TW200305556A - Organic compounds - Google Patents

Organic compounds Download PDF

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Publication number
TW200305556A
TW200305556A TW092106006A TW92106006A TW200305556A TW 200305556 A TW200305556 A TW 200305556A TW 092106006 A TW092106006 A TW 092106006A TW 92106006 A TW92106006 A TW 92106006A TW 200305556 A TW200305556 A TW 200305556A
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TW
Taiwan
Prior art keywords
group
halogen
alkyl
mono
unsubstituted
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TW092106006A
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Chinese (zh)
Inventor
Pierre Ducray
Thomas Goebel
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Novartis Ag
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Publication of TW200305556A publication Critical patent/TW200305556A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/02—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
    • A01N43/04—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 with one hetero atom
    • A01N43/06—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 with one hetero atom five-membered rings
    • A01N43/08—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 with one hetero atom five-membered rings with oxygen as the ring hetero atom
    • 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
    • A01N43/04—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 with one hetero atom
    • A01N43/06—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 with one hetero atom five-membered rings
    • A01N43/10—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 with one hetero atom five-membered rings with sulfur as the ring hetero atom
    • 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
    • A01N43/04—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 with one hetero atom
    • A01N43/06—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 with one hetero atom five-membered rings
    • A01N43/12—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 with one hetero atom five-membered rings condensed with a carbocyclic ring
    • 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
    • A01N43/36—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
    • A01N43/38—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 condensed with carbocyclic rings
    • 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
    • A01N43/42—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 condensed with carbocyclic rings
    • 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
    • A01N43/56—1,2-Diazoles; Hydrogenated 1,2-diazoles
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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
    • A01N43/58—1,2-Diazines; Hydrogenated 1,2-diazines
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
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    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/60—1,4-Diazines; Hydrogenated 1,4-diazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/24—Oxygen atoms attached in position 8
    • C07D215/26—Alcohols; Ethers thereof
    • C07D215/28—Alcohols; Ethers thereof with halogen atoms or nitro radicals in positions 5, 6 or 7
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
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    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
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    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Environmental Sciences (AREA)
  • Plant Pathology (AREA)
  • Engineering & Computer Science (AREA)
  • Dentistry (AREA)
  • Pest Control & Pesticides (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Agronomy & Crop Science (AREA)
  • Veterinary Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

The invention relates to compounds of the general formula, in which R1, R2, R3, R4, R5, R6, W, Ar1, Ar2, a and b are as defined in claim 1, and to any enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are particularly suitable for controlling parasites in warm- blooded animals.

Description

200305556 玫、發明說明： 【發明所屬之技術領域】 本發明是有關於式I之新穎醯胺基乙腈化合物··200305556 Rose, description of the invention: [Technical field to which the invention belongs] The present invention relates to a novel amidoacetonitrile compound of the formula I ...

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N 0 其中： 八“及A。互相獨立地是未經取代的或經單-或多取代 的芳基，其中ΑΓι& Aq的取代基互相獨立地係選擇自由幽 素、硝基、氰基、OH、SH、（:厂C6烷基〜函素—^—“烷基、 G-Ce烷氧基、鹵素-CrQ烷氧基、C2-C6烯基、鹵素一 烯基、C2-C6炔基、CfC6環烧基、C2-C6烯氧基、鹵素— CG稀氧基、（^-〇6烧硫基、鹵素-C^-C6烧硫基、产義乂 醯氧基、鹵素-Ci-C：6烷基磺醯氧基、CrC6烷基亞磺醯基、 鹵素-CrC6烷基亞磺醯基、q-C6烷基磺醯基、齒素一c ^ 院基崎醯基、c^-C6浠硫基、鹵素-C2-〇6缚硫基、c2—c稀美 亞石黃醢基、鹵素-C2_C6烯基亞磺醯基、CfC6烯基確醯基、 鹵素-Cg-C6烯基石黃醯基、CrC6烷胺基、二〜c!-c6燒胺武 (^-〇6烧基項醯胺基、鹵素烧基確醯胺基、c -c产義 罗炭基、鹵素-c!-Ce烧基幾基、Crce烧氧基幾基、c产義 胺基幾基及二-C^Cg烧基胺基幾基所組成的族群中·未^ 取代的或經單-或多取代的苯基胺基；未經取代的或經單 或多取代的苯基羰基；未經取代的或經單—或多取代的笨 基，其中取代基可以是互相獨立’並且選擇自由_素、硝 200305556 基、氰基、烧基、鹵素-C][-C6烧基、C][-C6燒氧基、齒 素-Ci-Ce烷氧基、CrC6烷硫基、鹵素-CrC6烷硫基、CrC6 烧基亞磺醯基、鹵素-C!-Ce烷基亞磺醯基、Crh烷基；ε黃醯 基及鹵素烧基石黃醢基所組成的族群中；未經取代的 或經單-或多取代的苯氧基，其中取代基可以是互相獨立 ，並且選擇自由鹵素、硝基、氰基、烷基、鹵素一Cl — Ce烧基、C^-C；6烧乳基、鹵素-CrC6烧氧基、c〗-〇6燒硫基、 鹵素-CrC；6烧硫基、C〗-C6烧基亞石黃醯基、鹵素C6烧基 亞續醯基、c】-Ce烧基橫醯基及鹵素-(：广(：6烷基續醯基所組 成的族群中；未經取代的或經單—或多取代的苯基乙炔基 ’其中取代基可以是互相獨立，並且選擇自由鹵素、确基 、氰基、CrC6烷基、鹵素-Ci-C：6烷基、CrC6烷氧基、鹵素 -Crc6烧氧基、Ci-C6烷硫基、_素义义烷硫基、Ci—C6烷 基亞磺醯基、函素-q-c6烷基亞磺醯基、C1-C6烷基磺醯基 及鹵素-CrC6烧基石黃醯基所組成的族群中；以及未經取代 的或經單-或多取代的毗啶氧基，其中取代基可以是互相獨 立，並且選擇自由鹵素、硝基、氰基、（:厂c6烷基、_素_ CrC6烷基、Ci—C6烷氧基、鹵素一Ci—C6烷氧基、Crh烷硫 基、鹵素-CrC6烷硫基、CrC6烷基亞磺醯基、鹵素一Ci-C6 烷基亞磺醯基、Ci —Ce烷基磺醯基及齒素吒厂心烷基磺醯基 所組成的族群中；或 藉由％碳原子而鍵結之未經取代的或經單—或多取代的 雜芳基，其中Ari& A。的取代基可以是互相獨立，並且選 擇自由_素、硕基、氰基、Cl-C6烧基、鹵素_Ci_c6烷基、 200305556N 0 of which: "A" and A. are independently unsubstituted or mono- or poly-substituted aryl groups, wherein the substituents of ΑΓι & Aq are independently selected from the group consisting of free heme, nitro, cyano, OH, SH, (: Plant C6 alkyl ~ functional element — ^ — alkyl, G-Ce alkoxy, halogen-CrQ alkoxy, C2-C6 alkenyl, halo-alkenyl, C2-C6 alkynyl , CfC6 cycloalkenyl, C2-C6 alkenyloxy, halogen-CG dilute oxy, (^ -〇6thiothio, halogen-C ^ -C6thiothio, halooxy, halogen-Ci- C: 6 alkylsulfonyloxy, CrC6 alkylsulfinyl, halo-CrC6 alkylsulfinyl, q-C6 alkylsulfinyl, halide-C ^ -C6 sulfanyl, halogen-C2-〇6 thiosulfanyl, c2-c dimethythazine fluorenyl, halogen-C2_C6 alkenylsulfenylfluorenyl, CfC6 alkenylsulfenyl, halogen-Cg-C6 alkenylsulfavinyl, CrC6 alkylamine group, di ~ c! -C6 alkylamine group (^ -〇6alkyl group amine group, halogen alkyl group amine group, c-c selenium carbon group, halogen-c! -Ce group In the group consisting of chloroamino, Crceoxyalkyl, c-synamino and bis-C ^ Cg alkylamino, ^ Substituted or mono- or poly-substituted phenylamino groups; unsubstituted or mono- or poly-substituted phenylcarbonyl groups; unsubstituted or mono- or poly-substituted stupid groups, wherein the substituents may be Independent of each other 'and select free _ prime, nitrate 200305556, cyano, alkynyl, halogen-C] [-C6 alkynyl, C] [-C6 alkoxy, dentin-Ci-Ce alkoxy, CrC6 alkane Sulfur group, halogen-CrC6 alkylthio group, CrC6 alkylsulfinylsulfenyl group, halogen-C! -Ce alkylsulfinylsulfenyl group, Crh alkyl group; ε-baicalyl group and halogen-calcinated baicalite group; Substituted or mono- or poly-substituted phenoxy, wherein the substituents may be independent of each other, and free halogen, nitro, cyano, alkyl, halogen-Cl-Ce, alkyl, C ^ -C are selected; 6 Burned milk group, halogen-CrC6 alkoxy group, c〗 -〇6 burned thio group, halogen-CrC; 6 burned thio group, C〗 -C6 burned sulfhydryl group, halogen C6 burned fluorenyl group, c] -Ce alkynyl and halogen-(-:-( 6,6-alkyl fluorenyl) groups; unsubstituted or mono- or poly-substituted phenylethynyl 'wherein the substituents may be each other alone , And choose free halogen, ceryl, cyano, CrC6 alkyl, halogen-Ci-C: 6 alkyl, CrC6 alkoxy, halogen-Crc6 alkoxy, Ci-C6 alkylthio, _suyisane In the group consisting of thio, Ci-C6 alkylsulfinyl sulfenyl, halo-q-c6 alkylsulfinyl sulfinyl, C1-C6 alkylsulfinyl sulfonyl, and halogen-CrC6 alkylsulfinyl scutellaria Substituted or mono- or poly-substituted pyridinyloxy, wherein the substituents may be independent of each other, and free halogen, nitro, cyano, (C6 alkyl, _ prime_CrC6 alkyl, Ci— C6 alkoxy, halogen-Ci-C6 alkoxy, Crh alkylthio, halogen-CrC6 alkylthio, CrC6 alkylsulfinamido, halogen-Ci-C6 alkylsulfinamido, Ci-Ce alkyl In the group consisting of sulfosulfenyl and haloalkylsulfonyl; or unsubstituted or mono- or polysubstituted heteroaryl groups bonded by% carbon atoms, where Ari & A. The substituents can be independent of each other and can be selected from free radicals, radicals, cyano, Cl-C6 alkyl, halogen_Ci_c6 alkyl, 200305556

CrC6烧氧基、鹵素一Ci-C6烷氧基、C2—c6烯氧基、鹵素一c2_ Cg烯氧基、CrC6烧硫基、鹵素-(^_〇6烧硫基、c6燒基亞 石黃酿基、鹵素-CVC6烷基亞磺醯基、CfC6烯硫基、函素一 C2-C6烯硫基、Crh烯基亞磺醯基、函素—C2—q烯基亞磺醯 基、ce烷基磺醯基、鹵素-Ci-Ce烷基磺醯基、c2—Ce烯基 石戸、基、鹵素-C2-C6烯基石黃醯基、Crh烧胺基及二一 烷胺基所組成的族群中；CrC6 alkyloxy, halogen-Ci-C6 alkoxy, C2-c6 alkenyloxy, halogen-c2_Cg alkenyloxy, CrC6 alkylthio, halogen-(^ _ 〇6thiothio, c6 alkylthio) Yellow alcohol, halogen-CVC6 alkylsulfinyl sulfenyl group, CfC6 alkenyl sulfenyl group, halo-C2-C6 alkenylthio group, Crh alkenyl sulfinyl sulfenyl group, halo-C2-q alkenylsulfinyl sulfenyl group, A group consisting of ce alkylsulfonyl, halogen-Ci-Ce alkylsulfonyl, c2-Ce alkenyl fluorenyl, radical, halogen-C2-C6 alkenyl luteinyl, Crh amine, and dialkylamino in;

Ri疋氫、q-C6燒基、鹵素-q-C6烧基、烯丙基或 烷氧基甲基； R2、h、R4、Rs及Re互相獨立地是氫、齒素、未經取 代的或經單-或多取代的Ci — Ce烷基、未經取代的或經單一 或多取代的（：厂(：6烯基、未經取代的或經單—或多取代的 C2-c6炔基、未經取代的或經單—或多取代的烷氧基， 其中在每個例子中的取代基可以是互相獨立，並且選擇自 由鹵素C1 ce燒氧基及鹵素-Ci-Ce烧氧基所組成的族群中 未、、取代的或經單—或多取代的h一環烧基，其中取代 基可以是互相獨立，並且選擇自由自素及C「C6烧氧基所 組成的族群中；或未經取代的或經單-或多取代的苯基， 八 戈基了以疋互相獨立，並且選擇自由_素、硝基、 亂基、Cl —h烷基、鹵素-c〗-C6烷基、Ci-Ce烷氧基、鹵素一 1 6烷氧基、Ci-Ce烷硫基、鹵素-Ci-C6烷硫基、（:丨一(；6烷 亞尹、4基、鹵素一C1-C6烷基亞磺醯基、c^-c6烷基磺醯基 鹵素C广C6烷基磺醯基、Ci—Q烷胺基及二_C1 —Q烷胺基 所組成的族群中； 200305556 或K及I 一起是c3-c5伸烷基； w 是 〇、s、s(o2)或 n(r7); R?是氫或c6烷基； a是1 b是0 、3或4 ;以及 、2、3 或 4 ; 一個制條件為…。中至少-個是雜芳基；以及另 條件為Ari及Ar2不會同時是卩^定基丨如果 不基:Γ1不是㈣；以及如果〜是苯基的話、 :要時’本發明也有關於非對映異構物、 、E/Z異構物之混合物及/或互變異構物，在每個例子中， =離的形式或以鹽類的形式存在；本發明也有關於其製 枯=用★’以控制在溫血的生產性家畜、馴養動物以及 =中或其上之體内及體外寄生蟲，特別是螺蟲；本發明 關於包括至少一種這些化合物的除害劑。 【先前技術】 具有除害劑活性之經取代的醯胺基乙腈化合物，是 露於例如歐洲專利EP_G 953 565 A2 t。然而，在其中所 特別揭顯不的活性成份，一直無法滿足有關效力及活 圍的需求。因&，對於具有改善的除害性質之活性成份广 财其需要。現在已發現，的酿胺基乙腈化合物:有 “I著的除害性質，特別是對於在生產性家畜、*丨養動物以 及植物中及其上之體内及體外寄生蟲。 200305556 【發明内容】 作為基團本身以及作為其他基團及化合物的結構性成 份^如’ μ基、炫氧基、烧硫基、燒基亞績醯基及烧 土 ’、Ιώ基在母個例子中，烷基係考慮在每個個別例子中 相關基15或化合物具有之碳原子數目’不論是直鏈的，例 如’甲基、乙基、丙基、丁基、戊基或己基；或是支鏈的 ，例如，異丙基、異丁基、第二—丁基、第三一丁基、異戊 基、新戊基或異己基。 ^作為基團本身以及作為其他基團及化合物的結構性成 份，在每個例子中，烯基係考慮在每個個別例子中相關基 團或化合物具有之碳原子數目以及共軛或分離的雙鍵，不 論是直鏈的，例如，烯丙基、2-丁烯基、3 —戊烯基、卜己 稀基或1，3 -己一烯基；或是支鏈的，例如，異丙烯基、異 丁烯基、異戊間二浠基、第三—戊烯基或異己烯基。 作為基團本身以及作為其他基團及化合物的結構性成 份，在每個例子中，炔基係考慮在每個個別例子中相關基 團或化合物具有之碳原子數目以及共軛或分離的三鍵，不 淪是直鏈的，例如，炔丙基、2- 丁炔基、3 —戊炔基、丨一己 炔基、1-庚炔基或3-己烯-1-炔基；或是支鏈的，例如， 3-甲基丁-1 -炔基、4-乙基戊—;ι 一炔基或4一曱基己—2—炔基 作為基團本身以及作為其他基團及化合物的結構性成 份’例如，鹵環烷基、環烷氧基或環烷硫基，在每個例子 中’環烧基係考慮在每個個別例子中相關基團或化合物具 200305556 有之碳原子數目，例如，環丙基、環丁基、環戊基或環己 基。 芳基是苯基或蔡基。 雜芳基是毗啶基、嘧啶基、s—三嗪基、丨，2, 4-三嗪基 、噬吩基、呋喃基、毗咯基、毗唑基、咪唑基、噬唑基、三 唑基、噁唑基、噻二唑基、噁二唑基、苯並噻吩基、苯並 呋喃基、苯並噻唑基、吲哚基、吲唑基或喹啉基。 作為基團本身以及作為其他基團及化合物的結構性成 份，例如，_烷基、鹵烷氧基、_烷硫基、鹵烷基亞磺醯 基及鹵烷基磺醯基，在每個例子中，鹵素是氟、氯、溴或 議’特別是氟、氣或溴，特別是氟或氯。 經鹵素取代的含碳基團及化合物，例如，鹵烷基、鹵 烧氧基、鹵烧硫基、函烷基亞磺醯基及_烷基磺醯基，可 被部份地鹵化或全函化，在多重鹵化的例子中，鹵素取代 基可以是相同或不同的。作為基團本身以及作為其他基團 及化合物的結構性成份，例如，鹵烷氧基或鹵烷硫基，鹵 烷基的例子是甲基，其係以氟、氯及/或溴經至多三次取 代，例如，CHF2或CF3 ;乙基，其係以氟、氯及/或溴經至 多五次取代，例如，CH2CF3、CF2CF3、CF2CC“、CF2CHC“、 CF2CHF2、CF2CFC12、CF2CHBr2、CF2CHC1F、CF2CHBrF 或 CC1FCHC1F ;丙基或異丙基，其係以氟、氣及/或溴經至多 七次取代，例如，CH2CHBrCH2Br、Cf2CHFCF3、Ch2CF2CF3 或 CIKCF3)2 ; 丁基或其異構物之一，其係以氟、氯及/或溴經 至多九次取代，例如，CF(CF3)CHFCF3或CH2(CF2)2CF3 ;戊 11 200305556 基或其異構物之-，其係以a、氯及/或演經至多十— 取代’例如，CF(CF3)(CHF)A 或 ch2(CF2)3CF3;以及^ 或其異構物之一 係以氟、氯及/或漠經至多…： 代，例 *，（Ch2)4ch謂2Br、CF2(chf)4CF3 或 c(cf3)2(chf)2cf3 。 4 匕 烧氧基較佳地具有1 i 6個碳原子的鍵長度。例如 烧氧基是甲氧基、乙氧基、丙氧基、#丙氧基、正Ri 疋 hydrogen, q-C6 alkyl, halogen-q-C6 alkyl, allyl or alkoxymethyl; R2, h, R4, Rs and Re are independently hydrogen, halo, unsubstituted Or mono- or poly-substituted Ci-Ce alkyl, unsubstituted or mono- or poly-substituted (: 6 (alkenyl, unsubstituted or mono- or poly-substituted C2-c6 alkyne) Group, unsubstituted or mono- or poly-substituted alkoxy groups, wherein the substituents in each example may be independent of each other, and a free halogen C1 ce alkoxy group and a halogen-Ci-Ce alkoxy group are selected An un, substituted or mono- or poly-substituted h-ring alkyl group in the group formed, wherein the substituents may be independent of each other, and can be selected from the group consisting of C and C6 alkyl groups; or Unsubstituted or mono- or poly-substituted phenyl, octadecyl and fluorene are independent of each other, and can be selected from free, nitro, alkynyl, Cl-h alkyl, halogen-c] -C6 alkyl , Ci-Ce alkoxy, halogen- 16 alkoxy, Ci-Ce alkylthio, halogen-Ci-C6 alkylthio, (: 丨-(; 6-alkanein, 4-yl, halogen-C1- C6 alkylsulfinyl sulfenyl , C ^ -c6 alkylsulfonyl halide C, C6 alkylsulfonyl, Ci-Q alkylamino and di_C1-Q alkylamino group; 200305556 or K and I together is c3- c5 alkylene; w is 0, s, s (o2) or n (r7); R? is hydrogen or c6 alkyl; a is 1 b is 0, 3 or 4; and 2, 3 or 4; a The condition is that at least one of them is a heteroaryl group; and the other condition is that Ari and Ar2 will not be 卩 ^ groups at the same time if not radical: Γ1 is not ㈣; and if ~ is phenyl, if necessary: The invention also relates to diastereomers, mixtures of E / Z isomers and / or tautomers. In each case, the = form exists or in the form of a salt; the invention also relates to its Withering = using '' to control warm-blooded productive domestic animals, domestic animals, and in vivo and ectoparasites, especially snails, in or on it; the present invention pertains to pesticides that include at least one of these compounds. [Prior art] Substituted amidinoacetonitrile compounds having pesticide activity are disclosed in, for example, European Patent EP_G 953 565 A2 t. However, what is specifically disclosed therein is not The active ingredient has not been able to meet the needs related to efficacy and activity. Because of & the need for an active ingredient with improved harmful properties, Guangcai, has been found. Now it has been found that the amino acetonitrile compounds: Harmful properties, especially for in vivo and ectoparasites in and on productive livestock, domestic animals and plants. 200305556 [Summary of the Invention] As a group itself and as a structural component of other groups and compounds ^ Such as' μ group, oxo group, thio group, thio group, thio group, thio group, thio group, etc. In the parent example, the alkyl group considers the carbon of the related group 15 or compound in each individual example. The number of atoms 'is either linear, such as' methyl, ethyl, propyl, butyl, pentyl, or hexyl; or branched, such as isopropyl, isobutyl, second-butyl, Tertiary butyl, isopentyl, neopentyl or isohexyl. ^ As a group itself and as a structural component of other groups and compounds, in each case, the alkenyl group takes into account the number of carbon atoms that the related group or compound has in each individual example and the conjugated or separated double Bonds, whether linear, for example, allyl, 2-butenyl, 3-pentenyl, dihexyl, or 1,3-hexanyl; or branched, for example, isopropene Group, isobutenyl, isoprenyl, tert-pentenyl or isohexenyl. As a group itself and as a structural component of other groups and compounds, in each case, the alkynyl group takes into account the number of carbon atoms and the conjugated or separated triple bond of the relevant group or compound in each individual example Is not straight-chain, for example, propargyl, 2-butynyl, 3-pentynyl, monohexynyl, 1-heptynyl, or 3-hexen-1-ynyl; or branched Chain, for example, 3-methylbut-1 -alkynyl, 4-ethylpentyl; ι-alkynyl or 4-methylhexyl-2-alkynyl as the group itself and as other groups and compounds Structural ingredients', for example, halocycloalkyl, cycloalkoxy, or cycloalkylthio. In each example, the 'cycloalkyl' group takes into account the relevant group or compound in each individual example with the number of carbon atoms in 200305556. , For example, cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl. Aryl is phenyl or Czeki. Heteroaryl groups are pyrimidinyl, pyrimidinyl, s-triazinyl, 2,4-triazinyl, phenophyl, furanyl, pyrrolyl, pyrazolyl, imidazolyl, pyrazolyl, tris An oxazolyl, oxazolyl, thiadiazolyl, oxadiazolyl, benzothienyl, benzofuranyl, benzothiazolyl, indolyl, indazolyl or quinolinyl. As a group itself and as a structural component of other groups and compounds, for example, _alkyl, haloalkoxy, _alkylthio, haloalkylsulfinamido, and haloalkylsulfonyl, in each In the examples, halogen is fluorine, chlorine, bromine or hydrogen, especially fluorine, gas or bromine, especially fluorine or chlorine. Halogen-substituted carbon-containing groups and compounds, such as haloalkyl, halooxy, halothio, haloalkylsulfinyl, and alkylsulfonyl, may be partially halogenated or fully halogenated In the case of multiple halogenation, the halogen substituents may be the same or different. As a group itself and as a structural component of other groups and compounds, for example, haloalkoxy or haloalkylthio, examples of haloalkyl are methyl, which are passed up to three times with fluorine, chlorine, and / or bromine Substitution, for example, CHF2 or CF3; ethyl, which is substituted up to five times with fluorine, chlorine and / or bromine, for example, CH2CF3, CF2CF3, CF2CC ", CF2CHC", CF2CHF2, CF2CFC12, CF2CHBr2, CF2CHC1F, CF2CHBrF or CC1FCHC1F Propyl or isopropyl, which is substituted with fluorine, gas, and / or bromine up to seven times, for example, CH2CHBrCH2Br, Cf2CHFCF3, Ch2CF2CF3, or CIKCF3) 2; butyl or one of its isomers, which is based on fluorine , Chlorine and / or bromine are substituted up to nine times, for example, CF (CF3) CHFCF3 or CH2 (CF2) 2CF3; pent 11 200305556-or its isomers, which are at most a, chlorine and / or evolution十 —Substitutions' For example, CF (CF3) (CHF) A or ch2 (CF2) 3CF3; and ^ or one of its isomers is fluorine, chlorine, and / or indifference at most ...: Generation, example *, (Ch2 ) 4ch is 2Br, CF2 (chf) 4CF3, or c (cf3) 2 (chf) 2cf3. 4-Alkyloxy has preferably a bond length of 1 to 6 carbon atoms. For example, alkoxy is methoxy, ethoxy, propoxy, #propoxy, n-

基、異丁氧基、第二-丁氧基及第三_丁氧基，以及也例如 是戊氧基及己氧基的異構物；較佳是甲氧基及乙氧基。齒 烧氧基較佳地具有！至6個碳原子的鏈長度。函烧氧基是 例如氟甲氧基、二氟曱氧基、三氟甲氧基、& ^ 1 t Λ 〇 乙，乙，Z二鼠乙 氧土、1，1’2, 2-四敦乙氧基、2_氟乙氧基、2_氣乙氧基、 2,2-二氟乙氧基以& 2,2’2_三氣乙氧基；較佳是二氟甲氧 基、2-氣乙氧基以及三氟甲氧基。 在本發明内容的範疇内之較佳具體實例是：Isomers, isobutoxy, second-butoxy and tertiary-butoxy, and isomers such as pentyloxy and hexyloxy; methoxy and ethoxy are preferred. Toothed alkoxide preferably has! Chain length to 6 carbon atoms. The alkoxy group is, for example, a fluoromethoxy group, a difluorofluorenyloxy group, a trifluoromethoxy group, & ^ 1 t Λ 〇 B, B, Z diratoxy ethoxide, 1, 1'2, 2- tetra Dunethoxy, 2-fluoroethoxy, 2-gasethoxy, 2,2-difluoroethoxy &2,2'2_trigasethoxy; difluoromethoxy is preferred And 2-fluoroethoxy and trifluoromethoxy. Preferred specific examples within the scope of the present invention are:

(1)具有包含先前提供的限制條件之式】化合物，其 中Ar〗及Arz互相獨立地是未經取代的或經單-或多取代的 方基’其中Ar!及Ar2的取代基互相獨立地選擇自由由素、 硝基、氰基、Cl-c6燒基、函素介Ce烧基、Ci_Cj氧基、 鹵素-以烷氧基、(^環烷基、Ci_C6烷基磺醯基、•素 -Κ6烧基項醢基、Cl-C6烧胺基、二_Ci_Ce貌胺基、 烷基羰基、鹵素-(VC6烷基幾基、Cl-C6烷氧基羰基、c|_c6 烷基胺基藏基及二-Cl-Ce烷基胺基幾基所組成的族群^ ;6 未經取代的或經單-或多取代的苯基羰基；未經取代的或 12(1) A compound having the formula including the previously provided restrictions], wherein Ar and Arz are independently unsubstituted or mono- or poly-substituted square radicals, wherein the substituents of Ar! And Ar2 are independent of each other Freedom to choose from nitro, nitro, cyano, Cl-c6 alkyl, ceto alkyl, Ci_Cj oxygen, halogen-alkoxy, (^ cycloalkyl, Ci_C6 alkylsulfonyl, -K6 alkyl group, Cl-C6 alkyl group, di-Ci_Ce amino group, alkylcarbonyl group, halogen- (VC6 alkyl group, Cl-C6 alkoxycarbonyl group, c | _c6 alkylamino group A group consisting of a Tibetan group and a di-Cl-Ce alkylamino group ^; 6 unsubstituted or mono- or poly-substituted phenylcarbonyl groups; unsubstituted or 12

V 200305556 經單-或多取代的苯基，其中取代基可以是互相獨立，並 且選擇自由鹵素、硝基、氰基、CrC6烷基、鹵素—Crc6烷 基、Ci-C6烧氧基及鹵素烧氧基所組成的族群中；未 經取代的或經單-或多取代的苯氧基，其中取代基可以是 互相獨立，並且選擇自由鹵素、硝基、氰基、烷基、 鹵素-CrC6烷基、Ci-C6烷氧基及鹵素一CrC6烷氧基所組成 的族群中；以及未經取代的或經單-或多取代的赃啶氧基 ，其中取代基可以是互相獨立，並且選擇自由_素、硝基 、氰基、C!-C6烧基、齒素-(:厂c6烷基、c6烷氧基及！I素 -Ci-C：6烷氧基所組成的族群中；或 藉由環碳原子而鍵結之未經取代的或經單_或多取代# 雜芳基，其中八^及Ah的取代基可以是互相獨立，並且還 擇自由鹵素、硝基、氰基、Cl_C6烷基、齒素气丨乂烷基、 (VC6烷氧基、函素介(：6烷氧基、Ci_C6烷基磺醯基、㈣ -CA烧基績醯基、Cl-Ce烧胺基及二_c广&烧胺基所組成 的族群中；V 200305556 Mono- or poly-substituted phenyl, wherein the substituents can be independent of each other, and free halogen, nitro, cyano, CrC6 alkyl, halogen-Crc6 alkyl, Ci-C6 alkoxy and halogen In the group consisting of oxy groups; unsubstituted or mono- or poly-substituted phenoxy groups, wherein the substituents may be independent of each other, and free halogen, nitro, cyano, alkyl, halogen-CrC6 alkane are selected In the group consisting of an alkyl group, a Ci-C6 alkoxy group and a halogen-CrC6 alkoxy group; and an unsubstituted or mono- or poly-substituted stipyridinyloxy group, wherein the substituents may be independent of each other and freely selected _ Group, nitro group, cyano group, C! -C6 alkyl group, halo- (C6 alkyl group, c6 alkoxy group, and! I-Ci-C: 6 alkoxy group; or Unsubstituted or mono- or poly-substituted #heteroaryl bonded by a ring carbon atom, in which the substituents of ^ and Ah may be independent of each other, and also selected from halogen, nitro, cyano, Cl_C6 alkyl, dentin gas, fluorenyl alkyl, (VC6 alkoxy, haloline (6 alkoxy, Ci_C6 alkylsulfonyl, fluorene -CA) In the group consisting of fluorenyl, Cl-Ce, and di-c-C &A;

特別是，互相獨立地，未經取代的或經單_或多取代# 芳基，其+ ΑιΆ Ar2的取代基互相獨立，係選擇自由^ 、石肖基、氰基、Μ燒基基、 、鹵素-Ci-烧氧基、-Cc 理、r η 3 烷基、（：广(：6烷基羰基及鹵Ί -Cl-C6烧基幾基所組成的族群中；未經取代的或經單—或； 取代的苯基幾基；未經取代的或經[或多取代的苯基 其中取代基可以是互相獨立，並且選擇自由㈣、氛基 c「c6烧基及i素介(：6燒基所組成的族群中；以及未㈣ 13 200305556 烷基所組成的族群中；或 代的或經單-或多取代的苯氧基，其中取代基可以是互相 獨立’並且選擇自由齒素、氰基、CrC6烷基及齒素-Cl—C6 —藉由環碳原+而鍵結之未經取代的或經單一或多取代的 雜芳基，其巾Arl及ΑΓ2的取代基可以是互相獨立，並且選 擇自由齒素、氰基、Cl—C6烧基、函素-CrC6烧基、CrC6烧 氧基及i素-Cl-Ce烷氧基所組成的族群中； “更特別是，互相獨立地，未經取代的或經單—或多取代 的方基，其巾ΑΓ1及Ar2的取代基互相獨立，係選擇自由齒 素、氣基、Cl - C4烧基、齒辛一 因京Ll C4烷基、Crc4烷氧基、i 素—C广c4烷氧基、c3-c環烷基、 W w烷基羰基及鹵素一Cr C4烧基m基所組成的族群中；未經取代的或經單-或多取代 的苯基幾基；以及未經取代的或經[或多取代的苯基， 其中取代基可以是互相獨立，並且 ^ n 卫且4擇自由_素、C丨-c4烷 基及鹵素-CrC4烧基所組成的族群中；戈 藉由環碳原子而鍵結之未經取代 ^代的或經皁-或多取代的 雜芳基，其中Arl及AI*2的取代基 J 乂疋互相獨立，並且選 擇自由鹵素、Ci-q烷基、鹵素—c c ^ ^ p n 1匕4燒基、（^-(:4烷氧基及 鹵素-Ci-C：4烷氧基所組成的族群中； (2 )具有包含先前提供的限制 .D θ ^ '、件之式I化合物，其 中Ri是氫、（VC4烷基、函素—c C、卜甘 基； 1 4現基或（VC4烷氧基甲 特別是氫、〇丨-〇2烧基或鹵素—c〜c产其 更特別是氫或（^-〇2燒基； 14 200305556 (3)具有包含先前提供的限制條件之式I化合物，其 中R2 R3、R4、R5及R6互相獨立地是氫、鹵素、未經取代 的或經單-或多取代的Γ ci C4烷基，其中取代基可以是互相 獨立，並且選擇自由南素及氧基所組成的族群中 ，C3-C5環烧基或未經取代的或經單_或多取 中取代基可以是互相獨立，並且選擇自由㈣ ； 、虐素-Cl-C4院基、Cl-Cj氧基及南梟=基 成的族群中； 1 4烷氧基所組 特別是’互相獨立地’氫、未經取 代的Cl-C4炫基，其中取代基可以是互相獨立、早'或夕取 自由㈣及（:…烧氧基所組成的族群中 ，並且選擇 更特別是，互相獨立地，氫、 ，s 3~C5環烷基； 基； Cl—C2燒基或VC5環貌 (4) 具有包含先前提供的限制條 中W是0或S; 化合物’其 特別是0 ; (5) 具有包含先前提供的限制條 中a是1、2或3; 化合物，其 特別是1或2 ; 更特別是1 ; (6) 具有包含先前提供的限制條 中b是0、1或2; 式1化合物，其 特別是0或1 ; 更特別是0 ; 15 200305556 (7 )具有包含先前提供的限制條件之式i化合物，其 ^ 中人“及Arz互相獨立地是未經取代的或經單-或多取代的 芳基，其中ΑΓι& Arz的取代基互相獨立地選擇自由_素、 硝基、氰基、Ci-C6烧基、鹵素-Ci-C6院基' 烷氧基、 鹵素-CVC6烷氧基、C：3-C6環烷基、CVC6烷基磺醯基、鹵素 A-c6烧基續醯基、Cl—c6烧胺基、二_Ci_C6烧胺基、 烷基羰基、鹵素-CrC6烷基羰基、Cl-C6烷氧基羰基、Ci-Ce 烷基胺基羰基及二-Cl-C6烷基胺基羰基所組成的族群中；6 未經取代的或經單-或多取代的苯基羰基；未經取代的或鲁 經單—或多取代的苯基，其中取代基可以是互相獨立，並 且選擇自由li素、硝基、氰基、Ci—C6燒基、函素—C「C6烷 基、C】-C6烷氧基及齒素_Ci_C6烷氧基所組成的族群中；未 經取代的或經單-或多取代的苯氧基，其中取代基可以是 互相獨立，並且選擇自由_素、硝基、氰基、烷基、 齒素-匕乂6烷基、C1—Ce烷氧基及_素—C1-Ce烷氧基所組成 的族群中；以及未經取代的或經單—或多取代的毗啶氧基， j中取代基可以是互相獨立，並且選擇自由_素、硝基、鲁 虱基、CrC6烷基、齒素吒丨乂6烷基、Ci-C6烷氧基及_素一 C1 一 C6烷氧基所组成的族群中；或 藉由環碳原子而鍵結之未經取代的或經單—或多取代的 雜芳基’其中Ari及Ar2的取代基可以是互相獨立，並且選 擇自由_素、硝基、氰基、C「c6烧基、鹵素-CrC6烧基、In particular, independently of each other, unsubstituted or mono- or poly-substituted # aryl groups, the substituents of its + ΑιΆ Ar2 are independent of each other, and are free to choose ^, schottyl, cyano, alkynyl, and halogen- In the group consisting of Ci-alkoxy group, -Cc group, r η 3 alkyl group, (C: (6 alkylcarbonyl group and halo-Cl-C6 alkyl group), unsubstituted or mono- Or; substituted phenyl groups; unsubstituted or substituted by [or poly-substituted phenyl groups in which the substituents may be independent of each other, and can be freely selected In the group consisting of alkyl groups; and in the group consisting of alkyl groups; 13 200305556 alkyl groups; or substituted or mono- or poly-substituted phenoxy groups, where the substituents may be independent of each other 'and choose free dentition, cyanide Group, CrC6 alkyl group, and halo-Cl—C6—unsubstituted or mono- or multi-substituted heteroaryl group bonded by ring carbon source +, the substituents of Arl and AΓ2 may be independent of each other And select from the group consisting of free dentition, cyano, Cl-C6 alkyl, halo-CrC6 alkyl, CrC6 alkyl, and i-Ci-Ce alkoxy In the ethnic group; "More particularly, independently of each other, unsubstituted or mono- or poly-substituted square groups, the substituents of AΓ1 and Ar2 are independent of each other, which are selected from the group consisting of free tooth element, gas group, and Cl-C4. Alkyl, octyl-Lin C4 alkyl, Crc4 alkoxy, i-C-C-c4 alkoxy, c3-c cycloalkyl, W w alkylcarbonyl and halogen-Cr C4 alkyl Groups consisting of; unsubstituted or mono- or poly-substituted phenyl groups; and unsubstituted or [-poly substituted phenyl groups, where the substituents may be independent of each other, and In the group consisting of 4 free radicals, C 丨 -c4 alkyl groups and halogen-CrC4 alkyl groups; unsubstituted or substituted or soap- or poly-substituted heteroaryl bonded by a ring carbon atom Group, in which the substituents J 乂 疋 of Arl and AI * 2 are independent of each other, and are selected from free halogen, Ci-q alkyl, halogen-cc ^ pn 1 alkyl, (^-(: 4alkoxy and Halogen-Ci-C: in the group consisting of 4 alkoxy groups; (2) having a compound containing the previously provided restriction D θ ^ ', wherein the compound of formula I, wherein Ri is hydrogen, (VC4 alkyl, functional element — c C, Bulkyl; 1 4 or 4 valenyl or (VC4 alkoxymethyl) especially hydrogen, 〇--0 2 alkynyl or halogen-c ~ c produced it is more particularly hydrogen or (^-〇 2 alkynyl; 14 200305556 (3) Compounds of formula I having previously provided restrictions, wherein R2, R3, R4, R5, and R6 are independently of each other hydrogen, halogen, unsubstituted or mono- or polysubstituted Γ ci C4 alkyl, wherein the substituents It may be independent of each other, and in the group consisting of free-nanin and oxy, the C3-C5 ring alkyl group or the unsubstituted or mono- or multiple-substituted substituents may be independent and free to choose; , Cl-C4 group, Cl-Cj oxygen group, and sulphur group; 14 alkoxy group is especially a hydrogen group, which is independent of each other, unsubstituted Cl-C4 group, Wherein the substituents can be independent of each other, and can be freely selected from the group consisting of alkoxy, and more specifically, independently of each other, hydrogen, s 3 ~ C5 cycloalkyl; Cl-C2 alkyl or VC5 ring (4) has the restriction bar provided previously where W is 0 or S; compound 'which is especially 0; (5) with Has a restriction bar provided previously where a is 1, 2 or 3; a compound, which is especially 1 or 2; more particularly 1; (6) has a restriction bar provided previously which contains b, 0, 1 or 2; formula 1 compound, especially 0 or 1; more particularly 0; 15 200305556 (7) a compound of formula i containing the previously provided restrictions, wherein ^ and "Arz are independently unsubstituted or monovalent -Or poly-substituted aryl groups, in which the substituents of ΑΓι & Arz are independently selected from free radicals, nitro, cyano, Ci-C6 alkyl, halogen-Ci-C6 alkyl 'alkoxy, halogen-CVC6 Alkoxy, C: 3-C6 cycloalkyl, CVC6 alkylsulfonyl, halogen A-c6 alkylsulfonyl, Cl-c6 alkylamino, di-Ci_C6 alkylamino, alkylcarbonyl, halogen- CrC6 alkylcarbonyl, Cl-C6 alkoxycarbonyl, Ci-Ce alkylaminocarbonyl and di-Cl-C6 alkylaminocarbonyl groups; 6 unsubstituted or mono- or polysubstituted Phenylcarbonyl; unsubstituted or mono- or polysubstituted phenyl, wherein the substituents can be independent of each other, and can be selected from Li, nitro, cyano, Ci-C6 alkyl, -C "C6 alkyl, C] -C6 alkoxy and dentin_Ci_C6 alkoxy group; unsubstituted or mono- or poly-substituted phenoxy group, wherein the substituent may be Are independent of each other, and are selected from the group consisting of oxin, nitro, cyano, alkyl, halo-dagger 6 alkyl, C1-Ce alkoxy, and oxin-C1-Ce alkoxy; and Unsubstituted or mono- or multi-substituted pyrimidinyloxy, the substituents in j may be independent of each other, and can be selected from free nitro, nitro, lutyl, CrC6 alkyl, and dentin In the group consisting of aryl, Ci-C6 alkoxy, and oxin-C1-C6 alkoxy; or unsubstituted or mono- or poly-substituted heteroaryl groups bonded by a ring carbon atom ' Among them, the substituents of Ari and Ar2 may be independent of each other, and may be selected from free radicals, nitro groups, cyano groups, C6 alkyl groups, halogen-CrC6 alkyl groups,

