TW201609650A - 新殺害蟲化合物及用途 - Google Patents
新殺害蟲化合物及用途 Download PDFInfo
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- TW201609650A TW201609650A TW103140581A TW103140581A TW201609650A TW 201609650 A TW201609650 A TW 201609650A TW 103140581 A TW103140581 A TW 103140581A TW 103140581 A TW103140581 A TW 103140581A TW 201609650 A TW201609650 A TW 201609650A
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- alkyl
- group
- halogen atoms
- halogen
- haloalkyl
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 241
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- JARYYMUOCXVXNK-CSLFJTBJSA-N validamycin A Chemical compound N([C@H]1C[C@@H]([C@H]([C@H](O)[C@H]1O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)CO)[C@H]1C=C(CO)[C@@H](O)[C@H](O)[C@H]1O JARYYMUOCXVXNK-CSLFJTBJSA-N 0.000 description 1
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- VRNFXUOQGOAQBZ-DYXAMGHASA-N veratrin Chemical compound C1[C@@H](C)CC[C@H]2[C@](O)(C)[C@@]3(O)[C@@H](O)C[C@@]4(O)[C@@H]5CC[C@H]6[C@]7(C)CC[C@H](OC(=O)C(\C)=C/C)[C@@]6(O)O[C@@]75C[C@@]4(O)[C@@H]3CN21.C1=C(OC)C(OC)=CC=C1C(=O)O[C@@H]1[C@@]2(O)O[C@@]34C[C@@]5(O)[C@H](CN6[C@@H](CC[C@H](C)C6)[C@@]6(C)O)[C@]6(O)[C@@H](O)C[C@@]5(O)[C@@H]4CC[C@H]2[C@]3(C)CC1 VRNFXUOQGOAQBZ-DYXAMGHASA-N 0.000 description 1
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- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 239000000664 voltage gated sodium channel blocking agent Substances 0.000 description 1
- BCEHBSKCWLPMDN-MGPLVRAMSA-N voriconazole Chemical compound C1([C@H](C)[C@](O)(CN2N=CN=C2)C=2C(=CC(F)=CC=2)F)=NC=NC=C1F BCEHBSKCWLPMDN-MGPLVRAMSA-N 0.000 description 1
- 229960004740 voriconazole Drugs 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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- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- DUBNHZYBDBBJHD-UHFFFAOYSA-L ziram Chemical compound [Zn+2].CN(C)C([S-])=S.CN(C)C([S-])=S DUBNHZYBDBBJHD-UHFFFAOYSA-L 0.000 description 1
- FJBGIXKIXPUXBY-UHFFFAOYSA-N {2-[3-(4-chlorophenyl)propyl]-2,4,4-trimethyl-1,3-oxazolidin-3-yl}(imidazol-1-yl)methanone Chemical compound C1=CN=CN1C(=O)N1C(C)(C)COC1(C)CCCC1=CC=C(Cl)C=C1 FJBGIXKIXPUXBY-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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Abstract
本發明係有關如式(I)之已知與新穎之苯烷基羧醯胺衍生物之用途
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其中結構元素係如說明書中指示之定義,其係用於控制線蟲與/或其他蠕蟲,特別指出現在農業與動物健康領域中者,並有關包含此等化合物之調配物,特別指農化調配物,及控制線蟲與蠕蟲之方法。本發明進一步係有關新穎之苯烷基羧醯胺衍生物、其製法、包含此等化合物之調配物、控制線蟲與蠕蟲之方法、及其作為害蟲控制劑(特別用為殺線蟲劑)之用途,及其作為對抗動物與人類之體內寄生蟲之殺蠕蟲劑之用途。
Description
本發明係有關一種以已知與新穎之苯烷基羧醯胺衍生物於控制線蟲與/或其他蠕蟲(特別指出現在農業與動物健康領域中者)上之用途、包含此等化合物之調配物(特別指農化調配物)、及控制線蟲與蠕蟲之方法。
本發明進一步係有關某些苯烷基羧醯胺衍生物、其製法、包含此等化合物之調配物、及其於農業與獸醫領域及需要處理害蟲之領域中之用途。該等化合物具有控制傷害植物之害蟲之活性;特別具有控制線蟲之活性。此外,該等化合物可作為對抗動物與人類之體內寄生蟲之殺蠕蟲劑。
線蟲會造成農業產物(包括食物與工業作物)之顯著損失,且係採用具有殺線蟲活性之化學化合物來防治。此等化合物應具有高度活性,對各種不同物種之線蟲具有廣譜活性,同時應對非標靶生物體沒有毒性。
在獸醫領域中,對所有市售殺蠕蟲劑產生抗性之問題已逐漸增加。因此極需要具有新穎之分子作用模式之殺體內寄生蟲劑。此等新穎活性成分應對廣譜蠕蟲及線蟲具有優異效力,同時不會對接受處理之脊椎動物產生任何不良毒性效應。殺體寄生蟲劑為用於防治或壓制動物或人類之體內寄生蟲之醫藥。
某些用於控制線蟲之N-2-(吡啶基)乙基-羧醯胺衍生物之用途已說明於WO2007/108483 A1與EP 2 132 987 A1。
某些羧醯胺作為殺寄生蟲劑之用途已說明於EP 1 997 800
A1、WO2012/118139 A1 WO2013/0676230 A1、WO2014/004064 A1、WO2014/034750 A1與WO2014/034751 A1。
此外,某些羧醯胺類說明於WO2013/064518 A1、
WO2013/064519 A1、WO2013/064520 A1、WO2013/064521 A1作為殺害蟲劑或說明於WO2013/064460 A1、WO2013/064461 A1與WO2013/120940 A2中作為殺線蟲劑。
現代之殺蠕蟲劑/殺線蟲劑必需符合許多要求,例如:與其
含量、效力持續期及其作用範圍及可能用途等相關方面。有關毒性及其與其他活性成份或調配輔劑之相容性問題亦如同活性成份所需之合成成本一般扮演某種角色。此外,還會發生抗性。基於所有此等理由,認為仍未完成新穎殺蠕蟲劑/殺線蟲劑之搜尋,仍然需要至少在各相關態樣上具有比已知化合物更改良性質之新穎化合物。
本發明之目的係提供一種可以在各種不同態樣中擴大殺害蟲劑範圍之化合物。特定言之,本發明之主題在於提供一種可作為殺線蟲劑使用之化合物,其具有令人滿意或改良之殺線蟲活性,尤其在相當低施用率下,具有高度選擇性及與栽種作物之高度相容性。本發明另一項特別主題為提供一種可作為殺體內寄生蟲劑使用之化合物,其具有對抗廣譜蠕蟲與線蟲之令人滿意或改良之殺蠕蟲活性,尤其在相當低劑量下,不會對接受處理之脊椎動物產生任何不良毒性效力。
本發明係有關一種式(I)化合物之用途
其中(具體實施例1-1)n 為0、1、2、3或4,其受到環中可用於連接取代基X之位置數量之限制,各X分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、羥基、胺基、-SH、-SF5、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C8-烷基、具有1至5個鹵原子之C1-C8-鹵烷基、C2-C8-烯基、C2-C8-炔基、C1-C8-烷基胺基、二-(C1-C8-烷基)胺基、C1-C8-烷氧基、具有1至5個鹵原子之C1-C8-鹵烷氧基、C2-C8-烯基氧、具有1至5個鹵原子之C2-C8-鹵烯基氧、C3-C8-炔基氧、具有1至5個鹵原子之C3-C8-鹵炔基氧、C3-C8-環烷基、具有1至5個鹵原子之C3-C8-鹵環烷基、C1-C8-烷基羰基、具有1至5個鹵原子之C1-C8-鹵烷基羰基、-CONH(C1-C8-烷基)、-CON(C1-C8-烷基)2、-CONH(OC1-C8-烷基)、-CON(OC1-C8-烷基)(C1-C8-烷基)、C1-C8-烷氧基羰基、具有1至5個鹵原子之C1-C8-鹵烷氧基羰基、C1-C8-烷基羰基氧、具有1至5個鹵原子之C1-C8-鹵烷基羰基氧、C1-C8-烷基羰基胺基、具有1至5個鹵原子之C1-C8-鹵烷基羰基胺基、-OCONH(C1-C8-烷基)、-OCON(C1-C8-烷基)2、-OCONH(OC1-C8-烷基)、-OCO(OC1-C8-烷基)、-S-C1-C8-烷基、具有1至5個鹵原子之-S-C1-C8-鹵烷基、-S(O)-C1-C8-烷基、具有1至5個鹵原子之-S(O)-C1-C8-鹵烷基、-S(O)2-C1-C8-烷基、具有1至5個鹵原子之-S(O)2-C1-C8-鹵烷基、
(C1-C6-烷氧基亞胺基)-C1-C6-烷基、(C2-C6-烯基氧亞胺基)-C1-C6-烷基、(C3-C6-炔基氧亞胺基)-C1-C6-烷基、(苯甲基氧亞胺基)-C1-C6-烷基、苯甲基氧、-S-苯甲基、苯甲基胺基、苯氧基、-S-苯基與苯基胺基,Q 代表芳香系或部份飽和或飽和之5-或6-員雜環,其包含1至4個選自N、S、與O且帶有取代基Ym之雜原子,m 為0、1、2、3或4,其受到Q中可用於連接取代基Y之位置數量之限制,與各Y分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、羥基、胺基、-SH、-SF5、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C8-烷基、具有1至5個鹵原子之C1-C8-鹵烷基、C2-C8-烯基、C2-C8-炔基、C1-C8-烷基胺基、二-(C1-C8-烷基)胺基、C1-C8-烷氧基、具有1至5個鹵原子之C1-C8-鹵烷氧基、C2-C8-烯基氧、具有1至5個鹵原子之C2-C8-鹵烯基氧、C3-C8-炔基氧、具有1至5個鹵原子之C3-C8-鹵炔基氧、C3-C8-環烷基、具有1至5個鹵原子之C3-C8-鹵環烷基、C1-C8-烷基羰基、具有1至5個鹵原子之C1-C8-鹵烷基羰基、-CONH(C1-C8-烷基)、-CON(C1-C8-烷基)2、-CONH(OC1-C8-烷基)、-CON(OC1-C8-烷基)(C1-C8-烷基)、-NH(C1-C8-烷基羰基)、C1-C8-烷氧基羰基、具有1至5個鹵原子之C1-C8-鹵烷氧基羰基、C1-C8-烷基羰基氧、具有1至5個鹵原子之C1-C8-鹵烷基羰基氧、C1-C8-烷基羰基胺基、具有1至5個鹵原子之C1-C8-鹵烷基羰基胺基、-OCONH(C1-C8-烷基)、-OCON(C1-C8-烷基)2、-OCONH(OC1-C8-烷基)、-OCO(OC1-C8-烷基)、-S-C1-C8-烷基、具有1至5個鹵原子
之-S-C1-C8-鹵烷基、-S(O)-C1-C8-烷基、具有1至5個鹵原子之-S(O)-C1-C8-鹵烷基、-S(O)2-C1-C8-烷基、具有1至5個鹵原子之-S(O)2-C1-C8-鹵烷基、-CH2-S-C1-C8-烷基、-CH2-S(O)-C1-C8-烷基、-CH2-S(O)2-C1-C8-烷基、(C1-C6-烷氧基亞胺基)-C1-C6-烷基、(C2-C6-烯基氧亞胺基)-C1-C6-烷基、(C3-C6-炔基氧亞胺基)-C1-C6-烷基、(苯甲基氧亞胺基)-C1-C6-烷基、苯甲基氧、-S-苯甲基、苯甲基胺基、苯氧基、-S-苯基與苯基胺基,R1、R2、R3與R4相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-SH、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C6-烷基、C2-C6-烯基、C2-C6-炔基、C1-C6-烷基胺基、二-(C1-C6-烷基)胺基、C1-C6-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、具有1至5個鹵原子之C1-C6-鹵烷基、具有1至5個鹵原子之C1-C6-鹵烷氧基、C2-C6-烯基氧、具有1至5個鹵原子之C2-C6-鹵烯基氧、C3-C6-炔基氧、具有1至5個鹵原子之C3-C6-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C6-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C6-烷基、C1-C6-烷基羰基、具有1至5個鹵原子之C1-C6-鹵烷基羰基、-CONH(C1-C6-烷基)、-CON(C1-C6-烷基)2、-CONH(OC1-C6-烷基)、-CON(OC1-C6-烷基)(C1-C6-烷基)、C1-C6-烷氧基羰基、具有1至5個鹵原子之C1-C6-鹵烷氧基羰基、-OC(O)-C1-C6-烷基、具有1至5個鹵原子之-OC(O)-C1-C6-鹵烷基、-NHC(O)-C1-C6-烷基、具有1至5個鹵原子之-NHC(O)-C1-C6-鹵烷基、-OCONH(C1-C6-烷基)、-OCON(C1-C6-烷基)2、-OCONH(OC1-C6-烷基)、OCO(OC1-C6-烷基)、-S-C1-C6-
烷基、具有1至5個鹵原子之-S-C1-C6-鹵烷基、-S(O)-C1-C6-烷基、具有1至5個鹵原子之-S(O)-C1-C6-鹵烷基、-S(O)2-C1-C6-烷基、具有1至5個鹵原子之-S(O)2-C1-C6-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,或R1與R2與其所鍵結之碳原子共同形成4-、5-或6-員碳環,且R3與R4相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-SH、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C6-烷基、C2-C6-烯基、C2-C6-炔基、C1-C6-烷基胺基、二-(C1-C6-烷基)胺基、C1-C6-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、具有1至5個鹵原子之C1-C6-鹵烷基、具有1至5個鹵原子之C1-C6-鹵烷氧基、C2-C6-烯基氧、具有1至5個鹵原子之C2-C6-鹵烯基氧、C3-C6-炔基氧、具有1至5個鹵原子之C3-C6-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C6-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C6-烷基、C1-C6-烷基羰基、具有1至5個鹵原子之C1-C6-鹵烷基羰基、-CONH(C1-C6-烷基)、-CON(C1-C6-烷基)2、-CONH(OC1-C6-烷基)、-CON(OC1-C6-烷基)(C1-C6-烷基)、C1-C6-烷氧基羰基、具有1至5個鹵原子之C1-C6-鹵烷氧基羰基、-OC(O)-C1-C6-烷基、具有1至5個鹵原子之-OC(O)-C1-C6-鹵烷基、-NHC(O)-C1-C6-烷基、具有1至5個鹵原子之-NHC(O)-C1-C6-鹵烷基、-OCONH(C1-C6-烷基)、-OCON(C1-C6-烷基)2、-OCONH(OC1-C6-烷基)、OCO(OC1-C6-烷基)、-S-C1-C6-
烷基、具有1至5個鹵原子之-S-C1-C6-鹵烷基、-S(O)-C1-C6-烷基、具有1至5個鹵原子之-S(O)-C1-C6-鹵烷基、-S(O)2-C1-C6-烷基、具有1至5個鹵原子之-S(O)2-C1-C6-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,或R3與R4與其所鍵結之碳原子共同形成3-、4-、5-或6-員碳環,且R1與R2相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-SH、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C6-烷基、C2-C6-烯基、C2-C6-炔基、C1-C6-烷基胺基、二-(C1-C6-烷基)胺基、C1-C6-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、具有1至5個鹵原子之C1-C6-鹵烷基、具有1至5個鹵原子之C1-C6-鹵烷氧基、C2-C6-烯基氧、具有1至5個鹵原子之C2-C6-鹵烯基氧、C3-C6-炔基氧、具有1至5個鹵原子之C3-C6-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C6-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C6-烷基、C1-C6-烷基羰基、具有1至5個鹵原子之C1-C6-鹵烷基羰基、-CONH(C1-C6-烷基)、-CON(C1-C6-烷基)2、-CONH(OC1-C6-烷基)、-CON(OC1-C6-烷基)(C1-C6-烷基)、C1-C6-烷氧基羰基、具有1至5個鹵原子之C1-C6-鹵烷氧基羰基、-OC(O)-C1-C6-烷基、具有1至5個鹵原子之-OC(O)-C1-C6-鹵烷基、-NHC(O)-C1-C6-烷基、具有1至5個鹵原子之-NHC(O)-C1-C6-鹵烷基、-OCONH(C1-C6-烷基)、-OCON(C1-C6-烷基)2、-OCONH(OC1-C6-烷基)、OCO(OC1-C6-烷基)、-S-C1-C6-
烷基、具有1至5個鹵原子之-S-C1-C6-鹵烷基、-S(O)-C1-C6-烷基、具有1至5個鹵原子之-S(O)-C1-C6-鹵烷基、-S(O)2-C1-C6-烷基、具有1至5個鹵原子之-S(O)2-C1-C6-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,或R2與R4與其所鍵結之碳原子共同形成5-或6-員非芳香系碳環,其可視需要經由1至4個C1-C8-烷基與1至4個鹵原子所組成群組中之取代基取代,且R1與R3相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-SH、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C6-烷基、C2-C6-烯基、C2-C6-炔基、C1-C6-烷基胺基、二-(C1-C6-烷基)胺基、C1-C6-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、具有1至5個鹵原子之C1-C6-鹵烷基、具有1至5個鹵原子之C1-C6-鹵烷氧基、C2-C6-烯基氧、具有1至5個鹵原子之C2-C6-鹵烯基氧、C3-C6-炔基氧、具有1至5個鹵原子之C3-C6-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C6-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C6-烷基、C1-C6-烷基羰基、具有1至5個鹵原子之C1-C6-鹵烷基羰基、-CONH(C1-C6-烷基)、-CON(C1-C6-烷基)2、-CONH(OC1-C6-烷基)、-CON(OC1-C6-烷基)(C1-C6-烷基)、C1-C6-烷氧基羰基、具有1至5個鹵原子之C1-C6-鹵烷氧基羰基、-OC(O)-C1-C6-烷基、具有1至5個鹵原子之-OC(O)-C1-C6-鹵烷基、-NHC(O)-C1-C6-烷基、具有1至5個鹵原子之-NHC(O)-C1-C6-鹵烷基、-OCONH(C1-C6-烷基)、
-OCON(C1-C6-烷基)2、-OCONH(OC1-C6-烷基)、OCO(OC1-C6-烷基)、-S-C1-C6-烷基、具有1至5個鹵原子之-S-C1-C6-鹵烷基、-S(O)-C1-C6-烷基、具有1至5個鹵原子之-S(O)-C1-C6-鹵烷基、-S(O)2-C1-C6-烷基、具有1至5個鹵原子之-S(O)2-C1-C6-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,或R1與R3與其所鍵結之碳原子共同形成5-或6-員非芳香系碳環,其可視需要經選自由1至4個C1-C8-烷基與1至4個鹵原子所組成群組中之取代基取代,且R2與R4相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-SH、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C6-烷基、C2-C6-烯基、C2-C6-炔基、C1-C6-烷基胺基、二-(C1-C6-烷基)胺基、C1-C6-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、具有1至5個鹵原子之C1-C6-鹵烷基、具有1至5個鹵原子之C1-C6-鹵烷氧基、C2-C6-烯基氧、具有1至5個鹵原子之C2-C6-鹵烯基氧、C3-C6-炔基氧、具有1至5個鹵原子之C3-C6-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C6-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C6-烷基、C1-C6-烷基羰基、具有1至5個鹵原子之C1-C6-鹵烷基羰基、-CONH(C1-C6-烷基)、-CON(C1-C6-烷基)2、-CONH(OC1-C6-烷基)、-CON(OC1-C6-烷基)(C1-C6-烷基)、C1-C6-烷氧基羰基、具有1至5個鹵原子之C1-C6-鹵烷氧基羰基、-OC(O)-C1-C6-烷基、具有1至5個鹵原子之-OC(O)-C1-C6-鹵烷基、
-NHC(O)-C1-C6-烷基、具有1至5個鹵原子之-NHC(O)-C1-C6-鹵烷基、-OCONH(C1-C6-烷基)、-OCON(C1-C6-烷基)2、-OCONH(OC1-C6-烷基)、OCO(OC1-C6-烷基)、-S-C1-C6-烷基、具有1至5個鹵原子之-S-C1-C6-鹵烷基、-S(O)-C1-C6-烷基、具有1至5個鹵原子之-S(O)-C1-C6-鹵烷基、-S(O)2-C1-C6-烷基、具有1至5個鹵原子之-S(O)2-C1-C6-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,R5 係選自下列所組成之群組中:氫、氰基、-CHO、-OH、C1-C6-烷基、具有1至5個鹵原子之C1-C6-鹵烷基、C1-C6-烷氧基、具有1至5個鹵原子之C1-C6-鹵烷氧基、C3-C7-環烷基、具有1至5個鹵原子之C3-C7-鹵環烷基、C3-C7-環烷基-C1-C6-烷基、-CONH(C1-C6-烷基)、C2-C6-烯基、C2-C6-炔基、C1-C6-烷氧基-C1-C6-烷基、C3-C7-環烷基-C1-C6-烷基、氰基-C1-C6-烷基、胺基-C1-C6-烷基、C1-C6-烷基胺基-C1-C6-烷基、二-(C1-C6-烷基)胺基-C1-C6-烷基、C1-C6-烷基羰基、具有1至5個鹵原子之C1-C6-鹵烷基羰基、C1-C6-烷氧基羰基、C1-C6-苯甲基氧羰基、C1-C6-烷氧基-C1-C6-烷基羰基、-S-C1-C6-烷基、具有1至5個鹵原子之-S-C1-C6-鹵烷基、-S(O)2-C1-C6-烷基、與具有1至5個鹵原子之-S(O)2-C1-C6-鹵烷基,A 代表式(A1)苯基
其中
o 為0、1、2、3、4或5,與各R 分別獨立選自下列所組成之群組中:鹵素、硝基、-OH、NH2、SH、SF5、CHO、OCHO、NHCHO、COOH、氰基、C1-C8-烷基、具有1至9個鹵原子之C1-C8-鹵烷基、C2-C8-烯基、C2-C8-炔基、C3-C6-環烷基、-S-C1-C8-烷基、具有1至5個鹵原子之-S-C1-C8-鹵烷基、C1-C8-烷氧基、具有1至5個鹵原子之C1-C8-鹵烷氧基、C1-C8-烷氧基-C2-C8-烯基、C1-C8-烷氧基羰基、具有1至5個鹵原子之C1-C8-鹵烷氧基羰基、C1-C8-烷基羰基氧、具有1至5個鹵原子之C1-C8-鹵烷基羰基氧、-S(O)-C1-C8-烷基、具有1至5個鹵原子之-S(O)-C1-C8-鹵烷基、-S(O)2-C1-C8-烷基、具有1至5個鹵原子之-S(O)2-C1-C8-鹵烷基、C1-C8-烷基磺醯胺、-NH(C1-C8-烷基)、N(C1-C8-烷基)2、苯基(可視需要經C1-C6-烷氧基取代)與苯氧基,或兩個鍵結在相鄰碳原子上之R共同代表-O(CH2)pO-,其中p代表1或2,或A 代表式(Het-1)雜環
其中R6與R7可相同或相異,且係選自下列所組成之群組中:氫、鹵素、胺基、硝基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R8 係選自下列所組成之群組中:氫、鹵素、硝基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-2)雜環
其中R9 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R10與R11可相同或相異,且係選自下列所組成之群組中:氫、鹵素、胺基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-3)雜環
其中R12 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R13 係選自下列所組成之群組中:氫、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-4)雜環
其中R14與R15可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、-S-C1-C4-烷基、-S(O)2-C1-C4-烷基、苯基(可視需要經鹵素或C1-C4-烷基取代)與吡
啶基(可視需要經鹵素或C1-C4-烷基取代),及R16係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,或A 代表式(Het-5)雜環
其中R17與R18可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、C1-C4-烷基氧與具有1至5個鹵原子之C1-C4-鹵烷基,及R19 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-6)雜環
其中R20 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R21與R23可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R22 係選自下列所組成之群組中:氫、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基-C1-C4-烷基、羥基-C1-C4-
烷基、-S(O)2-C1-C4-烷基、-S(O)2-N(C1-C4-烷基)2、C1-C6-烷基羰基、-S(O)2-苯基(可視需要經鹵素或C1-C4-烷基取代)與苯甲醯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-7)雜環
其中R24 係選自下列所組成之群組中:氫、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基-C1-C4-烷基、羥基-C1-C4-烷基、-S(O)2-C1-C4-烷基、-S(O)2-N(C1-C4-烷基)2、C1-C6-烷基羰基、-S(O)2-苯基(可視需要經鹵素或C1-C4-烷基取代)與苯甲醯基(可視需要經鹵素或C1-C4-烷基取代),及R25、R26與R27可相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與C1-C4-烷基羰基,或A 代表式(Het-8)雜環
其中R28 係選自下列所組成之群組中:氫與C1-C4-烷基,及R29 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-9)雜環
其中R30 係選自下列所組成之群組中:氫與C1-C4-烷基,及R31 係選自下列所組成之群組中:鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-10)雜環
其中R32 係選自下列所組成之群組中:氫、鹵素、胺基、氰基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),及R33 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基、具有1至9個鹵原子之C1-C5-鹵烷氧基、胺基、經取代或未經取代之C1-C5-烷基胺基或經取代或未經取代之二-(C1-C5-烷基)-胺基,或A 代表式(Het-11)雜環
其中R34 係選自下列所組成之群組中:氫、鹵素、胺基、氰基、C1-C4-烷基
胺基、二-(C1-C4-烷基)胺基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R35 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-12)雜環
其中R36 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、胺基羰基與胺基羰基-C1-C4-烷基,及R37 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、C1-C4-烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、與-S(O)2-C1-C4-烷基,及R38 係選自下列所組成之群組中:氫、苯基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、羥基-C1-C4-烷基、C2-C6-烯基、C3-C6-環烷基、C1-C4-烷基硫-C1-C4-烷基、C1-C4-烷基-S(O)-C1-C4-烷基、C1-C4-烷基-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基硫-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基-C1-C4-烷基,或A 代表式(Het-13)雜環
其中R39 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、胺基羰基與胺基羰基-C1-C4-烷基,及R40 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、與-S(O)2-C1-C4-烷基,及R41 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、羥基-C1-C4-烷基、C2-C6-烯基、C3-C6-環烷基、C1-C4-烷基硫-C1-C4-烷基、C1-C4-烷基-S(O)-C1-C4-烷基、C1-C4-烷基-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基硫-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基-C1-C4-烷基與苯基(可視需要經鹵素、C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基或硝基取代),或A 代表式(Het-14)雜環
其中
R42 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、胺基羰基與胺基羰基-C1-C4-烷基,及R43 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、C1-C4-烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、與具有1至5個鹵原子之C1-C4-鹵烷基,及R44 係選自下列所組成之群組中:氫、苯基、苯甲基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、羥基-C1-C4-烷基、C2-C6-烯基、C3-C6-環烷基、C1-C4-烷基硫-C1-C4-烷基、C1-C4-烷基-S(O)-C1-C4-烷基、C1-C4-烷基-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基硫-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基-C1-C4-烷基,或A 代表式(Het-15)雜環
其中R45與R46可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-16)雜環
其中R47與R48可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、苯基(可視需要經鹵素或C1-C4-烷基取代)、與雜環基,如:吡啶基、嘧啶基與噻二唑基(各可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-17)雜環
其中R49與R50可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-18)雜環
其中R51 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-19)雜環
其中R52 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵
原子之C1-C4-鹵烷基,及R53 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-20)雜環
其中R54 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-21)雜環
其中R55 係選自下列所組成之群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,及R56、R57與R58,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基與-S(O)2-C1-C4-烷基,或A 代表式(Het-22)雜環
其中R59 係選自下列所組成之群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4烷氧基、-S-C1-C5-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、-S-C2-C5-烯基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、苯基氧(可視需要經鹵素或C1-C4-烷基取代)與-S-苯基(可視需要經鹵素或C1-C4-烷基取代),及R60、R61與R62,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、N-嗎啉(可視需要經鹵素或C1-C4-烷基取代)、與噻吩基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-23)雜環
其中R63、R64、R65與R66,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原
子之-S-C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基與-S(O)2-C1-C4-烷基,或A 代表式(Het-24)雜環
其中R67 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R68 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C6-烷氧基羰基、苯甲基(可視需要經1至3個鹵原子取代)、苯甲基氧羰基(可視需要經1至3個鹵原子取代)、與雜環基,如:吡啶基與嘧啶基(各可視需要經鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基取代),或A 代表式(Het-25)雜環
其中R69 係選自下列所組成之群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,及R70 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、與苯甲基,或
A 代表式(Het-26)雜環
其中X1 係選自下列所組成之群組中:硫、-SO-、-SO2-與-CH2-,及R71 係選自下列所組成之群組中:C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R72與R73可相同或相異,且係選自下列所組成之群組中:氫與C1-C4-烷基,或A 代表式(Het-27)雜環
其中R74 係選自下列所組成之群組中:C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-28)雜環
其中R75 係選自下列所組成之群組中:C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-29)雜環
其中R76 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,其係用於控制線蟲與/或其他蠕蟲。
式(Het-1)至(Het-29)中,#代表式(I)化合物中連接A至C(O)NR5-部份基團之鍵結。通常,本申請案中,除非另有說明,否則#代表結構元素之連接鍵。
根據本發明任何化合物均可依該化合物中不對稱中心之數量決定,而呈一或多種光學或對掌性異構型。本發明因此同樣係有關所有光學異構物及其消旋或部份消旋混合物(術語"部份消旋"係指不同比例之對映異構物之混合物)及所有可能之立體異構物依所有比例形成之混合物。非對映異構物與/或光學異構物可由熟悉此相關技術者依據本身已知之方式分離。
本發明亦有關式(I)化合物之鹽類、N-氧化物、金屬錯合物與類金屬錯合物,及其用途。
本發明化合物亦可依化合物中雙鍵數量而定,而呈一或多種幾何異構型,尤指所有同側/反側(或順式/反式)異構物及其所有可能之同側/反側(或順式/反式)混合物。本發明因此同樣有關所有幾何異構物及其依所有比例形成之所有可能混合物。熟悉此相關技術者可依據本身已知之一般方法分離幾何異構物。
式(I)化合物可能因羥基、氫硫基或胺基之質子位移而呈其互變異構型。此等化合物之此等互變異構型亦為本發明之一部份。更一般而言,式(I)化合物之所有互變異構型及可視需要作為製程中間物使用之化合物(其定義將說明於此等製法中)之所有互變異構型亦屬於本發明之一部
份。
本文所採用術語“包含”、“含有”、“包括”、“涵括”、“有”、“具有”、“含”、“內含”、“特徵在於”或其任何其他變化術語均希望涵蓋非獨一性之涵括範圍,除非有明確指示之任何限制條件。例如:包含所列出元件之組成物、混合物、製程或方法不一定限制於彼等元件,反而可能包括此等組成物、混合物、製程或方法沒有列出或固有之其他元件。
連接語“由....組成”不包括未明確說明之任何元件、步驟或成份。若申請專利範圍中出現此等用語,則申請專利範圍僅限於其所陳述者及通常與其相關之雜質,且不包括其他部分。當片語“由....組成”出現在請求主文之子句中而非緊接在前言之後時,其則僅限制子句中指示之元件;申請專利範圍並未完全排除其他元件。
連接語“基本上由....組成”係用於界定該組成物或方法中除了彼等逐字揭示者外尚包括之材料、步驟、特色、組份或元件,但其限制條件為該等材料、步驟、特色、組份或元件不能實質影響該申請專利權之發明之基本與新穎特徵(群)。術語“基本上由....組成”係介於“包含”與“由....組成”之間之中間立場。
當申請者以開放之術語如:“包含”來界定本發明或其一部份時,應瞭解(除非另有說明)該說明應可解讀為亦採用“基本上由....組成”或“由....組成”來說明此發明。
此外,除非另有說明,否則“或”係指包容性的”或”,並非”排他性”的“或”。例如:下列任一項均可滿足條件A或B:A為真(或存在)與B為偽(或不存在)、A為偽(或不存在)與B為真(或存在),及A與B二者均為為真(或存在)。
此外,在本發明元件或組份之前的定冠詞“一”與“該”係指沒
有限定該元件或組份之出現(亦即發生)次數。因此“一”與“該”應解讀為包括一個或至少一個,且該元件或組份之單數型亦包括複數型,除非該數字顯然意指單數。
上文中單獨使用或組合使用(如:“鹵烷基”)之術語“烷基”,包括直鏈或分支烷基,如:甲基、乙基、正丙基、異丙基,或不同之丁基、戊基或己基異構物。“烯基”包括直鏈或分支烯基,如:乙烯基、1-丙烯基、2-丙烯基,與不同之丁烯基、戊烯基與己烯基異構物。“烯基”亦包括聚烯基,如:1,2-丙二烯基與2,4-己二烯基。“炔基”包括直鏈或分支炔基,如:乙炔基、1-丙炔基、2-丙炔基與不同之丁炔基、戊炔基與己炔基異構物。“炔基”亦包括由多重參鍵組成之部份基團,如:2,5-己二炔基。
“烷氧基”包括例如:甲氧基、乙氧基、正丙基氧、異丙基氧與不同之丁氧基、戊氧基與己基氧異構物。“烷氧基烷基”代表烷氧基取代在烷基上。“烷氧基烷基”實例包括CH3OCH2、CH3OCH2CH2、CH3CH2OCH2、CH3CH2CH2CH2OCH2與CH3CH2OCH2CH2。
“環烷基”包括例如:環丙基、環丁基、環戊基與環己基。術語“環烷基烷基”代表環烷基取代在烷基部份基團上。“環烷基烷基”實例包括環丙基甲基、環戊基乙基、與其他鍵結在直鏈或分支烷基上之環烷基部份基團。“環烯基”包括下列基團,如:環戊烯基與環己烯基,及包含超過一個雙鍵之基團,如:1,3-與1,4-環己二烯基。術語“環烷基環烷基”代表環烷基取代在另一個環烷基環上,其中各環烷基環分別獨立具有3至7個碳原子環組員。環烷基環烷基實例包括環丙基環丙基(如:1,1'-雙環丙-1-基、1,1'-雙環丙-2-基)、環己基環戊基(如:4-環戊基環己基)與環己基環己基(如:1,1'-雙環己-1-基),與不同之順式-與反式-環烷基環烷基異構物(如:(1R,2S)-1,1’-雙環丙-2-基與(1R,2R)-1,1’-雙環丙-2-基)。
單獨使用或組合使用(如:“鹵烷基”),或在敘述時使用(如:“經鹵素取代之烷基”)之術語“鹵素”包括氟、氯、溴或碘。此外,當組合使用(如:“鹵烷基”)或在敘述時使用(如:“經鹵素取代之烷基”),該烷基可能經相同或相異鹵原子部份或完全取代。“鹵烷基”或“經鹵素取代之烷基”之實例包括F3C、ClCH2、CF3CH2與CF3CCl2。術語“鹵烷氧基”、“鹵烯基”、“鹵炔基”,等等均具有類似術語“鹵烷基”之定義。“鹵烷氧基”實例包括CF3O、CCl3CH2O、HCF2CH2CH2O與CF3CH2O。“鹵烯基”實例包括(Cl)2C=CHCH2與CF3CH2CH=CHCH2。“鹵炔基”實例包括HC≡CCHCl、CF3C≡C、CCl3C≡C與FCH2C≡CCH2。
本文所採用化學縮語C(O)代表羰基部份基團。例如:C(O)CH3代表乙醯基。本文所採用化學縮語CO2與C(O)O代表酯部份基團。例如:CO2Me與C(O)OMe代表甲酯。CHO代表醛部份基團。
“OCN”意指-O-C≡N,及“SCN”意指-S-C≡N。
取代基中碳原子總數係以字首“Ci-Cj”表示,其中i與j為數字1至14。C2烷氧基烷基係指CH3OCH2;C3烷氧基烷基係指例如:CH3CH(OCH3)、CH3OCH2CH2或CH3CH2OCH2;及C4烷氧基烷基係指共包含4個碳原子之經烷氧基取代之烷基之各種不同異構物,其實例包括CH3CH2CH2OCH2與CH3CH2OCH2CH2。
當化合物經帶有下標之取代基取代且該下標指示該取代基之數量可超過1時,該等取代基(當超過1個時)係分別獨立選自所定義之取代基群組中,例如:n=0、1、2、3或4。當該基團包含之取代基可為氫時,例如:R2或R3,則當此取代基為氫時,咸瞭解其等同該基團未經取代。
除非另有說明,否則作為式(I)之組份之“環”或“環系”為碳環或雜環。術語“環系”代表兩個或更多個稠合環。術語“雜環”代表環中至少一
個形成環主幹之原子不為碳,例如:氮、氧或硫。通常,雜環包含不超過4個氮、不超過2個氧及不超過2個硫。除非另有說明,否則雜環可為飽和、部份不飽和、或完全不飽和環。術語“雜環系”代表該環系中至少一個環為雜環之環系。除非另有說明,否則雜環與環系可以利用任何可利用之碳或氮,置換該碳或氮上之氫來附接。
除非另有說明,否則本文將採用下列定義。術語“可視需要經取代”係與片語“經取代或未經取代”或與術語“(未)經取代”交換使用。“可視需要經1至4個取代基取代”之敘述意指沒有取代基(亦即未經取代)或有1、2、3或4個取代基(其受到可利用之鍵結位置數量之限制)。除非另有說明,否則可視需要經取代之基團可能在該基團可取代之各位置上具有一個取代基,且各取代基彼此分別獨立。
一項個別具體實施例(具體實施例1-2)中,式(I)化合物之結構元素係如下列定義:n 係如具體實施例1-1中之定義,各X 係如具體實施例1-1中之定義,Q 代表芳香系或部份飽和或飽和之5-或6-員雜環,其包含1至4個選自N、S與O且帶有取代基Ym之雜原子,m 為0、1、2、3或4,其受到Q中可用於連接取代基Y之位置數量之限制,與各Y 分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、羥基、胺基、-SH、-SF5、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C8-烷基、具有1至5個鹵原子之C1-C8-鹵烷基、C2-C8-烯基、C2-C8-炔基、C1-C8-烷基胺基、二-(C1-C8-烷基)胺基、C1-C8-烷氧基、具有1至5個鹵原
子之C1-C8-鹵烷氧基、C2-C8-烯基氧、具有1至5個鹵原子之C2-C8-鹵烯基氧、C3-C8-炔基氧、具有1至5個鹵原子之C3-C8-鹵炔基氧、C3-C8-環烷基、具有1至5個鹵原子之C3-C8-鹵環烷基、C1-C8-烷基羰基、具有1至5個鹵原子之C1-C8-鹵烷基羰基、-CONH(C1-C8-烷基)、-CON(C1-C8-烷基)2、-CONH(OC1-C8-烷基)、-CON(OC1-C8-烷基)(C1-C8-烷基)、-NH(C1-C8-烷基羰基)、C1-C8-烷氧基羰基、具有1至5個鹵原子之C1-C8-鹵烷氧基羰基、C1-C8-烷基羰基氧、具有1至5個鹵原子之C1-C8-鹵烷基羰基氧、C1-C8-烷基羰基胺基、具有1至5個鹵原子之C1-C8-鹵烷基羰基胺基、-OCONH(C1-C8-烷基)、-OCON(C1-C8-烷基)2、-OCONH(OC1-C8-烷基)、-OCO(OC1-C8-烷基)、-S-C1-C8-烷基、具有1至5個鹵原子之-S-C1-C8-鹵烷基、-S(O)-C1-C8-烷基、具有1至5個鹵原子之-S(O)-C1-C8-鹵烷基、-S(O)2-C1-C8-烷基、具有1至5個鹵原子之-S(O)2-C1-C8-鹵烷基、-CH2-S-C1-C8-烷基、-CH2-S(O)-C1-C8-烷基、-CH2-S(O)2-C1-C8-烷基、(C1-C6-烷氧基亞胺基)-C1-C6-烷基、(C2-C6-烯基氧亞胺基)-C1-C6-烷基、(C3-C6-炔基氧亞胺基)-C1-C6-烷基、(苯甲基氧亞胺基)-C1-C6-烷基、苯甲基氧、-S-苯甲基、苯甲基胺基、苯氧基、-S-苯基與苯基胺基,R1、R2、R3與R4相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-SH、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C6-烷基、C2-C6-烯基、C2-C6-炔基、C1-C6-烷基胺基、二-(C1-C6-烷基)胺基、C1-C6-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、具有1至5個鹵原子之C1-C6-鹵烷基、具有1至5個鹵原子之C1-C6-鹵烷氧基、C2-C6-烯基氧、具有1至5個鹵原子之C2-C6-鹵烯基氧、
C3-C6-炔基氧、具有1至5個鹵原子之C3-C6-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C6-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C6-烷基、C1-C6-烷基羰基、具有1至5個鹵原子之C1-C6-鹵烷基羰基、-CONH(C1-C6-烷基)、-CON(C1-C6-烷基)2、-CONH(OC1-C6-烷基)、-CON(OC1-C6-烷基)(C1-C6-烷基)、C1-C6-烷氧基羰基、具有1至5個鹵原子之C1-C6-鹵烷氧基羰基、-OC(O)-C1-C6-烷基、具有1至5個鹵原子之-OC(O)-C1-C6-鹵烷基、-NHC(O)-C1-C6-烷基、具有1至5個鹵原子之-NHC(O)-C1-C6-鹵烷基、-OCONH(C1-C6-烷基)、-OCON(C1-C6-烷基)2、-OCONH(OC1-C6-烷基)、OCO(OC1-C6-烷基)、-S-C1-C6-烷基、具有1至5個鹵原子之-S-C1-C6-鹵烷基、-S(O)-C1-C6-烷基、具有1至5個鹵原子之-S(O)-C1-C6-鹵烷基、-S(O)2-C1-C6-烷基、具有1至5個鹵原子之-S(O)2-C1-C6-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,其限制條件為R1為氟與/或R2為氟,R5 係如具體實施例1-1中之定義,及A 係如具體實施例1-1中之定義,其限制條件為Het-21中,R55不為CF3。
具體實施例1-1之另一項個別態樣中,R1為氟。具體實施例1-1之另一項個別態樣中,R2為氟。具體實施例1-1之另一項個別態樣中,R1為氟及R2為氟。具體實施例1-1之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例1-1之另一項個別態樣中,R1/R2組合為氟/氫。
具體實施例1-2之另一項個別態樣中,R1為氟。具體實施例1-2之另一項個別態樣中,R2為氟。具體實施例1-2之另一項個別態樣中,R1為氟及R2為氟。具體實施例1-2之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例1-2之另一項個別態樣中,R1/R2組合為氟/氫。
具體實施例1-1與1-2及該等具體實施例之各個別態樣中,Q較佳係代表選自Q-1至Q-64所組成群組中之可視需要經單-或多取代之雜芳香環(具體實施例1-1a與1-2a):
式(I)化合物中述及結構元素之較佳取代基或範圍說明如下(具體實施例2-1)。
n 為1或2,其受到環中可用於連接取代基X之位置數量之限制,各X 分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基羰基、
-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、C1-C4-烷基羰基氧、具有1至5個鹵原子之C1-C4-鹵烷基羰基氧、C1-C4-烷基羰基胺基、具有1至5個鹵原子之C1-C4-鹵烷基羰基胺基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、-OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、(C1-C4-烷氧基亞胺基)-C1-C4-烷基、(C2-C6-烯基氧亞胺基)-C1-C4-烷基、(C3-C6-炔基氧亞胺基)-C1-C4-烷基、(苯甲基氧亞胺基)-C1-C6-烷基、苯甲基氧、-S-苯甲基、苯甲基胺基、苯氧基、-S-苯基與苯基胺基,Q 代表可視需要經單-或多取代之雜芳香環,其選自下列各物所組成群組中:Q-1、Q-2、Q-3、Q-4、Q-5、Q-6、Q-7、Q-8、Q-9、Q-10、Q-11、Q-12、Q-13、Q-14、Q-15、Q-16、Q-17、Q-18、Q-19、Q-20、Q-21、Q-22、Q-23、Q-24、Q-25、Q-26、Q-27、Q-28、Q-29、Q-30、Q-31、Q-32、Q-33、Q-34、Q-35、Q-36、Q-37、Q-38、Q-39、Q-40、Q-41、Q-42、Q-43、Q-44、Q-45、Q-46、Q-47、Q-48、Q-49、Q-50、Q-51、Q-52、Q-53、Q-54、Q-55、Q-56、Q-57、Q-58、Q-59、Q-60、Q-61、Q-62、Q-63與Q-64其中m 為0、1或2,其受到Q中可用於連接取代基Y之位置數量之限制,與各Y 分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、
C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基羰基、-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、-NH(C1-C4-烷基羰基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、C1-C4-烷基羰基氧、具有1至5個鹵原子之C1-C4-鹵烷基羰基氧、C1-C4-烷基羰基胺基、具有1至5個鹵原子之C1-C4-鹵烷基羰基胺基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、-OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、-CH2-S-C1-C4-烷基、-CH2-S(O)-C1-C4-烷基、-CH2-S(O)2-C1-C4-烷基、(C1-C4-烷氧基亞胺基)-C1-C4-烷基、(C2-C6-烯基氧亞胺基)-C1-C4-烷基、(C3-C6-炔基氧亞胺基)-C1-C4-烷基、(苯甲基氧亞胺基)-C1-C6-烷基、苯甲基氧、-S-苯甲基、苯甲基胺基、苯氧基、-S-苯基與苯基胺基,R1、R2、R3與R4相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-CHO、-COOH、-CONH2、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷基、具有1至5個
鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C3-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C3-烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基羰基、-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、-OC(O)-C1-C4-烷基、具有1至5個鹵原子之-OC(O)-C1-C4-鹵烷基、-NHC(O)-C1-C4-烷基、具有1至5個鹵原子之-NHC(O)-C1-C4-鹵烷基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,或R1與R2與其所鍵結之碳原子共同形成4-或5-員碳環,且R3與R4相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-CHO、-COOH、-CONH2、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具
有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C3-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C3-烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基羰基、-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、-OC(O)-C1-C4-烷基、具有1至5個鹵原子之-OC(O)-C1-C4-鹵烷基、-NHC(O)-C1-C4-烷基、具有1至5個鹵原子之-NHC(O)-C1-C4-鹵烷基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,或R3與R4與其所鍵結之碳原子共同形成3-、4-或5-員碳環,且R1與R2相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-CHO、-COOH、-CONH2、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C3-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C3-烷基、C1-C4-
烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基羰基、-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、-OC(O)-C1-C4-烷基、具有1至5個鹵原子之-OC(O)-C1-C4-鹵烷基、-NHC(O)-C1-C4-烷基、具有1至5個鹵原子之-NHC(O)-C1-C4-鹵烷基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,或R2與R4與其所鍵結之碳原子共同形成5-員非芳香系碳環,其可視需要經選自由1至4個C1-C4-烷基與1至4個鹵原子所組成群組中之取代基取代,且R1與R3相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-CHO、-COOH、-CONH2、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C3-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C3-烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基
羰基、-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、-OC(O)-C1-C4-烷基、具有1至5個鹵原子之-OC(O)-C1-C4-鹵烷基、-NHC(O)-C1-C4-烷基、具有1至5個鹵原子之-NHC(O)-C1-C4-鹵烷基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,或R1與R3與其所鍵結之碳原子共同形成5-員非芳香系碳環,其可視需要經選自由1至4個C1-C4-烷基與1至4個鹵原子所組成群組中之取代基取代,且R2與R4相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-CHO、-COOH、-CONH2、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C3-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C3-烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基羰基、-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-
烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、-OC(O)-C1-C4-烷基、具有1至5個鹵原子之-OC(O)-C1-C4-鹵烷基、-NHC(O)-C1-C4-烷基、具有1至5個鹵原子之-NHC(O)-C1-C4-鹵烷基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,R5 係選自下列所組成之群組中:氫、-CHO、-OH、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷氧基-C1-C4-烷基、C3-C6-環烷基-C1-C3-烷基、氰基-C1-C4-烷基、胺基-C1-C4-烷基、C1-C4-烷基胺基-C1-C4-烷基、二-(C1-C4-烷基)胺基-C1-C4-烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基羰基、C1-C4-烷氧基羰基、苯甲基氧羰基、C1-C4-烷氧基-C1-C4-烷基羰基、-S(O)2-C1-C4-烷基、與具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基,A 代表式(A1)苯基
