TW201103430A - Triazole compounds carrying a sulfur substituent XII - Google Patents

Triazole compounds carrying a sulfur substituent XII Download PDF

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TW201103430A
TW201103430A TW099120001A TW99120001A TW201103430A TW 201103430 A TW201103430 A TW 201103430A TW 099120001 A TW099120001 A TW 099120001A TW 99120001 A TW99120001 A TW 99120001A TW 201103430 A TW201103430 A TW 201103430A
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het
group
compound
formula
combination
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TW099120001A
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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
    • A61P35/00Antineoplastic agents

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

201103430 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, 149027.doc 201103430201103430 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 fungicidal agent Uses and intermediate compounds used in the method of manufacture thereof. [Prior Art] Prevention and 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 the triazoles 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 applicable salts, 149027.doc 201103430

其中 ArWhere Ar

Het 〇j 有 1、2Λ 八 、3、4或5個取代基R2之苯基,或盔二有1、2或3個選自N、。及S之雜原子作為環成員 的 3·、4-、5-、6-十 1 〇s -員飽和、部分不飽和或芳族 ’其中該雜環可具有1、2、3或4個取代基^有1、2或3個選自N、㈣之雜原子作為環成 於、3_、4_、5_、6_或7_員飽和、部分不飽和或芳 R4雜環’其中該雜環可具有1、2、3或4個取代基Het 〇j has 1, 2, 8, 3, 4 or 5 substituents R2 phenyl, or helmet 2 has 1, 2 or 3 selected from N,. And a hetero atom of S as a member of the ring, 3, 4, 5, 6 - 10 1 〇 s - saturated, partially unsaturated or aromatic - wherein the heterocyclic ring may have 1, 2, 3 or 4 substitutions a hetero atom having 1, 2 or 3 selected from N, (d) as a ring, a 3, 4, 5, 6 or 7-membered saturated, partially unsaturated or aromatic R 4 heterocyclic ring wherein the heterocyclic ring Has 1, 2, 3 or 4 substituents

A Y R1 為可經1、2 境基橋; 為 0、S 或 NR6 ; 系選自氮、Cl_Cl〇院基、C Γ1 rfe «. 10 Ll_Ci〇 鹵院基、CVC,。烯 =、C2-Cl。函稀基、c2_Ci〇炔基、C2_c〗。齒快基、 3 ^⑺環烷基、(:3-(:10鹵環烷基、笨基、某 C4燒基,其中最後2個提及之基團中的笨㈣分; 具有1、2、3、4或5個取代基R7,及含有!、2或3 :固選自Ν、Ο及S之雜原子作為環成員的5_或6_員飽 σ、部分不飽和或芳族雜環,其中該雜環可具有 、3或4個取代基R5取代之直鏈^{5伸 149027.doc [S] 201103430 1、2或3個取代基R7 ;或在m*0之情況下, 〇 J選 自-C(=0)R、-C(=S)R8、_s(〇)2r8、_CN、ρ(υ^丨。 Μ及式ΠΙ之基團A Y R1 is a 1, 2 -based bridge; 0, S or NR6; is selected from nitrogen, Cl_Cl〇, C Γ1 rfe «. 10 Ll_Ci〇 halogen courtyard, CVC. Alkene =, C2-Cl. The function is dilute, c2_Ci decynyl, C2_c. Teeth, 3 ^(7)cycloalkyl, (: 3-(:10 halocycloalkyl, stupyl, some C4 alkyl, the stupid (four) of the last two mentioned groups; with 1, 2 , 3, 4 or 5 substituents R7, and containing ?, 2 or 3: 5 or 6-membered sigma, partially unsaturated or aromatic heteropoly which are selected from the heteroatoms of ruthenium, osmium and S as ring members a ring wherein the heterocyclic ring may have a linear chain substituted with 3 or 4 substituents R5; {5 extension 149027.doc [S] 201103430 1, 2 or 3 substituents R7; or in the case of m*0, 〇J is selected from the group consisting of -C(=0)R, -C(=S)R8, _s(〇)2r8, _CN, ρ(υ^丨.

其中among them

Ar、Het、A及Y係如式中所定義·且 #為連接至分子其餘部分之連接點;Ar, Het, A, and Y are as defined in the formula and # is the point of attachment to the rest of the molecule;

Rla 係選自 f、r r h « a 烧基、Cl_Ci〇_ 烧基、C2_C|〇稀 基、c2-c1G_歸基、c2_Ciq快基、C2_Ciq鹵炔基、 C^C10環烷基、C^Cio鹵環烷基 '笨基、苯基-Cl-4元基其中最後2個提及基團中的苯基部分可具 2 3、4或5個取代基R7,含有1、2或3個選 f ^ 〇及s之雜原子作為環成員的5_或6_員飽和、 不飽和或芳族雜環,其中該雜環可具有1、2 或3個取代基尺7,-c(=0)R8、-c(=s)R8、-S(0)2R8、 •CN、-P(=Q)R9Ri〇及 Μ; 各R獨立地選自占本 k 自齒素、OH、SH、N02、CN、Cl-C4烷 基、c】-c4_烧基' c2_c4烯基、C2_C4_稀基、οι炔基、 c2-c4 鹵 炔基、 c3_c8環烷基 、 c3_C8 鹵環 燒基、C ρ Λ- 4* 1丄4院氣基、Ci-C*鹵烷氧基、(^-(:4烯氧 149027.doc 201103430 基、CVC4鹵烯氧基、Cl-c4炔氧基、CVC4鹵炔氧 基、〇3-(:8環烷氧基、c3-c8鹵環烷氧基、cvq烧 硫基、CVC4鹵烷硫基、d-G烯硫基、CVC4 1I块 硫基 '苯基、苯基-CVC:4烷基、苯基-(^-(^烷氧 基、苯氧基、笨硫基,其中最後5個提及之基團中 的苯基部分可具有1、2、3' 4或5個取代基汉11 ; 含有1、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,其中該雜環可具有 R,COR丨2、c〇〇Ri2、c〇nr13rU、抓丨決丨4及 S(0)pR ,其中上述基團中之脂族部分可具有1、2 或3個取代基Rl5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Ri6 ;或 連接於相鄰碳環原子上之兩個基團r2連同立所連 接之碳環原子-起形成部分不飽和或最大不飽和 5_、6-或7-員碳環或含有1、2或3個選自〇、削 •5之雜原子料環成員的部分不飽和或最大不飽和 6或7.貝雜環;其中該碳環或雜環可具有卜〕 或3個取代基Rn ; 各R獨立地選自鹵素、〇h A SH、N02、CN、C丨-C4烷 土 Ci-C4_ 烷基、c Γ h块基、C-C… 2-C4㈣基、C2· 烷農 2 4 、 、C”Cs環烷基' C3-C8鹵環 土、ci_C4燒氧基、c 基、 丨-C4鹵烷氧基、C丨-C4烯氧Rla is selected from the group consisting of f, rrh « a alkyl group, Cl_Ci〇_ alkyl, C2_C| fluorene, c2-c1G_group, c2_Ciq fast group, C2_Ciq haloalkynyl group, C^C10 cycloalkyl group, C^Cio Halocycloalkyl 'phenyl, phenyl-Cl-4 group wherein the phenyl moiety of the last two mentioned groups may have 2 3, 4 or 5 substituents R7, containing 1, 2 or 3 a heterocyclic atom of ^ and s as a 5- or 6-membered saturated, unsaturated or aromatic heterocyclic ring of a ring member, wherein the heterocyclic ring may have 1, 2 or 3 substituent base blocks 7, -c (=0) R8, -c(=s)R8, -S(0)2R8, •CN, -P(=Q)R9Ri〇 and Μ; each R is independently selected from the group consisting of ko, OH, SH, N02 , CN, Cl-C4 alkyl, c]-c4_alkyl group c2_c4 alkenyl, C2_C4_thinyl, οι alkynyl, c2-c4 haloalkynyl, c3_c8 cycloalkyl, c3_C8 halocycloalkyl, C ρ Λ- 4* 1丄4 courtyard gas base, Ci-C* haloalkoxy, (^-(:4 olefin 149027.doc 201103430 base, CVC4 haloalkenyloxy, Cl-c4 alkynyloxy, CVC4 haloalkyne Oxy, 〇3-(:8 cycloalkoxy, c3-c8 halocycloalkoxy, cvq thiol, CVC4 haloalkylthio, dG olefinylthio, CVC4 1I thiol'phenyl, phenyl -CVC: 4 alkyl, phenyl-(^-(^ Alkoxy, phenoxy, thiol, wherein the phenyl moiety of the last five mentioned groups may have 1, 2, 3' 4 or 5 substituents 11; contains 1, 2 or 3 a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring selected from the group consisting of N, hydrazine and 8 heteroatoms, wherein the heterocyclic ring may have R,COR丨2, c〇〇Ri2, c〇nr13rU, 丨4 and S(0)pR, wherein the aliphatic moiety of the above group may have 1, 2 or 3 substituents Rl5 and wherein the above group The cycloaliphatic moiety may have 1, 2 or 3 substituents Ri6; or the two groups r2 attached to adjacent carbon ring atoms together with the attached carbon ring atom - form part of the unsaturated or maximum unsaturation a 5-, 6- or 7-membered carbocyclic ring or a partially unsaturated or maximally unsaturated 6 or 7. beryllylene ring containing 1, 2 or 3 heteroatom ring members selected from the group consisting of ruthenium and rhodium; wherein the carbon The ring or heterocyclic ring may have or have three substituents Rn; each R is independently selected from the group consisting of halogen, 〇h A SH, N02, CN, C丨-C4 alkane Ci-C4_alkyl, c Γ h block, CC... 2-C4(4), C2·Alkane 2 4 , , C”Cs naphthenes 'C3-C8 halocycloalkyl soil, ci_C4 burn group, C group, Shu -C4 haloalkoxy, C -C4 alkenyloxy Shu

Cl-C4鹵烯氧基、Γ Ρ ^ 炔氧基、c丨-c4鹵炔氧 149027.doc 201103430 基、C3-C8環烧氧基、C3-C8鹵環燒氧基、燒 硫基、CVC4鹵烷硫基、Cl_c4稀硫基、Ci_c4函炔 硫基、苯基、苯基-Cl-C4烷基、苯基_C〗_C4烷氧 基、苯氧基、苯硫基,其中最後5個提及之基團中 的苯基部分可具有1、2、3、4或5個取代基Ri 1 ; 含有1 ' 2或3個選自N、〇及S之雜原子作為環成員 的3-、4_、5_、6-或1 2 3 4_員飽和、部分不飽和或最大 不飽和雜環’其中該雜環可具有!、2或3個取代基 R1 丨;COR!2、COORi2、c〇nr13r14、皿丨、丨4: S(0)pR12,其中上述基團中之脂族部分可具有u 或3個取代基R15且其中上述其 /、T上返暴團中之環脂族部分 可具有1、2或3個取代基R»5 ;或 連接於(雜環Ar之)相鄰環屌+卜+工, 州衣原于上之兩個基團R3連 同其所連接之環原子一起形忐 、办咸部分不飽和或最大 不飽和5-、5_或1_員碳環或含有卜2或3個選自 〇、^N之雜原子作為環成員的部分不飽和戍最 大不飽和5-' 6-或7_員雜環; 丹甲該石反%或雜環可 具有1、2或3個取代基R11 ;Cl-C4 haloalkenyloxy, Γ Ρ ^ alkynyloxy, c丨-c4 haloacetylene 149027.doc 201103430 base, C3-C8 cycloalkoxy, C3-C8 halocycloalkyloxy, sulfur-burning, CVC4 Haloalkylthio, Cl_c4 disulfide, Ci_c4 alkynylthio, phenyl, phenyl-Cl-C4 alkyl, phenyl_C_c4 alkoxy, phenoxy, phenylthio, of which the last five The phenyl moiety in the group mentioned may have 1, 2, 3, 4 or 5 substituents Ri 1 ; 3 - 3 or 3 heteroatoms selected from N, oxime and S as ring members , 4_, 5_, 6- or 1 2 3 4 4_membered saturated, partially unsaturated or most unsaturated heterocyclic ring 'where the heterocyclic ring can have! , 2 or 3 substituents R1 丨; COR! 2, COORi2, c〇nr13r14, 丨, 丨 4: S(0)pR12, wherein the aliphatic moiety of the above group may have u or 3 substituents R15 And wherein the cycloaliphatic moiety in the above-mentioned /, T-back violent group may have 1, 2 or 3 substituents R»5; or attached to (heterocyclic Ar) adjacent ring 屌+卜+工, state The two groups R3 on the enamel together with the ring atom to which they are attached are shaped, and the salty partially unsaturated or maximally unsaturated 5-, 5- or 1-member carbon ring or contains 2 or 3 a hetero atom of 〇, ^N as a ring member, a partially unsaturated 戍 maximally unsaturated 5-' 6- or 7-membered heterocyclic ring; a dansylamine or a heterocyclic ring may have 1, 2 or 3 substituents R11 ;

各R 其 r r 上 NVJ2 ' CN ' 基、燒基、C2_C4歸基 r ^ 自烯基、C2- 4炔基、c2-c4鹵块基、C3_c ^ u r,^ 衣坑基、C3_C8鹵環 兀基、烷氧基、 I49027.doc 1 丞 Cl-C4鹵烯氧基、C丨-c4炔氧* 2 其^ P 4炔氧基、c,-c4卣炔氧 3 基、C3-C8環烷氧基、c3_c _ 4 囚衣烷氧基、c丨-c4烷 5 > C Γ ^ ^ ^ 兀虱基、C,-C4烯氧 201103430 硫基、(^-(:4_烷硫基、Ci_C4硫基、Ci_C4齒炔 硫基、苯基、苯基-Cl_C4烷基、笨基_Ci_c4烷氧 基、苯氧基、苯硫基,其中最後5個提及之基團中 的苯基部分可具有1、2、3、4或5個取代基Ru ; 含有1、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’其中該雜環可具有1、2或3個取代基 R" ; COR12、CO〇R〗2、c〇nr13rM 皿13ri4 及 S(0)PR ,其中上述基團中之脂族部分可具有丄、2 或3個取代m其中上述基團中之環脂族部分 可具有1、2或3個取代基r!6;或 連接於(Het之)相鄰環原子上之兩個基團r4連同其 所連接之環原子—起形成部分不絲或最大不飽 和5-、6-或7_員碳環或含有丨、2或3個選自〇、§及 N之雜原子作為環成員的部分不飽和或最大不餘 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Rn ; 各R獨立地選自鹵素、〇H、SH ' nr13r14、烷 基、cam基、C2_C4稀基、C2_c碯稀基、& ^快基、C2-C4函炔基、c,-c4烧氧基、Ci_C4函烧 氧基、eve:4烷硫基及Ci_C4_烷硫基,其中上述 基團中之脂族部分可具有丨、2或3個取代基…5;或 連接於兩個相鄰碳原子上的兩個基團R5連同其所 連接之碳原子—起形成3·、4_、5·、6_或7_員飽Each R has its NVJ2 ' CN ' group on rr, alkyl group, C2_C4 group-based r ^ self-alkenyl group, C2- 4 alkynyl group, c2-c4 halogen block group, C3_c ^ ur, ^ pit group, C3_C8 halogen ring fluorenyl group , alkoxy, I49027.doc 1 丞Cl-C4 haloalkenyloxy, C丨-c4 alkyneoxy* 2 2 P 4 alkynyloxy, c,-c4 decyneoxy 3, C3-C8 cycloalkoxy Base, c3_c _ 4 alkoxy, c丨-c4 alkane 5 > C Γ ^ ^ ^ thiol, C,-C4 olefin oxygen 201103430 thio, (^-(: 4_alkylthio, Ci_C4 sulfur a base, a Ci_C4 alkynylthio group, a phenyl group, a phenyl-Cl_C4 alkyl group, a phenyl-Ci_c4 alkoxy group, a phenoxy group, a phenylthio group, wherein the phenyl moiety in the last five mentioned groups may have 1, 2, 3, 4 or 5 substituents Ru; 3-, 4, 5...6_ or 7_members saturated with 1, 2 or 3 heteroatoms selected from N, 〇 and 8 as ring members a partially unsaturated or a maximum unsaturated heterocyclic ring wherein the heterocyclic ring may have 1, 2 or 3 substituents R"; COR12, CO〇R, 2, c〇nr13rM dish 13ri4 and S(0)PR, wherein The aliphatic moiety in the group may have 丄, 2 or 3 substituents m wherein the cycloaliphatic moiety of the above group may have 1, 2 or 3 substitutions r;6; or two groups r4 attached to an adjacent ring atom of (Het) together with the ring atom to which they are attached form a partially non-filament or maximum unsaturated 5-, 6- or 7-member carbon ring Or a partially unsaturated or maximally unsaturated 5- or 6- or 7-membered heterocyclic ring containing hydrazine, 2 or 3 heteroatoms selected from the group consisting of hydrazine, § and N; wherein the carbocyclic or heterocyclic ring may have 1, 2 or 3 substituents Rn; each R is independently selected from the group consisting of halogen, hydrazine H, SH ' nr13r14, alkyl, cam group, C2_C4 dilute group, C2_c碯 dilute group, & ^ fast radical, C2-C4 letter Alkynyl, c, -c4 alkoxy, Ci_C4 functional alkoxy, eve:4 alkylthio and Ci_C4_alkylthio, wherein the aliphatic moiety of the above group may have an anthracene, 2 or 3 substituents... 5; or two groups R5 attached to two adjacent carbon atoms together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7_

[SI 149027.doc 201103430 和、部分不飽和或最大不飽和碳環或含有丨' 2、 或3個選自〇·、之雜原子作為環成員的3_、4_ 、%、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丨' 2或3個取代基 R11 ; R6 係選自氫、CN、Γ r ρ a 门 虱 N Cl-C4烧基、C丨-C4IS 烧基、c2_c4 烯基、C2-C4函烯基、c2_c4块基、C2_C』快基、 氧基、Cl_c』烧氧基、苯基、苯基 烧基,其中最後2個提及基團中的苯基部分可具有 CONR13R丨4及 s(〇)pRi2 ; 各R7獨立地選自齒素、〇h、sh、nr13r14、cn n〇2、 I c4烧基院基、c2_c4^基、c2_Cj 烯 基、c2-c4炔基、 c4鹵烷氧基、c 中上述基團中之 R15 ; C2-C4鹵炔基、cvc4烷氧基、(V 1-C4烷硫基&Cl_c4鹵烷硫基,其 脂族部分可具有1、2或3個取代基 r! 係k自氫、CVCw貌基、Ci_Ci〇_烧基、烧 氧基'CrC“烷氧基、Ci_Ci❶胺基烧基、C3_C1。 環烷基、C3-Cl。南環烷基、苯基、苯基㈣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R7,含有丨、2或3個選自 Ν Ο及S之雜原子作為環成員的^或卜員飽和、部 分不飽和或芳族雜環,其中該雜環可具有卜2或3 149027.doc 201103430 個取代基R7,及NR13R14 ; R9及R10彼此獨立地選自cvcw烷基、Cl_Ci〇鹵烷基、C2_ c10 稀基、C2-Ci〇_ 稀基、C2-C10 块基、C2-C10 鹵炔 基、eve!。環炫:基、c3-c1Qii環燒基、Ci_c10炫氧 基、Ci-Cio鹵烷氧基、Ci-C^烷氧基_Cl_c10烷基、 Ci-C4烧氧基-Ci-Cio烧氧基、(^-(^。炫硫基、Ci-Ci〇ii烧硫基、C2-C1G烯氧基、c2-C1G烯硫基、C2-〇10炔氧基、C2-C1()炔硫基、c3-C1()環烧氧基、c3-Cio環烷硫基、苯基、苯基_c丨-c4烷基、苯硫基、 笨基-CVC4烷氧基及NR13R14 ; 各R丨1獨立地選自鹵素、OH、SH、NR13R丨4、CN、 N02、(VC4烧基、C丨-C4 li 院基、c2_c4烯基、c2_ c4 _烯基、C2-C4炔基、c2-c4鹵炔基、烷氧 基、(ν(:4ι|烧氧基、Ci-C^烧硫基及Ci_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R15 ; 各R12獨立地選自氫、Cl_c4烷基、Ci_c4_烷基、c2_c4 烯基、CrC4鹵烯基、CVC4胺基烷基、苯基、苯 基-C^C4烷基,其中最後2個提及之基團中的苯基 部分可具有1、2、3、4或5個取代基尺1〗,及含有 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R"; 各R13獨立地選自氫&Cl-c8烷基;[SI 149027.doc 201103430 and 3, 4, 4, %, 6 or 7-members, partially unsaturated or maximally unsaturated carbocyclic or containing 丨' 2, or 3 heteroatoms selected from 〇·, as ring members a saturated, partially unsaturated or maximum unsaturated heterocyclic ring wherein the carbocyclic or heterocyclic ring may have 丨' 2 or 3 substituents R11; R6 is selected from the group consisting of hydrogen, CN, Γr ρ a threshold N Cl-C4 Base, C丨-C4IS alkyl, c2_c4 alkenyl, C2-C4 alkenyl, c2_c4, C2_C, fast, oxy, Cl_c, alkoxy, phenyl, phenyl, the last two The phenyl moiety in the reference group may have CONR13R丨4 and s(〇)pRi2; each R7 is independently selected from the group consisting of dentate, 〇h, sh, nr13r14, cn n〇2, I c4, and c2_c4 ^, c2_Cj alkenyl, c2-c4 alkynyl, c4 haloalkoxy, R15 in the above group in c; C2-C4 haloalkynyl, cvc4 alkoxy, (V 1-C4 alkylthio & Cl_c4 haloalkylthio, the aliphatic moiety of which may have 1, 2 or 3 substituents r! k from hydrogen, CVCw appearance group, Ci_Ci〇-alkyl, alkoxy 'CrC“ alkoxy, Ci_Ci fluorenyl Calcination, C3_C1. Cycloalkyl, C3-Cl. Cycloalkyl, benzene The phenyl moiety of the phenyl(tetra)alkyl group wherein the last two of the groups mentioned may have 1 2 3 4 or 5 substituents R7, containing fluorene, 2 or 3 heteroatoms selected from the group consisting of ruthenium and osmium. a saturated or partially unsaturated or aromatic heterocyclic ring as a ring member, wherein the heterocyclic ring may have a substituent 2 or 3 149027.doc 201103430 substituents R7, and NR13R14; R9 and R10 are independently selected from the group consisting of cvcw Alkyl, Cl_Ci〇 haloalkyl, C2_c10 dilute, C2-Ci〇_ dilute, C2-C10 block, C2-C10 haloalkynyl, eve!. cyclodextrin: c, c3-c1Qii cycloalkyl, Ci_c10 methoxy, Ci-Cio halooxy, Ci-C^ alkoxy_Cl_c10 alkyl, Ci-C4 alkoxy-Ci-Cio alkoxy, (^-(^. thiol, Ci -Ci〇ii, sulfur-based, C2-C1G-alkenyloxy, c2-C1G-alkenylthio, C2-indole10-alkynyloxy, C2-C1()alkynylthio, c3-C1()cycloalkoxy, c3 -Ciocycloalkylthio, phenyl, phenyl-c丨-c4 alkyl, phenylthio, phenyl-CVC4 alkoxy and NR13R14; each R丨1 is independently selected from the group consisting of halogen, OH, SH, NR13R丨4. CN, N02, (VC4 alkyl, C丨-C4 li, c2_c4 alkenyl, c2_c4_alkenyl, C2-C4 alkynyl, c2-c4 haloalkynyl, alkoxy a group, (ν(:4ι| alkoxy, Ci-C^sulfuryl and Ci_c4_alkylthio), wherein the aliphatic moiety in the above group may have 1, 2 or 3 substituents R15; each R12 is independent Selected from hydrogen, Cl_c4 alkyl, Ci_c4_alkyl, c2_c4 alkenyl, CrC4 haloalkenyl, CVC4 aminoalkyl, phenyl, phenyl-C^C4 alkyl, of which the last two mentioned groups The phenyl moiety in the phenyl moiety may have 1, 2, 3, 4 or 5 substituents, and 5, or 6-members containing 1, 2 or 3 heteroatoms selected from N, oxime and S as ring members. a saturated, partially unsaturated or aromatic heterocyclic ring wherein the heterocyclic ring may have 1, 2 or 3 substituents R"; each R13 is independently selected from hydrogen & Cl-c8 alkyl;

[SI 149027.doc -10· 201103430 各R14獨立地選自氫、CVCs烷基、苯基及苯基-(^-山烷 基; 或R13及R14—起形成直鏈(^或…伸烷基橋或基團 -CH2CH2OCH2CH2-或-CH2CH2NR17CH2CH2-; 各R】5獨立地選自硝基、CN、OH、SH、COR12、 COOR12、c〇NR13R14 ; NR13R14、c3-c6環烷基、 C3-C6鹵環烷基、CVC4烷氧基、(:,-04鹵烷氧基、 匸3-0^6環烧氧基(CyCi〇ai〇Xy)、苯基及苯氧基; 各R16獨立地選自硝基、CN、〇H、SH、COR12、 coor12、C0NRnRl4、NR"Rl4、Ci_c4烧基、Ci_ C4i烧基、(:3-(:6環烷基、c3-c6鹵環烷基、cvc4 烧氧基、(VC4鹵烷氧基、c3-C6環烷氧基、苯基 及苯氧基; 各R17獨立地選自氫及(:1_(:4烷基; Q 為〇或s ; M 為金屬陽離子相等物或式(NRaRbRcRd)+之銨陽離 子,其中Ra、Rb ' 1^及Rd彼此獨立地選自氫、 CI0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:-素、CN、硝基、Cl-C4烧基、Cl_C4 _烷 基、G-C4烷氧基、Cl_C4鹵烷氧基及NRi3Ri4 ; m 為〇、1或2 ;且 P 為1或2。 本發明亦提供式I及Π三唑化合物及/或其農業上有用鹽 149027.doc 201103430 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丨及/或^(亦及/或式ιν ;參 見下文)之三唑化合物及/或其農業上可接受之鹽及適合載 劑的殺真菌組合物。適合之農業上可接受之載劑描述如 下。 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、滞轉異構體 (atr〇p1SOmers)及幾何異構體。熟習此項技術者應瞭解,當 -種立體異構體相對於其它立體異構體增濃時或當與其它 立體異構體分離時,其可更具活性及/或可顯示有益效 果°另外’熟,練技術人員知道如何分離、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!及„可互為位置/雙鍵異構體,至少在 基團RVW相同之情況下。在R1(當然以及Rla)為氫之情況 下,各別化合物I及II為互變異構體。 適合的農業上有用鹽尤其為陽離子之鹽或酸之酸加成 鹽’該等陽離子及陰離子分別對化合物咖之殺真菌作用 無不利影響。因此,適合之陽離 之陽離子尤其為鹼金屬離子,較 佳納及卸之離子;驗土金屬離子,較佳m鋇之離 子;及過渡金屬離子,較佳鐘,、鋅及鐵之離子;以及 敍離子(若需要,其可具有1至4個CVC4烧基取代基及⑷ 個苯基或节基取代基)’車交佳二異丙銨、四甲銨 149027.doc 201103430 銨、三甲苄銨;此外’鱗離子,锍離子,較佳三(Ci c4烧 基)疏’及氧化疏(sulfoxonium)離子,較佳三(c丨_c4烧美) 氧化銃。 有用之酸加成鹽之陰離子主要為氯離子、溴離子'、氣離 子、硫酸氫根、硫酸根、磷酸二氫根、麟酸氫根、填酸 根、硝酸根、碳酸氫根、碳酸根、六氟矽酸根、六氟填酸 根、苯曱酸根,以及C1-C4烷酸之陰離子,較佳為曱酸 根、乙酸根、丙酸根及丁酸根。其可由I或Π與相應陰離子 之酸(較佳鹽酸、氫溴酸、硫酸、填酸或硝酸)反應形成。 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 下於所討論之取代基或取代基部分中可能的碳原子數目。 鹵素:氟、氣、溴及碘; 烷基及烷氧基、烷氧基烷基、烷氧基烷氧基、烷基羰 基、烷硫基羰基、胺基烷基、烷基胺基、二烷基胺基、烷 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((CVC4烷基)、1至6個(CVC6烷基)、1 至8個(CrCs烷基)或1至1〇個(CfCw烷基)碳原子之飽和直 鏈或支鏈烴基。C2-C3烷基為乙基、正丙基或異丙基。 C2烷基為曱基或乙基。烷基為曱基、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-甲基丁基、2,2-二 149027.doc -13- 201103430 甲基丙基、1-乙基丙基、u_二甲基丙基、U二甲基丙 基、己基、1-甲基戊基、2-甲基戊基、3-甲基戊基、4_甲 基戊基、1,1-二甲基丁基、丨,2_二甲基丁基、込3二甲基丁 基、2,2-二甲基丁基' 2,3_二甲基丁基、3,3_二甲基丁基、 1-乙基丁基、2-乙基丁基、u,2_三甲基丙基、三甲 基丙基、1-乙基-1-曱基丙基或^乙基_2_甲基丙基。ei_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。CrCw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鹵烷基)、個(Ci_C3鹵烷 基)、1至4個(C〗-C4函烧基)、1至6個((:,-(:6函烧基)、1至8 個(Ci-Cg自烧基)、1至1〇個鹵烧基)或2至1〇個(c2-C10鹵烷基)碳原子之直鏈或支鏈烷基(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置 換·詳言之為Ci-C2鹵烧基,諸如氣曱基、漠曱基、二氣 曱基、三氣曱基、氟曱基、二氟甲基、三氟曱基、氯氟曱 基、二氣敗曱基、氣二氟曱基、1-氣乙基、1_漠曱基、1_ 氟乙基、2-氟乙基、2,2-二氟乙基、2,2,2-三氟乙基、2-氣-2-氟乙基、2-氯-2,2-二氟乙基、2,2-二氣-2-氟乙基、2,2,2-二氣乙基或五敗乙基。C1-C3鹵烧基另外為(例如三 氟丙-2-基、3,3,3-三氟丙基或七氟丙基。匸丨-匕鹵烷基另外 為(例如)1-氯丁基、2-氣丁基、3-氣丁基或4-氣丁基。[SI 149027.doc -10· 201103430 Each R14 is independently selected from the group consisting of hydrogen, CVCs alkyl, phenyl and phenyl-(^-alkenyl; or R13 and R14 together form a straight chain (^ or ... alkyl) Bridge or group -CH2CH2OCH2CH2- or -CH2CH2NR17CH2CH2-; each R]5 is independently selected from the group consisting of nitro, CN, OH, SH, COR12, COOR12, c〇NR13R14; NR13R14, c3-c6 cycloalkyl, C3-C6 halogen a cycloalkyl group, a CVC4 alkoxy group, a (:,-04 haloalkoxy group, a fluorene 3-0^6 ring alkoxy group (CyCi〇ai〇Xy), a phenyl group and a phenoxy group; each R16 is independently selected from the group consisting of Nitro, CN, 〇H, SH, COR12, coor12, C0NRnRl4, NR" Rl4, Ci_c4 alkyl, Ci_C4i alkyl, (: 3-(:6 cycloalkyl, c3-c6 halocycloalkyl, cvc4 Oxyl, (VC4 haloalkoxy, c3-C6 cycloalkoxy, phenyl and phenoxy; each R17 is independently selected from hydrogen and (:1_(:4 alkyl; Q is 〇 or s; M is a metal cation equivalent or an ammonium cation of the formula (NRaRbRcRd)+, wherein Ra, Rb '1^ and Rd are independently of each other selected from the group consisting of hydrogen, CI0 alkyl, phenyl and benzyl, of which the last two are mentioned in the group The phenyl moiety may have 1, 2 or 3 substituents independently selected from the group consisting of -N, CN, nitro, Cl-C4 alkyl, Cl_C4_alkyl, G-C4 alkoxy, Cl_C4 haloalkoxy and NRi3Ri4; m is 〇, 1 or 2; and P is 1 or 2. The invention also provides the use of the formula I and the oxatriazole compound and/or its agriculturally useful salt 149027.doc 201103430 for controlling harmful fungi. The invention further provides for the inclusion of the formula 丨 and/or ^ (also and/or Formula ιν; see below) Triazole compounds and/or agriculturally acceptable salts thereof and fungicidal compositions suitable for carriers. Suitable agriculturally acceptable carriers are described below. Compounds I and II may be one or more Stereoisomers exist. The various stereoisomers include enantiomers, diastereomers, atropisomers (atr〇p1SOmers) and geometric isomers. Those skilled in the art will appreciate that When the stereoisomers are concentrated relative to other stereoisomers or when separated from other stereoisomers, they may be more active and/or may exhibit beneficial effects. In addition, the skilled practitioner knows how to Separating, enriching and/or selectively preparing the stereoisomers. The compounds of the invention may It is now a mixture of stereoisomers (such as racemates), individual stereoisomers or optically active forms. It should be understood that the compounds! and „ can be mutually positional/double bond isomers, at least in the same group RVW In the case of In the case where R1 (and of course Rla) is hydrogen, the respective compounds I and II are tautomers. Suitable agriculturally useful salts are, in particular, salts of cations or acid addition salts of acids. The cations and anions, respectively, have no adverse effect on the fungicidal action of the compound. Therefore, suitable cationic cations are especially alkali metal ions, preferably neutralized ions; soil metal ions, preferably m钡 ions; and transition metal ions, preferably clocks, zinc and iron ions; And a sulphur ion (if necessary, it may have 1 to 4 CVC4 alkyl substituents and (4) phenyl or a sulfhydryl substituent) 'Cardipine diisopropylammonium, tetramethylammonium 149027.doc 201103430 ammonium, trimethylbenzyl Ammonium; in addition, 'scale ions, barium ions, preferably three (Ci c4 alkyl) sparse' and sulfoxonium ions, preferably three (c丨_c4 burnt) cerium oxide. Useful anion of acid addition salt is mainly chloride ion, bromide ion, gas ion, hydrogen sulfate, sulfate, dihydrogen phosphate, hydrogen hydride, acidate, nitrate, bicarbonate, carbonate, The hexafluoroantimonate, hexafluororesidate, benzoate, and the anion of the C1-C4 alkanoic acid are preferably decanoate, acetate, propionate and butyrate. It may be formed by reacting I or hydrazine with an acid of the corresponding anion, preferably hydrochloric acid, hydrobromic acid, sulfuric acid, 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 each case in the substituent or substituent moiety in question. Halogen: fluorine, gas, bromine and iodine; alkyl and alkoxy, alkoxyalkyl, alkoxyalkoxy, alkylcarbonyl, alkylthiocarbonyl, aminoalkyl, alkylamino, two Alkyl moiety in alkylamino, alkylaminocarbonyl, dialkylaminocarbonyl, alkylthio, alkylsulfonyl and the like: having 1 to 2 alkyl groups, 2 or 3 (C2-C3 alkyl), 1 to 4 ((CVC4 alkyl), 1 to 6 (CVC6 alkyl), 1 to 8 (CrCs alkyl) or 1 to 1 (CfCw alkyl) carbon a saturated linear or branched hydrocarbon group of an atom. The C2-C3 alkyl group is an ethyl group, a n-propyl group or an isopropyl group. The C2 alkyl group is a mercapto group or an ethyl group. The alkyl group is a mercapto group, an ethyl group, a propyl group or a different group. Propyl, butyl, 1-methylpropyl (second butyl), 2-methylpropyl (isobutyl) or 1,1-dimethylethyl (t-butyl Cl-C6 alkyl Further, for example, pentyl, 1-mercaptobutyl, 2-mercaptobutyl, 3-methylbutyl, 2,2-di 149027.doc -13-201103430 methylpropyl, 1-B Propyl, u-dimethylpropyl, U dimethylpropyl, hexyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methyl Pentyl, 1,1-dimethylbutyl, anthracene, 2-dimethylbutyl, hydrazine 3 dimethylbutyl, 2,2-dimethylbutyl' 2,3-dimethylbutyl Base, 3,3-dimethylbutyl, 1-ethylbutyl, 2-ethylbutyl, u, 2-trimethylpropyl, trimethylpropyl, 1-ethyl-1-anthracene The propyl group or the ethyl 2-methylpropyl group. The ei_c8 alkyl group is also additionally, for example, heptyl, octyl, 2-ethylhexyl and positional isomers thereof. The CrCw alkyl group is additionally (for example) a mercapto group, a mercapto group, a 2-propylheptyl group, a 3-propylheptyl group, and a positional isomer thereof. Haloalkyl group: having 1 to 2 (CVC2 haloalkyl), one (Ci_C3 haloalkyl), 1 to 4 (C--C4 functional base), 1 to 6 ((:,-(:6), 1 to 8 (Ci-Cg self-burning), 1 to 1 halogen) a linear or branched alkyl group of 2 to 1 (c2-C10 haloalkyl) carbon atom (as described above), wherein some or all of the hydrogen atoms of such groups may be as described above Halogen atom replacement. In detail, it is a Ci-C2 halogen group, such as gas sulfhydryl, desert sulfhydryl, dihalohydrazino, trimethyl fluorenyl, fluoroindolyl, difluoromethyl, trifluoromethyl, chloro fluorine Sulfhydryl, dioxin, fluorinated fluorenyl, 1-fluoroethyl, 1-methylidene, 1_fluoroethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2 ,2-trifluoroethyl, 2-gas-2-fluoroethyl, 2-chloro-2,2-difluoroethyl, 2,2-di-gas-2-fluoroethyl, 2,2,2- Di-ethyl or penta-ethyl. The C1-C3 halo group is additionally (for example, trifluoropropan-2-yl, 3,3,3-trifluoropropyl or heptafluoropropyl. The radical is additionally, for example, 1-chlorobutyl, 2-oxobutyl, 3-oxobutyl or 4-oxobutyl.

Ci-C1()羥烧基:具有1至2個(C〗-C2羥院基)、1至4個(C】-C4經烧基)、2至4個(C2-C4經烧基)、1至6個經烧Ci-C1 () hydroxyalkyl group: having 1 to 2 (C 〗 - C 2 hydroxy groups), 1 to 4 (C) - C4 burned base, 2 to 4 (C2-C4 burned) 1 to 6 burned