Cl—C6烷氧基、鹵素—c厂(：6烷氧基、CrC6烷基磺醯基、鹵素Cl-C6 alkoxy, halogen-c plant (: 6 alkoxy, CrC6 alkylsulfonyl, halogen

CrC6烧基確gf基、Ci-Ce烷胺基及二—C1_C6烷胺基所組成 的族群中； 16 200305556CrC6 alkyl group is composed of gf group, Ci-Ce alkylamino group and di-C1_C6 alkylamine group; 16 200305556

Ri是氫、CrC4烷基、鹵素—Ci-C4烷基或Cl_C4烷氧基 曱基； R2、1、R4、R5及Re互相獨立地是氫、鹵素、未經取 代的或經單-或多取代的（：厂(：4烷基，其中取代基可以是互 相獨立，並且選擇自由_素及Ci-C4烷氧基所組成的族群 中；CfC5環烷基或未經取代的或經單—或多取代的苯基， 其中取代基可以是互相獨立，並且選擇自由鹵素、Ci—q烷 基、鹵素烷基、CrC：4烷氧基及鹵素一Ci_c4烷氧基所 籲 組成的族群中； W是0或S ; a是1、2或3 ;以及 b是0、1或2 ; (8)具有包含先前提供的限制條件之式I化合物，其 中人“及Aq互相獨立地是未經取代的或經單—或多取代的 芳基，其中Aq及Aq的取代基互相獨立，係選擇自由鹵素 、硝基、氰基、CrC6烷基、鹵素一 CrC6烷基、q —。烷氧基鲁 、函素-c「c6^氧基、C「C6環烧基、Ci—Ce烧基毅基及㈣ -CrG烷基羰基所組成的族群中；未經取代的或經單-或多 取代的苯基幾基；未經取代的或經單— 其中取代基可以是互相獨立，並且選擇自由函素、氛基、 烷基及函素一Ci_c6烷基所組成的族群中；以及未經取 代的或經單-或多取代的苯氧基，其中取代基可以是互相 獨立，並且選擇自由㈣、氰基Ά烧基及函素_Ci_c6 燒基所組成的族群中；< 17 200305556 藉由環碳原子而鍵結之未經取代的或經單—或多取代的 雜芳基，其中Ar!及Ah的取代基可以是互相獨立，並且選 擇自由鹵素、氰基、Ci-C6烷基、鹵素—Ci—Ce烷基、Ci—C6烷 氧基及鹵素-Ci_c6烧氧基所組成的族群中； R!是氫、烧基或鹵素-(^-〇2燒基； R2、I、R4、R5及Re互相獨立地是氫、未經取代的或 經單-或多取代的CrQ烷基，其中取代基可以是互相獨立 ’並且選擇自由_素及q-C2烧氧基所組成的族群中戍 C3 - (：5環烷基； W是0 ; a是1或2 ;以及 b是0或1 ; (9 )具有包含先前提供的限制條件之式I化合物，其 中ΑΓι& Arz互相獨立地是未經取代的或經單—或多取代的 务基’其中Ar!及Ah的取代基互相獨立，係選擇自由幽素 、氰基、（Vc4烷基、i素-Cl-C4烷基、Ci—c4烷氧基、齒素 -Ci-C4烷氧基、C；3-C5環烷基、CrC4烷基羰基及鹵素—Ci—C4 烧基羰基所組成的族群中；未經取代的或經單—或多取代 的苯基獄基；以及未經取代的或經單-或多取代的苯基， 其中取代基可以是互相獨立，並且選擇自由鹵素、C「C4烷 基及鹵素-CrC4烷基所組成的族群中；或 藉由環碳原子而鍵結之未經取代的或經單—或多取代的 雜芳基，其中ΑΓι& Aq的取代基可以是互相獨立，並且選 擇自由鹵素、(VC4烷基、鹵素—。丨一匕烷基、。厂。烷氧基及 鹵素-Ci-C4烷氧基所組成的族群中； 200305556Ri is hydrogen, CrC4 alkyl, halogen-Ci-C4 alkyl or Cl_C4 alkoxyfluorenyl; R2, 1, R4, R5 and Re are independently of each other hydrogen, halogen, unsubstituted or mono- or poly Substituted (: factory (: 4 alkyl groups, where the substituents can be independent of each other, and can be selected from the group consisting of _ prime and Ci-C4 alkoxy group; CfC5 cycloalkyl or unsubstituted or mono- Or poly-substituted phenyl, wherein the substituents may be independent of each other, and selected from the group consisting of halogen, Ci-q alkyl, halogen alkyl, CrC: 4 alkoxy, and halogen-Ci_c4 alkoxy; W is 0 or S; a is 1, 2 or 3; and b is 0, 1 or 2; (8) a compound of formula I having the previously provided restrictions, wherein human "and Aq are independently unsubstituted from each other Or mono- or poly-substituted aryl groups, in which the substituents of Aq and Aq are independent of each other, and are selected from free halogen, nitro, cyano, CrC6 alkyl, halogen-CrC6 alkyl, and q-.alkoxylu , Halo-c "c6 ^ oxy, C" C6 cycloalkyl, Ci-Cealkyl, and ㈣-CrG alkylcarbonyl group; unsubstituted or Mono- or poly-substituted phenyl groups; unsubstituted or mono --- where the substituents can be independent of each other and selected from the group consisting of free-functional groups, aryl groups, alkyl groups, and functional group-Ci_c6 alkyl groups ; And unsubstituted or mono- or poly-substituted phenoxy, in which the substituents may be independent of each other, and selected from the group consisting of fluorenyl, cyanofluorenyl, and halo_Ci_c6 alkyl; & lt 17 200305556 Unsubstituted or mono- or poly-substituted heteroaryl bonded by a ring carbon atom, wherein the substituents of Ar! And Ah may be independent of each other, and free halogen, cyano, Ci -C6 alkyl group, halogen-Ci-Ce alkyl group, Ci-C6 alkoxy group and halogen-Ci_c6 alkyloxy group; R! Is hydrogen, alkyl or halogen-(^-〇2alkyl); R2, I, R4, R5 and Re are independently of each other hydrogen, unsubstituted or mono- or poly-substituted CrQ alkyl, wherein the substituents may be independent of each other 'and the choice of free element and q-C2 oxygen的 C3-(: 5 cycloalkyl; W is 0; a is 1 or 2; and b is 0 or 1; (9) The compound of formula I, in which ΑΓι & Arz is independently unsubstituted or mono- or multi-substituted, is provided as a constraint, wherein the substituents of Ar! And Ah are independent of each other. (Vc4 alkyl, i-Ci-C-C4 alkyl, Ci-c4 alkoxy, halo-Ci-C4 alkoxy, C; 3-C5 cycloalkyl, CrC4 alkylcarbonyl and halogen-Ci —C4 alkyl group; unsubstituted or mono- or poly-substituted phenylhexyl; and unsubstituted or mono- or poly-substituted phenyl, wherein the substituents may be each other Independent and selected from the group consisting of halogen, C, C4 alkyl and halogen-CrC4 alkyl; or unsubstituted or mono- or poly-substituted heteroaryl groups bonded by a ring carbon atom, Wherein the substituents of ΑΓι & Aq may be independent of each other, and free halogen, (VC4 alkyl, halogen-) are selected.丨 A dagger alkyl ,. plant. In the group consisting of alkoxy and halogen-Ci-C4 alkoxy; 200305556

Ri是氫或CrQ烷基； 1h、匕及h互相獨立地是氫 c3-c5環燒基； w是0 ;Ri is hydrogen or CrQ alkyl; 1h, d and h are independently of each other hydrogen c3-c5 cycloalkyl; w is 0;

Ci-C2烧基或 a是1 ;以及 b是〇 〇 在本發明内容的範圍内，特別較佳者為在表丨中所列牛的式I化合物，以及更特別者為在合成實施例中所提及 的式I化合物。 本發明之另一標的是製備式I化合物之方法，在每個 例子中’係以游離的形式或以鹽的形式而製備，例如，該 方法包括將式丨〗之化合物： β R1. «2 «3-(?)a-WHAr2 H CN I I R4 Re N· H， 其為已知的化合物或可類似於有關的已知化合物 備’以及其中 R1、R2、R3、R4、R5、R6、W、Ar2、a 及 如式I之定義，與式n〗之化合物反應：Ci-C2 alkyl or a is 1; and b is 0. Within the scope of the present invention, particularly preferred are the compounds of formula I listed in Table 丨, and more particularly in the synthesis examples The compounds of formula I mentioned. Another subject of the present invention is a method for preparing a compound of formula I. In each example, 'is prepared in free form or in the form of a salt. For example, the method includes converting the compound of formula 丨〗: β R1. «2 «3-(?) A-WHAr2 H CN II R4 Re N · H, which is a known compound or can be similar to the related known compound, and where R1, R2, R3, R4, R5, R6, W , Ar2, a and as defined in Formula I, react with a compound of formula n〗:

而製 b是And system b is

An—^丨1丨，Ο 其為已知的化合物或可類似於有關的已知化合物而製 備’以及其中Ari是如式I之定義，以及Q是離去基，必 19 200305556 要二：驗性催化劑的存在下反應；以及在每個例子中， 如果㈤要的話，將本發明方法或其他方式 合物，以游離的形式或以鹽的形式勺式 ^-將本發明方法所得的異構物之二== 刀離所要的異構物；及/或將本發明方 化合物轉換成鹽類，或將本發明方法所得的式Γ二:： 鹽類，轉換成式！之游離化合物或其他鹽類。化5物之 方式二二:广1之鹽類，也可相似地以關於其鹽類之 上及以下所提及的原料。 反應物可以例如3^ ^ ^…t ,— 田熔的形式而互相反應，也就是不須 加入溶劑或稀釋劑。然而，在大部分的例子中，加= 溶劑或稀釋劑或其混合物 、 之實例是：芳香! °14樣的溶劑或稀釋劑 ,, θ 、及月曰锿族碳氫化合物以及鹵化 Γ:Γ例如1、甲苯、二甲苯、…甲基 本、奈滿、氣苯、二裹絮 、一 — /、、溴本、石油醚、己烷、環己烷 二丙基St、二異丙基 乙二醇單甲基醚、乙 甲氧基二乙基鱗、四 丙酮、曱基乙基酮或 ::甲：、三氣甲院、四氯甲烧、二氣乙烧、三 或四風乙H例如，二乙_ 鱗、二丁基喊、第三-丁基甲基鱗 二醇單乙基醚、乙二醇二甲基醚、 氧雜環己烧；嗣，例如一… :;土 SR ’醯胺，例如，二 乙基甲醯胺、Ν，恥二 基鱗酸三醢胺；睛：=乙酸胺、Ν-甲基姐㈣酮或六甲 ，二甲基亞硼。]如，乙睛或丙腈；以及亞碾，例如 20 200305556 較佳的離去基Q是l|素、曱苯磺酸鹽、甲磺酸鹽及三 敦甲績酸鹽’特別較佳是_素，特別是氣。 適合於促進反應的鹼是例如，鹼金屬或鹼土金屬的氫 氧化物、氫化物、醯胺、烷酸鹽、醋酸鹽、碳酸鹽、二烷 基龜胺或烧基曱石夕烧基醯胺、烧基胺、烧撐二胺（若須要 ，係N-烧基化及飽和或不飽和的）、環烷基胺、鹼性雜環 、氫氧化錄以及碳環胺。例如，氫氧化鈉、氫化鈉、氨基 化鈉、甲酸鈉、醋酸鈉、碳酸鈉、第三_ 丁酸鉀、氫氧化 鉀、碳酸鉀、氫化鉀、二異丙基氨基化鋰、雙（三曱基曱 石夕烧基）氨基化鉀、氫化鈣、三乙基胺、二異丙基乙基胺 、二乙二胺、環己基胺、N-環己基-N，N-二甲基胺、n，N-二 乙基苯胺、吡啶、4-(N，N-二甲基胺基）毗啶、奎寧環（ Quinuclidine) 、N-曱基嗎啉、苄基三曱基氫氧化銨以及 1，5-二氮雜二環[5·4〇]十一碳-5 —烯（I)BU)。較佳是二異 丙基乙基胺以及4-（Ν，Ν-二甲基胺基）吡啶。 反應有利地是在約〇°C至約+1〇〇°c的溫度進行，較佳 是從約l〇°C至約+4〇°c。 在較佳的方法中，式11化合物是在函化的碳氫化合物 中（車乂佳疋二氣甲烧）’在驗的存在下（較佳是二異兩美 乙基胺以及4-(N，N-二甲基胺基）吡啶之混合物），與气 111化合物於周圍溫度下反應。 本發明之另一標的是製備式11化合物之方法，在每個 例子中，係以游離的形式或以鹽的形式而製備，例如，▲ 方法包括將式IV之化合物： 21 200305556An— ^ 丨 1 丨, 〇 It is a known compound or can be prepared similar to related known compounds' and where Ari is as defined in Formula I and Q is a leaving group, it must be 19 200305556 Reaction in the presence of a basic catalyst; and in each case, if necessary, the method of the present invention or other means is compounded in free form or in the form of a salt ^-isomerized by the method of the present invention The second thing is == the desired isomer; and / or the formula compound of the present invention is converted into a salt, or the formula Γ2 obtained by the method of the present invention is: a salt, converted into a formula! Free compounds or other salts. The way to make 5 things 22: The salt of Guang 1 can be similarly made with the raw materials mentioned above and below. The reactants can react with each other in the form of, for example, 3 ^^^ ... t, ie, without adding a solvent or diluent. However, in most cases, the solvent or diluent or mixture thereof is added. Examples are: aromatic! ° 14-like solvents or diluents, θ, and 锿 group hydrocarbons and halogenated Γ: Γ For example 1, toluene, xylene, ... methylbenzyl, naman, benzene, dioxane, mono- / ,, bromide, petroleum ether, hexane, cyclohexane dipropyl St, diisopropylethylene Alcohol monomethyl ether, ethoxydiethyl scale, tetraacetone, fluorenyl ethyl ketone or :: A :, Sanqi Jiayuan, tetrachloromethane, digas ethyl, three or four wind ethylH For example, diethylammonium, dibutylammonium, tertiary-butylmethylammonium glycol monoethyl ether, ethylene glycol dimethyl ether, oxetane; 嗣, such as one ...:; soil SR '醯Amines, for example, diethylformamidine, N, triamidine diammonium phosphonate; eyes: = amine acetate, N-methylacetophenone or hexamethylene, dimethylboron. ] For example, acetonitrile or propionitrile; and sub-mills, such as 20 200305556, the preferred leaving group Q is l | _ Prime, especially Qi. Suitable bases for accelerating the reaction are, for example, hydroxides, hydrides, ammonium amines, alkanoates, acetates, carbonates, dialkylpyrimidines, or pyroxylpyridylamines of alkali or alkaline earth metals , Alkylamine, alkylenediamine (N-alkylated and saturated or unsaturated if necessary), cycloalkylamine, basic heterocyclic ring, hydroxide and carbocyclic amine. For example, sodium hydroxide, sodium hydride, sodium amide, sodium formate, sodium acetate, sodium carbonate, potassium tertiary butyrate, potassium hydroxide, potassium carbonate, potassium hydride, lithium diisopropylamide, bis (triamidine Arsenite) potassium amide, calcium hydride, triethylamine, diisopropylethylamine, diethylenediamine, cyclohexylamine, N-cyclohexyl-N, N-dimethylamine, n, N-diethylaniline, pyridine, 4- (N, N-dimethylamino) pyridine, quinuclidine, N-fluorenylmorpholine, benzyltrimethylammonium hydroxide, and 1,5-diazabicyclo [5 · 4〇] undec-5-ene (I) BU). Diisopropylethylamine and 4- (N, N-dimethylamino) pyridine are preferred. The reaction is advantageously carried out at a temperature of about 0 ° C to about + 100 ° C, preferably from about 10 ° C to about + 40 ° C. In a preferred method, the compound of formula 11 is in a functionalized hydrocarbon (Carbonium dipyridine) in the presence of a test (preferably diisoamylethylamine and 4- ( N, N-dimethylamino) pyridine mixture), reacts with the gas 111 compound at ambient temperature. Another subject of the present invention is a method for preparing a compound of formula 11, in each case, it is prepared in free form or in the form of a salt. For example, the method includes the compound of formula IV: 21 200305556

其為已知的化合物或可類似於有關的已知化合物而製 備X及其中、R3、R4、R5、W、Ar2、a及b是如式 I之疋義，與無機或有機氰化物以及式Ri—之化合物反 應，其為已知的化合物或可類似於有關的已知化合物而製 。、及中h疋如式I之定義；以及在每個例子中，如 “ ^ 將本發明方法或其他方式所得到的式11化合 物:以游離的形式或以鹽的形式，轉換成式II的其他化合 物’將本發明方法所得的異構物之混合物加以分開，並分 離所要的異構物；及/或將本發明方法所得的式n之游離 化合物轉換成鹽類’或將本發明方法所得的式合物之 鹽類，轉換成式11之游離化合物或其他鹽類。It is a known compound or can be prepared similarly to the related known compound. X and R3, R4, R5, W, Ar2, a, and b are as defined in Formula I, and inorganic or organic cyanide and formula Ri-compound reaction, which is a known compound or can be made similar to the related known compound. , And h 疋 are as defined in Formula I; and in each case, such as "^ the compound of Formula 11 obtained by the method of the present invention or other methods: in free form or in the form of a salt, is converted into a compound of Formula II Other compounds 'separate the mixture of isomers obtained by the method of the present invention and isolate the desired isomers; and / or convert the free compounds of formula n obtained by the method of the present invention into salts' or by the method of the present invention The salt of the compound of formula is converted into the free compound of formula 11 or other salts.

適合的氰化物是氰化納、氰㈣、三甲基甲㈣基氛 化物以及丙顚I氰醇。 對於例如式1v之幾基化合物與例如式r6-nh2之氣化 及醯胺的反應之-般方法’是已知為streeker ^^Or.anic Synthesis Coll. 3：88 ( 1973 ) o 化：：丨的鹽類可以本身已知的方式而製備。因此 子二:;Γ的酸加成鹽可藉由以適合的酸或適合的纟 子父換斌劑處理而獲得， 心七、“ 于Μ及具有鹼的鹽類可藉由以適< 的鹼或適合的離子交換試劑處理而獲得。 22 200305556 化合物I的鹽類可藉由一妒的 儿入… 由身又的方式，而轉換成游離的 化合物I、酸加成鹽（例如，夢 精由以適合的鹼試劑或適合 的離子交換試劑處理）以及星 飞、口 /、百鹼的鹽頬（例如，藉由以 適合的酸或適合的離子交換試劑處理）。 化合物I的鹽類可以本身 十5 〇知的万式，而改變成化合Suitable cyanide compounds are sodium cyanide, cyanocyanine, trimethylformamyl, and propanyl I cyanohydrin. A general method for the reaction of several base compounds such as formula 1v with gasification and amidine such as formula r6-nh2 is known as streetker ^ Or.anic Synthesis Coll. 3:88 (1973). The salts can be prepared in a manner known per se. Therefore, the acid addition salt of Γ can be obtained by treatment with a suitable acid or a suitable parent-exchanger. Xin VII, "Salts with M and bases can be prepared with 〈 It can be obtained by treatment with alkali or suitable ion exchange reagents. 22 200305556 Salts of compound I can be converted into free compound I, acid addition salt (eg, dream essence) by envy Treated with a suitable base reagent or a suitable ion-exchange reagent) and Xingfei, Oral / Hexaline salts (for example, by treatment with a suitable acid or a suitable ion-exchange reagent). The salts of Compound I may be It ’s ten thousand things that you know, and change into a combination

物I的其他鹽類；酸力〇成g| I 丄^ 风a了轉換成其他的酸加成鹽，例 如，在一適合的溶劑中，μ ώ⑽_ 稭由將無機酸的鹽類（例如，_ 酉夂鹽）以適合的酸之金屬_ Γ 皿 卢理", n (例如，鈉鹽、鋇鹽或銀鹽） 處理，例如，以醋酸銀處理’其中所得的無㈣（例如， 乳化銀）是不溶性的，並因此可從反應混合物中沈殿出來。 根據所使用的方法或反應條俾 人从了 薦怿件，具有鹽形成特徵的化 σ ，可以游離的形式或以鹽類的形式而獲得。 化合物I也可以其水合物的 ^ ^ 观们小式而獲得，及/或也可包 括其他的溶劑，例如，當需要時 ^ 田而罟時该浴劑可用於以固體形 式存在的化合物之結晶。 化合物I可例如，根據不斜 不對％奴原子的數目、絕對及 相對組態，而以可能的異構物 ^ . 次彼專化合物的形式而 存在，如純的異構物形式（例 D, w u戈 九學異構物及/或非對 映異構物），或如異構物的混合 礼^、 Λ 匕σ物形式（例如，對映異構 物的混e物’例如，外消你从 , 非對映異構物的混合物或 卜消旋物的混合物）；本發明是 疋’關於純的異構物以及所 可能的異構物混合物，並且本日^ ^ ^ ^ ^ ^ ^ ^ ^ 升货η之刖以及之後的每個 例子應相同地理解為如此，即 ^ Μ更立體化學的的細節並未在 母個例子中特別指出亦缺。 23 200305556 1根據本發明方法（取決於原料及操作方法的選擇）或 他方式所侍之化合物丨的非對映異構物混合物或外消旋 物的他合物，可在其成份的物理化學差異之基礎上，以已 ^的方式而分離成純的非對映異構物或外消旋物，例如， 糟由部份結晶、蒸餾及/或色層分析而分離。 ^相同地，所獲得的對映異構物之混合物，例如，外消 旋物’可精由已知的方法而解析為光學異構物，例如，藉 從：子活丨生的溶劑中再結晶；藉由在不對稱的吸附劑上 曰析例如，在乙醯纖維素上進行高效能液態色層分 析（HPLC) ’在適當微生物的協助下，藉由 酵素而切割；經由包涵複合體（incluS1Qnc_lexes)匕的的 形成’例如，利用X料 異構物可被複! 的冠驗，藉此只有一個鏡像立體 除了經由對應的異構物混合物之分離外 :非：映異構物或對映異構物，也可經由-般已知的= :立體選擇性或對映立體選擇性之合成而獲得，例如: 出由:行本發明之方法，利用具有同樣適合的立體化學之； 對映效性的異構物(例如， 合物）是有利的二接/吧5物（例如，對映異構物之混 在太菸 月:獒為個別的成份具有不同的生物活性。 ^时法t，所使料原料及+ 產是:產生-開始說明之特別有效的化合物〗= 24 200305556 本發明特別是有關於在實施例中所說明的製備方法。 本發明用於製備新穎的化合物I所使用之原料及中間 產物，以及其用途及製備方法，也相同地構成本發明之標 的。Acid I to other salts; acidity 0 to g | I 丄 ^ a is converted to other acid addition salts, for example, in a suitable solvent, μ ⑽_ straw from inorganic acid salts (for example, _ Osmium salt) treated with a suitable acid metal Γ 卢 Luli ", n (for example, sodium, barium, or silver salt) treatment, for example, with silver acetate treatment 'the erbium-free (for example, emulsification) Silver) is insoluble and can therefore be removed from the reaction mixture. According to the method or reaction method used, people have recommended that the chemical σ with salt formation characteristics can be obtained in free form or in the form of salts. Compound I can also be obtained from its hydrated formula, and / or other solvents can also be included, for example, when needed ^ Tian Er 罟 This bath can be used to crystallize the compound in solid form . Compound I can exist, for example, in the form of possible isomers according to the number, absolute, and relative configuration of the non-slanted and misaligned% slave atoms, such as pure isomeric compounds (eg, D, wu Ge Jiu science isomers and / or diastereomers), or as a mixture of isomers ^, Λ σ σ (for example, a mixture of enantiomers' e. You start with, a mixture of diastereomers or a mixture of racemates); the present invention is about the pure isomers and possible isomer mixtures, and today ^ ^ ^ ^ ^ ^ ^ ^ ^ The description of the goods η and every subsequent example should be understood as such, that is, the details of more stereochemistry are not specifically pointed out in the parent example. 23 200305556 1 According to the method of the present invention (depending on the choice of raw materials and operating methods) or the compounds served by other methods 丨 diastereomeric mixtures or racemates other compounds, the physical chemistry of their components can be On the basis of the differences, it is separated into pure diastereomers or racemates in a manner already described, for example, the fraction is separated by partial crystallization, distillation, and / or chromatography analysis. ^ Similarly, the obtained mixture of enantiomers, for example, the racemates, can be resolved into optical isomers by known methods, for example, by using Crystallization; by analysis on an asymmetric adsorbent, for example, high-performance liquid chromatography (HPLC) on acetyl cellulose, with the assistance of appropriate microorganisms, cleavage by enzymes; via inclusion complexes ( incluS1Qnc_lexes) The formation of daggers', for example, the use of X-isomers can be recovered! The crown test, whereby only one mirror stereo in addition to separation through the corresponding mixture of isomers: non: enantiomers or enantiomer Isomers can also be obtained by the synthesis of generally-known =: stereoselectivity or enantioselectivity, such as: by the method of the present invention, using the same suitable stereochemistry; enantiomers Effective isomers (for example, compounds) are advantageous dimers / blocks (for example, enantiomeric mixtures in the smoky moon: 獒 is the individual components with different biological activities. ^ 时 法 t The raw materials and production are: production-start description Particularly effective compound = 24 200305556 The present invention is particularly related to the preparation method described in the examples. The raw materials and intermediate products used by the present invention for preparing the novel compound I, as well as their uses and preparation methods, are the same The ground constitutes the subject of the present invention.

根據本發明，化合物I之特徵是在於特別廣泛的活性 範圍，並且在害蟲控制的領域中是有價值的活性成份，特 別包括寄生動物的體内及體外寄生蟲之控制，但對於溫血 動物、魚類以及植物則是相當具有耐受性的。According to the invention, compound I is characterized by a particularly broad range of activity and is a valuable active ingredient in the field of pest control, including in particular the control of parasites in vivo and in vitro, but for warm-blooded animals, Fish and plants are quite tolerant.

