(Psychodidae)如白蛉(Phlebotomus),沙蠅(Lutzomyia),蝨子(lice),跳蚤(fleas),蠅(flies),蟎蟲(mites)及蜱(ticks),其可傳介病原體至動物及/或人類。
如果式(I)化合物可破除抗性,媒介控制亦屬可能。
式(I)化合物適用於預防由媒介所傳遞之疾病及/或病原體。因此,因此,本發明另一方面係式(I)化合物於媒介控制,例如於農業,於園藝,於林業,於花園及休閒設施,以及於物質保護及產品儲存上之用途。
式(I)化合物適用於保護工業物質以對抗昆蟲之攻擊或破壞,例如下列各目者:鞘翅目(Coleoptera),膜翅目(Hymenoptera),等翅目(Isoptera),鱗翅目(Lepidoptera),囓蟲目(Psocoptera)及衣魚目(Zygentoma)。
於本發明內文中,應瞭解工業物質係指無生命物質,如宜為塑膠,黏著劑,漿糊,紙張和卡片,皮革,木材,加工木製產品及塗料組成物。本發明於保護木材之用途特別適宜。
於其他具體例中,式(I)化合物係與至少一種其他殺昆蟲劑及/或至少一種殺真菌劑一起使用。
於其他具體例中,式(I)化合物係為隨時可用之殺蟲劑型式,意指其等可施用於有關之物質上而無需進一步改良。有用之其他殺昆蟲劑或殺真菌劑尤其是包括上述者。
令人驚奇的發現,式(I)化合物可用來保護與鹽水或苦鹹水接觸之物體,特別是船體,螢幕,網子,建築物,系泊設備和信號系統,以防止積垢。同樣地可單獨使用式(I)化合物,或與其他活性化合物合併,作為防汙劑。
式(I)化合物適用於控制衛生領域之動物蟲害。更特別的,本發明可用於家庭保護領域,於衛生保護領域及於保護儲存之產品,特別是控制在密閉空間中遇到的昆蟲,蜘蛛,蜱和蟎蟲,例如住宅,工廠大廳,辦公室,汽車坐艙,動物繁殖設施。於控制動物蟲害時,式(I)化合物係單獨使用或與其他活性化合物及/或輔助劑合併使用。其等宜使用於家庭殺蟲劑產品中。式(I)化合物可有效的對抗敏感及抗性品種,並對抗所有的發育階段。
這些蟲害包括,例如,蜘蛛(Arachnida)之蟲害,蠍目(Scorpiones),蜘
蛛目(Araneae)及盲蛛目(Opiliones),唇足綱(Chilopoda)及倍足綱(Diplopoda),昆蟲綱(Insecta)輝蠊目(Blattodea),鞘翅目(Coleoptera),革翅目(Dermaptera),雙翅目(Diptera),異翅目(Heteroptera),膜翅目(Hymenoptera),等翅目(Isoptera),鱗翅目(Lepidoptera),毛虱目(Phthiraptera),囓蟲目(Psocoptera),跳躍亞目(Saltatoria)或直翅目(Orthopter),蚤目(Siphonaptera)及衣魚目(Zygentoma)和軟甲綱(Malacostraca)等足目(Isopoda)。
施用可藉由下列:例如,氣溶膠,未加壓之噴霧產品,例如泵及霧化器噴霧,自動霧化系統,煙霧機,泡沫,凝膠,蒸發器產品,其具有由纖維或塑膠製成之蒸發器組,液體蒸發器,凝膠及膜蒸發器,推進器驅動的蒸發器,無能耗,或被動的蒸發系統,蛾紙,蛾袋及蛾膠,呈顆粒或粉塵,在傳播之餌料中或於誘餌站來實施。
式(I-A)化合物,其中Q代表氧,可,例如,藉由程式1所示之製法來合成。式(I-B)化合物,其中Q代表硫可由式(I-A)化合物,例如根據程式2而得到。於程式1及2所示之製法中,於各情況中,於各式中所使用之基團W,Y,V,A,L1及L2,除非另有指明,為較佳範圍(1)至(5)中給定之意義。
式(I-A)化合物之合成可如程式1所示,首先藉由將式(II)咪唑羧酸與式(III)胺基吡啶進行反應而得到式(IV)化合物(參見醯胺化過程)。然後將式(IV)化合物依類似方法以強鹼,例如,正丁基鋰,二異丙基胺鋰或第三丁醇鋰於低溫(-75至-100℃)時於溶劑如,例如,四氫呋喃或二乙基醚中予以去質子化,且然後與氯化劑如,例如,式(V)六氯乙烷進行反應而得到式(VI)氯咪唑(參見EP1988081;US20050250948)。然後可將式(VI)氯咪唑與式(VII)氮親核試劑進行反應而得到式(I-1)化合物。本文中,式(VII)化合物
可任意地使用鹼來去質子化。可藉由舉例方式提及之鹼類為:氫氧化鉀,第三丁醇鉀,三乙基胺,同樣地所有習用無機或有機鹼類,例如有機胺類如二異丙基乙基胺,N-甲基嗎福啉,吡啶或N,N-二甲基胺基吡啶,鹼金屬碳酸鹽及鹼土金屬碳酸鹽,如碳酸鋰,碳酸鈉,碳酸鉀或碳酸銫;鹼金屬碳酸氫鹽,如碳酸氫鈉或碳酸氫鉀。業已說明諸多藉由各種胺基化合物而於咪唑之2-位置上氯原子之取代的反應條件[參見,例如,US2005250948;WO2010144338;Jablonski,J.A.et al.,Bioorg.Med.Chem.Lett.2009,19,903-907;US2009186879]。
於製法中所需之式(II)咪唑基羧酸係市售可得或可,例如,藉由已知於文獻,如H.Rapoport et.al.;Synthesis 1988,10,767-771,BASF Aktiengesellschaft patent:US4864030 A1,1989,Takeda Pharmaceutical Company Limited patent:EP2530078 A1,2012,TAISHO PHARMACEUTICAL CO.,LTD.patent:US2012/10414 A1,2012,Subrayan,Ramachandran P.;Thurber,Ernest L.;Rasmussen,Paul G.Tetrahedron,1994,50,2641-2656之方法來製備。