其中
o 為0、1或2,及各R 分別獨立選自下列所組成之群組中:鹵素、硝基、-OH、CHO、OCHO、NHCHO、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C2-C4-烯基、C2-C4-炔基、C3-C6-環烷基、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C1-C4-烷氧基-C2-C4-烯基、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、C1-C4-烷基羰基氧、具有1至5個鹵原子之C1-C4-鹵烷基羰基氧、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、C1-C4-烷基磺醯胺、-NH(C1-C4-烷基)、N(C1-C4-烷基)2、苯基(可視需要經C1-C4-烷氧基取代)與苯氧基,或兩個鍵結在相鄰碳原子上之R共同代表-O(CH2)pO-,其中p代表1或2,或A 代表式(Het-1)雜環
其中R6與R7可相同或相異,且係選自下列所組成之群組中:氫、鹵素、硝基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R8 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-2)雜環
其中R9 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R10與R11可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基、苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-4)雜環
其中R14與R15可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、-S-C1-C4-烷基、-S(O)2-C1-C4-烷基、苯基(可視需要經鹵素或C1-C4-烷基取代)與吡啶基(可視需要經鹵素或C1-C4-烷基取代),及R16係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,或A 代表式(Het-5)雜環
其中
R17與R18可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、C1-C4-烷基氧與具有1至5個鹵原子之C1-C4-鹵烷基,及R19 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-6)雜環
其中R20 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R21與R23可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R22 係選自下列所組成之群組中:氫、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基-C1-C4-烷基,或A 代表式(Het-7)雜環
其中R24 係選自下列所組成之群組中:氫、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基-C1-C4-烷基、C1-C6-烷基羰基,或苯甲醯基(可視需要經鹵素或C1-C4-烷基取代),及
R25、R26與R27 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與C1-C4-烷基羰基,或A 代表式(Het-9)雜環
其中R30 係選自下列所組成之群組中:氫與C1-C4-烷基,及R31 係選自下列所組成之群組中:鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-10)雜環
其中R32 係選自下列所組成之群組中:氫、鹵素、胺基、氰基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),及R33 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基、包含1至9個鹵原子之C1-C5-鹵烷氧基、胺基、經取代或未經取代之C1-C5-烷基胺基或經取代或未經取代之二-(C1-C5-烷基)-胺基,或A 代表式(Het-11)雜環
其中R34 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R35 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-12)雜環
其中R36 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基與具有1至5個鹵原子之-S-C1-C4-鹵烷基,及R37 係選自下列各物所組成群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、C1-C4-烷氧基與-S-C1-C4-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基,及R38 係選自下列所組成之群組中:苯基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、羥基-C1-C4-烷基、C2-C6-烯基、C3-C6-環烷基、C1-C4-烷基硫-C1-C4-烷基、C1-C4-烷基-S(O)-C1-C4-烷基、C1-C4-烷基-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基硫
-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基-C1-C4-烷基,或A 代表式(Het-13)雜環
其中R39 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、胺基羰基與胺基羰基-C1-C4-烷基,及R40 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基,與-S(O)2-C1-C4-烷基,及R41 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、羥基-C1-C4-烷基、C2-C6-烯基、C3-C6-環烷基、C1-C4-烷基硫-C1-C4-烷基、C1-C4-烷基-S(O)-C1-C4-烷基、C1-C4-烷基-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基硫-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基-C1-C4-烷基與苯基(其可視需要經鹵素、C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基或硝基取代),或A 代表式(Het-14)雜環
其中R42 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、與-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、胺基羰基與胺基羰基-C1-C4-烷基,及R43 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、C1-C4-烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、與-S(O)2-C1-C4-烷基、與具有1至5個鹵原子之C1-C4-鹵烷基,及R44 係選自下列所組成之群組中:苯基、苯甲基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、羥基-C1-C4-烷基、C2-C6-烯基、C3-C6-環烷基、C1-C4-烷基硫-C1-C4-烷基、C1-C4-烷基-S(O)-C1-C4-烷基、C1-C4-烷基-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基硫-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基-C1-C4-烷基,或A 代表式(Het-15)雜環
其中R45與R46 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或
A 代表式(Het-16)雜環
其中R47與R48 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、苯基(可視需要經鹵素或C1-C4-烷基取代),或雜環基,如:吡啶基、嘧啶基與噻二唑基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-17)雜環
其中R49與R50 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-19)雜環
其中R52 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R53 係選自下列所組成之群組中:C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),或
A 代表式(Het-20)雜環
其中R54 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-21)雜環
其中R55 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,及R56、R57與R58,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、氟基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基與-S(O)2-C1-C4-烷基,或A 代表式(Het-22)雜環
其中R59 係選自下列所組成之群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4烷氧基、-S-C1-C5-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、-S-C2-C5-烯基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、苯基氧(可視需要經鹵素或C1-C4-烷基取代)與-S-苯基(可視需要經鹵素或C1-C4-烷基取代),及R60、R61與R62,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、N-嗎啉(可視需要經鹵素或C1-C4-烷基取代)與噻吩基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-23)雜環
其中R63、R64、R65與R66,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基與-S(O)2-C1-C4-烷基,或A 代表式(Het-24)雜環
其中R67 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R68 係選自下列所組成之群組中:C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C6-烷氧基羰基、苯甲基(可視需要經1至3個鹵原子取代)、苯甲基氧羰基(可視需要經1至3個鹵原子取代)與雜環基,如:嘧啶基(可視需要經鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基取代),或A 代表式(Het-25)雜環
其中R69 係選自下列所組成之群組中:氫、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R70 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯甲基,或A 代表式(Het-26)雜環
其中X1 係選自下列所組成之群組中:硫、-SO-,或-SO2-,及
R71 係選自下列所組成之群組中:C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R72與R73可相同或相異,且係選自下列所組成之群組中:氫與C1-C4-烷基,或A 代表式(Het-29)雜環
其中R76 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基。
另一項個別之具體實施例(具體實施例2-2)中,式(I)化合物中結構元素較佳係如下列定義:n 係如具體實施例2-1中之定義,各X係如具體實施例2-1中之定義,Q 代表可視需要經單-或多取代之雜芳香環,其係選自下列各物所組成群組中:Q-1、Q-2、Q-3、Q-4、Q-5、Q-6、Q-7、Q-8、Q-9、Q-10、Q-11、Q-12、Q-13、Q-14、Q-15、Q-16、Q-17、Q-18、Q-19、Q-20、Q-21、Q-22、Q-23、Q-24、Q-25、Q-26、Q-27、Q-28、Q-29、Q-30、Q-31、Q-32、Q-33、Q-34、Q-35、Q-36、Q-37、Q-38、Q-39、Q-40、Q-41、Q-42、Q-43、Q-44、Q-45、Q-46、Q-47、Q-48、Q-49、Q-50、Q-51、Q-52、Q-53、Q-54、Q-55、Q-56、Q-57、Q-58、Q-59、Q-60、Q-61、Q-62、Q-63與Q-64
其中m 為0、1或2,其受到Q中可用於連接取代基Y之位置數量之限制,
及各Y 分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基羰基、-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、-NH(C1-C4-烷基羰基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、C1-C4-烷基羰基氧、具有1至5個鹵原子之C1-C4-鹵烷基羰基氧、C1-C4-烷基羰基胺基、具有1至5個鹵原子之C1-C4-鹵烷基羰基胺基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、-OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、-CH2-S-C1-C4-烷基、-CH2-S(O)-C1-C4-烷基、-CH2-S(O)2-C1-C4-烷基、(C1-C4-烷氧基亞胺基)-C1-C4-烷基、(C2-C6-烯基氧亞胺基)-C1-C4-烷基、(C3-C6-炔基氧亞胺基)-C1-C4-烷基、(苯甲基氧亞胺基)-C1-C6-烷基、苯甲基氧、-S-苯甲基、苯甲基胺基、苯氧基、-S-苯基與苯基胺基,R1、R2、R3與R4相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-CHO、-COOH、-CONH2、C1-C4-烷基、
C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C3-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C3-烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基羰基、-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、-OC(O)-C1-C4-烷基、具有1至5個鹵原子之-OC(O)-C1-C4-鹵烷基、-NHC(O)-C1-C4-烷基、具有1至5個鹵原子之-NHC(O)-C1-C4-鹵烷基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,其限制條件為R1為氟與/或R2為氟,R5 係如具體實施例2-1中之定義,及A 係如具體實施例2-1中之定義,其限制條件為Het-21中之R55不為CF3。
具體實施例2-1之另一項個別態樣中,R1為氟。具體實施例
2-1之另一項個別態樣中,R2為氟。具體實施例2-1之另一項個別態樣中,R1為氟與R2為氟。具體實施例2-1之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例2-1之另一項個別態樣中,R1/R2組合為氟/氫。
具體實施例2-2之另一項個別態樣中,R1為氟。具體實施例2-2之另一項個別態樣中,R2為氟。具體實施例2-2之另一項個別態樣中,R1為氟與R2為氟。具體實施例2-2之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例2-2之另一項個別態樣中,R1/R2組合為氟/氫。
式(I)化合物中所述及結構元素之更佳取代基或範圍說明如下(具體實施例3-1):n 為1,X 係選自下列所組成之群組中:氫、鹵素、硝基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、具有1至5個鹵原子C1-C4-鹵烷氧基,Q 代表可視需要經單-或多取代之雜芳香環,其係選自下列各物所組成群組中:Q-4、Q-11、Q-21、Q-22、Q-25、Q-36、Q-37、Q-38、Q-40、Q-41、Q-42、Q-53、Q-58、Q-62、Q-63與Q-64,其中m 為0、1或2,其受到Q中可用於連接取代基Y之位置數量之限制,及各Y 分別獨立選自下列所組成之群組中:氫、-CF3、-CH2CF3、甲基、乙基、氟、氯、溴、碘、氰基、-OCH3、-OCH2CH3、-OCH(CH3)2、-OCH2CF3、S(O)2-CH3、NHC(O)CH3,R1與R2相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷氧基、C3-C6-
環烷基-C1-C3-烷基、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、-NHC(O)-C1-C4-烷基、與苯基,R3與R4相同或相異,且係選自下列所組成之群組中:氫、-COOH、C1-C4-烷基、C1-C4-鹵烷基C1-C4-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、-CONH(C1-C4-烷基)、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、與苯基,或R1與R2與其所鍵結之碳原子共同形成4或5-員碳環,且R3與R4相同或相異,且係選自下列所組成之群組中:氫、-COOH、C1-C4-烷基、C1-C4-鹵烷基C1-C4-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、-CONH(C1-C4-烷基)、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、與苯基,較佳係R1與R2與其所鍵結之碳原子共同形成環丁基或環戊基,或R3與R4與其所鍵結之碳原子共同形成3-、4-或5-員碳環,且R1與R2相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷氧基、C3-C6-環烷基-C1-C3-烷基、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、-NHC(O)-C1-C4-烷基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,較佳係R3與R4與其所鍵結之碳原子共同形成環丙基或環丁基,或R2與R4與其所鍵結之碳原子共同形成5-員非芳香系碳環,其可視需要經選自由1至4個C1-C3-烷基與1至2個鹵原子所組成群組中之取代基取代,且R1係選自下列所組成之群組中:氫、鹵素、氰基、
羥基、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷氧基、C3-C6-環烷基-C1-C3-烷基、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、-NHC(O)-C1-C4-烷基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,及R3係選自下列所組成之群組中:氫、-COOH、C1-C4-烷基、C1-C4-鹵烷基C1-C4-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、-CONH(C1-C4-烷基)、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、與苯基,較佳係R2與R4與其所鍵結之碳原子共同形成環戊基,或R1與R3與其所鍵結之碳原子共同形成5-員非芳香系碳環,其可視需要經選自由1至4個C1-C3-烷基與1至2個鹵原子所組成群組中之取代基取代,且R2係選自下列所組成之群組中:氫、鹵素、氰基、羥基、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷氧基、C3-C6-環烷基-C1-C3-烷基、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、-NHC(O)-C1-C4-烷基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,及R4係選自下列所組成之群組中:氫、-COOH、C1-C4-烷基、C1-C4-鹵烷基-C1-C4-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、-CONH(C1-C4-烷基)、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、與苯基,較佳係R1與R3與其所鍵結之碳原子共同形成環戊基,R5 係選自下列所組成之群組中:氫、C1-C4-烷基、C3-C6-環烷基、C1-C4-烷氧基、C1-C4-烷氧基-C1-C4-烷基、C1-C4-烷基羰基、C1-C4-烷氧基羰基,A 代表式(A1)苯基
其中o 為0、1或2,及各R 分別獨立選自下列所組成之群組中:鹵素、硝基、-OH、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、C1-C4-烷氧基羰基、-NH(C1-C4-烷基)、苯基(可視需要經C1-C4-烷氧基取代)與苯氧基,或A 代表式(Het-1)雜環
其中R6與R7可相同或相異,且係選自下列所組成之群組中:氫、鹵素、硝基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R8 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-2)雜環
其中R9 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R10與R11 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、
C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基、苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-4)雜環
其中R14與R15可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、-S-C1-C4-烷基、-S(O)2-C1-C4-烷基、苯基(可視需要經鹵素或C1-C4-烷基取代)與吡啶基(可視需要經鹵素或C1-C4-烷基取代),及R16係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,或A 代表式(Het-5)雜環
其中R17與R18可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、C1-C4-烷基氧與具有1至5個鹵原子之C1-C4-鹵烷基,及R19 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-6)雜環
其中R20 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R21與R23可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R22 係選自下列所組成之群組中:氫、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基-C1-C4-烷基,或A 代表式(Het-10)雜環
其中R32 係選自下列所組成之群組中:氫、鹵素、胺基、氰基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),及R33 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基、包含1至9個鹵原子之C1-C5-鹵烷氧基、胺基、經取代或未經取代之C1-C5-烷基胺基或經取代或未經取代之二-(C1-C5-烷基)-胺基,或A 代表式(Het-21)雜環
其中R55 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,及R56、R57與R58,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基與-S(O)2-C1-C4-烷基,或A 代表式(Het-22)雜環
其中R59 係選自下列所組成之群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4烷氧基、-S-C1-C5-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、-S-C2-C5-烯基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、苯基氧(可視需要經鹵素或C1-C4-烷基取代)與-S-苯基(可視需要經鹵素或C1-C4-烷基取代),及R60、R61與R62,其可相同或相異,且係選自下列各物所組成群組中:
氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、N-嗎啉(可視需要經鹵素或C1-C4-烷基取代)與噻吩基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-29)雜環
其中R76 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基。
另一項個別之具體實施例(具體實施例3-2)中,式(I)化合物之結構元素更佳係如下列定義:n 為1或2,各X係如具體實施例3-1中之定義,Q 代表可視需要經單-或多取代之雜芳香環,其係選自下列各物所組成群組中:Q-4、Q-11、Q-21、Q-22、Q-25、Q-36、Q-37、Q-38、Q-40、Q-41、Q-42、Q-45、Q-53、Q-58、Q-62、Q-63與Q-64,其中m 為0、1或2,其受到Q中可用於連接取代基Y之位置數量之限制,與各Y 分別獨立選自下列所組成之群組中:氫、-CF3、-CH2CF3、甲基、乙基、氟、氯、溴、碘、氰基、-OCH3、-OCH2CH3、-OCH(CH3)2、-OCH2CF3、S(O)2-CH3、NHC(O)CH3、NHCH3與N(CH3)2,
R1與R2相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷氧基、C3-C6-環烷基-C1-C3-烷基、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、-NHC(O)-C1-C4-烷基、與苯基,其限制條件為R1為氟與/或R2為氟,R3與R4相同或相異,且係選自下列所組成之群組中:氫、-COOH、C1-C4-烷基、C1-C4-鹵烷基C1-C4-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、-CONH(C1-C4-烷基)、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基與苯基,R5 係如具體實施例3-1中之定義,及A 係如具體實施例3-1中之定義,其限制條件為Het-21中,R55不為CF3。
具體實施例3-1之另一項個別態樣中,R1為氟。具體實施例3-1之另一項個別態樣中,R2為氟。具體實施例3-1之另一項個別態樣中,R1為氟與R2為氟。具體實施例3-1之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例3-1之另一項個別態樣中,R1/R2組合為氟/氫。
具體實施例3-2之另一項個別態樣中,R1為氟。具體實施例3-2之另一項個別態樣中,R2為氟。具體實施例3-2之另一項個別態樣中,R1為氟與R2為氟。具體實施例3-2之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例3-2之另一項個別態樣中,R1/R2組合為氟/氫。
式(I)化合物中所述及結構元素之特別佳取代基或範圍說明如下(具體實施例4-1):n 為1,X 係選自下列所組成之群組中:氫、鹵素、硝基、氰基、C1-C4-烷基、
具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基,Q 係選自:
R1與R2相同或相異,且係選自下列所組成之群組中:氫、甲基、乙基、甲氧基、乙氧基或氟,特定言之其中R1與R2均不為氫,R3與R4相同或相異,且係選自下列所組成之群組中:氫、甲基或乙基,R5 為氫,A 係選自:
或A 係選自:
另一項個別之具體實施例(具體實施例4-2)中,式(I)化合物之結構元素特別佳係如下列定義:n 為1或2,各X係如具體實施例4-1中之定義,Q 係選自:
R1與R2相同或相異,且係選自下列所組成之群組中:氫、甲基、乙基、甲氧基、乙氧基或氟,其限制條件為R1為氟與/或R2為氟,R3與R4相同或相異,且係選自下列所組成之群組中:氫、甲基或乙基,R5 係如具體實施例4-1中之定義,及A 係選自:
或A 係選自:
具體實施例4-1之另一項個別態樣中,R1為氟。具體實施例4-1之另一項個別態樣中,R2為氟。具體實施例4-1之另一項個別態樣中,R1為氟與R2為氟。具體實施例4-1之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例4-1之另一項個別態樣中,R1/R2組合為氟/氫。
具體實施例4-2之另一項個別態樣中,R1為氟。具體實施例4-2之另一項個別態樣中,R2為氟。具體實施例4-2之另一項個別態樣中,R1為氟與R2為氟。具體實施例4-2之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例4-2之另一項個別態樣中,R1/R2組合為氟/氫。
式(I)化合物中所述及結構元素之特別佳取代基或範圍之第
一項極明確態樣(具體實施例5-1)中,n 為1,X 係選自下列所組成之群組中:氫或氯,Q 係選自:
R1、R2、R3、R4與R5為氫,或R1與R2為氟,及R3、R4與R5為氫,A 為
或
式(I)化合物中所述及結構元素之特別佳取代基或範圍之第二項極明確態樣(具體實施例5-2)中,n 為1或2,各X係選自下列所組成之群組中:氫、氯、氰基、氟、甲基、三氟甲基與甲氧基,較佳係若n為1時,則X係選自下列所組成之群組中:氫、氯、氟、甲基、三氟甲基與甲氧基;若n為2時,則X為氟,Q 係選自:
R1與R2相同或相異,且係選自下列所組成之群組中:氫、甲基或氟,其限制條件為R1為氟與/或R2為氟,R3、R4與R5為氫,A 為
或
式(I)化合物中所述及結構元素之特別佳取代基或範圍之第三項極明確態樣(具體實施例5-3)中,n 為1,X 係選自下列所組成之群組中:氫或氯,Q 係選自:
R1與R2均為氟,或R1與R2為一個氟與一個氫,或R1與R2為一個氟與一個甲基,R3、R4與R5為氫,A 為
或
或
式(I)化合物中所述及結構元素之特別佳取代基或範圍之第四項極明確態樣(具體實施例5-4)中,n 為1或2,各X係選自下列所組成之群組中:氫、氯、氰基、氟、甲基、三氟甲
基與甲氧基,較佳係若n為1時,則X係選自下列所組成之群組中:氫、氯、氟、甲基、三氟甲基與甲氧基;若n為2時,則X為氟,Q 係選自:
R1與R2相同或相異,且係選自下列所組成之群組中:氫、甲基或氟,其限制條件為R1為氟與/或R2為氟,R3、R4與R5為氫,A 係選自:
或A為
或A為
具體實施例5-1之另一項個別態樣中,R1為氟與R2為氟。
具體實施例5-2之另一項個別態樣中,R1為氟。具體實施例5-2之另一項個別態樣中,R2為氟。具體實施例5-2之另一項個別態樣中,R1為氟與R2為氟。具體實施例5-2之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例5-2之另一項個別態樣中,R1/R2組合為氟/氫。
具體實施例5-3之另一項個別態樣中,R1為氟與R2為氟。具體實施例5-3之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例5-3之另一項個別態樣中,R1/R2組合為氟/氫。
具體實施例5-4之另一項個別態樣中,R1為氟。具體實施例5-4之另一項個別態樣中,R2為氟。具體實施例5-4之另一項個別態樣中,R1為氟與R2為氟。具體實施例5-4之另一項個別態樣中,R1/R2組合為氟/甲基。具體實施例5-4之另一項個別態樣中,R1/R2組合為氟/氫。
上述一般或較佳範圍中指示之基團定義與說明可以彼此自由組合,因此包括個別範圍與較佳範圍之間之組合。較佳特色之組合因此成為根據本發明化合物之子群。該等定義與說明因此同樣適用於終產物及
前體與中間物。
根據本發明較佳係式(I)化合物中有上述較佳定義之組合(較佳者),其中上述各較佳具體實施例即構成該個別組合。
根據本發明更佳係式(I)化合物中有上述更佳定義之組合(更佳者),其中上述各更佳具體實施例即構成該個別組合。
根據本發明特別佳係式(I)化合物中有上述特別佳定義之組合(特別佳者),其中上述各特別佳具體實施例即構成該個別組合。
根據本發明一項極明確態樣為式(I)化合物,其中有如上述作為結構元素之特別佳取代基或範圍之第一項極明確態樣(具體實施例5-1)所指示之定義組合。
根據本發明另一項極明確態樣為式(I)化合物,其中有如上述作為結構元素之特別佳取代基或範圍之第二項極明確態樣(具體實施例5-2)所指示之定義組合。
根據本發明另一項極明確態樣為式(I)化合物,其中有如上述作為結構元素之特別佳取代基或範圍之第三項極明確態樣(具體實施例5-3)所指示之定義組合。
根據本發明另一項極明確態樣為式(I)化合物,其中有如上述作為結構元素之特別佳取代基或範圍之第四項極明確態樣(具體實施例5-4)所指示之定義組合。
飽和或不飽和烴基,如:烷基、烷二基或烯基(單獨及與雜原子組合時,如烷氧基),例如:若可能時,可分別為直鏈或分支。
任何經取代之基團,除非另有說明,否則係經取代一次或多次,且多次取代時之取代基可能相同或相異。
在基團之較佳定義中,鹵素(鹵基)係氟、氯、溴與碘,極佳
係氟、氯與溴,特別佳係氟與氯。
本發明之其他明確具體實施例說明如下。
進一步較佳具體實施例中,本發明係有關一種式(I)中R3與R4與R5為氫之化合物(亦即式(I-1)化合物)之用途。
因此,一項明確具體實施例(具體實施例6-1)係式(I-1)化合物之用途
其中R1、R2、Q、X、n與A係如具體實施例1-1中定義,其係用於控制線蟲與/或其他蠕蟲。
本發明另一項明確具體實施例(具體實施例6-2)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例1-2中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例6-1a)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例1-1a中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例6-2a)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例1-2a中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例7-1)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例2-1中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例7-2)係以式(I-1)
中R1、R2、Q、X、n與A如具體實施例2-2中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例8-1)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例3-1中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例8-2)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例3-2中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例9-1)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例4-1中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例9-2)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例4-2中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例10-1)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例5-1中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例10-2)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例5-2中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例10-3)係以式(I-1)中R1、R2、Q、X、n與A如具體實施例5-3中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
本發明另一項明確具體實施例(具體實施例10-4)係以式(I-1)
中R1、R2、Q、X、n與A如具體實施例5-4中定義之化合物於控制線蟲與/或其他蠕蟲上之用途。
具體實施例1-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例1-1.1)。
具體實施例1-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例1-2.1)。
具體實施例1-1a及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例1-1a.1)。
具體實施例1-2a及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例1-2a.1)。
具體實施例2-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例2-1.1)。
具體實施例2-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例2-2.1)。
具體實施例3-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例3-1.1)。
具體實施例3-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例3-2.1)。
具體實施例4-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例4-1.1)。
具體實施例4-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例4-2.1)。
具體實施例5-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例5-1.1)。
具體實施例5-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例5-2.1)。
具體實施例5-3及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例5-3.1)。
具體實施例5-4及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例5-4.1)。
具體實施例6-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例6-1.1)。
具體實施例6-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例6-2.1)。
具體實施例6-1a及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例6-1a.1)。
具體實施例6-2a及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例6-2a.1)。
具體實施例7-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例7-1.1)。
具體實施例7-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例7-2.1)。
具體實施例8-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例8-1.1)。
具體實施例8-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例8-2.1)。
具體實施例9-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例9-1.1)。
具體實施例9-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例9-2.1)。
具體實施例10-1及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例10-1.1)。
具體實施例10-2及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例10-2.1)。
具體實施例10-3及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例10-3.1)。
具體實施例10-4及該具體實施例之各個別態樣中,Q較佳係在對位(具體實施例10-4.1)。
本發明係有關新穎之式(Ia)化合物
其中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例1-1中之定義,及R1a為氟(具體實施例Ia-1-1),較佳係如上述具體實施例1-1.1中之定義,且R1a為氟(具體實施例Ia-1-1.1)。
另一項具體實施例(具體實施例Ia-1-2)為式(Ia)化合物,其中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例1-2中之定義,且R1a為氟,較佳係如上述具體實施例1-2.1中之定義,且R1a為氟(具體實施例Ia-1-2.1)。
另一項具體實施例(具體實施例Ia-1-1a)為式(Ia)化合物,其
中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例1-1a中之定義,且R1a為氟,較佳係如上述具體實施例1-1a.1中之定義,且R1a為氟(具體實施例Ia-1-1a.1)。
另一項具體實施例(具體實施例Ia-1-2a)為式(Ia)化合物,其中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例1-2a中之定義,且R1a為氟,較佳係如上述具體實施例1-2a.1中之定義,且R1a為氟(具體實施例Ia-1-2a.1)。
另一項具體實施例(具體實施例Ia-2-1)為式(Ia)化合物,其中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例2-1中之定義,且R1a為氟,較佳係如上述具體實施例2-1.1中之定義,且R1a為氟(具體實施例Ia-2-1.1)。
另一項具體實施例(具體實施例Ia-2-2)為式(Ia)化合物,其中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例2-2中之定義,且R1a為氟,較佳係如上述具體實施例2-2.1中之定義,且R1a為氟(具體實施例Ia-2-2.1)。
另一項具體實施例(具體實施例Ia-3-1)為式(Ia)化合物,其中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例3-1中之定義,且R1a為氟,較佳係如上述具體實施例3-1.1中之定義,且R1a為氟(具體實施例Ia-3-1.1)。
另一項具體實施例(具體實施例Ia-3-2)為式(Ia)化合物,其中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例3-2中之定義,且R1a為氟,較佳係如上述具體實施例3-2.1中之定義,且R1a為氟(具體實施例Ia-3-2.1)。
另一項具體實施例(具體實施例Ia-4-1)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例4-1中之定義,且R1a為氟,較佳係如上述具體實施例4-1.1中之定義,且R1a為氟(具體實施例Ia-4-1.1)。
另一項具體實施例(具體實施例Ia-4-2)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例4-2中之定義,且R1a為氟,較佳係如上述具體實施例4-2.1中之定義,且R1a為氟(具體實施例Ia-4-2.1)。
另一項具體實施例(具體實施例Ia-5-1)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例5-1中之定義,且R1a為氟,較佳係如上述具體實施例5-1.1中之定義,且R1a為氟(具體實施例Ia-5-1.1)。
另一項具體實施例(具體實施例Ia-5-2)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例5-2中之定義,且R1a為氟,較佳係如上述具體實施例5-2.1中之定義,且R1a為氟(具體實施例Ia-5-2.1)。
另一項具體實施例(具體實施例Ia-5-3)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例5-3中之定義,且R1a為氟,較佳係如上述具體實施例5-3.1中之定義,且R1a為氟(具體實施例Ia-5-3.1)。
另一項具體實施例(具體實施例Ia-5-4)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例5-4中之定義,且R1a為氟,較佳係如上述具體實施例5-4.1中之定義,且R1a為氟(具體實施例Ia-5-4.1)。
另一項具體實施例(具體實施例Ia-6-1)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例6-1中之定義,且R1a為氟,較佳係如上述具體實施例6-1.1中之定義,且R1a為氟(具體實施例Ia-6-1.1)。
另一項具體實施例(具體實施例Ia-6-2)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例6-2中之定義,且R1a為氟,較佳係如上述具體實施例6-2.1中之定義,且R1a為氟(具體實施例Ia-6-2.1)。
另一項具體實施例(具體實施例Ia-6-1a)為式(Ia)化合物,其
中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例6-1a中之定義,且R1a為氟,較佳係如上述具體實施例6-1a.1中之定義,且R1a為氟(具體實施例Ia-6-1a.1)。
另一項具體實施例(具體實施例Ia-6-2a)為式(Ia)化合物,其
中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例6-2a中之定義,且R1a為氟,較佳係如上述具體實施例6-2a.1中之定義,且R1a為氟(具體實施例Ia-6-2a.1)。
另一項具體實施例(具體實施例Ia-7-1)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例7-1中之定義,且R1a為氟,較佳係如上述具體實施例7-1.1中之定義,且R1a為氟(具體實施例Ia-7-1.1)。
另一項具體實施例(具體實施例Ia-7-2)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例7-2中之定義,且R1a為氟,較佳係如上述具體實施例7-2.1中之定義,且R1a為氟(具體實施例Ia-7-2.1)。
另一項具體實施例(具體實施例Ia-8-1)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例8-1中之定義,且R1a為氟,較佳係如上述具體實施例8-1.1中之定義,且R1a為氟(具體實施例Ia-8-1.1)。
另一項具體實施例(具體實施例Ia-8-2)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例8-2中之定義,且R1a為氟,較佳係如上述具體實施例8-2.1中之定義,且R1a為氟(具體實施例Ia-8-2.1)。
另一項具體實施例(具體實施例Ia-9-1)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例9-1中之定義,且R1a為氟,較佳係如上述具體實施例9-1.1中之定義,且R1a為氟(具體實施例Ia-9-1.1)。
另一項具體實施例(具體實施例Ia-9-2)為式(Ia)化合物,其中
n、X、Q、R2、R3、R4、R5與A係如上述具體實施例9-2中之定義,且R1a為氟,較佳係如上述具體實施例9-2.1中之定義,且R1a為氟(具體實施例Ia-9-2.1)。
另一項具體實施例(具體實施例Ia-10-1)為式(Ia)化合物,其
中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例10-1中之定義,且R1a為氟,較佳係如上述具體實施例10-1.1中之定義,且R1a為氟(具體實施例Ia-10-1.1)。
另一項具體實施例(具體實施例Ia-10-2)為式(Ia)化合物,其
中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例10-2中之定義,且R1a為氟,較佳係如上述具體實施例10-2.1中之定義,且R1a為氟(具體實施例Ia-10-2.1)。
另一項具體實施例(具體實施例Ia-10-3)為式(Ia)化合物,其
中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例10-3中之定義,且R1a為氟,較佳係如上述具體實施例10-3.1中之定義,且R1a為氟(具體實施例Ia-10-3.1)。
另一項具體實施例(具體實施例Ia-10-4)為式(Ia)化合物,其
中n、X、Q、R2、R3、R4、R5與A係如上述具體實施例10-4中之定義,且R1a為氟,較佳係如上述具體實施例10-4.1中之定義,且R1a為氟(具體實施例Ia-10-4.1)。
特別佳式(Ia)化合物中,結構元素n、X、Q、R1a、R2與A均如上述具體實施例之說明(Ia-1-1至Ia-10-4.1),及R3與R4與R5為氫。
本發明亦有關一種新穎之式(Ib)化合物
其中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例1-1之定義,及R2a為氟(具體實施例Ib-1-1),較佳係如上述具體實施例1-1.1中之定義,且R2a為氟(具體實施例Ib-1-1.1)。
另一項具體實施例(具體實施例Ib-1-2)為式(Ib)化合物,其中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例1-2中之定義,且R2a為氟,較佳係如上述具體實施例1-2.1中之定義,且R2a為氟(具體實施例Ib-1-2.1)。
另一項具體實施例(具體實施例Ib-1-1a)為式(Ib)化合物,其中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例1-1a中之定義,且R2a為氟,較佳係如上述具體實施例1-1a.1中之定義,且R2a為氟(具體實施
例Ib-1-1a.1)。
另一項具體實施例(具體實施例Ib-1-2a)為式(Ib)化合物,其
中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例1-2a中之定義,且R2a為氟,較佳係如上述具體實施例1-2a.1中之定義,且R2a為氟(具體實施例Ib-1-2a.1)。
另一項具體實施例(具體實施例Ib-2-1)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例2-1中之定義,且R2a為氟,較佳係如上述具體實施例2-1.1中之定義,且R2a為氟(具體實施例Ib-2-1.1)。
另一項具體實施例(具體實施例Ib-2-2)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例2-2中之定義,且R2a為氟,較佳係如上述具體實施例2-2.1中之定義,且R2a為氟(具體實施例Ib-2-2.1)。
另一項具體實施例(具體實施例Ib-3-1)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例3-1中之定義,且R2a為氟,較佳係如上述具體實施例3-1.1中之定義,且R2a為氟(具體實施例Ib-3-1.1)。
另一項具體實施例(具體實施例Ib-3-2)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例3-2中之定義,且R2a為氟,較佳係如上述具體實施例3-2.1中之定義,且R2a為氟(具體實施例Ib-3-2.1)。
另一項具體實施例(具體實施例Ib-4-1)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例4-1中之定義,且R2a為氟,較佳係如上述具體實施例4-1.1中之定義,且R2a為氟(具體實施例
Ib-4-1.1)。
另一項具體實施例(具體實施例Ib-4-2)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例4-2中之定義,且R2a為氟,較佳係如上述具體實施例4-2.1中之定義,且R2a為氟(具體實施例Ib-4-2.1)。
另一項具體實施例(具體實施例Ib-5-1)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例5-1中之定義,且R2a為氟,較佳係如上述具體實施例5-1.1中之定義,且R2a為氟(具體實施例Ib-5-1.1)。
另一項具體實施例(具體實施例Ib-5-2)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例5-2中之定義,且R2a為氟,較佳係如上述具體實施例5-2.1中之定義,且R2a為氟(具體實施例Ib-5-2.1)。
另一項具體實施例(具體實施例Ib-5-3)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例5-3中之定義,且R2a為氟,較佳係如上述具體實施例5-3.1中之定義,且R2a為氟(具體實施例Ib-5-3.1)。
另一項具體實施例(具體實施例Ib-5-4)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例5-4中之定義,且R2a為氟,較佳係如上述具體實施例5-4.1中之定義,且R2a為氟(具體實施例Ib-5-4.1)。
另一項具體實施例(具體實施例Ib-6-1)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例6-1中之定義,且R2a為氟,較佳係如上述具體實施例6-1.1中之定義,且R2a為氟(具體實施例
Ib-6-1.1)。
另一項具體實施例(具體實施例Ib-6-2)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例6-2中之定義,且R2a為氟,較佳係如上述具體實施例6-2.1中之定義,且R2a為氟(具體實施例Ib-6-2.1)。
另一項具體實施例(具體實施例Ib-6-1a)為式(Ib)化合物,其
中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例6-1a中之定義,且R2a為氟,較佳係如上述具體實施例6-1a.1中之定義,且R2a為氟(具體實施例Ib-6-1a.1)。
另一項具體實施例(具體實施例Ib-6-2a)為式(Ib)化合物,其
中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例6-2a中之定義,且R2a為氟,較佳係如上述具體實施例6-2a.1中之定義,且R2a為氟(具體實施例Ib-6-2a.1)。
另一項具體實施例(具體實施例Ib-7-1)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例7-1中之定義,且R2a為氟,較佳係如上述具體實施例7-1.1中之定義,且R2a為氟(具體實施例Ib-7-1.1)。
另一項具體實施例(具體實施例Ib-7-2)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例7-2中之定義,且R2a為氟,較佳係如上述具體實施例7-2.1中之定義,且R2a為氟(具體實施例Ib-7-2.1)。
另一項具體實施例(具體實施例Ib-8-1)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例8-1中之定義,且R2a為氟,較佳係如上述具體實施例8-1.1中之定義,且R2a為氟(具體實施例
Ib-8-1.1)。
另一項具體實施例(具體實施例Ib-8-2)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例8-2中之定義,且R2a為氟,較佳係如上述具體實施例8-2.1中之定義,且R2a為氟(具體實施例Ib-8-2.1)。
另一項具體實施例(具體實施例Ib-9-1)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例9-1中之定義,且R2a為氟,較佳係如上述具體實施例9-1.1中之定義,且R2a為氟(具體實施例Ib-9-1.1)。
另一項具體實施例(具體實施例Ib-9-2)為式(Ib)化合物,其中
n、X、Q、R1、R3、R4、R5與A係如上述具體實施例9-2中之定義,且R2a為氟,較佳係如上述具體實施例9-2.1中之定義,且R2a為氟(具體實施例Ib-9-2.1)。
另一項具體實施例(具體實施例Ib-10-1)為式(Ib)化合物,其
中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例10-1中之定義,且R2a為氟,較佳係如上述具體實施例10-1.1中之定義,且R2a為氟(具體實施例Ib-10-1.1)。
另一項具體實施例(具體實施例Ib-10-2)為式(Ib)化合物,其
中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例10-2中之定義,且R2a為氟,較佳係如上述具體實施例10-2.1中之定義,且R2a為氟(具體實施例Ib-10-2.1)。
另一項具體實施例(具體實施例Ib-10-3)為式(Ib)化合物,其
中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例10-3中之定義,且R2a為氟,較佳係如上述具體實施例10-3.1中之定義,且R2a為氟(具體實施
例Ib-10-3.1)。
另一項具體實施例(具體實施例Ib-10-4)為式(Ib)化合物,其中n、X、Q、R1、R3、R4、R5與A係如上述具體實施例10-4中之定義,且R2為氟,較佳係如上述具體實施例10-4.1中之定義,且R2a為氟(具體實施例Ib-10-4.1)。