L SI 149027.doc • 14· 201103430 基)、2至6個(C2-C6經烧基)、uwC〗-c8經院基)、2至8 個(C2-C8經烧基)、1至10個(Cl_Cl〇M院基)或2至1〇個(C2_ Cl〇輕烧基)碳原子之直鏈或支鏈烧基(如上所述),其中至 少一個II原子經备基置換,諸如2-羥乙基或3-經丙基。 烯基及烯氧基、烯硫基、烯基羰基及其類似物中之烯基 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稀基)、3至8個(C3-C8烯基)、2至10個(C2-C10稀基) 或3至10個(C3-C|G稀基)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、丨_ 丁烯基、2_ 丁烯基、3-丁烯基、1-曱基-i_丙烯基、2_甲基_丨·丙烯基、 1-曱基-2-丙烯基或2-甲基-2-丙烯基,或例如,c2_c6^ 基’諸如乙烯基、1-丙烯基、2-丙烯基、ι_甲基乙烯基、 1-丁烯基、2-丁烯基、3-丁烯基、ι_曱基丙烯基、2_甲 基-1-丙烯基、1-甲基-2-丙烯基、2-甲基-2-丙烯基、1-戊 烯基、2-戊烯基、3-戊烯基、4-戊烯基、1-甲基-i_ 丁烯 基、2-曱基-1-丁烯基、3-曱基-i_ 丁烯基、卜曱基_2_ 丁烯 基、2-曱基-2-丁烯基、3 -曱基-2-丁烯基、1-曱基-3-丁烯 基、2-曱基-3-丁烯基、3-甲基-3-丁烯基、丨,1_二曱基_2·丙 烯基、1,2-二曱基-1-丙烯基、1,2_二曱基_2_丙烯基、丨_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、i_甲基_丨_戊烯基、2_曱基_ 1-戊浠基、3 -曱基-1-戊烯基、4-甲基_1_戊烯基、1_曱基_2_ 戊烯基、2-曱基-2-戊烯基、3-曱基-2-戊烯基、4-曱基-2- 149027.doc -15· 201103430 戊烯基、1-曱基-3-戊烯基、2-甲基-3-戊烯基、3_曱基_3_ 戊烯基、4-曱基_3-戊烯基、1-曱基_4-戊烯基、2_曱基_4_ 戊烯基、3-甲基_4_戊烯基、4-曱基-4-戊烯基、M_二曱基_ 2-丁烯基、1,1-二曱基_3_丁烯基、込厶二曱基]丁烯基、 1,2-二甲基-2-丁烯基、ι,2-二甲基-3-丁烯基、二甲基_ 1- 丁烯基、1,3-二曱基_2_丁烯基、1,3_二甲基_3_丁烯基、 2’2-—曱基-3-丁烯基、2,3-二甲基-1-丁烯基、2,3_二曱基_ 2- 丁烯基、2,3-二甲基-3-丁烯基、3,3-二曱基q•丁烯基、 3,3-一曱基-2-丁烯基' 1_乙基_ι_ 丁稀基、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、H2-三曱基_2_丙烯基、丨_乙基_1β 曱基-2-丙烯基、丨_乙基_2_甲基_丨_丙烯基 ' 丨_乙基_2曱基_ 2-丙烯基及其類似物; 鹵烯基及i烯氧基、_烯基羰基及其類似物中之_烯基 部分:具有2至4個(C2-C4鹵烯基)、2至6個(C2-C6鹵烯基)、 2至8個(C2-C8 _烯基)或2至10個(C2-C1() _烯基)碳原子及在 任意位置處之雙鍵的不飽和直鏈或支鏈烴基(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,例如氣乙烯基、氣烯丙基及 其類似物; 炔基及炔氧基、炔硫基、炔基羰基及其類似物中之炔基 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-C1G炔基) 或3至1 〇個(c3-C 1〇炔基)碳原子及一或兩個在任意位置處之 [S] I49027.doc -16· 201103430 參鍵的直鍵或支鍵煙基,例如’ C2-C4快基’諸如乙炔 基、1-丙炔基、2-丙炔基、1-丁炔基、2 -丁炔基、3 -丁块 基或1-甲基-2-丙快基,或例如,C2-C6炔基,諸如乙块 基、1-丙炔基、2-丙炔基' 1-丁炔基' 2-丁炔基' 3-丁炔 基、1-曱基-2-丙快基、1-戊快基、2 -戍块基、3 -戊块基、 4-戊炔基、1-曱基-2-丁炔基、1-甲基-3-丁炔基、2-曱基-3-丁炔基、3-曱基-1-丁炔基、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-甲基-2-戊炔基、1-曱基-3-戊炔基、1-甲基-4-戊炔基、2-甲基-3-戊炔基、2-曱基-4-戊炔基、3-曱基-1-戊炔基、3-甲基-4-戊炔基、4-曱基-1-戊炔基、4-甲基-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、3,3-二甲基-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-甲基-2-丙快基及其類似物; 鹵炔基及_炔氧基、_炔基羰基及其類似物中之齒炔基 部分:具有2至4個(CVC4鹵炔基)、2至6個(C2-C6鹵炔基)、 2至8個(C2-C8齒快基)或2至10個(C2-Clf)iS炔基)碳原子及一 或兩個在任意位置處之參鍵的不飽和直鏈或支鏈烴基(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; 環烷基及環烷氧基、環烷基羰基及其類似物中之環烷基 部分.具有3至6個(Cs-C:6環烷基)、3至8個(C3_C8環烷基)或 3至10個(C3_C1Q環烷基)碳環成員之單環飽和烴基,諸如, 149027.doc •17- 201103430 環辛基、環 環丙基、環丁基、環戊基、環己基、環庚基 壬基及環癸基; 鹵環烷基及鹵環烷氧基、_環烷基羰基及其類似物中之 i環烷基部分:具有3至6個(CrC6鹵環烷基)、3至8個 C8函環烧基)或3至_(C3_Ci〇_環炫基)碳環成員之單環 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、氣及溴)置換; 環稀基及環烯氧基、環稀基縣及其類似物中之環歸基 部分:具有3至6個(C3-C6環烯基)、π,%%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、:庚缚 基、環辛烯基、環壬烯基及環癸烯基; 齒環烯基及齒環烯氧基、鹵環烯基羰基及其類似物中之 鹵環烯基部分:具有3至6個((:3_(:61|環烯基)、3至8個(C3_ C8鹵環烯基)或3至10個(C3_Cl〇鹵環烯基)碳環成員之單環 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、氣及溴)置換;L SI 149027.doc • 14· 201103430 base), 2 to 6 (C2-C6 burned base), uwC〗-c8 via hospital base), 2 to 8 (C2-C8 burned base), 1 to 10 (Cl_Cl〇M) or 2 to 1 (C2_Cl〇 light alkyl) carbon or a linear or branched alkyl group (as described above), wherein at least one of the II atoms is replaced by a substituent, such as 2- Hydroxyethyl or 3-propyl. Alkenyl moiety in alkenyl and alkenyloxy, alkenylthio, alkenylcarbonyl and the like: having 2 to 4 (C2-C4 alkenyl), 2 to 6 (C2-C6 alkenyl), 2 Up to 8 (C2-C8 dilute), 3 to 8 (C3-C8 alkenyl), 2 to 10 (C2-C10 dilute) or 3 to 10 (C3-C|G dilute) carbon atoms And a monounsaturated linear or branched hydrocarbon group having 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, a fluorene-butene group Base, 2-butenyl, 3-butenyl, 1-indenyl-i-propenyl, 2-methyl-hydrazine-propenyl, 1-mercapto-2-propenyl or 2-methyl-2- Propylene group, or for example, c2_c6^ group such as vinyl, 1-propenyl, 2-propenyl, iota methyl, 1-butenyl, 2-butenyl, 3-butenyl, ι _mercaptopropenyl, 2-methyl-1-propenyl, 1-methyl-2-propenyl, 2-methyl-2-propenyl, 1-pentenyl, 2-pentenyl, 3- Pentenyl, 4-pentenyl, 1-methyl-i-butenyl, 2-mercapto-1-butenyl, 3-mercapto-i-butenyl, indolyl-2-butenyl, 2- Mercapto-2-butenyl, 3-mercapto-2-butenyl, 1- Mercapto-3-butenyl, 2-mercapto-3-butenyl, 3-methyl-3-butenyl, anthracene, 1-difluorenyl-2-propenyl, 1,2-dioxin 1-propenyl, 1,2-diindenyl-2-propenyl, oxime-ethyl-1-propenyl, 1-ethyl-2-propenyl, 1-hexenyl, 2-hexene , 3-hexenyl, 4-hexenyl, 5-hexenyl, i-methyl-hydrazine-pentenyl, 2-hydrazino-1-pentenyl, 3-mercapto-1-pentyl Alkenyl, 4-methyl-1-pentenyl, 1-hydrazino-2-pentenyl, 2-mercapto-2-pentenyl, 3-mercapto-2-pentenyl, 4-fluorenyl -2- 149027.doc -15· 201103430 Pentenyl, 1-mercapto-3-pentenyl, 2-methyl-3-pentenyl, 3-mercapto-3-indolyl, 4-mercapto _3-pentenyl, 1-decyl_4-pentenyl, 2-hydrazino-4-pentenyl, 3-methyl-4-pentenyl, 4-mercapto-4-pentenyl, M_dimercapto-2-butenyl, 1,1-diindenyl-3-butenyl, indenyl]butenyl, 1,2-dimethyl-2-butenyl, ι,2-dimethyl-3-butenyl, dimethyl-1-butenyl, 1,3-didecyl-2-butenyl, 1,3-dimethyl-3-butene Base, 2'2-mercapto-3-butenyl, 2,3-dimethyl-1-butenyl, 2,3-diindenyl-2-butene , 2,3-dimethyl-3-butenyl, 3,3-diindolyl q•butenyl, 3,3-indenyl-2-butenyl' 1_ethyl_ι_ Dilute, 丨_ethyl_2_butenyl, 1-ethyl-3-butenyl, 2-ethyl-1-butenyl, 2-ethyl-2-butenyl, 2-ethyl 3-butenyl, H2-trimethyl-2-propenyl, 丨_ethyl_1β decyl-2-propenyl, 丨_ethyl_2_methyl_丨_propenyl' 丨_B Base 2 fluorenyl-2-propenyl and analogs thereof; alkenyl group in the alkenyl group and the i-alkenyloxy group, the alkenylcarbonyl group and the like: having 2 to 4 (C2-C4 halogenated alkene) Base), 2 to 6 (C2-C6 haloalkenyl), 2 to 8 (C2-C8-alkenyl) or 2 to 10 (C2-C1()-alkenyl) carbon atoms and at any position a double-bonded unsaturated linear or branched hydrocarbon group (as described above) wherein some or all of the hydrogen atoms of such groups may be replaced by a halogen atom (especially fluorine, gas and bromine) as described above, such as Vinyl, allylic, and the like; alkynyl moiety in alkynyl and alkynyloxy, alkynylthio, alkynylcarbonyl, and the like: having 2 to 4 (C2-C4 alkynyl), 2 Up to 6 (C2-C6 alkynyl), 2 to 8 (C2-C8 alkynyl), 3 to 8 (C3-C8 alkynyl), 2 to 10 (C2-C1G alkynyl) or 3 to 1 fluorene (c3-C 1 decynyl) Carbon atom and one or two at any position [S] I49027.doc -16· 201103430 A direct bond or a bond group of a bond, such as 'C2-C4 fast group' such as ethynyl, 1-propynyl , 2-propynyl, 1-butynyl, 2-butynyl, 3-butenyl or 1-methyl-2-propanyl, or, for example, C2-C6 alkynyl, such as an alkenyl group, 1-propynyl, 2-propynyl '1-butynyl' 2-butynyl' 3-butynyl, 1-indolyl-2-propanyl, 1-pentyl, 2-indole Block group, 3-pentenyl group, 4-pentynyl group, 1-mercapto-2-butynyl group, 1-methyl-3-butynyl group, 2-mercapto-3-butynyl group, 3- Mercapto-1-butynyl, 1,1-dimercapto-2-propynyl, 1-ethyl-2-propynyl, 1-hexynyl, 2-hexynyl, 3-hexyne , 4-hexynyl, 5-hexynyl, 1-methyl-2-pentynyl, 1-mercapto-3-pentynyl, 1-methyl-4-pentynyl, 2-methyl 3-pentynyl, 2-mercapto-4-pentynyl, 3-mercapto-1-pentynyl, 3-methyl-4-pentynyl, 4-mercapto-1-pentyne Base, 4-methyl-2-pentynyl, 1,1-di 2-butynyl, 1,1-dimercapto-3-butynyl, 1,2-dimercapto-3-butynyl, 2,2-dimethyl-3-butynyl, 3 ,3-dimethyl-1-butynyl, 1-ethyl-2-butynyl, 1-ethyl-3-butynyl, 2-ethyl-3-butynyl, 1-ethyl 1-methyl-2-propanyl and the like; alkynyl moiety in alkynyl and ynkynyloxy, ynkynylcarbonyl and the like: having 2 to 4 (CVC4 haloalkynyl) ), 2 to 6 (C2-C6 haloalkynyl), 2 to 8 (C2-C8 tooth fast radical) or 2 to 10 (C2-Clf) iS alkynyl) carbon atoms and one or two in any a non-saturated linear or branched hydrocarbon group at a position (as described above) wherein some or all of the hydrogen atoms of the groups may be replaced by a halogen atom (especially fluorine, gas and bromine) as described above; a cycloalkyl moiety in a cycloalkyl group and a cycloalkyloxy group, a cycloalkylcarbonyl group, and the like. It has 3 to 6 (Cs-C: 6 cycloalkyl groups) and 3 to 8 (C3_C8 cycloalkyl groups). Or a monocyclic saturated hydrocarbon group of 3 to 10 (C3_C1Q cycloalkyl)carbocyclic members, such as 149027.doc • 17-201103430 cyclooctyl, cyclocyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl , cycloheptyl fluorenyl and cyclodecyl; i-cycloalkyl moiety of halocycloalkyl and halocycloalkoxy, cycloalkylcarbonyl and the like: having 3 to 6 (CrC6 halocycloalkyl) a monocyclic saturated hydrocarbon group of 3 to 8 C8 functional cycloalkyl) or 3 to _(C3_Ci〇_cyclohexyl) carbocyclic ring members (as described above), wherein some or all of the hydrogen atoms may be as described above Substitution of a halogen atom (especially fluorine, gas, and bromine); a ring-based moiety in a cycloaliphatic group and a cycloalkenyloxy group, a ring-like base, and the like: having 3 to 6 (C3-C6 cycloalkenyl groups), a monocyclic monounsaturated hydrocarbon group of π, %% cycloaliphatic) or 3 to 10 (C3-C1G cycloalkenyl) carbocyclic members, such as cyclopropenyl, cyclobutenyl, cyclopentenyl, cyclohexene a group: a heptyl group, a cyclooctenyl group, a cyclodecenyl group, and a cyclodecenyl group; a halocycloalkenyl group of a ring cycloalkenyl group and a ring cycloalkenyloxy group, a halocycloalkenylcarbonyl group, and the like: Monocyclic ring having 3 to 6 ((:3_(:61|cycloalkenyl)), 3 to 8 (C3_C8 halocycloalkenyl) or 3 to 10 (C3_Cl〇 halocycloalkenyl) carbon ring members Unsaturated hydrocarbon groups (as described above) 'some of them or There may be a hydrogen atom as a halogen atom (especially fluorine, bromine and gas) of the displacement;

CrC6環烷基-C,-C2烷基:如上所述之Ci_c2烷基殘基, 其中一個氫原子經C3-C6環烷基置換。實例為環丙基曱 基、環丁基甲基、環戊基甲基、環己基甲基、環丙基_卜乙 基、環丁基-1-乙基、環戊基_丨_乙基、環己基·丨_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_Ci〇環烷基-C1-C4烷基為如上所述之 q-c:4烷基殘基,其中一個氫原子經C3_Cig環烷基置換。除 [ 149027.doc -18· 201103430 了彼等以上提及的基團之外,C3-C6環烷基-Ci-CU烷基之實 例亦為環庚基曱基'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-i-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-1-丙基、環丙基-2-丙基、 環丙基-3-丙基、環丁基-1-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、壤庚基-2-丙基、環庚基-3-丙基、環辛基-1-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-1-丙基、環癸基_ 2-丙基、環癸基-3-丙基、環丙基-1- 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 丁基-2-丁基、環丁基-3-丁基、環丁基-4-丁基、環戊基_1_ 丁基、環戊基-2-丁基、環戊基-3-丁基、環戊基-4-丁基、 %己基-1-丁基、壞己基-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、環庚基-4-丁基、環辛基-1-丁基、環辛基-2-丁基、環 辛基-3-丁基、環辛基-4-丁基、環壬基-1-丁基、環壬基_2_ 丁基、環壬基-3-丁基、環壬基-4-丁基、環癸基丁基、 環癸基-2-丁基、環癸基-3-丁基、環癸基-4-丁基及其類似 物0 環烧基-Ci-C2烧基:如上所述之Ci-C〗烧基歹襄 基’其中一個氫原子經CrC6鹵環烷基置換。實例為丨_氯琴 149027.doc •19· 201103430 丙基甲基、ι·氣環丁基甲基、卜氯環戊基甲基 ' 卜氯環己 基甲基、1德環丙基小乙基、i'氣環丁基小乙基、卜氣環 戍基小乙基、1-氣環己基小乙基、i•氣環丙基_2·乙基、 k氣環丁基么乙基、i'氯環戊基乙基、卜氣環己基冬 乙基、氯環丙基甲基、2-氣環丁基甲基、2_氯環戊基甲 基、2-氣環己基甲基、2_氣環丙基+乙基、2'氯環丁基小 乙基、2-氣環戊基-卜乙基、2_氯環己基+乙基、^氣環丙 基_2-乙基、2-氣環丁基-2_乙基、2_氣環戊基_2•乙基、2_ 氣環己基-2-乙基、卜氟環丙基曱基、“氟環丁基甲基、卜 氟環戊基甲基、卜氟環己基甲基、κ氟環丙基]-乙基、卜 敗環丁基-r乙基、卜敗環戊基小乙基、卜氣環己基-卜乙 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、^氟環己基_2_乙基、2_氟環丙基曱基、氟環 丁基甲基、2-氟環戊基甲基、2-氟環己基甲基、2_氟環丙 基_1-乙基、2-氟環丁基-1-乙基、2_氟環戊基_丨·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 基乱%、戊基-2-乙基、2-環己基-2-乙基及其類似物。 Cs-C丨〇鹵環炫1基_c丨-C4烧基為如上所述之CrC4烧基殘基, 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。C^-C:2烷氧基為甲氧基或 乙氧基。C1-C3烧氧基另外為(例如)正丙氧基或1_曱基乙氧 基(異丙氧基)。Ci-C:4烷氧基另外為(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151_二曱 基乙氧基(第三丁氧基)。C^-C:6烷氧基另外為(例如)戊氧CrC6 cycloalkyl-C,-C2 alkyl: a Ci_c2 alkyl residue as described above wherein one hydrogen atom is replaced by a C3-C6 cycloalkyl group. Examples are cyclopropylindenyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, cyclopropyl-ethyl, cyclobutyl-1-ethyl, cyclopentyl-indole-ethyl, cyclohexyl.丨_Ethylcyclopropyl-2-ethyl, cyclobutyl-2-ethyl, cyclopentyl-2-ethylcyclohexyl-2-ethyl and the like. The C3_Ci〇cycloalkyl-C1-C4 alkyl group is a q-c:4 alkyl residue as described above in which one hydrogen atom is replaced by a C3_Cig cycloalkyl group. In addition to the groups mentioned above by [149027.doc -18· 201103430, examples of C3-C6 cycloalkyl-Ci-CU alkyl are also cycloheptyldecyl 'cyclooctylfluorenyl, ring. Indolyl, cyclodecylmethyl, cycloheptyl-1-ethyl, cyclooctyl-1-ethyl, cyclodecyl-i-ethyl, cyclodecyl-1-ethyl, cycloheptyl -2-ethyl, cyclooctyl-2-ethyl, cyclodecyl-2-ethyl, cyclodecyl-2-ethyl, cyclopropyl-1-propyl, cyclopropyl-2-propyl , cyclopropyl-3-propyl, cyclobutyl-1-propyl, cyclobutyl-2-propyl, cyclobutyl-3-propyl, cyclopentyl-1-propyl, cyclopentyl_ 2-propyl, cyclopentyl-3-propyl, cyclohexyl-1-propyl, cyclohexyl-2-propyl, cyclohexyl-3-propyl, cycloheptyl-1-propyl, phosphinyl -2-propyl, cycloheptyl-3-propyl, cyclooctyl-1-propyl, cyclooctyl-2-propyl, cyclooctyl-3-propyl, cyclodecyl-1-propyl , cyclodecyl-2-propyl, cyclodecyl-3-propyl, cyclodecyl-1-propyl, cyclodecyl-2-propyl, cyclodecyl-3-propyl, cyclopropyl- 1-butyl, cyclopropyl-2-butyl, cyclopropyl-3-butyl, cyclopropyl-4-butyl, cyclobutyl-1-butyl, cyclobutyl-2-butyl, ring Butyl-3-butyl, cyclobutyl-4-butyl, cyclopentyl-1_butyl, cyclopentyl-2-butyl, cyclopentyl-3-butyl, cyclopentyl-4-butyl Base, % hexyl-1-butyl, decyl-2-butyl, cyclohexyl-3-butyl, cyclohexyl-4-cyclobutyl, cycloheptyl-1-butyl, cycloheptyl-2-butyl Base, cycloheptyl_3_butyl, cycloheptyl-4-butyl, cyclooctyl-1-butyl, cyclooctyl-2-butyl, cyclooctyl-3-butyl, cyclooctyl -4-butyl, cyclodecyl-1-butyl, cyclodecyl-2-butyl, cyclodecyl-3-butyl, cyclodecyl-4-butyl, cyclodecylbutyl, cyclodecyl -2-butyl, cyclodecyl-3-butyl, cyclodecyl-4-butyl and the like 0. Cycloalkyl-Ci-C2 alkyl: Ci-C as described above One of the hydrogen atoms is replaced by a CrC6 halocycloalkyl group. An example is 丨_ 氯琴149027.doc •19· 201103430 propylmethyl, ι·cyclocyclobutylmethyl, chlorocyclopentylmethyl' chlorocyclohexylmethyl, 1 decyclopropylethyl, i 'Air ring butyl small ethyl, Buqi cyclodecyl small ethyl, 1-cyclohexyl small ethyl, i• gas cyclopropyl 2 · ethyl, k gas cyclobutyl ethyl, i' Chlorocyclopentylethyl, cyclohexanecyclohexylethyl, chlorocyclopropylmethyl, 2-cyclopentylmethyl, 2-chlorocyclopentylmethyl, 2-cyclohexylmethyl, 2-v ring Propyl + ethyl, 2' chlorocyclobutyl ethyl, 2-cyclopentyl-ethyl, 2-chlorocyclohexyl + ethyl, cyclohexane propyl 2-ethyl, 2-cyclohexane -2 - ethyl, 2 - gas cyclopentyl 2 - ethyl, 2 - cyclohexyl-2-ethyl, flufen cyclopropyl decyl, "fluorocyclobutyl methyl, fluorocyclopentylmethyl , fluorocyclohexylmethyl, κ fluorocyclopropyl]-ethyl, benzocyclobutyl-rethyl, phenoxycyclopentylethyl, b-cyclohexyl-ethyl, 1-fluorocyclopropyl -2-ethyl, 1-fluorocyclobutyl 2-ethyl, hydrazine-fluorocyclopentyl-2-ethyl, fluorocyclohexyl 2-ethyl, 2-fluorocyclopropyl fluorenyl, fluorine Cyclobutyl , 2-fluorocyclopentylmethyl, 2-fluorocyclohexylmethyl, 2-fluorocyclopropyl-1-ethyl, 2-fluorocyclobutyl-1-ethyl, 2-fluorocyclopentyl-丨· Ethyl, 2-fluorocyclohexyl-1-ethyl, 2-fluorocyclopropyl-2-ethyl, 2-fluorocyclobutyl-2-ethyl, pentyl-2-ethyl, 2- Cyclohexyl-2-ethyl and the like. Cs-C丨〇halocyclohexyl 1 _c丨-C4 alkyl is a CrC4 alkyl residue as described above, wherein one hydrogen atom is (: 3-( : 10 halocycloalkyl substitution. Alkoxy: an alkyl group attached via an oxygen. C^-C: 2 alkoxy is methoxy or ethoxy. C1-C3 alkoxy is additionally (for example) n-propyl Oxy or 1-mercaptoethoxy (isopropoxy). Ci-C: 4 alkoxy is additionally, for example, butoxy, 丨-methylpropoxy (second butoxy), 2 -methylpropoxy (isobutoxy) or 151-didecylethoxy (t-butoxy). C^-C: 6 alkoxy is additionally (for example) pentoxide

[SI 149027.doc -20- 201103430 基1-甲基丁氧基、2-甲基丁氧基、3_曱基丁氧基、u[SI 149027.doc -20- 201103430 base 1-methylbutoxy, 2-methylbutoxy, 3-mercaptobutoxy, u

二甲基丙氧基、U·二曱基丙氧基、2,2_二甲基丙氧基、L 乙基丙氧基、己氧基、丨_甲基戊氧基、2_甲基戊氧基、3· 曱基戊氧基、4_甲基戊氧基、1,1-二f基丁氧基、1,2-二甲 基丁氧基、1,3-二甲基丁氧基、2,2_二甲基丁氧基、2,3-二 曱基丁氧基、3,3-二曱基丁氧基、卜乙基丁氧基、2_乙基 丁氧基、1,1,2-三曱基丙氧基、丨,2,2•三曱基丙氧基、丨_乙 基-1-甲基丙氧基或卜乙基_2_甲基丙氧基。C1_C8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。Ci-C1Q烷氧基另外為(例如)壬氧基、癸氧基及其位置 ”構體C2-C1G烧氧基類似於炫氧基,但甲氧基除 外。 、 i烷氧基:如上所述之烷氧基,其經氟、氣、溴及/或 碘,較佳經氟部分或完全取代。Ci_C2鹵烷氧基為例如, 〇CH2F、0CHF2、〇CF3、0CH2a、〇CHCl2、〇ccl3、氣氟 曱氧基、二氣氟曱氧基、氯二氟甲氧基、2-氟乙氧基、2_ 氯乙氧基、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、2,2-二氯-2-氟乙氧基、2,2,2_三氣乙氡基或〇C2F5。 q-c:4鹵烷氧基另外為例如,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、%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、3,3,3-二氯丙氧基、〇ch2-C2F5、〇CF2-C2F5、 l-(CH2F)-2-敗乙氡基、卜仰仰冬氣乙氧基、卜仰刺· 149027.doc •21 - 201103430 2-溴乙氧基、4-氟丁氧基、4_氯丁氧基、4_溴丁氧基或九 氣丁氧基》烧氧基另外為例如,5_氟戊氧基、5_氣 戊氧基、5-漠戍氧基、5_蛾戊氧基、十一氣戊氧基、6-氣 己氧基、6-氯己氧基、6_溴己氧基、6碘己氧基或十二氟 己氧基。 稀氧基:經由氧原子連接的如上所述之稀基,例如, C2_ClG烯氧基,諸如丨-乙烯氧基、1-丙烯氧基、2-丙烯氧 基、1 -甲基乙烤氧基、1 · 丁说条且 丁烯氧基、2-丁烯氧基、3-丁烯 氧基、!-甲基-i-丙埽氧基、2_甲基小丙稀氧基、i•甲基_ 2-丙稀氧基、2•甲基_2_丙烯氧基叫姻氧基、2_戍稀氧 基、%戊婦氧基、4_戊稀氧基、卜甲基小丁烯氧基、Η 丁烯氧基、3·甲基小了烯氧基、"基_2_丁烤氧 基二-甲基-2-丁稀氧基、3·甲基_2_ 丁稀氧基、甲基 丁稀氧基、2 -曱基-3· 丁、膝g μ 、 田I。 / 丁歸氧基、3_甲基·3· 丁稀基、U-二 丙烯氧基' i-乙基-1_丙烯氧基 ,甲土 _2_ 稀氧基、、己稀氧基、己;氧^ 基、1_己 g, « , 烯氧基、4-己烯氧基、5-己烯 氧基' 1-曱基-1-戊烯氧基、2 ! Λ ^ ^ T基·1-戍烯氧基、3-曱基_ -戍婦氧基、4-曱基小戊稀氧基、卜甲 甲基-2-戊稀氧基、3_甲基- 土 ^ 基…基-戊稀氧基、曱基I戊稀氧 戊烯氧基、4_甲基-3-戊烯氧基、' 基3曱基·3_ “戊稀氧基、”基=歸氧峨基、I曱 基、&二曱…稀氧基、I:基甲:基I戊烯氧 丄,1·一甲基-3-丁烯氧基、 149027.doc -22- 201103430 1 ’2 - — f 基丁嫌 甲A-3-丁描备甘 子基_2~ 丁婦氧基、二 土_ 土、1,3-二甲基-1-丁烯氧基、1 3-二甲 Λ ) 丁稀氧基、i,3-二甲基-3-丁烯氧基' 2,2m丁;V 基、2,3-二,基_丨_稀 烯氧 二甲基…二 '基I 丁婦氧基、 甲其? ^基、3,3·二甲基]-丁婦氧基、3,3- Γ;::氧基、1_ 一稀氧基、“乙基〜 土 -乙基-3-丁烯氧基、2_乙基丁烯氧基、2 丁稀氧基、2-乙基_3_ 丁烯氧基、u,2_ —甲基-2·丙烯氧 : '卜乙基-1-甲基_2_丙稀氧基、i-乙基_2_甲基+丙歸氧 基及1-乙基-2-甲基_2_丙烯氧基及其類似物; _氧基:如上所述之稀氧基,其經氟、氯、演及 峨’較佳經氟部分或完全取代。 2 炔氧基:經由氧原子連接的如上所述之炔基,例如, C2-C1()炔氡基,諸如2_丙炔氧基、2_丁炔氧基、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、1-曱基-2-丁炔氧基、1_曱基_3_丁炔氧基、2甲 基-3-丁炔氧基、i-乙基_2•丙炔氧基、2_己炔氧基' 夂己炔 氧基、4-己炔氧基、5_己炔氧基、丨_曱基_2_戊炔氧基、i 曱基-3-戊炔氧基及其類似物; _炔氧基·_如上所述之炔氧基,其經氟、氣、漠及/戍 碘’較佳經氟部分或完全取代。 環娱•氧基:經由氧原子連接的如上所述之環烧基,例 如’ C3-C1Q環烧氧基或CyC8環烧氧基,諸如環丙氧基、環 戊氧基、環己氧基、環庚氧基、環辛氡基、環壬氧基、環 U9027.doc • 23· 201103430 癸氧基及其類似物; 齒環烧氧基:如上所述之環烧氧基,其經敗、氯、填及/ 或峨’較佳經氟部分或完全取代。 環烯氧基:經由氧原子連接的如上所述之環稀基,例 如,C3-C1G環烯氧基,cvc:8環烯氧基或較佳,環烯 氧基,諸如環戊-1-烯氧基、環戊_2_烯氧基、環己 基及環己-2-烯氧基; 烧氧基烧基:具有1至10個、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烷基,其中一個氫 原子經具有1至8個、1至6個、1至4個或丨至3個碳原子之烷 氧基置換,例如,甲氧基甲基、2_甲氧基乙基、乙氧基^ 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10個、1至8個、i至6個或i至4 個,尤其1至3個碳原子之如上所定義之烷氧基,其中—個 虱原子經具有1至8個、1至6個或尤其1至4個碳原子之烧氧 基置換’例如,2-曱氧基乙氧基、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。 烧基幾基:式R-CO-之基團,其中r為如上所定義之燒 基’例如’ CVCio烧基、(:丨-(:8烧基、烧基、cvc^ 基、CrC2院基或C3_C:4烧基。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、異丙基幾 基、正丁基羰基、第二丁基羰基、異丁基羰基及第三丁基 羰基。 鹵烧基幾基:式R-CO-之基團,其中r為如上所定義之 149027.doc -24- 201103430 _烷基,例如,Cl-C10鹵烷基、Ci_c8_烷基、Ci_c6_烷 基、C^-C4鹵烷基、c,-C2鹵烷基或C3_C4鹵烷基。實例為二 氟甲基叛基、三I甲基幾基、2,2_二氟乙基徵基、2,2,3•三 氟乙基羰基及其類似物。 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_C8烷氧基、Ci_C6烷氧 基、q-C4烷氧基4Cl_C2烷氧基。C「C4烷氧羰基之實例為 曱氧羰基、乙氧羰基、丙氧羰基、異丙氧羰基、正丁氧羰 基、第二丁氧羰基、異丁氧羰基及第三丁氧羰基。 鹵烷氧羰基:式R-CO-之基團,其中尺為如上所定義之 i烧氧基’例如’ Ci-Cw鹵烷氧基、Cl_c8鹵烷氧基、Cl_ C6_烧氧基、Cl_c4鹵烷氧基或Ci_c2鹵烷氧基。Ci_c4鹵烷 氧羰基之實例為二氟甲氧羰基、三氟曱氧羰基、2,2_二氟 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 義之烧基,例如,C丨-C1()烷基、Ci-Cs烷基、C〗-C6烷基、 C!-C4炫基、c丨-C2烷基或C3-C4烷基。C】-C4烷基胺基羰基 之實例為曱基胺基羰基、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。 二院基胺基羰基: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、(^-(^烷 基、CrCs烷基、CVC4烷基、CrG烷基或C3-C4烷基。二-(C^C4院基)_胺基羰基之實例為二甲基胺基羰基、二乙基 149027.doc -25- 201103430 胺基Μ基、二丙基胺基幾基、二異丙基胺基艘基及二丁基 胺基羰基。 胺基烧基.式R-NH2之基團’其中R為如上所定義之院 基,例如烧基、C〗-C8烧基、Ci-C6烧基、Ci-C4院 基、Ci-C2烷基或(:3_(:4烧基。實例為胺基曱基、丨_及2_胺 基乙基、1-、2-及3-胺基丙基、1-及2-胺基1-甲基乙基、卜 、2-、3-及4-胺基丁基及其類似物。 烧基續酿基.式R-S(O)2·之基團,其中r為如上所定義 之烷基,例如,CVCiq烷基、C丨-C8烷基、(:丨-(:6烷基、CV C4烷基或C】-C2烷基。C^-C4烷基磺醯基之實例為甲確醯 基、乙%酿基、丙項酿基 '異丙確醢基、正丁確醯基、第 二丁磺醯基、異丁磺醯基及第三丁磺醯基。 烧硫基:經由硫原子連接的如上所定義之烧基。 鹵烧硫基:經由硫原子連接的如上所定義之齒烧基。 稀硫基:經由硫原子連接的如上所定義之烯基。 鹵烯硫基:經由硫原子連接的如上所定義之鹵烯基。 块硫基:經由硫原子連接的如上所定義之炔基。 鹵炔硫基:經由硫原子連接的如上所定義之_炔基。 環炫硫基: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、蒽基、菲基、苐基及奠基。 芳基較佳為苯基或萘基,且尤其為笨基。 苯基-CrC4烷基:CrC4烷基(如上所定義),其中一個氫 原子經苯基置換’諸如苄基、笨乙基及其類似物。 149027.doc -26- 201103430 苯基-Crq烷氧基 個氫原子經苯基置換 物0 * C!-C4烧氧基(如上所定義),其中一 ,諸如苄氧基、笨乙基氧基及其類似 3_、4-、5_、6_赤7 〇 次7-貝飽和、部分不飽和或最大不飽和 碳環基團:環丙基、環 衣』卷' %戊基、環己基、環庚基、 環丙烯基、環丁烯基 -E _ ,., w 一 ^ %戍烯基、5衣己烯基、環庚烯基、 環丁二稀基、環戊二烯基、環己二稀基、環庚二烯基或環 庚三烯基。苯基在形式上亦包括在此定義中,而其亦包涵 在術語芳基(此處未列舉)中。 6或7-員飽和、部分不飽和或最大不飽和 雜環’其含有卜2或3個選自氧、氮(以_舰形式)及硫 (以S、SO或S〇2形式)之雜原子或含有雜原子的基團及視情 況可選的1或2個選自C(=〇)&c(=s)之基團作為環成員: _ %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1 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2-氮丙σ定基、1-、2-或3-氮雜環丁基, -5_或6-員飽和或部分木飽和雜環(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) 149027.doc -27- 201103430 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)2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個氧或硫原子成 一或兩個氧及/或硫原子及視情況可選的1或2個選自 C(=0)及C(=S)之基團,舉例而言,2-四氫呋喃基、3-四氧。夫°南基、3-四氫咬喃-2-酮基、4-四氫咳喃_2- ®同 基、5-四氫吱喃-2-酮基、2-四氫吱喃-3-酮基、4-四氫 咬喃-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_四氫噻吩網 基、5-四氫噻吩-2-酮基、2-四氫噻吩-3-酮基、4-四氫 。塞吩-3-酮基、5-四氫噻吩-3-酮基、2-吡洛咬基、3-11比 略啶基、1-吡咯啶-2-酮基、3-吡咯啶-2-酮基、4-吡咯 α定-2-酮基、5-°比嘻。定-2-酮基、1-°比°各咬-3-酮基、2-0比 51 各啶-3-酮基、4-吡咯啶-3-酮基、5-吡咯啶-3-酮基、卜 咯啶_2,5-二酮基、3-吡咯啶-2,5-二酮基、3-異嗞嗤 啶基、4-異噁唑啶基、5-異噁唑啶基、3-異噻唑啶基、 4-異°塞。坐。定基、5-異嘆唾咬基、3-他σ坐α定基、4-。比咬咬 基、5-吡唑啶基、2-噁唑啶基、4-噁唑啶基、5-噁嗤啶 基、2-噻唑咬基、4-噻唑啶基、5-噻唑啶基、2-咪咬啶 基' 4-咪唑咬基、1,2,4-°惡二。坐咬-3-基、1,2,4-°惡 啶-5-基、1,2,4-噻二唑啶-3-基、1,2,4-噻二唑啶-5- 基、丨,2,4-三唑啶-3-基、1,3,4-噁二唑啶-2-基、1,3,4-。塞二。坐°定-2-基、1,3,4-三嗤咬-2-基、2,3-二氫〇夫喊-2- -2S- 149027.doc 201103430 基、2,3 -二氮α夫喃-3 -基、2,4 -二氫咬°南-2 -基、2,4 -二氮 呋喃-3-基、2,3-二氫噻吩-2-基、2,3-二氫噻吩-3-基、 2.4- .—鼠α塞吩-2 -基、2,4 -二鼠α塞吩-3 -基、2 - °比0各σ林-2 -基、2 - Dtb鳴· ^木-3 -基、3 - °比洛嚇 - 2 -基、3 - °比鸣咐 - 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-異嗟。坐琳_ 5 -基、2,3 -二氫°比唾-1 -基、2,3 -二氫。比α坐-2 -基、2,3-二氫吡唑-3-基、2,3-二氫吡唑-4-基、2,3-二氫 。比。坐-5 -基、3,4 -二氫。比。坐-1 -基、3,4 -二氫°比。坐-3 -基、 3.4- 二氫°比。坐-4-基、3,4-二氫。比。坐-5-基、4,5-二氫0比 0坐-1-基、4,5-二氫°比。坐-3-基、4,5-二氫°比。坐-4-基、 4.5- 二氫。比。坐-5-基、2,3-二氫噁。坐-2-基、2,3-二氫。惡 唑-3-基、2,3-二氫噁唑-4-基、2,3-二氫噁唑-5-基、 3,4-二氫噁唑-2-基、3,4-二氫噁唑-3-基、3,4-二氫噁 。坐-4-基、3,4-二氫°惡唾-5-基、3,4-二氫°惡。坐-2-基、 3,4 -二氫°惡。坐-3-基、3,4 -二氫。惡。坐-4-基、2 -旅。定基、3-旅°定基、底σ定基、1,3-二。惡炫!-5 -基、2 -四氮°底喃 基、4-四氫旅喃基、2-四氫°塞吩基、3 -六氫噠嗪基、4-六氫噠嗓基、2-六氫。密咬基、4-六氫。密σ定基、5 -六氫°密 0定基、2 -旅°秦基、1,3,5 -六氣二°秦-2-基及1,2,4 -六氮三 149027.doc -29- 201103430 嗪-3-基以及相應的_亞基; ΙΓ成,Γ:來自由氧、氮及硫組成之群的雜原子作 的7Λ飽和或部分不飽和雜環:例如,具有7 人 衣丨示蚊j衣成貝之外,其亦 ^ 固氮原子及/或—個氧或硫原子或—或兩個氧 =硫原子,舉例南言’四氯氮呼基及六氣氣呼基, 诸如2,3,4,5-四氫[1H]氮呼小、_2_ ^ ' '4~ ' -5- ' -6- -4 ' -6-3·、-4-、-5- 2- 、 -3- 、 -4- 3- 或-4-基; 或-7-基、3,4,5,6-四氫[2印氮呼_2_、_3_ 或_7_基、2,3,4,7-四氫[1H]氮呼_丨、-2_ 、-6-或-7-基、2,3,6,7·四氫[1H]氮呼小 -5-、-6-或-7-基、六氫氮呼_卜、 -SK. , 四氫氧呼基及六氫氧呼基,諸 氧呼基及相應的-亞基Dimethylpropoxy, U·dimercaptopropoxy, 2,2-dimethylpropoxy, L ethylpropoxy, hexyloxy, 丨-methylpentyloxy, 2-methyl Pentyloxy, 3·decylpentyloxy, 4-methylpentyloxy, 1,1-di-f-butoxy, 1,2-dimethylbutoxy, 1,3-dimethylbutyl Oxy, 2,2-dimethylbutoxy, 2,3-didecylbutoxy, 3,3-dimercaptobutoxy, bethylbutoxy, 2-ethylbutoxy, 1 1,2-trimercaptopropoxy, hydrazine, 2,2•tridecylpropoxy, hydrazine-ethyl-1-methylpropoxy or phenylethyl-2-methylpropoxy. The C1_C8 alkoxy group is, for example, a heptyloxy group, an octyloxy group, a 2-ethylhexyloxy group, and a positional isomer thereof. The Ci-C1Q alkoxy group is additionally, for example, a decyloxy group, a decyloxy group and a position thereof. The structure C2-C1G alkoxy group is similar to a methoxy group, except for a methoxy group. The alkoxy group, which is preferably partially or completely substituted by fluorine, fluorine, gas, bromine and/or iodine. Ci_C2 haloalkoxy is, for example, 〇CH2F, 0CHF2, 〇CF3, 0CH2a, 〇CHCl2, 〇ccl3 , fluorofluoromethoxy, difluorofluoromethoxy, chlorodifluoromethoxy, 2-fluoroethoxy, 2-chloroethoxy, 2-bromoethoxy, 2-iodoethoxy, 2, 2_Difluoroethoxy, 2.2.2-trifluoroethoxy, 2_gas_2•fluoroethoxy, 2•gas_2,2-difluoroethoxy, 2,2-dichloro- 2-fluoroethoxy, 2,2,2-trioxalyl or hydrazine C2F5. qc: 4-haloalkoxy is additionally, for example, 2-fluoropropoxy, 3-fluoropropoxy, 2.2- Fluoropropoxy, 2,3-difluoropropoxy, 2-propyloxy, %-propoxy, 2,3-dipropoxy, 2-bromopropoxy, 3-bromopropoxy Base, 3,3,3_trifluoropropoxy, 3,3,3-dichloropropoxy, 〇ch2-C2F5, 〇CF2-C2F5, l-(CH2F)-2-f-ethylidene, Winter ethoxy, Bu Yang thorn · 149027.doc 21 - 201103430 2-Bromoethoxy, 4-fluorobutoxy, 4-chlorobutoxy, 4-bromobutoxy or nona-butoxy" alkoxy is additionally, for example, 5-fluoropentyloxy 5_ gas pentyloxy, 5-indolyloxy, 5-mothyloxy, undecylpentyloxy, 6-cyclohexyloxy, 6-chlorohexyloxy, 6-bromohexyloxy, 6 iodohexyloxy or dodecafluorohexyloxy. Dilute oxy: a dilute group as described above attached via an oxygen atom, for example, a C 2 —Cl G alkenyloxy group such as an anthracene-vinyloxy group, a 1-propenyloxy group, 2 - propyleneoxy, 1-methylethyloxyoxy, 1 · butyl and butenyloxy, 2-butenyloxy, 3-butenyloxy, !-methyl-i-propenyloxy , 2_Methyl propyleneoxy, i•methyl _ 2-propoxyoxy, 2·methyl 2 _ _ _ oxyoxy, 2 戍 diloxy, % pentyloxy , 4_pentamethoxy, benzyloxybutenyloxy, decenyloxy, 3·methyl oligoyloxy, "yl-2-butanoxyoxydi-methyl-2-butene Oxy, 3·methyl 2_butenyloxy, methylbutoxyoxy, 2-indolyl-3·butyl, knee g μ, Tian I. / Dic acid, 3_methyl·3· Butyl, U-dipropylene 'i-Ethyl-1_propenyloxy, metasoil_2_ diloxy, hexyloxy, hexyl; oxy group, 1_hexg, «, alkenyloxy, 4-hexenyloxy , 5-hexenyloxy ' 1-indenyl-1-pentenyloxy, 2 ! Λ ^ ^ T-yl 1-nonenyloxy, 3-indenyl--indenyloxy, 4-indenyl Small pentyloxy, b-methyl-2-pentenyloxy, 3-methyl-organic-yl-yl-pentenyloxy, fluorenyl-1 pentyloxypentenyloxy, 4-methyl-3- Penteneoxy, 'yl 3 decyl · 3 _ pentyleneoxy, yl = oxoindolyl, iminyl, & diterpene... diloxy, I: yl: pentene oxime ,1·monomethyl-3-butenyloxy, 149027.doc -22- 201103430 1 '2 - — f butyl succinyl A-3-butyl glucomannyl_2~butoxy, two soil _ soil, 1,3-dimethyl-1-butenyloxy, 1,3-dimethylhydrazine) butyloxy, i,3-dimethyl-3-butenyloxy 2,2 m butyl; V group, 2,3-di, _ _ _ _ _ olefin oxy dimethyl ... bis ' yl butyl ethoxy group, A? ^, 3,3. dimethyl]-butanyloxy, 3,3-indole;::oxy, -1-dioxy, "ethyl~ s-ethyl-3-butenyloxy, 2_ethylbutenyloxy, 2butyloxy, 2-ethyl-3-ylbutenyloxy, u,2_methyl-2-propenyloxy: 'Buethyl-1-methyl-2-propene Oxyl, i-ethyl 2 -methyl + apropyloxy and 1-ethyl-2-methyl-2-propenyloxy and the like; _oxy: a diloxy group as described above, It is preferably partially or completely substituted by fluorine, chlorine, and hydrazine. 2 alkynyloxy: an alkynyl group as described above attached via an oxygen atom, for example, a C2-C1()alkynyl group, such as 2_ Propynyloxy, 2-butynyloxy, butynyloxy, 1-methyl-2-propynyloxy, 2-pentynyloxy, 3-pentynyloxy, 4-pentynyloxy, 1-mercapto-2-butynyloxy, 1-hydrazino-3-butynyloxy, 2-methyl-3-butynyloxy, i-ethyl-2-propynyloxy, 2_hexyl Alkynyloxy-p-hexynyloxy, 4-hexynyloxy, 5-hexynyloxy, fluorenyl-hydrazino-2-pentynyloxy, i-decyl-3-pentynyloxy and the like ; alkynyloxy- _ alkynyloxy group as described above, which is preferably fluorine-containing, fluorine, gas, and hydrazine iodine Partially or completely substituted. Cyclophilic oxy group: a cycloalkyl group as described above attached via an oxygen atom, such as 'C3-C1Q cycloalkoxy or CyC8 cycloalkoxy, such as cyclopropoxy, cyclopentyloxy , cyclohexyloxy, cycloheptyloxy, cyclooctyl, cyclodecyloxy, ring U9027.doc • 23· 201103430 decyloxy and its analogues; dentate alkoxy: cycloalkoxy as described above, Its chloroform, chlorine, and/or hydrazine is preferably partially or completely substituted by fluorine. Cycloalkenyloxy: a cycloaliphatic group as described above attached via an oxygen atom, for example, a C3-C1G cycloalkenyloxy group, cvc : 8 cycloalkenyloxy or preferably, cycloalkenyloxy, such as cyclopent-1-enyloxy, cyclopent-2-enyloxy, cyclohexyl and cyclohex-2-enyloxy; Base: an alkyl group as defined above having from 1 to 10, from 1, to 6 or from 1 to 4, especially from 1 to 3, carbon atoms, wherein one hydrogen atom has from 1 to 8, from 1 to 6 Substituted by alkoxy groups of 1 to 4 or up to 3 carbon atoms, for example, methoxymethyl, 2-methoxyethyl, ethoxyoxy, 3-methoxypropyl, 3- Ethoxypropyl and its analogues. Alkoxy group: an alkoxy group as defined above having 1 to 10, 1 to 8, i to 6 or i to 4, especially 1 to 3, carbon atoms, wherein Replacement of alkoxy groups up to 8, 1 to 6 or especially 1 to 4 carbon atoms 'e.g. 2-methoxyethoxy, 2-ethoxyethoxy, 3, methoxypropoxy , 3-ethoxypropoxy and the like. A radical: a group of the formula R-CO-, wherein r is an alkyl group as defined above, for example, 'CVCio alkyl, (:丨-(: 8 burnt base, burnt base, cvc^ base, CrC2 yard base or C3_C: 4 burn base. Examples are ethyl acetyl, propyl thiol and the like. Examples of the CrC4 alkylcarbonyl group are a propylcarbonyl group, an isopropyl group, a n-butylcarbonyl group, a second butylcarbonyl group, an isobutylcarbonyl group and a tert-butylcarbonyl group. a group of the formula R-CO- wherein r is 149027.doc -24-201103430 _alkyl as defined above, for example, Cl-C10 haloalkyl, Ci_c8-alkyl, Ci_c6-alkane a group, C^-C4 haloalkyl, c, -C2 haloalkyl or C3_C4 haloalkyl. Examples are difluoromethyl-rebel, tri-l-methyl-methyl, 2,2-difluoroethyl ketone, 2,2,3•trifluoroethylcarbonyl and the like. Alkoxycarbonyl: a group of the formula R-CO-, wherein R is alkoxy as defined above, for example, Cl_ClQ alkoxy, Ci_C8 alkoxy, Ci_C6 alkoxy, q-C4 alkoxy 4Cl_C2 alkoxy base. Examples of the C "C4 alkoxycarbonyl group are an anthraceneoxycarbonyl group, an ethoxycarbonyl group, a propoxycarbonyl group, an isopropoxycarbonyl group, a n-butoxycarbonyl group, a second butoxycarbonyl group, an isobutoxycarbonyl group and a third butoxycarbonyl group. Oxycarbonyl: a group of the formula R-CO-, wherein the rudent is i alkoxy as defined above 'eg 'Ci-Cw haloalkoxy, Cl_c8 haloalkoxy, Cl_C6_alkoxy, Cl_c4 haloal Oxyl or Ci_c2 haloalkoxy. Examples of Ci_c4 haloalkyloxycarbonyl are difluoromethoxycarbonyl, trifluoromethoxycarbonyl, 2,2-difluoroethoxycarbonyl, 2,2,3-trifluoroethoxycarbonyl And an analogue thereof. Alkylaminocarbonyl: a group of the formula R-NH-CO-, wherein R is an alkyl group as defined above, for example, C丨-C1()alkyl, Ci-Cs alkyl, C - C6 alkyl, C!-C4 leumino, c丨-C2 alkyl or C3-C4 alkyl. C] -C4 alkylaminocarbonyl examples are mercaptoaminocarbonyl, ethylaminocarbonyl, A propylaminocarbonyl group, an isopropylaminocarbonyl group, a butylaminocarbonyl group, a second butylaminocarbonyl group, an isobutylaminocarbonyl group, and a tert-butylaminocarbonyl group. Rr, a group of N-CO-, wherein R and R are independently of each other An alkyl group as defined above, for example, Ci_Ciq alkyl, (^-(^ alkyl, CrCs alkyl, CVC4 alkyl, CrG alkyl or C3-C4 alkyl. Di-(C^C4))-amine Examples of carbonyl groups are dimethylaminocarbonyl, diethyl 149027.doc -25-201103430 aminoguanidino, dipropylamino group, diisopropylamino group and dibutylaminocarbonyl Alkyl group. A group of the formula R-NH2 wherein R is a group as defined above, for example, alkyl, C-C8 alkyl, Ci-C6 alkyl, Ci-C4, Ci-C2 Alkyl or (: 3_(: 4 alkyl). Examples are amino fluorenyl, hydrazine _ and 2-aminoethyl, 1-, 2- and 3-aminopropyl, 1- and 2-amino 1 -methylethyl, br, 2-, 3- and 4-aminobutyl and the like. A group of the formula RS(O)2, wherein r is an alkane as defined above a group, for example, CVCiq alkyl, C丨-C8 alkyl, (: 丨-(:6 alkyl, CV C4 alkyl or C)-C2 alkyl. An example of a C^-C4 alkylsulfonyl group is A It is confirmed that the base of the base, the base of the B, the base of the C, and the base of the C-based base are 'isopropylidene sulfhydryl group, n-butyl sulfhydryl group, the second butyl sulfonyl group, the isobutyl sulfonyl group and the third butyl sulfonyl group. through An alkyl group as defined above which is bonded by a sulfur atom. A halogen group: a dentate group as defined above which is bonded via a sulfur atom. A dilute sulfur group: an alkenyl group as defined above which is bonded via a sulfur atom. a haloalkenyl group as defined above, which is bonded via a sulfur atom. A thiol group: an alkynyl group as defined above which is bonded via a sulfur atom. Alkynylthio group: an alkynyl group as defined above which is bonded via a sulfur atom. Thio group: a cycloalkyl group as defined above attached via a sulfur atom. The aryl group is a carbocyclic aromatic monocyclic or polycyclic ring having 6 to 16 carbon atoms as a ring member. Examples are phenyl, naphthyl, anthracenyl, phenanthryl, anthracenyl and foundry. The aryl group is preferably a phenyl or naphthyl group, and is especially a stupid group. Phenyl-CrC4 alkyl: CrC4 alkyl (as defined above) wherein one hydrogen atom is replaced by a phenyl group such as benzyl, phenethyl and the like. 149027.doc -26- 201103430 Phenyl-Crq alkoxy hydrogen atom via phenyl replacement 0 * C!-C4 alkoxy (as defined above), one of which, such as benzyloxy, phenethyloxy And similar 3_, 4-, 5_, 6_erythro 7 贝 7-shell saturated, partially unsaturated or most unsaturated carbocyclic groups: cyclopropyl, ring-shaped volcano '% pentyl, cyclohexyl, ring Heptyl, cyclopropenyl, cyclobutenyl-E _ ,., w ^ 戍 戍 alkenyl, 5-hexenyl, cycloheptenyl, cyclobutadienyl, cyclopentadienyl, cyclohexyl Di-diyl, cycloheptadienyl or cycloheptatrienyl. Phenyl is also included in the definition in the form, and is also included in the term aryl (not listed here). 6 or 7-membered saturated, partially unsaturated or most unsaturated heterocyclic ring containing 2 or 3 selected from the group consisting of oxygen, nitrogen (in the form of ship) and sulfur (in the form of S, SO or S〇2) An atom or a group containing a hetero atom and, optionally, 1 or 2 groups selected from C(=〇)&c(=s) as ring members: _% or 4-member saturated or partially unsaturated a heterocyclic ring (hereinafter also referred to as a heterocyclic group) containing 1, 2 or 3 from oxygen, nitrogen (in the form of N*NR) and sulfur (in the form of S, SO or S〇2) a hetero atom of the group and, optionally, 1 or 2 groups selected from c(=0) and c(=S) as a ring member. For example, a monocyclic saturated or partially unsaturated heterocyclic carbon ring member In addition, it also contains 1 to 3 nitrogen atoms and / or 1 oxygen or sulfur atom or 1 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-thiapropyl, } or 2-aziridine, 1-, 2- or 3-azetidinyl, -5 a 6-membered saturated or partially wood-saturated heterocyclic ring (hereinafter also referred to as a heterocyclic group) containing 1, 2 or 3 derived from oxygen and nitrogen (in the form of N*NR) 149027.doc -27- 201103430 and heteroatoms of the group consisting of sulfur (in the form of s, so or s〇2) and optionally 1 or 2 selected from C(=0) and c(=s) a 2 group as a ring member: for example, a 'monocyclic saturated or partially unsaturated heterocyclic ring, which in addition to a carbocyclic ring member, also contains 1 to 3 nitrogen atoms and/or 1 oxygen or sulfur atom to form one or two oxygen atoms and / or a sulfur atom and optionally 1 or 2 groups selected from C (=0) and C (= S), for example, 2-tetrahydrofuranyl, 3-tetraoxy. °南基, 3-tetrahydro-butan-2-one, 4-tetrahydroc-butan-2-yl, 5-tetrahydrofuran-2-one, 2-tetrahydrofuran-3 a keto group, a 4-tetrahydroindan-3-one group, a 5-tetrahydrofuran-3-one group, a 2-tetrahydrothiophenyl group, a 3-tetrahydrothiophenyl group, a 3-tetrahydrothiophen-2-one group, 4_tetrahydrothiophene network, 5-tetrahydrothiophen-2-one, 2-tetrahydrothiophen-3-one, 4-tetrahydro. Desphen-3-one, 5-tetrahydrothiophen-3-one, 2-pylotyl, 3-11 bis-ridino, 1-pyrrolidin-2-one, 3-pyrrolidine-2 a keto group, a 4-pyrrole α-butan-2-one group, a 5-° ratio. Ding-2-keto group, 1-° ratio ° -3- keto group, 2-0 ratio 51 pyridine-3-one, 4-pyrrolidin-3-one, 5-pyrrolidin-3- Keto, bromidine-2,5-dione, 3-pyrrolidine-2,5-dione, 3-isoacridinyl, 4-isoxazolyl, 5-isoxazole Base, 3-isothiazolidinyl, 4-isoose. sit. Fixed base, 5-isolated sputum base, 3-he squat α-base, 4-. Specific bite, 5-pyrazolidinyl, 2-oxazolidinyl, 4-oxazolidinyl, 5-oxaridinyl, 2-thiazole, 4-thiazolidinyl, 5-thiazolidinyl , 2-imidyl pyridine ' 4-imidazole bite base, 1, 2, 4- ° dioxin. Sit-3-yl, 1,2,4-oxalin-5-yl, 1,2,4-thiadiazolidin-3-yl, 1,2,4-thiadiazolidine-5-yl , hydrazine, 2,4-triazolidine-3-yl, 1,3,4-oxadiazolidine-2-yl, 1,3,4-. Plug two.坐定定-2-基,1,3,4-三嗤 bit-2-yl, 2,3-dihydro〇fu shouting-2--2S-149027.doc 201103430 base, 2,3-dinitrogen α Furan-3-yl, 2,4-dihydrogenate, Nan-2-yl, 2,4-dinitrofuran-3-yl, 2,3-dihydrothiophen-2-yl, 2,3-di Hydrothiophen-3-yl, 2.4-.-rat α-cephen-2-yl, 2,4-di-r-α-e-phen-3-yl, 2 - ° ratio 0 σ lin-2 -yl, 2 - Dtb鸣·^木-3 -基,3 - °比洛,2- 2 -, 3 - °, 咐 - 3 -yl, 2-isoxazolin-3-yl, 3-isoxazoline-3 -yl, 4-isoxazolin-3-yl, 2-isoxazolin-4-yl, 3-isoxazolin-4-yl, 4-isoxazolin-4-yl, 2-iso Oxazolin-5-yl, 3-isoxazolin-5-yl, 4-isoxazolin-5-yl, 2-isothiazolin-3-yl, 3-isothiazolin-3-yl, 4-isothiazolin-3-yl, 2-isothiazolin-4-yl, 3-isothiazolin-4-yl, 4-isothiazolin-4-yl, 2-isothiazolin-5-yl, 3-isothiazolin-5-yl, 4-isoindole. Sitting _ 5 -yl, 2,3 - dihydrogen than saliva-1 -yl, 2,3-dihydrogen. 2 -yl, 2,3-dihydropyrazol-3-yl, 2,3-dihydropyrazol-4-yl, 2,3-dihydro. ratio. Take -5-based, 3,4-dihydrogen. ratio. Take the -1 - base, 3,4 - dihydrogen ratio. Take a 3-base, 3.4-dihydrogen ratio. Take 4-yl, 3,4-dihydrogen. ratio. Sit-5-yl, 4,5-dihydro 0 to 0-spin-1-yl, 4,5-dihydrogen ratio. Sitting on the -3- group, 4,5-dihydrogen ratio. Sit-4-yl, 4.5-dihydrogen. ratio. Sitting on a 5-based, 2,3-dihydrogen. Sitting 2-yl, 2,3-dihydrogen. Oxazol-3-yl, 2,3-dihydrooxazol-4-yl, 2,3-dihydrooxazol-5-yl, 3,4-dihydrooxazol-2-yl, 3,4- Dihydrooxazol-3-yl, 3,4-dihydrocarb. Sodium-4-yl, 3,4-dihydro-deso-5-yl, 3,4-dihydro. Sit-2-yl, 3,4-dihydrogen. Sit-3-yl, 3,4-dihydrogen. evil. Take 4-ki, 2 - brigade. Fixed base, 3-Brigade base, bottom σ base, 1,3-two.恶炫!-5-yl, 2 -tetrazine naphthyl, 4-tetrahydronaphthyl, 2-tetrahydro-septyl, 3-hexahydropyridazinyl, 4-hexahydroindenyl, 2-hexahydrogen. Density base, 4-hexahydrogen. Σσ定基,5 - hexahydro thiol 0 base, 2 - british Qin, 1,3,5 - hexahydro 2 - Qin-2-yl and 1,2,4 - hexanitrogen 149027.doc -29 - 201103430 azine-3-yl and the corresponding _ subunit; ΙΓ, Γ: 7Λ saturated or partially unsaturated heterocyclic ring derived from a hetero atom consisting of oxygen, nitrogen and sulfur: for example, having 7 people In addition to the shellfish, it also has a nitrogen-fixing atom and/or an oxygen or sulfur atom or—or two oxygen=sulfur atoms. For example, Nantou 'tetrachloro-nitrogen-based group and six-gas-based group, such as 2,3,4,5-tetrahydro[1H]azepine, _2_ ^ ' '4~ ' -5- ' -6- -4 ' -6-3·, -4-,-5- 2- , -3-, -4- 3- or -4-yl; or -7-yl, 3,4,5,6-tetrahydro [2-indole- 2, _3_ or _7-yl, 2, 3, 4,7-tetrahydro[1H]azepine, -2, -6- or -7-yl, 2,3,6,7-tetrahydro[1H]azepine-5-,-6- or -7-yl, hexahydroazepine-bu, -SK., tetrahydrooxoyl and hexahydrooxoyl, oxorehyl and corresponding-subunit