於製法中所需之式(III)3-胺基吡啶係市售可得或可,例如,藉由已知於文獻,如Liu,Zhen-Jiang;Vors,Jean-Pierre;Gesing,Ernst R.F.;Bolm,Carsten,Advanced Synthesis and Catalysis,2010,352,3158-3162,BAYER CROPSCIENCE AG patent:US2010/305124 A1,2010,Shafir,Alexandr;Buchwald,Stephen L.,Journal of the American Chemical Society,2006,128,8742-8743之方法來製備。
於製法中所需之式(VIII)NH化合物(例如烷基胺,二烷基胺,環胺,肼,吡唑,咪唑,三唑等)係市售可得或可藉由已知於有機化學之一般方法來製備。
式(I-B)硫代醯胺類可如程式2所示,藉由將式(I-A)化合物與硫化劑如,例如,五硫化二磷或Lawesson’s試劑(參見,例如,C.P.Dell in Comprehensive Organic Functional Group Transformations,Vol.5,Ed.:A.R.Katrizky,O.Meth-Cohn,C.W.Rees,Pergamon,Oxford,1995,S.565-628;M.Jesberger,T.P.Davis,L.Barner,Synthesis 2003,13,1929)類似於一般已知的方法來進行反應而合成。
於根據本發明之製法中的式(IV)化合物可使用已知於文獻之醯胺化過程或類似於明確提到之實例來合成。
已有描述醯胺化步驟之諸多反應條件,例如G.Benz in Comprehensive Organic Synthesis,1st Ed.,Pergamon Press,Oxford,1991,Vol.6,pp.381-417;P.D.Bailey et al.in Comprehensive Organic Functional Group Transformation,1st Ed.,Elsevier Science Ltd.,Oxford,1995,Vol.5,pp.257-308及R.C.Larock in Comprehensive Organic Transformations,2nd Ed.,Wiley-VCH,New York,Weinheim,1999,pp.1929-1994。這些反應中之一些係經由中間體碳醯氯來進行,其可以分離形式或以原位形式使用。
該醯胺化反應係任意地在一縮合劑存在下,任意地在一酸接受體存在下及任意地在一溶劑存在下進行。
有用之縮合劑為典型地可用於此等醯胺化反應之所有縮合劑。實例包括激活劑,如光氣,三氯化磷,三氯氧化磷,草醯氯,草醯溴或亞硫醯(二)氯;碳化二亞胺如N,N'-二環己基碳化二亞胺(DCC)及1-(3-二甲基胺基丙基)-3-乙基碳化二亞胺(EDCI),或其他習用縮合劑,如五氧化二磷,多磷酸,N,N'-羰基二咪唑,2-氯吡啶1-碘化氫(Mukaiyama's試劑),2-乙氧基-N-乙氧基羰基-1,2-二氫喹啉(EEDQ),三苯基膦/四氯化碳,溴三吡咯烷基鏻六氟磷酸鹽(BROP),O-(1H-苯并三唑-1-基氧基)三(二甲基胺基)鏻六氟磷酸鹽(BOP),N,N,N',N'-聯(四亞甲基)氯四氟硼酸鹽,O-(1H-苯并三唑-1-基)-N,N,N',N'-四甲基六氟磷酸鹽(HBTU),O-(1H-苯并三唑-1-基)-N,N,N',N'-聯(四亞甲基)六氟磷酸鹽,O-(1H-苯并三唑-1-基)-N,N,N',N'-四甲基四氟硼酸鹽(TBTU),O-(1H-苯并三唑-1-基)-N,N,N',N'-聯(四亞甲基)四氟硼酸鹽,O-(7-氮雜苯并三唑-1-基)-N,N,N',N'-四甲基六氟磷酸鹽(HATU),1-羥基苯并三唑(HOBt)及4-(4,6-二甲氧基-1,3,5-三-2-基)-4-甲基鎷福鹽(DMT.MM),通常以氯化物來使用。這些試劑可分開使用或合併使用。
適當的酸接受體為所有的習用無機或有機鹼類,例如有機胺類如三乙
基胺,二異丙基乙基胺,N-甲基嗎福啉,吡啶或N,N-二甲基胺基吡啶,鹼金屬及鹼土金屬碳酸鹽,如碳酸鋰,碳酸鈉,碳酸鉀或碳酸銫;鹼金屬碳酸氫鹽,如碳酸氫鈉或碳酸氫鉀。於根據本發明之製法中的醯胺化反應係任意地在一適當反應輔助劑,例如,N,N-二甲基甲醯胺或N,N-二甲基胺基吡啶存在之下進行。適當的溶劑或稀釋劑為所有的惰性有機溶劑,例如脂族或芳族烴類(如石油醚,甲苯,環己烷),鹵素化之烴類(如氯甲苯,二氯苯,二氯甲烷,氯仿,1,2-二氯乙烷),醚類(如二乙醚,二烷,四氫呋喃,1,2-二甲氧基乙烷),酯類(如乙基或醋酸甲酯),硝基烴類(如硝基甲烷,硝基乙烷,硝基苯),腈類(如乙腈,丙腈,丁腈,苄腈),醯胺類(如N,N-二甲基甲醯胺,N,N-二甲基乙醯胺,N-甲基甲醯苯胺,N-甲基吡咯烷酮,六甲基磷醯胺),以及二甲亞碸或水或所提及溶劑之混合物。
亦可使用混合的酸酐以製備式(III)化合物(參見J.Am.Chem.Soc.1967,5012)。於此製法中,其可使用氯甲酸酯,例如氯甲酸甲酯,氯甲酸乙酯,氯甲酸異丁酯及氯甲酸異丙酯。同樣地,為此目的其可使用二乙基乙醯氯,三甲基乙醯氯及類似化合物。
本發明亦提供式(VI)中間體
