JP6886970B2 - 害虫に対するノックダウン活性または吸血阻害活性を有する化合物および組成物 - Google Patents
害虫に対するノックダウン活性または吸血阻害活性を有する化合物および組成物 Download PDFInfo
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- JP6886970B2 JP6886970B2 JP2018517510A JP2018517510A JP6886970B2 JP 6886970 B2 JP6886970 B2 JP 6886970B2 JP 2018517510 A JP2018517510 A JP 2018517510A JP 2018517510 A JP2018517510 A JP 2018517510A JP 6886970 B2 JP6886970 B2 JP 6886970B2
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- trifluoromethyl
- anopheles
- pyridine
- compounds
- mosquitoes
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Classifications
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
- A01N43/88—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms six-membered rings with three ring hetero atoms
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
- A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
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- A—HUMAN NECESSITIES
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- A01M—CATCHING, TRAPPING OR SCARING OF ANIMALS; APPARATUS FOR THE DESTRUCTION OF NOXIOUS ANIMALS OR NOXIOUS PLANTS
- A01M1/00—Stationary means for catching or killing insects
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- A—HUMAN NECESSITIES
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- A01M—CATCHING, TRAPPING OR SCARING OF ANIMALS; APPARATUS FOR THE DESTRUCTION OF NOXIOUS ANIMALS OR NOXIOUS PLANTS
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- A—HUMAN NECESSITIES
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- 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
- A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
- A01N25/34—Shaped forms, e.g. sheets, not provided for in any other sub-group of this main group
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- A—HUMAN NECESSITIES
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
- A01N43/36—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings
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- A—HUMAN NECESSITIES
