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TW201103429A - Triazole compounds carrying a sulfur substituent XI - Google Patents

Triazole compounds carrying a sulfur substituent XI Download PDF

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Publication number
TW201103429A
TW201103429A TW099120000A TW99120000A TW201103429A TW 201103429 A TW201103429 A TW 201103429A TW 099120000 A TW099120000 A TW 099120000A TW 99120000 A TW99120000 A TW 99120000A TW 201103429 A TW201103429 A TW 201103429A
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group
compound
alkyl
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Sarah Ulmschneider
Jochen Dietz
Jens Renner
Thomas Grote
Wassilios Grammenos
Bernd Mueller
Jan Klaas Lohmann
Marianna Vrettou-Schultes
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Basf Se
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Plural Heterocyclic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to novel triazole compounds of the formulae I and II as defined below which carry a sulfur substituent, to agricultural compositions containing them, to their use as fungicides and to intermediate compounds used in the method of producing them.

Description

201103429 六、發明說明: 【發明所屬之技術領域】 本發明係關於一種具有硫取代基之如下所定義之新穎式 I及II之三唑化合物,含有其之農業組合物,其作為殺真菌 劑之用途及用於其製造方法中之中間化合物。 【先前技術 防治由植物病原真菌所引起的植物病對實現高產效而言 極其重要。觀賞作物、蔬菜作物、田間作物、榖類作物及 水果作物之植物病害可使生產力明顯降低,由此增加消費 者之成本。 WO 96/41804、WO 96/16048、WO 97/41107、WO 97/43269 及WO 97/44331描述硫化三唑基衍生物。該等化合物係用於 對抗有害真菌。 不斷需要一種新穎化合物,其更有效,成本更低,毒性 更小,對環境更安全及/或具有不同作用方式。 【發明内容】 因此,本發明之一目標在於提供具有較佳殺真菌活性及/ 或較佳作物相容性之化合物。 意外地,此等目標係由如下所定義之通式I及II之三唑化 合物及化合物I及II之農業上可接受之鹽實現。 因此,本發明係關於式I及II之三唑化合物及其農業上適 用之鹽, 149026.doc 201103429201103429 VI. OBJECTS OF THE INVENTION: TECHNICAL FIELD The present invention relates to a novel triazole compound of the formula I and II having a sulfur substituent as defined below, comprising an agricultural composition thereof as a fungicide Use and intermediate compounds used in the method of its manufacture. [Prior Art Control of plant diseases caused by phytopathogenic fungi is extremely important for achieving high productivity. Plant diseases in ornamental crops, vegetable crops, field crops, alfalfa crops, and fruit crops can significantly reduce productivity, thereby increasing the cost to consumers. The triazole-based derivatives are described in WO 96/41804, WO 96/16048, WO 97/41107, WO 97/43269 and WO 97/44331. These compounds are used against harmful fungi. There is a constant need for a novel compound that is more efficient, less costly, less toxic, safer to the environment, and/or has a different mode of action. SUMMARY OF THE INVENTION Accordingly, it is an object of the present invention to provide compounds having preferred fungicidal activity and/or better crop compatibility. Surprisingly, these objectives are achieved by triazole compounds of the formulae I and II as defined below and the agriculturally acceptable salts of the compounds I and II. Accordingly, the present invention relates to triazole compounds of the formulae I and II and their agriculturally acceptable salts, 149026.doc 201103429

s(〇)mR6 R6as(〇)mR6 R6a

其中among them

Het為含有1、2或3個選自 之雜原子作為環成員 _、4_、5-、6-或7_員飽和、部分不飽和或 環,其中該雜環可具有卜2、3或4個取代基r5;、雜 A為可經1、2、3或4個取代基R7取代之直鏈Cl_c5伸烧 基橋; Y R1 為 〇、S 或 NR8 ; R2、R3及R4彼此獨立地選自氫、齒素、OH、SH、 n〇2 ' cn、Cl_c4烧基、Ci_C4 齒烧基、C2_C4稀基、 c2-c4自稀基、cvC4快基、c2_C4 -块基、c3_c8環燒 基、G-C8齒環烷基、Cl_C4烷氧基、Ci_C4函烷氧基、 c】-c4_氧基、Cl_C4i烯氧基、Cl_c4炔氧基、Ci_C4 鹵炔氧基、C3_CS環院氧基、C3_CS鹵環燒氧基、c丨_c4 烷硫基、C丨-C4鹵烷硫基、c丨-C4烯硫基、c丨_c4鹵炔硫 基、苯基、苯基-CVC4烷基、苯基_Ci_c4烷氧基、笨 氧基、苯硫基’其中最後5個提及基團中的苯基部分 可具有1、2、3、4或5個取代基R9;含有1、2或3個選 自N、0及S之雜原子作為環成員的3-、4-、5-、6-或7* 員飽和、部分不飽和或最大不飽和雜環,其中該雜環 149026.doc • 4· 201103429 可具有1、2或3個取代基R9; C〇R»〇 , C〇〇Ri〇 CONR15Ri6、NRi VI S(0)pRi〇,其巾上述基團中之 脂族部分可具有1、2或3個取代基R18且其中上述美團 中之環脂族部分可具有1、2或3個取代基ri9 ;或 R1及R2或R3及R4連同其所連接之碳原子—起形成部分 不飽和或最大不飽和5-、6-或7-員碳環或含有丨、2戍3 個選自Ο、S及N之雜原子作為環成員的部分不飽和或 最大不飽和5-、6-或7-員雜環;其中該碳環或雜環可 具有1、2或3個取代基R9 ; 各R5獨立地選自鹵素、OH、SH、N〇2、CN、Ci_C4烷美、 K鹵烷基、C2_C4烯基、c2_C4自烯基、C2_Cd 基、c2-c4齒炔基、C3_C8環烷基、c3_C8函環烷基、 c!-c4烷氧基、Cl_C4鹵烷氧基、Ci_C4烯氧基、 齒烯氧基、Cl-c4炔氧基、Cl-c4齒炔氧基、C3_C8環烧4 氧基、CVC8鹵環烷氧基、CVC4烷硫基、Ci_C4鹵烷硫 基、c^-c*»嫦硫基、c!-C4鹵炔硫基、苯基、苯基_Ci C4烷基、苯基-Cl_(:4烷氧基、苯氧基、苯硫基其中 最後5個提及基團中的苯基部分可具有i、2、3、4或5 個取代基R9;含有丨、2或3個選自N、〇及8之雜原子 作為環成員的3·、4_、5_、6_或7_員飽和、部分不飽 和或最大不飽和雜環,其中雜環可具有丨、2或3個取 代基 R9 ; COR1。' c〇〇Rl。、c〇Nr15r16、nr15r16 及 S(〇)PR,其中上述基團中之脂族部分可具有【、2或3 個取代基R纟其中上述基團令之環脂族部分可具有 149026.doc 201103429 1、2或3個取代基rB ;或 連接於(Het之)相鄰環原子上的兩個基團R5連同其所連 接之環原子一起形成部分不飽和或最大不飽和5_、6_ 或7-員碳環或含有丨、2或3個選自〇、S&N之雜原子作 為環成員的部分不飽和或最大不飽和5_、6_或7_員雜 %,其中碳環或雜環可具有1、2或3個取代基尺9 ; R6係選自氫、CVCM燒基、Cl_ClG齒烷基、c2_CiG稀基、 Ca-Ci❶函稀基、c2_CiG炔基、c2_Ci一炔基、C3_CM環 烷基、C3-C10_環烷基、苯基、苯基_Ci_c4烷基,其 中最後2個提及基團中的苯基部分可具有1、2、3、4 或5個取代基R1〗’及含有丨、2或3個選自N、〇及8之雜 原子作為環成員的5_或6_員飽和、部分不飽和或芳族 雜環,其中該雜環可具有!、2或3個取代基Rii ;或在 m為0之情況下,亦可選自_c( = 〇)R〗2、c( = s)r丨2、 _s(o)2r〗2、_CN、_p(=q)r13r14、M及式ΙΠ之基團Het is a saturated, partially unsaturated or cyclic ring containing 1, 2 or 3 hetero atoms selected from the group as a ring member _, 4_, 5-, 6- or 7-member, wherein the heterocyclic ring may have a b, 2, 3 or 4 a substituent r5;, a hetero A is a linear Cl_c5 extension bridge which can be substituted by 1, 2, 3 or 4 substituents R7; Y R1 is 〇, S or NR8; R2, R3 and R4 are independently selected from each other From hydrogen, dentate, OH, SH, n〇2 'cn, Cl_c4 alkyl, Ci_C4 dentate, C2_C4, c2-c4 from dilute, cvC4 fast radical, c2_C4 -block, c3_c8 cycloalkyl, G-C8 dentate alkyl, Cl_C4 alkoxy, Ci_C4 alkoxy, c]-c4_oxy, Cl_C4i alkenyloxy, Cl_c4 alkynyloxy, Ci_C4 haloalkoxy, C3_CS ring oxy, C3_CS Halocycloalkyloxy, c丨_c4 alkylthio, C丨-C4 haloalkylthio, c丨-C4 alkenethio, c丨_c4 haloalienyl, phenyl, phenyl-CVC4 alkyl, The phenyl moiety of the phenyl-Ci_c4 alkoxy group, the phenoxy group, the phenylthio group wherein the last five of the groups mentioned may have 1, 2, 3, 4 or 5 substituents R9; Three 3-, 4-, 5-, 6- or 7*-membered heteroatoms selected from N, 0 and S are saturated, partially unsaturated or a highly unsaturated heterocyclic ring wherein the heterocyclic ring 149026.doc • 4· 201103429 may have 1, 2 or 3 substituents R9; C〇R»〇, C〇〇Ri〇CONR15Ri6, NNi VI S(0)pRi〇 The aliphatic moiety of the above-mentioned group of the towel may have 1, 2 or 3 substituents R18 and wherein the cycloaliphatic moiety of the above-mentioned melon may have 1, 2 or 3 substituents ri9; or R1 and R2 or R3 and R4 together with the carbon atom to which they are attached form a partially unsaturated or maximally unsaturated 5-, 6- or 7-membered carbocyclic ring or a hetero atom containing ruthenium, 2, 3 selected from ruthenium, S and N. a partially unsaturated or maximally unsaturated 5-, 6- or 7-membered heterocyclic ring of a ring member; wherein the carbocyclic or heterocyclic ring may have 1, 2 or 3 substituents R9; each R5 is independently selected from halo, OH , SH, N〇2, CN, Ci_C4 alkylene, K haloalkyl, C2_C4 alkenyl, c2_C4 from alkenyl, C2_Cd, c2-c4 alkynyl, C3_C8 cycloalkyl, c3_C8 functional cycloalkyl, c! -c4 alkoxy, Cl_C4 haloalkoxy, Ci_C4 alkenyloxy, dentenyloxy, Cl-c4 alkynyloxy, Cl-c4 alkynyloxy, C3_C8 cycloalkyloxy, CVC8 halocycloalkoxy , CVC4 alkylthio, Ci_C4 haloalkylthio, c^-c*»嫦thio, c !-C4 haloalkynylthio, phenyl, phenyl-Ci C4 alkyl, phenyl-Cl_(:4 alkoxy, phenoxy, phenylthio wherein the phenyl moiety of the last five mentioned groups May have i, 2, 3, 4 or 5 substituents R9; 3, 4, 5, 6 or 7 members containing ruthenium, 2 or 3 heteroatoms selected from N, oxime and 8 as ring members a saturated, partially unsaturated or maximum unsaturated heterocyclic ring wherein the heterocyclic ring may have fluorene, 2 or 3 substituents R9; COR1. ' c〇〇Rl. And c〇Nr15r16, nr15r16 and S(〇)PR, wherein the aliphatic moiety of the above group may have [, 2 or 3 substituents R, wherein the above-mentioned group is such that the cycloaliphatic moiety may have 149026.doc 201103429 1, 2 or 3 substituents rB; or two groups R5 attached to adjacent ring atoms (of Het) together with the ring atoms to which they are attached form a partially unsaturated or maximum unsaturated 5_, 6_ or 7- a carbon ring or a partially unsaturated or maximal unsaturated 5-, 6- or 7-membered hetero atom containing hydrazine, 2 or 3 heteroatoms selected from hydrazine, S&N, wherein the carbocyclic or heterocyclic ring may be Having 1, 2 or 3 substituent bases 9; R6 is selected from the group consisting of hydrogen, CVCM alkyl, Cl_ClG dentate, c2_CiG dilute, Ca-Ci 稀 dilute, c2_CiG alkynyl, c2_Ci-alkynyl, C3_CM naphthenic a group, a C3-C10_cycloalkyl group, a phenyl group, a phenyl-Ci_c4 alkyl group, wherein the phenyl moiety in the last two mentioned groups may have 1, 2, 3, 4 or 5 substituents R1" And a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic ring containing hydrazine, 2 or 3 heteroatoms selected from N, fluorene and 8 as ring members, wherein the heterocyclic ring may have! , 2 or 3 substituents Rii; or in the case where m is 0, may also be selected from _c(= 〇)R, 2, c(= s)r丨2, _s(o)2r, 2, _CN , _p(=q)r13r14, M and the group of the formula

、R3及R4係如式I灰Π中所定, R3 and R4 are as defined in Formula I Ashes

Het、a、γ、ri、 義;且 #為連接至分子其餘部分之連接點 149026.doc -6 · 201103429 R係選自氫' Ci-C10烷基、cvcj烷基、c2-c10烯基、 c2-c1()iS 稀基、c2_Ci。炔基、c2_Ci()^ 炔基、c3_Ci〇環 炫基、C3-C10_環烷基、笨基、笨基_Ci_C4烷基,其 中最後2個提及基團中的笨基部分可具有1、2、3、4 或5個取代基尺11 ’含有1、2或3個選自N、〇及s之雜 原子作為環成員的5 -或6-員飽和、部分不飽和或芳 族雜環’其中該雜環可具有1、2或3個取代基Rll,Het, a, γ, ri, meaning; and # is the point of attachment to the rest of the molecule 149026.doc -6 · 201103429 R is selected from hydrogen 'Ci-C10 alkyl, cvcj alkyl, c2-c10 alkenyl, C2-c1()iS dilute base, c2_Ci. Alkynyl, c2_Ci()^ alkynyl, c3_Ci fluorenyl, C3-C10_cycloalkyl, phenyl, phenyl-Ci_C4 alkyl, wherein the stupid moiety in the last two mentioned groups may have 1 , 2, 3, 4 or 5 substituted base gauges 11 'containing 1, 2 or 3 heteroatoms selected from N, 〇 and s as ring members, 5- or 6-membered saturated, partially unsaturated or aromatic Ring 'wherein the heterocyclic ring may have 1, 2 or 3 substituents R11,

-C(-〇)R丨2、_c(=S)R丨2、-S(〇)2R12、_CN、-P(=Q)R丨3rU 及Μ ; 各R7獨立地選自鹵素、OH、SH、NR,5R,6、Ci_C4烷基、 c,-c4 _ 烷基、C2_C4烯基、C2_C4 _ 烯基、块 基、c2-c4鹵炔基、c丨·(:4烷氧基、Ci-c4鹵烷氧基、 CrC4烷硫基及匕-匚4鹵烷硫基,其中上述基團中之脂 叙部分可具有1、2或3個取代基R18;或 連接於兩個相鄰碳原子上的兩個基團尺7連同其所連接 之碳原子一起形成3_、4-、5_、6-或7-員飽和、部分 不飽和或最大不飽和碳環或含有1、2或3個選自〇、= 5-、6_或7-員飽 其令該碳環或雜 及N之雜原子作為環成員的3_、4_ 和、部分不飽和或最大不飽和雜環, 環可具有1、2或3個取代基r9;-C(-〇)R丨2, _c(=S)R丨2, -S(〇)2R12, _CN, -P(=Q)R丨3rU and Μ; each R7 is independently selected from halogen, OH, SH, NR, 5R, 6, Ci_C4 alkyl, c, -c4 _ alkyl, C2_C4 alkenyl, C2_C4 _ alkenyl, alkyl, c2-c4 haloalkynyl, c丨·(:4 alkoxy, Ci a -c4 haloalkoxy group, a CrC4 alkylthio group, and a fluorenyl-fluorenyl 4-haloalkylthio group, wherein the aliphatic moiety of the above group may have 1, 2 or 3 substituents R18; or attached to two adjacent carbons The two radicals 7 on the atom together with the carbon atoms to which they are attached form a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated carbon ring or contain 1, 2 or 3 a 3_, 4_ and a partially unsaturated or a maximum unsaturated heterocyclic ring selected from the group consisting of 〇, = 5-, 6- or 7-membered as a ring member of the carbocyclic or heterocyclic and N, the ring may have 1 , 2 or 3 substituents r9;

K 1 4明抓恭、12<4婦 基、c2-c4函烯基' c2_c4块基、c2_C4齒块基、CM 炫氧基、CVCj炫氧基、苯基、笨基基, t最後2個提及基團中的苯基部分可具有〗、2、3 1 149026.doc 201103429 或 5 個取代基 R9 ; COR1。、COOR10、CONR15R16 及 S(0)pR10 ; 各R9獨立地選自鹵素、〇H、SH、NR15R16、CN、N〇2、 炫《基、CVC4 -炫基、c2_c4稀基、c2-C4鹵烯 基、c2-c4炔基、c2_c4_ 炔基、Ci_c4院氧基、Ci_c4 li烧氧基、CrC4烷硫基及心-匕鹵烷硫基,其中上述 基團中之脂族部分可具有1、2或3個取代基Ris ; 各Ri〇獨立地選自氫、Ci_C4烷基、Cl_c4鹵烷基、C2-C4烯 基、C2-C4齒烯基、C丨_c4胺基烷基、苯基、苯基_c「 C4烧基’其中最後2個提及基團中的苯基部分可具有 1、2、3、4或5個取代基R9,及含有1、2或3個選自 Ν、Ο及S之雜原子作為環成員的5_或6_員飽和、部分 不飽和或芳族雜環’其中雜環可具有1、2或3個取代 基R9 ; 各Ru獨立地選自鹵素、〇H、SH、NR15R16、CN、N02、 CVC4烧基、CVC4 i炫•基、c2-c4烯基、c2-c4鹵烯 基、C2-C4炔基、c2-C4鹵炔基、烷氧基、CVC4 鹵烷氧基、CrC4烷硫基及(^-(:4鹵烷硫基,其中上述 基團中之脂族部分可具有1、2或3個取代基R18 ; R12係選自氫、CVC丨〇烷基、c〗-c10鹵烷基、CVCM烷氧 基、CVCm鹵烷氧基、Ci-Cw胺基烷基、c3-C10環烷 基、C3_C10鹵環烷基、苯基、苯基_Cl_c4烷基,其中 最後2個提及基團中的苯基部分可具有1、2、3、4或5 個取代基R",含有1、2或3個選自Ν、Ο及S之雜原子 149026.doc 201103429 作為環成員的5-或6_員飽和、部分不飽和或芳族雜 環,其中該雜環可具有丨、2或3個取代基Rll,及 NR,5R16 ; R13及R14彼此獨立地選自Cl_Cl〇烷基、Ci_c〗〇鹵烷基、c2_ c10稀基、c2-c1()卣烯基、c2-C1()炔基、C2-C1()鹵炔 基、C3-C1G環烷基、c3_ClG函環烷基、Ci_CiG烧氧基、 CVCw函烧氧基、Ci_c4_烷氧基_c〗_ci〇烷基、Ci_c4_烷 氧基-CrCw烷氧基、d-Cw烷硫基、Ci-Cw鹵烷硫 基、C2-C1Q烯氧基、c2_c.1()_烯硫基、c2_CiG炔氧基、 C2-C1(r炔硫基、(:3_CiG環烷氧基、c3_CiQ•環烷硫基、 笨基、苯基-Ci-C4烷基、苯硫基、苯基_Cl_c4烷氧基 及 NR15R16 ; 各R15獨立地選自氫&Cl-c8烷基; 各Ri6獨立地選自氫、Cl-C8烷基、苯基及苯基-Cl_c4烷 基; 或R15及R16—起形成直鏈(:^或“伸烷基橋或基團 -CH2CH2OCH2CH2-或-CH2CH2NR丨7CH2CH2-; 各R17獨立地選自氫及(^-(:4烷基; * 各R18獨立地選自硝基、CN、OH、SH、COR丨❶、COOR10、 . conr15r16、nr15r16、c3-c6 環烧基、c3-c6 i 環烷 基、G-C4烷氧基、c】-C4鹵烷氧基、c3-c6環烷氧基 (cycloaloxy)、苯基及苯氧基; 各R19獨立地選自;6肖基、CN、OH、SH、COR10、COOR10、 CONR15R16、NR15R16、Ci_c4 烧基、Ci_c4 齒烧基、c3_ H9026.doc -9- 201103429 c6環烷基、C3_C6鹵環烷基、c「c4烷氧基、Cl-c4ii燒 氧基、c3-c6環烷氧基、苯基及苯氧基; Q 為Ο或S ; M 為金屬陽離子相等物或式(NRaRbReRd)+之銨陽離子, 其中Ra、Rb ' RC及Rd彼此獨立地選自氫、Ci_c丨〇烷 基、苯基及苄基,其中最後2個提及基團中的苯基部 分可具有1、2或3個獨立地選自以下之取代基:齒 素、CN、硝基、Cl_C4烷基、Cl-C4鹵烷基、Ci_C4燒 氧基、CVC4鹵烷氧基及NR15R16 ; m 為0、1或2 ;且 P 為1或2。 本發明亦提供式I及Π之三唑化合物及/或其農業上適用 之鹽的用途,其用於防治有害真菌。 本發明進一步提供包含此等式1及/或11(亦及/或式W ;參 見下文)之三唑化合物及/或其農業上可接受之鹽及合適載 劑的殺真菌組合物。如下描述合適之農業上可接受之載 劑。 化合物I及II可以一或多種立體異構體形式存在。各種立 體異構體包括對映異構體、非對映異構體、滯轉異構體及 幾何異構體。熟習此項技術者應瞭解當一種立體異構體相 對於其它(多種)立體異構體增濃時或當與其它立體異㈣ 分離時,其可更具活性及/或可顯示出有益效果。另外, 熟練技術人員知曉如何分離、增濃及/或選擇性地製備該 等立體異構體。本發明化合物可呈現為立體異構體之混合 [S] I49026.doc m 201103429 物(例如外消旋體)、個別立體異構體或光學活性形式。 應瞭解化合物απ互為位置/雙鍵異構H少在基團 R6/R6a相同之情況下。在r6(當然以及R6a)為氫之情況下, 各別化合物I及II為互變異構體。 δ適的農業上適用之鹽尤其為彼等陽離子之鹽或彼等酸 之酸加成鹽’該等陽離子及陰離子分別對化合物則之殺 真菌作用無副作用n合適之陽離子尤其為驗金屬離 子,較佳鈉及鉀之離子;鹼土金屬離子,較佳鈣、鎂及鋇 之離子;及過渡金屬離子’較佳錳,、辞及鐵之離子; 以及铵離子(若需要,其可具有個Ci_c4烧基取代基及/ 或1個苯基或节基取代基),較佳為^異丙敍、四甲銨、四 丁銨、二曱苄銨,此外有鱗離子、銕離子,較佳三(Cl _匸4 烷基)锍及氧化錡離子,較佳為三(Ci_c4烷基)氧化鈑。 適用之酸加成鹽之陰離子主要為氣離子、溴離子、氟離 子、硫酸氫根、硫酸根、磷酸二氫根、磷酸氫根、磷酸 根、硝酸根、碳酸氫根、碳酸根、六氟矽酸根、六氟磷酸 根笨甲酸根以及c丨-C:4烧酸之陰離子,較佳為甲酸根、 乙酸根、丙酸根及丁酸根。其可藉由使與相應陰離子 之馱(較佳鹽酸、氫溴酸、疏酸、磷酸或硝酸)反應來形 成。 在上述式中所給變數之定義中,對於所討論之取代基使 用通常具有代表性之集合術語。術語Cn_Cm表示在各情況 下於所时論之取代基或取代基部分中可能的碳原子數目: 鹵素:氟、氯、溴及碘; »49026.doc 201103429 烷基及烷氧基、烷氧基烷基、烷氧基烷氧基、烷基羰 基、烧硫基幾基、胺基烧基、烧基胺基、二烧基胺基、烧 基胺基羰基、二烷基胺基羰基、烷硫基、烷基磺醯基及其 類似物中之烷基部分:具有1至2個烷基)、2或3個 (C2-C3烷基)、1至4個(CVCU烷基)、1至6個(CrCe烷基)、1 至8個(CrC8烷基)或1至10個(CrCw烷基)碳原子之飽和直 鏈或支鏈烴基。CyC:3烷基為乙基、正丙基或異丙基。Cl_ C2烧基為曱基或乙基。C1-C4烧基為曱基、乙基、丙基、 異丙基、丁基、1-甲基丙基(第二丁基)、2-甲基丙基(異丁 基)或1,1-二甲基乙基(第三丁基)。Cl-C6烷基另外亦為(例 如)戊基、1-曱基丁基、2-曱基丁基、3 -曱基丁基、2,2-二 曱基丙基、1-乙基丙基、1,1_二曱基丙基、L2-二曱基丙 基、己基、1-曱基戊基、2-甲基戊基、3-曱基戊基、4-甲 基戊基、1,1_ 一曱基丁基、-二曱基丁基、1,3 -二甲基丁 基、2,2-二曱基丁基、2,3-二甲基丁基、3,3-二曱基丁基、 1-乙基丁基、2-乙基丁基、ι,ι,2-三甲基丙基、三曱 基丙基、1-乙基-1-曱基丙基或1_乙基_2_甲基丙基。Cl_c8 烷基另外亦為(例如)庚基、辛基、2-乙基己基及其位置異 構體。C^Cio烷基另外亦為(例如)壬基、癸基、2_丙基庚 基、3-丙基庚基及其位置異構體。 鹵烷基:具有1至2個(CVC2函烷基)、1至3個鹵烷 基)' 1至4個(CVC4画烧基)、1至6個(CVC6鹵烧基)、1至8 個(C,-C8_烧基)、1至1〇個(Ci_Ci〇齒烧基)或2至1〇個((:2_ C10函烷基)碳原子之直鏈或支鏈烷基(如上所述),其中此 149026.doc •12· 201103429 等基團中之-些或所有氫原子可經如上所述之㈣原子置 換.詳言之為Ci-C2鹵烷基,諸如氯甲基、溴曱基 '二氯 甲基、三氯甲基、氣甲農、-翁田I _卜 鼠T丞一鼠曱基、二鼠曱基、氣氟曱 基、二氣氟甲基、氯二氟甲基、卜氣乙基、i-溴甲基、^ 氟乙基、2-£乙基、2,2_二氣乙基、2,2,2_三氣乙基、2_氯_ 2-氟乙基、2-氯-2,2-二氟乙基、2,2-二氯_2_氣乙基、2,2,2_ 二氯乙基或五氟乙基'CVC3鹵烷基另外為(例如”丄卜三 氟丙-2-基、3,3,3-三氟丙基或七氟丙基。C^C4鹵烷基另外 為(例如)1-氯丁基、2-氯丁基、3-氣丁基或4_氣丁基。 (VCm羥烷基··具有}至2個(Ci_C2羥烷基)、個(Ci_ C4赵烧基)、2至4個(C2-C4經烧基)、1至6個(C「C6經烧 基)、2至6個(C2-C6經烧基)、1至8個(Cl_C8經烧基)、2至8 個(c2-c8經烧基)、丄至10個(Cl_Cl。經烧基)或2至1〇個(C2_ Ci〇經烷基)碳原子之直鏈或支鏈烷基(如上所述),其中至 少一個氫原子經羥基置換,諸如2-羥乙基或3-羥丙基。 稀基及稀氧基、稀硫基、稀基幾基及其類似物中之稀基 部分:具有2至4個(C2-C4烯基)、2至6個(C2-C6烯基)、2至8 個(C2-C8烯基)、3至8個(C3-C8烯基)、2至10個(C2-C1G烯基) 或3至1 〇個(C3-C1()烯基)碳原子及在任意位置處之雙鍵的單 不飽和直鏈或支鏈烴基,例如,C2-C4烯基,諸如乙烯 基、1-丙烯基、2-丙烯基、1-甲基乙烯基、1-丁烯基、2-丁烯基、3-丁烯基、1-曱基-1-丙烯基、2-甲基-1-丙烯基、 1-甲基-2-丙烯基或2-曱基-2-丙烯基,或例如,(:2-(:6烯 基’諸如乙烯基、1-丙烯基、2-丙烯基、1-曱基乙烯基、 149026.doc •13· 201103429 1-丁烯基、2-丁烯基、3-丁烯基、1-曱基-丨_丙烯基、2-甲 基-1-丙烯基、1-甲基-2-丙烯基、2-甲基-2-丙烯基、卜戊 烯基、2-戊烯基、3 -戊烯基、4-戊浠基、ι_甲基_1_ 丁稀 基、2-甲基-1-丁烯基、3·τ基-丨_ 丁烯基 ' 丨甲基_2 丁烯 基、2-甲基-2-丁烯基、3 -甲基-2-丁烯基、ι_曱基_3-丁稀 基、2-甲基-3-丁稀基、3-曱基-3-丁浠基、二甲基_2_丙 烯基、1,2-二曱基_1_丙烯基、ι,2·二曱基_2_丙烯基、卜乙 基-1-丙烯基、1-乙基-2-丙烯基、1-己烯基、2_己烯基、3-己烯基、4-己烯基、5-己烯基、1-曱基-丨—戊烯基、2-甲基- 1- 戊烯基、3-甲基-1-戊烯基、4-甲基-i_戊烯基、i_曱基-2-戊烯基、2-甲基-2-戊烯基、3 -曱基-2-戊烯基、4-甲基-2-戊烯基、1-曱基-3-戊烯基、2-曱基-3-戊烯基、3 -甲基-3-戊烯基、4-曱基-3-戊烯基、1-曱基_4_戊烯基、2-甲基-4-戊烯基、3 -曱基-4-戊烯基、4-曱基-4-戊烯基、1,1-二甲基- 2- 丁烯基、ι,ι·二曱基_3_ 丁烯基、j,2二曱基a-丁烯基、 1,2-二曱基-2-丁烯基、ι,2-二甲基·3· 丁烯基、ι,3-二曱基-卜丁烯基、1,3-二甲基丁烯基、i,3-二甲基_3_ 丁烯基、 2.2- 二甲基-3-丁烯基、2,3-二曱基_ι·丁烯基、2,3_二曱基-2-丁烯基、2,3-二甲基-3-丁烯基、3,3-二甲基-1-丁烯基、 3.3- 二曱基-2-丁烯基、1-乙基_丨·丁烯基、丨_乙基_2_ 丁烯 基、1-乙基-3-丁烯基、2-乙基-1-丁烯基、2-乙基-2-丁烯 基、2-乙基-3-丁烯基、l,l,2-三曱基_2_丙烯基、1-乙基-1-曱基-2-丙烯基、丨_乙基_2_曱基_丨-丙烯基、卜乙基_2_曱基_ 2-丙烯基及其類似物;K 1 4 明恭, 12 < 4 women's base, c2-c4 alkenyl 'c2_c4 block, c2_C4 tooth base, CM methoxy, CVCj methoxy, phenyl, stupid base, t last 2 The phenyl moiety in the reference group may have, 2, 3 1 149026.doc 201103429 or 5 substituents R9; COR1. , COOR10, CONR15R16 and S(0)pR10; each R9 is independently selected from the group consisting of halogen, hydrazine H, SH, NR15R16, CN, N 〇 2, 炫 "基, CVC4 - 炫, c2_c4, c2-C4 halene a group, a c2-c4 alkynyl group, a c2_c4_alkynyl group, a Ci_c4 alkoxy group, a Ci_c4 alkoxy group, a CrC4 alkylthio group, and a cardio-halohalothio group, wherein the aliphatic moiety in the above group may have 1, 2 Or 3 substituents Ris; each Ri? is independently selected from the group consisting of hydrogen, Ci_C4 alkyl, Cl_c4 haloalkyl, C2-C4 alkenyl, C2-C4 alkenyl, C丨_c4 aminoalkyl, phenyl, Phenyl-c "C4 alkyl" wherein the phenyl moiety of the last two mentioned groups may have 1, 2, 3, 4 or 5 substituents R9, and contain 1, 2 or 3 selected from hydrazine, a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic ring having a hetero atom of Ο and S as a ring member, wherein the heterocyclic ring may have 1, 2 or 3 substituents R9; each Ru is independently selected from halogen, 〇H, SH, NR15R16, CN, N02, CVC4 alkyl, CVC4 ixanyl, c2-c4 alkenyl, c2-c4 haloalkenyl, C2-C4 alkynyl, c2-C4 haloalkynyl, alkoxy , CVC4 haloalkoxy, CrC4 alkylthio and (^-(: 4-haloalkylthio), wherein the above group The aliphatic moiety may have 1, 2 or 3 substituents R18; R12 is selected from the group consisting of hydrogen, CVC decyl, c-c10 haloalkyl, CVCM alkoxy, CVCm haloalkoxy, Ci-Cw amine Alkyl, c3-C10 cycloalkyl, C3_C10 halocycloalkyl, phenyl, phenyl-Cl_c4 alkyl, wherein the phenyl moiety in the last two mentioned groups may have 1, 2, 3, 4 or 5 substituents R", containing 1, 2 or 3 heteroatoms selected from ruthenium, osmium and S 149026.doc 201103429 5- or 6-membered saturated, partially unsaturated or aromatic heterocycles as ring members, The heterocyclic ring may have an anthracene, 2 or 3 substituents R11, and NR, 5R16; R13 and R14 are independently selected from the group consisting of Cl_Cl〇 alkyl, Ci_c 〇 haloalkyl, c2_c10 dilute, c2-c1() Decenyl, c2-C1()alkynyl, C2-C1()halynyl, C3-C1G cycloalkyl, c3_ClG functional cycloalkyl, Ci_CiG alkoxy, CVCw alkoxy, Ci_c4_alkoxy _c〗 _ci 〇 alkyl, Ci_c4_alkoxy-CrCw alkoxy, d-Cw alkylthio, Ci-Cw haloalkylthio, C2-C1Q alkenyloxy, c2_c.1 ()-alkenylthio , c2_CiG alkynyloxy, C2-C1 (r alkynylthio, (: 3_CiG cycloalkoxy, c3_CiQ•cycloalkylthio, stupyl, phenyl-C i-C4 alkyl, phenylthio, phenyl-Cl_c4 alkoxy and NR15R16; each R15 is independently selected from hydrogen & Cl-c8 alkyl; each Ri6 is independently selected from hydrogen, Cl-C8 alkyl, benzene And phenyl-Cl_c4 alkyl; or R15 and R16 together form a straight chain (:^ or "alkylene bridge or group -CH2CH2OCH2CH2- or -CH2CH2NR丨7CH2CH2-; each R17 is independently selected from hydrogen and (^ -(:4 alkyl; * Each R18 is independently selected from the group consisting of nitro, CN, OH, SH, COR, COOR10, .conr15r16, nr15r16, c3-c6 cycloalkyl, c3-c6 i cycloalkyl, G -C4 alkoxy, c]-C4 haloalkoxy, c3-c6 cycloaloxy, phenyl and phenoxy; each R19 is independently selected from; 6 Schottky, CN, OH, SH, COR10, COOR10, CONR15R16, NR15R16, Ci_c4 alkyl, Ci_c4 dentate, c3_ H9026.doc -9- 201103429 c6 cycloalkyl, C3_C6 halocycloalkyl, c "c4 alkoxy, Cl-c4ii alkoxy, C3-c6 cycloalkoxy, phenyl and phenoxy; Q is hydrazine or S; M is a metal cation equivalent or an ammonium cation of the formula (NRaRbReRd)+, wherein Ra, Rb'RC and Rd are independently selected from each other Hydrogen, Ci_c丨〇 alkyl, phenyl and benzyl, of which the last two And the phenyl moiety in the group may have 1, 2 or 3 substituents independently selected from the group consisting of dentate, CN, nitro, Cl_C4 alkyl, Cl-C4 haloalkyl, Ci_C4 alkoxy, CVC4 Haloalkoxy and NR15R16; m is 0, 1 or 2; and P is 1 or 2. The invention also provides the use of a triazole compound of formula I and guanidine and/or an agriculturally acceptable salt thereof for controlling harmful fungi. The present invention further provides a fungicidal composition comprising the triazole compound of the above formula 1 and/or 11 (also and/or formula W; see below) and/or an agriculturally acceptable salt thereof and a suitable carrier. Suitable agriculturally acceptable carriers are described below. Compounds I and II may exist in one or more stereoisomeric forms. The various stereoisomers include enantiomers, diastereomers, singly isomers and geometric isomers. Those skilled in the art will appreciate that when one stereoisomer is concentrated relative to other stereoisomers or when separated from other stereoisomers, it may be more active and/or may exhibit beneficial effects. Additionally, the skilled artisan knows how to separate, enrich, and/or selectively prepare such stereoisomers. The compounds of the invention may be present as a mixture of stereoisomers [S] I49026.doc m 201103429 (e.g., a racemate), an individual stereoisomer, or an optically active form. It should be understood that the compounds απ are each position/double bond isomer H less in the case where the groups R6/R6a are the same. In the case where r6 (and of course R6a) is hydrogen, the respective compounds I and II are tautomers. δ Suitable agriculturally applicable salts are especially the salts of their cations or the acid addition salts of these acids. The cations and anions respectively have no side effects on the fungicidal action of the compounds. n Suitable cations are especially metal ions. Preferred are sodium and potassium ions; alkaline earth metal ions, preferably ions of calcium, magnesium and barium; and transition metal ions 'preferably manganese, and iron ions; and ammonium ions (if desired, they may have a Ci_c4 a pyridyl substituent and/or a phenyl or a sulfhydryl substituent), preferably isopropanyl, tetramethylammonium, tetrabutylammonium, diammonium benzylammonium, in addition to a scaly ion, a cerium ion, preferably three (Cl 匸 4 alkyl) ruthenium and ruthenium oxide ions, preferably tris(Ci_c4 alkyl) ruthenium oxide. Suitable anions of acid addition salts are mainly gas ions, bromide ions, fluoride ions, hydrogen sulfate, sulfate, dihydrogen phosphate, hydrogen phosphate, phosphate, nitrate, bicarbonate, carbonate, hexafluoride. An anion of citrate, hexafluorophosphate, and an anion of c丨-C:4 succinic acid, preferably formate, acetate, propionate and butyrate. It can be formed by reacting with a corresponding anion of hydrazine, preferably hydrochloric acid, hydrobromic acid, acid, phosphoric acid or nitric acid. In the definition of the variables given in the above formula, generally representative collective terms are used for the substituents in question. The term Cn_Cm denotes the number of possible carbon atoms in the substituent or substituent moiety in each case: halogen: fluorine, chlorine, bromine and iodine; »49026.doc 201103429 alkyl and alkoxy, alkoxy Alkyl, alkoxyalkoxy, alkylcarbonyl, thiomethyl, aminoalkyl, alkylamino, dialkylamino, alkylaminocarbonyl, dialkylaminocarbonyl, alkane An alkyl moiety in a thio group, an alkylsulfonyl group or the like: having 1 to 2 alkyl groups, 2 or 3 (C2-C3 alkyl groups), 1 to 4 (CVCU alkyl groups), 1 A saturated linear or branched hydrocarbon group of up to 6 (CrCe alkyl), 1 to 8 (CrC8 alkyl) or 1 to 10 (CrCw alkyl) carbon atoms. CyC: 3 alkyl is ethyl, n-propyl or isopropyl. The Cl_C2 alkyl group is a mercapto group or an ethyl group. C1-C4 alkyl is decyl, ethyl, propyl, isopropyl, butyl, 1-methylpropyl (second butyl), 2-methylpropyl (isobutyl) or 1,1 - dimethylethyl (t-butyl). The Cl-C6 alkyl group is additionally, for example, pentyl, 1-decylbutyl, 2-mercaptobutyl, 3-nonylbutyl, 2,2-dimercaptopropyl, 1-ethylpropane 1,1 -didecylpropyl, L2-dimercaptopropyl, hexyl, 1-decylpentyl, 2-methylpentyl, 3-mercaptopentyl, 4-methylpentyl, 1,1_-mercaptobutyl,-dimercaptobutyl, 1,3-dimethylbutyl, 2,2-dimercaptobutyl, 2,3-dimethylbutyl, 3,3- Dimercaptobutyl, 1-ethylbutyl, 2-ethylbutyl, ι,ι,2-trimethylpropyl, tridecylpropyl, 1-ethyl-1-mercaptopropyl or 1_ethyl 2 -methylpropyl. The Cl_c8 alkyl group is also additionally, for example, heptyl, octyl, 2-ethylhexyl and its positional isomers. The C?Cio alkyl group is also additionally, for example, an indenyl group, a fluorenyl group, a 2-propyl heptyl group, a 3-propylheptyl group, and a positional isomer thereof. Haloalkyl: having 1 to 2 (CVC2 functional alkyl), 1 to 3 haloalkyl) '1 to 4 (CVC4 alkyl), 1 to 6 (CVC6 halogen), 1 to 8 a linear or branched alkyl group (C, -C8_alkyl), 1 to 1 (Ci_Ci), or 2 to 1 ((2: C10) alkyl) Said), wherein some or all of the hydrogen atoms in the group such as 149026.doc •12·201103429 may be substituted by a (iv) atom as described above. In particular, Ci-C2 haloalkyl, such as chloromethyl, Bromoguanidino-dichloromethyl, trichloromethyl, gas-agriculture, -Wengtian I _ 鼠 丞 T丞- 曱 曱 、, 曱 曱 、, fluorofluoromethyl, di-fluoromethyl, chlor Fluoromethyl, b-ethyl, i-bromomethyl, fluoroethyl, 2-£ethyl, 2,2-dioxaethyl, 2,2,2_tris, ethyl 2-chloro 2-fluoroethyl, 2-chloro-2,2-difluoroethyl, 2,2-dichloro-2-ylethyl, 2,2,2-dichloroethyl or pentafluoroethyl 'CVC3 halane Further, the group is (for example, "trifluoropropyl-2-yl, 3,3,3-trifluoropropyl or heptafluoropropyl. C^C4 haloalkyl is additionally (for example) 1-chlorobutyl, 2 -Chlorobutyl, 3-oxobutyl or 4-tert-butyl. (VCm Alkyl·· has} to 2 (Ci_C2 hydroxyalkyl), one (Ci_C4 radix), 2 to 4 (C2-C4 burned), 1 to 6 (C "C6 burned") 2 to 6 (C2-C6 calcined), 1 to 8 (Cl_C8 calcined), 2 to 8 (c2-c8 calcined), hydrazine to 10 (Cl_Cl. calcined) or a linear or branched alkyl group of 2 to 1 (C2_Ci through alkyl) carbon atom (as described above) wherein at least one hydrogen atom is replaced by a hydroxyl group, such as 2-hydroxyethyl or 3-hydroxypropyl a dilute moiety in a dilute group and a dilute oxy group, a dilute thio group, a dilute yl group, and the like: having 2 to 4 (C2-C4 alkenyl) groups, 2 to 6 (C2-C6 alkenyl groups) 2 to 8 (C2-C8 alkenyl), 3 to 8 (C3-C8 alkenyl), 2 to 10 (C2-C1G alkenyl) or 3 to 1 (C3-C1() alkenyl a monounsaturated linear or branched hydrocarbon group having a carbon atom and a double bond at an arbitrary position, for example, a C2-C4 alkenyl group such as a vinyl group, a 1-propenyl group, a 2-propenyl group, a 1-methylvinyl group , 1-butenyl, 2-butenyl, 3-butenyl, 1-mercapto-1-propenyl, 2-methyl-1-propenyl, 1-methyl-2-propenyl or 2 - mercapto-2-propanoid Or, for example, (: 2-(:6 alkenyl) such as vinyl, 1-propenyl, 2-propenyl, 1-decylvinyl, 149026.doc •13·201103429 1-butenyl, 2 -butenyl, 3-butenyl, 1-decyl-fluorenyl-propenyl, 2-methyl-1-propenyl, 1-methyl-2-propenyl, 2-methyl-2-propenyl ,Pentenyl, 2-pentenyl, 3-pentenyl, 4-pentanyl, iota-methyl-1-butanyl, 2-methyl-1-butenyl, 3·τ-丨_butenyl' 丨methyl-2-butenyl, 2-methyl-2-butenyl, 3-methyl-2-butenyl, iota-yl-3-butanyl, 2- Methyl-3-butylenyl, 3-mercapto-3-butenyl, dimethyl-2-propenyl, 1,2-diindenyl-1-propenyl, iota, 2·didecyl _ 2-propenyl, ethyl-1-propenyl, 1-ethyl-2-propenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexene , 1-mercapto-fluorenyl-pentenyl, 2-methyl-1-pentenyl, 3-methyl-1-pentenyl, 4-methyl-i-pentenyl, i-fluorenyl -2-pentenyl, 2-methyl-2-pentenyl, 3-nonyl-2-pentenyl, 4-methyl-2-pentenyl, 1-decyl-3-pentenyl , 2-mercapto-3-pentenyl, 3 - 3-pentenyl, 4-mercapto-3-pentenyl, 1-decyl-4-enopentyl, 2-methyl-4-pentenyl, 3-mercapto-4-pentene Base, 4-mercapto-4-pentenyl, 1,1-dimethyl-2-butenyl, iota, ι-diyl-3-butenyl, j,2-didecyl a-butene 1,2-dimercapto-2-butenyl, iota, dimethyl-3-butenyl, iota, 3-didecyl-butenyl, 1,3-dimethyl Butenyl, i,3-dimethyl-3-butenyl, 2.2-dimethyl-3-butenyl, 2,3-diindenyl-ι-butenyl, 2,3-didecyl 2-butenyl, 2,3-dimethyl-3-butenyl, 3,3-dimethyl-1-butenyl, 3.3-dimercapto-2-butenyl, 1-B Base — 丨·butenyl, 丨_ethyl 2 —butenyl, 1-ethyl-3-butenyl, 2-ethyl-1-butenyl, 2-ethyl-2-butenyl , 2-ethyl-3-butenyl, l,l,2-trimethyl-2-propenyl, 1-ethyl-1-indenyl-2-propenyl, 丨_ethyl_2_曱a group of hydrazine-propenyl, acetophen-2-ylindolyl-2-propenyl and the like;

[SI 149026.doc • J4· 201103429 鹵稀基及鹵稀氧基、鹵稀基幾基及其類似物中之齒稀基 部分:具有2至4個(C2-C4i烯基)、2至6個(C2-C6鹵烯基)、 2至8個(CyC:8鹵烯基)或2至10個(C2-Ci〇鹵烯基)碳原子及在 任思位置處之雙鍵的不儉和直鍵或支鍵煙基(如上所述), 其中此%基團中之一些或所有氫原子可經如上所述之齒素 原子(尤其乾、氣及漠)置換’例如氯乙烯基、氣浠丙基及 其類似物; 炔基及炔氧基、炔硫基、炔基幾基及其類似物中之快基 部分.具有2至4個(C2-C4炔基)、2至6個(C2-C6炔基)' 2至8 個(C2-C8炔基)、3至8個(C3-C8炔基)、2至10個(C2-C1Q炔基) 或3至10個(C3_C 1〇炔基)碳原子及一或兩個在任意位置處之 參鍵的直鏈或支鏈烴基,例如,C2-C4炔基,諸如乙炔 基、1-丙炔基、2-丙快基、1-丁块基、2 -丁快基、3 -丁块 基或1-甲基-2-丙炔基,或例如,C2-C6快基,諸如乙快 基、1-丙快基、2-丙快基、1-丁快基、2-丁炔基、3-丁炔 基、1-甲基-2-丙炔基、1-戊炔基、2-戊炔基、3-戊炔基、 4-戊炔基、1-曱基-2-丁炔基、1-曱基-3-丁炔基、2-曱基-3-丁快基、3 -甲基-1-丁块基、1,1-二曱基-2-丙炔基、1-乙基_ 2-丙炔基、1-己炔基、2-己炔基、3-己炔基、4-己炔基、5-己炔基、1-曱基-2-戍炔基、1-曱基-3-戊炔基、1-曱基-4-戊炔基、2-曱基-3-戊炔基、2-曱基-4-戊炔基、3-甲基-1-戊炔基、3-曱基-4-戊炔基、4-甲基-1-戊炔基、4-曱基-2-戊炔基、1,1-二曱基-2-丁炔基、1,1-二曱基-3-丁炔基、 1,2-二曱基-3-丁炔基、2,2-二甲基-3-丁炔基、3,3-二曱基- 149026.doc •15- 201103429 1-丁炔基、1-乙基-2-丁炔基、1-乙基_3-丁炔基、2-乙基-3-丁炔基、1-乙基-1-曱基-2-丙快基及其類似物; 鹵炔基及il快氧基、齒快基炭基及其類似物中之齒炔基 部分:具有2至4個(C2-C4鹵炔基)、2至6個(C2-C6||炔基)、 2至8個(C2-C8ii炔基)或2至10個(C2-C10_炔基)碳原子及一 .或兩個在任,¾、位置處之參鍵的不飽和直鍵或支鍵煙基(如 上所述),其中此等基團中之一些或所有氫原子可經如上 所述之鹵素原子(尤其氟、氣及溴)置換; 環烧基及環烧氧基、環院基羰基及其類似物中之環烧基 部分:具有3至6個(CVC6環烷基)、:3至8個(C3-C8環烷基)或 3至10個(C3_C1G環烷基)碳環成員之單環飽和烴基,諸如, 環丙基、環丁基、環戊基、環己基、環庚基、環辛基、環 壬基及環癸基; 鹵環烷基及_環烷氧基、_環烷基羰基及其類似物中之 齒環烷基部分:具有3至6個(CVC6齒環烷基)、3至8個((:3_ Cs鹵環烷基)或3至10個(C3_C10鹵環烷基)碳環成員之單環 飽和經基(如上所述)’其中一些或所有氫原子可經如上所 述之鹵素原子(尤其氟、氣及溴)置換; 環晞基及環烯氧基、環稀基嫉基及其類似物令之環稀基 部分:具有3至6個(CVC:6環稀基)、3至8個(C3_c8環稀基)或 3至10個(C3-C1G環烯基)碳環成員之單環單不飽和烴基,諸 如環丙烯基、環丁烯基、環戊烯基、環己烯基、環庚烯 基、環辛烯基、環壬烯基及環癸烯基; 鹵環稀基及齒環烯氧基、函環稀基羰基及其類似物中之 149026.doc •16- 201103429 鹵環烯基部分:具有3至6個(CrC6鹵環烯基)、3至8個(<: 鹵環稀基)或3至10個(C3_C10鹵環烯基)碳環成員之單产 單不飽和烴基(如上所述)’其中一些或所有氫原子可經如 上所述之鹵素原子(尤其氟、氯及溴)置換; 環烧基- Ci-C2烧基:如上所述之(^_(^2烧基殘芙 其中一個氫原子經C3-C6環烷基置換。實例為環丙基甲 基、環丁基甲基、環戊基甲基、環己基甲基、環丙基丨乙 基、環丁基-1-乙基、環戊基-1-乙基、環己基乙基、環 丙基-2-乙基、環丁基-2-乙基、環戊基-2-乙基、環己基-2_ 乙基及其類似物。C3-C1()環烧基-Ci-C4烧基為如上所述之 Ci-c:4院基殘基,其中一個氫原子經C3_Cig環烷基置換。除 了彼等以上提及的基團之外,CrC6環烷基-Ci-q烷基之實 例亦為環庚基甲基、環辛基曱基、環壬基曱基、環癸基甲 基、環庚基-1-乙基、環辛基-1-乙基、環壬基_丨-乙基、環 癸基-1-乙基、環庚基-2-乙基、環辛基-2-乙基、環壬基_2· 乙基' 環癸基-2-乙基、環丙基_ι_丙基、環丙基_2_丙基、 環丙基-3-丙基、環丁基-i_丙基、環丁基_2_丙基、環丁基_ 3-丙基、環戊基-1-丙基、環戊基_2_丙基、環戊基_3丙 基、環己基-1-丙基、環己基-2-丙基、環己基-3-丙基、環 庚基-1-丙基、環庚基-2-丙基、環庚基_3_丙基、環辛基_ι_ 丙基、環辛基-2-丙基、環辛基_3_丙基、環壬基-1-丙基、 環壬基-2-丙基、環壬基-3-丙基、環癸基·ι·丙基、環癸基_ 2-丙基、環癸基-3-丙基、環丙基-丨·丁基、環丙基_2_ 丁 基、環丙基-3 -丁基、環丙基_4-丁基、環丁基-1-丁基、環 149026.doc •17- 201103429 丁基-2-丁基、環丁基-3-丁基、環丁基-4-丁基、環戊基 丁基、環戊基-2- 丁基、環戊基-3-丁基、環戊基_4_ 丁基、 環己基-1-丁基、環己基-2-丁基、環己基-3-丁基、環己基_ 4-丁基、環庚基-1-丁基、環庚基-2-丁基、環庚基_3-丁 基、%庚基-4-丁基、ί衣辛基-1-丁基、環辛基_2_丁基、環 辛基-3-丁基、環辛基-4-丁基、環壬基丁基、環壬基_2_ 丁基、環壬基-3-丁基、環壬基-4-丁基、環癸基_丨_丁基、 環癸基-2-丁基、環癸基-3-丁基、環癸棊·4-丁基及其類似 物。 C3,C6鹵環烧基-C】-C2院基:如上戶斤述之c! -C2烧基殘 基’其中一個氫原子經CrC6鹵環烷基置換。實例為^氣環 丙基曱基' 1-氣環丁基曱基、1-氣環戊基甲基、^氣環已 基甲基、1-氣環丙基-1-乙基、1-氣環丁基_丨_乙基、卜氣環 戊基-1-乙基、1-氣環己基-1-乙基、卜氣環丙基_2乙基、 κ氣環丁基-2-乙基、1-氣環戊基-2-乙基、1-氯環己基_2_ 乙基、2-氣環丙基甲基、2_氣環丁基曱基、孓氯環戊基曱 基、2-氣環己基甲基、2-氣環丙基-丨_乙基、2_氣環丁基^ 乙基、2-氣環戊基乙基、2_氣環己基乙基、孓氣環丙 基-2-乙基、2-氯環丁基-2-乙基、2-氣環戊基-2-乙基、2_ 氯環己基-2-乙基、1-氟環丙基曱基、丨_氟環丁基甲基、^ 氟環戊基甲基、卜氟環己基曱基、丨_氟環丙基_丨_乙基、卜 軋環丁基-1-乙基、1-氟環戊基_丨_乙基、丨·氟環己基_丨_乙 基、1-氟環丙基-2-乙基、1-氟環丁基_2_乙基、丨_氟環戊 基-2-乙基、丨_氟環己基_2•乙基、2_氟環丙基曱基、2_氟環 [S] 149〇26.d〇c •18· 201103429 丁基曱基、2-氟環戊基甲基、2-氟環己基曱基、2-氟環丙 基-1-乙基、2-氟環丁基-1-乙基、2-氟環戊基-1-乙基、2-氟環己基-1-乙基、2-氟環丙基-2-乙基、2-氟環丁基-2-乙 基、2-氟環戊基_2-乙基、2-氟環己基-2-乙基及其類似物。 。3-(:10鹵環烷基丨_c4烷基為如上所述之C丨-C4烷基殘基, 其中一個氫原子經(:3-(:10鹵環烷基置換。 烧氧基··經由氧連接之烷基^ 烷氧基為甲氧基或 乙氧基。C〗-C3烧氧基另外為(例如)正丙氧基或丨甲基乙氧 基(異丙氧基)。Ci-C:4烧氧基另外為(例如)丁氧基、丨_甲基 丙氧基(第二丁氧基)、2-甲基丙氧基(異丁氧基)或1}1_二曱 基乙氧基(第三丁氧基Cl_C6烷氧基另外為(例如)戊氧 基、1-甲基丁氧基、2-f基丁氧基、3_甲基丁氧基、u· 一甲基丙氧基、1,2-二甲基丙氧基、2,2~二甲基丙氧基、卜 乙基丙氧基、己氧基、丨_甲基戊氧基、2_曱基戊氧基、3_ 甲基戊氧基、4·甲基戊氧基、^―二甲基丁氧基、丨,2-二甲 基丁氧基、1,3-二甲基丁氧基、2,2_二甲基丁氧基、2,3_二 甲基丁氧基、3,3-二甲基丁氧基、卜乙基丁氧基、2_乙基 丁氧基、1,1,2-三甲基丙氧基、〗,2,2_三甲基丙氧基、卜乙 基-1-甲基丙氧基或!-乙基冬甲基丙氧基。Μ烷氧基另 外為(例如)庚氧基、辛氧基、2_乙基己氧基及其位置異構 體。C,-。。烷氧基另外為(例如)壬氧基、癸氧基及其位置 異構體。C2-C10烧氧基類似於氧基,但甲氧基除 夕卜0 ' 其經氟、氯、溴及/或 鹵烧氧基:如上所述之烷氧基 149026.doc -19- 201103429 換’較佳經氟部分或完全取代。c〗-c2鹵烷氧基為例如, OCH2F、〇CHF2、〇CF3、〇CH2Cn、0CHC12、0CC13、氣氟 曱氧基、二氣氟曱氧基、氣二氟曱氧基、2_氟乙氧基、2_ 氣乙氧基、2-溴乙氧基、2-碘乙氧基、2,2-二氟乙氧基、 2.2.2- 三氟乙氧基、2_氣·2·氟乙氧基、2_氣_2,2二氟乙氧 基、2,2-二氣-2-氟乙氧基、2,2,2-三氣乙氧基或〇C2f5。 Ci-C4 _烧氧基另外為例如,2_氟丙氧基、3_氟丙氧基、 2.2- 二氟丙氧基、2,3_二氟丙氧基、2_氣丙氧基、弘氣丙氧 基、2,3-二氣丙氧基、2_溴丙氧基、3_溴丙氧基、3,3,3_三 氟丙氧基、3,3,3-三氣丙氧基、OCH2_C2F5、〇CF2_c2F5、 1- (CH2F)-2-氟乙氧基、WCH2C1)_2_氣乙氧基、1(CH2Br)_ 2- 溴乙氧基、4_氟丁氧基、4_氣丁氧基、4_溴丁氧基或九 氟丁氧基。Ci-C6鹵烷氧基另外為例如,5·氟戊氧基、5_氯 戊氧基、5 -溴戊氧基、 己氧基、6-氣己氧基、 己氧基。 5- 峨戊氧基、十一氟戊氧基、6_氟 6- 溴己氧基、6·碘己氧基或十二氟 烯氧基··經 .經由氧原子連接的如上所述之烯基 ,例如,[SI 149026.doc • J4· 201103429 Toothed bases in halogenated and halooxy, halocarbyl and analogues thereof: having 2 to 4 (C2-C4i alkenyl), 2 to 6 (C2-C6 haloalkenyl), 2 to 8 (CyC: 8 haloalkenyl) or 2 to 10 (C2-Ci〇 haloalkenyl) carbon atoms and the double bond of the double bond at the position of Rens a direct bond or a bond radical (as described above), wherein some or all of the hydrogen atoms of the % group can be replaced by dentate atoms (especially dry, gas and desert) as described above, such as vinyl chloride, gas Mercaptopropyl and analogs thereof; fast radical moiety in alkynyl and alkynyloxy, alkynylthio, alkynyl and analogs thereof. 2 to 4 (C2-C4 alkynyl), 2 to 6 (C2-C6 alkynyl) '2 to 8 (C2-C8 alkynyl), 3 to 8 (C3-C8 alkynyl), 2 to 10 (C2-C1Q alkynyl) or 3 to 10 (C3_C a 1 〇 alkynyl) carbon atom and one or two straight or branched chain hydrocarbon groups at any position, for example, a C2-C4 alkynyl group, such as an ethynyl group, a 1-propynyl group, a 2-propanyl group , 1-butyryl, 2-butyryl, 3-butyryl or 1-methyl-2-propynyl, or for example C2-C6 fast radicals, such as ethyl bromide, 1-propanyl, 2-propanyl, 1-butanyl, 2-butynyl, 3-butynyl, 1-methyl-2-propyne , 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 1-indolyl-2-butynyl, 1-indolyl-3-butynyl, 2- Mercapto-3-butanyl, 3-methyl-1-butenyl, 1,1-dimercapto-2-propynyl, 1-ethyl-2-propynyl, 1-hexynyl , 2-hexynyl, 3-hexynyl, 4-hexynyl, 5-hexynyl, 1-indolyl-2-decynyl, 1-indolyl-3-pentynyl, 1-indole 4-pentynyl, 2-mercapto-3-pentynyl, 2-mercapto-4-pentynyl, 3-methyl-1-pentynyl, 3-mercapto-4-pentyne Base, 4-methyl-1-pentynyl, 4-mercapto-2-pentynyl, 1,1-didecyl-2-butynyl, 1,1-didecyl-3-butyne 1,2-dimercapto-3-butynyl, 2,2-dimethyl-3-butynyl, 3,3-didecyl- 149026.doc •15- 201103429 1-butynyl , 1-ethyl-2-butynyl, 1-ethyl-3-butynyl, 2-ethyl-3-butynyl, 1-ethyl-1-indenyl-2-propanyl and Analogs thereof; alkynyl moiety in a haloalkynyl group and an il-oxyl group, a tooth-based carbon group, and the like: having 2 to 4 (C) 2-C4 haloalkynyl), 2 to 6 (C2-C6||alkynyl), 2 to 8 (C2-C8ii alkynyl) or 2 to 10 (C2-C10-alkynyl) carbon atoms and one Or two inactive, 3⁄4, a positional unsaturated bond or a bond group (as described above), wherein some or all of the hydrogen atoms of such groups may pass through a halogen atom as described above ( In particular, fluorine, gas and bromine) substitution; cycloalkyl groups in the cycloalkyl and cycloalkoxy groups, ring-based carbonyl groups and the like: having 3 to 6 (CVC6 cycloalkyl groups), 3 to 8 a monocyclic saturated hydrocarbon group of (C3-C8 cycloalkyl) or 3 to 10 (C3_C1G cycloalkyl)carbocyclic members, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, ring Octyl, cyclodecyl and cyclodecyl; torsocycloalkyl moiety in halocycloalkyl and cycloalkoxy, cycloalkylcarbonyl and the like: having from 3 to 6 (CVC6 ring cycloalkyl) , 3 to 8 ((: 3_Cs halocycloalkyl) or 3 to 10 (C3_C10 halocycloalkyl) carbocyclic ring members of a monocyclic saturated meridine (as described above), some or all of which may be a halogen atom (especially fluorine) as described above Gas and bromine) substitution; cyclodecyl and cycloalkenyloxy, cycloazinyl thiol and the like thereof to give a ring-like moiety: 3 to 6 (CVC: 6 ring-dense), 3 to 8 ( a monocyclic monounsaturated hydrocarbon group of a C3_c8 cycloaliphatic) or 3 to 10 (C3-C1G cycloalkenyl) carbocyclic ring members, such as a cyclopropenyl group, a cyclobutenyl group, a cyclopentenyl group, a cyclohexenyl group, a ring Heptenyl, cyclooctenyl, cyclodecenyl and cyclodecenyl; halocyclo and ortho-alkenyloxy, functional ring dilute carbonyl and the like 149026.doc •16-201103429 halo ring Alkenyl moiety: a single production order having 3 to 6 (CrC6 halocycloalkenyl), 3 to 8 (<: halocyclo) or 3 to 10 (C3_C10 halocycloalkenyl) carbon ring members a saturated hydrocarbon group (as described above) wherein some or all of the hydrogen atoms may be replaced by a halogen atom as described above (especially fluorine, chlorine and bromine); a cycloalkyl group - Ci-C2 alkyl group: as described above (^_( ^2 A pyridyl group in which one of the hydrogen atoms is replaced by a C3-C6 cycloalkyl group. Examples are cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, cyclopropylphosphonium, cyclobutyl-1-ethyl, cyclopentyl-1-ethyl, cyclohexyl Ethyl, cyclopropyl-2-ethyl, cyclobutyl-2-ethyl, cyclopentyl-2-ethyl, cyclohexyl-2-ethyl and the like. The C3-C1()cycloalkyl-Ci-C4 alkyl group is a Ci-c:4-based residue as described above in which one hydrogen atom is replaced by a C3_Cig cycloalkyl group. In addition to the above-mentioned groups, examples of the CrC6 cycloalkyl-Ci-q alkyl group are also cycloheptylmethyl, cyclooctylfluorenyl, cyclodecylmercapto, cyclodecylmethyl, Cycloheptyl-1-ethyl, cyclooctyl-1-ethyl, cyclodecyl-丨-ethyl, cyclodecyl-1-ethyl, cycloheptyl-2-ethyl, cyclooctyl-2 -ethyl, cyclodecyl 2·ethyl 'cyclodecyl-2-ethyl, cyclopropyl_ι-propyl, cyclopropyl-2-propyl, cyclopropyl-3-propyl, ring Butyl-i-propyl, cyclobutyl-2-propyl, cyclobutyl-3-propyl, cyclopentyl-1-propyl, cyclopentyl-2-propyl, cyclopentyl-3 , cyclohexyl-1-propyl, cyclohexyl-2-propyl, cyclohexyl-3-propyl, cycloheptyl-1-propyl, cycloheptyl-2-propyl, cycloheptyl_3_ Propyl, cyclooctyl-yl-propyl, cyclooctyl-2-propyl, cyclooctyl_3-propyl, cyclodecyl-1-propyl, cyclodecyl-2-propyl, cyclodecyl 3-propyl, cyclodecyl·ι·propyl, cyclodecyl _ 2-propyl, cyclodecyl-3-propyl, cyclopropyl-fluorenyl butyl, cyclopropyl-2-butyl, Cyclopropyl-3-butyl, cyclopropyl-4-butyl, cyclobutyl-1-butyl, ring 149026.doc •17- 201103429 Butyl-2-butyl , cyclobutyl-3-butyl, cyclobutyl-4-butyl, cyclopentylbutyl, cyclopentyl-2-butyl, cyclopentyl-3-butyl, cyclopentyl_4_butyl , cyclohexyl-1-butyl, cyclohexyl-2-butyl, cyclohexyl-3-butyl, cyclohexyl-4-butyl, cycloheptyl-1-butyl, cycloheptyl-2-butyl Cycloheptyl-3-butyl, %heptyl-4-butyl, ε-octyl-1-butyl, cyclooctyl-2-butyl, cyclooctyl-3-butyl, cyclooctyl -4-butyl, cyclodecylbutyl, cyclodecyl-2-butyl, cyclodecyl-3-butyl, cyclodecyl-4-butyl, cyclodecyl-hydrazine-butyl, cyclodecyl 2-Butyl, cyclodecyl-3-butyl, cyclop-butyl 4-butyl and the like. C3, C6 halocycloalkyl-C]-C2, the base: as described above, c! -C2 alkyl residue, wherein one of the hydrogen atoms is replaced by a CrC6 halocycloalkyl group. Examples are gas cyclopropyl fluorenyl ' 1-cyclohexyl fluorenyl, 1-cyclopentylmethyl, oxacyclohexylmethyl, 1-cyclohexyl-1-ethyl, 1- Gas ring butyl 丨 乙基 ethyl, cyclohexane cyclopentyl-1-ethyl, 1-cyclohexyl-1-ethyl, cyclohexane propyl 2-ethyl, κ gas cyclobutyl -2- Ethyl, 1-cyclopentyl-2-ethyl, 1-chlorocyclohexyl-2-ethyl, 2-cyclohexylmethyl, 2-cyclopentyl fluorenyl, chlorocyclopentyl fluorenyl , 2-cyclohexylmethyl, 2-cyclohexyl-hydrazine-ethyl, 2-cyclopentylethyl, 2-cyclopentylethyl, 2-cyclohexylethyl, xenon Cyclopropyl-2-ethyl, 2-chlorocyclobutyl-2-ethyl, 2-cyclopentyl-2-ethyl, 2-chlorocyclohexyl-2-ethyl, 1-fluorocyclopropyl hydrazine Base, 丨-fluorocyclobutylmethyl, fluorocyclopentylmethyl, fluorocyclohexyl fluorenyl, hydrazine fluorocyclopropyl hydrazine 乙基 ethyl, hydrazine butyl-1-ethyl, 1-fluoro Cyclopentyl-indole-ethyl, fluorenylfluorocyclohexyl-indole-ethyl, 1-fluorocyclopropyl-2-ethyl, 1-fluorocyclobutyl-2-ethyl, hydrazine-fluorocyclopentyl -2-ethyl, 丨-fluorocyclohexyl 2•ethyl, 2-fluorocyclopropyl fluorenyl, 2-fluoro ring [S] 149 〇 26.d〇c • 18· 201 103429 butyl fluorenyl, 2-fluorocyclopentylmethyl, 2-fluorocyclohexyl decyl, 2-fluorocyclopropyl-1-ethyl, 2-fluorocyclobutyl-1-ethyl, 2-fluoro Cyclopentyl-1-ethyl, 2-fluorocyclohexyl-1-ethyl, 2-fluorocyclopropyl-2-ethyl, 2-fluorocyclobutyl-2-ethyl, 2-fluorocyclopentyl _2-Ethyl, 2-fluorocyclohexyl-2-ethyl and the like. . 3-(:10 halocycloalkylhydrazine-c4 alkyl is a C丨-C4 alkyl residue as described above, wherein one hydrogen atom is replaced by (:3-(:10 halocycloalkyl). - The alkyl group alkoxy group via an oxygen group is a methoxy group or an ethoxy group. The C-C3 alkoxy group is additionally, for example, n-propoxy or fluorenylmethylethoxy (isopropoxy). Ci-C: 4 alkoxy is additionally (for example) butoxy, 丨-methylpropoxy (second butoxy), 2-methylpropoxy (isobutoxy) or 1}1_ Dimercaptoethoxy (third butoxy Cl_C6 alkoxy group is additionally exemplified by, for example, pentyloxy, 1-methylbutoxy, 2-f-butoxy, 3-methylbutoxy, u · 1-Methylpropoxy, 1,2-dimethylpropoxy, 2,2-dimethylpropoxy, puethylpropoxy, hexyloxy, 丨-methylpentyloxy, 2_曱Pentyl pentyloxy, 3-methylpentyloxy, 4·methylpentyloxy, dimethyl butyloxy, hydrazine, 2-dimethylbutoxy, 1,3-dimethylbutoxy , 2,2-dimethylbutoxy, 2,3-dimethylbutoxy, 3,3-dimethylbutoxy, ethylideneoxy, 2-ethylbutoxy, 1,1 2-trimethylpropoxy , 〗 〖, 2,2_trimethylpropoxy, ethethyl-1-methylpropoxy or !-ethyl-whenylmethylpropoxy. The decyloxy group is additionally (for example) heptyloxy, octyloxy , 2-ethylhexyloxy and positional isomers thereof. C,-. Alkoxy is additionally, for example, a decyloxy group, a decyloxy group and a positional isomer thereof. C2-C10 alkoxy is similar In the oxy group, but the methoxy group is eve 0' which is via fluorine, chlorine, bromine and/or halogen alkoxy group: alkoxy group as described above 149026.doc -19- 201103429 for 'perfect fluorine partial or complete Substituted. c--c2 haloalkoxy is, for example, OCH2F, 〇CHF2, 〇CF3, 〇CH2Cn, 0CHC12, 0CC13, fluorofluoromethoxy, difluorofluoromethoxy, fluorodifluoromethoxy, 2_ Fluoroethoxy, 2-methoxyglycol, 2-bromoethoxy, 2-iodoethoxy, 2,2-difluoroethoxy, 2.2.2-trifluoroethoxy, 2_gas·2 Fluoroethoxy, 2_gas_2,2 difluoroethoxy, 2,2-dioxa-2-fluoroethoxy, 2,2,2-trisethoxy or guanidine C2f5. Further, C4 _ alkoxy is, for example, 2-fluoropropoxy, 3-fluoropropoxy, 2.2-difluoropropoxy, 2,3-difluoropropoxy, 2-propoxy, hongqi Propoxy, 2, 3-dipropoxy, 2-bromopropoxy, 3-bromopropoxy, 3,3,3-trifluoropropoxy, 3,3,3-tripropoxy, OCH2_C2F5, 〇CF2_c2F5 , 1-(CH2F)-2-fluoroethoxy, WCH2C1)_2_gas ethoxy, 1(CH2Br)_ 2-bromoethoxy, 4-fluorobutoxy, 4- methoxybutoxy, 4 _Bromobutoxy or nonafluorobutoxy. Ci-C6 haloalkoxy is additionally, for example, 5·fluoropentyloxy, 5-chloropentyloxy, 5-bromopentyloxy, hexyloxy, 6- Gas hexyloxy, hexyloxy. 5-峨-pentyloxy, undecafluoropentyloxy, 6-fluoro 6-bromohexyloxy, 6-iodohexyloxy or dodecafluoroaloxy-. via the oxygen atom as described above Alkenyl, for example,

-甲基_2-丁烯氧基、1- 149026.doc ^甲基-2- 丁烯氧 氧基、1-甲基-3- [S1 •20· 201103429 丁浠氧基、2-甲基-3_ 丁烯氧基、3_甲基_3_丁稀基、i山二 甲基-2-丙稀氧基、0二曱基小丙婦氧基、^二甲基_2· 丙烯氧基、1-乙基小丙烯氧基、κ乙基丙烯氧基、“己 烯氧基、2-己稀氧基、3_己烯氧基、4_己稀氧基、5_己稀 氧基、1-甲基-1-戊烯氧基、2_甲基小戊婦氧基、3_甲基· 1-戊稀氧基、4_甲基小戊稀氧基、丨_甲基_2•戊烯氧基、2· 曱基-2-戊烯氧基、3_甲基_2_戊烯氧基、4_甲基_2_戍稀氧 基、1-甲基I戊烯氧基、2_甲基·3·戍稀氧基、3•甲基_3· 戊烯氧基、4-f基_3_戊烯氧基、“甲基_4_戊烯氧基' 2_甲 基-心戊婦氧基、”基-4_戊婦氧基、4_甲基·4_戊稀氧 基、1,1_二f基-2-丁稀氧基、i山二甲基·3_丁稀氧基、 1,2_二曱基-1-丁烯氧基、基_2_丁稀氧基、以-二 甲基-3-丁稀氧基、以二甲基]•丁稀氧基、以二甲基I 丁烯氧基、1,3-二甲基_3_丁稀氧基、2,2·二甲基_3_丁稀氧 基、2,3-二甲基小丁烯氧基、2,3_二甲基·2_丁烯氧基、 2,3_二甲基-3-丁烯氧基、3,3_二曱基4 丁烯氧基、3,3·二 甲基-2·丁稀氧基、卜乙基·卜丁稀氧基、卜乙基_2_丁稀氧 基h乙基-3-丁烯氧基、2_乙基_丨_ 丁烯氧基、2·乙基 丁烯氧基2_乙基-3-丁烯氧基、ι,ι,2-三甲基_2_丙烯氧 基、1-乙基甲基_2_丙烯氧基、1-乙基-2-甲基-1-丙烯氧 基及1-乙基-2-曱基_2_丙烯氧基及其類似物; _稀氧基:如上所述之稀氧基,其經氟、氣、填及/或 碘,較佳經氟部分或完全取代。 一 炔氡基:經由氡原子連接的如上所述之炔基,例如, I49026.doc •21 · 201103429 C2-c1G炔氧基,諸如2_丙炔氧基、2_丁炔氧基、3_丁炔氧 基、1-甲基-2-丙炔氧基、2_戊炔氧基、3_戊炔氧基、4_戊 炔氧基、曱基_2_丁炔氧基、丨_甲基·3 丁炔氧基、2·甲 基-3-丁炔氧基、1-乙基_2_丙炔氧基、2_己炔氧基、3己炔 氧基' 4-己炔氧基、5_己炔氧基、甲基_2戍炔氧基、卜 甲基-3-戊炔氧基及其類似物; _炔氧基:如上所述之炔氧基,其經氟、氯、溴及/或 碘,較佳經氟部分或完全取代。 環烧氧基·經由氧原子連接的如上所述之環烧基,例 如’ C3-C1G環烧氧基或CpC:8環院氧基,諸如環丙氧基、環 戊氧基、環己氧基、環庚氧基、環辛氧基、環壬氧基、環 癸氧基及其類似物; 鹵環烷氧基:如上所述之環烷氧基,其經氟、氣、溴及/ 或碘,較佳經氟部分或完全取代。 環稀氧基:經由氧原子連接的如上所述之環稀基,例 如’ C3-C1G環烯氧基,C3-C8環烯氧基或較佳,c5-C6環烯 氧基’諸如環戊-1-烯氧基、環戊烯氧基、環己_丨_烯氧 基及環己-2-烯氧基; 烧氧基烧基:具有1至10個、1至8個、1至6個或1至4 個’尤其1至3個碳原子之如上所定義之烧基,其中一個氫 原子經具有1至8個、1至6個、1至4個或1至3個碳原子之院 氧基置換,例如,曱氧基曱基、2·甲氧基乙基、乙氧基甲 基、3-甲氧基丙基、3-乙氧基丙基及其類似物。 烷氧基烷氧基:具有1至1〇個、1至8個、1至6個或1至4-Methyl-2-butenyloxy, 1-149026.doc ^Methyl-2-butenoxyoxy, 1-methyl-3-[S1 •20· 201103429 Butanoxy, 2-methyl -3_butenyloxy, 3-methyl-3-indolyl, i-xyl dimethyl-2-propenyloxy, dioxin-based acetophenoxy, dimethyl-2-enyloxy , 1-ethyl propylene oxy, κ ethyl propylene oxy, "hexenyloxy, 2-hexyloxy, 3-hexenyloxy, 4-hexyloxy, 5-hexyloxy , 1-methyl-1-pentenyloxy, 2-methylpentanyloxy, 3-methyl-1-pentyloxy, 4-methylpentyloxy, 丨-methyl _2•pentenyloxy, 2·indol-2-pentenyloxy, 3-methyl-2-pentenyloxy, 4-methyl-2-indoleoxy, 1-methyl-I Alkenyloxy, 2-methyl·3·decyloxy, 3·methyl_3·pentenyloxy, 4-fyl-3-butenyloxy, “methyl-4-penteneoxy” ' 2 —Methyl-p-pentyloxy, phenyl-4-pentyloxy, 4-methyl-4-pentenyloxy, 1,1-di-f-yl-2-butanoxy, i Methylene-3,butoxyl, 1,2-didecyl-1-butenyloxy, benzyl-2-butanoxy, dimethyl-butenoxy Dimethyl]•butylene oxide With dimethyl I butyleneoxy, 1,3-dimethyl 3 - butyloxy, 2,2 dimethyl _ 3 - butyloxy, 2,3-dimethyl butyl Alkenyloxy, 2,3-dimethyl-2-butenyloxy, 2,3-dimethyl-3-butenyloxy, 3,3-diindolyl-4-butenyloxy, 3,3 · dimethyl-2·butoxy, ethyl, butyloxy, ethyl-2-butanoxyhethyl-3-butenyloxy, 2-ethyl-oxime-butenyloxy 2, ethylbutenyloxy 2_ethyl-3-butenyloxy, ι,ι,2-trimethyl-2-propenyloxy, 1-ethylmethyl-2-propenyloxy, 1-ethyl-2-methyl-1-propenyloxy and 1-ethyl-2-indolyl-2-propenyloxy and the like; _thinoxy: a diloxy group as described above, Fluorine, gas, and/or iodine, preferably partially or completely substituted by fluorine. Alkynyl group: an alkynyl group as described above attached via a ruthenium atom, for example, I49026.doc • 21 · 201103429 C2-c1G alkyne Oxyl group, such as 2-propynyloxy, 2-butynyloxy, 3-butynyloxy, 1-methyl-2-propynyloxy, 2-pentynyloxy, 3-pentynyloxy , 4_pentynyloxy, fluorenyl-2-butynyloxy, 丨-methyl·3 butynyloxy, 2· Methyl-3-butynyloxy, 1-ethyl-2-propynyloxy, 2-hexynyloxy, 3hexynyloxy '4-hexynyloxy, 5-hexynyloxy, A Alkynyloxy, benzyl-3-pentynyloxy and the like; _alkynyloxy: alkynyloxy as described above, which is preferably fluorine, chlorine, bromine and/or iodine, preferably fluorine Partially or completely replaced. a cycloalkyloxy group, a cycloalkyl group as described above attached via an oxygen atom, such as 'C3-C1G ring alkoxy or CpC: 8 ring alkoxy, such as cyclopropoxy, cyclopentyloxy, cyclohexyloxy a group, a cycloheptyloxy group, a cyclooctyloxy group, a cyclodecyloxy group, a cyclodecyloxy group and the like; a halocycloalkoxy group: a cycloalkoxy group as described above, which is fluorine, gas, bromine and/or Or iodine, preferably partially or completely substituted by fluorine. Cyclooxyl: a cycloaliphatic group as described above attached via an oxygen atom, such as 'C3-C1G cycloalkenyloxy, C3-C8 cycloalkenyloxy or preferably, c5-C6 cycloalkenyloxy' such as cyclopentane 1-enyloxy, cyclopentenyloxy, cyclohexanyloxy and cyclohex-2-enyloxy; alkoxyalkyl: 1 to 10, 1 to 8, 1 to 6 or 1 to 4 groups of alkyl groups as defined above, especially 1 to 3 carbon atoms, wherein one hydrogen atom has 1 to 8, 1 to 6, 1 to 4 or 1 to 3 carbon atoms The oxy group is substituted, for example, a decyloxy group, a methoxyethyl group, an ethoxymethyl group, a 3-methoxypropyl group, a 3-ethoxypropyl group, and the like. Alkoxyalkoxy: having 1 to 1 、, 1 to 8, 1 to 6, or 1 to 4