在本發明的說明中，名詞“體外寄生蟲”應理解為特 別是昆蟲、蝨子以及壁蝨。這些包括以下的昆蟲目：鱗翅 目{ Lepidoptera)、鞘翅目(Coleoptera)、同翅目（ Homoptera)、異翅目 Q Heteroptera)、雙翅目{ Diptera )、纓翅目(Thysanoptera)、直翅目{ Orthoptera、、 隱翅目i Anoplura)、管翅目Q Siphonaptera)、食毛目 (Mailophaga )、龜尾❾（Thysanura )、專遂芑 Q I sop ter a ) 、口齒蟲目（尸socopiera ) 以及膜翅目 （ iera )。然而，可被特別提及的體外寄生蟲是會擾 亂人類或動物以及攜帶病原體的體外寄生蟲，例如，蠅類 ，例如，家蠅（)、麗繩（见 vetustissima)、狀家規 i M· autumnal is)、素 1煎鐵{ Fannia canicularis) ' 1¾ 4¾ ( Sarcophaga carnaria)、 銅、綠繩(Lucilia cuprina )、年 1 琢 i Hypoderma bovis )、故皮鐵（ff· Iineatum)、白頭裸金織（C/uysoniyia chloropyga)、尺良織 i Dermatobia hominis)、螺、敬規 25 200305556 { Cochliomyia hominivorax)、綠 ％ 規 i GasterophilusIn the description of the present invention, the term "ectoparasite" is understood to mean especially insects, lice and ticks. These include the following insects: Lepidoptera, Coleoptera, Homoptera, Q Heteroptera, Diptera, Thysanoptera, Orthoptera {Orthoptera, I, Anoplura), Q Siphonaptera, Mailophaga, Thysanura, QI sop ter a), Hymenoptera (socopiera), and membrane Hemiptera (iera). However, ectoparasites that can be specifically mentioned are ectoparasites that disturb humans or animals and carry pathogens, for example, flies, for example, housefly (), fleece (see vetustissima), family rules i. Autumnal is), prime 1 fried iron {Fannia canicularis) '1¾ 4¾ (Sarcophaga carnaria), copper, green rope (Lucilia cuprina), year 1 cut i Hypoderma bovis), old leather iron (ff · Iineatum), white-headed bare gold weaving ( C / uysoniyia chloropyga), Ruler Liangi i Dermatobia hominis), snails, King Rule 25 200305556 {Cochliomyia hominivorax), Green% gauge Gasterophilus

、羊狂繩（(9f/s〇 、鹿螫蠅（ Stomoxys calci trans )、擾血繩(Haematobia irritans );以及蚊蚋類（長角亞目（))，例如，蚊 科（Qz/ic/i/ae )、蚋科（57yz7i////i/ae )、毛蛉科（ 户，還有吸血寄生蟲，例如，跳蚤，例如，猫 蚤(Ctenocephalides felis ) A §r ( Ctenocephalides )(貓及狗的跳蚤）、印度鼠蚤（/⑽叩印厂习 cheopis ) 、k %： i Pulex irritans )、驾良潛 §： i, Sheep mad rope ((9f / s〇, Stomoxys calci trans), haematobia irritans); and mosquito pupae (Longhorn suborder ()), for example, the family Mosquito (Qz / ic / i / ae), Polygonaceae (57yz7i //// i / ae), Ranunculaceae (households, and blood-sucking parasites, for example, fleas, such as Ctenocephalides felis) A §r (Ctenocephalides) (cat And dog flea), Indian rat flea (/ （印 厂 习 cheopis), k%: i Pulex irritans), driving good diving §: i

Derma tophi Jus penetrans );益子，合，J 士口 ，羊蟲（ Damal ina ον is)、頭兹(Pediculus human i s );牛 it 及 馬繩（it科）：馬蜗屬（及ae/z/a ίσρσ ia)，例如，馬绳（及· pluvial is );虹：屬，例如，綠頭虹：（TaAa/^s· nigrovi tta tus);斑虫亡屬(Chrysopsinae) ， 4列士口 ，白虫¢:Derma tophi Jus penetrans); Yizi, He, J Shikou, Sheep Worm (Damal ina ον is), Pediculus human is; Bovine it and Horse Rope (it family): Horse Snail (and ae / z / a ίσρσ ia), for example, horse rope (and · pluvial is); rainbow: genus, for example, green head rainbow: (TaAa / ^ s · nigrovi tta tus); chrysopsinae, 4 columns White bug ¢:

(Chrysops caecutiens);采采蠅，例如，采采繩屬（ 的種類；咬蟲，特別是蟑螂，例如，德國蟑螂 (Blatella german ica )、東方蜚蠊（万/aiia oriental is )、美洲斐蠊（a/z/eryca；7a);兹子，例如， M ^ ( Dermanyssus gallinae )、疮癣美（Sarcoptes scabiei )、丰浪 t% A ( Psoroptes ovis )及齋 A Μ ( )，以及最後但並非最不重要的是壁蝨 。後者是屬於碑目（)。已知代表性的壁蝨是，例 如，牛缉（Boophi】us)、炎缉（Ambiyomma)、簡歌缉（ Anocentor )、车碑（Dermacentor )、嗜群血蜱（ 26 200305556(Chrysops caecutiens); tsetse flies, for example, species of the genus T. genus; biting insects, especially cockroaches, for example, German cockroach (Blatella german ica), Oriental magpie (Aiia oriental is), Ficus americana (A / z / eryca; 7a); Zi, for example, M ^ (Dermanyssus gallinae), Sarcopses scabiei, Fenglang t% A (Psoroptes ovis), and ZAM A Μ (), and finally but not The least important is ticks. The latter belongs to the stele (). Known representative ticks are, for example, Boophi us, Ambiyomma, Anocentor, Dermacentor ) Haemophilus group (26 200305556

Haemaphysal 1 s)、壤 I 缉{ Hyalomma)、硬缉{ Ixodes) 、肖頭蜱（Rhipicentor)、巨足蜱（Margar〇pus)、烏頭 碑 i Rhipicephalus)、軟蜱 Urgas)、刺耳蜱（以 )及鈍緣蜱（)以及類似的壁蝨，其較佳是 寄生於溫血動物中，包括農場動物，例如，牛、豬、綿羊 及山羊；家禽，例如，雞、火雞及鵝；毛皮動物，例如， 紹、狐狸、栗鼠、兔子及類似動物；以及寵物，例如，貓 及狗；還包括人類。 本發明之化合物I也可有效於對抗所有及個別發育階 段的正常敏感性以及有抗性之動物害蟲，例如，昆蟲以及 代表性的蜱目。在本發明的方法中，活性成份的殺昆蟲、 殺卵及/或殺疥蟲作用，可直接地表現於例如殺死害蟲， 這可立即發生或是在若干時間之後才發生（例如，在蛻皮 期間），或殺死它們的卵；或間接地，例如，表現於減少 的印畔化及/或減少的孵化率，其中，優異的作用是相當 於至少50至60%的殺死率（死亡率）。 化合物I也可用於對抗衛生害蟲，特別是雙翅目的麻繩科 (Sarcophagidae )、瘧蚊科（知叩Λ/"办e )及蚊科（ ;直翅目；網翅目（化.，例如，斐蠊 科（幻办e);以及膜翅目’例如，蟻科（/〇r奶·c/^e)。 化合物I對於植物寄生性的蝨子以及昆蟲，也具有持 續的的活性。在蜱目中的葉蟎的例子中，它們可有效於對 抗葉蟎科（(葉蟎屬（以卜卿心5卿. )及（户spp.))的卵、蛹以及成蟲。 27 200305556 它們也高度有效於同翅目的吸蟲，特別是對抗蚜科（ 々7/zWae )、飛蝨科（)、葉蟬科（ )、木蝨科（户)、疮殼蟲科（ Loccidae) 、Μ 疥殼 A 科（Diaspididae)反疥 A 科（ iWop/z/iZ/i/ae)的害蟲（例如，柑橘果實上的銹蜱）；半 翅目、異翅目及纓翅目的害蟲；以及吃植物的鱗翅目、鞘 翅目、雙翅目及直翅目昆蟲。 它們有同樣適合作為在土壤中對抗害蟲的土壤殺蟲劑。 式I之化合物因此是有效於在作物上，例如，榖類、 棉花、稻米、玉米、大豆、馬鈴薯、蔬菜、水果、菸草、 啤酒花、柑橘、鱷梨以及其他作物，對抗所有發育階段的 吸蟲以及食蟲。 式I之化合物也可有效於對抗根瘤線蟲（ )、囊形線 A ( ffeterodera)、根腐線 A ( PratyJenchus )、1 線 A ( Di tylenchus)、穿礼線 A ( Radopholus)、 球莖線蟲（等種類的植物線蟲。 本發明之化合物是特別有效於對抗蠕蟲，其中體内寄 生的線蟲及吸蟲可能是哺乳動物及家禽的嚴重疾病之原因 ，這些動物例如，錦羊、緒、山羊、牛、馬、驢、狗、描 、天竺鼠以及外來的鳥類。這個跡象的典型線蟲是：血線 A ( ffaemonchus)、毛象氣（Thchostrongylus)、奐斯 特氣 A ( Ostertagia)、$田豫象 A ( Nematodirus)、古播 氏線蟲（Cooper/a )、虫回蟲（iscaWs )、鉤蟲（ Bunostonum)、食道線蟲（、查柏亞線 200305556 A i Charbertia、、鞭 A ( Trichuris )、圓轰（ Strongylus )、毛戴象 A ( Trichonema)、網尾線蟲（ ctyocaulus)、毛細象 A ( CapiIlaria)、異 M 象 A ( Jfeterakis)、弓細 A ( Toxocara) 、$% 细 A ( Ascaridia )、洗 A ( Oxyuris)、钩 A ( Ancylostoma)、鉤蟲（ Z/7?c//7aWa )、毒 4回蟲（Tbzascar/s )以及副 4回蟲（ 户ara w/s)。吸蟲尤其包括片形科（/"asc/Weae)， 特別是肝片吸蟲（/asc/o/a Z/epai/ca)。式I化合物特別 有利的是其可對抗對苯並咪唑類的活性成份有抗性的寄生 蟲之功效。 細頸線蟲、古柏氏線蟲及食道線蟲的特定害蟲種類， 寄生於宿主動物的腸道中，而其他血線蟲及奥斯特線蟲的 種類則寄生於胃部，以及網尾線蟲是寄生於肺部組織。絲 蟲科（及毛線蟲科（SeiaW/i/ae)的寄生蟲 ，可在内部的細胞組織以及器官中發現，例如，心臟、血 管、淋巴管以及皮下組織。特別值得注意的寄生蟲是犬心 絲蟲/歷/i/s)。式I之化合物可高度有效 地對抗這些寄生蟲。 可藉由式I化合物控制的害蟲，也包括以下害蟲：絛 蟲綱（絛蟲），中擬絛蟲科，特別是中 擬絛蟲屬（)，特別是中殖孔絛蟲（见 ;囊宮科，特別是犬腹孔絛蟲 (Djpy】i*diimcanjnuin).，l^%A(JoyeuxjeIIa)，^ 別是帕斯奎立絛蟲（)及雙孔絛蟲 200305556 屬 i Diplopylidium spp. ) ·，认反％ A 科 i Taeniidae)， 特別是豆狀絛蟲（)、鹿絛蟲（7· cerv〇 、羊絛 A C Τ· ovis)、水泡絛 A C Τ· Ziyc/atigena )、多頭％ A ( T· multiceps )、巨頸絛蟲（7· iae/?/ae/anz//s)、連節絛蟲（7· 及包生絛蟲 屬（fc/z/^oci/cci/s1 spp.);特別較佳是水泡絛蟲、羊絛蟲 、多頭絛蟲、連節絛蟲；細粒絛蟲（方· 及多 房型絛蟲（方· )以及多頭絛蟲 （Haemaphysal 1 s), I {Hyalomma, Ixodes, Rhipicentor, Margaroopus, Rhipicephalus, Urgas, Ixodes And ticks () and similar ticks, which are preferably parasitic in warm-blooded animals, including farm animals, such as cattle, pigs, sheep, and goats; poultry, such as chickens, turkeys, and geese; fur animals, such as , Shao, fox, chipmunk, rabbit and similar animals; and pets, such as cats and dogs; also humans. The compound I of the present invention is also effective against normal and sensitive animal pests of all and individual developmental stages, such as insects and representative ticks. In the method of the present invention, the insecticidal, egg-killing and / or tapeworm-killing effects of the active ingredients can be directly manifested, for example, by killing pests, which can occur immediately or only after a certain period of time (e.g., molting Period), or kill their eggs; or indirectly, for example, by reduced indipration and / or reduced hatchability, where the superior effect is equivalent to a kill rate (death of at least 50 to 60%) rate). Compound I can also be used to combat health pests, in particular Sarcophagidae, Diptera (Knowledge Λ / " Office e), and Mosquito (; Orthoptera; Reticulata). For example, Phytophidae (Phantoms e); and Hymenoptera 'for example, Formicidae (/ 〇r 奶 · c / ^ e). Compound I also has sustained activity against plant-parasitic lice and insects. In the case of the spider mites in the tick order, they are effective against eggs, maggots, and adults of the family Tetranychus ((Tetranychus (with Pu Qingxin 5 Qing.) And (House spp.)). 27 200305556 They It is also highly effective against trematodes of the same order, especially against aphids (科 7 / zWae), planthoppers (), leafhoppers (), psyllids (house), locust families (loccidae), Μ Pests of the Diaspididae (IWop / z / iZ / i / ae) family (eg, rust ticks on citrus fruits); pests of the order Hemiptera, Heteroptera, and Tadpoles; and eating Plants of the order Lepidoptera, Coleoptera, Diptera and Orthoptera. They have the same soil insecticides that are suitable for combating pests in the soil. The compounds of formula I are therefore Effective on crops, such as crickets, cotton, rice, corn, soybeans, potatoes, vegetables, fruits, tobacco, hops, citrus, avocado and other crops, against trematodes and insectivores at all stages of development. The compounds are also effective against Rhizobium nematodes (), ffeterodera, PratyJenchus, Di tylenchus, Radopholus, bulbous nematodes (and other species Plant nematodes. The compounds of the present invention are particularly effective against worms, in which endoparasitic nematodes and trematodes can be the cause of serious diseases in mammals and poultry, such as, for example, Jin sheep, thread, goats, cattle, horses , Donkey, dog, drawing, guinea pig, and exotic birds. Typical nematodes of this sign are: bloodline A (ffaemonchus), wool elephant gas (Thchostrongylus), osteoblast A (Ostertagia), $ 田 余 象 A (Nematodirus ), Cooper / a, iscaWs, Bunostonum, esophageal nematodes (, Chaboa 200305556 A i Charbertia, Trichuris) , Strongylus, Trichonema, ctyocaulus, CapiIlaria, Jfeterakis, Toxocara, $% Ascaridia ), Wash A (Oxyuris), Hook A (Ancylostoma), Hookworm (Z / 7? C // 7aWa), 4 worms (Tbzascar / s), and Para 4 worms (Hara w / s). The trematodes include, in particular, the Fabaceae (/ quot; asc / Weae), in particular the liver trematodes (/ asc / o / a Z / epai / ca). The compounds of the formula I are particularly advantageous in that they are effective against parasites which are resistant to the active ingredients of the benzimidazoles. Species of N. elegans, Cooperia nematodes, and esophageal nematodes are parasitic in the intestinal tract of the host animal, while other species of blood nematodes and Oerste nematodes are parasitic in the stomach, and networms are parasitic in lung tissue . Parasites in the family Filiidae (and SeiaW / i / ae) can be found in internal cellular tissues and organs, such as the heart, blood vessels, lymphatic vessels, and subcutaneous tissues. Particularly noteworthy parasites are dogs Heartworm / calendar / i / s). Compounds of formula I are highly effective against these parasites. Pests that can be controlled by compounds of the formula I also include the following pests: Ascaris (Ascaris), Mesidiomycetidae, especially Mesidiomycetes (), especially Mesoporus (see; Cystaceae, in particular Canine abdominal borer borer (Djpy) i * diimcanjnuin)., L ^% A (JoyeuxjeIIa), ^ Not Pasquilar borer () and Diploid borer 200305556 genus Diplopylidium spp. Taeniidae), especially pea-like roundworms (), deer roundworms (7 · cerv〇, yam 绦 AC Τ · vis), vesicular 绦 AC Τ · Ziyc / atigena), multi-head A (T · multiceps), giant necked worms ( (7 · iae /? / Ae / anz // s), arthropods (7 · and genus Ascaris (fc / z / ^ oci / cci / s1 spp.); Particularly preferred are vesicular tapeworms, sheep tapeworms, Multi-head tapeworms, arthropods; fine-grained roundworms (square · and multilocular tapeworms (square ·) and multi-head tapeworms (

Multiceps multiceps)。 以更特別較佳的方式，水泡絛蟲、豆狀絛蟲、羊絛蟲 、巨頸絛蟲、多頭絛蟲、帕斯奎立絛蟲、犬腹孔絛蟲、中 擬絛蟲屬、細粒絛蟲及多房型絛蟲，是與犬心絲蟲、鉤蟲 屬、弓蛔蟲屬及/或犬鞭蟲（71·叩7;?/^)，同時在狗及貓 上或狗及貓内被控制。也以較佳的方式，貓蚤及/或狗蚤 是與上述的線蟲及絛蟲同時被控制。 式I之化合物也適合於控制人類的病原性寄生蟲。在這 些當中，出現在消化道的典型代表種類是鉤蟲、板口線蟲（ yVecaiar)、虫回蟲、圓蟲、旋毛蟲（TWc/7/；7e//a)、毛細線 蟲、鞭蟲以及蟯蟲（。本發明之化合物也可有 效於對抗出現在血液、組織及各種器官中之絲蟲科吳策線蟲 凰{ Wuchereria)、布魯線蟲屬（及ri/g/a)、靖尾絲蟲屬（ )及羅阿絲蟲屬（Zoa)的寄生蟲，以及也可對 抗特別是感染胃腸道的龍線蟲（，以及類圓 線蟲屬（及旋毛蟲屬的寄生蟲。 200305556 此外，式I之化合物也可有效於對抗在植物以及在人 類及動物中會引起疾病的有害真菌。 本發明式I化合物之優異的除害活性，相當於至少 50-60%的上述害蟲之殺死率（死亡率）。特別地，式1化 合物之特徵是在於非常長的作用期間。 式I之化合物是以其本身的形式而使用，或較佳是與 傳統用於調配技藝中的佐劑一起使用，並可因此以已知的 方式而加工，以得到例％，可乳化的濃縮物、可直接稀釋 的溶液、稀釋乳液、可溶性粉末、在聚合物物質中的顆粒 或微包覆體。應、用方法以及組合物，是根據所要的目的以 及主要的環境而選擇。 包含式I的活性成份，或包含這些活性成份與其他活 性成份以及視需要地固體或液體添加物的組合之調配物（ 也就是組錢、製劑或組合物），是以已知的方式而製造 例士藉由充刀地混合及/或研磨活性成份與補充劑， 例如命刎固體載體以及視需要地表面活性化合物（界 面活性劑）。 ▲以下可使用作為溶劑：醇類，例如，乙醇、丙醇或丁 % ’以及甘醇及其醚類及酯_，例如，丙二醇、二丙二醇 :、乙二醇、乙二醇單甲基醚或單乙基醚；_員，例如， %己酮、異佛爾酮或二丙酮醇；強的極性溶劑，例如，N— 甲基-2 —毗咯烷酮、二甲基亞碾或二曱基甲醯胺；或水；植 *勿油例如/由菜油、萬麻子油、挪子油或大豆油，以及 若須要的話，矽酮油。 31 200305556 用於溫血動物以控制螺虫 J嗝触的較佳應用形式， 、乳液、懸浮液（浸液）、舍口 括，合液 艮口口添加物、粉末、錠劑 括發泡錠）、丸塊、膠囊、n 匕 从膠囊以及潑灑劑（pour_0 之調配物’其中’調配物賦彡 切賦形劑的生理相容性必須 慮。 ’ 用於錠劑及丸塊之適合的 的黏結劑，是可溶於水或醇類 之經化學修飾的聚合天然物暫 員 物貝，例如，澱粉、纖維素或 白質衍生物（例如，甲基_ 蛋 甲暴纖維素、羧基甲基纖維素、 經基乙基纖維素、蛋白皙如 ^ 货白貝例如玉蜀黍蛋白質、明膠以及 似物），以及合成的聚人胳 η 只 例如’聚乙稀醇、聚乙烯听Multiceps multiceps). In a more particularly preferred manner, the vesicular roundworm, pea-shaped roundworm, sheep roundworm, giant-necked roundworm, multihead roundworm, Pasquali roundworm, canine foraminifera, midge tapeworm, fine-grained roundworm, and multilocular roundworm, are It can be controlled on dogs and cats or in dogs and cats simultaneously with heartworm, Hookworm, Toxocara and / or canine whipworm (71 · 叩 7;? / ^). Also in a preferred manner, cat fleas and / or dog fleas are controlled simultaneously with the aforementioned nematodes and roundworms. Compounds of formula I are also suitable for controlling pathogenic parasites in humans. Among these, the typical representative species appearing in the digestive tract are hookworms, yVecaiar, worms, roundworms, trichinella (TWc / 7 /; 7e // a), capillary nematodes, whipworms, and pupae Insects (. The compounds of the present invention are also effective against the worms of the family Filiaceae Wuchereria, B. nematodes (and ri / g / a), and cercariae in blood, tissues, and various organs. Parasites of the genus () and Zoa, as well as worms that can infect the gastrointestinal tract, and parasites of the genus Trichomonas (and Trichinella). 200305556 In addition, The compounds are also effective against harmful fungi that cause disease in plants and in humans and animals. The excellent pesticidal activity of the compounds of the formula I according to the invention is equivalent to at least 50-60% of the killing rate (mortality of the abovementioned pests) ). In particular, the compound of formula 1 is characterized by a very long period of action. The compound of formula I is used in its own form, or preferably with an adjuvant traditionally used in the formulation arts, and can So processed in a known way In order to obtain example%, emulsifiable concentrates, directly dilutable solutions, diluent emulsions, soluble powders, particles or micro-encapsulations in polymer materials. Applications, methods and compositions are based on the desired purpose And the main environment to choose from. Formulations containing active ingredients of formula I, or combinations of these active ingredients with other active ingredients and optionally solid or liquid additives (ie, formulations, preparations, or compositions), are Manufactured in a known manner by mixing and / or grinding the active ingredients with supplements, such as solid carriers and optionally surface-active compounds (surfactants). ▲ The following can be used as solvents: Alcohols, such as ethanol, propanol, or butanol, and glycols and their ethers and esters, such as propylene glycol, dipropylene glycol :, ethylene glycol, ethylene glycol monomethyl ether, or monoethyl ether; Members, for example,% hexanone, isophorone, or diacetone alcohol; strong polar solvents, for example, N-methyl-2 -pyrrolidone, dimethylimine, or dimethylformamide; or Water For example / from vegetable oil, sesame oil, mochi oil or soybean oil, and if necessary, silicone oil. 31 200305556 Preferred application form for warm-blooded animals to control J. snail contact, emulsions, suspensions (Immersion solution), sacrifice, hydration, oral cavity additives, powders, tablets, including foam tablets), pills, capsules, capsules and sprays (the formulation of pour_0 'where') The physiological compatibility of excised excipients must be considered. 'Suitable binders for tablets and pills are chemically modified polymeric natural shellfish soluble in water or alcohol, such as , Starch, cellulose or white matter derivatives (for example, methyl _ egg methyl cellulose, carboxymethyl cellulose, transethyl cellulose, albumin such as ^ white shellfish such as maize protein, gelatin and the like) , And synthetic polymers such as' polyethylene, polyethylene

咯烷酮以及類似物。錠劑★ LC 狄w也包含充填劑（例如，澱粉、Pyrrolidone and the like. Lozenges LC LC also contains fillers (eg, starch,

晶體纖維素、蔗糖、II # ^ I 孔糖寻專）、滑劑以及崩散劑。Crystalline cellulose, sucrose, II # ^ I pore sugar search), lubricant and dispersant.

如果驅蟲劑組合妨7 I 疋^飼料濃縮物的形式而存在的 ，則所使用的載體是例如，古 v & π如，同效能飼料、飼料縠粒或蛋 質濃縮物。除了活性成价十 成知之外，這樣的飼料濃縮物或組合 物也可包含添加物、維决备 > ,士 、生素、杬生素、化學治療劑或其他 的殺蟲劑，主要是抑餡劍 4/ 士 _ Μ、抑真菌劑、抑球蟲劑，或甚至 是荷爾蒙製劑、具有人忐上 /、令口成代謝作用的物質，或可促進生長 、影響屠宰動物的囱皙―、〜4 貝或以其他的方式有益於生物體的物 質。如果包含其中的4 Τ τ曰]式I之組合物或活性成份，直接加到 動物飼料或飲水槽中，丨— r 則元成的飼料或完成的飲水較佳地 包括7辰度約0·〇〇〇5 $ π 〇·〇2重置％ (5-200 ppm)之活性成 份0 32 200305556 本發明之式i化合物可單獨地使用，或併用其他的殺 生物劑。它們可併用例如，具有相同作用方向（以增加作 用）的殺蟲劑，或可併用具有另—作用以（以可擴大活 性範圍殺蟲劑。它們也可合理添加可驅蟲的物質，即 已知的驅蟲劑。如果需要擴展有關體内寄生蟲（例如，蠕 蟲）的活性範圍的話，則式I化合物可適當地併用具有殺 體内寄生蟲性質的物質。它們也可自然地併用抗菌組合物 由於式I化a物疋殺成蟲藥，也就是，由於它們是特別 有效於對抗標的寄生蟲的成蟲階段，因此，添加可代替攻 擊寄生蟲的幼蟲階段之殺蟲劑，可以是非常有利的。以此 方式m大量經濟損I的最大部分之寄生蟲，將可被 涵蓋。此外，這個作用將實質上避免抗藥性的形成。許多 的組合物也可產生協同效果，也就是，可減少活性成份的 總量，這是從經濟的觀點所需要的。併用參與物的較佳族 群以及特別較佳的併用參與物在之後會提及，除了式丨化 合物之外，組合物還可包括一種或多種的這些參與物。 在混合物中之適合的參與物包括殺生物劑，例如，具 有不同作用機轉的殺昆蟲劑及殺疥蟲劑，其命名如下並且 已為熟悉於此技藝中之人士所長久已&，例如，幾丁質人 成抑制劑、生長調控劑；扮演幼蟲荷爾蒙的活性成份二 演殺成蟲劑的活性成份·，廣泛的殺昆蟲劑；廣泛的二疥二 劑及殺線蟲劑；以及也包含熟知的驅蟲藥及抑制昆蟲及/ 或疥蟲的物質，已知為驅蟲劑或剝離劑。 適合的殺昆蟲劑及殺疥蟲劑之非限制性實例是· 33 200305556 1.阿巴汀（Abamectin) 34.氯乙氧福（Chlorethoxyfos ) 67.依第磷（Etrimphos) 2. AC 303 630 35·克凡派（Chlorfenapyr) 68.芬滅松（Fenamiphos) 3.高滅磷（Acephate) 36.克福隆（Chlorfluazuron) 69.芬殺（Fenazaquin) 4.阿納寧（Acrinathrin) 37.氯甲硫磷（Chlormephos) 7〇·芬佈賜（Fenbutatinoxid) 5.棉鈴威（Alanycarb) 38.陶斯松（Chlorpyrifos) 71.撲滅松（Fenitrothion) 6.得滅克（Aldicarb) 39.順式-列滅寧（Cis-Resmethrin) 72. 丁基滅必蟲（Fenobucarb) 7·阿賽滅寧（α-Cypermethrin ) 40.克賽寧（Clocythrin) 73.芬硫克（Fenothiocarb) 8.亞滅寧（Alphamethrin) 41.克芬（Clofentezin) 74·芬諾克（Fenoxycarb) 9.三亞滿（Amitraz) 42.氰乃松（Cyanophos) 75·芬普寧（Fenpropathrin) 10.艾爾瑪克丁 B1 ( Avermectin B1 ) 43.乙氰菊酯（Cycloprothrin) 76.芬必瑞（Fenpyrad) 11. AZ 60541 44.賽扶寧（Cyfluthrin) 77·芬普滿（Fenpyroximate) 12.谷硫鱗 E (AzinphosA) 44.錫蹣丹（Cyhexatin) 78.芬殺松（Fenthion) 13.甲基谷硫磷 46. D 2341 79.芬化利（Fenvalerate) 14.亞環錫（Azocyclotin) 47.第滅寧（Deltamethrin) 80.芬普尼（Fipronil) 15.枯草桿菌毒素 48.滅賜松 M (DemetonM) 81.扶吉胺（Fluazinam) 16.免敵克（Bendiocarb) 49.滅賜松 S (DemetonS) 82.氟佐隆（Fluazuron) 17·免扶克（BenfUracarb) 50.滅賜松-S-甲基 83.氟環腺（flucycloxuron) 18.免速達（Bensultap) 51.除線磷（Dichlofenthion) 84.氣賽寧（Flucythrinate) 19.貝賽扶寧（/3-Cyflmhrin) 52·代立磷（Dicliphos) 85.氣芬隆（Flufenoxuron) 20.畢芬寧（Bifenthrin) 53.代依松（Diethion) 86.氟芬普（Flufenprox) 21. 丁基滅必蝨（BPMC) 54.二福隆（Diflubenzuron) 87.大福松（Fonophos) 22.布芬普（Brofenprox) 55.樂果（Dimethoat) 88·福木松（Formothion) 23·溴硫磷 E (BromophosE) 56.二甲基乙烯磷（ Dimethylvinphos ) 89.福賽多（Fosthiazate) 24.必克蟲（Bufencarb) 57.大克松（Dioxathion) 90.福芬普（Fubfenprox) 25.布芬淨（Buprofezin) 58. DPX-MP062 91.HCH 26.布托卡新（Butocarboxim) 59.護粒松（Edifenphos) 92.飛達松（Heptenophos) 27. 丁基毗啶苯 （ Butylpyridaben) 60.依瑪克丁（Emamectin ) 93·六伏隆（Hexaflumuron) 28.硫線磷（Cadusafos) 61.安殺番（Endosulfan) 94.合賽多（Hexythiazox) 29.加保利（Carbaryl) 62.氰戊菊醋（Esfenvalerate) 95.烯蟲乙酯（Hydroprene) 30.加保扶（CarbofUran) 63·愛芬克（Ethiofencarb) 96.益達胺（Imidacloprid) 31·加保芬寧（Carbophenthion ) 64·愛殺松（Ethion) 97.昆蟲活性真菌 (insect-active Pilze ) 32.培丹（Cartap) 65.依芬寧（Ethofenprox) 98.昆蟲活性線蟲 (insect-active nematoden ) 33.氯乙氧克（Chloethocarb) 66.普伏松（Ethoprophos)If the insect repellent combination is present in the form of a feed concentrate, the carrier used is, for example, an ancient v & pi, such as a feed of equal performance, feed pellets, or egg concentrate. In addition to the active cost of 10%, such feed concentrates or compositions may also contain additives, vitamins, vitamins, biotins, biotins, chemotherapeutics, or other pesticides, mainly Stuffing Sword 4 / Shi_M, fungicides, coccidiostats, or even hormonal preparations, substances that have a metabolizing effect on humans / metabolism, or can promote growth and affect the slaughter of animals- , ~ 4 shells or other substances that are beneficial to the organism. If it contains 4 Τ τ] the composition or active ingredient of formula I is directly added to the animal feed or drinking trough, 丨 -r, preferably the feed or finished drinking water includes 7 degrees about 0 · 〇〇5 $ π 〇2 Reset% (5-200 ppm) of the active ingredient 0 32 200305556 The compound of formula i of the present invention can be used alone or in combination with other biocides. They can be used in combination with, for example, insecticides that have the same action direction (to increase the action), or they can be used in combination with another action (to expand the range of active insecticides. They can also reasonably add insect repellent substances, that is, already If it is necessary to expand the range of activities related to endoparasites (for example, worms), the compounds of formula I can suitably use substances with endoparasite-killing properties. They can also use antibacterial agents naturally. The composition kills adult insecticides because the compounds of formula Ia, that is, since they are particularly effective against the adult stage of the target parasite, it may be very advantageous to add an insecticide that can replace the larval stage of the attack on the parasite. In this way, the largest part of the parasites with a large economic loss will be covered. In addition, this effect will substantially avoid the formation of drug resistance. Many compositions can also produce synergistic effects, that is, can reduce The total amount of active ingredients, which is needed from an economic point of view. Better groups of participants and particularly preferred participants will be mentioned later. In addition to the compound of formula, the composition may also include one or more of these participants. Suitable participants in the mixture include biocides, such as insecticides and insecticides with different mechanisms of action , Its name is as follows and has been long known by those familiar with this technology & for example, chitin human growth inhibitors, growth regulators; active ingredients acting as larval hormones and active ingredients acting as insecticides, widely Insecticides; a wide range of secondary agents and nematicides; and also well-known insect repellents and insect and / or tapeworm-inhibiting substances known as insect repellents or strippers. Suitable insecticides And non-limiting examples of insecticides are 33 200305556 1. Abamectin 34. Chlorethoxyfos 67. Etrimphos 2. AC 303 630 35 Chlorfenapyr 68. Fenamiphos 3. Acephate 36. Chlorfluazuron 69. Fenazaquin 4. Acrinathrin 37. Chlormephos 7 〇 · Fenbutatino xid) 5. Alanycarb 38. Chlorpyrifos 71. Fenitrothion 6. Aldicarb 39. Cis-Resmethrin 72. Butyl (Fenobucarb) 7. α-Cypermethrin 40. Clocythrin 73. Fenothiocarb 8. Alphamethrin 41. Clofentezin 74. Finnock (Fenoxycarb) 9. Amitraz 42. Cyanophos 75 Fenpropathrin 10. Avermectin B1 43. Cycloprothrin 76. Fenbi Fenpyrad 11. AZ 60541 44. Cyfluthrin 77 Fenpyroximate 12. AzinphosA 44. Cyhexatin 78. Fenthion 13 Methyl azinphos-methyl 46. D 2341 79. Fenvalerate 14. Azocyclotin 47. Deltamethrin 80. Fipronil 15. Subtilisin 48. Disinfection DemetonM 81. Fluazinam 16. Bendiocarb 49. DemetonS 82. Fluazuron 17. Freedom BenfUracarb 50. Methison-S-methyl 83. Flucycloxuron 18. Bensultap 51. Dichlofenthion 84. Flucythrinate 19. Besaifu / 3 (Cyflmhrin) 52. Dicliphos 85. Flufenoxuron 20. Bifenthrin 53. Dieth 86. Flufenprox 21. Butanil BPMC 54. Diflubenzuron 87. Fonophos 22. Brofenprox 55. Dimethoat 88 · Formothion 23 · Bronthion E ( BromophosE) 56. Dimethylvinphos 89. Fosthiazate 24. Bufencarb 57 Dioxathion 90. Fufenprox 25. Buprofezin) 58. DPX-MP062 91. HCH 26. Butocarboxim 59. Edifenphos 92. Heptenophos 27. Butylpyridaben 60. Emamectin 93. Hexaflumuron 28. Cadusafos 61. Endosulfan 94. Hexythiazox 29. Canada Carbaryl 62. Esfenvalerate 95. Hydrorene 30. CarbofUran 63 · Ethiofencarb 96. Imidacloprid 31 · Jiabao Carbophenthion 64. Ethion 97. Insect-active Pilze 32. Cartap 65. Ethofenprox 98. Insect-active nematoden 33. Chloethocarb 66. Ethoprophos

34 200305556 99.昆蟲活性病毒 (insect-active viruses ) 132.伏殺磷（Phosalone) 165.托福松（Terbufos) 100.丙基喜樂松Uprobenfos) 133.益滅松（Phosmet) 166. 四氯文松 （ Tetrachlorvinphos ) 101.亞芬松（Isofenphos) 134.巴賽松（Phoxim) 167.噻^歐（Thiafenox) 102.滅必蟲（Isoprocarb) 135.比加普（Pirimicarb) 168.硫敵克（Thiodicarb) 103·加福松（Isoxathion) 136.亞特松 E (PirimiphosA) 169. 18^歐（Thiafenox) 104·依爾瑪克丁（Ivermectin) 137.亞特松 M (Pirimiphos Μ ) Π0.磷化鋅（Thionazin) 105.賽洛寧（久-Cyhalothrin) 138.普滅克（Promecarb) 171.蘇力菌素 106.祿芬隆（Lufenuron) 139·加護松（Propaphos) 172.特多寧（Tralomethrin) 107.馬拉松（Malathion) 140.安丹（propoxur) 173.三亞森（Triarathene) 1〇8·滅力口松（Mecarbam) 141.普硫松（Prothiofos) 174.三氮酸（Triazamate) 109.滅硫芬磷（Mesulfenphos ) 142.飛克松（Prothoate) 175.三落松（Triazophos) 110.聚乙酸（Metaldehyde) 143. D比氯磷（Pyrachlophos) 176.三佐隆（Triazuron) 111 ·達馬松（Methamidophos ) 144.[]比芬松（Pyradaphenthion ) 177·三氯松（Trichlorfon) 112.滅賜克（Methiocarb) 145. D比滅寧（Pyresmethrin) 178.三福隆（Triflumuron) 113.納乃得（Methomyl) 146.除蟲菊（Pyrethrum) 179.三甲克（Trimethacarb) 114.美賜平（Methoprene) 147.畢達本（Pyridaben) 180·繁米松（Vamidothion) 115.治滅 1¾ (Metolcarb) 148.畢汰芬（Pyrimidifen) 181· XMC (3,5-甲基氨基甲酸 二甲苯基酯） 116.美文松（Mevinphos) 149.百利普芬（Pyriproxyfen) 182.賽克（Xylylcarb) 117.密瑪克丁（Milbemectin) 150. RH 5992 183. YI 5301/5302 118.莫昔克丁（Moxidectin) 151.RH-2485 184·瑞賽滅寧（（-Cypermethrin) 119.乃力松（Naled) 152.殺力松（Salithion) 185.瑞塔滅寧（Zetamethrin) 120. NC 184 153.克線丹（Sebufos) 121 · NI-25 亞滅培（Acetamiprid ) 154.砂護芬（Silafluofen) 122.尼藤Dtt藍（Nitenpyram) 155.賜諾殺（Spinosad) 123.歐滅松（Omethoate) 156.治螟磷（Sulfotep) 124.歐殺滅（Oxamyl) 157.甲丙硫磷（Sulprofos) 125. (Q?〇deme(an ) 158.得芬諾（Tebufenozide) 126.歐地普（Oxydeprofos) 159.得芬胺（Tebufenpyrad) 127.巴拉松（Parathion) 160.得D比磷（Tebupirimphos) 128.甲基巴拉松 161.得福隆（Teflubenzuron) 129.百滅寧（Permethrin) 162.七氟菊酯（Tefluthrin) 130.賽達松（Phenthoate) 163.亞培松（Temephos) 131.福瑞特（Phorate) 164.特本（Terbam)34 200305556 99. Insect-active viruses 132. Phosalone 165. Terbufos 100. Uprobenfos 133. Phosmet 166. (Tetrachlorvinphos) 101. Isofenphos 134. Phoxim 167. Thiafenox 102. Isoprocarb 135. Pirimicarb 168. Thiodicarb ) 103. Isoxathion 136. Atiron E (PirimiphosA) 169. 18 ^ Europe (Thiafenox) 104. Irmamtin (Ivermectin) 137. Atrium M (Pirimiphos Μ) Π0. Zinc phosphide (Thionazin) 105. Cylonothrin (Cyhalothrin) 138. Promecarb 171. Sulicin 106. Lufenuron 139 · Propaphos 172. Tralomethrin 107. Marathion 140. Propoxur 173. Triarathene 108 · Mecarbam 141. Prothiofos 174. Triazamate 109. Methioenphos 142. Prothoate 175. Triazophos 110. Polyacetic acid (Meta ldehyde) 143. D Pyrachlophos 176. Triazuron 111 Methamidophos 144. [] Pyradaphenthion 177 Trichlorfon 112. Trichlorfon 112 Methiocarb) 145. D than Pyresmethrin 178. Triflumuron 113. Methomyl 146. Pyrethrum 179. Trimethacarb 114. Methoprene 147. Pyridaben 180 · Vamidothion 115. Metolcarb 148. Pyrimidifen 181 · XMC (3,5-methylcarbamic acid ditolyl ester) 116. Mevinphos 149. Pyriproxyfen 182. Xylylcarb 117. Milbemectin 150. RH 5992 183. YI 5301/5302 118. Moxidectin 151 RH-2485 184 · Cypermethrin (-Cypermethrin) 119. Naled 152. Salithion 185. Zetamethrin 120. NC 184 153. Sebufos) 121 · NI-25 Acetamiprid 154. Silafluofen 122. Nitenpyram 155. Spinosad 123. Omethoate 156. Sulfotep 124. Oxamyl 157. Sulprofos 125. (Q? 〇deme (an) 158. Tebufenozide 126. Oxydeprofos 159. Tebufenpyrad 127. Parathion 160. Tebupirimphos 128. Methylparazon 161. Defu Teflubenzuron 129. Permethrin 162. Tefluthrin 130. Phenthoate 163. Temephos 131. Phorate 164. Teben ( Terbam)