特別佳式(Ib)化合物中,結構元素n、X、Q、R2a、R1與A均如上述具體實施例之說明(Ib-1-1至Ib-10-4.1),及R3與R4與R5為氫。
本發明亦有關一種新穎之式(Ic)化合物
其中n、X、Q、R3、R4、R5與A係如上述具體實施例1-1中之定義,且R1a與R2a均為氟(具體實施例Ic-1-1),較佳係如上述具體實施例1-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-1-1.1)。
另一項具體實施例(具體實施例Ic-1-2)為式(Ic)化合物,其中n、X、Q、R3、R4、R5與A係如上述具體實施例1-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例1-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-1-2.1)。
另一項具體實施例(具體實施例Ic-1-1a)為式(Ic)化合物,其中n、X、Q、R3、R4、R5與A係如上述具體實施例1-1a中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例1-1a.1中之定義,且R1a與R2a均為氟(具體實施例Ic-1-1a.1)。
另一項具體實施例(具體實施例Ic-1-2a)為式(Ic)化合物,其
中n、X、Q、R3、R4、R5與A係如上述具體實施例1-2a中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例1-2a.1中之定義,且R1a與R2a均為氟(具體實施例Ic-1-2a.1)。
另一項具體實施例(具體實施例Ic-2-1)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例2-1中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例2-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-2-1.1)。
另一項具體實施例(具體實施例Ic-2-2)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例2-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例2-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-2-2.1)。
另一項具體實施例(具體實施例Ic-3-1)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例3-1中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例3-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-3-1.1)。
另一項具體實施例(具體實施例Ic-3-2)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例3-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例3-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-3-2.1)。
另一項具體實施例(具體實施例Ic-4-1)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例4-1中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例4-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-4-1.1)。
另一項具體實施例(具體實施例Ic-4-2)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例4-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例4-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-4-2.1)。
另一項具體實施例(具體實施例Ic-5-1)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例5-1中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例5-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-5-1.1)。
另一項具體實施例(具體實施例Ic-5-2)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例5-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例5-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-5-2.1)。
另一項具體實施例(具體實施例Ic-5-3)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例5-3中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例5-3.1中之定義,且R1a與R2a均為氟(具體實施例Ic-5-3.1)。
另一項具體實施例(具體實施例Ic-5-4)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例5-4中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例5-4.1中之定義,且R1a與R2a均為氟(具體實施例Ic-5-4.1)。
另一項具體實施例(具體實施例Ic-6-1)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例6-1中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例6-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-6-1.1)。
另一項具體實施例(具體實施例Ic-6-2)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例6-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例6-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-6-2.1)。
另一項具體實施例(具體實施例Ic-6-1a)為式(Ic)化合物,其
中n、X、Q、R3、R4、R5與A係如上述具體實施例6-1a中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例6-1a.1中之定義,且R1a與R2a均為氟(具體實施例Ic-6-1a.1)。
另一項具體實施例(具體實施例Ic-6-2a)為式(Ic)化合物,其
中n、X、Q、R3、R4、R5與A係如上述具體實施例6-2a中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例6-2a.1中之定義,且R1a與R2a均為氟(具體實施例Ic-6-2a.1)。
另一項具體實施例(具體實施例Ic-7-1)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例7-1中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例7-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-7-1.1)。
另一項具體實施例(具體實施例Ic-7-2)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例7-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例7-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-7-2.1)。
另一項具體實施例(具體實施例Ic-8-1)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例8-1中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例8-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-8-1.1)。
另一項具體實施例(具體實施例Ic-8-2)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例8-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例8-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-8-2.1)。
另一項具體實施例(具體實施例Ic-9-1)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例9-1中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例9-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-9-1.1)。
另一項具體實施例(具體實施例Ic-9-2)為式(Ic)化合物,其中
n、X、Q、R3、R4、R5與A係如上述具體實施例9-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例9-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-9-2.1)。
另一項具體實施例(具體實施例Ic-10-1)為式(Ic)化合物,其
中n、X、Q、R3、R4、R5與A係如上述具體實施例10-1中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例10-1.1中之定義,且R1a與R2a均為氟(具體實施例Ic-10-1.1)。
另一項具體實施例(具體實施例Ic-10-2)為式(Ic)化合物,其
中n、X、Q、R3、R4、R5與A係如上述具體實施例10-2中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例10-2.1中之定義,且R1a與R2a均為氟(具體實施例Ic-10-2.1)。
另一項具體實施例(具體實施例Ic-10-3)為式(Ic)化合物,其
中n、X、Q、R3、R4、R5與A係如上述具體實施例10-3中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例10-3.1中之定義,且R1a與R2a均為氟(具體實施例Ic-10-3.1)。
另一項具體實施例(具體實施例Ic-10-4)為式(Ic)化合物,其
中n、X、Q、R3、R4、R5與A係如上述具體實施例10-4中之定義,且R1a與R2a均為氟,較佳係如上述具體實施例10-4.1中之定義,且R1a與R2a均為氟(具體實施例Ic-10-4.1)。
特別佳式(Ic)化合物中,結構元素n、X、Q、R1a、R2a與A均如上述具體實施例之說明(Ic-1-1至Ic-10-4.1),及R3與R4與R5為氫。
製程與方法
式(I)化合物之合成法可依據或類似反應圖1、2或3進行。所需之起始物係已知者或可經由一般已知製程取得,其更詳細說明於WO 2001/011965 A1(P1)、WO 2005/058828 A1(P2)、WO2005/014545 A2(P3)、WO 2005/103004 A1(P4)、WO 2006/122952 A1(P5)、EP 2 289 880 A1(P6)、WO 2006/008191 A1(P7)、WO 2006/008192 A1(P8)、WO 2004/074280 A1(P9)、WO 2005/058833 A2(P10)、WO 2005/085238 A1(P11)、WO 2005/103006 A1(P12)、WO 2006/122955 A1(P13)、WO 2006/008194 A1(P14)、WO 2006/008193 A1(P15)、WO 2006/067103 A2(P16)、及WO 2013/064460 A1(P17)(若R1=R2=氟)或WO 2007141009 A1(P18)(若R1=氟與R2=烷基或氫)。
苯甲基腈類,如:(II)可自商品取得或可依WO2013043232之說明合成,然後再於氯化鎳與Boc-酸酐之存在下,使用硼氫化鈉還原成Boc-保護之胺類(III)。受保護之胺類(III)可使用鹽酸,於甲醇中裂解成胺-鹽酸鹽(IV)。原則上,此等苯乙基胺類與其鹽類亦可自商品取得。
該胺-鹽酸鹽或胺類(IV)、(VIII)、(XIII)或(XV)再與適當酸及偶合劑(如:HOBT-EDC或TBTU)偶合,產生例如:醯胺類(V)、(IX)或(XIV)(其中B3或B6代表N或CH,及Ro係如上述定義)或醯胺(I-d)。或者,醯胺類(V)、(IX)、(XIV)或(I-d)可使用適當醯基氯部份基團與鹼(例如:亨尼氏
(Hünig’s)鹼)製備。
然後採用偶合反應合成式(I-a)、(I-b)或(I-c)化合物。若Q=N-
鍵結之唑類時,可使用氧化亞銅(I),以水楊醛肟作為配體,於溶劑(如:乙腈)中,於鹼(如:碳酸銫)之存在下進行由銅介導之製程。若Q=碳鍵結之雜環時,可採用適當二羥硼酸或酯,於鈀觸媒及鹼之存在下,進行鈴木型(Suzuki-type)偶合反應。或者,化合物(I-d)之合成法亦可在合成過程早期先引進Q部份基團,然後再類似反應圖4進行其中所例舉之一種合成途徑。
經吡啶基取代之胺類,如:(XVIII;3-或4-吡啶基時D1、D2為CH或N,Y與m如上述說明)係經由鈴木型(Suzuki type)偶合法,由苯基溴化物(如:(XVI))與適當之二羥硼酸(XVII-a;3-或4-吡啶基時,D1、D2為CH或N,Y與m係如上述說明)或頻哪醇酯(XVII-b;3-或4-吡啶基時,D1、D2為CH或N,Y與m係如上述說明),於鈀觸媒與鹼之存在下合成(反應圖5)。
特別值得注意本文所說明製程與方法中之中間物。此等中間物成為本發明之其他個別具體實施例。除了上述中間物外,其他中間物將於下文中說明。
另一項本發明具體實施例為式(INT)化合物
其中R1、R2、Q、X與n係如上述定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例1-1中之定義,較佳係如上述具體實施例1-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例
1-2中之定義,較佳係如上述具體實施例1-2.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例1-1a中之定義,較佳係如上述具體實施例1-1a.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例1-2a中之定義,較佳係如上述具體實施例1-2a.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例2-1中之定義,較佳係如上述具體實施例2-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例2-2中之定義及R1a為氟,較佳係如上述具體實施例2-2.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例3-1中之定義,較佳係如上述具體實施例3-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例3-2中之定義,較佳係如上述具體實施例3-2.1.中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例4-1中之定義,較佳係如上述具體實施例4-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例4-2中之定義,較佳係如上述具體實施例4-2.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例5-1中之定義,較佳係如上述具體實施例5-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例5-2中之定義,較佳係如上述具體實施例5-2.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例5-3中之定義,較佳係如上述具體實施例5-3.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例
5-4中之定義,較佳係如上述具體實施例5-4.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例6-1中之定義,較佳係如上述具體實施例6-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例6-2中之定義,較佳係如上述具體實施例6-2.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例6-1a中之定義,較佳係如上述具體實施例6-1a.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例6-2a中之定義,較佳係如上述具體實施例6-2a.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例7-1中之定義,較佳係如上述具體實施例7-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例7-2中之定義,較佳係如上述具體實施例7-2.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例8-1中之定義,較佳係如上述具體實施例8-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例8-2中之定義,較佳係如上述具體實施例8-2.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例9-1中之定義,較佳係如上述具體實施例9-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例9-2中之定義,較佳係如上述具體實施例9-2.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例10-1中之定義,較佳係如上述具體實施例10-1.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例
10-2中之定義,較佳係如上述具體實施例10-2.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例10-3中之定義,較佳係如上述具體實施例10-3.1中之定義。
一項個別態樣中,R1、R2、Q、X與n係如上述具體實施例10-4中之定義,較佳係如上述具體實施例10-4.1中之定義。
較佳式(INT)化合物之實例為如下式(INT-1)代表之化合物
較佳式(INT)化合物之另一項實例為如下式(INT-2)代表之化合物
根據本發明化合物可依據上述製法製備。儘管如此,咸了解熟悉此相關技術者均可依據其一般知識及可取得之文獻,根據需要合成之各明確化合物來擷用本方法。
其中本專利申請案特別有關式(I)化合物及明確之式(Ia)、(Ib)或(Ic)化合物之用途。因此咸了解下列說明係同等指本發明所有主題,尤指式(I)化合物及式(Ia)、(Ib)或(Ic)化合物之用途。
依取代基性質而定,式(I)、(Ia)、(Ib)或(Ic)化合物可呈幾何與/或光學活性異構物或相應異構物依各種不同組成之混合物。此等立體異構物為例如:對映異構物、非對映異構物、阻轉異構物或幾何異構物。因
此,本發明同時包括純立體異構物及此等異構物之任何混合物。
本發明亦有關控制動物害蟲之方法,其中由式(I)、(Ia)、(Ib)或(Ic)化合物作用在動物害蟲與/或其棲息地上。動物害蟲之控制較佳係在農業與森林,及原料保護上進行。較佳係排除人體或動物體之手術或醫療處理之方法及在人體或動物體上進行之診斷方法。
本發明亦有關式(I)、(Ia)、(Ib)或(Ic)化合物作為除害蟲劑,特定言之作為作物保護劑之用途。
本申請案內容中,各例中術語"除害蟲劑"亦總是包括術語"作物保護劑"。
式(I)、(Ia)、(Ib)或(Ic)化合物具有良好之植物耐受性、對恆溫動物有利之毒性及良好之環境相容性,適合保護植物與植物器官來對抗生物性與非生物性逆境壓力,提高收成產量、改進收成材料品質、及控制動物害蟲,尤指出現在農業、園藝、動物畜養、水產養殖、森林、花園與休閒設施之昆蟲、蜘蛛、蠕蟲、線蟲與軟體動物,可用於保護庫存產品與材料,及用於衛生領域。其較佳係作為除害蟲劑使用。其可活性對抗正常敏感性與抗性物種,及對抗所有或個別發展階段。上述害蟲包括:節肢動物門(Arthropoda),特定言之蛛形綱(Arachnida)之害蟲,例如:粗腳粉蟎(Acarus spp.)(例如:粉塵蟎(Acarus siro))、枸杞瘤節蜱(Aceria kuko)、桔瘤節蜱(Aceria sheldoni)、刺皮癭蟎屬(Aculops spp.)、刺癭蟎屬(Aculus spp.)(例如:福氏刺節蜱(Aculus fockeui)、蘋果銹蜱(Aculus schlechtendali))、花蜱屬(Amblyomma spp.)、橫紋葉蟎(Amphitetranychus viennensis)、銳緣蜱屬(Argas spp.)、牛蜱屬(Boophilus spp.)、紅鬚蟎屬(Brevipalpus spp.)(例如:紫紅短鬚蟎(Brevipalpus phoenicis))、禾草苔蟎(Bryobia graminum)、苜蓿苔
蟎(Bryobia praetiosa)、刺尾蠍屬(Centruroides spp.)、恙蟎屬(Chorioptes spp.)、雞皮刺蟎(Dermanyssus gallinae)、羽刺皮癬蟎(Dermatophagoides pteronyssinus)、美洲塵蟎(Dermatophagoides farinae)、革蜱屬(Dermacentor spp.)、始葉蟎屬(Eotetranychus spp.)(例如:核桃始葉蟎(Eotetranychus hicoriae))、梨上癭蟎(Epitrimerus pyri)、真葉蟎屬(Eutetranychus spp.)(例如:斑氏真葉蟎(Eutetranychus banksi))、癭蟎屬(Eriophyes spp.)(例如:梨癭蟎(Eriophyes pyri))、家食甜蟎(Glycyphagus domesticus)、足海鐮螯蟎(Halotydeus destructor)、半跗線蟎屬(Hemitarsonemus spp.)(例如:茶塵蟎(Hemitarsonemus latus)(=多食細蟎(Polyphagotarsonemus latus))、璃眼蜱屬(Hyalomma spp.)、硬蜱屬(Ixodes spp.)、球腹蛛屬(Latrodectus spp.)、褐隱蛛屬(Loxosceles spp.)、秋收恙蟎(Neutrombicula autumnalis)、Nuphersa屬、小爪蟎屬(Oligonychus spp.)(例如:針葉小爪蟎(Oligonychus coniferarum)、冬青小爪蟎(Oligonychus ilicis)、甘蔗小爪蟎(Oligonychus indicus)、芒果小爪蟎(Oligonychus mangiferus)、草地小爪蟎(Oligonychus pratensis)、石榴小爪蟎(Oligonychus punicae)、樟小爪蟎(Oligonychus yothersi))、鈍緣蜱屬(Ornithodorus spp.)、巨刺蟎屬(Ornithonyssus spp.)、紅蜘蛛屬(Panonychus spp.)(例如:桔全爪蟎(Panonychus citri)(=柑桔葉蟎(Metatetranychus citri))、榆全爪蟎(Panonychus ulmi)(=歐洲葉蟎(Metatetranychus ulmi)))、橘鏽蟎(Phyllocoptruta oleivora)、雜食葉蟎(Platytetranychus multidigituli)、多食細蟎(Polyphagotarsonemus latus)、癢蟎屬(Psoroptes spp.)、扇頭蜱屬(Rhipicephalus spp.)、根蟎屬(Rhizoglyphus spp.)、人疥蟎屬(Sarcoptes spp.)、蠍(Scorpio maurus)、狹跗線蟎屬(Stenotarsonemus spp.)、稻細蟎(Steneotarsonemus spinki)、細蟎屬(Tarsonemus spp.)(例如:亂跗線蟎(Tarsonemus confusus)、仙克萊細蟎(Tarsonemus pallidus))、紅葉蟎屬(Tetranychus spp.)(例如:加拿大葉蟎
(Tetranychus canadensis)、赤葉蟎(Tetranychus cinnabarinus)、土耳其斯坦葉蟎(Tetranychus turkestani)、二斑葉蟎(Tetranychus urticae))、秋蟎(Trombicula alfreddugesi)、蠍屬(Vaejovis spp.)、斜背瘤節蜱(Vasates lycopersici);唇足目(Chilopoda),例如:地蜈蚧屬(Geophilus spp.)、蚰蜓屬(Scutigera spp.);彈尾目(Collembola),例如:棘跳蟲(Onychiurus armatus);綠圓跳蟲(Sminthurus viridis);重足目(Diplopoda),例如:具斑馬陸(Blaniulus guttulatus);昆蟲綱(Insecta),例如:蜚蠊目(Blattodea)之昆蟲,例如:東方蜚蠊(Blatta orientalis)、蜚蠊(Blattella asahinai)、德國蜚蠊(Blattella germanica)、馬得拉蜚蠊(Leucophaea maderae)、古巴蜚蠊屬(Panchlora spp.)、帕科蜚蠊屬(Parcoblatta spp.)、家蠊(Periplaneta spp.)(例如:美洲家蠊(Periplaneta americana)、澳洲家蠊(Periplaneta australasiae))、美洲家蠊(Supella longipalpa);鞘翅目(Coleoptera),例如:鑲邊黃瓜甲蟲(Acalymma vittatum)、大豆象(Acanthoscelides obtectus)、麗金龜屬(Adoretus spp.)、赤楊紫跳甲(Agelastica alni)、叩頭蟲屬(Agriotes spp.)(例如:具條叩甲(Agriotes linneatus)、小麥金針蟲(Agriotes mancus))、外米擬步行蟲(Alphitobius diaperinus)、六月金龜子(Amphimallon solstitialis)、食骸蟲(Anobium punctatum)、天牛屬(Anoplophora spp.)、棉鈴象甲(Anthonomus spp.)(例如:苜蓿葉象甲(Anthonomus grandis))、蠹屬(Anthrenus spp.)、梨象屬(Apion spp.)、甘蔗金龜屬(Apogonia spp.)、隱食甲屬(Atomaria spp.)(例如:甜菜隱食甲(Atomaria linearis))、小鰹節蟲屬(Attagenus spp.)、象甲(Baris caerulescens)、豆象(Bruchidius obtectus)、豆象甲屬(Bruchus spp.)(例如:豌豆象甲(Bruchus pisorum)、蠶豆象甲(Bruchus rufimanus))、金花蟲屬(Cassida spp.)、大豆葉
甲(Cerotoma trifurcate)、象甲屬(Ceuthorrhynchus spp.)(例如:甘藍莢象甲(Ceutorrhynchus assimilis)、藍籽莖象甲(Ceutorrhynchus quadridens)、油菜象甲(Ceutorrhynchus rapa))、小金花蟲屬(Chaetocnema spp.)(例如:甘薯金花蟲(Chaetocnema confinis)、具齒跳甲(Chaetocnema denticulata)、玉米跳甲(Chaetocnema ectypa))、牛蒡象甲(Cleonus mendicus)、金針蟲屬(Conoderus spp.)、球莖象甲屬(Cosmopolites spp.)(例如:香蕉球莖象甲(Cosmopolites sordidus))、蠐螬(Costelytra zealandica)、叩頭蟲屬(Ctenicera spp.)、象甲屬(Curculio spp.)(例如:核桃象甲(Curculio caryae)、大栗象甲(Curculio caryatrypes)、榛子象甲(Curculio obtusus)、小栗象甲(Curculio sayi))、角胸粉扁蟲(Cryptolestes ferrugineus)、角胸扁蟲(Cryptolestes pusillus)、柳小隱喙象甲(Cryptorhynchus lapathi)、芒果象甲(Cryptorhynchus mangiferae)、莖象甲屬(Cylindrocopturus spp.)、密點細枝象甲(Cylindrocopturus adspersus)、黃杉枝象甲(Cylindrocopturus furnissi)、皮蠹屬(Dermestes spp.)、葉甲屬(Diabrotica spp.)(例如:巴西玉米根蟲(Diabrotica balteata)、北方玉米根蟲(Diabrotica barberi)、南部玉米根蟲(Diabrotica undecimpunctata howardi)、黃瓜十一星葉甲(Diabrotica undecimpunctata undecimpunctata)、玉米根蟲(Diabrotica virgifera virgifera)、墨西哥玉米根蟲(Diabrotica virgifera zeae))、蛀螟屬(Dichocrocis spp.)、水稻鐵甲蟲(Dicladispa armigera)、阿根廷兜蟲屬(Diloboderus spp.)、瓢蟲屬(Epilachna spp.)(例如:南瓜瓢蟲(Epilachna borealis)、食植瓢蟲(Epilachna varivestis))、跳甲屬(Epitrix spp.)(例如:黃瓜跳甲(Epitrix cucumeris)、茄跳甲(Epitrix fuscula)、煙草跳甲(Epitrix hirtipennis)、馬鈴薯跳甲(Epitrix subcrinita)、塊莖跳甲(Epitrix tuberis))、鑽孔蟲屬(Faustinus spp.)、麥蛛甲(Gibbium psylloides)、闊角穀盜(Gnathocerus cornutus)、菜心螟(Hellula undalis)、白蠐螬(Heteronychus arator)、天牛屬(Heteronyx spp.)、
金龜子(Hylamorpha elegans)、象天牛(Hylotrupes bajulus)、苜蓿象甲(Hypera postica)、藍綠象(Hypomeces squamosus)、小蠹屬(Hypothenemus spp.)(例如:咖啡果小蠹(Hypothenemus hampei)、蘋枝小蠹(Hypothenemus obscurus)、果小蠹(Hypothenemus pubescens))、鰓角金龜(Lachnosterna consanguinea)、煙甲蟲(Lasioderma serricorne)、長首穀盜(Latheticus oryzae)、薪甲屬(Lathridius spp.)、負泥甲屬(Lema spp.)、馬鈴薯甲蟲(Leptinotarsa decemlineata)、潛葉蛾屬(Leucoptera spp.)(例如:咖啡潛葉蛾(Leucoptera coffeella))、稻象甲(Lissorhoptrus oryzophilus)、黃象甲屬(Lixus spp.)、黃胸葉甲(Luperomorpha xanthodera)、葉甲屬(Luperodes spp.)、粉蠹屬(Lyctus spp.)、美洲葉甲屬(Megascelis spp.)、叩頭蟲(Melanotus spp.)(例如:奧勒岡州叩甲(Melanotus longulus oregonensis))、花粉甲(Meligethes aeneus)、吹粉金龜(Melolontha spp.)(例如:大栗鰓角金龜(Melolontha melolontha))、天牛屬(Migdolus spp.)、天牛屬(Monochamus spp.)、象甲(Naupactus xanthographus)、郭公蟲屬(Necrobia spp.)、金黃蛛甲(Niptus hololeucus)、犀角金龜(Oryctes rhinoceros)、鋸胸粉扁蟲(Oryzaephilus surinamensis)、稻象甲(Oryzaphagus oryzae)、深溝象甲(Otiorrhynchus spp.)(例如:蘋果白象甲(Otiorhynchus cribricollis)、苜蓿象甲(Otiorhynchus ligustici)、草莓根象甲(Otiorhynchus ovatus)、根象甲(Otiorhynchus rugosostriarus)、黑藤象甲(Otiorhynchus sulcatus))、銀點花金龜(Oxycetonia jucunda)、猿葉蟲(Phaedon cochleariae)、食葉蟲屬(Phyllophaga spp.)、鰓角金龜屬(Phyllophaga helleri)、葉蚤屬(Phyllotreta spp.)(例如:辣根跳甲(Phyllotreta armoraciae)、柔弱黑跳甲(Phyllotreta pusilla)、美條紋跳甲(Phyllotreta ramosa)、黃條葉蚤(Phyllotreta striolata))、日本麗金龜(Popillia japonica)、小象甲屬(Premnotrypes spp.)、大穀蠹(Prostephanus truncatus)、跳甲屬(Psylliodes spp.)(例如:馬鈴薯跳甲(Psylliodes affinis)、油菜蘭跳甲
(Psylliodes chrysocephala)、忽布跳甲(Psylliodes punctulata))、蛛甲屬(Ptinus spp.)、黑根瓢蟲(Rhizobius ventralis)、粉長蠹蟲(Rhizopertha dominica)、米象屬(Sitophilus spp.)(例如:穀象(Sitophilus granarius)、羅望子象(Sitophilus linearis)、米象(Sitophilus oryzae)、玉米象(Sitophilus zeamais))、穀象屬(Sphenophorus spp.)、藥材甲蟲(Stegobium paniceum)、莖象屬(Sternechus spp.)(例如:豆莖象(Sternechus paludatus))、扁肩象屬(Symphyletes spp.)、象甲屬(Tanymecus spp.)(例如:玉米葉象(Tanymecus dilaticollis)、纖毛象(Tanymecus indicus)、紅豆草灰象甲(Tanymecus palliates))、粉甲(Tenebrio molitor)、穀盜(Tenebrioides mauretanicus)、擬穀盜屬(Tribolium spp.)(例如:黑粉榖盜(Tribolium audax)、擬榖盜(Tribolium castaneum)、扁擬榖盜(Tribolium confusum))、鰹節蟲屬(Trogoderma spp.)、象甲屬(Tychius spp.)、虎天牛屬(Xylotrechus spp.)、步甲屬(Zabrus spp.)(例如:玉米步甲(Zabrus tenebrioides));雙翅目(Diptera),例如:伊蚊屬(Aedes spp.)(例如:埃及斑蚊(Aedes aegypti)、白線斑蚊(Aedes albopictus)、叮刺伊蚊(Aedes sticticus)、騷擾伊蚊(Aedes vexans))、潛蠅屬(Agromyza spp.)(例如:寬額斑潛蠅(Agromyza frontella)、美洲黍潛葉蠅(Agromyza parvicornis))、按實蠅屬(Anastrepha spp.)、按蚊屬(Anopheles spp.)(例如:四斑按蚊(Anopheles quadrimaculatus)、甘比亞瘧蚊(Anopheles gambiae))、癭蚊屬(Asphondylia spp.)、實蠅屬(Bactrocera spp.)(例如:瓜實蠅(Bactrocera cucurbitae)、東方果實蠅(Bactrocera dorsalis)、橄欖果蠅(Bactrocera oleae))、毛蚊(Bibio hortulanus)、麗蠅(Calliphora erythrocephala)、紅頭麗蠅(Calliphora vicina)、地中海果實蠅(Ceratitis capitata)、搖蚊屬(Chironomus spp.)金蠅屬(Chrysomyia spp.)、斑虻屬(Chrysops spp.)、麻翅虻(Chrysozona pluvialis)、刺蚊屬(Cochliomyia spp.)、康癭蚊屬(Contarinia
spp.)(例如:葡萄癭蚊(Contarinia johnsoni)、甘藍癭蚊(Contarinia nasturtii)、梨葉癭蚊(Contarinia pyrivora)、向日葵癭蚊(Contarinia schulzi)、高粱癭蚊(Contarinia sorghicola)、麥黃吸漿蟲(Contarinia tritici))、糞蠅(Cordylobia anthropophaga)、環足搖蚊(Cricotopus sylvestris)、庫蚊屬(Culex spp.)(例如:尖音庫蚊(Culex pipiens)、五帶淡色庫蚊(Culex quinquefasciatus))、庫蠓屬(Culicoides spp.)、脈毛蚊屬(Culiseta spp.)、疽蠅屬(Cuterebra spp.)、果蠅(Dacus oleae)、癭蚊屬(Dasyneura spp.)(例如:油菜莢葉癭蚊(Dasineura brassicae))、地種蠅屬(Delia spp.)(例如:蔥地種蠅(Delia antiqua)、麥種蠅(Delia coarctata)、毛跗地種蠅(Delia florilega)、灰地種蠅(Delia platura)、甘藍地種蠅(Delia radicum))、人膚蠅(Dermatobia hominis)、猩猩蠅(Drosophila spp.)(例如:黑腹果蠅(Drosphila melanogaster)、鈴木果蠅(Drosphila suzukii))、象甲屬(Echinocnemus spp.)、廄蠅屬(Fannia spp.)、胃蠅屬(Gastrophilus spp.)、舌蠅屬(Glossina spp.)、麻虻屬(Haematopota spp.)、稻心蠅(Hydrellia spp.)、水稻潛葉蠅(Hydrellia griseola)、種蠅屬(Hylemyia spp.)、虱蠅屬(Hippobosca spp.)、皮蠅屬(Hypoderma spp.)、潛蠅屬(Liriomyza spp.)(例如:白菜斑潛蠅(Liriomyza brassicae)、南美斑潛蠅(Liriomyza huidobrensis)、蔬菜斑潛蠅(Liriomyza sativae))、綠蠅屬(Lucilia spp.)(例如:絲光綠蠅(Lucilia cuprina))、羅蛉屬(Lutzomyia spp.)、沼蚊屬(Mansonia spp.)、家蠅屬(Musca spp.)(例如:家蠅(Musca domestica)、舍蠅(Musca domestica vicina))、狂蠅屬(Oestrus spp.)、瑞典蠅(Oscinella frit)、搖蚊屬(Paratanytarsus spp.)、搖蚊(Paralauterborniella subcincta)、潛蠅屬(Pegomya spp.)(例如:甜菜潛蠅(Pegomya betae)、菠菜潛蠅(Pegomya hyoscyami)、懸鉤子潛蠅(Pegomya rubivora))、白蛉屬(Phlebotomus spp.)、蚤蠅屬(Phorbia spp.)、伏蠅屬(Phormia spp.)、酪蠅(Piophila casei)、癭蚋屬(Prodiplosis spp.)、胡蘿蔔蠅(Psila rosae)、果實蠅屬
(Rhagoletis spp.)(例如:北美櫻桃實蠅(Rhagoletis cingulata)、核桃繞實蠅(Rhagoletis completa)、黑櫻桃實蠅(Rhagoletis fausta)、歐洲甜櫻桃繞實蠅(Rhagoletis indifferens)、藍橘繞實蠅(Rhagoletis mendax)、蘋果果實蠅(Rhagoletis pomonella))、肉蠅屬(Sarcophaga spp.)、蚋屬(Simulium spp.)(例如:南方蚋(Simulium meridionale))、螫蠅屬(Stomoxys spp.)、虻屬(Tabanus spp.)、直斑蠅屬(Tetanops spp.)、大蚊(Tipula spp.)(例如:歐洲大蚊(Tipula paludosa)、牧場大蚊(Tipula simplex)):半翅目(Hemiptera),例如:金合歡昆木虱(Acizzia acaciaebaileyanae)、木虱(Acizzia dodonaeae)、木虱(Acizzia uncatoides)、長頭蝗(Acrida turrita)、無網長管蟲牙屬(Acyrthosipon spp.)(例如:碗豆蚜(Acyrthosiphon pisum))、葉蟬屬(Acrogonia spp.)、Aeneolamia屬、隆脈木虱屬(Agonoscena spp.)、歐洲甘藍粉虱(Aleyrodes proletella)、甘蔗穴粉虱(Aleurolobus barodensis)、棉絮粉虱(Aleurothrixus floccosus)、榴蓮被榴蓮木虱(Allocaridara malayensis)、果葉蝶屬(Amrasca spp.)(例如:二點小綠葉蟬(Amrasca bigutulla)、棉葉蟬(Amrasca devastans))、飛廉短尾蚜(Anuraphis cardui)、腎圓盾介殼蟲屬(Aonidiella spp.)(例如:橘紅腎圓盾介殼蟲(Aonidiella aurantii)、橘黃腎圓盾介殼蟲(Aonidiella citrina)、木瓜腎圓盾介殼蟲(Aonidiella inornata))、梨瘤蚜(Aphanostigma piri)、蚜蟲屬(Aphis spp.)(例如:橘捲菜蚜(Aphis citricola)、豆蚜(Aphis craccivora)、黑豆蚜(Aphis fabae)、草莓根蚜(Aphis forbesi)、大豆蚜(Aphis glycines)、棉蚜(Aphis gossypii)、常春藤蚜(Aphis hederae)、葡萄蔓蚜(Aphis illinoisensis)、蚜蟲(Aphis middletoni)、鼠李馬鈴薯蚜(Aphis nasturtii)、夾竹桃蚜(Aphis nerii)、蘋果蚜(Aphis pomi)、繡線菊蚜(Aphis spiraecola)、莢蒾蚜(Aphis viburniphila))、葡萄二星斑葉蟬(Arboridia apicalis)、木虱屬(Arytainilla spp.)、小圓盾蚧屬(Aspidiella spp.)、圓盾階屬(Aspidiotus
spp.)(例如:夾竹桃圓蚧(Aspidiotus nerii))、Atanus屬、馬鈴薯蚜(Aulacorthum solani)、煙草粉虱(Bemisia tabaci)、芽木虱(Blastopsylla occidentalis)、茶樹蚜木虱(Boreioglycaspis melaleucae)、光管舌尾蚜(Brachycaudus helichrysi)、微管蟲牙屬(Brachycolus spp.)、菜蚜(Brevicoryne brassicae)、梨木虱屬(Cacopsylla spp.)(例如:梨黃木虱(Cacopsylla pyricola))、小褐稻虱(Calligypona marginata)、黃頭大葉蟬(Carneocephala fulgida)、甘蔗綿蚜(Ceratovacuna lanigera)、沫蟬科Cercopidae)、角蠟蚧屬(Ceroplastes spp.)、草莓毛管蚜(Chaetosiphon fragaefolii)、蔗黃雪盾蚧(Chionaspis tegalensis)、茶小綠葉蟬(Chlorita onukii)、臺灣大蝗(Chondracris rosea)、核桃黑斑蚜(Chromaphis juglandicola)、柑橘褐圓蚧(Chrysomphalus ficus)、玉米葉蟬(Cicadulina mbila)、Coccomytilus halli、蚧屬(Coccus spp.)(例如:扁堅蚧(Coccus hesperidum)、長堅蚧(Coccus longulus)、桔軟蠟蟲介(Coccus pseudomagnoliarum)、黃綠蚧(Coccus viridis))、茶藨隱瘤蚜(Cryptomyzus ribis)、Cryptoneossa屬、梳木虱屬(Ctenarytaina spp.)、黃翅葉蜂屬(Dalbulus spp.)、柑桔裸粉虱(Dialeurodes citri)、柑桔木虱(Diaphorina citri)、盾蚧屬(Diaspis spp.)、草履蚧屬(Drosicha spp.)、莖蚜蟲屬(Dysaphis spp.)(例如:銹條蚜(Dysaphis apiifolia)、車前圓尾蚜(Dysaphis plantaginea)、鬱金香鱗莖蚜蟲(Dysaphis tulipae))、灰粉蚧屬(Dysmicoccus spp.)、小綠葉蟬屬(Empoasca spp.)(例如:馬鈴薯葉蟬(Empoasca abrupta)、馬鈴薯葉蟬(Empoasca fabae)、蘋果小綠葉蟬(Empoasca maligna)、茄微葉蟬(Empoasca solana)、史蒂芬氏葉蟬(Empoasca stevensi))、綿蚜屬(Eriosoma spp.)(例如:美國綿蚜(Eriosoma americanum)、蘋果綿蚜(Eriosoma lanigerum)、居梨綿蚜(Eriosoma pyricola))、斑葉蟬屬(Erythroneura spp.)、檸檬桉木虱屬(Eucalyptolyma spp.)、褐木風屬(Euphyllura spp.)、鈍鼻葉蟬(Euscelis bilobatus)、拂粉蚧屬(Ferrisia spp.)、咖
啡粉蚧(Geococcus coffeae)、木虱屬(Glyeaspis spp.)、銀合歡木虱(Heteropsylla cubana)、頰木虱(Heteropsylla spinulosa)、褐透翅尖頭大葉蟬(Homalodisca coagulata)、桃大尾蚜(Hyalopterus arundinis)、桃粉蚜(Hyalopterus pruni)、吹綿蚧屬(Icerya spp.)(例如:吹綿蚧(Icerya purchasi))、片角葉蟬屬(Idiocerus spp.)、綠葉蟬屬(Idioscopus spp.)、灰飛虱(Laodelphax striatellus)、球蚧屬(Lecanium spp.)(例如:李蠟蚧(Lecanium corni)(=褐盔蠟蚧(Parthenolecanium corni))、蠣盾蚧屬(Lepidosaphes spp.)(例如:榆蠣盾蚧(Lepidosaphes ulmi))、偽菜蚜(Lipaphis erysimi)、斑衣蠟蟬(Lycorma delicatula)、長管蚜屬(Macrosiphum spp.)(例如:馬鈴薯長管蚜(Macrosiphum euphorbiae)、長管蚜(Macrosiphum lilii)、薔薇長管蚜(Macrosiphum rosae))、長針葉蟬(Macrosteles facifrons)、沫蝶屬(Mahanarva spp.)、黍蚜(Melanaphis sacchari)、Metcalfiella屬、蛾蠟蟬(Metcalfa pruinosa)、麥無網蚜(Metopolophium dirhodum)、黑緣平翅斑蚜(Monellia costalis)、胡桃黑蚜(Monelliopsis pecanis)、桃蚜屬(Myzus spp.)(例如:冬蔥瘤額蚜(Myzus ascalonicus)、李瘤蚜(Myzus cerasi)、女貞瘤額蚜(Myzus ligustri)、堇菜瘤蚜(Myzus ornatus)、桃赤蚜(Myzus persicae)、煙草蚜(Myzus nicotianae))、萵苣蚜(Nasonovia ribisnigri)、黑尾葉蟬屬(Nephotettix spp.)(例如:偽黑尾葉蟬(Nephotettix cincticeps)、黑條黑尾葉蟬(Nephotettix nigropictus))、褐飛虱(Nilaparvata lugens)、Oncometopia屬、旌蚧(Orthezia praelonga)、中華稻蝗(Oxya chinensis)、癭木虱屬(Pachypsylla spp.)、楊梅粉虱(Parabemisia myricae)、木虱屬(Paratrioza spp.)(例如:番茄木虱(Paratrioza cockerelli))、片盾蚧屬(Parlatoria spp.)、癭綿蚜屬(Pemphigus spp.)(例如:白楊癭綿蚜(Pemphigus bursarius)、多脈癭綿蚜(Pemphigus populivenae))、玉米飛虱(Peregrinus maidis)、粉蚧屬(Phenacoccus spp.)(例如:美地綿粉蚧(Phenacoccus madeirensis))、楊平翅棉蚜(Phloeomyzus passerinii)、
瘤蚜(Phorodon humuli)、桃根蚜屬(Phylloxera spp.)(例如:核桃根瘤蚜(Phylloxera devastatrix)、警根瘤蚜(Phylloxera notabilis))、橘長盾蚧(Pinnaspis aspidistrae)、粉蚧屬(Planococcus spp.)(例如:柑桔粉蚧(Planococcus citri))、黃粉蚧(Prosopidopsylla flava)、梨形原棉蚧(Protopulvinaria pyriformis)、桑白蚧(Pseudaulacaspis pentagona)、粉蚧屬(Pseudococcus spp.)(例如:柑桔棲粉蚧(Pseudococcus calceolariae)、康氏粉蚧(Pseudococcus comstocki)、長尾粉蚧(Pseudococcus longispinus)、葡萄粉蚧(Pseudococcus maritimus)、暗色粉蚧(Pseudococcus viburni))、Psyllopsis屬、梨木虱蟲(Psylla spp.)(例如:黃楊木虱(Psylla buxi)、蘋木虱(Psylla mali)、梨木虱(Psylla pyri))、金小蜂屬(Pteromalus spp.)、飛虱屬(Pyrilla spp.)、圓蚧屬(Quadraspidiotus spp.)(例如:胡桃圓盾蚧(Quadraspidiotus juglansregiae)、正楊笠圓盾蚧(Quadraspidiotus ostreaeformis)、梨圓盾蚧(Quadraspidiotus perniciosus))、Quesada gigas、粉蚧屬(Rastrococcus spp.)、頸狀蚜屬(Rhopalosiphum spp.)(例如:玉米蚜(Rhopalosiphum maidis)、縊管蚜(Rhopalosiphum oxyacanthae)、稻麥蚜(Rhopalosiphum padi)、紅腹縊管蚜(Rhopalosiphum rufiabdominale))、硬蚧屬(Saissetia spp.)(例如:咖啡硬蚧(Saissetia coffeae)、硬蚧(Saissetia miranda、Saissetia neglecta)、工脊硬蚧(Saissetia oleae))、螻蛄(Scaphoides titanus)、麥二叉蚜(Schizaphis graminum)、盾蚧(Selenaspidus articulatus)、麥長管蚜(Sitobion avenae)、飛虱屬(Sogata spp.)、白背飛虱(Sogatella furcifera)、飛虱屬(Sogatodes spp.)、沫蟬(Stictocephala festina)、梣粉虱(Siphoninus phillyreae)、聲蚜(Tenalaphara malayensis)、Tetragonocephela屬、核桃黑蚜(Tinocallis caryaefoliae)、沫蟬屬(Tomaspis spp.)、二叉蚜屬(Toxoptera spp.)(例如:小桔蚜(Toxoptera aurantii)、大桔蚜(Toxoptera citricidus))、溫室粉虱(Trialeurodes vaporariorm)、木虱屬(Trioza spp.)(例如:棉木虱(Trioza diospyri))、紅閃小
葉蟬屬(Typhlocyba spp.)、盾蚧屬(Unaspis spp.)、葡萄根瘤蚜(Viteus vitifolii)、斑點鋸蜂屬(Zygina spp.);異翅亞目(Heteroptera),例如:南瓜緣蝽(Anasa tristis)、芒果蝽屬(Antestiopsis spp.)、紅緣蝽屬(Boisea spp.)、麥長蝽屬(Blissus spp.)、盲蝽屬(Calocoris spp.)、盲蝽(Campylomma livida)、二尾蚜屬(Cavelerius spp.)、臭蟲屬(Cimex spp.)(例如:臭蟲(Cimex adjunctus)、熱帶臭蟲(Cimex hemipterus)、床蝨(Cimex lectularius)、蝠臭蟲(Cimex pilosellus))、盲蝽屬(Collaria spp.)、盲蝽(Creontiades dilutus)、胡椒緣蝽(Dasynus piperis)、二葉喙蝽(Dichelops furcatus)、胡椒網蝽(Diconocoris hewetti)、蝽象屬(Dysdercus spp.)、臭蝽屬(Euschistus spp.)(例如:大豆褐蝽(Euschistus heros)、褐臭蝽(Euschistus servus)、暗淡蝽象(Euschistus tristigmus)、一點褐蝽(Euschistus variolarius))、刺蝽屬(Eurygaster spp.)、褐翅蝽象(Halyomorpha halys)、夜蛾屬(Heliopeltis spp.)、稻緣蜂(Horcias nobilellus)、豬緣蝽屬(Leptocorisa spp.)、稻緣蝽象(Leptocorisa varicornis)、西方針葉樹種子甲蟲(Leptoglossus occidentalis)、葉足緣蝽(Leptoglossus phyllopus)、麗盲蝽屬(Lygocoris spp.)(例如:原麗盲蝽(Lygocoris pabulinus))、盲蝽屬(Lygus spp.)(例如:豆莢灰盲蝽(Lygus elisus)、豆莢草盲蝽(Lygus hesperus)、美國牧草盲蝽(Lygus lineolaris))、蔗黑長蝽(Macropes excavatus)、金光綠盲蝽(Monalonion atratum)、綠蝽屬(Nezara spp.)(例如:稻綠蝽象(Nezara viridula))、盾蝽屬(Oebalus spp.)、擬配軍蟲(Piesma quadrata)、壁蝽屬(Piezodorus spp.)(例如:紅蝽(Piezodorus guildinii))、盲蝽屬(Psallus spp.)、駱梨盲蝽象(Pseudacysta persea)、紅腹獵蝽屬(Rhodnius spp.)、可哥褐盲蝽(Sahlbergella singularis)、土蝽(Scaptocoris castanea)、稻黑蝽屬(Scotinophora spp.)、梨花網蝽(Stephanitis nashi)、臭蟲屬(Tibraca spp.)、椎蝽屬(Triatoma spp.);
膜翅目(Hymenoptera),例如:切葉蟻(Acromyrmex spp.)、葉蜂屬(Athalia spp.)(例如:紅角菜葉蜂(Athalia rosae))、切葉蟻屬(Atta spp.)、松葉蜂屬(Diprion spp.)(例如:歐洲赤松葉蜂(Diprion similis))、葉蜂屬(Hoplocampa spp.)(例如:櫻實葉蜂(Hoplocampa cookei)、蘋果葉蜂(Hoplocampa testudinea))、蟻屬(Lasius spp.)、廚蟻(Monomorium pharaonis)、樹蜂(Sirex spp.)、入侵紅火蟻(Solenopsis invicta)、酸臭蟻屬((Tapinoma spp.)、樹蜂(Urocerus spp.)、胡蜂屬(Vespa spp.)(例如:黃邊胡蜂(Vespa crabro))、樹蜂屬(Xeris spp.);等足目(Isopoda),例如:鼠婦(Armadillidium vulgare)、海蛆(Oniscus asellus)、球鼠婦(Porcellio scaber);等翅目(Isoptera),例如:乳白蟻(Coptotermes spp.)(例如:台灣家白蟻(Coptotermes formosanus))、白蟻(Cornitermes cumulans)、堆砂白蟻屬(Cryptotermes spp.)、楹白蟻(Incisitermes spp.)、甘蔗白蟻(Microtermes obesi)、土白蟻屬(Odontotermes spp.)、白蟻屬(Reticulitermes spp.)(例如:黃肢散白蟻(Reticulitermes flavipes)、西方犀白蟻(Reticulitermes hesperus)):鱗翅目(Lepidoptera),例如:小蠟蛾(Achroia grisella)、梁劍紋夜蛾(Acronicta major)、卷葉蛾屬(Adoxophyes spp.)(例如:棉褐帶卷蛾(Adoxophyes orana))、電紋夜蛾(Aedia leucomelas)、地老虎屬(Agrotis spp.)(例如:黃地老虎(Agrotis segetum)、小地老虎(Agrotis ipsilon))、棉葉波紋夜蛾(Alabama spp.)(例如:棉葉波紋夜蛾(Alabama argillacea))、蘋果蠹蛾(Amyelois transitella)、條麥蛾屬(Anarsia spp.)、夜蛾屬(Anticarsia spp.)(例如:大豆夜蛾(Anticarsia gemmatalis))、黃螟屬(Argyroploce spp.)、甘藍夜蛾(Barathra brassicae)、單帶弄蝶(Borbo cinnara)、棉葉穿孔潛蛾(Bucculatrix thurberiella)、松尺蠖(Bupalus piniarius)、夜蛾屬(Busseola spp.)、卷葉蛾屬(Cacoecia spp.)、茶細
