TWI402035B - 具殺昆蟲活性之化合物組合物(刺芒柄花素+殺昆蟲劑) - Google Patents
具殺昆蟲活性之化合物組合物(刺芒柄花素+殺昆蟲劑) Download PDFInfo
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- TWI402035B TWI402035B TW096145059A TW96145059A TWI402035B TW I402035 B TWI402035 B TW I402035B TW 096145059 A TW096145059 A TW 096145059A TW 96145059 A TW96145059 A TW 96145059A TW I402035 B TWI402035 B TW I402035B
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Classifications
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
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- A—HUMAN NECESSITIES
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Description
本發明係有關新穎之活性化合物組合物,其第一,由刺芒柄花素,其次,由已知之殺昆蟲活性化合物所組成。彼等活性化合物組合物高度適用於防治不欲之動物害物,例如昆蟲或蜱蟎,以及植物寄生性線蟲。
業界已知具下式(I)之刺芒柄花素,
一種由紅花苜蓿(Trifolium pratens
)產生之異黃酮,促進有用植物之根生長(US 5,002,603)。
再者,已知許多氯菸鹼醯基類、磷酸酯類、胺基甲酸酯類、雜環類、有機錫化合物、苯甲醯服類與擬除蟲菊酯類具有殺昆蟲、殺蟎與殺線蟲性質(參照,例如,EP 0 192 060、US 2,758,115、US 3,309,266、GB 1,181,657、WO 93/22297 A1、WO 93/10083 A1、DE 26 41 343 A1、EP 347 488 A1、EP 210 487 A1、US 3,264,177與EP 234 045 A2)。然而,彼等化合物之活性並非各方面都令人滿意。
令人驚奇地,頃發現刺芒柄花素增加殺昆蟲、殺蟎或殺線蟲活性化合物之活性。
再者,令人驚奇地,頃發現殺昆蟲、殺蟎或殺線蟲活性化合物增加以刺芒柄花素處理的作物植物之產量或生長,超越單獨以刺芒柄花素處理或單獨以殺昆蟲、殺蟎或殺線蟲活性化合物處理之效果或超越兩個個別活性之總和。
本發明頃提供具有極佳防治昆蟲、蜱蟎或植物寄生性線蟲性質之新穎之活性化合物組合物,除了刺芒柄花素之外,其含有選自下述第(2)至(24)組之至少一種活性化合物。第(2)組 乙醯膽鹼受體促效劑/拮抗劑(舉例而言,如,氯菸鹼醯基類/新菸鹼類;第(3)組 乙醯膽鹼酯酶(AChE)抑制劑(舉例而言,如,胺基甲酸酯類與有機磷酸酯類);第(4)組 鈉通道調節劑/電壓依賴性鈉通道封阻劑(舉例而言,如,擬除蟲菊酯類與二類);第(5)組 乙醯膽鹼受體調節劑(舉例而言,如,賜諾辛類(spinosyns));第(6)組 GABA調控之氯化物通道之拮抗劑(舉例而言,如,環二烯有機氯類與苯基吡唑類);第(7)組 氯化物通道活化劑(舉例而言,如,滅停類(mectins));第(8)組 青春激素模擬物;第(9)組 蛻皮激素促效劑/干擾劑(舉例而言,如,二醯基肼類);第(10)組 幾丁質生合成抑制劑(舉例而言,如,苯甲醯基脲類);第(11)組 氧化性磷酸化作用抑制劑、ATP干擾劑(舉例而言,如,有機錫化合物);第(12)組 利用干擾H-質子梯度而作用之氧化性磷酸化作用去偶聯劑(舉例而言,如,吡咯類與二硝基苯酚類);第(13)組 側鏈-I電子傳遞抑制劑(舉例而言,如,METI類);第(14)組 側鏈-II電子傳遞抑制劑;第(15)組 側鏈-III電子傳遞抑制劑;第(16)組 昆蟲腸膜之微生物干擾劑;第(17)組 脂肪合成抑制劑(舉例而言,如,4-羥乙醯乙酸內酯類與四聚酸類(tetramic acids));第(18)組 羧醯胺類;第(19)組 章魚胺作用促效劑;第(20)組 受鎂激發的ATP酵素之抑制劑;第(21)組 酞醯胺類;第(22)組 沙蠶毒素類似物;第(23)組 生物劑、激素或費洛蒙素;第(24)組 具有未知或不明確作用機制之活性化合物(舉例而言,如,燻劑、選擇性抗飼養劑與蟎生長抑制劑)。
令人驚奇地,根據本發明活性化合物組合物之殺昆蟲或殺蟎活性遠高於個別活性化合物活性之總和。因此,存在不可預見之效力,而非僅為諸活性之加成。
除了至少一種式(I)之異戊基碳醯胺苯化合物之外,根據本發明之活性化合物組合物含有第(2)至(24)組之至少一種活性化合物。
第(2)至(24)組之活性化合物包含下文列舉之大量可能混合搭擋。彼等活性化合物多數係市售可得及/或列入Pesticide Manual(The Pesticide Manual,13th edition,Editor:CDS Tomlin,British Crop Protection Council,ISBN 1 901396 13 4)。目前不可得或未列入Pesticide Manual中之活性化合物以其IUPAC名稱明確地確認。
第(2)組之乙醯膽鹼受體促效劑/拮抗劑具體而言包括下述活性化合物:(2.1)氯菸鹼醯基類/新菸鹼類(例如醋密普利(aceta miprid)、可尼丁(clothianidin)、達特喃(dinotefuran)、益達胺(imidacloprid)、尼天爛(nitenpyram)、尼賽淨(nithiazine)、噻洛利(thiacloprid)、賽美索佔(thiamethoxam)、益達替(imidaclotiz)((2E)-1-[(2-氯-1,3-噻唑-5-基)甲基]-N-硝基咪唑啶-1-亞胺)、AKD 1022((2E)-1-[(2-氯-1,3-噻唑-5-基)甲基]-3,5-二甲基-N-硝基-1,3,5-三喃-2-亞胺));(2.2) 菸鹼類、免速達(bensultap)、培丹(cartap)。
根據本發明之活性化合物組合物較佳為包含第(2)組之下述乙醯膽鹼受體促效劑/拮抗劑:(2.1.1)可尼丁(2.1.2)益達胺(2.1.3)噻洛利(2.1.4)賽美索佔(2.1.5)醋密普利(2.1.6)達特喃(2.1.7)尼天爛(2.1.8)益達替。
根據本發明之活性化合物組合物特佳為包含第(2)組之下述乙醯膽鹼受體促效劑/拮抗劑:(2.1.1)可尼丁(2.1.2)益達胺(2.1.3)噻洛利(2.1.4)賽美索佔(2.1.5)醋密普利。
第(3)組之乙醯膽鹼酯酶(AChE)抑制劑具體而言包括下述活性化合物:(3.1)胺基甲酸酯類(例如亞拉克(alanycarb)、得滅克(aldicarb)、亞喜克(aldoxycarb)、丙烯威(allyxycarb)、滅害威(aminocarb)、免敵克(bendiocarb)、免扶克(benfuracarb)、必克蝨(bufencarb)、布塔克(butacarb)、佈嘉信(butocarboxim)、丁氧喜信(butoxycarboxim)、加保利(carbaryl)、加保扶(carbofuran)、丁基加保扶(carbosulfan)、氯索克(chloethocarb)、大滅替爛(dimetilan)、愛殺克(ethiofencarb)、丁基滅必蝨(fenobucarb)、芬硫克(fenothiocarb)、覆滅滿(formetanate)、護拉克(furathiocarb)、滅必蝨(isoprocarb)、斯美地(metam-sodium)、滅賜克(methiocarb)、納乃得(methomyl)、治滅蝨(metolcarb)、歐殺滅(oxamyl)、磷克(phosphocarb)、比加普(pirimicarb)、普滅克(promecarb)、安丹(propoxur)、硫敵克(thiodicarb)、硫化隆(thiofanox)、三雜滅(triazamate)、三美克(trimethacarb)、XMC、滅爾蝨(xylylcarb));(3.2)有機磷酸酯類(例如歐殺松(acephate)、雜美松(azamethiphos)、谷速松(azinphos)(-甲基、-乙基)、