[SI 149026.doc •22- 201103429 個,尤其1至3個碳原子之如上所定義之烷氧基,其中一個 氫原子經具有1至8個、1至6個或尤其丨至4個碳原子之烷氧 基置換,例如,2-甲氧基乙氧基、2_乙氧基乙氧基、3_甲 氧基丙氧基、3 -乙氧基丙氧基及其類似物。 烷基羰基:式R-CO-之基團,其中R為如上所定義之烷 基,例如,q-Cw烧基、Cl-c8烧基、c丨_C6院基、Ci_c^ 基' q-C2烷基或CVC4烷基。實例為乙醯基、丙醯基及其 類似物。CrC4烷基羰基之實例為丙基羰基、異丙基羰 基、正丁基羰基、第二丁基羰基、異丁基羰基及第三丁基 艘基。 鹵烷基羰基:式R-CO-之基團,其中汉為如上所定義之 鹵烷基,例如,Cl-Cloi烷基、Ci_Cs鹵烷基、Ci_C6齒烷 基、c〗-c4_烷基、Cl_c2_烷基或c3_c4自烷基。實例為二 氟甲基羰基、三氟甲基羰基、2,2-二氟乙基羰基、2,2,3_三 氟乙基幾基及其類似物。 烷氧羰基:式R-CO-之基團,其中R為如上所定義之烷 氧基,例如,Cl_ClQ烷氧基、Ci_Cs烷氧基、c】_c6烷2 基、CrC4烷氧基或Ci_C2烷氧基。Ci_C4烷氧羰基之實例為 甲氧幾基乙氧幾基、丙氧幾基、異丙氧幾基、正丁氧幾 基、第二丁氧羰基、異丁氧羰基及第三丁氧羰基。 齒烷氧羰基:式R-CO-之基團,其中r為如上所定義之 函烧氧基,例如,C1_C10鹵烧氧基、C1U院氧基' c6_烷氧基、Ci_C4齒烷氧基或Ci_C2齒烷氧基。Ci_c碥烷 氧羰基之實例為二氟曱氧羰基、三氟曱氧羰基、2,2-二氟 149026.doc •23· 201103429 乙氧羰基、2,2,3-三氟乙氧羰基及其類似物。 烷基胺基羰基:式R-NH-CO-之基團,其中r為如上所定 義之烷基’例如’(VCiq烷基、C丨-C8烷基、C丨-C6烷基、 C「C4烷基、(VC2烷基或C3-C4烷基。CVC4烷基胺基羰基 之實例為甲基胺基羰基、乙基胺基羰基、丙基胺基羰基' 異丙基胺基羰基、丁基胺基羰基、第二丁基胺基羰基、異 丁基胺基羰基及第三丁基胺基羰基。 二烷基胺基羰基:式RR’N-CO-之基團,其中R及R'彼此 獨立地為如上所定義之烷基,例如,Ci_Ciq烷基、 基、C〗-C6烧基、c丨-C4烧基、c丨-c2烧基或c3-c4烧基。二-(C「C4烷基)-胺基羰基之實例為二曱基胺基羰基、二乙基 胺基幾基、二丙基胺基羰基、二異丙基胺基羰基及二丁基 胺基羰基。 胺基烧基:式R-NH2之基團,其中R為如上所定義之烷 基’例如’ CVCm烧基、C丨-C8院基、CVC6烧基、(VC4炫 基、Ci-C2烧基或C3-C4烷基。實例為胺基甲基、丨_及2-胺 基乙基、1-、2-及3-胺基丙基、i_及2-胺基1-曱基乙基、1_ 、2-、3-及4-胺基丁基及其類似物。 烧基磺醯基:式R-S(0)2-之基團,其中r為如上所定義 之院基,例如’ C丨·Ch>烷基、CVC8烷基、CVC6烧基、C,-C4院基或C^-C2烷基^ 烷基磺醯基之實例為甲磺醯 基、乙續酿基、丙磺醯基、異丙磺醯基、正丁磺醯基、第 二丁續醯基、異丁續醯基及第三丁續醯基。 烧硫基:經由硫原子連接的如上所定義之烷基。 149026.doc •24- 201103429 鹵烷硫基:經由硫原子連接的如上所定義之齒烷基。 稀硫基:經由硫原子連接的如上所定義之稀基。 鹵稀硫基:經由硫原子連接的如上所定義之_稀基。 炔硫基:經由硫原子連接的如上所定義之炔基。 鹵快硫基:經由硫原子連接的如上所定義之齒炔基。 環烧硫基:經由硫原子連接的如上所定義之環烧基。 芳基為含有6至16個碳原子作為環成員之碳環芳族單環 或多環。實例為苯基、萘基、葱基、菲基、第基及奠基。 芳基較佳為苯基或萘基,且尤其為苯基。 苯基_Cl_C4烧基·· Cl_C4烧基(如上所定義),其中一個氫 原子經苯基置換,諸”基、苯乙基及其類似物。 苯基-C丨-C4烧氧基:@ / r , _ &、…[SI 149026.doc • 22-201103429, especially alkoxy groups as defined above for 1 to 3 carbon atoms, wherein one hydrogen atom has from 1 to 8, 1 to 6, or especially to 4 carbon atoms The alkoxy group is substituted, for example, 2-methoxyethoxy, 2-ethoxyethoxy, 3-methoxypropoxy, 3-ethoxypropoxy and the like. Alkylcarbonyl: a group of the formula R-CO- wherein R is an alkyl group as defined above, for example, q-Cw alkyl, Cl-c8 alkyl, c丨_C6, and Ci_c^'q- C2 alkyl or CVC4 alkyl. Examples are ethyl acetyl, propyl thiol and the like. Examples of the CrC4 alkylcarbonyl group are a propylcarbonyl group, an isopropylcarbonyl group, a n-butylcarbonyl group, a second butylcarbonyl group, an isobutylcarbonyl group and a tert-butyl group. Haloalkylcarbonyl: a group of the formula R-CO-, wherein Han is a haloalkyl group as defined above, for example, Cl-Cloi alkyl, Ci_Cs haloalkyl, Ci_C6 dentate alkyl, c--c4-alkyl , Cl_c2_alkyl or c3_c4 from alkyl. Examples are difluoromethylcarbonyl, trifluoromethylcarbonyl, 2,2-difluoroethylcarbonyl, 2,2,3-trifluoroethylthio and the like. Alkoxycarbonyl: a group of the formula R-CO-, wherein R is alkoxy as defined above, for example, Cl_ClQ alkoxy, Ci_Cs alkoxy, c)-c6 alkane 2, CrC4 alkoxy or Ci_C2 alkane Oxygen. Examples of the Ci_C4 alkoxycarbonyl group are a methoxycarbonyloxymethyl group, a propoxymethyl group, an isopropoxymethyl group, a n-butoxymethyl group, a second butoxycarbonyl group, an isobutoxycarbonyl group and a third butoxycarbonyl group. P-Alkyloxycarbonyl: a group of the formula R-CO-, wherein r is a functional alkoxy group as defined above, for example, C1_C10 halo-oxyloxy, C1U- tothoxy' c6-alkoxy, Ci_C4 aldentyloxy Or Ci_C2 tooth alkoxy. Examples of the Ci_c-decaneoxycarbonyl group are difluorofluorenyloxycarbonyl, trifluorosulfonyloxycarbonyl, 2,2-difluoro 149026.doc • 23·201103429 ethoxycarbonyl, 2,2,3-trifluoroethoxycarbonyl and analog. Alkylaminocarbonyl: a group of the formula R-NH-CO-, wherein r is alkyl as defined above, eg, 'VCiq alkyl, C丨-C8 alkyl, C丨-C6 alkyl, C" C4 alkyl, (VC2 alkyl or C3-C4 alkyl. Examples of CVC4 alkylaminocarbonyl are methylaminocarbonyl, ethylaminocarbonyl, propylaminocarbonyl 'isopropylaminocarbonyl, butyl Alkylaminocarbonyl, a second butylaminocarbonyl, an isobutylaminocarbonyl and a tert-butylaminocarbonyl. A dialkylaminocarbonyl: a group of the formula RR'N-CO-, wherein R and R 'Alternately, each other is an alkyl group as defined above, for example, Ci_Ciq alkyl, yl, C-C6 alkyl, c丨-C4 alkyl, c丨-c2 alkyl or c3-c4 alkyl. Examples of C "C4 alkyl"-aminocarbonyl are dinonylaminocarbonyl, diethylamino, dipropylaminocarbonyl, diisopropylaminocarbonyl and dibutylaminocarbonyl. Aminoalkyl group: a group of the formula R-NH2, wherein R is an alkyl group as defined above, for example, 'CVC m alkyl, C丨-C8, CVC6 alkyl, (VC4, thio, Ci-C2 alkyl) Or a C3-C4 alkyl group. Examples are aminomethyl, hydrazine and 2-aminoethyl, 1-, 2- and 3-aminopropyl, i- and 2-amino 1-nonylethyl, 1-, 2-, 3- and 4-aminobutyl and the like. a group of RS(0)2- wherein r is a deutero group as defined above, for example 'C丨·Ch> alkyl, CVC8 alkyl, CVC6 alkyl, C, -C4 or C^-C2 alkane Examples of alkylsulfonyl groups are methanesulfonyl, ethyl, propylsulfonyl, isopropylsulfonyl, n-butylsulfonyl, second sulfhydryl, isobutyl sulfhydryl and The third alkyl group is a thiol group: an alkyl group as defined above which is bonded via a sulfur atom. 149026.doc •24- 201103429 Haloalkylthio: a t-alkyl group as defined above attached via a sulfur atom. Base: a dilute group as defined above attached via a sulfur atom. Halogenthio group: a dilute group as defined above attached via a sulfur atom. Alkynylthio group: an alkynyl group as defined above attached via a sulfur atom. Thio group: a treadyl group as defined above attached via a sulfur atom. A cycloalkyl group: a cycloalkyl group as defined above attached via a sulfur atom. An aryl group is a carbocyclic ring having 6 to 16 carbon atoms as a ring member. Aromatic single Or polycyclic. Examples are phenyl, naphthyl, onion, phenanthryl, yl and base. The aryl is preferably phenyl or naphthyl, and especially phenyl. phenyl_Cl_C4 alkyl ··Cl_C4 a group (as defined above) wherein one hydrogen atom is replaced by a phenyl group, a benzyl group, a phenethyl group and the like. Phenyl-C丨-C4 alkoxy group: @ / r , _ &,...

、5-、6-或7_員飽和、部分不飽和或最大不飽和, 5-, 6- or 7_ member saturated, partially unsaturated or maximal unsaturated

149026.doc 〜…外丁取言頁雜原子的基團及視情 C(=〇)及C(=S)之基團作為環成員: 201103429 -3-或4-員飽和或部分不飽和雜環(下文中亦稱為雜環 基),其含有1、2或3個來自由氧、氮(以N*NR之形式) 及硫(以S、SO或S〇2之形式)組成之群的雜原子及視情況 可選的1或2個選自C(=0)及C(=s)之基團作為環成員:例 如’單環飽和或部分不飽和雜環,除碳環成員之外,其 亦含有1至3個氮原子及/或1個氧或硫原子或i或2個氧及/ 或硫原子及視情況可選的1或2個選自c(=〇)及c(=S)之基 團’例如2-環氧乙基、2-硫雜環丙基、^或入氮丙啶 基、1-、2 -或3 -氮雜環丁基, -5-或6-員飽和或部分不飽和雜環(下文中亦稱為雜環 基),其含有1、2或3個來自由氧、氮(以N* NR之形式) 及硫(以S、SO或S〇2之形式)組成之群的雜原子及視情況 可選的1或2個選自C(=0)及C(=S)之基團作為環成員:例 如’單環飽和或部分不飽和雜環,除碳環成員之外,其 亦含有1至3個氮原子及/或1個氧或硫原子或一或兩個氧 及/或硫原子及視情況可選的1或2個選自c(=〇)及c(=s) 之基團,舉例而言’ 2_四氫呋喃基、3_四氫呋喃基、3_ 四氫呋喃-2-酮基、4-四氫呋喃-2-酮基、5·四氫吱喃-2_ 酮基、2_四氫呋喃-3-酮基、4_四氩呋喃_3_酮基、5_四氫 呋喃-3-酮基、2-四氫噻吩基、3-四氫噻吩基、3-四氫噻 吩-2-酮基、4-四氫噻吩-2-_基、5_四氫噻吩_2_酮基、 2- 四氫噻吩-3-銅基、4·四氫噻吩_3_酮基、5_四氫。塞吩_ 3- 酮基、2-吡咯啶基、3-吡咯啶基、丨_吡咯啶酮基、 3-吡咯啶-2-酮基、4-吡咯啶_2_酮基、5_吡咯啶_2_酮 t S1 149026.doc •26- 201103429 基、1-吡咯啶-3-酮基、2-吡咯啶-3-酮基、4-吡咯啶-3-酮基、5 - °比咯。定-3 -酮基、1 -D比洛咬-2,5 -二酮基、3 -。比0各 啶-2,5-二酮基、3-異噁唑啶基、4-異噁唑啶基、5-異噁 唑啶基、3-異噻唑啶基、4-異噻唑啶基、5-異噻唑啶 基、3 -。比°坐°定基、4 - °比°坐咬基、5 - °比α坐°定基、2 -。惡。坐〇定 基、4 -α惡。坐σ定基、5 - °惡。坐D定基、2 -α塞。坐。定基、4 -D塞。坐π定 基、5 -α塞。坐σ定基、2 -。米α坐咬基、4 -咪。坐α定基、1,2,4 -11 惡二 唑啶-3-基、1,2,4-噁二唑啶-5-基、1,2,4-噻二唑啶-3-基、1,2,4-噻二唑啶-5-基、1,2,4-三唑啶-3-基、1,3,4-噁 二唾咬-2-基、1,3,4-°塞二吐咬-2-基、1,3,4-三唾咬-2-基、2,3 -二鼠α夫喃-2 -基、2,3 -二氮。夫喃-3 -基、2,4 -二風 咬喃-2 -基、2,4 -二里^夫喃-3 -基、2,3 -二氮。塞吩-2-基、 2,3 -二氮α塞吩-3-基、2,4 -二鼠。塞吩-2-基、2,4 -二氮。塞吩-3 -基、2 -。比略琳-2 -基、2 - 匕略咐 - 3 -基、3 -。比略·咐 - 2 -基、 3- 吡咯啉-3-基、2-異噁唑啉-3-基、3-異噁唑啉-3-基、4-異噁唑啉-3-基、2-異噁唑啉-4-基、3-異噁唑啉-4-基、 4- 異噁唑啉-4-基、2-異噁唑啉-5-基、3-異噁唑啉-5-基、4-異噁唑啉-5-基、2-異噻唑啉-3-基、3-異噻唑啉-3-基、4-異噻唑啉-3-基、2-異噻唑啉-4-基、3-異噻唑 啉-4-基、4-異噻唑啉-4-基、2-異噻唑啉-5-基、3-異噻 唑啉-5-基、4-異噻唑啉-5-基、2,3-二氫吡唑-1-基、2,3-二氮D比唾·_2 -基、2,3 -二氮°比唾-3 -基、2,3 -二氮。比。坐-4-基、2,3 -二氣°比°坐-5 -基、3,4 -二氮。比α坐-1 -基、3,4 -二氮 0比σ坐-3-基、3,4-二氫°比。坐-4-基、3,4-二氫α比。坐-5-基、 149026.doc -27- 201103429 4,5 -二氫D比唾-1 -基、4,5 -二氫。比。坐-3 -基、4,5 -二氫。比。坐-4-基、4,5-二氫吡唑-5-基、2,3-二氫噁唑-2-基、2,3-二 氫°惡。坐-3-基、2,3-二氫°惡唾-4-基、2,3-二氫°惡。坐-5-基、 3,4-二氫噁。坐-2-基、3,4-二氫。惡唾-3-基、3,4-二氫°惡。坐-4-基、3,4-二氫噁唑-5-基、3,4-二氫噁唑-2-基、3,4-二 氫°惡α坐-3 -基、3,4 -二氫°惡。坐-4 -基、2 -娘。定基、3 -旅咬 基、4-°底π定基、1,3 -二α惡烧-5-基、2 -四氮α底喃基、4-四 氫°底喃基、2-四氫。塞吩基、3-六氫噠°秦基、4-六氫噠嗪 基、2-六氫。密咬基、4-六氫°密。定基、5-六氫°密°定基、2-0底嘻基、1,3,5-六鼠二°秦-2-基及1,2,4-六氮二嘻-3-基以 及相應的-亞基; -含有1、2或3個來自由氧、氮及硫組成之群的雜原子作 為環成員的7員飽和或部分不飽和雜環:例如,具有7個 環成員之單環及雙環雜環,除碳環成員之外,其亦含有 1至3個氮原子及/或一個氧或硫原子或一或兩個氧及/或 硫原子,舉例而言,四氫氮呼基及六氫氮呼基,諸如 2,3,4,5-四氫[1Η]氮呼-1-、 -2-、 -3- ' -4- ' -5- 、 -6-或 -7- 基、3,4,5,6-四氫[2Η]氮呼 -2-、 -3- 、-4-、 -5- 、 -6-或 -7- 基、2,3,4,7-四氫[111]氮呼 -1- ' -2- 、-3-、 -4- 、 -5-、 -6- 或-7-基、2,3,6,7-四氫[1Η]氮呼 -1- ' -2- ' -3- 、 -4-、 -5- 、-6 -或-7-基、六鼠氣呼-1-、-2-、-3 -或-4 -基,四氮氧 呼基及六氫氧呼基,諸如2,3,4,5-四氫[1Η]氧呼-2-、-Β-λ -4- 、 -5- 、 -6-或-7-基、 2,3,4,7-四氫 [1Η] 氧呼-2-、-3-、-4-、-5-、-6 -或-7-基、2,3,6,7-四氮[1Η]氧呼-2-、-3- [S] 149026.doc • 28 - 201103429 或·7-基,六氫氮呼_1 -4- -2- 讨· - -3-或 _4- 基’四-及六氯急σ承技 ,一氮呼基、四-及六氫-Μ-二氮呼 基、四-及六氣-1 3 - 〇亞急成盆 ,心氮千基、四-及六氫-Μ-噁氮呼 基、四·及六風_ 1 3 ·-费口巫且 , 氧千基、四-及六氫·1,4-二氧呼Α 及相應的-亞基。 干土 含有1、2或3個選自由氧、氮及硫組成之群的雜原子的 5-或6·員芳族(=最大不飽和)雜環(=雜芳族基團),例 如’經由碳連接且含有⑴個氮原子或個氮原子及 1個硫或氧原子作為環成員的5_Μ雜芳《,諸如2十南 基、3-呋喃基、2_噻吩基、夂噻吩基、孓吡咯基、3吡 咯基、3-異噁唑基、4_異噁唑基、5_異噁唑基、%異噻 唑基、4-異噻唑基、5_異噻唑基、3_吡唑基、4_吡唑 基5 -。比。坐基、2 - °惡。坐基、4 - °惡唾基、5 - °惡唾基、2 0塞 唑基、4-噻唑基、5_噻唑基、2-咪唑基、4-咪唑基、 1,2,4-噁二唑 _3-基、1,2,4-噁二唑-5-基、1,2,4-噻二唑 _3 基、1,2,4-噻二唑-5-基、1,2,4-三唑-3-基、1,3,4_ 噁二唑 2-基、1,3,4-噻二唑-2-基及1,3,4-三唑_2_基;經由氮連 接且含有1至3個氮原子作為環成員之5 -員雜芳式, 土 ’睹149026.doc ~... The external group reads the hetero atom of the page and the group of C(=〇) and C(=S) as the ring member: 201103429 -3- or 4-member saturated or partially unsaturated a ring (hereinafter also referred to as a heterocyclic group) containing 1, 2 or 3 groups derived from oxygen, nitrogen (in the form of N*NR) and sulfur (in the form of S, SO or S〇2) a hetero atom and, optionally, 1 or 2 groups selected from C(=0) and C(=s) as ring members: for example, a 'monocyclic saturated or partially unsaturated heterocyclic ring, except for a carbon ring member In addition, it also contains 1 to 3 nitrogen atoms and/or 1 oxygen or sulfur atom or i or 2 oxygen and/or sulfur atoms and optionally 1 or 2 selected from c(=〇) and c a group of (=S) such as 2-epoxyethyl, 2-thiopropyl, or aziridine, 1-, 2- or 3-azetidinyl, -5- or a 6-membered saturated or partially unsaturated heterocyclic ring (hereinafter also referred to as a heterocyclic group) containing 1, 2 or 3 derived from oxygen, nitrogen (in the form of N* NR) and sulfur (in S, SO or a hetero atom of the group consisting of S〇2 and optionally 1 or 2 groups selected from C(=0) and C(=S) as ring members: for example Monocyclic saturated or partially unsaturated heterocyclic ring containing, in addition to a carbon ring member, 1 to 3 nitrogen atoms and/or 1 oxygen or sulfur atom or one or two oxygen and/or sulfur atoms and optionally One or two selected from the group consisting of c(=〇) and c(=s), for example, '2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 3-tetrahydrofuran-2-one, 4-tetrahydrofuran-2 -keto,5-tetrahydrofuran-2-yl, 2-tetrahydrofuran-3-one, 4-tetrahydrofuran-3-yl, 5-tetrahydrofuran-3-one, 2-tetrahydrothiophenyl , 3-tetrahydrothiophenyl, 3-tetrahydrothiophen-2-one, 4-tetrahydrothiophen-2-yl, 5-tetrahydrothiophene-2-keto, 2-tetrahydrothiophene-3-copper Base, 4·tetrahydrothiophene-3-olone, 5-tetrahydrogen. Steroid -3- 3-keto, 2-pyrrolidinyl, 3-pyrrolidinyl, 丨-pyrrolidone, 3-pyrrolidin-2-one, 4-pyrrolidine-2-one, 5-pyrrole Pyridin-2-one t S1 149026.doc •26- 201103429 base, 1-pyrrolidin-3-one, 2-pyrrolidin-3-one, 4-pyrrolidin-3-one, 5-° ratio Oops. D--3-keto, 1-D-Bisto-2,5-diketonyl, 3-. Ratio 0 pyridine-2,5-dione, 3-isoxazolidinyl, 4-isoxazolidinyl, 5-isoxazolidinyl, 3-isothiazolidinyl, 4-isothiazolidinyl , 5-isothiazolidinyl, 3-. More than ° ° ° base, 4 - ° ratio ° sit bite, 5 - ° than α sitting ° base, 2 -. evil. Sitting on the base, 4 -α evil. Sit σ foundation, 5 - ° evil. Sit D base, 2 - alpha plug. sit. Fixed base, 4-D plug. Sit π-base, 5-α plug. Sit σ base, 2 -. Rice α sits on the base, 4 - microphone. Αα定,1,2,4 -11oxadiazolidin-3-yl, 1,2,4-oxadiazolidine-5-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazolidine-5-yl, 1,2,4-triazolidine-3-yl, 1,3,4-oxadipine-2-yl, 1,3,4- °Sebutin-2-yl, 1,3,4-triseptin-2-yl, 2,3-di-rat alpha-furan-2-yl, 2,3-dinitrogen. Furan-3-yl, 2,4-di- 2, 2,4,2,2,2,2,2,2,2,2 Desphen-2-yl, 2,3-diaza α-sent-3-yl, 2,4-dimur. Cet-2-yl, 2,4-dinitrogen. Cephen-3-yl, 2-. Tbilisi-2 - base, 2 - 匕 咐 - 3 - base, 3 -.比 咐 咐 - 2 -yl, 3-pyrolin-3-yl, 2-isoxazolin-3-yl, 3-isoxazolin-3-yl, 4-isoxazolin-3-yl , 2-isoxazolin-4-yl, 3-isoxazolin-4-yl, 4-isoxazolin-4-yl, 2-isoxazolin-5-yl, 3-isoxazole Benzin-5-yl, 4-isoxazolin-5-yl, 2-isothiazolin-3-yl, 3-isothiazolin-3-yl, 4-isothiazolin-3-yl, 2-iso Thiazolin-4-yl, 3-isothiazolin-4-yl, 4-isothiazolin-4-yl, 2-isothiazolin-5-yl, 3-isothiazolin-5-yl, 4-iso Thiazolin-5-yl, 2,3-dihydropyrazol-1-yl, 2,3-diaza D is more specific than salin-2-yl, 2,3-dinitrogen, sal-3-yl, 2, 3-dinitrogen. ratio. Sit-4-yl, 2,3 - 2 gas ratio ° sit -5-based, 3,4-dinitrogen. The ratio of -1 -yl, 3,4 -diaza 0 to σ sits on the -3-yl, 3,4-dihydrogen ratio. Sit-4-yl, 3,4-dihydro alpha ratio. Sit-5-based, 149026.doc -27- 201103429 4,5-dihydro D is more than sal-1--, 4,5-dihydro. ratio. Take -3 -yl, 4,5-dihydrogen. ratio. Sodium-4-yl, 4,5-dihydropyrazol-5-yl, 2,3-dihydrooxazol-2-yl, 2,3-dihydrogen. Sodium-3-yl, 2,3-dihydro-deso-4-yl, 2,3-dihydro oxime. Sitting on a 5-based, 3,4-dihydrogen. Sitting 2-yl, 3,4-dihydrogen. Cacao-3-yl, 3,4-dihydrogen. -4-yl, 3,4-dihydrooxazol-5-yl, 3,4-dihydrooxazol-2-yl, 3,4-dihydro oxazol-3-yl, 3,4 - Dihydrogen. Sit-4 - base, 2 - mother. Stationary, 3-branched bite base, 4-° bottom π-group, 1,3 -di-α-carbo-5-yl, 2-tetrazole α-pyranyl, 4-tetrahydronaphthyl, 2-tetrahydro . Steenyl, 3-hexahydroindole, 4-hexahydropyridazinyl, 2-hexahydro. Close bite, 4-hexahydro-dense. Stationary, 5-hexahydro-density, 2-0 thiol, 1,3,5-hexamol-2, and 1,2,4-hexanitrodiin-3-yl and corresponding - Subunit; a 7-membered saturated or partially unsaturated heterocyclic ring containing 1, 2 or 3 heteroatoms from a group consisting of oxygen, nitrogen and sulfur as ring members: for example, a single ring having 7 ring members And a bicyclic heterocyclic ring which, in addition to a carbocyclic member, also contains from 1 to 3 nitrogen atoms and/or an oxygen or sulfur atom or one or two oxygen and/or sulfur atoms, for example, tetrahydronitride And hexahydroazinyl, such as 2,3,4,5-tetrahydro[1Η]azepine-1-, -2-, -3-'-4-'-5-, -6- or -7- Base, 3,4,5,6-tetrahydro[2Η]azepine-2-, -3-, -4-, -5-, -6- or -7-yl, 2,3,4,7- Tetrahydro[111]azepine-1-'-2-,-3-, -4-, -5-, -6- or -7-yl, 2,3,6,7-tetrahydro[1Η]nitrogen -1--1- ' -2- ' -3-, -4-, -5-, -6- or -7-yl, six rat snorkeling -1, -2-, -3 - or -4 -yl , tetraazepine and hexahydrooxo group, such as 2,3,4,5-tetrahydro[1Η]oxo-2-, -Β-λ-4-, -5-, -6- or - 7-yl, 2,3,4,7-tetrahydro[1Η]oxo-2-,-3-,-4-,-5-,-6- Or 7-yl, 2,3,6,7-tetranitro[1Η]oxo-2-,-3-[S] 149026.doc • 28 - 201103429 or ·7-based, hexahydroxine _1 -4- -2- Discussing - -3- or _4-yl 'tetra- and hexachlorourethane sigma, azohime, tetra- and hexahydro-indole-diazol, four- and six Gas-1 3 - 〇亚急成盆,心氮千基,四- and hexahydro-Μ-oxazolyl group, four· and six winds _ 1 3 ·-Feikou Wuhe And hexahydro-1,4-dioxole and the corresponding -subunit. The dry soil contains 1, 2 or 3 5- or 6-membered aromatic (=maximum unsaturated) heterocyclic rings (=heteroaromatic groups) selected from heteroatoms consisting of oxygen, nitrogen and sulfur, for example, 5_Μ hetero-aryl which is bonded via carbon and which contains (1) a nitrogen atom or a nitrogen atom and a sulfur or oxygen atom as a ring member, such as 20-denyl, 3-furyl, 2-thienyl, thiothienyl, anthracene Pyrrolyl, 3-pyrrolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, %isothiazolyl, 4-isothiazolyl, 5-isothiazolyl, 3-pyrazolyl , 4_pyrazolyl 5-. ratio. Sitting on the base, 2 - ° evil. Sitrate, 4 - ° oxalyl, 5 - ° oxalyl, 20 oxazolyl, 4-thiazolyl, 5-thiazolyl, 2-imidazolyl, 4-imidazolyl, 1,2,4- Diazole-3-yl, 1,2,4-oxadiazol-5-yl, 1,2,4-thiadiazole-3-yl, 1,2,4-thiadiazol-5-yl, 1, 2,4-triazol-3-yl, 1,3,4-oxadiazole 2-yl, 1,3,4-thiadiazol-2-yl and 1,3,4-triazole-2-yl; 5-membered heteroaryl, which is attached via nitrogen and contains 1 to 3 nitrogen atoms as ring members,

如’ 11比洛-1 -基、α比唾-1 _基、味唾-1 _基、1,2 3 _ = J 5 —' σ里 _ 1 一 基及1,2,4-三唑-1-基;含有1、2或3個氮原子作為環成員 之6-員雜芳基,諸如吡啶_2_基、吡啶-3-基、。比 疋-4 - &、3-噠祕、4-噠減、2_似&、4-嘴。定基、5“密 11 定基、2-吡嗪基' 1,3,5-三嗪-2-基及1,2,4-三嗪_3_基; 直鏈C2或C3伸烷基:具有2或3個碳原子之二價未分支 149026.doc -29· 201103429 鏈,亦即ch2ch2及ch2ch2ch2。 直鏈CrC5伸烷基:具有1至5個碳原子之二價未分支 鍵’亦即 ch2、ch2ch2、ch2ch2ch2、ch2ch2ch2ch2& ch2ch2ch2ch2ch2。 C2-(:5伸烧基:具有2至5個碳原子之二價分支或較佳未 分支鏈,例如 CH2CH2、-CH(CH3)-、ch2ch2ch2、ch(ch3)ch2、 CH2CH(CH3)、CH2CH2CH2CH2、CH2CH2CH2CH2CH2。 CU-Cs伸烷基:具有4至5個碳原子之二價分支或較佳未 分支鏈,例如CH2CH2CH2CH2 或 ch2ch2ch2ch2ch2。 基團-SM更確切而言為基團-S-M+,其中M+為如上所定 義之金屬陽離子相等物或録陽離子。金屬陽離子相等物更 確切而言為1/a Ma+,其中a為金屬之原子價且一般為i、2 或3。 以下關於本發明化合物之合適且較佳特徵的陳述,尤其 關於其取代基 Het、A、Y、Ri、R2、r3、r4、r5、r6、 R6a、R7、R8、R9、Ri。、R丨丨、ri2、Rl3、Rl4、Rl5、r〗6、 關於其用途的陳述本身且尤其在彼此所有可能的組合中均 有效。Such as '11 bilo-1 -yl, α than sal -1 _ group, taste saliva-1 _ group, 1,2 3 _ = J 5 —' σ _ 1 yl and 1,2,4-triazole a -1- group; a 6-membered heteroaryl group having 1, 2 or 3 nitrogen atoms as a ring member, such as a pyridine-2-yl group, a pyridin-3-yl group. Than 疋-4 - &, 3-哒 secret, 4-哒 reduction, 2_like &, 4-mouth. Stationary, 5" dense 11-based, 2-pyrazinyl-1,3,5-triazin-2-yl and 1,2,4-triazinyl-3-yl; linear C2 or C3 alkylene: Divalent unbranched of 2 or 3 carbon atoms 149026.doc -29· 201103429 Chain, ie ch2ch2 and ch2ch2ch2. Linear CrC5 alkyl: a divalent unbranched bond having 1 to 5 carbon atoms', ie ch2 , ch2ch2, ch2ch2ch2, ch2ch2ch2ch2& ch2ch2ch2ch2ch2. C2-(:5): a divalent branch having 2 to 5 carbon atoms or preferably an unbranched chain, such as CH2CH2, -CH(CH3)-, ch2ch2ch2, ch( Ch3)ch2, CH2CH(CH3), CH2CH2CH2CH2, CH2CH2CH2CH2CH2. CU-Cs alkylene: a divalent branch having 4 to 5 carbon atoms or preferably an unbranched chain, such as CH2CH2CH2CH2 or ch2ch2ch2ch2ch2. The group-SM is more precise. The group is -S-M+, wherein M+ is a metal cation equivalent or a cation as defined above. The metal cation equivalent is more specifically 1/a Ma+, where a is the valence of the metal and is generally i. 2 or 3. The following statements regarding suitable and preferred characteristics of the compounds of the invention, especially with respect to their substituents Het, A, Y, Ri, R2 R3, r4, r5, r6, R6a, R7, R8, R9, Ri., R丨丨, ri2, Rl3, Rl4, Rl5, r, 6, statements about their use per se and especially in all possible combinations with each other Both are valid.

Het較佳係經由C原子連接至基團γ。 在本發明之-較佳實施例中,Het為含有】、2或3個選自 Ν、Ο及S之雜原子作為環成員的5_或6•員雜芳環,其中該 雜芳環可具有1、2、3或4個,較佳_個取代絲5。更確 切而言,Het較佳為含有i個選自N、〇及§之雜原子及視情 149026.docHet is preferably attached to the group γ via a C atom. In a preferred embodiment of the present invention, Het is a 5- or 6-membered heteroaryl ring containing, 2 or 3 hetero atoms selected from the group consisting of ruthenium, osmium and S as ring members, wherein the heteroaryl ring may be There are 1, 2, 3 or 4, preferably _, substituted filaments 5. More specifically, Het preferably contains i heteroatoms selected from N, oxime and § and as appropriate 149026.doc

[SI •30· 201103429 況可選的1或2個其他氮原子 7 丁作為環成貝的5-或6-員雜芳 環,其中該雜芳環可1古! /、有、2、3或4個,較佳1或2個取代 基R上文列舉了合適之5_或6_員雜芳族基團。 在上文列舉之雜芳環中,較佳為Μ基,諸如K-2-基、吡啶-3-基或吡啶_4_基;嘧啶基,諸如2嘧啶基、4·嘧 疋土或法定基,呋喃基’諸如2-呋喃基或3·呋喃基;噻 吻基冑如2-噻吩基或3_噻吩基;吡咯基,諸如卜吡咯 基、2-吼洛基或3,„各基,尤其2_吼洛基或3_吼略基…比 坐基諸如1_吡唑基、3-吡唑基、4_吡唑基或5_吡唑基, 尤其3比坐基、4-吡唑基或5_吡唑基;咪唑基,諸如卜咪 。坐基、2·咪唾基或4+坐基,尤其2_咪嗤基或4_味哇基; 惡唑基,諸如2-噁唑基、4_噁唑基或5_噁唑基;異噁唑 基諸士 3異惡唑基、4_異噁唑基或%異噁唑基;噻唑 基諸如2_噻唑基、4-噻唑基或5_噻唑基;異噻唑基,諸 如3-異噻唑基、4_異噻唑基或5-異噻唑基;及三唑基,諸 如1,2,4-三唾_1_基、丨,2,心三唑_3_基、三唑·‘基、 1,3,4_三°坐小基、1,3,4-三唑-2-基或1,3,4-三唑-3-基,尤其 1,2,4·三唑-3·基或i,3,4_三唑_2_基。指定連接位置應理解 為相對於環雜原子之卜位置且具有最高優先級。舉例而 a,在含有1個環雜原子之環中,指定連接位置相對於該 唯-核雜原子之i •位置。在吡唑基中,指定連接位置相對 於2個氮%原子之丨_及2_位置,在咪唑基中,指定連接位置 相對於2個氮環原子之1-及3-位置,在噁唑基中,指定連接 位置相對於氧環原子之丨_位置及氮環原子之3_位置,在異 149026.doc 201103429 噁唑基中,指定連接位置相對於氧環原子之丨_位置及氮環 原子之2-位置,在售嗤基中,指定連接位置相對於硫環: 子之W立置及氮環原子之3·位置,在異。塞。坐基中,指定連 接位置相對於硫環原子之丨_位置及氮環原子之2_位置,等 等。 更佳為吡啶基,諸如吡啶_2·基、吡啶_3_基或吡啶-基;噻吩基,諸如2-或3-噻吩基;及噻唑基,諸如2_噻唑 基、4-嗟》坐基或5-嘆。坐基。尤其較佳為〇比咬基,諸如吡。定_ 2-基、吡啶-3-基或吡啶-4-基,且尤其為吡啶_2•基。 在Het為6-員雜芳環之情況下,其較佳具有〇、丨、2或3 個,更佳0、1或2個取代基R5,其中兩個或兩個以上取代 基R5可相同或不同。在11以為5-員雜芳環之情況下,其較 佳具有〇、1或2個取代基R5,其中兩個取代基尺5可相同或 不同。 R5可經C或N連接’但較佳連接至Het之c原子。 R5較佳選自鹵素、OH、SH、N〇2、CN、CVC4烷基、 CrCj烧基、CVC4烷氧基-CVC4烷基、Ci-C4烷氧基、C,-C4烧氧基-CrC4烷氧基及Ci-C^鹵烷氧基,更佳選自氟、 氯、溴、(VC4烷基、(:丨-(:4鹵烷基、烷氧基及^-匕 鹵烷氧基,甚至更佳選自氟、氣、溴、CH3、chf2、 CF3、OCH3、OCHF2及〇cf3 ’且尤其選自氟、氣、溴、 CH3、CF3、och3及 ocf3。 詳言之,Het係選自下式Het.l至Het.49 :[SI • 30· 201103429 Conditional 1 or 2 other nitrogen atoms 7 butyl as a 5- or 6-membered heteroaryl ring of the ring-shaped shell, wherein the hetero-aromatic ring can be 1 ancient! /, Yes, 2, 3 or 4, preferably 1 or 2 substituents R are listed above as suitable 5 or 6-membered heteroaromatic groups. Among the heteroaryl rings exemplified above, a mercapto group such as a K-2-yl group, a pyridin-3-yl group or a pyridyl-4-yl group; a pyrimidinyl group such as a 2-pyrimidinyl group, a 4·pyrimidin or a legal group is preferred. a furyl group such as 2-furyl or 3·furanyl; a thiol group such as 2-thienyl or 3-thienyl; a pyrrolyl group such as a pyrrolyl group, a 2-meryl group or a 3, yl group , especially 2_吼洛基 or 3_吼基基... than a sitting group such as 1-pyrazolyl, 3-pyrazolyl, 4-pyrazolyl or 5-pyrazolyl, especially 3 than sitting, 4- Pyrazolyl or 5-pyrazolyl; imidazolyl, such as dipyridyl, succinyl, 2, merionyl or 4+, especially 2 mercapto or 4 acetonyl; oxazolyl, such as 2 -oxazolyl, 4-oxazolyl or 5-oxazolyl; isoxazolyl 3 isoxazolyl, 4-isoxazolyl or % isoxazolyl; thiazolyl such as 2-thiazolyl, 4-thiazolyl or 5-thiazolyl; isothiazolyl, such as 3-isothiazolyl, 4-isothiazolyl or 5-isothiazolyl; and triazolyl, such as 1,2,4-trisal_1 Base, oxime, 2, heart triazole _3_ group, triazole·' group, 1,3,4_three° siting base, 1,3,4-triazol-2-yl or 1,3,4 - triazol-3-yl, especially 1,2,4 · Triazol-3-yl or i,3,4-triazole_2-yl. The specified position of attachment is understood to be relative to the position of the heteroatom of the ring and has the highest priority. For example, a, contains 1 ring In the ring of a hetero atom, the position of the connection is specified relative to the i-position of the only-nuclear hetero atom. In the pyrazolyl group, the position of the connection is specified relative to the 氮_ and 2_ positions of the two nitrogen atoms, in the imidazolyl group. , specifying the position of the linkage relative to the 1- and 3-positions of the two nitrogen ring atoms. In the oxazolyl group, the position of the attachment is relative to the position of the oxygen ring atom and the position of the nitrogen ring atom at the 3_ position, in the different 149026. Doc 201103429 In the oxazolyl group, the position of the bond is specified relative to the 丨_position of the oxygen ring atom and the 2-position of the nitrogen ring atom. In the sold oxime group, the specified connection position is relative to the sulphur ring: the W stand and the nitrogen ring The position of the atom is in the same position as the pyridine group. a pyridine-3-yl or pyridyl group; a thienyl group such as a 2- or 3-thienyl group; and a thiazolyl group such as a 2-thiazolyl group, 4- "Sitting base or 5-s. Sitting base. Especially preferred is a thiol base such as pyridin-2-yl, pyridin-3-yl or pyridin-4-yl, and especially pyridine-2. In the case where Het is a 6-membered heteroaryl ring, it preferably has fluorene, fluorene, 2 or 3, more preferably 0, 1 or 2 substituents R5, wherein two or more substituents R5 may be the same Or different. In the case of 11-membered 5-membered heteroaryl ring, it preferably has fluorene, 1 or 2 substituents R5, wherein the two substituent bases 5 may be the same or different. R5 may be linked via C or N' However, it is preferably attached to the c atom of Het. R5 is preferably selected from the group consisting of halogen, OH, SH, N〇2, CN, CVC4 alkyl, CrCj alkyl, CVC4 alkoxy-CVC4 alkyl, Ci-C4 alkoxy, C,-C4 alkoxy-CrC4 Alkoxy and Ci-C^haloalkoxy, more preferably selected from the group consisting of fluorine, chlorine, bromine, (VC4 alkyl, (: 丨-(: 4-haloalkyl, alkoxy, and 匕-halo alkoxy) Even more preferably selected from the group consisting of fluorine, gas, bromine, CH3, chf2, CF3, OCH3, OCHF2 and 〇cf3' and especially selected from the group consisting of fluorine, gas, bromine, CH3, CF3, och3 and ocf3. From Het.l to Het.49 below:

t SI 149026.doc -32- 201103429 α # Λt SI 149026.doc -32- 201103429 α # Λ

ΝΝ

Het.1 Het.2 Het.3 Het.4 Het.5 Het.6 Het.7 Het.8Het.1 Het.2 Het.3 Het.4 Het.5 Het.6 Het.7 Het.8

άτϋ# A# /Άτϋ# A# /

H3CCT ▽ F3C(T v 「Cl’、^ Br’、^ H3C’、^ H3COH3CCT ▽ F3C (T v "Cl', ^ Br', ^ H3C', ^ H3CO

Het.9 Het.10 Het.11 Het.12 Het.13 Het.14 Het.15 Het.16Het.9 Het.10 Het.11 Het.12 Het.13 Het.14 Het.15 Het.16

Het.17 Het.18 Het.19 Het.20 Het.21 Het.22 Het.23 Het.24Het.17 Het.18 Het.19 Het.20 Het.21 Het.22 Het.23 Het.24

Het.39 Het.40 Het.41 Het.42 # # # # #Het.39 Het.40 Het.41 Het.42 # # # # # #

Het.43 Het.44 Het.45 Het.46 Het.47 Het.48 Het.49 在上式之中,較佳為基團Het. 1及Het.4至Het.42,更佳 為基團Het.l及Het.4至Het.24,且尤其較佳為Het.1、 Het.8、Het_12、Het.19及 Het.22。 在本發明之一較佳實施例中,R1、R2、R3及R4彼此獨立 •33· 149026.doc 201103429 地選自氮、函素、〇H ' SH、N02、CN、C,-C4烷基' C|. C4鹵烷基、Cl_c4烷氧基·CrG烷基、Ci_c&氧基、 烷氧基-c^-c:4烷氧基&Cl_C4齒烷氧基,更佳選自氫、氟、 氣 '溴、C】-C4烷基、Cl-C4^烷基、c〗_c4烷氧基及^-^ 鹵烧氧基,甚至更佳選自氫、氟、氣、溴、ch3、chf2、 CF3、〇ch3、〇CHFj OCF3,且尤其選自氫、氟、·氣、 溴、CH3、cf3、0CH3及 ocf3。 在本發明之一更佳實施例中,Ri、R2、RW中之2、3 或所有4個為氫且其餘個基團Ri、R2、R3及R4係選自 鹵素、OH、SH ' N〇2、CN、CVC4烧基、CVC4 齒烷基、 G-C4烷氧基-CVC4烷基、(VC4烷氧基、CVC4烷氧基-C,-C4烷氧基及CVC4鹵烷氧基,更佳選自氟、氣、溴、Ci_c4 烧基、Ci-C4鹵烷基、CVC4烷氧基及(^-(:4鹵烷氧基,甚至 更佳選自氟、氣、溴、甲基、乙基、CHF2、CF3、甲氧 基、乙氧基、OCHF2及OCF3,且尤其選自氟、氯、溴、 CH3、cf3、0CH3及OCF3。甚至更佳,R1、R2、R3AR4中 之3或所有4個為氫且其餘基團R1、R2、R3或R4係選自鹵 素、OH、SH、N02、CN、(VC4 烧基、Cl-C4 鹵院基 ' Cl_ c4烷氧基-CVC4烷基、CVC4烷氡基、CVC4烷氧基-c,-c4烷 氧基及CVC4鹵烷氧基’更佳選自氟、氣、溴、(^-(^烷 基、C「C4鹵烷基、CrC4烷氧基及匸广^鹵烷氧基,甚至更 佳選自氟、氯、溴、甲基、乙基、CHF2、CF3、甲氧基、 乙氧基' OCHF2及〇CF3 ’且尤其選自氟、氯、溴、ch3、 CF3、〇CH3及ocf3。詳言之,Ri、R2、尺3及尺4為氫或r2、 149026.doc •34- 201103429 R3及R4為氫且R1不為氫且較佳選自鹵素、OH、SH、 N〇2、CN、CVC4烷基、CVGi 烷基、烷氧基-(VC4 烷基、CVQ烷氧基、烷氧基-CVC4烷氧基及心-山鹵 烷氧基,更佳選自氟、氣、溴、CVC4烷基、CVC4鹵烷 基、Crq烷氧基及鹵烷氧基,甚至更佳選自氟、 氣、溴、甲基、乙基、CHF2、CF3、甲氧基、乙氧基、 ochf2及 ocf3,尤其選自氟、氣、溴、ch3、cf3、och3 及ocf3且尤其為曱基。 詳言之,R1、R2、R3及R4之組合含義係選自表1中所彙 編之以下組合: 表1Het.43 Het.44 Het.45 Het.46 Het.47 Het.48 Het.49 Among the above formulas, preferred groups are Het. 1 and Het. 4 to Het. 42, more preferably Het. .l and Het. 4 to Het. 24, and particularly preferably Het. 1, Het. 8, Het_12, Het. 19 and Het. In a preferred embodiment of the invention, R1, R2, R3 and R4 are independent of each other. • 33·149026.doc 201103429 is selected from the group consisting of nitrogen, a physin, 〇H 'SH, N02, CN, C, -C4 alkyl 'C|. C4 haloalkyl, Cl_c4 alkoxy·CrG alkyl, Ci_c&oxy, alkoxy-c^-c:4 alkoxy&Cl_C4 dentateoxy, more preferably selected from hydrogen, Fluorine, gas 'bromo, C】-C4 alkyl, Cl-C4 alkyl, c _c4 alkoxy and ^-^ halogen alkoxy, even more preferably selected from the group consisting of hydrogen, fluorine, gas, bromine, ch3, Chf2, CF3, 〇ch3, 〇CHFj OCF3, and especially selected from the group consisting of hydrogen, fluorine, gas, bromine, CH3, cf3, 0CH3 and ocf3. In a further preferred embodiment of the invention, 2, 3 or all 4 of Ri, R2, RW are hydrogen and the remaining groups Ri, R2, R3 and R4 are selected from the group consisting of halogen, OH, SH' N〇 2. CN, CVC4 alkyl, CVC4 dentate, G-C4 alkoxy-CVC4 alkyl, (VC4 alkoxy, CVC4 alkoxy-C, -C4 alkoxy and CVC4 haloalkoxy, more Preferably selected from the group consisting of fluorine, gas, bromine, Ci_c4 alkyl, Ci-C4 haloalkyl, CVC4 alkoxy and (^-(: 4-haloalkoxy, even more preferably selected from the group consisting of fluorine, gas, bromine, methyl, Ethyl, CHF2, CF3, methoxy, ethoxy, OCHF2 and OCF3, and especially selected from the group consisting of fluorine, chlorine, bromine, CH3, cf3, 0CH3 and OCF3. Even better, 3 of R1, R2, R3AR4 or All four are hydrogen and the remaining groups R1, R2, R3 or R4 are selected from the group consisting of halogen, OH, SH, N02, CN, (VC4 alkyl, Cl-C4 halogen-based 'Cl_c4 alkoxy-CVC4 alkyl , CVC 4 alkyl fluorenyl, CVC 4 alkoxy-c, -c 4 alkoxy and CVC 4 haloalkoxy' are more preferably selected from the group consisting of fluorine, gas, bromine, (^-(^ alkyl, C "C4 haloalkyl", CrC4 alkoxy group and fluorene alkoxy group, even more preferably selected from the group consisting of fluorine, chlorine, bromine, methyl, ethyl, CHF2, CF3, methoxy, B The oxy 'OCHF2 and 〇CF3' are especially selected from the group consisting of fluorine, chlorine, bromine, ch3, CF3, 〇CH3 and ocf3. In particular, Ri, R2, ruler 3 and ruler 4 are hydrogen or r2, 149026.doc • 34 - 201103429 R3 and R4 are hydrogen and R1 is not hydrogen and is preferably selected from the group consisting of halogen, OH, SH, N〇2, CN, CVC4 alkyl, CVGi alkyl, alkoxy-(VC4 alkyl, CVQ alkoxy alkoxy-CVC4 alkoxy and heart-and-haloalkoxy, more preferably selected from the group consisting of fluorine, gas, bromine, CVC4 alkyl, CVC4 haloalkyl, Crq alkoxy and haloalkoxy, even better Selected from fluorine, gas, bromine, methyl, ethyl, CHF2, CF3, methoxy, ethoxy, ochf2 and ocf3, especially selected from the group consisting of fluorine, gas, bromine, ch3, cf3, och3 and ocf3 and especially In particular, the combined meaning of R1, R2, R3 and R4 is selected from the following combinations compiled in Table 1: Table 1

編號 R1 RJ R4 1. Η H H H 2. Η F H H 3. Η Cl H H 4. Η Br H H 5. Η ch3 H H 6. Η CH2CH3 H H 7. Η chf2 H H 8. Η cf3 H H 9. Η OCH3 H H 10. Η OCH2CH3 H H 11. Η OCHF2 H H 12. Η OCF3 H H 13. F H H H 14. C1 H H H 15. Br H H H 16. ch3 H H H 17. CH2CH3 H H H 18. chf2 H H H 19. cf3 H H H 20. OCH3 H H H 21. OCH2CH3 H H H 22. OCHF2 H H H 23. OCF3 H H H 24. F F H H 25. H F H F 149026.doc -35- 201103429No. R1 RJ R4 1. Η HHH 2. Η FHH 3. Η Cl HH 4. Η Br HH 5. Η ch3 HH 6. Η CH2CH3 HH 7. Η chf2 HH 8. Η cf3 HH 9. Η OCH3 HH 10. Η OCH2CH3 HH 11. OC OCHF2 HH 12. Η OCF3 HH 13. FHHH 14. C1 HHH 15. Br HHH 16. ch3 HHH 17. CH2CH3 HHH 18. chf2 HHH 19. cf3 HHH 20. OCH3 HHH 21. OCH2CH3 HHH 22. OCHF2 HHH 23. OCF3 HHH 24. FFHH 25. HFHF 149026.doc -35- 201103429

編说 Rk R2 R3- R5 26. Η F F H 27. F H F H 28. Cl Cl H H 29. Η ~Cl ' H Cl 30. Η Cl Cl H 31. Cl H Cl H 32. F Cl H H 33. Cl F H H 34. H F H Cl 35. F H Cl H 36. H Cl ' F H 37. H F Cl H 38. CH3 CH3 H H 39. H CH3 H ch3 40. H CH3 ch3 H 41. ch3 H ch3 H 42. F CH3 H H 43. CH3 F H H 44. H F H ch3 45. F H ch3 H 46. H ~ch3 ~~ F H 47. H F ch3 H 48. F 〇CH3 H H 49. OCH3 F ~ H H 50. H F H OCH3 51. F H 〇CH3 H 52. H OCH3 F H 53. H F 〇CH, H 54. F F F H 55. F F H F 基團-C(=0)R12及-S(0)2r12中之R12較佳選自Ci_c4烧基、 C「C2鹵烧基、CVC4烧氧基、Ci-C2鹵烧氧基、苯基、苯氧 基及NR R ’更佳選自C1-C4院基、C^-Ca鹵烧基、q-C 烷氧基、C「C2鹵烷氧基及NR15R16,且甚至更佳選自(:_(: 烷基、C「C4烷氧基及NR15R16。在基團-C(=〇)r12中,r12 尤其為C^-C4烧基,諸如曱基、乙基、丙基、異丙美、正 基’或為 、異丙氣 丁基、第二丁基、異丁基或第三丁基,較佳為甲 C1-C4烧氧基’遠如曱氧基、乙氧基、丙氧基 149026.doc -36- 201103429 基、正丁氧基、坌-s 第一丁氧基、異丁氧基或第三丁氧基,較 佳2為甲氧基,且更尤其為甲基,且在基團_s⑼戊12中, R尤其為甲基。較佳地,R15為氫且R16係選自氫、Ca 烷基及苯基’較佳選自氫及C〗_C4烷基;或r15及r16均為Edit Rk R2 R3- R5 26. Η FFH 27. FHFH 28. Cl Cl HH 29. Η ~Cl ' H Cl 30. Η Cl Cl H 31. Cl H Cl H 32. F Cl HH 33. Cl FHH 34. HFH Cl 35. FH Cl H 36. H Cl ' FH 37. HF Cl H 38. CH3 CH3 HH 39. H CH3 H ch3 40. H CH3 ch3 H 41. ch3 H ch3 H 42. F CH3 HH 43. CH3 FHH 44. HHCH3 F. 53. HH3. HF 〇CH, H 54. FFFH 55. R12 in the FFHF group -C(=0)R12 and -S(0)2r12 is preferably selected from the group consisting of Ci_c4 alkyl, C"C2 halo, CVC4 alkoxy , Ci-C2 haloalkoxy, phenyl, phenoxy and NR R ' are more preferably selected from the group consisting of C1-C4, C^-Ca halo, qC alkoxy, C"C2 haloalkoxy" NR15R16, and even more preferably selected from (:_(: alkyl, C"C4 alkoxy and NR15R16. In the group -C(=〇)r12, r12 is especially C^-C4 alkyl, such as fluorenyl , ethyl, propyl, isopropyl, n- ortho, isopropyl butyl, t-butyl, isobutyl or tert-butyl, preferably C1-C4 oxygenated The base is as far as methoxy, ethoxy, propoxy 149026.doc -36-201103429, n-butoxy, 坌-s first butoxy, isobutoxy or tert-butoxy Preferably, 2 is a methoxy group, and more particularly a methyl group, and in the group _s(9) pentane 12, R is especially a methyl group. Preferably, R15 is hydrogen and R16 is selected from hydrogen, Ca alkyl and phenyl. 'preferably selected from hydrogen and C〗 _C4 alkyl; or r15 and r16 are

Cl-C4烷基,較佳為甲基或乙基。 Μ較佳選自驗金屬陽離子,驗土金屬陽離子相等物, Cu、Zn、Fe或Νι之陽離子相等物,或式(NRaRbRCRd)+之銨 陽離子,其中^…^,中之一者為氯且^、^^ &Rd中之三者彼此獨立地選自C|-C1G烷基。更佳地,河係 選自 Li+、Na+、K+、y2Mg2+ ’ Cu、Zn、Fe 或 Ni之陽離子相 等物,或式(NRaRbRCRd)+之銨陽離子,其中Ra、Rb、Rc& Rd中之一者為氫且Ra、Rb、…及Rd中之三者彼此獨立地選 自CVCw烷基。甚至更佳地,M係選自Na+、K+、1/2Mg2+、 !/2Cu2+、ZZn2·"、i/2Fe2+、i/2Ni2+、三乙銨及三曱銨。 在式III之基團中,變數較佳具有在分子I之其餘部分中 相同之含義。因此’上文關於基團之較佳含義的陳述亦適 用於此部分。 R6較佳選自氫、烷基、-C( = 〇)R12、-S(C〇2Ri2、 •CN、Μ及式III之基團,其中R12具有上述一般含義中之_ 者’或尤其上述較佳含義中之一者,且Μ具有上述一般含 義中之一者,或尤其上述較佳含義中之一者。 R6更佳選自氫、CVC4烷基、C3-C4烷基羰基、Cl-C4烷氧 羰基、烷基、-C(=0)N(C 丨-C4 烷基)2、Cl_ CU烷基磺醯基、CN、Μ及式III之基團,其中Μ具有上述— 149026.doc •37· 201103429 般含義中之一者,或尤其上述較佳含義中之一者。詳言 之,R6係選自氫、甲基、乙基、丙基、異丙基、甲基幾 基、曱氧羰基、-c(=o)n(ch3)2、CN、M及式⑴之基團, 其中Μ具有上述一般含義中之一者,或尤其上述較佳含義 中之一者,較佳為鹼金屬陽離子或% Cu2、詳言之,R6為 氫甲基、甲基戴基、甲氧|ί炭基、Na+或式ΠΙ之基團。、 R6a較佳選自氫、Cl-Cl0烷基、Ci_C4函烷基、苯基、笨 基-Ci-C4烷基、-C( = 0)R12及-s(〇)2Rl2,其中r12具有上述 一般含義令之一者,或尤其上述較佳含義中之一者。更佳 地,^係選自氫、Cl-C4烧基、Ci_C4函烧基、苯基、节 基、-(:(=0)!^2及_8(〇)21112’其中Rl2具有上述一般含義中 之一者,或尤其上述較佳含義中之一者,更佳選自氫、 c=c4烷基、Cl_c4_ 烷基、_c(=〇)Rl2&_s(〇)2Ri2,其中 R12具有上述-般含義令之一者’或尤其上述較佳含義中 之一者。R“尤其為氫、Cl_C4院基(較佳為曱基)或 c( 〇)R ,更尤其為氫、Cl_C4烷基(較佳為曱基卜甲基 %基或甲氧羰基’甚至更尤其為氫或烷基(較佳為甲 基)’特別為氫。 Y較佳為〇。 ' A較佳為直鏈匕扣伸烧基橋,其中伸烧基橋之鴻2個 氩原子可經1或2個取代基…置換,#中各r7獨立地選自 q-c4烧基、Cl_C4以基、Ci_c^氧基、烧氧基-c,-C4烷氧基及匕-匚4鹵烷氧基,且較佳選自甲基、乙基、曱 氧基、乙氧基及甲氧基甲氧基’或連接於相鄰碳原;上的 [S1 149026.doc -38- 201103429 兩個取代基R7連同其所連接之碳原子一起形成環戊基或環 己基環。更佳地’ A為直鏈(^2或(^伸烷基橋,其中伸烷基 橋之1個氫原子可經1個取代基R7置換,其中R7為C1 -C4烷 基。甚至更佳地,A為直鏈(32伸烷基橋,其中伸烷基橋之i 個氫原子可經1個取代基R7置換,其中R7為基且較 佳為甲基。詳言之,A為-CH(CH3)-CH2-。 若m為1,氧原子較佳經由雙鍵連接至硫原子上,由此 基團-S(0)m-R6形成基團_8(=〇)_尺6。,兩個氧原子 較佳均經由雙鍵連接至硫原子上,由此基團_s(〇)m_R6形成 基團- S( = 〇)2_r6。若111為3,則基團_s(〇)m_R6為基團 -S( = 〇)2-〇-R6 〇 m較佳為0或2且更佳為ο。 在一尤佳實施例中’在化合物工中,]11為〇且116為Η(或另 外’在化合物II中,R6^H)。 特定化合物I/II為以下: 2_{4_曱基~2-[2·曱基_4«咬_2-基氣基)_笨基H1,3_二氧 雜環戊烷-2-基曱基三唑_3_硫醇; 2-{4-曱基-2-[2-曱基_4_(5-三說曱基_D比啶J基氧基苯 基]-Π,3-二氧雜環戊烧·2_基甲基卜2_H_[i 2 4]三唑_3硫 醇; 2-{4-曱基-2-[4-(5-氣-3-氟」比啶基氧基)_2·甲基·苯 基Ηΐ,3-二氧雜環戊烧冬基曱基卜2_Η,π,2,4]三唑冬硫 醇; 2-{4-曱基-2·[4-(3,5-二氯Κ2_基氧基)·2_甲基_苯基]_ 149026.doc •39· 201103429 [1’3^雜環m基甲基}-2-Η-[1,2,4]三唾-3-硫醇; {2 [4-(3-氣-5-二氣甲基_。比。定_2_基氧基)2_甲基-苯基]· 心甲基-[1,3_二氧雜環戊燒_2_基甲基}2_即,2⑷三峻_3_ 硫醇; 2-{2-[4-(5-氯-3-氟比 二氧雜環戊烷-2-基甲基j 。定-2-基氧基)-苯基]-4-曱基-[1,3-'2-H-[1,2,4]三唑-3-硫醇。 較佳化合物I及II之實例為 式1.1至1.96及II. 1至11.48之化 合物’其中變數具有以上給出之一般含義或尤其較佳含義 中之一者。較佳化合物之實例為在以下表丨至4176中所彙 編之個別化合物。此外,如下針對表中之個別變數所述Cl-C4 alkyl, preferably methyl or ethyl. Preferably, the cerium is selected from the group consisting of a metal cation, a metal cation equivalent, a cation equivalent of Cu, Zn, Fe or Ν, or an ammonium cation of the formula (NRaRbRCRd)+, wherein one of the compounds is chlorine and Three of ^, ^^ & Rd are independently selected from C|-C1G alkyl. More preferably, the river system is selected from a cation equivalent of Li+, Na+, K+, y2Mg2+ 'Cu, Zn, Fe or Ni, or an ammonium cation of the formula (NRaRbRCRd)+, wherein one of Ra, Rb, Rc & Rd It is hydrogen and three of Ra, Rb, ... and Rd are independently selected from CVCw alkyl groups. Even more preferably, the M system is selected from the group consisting of Na+, K+, 1/2Mg2+, !/2Cu2+, ZZn2·", i/2Fe2+, i/2Ni2+, triethylammonium, and triammonium. In the group of formula III, the variables preferably have the same meaning in the remainder of molecule I. Therefore, the above statement regarding the preferred meaning of the group applies to this part as well. R6 is preferably selected from the group consisting of hydrogen, alkyl, -C(= 〇)R12, -S(C〇2Ri2, •CN, hydrazine, and a group of formula III, wherein R12 has the above general meaning or in particular One of the preferred meanings, and one of the above general meanings, or especially one of the above preferred meanings. R6 is more preferably selected from the group consisting of hydrogen, CVC4 alkyl, C3-C4 alkylcarbonyl, Cl-. a C4 alkoxycarbonyl group, an alkyl group, a -C(=0)N(C 丨-C4 alkyl group) 2, a Cl_ CU alkyl sulfonyl group, a CN, a hydrazine, and a group of the formula III, wherein hydrazine has the above - 149026. Doc •37· 201103429 One of the general meanings, or especially one of the above preferred meanings. In particular, R6 is selected from the group consisting of hydrogen, methyl, ethyl, propyl, isopropyl, methyl a group of oxime oxycarbonyl, -c(=o)n(ch3)2, CN, M and formula (1), wherein hydrazine has one of the above general meanings, or especially one of the above preferred meanings, Preferably, R6 is a hydrogen methyl group, a methyl group, a methoxy group, a Na+ group or a hydrazine group. R6a is preferably selected from the group consisting of hydrogen and Cl-Cl0. Alkyl, Ci_C4 functional alkyl, phenyl, stupid-Ci-C4 alkyl -C( = 0)R12 and -s(〇)2Rl2, wherein r12 has one of the above general meanings, or particularly one of the above preferred meanings. More preferably, the system is selected from the group consisting of hydrogen and Cl-C4. a base, a Ci_C4 functional group, a phenyl group, a benzyl group, -(:(=0)!^2, and _8(〇) 21112', wherein Rl2 has one of the above general meanings, or especially the above preferred meanings One of them is more preferably selected from the group consisting of hydrogen, c=c4 alkyl, Cl_c4_alkyl, _c(=〇)Rl2&_s(〇)2Ri2, wherein R12 has one of the above-mentioned general meanings or particularly preferred One of the meanings. R "especially hydrogen, Cl_C4, (preferably fluorenyl) or c( 〇)R, more particularly hydrogen, Cl_C4 alkyl (preferably fluorenylmethyl or methoxycarbonyl) 'Especially more hydrogen or alkyl (preferably methyl)' is especially hydrogen. Y is preferably 〇. 'A is preferably a linear chain-stretching bridge, of which 2 The argon atom may be replaced by 1 or 2 substituents, each of which is independently selected from the group consisting of q-c4 alkyl, Cl_C4, Ci_coxy, alkoxy-c, -C4 alkoxy and oxime-匚4 haloalkoxy, and preferably selected from methyl, ethyl, decyloxy, B And the methoxymethoxy group is attached to the adjacent carbon source; [S1 149026.doc -38- 201103429 Two substituents R7 together with the carbon atom to which they are attached form a cyclopentyl or cyclohexyl ring. More preferably, 'A is a straight chain (^2 or (2) alkyl bridge in which one hydrogen atom of the alkylene bridge can be substituted with one substituent R7, wherein R7 is a C1-C4 alkyl group. Even more preferably, A is a linear (32 alkylene bridge wherein the hydrogen atom of the alkylene bridge can be replaced by one substituent R7, wherein R7 is a group and preferably a methyl group. More specifically, A is -CH(CH3)-CH2-. If m is 1, the oxygen atom is preferably bonded to the sulfur atom via a double bond, whereby the group -S(0)m-R6 forms a group _8 (=〇) Preferably, both oxygen atoms are attached to the sulfur atom via a double bond, whereby the group _s(〇)m_R6 forms a group -S(= 〇)2_r6. If 111 is 3, the group _s(〇)m_R6 is a group -S(= 〇)2-〇-R6 〇m is preferably 0 or 2 and more preferably ο. In a particularly preferred embodiment, 'in the compound work, 11 is 116 and 116 is Η (or otherwise 'in compound II, R6^H). The specific compound I/II is as follows: 2_{4_曱基~2-[2·曱基_4«咬_2-base gas Base)_stupyl H1,3_dioxol-2-ylmercaptotriazole_3_thiol; 2-{4-mercapto-2-[2-indenyl_4_(5-three曱 _ _ D 啶 J 基 基 基 基 基 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- Mercapto-2-[4-(5-aza-3-fluoro)pyridyloxy)_2.methyl·phenylindole, 3-dioxolone曱基基b 2_Η,π,2,4]triazole thiol; 2-{4-mercapto-2·[4-(3,5-dichloroindol-2-yloxy)·2_methyl_ Phenyl]_149026.doc •39· 201103429 [1'3^heterocyclic m-methyl}-2-indole-[1,2,4]tris-trithiol; {2 [4-(3 - gas-5-dimethylmethyl.. ratio. _2_yloxy)2_methyl-phenyl]· cardiomethyl-[1,3-dioxol-2-a Base}2_, ie, 2(4) Sanjun_3_ mercaptan; 2-{2-[4-(5-chloro-3-fluorol-dioxolan-2-ylmethylj.din-2-yl) Oxy)-phenyl]-4-mercapto-[1,3-'2-H-[1,2,4]triazole-3-thiol. Examples of preferred compounds I and II are formula 1.1 to 1.96 and II.1 to 11.48 of the compound 'wherein the variable has one of the general meanings or especially preferred meanings given above. Examples of preferred compounds are the individual compounds compiled in the following Tables to 4176. As described below for individual variables in the table

含義本身(不依賴於提及該等變數之組合)為相關取 V 代基之 一尤佳實施例。The meaning itself (without relying on a combination of such variables) is a preferred embodiment of the relevant V base.