蛾(Caloptilia theivora)、煙捲葉蛾(Capua reticulana)、蘋果蠹蛾(Carpocapsa pomonella)、桃蛀果蛾(Carposina niponensis)、冬尺蛾(Cheimatobia brumata)、螟屬(Chilo spp.)(例如:稻秆螟(Chilo plejadellus)、二化螟(Chilo suppressalis))、雲杉卷葉蛾屬(Choristoneura spp.)、葡萄果蠹蛾(Clysia ambiguella)、卷螟屬(Cnaphalocerus spp.)、稻縱捲葉野螟蛾(Cnaphalocrocis medinalis)、雲卷蛾屬(Cnephasia spp.)、細蛾屬(Conopomorpha spp.)、黑象甲屬(Conotrachelus spp.)、夜蛾屬(Copitarsia spp.)、小卷蛾屬(Cydia spp.)(例如:豆英小卷蛾(Cydia nigricana)、蘋果蠹蛾(Cydia pomonella))、夜蛾(Dalaca noctuides)、野螟屬(Diaphania spp.)、小蔗螟(Diatraea saccharalis)、埃及金剛鑽屬(Earias spp.)、柑橘果蛾(Ecdytolopha aurantium)、南美玉米苗斑螟(Elasmopalpus lignosellus)、非洲莖螟(Eldana saccharina)、粉螟屬(Ephestia spp.)(例如:烟草粉螟(Ephestia elutella)、地中海斑螟(Ephestia kuehniella))、小卷蛾屬(Epinotia spp.)、蘋果飛蛾(Epiphyas postvittana)、螟蛾屬(Etiella spp.)、巧言蟲屬(Eulia spp.)、環針單紋卷蛾(Eupoecilia ambiguella)、毒蛾屬(Euproctis spp.)(例如:棕尾毒蛾(Euproctis chrysorrhoea))、切根蟲屬(Euxoa spp.)、褐夜蛾屬(Feltia spp.)、大蠟螟(Galleria mellonella)、潛葉細蛾屬(Gracillaria spp.)、小食心蟲屬(Grapholitha spp.)(例如:桃折心蟲(Grapholita molesta)、蘋小果蠹(Grapholita prunivora))、螟蛾屬(Hedylepta spp.)、夜蛾屬(Helicoverpa spp.)(例如:番茄夜蛾(Helicoverpa armigera)、玉米夜蛾(Helicoverpa zea))、棉鈴蟲屬(Heliothis spp.)(例如:綠棉鈴蟲(Heliothis virescens))、褐織夜蛾(Hofmannophila pseudospretella)、斑螟屬(Homoeosoma spp.)、卷葉蛾屬(Homona spp.)、櫻桃巢蛾(Hyponomeuta padella)、柿食心蟲(Kakivoria flavofasciata)、黏蟲屬(Laphygma spp.)、茄黃斑螟(Leucinodes orbonalis)、潛葉蛾屬(Leucoptera spp.)(例如:咖啡潛葉蛾(Leucoptera coffeella))、細蛾屬(Lithocolletis spp.)(例
如:斑幕潛葉蛾(Lithocolletis blancardella)、綠果夜蛾(Lithophane antennata))、卷蛾屬(Lobesia spp.)(例如:葡萄莓果飛蛾(Lobesia botrana))、豆白緣切根蟲(Loxagrotis albicosta)、毒蛾屬(Lymantria spp.)(例如:舞毒蛾(Lymantria dispar))、萊氏蛾屬(Lyonetia spp.)(例如:桃潛葉蛾(Lyonetia clerkella))、金龜(Malacosoma neustria)、豆莢螟(Maruca testulalis)、甘藍夜蛾(Mamstra brassicae)、暮眼蝶(Melanitis leda)、莖夜蛾屬(Mocis spp.)、榖蛾科(Monopis obviella)、東方黏蟲(Mythimna separate)、穀蛾(Nemapogon cloacellus)、水螟屬(Nymphula spp.)、扇頭蜱屬(Oiketicus spp.)、夜蛾屬(Oria spp.)、螟蛾屬(Orthaga spp.)、玉米螟屬(Ostrinia spp.)(例如:歐洲玉米螟(Ostrinia nubilalis))、橙足負泥蟲(Oulema melanopus)、稻負泥蟲(Oulema oryzae)、小眼夜蛾(Panolis flammea)、弄蝶屬(Parnara spp.)、紅鈴蟲屬(Pectinophora spp.)(例如:棉紅鈴蟲(Pectinophora gossypiella))、潛葉蛾屬(Perileucoptera spp.)、蠹蛾屬(Phthorimaea spp.)(例如:馬鈴薯塊莖蛾(Phthorimaea operculella))、橘葉潛蛾(Phyllocnistis citrella)、細蛾屬(Phyllonorycter spp.)(例如:斑幕潛葉(Phyllonorycter blancardella)、山楂潛葉蛾(Phyllonorycter crataegella))、粉蝶屬(Pieris spp.)(例如:紋白蝶(Pieris rapae))、荷蘭石竹小卷蛾(Platynota stultana)、印度穀斑螟(Plodia interpunctella)、擬尺蠖屬(Plusia spp.)、小菜蛾(Plutella xylostella)(=小菜蛾(Plutella maculipennis))、巢蛾屬(Prays spp.)、黏蟲屬(Prodenia spp.)、天蛾屬(Protoparce spp.)、黏蟲屬(Pseudaletia spp.)(例如:星黏蟲(Pseudaletia unipuncta))、大豆夜蛾(Pseudoplusia includens)、野螟(Pyrausta nubilalis)、薄荷灰夜蛾(Rachiplusia nu)、三化螟屬(Schoenobius spp.)(例如:三化螟(Schoenobius bipunctifer))、白禾螟蛾屬(Scirpophaga spp.)(例如:稻白螟(Scirpophaga innotata))、黃地老虎(Scotia segetum)、蛀莖夜蛾屬(Sesamia spp.)(例如:稻蛀莖夜蛾(Sesamia inferens))、卷葉蛾屬
(Sparganothis spp.)、斜紋夜蛾屬(Spodoptera spp.)(例如:斜紋夜蛾(Spodoptera eradiana)、甜菜夜蛾(Spodoptera exigua)、草地斜紋夜蛾(Spodoptera frugiperda)、灰翅夜蛾(Spodoptera praefica))、舉肢蛾屬(Stathmopoda spp.)、潛葉蟲(Stomopteryx subsecivella)、透翅蛾屬(Synanthedon spp.)、馬鈴薯塊莖蛾(Tecia solanivora)、幹煞夜蛾(Thermesia gemmatalis)、軟木長角蛾(Tinea cloacella)、網衣蛾(Tinea pellionella)、袋穀蛾(Tineola bisselliella)、櫟綠卷葉蛾屬(Tortrix spp.)、毛氈衣蛾(Trichophaga tapetzella)、夜蛾屬(Trichoplusia spp.)(例如:粉紋夜蛾(Trichoplusia ni))、三化螟(Tryporyza incertulas)、番茄斑潛蠅(Tuta absoluta)、小灰蝶科(Virachola spp.);直翅目(Orthoptera)或跳躍亞目(Saltatoria),例如:家蟋蟀(Acheta domesticus)、草蜢屬(Dichroplus spp.)、螻蛄屬(Gryllotalpa spp.)(例如:歐洲螻蛄(Gryllotalpa gryllotalpa))、蔗蝗屬(Hieroglyphus spp.)、飛蝗屬(Locusta spp.)(例如:東亞飛蝗(Locusta migratoria))、負蝗屬(Melanoplus spp.)(例如:赤地蚱蜢(Melanoplus devastator))、烏蘇裏擬寰螽(Paratlanticus ussuriensis)、群居蚱蜢(Schistocerca gregaria);毛蝨目(Phthiraptera),例如:毛蝨屬(Damalinia spp.)、豬蝨屬(Haematopinus spp.)、大蝨屬(Linognathus spp.)、人蝨屬(Pediculus spp.)、長角羽蝨(Phylloera vastatrix)、陰蝨(Pthirus pubis)、獸鳥蝨屬(Trichodectes spp.);囓蟲目(Psocoptera),例如:齧蟲屬(Lepinatus spp.)、書蝨屬(Liposcelis spp.);蚤目(Siphonaptera),例如:鼠蚤屬(Ceratophyllus spp.)、櫛頭蚤屬(Ctenocephalides spp.)(例如: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:玉米黃薊馬(Anaphothrips obscurus)、稻薊馬(Baliothrips biformis)、葡萄德薊馬(Drepanothris reuteri)、黃帶薊馬(Enneothrips flavens)、花薊馬屬(Frankliniella spp.)(例如:煙褐花薊馬(Frankliniella fusca)、西方花薊馬(Frankliniella occidentalis)、梳缺花薊馬(Frankliniella schultzei)、麥花薊馬(Frankliniella tritici)、越桔花薊馬(Frankliniella vaccinii)、威廉期花薊馬(Frankliniella williamsi))、網薊馬屬(Heliothrips spp.)、溫室條籬薊馬(Hercinothrips femoralis)、葡萄薊馬(Rhipiphorothrips cruentatus)、硬薊馬屬(Scirtothrips spp.)、薊馬(Taeniothrips cardamoni)、薊馬屬(Thrips spp.)(例如:南黃薊馬(Thrips palmi)、蔥薊馬(Thrips tabaci));纓尾目(Zygentoma)(=總尾目(Thysanura)),例如:櫛衣魚屬(Ctenolepisma spp.)、西洋衣魚(Lepisma saccharina)、盜火蟲(Lepismodes inquilinus)、斑衣魚(Thermobia domestica);結合綱(Symphyla),例如:蚰蜒屬(Scutigerella spp.),例如:白松蟲(Scutigerella immaculata);軟體動物門(Mollusca)之害蟲,例如:雙殼綱(Bivalva),例如:飾貝屬(Dreissena spp.)及腹足綱(Gastropoda),例如:蛞蝓屬(Arion spp.)(例如:紅蛞蝓(Arion ater rufus))、紅扁蜷屬(Biomphalaria spp.)、泡螺屬(Bulinus spp.)、灰蛞蝓屬(Deroceras spp.)(例如:黏液蛞蝓(Deroceras leave))、土蝸螺屬(Galba spp.)、椎實螺屬(Lymnaea spp.)、釘螺屬(Oncomelania spp.)、福壽螺屬(Pomacea spp.)、琥珀螺屬(Succinea spp.);來自扁形動物門(Plathelminthes)與線蟲綱(Nematoda)之動物與人類寄生蟲,例如:肺線蟲屬(Aelurostrongylus spp.)、裂口線蟲屬(Amidostomum spp.)、
鉤蟲屬(Ancylostoma spp.)、住血線蟲屬(Angiostrongylus spp.)、海獸胃線蟲屬(Anisakis spp.)、裸頭絛蟲屬(Anoplocephala spp.)、蛔蟲屬(Ascaris spp.)、禽蛔屬(Ascaridia spp.)、貝利蛔蟲屬(Baylisascaris spp.)、布魯線蟲(Brugia spp.)、仰口線蟲屬(Bunostomum spp.)、毛細線蟲屬(Capillaria spp.)、腸線蟲屬(Chabertia spp.)、支澤吸蟲屬(Clonorchis spp.)、古柏屬(Cooperia spp.)、環體線蟲屬(Crenosoma spp.)、節蟲屬(Cyathostoma spp.)、雙腔吸蟲屬(Dicrocoelium spp.)、網尾線蟲屬(Dictyocaulus spp.)、二葉槽蟲屬(Diphyllobothrium spp.)、瓜實絛蟲屬(Dipylidium spp.)、血直絲蟲屬(Dirofilaria spp.)、龍線蟲屬(Dracunculus spp.)、球絛蟲屬(Echinococcus spp.)、棘口吸蟲屬(Echinostoma spp.)、蟯蟲屬(Enterobius spp.)、優鞘線蟲屬(Eucoleus spp.)、吸蟲屬(Faciola spp.)、擬片形吸蟲屬(Fascioloides spp.)、薑片蟲屬(Fasciolopsis spp.)、類絲線蟲屬(Filaroides spp.)、筒線蟲屬(Gongylonema spp.)、三代蟲屬(Gyrodactylus spp.)、馬胃線蟲屬(Habronema spp.)、血矛線蟲屬(Haemonchus spp.)、螺旋線蟲屬(Heligmosomoides spp.)、異刺線蟲屬(Heterakis spp.)、膜殼絛蟲屬(Hymenolepis spp.)、下圓線蟲屬(Hyostrongulus spp.)、光絲蟲屬(Litomosoides spp.)、羅阿絲蟲(Loa spp.)、後圓線蟲屬(Metastrongylus spp.)、次睾吸蟲屬(Metorchis spp.)、中殖孔屬絛蟲屬(Mesocestoides spp.)、莫尼茨絛蟲屬(Moniezia spp.)、繆勒線蟲屬(Muellerius spp.)、鉤蟲屬(Necator spp.)、細頸線蟲屬(Nematodirus spp.)、日圓線蟲屬(Nippostrongylus spp.)、結線蟲屬(Oesophagostomum spp.)、壺肛線蟲屬(Ollulanus spp.)、盤尾線蟲(Onchocerca spp.)、後睪吸蟲屬(Opisthorchis spp.)、奧斯勒絲蟲屬(Oslerus spp.)、胃絲蟲屬(Ostertagia spp.)、尖尾線蟲屬(Oxyuris spp.)、毛細線蟲屬(Paracapillaria spp.)、類絲蟲屬(Parafilaria spp.),並殖吸蟲屬(Paragonimus spp.)、雙口吸蟲屬(Paramphistomum spp.)、副裸頭
絛蟲屬(Paranoplocephala spp.)、副蛔屬(Parascaris spp.)、栓尾線蟲屬(Passalurus spp.)、原圓線蟲屬(Protostrongylus spp.)、血吸蟲屬(Schistosoma spp.)、絲狀線蟲屬(Setaria spp.)、旋尾線蟲屬(Spirocerca spp.)、冠絲蟲屬(Stephanofilaria spp.)、冠尾線蟲屬(Stephanurus spp.)、糞類圓線蟲屬(Strongyloides spp.)、圓線蟲屬(Strongylus spp.)、比翼線蟲屬(Syngamus spp.)、帶絛蟲(Taenia spp.)、牛胃絲蟲屬(Teladorsagia spp.)、吸吮線蟲屬(Thelazia spp.)、弓蛔屬(Toxascaris spp.)、弓首線蟲屬(Toxocara spp.)、旋毛線蟲屬(Trichinella spp.)、毛畢屬(Trichobilharzia spp.)、毛圓線蟲屬(Trichostrongulus spp.)、鞭蟲(Trichuris spp.)、彎口線蟲屬(Uncinaria spp.)、吳策線蟲屬(Wuchereria spp.);來自線蟲綱(Nematoda)之植物害蟲,亦即植物寄生性線蟲,特定言之:墊刃線蟲屬(Aglenchus spp.)(例如:居農野外墊刃線蟲(Aglenchus agricola))、粒癭線蟲屬(Anguina spp.)(例如:小麥粒癭線蟲(Anguina tritici))、滑刃線蟲屬(Aphelenchoides spp.)(例如:花生滑刃線蟲(Aphelenchoides arachidis)、葉芽滑刃線蟲(Aphelenchoides fragariae))、刺線蟲屬(Belonolaimus spp.)(例如:豌豆刺線蟲(Belonolaimus gracilis)、長尾刺線蟲(Belonolaimus longicaudatus)、諾頓刺線蟲(Belonolaimus nortoni))、傘滑刃線蟲屬(Bursaphelenchus spp.)(例如:椰子紅環腐線蟲(Bursaphelenchus cocophilus)、傘滑刃線蟲(Bursaphelenchus eremus)、松材線蟲(Bursaphelenchus xylophilus))、固著線蟲屬(Cacopaurus spp.)(例如:波斯固著線蟲(Cacopaurus pestis))、環紋線蟲屬(Criconemella spp.)(例如:彎曲環紋線蟲(Criconemella curvata)、環紋線蟲(Criconemella onoensis)、裝飾環紋線蟲(Criconemella ornata)、環紋線蟲(Criconemella rusium)、葡萄環紋線蟲(Criconemella xenoplax)(=環腐線蟲(Mesocriconema xenoplax))、小環線蟲屬(Criconemoides spp.)(例如:弗尼亞
小環線蟲(Criconemoides ferniae)、小環線蟲(Criconemoides onoense)、杯口小環線蟲(Criconemoides ornatum))、莖囊線蟲(Ditylenchus spp.)(例如:莖線蟲(Ditylenchus dipsaci))、錐線蟲屬(Dolichodorus spp.)、包囊線蟲屬(Globodera spp.)(例如:馬鈴薯白線蟲(Globodera pallida)、黃色馬鈴薯包囊線蟲(Globodera rostochiensis))、螺旋線蟲屬(Helicotylenchus spp.)(例如:雙宮螺旋線蟲(Helicotylenchus dihystera))、半鞘線蟲屬(Hemicriconemoides spp.)、鞘線蟲屬(Hemicycliophora spp.)、異皮線蟲屬(Heterodera spp.)(例如:禾穀異皮線蟲(Heterodera avenae)、大豆異皮線蟲(Heterodera glycines)、甜菜異皮線蟲(Heterodera schachtii))、紐帶線蟲屬(Hoplolaimus spp.)、長刺線蟲屬(Longidorus spp.)(例如:非洲長刺線蟲(Longidorus africanus))、根瘤線蟲屬(Meloidogyne spp.)(例如:奇特伍德根瘤線蟲(Meloidogyne chitwoodi)、法克斯根瘤線蟲(Meloidogyne fallax)、北方根瘤線蟲(Meloidogyne hapla)、南方根瘤線蟲(Meloidogyne incognita))、根瘤線蟲屬(Meloinema spp.)、假根瘤線蟲屬(Nacobbus spp.)、擬莖線蟲屬(Neotylenchus spp.)、擬滑刃線蟲屬(Paraphelenchus spp.)、擬毛刺線蟲屬(Paratrichodorus spp.)(例如:微小擬毛刺線蟲(Paratrichodorus minor))、短體線蟲屬(Pratylenchus spp.)(例如:穿刺短體線蟲(Pratylenchus penetrans))、假海矛線蟲屬(Pseudohalenchus spp.)、平滑墊刃線蟲屬(Psilenchus spp.)、胞囊線蟲屬(Punctodera spp.)、溝線蟲屬(Quinisulcius spp.)、穿孔線蟲屬(Radopholus spp.)(例如:柑橘穿孔線蟲(Radopholus citrophilus)、香蕉穿孔線蟲(Radopholus similis))、腎狀線蟲屬(Rotylenchulus spp.)、盤旋線蟲屬(Rotylenchus spp.)、螺旋線蟲屬(Scutellonema spp.)、粒線蟲屬(Subanguina spp.)、毛刺線蟲屬(Trichodorus spp.)(例如:鈍毛刺線蟲(Trichodorus obtusus)、原始毛刺線蟲(Trichodorus primitivus))、矮化線蟲屬(Tylenchorhynchus spp.)(例如:飾環矮化線蟲
(Tylenchorhynchus annulatus))、半穿刺線蟲屬(Tylenchulus spp.)(例如:柑橘半穿刺線蟲(Tylenchulus semipenetrans))、劍線蟲屬(Xiphinema spp.)(例如:標準劍線蟲(Xiphinema index));此外亦可控制原生動物亞界(Protozoa),球蟲目(Coccidia),例如:艾美球蟲屬(Eimeria spp.)。
本文中,術語"線蟲"包括線蟲目(Nematoda)之所有物種及特定言之寄生在植物或真菌上(例如:來自滑刃目(Aphelenchida)、根瘤線蟲目(Meloidogyne)、墊刃目(Tylenchida)及其他之物種)或人類及動物上(例如:來自毛形亞目(Trichinellida)、墊刃目(Tylenchida)、小桿亞目(Rhabditina)及旋尾目(Spirurida)之物種)並在此等生物體中或生物體上造成傷害之所有寄生蟲物種,及其他寄生性蠕蟲。
本文所說明用於保護作物之殺線蟲劑可以控制線蟲。
術語"控制線蟲"係指殺死線蟲或防止或阻礙其發展或生長,或防止或阻礙其滲透植物組織或吸食植物組織。
此時,化合物之效力之決定法係在經過式(I)、(Ia)、(Ib)或(Ic)化合物處理之植物、植株部分或經過處理之土壤與未經過處理之植物、植株部分或未經過處理之土壤(100%)之間,比較線蟲之死亡率、蟲癭之形成、囊胞之形成、每單位體積土壤之線蟲密度、每支根之線蟲密度、每單位體積土壤之線蟲卵數量、線蟲感染率。此時,與未經過處理之植物、植株部分或未經過處理之土壤比較,較佳係達成降低25-50%,特別佳係降低51-79%及極特別佳係完全殺死及完全防止線蟲發展及生長,達降低80至100%。本文說明之線蟲控制亦包括控制線蟲繁殖(例如:囊胞與/或卵之發展)。式(I)、(Ia)、(Ib)或(Ic)化合物可用於保持植物或動物健康,且其可用於
治癒性、預防性或系統性控制線蟲。
熟悉此相關技術者均習知決定線蟲死亡率、蟲癭形成、囊胞形成、每單位體積土壤之線蟲密度、每支根之線蟲密度、每單位體積土壤之線蟲卵數量、線蟲感染率之方法。
使用式(I)、(Ia)、(Ib)或(Ic)化合物可保持植物健康,亦包括降低線蟲所造成之植物損害,及提高產量。
本文中,術語"植物線蟲"係指包括所有會傷害植物之線蟲。植物線蟲包括植物寄生性線蟲及土壤源性線蟲。植物寄生性線蟲包括(但不限於):體外寄生蟲,如:劍線蟲屬(Xiphinema spp.)、長刺線蟲屬(Longidorus spp.)及毛刺線蟲屬(Trichodorus spp.);半寄生蟲,如:鴕形線蟲屬(Tylenchulus spp.);遊走性體內寄生蟲,如:短體線蟲屬(Pratylenchus spp.)、穿孔線蟲屬(Radopholus spp.)及盾線蟲屬(Scutellonerna spp.);非遊走性寄生蟲,如:異皮線蟲屬(Heterodera spp.)、黃金線蟲屬(Globoderal spp.)及根瘤線蟲屬(Meloidogyne spp.),及莖與葉部之體內寄生蟲,如:莖線蟲屬(Ditylenchus spp.)、滑刃線蟲屬(Aphelenchoides spp.)及穿根線蟲屬(Hirshmaniella spp.)。特別傷害根部之寄生性土壤線蟲為例如:異皮線蟲屬(Heterodera)或黃金線蟲屬(Globodera)之包囊形成性線蟲,與/或根瘤線蟲屬(Meloidogyne)之根瘤線蟲。此等屬類之傷害性物種為例如:南方根瘤線蟲(Meloidogyne incognita)、大豆包囊線蟲(大豆異皮線蟲(Heterodera glycines))、馬鈴薯白線蟲(Globodera pallida)及馬鈴薯黃金線蟲(Globodera rostochiensis)(黃色馬鈴薯包囊線蟲),本文所說明化合物可有效控制此等物種。然而,本文所說明化合物絕未僅限於此等屬類或物種,而係亦可依相同方式沿用於其他線蟲。
植物線蟲包括(但不限於):例如:居農野外墊刃線蟲(Aglenchus agricola)、小麥粒癭線蟲(Anguina tritici)、花生滑刃線蟲
(Aphelenchoides arachidis)、草莓滑刃線蟲(Aphelenchoides fragaria),及滑刃線蟲屬(Aphelenchoides spp.)之莖與葉部體內寄生蟲;豌豆刺線蟲(Belonolaimus gracilis)、長尾刺線蟲(Belonolaimus longicaudatus)、諾頓刺線蟲(Belonolaimus nortoni)、椰子紅環腐線蟲(Bursaphelenchus cocophilus)、傘滑刃線蟲(Bursaphelenchus eremus)、松材線蟲(Bursaphelenchus xylophilus)及傘滑刃線蟲屬(Bursaphelenchus spp.):波斯固著線蟲(Cacopaurus pestis)、彎曲環紋線蟲(Criconemella curvata)、環紋線蟲(Criconemella onoensis)、裝飾環紋線蟲(Criconemella ornata)、環紋線蟲(Criconemella rusium)、葡萄環紋線蟲(Criconemella xenoplax)(=環腐線蟲(Mesocriconema xenoplax))及環紋線蟲屬(Criconemella spp.);弗尼亞小環線蟲(Criconemoides ferniae)、小環線蟲(Criconemoides onoense)、杯口小環線蟲(Criconemoides ornatum)及小環線蟲屬(Criconemoides spp.);馬鈴薯腐敗線蟲(Ditylenchus destructor)、莖線蟲(Ditylenchus dipsaci)、蘑菇莖線蟲(Ditylenchus myceliophagus)及莖線蟲屬(Ditylenchus spp.)之莖與葉部體內寄生蟲;異頭錐線蟲(Dolichodorus heterocephalus)、馬鈴薯白線蟲(Globodera pallida)(=馬鈴薯異皮線蟲(Heterodera pallida))、馬鈴薯黃金線蟲(Globodera rostochiensis)(黃色馬鈴薯包囊線蟲)、枯萎黃金線蟲(Globodera solanacearum)、菸草黃金線蟲(Globodera tabacum)、維吉尼亞黃金線蟲(Globodera virginia)及黃金線蟲屬(Globodera spp.)之非遊走性包囊形成性寄生蟲;雙角螺旋線蟲(Helicotylenchus digonicus)、雙宮螺旋線蟲(Helicotylenchus dihystera)、赤色螺旋線蟲(Helicotylenchus erythrine)、多帶螺旋線蟲(Helicotylenchus multicinctus)、短小螺旋線蟲(Helicotylenchus nannus)、假強壯螺旋線蟲(Helicotylenchus pseudorobustus)及螺旋線蟲屬(Helicotylenchus spp.);半鞘線
蟲(Hemicriconemoides)、花生鞘線蟲(Hemicycliophora arenaria)、裸出鞘線蟲(Hemicycliophora nudata)、塔堅鞘線蟲(Hemicycliophora parvana)、禾穀異皮線蟲(Heterodera avenae)、十字花科異皮線蟲(Heterodera cruciferae)、大豆包囊線蟲(大豆異皮線蟲(Heterodera glycines))、稻異皮線蟲(Heterodera oryzae)、甜菜異皮線蟲(Heterodera schachtii)、玉米異皮線蟲(Heterodera zeae)及異皮線蟲屬(Heterodera spp.)之非遊走性包囊形成性寄生蟲;細小潛根線蟲(Hirschmaniella gracilis)、稻潛根線蟲(Hirschmaniella oryzae)、刺尾潛根線蟲(Hirschmaniella spinicaudata)及潛根線蟲屬(Hirschmaniella spp.)之莖與葉部體內寄生蟲;埃及紐帶線蟲(Hoplolaimus aegyptii)、加州紐帶線蟲(Hoplolaimus californicus)、哥倫布紐帶線蟲(Hoplolaimus columbus)、帽狀紐帶線蟲(Hoplolaimus galeatus)、珍珠紐帶線蟲(Hoplolaimus indicus)、大針紐帶線蟲(Hoplolaimus magnistylus)、擬強壯紐帶線蟲(Hoplolaimus pararobustus)、非洲長刺線蟲(Longidorus africanus)、短環長刺線蟲(Longidorus breviannulatus)、橫帶長刺線蟲(Longidorus elongatus)、長刺線蟲(Longidorus laevicapitatus)、長刺線蟲(Longidorus vineacola)及長刺線蟲屬(Longidorus spp.)之體外寄生蟲;短尾根瘤線蟲(Meloidogyne acronea)、非洲根瘤線蟲(Meloidogyne africana)、花生根瘤線蟲(Meloidogyne arenaria)、花生根瘤線蟲湯氏亞種(Meloidogyne arenaria thamesi)、亞特力根瘤線蟲(Meloidogyne artiella)、奇特伍德根瘤線蟲(Meloidogyne chitwoodi)、咖啡根結線蟲(Meloidogyne coffeicola)、埃塞俄比亞根瘤線蟲(Meloidogyne ethiopica)、短小根瘤線蟲(Meloidogyne exigua)、法克斯根瘤線蟲(Meloidogyne fallax)、擬禾本科根瘤線蟲(Meloidogyne graminicola)、禾本科根瘤線蟲(Meloidogyne graminis)、北方根瘤線蟲(Meloidogyne hapla)、南方根瘤線蟲(Meloidogyne incognita)、南方根瘤線蟲亞力塔亞種(Meloidogyne
incognita acrita)、爪哇根瘤線蟲(Meloidogyne javanica)、吉庫尤根瘤線蟲(Meloidogyne kikuyensis)、小根瘤線蟲(Meloidogyne minor)、小麥根瘤線蟲(Meloidogyne naasi)、咖啡根瘤線蟲(Meloidogyne paranaensis)、泰晤士根瘤線蟲(Meloidogyne thamesi)及根瘤線蟲屬(Meloidogyne spp.)之非遊走性寄生蟲;根瘤線蟲屬(Meloinema spp.)、假根瘤線蟲(Nacobbus aberrans)、擬莖線蟲(Neotylenchus vigissi)、食菌性線蟲(Paraphelenchus pseudoparietinus)、蔥擬毛刺線蟲(Paratrichodorus allius)、擬毛刺線蟲(Paratrichodorus lobatus)、小擬毛刺線蟲(Paratrichodorus minor)、小擬毛刺線蟲(Paratrichodorus nanus)、有孔擬毛刺線蟲(Paratrichodorus porosus)、大麥光滑擬毛刺線蟲(Paratrichodorus teres)及擬毛刺線蟲屬(Paratrichodorus spp.);芹菜釘線蟲(Paratylenchus hamatus)、微小釘線蟲(Paratylenchus minutus)、突出釘線蟲(Paratylenchus projectus)及釘線蟲屬(Paratylenchus spp.);短體短體線蟲(Pratylenchus agilis)、亞倫氏短體線蟲(Pratylenchus alleni)、安第斯短體線蟲(Pratylenchus andinus)、短尾短體線蟲(Pratylenchus brachyurus)、小麥短體線蟲(Pratylenchus cerealis)、咖啡短體線蟲(Pratylenchus coffeae)、刻痕短體線蟲(Pratylenchus crenatus)、棉花短體線蟲(Pratylenchus delattrei)、吉伯氏短體線蟲(Pratylenchus giibbicaudatus)、古迪氏短體線蟲(Pratylenchus goodeyi)、漢氏短體線蟲(Pratylenchus hamatus)、六裂短體線蟲(Pratylenchus hexincisus)、盧斯短體線蟲(Pratylenchus loosi)、落選短體線蟲(Pratylenchus neglectus)、穿刺短體線蟲(Pratylenchus penetrans)、草地短體線蟲(Pratylenchus pratensis)、斯克裏布納短體線蟲(Pratylenchus scribneri)、大麥短體線蟲(Pratylenchus teres)、索氏短體線蟲(Pratylenchus thornei)、傷殘短體線蟲(Pratylenchus vulnus)、玉米短體線蟲(Pratylenchus zeae)及短體線蟲屬(Pratylenchus spp.)之遊走性體內寄生蟲;微小假海矛線蟲(Pseudohalenchus minutus)、平滑墊
刃線蟲(Psilenchus magnidens)、膨大平滑墊刃線蟲(Psilenchus tumidus)、墨西哥玉米胞囊線蟲(Punctodera chalcoensis)、五溝線蟲(Quinisulcius acutus)、柑橘穿孔線蟲(Radopholus citrophilus)、香蕉穿孔線蟲(Radopholus similis)、穿孔線蟲屬(Radopholus spp.)之遊走性體內寄生蟲;北方貝腎狀線蟲(Rotylenchulus borealis)、微小腎狀線蟲(Rotylenchulus parvus)、腎形腎狀線蟲(Rotylenchulus reniformis)及腎狀線蟲屬(Rotylenchulus spp.);直溝盤旋線蟲(Rotylenchus laurentinus)、大囊盤旋線蟲(Rotylenchus macrodoratus)、強壯盤旋線蟲(Rotylenchus robustus)、均勻盤旋線蟲(Rotylenchus uniformis)及盤旋線蟲屬(Rotylenchus spp.);小尾螺旋線蟲(Scutellonema brachyurum)、山藥螺旋線蟲(Scutellonema bradys)、卡維內斯螺旋線蟲(Scutellonema clathricaudatum)及螺旋線蟲屬(Scutellonema spp.)之遊走性體內寄生蟲;亞粒線蟲(Subanguina radiciola)、頭線蟲(Tetylenchus nicotianae)、圓桶毛刺線蟲(Trichodorus cylindricus)、微小毛刺線蟲(Trichodorus minor)、原始毛刺線蟲(Trichodorus primitivus)、普希毛刺線蟲(Trichodorus proximus)、相似毛刺線蟲(Trichodorus similis)、大蒜毛刺線蟲(Trichodorus sparsus)及毛刺線蟲屬(Trichodorus spp.)之體外寄生蟲;農田矮化線蟲(Tylenchorhynchus agri)、甘藍矮化線蟲(Tylenchorhynchus brassicae)、清亮矮化線蟲(Tylenchorhynchus clarus)、克萊頓矮化線蟲(Tylenchorhynchus claytoni)、指形矮化線蟲(Tylenchorhynchus digitatus)、伊布裏矮化線蟲(Tylenchorhynchus ebriensis)、最大矮化線蟲(Tylenchorhynchus maximus)、裸矮化線蟲(Tylenchorhynchus nudus)、普通矮化線蟲(Tylenchorhynchus vulgaris)及矮化線蟲屬(Tylenchorhynchus spp.);柑橘半穿刺線蟲(Tylenchulus semipenetrans)及半穿刺線蟲屬(Tylenchulus spp.)之半寄生蟲;美洲劍線蟲(Xiphinema americanum)、短頸劍線蟲劍線蟲(Xiphinema brevicolle)、雙型性劍線蟲(Xiphinema
dimorphicaudatum)、標準劍線蟲(Xiphinema index)及劍線蟲屬(Xiphinema spp.)之體外寄生蟲。
可使用式(I)、(Ia)、(Ib)或(Ic)化合物控制之線蟲包括:根瘤
線蟲屬(Meloidogyne)線蟲,如:南方根瘤線蟲(Meloidogyne incognita)、爪哇根瘤線蟲(Meloidogyne javanica)、北方根瘤線蟲(Meloidogyne hapla)及花生根瘤線蟲(Meloidogyne arenaria);腐敗線蟲屬(Ditylenchus)線蟲,如:馬鈴薯腐敗線蟲(Ditylenchus destructor)及莖與球莖線蟲(莖線蟲(Ditylenchus dipsaci));短體線蟲屬(Pratylenchus)線蟲,如:穗軸根腐線蟲(穿刺短體線蟲(Pratylenchus penetrans))、菊花根腐線蟲(菊花短體線蟲(Pratylenchus fallax))、咖啡根線蟲(咖啡短體線蟲(Pratylenchus coffeae))、茶樹根線蟲(盧斯短體線蟲(Pratylenchus loosi))及胡桃根腐線蟲(傷殘短體線蟲(Pratylenchus vulnus));黃金包囊線蟲屬(Globodera)線蟲,如:黃色馬鈴薯包囊線蟲(馬鈴薯黃金線蟲(Globodera rostochiensis))及白色馬鈴薯包囊線蟲(馬鈴薯白線蟲(Globodera pallida));異皮線蟲屬(Heterodera)之線蟲,如:大豆異皮線蟲(Heterodera glycines)及甜菜異皮線蟲(Heterodera schachtii));滑刃線蟲屬(Aphelenchoides)線蟲,如:稻白尖病線蟲(葉芽滑刃線蟲(Aphelenchoides besseyi))、菊花線蟲(菊花滑刃線蟲(Aphelenchoides ritzemabosi))及草莓線蟲(草莓滑刃線蟲(Aphelenchoides fragariae);真滑刃線蟲屬(Aphelenchus)線蟲,如:食真菌性線蟲(燕麥真滑刃線蟲(Aphelenchus avenae));穿孔線蟲屬(Radopholus)線蟲,如:穿孔線蟲(香蕉穿孔線蟲(Radopholus similis));半穿刺線蟲屬(Tylenchulus)線蟲,如:柑橘根線蟲(柑橘半穿刺線蟲(Tylenchulus semipenetrans));腎狀線蟲屬(Rotylenchulus)線蟲,如:腎形線蟲(腎形腎狀線蟲(Rotylenchulus reniformis));鑽木線蟲,如:松材線蟲(Bursaphelenchus xylophilus)及椰子紅環腐線蟲(Bursaphelenchus cocophilus),等等線蟲。
可使用式(I)、(Ia)、(Ib)或(Ic)化合物保護之植物包括下列植
物,如:穀類(例如:稻、大麥、小麥、裸麥、燕麥、玉米、高梁,等等)、豆類(大豆、紅豆、豆類、蠶豆、豌豆、花生,等等)、果樹/果實(蘋果、柑橘品種、梨、葡萄、桃、日本杏、櫻桃、胡桃、杏仁、香蕉、草莓,等等)、蔬菜品種(大白菜、番茄、菠菜、青花菜、萵苣、洋蔥、青蔥、青椒,等等)、根部作物(胡蘿蔔、馬鈴薯、地瓜、蘿蔔、蓮藕、大頭菜,等等)、工業原料用植物(棉花、麻、構樹、三椏樹、油菜、甜菜、啤酒花、甘蔗、甜菜、橄欖、橡膠、棕櫚樹、咖啡、菸草、茶葉,等等)、瓜類(南瓜、小黃瓜、西瓜、香瓜,等等)、草原植物(鴨茅、高粱、貓尾草、三葉草、苜蓿草,等等)、草皮(臺北草、康穗草,等等)、香料植物,等等(薰衣草、迷迭香、百里香、巴西利、胡椒、薑,等等)及花卉(菊花、玫瑰、蘭花,等等)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制咖啡線蟲,特定
言之:短尾短體線蟲(Pratylenchus brachyurus)、咖啡短體線蟲(Pratylenchus coffeae)、短小根瘤線蟲(Meloidogyne exigua)、南方根瘤線蟲(Meloidogyne incognita)、咖啡根結線蟲(Meloidogyne coffeicola)、螺旋線蟲屬(Helicotylenchus spp.)及咖啡根瘤線蟲(Meloidogyne paranaensis)、盤旋線蟲屬(Rotylenchus spp.)、劍線蟲屬(Xiphinema spp.)、矮化線蟲屬(Tylenchorhynchus spp.)與螺旋線蟲屬(Scutellonema spp.)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制馬鈴薯線蟲,特
定言之:短尾短體線蟲(Pratylenchus brachyurus)、草地短體線蟲(Pratylenchus pratensis)、斯克裏布納短體線蟲(Pratylenchus scribneri)、穿刺短體線蟲(Pratylenchus penetrans)、咖啡短體線蟲(Pratylenchus coffeae)、莖線蟲(Ditylenchus dipsaci)及亞倫氏短體線蟲(Pratylenchus alleni)、安第斯短體線蟲(Pratylenchus andinus)、小麥短體線蟲(Pratylenchus cerealis)、刻痕短體線蟲
(Pratylenchus crenatus)、六裂短體線蟲(Pratylenchus hexincisus)、盧斯短體線蟲(Pratylenchus loosi)、落選短體線蟲(Pratylenchus neglectus)、大麥短體線蟲(Pratylenchus teres)、索氏短體線蟲(Pratylenchus thornei)、傷殘短體線蟲(Pratylenchus vulnus)、長尾刺線蟲(Belonolaimus longicaudatus)、圓桶毛刺線蟲(Trichodorus cylindricus)、原始毛刺線蟲(Trichodorus primitivus)、普希毛刺線蟲(Trichodorus proximus)、相似毛刺線蟲(Trichodorus similis)、大蒜毛刺線蟲(Trichodorus sparsus)、小擬毛刺線蟲(Paratrichodorus minor)、蔥擬毛刺線蟲(Paratrichodorus allius)、小擬毛刺線蟲(Paratrichodorus nanus)、大麥光滑擬毛刺線蟲(Paratrichodorus teres)、花生根瘤線蟲(Meloidogyne arenaria)、法克斯根瘤線蟲(Meloidogyne fallax)、北方根瘤線蟲(Meloidogyne hapla)、泰晤士根瘤線蟲(Meloidogyne thamesi)、南方根瘤線蟲(Meloidogyne incognita)、奇特伍德根瘤線蟲(Meloidogyne chitwoodi)、爪哇根瘤線蟲(Meloidogyne javanica)、假根瘤線蟲(Nacobbus aberrans)、馬鈴薯黃金線蟲(Globodera rostochiensis)、馬鈴薯白線蟲(Globodera pallida)、馬鈴薯腐敗線蟲(Ditylenchus destructor)、香蕉穿孔線蟲(Radopholus similis)、腎形腎狀線蟲(Rotylenchulus reniformis)、擬莖線蟲(Neotylenchus vigissi)、食菌性線蟲(Paraphelenchus pseudoparietinus)、草莓滑刃線蟲(Aphelenchoides fragariae)與根瘤線蟲屬(Meloinema spp.)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制番茄線蟲,特定
言之:花生根瘤線蟲(Meloidogyne arenaria)、北方根瘤線蟲(Meloidogyne hapla)、爪哇根瘤線蟲(Meloidogyne javanica)、南方根瘤線蟲(Meloidogyne incognita)、穿刺短體線蟲(Pratylenchus penetrans)及短尾短體線蟲(Pratylenchus brachyurus)、咖啡短體線蟲(Pratylenchus coffeae)、斯克裏布納短體線蟲(Pratylenchus scribneri)、傷殘短體線蟲(Pratylenchus vulnus)、微小
短體線蟲(Paratrichodorus minor)、短小根瘤線蟲(Meloidogyne exigua)、假根瘤線蟲(Nacobbus aberrans)、枯萎黃金線蟲(Globodera solanacearum)、異頭錐線蟲(Dolichodorus heterocephalus)與腎形腎狀線蟲(Rotylenchulus reniformis)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制胡瓜植物線蟲,
特定言之:花生根瘤線蟲(Meloidogyne arenaria)、北方根瘤線蟲(Meloidogyne hapla)、爪哇根瘤線蟲(Meloidogyne javanica)、南方根瘤線蟲(Meloidogyne incognita)、腎形腎狀線蟲(Rotylenchulus reniformis)與索氏短體線蟲(Pratylenchus thornei)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制棉花線蟲,特定
言之:長尾刺線蟲(Belonolaimus longicaudatus)、南方根瘤線蟲(Meloidogyne incognita)、哥倫布紐帶線蟲(Hoplolaimus columbus)、帽狀紐帶線蟲(Hoplolaimus galeatus)與腎形腎狀線蟲(Rotylenchulus reniformis)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制玉米線蟲,特定
言之:長尾刺線蟲(Belonolaimus longicaudatus)、小短體線蟲(Paratrichodorus minor)及短尾短體線蟲(Pratylenchus brachyurus)、棉花短體線蟲(Pratylenchus delattrei)、六裂短體線蟲(Pratylenchus hexincisus)、穿刺短體線蟲(Pratylenchus penetrans)、玉米短體線蟲(Pratylenchus zeae)、豌豆刺線蟲(Belonolaimus gracilis)、諾頓刺線蟲(Belonolaimus nortoni)、短環長刺線蟲(Longidorus breviannulatus)、花生根瘤線蟲(Meloidogyne arenaria)、花生根瘤線蟲湯氏亞種(Meloidogyne arenaria thamesi)、禾本科根瘤線蟲(Meloidogyne graminis)、南方根瘤線蟲(Meloidogyne incognita)、南方根瘤線蟲亞力塔亞種(Meloidogyne incognita acrita)、爪哇根瘤線蟲(Meloidogyne javanica)、小麥根瘤線蟲(Meloidogyne naasi)、禾穀異皮線蟲(Heterodera avenae)、稻異皮
線蟲(Heterodera oryzae)、玉米異皮線蟲(Heterodera zeae)、墨西哥玉米胞囊線蟲(Punctodera chalcoensis)、莖線蟲(Ditylenchus dipsaci)、埃及紐帶線蟲(Hoplolaimus aegyptii)、大針紐帶線蟲(Hoplolaimus magnistylus)、帽狀紐帶線蟲(Hoplolaimus galeatus)、珍珠粟槍線蟲(Hoplolaimus indicus)、雙角螺旋線蟲(Helicotylenchus digonicus)、雙宮螺旋線蟲(Helicotylenchus dihystera)、假強壯螺旋線蟲(Helicotylenchus pseudorobustus)、美洲劍線蟲(Xiphinema americanum)、異頭錐線蟲(Dolichodorus heterocephalus)、裝飾環紋線蟲(Criconemella ornata)、環紋線蟲(Criconemella onoensis)、香蕉穿孔線蟲(Radopholus similis)、北方貝腎狀線蟲(Rotylenchulus borealis)、微小腎狀線蟲(Rotylenchulus parvus)、農田矮化線蟲(Tylenchorhynchus agri)、清亮矮化線蟲(Tylenchorhynchus clarus)、克萊頓矮化線蟲(Tylenchorhynchus claytoni)、最大矮化線蟲(Tylenchorhynchus maximus)、裸矮化線蟲(Tylenchorhynchus nudus)、普通矮化線蟲(Tylenchorhynchus vulgaris)、五溝線蟲(Quinisulcius acutus)、微小釘線蟲(Paratylenchus minutus)、塔堅鞘線蟲(Hemicycliophora parvana)、居農野外墊刃線蟲(Aglenchus agricola)、小麥粒癭線蟲(Anguina tritici)、花生滑刃線蟲(Aphelenchoides arachidis)、小尾盾線蟲(Scutellonema brachyurum)與亞粒線蟲(Subanguina radiciola)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制大豆線蟲,特定
言之:短尾短體線蟲(Pratylenchus brachyurus)、草地短體線蟲(Pratylenchus pratensis)、穿刺短體線蟲(Pratylenchus penetrans)、斯克裏布納短體線蟲(Pratylenchus scribneri)、長尾刺線蟲(Belonolaimus longicaudatus)、大豆異皮線蟲(Heterodera glycines)、哥倫布紐帶線蟲(Hoplolaimus columbus)及咖啡短體線蟲(Pratylenchus coffeae)、六裂短體線蟲(Pratylenchus hexincisus)、落選短體線蟲(Pratylenchus neglectus)、刻痕短體線蟲(Pratylenchus crenatus)、亞
倫氏短體線蟲(Pratylenchus alleni)、短體短體線蟲(Pratylenchus agilis)、玉米短體線蟲(Pratylenchus zeae)、傷殘短體線蟲(Pratylenchus vulnus)、豌豆刺線蟲(Belonolaimus gracilis)、花生根瘤線蟲(Meloidogyne arenaria)、南方根瘤線蟲(Meloidogyne incognita)、爪哇根瘤線蟲(Meloidogyne javanica)、北方根瘤線蟲(Meloidogyne hapla)、哥倫布紐帶線蟲(Hoplolaimus columbus)、帽狀紐帶線蟲(Hoplolaimus galeatus)與腎形腎狀線蟲(Rotylenchulus reniformis)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制菸草線蟲,特定
言之:南方根瘤線蟲(Meloidogyne incognita)、爪哇根瘤線蟲(Meloidogyne javanica)及短尾短體線蟲(Pratylenchus brachyurus)、草地短體線蟲(Pratylenchus pratensis)、六裂短體線蟲(Pratylenchus hexincisus)、穿刺短體線蟲(Pratylenchus penetrans)、落選短體線蟲(Pratylenchus neglectus)、刻痕短體線蟲(Pratylenchus crenatus)、索氏短體線蟲(Pratylenchus thornei)、傷殘短體線蟲(Pratylenchus vulnus)、玉米短體線蟲(Pratylenchus zeae)、橫帶長刺線蟲(Longidorus elongatu)、擬毛刺線蟲(Paratrichodorus lobatus)、毛刺線蟲屬(Trichodorus spp.)、花生根瘤線蟲(Meloidogyne arenaria)、北方根瘤線蟲(Meloidogyne hapla)、菸草黃金線蟲(Globodera tabacum)、枯萎黃金線蟲(Globodera solanacearum)、維吉尼亞黃金線蟲(Globodera virginiae)、莖線蟲(Ditylenchus dipsaci)、盤旋線蟲屬(Rotylenchus spp.)、螺旋線蟲屬(Helicotylenchus spp.)、美洲劍線蟲(Xiphinema americanum)、環紋線蟲屬(Criconcmella spp.)、腎形腎狀線蟲(Rotylenchulus reniformis)、克萊頓矮化線蟲(Tylenchorhynchus claytoni)、釘線蟲屬(Paratylenchus spp.)與頭線蟲(Tetylenchus nicotianae)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制柑橘線蟲,特定
言之:咖啡短體線蟲(Pratylenchus coffeae)及短尾短體線蟲(Pratylenchus
brachyurus)、傷殘短體線蟲(Pratylenchus vulnus)、長尾刺線蟲(Belonolaimus longicaudatus)、微小短體線蟲(Paratrichodorus minor)、有孔擬毛刺線蟲(Paratrichodorus porosus)、毛刺線蟲(Trichodorus)、南方根瘤線蟲(Meloidogyne incognita)、南方根瘤線蟲亞力塔亞種(Meloidogyne incognita acrita)、爪哇根瘤線蟲(Meloidogyne javanica)、大囊盤旋線蟲(Rotylenchus macrodoratus)、美洲劍線蟲(Xiphinema americanum)、短頸劍線蟲劍線蟲(Xiphinema brevicolle)、標準劍線蟲(Xiphinema index)、環紋線蟲屬(Criconemella spp.)、半鞘線蟲(Hemicriconemoides)、香蕉穿孔線蟲(Radopholus similis)、柑橘穿孔線蟲(Radopholus citrophilus)、花生鞘線蟲(Hemicycliophora arenaria)、裸出鞘線蟲(Hemicycliophora nudata)與柑橘半穿刺線蟲(Tylenchulus semipenetrans)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制香蕉線蟲,特定
言之:咖啡短體線蟲(Pratylenchus coffeae)、香蕉穿孔線蟲(Radopholus similis)及吉伯氏短體線蟲(Pratylenchus giibbicaudatus)、盧斯短體線蟲(Pratylenchus loosi)、根瘤線蟲屬(Meloidogyne spp.)、多帶螺旋線蟲(Helicotylenchus multicinctus)、雙宮螺旋線蟲(Helicotylenchus dihystera)與腎狀線蟲屬(Rotylenchulus spp.)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制鳳梨線蟲,特定
言之:玉米短體線蟲(Pratylenchus zeae)、草地短體線蟲(Pratylenchus pratensis)、短尾短體線蟲(Pratylenchus brachyurus)、古迪氏短體線蟲(Pratylenchus goodeyi)、根瘤線蟲屬(Meloidogyne spp.)、腎形腎狀線蟲(Rotylenchulus reniformis)及橫帶長刺線蟲(Longidorus elongatus)、長刺線蟲(Longidorus laevicapitatus)、原始毛刺線蟲(Trichodorus primitivus)、微小毛刺線蟲(Trichodorus minor)、異皮線蟲屬(Heterodera spp.)、蘑菇莖線蟲
(Ditylenchus myceliophagus)、加州紐帶線蟲(Hoplolaimus californicus)、擬強壯紐帶線蟲(Hoplolaimus pararobustus)、珍珠粟槍線蟲(Hoplolaimus indicus)、雙宮螺旋線蟲(Helicotylenchus dihystera)、短小螺旋線蟲(Helicotylenchus nannus)、多帶螺旋線蟲(Helicotylenchus multicinctus)、赤色螺旋線蟲(Helicotylenchus erythrine)、雙型性劍線蟲(Xiphinema dimorphicaudatum)、香蕉穿孔線蟲((Radopholus similis)、指形矮化線蟲(Tylenchorhynchus digitatus)、伊布裏矮化線蟲(Tylenchorhynchus ebriensis)、微小釘線蟲(Paratylenchus minutus)、卡維內斯螺旋線蟲(Scutellonema clathricaudatum)、山藥螺旋線蟲(Scutellonema bradys)、膨大平滑墊刃線蟲(Psilenchus tumidus)、平滑墊刃線蟲(Psilenchus magnidens)、微小假海矛線蟲(Pseudohalenchus minutus)、弗尼亞小環線蟲(Criconemoides ferniae)、小環線蟲(Criconemoides onoense)與杯口小環線蟲(Criconemoides ornatum)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制葡萄藤線蟲,特
定言之:傷殘短體線蟲(Pratylenchus vulnus)、花生根瘤線蟲(Meloidogyne arenaria)、南方根瘤線蟲(Meloidogyne incognita)、爪哇根瘤線蟲(Meloidogyne javanica)、美洲劍線蟲(Xiphinema americanum)、標準劍線蟲(Xiphinema index)及草地短體線蟲(Pratylenchus pratensis)、斯克裏布納短體線蟲(Pratylenchus scribneri)、落選短體線蟲(Pratylenchus neglectus)、短尾短體線蟲(Pratylenchus brachyurus)、索氏短體線蟲(Pratylenchus thornei)與柑橘半穿刺線蟲(Tylenchulus semipenetrans)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制樹類作物-仁果
之線蟲,特定言之穿刺短體線蟲(Pratylenchus penetrans)及傷殘短體線蟲(Pratylenchus vulnus)、橫帶長刺線蟲(Longidorus elongatus)、南方根瘤線蟲(Meloidogyne incognita)與北方根瘤線蟲(Meloidogyne hapla)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制線蟲樹類作物-
核果之線蟲,特定言之:穿刺短體線蟲(Pratylenchus penetrans)、傷殘短體線蟲(Pratylenchus vulnus)、花生根瘤線蟲(Meloidogyne arenaria)、北方根瘤線蟲(Meloidogyne hapla)、爪哇根瘤線蟲(Meloidogyne javanica)、南方根瘤線蟲(Meloidogyne incognita)、葡萄環紋線蟲(Criconemella xenoplax)及短尾短體線蟲(Pratylenchus brachyurus)、咖啡短體線蟲(Pratylenchus coffeae)、斯克裏布納短體線蟲(Pratylenchus scribneri)、玉米短體線蟲(Pratylenchus zeae)、長尾刺線蟲(Belonolaimus longicaudatus)、雙宮螺旋線蟲(Helicotylenchus dihystera)、美洲劍線蟲(Xiphinema americanum)、彎曲環紋線蟲(Criconemella curvata)、克萊頓矮化線蟲(Tylenchorhynchus claytoni)、芹菜釘線蟲(Paratylenchus hamatus)、突出釘線蟲(Paratylenchus projectus)、小尾盾線蟲(Scutellonema brachyurum)與帽狀紐帶線蟲(Hoplolaimus galeatus)。
式(I)、(Ia)、(Ib)或(Ic)化合物特別適合控制樹類作物、甘蔗
與稻之線蟲,特定言之:毛刺線蟲屬(Trichodorus spp.)、環紋線蟲屬(Criconemella spp.)及短體線蟲屬(Pratylenchus spp.)、擬毛刺線蟲屬(Paratrichodorus spp.)、根瘤線蟲屬(Meloidogyne spp.)、螺旋線蟲屬(Helicotylenchus spp.)、矮化線蟲屬(Tylenchorhynchus spp.)、滑刃線蟲屬(Aphelenchoides spp.)、異皮線蟲屬(Heterodera spp.)、劍線蟲屬(Xiphinema spp.)與波斯固著線蟲(Cacopaurus pestis)。
本文中,術語"線蟲"係指會傷害人類或動物之線蟲。
會傷害人類或動物之明確線蟲物種為:毛形亞目(Trichinellida),例如:毛首線蟲屬(Trichuris spp.)、毛細線蟲屬(Capillaria spp.)、毛細線蟲屬(Paracapillaria spp.),優鞘線蟲屬(Eucoleus spp.)、線蟲屬(Trichomosoides spp.)、旋毛蟲屬(Trichinella spp.)