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
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- A—HUMAN NECESSITIES
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
- A01N43/54—1,3-Diazines; Hydrogenated 1,3-diazines
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- A—HUMAN NECESSITIES
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- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
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Description
1.有害な蚊は、家の周囲でまたは公園およびレクリエーションエリアで人々に迷惑となり;
2.経済的に重要な蚊は、不動産価値を低下させるか、観光および関連する事業の利益に悪影響を及ぼすか、または家畜もしくは家禽の生産に悪影響を及ぼし;
3.蚊が感染性疾患の媒介動物または伝達者である場合には公衆衛生が焦点となる。
・生息地の制御 − 蚊が容易に繁殖し得る場所を取り除くまたは低減することは、個体群の増殖の制限に役立つことができる。例えば、停滞している水の除去、蚊の繁殖環境としての役割を果たす古いタイヤおよび缶の破壊、ならびに貯留水の良好な管理により、蚊が過剰に発生する場所を低減することができる。
・接触の低減 − 蚊への曝露を制限することにより、感染リスクを著しく低減することができる。例えば、蚊帳、家の窓網戸または保護服は、蚊との接触の可能性の低減に役立つことができる。効果的であるには、蚊の脅威に対する意識を高めるために住民の間での方法の教育および啓発が必要である。
・化学的防除 − 殺虫剤、幼虫駆除剤および忌避剤を使用して蚊を防除することができる。例えば、幼虫駆除剤を蚊の繁殖区域で使用することができ、防虫剤を家の壁または蚊帳に適用することができ、個人用忌避剤の使用により蚊の刺咬およびその結果としての感染の発生を低減することができる。媒介蚊の防除のための農薬の使用が世界保健機関(WHO)により促進され、非常に効果的であることが証明されている。
・生物学的防除 − 細菌毒素または植物性化合物等の媒介蚊の天敵の使用は、蚊の個体群の制御に役立つことができる。蚊の幼虫を食べる魚の使用は、ある程度の成功を収めることが実証されている。
・不妊化されたまたは遺伝子改変された雌の蚊の放出による個体群の制御により、媒介蚊の個体群が制御されて感染リスクが低減することも分かっている。
・良好な殺虫効果
・即効性の殺虫効力
・持続性の殺虫効力
・活性成分の均一な放出
・長期の耐久性(例えば、長期間にわたり複数回の洗浄に耐える)
・簡単な製造
・使用者にとって安全。
・標的昆虫は、通常、スプレー雲を通って飛行している(または曝露された表面上で休息している間に影響を受ける場合がある)。従って、スプレー液滴と標的昆虫との間の接触の効率が重要である。これは、スプレー液滴が最適な期間にわたり空中に残存することかつ殺虫剤の適切な用量を含むことを確保することにより達成される。これら2つの問題点は、液滴サイズを最適化することによりほとんど対処される。
・液滴が大きすぎる場合、液滴は地面へあまりにも急速に落下し、適用中に遭遇する植物または他の障害物に浸透しない(適用の有効面積が制限される)。これらの大きい液滴の1つが個々の昆虫に影響を及ぼす場合、個々の昆虫当たり高用量が送達されることから、この影響は「過剰殺傷」でもある。
・液滴が小さすぎる場合、以下のいずれかの場合がある:空気力学に起因して標的昆虫に沈着しない(衝突しない)か、または対流により大気中を上方へ運ばれ得る。
・空間スプレー用途の液滴の最適なサイズは、10〜25ミクロンの体積メジアン直径(VMD)を有する液滴である。
・IRS製剤としての使用の場合、この有効量は、表面上のAIの被覆率が1m2当たりAI 0.01〜2gであり、好ましくは1m2当たりAI 0.05〜1gであり、特に1m2当たりAI 0.1〜0.7gである。
・網または基体内に組み込まれて使用される場合、この有効量は0.05〜15重量%であり、好ましくは0.2〜10重量%であり、より好ましくは0.4〜8重量%であり、特に0.5〜5であり、例えば1〜3重量%である。