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R4R4

R4R4

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一-οOne-o

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R6*R6*

表1 R3及R4之 式1.1之化合物,其中化合物之Het、R1、R2、 組合在各情況下對應於表A之一列且R6為Η 表2 R3及R4之 式L1之化合物,其中化合物之Het、R1、R2、 組合在各情況下對應於表A之一列且R6為曱基 表3 R3及R4之 式L 1之化合物,其中化合物之Het、R1、R2、 組合在各情況下對應於表A之一列且R6為乙基 表4 149026.doc [ •50· 201103429 式1.1之化合物,其中化合物之Het、Ri、R2、R3&R4之 組合在各情況下對應於表A之一列且R6為丙基 表5 式1.1之化合物,其中化合物之Het、R丨、r2、R3&R4之 組合在各情況下對應於表A之一列且R6為異丙基 表6 式L1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為正丁基 表7 式M之化合物,其中化合物之Het、R丨、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為第二丁基 表8 式1,1之化合物’其中化合物之Het、R丨、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為異丁基 表9 式之化合物’其中化合物之Het、Rl、R2、R3及R4之 、且口在各情況下對應於表A之一列且R6為第三丁基 表1 0 ^ I 1 之化合物’其中化合物之Het、R1、r2、R3及R4之 組合在各情況下對應於表A之-列且R6為苯基 表11Table 1 Compounds of formula 1.1 wherein R3 and R4, wherein the combination of compounds Het, R1, R2, in each case corresponds to one of Table A and R6 is Η Table 2 R3 and R4 of formula L1, wherein the compound Het , R1, R2, in combination with a compound of formula L1 in each case corresponding to one of the columns of Table A and R6 being a fluorenyl group 3 R3 and R4, wherein the combination of Het, R1, R2 of the compound corresponds in each case to the table A column of A and R6 is a compound of the formula 1.4 149026.doc [•50· 201103429, wherein the combination of Het, Ri, R2, R3 & R4 of the compound corresponds in each case to one of the columns of Table A and R6 is The compound of the formula 1.1 wherein the combination of the compounds Het, R丨, r2, R3 & R4 corresponds in each case to one of the columns of Table A and R6 is an isopropyl group of the compound of the formula L1, wherein the compound The combination of Het, R1, R2, R3 and R4 corresponds in each case to one of the columns of Table A and R6 is a compound of the formula butyl N, wherein the combination of Het, R丨, R2, R3 and R4 of the compound is In each case, it corresponds to one of the columns of Table A and R6 is the second butyl group. The compound of formula 1,1 'Het, R of the compound The combination of 丨, R2, R3 and R4 corresponds in each case to one of the columns of Table A and R6 is an isobutyl group of the compound of the formula 9 wherein the compounds are Het, R1, R2, R3 and R4, and the mouth is in each case. A compound corresponding to one of the columns of Table A and R6 is a third butyl group 1 0 ^ I 1 wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the column of Table A and R6 For phenyl table 11

I: T 之化合物,其中化合物之Het、R丨、r2、R3及R4之 〇在各情况下對應於表A之一列且R6為苄基 表12 149026.doc -51 - 201103429 式M之化合物’其中化合物之Het、R丨、R2、R3及R4之 組合在各情泥下對應於表A之一列且R6為Li+ 表13 式M之化合物,其中化合物之Het、Ri、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為Na+ 表14 式1,1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為K+ 表15 式M之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為1/2]y[g2+ 表16 式Ll之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且尺6為!/2(:112+ 表17 式1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且尺6為1/2Zn2+ 表18 式Ll之化合物’其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為y2Fe2+ 表19 式^ 1之化合物’其中化合物之Het、R1、R2、R3及R4之 組。在各情況下對應於表A之一列且R6為ZNi24 表20I: A compound of T, wherein the compounds of Het, R丨, r2, R3 and R4 correspond in each case to one of the columns of Table A and R6 is a benzyl group. 12 149026.doc -51 - 201103429 Compound of formula M Wherein the combination of Het, R丨, R2, R3 and R4 of the compound corresponds to one of the tables A in each case and R6 is a compound of the formula M, wherein the compounds are Het, Ri, R2, R3 and R4. Combining in each case corresponds to a column of Table A and R6 is a compound of formula 1, formula 1, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6 K+ is a compound of the formula M wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6 is 1/2]y [g2+ the compound of the formula L1, Wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and the ruler 6 is !/2 (: 112 + Table 17 Compound of Formula 1 wherein the compound is Het, R1, R2 The combination of R3 and R4 corresponds in each case to one of the columns of Table A and the ruler 6 is 1/2 Zn2+. The compound of the formula L1, wherein the compounds are Het, R1, R2, R3 and R4 A group of Het, R1, R2, R3 and R4 of the compound corresponding to the compound of the formula y2Fe2+, wherein each of the compounds corresponds to one of the columns of Table A, and in each case corresponds to one of the columns of Table A and R6. For ZNi24 Table 20

[SI 149026.doc 52- 201103429 式1,1之化合物,其中化合物之Het、R丨、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為NH(CH3)3+ 表21 式Ll之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為NH(C2H5)3+ 表22 式L1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為 nh(ch2ch2ch2)3+ 表23 式1.1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為NH(CH(CH3)2)3 + 表24 式L1之化合物’其中化合物之Het、Ri、r2、R3及R4之 組合在各情況下對應於表A之一列且R6為 nh(ch2ch2ch2ch2)3+ 表25 式I· 1之化合物’其中化合物之Het ' R1、r2、R3及R4之 組合在各情況下對應於表A之一列且R6為甲基幾基 表26 式1.1之化合物’其中化合物之Het、R1、r2、r3及r4之 組合在各情況下對應於表A之一列且R6為乙基碳基 表27 式I · 1之化合物’其中化合物之Het、R1、r2、r3及r4之 149026.doc -53- 201103429 組合在各情況下對應於表A之一列且R6為丙基幾基 表28 式Ι·1之化合物’其中化合物之Het、、R2、r3&r4之 組合在各情況下對應於表A之一列且R6為異丙基幾基 表29 式1.1之化合物,其中化合物之Het、Ri、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為甲氧幾基 表30 式1.1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為乙氧幾基 表31 式1.1之化合物’其中化合物之Het、R丨、r2、R3&R4之 組合在各情況下對應於表A之一列且R6為丙氧幾基 表32 式L1之化合物’其中化合物之Het、R1、r2、r3及r4之 組合在各情況下對應於表A之一列且R6為異丙氧幾基 表33 式I·1之化合物,其中化合物之Het、R1、r2、r3及r4之 組合在各情況下對應於表A之一列且R6為苯氧羰基 表34 式I.1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為甲基胺基羰基 表35 式厂1之化合物,其中化合物之Het、R丨、R2、r3及R4之 [S1 149026.doc •54- 201103429 、’且0在各情況下對應於表A之一列且R6為乙基胺基羰基 表36 式Ll之化.合物,其中化合物iHet、R1、R2、R3及R4之 、组〇在各情況下對應於表A之一列且R6為丙基胺基羰基 ' 表37 ' 式U之化合物,其中化合物之Het、R1、R2、R3及R4之 '组合在各情況下對應於表A之一列且R6為異丙基胺基羰基 表38 式U之化合物,其中化合物之Het、R〗、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為苯基胺基羰基 表39 式Ll之化合物,其中化合物之Het、R1 ' R2、R3及R4之 組合在各情況下對應於表A之一列且R6為甲磺醯基 表40 式L1之化合物,其中化合物之Het、R1 ' R2、R3及R4之 組合在各情況下對應於表A之一列且R6為乙磺醯基 表41 式L 1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之/列且R6為丙磺醯基 表42 式I· 1之化合物,其中化合物之Het、Ri、R2、尺3及尺4之 組合在各情況下對應於表A之一列且R6為異丙磺醯基 表43 式I· 1之化合物,其中化合物之Het、R1、r2、r3及r4之 149026.doc -55- 201103429 組合在各情況下對應於表A之一列且R6為笨續醯基 表44 式L 1之化合物’其中化合物之Het、R1、r2、R3及R4之 組合在各情況下對應於表A之一列且R6為甲氧磺醯基 表45 式L 1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為乙氧項醯基 表46 式Ll之化合物,其中化合物之Het、R1、R2、R3&R4之 組合在各情況下對應於表A之一列且R6為丙氧續醯基 表47 式Ϊ.1之化合物,其中化合物之Het、R1、r2、R3及R4之 組合在各情況下對應於表A之一列且R6為異丙氧項醯基 表48 式之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為苯氧磺醯基 表49 式1之化合物’其中化合物之Het、R】、R2、R3及R4之 組合在各情況下對應於表A之一列且R6為CN 表50至98 式1.2之化合物’其中化合物之Het、r丨、R2、尺3及R4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表99至147 149026.doc[SI 149026.doc 52- 201103429 A compound of formula 1,1 wherein the combination of Het, R丨, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6 is NH(CH3)3+ A compound of the formula L1, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6 is NH(C2H5)3+ wherein the compound of the formula L1, wherein the compound is Het The combination of R1, R2, R3 and R4 corresponds in each case to one of the columns of Table A and R6 is nh(ch2ch2ch2)3+ the compound of the formula 1.1 in Table 23, wherein the combination of Het, R1, R2, R3 and R4 of the compound In each case, corresponding to one of the columns of Table A and R6 is NH(CH(CH3)2)3 + Table 24 Formula L1, wherein the combination of Het, Ri, r2, R3 and R4 of the compound corresponds in each case to A column of Table A and R6 is nh(ch2ch2ch2ch2)3+ Table 25 Compound of formula I·1 'wherein the combination of compounds Het' R1, r2, R3 and R4 corresponds in each case to one of Table A and R6 is A The compound of formula 1.1 wherein the combination of Het, R1, r2, r3 and r4 of the compound corresponds in each case to one of the columns of Table A and R6 is an ethyl carbon group. Table 27 Formula I · 1 The compound 'Het, R1, r2, r3 and r4 of the compound 149026.doc -53-201103429 combination in each case corresponds to one of the tables A and R6 is a propyl group of the compound of the formula 28·1 Wherein the combination of Het, R2, r3 & r4 of the compound corresponds in each case to one of the columns of Table A and R6 is an isopropyl group of the compound of the formula 1.1, wherein the compounds are Het, Ri, R2, R3 and R4 The combination in each case corresponds to one of the columns of Table A and R6 is a compound of the formula methoxy formula 30, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A. And R6 is an ethoxylated group of the compound of the formula 1.1 wherein the combination of Het, R丨, r2, R3 & R4 of the compound corresponds in each case to one of the columns of Table A and R6 is a propoxyl group. The compound 'in which the combination of Het, R1, r2, r3 and r4 of the compound corresponds in each case to one of the columns of Table A and R6 is a compound of the formula I.1 of the isopropoxyl group, wherein the compound Het, R1 The combination of r2, r3 and r4 corresponds in each case to one of the columns of Table A and R6 is a combination of phenoxycarbonyl group 34 and formula I.1. Wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6 is a compound of the formula 1 of the methylaminocarbonyl group, wherein the compound is Het, R丨, R2 [S1 149026.doc •54-201103429, 'and 0 in each case corresponds to one of the tables A and R6 is an ethylaminocarbonyl group of the formula L1, wherein the compound iHet, The group of R1, R2, R3 and R4, in each case corresponds to one of the columns of Table A and R6 is a propylaminocarbonyl group, the compound of the formula U, wherein the compounds are Het, R1, R2, R3 and R4 The 'combination in each case corresponds to one of the columns of Table A and R6 is a compound of the formula isopropylamine carbonyl group, wherein the combination of Het, R, R2, R3 and R4 of the compound corresponds in each case to Column A and R6 is a phenylaminocarbonyl group. Compounds of formula L1 wherein the combination of Het, R1 'R2, R3 and R4 of the compound corresponds in each case to one of Table A and R6 is methylsulfonyl. Table 40 Compounds of formula L1 wherein the combination of Het, R1 'R2, R3 and R4 of the compound corresponds in each case to one of Table A and R6 is ethyl sulfonate. The compound of the formula L1 wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the column of Table A and R6 is a compound of the formula I.1 of the propionyl group, Wherein the combination of Het, Ri, R2, 3 and 4 of the compound corresponds in each case to one of the columns of Table A and R6 is a compound of the formula I.1, wherein the compound is Het, R1. 149026.doc -55- 201103429 of r2, r3 and r4 The combination corresponds in each case to one of the columns of Table A and R6 is a compound of the formula L1, wherein the compounds are Het, R1, r2, R3 and The combination of R4 corresponds in each case to one of the columns of Table A and R6 is a compound of the formula methoxyl group, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the table. A compound of the formula A wherein R6 is an ethoxylated oxime group, wherein the combination of Het, R1, R2, R3 & R4 of the compound corresponds in each case to one of the columns of Table A and R6 is a propoxylated group. A compound of the formula 1.1, wherein the combination of Het, R1, r2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6 is isopropoxy A compound of the formula: wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6 is a phenoxysulfonyl group. The compound of the formula 1 wherein the compound The combination of Het, R], R2, R3 and R4 corresponds in each case to one of the columns of Table A and R6 is CN. Table 50 to 98 Compounds of the formula 1.2 wherein the compounds are Het, r丨, R2, 3 and R4 The combination corresponds in each case to one of the columns of Table A and R6 is as defined in any of Tables 1 to 49, tables 99 to 147 149026.doc

t SI -56· 201103429 式L3之化合物,其中化合物之Het、Ri、R2、尺3及尺4之 組合在各情況下對應於表A之〆列且R6係如在表i至49之任 一者中所定義 表148至196 式M之化合物,其中化合物之Het、R1、R2、…及尺4之 組合在各情況下對應於表A之一列且R6係如在表}至49之任 一者中所定義 表197至245 式L5之化合物,其中化合物之Het、R1、R2 ' “及尺4之 組合在各情況下對應於表A之一列且R6係如在表}至4 9之任 一者中所定義 表246至294 式L6之化合物,其中化合物之Het、Rl、R2、r3及μ之 組合在各情況下對應於表A之一列且R6係如在表丨至49之任 一者中所定義 表295至343 式[7之化合物,其中化合物之Het、R丨、R2、“及尺4之 組合在各情況下對應於表A之一列且R6係如在表丨至49之任 一者中所定義 表344至392 式L8之化合物,其中化合物之Het、Ri、R2、R3及R4之 組合在各情況下對應於表A之-列且R6係如在表!·之任 一者中所定義 表393至441 149026.doc -57· 201103429 式L9之化合物,其中化合物之Het、R1、r2、R3及尺4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者令所定義 表442至490 式1.1 0之化合物,其中化合物之Het、R1、r2、r3及r4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表491至539 式L11之化合物,其中化合物之Het、R1、R2、R3&R4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表540至588 式L12之化合物,其中化合物之Het、、R2、“及尺4之 組合在各情況下對應於表A之一列且R6係如在表!至49之任 一者中所定義 表589至637 式1.13之化合物,其中化合物之Het、ri、r2、R3及r4之 組合在各情況下對應於表A之一列且R6係如在表2至49之任 一者中所定義 表638至686 式M4之化合物,其中化合物之Het、R1、R2、R3&R4之 組合在各情況下對應於表A之一列且R6係如在表i至49之任 一者中所定義 表687至735 [S] 149026.doc -58- 201103429 式之化合物’其中化合物之Het、R1、r2、r3及r4之 組合在各情況下對應於表A之一列且R6係如在表1至的之任 一者中所定義 壬 表736至784 式之化合物’其中化合物之Het、Rl、R2、r3及μ之 組合在各情況下對應於表A之—列#係如在表149之任 一者中所定義 表785至833 式L17之化合物’其中化合物之Het、Ri、r2、尺3及汉4 組合在各情況下對應於表A之一列且R6係如在表丨至49之2 一者中所定義 表834至882 式1.18之化合物,其中化合物之Het、Ri、r2、汉3及尺4 組合在各情況下對應於表A之一列且尺6係如在表丨至49之2 一者中所定義 表883至931 式1.19之化合物’其中化合物之Het、Ri、R2、汉3及汉4之 組合在各情況下對應於表八之一列且r6係如在表丨至的之任 一者令所定義 表932至980 式1.20之化合物,其中化合物之Het、R]、r2、尺3及汉4之 組合在各情況下對應於表八之一列且R6係如在表^至的之任 一者中所定義 表981至1029 149026.doc .59- 201103429 式1.21之化合物,其中化合物之Het、R1、r2、r3及r4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表1030至1〇78 式1.22之化合物,其中化合物之Het、R1、r2、r3及r4之 組合在各情況下對應於表A之一列且R6係如在表i至49之任 一者中所定義 表 1079至1127 式1.23之化合物,其中化合物之Het、R1、R2、R3&R4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表 1128至 1176 式1_24之化合物’其中化合物之Het、R1、r2、R3及r4之 組合在各情況下對應於表A之一列且R6係如在表i至49之任 一者中所定義 表 1177至1225 式1.25之化合物,其申化合物之Het、r丨、2 八 κ及之 組合在各情況下對應於表A之一列且R6係如在表i至4 9之任 一者中所定義 表 1126至1274 式1.26之化合物,其中化合物之Het、R丨、r2 ' r3&r4 組合在各情況下對應於表A之一列且R6係如在表之任 一者中所定義 表 1275至1323 [S] 149026.doc •60- 201103429 式1_27之化合物,其中化合物之Het、Ri、r2 d3 a ^4 ^、κ及之 組合在各情況下對應於表A之一列且尺6係如在表1至49之任 一者中所定義 表 1324至1372 式1.28之化合物’其中化合物之Het、R!、尺2 ' r3及r4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表 1373至1421 式1.29之化合物,其中化合物之Het ' Ri、r2 ' ^及…之 組合在各情況下對應於表八之一列且R6係如在表i至49之任 一者中所定義 表 1422至1470 式1.30之化合物,其中化合物之Het、ri、R2、Rw之 組合在各情況下對應於表A之一列且尺6係如在表1至的之任 一者中所定義 表1471至1519 式1.31之化合物,其中化合物iHet、Ri、R2、R3及μ之 組合在各情況下對應於表A之一列且r6係如在表丨至的之任 . 一者中所定義 表1520至1568 式1.32之化合物’其中化合物之Het、ri、R2、R3及R4之 組合在各情況下對應於表A之一列且R6係如在表丨至的之任 一者中所定義 表 1569至1617 149026.doc 201103429 式1,33之化合物,其中化合物之Het、Ri、R2、R3及R4之 組合在各情況下對應於表A之一列且尺6係如在幻至 一者中所定義 表1618至1666 式1.34之化合物,其中化合物之^卜r,、R2、r3及y之 組合在各情況下對應於表A之-列且R6係如在表以钓之任 一者中所定義 表 1667至 1715 式1,35之化合物,其中化合物之Het、R1、R2、r3&r4 組合在各情況下對應於表A之一列且尺6係如在表丨至49之任 一者中所定義 表1716至1764 式1.36之化合物,其中化合物之Het、、R2、r3及Μ之 組合在各情況下對應於表A之一列且R6係如在表丨至的之任 一者中所定義 表 1765至 1813 式L37之化合物,其中化合物之Het、R1、R2、“及尺4之 組合在各情況下對應於表八之一列且R6係如在表1至竹之任 一者中所定義 表1814至1862 式L38之化合物,其中化合物之Het、R1、R2、R3及r4之 組合在各情況下對應於表A之一列且R6係如在表1至4 9之任 一者中所定義 表 1863至 1911 149026.doc m •62- 201103429 式1.39之化合物,其中化合物之Het、Ri、R2、r3及r4之 組合在各情況下對應於表A之一列且R6係如在表i至49之任 一者中所定義 表 1912至I960 式1.40之化合物,其中化合物之Het、Ri、R2 ' “及^之 組合在各情況下對應於表A之一列且R6係如在表i至49之任 一者中所定義 表 1961至 2009 式1.41之化合物,其中化合物之只6{'1^1、尺2、汉3及汉4之 組合在各情況下對應於表A之一列且R6係如在表i至49之任 一者中所定義 表 2010至 2058 式1,42之化合物’其中化合物之Het、R!、R2、尺3及尺4之 組合在各情況下對應於表A之一列且尺6係如在表1至49之任 一者中所定義 表 2059至 2107 式Ι·43之化合物’其中化合物之Het、r|、r2、尺3及尺4之 組合在各情況下對應於表A之一列且R6係如在表}至49之任 一者中所定義 表 2108至 2156 式Ι·44之化合物,其中化合物之Het、Ri、r2、…及尺4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表 2157至 2205 149026.doc •63- 201103429 式1.45之化合物,其中化合物之^1、1^、112、113及114之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表2206至2254 式1.46之化合物,其中化合物之Het、R1、r2、…及^^之 組合在各情況下對應於表A之一列且R6係如在表!至49之任 一者中所定義 表 2255至 2303 式1.47之化合物’其中化合物之Het、R1、R2、R3&R4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表 2304至 2352 式1.48之化合物,其中化合物之Het、Ri、r2、…及尺4之 組合在各情況下對應於表A之一列且R6係如在表1至49之任 一者中所定義 表 2353 式1.49之化合物’其中化合物之Het、Ri、R2、r3及r4之 組合在各情況下對應於表A之一列 表 2354 式L5〇之化合物,其中化合物之Het、R1 ' R2、R3及R4之 組合在各情況下對應於表A之一列 表 2355 式L51之化合物,其中化合物之Het、R1、R2、rW之 、·且&在各情况下對應於表A之一列 tt SI -56· 201103429 A compound of formula L3 wherein the combination of Het, Ri, R2, 3 and 4 of the compound corresponds in each case to the list of Table A and R6 is as in any of Tables i to 49. The compounds of formula 148 to 196 are defined in the formula, wherein the combination of Het, R1, R2, ... and 4 of the compound corresponds in each case to one of the columns of Table A and R6 is as in any of Tables} to 49. The compounds of formula 197 to 245, formula L5, wherein the combination of Het, R1, R2' and the ruler 4 of the compound correspond in each case to one of the columns of Table A and R6 is as in Tables to 49. A compound of the formula L246, wherein the combination of Het, R1, R2, r3 and μ of the compound corresponds in each case to one of the columns of Table A and R6 is as defined in any one of Tables to 49. Tables 295 to 343 are defined as compounds of formula [7, wherein the combination of Het, R丨, R2, "and 4" of the compound corresponds in each case to one of Table A and R6 is as shown in Tables to 49. The compounds of the formulae 344 to 392 of the formula L8, wherein the combination of Het, Ri, R2, R3 and R4 of the compound corresponds in each case to the column of Table A and R 6 series as in the table! Any of the compounds of formula L9, wherein the combination of Het, R1, r2, R3 and 4 of the compound corresponds in each case to one of Table A and is defined in any one of the tables 393 to 441 149026.doc -57·201103429 R6 is a compound of the formula 442 to 490, formula 1.1, as defined in any one of Tables 1 to 49, wherein the combination of Het, R1, r2, r3 and r4 of the compound corresponds in each case to one of Table A and R6 is a compound of formula 491 to 539, formula L11, as defined in any one of Tables 1 to 49, wherein the combination of Het, R1, R2, R3 & R4 of the compound corresponds in each case to one of Table A and R6 A compound of the formula 540 to 588 of the formula L12 as defined in any one of Tables 1 to 49, wherein the combination of Het, R2, "and 4" of the compound corresponds in each case to one of the columns of Table A and the R6 system The compounds of Tables 1.183 to 637 are as defined in any one of Tables to 49, wherein the combination of Het, ri, r2, R3 and r4 of the compound corresponds in each case to one of Table A and R6 is as Tables 638 to 686 are compounds of formula M4 as defined in any one of Tables 2 to 49, wherein the compounds are Het, R1, R2, R3 & R4 In each case, it corresponds to one of the columns of Table A and R6 is as defined in any of Tables i to 49. Tables 687 to 735 [S] 149026.doc -58- 201103429 Compounds of the formula 'Het, The combination of R1, r2, r3 and r4 corresponds in each case to one of the columns of Table A and R6 is as defined in any of Tables 1 to 化合物 compounds of the formula 736 to 784, wherein the compounds are Het, Rl The combination of R2, r3 and μ corresponds in each case to Table A. Column # is a compound of the formula 785 to 833 of the formula L17 as defined in any of Table 149, wherein the compound Het, Ri, r2 The combination of Rule 3 and Han 4 corresponds in each case to one of the columns of Table A and R6 is a compound of the formula 834 to 882 formula 1.18 as defined in Table 2 to 49, wherein the compound Het, Ri, r2 The combination of Han 3 and Rule 4 corresponds in each case to one of the columns of Table A and the rule 6 is as shown in Tables 丨 to 49 of 2, Table 883 to 931, the compound of the formula 1.19, in which the compound Het, Ri, R2 The combination of Han 3 and Han 4 corresponds to one of the eight tables in each case and r6 is as defined in any of the tables 932 to 980. The compound of .20, wherein the combination of the compound Het, R], r2, amp 3 and han 4 corresponds in each case to one of the columns of Table 8 and R6 is as defined in any of Tables 981. To 1029 149026.doc .59-201103429 A compound of formula 1.21 wherein the combination of Het, R1, r2, r3 and r4 of the compound corresponds in each case to one of the columns of Table A and R6 is as in any of Tables 1 to 49. The compounds of formula 1.32 are defined in Tables 1030 to 1〇78, wherein the combination of Het, R1, r2, r3 and r4 of the compound corresponds in each case to one of Table A and R6 is as shown in Tables i to 49. The compounds of the formulae 1.27 to 1127, formula 1.23, wherein the combination of Het, R1, R2, R3 & R4 of the compound corresponds in each case to one of the columns of Table A and R6 is as in any of Tables 1 to 49. Tables 1128 to 1176 are defined as compounds of formula 1-24, wherein the combination of Het, R1, r2, R3 and r4 of the compound corresponds in each case to one of the columns of Table A and R6 is as in any of Tables i to 49. The compounds of the formula 1.25 to 1225 are defined in the formula 1.25 to 1225, and the combination of the compounds Het, r丨, 2 VIII and the combination thereof are in each case And a compound of the formula 1.26 to 1274, formula 1.26, as defined in any one of Tables i to 49, wherein the combination of Het, R丨, r2 'r3 & r4 of the compound corresponds in each case Listed in Table A and R6 is as defined in any of the Tables Tables 1275 to 1323 [S] 149026.doc • 60-201103429 Formula 1-27, wherein the compound Het, Ri, r2 d3 a ^4 ^ The combination of κ and κ corresponds in each case to one of the columns of Table A and the ultra 6 is as defined in any of Tables 1 to 49. Table 1324 to 1372 The compound of the formula 1.28, wherein the compound is Het, R! The combination of 2 'r3 and r4 corresponds in each case to one of the columns of Table A and R6 is a compound of the formula 1.37 to 1421 of the formula 1.29 as defined in any one of Tables 1 to 49, wherein the compound Het ' Ri, r2 The combination of '^ and ... corresponds in each case to one of the columns of Table 8 and R6 is a compound of the formula 1.42 to 1470 of the formula 1.30 as defined in any one of Tables i to 49, wherein the compound Het, ri, R2 The combination of Rw corresponds in each case to one of the columns of Table A and the ruler 6 is as defined in any of Tables 1 to 1147 to 1519. The compound of .31, wherein the combination of the compounds iHet, Ri, R2, R3 and μ corresponds in each case to one of the columns of Table A and the r6 is as defined in Tables 1520 to 1568. 1. The compound of 1.32 wherein the combination of Het, ri, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6 is as defined in any of Tables 1 to 1617 149026. Doc 201103429 The compound of formula 1,33, wherein the combination of Het, Ri, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and the ruler 6 is as defined in Tables 1618 to 1666 as defined in the phantom to one. A compound of formula 1.34, wherein the combination of compounds, r, R2, r3 and y, in each case corresponds to the column of Table A and R6 is as defined in Table 1667 to 1715 as defined in any of the fishing. A compound of formula 1,35 wherein the combination of Het, R1, R2, r3 & r4 of the compound corresponds in each case to one of the columns of Table A and Rule 6 is as defined in Table 1716 as defined in any of Tables 4949 to 1764 A compound of formula 1.36 wherein the combination of Het, R2, r3 and hydrazine of the compound corresponds in each case to one of the columns of Table A and R6 A compound of the formula L1, R1, R2, "and the ruler 4 of the compound, as defined in any of the above, wherein the combination of Het, R1, R2, "and the ruler 4 of the compound corresponds in each case to the column of Table 8 and R6 A compound of the formula L18, as defined in any one of Tables 1 to 5, wherein the combination of Het, R1, R2, R3 and r4 of the compound corresponds in each case to one of the columns of Table A and the R6 system A compound of the formula 1.39 to 1911 149026.doc m • 62-201103429, wherein the combination of Het, Ri, R2, r3 and r4 of the compound corresponds in each case, as defined in any of Tables 1 to 49. And the combination of Het, Ri, R2 '" and ^ of the compound in each case corresponds to each of the compounds of Tables 1912 to I960 as defined in any one of Tables i to 49. A column of Table A and R6 is a compound of the formula 1961 to 2009 formula 1.41 as defined in any one of Tables i to 49, wherein the compound is only a combination of 6{'1^1, 2, 2, and 4 In each case corresponds to one of the columns of Table A and R6 is as defined in any of Tables i to 49. Tables 2010 to 2058 Formula 1, 42 The combination of Het, R!, R2, Ruler 3 and Ruler 4 of the compound in each case corresponds to one of Table A and Rule 6 is as defined in Tables 20 to 2107 as defined in any of Tables 1 to 49. A compound of the formula '43 wherein the combination of Het, r|, r2, 尺3 and 尺4 of the compound corresponds in each case to one of the columns of Table A and R6 is as defined in any of Tables 至49 Tables 2108 to 2156 are compounds of the formula: wherein the combination of Het, Ri, r2, ..., and 4 of the compound corresponds in each case to one of the columns of Table A and R6 is as in any of Tables 1 to 49. Tables 2157 to 2205 149026.doc • 63- 201103429 Compounds of the formula 1.45, wherein the combination of compounds 1, 1 , 112, 113 and 114 corresponds in each case to one of the tables A and the R 6 is as shown in the table. The compounds of the formulae 2206 to 2254, formula 1.46, as defined in any one of 1 to 49, wherein the combination of Het, R1, r2, ..., and ^^ of the compound corresponds in each case to one of the columns of Table A and the R6 is as shown in the table. ! Tables 2255 to 2303, as defined in any one of the formulas of formula 1.47 to 2303, wherein the combination of Het, R1, R2, R3 & R4 of the compound corresponds in each case to one of the columns of Table A and R6 is as shown in Table 1 to The compounds of Tables 1.48 to 2352, formula 1.48, as defined in any one of 49, wherein the combination of Het, Ri, r2, ..., and 4 of the compound corresponds in each case to one of Table A and R6 is as in Table 1 to The compound of formula 1.49 as defined in any one of 49' wherein the combination of Het, Ri, R2, r3 and r4 of the compound corresponds in each case to a compound of the formula 2354, formula L5, wherein the compound The combination of Het, R1 'R2, R3 and R4 corresponds in each case to the compound of the formula L2, formula L51, wherein the compounds Het, R1, R2, rW, and & in each case correspond to One of the tables A t

149026.doc • 64 - 201103429 表 2356 式1.52之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2357 式1.53之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2358 式1.54之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2359 式1.55之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2360 式1.5 6之化合物,其中化合物之1^1、111、112、113及114之 組合在各情況下對應於表A之一列 表 2361 式1.5 7之化合物,其中化合物之1^1、111、112、113及114之 組合在各情況下對應於表A之一列 表 2362 式1.58之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2363 式1.59之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 149026.doc -65· 201103429 表 2364式1.6〇之化合物,其中化合物之只61、尺1、 組合在各情況下對應於表A之一列 表 2365 式1.61之化合物,其中化合物之Het、R丨、 ,组合在各情況下對應於表A之一列 表 2366 式1.62之化合物,其中化合物之Het、R1 組合在各情況下對應於表A之一列 表 2367 式L63之化合物,其中化合物之Het、R1 組合在各情況下對應於表A之一列 表 2368 式L64之化合物,其中化合物之Het、R1 組合在各情況下對應於表A之一列 表 2369 式L65之化合物,其中化合物之Het、R1 組合在各情況下對應於表A之一列 表 2370 式1.66之化合物,其中化合物之Het、R1 ,组合在各情況下對應於表A之一列 表 237 1 式1.67之化合物,其中化合物之Het、R1 組合在各情況下對應於表A之一列 R2、R3 及 R4 之 R2、R3 及 R4 之 R2、R3 及 R4 之 R2、R3 及 R4 之 R2、R3 及 R4 之 R2、R3 及 R4 之 R2、R3 及 R4 之 R2、R3 及 R4 之 t S1 149026.doc -66- 201103429 表 2372 式1.68之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2373 式1.69之化合物,其中化合物之Het、R〗、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2374 式1.70之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2375 式1.71之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2376 式1.72之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2377 式1.73之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2378 式1.74之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2379 式1.75之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 149026.doc -67- 201103429 表 2380 式1.76之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2381 式1.77之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2382 式1.78之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2383 式1.79之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2384 式1.80之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2385 式1.81之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2386 式1.82之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2387 式1.83之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表Α之一列 [S1 149026.doc -68- 201103429 表 2388 式1.84之化合物,其中化合物之《^、111、112、113及114之 組合在各情況下對應於表A之一列 表 2389 式1.85之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2390 式1.86之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2391 式1.87之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2392 式1.88之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2393 式1.89之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2394 式1.90之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表2395 * 式1.91之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下’對應於表A之一列 149026.doc •69- 201103429 表 2396 式L92之化合物,其中化合物之Het、Ri、R2、R^R4之 組合在各情況下對應於表A之一列 表 2397 式L93之化合物’其中化合物之Het、R1、R2、R3及R4之 組合在各情况下對應於表A之一列 表 2398 式1,94之化合物,其中化合物之Het、R丨、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2399 式1,95之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列 表 2400 式L96之化合物,其中化合物之Het、Ri、R2、R3及R4之 組合在各情況下對應於表a之一列 表 2401 式11,1之化合物,其中化合物之Het、R丨、R2、R3及R4之 組合在各情況下對應於表A之一列且1163為Η 表 2402 式Π.1之化合物,其中化合物之Het、R1、R2、R3及R4之 ,、且〇在各情況下對應於表A之一列且R6a為曱基 表 2403 式Π.1之化合物,其中化合物之Het、r1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為乙基 I49026.doc 201103429 表 2404 式Π.1之化合物,其中化合物之Het、ri、R2、R3及R4之 組合在各情況下對應於表A之一列且為正丙基 表 2405 式H.1之化合物,其中化合物之Het、R丨、R2、R3及R4之 組合在各情況下對應於表A之一列且R&為異丙基 表 2406 式II. 1之化合物,其中化合物之Het、Ri、r2、r3及r4之 組合在各情況下對應於表A之一列且為正丁基 表 2407 式II. 1之化合物,其中化合物之Het、R丨、r2、R3及r4之 組合在各情況下對應於表A之一列且R6a為第二丁基 表 2408 式II. 1之化合物’其中化合物之Het、R丨、r2、r3及r4之 組合在各情況下對應於表A之一列且為異丁基 表 2409 式II· 1之化合物’其中化合物之Het、r1、r2、r3及r4之 組合在各情況下對應於表A之一列且R6a為第三丁基 表 2410 式Η. 1之化合物’其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為苯基 表 2411 式Π· 1之化合物’其中化合物之Het、Rl、R2、R3及R4之 '组合在各情況下對應於表A之一列且R6a為苄基 149026.doc -71· 201103429 表 2412 式Π·1之化合物,其中化合物之Het、r1、r2、之 組合在各情況下對應於表A之一列且R6a為曱基羰基 表 2413 式IL1之化合物,其中化合物之Het、R1 ' R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為乙基羰基 表 2414 式IM之化合物,其中化合物之Het、Ri、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為丙基羰基 表 2415 式11,1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為異丙基羰基 表 2416 式IL1之化合物’其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為笨基羰基 表 2417 式II. 1之化合物’其中化合物之Het、ri、r2、r3及r4之 組合在各情況下對應於表A之一列且R6a為甲氧羰基 表 2418 式Π.1之化合物’其中化合物之Het、R1、R2、R3及尺4之 組合在各情況下對應於表A之一列且R6a為乙氧羰基 表 2419 式II_ 1之化合物,其中化合物之Het、ri、r2、R3及r4之 組合在各情況下對應於表A之一列且R6a為丙氧羰基 [S1 149026.doc •72- 201103429 表 2420 式II. 1之化合物,其中化合物之Het、R1、r2、R3及R4之 組合在各情況下對應於表A之/列且R6a為異丙氧羰基 表 2421 式IL1之化合物’其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為苯氧羰基 表 2422 式Π.1之化合物’其中化合物之Het ' R1、R2、R3及R4之 組合在各情況下對應於表A之一列且為甲基胺基羰基 表 2423 式Π·1之化合物,其中化合物之Het、R丨、R2、R3及R4之 組合在各情況下對應於表A之一列且為乙基胺基羰基 表 2424 式Π.1之化合物’其中化合物之Het、R1、R2、R3及R4之 組合在各情况下對應於表A之一列且R6 a為丙基胺基羰基 表 2425 式IL1之化合物’其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為異丙基胺基羰基 表 2426 式Η. 1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且尺以為苯基胺基羰基 表 2427 式Π.1之化合物’其中化合物之Het、Ri、R2、R3及R4之 組合在各情況下對應於表A之一列且R 6 a為曱磺醯基 149026.dc -73- 201103429 表 2428 式Π.1之化合物’其中化合物之Het、ri、r2、R3及R4之 組合在各情況下對應於表A之一列且R6a為乙績醯基 表 2429 式Π.1之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為丙磺醯基 表 2430 式Π.1之化合物’其中化合物之Het、Ri、r2、R3及R4之 組合在各情況下對應於表A之一列且為異丙磺醯基 表 2431 式Π.1之化合物’其中化合物之Het、Ri、r2、R3及R4之 組合在各情況下對應於表A之一列且R6a為苯磺醯基 表 2432 式Π·1之化合物,其中化合物之Het、Ri、R2、以及尺4之 組合在各情況下對應於表A之一列且為甲氧磺醯基 表 2433 式π.ι之化合物,其中化合物之Het、Rl、r2、r3及r4之 組合在各情況下對應於表A之一列且R6a為乙氧磺醯基 表 2434 式π·ι之化合物,其中化合物之Het、Rl、R2、R3及R4之 組合在各情況下對應於表八之一列且為丙氧磺醯基 表 2435 式π.1之化合物,其中化合物之Het、Rl、Μ、r3及μ之 組合在各情況下對應於表八之一列且為異丙氡績醯基之 149026.doc149026.doc • 64 - 201103429 Table 2356 Compound of formula 1.52 wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of formula 2357, formula 1.53, wherein the compound is Het, The combination of R1, R2, R3 and R4 corresponds in each case to the compound of formula 1.54, formula 1.54, wherein the combination of compounds Het, R1, R2, R3 and R4 corresponds in each case to one of Table A The compound of formula 1.55, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of the formula 2360, formula 1.56, wherein the compound is 1^1, 111, 112, The combination of 113 and 114 corresponds in each case to the compound of formula 2361, formula 1.57 of Table A, wherein the combination of compounds 1^1, 111, 112, 113 and 114 corresponds in each case to a list of Table A 2362 A compound of the formula 1.58, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of the formula 2, formula 1.59 of Table A, wherein the compounds are Het, R1, R2, R3 and R4 The combination corresponds to one of the columns in Table A in each case 149026.doc -65· 201103429 Table 2364 Compounds of formula 1.6, wherein the combination of only 61 and 1 of the compound corresponds in each case to the compound of formula 2365, formula 1.61, wherein the compound is Het, R丨, , in each case corresponding to the compound of the formula 2366, formula 1.62, wherein the combination of Het and R1 of the compound corresponds in each case to the compound of the formula 2367, formula L63, wherein the compound Het, R1 combination In each case corresponds to the compound of the formula L2 in the formula 2368, wherein the Het, R1 combination of the compounds corresponds in each case to the compound of the formula 2369, formula L65, wherein the compound Het, R1 is combined in each In the case of a compound of the formula 16.6, formula 1.66, wherein the compound Het, R1, in each case corresponds to the compound of the formula 237 1 formula 1.67, wherein the compound Het, R1 is combined In the case, R2 of R2, R3 and R4 of R2, R3 and R4, R2 of R3, R3 and R4, R2 of R3 and R4, R2 of R4 and R4 of R4, R2, R3 and R4 of R4 R2, R3 And R4 t S1 149026.doc -66- 201103429 Table 2372 Compound of formula 1.68, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of formula 2373, formula 1.69, of Table A, Wherein the combination of Het, R, R2, R3 and R4 of the compound corresponds in each case to the compound of the formula 2374, formula 1.70 of Table A, wherein the combination of Het, R1, R2, R3 and R4 of the compound is in each case Corresponding to a compound of the formula 2375, formula 1.71, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of the formula 2376, formula 1.72, wherein the compound Het, R1 The combination of R2, R3 and R4 corresponds in each case to the compound of the formula 2377 Formula 1.73 of Table A, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to a list of Table A 2378 A compound of formula 1.74 wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of formula 2.379, formula 1.75 of Table A, wherein the compounds are Het, R1, R2, R3 and R4 The combination corresponds to Table A in each case Column 149026.doc -67- 201103429 Table 2380 Compound of formula 1.76, wherein the combination of compounds Het, R1, R2, R3 and R4 corresponds in each case to the compound of formula 2.81, formula 1.77, wherein the compound is Het The combination of R1, R2, R3 and R4 corresponds in each case to the compound of formula 2.38, formula 1.78 of Table A, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to Table A. A list of compounds of formula 2.39, formula 1.79, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of formula 2.38, formula 1.80 of Table A, wherein the compounds are Het, R1, R2, R3 and The combination of R4 corresponds in each case to the compound of formula 1.81, formula 1.81, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of formula 1.82, formula 1.82, in Table A. , wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of the formula 1387, formula 1.83, wherein the combination of Het, R1, R2, R3 and R4 of the compound is in each case Corresponds to one of the tables [S1 1490 26.doc-68-201103429 Table 2388 Compounds of the formula 1.84, wherein the combination of the compounds "^, 111, 112, 113 and 114 corresponds in each case to the compound of the formula 2.85 of the formula A, wherein the compound Het The combination of R1, R2, R3 and R4 corresponds in each case to the compound of formula 1390, formula 1.86 of Table A, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to Table A. A list of compounds of formula 1.87, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of the formula 1.88, formula 1.88 of Table A, wherein the compounds are Het, R1, R2, R3 and The combination of R4 corresponds in each case to the compound of formula 1.99 of Table A, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of formula 2394, formula 1.90, of Table A. , wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of the formula 2395 * Formula 1.91 of Table A, wherein the combination of Het, R1, R2, R3 and R4 of the compound is in each case Below 'corresponds to one of the columns in Table A 149026.do c • 69- 201103429 Table 2396 Compound of formula L92 wherein the combination of Het, Ri, R2, R^R4 of the compound corresponds in each case to one of the compounds in Table 2397, formula L93, in which the compound Het, R1 The combination of R2, R3 and R4 corresponds in each case to the compound of the formula 1398, formula 1, 94, wherein the combination of Het, R丨, R2, R3 and R4 of the compound corresponds in each case to Table A. A list of compounds of formula 1,399, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to the compound of formula 2400, formula L96, wherein the compound is Het, Ri, R2. The combination of R3 and R4 corresponds in each case to a compound of the formula 2, Formula 2, Formula 11, 1 wherein the combination of Het, R丨, R2, R3 and R4 of the compound corresponds in each case to one of Table A and 1163 is 化合物 Table 2402 A compound of the formula 1.1, wherein the compound is Het, R1, R2, R3 and R4, and 〇 in each case corresponds to one of the columns of Table A and R6a is a fluorenyl group 2403 Formula Π.1 a compound wherein the combination of Het, r1, R2, R3 and R4 of the compound corresponds in each case to Table A And R6a is an ethyl group I49026.doc 201103429 Table 2404 A compound of the formula 1.1, wherein the combination of Het, ri, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and is a n-propyl form. 2405 A compound of the formula H.1, wherein the combination of Het, R丨, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R& is a compound of the formula II. The combination of Het, Ri, r2, r3 and r4 of the compound corresponds in each case to one of the columns of Table A and is a compound of the formula 1-4, formula II.1, wherein the compounds are Het, R丨, r2, R3 and r4 The combination in each case corresponds to one of the columns of Table A and R6a is the second butyl group 2408. The compound of formula II.1 wherein the combination of Het, R丨, r2, r3 and r4 of the compound corresponds in each case to the table. One of A is an isobutyl group 2409. The compound of formula II.1 wherein the combination of Het, r1, r2, r3 and r4 of the compound corresponds in each case to one of the columns of Table A and R6a is the third butyl table 2410. The compound of formula 1 wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to Table A And R6a is a compound of the formula phenyl group 2411, wherein 'the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6a is benzyl 149026.doc-71 · 201103429 Table 2412 Compound of the formula ,1, wherein the combination of Het, r1, r2 of the compound corresponds in each case to one of the columns of Table A and R6a is a compound of the formula 11 carbonyl of the fluorenylcarbonyl group 2413, wherein the compound Het, The combination of R1 'R2, R3 and R4 corresponds in each case to one of the columns of Table A and R6a is a compound of the formula E., wherein the combination of Het, Ri, R2, R3 and R4 of the compound is in each case Corresponding to a column of Table A and R6a is a propylcarbonyl group 2415, a compound of formula 11,1 wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6a is isopropyl. The carbonyl group of the compound of the formula IL1 wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6a is a phenyl group of the formula 2417. The compound of the formula II. The combination of Het, ri, r2, r3 and r4 corresponds to one of Table A in each case And R6a is a methoxycarbonyl group 2418. The compound of formula '.1 wherein the combination of Het, R1, R2, R3 and 4 of the compound corresponds in each case to one of the columns of Table A and R6a is ethoxycarbonyl. A compound of II-1 wherein the combination of Het, ri, r2, R3 and r4 of the compound corresponds in each case to one of Table A and R6a is propoxycarbonyl [S1 149026.doc • 72-201103429 Table 2420 Formula II. 1 a compound wherein the combination of Het, R1, r2, R3 and R4 of the compound corresponds in each case to the column of Table A and R6a is isopropoxycarbonyl. Table 2421 Compound of formula IL1 wherein the compound is Het, R1, R2 The combination of R3 and R4 in each case corresponds to one of the columns of Table A and R6a is a phenoxycarbonyl group. The compound of the formula 22.1, wherein the combination of Het 'R1, R2, R3 and R4 of the compound corresponds in each case. A compound of the formula A, wherein the combination of Het, R, R 2 , R 3 and R 4 of the compound corresponds in each case to one of the columns of Table A and is ethyl. Aminocarbonyl group 2424 A compound of formula 11, wherein a combination of Het, R1, R2, R3 and R4 of the compound In each case, corresponding to one of the columns of Table A and R6 a is a propylaminocarbonyl group 2425, a compound of the formula IL1 wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the tables A and R6a is an isopropylaminocarbonyl group of the compound of formula 2626, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and is a phenylaminocarbonyl group. 2427 A compound of the formula 11 wherein the combination of Het, Ri, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R 6 a is sulfonyl 149026.dc -73- 201103429 Table 2428 A compound of the formula 11 wherein the combination of Het, ri, r2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6a is a compound of the formula 4291, 2, wherein the compound The combination of Het, R1, R2, R3 and R4 corresponds in each case to one of the columns of Table A and R6a is a compound of the formula propylsulfonyl group 2430, wherein the compounds are Het, Ri, r2, R3 and R4 Combinations in each case corresponding to one of the columns of Table A and being a compound of the formula isopropyl sulfonyl group 2431 Π.1 The combination of Het, Ri, r2, R3 and R4 corresponds in each case to one of the columns of Table A and R6a is a compound of the formula phenylsulfonyl group 2432, wherein the compound is Het, Ri, R2, and 4 The combination in each case corresponds to a compound of the formula A and is a compound of the formula oxime oxime 2433, wherein the combination of Het, Rl, r2, r3 and r4 of the compound corresponds in each case to Table A. And R6a is a compound of ethoxysulfonyl group 2434, π·ι, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of Table 8 and is propoxysulfonyl. Table 2435 Compound of the formula π.1, wherein the combination of Het, Rl, Μ, r3 and μ of the compound corresponds in each case to one of the columns of Table VIII and is isopropyl 氡 149 026.doc

[SI -74 · 201103429 表 2436 式Η.1之化合物’其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a為苯氧磺醯基 表 2437 式Π. 1之化合物,其中化合物之Het、r1、r2、r3及r4之 組合在各情況下對應於表A之一列且R&為cn 表2438至2474 式II.2之化合物’其中化合物之fjet、R1、R2、尺3及R4之 組合在各情況下對應於表A之一列且R&係如在表24〇1至 2437之任一者中所定義 表2475至2511 式Π.3之化合物,其中化合物之Het、R1、R2、尺3及尺4之 組合在各情況下對應於表A之一列且R“係如在表24〇1至 2437之任一者中所定義 表2512至2548 式Π.4之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R6a係如在表24〇1至 2437之任一者中所定義 表2549至2585 式II.5之化合物,其中化合物之Het、R1、R2、R3及R4之 組合在各情況下對應於表A之一列且R&係如在表24〇ι至 2437之任一者中所定義 表2586至2622 式Π·6之化合物,其中化合物之Het、R1、R2、Rw之 149026.doc •75- 201103429 組合在各情況下對應於表A之〆列且尺63係如在表24〇1至 2437之任一者中所定義 表2623至2659 式ΙΙ·7之化合物,其中化合物之Het、R丨、R2、R3及R4之 組合在各情況下對應於表A之,列且尺“係如在表240丨至 2437之任一者中所定義 表 2660至 2696 式Π,8之化合物,其中化合物之Het、R丨、r2、R3及R4之 組合在各情況下對應於表A之一列且尺“係如在表24〇1至 2437之任一者中所定義 表 2697至 2733 式Π·9之化合物,其中化合物之Het、R1、r2、R3及R4之 組合在各情況下對應於表A之一列且R“係如在表24〇1至 2437之任—者中所定義 表 2734至 2770 式1110之化合物,其中化合物之Het、R1、R2、尺3及R4 之組合在各情況下對應於表A之-列且R“係如在表24〇1至 2437之任—者中所定義 表 2771至 2807 ‘ Rl、R2、R3 及 R4 63係如在表2401至 式11,11之化合物’其中化合物之Het, 之組合在各情況下對應於表A之一列且汉 2437之任一者中所定義 表2808至2844 式11.12之化合物,其中化合物之1^、尺1、尺2、&3及尺 [.S] 149026.doc •76- 201103429 之組合在各情況下對應於表A之一列且玟63係如在表24〇1至 2437之任一者中所定義 表 2845至 2881 式Π·13之化合物,其中化合物之Het ' R1、r2、r3&r4 之組合在各情況下對應於表A之一列且R6a係如在表24〇1至 2437之任一者中所定義 表2882至2918 式11.14之化合物,其中化合物之11^、11丨、112、汉3及汉4 之組合在各情況下對應於表A之一列且係如在表24〇1至 2437之任一者中所定義 表2919至2955 式Π.15之化合物,其中化合物之fjet、Ri、r2、尺3及尺4 之組合在各情況下對應於表A之一列且尺63係如在表2401至 2437之任一者中所定義 表 2956至 2992 式11.16之化合物’其中化合物之^^、111、1^2、尺3及尺4 之組合在各情況下對應於表A之一列且係如在表24〇丨至 2437之任一者中所定義 表2993至3029 式11.17之化合物,其中化合物之1^'111、1^、113及1^4 之組合在各情況下對應於表A之一列且尺63係如在表24〇 j至 2437之任一者中所定義 表3030至3066 式II. 1 8之化合物,其中化合物之Het、R1、r2、r3及r4 149026.doc -77- 201103429 之組合在各情況下對應於表A之〆列且R6a係如在表240 1至 2437之任一者中所定義 表3067至3103 之組合在各情況下對應於表A之〆列且R6a係如在表240 1至 2437之任一者中所定義 表 3104至 3140 式IL20之化合物,其中化合物之Het、R1、R2、尺3及R4 之組合在各情況下對應於表A之〆列且尺“係如在表2401至 2437之任一者中所定義 表3141至3177 式II.21之化合物,其中化合物之Het、R丨、R2、R3及R4 之組合在各情況下對應於表A之-·•列且尺63係如在表2401至 2斗37之任一者中所定義 表3178至3214 式II.22之化合物,其中化合物之Het、R1、r2、r3及r4 之組合在各情況下對應於表A之一列且R6a係如在表24〇1至 2437之任一者中所定義 表3215至3251 式11.23之化合物,其中化合物之1^、尺1、尺2、113及114 之組合在各情況下對應於表八之一列且係如在表24〇1至 2437之任一者中所定義 表 3252至 3288 式11.24之化合物,其中化合物iHet、Ri、R2、R3及R4 ί 149026.doc •78- 201103429 之組合在各情況下對應於表A之一列且R6a係如在表24〇丨至 2437之任一者中所定義 表3289至3325 式Π·25之化合物,其中化合物之Het、R1、R2、r3&r4 之組合在各情況下對應於表A之一列且R6a係如在表24〇〖至 2437之任一者中所定義 表 3326至 3362 式Π.26之化合物,其中化合物之Het、R〗、R2、尺3及R4 之組合在各情況下對應於表A之一列且1163係如在表24〇1至 2437之任一者中所定義 表3363至3399 式Π.27之化合物,其中化合物之Het、R1、R2、R3及R4 之組合在各情況下對應於表A之一列且Rea係如在表MW至 2437之任一者中所定義 表3400至3436 式II.28之化合物,其中化合物之_、Rl、R2、R3及r4 之組合在各情況下對應於表A之一列且R&係如在表24〇1至 2斗37之任一者中所定義 表 3437至 3473 式Π.29之化合物,其中化合物之Het、Rl、R2、r3及μ 之組合在各情況下對應於表Α之-列且R“係如在表24〇1至 2437之任一者中所定義 表 3474至 3510 式Π·30之化合物,其中化合物之Het、R1、R2、…及厌4 149026.doc -79- 201103429 之組合在各情況下對應於表A之一列且尺6&係如在表2401至 2437之任—者中所定義 表3511至3547 式II.3 1之化合物,其中化合物之j|et、R1、r2、r3及r4 之組合在各情況下對應於表A之一列且R6a係如在表24〇丨至 2437之任—者中所定義 表3548至3584 式11.32之化合物,其中化合物之Het、R1、r2、r3及r4 之組合在各情況下對應於表A之一列且R6a係如在表24〇1至 2437之任一者中所定義 表3585至3621 式Π·33之化合物,其中化合物之Het、R1、r2、R3及R4 之組合在各情況下對應於表A之一列且Rea係如在表24〇ι至 2437之任一者中所定義 表3622至3658 式Π.34之化合物’其中化合物之Het、Ri、R2、尺3及R4 之組合在各情況下對應於表A之一列且Rea係如在表24〇1至 2437之任一者中所定義 表3659至3695 式II.35之化合物,其中化合物之Het、尺丨、r2、Rw 之組合在各情況下對應於表A之一列且尺63係如在表24〇 i至 2437之任一者中所定義 表3696至3732 式Π·36之化合物,其中化合物之Het、Ri、R2、R3及R4 [S] 149026.doc 201103429 之組合在各情況下對應於表A之一列且尺“係如在表2401至 2437之任一者中所定義 表 3733 至 3769 式II.37之化合物,其中化合物之fjet、r1、、尺3及r4 之組合在各情況下對應於表A之一列且1163係如在表2401至 2437之任一者中所定義 表 3770至 3806 式ΙΙ·38之化合物,其中化合物之Het、Ri、r2、r3&r4 之組合在各情況下對應於表A之一列且R6a係如在表24〇i至 2437之任一者中所定義 表3807至3843 式Π.39之化合物,其中化合物之Het、Ri、R2、R3及R4 之..且&在各隋况下對應於表A之一列且R6a係如在表Μ。1至 2437之任一者中所定義 表3844至3880 式11.40之化合物’其中化合物之Het、Rl、R2、仗3及汉4 之組合在各情況下對應於表A之一列且Rfia係如在表MW至 2437之任一者中所定義 表3881至3917 式11.41之化合物,其中化合物之Het、R丨、r2、&3及凡4 之組合在各情況下對應於表A之一列且尺63係如在表24〇1至 2437之任一者中所定義 表3918至3954 式11.42之化合物,其中化合物之Het、Rl、r2、r3及r4 149026.doc •81 - 201103429 之組合在各情況下對應於表A之一列且尺“係如在表2401至 2437之任一者中所定義 表3955至3991 式11.43之化合物,其中化合物之Het、R1、r2、及尺4 之組合在各情況下對應於表A之一列且尺“係如在表2401至 2437之任一者中所定義 表3992至4028 式Π.44之化合物’其中化合物之Het、R1、r2、尺3及R4 之組合在各情況下對應於表A之一列且係如在表24〇 1至 2437之任一者中所定義 表4029至4065 式Π·45之化合物,其中化合物之Het、R丨、R2、R3&R4 之組合在各情況下對應於表A之一列且R6a係如在表24〇ι至 2437之任一者中所定義 表 4066至 4102 式Π·46之化合物,其中化合物之Het、R1、R2、R3&R4 之組合在各情況下對應於表A之一列且1163係如在表24〇1至 2437之任一者中所定義 表4103至4139 式Π·47之化合物,其中化合物之Het、R1、R2、Rw 之組合在各情況下對應於表A之一列且R6a係如在表24〇1至 2437之任一者中所定義 表4140至4176 式Π.48之化合物,其中化合物之Het、R1、R2、r3&r4 149026.doc [S] ·82· 201103429 之組合在各情況下對應於表A之一列且R6a係如在表2401至 2437之任一者中所定義[SI-74 · 201103429 Table 2436 Compounds of the formula 11] wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6a is a phenoxysulfonyl group. The compound of Π. 1, wherein the combination of Het, r1, r2, r3 and r4 of the compound corresponds in each case to one of the columns of Table A and R& is cn. Table 2438 to 2474 The compound of the formula II.2 'where the compound of the fjet The combination of R1, R2, 3 and R4 corresponds in each case to one of the columns of Table A and R& is a compound of the formula 2475 to 2511 of the formula Π.3 as defined in any of Tables 24〇1 to 2437. Wherein the combination of Het, R1, R2, Ruler 3 and Ruler 4 of the compound corresponds in each case to one of the columns of Table A and R is as defined in Tables 2512 to 2548 as defined in any of Tables 24 to 1437. A compound of the formula 44, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and R6a is as defined in any of Tables 24 to 1437. 2549 to 2585 A compound of the formula II.5 wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and the R& Tables 2586 to 2622, which are defined in any of Tables 2 to 2437, are compounds of the formula ,6, wherein the compound Het, R1, R2, Rw 149026.doc • 75-201103429 combination corresponds in each case to the table The column of A and the ruler 63 are the compounds of the formulas 2623 to 2659 of the formula ΙΙ7 as defined in any one of Tables 24〇1 to 2437, wherein the combination of Het, R丨, R2, R3 and R4 of the compound is In each case, corresponding to Table A, the column is "as shown in any of Tables 240A to 2437, and the compounds of Tables 2660 to 2696, 8 are compounds of Het, R丨, r2, R3 of the compound. And the combination of R4 in each case corresponds to one of the columns of Table A and the ruler "is a compound of the formula 2697 to 2733 of the formula Π·9 as defined in any of Tables 24〇1 to 2437, wherein the compound Het, R1 The combination of r2, R3 and R4 corresponds in each case to one of the columns of Table A and R is as defined in Tables 2734 to 2770, formula 1110, as defined in Tables 24〇1 to 2437, wherein the compound Het The combination of R1, R2, 尺3 and R4 corresponds in each case to the column of Table A and R is as defined in Tables 24〇1 to 2437. Tables 2771 to 2807 'R1, R2, R3 and R4 63 are as shown in Table 2401 to Formula 11, 11 in which the compound 'Het, the combination of which corresponds to each of Table A and Han 2437 in each case Tables 2808 to 2844 of the formula 11.12, wherein the combination of compound 1^, ruler 1, ruler 2, & 3 and ruler [.S] 149026.doc • 76- 201103429 corresponds in each case to Table A And a combination of Het 'R1, r2, r3 & r4 of the compound, in each case, as defined in any of Tables 24 to 1 and 2437. Corresponding to one of the columns of Table A and R6a is a compound of the formulas 2882 to 2918 of the formula 11.14 as defined in any one of Tables 24 to 1437, wherein the compounds are 11^, 11丨, 112, Han 3 and Han 4 Combining the compounds of Tables 2919 to 2955, Π.15, as defined in any of Tables 24〇1 to 2437, in each case, wherein fjet, Ri, r2, ruler 3 of the compound The combination of the ruler 4 corresponds in each case to one of the columns of Table A and the ruler 63 is as defined in any of Tables 2401 to 2437, Tables 2956 to 29 92. The compound of formula 11.16 wherein the combination of compound ^^, 111, 1^2, 尺3 and 尺4 corresponds in each case to one of Table A and is as in any of Tables 24A to 2437. Tables 2993 to 3029 are defined as compounds of formula 11.17, wherein the combination of 1^'111, 1^, 113 and 1^4 of the compound corresponds in each case to one of the columns of Table A and the ruler 63 is as shown in Table 24〇 Tables 3030 to 3066, defined in any one of 2437, are compounds of formula II.18, wherein the combination of Het, R1, r2, r3 and r4 149026.doc-77-201103429 of the compound corresponds in each case to Table A. The combination of tables 3067 to 3103 as defined in any of Tables 240 1 to 2437 in each case corresponds to the array of Table A and R6a is as in any of Tables 240 1 to 2437. The compounds of the formula IL20 are defined in Tables 3104 to 3140, wherein the combination of Het, R1, R2, Ruler 3 and R4 of the compound corresponds in each case to the list of Table A and the ruler is as in Tables 2401 to 2437. Tables 3141 to 3177 of the formula II.21, wherein the combination of Het, R丨, R2, R3 and R4 of the compound corresponds in each case to Table A. • Column 63 is a compound of the formula II.22 as defined in any of Tables 2401 to 2, 37, wherein the combination of Het, R1, r2, r3 and r4 of the compound is in each case Corresponding to one of the columns of Table A and R6a is a compound of the formulae 3215 to 3251, formula 11.23 as defined in any one of Tables 24 to 1437, wherein the combination of the compound 1^, the ruler 1, the ruler 2, the 113 and the 114 In each case, corresponding to one of Tables 8 and as defined in any of Tables 24〇1 to 2437, compounds of formulas 3252 to 3288, formula 11.24, wherein compounds iHet, Ri, R2, R3 and R4 ί 149026. The combination of doc •78-201103429 corresponds in each case to one of the columns of Table A and R6a is a compound of the formula 28925, as defined in any of Tables 24A to 2437, wherein the compound Het The combination of R1, R2, r3 & r4 corresponds in each case to one of the columns of Table A and R6a is a compound of the formula 32626 of Tables 3326 to 3362, as defined in any of Tables 24 to 2437, wherein The combination of Het, R, R2, Ruler 3 and R4 of the compound corresponds in each case to one of the columns of Table A and 1163 is as shown in Table 24〇1 Any of the compounds of formulas 3363 to 3399, Π.27, as defined in any one of 2,437, wherein the combination of Het, R1, R2, R3 and R4 of the compound corresponds in each case to one of Table A and Rea is as in Table MW a compound of the formula II.28, as defined in any one of 2437 to 3,436, wherein the combination of the compound, R1, R2, R3 and r4 corresponds in each case to one of the columns of Table A and the R& Tables 3437 to 3473 are compounds of the formula 29.29 as defined in any one of Tables 24 to 3, wherein the combination of Het, R1, R2, r3 and μ of the compound corresponds in each case to the expression - And R "is a compound of the formula 3474 to 3510 of the formula Π·30 as defined in any of Tables 24 to 1437, wherein the compounds are Het, R1, R2, ... and ana 4 149026.doc -79- The combination of 201103429 corresponds in each case to one of the tables A and the ruler 6& is as defined in Tables 2401 to 2437, as defined in Tables 3511 to 3547, the compound of the formula II.3.1, wherein the compound j|et, The combination of R1, r2, r3 and r4 corresponds in each case to one of the columns of Table A and R6a is as defined in Tables 24A to 2437, as defined in Tables 3548 to 3584. A compound of the formula 11.32, wherein the combination of Het, R1, r2, r3 and r4 of the compound corresponds in each case to one of the columns of Table A and R6a is as defined in Table 3585 as defined in any of Tables 24 to 1437. 3621 A compound of the formula 33 wherein the combination of Het, R1, r2, R3 and R4 of the compound corresponds in each case to one of the columns of Table A and Rea is as defined in any of Tables 24 to 2437. Tables 3622 to 3658 Compounds of the formula 34.34 wherein the combination of Het, Ri, R2, ampule 3 and R4 of the compound corresponds in each case to one of the columns of Table A and Rea is as in any of Tables 24 to 1437. The compounds of the formula II.35 are defined in Tables 3659 to 3695, wherein the combination of Het, size, r2, and Rw of the compound corresponds in each case to one of the columns of Table A and the ruler 63 is as shown in Tables 24i to 2437. Any of the compounds of Tables 3696 to 3732, wherein 组合36, wherein the combination of compounds Het, Ri, R2, R3, and R4 [S] 149026.doc 201103429 corresponds in each case to one of Table A and The ruler "is a compound of the formulas 3733 to 3769 of the formula II.37 as defined in any of the forms 2401 to 2437, wherein the compound is fjet, r 1. The combination of ruler 3 and r4 corresponds in each case to one of the columns of Table A and 1163 is a compound of the formula 3770 to 3806 of the formula ΙΙ·38 as defined in any of Tables 2401 to 2437, wherein the compound Het The combination of Ri, r2, r3 & r4 corresponds in each case to one of the columns of Table A and R6a is a compound of the formula 3807 to 3843 of the formula Π.39 as defined in any of Tables 24i to 2437, wherein The compounds Het, Ri, R2, R3 and R4 of .. and & in each case correspond to one of the columns of Table A and R6a is as shown in Table Μ. The compounds of Tables 1844 to 3880, Formula 11.40, as defined in any of 1 to 2437, wherein the combination of Het, R1, R2, 仗3 and Han 4 of the compound corresponds in each case to one of Table A and Rfia is as in The compounds of the formulae 3881 to 3917, formula 11.41, as defined in any of Tables MW to 2437, wherein the combination of Het, R丨, r2, & 3 and 4 of the compounds corresponds in each case to one of the tables A and 63 is a compound of the formulae 3918 to 3954, formula 11.42, as defined in any one of Tables 24 to 1437, wherein a combination of Het, R1, r2, r3 and r4 149026.doc • 81 - 201103429 of the compound is in each case. The following corresponds to a column of Table A and the ruler "is a compound of the formulas 3955 to 3991, formula 11.43 as defined in any of Tables 2401 to 2437, wherein the combination of Het, R1, r2, and Rule 4 of the compound is in each case. The following corresponds to a column of Table A and the ruler "is a compound of the formula 399. In each case corresponds to one of the columns of Table A and is as defined in any of Tables 24〇1 to 2437, Table 4029 4065 A compound of the formula 45, wherein the combination of Het, R丨, R2, R3 & R4 of the compound corresponds in each case to one of the columns of Table A and R6a is as in any of Tables 24 to 2437. Tables 4066 to 4102 are compounds of the formula 46 wherein the combination of compounds Het, R1, R2, R3 & R4 corresponds in each case to one of the columns of Table A and 1163 is as in any of Tables 24 to 1437. Tables 4103 to 4139 are defined as compounds of formula 47, wherein the combination of Het, R1, R2, Rw of the compound corresponds in each case to one of the columns of Table A and R6a is as shown in Tables 24 to 1437. The compounds of the formula 140.48 defined in Table 4140 to 4176, wherein the combination of the compounds Het, R1, R2, r3 & r4 149026.doc [S] 82] 201103429 corresponds in each case to one of the tables A And R6a is as defined in any of Tables 2401 to 2437

表A 編號 R1 R" RJ R4 Het A-1 Η H H H Het.l A-2 F H H H Het.l A-3 Cl H H H Het.l A-4 Br H H H Het.l A-5 ch3 H H H Het.l A-6 chf2 H H H Het.l A-7 cf3 H H H Het.l A-8 och3 H H H Het.l A-9 ochf2 H H H Het.l A-10 OCF3 H H H Het.l A-11 H F H H Het.l A-12 H Cl H H Het.l A-13 H Br H H Het.l A-14 H ch3 H H Het.l A-15 H chf2 H H Het.l A-16 H cf3 H H Het.l A-17 H OCH3 H H Het.l A-18 H OCHF2 H H Het.l A-19 H OCF3 H H Het.l A-20 F F H H Het.l A-21 F H F H Het.l A-22 F H H F Het.l A-23 H F H F Het.l A-24 Cl H H F Het.l A-25 H H H H Het.2 A-26 F H H H Het.2 A-27 Cl H H H Het.2 A-28 Br H H H Het.2 A-29 ch3 H H H Het.2 A-30 chf2 H H H Het.2 A-31 cf3 H H H Het.2 A-32 OCH3 H H H Het.2 A-33 OCHF2 H H H Het.2 A-34 〇CF3 H H H Het.2 A-35 H F H H Het.2 A-36 H Cl H H Het.2 A-37 H Br H H Het.2 A-38 H ch3 H H Het.2 A-39 H chf2 H H Het.2 A-40 H cf3 H H Het.2 A-41 H OCH3 H H Het.2 A-42 H OCHF2 H H Het.2 149026.doc -83- 201103429 編號 R1 R3 R4 Het A-43 H OCF3 H H Het.2 A-44 F F H H Het.2 A-45 F H F H Het.2 A-46 F H H F Het.2 A-47 H F H F Het.2 A-48 Cl H H F Het.2 A-49 H H H H Het.3 A-50 F H H H Het.3 A-51 Cl H H H Het.3 A-52 Br H H H Het.3 A-53 ch3 H H H Het.3 A-54 chf2 H H H Het.3 A-55 cf3 H H H Het.3 A-56 OCH3 H H H Het.3 A-57 OCHF2 H H H Het.3 A-58 〇CF3 H H H Het.3 A-59 H F H H Het.3 A-60 H Cl H H Het.3 A-61 H Br H H Het.3 A-62 H ch3 H H Het.3 A-63 H chf2 H H Het.3 A-64 H cf3 H H Het.3 A-65 H OCH3 H H Het.3 A-66 H OCHF2 H H Het.3 A-67 H OCF3 H H Het.3 A-68 F F H H Het.3 A-69 F H F H Het.3 A-70 F H H F Het.3 A-71 H F H F Het.3 A-72 Cl H H F Het.3 A-73 H H H H Het.4 A-74 F H H H Het.4 A-75 Cl H H H Het.4 A-76 Br H H H Het.4 A-77 ch3 H H H Het.4 A-78 chf2 H H H Het.4 A-79 cf3 H H H Het.4 A-80 OCH3 H H H Het.4 A-81 OCHF2 H H H Het.4 A-82 OCF3 H H H Het.4 A-83 H F H H Het.4 A-84 H Cl H H Het.4 A-85 H Br H H Het.4 A-86 H ch3 H H Het.4 A-87 H chf2 H H Het.4 A-88 H cf3 H H Het.4 A-89 H OCH3 H H Het.4 A-90 H OCHF2 H H Het.4Table A No. R1 R" RJ R4 Het A-1 Η HHH Het.l A-2 FHHH Het.l A-3 Cl HHH Het.l A-4 Br HHH Het.l A-5 ch3 HHH Het.l A- 6 chf2 HHH Het.l A-7 cf3 HHH Het.l A-8 och3 HHH Het.l A-9 ochf2 HHH Het.l A-10 OCF3 HHH Het.l A-11 HFHH Het.l A-12 H Cl HH Het.l A-13 H Br HH Het.l A-14 H ch3 HH Het.l A-15 H chf2 HH Het.l A-16 H cf3 HH Het.l A-17 H OCH3 HH Het.l A -18 H OCHF2 HH Het.l A-19 H OCF3 HH Het.l A-20 FFHH Het.l A-21 FHFH Het.l A-22 FHHF Het.l A-23 HFHF Het.l A-24 Cl HHF Het.l A-25 HHHH Het.2 A-26 FHHH Het.2 A-27 Cl HHH Het.2 A-28 Br HHH Het.2 A-29 ch3 HHH Het.2 A-30 chf2 HHH Het.2 A -31 cf3 HHH Het.2 A-32 OCH3 HHH Het.2 A-33 OCHF2 HHH Het.2 A-34 〇CF3 HHH Het.2 A-35 HFHH Het.2 A-36 H Cl HH Het.2 A- 37 H Br HH Het.2 A-38 H ch3 HH Het.2 A-39 H chf2 HH Het.2 A-40 H cf3 HH Het.2 A-41 H OCH3 HH Het.2 A-42 H OCHF2 HH Het .2 149026.doc -83- 201103429 No. R1 R3 R4 Het A-43 H OCF3 HH Het.2 A-44 FFHH Het.2 A-45 FHFH Het.2 A-46 FHHF Het.2 A-47 HFHF Het.2 A-48 Cl HHF Het.2 A-49 HHHH Het.3 A-50 FHHH Het.3 A-51 Cl HHH Het.3 A-52 Br HHH Het.3 A-53 ch3 HHH Het.3 A-54 chf2 HHH Het.3 A-55 cf3 HHH Het.3 A-56 OCH3 HHH Het .3 A-57 OCHF2 HHH Het.3 A-58 〇CF3 HHH Het.3 A-59 HFHH Het.3 A-60 H Cl HH Het.3 A-61 H Br HH Het.3 A-62 H ch3 HH Het.3 A-63 H chf2 HH Het.3 A-64 H cf3 HH Het.3 A-65 H OCH3 HH Het.3 A-66 H OCHF2 HH Het.3 A-67 H OCF3 HH Het.3 A- 68 FFHH Het.3 A-69 FHFH Het.3 A-70 FHHF Het.3 A-71 HFHF Het.3 A-72 Cl HHF Het.3 A-73 HHHH Het.4 A-74 FHHH Het.4 A- 75 Cl HHH Het.4 A-76 Br HHH Het.4 A-77 ch3 HHH Het.4 A-78 chf2 HHH Het.4 A-79 cf3 HHH Het.4 A-80 OCH3 HHH Het.4 A-81 OCHF2 HHH Het.4 A-82 OCF3 HHH Het.4 A-83 HFHH Het.4 A-84 H Cl HH Het.4 A-85 H Br HH Het.4 A-86 H ch3 HH Het.4 A-87 H Chf2 HH Het.4 A-88 H cf3 HH Het.4 A-89 H OCH3 HH He T.4 A-90 H OCHF2 H H Het.4