墊刃目(Tylenchida),例如:細頸線蟲屬(Micronema spp.)、糞桿線蟲屬(Strongyloides spp.)
小桿亞目(Rhabditina),例如:圓線蟲屬(Strongylus spp.)、三齒線蟲屬(Triodontophorus spp.)、食道齒線蟲屬(Oesophagodontus spp.)、毛線線蟲屬(Trichonema spp.)、輻首線蟲屬(Gyalocephalus spp.)、柱咽線蟲屬(Cylindropharynx spp.)、盆口線蟲屬(Poteriostomum spp.)、線蟲屬(Cyclococercus spp.)、杯冠線蟲屬(Cylicostephanus spp.)、食道口線蟲屬(Oesophagostomum spp.)、夏桕線蟲屬(Chabertia spp.)、冠尾線蟲屬(Stephanurus spp.)、鉤蟲屬(Ancylostoma spp.)、彎口線蟲屬(Uncinaria spp.)、鉤蟲屬(Necator spp.)、仰口線蟲屬(Bunostomum spp.)、球首線蟲屬(Globocephalus spp.)、比翼線蟲屬(Syngamus spp.)、節蟲屬(Cyathostoma spp.)、後圓線蟲屬(Metastrongylus spp.)、網尾線蟲屬(Dictyocaulus spp.)、繆勒線蟲屬(Muellerius spp.)、原圓線蟲屬(Protostrongylus spp.)、新圓線蟲屬(Neostrongylus spp.)、囊尾線蟲屬(Cystocaulus spp.)、肺圓線蟲屬(Pneumostrongylus spp.)、指尾線蟲屬(Spicocaulus spp.)、鹿圓線蟲屬(Elaphostrongylus spp.)、副麂圓線蟲屬(Parelaphostrongylus spp.)、環體線蟲屬(Crenosoma spp.)、副環體線蟲屬(Paracrenosoma spp.)、奧斯勒絲蟲屬(Oslerus spp.)、住血線蟲屬(Angiostrongylus spp.)、肺線蟲屬(Aelurostrongylus spp.)、類絲線蟲屬(Filaroides spp.)、副類絲線蟲屬(Parafilaroides spp.)、毛圓線蟲屬(Trichostrongylus spp.)、血線蟲屬(Haemonchus spp.)、奧斯特線蟲屬(Ostertagia spp.)、牛胃絲蟲屬(Teladorsagia spp.)、馬歇爾線蟲屬(Marshallagia spp.)、古柏線蟲屬(Cooperia spp.)、日圓線蟲屬(Nippostrongylus spp.)、螺旋線蟲屬(Heligmosomoides spp.)、細頸線蟲(Nematodirus spp.)、胃圓線蟲屬(Hyostrongylus spp.)、尖頭胃線蟲屬(Obeliscoides spp.)、裂口線蟲屬
(Amidostomum spp.)、壺肛線蟲屬(Ollulanus spp.)
旋尾目(Spirurida),例如:尖尾線蟲屬(Oxyuris spp.)、蟯蟲屬(Enterobius spp.)、栓尾線蟲屬(Passalurus spp.)、管狀線蟲屬(Syphacia spp.)、無刺蟯蟲屬(Aspiculuris spp.)、異刺線蟲屬(Heterakis spp.);蛔蟲屬(Ascaris spp.)、弓蛔屬(Toxascaris spp.)、弓首線蟲屬(Toxocara spp.)、貝利蛔蟲屬(Baylisascaris spp.)、副蛔屬(Parascaris spp.)、海獸胃線蟲屬(Anisakis spp.)、禽蛔屬(Ascaridia spp.);棘口線蟲屬(Gnathostoma spp.)、泡翼線蟲屬(Physaloptera spp.)、吸吮線蟲屬(Thelazia spp.)、筒線蟲屬(Gongylonema spp.)、馬胃線蟲屬(Habronema spp.)、副柔絲線蟲屬(Parabronema spp.);德拉西線蟲屬(Draschia spp.)、龍線蟲屬(Dracunculus spp.);冠絲蟲屬(Stephanofilaria spp.)、類絲蟲屬(Parafilaria spp.)、絲狀線蟲屬(Setaria spp.)、羅阿絲蟲屬(Loa spp.)、血直絲蟲屬(Dirofilaria spp.)、光絲蟲屬(Litomosoides spp.)、血絲蟲屬(Brugia spp.)、吳策絲蟲屬(Wuchereria spp.)、蟠尾絲蟲屬(Onchocerca spp.)、旋尾線蟲屬(Spirocerca spp.)。
許多種已知殺線蟲劑同樣對其他寄生性蠕蟲具有活性,因此可用於控制不一定屬於線蟲類之人類與動物之寄生蟲。本發明亦有關以式(I)、(Ia)、(Ib)或(Ic)化合物作為殺蠕蟲藥之用途。病原性體內寄生性蠕蟲包括扁形動物門(Platyhelmintha)(例如:單殖吸蟲、絛蟲及吸蟲)、棘頭動物及舌形動物。較佳可述及下列蠕蟲:單殖吸蟲亞綱(Monogenea):例如:三代蟲屬(Gyrodactylus spp.)、指標蟲屬(Dactylogyrus spp.)、多盤吸蟲屬(Polystoma spp.);絛蟲:擬葉目(Pseudophyllidea),例如:廣節裂頭絛蟲屬(Diphyllobothrium spp.)、螺旋體蟲屬(Spirometra spp.)、裂頭絛蟲屬(Schistocephalus spp.)、舌狀絛蟲屬(Ligula spp.)、吸葉絛蟲屬(Bothridium spp.)、大複殖門絛蟲屬
(Diphlogonoporus spp.);圓葉目(Cyclophyllidea),例如:中殖孔屬絛蟲屬(Mesocestoides spp.)、裸頭絛蟲屬(Anoplocephala spp.)、副裸頭絛蟲屬(Paranoplocephala spp.)、莫尼茨絛蟲屬(Moniezia spp.)、隧體絛蟲屬(Thysanosoma spp.)、曲子官絛蟲屬(Thysaniezia spp.)、無卵黃腺絛蟲(Avitellina spp.)、史提拉絛蟲屬(Stilesia spp.)、錫帶絛蟲屬(Cittotaenia spp.)、安迪亞絛蟲屬(Andyra spp.)、伯特絛蟲屬(Bertiella spp.)、帶絛蟲屬(Taenia spp.)、棘球絛蟲屬(Echinococcus spp.)、泡尾絛蟲屬(Hydatigera spp.)、戴文絛蟲屬(Davainea spp.)、雷氏絛蟲屬(Raillietina spp.)、包膜絛蟲屬(Hymenolepis spp.)、瘍棘殼絛蟲屬(Echinolepis spp.)、棘葉絛蟲屬(Echinocotyle spp.)、迪克氏絛蟲屬(Diochis spp.)、瓜實絛蟲屬(Dipylidium spp.)、約優克斯絛蟲屬(Joyeuxiella spp.)、雙孔絛蟲屬(Diplopylidium spp.);吸蟲:複殖目(Digenea),例如:複口吸蟲屬(Diplostomum spp.)、莖雙穴吸蟲屬(Posthodiplostomum spp.)、血吸蟲屬(Schistosoma spp.)、毛畢屬(Trichobilharzia spp.)、毛樣線蟲屬(Ornithobilharzia spp.)、澳畢吸蟲屬(Austrobilharzia spp.)、巨畢吸蟲屬(Gigantobilharzia spp.)、彩蚴吸蟲屬(Leucochloridium spp.)、短咽吸蟲屬(Brachylaima spp.)、棘口吸蟲屬(Echinostoma spp.)、棘緣吸蟲屬(Echinoparyphium spp.)、棘隙吸蟲屬(Echinochasmus spp.)、低頸吸蟲屬(Hypoderaeum spp.)、肝吸蟲屬(Fasciola spp.)、擬片形吸蟲屬(Fasciolides spp.)、薑片蟲屬(Fasciolopsis spp.)、環腸吸蟲屬(Cyclocoelum spp.)、盲腔屬(Typhlocoelum spp.)、雙口吸蟲屬(Paramphistomum spp.)、杯殖吸蟲屬(Calicophoron spp.)、盤吸蟲屬(Cotylophoron spp.)、巨盤吸蟲屬(Gigantocotyle spp.)、菲策吸蟲屬(Fischoederius spp.)、腹袋吸蟲屬(Gastrothylacus spp.)、背孔吸蟲屬
(Notocotylus spp.)、下彎吸蟲屬(Catatropis spp.)、斜睾吸蟲屬(Plagiorchis spp.)、前殖吸蟲屬(Prosthogonimus spp.)、雙腔吸蟲屬(Dicrocoelium spp.)、闊盤吸蟲屬(Eurytrema spp.)、鮭吸蟲屬(Troglotrema spp.)、並殖吸蟲屬(Paragonimus spp.)、肛瘤吸蟲屬(Collyriclum spp.)、隱孔吸蟲屬(Nanophyetus spp.)、後睾吸蟲屬(Opisthorchis spp.)、支睪吸蟲屬(Clonorchis spp.)、次睾吸蟲屬(Metorchis spp.)、異形吸蟲屬(Heterophyes spp.)、後殖吸蟲屬(Metagonimus spp.);棘頭動物門(Acanthocephala):少棘目(Oligacanthorhynchida),例如:巨吻棘頭蟲屬(Macracanthorhynchus spp.)、前睾棘頭蟲屬(Prosthenorchis spp.);多形目(Polymorphida),例如:細頸棘頭蟲屬(Filicollis spp.);念珠目(Moniliformida),例如:聯珠狀棘頭蟲屬(Moniliformis spp.);棘吻目(Echinorhynchida),例如:棘頭蟲屬(Acanthocephalus spp.)、魚棘頭蟲屬(Echinorhynchus spp.)、似細吻棘頭蟲屬(Leptorhynchoides spp.);舌形動物門(Pentastoma):孔頭蟲目(Porocephalida),例如:舌形蟲屬(Linguatula spp.)。
在獸醫與動物飼養領域中,式(I)、(Ia)、(Ib)或(Ic)化合物係呈合適之製劑型式,採用相關技藝上已知方法投藥,直接投藥或依經腸、非經腸式、經皮膚或經鼻投藥。該投藥法可為預防性或醫療性。
式(I)、(Ia)、(Ib)或(Ic)化合物若適當時,亦可視需要在某些濃度或施用率下,作為除草劑、安全劑、生長調節劑或改善植物性質之製劑、或作為殺微生物劑或殺配子劑使用,例如:殺真菌劑、抗霉劑、殺細菌劑、殺病毒劑(包括對抗類病毒之製劑)或作為對抗MLO(似黴漿菌生物體)與RLO(似立克次體生物體)之製劑。若適當時,其亦可作為合成其他活性化合物之中間物或前體使用。
調配物
本發明進一步有關一種調配物及由其製成包含至少一種式(I)、(Ia)、(Ib)或(Ic)化合物之除害蟲劑之施用形式,例如:浸液、滴液及噴液。有些例子中,該等施用形式可進一步包含其他除害蟲劑與/或改良效用之佐劑,如:滲透劑,例如:植物油(例如:油菜籽油、葵花油)、礦物油(例如:石蠟油)、植物性脂肪酸之烷基酯類(例如:油菜籽油甲基酯或大豆油甲基酯)、或烷醇烷氧化物,與/或分佈劑,例如:烷基矽氧烷類,及/或鹽類,例如:有機或無機銨或鏻鹽類,例如:硫酸銨或磷酸氫二銨,與/或促進滯留劑,例如:磺基琥珀酸二辛酯或羥基丙基關華豆膠聚合物,與/或保濕劑,例如:甘油,與/或肥料,例如:含銨-、鉀-或磷之肥料。
常用調配物為例如:水溶性液體(SL)、乳化懸浮劑(EC)、水性乳液(EW)、懸浮濃縮劑(SC、SE、FS、OD)、水勻散性粒劑(WG)、粒劑(GR)及膠囊濃縮劑(CS);此等及其他可能調配物型態說明於例如:FAO/WHO農藥說明聯合會議(FAO/WHO Joint Meeting on Pesticide Specifications,2004,ISBN:9251048576)之”國際作物與農藥說明,FAO與WHO農藥發展與用法手冊,FAO植物生產與保護報告-173(Crop Life International and in Pesticide Specifications,Manual on development and use of FAO and WHO specifications for Pesticide,FAO Plant Production and Protection Papers-173)”。除了一或多種式(I)、(Ia)、(Ib)或(Ic)化合物外,調配物中尚可視需要包含其他農化活性化合物。
此等較佳係包含輔劑(例如:補充劑、溶劑、自發性促進劑、載劑、乳化劑、勻散劑、霜害保護劑、殺生物劑、增稠劑與/或其他輔劑,例如:佐劑)之調配物或施用型式。本文中之佐劑係指可加強調配物生物效應,但本身沒有任何生物效應之組份。佐劑實例為促進滯留、分佈、附著
葉表面或滲透之製劑。
此等調配物係依已知方式製備,例如:混合式(I)、(Ia)、(Ib)
或(Ic)化合物與輔劑,如,例如:補充劑、溶劑與/或固態載劑與/或其他輔劑,如,例如:界面活性劑。調配物製法係在施用前或施用期間於合適設備中進行。
所使用輔劑為彼等可對式(I)、(Ia)、(Ib)或(Ic)化合物之調配
物或此等調配物所製成之施用型式(例如:現成可用之除害蟲劑,如:噴灑液或拌種劑)賦與特殊性質,如:某些物理、技術與/或生物性質之物質。
合適之補充劑為例如:水、極性與非極性有機化學液體,例
如:芳香系與非芳香系烴類(如:鏈烷烴、烷基苯、烷基萘、氯苯)、醇類與多元醇(若適當時,亦可經取代、醚化與/或酯化)、酮類(如:丙酮、環己酮)、酯類(包括脂肪類與油類)與(聚)醚類、未取代與經取代之胺類、醯胺類、內醯胺類(如:N-烷基吡咯啶酮)與內酯類、碸類與亞碸類(如:二甲亞碸)。
若使用水作為補充劑時,亦可使用例如:有機溶劑作為輔助
溶劑。基本上適用之液態溶劑為:芳香烴(如:二甲苯、甲苯、或烷基萘類)、氯化芳香烴與氯化脂族烴類(如:氯苯、氯化乙烯或二氯甲烷)、脂族烴類(如:環己烷或石蠟,例如:礦物油分餾物、礦物油與植物油)、醇類(如:丁醇或二醇類,及其醚類與酯類)、酮類(如:丙酮、甲基乙基酮、甲基異丁基酮或環已酮)、強極性溶劑(如:二甲基甲醯胺與二甲亞碸),及水。
原則上可能使用所有合適溶劑。合適溶劑實例為:芳香烴類
(如:二甲苯、甲苯或烷基萘類)、氯化芳香烴與氯化脂族烴類(如:氯苯、氯化乙烯或二氯甲烷)、脂族烴類(如:環己烷、石蠟、石油分餾物、礦物油與植物油)、醇類(如:甲醇、乙醇、異丙醇、丁醇或二醇類及其醚類與酯類)、酮類(如:丙酮、甲基乙基酮、甲基異丁基酮或環已酮)、強極性溶劑(如:
二甲亞碸),及水。
原則上可能使用所有合適載劑。適用之載劑尤其包括例如:
銨鹽及天然礦物磨粉,如:高嶺土、黏土、滑石、白堊、石英、矽鎂土、蒙脫土或矽藻土,及合成礦物粉末,如:高分散度矽石、氧化鋁與天然或合成矽酸鹽、樹脂、蠟類與/或固體肥料。亦可使用此等載劑之混合物。適用於粒劑之載劑包括例如:粉碎與分碎天然礦石,如:方解石、大理石、浮石、海泡石、白雲石,及無機與有機粉末之合成顆粒,及有機材料之顆粒如:鋸屑、紙、椰子殼、玉米穗軸與菸草稈。
亦可使用液化氣體補充劑或溶劑。特別適用之補充劑或載體
係彼等在環境溫度與常壓下呈氣態之載劑,例如:氣霧劑推進劑氣體,如:鹵烴類及丁烷、丙烷、氮氣與二氧化碳。
離子性與非離子性質乳化劑與/或泡沫形成劑、勻散劑或濕化劑、或此等界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、環氧乙烷與脂肪醇類或與脂肪酸或與脂肪胺、與經取代之苯酚(較佳為烷基苯酚或芳基苯酚)之聚縮合物、磺基琥珀酸酯之鹽類、牛磺酸衍生物(較佳係牛磺酸烷基酯)、聚乙氧基化醇或苯酚之磷酸酯、多元醇之脂肪酸酯,及該等包含硫酸根、磺酸根與磷酸根之化合物之衍生物,例如:烷基芳基聚二醇醚類、烷基磺酸酯類、烷基硫酸酯類、芳基磺酸酯類、蛋白質水解物、木質素亞硫酸鹽廢液與甲基纖維素。,若其中一種式(I)、(Ia)、(Ib)或(Ic)化合物與/或其中一種惰性載體不可溶於水且當使用水施用時,宜包含界面活性劑。
可能使用著色劑,如:無機色素(例如:氧化鐵,氧化鈦與普魯士藍)及有機染料,如:茜素染料,偶氮染料及金屬酞花青染料,及營養素與微量營養素,如:鐵、錳、硼、銅、鈷、鉬與鋅之鹽類,作為調配
物及其所衍生施用形式之其他輔劑。
其他組份可為安定劑,如:低溫安定劑、防腐劑、抗氧化劑、
光安定劑或其他改善化學/物理安定性之製劑。亦可包含泡沫形成劑或消泡劑。
亦可使用膠黏劑,如:羧甲基纖維素、天然與合成粉狀、粒
狀或膠乳狀聚合物,如:阿拉伯膠、聚乙烯醇、聚乙酸乙烯酯,或天然磷脂類,如:腦磷脂與卵磷脂,與合成之磷脂類作為調配物及其所衍生施用形式之其他輔劑。其他可能輔劑為礦物油與植物油。
可視需要在調配物及其所衍生施用形式中包含其他輔劑。此
等添加劑實例包括香料、保護性膠體、結合劑、黏著劑、增稠劑、搖變劑、滲透劑、促進滯留劑、安定劑、螯合劑、錯化劑、保濕劑、分佈劑。通常,式(I)、(Ia)、(Ib)或(Ic)化合物可配合調配目的,與任何常用之固態或液態添加劑組合使用。
適用之促進滯留劑包括所有彼等降低動力表面張力之物質,
例如:磺基琥珀酸二辛酯,或提高黏彈性之物質,例如:羥基丙基關華豆膠聚合物。
本文之合適滲透劑包括所有彼等常用於促進農化活性物質
滲透進入植物中之所有物質。本文中,滲透劑之定義為其從(通常為水性)施用液體及/或從噴液層滲透進入植物表皮層並藉以提高活性化合物在表皮中移動性之能力。可採用文獻中說明之方法(Baur等人之1997,Pesticide Science 51,131-152)來測定此性質。其實例包括醇烷氧化物(如:椰子脂肪基乙氧化物(10)或異十三碳烷基乙氧化物(12))、脂肪酸酯類(例如:油菜籽油甲酯或大豆油甲酯)、脂肪胺烷氧化物(例如:獸脂胺乙氧化物(15))、或銨與/或鏻鹽類,例如:硫酸銨或磷酸氫二銨。
調配物較佳係包含佔調配物重量0.00000001%至98%重量
比之間之各式(I)、(Ia)、(Ib)或(Ic)化合物,或特別佳係0.01%至95%重量比之各式(I)、(Ia)、(Ib)或(Ic)化合物,更佳係0.5%至90%重量比之之各式(I)、(Ia)、(Ib)或(Ic)化合物。
由調配物製成之施用型式(特定言之除害蟲劑)中之各式(I)、
(Ia)、(Ib)或(Ic)化合物含量可在很大範圍內變化。施用型式中之各式(I)、(Ia)、(Ib)或(Ic)化合物濃度通常佔該施用形式重量之0.00000001%至95%重量比,較佳在0.00001%至1%重量比。
式(I)、(Ia)、(Ib)或(Ic)化合物亦可與一種或多種合適之殺真菌劑、殺細菌劑、殺蜱蟎劑、殺軟體動物劑、殺線蟲劑、殺昆蟲劑、殺微生物劑、有利物質、除草劑、肥料、驅鳥劑、強化植物劑、不孕劑、安全劑、化學信息物質及/或植物生長調節劑形成混合物使用,藉以例如:擴大作用範圍、延長作用效期、提高作用速率、防止排斥或預防發展出抗性。此外,這種活性化合物組合可以改善植物生長及/或對非生物性因子之耐受性,例如:對高溫或低溫、對乾旱或對水份及/或鹽份含量上升之耐受性。亦可改善開花與結果性能、優化發芽能力與根部發展、促進收成及改善產量、影響成熟、改善所收成產物之品質與/或營養價值、延長儲存壽命及/或改善所收成產物之可加工性。
此外,式(I)、(Ia)、(Ib)或(Ic)化合物可與其他活性化合物或化學信息物質(如:引誘劑與/或驅鳥劑與/或植物活化劑與/或生長調劑與/或肥料)形成混合物。同樣地,式(I)、(Ia)、(Ib)或(Ic)化合物可用於改善植物性質,如,例如:生長、產量、及所收成材料之品質。
根據本發明特定具體實施例中,式(I)、(Ia)、(Ib)或(Ic)化合
物係與其他化合物,較佳係與下文說明之化合物形成混合物而含在調配物中或由該調配物製成之施用型式中。
若下文述及之其中一種化合物可出現不同互變異構型,即使沒有個別出示,此等型式亦均包括在內。
本文中以其俗名稱呼之活性化合物為已知者且說明於例如:農藥手冊(“農藥指南(The Pesticide Manual)”第16版,British Crop Protection Council 2012)或可參見網際網路(例如:http://www.alanwood.net/pesticides)。
(1)乙醯基膽鹼酯酶(AChE)抑制劑,如,例如:胺甲酸酯類,例如:安利卡(alanycarb)、得滅克(aldicarb)、本得卡(bendiocarb)、本伏卡(benfuracarb)、布卡辛(butocarboxim)、丁氧布卡辛(buthoxycarboxim)、加保利(carbaryl)、加保扶(carbofuran)、丁基加保扶(carbosulfan)、抑芬卡(ethiofencarb)、芬布卡(fenobucarb)、覆滅蟎(formetanate)、伏賽卡(furathiocarb)、滅必蝨(isoprocarb)、滅賜克(methiocarb)、納乃得(methomyl)、滅特卡(metolcarb)、歐殺滅(oxamyl)、比加普(pirimicarb)、安丹(propoxur)、硫敵克(thiodicarb)、硫芬斯(thiofanox)、三辛滅(triazamate)、三滅卡(trimethacarb)、XMC與滅爾蝨(xylylcarb);或有機磷酸酯類,例如:歐殺松(acephate)、亞滅伏(azamethiphos)、谷速松(azinphos)-乙基、谷速松(azinphos)-甲基、卡速松(cadusafos)、氯乙松(chlorethoxyfos)、氯芬松(chlorfenvinphos)、氯滅松(chlormephos)、陶斯松(chlorpyrifos)-甲基、庫伏斯(coumaphos)、氰乃松(cyanophos)、滅賜松(demeton)-S-甲基、大利松(diazinon)、二氯松(dichlorvos)/DDVP、雙特松(dicrotophos)、大滅松(dimethoate)、大芬松(dimethylvinphos)、二硫松(disulfoton)、EPN、愛殺松(ethion)、普伏松
(ethoprophos)、胺磺磷(famphur)、芬滅松(fenamiphos)、撲滅松(fenitrothion)、芬殺松(fenthion)、福賽特(fosthiazate)、飛達松(heptenophos)、抑滅伏(imicyafos)、抑伏松(isofenphos)、O-(甲氧基胺基硫代磷醯基)水楊酸異丙基酯、抑殺松(isoxathion)、馬拉松(malathion)、滅加松(mecarbam)、達馬松(methamidophos)、滅大松(methidathion)、美文松(mevinphos)、亞素靈(monocrotophos)、乃立松(naled)、歐滅松(omethoate)、歐滅賜松(oxydemeton)-甲基、巴拉松(parathion)-甲基、賽達松(phenthoate)、福瑞松(phorate)、裕必松(phosalone)、益滅松(phosmet)、福賜米松(phosphamidon)、辛硫磷(phoxim)、亞特松(pirimiphos)-甲基、佈飛松(profenofos)、普丹松(propetamphos)、普硫松(prothiofos)、必伏松(pyraclofos)、必芬松(pyridaphenthion)、拜裕松(quinalphos)、速伏特(sulfotep)、特必松(tebupirimfos)、亞培松(temephos)、託福松(terbufos)、四氯松(tetrachlorvinphos)、硫滅松(thiometon)、三落松(triazophos)、三氯松(triclorfon)與繁米松(vamidothion)。
(2)GABA-閘控之氯離子通道擷抗劑,如,例如:環二烯有機氯,例如:克丹(chlordane)與安殺番(endosulfan);或苯基吡唑類(飛普洛類(Fiprole)),例如:抑普洛(ethiprole)與芬普洛(fipronil)。
(3)鈉通道調節劑/依賴電壓之鈉通道阻斷劑,如,例如:擬除蟲菊酯類,例如:阿納寧(acrinathrin)、丙烯菊酯(allethrin)、d-順式-反式丙烯菊酯(allethrin)、d-反式丙烯菊酯(allethrin)、畢芬寧(bifenthrin)、右亞列寧(bioallethrin)、右亞列寧(bioallethrin)S-環戊烯基異構物、必賽靈(bioresmethrin)、乙氰菊酯(cycloprothrin)、賽扶寧(cyfluthrin)、β-賽扶寧(cyfluthrin)、賽洛寧(cyhalothrin)、λ-賽洛寧(cyhalothrin)、γ-賽洛寧(cyhalothrin)、賽滅寧(cypermethrin)、α-賽滅寧(cypermethrin)、β-賽滅寧
(cypermethrin)、θ-賽滅寧(cypermethrin)、ζ-賽滅寧(cypermethrin)、賽芬寧(cyphenothrin)[(1R)-反式異構物]、第滅寧(deltamethrin)、依普靈(empenthrin)[(EZ)-(1R)異構物]、益化利(esfenvalerate)、依芬寧(etofenprox)、芬普寧(fenpropathrin)、芬化利(fenvalerate)、福本賽寧(flucythrinate)、伏滅寧(flumethrin)、τ-福化利(fluvalinate)、海本斯(halfenprox)、益普靈(imiprothrin)、剋特寧(kadethrin)、百滅寧(permethrin)、芬特寧(phenothrin)[(1R)-反式異構物)、普烈靈(prallethrin)、除蟲菊酯(pyrethrins(pyrethrum))、利滅靈(resmethrin)、希拉芬(silafluofen)、特伏靈(tefluthrin)、特滅靈(tetramethrin)、特滅靈(tetramethrin)[(1R)異構物)]、泰滅寧(tralomethrin)與參伏靈(transfluthrin);或DDT;或美克氯(methoxychlor)。
(4)菸鹼激導性乙醯基膽鹼受體(nAChR)促效劑,如,例如:類新菸鹼類,例如:乙醯普(acetamiprid)、克利定(clothianidin)、第諾芬(dinotefuran)、益達胺(imidacloprid)、尼普爛(nitenpyram)、硫克比(thiacloprid)與賽速安(thiamethoxam);或尼古丁或碸蟲啶(sulfoxaflor)。
(5)異位性菸鹼激導性乙醯基膽鹼受體(nAChR)活化劑,如,例如:賜諾殺類(Spinosyns)、例如:賜諾特(spinetoram)與賜諾殺(spinosad)。
(6)氯離子通道活化劑,如,例如:抑滅克定類(avermectins)/美保黴素(milbemycin),例如:艾滅克定(abamectin)、抑滅克定(emamectin)苯甲酸鹽、利滅克定(lepimectin)與美保克定(milbemectin)。
(7)幼保激素擬似物,如,例如:幼保激素類似物,例如:赫普靈(hydroprene)、克普靈(kinoprene)與滅普靈(methoprene);或吩克卡(fenoxycarb);或必普芬(pyriproxyfen)。
(8)作用機轉未知或非專一性之活性化合物,如,例如:烷基鹵化物,例如:甲基溴及其他烷基鹵化物;或氯吡靈(chloropicrin);或硫醯氟;或硼砂;或酒石酸銻鉀鹽。
(9)選擇性抗攝食劑,例如:必滅辛(pymetrozine)或伏卡滅(flonicamid)。
(10)蟎生長抑制劑,例如:克芬辛(clofentezine)、海賽唑(hexythiazox)與地伏辛(diflovidazin)或抑特唑(etoxazole)。
(11)昆蟲腸膜之微生物瓦解劑,例如:蘇雲金芽胞桿菌以色列亞種(Bacillus thuringiensis subspecies israelensis)、球形芽孢桿菌(Bacillus sphaericus)、蘇雲金芽胞桿菌鮎澤亞種(Bacillus thuringiensis subspecies aizawai)、蘇雲金芽胞桿菌庫斯塔基亞種(Bacillus thuringiensis subspecies kurstaki)、蘇雲金芽胞桿菌殺蟲亞種(Bacillus thuringiensis subspecies tenebrionis)與BT植物蛋白質:Cry1Ab、Cry1Ac、Cry1Fa、Cry2Ab、mCry3A、Cry3Ab、Cry3Bb、Cry34/35Ab1。
(12)氧化性磷酸化反應抑制劑,ATP瓦解劑,如,例如:地芬能(diafenthiuron);或有機錫化合物,例如:亞賽錫(azocyclotin)、賽赫錫(cyhexatin)與芬塔錫(fenbutatin)氧化物;或歐蟎多(propargite)或特達芬(tetradifon)。
(13)干擾H-質子梯度之氧化性磷酸化反應去偶合劑,如,例如:克芬吡(chlorfenapyr)、DNOC與氟蟲胺(sulfluramid)。
(14)菸鹼激導性乙醯基膽鹼受體擷抗劑,如,例如:本速達(bensultap)、培丹(cartap)鹽酸鹽、硫克蘭(thiocylam)與硫速伏(thiosultap)-鈉。
(15)幾丁質生合成抑制劑,第0型,如,例如:必賽伏(bistrifluron)、克伏能(chlofluazuron)、地伏能(diflubenzuron)、福環脲(flucycloxuron)、氟芬隆(flufenoxuron)、赫姆能(hexaflumuron)、利芬能(lufenuron)、利化能(novaluron)、諾化能(noviflumuron)、特速能(teflubenzuron)與三伏能(triflumuron)。
(16)幾丁質生合成抑制劑,第1型,如,例如:佈芬辛(buprofezin)。
(17)蛻變瓦解劑(特定言之雙翅目,亦即雙翅目昆蟲),如,例如:賽麻辛(cyromazine)。
(18)脫皮激素受體促效劑,如,例如:可芬諾(chromafenozide)、赫芬賽(halofenozide)、甲氧芬賽(methoxyfenozide)與特芬賽(tebufenozide)。
(19)章魚胺激導性促效劑,如,例如:三亞蟎(amitraz)。
(20)複合物-III電子傳遞抑制劑,如,例如:海滅能(hydramethylnone)或亞克希(acequinocyl)或伏克靈(fluacrypyrim)。
(21)複合物-I電子傳遞抑制劑,例如:METI殺蟎劑,例如:芬殺蟎(fenazaquin)芬普蟎(fenpyroximate)、普靈芬(pyrimidifen)、畢達本(pyridaben)、達芬必(tebufenpyrad)與特芬必(tolfenpyrad);或魚藤精(rotenone)(Derris)。
(22)電壓閘控之鈉通道阻斷劑,例如:因得克(indoxacarb)或滅伏美松(metaflumizone)。
(23)乙醯基-Co-A羧酸酶之抑制劑,如,例如:季酮酸與吡咯酮酸衍生物,例如:螺克芬(spirodiclofen)、螺滅芬(spiromesifen)與賜派滅(spirotetramat)。
(24)複合物-IV電子傳遞抑制劑,如,例如:膦類,例如:磷化鋁、磷化鈣、膦與磷化鋅;或氰化物。
(25)複合物-II電子傳遞抑制劑,如,例如:氰必吩(cyenopyrafen)與賽芬蟎(cyflumetofen)。
(28)蘭尼鹼(ryanodine)受體效應劑,如,例如:二醯胺類,例如:氯蔥吡咯(chlorantraniliprole)、氰蟲醯胺(cyantraniliprole)與表氟蟲胺(flubendiamide),其他活性化合物,如,例如:艾特本(afidopyropen)、查得定(azadirachtin)、苯克賽(benclothiaz)、苯賽滅(benzoximate)、必芬賽(bifenazate)、新殺蟎(bromopropylate)、蟎離丹(chinomethionat)、克利得(cryolite),
大克蟎(dicofol)、氟蟎四嗪(diflovidazin)、氟速吩(fluensulfone)、氟喹啉(flometoquin)、伏吩靈(flufenerim)、氟菌蟎酯(flufenoxystrobin)、丁烯氟蟲腈(flufiprole)、氟吡菌醯胺(fluopyram)、伏達隆(flupyradifurone)、呋喃蟲醯肼(fufenozide)、氯氟醚菊酯(heptafluthrin)、氯噻啉(imidaclothiz)、依普同(iprodione)、氯氟醚菊酯(meperfluthrin)、哌蟲啶(paichongding)、必伏拜(pyflubumide)、必伏松(pyrifluquinazon)、嘧蟎胺(pyriminostrobin)、四氟醚菊酯(tetramethylfluthrin)與碘甲烷;及其他基於堅強芽孢桿菌(Bacillus firmus)之製劑(I-1582,BioNeem,Votivo),與下列化合物:3-溴-N-{2-溴-4-氯-6-[(1-環丙基乙基)胺甲醯基]苯基}-1-(3-氯吡啶-2-基)-1H-吡唑-5-羧醯胺(自WO2005/077934中已知)與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(自WO2006/043635中已知)、{1'-[(2E)-3-(4-氯苯基)丙-2-烯-1-基]-5-氟螺[吲哚-3,4'-哌啶]-1(2H)-基}(2-氯吡啶-4-基)甲酮(自WO2003/106457中已知)、2-氯-N-[2-{1-[(2E)-3-(4-氯苯基)丙-2-烯-1-基]哌啶-4-基}-4-(三氟甲基)苯基]異菸鹼醯胺(自WO2006/003494中已知)、3-(2,5-二甲基苯基)-4-羥基-8-甲氧基-1,8-重氮螺[4.5]癸-3-烯-2-酮(自WO2009/049851中已知)、碳酸3-(2,5-二甲基苯基)-8-甲氧基-2-側氧基-1,8-重氮螺[4.5]癸-3-烯-4-基-乙基酯(自WO2009/049851中已知)、4-(丁-2-炔-1-基氧)-6-(3,5-二甲基哌啶-1-基)-5-氟嘧啶(自WO2004/099160中已知)、4-(丁-2-炔-1-基氧)-6-(3-氯苯基)嘧啶(自WO2003/076415中已知)、PF1364(CAS登錄號1204776-60-2)、4-[5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫-1,2-唑-3-基]-2-甲基-N-{2-側氧基-2-[(2,2,2-三氟乙基)胺基]乙基}苯甲醯胺(自WO2005/085216中已知)、4-{5-[3-氯-5-(三氟甲基)苯基]-5-(三氟甲基)-4,5-二氫-1,2-唑-3-基}-N-{2-側氧基-2-[(2,2,2-三氟乙基)胺基]乙基}-1-萘甲醯胺(自WO2009/002809中已知)、2-[2-({[3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-
基]羰基}胺基)-5-氯-3-甲基苯甲醯基]-2-甲基肼羧酸甲酯(自WO2005/085216中已知)、2-[2-({[3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基]羰基}胺基)-5-氰基-3-甲基苯甲醯基]-2-乙基肼羧酸甲酯(自WO2005/085216中已知)、2-[2-({[3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基]羰基}胺基)-5-氰基-3-甲基苯甲醯基]-2-甲基肼羧酸甲酯(自WO2005/085216中已知)、2-[3,5-二溴-2-({[3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基]羰基}胺基)苯甲醯基]-2-乙基肼羧酸甲基酯(自WO2005/085216中已知)、1-(3-氯吡啶-2-基)-N-[4-氰基-2-甲基-6-(甲基胺甲醯基)苯基]-3-{[5-(三氟甲基)-2H-四唑-2-基]甲基}-1H-吡唑-5-羧醯胺(自WO2010/069502中已知)、N-[2-(5-胺基-1,3,4-噻二唑-2-基)-4-氯-6-甲基苯基]-3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-羧醯胺(自CN102057925中已知)、3-氯-N-(2-氰基丙烷-2-基)-N-[4-(1,1,1,2,3,3,3-七氟丙烷-2-基)-2-甲基苯基]酞醯胺(自WO2012/034472中已知)、8-氯-N-[(2-氯-5-甲氧基苯基)磺醯基]-6-(三氟甲基)咪唑并[1,2-a]吡啶-2-羧醯胺(自WO2010/129500中已知)、4-[5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫-1,2-唑-3-基]-2-甲基-N-(1-氧離子基硫雜環丁烷-3-基)苯甲醯胺(自WO2009/080250中已知)、4-[5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫-1,2-唑-3-基]-2-甲基-N-(1-氧離子基硫雜環丁烷-3-基)苯甲醯胺(自WO2012/029672中已知)、1-[(2-氯-1,3-噻唑-5-基)甲基]-4-側氧基-3-苯基-4H-吡啶并[1,2-a]嘧啶-1-鎓-2-醇酸鹽(自WO2009/099929中已知)、1-[(6-氯吡啶-3-基)甲基]-4-側氧基-3-苯基-4H-吡啶并[1,2-a]嘧啶-1-鎓-2-醇酸鹽(自WO2009/099929中已知)、(5S,8R)-1-[(6-氯吡啶-3-基)甲基]-9-硝基-2,3,5,6,7,8-六氫-1H-5,8-環氧咪唑并[1,2-a]氮雜環庚烯(自WO2010/069266中已知)、(2E)-1-[(6-氯吡啶-3-基)甲基]-N'-硝基-2-亞戊基肼甲脒(自WO2010/060231中已知)、4-(3-{2,6-二氯-4-[(3,3-二氯丙-2-烯-1-基)氧]苯氧基}丙氧基)-2-甲氧基-6-(三氟甲基)嘧啶(自CN101337940中已知)、
N-[2-(第三丁基胺甲醯基)-4-氯-6-甲基苯基]-1-(3-氯吡啶-2-基)-3-(氟甲氧基)-1H-吡唑-5-羧醯胺(自WO2008/134969中已知)。
本文中以其俗名稱呼之活性化合物為已知者且說明於例如:“農藥指南(The Pesticide Manual)“或網際網路(例如:http://www.alanwood.net/pesticides)。
(1)麥角固醇生合成抑制劑,如,例如:(1.1)艾狄莫(aldimorph)、(1.2)阿克唑(azaconazole)、(1.3)拜坦諾(bitertanol)、(1.4)布康唑(bromuconazole)、(1.5)西普康唑(cyproconazole)、(1.6)二氯丁唑(diclobutrazole)、(1.7)地吩康唑(difenoconazole)、(1.8)地康唑(diniconazole)、(1.9)地康唑-M(diniconazole-M)、(1.10)得莫(dodemorph)、(1.11)得莫乙酸鹽(dodemorph acetate)、(1.12)環氧克唑(epoxiconazole)、(1.13)抑達唑(etaconzole)、(1.14)芬利莫(fenarimol)、(1.15)芬康唑(fenbuconazole)、(1.16)吩醯胺(fenhexamide)、(1.17)芬普定(fenpropidin)、(1.18)芬普福(fenpropimorph)、(1.19)伏克康唑(fluquinconazole)、(1.20)伏米得(flurprimidol)、(1.21)護矽得(flusilazole)、(1.22)護汰芬(flutriafol)、(1.23)伏康唑(furconazole)、(1.24)順式伏康唑(furconazole-cis))、(1.25)赫康唑(hexaconazole)、(1.26)依滅列(imazalil)、(1.27)依滅列硫酸鹽(imazalil sulphate)、(1.28)抑本康唑(imibenconazole)、(1.29)抑普康唑(ipconazole)、(1.30)滅康唑(metconazole)、(1.31)麥克坦尼(myclobutanil)、(1.32)納得吩(naftifin)、(1.33)紐莫(nuarimol)、(1.34)康唑(oxpoconazole)、(1.35)巴克素(paclobutrazole)、(1.36)比菲唑(pefurazoate)、(1.37)本康唑(penconazole)、(1.38)哌布靈(piperalin)、(1.39)撲克樂(prochloraz)、(1.40)普克利(propiconazole)、(1.41)普賽康唑(prothioconazole)、(1.42)必達克(pyributicarb)、(1.43)比芬斯(pyrifenox)、
(1.44)克康唑(quinconazole)、(1.45)辛康唑(simeconazole)、(1.46)賜必安(spiroxamine)、(1.47)得克利(tebuconazole)、(1.48)特本吩(terbinafin)、(1.49)特康唑(tetraconazole)、(1.50)三泰芬(triadimefon)、(1.51)三泰隆(triadimennol)、(1.52)賽得莫(tridemorph)、(1.53)三伏唑(triflumizol)、(1.54)賽福寧(triforine)、(1.55)三狄康唑(triticonazole)、(1.56)優康唑(uniconazole)、(1.57)優康唑-P(uniconazol-p)、(1.58)芬克唑(viniconazole)、(1.59)福康唑(voriconazole)、(1.60)1-(4-氯苯基)-2-(1H-1,2,4-三唑-1-基)環庚醇、(1.61)1-(2,2-二甲基-2,3-二氫-1H-茚-1-基)-1H-咪唑-5-羧酸甲酯、(1.62)N'-{5-(二氟甲基)-2-甲基-4-[3-(三甲基矽烷基)丙氧基]苯基}-N-乙基-N-甲基甲脒、(1.63)N-乙基-N-甲基-N'-{2-甲基-5-(三氟甲基)-4-[3-(三甲基矽烷基)丙氧基]苯基}甲脒與(1.64)O-[1-(4-甲氧基苯氧基)-3,3-二甲基丁烷-2-基]-1H-咪唑-1-硫代甲酸酯、(1.65)啶菌唑(pyrisoxazole)。
(2)呼吸抑制劑(呼吸鏈抑制劑),如,例如:(2.1)必賽吩(bixafen)、(2.2)保卡利(boscalid)、(2.3)卡布辛(carboxin)、(2.4)地伏滅靈(diflumetorim)、(2.5)芬伏爛(fenfuram)、(2.6)護派楠(fluopyram)、(2.7)護坦尼(flutolanil)、(2.8)護賽保(fluxapyroxad)、(2.9)福滅普(furametpyr)、(2.10)福滅克(furmecyclox)、(2.11)抑本散(isopyrazam)之順-差向異構體消旋物1RS,4SR,9RS與反-差向異構體消旋物1RS,4SR,9SR混合物、(2.12)抑本散(isopyrazam)(反-差向異構體消旋物)、(2.13)抑本散(isopyrazam)(反-差向異構體對映異構物1R,4S,9S)、(2.14)抑本散(isopyrazam)(反-差向異構體對映異構物1S,4R,9R)、(2.15)抑本散(isopyrazam)(順-差向異構體消旋物1RS,4SR,9RS)、(2.16)抑本散(isopyrazam)(順-差向異構體對映異構物1R,4S,9R)、(2.17)抑本散(isopyrazam)(順-差向異構體對映異構物1S,4R,9S)、(2.18)米普尼(mepronil)、(2.19)嘉得信(oxycarboxin)、(2.20)本福吩(penflufen)、(2.21)本賽能
(penthiopyrad)、(2.22)速達散(sedaxane)、(2.23)地伏醯胺(thifluzamid)、(2.24)1-甲基-N-[2-(1,1,2,2-四氟乙氧基)苯基]-3-(三氟甲基)-1H-吡唑-4-羧醯胺、(2.25)3-(二氟甲基)-1-甲基-N-[2-(1,1,2,2-四氟乙氧基)苯基]-1H-吡唑-4-羧醯胺、(2.26)3-(二氟甲基)-N-[4-氟-2-(1,1,2,3,3,3-六氟丙氧基)苯基]-1-甲基-1H-吡唑-4-羧醯胺、(2.27)N-[1-(2,4-二氯苯基)-1-甲氧基丙烷-2-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺、(2.28)5,8-二氟-N-[2-(2-氟-4-{[4-(三氟甲基)吡啶-2-基]氧}苯基)乙基]喹唑啉-4-胺、(2.29)苯索伏比(benzovindiflupyr)、(2.30)N-[(1S,4R)-9-(二氯亞甲基)-1,2,3,4-四氫-1,4-甲撐基萘-5-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺與(2.31)N-[(1R,4S)-9-(二氯亞甲基)-1,2,3,4-四氫-1,4-甲撐基萘-5-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺、(2.32)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-羧醯胺、(2.33)1,3,5-三甲基-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-羧醯胺、(2.34)1-甲基-3-(三氟甲基)-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-羧醯胺、(2.35)1-甲基-3-(三氟甲基)-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.36)1-甲基-3-(三氟甲基)-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.37)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-羧醯胺、(2.38)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-羧醯胺、(2.39)1,3,5-三甲基-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.40)1,3,5-三甲基-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.41)麥鏽靈(benodanil)、(2.42)2-氯-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)吡啶-3-羧醯胺、(2.43)抑吩滅(isofetamid)。
(3)作用於呼吸鏈複合物III之呼吸抑制劑(呼吸鏈抑制劑),如,例如:(3.1)辛唑嘧菌胺(ametoctradin)、(3.2)安美速(amisulbrom)、(3.3)亞托敏
(azoxystrobin)、(3.4)賽發滅(cyazofamid)、(3.5)甲香菌酯(coumethoxystrobin)、(3.6)丁香菌酯(coumoxystrobin)、(3.5)醚菌胺(dimoxystrobin)、(3.6)烯肟菌酯(enestroburin)、(3.9)芬色丹(famoxadone)、(3.10)芬滅酮(fenamidone)、(3.11)吩嘧菌酯(fenoxystrobin)、(3.12)氟嘧菌酯(fluoxastrobin)、(3.13)甲基醚菌酯(kresoxim-methyl)、(3.14)苯氧菌胺(metominostrobin)、(3.15)肟醚菌胺(orysastrobin)、(3.16)啶氧菌酯(picoxystrobin)、(3.17)唑菌胺酯(pyraclostrobin)、(3.18)唑胺菌酯(pyrametostrobin)、(3.19)唑菌酯(pyraoxystrobin)、(3.20)吡菌苯威(pyribencarb)、(3.21)三氯比(triclopyricarb)、(3.22)三氟敏(trifloxystrobin)、(3.23)(2E)-2-(2-{[6-(3-氯-2-甲基苯氧基)-5-氟嘧啶-4-基]氧}苯基)-2-(甲氧基亞胺基)-N-甲基乙醯胺、(3.24)(2E)-2-(甲氧基亞胺基)-N-甲基-2-(2-{[({(1E)-1-[3-(三氟甲基)苯基]亞乙基}胺基)氧]甲基}苯基)乙醯胺、(3.25)(2E)-2-(甲氧基亞胺基)-N-甲基-2-{2-[(E)-({1-[3-(三氟甲基)苯基]乙氧基}亞胺基)甲基]苯基}乙醯胺、(3.26)(2E)-2-{2-[({[(1E)-1-(3-{[(E)-1-氟-2-苯基乙烯基]氧}苯基)亞乙基]胺基}氧)甲基]苯基}-2-(甲氧基亞胺基)-N-甲基乙醯胺、(3.27)(2E)-2-{2-[({[(2E,3E)-4-(2,6-二氯苯基)亞丁-3-烯-2-基]胺基}氧)甲基]苯基}-2-(甲氧基亞胺基)-N-甲基乙醯胺、(3.28)2-氯-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)吡啶-3-羧醯胺、(3.29)5-甲氧基-2-甲基-4-(2-{[({(1E)-1-[3-(三氟甲基)苯基]亞乙基}胺基)氧]甲基}苯基)-2,4-二氫-3H-1,2,4-三唑-3-酮、(3.30)(2E)-2-{2-[({環丙基[(4-甲氧基苯基)亞胺基]甲基}氫硫基)甲基]苯基}-3-甲氧基丙-2-烯酸甲酯、(3.31)N-(3-乙基-3,5,5-三甲基環己基)-3-(甲醯基胺基)-2-羥基苯甲醯胺、(3.32)2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺。