其中該基團之意義係根據較佳範圍(1-1)至(5-1)或(1-2)至(5-2)之一者且尤其佳者係根據較佳範圍(5-1)或(5-2)之意義。
下文中之製備及用途實例係闡述本發明,但非侷限於此。
合成實例編號1
N,1-二甲基-N-(吡啶-3-基)-2-[3-(三氟甲基)-1H-吡唑-1-基]-1H-咪唑-5-甲醯胺(化合物編號I-1-007)
步驟1:N,1-二甲基-N-(吡啶-3-基)-1H-咪唑-5-甲醯胺
將12.71g(104.7mmol)亞硫醯(二)氯添加至含有12g(95.2mmol)1-甲基咪唑-5-羧酸於72ml甲苯之懸浮液中,並將混合物於130℃攪拌隔夜。將反應混合物於減壓下濃縮。將一含有10.3g(95.2mmol)3-甲基胺基吡啶於72ml吡啶之溶液添加至殘餘物中,並將產生的反應混合物於115℃加熱4小時。然後將混合物於減壓下再濃縮一次並將殘餘物藉由管柱色層分離法於矽膠上使用流動相乙腈/甲醇3:1予以純化。此得到8.1g(理論值之39.3%)標的化合物及9.5g(理論值之37.1%)標的化合物之HCl鹽。
HPLC-MS:logP[n]=0,44;mass(m/z):217,1;1H-NMR(CD3CN,400MHz);δ=3.39(s,3H),3.81(s,3H),6.17(s,1H),7.36-7.40(m,2H),7.67-7.70(m,1H),8.41(m,1H)8.47(m,1H)ppm。
步驟2:2-氯-N,1-二甲基-N-(吡啶-3-基)-1H-咪唑-5-甲醯胺
將10.0g(46.2mmol)N,1-二甲基-N-(吡啶-3-基)-1H-咪唑-5-甲醯胺溶解
於150ml無水THF中並冷卻至-78℃。將20.34ml(50.8mmol)2.5 molar含有n-BuLi於正己烷之溶液於5分鐘期間逐滴加入,並將混合物於-78℃再攪拌30分鐘。然後將溶解於100ml THF之12.0g(50.8mmol)六氯乙烷於5分鐘期間逐滴加入。將混合物於-78℃時再攪拌45分鐘且然後於60分鐘期間回暖至室溫。將混合物倒至400ml飽和氯化銨溶液中並重複地用二氯甲烷萃取。將有機相合併,用少許水清洗,並用硫酸鎂來乾燥。將溶劑蒸餾出來並將殘餘物藉由製備性逆相HPLC使用流動相水/乙腈予以純化。此得到7.27g(理論值之62%)2-氯-N,1-二甲基-N-(吡啶-3-基)-1H-咪唑-5-甲醯胺。
HPLC-MS:logP[n]=0.88;mass(m/z):251.1;1H-NMR(D6-DMSO,400MHz);δ=3.37(s,3H),3.75(s,3H),6.20(s,1H),7.45(m,1H),7.86(m,1H),8.49(m,1H)8.53(m,1H)ppm。
步驟3:
N,1-二甲基-N-(吡啶-3-基)-2-[3-(三氟甲基)-1H-吡唑-1-基]-1H-咪唑-5-甲醯胺(化合物編號I-1-007)
首先將2-氯-N,1-二甲基-N-(吡啶-3-基)-1H-咪唑-5-甲醯胺(150mg,0.59mmol)添加至二甲基甲醯胺(5.0ml)中,並將碳酸銫(389.9mg,1.19mmol)加入。將反應混合物於120℃攪拌隔夜且然後將溶劑於減壓下完全蒸餾出來。將殘餘物於矽膠上用流動相醋酸乙酯/甲醇(80:20)予以色層分離。此得到61mg(理論值之29.1%)N,1-二甲基-N-(吡啶-3-基)-2-[3-(三氟甲基)-1H-吡唑-1-基]-1H-咪唑-5-甲醯胺。
HPLC-MS:logP[n]=1.87;mass(m/z):351.1;1H-NMR(D6-DMSO,400MHz);δ=3.42(s,3H),3.81(s,3H),6.28(s,1H),6.83(m,1H),7.39(m,1H),
7.73(m,1H),8.08(m,1H),8.49(m,2H)ppm。
合成實例編號2
N,1-二甲基-2-(嗎福啉-4-基)-N-(吡啶-3-基)-1H-咪唑-5-甲醯胺(化合物編號I-1-009)
將2-氯-N,1-二甲基-N-(吡啶-3-基)-1H-咪唑-5-甲醯胺(150mg,0.59mmol)及嗎福啉(216mg,2.48mmol)於100℃攪拌隔夜。將混合物倒至水中並重複地用醋酸乙酯萃取。將合併之有機相於硫酸鎂上乾燥,將溶劑於減壓時蒸餾出來並將殘餘物藉由製備性逆相HPLC使用流動相水/乙腈予以純化。此得到135mg(理論值之75.8%)N,1-二甲基-2-(嗎福啉-4-基)-N-(吡啶-3-基)-1H-咪唑-5-甲醯胺。
HPLC-MS:logP[n]=0.85;mass(m/z):302.1;1H-NMR(CD3CN,400MHz);δ 1=3.26(m,2H),3.30(s,3H),3.44(m,2H),3.57(s,3H),3.80(m,2H),3.93(m,2H),5.90(s,1H),7.6-8.0(m,2H),8.38-8.47(m,1H),8.59-8.67(m,1H)ppm。
類似於上述實例製備之其他式(I)化合物係列於表1。
表1式(I-1)化合物
a)於上表及製備實例中所述之logP值係根據EEC directive 79/831 Annex V.A8藉由HPLC(高效液體色層分離法)使用逆相管柱(C18)來測量。溫度:43℃。該校準係使用未分支之烷-2-酮(具有3至16個碳原子)來進行,其中,該logP值係已知。
M+藉由LC-MS於酸性範圍之測定係於pH 2.7使用流動相0.1%水性甲酸及乙腈(含有0.1%甲酸);線性梯度由10%乙腈至95%乙腈,儀器:Agilent 1100 LC system,Agilent MSD system,HTS PAL。