35 200305556 適合的驅蟲劑之非限制性實例是命名如下，其中一此 代表物除了驅蟲活性之外，還具有殺昆蟲及殺疥蟲的活性 ，以及部份已列舉如上。 (A1 ) DH;喹酮（Praziauantel) = 2-環己基羰基一4一氧 基-1，2,3,6,7，1113-六氫-411-毗嗪並[2，1-〇:]異喹咐。 (A2)氯氰碘柳胺（Closante]) = 3, 5-二碘-N-[ 5-氯 - 2-甲基-4 -（a-氰基-4-氯节基）苯基]水揚醯胺。 (A3)三氣苯嗤（Triclabendazole ) = 5-氯-6-(2,3-二氯苯氧基）-2-甲基硫基-1H-苯並咪唑。 (A4 )左旋咪唾（Levamisol ) = L-(-)-2, 3, 5, 6-四氫 -6-苯基味嗤並[2，1 b]瞳嗤。 (A5 )二苯酮咪胺酯（Mebendazole ) = (5-苯甲醯-1H-苯基味嗤-2-基）氨基甲酸曱基s旨。 (A6)腾菇素（Omphalot in)=說明於 WO 97/20857 的 真菌發光臍益（Omphalotus 〇1 earius)之巨環類發酵產物。 (A7 )阿巴汀（Abamectin )= 艾爾瑪克丁 βΐ ( Avermectin B1) 0 (A8 )依爾瑪克丁（ Ivermectin) = 22, 23-二氫艾爾 瑪克丁 B1。 (A9 )莫昔克丁（ Moxidectin ) = 5-0-脫甲基-28-脫 氧-25 -（1，3-二甲基-1 - 丁烯基）-6,28-環氧基-23-(甲氧基 亞胺基）-倍脈心B (milbemycin B)。 (A1 0 )多瑪克丁（ Doramectin ) = 25-環己基-5-0-脫 甲基-25 -脫（1-甲基丙基）-艾爾瑪克丁 Ala。 36 200305556 (All)密瑪克丁（ Mi lbemect in)=倍脈心A3及倍脈 心A4之混合物。 (A12 )倍脈心 flg ( Mi lbemvcinoxime )二倍脈心之 5- 肟。 適合的驅蟲劑及剝離劑之非限制性實例是： (R1 ) DEET: (N，N -二乙基-間-曱苯酿胺）。 (R2) KBR 3023= N-丁基-2-氧基羰基-（2_羥基）-六氫 吡啶。 (R3 )赛咪唑（Cymiazole ) = N-2, 3-二氫一3- 甲基一 1，3-噻唑-2-烷基-2, 4-二曱苯胺。 在混合物中的這些參與物，對於在此技藝中之人士是 非常熟悉的。大部分是說明在各種版本的除害劑手冊中（ 英國作物保護委員會’倫敦），以及其他是說明在各種版 本的默克索引（Merck& Co·公司，Rahway，紐澤西，美國 )或專利文獻中。因此，以下所列舉的是限於一些以實例 的方式可發現它們的出處。 (I) 2-曱基-2-（甲基硫基）丙駿一 〇-曱基氨基甲醯脂（ 得滅克）’除害劑手冊第11版（1 997 )，英國作物保護委 員會（倫敦），第26頁； (II ) S-(3, 4-二氫-4-氧苯並[d]-[i, 2, 3]—三嗪—3一基 甲基）-0,0-二曱基-偶磷二硫代酸酯（甲基谷硫磷），除害 劑手冊第11版（ 1 997 )，英國作物保護委員會（倫敦 第67頁； ^ ’ (III) N- [2, 3-二氫-2, 2 -二甲基笑甘吐 土 I本並呋喃—7-基氧基 37 200305556 羰基-（f基）胺基硫基異丙基氨基丙酸乙基酯（免 扶克），除害劑手冊第〗〗版（〗997)，英國作物保護委員 會（倫敦），第96頁； (w) (Z)-(1RS)-順式-3_(2_氯 _3, 3, 3_三氟丙 一烯 基）-2’ 2-二甲基環丙烷羧酸_2_甲基聯苯_3_基甲基酯（畢 芬寧），除害劑手冊第11版（1997)，英國作物保護委員 會（倫敦），第118頁； (V) 2-第二丁基亞胺基—3—異丙基苯基_ι，3, 5一_ 一嗪一4 —酮（布芬淨），除害劑手冊第11版（ 1 997 )，英 國作物保護委員會（倫敦），第1 5 7頁； (VI) 2, 3-二氫-2,2-二曱基苯並呋喃_7 一基甲基氨基 甲酸酯（加保扶），除害劑手冊第，英國作 物保護委員會（倫敦），第18 6頁； (VII) 2, 3-二氫-2, 2-二甲基苯並呋喃-7一基—（二丁基 胺基硫基）甲基氨基甲酸§旨（丁基加保扶），除害劑手^ 第11版（ 1997 ) ’英國作物保護委員會（儉敦），第⑽ 頁； (VIII ) S’S -(2-二甲基胺基三甲撐)_雙(硫基氨基 酸酿）（培丹）’除害劑手冊第11版（ 1 997 )，英國作物 保遵委員會（倫敦），第igg頁· (IX) 1 [3,5-—乳一 4一（3 一氣一 5 一三氟甲基一 2 一吡啶氧義 )本基]- 3 -（2，6-二氟笨甲醯、席本 T )尿素（克福隆），除害劑手冊 第11版（1 997 )，英國竹私^4 頁· 兴闼作物保護委員會（倫敦），第213 38 200305556 (X ) 0-3, 5, 6-三氣-2-Dttπ定偶構硫代酸~〇, 〇-二乙美醋 (陶斯松），除害劑手冊第11版（1 997 )，英國作物彳呆護 委員會（倫敦），第235頁； (XI) (lRS，3RS;lRS，3RS)-3-（2,2-二氯乙烯基）— 2 2-二甲基環丙烷羧酸-（RS)-α -氰基-4-氟-3-苯氧基节基醋（ 賽扶寧），除害劑手冊第11版（1997 )，英國作物保護委 員會（倫敦），第293頁； (XII) (Z)-(lR，3R)-3-(2-氯-3,3,3-三氟丙歸基）一 2, 2-二甲基環丙烷羧酸-(S)-o:-氰基-3-苯氧基节基醋以及 (2)-(11?，31〇-3-（2-氯-3,3,3-三氟^丙稀基）-2,2-二甲美環 丙烧羧酸- (R)-α -氰基-3-苯氧基节基酯之混合物（赛洛宜 )’除害劑手冊第11版（1997)，英國作物保護委員合（ 倫敦），第300頁； (XIII) 由（Ζ)-（1R，3R)-3-(2,2-二氣乙烯基）一2,2一二 甲基環丙烷羧酸-（S)- α -氰基-3-苯氧基苄基g旨以及 (1S，3S)-3-（2, 2-二氯乙烯基）-2, 2-二曱基環丙烷羧酸一 (R)- α -氰基-3-苯氧基苄基酯所組成的外消旋物（阿赛滅 寧）’除害劑手冊第11版（1997 )，英國作物保護委員會 (倫敦），第308頁； (XIV) (1RS，3RS; lRS，3RS)-3-(2,2-二氣乙烯基）一 2, 2-二甲基環丙烷羧酸—（s)_a —氰基_3 —苯氧基苄基酯的立 體異構物之混合物（瑞赛滅寧），除害劑手冊第丨丨版（ 1 997 )，英國作物保護委員會（倫敦），第314頁； (《▽)(11?，31〇-3-（2,2-二氯乙烯基）-2,2-二甲基環丙 39 200305556 烷羧酸-（S)-α -氰基-3-笨惫其眾甘此/ *丄、七 氧基下基g日（第滅争），除害劑 手冊第11版（1 997)，箪爾政仏^ 央國作物保護委員會（倫敦），第 344 頁； (XVI) (4 -氯苯基）〜3 —ο β —，# 说#、 d U，6-一贶苯甲醯）尿素（二福 隆），除害劑手冊第11版nqQ7、 U 9 9 7 )，夬國作物保護委員合 (倫敦），第395頁； '曰 (XVII) (1,4,5,6,7,7-^ s 〇 m /、乳-8, 9, 10-二原冰片—5一稀— 2’3-基二甲撲)亞硫酸鹽（安殺番），除害劑手冊第u版 U99O ’英國作物保護委員會（倫敦），第459頁； (XVIII) 曱基氨基甲酸乙基硫基_鄰_甲苯基酯（ 愛芬克）’除害劑手冊第心⑴⑺，英國作物保護委 員會（倫敦），第479頁； (XIX) 0-4-硝基-間—甲苯基_偶磷硫代酸二甲美 醋（撲滅松）’除害劑手冊第η版（則，英國作物： 護委員會（倫敦），第514頁； (XX)甲基氨基甲酸I第二丁基苯基醋（丁基滅必兹 )，除害劑手冊第11版（1997)，英國作物保護委員 倫敦），第51 6頁； (XXI) (RS)-2-(4-氣苯基）-3—甲基丁酸—（RS)1 —氮 基3苯氧基节基_ (氰戊菊_)，除害劑手冊第U版（ 1 997 ) ’英國作物保護委員會（倫敦），第539頁； (XXII) 〇,〇-二甲基—偶磷二硫代酸一3一[曱醯（甲 基:酿甲基]醋（福木松），除害劑手冊第11版（i =97) 央國作物保護委員會（倫敦），第625頁； 200305556 (XXIII) 甲基氨基甲酸+甲基硫基—3,5—二甲苯基酿 (滅賜克），除害劑手冊第11版（1997)，英國作物保護 委員會（倫敦），第8丨3頁； (XXIV) 7-虱二環[3. 2· 〇]庚—2, 6一二烯一6一 基—二甲基 磷酸酯（飛達松）’除害劑手冊第11版（ 1 997)，英國作 物保護委員會（倫敦），第670頁； (XXV) 1-(6-氣_3_卩比。定基甲基）m米唾燒_2_又 胺（益達胺），除害劑手冊第u版（1 997 )，英國作物保 遵委貝會（倫玫），第706頁； _)甲基氨基甲酸_2_異丙基苯基醋（滅必幻， 除害劑手冊第1!版（1997 )，英國作物保護委員會（ )，第729頁； (XXVII) 磷醯胺硫代酸_0,3_二曱基酯（達馬松）， 除害劑手冊第11版（1997 )，英國作物保護委員會（ )，第 808 頁； (XXVIII) N-（甲基氨基甲醯氧基）硫代乙醯亞氨酸〜 甲基酯（納乃得），除害劑手冊第丨丨版（丨997 )，英國 物保護委員會（倫敦），第815頁； 3 (XXIX) 3-(二曱氧基膦醯氧基）丁—2一烯酸曱基酯（美 文松），除害劑手冊第11版（1997 )，英國作物保護委員 會（偷放）’第844頁； (XXX) 0-4-硝基苯基-偶磷硫代酸-〇,〇〜二乙基酷（巴 拉松），除害劑手冊第11版（ 1 997 )，英國作物保護委員 會（倫敦），第926頁； 200305556 (mi) ο 4一硝基苯基—偶磷硫代酸二甲 甲基巴拉松），除宝南丨丰·笛 土-日（ 弟11版（1 997 )，英國作物保 漢委貝會（偷放），第928頁； 、 (mn) 〇,〇—一乙基—偶碟二硫代酸6—氯—2卜二 2-氧基-1，3-苯並噁唑一 3 一基甲美 ’ 一虱— 土酉曰（伏殺麟），除害劑手冊筮 版(=;英國作物保護委員會(倫敦），第咖頁； 基心-4:二甲t氨基甲酸+二甲基胺基' 6-二甲 — 土曰t加普），除害劑手冊第11版（1 997 ) ，奂國作物保護委員會（倫敦）， ⑴即^基甲酸苯基8旨（安丹） ，除害劑手冊第11版（199n M m ^ ; ,,,^ 1 1 997 )，夬國作物保護委員會（倫 放），第1036頁； (XXXV)卜（3, 5-二衰一9 /1 -- 甲m、尸本广 、，一氟苯基卜3-(2,6—二氟苯 ra 素（得福隆）’除害劑手冊第11版U 997)，英 國作物保護委員會（倫敦）.，第1158頁； (xml) 〇’〇-二甲基_偶鱗二硫代酸_s_第三丁基硫基 :基醋（托福松），除害劑手冊第11版U 997 )，英國作 物保濩委員會（倫敦），第1165頁； (mm) (3-第三丁基_卜：甲基氨基甲酿_ih 一 ，’4-三哇-5-基-硫基）醋酸乙基酯（三氮酸），除害劑手 ^第U版（1997 )，英國作物保護委員會（偷敦），第 1224 頁； + (XXXVIII)阿巴汁’除害劑手冊第u版（1997 )， 央國作物保護委員會（倫敦），第3頁； 42 200305556 (XXXIX)曱基氨基曱酸-2-第二丁基苯基酯（丁基滅 必蝨），除害劑手冊第11版（1 997 )，英國作物保護委員 會（倫敦），第516頁； (XL) N〜第三丁基-N -（4-乙基苯曱酿）一3, 5 -二曱基苯 並醯肼（得芬諾），除害劑手冊第H版（1 997 )，英國作 物保護委員會（倫敦），第114 7頁； (乂[1)(±) — 5_胺基-1-（2,6-二氯-〇：，〇；，〇：-三氟-對 -甲苯基）-4-三氟甲基-硫毗唑-3-碳腈（芬普尼），除害劑 手冊第11版（ 1997 )，英國作物保護委員會（倫敦），第 545 頁； (XLII) (1RS，3RS; 1rs，3RS)-3-(2,2—二氣乙烯基）一 2,2-二甲基環丙烷羧酸-(防）_〇;—氰基-4—氟—3-苯氧基苄基 '(貝賽扶寧），除害劑手冊第11版（ 1 997 )，英國作物 保護委員會（倫敦），第295頁； (XLIII) (4一乙氧基苯基）一[3_(4一氟-3一苯氧基苯基35 200305556 Non-limiting examples of suitable insect repellents are named as follows. One of these representatives has insecticidal and pinworm-killing activity in addition to insect-repellent activity, and some are listed above. (A1) DH; Praziauantel = 2-cyclohexylcarbonyl-4-dioxy-1,2,3,6,7,1113-hexahydro-411-pyrazino [2,1-〇:] Isoquined. (A2) Closanante) = 3, 5-diiodo-N- [5-chloro-2-methyl-4-(a-cyano-4-chlorobenzyl) phenyl] water Lianamine. (A3) Triclabendazole = 5-chloro-6- (2,3-dichlorophenoxy) -2-methylthio-1H-benzimidazole. (A4) Levamisol = L-(-)-2, 3, 5, 6-tetrahydro-6-phenyl miso and [2, 1 b] Hitomi. (A5) Mebendazole = (5-Benzamidine-1H-phenyl miso-2-yl) carbamate syl group. (A6) Omphalot in = a macrocyclic fermentation product of the fungal luminescent navel (Omphalotus 〇1 earius) described in WO 97/20857. (A7) Abamectin = Elmectin βΐ (Avermectin B1) 0 (A8) Ivermectin = 22, 23-Dihydro Elmectin B1. (A9) Moxidectin = 5-0-demethyl-28-deoxy-25-(1,3-dimethyl-1 -butenyl) -6,28-epoxy-23 -(Methoxyimino)-milbemycin B. (A1 0) Doramectin = 25-cyclohexyl-5-0-demethyl-25-de (1-methylpropyl) -elmaktin Ala. 36 200305556 (All) Mi lbemect in = Blend of heart A3 and A4 of heart. (A12) Double oxime flg (Mi lbemvcinoxime). Non-limiting examples of suitable insect repellents and strippers are: (R1) DEET: (N, N-diethyl-m-xanthenamine). (R2) KBR 3023 = N-butyl-2-oxycarbonyl- (2-hydroxy) -hexahydropyridine. (R3) Cymiazole = N-2,3-dihydro-3-methyl-1,3-thiazole-2-alkyl-2,4-dihydrazidine. These participants in the mixture are very familiar to those skilled in the art. Most are described in various versions of the Pesticides Handbook (British Crop Protection Commission's London), and others are listed in various versions of the Merck Index (Merck & Co., Rahway, New Jersey, United States) or patents In the literature. Therefore, the following list is limited to some examples where they can be found. (I) 2-fluorenyl-2- (methylthio) propanyl 10-fluorenylcarbamate (Temex) 'Pesticides Handbook 11th Edition (1 997), UK Crop Protection Commission ( London), p. 26; (II) S- (3, 4-dihydro-4-oxobenzo [d]-[i, 2, 3] -triazine-3-ylmethyl) -0,0 -Difluorenyl-phosphonodithioate (methyl azinphos-methyl), Pesticides Handbook 11th Edition (1 997), British Crop Protection Council (London, p. 67; ^ '(III) N- [ 2,3-dihydro-2,2-dimethylxanthanitone I Benzofuran-7-yloxy 37 200305556 carbonyl- (f-) aminothioisopropylaminopropionic acid ethyl ester ( Exemption), Pesticides Handbook, Edition 〖〗 (997), British Crop Protection Commission (London), p. 96; (w) (Z)-(1RS) -cis-3_ (2_chlorine_ 3, 3, 3_trifluoropropenyl) -2 '2-dimethylcyclopropanecarboxylic acid_2_methylbiphenyl_3_ylmethyl ester (Bifennin), Pesticide Handbook, 11th edition (1997), British Crop Protection Commission (London), p. 118; (V) 2-Secondylbutylimino-3-isopropylphenyl_, 3, 5-mono_monoazine-4-one (Bufennet) Pesticides Handbook, 11th edition (1 997), British Crop Protection Commission (London), p. 157; (VI) 2, 3-dihydro-2,2-difluorenylbenzofuran_7-based Methyl Carbamate (Carbofuran), Pesticides Handbook, British Crop Protection Commission (London), p. 18 6; (VII) 2, 3-Dihydro-2, 2-dimethylbenzo Furan-7-yl- (dibutylaminothio) methylcarbamic acid § intent (Butyl plus protection), Pesticides Hand ^ 11th edition (1997) 'British Crop Protection Commission (Junetown), Page ；; (VIII) S'S-(2-dimethylaminotrimethylene) _bis (thioamino acid) (Pedan) 'Pesticides Handbook 11th Edition (1 997), UK Crop Compliance Committee (London), p.igg · (IX) 1 [3,5-—milk 4— (3 gas—5—trifluoromethyl—2—pyridinyloxy) benzyl]-3-(2,6- Difluorobenzidine, Xiben T) Urea (Keflon), Pesticides Handbook 11th Edition (1 997), British Bamboo Private ^ 4 · Hing ’s Crop Protection Committee (London), 213 38 200305556 ( X) 0-3, 5, 6-trigas-2-Dttπ destabilized thio acid ~ 〇, 〇- 二American Vinegar (Tausson), Pesticides Handbook, 11th Edition (1 997), British Crop Steal Care (London), p. 235; (XI) (lRS, 3RS; lRS, 3RS) -3- (2, 2-Dichlorovinyl) — 2 2-dimethylcyclopropanecarboxylic acid- (RS) -α-cyano-4-fluoro-3-phenoxybenzyl vinegar (Sefonin), Pesticide Handbook 11th edition (1997), British Crop Protection Commission (London), p. 293; (XII) (Z)-(lR, 3R) -3- (2-chloro-3,3,3-trifluoropropionate ) 2,2-dimethylcyclopropanecarboxylic acid- (S) -o: -cyano-3-phenoxybenzyl vinegar and (2)-(11?, 31〇-3- (2-chloro -3,3,3-trifluoro ^ propenyl) -2,2-dimethylmetapropanecarboxylic acid-(R) -α-cyano-3-phenoxybenzyl ester mixture (Xylo Should) 'Pesticide Handbook, 11th edition (1997), UK Crop Protection Commission (London), p. 300; (XIII) by (Z)-(1R, 3R) -3- (2,2-Digas Vinyl) -2,2-dimethylcyclopropanecarboxylic acid- (S) -α-cyano-3-phenoxybenzyl g and (1S, 3S) -3- (2, 2-dichloro Vinyl) -2,2-Difluorenylcyclopropanecarboxylic acid mono (R) -α-cyano-3-phenoxybenzyl ester Siemenin) 'Pesticides Handbook, 11th edition (1997), British Crop Protection Commission (London), p. 308; (XIV) (1RS, 3RS; lRS, 3RS) -3- (2,2-Digas Vinyl) 2,2-dimethylcyclopropanecarboxylic acid— (s) _a —Cyano_3 — Stereoisomeric mixture of phenoxybenzyl esters (Rexamin), Pesticide Handbook Edition 丨 丨 (1 997), British Crop Protection Commission (London), p. 314; ("▽) (11 ?, 31〇-3- (2,2-dichlorovinyl) -2,2-di Methylcyclopropane 39 200305556 Alkane carboxylic acid- (S) -α-cyano-3-benzyl, which is the most popular / * 丄, hepyloxy group (day), Pesticide Handbook No. 11 Edition (1 997), Government Policy ^ Central State Crop Protection Commission (London), p. 344; (XVI) (4-chlorophenyl) ~ 3 —ο β —, # 说 #, d U, 6- One benzamidine) urea (difuron), Pesticides Handbook 11th Edition nqQ7, U 9 9 7), Lao Crop Protection Commission (London), p. 395; 'Yue (XVII) (1, 4,5,6,7,7- ^ s 0m /, milk-8, 9, 10- two original borneol — 5 dilute — 2'3-yl dimethyl sulfite) (sulfuric acid), except Pesticide Handbook U99O 'British Crop Protection Commission (London), p. 459; (XVIII) Ethylthiocarbamate-o-tolyl ester (Efenk)' Pesticide Handbook, Crop Protection Council of the United Kingdom (London), p. 479; (XIX) 0-4-Nitro-m-tolyl_azophosphothiothioic acid dimethyl vinegar (fenoxon) 'Pesticide Handbook, n version , British Crops: Conservation Commission (London), p. 514; (XX) Methyl Carbamate I Second Butyl Phenyl Acetate (Butyl Metiz), Pesticides Handbook 11th Edition (1997), British Crops Protection Committee, London), p. 51.6; (XXI) (RS) -2- (4-Gaphenyl) -3-methylbutanoic acid— (RS) 1-nitro-3phenoxybenzyl group— (cyano Fenju_), Pesticides Handbook, U Edition (1 997) 'British Crop Protection Commission (London), p. 539; (XXII) 〇, 〇-dimethyl-phosphadithioic acid 1-3 [曱 醯 (Methyl: Brewed Methyl) Vinegar (Fukumatsu), Pesticides Handbook 11th Edition (i = 97) Central State Crop Protection Commission (London), p. 625; 200305556 (XXIII) Methyl Carbamate + Methylsulfanyl—3,5— Tolyl-based brewing (Mechoke), Pesticides Handbook, 11th edition (1997), British Crop Protection Commission (London), pages 8 丨 3; (XXIV) 7-lice second ring [3. 2 · 〇] —2, 6-Diene-6-yl-Dimethyl Phosphate (Fedarson) 'Pesticides Handbook 11th Edition (1 997), British Crop Protection Commission (London), p. 670; (XXV) 1- (6-qi_3_ 卩 ratio. (Aminomethyl) m-salamine _2_yamine (Yidamin), Pesticides Handbook U Edition (1 997), UK Crop Protection and Regulatory Commission (Ryme), page 706; _) A Carbamic acid _2_isopropylphenyl vinegar (mebiquan, Pesticide Handbook 1st Edition (1997), British Crop Protection Council (), p. 729; (XXVII) Phosphatamine Thioacid_ 0,3_Dimethanyl ester (Damasson), Pesticides Handbook, 11th edition (1997), British Crop Protection Council (), p. 808; (XXVIII) N- (methylcarbamyloxy) Thioacetamidine ~ Methyl Ester (Nanaide), Pesticides Handbook 丨 丨 Edition (丨 997), British Council for Physical Protection (London), p. 815; 3 (XXIX) 3- (2 (Methoxyphosphine, ethoxy) butan-2-enoate (Mexonson), Pesticides Handbook, 11th edition (1997), British Crop Protection Commission (Sneak), p. 844; (XXX) 0 -4-Nitrophenyl-phosphonothiothioate-〇, 〇 ~ Diethyl Cool (Balason), Pesticides Handbook 11th Edition (1 997), British Crop Protection Council (London), 926 Page; 200305556 (mi) ο 4-mononitrophenyl Dimethyl parathionyl phosphorothioate), except Baonan 丨 Feng Ditu-ri (11th edition (1 997), British Crop Protection Committee (Sneak)), p. 928; (mn) 〇, 〇-ethyl-diacetate dithio acid 6-chloro-2 bu dioxo-2, oxy-2, 3-benzoxazole- 3 monomethylmethanyl ' (Foxarin), Pesticides Handbook 筮 Edition (=; British Crop Protection Commission (London), p. C .; Core-4: dimethyl t-carbamic acid + dimethylamino '6-dimethyl — soil T Gap), Pesticides Handbook, 11th Edition (1 997), Lao National Crop Protection Commission (London), Phenyl Phenyl Carboxylate 8 (Andane), Pesticides Handbook, 11th Edition (199n) M m ^; ,,, ^ 1 1 997), Lao National Crop Protection Commission (Lun Fang), p. 1036; (XXXV) Bu (3, 5-Second Decay One 9/1-Jiam, Shibenguang ,, Monofluorophenyl 3- (2,6-difluorobenzene raline (Teflon) 'Pesticides Handbook 11th Edition U 997), British Crop Protection Commission (London)., P. 1158; ( xml) 〇′〇-dimethyl_dichlorodithioic acid_s_ tertiary butylthio: yl acetic acid (tofosone), except Agent Handbook 11th Edition U 997), British Crop Protection Board (London), p. 1165; (mm) (3-Third-Butyl_Bu: Methyl Carbamate_ih One, '4-Tri-Wa- 5-yl-thio) ethyl acetate (triazic acid), Pesticides Handbook U Edition (1997), British Crop Protection Council (St. John), page 1224; + (XXXVIII) Abba Juice ' Pesticides Handbook, U Edition (1997), Central State Crop Protection Commission (London), p. 3; 20032003556 (XXXIX) 2-Aminoaminophosphonic acid-2-second butylphenyl ester ), Pesticides Handbook, 11th Edition (1 997), British Crop Protection Council (London), p. 516; (XL) N ~ Third-butyl-N- (4-ethylbenzene), 3, 5-Difluorenylbenzopyrazine (Defeno), Pesticides Handbook H Edition (1 997), British Crop Protection Commission (London), p. 114 7; (乂 [1) (±) — 5 _Amino-1- (2,6-dichloro-〇:, 〇;, 〇: -trifluoro-p-tolyl) -4-trifluoromethyl-thiopyrazole-3-carbonitrile (Fenpu Nigeria), Pesticides Handbook, 11th edition (1997), British Crop Protection Commission (London), 545 Page; (XLII) (1RS, 3RS; 1rs, 3RS) -3- (2,2-digasvinyl) -2,2-dimethylcyclopropanecarboxylic acid- (anti) _〇; -cyano- 4-Fluoro-3-phenoxybenzyl '(Becetinine), Pesticides Handbook, 11th Edition (1 997), British Crop Protection Council (London), p. 295; (XLIII) (4-B Oxyphenyl)-[3_ (4-fluoro-3-phenoxyphenyl

丙基](一 T基)矽烷（矽護芬），除害劑手冊第U版 1 997)，英國作物保護委員會（倫敦），第1105頁； (XLIV) (E)一 α 一〇 q — 撑胺基-氧甲基.苯氧基心4—基1 手冊第u版心:第三丁基醋（芬普璃），除害齊 53〇頁； 央國作物保護委員會（倫敦），第 以LV) 2-第三丁基〜5 -3(2H)-酮（畢達本）a第二丁基卞基硫基)_4'氯噠 ^ 達本），除害劑手冊第11版（ 1 997)，英 國作物保護委員會彳| 、 、偏放），第1161頁； 43 200305556 (XLVI ) 4 - [[4-（1，1-二曱基苯基）苯基]乙氧基]-嗟嗤 咐（芬殺），除害劑手冊第11版（1997 )，英國作物保護 委員會（倫敦），第507頁； (XLVII) 4-苯氧基苯基-（RS)-2-(吡啶基氧基）丙基-鱗（百利普芬），除害劑手冊第11版（1 997 )，英國作物 保護委員會（倫敦），第1073頁；(Propyl) (-T-based) silane (siloxan), Pesticides Handbook U Edition 1 997), British Crop Protection Commission (London), p. 1105; (XLIV) (E) -α-10 Amino-Oxymethyl. Phenoxy 4- 4-yl 1 Manual, Version u: Third Butyl Vinegar (Fenpri), Pest Removal pp. 53; Central State Crop Protection Commission (London), p. LV) 2-third butyl ~ 5 -3 (2H) -one (Pidaben) a second butyl fluorenylthio) _4 'chloro ^ ^ daben), Pesticides Handbook 11th Edition ( 1 997), British Crop Protection Commission 彳 |, 偏, bias), p. 1161; 43 200305556 (XLVI) 4-[[4- (1,1-Difluorenylphenyl) phenyl] ethoxy]- Commanded (Fencidium), Pesticides Handbook, 11th edition (1997), British Crop Protection Commission (London), p. 507; (XLVII) 4-phenoxyphenyl- (RS) -2- (pyridine) Oxy) propyl-scale (Balipufen), Pesticides Handbook 11th Edition (1 997), British Crop Protection Council (London), p. 1073;

(乂1^111)5-氯-1^-{2-[4-（2-乙氧基乙基）-2,3-二甲 基苯氧基]乙基卜6-乙基嘧啶-4-胺（畢汰芬），除害劑手 冊第11版（1997)，英國作物保護委員會（倫敦），第 1 070 頁； (XLIX) (E)-N-(6-氣-3-吡啶基甲基）一n-乙基一n—甲基· 2石肖基乙烯叉二胺（尼藤卩比藍），除害劑手冊第11版（ 1997 )，英國作物保護委員會（倫敦），第88〇頁； (L) (E)-N1 -[(6-氣-3-吡啶基）曱基]—N2一氰基—N1 一甲 基乙胖（NI-25亞滅培），除害劑手冊第u版（1997)， 英國作物保護委員會（倫敦），第9頁；(乂 1 ^ 111) 5-chloro-1 ^-{2- [4- (2-ethoxyethyl) -2,3-dimethylphenoxy] ethylbenzene 6-ethylpyrimidine-4 -Amine (Pyridine), Pesticides Handbook 11th Edition (1997), British Crop Protection Commission (London), p. 1 070; (XLIX) (E) -N- (6-Ga-3-pyridyl) (Methyl) -n-ethyl-n-methyl · 2 schottyl vinylidene diamine (Nittenox blue), Pesticides Handbook 11th Edition (1997), British Crop Protection Council (London), 88. Pages; (L) (E) -N1-[(6-Gas-3-pyridyl) fluorenyl] —N2—cyano—N1—methylethenyl (NI-25 acetamidol), Pesticides Handbook Edition u (1997), British Crop Protection Commission (London), p. 9;

(LI )艾爾瑪克丁 B1，除害劑手冊第^版（MW) ’英國作物保護委員會（倫敦），第3頁； (LII )來自植物之昆蟲活性萃取物，特別巧 (2R’ 6aS，12aS)-1，2, 6, 6a，12, 12a-六氫-2-異丙烯—8 9一一 氧基-色烯並[3, 4-b]糠[2, 3-h]色烯-6一酉同（备’二^ R〇t_e) ’除害劑手冊第u版（1997 )，英國作物 委貝會（倫敦），第1097頁；以及來自印度苦棟 之萃取物，特別 二 1及古楝素，時 44 200305556 害劑手冊第11版（1997 )，英國作物保護委員會（倫敦） ，第59頁； (L111 )包含昆蟲活性線蟲，較佳是異小桿線蟲(LI) Elmaktin B1, Pesticides Handbook ^ Edition (MW) 'Crop Protection Commission (London), p. 3; (LII) Insect-active extracts from plants, particularly ingenious (2R' 6aS , 12aS) -1,2,6,6a, 12,12a-hexahydro-2-isopropene-8 9-monooxy-chromene [3, 4-b] furan [2, 3-h] color Ene-6 is identical (prepare 'Ro ^ _e)' Pesticide Handbook, U Edition (1997), British Crop Commission (London), p. 1097; and extracts from Kudong, India, particularly 22 and Gulin, Hours 2003200305556 Pesticide Handbook 11th Edition (1997), British Crop Protection Commission (London), p. 59; (L111) Contains insect-active nematodes, preferably Heterorhabditis elegans

Heterorhabditis bacteriophora 反 H. megidis 之 I 儀物 ’除害劑手冊第11版（1997)，英國作物保護委員會（倫 敦）’弟671頁，包含蟲生線蟲（5^己//7(?/77己則/Wi/ae) 之製備物，除害劑手冊第11版（1 997 )，英國作物保護委 員會（倫敦）’第1Π5頁；以及包含蟲生線蟲（乂 scapier/sc/)之製備物，除害劑手冊第u版（1 997)， 英國作物保護委員會（倫敦），第1丨丨6頁； (LIV)得自枯草桿菌（万ac/7/似之製傷 物’除害劑手冊第11版（ 1 997 )，英國作物保護委員會（ 倫敦），第72頁；或得自蘇力菌（及之 製備物’但除了分離自GC91或NCTC11821的化合物之外， 除害劑手冊第11版（ 1997 )，英國作物保護委員會（倫敦 )，第73頁； (LV )包含昆蟲活性真菌，較佳是蠟蚧幹枝孢菌（ /eca;?//)之製備物，除害劑手冊第u版（ 1 997 )，英國作物保護委員會（倫敦），第1266頁；包含 白僵菌（肋仙之製備物，除害劑手冊 第11版（1997 )，英國作物保護委員會（倫敦），第郎 頁；以及包含球孢白僵菌（及如仙）之製備物，除害 劑手冊第11版（1997 )，英國作物保護委員會（倫敦）， 第83頁； 45 200305556 (LVI )包含昆蟲活性病毒，較佳是核多角體病毒（ Neodipridon Sertifer NPV)之製備物，除害劑手冊第u 版（ 1 997 )，英國作物保護委員會（倫敦），第^“頁； 包含甘蘭夜蛾（’ayz/esira Araw/cae)核多角體病毒之製 備物’除害劑手冊第11版（1997 )，英國作物保護委員會 (倫敦），第759頁；以及包含蘋果蠹蛾（q心·习 病毒之製備物，除害劑手冊第η 版（ 1 997 )，英國作物保護委員會（倫敦），第291頁； ((：1^乂乂1)7-氣-2,3,4&，5-四氫-2-[甲氧基羰基（4一三 氟曱乳基本基）氣基甲酿]口引U朵[1，2 e ] °惡σ坐咐一 4 a-魏酸@旨（ DPX-MP062，郎蟲威（ind〇xyCarb ))，除害劑手冊第11 版（ 1997 )，英國作物保護委員會（倫敦），第453頁； (CLXXXII) N，-第三丁基-N，-(3,5一二曱基苯曱醯）〜3一 甲氧基-2-曱基苯並醯肼（rH一2485，甲氧芬胁（ Methoxyfenozide))除害劑手冊第u版（1 997 )，英國 作物保護委員會（倫敦），第1 〇94頁；以及 (CLXXXIII ) N’-[4-曱氧基-聯苯-3-基]-肼羧酸異丙基 醋（D 2341 )，布萊頓作物保護委員會（1 996 )，第487〜 493 頁； (R2)摘要冊，第212屆ACS國際會議，奥蘭多，佛 羅里達，8月25-29日（1996 ) ，AGR0-020。發行者：美國 化學協會，華盛頓，C0NEN : 63BFAF。 根據以上成明的結果’本發明進一步的基本形態是有 關於控制溫血動物上的害蟲之組合製備物，除了式I化合 46 200305556 物之外，甘、如 、遇包括至少一種具有相同或不同作用方向的兑 他活性成份， 八 Μ及至少一種生理上可接受的載體。本發明 並不限於兩種的組合物。 ^本I明之驅蟲組合物通常包括0· 1至99重量％，特別 是〇·1至+、 重1%之式I的活性成份或其混合物；以及 99.9至1重量％ ’特別是99·8 i 5重量％之固體或液體 添加物’其包括0至25重量％，特別是0.1至25重量％ 之界面活性劑。Heterorhabditis bacteriophora Anti-H. Megidis I Pesticides 'Pesticides Handbook 11th Edition (1997), British Crop Protection Commission (London)' p. 671, contains entomogenous nematodes (5 ^^ // 7 (? / 7777) / Wi / ae) preparations, Pesticides Handbook 11th Edition (1 997), British Crop Protection Commission (London) 'p. 1Π5; and preparations containing entomogenous nematodes (乂 scapier / sc /), Pesticide Handbook, U Edition (1 997), British Crop Protection Commission (London), pages 1 丨 6; (LIV) from Bacillus subtilis (10,000 ac / 7 / Similar Injury Preparation 'Pesticide Handbook 11th Edition (1 997), British Crop Protection Commission (London), p. 72; or from Sulfur (and preparations thereof) but except for compounds isolated from GC91 or NCTC11821, Pesticides Handbook 11th Edition (1997), British Crop Protection Commission (London), p. 73; (LV) Preparations containing insect-active fungi, preferably Cladosporium cereus (/ eca;? //), Pesticide Handbook p. U Edition (1 997), British Crop Protection Commission (London), p. 1266; contains Beauveria bassiana , Pesticides Handbook 11th Edition (1997), British Crop Protection Commission (London), p. Lange; and preparations containing Beauveria bassiana (and Ruxian), Pesticides Handbook 11th Edition (1997) , British Crop Protection Council (London), p. 83; 45 200305556 (LVI) contains preparations of insect-active viruses, preferably nuclear polyhedrosis virus (Neodipridon Sertifer NPV), Pesticides Handbook, U Edition (1 997) , British Crop Protection Commission (London), p. ^ "; Preparations containing 'ayz / esira Araw / cae' nuclear polyhedrosis virus", Pesticides Handbook, 11th edition (1997), British Crop Protection Commission (London), p. 759; and preparations containing codling moth (preparation of q-heart virus, Pesticides Handbook, n version (1 997), British Crop Protection Commission (London), p. 291; (( : 1 ^ 乂 乂 1) 7- 气 -2,3,4 &, 5-tetrahydro-2- [methoxycarbonyl (4-trifluorofluorene milk base) gas-based methyl alcohol] Introduced U flower [ 1, 2 e] ° Evil σ sat on a 4 a-wei acid @purpose (DPX-MP062, indoxy carb), Pesticides Handbook 11th Edition 1997), British Crop Protection Commission (London), p. 453; (CLXXXII) N, -Third-butyl-N,-(3,5-Difluorenylphenylhydrazone) ~ 3-methoxy-2- Pyridylbenzopyrazine (rH-2485, Methoxyfenozide) Pesticides Handbook U Edition (1 997), UK Crop Protection Council (London), p. 1094; and (CLXXXIII) N '-[4-Methoxy-biphenyl-3-yl] -hydrazinecarboxylic acid isopropyl acetate (D 2341), Brighton Crop Protection Commission (1 996), pp. 487 ~ 493; (R2) Abstract Booklet, 212th ACS International Conference, Orlando, Florida, August 25-29 (1996), AGR0-020. Issued by: American Chemical Society, Washington, CONEN: 63BFAF. According to the results of the above, 'A further basic form of the present invention is a combined preparation for controlling pests on warm-blooded animals. In addition to the compound of Formula I, 2003 200305556, Gan, Ru, and Yu include at least one of the same or different Direction of action: Dalta active ingredient, BaM and at least one physiologically acceptable carrier. The invention is not limited to a combination of two. ^ The insect repellent composition of the present invention generally comprises from 0.1 to 99% by weight, in particular from 0.1 to +, 1% by weight of the active ingredient of the formula I or a mixture thereof; and from 99.9 to 1% by weight 'in particular 99 · 8 i 5% by weight of solid or liquid additives, which include 0 to 25% by weight, especially 0.1 to 25% by weight of a surfactant.