(4)有絲分裂與細胞分化之抑制劑,如,例如:(4.1)免賴德(benomyl)、(4.2)
卡苯辛(carbendazim)、(4.3)氯吩唑(chlorfenazole)、(4.4)地吩卡(diethofencarb)、(4.5)噻唑菌胺(ethaboxam)、(4.6)氟吡菌胺(fluopicolide)、(4.7)伏塔唑(fuberidazole)、(4.8)賓克隆(pencyeuron)、(4.9)腐絕(thiabendazole)、(4.10)甲基多保淨(thiophanate-methyl)、(4.11)多保淨(thiophanate)、(4.12)索醯胺(zoxamide)、(4.13)5-氯-7-(4-甲基哌啶-1-基)-6-(2,4,6-三氟苯基)[1,2,4]三唑并[1,5-a]嘧啶與(4.14)3-氯-5-(6-氯吡啶-3-基)-6-甲基-4-(2,4,6-三氟苯基)嗒。
(5)具有多重位點活性之化合物,如,例如:(5.1)波爾多(Bordeaux)混合物、(5.2)四氯丹(captafol)、(5.3)蓋普丹(captan)、(5.4)四氯異苯腈(chlorothalonil)、(5.5)銅製劑,如:氫氧化銅、(5.6)萘甲酸銅、(5.7)氧化銅、(5.8)鹼性氯氧化銅、(5.9)硫酸銅、(5.10)益發靈(dichlofluanid)、(5.11)腈硫醌(dithianon)、(5.12)多寧(dodine)、(5.13)多寧游離鹼、(5.14)富爾邦(ferbam)、(5.15)護福爾培(fluorofolpet)、(5.16)福爾培(folpet)、(5.17)免熱淨(guazatine)、(5.18)免熱淨乙酸鹽(guazatine acetate)、(5.19)抑克定(iminoctadine)、(5.20)抑克定苯烷磺酸鹽(iminoctadine albesilate)、(5.21)抑克定(iminoctadine)三乙酸鹽、(5.22)錳銅(mancopper)、(5.23)錳粉克(mancozeb)、(5.24)錳乃浦(maneb)、(5.25)滅得賴(metiram)、(5.26)滅得賴鋅鹽、(5.27)快得寧(copper-oxine)、(5.28)丙氧苯脒(propamidine)、(5.29)甲基鋅乃浦(propineb)、(5.30)硫與硫製劑,如,例如:多硫化鈣、(5.31)得恩地(thiram)、(5.32)特伏奈(tolylfluanid)、(5.33)鋅乃浦(zineb)、(5.34)益穗(ziram)與(5.35)敵菌靈(anilazine)。
(6)抗性誘發劑,如,例如:(6.1)阿拉酸式苯(acibenzolar)-S-甲基、(6.2)異噻菌胺(isotianil)、(6.3)撲殺熱(probenazole)、(6.4)地得尼(tiadinil)與(6.5)昆布多醣(laminarin)。
(7)胺基酸與蛋白質生合成抑制劑,如,例如:(7.1)、(7.2)保米黴素(blasticidin-S)、(7.3)嘧菌環胺(cyprodinil)、(7.4)賜黴素(kasugamycin)、(7.5)
賜黴素鹽酸鹽水合物(kasugamycin hydrochloride hydrate)、(7.6)米本靈(mepanipyrim)、(7.7)比坦尼(pyrimethanil)、(7.8)3-(5-氟-3,3,4,4-四甲基-3,4-二氫異喹啉-1-基)喹啉、與(7.9)土黴素(oxytetracycline)與(7.10)鏈黴素(streptomycin)。
(8)ATP生產抑制劑,如,例如:(8.1)三苯醋錫(fentin acetate)、(8.2)三苯氯錫(fentin chloride)、(8.3)三苯錫氫氧化物(fentin hydroxide)與(8.4)矽硫吩(silthiofam)。
(9)細胞壁合成抑制劑,如,例如:(9.1)苯賽卡(benthiavalicarb)、(9.2)地滅莫(dimethomorph)、(9.3)伏莫(flumorph)、(9.4)抑發利(iprovalicarb)、(9.5)曼普胺(mandipropamid)、(9.6)保粒黴素(polyoxins)、(9.7)保粒靈(polyoxorim)、(9.8)瓦利黴素(validamycin A)、(9.9)發利列(valifenalate)與(9.10)保粒黴素(polyoxin)B。
(10)脂質與膜合成抑制劑,如,例如:(10.1)聯苯、(10.2)地茂散(chloroneb)、(10.3)大克爛(dicloran)、(10.4)護粒松(edifenphos)、(10.5)依得利(etridiazole)、(10.6)碘卡(iodocarb)、(10.7)丙基喜樂松(iprobenfos)、(10.8)亞賜普醇烷(isoprothiolane)、(10.9)普莫卡(propamocarb)、(10.10)普莫卡鹽酸鹽(propamocarb hydrochloride)、(10.11)硫菌威(prothiocarb)、(10.12)白粉松(pyrazophos)、(10.13)五氯硝苯(quintozene)、(10.14)四氯硝苯(tecnazene)與(10.15)特克斯-甲基(tolclofos-methyl)基。
(11)黑色素生合成抑制劑,如,例如:(11.1)卡普醯胺(capropamid))、(11.2)地克賽(diclocymet)、(11.3)芬散尼(fenoxanil)、(11.4)太得(fthalide)、(11.5)百快隆(pyroquilon)、(11.6)三賽唑(tricyclazole)與(11.7){3-甲基-1-[(4-甲基苯甲醯基)胺基]丁烷-2-基}胺甲酸2,2,2-三氟乙基酯。
(12)核酸合成抑制劑,如,例如:(12.1)本達樂(benalaxyl)、(12.2)本達樂
-M(benalaxyl-M)(克拉利(kiralaxyl))、(12.3)布滅莫(bupirimate)、(12.4)克拉肯(clozylacon)、(12.5)地滅利(dimethirimol)、(12.6)抑利莫(ethirimol)、(12.7)伏拉希(furalaxyl)、(12.8)殺紋寧(hymexazol)、(12.9)滅達樂(metalaxyl)、(12.10)滅達樂-M(metalaxyl-M)(滅芬散(mefenoxam))、(12.11)歐弗斯(ofurace)、(12.12)歐殺斯(oxadixyl)、(12.13)啉酸(oxolinic acid)與(12.14)歐奇農(octhilinone)。
(13)訊號轉導抑制劑,如,例如:(13.1)氯唑內(chlozolinate)、(13.2)拌種咯(fenpiclonil)、(13.3)護汰寧(fludioxonil)、(13.4)依普同(iprodione)、(13.5)撲滅寧(procymidone)、(13.6)快諾芬(quinoxyfen)、(13.7)免克寧(vinclozolin)與(13.8)丙氧喹啉(proquinazid)。
(14)去偶合劑,如,例如:(14.1)百蟎克(binapacryl)、(14.2)白粉克(dinocap)、(14.3)富米松(ferimzone)、(14.4)扶吉胺(fluazinam))與(14.5)敵蟎普(meptyldinocap)。
(15)其他化合物,如,例如:(15.1)本塞唑(benthizole)、(15.2)苯(bethoxazine)、(15.3)卡普黴素(capsimycin)、(15.4)卡吩(carvone)、(15.5)喹啉甲硫胺酸鹽(chinomethionat)、(15.6)必伏農(pyriofenone)(克吩農(chlazafenon))、(15.7)庫發尼(cufraneb)、(15.8)賽伏醯胺(cyflufenamid)、(15.9)西莫尼(cymoxanil)、(15.10)環丙磺草胺(cyprosulfamide)、(15.11)邁隆(dazomet)、(15.12)迪布卡(debacarb)、(15.13)二氯吩(dichlorophen)、(15.14)地克美辛(diclomezine)、(15.15)地吩唑克(difenzoquat)、(15.16)地吩唑克甲基硫酸鹽、(15.17)二苯基胺、(15.18)抑克滅(EcoMate)、(15.19)吩普胺(fenpyrazamine)、(15.20)伏特夫(flumetover)、(15.21)氟菌丹(fluoromid)、(15.22)護硫醯胺(flusulphamide)、(15.23)噻菌淨(flutianil)、(15.24)福賽得鋁(fosetyl-aluminium)、(15.25)福賽得鈣(fosetyl-calcium)、(15.26)福賽得鈉
(fosetyl-sodium)、(15.27)六氯苯、(15.28)依麻黴素(irumamycin)、(15.29)滅速卡(methasulfocarb)、(15.30)異硫氰酸甲酯、(15.31)滅奇吩(metrafenone)、(15.32)米德黴素(mildiomycin)、(15.33)納坦黴素(natamycin)、(15.34)二甲基二硫代胺甲酸鎳、(15.35)硝基太(nitrothal)-異丙基、(15.36)歐奇農(octhilinone)、(15.37)歐賽保(oxamocarb)、(15.38)歐芬汀(oxyfenthiin)、(15.39)五氯酚與其鹽類、(15.40)酚丁滅蝨(phenothrin)、(15.41)磷酸與其鹽類、(15.42)霜黴威乙膦酸鹽(propamocarb-fosetylate)、(15.43)普辛(propanosine)-鈉、(15.44)丁吡嗎啉(pyrimorph)、(15.45)(2E)-3-(4-第三丁基苯基)-3-(2-氯吡啶-4-基)-1-(嗎啉-4-基)丙-2-烯-1-酮、(15.46)(2Z)-3-(4-第三丁基苯基)-3-(2-氯吡啶-4-基)-1-(嗎啉-4-基)丙-2-烯-1-酮、(15.47)吡咯靈(pyrrolnitrin)、(15.48)美爾奎寧(tebufloquin)、(15.49)特克爛(tecloftalam)、(15.50)特伏尼(tolnifanid)、(15.51)三唑氧(triazoxide)、(15.52)三氯醯胺(trichlamide)、(15.53)奇利醯胺(zarilamid)、(15.54)2-甲基丙酸(3S,6S,7R,8R)-8-苯甲基-3-[({3-[(異丁醯基氧)甲氧基]-4-甲氧基吡啶-2-基}羰基)胺基]-6-甲基-4,9-二側氧基-1,5-二側氧基壬-7-基酯、(15.55)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}哌啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮、(15.56)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}哌啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮、(15.57)1-(4-{4-[5-(2,6-二氟苯基)-4,5-二氫-1,2-唑-3-基]-1,3-噻唑-2-基}哌啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮、(15.58)1H-咪唑-1-羧酸1-(4-甲氧基苯氧基)-3,3-二甲基丁烷-2-基酯、(15.59)2,3,5,6-四氯-4-(甲基磺醯基)吡啶、(15.60)2,3-二丁基-6-氯噻吩并[2,3-d]嘧啶-4(3H)-酮、(15.61)2,6-二甲基-1H,5H-[1,4]二硫并[2,3-c:5,6-c']二吡咯-1,3,5,7(2H,6H)-四酮、(15.62)2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]-1-(4-{4-[(5R)-5-苯基-4,5-二氫-1,2-唑-3-基]-1,3-噻唑
-2-基}哌啶-1-基)乙酮、(15.63)2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]-1-(4-{4-[(5S)-5-苯基-4,5-二氫-1,2-唑-3-基]-1,3-噻唑-2-基}哌啶-1-基)乙酮、(15.64)2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]-1-{4-[4-(5-苯基-4,5-二氫-1,2-唑-3-基)-1,3-噻唑-2-基]哌啶-1-基}乙酮、(15.65)2-丁氧基-6-碘-3-丙基-4H-色烯-4-酮、(15.66)2-氯-5-[2-氯-1-(2,6-二氟-4-甲氧基苯基)-4-甲基-1H-咪唑-5-基]吡啶、(15.67)2-苯基苯酚與鹽類、(15.68)3-(4,4,5-三氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉、(15.69)3,4,5-三氯吡啶-2,6-二甲腈、(15.70)3-氯-5-(4-氯苯基)-4-(2,6-二氟苯基)-6-甲基嗒、(15.71)4-(4-氯苯基)-5-(2,6-二氟苯基)-3,6-二甲基嗒、(15.72)5-胺基-1,3,4-噻二唑-2-硫醇、(15.73)5-氯-N'-苯基-N'-(丙-2-炔-1-基)噻吩-2-亞硫羧基醯肼、(15.74)5-氟-2-[(4-氟苯甲基)氧]嘧啶-4-胺、(15.75)5-氟-2-[(4-甲基苯甲基)氧]嘧啶-4-胺、(15.76)5-甲基-6-辛基[1,2,4]三唑并[1,5-a]嘧啶-7-胺、(15.77)(2Z)-3-胺基-2-氰基-3-苯基丙烯酸乙酯、(15.78)N'-(4-{[3-(4-氯苯甲基)-1,2,4-噻二唑-5-基]氧}-2,5-二甲基苯基)-N-乙基-N-甲基甲脒、(15.79)N-(4-氯苯甲基)-3-[3-甲氧基-4-(丙-2-炔-1-基氧)苯基]丙醯胺、(15.80)N-[(4-氯苯基)(氰基)甲基]-3-[3-甲氧基-4-(丙-2-炔-1-基氧)苯基]丙醯胺、(15.81)N-[(5-溴-3-氯吡啶-2-基)甲基]-2,4-二氯菸醯胺、(15.82)N-[1-(5-溴-3-氯吡啶-2-基)乙基]-2,4-二氯菸醯胺、(15.83)N-[1-(5-溴-3-氯吡啶-2-基)乙基]-2-氟-4-碘菸醯胺、(15.84)N-{(E)-[(環丙基甲氧基)亞胺基][6-(二氟甲氧基)-2,3-二氟苯基]甲基}-2-苯基乙醯胺、(15.85)N-{(Z)-[(環丙基甲氧基)亞胺基][6-(二氟甲氧基)-2,3-二氟苯基]甲基}-2-苯基乙醯胺、(15.86)N'-{4-[(3-第三丁基-4-氰基-1,2-噻唑-5-基)氧]-2-氯-5-甲基苯基}-N-乙基-N-甲基甲脒、(15.87)N-甲基-2-(1-{[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-N-(1,2,3,4-四氫萘-1-基)-1,3-噻唑-4-羧醯胺、(15.88)N-甲基-2-(1-{[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-
基)-N-[(1R)-1,2,3,4-四氫萘-1-基]-1,3-噻唑-4-羧醯胺、(15.89)N-甲基-2-(1-{[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-N-[(1S)-1,2,3,4-四氫萘-1-基]-1,3-噻唑-4-羧醯胺、(15.90){6-[({[(1-甲基-1H-四唑-5-基)(苯基)亞甲基]胺基}氧)甲基]吡啶-2-基}胺甲酸戊酯、(15.91)吩-1-羧酸、(15.92)喹啉-8-醇、(15.93)喹啉-8-醇硫酸酯(2:1)、(15.94){6-[({[(1-甲基-1H-四唑-5-基)(苯基)亞甲基]胺基}氧)甲基]吡啶-2-基}胺甲酸第三丁基酯、(15.95)1-甲基-3-(三氟甲基)-N-[2'-(三氟甲基)聯苯-2-基]-1H-吡唑-4-羧醯胺、(15.96)N-(4'-氯聯苯-2-基)-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.97)N-(2',4'-二氯聯苯-2-基)-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.98)3-(二氟甲基)-1-甲基-N-[4'-(三氟甲基)聯苯-2-基]-1H-吡唑-4-羧醯胺、(15.99)N-(2',5'-二氟聯苯-2-基)-1-甲基-3-(三氟甲基)-1H-吡唑-4-羧醯胺、(15.100)3-(二氟甲基)-1-甲基-N-[4'-(丙-1-炔-1-基)聯苯-2-基]-1H-吡唑-4-羧醯胺、(15.101)5-氟-1,3-二甲基-N-[4'-(丙-1-炔-1-基)聯苯-2-基]-1H-吡唑-4-羧醯胺、(15.102)2-氯-N-[4'-(丙-1-炔-1-基)聯苯-2-基]菸醯胺、(15.103)3-(二氟甲基)-N-[4'-(3,3-二甲基丁-1-炔-1-基)聯苯-2-基]-1-甲基-1H-吡唑-4-羧醯胺、(15.104)N-[4'-(3,3-二甲基丁-1-炔-1-基)聯苯-2-基]-5-氟-1,3-二甲基-1H-吡唑-4-羧醯胺、(15.105)3-(二氟甲基)-N-(4'-乙炔基聯苯-2-基)-1-甲基-1H-吡唑-4-羧醯胺、(15.106)N-(4'-乙炔基聯苯-2-基)-5-氟-1,3-二甲基-1H-吡唑-4-羧醯胺、(15.107)2-氯-N-(4'-乙炔基聯苯-2-基)菸醯胺、(15.108)2-氯-N-[4'-(3,3-二甲基丁-1-炔-1-基)聯苯-2-基]菸醯胺、(15.109)4-(二氟甲基)-2-甲基-N-[4'-(三氟甲基)聯苯-2-基]-1,3-噻唑-5-羧醯胺、(15.110)5-氟-N-[4'-(3-羥基-3-甲基丁-1-炔-1-基)聯苯-2-基]-1,3-二甲基-1H-吡唑-4-羧醯胺、(15.111)2-氯-N-[4'-(3-羥基-3-甲基丁-1-炔-1-基)聯苯-2-基]菸醯胺、(15.112)3-(二氟甲基)-N-[4'-(3-甲氧基-3-甲基丁-1-炔-1-基)聯苯-2-基]-1-甲基-1H-吡唑-4-羧醯
胺、(15.113)5-氟-N-[4'-(3-甲氧基-3-甲基丁-1-炔-1-基)聯苯-2-基]-1,3-二甲基-1H-吡唑-4-羧醯胺、(15.114)2-氯-N-[4'-(3-甲氧基-3-甲基丁-1-炔-1-基)聯苯-2-基]菸醯胺、(15.115)(5-溴-2-甲氧基-4-甲基吡啶-3-基)(2,3,4-三甲氧基-6-甲基苯基)甲酮、(15.116)N-[2-(4-{[3-(4-氯苯基)丙-2-炔-1-基]氧}-3-甲氧基苯基)乙基]-N2-(甲基磺醯基)纈醯胺、(15.117)4-側氧基-4-[(2-苯基乙基)胺基]丁酸、(15.118){6-[({[(Z)-(1-甲基-1H-四唑-5-基)(苯基)亞甲基]胺基}氧)甲基]吡啶-2-基}胺甲酸丁-3-炔-1-基酯、(15.119)4-胺基-5-氟嘧啶-2-醇(互變異構型:4-胺基-5-氟嘧啶-2(1H)-酮)、(15.120)3,4,5-三羥基苯甲酸丙酯、(15.121)1,3-二甲基-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-羧醯胺、(15.122)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-羧醯胺、(15.123)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-羧醯胺、(15.124)[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、(15.125)(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、(15.126)(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、(15.127)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、(15.128)硫代氰酸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-基酯、(15.129)5-(烯丙基氫硫基)-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、(15.130)2-[1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.131)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、(15.132)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、(15.133)硫代氰酸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-基酯、
(15.134)硫代氰酸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-基酯、(15.135)5-(烯丙基氫硫基)-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、(15.136)5-(烯丙基氫硫基)-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、(15.137)2-[(2S,4S,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.138)2-[(2R,4S,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.139)2-[(2R,4R,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.140)2-[(2S,4R,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.141)2-[(2S,4S,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.142)2-[(2R,4S,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.143)2-[(2R,4R,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.144)2-[(2S,4R,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.145)2-氟-6-(三氟甲基)-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)苯甲醯胺、(15.146)2-(6-苯甲基吡啶-2-基)喹唑啉、(15.147)2-[6-(3-氟-4-甲氧基苯基)-5-甲基吡啶-2-基]喹唑啉、(15.148)3-(4,4-二氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉、(15.149)脫落酸、(15.150)3-(二氟甲基)-N-甲氧基-1-甲基-N-[1-(2,4,6-三氯苯基)丙烷-2-基]-1H-吡唑-4-羧醯胺、(15.151)N'-[5-溴-6-(2,3-二氫-1H-茚-2-基氧)-2-甲基吡啶-3-基]-N-乙基-N-甲基甲脒、(15.152)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-甲基甲脒、(15.153)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-甲基甲脒、(15.154)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-甲基甲脒、(15.155)N'-{5-溴-6-[(順式-4-異丙基環己基)氧]-2-甲基吡啶-3-基}-N-乙基-N-甲基甲脒、(15.156)N'-{5-溴-6-[(反式-4-異丙基環己基)氧]-2-甲基吡啶-3-基}-N-乙基-N-甲基甲脒、(15.157)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基苯甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.158)N-環丙基-N-(2-環丙基苯甲基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.159)N-(2-第三丁基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.160)N-(5-氯-2-乙基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.161)N-(5-氯-2-異丙基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.162)N-環丙基-3-(二氟甲基)-N-(2-乙基-5-氟苯甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.163)N-環丙基-3-(二氟甲基)-5-氟-N-(5-氟-2-異丙基苯甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.164)N-環丙基-N-(2-環丙基-5-氟苯甲基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.165)N-(2-環戊基-5-氟苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.166)N-環丙基-3-(二氟甲基)-5-氟-N-(2-氟-6-異丙基苯甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.167)N-環丙基-3-(二氟甲基)-N-(2-乙基-5-甲基苯甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.168)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基-5-甲基苯甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.169)N-環丙基-N-(2-環丙基-5-甲基苯甲基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.170)N-(2-第三丁基-5-甲基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.171)N-[5-氯-2-(三氟甲基)苯甲基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.172)N-環丙基-3-(二氟甲基)-5-氟-1-甲基-N-[5-甲基-2-(三氟甲基)苯甲基]-1H-吡唑-4-羧醯胺、(15.173)
N-[2-氯-6-(三氟甲基)苯甲基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.174)N-[3-氯-2-氟-6-(三氟甲基)苯甲基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.175)N-環丙基-3-(二氟甲基)-N-(2-乙基-4,5-二甲基苯甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.176)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基苯甲基)-1-甲基-1H-吡唑-4-羧硫醯胺、(15.177)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-羧醯胺、(15.178)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-羧醯胺、(15.179)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-羧醯胺、(15.180)N'-(2,5-二甲基-4-苯氧基苯基)-N-乙基-N-甲基甲脒、(15.181)N'-{4-[(4,5-二氯-1,3-噻唑-2-基)氧]-2,5-二甲基苯基}-N-乙基-N-甲基甲脒、(15.182)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。所有第(1)至(15)類所述之混合組份依據其官能基而定,可視需要與合適酸或鹼形成鹽類。
式(I)、(Ia)、(Ib)或(Ic)化合物可與生物性除害蟲劑組合。
生物性除害蟲劑特定言之包括細菌、真菌、酵母、植物抽出物及微生物製品,包括蛋白質與二次代謝物。
生物性除害蟲劑包括細菌,如:形成孢子之細菌、定殖在根部之細菌及具有生物性殺昆蟲劑、殺真菌劑或殺線蟲劑作用之細菌。
此等可作為或用為生物性除害蟲劑之細菌實例為:液化澱粉芽孢桿菌(Bacillus amyloliquefaciens)菌株FZB42(DSM 231179),或仙人掌桿菌(Bacillus cereus),特定言之仙人掌桿菌(B.cereus)菌株CNCM I-1562或堅強芽胞桿菌(Bacillus firmus)菌株I-1582(登錄號CNCM 1-1582)或短小芽胞桿菌(Bacillus pumilus),特定言之菌株GB34(登錄號
ATCC 700814)與菌株QST2808(登錄號NRRL B-30087),或枯草桿菌(Bacillus subtilis),特定言之菌株GB03(登錄號ATCC SD-1397),或枯草桿菌(Bacillus subtilis)菌株QST713(登錄號NRRL B-21661)或枯草桿菌(Bacillus subtilis)菌株OST 30002(登錄號NRRL B-50421)、蘇雲金芽孢桿菌(Bacillus thuringiensis),特定言之蘇雲金芽胞桿菌以色列亞種(B.thuringiensis subspecies israelensis)(血清型H-14)、菌株AM65-52(登錄號ATCC 1276),或蘇雲金芽胞桿菌鮎澤亞種(B.thuringiensis subsp.aizawai),特定言之菌株ABTS-1857(SD-1372),或蘇雲金芽胞桿菌庫斯塔基亞種(B.thuringiensis subsp.kurstaki)菌株HD-1,或蘇雲金芽胞桿菌殺蟲亞種(B.thuringiensis subsp.tenebrionis)菌株NB 176(SD-5428)、穿刺巴斯德菌(Pasteuria penetrans)、巴斯德菌屬(Pasteuria spp.)(腎形腎狀線蟲(Rotylenchulus reniformis))-PR3(登錄號ATCC SD-5834)、細黃鏈黴菌(Streptomyces microflavus)菌株AQ6121(=QRD 31.013、NRRL B-50550)、鮮黃鏈黴菌(Streptomyces galbus)菌株AQ 6047(登錄號NRRL 30232)。
此等可作為或用為生物性除害蟲劑之真菌及酵母實例為:
巴氏蠶白僵菌(Beauveria bassiana),特定言之菌株ATCC 74040;微坦盾殼黴(Coniothyrium minitans),特定言之菌株CON/M/91-8(登錄號DSM-9660);輪枝菌屬(Lecanicillium spp.),特定言之菌株HRO LEC 12;蠟蚧輪枝菌(Lecanicillium lecanii)(過去稱為Verticillium lecanii),特定言之菌株KV01;黑殭菌(Metarhiziumr anisopliae),特定言之菌株F52(DSM3884/ATCC 90448);核果梅奇酵母(Metschnikowia fructicola),特定言之菌株NRRL Y-30752;玫煙色擬青霉(Paecilomyces fumosoroseus)(現在稱為:玫烟色棒束孢(Isaria fumosorosea)),特定言之菌株IFPC 200613,或菌株Apopka 97(登錄號ATCC 20874);淡紫色擬青霉(Paecilomyces lilacinus),特定言之淡紫色擬青霉(P. lilacinus)菌株251(AGAL 89/030550);大孢籃狀菌(Talaromyces flavus),特定言之菌株V117b;深綠木黴(Trichoderma atroviride),特定言之菌株SC1(登錄號CBS 122089);哈茨木黴(Trichoderma harzianum),特定言之哈茨木黴(T.harzianum rifai)T39(登錄號CNCM I-952)。
此等可作為或用為生物性除害蟲劑之病毒實例為:
棉褐帶卷蛾(Adoxophyes orana)顆粒體病毒(GV)、蘋果蠹蛾(Cydia pomonella)顆粒體病毒(GV)、番茄夜蛾(Helicoverpa armigera)(棉蛉蟲)核型多角體病毒(NPV)、甜菜夜蛾(Spodoptera exigua)mNPV、草地斜紋夜蛾(Spodoptera frugiperda)mNPV、棉貪夜蛾(Spodoptera littoralis)NPV。
亦包括以細菌與真菌作為'菌種'加至植物或植株部分或植物
器官中,並利用其特殊性質,促進植物生長與植物健康。可述及之實例為:土壤桿菌屬(Agrobacterium spp.)、甘藍固氮根瘤菌(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.)(特定言之洋蔥伯克氏菌(Burkholderia cepacia)(過去稱為洋蔥假單胞菌(Pseudomonas cepacia)))、巨孢球囊黴屬(Gigaspora spp.)或單孢巨孢球囊黴(Gigaspora monosporum)、菌根菌屬(Glomus spp.)、蠟蘑菌屬(Laccaria spp.)、布氏乳桿菌(Lactobacillus buchneri)、類球囊黴屬(Paraglomus spp.)、豆包菌(Pisolithus tinctorus)、假單胞菌屬(Pseudomonas spp.)、根瘤菌屬(Rhizobium spp.)(特定言之三葉草根瘤菌(Rhizobium trifolii))、松露屬(Rhizopogon spp.)、硬皮馬勃菌屬(Scleroderma spp.)、乳牛肝菌屬(Suillus spp.)、鏈黴菌屬(Streptomyces spp.)。
可作為或用為生物性除害蟲劑之植物抽出物及由微生物
形成之產物(包括蛋白質與二次代謝物)實例為:
大蒜(Allium sativum)、中亞苦蒿(Artemisia absinthium)、印楝素(azadirachtin)、Biokeeper WP、肉桂(Cassia nigricans)、苦皮藤(Celastrus angulatus)、臭杏(Chenopodium anthelminticum)、幾丁質、Armour-Zen、歐洲鱗毛蕨(Dryopteris filix-mas)、問荊草(Equisetum arvense)、Fortune Aza、Fungastop、Heads Up(藜麥(Chenopodium quinoa)皂苷抽出物)、除蟲菊/除蟲菊酯、苦木(Quassia amara)、櫟屬(Quercus)、皂樹(Quillaja)、虎杖抽出物(Regalia)、"RequiemTM Insecticide"、魚藤酮、魚尼丁(ryania)/雷諾丁(ryanodine)、聚合草(Symphytum officinale)、菊蒿(Tanacetum vulgare)、百里酚、Triact 70、TriCon、金蓮花(Tropaeulum majus)、大蕁麻(Urtica dioica)、藜蘆鹼(Veratrin)、槲寄生(Viscum album)、十字花科抽出物,特定言之油菜籽粉或芥末粉。
式(I)、(Ia)、(Ib)或(Ic)化合物可與安全劑組合,如,例如:解草酮(benoxacor)、解毒喹(cloquintocet(-mexyl))、解草胺腈(cyometrinil)、環丙磺草胺(cyprosulfamide)、二氯丙烯胺(dichlormid)、解草唑(fenchlorazole)(-ethyl)、解草啶(fenclorim)、解草安(flurazole)、氟草肟(fluxofenim)、解草唑(furilazole)、雙苯唑酸(isoxadifen(-ethyl))、吡唑解草酯(mefenpyr(-diethyl))、萘甲酸酐、解草腈(oxabetrinil)、2-甲氧基-N-({4-[(甲基胺甲醯基)胺基]苯基}磺醯基)苯甲醯胺(CAS 129531-12-0)、4-(二氯乙醯基)-1-氧雜-4-氮雜螺[4.5]癸烷(CAS 71526-07-3)、2,2,5-三甲基-3-(二氯乙醯基)-1,3-唑啶(CAS 52836-31-4)。
所有植物與植株部份均可根據本發明處理。此時,咸瞭解植物係指所有植物及植株部份,如:需要及不需要之野生植物或作物(包括天然作物),例如:穀類(小麥、稻、硬粒小麥、大麥、裸麥、燕麥)、玉米、
大豆、馬鈴薯、甜菜、甘蔗、番茄、豆與其他蔬菜類、棉花、菸草、油菜、與果實植物(蘋果、梨、柑橘類果實與葡萄)。作物可為得自依傳統育種法與最適化方法或利用生物技術與遺傳工程法或此等方法之組合所取得者,包括轉殖基因植物,及包括受植物育種者權益保護或未受保護之植物栽培品種。咸瞭解,植株部份意指植物之所有地上及地下部份與器官,如:芽、葉、花與根,其實例可述及:闊葉、針葉、莖、樹幹、花、果實體、果實、種子,及球莖、根與根莖。植株部份亦包括收成之植物,與無性及有性繁殖材料,例如:扦插、球莖、根莖、插枝與種子。
根據本發明使用式(I)、(Ia)、(Ib)或(Ic)化合物處理植物與植
株部份之方法係依習用之處理法直接處理或使化合物作用在其周圍、環境或庫存空間,例如:浸泡、噴灑、蒸發、霧化、撒播、塗刷、注射,且若處理繁殖材料時,特定言之處理種子時,亦可施加一層或多層包衣。
如上述,根據本發明亦可處理所有植物與其部份植株。較佳
具體實施例中係處理野生植物品種與植物栽培品種或彼等由傳統生物育種法(如:交配法或原生質融合法)取得者,與其部份植株。另一項較佳具體實施例中,係處理由遺傳工程方法(若適當時,可併用傳統方法)得到之轉殖基因植物與植物栽培品種(基因改造生物),及其部份植株。術語"部份"或"植株部份"或"部份植株"已如上述說明。特別佳者,本發明係處理自商品取得或使用中之植物栽培品種之植物。咸瞭解,植物栽培品種意指經由傳統育種法、誘變法或重組DNA技術得到之具有新穎性質("性狀")之植物。其可為生物型或基因型栽培品種、變異種。
根據本發明處理之較佳轉殖基因植物或植物栽培品種(彼等由遺傳工程取得者)包括所有透過基因改造過程,接受賦與特別有利性質(”
性狀”)之遺傳物質之植物。此等性質實例為改善植物生長、提高對高溫或低溫之耐受性、提高對乾旱或對水含量或土壤鹽含量之耐受性、提高開花率、簡化收成、加速成熟、提高收成量、提高所收成產品之品質與/或提高營養價值、更佳儲存壽命與/或提高所收成產品之可加工性。其他及特別強調之此等性質實例為植物對抗動物害蟲與有害微生物之更佳防禦性,如:由例如:植物內所形成之毒素,特定言之由來自蘇雲金芽孢桿菌(Bacillus thuringiensis)之遺傳物質(例如:基因CryIA(a)、CryIA(b)、CryIA(c)、CryIIA、CryIIIA、CryIIIB2、Cry9c Cry2Ab、Cry3Bb與CryIF及其組合)於植物中產生之毒素來對抗昆蟲、蜘蛛、線蟲、蟎類、蛞蝓與蝸牛,進一步利用例如:後天取得之全株抗性(SAR)、系統素(systemin)、植物抗毒素(phytoalexins)、誘發素(elicitors)與抗性基因,及相應表現之蛋白質與毒素,提高植物對抗植物病原性真菌、細菌與/或病毒之抗性,亦提高植物對某些除草活性化合物,例如:咪唑啉酮類、磺醯脲類、嘉磷塞(glyphosate)或草銨膦(phosphonotricin)之耐受性(例如:"PAT"基因)。此等賦與所需性狀之基因亦可相互組合進入轉殖基因植物中。可述及之轉殖基因植物實例為重要作物,如:穀類(小麥、稻、硬粒小麥、大麥、裸麥、燕麥)、玉米、大豆、馬鈴薯、甜菜、甘蔗、番茄、豌豆及其他蔬菜品種、棉花、菸草、油菜與果實植物(生產蘋果、梨、柑橘類水果與葡萄),特別著重於玉米、大豆、小麥、稻、馬鈴薯、棉花、甘蔗、番茄與油菜。特別強調之性狀為提高植物對抗昆蟲、蜘蛛、線蟲、蛞蝓與蝸牛之抗性。
使用式(I)、(Ia)、(Ib)或(Ic)化合物處理植物與植株部份之方法係依習用之處理法直接處理或使化合物作用在其周圍、棲息地或庫存空間,例如:浸泡、噴灑、噴霧、灌注、蒸發、撒粉、霧化、撒播、起泡、
塗刷、散播、注射、澆水(澆淋)、滴灌,若處理繁殖材料時,特定言之處理種子時,可進一步為供乾式處理種子之粉末、濕式處理種子之溶液、漿式處理種子之水溶性粉末、包殼、塗佈一層或多層包衣,等等。亦可進一步採用超低體積法施用式(I)、(Ia)、(Ib)或(Ic)化合物或取施用型式或式(I)、(Ia)、(Ib)或(Ic)化合物本身注射至土壤中。
植物之較佳直接處理法為葉部施用法,亦即讓式(I)、(Ia)、
(Ib)或(Ic)化合物施用在葉部,其中處理頻率及施用率應配合所針對害蟲之感染程度來調整。
若為全株作用性活性化合物時,式(I)、(Ia)、(Ib)或(Ic)化合
物亦可經由根系到達植物。因此可藉由式(I)、(Ia)、(Ib)或(Ic)化合物對植物所在地之作用來處理植物。其作法可為例如:浸泡或混合至土壤或營養液中,亦即在植物所在地(例如:土壤或水耕系統)浸入液體型式之式(I)、(Ia)、(Ib)或(Ic)化合物,或藉由土壤施用法,亦即將根據本發明式(I)、(Ia)、(Ib)或(Ic)化合物以固體型式(例如:呈粒劑型式)加至植物所在地。若為水稻作物時,其作法為量取式(I)、(Ia)、(Ib)或(Ic)化合物固體施用型式(例如:粒劑)加至水稻田中。
長久以來已知藉由處理植物種子來控制動物害蟲且仍在改良中。然而,處理種子時,經常出現一些無法以令人滿意之方式解決之問題。因此需要發展一種保護種子及發芽植物之方法,其可以在儲存期間、播種後或植物發芽後免除或至少顯著減少另外施用除害蟲劑。亦需要使活性化合物以最適當用量提供種子及發芽植物最佳保護程度,以免動物害蟲侵害,且不受所使用活性化合物傷害植物本身。特定言之,處理種子之方法亦應考量可抵抗或耐受害蟲之轉殖基因植物固有之殺昆蟲或殺線蟲性質,
以便在最低之除害蟲劑用量下,對種子及發芽植物達最佳保護程度。
特定言之,本發明因此亦有關使用一種式(I)、(Ia)、(Ib)或(Ic)化合物處理種子,以保護種子與發芽植物免於害蟲侵害之方法。根據本發明保護種子與發芽植物免於害蟲侵害之方法亦包括以式(I)、(Ia)、(Ib)或(Ic)化合物與混合組份在一次操作中同時處理或依序處理之方法。亦包括以式(I)、(Ia)、(Ib)或(Ic)化合物與混合組份在不同時間處理種子之方法。
本發明同樣係有關一種以式(I)、(Ia)、(Ib)或(Ic)化合物於處理種子上之用途,以保護種子與發芽植物免於動物害蟲侵害。
此外,本發明係有關一種已經過根據本發明式(I)、(Ia)、(Ib)或(Ic)化合物處理之種子,以保護免於動物害蟲侵害。本發明亦係有關一種經過式(I)、(Ia)、(Ib)或(Ic)化合物與混合對象同時處理之種子。本發明亦有關一種經過式(I)、(Ia)、(Ib)或(Ic)化合物與混合對象在不同時間點處理之種子。若為經過式(I)、(Ia)、(Ib)或(Ic)化合物與混合對象在不同時間點處理之種子時,本發明組成物中之個別物質可存在於種子之不同覆層中。此時,包含式(I)、(Ia)、(Ib)或(Ic)化合物與混合對象之覆層可視需要利用中間層分隔。本發明亦係有關一種已經過式(I)、(Ia)、(Ib)或(Ic)化合物與混合對象作為包衣組份或作為包衣以外之另一層或多層塗覆之種子。
此外,本發明係有關一種種子,其在經過式(I)、(Ia)、(Ib)或(Ic)化合物處理後,再經過包膜衣製程,以防止種子被塵粉磨損。
式(I)、(Ia)、(Ib)或(Ic)之全株作用性化合物之優點之一在於經過此等處理之種子不僅可保護種子本身,而且可保護種子出土後所長成植株,免於動物害蟲侵害。依此方式,即不需要在播種期間或播種後短時間內立即處理作物。
另一項優點在於透過式(I)、(Ia)、(Ib)或(Ic)化合物處理種子
後,可促進該經過處理之種子發芽及出土。
同樣可視為優點之處在於式(I)、(Ia)、(Ib)或(Ic)化合物亦可特別用於轉殖基因種子。
此外,式(I)、(Ia)、(Ib)或(Ic)化合物亦可與訊號轉導技術組成物或化合物組合使用,結果可以例如:改善與共生菌(例如:根瘤菌、菌根菌與/或內生細菌)之定殖,及/或達最佳固氮作用。
式(I)、(Ia)、(Ib)或(Ic)化合物適合保護任何用於農業、溫室、森林或園藝之植物品種之種子。更特定言之,該等種子係指穀類(如:小麥、大麥、裸麥、燕麥與小米)、玉米、棉花、大豆、稻、馬鈴薯、葵花、咖啡、菸草、芥花、油菜、甜菜(例如:製糖用甜菜與飼料用甜菜)、花生、蔬菜(如:番茄、胡瓜、豆、十字花科蔬菜、洋蔥與萵苣)、果實植物、草皮與觀賞植物之種子。特別重要為處理穀類(如:小麥、大麥、裸麥與燕麥)、玉米、大豆、棉花、芥花、油菜與稻之種子。
亦如上述,式(I)、(Ia)、(Ib)或(Ic)化合物對轉殖基因種子之處理法亦特別重要。此時該植物種子之形式通常包含至少一種可以控制特定言之具有殺昆蟲性質與/或殺線蟲性質之多肽表現之異源基因。該轉殖基因種子中之此等異源基因可源自下列微生物屬種,如:芽胞桿菌(Bacillus)、根瘤菌(Rhizobium)、假單胞菌(Pseudomonas)、沙雷氏菌(Serratia)、木黴(Trichoderma)、棒形桿菌(Clavibacter)、菌根菌(Glomus)或黏帚黴(Gliocladium)。本發明特別適合處理包含至少一種來自芽胞桿菌屬(Bacillus sp.)之異源基因之轉殖基因種子。特別佳為該異源基因係來自蘇雲金芽胞桿菌(Bacillus thuringiensis)。
本發明內容中,式(I)、(Ia)、(Ib)或(Ic)化合物係施用至種子上。接受處理之種子最好處於充份穩定狀態,以免在處理期間損傷。通常,
可在收穫至播種期間任何時間點處理種子。所採用之種子通常已與植株分離且已脫除軸、殼、稈、包衣、穗或果肉。因此例如:可採用已經過採收、清潔且乾燥至可以儲存之水份含量之種子。或者亦可使用乾燥後再例如:經過水處理後再度乾燥之種子,例如:底層處理。
當處理種子時,通常必需小心選擇施用至種子之式(I)、(Ia)、(Ib)或(Ic)化合物與/或其他添加劑之施用量,以免破壞種子發芽且/或不會傷害由該種子長成之植物。尤其當活性成份在特定施用率下可能具有植物毒性時,必需確保此點。
通常,式(I)、(Ia)、(Ib)或(Ic)化合物係呈合適調配物施用至種子上。處理種子之合適調配物與方法係習此相關技藝之人士習知者。
式(I)、(Ia)、(Ib)或(Ic)化合物可轉換成常用拌種調配物,如:溶液、乳液、懸浮液、粉劑、發泡劑、漿物或種子之其他包衣組成物,與ULV調配物。
此等調配物可依已知方式製造,混合式(I)、(Ia)、(Ib)或(Ic)化合物與常用之添加劑,如,例如:常用之補充劑,及溶劑或稀釋劑、著色劑、濕化劑、勻散劑、乳化劑、消泡劑、防腐劑、二次增稠劑、膠黏劑、赤霉素,及水。
根據本發明可使用之拌種調配物中可包含之著色劑為此等目的常用之所有著色劑。此時,不僅可使用水溶解度低之色素,亦可使用水溶性染劑。可述及之實例包括彼等已知名稱為若丹明B(Rhodamin B)、C.I.紅色(Pigment Red)112號與C.I.溶劑紅(Solvent Red)1號之染劑。
根據本發明可使用之拌種調配物中可包含之濕化劑為可促進濕化及調配農化活性成份時常用之所有物質。較佳為使用萘磺酸烷基酯類,如:萘磺酸二異丙基酯或-二異丁基酯。
根據本發明可使用之拌種調配物中適用之勻散劑與/或乳化
劑為調配農化活性成份時常用之所有非離子性、陰離子性與陽離子性勻散劑。較佳為使用非離子性或陰離子性勻散劑或非離子性或陰離子性勻散劑之混合物。合適之非離子性勻散劑尤其包括環氧乙烷/氧化丙烯嵌段聚合物、烷基苯酚聚二醇醚與三苯乙烯苯酚聚二醇醚,及其磷酸化或硫酸化衍生物。
合適之陰離子性勻散劑尤其指木質素磺酸鹽、聚丙烯酸鹽與芳基磺酸鹽/甲醛縮合物。
根據本發明可使用之拌種調配物中可包含之消泡劑為調配
農化活性成份時常用之所有抑制泡沫物質。較佳為使用聚矽氧消泡劑與硬脂酸鎂。
根據本發明可使用之拌種調配物中可包含之防腐劑為農化
組成物中為了此等目的常用之所有物質。其實例包括二氯吩(dichlorophen)與苯甲醇半縮甲醛。
根據本發明可使用之拌種調配物中可包含之二次增稠劑為
農化組成物中為了此等目的常用之所有物質。較佳為纖維素衍生物、丙烯酸衍生物、黃原膠、改質黏土與高分散性矽石。
根據本發明可使用之拌種調配物中可包含之膠黏劑為拌種
產品中所有常用之結合劑。較佳者可述及聚乙烯基吡咯啶酮、聚乙酸乙烯酯、聚乙烯醇,與纖基乙酸鈉(tylose)。