M+藉由LC-MS於中性範圍之測定係於pH 7.8使用流動相0.001 molar碳酸氫銨水溶液及乙腈來進行;線性梯度由10%乙腈至95%乙腈。
酸性範圍(如logP[a])及/或中性範圍(如logP[n])之logP值係陳述於上表及實例中。
b)1H NMR值之測定係使用裝配有樣品流動頭(容量60μl)之Bruker Avance 400,以四甲基矽烷作為參考值(0.0)及溶劑CD3CN,CDCl3或D6-DMSO來進行。
所選擇實例之NMR數據係以習用型式(δ值,複數峰分裂,氫原子數目)或呈NMR峰列而列出。
NMR峰列方法
所選擇實例之1H NMR數據係以1H NMR峰列之方式陳述。對於每一個信號峰值,首先為δ之ppm值且然後列出圓括號中之信號強度。該δ值-不同信號峰之信號強度數目對係被列出並用分號相互分開。
因此一個實例之峰列型式為:δ1(強度1);δ2(強度2);......;δi(強度i);......;δn(強度n)
於NMR光譜之一印示實例中與訊號高度相關之尖銳訊號強度以cm表示且顯示真實的訊號強度關係。於寬訊號之情況時,數個峰或訊號中間及其相關之強度可顯示於以與光譜中最強訊號相比較。
1H-NMR光譜之化學位移的校準係使用四甲基矽烷及/或溶劑之化學位移來完成,特別為於DMSO中測量光譜時。因此,四甲基矽烷峰可以但無需出現於NMR峰列中。
1H-NMR之峰列類似於傳統1H-NMR列印出來者且因此通常含有所有列於傳統NMR解讀之峰。
此外,如同傳統1H NMR列印出來者,其等可顯示出溶劑訊號,目標化合物之立體異構物的訊號,其同樣由本發明提供,及/或不純物之峰。
於溶劑及/或水之δ範圍之化合物訊號報導中,吾等所列1H NMR峰顯示標準溶劑峰,例如DMSO於DMSO-D6之峰及水之峰,其通常平均具有高強度。
該目標化合物之立體異構物的峰及/或不純物的峰通常較目標化合物的峰具有較低平均強度(例如,其純度>90%)。
此等立體異構物及/或不純物可能是典型的特別製備方法。因此其等峰可於此情況中參照「副產物指紋」幫忙確認吾等製備方法之再現。
一專家藉由已知方法計算目標化合物之峰(MestreC,ACD刺激,但亦憑經驗來評估期望值),如果需要,可任意使用其他強度之濾器,單離目標化合物之峰。此單離將類似於在習用1H-NMR解讀中之相關峰值挑選。
1H NMR峰列之其他詳細說明可見於Research Disclosure Database Number 564025。
下列實例證明了根據本發明化合物之殺昆蟲及殺蟎蟲作用。於這些實例中,所引述之根據本發明的化合物係相關於列於表1具有相關參考編號(No.)之化合物:
澳洲牛蜱(Boophilus microplus)-注射測試
溶劑:二甲亞碸
為了製備適當之活性化合物製劑,將10mg活性化合物與0.5ml溶劑摻合並將濃縮物用溶劑稀釋成想要的濃度。
將1μl活性化合物溶液注射至5隻成年雌性牛蜱腹部(澳洲牛蜱)。將動物轉移至盤中並保存在氣候控制室。
7天後藉由孵育受精卵來評估功效。將未明顯受精之卵存放在氣候控制室直到於約42天後孵出幼蟲。100%之功效意指沒有蜱蟲產下任何受精卵;0%意指所有的卵都受精。
於此測試中,例如,來自製備實例之下列化合物於20μg/每隻動物之施用率時顯示80%之功效:I-1-031
桃蚜(Myzus persicae)-口服測試
溶劑:100重量份之丙酮
為了製備適當之活性化合物製劑,將1重量份之活性化合物用所述重量份之溶劑溶解並加入水直到達到想要的濃度。
將50μl活性化合物製劑轉移至微量滴定板並用150μl之IPL41昆蟲介質(33%+15%糖)使最終體積成為200μl。隨即,將該板用石蠟膜密封,其
中第二微量滴定板中的綠桃蚜蟲(桃蚜)的混合種群能夠刺穿它並通過它而吸收溶液。
5天後,測定功效%。100%意指所有的蚜蟲均被殺死;0%意指沒有蚜蟲被殺死。
於此測試中,例如,來自製備實例之下列化合物於20ppm之施用率時顯示100%之功效:I-1-001,I-1-002,I-1-003,I-1-004,I-1-005,I-1-006,I-1-007,I-1-008,I-1-009,I-1-010,I-1-011,I-1-012,I-1-013,I-1-014,I-1-015,I-1-016,I-1-017,I-1-018,I-1-019,I-1-020,I-1-021,I-1-022
桃蚜(Myzus persicae)-噴灑測試
溶劑:78重量份之丙酮1.5重量份之二甲基甲醯胺
乳化劑:烷基芳基聚乙二醇醚
為了製備適當之活性組成份調配物,將1重量份之活性組成份溶解於所述重量份之溶劑中並加入含有乳化劑濃度為1000ppm的水直到達到想要的濃度。為了製備其他測試濃度,將調配物用含有乳化劑之水來稀釋。
將中國捲心菜(結球白菜)之葉片用所有階段已用想要濃度之活性化合物調配物噴灑之桃蚜(Myzus persicae)感染。
5-6天後,測定功效%。100%意指所有的蚜蟲均被殺死;0%意指沒有蚜蟲被殺死。
於此測試中,例如,來自製備實例之下列化合物於500g/ha之施用率時顯示100%之功效:I-1-004,I-1-006,I-1-007,I-1-008,I-1-009,I-1-010,I-1-011,I-1-013,I-1-017,I-1-018,I-1-019,I-1-020,I-1-021
於此測試中,例如,來自製備實例之下列化合物於500g/ha之施用率時顯示90%之功效:I-1-001,I-1-002,I-1-003,I-1-005,I-1-012,I-1-014,