a)使用するポリマーと1つまたは複数の殺虫活性成分とを120〜250℃の温度で一緒にまたは別々に融解させる工程、
b)工程a)の融解物を紡績糸に形成して冷却する工程、
c)任意選択的に、工程b)で形成された紡績糸を延伸システムに通して誘導し、延伸させ、次いで任意選択的に糸を硬化させる工程、
d)紡績糸を編んで網を形成する工程、
e)この網に、熱硬化操作の温度が使用するポリマーの融解温度よりも20℃低いように選択されている熱硬化操作を行う工程。
・表1で列挙された少なくとも1つの4−(トリフルオロメチル)ピリジン化合物(A)を含む第1の成分、および
・少なくとも1つの高分子バインダー(B)を含む第2の成分。
・更なる添加剤(D)は、このキットの第3の別の成分であってもよく、または成分(A)および/もしくは(B)と既に混合されていてもよい。
・表1で列挙された4−(トリフルオロメチル)ピリジン化合物(A)および任意選択的に水(C)の一製剤、ならびに
・少なくとも1つの高分子バインダー(B)、成分(C)としての水および任意選択的に成分(D)の第2の別の製剤。
a)以下の群から選択される手順のいずれかにより本発明に係る水性製剤で網および/または織物を処理する工程:
(a1)材料を製剤に通す工程;または
(a2)材料と、製剤に部分的にまたは完全に浸漬されたローラーとを接触させ、この材料のローラーとの接触面に製剤を引き寄せる工程、または
(a3)材料を製剤中に浸す工程、または
(a4)材料に製剤を噴霧する工程、または
(a5)製剤を材料上にまたは材料中にブラシで塗布する工程、または
(a6)製剤を発泡体として適用する工程、または
(a7)製剤を材料上にコーティングする工程、
b)任意選択的に、ローラー間で材料を圧搾することによりまたはドクターブレードにより過剰な製剤を除去する工程、ならびに
c)材料を乾燥させる工程。
材料を水性製剤に通すことにより製剤を適用する。前記工程はパディングとして当業者に既知である。好ましい実施形態では、溶液を含む槽中の水性製剤に材料を完全に浸すか、または2つの水平に配向されたローラー間に保持された製剤に材料を通す。本発明によれば、材料を製剤に通すことができるか、または製剤を材料に通すことができる。製剤の取り込み量は、濃縮浴の安定性、レベル分布の必要性、材料の密度、ならびに乾燥工程および硬化工程のエネルギーコストを節約することの要望によって影響を受ける。通常の溶液取り込みは、材料の重量に対して40〜150%であり得る。当業者は最適値の決定に精通している。工程a1)は、後に網へと仕立てられる開放幅の材料をコーティングするのに好ましい。
分散液に部分的に浸漬させたローラーにより材料に水性製剤を適用し、それにより材料のローラーとの接触面に分散液を適用することも更に可能である(キスローリング(kiss−rolling))。この方法により材料の片面のみをコーティングすることが可能であり、これは、例えばヒトの皮膚と殺虫剤処理された材料との直接接触を避けるべきである場合に有利である。
スプレー液を、噴霧装置を備えた適切な繊維機械において(例えば、オープンポケットの衣類洗濯機/遠心分離式脱水機において)連続プロセスまたはバッチ式プロセスで適用することができる。そのような装置は、既成の網に含浸させるのに特に適している。
発泡体は、上述した分散液と比べて少量の水を含む。従って、乾燥プロセスは非常に短くてもよい。この処理を、ガスまたはガスのブレンド(例えば、空気)を注入することにより実施することができる。好ましくは、膜形成特性を有する界面活性剤の添加が必要な場合がある。適切な界面活性剤および必要な技術的装置は当業者に既知である。
コーティングプロセスを好ましくはドクターブレードプロセスで実行することができる。このプロセスの条件は当業者に既知である。
通常、材料を圧搾することにより、好ましくは当技術分野で既知であるように材料をローラー間に通すことにより、過剰な乳濁液を除去し、それにより規定の溶液取り込みを達成する。圧搾された溶液を再使用することができる。あるいは、遠心分離または真空吸引により過剰な水性乳濁液または水性分散液を除去することができる。
乾燥を周囲温度で実施することができる。具体的には、そのような受動乾燥を高温乾燥気候で実行することができる。当然のことながら、高温を適用することにより、この乾燥プロセスを加速させることができる。能動乾燥プロセスは、通常、高スケール処理中に実施されることになる。この乾燥を概して200℃未満の温度で実行する。好ましい温度は30〜170℃、より好ましくは室温である。温度の選択は、製剤中の殺虫剤の熱安定性および含浸される非生体材料の熱安定性によって決定される。
実施例P1−化合物(1.5)−5−[4−(トリフルオロメチル)−3−ピリジル]−1,2,4−オキサチアゾール−3−オン