根據本發明可使用之拌種調配物中可包含之赤霉素較佳為
赤霉素A1、A3(=赤霉酸)、A4與A7;以使用赤霉酸特別佳。該赤霉素係已知者(參見R.Wegler“作物保護劑與農藥之化學(Chemie der Pflanzenschutz-und Schädlingsbekämpfungsmittel)”,Vol.2,Springer Verlag,1970,pp.401-412)。
根據本發明可使用之拌種調配物可直接使用或加水稀釋後
使用,用於處理各種不同種子。例如:該濃縮劑或其加水稀釋後所得之製劑可用於包覆穀類(如:小麥、大麥、裸麥、燕麥與硬粒小麥)之種子,及玉米、稻、油菜、豌豆、豆類、棉花、葵花、大豆及甜菜之種子,或任何各種不同蔬菜之種子。可根據本發明使用之拌種調配物或其稀釋之施用型式亦可用於包覆轉殖基因植物之種子。
根據本發明可使用之拌種調配物或其加水後所製成施用型
式用於處理種子時,可使用所有常用於拌種之合適混合裝置。更明確言之,進行該拌種過程時,將種子置入混合機中,依分批或連續方式,添加所需拌種調配物特定用量,可直接添加或先加水稀釋後添加,混合所有內容物,直到調配物均勻分佈在種子上為止。若適當時可接著進行乾燥過程。
根據本發明可使用之拌種調配物之施用率可在相當大範圍
內變化。其依據調配物中式(I)、(Ia)、(Ib)或(Ic)化合物之特定含量及依據種子而變化。各式(I)、(Ia)、(Ib)或(Ic)化合物之施用率通常在每公斤種子0.001至50克之間,較佳為每公斤種子0.01至15克之間。
在動物健康方面(亦即獸醫學領域),式(I)、(Ia)、(Ib)或(Ic)化合物可活性對抗動物寄生蟲,特定言之體外寄生蟲或體內寄生蟲。術語"體內寄生蟲"尤其包括蠕蟲與原蟲,如:球蟲目(Coccidia)。體外寄生蟲通常且較佳為節肢動物,特定言之昆蟲與蜱蟎類。
在獸醫學領域中,對恆溫動物具有有利毒性之式(I)、(Ia)、(Ib)或(Ic)化合物適合在畜牧、養殖業、動物園、實驗室、實驗與家畜動物中控制出現在動物養殖及動物畜養中之寄生蟲。其可活性對抗寄生蟲之所有或特定發展階段。
農業牲畜包括例如:哺乳動物,如:綿羊、山羊、馬、驢、駱駝、水牛、兔子、馴鹿、黇鹿及尤指牛與豬,或禽類,如:火雞、鴨、鵝,及尤指雞;魚類或甲殼類,例如:水產養殖,及昆蟲,如:蜜蜂。
家畜動物包括例如:哺乳動物,如:倉鼠、天竺鼠,大鼠、小鼠、栗鼠、雪貂,及特定言之狗、貓、籠內的鳥、爬蟲類、兩棲類或水族箱內的魚。
根據較佳具體實施例,式(I)、(Ia)、(Ib)或(Ic)化合物係投與哺乳動物。
根據另一項較佳具體實施例,式(I)、(Ia)、(Ib)或(Ic)化合物係投與鳥類,亦即籠內的鳥,且尤指禽類。
使用式(I)、(Ia)、(Ib)或(Ic)化合物控制動物寄生蟲,係計畫降低或防止生病、死亡例及下降之效能(指肉品、乳品、毛、皮、蛋、蜂蜜,等等),因此可以達到更經濟及更簡單之動物管理及更佳之動物效益。
在動物健康之相關領域中,術語"控制"或"防治"係指式(I)、(Ia)、(Ib)或(Ic)化合物可有效降低各寄生蟲在感染此等寄生蟲之動物中之發病率,使此等寄生蟲降至無害程度。更明確言之,本文所採用之"控制"係指式(I)、(Ia)、(Ib)或(Ic)化合物可以有效殺死各寄生蟲、抑制其生長或抑制其繁殖。
節胺動物包括:蝨目(Anoplurida),例如:盲蝨屬(Haematopinus spp.)、長顎蝨屬(Linognathus spp.)、蝨蟎屬(Pediculus spp.)、陰蝨屬(Phtirus spp.)、管蝨屬(Solenopotes spp.);食毛目(Mallophagida)及鈍角亞目(Amblycerina)與細角亞目(Ischnocerina),例如:毛鳥蝨屬(Trimenopon spp.)、雞蝨屬(Menopon spp.)、巨毛蝨屬(Trinoton spp.)、羽蝨屬(Bovicola spp.)、嚼蝨屬(Werneckiella spp.)、
毛虱屬(Lepikentron spp.)、食蟲虻屬(Damalina spp.)、獸鳥蝨屬(Trichodectes spp.)、貓羽蝨屬(Felicola spp.);雙翅目(Diptera)及長角亞目(Nematocerina)與短角亞目(Brachycerina),例如:伊蚊屬(Aedes spp.)、按蚊屬(Anopheles spp.)、庫蚊屬(Culex spp.)、蚋蚊屬(Simulium spp.)、真蚋屬(Eusimulium spp.)、白蛉屬(Phlebotomus spp.)、沙蠅屬(Lutzomyia spp.)、蚊屬(Culicoides spp.)、斑虻屬(Chrysops spp.)、蚋屬(Odagmia spp.)、維蚋屬(Wilhelmia spp.)、瘤虻屬(Hybomitra spp.)、黃虻屬(Atylotus spp.)、虻屬(Tabanus spp.)、麻翅虻屬(Haematopota spp.)、Philipomyia屬、蜂虱屬(Braula spp.)、家蠅屬(Musca spp.)、齒股蠅屬(Hydrotaea spp.)、螫蠅屬(Stomoxys spp.)、血蠅屬(Haematobia spp.)、莫蠅屬(Morellia spp.)、廄蠅屬(Fannia spp.)、舌蠅屬(Glossina spp.)、麗蠅屬(Calliphora spp.)、綠蠅屬(Lucilia spp.)、金蠅屬(Chrysomyia spp.)、肉蠅屬(Wohlfahrtia spp.)、麻蠅屬(Sarcophaga spp.)、狂蠅屬(Oestrus spp.)、皮蠅屬(Hypoderma spp.)、胃蠅屬(Gasterophilus spp.)、蝨蠅屬(Hippobosca spp.)、蝨蠅屬(Lipoptena spp.)、羊蝨蠅屬(Melophagus spp.)、鼻狂蠅屬(Rhinoestrus spp.)、大蚊屬(Tipula spp.);蚤目(Siphonapterida),例如:蚤屬(Pulex spp.)、櫛頭蚤屬(Ctenocephalides spp.)、潛蚤屬(Tunga spp.)、鼠蚤屬(Xenopsylla spp.)、角葉蚤屬(Ceratophyllus spp.);異翅目(Heteropterida),例如:臭蟲屬(Cimex spp.)、錐蝽屬(Triatoma spp.)、紅腹獵蝽屬(Rhodnius spp.)、金圓蝽屬(Panstrongylus spp.);及蜚蠊目(Blattaria)之擾人及衛生害蟲。
節胺動物進一步包括:蜱蟲(Acari)之亞綱(蜱蟎亞綱(Acarina))及後氣亞目(Metastigmata),例如:軟蜱科(Argasidae),如:銳緣蜱屬(Argas spp.)、鈍緣蜱屬(Ornithodorus spp.)、殘緣蜱屬(Otobius spp.);硬蜱科(Ixodidae),如:硬蜱屬(Ixodes spp.)、花蜱
屬(Amblyomma spp.)、扇頭蜱(Rhipicephalus(牛蜱(Boophilus))屬、革蜱屬(Dermacentor spp.)、血蜱屬(Haemophysalis spp.)、璃眼蜱屬(Hyalomma spp.)、扇頭蜱屬(Rhipicephalus spp.)(多重宿主蜱之原始屬種);中氣亞目(Mesostigmata),如:刺皮蟎屬(Dermanyssus spp.)、禽刺蟎屬(Ornithonyssus spp.)、肺刺蟎屬(Pneumonyssus spp.)、耳蟎屬(Raillietia spp.)、肺刺蟎屬(Pneumonyssus spp.)、胸孔蟎屬(Sternostoma spp.)、瓦蟎屬(Varroa spp.)、蜂蟎屬(Acarapis spp.);光芒蟲亞目(Actinedida)(前氣亞目(Prostigmata)),例如:蜂蟎屬(Acarapis spp.)、姬蟄蟎屬(Cheyletiella spp.)、禽螫蟎屬(Ornithocheyletia spp.)、肉蟎屬(Myobia spp.)、綿羊疥蟎(Psorergates spp.)、脂蟎屬(Demodex spp.)、恙蟎屬(Trombicula spp.)、新恙蟎屬(Neotrombicula spp.)、螫蟎屬(Listrophorus spp.);及粉蟎亞目(Acaridida)(無氣亞目(Astigmata)),例如:粉蟎屬(Acarus spp.)、食酪蟎屬(Tyrophagus spp.)、嗜木蟎屬(Caloglyphus spp.)、皮頸下蟎屬(Hypodectes spp.)、翼衣屬(Pterolichus spp.)、癢蟎屬(Psoroptes spp.)、皮蟎屬(Chorioptes spp.)、耳蟎屬(Otodectes spp.)、疥蟎屬(Sarcoptes spp.)、耳蟎屬(Notoedres spp.)、鳥疥蟎屬(Knemidocoptes spp.)、雞蟎屬(Cytodites spp.)、雞雛蟎屬(Laminosioptes spp.)。
寄生性原蟲實例包括:鞭毛門(Mastigophora)(鞭毛動物綱(Flagellata)),如,例如:錐蟲科(Trypanosomatidae),例如:布氏錐蟲(Trypanosoma b.brucei)、布氏剛比亞錐蟲(T.b.gambiense)、布氏羅德西亞錐蟲(T.b.rhodesiense)、剛果錐蟲(T.congolense)、克氏錐蟲(T.cruzi)、伊氏錐蟲(T.evansi)、馬錐蟲(T.equinum)、路易氏錐蟲(T.lewisi)、鱸魚錐蟲(T.percae)、猿猴錐蟲(T.simiae)、活動錐蟲(T.vivax)、巴西利什曼原蟲(Leishmania brasiliensis)、杜氏利什曼原蟲(L.
donovani)、熱帶利什曼原蟲(L.tropica),如,例如:毛滴蟲科(Trichomonadidae),例如:藍氏賈第鞭毛蟲(Giardia lamblia)、犬賈第鞭毛蟲(G.canis)肉質鞭毛蟲門(Sarcomastigophora))(根足蟲綱(Rhizopoda)),如:內阿米巴科(Entamoebidae),例如:溶組織內阿米巴(Entamoeba histolytica)、哈曼原蟲(Hartmanellidae),例如:棘阿米巴屬(Acanthamoeba sp.)、哈曼原蟲屬(Harmanella sp.)
頂複合器門(Apicomplexa)(孢子蟲綱(Sporozoa)),如:艾美球蟲科(Eimeridae),例如:雞球蟲(Eimeria acervulina)、腺樣艾美球蟲(E.adenoides)、阿拉巴艾美爾球蟲(E.alabamensis)、鴨艾美耳球蟲(E.anatis)、鵝艾美球蟲(E.anseris)、阿氏艾美球蟲(E.arloingi)、阿洛尼氏艾美球蟲(E.ashata)、奧本艾美球蟲(E.auburnensis)、牛艾美球蟲(E.bovis)、波氏艾美球蟲(E.brunetti)、犬艾美球蟲(E.canis)、栗鼠艾美球蟲(E.chinchillae)、鯡魚艾美球蟲(E.clupearum)、鴿艾美球蟲(E.columbae)、扭轉艾美球蟲(E.contoita)、槌狀艾美球蟲(E.crandalis)、狄氏艾美球蟲(E.debliecki)、分散艾美球蟲(E.dispersa)、橢圓艾美球蟲(E.ellipsoidales)、鐮形艾美球蟲(E.falciformis)、福氏艾美球蟲(E.faurei)、黃色艾美球蟲(E.flavescens)、加洛帕沃尼艾美球蟲(E.gallopavonis)、哈氏艾美球蟲(E.hagani)、腸艾美球蟲(E.intestinalis)、易洛魁艾美球虫(E.iroquoina)、伊氏艾美球虫(E.irresidua)、拉本艾美球虫(E.labbeana)、留氏艾美球蟲(E.leucarti)、大型艾美球蟲(E.magna)、巨型艾美球蟲(E.maxima)、中型艾美球蟲(E.media)、火雞艾美球蟲(E.meleagridis)、火雞和緩艾美球蟲(E.meleagrimitis)、和緩艾美球蟲(E.mitis)、毒害艾美球蟲(E.necatrix)、雅氏艾美球蟲(E.ninakohlyakimovae)、羊艾美球蟲(E.ovis)、小型艾美球蟲(E.parva)、孔雀艾美球蟲(E.pavonis)、穿孔艾美球蟲(E.perforans)、法森艾美球蟲(E.phasani)、梨形艾美球蟲(E.piriformis)、早熟艾美球蟲(E.praecox)、
艾美球蟲(E.residua)、粗糙艾美球蟲(E.scabra)、艾美球蟲屬(E.spec.)、斯氏艾美球蟲(E.stiedai)、豬艾美球蟲(E.suis)、柔嫩艾美球蟲(E.tenella)、樹艾美球蟲(E.truncata)、特魯特艾美球蟲(E.truttae)、朱氏艾美球蟲(E.zuernii)、球蟲屬(Globidium spec.)、貝氏等孢球蟲(Isospora belli)、犬等孢球蟲(I.canis)、貓等孢球蟲(I.felis)、俄亥俄等孢球蟲(I.ohioensis)、芮氏等孢球蟲(I.rivolta)、等孢球蟲屬(I.spec.)、豬等孢球蟲(I.suis)、囊等孢球蟲屬(Cystisospora spec.)、隱孢子蟲屬(Cryptosporidium spec.),特定言之小隱孢子蟲(C.parvum);如:弓形蟲科(Toxoplasmadidae),例如:鼠弓形蟲(Toxoplasma gondii)、哈芒球蟲(Hammondia heydornii)、犬新孢子蟲(Neospora caninum)、貝內特貝斯諾孢子蟲(Besnoitia besnoitii);如:肉孢子蟲科(Sarcocystidae),例如:牛犬肉孢子蟲(Sarcocystis bovicanis)、牛人肉孢子蟲(S.bovihominis)、羊犬肉孢子蟲(S.ovicanis)、羊貓肉孢子蟲(S.ovifelis)、神經肉孢子蟲(S.neurona)、肉孢子蟲屬(S.spec.)、豬人肉孢子蟲(S.suihominis);如:白細胞蟲科(Leucozoidae),例如:西氏住白細胞蟲(Leucozytozoon simondi);如:瘧原蟲科(Plasmodiidae),例如:柏格氏鼠瘧原蟲(Plasmodium berghei)、惡性瘧原蟲(P.falciparum)、三日瘧原蟲(P.malariae)、卵形瘧原蟲(P.ovale)、間日瘧原蟲(P.vivax)、瘧蟲屬(P.spec.);如:焦蟲目(Piroplasmea),例如:阿根廷巴貝蟲(Babesia argentina)、牛巴貝蟲(B.bovis)、犬巴貝蟲(B.canis)、巴貝蟲屬(B.spec.)、小泰勒蟲(Theileria parva)、泰勒蟲屬(Theileria spec.);如:匿蟲亞目(Adeleina),例如:犬肝簇蟲(Hepatozoon canis)、肝簇蟲屬(H.spec.)。
病原性體內寄生蟲為蠕蟲,包括:扁形動物門(Platyhelmintha)(例如:單殖吸蟲、絛蟲及吸蟲)、線蟲、棘頭動物與舌形動物,包括:單殖吸蟲亞綱(Monogenea):例如:三代蟲屬(Gyrodactylus spp.)、指標蟲屬
(Dactylogyrus spp.)、多盤吸蟲屬(Polystoma spp.);絛蟲:擬葉目(Pseudophyllidea),例如:廣節裂頭絛蟲屬(Diphyllobothrium spp.)、螺旋體蟲屬(Spirometra spp.)、裂頭絛蟲(Schistocephalus spp.)、舌狀絛蟲屬(Ligula spp.)、吸葉絛蟲屬(Bothridium spp.)、大複殖門絛蟲屬(Diphlogonoporus spp.);圓葉目(Cyclophyllidea),例如:中殖孔屬絛蟲屬(Mesocestoides spp.)、裸頭絛蟲屬(Anoplocephala spp.)、副裸頭絛蟲屬(Paranoplocephala spp.)、莫尼茨絛蟲屬(Moniezia spp.)、隧體絛蟲屬(Thysanosoma spp.)、曲子官絛蟲屬(Thysaniezia spp.)、無卵黃腺絛蟲(Avitellina spp.)、史提拉絛蟲屬(Stilesia spp.)、錫帶絛蟲屬(Cittotaenia spp.)、安迪亞絛蟲屬(Andyra spp.)、伯特絛蟲屬(Bertiella spp.)、帶絛蟲屬(Taenia spp.)、棘球絛蟲屬(Echinococcus spp.)、泡尾絛蟲屬(Hydatigera spp.)、戴文絛蟲屬(Davainea spp.)、雷氏絛蟲屬(Raillietina spp.)、包膜絛蟲屬(Hymenolepis spp.)、瘍棘殼絛蟲屬(Echinolepis spp.)、棘葉絛蟲屬(Echinocotyle spp.)、迪克氏絛蟲屬(Diochis spp.)、瓜實絛蟲屬(Dipylidium spp.)、約優克斯絛蟲屬(Joyeuxiella spp.)、雙孔絛蟲屬(Diplopylidium spp.);吸蟲:複殖綱(Digenea),例如:複口吸蟲屬(Diplostomum spp.)、莖雙穴吸蟲屬(Posthodiplostomum spp.)、血吸蟲屬(Schistosoma spp.)、毛畢屬(Trichobilharzia spp.)、毛樣線蟲屬(Ornithobilharzia spp.)、澳畢吸蟲屬(Austrobilharzia spp.)、巨畢吸蟲屬(Gigantobilharzia spp.)、彩蚴吸蟲屬(Leucochloridium spp.)、短咽吸蟲屬(Brachylaima spp.)、棘口吸蟲屬(Echinostoma spp.)、棘緣吸蟲屬(Echinoparyphium spp.)、棘隙吸蟲屬(Echinochasmus spp.)、低頸吸蟲屬(Hypoderaeum spp.)、肝吸蟲屬(Fasciola spp.)、擬片形吸蟲屬(Fasciolides spp.)、薑片蟲屬(Fasciolopsis spp.)、環腸吸
蟲屬(Cyclocoelum spp.)、盲腔屬(Typhlocoelum spp.)、雙口吸蟲屬(Paramphistomum spp.)、杯殖吸蟲屬(Calicophoron spp.)、盤吸蟲屬(Cotylophoron spp.)、巨盤吸蟲屬(Gigantocotyle spp.)、菲策吸蟲屬(Fischoederius spp.)、腹袋吸蟲屬(Gastrothylacus spp.)、背孔吸蟲屬(Notocotylus spp.)、下彎吸蟲屬(Catatropis spp.)、斜睾吸蟲屬(Plagiorchis spp.)、前殖吸蟲屬(Prosthogonimus spp.)、雙腔吸蟲屬(Dicrocoelium spp.)、闊盤吸蟲屬(Eurytrema spp.)、鮭吸蟲屬(Troglotrema spp.)、並殖吸蟲屬(Paragonimus spp.)、肛瘤吸蟲屬(Collyriclum spp.)、隱孔吸蟲屬(Nanophyetus spp.)、後睾吸蟲屬(Opisthorchis spp.)、支睪吸蟲屬(Clonorchis spp.)、次睾吸蟲屬(Metorchis spp.)、異形吸蟲屬(Heterophyes spp.)、後殖吸蟲屬(Metagonimus spp.);線蟲:毛形亞目(Trichinellida),例如:毛首線蟲屬(Trichuris spp.)、毛細線蟲屬(Capillaria spp.)、毛細線蟲屬(Paracapillaria spp.)、優鞘線蟲屬(Eucolcus spp.)、線蟲屬(Trichomosoidcs spp.)、旋毛蟲屬(Trichinella spp.);墊刃目(Tylenchida),例如:細頸線蟲屬(Micronema spp.)、糞桿線蟲屬(Strongyloides spp.);小桿亞目(Rhabditina),例如:圓線蟲屬(Strongylus spp.)、三齒線蟲屬(Triodontophorus spp.)、食道齒線蟲屬(Oesophagodontus spp.)、毛線線蟲屬(Trichonema spp.)、輻首線蟲屬(Gyalocephalus spp.)、柱咽線蟲屬(Cylindropharynx spp.)、盆口線蟲屬(Poteriostomum spp.)、線蟲屬(Cyclococercus spp.)、杯冠線蟲屬(Cylicostephanus spp.)、食道口線蟲屬(Oesophagostomum spp.)、夏桕線蟲屬(Chabertia spp.)、冠尾線蟲屬(Stephanurus spp.)、鉤蟲屬(Ancylostoma spp.)、彎口線蟲屬(Uncinaria spp.)、鉤蟲屬(Necator spp.)、仰口線蟲屬(Bunostomum spp.)、球首線蟲屬
(Globocephalus spp.)、比翼線蟲屬(Syngamus spp.)、節蟲屬(Cyathostoma spp.)、後圓線蟲屬(Metastrongylus spp.)、網尾線蟲屬(Dictyocaulus spp.)、繆勒線蟲屬(Muellerius spp.)、原圓線蟲屬(Protostrongylus spp.)、新圓線蟲屬(Neostrongylus spp.)、囊尾線蟲屬(Cystocaulus spp.)、肺圓線蟲屬(Pneumostrongylus spp.)、指尾線蟲屬(Spicocaulus spp.)、鹿圓線蟲屬(Elaphostrongylus spp.)、副麂圓線蟲屬(Parelaphostrongylus spp.)、環體線蟲屬(Crenosoma spp.)、副環體線蟲屬(Paracrenosoma spp.)、奧斯勒絲蟲屬(Oslerus spp.)、住血線蟲屬(Angiostrongylus spp.)、肺線蟲屬(Aelurostrongylus spp.)、類絲線蟲屬(Filaroides spp.)、副類絲線蟲屬(Parafilaroides spp.)、毛圓線蟲屬(Trichostrongylus spp.)、血線蟲屬(Haemonchus spp.)、奧斯特線蟲屬(Ostertagia spp.)、牛胃絲蟲屬(Teladorsagia spp.)、馬歇爾線蟲屬(Marshallagia spp.)、古柏線蟲屬(Cooperia spp.)、日圓線蟲屬(Nippostrongylus spp.)、螺旋線蟲屬(Heligmosomoides spp.)、細頸線蟲(Nematodirus spp.)、胃圓線蟲屬(Hyostrongylus spp.)、尖頭胃線蟲屬(Obeliscoides spp.)、裂口線蟲屬(Amidostomum spp.)、壺肛線蟲屬(Ollulanus spp.);旋尾目(Spirurida),例如:尖尾線蟲屬(Oxyuris spp.)、蟯蟲屬(Enterobius spp.)、栓尾線蟲屬(Passalurus spp.)、管狀線蟲屬(Syphacia spp.)、無刺蟯蟲屬(Aspiculuris spp.)、異刺線蟲屬(Heterakis spp.);蛔蟲屬(Ascaris spp.)、弓蛔屬(Toxascaris spp.)、弓首線蟲屬(Toxocara spp.)、貝利蛔蟲屬(Baylisascaris spp.)、副蛔屬(Parascaris spp.)、海獸胃線蟲屬(Anisakis spp.)、禽蛔屬(Ascaridia spp.);棘口線蟲屬(Gnathostoma spp.)、泡翼線蟲屬(Physaloptera spp.)、吸吮線蟲屬(Thelazia spp.)、筒線蟲屬(Gongylonema spp.)、馬胃線蟲屬(Habronema spp.)、副柔絲線蟲屬(Parabronema spp.)、德拉西線蟲屬(Draschia spp.)、龍線蟲屬(Dracunculus spp.);冠絲蟲屬(Stephanofilaria spp.)、類絲蟲屬
(Parafilaria spp.)、絲狀線蟲屬(Setaria spp.)、羅阿絲蟲屬(Loa spp.)、血直絲蟲屬(Dirofilaria spp.)、光絲蟲屬(Litomosoides spp.)、血絲蟲屬(Brugia spp.)、吳策絲蟲屬(Wuchereria spp.)、蟠尾絲蟲屬(Onchocerca spp.)、旋尾線蟲屬(Spirocerca spp.);棘頭動物門(Acantocephala):少棘目(Oligacanthorhynchida),例如:巨吻棘頭蟲屬(Macracanthorhynchus spp.)、前睾棘頭蟲屬(Prosthenorchis spp.);多形目(Polymorphida),例如:細頸棘頭蟲屬(Filicollis spp.);念珠目(Moniliformida),例如:聯珠狀棘頭蟲屬(Moniliformis spp.);棘吻目(Echinorhynchida),例如:棘頭蟲屬(Acanthocephalus spp.)、魚棘頭蟲屬(Echinorhynchus spp.)、似細吻棘頭蟲屬(Leptorhynchoides spp.);舌形動物門(Pentastoma):孔頭蟲目(Porocephalida),例如:舌形蟲屬(Linguatula spp.)。
在獸醫與動物飼養領域中,式(I)、(Ia)、(Ib)或(Ic)化合物係呈合適之製劑型式,採用相關技藝上已知方法投藥,如:經腸、非經腸式、經皮膚或經鼻投藥。該投藥法可為預防性或醫療性。
因此,本發明一項具體實施例係指以式(I)、(Ia)、(Ib)或(Ic)化合物作為醫藥之用途。
另一態樣係指一種以式(I)、(Ia)、(Ib)或(Ic)化合物作為抗體內寄生蟲劑,特定言之殺蠕蟲劑或抗原蟲劑之用途。式(I)、(Ia)、(Ib)或(Ic)化合物適合在例如:動物畜養、動物養殖、動物圈養及衛生領域中作為抗體內寄生蟲劑,特定言之殺蠕蟲劑或抗原蟲劑使用。
另一態樣係有關一種以式(I)、(Ia)、(Ib)或(Ic)化合物作為抗體外寄生蟲劑,特定言之殺節胺動物劑,如:殺昆蟲劑或殺蜱蟎劑之用途。另一態樣係指一種以式(I)、(Ia)、(Ib)或(Ic)化合物在例如:動物畜養、動物
養殖、動物圈養及衛生領域中作為抗體外寄生蟲劑,尤指殺節胺動物劑,如:殺昆蟲劑或殺蜱蟎劑之用途。
可述及下列殺蠕蟲混合組份實例:殺蠕蟲活性化合物包括殺吸蟲與殺絛蟲活性化合物:大環內酯類,例如:阿巴汀(abamectin)、多拉菌素(doramectin)、埃瑪菌素(emamectin)、埃普利諾菌素(eprinomectin)、伊維菌素(ivermectin)、米爾倍黴素(milbemycin)、莫西菌素(moxidectin)、奈馬菌素(nemadectin)、色拉菌素(selamectin);苯并咪唑類與原苯并咪唑類、例如:阿苯達唑(albendazole)、阿苯達唑-亞碸、邊達唑(cambendazole)、環苯達唑(cyclobendazole)、非班太爾(febantel)、芬苯達唑(fenbendazole)、氟苯噠唑(flubendazole)、美鞭達唑(mebendazole)、奈托比胺(netobimin)、奧吩達唑(oxfendazole)、奧苯達唑(oxibendazole)、撲殺熱(parbendazole)、腐絕(thiabendazole)、多保淨(thiophanate)、三氯苯咪唑(triclabendazole);環八縮肽類,例如:艾默德斯(emodepside)、PF1022;胺基乙腈衍生物類,例如:莫內太爾(monepantel);四氫嘧啶類,例如:摩朗得(morantel)、噻嘧啶(pyrantel)、酚嘧啶(oxantel);咪唑并噻唑類,例如:丁咪唑(butamisole)、左旋咪唑(levamisole)、四咪唑(tetramisole);水楊醯替苯胺類,例如:溴氟硝柳胺(bromoxanide)、溴替尼特(brotianide)、氯碘柳苯胺(clioxanide)、氯氰碘柳胺(closantel)、耐克螺(niclosamide)、氯羥柳胺(oxyclozanide)、碘醚柳胺(rafoxanide)、三溴水楊胺(tribromsalan);對郝喹醯胺類(paraherquamide),例如:得曲恩特(derquantel)、對郝喹醯胺
(paraherquamide);胺基苯基脒類,例如:阿米太爾(amidantel)、脫醯基阿米太爾(amidantel)(dAMD)、三苯雙脒(tribendimidine);有機磷酸酯類,例如:香豆磷(coumaphos)、育畜磷(crufomate)、二氯松(dichlorvos)、哈洛克酮(haloxone)、萘伏斯(naphthalofos)、三氯松(trichlorfon);經取代苯酚類,例如:硫双二氯酚(bithionol)、二碘硝基酚(disophenol)、六氯酚(hexachlorophene)、聯硝氯酚(niclofolan)、滅硝氯酚(meniclopholan)、硝碘酚腈(nitroxynil);哌 酮類,例如:吡喹酮(praziquantel)、依西太爾(epsiprantel);各種不同其他類,例如:硝硫氰胺(amoscanate)、溴芐芬寧(bephenium)、丁萘脒(bunamidine)、氯硝西泮(clonazepam)、氯舒隆(clorsulon)、地芬尼泰(diamfenetid)、二氯吩(dichlorophen)、二乙基卡馬西平(diethylcarbamazine)、吐根鹼(emetine)、海妥林(hetolin)、羥胺硫蒽酮(hycanthone)、硫蒽酮(lucanthone)、甲硫蒽酮(Miracil)、米拉散(mirasan)、耐克螺(niclosamide)、硝唑咪(niridazole)、硝碘酚腈(nitroxynil)、硝硫氰酯(nitroscanate)、奧替普拉(oltipraz)、臍菇亭(omphalotin)、奥沙尼喹(oxamniquin)、巴龍黴素(paromomycin)、哌(piperazine)、雷瑣侖太(resorantel)。
式(I)、(Ia)、(Ib)或(Ic)化合物亦可用於控制病媒。本發明之目的中,病媒係節胺動物,特定言之,會從帶原者(植物、動物、人類,等等)傳播病原菌(如,例如:病毒、蠕蟲、單細胞生物與細菌)給宿主之昆蟲或蜘蛛類。該病原菌可經由機械式傳播至宿主(例如:經由非叮咬性蠅傳播之沙眼)或經由注入傳播至宿主(例如:由蚊子傳播之瘧疾寄生蟲)。
病媒及其所傳播之疾病或病原菌之實例為:
1)蚊子
- 按蚊(Anopheles):瘧疾、絲蟲病;- 庫蚊(Culex):日本腦炎、絲蟲病、其他病毒疾病、蠕蟲之傳播;- 伊蚊(Aedes):黃熱病、登格熱、絲蟲病、其他病毒疾病;- 蚋科(Simuliidae):傳播蠕蟲,特定言之,盤尾線蟲(Onchocerca volvulus)
2)蝨:皮膚傳染病、流行性斑疹傷寒;
3)跳蚤:疫病、鼠型斑疹傷寒;
4)蠅:昏睡病(錐蟲病);霍亂、其他細菌性疾病;
5)蟎:家畜疥癣病、流行性斑疹傷寒、立克次痘疹(Rickettsialpox)、兔熱病(Tularamia)、聖路易腦炎(Saint-Louis encephalitis)、蜱傳播性腦炎(TBE)、克里米亞-剛果惡性血液疾病(Krim-Kongo haematologic fever)、疏螺旋體病;
6)蜱:疏螺旋體病(Borelliosis),如:杜通氏螺旋體(Borrelia duttoni)、蜱傳播性腦炎、Q熱(貝氏考克斯菌(Coxiella burnetii))、焦蟲症(犬焦蟲症(Babesia canis canis))。
本發明之病媒實例為昆蟲,例如:會傳播植物病毒給植物之蚜蟲、蠅、葉蟬或薊馬。其他會傳播植物病毒之病媒為蜘蛛蟎、蝨、甲蟲與線蟲。
本發明病媒之其他實例為昆蟲與蜘蛛類,如:蚊子,特定言之可能傳播病原菌給動物與/或人類之伊蚊(Aedes)、按蚊(Anopheles),例如:甘比亞按蚊(A.gambiae)、阿拉伯按蚊(A.arabiensis)、致死按蚊(A.funestus)、大劣按蚊(A.dirus)(瘧疾)與庫蚊(Culex)、蝨、跳蚤、蠅、蟎、與蜱。
亦可能使用突破抗性之式(I)、(Ia)、(Ib)或(Ic)化合物控制病媒。
式(I)、(Ia)、(Ib)或(Ic)化合物適用於預防由病媒傳播之疾病或病原菌。因此本發明另一態樣係以式(I)、(Ia)、(Ib)或(Ic)化合物於控制病媒之用途,例如:用於農業、園藝、花園與休閒活動設施,及亦用於保護原料與庫存產品。
式(I)、(Ia)、(Ib)或(Ic)化合物適用於保護工業材料,對抗昆蟲之侵害或破壞,例如:鞘翅目(Coleoptera)、膜翅目(Hymenoptera)、等翅目(Isoptera)、鱗翅目(Lepidoptera)、囓蟲目(Psocoptera)與總尾目(Zygentoma)。
咸了解,本文所指之工業材料為無生命材料,如:較佳為塑膠、膠黏劑、膠水、紙張與紙板、皮革、木料、加工木製品與塗料組成物。本發明用途特別適合保護木料。
另一項具體實施例中,式(I)、(Ia)、(Ib)或(Ic)化合物係與至少一種其他殺昆蟲劑與/或至少一種殺真菌劑共同使用。
另一項具體實施例中,式(I)、(Ia)、(Ib)或(Ic)化合物係呈即用型除害蟲劑,亦即其不需要進一步修飾即可施用在所需材料上。合適之其他殺昆蟲劑或殺真菌劑特定言之係如上述說明者。
亦已驚人地發現,式(I)、(Ia)、(Ib)或(Ic)化合物可用於保護與鹽水或鹹水接觸之物品,特定言之船體、隔板、編網、建築物、繫船設備及訊號系統,防止污塞。同樣地,式(I)、(Ia)、(Ib)或(Ic)化合物可單獨使用或與其他活性化合物組合,作為抗污塞劑使用。
式(I)、(Ia)、(Ib)或(Ic)化合物適合在衛生領域中控制動物害
蟲。特定言之,本發明可應用在居家領域、衛生領域及保護庫存產品中,尤其控制出現在如:住家、廠房、辦公室、車廂等封閉空間之昆蟲、蜘蛛與蟎類。式(I)、(Ia)、(Ib)或(Ic)化合物可單獨使用或與其他活性化合物與/或輔劑組合用於控制動物害蟲。該等其他化合物較佳係家庭用殺昆蟲劑產品。式(I)、(Ia)、(Ib)或(Ic)化合物可有效對抗敏感性及抗性品種,並對抗所有發展階段。
此等害蟲包括例如:蜘蛛綱(Arachnida),蠍目(Scorpiones)、
蜘蛛目(Araneae)與盲蛛目(Opiliones);唇足目(Chilopoda)與重足目(Diplopoda);昆蟲綱,蜚蠊目(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)、毛蝨目(Phthiraptera)、囓蟲目(Psocoptera)、跳躍亞目(Saltatoria)或直翅目(Orthoptera)、蚤目(Siphonaptera)與總尾目(Zygentoma),及軟甲綱(Malacostraca)等足目(Isopoda)。
其可呈例如:氣霧劑、無壓力噴灑產品,例如:泵壓及霧
化噴灑器、自動噴霧系統、霧化器、發泡物、凝膠、使用由纖維素或塑膠製成之蒸發片之蒸發器產品、液體蒸發器、凝膠及膜式蒸發器、螺漿驅動式蒸發器、無能源或被動式蒸發系統、防蟲紙、防蟲袋及防蟲膠,呈粒狀或細粉,用於撒播式誘餌或用於誘餌台等形式使用。
現在將參考下列沒有限制性之製造與使用實例說明本發明
各種不同態樣。
方法M1:1H-NMR-數據係採用Bruker Avance 400,加裝流動池(60μl體積)或採用Bruker AVIII 400,加裝1.7mm cryo CPTCI探頭或採用Bruker AVII 600(600.13MHz),加裝5mm cryo TCI探頭或採用Bruker AVIII 600(601.6MHz),加裝5mm cryo CPMNP探頭,使用四甲基矽烷作為參考物(0.0)與溶劑CD3CN、CDCl3或D6-DMSO測定。
方法M2:或者,1H-NMR-數據係採用Bruker DMX300(1H-NMR:300MHz),使用四甲基矽烷作為參考標準物測定。
所選出實例之NMR-數據係依標準格式(化學位移δ,多峰性,氫原子數)或NMR-波峰列表出示。
LCMS(M+H):405.8,407.8
1H-NMR(400MHz,d6-DMSO,方法M1);δ 8.61(t,1H,NH),7.77-7.62(m,3H),7.53-7.51(dd,1H),7.46(d,1H),7.35(d,1H),3.50-3.45(qu,2H),2.91(t,2H)。
1H-NMR(400MHz,d6-DMSO,方法M1);δ 8.91(s,1H),8.68(t,1H,NH),8.64(s,1H),8.33(s,1H),7.94(s,1H),7.83-7.46(m,6H),3.55-3.50(qu,2H),3.00(t,2H)。
1H-NMR(400MHz,d6-DMSO,方法M1);δ 7.91(s,1H),7.74(d,1H),7.57(d,1H),4.68(bs,2H,NH2),3.46(t,2H)。
1H-NMR(400MHz,d6-DMSO,方法M1);δ 8.98(t,1H,NH),7.91(s,1H),7.77-7.56(m,5H),7.36(d,1H),4.17(dt,2H)。
1H-NMR(400MHz,d6-DMSO,方法M1);δ 9.38(s,1H),9.03(t,1H,NH),8.31(s,1H),8.20(d,1H),8.06(dd,1H),7.83-7.49(m,4H),7.39(d,1H),4.22(dr,2H)。
1H-NMR(400MHz,d6-DMSO,方法M1);δ 9.03(t,1H,NH),8.67(s,1H),8.42-8.38(dt,1H),8.02(s,1H),7.88(d,1H),7.77-7.62(m,4H),7.39-7.32(d+d,2H),4.26-4.18(dt,1H)。
1H-NMR(400MHz,d6-DMSO方法M1);δ 8.60(sb,3H),7.87(s,1H),7.73(dd,1H),7.56(d,1H),6.22(m,1H),3.44-3.21(m,2H)。
LCMS(M-HCl+H)+:252.0,254.0
1H-NMR(400MHz,d6-DMSO方法M1);δ 8.91(t,1H),7.82-7.63(m,5H),7.54-7.45(m,2H),6.00(dt,1H),3.81-3.69(m,2H)
1H-NMR:參見表中NMR波峰列表,實例1-73
LCMS(M+H)+:257.0,459.0
LCMS(M+H):278.0,280.0
LCMS(M+H)+:233.1,234.9
1H-NMR(400MHz,d6-DMSO,方法M1);δ 8.90(s,1 H),8.65(d,1 H),8.22(d,1 H),8.02(d,1 H),7.82-7.93(m,2 H),2.63(s,3 H)
LCMS(M+H)+:250.0
1H-NMR(400MHz,d6-DMSO,方法M1);δ 8.87(s,1 H),8.64(d,1 H),8.18(m,1 H),8.01(d,1 H),8.85(m,2 H),7.66(s,1H),1.90(s,3 H)
LCMS(M+H)+:277.1
1H-NMR(400MHz,CD3CN,方法M1);δ 8.75(t,1 H),8.54(d,1 H),7.92(d,1 H),7.87(m,1 H),7.77(d,2 H),2.26(d,3 H)
LCMS(M+H)+:279.1
1H-NMR(400MHz,d6-DMSO,方法M1);δ 8.89(s,1 H),8.66(d,1 H),8.33(s,2 H),8.22(dd,1 H),8.04(m,1 H),7.93(dd,1H),7.73(d,1H),4.2(bs,2H),1.97(d,3H)
LCMS(M+H-HCl)+:283.0
1H-NMR:參見表中NMR波峰列表,實例1-101。
LCMS(M+H)+:455.0
1H-NMR(400MHz,CD3CN,方法M1);δ,7.63(m,2H),7.50(dd,1H),2.20(d,3H)。
1H-NMR(400MHz,d6-DMSO,方法M1);δ,8.10(s,3H),7.73(s,1H),7.59(m,2H),3.67-3.50(m,2H),1.87(d,3H);LCMS(M+H-HCl)+:220.0
1H-NMR(400MHz,CDCl3,方法M1);δ,7.69(m,1H),7.57-7.50(m,3H),7.44(d,1H),7.33(m,2H),5.92(s,1H),4.28-4.16(m,2H),1.91(d,3H);LC-MS:(M+H)+:395.0
1H-NMR:參見表中NMR波峰列表,實例1-130。
LC-MS:(M+H)+:455.1
反應混合物使用水(300ml)稀釋,分離有機層。水層使用乙醚(2*100ml)萃取。合併之有機層與10%鹽酸(500ml)混合,混合物過濾。濾餅使用乙醚與甲苯洗滌。分離濾液。
水層與固體材料合併,混合物依序使用碳酸氫鈉與碳酸鈉中和。粗製胺使用醚(3 x 150ml)萃取。萃液使用水(150ml)、鹽水(150ml)洗滌,脫水(Na2SO4),使用醚-鹽酸溶液處理。
濾出粗製2-[2-氯-4-(6-氟-3-吡啶基)苯基]-2,2-二氟-1-乙胺鹽酸鹽(32g,76%產率),使用醚洗滌,與真空乾燥。
1H-NMR(400.0MHz,DMSO,方法M1):δ 1=8.79(bs,3H,NH3 +),8.69(d,1H),8.45-8.40(dt,1H),8.08(s,1H),7.93-7.91(d,1H),7.80-7.78(d,1H),7.38-7.35(dd,1H),3.92-3.81(bt,2H)。
依據上述方法,製備下列通式(I)化合物與中間物(INT)。
所選定實例之1H-NMR數據係以書寫之1H-NMR-波峰列表出示。每個訊號峰均以δ-值(ppm)表示,訊號強度則列於圓括號中。每對δ-值-訊號強度之間以分號作為分隔符號。
因此某一實例之波峰列表型式為:δ1(強度1);δ2(強度2);......;δi(強度i);......;δn(強度n)
陡峰訊號強度係與印出之NMR光譜實例中訊號高度(以cm計)呈相關性,且顯示訊號強度之真實比例關係。在寬峰訊號中,則可出示複數個峰或中間訊號及其相較於光譜中最高強度訊號之相對強度。
採用四甲基矽烷與/或所使用溶劑之化學位移(尤其用在DMSO中測定光譜時)進行校準。因此四甲基矽烷峰有可能但不一定會出現在NMR波峰列表中。
1H-NMR波峰列表類似印出之典型1H-NMR圖,因此通常包含列於典型NMR-解讀中之所有波峰。
此外,其可如同印出之典型1H-NMR圖,其亦顯示溶劑訊號、目標化合物之立體異構物(其亦為本發明之目標之一部份)訊號及/或雜質之波峰。
在溶劑與/或水之δ-範圍內顯示化合物訊號時,一般溶劑波峰(例如:
DMSO-D6中之DMSO波峰)及水之波峰係示於吾等之1H-NMR波峰列表,其通常以高強度平均值表示。
目標化合物之立體異構物波峰與/或雜質波峰之平均強度通常低於目標化合物(例如:純度>90%)之波峰強度。
此等立體異構物與/或雜質係典型出現在特定製法中。因此其波峰有助於藉由“副產物指印”辨識吾等製法之再現性。
可以採用已知方法(MestreC,ACD-模擬法,但亦採用實驗性分析之預期數值)計算目標化合物波峰之專家可依需要另外採用其他強度濾波器,單離出目標化合物之波峰。此單離法即類似典型1H-NMR解讀中相關波峰挑選法。
有關使用波峰列表說明1H NMR數據之進一步詳細內容可參見文獻:Research Disclosure Database Number 564025之”Citation of NMR Peaklist Data within Patent Applications“。
MS儀器型態:Agilent Technologies 6130 Quadrupole LC-MS;HPLC儀器型態:Agilent Technologies 1260 Infinity;管柱:Waters XSelect(C18,50x2.1mm,3.5μ);流速:0.8mL/min;管柱溫度:35℃;溶離液A:0.1%甲酸之乙腈溶液;溶離液B:0.1%甲酸之水溶液;線性梯度:t=0 min 5% A,t=3.5min 98% A,t=6min 98% A;檢測:DAD(220-320nm);檢測:MSD(ESI pos/neg)質量範圍:100-800;檢測:ELSD(PL-ELS 2100):氣體流速1.2mL/min,氣體溫度:70℃,neb:50℃。
MS儀器型態:Agilent Technologies LC/MSD SL;HPLC儀器型態:Agilent Technologies 1100 Series;管柱:Waters XSelect(C18,50x2.1mm,3.5μ;流速:0.8mL/min;管柱溫度:25℃;溶離液A:95%乙腈+5%碳酸氫銨之水溶液;溶離液B:10mM碳酸氫銨之水溶液,pH=9.0;線性梯度:t=0min 5% A,t=3.5min 98% A,t=6min 98% A;檢測:DAD(220-320nm);檢測:MSD(ESI pos/neg)質量範圍:100-800。
1H-儀器型態:Bruker DMX300(1H-NMR:300MHz);內標準物:四甲基矽烷;化學位移(δ)係以每百萬分之一[ppm]表示;採用下列縮寫:s=單峰,d=雙峰,t=參峰,q=肆峰,m=多峰,br.=寬峰;偶合常數係以赫茲[Hz]
表示。
製造合適之活性化合物製劑時,取10mg活性化合物溶於0.5ml溶劑中,使用”林格氏溶液(Ringer’s solution)”稀釋該濃縮液至所需濃度。
取約40隻扭轉血矛線蟲(Haemonchus contortus)幼蟲移至含有化合物溶液之試管中。
5天後,記錄幼蟲死亡率。100%效力係指所有幼蟲均死亡;0%效力係指沒有任何幼蟲死亡。
此試驗中,下列製備實例之化合物在20ppm之施用率下顯示100%之良好活性:1-33、1-35、1-37、1-38、1-39、1-40、1-42、1-43、1-44、1-45、1-47、1-48、1-53、1-62、1-66、1-68、1-69、1-72、1-73、1-74、1-75、1-77、
1-78、1-79、1-80、1-81、1-82、1-83、1-84、1-85、1-86、1-87、1-88、1-89、1-90、1-92、1-93、1-94、1-96、1-97、1-98、1-99、1-100、1-101、1-102、1-103、1-106、1-107、1-111、1-120、1-122、1-126、1-127、1-128。
此試驗中,下列製備實例之化合物在20ppm之施用率下顯示90%之良好活性:1-3、1-5、1-12、1-14、1-32、1-41、1-49、1-67、1-70、1-71、1-104、1-110。
此試驗中,下列製備實例之化合物在20ppm之施用率下顯示80%之良好活性:1-1、1-11、1-16、1-20、1-27、1-28、1-56、1-57、1-58、1-60、1-64、1-114、1-121。
此試驗中,下列製備實例之化合物在4ppm之施用率下顯示90%之良好活性:1-15、1-124。
製造合適之活性化合物製劑時,取10mg活性化合物溶於0.5ml溶劑中,使用”林格氏溶液”稀釋該濃縮液至所需濃度。
取約40隻線蟲幼蟲(短古柏線蟲(Cooperia curticei))移至含有化合物溶液之試管中。
5天後,記錄幼蟲死亡率。100%效力係指所有幼蟲均死亡;0%效力係指沒有任何幼蟲死亡。
此試驗中,例如:下列製備實例之化合物在20ppm之施用率下顯示100%之良好活性:1-9、1-12、1-14、1-15、1-16、1-18、1-19、1-20、1-21、1-31、1-32、1-33、1-34、1-35、1-37、1-38、1-39、1-40、1-41、1-42、1-43、1-44、1-45、1-46、1-47、1-48、1-49、1-51、1-52、1-53、1-55、1-57、1-58、1-59、1-60、1-62、1-64、1-66、1-68、1-69、1-70、1-71、1-72、1-73、1-74、
1-75、1-77、1-78、1-79、1-80、1-81、1-82、1-83、1-84、1-85、1-86、1-87、1-88、1-89、1-90、1-91、1-92、1-93、1-94、1-96、1-97、1-98、1-99、1-100、1-101、1-102、1-106、1-146、1-107、1-110、1-111、1-114、1-120、1-122、1-126、1-127、1-128。
此試驗中,例如:下列製備實例之化合物在20ppm之施用率下顯示90%之良好活性:1-24、1-26、1-50、1-65、1-105、1-124。
此試驗中,例如:下列製備實例之化合物在20ppm之施用率下顯示80%之良好活性:1-1、1-13、1-23、1-27、1-28、1-36、1-56、1-121、1-125。
此試驗中,例如:下列製備實例之化合物在4ppm之施用率下顯示100%之良好活性:1-104。
此試驗中,例如:下列製備實例之化合物在4ppm之施用率下顯示90%之良好活性:1-67、1-149。
取巴西日圓線蟲(Nippostrongylus brasiliensis)成蟲使用包含100U/ml青黴素、0.1mg/ml鏈黴素與2.5μg/ml兩性黴素(amphotericin)B之生理食鹽水緩衝液洗滌。試驗化合物溶於DMSO,該蠕蟲使用最終濃度10μg/ml(10ppm)於培養基中培養。取一份培養基來測定乙醯基膽鹼酯酶活性,並與陰性對照組比較。依Rapson等人(1986)與Rapson等人(1987)所說明之原理測定乙醯基膽鹼酯酶活性,代表殺蠕蟲活性。
下列實例在10ppm下展現60%或更高之活性(相對於陰性對照組之AChE降低程度:1-1;1-9;1-33;1-37;1-44;1-45;1-48;1-49;1-53;1-68;1-69;1-70;1-73;1-74;1-75;1-77;1-78;1-82;1-87;1-88;1-89;1-90;1-92;1-93;