I-1-015,I-1-016,I-1-022
二斑葉蟎(Tetranychus urticae)-噴灑測試,OP-抗性
溶劑:78.0重量份之丙酮1.5重量份之二甲基甲醯胺
乳化劑:烷基芳基聚乙二醇醚
為了製備適當之活性化合物製劑,將1重量份之活性化合物用指明重量份之溶劑來溶解並加入含有濃度為1000ppm之乳化劑的水直到達到想要的濃度。為了製備其他測試濃度,將調配物用含有乳化劑之水稀釋。
將豆葉(菜豆(Phaseolus vulgaris))之葉片用所有階段已用想要濃度之活性化合物調配物噴灑之温室红蜘蛛螨(二斑葉蟎)感染。
6天後,測定功效%。100%意指所有的蜘蛛螨均被殺死;0%意指沒有蜘蛛螨被殺死。
於此測試中,例如,來自製備實例之下列化合物於500g/ha之施用率時顯示90%之功效:I-1-009,I-1-015。
桃蚜(Myzus persicae)-噴灑測試(MYZUPE)
溶劑:78.0重量份之丙酮1.5重量份之二甲基甲醯胺
乳化劑:烷基芳基聚乙二醇醚
為了製備適當之活性化合物製劑,將1重量份之活性化合物用指明重量份之溶劑來溶解並加入含有1000ppm乳化劑濃度之水直到達到想要的濃度。為了製備其他測試濃度,將調配物用含有乳化劑之水來稀釋。
將中國捲心菜(結球白菜)之葉片用所有階段已用想要濃度之活性化合
物調配物噴灑之桃蚜(Myzus persicae)感染。
於想要的時間間隔後(dat),測定功效%。100%意指所有的蚜蟲均被殺死;0%意指沒有蚜蟲被殺死。
於此測試中,例如,來自製備實例之下列化合物較已知技藝者顯示較優異功效:參見表3
桃蚜(Myzus persicae)-口服測試(MYZUPE O)
溶劑:100重量份之丙酮
為了製備適當之活性化合物製劑,將1重量份之活性化合物溶解於所述重量份之溶劑中並用水調整直到達到想要的濃度。
將50μl活性化合物製劑轉移至微量滴定板並用150μl之IPL41昆蟲介質(33%+15%糖)使最終體積成為200μl。隨即,將該板用石蠟膜密封,其中第二微量滴定板中的綠桃蚜蟲(桃蚜)的混合種群能夠刺穿它並通過它而吸收溶液。
於想要的時間間隔後(dat),測定功效%。100%意指所有的蚜蟲均被殺死;0%意指沒有蚜蟲被殺死。
於此測試中,例如,來自製備實例之下列化合物顯示較已知技藝者顯示較優異功效:參見表3
二斑葉蟎(Tetranychus urticae)-噴灑測試,OP-抗性(TETRUR)
溶劑:78.0重量份之丙酮1.5重量份之二甲基甲醯胺
乳化劑:烷基芳基聚乙二醇醚
為了製備適當之活性活性化合物製劑,將1重量份之活性化合物用指明重量份之溶劑來溶解並用含有乳化劑濃度為1000ppm之水調整直到達到
想要的濃度。為了製備其他測試濃度,將調配物用含有乳化劑之水來稀釋。
將豆葉(菜豆(Phaseolus vulgaris))之葉片用所有階段已用想要濃度之活性化合物調配物噴灑之温室红蜘蛛螨(二斑葉蟎)感染。
於想要的時間間隔後(dat),測定功效%。100%意指所有的蜘蛛螨均被殺死;0%意指沒有蜘蛛螨被殺死。
於此測試中,例如,來自製備實例之下列化合物較已知技藝者顯示較優異功效:參見表3
Claims (14)
- 一種式(I)化合物,
其中Q 代表氧或硫,V 代表由氫,鹵素,烷基,鹵烷基,烷氧基,鹵烷氧基及氰基所組成群組之一基團,W 代表由氫,鹵素,烷基,鹵烷基,烷氧基,鹵烷氧基及氰基所組成群組之一基團,Y 代表由氫,氰基,可選擇地經取代之烷基、烯基或炔基,可選擇地經取代之環烷基其可選擇地插入雜原子,可選擇地經取代之環烷基烷基其可選擇地插入雜原子,芳基烷基或雜芳基烷基所組成群組之一基團,A 代表由氫,可選擇地經取代之烷基,烯基或炔基及可選擇地經取代之環烷基或環烷基烷基其可選擇地插入雜原子所組成群組之一基團,T 代表氧或一電子對,L1 代表由氫,可選擇地經取代之烷基、烯基、炔基或環烷基所組成群組之一基團及代表基團C(O)R2,C(O)N(R3)(R4),C(O)OR5及 SO2R6,L2 代表由氫,N(R3a)(R4a),可選擇地經取代之烷基、烯基、炔基或烷氧基,可選擇地經取代之環烷基或環烷基烷基其可選擇地插入雜原子,及可選擇地經取代之芳基、芳基烷基、雜芳基或雜芳基烷基所組成群組之一基團,或L1及L2 與其等所連接之氮原子一起,代表可選擇地經取代之飽和,部份飽和或具有3至7個環原子之芳族雜環其可選擇地插入其他雜原子及/或一個或兩個C=O基團,R2 代表由氫,可選擇地經取代之烷基、烯基或炔基,可選擇地經取代之環烷基,可選擇地經取代之芳基或雜芳基及可選擇地經取代之芳基烷基或雜芳基烷基所組成群組之一基團,R3及R4 各自獨立代表由氫,可選擇地經取代之烷基、烯基或炔基,可選擇地經取代之飽和或不飽和環烷基、環烷基烷基、芳基、雜芳基、芳基烷基或雜芳基烷基所組成群組之一基團,或R3及R4一起形成可選擇地經取代之三-至七-員脂族環,其任意含有一氮,硫或氧原子,R3a 代表由氫,可選擇地經取代之烷基,可選擇地經取代之環烷基、芳基、雜芳基、芳基烷基或雜芳基烷基所組成群組之一基團,R4a 代表由氫,可選擇地經取代之烷基,可選擇地經取代之C3-C6-環烷基所組成群組之一基團且代表基團C(O)R2,C(O)OR5及SO2R6,R5 代表可選擇地經取代之烷基、烯基或炔基,可選擇地經取代之環烷基或環烷基烷基, R6 代表來自包含可選擇地經取代之烷基、烯基或炔基,可選擇地經取代之環烷基環烷基烷基、芳基、芳基烷基、雜芳基或雜芳基烷基之基團,及其鹽類。 - 根據請求項1之化合物,其中Q 代表氧或硫,V 代表由氫,鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基及氰基所組成群組之一基團,W 代表由氫,鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基及氰基所組成群組之一基團,Y 代表由氫,C1-C6-烷基,C3-C6-烯基或C3-C6-炔基所組成群組之一基團,彼此獨立可選擇地經被下列者所單-至多取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基;C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基;直鏈或分支之C3-C8-環烷基-C1-C4-烷基,彼此獨立可選擇地插入下列者單或二次:O,S(O)n,CO或NR4a且彼此獨立可選擇地被下列者所單-至四取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基;芳基-C1-C4-烷基或雜芳基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,A 代表由下列所組成群組之一基團:氫,C1-C6-烷基,C3-C6-烯基或C3-C6-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基;及C3-C6-環烷基,彼 此獨立可選擇地被下列者所單-或二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基;及C1-C6-烷基,C3-C6-烯基或C3-C6-炔基彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基;及直鏈或分支之C3-C8-環烷基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,T 代表氧或一電子對,L1 代表由下列所組成群組之一基團:氫,C1-C4-烷基,C3-C6-烯基或C3-C6-炔基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基;C3-C6-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基;及代表基團C(O)R2,C(O)N(R3)(R4),C(O)OR5及SO2R6,L2 代表由下列所組成群組之一基團:氫,-N(R3a)(R4a),C1-C4-烷基,C3-C6-烯基,C3-C6-炔基或C1-C4-烷氧基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷氧基,C1-C4-烷基-S(O)n-或氰基;直鏈或分支之C3-C8-環烷基或C3-C8-環烷基-C1-C4-烷基,彼此獨立可選擇地插入下列者單-或二次:O,S(O)n,CO或NR4a且彼此獨立可選擇地被下列者所單-至四取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基;芳基,雜芳基,芳基烷基或雜芳基烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,或L1及L2 與N一起代表來自基團U-1至U-36之雜環
Xb 代表由下列所組成群組之一基團:鹵素,硝基,氰基,C1-C4-烷基,C3-C6-環烷基,C1-C5-鹵素烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基,C3-C6-鹵環烷基,C1-C4-烷氧基-C1-C4-烷基,氰基-C1-C4-烷基,C3-C6-環烷基-C1-C4-烷基,C2-C6-烯基,C3-C6-炔基,C1-C4-烷基-S(O)n-,C1-C4-烷基羰基,C1-C6-鹵烷基羰基,C1-C6-烷氧基羰基,C1-C6-烷基胺基羰基,二-(C1-C6)烷基胺基羰基,C1-C6-烷基羰基胺基,芳基及雜芳基,其中該取代基芳基及雜芳基可任 意地被選自包含下列所組成群組之取代基所單-或多取代:鹵素,氰基,硝基,C1-C6-烷基,C2-C6-烯基,C2-C6-炔基,C1-C4-烷氧基,C1-C4-鹵烷基,C1-C6-鹵烷氧基及C1-C4-烷基硫基且其中該環氮原子於U-13,U-14,U-16,U-28及U-35未被鹵素,硝基,氰基,C1-C4-烷氧基,C1-C4-鹵烷氧基,C1-C4-烷氧基-C1-C4-烷基氧基所取代,R2 代表由下列所組成群組之一基團:氫,C1-C8-烷基,C3-C8-烯基或C3-C8-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基或C1-C4-烷基-S(O)n-;C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基;芳基或雜芳基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基;及直鏈或分支之芳基-C1-C4-烷基或雜芳基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,R3,R4 