Aj,4,5-四氫[1H]氧呼_ 2-、-3-、一如-6|7_基、2,3,4,7_四氫_氧哩_ 2-、-3-、·4·、m7•基、2,3,6,7•四氫_氧呼_ 2-、小、-4-、-5-、_6-或-7-基,六氫氮呼小、_2_、 丨或I基;四-及六氫…3-二氮呼基、四及六氫-Μ· 一氮呼基、四-及六氫-1,3·噁氮呼基、四-及六氫],4_ 。惡氮呼基、四-及六氯Μ二氧呼基、四-及六氫-Μ_ 含有卜2或3個來自由氧、氮及硫組成之群的雜原子的 5-或6-貝芳族(=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⑷個氣原子 及!個硫或氧原子作為環成員的5•員雜芳基,諸如2“夫 喊基、3“夫喃基、2“塞吩基、3·嗔吩基、2“比略基、3· J49027.doc -30- 201103430 吡咯基、3-異噁唑基、4-異噁唑基、5_異噁唑基、3異 噻唑基、4-異噻唑基、5-異噻唑基、3_吡唑基、扣吡唑 基、5-吡唑基、2-噁唑基、4-噁唑基、5_噁唑基、2_噻 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、丨,2,4-噻二唑 _ 3-基、1,2,4-噻二唑-5-基、1,2,4-三唑_3_基、^,扣噁 二唑-2-基、l,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 基,諸如,。比π各_ 1 _基、β比唾_ 1 _基、味吐_ 1 _基、1 2 3 三唑-1-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》比咬基、〇比β定_3_美、 0比啶-4-基、3-噠唤基、4-違嗓基、2-嘧啶基、4-喷。定 基、5-嘧啶基、2-吡嗪基、1,3,5-三嗪-2-基及l,2,4-三 嘻-3 -基; 直鏈C2伸烷基:具有2個碳原子之二價未分支鏈,亦即 CH2CH2。 直鍵C2或〇3伸烧基:具有2或3個碳原子之二價未分支 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 鏈,亦即 CH2、CH2CH2、CH2CH2CH2、CH2CH2CH2CH2及 CH2CH2CH2CH2CH2。 C2-C5伸烷基: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。 149027.doc •31 · 201103430Aj,4,5-tetrahydro[1H]oxo_2-, -3-, mono--6|7-yl, 2,3,4,7-tetrahydro-oxo_2-,-3- , ·4·, m7•基, 2,3,6,7•tetrahydro-oxo_2-, small, -4-,-5-, _6- or -7-yl, hexahydro-nitrogen _2_, hydrazine or I group; tetra- and hexahydro-(3-diazine-based, tetra- and hexahydro-indole-nitrohavyl, tetra- and hexahydro-1,3-oxazolyl, tetra- and Hexahydro], 4_. Oxazepine, tetra- and hexachloropurine dioxohyl, tetra- and hexahydro-indole_ 5- or 6-carbene containing 2 or 3 heteroatoms from a group consisting of oxygen, nitrogen and sulfur Family (=maximum unsaturated) heterocyclic ring (=heteroaromatic group), for example 'connected via carbon and contains (1) nitrogen atom or (4) gas atom and! a sulphur or oxygen atom as a ring member of a 5-membered heteroaryl group, such as 2 "fussing base, 3" phoranyl, 2" thiophene, 3 thiophene, 2" bicinch, 3 · J49027 .doc -30- 201103430 Pyrrolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, 3-isothiazolyl, 4-isothiazolyl, 5-isothiazolyl, 3-pyridyl Azyl, pyrazolyl, 5-pyrazolyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 2-imidazole , 4-imidazolyl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazole-5-yl, anthracene, 2,4-thiadiazole-3-yl, 1 , 2,4-thiadiazol-5-yl, 1,2,4-triazole-3-yl, ^, oxadiazole-2-yl, 1,3,4-thiadiazol-2-yl And a 1,3,4-triazole-2-yl group; a 5-membered heteroaryl group which is bonded via a nitrogen and has 1 to 3 nitrogen atoms as a ring member, such as. Ratio π _ 1 _ base, β ratio sal _ 1 _ base, taste _ 1 _ base, 1 2 3 triazol-1-yl and 1,2,4-triazol-1-yl; contains 1, 2 Or a 6-membered heteroaryl group having 3 nitrogen atoms as a ring member, such as "biter base, 〇 ratio β _3_美, 0 pyridine-4-yl, 3- 哒, 4- 嗓 嗓, 2-pyrimidinyl, 4-spray. Stationary, 5-pyrimidinyl, 2-pyrazinyl, 1,3,5-triazin-2-yl and 1,2,4-triazin-3-yl; linear C2 alkyl: 2 carbons The divalent unbranched chain of atoms, also known as CH2CH2. The direct bond C2 or 〇3 is a divalent unbranched chain having 2 or 3 carbon atoms, that is, CH2CH2 and CH2CH2CH2. Linear CrC5 alkylene: a divalent unbranched chain having from 1 to 5 carbon atoms, i.e., CH2, CH2CH2, CH2CH2CH2, CH2CH2CH2CH2, and CH2CH2CH2CH2CH2. C2-C5 alkylene: a divalent or preferably unbranched chain having 2 to 5 carbon atoms, such as CH2CH2, -CH(CH3)-, CH2CH2CH2, CH(CH3)CH2, CH2CH(CH3), CH2CH2CH2CH2 CH2CH2CH2CH2CH2. 149027.doc •31 · 201103430

CcC5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銨陽離子。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 〇 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Ar、Het、A、γ、r1、r2、r3、尺4、尺5、 R6、R6a、R7、R8、R9、R丨。、R,丨、Rl2、Rl3、Rl4、r15、 r16、m、Rd、M、Q及指數,且關於 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。 若Ar為如上所定義之雜環,則其較佳經由c原子連接至 基團Y。 在本發明之一較佳實施例中,Ar為可具有 5個,較佳1、2或3個’更佳丨或2個取代基尺2之苯基,或為 含有1、2或3個選自N、〇及5之雜原子作為環成員的%或^ 員雜芳環,其中該雜芳環可具有卜^^個,較佳卜2 或3個,更佳個取代基r3。更確切而言,純佳為可 '、有/ 2 3 4或5個,較佳卜2或3個,更佳】或2個取代 基R2之苯基或為含有!個選自N、〇及8之雜原子及視情況 可選的1或2個其他氮原子作為環成員的5·或6_員雜芳環, 其中該雜芳環可具有1、2、3或4個,較佳⑷個取代基 R3。上文列舉了合適之5_或6•員雜芳族基團。 m 149027.doc -32- 201103430 在上文列舉之雜芳環47 ’較佳為°比°定基,諸如吼咬-2-基、吡啶基或吡啶-4-基;嘧啶基,諸如2-嘧啶基' 4-嘧 定基或5-啦唆基;吱喃基’諸如2-呋喃基或3-呋喃基;噻 吩基’諸如2-噻吩基或3·噻吩基;吡咯基,諸如丨_吡咯 基、2-吡咯基或3·吡咯基,尤其2_吡咯基或3_吡咯基;吡 °坐基’諸如1_吡唑基、3_吡唑基、4_吡唑基或5_吡唑基, 尤其3-吡唑基、4_吡唑基或5_吡唑基;咪唑基,諸如丨_咪 坐基2_咪。坐基或4-咪唾基,尤其2-咪嗤基或4-味嗤基; 噁唑基,諸如2_噁唑基、4噁唑基或5_噁唑基;異噁唑 基°者如3_異°惡唾基、4-異噁唑基或5 -異噁唑基;D塞唑 基’諸如2-嗟唾基、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1,2,4-二唑基、丨,2,4_三唑_3_基、丨,2,4•三唑基、 込3,4-三唑-1-基 ' 丨,3,4·三唑-2-基或1,3,4-三唑-3-基,尤其 1,2’4-三唑基或三唑_2_基。指定連接位置應理解 為相對於環雜原子之“位置且具有最高優先級。舉例而 5,在含有1個環雜原子之環中指定連接位置相對於該 唯-壤雜原子之1·位置。在対基巾,指定連接位置相對 於2個氮環原子之丨及2_位置,在咪録巾,指定連接位置 相對於2個氮環原子之!·及3·位置,在^基中,指定連接 位置相對於氧環原子之!·位置及氮環原子之3_位置,在異 惡嗤基中’指定連接位置相對於氧環原子之i •位置及氮環 原子之2-位置,在㈣基中,指定連接位置相對於硫環原 子之1-位置及氮環原子之3_位置’在異噻唑基中,指定連 149027.doc -33- 201103430 接位置相對於硫環原子之位置及氮環原子之2·位置 等。CcC5 alkylene group: a divalent branch having 4 to 5 carbon atoms or preferably an unbranched chain 'e.g., ch2ch2ch2ch2 or ch2ch2ch2ch2ch2. The group -SM is more specifically a group _S-M+, wherein M+ is a metal cation equivalent or an ammonium 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 Å. Statements on suitable and preferred characteristics of the compounds of the invention, especially with respect to their substituents Ar Het, A, γ, r1, r2, r3, ruler 4, ruler 5, R6, R6a, R7, R8, R9, R丨. , R, 丨, Rl2, Rl3, Rl4, r15, r16, m, Rd, M, Q and indices, and the statements about their use are themselves and in particular in all possible combinations with each other. If Ar is a heterocyclic ring as defined above, it is preferably attached to the group Y via a c atom. In a preferred embodiment of the invention, Ar is a phenyl group which may have 5, preferably 1, 2 or 3 'better' or 2 substituted base 2, or 1 , 2 or 3 A hetero atom having a hetero atom selected from N, oxime and 5 as a member of a ring, wherein the heteroaryl ring may have a ruthenium group, preferably 2 or 3, more preferably a substituent r3. More specifically, it is preferably selected from the group consisting of N, 有, / 2 3 4 or 5, preferably 2 or 3, more preferably 2 or 2 substituents R 2 phenyl or And a hetero atom of 8 and optionally 1 or 2 other nitrogen atoms as a 5 or 6-membered heteroaryl ring of the ring member, wherein the heteroaryl ring may have 1, 2, 3 or 4, preferably (4) a substituent R3. Suitable 5 or 6 member heteroaromatic groups are listed above. m 149027.doc -32- 201103430 The heteroaryl ring 47' recited above is preferably a ° ratio, such as a guanidine-2-yl, pyridyl or pyridin-4-yl group; a pyrimidinyl group such as 2-pyrimidine '' 4-pyridyl or 5-ylidene; fluorenyl 'such as 2-furyl or 3-furyl; thienyl' such as 2-thienyl or 3-thiophenyl; pyrrolyl, such as 丨-pyrrolyl , 2-pyrrolyl or 3·pyrrolyl, especially 2-pyrrolyl or 3-pyrrolyl; pyridyl such as 1-pyrazolyl, 3-pyrazolyl, 4-pyrazolyl or 5-pyrazole Base, especially 3-pyrazolyl, 4-pyrazolyl or 5-pyrazolyl; imidazolyl, such as 丨_米坐基2_咪. Sodium or 4-mercapto group, especially 2-amimidyl or 4-myristyl; oxazolyl, such as 2-oxazolyl, 4-oxazolyl or 5-oxazolyl; isoxazolyl Such as 3-isooxasyl, 4-isoxazolyl or 5-isoxazolyl; D-zezolyl 'such as 2-hydrazino, 4-thiazolyl or 5-thiazolyl; isothiazolyl, such as 3-isothiazolyl, 4-isothiazolyl or 5-isothiazolyl; and triazolyl, such as 1,2,4-diazolyl, indole, 2,4-triazole-3-yl, anthracene, 2 , 4•Triazolyl, 込3,4-triazol-1-yl' oxime, 3,4·triazol-2-yl or 1,3,4-triazol-3-yl, especially 1,2' 4-Triazolyl or triazole-2-yl. The specified position of attachment is understood to be the "position" with respect to the ring heteroatom and has the highest priority. For example, 5, the position of the connection is specified in the ring containing one ring heteroatom relative to the position of the only-organic hetero atom. In the base towel, the position of the connection is specified relative to the two nitrogen ring atoms and the 2_ position. In the microphone, the specified connection position is relative to the two nitrogen ring atoms!··3· position, in the base, Specify the position of the connection relative to the oxygen ring atom: · position and the 3_ position of the nitrogen ring atom, in the hetero-oxo group 'specified connection position relative to the oxygen ring atom i position and the nitrogen ring atom 2-position, in (d) In the base, the position of the connection is specified relative to the 1-position of the sulfur ring atom and the 3_position of the nitrogen ring atom. In the isothiazolyl group, the position of the 149027.doc -33-201103430 is determined relative to the position of the sulfur ring atom and The position of the nitrogen ring atom, etc.

Ar更佳為可具有i、2、q、/i4、CAn , 更 芳 噻 4- 々八们Z 3、4或5個,較佳!、2或3個, 佳1或2個取代基R2之苯基,戋為 4馮選自以下之5-或6-員雜 環:吡咬基,諸如η比咬_2_基、„比咬_3_基或。比。定·4·基; 吩基,諸如2-或3“塞吩基;及。塞嗤基,諸如2嗟唑基、 嗟唾基或5-嗟唑基。尤其較佳為吼啶基,諸如。比咬·^基 吡啶-3-基或吡啶-肛基,|尤其為吡啶_2_基,其中該雜芳 環可具有!、2、3或4個,較佳i、2或3個,更佳M2個取 代基R3。 在Ar為6-員雜芳環之情況下,其較佳具有〇、i、2或3 個,更佳0、1或2個取代基r3,其中兩個或兩個以上取代 基R3可相同或不同。在心為5_員雜芳環之情況下,其較佳 具有0、1或2個取代基R3,其令兩個取代基尺3可相同或不 同。 R2較佳選自齒素、OH、SH、N02、CN、CVC4烷基、 CVC4鹵烷基、Ci-C4烷氧基_Cl_C4烷基、Cl_c^氧基、Cl_ C4院氧基-C「C4烧氧基及c〗-C4鹵烷氧基,更佳選自氟、 氣、溴、(VC4烷基、(VC4鹵烷基、Ci-C*烷氧基及^心 鹵炫氧基’甚至更佳選自氟、氯、溴、CH3、chf2、 CF3、0CH3、OCHF2及0CF3,且尤其選自氟、氣、溴、 ch3、cf3、och3及 ocf3。 R3可經C或N連接,但較佳連接至Ar之C原子。 R3較佳選自鹵素' OH、SH、N〇2、CN、CVC4烷基、More preferably, Ar may have i, 2, q, /i4, CAn, more aryl thiophene 4- 々8 Z 3, 4 or 5, preferably! , 2 or 3, preferably 1 or 2 substituents R 2 phenyl, 戋 4 von selected from the following 5- or 6-membered heterocyclic ring: pyridyl group, such as η than bite_2_ base, „ ratio Bite _3_ base or. ratio. 1,4-group; phenyl, such as 2- or 3" thiophene; and. A thiol group such as 2 oxazolyl, oxime or 5-carbazolyl. Especially preferred is an acridinyl group such as. The pyridine-3-yl group or the pyridine-anion group, especially the pyridine-2-yl group, wherein the heteroaromatic ring can have! 2, 3 or 4, preferably i, 2 or 3, more preferably M2 substituents R3. In the case where Ar is a 6-membered heteroaryl ring, it preferably has 〇, i, 2 or 3, more preferably 0, 1 or 2 substituents r3, wherein two or more substituents R3 may be the same Or different. In the case where the core is a 5-membered heteroaryl ring, it preferably has 0, 1 or 2 substituents R3 which may make the two substituent bases 3 the same or different. R2 is preferably selected from the group consisting of dentate, OH, SH, N02, CN, CVC4 alkyl, CVC4 haloalkyl, Ci-C4 alkoxy_Cl_C4 alkyl, Cl_coxy, Cl_C4 alkoxy-C "C4 Alkoxy groups and c--C4 haloalkoxy groups, more preferably selected from the group consisting of fluorine, gas, bromine, (VC4 alkyl, (VC4 haloalkyl, Ci-C* alkoxy and ^halohaloxy) even More preferably selected from the group consisting of fluorine, chlorine, bromine, CH3, chf2, CF3, 0CH3, OCHF2 and 0CF3, and especially selected from the group consisting of fluorine, gas, bromine, ch3, cf3, och3 and ocf3. R3 may be connected via C or N, but Preferably, it is bonded to the C atom of Ar. R3 is preferably selected from the group consisting of halogen 'OH, SH, N〇2, CN, CVC4 alkyl,

LSI 149027.doc ·34· 201103430 C!-C4_^ 基、Ci-C4 烧氧基 _ C 1 - C 4 炫基、C 1 - C 4 烧氧基、C 1 -C4烧乳基- C1-C4烧氧基及C1-C4鹵烧氧基,更佳選自氟、 氣、溴、(VC4烷基、CVCU鹵烷基、CVC4烷氧基及心-匕 鹵烷氧基,甚至更佳選自氟、氣、溴、CH3、CHF2、 CF3、OCH3、OCHF2及OCF3,且尤其選自氟、氣、溴、 CH3、CF3、OCH3及 OCF3。 詳言之,Ar係選自下式Ar.l至Ar.50,其中在式Ar.l中, 變數R21、R22、R23、R24及R25之組合係選自以下表A之一 列中所給出的定義。LSI 149027.doc ·34· 201103430 C!-C4_^ Base, Ci-C4 alkoxy _ C 1 - C 4 炫, C 1 - C 4 alkoxy, C 1 -C4 succinyl - C1-C4 Alkoxy groups and C1-C4 halogen alkoxy groups, more preferably selected from the group consisting of fluorine, gas, bromine, (VC4 alkyl, CVCU haloalkyl, CVC4 alkoxy and cardio-halo alkoxy, even more preferably selected from Fluorine, gas, bromine, CH3, CHF2, CF3, OCH3, OCHF2 and OCF3, and especially selected from the group consisting of fluorine, gas, bromine, CH3, CF3, OCH3 and OCF3. In detail, the Ar system is selected from the following formula Ar.l to Ar. 50, wherein in the formula Ar.l, the combination of the variables R21, R22, R23, R24 and R25 is selected from the definitions given in the column of Table A below.

Ar.2Ar.2

Ar.3 Αγ.4 Ar.5 Ar.6 Ar.7Ar.3 Αγ.4 Ar.5 Ar.6 Ar.7

ΑΠΟ Ar.11 Ar.12 Ar.13 Ar.14 Ar.15ΑΠΟ Ar.11 Ar.12 Ar.13 Ar.14 Ar.15

Ar.8 Ar.9Ar.8 Ar.9

Ar.16 Ar.17 Ar.18 Ar.19 Ar.20 Ar.21 Ar.22 Ar.23Ar.16 Ar.17 Ar.18 Ar.19 Ar.20 Ar.21 Ar.22 Ar.23

Ar.32 Ar.33 Ar.34 Ar.35 Ar.36 Ar.37 Ar.38 Ar.39Ar.32 Ar.33 Ar.34 Ar.35 Ar.36 Ar.37 Ar.38 Ar.39

Ar.40Ar.40

Ar.41Ar.41

Ar.42 Ar.43 149027.doc -35- 201103430Ar.42 Ar.43 149027.doc -35- 201103430

Ar.44 Ar.45 Ar.46 Ar.47 Ar.48 Ar.49 Ar.50Ar.44 Ar.45 Ar.46 Ar.47 Ar.48 Ar.49 Ar.50

表A 編號 R21 R22 R23 R24 R25 A-l H H H H H A-2 F H H H H A-3 H F H H H A-4 H H F H H A-5 Cl H H H H A-6 H Cl H H H A-7 H H Cl H H A-8 Br H H H H A-9 H Br H H H A-10 H H Br H H A-ll ch3 H H H H A-12 H ch3 H H H A-l 3 H H ch3 H H A-14 chf2 H H H H A-l 5 H chf2 H H H A-16 H H chf2 H H A-17 cf3 H H H H A-l 8 H cf3 H H H A-19 H H cf3 H H A-20 och3 H H H H A-21 H OCH3 H H H A-22 H H OCH3 H H A-23 OCHF2 H H H H A-24 H OCHF2 H H H A-25 H H OCHF2 H H A-26 OCF3 H H H H A-27 H OCF3 H H H m 149027.doc -36· 201103430Table A No. R21 R22 R23 R24 R25 Al HHHHH A-2 FHHHH A-3 HFHHH A-4 HHFHH A-5 Cl HHHH A-6 H Cl HHH A-7 HH Cl HH A-8 Br HHHH A-9 H Br HHH A-10 HH Br HH A-ll ch3 HHHH A-12 H ch3 HHH Al 3 HH ch3 HH A-14 chf2 HHHH Al 5 H chf2 HHH A-16 HH chf2 HH A-17 cf3 HHHH Al 8 H cf3 HHH A- 19 HH cf3 HH A-20 och3 HHHH A-21 H OCH3 HHH A-22 HH OCH3 HH A-23 OCHF2 HHHH A-24 H OCHF2 HHH A-25 HH OCHF2 HH A-26 OCF3 HHHH A-27 H OCF3 HHH m 149027.doc -36· 201103430

編號 R21 R22 R23 R24 R25 A-28 H H OCF3 H H A-29 F F H H H A-30 F H F H H A-31 F H H F H A-32 F H H H F A-33 H F F H H A-34 H F H F H A-35 Cl Cl H H H A-36 Cl H Cl H H A-37 Cl H H Cl H A-38 Cl H H H Cl A-39 H Cl Cl H H A-40 H Cl H Cl H A-41 Br Br H H H A-42 Br H Br H H A-43 Br H H Br H A-44 Br H H H Br A-45 H Br Br H H A-46 H Br H Br H A-47 ch3 ch3 H H H A-48 ch3 H ch3 H H A-49 ch3 H H ch3 H A-50 ch3 H H H ch3 A-51 H ch3 ch3 H H A-52 H ch3 H ch3 H A-53 chf2 chf2 H H H A-54 chf2 H chf2 H H A-55 chf2 H H chf2 H A-56 chf2 H H H chf2 A-57 H chf2 chf2 H H A-58 H chf2 H chf2 H A-59 cf3 cf3 H H H A-60 cf3 H cf3 H H A-61 cf3 H H cf3 H 149027.doc -37- 201103430No. R21 R22 R23 R24 R25 A-28 HH OCF3 HH A-29 FFHHH A-30 FHFHH A-31 FHHFH A-32 FHHHF A-33 HFFHH A-34 HFHFH A-35 Cl Cl HHH A-36 Cl H Cl HH A -37 Cl HH Cl H A-38 Cl HHH Cl A-39 H Cl Cl HH A-40 H Cl H Cl H A-41 Br Br HHH A-42 Br H Br HH A-43 Br HH Br H A-44 Br HHH Br A-45 H Br Br HH A-46 H Br H Br H A-47 ch3 ch3 HHH A-48 ch3 H ch3 HH A-49 ch3 HH ch3 H A-50 ch3 HHH ch3 A-51 H ch3 ch3 HH A-52 H ch3 H ch3 H A-53 chf2 chf2 HHH A-54 chf2 H chf2 HH A-55 chf2 HH chf2 H A-56 chf2 HHH chf2 A-57 H chf2 chf2 HH A-58 H chf2 H chf2 H A-59 cf3 cf3 HHH A-60 cf3 H cf3 HH A-61 cf3 HH cf3 H 149027.doc -37- 201103430

編號 R21 R22 R23 R24 R25 A-62 cf3 H H H cf3 A-63 H cf3 cf3 H H A-64 H cf3 H cf3 H A-65 OCH3 OCH3 H H H A-66 OCH3 H OCH3 H H A-67 OCH3 H H OCH3 H A-68 OCH3 H H H OCH3 A-69 H OCH3 OCH3 H H A-70 H OCH3 H OCH3 H A-71 OCHF2 OCHF2 H H H A-72 OCHF2 H OCHF2 H H A-73 OCHF2 H H OCHF2 H A-74 OCHF2 H H H OCHF2 A-75 H OCHF2 OCHF2 H H A-76 H ochf2 H OCHF2 H A-77 OCF3 OCF3 H H H A-78 OCF3 H OCF3 H H A-79 OCF3 H H OCF3 H A-80 OCF3 H H H OCF3 A-81 H OCF3 OCF3 H H A-82 H OCF3 H OCF3 H A-83 F Cl H H H A-84 F H Cl H H A-85 F H H Cl H A-86 F H H H Cl A-87 H F Cl H H A-88 H F H Cl H A-89 Cl F H H H A-90 Cl H F H H A-91 Cl H H F H A-92 H Cl F H H A-93 F Br H H H A-94 F H Br H H A-95 F H H Br HNo. R21 R22 R23 R24 R25 A-62 cf3 HHH cf3 A-63 H cf3 cf3 HH A-64 H cf3 H cf3 H A-65 OCH3 OCH3 HHH A-66 OCH3 H OCH3 HH A-67 OCH3 HH OCH3 H A-68 OCH3 HHH OCH3 A-69 H OCH3 OCH3 HH A-70 H OCH3 H OCH3 H A-71 OCHF2 OCHF2 HHH A-72 OCHF2 H OCHF2 HH A-73 OCHF2 HH OCHF2 H A-74 OCHF2 HHH OCHF2 A-75 H OCHF2 OCHF2 HH A-76 H ochf2 H OCHF2 H A-77 OCF3 OCF3 HHH A-78 OCF3 H OCF3 HH A-79 OCF3 HH OCF3 H A-80 OCF3 HHH OCF3 A-81 H OCF3 OCF3 HH A-82 H OCF3 H OCF3 H A-83 F Cl HHH A-84 FH Cl HH A-85 FHH Cl H A-86 FHHH Cl A-87 HF Cl HH A-88 HFH Cl H A-89 Cl FHHH A-90 Cl HFHH A-91 Cl HHFH A-92 H Cl FHH A-93 F Br HHH A-94 FH Br HH A-95 FHH Br H

[SI 149027.doc -38- 201103430[SI 149027.doc -38- 201103430

編號 R21 R22 R23 R24 R25 A-96 F H H H Br A-97 H F Br H H A-98 H F H Br H A-99 Br F H H H A-100 Br H F H H A-101 Br H H F H A-102 H Br F H H A-103 F ch3 H H H A-104 F H ch3 H H A-105 F H H ch3 H A-106 F H H H ch3 A-107 H F ch3 H H A-108 H F H ch3 H A-109 ch3 F H H H A-110 ch3 H F H H A-lll ch3 H H F H A-112 H ch3 F H H A-113 F chf2 H H H A-114 F H chf2 H H A-115 F H H chf2 H A-116 F H H H chf2 A-117 H F chf2 H H A-118 H F H chf2 H A-119 chf2 F H H H A-120 chf2 H F H H A-121 chf2 H H F H A-122 H chf2 F H H A-123 F cf3 H H H A-124 F H cf3 H H A-125 F H H cf3 H A-126 F H H H cf3 A-127 H F cf3 H H A-128 H F H cf3 H A-129 cf3 F H H H 149027.doc •39- 201103430No. R21 R22 R23 R24 R25 A-96 FHHH Br A-97 HF Br HH A-98 HFH Br H A-99 Br FHHH A-100 Br HFHH A-101 Br HHFH A-102 H Br FHH A-103 F ch3 HHH A-104 FH ch3 HH A-105 FHH ch3 H A-106 FHHH ch3 A-107 HF ch3 HH A-108 HFH ch3 H A-109 ch3 FHHH A-110 ch3 HFHH A-lll ch3 HHFH A-112 H ch3 FHH A-113 F chf2 HHH A-114 FH chf2 HH A-115 FHH chf2 H A-116 FHHH chf2 A-117 HF chf2 HH A-118 HFH chf2 H A-119 chf2 FHHH A-120 chf2 HFHH A-121 chf2 HHFH A-122 H chf2 FHH A-123 F cf3 HHH A-124 FH cf3 HH A-125 FHH cf3 H A-126 FHHH cf3 A-127 HF cf3 HH A-128 HFH cf3 H A-129 cf3 FHHH 149027.doc • 39- 201103430

編號 R21 R22 R23 R24 R25 A-130 cf3 H F H H A-131 cf3 H H F H A-132 H cf3 F H H A-133 F och3 H H H A-134 F H och3 H H A-135 F H H och3 H A-136 F H H H och3 A-137 H F och3 H H A-138 H F H och3 H A-139 och3 F H H H A-140 och3 H F H H A-141 och3 H H F H A-142 H och3 F H H A-143 F ochf2 H H H A-144 F H ochf2 H H A-145 F H H ochf2 H A-146 F H H H ochf2 A-147 H F ochf2 H H A-148 H F H ochf2 H A-149 ochf2 F H H H A-150 ochf2 H F H H A-151 ochf2 H H F H A-152 H ochf2 F H H A-153 F ocf3 H H H A-154 F H ocf3 H H A-155 F H H ocf3 H A-156 F H H H ocf3 A-157 H F ocf3 H H A-158 H F H ocf3 H A-159 ocf3 F H H H A-160 ocf3 H F H H A-161 ocf3 H H F H A-162 H ocf3 F H H A-163 Cl Br H H HNo. R21 R22 R23 R24 R25 A-130 cf3 HFHH A-131 cf3 HHFH A-132 H cf3 FHH A-133 F och3 HHH A-134 FH och3 HH A-135 FHH och3 H A-136 FHHH och3 A-137 HF och3 HH A-138 HFH och3 H A-139 och3 FHHH A-140 och3 HFHH A-141 och3 HHFH A-142 H och3 FHH A-143 F ochf2 HHH A-144 FH ochf2 HH A-145 FHH ochf2 H A-146 FHHH Ochf2 A-147 HF ochf2 HH A-148 HFH ochf2 H A-149 ochf2 FHHH A-150 ochf2 HFHH A-151 ochf2 HHFH A-152 H ochf2 FHH A-153 F ocf3 HHH A-154 FH ocf3 HH A-155 FHH Ocf3 H A-156 FHHH ocf3 A-157 HF ocf3 HH A-158 HFH ocf3 H A-159 ocf3 FHHH A-160 ocf3 HFHH A-161 ocf3 HHFH A-162 H ocf3 FHH A-163 Cl Br HHH

[si 149027.doc -40- 201103430[si 149027.doc -40- 201103430

編號 R21 R22 R23 R24 R25 A-164 Cl H Br H H A-165 Cl H H Br H A-166 Cl H H H Br A-167 H Cl Br H H A-168 H Cl H Br H A-169 Br Cl H H H A-170 Br H Cl H H A-171 Br H H Cl H A-172 H Br Cl H H A-173 Cl ch3 H H H A-174 Cl H ch3 H H A-175 Cl H H ch3 H A-176 Cl H H H ch3 A-177 H Cl ch3 H H A-178 H Cl H ch3 H A-179 ch3 Cl H H H A-180 ch3 H Cl H H A-181 ch3 H H Cl H A-182 H ch3 Cl H H A-183 Cl chf2 H H H A-184 Cl H chf2 H H A-185 Cl H H chf2 H A-186 Cl H H H chf2 A-187 H Cl chf2 H H A-188 H Cl H chf2 H A-189 chf2 Cl H H H A-190 chf2 H Cl H H A-191 chf2 H H Cl H A-192 H chf2 Cl H H A-193 Cl cf3 H H H A-194 Cl H cf3 H H A-195 Cl H H cf3 H A-196 Cl H H H cf3 A-197 H Cl cf3 H H 149027.doc • 41 · 201103430No. R21 R22 R23 R24 R25 A-164 Cl H Br HH A-165 Cl HH Br H A-166 Cl HHH Br A-167 H Cl Br HH A-168 H Cl H Br H A-169 Br Cl HHH A-170 Br H Cl HH A-171 Br HH Cl H A-172 H Br Cl HH A-173 Cl ch3 HHH A-174 Cl H ch3 HH A-175 Cl HH ch3 H A-176 Cl HHH ch3 A-177 H Cl ch3 HH A-178 H Cl H ch3 H A-179 ch3 Cl HHH A-180 ch3 H Cl HH A-181 ch3 HH Cl H A-182 H ch3 Cl HH A-183 Cl chf2 HHH A-184 Cl H chf2 HH A -185 Cl HH chf2 H A-186 Cl HHH chf2 A-187 H Cl chf2 HH A-188 H Cl H chf2 H A-189 chf2 Cl HHH A-190 chf2 H Cl HH A-191 chf2 HH Cl H A-192 H chf2 Cl HH A-193 Cl cf3 HHH A-194 Cl H cf3 HH A-195 Cl HH cf3 H A-196 Cl HHH cf3 A-197 H Cl cf3 HH 149027.doc • 41 · 201103430

編號 R21 R22 R23 R24 R25 A-198 H Cl H cf3 H A-199 cf3 Cl H H H A-200 cf3 H Cl H H A-201 cf3 H H Cl H A-202 H cf3 Cl H H A-203 Cl och3 H H H A-204 Cl H och3 H H A-205 Cl H H och3 H A-206 Cl H H H och3 A-207 H Cl och3 H H A-208 H Cl H och3 H A-209 och3 Cl H H H A-210 och3 H Cl H H A-211 och3 H H Cl H A-212 H och3 Cl H H A-213 Cl ochf2 H H H A-214 Cl H ochf2 H H A-215 Cl H H ochf2 H A-216 Cl H H H OCHF2 A-217 H Cl ochf2 H H A-218 H Cl H ochf2 H A-219 ochf2 Cl H H H A-220 ochf2 H Cl H H A-221 ochf2 H H Cl H A-222 H ochf2 Cl H H A-223 Cl ocf3 H H H A-224 Cl H ocf3 H H A-225 Cl H H ocf3 H A-226 Cl H H H OCF3 A-227 H Cl ocf3 H H A-228 H Cl H ocf3 H A-229 ocf3 Cl H H H A-230 ocf3 H Cl H H A-231 ocf3 H H Cl H m: 149027.doc -42- 201103430No. R21 R22 R23 R24 R25 A-198 H Cl H cf3 H A-199 cf3 Cl HHH A-200 cf3 H Cl HH A-201 cf3 HH Cl H A-202 H cf3 Cl HH A-203 Cl och3 HHH A-204 Cl H och3 HH A-205 Cl HH och3 H A-206 Cl HHH och3 A-207 H Cl och3 HH A-208 H Cl H och3 H A-209 och3 Cl HHH A-210 och3 H Cl HH A-211 och3 HH Cl H A-212 H och3 Cl HH A-213 Cl ochf2 HHH A-214 Cl H ochf2 HH A-215 Cl HH ochf2 H A-216 Cl HHH OCHF2 A-217 H Cl ochf2 HH A-218 H Cl H ochf2 H A-219 ochf2 Cl HHH A-220 ochf2 H Cl HH A-221 ochf2 HH Cl H A-222 H ochf2 Cl HH A-223 Cl ocf3 HHH A-224 Cl H ocf3 HH A-225 Cl HH ocf3 H A-226 Cl HHH OCF3 A-227 H Cl ocf3 HH A-228 H Cl H ocf3 H A-229 ocf3 Cl HHH A-230 ocf3 H Cl HH A-231 ocf3 HH Cl H m: 149027.doc -42- 201103430