4−トリフルオロメチル−ニコチンアミド(285mg、1.50mmol)をトルエン(5ml)中に懸濁させ、クロロカルボニルスルフェニルクロリド(42.0μl、0.50mmol)を添加した。この反応混合物を3時間にわたり還流で撹拌した。次いで、この反応混合物をろ過し、ろ液を濃縮した。残留物をFlashmaster(中間カラム、溶離液:CycHex/EtOAc)で精製し、黄色固体として67mgの5−[4−(トリフルオロメチル)−3−ピリジル]−1,2,4−オキサチアゾール−3−オンを得た。
化合物(1.7)を、N.Matsumura,Y.Otsuji,E.Imoto,Nippon Kagaku Kaishi 1976,5,782−784において類似の非置換フェニル誘導体に関して説明されているように調製することができる。N’−イソプロピル−4−(トリフルオロメチル)ピリジン−3−カルボヒドラジド(74mg、0.28mmol)のピリジン(1ml)溶液に室温でクロロギ酸エチル(0.062ml、0.57mmol)を添加した。この反応混合物を室温で3日にわたり撹拌した。少量のトルエンを添加し、溶媒を45℃において真空下で除去した。残留物を、溶離液としてシクロヘキサンおよび酢酸エチルを用いるCombiflashで精製し、黄色オイル状物として15mgの3−イソプロピル−5−[4−(トリフルオロメチル)−3−ピリジル]−1,3,4−オキサジアゾール−2−オンを得た。
この化合物を、D.Geffken,Chem.Ber.,1986,119(2),744−746において類似の非置換フェニル誘導体に関して説明されているように調製することができる。N−イソプロピル−ヒドロキシルアミンヒドロクロリド(1.84g、16.5mmol)をジクロロメタン(50ml)中に懸濁させ、DBU(2.24ml)およびピリジン(2.41ml)を添加した。この反応混合物を0℃まで冷却し、ジクロロメタン25ml中の4−(トリフルオロメチル)ピリジン−3−カルボニルクロリドを滴下漏斗で滴下した。この反応混合物を0℃で2時間にわたり撹拌し、次いで室温で2日にわたり撹拌した。この反応混合物をNHCO3溶液、水および1MのHClで洗浄した。有機相をNa2SO4で乾燥させ、ろ過し、次いで濃縮した。残留物を、溶離液としてシクロヘキサンおよび酢酸エチルを用いるFlashmasterで精製し、黄色オイル状物として1.92gの(イソプロピルアミノ)4−(トリフルオロメチル)ピリジン−3−カルボキシレートを得た。
実施例B1〜B10 アノフェレス・ステフェンシ(Anopheles stephensi)(インディアンマラリア蚊(Indian malaria mosquito))
6個のウェル組織培養プレートの個々のウェルを、所定の濃度で試験化合物を含むエタノール溶液250μlで処理した。沈着物が乾燥すると直ちに10匹の非吸血の成体雌のアノフェレス・ステフェンシ(Anopheles stephensi)(2〜5日齢)を各ウェルに加え、脱脂綿栓中の10%ショ糖溶液で生存させた。1時間後にノックダウンの評価を実行し(表B1〜B10)、24時間後および48時間後に死亡率の評価を実行した(表B1〜B4)。
以下の試験は「WHOPESトンネル試験」(http://apps.who.int/iris/bitstream/10665/80270/1/9789241505277_eng.pdfで説明されている)をベースとする。
「CDCボトルアッセイ」(http://www.cdc.gov/malaria/resources/pdf/fsp/ir_manual/ir_cdc_bioassay_en.pdfで説明されている)に基づいて、所定の濃度で試験化合物を含むエタノール1mlを250mlのガラス瓶に入れ、この瓶を回転テーブルに置き、溶媒を蒸発させつつ内面をコーティングした。乾燥すると直ちに適切な種および株(それぞれ3日齢)の25匹の非吸血の成体雌の蚊をストック培養物から吸引し、暴露瓶に穏やかに吹き入れた。この瓶の蓋を交換し、標準的な培養条件(名目上28℃および60〜80%相対湿度)下でこの瓶を、直射日光を避けて直立させた。
12個のウェル組織培養プレートの個々のウェルを、所定の濃度で試験化合物を含むエタノール溶液100μlで処理した。沈着物が乾燥すると直ちに5匹の非吸血の成体雌のアエデス・アエジプティ(Aedes aegypti)またはアノフェレス・ステフェンシ(Anopheles stephensi)(2〜5日齢)を各ウェルに加え、脱脂綿栓中の10%ショ糖溶液で生存させた。1時間後にノックダウンの評価を実行した。処理を複数回繰り返している場合、これらの繰り返しの平均を報告する。結果を表B23に示す。