溴磷松(bromophos)-乙基、溴芬松(bromfenvinfos)-甲基、布硫松(butathiofos)、卡杜松(cadusafos)、加芬松(carbophenothion)、氯乙氧松(chlorethoxyfos)、氯芬松(chlorfenvinphos)、克美松(chlormephos)、陶斯松(chlorpyrifos)(-甲基/-乙基)、可馬松(coumaphos)、施力松(cyanofenphos)、氰基松(cyanophos)、滅賜松(demeton)-S-甲基、滅賜松-S-甲基碸、得拉松(dialifos)、大利松(diazinon)、二氯芬松(dichlofenthion)、二氯松(dichlorvos)/DDVP、雙特松(dicrotophos)、大滅松(dimethoate)、二甲基芬松(dimethylvinphos)、二苯松(dioxabenzofos)、二硫松(disulfoton)、EPN、愛殺松(ethion)、普伏松(ethoprophos)、益多松(etrimfos)、胺磺磷(famphur)、芬滅松(fenamiphos)、撲滅松(fenitrothion)、繁福松(fensulfothion)、芬殺松(fenthion)、氟吡唑松(flupyrazofos)、大福松(fonofos)、福木松(formothion)、松美爛(fosmethilan)、松賽殺(fosthiazate)、飛達松(heptenophos)、碘芬松(iodofenphos)、丙基喜樂松(iprobenfos)、依殺松(isazofos)、亞芬松(isofenphos)、O-水楊酸異丙酯、加福松(isoxathion)、馬拉松(malathion)、滅加松(mecarbam)、滅克松(methacrifos)、達馬松(methamidophos)、滅大松(methidathion)、美文松(mevinphos)、亞素靈(monocrotophos)、那列(naled)、歐滅松(omethoate)、滅多松(oxydemeton)-甲基、巴拉松(-甲基/-乙基)、賽達松(phenthoate)、福瑞松(phorate)、裕必松(phosalone)、益滅松(phosmet)、福賜米松(phosphamidon)、磷克(phosphocarb)、巴賽松(phoxim)、亞特松(pirimiphos)(-甲基/-乙基)、佈飛松(profenofos)、加護松(propaphos)、撲達松(propetamphos)、普硫松(prothiofos)、飛克松(prothoate)、白克松(pyraclofos)、必芬松(pyridaphenthion)、必達松(pyridathion)、拜裕松(quinalphos)、西布松(sebufos)、硫帖(sulfotep)、沙洛松(sulprofos)、得寧松(tebupirimifos)、得美松(temephos)、托福松(terbufos)、樂本松(tetrachlorvinphos)、硫滅松(thiometon)、三落松(triazophos)、三氯松(triclorfon)、繁米松(vamidothion))。
根據本發明之活性化合物組合物較佳為包含第(3)組之下述乙醯膽鹼酯酶(AChE)抑制劑:(3.1.1)滅賜克(3.1.2)硫敵克(3.1.3)普伏松(3.1.4)得滅克(3.1.5)芬滅松(3.2.1)得寧松(3.2.2)卡杜松(3.2.3)歐殺滅(3.2.4)松賽殺陶斯松(-甲基/-乙基)。
根據本發明之活性化合物組合物特佳為包含第(3)組之下述乙醯膽鹼酯酶(AChE)抑制劑:(3.1.1)滅賜克(3.1.2)硫敵克(3.1.3)得滅克(3.2.1)普伏松(3.2.2)芬滅松。
第(4)組之鈉通道調節劑/電壓依賴性鈉通道封阻劑具體而言包括下述活性化合物:(4.1)擬除蟲菊酯類(例如亞那寧(acrinathrin)、亞烈寧(allethrin)(d-順式-反式、d-反式)、β-賽扶寧(beta-cyfluthrin)、畢芬寧(bifenthrin)、百亞烈寧(bioallethrin)、百亞烈寧-S-環戊基-異構物、拜殺滅寧(bioethanomethrin)、拜帕滅寧(biopermethrin)、百烈滅寧(bioresmethrin)、克瓦寧(chlovaporthrin)、順式賽滅寧(cis-cypermethrin)、順式烈滅寧(cis-resmethrin)、順式帕滅寧(cis-permethrin)、克洛賽寧(clocythrin)、環普洛寧(cycloprothrin)、賽扶寧、賽鹵寧(cyhalothrin)、賽滅寧(cypermethrin)(α-、β-、θ-、ξ-)、賽酚寧(cyphenothrin)、D DT、第滅寧(deltamethrin)、安潘寧(empenthrin)(1R-異構物)、益化利(esfenvalerate)、益多芬洛(etofenprox)、芬氟寧(fenfluthrin)、芬普寧(fenpropathrin)、芬拜寧(fenpyrithrin)、芬化利(fenvalerate)、護溴賽寧(flubrocythrinate)、護賽寧(flucythrinate)、福芬洛(flufenprox)、福美寧(flumethrin)、福利松(fluvalinate)、護芬洛(fubfenprox)、γ-賽鹵寧、依普寧(imiprothrin)、剋特寧(kadethrin)、λ-賽鹵寧、美托寧(metofluthrin)、百滅寧(permethrin)(順式-、反式-)、酚丁滅蝨(phenothrin)(1R-反式異構物)、普亞列寧(prallethrin)、普氟寧(profluthrin)、普三芬(protrifenbute)、拜滅寧(pyresmethrin)、烈滅寧、RU 15525、西拉福芬(silafluofen)、τ-福利松、得福寧(tefluthrin)、環戊烯丙菊酯(terallethrin)、治滅寧(tetramethrin)(1R-異構物)、泰賽寧(tralocythrin)、泰滅寧(tralomethrin)、拜富寧(transfluthrin)、ZXI 8901、除蟲菊酯類(除蟲菊粉));(4.2)二類(例如因得克(indoxacarb))。
根據本發明之活性化合物組合物較佳為包含第(4)組之下述鈉通道調節劑/電壓依賴性鈉通道封阻劑:(4.1.1)β-賽扶寧(4.1.2)賽扶寧(4.1.3)第滅寧(4.1.4)得福寧(4.1.5)畢芬寧(4.2.1)因得克。
根據本發明之活性化合物組合物特佳為包含第(4)組之下述鈉通道調節劑/電壓依賴性鈉通道封阻劑:(4.1.1)β-賽扶寧(4.1.2)賽扶寧(4.1.3)第滅寧(4.1.4)得福寧(4.2.1)因得克。
第(5)組之乙醯膽鹼受體調節劑具體而言包括下述活性化合物:(5.1)賜諾辛類(spinosyns)(例如賜諾殺(spinosad));得自Dow之新穎賜諾辛。
根據本發明之活性化合物組合物較佳為包含第(5)組之下述乙醯膽鹼受體調節劑:(5.1.1)賜諾殺(5.1.2)XDE-175係具下式(II)之化合物(自WO 97/00265 A1、US 6001981與Pest Manag.Sci.57,177-185,2001得知)
第(6)組之GABA調控之氯化物通道之拮抗劑具體而言包括下述活性化合物:(6.1)安殺番(endosulphan)除外之環二烯有機氯類(例如毒殺芬(camphechlor)、克氯丹(chlordane)、γ-HCH、HCH、飛佈達(heptachlor)、靈丹(lindane)、甲氧飛佈達(methoxychlor));(6.2)苯基吡唑類(例如乙醯普洛(acetoprole)、愛殺普洛(ethiprole)、芬普尼(fipronil)、繁尼洛(vaniliprole))。
根據本發明之活性化合物組合物較佳為包含第(6)組之下述GABA調控之氯化物通道之拮抗劑:(6.2.1)芬普尼(6.2.2)愛殺普洛。
第(7)組之氯化物通道活化劑具體而言包括下述活性化合物:(7.1)滅停類(mectins)(例如阿巴汀(abamectin)、亞滅停(avermectin)、益滅停(emamectin)、因滅汀(emamectin-benzoate)、愛滅停(ivermectin)、密貝停(milbemectin)、米貝黴素(milbemycin))。