編號 R21 R22 R23 R24 R25 A-232 H OCF3 Cl H H A-233 Br ch3 H H H A-234 Br H ch3 H H A-235 Br H H ch3 H A-236 Br H H H ch3 A-237 H Br ch3 H H A-238 H Br H ch3 H A-239 ch3 Br H H H A-240 ch3 H Br H H A-241 ch3 H H Br H A-242 H ch3 Br H H A-243 Br chf2 H H H A-244 Br H chf2 H H A-245 Br H H chf2 H A-246 Br H H H chf2 A-247 H Br chf2 H H A-248 H Br H chf2 H A-249 chf2 Br H H H A-250 chf2 H Br H H A-251 chf2 H H Br H A-252 H chf2 Br H H A-253 Br cf3 H H H A-254 Br H cf3 H H A-255 Br H H cf3 H A-256 Br H H H cf3 A-257 H Br cf3 H H A-258 H Br H cf3 H A-259 cf3 Br H H H A-260 cf3 H Br H H A-261 cf3 H H Br H A-262 H cf3 Br H H A-263 Br OCH3 H H H A-264 Br H OCH3 H H A-265 Br H H OCH3 H 149027.doc -43- 201103430No. R21 R22 R23 R24 R25 A-232 H OCF3 Cl HH A-233 Br ch3 HHH A-234 Br H ch3 HH A-235 Br HH ch3 H A-236 Br HHH ch3 A-237 H Br ch3 HH A-238 H Br H ch3 H A-239 ch3 Br HHH A-240 ch3 H Br HH A-241 ch3 HH Br H A-242 H ch3 Br HH A-243 Br chf2 HHH A-244 Br H chf2 HH A-245 Br HH chf2 H A-246 Br HHH chf2 A-247 H Br chf2 HH A-248 H Br H chf2 H A-249 chf2 Br HHH A-250 chf2 H Br HH A-251 chf2 HH Br H A-252 H chf2 Br HH A -253 Br cf3 HHH A-254 Br H cf3 HH A-255 Br HH cf3 H A-256 Br HHH cf3 A-257 H Br cf3 HH A-258 H Br H cf3 H A-259 cf3 Br HHH A-260 cf3 H Br HH A-261 cf3 HH Br H A-262 H cf3 Br HH A-263 Br OCH3 HHH A-264 Br H OCH3 HH A-265 Br HH OCH3 H 149027.doc -43- 201103430

編號 R21 R22 R23 R24 R25 A-266 Br H H H OCH3 A-267 H Br OCH3 H H A-268 H Br H OCH3 H A-269 OCH3 Br H H H A-270 OCH3 H Br H H A-271 OCH3 H H Br H A-272 H OCH3 Br H H A-273 Br OCHF2 H H H A-274 Br H OCHFz H H A-275 Br H H OCHF2 H A-276 Br H H H OCHFz A-277 H Br OCHF2 H H A-278 H Br H OCHF2 H A-279 OCHF2 Br H H H A-280 OCHF2 H Br H H A-281 OCHF2 H H Br H A-282 H OCHF2 Br H H A-283 Br OCF3 H H H A-284 Br H OCF3 H H A-285 Br H H OCF3 H A-286 Br H H H OCF3 A-287 H Br OCF3 H H A-288 H Br H OCF3 H A-289 OCF3 Br H H H A-290 OCF3 H Br H H A-291 OCF3 H H Br H A-292 H OCF3 Br H H A-293 ch3 chf2 H H H A-294 ch3 H chf2 H H A-295 ch3 H H chf2 H A-296 ch3 H H H chf2 A-297 H ch3 chf2 H H A-298 H ch3 H chf2 H A-299 chf2 ch3 H H H m 149027.doc -44- 201103430No. R21 R22 R23 R24 R25 A-266 Br HHH OCH3 A-267 H Br OCH3 HH A-268 H Br H OCH3 H A-269 OCH3 Br HHH A-270 OCH3 H Br HH A-271 OCH3 HH Br H A-272 H OCH3 Br HH A-273 Br OCHF2 HHH A-274 Br H OCHFz HH A-275 Br HH OCHF2 H A-276 Br HHH OCHFz A-277 H Br OCHF2 HH A-278 H Br H OCHF2 H A-279 OCHF2 Br HHH A-280 OCHF2 H Br HH A-281 OCHF2 HH Br H A-282 H OCHF2 Br HH A-283 Br OCF3 HHH A-284 Br H OCF3 HH A-285 Br HH OCF3 H A-286 Br HHH OCF3 A- 287 H Br OCF3 HH A-288 H Br H OCF3 H A-289 OCF3 Br HHH A-290 OCF3 H Br HH A-291 OCF3 HH Br H A-292 H OCF3 Br HH A-293 ch3 chf2 HHH A-294 ch3 H chf2 HH A-295 ch3 HH chf2 H A-296 ch3 HHH chf2 A-297 H ch3 chf2 HH A-298 H ch3 H chf2 H A-299 chf2 ch3 HHH m 149027.doc -44- 201103430

編號 R21 R22 R23 R24 R25 A-300 chf2 H ch3 H H A-301 chf2 H H ch3 H A-302 H chf2 ch3 H H A-303 ch3 cf3 H H H A-304 ch3 H cf3 H H A-305 ch3 H H cf3 H A-306 ch3 H H H cf3 A-307 H ch3 cf3 H H A-308 H ch3 H cf3 H A-309 cf3 ch3 H H H A-310 cf3 H ch3 H H A-311 cf3 H H ch3 H A-312 H cf3 ch3 H H A-313 ch3 och3 H H H A-314 ch3 H OCH3 H H A-315 ch3 H H OCH3 H A-316 ch3 H H H OCH3 A-317 H ch3 OCH3 H H A-318 H ch3 H OCH3 H A-319 OCH3 ch3 H H H A-320 OCH3 H ch3 H H A-321 OCH3 H H ch3 H A-322 H 〇CH3 ch3 H H A-323 ch3 OCHF2 H H H A-324 ch3 H OCHF2 H H A-325 ch3 H H OCHF2 H A-326 ch3 H H H OCHF2 A-327 H ch3 OCHF2 H H A-328 H ch3 H OCHF2 H A-329 OCHF2 ch3 H H H A-330 OCHF2 H ch3 H H A-331 OCHF2 H H ch3 H A-332 H OCHF2 ch3 H H A-333 ch3 OCF3 H H H 149027.doc -45- 201103430No. R21 R22 R23 R24 R25 A-300 chf2 H ch3 HH A-301 chf2 HH ch3 H A-302 H chf2 ch3 HH A-303 ch3 cf3 HHH A-304 ch3 H cf3 HH A-305 ch3 HH cf3 H A-306 Ch3 HHH cf3 A-307 H ch3 cf3 HH A-308 H ch3 H cf3 H A-309 cf3 ch3 HHH A-310 cf3 H ch3 HH A-311 cf3 HH ch3 H A-312 H cf3 ch3 HH A-313 ch3 och3 HHH A-314 ch3 H OCH3 HH A-315 ch3 HH OCH3 H A-316 ch3 HHH OCH3 A-317 H ch3 OCH3 HH A-318 H ch3 H OCH3 H A-319 OCH3 ch3 HHH A-320 OCH3 H ch3 HH A -321 OCH3 HH ch3 H A-322 H 〇CH3 ch3 HH A-323 ch3 OCHF2 HHH A-324 ch3 H OCHF2 HH A-325 ch3 HH OCHF2 H A-326 ch3 HHH OCHF2 A-327 H ch3 OCHF2 HH A-328 H ch3 H OCHF2 H A-329 OCHF2 ch3 HHH A-330 OCHF2 H ch3 HH A-331 OCHF2 HH ch3 H A-332 H OCHF2 ch3 HH A-333 ch3 OCF3 HHH 149027.doc -45- 201103430

編號 R21 R22 R23 R24 R25 A-334 ch3 H OCF3 H H A-335 ch3 H H OCF3 H A-336 ch3 H H H OCF3 A-337 H ch3 OCF3 H H A-338 H ch3 H OCF3 H A-339 OCF3 ch3 H H H A-340 OCF3 H ch3 H H A-341 OCF3 H H ch3 H A-342 H OCF3 ch3 H H A-343 chf2 cf3 H H H A-344 chf2 H cf3 H H A-345 chf2 H H cf3 H A-346 chf2 H H H cf3 A-347 H chf2 cf3 H H A-348 H chf2 H cf3 H A-349 cf3 chf2 H H H A-350 cf3 H chf2 H H A-351 cf3 H H chf2 H A-352 H cf3 chf2 H H A-353 chf2 OCH3 H H H A-354 chf2 H OCH3 H H A-355 chf2 H H OCH3 H A-356 chf2 H H H OCH3 A-357 H chf2 OCH3 H H A-358 H chf2 H OCH3 H A-359 OCH3 chf2 H H H A-360 OCH3 H chf2 H H A-361 OCH3 H H chf2 H A-362 H OCH3 chf2 H H A-363 chf2 OCHF2 H H H A-364 chf2 H OCHF2 H H A-365 chf2 H H OCHF2 H A-366 chf2 H H H OCHF2 A-367 H chf2 OCHF2 H HNo. R21 R22 R23 R24 R25 A-334 ch3 H OCF3 HH A-335 ch3 HH OCF3 H A-336 ch3 HHH OCF3 A-337 H ch3 OCF3 HH A-338 H ch3 H OCF3 H A-339 OCF3 ch3 HHH A-340 OCF3 H ch3 HH A-341 OCF3 HH ch3 H A-342 H OCF3 ch3 HH A-343 chf2 cf3 HHH A-344 chf2 H cf3 HH A-345 chf2 HH cf3 H A-346 chf2 HHH cf3 A-347 H chf2 cf3 HH A-348 H chf2 H cf3 H A-349 cf3 chf2 HHH A-350 cf3 H chf2 HH A-351 cf3 HH chf2 H A-352 H cf3 chf2 HH A-353 chf2 OCH3 HHH A-354 chf2 H OCH3 HH A -355 chf2 HH OCH3 H A-356 chf2 HHH OCH3 A-357 H chf2 OCH3 HH A-358 H chf2 H OCH3 H A-359 OCH3 chf2 HHH A-360 OCH3 H chf2 HH A-361 OCH3 HH chf2 H A-362 H OCH3 chf2 HH A-363 chf2 OCHF2 HHH A-364 chf2 H OCHF2 HH A-365 chf2 HH OCHF2 H A-366 chf2 HHH OCHF2 A-367 H chf2 OCHF2 HH

[s] 149027.doc • 46- 201103430[s] 149027.doc • 46- 201103430

編號 R21 R22 R23 R24 R25 A-368 H chf2 H OCHF2 H A-369 OCHF2 chf2 H H H A-370 OCHF2 H chf2 H H A-371 OCHF2 H H chf2 H A-372 H OCHF2 chf2 H H A-373 chf2 OCF3 H H H A-374 chf2 H OCF3 H H A-375 chf2 H H OCF3 H A-376 chf2 H H H OCF3 A-377 H chf2 OCF3 H H A-378 H chf2 H OCF3 H A-379 〇CF3 chf2 H H H A-380 OCF3 H chf2 H H A-381 OCF3 H H chf2 H A-382 H OCF3 chf2 H H A-383 cf3 OCH3 H H H A-384 cf3 H OCH3 H H A-385 cf3 H H OCH3 H A-386 cf3 H H H OCH3 A-387 H cf3 OCH3 H H A-388 H cf3 H 〇CH3 H A-389 OCH3 cf3 H H H A-390 OCH3 H cf3 H H A-391 OCH3 H H cf3 H A-392 H OCH3 cf3 H H A-393 cf3 OCHF2 H H H A-394 cf3 H OCHF2 H H A-395 cf3 H H OCHF2 H A-396 cf3 H H H OCHF2 A-397 H cf3 OCHF2 H H A-398 H cf3 H ochf2 H A-399 OCHF2 cf3 H H H A-400 OCHF2 H cf3 H H A-401 OCHF2 H H cf3 H 149027.doc -47- 201103430No. R21 R22 R23 R24 R25 A-368 H chf2 H OCHF2 H A-369 OCHF2 chf2 HHH A-370 OCHF2 H chf2 HH A-371 OCHF2 HH chf2 H A-372 H OCHF2 chf2 HH A-373 chf2 OCF3 HHH A-374 Chf2 H OCF3 HH A-375 chf2 HH OCF3 H A-376 chf2 HHH OCF3 A-377 H chf2 OCF3 HH A-378 H chf2 H OCF3 H A-379 〇CF3 chf2 HHH A-380 OCF3 H chf2 HH A-381 OCF3 HH chf2 H A-382 H OCF3 chf2 HH A-383 cf3 OCH3 HHH A-384 cf3 H OCH3 HH A-385 cf3 HH OCH3 H A-386 cf3 HHH OCH3 A-387 H cf3 OCH3 HH A-388 H cf3 H 〇 CH3 H A-389 OCH3 cf3 HHH A-390 OCH3 H cf3 HH A-391 OCH3 HH cf3 H A-392 H OCH3 cf3 HH A-393 cf3 OCHF2 HHH A-394 cf3 H OCHF2 HH A-395 cf3 HH OCHF2 H A -396 cf3 HHH OCHF2 A-397 H cf3 OCHF2 HH A-398 H cf3 H ochf2 H A-399 OCHF2 cf3 HHH A-400 OCHF2 H cf3 HH A-401 OCHF2 HH cf3 H 149027.doc -47- 201103430

編號 R21 R22 r23 R24 R25 A-402 H OCHF2 cf3 H H A-403 cf3 OCF3 H H H A-404 cf3 H OCF3 H H A-405 cf3 H H OCF3 H A-406 cf3 H H H OCF3 A-407 H cf3 OCF3 H H A-408 H cf3 H OCF3 H A-409 OCF3 cf3 H H H A-410 OCF3 H cf3 H H A-411 OCF3 H H cf3 H A-412 H OCF3 cf3 H H A-413 OCH3 ochf2 H H H A-414 OCH3 H OCHF2 H H A-415 OCH3 H H OCHF2 H A-416 OCH3 H H H OCHF2 A-417 H OCH3 OCHF2 H H A-418 H OCH3 H OCHF2 H A-419 ochf2 OCH3 H H H A-420 OCHF2 H OCH3 H H A-421 OCHF2 H H OCH3 H A-422 H OCHF2 OCH3 H H A-423 OCH3 OCF3 H H H A-424 OCH3 H OCF3 H H A-425 OCH3 H H OCF3 H A-426 OCH3 H H H OCF3 A-427 H OCH3 OCF3 H H A-428 H OCH3 H OCF3 H A-429 OCF3 OCH3 H H H A-430 OCF3 H OCH3 H H A-431 OCF3 H H OCH3 H A-432 H OCF3 OCH3 H H A-433 ochf2 OCF3 H H H A-434 OCHF2 H OCF3 H H A-435 OCHF2 H H OCF3 HNo. R21 R22 r23 R24 R25 A-402 H OCHF2 cf3 HH A-403 cf3 OCF3 HHH A-404 cf3 H OCF3 HH A-405 cf3 HH OCF3 H A-406 cf3 HHH OCF3 A-407 H cf3 OCF3 HH A-408 H Cf3 H OCF3 H A-409 OCF3 cf3 HHH A-410 OCF3 H cf3 HH A-411 OCF3 HH cf3 H A-412 H OCF3 cf3 HH A-413 OCH3 ochf2 HHH A-414 OCH3 H OCHF2 HH A-415 OCH3 HH OCHF2 H A-416 OCH3 HHH OCHF2 A-417 H OCH3 OCHF2 HH A-418 H OCH3 H OCHF2 H A-419 ochf2 OCH3 HHH A-420 OCHF2 H OCH3 HH A-421 OCHF2 HH OCH3 H A-422 H OCHF2 OCH3 HH A -423 OCH3 OCF3 HHH A-424 OCH3 H OCF3 HH A-425 OCH3 HH OCF3 H A-426 OCH3 HHH OCF3 A-427 H OCH3 OCF3 HH A-428 H OCH3 H OCF3 H A-429 OCF3 OCH3 HHH A-430 OCF3 H OCH3 HH A-431 OCF3 HH OCH3 H A-432 H OCF3 OCH3 HH A-433 ochf2 OCF3 HHH A-434 OCHF2 H OCF3 HH A-435 OCHF2 HH OCF3 H

[si 149027.doc -48- 201103430 編號 R21 R22 R23 R24 R25 A-436 OCHF2 H H H OCF3 A-437 H OCHF2 OCF3 H H A-438 H OCHF2 H OCF3 H A-439 OCF3 OCHF2 H H H A-440 OCF3 H OCHF2 H H A-441 OCF3 H H OCHF2 H A-442 H OCF3 OCHF2 H H A-443 F F F H H A-444 F F H F H A-445 F F H H F A-446 F H F F H A-447 F H F H F A-448 H F F F H A-449 Cl Cl Cl H H A-450 Cl Cl H Cl H A-451 Cl Cl H H Cl A-452 Cl H Cl Cl H A-453 Cl H Cl H Cl A-454 H ei Cl Cl H A-455 Br Br Br H H A-456 Br Br H Br H A-457 Br Br H H Br A-458 Br H Br Br H A-459 Br H Br H Br A-460 H Br Br Br H A-461 ch3 ch3 ch3 H H A-462 ch3 ch3 H ch3 H A-463 ch3 ch3 H H ch3 A-464 ch3 H ch3 ch3 H A-465 ch3 H ch3 H ch3 A-466 H ch3 ch3 ch3 H A-467 cf3 cf3 cf3 H H A-468 cf3 cf3 H cf3 H A-469 cf3 cf3 H H cf3 149027.doc 49- 201103430[si 149027.doc -48- 201103430 No. R21 R22 R23 R24 R25 A-436 OCHF2 HHH OCF3 A-437 H OCHF2 OCF3 HH A-438 H OCHF2 H OCF3 H A-439 OCF3 OCHF2 HHH A-440 OCF3 H OCHF2 HH A -441 OCF3 HH OCHF2 H A-442 H OCF3 OCHF2 HH A-443 FFFHH A-444 FFHFH A-445 FFHHF A-446 FHFFH A-447 FHFHF A-448 HFFFH A-449 Cl Cl Cl HH A-450 Cl Cl H Cl H A-451 Cl Cl HH Cl A-452 Cl H Cl Cl H A-453 Cl H Cl H Cl A-454 H ei Cl Cl H A-455 Br Br Br HH A-456 Br Br H Br H A- 457 Br Br HH Br A-458 Br H Br Br H A-459 Br H Br H Br A-460 H Br Br Br H A-461 ch3 ch3 ch3 HH A-462 ch3 ch3 H ch3 H A-463 ch3 ch3 HH Ch3 A-464 ch3 H ch3 ch3 H A-465 ch3 H ch3 H ch3 A-466 H ch3 ch3 ch3 H A-467 cf3 cf3 cf3 HH A-468 cf3 cf3 H cf3 H A-469 cf3 cf3 HH cf3 149027.doc 49- 201103430

編號 R21 R22 R23 R24 R25 A-470 cf3 H cf3 cf3 H A-471 cf3 H cf3 H cf3 A-472 H cf3 cf3 cf3 H A-473 F H Cl H F A-474 F H F H Cl A-475 F H Cl F H A-476 F H Cl H Cl A-477 Cl H F H Cl A-478 Cl H Cl F H A-479 Cl H Cl H F A-480 Cl H F F H A-481 Cl F H F H A-482 F H H F Cl A-483 F Cl H Cl H A-484 F Cl H H Cl A-485 H F F H Cl A-486 Cl F H H F A-487 F H Cl Cl H A-488 F H ch3 H F A-489 F H F H ch3 A-490 F H ch3 F H A-491 F H ch3 H ch3 A-492 ch3 H F H ch3 A-493 ch3 H ch3 F H A-494 ch3 H ch3 H F A-495 ch3 H F F H A-496 ch3 F H F H A-497 F H H F ch3 A-498 F ch3 H ch3 H A-499 F ch3 H H ch3 A-500 H F F H ch3 A-501 ch3 F H H F A-502 F H ch3 ch3 H A-503 F H cf3 H FNo. R21 R22 R23 R24 R25 A-470 cf3 H cf3 cf3 H A-471 cf3 H cf3 H cf3 A-472 H cf3 cf3 cf3 H A-473 FH Cl HF A-474 FHFH Cl A-475 FH Cl FH A-476 FH Cl H Cl A-477 Cl HFH Cl A-478 Cl H Cl FH A-479 Cl H Cl HF A-480 Cl HFFH A-481 Cl FHFH A-482 FHHF Cl A-483 F Cl H Cl H A-484 F Cl HH Cl A-485 HFFH Cl A-486 Cl FHHF A-487 FH Cl Cl H A-488 FH ch3 HF A-489 FHFH ch3 A-490 FH ch3 FH A-491 FH ch3 H ch3 A-492 ch3 HFH Ch3 A-493 ch3 H ch3 FH A-494 ch3 H ch3 HF A-495 ch3 HFFH A-496 ch3 FHFH A-497 FHHF ch3 A-498 F ch3 H ch3 H A-499 F ch3 HH ch3 A-500 HFFH ch3 A-501 ch3 FHHF A-502 FH ch3 ch3 H A-503 FH cf3 HF

L SI 149027.doc -50- 201103430 編號 R21 R22 R23 R24 R25 A-504 F H F H cf3 A-505 F H cf3 F H A-506 F H cf3 H cf3 A-507 cf3 H F H cf3 A-508 cf3 H cf3 F H A-509 cf3 H cf3 H F A-510 cf3 H F F H A-511 cf3 F H F H A-512 F H a H F cf3 A-513 F cf3 H cf3 H A-514 F cf3 H H cf3 A-515 H F F H cf3 A-516 cf3 F H H F A-517 F H cf3 cf3 H A-518 Cl H ch3 H Cl A-519 Cl H Cl H ch3 A-520 Cl H ch3 Cl H A-521 Cl H ch3 H ch3 A-522 ch3 H Cl H ch3 A-523 ch3 H ch3 Cl H A-524 ch3 H ch3 H Cl A-525 ch3 H Cl Cl H A-526 ch3 Cl H Cl H A-527 Cl H H Cl ch3 A-528 Cl ch3 H ch3 H A-529 Cl ch3 H H ch3 A-530 H Cl Cl H ch3 A-531 ch3 Cl H H Cl A-532 Cl H ch3 ch3 H A-533 Cl H cf3 H Cl A-534 Cl H Cl H cf3 A-535 Cl H cf3 Cl H A-536 Cl H cf3 H cf3 A-537 cf3 H Cl H cf3 149027.doc -51 - 201103430 編號 R21 R22 R23 R24 r25 Α-538 cf3 H cf3 Cl H Α-539 cf3 H cf3 H ---—. Cl Α-540 cf3 H Cl Cl ---— H Α-541 cf3 Cl H Cl ---—. H Α-542 Cl H H Cl cf3 ~~~~~~ Α-543 Cl cf3 H cf3 — H Α-544 Cl cf3 H H cf3 Α-545 H Cl Cl H cf3 Α-546 cf3 Cl H H ----- Cl Α-547 Cl H cf3 CF3 — H Α-548 cf3 H Cl H ---- F Α-549 Cl H cf3 F ---___ H Α-550 cf3 H Cl F ——_ H Α-551 cf3 F H Cl ---— H Α-552 Cl H H F —--- cf3 Α-553 Cl H cf3 F ---— H Α-554 Cl H ch3 F H Α-555 ch3 F H Cl " ----~-- H Α-556 ch3 H Cl F ---- H Α-557 Cl H — H F ch3 Α-558 Cl H ch3 F H '------L SI 149027.doc -50- 201103430 No. R21 R22 R23 R24 R25 A-504 FHFH cf3 A-505 FH cf3 FH A-506 FH cf3 H cf3 A-507 cf3 HFH cf3 A-508 cf3 H cf3 FH A-509 cf3 H cf3 HF A-510 cf3 HFFH A-511 cf3 FHFH A-512 FH a HF cf3 A-513 F cf3 H cf3 H A-514 F cf3 HH cf3 A-515 HFFH cf3 A-516 cf3 FHHF A-517 FH cf3 Cf3 H A-518 Cl H ch3 H Cl A-519 Cl H Cl H ch3 A-520 Cl H ch3 Cl H A-521 Cl H ch3 H ch3 A-522 ch3 H Cl H ch3 A-523 ch3 H ch3 Cl H A-524 ch3 H ch3 H Cl A-525 ch3 H Cl Cl H A-526 ch3 Cl H Cl H A-527 Cl HH Cl ch3 A-528 Cl ch3 H ch3 H A-529 Cl ch3 HH ch3 A-530 H Cl Cl H ch3 A-531 ch3 Cl HH Cl A-532 Cl H ch3 ch3 H A-533 Cl H cf3 H Cl A-534 Cl H Cl H cf3 A-535 Cl H cf3 Cl H A-536 Cl H cf3 H Cf3 A-537 cf3 H Cl H cf3 149027.doc -51 - 201103430 No. R21 R22 R23 R24 r25 Α-538 cf3 H cf3 Cl H Α-539 cf3 H cf3 H ---—. Cl Α-540 cf3 H Cl Cl ---- H Α-541 cf3 Cl H Cl ---.. H Α-542 Cl HH Cl cf3 ~~~~~~ Α-543 Cl cf3 H cf3 — H Α-544 Cl cf3 HH cf3 Α-545 H Cl Cl H cf3 Α-546 cf3 Cl HH ----- Cl Α-547 Cl H cf3 CF3 — H Α-548 cf3 H Cl H ---- F Α-549 Cl H Cf3 F ---___ H Α-550 cf3 H Cl F —— _ H Α-551 cf3 FH Cl --- — H Α-552 Cl HHF —--- cf3 Α-553 Cl H cf3 F ---- H Α-554 Cl H ch3 FH Α-555 ch3 FH Cl " ----~-- H Α-556 ch3 H Cl F ---- H Α-557 Cl H — HF ch3 Α-558 Cl H ch3 FH '------

Het較佳經由兩個環c-原子連接至基團γ及第四碳原子 (具有縮8同基團及三唾基甲基)。 在本發明之一較佳實施例中,Het為含有i、2或3個選自 N、〇及8之雜原子作為環成員的(:價)5·或6·員雜芳環, 其4中該雜芳環可具有1、2、3或4個,較佳!或2個取代基 R。更確切而言,Het較佳A冬古κ 為3有1個選自N、Ο及S之雜原 子及視情況可選的丨或2個其 Μ μ # d, 、他氮原子作為環成員的5-或6- 貝雜方裱,其中該雜芳環 個取代其R4 μ + 、有1、2、3或4個,較佳1或2 個取代基R。上文列舉了 疋5-或6_貝雜芳族基團。 149027.doc •52· 201103430 在以上列舉之雜芳環中,較佳為伸π比啶基,諸如2,3-伸 吡啶基、2,4-伸。比啶基、2,5_伸吡啶基、2,6-伸。比啶基、 3.4- 伸吡啶基或3,5-伸吡啶基;伸嘧啶基,諸如2,4_伸嘧啶 基、2,5-伸嘧啶基、4,5-伸嘧啶基或4,6_伸嘧啶基;伸呋喃 基’諸如2,3·伸咬嗔基、2,4_伸„夫味基、2,5_伸吱蜂基或 3.4- 伸呋喃基;噻吩基,諸如2,3_伸噻吩基、2,心伸噻吩 基、2,5-伸噻吩基或3,4_伸嗟吩基;π比咯基,諸如丨,2•伸吡 咯基、1,3-伸吼咯基、2,3_伸吼咯基、2,4伸吼咯基、2,5· 伸吡咯基或3,4-伸吡咯基;伸吡唑基,諸如伸吡唑 基、1,4-伸吼唑基、以十比唾基、3,4_伸。比唑基或3,5-伸 吡唑基;伸咪唑基,諸如i,伸咪唑基、M_伸咪唑基、 1’5·伸Μ基、2’4-伸咪D坐基、2,5_伸味嗤基或4,5_伸咪唑 基H坐基,諸如2,4-伸鳴唑基或2,5•伸噁唑基;異噁 唑基’諸如M-伸異噁唑基或3,5_伸異噁唑基;伸噻: 基,諸如2,4-伸噻唑基或2,5_伸噻唑基;伸異噻唑基,諸 如3,4-伸異㈣基或3,5·伸異嘆唾基;及伸三。坐基,諸如 1二3-伸三録、山·伸三唾基或伸三唾基。指定 連接位置應理解為相對於環雜原子d•位置且具有最高優 先級。舉例而言,在含有丨個環雜原子之環中,指定連接 位置係相對於該唯-環雜原子之丨·位置m坐基中, 指定連接位置相對於2個氮環原子之卜及2_位置,在伸心 基中’指定連接位置相對於2個氮環原子之卜及^位置,在 伸噪唾基中,指定連接位置相對於氧環原子之卜位置及氮 環原子之3-位置,在伸異噁唑基中,指定連接位置相對於 H9027.doc 53· 201103430 氧環原子之!位置及氮環原子之2_位置,在伸噻唑基中, 私疋連接位置相對於硫環原子之i位置及氮環原子之位 置,在伸異嚷。坐I巾,指定連接位置相對於硫環原子之卜 位置及氮環原子之2-位置,等等。 更佳為伸吡啶基,尤其2,5_或3’6_伸。比啶基;伸噻吩 基,尤其2,4-或2,5-伸噻吩基;及伸噻唑基,尤其-伸噻 唑基或2,5-伸噻唑基。甚至更佳為伸。比啶基,尤其2,5•或 3,6-伸吼啶基;及伸噻吩基,尤其2,4_或2,5_伸噻吩基。尤 佳為伸吼啶基,尤其為2,5_或3,6_伸吼啶基。 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R4,其中兩個或兩個以上取代 基R4可相同或不同。在Het為5-員雜芳環之情況下,其較 佳具有0、1或2個取代基R4,其中兩個取代基尺4可相同或 不同。 R4可經C-或Ν-連接,但較佳連接至Het之c原子。 R4較佳選自鹵素、OH、SH ' N02、CN、Ci_c4烧基、 G-C4鹵烧基、Ci-C*炫氧基-CVC4烧基、Ci-Czj烧氧基、c] C4烧氧基-CVC4烧氧基及C】-C:4鹵烧氧基,更佳選自氣、 氣、溴、C〗-C4烷基、C丨-C4鹵烷基、C丨-c4烷氧基及〇丨_(34 鹵烷氧基’甚至更佳選自氟、氣、溴、CH3、CHF2、 CF3、OCH3、OCHFA OCF3,尤佳選自氟、氣、演、 CH3、cf3 ' och3及OCF3,且尤其選自氟及氣。 詳言之,Het係選自下式Het.l至Het.16,其中#為連接至 第四碳原子(其具有縮酮及三唑基甲基)之連接點且*為連接Het is preferably attached to the group γ and the fourth carbon atom (having a condensed group of 8 and a tris-l-methyl group) via two ring c-atoms. In a preferred embodiment of the present invention, Het is a (:valent) 5 or 6-membered heteroaryl ring containing i, 2 or 3 hetero atoms selected from N, fluorene and 8 as ring members, 4 The heteroaromatic ring may have 1, 2, 3 or 4, preferably ! or 2 substituents R. More specifically, Het is preferably A winter κ is 3 having one hetero atom selected from N, Ο and S and optionally 丨 or 2 Μ μ # d, and his nitrogen atom as a ring member 5- or 6-beyzepine wherein the heteroaryl ring is substituted for R4 μ + , with 1, 2, 3 or 4, preferably 1 or 2 substituents R. The 疋5- or 6-bey heteroaromatic groups are listed above. 149027.doc • 52· 201103430 In the heteroaryl ring enumerated above, it is preferred to extend a π-pyridyl group such as a 2,3-extended pyridyl group and a 2,4-extension. Bipyridyl, 2,5-extended pyridyl, 2,6-extension. Pyridyl, 3.4-extended pyridyl or 3,5-extended pyridyl; pyrimidinyl, such as 2,4-exipyridyl, 2,5-exipyrimidinyl, 4,5-exipyrimidinyl or 4,6 _ stretching pyrimidinyl; stretching furanyl 'such as 2,3 · 嗔 嗔 base, 2, 4 _ „ 夫 味, 2,5 _ 吱 吱 or 3.4- stretching furyl; thienyl, such as 2, 3_Thienyl, 2, thiophene, 2,5-thienyl or 3,4-extended phenyl; π-pyrylene, such as hydrazine, 2, pyrrolyl, 1,3-extension a thiol group, a 2,3-extended fluorenyl group, a 2,4-extended fluorenyl group, a 2,5-extended pyrrolyl group or a 3,4-extended pyrrolyl group; a pyrazolyl group such as a pyrazolyl group, 1, 4 - an extended carbazolyl group, a ten-saltyl group, a 3,4-extension, a oxazolyl group or a 3,5-exi-pyrazolyl group; an extended imidazolyl group such as i, an extended imidazolyl group, an M-extended imidazolyl group, 1' 5· stretching base, 2'4-extension D sitting base, 2,5_ stretching base or 4,5_extension imidazolyl H sitting group, such as 2,4-thiazole or 2,5• An oxazolyl group; an isoxazolyl group such as an M-exoisoxazole group or a 3,5-exoisoxazolyl group; a thiophene group; a group such as a 2,4-thiazole or a 2,5-thiazolyl group; Extending a thiazolyl group, such as a 3,4-extended (tetra) group or a 3,5-extension sigh; Sitting base, such as 1 2 - stretching, recording, or stretching, and specifying the position of the connection is understood to be the highest priority with respect to the ring heteroatom d• position. For example, in the case of In the ring of the ring hetero atom, the specified connection position is in the 坐· position m of the mono-ring hetero atom, and the specified connection position is relative to the two nitrogen ring atoms and the 2_ position, in the extension center 'Specified connection position relative to the position of the two nitrogen ring atoms and the position of the ^, in the exudation of the saliva group, the position of the connection position relative to the position of the oxygen ring atom and the position of the nitrogen ring atom 3-position, in the extension of the oxazolyl group Wherein, the specified position is relative to the position of the oxygen ring atom and the position of the nitrogen ring atom in the position of H9027.doc 53·201103430, in the thiazolyl group, the position of the crypto connection relative to the position of the sulfur ring atom and the nitrogen ring atom The position is in the extension. Sitting on the I towel, specifying the position of the connection relative to the position of the sulfur ring atom and the 2-position of the nitrogen ring atom, etc. More preferably, the pyridyl group, especially 2, 5 or 3' 6_Extension: a pyridyl group; a thienyl group, especially a 2,4- or 2,5-thenylene group; An oxazolyl group, especially a thiazole group or a 2,5-thiazole group. Even more preferably, it is a pyridine group, especially a 2,5• or 3,6-extended azide group; and a thienyl group, especially 2, 4_ or 2,5_Thienthylene, especially preferably an exifluoridyl group, especially a 2,5- or 3,6-exetidinyl group. In the case where Het is a 6-membered heteroaryl ring, Preferably, it has fluorene, fluorene, 2 or 3, more preferably 0, 1 or 2 substituents R4, wherein two or more substituents R4 may be the same or different. In the case where Het is a 5-membered heteroaryl ring It preferably has 0, 1 or 2 substituents R4, wherein the two substituent bases 4 may be the same or different. R4 may be attached via C- or Ν-, but is preferably attached to the c atom of Het. R4 is preferably selected from the group consisting of halogen, OH, SH'N02, CN, Ci_c4 alkyl, G-C4 halogen alkyl, Ci-C* methoxy-CVC4 alkyl, Ci-Czj alkoxy, c] C4 oxygenated -CVC4 alkoxy and C]-C: 4 halo alkoxy, more preferably selected from the group consisting of gas, gas, bromine, C-C4 alkyl, C丨-C4 haloalkyl, C丨-c4 alkoxy And 〇丨_(34 haloalkoxy) is even more preferably selected from the group consisting of fluorine, gas, bromine, CH3, CHF2, CF3, OCH3, OCHFA OCF3, especially preferably selected from the group consisting of fluorine, gas, and CH3, cf3 'och3 and OCF3 And especially selected from the group consisting of fluorine and gas. In particular, Het is selected from the group consisting of Het.l to Het.16, wherein # is the linkage to the fourth carbon atom (which has a ketal and a triazolylmethyl group). Point and * is the connection

t SI 149027.doc -54- 201103430 至基圑γ之連接點:t SI 149027.doc -54- 201103430 Connection point to base 圑:

Xr#Xr#

Het.2Het.2

ClCl

# F Het.3# F Het.3

##

Het.1 Het.4Het.1 Het.4

Het.11 Het.12 Het.13Het.11 Het.12 Het.13

Het.14Het.14

Het.15 Het.16 在上式之中,較佳為基團Het丨至Het丨〇。 基團-c(=〇)m _S(0)2R8中之汉8較佳選自Ci_C4烧基、 CVCd烷基、(^-(^烷氧基、Ci_Cd烷氧基、笨基、苯氧 基及NRl3Rl4,更佳選自CA烧基、CrC2齒烷基、Cl_C4 烧氧基、CVCd炫氧基&NRnRl4且甚至更佳選自CA烧 基、CVC4烷氧基&NRnRu。在基團_c卜〇)r8中,r8尤其 為匸心烧基,諸如甲基、乙基、丙基、異丙基、正丁 基、第二丁基、異丁基或第三丁基’較佳為曱基,或為 G-C4烷氧基,諸如甲氧基、乙氧基、丙氧基、異丙氧 基、正丁氧基、第二丁氧基、異丁氧基或第三丁氧基,較 佳為甲氧基,且更尤其為甲基,且在基團_s(〇)2R8中,γ 尤其為甲基。較佳地,R13為氫且RI4係選自氫、烷基 及苯基,較佳選自氫及Ci_C4烷基;或尺丨3及尺丨4皆為C】_C4 149027.doc -55- 201103430 烷基,較佳為甲基或乙基。 Μ較佳選自鹼金屬陽離子、鹼土金屬陽離子相等物、 Cu、Zn、Fe或Ni之陽離子相等物或式(NRaRbReRd)+之銨陽 離子,其中Ra、Rb、^及…中之一者為氫且Ra、Rb、^及 Rd中之三者彼此獨立地選自Ci_C|g烷基。更佳地,%係選 自L丨+、Na+、K+、〗/2Mg2+、Cu、Ζη、卜或恥之陽離子相等 物及式(NRaRbRCRY之銨陽離子,其十Ra、Rb、rc及Rd中 之一者為氫且V、R、^及…中之三者彼此獨立地選自 q-c〗。烧基。甚至更佳地,M係選自Na+、κ+、1/2心2+、 《Cu2、i/2Zn2+、1歲2+、_2+、三乙銨及三甲銨。 在式ΠΙ之基團中,變數較佳具有與在分子j之其餘部分 中相同之含義。因&,上文關於基團之較佳含義的隊述亦 適用於此部分。 R 較佳選自氫、〇^-(:4烷基、_C( = 〇)R8、s(〇)2r8、 -CN、Μ及式m之基團’其中R8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且M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。 R更佳選自氫、c〗-C4烷基、cvc:4烷基羰基、C]_C4烷氧 羰基、-CPCONCI^CVC^ 烷基、-C(=0)n(Ci_C4 烷基)2、Ci_ C4烷基磺醯基、CN、M及式m之基團,其中M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。詳言 之’R係選自氫、曱基、乙基、丙基、異丙基、甲基幾 基甲氧紅基、_C(=0)N(CH3)2、CN、μ及式III之基團, 其中Μ具有上述一般含義中之一纟’或尤其上述較佳含義 [ 149027.doc -56· 201103430 中之一者且較佳為驗金屬陽離子或% Cu2+®詳言之,r1為 氫、甲基、曱基羰基、曱氧羰基、Na+或式III之基團。 «^較佳選自氫、CVCm烷基、CVC4鹵烷基、苯基、苯 基-C丨-C4烷基、-C(=〇)R8及-S(0)2R8,其中R8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 地,Rla係選自氫、CVC4烷基、C,-C4鹵烷基、苯基、节 基、-C(=0)R8及-S(0)2R8,其中R8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,且更佳選自氫、 Ci-C4烷基、CVC4 _ 烷基、-C(=〇)R8及 _s(〇)2r8,其中 Rs 具有上述一般含義中之一者,或尤其上述較佳含義令之一 者洋5之’11為氫、C!-C4烧基’較佳為甲基或 -C(=〇)R8,更尤其為氫、Ci_C4烷基,較佳為甲基、甲基 羰基或甲氧羰基,甚至更尤其為氫或Ci_C4烷基,較佳為 曱基且尤其為氫。 γ較佳為〇。 A較佳為直鏈C:2或C3伸烷基橋,其中伸烷基橋之工或之個 氫原子可經1或2個取代基R5置換,其中各汉5獨立地選自 c】-c4烧基、Cl_C4_炫基、Ci_c^氧基、燒氧基 C4烷氧基及(^-<:4鹵烷氧基,且較佳選自曱基、乙基、甲 氧基乙氧基及曱氧基甲氧基,或連接於相鄰碳原子上的 兩個取代基R5連同其所連接之碳原子—起形成環戊基或環 己基環。更佳地,A為直鏈Q或C3伸烷基橋,其中伸烷基 橋之1個氫原子可經丨個取代基…置換,立 Λ ,、τ 钓 院 土。至更佳地’ A為直鏈〇2伸烧基橋,其中伸燒基橋之丄 I49027.doc -57- 201103430 個氮原子可經1個取代基r5置換,其中R5為〇^(:4烧基且較 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(o)m_Rl形成基『s(=〇)_Rl。若爪為2,兩個氧原子 較佳均經由雙鍵連接至硫原子上,由此基團·s(Q)m_Ri形成 基團_S(=〇)2_Rl。若4 3,則基團-s(o)m_Rl為基團 -S( = 0)2-0-R' 〇 m較佳為〇或2且更佳為〇。 在尤佳實把例中,在化合物工令,⑺為〇且^為Η(或另 外’在化合物II中’ Η)。 特定化合物Ι/ΙΙ為以下: 較佳化合物I及II之實例盔斗,τ , ^ 頁例為式L1至1.192及II.1至π.96之化 合物,其中變數具有以上给 、,口出之一般含義或尤其較佳含義 中之一者。較佳化合物之督 耳例為在以下表1至70992中所彙Het. 15 Het. 16 Among the above formulas, preferred groups are Het丨 to Het丨〇. The group 8 in the group -c(=〇)m _S(0)2R8 is preferably selected from the group consisting of Ci_C4 alkyl, CVCd alkyl, (^-(^ alkoxy, Ci_Cd alkoxy, stupyl, phenoxy) And NRl3Rl4, more preferably selected from the group consisting of CA alkyl, CrC2 dentate, Cl_C4 alkoxy, CVCd methoxy & NRnR14 and even more preferably selected from the group consisting of CA alkyl, CVC4 alkoxy & NRnRu. In the case of r8, r8 is especially a fluorene group, such as methyl, ethyl, propyl, isopropyl, n-butyl, t-butyl, isobutyl or t-butyl' is preferably Indenyl, or a G-C4 alkoxy group such as methoxy, ethoxy, propoxy, isopropoxy, n-butoxy, second butoxy, isobutoxy or tert-butoxy a group, preferably a methoxy group, and more particularly a methyl group, and in the group _s(〇)2R8, γ is especially a methyl group. Preferably, R13 is hydrogen and RI4 is selected from hydrogen, alkyl. And phenyl, preferably selected from hydrogen and Ci_C4 alkyl; or both 丨3 and 丨4 are C] _C4 149027.doc -55- 201103430 alkyl, preferably methyl or ethyl. From an alkali metal cation, an alkaline earth metal cation equivalent, a cation equivalent of Cu, Zn, Fe or Ni or a formula (N An ammonium cation of RaRbReRd), wherein one of Ra, Rb, ^ and ... is hydrogen and three of Ra, Rb, ^ and Rd are independently selected from each other from Ci_C|g alkyl. More preferably, % is Equivalent from L丨+, Na+, K+, 〖/2Mg2+, Cu, Ζη, 卜 or shame, and an ammonium cation of the formula (NRaRbRCRY, one of ten Ra, Rb, rc and Rd is hydrogen and V Three of R, ^ and ... are independently selected from qc. Burning groups. Even more preferably, M is selected from the group consisting of Na+, κ+, 1/2 core 2+, "Cu2, i/2Zn2+, 1 2+, _2+, triethylammonium and trimethylammonium. In the group of the formula, the variable preferably has the same meaning as in the rest of the molecule j. Because &, the above meanings about the group The same applies to this part. R is preferably selected from the group consisting of hydrogen, 〇^-(:4 alkyl, _C(= 〇)R8, s(〇)2r8, -CN, Μ and the group of formula m. R8 has one of the above general meanings, or particularly one of the above preferred meanings, and M has one of the above general meanings, or particularly one of the above preferred meanings. R is more preferably selected from the group consisting of hydrogen and c. 〖-C4 alkyl, cvc: 4 alkyl carbonyl, C] _C4 Oxycarbonyl, -CPCONCI^CVC^alkyl, -C(=0)n(Ci_C4 alkyl)2, Ci_C4 alkylsulfonyl, CN, M and a group of formula m, wherein M has the above general meaning One of, or especially one of the above preferred meanings. In detail, 'R is selected from the group consisting of hydrogen, mercapto, ethyl, propyl, isopropyl, methyl methoxy red, _C (= 0) N(CH3)2, CN, μ and a group of the formula III, wherein hydrazine has one of the above general meanings ′ or particularly one of the above preferred meanings [149027.doc-56·201103430 and preferably For the purpose of examining metal cations or % Cu2+®, r1 is hydrogen, methyl, decylcarbonyl, oxime carbonyl, Na+ or a group of formula III. «^ is preferably selected from the group consisting of hydrogen, CVCm alkyl, CVC4 haloalkyl, phenyl, phenyl-C丨-C4 alkyl, -C(=〇)R8 and -S(0)2R8, wherein R8 has the above general One of the meanings' or one of the above preferred meanings. More preferably, Rla is selected from the group consisting of hydrogen, CVC4 alkyl, C, -C4 haloalkyl, phenyl, benzyl, -C(=0)R8 and -S(0)2R8, wherein R8 has the above general meaning One, or especially one of the above preferred meanings, and more preferably selected from the group consisting of hydrogen, Ci-C4 alkyl, CVC4_alkyl, -C(=〇)R8 and _s(〇)2r8, wherein Rs One of the above general meanings, or especially one of the above preferred meanings, is that '11 is hydrogen, C!-C4 alkyl' is preferably methyl or -C(=〇)R8, more particularly It is hydrogen, Ci_C4 alkyl, preferably methyl, methylcarbonyl or methoxycarbonyl, even more particularly hydrogen or Ci_C4 alkyl, preferably fluorenyl and especially hydrogen. γ is preferably 〇. A is preferably a linear C:2 or C3 alkylene bridge wherein the alkylene or one of the hydrogen atoms may be replaced by one or two substituents R5, wherein each Han 5 is independently selected from c]- C4 alkyl, Cl_C4_Hyun, Ci_coxy, alkoxy C4 alkoxy and (^-<:4 haloalkoxy, and preferably selected from decyl, ethyl, methoxyethoxy And a methoxymethoxy group, or two substituents R5 attached to an adjacent carbon atom, together with the carbon atom to which they are attached, form a cyclopentyl or cyclohexyl ring. More preferably, A is a linear Q. Or a C3 alkylene bridge in which one hydrogen atom of the alkylene bridge can be replaced by a substituent, a crucible, a τ fishing ground soil. More preferably, the 'A is a linear 〇2 extension base bridge , wherein the nitrogen atom can be replaced by one substituent r5, wherein R5 is 〇^(:4 alkyl and preferably methyl. In detail, '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(o)m_Rl forms a group "s(=〇)_Rl. If the claw is 2 Preferably, both oxygen atoms are attached to the sulfur atom via a double bond, whereby the group s(Q)m_ Ri forms a group _S(=〇)2_Rl. If 4 3, the group -s(o)m_Rl is a group -S(=0)2-0-R' 〇m is preferably 〇 or 2 and more In the example of the compound, in the compound order, (7) is 〇 and ^ is Η (or otherwise 'in compound II' Η). The specific compound Ι / ΙΙ is as follows: Preferred compounds I and II Examples of helmets, τ , ^ The examples are compounds of the formulae L1 to 1.192 and II.1 to π.96, wherein the variables have one of the above, or the general meaning of the mouth, or particularly preferred meaning. Examples of compounds are summarized in Tables 1 to 70992 below.