〔1〕有害で、疾患媒介性のまたは吸血性の双翅類、オオサシガメ亜科(triatominae)またはトコジラミ科(cimicidae)の害虫を防除する方法であって、前記害虫にまたは前記防除が所望される場所に、ノックダウンまたは吸血阻害に有効な量の4−(トリフルオロメチル)ピリジン化合物を含有する組成物を適用する工程を含み、前記4−(トリフルオロメチル)ピリジン化合物が、以下の式1.1〜1.29で表される化合物からなる群から選択されることを特徴とする、方法。
〔3〕蚊を防除する方法であって、前記蚊にまたはヒトもしくは哺乳動物と前記蚊との間の潜在的なもしくは既知の相互作用の場所に、前記〔1〕に記載の式(1.1)〜(1.29)のピリジン化合物からなる群から選択される化合物を含む組成物のノックダウンまたは吸血阻害に有効な量を含む活性化合物組成物を適用する工程を含むことを特徴とする、方法。
〔4〕前記活性化合物組成物が、前記蚊と前記ヒトまたは哺乳動物との間の潜在的なまたは既知の相互作用の場所で、非生体材料または基体に適用される、前記〔3〕に記載の方法。
〔5〕前記蚊が、アエデス・アエジプティ(Aedes aegypti)、アエデス・アルボピクタス(Aedes albopictus)、アエデス・ジャポニカス(Aedes japonicas)、アエデス・ベクサンス(Aedes vexans)、クレックス・モレスツス(Culex molestus)、クレックス・パレンス(Culex pallens)、クレックス・ピピエンス(Culex pipiens)、クレックス・キンケファシアタス(Culex quinquefasciatus)、クレックス・レスツアンス(Culex restuans)、クレックス・タルサリス(Culex tarsalis)、アノフェレス・アルビマナス(Anopheles albimanus)、アノフェレス・アラビエンシス(Anopheles arabiensis)、アノフェレス・ダルリンギ(Anopheles darlingi)、アノフェレス・ダイラス(Anopheles dirus)、アノフェレス・フネスツス(Anopheles funestus)、アノフェレス・ガンビアエs.l.(Anopheles gambiae s.l.)、アノフェレス・メラス(Anopheles melas)、アノフェレス・ミニムス(Anopheles minimus)、アノフェレス・シネンシス(Anopheles sinensis)、アノフェレス・ステフェンシ(Anopheles stephensi)、マンソニア・チチランス(Mansonia titillans)から選択される、前記〔3〕に記載の方法。
〔6〕前記蚊が、マラリアの媒介動物である、前記〔5〕に記載の方法。
〔7〕前記4−(トリフルオロメチル)ピリジン化合物が、式1.3で表される化合物から選択される、前記〔1〕に記載の方法。
〔8〕前記組成物が、ペルメトリン、クロルフェナピル、ピリミホスメチル、インドキサカルブ、ラムダ−シハロトリン、デルタメトリン、シアントラニリプロールおよびクロラントラニリプロールから選択される少なくとも1つの殺虫剤を更に含む、前記〔1〕に記載の方法。
〔9〕双翅類またはトコジラミ科(cimicidae)の害虫のノックダウンまたは吸血阻害を引き起こすための総合的な媒介蚊防除の解決手段であって、前記〔1〕に記載の式1.1〜1.29の化合物から選択される1種以上の4−(トリフルオロメチル)ピリジン化合物を含むことを特徴とする、総合的な媒介蚊防除の解決手段。
〔10〕前記4−(トリフルオロメチル)ピリジン化合物1.1〜1.29の1種以上が組み込まれた網である、前記〔9〕に記載の媒介蚊防除の解決手段。
〔11〕網をコーティングするための組成物であって、前記4−(トリフルオロメチル)ピリジン化合物1.1〜1.29の1種以上を含む組成物である、前記〔9〕に記載の媒介蚊防除の解決手段。
〔12〕住居の表面に噴霧するための組成物であって、前記4−(トリフルオロメチル)ピリジン化合物1.1〜1.29の1種以上を含む組成物である、前記〔9〕に記載の媒介蚊防除の解決手段。
〔13〕前記〔1〕に記載の式1.1〜1.29の化合物から選択される1種以上の4−(トリフルオロメチル)ピリジン化合物が組み込まれている、双翅類またはトコジラミ科(cimicidae)の害虫のノックダウンまたは吸血阻害を引き起こすためのポリマー材料であって、より糸(thread)、線維、糸(yarn)、ペレット、網および織物等の、基体または非生体材料を製造するのに有用であることを特徴とする、ポリマー材料。