根據本發明之活性化合物組合物較佳為包含第(7)組之下述氯化物通道活化劑:(7.1.1)因滅汀(7.1.2)亞滅停。
第(8)組之青春激素模擬物具體而言包括下述活性化合物:二芬爛(diofenolan)、依普芬爛(epofenonane)、芬諾克(fenoxycarb)、氫普寧(hydroprene)、基諾普寧(kinoprene)、美索普寧(methoprene)、百利普芬(pyriproxifen)、三普寧(triprene)。
根據本發明之活性化合物組合物較佳為包含第(8)組之下述青春激素模擬物:(8.1.1)百利普芬。
第(9)組之蛻皮激素促效劑/干擾劑具體而言包括下述活性化合物:(9.1)二醯基肼類(例如克芬諾(chromafenozide)、鹵芬諾(halofenozide)、甲氧芬諾(methoxyfenozide)、得芬諾(tebufenozide))。
根據本發明之活性化合物組合物較佳為包含第(9)組之下述蛻皮激素促效劑/干擾劑:(9.1.1)甲氧芬諾。
第(10)組之幾丁質生合成抑制劑具體而言包括下述活性化合物:(10.1)苯甲醯基脲類(例如雙三福隆(bistrifluron)、克福隆(chlofluazuron)、二福隆(diflubenzuron)、扶助隆(fluazuron)、福環隆(flucycloxuron)、福芬隆(flufenoxuron)、六伏隆(hexaflumuron)、路芬隆(lufenuron)、諾瓦隆(novaluron)、諾維隆(noviflumuron)、噴福隆(penfluron)、得福隆(teflubenzuron)、三福隆(triflumuron));(10.2)布芬淨(buprofezin);(10.3)賽滅淨(cyromazine)。
根據本發明之活性化合物組合物較佳為包含第(10)組之下述幾丁質生合成抑制劑:(10.1.1)三福隆(10.1.2)福芬隆。
第(11)組之氧化性磷酸化作用抑制劑、ATP干擾劑具體而言包括下述活性化合物:(11.1)肽芬隆(diafenthiuron):(11.2)有機錫化合物(例如亞環錫(azocyclotin)、錫蟎丹(cyhexatin)、芬佈賜(fenbutatin oxide))。
第(12)組之利用干擾H-質子梯度而作用之氧化性磷酸化作用去偶聯劑具體而言包括下述活性化合物:(12.1)吡咯類(例如克凡派(chlorfenapyr));(12.2)二硝基苯酚類(例如必諾派(binapacyrl)、大脫蟎(dinobuton)、白粉克(dinocap)、DNOC)。
第(13)組之側鏈-I電子傳遞抑制劑具體而言包括下述活性化合物:(13.1)METI類(例如芬殺蟎(fenazaquin)、芬普蟎(fenpyroximate)、畢米芬(pyrimidifen)、畢達本(pryidaben)、得芬拜(tebufenpyrad)、托芬拜(tolfenpyrad));(13.2)愛美松(hydramethylnone);(13.3)大克蟎(dicofol)。
根據本發明之活性化合物組合物較佳為包含第(13)組之下述側鏈-I電子傳遞抑制劑:(13.1.1)得芬拜(13.2.1)愛美松。
第(14)組之側鏈-II電子傳遞抑制劑具體而言包括下述活性化合物:(14.1.1)魚藤精(rotenone)。
第(15)組之側鏈-III電子傳遞抑制劑具體而言包括下述活性化合物:(15.1)亞醌蟎(acequinocyl)、嘧蟎酯(fluacrypyrim)。
第(16)組之昆蟲腸膜之微生物干擾劑具體而言包括下述活性化合物:(16.1)蘇力菌(Bacillus thuringiensis)菌株。
第(17)組之脂肪合成抑制劑具體而言包括下述活性化合物:(17.1)4-羥乙醯乙酸內酯類(例如螺旋二氯芬(spirodiclofen)、螺旋麥西芬(spiromesifen));(17.2)四聚酸類(tetramic acids)(例如3-(2,5-二甲基苯基)-8-甲氧基-2-酮基-1-氮雜螺[4.5]癸-3-烯-4-基乙基碳酸酯(別名:碳酸3-(2,5-二甲基苯基)-8-甲氧基-2-酮基-1-氮雜螺[4.5]癸-3-烯-4-基乙酯,CAS-Reg.-No.:382608-10-8)與碳酸順式-3-(2,5-二甲基苯基)-8-甲氧基-2-酮基-1-氮雜螺[4.5]癸-3-烯-4-基乙酯,(CAS-Reg.-No.:203313-25-1))。
根據本發明之活性化合物組合物較佳為包含第(17)組之下述脂肪合成抑制劑:(17.1.1)螺旋二氯芬(17.1.2)螺旋麥西芬(17.2.1)碳酸3-(2,5-二甲基苯基)-8-甲氧基-2-酮基-1-氮雜螺[4.5]癸-3-烯-4-基乙酯。
第(18)組之羧醯胺類具體而言包括下述活性化合物:(18.1.1)福隆卡密(flonicamid)。
第(19)組之章魚胺作用促效劑具體而言包括下述活性化合物:(19.1.1)三亞蟎(amitraz)。
第(20)組之受鎂激發的ATP酵素之抑制劑具體而言包括下述活性化合物:(20.1.1)歐蟎多(propargite)。
第(21)組之酞醯胺類具體而言包括下述活性化合物:(21.1.1)N2
-[1,1-二甲基-2-(甲基磺醯基)乙基]-3-碘-N1
-[2-甲基-4-[1,2,2,2-四氟-1-(三氟甲基)乙基]苯基]-1,2-苯二羧醯胺(氟苯二醯胺(flubendiamide),CAS-Reg.-No.:272451-65-7)(21.1.2)具下式(III)之理那派(rynaxypyr)
第(22)組之沙蠶毒素類似物具體而言包括下述活性化合物:硫賜安(thiocyclam)草酸氫鹽、硫速達(thiosultap)-鈉。
第(23)組之生物劑、激素或昆蟲性激素具體而言包括下述活性化合物:雜拉錫(azadirachtin)、桿菌(Bacillus)屬、白僵菌(Beauveria)屬、蘋果蠹蛾激素、綠僵菌(Metarrhizium)屬、擬青黴菌(Paecilomyces)屬、蘇力菌素、輪枝孢(Verticillium)屬。
第(24)組之具有未知或不明確作用機制之活性化合物具體而言包括下述活性化合物:(24.1)燻劑(例如磷化鋁、甲基溴、硫醯氟);(24.2)選擇性抗飼養劑(例如冰晶石(cryolite)、福隆卡密、拜滅淨(pymetrozine));(24.3)蟎生長抑制劑(例如克洛芬淨(clofentezine)、益多康座(etoxazole)、合賽多(hexythiazox));(24.4)阿密氟美(amidoflumet)、苯洛賽(benclothiaz)、西脫蟎(benzoximate)、必芬那(bifenazate)、新殺蟎(bromopropylate)、布芬淨、滿離丹(chinomethionat)、殺蟲脒(chlordimeform)、克氯苯(chlorobenzilate)、氯化苦(chloropicrin)、克噻苯(clothiazoben)、環普寧(cycloprene)、賽福芬(cyflumetofen)、二賽尼(dicyclanil)、芬殺寧(fenoxacrim)、芬三尼(fentrifanil)、福苯明(flubenzimine)、福芬寧(flufenerim)、福添淨(flutenzin)、戈昔流(gossyplure)、愛美松、扎波流(japonilure)、滅多松(metoxadiazone)、石油、協力精(piperonyl butoxide)、油酸鉀、百福洛(pyrafluprole)、百大力(pyridalyl)、百利洛(pyriprole)、沙福拉密(sulphluramid)、得脫蟎(tetradifon)、殺蟎硫醚(tetrasul)、三拉森(triarathene)、維布亭(verbutin)、再者,化合物丙基胺甲酸3-甲基苯酯(速滅威(tsumacide)Z)、化合物3-(5-氯-3-吡啶基)-8-(2,2,2-三氟乙基)-8-氮雜雙環[3.2.1]辛烷-3-甲腈(CAS-Reg.No.185982-80-3)與對應之3-內向-異構物(CAS-Reg.No.185984-60-5)(參照WO-96/37494、WO-98/25923)、以及包含殺昆蟲活性植物抽取物、線蟲、真菌或病毒之製劑。
根據本發明之特佳組合物如下文表1所示。
根據本發明,除了刺芒柄花素之外,亦可使用其鹽,特別是其鹼金屬鹽。
此外,彼等活性化合物組合物於混合物中亦可包含進一步之殺真菌、殺蟎或殺昆蟲活性成分。