本發明的組合物可局部、經口、非腸胃道或皮下地施 用到要治療的動物上，組合物是以溶液、乳液、懸浮液（ 反液）、粉末、錠劑、丸塊、膠囊或潑灑劑調配物的形式 而存在。The composition of the present invention can be applied topically, orally, parenterally or subcutaneously to the animal to be treated. The composition is a solution, emulsion, suspension (reflux), powder, lozenge, pellet, capsule or Existing as a spray formulation.

潑灑或滴藥的方法包含將式丨化合物施用到皮膚或皮 毛的局部限定部位，有利地是施用到動物的頸部或脊骨。 k可藉由將潑灑劑或滴劑調配物的海綿或喷液，施用到毛 皮上相當小的區域而進行，在該處，活性物質幾乎自動地 散佈於毛皮的廣泛區域上，這是因為在調配物中的成份之 分散特性以及動物運動的協助所致。 潑灑劑或滴劑的調配物可有利地包括載體，其可促進 在動物宿主的皮膚表面上或毛皮中之快速的散佈，並且載 體通常被視為是散佈油脂。適合的載體是例如，油質溶液 ，乙醇及異丙醇溶液’例如，2-辛基十二烷醇或油醇的溶 液，單魏酸酯之;谷液，例如，肉豆蔻酸異丙基酯、棕櫚酸 異丙基酉曰、卓酉文月桂基S旨、油酸油基g旨、油酸癸基g旨、月 47 200305556 桂酸己基酯、油酸油基酯、鏈長度Ci2-Ci8的飽和脂肪醇之 癸酸二羧酸酯之溶液，例如，酞酸二丁基酯、異肽酸 二異丙基酯、己二酸二異丙基酯、己二酸二（正丁基）酯； 或脂肪酸酯之溶液，例如，甘醇。可有利的是額外地存在 分散劑’例如，製藥業或化妝品業所熟知的分散劑。實例 是2-卩比略烧酮、2-(N-烷基）毗咯烷酮、丙酮、聚乙二醇及 其鱗類及醋類、聚丙二醇或合成的三酸甘油酯。The method of spraying or dripping comprises applying a compound of formula 丨 to a locally defined part of the skin or fur, advantageously to the neck or spine of an animal. k can be performed by applying a sponge or spray of a spray or drop formulation to a relatively small area on the fur, where the active substance is spread almost automatically over a wide area of the fur, because The dispersion characteristics of the ingredients in the formulation and the assistance of animal movement. Formulations of sprays or drops may advantageously include a carrier that facilitates rapid spread on the skin surface of the animal host or in the fur, and the carrier is generally considered to be a spread of grease. Suitable carriers are, for example, oily solutions, ethanol and isopropanol solutions, such as a solution of 2-octyldodecanol or oleyl alcohol, of a monoweilate; a cereal fluid, for example, isopropyl myristate Ester, Isopropyl palmitate, Lauryl succinate, oleyl g oleate, decyl g oleate, July 47 200305556 hexyl laurate, oleyl oleate, chain length Ci8 saturated fatty alcohol decanoate dicarboxylate solution, for example, dibutyl phthalate, diisopropyl isopeptide, diisopropyl adipate, di (n-butyl adipate) ) Esters; or solutions of fatty acid esters, for example, glycols. It may be advantageous to additionally have a dispersant ', e.g., a dispersant well known in the pharmaceutical or cosmetic industry. Examples are 2-pyrrolidone, 2- (N-alkyl) pyrrolidone, acetone, polyethylene glycol and its scales and vinegars, polypropylene glycol or synthetic triglycerides.

油毖溶液包括，例如，植物油，例如，橄欖油、落花 生油、芝麻油、松油、亞麻子油或蓖麻油。植物油也可以 環氧化的形式而存在。也可使用石蠟以及矽酮油。 般而δ ’潑灑劑或滴劑的調配物包括1至2 〇重量％ 之式I化合物、〇· 1至50重量％之分散劑以及45至98· 9 重量％之溶劑。Oil tincture solutions include, for example, vegetable oils, such as olive oil, virgin oil, sesame oil, pine oil, linseed oil, or castor oil. Vegetable oils can also exist in epoxidized form. Paraffin and silicone oils can also be used. In general, the formulation of a δ ' spray or drop includes 1 to 20% by weight of a compound of formula I, 0.1 to 50% by weight dispersant, and 45 to 98.9% by weight of a solvent.

潑灑或滴藥的方法可特別有利地使用在畜群動物上， 例如，牛、馬、綿羊或豬’纟中要藉由口服或注射而治療 所有的動物是困難或費時的。由於其簡便性，目此，這個 方法當然也可用於所有的其他動物，包括個別㈣養動物 或寵物，並且非常受到動物飼養者的喜愛，因為它可經常 的進行而無須獸醫專家的存在。 雖然濃縮的組合物是更佳適合作為商用產品，但最後 的使用者通常將使用稀釋的組合物。 這樣的組合物也可包括其他添加物，例如，穩定劑、 消泡劑、黏度調控劑、黏結劑、增稍劑以及其㈣活性成 份，以達到特殊的效果。 48 200305556 最後的使用者所使用的這種驅蟲組合物，同樣也形成 本發明之部份。 在本發明用於害蟲控制的各種方法中，或在本發明的 各種害蟲控制組合物中，式I之活性成份可以其全部的立 體構形或其混合物的形式而使用。 本表月也包括一種預防性保護溫血動物（特別是生產 性家畜、馴養動物以及寵物）避免寄生蠕蟲之方法，其包Sprinkling or dripping methods can be used particularly advantageously on herd animals, e.g. cattle, horses, sheep or pigs' boils. It is difficult or time consuming to treat all animals by oral or injection. Due to its simplicity, of course, this method can also be used for all other animals, including individual domestic animals or pets, and is very popular with animal breeders because it can be performed often without the need for a veterinary expert. Although concentrated compositions are more suitable as commercial products, end users will typically use dilute compositions. Such a composition may also include other additives such as stabilizers, defoamers, viscosity modifiers, binders, thinners, and its active ingredients to achieve special effects. 48 200305556 This insect repellent composition used by the last user also forms part of the present invention. In the various methods for pest control of the present invention, or in the various pest control compositions of the present invention, the active ingredient of the formula I may be used in its entire stereo configuration or as a mixture thereof. This month also includes a preventive method to protect warm-blooded animals (especially productive domestic animals, domestic animals, and pets) from parasitic worms.

㈣式I之活性成份或從其中製備的活性成份調配物= 樂至動物作為飼料或飲水的添加物，或以固體或液體的妒 式’口服或注射或非腸胃道地投藥。本發明也包括將本發 明之式I化合物用於上述方法之一。 實施方式 以下的實施例僅作為舉例說明本發明，而非限制之 ，名詞“活性成份，，表示列舉在表1中的物質。 百分::佳的調配物特別是以下述方式而組成：（％=重 調配物實施你I 顆验物： 活性成份 高嶺土 高度分散的二氧化石夕 水合矽酸鋁鎂 將活性成份溶解於二氣甲浐 =容劑在減壓環境下藉由“= 可與動物飼料混合。 < wThe active ingredient of formula I or an active ingredient formulation prepared therefrom = Leto animals as an additive to feed or drinking water, or in solid or liquid form, orally or by injection or parenterally. The invention also includes the use of a compound of formula I of the invention in one of the methods described above. Embodiments The following examples are merely for the purpose of illustrating the present invention and are not limiting. The term "active ingredient" refers to the substances listed in Table 1. Percentage :: The best formulation is composed in the following way: ( % = Re-formulation to implement your I test: The active ingredient kaolin is highly dispersed. The active ingredient is dissolved in digas formamidine. The solvent is in a reduced pressure environment. Animal feed mix. ≪ w

(a) 5% 94% 1% (b) 10% 90% 噴塗在載 體 類 上’之後 型的顆粒 49 200305556 2·顆粒物： 活性成份 3% 聚乙二醇（MW 200) 3% 高嶺土 (MW=分子量） 94% 在混合器中， 將細微研磨的活性成份均勻地塗到已經 以聚乙二酵濕潤的高嶺土。以此方式’可得到無灰塵的顆 粒物。 t錠劑或丸塊： I 活性成份 33. 00% 甲基纖維素 0.80% 高度分散的二氧化矽 0. 80% 玉米澱粉 8.40% II乳糖晶體 22. 50% 玉米澱粉 17. 00% 微晶體纖維素 16. 5% 硬脂酸鎂 1.00% (Ϊ )將甲基纖維素在水中授拌 在材料膨脹之後，將 二氧化石夕於其中授拌，並將混合物均質地懸浮。將活性成 份以及玉米澱粉混合。將水溶性料液併人到這個混合物 中，並將其揉成團狀。將所得的物f經由12 M的篩網而粒 化，並且乾燥。 (II)將所有的4個賦形劑充分混合。 、（111 )冑（I )及（II)所得到的前混合物加以混合 ’並且壓成錠劑或丸塊。 50 200305556 i.注射劑= Α·油皙載體（緩釋）： 〇.1-1.〇克 加到100亳升 〇· 1-1.0 克 加到100亳升 1. 活性成份 落花生油 2. 活性成份 芝麻油 製備：將活性成份溶解在部份的油脂中同時攪拌，如 果需要的話，可溫和地加熱，接著在冷卻之後，補足到所 要的體積，並且經由具有〇· 221孔徑的適合膜濾紙而無菌 過渡。 Β.可輿水相溶的溶劑（平均的釋放速率）： 1·活性成份 0.Μ.0克 4-羥基曱基-1，3-二噁茂烷（甘油縮甲醛）4〇克 1，2-丙二醇 加到100毫升 2·活性成份 〇卜1〇克 甘油二甲基縮酮 4〇克 加到1G0毫升 製備：將活性成份溶解在部份的溶劑中同時攪拌，補 足到所要的體積’並且經由具有0 22μπι孔徑的適合膜滤紙 而無菌過濾。 C·丞溶性溶質物（快速釋放） 0· 1 -1· 0 克 10克 20克 1克 加到100毫升 1·活性成份 5^乙氧基化的葱麻油（40環氧乙燒單位） 1，2-丙二醇 卞基醇 注射用水 51 200305556 2.活性成份 0.1-1.0克 聚乙氧基化的山梨聚糖單油基酯（20環氧乙烷單位）8克 4-羥基甲基-1，3-二噁茂烷（甘油縮曱醛） 20克 苄基醇 1克 注射用水 加到100毫升 製備：將活性成份溶解於溶劑及界面活性劑中，並以 水補足到所要的體積。經由0. 22μιη孔徑的適合膜濾紙進行 無菌過濾。 5.潑灑劑： Α. 活性成份 5克 肉豆蔻酸異丙基酯 10克 異丙醇 加到100毫升 Β. 活性成份 2克 月桂酸己基酯 5克 中等鏈之三酸甘油酉旨 15克 乙醇 加到100毫升 C. 活性成份 2克 油酸油基酯 5克 Ν-甲基-毗咯烷酮 40克 異丙醇 加到100毫升(a) 5% 94% 1% (b) 10% 90% after spraying on the carrier's particles 49 200305556 2 · particulate matter: active ingredient 3% polyethylene glycol (MW 200) 3% kaolin (MW = Molecular weight) 94% In a mixer, apply the finely ground active ingredient evenly to kaolin that has been moistened with polyethylene glycol. In this way ', dust-free particles can be obtained. Lozenges or pills: I Active ingredient 33.0% Methylcellulose 0.80% Highly dispersed silicon dioxide 0.80% Corn starch 8.40% II Lactose crystals 22. 50% Corn starch 17. 00% Microcrystals Cellulose 16.5% magnesium stearate 1.00% (Ϊ) Methylcellulose is mixed in water. After the material swells, stone dioxide is mixed therein, and the mixture is suspended homogeneously. Mix active ingredients with corn starch. Combine the water-soluble feed solution into this mixture and knead it into a dough. The obtained product f was granulated through a 12 M screen and dried. (II) Mix all 4 excipients thoroughly. , (111), (I) and (II), the pre-mixtures obtained are mixed 'and compressed into tablets or pellets. 50 200305556 i. Injection = Α · oily carrier (sustained release): 〇.1-1.10 grams to 100 liters 〇. 1-1.0 grams to 100 liters 1. Active ingredient groundnut oil 2. Active ingredients Preparation of sesame oil: Dissolve the active ingredients in part of the fat while stirring. If necessary, heat gently, then after cooling, make up to the required volume, and aseptically transition through a suitable membrane filter paper with a pore size of 221 . Β. Water-miscible solvents (average release rate): 1. Active ingredient 0. 4.0 g 4-hydroxyfluorenyl-1,3-dioxane (glycerol formal) 40 g 1, 2 -Propylene glycol is added to 100 ml of 2 active ingredients. 10 g of glycerol dimethyl ketal is added to 1 g of 0 ml. Preparation: Dissolve the active ingredient in part of the solvent while stirring to make up to the desired volume. Sterile filtration through a suitable membrane filter paper with a pore size of 0 22 μm. C. Soluble solutes (quick release) 0 · 1 -1 · 0 g 10 g 20 g 1 g 100 ml 1. Active ingredient 5 ^ ethoxylated onion sesame oil (40 ethoxylated units) 1 2,2-propanediol fluorenyl alcohol water for injection 51 200305556 2. Active ingredient 0.1-1.0 g polyethoxylated sorbitan monooleyl ester (20 ethylene oxide units) 8 g 4-hydroxymethyl-1, 3-Dioxane (glycerol acetal) 20 g of benzyl alcohol 1 g of water for injection is added to 100 ml of preparation: the active ingredient is dissolved in a solvent and a surfactant, and the required volume is made up with water. Sterile filtration was performed through a suitable membrane filter paper with a pore size of 0.22 μm. 5. Sprinkler: Α. Active ingredient 5 grams of isopropyl myristate 10 grams of isopropanol are added to 100 ml Β. Active ingredient 2 grams of hexyl laurate 5 grams of medium chain triglyceride 15 grams of ethanol Add to 100 ml of C. Active ingredient 2 g of oleyl oleate 5 g of N-methyl-pyrrolidone 40 g of isopropanol Add to 100 ml

水溶性系統也可較佳地用於口服及/或瘤胃内的施用。 組合物也可包括其他的添加物，例如，穩定劑，例如 ，環氧化或非環氧化的植物油（環氧化的椰子油、油菜籽 油或大豆油）；消泡劑，例如，矽油；防腐劑；黏度調控 劑；黏結劑；增稠劑；以及肥料或其他的活性成份，以達 到特殊的效果。 52 200305556 其他的生物活性物質或添加物（其對於式i化合物是 中性的並且對於要治療的宿主動物不具有有害效果），2 及礦物鹽或維生素，也可加到上述組合物中。Water-soluble systems are also preferred for oral and / or rumen administration. The composition may also include other additives, for example, stabilizers, such as epoxidized or non-epoxidized vegetable oils (epoxidized coconut oil, rapeseed oil, or soybean oil); defoamers, such as silicone oil; preservatives ; Viscosity regulators; binders; thickeners; and fertilizers or other active ingredients to achieve special effects. 52 200305556 Other biologically active substances or additives (which are neutral to the compound of formula i and have no harmful effect on the host animal to be treated), 2 and mineral salts or vitamins may also be added to the above composition.

以下的實施例是作為舉例說明本發明’而非限制本發 明之用。字母“h”代表小時。 X 製備實施例 貫1例1 · 7-二氧唪二^基氣某 ]乙基）_4-三氟甲基苯酼眩 (a) 將2克的5, 7-二氯-8-羥基喹啉、1· 22克的氯丙 酮、1· 46克的碳酸鉀以及〇14克的氣化鉀溶解於2〇毫升 的丙酮中，並迴流同時攪拌18小時。在濾除並以丙酮清洗 之後，以此方式得到1-(5,7_二氣喹咐_8_基氧基）丙二g同， 為白色晶體。 (b) 將200毫克的氰化鈉及275毫克的氣化銨，加到 溶於2·8毫升25%氨水溶液中的923·5毫克1 —(5,7—二氣 喹啉-8 -基氧基）丙一 _之溶液，並將混合物在周圍溫度下 攪拌2天。之後’將混合物以1 〇毫升的乙酸乙酯處理，並 將有機相刀離、以水清洗並以氣化鈉溶液飽和、以硫酸鎂 乾燥、過遽以及蒸發。將殘留物藉由快速色層分析法純化 之後，以此方式得到2-胺基-3-(5, 7-二氯喹啉-8-基氧基）〜 2-甲基丙腈。 (c) 將275毫克的2-胺基-3-(5,7-二氯喹啉-8-基氧 基）_2-甲基丙腈溶解於7毫升的二氯甲烷，並加入218毫 53 200305556 克的三氟甲基苯曱酸、175毫克的乙基二異丙基胺、12 毫克的4-二甲基胺基吡啶以及185毫克的N-(3-二甲基胺 基丙基）〜N，-乙基碳化二亞胺氫氣化物。將混合物在周圍溫 度下授拌18小時，然後以20毫升的乙酸乙酯稀釋、以飽 矛的兔酸氫納溶液及飽和的氯化鈉溶液清洗、以硫酸鎂乾 ’:^源以及蒸發。將殘留物藉由快速色層分析法純化之 後’：此方式得到標題化合物，為白色晶體。 不The following examples are intended to illustrate the invention ' and not to limit the invention. The letter "h" stands for hour. X Preparation Example 1 Example 1 · 7-Dioxo di ^ hydrazine] ethyl) _4-trifluoromethylbenzene diazepam (a) 2 g of 5, 7-dichloro-8-hydroxyquine Porphyrin, 1.22 g of chloroacetone, 1.46 g of potassium carbonate, and 014 g of potassium gaseous were dissolved in 20 ml of acetone and stirred under reflux for 18 hours. After filtering off and washing with acetone, 1- (5,7_digasquina_8_yloxy) propanedig was obtained in the same manner as white crystals. (b) Add 200 mg of sodium cyanide and 275 mg of ammonium vaporized to 923.5 mg of 1- (5,7-digasquinoline-8-dissolved in 2.8 ml of a 25% aqueous ammonia solution. Alkoxy) propane, and the mixture was stirred at ambient temperature for 2 days. After that, the mixture was treated with 10 ml of ethyl acetate, and the organic phase was cut off, washed with water and saturated with a sodium vaporized solution, dried over magnesium sulfate, filtered, and evaporated. After the residue was purified by flash chromatography, 2-amino-3- (5, 7-dichloroquinolin-8-yloxy) ~ 2-methylpropionitrile was obtained in this way. (c) Dissolve 275 mg of 2-amino-3- (5,7-dichloroquinolin-8-yloxy) _2-methylpropionitrile in 7 ml of dichloromethane and add 218 mmol 53 200305556 Gram of trifluoromethylbenzoic acid, 175 mg of ethyldiisopropylamine, 12 mg of 4-dimethylaminopyridine, and 185 mg of N- (3-dimethylaminopropyl) ~ N, -ethylcarbodiimide hydrogenate. The mixture was allowed to stir at ambient temperature for 18 hours, then diluted with 20 ml of ethyl acetate, washed with saturated sodium bicarbonate solution and saturated sodium chloride solution, dried over magnesium sulfate, and evaporated. After the residue was purified by flash chromatography analysis': In this way, the title compound was obtained as white crystals. Do not

rft _ m表秸中所提及的物質，也可以類似於上述的方法 而製備。熔點值是以它表The substances mentioned in the rft_m table straw can also be prepared similarly to the method described above. Melting point is based on it

編號 1· 1 2-C1-苯基 1.2 2-C1-苯基 1· 3 2-C1-苯基 1.4 2-C1-苯基 1.5 2-C1-苯基 1· 6 2-C1-苯基 1.7 2-C1-苯基 1.8 2_C1_ 苯基 1.9 2-C1-苯基 ___ hr,_物理數據Number 1 · 1 2-C1-phenyl1.2 2-C1-phenyl1 · 3 2-C1-phenyl1.4 2-C1-phenyl 1.5 2-C1-phenyl1 · 6 2-C1-phenyl1.7 2-C1-phenyl 1.8 2_C1_phenyl 1.9 2-C1-phenyl ___ hr, _physical data

2-笨並呋喃基 2 -噻吩基 3 -噻吩基 2,嗪基 2-喹咐基 2-呋喃基 4 - CH3-噻吩一 2 一基 4 - Cl-噻吩-2-基 3 - CH*吩-2-基 54 200305556 1.10 2-α_苯基 苯並噻吩-2-基 1.11 2 - Cl-苯基 3 - C1-苯並噻吩-2-基 1.12 2-C1-苯基 唾林-3-基 1.13 2-C1-苯基 喹咐-4-基 1.14 2-C1-苯基 7-CF3-嗤咐-3-基 1.15 2-C1-苯基 1 - CH3-3-CF3-吡唑-5-基 1.16 2-C1-苯基 1 - CH3-4-CF3--基 熔點 47-50°C 1.17 2-C1-苯基 5 - Cl-2-瞳吩基 1.18 2-C1-苯基 5-CH3-2_[g 吩基 1.19 2-C1-苯基 5-C1-3-噻吩基 1.20 2 - Cl-苯基 5-CH3-3-_ 吩基 1.21 2-α-苯基 1-CH3-3-CF3-4-C1 -吡唑-5-基 1.22 2-C1-苯基 l-CH3-3-C6H5-4-Cl-吡唑-5-基 1.23 2-C1-苯基 5 - N〇2-2-呋喃基 1.24 2-C1-苯基 5-CH3-2-咲喃基 1.25 2-C1-苯基 3-呋喃基 1.26 2-C1-苯基 2 - CH3-3-咲喃基 1.27 2-CF3-苯基 2-苯並咲σ南基 1.28 2-CF3_苯基 2-噻吩基 熔點 153-5°C 1.29 2-CF3-苯基 3 -噻吩基 熔點 143 - 5°C 1.30 2 - CF3-苯基 2_[]比嗪基 膠狀 1.31 2-CF3-苯基 2-喹啉基 熔點 137-40°C 1.32 2 - CF3-苯基 2-呋σ南基 膠狀 1.33 2-CF3-苯基 4_CH3-噻吩-2-基 膠狀2-benzylfuryl 2-thienyl 3-thienyl 2, azinyl 2-quinyl 2-furyl 4-CH3-thienyl-2 monoyl 4-Cl-thien-2-yl 3-CH * phene 2-yl 54 200305556 1.10 2-α-phenylbenzothiophen-2-yl 1.11 2-Cl-phenyl 3-C1-benzothiophen-2-yl 1.12 2-C1-phenylsialin-3- 1.13 2-C1-phenylquinol-4-yl 1.14 2-C1-phenyl7-CF3-fluoren-3-yl 1.15 2-C1-phenyl1-CH3-3-CF3-pyrazole-5 -Radical 1.16 2-C1-phenyl 1-CH3-4-CF3-- radical melting point 47-50 ° C 1.17 2-C1-phenyl 5-Cl-2- pupillyl 1.18 2-C1-phenyl 5- CH3-2_ [g phenyl 1.19 2-C1-phenyl 5-C1-3-thienyl 1.20 2-Cl-phenyl 5-CH3-3-_ phenyl 1.21 2-α-phenyl 1-CH3-3 -CF3-4-C1 -pyrazol-5-yl1.22 2-C1-phenyll-CH3-3-C6H5-4-Cl-pyrazol-5-yl1.23 2-C1-phenyl5-N〇2 2-furyl 1.24 2-C1-phenyl 5-CH3-2-fluoranyl 1.25 2-C1-phenyl 3-furanyl 1.26 2-C1-phenyl 2-CH3-3-fluoranyl 1.27 2 -CF3-phenyl 2-benzopyrene sigma 1.28 2-CF3-phenyl 2-thienyl melting point 153-5 ° C 1.29 2-CF3-phenyl 3 -thienyl melting point 143-5 ° C 1.30 2- CF3-phenyl 2_ [] Zinyl colloid 1.31 2-CF3-phenyl 2-quinolinyl Melting point 137-40 ° C 1.32 2-CF3-phenyl 2-furyl sigma gel 1.33 2-CF3-phenyl 4_CH3-thiophene-2- Gelatinous

55 200305556 1.34 2 - CF3-苯基 4-Π-噻吩-2-基 熔點 128-30°C 1.35 2-CF3-苯基 3-CHS 吩-2-基 膠狀 1.36 2-CF3-苯基 苯並瞳吩-2-基 熔點 63-70°C 1.37 2 - CF3··苯基 3-C1 -苯並瞎吩-2-基 熔點 47-51°C 1.38 2 - CF3-苯基 嗤咐-3-基 膠狀 1.39 2 - CF3-苯基 喹啉-4-基 膠狀 1.40 2-CF3-苯基 7-CF3-嗤咐-3-基 熔點 209-12°C 1.41 2 - CF3-苯基 1 - CH3-3-CF3-毗唑-5-基 1.42 2_CF3-苯基 1 - CH3-4-CF3-毗咯-3-基 1.43 2-CF3-苯基 5-C1-2-噻吩基 1.44 2-CF3-苯基 5-CH3-2-噻吩基 1.45 2-CF3-苯基 5 - C1-3-噻吩基 1.46 2 - CF3-苯基 5-CH3-3-噻吩基 1.47 2-CF3_苯基 l-CHr3-CFr4-Cl-吡唑-5-基 1.48 2-CF3-苯基 1 - CH3-3-C6H5-4-C1 _〇比°坐_5-基 1.49 2-CF3-苯基 5 - N02-2-呋喃基 1.50 2-CF3-苯基 5-CH3-2-呋喃基 1.51 2 - CF3-苯基 3-呋喃基 1.52 2 - CFg-苯基 2 - CH3-3_咲喃基 1.53 5, 7-Cl2-嗤咐-8-基 4-CF3-苯基 1.54 5, 7-Cl2-_-8-基 4-0CF3-苯基 1.55 5, 7-Cl2-嗤琳一8-基 4-C6H5CO-苯基 1.56 5, 7-Cl2-喹啉-8-基 2, 6-Clg-苯基 1.57 5, 7-C1厂喹啉-8-基 4 - C1-苯基55 200305556 1.34 2-CF3-phenyl 4-Π-thiophen-2-yl Melting point 128-30 ° C 1.35 2-CF3-phenyl 3-CHS phen-2-yl colloid 1.36 2-CF3-phenylbenzo The melting point of citrin-2-yl is 63-70 ° C 1.37 2-CF3 ·· phenyl 3-C1 -benzobenzophen-2-yl melting point 47-51 ° C 1.38 2-CF3-phenyl Base colloid 1.39 2-CF3-phenylquinolin-4-yl colloid 1.40 2-CF3-phenyl 7-CF3- 嗤 -3-yl Melting point 209-12 ° C 1.41 2-CF3-phenyl 1- CH3-3-CF3-pyrazol-5-yl 1.42 2-CF3-phenyl 1-CH3-4-CF3-pyrrole-3-yl 1.43 2-CF3-phenyl 5-C1-2-thienyl 1.44 2-CF3 -Phenyl 5-CH3-2-thienyl 1.45 2-CF3-phenyl 5-C1-3-thienyl 1.46 2-CF3-phenyl 5-CH3-3-thienyl 1.47 2-CF3_phenyl 1- CHr3-CFr4-Cl-pyrazol-5-yl 1.48 2-CF3-phenyl 1-CH3-3-C6H5-4-C1 _〇 ratio ° 5-yl 1.49 2-CF3-phenyl 5-N02- 2-furyl 1.50 2-CF3-phenyl 5-CH3-2-furyl 1.51 2-CF3-phenyl 3-furyl 1.52 2-CFg-phenyl 2-CH3-3_pyranyl 1.53 5, 7 -Cl2- 嗤 -8-yl 4-CF3-phenyl 1.54 5, 7-Cl2 -_- 8-yl 4-0CF3-phenyl 1.55 5, 7-Cl2-pyridine-8-yl 4-C6H5CO- benzene 1.56 5, 7-Cl2- quinolin-8-yl 2, 6-Clg- phenyl 1.57 5, 7-C1 plant quinolin-8-yl 4 - C1- phenyl

56 200305556 1.58 5, 7-Cl2-_-8-基 1.59 5, 7-Cl2-_-8-基 1.60 5, 7-Cl2-喹咐-8-基 1. 61 5, 7-Cl2-嗤咐-8-基 1.62 5, 7-Cl2-_-8-基 1.63 5, 7-Cl2-喹咐-8-基 1.64 5, 7-Cl2-_-8-基 1.65 5, 7_C12-喹啉-8-基 1.66 5, 7_C12-喹啉-8-基 1.67 5, 7_Cl2-_-8-基 1. 68 5, 7-C12-嗤琳-8-基 1.69 5, 7-Cl2-_-8-基 1.70 5, 7_Cl2-_-8-基 1.71 5, 7-Cl2-喹啉一8-基 1.72 5, 7_C12-喹啉-8-基 1.73 5, 7-Cl2-喹啉-8-基 1. 74 5, 7-Cl2-嗤琳-基 1.75 5, 7_Cl2-_-8-基 1. 76 5, 7-Cl2-唾咐-8-基 1.77 5, 7-Cl2-_-8-基 1.78 5, 7-Cl2-_-8-基 1.79 5, 7-Cl2-_-8-基 1.80 5, 7-Cl2-_-8-基 1.81 5, 7-Cl2-喹啉-8-基 2-苯並咲喃基 2- 噻吩基 3- 噻吩基 2-[]比嗪基 2-喹啉基 2- 咲喃基 4- CH3-噻吩-2-基 4- α-噻吩-2-基 3- CH* 吩 _2-基 苯並噻吩基 3-α-苯並噻吩-2-基 喹咐-3-基 喹啉-4-基 7 - CF3-嗤咐-3-基 l-CH3-3-CF3-毗唑-5-基 1 -CH3-4-CF3-Dtt^_3-基 5- C1-2-噻吩基 5-CH3-2-噻吩基 5 - C1-3-DI 吩基 5-CH3_3-噻吩基 l-CH3-3-CFr4-C 卜吡唑-5-基 1 - CHr3_C6H5_4-C1-吡唑-5-基 5 - N02-2-呋喃基 5 - CH3-2-呋喃基56 200305556 1.58 5, 7-Cl2 -_- 8-yl 1.59 5, 7-Cl2 -_- 8-yl 1.60 5, 7-Cl2-quinyl-8-yl 1. 61 5, 7-Cl2- -8-yl 1.62 5, 7-Cl2 -_- 8-yl 1.63 5, 7-Cl2-quinol-8-yl 1.64 5, 7-Cl2 -_- 8-yl 1.65 5, 7_C12-quinoline-8 -Yl 1.66 5, 7-C12-quinolin-8-yl 1.67 5, 7-Cl2 -_- 8-yl 1. 68 5, 7-C12-quinolin-8-yl 1.69 5, 7-Cl2 -_- 8-yl 1.70 5, 7-Cl2 -_- 8-yl 1.71 5, 7-Cl2-quinoline-8-yl 1.72 5, 7-C12-quinoline-8-yl 1.73 5, 7-Cl2-quinoline-8-yl 1. 74 5, 7-Cl2-pyrene-yl 1.75 5, 7-Cl2 -_- 8-yl 1. 76 5, 7-Cl2-salyl-8-yl 1.77 5, 7-Cl2 -_- 8-yl 1.78 5, 7-Cl2 -_- 8-yl 1.79 5, 7-Cl2 -_- 8-yl 1.80 5, 7-Cl2 -_- 8-yl 1.81 5, 7-Cl2-quinolin-8-yl 2-benzo Sulfanyl 2-thienyl 3-thienyl 2-[] pyrazinyl 2-quinolinyl 2- sulfanyl 4- CH3-thien-2-yl 4- α-thien-2-yl 3- CH * Phen_2-ylbenzothienyl 3-α-benzothien-2-ylquinol-3-ylquinolin-4-yl 7-CF3-fluoren-3-yl l-CH3-3-CF3- Pyrazol-5-yl 1 -CH3-4-CF3-Dtt ^ _3-yl 5- C1-2-thienyl 5-CH3-2-thienyl 5-C1-3-DI phenyl 5-CH3_3-thienyl l-CH3-3-CFr4-C Pyrazol-5-yl 1-CHr3_C6H5_4 -C1-pyrazol-5-yl 5-N02-2-furyl 5-CH3-2-furyl