[SI 149026.doc -84- 201103429 編號 R* RJ R4 Het A-91 H ocf3 H H Het.4 A-92 F F H H Het.4 A-93 F H F H Het.4 A-94 F H H F Het.4 A-95 H F H F Het.4 A-96 Cl H H F Het.4 A-97 H H H H Het.5 A-98 F H H H Het. 5 A-99 Cl H H H Het.5 A-100 Br H H H Het.5 A-101 ch3 H H H Het.5 A-102 chf2 H H H Het.5 A-103 cf3 H H H Het.5 A-104 och3 H H H Het.5 A-105 ochf2 H H H Het.5 A-106 〇cf3 H H H Het.5 A-107 H F H H Het.5 A-108 H Cl H H Het.5 A-109 H Br H H Het.5 A-110 H ch3 H H Het.5 A-lll H chf2 H H Het.5 A-112 H cf3 H H Het.5 A-113 H och3 H H Het.5 A-114 H ochf2 H H Het.5 A-115 H ocf3 H H Het.5 A-116 F F H H Het.5 A-117 F H F H Het.5 A-118 F H H F Het.5 A-119 H F H F Het.5 A-120 Cl H H F. Het.5 A-121 H H H H Het.6 A-122 F H H H Het.6 A-123 Cl H H H Het.6 A-124 Br H H H Het.6 A-125 ch3 H H H Het.6 A-126 chf2 H H H Het.6 A-127 cf3 H H H Het.6 A-128 och3 H H H Het.6 A-129 ochf2 H H H Het.6 A-130 ocf3 H H H Het.6 A-131 H F H H Het.6 A-132 H Cl H H Het.6 A-133 H Br H H Het.6 A-134 H ch3 H H Het.6 A-135 H chf2 H H Het.6 A-136 H cf3 H H Het.6 A-137 H och3 H H Het.6 A-138 H ochf2 H H Het.6 149026.doc -85- 201103429 編號 R1 R2 RJ R4 Het A-139 H ocf3 H H Het.6 A-140 F F H H Het.6 A-141 F H F H Het.6 A-142 F H H F Het.6 A-143 H F H F Het.6 A-144 Cl H H F Het.6 A-145 H H H H Het.7 A-146 F H H H Het.7 A-147 Cl H H H Het.7 A-148 Br H H H Het.7 A-149 ch3 H H H Het.7 A-150 chf2 H H H Het.7 A-151 cf3 H H H Het.7 A-152 och3 H H H Het.7 A-153 ochf2 H H H Het.7 A-154 ocf3 H H H Het.7 A-155 H F H H Het.7 A-156 H Cl H H Het.7 A-157 H Br H H Het.7 A-158 H ch3 H H Het.7 A-159 H chf2 H H Het.7 A-160 H cf3 H H Het.7 A-161 H och3 H H Het.7 A-162 H ochf2 H H Het.7 A-163 H ocf3 H H Het.7 A-164 F F H H Het.7 A-165 F H F H Het.7 A-166 F H H F Het.7 A-167 H F H F Het.7 A-168 Cl H H F Het.7 A-169 H H H H Het.8 A-170 F H H H Het.8 A-171 Cl H H H Het.8 A-172 Br H H H Het.8 A-173 ch3 H H H Het.8 A-174 chf2 H H H Het.8 A-175 cf3 H H H Het.8 A-176 och3 H H H Het.8 A-177 ochf2 H H H Het.8 A-178 ocf3 H H H Het.8 A-179 H F H H Het.8 A-180 H Cl H H Het.8 A-181 H Br H H Het.8 A-182 H ch3 H H Het.8 A-183 H chf2 H H Het.8 A-184 H cf3 H H Het.8 A-185 H och3 H H Het.8 A-186 H ochf2 H H Het.8 m 149026.doc -86- 201103429 編號 R1 R2 R3 R4 Het A-187 H ocf3 H H Het.8 A-188 F F H H Het. 8 A-189 F H F H Het.8 A-190 F H H F Het.8 A-191 H F H F Het.8 A-192 Cl H H F Het.8 A-193 H H H H Het.9 A-194 F H H H Het.9 A-195 Cl H H H Het.9 A-196 Br H H H Het.9 A-197 ch3 H H H Het.9 A-198 chf2 H H H Het.9 A-199 cf3 H H H Het.9 A-200 och3 H H H Het.9 A-201 ochf2 H H H Het.9 A-202 ocf3 H H H Het.9 A-203 H F H H Het.9 A-204 H Cl H H Het.9 A-205 H Br H H Het.9 A-206 H ch3 H H Het.9 A-207 H chf2 H H Het.9 A-208 H cf3 H H Het.9 A-209 H och3 H H Het.9 A-210 H ochf2 H H Het.9 A-211 H ocf3 H H Het.9 A-212 F F H H Het.9 A-213 F H F H Het.9 A-214 F H H F Het.9 A-215 H F H F Het.9 A-216 Cl H H F Het.9 A-217 H H H H Het. 10 A-218 F H H H Het. 10 A-219 Cl H H H Het. 10 A-220 Br H H H Het. 10 A-221 ch3 H H H Het. 10 A-222 chf2 H H H Het. 10 A-223 cf3 H H H Het. 10 A-224 och3 H H H Het. 10 A-225 ochf2 H H H Het. 10 A-226 ocf3 H H H Het. 10 A-227 H F H H Het. 10 A-228 H Cl H H Het. 10 A-229 H Br H H Het. 10 A-230 H ch3 H H Het. 10 A-231 H chf2 H H Het. 10 A-232 H cf3 H H Het. 10 A-233 H och3 H H Het. 10 A-234 H ochf2 H H Het. 10 149026.doc -87- 201103429 編號 R丨 RJ R4 Het A-235 H OCF3 H H Het.10 A-236 F F H H Het. 10 A-237 F H F H Het.10 A-238 F H H F Het.10 A-239 H F H F Het.10 A-240 Cl H H F Het.10 A-241 H H H H Het. 11 A-242 F H H H Het. 11 A-243 Cl H H H Het. 11 A-244 Br H H H Het. 11 A-245 ch3 H H H Het. 11 A-246 chf2 H H H Het. 11 A-247 cf3 H H H Het. 11 A-248 OCH3 H H H Het. 11 A-249 OCHF2 H H H Het. 11 A-250 OCF3 H H H Het. 11 A-251 H F H H Het. 11 A-252 H Cl H H Het. 11 A-253 H Br H H Het. 11 A-254 H ch3 H H Het. 11 A-255 H chf2 H H Het. 11 A-256 H cf3 H H Het. 11 A-257 H OCH3 H H Het. 11 A-258 H OCHF2 H H Het. 11 A-259 H OCF3 H H Het. 11 A-260 F F H H Het. 11 A-261 F H F H Het. 11 A-262 F H H F Het. 11 A-263 H F H F Het. 11 A-264 Cl H H F Het. 11 A-265 H H H H Het. 12 A-266 F H H H Het. 12 A-267 Cl H H H Het. 12 A-268 Br H H H Het. 12 A-269 ch3 H H H Het. 12 A-270 chf2 H H H Het. 12 A-271 cf3 H H H Het. 12 A-272 OCH3 H H H Het. 12 A-273 OCHF2 H H H Het. 12 A-274 OCF3 H H H Het. 12 A-275 H F H H Het. 12 A-276 H Cl H H Het. 12 A-277 H Br H H Het. 12 A-278 H ch3 H H Het. 12 A-279 H chf2 H H Het. 12 A-280 H cf3 H H Het. 12 A-281 H OCH3 H H Het. 12 A-282 H OCHF2 H H Het. 12 [s] 149026.doc -88- 201103429 編號 R1 R2 RJ r Het A-283 H OCF3 H H Het.12 A-284 F F H H Het. 12 A-285 F H F H Het.12 A-286 F H H F Het.12 A-287 H F H F Het.12 A-288 Cl H H F Het.12 A-289 H H H H Het. 13 A-290 F H H H Het. 13 A-291 Cl H H H Het. 13 A-292 Br H H H Het. 13 A-293 ch3 H H H Het. 13 A-294 chf2 H H H Het. 13 A-295 cf3 H H H Het. 13 A-296 OCH3 H H H Het. 13 A-297 OCHF2 H H H Het. 13 A-298 OCF3 H H H Het. 13 A-299 H F H H Het. 13 A-300 H Cl H H Het. 13 A-301 H Br H H Het. 13 A-302 H ch3 H H Het. 13 A-303 H chf2 H H Het. 13 A-304 H cf3 H H Het. 13 A-305 H OCH3 H H Het. 13 A-306 H OCHF2 H H Het. 13 A-307 H OCF3 H H Het. 13 A-308 F F H H Het. 13 A-309 F H F H Het. 13 A-310 F H H F Het. 13 A-311 H F H F Het. 13 A-312 Cl H H F Het. 13 A-313 H H H H Het. 14 A-314 F H H H Het. 14 A-315 Cl H H H Het. 14 A-316 Br H H H Het. 14 A-317 ch3 H H H Het. 14 A-318 chf2 H H H Het. 14 A-319 cf3 H H H Het. 14 A-320 OCH3 H H H Het. 14 A-321 OCHF2 H H H Het. 14 A-322 OCF3 H H H Het. 14 A-323 H F H H Het. 14 A-324 H Cl H H Het. 14 A-325 H Br H H Het.14 A-326 H ch3 H H Het. 14 A-327 H chf2 H H Het.14 A-328 H cf3 H H Het.14 A-329 H OCH3 H H Het.14 A-330 H ochf2 H H Het.14 149026.doc -89- 201103429 編號 R1 R/ R3 r Het A-331 H OCF3 H H Het.14 A-332 F F H H Het. 14 A-333 F H F H Het.14 A-334 F H H F Het.14 A-335 H F H F Het.14 A-336 Cl H H F Het.14 A-337 H H H H Het. 15 A-338 F H H H Het. 15 A-339 Cl H H H Het. 15 A-340 Br H H H Het. 15 A-341 ch3 H H H Het. 15 A-342 chf2 H H H Het. 15 A-343 cf3 H H H Het. 15 A-344 OCH3 H H H Het. 15 A-345 OCHF2 H H H Het. 15 A-346 OCF3 H H H Het. 15 A-347 H F H H Het. 15 A-348 H Cl H H Het. 15 A-349 H Br H H Het. 15 A-350 H ch3 H H Het. 15 A-351 H chf2 H H Het. 15 A-352 H cf3 H H Het. 15 A-353 H OCH3 H H Het. 15 A-354 H OCHF2 H H Het. 15 A-355 H OCF3 H H Het. 15 A-356 F F H H Het. 15 A-357 F H F H Het. 15 A-358 F H H F Het. 15 A-359 H F H F Het. 15 A-360 Cl H H F Het. 15 A-361 H H H H Het. 16 A-362 F H H H Het. 16 A-363 Cl H H H Het. 16 A-364 Br H H H Het.16 A-365 ch3 H H H Het. 16 A-366 chf2 H H H Het.16 A-367 cf3 H H H Het.16 A-368 OCH3 H H H Het.16 A-369 OCHF2 H H H Het.16 A-370 OCF3 H H H Het.16 A-371 H F H H Het.16 A-372 H Cl H H Het.16 A-373 H Br H H Het.16 A-374 H ch3 H H Het.16 A-375 H chf2 H H Het.16 A-376 H cf3 H H Het.16 A-377 H OCH3 H H Het.16 A-378 H OCHF2 H H Het.16 [si 149026.doc -90- 201103429 編號 R1 Rj R4 Het A-379 H OCF3 H H Het.16 A-380 F F H H Het. 16 A-381 F H F H Het.16 A-382 F H H F Het.16 A-383 H F H F Het.16 A-384 Cl H H F Het.16 A-385 H H H H Het. 17 A-386 F H H H Het. 17 A-387 Cl H H H Het. 17 A-388 Br H H H Het. 17 A-389 ch3 H H H Het. 17 A-390 chf2 H H H Het. 17 A-391 cf3 H H H Het. 17 A-392 OCH3 H H H Het. 17 A-393 OCHF2 H H H Het. 17 A-394 OCF3 H H H Het. 17 A-395 H F H H Het. 17 A-396 H Cl H H Het. 17 A-397 H Br H H Het. 17 A-398 H ch3 H H Het. 17 A-399 H chf2 H H Het. 17 A-400 H cf3 H H Het. 17 A-401 H OCH3 H H Het. 17 A-402 H OCHF2 H H Het. 17 A-403 H OCF3 H H Het. 17 A-404 F F H H Het. 17 A-405 F H F H Het. 17 A-406 F H H F Het. 17 A-407 H F H F Het. 17 A-408 Cl H H F Het. 17 A-409 H H H H Het. 18 A-410 F H H H Het. 18 A-411 Cl H H H Het. 18 A-412 Br H H H Het. 18 A-413 ch3 H H H Het. 18 A-414 chf2 H H H Het. 18 A-415 cf3 H H H Het. 18 A-416 OCH3 H H H Het. 18 A-417 OCHF2 H H H Het. 18 A-418 OCF3 H H H Het. 18 A-419 H F H H Het. 18 A-420 H Cl H H Het. 18 A-421 H Br H H Het. 18 A-422 H ch3 H H Het. 18 A-423 H chf2 H H Het. 18 A-424 H cf3 H H Het. 18 A-425 H OCH3 H H Het. 18 A-426 H OCHF2 H H Het. 18 149026.doc -91 - 201103429 編號 R1 RJ r Het A-427 H OCF3 H H Het.18 A-428 F F H H Het. 18 A-429 F H F H Het.18 A-430 F H H F Het.18 A-431 H F H F Het.18 A-432 Cl H H F Het.18 A-433 H H H H Het. 19 A-434 F H H H Het. 19 A-435 Cl H H H Het. 19 A-436 Br H H H Het. 19 A-437 ch3 H H H Het. 19 A-438 chf2 H H H Het. 19 A-439 cf3 H H H Het. 19 A-440 OCH3 H H H Het. 19 A-441 OCHF2 H H H Het. 19 A-442 OCF3 H H H Het. 19 A-443 H F H H Het. 19 A-444 H Cl H H Het. 19 A-445 H Br H H Het. 19 A-446 H ch3 H H Het. 19 A-447 H chf2 H H Het. 19 A-448 H cf3 H H Het. 19 A-449 H OCH3 H H Het. 19 A-450 H OCHF2 H H Het. 19 A-451 H OCF3 H H Het. 19 A-452 F F H H Het. 19 A-453 F H F H Het. 19 A-454 F H H F Het. 19 A-455 H F H F Het. 19 A-456 Cl H H F Het. 19 A-457 H H H H Het.20 A-458 F H H H Het.20 A-459 Cl H H H Het.20 A-460 Br H H H Het.20 A-461 ch3 H H H Het.20 A-462 chf2 H H H Het.20 A-463 cf3 H H H Het.20 A-464 OCH3 H H H Het.20 A-465 OCHF2 H H H Het.20 A-466 OCF3 H H H Het.20 A-467 H F H H Het.20 A-468 H Cl H H Het.20 A-469 H Br H H Het.20 A-470 H ch3 H H Het.20 A-471 H chf2 H H Het.20 A-472 H cf3 H H Het.20 A-473 H OCH3 H H Het.20 A-474 H OCHF2 H H Het.20 m 149026.doc -92- 201103429 編號 R1 R2 RJ R4 Het A-475 H OCF3 H H Het.20 A-476 F F H H Het.20 A-477 F H F H Het.20 A-478 F H H F Het.20 A-479 H F H F Het.20 A-480 Cl H H F Het.20 A-481 H H H H Het.21 A-482 F H H H Het.21 A-483 Cl H H H Het.21 A-484 Br H H H Het.21 A-485 ch3 H H H Het.21 A-486 chf2 H H H Het.21 A-487 cf3 H H H Het.21 A-488 OCH3 H H H Het.21 A-489 OCHF2 H H H Het.21 A-490 OCF3 H H H Het.21 A-491 H F H H Het.21 A-492 H Cl H H Het.21 A-493 H Br H H Het.21 A-494 H ch3 H H Het.21 A-495 H chf2 H H Het.21 A-496 H cf3 H H Het.21 A-497 H OCH3 H H Het.21 A-498 H OCHF2 H H Het.21 A-499 H OCF3 H H Het.21 A-500 F F H H Het.21 A-501 F H F H Het.21 A-502 F H H F Het.21 A-503 H F H F Het.21 A-504 Cl H H F Het.21 A-505 H H H H Het.22 A-506 F H H H Het.22 A-507 Cl H H H Het.22 A-508 Br H H H Het.22 A-509 ch3 H H H Het.22 A-510 chf2 H H H Het.22 A-511 cf3 H H H Het.22 A-512 OCH3 H H H Het.22 A-513 OCHF2 H H H Het.22 A-514 OCF3 H H H Het.22 A-515 H F H H Het.22 A-516 H Cl H H Het.22 A-517 H Br H H Het.22 A-518 H ch3 H H Het.22 A-519 H chf2 H H Het.22 A-520 H cf3 H H Het.22 A-521 H OCH3 H H Het.22 A-522 H OCHF2 H H Het.22 149026.doc -93- 201103429 編號 R1 R2 Rj R4 Het Α-523 Η ocf3 H H Het.22 Α-524 F F H H Het.22 Α-525 F Η F H Het.22 Α-526 F Η H F Het.22 Α-527 Η F H F Het.22 Α-528 C1 Η H F Het.22 Α-529 Η Η H H Het.23 Α-530 F Η H H Het.23 Α-531 C1 Η H H Het.23 Α-532 Br Η H H Het.23 Α-533 ch3 Η H H Het.23 Α-534 chf2 Η H H Het.23 Α-535 cf3 Η H H Het.23 Α-536 OCH3 Η H H Het.23 Α-537 OCHF2 Η H H Het.23 Α-538 OCF3 Η H H Het.23 Α-539 Η F H H Het.23 Α-540 Η C1 H H Het.23 Α-541 Η Br H H Het.23 Α-542 Η ch3 H H Het.23 Α-543 Η chf2 H H Het.23 Α-544 Η cf3 H H Het.23 Α-545 Η OCH3 H H Het.23 Α-546 Η OCHF2 H H Het.23 Α-547 Η OCF3 H H Het.23 Α-548 F F H H Het.23 Α-549 F H F H Het.23 Α-550 F H H F Het.23 Α-551 Η F H F Het.23 Α-552 C1 H H F Het.23 Α-553 Η H H H Het.24 Α-554 F H H H Het.24 Α-555 C1 H H H Het.24 Α-556 Βγ H H H Het.24 Α-557 ch3 H H H Het.24 Α-558 chf2 H H H Het.24 Α-559 cf3 H H H Het.24 Α-560 〇CH3 H H H Het.24 Α-561 OCHF2 H H H Het.24 Α-562 OCF3 H H H Het.24 Α-563 Η F H H Het.24 Α-564 Η Cl H H Het.24 Α-565 Η Br H H Het.24 Α-566 Η ch3 H H Het.24 Α-567 Η chf2 H H Het.24 Α-568 Η cf3 H H Het.24 Α-569 Η 〇CH3 H H Het.24 Α-570 Η OCHF2 H H Het.24 [s] 149026.doc -94· 201103429 編號 R1 R2 R4 Het A-571 H OCF3 H H Het.24 A-572 F F H H Het.24 A-573 F H F H Het.24 A-574 F H H F Het.24 A-575 H F H F Het.24 A-576 Cl H H F Het.24 A-577 H H H H Het.25 A-578 F H H H Het.25 A-579 Cl H H H Het.25 A-580 Br H H H Het.25 A-581 ch3 H H H Het.25 A-582 chf2 H H H Het.25 A-583 cf3 H H H Het.25 A-584 OCH3 H H H Het.25 A-585 OCHF2 H H H Het.25 A-586 OCF3 H H H Het.25 A-587 H F H H Het.25 A-588 H Cl H H Het.25 A-589 H Br H H Het.25 A-590 H ch3 H H Het.25 A-591 H chf2 H H Het.25 A-592 H cf3 H H Het.25 A-593 H OCH3 H H Het.25 A-594 H OCHF2 H H Het.25 A-595 H OCF3 H H Het.25 A-596 F F H H Het.25 A-597 F H F H Het.25 A-598 F H H F Het.25 A-599 H F H F Het.25 A-600 Cl H H F Het.25 A-601 H H H H Het.26 A-602 F H H H Het.26 A-603 Cl H H H Het.26 A-604 Br H H H Het.26 A-605 ch3 H H H Het.26 A-606 chf2 H H H Het.26 A-607 cf3 H H H Het.26 A-608 OCH3 H H H Het.26 A-609 OCHF2 H H H Het.26 A-610 OCF3 H H H Het.26 A-611 H F H H Het.26 A-612 H Cl H H Het.26 A-613 H Br H H Het.26 A-614 H ch3 H H Het.26 A-615 H chf2 H H Het.26 A-616 H cf3 H H Het.26 A-617 H OCH3 H H Het.26 A-618 H OCHF2 H H Het.26 149026.doc -95- 201103429 編號 R丨 Rz RJ R4 Het Α-619 Η OCF3 H H Het.26 Α-620 F F H H Het.26 Α-621 F Η F H Het.26 Α-622 F Η H F Het.26 Α-623 Η F H F Het.26 Α-624 C1 Η H F Het.26 Α-625 Η Η H H Het.27 Α-626 F Η H H Het.27 Α-627 C1 Η H H Het.27 Α-628 Br Η H H Het.27 Α-629 ch3 Η H H Het.27 Α-630 chf2 Η H H Het.27 Α-631 cf3 Η H H Het.27 Α-632 OCH3 Η H H Het.27 Α-633 OCHF2 Η H H Het.27 Α-634 OCF3 Η H H Het.27 Α-635 Η F H H Het.27 Α-636 Η C1 H H Het.27 Α-637 Η Βγ H H Het.27 Α-638 Η ch3 H H Het.27 Α-639 Η chf2 H H Het.27 Α-640 Η cf3 H H Het.27 Α-641 Η OCH3 H H Het.27 Α-642 Η OCHF2 H H Het.27 Α-643 Η OCF3 H H Het.27 Α-644 F F H H Het.27 Α-645 F Η F H Het.27 Α-646 F Η H F Het.27 Α-647 Η F H F Het.27 Α-648 C1 Η H F Het.27 Α-649 Η Η H H Het.28 Α-650 F Η H H Het.28 Α-651 C1 Η H H Het.28 Α-652 Βγ Η H H Het.28 Α-653 ch3 Η H H Het.28 Α-654 chf2 Η H H Het.28 Α-655 cf3 Η H H Het.28 Α-656 OCH3 Η H H Het.28 Α-657 OCHF2 Η H H Het.28 Α-658 OCF3 Η H H Het.28 Α-659 Η F H H Het.28 Α-660 Η C1 H H Het.28 Α-661 Η Br H H Het.28 Α-662 Η ch3 H H Het.28 Α-663 Η chf2 H H Het.28 Α-664 Η cf3 H H Het.28 Α-665 Η OCH3 H H Het.28 Α-666 Η OCHF2 H H Het.28 [si 149026.doc ·96· 201103429 編號 R1 R2 RJ r Het A-667 H OCF3 H H Het.28 A-668 F F H H Het.28 A-669 F H F H Het.28 A-670 F H H F Het.28 A-671 H F H F Het.28 A-672 Cl H H F Het.28 A-673 H H H H Het.29 A-674 F H H H Het.29 A-675 Cl H H H Het.29 A-676 Br H H H Het.29 A-677 ch3 H H H Het.29 A-678 chf2 H H H Het.29 A-679 cf3 H H H Het.29 A-680 OCH3 H H H Het.29 A-681 OCHF2 H H H Het.29 A-682 OCF3 H H H Het.29 A-683 H F H H Het.29 A-684 H Cl H H Het.29 A-685 H Br H H Het.29 A-686 H ch3 H H Het.29 A-687 H chf2 H H Het.29 A-688 H cf3 H H Het.29 A-689 H OCH3 H H Het.29 A-690 H OCHF2 H H Het.29 A-691 H OCF3 H H Het.29 A-692 F F H H Het.29 A-693 F H F H Het.29 A-694 F H H F Het.29 A-695 H F H F Het.29 A-696 Cl H H F Het.29 A-697 H H H H Het.30 A-698 F H H H Het.30 A-699 Cl H H H Het.30 A-700 Br H H H Het.30 A-701 ch3 H H H Het.30 A-702 chf2 H H H Het.30 A-703 cf3 H H H Het.30 A-704 OCH3 H H H Het.30 A-705 OCHF2 H H H Het.30 A-706 OCF3 H H H Het.30 A-707 H F H H Het.30 A-708 H Cl H H Het.30 A-709 H Br H H Het.30 A-710 H ch3 H H Het.30 A-711 H chf2 H H Het.30 A-712 H cf3 H H Het.30 A-713 H OCH3 H H Het.30 A-714 H OCHF2 H H Het.30 149026.doc -97- 201103429 編號 R1 R" RJ R4 Het A-715 H OCF3 H H Het.30 A-716 F F H H Het.30 A-717 F H F H Het.30 A-718 F H H F Het.30 A-719 H F H F Het.30 A-720 Cl H H F Het.30 A-721 H H H H Het.31 A-722 F H H H Het.31 A-723 Cl H H H Het.31 A-724 Br H H H Het.31 A-725 ch3 H H H Het.31 A-726 chf2 H H H Het.31 A-727 cf3 H H H Het.31 A-728 OCH3 H H H Het.31 A-729 OCHF2 H H H Het.31 A-730 OCF3 H H H Het.31 A-731 H F H H Het.31 A-732 H Cl H H Het.31 A-733 H Br H H Het.31 A-734 H ch3 H H Het.31 A-735 H chf2 H H Het.31 A-736 H cf3 H H Het.31 A-737 H OCH3 H H Het.31 A-738 H OCHF2 H H Het.31 A-739 H OCF3 H H Het.31 A-740 F F H H Het.31 A-741 F H F H Het.31 A-742 F H H F Het.31 A-743 H F H F Het.31 A-744 Cl H H F Het.31 A-745 H H H H Het.32 A-746 F H H H Het.32 A-747 Cl H H H Het.32 A-748 Br H H H Het.32 A-749 ch3 H H H Het.32 A-750 chf2 H H H Het.32 A-751 cf3 H H H Het.32 A-752 OCH3 H H H Het.32 A-753 OCHFz H H H Het.32 A-754 OCF3 H H H Het.32 A-755 H F H H Het.32 A-756 H Cl H H Het.32 A-757 H Br H H Het.32 A-758 H ch3 H H Het.32 A-759 H chf2 H H Het.32 A-760 H cf3 H H Het.32 A-761 H OCH3 H H Het.32 A-762 H OCHF2 H H Het.32 [si 149026.doc •98- 201103429 編號 RJ R" RJ R4 Het A-763 H OCF3 H H Het.32 A-764 F F H H Het.32 A-765 F H F H Het.32 A-766 F H H F Het.32 A-767 H F H F Het.32 A-768 Cl H H F Het.32 A-769 H H H H Het.33 A-770 F H H H Het.33 A-771 Cl H H H Het.33 A-772 Br H H H Het.33 A-773 ch3 H H H Het.33 A-774 chf2 H H H Het.33 A-775 cf3 H H H Het.33 A-776 OCH3 H H H Het.33 A-777 OCHF2 H H H Het.33 A-778 OCF3 H H H Het.33 A-779 H F H H Het.33 A-780 H Cl H H Het.33 A-781 H Br H H Het.33 A-782 H ch3 H H Het.33 A-783 H chf2 H H Het.33 A-784 H cf3 H H Het.33 A-785 H OCH3 H H Het.33 A-786 H OCHF2 H H Het.33 A-787 H OCF3 H H Het.33 A-788 F F H H Het.33 A-789 F H F H Het.33 A-790 F H H F Het.33 A-791 H F H F Het.33 A-792 Cl H H F Het.33 A-793 H H H H Het.34 A-794 F H H H Het.34 A-795 Cl H H H Het.34 A-796 Br H H H Het.34 A-797 ch3 H H H Het.34 A-798 chf2 H H H Het.34 A-799 cf3 H H H Het.34 A-800 OCH3 H H H Het.34 A-801 OCHF2 H H H Het.34 A-802 OCF3 H H H Het.34 A-803 H F H H Het.34 A-804 H Cl H H Het.34 A-805 H Br H H Het.34 A-806 H ch3 H H Het.34 A-807 H chf2 H H Het.34 A-808 H cf3 H H Het.34 A-809 H och3 H H Het.34 A-810 H OCHF2 H H Het.34 149026.doc -99- 201103429 編號 R1 Rz RJ r Het A-811 H OCF3 H H Het.34 A-812 F F H H Het.34 A-813 F H F H Het.34 A-814 F H H F Het.34 A-815 H F H F Het.34 A-816 Cl H H F Het.34 A-817 H H H H Het.35 A-818 F H H H Het.35 A-819 Cl H H H Het.35 A-820 Br H H H Het.35, A-821 ch3 H H H Het.35 A-822 chf2 H H H Het.35 A-823 cf3 H H H Het.35 A-824 OCH3 H H H Het.35 A-825 OCHF2 H H H Het.35 A-826 OCF3 H H H Het.35 A-827 H F H H Het.35 A-828 H Cl H H Het.35 A-829 H Br H H Het.35 A-830 H ch3 H H Het.35 A-831 H chf2 H H Het.35 A-832 H cf3 H H Het.35 A-833 H OCH3 H H Het.35 A-834 H OCHF2 H H Het.35 A-835 H OCF3 H H Het.35 A-836 F F H H Het.35 A-837 F H F H Het.35 A-838 F H H F Het.35 A-839 H F H F Het.35 A-840 Cl H H F Het.35 A-841 H H H H Het.36 A-842 F H H H Het.36 A-843 Cl H H H Het.36 A-844 Br H H H Het.36 A-845 ch3 H H H Het.36 A-846 chf2 H H H Het.36 A-847 cf3 H H H Het.36 A-848 OCH3 H H H Het.36 A-849 OCHF2 H H H Het.36 A-850 OCF3 H H H Het.36 A-851 H F H H Het.36 A-852 H Cl H H Het.36 A-853 H Br H H Het.36 A-854 H ch3 H H Het.36 A-855 H chf2 H H Het.36 A-856 H cf3 H H Het.36 A-857 H OCH3 H H Het.36 A-858 H OCHF2 H H Het.36[SI 149026.doc -84- 201103429 No. R* RJ R4 Het A-91 H ocf3 HH Het.4 A-92 FFHH Het.4 A-93 FHFH Het.4 A-94 FHHF Het.4 A-95 HFHF Het .4 A-96 Cl HHF Het.4 A-97 HHHH Het.5 A-98 FHHH Het. 5 A-99 Cl HHH Het.5 A-100 Br HHH Het.5 A-101 ch3 HHH Het.5 A- 102 chf2 HHH Het.5 A-103 cf3 HHH Het.5 A-104 och3 HHH Het.5 A-105 ochf2 HHH Het.5 A-106 〇cf3 HHH Het.5 A-107 HFHH Het.5 A-108 H Cl HH Het.5 A-109 H Br HH Het.5 A-110 H ch3 HH Het.5 A-lll H chf2 HH Het.5 A-112 H cf3 HH Het.5 A-113 H och3 HH Het.5 A-114 H ochf2 HH Het.5 A-115 H ocf3 HH Het.5 A-116 FFHH Het.5 A-117 FHFH Het.5 A-118 FHHF Het.5 A-119 HFHF Het.5 A-120 Cl HH F. Het.5 A-121 HHHH Het.6 A-122 FHHH Het.6 A-123 Cl HHH Het.6 A-124 Br HHH Het.6 A-125 ch3 HHH Het.6 A-126 chf2 HHH Het .6 A-127 cf3 HHH Het.6 A-128 och3 HHH Het.6 A-129 ochf2 HHH Het.6 A-130 ocf3 HHH Het.6 A-131 HFHH Het.6 A-132 H Cl HH Het.6 A-133 H Br HH Het.6 A-134 H ch3 HH Het.6 A-135 H chf2 HH Het.6 A-136 H cf3 HH Het.6 A-137 H och3 HH Het.6 A-138 H ochf2 HH Het.6 149026.doc -85- 201103429 No. R1 R2 RJ R4 Het A-139 H ocf3 HH Het.6 A-140 FFHH Het.6 A-141 FHFH Het.6 A-142 FHHF Het.6 A-143 HFHF Het.6 A-144 Cl HHF Het.6 A-145 HHHH Het.7 A-146 FHHH Het.7 A-147 Cl HHH Het.7 A-148 Br HHH Het.7 A-149 ch3 HHH Het.7 A-150 chf2 HHH Het.7 A-151 cf3 HHH Het.7 A-152 och3 HHH Het.7 A-153 ochf2 HHH Het.7 A-154 ocf3 HHH Het.7 A-155 HFHH Het.7 A-156 H Cl HH Het .7 A-157 H Br HH Het.7 A-158 H ch3 HH Het.7 A-159 H chf2 HH Het.7 A-160 H cf3 HH Het.7 A-161 H och3 HH Het.7 A-162 H ochf2 HH Het.7 A-163 H ocf3 HH Het.7 A-164 FFHH Het.7 A-165 FHFH Het.7 A-166 FHHF Het.7 A-167 HFHF Het.7 A-168 Cl HHF Het. 7 A-169 HHHH Het.8 A-170 FHHH Het.8 A-171 Cl HHH Het.8 A-172 Br HHH Het.8 A-173 ch3 HHH Het.8 A-174 chf2 HHH Het.8 A-175 Cf3 H HH Het.8 A-176 och3 HHH Het.8 A-177 ochf2 HHH Het.8 A-178 ocf3 HHH Het.8 A-179 HFHH Het.8 A-180 H Cl HH Het.8 A-181 H Br HH Het.8 A-182 H ch3 HH Het.8 A-183 H chf2 HH Het.8 A-184 H cf3 HH Het.8 A-185 H och3 HH Het.8 A-186 H ochf2 HH Het.8 m 149026 .doc -86- 201103429 No. R1 R2 R3 R4 Het A-187 H ocf3 HH Het.8 A-188 FFHH Het. 8 A-189 FHFH Het.8 A-190 FHHF Het.8 A-191 HFHF Het.8 A -192 Cl HHF Het.8 A-193 HHHH Het.9 A-194 FHHH Het.9 A-195 Cl HHH Het.9 A-196 Br HHH Het.9 A-197 ch3 HHH Het.9 A-198 chf2 HHH Het.9 A-199 cf3 HHH Het.9 A-200 och3 HHH Het.9 A-201 ochf2 HHH Het.9 A-202 ocf3 HHH Het.9 A-203 HFHH Het.9 A-204 H Cl HH Het. 9 A-205 H Br HH Het.9 A-206 H ch3 HH Het.9 A-207 H chf2 HH Het.9 A-208 H cf3 HH Het.9 A-209 H och3 HH Het.9 A-210 H Ochf2 HH Het.9 A-211 H ocf3 HH Het.9 A-212 FFHH Het.9 A-213 FHFH Het.9 A-214 FHHF Het.9 A-215 HFHF Het.9 A-216 Cl HHF Het.9 A-217 H 10 A-218 FHHH Het. 10 A-219 Cl HHH Het. 10 A-220 Br HHH Het. 10 A-221 ch3 HHH Het. 10 A-222 chf2 HHH Het. 10 A-223 cf3 HHH Het. 10 A-225 ochf2 HHH Het. 10 A-226 ocf3 HHH Het. 10 A-227 HFHH Het. 10 A-228 H Cl HH Het. 10 A-229 H Br HH Het. 10 10 A-232 H cf3 HH Het. 10 A-233 H och3 HH Het. 10 A-234 H ochf2 HH Het. 10 149026.doc -87 - 201103429 No. R丨RJ R4 Het A-235 H OCF3 HH Het.10 A-236 FFHH Het. 10 A-237 FHFH Het.10 A-238 FHHF Het.10 A-239 HFHF Het.10 A-240 Cl HHF Heal.10 A-241 HHHH Het. 11 A-242 FHHH Het. 11 A-243 Cl HHH Het. 11 A-244 Br HHH Het. 11 A-245 ch3 HHH Het. 11 A-246 chf2 HHH Het. 11 A 247 AH3 HeH. Heter. H Br HH Het. 11 A-254 H ch3 HH Het. 11 A-255 H chf2 HH Het. 11 A -16 H cf3 HH Het. 11 A-257 H OCH3 HH Het. 11 A-258 H OCHF2 HH Het. 11 A-259 H OCF3 HH Het. 11 A-260 FFHH Het. 11 A-261 FHFH Het. 11 A -262 FHHF Het. 11 A-263 HFHF Het. 11 A-264 Cl HHF Het. 11 A-265 HHHH Het. 12 A-266 FHHH Het. 12 A-267 Cl HHH Het. 12 A-268 Br HHH Het. 12 A-269 ch3 HHH Het. 12 A-270 chf2 HHH Het. 12 A-271 cf3 HHH Het. 12 A-272 OCH3 HHH Het. 12 A-273 OCHF2 HHH Het. 12 A-274 OCF3 HHH Het. 12 A -275 HFHH Het. 12 A-276 H Cl HH Het. 12 A-277 H Br HH Het. 12 A-278 H ch3 HH Het. 12 A-279 H chf2 HH Het. 12 A-280 H cf3 HH Het. 12 A-281 H OCH3 HH Het. 12 A-282 H OCHF2 HH Het. 12 [s] 149026.doc -88- 201103429 No. R1 R2 RJ r Het A-283 H OCF3 HH Het.12 A-284 FFHH Het. 12 A-285 FHFH Het.12 A-286 FHHF Het.12 A-287 HFHF Het.12 A-288 Cl HHF Het.12 A-289 HHHH Het. 13 A-290 FHHH Het. 13 A-291 Cl HHH Het 13 A-292 Br HHH Het. 13 A-293 ch3 HHH Het. 13 A-294 chf2 HHH Het. 13 A-295 cf3 HHH Het. 13 A-296 OCH3 HHH Het. 13 A-297 OCHF2 HHH Het. 13 A-298 OCF3 HHH Het. 13 A-299 HFHH Het. 13 A-300 H Cl HH Het. 13 A- 301 H Br HH Het. 13 A-302 H ch3 HH Het. 13 A-303 H chf2 HH Het. 13 A-304 H cf3 HH Het. 13 A-305 H OCH3 HH Het. 13 A-306 H OCHF2 HH Het 13 A-307 H OCF3 HH Het. 13 A-308 FFHH Het. 13 A-309 FHFH Het. 13 A-310 FHHF Het. 13 A-311 HFHF Het. 13 A-312 Cl HHF Het. 13 A-313 14 A-314 FHHH Het. 14 A-315 Cl HHH Het. 14 A-316 Br HHH Het. 14 A-317 ch3 HHH Het. 14 A-318 chf2 HHH Het. 14 A-319 cf3 HHH Het. 14 A-320 OCH3 HHH Het. 14 A-321 OCHF2 HHH Het. 14 A-322 OCF3 HHH Het. 14 A-323 HFHH Het. 14 A-324 H Cl HH Het. 14 A-325 H Br HH Het.14 A-326 H ch3 HH Het. 14 A-327 H chf2 HH Het.14 A-328 H cf3 HH Het.14 A-329 H OCH3 HH Het.14 A-330 H ochf2 HH Het.14 149026.doc -89 - 201103429 No. R1 R/ R3 r Het A-331 H OCF3 HH Het.14 A-332 FFHH Het. 14 A-333 FHF H Het.14 A-334 FHHF Het.14 A-335 HFHF Het.14 A-336 Cl HHF Het.14 A-337 HHHH Het. 15 A-338 FHHH Het. 15 A-339 Cl HHH Het. 15 A- 152 Br HHH Het. 15 A-341 ch3 HHH Het. 15 A-342 chf2 HHH Het. 15 A-343 cf3 HHH Het. 15 A-344 OCH3 HHH Het. 15 A-345 OCHF2 HHH Het. 15 A-346 OCF3 15 A-347 H Cl HH Het. 15 A-349 H Br HH Het. 15 A-350 H ch3 HH Het. 15 A-351 H chf2 HH Het. 15 A-352 H cf3 HH Het. 15 A-353 H OCH3 HH Het. 15 A-354 H OCHF2 HH Het. 15 A-355 H OCF3 HH Het. 15 A-356 FFHH Het. 15 A-357 FHFH Het. 15 A-358 15 A-359 HFHF Het. 15 A-360 Cl HHF Het. 15 A-361 HHHH Het. 16 A-362 FHHH Het. 16 A-363 Cl HHH Het. 16 A-364 Br HHH Het.16 A -365 ch3 HHH Het. 16 A-366 chf2 HHH Het.16 A-367 cf3 HHH Het.16 A-368 OCH3 HHH Het.16 A-369 OCHF2 HHH Het.16 A-370 OCF3 HHH Het.16 A-371 HFHH Het.16 A-372 H Cl HH Het.16 A-373 H Br HH Het.16 A-374 H ch3 HH Het.1 6 A-375 H chf2 HH Het.16 A-376 H cf3 HH Het.16 A-377 H OCH3 HH Het.16 A-378 H OCHF2 HH Het.16 [si 149026.doc -90- 201103429 No. R1 Rj R4 Het A-379 H OCF3 HH Het.16 A-380 FFHH Het. 16 A-381 FHFH Het.16 A-382 FHHF Het.16 A-383 HFHF Het.16 A-384 Cl HHF Het.16 A-385 HHHH 17 A-386 FHHH Het. 17 A-387 Cl HHH Het. 17 A-388 Br HHH Het. 17 A-389 ch3 HHH Het. 17 A-390 chf2 HHH Het. 17 A-391 cf3 HHH Het. 17 A-392 OCH3 HHH Het. 17 A-393 OCHF2 HHH Het. 17 A-394 OCF3 HHH Het. 17 A-395 HFHH Het. 17 A-396 H Cl HH Het. 17 A-397 H Br HH Het. 17 A -398 H ch3 HH Het. 17 A-399 H chf2 HH Het. 17 A-400 H cf3 HH Het. 17 A-401 H OCH3 HH Het. 17 A-402 H OCHF2 HH Het. 17 A-403 H OCF3 HH Heter. 17 A-404 FHFH Het. 17 A-406 FHHF Het. 17 A-407 HFHF Het. 17 A-408 Cl HHF Het. 17 A-409 HHHH Het. 18 A-410 FHHH Het. 18 A-411 Cl HHH Het. 18 A-412 Br HHH Het. 18 A-413 ch3 HHH Het. 18 A-414 chf2 HHH Het. 18 A-415 cf3 HHH Het. 18 A-416 OCH3 HHH Het. 18 A-417 OCHF2 HHH Het. 18 A-418 OCF3 HHH Het. 18 A-419 HFHH Het. 18 A-420 18 A-422 H BrH HH Het. 18 A-423 H chf2 HH Het. 18 A-424 H cf3 HH Het. 18 A-425 H OCH3 HH Het. 18 A-426 H OCHF2 HH Het. 18 149026.doc -91 - 201103429 No. R1 RJ r Het A-427 H OCF3 HH Het.18 A-428 FFHH Het. 18 A-429 FHFH Het.18 A-430 FHHF Het .18 A-431 HFHF Het.18 A-432 Cl HHF Het.18 A-433 HHHH Het. 19 A-434 FHHH Het. 19 A-435 Cl HHH Het. 19 A-436 Br HHH Het. 19 A-437 19 A-438 chf2 HHH Het. 19 A-439 cf3 HHH Het. 19 A-440 OCH3 HHH Het. 19 A-441 OCHF2 HHH Het. 19 A-442 OCF3 HHH Het. 19 A-443 HFHH Het 19 A-444 H Cl HH Het. 19 A-445 H Br HH Het. 19 A-446 H ch3 HH Het. 19 A-447 H chf2 HH Het. 19 A-448 H cf3 HH Het. 19 A-449 H OCH3 HH Het. 19 A-450 H OCHF2 HH Het. 19 A-451 H OCF3 HH Het. 19 A-452 FF 19 A-453 FHFH Het. 19 A-454 FHHF Het. 19 A-455 HFHF Het. 19 A-456 Cl HHF Het. 19 A-457 HHHH Het.20 A-458 FHHH Het.20 A-459 Cl HHH Het.20 A-460 Br HHH Het.20 A-461 ch3 HHH Het.20 A-462 chf2 HHH Het.20 A-463 cf3 HHH Het.20 A-464 OCH3 HHH Het.20 A-465 OCHF2 HHH Het.20 A-466 OCF3 HHH Het.20 A-467 HFHH Het.20 A-468 H Cl HH Het.20 A-469 H Br HH Het.20 A-470 H ch3 HH Het.20 A-471 H chf2 HH Het.20 A-472 H cf3 HH Het.20 A-473 H OCH3 HH Het.20 A-474 H OCHF2 HH Het.20 m 149026.doc -92- 201103429 No. R1 R2 RJ R4 Het A-475 H OCF3 HH Het.20 A-476 FFHH Het.20 A-477 FHFH Het.20 A-478 FHHF Het.20 A-479 HFHF Het.20 A-480 Cl HHF Het.20 A-481 HHHH Het.21 A-482 FHHH Het.21 A-483 Cl HHH Het.21 A-484 Br HHH Het.21 A-485 ch3 HHH Het.21 A-486 chf2 HHH Het.21 A-487 cf3 HHH Het.21 A-488 OCH3 HHH Het .21 A-489 OCHF2 HHH Het.21 A-490 OCF3 HHH Het.21 A-491 HFHH Het.21 A-492 H Cl HH Het.21 A-493 H Br HH Het.21 A-494 H ch3 HH Het.21 A-495 H chf2 HH Het.21 A-496 H cf3 HH Het.21 A-497 H OCH3 HH Het.21 A- 498 H OCHF2 HH Het.21 A-499 H OCF3 HH Het.21 A-500 FFHH Het.21 A-501 FHFH Het.21 A-502 FHHF Het.21 A-503 HFHF Het.21 A-504 Cl HHF Het .21 A-505 HHHH Het.22 A-506 FHHH Het.22 A-507 Cl HHH Het.22 A-508 Br HHH Het.22 A-509 ch3 HHH Het.22 A-510 chf2 HHH Het.22 A- 511 cf3 HHH Het.22 A-512 OCH3 HHH Het.22 A-513 OCHF2 HHH Het.22 A-514 OCF3 HHH Het.22 A-515 HFHH Het.22 A-516 H Cl HH Het.22 A-517 H Br HH Het.22 A-518 H ch3 HH Het.22 A-519 H chf2 HH Het.22 A-520 H cf3 HH Het.22 A-521 H OCH3 HH Het.22 A-522 H OCHF2 HH Het.22 149026.doc -93- 201103429 No. R1 R2 Rj R4 Het Α-523 Η ocf3 HH Het.22 Α-524 FFHH Het.22 Α-525 F Η FH Het.22 Α-526 F Η HF Het.22 Α-527 Η FHF Het.22 Α-528 C1 Η HF Het.22 Α-529 Η Η HH Het.23 Α-530 F Η HH Het.23 Α-531 C1 Η HH Het.23 Α-532 B r Η HH Het.23 Α-533 ch3 Η HH Het.23 Α-534 chf2 Η HH Het.23 Α-535 cf3 Η HH Het.23 Α-536 OCH3 Η HH Het.23 Α-537 OCHF2 Η HH Het. 23 Α-538 OCF3 Η HH Het.23 Α-539 Η FHH Het.23 Α-540 Η C1 HH Het.23 Α-541 Η Br HH Het.23 Α-542 Η ch3 HH Het.23 Α-543 Η chf2 HH Het.23 Α-544 Η cf3 HH Het.23 Α-545 Η OCH3 HH Het.23 Α-546 Η OCHF2 HH Het.23 Α-547 Η OCF3 HH Het.23 Α-548 FFHH Het.23 Α-549 FHFH Het.23 Α-550 FHHF Het.23 Α-551 Η FHF Het.23 Α-552 C1 HHF Het.23 Α-553 Η HHH Het.24 Α-554 FHHH Het.24 Α-555 C1 HHH Het.24 Α-556 Βγ HHH Het.24 Α-557 ch3 HHH Het.24 Α-558 chf2 HHH Het.24 Α-559 cf3 HHH Het.24 Α-560 〇CH3 HHH Het.24 Α-561 OCHF2 HHH Het.24 Α -562 OCF3 HHH Het.24 Α-563 Η FHH Het.24 Α-564 Η Cl HH Het.24 Α-565 Η Br HH Het.24 Α-566 Η ch3 HH Het.24 Α-567 Η chf2 HH Het. 24 Α-568 Η cf3 HH Het.24 Α-569 Η 〇CH3 HH Het.24 Α-570 Η OCHF2 HH Het.24 [s] 149 026.doc -94· 201103429 No. R1 R2 R4 Het A-571 H OCF3 HH Het.24 A-572 FFHH Het.24 A-573 FHFH Het.24 A-574 FHHF Het.24 A-575 HFHF Het.24 A -576 Cl HHF Het.24 A-577 HHHH Het.25 A-578 FHHH Het.25 A-579 Cl HHH Het.25 A-580 Br HHH Het.25 A-581 ch3 HHH Het.25 A-582 chf2 HHH Het.25 A-583 cf3 HHH Het.25 A-584 OCH3 HHH Het.25 A-585 OCHF2 HHH Het.25 A-586 OCF3 HHH Het.25 A-587 HFHH Het.25 A-588 H Cl HH Het. 25 A-589 H Br HH Het.25 A-590 H ch3 HH Het.25 A-591 H chf2 HH Het.25 A-592 H cf3 HH Het.25 A-593 H OCH3 HH Het.25 A-594 H OCHF2 HH Het.25 A-595 H OCF3 HH Het.25 A-596 FFHH Het.25 A-597 FHFH Het.25 A-598 FHHF Het.25 A-599 HFHF Het.25 A-600 Cl HHF Het.25 A-601 HHHH Het.26 A-602 FHHH Het.26 A-603 Cl HHH Het.26 A-604 Br HHH Het.26 A-605 ch3 HHH Het.26 A-606 chf2 HHH Het.26 A-607 cf3 HHH Het.26 A-608 OCH3 HHH Het.26 A-609 OCHF2 HHH Het.26 A-610 OCF3 HHH Het.26 A-611 HFH H Het.26 A-612 H Cl HH Het.26 A-613 H Br HH Het.26 A-614 H ch3 HH Het.26 A-615 H chf2 HH Het.26 A-616 H cf3 HH Het.26 A -617 H OCH3 HH Het.26 A-618 H OCHF2 HH Het.26 149026.doc -95- 201103429 No. R丨Rz RJ R4 Het Α-619 Η OCF3 HH Het.26 Α-620 FFHH Het.26 Α-621 F Η FH Het.26 Α-622 F Η HF Het.26 Α-623 Η FHF Het.26 Α-624 C1 Η HF Het.26 Α-625 Η Η HH Het.27 Α-626 F Η HH Het.27 Α-627 C1 Η HH Het.27 Α-628 Br Η HH Het.27 Α-629 ch3 Η HH Het.27 Α-630 chf2 Η HH Het.27 Α-631 cf3 Η HH Het.27 Α-632 OCH3 Η HH Het.27 Α-633 OCHF2 Η HH Het.27 Α-634 OCF3 Η HH Het.27 Α-635 Η FHH Het.27 Α-636 Η C1 HH Het.27 Α-637 Η Βγ HH Het.27 Α- 638 Η ch3 HH Het.27 Α-639 Η chf2 HH Het.27 Α-640 Η cf3 HH Het.27 Α-641 Η OCH3 HH Het.27 Α-642 Η OCHF2 HH Het.27 Α-643 Η OCF3 HH Het .27 Α-644 FFHH Het.27 Α-645 F Η FH Het.27 Α-646 F Η HF Het.27 Α-647 Η FHF Het.27 Α-648 C1 Η HF Het.27 Α-64 9 Η Η HH Het.28 Α-650 F Η HH Het.28 Α-651 C1 Η HH Het.28 Α-652 Βγ Η HH Het.28 Α-653 ch3 Η HH Het.28 Α-654 chf2 Η HH Het .28 Α-655 cf3 Η HH Het.28 Α-656 OCH3 Η HH Het.28 Α-657 OCHF2 Η HH Het.28 Α-658 OCF3 Η HH Het.28 Α-659 Η FHH Het.28 Α-660 Η C1 HH Het.28 Α-661 Η Br HH Het.28 Α-662 Η ch3 HH Het.28 Α-663 Η chf2 HH Het.28 Α-664 Η cf3 HH Het.28 Α-665 Η OCH3 HH Het.28 Α-666 Η OCHF2 HH Het.28 [si 149026.doc ·96· 201103429 No. R1 R2 RJ r Het A-667 H OCF3 HH Het.28 A-668 FFHH Het.28 A-669 FHFH Het.28 A-670 FHHF Het.28 A-671 HFHF Het.28 A-672 Cl HHF Het.28 A-673 HHHH Het.29 A-674 FHHH Het.29 A-675 Cl HHH Het.29 A-676 Br HHH Het.29 A -677 ch3 HHH Het.29 A-678 chf2 HHH Het.29 A-679 cf3 HHH Het.29 A-680 OCH3 HHH Het.29 A-681 OCHF2 HHH Het.29 A-682 OCF3 HHH Het.29 A-683 HFHH Het.29 A-684 H Cl HH Het.29 A-685 H Br HH Het.29 A-686 H ch3 HH Het.29 A-687 H chf2 H H Het.29 A-688 H cf3 HH Het.29 A-689 H OCH3 HH Het.29 A-690 H OCHF2 HH Het.29 A-691 H OCF3 HH Het.29 A-692 FFHH Het.29 A-693 FHFH Het.29 A-694 FHHF Het.29 A-695 HFHF Het.29 A-696 Cl HHF Het.29 A-697 HHHH Het.30 A-698 FHHH Het.30 A-699 Cl HHH Het.30 A- 700 Br HHH Het.30 A-701 ch3 HHH Het.30 A-702 chf2 HHH Het.30 A-703 cf3 HHH Het.30 A-704 OCH3 HHH Het.30 A-705 OCHF2 HHH Het.30 A-706 OCF3 HHH Het.30 A-707 HFHH Het.30 A-708 H Cl HH Het.30 A-709 H Br HH Het.30 A-710 H ch3 HH Het.30 A-711 H chf2 HH Het.30 A-712 H cf3 HH Het.30 A-713 H OCH3 HH Het.30 A-714 H OCHF2 HH Het.30 149026.doc -97- 201103429 No. R1 R" RJ R4 Het A-715 H OCF3 HH Het.30 A-716 FFHH Het.30 A-717 FHFH Het.30 A-718 FHHF Het.30 A-719 HFHF Het.30 A-720 Cl HHF Het.30 A-721 HHHH Het.31 A-722 FHHH Het.31 A-723 Cl HHH Het.31 A-724 Br HHH Het.31 A-725 ch3 HHH Het.31 A-726 chf2 HHH Het.31 A-727 cf3 HHH He T.31 A-728 OCH3 HHH Het.31 A-729 OCHF2 HHH Het.31 A-730 OCF3 HHH Het.31 A-731 HFHH Het.31 A-732 H Cl HH Het.31 A-733 H Br HH Het .31 A-734 H ch3 HH Het.31 A-735 H chf2 HH Het.31 A-736 H cf3 HH Het.31 A-737 H OCH3 HH Het.31 A-738 H OCHF2 HH Het.31 A-739 H OCF3 HH Het.31 A-740 FFHH Het.31 A-741 FHFH Het.31 A-742 FHHF Het.31 A-743 HFHF Het.31 A-744 Cl HHF Het.31 A-745 HHHH Het.32 A -746 FHHH Het.32 A-747 Cl HHH Het.32 A-748 Br HHH Het.32 A-749 ch3 HHH Het.32 A-750 chf2 HHH Het.32 A-751 cf3 HHH Het.32 A-752 OCH3 HHH Het.32 A-753 OCHFz HHH Het.32 A-754 OCF3 HHH Het.32 A-755 HFHH Het.32 A-756 H Cl HH Het.32 A-757 H Br HH Het.32 A-758 H ch3 HH Het.32 A-759 H chf2 HH Het.32 A-760 H cf3 HH Het.32 A-761 H OCH3 HH Het.32 A-762 H OCHF2 HH Het.32 [si 149026.doc •98- 201103429 RJ R" RJ R4 Het A-763 H OCF3 HH Het.32 A-764 FFHH Het.32 A-765 FHFH Het.32 A-766 FHHF Het.32 A-767 H FHF Het.32 A-768 Cl HHF Het.32 A-769 HHHH Het.33 A-770 FHHH Het.33 A-771 Cl HHH Het.33 A-772 Br HHH Het.33 A-773 ch3 HHH Het.33 A-774 chf2 HHH Het.33 A-775 cf3 HHH Het.33 A-776 OCH3 HHH Het.33 A-777 OCHF2 HHH Het.33 A-778 OCF3 HHH Het.33 A-779 HFHH Het.33 A-780 H Cl HH Het.33 A-781 H Br HH Het.33 A-782 H ch3 HH Het.33 A-783 H chf2 HH Het.33 A-784 H cf3 HH Het.33 A-785 H OCH3 HH Het. 33 A-786 H OCHF2 HH Het.33 A-787 H OCF3 HH Het.33 A-788 FFHH Het.33 A-789 FHFH Het.33 A-790 FHHF Het.33 A-791 HFHF Het.33 A-792 Cl HHF Het.33 A-793 HHHH Het.34 A-794 FHHH Het.34 A-795 Cl HHH Het.34 A-796 Br HHH Het.34 A-797 ch3 HHH Het.34 A-798 chf2 HHH Het. 34 A-799 cf3 HHH Het.34 A-800 OCH3 HHH Het.34 A-801 OCHF2 HHH Het.34 A-802 OCF3 HHH Het.34 A-803 HFHH Het.34 A-804 H Cl HH Het.34 A -805 H Br HH Het.34 A-806 H ch3 HH Het.34 A-807 H chf2 HH Het.34 A-808 H cf3 HH Het.34 A-809 H och3 HH Het.34 A-810 H OCHF2 HH Het.34 149026.doc -99- 201103429 No. R1 Rz RJ r Het A-811 H OCF3 HH Het.34 A-812 FFHH Het.34 A-813 FHFH Het.34 A- 814 FHHF Het.34 A-815 HFHF Het.34 A-816 Cl HHF Het.34 A-817 HHHH Het.35 A-818 FHHH Het.35 A-819 Cl HHH Het.35 A-820 Br HHH Het.35 , A-821 ch3 HHH Het.35 A-822 chf2 HHH Het.35 A-823 cf3 HHH Het.35 A-824 OCH3 HHH Het.35 A-825 OCHF2 HHH Het.35 A-826 OCF3 HHH Het.35 A -827 HFHH Het.35 A-828 H Cl HH Het.35 A-829 H Br HH Het.35 A-830 H ch3 HH Het.35 A-831 H chf2 HH Het.35 A-832 H cf3 HH Het. 35 A-833 H OCH3 HH Het.35 A-834 H OCHF2 HH Het.35 A-835 H OCF3 HH Het.35 A-836 FFHH Het.35 A-837 FHFH Het.35 A-838 FHHF Het.35 A -839 HFHF Het.35 A-840 Cl HHF Het.35 A-841 HHHH Het.36 A-842 FHHH Het.36 A-843 Cl HHH Het.36 A-844 Br HHH Het.36 A-845 ch3 HHH Het .36 A-846 chf2 HHH Het.36 A-847 cf3 HHH Het.36 A-848 OCH3 HHH Het.36 A-849 OCHF2 HHH Het.36 A-850 OCF3 HHH Het.36 A-851 HFHH Het.36 A-852 H Cl HH Het.36 A-853 H Br HH Het.36 A-854 H ch3 HH Het.36 A-855 H chf2 HH Het. 36 A-856 H cf3 HH Het.36 A-857 H OCH3 HH Het.36 A-858 H OCHF2 HH Het.36

[SI 149026.doc -100- 201103429 編號 RJ R2 r Het A-859 H OCF3 H H Het.36 A-860 F F H H Het.36 A-861 F H F H Het.36 A-862 F H H F Het.36 A-863 H F H F Het.36 A-864 Cl H H F Het.36 A-865 H H H H Het.37 A-866 F H H H Het.37 A-867 Cl H H H Het.37 A-868 Br H H H Het.37 A-869 ch3 H H H Het.37 A-870 chf2 H H H Het.37 A-871 cf3 H H H Het.37 A-872 och3 H H H Het.37 A-873 OCHF2 H H H Het.37 A-874 OCF3 H H H Het.37 A-875 H F H H Het.37 A-876 H Cl H H Het.37 A-877 H Br H H Het.37 A-878 H ch3 H H Het.37 A-879 H chf2 H H Het.37 A-880 H cf3 H H Het.37 A-881 H OCH3 H H Het.37 A-882 H OCHF2 H H Het.37 A-883 H OCF3 H H Het.37 A-884 F F H H Het.37 A-885 F H F H Het.37 A-886 F H H F Het.37 A-887 H F H F Het.37 A-888 Cl H H F Het.37 A-889 H H H H Het.38 A-890 F H H H Het.38 A-891 Cl H H H Het.38 A-892 Br H H H Het.38 A-893 ch3 H H H Het.38 A-894 chf2 H H H Het.38 A-895 cf3 H H H Het.38 A-896 OCH3 H H H Het.38 A-897 OCHF2 H H H Het.38 A-898 OCF3 H H H Het.38 A-899 H F H H Het.38 A-900 H Cl H H Het.38 A-901 H Br H H Het.38 A-902 H ch3 H H Het.38 A-903 H chf2 H H Het.38 A-904 H cf3 H H Het.38 A-905 H 〇CH3 H H Het.38 A-906 H ochf2 H H Het.38 149026.doc -101 - 201103429 編號 R1 Rz RJ R4 Het A-907 H OCF3 H H Het.38 A-908 F F H H Het.38 A-909 F H F H Het.38 A-910 F H H F Het.38 A-911 H F H F Het.38 A-912 Cl H H F Het.38 A-913 H H H H Het.39 A-914 F H H H Het.39 A-915 Cl H H H Het.39 A-916 Br H H H Het.39 A-917 ch3 H H H Het.39 A-918 chf2 H H H Het.39 A-919 cf3 H H H Het.39 A-920 OCH3 H H H Het.39 A-921 OCHF2 H H H Het.39 A-922 OCF3 H H H Het.39 A-923 H F H H Het.39 A-924 H Cl H H Het.39 A-925 H Br H H Het.39 A-926 H ch3 H H Het.39 A-927 H chf2 H H Het.39 A-928 H cf3 H H Het.39 A-929 H OCH3 H H Het.39 A-930 H OCHF2 H H Het.39 A-931 H OCF3 H H Het.39 A-932 F F H H Het.39 A-933 F H F H Het.39 A-934 F H H F Het.39 A-935 H F H F Het.39 A-936 Cl H H F Het.39 A-937 H H H H Het.40 A-938 F H H H Het.40 A-939 Cl H H H Het.40 A-940 Br H H H Het.40 A-941 ch3 H H H Het.40 A-942 chf2 H H H Het.40 A-943 cf3 H H H Het.40 A-944 OCH3 H H H Het.40 A-945 OCHF2 H H H Het.40 A-946 OCF3 H H H Het.40 A-947 H F H H Het.40 A-948 H Cl H H Het.40 A-949 H Br H H Het.40 A-950 H ch3 H H Het.40 A-951 H chf2 H H Het.40 A-952 H cf3 H H Het.40 A-953 H OCH3 H H Het.40 A-954 H OCHF2 H H Het.40 [si 149026.doc -102- 201103429 編號 R1 R2 Rj R4 Het A-955 H ocf3 H H Het.40 A-956 F F H H Het.40 A-957 F H F H Het.40 A-958 F H H F Het.40 A-959 H F H F Het.40 A-960 Cl H H F Het.40 A-961 H H H H Het.41 A-962 F H H H Het.41 A-963 Cl H H H Het.41 A-964 Br H H H Het.41 A-965 CH3 H H H Het.41 A-966 chf2 H H H Het.41 A-967 cf3 H H H Het.41 A-968 och3 H H H Het.41 A-969 ochf2 H H H Het.41 A-970 ocf3 H H H Het.41 A-971 H F H H Het.41 A-972 H Cl H H Het.41 A-973 H Br H H Het.41 A-974 H ch3 H H Het.41 A-975 H chf2 H H Het.41 A-976 H cf3 H H Het.41 A-977 H och3 H H Het.41 A-978 H ochf2 H H Het.41 A-979 H ocf3 H H Het.41 A-980 F F H H Het.41 A-981 F H F H Het.41 A-982 F H H F Het.41 A-983 H F H F Het.41 A-984 Cl H H F Het.41 A-985 H H H H Het.42 A-986 F H H H Het.42 A-987 Cl H H H Het.42 A-988 Br H H H Het.42 A-989 ch3 H H H Het.42 A-990 chf2 H H H Het.42 A-991 cf3 H H H Het.42 A-992 och3 H H H Het.42 A-993 ochf2 H H H Het.42 A-994 ocf3 H H H Het.42 A-995 H F H H Het.42 A-996 H Cl H H Het.42 A-997 H Br H H Het.42 A-998 H ch3 H H Het.42 A-999 H chf2 H H Het.42 A-1000 H cf3 H H Het.42 A-1001 H och3 H . H Het.42 A-1002 H ochf2 H H Het.42 149026.doc -103- 201103429 編號 R1 RJ r Het A-1003 H ocf3 H H Het.42 A-1004 F F H H Het.42 A-1005 F H F H Het.42 A-1006 F H H F Het.42 A-1007 H F H F Het.42 A-1008 Cl H H F Het.42 A-1009 H H H H Het.43 A-1010 F H H H Het.43 A-1011 Cl H H H Het.43 A-1012 Br H H H Het.43 A-1013 ch3 H H H Het.43 A-1014 chf2 H H H Het.43 A-1015 cf3 H H H Het.43 A-1016 och3 H H H Het.43 A-1017 ochf2 H H H Het.43 A-1018 ocf3 H H H Het.43 A-1019 H F H H Het.43 A-1020 H Cl H H Het.43 A-1021 H Br H H Het.43 A-1022 H ch3 H H Het.43 A-1023 H chf2 H H Het.43 A-1024 H cf3 H H Het.43 A-1025 H och3 H H Het.43 A-1026 H ochf2 H H Het.43 A-1027 H ocf3 H H Het.43 A-1028 F F H H Het.43 A-1029 F H F H Het.43 A-1030 F H H F Het.43 A-1031 H F H F Het.43 A-1032 Cl H H F Het.43 A-1033 H H H H Het.44 A-1034 F H H H Het.44 A-1035 Cl H H H Het.44 A-1036 Br H H H Het.44 A-1037 ch3 H H H Het.44 A-1038 chf2 H H H Het.44 A-1039 cf3 H H H Het.44 A-1040 och3 H H H Het.44 A-1041 ochf2 H H H Het.44 A-1042 ocf3 H H H Het.44 A-1043 H F H H Het.44 A-1044 H Cl H H Het.44 A-1045 H Br H H Het.44 A-1046 H ch3 H H Het.44 A-1047 H chf2 H H Het.44 A-1048 H cf3 H H Het.44 A-1049 H och3 H H Het.44 A-1050 H ochf2 H H Het.44 [s] 149026.doc •104- 201103429 編號 R1 R2 RJ r Het A-1051 H ocf3 H H Het.44 A-1052 F F H H Het.44 A-1053 F H F H Het.44 A-1054 F H H F Het.44 A-1055 H F H F Het.44 A-1056 Cl H H F Het.44 A-1057 H H H H Het.45 A-1058 F H H H Het.45 A-1059 Cl H H H Het.45 A-1060 Br H H H Het.45 A-1061 ch3 H H H Het.45 A-1062 chf2 H H H Het.45 A-1063 cf3 H H H Het.45 A-1064 och3 H H H Het.45 A-1065 ochf2 H H H Het.45 A-1066 ocf3 H H H Het.45 A-1067 H F H H Het.45 A-1068 H Cl H H Het.45 A-1069 H Br H H Het.45 A-1070 H ch3 H H Het.45 A-1071 H chf2 H H Het.45 A-1072 H cf3 H H Het.45 A-1073 H och3 H H Het.45 A-1074 H ochf2 H H Het.45 A-1075 H OCF3 H H Het.45 A-1076 F F H H Het.45 A-1077 F H F H Het.45 A-1078 F H H F Het.45 A-1079 H F H F Het.45 A-1080 Cl H H F Het.45 A-1081 H H H H Het.46 A-1082 F H H H Het.46 A-1083 Cl H H H Het.46 A-1084 Br H H H Het.46 A-1085 ch3 H H H Het.46 A-1086 chf2 H H H Het.46 A-1087 cf3 H H H Het.46 A-1088 och3 H H H Het.46 A-1089 ochf2 H H H Het.46 A-1090 ocf3 H H H Het.46 A-1091 H F H H Het.46 A-1092 H Cl H H Het.46 A-1093 H Br H H Het.46 A-1094 H ch3 H H Het.46 A-1095 H chf2 H H Het.46 A-1096 H cf3 H H Het.46 A-1097 H OCH3 H H Het.46 A-1098 H OCHF2 H H Het.46 149026.doc -105- 201103429 編號 R1 RJ R4 Het A-1099 H ocf3 H H Het.46 A-1100 F F H H Het.46 A-1101 F H F H Het.46 A-1102 F H H F Het.46 A-1103 H F H F Het.46 A-1104 Cl H H F Het.46 A-1105 H H H H Het.47 A-1106 F H H H Het.47 A-1107 Cl H H H Het.47 A-1108 Br H H H Het.47 A-1109 ch3 H H H Het.47 A-1110 chf2 H H H Het.47 A-llll cf3 H H H Het.47 A-1112 och3 H H H Het.47 A-1113 ochf2 H H H Het.47 A-1114 ocf3 H H H Het.47 A-1115 H F H H Het.47 A-1116 H Cl H H Het.47 A-1117 H Br H H Het.47 A-1118 H ch3 H H Het.47 A-1119 H chf2 H H Het.47 A-1120 H cf3 H H Het.47 A-1121 H och3 H H Het.47 A-1122 H ochf2 H H Het.47 A-1123 H ocf3 H H Het.47 A-1124 F F H H Het.47 A-1125 F H F H Het.47 A-1126 F H H F Het.47 A-1127 H F H F Het.47 A-1128 Cl H H F Het.47 A-1129 H H H H Het.48 A-1130 F H H H Het.48 A-1131 Cl H H H Het.48 A-1132 Br H H H Het.48 A-1133 ch3 H H H Het.48 A-1134 chf2 H H H Het.48 A-1135 cf3 H H H Het.48 A-1136 och3 H H H Het.48 A-1137 ochf2 H H H Het.48 A-1138 ocf3 H H H Het.48 A-1139 H F H H Het.48 A-1140 H Cl H H Het.48 A-1141 H Br H H Het.48 A-1142 H ch3 H H Het.48 A-1143 H chf2 H H Het.48 A-1144 H cf3 H H Het.48 A-1145 H och3 H H Het.48 A-1146 H ochf2 H H Het.48 [si 149026.doc •106- 201103429[SI 149026.doc -100- 201103429 No. RJ R2 r Het A-859 H OCF3 HH Het.36 A-860 FFHH Het.36 A-861 FHFH Het.36 A-862 FHHF Het.36 A-863 HFHF Het. 36 A-864 Cl HHF Het.36 A-865 HHHH Het.37 A-866 FHHH Het.37 A-867 Cl HHH Het.37 A-868 Br HHH Het.37 A-869 ch3 HHH Het.37 A-870 Chf2 HHH Het.37 A-871 cf3 HHH Het.37 A-872 och3 HHH Het.37 A-873 OCHF2 HHH Het.37 A-874 OCF3 HHH Het.37 A-875 HFHH Het.37 A-876 H Cl HH Het.37 A-877 H Br HH Het.37 A-878 H ch3 HH Het.37 A-879 H chf2 HH Het.37 A-880 H cf3 HH Het.37 A-881 H OCH3 HH Het.37 A- 882 H OCHF2 HH Het.37 A-883 H OCF3 HH Het.37 A-884 FFHH Het.37 A-885 FHFH Het.37 A-886 FHHF Het.37 A-887 HFHF Het.37 A-888 Cl HHF Het .37 A-889 HHHH Het.38 A-890 FHHH Het.38 A-891 Cl HHH Het.38 A-892 Br HHH Het.38 A-893 ch3 HHH Het.38 A-894 chf2 HHH Het.38 A- 895 cf3 HHH Het.38 A-896 OCH3 HHH Het.38 A-897 OCHF2 HHH Het.38 A-898 OCF3 HHH Het.38 A-899 HFHH Het.38 A-900 H Cl HH Het.38 A-901 H Br HH Het.38 A-902 H ch3 HH Het.38 A-903 H chf2 HH Het.38 A-904 H cf3 HH Het.38 A -905 H 〇CH3 HH Het.38 A-906 H ochf2 HH Het.38 149026.doc -101 - 201103429 No. R1 Rz RJ R4 Het A-907 H OCF3 HH Het.38 A-908 FFHH Het.38 A-909 FHFH Het.38 A-910 FHHF Het.38 A-911 HFHF Het.38 A-912 Cl HHF Het.38 A-913 HHHH Het.39 A-914 FHHH Het.39 A-915 Cl HHH Het.39 A- 916 Br HHH Het.39 A-917 ch3 HHH Het.39 A-918 chf2 HHH Het.39 A-919 cf3 HHH Het.39 A-920 OCH3 HHH Het.39 A-921 OCHF2 HHH Het.39 A-922 OCF3 HHH Het.39 A-923 HFHH Het.39 A-924 H Cl HH Het.39 A-925 H Br HH Het.39 A-926 H ch3 HH Het.39 A-927 H chf2 HH Het.39 A-928 H cf3 HH Het.39 A-929 H OCH3 HH Het.39 A-930 H OCHF2 HH Het.39 A-931 H OCF3 HH Het.39 A-932 FFHH Het.39 A-933 FHFH Het.39 A-934 FHHF Het.39 A-935 HFHF Het.39 A-936 Cl HHF Het.39 A-937 HHHH Het.40 A-938 FHHH Het.40 A-939 Cl HHH Het.40 A-940 Br HHH Het.40 A-941 ch3 HHH Het.40 A-942 chf2 HHH Het.40 A-943 cf3 HHH Het.40 A-944 OCH3 HHH Het.40 A-945 OCHF2 HHH Het. 40 A-946 OCF3 HHH Het.40 A-947 HFHH Het.40 A-948 H Cl HH Het.40 A-949 H Br HH Het.40 A-950 H ch3 HH Het.40 A-951 H chf2 HH Het .40 A-952 H cf3 HH Het.40 A-953 H OCH3 HH Het.40 A-954 H OCHF2 HH Het.40 [si 149026.doc -102- 201103429 No. R1 R2 Rj R4 Het A-955 H ocf3 HH Het.40 A-956 FFHH Het.40 A-957 FHFH Het.40 A-958 FHHF Het.40 A-959 HFHF Het.40 A-960 Cl HHF Het.40 A-961 HHHH Het.41 A-962 FHHH Het.41 A-963 Cl HHH Het.41 A-964 Br HHH Het.41 A-965 CH3 HHH Het.41 A-966 chf2 HHH Het.41 A-967 cf3 HHH Het.41 A-968 och3 HHH Het. A-969 ochf2 HHH Het. 41 A-975 H chf2 HH Het.41 A-976 H cf3 HH Het.41 A-977 H och3 HH Het.41 A-978 H ochf2 HH Het.41 A-979 H ocf3 HH Het.41 A-980 FFHH Het.41 A-981 FHFH Het.41 A-982 FHHF Het.41 A-983 HFHF Het.41 A-984 Cl HHF Het.41 A-985 HHHH Het.42 A -986 FHHH Het.42 A-987 Cl HHH Het.42 A-988 Br HHH Het.42 A-989 ch3 HHH Het.42 A-990 chf2 HHH Het.42 A-991 cf3 HHH Het.42 A-992 och3 HHH Het.42 A-993 ochf2 HHH Het.42 A-994 ocf3 HHH Het.42 A-995 HFHH Het.42 A-996 H Cl HH Het.42 A-997 H Br HH Het.42 A-998 H ch3 HH Het.42 A-999 H chf2 HH Het.42 A-1000 H cf3 HH Het.42 A-1001 H och3 H . H Het.42 A-1002 H ochf2 HH Het.42 149026.doc -103- 201103429 R1 RJ r Het A-1003 H ocf3 HH Het.42 A-1004 FFHH Het.42 A-1005 FHFH Het.42 A-1006 FHHF Het.42 A-1007 HFHF Het.42 A-1008 Cl HHF Het.42 A -1009 HHHH Het.43 A-1010 FHHH Het.43 A-1011 Cl HHH Het.43 A-1012 Br HHH Het.43 A-1013 ch3 HHH Het.43 A-1014 chf2 HHH Het.43 A-1015 cf3 HHH Het.43 A-1016 och3 HHH Het.43 A-1017 ochf2 HHH Het.43 A-1018 ocf3 HHH Het. 43 A-1019 HFHH Het.43 A-1020 H Cl HH Het.43 A-1021 H Br HH Het.43 A-1022 H ch3 HH Het.43 A-1023 H chf2 HH Het.43 A-1024 H cf3 HH Het.43 A-1025 H och3 HH Het.43 A-1026 H ochf2 HH Het.43 A-1027 H ocf3 HH Het.43 A-1028 FFHH Het.43 A-1029 FHFH Het.43 A-1030 FHHF Het. 43 A-1031 HFHF Het.43 A-1032 Cl HHF Het.43 A-1033 HHHH Het.44 A-1034 FHHH Het.44 A-1035 Cl HHH Het.44 A-1036 Br HHH Het.44 A-1037 ch3 HHH Het.44 A-1038 chf2 HHH Het.44 A-1039 cf3 HHH Het.44 A-1040 och3 HHH Het.44 A-1041 ochf2 HHH Het.44 A-1042 ocf3 HHH Het.44 A-1043 HFHH Het. 44 A-1044 H Cl HH Het.44 A-1045 H Br HH Het.44 A-1046 H ch3 HH Het.44 A-1047 H chf2 HH Het.44 A-1048 H cf3 HH Het.44 A-1049 H Och3 HH Het.44 A-1050 H ochf2 HH Het.44 [s] 149026.doc •104- 201103429 No. R1 R2 RJ r Het A-1051 H ocf3 HH Het.44 A-1052 FFHH Het.44 A-1053 FHFH Het.44 A-1054 FHHF Het.44 A-1055 HFHF Het.44 A-1056 Cl HHF Het.44 A-1057 H HHH Het.45 A-1058 FHHH Het.45 A-1059 Cl HHH Het.45 A-1060 Br HHH Het.45 A-1061 ch3 HHH Het.45 A-1062 chf2 HHH Het.45 A-1063 cf3 HHH Het. 45 A-1064 och3 HHH Het.45 A-1065 ochf2 HHH Het.45 A-1066 ocf3 HHH Het.45 A-1067 HFHH Het.45 A-1068 H Cl HH Het.45 A-1069 H Br HH Het.45 A-1070 H ch3 HH Het.45 A-1071 H chf2 HH Het.45 A-1072 H cf3 HH Het.45 A-1073 H och3 HH Het.45 A-1074 H ochf2 HH Het.45 A-1075 H OCF3 HH Het.45 A-1076 FFHH Het.45 A-1077 FHFH Het.45 A-1078 FHHF Het.45 A-1079 HFHF Het.45 A-1080 Cl HHF Het.45 A-1081 HHHH Het.46 A-1082 FHHH Het.46 A-1083 Cl HHH Het.46 A-1084 Br HHH Het.46 A-1085 ch3 HHH Het.46 A-1086 chf2 HHH Het.46 A-1087 cf3 HHH Het.46 A-1088 och3 HHH Het .46 A-1089 ochf2 HHH Het.46 A-1090 ocf3 HHH Het.46 A-1091 HFHH Het.46 A-1092 H Cl HH Het.46 A-1093 H Br HH Het.46 A-1094 H ch3 HH Het .46 A-1095 H chf2 HH Het.46 A-1096 H cf3 HH Het.46 A-1097 H OCH3 HH Het .46 A-1098 H OCHF2 HH Het.46 149026.doc -105- 201103429 No. R1 RJ R4 Het A-1099 H ocf3 HH Het.46 A-1100 FFHH Het.46 A-1101 FHFH Het.46 A-1102 FHHF Het.46 A-1103 HFHF Het.46 A-1104 Cl HHF Het.46 A-1105 HHHH Het.47 A-1106 FHHH Het.47 A-1107 Cl HHH Het.47 A-1108 Br HHH Het.47 A- 1109 ch3 HHH Het.47 A-1110 chf2 HHH Het.47 A-llll cf3 HHH Het.47 A-1112 och3 HHH Het.47 A-1113 ochf2 HHH Het.47 A-1114 ocf3 HHH Het.47 A-1115 HFHH Het.47 A-1116 H Cl HH Het.47 A-1117 H Br HH Het.47 A-1118 H ch3 HH Het.47 A-1119 H chf2 HH Het.47 A-1120 H cf3 HH Het.47 A- 1121 H och3 HH Het.47 A-1122 H ochf2 HH Het.47 A-1123 H ocf3 HH Het.47 A-1124 FFHH Het.47 A-1125 FHFH Het.47 A-1126 FHHF Het.47 A-1127 HFHF Het.47 A-1128 Cl HHF Het.47 A-1129 HHHH Het.48 A-1130 FHHH Het.48 A-1131 Cl HHH Het.48 A-1132 Br HHH Het.48 A-1133 ch3 HHH Het.48 A -1134 chf2 HHH Het.48 A-1135 cf3 HHH Het.48 A-1136 och3 HHH Het.48 A-1137 ochf2 HHH Het.48 A-1138 ocf3 HHH Het.48 A-1139 HFHH Het.48 A-1140 H Cl HH Het.48 A-1141 H Br HH Het.48 A-1142 H ch3 HH Het.48 A-1143 H chf2 HH Het.48 A-1144 H cf3 HH Het.48 A-1145 H och3 HH Het.48 A-1146 H ochf2 HH Het.48 [si 149026.doc •106- 201103429

基團Het· 1至Het.49對應於上文所列作為式Het」至Het 49 之基團的Het之特定實施例的基團。 在上述化合物中,較佳為式L1至124、」 至II.24之化合物。在此等化合物中,較佳為化合物u、 1.2 ^1.13 ^1.14 >1.49 ^1.50, 1.61^ 1.62^ IU,II2,II13 及Π.14。更佳為化合物U、1.2、1.49、f.5〇、η ]及JI2且 甚至更佳為化合物及„·2β 式I及II之化合物可藉由一 Α夕禋卜列如下文流程1至9及 149026.doc .107- 201103429 合成詳情中所述之方法及變化形式來製備。變數係如上文 對式I及π所定義。 式1化合物,其中r6為Η且m為0(或化合物II,其中R6a為 H)可如流私1中所概述藉由硫化相應的三唑衍生物a來製 備硫化反應可類似於(例如’如WO 96/41 804中所述之) 已头方法來進行。舉例而言,三唑基環可首先用以下強鹼 去除質子化,例如有機鋰鹼,諸如正丁基鋰、第三丁基鋰The groups Het·1 to Het.49 correspond to the groups of the specific examples of Het listed above as the group of the formulas Het" to Het 49. Among the above compounds, preferred are compounds of the formulae L1 to 124, and to II.24. Among these compounds, preferred are compounds u, 1.2 ^ 1.13 ^ 1.14 > 1.49 ^ 1.50, 1.61 ^ 1.62 ^ IU, II 2 , II 13 and Π. More preferably, the compounds U, 1.2, 1.49, f.5, η, and JI2 and even more preferably are compounds and „·2β compounds of the formulae I and II can be listed by the following schemes 1 to 9 And 149026.doc.107-201103429 The methods and variations described in the synthesis details are prepared. The variables are as defined above for Formulas I and π. Compounds of Formula 1, wherein r6 is oxime and m is 0 (or Compound II, Wherein R6a is H), the vulcanization reaction can be carried out by vulcanization of the corresponding triazole derivative a as outlined in Flow 1, which can be carried out analogously (e.g., as described in WO 96/41 804). For example, a triazolyl ring may first be deprotonated with a strong base such as an organolithium base such as n-butyllithium, tert-butyllithium

基乙二胺(TMEDA)混合之第三丁醇鉀,隨後所得陰離子與 兀素硫反應。-般使用粉末狀硫。反應一般在惰性溶劑, 甲基第三丁基趟、四氫吱喃或二 液氨、二甲亞砜或二曱基曱醯胺 諸如趟類(例如二乙喊、甲基穿 °惡烷)、二甲氧基乙烷、液氨、 中進行。反應溫度不是很關鍵且可在例如_7〇至+5〇。〇,較 佳-70至〇°C之範圍内。或者,硫化反應可在不存在驗之情 況下,藉由使7與元素硫在高沸點溶劑(諸如N_甲基吡咯啶 二甲基甲酿胺)中反應同時加熱至例如 。在元成該反應之後,例如藉由添加水 酮、二噁烷或N,N-二 160至250°C來進行。 或含水酸,諸如無機酸(例如稀硫酸或鹽酸卜乙酸或氯化 鈹來水解所得混合物,得到化合物I。 流程1Potassium tert-butoxide mixed with ethylenediamine (TMEDA), and the resulting anion is then reacted with alizarin sulfur. General use of powdered sulfur. The reaction is generally carried out in an inert solvent, methyl tert-butyl hydrazine, tetrahydrofuran or two-liquid ammonia, dimethyl sulfoxide or decyl decylamine such as hydrazine (for example, diethyl sulfonate, methyl phthalocyanine). , dimethoxyethane, liquid ammonia, medium. The reaction temperature is not critical and can be, for example, from _7 〇 to +5 〇. 〇, preferably within the range of -70 to 〇 °C. Alternatively, the sulfurization reaction may be heated to, for example, by reacting 7 with elemental sulfur in a high boiling solvent such as N-methylpyrrolidine dimethylamine, in the absence of a test. After the reaction, the reaction is carried out, for example, by adding water ketone, dioxane or N, N-di 160 to 250 °C. Or aqueous acid, such as a mineral acid such as dilute sulfuric acid or hydrochloric acid or acetic acid to hydrolyze the resulting mixture to give compound I. Scheme 1

149026.doc -108- 201103429 如流程2中所概述,三唑化合物IV可類似於已知方法(諸 如在例如EP-A-0065485中所述)來製備。舉例而言,化合 物;1(其中X為良好的脫離基,諸如南素原子,尤其Ο、^ 或I’苯基磺醯基氧基、對甲苯磺醯基氧基、三氟乙醯氧 基或烧基續醯基氧基,諸如曱續醯基氧基)可與 二唑化合物2(其中Μ為氫原子或金屬原子,尤其鹼金屬原 子,諸如Li、Na或Κ)反應《在肘為11之情況下,反應宜在 鹼,諸如鹼金屬氫化物(例如氫化鈉、氫化鉀)、鹼金屬氫 氧化物(例如氫氧化鈉、氫氧化鉀)、鹼金屬碳酸鹽(例如碳 酸鈉、碳酸鉀、碳酸鉋)或合適之胺(例如三乙胺、三伸乙 二胺、哌啶、吡啶、4-二甲基胺基吡啶、4_吡咯啶基吡啶) 存在下進行。若X為C1或Br,則可藉由添加鹼金屬碘化物 (諸如Nal或KI)來促進反應。反應宜在溶劑中進行。合適 之溶劑為惰性溶劑而反應物與產物相當有極性,例如, N,N_二甲基曱醯胺、N,N-二曱基乙醯胺、二曱亞碾、乙 腈、本甲腈、謎類(諸如二乙鱗、二丙謎、甲基第r 丁美 醚、四氫呋喃或二噁烷)及其類似物,且可與以下其他極 性較小之惰性溶劑組合使用,諸如苯 '甲苯、二曱苯、氣 苯、硝基苯、己烷、庚烷、石油醚及其類似物。反應溫度 不是很關鍵且可在例如0至220。〇且較佳80至170°C之範圍 内。反應宜在反應混合物之回流溫度下進行。 149026.doc •109- 201103429 流程2149026.doc -108- 201103429 As outlined in Scheme 2, the triazole compound IV can be prepared analogously to known methods, such as described, for example, in EP-A-0 065 485. For example, a compound; 1 (wherein X is a good leaving group, such as a ruthenium atom, especially oxime, ^ or I'phenylsulfonyloxy, p-toluenesulfonyloxy, trifluoroacetoxy Or a mercapto group, such as a fluorenyloxy group, can be reacted with an oxadiazole compound 2 (wherein hydrazine is a hydrogen atom or a metal atom, especially an alkali metal atom such as Li, Na or hydrazine) In the case of 11, the reaction is preferably carried out in a base such as an alkali metal hydride (e.g., sodium hydride, potassium hydride), an alkali metal hydroxide (e.g., sodium hydroxide, potassium hydroxide), an alkali metal carbonate (e.g., sodium carbonate, carbonic acid). It is carried out in the presence of potassium, carbonic acid or a suitable amine such as triethylamine, triethylenediamine, piperidine, pyridine, 4-dimethylaminopyridine or 4-pyrrolidinylpyridine. If X is C1 or Br, the reaction can be promoted by the addition of an alkali metal iodide such as Nal or KI. The reaction is preferably carried out in a solvent. Suitable solvents are inert solvents and the reactants are quite polar to the product, for example, N,N-dimethyl decylamine, N,N-dimercaptoacetamide, diterpene, acetonitrile, carbonitrile, A mystery (such as di-butyl scale, diacetyl, methyl ri-butyl ether, tetrahydrofuran or dioxane) and its analogs, and can be used in combination with other less polar inert solvents such as benzene'toluene, Diphenylbenzene, gas benzene, nitrobenzene, hexane, heptane, petroleum ether and the like. The reaction temperature is not critical and can be, for example, from 0 to 220. Preferably, it is in the range of 80 to 170 °C. The reaction is preferably carried out at the reflux temperature of the reaction mixture. 149026.doc •109- 201103429 Process 2

如以下流程3中所概述,化合物J又可類似於已知方法 (諸如,在 EP-A-0065485或 Synthesis,1974,I,23 中所述)來 製備。舉例而言,酮3可與二醇H〇_A_〇t^i佳在形成共沸 物的化合物(諸如苯、曱苯、二曱苯、氣仿或四氣甲烷, 其亦可充當反應溶劑)存在下反應若干小時。藉由強酸(諸 如對甲苯續酸)之存在來促進縮酮化反應(ketalization reaction)。後續鹵化所得縮酮4產生縮酮1,其中又為_素 原子,若需要,則其可轉化為化合物j,其中χ為除鹵素以 外的脫離基。 流程3Compound J can, in turn, be prepared analogously to known methods, such as those described in EP-A-0 065 485 or Synthesis, 1974, I, 23, as outlined in Scheme 3 below. For example, ketone 3 may be a compound which forms an azeotrope with diol H〇_A_〇t^i (such as benzene, toluene, diphenylbenzene, gas, or tetra-methane, which may also act as a reaction). The reaction is carried out for several hours in the presence of a solvent. The ketalization reaction is promoted by the presence of a strong acid such as p-toluene. Subsequent halogenation of the resulting ketal 4 produces a ketal 1, which in turn is a zeolitic atom which, if desired, can be converted to compound j, wherein oxime is a cleavage group other than halogen. Process 3