根據本發明活性化合物組合物中之活性化合物若存在特定重量比,則其增效效應特別顯著。然而,活性化合物組合物中諸活性化合物之重量比可於相當寬廣範圍內有所不同。一般而言,根據本發明之組合物含有下文表中所述之較佳混合比率之式(I)活性化合物與其混合搭檔,其中混合比率係以重量比計。
該比率被瞭解為意指刺芒柄花素:混合搭檔。
根據本發明之活性化合物組合物適用於防治動物害物(較佳為節肢動物與線蟲,特別是於農業、動物防疫、森林、貯存產品與物料之保護、及於保健領域中所見之線蟲與昆蟲);彼等對於一般敏感與抗性品系及所有或某些發育階段均具活性。上述害物包括:屬於等足目(Isopoda)者,例如,海蛆屬之Oniscus asellus
、鼠婦(Armadillidium vulgare
)、Porcellio scaber
;屬於雙足目(Diplopoda)者,例如,Blaniulus guttulatus
;屬於唇足目(Chilopoda)者,例如,地蜈蚣屬之Geophilus carpophagus
、蚰蜒(Scutigera
)屬;屬於綜合目(Symphyla)者,例如,Scutigerella immaculata
;屬於纓尾目(Thysanura)者,例如,西洋衣魚(Lepisma saccharina
);屬於彈尾目(Collembola)者,例如,棘跳蟲屬之Onychiurus armatus
;屬於直翅目(Orthoptera)者,例如,家蟋蟀(Acheta domesticus
)、螻站(Gryllotalpa
)屬、熱帶飛蝗(Locusta migratoria migratorioides
)、蚱蜢(Melanoplus
)屬、群居蚱蜢(Schistocerca gregaria
);屬於蠊目(Blattaria)者,例如,東方蠊(Blatta orientalis
)、馬得拉蠊(Leucophaea maderae
)、德國小蠊(Blattella germanica
);屬於革翅目(Dermaptera)者,例如,歐洲球螋(Forficula auricularia
);屬於等翅目(Isoptera)者,例如,網白蟻(Reticulitermes
)屬;屬於蝨目(Phthiraptera)者,例如,人體蝨(Pediculus humanus corporis
)、血蝨(Haematopinus
)屬、毛蝨(Linognathus
)屬、嚙毛蝨(Trichodectes
)屬、羊蝨(Dalmalinia
)屬;屬於纓翅目(Thysanoptera)者,例如,溫室條薊馬(Hercinothrips femoralis
)、蔥薊馬(Thrips tabaci
)、南黃薊馬(Thrips palmi
)、苜蓿薊馬(Frankliniella accidentalis
);屬於異翅亞目(Heteroptera)者,例如,褐盾蝽(Eurygaster
)屬、間型紅蝽(Dysdercus intermedius
)、甜菜擬網蝽(Piesma quadrata
)、臭蟲(Cimex lectularius
)、錐鼻蟲屬之錐蝽(Rhodnius prolixus
)、獵蝽(Triatoma
)屬;屬於同翅目(Homoptera)者,例如,甘藍粉虱(Aleurodes brassicae
)、蔥粉虱(Bemisia tabaci
)、温室粉虱(Trialeurodes vaporariorum
)、棉蚜(Aphis gossypii
)、甘藍蚜(Brevicoryne brassicae
)、茶藨隱瘤額蚜(Cryptomyzus ribis
)、蚕豆蚜(Aphis fabae
)、蘋果蚜(Aphis pomi
)、蘋果棉蚜(Eriosoma lanigerum
)、桃大尾蚜(Hyalopterus arundinis
)、葡萄根瘤蚜(Phylloxera vastatrix
)、癭棉蚜(Pemphigus
)屬、麥長管蚜(Macrosiphum avenae
)、瘤額蚜(Myzus
)屬、Phorodon humuli
、粟縊管蚜(Rhopalosiphum padi
)、葉蟬(Empoasca
)屬、二葉葉蟬(Euscelis bilobatus
)、黑尾葉蟬(Nephotettix cincticeps
)、李蠟蚧(Lecanium corni
)、工脊硬蚧(Saissetia oleae
)、稻灰飛虱(Laodelphax striatellus
)、稻褐飛虱(Nilaparvata lugens
)、紅圓蚧(Aonidiella aurantii
)、常春圓蚧(Aspidiotus hederae
)、粉蚧(Pseudococcus
)屬、木虱(Psylla
)屬;屬於鱗翅目(Lepidoptera)者,例如,紅鈴蟲(Pectinophora gossypeilla
)、松尺蠖(Bupalus piniarius
)、Cheimatobia brumata
、細蛾屬之Lithocolletis blancardella
、櫻桃巢蛾(Hyponomeuta padella
)、小菜蛾(Plutella xylostella
)、天幕毛蟲(Malacosoma neustria
)、褐尾蛾(Euproctis chrysorrhoea
)、毒蛾(Lymantria
)屬、棉葉穿孔潛蛾(Bucculatrix thurberiella
)、柑橘潛夜蛾(Phyllocnistis citrella
)、地老虎(Agrotis
)屬、切根蟲(Euxoa
)屬、夜蛾(Feltia
)屬、埃及金剛鑽(Earias insulana
)、夜蛾(Heliothis
)屬、甘藍夜蛾(Mamestra brassicae
)、Panolis flammea
、黏蟲(Spodoptera
)屬、粉紋夜蛾(Trichoplusia ni
)、蘋果蠹蛾(Carpocapsa pomonella
)、粉蝶(Pieris
)屬、螟(Chilo
)屬、野螟屬之Pyrausta nubilalis
、地中海粉斑螟(Ephestia kuehniella
)、大蠟螟(Galleria mellonella
)、袋衣蛾(Tineola bisselliella
)、網衣蛾(Tinea pellionella
)、褐織葉蛾(Hofmannophila pseudospretella
)、捲葉蛾屬之Cacoecia podana
、Capua reticulana
、雲杉捲夜蛾(Choristoneura fumiferana
)、葡萄果蠹蛾(Clysia ambiguella
)、茶捲夜蛾(Homona magnanima
)、櫟綠捲葉蛾(Tortrixviridana
)、捲螟(Cnaphalocerus
)屬、稻負泥蟲(Oulema oryzae
);屬於鞘翅目(Coleoptera)者,例如,家具竊蠹(Anobium punctatum
)、穀蠹(Rhizopertha dominica
)、豆象屬之Bruchidius obtectus
、大豆象(Acanthoscelides obtectus
)、家天牛(Hylotrupes bajulus)
、Agelastica alni
、馬鈴薯甲蟲(Leptinotarsa decemlineata
)、芥菜猿葉蟲(Phaedon cochleariae
)、葉甲(Diabrotica
)屬、油菜蘭跳甲(Psylliodes chrysocephala
)、墨西哥豆瓢蟲(Epilachna varivestis
)、寶螺(Atomaria
)屬、鋸穀盜(Oryzaephilus surinamensis
)、象甲(Anthonomus
)屬、象鼻蟲(Sitophilus
)屬、深溝象甲(Otiorrhynchus sulcatus
)、香蕉球莖象鼻蟲(Cosmopolites sordidus
)、甘藍莢象甲(Ceuthorrhynchus assimilis
)、苜蓿葉象甲(Hypera postica
)、皮蠹(Dermestes
)屬、斑皮蠹(Trogoderma
)屬、皮蠹(Anthrenus
)屬、黑皮蠹(Attagenus
)屬、粉蠹(Lyctus
)屬、花粉甲蟲(Meligethes aeneus
)、蜘甲(Ptinus
)屬、金黃珠甲(Niptus hololeucus
)、麥珠甲(Gibbium psylloides
)、粉甲(Tribolium
)屬、黃粉甲(Tenebrio molitor