57 200305556 1.82 5, 7-Cl2-_-8-基 1.83 5, 7-Cl2-嗤咐-8-基 1.84 4, 5-Cl2-苯基 1.85 4, 5-Cl2-苯基 1.86 4, 5-Cl2_苯基 1.87 4, 5-Cl2-苯基 1.88 4, 5-Cl2-苯基 1.89 4, 5-Cl2-苯基 1.90 4, 5-Cl2-苯基 1.91 4, 5-Cl2-苯基 1.92 4, 5-Cl2-苯基 1.93 4, 5_C12-苯基 1.94 4, 5-Cl2-苯基 1.95 4, 5-Cl2-苯基 1.96 4, 5-Cl2-苯基 1.97 4, 5-Cl2-苯基 1.98 4,5-Cl2-苯基 1.99 4, 5-Cl2-苯基 1.100 4, 5-Cl2_苯基 1.101 4, 5-Cl2-苯基 1.102 4,5-Cl2-苯基 1.103 4, 5-Cl2-苯基 1.104 4,5-Cl2-苯基 1.105 4,5-Cl2_苯基 3- 呋喃基 2-CH3-3-映喃基 2-苯並咲喃基 2售吩基 3 - _吩基 2.秦基 2-嗟琳基 2- 咲口南基 4- CH3-瞳吩-2-基 4 - Cl-噻吩-2-基 3 - Cl-噻吩-2-基 苯並噻吩-2-基 3- C1-苯並_吩_2-基 喔咐-3-基 嗤琳-4-基 7_CF3-喔咐-3-基 l-CH3-3-CF3-吡唑-5-基 l-CH3-4-CF3-吡咯-3-基 5- Π - 2-噻吩基 5-CHr2-噻吩基 5-C卜3 -噻吩基 5 - CH3-3-[«吩基 l-CH3-3-CF3-4-Cl-毗唑-5-基 l-CH3-3-C6H5_4-a-毗唑-5-基57 200305556 1.82 5, 7-Cl2 -_- 8-yl 1.83 5, 7-Cl2- -8-yl 1.84 4, 5-Cl2-phenyl 1.85 4, 5-Cl2-phenyl 1.86 4, 5- Cl2-phenyl 1.87 4, 5-Cl2-phenyl 1.88 4, 5-Cl2-phenyl 1.89 4, 5-Cl2-phenyl 1.90 4, 5-Cl2-phenyl 1.91 4, 5-Cl2-phenyl 1.92 4, 5-Cl2-phenyl 1.93 4, 5-C12-phenyl 1.94 4, 5-Cl2-phenyl 1.95 4, 5-Cl2-phenyl 1.96 4, 5-Cl2-phenyl 1.97 4, 5-Cl2-benzene Group 1.98 4,5-Cl2-phenyl 1.99 4, 5-Cl2-phenyl 1.100 4, 5-Cl2-phenyl 1.101 4, 5-Cl2-phenyl 1.102 4, 5-Cl2-phenyl 1.103 4, 5 -Cl2-phenyl1.104 4,5-Cl2-phenyl1.105 4,5-Cl2-phenyl3-furanyl 2-CH3-3-enyl-2-benzopyranyl 2 phenenyl 3-_ Phenyl 2. Qinyl 2-Phenyl 2-Phenanyl 4-CH3- Putophen-2-yl 4 -Cl-thiophen-2-yl 3 -Cl-thiophen-2-ylbenzothiophene-2 -Yl 3-C1-benzo_phen_2-yloxazol-3-ylpyridin-4-yl7_CF3-oxazol-3-yll-CH3-3-CF3-pyrazol-5-yll- CH3-4-CF3-pyrrole-3-yl 5- Π-2-thienyl 5-CHr2-thienyl 5-Cb 3-thienyl 5-CH3-3-[«phenyll-CH3-3-CF3 -4-Cl-pyrazol-5-yl l-CH3-3-C6H5_4-a-pyrazol-5-yl

58 200305556 1.106 4,5-Cl2-苯基 1.107 4,5-Cl2-苯基 1.108 4,5-Cl2-苯基 1.109 4,5-Cl2-苯基 1.110 4-0CH3-苯基 1.111 4-OCH3-苯基 1.112 4-OCH3-苯基 1.113 4-OCH3-苯基 1.114 4-OCH3-苯基 1.115 4-OCH3-苯基 1.116 4-OCH3-苯基 1.117 4-0CH3-苯基 1.118 4-OCH3-苯基 1.119 4-0CH3-苯基 1.120 4-0CH3-苯基 1.121 4-OCH3-苯基 1.122 4-0CH3-苯基 1.123 4-0CH3-苯基 1.124 4-0CH3-苯基 1.125 4-0CH3-苯基 1.126 4-OCH3-苯基 1.127 4-OCH3-苯基 1.128 4-0CH3-苯基 1.129 4-0CH3-苯基 5-NO「2-呋喃基 5 - CH3 - 2-咲喃基 3-咲喃基 2 - CH3-3-呋喃基 2- 苯並呋喃基 2 -噻吩基 3- 噻吩基 2-Dtt嗪基 2-喹咐基 2- 映喃基 4 - cHrni 吩-2-基 4- CH*吩-2-基 3- CH* 吩-2-基 苯並_吩-2-基 3 - C1-苯並噻吩-2-基 嗤咐-3-基 喹啉-4-基 7 - CF3-喹啉-3-基 1-CH3-3-CFr 毗唑-5-基 卜CHr4-0&毗咯-3-基 5- C1-2-瞎吩基 5-CHr2-噻吩基 5 - C1-3-噻吩基 5-CH3-3-l® 吩基58 200305556 1.106 4,5-Cl2-phenyl 1.107 4,5-Cl2-phenyl 1.108 4,5-Cl2-phenyl 1.109 4,5-Cl2-phenyl 1.110 4-0CH3-phenyl 1.111 4-OCH3- Phenyl 1.112 4-OCH3-phenyl 1.113 4-OCH3-phenyl 1.114 4-OCH3-phenyl 1.115 4-OCH3-phenyl 1.116 4-OCH3-phenyl 1.117 4-0CH3-phenyl 1.118 4-OCH3-benzene Group 1.119 4-0CH3-phenyl 1.120 4-0CH3-phenyl 1.121 4-OCH3-phenyl 1.122 4-0CH3-phenyl 1.123 4-0CH3-phenyl 1.124 4-0CH3-phenyl 1.125 4-0CH3-phenyl 1.126 4-OCH3-phenyl 1.127 4-OCH3-phenyl 1.128 4-0CH3-phenyl 1.129 4-0CH3-phenyl 5-NO, 2-furanyl 5-CH3-2-fluoranyl 3-fluoranyl 2-CH3-3-furanyl 2-benzofuranyl 2-thienyl 3-thienyl 2-Dttazinyl 2-quinolyl 2-enanyl 4-cHrni phen-2-yl 4-CH * phene 2-yl 3-CH * phen-2-ylbenzo-phen-2-yl 3-C1-benzothiophen-2-ylsulfonyl-3-ylquinolin-4-yl 7-CF3-quinoline -3-yl 1-CH3-3-CFr pyrazol-5-ylb CHr4-0 & pyrrol-3-yl 5- C1-2-benzophenyl 5-CHr2-thienyl 5-C1-3-thiophene 5-CH3-3-l® phenyl

59 200305556 1.130 4-0CH3-苯基 1.131 4-0CH3-苯基 1.132 4-0CH3-苯基 1.133 4-0CH3-苯基 1.134 4-0CH3-苯基 1.135 4-0CH3-苯基 1.136 2-Bi·-4,5-F2-苯基 1.137 2-Bi-4,5-F2-苯基 1.138 2-Br-4,5-F2-苯基 1.139 2-Br-4,5-F2-苯基 1.140 2-Br-4,5-F2-苯基 1.141 2_Br-4, 5-F2_苯基 1.142 2-Br-4,5-F2-苯基 1.143 2-Br-4,5-F2-苯基 1.144 2-Br-4,5-F2-苯基 1.145 2-Br-4,5-F2-苯基 1.146 2-Br-4,5-F2-苯基 1.147 2-Br-4,5-F2-苯基 1.148 2-Br-4,5-F2-苯基 1.149 2-Br-4,5-F2-苯基 1.150 2-Br-4, 5-F2-苯基 1.151 2-Br-4,5-F2-苯基 1.152 2-Br-4,5_F2-苯基 1.153 2-Br-4,5-F2-苯基 l-CHr3-CF3-4-Cl-吡唑-5-基 1- CH3-3-C6H5-4-Cl-毗唑-5-基 5~·Ν〇2-2-咲喃基 5-CH3-2-呋喃基 3-咲喃基 2- CH3 - 3-咲喃基 2 -苯並呋喃基 2- _吩基 3- 噻吩基 2-Dtt嗪基 2- 喹啉基 呋喃基 4- CH3-噻吩_2-基 4-C1-噻吩-2-基 3- CHi 吩-2-基 苯並噻吩-2-基 3-C1 -苯並瞎吩-2-基 嗤咐-3-基 喹啉-4-基 7-CF3-嗤琳-3-基 l-CH3-3-CF3-毗唑 -基 1 - CH3-4-CF3-[ll;b各-3-基 5 - α-2-ui 吩基 5 - CH3-2-噻吩基59 200305556 1.130 4-0CH3-phenyl 1.131 4-0CH3-phenyl 1.132 4-0CH3-phenyl 1.133 4-0CH3-phenyl 1.134 4-0CH3-phenyl 1.135 4-0CH3-phenyl 1.136 2-Bi ·- 4,5-F2-phenyl 1.137 2-Bi-4,5-F2-phenyl 1.138 2-Br-4,5-F2-phenyl 1.139 2-Br-4,5-F2-phenyl 1.140 2- Br-4,5-F2-phenyl 1.141 2_Br-4, 5-F2_phenyl 1.142 2-Br-4,5-F2-phenyl 1.143 2-Br-4,5-F2-phenyl 1.144 2- Br-4,5-F2-phenyl 1.145 2-Br-4,5-F2-phenyl 1.146 2-Br-4,5-F2-phenyl 1.147 2-Br-4,5-F2-phenyl 1.148 2-Br-4,5-F2-phenyl 1.149 2-Br-4,5-F2-phenyl 1.150 2-Br-4, 5-F2-phenyl 1.151 2-Br-4,5-F2-benzene Group 1.152 2-Br-4,5-F2-phenyl 1.153 2-Br-4,5-F2-phenyl l-CHr3-CF3-4-Cl-pyrazol-5-yl 1-CH3-3-C6H5-4 -Cl-pyrazol-5-yl 5 ~ · NO2-2-fluoranyl 5-CH3-2-furanyl 3-fluoranyl 2- CH3-3-fluoranyl 2-benzofuranyl 2 -_Phenyl 3-thienyl 2-Dttazinyl 2-quinolinylfuranyl 4- CH3-thienyl-2-yl 4-C1-thien-2-yl 3- CHi phen-2-ylbenzothiophene- 2-yl 3-C1 -benzobenzophen-2-ylsulfonyl-3-ylquinolin-4-yl 7-CF3-fluorin-3-yll-CH3-3-CF3-pyrazole-yl-1 -CH3-4-CF3- [ll; b each-3-yl 5- α-2-ui Phenyl 5-CH3-2-thienyl

60 200305556 1.154 2-Br-4,5-F2-苯基 1.155 2-Br-4,5-F2-苯基 1.156 2-Br-4,5-F2-苯基 1.157 2-Br-4,5-F2_ 苯基 1.158 2-Br~~4, 5-F2_ 苯基 1.159 2-Br-4,5-F2-苯基 1.160 2-Br_4,5-F2-苯基 1.161 2-Br~4, 5_F2-苯基 1.162 3-C2H502C-2-呋喃基 1.163 3-C2H502C-2-呋喃基 1.164 3-C2H502C-2-呋喃基 1.165 3-C2H502C-2-呋喃基 1.166 3-C2H502C-2-映喃基 1.167 3-C2H502C-2-呋喃基 1.168 3-C2H502O2-呋喃基 1.169 3-C2H502C-2-呋喃基 1.170 3-C2H502C-2-呋喃基 1.171 3-C2H502C-2-呋喃基 1.172 3-C2H502C-2-呋喃基 1.173 3-C2H502C-2-呋喃基 1.174 3-C2H502C-2-呋喃基 1.175 3-C2H502C-2-呋喃基 1.176 3-C2H502C-2-呋喃基 1.177 3-C2H502C-2-呋喃基 5-C1-3-噻吩基 5-CH3-3-Di 吩基 l-CH3-3-CF3-4-α-毗唑 _5-基 1- CH3-3-C6H5-4-Cl-毗唑-5-基 5-N〇2-2-咲喃基 5-CH3-2-呋喃基 3-映喃基 2- CH3-3-呋喃基 2-苯並呋喃基 2- 噻吩基 3- 噻吩基 2 - [I比嗦基 2- 喹啉基 咲喃基 4- CH3-噻吩-2-基 4-C1-瞳吩-2-基 3- C1-瞎吩-2-基 苯並噻吩-2-基 3-C1-苯並_吩-2-基 嗤咐-3-基 嗤咐-4-基 7_CF3-嗤琳-3-基 1 - CH3-3-CF3_ 吡唑-5-基 1-CH3-4_CF3-D[tp各基60 200305556 1.154 2-Br-4,5-F2-phenyl 1.155 2-Br-4,5-F2-phenyl 1.156 2-Br-4,5-F2-phenyl 1.157 2-Br-4,5- F2_phenyl 1.158 2-Br ~~ 4, 5-F2_phenyl 1.159 2-Br-4,5-F2-phenyl 1.160 2-Br_4,5-F2-phenyl 1.161 2-Br ~ 4, 5_F2-benzene 1.162 3-C2H502C-2-furyl 1.163 3-C2H502C-2-furyl 1.164 3-C2H502C-2-furyl 1.165 3-C2H502C-2-furyl 1.166 3-C2H502C-2-enyl 1.167 3- C2H502C-2-furyl 1.168 3-C2H502O2-furyl 1.169 3-C2H502C-2-furyl 1.170 3-C2H502C-2-furyl 1.171 3-C2H502C-2-furyl 1.172 3-C2H502C-2-furyl 1.173 3-C2H502C-2-furyl 1.174 3-C2H502C-2-furyl 1.175 3-C2H502C-2-furyl 1.176 3-C2H502C-2-furyl 1.177 3-C2H502C-2-furyl 5-C1-3- Thienyl 5-CH3-3-Di phenyl l-CH3-3-CF3-4-α-pyrazol_5-yl 1-CH3-3-C6H5-4-Cl-pyrazol-5-yl 5-N 〇2-2-Pyranyl 5-CH3-2-furyl 3-enantyl 2-CH3-3-furyl 2-benzofuryl 2-thienyl 3-thienyl 2-[I 2-quinolinylpyranyl 4-CH3-thien-2-yl 4-C1- pupill-2-yl 3-C1-blphen-2-ylbenzothien-2-yl 3-C1-benzene _ 2-yl-3-laugh laugh commanded commanded lin-4-yl-3-7_CF3- laugh 1 - CH3-3-CF3_ pyrazol-5-yl 1-CH3-4_CF3-D [tp of each group

61 200305556 1.178 3_C2H502C-2-呋喃基 1.179 3-C2H502C-2-呋喃基 1· 180 3Η^Η5020-2-咲喃基 1.181 3-C2H502C-2-呋喃基 1.182 3-C2H502C-2-呋喃基 1.183 3_C2H502C-2-呋喃基 1.184 3-C2H502C-2-呋喃基 1.185 3-C2H502C-2-呋喃基 1.186 3-C2H5〇2C-2-咲喃基 1.187 3_C2H502C-2-呋喃基 1.188 1_CH3-2-口引 P 朵基 1.189 l_CH3-2-口3丨D朵基 1.190 l_CH3-2-口3丨D朵基 1.191 1-CH3-2-吲哚基 1.192 M：H3-2-吲哚基 1.193 l-CH3-2-吲哚基 1.194 1 -CH3-2-吲哚基 1.195 l-CH3-2-吲哚基 1.196 l-CH3-2-吲哚基 1.197 l_CH3-2-吲哚基 1_ 198 1 - CH3-2-口3P 朵基 1.199 l-CHr2-_朵基 1.200 l-CH3-2-U3丨哚基 1. 201 1-CH3-2-D3丨P朵基 5 - C1-2-噻吩基 5-CH3-2-噻吩基 5-Cl-3_Hl 吩基 5-CH3-3-噻吩基 1 -CH3-3-CF3-4-Cl -吡唑-5-基 1- CH3-3-C6H5-4-C 卜吡唑 基 5 - NO「2-呋喃基 5-CH3-2-呋喃基 3-呋喃基 2- CH3-3-呋喃基 2-苯並咲喃基 2- 噻吩基 3- 噻吩基 2-瞧基 2_喹咐基 2- 呋喃基 4 - CH3-噻吩-2-基 4- Π-噻吩-2-基 3- α-_ 吩-2-基 苯並噻吩-2-基 3 - C1-苯並噻吩-2-基 喹琳-3-基 喹琳-4-基 7-CF3-嗤咐-3-基61 200305556 1.178 3_C2H502C-2-furyl 1.179 3-C2H502C-2-furyl 1. 180 3 Η Η 5020-2-fluoranyl 1.181 3-C2H502C-2-furyl 1.182 3-C2H502C-2-furyl 1.183 3_C2H502C 2-furyl 1.184 3-C2H502C-2-furyl 1.185 3-C2H502C-2-furyl 1.186 3-C2H5〇2C-2-fluoranyl 1.187 3_C2H502C-2-furyl 1.188 1_CH3-2- Dodecyl 1.189 l_CH3-2-port 3 丨 D Dolyl 1.190 l_CH3-2-port 3 丨 D Dolyl 1.191 1-CH3-2-indolyl 1.192 M: H3-2-indolyl 1.193 l-CH3-2 -Indolyl 1.194 1 -CH3-2-indolyl 1.195 l-CH3-2-indolyl 1.196 l-CH3-2-indolyl 1.197 l_CH3-2-indolyl 1- 198 1-CH3-2- Methyl 3P dolyl 1.199 l-CHr2-_dolyl 1.200 l-CH3-2-U3 丨 indolyl 1. 201 1-CH3-2-D3 丨 P dolyl 5-C1-2-thienyl 5-CH3-2 -Thienyl 5-Cl-3_Hl phenyl 5-CH3-3-thienyl 1 -CH3-3-CF3-4-Cl -pyrazol-5-yl 1-CH3-3-C6H5-4-C 5-NO "2-furyl 5-CH3-2-furyl 3-furyl 2-CH3-3-furyl 2-benzopyranyl 2- thienyl 3- thienyl 2-carbyl 2_ Quinyl 2-furyl 4-CH3-thien-2-yl 4- Π-thien-2-yl 3- α-_phen-2- Benzothiophen-2-yl 3 - C1- benzothiophen-2-yl-3-quinolin Lin Lin quinolin-4-yl 7-CF3- 3-laugh commanded

62 200305556 1.202 l-CH3-2-吲哚基 l-CH3-3-CF3-毗唑-5-基 1.203 l_CH3-2-吲哚基 l-CH3-4-CF3-毗咯-3-基 1.204 1-CH3-2_I1 引哚基 5-C1-2-噻吩基 1.205 1-CH3 - 2-吲哚基 5 - CH3_2_瞎吩基 1.206 l-CH3-2-吲哚基 5-C1-3-噻吩基 1.207 l-CH3-2-吲 11 朵基 5-CH3-3-噻吩基 1.208 l-CH3-2-吲哚基 1-CH3-3-CFr4-C 卜毗唑-5-基 1.209 l-CH3-2-吲哚基 1 -CH3-3-C6H5-4_a -毗唑-5-基 1.210 l-CH3-2-吲哚基 5倚2-呋喃基 1. 211 1 -CH3-2-口引D朵基 5-CH3-2-咲喃基 1.212 l-CH3-2-吲哚基 3-呋喃基 1.213 1-CH3_2-吲哚基 2-CH3-3-咲喃基 1. 214 1-CH3-3-D引除基 2 -苯並呋喃基 1.215 1-CH3-3-吲 D 朵基 2-_吩基 1.216 1_CH3-3-吲 U 朵基 3 - _吩基 1.217 l-CH3-3-吲哚基 2 - Dtt嗉基 1.218 1-CH3-3-吲哚基 2-喹啉基 1.219 1-CH3_3-吲哚基 2_呋。南基 1.220 l_CH3-3-吲哚基 4 - CHr噻吩-2-基 1.221 1-013-3_吲哚基 4-CH*吩-2-基 1.222 l-CH3-3-D引哚基 3-CH*吩-2-基 1.223 l-CH3-3-口3丨哚基 苯並瞎吩-2-基 1.224 l-CHr3-吲哚基 3-C1-苯並瞳吩-2-基 1.225 l_CH3-3-D引晬基 嗤咐-3-基 63 200305556 1.226 l-CH3-3-吲哚基 1.227 l-CH3-3-吲哚基 1.228 l-CH3-3-吲D朵基 1.229 l-CH3-3-吲哚基 1.230 l-CH3-3-D引Q朵基 1.231 l-CH3-3-吲 D 朵基 1.232 l-CH3-3-吲哚基 1.233 l-CH3-3-吲哚基 1.234 l-CH3-3-吲哚基 1.235 1-CH3-3-吲哚基 1.236 l-CH3-3-吲II朵基 1.237 l-CHr3-吲哚基 1.238 1-CH3-3-吲哚基 1.239 l-CH3-3-吲哚基 1.240 l_CH3-2-CN_3-吲哚基 1.241 1-CH3-2-CN-3-吲哚基 1.242 1-CH3-2-CN - 3-闲丨哚基 1.243 l_CH3-2-CN-3-吲哚基 1.244 l-CHr2-CN-3-吲D朵基 1. 245 I-CH3-2-CN-3-口3丨時基 1 · 246 1-CH3-2-CN-3-口引D朵基 1.247 l_CH3-2-CN-3-吲哚基 1.248 1_CH3-2 - CN-3-吲哚基 1.249 1-CH3-2-CN-3-吲哚基 喔咐-4-基 7 - CFr_-3-基 1 - CH3-3-CF3-毗唑-5-基 l-CH3-4-CF3-毗咯-3-基 5 -C1-2-瞳吩基 5-CH3-2-噻吩基 5-C1-3-噻吩基 5-CH3-3-Di 吩基 1 -CH3-3-CF3-4-C1 --基 1- CH3-3-C6H5-4-a-毗唑-5-基 5-N02-2-呋喃基 5倚2-呋喃基 3- 呋喃基 2_CH3-3-咲喃基 2- 苯並呋喃基 2-_吩基 3 -噻吩基 2-D比嗪基 2-喔咐基 2-呋喃基 4- CH3-噻吩-2-基 4-Π-噻吩-2-基 3 -α_噻吩-2-基 苯並_吩-2-基62 200305556 1.202 l-CH3-2-indolyl l-CH3-3-CF3-pyrazol-5-yl 1.203 l_CH3-2-indolyl l-CH3-4-CF3-pyrrole-3-yl 1.204 1 -CH3-2_I1 Indolyl 5-C1-2-thienyl 1.205 1-CH3-2-indolyl 5--CH3_2-blindenyl 1.206 l-CH3-2-indolyl 5-C1-3-thienyl 1.207 l-CH3-2-in11 odoyl 5-CH3-3-thienyl 1.208 l-CH3-2-indolyl 1-CH3-3-CFr4-C pipizol-5-yl 1.209 l-CH3- 2-Indolyl 1 -CH3-3-C6H5-4_a -Pyrazol-5-yl 1.210 l-CH3-2-indolyl 5 1-furyl 1.211 1 -CH3-2- 5-CH3-2-fluoranyl 1.212 l-CH3-2-indolyl 3-furanyl 1.213 1-CH3_2-indolyl 2-CH3-3-fluoranyl 1. 214 1-CH3-3- D-Executive 2-Benzofuranyl 1.215 1-CH3-3-indodol 2- 2-phenyl 1.216 1-CH3-3-in U dol 3- 3-phenyl 1.217 l-CH3-3-indolyl 2-Dttamido 1.218 1-CH3-3-indolyl 2-quinolinyl 1.219 1-CH3_3-indolyl 2-furyl. South base 1.220 l_CH3-3-indolyl 4-CHr thienyl-2-yl 1.221 1-013-3_indolyl 4-CH * phen-2-yl 1.222 l-CH3-3-D indolyl 3- CH * phen-2-yl 1.223 l-CH3-3-port 3-indolylbenzophen-2-yl 1.224 l-CHr3-indolyl 3-C1-benzophenphen-2-yl 1.225 l_CH3- 3-D indioyl-3-yl 63 200305556 1.226 l-CH3-3-indolyl 1.227 l-CH3-3-indolyl 1.228 l-CH3-3-indolyl 1.229 l-CH3- 3-Indolyl 1.230 l-CH3-3-D Q-introducer 1.231 l-CH3-3-inD-indolent 1.232 l-CH3-3-indolyl 1.233 l-CH3-3-indolyl 1.234 l -CH3-3-indolyl 1.235 1-CH3-3-indolyl 1.236 l-CH3-3-indolyl 1.237 l-CHr3-indolyl 1.238 1-CH3-3-indolyl 1.239 l- CH3-3-indolyl 1.240 l_CH3-2-CN_3-indolyl 1.241 1-CH3-2-CN-3-indolyl 1.242 1-CH3-2-CN-3-oxolinyl 1.243 l_CH3-2 -CN-3-indolyl 1.244 l-CHr2-CN-3-indolyl 1.245 I-CH3-2-CN-3-port 3 丨 time base 1 246 1-CH3-2-CN- 3-Port D-Doxy 1.247 l_CH3-2-CN-3-indolyl 1.248 1_CH3-2-CN-3-indolyl 1.249 1-CH3-2-CN-3-indolyl 7-CFr_-3-yl 1-CH3-3-CF3-pyrazol-5-yl l-CH3-4-CF3- Pyrrol-3-yl 5 -C1-2-pidophenyl 5-CH3-2-thienyl 5-C1-3-thienyl 5-CH3-3-Di phenyl 1 -CH3-3-CF3-4- C1 --yl 1-CH3-3-C6H5-4-a-pyrazol-5-yl 5-N02-2-furanyl 5-2-furanyl 3-furanyl 2-CH3-3-fluoranyl 2-benzene Benzofuranyl 2-_phenyl 3-thienyl 2-D bisazinyl 2-oxanyl 2-furyl 4-CH3-thien-2-yl 4-Π-thien-2-yl 3 -α-thiophen 2-ylbenzo-phen-2-yl

64 200305556 1.250 l-CH3-2-CN-3M[Il 朵基 3-C1-苯並噻吩-2-基 1.251 1 -CH3-2-CN-3-卩3 P 朵基 唾林-3-基 1.252 1 -CH3 - 2-CN-3-口3 丨 D 朵基 喹咐-4-基 1.253 1 - CH3-2-CN-3-口5 丨 D 朵基 7 - CF3-嗤咐-3-基 1.254 l-CHr2-CN-3-吲 B 朵基 l-CH3-3-CF3-毗唑-5-基 1.255 1 - CH3-2-CN-3-口引 B 朵基 1 -CH3-4-CF3-Dtb各 基 1.256 1-CV2-CN-3-D3 丨 n 朵基 5-C1-2-噻吩基 1.257 l-CHr2-CN-3-口3 丨 D 朵基 5 - CH3-2-噻吩基 1.258 1-CH3-2-CN-3-别 η 朵基 5-α-3-_ 吩基 1.259 1-CH3-2 - CN - 3_ 口引 Β 朵基 5-CH3-3-Hi 吩基 1.260 1 -CH3-2-CN-3_口5旧朵基 1 -CH3-3-CF3-4-a -吡唑-5-基 1.261 1 - CH3-2-CN-3-卩引 D 朵基 1 - CHr3-C6H5-4-C1-毗唑-5-基 1.262 l-CH3-2-CN-3-D3 丨 H 朵基 5-ΝΟΓ2-呋喃基 1.263 1 -CH3-2-CN-3-闲丨D 朵基 5-CHr2-呋喃基 1.264 l-CH3-2-CN-3-口3 丨時基 3-映喃基 1.265 1-CH3-2-CN-3-D3[II 朵基 2-CH3-3-肤喃基 1.266 1，2-(CH3)2-3-C2H502C-4-吡咯基 2-苯並呋喃基 1.267 1，2-(CH3)r3-C2H502C-4-吡咯基 2-噻吩基 1.268 1，2-(CH3)2_3-C2H502C-4-吡咯基 3-噻吩基 1.269 1，2-(CH3)2-3-C2H502C-4-吡咯基 2-Dtt嗪基 1.270 1，2-(CH3)2-3-C2H502C-4-吡咯基 2-瞳咐基 1.271 1，2-(CH3)2_3- 2-咲口南基 1.272 1，2-(CH3)2-3-C2H502C-4-吡咯基 4-CH3-瞳吩-2-基 1.273 1，2-(CH3)2-3-C2H502C-4-吡咯基 4 - Cl-噻吩-2-基 65 200305556 1.274 1，2-(CH3)2*~3-C2H5〇2C-4_Dtt洛基 3 - CH8 吩-2-基 1.275 1，2-(CH3)2-3-C2H502C-4-口比咯基 苯並瞎吩基 1.276 1，2-(CH3)2-3-C2H502C-4-毗咯基 3 - C1 -苯並瞎吩-2-基 1.277 1，2-(CH3)2-3-C2H502C_4_毗咯基 喔咐-3-基 1.278 1，2_(CH3)2-3-C2H502C-4-毗咯基 喹咐-4-基 1.279 1，2-(CH3)2-3_C2H502C_4_卩比11 各基 7-CF3-_-3-基 1.280 1， l-CHr3-CF3-吡唑-5-基 1.281 1，2-(CH3)2-3-C2H502C-4-吡咯基 1-013-445_吡咯-3-基 1.282 1，2-(CH3)2-3-C2H502C_4-卩比p各基 5 - C1-2-噻吩基 1.283 1，2-(CH3)2-3-C2H502C-4_吡咯基 5 - CH3-2-Di 吩基 1.284 1，2-(CH3)2-3-C2H502C-4-吡咯基 5-α-3-_ 吩基 1.285 1，2-(CH3)2-3-C2H502C_4-吡咯基 5 - CH3-3__ 吩基 1.286 1，2-(CH3)2-3-C2H502C-4-吡咯基 1 -CH3-3-CF3-4-C1 -吡唑-5-基 1.287 1，2-(CH3)2-3-C2H502C-4-吡咯基 l-CH3-3-C6Hr4-C 卜吡唑-5-基 1.288 1，2_(CH3)2_3-C2H5〇2C-4-D比13各基 5 - N02-2-呋喃基 1.289 1，2-(CH3)2-3-C2H502C-4-吡咯基 5 - 013-2-映11南基 1.290 1，2-(CH3)2-3-C2H502C-4-吡咯基 3-咲1^基 1.291 1，2-(CH3)2-3-C2H5〇2C-4-卩[;卜各基 2 - CH3-3-呋喃基 1.292 6-C2H50-苯並噻吩-3-基 2-苯並呋喃基 1.293 6-C2H50-苯並_吩-3-基 2-噻吩基 1.294 6-C2H50-苯並噻吩-3-基 3-_吩基 1.295 6-C2H50-苯並噻吩-3-基 2-[]比嗪基 1.296 6-C2H50-苯並瞳吩-3-基 2-喔咐基 1.297 6-C2H50-苯並噻吩-3-基 2-映σ南基 66 200305556 1.298 6-C2H50-苯並噻吩-3-基 1.299 6-C2H50-苯並噻吩-3-基 1.300 6-C2H50-苯並噻吩-3-基 1.301 6-C2H50-苯並噻吩-3-基 1.302 6-C2H50-苯並噻吩-3-基 1.303 6-C2H5〇-苯並噻吩-3-基 1.304 6-C2H50-苯並噻吩-3-基 1.305 6-C2H50-苯並_吩-3-基 1.306 6-C2H50-苯並噻吩-3-基 1.307 6-C2H50-苯並噻吩-3-基 1.308 6-C2H50-苯並噻吩-3-基 1.309 6-C2H50-苯並噻吩-3-基 1.310 6-C2H5〇-苯並噻吩-3-基 1. 311 6-C2H50-苯並噻吩-3-基 1.312 6-C2H50-苯並噻吩-3-基 1.313 6-C2H50-苯並噻吩-3-基 1.314 6-C2H50-苯並_吩-3-基 1.315 6-C2H50-苯並噻吩-3-基 1.316 6-C2H50-苯並噻吩-3-基 1.317 6-C2H50-苯並噻吩-3-基 1. 318 2-CH302C-4*~Br-3-瞳吩基 1.319 2-CH302C-4-Br-3-噻吩基 1.320 2-CH302C-4-Br+噻吩基 1.321 2 - CHAC-4 - Br - 3-噻吩基 4-CH3-瞳吩-2-基 4- α-噻吩-2-基 3-C卜噻吩-2-基 苯並噻吩-2-基 3-C1 -苯並瞎吩-2-基 嗟咐-3-基 嗤咐-4-基 7-CF3-喹啪-3-基 1 - CH3-3-CF3-吡唑-5-基 1 -CH3-4-CF3-日[;卜各_3-基 5- C1-2-噻吩基 5-CH3-2-_ 吩基 5 - C1-3-噻吩基 5 - CH3-3-噻吩基 l-CH3-3-CF3-4-Π-吡唑-5-基 1- CHr3-C6H5-4-C 卜毗唑-5-基 5-N02-2-呋喃基 5 - CH3-2-咲°南基 3-咲喃基 2 - CH「3-呋喃基 2- 苯並呋喃基 2-噻吩基 3 -噻吩基 2-0比嗪基64 200305556 1.250 l-CH3-2-CN-3M [Il dolyl 3-C1-benzothiophen-2-yl 1.251 1 -CH3-2-CN-3-fluorene 3 P dolyl salin-3-yl 1.252 1 -CH3-2-CN-3-port 3 丨 D dorylquinol-4-yl1.253 1 -CH3-2-CN-3-port 5 丨 D doryl7-CF3-fluoron-3-yl1.254 l-CHr2-CN-3-inB dolyl l-CH3-3-CF3-pyrazol-5-yl 1.255 1-CH3-2-CN-3- methylol 1-CH3-4-CF3- Dtb each group 1.256 1-CV2-CN-3-D3 丨 n aryl 5-C1-2-thienyl 1.257 l-CHr2-CN-3-port 3 丨 D aryl 5-CH3-2-thienyl 1.258 1 -CH3-2-CN-3-Alleta dol 5-α-3-_ phenyl 1.259 1-CH3-2-CN-3_ Ortho Benzyl 5-CH3-3-Hi phen 1.260 1 -CH3 -2-CN-3_port 5 old dolyl 1 -CH3-3-CF3-4-a -pyrazol-5-yl 1.261 1-CH3-2-CN-3- C6H5-4-C1-pyrazol-5-yl 1.262 l-CH3-2-CN-3-D3 丨 H aryl 5-NΟΓ2-furyl 1.263 1 -CH3-2-CN-3-yl 丨 D aryl 5-CHr2-furyl 1.264 l-CH3-2-CN-3-port 3 丨 Time base 3-enanyl 1.265 1-CH3-2-CN-3-D3 [II Uranyl 1.266 1,2- (CH3) 2-3-C2H502C-4-pyrrolyl 2-benzofuranyl 1.267 1,2- (CH3) r3-C2H502C-4 -Pyrrolyl 2-thienyl 1.268 1,2- (CH3) 2_3-C2H502C-4-pyrrolyl 3-thienyl 1.269 1,2- (CH3) 2-3-C2H502C-4-pyrrolyl 2-Dttazinyl 1.270 1,2- (CH3) 2-3-C2H502C-4-pyrrolidinyl 2-titrinyl 1.271 1,2- (CH3) 2_3- 2-Houkounanji 1.272 1,2- (CH3) 2-3 -C2H502C-4-pyrrolidinyl 4-CH3- pupilphen-2-yl 1.273 1,2- (CH3) 2-3-C2H502C-4-pyrrolidinyl 4- Cl-thien-2-yl 65 200305556 1.274 1,2 -(CH3) 2 * ~ 3-C2H5〇2C-4_Dtt Rockyl 3-CH8 phen-2-yl 1.275 1,2- (CH3) 2-3-C2H502C-4-pyrrolylbenzophenone 1.276 1,2- (CH3) 2-3-C2H502C-4-pyrrolyl 3-C1 -benzobenzophen-2-yl 1.277 1,2- (CH3) 2-3-C2H502C_4_pyrrolyl 3-yl 1.278 1,2_ (CH3) 2-3-C2H502C-4-pyrrolylquinyl-4-yl 1.279 1,2- (CH3) 2-3_C2H502C_4_fluorene ratio 11 each group 7-CF3 -_- 3-yl 1.280 1, l-CHr3-CF3-pyrazol-5-yl 1.281 1,2- (CH3) 2-3-C2H502C-4-pyrrolidinyl 1-013-445_pyrrole-3-yl 1.282 1, 2- (CH3) 2-3-C2H502C_4-fluorene ratio p each group 5-C1-2-thienyl 1.283 1,2- (CH3) 2-3-C2H502C-4_pyrrolyl 5-CH3-2-Di phen 1.284 1,2- (CH3) 2-3-C2H502C-4-pyrrolidinyl 5-α-3- _ Phenyl 1.285 1,2- (CH3) 2-3-C2H502C_4-Pyrrolyl 5-CH3-3__ Phenyl 1.286 1,2- (CH3) 2-3-C2H502C-4-Pyrrolyl 1 -CH3-3- CF3-4-C1 -pyrazol-5-yl 1.287 1,2- (CH3) 2-3-C2H502C-4-pyrrolyl l-CH3-3-C6Hr4-C Propyrazol-5-yl 1.288 1, 2_ (CH3) 2_3-C2H5〇2C-4-D ratio 13 each group 5-N02-2-furyl 1.289 1,2- (CH3) 2-3-C2H502C-4-pyrrolidinyl 5-013-2- South base 1.290 1,2- (CH3) 2-3-C2H502C-4-pyrrolidinyl 3-fluorenyl-1-yl 1.291 1,2- (CH3) 2-3-C2H5〇2C-4-fluorene [; Bu Geji 2-CH3-3-furyl 1.292 6-C2H50-benzothien-3-yl 2-benzofuranyl 1.293 6-C2H50-benzo_phen-3-yl 2-thienyl 1.294 6-C2H50-benzo Thien-3-yl 3-_phenyl 1.295 6-C2H50-benzothien-3-yl 2-[] pyrazinyl 1.296 6-C2H50-benzophenphen-3-yl 2-oxenyl 1.297 6- C2H50-benzothiophen-3-yl 2-enantiomer sulphuryl 66 200305556 1.298 6-C2H50-benzothiophen-3-yl 1.299 6-C2H50-benzothiophen-3-yl 1.300 6-C2H50-benzothiophene- 3-yl 1.301 6-C2H50-benzothiophen-3-yl 1.302 6-C2H50-benzothiophen-3-yl 1.303 6-C2H50 0-benzothiophen-3-yl 1.304 6-C2H50-benzothiophen-3 -Base 1 .305 6-C2H50-benzo_phen-3-yl 1.306 6-C2H50-benzothiophen-3-yl 1.307 6-C2H50-benzothiophen-3-yl 1.308 6-C2H50-benzothiophen-3-yl 1.309 6-C2H50-benzothiophen-3-yl 1.310 6-C2H50 0-benzothiophen-3-yl 1. 311 6-C2H50-benzothiophen-3-yl 1.312 6-C2H50-benzothiophen-3- 1.313 6-C2H50-benzothiophen-3-yl 1.314 6-C2H50-benzo-phen-3-yl 1.315 6-C2H50-benzothiophen-3-yl 1.316 6-C2H50-benzothiophen-3-yl 1.317 6-C2H50-benzothiophen-3-yl 1. 318 2-CH302C-4 * ~ Br-3- pupillyl 1.319 2-CH302C-4-Br-3-thienyl 1.320 2-CH302C-4-Br + Thienyl 1.321 2-CHAC-4-Br-3-thienyl 4-CH3- pupilphen-2-yl 4- α-thien-2-yl 3-C-thienyl-2-ylbenzothien-2-yl 3-C1 -benzobenzophen-2-ylsulfonyl-3-ylsulfonyl-4-yl7-CF3-quinop-3-yl1-CH3-3-CF3-pyrazol-5-yl1- CH3-4-CF3-J [; Bu_3-yl 5-C1-2-thienyl 5-CH3-2-_phenyl 5-C1-3-thienyl 5-CH3-3-thienyl 1- CH3-3-CF3-4-Π-pyrazol-5-yl 1-CHr3-C6H5-4-C Pubizol-5-yl 5-N02-2-furyl 5-CH3-2- 咲 ° South 3-fluoranyl 2-CH, "3-furyl 2-benzofuranyl 2-thiophene 3-thienyl 2-0