編之個別化合物。此外,I s下針對表中之個別變數所述之 含義本身(不依賴於提及該蓉與 X寺k數之組合)為相關取代基之 一尤佳實施例。Edited individual compounds. Furthermore, the meaning of I s for individual variables in the table itself (not dependent on the combination of the k and the number of k-numbers) is a preferred embodiment of the relevant substituents.

J49027.doc [S3: -58- 201103430J49027.doc [S3: -58- 201103430

149027.doc -59 201103430149027.doc -59 201103430

s—sS-s

R23 R22R23 R22

(1.53)(1.53)

R23 Ri2R23 Ri2

OMeOMe

[SI 149027.doc -60 201103430[SI 149027.doc -60 201103430

149027.doc -61 · 201103430149027.doc -61 · 201103430

R21R21

(1.70)(1.70)

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(1.92)(1.92)

m 149027.doc •64- 201103430m 149027.doc •64- 201103430

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[s] 149027.doc -66- 201103430[s] 149027.doc -66- 201103430

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MeOMeO

OMeOMe

[:s ] 149027.doc • 68 - 201103430[:s ] 149027.doc • 68 - 201103430

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c 201103430c 201103430

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149027.doc 73- 201103430149027.doc 73- 201103430

表1 式I · 1之化合物 之組合在各情況 之基團且R1為η 表2 其中化合物之R21、R22 了對應於上述表Α之一列 、R23、R24及 R25 ,Het 為式 Het. 1 式i.i之化合物’其中化合物之r2i、r22 之組合在各情況下對應於上述表A之一列 之基團且R1為曱基 表3 、R23、R24及 R25 ,Het 為式 Het.1 式1.1之化合物,其中化合物之r21、r22、r23、r24及r25 H在各情況下對應於上述表A之-列,Het為式Het. 1 之基團且R1為乙基 表4 149027.docTable 1 Combination of the compounds of formula I · 1 in each case and R1 is η. Table 2 wherein R21 and R22 of the compound correspond to one of the above-mentioned tables, R23, R24 and R25, and Het is a formula of Het. The compound of ii wherein the combination of r2i and r22 of the compound corresponds in each case to the group listed in the above Table A and R1 is a fluorenyl group, 3, R23, R24 and R25, and Het is a compound of the formula Het.1. Wherein the compounds r21, r22, r23, r24 and r25H correspond in each case to the column of the above Table A, Het is a group of the formula Het. 1 and R1 is an ethyl group 4 149027.doc

t SI -74- 201103430 、R23、R24及 R25 ,Het 為式 Het. 1 式i. 1之化合物,甘^ 其中化合物之r21、r2 之組合在各情況下 于應於上述表A之一歹 之基團且R1為丙基 表5 其中化合物之R2 1、R 下對應於上述表Α之一 丙基 式Ι·1之化合物 之組合在各情況 之基團且汉】為異 表6 22、R23、R24及 R25 列,Het為式Het. 1 式I · 1之化合物 之組合在各情況 之基團且R1為正 表7 ’其中化合物之R21、r22 下對應於上述表A之一列 丁基 、R23 ' R24及 R25 ,Het 為式 Het. 1 式1.1之化合物,其中 之組合在各情況下對應 之基團且為第二丁基 表8 化合物之R21、R22、R23、R24&R25 於上述表A之一列,Het為式Het. 1 式L1之化合物,其中化合物之R2〗、R22 之組合在各情況下對應於上述表A之一列 之基團且R1為異丁基 表9 、R23、R24及 R25 ,Het為式 Het.1 式1.1之化合物,其中化合物之r21、r22、r23、r24及r25 之..且σ在各情況下對應於上述表a之一列,為式^ 之基團且R1為第三丁基 表10 149027.doc -75· 201103430 式L1之化合物,其中化合物之尺21、R22、R23、1124及1125 之組合在各情況下對應於上述表A之一列,Het為式Het.l 之基團且R1為苯基 表11 式L1之化合物,其中化合物之尺21、R22、r23、尺24及r25 之組合在各情況下對應於上述表八之一列,Het為式Het l 之基團且R1為苄基 表12 式L1之化合物,其中化合物之R21、R22、R23、R24&R25 之組合在各情況下對應於上述表八之一列,Het為式Het」 之基團且R1為Li + 表13 式I . 1之化合物,其中化合物之r21、r22、r23、r24及r25 之組合在各情況下對應於上述表八之一列,Het為式Het」 之基團且Ri為Na+ 表14 式1.1之化合物,其中化合物之r21、r22、r23、r24及r25 之組合在各情況下對應於上述表A之一列,Het為式Hetl 之基團且R1為K+ 表15 式L 1之化合物’其中化合物之r2i、r22、r23、r24及r25 之組σ在各情況下對應於上述表八之一列,Het為式^ 之基團且尺]為i/2Mg2+ 表16t SI -74- 201103430 , R23, R24 and R25 , Het is a compound of the formula Het. 1 , formula i. 1 , wherein the combination of the compounds r21 and r2 is in each case in one of the above Table A a group and R1 is a propyl group 5 wherein a compound of R2 1 , R corresponds to a combination of the above-mentioned one of the compounds of the formula propyl group 1 in each case, and the group is a hetero-table 6 22, R 23 , R24 and R25, Het is a group of the formula Het. 1 compound of formula I · 1 in each case and R1 is a positive table 7 'where the compound R21, r22 corresponds to one of the above table A, butyl, R23 ' R24 and R25 , Het are a compound of the formula Het. 1 formula 1.1, wherein the combination is in each case the corresponding group and is the second butyl group 8 compound of R21, R22, R23, R24 & R25 in the above table In one of the columns A, Het is a compound of the formula H1. Formula L1, wherein the combination of R2 and R22 of the compound corresponds in each case to the group listed in the above Table A and R1 is isobutyl. Tables 9, R23, R24 And R25, Het is a compound of the formula Het.1, wherein the compound is r21, r22, r23, r24 and r25. and σ is in each case Corresponding to one of the above Tables a, is a group of the formula ^ and R1 is a compound of the third butyl group 10 149027.doc -75 · 201103430 Formula L1, wherein the combination of the compound of the ruler 21, R22, R23, 1124 and 1125 In each case corresponding to one of the above Table A, Het is a group of the formula Het.l and R1 is a compound of the formula L1 of the phenyl group, wherein the combination of the ruler 21, R22, r23, ruler 24 and r25 of the compound is In each case, corresponding to one of the above Tables 8, Het is a group of the formula Het l and R1 is a compound of the formula benzyl 12, wherein the combination of the compounds R21, R22, R23, R24 & R25 corresponds in each case. In one of the above Tables 8, Het is a group of the formula Het" and R1 is a compound of the formula I.1, wherein the combination of the compounds r21, r22, r23, r24 and r25 corresponds in each case to the above In one of Table 8, Het is a group of the formula Het" and Ri is Na + a compound of the formula 1.1 in Table 14, wherein the combination of the compounds r21, r22, r23, r24 and r25 corresponds in each case to one of the above Table A, Het is a group of the formula Hetl and R1 is K+. Table 15 is a compound of the formula L1 wherein the compound is r2i, r22, r23 r24 and r25 of σ groups in each case one table corresponding to the eight, Het is a group of the formula ^ and feet] of i / 2Mg2 + Table 16

[SI 149027.doc •76· 201103430 式ι·ι之化合物,其中化合物之尺2丨、R22、 之組合在各情況下對應於上述表A之一列 之基團且以為l/2Cu2 + 表17 - 式L1之化合物,其中化合物之R21、R22、 . 之組合在各情況下對應於上述表A之一列 之基團且以為ι/2Ζη2 + 表18 式1,1之化合物,其中化合物之R21、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為i/2Fe2+ 表19 式hl之化合物,其中化合物之R21、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為i/2Ni2+ 表20 式L1之化合物,其中化合物之R21、R22、 之組合在各情況下對應於上述表A之一列 之基團且R丨為NH(CH3)3 + - 表21 式L1之化合物,其中化合物之R2I、R22、 之組合在各情況下對應於上述表A之一列: 之基團且R1為nh(c2h5)3+ 表22 149027.doc 'R23、R24及 R25 ,Het為式 Het. 1 R23、R24及 R25 ,Het為式 Het. 1 R23、R24及 R25 ,Het為式 Het.1 R23、R24及 R25 ,Het為式 Het.1 R23、R24及 R25 ,Het 為式 Het.1 R23、R24及 R25 Het為式 Het.1 77· 201103430 式I. 1之化合物,其中化合物之R2!、R22、 之組合在各情況下對應於上述表A之一列, 之基團且 R1 為 NH(CH2CH2CH2)3+ 表23 式1.1之化合物’其中化合物之R2丨、R22、 之組合在各情況下對應於上述表A之一列 之基團且 R1 為 NH(CH(CH3)2)3+ 表24 式1.1之化合物,其中化合物之尺2丨、R22、 之組合在各情況下對應於上述表A之一列 之基團且 R1 為 ΝΗ((:Η2(:Η2(:Η2(:ϋ2)3 + 表25 式Ι·1之化合物’其中化合物之R2!、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為甲基羰基 表26 式1.1之化合物,其中化合物之尺2丨、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為乙基羰基 表27 式1.1之化合物,其中化合物之尺2丨、R22、 之组合在各情況下對應於上述表A之一列 之基團且R1為丙基羰基 表28 149027.doc R23、R24及 R25 Het 為式 Het. 1 R23、R24及 R25 ,Het 為式 Het.1 R23、R24及 R25 * Het 為式 Het. 1 R23、R24及 R25 ,Het為式 Het.1 R23、R24及 R25 ,Het為式 Het.1 R23、R24及 R25 ,Het為式 Het.1 [S] •78· 式i. 1之化合物 之組合在各情況 之基團且R1為異 表29 201103430 ,其中化合物之R21、r22 下對應於上述表A之一列 丙基羰基 式1.1之化合物,其十化合物之汉21、r22 之组合在各情況下對應於上述表A之-列 之基團且R1為甲氧羰基 表30 式L1之化合物,其中化合物之r2i、R22 之組合在各情況下對應於上述表A之一列 之基團且R1為乙氧羰基 表31 式1.1之化合物,其中化合物之尺2,、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為丙氧羰基 表32 式1.1之化合物,其中化合物之尺21、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為異丙氧羰基 表33 式Ι·1之化合物,其巾化合物之R21、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為苯氧羰基 表34 .R23、R24及 R25 ,Het為式 Het.l ‘ R23、R24及 R25 ,Het為式 Het.l R23、R24及 R25 ,Het為式 Het.l R23、R24及 R25 ,Het為式 Het. 1 R23、R24及 R25 ,Het 為式 Het. 1 R23、R24及 R25 ,Het為式 Het.l 149027.doc •79· 201103430 式之化合物,其中化合物之r21、r22、r23、r24及r25 之、,且0在各情況下對應於上述表A之一列,Het為式Het.l 之基團且R1為甲基胺基羰基 表35 式L1之化合物’其中化合物之R21、R22、R23、R24及R25 之組合在各情況下對應於上述表A之-列,Het為式Het.l 之基團且汉丨為乙基胺基羰基 表3 6 式L1之化合物,其中化合物之R21、R22、R23、R24及R25 之組合在各情況下對應於上述表A之-列,Het為式Het.l 之基團且R1為丙基胺基羰基 表37 式L1之化合物,其中化合物之R21、R22、R23、R24及R25 之組合在各情況下對應於上述表A之一列,Het為式Het.l 之基團且R1為異丙基胺基羰基 表38 式M之化合物’其中化合物之R21、R22、R23、R24及R25 之組合在各情況下對應於上述表A之一列,Het為式Het.l 之基團且R1為苯基胺基羰基 表39 式L1之化合物’其中化合物之R21、R22、R23、R24及R25 之組0在各情況下對應於上述表A之一列,Het為式Het.l 之基團且R丨為曱磺醯基 表40[SI 149027.doc • 76· 201103430 A compound of the formula ι·ι, wherein the combination of the compounds of the formula 2丨, R22, in each case corresponds to the group listed in the above Table A and is considered to be l/2Cu2 + Table 17 - A compound of the formula L1, wherein the combination of the compounds R21, R22, . . . corresponds in each case to the group listed in the above Table A and is considered to be ι/2Ζη2 + Table 18 Formula 1,1, wherein the compound R21, R22 And a combination of R21 in the present case corresponding to the group of the above Table A and R1 is i/2Fe2+ wherein the combination of R21, R22, in each case corresponds to one of the above Table A And R1 is a compound of formula L1, wherein the combination of R21, R22 of the compound corresponds in each case to the group of one of the above Table A and R is NH(CH3)3 + - TABLE 21 A compound of the formula L1 wherein the combination of R2I, R22 of the compound corresponds in each case to the group of the above Table A: R1 is nh(c2h5)3+ Table 22 149027.doc 'R23, R24 and R25, Het is of the formula Het. 1 R23, R24 and R25, Het is of the formula Het. 1 R23, R24 and R25, Het is the formula Het.1 R2 3, R24 and R25, Het is a formula Het.1 R23, R24 and R25, Het is a formula Het.1 R23, R24 and R25 Het is a compound of the formula Het.1 77· 201103430 Formula I. 1, wherein the compound R2! The combination of R22, in each case corresponds to a group of the above Table A, and R1 is NH(CH2CH2CH2)3+ Table 23 Compound of formula 1.1 wherein the combination of compounds R2丨, R22, in each case Corresponding to the group listed in the above Table A and R1 is NH(CH(CH3)2)3+, the compound of the formula 1.1, wherein the combination of the ruler 2丨, R22 of the compound corresponds in each case to the above Table A One of the groups and R1 is ΝΗ((:Η2(:Η2(:Η2(:ϋ2)3 + Table 25 Formula Ι·1 of the compound' wherein the combination of the compound R2!, R22, in each case corresponds to a group of the above Table A and R1 is a methylcarbonyl group of the compound of the formula 1.1, wherein the combination of the compounds of the formula 2, R22, in each case corresponds to the group listed in the above Table A and R1 is B. The compound of the formula 1.1 wherein the combination of the ruthenium 2, R22 of the compound corresponds in each case to the group of one of the above Table A and R1 is propylcarbonyl. Table 28 149027.doc R23, R24 and R25 Het are of the formula Het. 1 R23, R24 and R25, Het is of the formula Het.1 R23, R24 and R25 * Het is a formula Het. 1 R23, R24 and R25 Het is of the formula Het.1 R23, R24 and R25, Het is the formula Het.1 R23, R24 and R25, and Het is the formula Het.1 [S] •78· The combination of the compounds of formula i.1 is based on each case. And R1 is a different form 29 201103430, wherein the compound of R21 and r22 corresponds to a compound of the above formula A, which is a compound of the formula propyl group 1.1, and the combination of the ten compounds of the compound 21 and r22 corresponds in each case to the above table A. a group of the formula and R1 is a methoxycarbonyl group of the compound of the formula L1, wherein the combination of the compounds r2i, R22 corresponds in each case to the group listed in the above Table A and R1 is an ethoxycarbonyl group 31 The compound of 1.1, wherein the combination of the ruler 2, R22 of the compound corresponds in each case to the group listed in the above Table A and R1 is a compound of the formula 1.1 of the propoxycarbonyl group, wherein the compound has a size of 21, R22, The combination in each case corresponds to the group listed in the above Table A and R1 is a combination of isopropoxycarbonyl table 33 Ι·1 The combination of R21 and R22 of the towel compound corresponds in each case to the group listed in the above Table A and R1 is a phenoxycarbonyl group 34. R23, R24 and R25, and Het is a formula Het.l 'R23, R24 and R25, Het is Het.l R23, R24 and R25, Het is Het.l R23, R24 and R25, Het is Het. 1 R23, R24 and R25, Het is Het. 1 R23, R24 and R25, Het is a compound of the formula Het.l 149027.doc •79·201103430, wherein the compound is a combination of r21, r22, r23, r24 and r25, and 0 corresponds in each case to one of the above Table A, Het is a group of the formula Het.l and R1 is a methylaminocarbonyl group. The compound of the formula L1 wherein the combination of R21, R22, R23, R24 and R25 of the compound corresponds in each case to the column of the above Table A, Het Is a group of the formula Het.l and the oxime is an ethylaminocarbonyl group of the compound of the formula L1, wherein the combination of the compounds R21, R22, R23, R24 and R25 corresponds in each case to the above Table A - Column, Het is a group of the formula Het.l and R1 is a propylaminocarbonyl group of the compound of the formula L1, wherein the combination of the compound of R21, R22, R23, R24 and R25 is in each case. In the case of one of the above Table A, Het is a group of the formula Het.1 and R1 is an isopropylaminocarbonyl group. The compound of the formula M wherein the compound of the combination of R21, R22, R23, R24 and R25 is In each case, corresponding to one of the above Table A, Het is a group of the formula Het.1 and R1 is a phenylaminocarbonyl group. The compound of the formula L1 wherein the compound is a group of R21, R22, R23, R24 and R25. In each case corresponding to one of the above Table A, Het is a group of the formula Het.l and R is a sulfonyl sulfhydryl group 40

E SI 149027.doc •80· 201103430 式L1之化合物,其中化合物之R21、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為乙磺醯基 表41 式L1之化合物,其中化合物之R21、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為丙績醯基 表42 式1.1之化合物,其中化合物之R2〗、r22、 之組合在各情況下對應於上述表A之一列 之基團且R1為異丙確醯基 表43 式L1之化合物,其中化合物之R21、R22、 之組合在各情況下對應於上述表a之一列 之基團且R1為苯磺醯基 表44 式1.1之化合物,其中化合物之rZ1、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為甲氧磺醯基 表45 式1.1之化合物’其中化合物之rS1、R22、 之組合在各情況下對應於上述表A之一列 之基團且R1為乙氧磺醯基 表46 149027.doc R23、R24及 R25 ,Het為式 Het. 1 R23、R24及 R25 ,Het 為式 Het.1 R23、R24及 R25 ,Het為式 Het. 1 R23、R24及 R25 ,Het 為式 Het. 1 R23、R24及 R25 ,Het為式 Het. 1 R23、R24及 R25 ^ Het 為式 Het. 1 •81 - 201103430 式L1之化合物,其中化合物之R21、 之組合在各情況下對應於上述表八之-之基團且R1為丙氧磺醯基 表47 式L1之化合物,其中化合物之R21、 之組合在各情況下對應於上述表A之- 之基團且R1為異丙氧磺醯基 表48 式1.1之化合物,其中化合物之R2丨、 之組合在各情況下對應於上述表A之· 之基團且R為苯氧石黃酿基 表49 式之化合物’其中化合物之R21、 之組合在各情況下對應於上述表A之 之基團且R1為CN 表50至98 式L1之化合物,其中化合物之尺21、 之組合在各情況下對應於表A之一列, 任一者中所定義且Het為式Het.2之基團 表99至147 式之化合物,其中化合物之R2〗、 之組合在各情況下對應於表A之一列, 任一者中所定義且Het為式Het.3之基團 表148至196 149027.doc R22、R23、R24及 R25 -列,Het 為式 Het. 1 R22、R23、R24及 R25 -列,Het 為式 Het. 1 R22、R23、R24及 R25 -列,Het 為式 Het. 1 R22、R23、R24及 R25 -列,Het為式 Het. 1 R22、R23、R24及 R25 R1係如在表1至49之 r22、R23、R24及 R25 Rl係如在表1至49之 [.S] -82- 201103430 式1.1之化合物,其中化合物之R21、R22、R23、R24及r25 之組合在各情況下對應於表A之一列,R1係如在表1至49之 任一者中所定義且Het為式Het.4之基團 表197至245 式Ι·1之化合物,其中化合物之R21、R22、R23、汉24及尺25 之組合在各情況下對應於表Α之一列,R1係如在表1至49之 任一者中所定義且Het為式Het.5之基團 表246至294 式I. 1之化合物,其中化合物之R21、R22、R23、R24及R25 之組合在各情況下對應於表A之一列,R1係如在表1至49之 任一者中所定義且Het為式Het.6之基團 表295至343 式之化合物’其中化合物之R21、R22、R23 '汉以及^^ 之組合在各情況下對應於表A之一列,R1係如在表1至49之 任一者中所定義且Het為式Het.7之基團 表344至392 式L 1之化合物,其中化合物之R21、R22、r23、r24及r25 之組合在各情況下對應於表a之一列,R1係如在表1至49之 任一者中所定義且Het為式Het.8之基團 表393至441 式1.1之化合物,其中化合物之R21、R22、r23、反24及尺25 之組合在各情況下對應於表A之一列,R1係如在表i至49之 任一者中所定義且Het為式Het.9之基團 表442至490 149027.doc -83- 201103430 式1.1之化合物,其中化合物之、R22、 κ 、R24及 R25 之組合在各情況下對應於表A之一列,R1係如在表1至49之 任一者中所定義且Het為式Het.10之基團 表491至539 式L1之化合物,其中化合物之R21、R22、R23、r24及r25 之組合在各情況下對應於表A之一列,R1係如在表丨至49之 任一者中所定義且Het為式Het. 11之基團 表540至588 式1.1之化合物,其中化合物之尺21、R22、r23、r24及r25 之組合在各情況下對應於表A之一列,係如在表!至49之 任一者中所定義且Het為式Het. 12之基團 表589至637 式Ι·1之化合物,其中化合物之r21、r22、r23、尺24及尺25 之組合在各情況下對應於表A之一列,R1係如在表1至49之 任一者中所定義且Het為式Het. 13之基團 表638至686 式I. 1之化合物,其中化合物之r21、r22、r23、r24及尺25 之組合在各情況下對應於表A之一列,r1係如在表1至49之 任一者中所定義且Het為式Het. 14之基團 表687至735 式L1之化合物’其中化合物之R21、r22、R23、r24及只25 之組合在各情況下對應於表A之一列,R1係如在表1至49之 任一者中所定義且Het為式Het.l 5之基團 表736至784 149027.doc -84 - 201103430 式L1之化合物,其中化合物之R21、R22、R23、r24及r25 之組合在各情況下對應於表A之一列,Ri係如在表丨至49之 任一者中所定義且Het為式Het_16之基團 表 785至1568 式1.2之化合物’其中化合物之R2!、r22、r23、尺24及尺25 之組合在各情況下對應於表A之一列且R1與Het之組合係如 在表1至784之任一者中所定義 表1569至2352 式1.3之化合物,其中化合物之、r22、r23、尺24及尺25 之組合在各情況下對應於表A之一列且R1與H e t之組合係如 在表1至784之任一者中所定義 表2353至3136 式1.4之化合物,其中化合物之r2i、r22、r23、r24及r25 之組合在各情況下對應於表A之一列且R1與Het之組合係如 在表1至784之任一者中所定義 表3137至3920 式1.5之化合物,其中化合物之r21、r22、r23、尺24及尺25 之組合在各情況下對應於表a之一列且R1與Het之組合係如 在表1至784之任一者中所定義 表3921至4704 式1.6之化合物,其中化合物之r2i、R22、r23、r24及r25 之組合在各情況下對應於表A之一列且ri與Het之組合係如 在表1至784之任一者中所定義 表4705至5488 149027.doc -85- 201103430 式L7之化合物,其中化合物之R2〗、R22、R23、R24及r25 之組合在各情況下對應於表A之—列且Rl|%Het之組合係如 在表1至784之任一者中所定義 表 5489至 6272 式L8之化合物,其中化合物之R21、R22、RU、R24及r25 之組合在各情況下對應於表以—列且Rl^et之組合係如 在表1至784之任一者中所定義 表 6273至 7056 式1.9之化合物,其中化合物之r21、r22、r23、r24及 之組合在各情況下對應於表人之一列且之組合係如 在表1至784之任一者中所定義 表7057至7840 式1.10之化合物,其中化合物之尺2丨、r22、r23、r24及 R25之組合在各情況下對應於表A之一列且Ri與Het之組合 係如在表1至784之任一者中所定義 表7841至8624 式Ι.Π之化合物,其中化合物之尺2丨、R22、r23、r24及 R25之組合在各情況下對應於表A之一列且Ri與Het之組合 係如在表1至784之任一者中所定義 表 8625至 9408 式1.12之化合物,其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表八之一列且之組合 係如在表1至784之任一者中所定義 表 9409至10192 149027.docE SI 149027.doc • 80· 201103430 A compound of the formula L1, wherein the combination of the compounds R21, R22, in each case corresponds to the group listed in the above Table A and R1 is a compound of the formula E1. Wherein the combination of R21 and R22 of the compound corresponds in each case to the group listed in the above Table A and R1 is a compound of the formula 1.4 in the formula 1.4, wherein the combination of the compound R2, r22, In the case of a group corresponding to one of the above Table A and R1 is a compound of the formula L1, wherein the combination of R21, R22 of the compound corresponds in each case to the group of one of the above Tables a. And R1 is a compound of the formula 1-1, wherein the combination of the compounds rZ1, R22, in each case corresponds to a group of the above Table A and R1 is a methoxysulfonyl group. The compound 'wherein the combination of the compounds rS1, R22, in each case corresponds to the group listed in the above Table A and R1 is ethoxysulfonyl group 46 149027.doc R23, R24 and R25, and Het is a formula Het. 1 R23, R24 and R25, Het is the formula Het.1 R23, R24 and R25, Het is Het. 1 R23, R24 and R25, Het is a formula Het. 1 R23, R24 and R25, Het is a formula Het. 1 R23, R24 and R25 ^ Het is a formula Het. 1 •81 - 201103430 A compound of the formula L1, wherein the compound The combination of R21, in each case corresponds to the group of the above Table 8 and R1 is a compound of the formula L1 of the propoxysulfonyl group, wherein the combination of the compound R21, in each case corresponds to the above Table A a group of - and R1 is isopropoxysulfonyl. The compound of formula 1.1 wherein the combination of R2, in each case corresponds to the group of Table A above and R is phenoxy yellow. The compound of the formula 49 wherein R21 of the compound, in each case corresponds to the group of the above Table A, and R1 is a compound of the formula 50 to 98, wherein the compound of the compound 21 is in the combination of In each case corresponds to a column of Table A, a compound of the formulae 99 to 147 as defined in any of the formulas and Het is a group of the formula Het. 2, wherein the combination of the compounds R2, in each case corresponds to Table A One of the columns, defined in either of them, and Het is a group of the formula Het. 3, Tables 148 to 196 149027.doc R22, R23 , R24 and R25 - columns, Het is a formula Het. 1 R22, R23, R24 and R25 - columns, Het is a formula Het. 1 R22, R23, R24 and R25 - columns, Het is a formula Het. 1 R22, R23, R24 And R25-column, Het is of the formula Het. 1 R22, R23, R24 and R25 R1 are as shown in Tables 1 to 49, r22, R23, R24 and R25 Rl are as shown in Tables 1 to 49 [.S] -82- 201103430 A compound of formula 1.1 wherein the combination of R21, R22, R23, R24 and r25 of the compound corresponds in each case to one of the columns of Table A, and R1 is as defined in any of Tables 1 to 49 and Het is a formula Groups of Het. 4 Tables 197 to 245 Compounds of the formula ,·1, wherein the combination of the compounds R21, R22, R23, Han 24 and Ruler 25 corresponds in each case to one of the columns, and R1 is as shown in Table 1. A compound of the formula I wherein the Het is a group of the formula Het. 5, wherein the combination of R21, R22, R23, R24 and R25 of the compound corresponds in each case to In a column of Table A, R1 is as defined in any one of Tables 1 to 49 and Het is a group of the formula Het. 6 in the compounds of the formulae 295 to 343, wherein the compound R21, R22, R23 'han and ^ ^ The combination is in each case In the column of Table A, R1 is as defined in any one of Tables 1 to 49 and Het is a compound of the formulae 344 to 392 of the formula Het. 7 wherein R21, R22, r23, The combination of r24 and r25 corresponds in each case to one of the columns of Table a, R1 is as defined in any of Tables 1 to 49 and Het is a compound of the formulae 393 to 441 of the formula Het. Wherein the combination of R21, R22, r23, trans 24 and ruler 25 of the compound corresponds in each case to one of the columns of Table A, R1 is as defined in any of Tables i to 49 and Het is of the formula Het. Groups 442 to 490 149027.doc -83 - 201103430 Compounds of formula 1.1, wherein the combination of compounds, R22, κ, R24 and R25 corresponds in each case to one of Table A, and R1 is as in Tables 1 to 49. A compound of the formula L1, R22, R23, r24 and r25, as defined in any of the formulas, wherein Het is a group of the formula Het. 10, wherein the combination of R21, R22, R23, r24 and r25 of the compound corresponds in each case to one of the columns of Table A. R1 is a compound as defined in any one of Tables to 49 and Het is a group of formulas 540 to 588 of formula Het. 11 wherein the compound is 21, R22, r23 r24 and r25 of the composition in each case corresponds to one row in Table A, lines as shown in Table! a compound of the formula 589 to 637 of the formula Het. 12, wherein the combination of r21, r22, r23, ruler 24 and ruler 25 of the compound is in each case Corresponding to one of the columns of Table A, R1 is as defined in any one of Tables 1 to 49 and Het is a group of the formula Het. 13 in Tables 638 to 686. The compound of the formula I.1, wherein the compound is r21, r22, The combination of r23, r24 and ruler 25 corresponds in each case to one of the columns of Table A, r1 is as defined in any of Tables 1 to 49 and Het is a group of the formula Het. 14 Tables 687 to 735 Formula L1 The compound 'wherein the combination of R21, r22, R23, r24 and only 25 of the compound corresponds in each case to one of the columns of Table A, R1 is as defined in any of Tables 1 to 49 and Het is of the formula Het. The group of formula L1, wherein the combination of R21, R22, R23, r24 and r25 of the compound corresponds in each case to one of the tables A, and Ri is as in the case of Table 736 to 784 149027.doc -84 - 201103430 Groups 785 to 1568 of the formula Het_16, which are defined in any one of the above-mentioned, and wherein Het is a compound of the formula Het_16, wherein the compound is R2!, r22, r23, ruler 24 and ruler 25 A combination of R1 and Het in each case, and a compound of formula 1.31 to 2352, as defined in any of Tables 1 to 784, wherein the compound, r22, r23, rule 24 And the combination of the ruler 25 corresponds in each case to one of the columns of Table A and the combination of R1 and H et is a compound of the formula 1.43 to 3136 of the formula 1.4 as defined in any one of Tables 1 to 784, wherein the compound r2i, The combination of r22, r23, r24 and r25 corresponds in each case to one of the columns of Table A and the combination of R1 and Het is a compound of the formula 1.51 to 3920, as defined in any of Tables 1 to 784, wherein the compound The combination of r21, r22, r23, ruler 24 and ruler 25 corresponds in each case to one of the columns of Table a and the combination of R1 and Het is as defined in any of Tables 1 to 784, Tables 3921 to 4704, Equation 1.6 a compound wherein the combination of the compounds r2i, R22, r23, r24 and r25 corresponds in each case to one of the columns of Table A and the combination of ri and Het is as defined in Tables 4705 as defined in any of Tables 1 to 784. 5488 149027.doc -85- 201103430 Compound of formula L7, wherein the group of compounds R2, R22, R23, R24 and r25 The combination corresponding to the column of Table A and Rl|%Het in each case is a compound of the formula L5, as defined in any one of Tables 1 to 784, wherein R21, R22, RU, The combination of R24 and r25 corresponds in each case to the column of the column and the combination of Rl^et is as shown in any of Tables 1 to 784, as defined in any of Tables 6273 to 7056, the compound of formula 1.9, wherein the compound is r21, r22 And r23, r24, and combinations thereof, in each case corresponding to one of the listed persons, and the combination is as shown in any one of Tables 1 to 784, and the compounds of the formulas 1.705 to 7840, formula 1.10, wherein the compound is 2, The combination of r22, r23, r24 and R25 corresponds in each case to one of the columns of Table A and the combination of Ri and Het is a compound of the formula 7841 to 8624 as defined in any of Tables 1 to 784. Wherein the combination of the compounds 2, R22, r23, r24 and R25 corresponds in each case to one of the columns of Table A and the combination of Ri and Het is as defined in any of Tables 1 to 784, tables 8625 to 9408. A compound of the formula 1.12, wherein the combination of the compounds r21, r22, r23, r24 and R25 corresponds in each case to Table VIII And a combination of lines as defined in Table 9409 to 10192 149027.doc in Tables 1 to 784 of any one of

[SI -86· 201103430 式1.13之化合物’其中化合物之r2i ' r22 ' r23、r24及 R25之組合在各情況下對應於表A之一列且尺1與Het之組合 係如在表1至784之任一者中所定義 表10193至10976 式I. 14之化合物,其中化合物之r21、r22、汉23、r24及 R 5之組合在各情況下對應於表A之一列且R〗與之組合 係如在表1至784之任一者中所定義 表10977至11760 式1.15之化合物,其中化合物之尺2丨、R22、r23、r24及 R之組合在各情況下對應於表A之一列且Ri與Het之組合 係如在表1至784之任一者中所定義 表11761至12544 式1.16之化合物,其中化合物之艮21、r22、r23、r24及 R之組合在各情況下對應於表A之一列且Rl與Het之組合 係如在表1至784之任一者中所定義 表12545至13328 式1.17之化合物’其中化合物之r2丨、r22、r23、r24及 R 5之組合在各情況下對應於表a之一列且…與只以之組合 係如在表1至784之任一者中所定義 表 13329至 141 12 式1.18之化合物,其令化合物之尺21、r22、r23、尺24及 R之組合在各情況下對應於表A之一列且R丨與Het之組合 係如在表1至7 8 4之任一者中所定義 表14113至14896 149027.doc •87· 201103430 式1.19之化合物,其中化合物之1^21、1122、1123、尺24及 R25之組合在各情況下對應於表A之一列且尺丨與只以之組合 係如在表1至7 8 4之任一者中所定義 表14897至15680 式L20之化合物,其中化合物之R21 ' R22、R23、R24及 R25之組合在各情況下對應於表八之一列且Rl與Het之組合 係如在表1至7 8 4之任一者中所定義 表15681至16464 式1.21之化合物,其中化合物之r21、r22、r23、尺24及 R之組合在各情況下對應於表A之一列且Rl與之組合 係如在表1至7 8 4之任一者中所定義 表 16465至 17248 式1.22之化合物,其中化合物之尺21、r22、r23、r24及 R之組合在各情況下對應於表A之一列且R1與之組合 係如在表1至7 8 4之任一者中所定義 表17249至18032 式1.23之化合物,其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表A之一列且Ri與Het之組合 係如在表1至7 8 4之任一者中所定義 表18033至18816 式1.24之化合物,其中化合物之尺21、r22、r23、r24及 R25之組合在各情況下對應於表八之一列且Rl與Het之組合 係如在表1至784之任一者中所定義 表 18817至 19600 149027.doc ί -88- 201103430 式Ι·25之化合物,其中化合物之r2i、r22、r23、r24及 R之組合在各情況下對應於表A之一列且R1與Het之組合 係如在表1至784之任—者中所定義 表 19601至20384 式1.26之化合物,其中化合物之尺2丨、r22、r23、r24及 2 5 R之組合在各情況下對應於表Λ之一列且R丨與Het之組合 係如在表1至784之任一者中所定義 表 20485至 21168 式1.27之化合物,其中化合物之尺21、R22、r23、r24及 R之組合在各情况下對應於表A之一列且R1與Het之組合 係如在表1至784之任一者中所定義 表21169至21952 式1.28之化合物,其中化合物之R21、R22、r23、r24及 R之組合在各情況下對應於表A之一列且R1與Het之組合 係如在表1至784之任一者中所定義 表21953至22736 式1.29之化合物,其中化合物之尺2!、R22、r23 ' r24及 2 5 R之組合在各情況下對應於表A之一列且r丨與Het之組合 係如在表1至784之任一者中所定義 表22737至23520 式1.30之化合物,其中化合物之r2i、r22、r23、r24及 R25之組合在各情況下對應於表A之一列且Ri與Het之組合 係如在表1至784之任一者中所定義 表23521至24304 149027.doc •89· 201103430 25式1.31之化合物,其中化合物之尺21、尺22、&23、尺24及 R25之組合在各情況下對應於表A之-列且Ri與Het之組合 係如在表1至784之任一者中所定義 表 24305至 25088 μ式1.32之化合物,其中化合物之尺2丨、r22、r23、尺以及 . 心之組合在各情況下對應於表A之-列且Ri與Het之組合: 係如在表1至784之任一者中所定義 表 25089至 25872 式L33之化合物,其中化合物之R2i、R22、R23、r24及 R25之組合在各情況下對應於表A之-列且Ri與Het之組合 係如在表1至784之任一者中所定義 表25873至26656 2式Ι·34之化合物,其中化合物之尺2丨、r22、R23、r24及 R25之組合在各情況下對應於表AmR丨與此之組合 係如在表1至784之任一者中所定義 表 26657至 27440 式1_35之化合物,其中化合物之r2i、r22、r23、尺24及 R25之組合在各情況下對應於表八之一列且以此之組合 係如在表1至784之任一者中所定義 表27441至28224 式1.36之化合物,其中化合物之r2i、r22、尺23、尺24及 R25之組合在各情況下對應於表八之—列且Rl#Het之組合 係如在表1至784之任一者中所定義 表 28225至 29008 149027.doc[SI-86·201103430 The compound of the formula 1.13 wherein the combination of the compound r2i 'r22 'r23, r24 and R25 corresponds in each case to one of the tables A and the combination of the ruler 1 and Het is as shown in Tables 1 to 784. Any of the compounds of formula I.14 to 10976, formula I.14, wherein the combination of the compounds r21, r22, Han23, r24 and R5 corresponds in each case to one of the columns of Table A and is in combination with R. A compound of the formulae 1.15 to 11760, as defined in any one of Tables 1 to 784, wherein the combination of the ruthenium 2, R22, r23, r24 and R of the compound corresponds in each case to one of the columns of Table A and Ri The combination with Het is as defined in any of Tables 1 to 784, and the combination of 艮21, r22, r23, r24 and R of the compound corresponds in each case to Table A. A combination of R1 and Het is as defined in any of Tables 1 to 784. Tables 12545 to 13328, a compound of formula 1.17, wherein a combination of compounds r2丨, r22, r23, r24 and R 5 is used in each case. The lower one corresponds to one of the columns of the table a and is combined with only the table defined as in any of the tables 1 to 784. 3329 to 141 12 a compound of the formula 1.18, wherein the combination of the ruler 21, r22, r23, ruler 24 and R of the compound corresponds in each case to one of the columns of Table A and the combination of R and Het is as shown in Tables 1 to 7. Table 14113 to 14896 149027.doc • 87· 201103430 A compound of the formula 1.19 in which the combination of 1^21, 1122, 1123, 24 and R25 of the compound corresponds in each case to Table A. And a combination of only R6' R22, R23, R24 and R25 of the compound as defined in any one of Tables 1 to 784. In each case, it corresponds to a column of Table 8 and the combination of R1 and Het is a compound of the formulae 1.261 to 16464 of formula 1.21 as defined in any one of Tables 1 to 784, wherein the compound is r21, r22, r23, and ruler. The combination of 24 and R corresponds in each case to one of the columns of Table A and R1 is combined with a compound of the formulae formulae 16465 to 17248, formula 1.22 as defined in any one of Tables 1 to 784, wherein the compound is 21 The combination of r22, r23, r24 and R corresponds in each case to one of the columns of Table A and R1 is combined with it as shown in Table 1 to A compound of the formula: formula 1249 to 18032, formula 1.23, wherein the combination of the compounds r21, r22, r23, r24 and R25 corresponds in each case to one of the columns of Table A and the combination of Ri and Het A compound of the formula: formula 1.823 to 18816, formula 1.24, as defined in any one of Tables 1 to 784, wherein the combination of the ruler 21, r22, r23, r24 and R25 of the compound corresponds in each case to one of the The combination of R1 and Het is as defined in any one of Tables 1 to 784, and the compounds of the formula 188 17 88 88 88 88 88 25 25 25 25 , , 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 25 The combination in each case corresponds to one of the columns of Table A and the combination of R1 and Het is a compound of the formula 1601 to 20384, formula 1.26 as defined in any of Tables 1 to 784, wherein the compound is 2, r22, The combination of r23, r24 and 2 5 R corresponds in each case to one of the columns and the combination of R and Het is a compound of the formula: formula 1 485 to 21168, formula 1.27, as defined in any of Tables 1 to 784, wherein The combination of the ruler 21, R22, r23, r24 and R of the compound corresponds in each case to one of the columns of Table A and R1 The combination of Het is as defined in any one of Tables 1 to 784, and the combination of R21, R22, r23, r24 and R of the compound corresponds in each case to one of the columns of Table A. And the combination of R1 and Het is as shown in any one of Tables 1 to 784, and the combination of the compound of the formula 2953 to 22736, formula 1.29, wherein the combination of the compound of the ruler 2!, R22, r23 'r24 and 2 5 R is in each case The following corresponds to a column of Table A and the combination of r丨 and Het is a compound of the formulae 12.737 to 23520, formula 1.30, as defined in any of Tables 1 to 784, wherein the compounds are r2i, r22, r23, r24 and R25 The combination corresponds in each case to one of the columns of Table A and the combination of Ri and Het is as defined in any of Tables 1 to 784. Tables 23521 to 24304 149027.doc • 89· 201103430 25 Formula 1.1, wherein the compound The combination of Ruler 21, Ruler 22, & 23, Ruler 24 and R25 corresponds in each case to the column of Table A and the combination of Ri and Het is as defined in any of Tables 1 to 784. Table 24305 Up to 25088 μ of the compound of formula 1.32, wherein the compound is in the range of 2丨, r22, r23, ruler and heart. Corresponding to the column of Table A and the combination of Ri and Het: a compound of the formula L259, 25872, L33, as defined in any of Tables 1 to 784, wherein the compound is R2i, R22, R23, r24 and The combination of R25 corresponds in each case to the column of Table A and the combination of Ri and Het is a compound of the formula 25873 to 26656 as defined in any of Tables 1 to 784. The combination of 2丨, r22, R23, r24 and R25 corresponds in each case to the combination of the table AmR丨 and the compound of the formulae 1 to 35, as defined in any of Tables 1 to 784, wherein the compound The combination of r2i, r22, r23, ruler 24 and R25 corresponds in each case to one of the columns of Table 8 and the combination thereof is as defined in any of Tables 1 to 784. Tables 27441 to 28224 Formula 1.36 Wherein the combination of the compound r2i, r22, ruler 23, ruler 24 and R25 corresponds in each case to the column of Table 8 and the combination of Rl#Het is as defined in any of Tables 1 to 784. To 29008 149027.doc