)、叩甲(Agriotes
)屬、金針蟲(Conoderus
)屬、鰓角金龜(Melolontha melolontha
)、六月金龜(Amphimallon solstitialis
)、草蛆(Costelytra zealandica
)、稻象甲(Lissorhoptrus oryzophilus
);屬於膜翅目(Hymenoptera)者,例如,鋸角葉蜂(Diprion
)屬、葉蜂(Hoplocampa
)屬、蟻(Lasius
)屬、廚蟻(Monomorium pharaonis
)、胡蜂(Vespa
)屬;屬於雙翅目(Diptera)者,例如,伊蚊(Aedes
)屬、按蚊(Anopheles
)屬、庫蚊(Culex
)屬、黃猩猩果蠅(Drosophila melanogaster
)、家蠅(Musca
)屬、廄蠅(Fannia
)屬、紅頭麗蠅(Calliphora erythrocephala
)、綠蠅(Lucilia
)屬、麗蠅(Chrysomyia
)屬、疽蠅(Cuterebra
)屬、胃蠅(Gastrophilus
)屬、Hyppobosca
屬、螫蠅(Stomoxys
)屬、狂蠅(Oestrus
)屬、皮蠅(Hypoderma
)屬、牛虻(Tabanus
)屬、夜蟬(Tannia
)屬、毛蚊屬之Bibio hortulanus
、瑞典麥杵蠅(Oscinella frit
)、蠅(Phorbia
)屬、甜菜潛葉蠅(Pegomyia hyoscyami
)、地中海實蠅(Ceratitis capitata
)、油橄欖實蠅(Dacus oleae
)、歐洲大蚊(Tipula paludosa
)、(Hylemyia
)屬、潛蠅(Liriomyza
)屬;屬於蚤目(Siphonaptera)者,例如,東方鼠蚤(Xenopsyolla cheopis
)、蚤(Ceratophyllus
)屬;屬於蛛形綱(Arachnida)者,例如,中東金蠍(Scorpio maurus
)、黑寡婦球腹蛛(Latrodectus mactans
)、粗腳粉蟎(Acarus siro
)、隱喙蜱(Argas
)屬、鈍喙蜱(Ornithodoros
)屬、雞皮刺蟎(Dermanyssus gallinae
)、蠟蚧癭蟎(Eriophyes ribis
)、柑橘銹蟎(Phyllocoptruta oleivora
)、牛蜱(Boophilus
)屬、扇頭蜱(Rhipicephalus
)屬、花蜱(Amblyomma
)屬、璃眼蜱(Hyalomma
)屬、硬蜱(Ixodes
)屬、癢蟎(Psoroptes
)屬、食皮蚧蟲(Chorioptes
)屬、疥蟎(Sarcoptes
)屬、跗線蟎(Tarsonemus
)屬、苜蓿苔蟎(Bryobia praetiosa
)、全爪蟎(Panonychus
)屬、葉蟎(Tetranychus
)屬、半跗線蟎(Hemitarsonemus
)屬、偽葉蟎(Brevipalpus
)屬;植物寄生性線蟲包含,例如,根腐線蟲(Pratylenchus
)屬、穿孔線蟲(Radopholus similis
)、莖線蟲(Ditylenchus dipsaci
)、橘墊刃線蟲(Tylenchulus semipenetrans
)、包囊線蟲(Heterodera
)屬、包囊線蟲(Globodera
)屬、根瘤線蟲(Meloidogyne
)屬、葉芽線蟲(Aphelenchoides
)屬、長針線蟲(Longidorus
)屬、劍線蟲(Xiphinema
)屬、殘根線蟲(Trichodorus
)屬、松材線蟲(Bursaphelenchus
)屬。
活性化合物組合物可轉化成習知調配劑例如溶液、乳液、可濕性粉劑、懸浮液、粉劑、細粉劑、可溶性粉劑、粒劑、懸浮液-乳液濃縮物、與活性化合物一起浸漬之天然與合成物質、及於聚合物質中予以微膠囊化。
彼等調配劑係以已知方法製造,例如將活性化合物與增充劑(亦即,液體溶劑及/或固體載劑)混合,視需要使用界面活性劑(亦即,乳化劑及/或分散劑、及/或泡沫形成劑)。
若所用填充劑為水,則亦可,例如,使用有機溶劑作用輔助溶劑。本質上適當之液體溶劑為:芳族烴例如二甲苯、甲苯或烷基萘類;氯化芳族烴或氯化脂族烴例如氯苯類、氯乙烯類與二氯甲烷;脂族烴例如環己烷或鏈烷烴,例如礦物油餾分、礦物油與植物油;醇類例如丁醇或乙二醇及其醚和酯;酮類例如丙酮、甲基乙基酮、甲基異丁基酮或環己酮;強極性溶劑例如二甲基甲醯胺與二甲亞碸;或者水。
適當固體載劑為:舉例而言,銨鹽與細磨之天然礦物例如高嶺土、黏土、滑石粉、白堊、石英、綠坡縷石、蒙脫土或矽藻土,及細磨之合成物料例如細微分割之矽石、氧化鋁與矽酸鹽;用於粒劑之適當固體載劑為:舉例而言,經壓碎與分級之天然岩石例如方解石、大理石、浮石、海泡石及白雲石,或者無機與有機粗粉之合成粒劑,及有機物料例如鋸屑、椰殼、玉米穗及煙草稈之粒劑;適當之乳化劑及/或泡沫形成劑為:舉例而言,非離子性與陰離子性乳化劑例如聚氧乙烯脂肪酸酯類、聚氧乙烯脂肪醇醚類,例如烷基芳基聚乙二醇醚類、烷基磺酸酯類、烷基硫酸酯類、芳基磺酸酯類、或蛋白質水解物;適當之分散劑為:例如木質亞硫酸鹽廢液與甲基纖維素。
調配劑中可使用增黏劑例如羧甲基纖維素、呈粉劑、粒劑或膠乳形式之天然及合成聚合物,例如阿拉伯膠、聚乙烯醇及聚乙酸乙烯酯,或天然磷脂類例如腦-磷脂類與卵磷脂類,及合成磷脂類。其他可能的添加劑為礦物及植物油。
亦可使用著色劑例如無機色素,例如氧化鐵、氧化鈦與普魯士藍,及有機色料例如茜素色料、偶氮色料與金屬酞菁色料,及微量營養素例如鐵、錳、硼、銅、鈷、鉬與鋅等鹽。
調配劑通常含有0.1與95%重量比間,較佳為0.5與90%重量比間之活性化合物。
根據本發明之活性化合物組合物可呈其市售可用之調配劑及以彼等調配劑製備之諸使用形式(與其他活性化合物例如殺昆蟲劑、引誘劑、消毒劑、殺細菌劑、殺蟎劑、殺線蟲劑、殺真菌劑、生長調節物質或除草劑之混合物)存在。殺昆蟲劑包含,例如,磷酸酯類、胺基甲酸酯類、羧酸酯類、氯化烴、苯基脲類及由微生物產生之物質。
亦可為與其他已知活性化合物例如除草劑或與肥料及生長調節劑之混合物。
作為殺昆蟲劑用時,根據本發明之活性化合物組合物可進一步呈其市售可得之調配劑及以彼等調配劑製備之諸使用形式(與增效劑之混合物)存在。增效劑係增加活性化合物作用之化合物,惟所添加之增效劑本身不必具有活性。
以市售調配劑製備之使用形式之活性化合物含量可於寬廣範圍內有所不同。諸使用形式之活性化合物濃度可為0.0000001至95重量%活性化合物,較佳為0.0001至1重量%。
該等化合物係以適用於諸使用形式之習知方式使用。活性化合物組合物可就這樣、呈濃縮物形式或呈一般習知調配劑形式(例如粉劑、粒劑、溶液、懸浮液、乳液或糊劑)使用。
前述調配劑可以本質上已知之方法(例如利用混合活性化合物與至少一種溶劑或稀釋劑、乳化劑、分散劑及/或黏合劑或固色劑、防水劑;需要時使用乾燥劑與UV安定劑,及使用著色劑與色料及其他加工處理佐劑)予以製備。
用於保護木材與木料產品之殺昆蟲劑組成物或濃縮物含有濃度為0.0001至95重量%,特別是0.001至60重量%之根據本發明之活性化合物。
所用組成物或濃縮物之量視昆蟲品系與量及介質而不同。於各情形下,所用最適量可藉施用時之試驗系列予以測定。然而,一般而言,以擬保護之物料計,使用0.0001至20重量%,較佳為,0.001至10重量%,即足夠。
適當之溶劑及/或稀釋劑為有機化學溶劑或溶劑混合物及/或具低揮發性之任何油性或油型有機化學溶劑或溶劑混合物及/或極性有機化學溶劑或溶劑混合物及/或水,適當時,含有乳化劑及/或潤濕劑。
較喜使用之有機化學溶劑為蒸發值35以上及燃點30℃以上(較佳為45℃以上)之油性或油型溶劑。所使用之此等不溶於水、具低揮發性之油性或油型溶劑為適當礦物油或其芳族餾分或含礦物油之溶劑混合物,較佳為石油溶劑油、石油及/或烷基苯。
以使用沸點範圍在170至220℃之礦物油、沸點範圍在170至220℃之石油溶劑油、沸點範圍在250至350℃之錠子油、沸點範圍在160至280℃之石油與芳族烴、松節油等較為有利。
於較佳具體實例中,係使用沸點範圍在180至210℃之液態脂族烴或沸點範圍在180至220℃之芳族烴與脂族烴之高沸點混合物及/或錠子油及/或單氯萘(較佳為α-單氯萘)。
蒸發值35以上及燃點30℃以上(較佳為45℃以上)之有機油性或油型溶劑可被高度或中度揮發性有機化學溶劑部分置換,惟該溶劑混合物亦須具有35以上之蒸發值及30℃以上(較佳為45℃以上)之燃點,且該混合物於此溶劑混合物中可溶或可乳化。