〔14〕前記〔1〕に記載の式1.1〜1.29の化合物から選択される1種以上の4−(トリフルオロメチル)ピリジン化合物を用いて、ノックダウンまたは吸血阻害により、蚊、好ましくは病原性疾患の媒介蚊を防除する方法。
〔15〕繊維、糸、網および織物を、それに洗濯耐性の昆虫防除特性をコーティングすることによって処理するためのキットであって、前記〔1〕に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物の予め測定された量を含む第1の小袋と、少なくとも1種の高分子バインダーの予め測定された量を含む第2の小袋とを含むことを特徴とする、キット。
〔16〕繊維、糸、網および織物を、それに洗濯耐性の昆虫防除特性をコーティングすることによって処理する方法であって、(i)前記〔1〕に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物を含む処理用組成物を調製する工程と、(ii)前記繊維、糸、網および織物を処理する工程と、(iii)それよって得られる処理済みの繊維、糸、網および織物を乾燥させる工程とを含むことを特徴とする、方法。
〔17〕前記〔1〕に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物が含浸されたポリマー材料を調製する方法であって、前記材料は、より糸、線維、糸、ペレット、網および織物など、双翅類またはトコジラミ科(cimicidae)の害虫のノックダウンまたは吸血阻害を引き起こすための基体または非生体材料を製造するのに有用であり、前記方法が、120〜150℃の温度において、ポリマーと前記〔1〕に記載の4−(トリフルオロメチル)ピリジン化合物とを混合する工程を含むことを特徴とする、方法。
〔18〕ノックダウンまたは吸血阻害によって媒介蚊を防除する方法であって、(a)前記〔1〕に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物と、高分子バインダーと、任意で1種以上の他の殺虫剤および/または共力剤とを含む液体組成物のノックダウンまたは吸血阻害に有効な量を、住居の表面に適用する工程、および/または(b)前記少なくとも1種の4−(トリフルオロメチル)ピリジン化合物と、任意で添加剤、1種以上の他の殺虫剤、および/または共力剤とが組み込まれた基体または非生体材料を、住居内に配置する工程を含むことを特徴とする、方法。
〔19〕20回の洗濯後に、95%〜100%の60分後ノックダウンおよび/または80%〜100%の24時間後死亡率という、WHOPESガイドラインに従った生物活性を有する、前記〔1〕に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物が組み込まれた網。
〔20〕前記〔1〕に記載の式1.5、1.7、1.11、1.12、1.15、1.18、1.20、1.26および1.27からなる群から選択される、4−(トリフルオロメチル)ピリジン化合物。
Claims (16)
- 蚊を防除する方法であって、前記蚊にまたはヒトもしくは哺乳動物と前記蚊との間の潜在的なもしくは既知の相互作用の場所に、請求項1に記載の式(1.1)〜(1.29)のピリジン化合物からなる群から選択される化合物を含む組成物のノックダウンまたは吸血阻害に有効な量を含む活性化合物組成物を適用する工程を含むことを特徴とする、方法(ただし、ヒトに適用される方法は除く)。
- 前記活性化合物組成物が、前記蚊と前記ヒトまたは哺乳動物との間の潜在的なまたは既知の相互作用の場所で、非生体材料または基体に適用される、請求項2に記載の方法。
- 前記蚊が、アエデス・アエジプティ(Aedes aegypti)、アエデス・アルボピクタス(Aedes albopictus)、アエデス・ジャポニカス(Aedes japonicas)、アエデス・ベクサンス(Aedes vexans)、クレックス・モレスツス(Culex molestus)、クレックス・パレンス(Culex pallens)、クレックス・ピピエンス(Culex pipiens)、クレックス・キンケファシアタス(Culex quinquefasciatus)、クレックス・レスツアンス(Culex restuans)、クレックス・タルサリス(Culex tarsalis)、アノフェレス・アルビマナス(Anopheles albimanus)、アノフェレス・アラビエンシス(Anopheles arabiensis)、アノフェレス・ダルリンギ(Anopheles darlingi)、アノフェレス・ダイラス(Anopheles dirus)、アノフェレス・フネスツス(Anopheles funestus)、アノフェレス・ガンビアエs.l.(Anopheles gambiae s.l.)、アノフェレス・メラス(Anopheles melas)、アノフェレス・ミニムス(Anopheles minimus)、アノフェレス・シネンシス(Anopheles sinensis)、アノフェレス・ステフェンシ(Anopheles stephensi)、マンソニア・チチランス(Mansonia titillans)から選択される、請求項2に記載の方法。