[SI -90· 201103430 式1,37之化合物,其中化合物之R21、R22、R23、R24及 R之組合在各情況下對應於表A之一列且Ri與Het之組合 係如在表丨至784之任—者中所定義 表 29009至 29792 式L38之化合物,其中化合物之r21、r22、r23、r24 2 5 R之組合在各情況下對應於表A之一列且Ri與Het之組合 係如在表1至784之任—者中所定義 表 29793至 30576 式1.39之化合物,其中化合物之尺2|、r22、r23、r24及 R25之組合在各情況下對應於表A之一列且Ri與Het之組合 係如在表1至7料之任一者中所定義 表30577至31360 式1.40之化合物,其中化合物之尺2丨、R22、R23、R24及 R25之組合在各情況下對應於表A之一列且之組合 係如在表1至784之任一者中所定義 表31361至32144 式1.41之化合物,其中化合物之尺2丨、r22、r23、r24及 R之組合在各情況下對應於表八之一列且Rl與Het之組合 係如在表1至7 8 4之任一者中所定義 表32145至32928 式1.42之化合物’其中化合物之R2i、R22、r23、r24及 R之組合在各情況下對應於表A之一列且Ri與Het之組合 係如在表1至7 8 4之任一者中所定義 表32929至33712 149027.doc -91· 201103430 式1.43之化合物,其中化合物之1121、1122、1123、尺24及 R25之組合在各情況下對應於表A之一列且Rl與Het之組合 係如在表1至784之任一者中所定義 表 33713 至 34496 式1.44之化合物’其中化合物之r21、r22、r23、r24及 τι 2 5 之組合在各情況下對應於表Α之一列且R1與Het之組合 係如在表1至7 8 4之任一者中所定義 表 34497至 35280 式1.45之化合物,其中化合物之尺21、R22、r23、r24及 R25之組合在各情況下對應於表A之一列且R1與Het之組合 係如在表1至784之任一者中所定義 表 35281 至 36064 式1.46之化合物’其中化合物之r2i、r22、r23、r24及 R25之組合在各情況下對應於表A之一列且R1與Het之組合 係如在表1至784之任一者中所定義 表 36065至 36848 式1.47之化合物,其中化合物之R21、R22、r23、r24及 2 5 R之組合在各情況下對應於表A之一列且R1與Het之組合 係如在表1至784之任一者中所定義 表 36849至 37632 式1_48之化合物,其中化合物之r2i、r22、r23、r24及 R25之組合在各情況下對應於表A之一列且R1與Het之組合 係如在表1至784之任一者中所定義 表 37633 LS1 149027.doc -92- 201103430 式Ϊ.49之化合物,其中化合物之R21、r22、r23、r24及 2 5 R之組合在各情 況下對應於表A之一列且Het為式Het.l之 基團 表37634 式L49之化合物,其中化合物之R21、R22、R23、R24及 R之組合在各情況下對應於表A之一列且Het為式Het.2之 基團 表 37635 式1.49之化合物,其中化合物之r21、r22、r23、r24及 R之組合在各情況下對應於表A之一列且Het為式Het.3 l 基團 表37636 式1.49之化合物,其中化合物之r21、r22、r23、r24及 2 5 R之組合在各情況下對應於表A之一列且Het為式Het_4之 基團 表37637 式之化合物,其中化合物之R21、r22、r23、r24及 2 5 R之組合在各情況下對應於表A之一列且Het為式Het.5 l 基團 表37638 式L49之化合物,其中化合物之r21、r22、r23、r24及 2 5 R之組合在各情況下對應於表A之一列且Het為式Het.6之 基團 表 37639 149027.doc -93- 201103430 25式L49之化合物’其中化合物之R21、R22、R23、R24及 之且0在各情況下對應於表A之一列且Het為式Het.7之 基團 表 37640 μ式1.49之化合物,其中化合物之r2〗、r22、r23、r24及 R之、且口在各情況下對應於表A之一列且Piet為式net.8之 基團 表 37641 式149之化合物,其中化合物之R21、R22、R23、R24及 Κ之、且〇在各情況下對應於表A之一列且Het為式Het.9之 基團 表 37642 式L49之化合物’其中化合物之R21、R22、R23、R24及 2 5 R之組合在各情況下對應於表A之一列且Het為式Het.10之 基團 表 37643 式L49之化合物,其中化合物之R21、R22、R23、R24及 2 5 R之組合在各情況下對應於表A之一列且Het為式Het.l 1之 基團 表 37644 式1.49之化合物,其中化合物之r2i、r22、r23、r24及 2 5 R之組合在各情況下對應於表A之一列且Het為式Het. 1 2之 基團 表 37645 [si 149027.doc -94- 201103430 式L49之化合物,其中化合物之r21、r22、R23、R24及 2 5 R之組合在各情況下對應於表A之一列且Het為式Het.13之 基團 表37646 式1.49之化合物,其中化合物之r21、r22、r23、r24及 R之組合在各情況下對應於表A之一列且Het為式Het. 14之 基團 表37647 式1.49之化合物,其中化合物之r21、r22、r23、r24及 R之組合在各情況下對應於表A之一列且Het為式Het. 15之 基團 表 37648 式1.49之化合物,其中化合物之R2!、R22、R23、R24及 R25之組合在各情況下對應於表八之一列且Het為式Het 16之 基團 表37649至37664 式1.50之化合物,其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表A之一列且係如在表 37633至37648之任一者中所定義 表 37665至 37680 、R22、R23、R24 及 列且Het係如在表 式1.51之化合物’其中化合物之r2] R 5之組合在各情況下對應於表A之— 37633至37648之任—者中所定義 表37681至37696 149027.doc •95- 201103430 式1,52之化合物,其中化合物之R21、R22、R23、R24及 R之組合在各情況下對應於表A之一列且Het係如在表 37633至3764 8之任—者中所定義 表37697至37712 式1.53之化合物,其中化合物之尺2丨、R22、R23、r24及 2 5 R之組合在各情況下對應於表A之一列且Het係如在表 37633至37648之任一者中所定義 表37713至37728 式1.54之化合物,其中化合物之R21、R22、R23、r24及 R之組合在各情況下對應於表A之一列且Het係如在表 37633至37648之任一者中所定義 表37729至37744 式1_55之化合物,其中化合物之r21、r22、r23、R24及 R 5之組合在各情況下對應於表A之一列且Het係如在表 37633至37648之任一者中所定義 表37745至37760 式1.56之化合物,其中化合物之R2i、r22、r23、r24及 R之組合在各情況下對應於表A之一列且Het係如在表 3:7633至;3 7648之任一者中所定義 表37761至37776 式1.57之化合物,其中化合物之r2i、r22、r23、r24及 R25之組合在各情況下對應於表八之一列且Het係如在表 3763 3至37648之任一者中所定義 表37777至37792 149027.doc -96- 201103430 式1.5 8之化合物,其 R之組合在各情況下 37633至37648之任一者 表37793至37808 式I · 5 9之化合物,甘 R之組合在各情況下 37633至37648之任—者 表37809至37824 式I · 6 0之化合物,复 R之組合在各情況下 37633至37648之任—者 表37825至37840 式1.61之化合物,其 R之組合在各情況下 37633至37648之任—者 表 37841至 37856 式1.6 2之化合物,芦. R25之組合在各情況下 ; 37633至37648之任一者 表 37857至 378872 式Ι·63之化合物,其 R25之組合在各情况下 37633至37648之任—者 表37873至378888 中化合物之R21、R22、R23、R24及 對應於表A之一列且Het係如在表 中所定義 中化合物之R21、R22、R23、R24及 對應於表A之一列且Het係如在表 中所定義 中化合物之R21、R22、R23、R24及 對應於表A之一列且Het係如在表 中所定義 中化合物之R21、R22、r23、r24及 對應於表A之一列且Het係如在表 中所定義 中化合物之R21、R22、r23、r24及 對應於表A之一列且Het係如在表 中所定義 中化合物之R21 ' R22、r23、r24及 對應於表A之一列且Het係如在表 中所定義 149027.doc -97- 201103430 其中化合物之R2〗 下對應於表Α之一 者中所定義 其中化合物之R21 下對應於表A之一 者中所定義 其中化合物之R21 下對應於表A之一 者中所定義 其中化合物之R21 下對應於表A之一 者中所定義 其中化合物之R21 下對應於表A之一 者中所定義 其中化合物之R21 下對應於表A之-者中所定義 式1_64之化合物, R之組合在各情況 37633至 37648之任— 表37889至37904 式1.65之化合物, R之組合在各情況 37633至 37648之任— 表37905至37920 式1.66之化合物, R25之組合在各情況 37633至 37648之任— 表37921至37936 式1.6 7之化合物, R25之組合在各情況 3763.3至 37648之任 _ 表37937至37952 式I · 6 8之化合物, R25之組合在各情況 37633至 37648之任— 表37953至37968 式Ι·69之化合物, R25之組合在各情況 37633至 37648之任一 表37969至37984 、R22、R23、R24 及 列且Het係如在表 、R22、R23、R24 及 列且Het係如在表 、R22、R23、R24 及 列且Het係如在表 、R22、R23、R24 及 列且Het係如在表 、R22、R23、R24 及 列且Het係如在表 、R22、R23、R24 及 列且Het係如在表 I49027.doc •98- 201103430 式I · 7 0之化合物, R之組合在各情况 37633 至 37648之任— 表37985至38000 式I · 71之化合物, R25之組合在各情況 37633至 37648之任— 表38001至38016 其中化合物之R21、R22、R23、R24及 下對應於表A之一列且Het係如在表 者中所定義 其中化合物之R21、R22、R23、R24及 下對應於表A之一列且Het係如在表 者中所定義 式2之化s物,其中化合物之r21 ' r22、r23、r24及 R之、,且σ在各情況下對應於表A之一列且係如在表 37633至37648之任—者中所定義 表38017至38032 式1.73之化合物,其中化合物之r21、r22、r23、尺24及 R25之組合在各情況下對應於表A之一列且HU係如在表 37633至37648之任一者中所定義 表38033至38048 式1.74之化合物,其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表A之一列且Het係如在表 37633至37648之任一者中所定義 表38049至38064 式1.75之化合物,其中化合物之R21、r22、R23、r24及 R25之組合在各情況下對應於表A之一列且Het係如在表 37633至37648之任一者中所定義 表38065至38080 149027.doc -99- 201103430 R之組合在各情況下 37633至37648之任一者中所定 表38113至38128 式1.79之化合物’其中化合物之rZ1 R25之組合在各情況下對應於表A之一 37633至3:7648之任一者中所定義 表38129至38144 式1.80之化合物,其中化合物之r2】 R25之組合在各情況下對應於表A之一 37633至376<48之任一者中所定義 表38145至38160 式1.81之化合物,其中化合物之R2丨 R25之組合在各情況下對應於表A之一 37633至37648之任一者中所定義 表38161至38176 其中化合物之R21 下對應於表A之一 者中所定義 其中化合物之R21 下對應於表A之一 者中所定義 其中化合物之R21 對應於表A之一 式1.76之化合物, R25之組合在各情況 37633 至 37648之任— 表38081至38096 式1.77之化合物, R25之組合在各情況 37633 至 37648 之任 _ 表38097至38112 式丄·/»之 、R22、R23、R24 及 列且Het係如在表 、R22、R23、R24 及 列且Het係如在表 、R22、R23、R24 及 列且Het係如在表 、R22、R23、R24及 列且Het係如在表 、R22、R23、R24 及 列且Het係如在表 、R22、R23、R24 及 列且Het係如在表 149027.doc -100- 201103430 式L82之化合物,其中化合物之R21 R25之組合在各情況下對應於表A之一 37633至37648之任—者中所定義 表38177至38192 式1.83之化合物,其中化合物之rZ1 R25之組合在各情況下對應於表A之一 37633至376M之任—者中所定義 表38193至38208 式Ι·84之化合物,其申化合物之r2丨 R25之組合在各情況下對應於表Α之一 37633至37648之任一者中所定義 表38209至38224 式Ι·85之化合物,其中化合物之R2〗 R25之組合在各情況下對應於表Α之一 37633至37648之任一者中所定義 表38225至38240 式Ι·86之化合物,其中化合物之R2】 R25之組合在各情況下對應於表A之一 37633至3了648之任一者中所定義 表 38241至38256 式1.87之化合物,其中化合物之尺2丨 R25之組合在各情況下對應於表A之一 3763 3至37648之任一者中所定義 表 38257至 38272 149027.doc ' R22、R23、R24及 列且Het係如在表 .R22、R23、R24 及 列且Het係如在表 R22、R23、R24 及 列且Het係如在表 R22、R23、R24 及 列且Het係如在表 R22、R23、R24及 列且Het係如在表 ‘ R22、R23、R24 及 列且Het係如在表 -101 - 201103430 式I · 8 8之化合物,其中化合物之r2 1、 R25之組合在各情況下對應於表A之一 37633至37648之任一者中所定義 表38273至38288 式1.89之化合物,其中化合物之r2i、 R之組合在各情況下對應於表A之一 37633至376斗8之任一者中所定義 表38289至38304 式1_90之化合物,其中化合物之Rn R之組合在各情況下對應於表A之一 37633至37648之任一者中所定義 表38305至38320 式1.91之化合物,其中化合物之R:n R25之組合在各情況下對應於表A之一 3 763 3至376*48之任一者中所定義 表38321至38336 式1.92之化合物,其中化合物之 R25之組合在各情況下對應於表A之一 3了633至3764·8之任一者中所定義 表38337至38352 式1.93之化合物,其中化合物之r2〗 R25之組合在各情況下對應於表A之一 37633至3<7648之任一者中所定義 表38353至38368 149027.doc H22、R23、RU 及 列且Het係如在表 R22、R23、R24 及 列且Het係如在表 .R22、R23、R24 及 列且Het係如在表 、R22、R23、及 列且Het係如在表 、R22、R23、及 列且Het係如在表 、R22、R23、r24 及 列且Het係如在表 -102- 201103430 、R22、R23、r24 及 列且Het係如在表 、R22、R23、R24及 列且Het係如在表 式1.94之化合物,其中化合物之r2, r25之組合在各情況下對應於表A之一 37633至3764*8之任一者中所定義 表 38369至 38384 式1.95之化合物,其中化合物之r2丨 R25之組合在各情況下對應於表A之一 37633至37648之任一者中所定義 表38385至38400 、R22、R23、R24 列且Het係如在 及 表 式1_96之化合物’其中化合物之ru R25之組合在各情況下對應於表A之一 37633至37648之任一者中所定義 表38401至38449 式1.97之化合物, 況下對應於表8之一 表38450至38498 其中化合物之Het與Ar,之組合在各情 列且R1係如在表丨至的之任一者中所定^ 式1.98之化合物 況下對應於表8之_ 表38499至38547 式1.99之化合物 況下對應於表B之一 表38548至38596 其中化合物之Het與Ar·之組合在各情 列且R1係如在表1至4 9之任一者中所定^ 其中化合物之Het與Ar,之組合在各情 列且R1係如在表丨至49之任一者中所定= 式1.100之化合物,其中化合物之11以與心,之級合在 況下對應於表B之一列且R1係如在表丨至4 9之任一者 ^情 表38597至38645 戶斤定義 149027.doc •103- 201103430 式1.101之化合物 況下對應於表B之一 表 38646至38694 式1.102之化合物 況下對應於表B之一 表38695至38743 式1.103之化合物 況下對應於表B之一 表 38744至 38792 式1.104之化合物 況下對應於表B之一 表 38793至 38841 式1.1 0 5之化合物 況下對應於表B之一 表38842至38890 式1.106之化合物 況下對應於表B之一 表 38891至 38939 式1.107之化合物 況下對應於表B之一 表38940至38988 式1.108之化合物 況下對應於表B之一 表38989至39037 ’其中化合物之Het與Ar,之組合在各产 列且R1係如在表丨至49之任—者中所定^ ,其中化合物之Het與Ar,之組合在各情 列且R1係如在表1至49之任—去由& 月 百肀所定義 ,其中化合物之Het與Ar,之組合在各情 列且R1係如在表i至4 9之任—者中所定= ,其中化合物之Het與Ar,之組合在各情 列且R1係如在表丨至49之任—者中所a 2 ,其中化合物之Het與Ar,之組合在各情 列且R】係如在表1至49之任一者中所a ,其中化合物之Het與Ar,之組合在各情 列且R1係如在表丨至49之任—者中所定義 ’其中化合物之Het與W之組合在各情 列且R1係如在表^的之任一者中所定: ,其中化合物之1^1與八1·,之組合在各情 列且R1係如在之任一者中所定^ 149027.doc •104- [S] 201103430 式Ι· 109之化合物 況下對應於表Β之一 表39038至39086 式1.110之化合物 況下對應於表Β之一 表39087至39135 式1.111之化合物 況下對應於表Β之一 表39136至39184 式1.112之化合物 況下對應於表Β之一 表39185至39233 式1.113之化合物 況下對應於表Β之一 表39234至39282 式1.114之化合物 況下對應於表Β之一 表39283至39331 式1.115之化合物 況下對應於表Β之一 表39332至39380 式I. _116之化合物 況下對應於表B之一 表39381至39429 ’其中化合物之Het與Ar,之組合在各情 列且R1係如在表U49之任_者中所定義 ,其中化合物之Het與Ari之組合在各情 列且R1係如在表心之任—者中所定義 ,其中化合物之HeW^Ar,之組合在各情 列且R1係如在幻至的之任—者中所定義 ,其中化合物之Het與Ar,之組合在各情 列且R1係如在⑸至的之任—者中所定義 ,其中化合物之Het與Ar,之組合在各情 列且R1係如在表i至49之任—者中所定義 ,其中化合物之Het與Ar,之組合在各情 列且R丨係如在表149之任一者中所定義 ,其中化合物之11以與^,之組合在各情 列且R1係如在表^的之任—者中所定義 其中化合物之Het與Ar'之組合在各情 列且R1係如在表之任—者中所定義 149027.doc -105- 201103430 式1.117之化合物,其中化合物之之組合在各情 況下對應於表B之一列且R1係如在表1至49之任一者中所定義 表 39430至 39478 式1.118之化合物,其中化合物之]^以與心,之組合在各情 況下對應於表B之一列且R1係如在表丨至的之任一者中所定義 表39479至39527 式1.119之化合物,其中化合物之^【與心,之組合在各情 況下對應於表B之一列且R〗係如在表〖至的之任一者中所定義 表39528至39576 式1.120之化合物,其中化合物之H_Ar,之組合在各情 況下對應於表B之一列且R1係如在表丨至49之任一者中所定 表39577至39625 式1.121之化合物,其中化合物之此與心,之組合在各,产 況下對應於表B之-列仏係如在表U49之任一者中: 表39626至39674 ^ 之組合在各情 一者中所定義 式1.122之化合物,其中化合物之Het與斛, 況下對應於表B之一列且R1係如在表丨至4 9之任 表39675至39723 ……〜姐各、在 況下對應於表B之-列且R、如在表^的之任—者 表39724至39772 式1.124之化合物,其中化合物之此與心,之組合在 況下對應於表B之-列且如在表ι49之任—者° 表39773至39821 斤 I49027.doc -106- 201103430 式L125之化合物,其中化合物之Het與Ar,之虹合在各产 況下對應於表B之-列W係如在幻㈣之任—者中所定二 表39822至39870 ^ ^ 式1.126之化合物’其中化合物之此與",之組合在各产 況下對應於表B之-列且以如在表(至心之任一者中所定^ 表39871至39919 式1.127之化合物,其中化合物之Het與Ar,之組合在各怦 況下對應於表B之-列且…係如在表丨至的之任—者中所定^ 表39920至39968 式1.128之化合物,其中化合物之H^Ar,之組合在各情 況下對應於表B之-列且如在表u49之任_者中所定^ 表39969至40017 式1.129之化合物,其中化合物之此與Ar,之組合在各情 況下對應於表B之-列_S_rM系如在幻至做任—者中所定^ 表40018至40066 式1.130之化合物,其中化合物之_與之組合在各情 況下對應於表B之-列且如在表u49之任—者中所定^ 表40067至40115 式1.13工之化合物,丨中化合物之此與心,之組合在各情 況下對應於表B之-列且R1係如在表i至4 9之任—者中所定^ 表40116至40164 式J.132之化合物,其中化合物之组合在各情 況下對應於表B之-列W係如在幻至的之任—者_所 表40165至40213 149027.doc ' 107- 201103430 式1.133之化合物 況下對應於表B之一 表40214至40262 式1.134之化合物 況下對應於表B之一 表40263至40311 式1.135之化合物 況下對應於表B之一 表40312至40360 式1.13 6之化合物 況下對應於表B之一 表40361至40409 式1.1 3 7之化合物 況下對應於表B之一 表40410至40458 式1.138之化合物 況下對應於表B之一 表40459至40507 式1.139之化合物 況下對應於表B之一 表40508至40556 式1.140之化合物 況下對應於表B之一 表 40557至 40605 ,其中化合物之Het與Ar,之組合在各情 列且R1係如在表上至的之任一者中所定義 ,其中化合物之Het與Ar,之組合在各情 列且R1係如在表1至49之任一者中所定義 ,其中化合物之Het與Ar,之組合在各情 列且R1係如在表1至49之任一者中所定義 ’其中化合物之Het與Ar,之組合在各情 列且R1係如在表1至49之任一者中所定義 ,其中化合物之Het與Ar·之組合在各情 列且R1係如在表1至49之任一者中所定義 ’其中化合物之Het與Ar'之組合在各情 列且R1係如在表1至49之任一者中所定義 ,其中化合物之Het與Ar,之組合在各情 列且R1係如在表1至49之任一者中所定義 ’其中化合物之Het與Ar,之紕合在各情 列且R1係如在表1至49之任一者中所定義 149027.doc[SI-90·201103430 A compound of formula 1,37 wherein the combination of R21, R22, R23, R24 and R of the compound corresponds in each case to one of the columns of Table A and the combination of Ri and Het is as shown in Table 784 to The compounds of the formula L29, wherein the combination of r21, r22, r23, r24 2 5 R of the compound corresponds in each case to one of the columns of Table A and the combination of Ri and Het is as in Tables 29793 to 30576, the compounds of formula 1.39, as defined in Tables 1 to 784, wherein the combination of the rulers 2|, r22, r23, r24 and R25 of the compounds corresponds in each case to one of the columns of Table A and Ri and Het The combination is as defined in any of Tables 1 to 7 of Tables 30577 to 31360, formula 1.40, wherein the combination of the compounds 2, R22, R23, R24 and R25 corresponds in each case to Table A. One of the combinations is a compound of the formula: 31361 to 32144, formula 1.41, as defined in any one of Tables 1 to 784, wherein the combination of the compounds 2, r22, r23, r24 and R corresponds in each case to A combination of R1 and Het is as shown in any of Tables 1 to 784. Table 32145 32928 Compound of the formula 1.42 wherein the combination of R2i, R22, r23, r24 and R of the compound corresponds in each case to one of the columns of Table A and the combination of Ri and Het is as in any of Tables 1 to 784. Tables 32929 to 33712 149027.doc -91· 201103430 Compounds of the formula 1.43, wherein the combination of the compounds 1121, 1122, 1123, 24 and R25 corresponds in each case to one of the columns of Table A and the combination of R1 and Het Tables 33713 to 34496, as defined in any of Tables 1 to 784, of the compound of formula 1.44, wherein the combination of the compounds r21, r22, r23, r24 and τι 2 5 corresponds in each case to one of the columns and R1 The combination with Het is as defined in any of Tables 1 to 784, and the combination of the compounds of the formulae 21497 to 35280, wherein the combination of the compounds 21, R22, r23, r24 and R25 corresponds in each case to The combination of R1 and Het is as shown in any one of Tables 1 to 784, and the combination of r2i, r22, r23, r24 and R25 of the compound is as defined in any of Tables 1 to 784. The lower one corresponds to one of the columns of Table A and the combination of R1 and Het is as shown in Tables 1 to 784. A compound of formula 1.476, wherein the combination of R21, R22, r23, r24 and 2 5 R of the compound corresponds in each case to one of the columns of Table A and the combination of R1 and Het is as shown in the table. The compounds of the formulae 1 to 784, wherein the combination of the compounds r2i, r22, r23, r24 and R25 corresponds in each case to one of the columns of Table A and the combination of R1 and Het is defined in any one of 1 to 784. Table 34633 LS1 149027.doc -92- 201103430 A compound of the formula 4949, wherein the combination of R21, r22, r23, r24 and 2 5 R of the compound is in each case, as defined in any of Tables 1 to 784 Corresponding to a group of Table A and Het is a compound of the formula Het.l, Table 34634, Formula L49, wherein the combination of R21, R22, R23, R24 and R of the compound corresponds in each case to one of Table A and Het is Groups of formula Het. 2 Table 37635 Compounds of formula 1.49 wherein the combination of compounds r21, r22, r23, r24 and R corresponds in each case to one of Table A and Het is a formula of Het. 3 l Group Table 37636 a compound of the formula 1.49, wherein the combination of the compounds r21, r22, r23, r24 and 2 5 R is in each case The compound corresponding to the group of Table A and Het is a group of the formula Het_4, wherein the combination of R21, r22, r23, r24 and 2 5 R of the compound corresponds in each case to one of the columns of Table A and Het is Het. 5 l Group Table 37638 Compound of the formula L49 wherein the combination of the compounds r21, r22, r23, r24 and 2 5 R corresponds in each case to one of the columns of Table A and Het is a group of the formula Het. Table 37639 149027.doc -93- 201103430 25 Compound of formula L49 'wherein the compounds R21, R22, R23, R24 and 0 and in each case correspond to one of the tables A and Het is a group of the formula Het. 37640 μ Compound of formula 1.49, wherein the compound is r2, r22, r23, r24 and R, and the mouth corresponds in each case to one of the columns of Table A and Piet is a group of the formula net.8. Table 37641 Formula 149 , wherein R21, R22, R23, R24 and hydrazine of the compound, and hydrazine in each case correspond to one of the columns of Table A and Het is a group of the formula Het.9, Table 37642, a compound of the formula L49, wherein the compound R21, R22 The combination of R23, R24 and 2 5 R corresponds in each case to one of the columns of Table A and Het is a group of the formula Het. 10 a compound of the formula L49, wherein the combination of the compounds R21, R22, R23, R24 and 2 5 R corresponds in each case to one of the columns of Table A and Het is a group of the formula Het.l 1 of the formula 37644 formula 1.49, Wherein the combination of the compounds r2i, r22, r23, r24 and 2 5 R corresponds in each case to one of the columns of Table A and Het is a group of the formula Het. 1 2 Table 34545 [si 149027.doc -94- 201103430 Formula L49 a compound wherein the combination of the compounds of r21, r22, R23, R24 and 2 5 R corresponds in each case to one of the columns of Table A and Het is a group of the formula Het. 13 of the formula 37646 of the formula 1.49, wherein the compound r21 The combination of r22, r23, r24 and R corresponds in each case to one of the columns of Table A and Het is a group of the formula Het. 14 of the formula 37647. The compound of the formula 1.49 wherein the compounds are r21, r22, r23, r24 and R Combining the compounds in each case corresponding to one of the columns of Table A and Het is a group of the formula Het. 15 of the formula 37648 formula 1.49, wherein the combination of the compounds R2!, R22, R23, R24 and R25 corresponds in each case to the table One of the eight columns and Het is a group of the formula Het 16 of Tables 37649 to 37664 of the formula 1.50, wherein the compound The combination of r21, r22, r23, r24 and R25 corresponds in each case to one of the columns of Table A and is as defined in any of Tables 37633 to 37648, tables 37656 to 37680, R22, R23, R24 and Het is as shown in Table 1.51, wherein the combination of the compound r2] R 5 corresponds in each case to Table A - 37633 to 37648 - Tables 37681 to 37696 149027.doc • 95-201103430 A compound of formula 1,52 wherein the combination of R21, R22, R23, R24 and R of the compound corresponds in each case to one of Table A and Het is as defined in Tables 37763 to 3764 8 of Table 37697 To a compound of formula 1.53, wherein the combination of the compounds of the formula 2, R22, R23, r24 and 2 5 R corresponds in each case to one of the columns of Table A and the Het is as in any of Tables 37633 to 37648. Tables 37713 to 37728 are compounds of formula 1.54 wherein the combination of R21, R22, R23, r24 and R of the compound corresponds in each case to one of the columns of Table A and the Het is as defined in any of Tables 37633 to 37648. Tables 37729 to 37574 compounds of formula 1-55, wherein the compounds are r21, r22, r23, R24 The combination of R 5 corresponds in each case to one of the columns of Table A and the Het is a compound of the formula: 37.754 to 37760, formula 1.56, as defined in any of Tables 37633 to 37648, wherein the compounds are R2i, r22, r23, r24 and The combination of R corresponds in each case to one of the columns of Table A and the Het is a compound of the formula: formula 37761 to 37776, formula 1.57, as defined in any of Tables 3:7633 to 3768, wherein the compound is r2i, r22, r23 The combination of r24 and R25 corresponds in each case to one of the columns of Table 8 and the Het is a compound of the formula 37777 to 37792 149027.doc-96-201103430 Formula 1.5 8 as defined in any of Tables 3763 3 to 37648, The combination of R in each case 37633 to 37648, Tables 37793 to 37808, the compound of formula I · 5 9 , the combination of Gan R in each case 37633 to 37648 - Table 37809 to 37824 Formula I · 6 The compound of 0, the combination of complex R in each case 37633 to 37648 - the compound of Table 37825 to 37840 Formula 1.61, the combination of R in each case 37633 to 37648 - Table 37841 to 37856 Formula 1.6 2 Compound, Lu. Combination of R25 in each case; 37633 to 37648 Any of the compounds of Tables 37857 to 378872, the combination of R25 in each case 37633 to 37648 - the compounds of Tables 37873 to 378888, R21, R22, R23, R24 and corresponding to Table A And Het is as defined in the table, R21, R22, R23, R24 of the compound and R21, R22, R23, R24 corresponding to the compound of Table A and Het is as defined in the table and corresponds to Table A One of the columns and Het is as defined in the table, R21, R22, r23, r24, and R21, R22, r23, r24 corresponding to the compound of Table A and Het is as defined in the table and corresponds to Listed in Table A and Het is R21 'R22, r23, r24 as defined in the table and corresponds to one of Table A and Het is as defined in the table 149027.doc -97- 201103430 wherein R2 of the compound The lower one corresponding to the one defined in the table, wherein the compound under R21 corresponds to the one defined in Table A, wherein the compound under R21 corresponds to the one defined in Table A, wherein R21 corresponds to the table. Corresponding to R21 under the definition of one of A A compound of the formula 1-64, wherein R21 of the compound corresponds to the formula 1-64 as defined in Table A, a combination of R in each case 37633 to 37648 - a compound of the formula 1.6889 to 37904 formula 1.65, The combination of R in each case 37633 to 37648 - Tables 37905 to 37920 The compound of formula 1.66, the combination of R25 in each case 37633 to 37648 - Tables 37921 to 37936 The compound of formula 1.6 7 , the combination of R25 in each case 3763.3 To 37648 _ Tables 37937 to 37952 Compounds of Formula I · 6 8 , combinations of R 25 in each case 37633 to 37648 - Tables 37953 to 37968 Compounds of formula 69 69, combinations of R 25 in each case 37633 to 37648 Either Tables 37969 to 37984, R22, R23, R24 and Columns and Het are as shown in Table, R22, R23, R24 and Column and Het is as shown in Table, R22, R23, R24 and Column and Het is as shown in Table, R22 , R23, R24 and Rhe are as shown in Table, R22, R23, R24 and Het are as shown in Table, R22, R23, R24 and Column and Het is as shown in Table I49027.doc •98- 201103430 Formula I 70 compounds, R combination in any case 37633 to 37648 - 37985至38000 The compound of formula I · 71, the combination of R25 is in any case of 37633 to 37648 - Tables 38001 to 38016 wherein R21, R22, R23, R24 of the compound and the lower one correspond to one of Table A and the Het is as shown in the table. Wherein R21, R22, R23, R24 of the compound and the lower one corresponding to one of Table A and Het are as defined in the formula 2, wherein the compound r21 'r22, r23, r24 and R, and σ in each case corresponds to one of the tables A and is as defined in Tables 37633 to 37648, as defined in Tables 37017 to 38032, formula 1.73, wherein the compound is r21, r22, r23, ruler The combination of 24 and R25 corresponds in each case to one of the columns of Table A and the HU is as defined in any of Tables 37633 to 37648, as shown in any of Tables 38033 to 3848, compounds of formula 1.74, wherein the compounds are r21, r22, r23, r24 And the combination of R25 corresponds in each case to one of the columns of Table A and the Het is a compound of the formula 3,490 to 38,064, as defined in any of Tables 37633 to 37648, wherein the compound is R21, r22, R23, r24 and The combination of R25 corresponds in each case to one of the columns of Table A and the Het is Tables 38065 to 38080 149027.doc-99-201103430 R, as defined in any of Tables 37633 to 37648, in each case 37113 to 37648, as defined in any of the tables 38113 to 38128, the compound of the formula 1.79, wherein the compound The combination of rZ1 R25 corresponds in each case to the compound of the formulae 38129 to 38144 of the formulae defined in any one of Tables A37, 33 to 3, 7648, wherein the combination of the compounds r2] R25 corresponds in each case to the table. Table 38145 to 38160, a compound of formula 1.81, as defined in any one of A 37, 376 to 376 < 48, wherein the combination of R 2 丨 R 25 of the compound corresponds in each case to any one of the ones of Table A, 37633 to 37648. Tables 36161 to 38176 are defined, wherein R21 of the compound corresponds to a compound defined by one of Table A, wherein R21 of the compound corresponds to one of Table A, wherein R21 of the compound corresponds to Formula 1.76 of Table A, The combination of R25 is in any case of 37633 to 37648 - Table 38081 to 38096 The compound of formula 1.77, the combination of R25 is in any case of 37633 to 37648 - Tables 38097 to 38112, R·/», R22, R23, R24 and Column Het is as shown in Table, R22, R23, R24 and Het is as shown in Table, R22, R23, R24 and Column and Het is as shown in Table, R22, R23, R24 and Column and Het is as shown in Table, R22, R23, R24 and the columns and Het are as shown in the table, R22, R23, R24 and Het are as shown in Table 149027.doc -100-201103430 Formula L82, wherein the combination of the compound R21 R25 corresponds in each case to Tables 38177 to 38192 of any of Tables 37 to 37, 648, wherein the combination of compounds of rZ1 R25, in each case corresponds to one of Tables A, 37,533 to 376, M. Tables 38193 to 38208 Compounds of the formula 8484, the combination of the compounds of the formula r2丨R25, in each case corresponding to the compounds of Tables 38209 to 38824, as defined in any one of the classes 37633 to 37648, Ι·85 , wherein the combination of R2 and R25 of the compound corresponds in each case to the compound of the formula 38925 to 38240, which is defined in any one of the classes 37633 to 37648, wherein the combination of the compound R2] R25 is In the case corresponding to the table defined in any one of Tables 37633 to 3, 648 38241 to 38256 A compound of the formula 1.87, wherein the combination of the compound of the formula 2丨R25 corresponds in each case to Table 38257 to 38272 149027.doc 'R22, R23, as defined in any one of Tables 3763 to 3648. R24 and List and Het are as listed in Tables R22, R23, R24 and Column and Het is as shown in Tables R22, R23, R24 and Column and Het is as shown in Tables R22, R23, R24 and Column and Het is as shown in Table R22. , R23, R24 and the columns and Het are as shown in the table 'R22, R23, R24 and column and Het is as shown in Table-101 - 201103430 Formula I · 8 8 compounds, wherein the combination of compounds r2 1 and R25 in each case The compounds corresponding to Tables 38273 to 38288, formula 1.89, as defined in any one of Tables A37, 33 to 37,648, wherein the combination of the compounds r2i, R corresponds in each case to one of Tables A, 37,536 to 376, Table 38289 to 38304, as defined in any one of formulas 1-90, wherein the combination of Rn R of the compound corresponds in each case to the compound of formulas 38305 to 38320 of formula 1.91 as defined in any one of Tables 37633 to 37648 , wherein the combination of R:n R25 of the compound corresponds in each case to one of the tables A 3 763 3 Tables 38321 to 38336 of any of 376*48 are defined as compounds of formula 1.92, wherein the combination of R25 of the compound corresponds in each case to the table defined in any one of Tables 633 to 3764. 38337 to 38352 A compound of the formula 1.93, wherein the combination of the compound r2 and R25 corresponds in each case to Table 38353 to 38368 149027.doc H22, R23, RU as defined in any one of Tables A, 37,633 to 3 <7648 And Het is as listed in Tables R22, R23, and R24 and Het is as shown in Tables R22, R23, and R24, and Het is as shown in Table, R22, R23, and Het, and Het is as shown in Table, R22. , R23, and List and Het are listed in the table, R22, R23, r24 and Het are as shown in Table-102-201103430, R22, R23, r24 and Het are as shown in Table, R22, R23, R24 and And Het is a compound of the formula: 1.94, wherein the combination of the compounds r2, r25 corresponds in each case to the compound of the formula 38369 to 38384, formula 1.95, as defined in any one of Tables 37633 to 3764*8. , wherein the combination of the compounds r2 丨 R25 corresponds in each case to the table defined in any one of Tables A37533 to 37648 38385 to 38400, R22, R23, R24 and Het are as in the compound of the formula 1_96 'wherein the combination of the compounds ru R25 corresponds in each case to the table defined in any one of Tables A37633 to 37648 38401 to 38849 compounds of formula 1.97, corresponding to Tables 38450 to 38498 of Table 8, wherein the combination of Het and Ar of the compound is in each case and R1 is as defined in any of the formulas. The compound of 1.98 corresponds to Table 8 of Table 8 38499 to 38547. The compound of formula 1.99 corresponds to Table 38548 to 38596 of Table B, wherein the combination of Het and Ar· of the compound is in each case and R1 is as shown in the table. In any one of 1 to 49, wherein a combination of Het and Ar of the compound is in each case and R1 is as defined in any one of Tables to 49 = a compound of the formula 1.100, wherein the compound 11 is In combination with the heart, the gradation corresponds to one of the tables in Table B and R1 is as shown in any of Tables 丨 to 49. _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ The following corresponds to Table B, one of Tables 38646 to 38694, and the compound of formula 1.102 corresponds to Table B. Tables 38695 to 38743 The compound of formula 1.103 corresponds to one of Table B. Tables 38844 to 38792. The compound of formula 1.104 corresponds to one of Table B. Tables 38793 to 38841. The compound of formula 1.1 0 5 corresponds to one of Table B. Tables 38842 to 38890 The compound of formula 1.106 corresponds to one of Table B. Table 38891 to 38939. The compound of formula 1.107 corresponds to one of Table B. Table 38940 to 38988. The compound of formula 1.108 corresponds to Table 38 of Table B. To 39037 'where the compound Het and Ar, the combination is in each column and R1 is as shown in Table 丨 to 49, where the compound Het and Ar, the combination in each case and the R1 system In Tables 1 to 49 - as defined by & Month, where the combination of Het and Ar of the compound is in each case and R1 is as defined in Tables i to 49, where The combination of Het and Ar of the compound is in each case and R1 is as in the range of Tables to 49, wherein the combination of Het and Ar of the compound is in each case and R] is as shown in the table. Any one of 1 to 49, wherein a combination of Het and Ar of the compound is in each case and R1 is as in Tables 丨 to 49 are defined as 'where the combination of Het and W of the compound is in each case and R1 is as defined in any of the tables: wherein 1^1 and VIII of the compound are The combination of each case and the R1 system as defined in any of the 149027.doc •104- [S] 201103430 formula 109· 109 compounds corresponds to one of the tables 39039038 to 39086, formula 1.110 In the case of a compound, it corresponds to one of the compounds of Tables 39087 to 39135. The compound of formula 1.111 corresponds to one of the compounds of Table 39136 to 39184. The compound of formula 1.112 corresponds to one of the formulas of Table 39185 to 39233 of formula 1.113. The compound corresponding to one of the following tables, table 39234 to 39282, formula 1.114, corresponding to one of the compounds, Table 39283 to 39331, formula 1.115, corresponds to one of the tables, table 39332 to 39380, formula I. _116. The following corresponds to Tables 39381 to 39429 of Table B, in which the combination of Het and Ar of the compound is in each case and R1 is as defined in any of Table U49, wherein the combination of Het and Ari of the compound is Emotion and R1 is defined as in the core of the heart, in which the compound HeW ^Ar, the combination is defined in each case and R1 is as defined in the illusion, where the compound Het and Ar, the combination is in each case and the R1 is in (5) to As defined therein, wherein the combination of Het and Ar of the compound is in each case and R1 is as defined in Tables i to 49, wherein the combination of Het and Ar of the compound is in each case and R丨Is defined in any of Table 149, wherein the compound 11 is combined with ^, in each case and R1 is as defined in the table, wherein the compound is Het and Ar' Compounds of the formula 1.117 are defined in each case and R1 is as defined in the table, wherein the combination of compounds corresponds in each case to one of the columns of Table B and R1 is as in Tables 39430 to 39478, as defined in any one of Tables 1 to 49, are compounds of the formula 1.118, wherein the combination of the compound and the heart corresponds in each case to one of the tables B and the R1 is as shown in the table. Any of the compounds defined in Tables 39479 to 39527, formula 1.119, wherein the compound is combined with the heart, in each case Corresponding to one of the columns of Table B and R is a compound of the formula: formula 1.392 to 39576, formula 1.120, as defined in any of the tables, wherein the combination of compounds H_Ar, in each case corresponds to one of the tables B and R1 is a compound of the formula: formula 39577 to 39625, formula 1.121, as defined in any one of Tables to 49, wherein the combination of the compound and the heart is in each case, and the table corresponds to the column-column in the table. In any of U49: a combination of Tables 39926 to 39674^, wherein a compound of formula 1.122 is defined in each of the following, wherein Het and hydrazine of the compound correspond to one of Table B and R1 is as shown in Table 丨4 9 of the table 39675 to 39723 ... ~ sister, in each case corresponding to the column of the table B and R, as in the table ^ - table 39724 to 39772 formula 1.124, wherein the compound and The combination of heart, in the case corresponding to the column of Table B and as shown in Table ι49 - Table 39773 to 39821 kg I49027.doc -106-201103430 Formula L125, in which the compound Het and Ar, the rainbow In each case, it corresponds to Table B - Column W is as defined in the illusion (4) of the two tables 39822 to 39870 ^ ^ The compound of the formula 1.126, wherein the combination of the compound and the ", corresponds to the column of Table B in each case and is as shown in the table (any of the cents) Table 39871 to 39919 Formula 1.127 The compound, wherein the combination of Het and Ar of the compound, in each case corresponds to the column of Table B, and is as defined in Table 399 to 39968, the compound of the formula 1.128, wherein the compound The combination of H^Ar, in each case corresponds to the column of Table B and as defined in Table u49, the compound of formula 39969 to 40017, formula 1.129, wherein the compound is combined with Ar, In the case of the table B, the column _S_rM is as defined in the formula 401 to 40066 of the formula 1.130, wherein the compound _ is combined with the column B in each case. And as defined in Table u49, the compound of Table 1.067 to 40115 is the compound of formula 1.13, and the combination of this compound and the heart of the compound in each case corresponds to the column of Table B and R1 is as shown in Table i. To the stipulations of the stipulations in Tables 4116 to 40164, the compounds of the formula J.132, in which the combinations of the compounds are in each case. The following corresponds to Table B - Column W is as in the case of Magic to - Table 40165 to 40213 149027.doc ' 107- 201103430 Formula 1.133 of the formula corresponds to Table B of one of the tables 4014 to 40262 Formula 1.134 In the case of the compound, it corresponds to Table 40263 to 40311 of Table B. The compound of formula 1.135 corresponds to one of Table B. Table 40312 to 40360. The compound of formula 1.13 6 corresponds to one of Table B. Table 40361 to 40409 Formula 1.1 3 The compound of 7 corresponds to the compound of the formula Table 40410 to 40458 of the formula B. The compound of the formula 1.138 corresponding to the table 40459 to 40507 of the formula B. The compound of the formula 1.139 corresponds to the formula 40508 to 40556 of the formula 1.140. In the case of the compound, it corresponds to Tables 40557 to 40605 of Table B, wherein the combination of Het and Ar of the compound is in each case and R1 is as defined in any of the above, wherein the compound Het and Ar The combination is in each case and R1 is as defined in any one of Tables 1 to 49, wherein the combination of Het and Ar of the compound is in each case and R1 is as in any of Tables 1 to 49. The definition of 'the compound Het and Ar, the combination in each case and the R1 system as in Any one of 1 to 49, wherein a combination of Het and Ar· of the compound is in each case and R1 is as defined in any one of Tables 1 to 49, wherein the combination of Het and Ar' of the compound In each case and R1 is as defined in any of Tables 1 to 49, wherein the combination of Het and Ar of the compound is in each case and R1 is as defined in any of Tables 1 to 49. 'where the compound Het and Ar are combined in each case and R1 is as defined in any of Tables 1 to 49 149027.doc