67 200305556 1.322 2-CH302C-4_Br-3-噻吩基 1.323 2-CH302C-4-Br-3-噻吩基 1.324 2-CH302C-4-Bi-3-噻吩基 1.325 2-CH302C-4HBr-3-噻吩基 1.326 2-CH302C-4-Br+噻吩基 1.327 2-CH302C-4-Br-3-噻吩基 1.328 2-CH302C-4-Br-3-噻吩基 1.329 2-CH302C-4-Br-3_噻吩基 1.330 2-CH302C-4-Br-3-_吩基 1.331 2-CH302C-4-Br-3-_ 吩基 1.332 2-CH302C-4-Br-3-噻吩基 1.333 CH302C-4-Br-3-lS吩基 1.334 2_CH302C-4HBr-3-噻吩基 1.335 2-CH302C-4-Br-3-噻吩基 1.336 2-CH302C-4-Br-3_噻吩基 1.33Y 2-CH302C_4-Br-3-噻吩基 1.338 2-CH302C-4-Br-3-噻吩基 1.339 2-CH302C-4-Br-3-噻吩基 1.340 2-CHAC-4-Br-3-_吩基 1.341 2-CH302C_4-Br-3-噻吩基 1.342 2-CH302C-4-Br-3-噻吩基 1.343 2-CH302C+Br-3-噻吩基 1.344 2-CH302C-3-噻吩基 1.345 2-CH302C-3-Di吩基 2-嗤咐基 2- 呋喃基 4 - CH3-噻吩-2-基 4- α-噻吩-2-基 3- C1 -瞎吩-2-基 苯並瞎吩-2-基 3-C1 -苯並瞎吩-2-基 嗤咐-3-基 喹啉-4-基 7 - CF3-嗤咐-3-基 卜 CH3-3-CF3-毗唑-5-基 1 -CH3-4-CF3_|]比p各 _3-基 5- C1 - 2-噻吩基 5-CH3-2-噻吩基 5-Cl-3_噻吩基 5 - CH3-3-_ 吩基 1 - CH3-3-CF3-4-C卜毗唑-5-基 1- CH3-3-C6H5-4-Cl-毗唑 _5-基 5 - N02-2_呋喃基 5-CH3-2-呋喃基 3-咲17南基 2- CH3-3_呋喃基 2 -苯並咲n南基 2-_吩基67 200305556 1.322 2-CH302C-4_Br-3-thienyl 1.323 2-CH302C-4-Br-3-thienyl 1.324 2-CH302C-4-Bi-3-thienyl 1.325 2-CH302C-4HBr-3-thienyl 1.326 2-CH302C-4-Br + thienyl 1.327 2-CH302C-4-Br-3-thienyl 1.328 2-CH302C-4-Br-3-thienyl 1.329 2-CH302C-4-Br-3_thienyl 1.330 2-CH302C-4-Br-3-_phenyl 1.331 2-CH302C-4-Br-3-_ phenyl 1.332 2-CH302C-4-Br-3-thienyl 1.333 CH302C-4-Br-3-lS Phenyl 1.334 2_CH302C-4HBr-3-thienyl 1.335 2-CH302C-4-Br-3-thienyl 1.336 2-CH302C-4-Br-3_thienyl 1.33Y 2-CH302C_4-Br-3-thienyl 1.338 2-CH302C-4-Br-3-thienyl 1.339 2-CH302C-4-Br-3-thienyl 1.340 2-CHAC-4-Br-3-_phenyl 1.341 2-CH302C_4-Br-3-thienyl 1.342 2-CH302C-4-Br-3-thienyl 1.343 2-CH302C + Br-3-thienyl 1.344 2-CH302C-3-thienyl 1.345 2-CH302C-3-Diphenyl 2-sulfonyl 2- Furyl 4-CH3-thien-2-yl 4- α-thien-2-yl 3- C1 -benzophen-2-ylbenzobenzo-2-yl 3-C1 -benzobenzophen-2-yl -3--3-ylquinolin-4-yl 7-CF3- -3--3-ylbu CH3-3-CF3-pyrazol-5-yl 1 -CH3-4-CF3_ |] than p each _3- Base 5- C1-2- Phenyl 5-CH3-2-thienyl 5-Cl-3_thienyl 5-CH3-3-_ Phenyl 1-CH3-3-CF3-4-C Pipizol-5-yl 1-CH3-3 -C6H5-4-Cl-pyrazol-5-yl 5-N02-2_furanyl 5-CH3-2-furanyl 3-fluorenyl 17 sulfanyl 2- CH3-3_furanyl 2 -benzopyridinium 2-phenoyl

68 200305556 1.346 2-CH302C_3-噻吩基 1.347 2-CH302C-3-噻吩基 1.348 2-CH302C-3-噻吩基 1.349 2-CH302C-3-lS吩基 1.350 2-CH302C-3-噻吩基 1.351 2-CH302C-3-噻吩基 1.352 2-CH302C-3-_吩基 1.353 CH302C-3-噻吩基 1.354 2-CH302C-3-噻吩基 1.355 2-CH302C-3H*吩基 1.356 2-CH302C-3-噻吩基 1.357 2-CH302C-3-噻吩基 1.358 2-CH302C-3-噻吩基 1.359 2-CH302C-3-噻吩基 1.360 2-CH302O3-_吩基 1.361 2-CH302C-3-Di 吩基 1.362 2-CH302C-3-噻吩基 1.363 2-CH302C-3-噻吩基 1.364 2-CH302C-3-噻吩基 1.365 2-CH302C_3-噻吩基 1.36Θ 2-CH302C-3-噻吩基 1.367 2-CH302C-3-Di吩基 1.368 2-CH302C-3-_吩基 1.369 2-CH302C-3-噻吩基 1.370 2-CN-苯並噻吩-3-基 3- _吩基 2-D比嗪基 2-喹啉基 2- 呋口南基 4- CH3-噻吩-2-基 4- CH® 吩-2-基 吩-2-基 苯並_吩-2-基 3- C1 -苯並瞎吩_2-基 唾林-3_基 嗤咐-4-基 7-CF3-喹啉-3-基 1 - CH3-3-CF3-吡唑-5-基 1 _CH3-4-CF3-Q 比ϋ各 _3-基 5- C1-2-瞳吩基 5-CH3-2-噻吩基 5-C1-3-噻吩基 5-CH3_3-噻吩基 l-CH3-3-CF3-4-C1-吡唑-5-基 1- CH3_3-C6H5-4-a-吡唑-5-基 5 - NO「2-呋喃基 5-CH3_2_咲喃基 3-呋喃基 2- CH3-3_呋喃基 2-苯並呋喃基68 200305556 1.346 2-CH302C_3-thienyl 1.347 2-CH302C-3-thienyl 1.348 2-CH302C-3-thienyl 1.349 2-CH302C-3-lSphenyl 1.350 2-CH302C-3-thienyl 1.351 2-CH302C 3-thienyl 1.352 2-CH302C-3-_phenyl 1.353 CH302C-3-thienyl 1.354 2-CH302C-3-thienyl 1.355 2-CH302C-3H * phenyl 1.356 2-CH302C-3-thienyl 1.357 2-CH302C-3-thienyl 1.358 2-CH302C-3-thienyl 1.359 2-CH302C-3-thienyl 1.360 2-CH302O3-_phenyl 1.361 2-CH302C-3-Di phenyl 1.362 2-CH302C-3 -Thienyl 1.363 2-CH302C-3-thienyl 1.364 2-CH302C-3-thienyl 1.365 2-CH302C_3-thienyl 1.36Θ 2-CH302C-3-thienyl 1.367 2-CH302C-3-Diphenyl 1.368 2 -CH302C-3-_phenyl 1.369 2-CH302C-3-thienyl 1.370 2-CN-benzothien-3-yl 3-_phenyl 2-D bisazinyl 2-quinolinyl 2-furonan 4-CH3-thien-2-yl 4-CH®phen-2-ylphen-2-ylbenzo-phen-2-yl 3-C1 -benzobenzophen-2-ylsulfalin-3-yl Command 4-yl 7-CF3-quinolin-3-yl 1-CH3-3-CF3-pyrazol-5-yl 1 _CH3-4-CF3-Q ratio -Pidophenyl 5-CH3-2-thienyl 5-C1-3-thienyl 5-CH3_3-thienyl 1-CH 3-3-CF3-4-C1-pyrazol-5-yl 1-CH3_3-C6H5-4-a-pyrazol-5-yl 5-NO, "2-furyl 5-CH3_2-pyranyl 3-furan 2-CH3-3_furanyl 2-benzofuranyl

69 200305556 1.371 2-CN-苯並噻吩-3-基 1.372 2-CN-苯並噻吩-3-基 1.373 2-CN-苯並噻吩-3-基 1.374 2-CN-苯並噻吩-3-基 1.375 2-CN-苯並噻吩-3-基 1.376 2-CN-苯並噻吩-3-基 1.377 2-CN-苯並噻吩-3-基 1.378 2-CN-苯並噻吩-3-基 1.379 2-CN-苯並噻吩-3-基 1.380 2-CN-苯並噻吩-3-基 1.381 2-CN-苯並噻吩-3-基 1.382 2-CN-苯並_吩-3-基 1.383 2-CN-苯並_吩-3-基 1.384 2-CN-苯並噻吩-3-基 1.385 2-CN-苯並噻吩-3-基 1.386 2-CN-苯並噻吩-3-基 1.387 2-CN-苯並噻吩-3-基 1.388 2-CN-苯並噻吩-3-基 1.389 2-CN-苯並_吩-3-基 1.390 2-CN-苯並噻吩-3-基 1.391 2-CN-苯並噻吩-3-基 1.392 2-CN-苯並噬吩-3-基 1.393 2-CN-苯並_吩-3-基 1.394 2-CN-苯並噻吩-3-基 1.395 2-CN-苯並噻吩_3-基 2- 噻吩基 3- 瞎吩基 2-Dtt嗪基 2-喹啉基 2- 咲口南基 4 - cv_ 吩-2-基 4- C1 -瞎吩-2-基 3- (：1-噻吩-2-基 苯並噻吩-2-基 3-C1-苯並_吩-2-基 嗤咐-3-基 唾林-4-基 7-CF3-嗤琳-3-基 1 - CH3-3-CF3_ 毗唑-5-基 l-CH3-4-CF3_D 比p各 _3-基 5 - C1-2-噻吩基 5- CHr2-_ 吩基 5-C1-3-噻吩基 5-CH3-3-噻吩基 l-CHr3-CF3-4-C 卜吡唑-5-基 1- CH3-3_C6Hr4-a-毗唑-5-基 5 - Ν〇2-2-咲11南基 5-CH3-2-咲喃基 3-呋喃基 2- CH3-3_呋喃基69 200305556 1.371 2-CN-benzothiophen-3-yl 1.372 2-CN-benzothiophen-3-yl 1.373 2-CN-benzothiophen-3-yl 1.374 2-CN-benzothiophen-3-yl 1.375 2-CN-benzothiophen-3-yl 1.376 2-CN-benzothiophen-3-yl 1.377 2-CN-benzothiophen-3-yl 1.378 2-CN-benzothiophen-3-yl 1.379 2 -CN-benzothiophen-3-yl 1.380 2-CN-benzothiophen-3-yl 1.381 2-CN-benzothiophen-3-yl 1.382 2-CN-benzo_phen-3-yl 1.383 2- CN-benzo_phen-3-yl 1.384 2-CN-benzothiophen-3-yl 1.385 2-CN-benzothiophen-3-yl 1.386 2-CN-benzothiophen-3-yl 1.387 2-CN -Benzothiophen-3-yl 1.388 2-CN-benzothiophen-3-yl 1.389 2-CN-benzo_phen-3-yl 1.390 2-CN-benzothiophen-3-yl 1.391 2-CN- Benzothiophen-3-yl 1.392 2-CN-benzophenphen-3-yl 1.393 2-CN-benzo_phen-3-yl 1.394 2-CN-benzothiophen-3-yl 1.395 2-CN- Benzothiophene 3-yl 2-thienyl 3-benzophenyl 2-Dttazinyl 2-quinolinyl 2- pinanyl 4-cv_phen-2-yl 4- C1 -benzophen-2-yl 3- (: 1-thien-2-ylbenzothien-2-yl 3-C1-benzo_phen-2-yl -Yl 1-CH3-3-CF3_ pyrazol-5-yl l-CH3 -4-CF3_D than p_3-yl 5-C1-2-thienyl 5- CHr2-_phenyl 5-C1-3-thienyl 5-CH3-3-thienyl 1-CHr3-CF3-4- C Propyrazol-5-yl 1-CH3-3_C6Hr4-a-pyrazol-5-yl 5-NO 2-2-fluorenyl 11 Southern 5-CH3-2-fluoranyl 3-furyl 2-CH3 -3_furanyl

70 200305556 生物學實施例：70 200305556 Biological examples:

將六至八週大的蒙古沙鼠，各自以人工餵食各大約 2_個三齡期的蛇形毛線蟲及扭旋血線蟲之幼蟲而感染。 感染之後6天，將沙鼠以N20輕微地麻醉，並以1〇〇、32 及10-0· 1毫克/公斤的量經σ施用測試化合物而治療，該 測試化合物是溶解於2份二甲基亞》及1份聚乙二醇（PEG 300 )的混合物中。在第9天（治療後3天），當大部分仍 存在的扭旋血線蟲幼蟲是晚四齡期以及大部分的蛇形毛線 蟲疋未成熟的成蟲時，將沙鼠殺死以計數蠕蟲。功效是以 在母隻沙鼠中’蠕蟲數目的減少百分比而計算，相較於8 隻感染及未治療的沙鼠之蠕蟲的幾何平均數。 在這個測，式中’ 4 I之化合物可大幅減少線蟲的寄生 侵擾。因此，扭旋血線蟲的寄生侵擾可藉由表丨中的化合 物1 · 2 7及1 · 5 3而明顯減少。 可使用以下的試驗方法，以研究式j化合物對於動物 及植物之殺昆蟲及/或殺療蟲的作用。 的丄幼盔之 作用： ~ 將1 升要測試的活性物質之水溶性懸浮液，與3毫 升的特疋幼蟲生長培養液，在大約5〇c>c下混合，以便形成 71 200305556 八有250或125 ppm活性成份含量的均質物。將大約3〇個 絲光綠蠅幼蟲（< τ、道λ s 7 虫I h)導入至母個試管樣品中。4天之後測 定死亡率。 、丄牛蜱（如即/?""/； ygkmpyt/g1 ; Biarra 品 盖）之殺砰·Αϋ用： 將一片膠帶水平地貼到聚氣乙烯（pvc)薄板，使得 〇又70王允足血的微小牛蜱（Biarra品系）之雌壁蝨，可 起排地黏到其背面。使用注射針，將1微升的液體注 射到每隻壁蝨’該液體是聚乙二醇及丙酮的1 : 1混合物， =及其中係溶解可選擇的1、〇·1或0.01微克/壁蝨之特定 里的活性成份。對照組動物接受不含活性成份的注射。在 治療之後，將動物在正常條件下，保持在大約28t以及8〇 ^相對屋度的昆蟲館中，直到產卵以及幼蟲已從對照組動 物的卵中孵化為止。測試物質的活性是藉纟％。而測定， 也就是，評估10隻雌壁蝨中的9隻（=90%)產卵在3〇 天之後仍不能孵化的活性成份之劑量。Mongolian gerbils, six to eight weeks old, were each manually infected with about two to three instar larvae of Trichinella spiralis and Haemophilus contortus. Six days after the infection, the gerbils were lightly anesthetized with N20 and treated with sigma administration test compounds at 100, 32, and 10-0 · 1 mg / kg, which test compounds were dissolved in 2 portions of dimethyl ether Gia and 1 part of polyethylene glycol (PEG 300). On the 9th day (3 days after treatment), when most of the surviving Haemophilus larvae are late fourth instars and most of the immature adults of the serpentine worm are killed, the gerbils are killed to count the worm insect. Efficacy was calculated as a percentage reduction in the number of worms in female gerbils, compared to the geometric mean of worms in 8 infected and untreated gerbils. In this test, the compound of '4 I in the formula can greatly reduce the parasitic infestation of nematodes. Therefore, the parasitic infestation of H. contortus can be significantly reduced by the compounds 1 · 2 7 and 1 · 5 3 in the table. The following test methods can be used to investigate the insecticidal and / or insecticidal effects of compounds of formula j on animals and plants. The role of the pupa helmet: ~ 1 liter of a water-soluble suspension of the active substance to be tested is mixed with 3 ml of the special pupa larva growth culture solution at about 50c > c to form 71 200305556 Bayou 250 Or a homogeneous content of 125 ppm active ingredient. Approximately 30 larvae of Cercospora cirrhosa (< τ, λ s 7 worm I h) were introduced into female test tube samples. Mortality was measured after 4 days. 2. The killing of yak ticks (such as /? &Quot; "/; ygkmpyt / g1; Biarra cover) · Aϋ Application: Apply a piece of tape horizontally to a sheet of polyvinyl chloride (PVC) sheet, so that 70 and 70 kings allow Female ticks of the bloody bovine tick (Biarra strain) can stick to the back in rows. Use an injection needle to inject 1 microliter of liquid into each tick. The liquid is a 1: 1 mixture of polyethylene glycol and acetone, and its medium can be dissolved by 1, 0.1 or 0.01 micrograms per tick. Specific active ingredients. Control animals received injections without active ingredients. After the treatment, the animals were kept under normal conditions in an insect house of approximately 28 t and a relative house of 80 直到 until the eggs were laid and the larvae had hatched from the eggs of the control animals. The activity of the test substance is in%. And the determination, that is, the evaluation of the dose of the active ingredient in which 9 of the 10 female ticks (= 90%) were unable to hatch after 30 days.

外活姓： 將4 X 1〇隻0P-抗性的BIARRA品系之吮足血的雌壁 兹黏到膠帶，並以分別浸泡在濃度500、125、31以及8 PPm的測試化合物乳液或懸浮液中之棉紗球而覆蓋^小時 。評估28天之後的死亡率、產卵以及孵化的幼蟲。 測試化合物的活性之指標，是以具有下列特徵的雌壁 蝨之數目而顯示： 72 200305556 一產卵前迅速死亡； -存活一段時間，但沒有產卵； -產出其中沒有形成胚胎的卵； 一產出形成胚胎、但沒有孵化出幼蟲的卵；以及 產出形成胚胎、幼蟲在2 6到2 7天内正常赙化的印 〇 ^~~蟹Jt希伯來花蜱（Ambivonma hebraeum、％蝻之活 體外活姓： 將大約5隻飢餓的蛹置於包括2毫升測試化合物溶於 溶液、懸浮液或乳液的聚苯乙烯試管中。 在次泡1 〇分鐘並在旋渴混合|§中搖晃2 X 1 q秒之後 ，將試管以厚脫脂棉團塞住並且倒立。當所有的液體已被 脫脂棉團吸收後，就將脫脂棉團推到仍倒立的試管中間， 使得大部分的液體擠出脫脂棉團，並流向底下的培養皿。 然後在周圍溫度下，將試管儲存在光照的房間，直到 進行評估為止。14天之後，將試管浸泡在沸水的燒杯中。 如果壁歲開始對熱反應而移動的話，則該測試濃度的測試 物質是無作用的，否則將壁蝨視為死亡，並且在該測試濃 度的測試物質是視為活性的。將所有的物質都在〇·丨到 1 〇〇 ppm的濃度範圍進行測試。 ^~~iAJI 兹(Dermanvssus ^al 1 . 將2到3毫升包含l〇 ppm活性成份的溶液，以及大約 2〇〇隻不同發育階段的兹子（雞幻，加到頂端開口的玻 璃容器中。接著將容器以脫脂棉團塞住，搖晃ι〇分鐘直到 73 200305556 蝨子完全渔潤為止，然後短暫地倒立，使得剩下的測試溶 液可由脫脂棉所吸收。3天之後，藉由計數死亡的個體而 測定蝨子的死亡率，並且以百分比表示。 L_對益家蠅（Joyces以〜）之作用·· 將方糖以測試物質的溶液處理，使得乾燥隔夜後，測 試物質在蔗糖中的濃度是250 ppm。將以此方式處理之方 糖’置於含有座脫脂棉團以及1 〇隻〇p—抗性品系的家繩成 蟲之銘盤上，以燒杯覆蓋，並且在25C培養。24小時之後 測定死亡率。Outer surname: 4 x 10 OPP-resistant BIARRA strains of the blood-sucking female wall are glued to the tape and immersed in test compound emulsions or suspensions at concentrations of 500, 125, 31, and 8 PPm, respectively Covered with cotton yarn for ^ hours. Assess mortality, spawning, and hatched larvae after 28 days. An indicator of the activity of the test compound is shown by the number of female ticks having the following characteristics: 72 200305556 One died immediately before laying eggs;-survived for a while but did not lay eggs;-produced eggs in which embryos were not formed;- Produce eggs that form embryos, but do not hatch larvae; and produce seals that form embryos and larvae that normally pupate within 26 to 27 days. ^^ ~ Crab Jt Hebrew flower ticks (Ambivonma hebraeum,% 蝻 之) Living names in vitro: Approximately 5 hungry salamanders were placed in polystyrene test tubes containing 2 ml of the test compound dissolved in a solution, suspension or emulsion. Soak for 10 minutes in the subsoak and shake in a thirst mixing | § 2 After X 1 q seconds, plug the test tube with a thick absorbent cotton ball and stand upside down. When all the liquid has been absorbed by the absorbent cotton ball, push the absorbent cotton ball to the middle of the test tube that is still upside down, so that most of the liquid is squeezed out of the absorbent cotton ball. It flows down to the petri dish below. Then the test tube is stored at ambient temperature in a lighted room until evaluation. After 14 days, the test tube is immersed in a beaker of boiling water. If the wall is old If it starts to move in response to heat, the test substance at the test concentration will have no effect, otherwise the tick will be regarded as dead, and the test substance at the test concentration will be regarded as active. All substances are in the range of 〇 · 丨Test to a concentration range of 100 ppm. ^ ~~ iAJI (Dermanvssus ^ al 1. 2 to 3 ml of a solution containing 10 ppm active ingredient, and about 200 different stages of development (chicken Put it in a glass container with an open top. Then plug the container with a cotton pad and shake it for 73 minutes until the lice are completely fished, and then stand upside down briefly so that the remaining test solution can be absorbed by the cotton pad. 3 After a few days, the mortality of lice was determined by counting dead individuals, and expressed as a percentage. L_Effects on housefly (Joyces ~) · The cube sugar was treated with a solution of the test substance to dry overnight The concentration of the test substance in sucrose was 250 ppm. The sugar cubes treated in this way were placed on the house cord adult worms containing absorbent cotton swabs and 10 oop-resistant strains. On to a covered beaker, and the mortality was measured after culturing 25C .24 hr.

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Claims (1)