- 前記蚊が、マラリアの媒介動物である、請求項4に記載の方法。
- 前記4−(トリフルオロメチル)ピリジン化合物が、式1.3で表される化合物から選択される、請求項1に記載の方法。
- 前記組成物が、ペルメトリン、クロルフェナピル、ピリミホスメチル、インドキサカルブ、ラムダ−シハロトリン、デルタメトリン、シアントラニリプロールおよびクロラントラニリプロールから選択される少なくとも1つの殺虫剤を更に含む、請求項1に記載の方法。
- 請求項1に記載の式1.1〜1.29の化合物から選択される1種以上の4−(トリフルオロメチル)ピリジン化合物が組み込まれている、双翅類またはトコジラミ科(cimicidae)の害虫のノックダウンまたは吸血阻害を引き起こすためのポリマー材料であって、より糸(thread)、線維、糸(yarn)、ペレット、網および織物等の、基体または非生体材料を製造するのに有用であることを特徴とする、ポリマー材料。
- 請求項1に記載の式1.1〜1.29の化合物から選択される1種以上の4−(トリフルオロメチル)ピリジン化合物を用いて、ノックダウンまたは吸血阻害により、蚊を防除する方法(ただし、ヒトに適用する方法は除く)。
- 繊維、糸、網および織物を、それに洗濯耐性の昆虫防除特性をコーティングすることによって処理するためのキットであって、請求項1に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物の予め測定された量を含む第1の小袋と、少なくとも1種の高分子バインダーの予め測定された量を含む第2の小袋とを含むことを特徴とする、キット。
- 繊維、糸、網および織物を、それに洗濯耐性の昆虫防除特性をコーティングすることによって処理する方法であって、(i)請求項1に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物を含む処理用組成物を調製する工程と、(ii)前記繊維、糸、網および織物を処理する工程と、(iii)それよって得られる処理済みの繊維、糸、網および織物を乾燥させる工程とを含むことを特徴とする、方法。
- 請求項1に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物が含浸されたポリマー材料を調製する方法であって、前記材料は、より糸、線維、糸、ペレット、網および織物など、双翅類またはトコジラミ科(cimicidae)の害虫のノックダウンまたは吸血阻害を引き起こすための基体または非生体材料を製造するのに有用であり、前記方法が、120〜250℃の温度において、ポリマーと請求項1に記載の4−(トリフルオロメチル)ピリジン化合物とを混合する工程を含むことを特徴とする、方法。
- ノックダウンまたは吸血阻害によって媒介蚊を防除する方法であって、(a)請求項1に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物と、高分子バインダーと、任意で1種以上の他の殺虫剤および/または共力剤とを含む液体組成物のノックダウンまたは吸血阻害に有効な量を、住居の表面に適用する工程、および/または(b)前記少なくとも1種の4−(トリフルオロメチル)ピリジン化合物と、任意で添加剤、1種以上の他の殺虫剤、および/または共力剤とが組み込まれた基体または非生体材料を、住居内に配置する工程を含むことを特徴とする、方法。
- 請求項1に記載の式1.1〜1.29の化合物から選択される少なくとも1種の4−(トリフルオロメチル)ピリジン化合物が組み込まれた網。
- 請求項1に記載の式1.5、1.7、1.11、1.12、1.15、1.20、1.26および1.27からなる群から選択される、4−(トリフルオロメチル)ピリジン化合物。
- 請求項1に記載の式1.3の4−(トリフルオロメチル)ピリジン化合物をノックダウンまたは吸血阻害に有効な量で含み、かつ、ペルメトリン、クロルフェナピル、ピリミホスメチル、インドキサカルブ、ラムダ−シハロトリン、デルタメトリン、シアントラニリプロールおよびクロラントラニリプロールから選択される少なくとも1つの殺虫剤を含む、殺蚊性組成物。
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