L SI •108- 201103430 式1.141之化合物,其中化合物之Het與Ar’之組合在各情 況下對應於表B之一列且R1係如在表1至49之任一者中所定義 表 40606至40654 式1.142之化合物,其中化合物之Het與Ar·之組合在各情 況下對應於表B之一列且R1係如在表1至49之任一者中所定義 表 40655至 40703 式1.143之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且R1係如在表1至49之任一者中所定義 表 40704至40752 式1.144之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且R1係如在表1至49之任一者中所定義 表 40753 式1.145之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表 40754 式1.146之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表 40755 式1.147之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表40756 式1.148之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表40757 149027.doc -109· 201103430 式1.149之化合物,其十化合物之此與心,之組合在各情 況下對應於表B之一列 表40758 式1.150之化合物,其中化合物之Het與Ar,之組合在各情 況下對應於表B之一列 表40759 式L151之化合物,其中化合物之Het與Ar,之組合在各情 況下對應於表B之一列 表40760 式1.1 2之化5物,其中化合物之此與心,之組合在各情 況下對應於表B之一列 表40761 式L153之化合物,其中化合物之》^與心,之組合在各情 況下對應於表B之一列 表40762 式L154之化合物,其中化合物之Het與Ar,之組合在各情 況下對應於表B之一列 ^ 表40763L SI •108- 201103430 The compound of formula 1.141, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and R1 is as defined in any of Tables 1 to 49, tables 40606 to 40654. A compound of the formula 1.142, wherein the combination of Het and Ar. of the compound corresponds in each case to one of the columns of Table B and R1 is a compound of the formula: formula: formula 165 to 40703, formula 1.143, as defined in any one of Tables 1 to 49, wherein The combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and R1 is a compound of the formula: formulas 11040 to 40752, formula 1.144, as defined in any of Tables 1 to 49, wherein the compounds are Het and Ar' The combination in each case corresponds to one of the columns of Table B and R1 is a compound of the formula: Formula 4, Formula 1.145 as defined in any one of Tables 1 to 49, wherein the combination of Het and Ar' of the compound corresponds in each case to Table B is a list of compounds of formula 1.146, wherein the combination of Het and Ar' of the compound corresponds in each case to a compound of the formula B, Formula 4, Formula 1.147, wherein the combination of Het and Ar' of the compound is in each case Corresponding to one of the tables B, list 40756, formula 1.1 The compound of 48, wherein the combination of Het and Ar' of the compound corresponds in each case to the compound of the formula 40757 149027.doc-109·201103430, formula 1.149, the combination of the ten compounds and the heart, in each case The compound corresponding to one of the following Table B, list 40758, formula 1.150, wherein the combination of Het and Ar of the compound corresponds in each case to the compound of the formula B 751, formula L 151, wherein the combination of Het and Ar of the compound In each case, corresponding to the list 5 of Table B, the formula 5, the formula 5, wherein the combination of the compound and the heart, in each case corresponds to a compound of the formula B761, formula L153, wherein the compound The combination with the heart, in each case corresponds to the compound of the formula B 762 L154 in Table B, wherein the combination of Het and Ar of the compound corresponds in each case to one of the tables B ^ Table 40763

Het與Ar’之組合在各情 式1.155之化合物,其中化合物之 況下對應於表B之—列 表40764 式L156之化合物’其中化合物之Het與Ar,之組合在各 況下對應於表B之一列 m 表 40765 [S1 149027.doc -110- 201103430 式1.157之化合物 況下對應於表B之一列 表40766 式1.158之化合物,其 ' 況下對應於表B之一列 - 表40767 式1.159之化合物,其 況下對應於表B之一列 表40768 式1.160之化合物,其 況下對應於表B之一列 表 40769 式1.161之化合物,其 況下對應於表B之一列 表40770 式1.162之化合物,其 況下對應於表B之一列 表40771 ; 式1.163之化合物,其 . 況下對應於表B之一列 表40772 式1.164之化合物,其 況下對應於表B之一列 表40773 其中化合物之Het與Ar'之組合在各情 中化合物之Het與Ar'之組合在各情 中化合物之Het與Ar'之組合在各情 中化合物之Het與Ar'之組合在各情 中化合物之Het與Ar’之組合在各情 中化合物之Het與Ar'之組合在各情 中化合物之Het與Ar'之組合在各情 中化合物之Het與Ar1之組合在各情 149027.doc -111 - 201103430 組合在各情 組合在各情 者中所定義 式1.165之化合物,其中化合物之Het與斛,之 況下對應於表B之一列 表40774 中化合物之與Ar,之組合在各情 式1.1 66之化合物,其 況下對應於表B之一列 表40775 式1.167之化合物 ' ,,w 口 v 〜net兴 Ar ^ 況下對應於表B之一列且尺1係如在表丨至49之任 表 40776 中化合物之Het與A_r, 之組合在各情 式1.168之化合物,其 況下對應於表B之一列 表40777 式1.169之化合物,其中化合物 況下對應於表B之一列 』之組合在各情 表40778 式L17〇之化合物,其中化合物之叫與心,之組 況下對應於表B之一列 合慣 表40779 組合在各情 組合在各情 式i.m之化合物,其中化合物之Het與Ar,之 況下對應於表B之一列 表40780 式L172之化合物,其中化合物之Het與Ar,之 況下對應於表B之一列 表40781 149027.doc -112- [S] 201103430 式1.173之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表 40782 式1.174之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且R1係如在表1至49之任一者中所定義 表 40783 式1.175之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表 40784 式1.176之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表40785 式1.177之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表 40786 式1.178之化合物,其中化合物之Het與Af之組合在各情 況下對應於表B之一列 表40787 式1.1 79之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表 40788 式1.180之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表40789 149027.doc -113· 201103430 式1.181之化合物,其中化合物之Het與Ar’之組合在各情 況下對應於表B之一列 表 40790 式1.182之化合物,其中化合物之Het與Ar1之組合在各情 況下對應於表B之一列 表 40791 式1.183之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表40792 式1.184之化合物,其中化合物之Het與Ar’之組合在各情 況下對應於表B之一列 表40793 式1.185之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表 40794 式1.186之化合物,其中化合物之Het與Ar1之組合在各情 況下對應於表B之一列 表 40795 式1.187之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列 表 40796 式1.188之化合物,其中化合物之Het與Ar1之組合在各情 況下對應於表B之一列 表 40797The combination of Het and Ar' in each case 1.155, wherein the compound corresponds to Table B - List 40764 Formula L156 Compound 'Het and Ar of the compound, in each case corresponds to Table B A list of compounds of the formula: formula </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> <RTIgt; In this case, it corresponds to a compound of the formula B60, formula 1.160, in Table B, which corresponds to a compound of the formula B, formula No. 1.161, of Table B, which corresponds to a compound of the formula B. The following corresponds to a list of Table B, list 40771; a compound of formula 1.163, which corresponds to a compound of the list of Table B, Form 40772, formula 1.164, in which case corresponds to a list of Table B, 40773, wherein the compounds are Het and Ar' The combination of Het and Ar' of the compound in each case. The combination of Het and Ar' of the compound in each case. The combination of Het and Ar' of the compound in each case. The combination of Het and Ar' of the compound in each case. In each situation The combination of Het and Ar' in the compound in each case, the combination of Het and Ar' in each case. The combination of Het and Ar1 in each case is combined in each case 149027.doc -111 - 201103430 in each situation. A compound of the formula 1.165, wherein the compound of Het and hydrazine, in the case of a compound of the formula B, and the combination of Ar and the combination of Ar, in the case of the formula, in each case 1.1 66, in the case corresponding to the table A list of B, 40775, a compound of the formula 1.167, and a port v, a net of Ar^, corresponds to one of the tables B, and the ruler 1 is such as Het and A_r of the compound in Table 40776 of Tables 49 to 49, a compound of the formula 1.168, which in any case corresponds to a compound of the formula B777, formula 1.169, wherein the compound corresponds to a column of the table B, in the compound of the formula 40778, formula L17, wherein The compound is called the heart, and the group corresponds to one of the table B. The combination of the table 40779 is combined in each case of the compound of the formula im, in which the compound Het and Ar, in the case of a list of the table B 40780 Compound of formula L172, wherein compound H Et and Ar, in the case of a list of Table B, 40,781, 149,027.doc -112- [S] 201103430, a compound of formula 1.173, wherein the combination of Het and Ar' of the compound corresponds in each case to a list of Table B 40782 Compound of the formula 1.174, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and R1 is a compound of the formula: formula 1.175, as defined in any one of Tables 1 to 49, wherein the compound The combination of Het and Ar' corresponds in each case to the compound of the formula B, formula 1.176, in Table B, wherein the combination of Het and Ar' of the compound corresponds in each case to the compound of the formula 40. Wherein the combination of Het and Ar' of the compound corresponds in each case to the compound of the formula 4078, formula 1.178, wherein the combination of Het and Af of the compound corresponds in each case to one of the lists B, list 40787, formula 1.179. The compound, wherein the combination of Het and Ar' of the compound corresponds in each case to the compound of the formula 40788, formula 1.180, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the tables B. List 40789 149027 .do C-113·201103430 A compound of the formula 1.181 wherein the combination of Het and Ar' of the compound corresponds in each case to the compound of the formula 40790, formula 1.182, wherein the combination of Het and Ar1 of the compound corresponds in each case to a list of compounds of formula 1.183, wherein the combination of Het and Ar' of the compound corresponds in each case to the compound of the formula B, list of formula B, formula 1.184, wherein the combination of Het and Ar' of the compound is in each case Corresponding to a compound of the formula B </ RTI> </ RTI> <RTIgt; </ RTI> </ RTI> <RTIgt; </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> The following corresponds to a compound of the formula Table B, formula: 1.187, wherein the combination of Het and Ar' of the compound corresponds in each case to the compound of the formula 4088, formula 1.188, wherein the combination of Het and Ar1 of the compound is In the case corresponding to one of the tables B list 40797

[SI 149027.doc -114- 201103430 式1.189之化&amp;物,其中化合物之Het與Ar’之組合在各情 況下對應於表B之一列 表 40798 式1.190之化&amp;物,其中化合物之Het與αγ'之組合在各情 況下對應於表B之一列 表40799 式1.191之化&amp;物,其中化合物之Het與αγ·之組合在各情 況下對應於表Β之一歹 表40800 式1.192之化合物,其中化合物之Het與αγ·之組合在各情 況下對應於表Β之一歹I] 表40801 式ΙΙ.1之化合物,其中化合物之r21、r22、r23、r24及 R之組合在各情況下對應於表A之一列,Het為式Het丨之 基團且1113為11 表40802 式II.1之化合物,其中化合物之尺21、r22、r23、r24及 R之組合在各情況下對應於表八之一列,Het為式Het」之 基團且Rla為甲基 表40803 式II.1之化合物,其中化合物之r21、r22、r23、r24及 R之組合在各情況下對應於表A之一列,Het為式Het ^之 基團且Rla為乙基 表40804 · 149027.doc -115· 201103430 式η· 1之化合物,其中化合物之R21、R22、R23、R24及 R25之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且尺13為正丙基 表40805 式II.1之化合物,其中化合物之R21、R22、R23、R24及 2 5 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為異丙基 表40806 式Π·1之化合物,其中化合物之r21、R22、r23、R24及 2 5 R之組合在各情況下對應於表A之一列,Het為式Het. 1之 基團且Rla為正丁基 表 40807 式Π.1之化合物,其中化合物之r21、r22、r23、R24及 2 5 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為第二丁基 表 40808 式II.1之化合物,其中化合物之、r22、R23、R24及 R之組合在各情況下對應於表A之一列,Het為式Het. 1之 基團且1113為異丁基 表 40809 式H.1之化合物,其中化合物之尺21、r22、r23、r24及 R25之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為第三丁基 表 40810[SI 149027.doc -114-201103430 Formula 1.89, the combination of Het and Ar' of the compound, in each case corresponds to the list &lt;RTI ID=0.0&gt;&gt; The combination with αγ' corresponds in each case to the composition &amp; matter of the list 40799, formula 1.191, wherein the combination of Het and αγ of the compound corresponds in each case to one of the expressions, Table 40800, formula 1.192 The compound, wherein the combination of Het and αγ· of the compound corresponds in each case to one of the formulas 歹I] Table 40801 Formula ΙΙ.1, wherein the combination of the compounds r21, r22, r23, r24 and R is in each case The lower one corresponds to one of the columns of Table A, Het is a group of the formula Het丨 and 1113 is 11 the compound of the formula II.1, wherein the combination of the ruler 21, r22, r23, r24 and R of the compound corresponds in each case to In one of Table 8, Het is a group of the formula Het" and Rla is a methyl group 40803. The compound of the formula II.1, wherein the combination of the compounds r21, r22, r23, r24 and R corresponds in each case to Table A. In a column, Het is a group of the formula Het ^ and Rla is an ethyl group 40804 · 149027.doc -115· 20 1103430 A compound of the formula η·1, wherein the combination of R21, R22, R23, R24 and R25 of the compound corresponds in each case to one of the columns of Table A, Het is a group of the formula Het.1 and the ruler 13 is a n-propyl group. 40805 A compound of the formula II.1, wherein the combination of R21, R22, R23, R24 and 2 5 R of the compound corresponds in each case to one of the columns of Table A, Het is a group of the formula Het.1 and Rla is an isopropyl group. Table 40806 Compound of the formula ,1, wherein the combination of the compounds r21, R22, r23, R24 and 2 5 R corresponds in each case to one of the tables A, Het is a group of the formula Het. 1 and Rla is a n-butyl group The compound of the formula 807.1, wherein the combination of the compounds r21, r22, r23, R24 and 2 5 R corresponds in each case to one of the columns of Table A, Het is a group of the formula Het.1 and Rla is Dibutyl form 40808 The compound of formula II.1, wherein the combination of the compound, r22, R23, R24 and R corresponds in each case to one of the tables A, Het is a group of the formula Het. 1 and 1113 is isobutyl Base Table 40809 A compound of the formula H.1 wherein the combination of the compounds 21, r22, r23, r24 and R25 corresponds in each case to one of the tables A, and Het is a formula Het.l Group and Rla is a third butyl group

[SI I49027.doc -116- 201103430 式II.1之化合物,其中化合物之尺2丨、 2 5 R之組合在各情況下對應於表A之一列 基團且Rla為苯基 表40811 式II. 1之化合物,其中化合物之尺2丨、 R之組合在各情況下對應於表A之一列 基團且Rla為苄基 表40812 式IL1之化合物,其中化合物之:R21、 2 5 R之組合在各情況下對應於表A之一列 基團且rU為甲基羰基 表40813 式II. 1之化合物,其中化合物之r2i、 R25之組合在各情況下對應於表A之一列 基團且Rla為乙基羰基 表 40814 式II.1之化合物,其中化合物之R21、 R25之組合在各情況下對應於表A之一列 基團且Rla為丙基羰基 表40815 式II.1之化合物,其中化合物之R21、 R25之組合在各情況下對應於表A之一列 基團且Rla為異丙基羰基 表40816 149027.doc R22、R23、R24及 ,Het為式Het. 1之 R22、R23、R24 及 ,Het為式Het.l之 R22、R23、R24 及 ,Het為式Het.l之 R22、R23、R24 及 ,Het為式Het.l之 R22、R23、R24 及 ,Het為式Het.l之 R22、R23、R24 及 ,Het為式Het. 1之 201103430 式IL 1之化合物,其中化合物之r21、r22、r23、r24及 2 5 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為苯基羰基 表40817 式II.1之化合物,其中化合物之R21、R22、R23、R24及 2 5 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為甲氧羰基 表40818 式II.1之化备物,其中化合物之R21、R22、R23、R24及 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為乙氧羰基 表40819 式Η·1之化合物,其中化合物之R2i、R22、R23、R24及 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為丙氧羰基 表40820 式II.1之化合物,其中化合物之R21、R22、R23、R24及 R之組合在各情況下對應於表A之一列,Het為式Het. 1之 基團且Rla為異丙氧羰基 表40821 式II.1之化合物,其中化合物之尺21、R22、R23、R24及 R25之組合在各情況下對應於表A之一列’ Het為式Het.l之 基團且Rla為笨氧羰基 表40822[SI I49027.doc -116- 201103430 The compound of the formula II.1, wherein the combination of the compound of the formula 2丨, 2 5 R corresponds in each case to a group of the group A and Rla is a phenyl group 40811 formula II. A compound of 1, wherein the combination of the ruthenium 2, R of the compound corresponds in each case to a group of the group A and Rla is a compound of the formula benzyl group 40812, wherein the combination of the compound: R21, 2 5 R In each case, a group corresponding to one of the columns of Table A and rU is a methylcarbonyl group 40813. The compound of formula II.1, wherein the combination of the compounds r2i, R25 corresponds in each case to one of the groups of Table A and Rla is B. A compound of the formula II.1 wherein the combination of R21 and R25 of the compound corresponds in each case to a group of the group A and Rla is a compound of the formula propylcarbonyl group 40815, wherein the compound R21 The combination of R25 corresponds to one of the groups in Table A in each case and Rla is isopropylcarbonyl table 40816 149027.doc R22, R23, R24 and Het is R22, R23, R24 and Het of the formula Het. R22, R23, R24 and Het of the formula Het.l, R22, R23, R24 and Het of the formula Het.l R22, R23, R24 of the formula Het.l and Het are R22, R23, R24 of the formula Het.l and Het is a compound of the formula Het. 1 of 201103430 of the formula IL1, wherein the compound is r21, r22, r23, r24 And the combination of 2 5 R corresponds in each case to one of the columns of Table A, Het is a group of the formula Het.1 and Rla is a compound of the formula phenylcarbonyl 40817 formula II.1, wherein the compound is R21, R22, R23, The combination of R24 and 2 5 R corresponds in each case to one of the tables A, Het is a group of the formula Het.1 and Rla is a methoxycarbonyl table 40818. The compound of the formula II.1, wherein the compound R21, R22 The combination of R23, R24 and R corresponds in each case to one of the columns of Table A, Het is a group of the formula Het.1 and Rla is a compound of the formula ethoxylate carbonyl group 40819, wherein the compound R2i, R22, The combination of R23, R24 and R corresponds in each case to one of the columns of Table A, Het is a group of the formula Het.1 and Rla is a compound of the formula (II) of the propoxycarbonyl table 40820, wherein the compound is R21, R22, R23 The combination of R24 and R corresponds in each case to one of the columns of Table A, Het is a group of the formula Het. 1 and Rla is a compound of the formula isopropoxycarbonyl table 40821 of the formula II. The combination of the ruthenium 21, R22, R23, R24 and R25 in each case corresponds to one of the columns of Table A. Het is a group of the formula Het.l and Rla is an oxocarbonyl group.

[SI 149027.doc -118- 201103430 式Π.1之化合物,其中化合物之R21.、 R25之組合在各情況下對應於表A之一列 基團且Rla為甲基胺基羰基 表 40823 式II.1之化合物’其中化合物之r2〗、 R25之組合在各情況下對應於表A之一列 基團且Rla為乙基胺基羰基 表40824 式II.1之化合物,其中化合物之r2i、 R25之組合在各情況下對應於表A之一列 基團且111&amp;為丙基胺基羰基 表40825 式II. 1之化合物,其中化合物之r2 1、 R25之組合在各情況下對應於表A之一列 基團且Rla為異丙基胺基羰基 表40826 式II. 1之化合物,其中化合物之r2i、 R25之組合在各情況下對應於表A之一列 基團且1^&amp;為苯基胺基羰基 表40827 式II.1之化合物,其中化合物之R21、 R25之組合在各情況下對應於表A之一列 基團且Rla為甲磺醯基 表40828 R22、R23、R24及 ,Het為式Het. 1之 R22、R23、R24 及 ,Het為式Het. 1之 R22、R23、R24 及 ,Het為式Het.1之 R22、R23、R24 及 ,Het為式Het.l之 R22、R23、R24 及 ,Het為式 Het. 11 R22、R23 H ,Het為式 Het. 11 149027.doc •119- 201103430 式Π·1之化合物,其中化合物之R21、r22、r23、r24及 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為乙磺醯基 表40829 式II.1之化合物,其中化合物之R21、R22、R23、R24及 R25之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Ru為丙磺醯基 表40830 式II.1之化合物,其中化合物之尺2丨、R22、R23、R24及 2 5 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且R為異丙績醯基 表40831 式II.1之化合物,其中化合物之r21、R22、R23、R24及 R之組合在各情況下對應於表A之一列,Het為式Het. 1之 基團且Rla為笨磺醯基 表 40832 式II.1之化合物,其中化合物之r21、r22、R23 ' R24及 2 5 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為曱氧磺醯基 表40833 式II.1之化合物’其中化合物之r21、R22、R23、R24及 2 3 R之組合在各情況下對應於表A之一列,Het為式Het.l之 基團且Rla為乙氧磺醯基 表40834[SI 149027.doc -118-201103430 A compound of the formula 1.1, wherein the combination of R21. and R25 of the compound corresponds in each case to a group of the group A and Rla is a methylaminocarbonyl group 40823. The compound of 1 wherein the combination of the compound r2 and R25 corresponds in each case to a group of the group A and Rla is an ethylaminocarbonyl group 40824. The compound of the formula II.1, wherein the combination of the compound r2i, R25 In each case corresponds to a group of the table A and 111 &amp; is a propylaminocarbonyl table 40825. The compound of formula II.1, wherein the combination of the compounds r2 1 , R25 corresponds in each case to one of the columns of Table A And Rla is an isopropylaminocarbonyl group 40826. The compound of formula II.1, wherein the combination of the compound r2i, R25 corresponds in each case to one of the groups listed in Table A and 1^&amp; is phenylaminocarbonyl Table 40827. The compound of formula II.1, wherein the combination of R21 and R25 of the compound corresponds in each case to one of the groups of Table A and Rla is methylsulfonyl. Tables 40828 R22, R23, R24 and Het are of the formula Het. 1 R22, R23, R24 and Het are R22, R23, R24 and Het. 1 and Het is H R22, R23, R24 and Et.1, Het is R22, R23, R24 of the formula Het.l, Het is of the formula Het. 11 R22, R23 H, Het is the formula Het. 11 149027.doc •119- 201103430 A compound of Π·1, wherein the combination of R21, r22, r23, r24 and R of the compound corresponds in each case to one of the columns of Table A, Het is a group of the formula Het.1 and Rla is an ethylsulfonyl group 40829 A compound of II.1, wherein the combination of R21, R22, R23, R24 and R25 of the compound corresponds in each case to one of the columns of Table A, Het is a group of the formula Het.1 and Ru is a propioninyl group 40830 The compound of II.1, wherein the combination of the ruthenium 2, R22, R23, R24 and 2 5 R of the compound corresponds in each case to one of the tables A, Het is a group of the formula Het.1 and R is an isopropyl group.醯基表40831 A compound of the formula II.1, wherein the combination of the compounds r21, R22, R23, R24 and R corresponds in each case to one of the tables A, Het is a group of the formula Het. 1 and Rla is a sulphur醯基表40832 A compound of the formula II.1 wherein the combination of the compounds r21, r22, R23' R24 and 2 5 R corresponds in each case to one of the columns of Table A, Het is a group of the formula Het.1 and Rla is曱Oxysulfonyl group 40833 Compound of formula II.1 wherein the combination of compounds r21, R22, R23, R24 and 2 3 R corresponds in each case to one of Table A, and Het is a group of formula Het. Rla is ethoxysulfonyl table 40834

i SI 149027.doc •120- 201103430 式II.1之化合物,其中化合物之r21、r22、r23、R24及 2 5 R之組合在各情況下對應於表A之一列,Het為式Het. 1之 基團且Rla為丙氧磺醯基 表40835 式11 ·1之化合物,其中化合物之R2丨、R22、R23、R24及 2 5 R之組合在各情況下對應於表A之一列,Het為式Het.i之 基團且1113為異丙氧績酿基 表40836 式II. 1之化合物,其中化合物之r21、r22、r23、R24及 R25之組合在各情況下對應於表A之一列,Het為式Het. 1之 基團且Rla為苯氧磺醯基 表40837 式II. 1之化合物,其中化合物之r21、r22、R23、R24及 R25之組合在各情況下對應於表A之一列,Het為式Het. 1之 基團且Rla為CN 表40838至40874 式II.1之化合物,其中化合物之、r22、r23、R24及 R25之組合在各情況下對應於表a之一列,R1 a係如在表 : 40800至4083 7之任一者中所定義且Het為式Het.2之基團 表40875至40911 式II.1之化合物,其中化合物之R21、R22、R23、r24及 R25之組合在各情況下對應於表A之一列,尺13係如在表 40800至40837之任一者中所定義且Het為式Het.3之基團 表40912至40948 -121- 149027.doc 201103430 式II.1之化合物, R25之組合在各情况 40800至 40837之任一 表40949至40985 其中化合物之R21、R22、R23、R24及 下對應於表A之一列,R1 a係如在表 者中所定義且Het為式Het.4之基團 式II.1之化合物,美 R25之組合在各情況不 40800至 40837之任# 表40986至41022 中化合物之R21、R22、R23、R24及 對應於表A之一列,Rla係如在表 中所定義且Het為式Het.5之基團 式Π.1之化合物,复 R25之組合在各情况了 40800至40837之任一者 表41023至41059 中化合物之R2】、R22、R23、R24及 對應於表A之一列,1113係如在表 中所定義且Het為式Het.6之基團 式Η · 1之化合物, R25之組合在各情況 40800至 40837之任一 表41060至41096 其中化合物之R21、R22、R23、R24及 下對應於表A之一列,111&amp;係如在表 者中所定義且Het為式Het.7之基團 式II· 1之化合物, R25之組合在各情況 40800至 40837之任-~ 表41097至41133 其申化合物之R21、R22、R23、R24及 下對應於表A之一列,11丨3係如在表 者中所定義且Het為式Het.8之基團 式ii.i之化合物,其中化合物之rZ1、R22、R23、r24及 R”之組合在各情况下對應於表A之一列,rU係如在表 40800至40837之任〜去士 π a β L 者中所定義且Het為式Het.9之基團表41134至41170 149027.doci SI 149027.doc • 120- 201103430 The compound of the formula II.1, wherein the combination of the compounds r21, r22, r23, R24 and 2 5 R corresponds in each case to one of the tables A, and Het is a formula Het. a group and Rla is a compound of the formula propyl sulfonyl group 40835, wherein the combination of R 2 丨, R 22 , R 23 , R 24 and 2 5 R of the compound corresponds in each case to one of the columns of Table A, and Het is a formula a group of Het.i and 1113 is a compound of the formula iodine 40836, formula II. 1, wherein the combination of the compounds r21, r22, r23, R24 and R25 corresponds in each case to one of the tables A, Het Is a group of the formula Het. 1 and Rla is a phenoxysulfonyl group 40837. A compound of the formula II.1, wherein the combination of the compounds r21, r22, R23, R24 and R25 corresponds in each case to one of the tables A. Het is a group of the formula Het. 1 and Rla is a compound of the formula 40838 to 40874 of the formula II.1, wherein the combination of the compounds, r22, r23, R24 and R25 corresponds in each case to one of the tables a, R1 a A compound of the formula II.1, wherein the compound is as defined in any of the formulas: 40800 to 4083, and Het is a group of the formula Het. 2, formula 40875 to 40911, wherein the compound The combination of R21, R22, R23, r24 and R25 corresponds in each case to one of the columns of Table A, which is as defined in any of Tables 40800 to 40837 and Het is a group table 40912 of the formula Het. To 40948 -121- 149027.doc 201103430 The compound of formula II.1, the combination of R25 in any of the cases 40800 to 40837, the table 40949 to 40985 wherein the compound R21, R22, R23, R24 and below correspond to one of the tables A , R1 a is as defined in the table and Het is a compound of the formula II.1 of the formula Het.4, and the combination of the beauty R25 is not 40800 to 40837 in each case# R21 of the compound in Table 40986 to 41022 , R22, R23, R24 and corresponding to one of the tables A, Rla is as defined in the table and Het is a compound of the formula Π.1 of the formula Het.5, and the combination of the complex R25 is 40800 to 40837 in each case. R2, R22, R23, R24 of the compound in any of the tables 41023 to 41059 and corresponding to one of the tables A, 1113 is as defined in the table and Het is a group of the formula Het. 6 1 1 The compound, R25 combination, in any of the cases 40800 to 40837, each of the tables 41060 to 41096, wherein the compound R21, R22, R23, R24 and the corresponding In one of the tables A, 111 &amp; is as defined in the Table and Het is a compound of the formula II.1 of the formula Het.7, and the combination of R25 is in any case 40800 to 40837 - Table 41097 to 41133 Its compound R21, R22, R23, R24 and the lower corresponding to one of the tables A, 11丨3 are as defined in the table and Het is a compound of the formula ei.i of the formula Het.8, wherein the compound The combination of rZ1, R22, R23, r24 and R" corresponds in each case to one of the columns of Table A, and the rU is as defined in the table 40800 to 40837, and the formula is Het π a β L and Het is the formula Het .9 group table 41134 to 41170 149027.doc

LSI -122· 201103430 式IL1之化合物,其中化合物之R21、R22、R23、R24及 R25之組合在各情況下對應於表A之-列,C係如在表 40800至 40837之任一去 士 &amp; 有中所定義且Het為式Het.10之基團 表41171至41207 式Π_1之化合物,其中化合物之R2丨、R22、R23、R24及 R25之組合在各情況下對應於表A之一列,Rla係如在表 40800至4083 7之任-者中所定義且㈣為式此」i之基團 表41208至41244 式II.1之化合物,其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表八之一列,Rla係如在表 40800至40837之任一者中所定義且Het為式Het.12之基團 表41245至41281 式II.1之化合物’其中化合物之r21、r22、r23、r24及 R之組合在各情況下對應於表A之一列,Rla係如在表 40800至40837之任一者中所定義且Het為式Het_13之基團 表41282至41318 式IL1之化合物,其中化合物之R21、R22、R23、R24及 R25之組合在各情況下對應於表A之一列,Rla係如在表 40800至4083 7之任一者中所定義且Het為式Het.丨4之基團 表41319至41355 式II.1之化合物,其中化合物之r21、R22、R23、r24及 R25之組合在各情況下對應於表A之一列,Rla係如在表 40800至40837之任—者中所定義且Het為式Het. 15之基團 表41356至41392 149027.doc -123- 201103430 式II.1之化合物,其中化合物之尺21、r22、r23、r24及 R25之組合在各情況下對應於表八之一列,Rla係如在表 40800至40837之任一者中所定義且Het為式HeM6之基團 表41393至41984 式II.2之化合物,其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表八之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表41985至42576 式II.3之化合物,其中化合物之R21、R22、r23、r24及 R25之組合在各情況下對應於表A之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表42577至43168 式Π·4之化合物,其中化合物之R2丨、R22、R23、r24及 R25之組合在各情況下對應於表八之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表43169至43760 式II.5之化合物,其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表八之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表43761至44352 式II.6之化合物,其中化合物之r21、r22、尺23、r24及 R25之組合在各情況下對應於表八之一列且Rla與Hu之組合 係如表40800至41392之任一者中所定義 表 44353至44944 149027.doc •124· 201103430 式II.7之化合物,其中化合物之R2丨、R22、r23、r24及 R25之組合在各情況下對應於表A之一列且與Het之組合 係如表40800至41392之任一者中所定義 表 44945至 45536 式II.8之化合物,其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表八之一列且Rla與之組合 係如表4 0 8 0 0至413 9 2之任者中所定義 表45537至46128 式II.9之化合物,其中化合物之R21、R22、r23、尺24及 R之組合在各情況下對應於表A之一列且11丨3與1^丨之組合 係如表40800至41 392之任一者中所定義 表46129至46720 式11.1〇之化合物,其中化合物之尺21、尺22、尺23、尺24及 R25之組合在各情況下對應於表八之一列且Rla與之組合 係如表40800至4 1392之任一者中所定義 表46721至47312LSI-122·201103430 A compound of the formula IL1, wherein the combination of the compounds R21, R22, R23, R24 and R25 corresponds in each case to the column of Table A, and the C system is as in any of the forms 40800 to 40837. And a compound of the formulae 41171 to 41207 of the formula Het.10, wherein the combination of R2丨, R22, R23, R24 and R25 of the compound corresponds in each case to one of the tables A, Rla is as defined in any of the tables 40800 to 4083, and (d) is a compound of the formula 41208 to 41244 of the formula II.1, wherein the compounds are r21, r22, r23, r24 and R25 The combination corresponds in each case to one of the columns of Table 8, Rla is as defined in any of Tables 40800 to 40837 and Het is a group of the formula Het. 12, Tables 41245 to 41281, a compound of the formula II.1 The combination of r21, r22, r23, r24 and R corresponds in each case to one of the columns of Table A, Rla is as defined in any of Tables 40800 to 40837 and Het is a group table 41282 to 41318 of the formula Het_13 A compound of the formula IL1, wherein the combination of the compounds R21, R22, R23, R24 and R25 corresponds in each case to Table A In one column, Rla is as defined in any one of Tables 40800 to 4083, and Het is a group of formulas 41419 to 41355 of the formula Het.丨4, a compound of the formula II.1, wherein the compound is r21, R22, R23, r24 And the combination of R25 corresponds in each case to one of the columns of Table A, Rla is as defined in any of Tables 40800 to 40837 and Het is a group of the formula Het. 15 Table 41356 to 41392 149027.doc -123- 201103430 A compound of the formula II.1, wherein the combination of the compounds 21, r22, r23, r24 and R25 corresponds in each case to one of the columns of Table 8, and Rla is as defined in any of Tables 40800 to 40837 and Het is a compound of the formula HeM6, in the group of 41,393 to 4,1984, a compound of the formula II.2, wherein the combination of the compounds of r21, r22, r23, r24 and R25 corresponds in each case to one of the columns of Table 8 and the combination of Rla and Het is as Tables 41985 to 42576, the compounds of formula II.3, as defined in any of Tables 40800 to 41392, wherein the combination of R21, R22, r23, r24 and R25 of the compound corresponds in each case to one of Table A and Rla and Het The combination of the compounds of the formulas 42577 to 43168, as defined in any of Tables 40800 to 41392, of the formula ,·4, The combination of R2丨, R22, R23, r24 and R25 of the compound corresponds in each case to one of the columns of Table 8 and the combination of Rla and Het is as defined in any of Tables 40800 to 41392, as defined in Tables 43169 to 43760, Formula II. a compound of 5, wherein the combination of r21, r22, r23, r24 and R25 of the compound corresponds in each case to one of the columns of Table 8 and the combination of Rla and Het is as shown in Table 43761 as defined in any of Tables 40800 to 41392. 44352 A compound of the formula II.6, wherein the combination of the compounds r21, r22, 尺23, r24 and R25 corresponds in each case to one of the columns of Table 8 and the combination of Rla and Hu is as in any of Tables 40800 to 41392. Tables 44353 to 44944 149027.doc • 124· 201103430 Compounds of the formula II.7, wherein the combination of R 2 丨, R 22 , r 23 , r 24 and R 25 of the compounds corresponds in each case to one of the columns of Table A and in combination with Het A compound of the formula II.8 as defined in any one of Tables 40800 to 41392, wherein the combination of the compounds r21, r22, r23, r24 and R25 corresponds in each case to one of the columns of Table 8 and Rla The combination is as defined in Table 4 0 0 0 0 to 413 9 2 45537至46128 A compound of the formula II.9, wherein the combination of the compounds R21, R22, r23, quaternary 24 and R corresponds in each case to one of the columns of Table A and the combination of 11丨3 and 1丨 is as shown in Table 40800. A compound of the formulae 11.129 to 46720, formula 11.1, as defined in any one of 41,392, wherein the combination of the ruler 21, ruler 22, ruler 23, ruler 24 and R25 of the compound corresponds in each case to one of the columns of Table 8 and Rla and The combination is as defined in any of Tables 40800 to 4 1392, tables 46721 to 47312

列且1113與Het之組合 式11.11之化合物,其中化合物之r R25之組合在各情況下對應於表A之一歹 係如表40800至4丨392之任一者中所定義 表 47313至47904 、R 、R23、R24及 列且R1 a與Het之組合 式II.12之化合物,其中化合物之rS1 R之組合在各情況下對應於表A之一歹i 係如表4〇8〇0至41392之任一者中所定義 表47905至48496 149027.doc -125- 201103430 式11.13之化合物,其中化合物之112丨、1122、1123、尺24及 R25之組合在各情況下對應於表八之一列且1^3與11以之組合 係如表40800至41392之任一者中所定義 表48497至49088 式11.14之化合物,其中化合物之尺2丨、尺22、尺23、尺24及 R25之組合在各情況下對應於表八之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表 49089至 49680 式11.15之化合物,其中化合物之r21、r22、r23、尺24及 R25之組合在各情況下對應於表A之一列且Rla與之組合 k如表40800至41392之任—者中所定義 表 49681 至 50272 式Π.16之化合物,其中化合物之R2丨、R22、R23、R24及 R25之組合在各情況下對應於表八之—列且Rla與此之組合 係如表40800至41392之任'一者中所定義 表50273至50864 式11.17之化合物,其中化合物之1121、尺22、尺23、尺24及 R25之組合在各情況下對應於表八之—列且R】a與此之組合 係如表40800至41 392之任一者中所定義 表50865至51456 式仄^之化合物’其中化合物之“丨^^^^尺以及 R25之組合在各情況下對應於表八之一列且Rla與細之組合 係如表40800至41 392之任一者中所定義 表 51457至 52048 149027.doc •126- 201103430 式11.19之化合物,其中化合物之尺21、1122、尺23、尺24及 R25之組合在各情況下對應於表A之一列且Rla與之組合 係如表40800至41;392之任一者中所定義 表52049至52640 式Η·20之化合物,其中化合物之R21、R22、r23、R24及 ; R25之組合在各情況下對應於表Λ之一列且R丨a與Het之組合 係如表40800至41392之任一者中所定義 表 52641至 53232 式Π·21之化合物,其中化合物之R21、R22 ' R23、r24及 R25之組合在各情況下對應於表八之一列且Rla與ΗΜ之組合 係如表40800至41392之任一者中所定義 表 53233至 53824 式IL22之化合物,其中化合物之r21、r22、r23、尺24及 R25之組合在各情況下對應於表八之一列且Rla與之組合 係如表40800至41392之任一者中所定義 表53825至54416 式Π.23之化合物,其中化合物之R2〗、R22、R23、R24及 R2 5之組合在各情況下對應於表A之一列且R丨a與h e丨之組合 係如表40800至41392之任一者中所定義 表54417至55008 式Π.24之化合物,其中化合物之R2〗、R22、R23、r24及 R25之組合在各情況下對應於表八之一列且Rla與之組合 係如表40800至41392之任一者中所定義 表55009至55600 149027.doc ^ 127- 201103430 式II.25之化合物,其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表A之一列且RU與Het之組合 係如表40800至41392之任一者中所定義 表 55601 至56192 式11.26之化合物,其中化合物之尺21、尺22、尺23、尺24及 R之組合在各情況下對應於表八之一列且之組合 係如表40800至41392之任一者中所定義 表 56193至 56784 式11.27之化合物,其中化合物之1121、1122、汉23、尺24及 R25之組合在各情況下對應於表八之一列且Rla與之組合 係如表40800至41392之任一者中所定義 表56785至57376 式11.28之化合物,其中化合物之1121、1122、尺23、尺24及 R25之組合在各情況下對應於表八之一列且Rla與ΗΜ之組合 係如表40800至41392之任一者中所定義 表57377至57968 式Π_29之化合物,其中化合物之R21、R22、R23、r24及 R25之組合在各情況下對應於表八之一列且Rla與此之組合 係如表40800至41392之任一者中所定義 表 57969至 58560 式Π·30之化合物,其中化合物之R21、R22、R23、R24及 R25之組合在各情況下對應於表八之一列且Rla與此之組合 係如表40800至41392之任一者中所定義 表 58561 至59152 149027.doc [S1 -128· 201103430 式II.3 1之化合物’其令化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表八之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表 59153至 59744 式11.32之化合物,其中化合物之r21、r22、r23、r24及 ' R之組合在各情況下對應於表A之一列且尺^與只以之組合 係如表40800至41392之任^一者中所定義 表59745至60336 式11.33之化合物,其中化合物之尺21、R22、r23、r24及 R25之組合在各情況下對應於表八之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表60337至60982 式Π.34之化合物,其中化合物之R21、R22、R23、r24及 R之組合在各情況下對應於表人之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表60983至61520 式11.35之化合物,其中化合物之尺2丨、r22、r23、尺以及 R25之組合在各情況下對應於表八之一列且Rla與Het之組合 係如表40800至413 92之任一者中所定義 - 表61521至62112 式Π·36之化合物,其中化合物之R21、R22、R23、r24及 R25之組合在各情況下對應於表八之一列且Rla與之組合 係如表40800至41392之任一者中所定義 表62113至62704 149027.doc •129- 201103430 式11.37之化合物,其中化合物之r21、r22、r23、r24及 R 5之組合在各情況下對應於表A之一列且Rl a與Het之組合 係如表40800至41392之任一者中所定義 表62705至63296 式11.38之化合物’其中化合物之|^21、尺22、尺23、尺24及 R25之組合在各情況下對應於表A之一列且Ru與Het之組合 係如表40800至41392之任一者中所定義 表63297至63888 式11.39之化合物,其中化合物之尺2丨、R22、r23、r24及 R 5之組合在各情況下對應於表A之一列且Rla與之組合 係如表40800至41;392之任一者中所定義 表 63889至 64480 式11.40之化合物,其中化合物之r21、r22、r23、r24及 R之組合在各情況下對應於表A之一列且尺1&amp;與Het之組合 係如表40800至41392之任一者中所定義 表4481至 65072 式11.41之化合物,其中化合物之r21、r22、r23、尺24及 R25之組合在各情況下對應於表八之一列且Rla與之組合 係如表40800至41392之任一者中所定義 表 65073至65664 式11.42之化合物,其中化合物之尺21、尺22、尺23、尺24及 R25之組合在各情況下對應於表八之一列且Rla與Hu之組合 係如表40800至41392之任一者中所定義 表 65 665 至 66256 J49027.doc ί S1 •130· 201103430 式Π.43之化合物,其中化合物之R21、R22、R23、R24及 R25之組合在各情況下對應於表入之一列且Rla與叫之組合 係如表40800至41392之任一者中所定義 表66257至66848 式Π.44之化合物,其中化合物之R21、R22 ' R23、R24及 R25之組合在各情況下對應於表蚊—列且Rla與此之組合 係如表40800至41392之任一者中所定義 表 66849至 67440 式11.45之化合物,其中化合物之尺21、尺22、尺23、尺24及 R25之組合在各情況下對應於表八之一列且Rla與之組合 係如表4〇800至41392之任一者中所定義 表67441至68032 式11.46之化合物,其中化合物之R2!、R22、r23、R24及 R25之組合在各情況下對應於表A之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表68033至68624 式11.47之化合物,其中化合物之尺21、r22、r23、r24及 R之組合在各情況下對應於表八之一列且Rla與之組合 係如表4 0 8 0 0至413 9 2之任—者中所定義 表68625至69216 式11.48之化合物’其中化合物之r21、r22、r23、r24及 R25之組合在各情況下對應於表八之一列且Rla與Het之組合 係如表40800至41392之任一者中所定義 表69217至69253 149027.doc 131 · 201103430 式II.49之化合物,其中化合物之Het與Ar’之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69254至69290 式11.50之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 69291 至 69327 式II.51之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69328至69364 式II.52之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69365至69401 式II.53之化合物,其中化合物之Het與Ar'之组合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69402至69438 式II.54之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至4083 7之任一者 中所定義 表69439至69475And a combination of compounds of formula 11.11, wherein the combination of compounds R1, in each case corresponds to one of Tables A, such as Tables 47013 to 47904, as defined in any of Tables 40800 to 4,392, R, R23, R24 and the combination of R1 a and Het, the compound of formula II.12, wherein the combination of the compound rS1 R corresponds in each case to one of the tables A, as shown in Table 4〇8〇0 to 41392 A compound of the formula 11.13, wherein the combination of 112丨, 1122, 1123, 尺 24 and R25 of the compound corresponds in each case to one of the tables and is defined in any one of the following Tables 47905 to 48496 149027.doc -125-201103430 The combination of 1^3 and 11 is a compound of the formulae 48497 to 49088, formula 11.14, as defined in any of the forms 40800 to 41392, wherein the combination of the ruler 2, the ruler 22, the ruler 23, the ruler 24 and the R25 of the compound is In each case, corresponding to one of the columns of Table 8 and the combination of Rla and Het is a compound of the formula 11.089 to the formula 11.15 as defined in any of the forms 40800 to 41392, wherein the compound is r21, r22, r23, ruler 24 and R25. The combination in each case corresponds to one of the columns of Table A and Rla is combined with k as shown in Table 40800 41392 to 50272, a compound of the formula 1616, wherein the combination of R2丨, R22, R23, R24 and R25 of the compound corresponds in each case to the column of Table 8 and Rla The combination is a compound of the formulae 50273 to 50864 of the formula 11.17 as defined in any one of the tables 40800 to 41392, wherein the combination of the compound 1121, the ruler 22, the ruler 23, the ruler 24 and the R25 corresponds in each case to the table - The combination of R and a is a combination of the compounds of the formula 50865 to 51456 as defined in any of the forms 40800 to 41 392, wherein the compound "之^^^^" and the combination of R25 In the case of a column corresponding to one of the Tables and a combination of Rla and fine, as defined in any of Tables 40800 to 41 392, the formula 51457 to 52084 149027.doc • 126-201103430, the compound of the formula 11.19, wherein the compound is 21 The combination of 1122, ruler 23, ruler 24 and R25 corresponds in each case to one of the columns of Table A and Rla is combined therewith as shown in any of Tables 40800 to 41; 392, Tables 52049 to 52640, Η 20 a compound in which a combination of the compounds R21, R22, r23, R24 and R25 is in each case The following corresponds to one of the columns and the combination of R丨a and Het is a compound of the formula 52641 to 53232, which is defined in any one of Tables 40800 to 41392, wherein the compound is R21, R22 'R23, r24 and The combination of R25 corresponds in each case to one of the columns of Table 8 and the combination of Rla and hydrazine is a compound of the formula IL32 as defined in any of Tables 40800 to 41392, wherein the compound is r21, r22, r23, The combination of rule 24 and R25 corresponds in each case to one of the columns of Table 8 and Rla is combined with a compound of the formula 53823 to 54416 of the formula Π.23 as defined in any of Tables 40800 to 41392, wherein the compound R2 The combination of R22, R23, R24 and R2 5 corresponds in each case to one of the columns of Table A and the combination of R丨a and he丨 is as defined in any of Tables 40800 to 41392, as shown in Tables 54417 to 55008. a compound of 24, wherein the combination of R2, R22, R23, r24 and R25 of the compound corresponds in each case to one of the columns of Table 8 and Rla is combined therewith in Tables 55009 as defined in any of Tables 40800 to 41392. 55600 149027.doc ^ 127- 201103430 Compound of formula II.25, wherein the compound The combination of r21, r22, r23, r24 and R25 corresponds in each case to one of the columns of Table A and the combination of RU and Het is a compound of the formulae 55601 to 56192, formula 11.26, as defined in any of Tables 40800 to 41392, Wherein the combination of the ruler 21, ruler 22, ruler 23, ruler 24 and R of the compound corresponds in each case to one of the columns of Table 8 and the combination is as defined in any of Tables 40800 to 41392, Table 56193 to 56784, Equation 11.27 a compound wherein the combination of the compounds 1121, 1122, han 23, ul. 24 and R25 corresponds in each case to one of the columns of Table 8 and Rla is in combination with Table 56785 as defined in any of Tables 40800 to 41392. 57376 A compound of the formula 11.28, wherein the combination of the compounds 1121, 1122, 23, 24 and R25 corresponds in each case to one of the columns of Table 8 and the combination of Rla and hydrazine is as in any of Tables 40800 to 41392. Table 57377 to 57968 Compounds of the formula 2929, wherein the combination of R21, R22, R23, r24 and R25 of the compound corresponds in each case to one of the columns of Table 8 and the combination of Rla and any of them is as shown in any of Tables 40800 to 41392. Table 57969 to 58560 defined in the formula Π·30 A compound wherein the combination of R21, R22, R23, R24 and R25 of the compound corresponds in each case to one of the columns of Table 8 and the combination of Rla and the combination is as defined in any of Tables 40800 to 41392, tables 58561 to 59152 149027 .doc [S1 -128· 201103430 Compound of formula II.3 1] wherein the combination of r21, r22, r23, r24 and R25 of the compound corresponds in each case to one of the columns of Table 8 and the combination of Rla and Het is as shown in the table. A compound of the formulae 59153 to 59734, formula 11.32, as defined in any one of 40,800 to 41,392, wherein the combination of the compounds of r21, r22, r23, r24 and 'R, in each case corresponds to one of the columns of Table A and is only The combination is a compound of the formula: 51,945 to 60,336, formula 11.33, as defined in any of Tables 40800 to 41392, wherein the combination of the ruler 21, R22, r23, r24 and R25 of the compound corresponds in each case to one of the columns of Table 8. And a combination of Rla and Het is a compound of the formula 60337 to 60982 of the formula 34.34 as defined in any one of Tables 40800 to 41392, wherein the combination of the compounds R21, R22, R23, r24 and R corresponds in each case to One of the listed persons and the combination of Rla and Het is shown in Tables 40800 to 41. Table 60983 to 61520, a compound of formula 11.35, as defined in any one of 392, wherein the combination of the ruthenium 2, r22, r23, ruthenium and R25 of the compound corresponds in each case to one of the columns of Table 8 and the combination of Rla and Het As defined in any of Tables 40800 to 413 92 - Tables 61521 to 62112 are compounds of the formula 36 wherein the combination of R21, R22, R23, r24 and R25 of the compound corresponds in each case to one of Tables 8 and Rla is in combination with a compound of the formula: 62113 to 62704 149027.doc • 129-201103430, which is a compound of the formula 11.37, wherein the combination of the compounds r21, r22, r23, r24 and R 5 is In the case of a column corresponding to one of the tables A and the combination of Rl a and Het is a compound of the formulae 62705 to 63296 of the formula 11.38 as defined in any one of the tables 40800 to 41392, wherein the compound|^21, the ruler 22, the ruler 23, The combination of Rule 24 and R25 corresponds in each case to one of the columns of Table A and the combination of Ru and Het is a compound of the formulae 13.297 to 63888 of the formula 11.39 as defined in any of Tables 40800 to 41392, wherein the compound has a size of 2丨, the combination of R22, r23, r24 and R 5 corresponds in each case A compound of the formulae 63889 to 64480, formula 11.40, as defined in any one of Tables 40800 to 41; 392, wherein the combination of the compounds r21, r22, r23, r24 and R is In the case of a combination of Table A and the combination of Ruler 1&amp; and Het are the compounds of Tables 4481 to 65072, formula 11.41, as defined in any of Tables 40800 to 41392, wherein the compounds are r21, r22, r23, ruler 24 and The combination of R25 corresponds in each case to one of the columns of Table 8 and Rla is combined with a compound of the formula 65073 to 65564, formula 11.42 as defined in any of Tables 40800 to 41392, wherein the compound has a ruler 21, a ruler 22, and a ruler. 23, the combination of ruler 24 and R25 corresponds in each case to one of the columns of Table 8 and the combination of Rla and Hu is as defined in any of Tables 40800 to 41392. Table 65 665 to 66256 J49027.doc S S1 • 130· 201103430 A compound of the formula 43 wherein the combination of R21, R22, R23, R24 and R25 of the compound corresponds in each case to one of the columns and the combination of Rla and the combination is as in any of the forms 40800 to 41392. Define compounds of formulas 66257 to 66848, Π.44, wherein The combination of R21, R22 'R23, R24 and R25 in each case corresponds to the species of the genus Mosquito and the combination of Rla and the combination of the compounds defined in Tables 40800 to 41392, as defined in any of Tables 40800 to 41392, of the formula 11.45 , wherein the combination of the ruler 21, the ruler 22, the ruler 23, the ruler 24 and the R25 of the compound corresponds in each case to one of the columns of Table 8 and the combination of Rla is as defined in any of Tables 4 to 800 to 41392. 67441 to 68032 A compound of the formula 11.46 wherein the combination of R2!, R22, r23, R24 and R25 of the compound corresponds in each case to one of the columns of Table A and the combination of Rla and Het is as in any of Tables 40800 to 41392. Tables 68033 to 68624 are defined as compounds of formula 11.47, wherein the combination of the compounds 21, r22, r23, r24 and R corresponds in each case to one of the columns of Table 8 and Rla is combined therewith as shown in Table 4 0 0 0 0 413 9 2 ─ ─ defined as the table 68625 to 69216 compound of the formula 11.48 'wherein the combination of the compound r21, r22, r23, r24 and R25 in each case corresponds to one of the eight columns and the combination of Rla and Het Tables 69217 to 69253 149027.doc 1 as defined in any of Tables 40800 to 41392 31 · 201103430 A compound of the formula II.49, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as defined in any of Tables 40800 to 40837. Table 69054 to 69290 Formula 11.50 a compound wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is a compound of the formula II.51 as defined in any one of Tables 40800 to 40837, wherein the compound The combination of Het and Ar' corresponds in each case to one of Table B and Rla is a compound of formula II.52 as defined in any of Tables 40800 to 40837, wherein Het and Ar' of the compound The combination in each case corresponds to one of the columns of Table B and Rla is a compound of the formula II.53 as defined in any of Tables 40800 to 40837, wherein the combination of Het and Ar' of the compound is in each case. The following corresponds to a column of Table B and Rla is a compound of Tables 69402 to 69438, Formula II.54, as defined in any of Tables 40800 to 40837, wherein the combination of Het and Ar' of the compound corresponds in each case to Table B. One of the columns and Rla is as shown in any of Tables 40800 to 4083 Defined in Tables 69439 to 69475