200305556 拾、申請專利範圍：200305556 Scope of patent application: 一種式I化合物，A compound of formula I, 〇 (严-W—(产 R4 Re "Ar, 其中 Ar〗及Arz互相獨立地是未經取代的或經單-或多取代 的方基’其中人:^及Αι*2的取代基互相獨立地係選擇自由齒 素、硝基、氰基、OH、SH、CrCe烷基、鹵素—烷基、 (VC6烷氧基、鹵素-(：丨-(：6烷氧基、C2-ce烯基、鹵素—C2-C6 烯基、（VQ炔基、Cs-C6環烷基、C2-C6烯氧基、鹵素—C2— C6烯氧基、C^-C6烧硫基、鹵素—(^-C；6烧硫基、烧基石黃 醯氧基、鹵素-q-C6烷基磺醯氧基、Ci—Ce烷基亞磺醯基、 鹵素-CrG烷基亞磺醯基、Cl—C6烷基磺醯基、鹵素一 烷基磺醯基、q-C6烯硫基、鹵素-c：2—Ce烯硫基、C2—&烯基 亞磺醯基、鹵素-CfC6烯基亞磺醯基、〇2—&烯基磺醯基、 鹵素-CrC6烯基磺醯基、CrC：6烷胺基、二一Ci — C6烷胺基、 Ci-C6烷基磺醯胺基、鹵素-CrC6烷基磺醯胺基、Ci-Ce烷基 羰基、鹵素-CrC6烷基羰基、c!-C6烷氧基羰基、Ci —Ce烷基 胺基羰基及二-Ci-Ce烷基胺基羰基所組成的族群中；未經 取代的或經單-或多取代的苯基胺基；未經取代的或經單一 或多取代的苯基羰基；未經取代的或經單—或多取代的笨 基，其中取代基可以是互相獨立，並且選擇自由_素、= 75 200305556 基、氰基、C—广C6烷基、齒素—Ci_c6烷基、Ci_C6烷氧基、齒· 素Ci Ce烷氧基、Ci — C6烷硫基、鹵素一C「C6烷硫基、 烷基亞磺醯基、齒素—Ci-C6烷基亞磺醯基、Cl—c6烷基磺醯 基及鹵素-CrC6烷基磺醯基所組成的族群中；未經取代的 或經單-或多取代的苯氧基，其中取代基可以是互相獨立 ，並且選擇自由鹵素、辅基、氰基、C「c6烧基、_素〜Ci— c6烷基、（VC6烷氧基、鹵素-Ci—h烷氧基、Ci_Ce烷硫基^ i素-CrC6烷硫基、Cl_(；6烷基亞磺醯基、鹵素—Ci—C6烷基 亞磺醯基、乂广C6烷基磺醯基及函素-Ci-C6烷基磺醯基所組 鲁 成的族群中；未經取代的或經單—或多取代的苯基乙炔基 ’其中取代基可以是互相獨立，並且選擇自由鹵素、確基 、氰基、（Vc：6烷基、鹵素-(：广(：6烷基、CrC6烷氧基、鹵素 一CrC6烧氧基、Ci-C6烷硫基、鹵素-CrC：6烷硫基、Crc6燒 基亞％醯基、鹵素-CrC6烧基亞續醯基、〇厂(；6烧基續醯基 及鹵素-CrC；6烧基石黃醢基所組成的族群中；以及未經取代 的或經單-或多取代的吡啶氧基，其中取代基可以是互相獨 立，並且選擇自由_素、硝基、氰基、Cl_C6烷基、齒素_ 籲 Ci C6烧基、C^-C6烧乳基、鹵素-Ci - C6烧氧基、Ci-Cg燒硫 基、鹵素-CrCe烧硫基、C「C6燒基亞續醯基、_素一Ci一c 烧基亞績醯基、CrC6烧基續醯基及鹵素-烧基續醯基 所組成的族群中；或 藉由環碳原子而鍵結之未經取代的或經單—或多取代的 雜芳基，其中Ar!及A]：2的取代基可以是互相獨立，並且選 擇自由鹵素、硝基、氣基、C；[-Ce烧基、鹵素烧基、 76 200305556 (：厂(：6烷氧基、鹵素-Crh烷氧基、C2-C6烯氧基、鹵素一c2— Ce烯氧基、Ci-Ce烷硫基、鹵素-c〗-C6烷硫基、（：厂c6烷基亞 磺醯基、鹵素-CrCs烷基亞磺醯基、c2-C6烯硫基、齒素一 Cz-C6稀硫基、CrC6烯基亞續醯基、鹵素-c2-C6烯基亞續醯 基、Ci-Ce烷基磺醯基、鹵素-Ci—Ce烷基磺醯基、c厂c6烯基 磺醢基、鹵素-C2-C6烯基磺醯基、CrC6烷胺基及二-Ci-C6 烧胺基所組成的族群中； Ri疋氫、烧基、鹵素烧基、烯丙基或 ^ 1 ^6 烷氧基甲基； ^h1及Κβ互相獨立地是氫、ώ素、未經取 代的或經單-或多取代的Cl-(：6烷基、未經取代的或經單一 或多取代的C2-C6烯基、未經取代的或經單—或多取代的 C2-C6炔基、未經取代的或經單—或多取代的氧基， 其中在每個例子中的取代基可以是互相獨立，並且選擇自 由齒素、CrC6烷氧基及鹵素-Cl-C6烷氧基所組成的族群中 ’未經取代的或經單-或多取代的C3-c6環烷基，其中取代 基可以是互相獨立，並且選擇自由_素及Cl-c6烷氧基所 組成的族群中；或未經取代的或經單—或多取代的苯基， 其中取代基可以是互相獨立，並且選擇自由鹵素、硝基、 亂基、CrC6烷基、鹵素_Ci_C6烷基、Ci—Ce烷氧基、_素一 Ci 一 烧氧基、Cl-C6烧硫基、鹵素烧硫基、（VC6烷 基亞磺醯基、鹵素-C「C6烷基亞磺醯基、CrG烷基磺醯基 、齒素—crCe烷基磺醯基、Ci_C6烷胺基及二—Ci_Ce烷胺基 所組成的族群中； 77 或^及R3 一起是C3-C5伸燒基； w 是 0、s、s(〇2)或 n(r7); 尺7疋氫或（^-(:6烷基； a是1、2、3或4 ;以及 b是0、卜2、3或4 ; 其限制條件為Ari及紅2中至少_個 一個限制條件為A ”方土，以及， m… 同時是毗啶基；如果W 本基的活，Ari不是毗啶基；以〇 (严 -W— (producing R4 Re " Ar, where Ar〗 and Arz are independently unsubstituted or mono- or poly-substituted square groups' wherein: ^ and Al * 2's substituents each other Independently select free tooth element, nitro, cyano, OH, SH, CrCe alkyl, halogen-alkyl, (VC6 alkoxy, halogen- (: 丨-(: 6 alkoxy, C2-ceene) Group, halogen—C2-C6 alkenyl, (VQ alkynyl, Cs-C6 cycloalkyl, C2-C6 alkenyloxy, halogen—C2—C6 alkenyloxy, C ^ -C6 sulfanyl, halogen — (^ -C; 6-sulfanyl group, sulfanyl sulfoxanthryloxy group, halogen-q-C6 alkylsulfonylfluorenyloxy group, Ci-Ce alkylsulfinylfluorenyl group, halogen-CrG alkylsulfinylfluorenyl group, Cl-C6 Alkylsulfonyl, halo-alkylsulfonyl, q-C6 alkenylthio, halo-c: 2-Ce alkenylthio, C2—alkenylsulfinyl, halo-CfC6 alkenylsulfinyl Fluorenyl, 02- & alkenylsulfonyl, halogen-CrC6 alkenylsulfonyl, CrC: 6 alkylamino, di-Ci-C6 alkylamino, Ci-C6 alkylsulfonamido, halogen -CrC6 alkylsulfonamido, Ci-Ce alkylcarbonyl, halogen-CrC6 alkylcarbonyl, c! -C6 alkoxycarbonyl, Ci-Ce alkylamino Carbonyl groups and di-Ci-Ce alkylaminocarbonyl groups; unsubstituted or mono- or poly-substituted phenylamino groups; unsubstituted or mono- or poly-substituted phenylcarbonyl groups; Unsubstituted or mono- or poly-substituted benzyl, wherein the substituents may be independent of each other, and the choice is free_prime, = 75 200305556, cyano, C-wide C6 alkyl, halo-Ci_c6 alkyl , Ci_C6 alkoxy group, Ci Ce alkoxy group, Ci-C6 alkylthio group, halogen-C6 alkylthio group, alkylsulfinyl sulfenyl group, dentin-Ci-C6 alkylsulfinyl sulfenyl group , Cl-c6 alkylsulfonyl and halogen-CrC6 alkylsulfonyl groups; unsubstituted or mono- or poly-substituted phenoxy groups, where the substituents may be independent of each other and selected Free halogen, prosthetic group, cyano group, C, C6 alkyl group, C-C6 alkyl group, (VC6 alkoxy group, halogen-Ci-h alkoxy group, Ci_Ce alkylthio group, i-Ce-CrC6 alkylthio group Group consisting of sulfonyl group, Cl_ (; 6 alkylsulfinyl sulfenyl group, halogen-Ci-C6 alkyl sulfinyl sulfonyl group, fluorinated C6 alkyl sulfinyl sulfonyl group and halo-Ci-C6 alkyl sulfinyl sulfonyl group Ethnic group Substituted or mono- or poly-substituted phenylethynyl 'wherein the substituents may be independent of each other, and free halogen, acyl, cyano, (Vc: 6 alkyl, halogen- (: Radical, CrC6 alkoxy, halogen-CrC6 alkyloxy, Ci-C6 alkylthio, halogen-CrC: 6 alkylthio, Crc6 alkylene fluorenyl, halogen-CrC6 alkylene sulfonyl, 〇plant (; 6-alkynyl and fluorenyl and halogen-CrC; 6-alkynyl stilbene group; and unsubstituted or mono- or poly-substituted pyridyloxy, wherein the substituents may be independent of each other, and is selected Free_prime, nitro, cyano, Cl_C6 alkyl, dentin_Ci C6 alkyl, C ^ -C6 alkyl, halogen-Ci-C6 alkyl, Ci-Cg sulfur, halogen-CrCe In the group consisting of thiol, C, C6, alkynyl, sulfo-Ci, alkynyl, CrC6, alkynyl, and halogen-alkyl; and An unsubstituted or mono- or poly-substituted heteroaryl group bonded to a ring carbon atom, wherein the substituents of Ar! And A]: 2 may be independent of each other, and may be selected from halogen, nitro, Group, C; [-Ce alkyl group, halogen alkyl group, 76 200305556 (: factory (: 6 alkoxy group, halogen-Crh alkoxy group, C2-C6 alkenyl group, halogen-c2-Ce alkenyl group, Ci -Ce alkylthio, halogen-c〗 -C6 alkylthio, (C6 alkylsulfinamilide, halogen-CrCs alkylsulfinylene, c2-C6 alkenylthio, halo-Cz-C6 Diluted thio, CrC6 alkenyl fluorenylene, halogen-c2-C6 alkenyl fluorenylene, Ci-Ce alkylsulfonyl, halogen-Ci-Ce alkylsulfonyl, c6 alkenyl sulfonyl In the group consisting of fluorenyl, halogen-C2-C6 alkenylsulfonyl, CrC6 alkylamino, and di-Ci-C6 alkylamino; Rifluorene hydrogen, alkyl, halogen alkyl, allyl, or ^ 1 ^ 6 alkoxymethyl; ^ h1 and κβ are independently hydrogen, free vegetarian, unsubstituted or mono- or poly-substituted Cl-(: 6 alkyl, unsubstituted or mono- or poly Substituted C2-C6 alkenyl, unsubstituted or mono- or poly-substituted C2-C6 alkynyl, unsubstituted or mono- or poly-substituted oxy, wherein the substituents in each example Can be independent of each other, and select free tooth element, CrC6 alkoxy and halogen-Cl-C6 alkoxy In the group consisting of 'unsubstituted or mono- or poly-substituted C3-c6 cycloalkyl groups, the substituents may be independent of each other, and selected from the group consisting of free radicals and Cl-c6 alkoxy groups; Or unsubstituted or mono- or poly-substituted phenyl, wherein the substituents may be independent of each other, and free halogen, nitro, alkynyl, CrC6 alkyl, halogen_Ci_C6 alkyl, Ci-Ce alkoxy Group, Ci-Ci-alkyloxy group, Cl-C6 alkylthio group, halogen alkylthio group, (VC6 alkylsulfinyl group, halogen-C, C6 alkylsulfinyl group, CrG alkylsulfinyl group , Halo-crCe alkylsulfonyl, Ci_C6 alkylamino and di-Ci_Ce alkylamino group; 77 or ^ and R3 together are C3-C5 elongation group; w is 0, s, s ( 〇2) or n (r7); 疋 7 疋 hydrogen or (^-(: 6 alkyl; a is 1, 2, 3 or 4; and b is 0, Bu 2, 3 or 4; the restriction is Ari And at least one of the red 2 conditions is A ”square earth, and, m ... is also a pyrimidinyl group; if the W radical is active, Ari is not a pyrimidinyl group; 不是I定基。 果An疋本基的话，Al 獨立地選擇自由_素、 C6烷基、CrC6烷氧基、 2.根據申請專利範圍第i項之式】化合物，在每個合 ’以游離的形式或以鹽類的形式存在，係具有包含身 前提供的限制條件，其中Απ及〜互相獨立地是未經㈣ 勺或丄單或夕取代的芳基’其中a及紅2的取代基互相 硝基、氰基、Crh烷基、鹵素-(:厂 鹵素一CrCe烷氧基、c3-c6環烷基、Not I-fixed. If An base is selected, Al independently selects free radicals, C6 alkyl, CrC6 alkoxy, 2. According to the formula of the scope of application for patent i] compounds, each compound is in a free form or in a salt It exists in the form of a class, which includes the restrictions provided in front of it, where Απ and ~ are independently aryl groups that are not substituted with ㈣ or 丄, or 夕, where the substituents of a and red 2 are nitro and cyano. Group, Crh alkyl, halogen- (: factory halogen-CrCe alkoxy, c3-c6 cycloalkyl, C】Ce烷基嶒醯基、鹵素—C1 —q烷基磺醯基、Ci—C6烷胺基、 二一C厂C6烷胺基、Crh烷基羰基、鹵素_c「Ce烷基羰基、 CfCe烷氧基羰基、c厂Ce烷基胺基羰基及二_C1—Q烷基胺基 羰基所組成的族群中；未經取代的或經單-或多取代的苯基 羰基，未經取代的或經單—或多取代的苯基，其中取代基可 以是互相獨立，並且選擇自由鹵素、硝基、氰基、Ci_C6烷 基、函素-CrC6烧基、CrC6烷氧基及鹵素-c!_c6烷氧基所 組成的族群中；未經取代的或經單-或多取代的苯氧基，其 中取代基可以是互相獨立，並且選擇自由鹵素、硝基、氰 78 200305556 基、（VC6烧基、齒素-Cl-C6烷基、Cl-C6烷氧基及齒素一^一 * Ce烷氧基所組成的族群中；以及未經取代的或經單-或多取 代的卩比淀氧基’其中取代基可以是互相獨立，並且選擇自 由鹵素、确基、氰基、CrC6烷基、函素一c「c6烷基、Ce 烧氧基及鹵素-CrC6烧氧基所組成的族群中；或 藉由環碳原子而鍵結之未經取代的或經單_或多取代的 雜芳基，其中人^及Aq的取代基可以是互相獨立，並且選 擇自由鹵素、頌基、氰基、Cl-C6烧基、齒素_Ci_c6烧基、 C「C4氧基、i素介(：6炫氧基、院基伽基、^ ♦ -Κ6烧基續醯基、Cl-C6烧胺基及二_Ci_Ce燒胺基所組成 的族群中。 3·根據申請專利範圍第丨項之式〗化合物，在每個 例子中，以游離的形式或以鹽類的形式存在，係具有包含 先前提供的限制條件，其中Arl& 互相獨立地是未經取 代的或經單-或多取代的芳基，其中ΑΓ1及ΑΓ2的取代基互 相獨立，係選擇自由鹵素、硝基、氰基、CrC6烧基、函素 -c】-c6烧基、Cl_c6^氧基、m_Ci_C6烷氧基、環烷鲁 基、Crh烷基羰基及鹵素—Ci-C6烷基羰基所組成的族群中 ;未經取代的或經單-或多取代的苯基羰基；未經取代的 或經單-或多取代的苯基，其中取代基可以是互相獨立， 並且選擇自由鹵素、氰基、CrC6烧基及函素—Κ6烧基所 組成的族群中；以及未經取代的或經單-或多取代的苯氧 基，其中取代基可以是互相獨立，並且選擇自由鹵素、氰 基、CrC6烷基及鹵素一烷基所組成的族群中；或 79 200305556 藉由環碳原子祕結之未經取代的或經單_或多取代的 雜芳基’其中Ari Ah的取代基可以是互相獨纟，並且選 擇=由函素、氰基？Ί齒素々c6院基、以院 氧土及_素-Ci-C6：^元乳基所組成的族群中。 4. 根據申請專利範圍第1項之式I化合物，在每個例 子中’以游離的形式或以鹽類的形式存在，係具有包 提供的限制條件，其中^及〜互相獨立地是未經取代的 或經單-或多取代的芳基，其中 T八“及Ar2的取代基互 ’係選擇自由函素、氮基、W㈣ J立 Cl-C4烧氧基、函素-Cl-C4院氧基、c3—c5環燒 C二其 幾糾素今c4編炭基所組成的族群中；未經取二： 經早-或多取代的苯基Μ基；以及未經取代的或經單—= 代的苯基’其中取代基可以是互相獨立，並且選擇 ： 、c「c4烷基及鹵素-以烷基所組成的族群中；A 素 藉由環碳原子而鍵結之未經取代的或經單一或 雜芳基’其中Arl及Ar2的取代基可以是互相獨立，並2 擇自由鹵素、c「c4烷基、_素—Ci—c4烷基、Cl—c 、 鹵素-(^-〇4烧氧基所組成的族群中。 土及 5. 根據申請專利範圍第！項之式J化合物A 例子中，以游離的形式或以鹽類㈣式存纟1 母個 先前提供的限制條件，其中Ri是氫、 ’〜、有包含 c4烷基或（：丨-(：4烷氧基甲基。 I C1〜 6·根據申請專利範圍第i項之式j化n 例子中，以游離的形式或以鹽類的形式存在，係 = 200305556 =供的限制條件’其"1是氫、Ci_c2烧基或_素々 :根據申請專利細"員之式！化合物，在每個 歹二中，以游離的形式或以鹽類的形式存在，係具有包含 先前提供的限制條件，其中Ri是氫或Ci_W基。、δ 根據申請專利刪1項之式I化合物，在每個 列中，以游離的形式或以鹽類的形式存在，係呈有包人 =提供的限制條件，其中互相獨1 ，：：、函素、未經取代的或經單—或多取代的Ci_C4貌基 /、取代基可以是互相獨立，並且選擇自由函素及 院氧基所組成的族群中；c3_c5環燒基或未經取代的或經4 擇Λ取Λ的苯基，其中取代基可以是互相獨立，並且選 擇自由齒素、CrC4燒基、函素_Ci_C4燒基 函素Ά燒氧基所組成的族群中。 "氧基及 根據申請專利範圍第1項之式！化合物，在每個 游離的形式或以鹽類的形式存在，係具有包含 限制條件，其中…6互相獨立 =、未經取代的或經單-或多取代的…基，其中 美所：：以疋互相獨立，並且選擇自由齒素及Μ燒氧 基所、、且成的族群中；或C3 - c5環烷基。 :·，根據申請專利则i項之式！化合物，在每個 先離的形式或以鹽類的形式存在，係具有包含 条件，其"2、R3、R4、…6互相獨立 也疋虱、CrC2烷基或q 一 G環烷基。 81 200305556 I u·根據申請專利範圍第l項之式丨化合物，在每個 例子中’ α游離的形式或以鹽類的形式存在，係具有包含 先前提供的限制條件，其中ψ是0或s。 12·根據申請專利範圍第！項之式j化合物，在每個 例：中’ u游離的形式或以鹽類的形式存在，係具有包含 先如&供的限制條件，其中ψ是〇。C] Ce alkylfluorenyl, halogen-C1-Q alkylsulfonyl, Ci-C6 alkylamino, C6 alkylamino, Crh alkylcarbonyl, halogen_Ce alkylcarbonyl, In the group consisting of CfCe alkoxycarbonyl, c-Ce alkylaminocarbonyl and di_C1-Q alkylaminocarbonyl; unsubstituted or mono- or polysubstituted phenylcarbonyl, unsubstituted Or mono- or poly-substituted phenyl, wherein the substituents may be independent of each other, and free halogen, nitro, cyano, Ci_C6 alkyl, halo-CrC6 alkyl, CrC6 alkoxy, and halogen-c are selected ! _c6 alkoxy group; unsubstituted or mono- or poly-substituted phenoxy group, where the substituents can be independent of each other, and free halogen, nitro, cyano 78 200305556 group, (VC6 In the group consisting of alkynyl, dentin-Cl-C6 alkyl, Cl-C6 alkoxy, and dentin 1 ^ -1 * Ce alkoxy; and the ratio of unsubstituted or mono- or poly-substituted fluorene Alkyloxy 'wherein the substituents may be independent of each other, and free halogen, acyl, cyano, CrC6 alkyl, halo-c6c6 alkyl, Ce alkyl In the group consisting of halogen-CrC6 alkoxy; or unsubstituted or mono- or poly-substituted heteroaryl bonded by a ring carbon atom, the substituents of human and Aq may be independent of each other , And choose free halogen, succinyl, cyano, Cl-C6 alkyl, dentin_Ci_c6 alkyl, C4C4oxy, i-selenium (: 6xyloxy, cyanoyl, ^--K6 In the group consisting of sulfanyl, fluorenyl, Cl-C6 amine, and di_Ci_Ce amine. 3. According to the formula in the scope of the patent application, the compound, in each example, is in free form or It exists in the form of salts, which has the restriction conditions previously provided, in which Arl & are independently unsubstituted or mono- or polysubstituted aryl groups, in which the substituents of ΑΓ1 and ΑΓ2 are independent of each other, which is selected Free halogen, nitro, cyano, CrC6 alkyl, halo-c] -c6 alkyl, Cl_c6 ^ oxy, m_Ci_C6 alkoxy, naphthene, Crh alkylcarbonyl, and halogen-Ci-C6 alkyl In the group consisting of carbonyl groups; unsubstituted or mono- or poly-substituted phenylcarbonyl groups; unsubstituted or mono- or Substituted phenyl groups, in which the substituents may be independent of each other, and are selected from the group consisting of halogen, cyano, CrC6 alkyl and halo-K6 alkyl; and unsubstituted or mono- or poly-substituted Phenoxy, in which the substituents may be independent of each other, and selected from the group consisting of halogen, cyano, CrC6 alkyl, and halogen-alkyl; or 79 200305556 unsubstituted or substituted by a ring carbon atom Mono- or poly-substituted heteroaryl 'in which the substituents of Ari Ah can be independent of each other, and the choice is = by the functional element, cyano? Ί 牙 素 々 c6 院 基, the group consisting of oxygen soil and _ 素 -Ci-C6: 乳 元 乳 基. 4. According to the compound of formula I in item 1 of the scope of the patent application, in each case 'exists in free form or in the form of salts, there are restrictions provided by the package, where ^ and ~ are independent of each other. Substituted or mono- or poly-substituted aryl groups, in which the substituents of T8 "and Ar2 are mutually selected from the group consisting of free-formin, nitrogen, W㈣J-Cl-C4, alkoxy, and funin-Cl-C4. Oxygen, c3-c5 ring-burning C, its chitosan group and c4 carbon group; unselected two: early- or poly-substituted phenyl M group; and unsubstituted or mono- — = Substituted phenyl 'in which the substituents may be independent of each other, and is selected from the group consisting of: c, c4 alkyl, and halogen-alkyl group; unsubstituted A element bonded by a ring carbon atom Or via a single or heteroaryl group, where the substituents of Arl and Ar2 may be independent of each other, and may be selected from halogen, c, c4 alkyl, 素 prime-Ci-c4 alkyl, Cl-c, halogen-(^ -〇4alkoxy group. Soil and 5. According to the scope of the patent application of the formula J compound A in the example, in the free form Or, it is stored in the form of a salt 1 of the previously provided restrictions, where Ri is hydrogen, '~, has a c4 alkyl group or (: 丨-(: 4 alkoxymethyl group. I C1 ~ 6 · according to In the example of the formula i in the scope of the patent application, the examples exist in the free form or in the form of salts, = 200305556 = the restriction of the supply 'its " 1 is hydrogen, Ci_c2 alkyl or _ prime 々: According to the patent application formula, the compound, in each form, exists in free form or in the form of a salt, with the restriction conditions previously provided, wherein Ri is hydrogen or Ci_W group., Δ According to the deletion of one item of the compound of formula I according to the application patent, in each column, it exists in free form or in the form of salts, which is subject to the restrictions provided by Baoren =, which are independent of each other ::, Unsubstituted or mono- or multi-substituted Ci_C4 morpho /, the substituents may be independent of each other, and selected from the group consisting of free-formin and oxo; c3_c5 cycloalkyl or unsubstituted or The phenyl group is taken by Λ, where the substituents may be independent of each other, and Choose from the group consisting of free halides, CrC4 alkyls, and functional groups _Ci_C4 alkyls and stilbyloxy groups. &Quot; Oxygen and formula according to item 1 of the scope of patent application! Compounds in each free form Or it exists in the form of salt, which has the restriction conditions, in which ... 6 are independent of each other =, unsubstituted or mono- or polysubstituted ... groups, where Meisuo :: is independent of each other, and chooses free teeth Or C3-c5 cycloalkyl groups::, according to the formula of item i according to the patent application! The compounds, which exist in each pre-isolated form or in the form of a salt, have inclusion conditions, which are independent of each other, and also include ticks, CrC2 alkyl, or q-G cycloalkyl. 81 200305556 I u · Compounds according to formula l in the scope of application for patent application 丨 In each case, 'α free form or salt form exists, including the constraints provided previously, where ψ is 0 or s . 12 · According to the scope of patent application! The compound of formula j, in each case: ′ u exists in free form or in the form of a salt, and has a restriction condition including 供 & where ψ is 0. .根據巾請專利範圍第1項之式丨化合物，在每個 :子中’以游離的形式或以鹽類的形式存在，係且有 先前提供的限制條件’其中a是卜2或3。 存丨根據^請專利範圍第1項之式1化合物，在每個 先^，以游離的形式或以鹽類的形式存在，係具有包含 先4供的限制條件，其中&是i或2。 例子1 中5.，根據申請專利範圍第1項之式I化合物，在每個 先游離的形式或以鹽類的形式存在，係具有包含 先剛k供的限制條件，其中&是工。According to the formula 丨 compound of claim 1, in each of the following formulae, 'is present in free form or in the form of a salt, and there are restrictions provided previously' where a is Bu 2 or 3. According to ^, the compound of formula 1 in the first item of the patent scope exists in free form or in the form of a salt in each antecedent, which has the restriction that the antecedent is provided, where & is i or 2 . 5. In Example 1, the compound of formula I according to item 1 of the scope of patent application, which exists in each free form or in the form of a salt, has a restriction condition that includes the first supply, where & is a worker. 例/φ6.㈣中請專利範圍第1項之式1化合物，在每個 ’以游離的形式或以鹽類的形式存 先則提供的限制條件，其“是0、〗或卜 例子1 中7.，=Γ專利範圍第1項之式1化合物，在每個 離的形式或以鹽類的形式存在，係具有包含 先别提供的限制條件，其中或卜 3 例子1 中8·，=請專利範圍第1項之式1化合物，在每個 先前提供的二，的形式或以鹽類的形式存在，係具有包含 先月供的限制條件，其中b是0。 82 200305556 19·根據申請專利範圍第1項之式I化合物，在每個 例子中，以游離的形式或以鹽類的形式存在，係具有包含 先前提供的限制條件，其中Ari及Ar2互相獨立地是未經取 代的或經單-或多取代的芳基，其中An及Ar2的取代基互 相獨立地選擇自由鹵素、硝基、氰基、Cl—c6烷基、iS素-匕-〇：6烧基、（：丨-(：6烷氧基、鹵素烷氧基、C3-C6環烷 基、C6烷基磺醯基、鹵素-Ci_C6烷基磺醯基、Cl_c6烷胺 基、二-CrC6烷胺基、Cl—c6烷基羰基、鹵素—Ci_C6烷基羰 基、G-C：6烷氧基羰基、Ci-C6烷基胺基羰基及二-Ci_Ce烷基 · 胺基幾基所組成的族群中；未經取代的或經單—或多取代 的苯基羰基；未經取代的或經單—或多取代的苯基，其中 取代基可以是互相獨立，並且選擇自由鹵素、硝基、氰基 、1-(：6烷基、画素—Ci — C6烷基、c厂C6烷氧基及鹵素一 烷氧基所組成的族群中；未經取代的或經單—或多取代的 苯氧基，其中取代基可以是互相獨立，並且選擇自由鹵素 、硝基、虱基、Cl-C6烷基、_素―Ci —c6烷基、c「c6烷氧基 及鹵素CrC6烧氧基所組成的族群中；以及未經取代的或 _ 經單-或多取代的Dtt啶氧基，其中取代基可以是互相獨立： 並且選擇自由齒素、石肖基、氰基、W烷 雜芳基，心取代的或經單〜或多取代的 ' 土 ’、令Ar!及Ar2的取代其^p s π J γ 摞自由HI冬 取代基可以疋互相獨立，並且選 擇自由函素、硝基、氰基、c 1 %烷基、鹵素一c〗-c6烷基、 83 200305556 <VC6烷氧基、鹵素一Ci—C6烷氧基、Ci-c6烷基磺醯基、鹵素 -Κ6烧基磺醯基、Cl—c6烷胺基及二-Ci_C6烷胺基所組成 的族群中； h是氫、（Vc4烷基、鹵素-Cl-C4烷基或Cl-c4烷氧基 曱基； 1h、R4、Rs及r6互相獨立地是氫、齒素、未經取 代的或經單-或多取代的Cl-c4烷基，其中取代基可以是互 相獨立’並且選擇自由函素及烷氧基所組成的族群 中，C3-Cs環烷基或未經取代的或經單-或多取代的苯基， 其中取代基可以是互相獨立，並且選擇自由鹵素、Ci-C4烷 基、幽素-CrG烧基、c!-c4烷氧基及鹵素-C!-C4烷氧基所 組成的族群中； W是0或S ; a是1、2或3 ;以及 b是0、1或2。 2〇·根據申請專利範圍第1項之式I化合物，在每個 例子中’以游離的形式或以鹽類的形式存在，係具有包含 先刖提供的限制條件，其中Ari及Ar2互相獨立地是未經取 代的或經單-或多取代的芳基，其中Ari及Ar2的取代基互 相獨立，係選擇自由_素、硝基、氰基、Ci — C6烷基、鹵素 -Ci C6燒基、C〗-C6燒氧基、鹵素_(^一(]6烧氧基、c3-c6環烧 基、c广ce烷基羰基及鹵素一Cl-C6烷基羰基所組成的族群中 •，未經取代的或經單-或多取代的苯基羰基；未經取代的 或經單-或多取代的笨基，其中取代基可以是互相獨立， 84 200305556 並且選擇自由鹵素、氰基、q-C6烷基及鹵素—Ci-Ce烷基所 組成的族群中；以及未經取代的或經單—或多取代的苯氧 基’其中取代基可以是互相獨立，並且選擇自由鹵素、氰 基、c!-烧基及鹵素-q-C6烧基所組成的族群中；或 藉由環碳原子而鍵結之未經取代的或經單—或多取代的 雜芳基，其中Ar!及Arz的取代基可以是互相獨立，並且選 擇自由鹵素、氰基、CrC6烷基、鹵素-Crh烷基、Cl—c6烷 氧基及鹵素-CrCe烷氧基所組成的族群中； Ri是氳、烧基或鹵素-(^-〇2院基； 尺2、hh、R5及Re互相獨立地是氫、未經取代的或 經單-或多取代的Ci-C4烷基，其中取代基可以是互相獨立 ’並且選擇自由鹵素及CrC2烧氧基所組成的族群中；或 〔3-[5環烧基； w是0 ; a是1或2 ;以及 b是0或1。 21 ·根據申請專利範圍第1項之式I化合物，在每個 例子中，以游離的形式或以鹽類的形式存在，係具有包含 先如提供的限制條件，其中Aq及Ai：2互相獨立地是未經取 代的或經單-或多取代的芳基，其中Ar!及Ar2的取代基互 相獨立，係選擇自由鹵素、氰基、Cl-c4烷基、鹵素—Ci_C4 烧基、C^C：4烷氧基、鹵素-q-C4烷氧基、C3-C5環烷基、 Ci-C4烷基羰基及函素-Ci—h烷基羰基所組成的族群中；未 經取代的或經單-或多取代的苯基羰基；以及未經取代的 85 200305556 或經單-或多取代的苯基，其中取代基可以是互相獨立， 並且選擇自由鹵素、CrC4烷基及鹵素-C广c4烷基所組成的 族群中；或 藉由環碳原子而鍵結之未經取代的或經單—或多取代的 雜芳基，其中Ari及Arz的取代基可以是互相獨立，並且選 擇自由函素、Cl-C4烧基、函素_Ci_c4烧基、Ci_c々氧基及 _素-Ci-C4烷氧基所組成的族群中； Ri是氫或Ci-C2院基； Cl -C2燒基或 、R3、、r5及R6互相獨立地是氫 C3-C5環烧基； W是0 ; a是1 ;以及 b是0 〇 22·根據申請專利範圍第丨項之式丨化合 、 的形式或以鹽類的形式存在，具有名稱為二’广游離 [5, 7-二氣喹咐-8_基氧基甲基]乙基）_4一三 氰土-卜 〇 〇 _ ^ 氟甲基笨醯胺。 23· 一種製備如申請專利範圍第1項的 方法，在每個例子中，係以游離：化合物之 備，其包括將式"之化合物： U鹽的形式而製 ' «2 N-- H CN (C)a—W~(C)f~Ar2 k k 86 II， 200305556 其為已知的化合物或可類似於有關的已知化合物而製 備，以及其中 R】、r2、R3、R4、R5、r6、w、Ar2、a 及 b 是 如式I之定義，與式IΠ之化合物反應： /Q An—^ hi, O # 丹钓匕知的化合物或可類似於有關的已知化合物而 備’以及其中ΑΠ是如式！之定義’以及Q是離去基， 要時，在驗性催化劑的存在下反應；以及在每個例子中 如果需要的話，將該方法或其他方式所得到的式j化人 ，以游離的形式或以鹽的形式 口 ;將該方法所得的異構物I::成…其他化合 的異構物；及/或將該方法:二一 鹽類，或將該方法所得的式：之游離化合物轉換. 之游離化合物或其他鹽類。“物之鹽類’轉換成式 Μ. —種製備式ΠExample / φ6. Please apply for the compound of formula 1 in the first item of the patent scope. In each of the restrictions provided in the free form or in the form of salts, "is 0," or in Example 1. 7., = Γ The compound of formula 1 in the first item of the patent scope exists in each isolated form or in the form of a salt, and has a restriction condition including the provision provided in advance, in which, or Example 3 in Example 1, 8 ·, = The compound of formula 1 in item 1 of the patent scope exists in the form of each of the two previously provided, or in the form of a salt, which has a restriction condition that includes a monthly payment, where b is 0. 82 200305556 19 · According to the patent application The compound of formula I in the scope of item 1, in each case, exists in free form or in the form of a salt, with the restriction conditions previously provided, in which Ari and Ar2 are independently unsubstituted or Mono- or poly-substituted aryl groups, in which the substituents of An and Ar2 are independently selected from the group consisting of halogen, nitro, cyano, Cl-c6 alkyl, iS element-D-O: 6alkyl, (: 丨- (: 6 alkoxy, halogen alkoxy, C3-C6 cycloalkyl, C6 alkylsulfonyl, Halo-Ci_C6 alkylsulfonyl, Cl_c6 alkylamino, di-CrC6 alkylamino, Cl-c6 alkylcarbonyl, halogen-Ci_C6 alkylcarbonyl, GC: 6 alkoxycarbonyl, Ci-C6 alkylamino Carbonyl and di-Ci_Ce alkyl · amino groups; unsubstituted or mono- or poly-substituted phenylcarbonyl groups; unsubstituted or mono- or poly-substituted phenyl groups, where Substituents may be independent of each other, and are selected from the group consisting of halogen, nitro, cyano, 1-(: 6-alkyl, pixel-Ci-C6 alkyl, C6 alkoxy and halogen-alkoxy Medium; unsubstituted or mono- or poly-substituted phenoxy, in which the substituents can be independent of each other, and the choice is free halogen, nitro, tick, Cl-C6 alkyl, _ prime -Ci -c6 alkane In the group consisting of alkyl, c, c6 alkoxy and halogen CrC6 alkoxy; and unsubstituted or _ mono- or poly-substituted Dttpyridyloxy, wherein the substituents may be independent of each other: and the choice is free Halogen, Schottyl, Cyano, W-heteroaryl, heart-substituted or mono- or poly-substituted 'Earth', let Ar! And Ar2 ^ Ps π J γ 摞 free HI winter substituents can be independent of each other, and choose free funin, nitro, cyano, c 1% alkyl, halogen-c6 alkyl, 83 200305556 < In the group consisting of VC6 alkoxy, halogen-Ci-C6 alkoxy, Ci-c6 alkylsulfonyl, halogen-K6 alkylsulfonyl, Cl-c6 alkylamino and di-Ci_C6 alkylamino ; H is hydrogen, (Vc4 alkyl, halogen-Cl-C4 alkyl, or Cl-c4 alkoxyfluorenyl; 1h, R4, Rs, and r6 are each independently hydrogen, dentin, unsubstituted or monosubstituted -Or multi-substituted Cl-c4 alkyl, wherein the substituents may be independent of each other and selected from the group consisting of free-formin and alkoxy, C3-Cs cycloalkyl or unsubstituted or mono- or Poly-substituted phenyl, wherein the substituents may be independent of each other, and selected from halogen, Ci-C4 alkyl, peptidyl-CrG alkyl, c! -C4 alkoxy, and halogen-C! -C4 alkoxy In the group consisting of; W is 0 or S; a is 1, 2 or 3; and b is 0, 1 or 2. 2． According to the compound of formula I according to item 1 of the scope of the patent application, in each case 'exists in free form or in the form of a salt, it has the restriction conditions including those provided by the former, in which Ari and Ar2 are independent of each other. Is an unsubstituted or mono- or poly-substituted aryl group, in which the substituents of Ari and Ar2 are independent of each other, which are freely selected from the group consisting of halogen, nitro, cyano, Ci-C6 alkyl, and halogen-Ci C6 alkyl. , C〗 -C6 alkoxy, halogen _ (^ a () 6 alkoxy, c3-c6 cycloalkoxy, c-Ce alkylcarbonyl, and halo-Cl-C6 alkylcarbonyl group •, Unsubstituted or mono- or poly-substituted phenylcarbonyl; unsubstituted or mono- or poly-substituted phenyl, wherein the substituents may be independent of each other, 84 200305556 and select free halogen, cyano, q -C6 alkyl group and halogen-Ci-Ce alkyl group; and unsubstituted or mono- or poly-substituted phenoxy 'wherein the substituents may be independent of each other, and free halogen, cyano are selected , C! -Alkyl and halogen-q-C6 alkyl; or unbound by a ring carbon atom Substituted or mono- or poly-substituted heteroaryl, in which the substituents of Ar! And Arz may be independent of each other, and free halogen, cyano, CrC6 alkyl, halogen-Crh alkyl, Cl-c6 alkyl are selected In the group consisting of alkoxy and halogen-CrCe alkoxy; Ri is fluorene, alkynyl or halogen-(^-〇2 courtyard; Chi 2, hh, R5 and Re are independently hydrogen, unsubstituted Or a mono- or poly-substituted Ci-C4 alkyl group, in which the substituents may be independent of each other and selected from the group consisting of halogen and CrC2 alkoxy; or [3- [5 ring alkynyl; w is 0 a is 1 or 2; and b is 0 or 1. 21 · According to the compound of formula I in item 1 of the scope of the patent application, in each example, it exists in free form or in the form of a salt, which has a If provided with restrictions, where Aq and Ai: 2 are independently unsubstituted or mono- or poly-substituted aryl groups, where the substituents of Ar! And Ar 2 are independent of each other, free halogen, cyano, Cl-c4 alkyl, halogen-Ci_C4 alkyl, C ^ C: 4 alkoxy, halogen-q-C4 alkoxy, C3-C5 cycloalkyl, Ci-C4 alkylcarbonyl, and In the group of halo-Ci-h alkylcarbonyl groups; unsubstituted or mono- or polysubstituted phenylcarbonyl groups; and unsubstituted 85 200305556 or mono- or polysubstituted phenyl groups, of which The substituents may be independent of each other and selected from the group consisting of halogen, CrC4 alkyl and halogen-C-c4 alkyl; or unsubstituted or mono- or polysubstituted by a ring carbon atom Heteroaryl group, in which the substituents of Ari and Arz can be independent of each other, and the choice of free function element, Cl-C4 alkyl group, functional element _Ci_c4 alkyl group, Ci_c alkoxy group and _ prime-Ci-C4 alkoxy In the group consisting of; Ri is hydrogen or Ci-C2 radical; Cl-C2 alkyl or R3, R5 and R6 are independently hydrogen C3-C5 cycloalkyl; W is 0; a is 1; and b is 0 〇22 · According to the formula in the scope of the patent application, the form of the compound, or exists in the form of salts, and has the name di 'wide free [5, 7-digasquinol-8-yloxy Methyl] ethyl) -4-tricyanotoxan-b-fluoromethylbenzylamine. 23 · A method for preparing as described in item 1 of the scope of the patent application, in each case, it is prepared as a free: compound, which includes a compound of formula " U salt form '' «2 N--H CN (C) a—W ~ (C) f ~ Ar2 kk 86 II, 200305556 It is a known compound or can be prepared similar to the related known compound, and wherein R], r2, R3, R4, R5, r6, w, Ar2, a, and b are as defined in Formula I and react with compounds of Formula IΠ: / Q An— ^ hi, O # Compounds known by Dan Diao or may be prepared similar to related known compounds. And where ΑΠ is like this! The definition of 'and Q is a leaving group, if necessary, the reaction in the presence of an empirical catalyst; and in each case, if necessary, the formula obtained by this method or other means is converted into a free form Or in the form of a salt; the isomer I: obtained by the method is: other isomers; and / or the method: a dione salt, or the free compound of the formula: Conversion of free compounds or other salts. "Salts of matter" is transformed into formula M. — a preparation formula Π 係以游離的形式或以鹽的形：：方法’在每個例子中 合物： 》製備，其包括將式IV之,Is in free form or in the form of a salt :: method ' in each example, a compound: " 備 其為已知的化合物或 八J _似Μ ‘ 以及其中R2、R3、R、 ；有關的已知化合物而製 4 尺5、R6、你 Λ 6 W、Ar2、a及b是如式 87 200305556 岸與無機或有機氮化物以及式Ri為之化合物反 二的化合物或可類似於有關的已知 L:1是如式1之定義；以及在每個例子中，如 而的活，將该方法或其他方式所得到 以游離的形式或以鹽的形式， 化口物 u. ^ . 轉換成式1 1的其他化合物； 將该方法所得的異構物之混 里媸必· n U 初加以刀開，並分離所要的 /、構物，及/或將該方法所得 睡類，m… 斤侍的式11之游離化合物轉換成 員、或將该方法所得的式π化合物之鹽類 π之游離化合物或其他鹽類。 、> 25· —種控制寄生蟲之 . s , 口物，其包括除了載體及/ 物作為活性成份。 貝之式I化合 26· —種如申請專利範圍第1 7么m 只曰〕式I化合物之庫用 ，係用於控制寄生蟲。 < 應用 27· —種控制寄生蟲 _錄+ A / ，八匕括將有效量的至少 種如申請專利範圍第1項 夕 # 。 、式1化合物用於對抗寄生蟲 28· —種如申請專利範 .. 圍第1項的式I化合物之庫用 ，係用於控制溫血動物的寄生蟲之方去 μ 29. -種如申請專利範圍第μ ，係用於製備對抗溫血動物的 之應用 初的寄生蟲之醫藥組合物。 拾壹、圖式·· 88 200305556 柒、指定代表圖： (一) 本案指定代表圖為：第（無）圖。 (二) 本代表圖之元件代表符號簡單說明： 無 捌、本案若有化學式時，請揭示最能顯示發明特徵的化學式Let it be a known compound or JJ_like M ′ and among them R2, R3, R,; related known compounds are prepared in 4, 5, R6, Λ 6 W, Ar2, a and b are as shown in formula 87 200305556 Shore and inorganic or organic nitrides and compounds of the formula Ri may be similar to the related known L: 1 is as defined in Formula 1; and in each case, as is the case, the It is obtained in a free form or in the form of a salt by a method or other method, and is converted into other compounds of formula 1 1 in a free form or in a salt form; Knife open, and separate the desired /, structure, and / or sleep class obtained by the method, m ... Jins free compound of formula 11 conversion members, or free salt of the compound of formula π obtained by this method Compounds or other salts. ≫ 25 · —A species of parasite-controlling oral substance, which includes, in addition to the carrier and / or substance, the active ingredient. The compound of the formula I is 26. A kind of compound of the formula I, such as the scope of the patent application (17), is used for the control of parasites. < Application 27 · —Species for controlling parasites _ 录 + A /, the effective amount of at least one species is as in the scope of patent application item 1 Xi #. 1. Compounds of formula 1 are used to fight parasites 28 · — species such as patent applications. The library of compounds of formula I around item 1 is used to control parasites in warm-blooded animals μ 29.-Species such as The scope of application for patent is μ, which is used for preparing a pharmaceutical composition against the parasites in the beginning of application for warm-blooded animals. (1) Designated representative map: (1) The designated representative map in this case is: (none) map. (2) Brief description of the component symbols in this representative map: None 捌 If there is a chemical formula in this case, please disclose the chemical formula that can best show the characteristics of the invention 55
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