如以下流程4中所概述,酮3可類似於已知方法(諸如, 在例如ΕΡ-Α-0065485中所述,化合物5與6之縮合反應)沪 得’其中X1為基團γ_Η或Υ-Μ,其中Μ為金屬原子,尤其 鹼金屬原子,諸如Li、Na或Κ,且X2為良好的脫離基,諸 如鹵素原子’諸如F、Cl、Br或I’苯基確酿基氧基、對甲 149026.doc • 110- 201103429 苯磺醯基氧基、三氟乙醯氧基或烷基磺醯基氧基,諸如甲 磺酿基氧基’或反之亦然,其中X1為良好的脫離基且χ2為 基團Y-H或Y-M。在X1或X2為Y-H之情況下,反應宜在驗, 諸如鹼金屬氫化物(例如氫化納、氫化鉀)、驗金屬氫氧化 物(例如氩氧化鈉、氫氧化鉀)、鹼金屬碳酸鹽(例如碳酸 鈉、碳酸鉀、碳酸絶)或合適之胺(例如三乙胺、三伸乙二 胺、哌啶、吡啶、4-二甲基胺基吡啶、4-吡咯啶基吡啶)存 在下進行。若脫離基X1或X2為C1或Br,則可藉由添加鹼金 屬硬化物(諸如NaI或KI)促進反應。反應宜在溶劑中進 行。合適之溶劑為惰性溶劑而反應物與產物相當有極性, 例如,Ν,Ν-二曱基曱醯胺、Ν,Ν·二甲基乙醯胺、二曱亞 碾、乙腈、笨甲腈、醚類(諸如二乙趟、二丙喊、甲基第 二丁基醚、四氫呋喃或二噁烷)及其類似物,且可與以下 其他極性較小之惰性溶劑組合使用,諸如苯、曱笨、二曱 苯、氯苯、硝基苯、己烷、庚烷、石油醚及其類似物。反 應溫度不是很關鍵且可在例如〇至22〇。〇且較佳8〇至17〇。〇 之範圍内。反應宜在反應混合物之回流溫度下進行。 流程4As outlined in Scheme 4 below, ketone 3 can be similar to known methods (such as, for example, the condensation reaction of compounds 5 and 6 as described in ΕΡ-Α-0065485), where X1 is a group γ_Η or Υ- Μ, wherein Μ is a metal atom, especially an alkali metal atom such as Li, Na or ruthenium, and X 2 is a good leaving group such as a halogen atom such as F, Cl, Br or I'phenyl acyloxy, A 149026.doc • 110-201103429 Benzenesulfonyloxy, trifluoroacetoxy or alkylsulfonyloxy, such as methylsulfonyloxy' or vice versa, where X1 is a good leaving group And χ2 is a group YH or YM. In the case where X1 or X2 is YH, the reaction is preferably tested, such as alkali metal hydride (such as sodium hydride, potassium hydride), metal hydroxide (such as sodium aroxide, potassium hydroxide), alkali metal carbonate ( For example, sodium carbonate, potassium carbonate, carbonic acid or a suitable amine (for example, triethylamine, triethylenediamine, piperidine, pyridine, 4-dimethylaminopyridine, 4-pyrrolidinopyridine) . If the leaving group X1 or X2 is C1 or Br, the reaction can be promoted by adding an alkali metal hardened substance such as NaI or KI. The reaction is preferably carried out in a solvent. Suitable solvents are inert solvents and the reactants are quite polar to the product, for example, hydrazine, hydrazine-dimercaptoamine, hydrazine, hydrazine dimethyl acetamide, bismuth acetonitrile, acetonitrile, carbonitrile, Ethers (such as diethyl hydrazine, dipropylene, methyl second butyl ether, tetrahydrofuran or dioxane) and the like, and can be used in combination with other less polar inert solvents, such as benzene, hydrazine Diphenylbenzene, chlorobenzene, nitrobenzene, hexane, heptane, petroleum ether and the like. The reaction temperature is not critical and can range, for example, to 22 Torr. And preferably 8 to 17 inches. Within the scope of 〇. The reaction is preferably carried out at the reflux temperature of the reaction mixture. Process 4

作為流程4中所述之方法的替代,如以下流程5中所概 述綱3(其中丫為0( = 3,))可類似於εΡ-α_〇〇65485中所述 149026.doc 201103429 之方法藉由碳酸酯7之脫羧反應來製備。其又可自羥基化 合物8來製備:羥基化合物8與以下碳酸之雙官能衍生物9 反應,諸如光氣、鹵素曱酸二醋、二炫基碳酸二S旨或二苯 基碳酸二S旨,且與紛10進一步反應。藉由實際上或在南〉弗 點惰性溶劑(諸如二苯醚或乙二醇二曱醚)中加熱7至120至 220°C範圍内之溫度進行脫羧反應。 流程5As an alternative to the method described in Scheme 4, as outlined in Scheme 5 below, Scheme 3 (where 丫 is 0 (= 3,)) can be similar to the method of 149026.doc 201103429 in εΡ-α_〇〇65485 It is prepared by the decarboxylation reaction of carbonate 7. It can also be prepared from hydroxy compound 8: hydroxy compound 8 is reacted with a difunctional derivative 9 of the following carbonic acid, such as phosgene, halogen bismuth diacetate, dimercaptocarbonate or S, or diphenyl carbonate. And further react with the 10. The decarboxylation reaction is carried out by heating in an inert solvent such as diphenyl ether or ethylene glycol dioxime in the range of from 7 to 120 to 220 °C. Process 5

+认+ recognition

作為流程2中所述之方法的替代,如以下流程6中所概 述,化合物IV可類似於Ep_A_0065485中所述之方法,藉由 酮11與二醇HO-A-OH之縮酮化反應來製備,可在流程3中 所述之反應條件下進行縮酮化反應。 流程6As an alternative to the method described in Scheme 2, compound IV can be prepared by a ketalization reaction of ketone 11 with diol HO-A-OH, similar to the method described in Ep_A_0065485, as outlined in Scheme 6 below. The ketalization reaction can be carried out under the reaction conditions described in Scheme 3. Process 6

149026.doc • 112- 201103429 中所述之方法’藉由使化合物12(其中X為良好的脫離基, 諸如鹵素原子,尤其C1、玢或工,苯基磺醯基氧基、對曱 苯磺醯基氧基、三氟乙醯氧基或烷基磺醯基氧基,諸如甲 磺醯氧基)與三唑化合物2在針對流程2中之反應所述的反 應條件下反應來製備。化合物12又可自酮3之鹵化反應獲 得。 流程7149026.doc • The method described in 112-201103429 'by compound 12 (wherein X is a good leaving group, such as a halogen atom, especially C1, hydrazine or phenylsulfonyloxy, p-toluenesulfonate) The decyloxy, trifluoroacetoxy or alkylsulfonyloxy group, such as methylsulfonyloxy, is prepared by reacting the triazole compound 2 under the reaction conditions described for the reaction in Scheme 2. Compound 12 is in turn obtainable from the halogenation of ketone 3. Process 7

作為流程2中所述方法的替代,如以下流程8中所概述, 化合物IV可類似於EP_A_0065485中所述之方法,藉由使化 合物13與14在針對流程4所述之反應條件下縮合來製備,其 中X1為基團Y-H或Y-M,其中Μ為金屬原子,尤其鹼金屬原 子,諸如Li、Na或Κ,且X2為良好的脫離基,諸如_素原 子’尤其Cl、Br或I,笨基續酿基氧基、對曱苯續酿基氧臭 二氣乙醯氧基或烧基續醯基氧基,諸如甲續醯基氧其,戈反 之亦然,其中X1為良好的脫離基且X2為基團γ_Η或γ·Μ。 流程8As an alternative to the process described in Scheme 2, compound IV can be prepared analogously to the process described in EP_A_0065485 by condensing compounds 13 and 14 under the reaction conditions described in Scheme 4, as outlined in Scheme 8 below. Wherein X1 is a group YH or YM, wherein hydrazine is a metal atom, especially an alkali metal atom such as Li, Na or hydrazine, and X2 is a good cleavage group, such as a _ atomic atom 'particularly Cl, Br or I, a stupid group Continuing the oxy-oxyl group, the fluorene-based phenolic aldehyde, the aldehyde or the decyloxy group, such as a fluorenyloxy group, and vice versa, wherein X1 is a good leaving group and X2 is a group γ_Η or γ·Μ. Process 8

149026.doc -113 - 201103429 作為流程2中所述方法的替代,如以下流程9中所概述, 化合物iv(其中γ為0( = IV,))可類似於eP_a_0065485中所 述之方法,藉由在針對流程5所述之反應條件下使碳酸酯 15脫羧來製備。碳酸酯15又可在針對流程5中之縮合反應 所述的反應條件下製備。 流程9149026.doc -113 - 201103429 As an alternative to the method described in Scheme 2, compound iv (where γ is 0 (= IV,)) can be similar to the method described in eP_a_0065485, as outlined in Scheme 9 below. Prepared by decarboxylation of carbonate 15 under the reaction conditions described in Scheme 5. Carbonate 15 can in turn be prepared under the reaction conditions described for the condensation reaction in Scheme 5. Process 9

可購得用於上述反應中之化合物5、6、8、9及1〇或可藉 由熟習此項技術者已知之標準方法來製造。 若上述反應物中之基團R,、R2、R3、R4及R5對各別反應 呈現惰性,則其可存在於上述反應步财或可在後—階段 引入(例如)化合物IV中。 式1化合物(其中R6不為氫且,可由化合物1(1中 R6=H且m=〇)來製備。 式】化合物(其中m為〇且r6為c r κ. « 其r Γ 巧且R為"3丨-Ci〇烷基、鹵烷 基2-Cl°稀基、C-c“烯基、c2-Cl。块基、c2_c“炔 基、C3-C丨。環院基、c 、 基装… 3 10齒㈣基、苯基、苯基似4烷 基,其十最後2個提及基團中 /JU s人士 J不丞4刀可如上所述經取 代,3有1、2或3個選自N、0及8之雜原 的5-或6-員飽和、邻八 乍為衣成貝 邛刀不飽和或方族雜環,其中雜環可如 [si 149026.doc -114- 201103429 上所述經取代)可類似於DE-A-19520098或WO 96/41804中 所述之方法,藉由使化合(其中111為〇且116為印與化合物 R6-LG(其中R6具有上述含義中之一者且[ο為脫離基,諸 如鹵基(例如Cl、Br、I)、甲笨磺酸酯基或曱磺酸酯基)反 應來製備。合適之鹼為例如,鹼金屬氫化物(例如氫化 鈉、氫化鉀)、鹼金屬氫氧化物(例如氫氧化鈉、氫氧化 鉀)、鹼金屬碳酸鹽(例如碳酸鈉、碳酸鉀、碳酸鉋)、鹼金 屬醇鹽(例如甲醇鈉、甲醇鉀、乙醇鈉、乙醇鉀、第三丁 醇鉀)或有機鋰鹼(例如正丁基鋰、第二丁基鋰、第三丁基 鋰及二異丙胺鋰广一般在合適之溶劑中進行反應。合適 之溶劑為例如甲苯、N_甲基吡咯啶酮、醚類(例如二乙 鍵、四氫咬喃、二。惡烧、12.二甲氧基乙烧)、乙腈' n,n_ 二曱基曱醯胺或二甲亞砜。 或者,式I化合物(其中„1為0且尺6為Ci_Ci〇烷基、Ci_c 函烷基、c2-ClG烯基' C2_CiG鹵稀基、C2_Ci❶块基、c2_c i炔基、匚3-(:10環烷基、C3_Ci〇函環烷基、苯基、笨基_c c4烧基’ Μ最後2個提及基團中的苯基部分可如上所述 經取代,及含有卜2或3個選自Ν、〇及8之雜原子作為環 成員的5·或6·員飽和、部分不飽和或芳族雜環,其中雜環 可如上所述經取代)可類似於Heter〇cycles,23(7),1645_ 祕,1985中所述之方法,藉由在類似於針對流程!所述之 條件下使化合物與二硫化物R6_s_m強驗存在下 式I化合物(其中為·C(=〇)R、c(=s)Ri2)可類 149026.doc -115- 201103429 似於DE-A-19617461中所述之方法,藉由使化合^(其中爪 為 0且 R6為 Η)與化合物 ri2_c(=〇)_w、r12_c(=s)_w、Rn,_ N=00或Ri2’_N=c = s(其中Rl2具有上述含義中之一, (VC,。烧基或Ci_ClGM基且|為良好的脫離基,諸如齒 基(例如Cl Br、I)、烷氧基(例如曱烷氧基、乙烷氧基)或 五氟苯氧基)在驗存在下反應來製備。合適之驗為例如, 时屬氫化物(例如氫化鈉、氫化鉀)、驗金屬氫氧化物(例 如氫氧化鈉、氫氧化鉀)、鹼金屬碳酸鹽“列如碳酸鈉、碳 酸鉀、碳酸絶)、驗金屬醇鹽(例如甲醇鈉、甲醇_、乙醇 鈉、乙醇鉀、第三丁醇鉀)或有機鋰鹼(例如正丁基鋰、第 二丁基經、第三丁基經及二異丙胺鐘)。反應—般在合適 之溶劑中進行。合適之溶劑為例如甲苯、n•甲基吼口各咬 酮、醚類(例如二乙醚、四氫呋喃、二噁烷、i,2-二甲氧基 乙烷)、〔腈、N,N-二曱基曱醯胺或二曱亞砜。 式1化合物(其巾①為0且R6為-so2r12)可類似於DE_a· 19620590 中所述之方、; 万法藉由使化合物1(其中m為0且R6為 H)與化合物R's〇2_w(其中Rl2具有上述含義中之一且w為 良好的脫離基,諸如齒基(例如a、氧基(例如 曱烧氧基6燒氧基)或五氟苯氧基)在驗存在下反應來製 備。合適之鹼為例 鹼金屬氫化物(例如氫化鈉、氫化 扪、鹼金屬氫氧化物(例如氫氧化納、氯氧化舒)、驗金屬 碳酸鹽(例如碳酸納、碳酸钟、碳酸铯)、鹼金屬醇鹽(例如 甲醇鈉、曱醇鉀、乙醇鈉、乙醇鉀、第三丁醇鉀)或有機 鋰鹼(例如正丁基鋰、第二丁基鋰、第三丁基鋰、二異丙 149026.doc -116- 201103429 胺鋰)。反應一般在合適之溶劑中進行。合適之溶劑為例 如曱笨、Ν-甲基吡咯啶_、醚類(例如二乙醚、四氫呋 喃、二噁烷、1,2-二曱氡基乙烷)、乙腈、Ν,Ν_二曱基甲醯 胺或二曱亞硬。 式I化合物(其中m為〇且R6為-CN)可類似於De_a· 19620407中所述之方法,藉由使化合物工(其中以為〇且…為 H)與化合物CN-W(其中|為良好的脫離基,諸如鹵基(例如 Cl、Br、I))在鹼存在下反應來製備。合適之鹼為例如,鹼 盘屬氫化物(例如氫化鈉、氫化钟)、鹼金屬氫氧化物(例如 氫氧化鈉、氫氧化鉀)、鹼金屬碳酸鹽(例如碳酸鈉、碳酸 鉀、碳酸铯)、鹼金屬醇鹽(例如甲醇鈉、曱醇鉀、乙醇 納乙醇钾第二丁醇卸)或有機裡驗(例如正丁基|里、第 二丁基鋰、第三丁基鋰、二異丙胺鋰)。反應一般在合適 之溶劑中進行。合適之溶劑為例如曱苯、N-甲基吡咯啶 酮、醚類(例如二乙醚、四氫呋喃、二噁烷、丨,2-二曱氧基 乙烷)、乙腈、N,N-二曱基甲醯胺或二甲亞砜。 式1化&物(其中〇1為0且尺6為皿)可類似於1)£_八-196^82 中所述之方法,藉由使化合物1(其中m為0且R6為H)與胺 NR R R (其中Ra、Rb&RC係如上所定義)或與金屬鹽(諸如 氫氧化鈉、氫氧化鉀或乙酸銅)反應來製備。 式I化合物(其中„!為〇且R6為式m之基團)可類似於w〇 97/43269中所述之方法,藉由使化合(其中m為〇且R6為 H)與鹵素(尤其碘)在鹼存在下反應來製備。合適之鹼為例 如,鹼金屬氫化物(例如氫化鈉、氫化鉀)、驗金屬氫氧化 I49026.doc 117 201103429 物(例如虱氧化鈉、氫氧化 鈉、碳酸鉀、碳酸)鹼金屬碳酸鹽(例如碳酸 钟、乙_ )、驗金屬醇鹽(例如甲醇納 '甲醇 鉀、乙西子鈉、乙醇鉀、第三 r ^ - -r ^ ^ — 丁醇鉀)或有機鋰鹼(例如正丁 暴鋰、第—丁基鋰、 如产入、* 、 丁基鐘、二異丙胺鋰)。反應一 身又在δ適之溶劑中推/· . * 仃。5適之溶劑為例如甲苯、Ν-甲基 吡咯啶酮、醚類(例如二 卜 Τ基 ψ m Μ ^ 四虱呋喃、二噁烷、1,2-二 甲氧基乙烷)、乙腈、Ν _ ,T ., . ,—甲基甲醯胺或二.甲亞砜。 式1化&物(其中m為〇曰只6^_乃 'Compounds 5, 6, 8, 9 and 1 which are commercially available for use in the above reactions may be made by standard methods known to those skilled in the art. If the groups R, R2, R3, R4 and R5 in the above reactants are inert to the respective reactions, they may be present in the above reaction step or may be introduced in, for example, the compound IV in the latter stage. A compound of formula 1 wherein R6 is not hydrogen and can be prepared from compound 1 (R6=H and m=〇 in 1). Formula (where m is 〇 and r6 is cr κ. « Its r Γ and R is "3丨-Ci〇alkyl, haloalkyl 2-Cl° dilute, Cc“alkenyl, c2-Cl. Block, c2_c “alkynyl, C3-C丨. Ring-based, c, base ... 3 10 tooth (tetra), phenyl, phenyl like 4 alkyl, the last two of which are mentioned in the group /JU s person J can be replaced as described above, 3 has 1, 2 or 3 The 5- or 6-membered saturated or adjacent gossip of the heterogenes selected from N, 0 and 8 is an unsaturated or aristocratic heterocyclic ring, wherein the heterocyclic ring can be as [si 149026.doc -114- 201103429 The above substituted) can be similar to the method described in DE-A-19520098 or WO 96/41804 by combining (wherein 111 is 〇 and 116 is imprinted with compound R6-LG (wherein R6 has the above meaning) One of the compounds is prepared by reacting a group such as a halogen group (e.g., Cl, Br, I), a sulfonate group or an oxime sulfonate group. Suitable bases are, for example, alkali metal hydrides. (such as sodium hydride, potassium hydride), alkali metal hydroxide (such as hydrogen and oxygen) Sodium, potassium hydroxide), alkali metal carbonates (such as sodium carbonate, potassium carbonate, carbonic acid planing), alkali metal alkoxides (such as sodium methoxide, potassium methoxide, sodium ethoxide, potassium ethoxide, potassium butoxide) or organic Lithium bases (for example, n-butyllithium, t-butyllithium, t-butyllithium, and lithium diisopropylamine are generally reacted in a suitable solvent. Suitable solvents are, for example, toluene, N-methylpyrrolidone, Ethers (eg, diethyl bond, tetrahydroanion, dialdehyde, 12. dimethoxyethane), acetonitrile 'n, n-didecylguanamine or dimethyl sulfoxide. Alternatively, a compound of formula I (where „1 is 0 and the uldent 6 is Ci_Ci〇alkyl, Ci_c-alkyl, c2-ClGalkenyl' C2_CiG halo, C2_Ci❶ block, c2_c i alkynyl, 匚3-(:10 cycloalkyl, C3_Ci 〇 环 、 、, phenyl, phenyl _c c4 alkyl' 苯基 The phenyl moiety in the last two mentioned groups may be substituted as described above, and contains 2 or 3 selected from Ν, 〇 And a hetero atom of 8 as a ring member, a 5 or 6 member saturated, partially unsaturated or aromatic heterocyclic ring wherein the heterocyclic ring may be substituted as described above) may be similar to Heter〇cycles 23(7), 1645_ secret, the method described in 1985, by reacting a compound with a disulfide R6_s_m in the presence of a compound similar to that described in Scheme! (where is a C (=〇) R,c(=s)Ri2) can be classified as 149026.doc -115-201103429. The method described in DE-A-19617461, by compounding ^ (where the claw is 0 and R6 is Η) and the compound ri2_c (=〇)_w, r12_c(=s)_w, Rn,_N=00 or Ri2'_N=c = s (where Rl2 has one of the above meanings, (VC,. An alkyl group or a Ci_ClGM group and is a good leaving group such as a dentate group (e.g., Cl Br, I), an alkoxy group (e.g., a decyloxy group, an ethoxyoxy group) or a pentafluorophenoxy group. The reaction is prepared. Suitable tests are, for example, hydrides (such as sodium hydride, potassium hydride), metal hydroxides (such as sodium hydroxide, potassium hydroxide), alkali metal carbonates such as sodium carbonate, potassium carbonate, and carbonic acid. a metal alkoxide (such as sodium methoxide, methanol _, sodium ethoxide, potassium ethoxide, potassium butoxide) or an organic lithium base (such as n-butyl lithium, second butyl, tert-butyl, and Isopropylamine clock. The reaction is generally carried out in a suitable solvent. Suitable solvents are, for example, toluene, n-methyl sulfonate, and ethers (eg diethyl ether, tetrahydrofuran, dioxane, i, 2-di) Methoxyethane), [nitrile, N,N-didecylguanamine or disulfoxide. The compound of formula 1 (whose towel 1 is 0 and R6 is -so2r12) can be similar to that described in DE_a. By way of example, compound 1 (where m is 0 and R6 is H) and compound R's〇2_w (wherein Rl2 has one of the above meanings and w is a good leaving group, such as a dentate group (eg, a, An oxy group (for example, anthraceneoxy 6 alkoxy) or pentafluorophenoxy) is prepared by reacting in the presence of a test. Metal hydrides (such as sodium hydride, cesium hydride, alkali metal hydroxides (such as sodium hydroxide, chlorinated oxime), metal carbonates (such as sodium carbonate, carbonic acid, barium carbonate), alkali metal alkoxides (such as methanol) Sodium, potassium steroxide, sodium ethoxide, potassium ethoxide, potassium butoxide) or organic lithium base (eg n-butyl lithium, second butyl lithium, tert-butyl lithium, diisopropyl 149026.doc -116- 201103429 Lithium amine). The reaction is generally carried out in a suitable solvent. Suitable solvents are, for example, hydrazine, hydrazine-methylpyrrolidine, ethers (e.g., diethyl ether, tetrahydrofuran, dioxane, 1,2-dioxene). Ethyl ethane), acetonitrile, hydrazine, hydrazine-dimercaptocaramine or diterpene. The compound of formula I (wherein m is hydrazine and R6 is -CN) can be similar to the method described in De_a 19620407, It is prepared by reacting a compound (in which 〇 and ... is H) with a compound CN-W (where | is a good leaving group such as a halogen group (e.g., Cl, Br, I)) in the presence of a base. For example, an alkali disk hydride (such as sodium hydride, hydrogenation clock), an alkali metal hydroxide (such as sodium hydroxide, Potassium oxide), alkali metal carbonates (such as sodium carbonate, potassium carbonate, cesium carbonate), alkali metal alkoxides (such as sodium methoxide, potassium decoxide, potassium ethoxide, second butanol) or organic tests (such as positive Butyl | butyl, lithium butyl lithium, lithium butyl hydride, lithium diisopropyl amide. The reaction is generally carried out in a suitable solvent. Suitable solvents are, for example, toluene, N-methylpyrrolidone, ethers. (e.g., diethyl ether, tetrahydrofuran, dioxane, hydrazine, 2-dimethoxy ethane), acetonitrile, N,N-dimercaptocaramine or dimethyl sulfoxide. 1 is 0 and the rule 6 is a dish) can be similar to the method described in 1) £_8-196^82 by making compound 1 (where m is 0 and R6 is H) and amine NR RR (where Ra, Rb&RC is as defined above) or prepared by reaction with a metal salt such as sodium hydroxide, potassium hydroxide or copper acetate. A compound of formula I (wherein „! is 〇 and R 6 is a group of formula m) can be similar to the method described in w〇97/43269 by combining (where m is 〇 and R6 is H) with halogen (especially Iodine) is prepared by reacting in the presence of a base. Suitable bases are, for example, alkali metal hydrides (e.g., sodium hydride, potassium hydride), metal hydroxides I49026.doc 117 201103429 (e.g., sodium bismuth oxide, sodium hydroxide, carbonic acid) Potassium, carbonic acid) alkali metal carbonate (such as carbonic acid clock, B), metal alkoxide (such as methanol sodium 'potassium methoxide, sodium ethoxide, potassium ethoxide, third r ^ - -r ^ ^ - potassium butoxide) Or an organic lithium base (such as lithium n-butylate, n-butyl lithium, such as yttrium, butyl ketone, lithium diisopropylamine). The reaction is pushed in a solvent of δ. * 仃.5 Suitable solvents are, for example, toluene, hydrazine-methylpyrrolidone, ethers (for example, dipo-indenyl m Μ ^ tetrahydrofuran, dioxane, 1,2-dimethoxyethane), acetonitrile, hydrazine _ , T . , . , --Methylformamide or dimethyl sulfoxide. Formula 1 & (where m is 6 only 6^_ is '

QQ/OS14Q cfa ό 為-P( = Q)Rl3R14)可類似於 WO 99/〇5149中所述之方法來製備。 式Π化合物(其中R 6a A於 6 為虱)可藉由類似於化合物I(Ji中 s 轉化反應使顺“基團(其中h)反應㈣ R不為Η之化合物來製備。 化合物1(其中爪為丨或 -)了藉由氧化反應自各別化合物 1(其中m為0)來製備。赤參 ,,.u 次者’化合物1(其中〇為2)可藉由首 先使三嗤基環去除皙$ # 、 化’豉後與磺醯氣R6S02C1反應自 化。物IV來t備。化合物!(其中爪為3)可藉由首先使三唾 土裒去除質子化’隨後與硫酸氣化物或式之硫酸 醋氣化物(其中R6係選自f、 疋目H、C丨-Cw院基、C广u烷基、 C2-Ci璘基、C2-C“稀基、C2_Ci〇炔基、c2_c』炔基、 C3-Cl^烷基、C3'ClQ齒環烷基、苯基、苯基-Cl-C4烧基, 其中最後2個提及之基團中的苯基部分可如上所述經取 代及a有1 2或3個選自N、〇as之雜原子的5_或6•員飽 和、部分不飽和或芳族雜環,其中雜環可如上所述經取 代)反應自化合物IV來製備。 [S] 149026.doc -118- 201103429 若個別化合物不能經由上述途徑製備,則其可藉由其他 化合物I及II之衍生反應或藉由所述合成途徑之習用修改來 製備。 反應混合物係以習用方式來處理,例如藉由與水混合, 分離各相且適當時’藉由例如於氧化鋁或矽膠上層析來純 化粗產物°可獲得一些呈無色或淡褐色黏性油狀之中間物 及終產物,其不含揮發性組份或在減壓及中等高溫下純化 而不含揮發性組份。若獲得呈固體狀之中間物及終產物, 則其可藉由再結晶或分解來純化。 本發明之另一態樣係關於式IV之化合物:QQ/OS14Q cfa ό is -P(=Q)Rl3R14) can be prepared similarly to the method described in WO 99/〇5149. A hydrazone compound (wherein R 6a A is 6 in hydrazine) can be prepared by a compound similar to the compound I (in the s conversion reaction of Ji, the cis " group (where h) is reacted with (4) R is not ruthenium. The claw is 丨 or -) prepared by oxidation reaction from each compound 1 (where m is 0). Red ginseng, .u second 'Compound 1 (where 〇 is 2) can be made by first making a trimethyl fluorene ring After removing 皙$#, 豉'豉 and reacting with sulfonium gas R6S02C1. Compound IV is prepared. Compound! (where the claw is 3) can be first protonated by removing the salicin from the salicinium. Or a sulphuric acid vinegar vaporized product (wherein R6 is selected from the group consisting of f, hydrazine H, C 丨-Cw, sulphate, C-uu-alkyl, C2-Ci fluorenyl, C2-C "dilute, C2_Ci decynyl, C2_c"alkynyl, C3-Cl^alkyl, C3'ClQ-dental alkyl, phenyl, phenyl-Cl-C4 alkyl, wherein the phenyl moiety in the last two mentioned groups can be as described above Substituted and a having 2 or 3 of a 5 or 6 membered saturated, partially unsaturated or aromatic heterocyclic ring selected from the heteroatoms of N, 〇as, wherein the heterocyclic ring may be substituted as described above) Prepared by IV. [S] 1 49026.doc -118- 201103429 If individual compounds cannot be prepared by the above route, they can be prepared by derivatization of other compounds I and II or by conventional modification of the synthetic route. The reaction mixture is treated in a conventional manner. For example, by mixing with water, separating the phases and, if appropriate, purifying the crude product by chromatography, for example, on alumina or tannin, some intermediates and final products in the form of colorless or light brown viscous oils are obtained. It does not contain volatile components or is purified under reduced pressure and moderately high temperature without volatile components. If intermediates and final products are obtained in solid form, they can be purified by recrystallization or decomposition. Another aspect is related to the compound of formula IV:

其中Het、A、Y、R1、r2、r3&r4具有上述針對化合物 II給出之一般或尤其較佳含義中之一者。 化合物IV—方面為化合物I及II之製備(參見上述流程)中 的有用中間物,而另一方面亦具有顯著的殺真菌活性。 尤佳化合物1V為式IV. 1至IV.48之化合物,其中Het、 R、R2、R3及R4之組合在各情況下對應於上述表A中之一 列。Wherein Het, A, Y, R1, r2, r3 & r4 have one of the general or particularly preferred meanings given above for compound II. Compound IV - aspects are useful intermediates in the preparation of compounds I and II (see the above scheme), and on the other hand have significant fungicidal activity. Particularly preferred compound 1V is a compound of the formulae IV.1 to IV.48, wherein the combination of Het, R, R2, R3 and R4 corresponds in each case to one of the above Table A.

149026.doc •119- 201103429149026.doc •119- 201103429

[SI 149026.doc 120 201103429[SI 149026.doc 120 201103429

在此等化合物中’車交佳為化合物ιν ι至ιν 24,更佳為化 合物IV. 1至IV. 12 ’甚至更佳為化合物IV」及IV 2且尤其較 佳為化合物IV.2。 本發明進一步係關於一種農業組合物,其包含至少一種 如上所定義之式I、^及/或^之化合物或其農業上可接受 149026.doc •121- 201103429 之鹽及液體或固體載劑。亦可包含於本發明組合物中的合 適載劑以及助劑及其他活性化合物係如下定義。 化合物I及II以及IV及本發明組合物分別適用作殺真菌 劑。其特點為顯著有效對抗廣譜植物致病真菌,包括土壞 傳播真菌,尤其來源於以下類別纟:根腫菌綱 (PlaSm〇di〇Ph〇r〇myCetes)、卵菌綱(per〇n〇sp〇r〇mycetes, 〇〇mycetse)、壺 g 綱(Chytridi〇mycetes)、接合菌綱 (zyg〇mycetes)、子囊菌綱(Asc〇mycetes)、擔子菌綱 (Basidiomycetes)及半知菌綱(Deuter〇myce㈣⑺義詞不 完全菌綱(Fungi imperfecti))。其中一些係全身有效的且其 可作為葉面殺真菌劑、拌種殺真菌劑及土壤殺真菌劑用於 作物保護中。此外,其適用於防治有害真菌,尤其出現於 木材或植物根部之真菌。 化合物卜Π及…及本發明組合物在防治以下大量植物$ 病真菌中尤其重要:各種栽培植物上之真菌,諸如榖類 例如,小麥、裸麥、大麥、黑小麥、燕麥或稻穀;甜菜, 例如’糖用甜菜或飼用甜菜;水果,諸如仁果、核果或· 果(soft fruit),❹,韻果、梨 '李子、桃、杏仁、相 桃”、黑每或醋栗;豆科植物,諸如小扁豆、 豌丑、苜#或大ΐ ;油料作物,諸如油菜、齐末、撤檀、 :曰蔡、椰子、可可豆、莲麻、油棕、落花生或大豆;光 诸如南瓜、胡瓜或甜瓜;纖維植物,諸如棉花、亞 大麻或黃麻;柑㈣水果,諸如料、擰檬、葡萄柏 或柑’蔬菜,_菜、葛[董筒、甘藍菜、胡蘿葡、 [S] M9026.doc •122- 201103429 洋蔥、番茄、馬鈴薯、瓜齙十 别_ a 瓜頰或辣椒;月桂科植物’諸如鱷 梨 菜 蕉 皮 木 , ·一 ·, ,《«_ ·〜 5¾ 戈〇 肉㈣樟腦;能量及原料植物,諸如玉米、大豆、油 甘蔗或油棕;玉米;菸草;堅果;咖啡;苓葉香 藤本植物(鮮食葡萄及葡萄汁葡萄藤);蛇麻;;’ 天然橡膠植物或觀賞植物及林業植物,諸如花、灌 闊葉樹或常綠樹’例如針葉樹;及植物繁殖材料上之 真菌’諸如種子’及此等植物之作物材料。 較佳地,化合物卜11及1乂及其組合物分別用於防治以下 各物上的大量真菌:田間作 ”勿_如馬鈴薯、糖用甜菜、 於草、小麥、裸麥、大麥、燕麥、稻穀、玉米、棉花、大 丑、油菜、豆類、向曰葵、咖啡或甘蔗;水果;藤本棺 物;觀賞植物;或蔬菜,諸如胡, 乃瓜奄加、立或南瓜。 應瞭解術語「植物繁殖姑祖主_ 繁殖材料」表不可用於繁殖植物的所 有植物生純料,諸如料,及營養性㈣材料,諸如 插條及塊莖(例如馬鈴薯)。此包括種子、根、果音、 莖、«、根莖、枝、幼枝及植物之其他部分,包括2 :秧田’其係在萌芽之後或在露出土壤之後被移植。亦可 秩:植之前藉由浸潰或傾注之全部或部分處理來保護此等 較佳地’分別以化合物卜咖及其組合物處理 殖材料係用於防治以下各物上之 I, 里具菌.殺類,諸如小 麥稞麥、大麥及燕麥;稻穀、玉米、棉花及大豆。 術語「栽培植物」應理解為包括 或遺傳工程設計經修飾之植物,包括心二);: = 149026.doc -123· 201103429 發中之農業生物技術產品(參考:http://www.bio.org/speeches/pubs/ er/agri_products.asp)。經遺傳修飾之植物為如下植物,其遺傳 物質已藉由使用重組DNA技術而修飾,該種修飾在天然情 況下不易藉由雜交育種、突變或天然重組獲得。通常,已 將一或多種基因整合至經遺傳修飾植物的遺傳物質中以改 良植物之某些性質。該等遺傳修飾亦包括(但不限於)例如 藉由糖基化或聚合物添加(諸如異戊二烯化(prenylated)、 乙醯化或法呢基化(farnesylated)部分或PEG部分)進行蛋白 質、寡肽或多肽之轉譯後靶向修飾。In these compounds, the compound is preferably a compound ιν ι to ιν 24, more preferably a compound IV. 1 to IV. 12 ‘ even more preferably a compound IV” and IV 2 and particularly preferably a compound IV.2. The invention further relates to an agricultural composition comprising at least one compound of formula I, ^ and/or ^ as defined above, or a salt thereof and a liquid or solid carrier of agriculturally acceptable 149026.doc • 121-201103429. Suitable carriers and auxiliaries and other active compounds which may also be included in the compositions of the invention are as defined below. The compounds I and II and IV and the compositions of the invention are each suitable as a fungicide. It is characterized by significant effectiveness against a wide range of phytopathogenic fungi, including soil-borne fungi, especially from the following categories: Plasm〇di〇Ph〇r〇myCetes, Oomycetes (per〇n〇) Sp〇r〇mycetes, 〇〇mycetse), Chytridi〇mycetes, zyg〇mycetes, Asc〇mycetes, Basidiomycetes, and Deuteromycetes Deuter〇myce (4) (7) The term "Fungi imperfecti". Some of them are systemically effective and can be used as crop fungicides, seed dressing fungicides and soil fungicides for crop protection. In addition, it is suitable for controlling harmful fungi, especially fungi that occur in the roots of wood or plants. The compounds and the compositions of the present invention are particularly important in controlling a large number of plant-derived fungi: fungi on various cultivated plants, such as alfalfa such as wheat, rye, barley, triticale, oats or rice; beets, For example 'sugar beet or beet; fruit, such as pome fruit, stone fruit or soft fruit, ❹, rhyme, pear 'plum, peach, almond, phase peach', black per vine or gooseberry; legume Plants, such as lentils, peas, cockroaches, or cockroaches; oil crops, such as rapeseed, glutinous rice, black sandalwood, 曰Cai, coconut, cocoa, lotus, oil palm, groundnut or soybean; light such as pumpkin, Cucumber or melon; fiber plant, such as cotton, sub-hemp or jute; mandarin (four) fruit, such as material, lemon, grape cypress or mandarin 'vegetables, _ vegetables, geese [dong tube, kale, carrot, [S M9026.doc •122- 201103429 Onion, tomato, potato, melon 龅 _ a melon cheek or pepper; laurel plant 'such as avocado vegetable banana wood, · a ·, , «_ · ~ 53⁄4 戈〇肉(4) camphor; energy and raw materials such as jade , soybean, oil cane or oil palm; corn; tobacco; nuts; coffee; eucalyptus vines (fresh grapes and grape vines); hops;; 'natural rubber plants or ornamental plants and forestry plants, such as flowers, Perfusing broadleaf trees or evergreen trees such as conifers; and fungi such as seeds on plant propagation materials and crop materials of such plants. Preferably, the compounds 11 and 1 and their compositions are used to control the following A large number of fungi on the field: field work "Do not _ such as potatoes, sugar beets, grass, wheat, rye, barley, oats, rice, corn, cotton, big ugly, rape, beans, geranium, coffee or sugar cane; Fruit; vines; ornamental plants; or vegetables, such as hu, melon, garnish, or pumpkin. It should be understood that the term "plant breeding ancestor _ reproductive material" table may not be used to propagate all plant pure materials, such as materials, and nutritive (four) materials, such as cuttings and tubers (such as potatoes). This includes seeds, roots, fruit notes, stems, «, rhizomes, branches, young shoots and other parts of the plant, including 2: Putian' which is transplanted after germination or after exposure to the soil. It can also be used to protect these preferably by using the compound or the composition of the composition, and to treat the following materials, respectively, by means of all or part of the treatment by dipping or pouring. Bacteria, such as wheat buckwheat, barley and oats; rice, corn, cotton and soybeans. The term "cultivated plants" is to be understood to include or genetically engineered modified plants, including the heart);: = 149026.doc -123· 201103429 Agricultural biotechnology products in the market (Reference: http://www.bio. Org/speeches/pubs/ er/agri_products.asp). Genetically modified plants are plants whose genetic material has been modified by the use of recombinant DNA techniques which, in the natural case, are not readily obtainable by cross breeding, mutation or natural recombination. Typically, one or more genes have been integrated into the genetic material of a genetically modified plant to improve certain properties of the plant. Such genetic modifications also include, but are not limited to, proteins by, for example, glycosylation or polymer addition (such as prenylated, acetylated or farnesylated moieties or PEG moieties). Post-translational modification of the oligopeptide or polypeptide.

已藉由育種、突變誘發或遺傳工程設計經修飾之植物由 於習知育種或遺傳工程設計方法(例如)對特定類別除草劑 之施用產生耐受性,諸如羥苯基丙酮酸二加氧酶(HPPD)抑 制劑;乙醯乳酸合成酶(ALS)抑制劑,諸如磺醯脲(例如參 見 US 6,222,100、WO 01/82685、WO 00/26390、WO 97/41218、WO 98/02526、WO 98/02527、WO 04/106529、WO 05/20673、WO 03/14357、WO 03/13225、WO 03/14356、WO 04/16073)或咪唑啉酮(例如參見US 6,222,100、WOPlants that have been modified by breeding, mutation induction or genetic engineering are resistant to the application of specific classes of herbicides, such as hydroxyphenylpyruvate dioxygenase, by conventional breeding or genetic engineering methods (for example). Inhibitor of acetaminophen lactic acid synthase (ALS), such as sulfonium urea (see, for example, US 6,222,100, WO 01/82685, WO 00/26390, WO 97/41218, WO 98/02526, WO 98 /02527, WO 04/106529, WO 05/20673, WO 03/14357, WO 03/13225, WO 03/14356, WO 04/16073) or imidazolinones (see for example US 6,222,100, WO)

01/82685、WO 00/026390、WO 97/41218、WO 98/002526、WO01/82685, WO 00/026390, WO 97/41218, WO 98/002526, WO

98/02527、WO 04/106529 ' WO 05/20673、WO 03/014357、WO 03/13225、WO 03/14356、WO 04/16073);烯醇丙酮醯莽草 酸-3-磷酸合成酶(EPSPS)抑制劑,諸如嘉磷塞 (glyphosate)(例如參見WO 92/00377);麵酿胺酸合成酶 (GS)抑制劑,諸如固殺草(glufosinate)(例如參見EP-A 242 236、EP-A 242 246)或碘苯腈(oxynil)除草劑(例如參見US98/02527, WO 04/106529 'WO 05/20673, WO 03/014357, WO 03/13225, WO 03/14356, WO 04/16073); enol acetone oxalic acid-3-phosphate synthase (EPSPS) Inhibitors, such as glyphosate (see, for example, WO 92/00377); flavonoid synthase (GS) inhibitors, such as glufosinate (see, for example, EP-A 242 236, EP-A) 242 246) or oxynil herbicides (see for example US

[SI 149026.doc -124- 201103429 5,559,024)。習知育種方法(突變誘發)已使若干栽培植物耐 受除草劑,例如Clearfield®夏季油菜(Canola,BASF SE, Germany)對ϋ米。坐琳酮(例如曱氧σ米草於(imazamox))具財受 性。已使用遺傳工程設計方法使栽培植物(諸如大豆、棉 花、玉米、甜菜及油菜)耐受除草劑(諸如嘉磷塞及固殺 草),其中一些植物以商標名RoundupReady®(财受嘉填 塞,Monsanto, U.S.A.)及 LibertyLink®(而才受固殺草,Bayer CropScience,Germany)市售。 此外,亦包括藉由使用重組DNA技術而能夠合成一或多 種殺昆蟲蛋白之植物,尤其為彼等來自細菌桿菌屬(genus 5i?cz7/ws), 特別來自蘇雲金芽孢桿菌 i/zwr/wg/e似b)之蛋白,諸如δ-内毒素,例如,CrylA(b)、 CrylA(c)、CrylF、CryIF(a2)、CryIIA(b)、CrylllA、CrylllB(bl) 或Cry9c ;營養期殺昆蟲蛋白(VIP),例如VIP1、VIP2、 VIP3或VIP3A ;定殖線蟲之細菌(例如發光桿菌屬 (jP/zoior/zaZjc/ws spp·)或嗜線蟲致病桿菌屬 spp.))之殺昆蟲蛋白;由動物產生之毒素,諸如蛾毒素、 虫知蛛毒素、黃蜂毒素或其他昆蟲特異性神經毒素;由真菌 產生之毒素,諸如鍵徽菌毒素、植物凝集素,諸如婉豆或 大麥凝集素;凝集素;蛋白酶抑制劑,諸如胰蛋白酶抑制 劑、絲胺酸蛋白酶抑制劑、塊莖儲藏蛋白(patatin)抑制 劑、半胱胺酸蛋白酶抑制劑或木瓜蛋白酶抑制劑;核糖 體-失活蛋白(RIP),諸如蓖麻毒素、玉蜀黍-RIP、相思子 素、絲瓜籽毒蛋白、沙泊寧(saporin)或異株腹瀉毒蛋白 149026.doc -125 - 201103429 諸如3-羥基類固醇氧化酶、脫 、膽固醇氧化酶、蛻皮激素抑 離子通道阻斷劑’諸如鈉通道 (bryodin);類固醇代謝酶, 皮類固醇-IDP-牆基轉移酶 制劑或HMG-C〇A-還原酶; 或鈣通道阻斷劑;保幼激素酯酶;利尿激素受體(異株瀉 根毒蛋白受體);K合成酶、聯苯曱基合成酶、殼多糖酶 (chitinase)或葡聚糖酶。在本發明之上下文中亦應明確 地將此等殺昆蟲蛋白或毒素理解為前毒素、雜交蛋白截 短或另外經修飾之蛋白 雜交蛋白之特徵為蛋白質結構域 之新穎組合(例如參見W0 〇2/〇157〇1)。該等毒素或能夠合 成該等毒素之經遺傳修飾之植物的其他實例係揭示於例如 EP-A 374 753 、 WO 93/007278、WO 95/34656、EP-A 427 529、EP-A 451 878、WO 03/18810及 WO 03/52073 中。用 於產生該等經遺傳修飾植物之方法一般為熟習此項技術者 所知且描述於例如上述公開案中。包含於經遺傳修飾之植 物中的此等殺昆蟲蛋白使得產生此等蛋白之植物耐受來自 以下之有害害蟲:所有節肢動物分類群,尤其甲蟲(鞘翅 目(Coleoptera))、兩翼昆蟲(雙翅目(Diptera))及蛾(鱗翅目 (Lepidoptera)),及線蟲(線蟲綱(Nemat〇da))。能夠合成一 或多種殺昆蟲蛋白的經遺傳修飾之植物係例如描述於上述 公開案中’且可購得其中一些:諸如YieldGard®(產生 CrylAb毋素之玉米栽培品種)、YieidGard® Plus(產生[SI 149026.doc -124- 201103429 5,559,024). Conventional breeding methods (mutation induced) have rendered several cultivated plants resistant to herbicides such as Clearfield® Summer Canola (Canola, BASF SE, Germany) to glutinous rice. Selenone (for example, 曱 σ σ 于 于 (imazamox)) is financially acceptable. Genetically engineered methods have been used to render cultivated plants (such as soybeans, cotton, corn, sugar beets, and canola) tolerant to herbicides (such as galaxin and chlorpyrifos), some of which are under the trade name RoundupReady®. Monsanto, USA) and LibertyLink® (commercially available, Bayer CropScience, Germany) are commercially available. Also included are plants capable of synthesizing one or more insecticidal proteins by using recombinant DNA techniques, especially from the genus Bacillus (genus 5i?cz7/ws), especially from Bacillus thuringiensis i/zwr/wg/ e) protein such as δ-endotoxin, for example, CrylA(b), CrylA(c), CrylF, CryIF(a2), CryIIA(b), CrylllA, CrylllB(bl) or Cry9c; vegetative insecticide Protein (VIP), such as VIP1, VIP2, VIP3 or VIP3A; insecticidal proteins of colonizing nematode bacteria (eg, Photobacterium (jP/zoior/zaZjc/ws spp.) or Nematophagous sp.) a toxin produced by an animal, such as a moth toxin, a spider toxin, a wasptoxin or other insect-specific neurotoxin; a toxin produced by a fungus, such as a toxin, a plant lectin, such as cowpea or barley agglutinin; Lectin; protease inhibitors such as trypsin inhibitors, serine protease inhibitors, patatin inhibitors, cysteine protease inhibitors or papain inhibitors; ribosome-inactivated proteins (RIP) ), such as ricin Yuxi-RIP, acacia, loofahin, saporin or diarrhea toxic protein 149026.doc -125 - 201103429 such as 3-hydroxysteroid oxidase, deoxygenase, cholesterol oxidase, ecdysone inhibitor Channel blocker 'such as sodium channel (bryodin); steroid metabolism enzyme, dermal steroid-IDP-wall transferase preparation or HMG-C〇A-reductase; or calcium channel blocker; juvenile hormone esterase; diuretic Hormone receptor (heterologous genus protein receptor); K synthase, biphenyl thiol synthase, chitinase or glucanase. It is also expressly understood in the context of the present invention that such insecticidal proteins or toxins are understood to be protoxins, hybrid protein truncations or otherwise modified protein hybrid proteins characterized by novel combinations of protein domains (see, for example, W0 〇 2 /〇157〇1). Other examples of such toxins or genetically modified plants capable of synthesizing such toxins are disclosed, for example, in EP-A 374 753, WO 93/007278, WO 95/34656, EP-A 427 529, EP-A 451 878, WO 03/18810 and WO 03/52073. Methods for producing such genetically modified plants are generally known to those skilled in the art and are described, for example, in the above publication. Such insecticidal proteins contained in genetically modified plants allow plants producing such proteins to tolerate harmful pests from all: arthropod taxa, especially beetles (Coleoptera), two-winged insects (double wings) Diptera) and moths (Lepidoptera), and nematodes (Nemat〇da). Genetically modified plant lines capable of synthesizing one or more insecticidal proteins are described, for example, in the above publications' and some of them are commercially available: such as YieldGard® (a corn cultivar producing CrylAbsulin), YiiedGard® Plus (produced)

CrylAb及Cry3Bbl毒素之玉米栽培品種)、Starlink®(產生 Cry9c毋素之玉米栽培品種)、Herculex® RW(產生 0^34八131、(:735入1)1及酶膦||麻鹼_:^_乙醯基轉移酶[?八1:] [S1 149026.doc -126- 201103429 之玉米栽培品種);NuCOTN® 33B(產生CrylAc毒素之棉花 栽培品種)、Bollgard® 1(產生CrylAc毒素之棉花栽培品 種)、Bollgard® 11(產生CrylAc及Cry2Ab2毒素之棉花栽培 品種);VIPCOT®(產生VIP-毒素之棉花栽培品種); NewLeaf®(產生Cry3 A毒素之馬鈴薯栽培品種);Bt-Xtra®、 NatureGard®、KnockOut®、BiteGard®、Protecta®、自 Syngenta Seeds SAS, France 購得之 Btll(例如,Agrisure® CB)及 Btl 76(產生Cry lAb毒素及PAT酶之玉米栽培品種)、自 Syngenta Seeds SAS,France購得之MIR604(產生經修飾形 式之Cry3 A毒素的玉米栽培品種,參考WO 03/018810)、自 Monsanto Europe S.A·, Belgium 購得之 MON 863(產生 Cry3Bbl毒素之玉米栽培品種)、自Monsanto Europe S.A., Belgium賭得之IPC 53 1(產生經修飾形式之CrylAc毒素的 棉花栽培品種)及自 Pioneer Overseas Corporation, Belgium 購得之1507(產生CrylF毒素及PAT酶之玉米栽培品種)。 此外,亦包括藉由使用重組DNA技術而能夠合成一或多 種增加彼等植物對細菌、病毒或真菌病原體之抗性.或耐受 性之蛋白質的植物。該等蛋白質之實例為所謂的「致病相 關蛋白(pathogenesis-related protein)」(PR蛋白,例如參見 EP-A 392 225)、植物抗病基因(例如,馬鈐薯栽培品種, 其表現用以對抗源自墨西哥野生馬鈴薯二倍體品種 {Solarium iawww)之馬鈐薯疫病菌的抗性基因)或 T4-溶菌酶(例如,能夠合成此等蛋白質之馬鈴薯栽培品 種,其對諸如梨火傷_病菌(五rwzWa izm_y/vora)之細菌抗性增 149026.doc -127- 201103429 加)。製造該等經遺傳修飾之植物的方法一般為熟習此項 技術者所知且例如描述於上述公開案中。 此外,亦包括藉由使用重組DNA技術而能夠合成一或多 種蛋白質之植物,該等蛋白質提高生產力(例如,生物質 量產生、榖粒產量、澱粉含量、油含量或蛋白質含量)、 耐旱性、耐鹽性或對其他生長限制性環境因素的耐受性或 對害蟲及彼等植物之真菌、細菌或病毒病原體之耐受性。 此外,為了特定地改善人類或動物營養狀況,亦包括藉 由使用重組DNA技術而含有變化量之内含物質或新穎内含 物質的植物,例如,產生促進健康之長鏈ω_3脂肪酸或不 飽和ω-9脂肪酸之油料作物(例如,Nexera®油菜,Corn cultivar of CrylAb and Cry3Bbl toxin), Starlink® (Cry cultivar producing Cry9c glutinin), Herculex® RW (production of 0^34 八131, (:735 into 1)1 and enzyme phosphine||麻碱_: ^_Acetyltransferase [?8:] [S1 149026.doc -126-201103429 corn cultivar); NuCOTN® 33B (cotton cultivar producing CrylAc toxin), Bollgard® 1 (cotton producing CrylAc toxin) Cultivars), Bollgard® 11 (cotton cultivar producing CrylAc and Cry2Ab2 toxins); VIPCOT® (cotton cultivar producing VIP-toxin); NewLeaf® (potato cultivar producing Cry3 A toxin); Bt-Xtra®, NatureGard®, KnockOut®, BiteGard®, Protecta®, Btll available from Syngenta Seeds SAS, France (eg Agrisure® CB) and Btl 76 (corn cultivar producing Cry lAb toxin and PAT enzyme), from Syngenta Seeds SAS MIR604 (a corn cultivar producing a modified form of Cry3 A toxin, see WO 03/018810), MON 863 (a corn cultivar producing Cry3Bbl toxin) purchased from Monsanto Europe SA·, Belgium, Mo Nsanto Europe S.A., Belgium's IPC 53 1 (cotton cultivar producing a modified form of CrylAc toxin) and 1507 (a corn cultivar producing CrylF toxin and PAT enzyme) purchased from Pioneer Overseas Corporation, Belgium. Also included are plants which are capable of synthesizing one or more proteins which increase the resistance or tolerance of their plants to bacterial, viral or fungal pathogens by using recombinant DNA techniques. Examples of such proteins are the so-called "pathogenesis-related proteins" (PR proteins, see for example EP-A 392 225), plant resistance genes (for example, horse yam cultivars, which are used for Against a resistance gene derived from the potato Phytophthora infestans from the Mexican wild potato diploid variety {Solarium iawww) or T4-lysozyme (for example, a potato cultivar capable of synthesizing such proteins, such as pear fire injury _ pathogens (Five rwzWa izm_y/vora) bacterial resistance increased 149026.doc -127- 201103429 plus). Methods of making such genetically modified plants are generally known to those skilled in the art and are described, for example, in the above publication. Also included are plants capable of synthesizing one or more proteins by using recombinant DNA techniques that increase productivity (eg, biomass production, grain yield, starch content, oil content or protein content), drought tolerance, Salt tolerance or tolerance to other growth limiting environmental factors or to fungi, bacterial or viral pathogens of pests and their plants. In addition, in order to specifically improve the nutritional status of humans or animals, plants comprising varying amounts of inclusions or novel inclusions by using recombinant DNA techniques, for example, to produce healthy long-chain ω-3 fatty acids or unsaturated ω -9 fatty acid oil crops (eg, Nexera® canola,

Agro Sciences, Canada) ° 此外,為了特定地改良原料生產,亦包括藉由使用重組 DNA技術而含有變化量之内含物質或新穎内含物質之植 物,例如,產生增加量之支鏈澱粉的馬鈐薯(例如, AmHora 馬龄著 ’ BASF SE, Germany)。 化合物I、II及IV及其組合物分別尤其適用於防治下列植 物病: 白鏽病菌屬〇4/6叹〇 spp.)(白鏽病):於觀賞植物、趙菜 (例如,油菜白鏽病菌(A 心))及向曰葵(例如,婆羅 門白鏽病菌(儿上;交鏈孢菌屬⑺ spp.)(黑斑病(Alternaria leaf spot)):於蔬菜 '油菜(芸公交 鍵孢菌(儿或、糖用甜菜(細交鍵抱菌 (A· tenuis))、水果、稻縠、大豆、馬铃薯(例如,馬鈐薯交 I49026.doc -128- 201103429 鏈孢菌(儿w/am·)或互格交鏈孢菌(丄番茄(例 如,馬鈴薯交鏈孢菌或互格交鏈孢菌)及小麥上;糖用甜 菜及&菜上之根腐病菌屬spp_);榖類及蔬 菜上之輪紋病菌屬spp.),例如,小麥上之小麥 輪紋病菌〇4·炭疽病)及大麥上之大麥輪紋病菌仏 hordei) ’平臍蠕抱屬(Bip〇laris 5沖)反杓臍緯抱屬 spp.)(有性態:旋孢腔菌屬(C〇CW〇h/Mi spp.)),例如,玉米上之南方葉枯病(玉蜀黍長蠕孢 所叮山\〇)或北方葉枯病(玉米生平臍蠕孢(及,例 如’穀類上之斑點病(小麥根腐平臍蠕孢(5 ㈡) 及例如稻穀及草皮上之稻平臍螺孢(及or^yzae);縠類上(例 如小麥或大麥上)之白粉病菌(5/wweWa grawn.wbK先前稱 為五〇^>心白粉病);水果及漿果(例如,草 莓)、蔬菜(例如,萵苣、胡蘿蔔、芹菜及甘藍菜)、油菜、 花、藤本植物、林業植物及小麥上之灰葡萄孢⑺心 Wea)(有性態:灰黴病菌(…外⑽_ /wc知⑹⑽):灰 M),萵苣上之萵苣露菌病(5re/wz.a Mciwc<2e)(霜黴病);闊 葉樹及常綠樹上之長喙殼屬spp )(同義詞長 喙黴屬spp.))(腐爛或枯萎),例如榆樹上之榆 長喙殼菌(C. w/mi)(荷蘭榆樹病);葉斑病菌屬(Cerc〇5p〇rfl spp_)(葉斑病):於玉米(例如,灰色葉斑病:玉米灰斑病菌 (C 、稻縠、糖用甜菜(例如,甜菜褐斑病菌 (C. Z>e〇C〇/i7))、甘蔗、蔬菜、咖啡、大豆(例如,大豆灰斑 病菌(C Μϋα)或大豆紫斑病菌(c 及稻榖上;黑 149026.doc •129· 201103429 變病菌屬spp.):於番茄(例如,葉黑變病菌 (C. /Wvwm) •葉摄病)及穀類上’例如小麥上之麥類專變病 菌(C. /zdarMm)(黑穗病);榖類上之黑麥角菌(c/aWce^ pwrpwr扣)(麥角症);旋孢腔菌屬(Coc/z/z〇Z)〇h^ spp.)(無性 態·平膽螺抱屬之長螺抱葉斑病): 於玉米(玉米旋孢腔菌(c. carhwMm))、縠類(例如,禾旋孢 腔菌(C. Μί/νΜ·?),無性態:麥根腐平臍緯抱菌(凡 sorokiniana))及稻穀(例如,宮部旋孢腔菌(c ⑽’無性態··水稻長蠕孢菌(// 乃上;刺 盤孢屬(Co//eioir/c/2wm spp.)(有性態:炭疽病菌屬 (G/omerWa Spp_))(炭疽病):於棉花(例如,棉刺盤孢(c g〇以;/户⑺)、玉米(例如’禾刺盤孢(c •⑴·c〇/a):炭疽 莖腐病)、軟果、馬鈴薯(例如,果腐刺盤孢(c. coccoi/e·?).黑斑病)、豆(例如,菜豆刺盤孢(c. /MAmwi/n·⑽謂))及大豆(例如,平頭刺盤孢(c ⑽請) 或膠孢炭疽病菌(C. g/oeosporioic/e·?))上;伏革菌屬 spp.) ’例如,稻穀上之紋枯病菌(c μ扣仏·)(紋 枯病);大豆及觀賞植物上之山扁豆生棒孢菌(c〇AT„eip〇ra Cai^7c〇/a)(葉斑病);環錐孢菌屬(Cycl〇c〇nium spp.),例 如’油撤禮樹上之油撤欖環錐抱菌(C. ο/eag/WMW);柱抱菌 屬(C_y"«办οαν⑽spp.)(例如,果樹癌腫病或藤本植物秧 衰敗(young vine decline),有性態:叢赤殼菌屬(Arecirk SPP.)或新叢赤殼菌屬(iVeoweciWa spp.)):於果樹、藤本植 物(例如,鶴掌揪柱抱菌(C. ,有性態:鶴掌揪 149026.doc •130- 201103429 新叢赤殼菌(A/ecmec/rz.a /z>z’oc^«drz’):黑腳病)及觀賞植物 上’大豆上之褐束絲菌(£)e讲邮⑺⑺、)(有性態: 褐堅座殼菌(iJoje/hWa/ecaWx))(根腐病及莖腐病);間座 威菌屬(D/apori/ze spp_),例如,大豆上之菜豆間座殼菌 (D· phieo/or請)(猝倒病广内臍蠕孢屬「同義詞長蠕孢 屬'有性態:核腔菌..於玉米、榖類,諸 如大麥(例如,圓内臍螺抱菌(/) ierei),網斑病)及小麥(例 如’兴斑小麥内腾螺抱菌(£)·卜⑴c卜span’s,褐斑病))、 稻榖及草皮上;藤本植物上之EsCa(頂枯病,乾枯病),由 斑點礼蛰{Formitiporia punctata,Phellinus punctata")、地 中海孔菌(F. 、垣孢伐莫尼亞菌 (户/2邮〇所〇則>//<3 c/z/awydosporaK早期之厚垣褐枝頂抱 (Phaeoacremonium chlamydosporum))、寄生瓶黴菌 (P/zfleoflcr㈣omwm fl/eop/n’/ww)及/或圓頭葡萄座腔菌 (Botryosphaeria obtusa)所弓丨起·,痂囊腔 M 屬(Ehin〇e SPP.).於仁果(梨病囊腔菌(五.p;;rz·))、軟果(懸鈴木痂囊腔 菌(£. veneia):炭疽病)及藤本植物(葡萄痂囊腔菌 ampe/ina):炭疽病)上·,稻縠上之稻葉黑腫病菌(心如〇咖 〇〇^e)(葉黑穗病);小麥上黑附球菌屬(五〆c〇cc_ SPP.)(黑彳放病)’白粉病菌屬(五spp.)(白粉病):於糖 用甜菜(甜菜白粉病菌(£. Z^iae))、蔬菜(例如,豌豆白粉病 菌(£_ pw))、諸如瓜類(例如,二抱白粉病菌(五 cic/zoraceawm))、甘藍菜 '油菜(例如,十字花白粉病菌 (£· cr«c如rarim))上·,於果樹、藤本植物及觀賞植物樹木 149026.doc • 131 · 201103429 上之多彎孢殼菌(五葡萄癌腫病或頂枯病,無性 態:多殼囊孢菌/αία)(同義詞百筋花盤針孢菌 (Lz·心rie/M 6/ep;2arb)));於玉米(例如,大斑突臍罐抱菌 (£· iwrchm))上之突臍孢菌屬(ExSerohilum spp,同義詞 長螺抱屬);各種植物上之鐮孢菌屬(7^似aWww spp )(有性 態:赤黴菌屬sPP.))(凋萎病、根腐病或莖腐 病),諸如毅類(例如小麥或大麥)上之禾穀鐮孢菌(f graminearum)氙夤色镰孢^(F. Culmorum^根腐病、瘡恭病 或赤黴病(head blight))、番茄上之錘形鐮孢菌π oxj^porwm)、大豆上之茄鐮孢菌(尺⑴.)及玉米上之輪枝 鐮孢菌(厂verAz7/ioWej) /榖類(例如小麥或大麥)及玉米 上之禾頂囊殼菌(Gaewwa/mo所少cei 全钮病),.赤 黴菌屬spp·):於榖類(例如玉米根腐赤黴菌 zew))及稻穀(例如藤倉赤黴菌(G. /wy^wroz·):惡苗病)上,. 藤本植物、仁果及其他植物上之炭疽病菌(G/〇則π — 及棉化上之棉炭症病菌(G· g〇|Si^pZ’z’),.稻穀上之 格蘭染色複合物(Grainstaining complex);藤本植物上之葡 萄球座菌出〇(黑腐病),.薔薇科植物及刺 柏上之膠鑛菌屬spp.),例如梨上之薩 賓膠鏽菌(G. (鏽病),·玉米、縠類及稻縠上之長蠕 抱屬(同義詞内臍蠕孢’有性態:旋孢腔菌),.鏽菌屬 (//ewi/em spp.),例如咖啡上之駝孢鏽菌(开請 咖啡葉鏽病),.藤本植物上之葡萄褐斑病菌 (/庸_A c/aW印ora)(同義詞葡萄黑變病菌(cw〇v〇rz.謂 149026.doc •132- 201103429Agro Sciences, Canada) ° In addition, in order to specifically improve the production of raw materials, plants containing varying amounts of inclusions or novel inclusions by using recombinant DNA techniques, for example, horses producing increased amounts of amylopectin Sweet potato (for example, AmHora is at the age of 'BASF SE, Germany). Compounds I, II and IV and their compositions are especially suitable for controlling the following plant diseases: White rust pathogen 〇 4/6 sigh spp.) (white rust): in ornamental plants, Zhao dishes (for example, rape white rust pathogens) (A heart)) and hollyhock (for example, Brahman white rust (Children; Alternaria spp.) (Alternaria leaf spot): in the vegetable 'Rapeseed (Children, sugar beet (A. tenuis), fruit, rice bran, soybean, potato (for example, horse yam, I49026.doc -128- 201103429) /am·) or Alternaria alternata (丄 tomato (for example, Alternaria alternata or Alternaria alternata) and wheat; sugar beet and & root rot pathogen spp_); The genus Spirulina spp.) on moss and vegetables, for example, wheat ring rot fungus 小麦 4 · anthracnose on wheat and barley rot hordei on barley) 'Bip〇laris 5 rush) ruminant umbilical genus spp.) (has a sexual state: C. cerevisiae (C〇CW〇h/Mi spp.)), for example, southern leaf blight on corn (maize long creep (叮山〇) or northern leaf blight (corner umbilical larvae of corn) (and, for example, 'spot disease on cereals (wheat root rot (5)) and rice snails on rice and turf Spores (and or^yzae); powdery mildew on alfalfa (such as wheat or barley) (5/wweWa grawn.wbK formerly known as Wuzhi^>xin powdery mildew); fruits and berries (eg, strawberries), Vegetables (eg, lettuce, carrots, celery and kale), rapeseed, flowers, vines, forestry plants and Botrytis cinerea on wheat (7) Heart Wea) (have a state: Botrytis cinerea (...) (10)_ /wc know (6)(10) ): Gray M), lettuce oncuce on lettuce (5re/wz.a Mciwc < 2e) (downy mildew); broad-leaved tree and evergreen tree genus spp) (synonym long genus spp. )) (rot or wither), such as C. w/mi on the eucalyptus (Dutch eucalyptus); Cerc〇5p〇rfl spp_ (leaf leaf spot): in corn (eg, gray leaf spot: gray leaf spot (C, rice bran, sugar beet (eg, beet brown spot (C. Z> e〇C〇/i7)), sugar cane, Vegetables, coffee, soybeans (for example, Phytophthora sojae (C Μϋα) or Phytophthora sojae (c and rice blast; black 149026.doc • 129· 201103429 genus spp.): in tomato (for example, leaf blackening) Pathogens (C. / Wvwm) • Leaf disease) and cereals such as wheat-specific wheat (C. / zdarMm) (smut); ryegrass on clams (c/aWce^ Pwrpwr () ergot); genus genus (Coc/z/z〇Z) 〇h^ spp.) (non-sexual snail snail) (C. carhwMm), mites (eg, Helicobacter pylori (C. /ί/νΜ·?), asexual: wheat root rot, umbilical cord worm (where sorokiniana)) And rice (for example, Helminthosporium cerevisiae (c (10)' asexual state · Helminthosporium hirsutum (/ / 上;; Phytophthora (Co//eioir/c/2wm spp.) : Anthracnose (G/omerWa Spp_)) (anthrax): in cotton (for example, C. sinensis (cg〇;; household (7)), corn (eg 'P. sinensis (c • (1)·c〇) /a): anthrax stem rot), soft fruit, potato (for example, fruit rot . coccoi/e·?). black spot), beans (for example, Phytophthora sojae (c. /MAmwi/n·(10))) and soybeans (for example, sphaerocephala (c (10)) or spores Anthracnose (C. g/oeosporioic/e·?)); Phytophthora spp.) 'For example, Rhizoctonia solani (c μ 仏 ·) on rice (stained blight); soybean and ornamental plants Phytophthora sojae (c〇AT„eip〇ra Cai^7c〇/a) (leaf leaf spot); Cycl〇c〇nium spp., such as on the oil-removing tree Oil withdrawal from C. elegans (C. ο/eag/WMW); Pseudomonas (C_y" «do οαν(10)spp.) (for example, fruit tree cancer or vine decline, morphological: Arecirk SPP. or iVeoweciWa spp.: in fruit trees and vines (for example, the stalk of the palm stalk (C., sexual state: 揪掌揪149026) .doc •130- 201103429 Phytophthora capsici (A/ecmec/rz.a /z>z'oc^«drz'): Blackfoot disease) and ornamental plants on 'S. cerevisiae (£) E-mail (7) (7),) (has a sexual state: C. serrata (iJoje/hWa/ecaWx) ) (root rot and stem rot); D/apori/ze spp_, for example, D. phieo/or on the soybean (D· phieo/or please) Spore "synonymous genus Helminthus" has a sexual state: nucleocapsid: in corn, mites, such as barley (for example, umbilical umbilical (/) ierei), and wheat (such as ' Xingxian wheat snails (£)· Bu (1) c span's, brown spot)), rice blast and turf; EsCa (top blight, dry blight) on vines, by spot ritual {Formitiporia punctata , Phellinus punctata"), Mediterranean bacterium (F., Fusarium faecalis) (housekeeping / postal 〇 & & / / 3 3 3 3 3 3 3 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期 早期Phaeoacremonium chlamydosporum)), parasitic bottle mold (P/zfleoflcr (4) omwm fl/eop/n'/ww) and/or Botryosphaeria obtusa, bowed, M genus (Ehin〇e SPP) .). in Renguo (Pear Helicobacter pylori (5.p;; rz·)), soft fruit (P. sylvestris (£. veneia: anthracnose) and vine (V. serrata) /ina): Rickets), on the rice stalks, the black leaf disease of the rice leaf (heart such as 〇 〇 〇〇 ^e) (leaf smut); the genus of black bacterium in the wheat (5 〆 c〇cc_ SPP.) Disease) 'Ginkgo genus (five spp.) (powder disease): in sugar beet (Beet powdery mildew (£. Z^iae)), vegetables (for example, pea powdery mildew (£_pw)), such as melon (for example, two white powdery mildew (five / zoraceawm)), cabbage (canola) (for example, crucian powdery mildew (£· cr«c such as rarim)), in fruit trees, vines and ornamental trees 149026. Doc • 131 · 201103429 More than C. oxysporum (five grape cancer or top blight, asexual: polycystis/αία) (synonym: Lz·heart rie/M 6/ep; 2arb))); in the corn (for example, the large spotted umbilical bacterium (£· iwrchm)), the genus Umbra (ExSerohilum spp, synonymous snail); Helicobacter (7^like aWww spp) (having a sexual state: Gibberella sPP.)) (wild wilt, root rot or stem rot), such as cereals on the genus (eg wheat or barley) Spore Inearum) Fusarium oxysporum ^ (F. Culmorum ^ root rot, sore ill or head blight), Fusarium oxysporum π oxj^porwm on tomato, Fusarium solani on soybean Phytophthora (feet (1).) and Fusarium oxysporum (plant verAz7/ioWej) / mites (such as wheat or barley) and Phytophthora capsici on corn (Gaewwa/mo less cei full button disease) , Gibberella spp·): on mites (eg, Zew root zewing), and rice (eg, G. wy^wroz): locust disease, vines, kernels Anthracnose on fruit and other plants (G/〇 π - and cotton phlegm on cotton (G· g〇|Si^pZ'z'). Grans staining complex on rice (Grainstaining complex) ); the sputum of the genus Coccinella on the vine (black rot), the genus spp. on the genus Rosaceae and the juniper, such as the Sabin rust on the pear (G. (rust) , · Corn, scorpion and long genus on the rice stalk (synonym umbilical sarcophagus 'has a sexual state: Helminthosporium), rust genus (//ewi/em spp.), such as coffee Helminthosporium rust (open coffee leaf rust) ,. Phytophthora infestans on vines (/Yong _A c/aW printed ora) (synonymous grape mutans (cw〇v〇rz. 149026.doc •132-201103429

Wi/s)) /大豆及棉花上之菜豆殼球孢菌(Macrc>jc>/zc>mz·似 phaseolina,Macrophomina phaseoli)(根腐病反 1 腐病); 穀類(例如小麥或大麥)上之雪腐微結節菌(M/crc?t/oc/^ww mWe)(同義詞雪腐鐮孢菌(Fwiarz'wm «iva/e))(雪徽病),·大 豆上之黃華披散叉絲殼(A/7cr〇i_p/z<3era 白粉病); 褐腐病菌屬(Mom7zWa spp.),例如,核果及其他薔薇科植 物上之核果褐腐病菌(Μ· /(3X<3)、美澳型核果褐腐病菌(M. /rwchco/a)及仁果褐腐病菌(M (花腐病及枝枯病 (bloom and twig blight)、褐腐病);榖類、香蕉、軟果及 落花生上之球腔菌屬(Mycosp/zaereZ/a spp.),諸如小麥上 之禾球腔菌(M.尽ramzWco/a)(無性態:小麥殼針抱菌 ,殼針抱菌斑病(Septoria blotch)),或香 蕉上之斐濟球腔菌(Μ 黑香蕉葉斑病),·霜黴菌屬 (Pero⑽印ora spp.)(霜黴病):於甘藍菜(例如芸苔霜徽病(Ρ. brawicae))、油菜(例如寄生霜黴菌(P. /jaran'hca))、洋蔥 (例如毀壞霜黴菌(P. ☆yirwcior))、於草(终草霜黴菌(P. i(30ack<3))及大豆(例如大豆霜黴菌(尸.ma/^/zwrica))上;大 豆上之豆薯層鏽菌(P/zaAoporo! p<3c/2_yr/n‘zi·)及山馬*皇層鑛 菌(P_ meibomiae)(大豆鏽病)I 瓶徽菌屬(PhiaZophora spp.):例如於藤本植物(例如管胞瓶黴菌(P. ir<3c/ze(p/2//(3) 及四孢瓶黴菌(Ρ· 及大豆(例如大豆莖瓶徽菌(P. gregaia):莖腐病)上;油菜及甘藍菜上之黑脛莖點黴菌 (P/zom<3 /z'/igam)(根腐病及莖腐病),及糖用甜菜上之甜菜 莖點黴菌(户· 6以以)(根腐病、葉斑病及立枯病),·擬莖點黴 149026.doc -133- 201103429 菌屬(P/zomopWi spp.):於向曰葵、藤本植物(例如葡萄生 擬莖點黴菌(/>· Whco/α):葉斑病(can and ieaf spot))及大豆 (例如莖腐病:菜豆擬莖點黴菌(/>·如仍印⑺,有性態:菜 豆間座殼菌上;玉米上之玉米節 壺菌則;;山\?)(褐斑病);以下各種植物上之疫 黴菌屬spp.)(凋萎病,根、葉、果及莖腐 病):諸如辣椒及瓜類(例如辣椒疫黴菌(p c叩价z·))、大豆 (例如大豆疫黴菌(i>. ,户、馬鈐薯及番 力S (例如致病疫黴菌(/>· /咖加似):晚疫病)及闊葉樹(例如 多枝疫黴菌(户· ramorwm):橡樹突死);甘藍菜、油菜、蘿 蔔及其他植物上之芸苔根腫菌(ρ/αι^〇Α·σ;?/2〇π 如_cae)(根腫病)/單軸黴菌屬(ρ/α叩spp.),例如 藤本植物上之葡萄生單軸黴菌(户· Wn.co/a)(葡萄藤霜黴 病),及向曰葵上之霍爾斯單軸黴菌(户· ;薔薇科 植物、蛇麻子、仁果及軟果上之叉絲單囊殼菌属 (Ρ〇ύ?〇Μ/2απα Spp.)(白粉病),例如蘋果上之白叉絲單囊殼 菌(户· /ewcoiric/za);多黏菌屬(/>c)/_yWyxa spp.),例如在縠類 (諸如大麥及小麥)(禾多黏菌(户.及糖用甜菜(甜 菜多黏菌(P. feeiae))上’及由此傳播之病毒疾病,.縠類(例 如小麥或大麥)上之蔓毛殼假尾抱(户 herp〇trichoides)(輪故病,有性態:Tapesia γα11ιιηάα^ .,知 種植物上之假霜黴菌霜黴病),例如 瓜類上之南瓜假霜黴菌(尸cwijewh·?)或蛇麻子上之潷草假 霜黴菌(户· /2謂出);藤本植物上之葡萄角斑葉焦病菌Wi/s)) / Soybean and cotton on the bacterium (Macrc > jc > / zc > mz · phasephase, Macrophomina phaseoli) (root rot anti-1 rot); on cereals (such as wheat or barley) Snow rot microbe nodules (M/crc?t/oc/^ww mWe) (synonym Fwiarz'wm «iva/e) (snow emblem), · Huanghua shawl on soybean Silk shell (A/7cr〇i_p/z<3era powdery mildew); brown rot (Mom7zWa spp.), for example, stone fruit rot and other brown plants on the Rosaceae plant (Μ· /(3X<3), US-Australian type of brown rot fungus (M. /rwchco/a) and brown rot fungus (M (flower rot and twig blight, brown rot); mites, bananas, soft fruits And Mycosp/zaereZ/a spp. on the groundnut, such as the bacterium of the genus M. granulosus (M. ramzWco/a) (non-sexual state: wheat sclerotium, acicular plaque Disease (Septoria blotch), or Filipino sclerotium on banana (Μ black banana leaf spot), Downy mildew (Pero (10) printed ora spp.) (downy mildew): in cabbage (such as canola cream Disease (Ρ. brawicae)), rapeseed ( Such as parasitic downy mildew (P. / jaran'hca), onions (such as P. ☆ yirwcior), grass (P. i (30ack < 3)) and soybeans (such as soybeans) Downy mildew (corpse.ma/^/zwrica)); Pleurotus ostreatus on soybean (P/zaAoporo! p<3c/2_yr/n'zi·) and mountain horse*Pymeibomiae (Soybean rust) I PhiaZophora spp.: for example, in vines (eg, piperculosis (P. ir<3c/ze(p/2//(3)) and Tetrasporium (Ρ· And soybeans (eg, P. gregaia: stem rot); P. sphaeroides (P/zom < 3 /z'/igam) on rapeseed and cabbage (root rot and stem) Rot), and sugar beet on the beet stem mold (house 6 to) (root rot, leaf spot and blight), P. sinensis 149026.doc -133- 201103429 P/zomopWi spp.): to the hollyhock, vine (such as P. sphaeroides (/> Whco / α): leaf spot disease (can and ieaf spot) and soybeans (such as stem rot: Beans and Phomopsis molds (/>·If still printed (7), there are sexual states: Phytophthora sinensis; Potamoca sinensis on rice; mountain \?) (brown spot disease); Phytophthora spp.) (wild wilt, root, leaf, fruit and stem rot) on various plants: Melons (such as Phytophthora capsici (pc 叩 z)), soybeans (such as Phytophthora sojae (i>., household, horse yam and Fan Li S (such as Phytophthora infestans (/>· /Caga Like): late blight) and broad-leaved trees (such as Phytophthora sojae (R. ramorwm): oak tree death); Brassica campestris, rapeseed, radish and other plants on the roots of Phytophthora (ρ/αι^〇Α·σ ;?/2〇π such as _cae) (root swollen disease) / unicorn mold (ρ / α 叩 spp.), such as vines on the vines of the unicorn mold (W · Wn.co / a) (grape Rattan downy mildew), and the Helicobacter pylori on the hollyhock (household; Rosaceae, hops, pomegranate, and soft fruit) /2απα Spp.) (powder disease), such as the white sclerotium on the apple (H. / ewcoiric / za); polymyxa (/ > c) / _yWyxa spp.), for example in the mites (such as barley and wheat) (polymyxobacteria (household and sugar beet ( P. feeiae) and viral diseases transmitted by it, 蔓 ( ( ( ( ( ( her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her her State: Tapesia γα11ιιηάα^ ., known as the downy mildew mildew on plantings, such as pumpkin squash on the melon (cwijewh??) or shamrock on the hops (household /2) Said)); vines on the vines

t SI 149026.doc •134- 201103429 (PmW叩kac/^&gt;/nVc〇(紅火病(red 行代 disease)或 rotbrenner,無性態.瓶黴菌,.各種植物上 之柄鏽菌屬(PMccz’m’a spp.)(鏽病),例如穀類(例如小麥、 大麥或黑麥)上之小麥柄鏽菌(/&gt;·斤出·^•心)(褐鏽病或葉鏽 病)、條形柄鏽菌(P. 條鏽病或黃鏽病)、麥芽 柄鏽菌(户· /zorc?ei)(矮錄病(dwarf rust))、禾柄鏽菌(户. (莖鏽病或黑鏽病)或隱匿柄鏽菌(户(褐 鏽病或葉鏽病),及蘆筍上之柄鏽菌屬(例如蘆筍柄鏽菌(户 avar叹〇);小麥上之黃斑小麥核腔菌(户少刚叩心〜 irziwzrepe«沿)(無性態:黃斑小麥内臍蠕孢菌(Drec/^/era 褐斑病)或大麥上之圓核腔菌(户化^)(網 斑病),·梨抱菌屬(i&gt;rz‘cw/aWa spp.),例如稻榖上之水稻梨 孢菌(/*. or少zae)(有性態·稻瘦痛,稻 癌·病)及草皮及滅類上之灰梨抱菌(/&gt;. ;草皮、稻 穀、玉米、小麥、棉花、油菜、向曰葵、大豆、糖用甜 菜、蔬菜及各種其他植物上之腐徽菌屬Spp.)(立 枯病)(例如終末腐黴菌(P. M/i/mMw)或瓜果腐黴菌(/&gt;. aphanidermatum)),故满抱遠屬(Ramularia spp.),例如大 麥上之克樂希柱隔抱菌(兄coZ/ocygm.)(柱隔孢菌葉斑病, 生理性葉斑病)及糖用甜菜上之甜菜柱隔孢菌(兄 ;棉花、稻榖、馬鈐薯、草皮、玉米、油菜、馬 鈴薯、糖用甜菜、蔬菜及各種其他植物上之絲核菌屬 spp.),例如大豆上之茄絲核菌(及._5〇/⑽/)(根 腐病及莖腐病)、稻穀上之茄絲核菌(紋枯病)或小麥或大麥 I49026.doc •135· 201103429 上之禾穀絲核菌(/?. cerea/b)(絲核菌春枯病(Spring blight));草莓、胡蘿蔔、甘藍菜、藤本植物及番茄上之匍 枝根黴菌(及/n'zopMs(黑黴病' 軟腐病),.大麥、 黑麥及黑小麥上之黑麥缘抱菌謂褐 斑病),稻榖上之稻帚梗柱抱菌(Saroc/aAwm oryzae)及長 管帚梗柱孢菌(51· ⑽aiwm)(稍腐病);核盤菌屬 (•Sderoikk spp.)(莖腐病或白黴病):於蔬菜及田間作物, 諸如油菜、向曰葵(例如菌核核盤菌(S. π&amp;Γ〇η·〇ΓΜ/η))及大 豆(例如齊整核盤菌(iS r〇/yw〇或菌核核盤菌)上;各種植物 上之殼針孢菌屬’例如大豆上之甘胺酸殼針孢菌(&amp; 客/_^ζ·πα)(褐斑病)、小麥上之小麥殼針孢菌(&gt;s以出以)(殼針 孢菌斑病)及榖類上之穎枯殼針孢菌(iS·.⑽而⑶所)(同義詞賴 枯般多抱菌(iSYagowowora ”〇i/orww))(殼多孢菌斑病),.藤 本植物上之葡萄鉤絲殼菌weca(or)(同義詞葡萄 白粉病菌〇£&gt;少^&gt;/^ «ecaior))(白粉病,無性態:托氏粉孢 菌(Ch'cZ/wm iwcA:er/));刺球腔菌屬spp.)(葉枯 病):於玉米(例如大斑刺球腔菌(&amp; iwrdcwm),同義詞大斑 長緯抱菌(Heiminihosporium turcicum))反萆皮 _L ’,黑穩病 菌屬(•Sp/mce/oi/zeca spp.)(黑穗病):於玉米(例如玉米絲黑 穗病卤(&lt;S. rei/z*a;7£z):絲黑穗病(head smut))、高粱及甘藉 上’瓜類上之蒼耳單絲殼菌(^/meroi/zeca /w/4/«ea)(白粉 病)’馬鈴薯上之馬鈴薯粉癌菌(办OWgOiSp0ra (白 病病)及由此傳播之病毒疾病;穀類上之殼多孢菌屬,例 如小麥上之穎枯殼多抱菌($· 殼多抱菌斑病,有t SI 149026.doc •134- 201103429 (PmW叩kac/^&gt;/nVc〇 (red fire disease (red generation disease) or rotbrenner, asexuality. Bottle mold, Phytophthora on various plants (PMccz 'm'a spp.) (rust), such as wheat rust fungus (/&gt; 斤出•^• heart) (brown rust or leaf rust), strips on cereals (eg wheat, barley or rye) Rust fungus (P. stripe rust or yellow rust), malt rust (household / zorc? ei) (dwarf rust), rust rust (houser. (stem rust or black rust) Or concealed rust fungus (household (brown rust or leaf rust), and rust fungus on asparagus (such as asparagus rust fungus (household avar sigh); wheat on the yellow spot wheat nucleus bacteria (hu Shaogang heart ~ irziwzrepe « along) (non-sexuality: Helminthosporium umbellata (Drec/^/era brown spot) in the yellow spotted wheat or the nucleus of the genus on the barley (housekeeping ^) (net spot disease), · Pear Genus (i&gt;rz'cw/aWa spp.), such as P. sphaeroides (/*. or less zae) on rice cultivars (having sexuality, rice and rice pain, rice cancer, disease) and turf and extinction Grifola sinensis (/&gt;.; turf, rice, corn, Wheat, cotton, canola, hollyhocks, soybeans, sugar beets, vegetables, and various other plants of the genus Spp.) (Phenosis) (eg Pythium pyogenes (P. M/i/mMw) or Pythium genus (/&gt;. aphanidermatum), so it is full of genus (Ramularia spp.), such as Klein column on the barley (brother coZ / ocygm.) (S. sphaeroides leaf spot) , physiological leaf spot) and the sugar beet on the beetle sclerotium (brother; cotton, rice bran, horse yam, turf, corn, rape, potato, sugar beet, vegetables and various other plants on the silk Rhizoctonia spp.), such as Rhizoctonia solani (and ._5〇/(10)/) (root rot and stem rot), Rhizoctonia solani (strain) or wheat or barley on rice I49026.doc • 135· 201103429 The Rhizoctonia cereal (/?. cerea/b) (Spring blight); lychee on strawberries, carrots, kale, vines and tomatoes Rhizopus (and /n'zopMs (black mold disease 'soft rot), barley, rye and black wheat on the rye sclerotium called brown spot disease), rice blast on the rice stalk Aroc/aAwm oryzae) and Rhizoctonia solani (51·(10)aiwm) (slightly rot); Sclerotinia (•Sderoikk spp.) (stalk rot or white mold): in vegetables and field crops, Such as rapeseed, geranium (such as Sclerotinia sclerotiorum (S. π & Γ〇η·〇ΓΜ / η)) and soybeans (such as sclerotium sclerotium (iS r〇 / yw〇 or Sclerotinia sclerotiorum) Upper; Phytophthora on various plants' such as Glycyrrhiza glabrata (&amp; _^ζ·πα) (brown spot) on soybean, and Saccharomyces cerevisiae on wheat (&gt ;s out of () scleroderma) and scorpion sclerotium (iS·.(10) and (3)) (synonymous lyrics (iSYagowowora 〇i/orww) ) (shell plaque), vines on the vines of the genus weca (or) (synonym grape powdery mildew > less ^ &gt; / ^ «ecaior)) (powder disease, asexual state : Chrysosporium sinensis (Ch'cZ/wm iwcA: er/)); Phytophthora spp.) (leaf blight): in corn (eg, &amp; iwrdcwm), synonym Heiminihosporium turcicum, anti-skin _L ', black-stable disease Genus (•Sp/mce/oi/zeca spp.) (smut): in corn (eg, corn smut (<S rei/z*a; 7£z): silk smut (head smut)), sorghum and sorghum borrowed potato sclerotium from the 'Me/Milo/zeca /w/4/«ea' (powder disease) potato on the melon OWgOiSp0ra (white disease) and the viral disease transmitted thereby; the genus Pseudomonas on the cereal, such as the sclerotium on the wheat ($· 多 抱 菌 plaque,