於較佳具體實例中,有些有機化學溶劑或溶劑混合物或脂族極性有機化學溶劑或溶劑混合物被置換。較佳為使用含有羥基及/或酯及/或醚基團之有機化學溶劑,舉例而言,如乙二醇醚類、酯類等。
供本發明目的所用之有機化學黏合劑為本質上已知且可於水中稀釋及/或於所用有機化學溶劑中溶解或分散或乳化之合成樹脂及/或黏合乾性油,特別是含有或由丙烯酸系樹脂、乙烯系樹脂(例如聚乙酸乙烯酯)、聚酯樹脂、縮聚或加聚樹脂、聚胺基甲酸酯樹脂、醇酸樹脂或經改造之醇酸樹脂、酚醛樹脂、烴樹脂例如茚/香豆酮樹脂、矽樹脂、乾性植物油及/或乾性油及/或天然及/或合成樹脂系完全乾性黏合劑組成之黏合劑。
作為黏合劑之合成樹脂可呈乳液、分散液或溶液等形式使用。瀝青或含瀝青物質可作為黏合劑使用,其量至多達10重量%。此外,可使用本質上已知之著色劑、色料、防水劑、掩味劑、抑制劑或防腐劑等。
根據本發明,組成物或濃縮物較佳為含有至少一種醇酸樹脂或經改造之醇酸樹脂及/或乾性植物油作為有機化學黏合劑。根據本發明較喜用之醇酸樹脂為油含量在45重量%以上,較佳為50至68重量%者。
上述黏合劑部分或全部可被固定劑(混合物)或增塑劑(混合物)置換。彼等添加劑意欲防止活性化合物揮發、結晶化或沉澱。彼等較佳為置換0.01至30%黏合劑(以所用黏合劑100%計)。
增塑劑係得自酞酸酯類例如酞酸二丁酯、酞酸二辛酯或酞酸苯基丁基酯;磷酸酯類例如磷酸三丁酯;己二酸酯類例如己二酸二(2-乙基己基)酯;硬脂酸酯類例如硬脂酸丁酯或硬脂酸戊酯;油酸酯類例如油酸丁酯;甘油醚類或高分子量乙二醇醚類;甘油酯類及對甲苯磺酸酯類等化學類別。
固定劑於化學上係以聚乙烯烷基醚類舉例而言,如聚乙烯甲醚;或酮例如二苯甲酮與伸乙基二苯甲酮為基底。
其他適當溶劑或稀釋劑為,特別是,水,適當時,呈與一或多種上述有機化學溶劑或稀釋劑、乳化劑與分散劑之混合物。
活性化合物組合物亦適用於防治動物害物,特別是於封閉空間,舉例而言,如住宅、工廠通道、辦公室、車艙等處發現之昆蟲、蛛形綱動物及蜱蟎;彼等可於家用殺昆蟲劑產品中使用以防治彼等害物;其對於敏感及抗性品系及所有發育階段均具活性。上述害物包括:屬於蠍目(Scorpionidea)者,例如,地中海黃蠍(Buthus occitanus
);屬於蜱蟎目者,例如,雞壁蝨(Argas persicus
)、鴿壁蝨(Argas reflexus
)、苔蟎(Bryobia
)屬、雞皮刺蟎、住家食甜恙蟲(Glyciphagus domesticus
)、非洲鳥壁蝨(Ornithodorus moubat
)、血色扇頭蝨蟲(Rhipicephalus sanguineus
)、刺激秋恙蟲(Trombicula alfreddugesi
)、Neutrombicula autumnalis
、歐洲家刺皮蟎(Dermatophagoides pteronissimus
)、美洲家刺皮蟎(Dermatophagoides forniae
);屬於蜘蛛目(Araneae)者,例如,Aviculariidae
、圓蛛科(Araneidae
);屬於盲蛛目(Opiliones)者,例如,擬蝎屬之Pseudoscorpiones chelifer
與Pseudoscorpiones cheiridium
、盲蛛屬之Opiliones phalangium
;屬於等足目者,例如,海蛆屬之Oniscus asellus
、Porcellio scaber
;屬於雙足目者,例如,Blaniulus guttulatus
、山蛩蟲(Polydesmus
)屬;屬於唇足目者,例如,地蜈蚣(Geophilus
)屬;屬於衣魚亞目(Zygentoma)者,例如,衣魚(Ctenolepisma
)屬、西洋衣魚(Lepisma saccharina
)、盜火蟲(Lepismodes inquilinus
);屬於蠊目者,例如,東方蠊、德國小蠊、亞洲蟑螂(Blattella asahinai
)、馬得拉蠊、蠊(Panchlora
)屬、蠊(Parcoblatta
)屬、澳洲大蠊(Periplaneta australasiae
)、美洲大蠊(Periplaneta americana
)、褐色大蠊(Periplaneta brunnea
)、煙色大蠊(Periplaneta fuliginosa
)、長鬚蠊(Supella longipalpa
);屬於跳躍亞目(Saltatoria)者,例如,家蟋蟀(Acheta domesticus
);屬於革翅目者,例如,歐洲球螋;屬於等翅目者,例如,木白蟻(Kalotermes
)屬、網白蟻屬;屬於嚙蟲目(Psocoptera)者,例如,書蝨(Lepinatus
)屬、書蝨(Liposcelis
)屬;屬於鞘翅目者,例如,皮蠹(Anthrenus
)屬、黑皮蠹(Attagenus
)屬、皮蠹(Dermestes
)屬、長頭穀盜(Latheticus oryzae
)、郭公蟲(Necrobia
)屬、蜘甲(Ptinus
)屬、穀蠹、穀象(Sitophilus granarius
)、米象(Sitophilus oryzae
)、玉米象(Sitophilus zeamais
)、藥材甲蟲(Stegobium paniceum
);屬於雙翅目者,例如,埃及黑蚊(Aedes aegypti
)、白斑蚊(Aedes albopictus
)、黑斑蚊(Aedes taeniorhynchus
)、按蚊(Anopheles
)屬、紅頭麗蠅、Chrysozona pluvialis
、五帶淡色庫蚊(Culex quinquefasciatus
)、家蚊(Culex pipiens
)、媒斑蚊(Culex tarsalis
)、果蠅(Drosophila
)屬、黃腹廄蠅(Fannia canicularis
)、家蠅(Musca domestica
)、糠蚊(Phlebotomus
)屬、麻蠅(Sarcophaga
)屬、蚋蠅(Simulium
)屬、螫蠅(Stomoxys calcitrans
)、歐洲大蚊;屬於鱗翅目者,例如,小蠟螟(Achroia grisella
)、大蠟螟、印度穀螟(Plodia interpunctella
)、衣蛾屬之Tinea cloacella
、網衣蛾、袋衣蛾;屬於蚤目者,例如,犬蚤(Ctenocephalides canis
)、貓蚤(Ctenocephalides felis
)、人蚤(Pulex irritans
)、穿皮潛蚤(Tunga penetrans
)、東方鼠蚤;屬於膜翅目者,例如,大黑蟻(Camponotus herculeanus
)、黑草蟻(Lasius fuliginosus
)、普通黑蟻(Lasius niger
)、Lasius umbratus
、廚蟻(Monomorium pharaonis
)、Paravespula
屬、鋪道蟻(Tetramorium caespitum
);屬於虱目者,例如,頭虱(Pediculus humanus capitis
)、衣虱(Pediculus humanus corporis
)、陰虱(Phthirus pubis
);屬於異翅亞目者,例如,熱帶臭蟲(Cimex hemipterus
)、臭蟲(Cimex lectularius
)、錐蝽、騷擾蠟蝽(Triatoma infestans
)。
彼等係於氣溶膠、無壓力噴霧產物例如泵與霧化器噴霧、自動生霧系、煙霧彈、泡沫、凝膠、具有由纖維素或聚合物製成的蒸發器錠劑之蒸發器產物、液體蒸發器、凝膠與膜蒸發器、推進劑驅動式蒸發器、無能量或被動式蒸發器系、蛾紙、蛾袋與蛾凝膠中,或呈粒劑或細粉劑,或於散佈用餌料或於餌站中使用。
根據本發明之混合物特別適用於處理種子。於此,以上文提及之較佳或特佳之根據本發明之組合物為較佳。由害物引發之對作物植物之傷害極大部分發生於最早期,如種子於貯存期間、於被引入土壤中後、其間及就在植物發芽後被侵襲;此階段特別具關鍵性,因為生長中植物的根與幼芽特別敏感,即使小傷害亦可導致整株植物死亡。因此使用適當組成物以保護種子及發芽中之植物尤其引起關注。
藉處理植物種子以防治害物長久以來已為業界悉知,主要問題在於持續改善。然而,種子之處理常常產生無法以令人滿意的方式解決之一系列問題。因此,業界期盼開發出於播種或植物萌芽後不需額外施加作物保護劑之用於保護種子與發芽植物之方法;進一步期盼使用最適量之活性化合物以對種子與發芽植物提供最大保護而免害物侵襲,惟所用活性化合物不傷害植物本身。特別是,種子處理方法亦須將基因轉殖植物固有之殺昆蟲性質列入考量,以使用最少量作物保護劑而達成對種子與發芽植物之最適保護。