各自獨立代表由下列所組成群組之一基團:氫,C1-C8-烷基,C3-C8-烯基或C3-C8-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基或C1-C4-烷基-S(O)n-;C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基;芳基或雜芳基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基;及直鏈或分支之芳基-C1-C4-烷基或雜芳基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,R3a 代表由下列所組成群組之基團:氫,C1-C8-烷基,彼此獨立可選擇 地被下列者所單-至多取代:鹵素,氰基或C1-C4-烷氧基;C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基或C1-C4-烷氧基;芳基或雜芳基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基;及直鏈或分支之芳基-C1-C4-烷基或雜芳基-C1-C4-烷基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,硝基或氰基,R4a 代表由下列所組成群組之一基團:氫,C1-C4-烷基,彼此獨立可選擇地被下列者所單-至多取代:鹵素或C1-C4-烷氧基;C3-C6-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基或C1-C4-烷氧基;且代表基團C(O)R2,C(O)OR5及SO2R6,R5 代表C1-C8-烷基,C3-C8-烯基或C3-C8-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基或C1-C4-烷基-S(O)n-;C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基,R6 代表由下列所組成群組之基團:C1-C8-烷基,C3-C8-烯基或C3-C8-炔基,彼此獨立可選擇地被下列者所單-至多取代:鹵素,C1-C4-烷氧基或C1-C4-烷基-S(O)n-;C3-C8-環烷基,彼此獨立可選擇地被下列者所單-至二取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基或氰基;芳基或雜芳基,彼此獨立可選擇地被下列者所單-至三取代:鹵素,C1-C4-烷基,C1-C4-鹵烷基,C1-C4-烷氧基,C1-C4-烷基-S(O)n-,C1-C4-鹵烷氧基,C1-C4-鹵烷基-S(O)n-,硝基或氰基,m 代表0,1,2或3之數目,n 代表0,1或2之數目,及其鹽類。 - 根據請求項2之化合物,其中Q 代表氧,V 代表由氫,氟,氯,溴,甲基及乙基所組成群組之一基團,W 代表由氫,氟,氯,溴,氰基及甲基所組成群組之一基團,Y 代表由下列所組成群組之一基團:氫,C1-C4-烷基,C3-C4-烯基或C3-C4-炔基,彼此獨立可選擇地被下列者所單-至五取代:氟,氯,溴,甲氧基或乙氧基;及C3-C6-環烷基,彼此獨立可選擇地被下列者所單-至二取代:氟,氯,溴,甲基,乙基,三氟甲基,甲氧基,乙氧基或氰基,A 代表由下列所組成群組之一基團:氫,C1-C6-烷基,C3-C6-烯基或C3-C6-炔基,彼此獨立可選擇地被下列者所單-至五取代:氟,氯,溴,甲氧基,乙氧基或氰基;及C3-C6-環烷基,彼此獨立可選擇地被下列者所單-至二取代:氟,氯,溴,甲基,乙基,三氟甲基,甲氧基,乙氧基或氰基,T 代表一電子對,L1及L2 與N一起代表來自基團U-1,U-2,U-3,U-4,U-5,U-6,U-7,U-25,U-26,U-27,U-28,U-29及U-30之雜環,Xb 代表由下列所組成群組之一基團:鹵素,硝基,氰基,胺基,C1-C4-烷基,C3-C6-環烷基,C1-C2-鹵烷基,C1-C4-烷氧基,C1-C4-鹵烷氧基,C3-C6-鹵環烷基,C1-C4-烷氧基-C1-C4-烷基,C1-C6-烷基硫基,C1-C4-烷氧基羰基,C1-C4-烷基胺基羰基,C1-C6-烷基磺醯基,C1-C6-烷基羰基胺基及苯基,其中苯基可可選擇地被氟,氯,溴,甲基,乙基,二氟甲基,三氟甲基,甲氧基,乙氧基,Me-S(O)n-,Et-S(O)n-,二氟甲氧基,三氟甲氧基,三氟甲基-S(O)n-,二氟乙基-S(O)n-,三氟乙基-S(O)n-,硝基或氰基所單-至三取代,或Xb 代表一C3-C5-碳鏈,其係連接至兩個相鄰的環位置並形成脂族環,於此情況下m等於2,m 代表0,1或2之數目, n 代表0,1或2之數目,及其鹽類。
- 根據請求項2之式(I-1)化合物,
其中V 代表由氫,氟,氯,甲基及氰基所組成群組之一基團,W 代表由氫,氟,氯,溴及甲基所組成群組之一基團,Y 代表由下列所組成群組之一基團:甲基,乙基,丙基,烯丙基或炔丙基,彼此獨立可選擇地被下列者所單-至三取代:氟,甲氧基,乙氧基或氰基,A 代表由下列所組成群組之一基團:氫,甲基,乙基,丙基,烯丙基,炔丙基或環丙基,彼此獨立可選擇地被下列者所單-至三取代:氟,甲氧基,乙氧基或氰基,T 代表一電子對,L1及L2 與N一起代表來自基團U-1,U-2,U-3,U-4,U-5,U-6,U-7,U-25,U-26,U-27,U-29及U-30之雜環,Xb 代表由下列所組成群組之一基團:氟,氯,溴,氰基,胺基,甲基,乙基,正-及異丙基,環丙基,三氟甲基,二氟甲基,三氟乙基,甲氧基,乙氧基,正-及異丙氧基,三氟甲氧基,甲氧基甲基,乙氧基甲基,甲氧基乙基,乙氧基乙基,甲基-S(O)n-,乙基-S(O)n-,甲氧基羰基,乙氧基羰基,甲基胺基羰基,甲基羰基胺基或苯基,其中苯基可可選擇地被氟,氯,溴,甲基,乙基,二氟甲基,三氟甲基,甲氧基,乙氧基,硝基或氰基所單-至三取代, 或Xb 代表一C3-C4-碳鏈,其係連接至兩個相鄰的環位置並形成脂族環,於此情況下m等於2,m 代表0,1或2之數目,n 代表0,1或2之數目,及其鹽類。 - 根據請求項4之化合物,其中V 代表氫,W 代表氫,Y 代表由氫,甲基,乙基,烯丙基及炔丙基所組成群組之一基團,A 代表由氫,甲基,乙基及環丙基所組成群組之一基團,T 代表一電子對,L1及L2 與N一起代表來自基團U-1,U-2,U-3,U-6,U-25,U-26及U-29之雜環,Xb 代表由氟,氯,溴,氰基,胺基,甲基,乙基,正-及異丙基,三氟甲基,甲氧基,乙氧基,甲基硫基及苯基所組成群組之一基團,其中苯基可可選擇地被氟,氯,甲基或甲氧基所單-至三取代,或Xb 代表一C3-C4-碳鏈,其係連接至兩個相鄰的環位置並形成脂族環,於此情況下m等於2,m 代表0,1或2之數目,及其鹽類。
- 根據請求項4之化合物,其中V 代表氫,W 代表氫,Y 代表甲基,A 代表甲基,乙基或環丙基,T 代表一電子對,L1及L2 與N一起代表來自包含基團U-1,U-2,U-3,U-6,U-25, U-26及U-29之雜環,Xb 代表由氯,氰基,胺基,甲基,異丙基,三氟甲基,甲基硫基及苯基所組成群組之一基團,或Xb 代表-(CH2)3-,其係連接至兩個相鄰的環位置並形成脂族環,於此情況下m等於2,m 代表0,1或2之數目,及其鹽類。
- 一種組成物,其係包含至少一種根據請求項1至6中任一項之化合物及習用擴充劑及/或表面活性劑,特別是為了控制動物蟲害。
- 一種控制動物蟲害的方法,其係將至少一種根據請求項1至6中任一項之化合物或根據請求項7之組成物予以作用在動物蟲害上及/或其等之棲息地。
- 一種至少一種根據請求項1至6中任一項之化合物或根據請求項7之組成物於控制動物蟲害之用途。
- 根據請求項8之方法或根據請求項9之用途,其中不包括對人體或動物體之手術,診療及診斷治療。
- 一種至少一種根據請求項1至6中任一項之化合物於保護植物繁殖物質之用途。
- 一種農化調配物,其包括至少一種根據請求項1至6中任一項之化合物,其以農化調配物之重量計為由0.00000001至98%重量之生物有效量,以及擴充劑及/或表面活性劑。
- 根據請求項12之農化調配物,其另外包含其他農化活性化合物。
- 一種式(VI)之中間體,
其中該基團具有根據請求項1至6項中之意義,且尤其佳者為根據請求項6之意義。
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| BR112018016365A2 (pt) * | 2016-02-11 | 2018-12-26 | Bayer Cropscience Aktiengesellschaft | oxiimidazolilcarboxamidas substituídas como pesticidas |
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| WO2019137995A1 (en) | 2018-01-11 | 2019-07-18 | Basf Se | Novel pyridazine compounds for controlling invertebrate pests |
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| FR2827286A1 (fr) * | 2001-07-11 | 2003-01-17 | Aventis Cropscience Sa | Nouveaux composes fongicides |
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| RU2018132164A (ru) | 2020-03-12 |
| CA3013960A1 (en) | 2017-08-17 |
| KR20180107141A (ko) | 2018-10-01 |
| JP6892452B2 (ja) | 2021-06-23 |
| CO2018008397A2 (es) | 2018-08-21 |
| CN109071507A (zh) | 2018-12-21 |
| WO2017137337A1 (de) | 2017-08-17 |
| US10501441B2 (en) | 2019-12-10 |
| UY37119A (es) | 2017-09-29 |
| CL2018002295A1 (es) | 2018-11-30 |
| IL260829B (en) | 2021-05-31 |
| AU2017217580A1 (en) | 2018-08-16 |
| AR107588A1 (es) | 2018-05-16 |
| JP2019507745A (ja) | 2019-03-22 |
| BR112018016362A2 (pt) | 2018-12-18 |
| MX2018009805A (es) | 2018-09-10 |
| PH12018501705A1 (en) | 2019-06-10 |
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