1-96;1-97;1-98;1-99;1-100;1-101;1-106;1-107;1-111
下列實例在10ppm下展現80%或更高之活性(相對於陰性對照組之AChE降低程度:1-1、1-33、1-37、1-45、1-53、1-68、1-69、1-70、1-73、1-74、1-77、1-82、1-93、1-96、1-97、1-99、1-100、1-106、1-107、1-111。
溶劑:125.0 份重量比丙酮
製造合適之活性化合物製劑時,取1份重量比之活性化合物與上述量溶劑混合,並加水稀釋該濃縮液至所需濃度。
在容器中填充砂子、活性成份溶液、含有南方根瘤線蟲(Meloidogyne incognita)之卵與幼蟲之懸浮液及生菜(salad)種子。讓生菜種子發芽及長成幼苗。在根部形成蟲癭。
14天後,依據所形成之蟲癭決定殺線蟲之活性。100%意指沒有出現蟲癭;0%意指處理組植物根部之蟲癭數等於未處理對照組。
此試驗中,例如:下列製備實例之化合物在20ppm之施用率下顯示100%之良好活性:1-39、1-47、1-69、1-70、1-73、1-81、1-82、1-85、1-86、1-87、1-88、1-89、1-93、1-94、1-104、1-120、1-128、1-129、1-130。
此試驗中,例如:下列製備實例之化合物在20ppm之施用率下顯示90%之良好活性:1-16、1-19、1-20、1-24、1-37、1-42、1-44、1-48、1-66、1-68、1-74、1-80、1-106、1-126、1-136、1-140。
取經過實驗性感染血矛線蟲(Haemonchus)與/或毛圓線蟲(Trichostrongylus)之沙鼠在前開放期後段期間處理一次。試驗化合物係調配
成溶液或懸浮液,並經腹膜內或皮下施用。
在驗屍後,與已感染且經安慰劑處理之對照組比較,分別計算胃與小腸中蠕蟲數量減少程度,來測定每組之效力。
測試下列實例,且在指定劑量下接受腹膜內處理後之活性為90%或更高:
取從血液中新鮮純化之250隻犬心絲蟲(Dirofilaria immitis)微絲蟲加至含有含營養培養基與試驗化合物之DMSO之微滴定板中。依5種濃度-效應分析法,以二重覆測試化合物。以曝露在沒有試驗化合物之DMSO中之幼蟲作為陰性對照組。與化合物培養72小時後分析幼蟲。與陰性對照組比較,由活動力下降程度來決定效力。依據5種濃度之評估結果,計算濃度-效應曲線及EC50-值。
下列實例之EC50為<5ppm:1-70;1-73;1-74;1-77;1-78;1-89;1-93;1-99;1-100;1-101
下列實例之EC50為<2.5ppm:1-93
製造合適之活性化合物製劑時,取10mg活性化合物溶於0.5ml溶劑中,使用”林格氏溶液”稀釋該濃縮液至所需濃度。
取約40隻扭轉血矛線蟲(Haemonchus contortus)幼蟲移至含有化合物溶
液之試管中。
5天後,記錄幼蟲死亡率。100%效力係指所有幼蟲均死亡;0%效力係指沒有任何幼蟲死亡。
此試驗中,例如:下列製備實例之化合物所展現之活性程度優於先前技藝:參見下表4。
Claims (21)
- 一種式(I)化合物之用途,
其中n 為0、1、2、3或4,其受到環中可用於連接取代基X之位置數量之限制,各X分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、羥基、胺基、-SH、-SF5、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C8-烷基、具有1至5個鹵原子之C1-C8-鹵烷基、C2-C8-烯基、C2-C8-炔基、C1-C8-烷基胺基、二-(C1-C8-烷基)胺基、C1-C8-烷氧基、具有1至5個鹵原子之C1-C8-鹵烷氧基、C2-C8-烯基氧、具有1至5個鹵原子之C2-C8-鹵烯基氧、C3-C8-炔基氧、具有1至5個鹵原子之C3-C8-鹵炔基氧、C3-C8-環烷基、具有1至5個鹵原子之C3-C8-鹵環烷基、C1-C8-烷基羰基、具有1至5個鹵原子之C1-C8-鹵烷基羰基、-CONH(C1-C8-烷基)、-CON(C1-C8-烷基)2、-CONH(OC1-C8-烷基)、-CON(OC1-C8-烷基)(C1-C8-烷基)、C1-C8-烷氧基羰基、具有1至5個鹵原子之C1-C8-鹵烷氧基羰基、C1-C8-烷基羰基氧、具有1至5個鹵原子之C1-C8-鹵烷基羰基氧、C1-C8-烷基羰基胺基、具有1至5個鹵原子之C1-C8-鹵烷基羰基胺基、-OCONH(C1-C8-烷基)、-OCON(C1-C8-烷基)2、-OCONH(OC1-C8-烷基)、-OCO(OC1-C8-烷基)、-S-C1-C8-烷基、具有1至5個鹵原子之-S-C1-C8-鹵烷基、 -S(O)-C1-C8-烷基、具有1至5個鹵原子之-S(O)-C1-C8-鹵烷基、-S(O)2-C1-C8-烷基、具有1至5個鹵原子之-S(O)2-C1-C8-鹵烷基、(C1-C6-烷氧基亞胺基)-C1-C6-烷基、(C2-C6-烯基氧亞胺基)-C1-C6-烷基、(C3-C6-炔基氧亞胺基)-C1-C6-烷基、(苯甲基氧亞胺基)-C1-C6-烷基、苯甲基氧、-S-苯甲基、苯甲基胺基、苯氧基、-S-苯基與苯基胺基,Q 代表芳香系或部份飽和或飽和之5-或6-員雜環,其包含1至4個選自N、S、與O且帶有取代基Ym之雜原子,m 為0、1、2、3或4,其受到Q中可用於連接取代基Y之位置數量之限制,與各Y分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、羥基、胺基、-SH、-SF5、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C8-烷基、具有1至5個鹵原子之C1-C8-鹵烷基、C2-C8-烯基、C2-C8-炔基、C1-C8-烷基胺基、二-(C1-C8-烷基)胺基、C1-C8-烷氧基、具有1至5個鹵原子之C1-C8-鹵烷氧基、C2-C8-烯基氧、具有1至5個鹵原子之C2-C8-鹵烯基氧、C3-C8-炔基氧、具有1至5個鹵原子之C3-C8-鹵炔基氧、C3-C8-環烷基、具有1至5個鹵原子之C3-C8-鹵環烷基、C1-C8-烷基羰基、具有1至5個鹵原子之C1-C8-鹵烷基羰基、-CONH(C1-C8-烷基)、-CON(C1-C8-烷基)2、-CONH(OC1-C8-烷基)、-CON(OC1-C8-烷基)(C1-C8-烷基)、-NH(C1-C8-烷基羰基)、C1-C8-烷氧基羰基、具有1至5個鹵原子之C1-C8-鹵烷氧基羰基、C1-C8-烷基羰基氧、具有1至5個鹵原子之C1-C8-鹵烷基羰基氧、C1-C8-烷基羰基胺基、具有1至5個鹵原子之C1-C8-鹵烷基羰基胺基、 -OCONH(C1-C8-烷基)、-OCON(C1-C8-烷基)2、-OCONH(OC1-C8-烷基)、-OCO(OC1-C8-烷基)、-S-C1-C8-烷基、具有1至5個鹵原子之-S-C1-C8-鹵烷基、-S(O)-C1-C8-烷基、具有1至5個鹵原子之-S(O)-C1-C8-鹵烷基-S(O)2-C1-C8-烷基、具有1至5個鹵原子之-S(O)2-C1-C8-鹵烷基、-CH2-S-C1-C8-烷基、-CH2-S(O)-C1-C8-烷基、-CH2-S(O)2-C1-C8-烷基、(C1-C6-烷氧基亞胺基)-C1-C6-烷基、(C2-C6-烯基氧亞胺基)-C1-C6-烷基、(C3-C6-炔基氧亞胺基)-C1-C6-烷基、(苯甲基氧亞胺基)-C1-C6-烷基、苯甲基氧、-S-苯甲基、苯甲基胺基、苯氧基、-S-苯基與苯基胺基,R1、R2、R3與R4相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、胺基、-SH、-CHO、-OCHO、-NHCHO、-COOH、-CONH2、-CONH(OH)、-OCONH2、(羥亞胺基)-C1-C6-烷基、C1-C6-烷基、C2-C6-烯基、C2-C6-炔基、C1-C6-烷基胺基、二-(C1-C6-烷基)胺基、C1-C6-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、具有1至5個鹵原子之C1-C6-鹵烷基、具有1至5個鹵原子之C1-C6-鹵烷氧基、C2-C6-烯基氧、具有1至5個鹵原子之C2-C6-鹵烯基氧、C3-C6-炔基氧、具有1至5個鹵原子之C3-C6-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C3-C6-環烷基-C1-C6-烷基、具有1至5個鹵原子之C3-C6-鹵環烷基-C1-C6-烷基、C1-C6-烷基羰基、具有1至5個鹵原子之C1-C6-鹵烷基羰基、-CONH(C1-C6-烷基)、-CON(C1-C6-烷基)2、-CONH(OC1-C6-烷基)、-CON(OC1-C6-烷基)(C1-C6-烷基)、C1-C6-烷氧基羰基、具有1至5個鹵原子之C1-C6-鹵烷氧基羰基、-OC(O)-C1-C6-烷基、具有1至5個鹵原子之-OC(O)-C1-C6-鹵烷基、-NHC(O)-C1-C6-烷基、具有1至5個鹵原子 之-NHC(O)-C1-C6-鹵烷基、-OCONH(C1-C6-烷基)、-OCON(C1-C6-烷基)2、-OCONH(OC1-C6-烷基)、OCO(OC1-C6-烷基)、-S-C1-C6-烷基、具有1至5個鹵原子之-S-C1-C6-鹵烷基、-S(O)-C1-C6-烷基、具有1至5個鹵原子之-S(O)-C1-C6-鹵烷基、-S(O)2-C1-C6-烷基、具有1至5個鹵原子之-S(O)2-C1-C6-鹵烷基、苯甲基、苯甲基氧、-S-苯甲基、-S(O)-苯甲基、-S(O)2-苯甲基、苯甲基胺基、苯氧基、-S-苯基、-S(O)-苯基、-S(O)2-苯基、苯基胺基、苯基羰基胺基、2,6-二氯苯基-羰基胺基、2-氯苯基-羰基胺基與苯基,但其限制條件為R1為氟與/或R2為氟,R5 係選自下列所組成之群組中:氫、氰基、-CHO、-OH、C1-C6-烷基、具有1至5個鹵原子之C1-C6-鹵烷基、C1-C6-烷氧基、具有1至5個鹵原子之C1-C6-鹵烷氧基、C3-C7-環烷基、具有1至5個鹵原子之C3-C7-鹵環烷基、C3-C7-環烷基-C1-C6-烷基、-CONH(C1-C6-烷基)、C2-C6-烯基、C2-C6-炔基、C1-C6-烷氧基-C1-C6-烷基、C3-C7-環烷基-C1-C6-烷基、氰基-C1-C6-烷基、胺基-C1-C6-烷基、C1-C6-烷基胺基-C1-C6-烷基、二-(C1-C6-烷基)胺基-C1-C6-烷基、C1-C6-烷基羰基、具有1至5個鹵原子之C1-C6-鹵烷基羰基、C1-C6-烷氧基羰基、C1-C6-苯甲基氧羰基、C1-C6-烷氧基-C1-C6-烷基羰基、-S-C1-C6-烷基、具有1至5個鹵原子之-S-C1-C6-鹵烷基、-S(O)2-C1-C6-烷基、與具有1至5個鹵原子之-S(O)2-C1-C6-鹵烷基,A 代表式(A1)苯基 其中 o 為0、1、2、3、4或5,及各R 分別獨立選自下列所組成之群組中:鹵素、硝基、-OH、NH2、SH、SF5、CHO、OCHO、NHCHO、COOH、氰基、C1-C8-烷基、具有1至9個鹵原子之C1-C8-鹵烷基、C2-C8-烯基、C2-C8-炔基、C3-C6-環烷基、-S-C1-C8-烷基、具有1至5個鹵原子之-S-C1-C8-鹵烷基、C1-C8-烷氧基、具有1至5個鹵原子之C1-C8-鹵烷氧基、C1-C8-烷氧基-C2-C8-烯基、C1-C8-烷氧基羰基、具有1至5個鹵原子之C1-C8-鹵烷氧基羰基、C1-C8-烷基羰基氧、具有1至5個鹵原子之C1-C8-鹵烷基羰基氧、-S(O)-C1-C8-烷基、具有1至5個鹵原子之-S(O)-C1-C8-鹵烷基、-S(O)2-C1-C8-烷基、具有1至5個鹵原子之-S(O)2-C1-C8-鹵烷基、C1-C8-烷基磺醯胺、-NH(C1-C8-烷基)、N(C1-C8-烷基)2、苯基(可視需要經C1-C6-烷氧基取代)與苯氧基,或兩個鍵結在相鄰碳原子上之R共同代表-O(CH2)pO-,其中p代表1或2,或A 代表式(Het-1)雜環 其中R6與R7可相同或相異,且係選自下列所組成之群組中:氫、鹵素、胺基、硝基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R8 係選自下列所組成之群組中:氫、鹵素、硝基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-2)雜環 其中R9 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R10與R11 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、胺基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-3)雜環 其中R12 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R13 係選自下列所組成之群組中:氫、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-4)雜環 其中R14與R15可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、-S-C1-C4-烷基、-S(O)2-C1-C4-烷基、苯基(可視需要經鹵素或C1-C4-烷基取代)與吡 啶基(可視需要經鹵素或C1-C4-烷基取代),及R16 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,或A 代表式(Het-5)雜環 其中R17與R18 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、C1-C4-烷基氧與具有1至5個鹵原子之C1-C4-鹵烷基,及R19 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-6)雜環 其中R20 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R21與R23 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R22 係選自下列所組成之群組中:氫、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基-C1-C4-烷基、羥基-C1-C4- 烷基、-S(O)2-C1-C4-烷基、-S(O)2-N(C1-C4-烷基)2、C1-C6-烷基羰基、-S(O)2-苯基(可視需要經鹵素或C1-C4-烷基取代)與苯甲醯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-7)雜環 其中R24 係選自下列所組成之群組中:氫、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基-C1-C4-烷基、羥基-C1-C4-烷基、-S(O)2-C1-C4-烷基、-S(O)2-N(C1-C4-烷基)2、C1-C6-烷基羰基、-S(O)2-苯基(可視需要經鹵素或C1-C4-烷基取代)與苯甲醯基(可視需要經鹵素或C1-C4-烷基取代),及R25、R26與R27 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與C1-C4-烷基羰基,或A 代表式(Het-8)雜環 其中R28 係選自下列所組成之群組中:氫與C1-C4-烷基,及R29 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-9)雜環 其中R30 係選自下列所組成之群組中:氫與C1-C4-烷基,及R31 係選自下列所組成之群組中:鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-10)雜環 其中R32 係選自下列所組成之群組中:氫、鹵素、胺基、氰基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),及R33 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基、具有1至9個鹵原子之C1-C5-鹵烷氧基、胺基、經取代或未經取代之C1-C5-烷基胺基或經取代或未經取代之二-(C1-C5-烷基)-胺基,或A 代表式(Het-11)雜環 其中R34 係選自下列所組成之群組中:氫、鹵素、胺基、氰基、C1-C4-烷基 胺基、二-(C1-C4-烷基)胺基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R35 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-12)雜環 其中R36 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、胺基羰基與胺基羰基-C1-C4-烷基,及R37 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、C1-C4-烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、與-S(O)2-C1-C4-烷基,及R38 係選自下列所組成之群組中:氫、苯基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、羥基-C1-C4-烷基、C2-C6-烯基、C3-C6-環烷基、C1-C4-烷基硫-C1-C4-烷基、C1-C4-烷基-S(O)-C1-C4-烷基、C1-C4-烷基-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基硫-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基-C1-C4-烷基,或A 代表式(Het-13)雜環 其中R39 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、胺基羰基與胺基羰基-C1-C4-烷基,及R40 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、與-S(O)2-C1-C4-烷基,及R41 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、羥基-C1-C4-烷基、C2-C6-烯基、C3-C6-環烷基、C1-C4-烷基硫-C1-C4-烷基、C1-C4-烷基-S(O)-C1-C4-烷基、C1-C4-烷基-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基硫-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基-C1-C4-烷基與苯基(可視需要經鹵素、C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基或硝基取代),或A 代表式(Het-14)雜環 其中 R42 係選自下列所組成之群組中:氫、鹵素、氰基、硝基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、胺基羰基與胺基羰基-C1-C4-烷基,及R43 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、C1-C4-烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、與具有1至5個鹵原子之C1-C4-鹵烷基,及R44 係選自下列所組成之群組中:氫、苯基、苯甲基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、羥基-C1-C4-烷基、C2-C6-烯基、C3-C6-環烷基、C1-C4-烷基硫-C1-C4-烷基、C1-C4-烷基-S(O)-C1-C4-烷基、C1-C4-烷基-S(O)2-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基硫-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基-C1-C4-烷基,或A 代表式(Het-15)雜環 其中R45與R46 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-16)雜環 其中R47與R48 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、苯基(可視需要經鹵素或C1-C4-烷基取代)、與雜環基,如:吡啶基、嘧啶基與噻二唑基(各可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-17)雜環 其中R49與R50可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-18)雜環 其中R51 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-19)雜環 其中R52 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵 原子之C1-C4-鹵烷基,及R53 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原 子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-20)雜環 其中R54 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵 原子之C1-C4-鹵烷基,或A 代表式(Het-21)雜環 其中R55 係選自下列所組成之群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,其限制條件為Het-21中,R55不為CF3,及R56、R57與R58,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基與-S(O)2-C1-C4-烷基,或A 代表式(Het-22)雜環 其中R59 係選自下列所組成之群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4烷氧基、-S-C1-C5-烷基、S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、-S-C2-C5-烯基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、苯基氧(可視需要經鹵素或C1-C4-烷基取代)與-S-苯基(可視需要經鹵素或C1-C4-烷基取代),及R60、R61與R62,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、N-嗎啉(可視需要經鹵素或C1-C4-烷基取代)、與噻吩基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-23)雜環 其中R63、R64、R65與R66,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原 子之-S-C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基與-S(O)2-C1-C4-烷基,或A 代表式(Het-24)雜環 其中R67 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R68 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C6-烷氧基羰基、苯甲基(可視需要經1至3個鹵原子取代)、苯甲基氧羰基(可視需要經1至3個鹵原子取代)、與雜環基,如:吡啶基與嘧啶基(各可視需要經鹵素、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基取代),或A 代表式(Het-25)雜環 其中R69 係選自下列所組成之群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,及R70 係選自下列所組成之群組中:氫、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、與苯甲基,或 A 代表式(Het-26)雜環 其中X1 係選自下列所組成之群組中:硫、-SO-、SO2-與-CH2-,及R71 係選自下列所組成之群組中:C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R72與R73 可相同或相異,且係選自下列所組成之群組中:氫與C1-C4-烷基,或A 代表式(Het-27)雜環 其中R74 係選自下列所組成之群組中:C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-28)雜環 其中R75 係選自下列所組成之群組中:C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-29)雜環 其中R76 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,其係用於控制線蟲與/或其他蠕蟲。 - 根據申請專利範圍第1項之用途,其中X、n、R1、R2、R3、R4、R5與A係如申請專利範圍第1項之定義;Q代表可視需要經單-或多取代之雜芳香環,其係選自Q-1至Q-64所組成群組中:
其中m 為0、1或2,其受到Q中可用於連接取代基Y之位置數量之限制,及各Y分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基、C2-C4-烯基氧、具有1至5個鹵原子之C2-C4-鹵烯基氧、C3-C4-炔基氧、具有1至5個鹵原子之C3-C4-鹵炔基氧、C3-C6-環烷基、具有1至5個鹵原子之C3-C6-鹵環烷基、C1-C4-烷基羰基、具有1至5個鹵原子之C1-C4-鹵烷基 羰基、-CONH(C1-C4-烷基)、-CON(C1-C4-烷基)2、-CONH(OC1-C4-烷基)、-CON(OC1-C4-烷基)(C1-C4-烷基)、-NH(C1-C4-烷基羰基)、C1-C4-烷氧基羰基、具有1至5個鹵原子之C1-C4-鹵烷氧基羰基、C1-C4-烷基羰基氧、具有1至5個鹵原子之C1-C4-鹵烷基羰基氧、C1-C4-烷基羰基胺基、具有1至5個鹵原子之C1-C4-鹵烷基羰基胺基、-OCONH(C1-C4-烷基)、-OCON(C1-C4-烷基)2、-OCONH(OC1-C4-烷基)、-OCO(OC1-C4-烷基)、-S-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、-S(O)-C1-C4-烷基、具有1至5個鹵原子之-S(O)-C1-C4-鹵烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S(O)2-C1-C4-鹵烷基、-CH2-S-C1-C4-烷基、-CH2-S(O)-C1-C4-烷基、-CH2-S(O)2-C1-C4-烷基、(C1-C4-烷氧基亞胺基)-C1-C4-烷基、(C2-C6-烯基氧亞胺基)-C1-C4-烷基、(C3-C6-炔基氧亞胺基)-C1-C4-烷基、(苯甲基氧亞胺基)-C1-C6-烷基、苯甲基氧、-S-苯甲基、苯甲基胺基、苯氧基、-S-苯基與苯基胺基。 - 根據申請專利範圍第1或2項之用途,其中n 為1或2,各X分別獨立選自下列所組成之群組中:氫、鹵素、硝基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基,Q 代表可視需要經單-或多取代之雜芳香環,其係選自下列各物所組成群組中:Q-4、Q-11、Q-21、Q-22、Q-25、Q-36、Q-37、Q-38、Q-40、Q-41、Q-42、Q-45、Q-53、Q-58、Q-62、Q-63與Q-64,其中m 為0、1或2,其受到Q中可用於連接取代基Y之位置數量之限制, 與各Y分別獨立選自下列所組成之群組中:氫、-CF3、-CH2CF3、甲基、乙基、氟、氯、溴、碘、氰基、-OCH3、-OCH2CH3、-OCH(CH3)2、-OCH2CF3、S(O)2-CH3、NHC(O)CH3、NHCH3與N(CH3)2,R1與R2相同或相異,且係選自下列所組成之群組中:氫、鹵素、氰基、羥基、C1-C4-烷基、C2-C4-烯基、C2-C4-炔基、C1-C4-烷氧基、C3-C6-環烷基-C1-C3-烷基、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基、-NHC(O)-C1-C4-烷基、與苯基,其限制條件為R1為氟與/或R2為氟,R3與R4相同或相異,且係選自下列所組成之群組中:氫、-COOH、C1-C4-烷基、C1-C4-鹵烷基C1-C4-烷氧基、羥基-C1-C4-烷基、C1-C4-烷氧基-C1-C3-烷基、-CONH(C1-C4-烷基)、C1-C4-烷氧基羰基、-OC(O)-C1-C4-烷基與苯基,R5 係選自下列所組成之群組中:氫、C1-C4-烷基、C3-C6-環烷基、C1-C4-烷氧基、C1-C4-烷氧基-C1-C4-烷基、C1-C4-烷基羰基、C1-C4-烷氧基羰基,A 代表式(A1)苯基
其中o 為0、1或2,及各R 分別獨立選自下列所組成之群組中:鹵素、硝基、-OH、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C3-C6-環烷基、C1-C4-烷氧基、C1-C4-烷氧基羰基、-NH(C1-C4-烷基)、苯基(可視需 要經C1-C4-烷氧基取代)與苯氧基,或A 代表式(Het-1)雜環 其中R6與R7可相同或相異,且係選自下列所組成之群組中:氫、鹵素、硝基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R8 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-2)雜環 其中R9 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R10與R11可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基、苯基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-4)雜環 其中R14與R15可相同或相異,且係選自下列所組成之群組中:氫、鹵素、 C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、-S-C1-C4-烷基、-S(O)2-C1-C4-烷基、苯基(可視需要經鹵素或C1-C4-烷基取代)與吡啶基(可視需要經鹵素或C1-C4-烷基取代),及R16係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,或A 代表式(Het-5)雜環 其中R17與R18可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基、C1-C4-烷基氧與具有1至5個鹵原子之C1-C4-鹵烷基,及R19 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,或A 代表式(Het-6)雜環 其中R20 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及R21與R23 可相同或相異,且係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基,及 R22 係選自下列所組成之群組中:氫、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基-C1-C4-烷基,或A 代表式(Het-10)雜環 其中R32 係選自下列所組成之群組中:氫、鹵素、胺基、氰基、C1-C4-烷基胺基、二-(C1-C4-烷基)胺基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基與苯基(可視需要經鹵素或C1-C4-烷基取代),及R33 係選自下列所組成之群組中:鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基、包含1至9個鹵原子之C1-C5-鹵烷氧基、胺基、經取代或未經取代之C1-C5-烷基胺基或經取代或未經取代之二-(C1-C5-烷基)-胺基,或A 代表式(Het-21)雜環 其中R55 係選自下列所組成之群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、具有1至5個鹵原子之-S-C1-C4-鹵烷基與具有1至5個鹵原子之C1-C4-鹵烷氧基,其限制條件為Het-21中,R55不為CF3,及R56、R57與R58,其可相同或相異,且係選自下列各物所組成群組中: 氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基與-S(O)2-C1-C4-烷基,或A 代表式(Het-22)雜環 其中R59 係選自下列所組成之群組中:氫、鹵素、羥基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4烷氧基、-S-C1-C5-烷基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、-S-C2-C5-烯基、具有1至5個鹵原子之-S-C1-C4-鹵烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、苯基氧(可視需要經鹵素或C1-C4-烷基取代)與-S-苯基(可視需要經鹵素或C1-C4-烷基取代),及R60、R61與R62,其可相同或相異,且係選自下列各物所組成群組中:氫、鹵素、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、-S-C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷氧基、-S(O)-C1-C4-烷基、-S(O)2-C1-C4-烷基、N-嗎啉(可視需要經鹵素或C1-C4-烷基取代)與噻吩基(可視需要經鹵素或C1-C4-烷基取代),或A 代表式(Het-29)雜環 其中 R76 係選自下列所組成之群組中:氫、鹵素、C1-C4-烷基與具有1至5個鹵原子之C1-C4-鹵烷基。 - 根據申請專利範圍第1至3項之用途,其中n 為1或2,各X係選自下列所組成之群組中:氫、鹵素、硝基、氰基、C1-C4-烷基、具有1至5個鹵原子之C1-C4-鹵烷基、C1-C4-烷氧基、具有1至5個鹵原子之C1-C4-鹵烷氧基,Q 係選自:
R1與R2相同或相異,且係選自下列所組成之群組中:氫、甲基、乙基、 甲氧基、乙氧基或氟,其限制條件為R1為氟與/或R2為氟,R3與R4相同或相異,且係選自下列所組成之群組中:氫、甲基或乙基,R5 為氫,及A 係選自: 或A 係選自: - 根據申請專利範圍第1至4項之用途,其係用於保護作物。
- 根據申請專利範圍第1至4項之用途,其係用於動物健康領域。
- 一種式(Ia)化合物
其中n、X、Q、R2、R3、R4、R5與A係如申請專利範圍第1項或第2項或第3項或第4項之定義,及R1a為氟。 - 一種式(Ib)化合物
其中 n、X、Q、R1、R3、R4、R5與A係如申請專利範圍第1項或第2項或第3項或第4項之定義,及R2a為氟。 - 一種式(Ic)化合物
其中n、X、Q、R3、R4、R5與A係如申請專利範圍第1項或第2項或第3項或第4項之定義,及R1a與R2a均為氟。 - 一種調配物,特定言之農化調配物,其包含至少一種如申請專利範圍第1至4項中定義之式(I)化合物。
- 一種調配物,特定言之農化調配物,其包含至少一種如申請專利範圍第7至9項中定義之化合物。
- 根據申請專利範圍第10或11項之調配物,其進一步包含至少一種補充劑與/或至少一種界面活性劑。
- 根據申請專利範圍第10至12項之調配物,其中該式(I)、(Ia)、(Ib)或(Ic)化合物係與至少一種其他活性化合物形成混合物。
- 一種控制動物害蟲之方法,其中由如申請專利範圍第1至4項中定義之式(I)化合物或根據申請專利範圍第7至9項之化合物或根據申請專利範圍第10至13項之調配物作用在動物害蟲與/或其棲息地上。
- 根據申請專利範圍第14項之方法,其中該等動物害蟲包含線蟲或為線蟲。
- 一種保護種子與/或發芽中之植物免於害蟲(特定言之線蟲)侵害之方法,其包括之步驟為由種子與如申請專利範圍第1至4項中定義之式(I)化合物或根據申請專利範圍第7至9項之化合物或根據申請專利範圍第10至13項之調配物接觸。
- 一種種子,其係採用根據申請專利範圍第16項之方法得到。
- 一種以根據申請專利範圍第7至9項之化合物或根據申請專利範圍第10至13項之調配物於控制動物害蟲上之用途。
- 根據申請專利範圍第18項之用途,其中該等動物害蟲包含線蟲或為線蟲。
- 根據申請專利範圍第18或19項之用途,其係用於保護作物或用於動健康領域。
- 一種式(INT)化合物
其中R1、R2、Q、X與n係如申請專利範圍第1項或第2項或第3項或第4項之定義。
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| MA37756B1 (fr) | 2012-06-13 | 2018-09-28 | Hoffmann La Roche | Nouveaux composés diazaspirocycloalcane et azaspirocycloalcane |
| SI2900669T1 (sl) | 2012-09-25 | 2019-12-31 | F. Hoffmann-La Roche Ag | Derivati heksahidropirolo(3,4-C)pirola in sorodne spojine kot zaviralci avtotaksina (ATX) in kot zaviralci tvorbe lizofosfatidne kisline (LPA) za zdravljenje npr. bolezni ledvic |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| UA118201C2 (uk) | 2013-11-26 | 2018-12-10 | Ф. Хоффманн-Ля Рош Аг | НОВИЙ ОКТАГІДРОЦИКЛОБУТА[1,2-c;3,4-c']ДИПІРОЛ-2-ІЛ |
| MX374120B (es) * | 2014-03-05 | 2025-03-05 | Univ Tokyo | Compuestos derivados de carboxamida y el uso de los mismos para controlar endoparásitos en mamíferos. |
| AU2015224926B2 (en) * | 2014-03-05 | 2019-07-18 | Nihon Nohyaku Co., Ltd. | Endoparasite control agent |
| EA032357B1 (ru) | 2014-03-26 | 2019-05-31 | Ф. Хоффманн-Ля Рош Аг | Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
| CA2937616A1 (en) | 2014-03-26 | 2015-10-01 | F. Hoffmann-La Roche Ag | Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| PE20180479A1 (es) | 2015-09-04 | 2018-03-07 | Hoffmann La Roche | Nuevos derivados de fenoximetilo |
| EP3353176B1 (en) | 2015-09-24 | 2022-01-19 | F. Hoffmann-La Roche AG | Bicyclic compounds as atx inhibitors |
| AU2016328535A1 (en) | 2015-09-24 | 2017-11-09 | F. Hoffmann-La Roche Ag | Bicyclic compounds as ATX inhibitors |
| EP3353178B1 (en) | 2015-09-24 | 2021-07-14 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| JP6845230B2 (ja) | 2015-09-24 | 2021-03-17 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | デュアルatx/ca阻害剤としての新規な二環式化合物 |
| ES2884073T3 (es) * | 2016-11-11 | 2021-12-10 | Bayer Animal Health Gmbh | Nuevos derivados antihelmínticos de quinolina-3-carboxamida |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ.ホフマン-ラ ロシュ アーゲー | Atxインヒビターとしての新規二環式化合物 |
| CN110392679B (zh) | 2017-03-16 | 2023-04-07 | 豪夫迈·罗氏有限公司 | 可用作双重atx/ca抑制剂的杂环化合物 |
| AU2018311019B2 (en) * | 2017-08-04 | 2022-05-26 | Elanco Animal Health Gmbh | Quinoline derivatives for treating infections with helminths |
| US11040945B2 (en) | 2017-12-06 | 2021-06-22 | Lin Bioscience Pty Ltd. | Tubulin inhibitors |
| KR20200099548A (ko) | 2017-12-15 | 2020-08-24 | 바이엘 애니멀 헬스 게엠베하 | 구충제 4-아미노-퀴놀린-3-카르복스아미드 유도체를 제조하는 방법 |
| EP3790874B1 (en) * | 2018-05-09 | 2023-03-15 | Bayer Animal Health GmbH | Anthelmintic quinoline derivatives |
| AR117169A1 (es) | 2018-11-28 | 2021-07-14 | Bayer Ag | (tio)amidas de piridazina como compuestos fungicidas |
| UY38623A (es) | 2019-03-29 | 2020-10-30 | Syngenta Crop Protection Ag | Compuestos de diazina-amida activos como pesticidas |
| EP4146628A1 (en) | 2020-05-06 | 2023-03-15 | Bayer Aktiengesellschaft | Pyridine (thio)amides as fungicidal compounds |
| BR112022023012A2 (pt) | 2020-05-12 | 2022-12-20 | Bayer Ag | (tio)amidas de triazina e pirimidina como compostos fungicidas |
| EP4153566A1 (en) | 2020-05-19 | 2023-03-29 | Bayer CropScience Aktiengesellschaft | Azabicyclic(thio)amides as fungicidal compounds |
| EP4156936A1 (en) | 2020-05-27 | 2023-04-05 | Bayer Aktiengesellschaft | Active compound combinations |
| CN111943886B (zh) * | 2020-08-07 | 2022-02-08 | 华中师范大学 | 一类取代吡啶化合物及其制备方法 |
| CN113265385B (zh) * | 2021-05-25 | 2022-05-20 | 西南大学 | 构树抗菌蛋白BpChiI及其重组表达载体和提高植物对黄萎病抗性中的应用 |
| US20250064060A1 (en) | 2021-11-03 | 2025-02-27 | Bayer Aktiengesellschaft | Bis(hetero)aryl thioether (thio)amides as fungicidal compounds |
| WO2025026281A1 (zh) * | 2023-07-31 | 2025-02-06 | 江苏中旗科技股份有限公司 | 含突烯片段的化合物及其应用、用于防治线虫和真菌的农药、防治线虫和真菌的方法 |
| CN116947749B (zh) * | 2023-09-18 | 2023-12-01 | 帕潘纳(北京)科技有限公司 | 一类酰胺类化合物及其应用 |
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| TWI435863B (zh) * | 2006-03-20 | 2014-05-01 | Nihon Nohyaku Co Ltd | N-2-(雜)芳基乙基甲醯胺衍生物及含該衍生物之蟲害防治劑 |
| AU2012224015B2 (en) * | 2011-03-02 | 2017-04-13 | Nihon Nohyaku Co., Ltd. | Internal parasiticide |
| TWI654180B (zh) * | 2012-06-29 | 2019-03-21 | 美商艾佛艾姆希公司 | 殺真菌之雜環羧醯胺 |
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- 2014-11-24 RU RU2016125306A patent/RU2016125306A/ru unknown
- 2014-11-24 EP EP14802067.0A patent/EP3073827A1/en not_active Withdrawn
- 2014-11-24 CA CA2931265A patent/CA2931265A1/en not_active Abandoned
- 2014-11-24 UY UY0001035853A patent/UY35853A/es not_active Application Discontinuation
- 2014-11-24 CN CN201480073760.3A patent/CN106061255A/zh active Pending
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- 2014-11-24 TW TW103140581A patent/TW201609650A/zh unknown
- 2014-11-24 JP JP2016554909A patent/JP2016540832A/ja not_active Withdrawn
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| WO2015078800A1 (en) | 2015-06-04 |
| RU2016125306A (ru) | 2018-01-09 |
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| US20170044104A1 (en) | 2017-02-16 |
| ZA201603549B (en) | 2019-04-24 |
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| UY35853A (es) | 2015-06-30 |
| AR098475A1 (es) | 2016-06-01 |
| MX2016006841A (es) | 2016-12-07 |
| EP3073827A1 (en) | 2016-10-05 |
| CN106061255A (zh) | 2016-10-26 |
| AU2014356673B2 (en) | 2018-04-12 |
| CA2931265A1 (en) | 2015-06-04 |
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