因此,本發明尤其亦係有關藉使用根據本發明之組成物處理種子,以保護種子與發芽植物免受害物侵襲之方法。本發明亦係有關使用根據本發明之組成物處理種子,以保護種子與發芽植物免受害物侵襲之用途。再者,本發明乃有關已使用根據本發明之組成物處理而提供對害物之保護之種子。
再者,必須列入考量之優點為,根據本發明之混合物尤其亦可用於基因轉殖種子,由此種子產生之植物能表現被指引對抗害物之蛋白質。藉使用根據本發明組成物處理此等種子。
根據本發明,所有植物與部分植物體均可能處理。於本文中,植物欲被瞭解為意指所有植物與植物族群,例如需要及不需要之野生植物或收成植物(包括天然存在之收成植物)。收成植物為可利用習知植物育種及最適方法或利用生物技術與遺傳工程方法或這些方法之組合獲得之植物,包括基因轉殖植物及受或不受植物育種者之權利保護之植物栽培品種。部分植物體欲被瞭解為意指植物之所有地上與地下部分與器官,例如苗、葉、花與根,可述及之實例為葉、針、柄、莖、花、果實體、果實與種子以及根、塊莖與根莖。部分植物體亦包含經收獲之物料,及無性與有性繁殖物料,例如幼苗、塊莖、根莖、插條及種子。
根據本發明,以活性化合物處理植物及部分植物體係直接進行或根據習知處理法,例如利用浸漬、噴霧、蒸發、生霧、撒佈、漆上及於繁殖體之情形下,特別是於種子之情形下,亦利用施敷一或多層,使該等化合物作用於其周圍、環境或貯存處。
如上所述,根據本發明,得以處理所有植物及部分植物體。於較佳具體實例中,係處理野生植物及植物栽培品種、或利用習知生物育種方法(例如雜交或原生質體融合)獲得者、及部分植物體。於進一步較佳具體實例中,則處理利用遺傳工程(適當時,與習知方法組合)獲得之基因轉殖植物及植物栽培品種(基因改造生物),及部分植物體。「部分」或「部分植物體」等詞已於上文說明。
特佳為,根據本發明處理於各情形下市售可得或使用中之植物栽培品種之植物。
視植物種類或栽培品種、其位置及生長條件(土壤、氣候、植被期、養料)而異,根據本發明之處理亦可能產生超增加(「增效」)之效果。因此,舉例而言,超越實際預期效果之施加率減少及/或活性譜變廣及/或根據本發明可用之物質及組成物之活性增加、植物生長較佳、對高溫或低溫之耐性增加、對乾旱或對水或土壤鹽含量之耐性增加、花開得多、易於收割、加速成熟、收獲率較高、品質較佳及/或收成產品營養價值較高、貯存安定性及/或收成產品加工性較好等均可能發生。
較佳及擬根據本發明處理之基因轉殖植物或植物栽培品種(亦即以遺傳工程方法獲得者)包含,於基因改造中,得到賦與該等植物特別有利之有用性質(「特性」)的遺傳物質之所有植物。此等性質之實例為植物生長較佳、對高溫或低溫之耐性增加、對乾旱或對水或土壤鹽含量之耐性增加、花開得多、易於收割、加速成熟、收獲率較高、品質較佳及/或收成產品營養價值較高、貯存安定性及/或收成產品加工性較好。此等性質之進一步及特別著重之實例為植物對抗動物及微生物害物(例如對抗昆蟲、蜱蟎、植物病原性真菌、細菌及/或病毒)之防禦力較佳、以及植物對特定具除草活性化合物之耐性增加。可述及之基因轉殖植物之實例為重要收成作物,例如穀類(小麥、稻米)、玉米、大豆、馬鈴薯、棉花、油菜及水果作物(蘋果、梨、柑橘類水果及葡萄),特別是玉米、大豆、馬鈴薯、棉花與油菜。特別著重之特性為由於在植物中產生毒素,特別是由得自蘇雲金芽孢桿菌之遺傳物質[例如由CryIA(a)、CryIA(b)、CryIA(c)、CryIIA、CryIIIA、CryIIIB2、Cry9c、Cry2Ab、Cry3Bb與CryIF等基因以及其組合物]於植物中產生者(下文稱為「Bt植物」,使植物對昆蟲之防禦力增加。進一步特別著重之特性為植物對特定具除草活性化合物,例如咪唑啉酮類、磺醯脲類、嘉磷塞(glyphosate)或次膦醯麥黃酮(例如「PAT」基因)之耐性增加。賦與論及之所需特性之基因亦可互相組合而存在基因轉殖植物中。可述及之「Bt植物」實例為以商品名YIELD GARD(例如玉米、棉花、大豆)、KnockOut(例如玉米)、StarLink(例如玉米)、Bollgard(棉花)、Nucotn(棉花)及NewLea(馬鈴薯)出售之玉米變種、棉花變種、大豆變種及馬鈴薯變種。可述及之對除草劑具耐性植物之實例為以商品名Roundup Ready(對嘉磷塞具耐性,例如玉米、棉花、大豆)、Liberty Link(對次膦醯麥黃酮具耐性,例如油菜)、IMI(對咪唑啉酮類具耐性)及STS(對磺醯脲類具耐性,例如玉米)出售之玉米變種、棉花變種及大豆變種。可述及之對除草劑具耐性之植物(以習知方法針對除草劑耐性育種之植物)包含以商品名Clearfield(例如玉米)出售之變種。當然,彼等敘述亦可應用於具有此等遺傳特性或仍待開發之遺傳特性之植物栽培品種,該等植物未來將開發及/或上市。
所列舉之植物可使用根據本發明之活性化合物混合物根據本發明以特別有利之方式處理。上文敘述混合物之較佳範圍亦適用於處理彼等植物。特別強調的為使用本說明書中具體提及之混合物之植物處理。
根據本發明活性化合物組合物之良好殺昆蟲、殺蟎及殺線蟲作用,舉例而言,可使用WO 2005/102056中敘述之方法予以測定。雖然個別活性化合物於其活性上顯得薄弱,然而組合物顯示超越諸活性單純加總之活性。
當活性化合物組合物之殺昆蟲
、殺蟎
或殺線蟲
作用超越個別施加活性化合物之作用總和時,則該等殺昆蟲劑
、殺蟎劑
與殺線蟲劑
之增效效應隨時存在。
根據S.R.Colby(“Calculating Synergistic and Antagonistic Responses of Herbicide Combinations”,Weeds1967
,15
,20-22),兩個活性化合物之既定組合物之預期殺昆蟲
、殺蟎
或殺線蟲
作用可計算如下:若X係以m
g/ha之施加率或m
ppm之濃度施用活性化合物A時之殺害率(以未處理對照組之%表示),Y係以n
g/ha之施加率或n
ppm之濃度施用活性化合物B時之殺害率(以未處理對照組之%表示)及E係以m
與n
g/ha之施加率或m
與n
ppm之濃度施用活性化合物A與B時之殺害率(以未處理對照組之%表示)及則
若對昆蟲之實際殺害率超過計算值,則稱該組合物之殺害率具超增加性,亦即存在增效效應。於此情形下,實際觀察到之殺害率必須大於使用上式計算出之預期殺害率之值(E)。
根瘤線蟲(Meloidogyne incognita
)試驗(MELGIN)
為了製造活性化合物之適當製劑,使1重量份活性化合物與所述量溶劑及乳化劑混合,以水稀釋此濃縮物至所需濃度。
以所需量之刺芒柄花素施敷於萵苣種子。於容器中裝填以菌根、活性化合物溶液、根瘤線蟲卵/幼蟲懸浮液感染之土壤及經處理之種子。令萵苣種子發芽,逐漸產生植株。於根上,形成癭瘤(galls)。
經所需時間後,利用癭之形成測定殺線蟲效力(單位%)。100%意指未發現癭;0%意指經處理植株上之癭數與未經處理之對照組相當。
於此試驗中,相較於單獨施敷活性化合物,根據本發明之下述活性化合物組合物展現增效提高之活性:
Claims (7)
- 一種活性化合物組合物,其包含具下式(I)之刺芒柄花素或其鹽
與選自下述第(2)至(3)組之至少一種活性殺昆蟲化合物:(2.1)氯菸鹼醯基類(chloronicotinyl)及/或新菸鹼類(neonictonoids);及(3.2)有機磷酸酯類(organophosphates)。 - 根據申請專利範圍第1項之活性化合物組合物,其中第(2)至(3)組之活性化合物係選以下表列:(2.1.1)可尼丁(clothianidin);(2.1.2)益達胺(imidacloprid);(2.1.3)噻洛利(thiacloprid);(2.1.4)賽美索佔(thiamethoxam);(2.1.5)醋密普利(acetamiprid);(2.1.6)達特喃(dinotefuran);(2.1.7)尼天爛(nitenpyram);(2.1.8)氯噻啉(imidaclothiz);(3.2.1)丁基嘧啶磷(tebupirimfos);(3.2.2)加奪松(cadusaphos);(3.2.3)松賽殺(fosthiazate);(3.2.4)普伏松(ethopopphos);及 (3.2.5)芬滅松(fenamiphos)。
- 根據申請專利範圍第1項之活性化合物組合物,其包含刺芒柄花素與益達胺。