[s I 149026.doc -136- 201103429 性態.穎枯小球腔菌ποί/orwm)[同義詞顆括 殼針孢菌(PZ/aeoip/meha ;馬鈐薯上之内生集 壺菌(办《c/zyWww 馬鈴薯癌腫病);外囊菌 屬[Taphrina spp.),例如桃上之畸形外囊菌(厂 縮葉病)及李子上之李外囊菌(r ⑴·)(李囊果 病),邊草、仁果、蔬菜、大豆及棉花上之根串珠黴菌屬 (772k/izWo;^·5 spp.)(黑根腐病),例如菸草根串珠黴菌(Γ 办adcoM)(同義詞優雅橫節黴菌(C;m/iJra ;穀類上 之腥黑穗病菌屬(77//eik spp.)(常見之黑穗病或腥黑穗病 (stinking smut)),諸如小麥上之小麥腥黑穗病菌(r 〜〜/)(同義詞網腥黑穗病菌(T. caries),小麥黑穗病)及矮 腥黑穗病菌(Γ. cowirover^)(矮黑穗病);大麥或小麥上之 紅核瑚菌⑽M)(灰雪黴病);條黑穗病菌屬 他spp_),例如黑麥上之黑麥桿黑穗病菌以 μ⑶-)(莖黑穗病),·蔬菜上之單孢鏽菌屬(t/r〇WCa spp.)(鏽病)’諸如於豆(例如疣頂單孢鏽菌… “即⑼心⑶/加似),同義詞菜豆單孢鏽菌((/ 0如⑼⑺)及糖 用甜菜(例如甜菜單抱鑛菌(t/. 0eme))上;黑穗病菌屬 (¢/扣7叹〇 sPP.)(散黑穗病(loose smut)):於縠類(例如裸黑 穗病菌(t/.⑽而)及燕麥黑穗病菌(t/.、玉米(例如 玉蜀黍黑穗病菌(ίλ讲叮山·^ :玉米黑穗病菌)及甘蔗上;黑 星菌屬(Rwwk sPP.)(瘡痂病):於蘋果(例如蘋果黑星菌 (K ka叫wa/b))及梨上;及各種植铷 裡植物(啫如水果及觀賞植 物、藤本植物、軟果、蔬菜及田間作铷 间作物)上之半身萎凋病 149026.doc -137· 201103429 菌屬(KemW/Hwm spp.)(凋萎病),例如草莓、油菜、馬於 薯及番茄上之大理菊萎凋病菌(K如/2/ke)。 化合物I、II及IV及其組合物分別亦適用於在保護儲存產 物或收穫物及保護材料中防治有害真菌。術語「保護材 料」應理解為表不保s蔓以下技術及非生物材料來對抗有宝 微生物(諸如真菌及細菌)之侵染及破壞:該等材料諸如黏 著劑、膠、木材、紙及紙板、紡織品、皮革、油漆分散 液、塑膠、冷卻潤滑劑、纖維或織物。關於保護木材及其 他材料,尤其應注意以下有害真菌:子囊菌綱,諸如長嗓 殼屬(Op/n’oWoma spp.)、青變真菌屬spp.)、 出芽短梗黴(dwreoftasWww pw/Zw/a;^)、擬莖點黴屬 (Sclefophoma spp.)、毛殼菌屬(Chaetomium spp.)、腐殖菌 屬(i/wmico/α spp.)、彼得殼屬(尸eir/e/M spp.)、毛束黴屬 (7&gt;&amp;/2μγμ·5 spp·);擔子菌綱’諸如粉孢革菌屬•印; spp.)、革蓋菌屬(Corio/ws spp.)、褐褶菌屬 spp.)、香菰屬spp.)、側耳屬(p/ewroiw spp.)、获 苓屬(Por/α spp.)、蟠龍介屬(Serpw/iz spp.)及乾酪菌屬 (7&gt;row_yce;s spp.);半知菌綱,諸如麴菌屬 spp.)、黑變病菌屬、青黴菌屬(Pen/ci/ZiMm spp.)、木徽菌 屬spp.)、交鏈孢菌屬、擬青黴屬 (Paecz’/omyca spp.)及接合菌綱,諸如毛黴菌屬(Mwcor spp.),且此外在保護儲存產物及收穫物中,應注意以下酵 母真菌:念珠菌屬(Ca«山'c/α spp.)及釀酒酵母菌 [S] 149026.doc •138- 201103429 化合物I、II及IV及其組合物分別可用於改善植物之健康 狀況。本發明亦係關於一種藉由分別以有效量之化合物 I、II及/或IV及其組合物來處理植物、其繁殖材料及/或植 物所生長或將要生長之場所來改善植物健康狀況之方法。 術語「植物健康狀況」應理解為表示植物及/或其產品 之狀況,其係由以下若干指示物單獨或彼此組合來確定: 諸如產量(例如,生物質量增加及/或有用成份含量增加)、 植物生長力[例如,植物生長.改善及/或葉子更綠(「變綠效 應J )]、品質(例如,某些成份之含量或組成改善)及對非 生物性及/或生物性逆境之耐受@。以上鐘別出之植物健 康狀況之指示物可相互依存或可彼此互為因果。 式I、II及IV之化合物可以不同結晶變體(其生物活性可 相異)形式存在。其同樣為本發明之標的物。 當藉由以殺真菌有效量之活性物質處理真菌或植物、植 物繁殖材料(諸如種子、土壤、表面、材料或房間)以使其 免受真g侵襲時’化合物卜肢㈣按原狀使用或以組合 物开&gt; 式使f在植物、植物繁殖材料(諸如種子、土壤、 材料或房間)文到真菌感染之前及之後均可施用。 可在種植或移植之1 之寺或之刖以化合物J、π及/或1¥按原 狀或以包含至少—錄彳μ人^ τ 種化合物1、II及/或IV之組合物預防性 地處理植物繁殖材料。 本發明亦係關於包含溶劑或固體載劑及至少一種化合物 及或IV之農用化學組合物及用於防治有害真菌之用 〇 149026.doc •139· 201103429 農用化學組合物包含殺真菌有效量之化合物I、II及/或 IV。術語「有效量」表示足以防治栽培植物上之有害真菌 或保護材料且不對經處理植物產生實質上損害的化合物 I、II及/或IV之組合物或化合物I、II及/或IV的量。該量可 在寬的範圍内變化且視以下各種因素而定:諸如受到防治 真菌之種類、經處理之栽培植物或材料、氣候條件及所用 特定化合物I。 化合物I、II及IV及其鹽可轉化為習用類型之農用化學組 合物,例如溶液、乳液、懸浮液、粉劑、散劑、糊狀物及 顆粒。組合物類型視特定預期目的而定;在各情況下,應 確保本發明之化合物精細且均勻分佈。 組合物類型之實例為懸浮液(SC、OD、FS)、可乳化濃 縮物(EC)、乳液(EW、EO、ES)、糊狀物、片劑、可濕潤 散劑或粉劑(WP、SP、SS、WS、DP、DS)或顆粒(GR、 FG ' GG、MG),其可為水溶性或可濕潤的,以及用於處 理植物繁殖材料(諸如種子)之凝膠調配物。 組合物類型(例如 SC、OD、FS、EC、WG、SG、WP、 SP、SS、WS、GF)通常在稀釋後使用。組合物類型(諸如 DP、DS、GR、FG、GG及MG)通常未經稀釋即使用。 以已知方式製備組合物(參看,US 3,060,084、EP-A 707 445(液體濃縮物),Browning:「Agglomeration」,Chemical Engineering, 1967 年 12 月 4 日,147-48,Perry's Chemical Engineer's Handbook,第 4版,McGraw-Hill,New York,1963,[s I 149026.doc -136- 201103429 modality. Phytophthora vaginalis ποί/orwm) [synonym for Pseudomonas sinensis (PZ/aeoip/meha; endophytic chytrid on horse yam "c/zyWww potato cancer disease"; genus [Taphrina spp.), such as the deformed outer sac of the peach (plant leaf defect) and the outer bacterium of the plum on the plum (r (1) ·) (Li capsule Disease), the genus Rhizopus on the grass, pome fruit, vegetables, soybeans and cotton (772k/izWo; ^·5 spp.) (black root rot), such as Toxoplasma gondii (adcoM) (synonym) Elegant Phytophthora infestans (C; m/iJra; sorghum genus (77//eik spp.) on cereals (common smut or stinking smut), such as wheat stalks on wheat Smut (r ~ ~ /) (synonym T. caries, wheat smut) and dwarf smut (Γ. cowirover ^) (dwarf smut); barley or wheat Rhodopseudomonas palustris (10)M) (Glyph of snow ash); smut ssp.), such as rye smut on rye, μ(3)-) (stalk smut), · single on vegetables Spore rust (t/r〇WCa spp.) (rust disease) 'such as beans (such as the sclerotium sclerotium ... "ie (9) heart (3) / plus), the synonym of Phytophthora sinensis (( / 0 such as (9) (7)) and sugar beet (such as sweet menu ore (t/. 0eme)); smut (¢/扣7〇 sPP.) (loose smut): in mites (such as smut (t/. (10)) And oat smut (t/., corn (such as maize smut) (ίλ speaks ··· : corn smut) and sugar cane; Helicobacter (Rwwk sPP.) (scared disease): in apple (eg, apple black bacillus (K ka called wa/b)) and pears; and the body of various planted sorghum plants (such as fruits and ornamental plants, vines, soft fruits, vegetables, and intercropping crops) Withering disease 149026.doc -137· 201103429 genus (KemW/Hwm spp.) (wild wilt), such as strawberry, rapeseed, horse-to-potato and tomato on the pathogen (K, /2 / ke). I, II and IV and their compositions are also suitable for controlling harmful fungi in the protection of stored products or harvests and protective materials, respectively. The term "protective material" should be understood as Underlying technical and non-biological materials to combat the infestation and destruction of valuable microorganisms such as fungi and bacteria: such materials as adhesives, glues, wood, paper and cardboard, textiles, leather, paint dispersions, plastics, cooling lubrication Agents, fibers or fabrics. For the protection of wood and other materials, special attention should be paid to the following harmful fungi: Ascomycetes, such as Op/n'o Woma spp., Spirulina spp. Mold (dwreoftasWww pw/Zw/a; ^), Sclefophoma spp., Chaetomium spp., Humicola (i/wmico/α spp.), Peter's genus (corporate eir/e/M spp.), genus genus (7&gt;&amp;/2μγμ·5 spp·); basidiomycete 'such as Helicobacter spp.; spp.), genus Corio/ws spp.), Pleurotus spp.), Citrus spp.), Pleurotus spp., Por/α spp., Serpent/iz Spp.) and Cases (7&gt;row_yce;s spp.); deuteromycetes, such as the genus Sputum spp.), genus Helicobacter, Penicillium (Pen/ci/ZiMm spp.), wood emblem Phytophthora spp.) Genus, Paecz'/omyca spp. and zygomycetes, such as Mwcor spp., and in addition to protecting stored products and harvests, the following yeast fungi should be noted: Candida (Ca) «Mountain 'c/α spp.) and Saccharomyces cerevisiae [S] 149026.doc • 138- 201103429 Compounds I, II and IV and their compositions, respectively, can be used to improve the health of plants. The invention also relates to a method for improving the health of a plant by treating the plant, its propagation material and/or the place where the plant is grown or to be grown, in an effective amount of the compound I, II and/or IV, and combinations thereof, respectively. . The term "phytosanitary condition" is understood to mean the condition of a plant and/or its products, which is determined by several indicators, either alone or in combination with each other: such as yield (eg, increased biomass and/or increased content of useful ingredients), Plant growth [eg, plant growth. Improvement and/or greener leaves ("greening effect"), quality (eg, improved content or composition of certain ingredients), and abiotic and/or biological adversity Tolerance @. The indicators of plant health status above may be interdependent or mutually damaging. The compounds of formulas I, II and IV may exist in different crystalline variants (which may differ in biological activity). Also the subject matter of the invention. When a fungus or plant, plant propagation material (such as seeds, soil, surface, material or room) is treated with a fungicidally effective amount of active substance to protect it from true g attack The limbs (4) are used as they are or in the form of a composition to make f in plants, plant propagation materials (such as seeds, soil, materials or rooms) before and after fungal infections. Administration: It can be prevented by compound J, π and/or 1 ¥ in the plant or transplanted 1 or in combination with a compound containing at least 彳 人 ^ 化合物 compound 1, II and / or IV The invention relates to the treatment of plant propagation materials. The invention also relates to agrochemical compositions comprising a solvent or a solid carrier and at least one compound and or IV and for controlling harmful fungi. 149026.doc • 139· 201103429 Agrochemical composition A fungicidally effective amount of Compound I, II and/or IV is included. The term "effective amount" means a compound I, II and/or IV which is sufficient to control harmful fungi or protective materials on cultivated plants and which does not substantially harm the treated plants. The amount of the composition or compound I, II and/or IV. The amount can vary within wide limits and depends on various factors such as the type of fungus being treated, the cultivated plant or material being treated, the climatic conditions, and the particular compound I used. The compounds I, II and IV and their salts can be converted into conventional agrochemical compositions such as solutions, emulsions, suspensions, powders, powders, pastes and granules. The type of composition will depend on the particular intended purpose; in each case, it will be ensured that the compounds of the invention are finely and uniformly distributed. Examples of composition types are suspensions (SC, OD, FS), emulsifiable concentrates (EC), emulsions (EW, EO, ES), pastes, tablets, wettable powders or powders (WP, SP, SS, WS, DP, DS) or particles (GR, FG 'GG, MG), which may be water soluble or wettable, and gel formulations for treating plant propagation materials such as seeds. The type of composition (e.g., SC, OD, FS, EC, WG, SG, WP, SP, SS, WS, GF) is typically used after dilution. The type of composition (such as DP, DS, GR, FG, GG, and MG) is usually used without dilution. The composition is prepared in a known manner (see, US 3,060,084, EP-A 707 445 (Liquid Concentrate), Browning: "Agglomeration", Chemical Engineering, December 4, 1967, 147-48, Perry's Chemical Engineer's Handbook, 4th edition, McGraw-Hill, New York, 1963,

第 8-57 頁,以下各頁,WO 91/13546、US 4,172,714、USPages 8-57, following pages, WO 91/13546, US 4,172,714, US

[S] 149026.doc -140· 201103429 4,144,050 ^ US 3,920,442 ' US 5,180,587 ' US 5,232,701 &gt; US 5,208,030 ' GB 2,095,558 ' US 3,299,566 &gt; Klingman: Weed Control as a Science (J. Wiley &amp; Sons,New York, 1961),Hance等 人:Weed Control Handbook (第 8 版,Blackwell Scientific, Oxford, 1989)及 Mollet, H. and Grubemann, A·: Formulation technology (Wiley VCH Verlag, Weinheim,2001))。 農用化學組合物亦可包含在農用化學組合物中習用之助 劑。所用助劑分別視特定應用形式及活性物質而定。 合適助劑之實例為溶劑、固體載劑、分散劑或乳化劑 (諸如,其他增溶劑、保護性膠體、界面活性劑及黏合 劑)、有機及無機稠化劑、殺細菌劑、防;東劑、消泡劑、 (若適當)著色劑及增黏劑或黏合劑(例如,用於種子處理調 配物)。 合適之溶劑為水;有機溶劑,諸如中至高沸點之礦物油 部分,諸如煤油或柴油;此外有煤焦油及植物或動物來源 之油;脂族、環狀及芳族烴,例如曱苯、二甲苯、石蠟、 四氫化萘、烷基化萘或其衍生物;醇類,諸如曱醇、乙 醇、丙醇、丁醇及環己醇;二醇類;酮類,諸如環己酮及 γ- 丁内酯;脂肪酸二甲醯胺、脂肪酸及脂肪酸酯及強極性 溶劑,例如胺,諸如Ν-曱基。比°各咬酮。 固體載劑為礦物土,諸如矽酸鹽、矽膠、滑石、高嶺 土、石灰石、石灰、白堊、紅玄武土、黃土、黏土、白雲 石、矽藻土、硫酸鈣、硫酸鎂、氧化鎂;經研磨之合成材 料;肥料,諸如硫酸銨、磷酸銨、硝酸銨、尿素;及植物 149026.doc -141 - 201103429 來源產物,諸如穀類粗粉、樹皮粗粉、木材粗粉及堅果殼 粗粉、纖維素粉末;及其他固體載劑。 合適之界面活性劑(佐劑、濕潤劑、增黏劑、分散劑或 乳化劑)為芳族磺酸(例如木質素磺酸(B〇rresperse&lt;&amp;型, Borregaard,Norway)、酚磺酸、萘磺型,Akz〇[S] 149026.doc -140· 201103429 4,144,050 ^ US 3,920,442 ' US 5,180,587 ' US 5,232,701 &gt; US 5,208,030 'GB 2,095,558 ' US 3,299,566 &gt; Klingman: Weed Control as a Science (J. Wiley &amp; Sons, New York, 1961), Hance et al.: Weed Control Handbook (8th ed., Blackwell Scientific, Oxford, 1989) and Mollet, H. and Grubemann, A: Formulation technology (Wiley VCH Verlag, Weinheim, 2001)). Agrochemical compositions may also contain conventional adjuvants in agrochemical compositions. The auxiliaries used will depend on the particular application and the active substance. Examples of suitable auxiliaries are solvents, solid carriers, dispersants or emulsifiers (such as other solubilizers, protective colloids, surfactants and binders), organic and inorganic thickeners, bactericides, defenses; Agents, defoamers, (if appropriate) colorants and tackifiers or binders (for example, for seed treatment formulations). Suitable solvents are water; organic solvents such as medium to high boiling mineral oil fractions such as kerosene or diesel; in addition to coal tar and oils of vegetable or animal origin; aliphatic, cyclic and aromatic hydrocarbons such as toluene, Toluene, paraffin, tetralin, alkylated naphthalene or derivatives thereof; alcohols such as decyl alcohol, ethanol, propanol, butanol and cyclohexanol; glycols; ketones such as cyclohexanone and γ- Butyrolactone; fatty acid dimethylamine, fatty acids and fatty acid esters and strong polar solvents such as amines such as anthracene-fluorenyl. Than each biting ketone. The solid carrier is mineral soil, such as silicate, tannin, talc, kaolin, limestone, lime, chalk, red basalt, loess, clay, dolomite, diatomaceous earth, calcium sulfate, magnesium sulfate, magnesium oxide; Synthetic materials; fertilizers such as ammonium sulphate, ammonium phosphate, ammonium nitrate, urea; and plants 149026.doc -141 - 201103429 Source products, such as cereal meal, bark meal, wood meal and nut meal, cellulose Powder; and other solid carriers. Suitable surfactants (adjuvants, wetting agents, tackifiers, dispersants or emulsifiers) are aromatic sulfonic acids (eg lignin sulfonic acid (B〇rresperse &lt;&amp; type, Borregaard, Norway), phenolic sulfonic acid , naphthalene sulfonate type, Akz〇

Nobel, U.S.A) 一 丁基奈續酸(Nekal® 型,BASF Germany))及脂肪酸之鹼金屬鹽、鹼土金屬鹽及銨鹽;烷 基磺酸鹽、烷基芳基磺酸鹽、烷基硫酸鹽、月桂基醚硫酸 鹽、脂肪醇硫酸鹽;及硫酸化十六烷醇、十七烷醇及十八 烷醇之鹽、硫酸化脂肪醇二醇醚、此外有萘或萘磺酸與苯 酚及曱醛之縮合物、聚氧乙烯辛基苯基醚、乙氧基化異辛 土盼辛基龄、壬基齡、烧基苯基聚乙二醇驗、三丁基苯 基聚乙二醇醚、三硬脂醯基苯基聚乙二醇醚、烷基芳基聚 醚醇、醇及脂肪醇/環氧乙烷縮合物、乙氧基化乾麻油、 聚氧乙烯烷基醚、乙氧基化聚氧丙烯、月桂醇聚乙二醇醚 縮醛、山梨糖醇酯、木質素亞硫酸鹽廢液及蛋白質、變性 蛋白質、多醣(例如,曱基纖維素)、疏水性改質澱粉、聚 乙烯醇(Mowiol® 型,Ciariant,Switzeriand)、聚羧酸酯 (S〇k〇ian®型,BASF,、聚烷氧基化物、聚乙烯胺 (pas〇l型,BASF,Germany)、聚乙烯η比洛咬酮及其共聚 物。Nobel, USA) monobutyl phthalate (Nekal® type, BASF Germany) and alkali metal, alkaline earth metal and ammonium salts of fatty acids; alkyl sulfonates, alkyl aryl sulfonates, alkyl sulphates Salt, lauryl ether sulfate, fatty alcohol sulfate; and sulfated cetyl alcohol, heptadecyl alcohol and stearyl alcohol salt, sulfated fatty alcohol glycol ether, in addition to naphthalene or naphthalenesulfonic acid and phenol And furfural condensate, polyoxyethylene octyl phenyl ether, ethoxylated isooctyl octyl age, bismuth base, pyridyl phenyl polyethylene glycol test, tributyl phenyl polyglycol ether , tristearyl nonyl phenyl polyglycol ether, alkyl aryl polyether alcohol, alcohol and fatty alcohol / ethylene oxide condensate, ethoxylated dry sesame oil, polyoxyethylene alkyl ether, ethoxy Polyoxypropylene, lauryl polyethylene glycol ether acetal, sorbitol ester, lignin sulfite waste liquid and protein, denatured protein, polysaccharide (for example, mercapto cellulose), hydrophobic modified starch, Polyvinyl alcohol (Mowiol® type, Ciariant, Switzeriand), polycarboxylate (S〇k〇ian® type, BASF, polyalkoxylate, Polyvinylamine (pas〇l type, BASF, Germany), polyethylene η pirone and its copolymer.

稠化劑之貫例(亦即,賦予組合物以改良的流動性之化 D物,亦即在靜態條件下之高黏度及在振盪期間之低黏 度)為多醣及有機及無機黏土,諸如三仙膠(Kelzan@, CPThe example of the thickening agent (that is, the D which imparts improved fluidity to the composition, that is, the high viscosity under static conditions and the low viscosity during the oscillation) are polysaccharides and organic and inorganic clays, such as three. Celery (Kelzan@, CP

[S] 149026.doc •142· 201103429[S] 149026.doc •142· 201103429

Kelco, U.S.A.) ^ Rhodopol® 23(Rhodia, France) ^ Veegum®(R.T.Kelco, U.S.A.) ^ Rhodopol® 23 (Rhodia, France) ^ Veegum® (R.T.

Vanderbilt,U.S.A.)或Attaclay®(Engelhard Corp” NJ,USA)。 可添加殺細菌劑以便保存組合物且使組合物穩定。合適 殺細菌劑之實例為彼等基於雙氯酚及笨甲醇半縮曱醛(ια 之 Proxel® 或 Thor Chemie之 Acticide® RS及 Rohm &amp; Haas之Vanderbilt, USA) or Attaclay® (Engelhard Corp. NJ, USA). A bactericide may be added to preserve the composition and stabilize the composition. Examples of suitable bactericides are those based on dichlorophenol and stupid methanol hemi-reducing Aldehyde (Proxel® from ια or Acticide® RS from Thor Chemie and Rohm &amp; Haas

Kathon® MK)的殺細菌劑及異噻唑啉酮衍生物,諸如烷基 異漆。坐琳酮及苯并異噻唑啉酮(Th〇r chemie之Acticide® MBS)。 合適防凍劑之實例為乙二醇、丙二醇、尿素及甘油。 消泡劑之實例為聚矽氧乳液(諸如,SUik〇n® SRE,Kathon® MK) is a bactericide and an isothiazolinone derivative such as an alkyl lacquer. Selenone and benzisothiazolinone (Acticide® MBS from Th〇r chemie). Examples of suitable antifreeze agents are ethylene glycol, propylene glycol, urea and glycerin. An example of a defoaming agent is a polyoxyl emulsion (such as SUik〇n® SRE,

Wacker,Germany 或 Rhodorsil®,Rhodia,France)、長鏈醇、 脂肪酸、脂肪酸鹽、氟有機化合物及其混合物。 合適之著色劑為低水溶性顏料及水溶性染料。所提及且 命名之實例為若丹明B(rh〇damin B)、c〗顏料紅m、C丄 溶劑紅1、顏料藍15:4、顏料藍15:3、顏料藍15:2、顏料藍 15:1、顏料藍80、顏料黃丨、顏料黃13、顏料紅ιΐ2、顏料 紅48:2、顏料紅48:1、顏料紅刃]、顏料紅53:i、顏料橙 43、顏料橙34、顏料橙5、顏料綠%、顏料綠7、顏料白 6、顏料棕25、驗性紫10、鹼性紫49、酸性紅51、酸性紅 52、酸性紅14、酸性藍9、酸性黃23、驗性㈣、驗性紅 108。 〜黏劑或黏合劑之實例為聚乙烯。比略相、聚乙酸乙稀 醋、聚乙稀醇及纖維素崎㈤⑽' 他㈣印,叫岭 可藉由將化合物1及(若適當)其他活性物質與至少-種固 149026.doc •143· 201103429 體載劑混合或伴隨研磨來製備散劑、散播用物質及粉劑。 可藉由使活性物質黏合至固體載劑上來製備顆粒,例 如,包衣顆粒、浸潰顆粒及均質顆粒。固體載劑之實例為 礦物土,諸如矽膠、矽酸鹽、滑石、高嶺土、美國活性白 土、石灰石、石灰、白堊、紅玄武土、黃土、黏土、白雲 石、矽藻土、硫酸鈣、硫酸鎂、氧化鎂;經研磨之合成材 料;肥料,諸如硫酸銨、磷酸銨、硝酸銨、尿素;及植物 來源產物,諸如榖類粗粉、樹皮粗粉、木材粗粉及堅果殼 粗粉、纖維素粉末;及其他固體載劑。 組合物類型之實例為: 1 ·以水稀釋之組合物類型 i) 水溶性濃縮物(SL、LS) 將1〇重量份本發明化合物T溶解於9〇重量份水中或水溶 性溶劑中。或者,添加潤濕劑或其它助劑。一旦以水稀 釋,活性物質即溶解。以此方式,獲得具有1〇重量%活性 物質含量之組合物。 ii) 分散性濃縮物(DC) 將20重量份本發明化合物!溶於7〇重量份環己鲷中,同 時添加㈣量份分散劑,例如聚乙稀D比…。以水稀 釋,產生分散液。活性物質含量為2〇重量%。 出)可乳化濃縮物(EC) 將1 5重量份本發明化合物j溶解於75重量份二甲苯中, ,時添加十二烷基苯磺酸鈣及萬麻油乙氧化物(分別為5重 置伤)。以水稀釋,產生乳液°該組合物具有15重量%之活 [S1 149026.doc •144· 201103429 性物質含量。 lv)乳液(EW ' E〇、ES) 將25重量份本發明化合物I溶解於35重量份二甲苯中, 同時添加十二烷基苯磺酸鈣及蓖麻油乙氧化物(分別為5重 莖份)。將此混合物藉助於乳化機(Uhraturax)引入3〇重量 份水中且將其製成均質乳液。以水稀釋,產生乳液。該組 合物具有2 5重量%之活性物質含量。 v)懸浮液(SC、OD、FS) 在搜動式球磨機中’將20重量份本發明化合物I碾磨, 同時添加1 0重量份分散劑及濕潤劑及7〇重量份水或有機溶 劑’得到精細的活性物質懸浮液β以水稀釋,產生活性物 質之穩定懸浮液。組合物中活性物質含量為2〇重量0/〇。 V1)水分散性顆粒及水溶性顆粒(WG、SG) 將50重量份本發明化合物I細磨,同時添加50重量份分 散劑及濕潤劑,藉助於工業級設備(例如擠壓機、噴霧 塔、流體化床)將其製備成水分散性或水溶性顆粒。以水 稀釋,產生活性物質之穩定分散液或溶液。該組合物具有 50重量%之活性物質含量。 vii) 水分散性散劑及水溶性散劑(WP、SP、SS、WS) 在轉子定子研磨機中研磨75重量份本發明化合物丨,同 時添加25重量份分散劑、濕潤劑及矽膠。以水稀釋,產生 活性物質之穩定分散液或溶液。組合物中活性物質含量為 75重量%。 viii) 凝膠(GF) 149026.doc -145- 201103429 在授動式球磨機中,將20重量份本發明化合物】礙磨, 同時添加1 〇重量松&quot;分散密丨]、〗舌旦八 里伪刀戒y 1重里份膠凝劑濕潤劑及70重 量份水或有機溶劑,得到活性物質之精.細懸浮液。以水稀 釋,產生活性物質之穩定懸浮液,藉以獲得具有20%(w/w) 活性物質之組合物。 2.未經稀釋而施用之組合物類型 ix)可粉化散劑(DP、DS) 將5重量份本發明化合物j細磨且與9 5重量份細粉狀高嶺 土緊密混合。此操作得到具有5重量%活性物質含量的可 粉化組合物。 X)顆粒(GR、FG、GG、MG) 將〇·5重量份本發明化合物厂細磨且與99 5重量份載劑組 合。當前方法為擠壓、喷霧乾燥或流體化床。此操作得到 具有〇.5重量%活性物質含量的未經稀釋而施用之顆粒。 xi) ULV溶液(UL) 將10重量份本發明化合物工溶於90重量份有機溶劑(例如 二曱苯)中。此操作得到具有10重量%活性物質含量的未經 稀釋而施用之組合物。 農用化學組合物通常包含0 01與95重量%,較佳0丨與卯 重量%之間’最佳0.5與90重量%之間的活性物質。使用純 度為90%至100%,較佳95%至1〇〇%(根據nmr光譜)之活性 物質。 通常出於處理植物繁殖材料(尤其種子)之目的而使用水 溶性濃縮物(LS)、可流動濃縮物(FS)、供乾燥處理之散劑 149026.doc -146- 201103429 (DS)、供漿料處理之水分散性散劑(ws)、水溶性散劑 (SS)、乳液(ES)、可乳化濃縮物(EC)及凝膠。可將此 等組合物在稀釋或未經稀釋之情況下施用於植物繁殖材 料,尤其種子。相關組合物在2至1〇倍稀釋之後在即用製 劑中得到0.01至60重量%,較佳心丨至扣重量%之活性物質 濃度。可在播種之前或期間進行施用。將農用化學化合物 及其組合物分別施用於植物繁殖材料(尤其種子)上或處理 其之方法在此項技術中已知且包括繁殖材料之拌種、包 衣、^化H浸泡及沿溝施用方法。在—較佳實施例 中,藉由不會誘導發芽之方法(例如,藉由拌種、丸化、 包衣及喷粉)將化合物或其組合物分別施用於植物繁殖材 料上》 ^ 在一較佳實施例中,懸浮液型(FS)組合物係用於種子處 理。通常,FS組合物可包含U00 g/丨活性物質、g&quot; 界面活性劑、〇至200 §/1防;東劑、0至400 g/丨黏合劑、〇8至 20〇 g/i顏料及至多1公升之溶劑(較佳為水)。 活性物質可按原狀或以其組合物形式藉助於噴灑、霧 化、噴粉、散播、刷塗、浸潰或傾注來使用,例如,以直 接可噴丨麗溶液、散劑、㈣液、分散液、乳液、油性分散 液、糊狀物、可粉化產品、散播用物質或顆粒之形式=施 用形式完全視預期目的而定;希望確保本 ,饰不發明之活性物質 在各情況下儘可能最精細的分佈。 可由乳液濃縮物、糊狀物或可濕潤散劑(可噴灑散劑, 油性分散液)藉由添加水來製備含水施用形式。、為^備乳 149026.doc •147· 201103429 液、糊狀物或油性分散液,可藉助於潤濕劑、增黏劑、分 政劑或乳化劑使原狀或溶解於油或溶劑中之物質在水中均 質化。或者,有可能製備由活性物質、濕潤劑、增黏劑、 为散劑或乳化劑及(若適當)溶劑或油構成之濃縮物,且該 等濃縮物適於以水稀釋。 即用製劑中之活性物質濃度可在相對較寬範圍内變化。 一般而言,濃度範圍為0.0001至10重量%,較佳〇 〇〇1至夏 重量^之活性物質。 亦可以超低容量法(ULV)成功地使用活性物質,有可能 施用包含高於95重量%之活性物質之組合物,或甚至在無 添加劑情況下施用活性物質。 當用於植物保護時,視所需作用種類而定,所施用的活 !·生物質之量為0.001至2公斤/公項(kg/ha),較佳〇 〇〇5至之公 斤/公項,更佳0.05至0.9公斤/公項,尤其〇1至〇75公斤/公 項。 在例如藉由喷粉、包衣或浸透種子來處理植物繁殖材料 (諸如種子)時,活性物質量一般需要在以下範圍内:〇1至 1000公克,較佳1至1000公克,更佳1至1〇〇公克且最佳5至 1 〇〇公克/100公斤植物繁殖材料(較佳為種子)。 當用於保護材料或儲存產物時,所施用的活性物質量視 知用領域類型及所需作用而定。慣常用於材料保護中的量 為例如0.001公克至2公斤,較佳0.005公克至i公斤活性物 質/立方公尺經處理材料。 可將多種類型之油劑、潤濕劑、佐劑、除草劑、殺細菌 [ 149026.doc •148· 201103429 劑、其他殺真菌劑及/或殺蟲劑添加至活性物質或包含其 之組合物中,(若適當)直至即將使用之前才加入(槽内混 合)。可將此等試劑與本發明組合物以1:100至100:1,較佳 1:10至10:1之重量比混合。 可使用之佐劑尤其為改質有機聚矽氧烷,諸如Break Thru S 240®;醇烷氧基化物,諸如 Atplus 245®、Atplus MBA 1303®、Plurafac LF 300®及 Lutensol ON 30® ; EO/PO 嵌段聚合物,例如,PluronicRPE 203 5®及GenapolB®;醇 乙氧基化物,諸如Lutensol XP 80®;及二辛基磺基琥珀酸 納,諸如 Leophen RA®。 呈殺真菌劑使用形式的本發明組合物亦可連同其他活性 物質一起提供,例如除草劑、殺蟲劑、生長調節劑、殺真 菌劑或肥料,作為預混合物或(若適當)直至即將使用之前 才混合(槽内混合)。 使呈殺真菌劑使用形式的化合物I、II及/或IV或包含其 之組合物與其他殺真菌劑混合導致許多情況:所獲殺真菌 活性範圍(fungicidal spectrum of activity)擴大或防止殺真 菌劑抗性發展。此外,在許多情況下,獲得協同效應。 可與本發明化合物聯合使用的活性物質之如下清單意欲 說明可能之組合,但並不對其進行限制: A)嗜毯果傘素(strobilurin) 亞托敏(azoxystrobin)、地莫菌胺(dimoxystrobin)、稀 月亏菌 S旨(enestroburin)、氣氧菌胺(fluoxastrobin)、克收 欣(kresoxim-methyl)、苯氧菌胺(metominostrobin)、奥 149026.doc -149- 201103429 瑞菌胺(orysastrobin)、。定氧菌胺(picoxystrobin)、百克 敏(pyraclostrobin)、β比瑞苯卡(pyribencarb)、三氟敏 (trifloxystrobin)、2-(2-(6-(3-氣-2-曱基-苯氧基)-5-氟-嘧啶-4-基氧基)-苯基)-2-曱氧基亞胺基-N-曱基-乙醯 胺、3-曱氧基-2-(2-(N-(4-甲氧基-苯基)-環丙烷-甲醯亞 胺基硫基曱基)-苯基)-丙烯酸曱酯、(2-氣-5-[ 1-(3-甲基 苄氧基亞胺基)乙基]苄基)胺基甲酸曱酯及2-(2-(3-(2,6-二氣苯基)-1-甲基-亞烯丙基胺基氧基曱基)-苯基)-2-甲 氧基亞胺基-N-曱基-乙酿胺; B)羧醯胺類 - 缓醯苯胺類:苯霜靈(benalaxyl)、苯霜靈-M(benalaxyl-M)、 麥鏽靈(benodanil)、必殺吩(bixafen)、博克利 (boscalid)、萎鏽靈(carboxin)、甲。夫醯胺(fenfuram)、 環醯菌胺(fenhexamid)、氟多寧(flutolanil)、福拉比 (furametpyr)、異0比贊(isopyrazam)、異 D塞菌胺(isotianil)、 克拉昔(kiralaxyl)、滅鏽胺(mepronil)、滅達樂 (metalaxyl)、滅達樂-M(甲霜靈(mefenoxam))、°夫酿胺 (ofurace)、 歐殺斯(oxadixyl)、 氧化萎鏽靈 (oxycarboxin)、°比《•塞菌胺(penthiopyrad)、森達先 (sedaxane) 克枯爛(tecloftalam)、赛氟滅 (thifluzamide)、汰敵寧(tiadinil)、2-胺基-4-甲基塞 °坐-5-曱醯苯胺、2-氣-N-(l,l,3-三曱基-茚滿-4-基)-菸鹼醯 胺、Ν-(3,,4·,5,-三氟聯苯-2-基)-3-二氟曱基-1-曱基-1H-吡唑-4-甲醯胺、Ν-(4·-三氟曱基硫基聯苯-2-基)-3-二氟 m 149026.doc -150- 201103429 甲基-1-甲基-1H-吡唑-4-曱醯胺、N-(2-(l,3-二曱基-丁 基)-苯基)-1,3-二曱基-5-氟-1H-吡唑-4-曱醯胺及Ν-ρ-ί 1 ’ 3 , 3 - 二甲基 -丁基 ) - 苯基 ) _ 1 , 3 - 二甲基 -5- 乳 -1H-0 比 。坐-4-甲醯胺; 幾·基嗎琳類:達滅芬(dimethomorph)、氟嗎 (flumorph)、丁 吡嗎啉(pyrim〇rph); ' 苯曱酸酿胺:氟美醯胺(flumetover)、It °比菌胺 (fluopicolide)、氟 °比胺(fluopyram)、氯苯醯胺 (zoxamide)、N-(3-乙基-3,5,5-三曱基-環己基)-3-曱醯 基胺基-2-羥基-苯曱醯胺; 其他緩醯胺:加普胺(carpropamid)、百治美特 (dicyclomet)、雙炔醯菌胺(mandiproamid)、土黴素 (oxytetracyclin)、矽硫芬(silthiofarm)及 N-(6-曱氧基-吡啶-3-基)環丙烷甲酸醯胺; C) «»坐類 - 三唑類:阿紮康唑(azaconazole)、比多農(bitertanol)、 &gt;臭克嗤(bromuconazole)、環克。坐(cyproconazole)、苯 謎曱環0坐(difenoconazole)、二石肖康0坐(diniconazole)、 二石肖康°坐-Μ、氟環嗤(epoxiconazole)、芬布康。坐 (fenbuconazole)、氣奎康 u坐(fluquinc.onazole)、氟石夕。坐 (flusilazole)、護汰芬(flutriafol)、六康 °坐(hexaconazole)、 亞胺唑(imibenconazole)、依普克唑(ipconazole)、葉菌 唑(metconazole)、麥環丁尼(myclobutanil)、嗯咪唑 (oxpoconazole)、巴克素(paclobutrazole)、潘康唾 149026.doc 151 - 201103429 (penconazole)、丙環唾(propiconazole)、丙硫醇克 η坐 (prothioconazole)、石夕敗 °坐(simeconazole)、得克利 (tebuconazole)、氣醚口坐(tetraconazole)、三泰芬 (triadimefon)、三泰隆(triadimenol)、環菌唾 (triticonazole)、稀效唾(uniconazole)、1-(4-氣-苯基)-2-([1,2,4]三唑-1-基)-環庚醇; -°米°坐類:赛座滅(cyazofamid)、依滅列(imazalil)、稻痕 醋(pefurazoate)、撲克拉(prochloraz)、赛福座 (triflumizole); 苯并咪0坐類:苯菌靈(benomyl)、貝芬替(carbendazim)、 麥穗靈(fuberidazole)、°塞苯味。坐(thiabendazole); - 其他:乙嘆博胺(ethaboxam)、依得利(etridiazole)、口惡 黴靈(hymexazole)及 2-(4-氣-苯基)-N-[4-(3,4-二甲氧基-苯基)-異噁唑-5-基]-2-丙-2-炔氧基-乙醯胺; D)雜環化合物 -。比0定類:扶吉胺(fluazinam)、比芬諾(pyrifenox)、3-[5-(4-氣-苯基)-2,3-二甲基-異噁唑啶-3-基]-吡啶、3-[5-(4-甲基-苯基)-2,3-二甲基·異噁唑啶-3-基]-吡啶、 2,3,5,6-四-氣-4-甲磺醯基-。比啶、3,4,5-三氯吡啶-2,6-一 _曱腈、N-( 1-(5-漠-3-氣-。比。定-2-基)-乙基)-2,4-二氣 菸鹼醯胺、N-[(5-溴-3-氯-η比啶-2-基)-曱基]-2,4-二氣-於驗醯胺; - 嘧。定類:石黃嘧菌靈(bupirimate)、西波定(cyprodinil)、 一氟林(diflumetorim)、芬瑞莫(fenarimol)、0密菌腙Wacker, Germany or Rhodorsil®, Rhodia, France), long chain alcohols, fatty acids, fatty acid salts, fluoroorganic compounds and mixtures thereof. Suitable colorants are low water soluble pigments and water soluble dyes. Examples mentioned and named are rh〇damin B, c pigment red m, C丄 solvent red 1, pigment blue 15:4, pigment blue 15:3, pigment blue 15:2, pigment Blue 15:1, Pigment Blue 80, Pigment Astragalus, Pigment Yellow 13, Pigment Red ΐ2, Pigment Red 48:2, Pigment Red 48:1, Pigment Red Blade], Pigment Red 53:i, Pigment Orange 43, Pigment Orange 34, Pigment Orange 5, Pigment Green%, Pigment Green 7, Pigment White 6, Pigment Brown 25, Test Purple 10, Basic Violet 49, Acid Red 51, Acid Red 52, Acid Red 14, Acid Blue 9, Acid Yellow 23, testability (four), test red 108. An example of a binder or binder is polyethylene. Ratio of slightly, polyethylene acetate vinegar, polyethylene glycol and cellulose (5) (10) 'He (four) India, called Ling can be by compound 1 and (if appropriate) other active substances with at least - seed 149026.doc • 143 · 201103429 The bulk carrier is mixed or accompanied by grinding to prepare powders, dispersion materials and powders. Granules can be prepared by binding the active material to a solid carrier, for example, coated granules, impregnated granules, and homogeneous granules. Examples of solid carriers are mineral soils such as tannin, silicate, talc, kaolin, activated clay, limestone, lime, chalk, red basalt, loess, clay, dolomite, diatomaceous earth, calcium sulfate, magnesium sulfate. , magnesium oxide; ground synthetic material; fertilizer, such as ammonium sulfate, ammonium phosphate, ammonium nitrate, urea; and plant-derived products, such as glutinous meal, bark meal, wood meal and nut meal, cellulose Powder; and other solid carriers. Examples of the type of the composition are: 1) Type of the composition diluted with water i) Water-soluble concentrate (SL, LS) 1 part by weight of the compound T of the present invention is dissolved in 9 parts by weight of water or a water-soluble solvent. Alternatively, add a wetting agent or other adjuvant. Once diluted with water, the active substance dissolves. In this way, a composition having an active substance content of 1% by weight was obtained. Ii) Dispersible Concentrate (DC) 20 parts by weight of the compound of the present invention is dissolved in 7 parts by weight of cyclohexanone while (4) parts of a dispersing agent such as polyethylene D ratio is added. Dilute with water to produce a dispersion. The active substance content was 2% by weight. Emulsifying Concentrate (EC) 15 parts by weight of the compound j of the present invention is dissolved in 75 parts by weight of xylene, and calcium dodecylbenzenesulfonate and eucalyptus ethoxylate are added (reset 5 respectively) hurt). Dilution with water to produce an emulsion. The composition has a 15% by weight activity [S1 149026.doc • 144·201103429). Lv) Emulsion (EW 'E〇, ES) 25 parts by weight of the compound I of the invention is dissolved in 35 parts by weight of xylene, while adding calcium dodecylbenzenesulfonate and castor oil ethoxylate (5 stalks respectively) Share). This mixture was introduced into 3 parts by weight of water by means of an emulsifier (Uhraturax) and made into a homogeneous emulsion. Dilute with water to produce an emulsion. The composition has an active substance content of 25% by weight. v) Suspensions (SC, OD, FS) In a searchable ball mill '20 parts by weight of compound I of the invention, while adding 10 parts by weight of dispersant and wetting agent and 7 parts by weight of water or organic solvent' A fine active substance suspension β is obtained which is diluted with water to produce a stable suspension of the active substance. The active substance content of the composition is 2 〇 weight 0 / 〇. V1) Water-dispersible granules and water-soluble granules (WG, SG) 50 parts by weight of the compound I of the invention are finely ground while adding 50 parts by weight of a dispersing agent and a wetting agent, by means of industrial grade equipment (for example, an extruder, a spray tower) , fluidized bed) is prepared as water-dispersible or water-soluble particles. Dilution with water produces a stable dispersion or solution of the active substance. The composition has an active substance content of 50% by weight. Vii) Water-dispersible powder and water-soluble powder (WP, SP, SS, WS) 75 parts by weight of the compound of the present invention were ground in a rotor stator mill while 25 parts by weight of a dispersing agent, a wetting agent and a silicone rubber were added. Dilution with water produces a stable dispersion or solution of the active substance. The active substance content in the composition was 75 wt%. Viii) Gel (GF) 149026.doc -145- 201103429 In an actuated ball mill, 20 parts by weight of the compound of the present invention is impaired, and 1 〇 weight loose &quot;dispersed secret 丨], 〗 〖 舌 八Knife ring y 1 heavy gelling agent wetting agent and 70 parts by weight of water or organic solvent to obtain a fine suspension of the active substance. Dilution with water produces a stable suspension of the active substance to obtain a composition having 20% (w/w) active material. 2. Type of composition to be applied without dilution ix) Powderable powder (DP, DS) 5 parts by weight of the compound j of the present invention was finely ground and intimately mixed with 95 parts by weight of fine powdery kaolin. This operation gave a pulverizable composition having an active substance content of 5% by weight. X) Granules (GR, FG, GG, MG) 5 parts by weight of the compound of the present invention were finely ground and combined with 99 parts by weight of a carrier. Current methods are extrusion, spray drying or fluidized beds. This operation resulted in undiluted granules having an active substance content of 5% by weight. Xi) ULV solution (UL) 10 parts by weight of the compound of the present invention is dissolved in 90 parts by weight of an organic solvent such as diphenylbenzene. This operation gave a composition which was applied without dilution as having an active substance content of 10% by weight. The agrochemical composition typically comprises between 0 and 95% by weight, preferably between 0 and 90% by weight of the active material between the optimum 0.5 and 90% by weight. An active material having a purity of from 90% to 100%, preferably from 95% to 1% by weight (based on the nmr spectrum) is used. Water-soluble concentrates (LS), flowable concentrates (FS), powders for drying treatment, 149026.doc-146-201103429 (DS), for slurry, are usually used for the purpose of treating plant propagation materials, especially seeds. Treated water dispersible powder (ws), water soluble powder (SS), emulsion (ES), emulsifiable concentrate (EC) and gel. These compositions can be applied to plant propagation material, especially seeds, either diluted or undiluted. The relevant composition obtains an active substance concentration of from 0.01 to 60% by weight, preferably from enamel to weight%, in a ready-to-use preparation after 2 to 1 稀释 dilution. Administration can be carried out before or during sowing. Methods of applying agrochemical compounds and compositions thereof to plant propagation materials, particularly seeds, respectively, or treating them are known in the art and include seed dressing, coating, H-soaking, and application along the furrow of the propagation material. method. In a preferred embodiment, the compound or composition thereof is separately applied to the plant propagation material by a method that does not induce germination (for example, by seed dressing, pelletization, coating, and dusting). In a preferred embodiment, a suspension type (FS) composition is used for seed treatment. Typically, the FS composition may comprise U00 g/丨 active material, g&quot; surfactant, 〇 to 200 §/1 prevention; east agent, 0 to 400 g/丨 binder, 〇8 to 20 〇g/i pigment and More than 1 liter of solvent (preferably water). The active substance can be used as it is or in the form of its composition by means of spraying, atomizing, dusting, spreading, brushing, dipping or pouring, for example, directly squirting a solution, a powder, a liquid, a dispersion , emulsion, oily dispersion, paste, powderable product, material for dispersion or granules = application form depends entirely on the intended purpose; it is desirable to ensure that the active substance that is not invented is as Fine distribution. Aqueous application forms can be prepared from emulsion concentrates, pastes or wettable powders (sprayable powders, oily dispersions) by the addition of water. Prepare milk for 149026.doc •147· 201103429 Liquid, paste or oily dispersion, which can be dissolved in oil or solvent by means of a wetting agent, tackifier, sub-agent or emulsifier. Homogenized in water. Alternatively, it is possible to prepare a concentrate consisting of an active substance, a wetting agent, a tackifier, a powder or an emulsifier and, if appropriate, a solvent or oil, and such concentrates are suitable for dilution with water. The concentration of the active substance in the ready-to-use preparation can vary over a relatively wide range. In general, the concentration ranges from 0.0001 to 10% by weight, preferably from 〇1 to summer by weight. It is also possible to successfully use the active substance by the ultra low volume method (ULV), it is possible to apply a composition comprising more than 95% by weight of the active substance, or even to apply the active substance without additives. When used for plant protection, depending on the type of action required, the amount of biomass applied is 0.001 to 2 kg / kg (ha / ha), preferably 〇〇〇 5 to kg / ha Item, better 0.05 to 0.9 kg / public, especially 〇 1 to 〇 75 kg / public. When the plant propagation material (such as a seed) is treated, for example, by dusting, coating or soaking the seed, the active mass generally needs to be in the range of 〇1 to 1000 grams, preferably 1 to 1000 grams, more preferably 1 to 1 gram and preferably 5 to 1 gram per 100 kg of plant propagation material (preferably seed). When used to protect materials or store products, the quality of the active applied is determined by the type of field and the desired effect. The amount conventionally used in material protection is, for example, from 0.001 g to 2 kg, preferably from 0.005 g to i kg of active material per cubic meter of treated material. Various types of oils, wetting agents, adjuvants, herbicides, bactericidal agents, 149026.doc • 148.201103429 agents, other fungicides and/or insecticides may be added to the active substance or compositions thereof Medium, (if appropriate) is added until the time of use (in-tank mixing). These agents may be combined with the compositions of the present invention in a weight ratio of from 1:100 to 100:1, preferably from 1:10 to 10:1. Adjuvants which may be used are especially modified organic polyoxyalkylenes such as Break Thru S 240®; alcohol alkoxylates such as Atplus 245®, Atplus MBA 1303®, Plurafac LF 300® and Lutensol ON 30®; EO/ PO block polymers, for example, Pluronic RPE 203 5® and Genapol B®; alcohol ethoxylates such as Lutensol XP 80®; and sodium dioctylsulfosuccinate such as Leophen RA®. The compositions of the invention in the form of fungicides may also be provided together with other active substances, such as herbicides, insecticides, growth regulators, fungicides or fertilizers, as premixes or, if appropriate, until ready for use. Only mix (mixed in the tank). Mixing Compounds I, II and/or IV in the form of a fungicide or a composition comprising the same with other fungicides results in a number of situations: the fungicidal spectrum of activity expands or prevents fungicides Resistance development. In addition, in many cases, synergies are obtained. The following list of actives that can be used in combination with the compounds of the present invention is intended to illustrate possible combinations, but is not intended to be limiting: A) strobilurin, azoxystrobin, dimoxystrobin , enestroburin, fluoxastrobin, kresoxim-methyl, metominostrobin, 149026.doc -149- 201103429 RESSOstrobin ,. Picoxystrobin, pyraclostrobin, pyripencarb, trifloxystrobin, 2-(2-(6-(3-)-2-mercapto-phenoxy 5-)fluoro-pyrimidin-4-yloxy)-phenyl)-2-oxooxyimido-N-indenyl-acetamide, 3-decyloxy-2-(2-( N-(4-methoxy-phenyl)-cyclopropane-mercaptoimidothioindolyl)-phenyl)-decyl acrylate, (2-a-5-[ 1-(3-methyl) Benzyloxyimido)ethyl]benzyl)carbazate and 2-(2-(3-(2,6-diphenyl)-1-methyl-allylamino) (Alkyl)-phenyl)-2-methoxyimino-N-indenyl-ethinylamine; B) Carboxylamamines - sulfonamides: benylaxyl, benzathine M (benalaxyl-M), benodanil, bixafen, boscalid, carboxin, nail. Fenfuram, fenhexamid, flutolanil, furametpyr, isopyrazam, isotianil, kiralaxyl ), mepronil, metalaxyl, methaul-M (mefenoxam), ofurace, oxadixyl, oxidized rust Oxycarboxin), ° compared to "penthiopyrad", sedaxane, tecloftalam, thifluzamide, tiadinil, 2-amino-4-methyl °°坐-5-aniline, 2-gas-N-(l,l,3-tridecyl-indan-4-yl)-nicotinamide, Ν-(3,,4·,5 ,-Trifluorobiphenyl-2-yl)-3-difluoroindol-1-yl-1H-pyrazole-4-carboxamide, Ν-(4·-trifluorodecylthiobiphenyl- 2-yl)-3-difluorom 149026.doc -150- 201103429 Methyl-1-methyl-1H-pyrazole-4-nonylamine, N-(2-(l,3-didecyl)- Butyl)-phenyl)-1,3-dimercapto-5-fluoro-1H-pyrazole-4-nonylamine and Ν-ρ-ί 1 ' 3 , 3 -dimethyl-butyl) - Phenyl) _ 1 , 3 -dimethyl-5-milk-1H-0 ratio. Sodium methionine; kimenline: dimethomorph, flumorph, pyrim〇rph; 'benzoic acid enriched amine: flumethamine ( Flumetover), It ° fluopicolide, fluopyram, zoxamide, N-(3-ethyl-3,5,5-tridecyl-cyclohexyl)- 3-mercaptoamino-2-hydroxy-benzoguanamine; other slowing amines: carpropamid, dicyclomet, mandiproamid, oxytetracyclin ), silthiofarm and N-(6-decyloxy-pyridin-3-yl)cyclopropanecarboxylic acid decylamine; C) «»Sit-like - triazoles: azaconazole, ratio Bitertanol, &gt;bromuconazole, ring grams. Sitting (cyproconazole), benzene 曱 曱 ring 0 sitting (difenoconazole), 二石肖康0 sitting (diniconazole), 二石肖康 ° sitting-Μ, epoxiconazole, fenbukon. Sitting (fenbuconazole), qikuikun u sitting (fluquinc.onazole), fluorite eve. Flusilazole, flutriafol, hexaconazole, imibenconazole, ipconazole, metconazole, myclobutanil, Ixazole (oxpoconazole), paclobutrazole, Pan Kang sal 149026.doc 151 - 201103429 (penconazole), propiconazole, propionazole, prothioconazole, simeconazole , tebuconazole, tetraconazole, triadimefon, triadimenol, triticonazole, uniconazole, 1-(4-gas-benzene Base)-2-([1,2,4]triazol-1-yl)-cycloheptanol; -°m° sitting class: cyazofamid, imazalil, rice vinegar ( Pefurazoate), prochloraz, triflumizole; benzopyrene 0 sitting class: benomyl (benomyl), phenendazim (carbendazim), wheat ear (fuberidazole), ° benzene. Sitting (thiabendazole); - Others: ethaboxam, etridiazole, hymexazole, and 2-(4-gas-phenyl)-N-[4-(3, 4-Dimethoxy-phenyl)-isoxazole-5-yl]-2-prop-2-ynyloxy-acetamide; D) Heterocyclic compound-. Specific to 0: fluazinam, pyrifenox, 3-[5-(4-a-phenyl)-2,3-dimethyl-isoxazodin-3-yl] -pyridine, 3-[5-(4-methyl-phenyl)-2,3-dimethylisoxazol-3-yl]-pyridine, 2,3,5,6-tetra-gas- 4-methanesulfonyl-. Bisidine, 3,4,5-trichloropyridine-2,6-mono-carbonitrile, N-(1-(5- desert-3-gas-.pyr.din-2-yl)-ethyl)- 2,4-di-nicotinine decylamine, N-[(5-bromo-3-chloro-η-pyridin-2-yl)-indenyl]-2,4-di-gas - prodecylamine; - pyrimidine . Classification: bupirimate, cyprodinil, diflumetorim, fenarimol, 0 bacterium

[SI 149026.doc •152· 201103429 (ferimzone)、米潘尼比林(mepanipyrim)、氣。定 (nitrapyrin)、氟苯°密。定醇(nuarimol)、比利美沙尼 (pyrimethanil); - 旅嗪類:赛福寧(triforine); -°比 π各類:拌種 B各(fenpiclonil)、護汰寧(fludioxonil); - 嗎淋類:阿迪嗎淋(aldimorph)、嗎菌靈(dodemorph)、 乙酸嗎菌靈、粉鐘嚇 (fenpropimorph)、十三嗎琳 (tridemorph); - 派σ定類:苯鏽咬(fenpropidin); - 二甲酸亞胺:氟醯亞胺(fluoroimid)、依普同(iprodione)、 撲滅寧(procymidone)、免克寧(vinclozolin); - 非芳族5 -員雜環:°惡吐菌酮(famoxadone)、σ米》坐菌酮 (fenamidone)、說多寧(flutianil)、辛0塞 _ (octhilinone)、 °塞菌靈(probenazole)、、5-胺基-2-異丙基-3-側氧基-4-鄰-曱苯基-2,3-二氫-吡唑-1-硫代甲酸S-烯丙酯; - 其他:酸化苯并0塞二。坐-S-曱酉旨(acibenzolar-S-methyl)、σ引 π坐石夤菌胺(amisulbrom)、敵菌靈(anilazin)、殺稻遮素-S(blasticidin-S)、四氣丹(captafol)、蓋普丹(captan)、 滅蜗猛(chinomethionat)、邁隆(dazomet)、咪菌威 (debacarb)、噠菌清(diclomezine)、苯敵快 (difenzoquat)、苯敵快-甲基硫酸鹽、禾草靈 (fenoxanil)、福爾培(Folpet)、歐索林酸(oxolinic acid)、粉病靈(piperalin)、普奎那兹(proquinazid)、百 快隆(pyroquilon)、快諾芬(quinoxyfen)、°米 α坐嗓 149026.doc -153 - 201103429 (triazoxide)、三赛《•坐(tricyclazole)、2-丁氧基-6-破-3_ 丙基咬烯-4-酮、5-氯-l-(4,6-二甲氧基-嘴咬-2-基)-2-曱 基-1H-苯并咪唑、5-氣-7-(4-曱基旅。定-1·基)_6-(2,4,6-三氟苯基)-[1,2,4]三唑并[l,5-a]嘧啶及5 -乙基-6-辛基-[1,2,4]三唑并[l,5-a]嘧啶-7-基胺; E) 胺基甲酸酯 - 硫代胺基曱酸酯及二硫代胺基曱酸酯,福美鐵 (ferbam)、代森猛辞(mancozeb)、代森猛(maneb)、咸 百故(metam)、罐菌威(methasulphocarb)、代森聯 (metiram)、丙森鋅(propineb)、福美雙(thiram)、代森 辞(zineb)、福美辞(ziram); - 胺基曱酸西旨:苯0塞瓦利(benthiavalicarb)、乙黴威 (diethofencarb)、绳黴威(iprovalicarb)、霜黴威 (propamocarb)、霜黴威鹽酸鹽、威立芬那(valiphenal) 及N-(l-(1-(4-氰基-笨基)乙磺醯基)-丁-2-基)胺基曱酸-(4-氟苯基)酯; F) 其他活性物質 - 胍類:胍、多寧(dodine)、多寧游離鹼、雙脈辛 (guazatine)、雙胍辛乙酸鹽、克熱淨(iminoctadine)、 克熱淨三乙酸鹽、克熱淨(烷苯磺酸鹽); - 抗生素:春日徽素(kasugamycin)、春日黴素鹽酸鹽水 合物、鏈黴素(streptomycin)、多氧菌素(P〇ly〇xine)、 有效徽素 A(validamycin A); • 硝基苯基衍生物:百蟎克(binapacryl)、大脫瞒[SI 149026.doc • 152· 201103429 (ferimzone), mepanipyrim (mepanipyrim), gas. Set (nitrapyrin), fluorobenzene ° dense. Nuarimol, pyrimethanil; - pilazines: triforine; -° ratio π: seed dressing B (fenpiclonil), deficiency (fludioxonil); Dripping: aldimorph, dodemorph, acetaminophen, fenpropimorph, tridemorph; - sigma: fenpropidin; - Dicarboxylic acid imine: fluoroimid, iprodione, procymidone, vinclozolin; - non-aromatic 5-membered heterocycle: ° oxacillin ( Famoxadone), σ米》fenamidone, flutianil, octhilinone, probenazole, 5-amino-2-isopropyl-3- Side oxy-4-o-indolephenyl-2,3-dihydro-pyrazole-1-thiocarboxylic acid S-allyl ester; - Other: acidified benzox. -S-曱酉-(Acibenzolar-S-methyl), σ π 坐 坐 坐 坐 ami ami ami ami ami ami ami 、 、 、 、 、 ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani ani Captafol), captan, chinomethionat, dazomet, debacarb, diclomezine, difenzoquat, benzophenone-methyl Sulfate, fenoxanil, Folpet, oxolinic acid, piperalin, proquinazid, pyroquilon, veolifen (quinoxyfen), °mα sitting 嗓 026 026 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓 嗓-Chloro-l-(4,6-dimethoxy-mouth-2-yl)-2-mercapto-1H-benzimidazole, 5-gas-7-(4-anthracen brigade. ·)) 6-(2,4,6-trifluorophenyl)-[1,2,4]triazolo[l,5-a]pyrimidine and 5-ethyl-6-octyl-[1, 2,4]triazolo[l,5-a]pyrimidin-7-ylamine; E) urethane-thioamino phthalate and dithioamino phthalate, thiram (ferbam) ), Daisen’s words Mancozeb), maneb, manam, metasulphocarb, metiram, propineb, thiram, zineb , ziram (ziram); - amino citrate oxime: benzene 0 sali (benthiavalicarb), methimcarb (diethofencarb), iprolim (iprovalicarb), propamocarb (propamocarb), propamocarb hydrochloride Salt, valiphenal and N-(l-(1-(4-cyano-phenyl)ethenyl)-butan-2-yl) decanoic acid-(4-fluorophenyl) Ester; F) Other active substances - terpenoids: hydrazine, dodine, toxin free base, guazatine, bismuthinoic acid acetate, iminoctadine, gram heat triacetate , 克热净 (alkylbenzene sulfonate); - antibiotics: kasugamycin, kasugamycin hydrochloride, streptomycin, polyoxin (P〇ly〇xine), effective Validamycin A; • Nitrophenyl derivative: binapacryl, large dislocation