- 一種增效性活性化合物組合物,其包含根據申請專利範圍第1項之活性化合物組合物。
- 根據申請專利範圍第4項之增效性活性化合物組合物,其中第(2)至(3)組之活性化合物係選以下表列:(2.1.1)可尼丁(clothianidin);(2.1.2)益達胺(imidacloprid);(2.1.3)噻洛利(thiacloprid);(2.1.4)賽美索佔(thiamethoxam);(2.1.5)醋密普利(acetamiprid);(2.1.6)達特喃(dinotefuran);(2.1.7)尼天爛(nitenpyram);(2.1.8)氯噻啉(imidaclothiz);(3.2.1)丁基嘧啶磷(tebupirimfos);(3.2.2)加奪松(cadusaphos);(3.2.3)松賽殺(fosthiazate);(3.2.4)普伏松(ethopopphos);及(3.2.5)芬滅松(fenamiphos)。
- 根據申請專利範圍第4項之增效性活性化合物組合物,其包含刺芒柄花素與益達胺。
- 根據申請專利範圍第4項之增效性活性化合物組合物,其包含刺芒柄花素與芬滅松。
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| CN101610672A (zh) * | 2007-01-16 | 2009-12-23 | 先正达参股股份有限公司 | 农药组合 |
| PL2124557T3 (pl) * | 2007-02-02 | 2015-06-30 | Plant Health Care Inc | Synergistyczne kombinacje grzybobójcze zawierające formononetynę |
| US9049814B2 (en) | 2007-02-23 | 2015-06-09 | Vamtech, Llc | Coated seeds and methods of making coated seeds |
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2006
- 2006-11-29 DE DE102006056544A patent/DE102006056544A1/de not_active Withdrawn
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2007
- 2007-11-16 JP JP2009538612A patent/JP5513121B2/ja active Active
- 2007-11-16 MX MX2009005522A patent/MX2009005522A/es active IP Right Grant
- 2007-11-16 CN CNA2007800443830A patent/CN101547605A/zh active Pending
- 2007-11-16 CA CA2670637A patent/CA2670637C/en not_active Expired - Fee Related
- 2007-11-16 AU AU2007324936A patent/AU2007324936B2/en not_active Ceased
- 2007-11-16 US US12/515,954 patent/US8334268B2/en not_active Expired - Fee Related
- 2007-11-16 EP EP07819832.2A patent/EP2107871B1/de not_active Not-in-force
- 2007-11-16 KR KR1020097013403A patent/KR101283369B1/ko not_active Expired - Fee Related
- 2007-11-16 ES ES07819832.2T patent/ES2627423T3/es active Active
- 2007-11-16 WO PCT/EP2007/009898 patent/WO2008064778A2/de not_active Ceased
- 2007-11-16 BR BRPI0718936-2A patent/BRPI0718936A2/pt not_active IP Right Cessation
- 2007-11-28 CL CL200703420A patent/CL2007003420A1/es unknown
- 2007-11-28 TW TW096145059A patent/TWI402035B/zh not_active IP Right Cessation
- 2007-11-29 AR ARP070105304A patent/AR064028A1/es unknown
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2009
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5002603A (en) * | 1989-12-04 | 1991-03-26 | Board Of Trustees Operating Michigan State University | Method and compositions for stimulating vesicular-arbuscular mycorrhizal fungi |
Non-Patent Citations (1)
| Title |
|---|
| Yue B. et al. Evaluation of thiamethoxam and imidacloprid as seed treatments to control European corn borer and Indianmeal moth (Lepidoptera: Pyralidae) larvae. J. Econ. Entomol. 2003, 96, 503-509. * |
Also Published As
| Publication number | Publication date |
|---|---|
| US8334268B2 (en) | 2012-12-18 |
| US20100048497A1 (en) | 2010-02-25 |
| WO2008064778A3 (de) | 2009-02-26 |
| ZA200903547B (en) | 2010-08-25 |
| KR20090097168A (ko) | 2009-09-15 |
| AR064028A1 (es) | 2009-03-04 |
| EP2107871B1 (de) | 2017-04-12 |
| JP2010510996A (ja) | 2010-04-08 |
| CO6180478A2 (es) | 2010-07-19 |
| BRPI0718936A2 (pt) | 2013-12-10 |
| WO2008064778A2 (de) | 2008-06-05 |
| JP5513121B2 (ja) | 2014-06-04 |
| AU2007324936B2 (en) | 2013-08-22 |
| KR101283369B1 (ko) | 2013-07-15 |
| TW200829163A (en) | 2008-07-16 |
| AU2007324936A1 (en) | 2008-06-05 |
| CA2670637A1 (en) | 2008-06-05 |
| DE102006056544A1 (de) | 2008-06-05 |
| CA2670637C (en) | 2014-03-25 |
| MX2009005522A (es) | 2009-06-12 |
| EP2107871A2 (de) | 2009-10-14 |
| CL2007003420A1 (es) | 2008-05-23 |
| ES2627423T3 (es) | 2017-07-28 |
| CN101547605A (zh) | 2009-09-30 |
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