[SI 149026.doc -154- 201103429 (dinobuton)、白粉克(dinocap)、酞菌醋(nitrthal-isopropyl)、四氯硝基苯(tecnazen);有機金屬化合物: 三苯錫鹽(fentin salts)、諸如三苯醋錫、三苯錫氣或毒 菌錫(fentin hydroxide); - 含硫雜環基化合物:腈硫酿(dithianon)、稻痕靈 (isoprothiolane); - 有機填化合物:護粒松(edifenphos)、三乙膦酸 (fosetyl)、三乙膦酸铭(fosetyl-aluminum)、丙基喜樂 松(iprobenfos)、亞構酸及其鹽、白粉松(pyrazophos)、 脫克松(tolclofos-methyl); - 有機氯化合物:百菌清(chlorothalonil)、益發靈 (dichlofluanid)、雙氯酌 (dichlorophen)、It 硫滅 (flusulfamide)、六氣苯、賓克隆(pencycuron)、五氣酌· 及其鹽、苯酉大(phthalide)、奎脫辛(quintozene)、甲基 多保淨 (thiophanate-methyl)、 曱基益發靈 (tolylfluanid)、N-(4 -氣-2-石肖基-苯基)-N-乙基-4-甲基-苯磺醯胺; - 無機活性物質:波爾多液(Bordeaux mixture)、乙酸 銅、氫氧化銅、氣氧化銅、鹼式硫酸銅、硫; - 其他:聯苯、漠補醇(b r ο η ο ρ ο 1) 、°塞芬胺 (cyflufenamid)、霜脲氰(cymoxanil)、二苯胺、美曲芬 謹(metrafenone)、滅粉黴素(mildiomycin)、經基喧琳 銅(〇乂111-。〇卩卩61&gt;)、調環酸|弓(卩1*〇116乂3(^01^-。31(^11111)、螺 環菌胺(spiroxamine)、曱基益發靈(tolylfluanid)、N- 149026.doc -155 - 201103429 (環丙基甲氧基亞胺基_(6_二氟-甲氧基·2,3_二氟-苯基)_ 曱基)-2-本基乙酿胺、ν’-(4-(4-氣-3-二氣曱基-苯氧 基)-2,5-二曱基-苯基乙基-N-曱基曱脒、N'-(4-(4-說-3-三氟甲基·苯氧基)_2,5_二曱基_苯基乙基-N-曱 基曱脒、N,-(2-甲基-5-三氟甲基-4-(3-三甲基矽烷基-丙 氧基)-苯基)-N-乙基-N-甲基甲脒、N,-(5-二氟甲基-2-曱基-4-(3-三曱基矽烷基-丙氧基)-苯基)-N-乙基-N-甲 基甲脒、2-{1-[2-(5•曱基-3-三氟曱基-。比唑-1-基)-乙醯 基]-哌啶-4-基}-噻唑-4-曱酸曱基-(1,2,3,4-四氫-萘-1-基)-醯胺、2-{1-[2-(5-甲基-3-三氟甲基-吡唑-1-基)-乙 醯基]-哌啶-4-基}-噻唑-4-甲酸曱基-(R)-l,2,3,4-四氫-萘-1-基-醯胺、乙酸6-第三丁基-8-氟-2,3-二曱基-喹啉-4-基酯及曱氧基-乙酸6-第三丁基-8-氟-2,3-二曱基-喹 淋-4-基酉旨。 G)生長調節劑 脫落酸、。夫喃丹(amidochlor)、三環苯嘴醇 (ancymidol)、6-苄基胺基嘌呤、芸苔素内酯 (brassinolide)、雙 丁樂靈(butralin)、克美素 (chlormequat)(矮壯素(chlormequat chloride))、氣化膽 驗(choline chloride)、環院基酿苯胺(cyclanilide)、丁 醢肼(daminozide)、敵草克(dikegulac)、。塞節因 (dimethipin)、2,6-二曱基0比咬、益收生長素(ethephon)、 lL 節胺(flumetralin)、°夫响醇(flurprimidol)、達草氟 (fluthiacet)、氣 °比服(forchlorfenuron)、赤黴酸 [S1 149026.doc 156- 201103429 (gibberellic acid)、依納素(inabenfide)、。引。朵 _3-乙酸、 順丁烯二酿肼(maleic hydrazide)、敦績醯草胺 (mefluidide)、壯棉素(mepiquat)(壯棉素氣化物)、萘乙 酸、N-6-苄基腺嘌吟、巴克素、調環酸(調環酸約)、 茉莉酸丙酯(prohydrojasmon)、噻苯隆(thidiazuron)、 抑芽唑(triapenthenol)、三丁基三硫磷酸酯、2,3,5-三 璜苯甲酸、抗倒醋(trinexapac-ethyl)及稀效。坐; H)除草劑 - 乙醯胺類:乙草胺(acetochlor)、甲草胺(alachlor)、去 草胺(butachlor)、二曱草胺(dimethachlor)、二甲嗔草 胺(dimethenamid)、氟噻草胺(flufenacet)、苯噻醯草胺 (mefenacet)、異丙甲草胺(metolachlor)、吡草胺 (metazachlor)、萘氧丙草胺(napropamide)、萘丙胺 (naproanilide)、烯草胺(pethoxamid)、丙草胺 (pretilachlor)、毒草安(propachlor)、甲氧嗟草胺 (thenylchlor); - 胺基酸衍生物:畢拉草(bilanafos)、嘉填塞 (glyphosate)、固殺草(glufosinate)、硫復松 (sulfosate); - 芳氧基苯氧基丙酸酯類:炔草酸(clodinafop)、丁基赛 伏草(cyhalofop-butyl)、°惡 °坐禾草靈(fenoxaprop)、0比 氟禾草靈(fluazifop)、°比氟氯禾靈(haloxyfop)、°惡β坐醯 草胺(metamifop)、普拔草(propaquizafop)、啥禾靈 (quizalofop)、喧禾靈糠醋(quizalofop-P-tefuryl); 149026.doc -157- 201103429 聯°比α定類.敵草快(diquat)、百草枯(paraquat); -(硫代)胺基甲酸酯類:亞速爛 (asulam)、蘇達滅 (butylate)、卡草胺(carbetamide)、甜菜安(desmedipham)、 哌草丹(dimepiperate)、撲草滅(eptam,EPTC)、戊草 丹(esprocarb)、得草滅(m〇iinate)、坪草丹(orbencarb)、 甜菜寧(phenmedipham)、苄草丹(prosulfocarb)、稗草 畏(pyributicarb)、殺丹(thiobencarb)、野麥畏(triallate); &quot; 環己一鲷類:丁苯草鋼(butroxydim)、克草同 (clethodim)、環殺草(cyci〇xydim)、環苯草酮 (profoxydim)、西殺草(sethoxydim)、得殺草 (tepraloxydim)、苯草酮(tralkoxydim); -一硝基苯胺類:倍尼芬(benfluralin)、乙丁稀氟靈 (ethalfluralin)、安項靈(〇ryzalin)、二甲戊樂靈 (pendimethalin)、胺說樂靈(prodiamine)、敗樂靈 (trifluralin); -一苯謎類:三It緩草醚(acifluorfen)、苯草鱗 (aclonifen)、必芬諾(bifenox)、禾草靈(diclofop)、氯 氟草醚(ethoxyfen)、氟磺胺草醚(fomeSafen)、乳氟禾 草靈(lactofen)、乙氧氟草趟(〇xyfluorfen); - 經基苯曱腈類:溴苯腈(bomoxynil)、二氣苯腈 (dichlobenil)、峨苯腈; &quot;0米0坐琳酮類:咪草醋(imazamethabenz)、曱氧味草於 (imazamox)、甲咪唑菸酸(imazapic)、滅草菸(imaza_ Pyr)、滅草啥(imazaquin)、σ米草於(imazethapyr); 149026.doc •158- 201103429 - 苯氧基乙酸類:稗草胺(clomeprop)、2,4-二氣笨氧乙 酸(2,4-D)、2,4-DB、濟丙酸(dichlorprop)、MCPA、 MCPA-硫乙基、MCPB、2 -甲-4-氯丙酸(Mecoprop); -°比°秦類:氣草敏(chloridazon)、氟嗔°秦草酯(flufenpyr-ethyl)、氟 °塞乙草酯(fluthiacet)、氟草敏(norflurazon)、 嚷草特(pyridate); -β比咬類:氯胺D比咬酸(aminopyralid)、畢克草 (clopyralid)、°比氟草胺(diflufenican)、氟硫草定 (dithiopyr)、氟咬草酮(fluridone)、氟草於(fluroxy-pyr)、毒莠定(picloram)、氟。比草胺(picolinafen)、&lt;·塞草 咬(thiazopyr); - 續醯脲類:醯°密續隆(amidosulfuron)、四°坐°密績隆 (azimsulfuron)、苄。密磺隆(bensulfuron)、乙基氣濟績 隆(chlorimuron-ethyl)、氣續隆(chloi’sulfuron)、趟續隆 (cinosulfuron)、環丙嘴績隆(cyclosulfamuron)、乙氧喷 續隆(ethoxysulfuron)、伏速隆(flazasulfuron)、比續 隆(flucetosulfuron)、氟咬0密項隆(flupyrsulfuron)、甲 醯胺續隆(foramsulfuron)、氯。比嘴石黃隆(halosulfuron)、 〇坐0比0^ 績隆(imazosulfuron)、蛾甲續隆(iodosulfuron)、甲 確胺確隆(mesosulfuron)、曱基曱績隆(metsulfuron-methyl)、於。密續隆(nicosulfuron)、環氧痛黃隆 (oxasulfuron)、氟。密磺隆(primisulfuron)、氟續隆 (prosulfuron)、°比 °密石黃隆(pyrazosulfuron)、颯啦續隆 (rimsulfuron)、曱0密確隆(sulfometuron)、罐嘴績隆 149026.doc -159- 201103429 (sulfosulfuron)、嗟吩續隆(thifensulfuron)、醚苯續隆 (triasulfuron)、苯續隆(tribenuron)、三敗咬項隆 (trifloxysulfuron)、氟胺續隆(triflusulfuron)、三氟曱 石黃隆(tritosulfuron)、1-((2 -氣-6-丙基-味 °坐并[l,2-b]噠 嗪-3-基)磺醯基)-3-(4,6-二甲氧基-嘧啶-2-基)脲; - 三嗓類:莠滅淨(ametryn)、莠去津(atrazine)、氰草津 (cyanazine)、異戍乙淨(dimethametryn)、乙0秦草酮 (ethiozin)、環 °秦 _ (hexazinone)、苯0秦草酮(metami-tron)、賽克津(metribuzin)、撲草淨(prometryn)、西瑪 津(simazine)、特丁津(terbuthylazine)、特丁淨 (terbutryn)、三 °秦敗草胺(triaziflam); -脲類:綠麥隆(chlorotoluron) ' 殺草隆(daimuron)、敵 草隆(diuron)、伏草隆(fluometuron)、異丙隆 (isoproturon)、利穀隆(linuron)、甲苯0塞隆(methabenz-thiazuron)、丁°塞隆(tebuthiuron); - 其他乙醯乳酸合成酶抑制劑:雙草醚-鈉(bispyribac-sodium)、曱基氣醋石黃草胺(cloransulam-methyl)、雙氣 石黃草胺(diclosulam)、雙氣續草胺(florasulam)、氟酮石黃 隆(flucarbazone)、β坐喊石黃草胺(flumetsulam)、續草0圭 胺(metosulam)、°密苯胺績隆(ortho-sulfamuron)、平速 爛(penoxsulam)、丙苯續隆(propoxycarbazone)、丙醋 草喊(pyribambenz-propyl)、响 °定月亏草輕(pyribenzoxim)、 環西旨草醚(pyriftalid)、曱基嘯草喊(pyriminobac-methyl)、,沙泛(pyrimisulfan)、喊硫草醚(pyrithiobac)、[SI 149026.doc -154- 201103429 (dinobuton), white powder (dinocap), nitrthal-isopropyl, tetrachloronitrobenzene (tecnazen); organometallic compounds: fentin salts (fentin salts), Such as triphenyltin sulphate, triphenyltin or fentin hydroxide; - sulfur-containing heterocyclic compounds: dithianon, isoprothiolane; - organic compound: granules Edifenphos), foetyl, fosetyl-aluminum, iprobenfos, eutectic acid and its salts, pyrazophos, tolclofos-methyl ); - organochlorine compounds: chlorothalonil, dichlofluanid, dichlorophen, flusulfamide, hexaesene, pencycuron, five gas and its Salt, phthalide, quintozene, thiophanate-methyl, tolylfluanid, N-(4- gas-2-stone Schottyl-phenyl)- N-ethyl-4-methyl-benzenesulfonamide; - Inorganic active substance: Bordeaux mixture (Bordeaux mix (ture), copper acetate, copper hydroxide, copper oxide, basic copper sulfate, sulfur; - other: biphenyl, indomethacin (br ο η ο ρ ο 1), ° cyflufenamid, cream urea Cyanoxanil, diphenylamine, metrafenone, mildiomycin, carbendazim copper (〇乂111-.〇卩卩61&gt;), cyclohexanoic acid|bow (卩1 *〇116乂3(^01^-.31(^11111), spiroxamine, tolylfluanid, N-149026.doc -155 - 201103429 (cyclopropylmethoxy) Amino-(6-difluoro-methoxy-2,3-difluoro-phenyl)-indenyl-2-propenylamine, ν'-(4-(4-gas-3-di Gasoyl-phenoxy)-2,5-dimercapto-phenylethyl-N-mercaptopurine, N'-(4-(4-]-3-trifluoromethylphenoxy _2,5-didecyl-phenylethyl-N-indenyl hydrazine, N,-(2-methyl-5-trifluoromethyl-4-(3-trimethyldecyl-propyloxy) -Phenyl)-N-ethyl-N-methylformamidine, N,-(5-difluoromethyl-2-indolyl-4-(3-tridecylfluorenyl-propoxy) -Phenyl)-N-ethyl-N-methylformamidine, 2-{1-[2-(5•indolyl-3-trifluoromethyl)-. Bisazo-1-yl)-ethinyl]-piperidin-4-yl}-thiazole-4-furoate-yl-(1,2,3,4-tetrahydro-naphthalen-1-yl)-indole Amine, 2-{1-[2-(5-methyl-3-trifluoromethyl-pyrazol-1-yl)-ethinyl]-piperidin-4-yl}-thiazole-4-carboxylic acid hydrazine --(R)-l,2,3,4-tetrahydro-naphthalen-1-yl-decylamine, 6-tert-butyl-8-fluoro-2,3-dimercapto-quinoline-4 - Alkyl ester and decyloxy-acetic acid 6-tert-butyl-8-fluoro-2,3-dimercapto-quinolin-4-yl. G) Growth regulator Abscisic acid. Amidochlor, ancymidol, 6-benzylaminopurine, brassinolide, butralin, chlormequat (chlormequat) (chlormequat chloride)), choline chloride, cyclanilide, daminozide, dikegulac. Dimethipin, 2,6-dimercapto 0 bite, ethephon, lL flumetralin, flurprimidol, fluthiacet, gas ° Forchlorfenuron, gibberellic acid [S1 149026.doc 156- 201103429 (gibberellic acid), inabenfide,. lead. _3-acetic acid, maleic hydrazide, mefluidide, mepiquat (strong cotton), naphthaleneacetic acid, N-6-benzyl gland嘌吟, bucksin, cyclized acid (about cyclic acid), propyl jasmonate (prohydrojasmon), thidiazuron, triapenthenol, tributyl trithiophosphate, 2, 3, 5-triterpene benzoic acid, trinexapac-ethyl and thin effect. H) Herbicide - Acetamamine: acetochlor, alachlor, butachlor, dimethachlor, dimethenamid, Flufenacet, mefenacet, metolachlor, metazachlor, napropamide, naproanilide, enegrass Pethoxamid, pretilachlor, propachlor, thenylchlor; - amino acid derivatives: bianafos, glyphosate, sessile (glufosinate), sulfosate; - aryloxyphenoxypropionates: clodinafop, cyhalofop-butyl, °° fenoxaprop , 0 fluazifop, ° haloxyfop, ° β 醯 胺 met met (metamifop), propaquizafop, qui 灵 灵 (quizalofop), 喧 糠 糠Vinegar (quizalofop-P-tefuryl); 149026.doc -157- 201103429 联° ratio α categorization. Diquat, herb (paraquat); -(thio)carbamates: asulam, butarate, carbeamide, desmedipham, dimepiperate, flutter Herbicide (eptam, EPTC), esprocarb, m〇iinate, orbencarb, phenmedipham, prosulfocarb, pyributicarb , thiobencarb, triallate; &quot; cycloheximide: butroxydim, clethodim, cyci〇xydim, benzophenone (profoxydim), sethoxydim, tepraloxydim, tralkoxydim; -mononitroaniline: benfluralin, etalfluralin, safety Ling (〇ryzalin), pendimethalin, amine prodiamine, trifluralin; - benzene mystery: three it acifluorfen, benzene grass scale (aclonifen ), bifenox, diclofop, ethoxyfen, flufenacetate (fomeSafen) ), lactofen, oxyfluorfen; - benzoquinones: bomoxynil, dichlobenil, benzonitrile; &quot; 0 m 0 sitny ketones: imazamethabenz, imazamox, imidazonic acid (imazapic), imaza_ Pyr, imazaquin, σ米草于(imazethapyr); 149026.doc •158- 201103429 - Phenoxyacetic acid: clomeprop, 2,4-dioxyacetic acid (2,4-D), 2,4-DB, Dichlorprop, MCPA, MCPA-thioethyl, MCPB, 2-methyl-4-chloropropionic acid (Mecoprop); -° ratio ° Qin: chloridazon, flurazepam Flufenpyr-ethyl), fluthiacet, norflurazon, pyridate; -beta ratio: chloramine D than aminopyralid, clopyralid ), ° diflufenican, dithiopyr, fluridone, fluroxy-pyr, picloram, fluoride. Picolinfen, &lt;thiazopyr; - continuation of urea: ami 密 密 续 ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami ami Bensulfuron, chlorimuron-ethyl, chloi'sulfuron, cinosulfuron, cyclosulfamuron, ethoxy sulfonate Ethoxysulfuron), flazasulfuron, flucetosulfuron, flupyrsulfuron, foramsulfuron, chlorine. Halosulfuron, 〇 0 0-0 0^, iazosulfuron, iodosulfuron, mesosulfuron, metsulfuron-methyl, . Nicosulfuron, oxasulfuron, fluorine. Primisulfuron, prosulfuron, ° ratio, pyrazosulfuron, rimsulfuron, sulfometuron, canning 149026.doc - 159-201103429 (sulfosulfuron), thifensulfuron, triasulfuron, tribenuron, trifloxysulfuron, triflusulfuron, trifluorosulfon Tritosulfuron, 1-((2-gas-6-propyl-flavored[1,2-b]pyridazin-3-yl)sulfonyl)-3-(4,6- Dimethoxy-pyrimidin-2-yl)urea; - triterpenoids: ametryn, atrazine, cyanazine, dimethametryn, gamma Ketone (ethiozin), hexazinone, metami-tron, metribuzin, prometryn, simazine, terbuthylazine ), terbutryn, triaziflam; -urea: chlorotoluron 'daimuron, diuron, fluometuron ), isoproturon, linuron, methabenz-thiazuron, tebuthiuron; - other acetamidine lactate synthase inhibitor: bispyribac-sodium ( Bispyribac-sodium), cloransulam-methyl, diclosulam, florasulam, flucarbazone, beta Flumetsulam, metasulam, ortho-sulfamuron, penoxsulam, propoxycarbazone, propyl vinegar (pyribambenz- Propylbenzoxim, pyrifalid, pyrimiminobac-methyl, pyrimisulfan, pyrithiobac,

[SI 149026.doc -160- 201103429 普羅蘇芬(pyroxasulfone)、甲氧續草胺(pyroxsulam); 其他:胺。坐草酮(amicarbazone)、胺基三。坐、莎稗填 (anilofos)、氟丁 醯草胺(beflubutamid)、草除靈(ben-azolin)、苯卡巴月宗(bencarbazone)、咬草石黃(benflu-resate)、°比草酮(benzofenap)、苯達松(bentazone)、苯 并雙環酮(benzobicyclon)、除草定(bromacil)、漠丁醯 草胺(bromobutide)、氟丙°密草醋(butafenacil)、抑草構 (butamifos)、唾草胺(cafenstrole) 、°坐酿| 草醋 (carfentrazone)、n弓丨 °朵酮草醋(cinidon-ethlyl)、敵草索 (chlorthal)、環庚草鱗(cinmethylin)、可滅蹤 (clomazone)、节草隆(cumyluron)、°塞普續醯胺 (cyprosulfamide)、麥草畏(dicamba)、苯敵快 (difenzoquat)、二氟 D比隆(diflufenzopyr)、稗内臍螺孢 菌(Z)rec/^/era monoceras)、草0多 °索(endothal)、乙吱草 續(ethofumesate)、乙氧苯草胺(etobenzanid)、四 °坐酿 草胺(fentrazamide)、戊基氣胺草酯(flumiclorac-pentyl)、丙炔氟草胺(flumioxazin)、氟胺草《•坐 (flupoxam)、氟略草酮(flurochloridone)、咳草鲷 (flurtamone)、茚草酮(indanofan)、異 °惡草胺 (isoxaben)、異 °惡吐草酮(isoxaflutole)、環草定 (lenacil)、敵稗(propanil)、戊诀草胺(propyzamide)、 二氯0# 琳酸(quinclorac)、喧草酸(quinmerac)、甲基續 草酮(mesotrione)、曱基胂酸、萘草胺(naptalam)、丙 炔°惡草酮(oxadiargyl)、°惡草酮(oxadiazon)、°惡嗪草酮 149026.doc -161 - 201103429 (oxaziclomefone)、環戊 °惡草酮(pentoxazone)、唾琳草 酯(pinoxaden)、雙唑草腈(pyraclonil)、乙基吡草趟 (pyraflufen-ethyl)、。比續托利(pyrasulfotole)、节草哇 (pyrazoxyfen)、比拉。圭諾(pyrazolynate)、滅藻蛾 (quinoclamine)、嘴咬肪草輕(saflufenacil)、確草嗣 (sulcotrione)、曱續草胺(sulfentrazone)、特草定 (terbacil)、特伏曲 _ (tefuryltrione)、替莫曲酮 (tembotrione)、°塞吩卡巴膝(thiencarbazone)、拓普美 膝(topramezone)、4-羥基-3-[2-(2-曱氧基-乙氧基曱基)_ 6-三氟甲基比啶-3-羰基]-雙環[3.2.1]辛-3-烯-2-酮、 (3-[2 -氣-4-氟-5-(3 -曱基-2,6-二側氧基-4-二氣曱基-3,6_ 二氮-2Η-σ密β定-1-基)-笨氧基]比D定-2 -基氧基)-乙酸乙 酉旨、6 -胺基-5-氣-2 -ί哀丙基- °¾°定-4-甲酸曱醋、6 -氣-3_ (2-環丙基-6-甲基-苯氧基)-噠嗪-4-醇、4-胺基-3-氣-6-(4-氣-苯基)-5·氟-吡啶-2-甲酸、4-胺基-3-氣-6-(4-氣-2· 氟-3-曱氧基-苯基)-吡啶-2-曱酸曱酯及4-胺基-3-氯-6-(4-氣-3-二甲基胺基-2-氟-苯基)-吡啶-2-曱酸曱酯。 I)殺蟲劑 - 有機(硫代)攝酸鹽類:歐殺松(acephate)、曱基〇比咬磷 (azamethiphos)、曱基穀硫鱗(azinphos-methyl)、毒死 蜱(chlorpyrifos)、曱基毒死碑(chlorpyrifos-methyl)、 氣芬填(chlorfenvinphos)、二 °秦農(diazinon)、敵敵畏 (dichlorvos)、百治磷(dicrotophos)、大滅松(dimethoate)、 二硫松(disulfoton)、愛殺松(ethion)、撲滅松 -162- 149026.doc 201103429 (fenitrothion)、芬殺松(fenthion)、加福松(isoxathion)、 馬拉松(malathion)、達馬松(methamidophos)、滅大松 (methidathion)、曱基巴拉松(methyl-parathion)、美文 松(mevinphos)、亞素靈(monocrotophos)、滅多松 (oxydemeton-methyl) &gt; 巴拉奥克松(paraoxon)、巴拉松 (parathion)、賽達松(phenthoate)、裕必松(phosalone)、 益滅松(phosmet)、福賜米松(phosphamidon)、福瑞松 (phorate)、巴赛松(phoxim)、亞特松(pirimiphos-methyl)、 布飛松(profenofos)、普硫松(prothiofos)、殺普松 (sulprophos)、樂本松(tetrachlorvinphos)、託福松 (terbufos)、三落松(triazophos)、三氣松(trichlorfon); - 胺基甲酸S旨類:棉靈威(alanycarb)、得滅克(aldicarb)、 免敵克(bendiocarb) '免扶克(benfuracarb)、加保利 (carbaryl)、加保扶(carbofuran)、丁基加保扶(carbosulfan)、 芬謹克(fenoxycarb)、咬線威(furathiocarb)、滅蟲威 (methiocarb)、納乃得(methomyl)、歐殺滅(oxamyl)、 抗財威(pirimicarb)、殘殺威(propoxur)、硫雙威 (thiodicarb)、°坐财威(triazamate); - 擬除蟲菊酯:丙烯除蟲菊(allethrin) '畢芬寧 (bifenthrin)、賽扶寧(cyfluthrin)、賽洛寧 (cyhalothrin)、赛紛寧(cyphenothrin)、賽滅寧 (cypermethrin)、α-赛滅寧、β-賽滅寧、ζ-賽滅寧(zeta-cypermethrin)、第滅寧(deltamethrin)、益化利 (esfenvalerate) ' 依芬寧(etofenprox)、芬普寧 149026.doc -163- 201103429 (fenpropathrin) &gt; 芬化利(fenvalerate)、依普寧 (imiprothrin)、λ-赛洛寧(lambda cyhal〇thrin)、百滅寧 (permethrin)、普亞列寧(praUethrin)、除蟲菊精 (Pyrethrin)I及II、異列滅寧(resmethHn)、氟矽菊酯 (silafluofen)、τ-福化利(tau_fiuvaiinate)、七 i 菊醋 (tefluthrin)、四甲司林(tetramethrin)、泰滅寧 (tralomethrin)、拜富寧(transfiuthrin)、丙 i 菊 g旨 (profluthrin)、四氟曱喊菊自旨(dimefluthrin); -昆蟲生長調節劑:a)曱殼素合成抑制劑:苯曱醯基脲 (benzoylureas) ·克福隆(chi〇rfiuazuron)、賽滅淨 (cyramazin) 一 福隆(diflubenzuron)、福環腺 (flucycloxuron)、IL 芬隆(flufenoxuron)、六伏隆 (hexaflumuron)、祿芬隆(lufenuron)、諾瓦隆 (novaluron)、得福隆(teflubenzuron)、三福隆 (triflumuron);布芬淨(buprofezin)、苯蟲醚 (diofenolan)、合赛多(hexythiazox)、依殺瞒 (etoxazole)、克芬蟎(clofentazine) ; b)蛻皮激素拮抗 劑:合芬隆(halofenozide)、滅芬諾(methoxyfenozide)、 得芬諾(tebufenozide)、印楝素(azadirachtin) ; c)保幼 激素類似物:百利普芬(pyriproxyfen)、美賜平 (methoprene)、芬諾克;d)脂質生物合成抑制劑:螺瞒 酉旨(spirodiclofen)、螺曱瞒S旨(spiromesifen)、螺蟲乙酉旨 (spirotetramat); - 菸鹼樣受體促效藥/拮抗劑化合物:可尼丁 149026.doc 201103429 (clothianidin)、咬蟲胺(dinotefuran)、益達胺 (imidacloprid)、°塞蟲嗓(thiamethoxam)、烯 °定蟲胺 (nitenpyram)、啶蟲脒(acetamiprid) 、 °塞蟲淋 (thiacloprid)、1 -(2-氯塞唾-5-基甲基)-2-石肖基亞胺基-3,5-二曱基-[1,3,5]三嗪; -GABA拮抗劑化合物:硫丹(endosulfan)、乙蟲清 (ethiprole)、芬普尼(fipronil)、萬尼普(vaniliprole)、 氟蟲腈(pyrafluprole)、派瑞樂(pyriprole)、5-胺基-1-(2,6-二氯-4-甲基-苯基)-4-胺亞磺醯基-1H-吡唑-3-硫代 曱酸醯胺; - 大環内醋殺蟲劑:阿巴;丁(abamectin)、因滅汀 (emamectin)、密滅汀(milbemectin)、林皮沒丁 (lepimectin)、賜諾殺(spinosad)、斯平托蘭 (spinetoram); - 線粒體電子傳遞抑制劑(METI)I殺蟎劑:芬殺蟎 (fenazaquin) 比達本(pyridaben)、得芬瑞 (tebufenpyrad)、脫芬瑞(tolfenpyrad)、氟芬内林 (flufenerim); -METI II及III化合物:亞醌蟎(acequinocyl)、福希普 (fluacyprim)、伏蟻月宗(hydramethylnon); - 解偶聯劑:蟲瞒腈(chlorfenapyr); - 氧化磷酸化抑制劑:環己錫(cyhexatin)、汰芬隆 (diafenthiuron)、芬布賜(fenbutatin oxide)、殿瞒多 (propargite); 149026.doc -165- 201103429 - 規皮破裂劑化合物.赛滅淨(cryomazine); - 混合功能氧化轉抑制劑:胡椒基丁鍵(piperonyl butoxide) &gt; - 鈉通道阻斷劑.茚蟲威(indoxacarb)、美氟膝 (metaflumizone) ί - 其他·本克°塞(benclothiaz)、畢芬載(bifenazate)、殺堵 丹(cartap)、敦尼月女(fl〇nicamid)、°定蟲丙鍵(pyridalyl)、 派滅淨(pymetrozine) ' 硫、硫賜安(thiocyclam)、福本 胺(flubendiamide)、氣鄰胺基苯甲普(chi〇rantraniliprole)、 魚尼汀受體抑制劑(cyazypyr,HGW86)、塞諾吡芬 (cyenopyrafen)、。比 I 硫填(fiupyrazofos)、0塞氟美芬 (cyflumetofen)、醯胺氣美(amid〇fiumet) ' 口米克芬 (imicyafos)、雙三I蟲脲(bistrifluron)及。比氟喧月宗 (pyrifluquinazon) ° 本發明此外係關於農用化學組合物,其包含至少一種化 合物I、II及/或IV(組份丨)及至少另一種適用於植物保護之 活性物質(例如,選自群A)至1))(組份2),尤其另一殺真菌 劑’例如一或多種來自如上所述之群A)至F)之殺真菌劑, 及(若需要)一種合適之溶劑或固體載劑的混合物。尤其關 注彼等混合物’因為在同一施用率下,其中很多混合物展 示對抗有害真菌之更高功效。此外’以化合物I、II及/或 IV及至少_種來自如上所述之群A)至之殺真菌劑的混合 物對抗有害真菌比以個別化合物I、II或IV或來自群A)至F) 之個別殺真菌劑對抗彼等真菌更有效。藉由施用化合物 I S ] 149026.doc -166- 201103429 I、II及/或IV連同至少一種來自群A)至】:)之活性物質,可獲 得協同效應’亦即’獲得的不僅僅係個別效應之簡單相加 (協同混合物)。 根據本發明,施用化合物t或^連同至少另一種 活性物質應理解為表示至少 一種式I、II及/或IV之化合物 及至少另-種活性物質以殺真时效量同時出現在作用點 (亦即,受到防治的有害真菌或其樓息地,諸如受感毕植 物、植物繁殖材料(尤其種子)、表面、材料或土壤以及經 保護以免受真菌侵襲之植物、植物繁殖材料(尤其種子)、 土壤、表面、材料或房間)。可藉由同時(聯合(例如以槽内 混合製劑形式)或分別)或連續施用化合物〗、11及/或1、及至 少另-種活性物質完成此操作,《中介於個別施用之間的 時間間隔經選擇以確保首先施用之活性物質在施用另一活 性物質之時仍以^夠量出現在作用點、施用順序對本發明 之實施並不重要。 在元混。物(亦即包含一種化合物I、II或IV(組份1)及 另一活性物質(組份2)(例如,來自群八⑷)之活性物質)的 本發明組合物)_ ’组份!與組份2之重量比一般視所用活 性物質之性質而定’通常在1:100至100:1之範圍内,經常 在1.50至50:1之範圍内,較佳在1:2〇至2〇1之範圍内更 佳在1:10至1():1之範圍内且尤其在i⑴]之範圍内。 在二兀混合物(亦即包含一種化合物1(組份1)及第一其他 活性物質(組份2)及第:其他活性物f (組份糊如,來自 群A)至Ό之兩種活性物質)的本發明組合物)中,組份i與組 149026.doc -167- 201103429 份2之重量比視所用活性物質之性質而定,較佳在丨:5〇至 50:1之範圍内且尤其在1:10至10:1之範圍内,且組份1與組 份3之重量比較佳在1:50至5〇:1之範圍内且尤其在1:1〇至 1 〇: 1之範圍内。 該等組份可個別使用或已部分或完全彼此混合以製備本 發明組合物。其亦可能另外包裝為組合組合物(諸如分裝 部分之套組)且使用。 在本發明之一實施例中,套組可包括一或多種(包括所 有)可用以製備本發明之農用化學組合物的組份。例如, 套組可包括一或多種殺真菌劑組份及/或佐劑組份及/或殺 蟲劑組份及/或生長調節劑組份及/或除草劑。可能已將一 或多種組份合併在一起或預調配。在套組中提供兩種以上 組份之彼等實施例中,可將組份合併在一起,因而包裝於 單個容器(諸如小瓶、瓶子、罐子、+袋、袋子或小罐) t。在其他實施例中,可分別包裝套組之兩種或兩種以上 組伤,亦即不進行預調配。因而,套組可包括一或多個單 獨的容器’諸如小瓶'罐子、瓶子、小袋、袋子或小罐, 各容器含有農用化學組合物之單獨組份。在兩種形式下, 套組之組份可與其他組份分開或連同其他組份一起施用或 作為用於製備本發明組合物的本發明组合組合物之組份來 施用。 使用者通常由預劑量裝置、背負式喷霧器、喷淋槽或喷 灑飛機來施用本發明組合物。此處,以水及/或緩衝液使 農用化學組合物補足達到所需施用濃度,適當時可能添加 I49026.doc -168- 201103429 其他助劑,由此獲得本發明之gp田〗 — 月 &lt; 即用型噴灑液或農用化學組 合物。通常,每公頃農業有效面并 β双曲積施用50至500公升即用 型噴灑液,較佳100至400公升。 根據-實施例,可由使用者本人於噴淋槽中混合本發明 . 組合物之個別組份(諸如套組之部分或二元或三元混合物 之部分)且(若適當)可添加其他助劑(槽内混合)。 在另-實施例中,可由使用者於喷淋槽中混合本發明組 合物之個別組份或部分預混合組份(例如,包含化合物工' II及/或IV及/或來自群八)至1}之活性物質的組份)且(若適 當)可添加其他助劑及添加劑(槽内混合)。 在另一實施例中,可聯合(例如在槽内混合之後)或連續 地施用本發明組合物之個別組份或部分預混合組份(例 如,包含化合物I、II及/或IV及/或來自群八彡至!)之活性物 質的組份)。 亦較佳為包含化合物I、II及/或IV(組份1)及至少一種選 自群A)之嗜毬果傘素(組份2)且尤其選自亞托敏、地莫菌 胺、氟氧菌胺、克收欣、奥瑞菌胺 '啶氧菌胺、唑菌胺酯 及月亏菌酯的活性物質之混合物。 亦較佳為包含化合物I、II及/或IV(組份1)及至少一種選 自群B)之羧醯胺類(組份2)且尤其選自必殺吩、博克利、森 達先、環醯菌胺、滅達樂、異σ比贊、甲霜靈、吱醯胺、達 滅芬、氟嗎啉、氟吡菌胺(匹克苯甲咪)、氯笨醯胺、加普 胺、雙炔醯菌胺(mandipropamid)及Ν-(3,,4',5'-三氟聯苯-2-基)-3-二氟曱基-1-甲基_1Η_吡唑_4_甲醯胺的活性物質之混 149026.doc •169· 201103429 合物。 較佳為包含式1、11及/或1v之化合物(組份1)及至少一種 群)之生類(組份2)且尤其選自環克唾、苯醚甲環唾、 亂壤唑、氟奎康唑、氟矽唑、護汰芬、葉菌唑、麥環丁 尼潘康唑、丙環唑、丙硫醇克唑、三泰芬、三泰隆、得 克利、、環菌唾、撲克拉、赛座滅、苯龍、貝芬 替及乙噻博胺的活性物質之混合物。 亦較佳為包含化合物I、π及/或IV(組份1)及至少一種選 自群D)之雜環化合物(組份2)且尤其選自扶吉胺、西波 定、芬瑞莫、米潘尼比林、比利美沙尼、赛福寧、護汰 ^馬菌靈、粉鐵琳、十三嗎啉、苯鏽啶、依普同、免克 卞、噁唑菌酮、咪唑菌酮、噻菌靈、普奎那茲、酸化笨并 噻二唑-s-甲酯、四氣丹、福爾培、禾草靈、快諾芬及5_乙 基-6-辛基-[1,2,4]三唑并[u — a]嘧啶_7_基胺的活性物質之 混合物。 亦較佳為包含化合物j、π及/或1¥(組份丨)及至少一種選 自群E)之胺基曱酸酯(組份2)且尤其選自代森錳鋅、代森 聯、丙森鋅、福美雙、纈黴威、苯噻瓦利及霜黴威的活性 物質之混合物。 亦較佳為包含化合物I、Π及/或IV(組份1)及至少一種選 自群F)中給出之殺真菌劑(組份2)且尤其選自腈硫醌、三笨 錫鹽(諸如三苯醋錫)' 三乙鱗酸、三乙膦酸銘、H3Pq3&amp; 其鹽、百菌清、益發靈、曱基多保淨、乙酸銅、氫氡化 銅、氯氧化銅、硫酸銅、硫、霜脲氰、美曲芬諾及螺環菌 149026.doc -170· 201103429 胺的活性物質之混合物。 因此,本發明此外係關於包含化合物I、Π及/或IV(組份 1)及另一活性物負(組份2)之組合物’該另一活性物質係選 自表B之B-1至B-3 46列之「組份2」行。 另一實施例係關於表B中所列之組合物B _ 1至b _ 3 4 6,其 中表B之一列在各情況下對應於包含一種本說明書之個別 化式I、II或IV之化合物(組份1)及相關列中所述之來自群 A)至I)之各別其他活性物質(組份2)的殺真菌組合物。較佳 地,所述組合物包含協同有效量之活性物質。 表B :包含一種個別化化合物I、Π或IV及另一來自群A) 至I)之活性物質的組合物 混合物 組份1 組份2 B-1 一種個別化化合物I、II或IV 亞托敏 '—- B-2 一種個別化化合物I、II或IV —渑莫菌胺 -— B-3 一種個別化化合物I、II或IV 烯肟菌酯 B-4 一種個別化化合物I、II或IV 氟氧菌胺 B-5 一種個別化化合物I、II或IV 克收欣 ~~- B-6 一種個別化化合物I、II或IV 苯氧菌胺 ' B-7 一種個別化化合物I、II或IV 奥瑞菌胺 -- B-8 一種個別化化合物I、II或IV 長氧菌胺 --- B-9 一種個別化化合物I、II或IV 百克敏 — B-10 一種個別化化合物I、II或IV 吡瑞苯卡 _-- B-11 一種個別化化合物1、U或IV 三氟敏 ~ '--~~~ B-12 一種個別化化合物I、II或IV 2-(2-(6-(3-氣·2-曱墓-苯 嘧啶-4-基氧基)-苯基)-2-曱氧基亞胺 基-N-甲基-乙醢胺 B-13 一種個別化化合物I、Π或IV 2-(鄰-((2,5-一曱基笨基-氧亞甲基)笨 基)-3-曱氧基-丙稀酸(acrylsaure)甲 酯 B-14 一種個別化化合物I、Π或IV 3-曱氧基-2-(2-(N-(4-曱氧基-苯基)-環丙烷曱醯亞胺基硫基甲基)·笨基)· 丙稀酸曱醋 149026.doc -171 - 201103429 混合物 組份1 組份2 B-15 一種個別化化合物I、II或IV 2-(2-(3-(2,6-二氣苯基)-1-曱基-亞烯 丙基胺基氧基曱基)-苯基)-2-曱氧基 亞胺基-N-甲基-乙醯胺 B-16 一種個別化化合物I、II或IV 苯霜靈 B-17 一種個別化化合物I、II或IV 苯霜靈-M B-18 一種個別化化合物I、II或IV 麥鏽靈 B-19 一種個別化化合物I、II或IV 必殺吩 B-20 一種個別化化合物I、II或IV 博克利 B-21 一種個別化化合物I、II或IV 萎鑛靈 B-22 一種個別化化合物I、II或IV 曱呋醯胺 B-23 一種個別化化合物I、II或IV 環醯菌胺 B-24 一種個別化化合物I、II或IV 氟多寧 B-25 一種個別化化合物I、II或IV 福拉比 B-26 一種個別化化合物I、II或IV 異°比贊 B-27 一種個別化化合物I、II或IV 異噻菌胺 B-28 一種個別化化合物I、II或IV 克拉昔 B-29 一種個別化化合物I、II或IV 滅鏽胺 B-30 一種個別化化合物I、II或IV 滅達樂 B-31 一種個別化化合物I、II或IV 滅達樂-M B-32 一種個別化化合物I、II或IV 咬醯胺 B-33 一種個別化化合物I、II或IV 歐殺斯 B-34 一種個別化化合物I、II或IV 氧化萎鏽靈 B-35 一種個別化化合物I、II或IV 吡噻菌胺 B-36 一種個別化化合物I、II或IV 森達先 B-37 一種個別化化合物I、II或IV 克枯爛 B-38 一種個別化化合物I、II或IV 赛氟滅 B-39 一種個別化化合物I、II或IV 汰敵寧 B-40 一種個別化化合物I、II或IV 2-胺基-4-曱基-α塞嗤-5-曱酿苯胺 B-41 一種個別化化合物I、II或IV 2-氣-N-(l,l,3-二曱基-滿-4·基)-終 驗酿胺 B-42 一種個別化化合物I、Π或IV N-(3',4',5L三氟聯苯-2-基)-3-二氟甲 基-1-曱基-1H-吡唑-4-曱醯胺 B-43 一種個別化化合物I、II或IV N-(4L二氣曱基硫基聯苯-2_基)-3-二 氟甲基-1-曱基比唑-4-甲醯胺 B-44 一種個別化化合物I、II或IV N-(2-(l,3-二甲基-丁基)-苯基)-1,3-二 甲基-5-氟-1H-。比。坐-4-曱醯胺 B-45 一種個別化化合物I、II或IV 队(2-(1,3,3-三曱基-丁基)-笨基)-1,3-二甲基-5-氟-1H-吡唑-4-甲醯胺 B-46 一種個別化化合物I、II或IV 、土》Λ» Λ#· 達滅分 B-47 一種個別化化合物I、II或IV 氟嗎琳 B-48 一種個別化化合物I、II或IV 丁0比嗎喻 B-49 一種個別化化合物I、Π或IV 氟美醯胺 B-50 一種個別化化合物I、II或IV 氟0比菌胺 [si 149026.doc -172- 201103429 混合物 組份1 組份2 B-51 一種個別化化合物I' II或IV 氟吡胺 B-52 一種個別化化合物I、II或IV 氣苯醯胺 B-53 一種個別化化合物I、II或IV N-(3-乙基-3,5,5-三曱基-環己基)-3-曱醯基胺基-2-羥基-苯甲醯胺 B-54 一種個別化化合物I、II或IV 加普胺 B-55 一種個別化化合物I、II或IV 二氯西莫 B-56 一種個別化化合物I、II或IV 雙炔醯菌胺 B-57 一種個別化化合物I、II或IV 土黴素 B-58 一種個別化化合物I、II或IV 石夕硫芬(Silthiofam) B-59 一種個別化化合物I、II或IV N-(6-甲氧基-°比咬-3-基)環丙烧曱酸 醯胺 B-60 一種個別化化合物I、II或IV 阿紮康唑 B-61 一種個別化化合物I、II或IV 比多農 B-62 一種個別化化合物I、II或IV 溴克唑 B-63 一種個別化化合物I、II或IV 環克嗤 B-64 一種個別化化合物I、II或IV 苯醚甲環唑 B-65 一種個別化化合物I、II或IV 二硝康唑 B-66 一種個別化化合物I、II或IV 二硝康嗤-M B-67 一種個別化化合物I、II或IV 氟環嗤 B-68 一種個別化化合物I、II或IV 芬布康嗤 B-69 一種個別化化合物I、II或IV 氟奎康唑 B-70 一種個別化化合物I、II或IV 氟矽唑 B-71 一種個別化化合物I、II或IV 護汰芬 B-72 一種個別化化合物I、II或IV 六康唾 B-73 一種個別化化合物I、II或IV 亞胺唑 B-74 一種個別化化合物I、II或IV 依普克唑 B-75 一種個別化化合物I、Π或IV 葉菌唑 B-76 一種個別化化合物I、II或IV 麥環丁尼 B-77 一種個別化化合物I、II或IV 嗯。米。坐 B-78 一種個別化化合物I、II或IV 巴克素 B-79 一種個別化化合物I、II或IV 潘康。坐 B-80 一種個別化化合物I、II或IV 丙環。坐 B-81 一種個別化化合物I、II或IV 丙硫醇克唑 B-82 一種個別化化合物I、II或IV 矽氟唑 B-83 一種個別化化合物I、II或IV 得克利 B-84 一種個別化化合物I、II或IV 氟醚嗤 B-85 一種個別化化合物I、II或IV 三泰芬 B-86 一種個別化化合物I、II或IV 三泰隆 B-87 一種個別化化合物I、II或IV 環菌。坐 B-88 一種個別化化合物I、II或IV 稀效°坐 B-89 一種個別化化合物I、II或IV 1 -(4-氯-苯基)-2-([ 1,2,4]三唑-1 -基)-環庚醇 B-90 一種個別化化合物I、II或IV #座滅 149026.doc •173- 201103429 混合物 組份1 組份2 B-91 一種個別化化合物I、Π或IV 依滅列 B-92 一種個別化化合物I、II或IV 依滅列硫酸鹽 B-93 一種個別化化合物I、II或IV 稻瘟酯 B-94 一種個別化化合物I、II或IV 撲克拉 B-95 一種個別化化合物I、II或IV 賽福座 B-96 一種個別化化合物I、II或IV 苯菌靈 B-97 一種個別化化合物I、II或IV 貝芬替 B-98 一種個別化化合物I、II或IV 麥穗靈 B-99 一種個別化化合物I、II或IV 噻苯咪唑 B-100 一種個別化化合物I、Π或IV 乙噻博胺 B-101 一種個別化化合物I、II或IV 依得利 B-102 一種個別化化合物I、II或IV 噁黴靈 B-103 一種個別化化合物I、II或IV 2-(4-氯-苯基)-N-[4-(3,4-二甲氧基-苯 基)·異°惡°坐-5-基]-2-丙-2-快基氧基-乙醯胺 B-104 一種個別化化合物I、II或IV 扶吉胺 B-105 一種個別化化合物I、II或IV 比芬諾 B-106 一種個別化化合物I、II或IV 3-[5-(4-氣-苯基)-2,3-二甲基-異噁唑 0定-3-基]-α比咬 B-107 一種個別化化合物I、II或IV 3-[5-(4-甲基-苯基)-2,3-二甲基-異噁 σ坐咬-3-基]-°比。定 B-108 一種個別化化合物I、II或IV 2,3,5,6-四氯-4-甲磺醯基-吡啶 B-109 一種個別化化合物I、II或IV 3,4,5-三氯比啶-2,6-二甲腈 B-110 一種個別化化合物I、II或IV N-(l-(5_ &gt;臭-3-氯-π比咬-2-基)-乙基)-2,4-二氯_菸鹼醯胺 B-lll 一種個別化化合物I、II或IV Ν-((5-漠-3-氯-°比°定-2-基)-甲基)-2,4-二氯-菸鹼醯胺 B-112 一種個別化化合物I、II或IV 磺嘧菌靈 B-113 一種個別化化合物I、II或IV 西波定 B-114 一種個別化化合物I、II或IV 二氟林 B-115 一種個別化化合物I、II或IV 芬瑞莫 B-116 一種個別化化合物I、II或IV 嘧菌腙 B-117 一種個別化化合物I、Π或IV 米潘尼比林 B-118 一種個別化化合物I、II或IV 氯啶 B-119 一種個別化化合物I、II或IV 氟苯嘧啶醇 B-120 一種個別化化合物I、II或IV 比利美沙尼 B-121 一種個別化化合物I、II或IV 赛福寧 B-122 一種個別化化合物I、II或IV 拌種咯 B-123 一種個別化化合物I、II或IV 護汰寧 B-124 一種個別化化合物I、II或IV 阿迪嗎琳 B-125 一種個別化化合物I、II或IV 嗎菌靈 B-126 一種個別化化合物I、II或IV 乙酸嗎菌靈 B-127 一種個別化化合物I、II或IV 粉鏽啉 [si 149026.doc •174- 201103429 混合物 M份1 組份2 -- B-128 一種個別化化合物I、Π或IV 十三嗎淋 --- B-129 一種個別化化合物I、II或IV 苯鏽啶 B-130 一種個別化化合物I、II或IV 亂酿亞胺 __ B-131 一種個別化化合物I、Π或IV 依普同 ---- B-132 一種個別化化合物I、II或IV 撲滅寧 — B-133 一種個別化化合物I、II或IV 免克寧 __— B-134 一種個別化化合物I、II或IV 鳴唾菌酮 -- B-135 一種個別化化合物I、Π或IV σ米σ坐菌酮 B-136 一種個別化化合物I、II或rv 氟多寧 __— B-137 一種個別化化合物I、Π或IV 辛嗟闺 B-138 一種個別化化合物I、Π或IV 噻菌靈 —_— B-139 一種個別化化合物I、II或rv 5-胺基-2-異-丙基-4-鄰-甲苯基-2,j-二氫-吡唑-1 -硫代甲酸s-烯丙醋 B-140 一種個別化化合物I、II或IV 酸化苯并噻二吐-s-甲酯 - B-141 一種個別化化合物I、Π或IV 吲唑磺菌胺 B-142 一種個別化化合物I、II或rv 敵菌靈 __ B-143 一種個別化化合物I、II或rv 殺稻瘟素-S B-144 一種個別化化合物I、Π或IV 四氣丹 B-145 一種個別化化合物I、Π或IV 蓋普丹 B-146 一種個別化化合物I、Π或IV 滅蟎猛 B-147 一種個別化化合物I、Π或IV 邁隆 B-148 一種個別化化合物I、II或IV 咪菌威 B-149 一種個別化化合物I、Π或IV 噠菌清 B-150 一種個別化化合物I、Π或IV 苯敵快 B-151 一種個別化化合物I、II或IV 甲基硫酸苯敵快 B-152 一種個別化化合物I、π或rv 禾草靈 B-153 一種個別化化合物I、Π或IV 福爾培 B-154 一種個別化化合物I、Π或IV 草酸(OxolinsSure) B-155 一種個別化化合物I、Π或IV 粉病靈 B-156 一種個別化化合物I、II或IV 普奎那茲 ~~— B-157 一種個別化化合物I、Π或IV 百快隆 -- B-158 一種個別化化合物I、II或IV 7夬諾芬 ' ~~~— B-159 —種個別化化合物I、II或IV 咪唑嗪 — B-160 一種個別化化合物I、II或rv 三賽唑 — B-161 一種個別化化合物I、Π或IV 2-丁氡基·6-蛾-3-丙基·咬煤 B-162 一種個別化化合物I、Π或IV 曱基-1Η-苯并咪唑 B-163 一種個別化化合物I、II或IV 5-氣-7-(4-曱基-0底咬 三氟-苯基⑷训三。坐并 B-164 一種個別化化合物I、Π或IV 5-乙基-6·辛基·[〗,2,4]三 嘧咬-7-基胺 [,5'a] B-165 一種個別化化合物I、Η或IV 福美鐵 — B-166 一種個別化化合物I、Π或IV 錳鋅 -175· 149026.doc 201103429 混合物 組份1 組份2 B-167 一種個別化化合物I、II或IV 代森猛 B-168 一種個別化化合物I、II或IV 威百故 B-169 一種個別化化合物I、Π或IV 確菌威 B-170 一種個別化化合物I、II或IV 代森聯 B-171 一種個別化化合物I、II或rv 丙森鋅 B-172 一種個別化化合物I、II或IV 福美雙 B-173 一種個別化化合物I、II或rv 代森鋅 B-174 一種個別化化合物I、II或IV 福美辞 B-175 一種個別化化合物I、II或IV 乙黴威 B-176 一種個別化化合物I、II或IV 苯噻瓦利' B-177 一種個別化化合物I、Π或IV 纈黴威 B-178 一種個別化化合物I、Π或IV 霜黴威 B-179 一種個別化化合物I、Π或IV 霜黴威鹽酸鹽 B-180 一種個別化化合物I、Π或IV 威立芬那 B-181 一種個別化化合物I、II或IV N-(l-(l-(4-氰基苯基)乙磺醯基)-丁-2-基)胺基曱酸-(4-氟笨基)酯 B-182 一種個別化化合物I、II或rv 多寧 B-183 一種個別化化合物I、Π或IV 多寧游離鹼 B-184 一種個別化化合物I、Π或IV 雙胍辛 B-185 一種個別化化合物I、II或IV 雙胍辛乙酸鹽 B-186 一種個別化化合物I、π或rv 雙胍辛胺 B-187 一種個別化化合物I、II或rv 雙胍辛胺三乙酸鹽 B-188 一種個別化化合物I、II或IV 克熱淨(烷苯績酸鹽) B-189 一種個別化化合物I、II或IV 春曰黴素 B-190 一種個別化化合物I、II或IV 春曰黴素鹽酸鹽水合物 B-191 一種個別化化合物I、II或IV 多氧菌素 B-192 一種個別化化合物I、II或IV 鏈黴素 B-193 一種個別化化合物I、II或rv 有效黴素A B-194 一種個別化化合物I、II或IV 百蟎克 B-195 一種個別化化合物I、π或IV 氣硝胺(Dicloran) B-196 一種個別化化合物I、II或rv 大脫蟎 B-197 一種個別化化合物I、II或IV 白粉克 B-198 一種個別化化合物I、II或IV 酞菌酯 B-199 一種個別化化合物I、II或rv 四氣硝基苯 B-200 一種個別化化合物I、π或rv 三苯錫鹽 B-201 一種個別化化合物I、II或IV 腈硫醌 B-202 一種個別化化合物I、II或IV 稻瘟靈 B-203 一種個別化化合物I、π或rv 護粒松 B-204 一種個別化化合物I、II或rv 三乙膦酸、三乙膦酸鋁 B-205 一種個別化化合物I、π或IV 丙基喜樂松 B-206 一種個別化化合物I、π或IV 磷酸(h3po3)及衍生物 B-207 一種個別化化合物I、Π或IV 白粉松 B-208 一種個別化化合物I、π或rv 脫克松 [si 149026.doc •176- 201103429 混合物 組份1 組份2 B-209 一種個別化化合物I、II或IV 百菌清 B-210 一種個別化化合物I、II或IV 益發靈 B-211 一種個別化化合物I、II或IV 雙氣酚 - B-212 一種個別化化合物I、Π或IV 氟硫滅 — B-213 一種個別化化合物I、Π或IV 六氣幕 B-214 一種個別化化合物I、II或IV 賓-克隆 ~- B-215 一種個別化化合物I、Π或IV 五氣盼及其鹽 B-216 一種個別化化合物I、II或IV 苯酞 _ 一~ B-217 一種個別化化合物I' II或IV 奎脫辛~~' —- B-218 一種個別化化合物I、II或IV 甲基多保淨 B-219 一種個別化化合物I、II或IV 甲基益發靈 B-220 一種個別化化合物I、Π或IV Ν-(4-氯-2-硝基-苯基)-Ν-乙基-4-甲 基-苯續酿胺 B-221 一種個別化化合物I、II或IV 波爾多液 B-222 一種個別化化合物I、II或IV 乙酸銅 B-223 一種個別化化合物I、II或IV 氫氧化銅 B-224 一種個別化化合物I、II或IV 氣氧化銅 — B-225 一種個別化化合物I、Η或IV Γ驗式硫酸銅 B-226 一種個別化化合物I、II或IV B-227 一種個別化化合物I、Π或IV 聯笨 - B-228 一種個別化化合物I、II或IV 溴硝醇~~ -- B-229 一種個別化化合物I、II或IV 噻芬胺 B-230 一種個別化化合物I、II或IV 霜脲氰 B-231 一種個別化化合物I、Π或IV 二笨胺 B-232 一種個別化化合物I、Π或IV 奚曲芬諾 B-233 一種個別化化合物I、II或IV _滅粉蘇 ~~ B-234 一種個別化化合物I、II或IV 經基啥淋銅 B-235 一種個別化化合物I、II或IV 調環酸鈣 B-236 一種個別化化合物I、II或IV 螺環菌胺 B-237 一種個別化化合物I、Π或IV B-238 一種個別化化合物I、II或IV Ν-(環丙基曱氧基亞胺基·(6_二氟曱 氧基·2,3-二氟-苯基)-甲基)-2-笨基乙 醯胺 B-239 一種個別化化合物I、Π或IV Ν'·(4-(4-氯-3-三氟曱基-笨氧基&gt;21 二曱基-苯基VN-乙基-Ν-曱基曱脒 B-240 一種個別化化合物I、Π或IV Ν'-(4-(4-氟-3-三氟曱基-苯氧基)-2,5-二曱基-笨基VN-乙基-Ν·曱基曱脒 B-241 一種個別化化合物I、Π或IV Ν'-(2_曱基-5-三氟曱基-4-(3-三曱基 矽烷基-丙氧基)-苯基)-N-乙基-N-甲 基甲脒 B-242 一種個別化化合物I、Π或IV 凡-(5-二氟甲曱基-4-(3-三甲基 矽烷基-丙氧基)-苯基)-N-乙基-N-甲 基甲脒 149026.doc -177· 201103429 混合物 組份1 組份2 B-243 一種個別化化合物I、II或IV 2-{1-[2-(5-曱基-3-三氟甲基-吡唑-1-基)-乙醯基]-哌啶-4-基}-噻唑-4-曱酸 曱基_(1,2,3,4_四氮-奈-1-基)-酿胺 B-244 一種個別化化合物I、II或IV 2-{1-[2-(5-甲基-3-三氟曱基-吡唑-1-基)-乙醯基]-哌啶-4-基}-噻唑-4-曱酸 甲基-(R)-l,2,3,4-四氮-蔡-1·基-酿胺 B-245 一種個別化化合物I、II或IV 乙酸6-第三丁基-8-敗-2,3·二曱基啥 琳-4-基酉旨 B-246 一種個別化化合物I、II或IV 曱氧基-乙酸6-第三丁基-8-氟-2,3-二 甲基-哇嚇&gt;-4-基醋 B-247 一種個別化化合物I、II或IV 加保利 B-248 一種個別化化合物I、II或IV 加保扶 B-249 一種個別化化合物I、II或IV 丁基加保扶 B-250 一種個別化化合物I、II或IV 納乃得硫雙威 B-251 一種個別化化合物I、II或IV 畢芬寧 B-252 一種個別化化合物I、II或IV 賽扶寧 B-253 一種個別化化合物I、II或IV 赛滅寧 B-254 一種個別化化合物I、II或IV 亞滅寧 B-255 一種個別化化合物I、II或IV ζ-氣氛菊S旨 B-256 一種個別化化合物I、II或IV 第滅寧 B-257 一種個別化化合物I、II或IV 益化利 B-258 一種個別化化合物I、Π或IV λ-赛洛寧 B-259 一種個別化化合物I、II或IV 百滅寧 B-260 一種個別化化合物I、II或IV 七氟菊酯 B-261 一種個別化化合物I、II或IV 二福隆 B-262 一種個別化化合物I、II或IV 氟芬隆 B-263 一種個別化化合物I、II或IV 祿芬隆 B-264 一種個別化化合物I、II或IV 得福隆 B-265 一種個別化化合物I、II或IV 螺蟲乙酯 B-266 一種個別化化合物I、II或IV 可尼丁 B-267 一種個別化化合物I、II或IV ϋ夫蟲胺 B-268 一種個別化化合物I、II或IV 益達胺 B-269 一種個別化化合物I、II或IV 噻蟲嗪 B-270 一種個別化化合物I、Π或IV 咬蟲月东 B-271 一種個別化化合物I、II或IV 。塞蟲琳 B-272 一種個別化化合物I、II或IV 硫丹 B-273 一種個別化化合物I、Π或IV 芬普尼 B-274 一種個別化化合物I、II或IV 阿巴汀 B-275 一種個別化化合物I、II或IV 因滅汀 B-276 一種個別化化合物I、II或IV 賜諾殺 B-277 一種個別化化合物I、II或IV 斯平托蘭 B-278 一種個別化化合物I、II或IV 伏蟻腙 B-279 一種個別化化合物I、II或IV 蟲蟎腈[SI 149026.doc -160- 201103429 Pyroxasulfone, pyrocycline (pyroxsulam); Other: Amine. Take amicarbazone and amine III. Sit, anilofos, beflubutamid, ben-azolin, bencarbazone, benflu-resate, bisflurone Benzofenap), bentazone, benzobicyclon, bromacil, bromobutide, butafenacil, butamifos, Cafenstrole, ° sitting brewing | Carfentrazone, cinidon-ethlyl, chlorthal, cinmethylin, can be eliminated ( Clomazone), cumyluron, °cyprosulfamide, dicamba, difenzoquat, diflufenzopyr, Helicobacter sphaeroides )rec/^/era monoceras), grass 0 more endothal, ethofumesate, etobenzanid, fentrazamide, amylamine Flumiclorac-pentyl, flumioxazin, flubenzol, fluchaxam, flurochl Oridone), flurtamone, indanofan, isoxaben, isoxaflutole, lenacil, propanil, pent Propyzamide, quinclorac, quinmerac, mesotrione, decyl decanoic acid, naptalam, propane oxacillin (oxadiargyl), oxadiazon, oxazinone 149026.doc -161 - 201103429 (oxaziclomefone), pentoxazone, pinoxaden, oxazolidine (pyraclonil), pyraflufen-ethyl, pyraflufen-ethyl. More than tori (pyrasulfotole), pyrazoxyfen, yala. Pyrazolynate, quinocal, sulcotrione, sulfentrazone, terbacil, tefuryltrione ), tembotrione, °thiencarbazone, topramezone, 4-hydroxy-3-[2-(2-decyloxy-ethoxyindolyl)_ 6-trifluoromethylpyridin-3-carbonyl]-bicyclo[3.2.1]oct-3-en-2-one, (3-[2- gas-4-fluoro-5-(3-indolyl)- 2,6-di-oxy-4-dioxamethyl-3,6-diaza-2Η-σ-[beta]-1-yl)-indolyl]pyredo-2-yloxy)-acetic acid乙酉,6-Amino-5-Ga-2 -ί哀propyl- °3⁄4°定-4-carboxylic acid vinegar, 6-gas-3_(2-cyclopropyl-6-methyl-phenoxy )-pyridazin-4-ol, 4-amino-3-gas-6-(4-a-phenyl)-5.fluoro-pyridine-2-carboxylic acid, 4-amino-3-gas-6- (4-Ga-2·Fluoro-3-indolyl-phenyl)-pyridin-2-indole decyl ester and 4-amino-3-chloro-6-(4- gas-3-dimethylamine Ethyl-2-fluoro-phenyl)-pyridine-2-decanoate. I) Insecticides - Organic (thio) acid salts: acephate, azamethiphos, azinphos-methyl, chlorpyrifos, strontium Chlorpyrifos-methyl, chlorfenvinphos, dizinon, dichlorvos, dicrotophos, dimethoate, disulfoton , ethion, sputum-162- 149026.doc 201103429 (fenitrothion), fenthion, isoxathion, malathion, methamidophos, methadinion ), methyl-parathion, mevinphos, monocrotophos, oxydemeton-methyl &gt; paraoxon, parathion , phenthoate, phosalone, phosmet, phosphamidon, phorate, phoxim, pirimiphos-methyl , profenofos, prothiofos ), sulprophos, tetrachlorvinphos, terbufos, triazophos, trichlorfon; - urethane for the purpose: alanycarb , aldicarb, bendiocarb 'benfuracarb, carbaryl, carbofuran, carbosulfan, fenoxycarb , furathiocarb, metiocarb, methodyl, oxamyl, pirimicarb, propoxur, thiodicarb, ° Sitting on triazamate; - pyrethroid: acryl pyrethrum (allethrin) bifenthrin, cyfluthrin, cyhalothrin, cyphenothrin, race Nyper (cypermethrin), α-saidingin, β-saidingin, zeta-cypermethrin, deltamethrin, esfenvalerate 'etofenprox, fen Puning 149026.doc -163- 201103429 (fenpropathrin) &gt; Fenvalerate, Epnin ( Imiprothrin), lambda cyhal〇thrin, permethrin, praUethrin, pyrethrin I and II, resmethHn, fluoroquinone Silamfluofen, tau_fiuvaiinate, tefluthrin, tetramethrin, tralmethrin, transfiuthrin, propyl i chrysanthemum (profluthrin), PTFE, dimethfluthrin; - insect growth regulator: a) chitin synthesis inhibitor: benzoylureas, chifu rfiuazuron, race Cyramazin - diflubenzuron, flucycloxuron, flufenoxuron, hexaflumuron, lufenuron, novaluron, defolon Teflubenzuron), triflumuron; buprofezin, diofenolan, hexythiazox, etoxazole, clofentazine; b) ecdysone antagonism Agent: hafenofozide, methoxyfenozide, defenof Tebufenozide), azadirachtin; c) juvenile hormone analogues: pyriproxyfen, metopor, fenolect; d) lipid biosynthesis inhibitors: Spirodiclofen), spiromesifen, spirotetramat; - nicotinic receptor agonist/antagonist compound: cotinine 149026.doc 201103429 (clothianidin), bituminamine (dinotefuran) ), imidacloprid, thiamethoxam, nitenpyram, acetamiprid, thiacloprid, 1- (2-Chlorosine- 5-ylmethyl)-2-stone succinimido-3,5-diindolyl-[1,3,5]triazine; -GABA antagonist compound: endosulfan, ethiprole , fipronil, vaniliprole, pyrafluprole, pyriprole, 5-amino-1-(2,6-dichloro-4-methyl-benzene Base 4-aminosulfinyl-1H-pyrazole-3-thiodecanoic acid decylamine; - macrocyclic vinegar insecticide: aba; adam (abamectin), emtermectin (ememectin), dense Miltmectin Lepimectin, spinosad, spinetoram; - mitochondrial electron transport inhibitor (METI) I acaricide: fenazaquin, pyridaben, Tebufenpyrad, tolfenpyrad, flufenerim; -METI II and III compounds: acequinocyl, fluacyprim, hydramethylnon ; - Uncoupling agent: chlorfenapyr; - oxidative phosphorylation inhibitors: cyhexatin, diafenthiuron, fenbutatin oxide, propargite; 149026.doc -165- 201103429 - Fracturing agent compound. Cryomazine; - Mixed functional oxidation inhibitor: piperonyl butoxide &gt; - Sodium channel blocker. Indoxacarb ( Indoxacarb), metaflumizone ί - other · Benkeeze (benclothiaz), bifenazate, catapap, dr〇nicamid, ° (pyridalyl), pymetrozine ' thio, thiocyclam, blessing Flubendiamide, chitrantraniliprole, cyanidin receptor (cyazypyr, HGW86), cyenopyrafen, cyenopyrafen. Compared with I, fiupyrazofos, 0 cyflumetofen, amid 〇 fiumet 'imicyafos, bistrifluron and bistrifluron. Pyrifluquinazon ° The present invention further relates to an agrochemical composition comprising at least one compound I, II and/or IV (component hydrazine) and at least one other active substance suitable for plant protection (for example, Selected from Groups A) to 1)) (Component 2), especially another fungicide such as one or more fungicides from Groups A) to F) as described above, and, if desired, a suitable A mixture of solvents or solid carriers. Particular attention is paid to their mixtures' because at the same application rate, many of them exhibit a higher efficacy against harmful fungi. Furthermore, the mixture of the fungicides of the compounds I, II and/or IV and at least _ from the group A as described above against the harmful fungi is compared to the individual compounds I, II or IV or from the groups A) to F) Individual fungicides are more effective against their fungi. By administering the compound IS ] 149026.doc -166- 201103429 I, II and/or IV together with at least one active substance from groups A) to :), a synergistic effect can be obtained, ie not only individual effects are obtained Simple addition (collaboration mixture). According to the invention, the administration of the compound t or ^ together with at least one other active substance is understood to mean that at least one compound of the formula I, II and/or IV and at least one further active substance occur simultaneously at the point of action in the true-acting amount (also That is, harmful fungi or their habitats, such as susceptible plants, plant propagation materials (especially seeds), surfaces, materials or soil, and plants, plant propagation materials (especially seeds) that are protected from fungal attack, Soil, surface, material or room). This can be done by simultaneous (in combination (for example in the form of a mixed formulation in the tank) or separately) or by continuous application of the compound, 11 and/or 1, and at least another active substance, the time between individual administrations The interval is selected to ensure that the active substance applied first is still present at the point of action when the other active substance is applied, and the order of application is not critical to the practice of the invention. Mixed in the yuan. (i.e., a composition of the invention comprising a compound I, II or IV (component 1) and another active substance (component 2) (e.g., active from group VIII (4))) _ component! The weight ratio to component 2 generally depends on the nature of the active substance used, usually in the range of 1:100 to 100:1, often in the range of 1.50 to 50:1, preferably 1:2 to 2 More preferably, the range of 〇1 is in the range of 1:10 to 1 (): 1 and especially in the range of i(1)]. In the diterpene mixture (ie containing one compound 1 (component 1) and the first other active substance (component 2) and the: other active substance f (component paste, eg from group A) to the two activities of hydrazine In the composition of the invention), the weight ratio of component i to the group 149026.doc-167-201103429 part 2 depends on the nature of the active substance used, preferably in the range of 〇:5〇 to 50:1. And especially in the range of 1:10 to 10:1, and the weight of component 1 and component 3 is preferably in the range of 1:50 to 5〇:1 and especially in the range of 1:1〇 to 1 〇: 1 Within the scope. The components may be used individually or partially or completely mixed with each other to prepare the compositions of the present invention. It may also be additionally packaged as a combination composition (such as a kit of dispensing parts) and used. In one embodiment of the invention, the kit may include one or more (including all) components useful for preparing the agrochemical compositions of the present invention. For example, the kit may include one or more fungicide components and/or adjuvant components and/or insecticide components and/or growth regulator components and/or herbicides. One or more components may have been combined or pre-provisioned. In embodiments in which more than two components are provided in a kit, the components may be combined together and packaged in a single container (such as a vial, bottle, can, + bag, bag or can). In other embodiments, two or more sets of injuries may be packaged separately, i.e., no pre-distribution is performed. Thus, the kit can include one or more separate containers 'such as vial' cans, bottles, sachets, bags or cans, each containing a separate component of the agrochemical composition. In both forms, the components of the kit may be administered separately from the other components or together with the other components or as a component of the combination composition of the invention for use in preparing the compositions of the invention. The user typically applies the compositions of the present invention from a pre-dosing device, a knapsack sprayer, a spray tank or a spray aircraft. Here, the agrochemical composition is supplemented with water and/or a buffer to a desired application concentration, and if appropriate, I49026.doc-168-201103429 may be added, thereby obtaining the gp field of the present invention - month &lt; ready-to-use spray or agrochemical composition. Typically, 50 to 500 liters of ready-to-use spray fluid, preferably 100 to 400 liters, is applied per hectare of agriculturally effective surface and beta hyperbolic. According to an embodiment, the individual components of the composition (such as parts of a kit or portions of a binary or ternary mixture) may be mixed by the user himself in a spray tank and, if appropriate, other auxiliaries may be added. (mixed in the tank). In another embodiment, the individual components or portions of the pre-mixed components of the compositions of the present invention (eg, comprising Compounds 'II and/or IV and/or from Group 8) may be mixed by the user in a spray tank. 1} component of the active substance) and (if appropriate) other additives and additives (in-tank mixing) may be added. In another embodiment, the individual components or portions of the pre-mixed components of the compositions of the invention may be combined (eg, after mixing in a tank) or continuously (eg, comprising Compounds I, II, and/or IV and/or The components of the active substances from the group gossip to !)). Preference is also given to the inclusion of compounds I, II and/or IV (component 1) and at least one of the estrogens (component 2) selected from group A) and in particular from atoximin, toxix, A mixture of active substances of fluoxetamine, kexinxin, oryzanidin, oxymyrazine, pyraclostrobin and sulphate. Also preferably, it comprises a compound I, II and/or IV (component 1) and at least one carboxamide selected from the group B) (component 2) and is especially selected from the group consisting of fennel, bokley, sender, Cyclosporine, chlorhexidine, iso-sigzazin, metalaxyl, guanamine, daxen, flumorph, fluopyramine (picmidine), chloramphenicol, gupamine, Mandipropamid and Ν-(3,,4',5'-trifluorobiphenyl-2-yl)-3-difluorodecyl-1-methyl-1Η-pyrazole_4_ Mixture of active substances of methopea 149026.doc • 169· 201103429. Preferably, it comprises a compound of the formula 1, 11 and/or 1v (component 1) and at least one group (component 2) and is especially selected from the group consisting of cyclosporine, difenophene, spiroxazole, fluorine. Queconazole, fluoxazole, dimethoate, meconazole, dexamethasone, propiconazole, propylthioglycol, trimethoate, three tailong, dexke, cyclamate, poker A mixture of active substances of pull, racen, benzon, befenfen and ethipramine. Also preferably, it comprises a compound I, π and/or IV (component 1) and at least one heterocyclic compound selected from group D) (component 2) and is especially selected from the group consisting of chlorhexidine, simboldine and fenremore. ,Mippanicin, Billy Methani, Saifunin, Tiemar, Mamulin, Fen Tinglin, Tridemorpholine, Benzidine, Epto, Ethyl, Oxazone, Imidazole Ketone, thiabendazole, puquinaz, acidified stupid and thiadiazole-s-methyl ester, tetradone, fore, phlorin, vebufen and 5_ethyl-6-octyl-[ A mixture of 1,2,4]triazolo[u-a]pyrimidine-7-ylamine actives. It is also preferred to comprise the compound j, π and/or 1 ¥ (component 丨) and at least one amine decanoate selected from the group E) (component 2) and especially selected from the group consisting of mancozeb and desen , a mixture of active substances of zinc, zinc, thiram, carbendazim, phenthiali and propamocarb. Also preferably, it comprises a compound I, hydrazine and/or IV (component 1) and at least one fungicide (component 2) selected from the group F) and is especially selected from the group consisting of nitrile sulfonium and tribasic tin salts. (such as triphenyl vinegar) 'triethyl sulphate, triethylphosphonic acid ing, H3Pq3 &amp; its salt, chlorothalonil, Yifaling, thiopurine, copper acetate, copper hydride, copper oxychloride, sulfuric acid Copper, sulfur, cymoxanil, metribenol and spirobacteria 149026.doc -170· 201103429 A mixture of active substances of amines. Accordingly, the present invention is further directed to a composition comprising Compound I, hydrazine and/or IV (Component 1) and another active negative (Component 2) 'The other active substance is selected from Table B B-1 Go to the "Component 2" line in column B-3. Another embodiment relates to the compositions B _ 1 to b _ 3 4 6 listed in Table B, wherein one of the tables B is in each case corresponding to a compound comprising an individualized formula I, II or IV of the present specification (French 1) and the fungicidal compositions of the respective other active substances (component 2) from groups A) to I) as described in the relevant columns. Preferably, the composition comprises a synergistically effective amount of active material. Table B: Composition mixture comprising an individual compound I, hydrazine or IV and another active substance from groups A) to I) Component 1 Component 2 B-1 An individualized compound I, II or IV敏'-- B-2 an individualized compound I, II or IV - simianid--B-3 an individualized compound I, II or IV enestrobin B-4 an individualized compound I, II or IV fluoxetine B-5 an individualized compound I, II or IV 克收欣~~- B-6 an individualized compound I, II or IV phenoxybamine 'B-7 an individualized compound I, II Or IV orystatin-- B-8 an individualized compound I, II or IV-hyperoxybamine--- B-9 an individualized compound I, II or IV 100-sensitive - B-10 an individualized compound I , II or IV pyrabenyl _-- B-11 an individualized compound 1, U or IV trifluoro-sensitive ~ '--~~~ B-12 an individualized compound I, II or IV 2-(2- (6-(3-Gas-2-pyroxyl-phenylpyrimidin-4-yloxy)-phenyl)-2-indolyloxyimido-N-methyl-acetamide B-13 Compound I, hydrazine or IV 2-(o-((2,5-indolyl)-oxymethylene)phenyl)-3-decyloxy- Acrylate methyl ester B-14 An individualized compound I, hydrazine or IV 3-decyloxy-2-(2-(N-(4-decyloxy-phenyl)-cyclopropanimide) Alkylthiomethyl)·Acrylic Acid·Acrylic Acid Vinegar 149026.doc -171 - 201103429 Mixture Component 1 Component 2 B-15 An Individualized Compound I, II or IV 2-(2-(3- (2,6-diphenyl)-1-indolyl-allylaminooxyindolyl)-phenyl)-2-indolyloxyimido-N-methyl-acetamidamine B -16 An individualized compound I, II or IV Benzophene B-17 An individualized compound I, II or IV Benzocycline-M B-18 An individualized compound I, II or IV A wheat rust B-19 Individualized compound I, II or IV fennel B-20 An individualized compound I, II or IV Bokley B-21 an individualized compound I, II or IV oxazepine B-22 an individualized compound I, II or IV furfuramide B-23 an individualized compound I, II or IV cyclosporin B-24 an individualized compound I, II or IV fluentin B-25 an individualized compound I, II or IV An individualized compound of B-27, an individualized compound I, II or IV I, II or IV Isotianil B-28 An individualized compound I, II or IV Carrageen B-29 An individualized compound I, II or IV rust-free amine B-30 An individualized compound I, II or IV达达乐 B-31 An individualized compound I, II or IV statin-M B-32 an individualized compound I, II or IV ocalamine B-33 an individualized compound I, II or IV B-34 An individualized compound I, II or IV oxidized wilting B-35 an individualized compound I, II or IV pirimipenem B-36 an individualized compound I, II or IV 森达先 B-37 An individualized compound I, II or IV gram-depleted B-38 an individualized compound I, II or IV cyprofen B-39 an individualized compound I, II or IV steroidal B-40 an individualized compound I , II or IV 2-Amino-4-mercapto-α-Serb-5-anthracene aniline B-41 An individualized compound I, II or IV 2-gas-N-(l,l,3-dioxin Base-man-4 base)-final amine B-42 an individualized compound I, hydrazine or IV N-(3',4',5L-trifluorobiphenyl-2-yl)-3-difluoromethyl Alkyl-1-mercapto-1H-pyrazole-4-decylamine B-43 an individualized compound I, II IV N-(4L Dimethylsulfonylbiphenyl-2-yl)-3-difluoromethyl-1-indolylpyrazole-4-carboxamide A-II An individualized compound I, II or IV N-(2-(l,3-dimethyl-butyl)-phenyl)-1,3-dimethyl-5-fluoro-1H-. ratio. -4-Methylamine B-45 An individualized compound I, II or IV (2-(1,3,3-tridecyl-butyl)-phenyl)-1,3-dimethyl- 5-fluoro-1H-pyrazole-4-carboamine B-46 An individualized compound I, II or IV, earth Λ» Λ#· 达灭分 B-47 an individualized compound I, II or IV fluoride琪琳B-48 An individualized compound I, II or IV butyl 0 ratio B-49 an individualized compound I, hydrazine or IV flumetamide B-50 an individualized compound I, II or IV fluoro 0 ratio Azinamide [si 149026.doc -172- 201103429 Mixture component 1 component 2 B-51 an individualized compound I' II or IV flupirtine B-52 an individualized compound I, II or IV gas benzoguanamine B -53 An individualized compound I, II or IV N-(3-ethyl-3,5,5-trimethyl-cyclohexyl)-3-indolylamino-2-hydroxy-benzamide-5 -54 an individualized compound I, II or IV gupamine B-55 an individualized compound I, II or IV diclocarbam B-56 an individualized compound I, II or IV diacetylidin B-57 An individualized compound I, II or IV oxytetracycline B-58 an individualized compound I, II or IV Sirthiofam B-59 An individualized compound I, II or IV N-(6-methoxy-° ratio -3-yl) cyproterone decanoate B-60 An individualized compound I, II or IV Aza Conazole B-61 an individualized compound I, II or IV than donut B-62 an individualized compound I, II or IV bromoxynazole B-63 an individualized compound I, II or IV cycloheximide B-64 An individualized compound I, II or IV difenoconazole B-65 an individualized compound I, II or IV diconazole B-66 an individual compound I, II or IV dinitron-M B- 67 An individualized compound I, II or IV fluorocyclic guanidine B-68 an individualized compound I, II or IV fenbucarbin B-69 an individualized compound I, II or IV fluquinazole B-70 an individual Compound I, II or IV Fluorocarbazole B-71 An individualized compound I, II or IV Difluben B-72 An individualized compound I, II or IV Liukang Sal B-73 An individualized compound I, II Or IV imidazole B-74 an individualized compound I, II or IV Epproxazole B-75 An individualized compound I, hydrazine or IV fluconazole B-76 An individualized compound I, II or IV B-77 Tennyson individualized one kind of compound I, II or IV ah. Meter. Sit B-78 An individualized compound I, II or IV Bark B-79 An individualized compound I, II or IV Pancon. Sit B-80 An individualized compound I, II or IV. S-B-81 an individualized compound I, II or IV propyl thiol azole B-82 an individualized compound I, II or IV fluorazole B-83 an individualized compound I, II or IV Dekley B-84 An individualized compound I, II or IV fluoroether oxime B-85 an individualized compound I, II or IV ternate B-86 an individualized compound I, II or IV three tylon B-87 an individualized compound I, II or IV ring bacteria. S-B-88 An individualized compound I, II or IV Difficulty sitting B-89 An individualized compound I, II or IV 1 -(4-chloro-phenyl)-2-([ 1,2,4] Triazol-1-yl)-cycloheptanol B-90 An individualized compound I, II or IV #座灭149026.doc •173- 201103429 Mixture component 1 Component 2 B-91 An individualized compound I, Π Or IV according to B-92 an individualized compound I, II or IV thiosulfate B-93 an individualized compound I, II or IV indole ester B-94 an individualized compound I, II or IV Poker Pulling B-95 an individualized compound I, II or IV Safran B-96 an individualized compound I, II or IV benomyl B-97 an individualized compound I, II or IV befenfen B-98 Individualized compound I, II or IV Maishenling B-99 An individualized compound I, II or IV Thiabendazole B-100 An individualized compound I, oxime or IV Thiabamide B-101 An individualized compound I , II or IV eduli B-102 an individualized compound I, II or IV carbendazim B-103 an individualized compound I, II or IV 2-(4-chloro-phenyl)-N-[4- (3,4-dimethoxy-phenyl)恶°坐-5-yl]-2-propan-2-freeoxy-acetamidamine B-104 an individualized compound I, II or IV edugamine B-105 an individualized compound I, II or IV Bifeno B-106 an individualized compound I, II or IV 3-[5-(4-a-phenyl)-2,3-dimethyl-isoxazole quinone-3-yl]-α ratio Bite B-107 An individualized compound I, II or IV 3-[5-(4-methyl-phenyl)-2,3-dimethyl-isoxime sulphate-3-yl]-° ratio. B-108 An individualized compound I, II or IV 2,3,5,6-tetrachloro-4-methylsulfonyl-pyridine B-109 An individualized compound I, II or IV 3,4,5- Triclopyridin-2,6-dicarbonitrile B-110 An individualized compound I, II or IV N-(l-(5_ &gt;odor-3-chloro-π ratio-2-yl)-ethyl -2,4-Dichloro-nicotinium amide B-lll An individualized compound I, II or IV Ν-((5-involved-3-chloro-° ratio ̄-2-yl)-methyl) -2,4-Dichloro-nicotinium amide A-II, an individualized compound I, II or IV, sulfamethoxazole B-113, an individualized compound I, II or IV, Sibodine B-114, an individualized compound I, II or IV diflurine B-115 an individualized compound I, II or IV fenrimyl B-116 an individualized compound I, II or IV azoxystrobin B-117 an individualized compound I, hydrazine or IV Mippanicin B-118 an individualized compound I, II or IV chloropyridine B-119 an individualized compound I, II or IV fluoropyrimidinol B-120 an individualized compound I, II or IV B-121 An individualized compound I, II or IV Safranine B-122 An individualized compound I, II or IV Seed dressing B-123 Alimentation of Compound I, II or IV Refining B-124 An Individualized Compound I, II or IV Adiline B-125 An Individualized Compound I, II or IV. carbendazim B-126 An Individualized Compound I, II or IV carbendazim acetate B-127 an individualized compound I, II or IV powder rust [si 149026.doc •174- 201103429 mixture M part 1 component 2 -- B-128 an individualized compound I, Π Or IV thirteen--- B-129 an individualized compound I, II or IV fenpropidin B-130 an individualized compound I, II or IV messy imine __ B-131 an individualized compound I , Π or IV 依普同---- B-132 an individualized compound I, II or IV fentanyl - B-133 an individualized compound I, II or IV konkening __- B-134 Compound I, II or IV sputum ketone -- B-135 An individualized compound I, hydrazine or IV σ σ 坐 oxycodone B-136 An individualized compound I, II or rv fluentin __- B- 137 An individualized compound I, hydrazine or IV bismuth B-138 An individualized compound I, hydrazine or IV thiabendazole - _ - B-139 an individualized compound I, II or rv 5-Amino-2-iso-propyl-4-o-tolyl-2,j-dihydro-pyrazole-1 -thiocarboxylic acid s-allyl vinegar B-140 An individualized compound I, II or IV Acidified benzothiazepine-s-methyl ester - B-141 An individualized compound I, hydrazine or IV carbazolam bromide B-142 An individualized compound I, II or rv carbendazim __ B-143 An individualized compound I, II or rv blasticidin-S B-144 an individualized compound I, hydrazine or IV ethene B-145 an individualized compound I, hydrazine or IV cappdan B-146 an individual Compound I, Π or IV 螨 螨 B-147 An individualized compound I, Π or IV 迈隆 B-148 An individualized compound I, II or IV imiprozil B-149 an individualized compound I, hydrazine or IV 哒菌清 B-150 An individualized compound I, Π or IV benzophenone fast B-151 An individualized compound I, II or IV methyl acesulfate benzoate B-152 an individualized compound I, π or rv Cao Ling B-153 An individualized compound I, oxime or IV Forbeline B-154 An individualized compound I, oxime or IV Oxolins Sure B-155 An individualized compound I, Π or IV powder disease B- 156 one Individualized compound I, II or IV Puccinaz ~~- B-157 An individualized compound I, hydrazine or IV 百--- B-158 an individualized compound I, II or IV 7 夬norfen' ~ ~~- B-159 - Individualized compound I, II or IV Imidazolium - B-160 An individualized compound I, II or rv Trixazole - B-161 An individualized compound I, hydrazine or IV 2-butenyl · 6-Moth-3-propyl · bite coal B-162 an individualized compound I, hydrazine or IV fluorenyl-1 Η-benzimidazole B-163 an individualized compound I, II or IV 5-gas-7- (4-mercapto-0 bottom bite trifluoro-phenyl (4) training three. Sit and B-164 an individualized compound I, hydrazine or IV 5-ethyl-6·octyl·[〗, 2,4]triazime-7-ylamine [,5'a] B-165 an individual Compound I, hydrazine or IV thiram - B-166 an individualized compound I, hydrazine or IV Mn-Zn-175· 149026.doc 201103429 Mixture component 1 Component 2 B-167 An individualized compound I, II or IV代森猛 B-168 An individualized compound I, II or IV Wei Biao B-169 An individualized compound I, Π or IV 菌菌B-170 An individualized compound I, II or IV 森森联 B- 171 An individualized compound I, II or rv propyl zinc B-172 An individualized compound I, II or IV thiram B-173 An individualized compound I, II or rv Desensen B-174 An individualized compound I , II or IV 福美辞 B-175 an individualized compound I, II or IV. carbendazim B-176 an individualized compound I, II or IV phenothranol' B-177 an individualized compound I, hydrazine or IV缬 威B-178 An individualized compound I, hydrazine or IV acesulfame B-179 An individualized compound I, hydrazine or IV Phytophthora hydrochloride B-180 An individualized Compound I, hydrazine or IV virifene B-181 an individualized compound I, II or IV N-(l-(l-(4-cyanophenyl)ethanesulfonyl)-butan-2-yl) Amino phthalic acid-(4-fluorophenyl) ester B-182 An individualized compound I, II or rv. Tonin B-183 An individualized compound I, hydrazine or IV. Toxin free base B-184 an individual compound I, hydrazine or IV bisindole B-185 an individualized compound I, II or IV bisindole octyl acetate B-186 an individualized compound I, π or rv bis-octylamine B-187 an individualized compound I, II or rv Bis-octylamine triacetate B-188 An individualized compound I, II or IV grams of pyrogen (alkane) B-189 An individualized compound I, II or IV Chunctomycin B-190 Compound I, II or IV Salicin Hydrochloride Salt B-191 An Individualized Compound I, II or IV Polyoxin B-192 An Individualized Compound I, II or IV Streptomycin B-193 An Individual Compound I, II or rv Aminomycin A B-194 An individualized compound I, II or IV Baikeke B-195 An individualized compound I, π or IV Dicloran B-196 Alimentation of compound I, II or rv Large depurination B-197 An individualized compound I, II or IV White powder B-198 An individualized compound I, II or IV Trichostatin B-199 An individualized compound I, II Or rv tetra-nitrobenzene B-200 an individualized compound I, π or rv triphenyltin salt B-201 an individualized compound I, II or IV nitrile sulfonium B-202 an individualized compound I, II or IV Indigo B-203 An individualized compound I, π or rv Pleurotus ostreatus B-204 An individualized compound I, II or rv Triethylphosphonic acid, aluminum triethylphosphonate B-205 An individualized compound I, π Or IV propyl chelsson B-206 an individualized compound I, π or IV phosphoric acid (h3po3) and derivative B-207 an individualized compound I, hydrazine or IV white pine B-208 an individualized compound I, π or Rv 脱克松[si 149026.doc •176- 201103429 Mixture Component 1 Component 2 B-209 An Individualized Compound I, II or IV Chlorothalon B-210 An Individualized Compound I, II or IV Yifaling B -211 An individualized compound I, II or IV Bisphenol - B-212 An individualized compound I, hydrazine or IV fluorosulfur B-213 An individualized compound I, hydrazine or IV hexascreen B-214 An individualized compound I, II or IV Bin-clone ~- B-215 An individualized compound I, hydrazine or IV pentoxide and its salts B-216 An individualized compound I, II or IV phenylhydrazine _ a ~ B-217 an individualized compound I' II or IV quetiacin ~~' --- B-218 an individualized compound I, II or IV Quitopurine B-219 An individualized compound I, II or IV methyl valproate B-220 An individualized compound I, hydrazine or IV Ν-(4-chloro-2-nitro-phenyl)-hydrazine- Ethyl-4-methyl-benzoic amine B-221 an individualized compound I, II or IV Bordeaux B-222 An individualized compound I, II or IV Copper acetate B-223 An individualized compound I, II Or IV copper hydroxide B-224 an individualized compound I, II or IV gas oxidized copper - B-225 an individualized compound I, hydrazine or IV Γ test copper sulphate B-226 an individualized compound I, II or IV B-227 An individualized compound I, hydrazine or IV conjugated - B-228 An individualized compound I, II or IV bronopol ~~ -- B-229 An individualized compound I, II or IV thiophene Amine B-230 An individualized compound I, II or IV sulphonyl cyanide B-231 An individualized compound I, hydrazine or IV diammonium B-232 An individualized compound I, hydrazine or IV ochrexene B-233 an individual Compound I, II or IV _ 灭粉~~ B-234 An individualized compound I, II or IV via copper bismuth B-235 An individualized compound I, II or IV calcium cyclate B-236 Individualized Compound I, II or IV spirulina B-237 An individualized compound I, hydrazine or IV B-238 An individualized compound I, II or IV Ν-(cyclopropyl decyloxyimino) 6_Difluoromethoxy 2,3-difluoro-phenyl)-methyl)-2-indolyl B-239 An individualized compound I, hydrazine or IV Ν'·(4-(4 -Chloro-3-trifluoromethyl-p-oxyl&gt;21 Dimercapto-phenyl VN-ethyl-fluorenyl-fluorenyl b-240 An individualized compound I, hydrazine or IV Ν'-(4 -(4-Fluoro-3-trifluoromethyl-phenoxy)-2,5-diindenyl-phenyl-VN-ethyl-indole-indenyl B-241 An individualized compound I, hydrazine or IV Ν'-(2_Mercapto-5-trifluoromethyl-4-(3-tridecylfluorenyl-propoxy)-phenyl)-N-ethyl-N-methylformamidine B- 242 one by one Differentiation of compound I, hydrazine or IV van-(5-difluoromethylindolyl-4-(3-trimethyldecyl-propoxy)-phenyl)-N-ethyl-N-methylformamidine 149026.doc -177· 201103429 Mixture component 1 Component 2 B-243 An individualized compound I, II or IV 2-{1-[2-(5-fluorenyl-3-trifluoromethyl-pyrazole- 1-yl)-ethinyl]-piperidin-4-yl}-thiazole-4-furoate hydrazino-(1,2,3,4-tetrazo-n-yl)-bristamine B- 244 An individualized compound I, II or IV 2-{1-[2-(5-methyl-3-trifluoromethyl-pyrazol-1-yl)-ethinyl]-piperidin-4-yl }-thiazole-4-decanoic acid methyl-(R)-l,2,3,4-tetrazine-cai-1·yl-bristamine B-245 an individualized compound I, II or IV acetic acid 6- Tributyl-8-oxa-2,3·diindolyl-4-ylindole B-246 An individualized compound I, II or IV methoxy-acetic acid 6-t-butyl-8-fluoro -2,3-dimethyl-wow scare&gt;-4-yl vinegar B-247 an individualized compound I, II or IV plus Poly B-248 an individualized compound I, II or IV plus Bao B-249 An individualized compound I, II or IV butyl plus Bao B-250 an individualized compound I, II or IV Na Nade thiodicarb B-251 an individualized combination I, II or IV Bifenin B-252 An individualized compound I, II or IV Safranine B-253 An individualized compound I, II or IV Saining B-254 An individualized compound I, II or IV sub-extinction Ning B-255 An individualized compound I, II or IV ζ-ambience Chrysanthemum S-B-256 An individualized compound I, II or IV Dingning B-257 An individualized compound I, II or IV Yi Bili B -258 An individualized compound I, hydrazine or IV λ-赛洛宁 B-259 An individualized compound I, II or IV Benzene B-260 An individualized compound I, II or IV Tefluthrin B-261 An individualized compound I, II or IV Fufulon B-262 An individualized compound I, II or IV Flufuron B-263 An individualized compound I, II or IV Lucendron B-264 An individualized compound I , II or IV Devalon B-265 An individualized compound I, II or IV Spirotetramat ethyl ester B-266 An individualized compound I, II or IV Cotinine B-267 An individualized compound I, II or IV Anthraquinone B-268 An individualized compound I, II or IV etadamine B-269 An individualized compound I, II or IV thiamethoxam B-27 0 An individualized compound I, guanidine or IV biting insect Yuedong B-271 An individualized compound I, II or IV. Sesinolin B-272 An individualized compound I, II or IV Endosulfan B-273 An individualized compound I, hydrazine or IV Fenpney B-274 An individualized compound I, II or IV Abatatin B-275 An individualized compound I, II or IV Inhibitor B-276 An individualized compound I, II or IV Schnauzer B-277 An individualized compound I, II or IV Spinoline B-278 An individual compound I, II or IV Volt B-279 An individualized compound I, II or IV

[SI 149026.doc -178- 201103429 混合物 組份1 組份2 B-280 一種個別化化合物I、II或IV 芬布賜 B-281 一種個別化化合物I、II或IV 茚蟲威 B-282 一種個別化化合物I、II或IV 美氟腙 B-283 一種個別化化合物I、II或IV 氟尼胺 B-284 一種個別化化合物I、II或IV 福本胺 B-285 一種個別化化合物I、II或IV 氯鄰胺基苯甲普 B-286 一種個別化化合物I、II或IV 魚尼汀受體抑制劑(HGW86) B-287 一種個別化化合物I、II或IV 噻氟美芬 B-288 一種個別化化合物I、II或IV 乙草胺 B-289 一種個別化化合物I、II或IV 二甲噻草胺 B-290 一種個別化化合物1' II或IV 異丙曱草胺 B-291 一種個別化化合物I、II或IV °比草胺 B-292 一種個別化化合物I、II或IV 嘉磷塞 B-293 一種個別化化合物I、II或IV 固殺草 B-294 一種個別化化合物I、II或IV 硫復松 B-295 一種個別化化合物I、II或IV 炔草酸 B-296 一種個別化化合物I、II或IV 噁唑禾草靈 B-297 一種個別化化合物I、II或IV 。比氟禾草靈 B-298 一種個別化化合物I、II或IV °比氟氯禾靈 B-299 一種個別化化合物I、II或IV 百草枯 B-300 一種個別化化合物I、II或IV 甜菜寧 B-301 一種個別化化合物I、II或IV 克草同 B-302 一種個別化化合物I、II或IV 環殺草 B-303 一種個別化化合物I、II或IV 環苯草酮 B-304 一種個別化化合物I、II或IV 西殺草 B-305 一種個別化化合物I、II或IV 得殺草 B-306 一種個別化化合物I、II或IV 二甲戊樂靈 B-307 一種個別化化合物I、II或IV 胺氟樂靈 B-308 一種個別化化合物I、II或IV 氟樂靈 B-309 一種個別化化合物I、II或IV 三氟羧草醚 B-310 一種個別化化合物I、II或IV &gt;臭苯猜 B-311 一種個別化化合物I、II或IV 咪草酯 B-312 一種個別化化合物I、II或IV 曱氧咪草菸 B-313 一種個別化化合物I、II或IV 甲咪唑菸酸 B-314 一種個別化化合物I、II或IV 滅草於 B-315 一種個別化化合物I、II或IV 滅草唾 B-316 一種個別化化合物I、II或IV °米草終 B-317 一種個別化化合物I、II或IV 2,4-二氯苯氧基乙酸(2,4-D) B-318 一種個別化化合物I、II或IV 氣草敏 B-319 一種個別化化合物I、II或IV 畢克草 B-320 一種個別化化合物I、II或IV 氟草菸 B-321 一種個別化化合物I、II或IV 毒莠定 B-322 一種個別化化合物I、II或IV 氟吡草胺 -179- 149026.doc 201103429 混合物 組份1 組份2 B-323 一種個別化化合物I、II或IV 苄嘧磺隆 B-324 一種個別化化合物I、II或IV 乙基氣嘧磺隆 B-325 一種個別化化合物I、II或IV 環丙嘴績隆 B-326 一種個別化化合物I、II或IV 碘甲磺隆 B-327 一種個別化化合物I、II或IV 甲磺胺磺隆 B-328 一種個別化化合物I、II或IV 曱基甲磺隆 B-329 一種個別化化合物I、II或IV 菸嘧磺隆 B-330 一種個別化化合物I、II或IV 颯嘧磺隆 B-331 一種個別化化合物I、II或IV 氣胺續隆 B-332 一種個別化化合物I、II或IV 莠去津 B-333 一種個別化化合物I、II或IV 環嗪酮 B-334 一種個別化化合物I、II或IV 歒草隆 B-335 一種個別化化合物I、II或IV 雙氟磺草胺 B-336 一種個別化化合物I、II或IV 普羅蘇芬 B-337 一種個別化化合物I、II或IV 苯達松 B-338 一種個別化化合物I、II或IV 吲哚酮草酯 B-339 一種個別化化合物I、11或IV 環庚草醚 B-340 一種個別化化合物I、Π或IV 麥草畏 B-341 一種個別化化合物I、II或IV 二氟吡隆 B-342 一種個別化化合物I、II或IV 二氣唾#酸 B-343 一種個別化化合物I、Π或IV 喹草酸 B-344 一種個別化化合物I、II或IV 甲基績草酮 B-345 一種個別化化合物I、Π或IV 嘧啶肟草醚 B-346 —種個別化化合物I、Π或IV 拓普美腙 被稱為組份2之活性物質、其製備及其對抗有害真菌之 活性係已知的(參看,http://www.alanwood.net/pesticides/);此 等物質可於市面上購得。由IUPAC命名法所述之化合物、 其製備及其殺真菌活性亦為已知的(參看,Can. J· Plant Sci. 48(6), 587-94, 1968 ; EP-A 141 317 ; EP-A 152 031 ; EP-A 226 917 ; EP-A 243 970 ; EP-A 256 503 ; EP-A 428 941 ; EP-A 532 022 ; EP-A 1 028 125 ; EP-A 1 035 122 ; EP-A 1 201 648 ; EP-A 1 122 244 ; JP 2002316902 ; DE 19650197 ; DE 10021412 ; DE 102005009458 ; US 3,296,272 ; US 3,325,503 ;[SI 149026.doc -178- 201103429 Mixture component 1 Component 2 B-280 An individualized compound I, II or IV Fenbu B-281 An individualized compound I, II or IV Indomethacin B-282 Individualized compound I, II or IV fluorinated B-283 an individualized compound I, II or IV flunisamine B-284 an individualized compound I, II or IV fubenamine B-285 an individualized compound I, II Or IV chloro-amidobenzil B-286 an individualized compound I, II or IV a ghectin receptor inhibitor (HGW86) B-287 an individualized compound I, II or IV tiflumeimide B-288 An individualized compound I, II or IV acetochlor B-289 an individualized compound I, II or IV dimethacin B-290 an individualized compound 1' II or IV isopropyl valeramine B-291 Individualized compound I, II or IV ° oxalate B-292 An individualized compound I, II or IV jiaphosphonate B-293 An individualized compound I, II or IV Phytophthora B-294 An individualized compound I , II or IV thiolopine B-295 an individualized compound I, II or IV acetyl oxalic acid B-296 an individualized compound I, II or IV Fenoxaprop B-297 one kind of individual compounds I, II or IV. Bifluoxacillin B-298 An individualized compound I, II or IV ° chlorhexidine B-299 An individualized compound I, II or IV Paraquat B-300 An individualized compound I, II or IV beet Ning B-301 An individualized compound I, II or IV gram of grass with B-302 an individualized compound I, II or IV Cycloheximide B-303 An individualized compound I, II or IV Cyclopentanone B-304 An individualized compound I, II or IV chlorpyrifos B-305 an individualized compound I, II or IV from chlorpyrifos B-306 an individualized compound I, II or IV pendimethalin B-307 Compound I, II or IV Amphetamine B-308 An individualized compound I, II or IV Trifluralin B-309 An individualized compound I, II or IV Acifluorfen B-310 An individualized compound I , II or IV &gt; odor benzene guess B-311 an individualized compound I, II or IV imazethate B-312 an individualized compound I, II or IV oxazepam B-313 an individualized compound I, II or IV meidazolium nicotinic acid B-314 an individualized compound I, II or IV herbicide in B-315 an individualized compound I, II or I V 灭草, S-B-316, an individualized compound I, II or IV ° rice grass, final B-317, an individualized compound I, II or IV 2,4-dichlorophenoxyacetic acid (2,4-D) B -318 An individualized compound I, II or IV Aerosol-sensitive B-319 An individualized compound I, II or IV Becker grass B-320 An individualized compound I, II or IV Fluroxypyr B-321 Compound I, II or IV Toxicidine B-322 An individualized compound I, II or IV Flumazepam-179-149026.doc 201103429 Mixture component 1 Component 2 B-323 An individualized compound I, II or IV Bensulfuron-B-324 An individualized compound I, II or IV Ethylsulfuron-B-325 An individualized compound I, II or IV Cyclopropylidene B-326 An individualized compound I, II or IV Iodomethylsulfuron B-327 An individualized compound I, II or IV Mesulsulfuron-B-328 An individualized compound I, II or IV Mercaptomethylsulfuron B-329 An individualized compound I, II or IV Nicosulfuron B-330 An individualized compound I, II or IV Resinsulfuron B-331 An individualized compound I, II or IV gas amine sulphide B-332 Compound I, II or IV Atrazine B-333 An Individualized Compound I, II or IV Cyazinone B-334 An Individualized Compound I, II or IV Valerian B-335 An Individualized Compound I, II Or IV diflufenacil B-336 an individualized compound I, II or IV prosufon B-337 an individualized compound I, II or IV bentazon B-338 an individualized compound I, II or IV Indolinone B-339 An individualized compound I, 11 or IV cycloheptyl ether B-340 an individualized compound I, hydrazine or IV dicamba B-341 an individualized compound I, II or IV diflupiron B-342 An individualized compound I, II or IV dioxate #acid B-343 an individual compound I, hydrazine or IV quinoxalate B-344 an individual compound I, II or IV methyl chlorfenapyr B- 345 An individualized compound I, hydrazine or IV pyrithione B-346 - an individualized compound I, hydrazine or IV Topex is known as component 2 active substance, its preparation and its activity against harmful fungi It is known (see, http://www.alanwood.net/pesticides/); these materials are commercially available. The compounds described by the IUPAC nomenclature, their preparation and their fungicidal activity are also known (see, Can. J. Plant Sci. 48(6), 587-94, 1968; EP-A 141 317; EP- A 152 031; EP-A 226 917; EP-A 243 970; EP-A 256 503; EP-A 428 941; EP-A 532 022; EP-A 1 028 125; EP-A 1 035 122; A 1 201 648 ; EP-A 1 122 244 ; JP 2002316902 ; DE 19650197 ; DE 10021412 ; DE 102005009458 ; US 3,296,272 ; US 3,325,503 ;

[SI 149026.doc •180- 201103429 WO 98/46608 ; WO 99/14187 ; WO 99/24413 ; WO 99/27783 ; WO 00/29404 ; WO 00/46148 ; WO 00/65913 ; WO 01/54501 ; WO 01/56358 ; WO 02/22583 ; WO 02/40431 ; WO 03/10149 ; WO 03/11853 ; WO 03/14103 ; WO 03/16286 ; WO 03/53145 ; WO 03/61388 ; WO 03/66609 ; WO 03/74491 ; WO 04/49804 ; WO 04/83193 ; WO 05/120234 ; WO 05/123689 ; WO 05/123690 ; WO 05/63721 ; WO 05/87772 ; WO 05/87773 ; WO 06/15866 ; WO 06/87325 ; WO 06/87343 ; WO 07/82098 ; WO 07/90624)。 可藉由常見方法,例如藉由對於化合物I、Π及/或IV之 組合物所給出之方法以組合物形式製備活性物質之混合 物,該等組合物除活性成份之外亦包含至少一種惰性成 份。 關於該等組合物之常見成份,參考對於含有化合物I、II 及/或IV之組合物所作出的解釋。 本發明活性物質之混合物適用作殺真菌劑,式I、II及IV 之化合物亦適用作殺真菌劑。其特點在於對廣譜植物致病 真菌之顯著有效性,尤其對來自以下類別之真菌:子囊菌 綱、擔子菌綱、半知菌綱及卵菌綱。此外,參考關於化合 物及分別含有化合物I、II及/或IV之組合物的殺真菌活性 之解釋。 化合物I、II及IV及其醫藥學上可接受之鹽亦適用於治療 人類及動物之疾病,尤其作為抗黴劑,用於治療癌症且用 於治療病毒感染。術語「抗黴劑」不同於術語「殺真菌 149026.doc -181 - 201103429 劑」’其係指用於對抗動物致病性或人類致病性真菌之藥 劑’亦即用於對抗動物中,尤其哺乳動物(包括人類)及鳥 類中之真菌的藥劑。 因此’本發明之另一態樣係關於包含至少一種式I、π及/ 或IV之化合物及/或至少一種其醫藥學上可接受之鹽及醫 藥學上可接受之載劑的藥劑。 合適之醫藥學上可接受之鹽尤其為化合物I之生理上耐 文之鹽’詳言之’生理上可接受之酸之酸加成鹽。合適之 有機及無機酸之實例為鹽酸、氫溴酸、磷酸、硫酸、C1_ C4烧基磺酸(諸如曱磺酸)、芳族磺酸(諸如苯續酸及甲苯磺 酉欠)、草酸、順丁稀二酸、反丁稀二酸、乳酸、酒石酸、 己二酸及笨甲酸。其他合適之酸係描述於例如F〇rtschritte der Arzneimittelforschung,第 1〇 卷,第 ff.頁,BirkhSuser[SI 149026.doc • 180-201103429 WO 98/46608; WO 99/14187; WO 99/24413; WO 99/27783; WO 00/29404; WO 00/46148; WO 00/65913; WO 01/54501; 01/56358; WO 02/22583; WO 02/40431; WO 03/10149; WO 03/11853; WO 03/14103; WO 03/16286; WO 03/53145; WO 03/61388; WO 03/66609; WO 04/74491; WO 04/83193; WO 05/120234; WO 05/123689; WO 05/123690; WO 05/63721; WO 05/87772; WO 05/87773; WO 06/15866; 06/87325; WO 06/87343; WO 07/82098; WO 07/90624). Mixtures of the active substances can be prepared in the form of compositions by conventional methods, for example, by the methods specified for the compositions of the compounds I, oxime and/or IV, which compositions comprise at least one inert ingredient in addition to the active ingredient. Ingredients. For the common ingredients of such compositions, reference is made to the explanations for compositions containing compounds I, II and/or IV. Mixtures of the active substances according to the invention are suitable as fungicides, and the compounds of the formulae I, II and IV are also suitable as fungicides. It is characterized by significant efficacy against a broad spectrum of phytopathogenic fungi, especially for fungi from the following classes: Ascomycetes, Basidiomycetes, Deuteromycetes and Oomycetes. Further, reference is made to the explanation regarding the fungicidal activity of the compound and the composition containing the compounds I, II and/or IV, respectively. The compounds I, II and IV and their pharmaceutically acceptable salts are also suitable for the treatment of diseases in humans and animals, especially as anti-mold agents for the treatment of cancer and for the treatment of viral infections. The term "anti-fungal agent" is different from the term "fungicide 149026.doc -181 - 201103429", which means an agent used against animal pathogenic or human pathogenic fungi, ie for combating animals, especially An agent for fungi in mammals, including humans, and birds. Thus, another aspect of the invention pertains to medicaments comprising at least one compound of the formula I, π and/or IV and/or at least one pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. Suitable pharmaceutically acceptable salts are, in particular, the physiologically acceptable acid addition salts of the physiologically acceptable salts of the compound I. Examples of suitable organic and inorganic acids are hydrochloric acid, hydrobromic acid, phosphoric acid, sulfuric acid, C1_C4 alkylsulfonic acid (such as sulfonic acid), aromatic sulfonic acids (such as benzoic acid and toluene), oxalic acid, Succinic acid, antibutanic acid, lactic acid, tartaric acid, adipic acid and benzoic acid. Other suitable acid systems are described, for example, in F〇rtschritte der Arzneimittelforschung, Volume 1, page ff., BirkhSuser

Verlag,Basle and Stuttgart,1966中,該文獻之全部内容以引用 的方式明確地併入本文中。 合適之載劑為例如通常用於醫藥調配物中之溶劑、載 劑、賦形劑、黏合劑及其類似物,在下文中以針對個別投 藥類型之例示性方式對其進行描述。 本發明之另一態樣係關於化合物I、11及IV或其醫藥學上 可接受之鹽用於製備抗黴藥劑之用途;亦即,製備用於治 療及/或預防人類致病性及/或動物致病性真菌之感染的藥 劑。本發明之另一態樣係關於式j、π及/或IV之化合物或 其醫藥學上可接受之鹽用於製備供治療癌症用之藥劑的用 途。本發明之另一態樣係關於式】、π及/或以之化合物或 149026.doc -182· 201103429 其醫藥學上可接受之鹽用於製備供治療或預防病毒感染用 之藥劑的用途。 式I、II及IV之化合物及/或其醫藥學上可接受之鹽適用 於治療、抑制或控制腫瘤細胞之生長及/或增殖及與其相 關之病症。因此,其適用於以下動物之癌症療法:溫血脊 椎動物,例如,哺乳動物及鳥類,尤其雄性,及其他哺乳 動物,尤其有用之家畜,諸如狗、貓、豬、反羁動物 (牛、綿羊、山羊、野牛等)、馬,及鳥類,諸如雞火 雞、鴨、鵝、珠雞及其類似物。 式I、II及IV之化合物及/或其醫藥學上可接受之鹽適用 於以下器官之癌症或癌性病症的療法:乳房、肺、腸、前 列腺、皮膚(黑色素瘤)、腎臟、膀胱、口腔、喉、食道、 月部、卵巢、胰腺、肝臟及大腦或CNS。 式I、II及IV之化合物及/或其醫藥學上可接受之鹽適) 於治療以下動物之病毒感帛:溫血脊椎動物,例如&quot;以 動物及鳥類,尤其雄性,及其他哺乳動物,尤其有用之g 畜’諸如狗、猫、豬、反羁動物(牛 ' 綿羊、山羊、野2 等)、馬,及鳥類,諸如雞、火雞、鴨、鵝、珠雞及其· 似物。其適用於治療病毒感染,例如反轉錄病毒感染,拿 如HIV及HTLV、流感病毒感染、鼻病毒感染、范療及 似感染。 .八 ,例如經口、靜脈 ’可將活性化合物 可將其包埋於硬質 本發明之化合物可以習用方式投與 内、肌肉内或皮下。對於經口投與而言 …例如惰性稀釋劑或可食用載劑混合; 149026.doc -183- 201103429 或軟質明膠膠囊中,可將其壓成錠劑或可將其直接與食物/ 飼料混合。活性化合物可與賦形劑混合且以難消化之旋 劑、口腔錠劑'片劑、丸劑、膠囊、懸浮液、飲劑、糖漿 及其類似物形式投與。該等製劑應含有至少〇 1%活性化合 物。製劑之組成當然可不同。以相關製劑之總重量計(劑 量單位)’其通常包含2至60重量%之活性化合物。本發明 之化合物I之較佳製劑包含10至1000 mg之活性化合物/口服 劑量單位。 此外’錠劑、片劑、丸劑、膠囊及其類似物可包含以下 組份:黏合劑’諸如黃蓍膠、阿拉伯膠、玉米澱粉或明 膠;賦形劑,諸如磷酸氫鈣;崩解劑,諸如玉米澱粉、馬 鈴薯澱粉、褐藻酸及其類似物;助流劑,諸如硬脂酸鎂; 甜味劑,諸如蔗糖、乳糖或糖精;及/或調味劑,諸如胡 椒4荷、香草及其類似物。此外,膠囊可包含液體載劑。 亦可使用其他改良劑量單位之性質的物質。舉例而言,錠 劑、丸劑及膠囊可經蟲膠(scheUack)、糖或其混合物包 衣。除活性化合物之外,糖漿或飲劑亦可包含糖(或其他 甜味劑)、作為防腐劑之對羥基苯曱酸甲酯或對羥基苯甲 酸丙酯、著色劑及/或調味劑。當然,活性化合物製劑之 組份必須為醫藥學上純的且在所用數量下為無毒的。此 外’可將活性化合物調配為控制釋放活性化合物之製劑, 例如延遲釋放製劑。 亦可非經腸或腹膜内投與活性化合物。可使用合適之濕 潤劑(諸如羥丙基纖維素)以水來製備活性化合物或其鹽之 149026.doc •184· 201103429 溶液或懸浮液。★ ^ 亦可使用甘油、液態聚乙二醇及其於油中 °來製備分散液。此等製劑常另外包含防腐劑以防 止微生物生長。 人仏'主射用之製劑包含無菌水溶液及分散液以及用於製 備了、菌'备液及分散、液之無菌粉末。製劑必須具有足夠流動 陡以供/主射。其在製備及儲藏條件下必須為穩定的且必須 防止其受到微生物污染。載劑可為溶劑或分散介質,例如 X乙醇、夕元醇(例如甘油、丙二醇或液態聚乙二醇)及 其混合物及/或植物油。 【實施方式】 由以下非限制性實例來進一步說明本發明。 I. 合成實例 II. 對抗有害真菌作用之實例 藉由以下實驗證明式I及II之化合物的殺真菌作用: A)微量滴定試驗 活性物質於二曱亞砜(DMS0)中單獨地調配成儲備溶 液’濃度為10 〇〇〇 ppm。 使用貫例1 .於微量滴定試驗中對抗晚疫病病原體致病疫 黴菌之活性 將儲備溶液吸入微量滴定盤(MTP)中且使用供真菌用的 豌豆汁基水性營養培養基將其稀釋至規定的活性物質濃 度。隨後添加致病疫黴菌之遊走孢子水性懸浮液。將盤i 於溫度為.18°C的水蒸汽飽和之室内。使用吸收式光度t十, 在接種之後第7天在405 nm下量測MTP。將所量測之參數 149026.doc .185- 201103429 與不含活性物質之對照變體(=100%)之生長進行比較且與 不含真菌及活性物質之空白試驗值進行比較,以確定病原 體在個別活性物質中之相對生長%。 使用實例2 :在微量滴定試驗中對抗由水稻梨孢菌所引起 之稻盘病病原體的活性 將儲備溶液吸入微量滴定盤(MTP)中且使用供真菌用的 麥芽基水性營養培養基將其稀釋至規定的活性物質濃度。 隨後添加水稻梨孢菌之孢子水性懸浮液。將盤置於溫度為 1 8°C的水蒸汽飽和之室内。使用吸收式光度計,在接種之 後第7天在405 nm下量測微量滴定盤。將所量測之參數與 不含活性物質之對照變體(=1〇〇%)之生長進行比較且與不 含真菌及活性物質之空白試驗值進行比較,以確定病原體 在個別活性物質中之相對生長0/〇。 使用實例3 :在微量滴定試驗中對抗由小麥殼針孢菌所引 起之殼針孢菌斑病病原體的活性 將儲備溶液吸入微量滴定盤(MTP)中且使用供真菌用的 麥芽基水性營養培養基將其稀釋至規定的活性物質濃度。 隨後添加小麥殼針孢菌之孢子水性懸浮液。將盤置於溫度 為18°C的水蒸汽飽和之室内。使用吸收式光度計,在接種 之後第7天在405 nm下量測微量滴定盤。將所量測之參數 與不含活性物質之對照變體(=100%)之生長進行比較且與 不含真菌及活性物質之空白試驗值進行比較,以確定病原 體在個別活性物質中之相對生長%。 B)溫室試驗 149026.doc •186- 201103429 將活性物質單獨或共同調配成包含25 mg活性物質之儲 備溶液’使用丙酮及/或二甲亞颯(DMSO)與乳化劑Wettol EM 3 1 (具有乳化及分散作用的基於乙氧基化烧基盼之潤濕 劑)之混合物以溶劑/乳化劑99:1之體積比將其補足至! 〇 ml。隨後使用水將該溶液補足至10〇 m卜以所述溶劑/乳化 劑/水混合物將此儲備溶液稀釋至以下給出之活性物質濃 度。 使用實例4 :以保護性施用對抗由致病疫黴菌所引起之番 蘇早疫病之活性 使番茄植物幼苗於盆中生長。以含有下文規定之活性物 質濃度的水性懸浮液喷灑植物直至溢流為止。次日,處理 組植物接種致病疫黴菌孢子囊之水性懸浮液β在接種之 後’將試驗植物立即轉移至潮濕室内。在置於^至“·^及 接近100%之相對濕度下6天之後,目視評估葉上真菌侵襲 程度’以染病葉面積%表示。 使用貫例5 .對抗小麥上之隱匿柄鏽菌(小麥褐鏽病)的治療 性作用 以小麥褐鏽病(隱匿柄鏽菌)之孢子懸浮液噴灑栽培品種 「Kanzler」之盆栽小麥幼苗葉。隨後將植物置於高大氣濕 度(90至95%)及20-22C之室内24小時。在此期間,抱子發 芽且芽管透入葉片組織中。次日,以具有下文規定之活性 物質濃度的水性懸浮液喷灑受感染植物直至溢流點為止。 在經噴灑懸浮液乾燥後,使試驗植物返回溫室中且在2〇與 22 C之間的溫度及65至70%之相對大氣濕度下再培養7天。 149026.doc -187 - 201103429 隨後目測葉上之鏽病進展程度。 使用實例6 :對抗小麥上之隱匿柄鏽菌(小麥褐鑛病)之保護 性作用 以具有下文規定之活性物質濃度的水性懸浮液喷灑栽培 品種「Kanz丨er」之盆栽小麥幼苗葉直至溢流點為止。次 曰,以小麥褐鏽病(隱匿柄鏽菌)之孢子懸浮液喷灑處理組 植物隨後將植物置於向大氣濕度(90至95%)及20-22°C之 至内24小時。在此期間,孢子發芽且芽管透入葉片組織 中。次日’使試驗植物返回溫室中且在職抓之間的溫 度及65至70%之相對大氣濕度下再培養7天。隨後目測葉 上之鏽病進展程度。 使用貫例7 f:j•抗小麥上之小麥白粉病菌(小麥白粉病)的保 護性作用 以具有下文規定之活性物f濃度之水性⑽液噴麗栽培 品種「Kanz丨er」之盆栽小麥幼苗葉直至溢流點為止。次 J麥白物病(小麥白粉病菌)之抱子懸浮液喷麗處理 、·且植物(¾後使植物返回溫室中且在與2代之間的溫度 及至90/。之相對大氣濕度下再培養7天。隨後目測葉片 上之白粉病進展程度。 使用實例8 :對抗胡瓜卜夕艾ι „ 瓜上之蒼耳早絲殼菌(胡瓜白粉病)的保 護性作用 以具有下文規疋之活性物f濃度之水性懸浮液喷麗盆栽 胡瓜幼苗(處於胚層階段)葉直至溢流點。次日以胡瓜白 粉病(蒼耳料殼菌)之孢子懸浮液錢處理組植物。隨後 [S1 149026.doc -188· 201103429 使植物返回溫室中且在20與24°C之間的溫度及60至80%之 相對大氣濕度下再培養7天。隨後目測子葉上之白粉病進 展程度。 149026.doc -189-Verlag, Basle and Stuttgart, 1966, the entire contents of which is expressly incorporated herein by reference. Suitable carriers are, for example, solvents, carriers, excipients, binders, and the like, which are conventionally used in pharmaceutical formulations, which are described hereinafter in an exemplary manner for the particular mode of administration. Another aspect of the present invention relates to the use of Compounds I, 11 and IV or a pharmaceutically acceptable salt thereof for the preparation of an anti-fungal agent; that is, for the treatment and/or prevention of human pathogenicity and/or Or an agent for the infection of an animal pathogenic fungus. Another aspect of the invention is the use of a compound of formula j, π and/or IV or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of cancer. Another aspect of the present invention relates to the use of a compound of the formula, π and/or the compound or 149026.doc-182·201103429, a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment or prevention of a viral infection. The compounds of formula I, II and IV and/or their pharmaceutically acceptable salts are useful for treating, inhibiting or controlling the growth and/or proliferation of tumor cells and the conditions associated therewith. Therefore, it is suitable for cancer therapy of the following animals: warm-blooded vertebrates, for example, mammals and birds, especially males, and other mammals, especially useful domestic animals such as dogs, cats, pigs, ruminants (bovine, sheep) , goats, bison, etc.), horses, and birds, such as chicken turkeys, ducks, geese, pheasants, and the like. The compounds of formulae I, II and IV and/or their pharmaceutically acceptable salts are suitable for the treatment of cancer or cancerous conditions of the following organs: breast, lung, intestine, prostate, skin (melanoma), kidney, bladder, Oral, larynx, esophagus, lunar, ovarian, pancreatic, liver and brain or CNS. The compounds of formulae I, II and IV and/or their pharmaceutically acceptable salts are suitable for treating viral sensations in the following animals: warm-blooded vertebrates, such as &quot;in animals and birds, especially males, and other mammals Especially useful for animals such as dogs, cats, pigs, ruminants (cattle 'sheep, goats, wild 2, etc.), horses, and birds, such as chickens, turkeys, ducks, geese, pheasants and their likes Things. It is suitable for the treatment of viral infections, such as retroviral infections, such as HIV and HTLV, influenza virus infection, rhinovirus infection, paratherapy and infection. 8. For example, the active compound can be embedded in the hard by the mouth or vein, and the compound of the present invention can be administered intramuscularly, intramuscularly or subcutaneously in a conventional manner. For oral administration, such as an inert diluent or an edible carrier; 149026.doc -183- 201103429 or a soft gelatin capsule, it can be compressed into a lozenge or it can be mixed directly with the food/feed. The active compound may be mixed with excipients and administered in the form of indigestible elixirs, buccal tablets, tablets, pills, capsules, suspensions, liquids, syrups and the like. These preparations should contain at least 1% active compound. The composition of the formulation may of course vary. It is usually included in an amount of from 2 to 60% by weight of the active compound, based on the total weight of the relevant formulation (dosage unit). Preferred formulations of Compound I of the present invention comprise from 10 to 1000 mg of active compound per oral dosage unit. Further, 'tablets, tablets, pills, capsules and the like may contain the following components: binders such as tragacanth, acacia, corn starch or gelatin; excipients such as calcium hydrogen phosphate; disintegrants, Such as corn starch, potato starch, alginic acid and the like; a glidant such as magnesium stearate; a sweetener such as sucrose, lactose or saccharin; and/or a flavoring agent such as pepper 4, vanilla and the like Things. Additionally, the capsules can contain a liquid carrier. Other substances of modified dosage unit properties may also be used. For example, tablets, pills and capsules may be coated with scheUack, sugar or mixtures thereof. The syrup or drink may contain, in addition to the active compound, a sugar (or other sweetener), a methyl p-hydroxybenzoate or a propyl paraben, a colorant and/or a flavoring agent as a preservative. Of course, the components of the active compound formulation must be pharmaceutically pure and non-toxic in the amounts employed. Further, the active compound may be formulated as a formulation for controlled release of the active compound, such as a delayed release formulation. The active compound can also be administered parenterally or intraperitoneally. The solution or suspension of the active compound or its salt can be prepared in water using a suitable wetting agent such as hydroxypropylcellulose. ★ ^ It is also possible to use glycerin, liquid polyethylene glycol and its preparation in oil to prepare a dispersion. These formulations often additionally contain a preservative to prevent microbial growth. The preparation for human injection includes a sterile aqueous solution and a dispersion, and a sterile powder for preparing a liquid preparation and dispersion liquid. The formulation must have sufficient flow for steepness/main shot. It must be stable under the conditions of manufacture and storage and must be protected from microbial contamination. The carrier can be a solvent or dispersion medium such as X-ethanol, oxime (e.g., glycerol, propylene glycol or liquid polyethylene glycol) and mixtures thereof and/or vegetable oils. [Embodiment] The present invention will be further illustrated by the following non-limiting examples. I. Synthesis Example II. Examples of the action against harmful fungi The fungicidal action of the compounds of the formulae I and II is demonstrated by the following experiments: A) Microtitration test The active substance is separately formulated into a stock solution in disulfoxide (DMS0). 'The concentration is 10 〇〇〇ppm. Use example 1. In the microtiter test against the activity of Phytophthora infestans in late blight pathogens. Store the stock solution in a microtiter plate (MTP) and dilute it to the specified activity using a pea juice-based aqueous nutrient medium for fungi. Substance concentration. An aqueous suspension of zoospores of Phytophthora infestans is then added. Place the disk i in a room where the water vapor at a temperature of .18 ° C is saturated. MTP was measured at 405 nm on the 7th day after inoculation using an absorbance luminosity t10. The measured parameters 149026.doc .185- 201103429 were compared to the growth of control variants (=100%) without active substance and compared to blank test values without fungi and active substances to determine the pathogen % relative growth in individual active substances. Use example 2: Against the activity of the rice blast pathogen caused by P. sphaeroides in a microtiter test. Inject the stock solution into a microtiter plate (MTP) and dilute it with a malt-based aqueous nutrient medium for fungi. To the specified active substance concentration. An aqueous suspension of spores of P. sphaeroides was subsequently added. The disk was placed in a room saturated with water vapor at a temperature of 18 °C. The microtiter plate was measured at 405 nm on the 7th day after inoculation using an absorption photometer. Comparing the measured parameters to the growth of the control variant (=1%%) without active substance and comparing it to the blank test value without fungi and active substance to determine the pathogen in the individual active substance Relative growth 0 / 〇. Use Example 3: Resistance to the pathogen of the Phytophthora sphaeroides caused by Phytophthora hirsutum in a microtiter test. Inhalation of the stock solution into a microtiter plate (MTP) and use of malt-based water-based nutrients for fungi The medium is diluted to the specified active substance concentration. An aqueous suspension of spores of S. hirsutum was subsequently added. The disk was placed in a room saturated with water vapor at a temperature of 18 °C. The microtiter plate was measured at 405 nm on the 7th day after inoculation using an absorption photometer. The measured parameters were compared to the growth of control variants (=100%) without active substance and compared to blank test values without fungi and active substances to determine the relative growth of pathogens in individual active substances. %. B) Greenhouse test 149026.doc •186- 201103429 The active substance is formulated separately or together to a stock solution containing 25 mg of active substance 'Using acetone and/or dimethyl hydrazine (DMSO) with emulsifier Wettol EM 3 1 (with emulsification) And a mixture of dispersing ethoxylated oxime-based wetting agents) is supplemented by a solvent/emulsifier 99:1 volume ratio! 〇 ml. The solution is then made up to 10 〇 m with water and the stock solution is diluted with the solvent/emulsifier/water mixture to the concentration of active substance given below. Use Example 4: Protective application against the activity of Phytophthora infestans caused by Phytophthora infestans Tomato plant seedlings were grown in pots. The plants are sprayed with an aqueous suspension containing the active substance concentrations specified below until overflowing. On the next day, the treatment group was inoculated with an aqueous suspension of Phytophthora infestans sporangia β immediately after inoculation, and the test plants were immediately transferred to a humid chamber. Visually assess the degree of fungal attack on the leaf after 6 days of exposure to ^··· and close to 100% relative humidity, expressed as % of diseased leaf area. Use Example 5. Fight against Puccinia reticulata on wheat (wheat) Therapeutic effect of brown rust) The potted wheat seedling leaves of the cultivar "Kanzler" were sprayed with a spore suspension of wheat brown rust (Puccinia recondita). The plants were then placed in a high atmospheric humidity (90 to 95%) and a room at 20-22 C for 24 hours. During this time, the buds sprouted and the buds penetrated into the leaf tissue. The next day, the infected plants were sprayed with an aqueous suspension having the concentration of active substance specified below until the overflow point. After drying through the spray suspension, the test plants were returned to the greenhouse and cultured for a further 7 days at a temperature between 2 and 22 C and a relative atmospheric humidity of 65 to 70%. 149026.doc -187 - 201103429 The extent of rust progression on the leaves was then visually observed. Use example 6: Protective effect against Puccinia glabrata (wheat brown ore) on wheat Spraying the potted wheat seedling leaves of the cultivar "Kanz丨er" with an aqueous suspension having the active substance concentration specified below The flow point is up. The sputum was sprayed with a spore suspension of wheat brown rust (Puccinia recondita) and the plants were then placed in atmospheric humidity (90 to 95%) and 20-22 ° C for 24 hours. During this time, the spores germinate and the germ tubes penetrate into the leaf tissue. On the next day, the test plants were returned to the greenhouse and cultured for a further 7 days at a temperature between 65 °C and 70% of the relative atmospheric humidity. The extent of rust progression on the leaves was then visually observed. Use of a protective effect against the wheat powdery mildew (wheat powdery mildew) on wheat (7): water-based (10) potted wheat seedlings of the "Kanz丨er" cultivar "Kanz丨er" with the active substance f concentration specified below Leaves up to the overflow point. Sub-J whitening disease (wheat powdery mildew), the suspension of the scorpion suspension, and the plants (3⁄4 after returning the plants to the greenhouse and at a temperature between the 2nd generation and the relative atmospheric humidity of 90/. The culture was carried out for 7 days. Then the degree of powdery mildew progress on the leaves was visually observed. Example 8: The protective effect against the cucurbits of the genus Pleurotus ostreatus (courgette powdery mildew) on the melons to have the following activities The aqueous suspension of the substance f concentration sprayed the leaves of the courgette seedlings (at the stage of the germ layer) until the overflow point. The next day, the group of plants was treated with the spore suspension of the melon powdery mildew (C. sinensis). Subsequently [S1 149026. Doc -188· 201103429 The plants are returned to the greenhouse and cultured for a further 7 days at a temperature between 20 and 24 ° C and a relative atmospheric humidity of 60 to 80%. The degree of powdery mildew progression on the cotyledons is then visually observed. 149026.doc - 189-

Claims (1)

201103429 七、申請專利範圍: 1.式I及II之三唑化合物,201103429 VII. Scope of application for patents: 1. Triazole compounds of formula I and II, Ύ 為3有卜2或3個選自Ν、〇及S之雜原子作為學成 的3-“—員飽和、部分不飽和或;: 環’其中該雜環可具有1、2、3或4個取代基汉5.、 Α為可經卜2、3或4個取代㈣取代之直鏈c 基橋; W Y R1 為 Ο、S 或 NR8 ; 、R2、R3及R4彼此獨立地選自氫、齒素、〇h、阳、 N02、CN、CVQ烧基、Ci_C4i 烧基、c2_C4烯基、 c2-c4齒烯基、c2-c4炔基、C2_C4鹵炔基、C3_C8環怎 基、c3-c8鹵環烷基' (^匕烷氧基、Ci_c4 _烷章 基、C丨-C4烯氧基、CVC4鹵烯氧基、c「cv炔氧基、 CrC:4鹵炔氧基、C3-Cs環烷氧基、C3_C8鹵環烷章 基、c丨-C4烷硫基、C丨-c4鹵烷硫基、CVC4烯硫基、 Ci-C4齒炔硫基、苯基、笨基_Ci_C4烷基、笨基_Ci_c4 烷氧基、苯氧基、苯硫基,其中最後5個提及基團中 的苯基部分可具有1、2、3、4或5個取代基R9;含有 149026.doc 201103429 1、 2或3個選自N、〇及S之雜原子作為環成員的3_、 ? 5-、6-或7-員飽和、部分不飽和或最大不飽和雜 環’其中§亥雜環可具有1、2或3個取代基R9 . C〇R^COORl〇、CONRl5Rl6、NRlVis((^Ri〇’, 其中上述基團中之脂族部分可具有i、2或3個取代基 R18,且其中上述基團中之環脂族部分可具有i、2或 3個取代基R19 ;或 R1及R2,或R3及R4,連同其所連接之碳原子一起形 成部分不飽和或最大不飽和5·、6_或7_員碳環,或含 有卜2或3個選自〇、SaN之雜原子作為環成員的: 分不飽和或最大不飽和5-、6·或7_員雜環;其中該碳 環或雜環可具有1、2或3個取代基r9 ; 各R5獨立地選自_素、0H、SH、N〇2、CN、 L 1 ·14 現 土、CVC4 齒院基、c2-c4稀基、c2_c4 _ 烯基、 炔基、c2-c4 _炔基、c3_c^貌基、c3_c^環院4 基、CVC4院氧基、cvc4函烧氧基、Ci_c4稀氧基、 CVC4南烯氧基、cvc:4炔氧基、C〗_C4鹵炔氧基、 C8環烷氧基、c3-c8_環烷氧基、Ci_C4烷硫^ C4i烷硫基、(^-(^烯硫基、Ci_c4_炔硫基、苯基1 笨基-q-C4烷基、苯基_Cl_C4烷氧基、苯氧基 '苯硫 基,其中最後5個提及基團中的苯基部分可具有丨^ 2、 3、4或5個取代基仏含有卜2或3個選’自N、〇 及S之雜原子作為環成員的3…4_、5_、6句_員飽 和、部分不飽和或最大不飽和雜環,其中雜環可具 149026.doc [SI 201103429 有 1、2 或 3 個取代基 R9 ; COR10、COOR10、 C〇NR】5R16、NR15R16及S(0)p R10,其中上述基團中 之脂族部分可具有1、2或3個取代基R18,且其中上 述基團中之環脂族部分可具有1、2或3個取代基 R19 ;或 連接於相鄰環原子上的兩個基團R5連同其所連接之 環原子一起形成部分不飽和或最大不飽和5-、6-或7-員碳環’或含有1、2或3個選自〇、S及N之雜原子作 為環成員的部分不飽和或最大不飽和5_、6_或7_員雜 環;其中該碳環或雜環可具有i、2或3個取代基尺9 ; R6係選自氫、cvcw院基、c^-c, C2-C,。函烯基、C2_Ciq快基、 院基、c2-C10稀基、 共基、C2-Ci〇鹵块基、C3-Ci 149026.doc 環烷基、C3-c10_環烷基、苯基、苯基_Ci_C4烷基,Ύ is 3 or 2 heteroatoms selected from ruthenium, osmium and S as a 3-"-saturated, partially unsaturated or; ring: wherein the heterocyclic ring may have 1, 2, 3 or 4 substituents 5., Α is a linear c-base bridge which can be substituted by 2, 3 or 4 substitutions (4); WY R1 is Ο, S or NR8; R2, R3 and R4 are independently selected from hydrogen , dentate, 〇h, cation, N02, CN, CVQ alkyl, Ci_C4i alkyl, c2_C4 alkenyl, c2-c4 alkenyl, c2-c4 alkynyl, C2_C4 haloalkynyl, C3_C8 cyclocaryl, c3- C8 halocycloalkyl '(^匕alkoxy, Ci_c4_alkylidene, C丨-C4 alkenyloxy, CVC4 haloalkenyloxy, c"cv alkynyloxy, CrC:4haloalkynyloxy, C3- Cs cycloalkoxy, C3_C8 halocycloalkane, c丨-C4 alkylthio, C丨-c4 haloalkylthio, CVC4 alkenylthio, Ci-C4 alkynylthio, phenyl, stupyl_Ci_C4 Alkyl, phenyl-Ci_c4 alkoxy, phenoxy, phenylthio, wherein the phenyl moiety of the last five mentioned groups may have 1, 2, 3, 4 or 5 substituents R9; .doc 201103429 1, 2 or 3 heteroatoms selected from N, 〇 and S as ring members 3_, ? 5-, 6- or 7-satisfy And a partially unsaturated or a maximum unsaturated heterocyclic ring wherein the §heheheterocyclic ring may have 1, 2 or 3 substituents R9. C〇R^COORl〇, CONRl5Rl6, NRlVis((^Ri〇', wherein the above group The aliphatic moiety may have i, 2 or 3 substituents R18, and wherein the cycloaliphatic moiety of the above group may have i, 2 or 3 substituents R19; or R1 and R2, or R3 and R4, Together with the carbon atoms to which they are attached, form a partially unsaturated or maximally unsaturated 5, 6 or 7-membered carbocyclic ring, or contain 2 or 3 heteroatoms selected from the group consisting of ruthenium and SaN as ring members: a saturated or maximally unsaturated 5-, 6 or 7-membered heterocyclic ring; wherein the carbocyclic or heterocyclic ring may have 1, 2 or 3 substituents r9; each R5 is independently selected from the group consisting of _, 0, SH, N 〇2, CN, L 1 ·14 soil, CVC4 tooth base, c2-c4 thin base, c2_c4 _ alkenyl, alkynyl, c2-c4 _ alkynyl, c3_c^ appearance base, c3_c^ ring hospital 4 base, CVC4, alkoxy, cvc4, alkoxy, Ci_c4, dioxyl, CVC4, butylene, cvc: 4 alkynyl, C, _C4, haloalkoxy, C8 cycloalkoxy, c3-c8, cycloalkoxy Base, Ci_C4 alkyl sulfide ^ C4i alkylthio group, (^-(^-enethio group, Ci_c4_) Thio group, phenyl 1 phenyl-q-C4 alkyl group, phenyl-Cl_C4 alkoxy group, phenoxy 'phenylthio group, wherein the phenyl moiety in the last 5 mentioned groups may have 丨^2 3, 4 or 5 substituents containing 2 or 3 selected from the hetero atom of N, 〇 and S as ring members 3...4_, 5_, 6 sentences _ member saturated, partially unsaturated or maximum unsaturated a ring wherein the heterocyclic ring may have 149026.doc [SI 201103429 has 1, 2 or 3 substituents R9; COR10, COOR10, C〇NR] 5R16, NR15R16 and S(0)p R10, wherein the lipid in the above group The moiety may have 1, 2 or 3 substituents R18, and wherein the cycloaliphatic moiety of the above group may have 1, 2 or 3 substituents R19; or two groups attached to adjacent ring atoms R5, together with the ring atom to which it is attached, forms a partially unsaturated or maximally unsaturated 5-, 6- or 7-membered carbocyclic ring' or contains 1, 2 or 3 heteroatoms selected from the group consisting of ruthenium, S and N as ring members. a partially unsaturated or maximally unsaturated 5-, 6- or 7-membered heterocyclic ring; wherein the carbocyclic or heterocyclic ring may have i, 2 or 3 substituents 9; R6 is selected from the group consisting of hydrogen, cvcw, and c ^-c, C2-C,. Alkenyl, C2_Ciq fast radical, decentral, c2-C10 dilute, co-group, C2-Ci〇 halo block, C3-Ci 149026.doc cycloalkyl, C3-c10_cycloalkyl, phenyl, benzene Base _Ci_C4 alkyl, -、μ θ ti’j 5 -或6 -員飽和、部分不飽和-, μ θ ti’j 5 - or 6-member saturated, partially unsaturated HI之基團HI group A 201103429 其中 Het、A、Υ、r1、R2、r3及r4係如式j及π中所定 義;及 #為連接至分子其餘部分之連接點; R係選自氫、Ci-CiQ炫基、C〗-C1Q齒炫《基、C2-C1()稀基、 c2-c10ii 烯基、C2_Ci〇 快基、C2_Ci〇 鹵炔基、C3_Ci〇 %烷基、C^Cio鹵環烷基、苯基、苯基-CVC4烷基, 其中最後2個提及基團中的苯基部分可具有1、2、 3、4或5個取代基R11,含有丨、2或3個選自n、〇及S 之雜原子作為環成員的5_或6-員飽和、部分不飽和或 芳族雜環,其中該雜環可具有1、2或3個取代基 R丨丨 ’ -C( = 〇)R丨2、_C( = S)Ri2、_s(〇)2Rl2、_CN、 -P(=Q)R13R14及 Μ ; 各R7獨立地選自鹵素、〇Η、SH、NR15R16、(^-(:4烧基、 cvcu齒烧基、C2-C4烯基、C2_C4|i 婶基、c2_c^ 基、c2-c4鹵炔基、CVC4烧氧基、Ci-C4鹵烷氧基、 C1-C4烧硫基及c「C4鹵院硫基,其中上述基團中之脂 族部分可具有1、2或3個取代基R18 ;或 連接於兩個相鄰碳原子上的兩個基團連同其所連 接之碳原子一起形成3-、4-、5-、6-或7-員飽和、部 分不飽和或最大不飽和碳環’或含有1、2或3個選自 〇、S及N之雜原子作為環成員的3-、4-、5-、6-或7 員飽和、部分不飽和或最大不飽和雜環,其中該碳 環或雜環可具有1、2或3個取代基R9 ; ί 149026.doc 201103429 R8係選自氫、CN、(VC4烧基、CVC4齒烧基、c2-c4烯 基、c2-c4齒烯基、C2_C4炔基、c2_C4li 炔基、Ci_c4 烧氧基' C,-C4鹵烷氧基、苯基、苯基-Cl_c4烷基, 其中最後2個提及基團中的苯基部分可具有1、2、 3、4或 5個取代基尺9 ; c〇Rio、c〇〇Rl0、c〇nr15r16 及 S(0)pR10 ; 各R9獨立地選自鹵素、〇H、SH、NRi5R16、CN、N02、 Cl-C4烧基、Ci-C4 _ 烷基、C2-C4烯基、C2-C4 _ 烯 基、c2-c4炔基、c2_C4-炔基、Ci_C4炫氧基、Ci-C4 鹵烷氧基、Ci-C4烷硫基及Cl_c4_烷硫基,其中上述 基團中之脂族部分可具有1、2或3個取代基R18 ; 各汉10獨立地選自氫、C,-C4烧基、Cl_C4_烧基、C2_C4 基、C2_C4鹵烯基、C丨-C4胺基烷基、苯基、苯基_C丨- C4烧基’其中最後2個提及基團中的苯基部分可具有 1 2 3、4或5個取代基R9,及含有1、2或3個選自 之雜原子作為環成員的5 -或6-員飽和、部分 不飽和或芳族雜環,其中該雜環可具有i、2或3個取 代基R9 ; 各妙獨立地選自自素、〇H、SH、NRi5R16、CN、N02、 Cl C4烧基、Cl~C4 _院基、C2-C4烯基、C2-C4鹵烯 基C2 C4块&quot;基、C2_C4 _炔基、CVC4烧氧基、CVC4 鹵烧氧基、a — « h烧硫基及(^-(:4鹵烷硫基,其中上述 12基團中之脂族部分可具有1、2或3個取代基R18 ; R 2係選自氫、K γ ρ 10炫基、CrC!—烧基,、CVCu院氧 149026.doc 201103429 基、CrCw鹵烷氧基、CrCw胺基烷基、c3-c】0環燒 基、C3_C丨〇鹵環烷基、苯基、苯基_C]_C4烷基,其中 最後2個提及基團中的苯基部分可具有1、2、3、4或 5個取代基R11 ’含有1、2或3個選自N、Ο及S之雜原 子作為環成員的5-或6-員飽和、部分不飽和或芳族雜 環’其中該雜環可具有1、2或3個取代基R11,及 NRI5R16 ; R13及R14彼此獨立地選自C〗-C丨〇烷基、C丨-C丨〇鹵烷基、 CVC,。稀基、C2-C1()i 烯基、C2-C,。炔基、C2-C10l| 炔基、(:3-(:10環烷基、C3-C〗〇鹵環烷基、CVCw烷氧 基、CVCw鹵烷氧基、CVC4-烷氧基-CVCw烷基、 Ci-C4-烷氧基-〇:〗-(:〗()烷氧基、Ci-Cw烷硫基、Ci-C,。 鹵烷硫基、(:2-(:10稀氧基、C2-C10-烯硫基、(:2-(:10炔 氧基、C2-CiG-快硫基、C3-Ci()環烧氧基、C3-C1()-環 烷硫基、苯基、苯基烷基、苯硫基、苯基 c4烷氧基及NR15R16 ; 各R15獨立地選自氫及c〗-c8烷基; 各R16獨立地選自氫、Ci-C8烷基、苯基及苯基-Ci-Q烷 基; 或R 5及R16—起形成直鏈C4或(1!5伸烧基橋或基團 _CH2CH2〇CH2CH2-或 _ch2ch2nr17ch2ch2-; 各R17獨立地選自氫及(:1-(:4烷基; 各獨立地選自硝基、CN、OH ' SH、COR丨0、 COOR1。、c〇NR15R16、NR15R16、C3-C4 烧基、c3_ 149026.doc 201103429 C6齒環烧基、(^-山烷氧基、CVC4鹵烷氧基、c3_c6 %燒氧基(cycloaloxy)、苯基及苯氧基; 各R獨立地選自琐基、CN、OH、SH、COR10、 c〇〇R10、c〇NR15R16、nr15r16、Cl_c4院基、Cl_c4 齒燒基、匚3-(26環烧基、C3-C6鹵環烧基、C1-C4院氧 基、Ci-C:4鹵烷氧基、Cs-C:6環烷氧基、苯基及苯氧 基; Q為0或s ; M為金屬陽離子相等物或式(NRaRbR(:Rd)+之銨陽離子, 其中Ra、Rb、Rc及Rd彼此獨立地選自氫、C|_C丨〇烷 基、苯基及苄基,其中最後2個提及基團中的苯基部 刀可具有1、2或3個獨立地選自以下之取代基:鹵 素、CN、石肖基、Cl_C4烧基、Ci_C4i| 院基、Ci_C4^ 氧基、(VC4鹵烷氧基及NR15R16 ; m 為ο、1或2 ;及 Ρ 為1或2 ; 及其農業上可接受之鹽。 2-如。胃求項1之式I及II之化合物,其中Het為含有1、2或3 個選自N、Ο及S之雜原子作為環成員的5_或6_員雜芳 環,其中該雜芳環可具有1、2、3或4個取代基尺5。 3.如請求項2之式I及II之化合物,其中Het為選自吡啶基、 嘧啶基、呋喃基、噻吩基、吡咯基、吡唑基、咪唑基、 噁唑基、異噁唑基、噻唑基、異噻唑基及三唑基之5-或 6-員雜芳環,其中該雜芳環可具有丨、2、3或4個,較佳^ 149026.doc 201103429 或2個取代基r5。 4.如請求項3之式I及π之化合物,其中Het為選自吡啶基、 嗟吩基及噻唑基之5_或6-員雜芳環’較佳為吡啶基,其 中該雜芳環可具有1、2、3或4個,較佳1或2個取代基 R5。 5 ·如前述請求項中任一項之式I及II之化合物,其中R!、 R2、R3及R4彼此獨立地選自氫、齒素、〇H、SH、N02、 CN、CVC4烷基、Cl-C4 鹵烷基、CVC4烷氧基 基、烷氧基、Cl-C4烷氧基-C!-C4烷氧基及(^-(:4鹵 烧氧基’較佳選自氫、氟、氯、溴、Cl_C4烷基、Cl_c4 ifi炫•基、C丨-C4烷氧基及C丨-C4鹵烷氧基。 6. 如前述請求項中任一項之式I及π之化合物,其中各尺5獨 立地選自自素、0H、SH、N〇2、CN、C]_C4烧基、Ci_C4 函烧基、C”C4烧氧基-Cl-C4烧基、CVQ烧氧基、Cl_C4 烧氧基-CrC4烷氧基及Cl-C4鹵烷氧基,較佳選自氣、 氣、溴、Ci-C4烧基、c,_c4_烷基、Cl_c4燒氧基及^心 鹵烷氧基。 7. 如前述請求項中任一項之式丨及11之化合物,其中係 選自Cl-C4燒基、Ci-C2齒烷基、c〗-c4烧氧基、Ci_c2i烷 氧基、苯基、苯氧基及NR15R16,其中R15為氫,R16係選 自氮、(VC道基及笨基,或RijRi6均為Ci_C4院基。 8. 如前述請求項中任一項之式之化合物,其中r6係選 自氫、Ci-C4垸基、_c(=〇)r!2、_s(〇)2Ri2、CN、m及式 III之基團。 [SI 149026.doc 201103429 9.如請求項8之式I及II之化合物,其中R6係選自氣、甲 基、乙基、丙基、異丙基、·&lt;:(=0)(:Η3、、 -C(=0)N(CH3)2、CN、式III之基團、鹼金屬陽離子及% Cu2+ 〇 10. 如前述請求項中任一項之式I及II之化合物,其中Rea係選 自氫、(^(:4烷基、-S(0)2R12及-C(=0)R12。 11. 如前述請求項中任一項之式I及Π之化合物,其中A為直 鏈C2或C3伸烷基橋’其中該伸烷基橋個氣原子可 經1或2個取代基R7置換,其中各R7獨立地選自Ci_c4院 基、eve*鹵烷基、cvq烷氧基、cvc4烷氧基_Ci_C4烧 氧基及C^-C4鹵烧氧基,較佳選自甲基、乙基、甲氧芙、 乙氧基及甲氧基甲氧基,或連接於相鄰碳原子上的兩個 取代基R7連同其所連接之碳原子一起形成環戊基戋琿己 基環。 义 12. 如前述請求項中任一項之式1及„之化合物其中γ為 Ο。 13. 如前述請求項中任一項之式之化合物, 六Υ ΓΠ马〇。 14. 一種式IV之化合物,A 201103429 wherein Het, A, Υ, r1, R2, r3 and r4 are as defined in formulas j and π; and # is the point of attachment to the rest of the molecule; R is selected from hydrogen, Ci-CiQ stimuli, C〗 - C1Q Toothing "Base, C2-C1 () dilute, c2-c10ii alkenyl, C2_Ci 〇 fast radical, C2_Ci 〇 haloalkynyl, C3_Ci 〇 % alkyl, C ^ Cio halocycloalkyl, phenyl a phenyl-CVC4 alkyl group, wherein the phenyl moiety in the last two mentioned groups may have 1, 2, 3, 4 or 5 substituents R11, containing ruthenium, 2 or 3 selected from n, oxime and a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic ring having a hetero atom of S as a ring member, wherein the heterocyclic ring may have 1, 2 or 3 substituents R 丨丨 ' -C( = 〇)R丨2, _C(=S)Ri2, _s(〇)2Rl2, _CN, -P(=Q)R13R14 and Μ; each R7 is independently selected from the group consisting of halogen, hydrazine, SH, NR15R16, (^-(:4) Base, cvcu dentate group, C2-C4 alkenyl group, C2_C4|i fluorenyl group, c2_c^ group, c2-c4 haloalkynyl group, CVC4 alkoxy group, Ci-C4 haloalkoxy group, C1-C4 sulfur-burning group and c "C4 halogen thio, wherein the aliphatic moiety of the above group may have 1, 2 or 3 substituents R18; or Two groups on adjacent carbon atoms together with the carbon atom to which they are attached form a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated carbon ring' or contain 1, 2 or 3 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated heterocyclic rings selected from the group consisting of a hetero atom of hydrazine, S and N as a ring member, wherein the carbocyclic or heterocyclic ring The ring may have 1, 2 or 3 substituents R9; ί 149026.doc 201103429 R8 is selected from the group consisting of hydrogen, CN, (VC4 alkyl, CVC4 dentate, c2-c4 alkenyl, c2-c4 alkenyl, C2_C4 Alkynyl, c2_C4li alkynyl, Ci_c4 alkoxy 'C, -C4 haloalkoxy, phenyl, phenyl-Cl_c4 alkyl, wherein the phenyl moiety in the last two mentioned groups may have 1, 2 3, 4 or 5 substituent base 9; c〇Rio, c〇〇R10, c〇nr15r16 and S(0)pR10; each R9 is independently selected from halogen, 〇H, SH, NRi5R16, CN, N02, Cl -C4 alkyl, Ci-C4 _ alkyl, C2-C4 alkenyl, C2-C4-alkenyl, c2-c4 alkynyl, c2_C4-alkynyl, Ci_C4 decyloxy, Ci-C4 haloalkoxy, Ci a -C4 alkylthio group and a Cl_c4_alkylthio group, wherein the aliphatic moiety in the above group may have 1, 2 or 3 substituents R18; each Han 10 is independently selected from the group consisting of hydrogen, C, -C4 alkyl, Cl_C4_alkyl, C2_C4, C2_C4 haloalkenyl, C丨-C4 aminoalkyl, phenyl, phenyl _ The phenyl moiety of the C 2 -C 4 alkyl group wherein the last 2 of the groups may have 1, 2 3, 4 or 5 substituents R 9 and 1 , 2 or 3 hetero atoms selected from the group as ring members a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic ring wherein the heterocyclic ring may have i, 2 or 3 substituents R9; each independently selected from the group consisting of arginine, hydrazine H, SH, NRi5R16, CN, N02, Cl C4 alkyl, Cl~C4 _院, C2-C4 alkenyl, C2-C4 haloalkenyl C2 C4 block &quot; base, C2_C4 _ alkynyl, CVC4 alkoxy, CVC4 halogen alkoxy , a — « h-sulfuryl group and (^-(: 4-haloalkylthio group, wherein the aliphatic moiety of the above 12 groups may have 1, 2 or 3 substituents R18; R 2 is selected from hydrogen, K γ ρ 10 炫, CrC!—alkyl, CVCu, 149026.doc 201103429, CrCw haloalkoxy, CrCw aminoalkyl, c3-c] 0 ring alkyl, C3_C丨〇 halocycloalkyl Phenyl, phenyl-C]-C4 alkyl, of which the last two refer to the phenyl moiety in the group a 5- or 6-membered saturated, partially unsaturated or aromatic having 1, 2, 3, 4 or 5 substituents R11' containing 1, 2 or 3 heteroatoms selected from N, fluorene and S as ring members a heterocyclic ring wherein the heterocyclic ring may have 1, 2 or 3 substituents R11, and NRI5R16; R13 and R14 are independently of each other selected from C-C alkyl, C丨-C丨〇 haloalkyl, CVC ,. Dilute, C2-C1()i alkenyl, C2-C,. Alkynyl, C2-C10l|alkynyl, (3-(:10-cycloalkyl, C3-C)-halohalocycloalkyl, CVCw alkoxy, CVCw haloalkoxy, CVC4-alkoxy-CVCw , Ci-C4-alkoxy-oxime:--: (: () alkoxy, Ci-Cw alkylthio, Ci-C, haloalkylthio, (: 2-(: 10 diloxy) , C2-C10-enylthio, (: 2-(:10 alkynyloxy, C2-CiG-fast thio, C3-Ci() ring alkoxy, C3-C1()-cycloalkylthio, benzene a group, a phenylalkyl group, a phenylthio group, a phenyl c4 alkoxy group, and NR15R16; each R15 is independently selected from the group consisting of hydrogen and c--c8 alkyl; each R16 is independently selected from the group consisting of hydrogen, Ci-C8 alkyl, and benzene. And phenyl-Ci-Q alkyl; or R 5 and R16 together form a linear C4 or (1! 5 stretching bridge or group -CH2CH2〇CH2CH2- or _ch2ch2nr17ch2ch2-; each R17 is independently selected from Hydrogen and (: 1-(:4 alkyl; each independently selected from nitro, CN, OH 'SH, COR丨0, COOR1., c〇NR15R16, NR15R16, C3-C4 alkyl, c3_149026.doc 201103429 C6 dentate, (^-alkenyloxy, CVC4 haloalkoxy, c3_c6 % cycloaloxy, phenyl and phenoxy; each R is independently selected from the group consisting of trityl, CN, OH, SH , COR1 0, c〇〇R10, c〇NR15R16, nr15r16, Cl_c4, Ke_c4, 匚3-(26 ring alkyl, C3-C6 halocycloalkyl, C1-C4 alkoxy, Ci-C: 4-haloalkoxy, Cs-C: 6 cycloalkoxy, phenyl and phenoxy; Q is 0 or s; M is a metal cation equivalent or an ammonium cation of the formula (NRaRbR(:Rd)+, wherein Ra , Rb, Rc and Rd are independently of each other selected from the group consisting of hydrogen, C|_C丨〇alkyl, phenyl and benzyl, wherein the phenyl moiety in the last two mentioned groups may have 1, 2 or 3 independently Substituents selected from the group consisting of halogen, CN, schlossyl, Cl_C4 alkyl, Ci_C4i|, Ci_C4 oxy, (VC4 haloalkoxy and NR15R16; m is ο, 1 or 2; and Ρ is 1 or 2 And an agriculturally acceptable salt thereof. 2-. The compound of the formula I and II of the stomach of claim 1, wherein Het is a ring member having 1, 2 or 3 hetero atoms selected from N, oxime and S. a 5- or 6-membered heteroaryl ring, wherein the heteroaryl ring may have 1, 2, 3 or 4 substituent bases 5. 3. A compound of the formulae I and II according to claim 2, wherein Het is selected from the group consisting of pyridine Base, pyrimidinyl, furyl, thienyl, pyrrolyl, pyrazolyl, imidazole a 5- or 6-membered heteroaryl ring of oxazolyl, isoxazolyl, thiazolyl, isothiazolyl and triazolyl, wherein the heteroaryl ring may have hydrazine, 2, 3 or 4, preferably ^ 149026.doc 201103429 or 2 substituents r5. 4. The compound of the formula I and π of claim 3, wherein Het is a 5- or 6-membered heteroaryl ring selected from pyridyl, porphinyl and thiazolyl, preferably pyridyl, wherein the heteroaryl ring There may be 1, 2, 3 or 4, preferably 1 or 2 substituents R5. The compound of the formulae I and II according to any one of the preceding claims, wherein R!, R2, R3 and R4 are independently of each other selected from the group consisting of hydrogen, dentate, hydrazine H, SH, N02, CN, CVC4 alkyl, Cl-C4 haloalkyl, CVC4 alkoxy, alkoxy, Cl-C4 alkoxy-C!-C4 alkoxy and (^-(:4 halooxy) are preferably selected from hydrogen and fluorine. , chloro, bromine, Cl_C4 alkyl, Cl_c4 ifixanyl, C丨-C4 alkoxy and C丨-C4 haloalkoxy. 6. A compound of formula I and π according to any of the preceding claims, Wherein each ruler 5 is independently selected from the group consisting of self-priming, 0H, SH, N〇2, CN, C]_C4 alkyl, Ci_C4 functional alkyl, C"C4 alkoxy-Cl-C4 alkyl, CVQ alkoxy, Cl_C4 alkoxy-CrC4 alkoxy group and Cl-C4 haloalkoxy group, preferably selected from the group consisting of gas, gas, bromine, Ci-C4 alkyl, c, _c4_alkyl, Cl_c4 alkoxy and halothane 7. A compound of the formula 11 and 11 according to any one of the preceding claims, wherein the compound is selected from the group consisting of Cl-C4 alkyl, Ci-C2 dentate alkyl, c--c4 alkoxy, Ci_c2i alkoxy. And phenyl, phenoxy and NR15R16, wherein R15 is hydrogen, R16 is selected from nitrogen, (VC base and stupid, or RijRi6 are all Ci_C4 hospital base. 8. The compound of any one of the preceding claims, wherein r6 is selected from the group consisting of hydrogen, Ci-C4 fluorenyl, _c(=〇)r!2, _s(〇)2Ri2, CN, m and formula III [SI 149026.doc 201103429 9. The compound of the formulae I and II of claim 8, wherein R6 is selected from the group consisting of gas, methyl, ethyl, propyl, isopropyl, ·&lt;: (=0 (: Η3,, -C(=0)N(CH3)2, CN, a group of formula III, an alkali metal cation, and a % Cu2+ 〇10. A compound of formulas I and II according to any of the preceding claims. And wherein Rea is selected from the group consisting of hydrogen, (^(:4 alkyl, -S(0)2R12, and -C(=0)R12. 11. The compound of formula I and hydrazine according to any one of the preceding claims, wherein A is a linear C2 or C3 alkylene bridge where the gas atom of the alkylene bridge can be replaced by 1 or 2 substituents R7, wherein each R7 is independently selected from the group consisting of Ci_c4, eve* haloalkyl, cvq Alkoxy, cvc4 alkoxy_Ci_C4 alkoxy and C^-C4 halo alkoxy, preferably selected from methyl, ethyl, methoxy, ethoxy and methoxymethoxy, or linked Two substituents R7 on adjacent carbon atoms together with the carbon atom to which they are attached form a cyclopentyl group The compound of the formula 1 and the compound of any one of the preceding claims, wherein γ is Ο. 13. A compound of the formula of any of the preceding claims, hexamidine. 14. A compound of formula IV, 其中 Het、A、Υ、R1、R2 R3及R4係如請求項 1至6及11 149026.doc 201103429 至13中任—項所定義。 15 16. 17. 18. 19. 20. 21. 一種農業組合物’其包含至少一種如請求項1至14令任 項之式I、11及/或1V之化合物或其農業上可接受之鹽 及液體或固體載劑。 一種如請求項1至14中任—項之式卜Η及/或IV之化合物 的用途,其用於防治有害真菌。 -種防治有害真菌之方法,其中該真菌、其棲息地或經 保護以免受真菌侵襲之材料或植物、或土壤或繁殖材料 係以有效量之至少—種式卜„及/或1¥之化合物處理,1 中化合物Ι、π&amp;ιν係如請求項1至14中任一項所定義。'、 一種種子,每⑽公斤種子包含U公克至1G公斤量的至 少一種式I、Π及/或以之化合物,其中化合物卜 係如請求項1至14中任一項所定義。 -種醫藥組合物,纟包含至少一種如請求項m中任 一項之式I、π及/或…之化合物或其醫藥學上可接受之 鹽及至少一種醫藥學上可接受之載劑。 一種如請求項1至14中任-項之式I、II及/或以之化合物 或其醫藥學上可接受之鹽的用途,其係用於製備供治療 癌症或病毒感染之藥劑或用於製備抗黴藥劑。 -種治療癌症或病毒感染或對抗動物致病性或人類致病 性真菌之方法,其包含以至少—種如請求項】至14中任 一項之式I、II及/或IV之化合物、至少 可接受之鹽或如請求項19之醫藥組合物 個體。 一種其醫藥學上 治療有此需要之 149026.doc -10· i S] 201103429 四、指定代表圖: (一) 本案指定代表圖為:(無) (二) 本代表圖之元件符號簡單說明: 五、本案若有化學式時,請揭示最能顯示發明特徵的化學式:Wherein Het, A, Υ, R1, R2 R3 and R4 are as defined in claims 1 to 6 and 11 149026.doc 201103429 to 13. 15 16. 17. 18. 19. 20. 21. An agricultural composition comprising at least one compound of the formulae I, 11 and/or 1V as claimed in claims 1 to 14 or an agriculturally acceptable salt thereof And a liquid or solid carrier. A use of a compound of the formulae of any of claims 1 to 14 and/or IV for controlling harmful fungi. - a method for controlling harmful fungi, wherein the fungus, its habitat or a material or plant protected by fungi, or soil or propagation material is an effective amount of at least - a compound of the formula and/or 1 The compound Ι, π &amp; ιν is as defined in any one of claims 1 to 14. ', a seed, each (10) kg of seeds comprising at least one of Formula I, Π and/or from U gram to 1 G kg. A compound, wherein the compound is as defined in any one of claims 1 to 14. A pharmaceutical composition comprising at least one compound of the formula I, π and/or ... according to any one of the claims m Or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable carrier. A compound of the formula I, II and/or according to any one of claims 1 to 14 or a pharmaceutically acceptable compound thereof Use of a salt for the preparation of a medicament for the treatment of cancer or a viral infection or for the preparation of an anti-fungal agent. A method of treating a cancer or a viral infection or combating an animal pathogenic or human pathogenic fungus, comprising At least - such as request items] to 14 Any of the compounds of formula I, II and/or IV, at least an acceptable salt or a pharmaceutical composition according to claim 19, 149026.doc -10· i S] of a pharmaceutical treatment thereof 201103429 IV. Designated representative map: (1) The representative representative of the case is: (none) (2) The symbolic symbol of the representative figure is simple: 5. If there is a chemical formula in this case, please disclose the chemical formula that best shows the characteristics of the invention: LSI 149026.docLSI 149026.doc
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