LSI 149027.doc •132- 201103430 式11.55之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且RIa係如表40800至40837之任一者 中所定義 表69476至69512 式11.56之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69513至69549 式11.57之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69550至69586 式11.58之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至4083 7之任一者 中所定義 表69587至69623 式11.59之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至4083 7之任一者 中所定義 表69624至69660 式II. 60之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69661至69697 149027.doc -133- 201103430 式II.61之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69698至69734 式II.62之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69735至69771 式II.63之化合物,其中化合物之Het與Ar’之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 69772至 69808 式II.64之化合物,其中化合物之Het與Af之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69809至69845 式II.65之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69846至69882 式II.66之化合物,其中化合物之Het與Ar1之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69883至69919LSI 149027.doc • 132- 201103430 The compound of formula 11.55, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and the RIa is as defined in Table 69476 as defined in any of Tables 40800 to 40837. 69512 A compound of the formula 11.56, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is a compound of the formula: formula 69513 to 69549, formula 11.57, as defined in any one of Tables 40800 to 40837, wherein The combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is a compound of the formula: formula 65950 to 69586, formula 11.58, as defined in any one of Tables 40800 to 40837, wherein the compounds are Het and Ar' Combinations in each case correspond to one of the columns of Table B and Rla is a compound of the formulae 69587 to 69623, formula 11.59, as defined in any of Tables 40800 to 4083, wherein the combination of Het and Ar' of the compound corresponds in each case The compounds of the formula II.60, wherein the combination of Het and Ar' of the compound, in each case corresponds to Table B, is listed in Table B and Rla is as defined in any of Tables 40800 to 4083. One column and Rla are as shown in Tables 40800 to 4083 Tables 69061 to 69697 149027.doc -133- 201103430 of any of the formulas of formula II.61, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and the Rla is as listed A compound of the formula II.62 as defined in any one of 40,800 to 40,837, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as shown in Tables 40800 to 40837. A compound of the formula II.63 as defined in one of the formulas 69935 to 69713, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as defined in any of Tables 40800 to 40837. Tables 69972 to 69808 Compounds of the formula II.64, wherein the combination of Het and Af of the compound corresponds in each case to one of the columns of Table B and Rla is as defined in any of Tables 40800 to 40837, Tables 69809 to 69845 Formula II The compound of .65, wherein the combination of Het and Ar' of the compound corresponds in each case to one of Table B and Rla is a compound of the formula II.66 to 69882 of the formula II.66 as defined in any of Tables 40800 to 40837, Wherein the combination of Het and Ar1 of the compound corresponds in each case to One column B and Rla based 40800-40837 Table according to any one of those defined in Table 69883-69919

[SI 149027.doc •134- 201103430 式II. 67之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69920至69956 式II.68之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69957至69993 式II.69之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表69994至70030 式II .70之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表70031至70067 式11.71之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70068至 70104 式II· 72之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表70105至70141 149027.doc •】35 - 201103430 式II.73之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且R1 a係如表40800至40837之任一者 中所定義 表 70142至 70178 式II.74之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70179至 70215 式II.75之化合物,其中化合物之Het與Ar'之組合在各情 況下對k於表B之一列且Rla係如表40800至40837之任一者 中所定義 表70216至70252 式II.76之化合物,其中化合物之Het與Ar’之組合在各情 況下對應於表B之一列且Ria係如表40800至40837之任一者 中所定義 表 70253至 70289 式II.77之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表70290至70326 式II.78之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70327至 70363 [S1 149027.doc •136- 201103430 式II.79之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70364至 70400 式II.80之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70401至 70437 式11.81之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70438至 70474 式ΙΙ·82之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表70475至70511 式II.83之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70512至 70548 式11.84之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表70549至70585 149027.doc -137- 201103430 式II.85之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70586至 70622 式II.86之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70623至 70659 式II.87之化合物,其中化合物之Het與Ar’之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70660至 70696 式II.88之化合物,其中化合物之Het與Af之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70697至 70733 式II.89之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表70734至70770 式11.90之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表70771至70807[SI 149027.doc • 134-201103430 The compound of formula II. 67, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as defined in any of Tables 40800 to 40837. Table 69920 to 69956 The compound of formula II.68 wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as defined in any of Tables 40800 to 40837, in the form of Tables 69957 to 69993. A compound of II.69, wherein the combination of Het and Ar' of the compound corresponds in each case to one of Table B and Rla is a compound of Table 69094 to 70030 Formula II.70 as defined in any of Tables 40800 to 40837. Wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is a compound of the formula: Tables 71.31 to 70067, formula 11.71, as defined in any one of Tables 40800 to 40837, wherein the compound Het and Ar The combination of 'in each case corresponds to one of the columns of Table B and Rla is a compound of the formulas 70068 to 70104 of the formula II.72 as defined in any of the forms 40800 to 40837, wherein the combination of Het and Ar' of the compound is in each In the case corresponding to one of the columns of Table B and Rla is as shown in Tables 40800 to 4 Table 70105 to 70141 149027.doc as defined in any of 0837.] 35 - 201103430 The compound of formula II.73, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and the R1 a system The compounds of formula II.74, as defined in any of Tables 40800 to 40837, wherein the combination of Het and Ar' of the compound corresponds in each case to one of Table B and Rla is as shown in Tables 40800 to 40837. Any of the compounds of formula II.75, defined in any one of the formulas 70179 to 70215, wherein the combination of Het and Ar' of the compound is in each case k is listed in one of Table B and Rla is in any of Tables 40800 to 40837. The compounds of formula II.76 are defined in Tables 70216 to 70252, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Ria is as defined in any of Tables 40800 to 40837. The compound of formula II.77, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as defined in any of Tables 40800 to 40837, Tables 70090 to 70326, Formula II. Compound of 78, wherein the combination of Het and Ar' of the compound is in each case Corresponding to one of the columns of Table B and Rla is a combination of Tables 70327 to 70363 as defined in any of Tables 40800 to 40837 [S1 149027.doc • 136-201103430 Formula II.79, wherein the combination of Het and Ar' of the compound In each case corresponds to one of the columns of Table B and Rla is a compound of the formula 70364 to 70400 of the formula II.80 as defined in any of the forms 40800 to 40837, wherein the combination of Het and Ar' of the compound corresponds in each case The compounds of Tables 11401 to 70437, formula 11.81, as defined in any of Tables 40800 to 40837, wherein the combination of Het and Ar' of the compound corresponds in each case to one of Table B and Rla A compound of the formula 70438 to 70474, as defined in any one of Tables 40800 to 40837, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as shown in Table 40800. A compound of the formula II.83 as defined in any of 40,837, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as in any of Tables 40800 to 40837. Compounds defined in Tables 70512 to 70548, formula 11.84 Wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as defined in any of Tables 40800 to 40837. Tables 70549 to 70585 149027.doc -137-201103430 Formula II.85 a compound wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is a compound of the formula II.86 as defined in any of Tables 40800 to 40837, wherein the compound The combination of Het and Ar' corresponds in each case to one of the columns of Table B and Rla is a compound of the formula II.87 to 70659, formula II.87, as defined in any of Tables 40800 to 40837, wherein the compound Het and Ar' The combination in each case corresponds to one of the columns of Table B and Rla is a compound of the formula II.88 as defined in any of Tables 40800 to 40837, wherein the combination of Het and Af of the compound is in each case Corresponding to one of the columns of Table B and Rla is a compound of the formula II.89 as defined in any of Tables 40800 to 40837, wherein the combination of Het and Ar' of the compound corresponds in each case to Table B. One column and Rla are as in any of Tables 40800 to 40837 Definitions Tables 70734 to 70770 Compounds of formula 11.90 wherein the combination of Het and Ar' of the compound corresponds in each case to one of Table B and Rla is as defined in any of Tables 40800 to 40837. Tables 70771 to 70807

[SI 149027.doc -138- 201103430 式11.91之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70808至70844 式II. 92之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70845至 70881 式II. 93之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70882至 70918 式II. 94之化合物,其中化合物之Het與Ar'之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表 70919至 70955 式11.95之化合物,其中化合物之Het與Ar1之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 表70956至70992 式II.96之化合物,其中化合物之Het與Af之組合在各情 況下對應於表B之一列且Rla係如表40800至40837之任一者 中所定義 149027.doc -139- 201103430[SI 149027.doc -138- 201103430 A compound of the formula 11.91, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as defined in any of Tables 40800 to 40837. The compound of formula II.92, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is as defined in any of Tables 40800 to 40837, Tables 70845 to 70881, Formula II. a compound of 93, wherein the combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is a compound of the formula II.94, wherein the formula 70882 to 70918 of the formula II.94 is defined in any one of the forms 40800 to 40837, wherein The combination of Het and Ar' of the compound corresponds in each case to one of the columns of Table B and Rla is a compound of the formula No. 70919 to 70955 of the formula 11.95 as defined in any one of Tables 40800 to 40837, wherein the combination of Het and Ar1 of the compound In each case corresponds to a column of Table B and Rla is a compound of the formula II.96 as defined in any of Tables 40800 to 40837, wherein the combination of Het and Af of the compound corresponds in each case to One of the tables B and Rla is as shown in Table 40800 Defined in any of 40837 149027.doc -139- 201103430

表B 編號 Ar, Het 編號 Ar' Het B-l Ar.2 Het.l B-33 Ar.34 Het.l B-2 Ar.3 Het.l B-34 Ar.3 5 Het.l B-3 Ar.4 Het.l B-35 Ar.36 Het.l B-4 Ar.5 Het.l B-36 Ar.37 Het.l B-5 Ar.6 Het.l B-37 Ar.3 8 Het.l B-6 Ar.7 Het.l B-3 8 Ar.39 Het.l B-7 Ar.8 Het.l B-39 Ar.40 Het.l B-8 Ar.9 Het.l B-40 Ar.41 Het.l B-9 Ar.10 Het.l B-41 Ar.42 Het.l B-10 Ar.ll Het.l B-42 Ar.43 Het.l B-ll Ar.12 Het.l B-43 Ar.44 Het.l B-12 Ar.13 Het.l B-44 Ar.45 Het.l B-13 Ar.14 Het.l B-45 Ar.46 Het.l B-14 Ar.15 Het.l B-46 Ar.47 Het.l B-15 Ar.16 Het.l B-47 Ar.48 Het.l B-16 Ar.17 Het.l B-48 Ar.49 Het.l B-17 Ar.18 Het.l B-49 Ar.50 Het.l B-18 Ar_19 Het.l B-50 Ar.2 Het.2 B-19 Ar.20 Het.l B-51 Ar.3 Het.2 B-20 Ar.21 Het.l B-52 Ar.4 Het.2 B-21 Ar.22 Het.l B-53 Ar.5 Het.2 B-22 Ar.23 Het.l B-54 Ar.6 Het.2 B-23 Ar.24 Het.l B-55 Ar.7 Het.2 B-24 Ar.25 Het.l B-56 Ar.8 Het.2 B-25 Ar.26 Het.l B-57 Ar.9 Het.2 B-26 Ar.27 Het.l B-5 8 Ar.10 Het.2 B-27 Ar.28 Het.l B-59 Ar.ll Het.2 B-28 Ar.29 Het.l B-60 Ar.12 Het.2 B-29 Ar.30 Het.l B-61 Ar.13 Het.2 B-30 Ar.31 Het.l B-62 Ar.14 Het.2 B-31 Ar.32 Het.l B-63 Ar.15 Het.2 B-32 Ar.33 Het.l B-64 Ar.16 Het.2Table B No. Ar, Het No. Ar' Het Bl Ar. 2 Het.l B-33 Ar.34 Het.l B-2 Ar.3 Het.l B-34 Ar.3 5 Het.l B-3 Ar. 4 Het.l B-35 Ar.36 Het.l B-4 Ar.5 Het.l B-36 Ar.37 Het.l B-5 Ar.6 Het.l B-37 Ar.3 8 Het.l B-6 Ar.7 Het.l B-3 8 Ar.39 Het.l B-7 Ar.8 Het.l B-39 Ar.40 Het.l B-8 Ar.9 Het.l B-40 Ar .41 Het.l B-9 Ar.10 Het.l B-41 Ar.42 Het.l B-10 Ar.ll Het.l B-42 Ar.43 Het.l B-ll Ar.12 Het.l B-43 Ar.44 Het.l B-12 Ar.13 Het.l B-44 Ar.45 Het.l B-13 Ar.14 Het.l B-45 Ar.46 Het.l B-14 Ar. 15 Het.l B-46 Ar.47 Het.l B-15 Ar.16 Het.l B-47 Ar.48 Het.l B-16 Ar.17 Het.l B-48 Ar.49 Het.l B -17 Ar.18 Het.l B-49 Ar.50 Het.l B-18 Ar_19 Het.l B-50 Ar.2 Het.2 B-19 Ar.20 Het.l B-51 Ar.3 Het. 2 B-20 Ar.21 Het.l B-52 Ar.4 Het.2 B-21 Ar.22 Het.l B-53 Ar.5 Het.2 B-22 Ar.23 Het.l B-54 Ar .6 Het.2 B-23 Ar.24 Het.l B-55 Ar.7 Het.2 B-24 Ar.25 Het.l B-56 Ar.8 Het.2 B-25 Ar.26 Het.l B-57 Ar.9 Het.2 B-26 Ar.27 Het.l B-5 8 Ar.10 Het.2 B-27 Ar.28 Het.l B-59 Ar.ll Het.2 B-28 Ar .29 H Et.l B-60 Ar.12 Het.2 B-29 Ar.30 Het.l B-61 Ar.13 Het.2 B-30 Ar.31 Het.l B-62 Ar.14 Het.2 B- 31 Ar.32 Het.l B-63 Ar.15 Het.2 B-32 Ar.33 Het.l B-64 Ar.16 Het.2

[SI 149027.doc -140- 201103430 編號 Ar, Het B-65 Ar.17 Het.2 B-66 Ar.18 Het.2 B-67 Ar.19 Het.2 B-68 Ar.20 Het.2 B-69 Ar.21 Het.2 B-70 Ar.22 Het.2 B-71 Ar.23 Het.2 B-72 Ar.24 Het.2 B-73 Ar.25 Het.2 B-74 Ar.26 Het.2 B-75 Ar.27 Het.2 B-76 Ar.28 Het.2 B-77 Ar.29 Het.2 B-78 Ar.30 Het.2 B-79 Ar.31 Het.2 B-80 Ar.32 Het.2 B-81 Ar.33 Het.2 B-82 Ar.34 Het.2 B-83 Ar.35 Het.2 B-84 Ar.36 Het.2 B-85 Ar.37 Het.2 B-86 Ar.38 Het.2 B-87 Ar.39 Het.2 B-88 Ar.40 Het.2 B-89 Ar.41 Het.2 B-90 Ar.42 Het.2 B-91 Ar.43 Het.2 B-92 Ar.44 Het.2 B-93 Ar.45 Het.2 B-94 Ar.46 Het.2 B-95 Ar.47 Het.2 B-96 Ar.48 Het.2 B-97 Ar.49 Het.2 B-98 Ar.50 Het.2 編號 At' Het B-99 Ar.2 Het.3 B-100 Ar.3 Het.3 B-101 Ar.4 Het.3 B-102 Ar.5 Het.3 B-103 Ar.6 Het.3 B-104 Ar.7 Het.3 B-105 Ar.8 Het.3 B-106 Ar.9 Het.3 B-107 Ar.10 Het.3 B-108 Ar.ll Het.3 B-109 Ar.12 Het.3 B-110 Ar.13 Het.3 B-lll Ar.14 Het.3 B-112 Ar.15 Het.3 B-113 Ar.16 Het.3 B-114 Ar.17 Het.3 B-115 Ar.18 Het.3 B-116 Ar.19 Het.3 B-117 Ar.20 Het.3 B-118 Ar.21 Het.3 B-119 Ar.22 Het.3 B-120 Ar.23 Het.3 B-121 Ar.24 Het.3 B-122 Ar.25 Het.3 B-123 Ar.26 Het.3 B-124 Ar.27 Het.3 B-125 Ar.28 Het.3 B-126 Ar.29 Het.3 B-127 Ar.30 Het.3 B-128 Ar.31 Het.3 B-129 Ar.32 Het.3 B-130 Ar.33 Het.3 B-131 Ar.34 Het.3 B-132 Ar.35 Het.3 149027.doc -141 - 201103430 編號 At, Het B-133 Ar.36 Het.3 B-134 Ar.37 Het.3 B-135 Ar.38 Het.3 B-136 Ar.39 Het.3 B-137 Ar.40 Het.3 B-138 Ar.41 Het.3 B-139 Ar.42 Het.3 B-140 Ar.43 Het.3 B-141 Ar.44 Het.3 B-142 Ar.45 Het.3 B-143 Ar.46 Het.3 B-144 Ar.47 Het.3 B-145 Ar.48 Het.3 B-146 Ar.49 Het.3 B-147 Ar.50 Het.3 B-148 Ar.2 Het.4 B-149 Ar.3 Het.4 B-150 Ar.4 Het.4 B-151 Ar.5 Het.4 B-152 Ar.6 Het.4 B-153 Ar.7 Het.4 B-154 Ar.8 Het.4 B-155 Ar.9 Het.4 B-156 Ar.10 Het.4 B-157 Ar.ll Het.4 B-158 Ar_12 Het.4 B-159 Ar.13 Het.4 B-160 Ar.14 Het.4 B-161 Ar.15 Het.4 B-162 Ar. 16 Het.4 B-163 Ar.17 Het.4 B-164 Ar.18 Het.4 B-165 Ar.19 Het.4 B-166 Ar.20 Het.4 編號 Ar, Het B-167 Ar.21 Het.4 B-168 Ar.22 Het.4 B-169 Ar.23 Het.4 B-170 Ar.24 Het.4 B-171 Ar.25 Het.4 B-172 Ar.26 Het.4 B-173 Ar.27 Het.4 B-174 Ar.28 Het.4 B-175 Ar.29 Het.4 B-176 Ar.30 Het.4 B-177 Ar.31 Het.4 B-178 Ar.32 Het.4 B-179 Ar.33 Het.4 B-180 Ar.34 Het.4 B-181 Ar.35 Het.4 B-182 Ar.36 Het.4 B-183 Ar.37 Het.4 B-184 Ar.38 Het.4 B-185 Ar.39 Het.4 B-186 Ar.40 Het.4 B-187 Ar.41 Het.4 B-188 Ar.42 Het.4 B-189 Ar.43 Het.4 B-190 Ar.44 Het.4 B-191 Ar.45 Het.4 B-192 Ar.46 Het.4 B-193 Ar.47 Het.4 B-194 Ar.48 Het.4 B-195 Ar.49 Het.4 B-196 Ar.50 Het.4 B-197 Ar.2 Het.5 B-198 Ar.3 Het.5 B-199 Ar.4 Het.5 B-200 Ar.5 Het.5 [s] 149027.doc -142- 201103430 編號 Ar, Het B-201 Ar.6 Het.5 B-202 Ar.7 Het.5 B-203 Ar.8 Het.5 B-204 Ar.9 Het.5 B-205 Ar.10 Het.5 B-206 Ar.ll Het.5 B-207 Ar.12 Het.5 B-208 Ar.13 Het.5 B-209 Ar.14 Het.5 B-210 Ar. 15 Het.5 B-211 Ar.16 Het.5 B-212 Ar.17 Het.5 B-213 Ar.18 Het.5 B-214 Ar_19 Het.5 B-215 Ar.20 Het.5 B-216 Ar.21 Het.5 B-217 Ar.22 Het.5 B-218 Ar.23 Het.5 B-219 Ar.24 Het.5 B-220 Ar.25 Het.5 B-221 Ar.26 Het.5 B-222 Ar.27 Het.5 B-223 Ar.28 Het.5 B-224 Ar.29 Het.5 B-225 Ar.30 Het.5 B-226 Ar.31 Het.5 B-227 Ar.32 Het.5 B-228 Ar.33 Het.5 B-229 Ar.34 Het.5 B-230 Ar.35 Het.5 B-231 Ar.36 Het.5 B-232 Ar.37 Het.5 B-233 Ar.38 Het.5 B-234 Ar.39 Het.5 編號 At' Het B-235 Ar.40 Het.5 B-236 Ar.41 Het.5 B-237 Ar.42 Het.5 B-238 Ar.43 Het.5 B-239 Ar.44 Het.5 B-240 Ar.45 Het.5 B-241 Ar.46 Het.5 B-242 Ar.47 Het.5 B-243 Ar.48 Het.5 B-244 Ar.49 Het.5 B-245 Ar.50 Het.5 B-246 Ar.2 Het.6 B-247 Ar.3 Het.6 B-248 Ar.4 Het.6 B-249 Ar.5 Het.6 B-250 Ar.6 Het.6 B-251 Ar.7 Het.6 B-252 Ar.8 Het.6 B-253 Ar.9 Het.6 B-254 Ar.10 Het.6 B-255 Ar.ll Het.6 B-256 Ar.12 Het.6 B-257 Ar.13 Het.6 B-258 Ar.14 Het.6 B-259 Ar.15 Het.6 B-260 Ar.16 Het.6 B-261 Ar.17 Het.6 B-262 Ar.18 Het.6 B-263 Ar.19 Het.6 B-264 Ar.20 Het.6 B-265 Ar.21 Het.6 B-266 Ar.22 Het.6 B-267 Ar.23 Het.6 B-268 Ar.24 Het.6 149027.doc -143- 201103430 編號 Ar, Het B-269 Ar.25 Het.6 B-270 Ar.26 Het.6 B-271 Ar.27 Het.6 B-272 Ar.28 Het.6 B-273 Ar.29 Het.6 B-274 Ar.30 Het.6 B-275 Ar.31 Het.6 B-276 Ar.32 Het.6 B-277 Ar.33 Het.6 B-278 Ar.34 Het.6 B-279 Ar.35 Het.6 B-280 Ar.36 Het.6 B-281 Ar.37 Het.6 B-282 Ar.38 Het.6 B-283 Ar.39 Het.6 B-284 Ar.40 Het.6 B-285 Ar.41 Het.6 B-286 Ar.42 Het.6 B-287 Ar.43 Het.6 B-288 Ar.44 Het.6 B-289 Ar.45 Het.6 B-290 Ar.46 Het.6 B-291 Ar.47 Het.6 B-292 Ar.48 Het.6 B-293 Ar.49 Het.6 B-294 Ar.50 Het.6 B-295 Ar.2 Het.7 B-296 Ar.3 Het.7 B-297 Ar.4 Het.7 B-298 Ar.5 Het.7 B-299 Ar.6 Het.7 B-300 Ar.7 Het.7 B-301 Ar.8 Het.7 B-302 Ar.9 Het.7 編號 Ar, Het B-303 Ar.10 Het.7 B-304 Ar.ll Het.7 B-305 Ar.12 Het.7 B-306 Ar.13 Het.7 B-307 Ar.14 Het.7 B-308 Ar.15 Het.7 B-309 Ar.16 Het.7 B-310 Ar.17 Het.7 B-311 Ar.18 Het.7 B-312 Ar.19 Het.7 B-313 Ar.20 Het.7 B-314 Ar_21 Het.7 B-315 Ar.22 Het.7 B-316 Ar.23 Het.7 B-317 Ar.24 Het.7 B-318 Ar.25 Het.7 B-319 Ar.26 Het.7 B-320 Ar.27 Het.7 B-321 Ar.28 Het.7 B-322 Ar.29 Het.7 B-323 Ar.30 Het.7 B-324 Ar_31 Het.7 B-325 Ar.32 Het.7 B-326 Ar.33 Het.7 B-327 Ar.34 Het.7 B-328 Ar.35 Het.7 B-329 Ar.36 Het.7 B-330 Ar.37 Het.7 B-331 Ar.38 Het.7 B-332 Ar.39 Het.7 B-333 Ar.40 Het.7 B-334 Ar.41 Het.7 B-335 Ar.42 Het.7 B-336 Ar.43 Het.7 [si 149027.doc -144- 201103430 編號 Ar' Het B-337 Ar.44 Het.7 B-338 Ar.45 Het.7 B-339 Ar.46 Het.7 B-340 Ar.47 Het.7 B-341 Ar.48 Het.7 B-342 Ar.49 Het.7 B-343 Ar.50 Het.7 B-344 Ar.2 Het. 8 B-345 Ar.3 Het. 8 B-346 Ar.4 Het.8 B-347 Ar.5 Het. 8 B-348 Ar.6 Het.8 B-349 Ar.7 Het.8 B-350 Ar.8 Het.8 B-351 Ar.9 Het.8 B-352 Ar.10 Het.8 B-353 Ar.ll Het.8 B-354 Ar.12 Het.8 B-355 Ar.13 Het.8 B-356 Ar.14 Het.8 B-357 Ar.15 Het.8 B-358 Ar.16 Het.8 B-359 Ar.17 Het.8 B-360 Ar.18 Het.8 B-361 Ar.19 Het.8 B-362 Ar.20 Het.8 B-363 Ar.21 Het.8 B-364 Ar.22 Het.8 B-365 Ar.23 Het.8 B-366 Ar.24 Het.8 B-367 Ar.25 Het.8 B-368 Ar.26 Het.8 B-369 Ar.27 Het.8 B-370 Ar.28 Het.8 編號 Ar' Het B-371 Ar.29 Het.8 B-372 Ar.30 Het.8 B-373 Ar.31 Het.8 B-374 Ar.32 Het.8 B-375 Ar.33 Het.8 B-376 Ar.34 Het.8 B-377 Ar.35 Het.8 B-378 Ar.36 Het.8 B-379 Ar.37 Het.8 B-380 Ar.3 8 Het.8 B-381 Ar.39 Het.8 B-382 Ar.40 Het.8 B-383 Ar.41 Het.8 B-384 Ar.42 Het.8 B-385 Ar.43 Het.8 B-386 Ar.44 Het.8 B-387 Ar.45 Het.8 B-388 Ar.46 Het.8 B-389 Ar.47 Het.8 B-390 Ar.48 Het.8 B-391 Ar.49 Het.8 B-392 Ar.50 Het.8 B-393 Ar.2 Het.9 B-394 Ar.3 Het.9 B-395 Ar.4 Het.9 B-396 Ar.5 Het.9 B-397 Ar.6 Het.9 B-398 Ar.7 Het.9 B-399 Ar.8 Het.9 B-400 Ar.9 Het.9 B-401 Ar.10 Het.9 B-402 Ar.ll Het.9 B-403 Ar.12 Het.9 B-404 Ar.13 Het.9 149027.doc •145- 201103430 編號 Ar' Het 編號 At' Het B-405 Ar.14 Het.9 B-439 Ar.48 Het.9 B-406 Ar.15 Het.9 B-440 Ar.49 Het.9 B-407 Ar.16 Het.9 B-441 Ar.50 Het.9 B-408 Ar.17 Het.9 B-442 Ar.2 Het. 10 B-409 Ar.18 Het.9 B-443 Ar.3 Het. 10 B-410 Ar.19 Het.9 B-444 Ar.4 Het. 10 B-411 Ar.20 Het.9 B-445 Ar.5 Het. 10 B-412 Ar.21 Het.9 B-446 Ar.6 Het. 10 B-413 Ar.22 Het.9 B-447 Ar.7 Het. 10 B-414 Ar.23 Het.9 B-448 Ar.8 Het. 10 B-415 Ar.24 Het.9 B-449 Ar.9 Het. 10 B-416 Ar.25 Het.9 B-450 Ar.10 Het. 10 B-417 Ar.26 Het.9 B-451 Ar.ll Het. 10 B-418 Ar.27 Het.9 B-452 Ar.12 Het. 10 B-419 Ar.28 Het.9 B-453 Ar.13 Het. 10 B-420 Ar.29 Het.9 B-454 Ar.14 Het. 10 B-421 Ar.30 Het.9 B-455 Ar.15 Het. 10 B-422 Ar.31 Het.9 B-456 Ar.16 Het. 10 B-423 Ar.32 Het.9 B-457 Ar.17 Het 10 B-424 Ar.33 Het.9 B-458 Ar.18 Het. 10 B-425 Ar.34 Het.9 B-459 Ar.19 Het. 10 B-426 Ar.35 Het.9 B-460 Ar.20 Het. 10 B-427 Ar.36 Het.9 B-461 Ar.21 Het. 10 B-428 Ar.37 Het.9 B-462 Ar.22 Het. 10 B-429 Ar.38 Het.9 B-463 Ar.23 Het. 10 B-430 Ar.39 Het.9 B-464 Ar.24 Het. 10 B-431 Ar.40 Het.9 B-465 Ar.25 Het. 10 B-432 Ar.41 Het.9 B-466 Ar.26 Het. 10 B-433 Ar.42 Het.9 B-467 Ar.27 Het. 10 B-434 Ar.43 Het.9 B-468 Ar.28 Het. 10 B-435 Ar.44 Het.9 B-469 Ar.29 Het. 10 B-436 Ar.45 Het.9 B-470 Ar.30 Het. 10 B-437 Ar.46 Het.9 B-471 Ar.31 Het. 10 B-438 Ar.47 Het.9 B-472 Ar.32 Het. 10 [si 149027.doc -146· 201103430 編號 Ar' Het B-473 Ar.33 Het.10 B-474 Ar.34 Het. 10 B-475 Ar.35 Het.10 B-476 Ar.36 Het.10 B-477 Ar.37 Het.10 B-478 Ar.38 Het.10 B-479 Ar.39 Het.10 B-480 Ar.40 Het.10 B-481 Ar.41 Het.10 B-482 Ar.42 Het.10 B-483 Ar.43 Het.10 B-484 Ar.44 Het.10 B-485 Ar.45 Het.10 B-486 Ar.46 Het.10 B-487 Ar.47 Het.10 B-488 Ar.48 Het.10 B-489 Ar.49 Het.10 B-490 Ar.50 Het.10 B-491 Ar.2 Het. 11 B-492 Ar.3 Het. 11 B-493 Ar.4 Het. 11 B-494 Ar.5 Het. 11 B-495 Ar.6 Het. 11 B-496 Ar.7 Het. 11 B-497 Ar.8 Het. 11 B-498 Ar.9 Het. 11 B-499 Ar.10 Het. 11 B-500 Ar.ll Het. 11 B-501 Ar.12 Het. 11 B-502 Ar.13 Het. 11 B-503 Ar.14 Het. 11 B-504 Ar.15 Het. 11 B-505 Ar.16 Het. 11 B-506 Ar.17 Het. 11 編號 Ar, Het B-507 Ar.18 Het. 11 B-508 Ar.19 Het. 11 B-509 Ar.20 Het. 11 B-510 Ar.21 Het. 11 B-511 Ar.22 Het. 11 B-512 Ar.23 Het. 11 B-513 Ar.24 Het. 11 B-514 Ar.25 Het. 11 B-515 Ar.26 Het. 11 B-516 Ar.27 Het. 11 B-517 Ar.28 Het. 11 B-518 Ar.29 Het. 11 B-519 Ar.30 Het. 11 B-520 Ar.31 Het. 11 B-521 Ar.32 Het. 11 B-522 Ar.33 Het. 11 B-523 Ar.34 Het. 11 B-524 Ar.35 Het. 11 B-525 Ar.36 Het. 11 B-526 Ar.37 Het. 11 B-527 Ar.38 Het. 11 B-528 Ar.39 Het 11 B-529 Ar.40 Het. 11 B-530 Ar.41 Het. 11 B-531 Ar.42 Het. 11 B-532 Ar.43 Het. 11 B-533 Ar.44 Het. 11 B-534 Ar.45 Het. 11 B-535 Ar.46 Het. 11 B-536 Ar.47 Het. 11 B-537 Ar.48 Het. 11 B-538 Ar.49 Het. 11 B-539 Ar.50 Het. 11 B-540 Ar.2 Het. 12 149027.doc -147· 201103430 編號 At' Het B-541 Ar.3 Het.12 B-542 Ar.4 Het.12 B-543 Ar.5 Het.12 B-544 Ar.6 Het.12 B-545 Ar.7 Het.12 B-546 Ar.8 Het.12 B-547 Ar.9 Het.12 B-548 Ar.10 Het.12 B-549 Ar.ll Het.12 B-550 Ar.12 Het.12 B-551 Ar.13 Het.12 B-552 Ar.14 Het.12 B-553 Ar.15 Het.12 B-554 Ar.16 Het.12 B-555 Ar.17 Het.12 B-556 Ar.18 Het.12 B-557 Ar.19 Het.12 B-558 Ar.20 Het.12 B-559 Ar.21 Het.12 B-560 Ar.22 Het.12 B-561 Ar.23 Het.12 B-562 Ar.24 Het.12 B-563 Ar.25 Het.12 B-564 Ar.26 Het.12 B-565 Ar.27 Het.12 B-566 Ar.28 Het.12 B-567 Ar.29 Het.12 B-568 Ar.30 Het.12 B-569 Ar.31 Het.12 B-570 Ar.32 Het.12 B-571 Ar.33 Het.12 B-572 Ar.34 Het.12 B-573 Ar.35 Het.12 B-574 Ar.3 6 Het.12 編號 Ar' Het B-575 Ar.37 Het.12 B-576 Ar.38 Het. 12 B-577 Ar.39 Het.12 B-578 Ar.40 Het.12 B-579 Ar.41 Het.12 B-580 Ar.42 Het.12 B-581 Ar.43 Het.12 B-582 Ar.44 Het.12 B-583 Ar.45 Het.12 B-584 Ar.46 Het.12 B-585 Ar.47 Het.12 B-586 Ar.48 Het.12 B-587 Ar.49 Het.12 B-588 Ar.50 Het.12 B-589 Ar.2 Het. 13 B-590 Ar.3 Het. 13 B-591 Ar.4 Het. 13 B-592 Ar.5 Het. 13 B-593 Ar.6 Het. 13 B-594 Ar.7 Het. 13 B-595 Ar.8 Het. 13 B-596 Ar.9 Het. 13 B-597 Ar.10 Het. 13 B-598 Ar.ll Het. 13 B-599 Ar.12 Het. 13 B-600 Ar.13 Het. 13 B-601 Ar.14 Het. 13 B-602 Ar.15 Het. 13 B-603 Ar.16 Het. 13 B-604 Ar.17 Het. 13 B-605 Ar.18 Het. 13 B-606 Ar.19 Het. 13 B-607 Ar.20 Het. 13 B-608 Ar.21 Het. 13 149027.doc -148- 201103430 編號 At' Het B-609 Ar.22 Het.13 B-610 Ar.23 Het. 13 B-611 Ar.24 Het.13 B-612 Ar.25 Het.13 B-613 Ar.26 Het.13 B-614 Ar.27 Het.13 B-615 Ar.28 Het.13 B-616 Ar.29 Het.13 B-617 Ar.30 Het.13 B-618 Ar.31 Het.13 B-619 Ar.32 Het.13 B-620 Ar.33 Het.13 B-621 Ar.34 Het.13 B-622 Ar.35 Het.13 B-623 Ar.36 Het.13 B-624 Ar.37 Het.13 B-625 Ar.38 Het.13 B-626 Ar.39 Het.13 B-627 Ar.40 Het.13 B-628 Ar.41 Het.13 B-629 Ar.42 Het.13 B-630 Ar.43 Het.13 B-631 Ar.44 Het.13 B-632 Ar.45 Het.13 B-633 Ar.46 Het.13 B-634 Ar.47 Het.13 B-635 Ar.48 Het.13 B-636 Ar.49 Het.13 B-637 Ar.50 Het.13 B-638 Ar.2 Het. 14 B-639 Ar.3 Het. 14 B-640 Ar.4 Het. 14 B-641 Ar.5 Het. 14 B-642 Ar.6 Het. 14 編號 Ar' Het B-643 Ar.7 Het. 14 B-644 Ar.8 Het. 14 B-645 Ar.9 Het. 14 B-646 Ar.10 Het:14 B-647 Ar.ll Het. 14 B-648 Ar.12 Het. 14 B-649 Ar.13 Het. 14 B-650 Ar.14 Het. 14 B-651 Ar.15 Het. 14 B-652 Ar.16 Het. 14 B-653 Ar.17 Het. 14 B-654 Ar.18 Het. 14 B-655 Ar.19 Het. 14 B-656 Ar.20 Het. 14 B-657 Ar.21 Het. 14 B-658 Ar.22 Het. 14 B-659 Ar.23 Het. 14 B-660 Ar.24 Het. 14 B-661 Ar.25 Het. 14 B-662 Ar.26 Het. 14 B-663 Ar.27 Het. 14 B-664 Ar.28 Het. 14 B-665 Ar.29 Het. 14 B-666 · Ar.30 Het. 14 B-667 Ar.31 Het. 14 B-668 Ar.32 Het. 14 B-669 Ar.33 Het. 14 B-670 Ar.34 Het. 14 B-671 Ar.35 Het. 14 B-672 Ar.36 Het. 14 B-673 Ar.37 Het. 14 B-674 Ar.38 Het. 14 B-675 Ar.39 Het. 14 B-676 Ar.40 Het. 14 149027.doc •149· 201103430 編號 Ar’ Het B-677 Ar.41 Het. 14 B-678 Ar.42 Het. 14 B-679 Ar.43 Het. 14 B-680 Ar.44 Het. 14 B-681 Ar.45 Het. 14 B-682 Ar.46 Het. 14 B-683 Ar.47 Het. 14 B-684 Ar.48 Het. 14 B-685 Ar.49 Het. 14 B-686 Ar.50 Het. 14 B-687 Ar.2 Het.15 B-688 Ar.3 Het.15 B-689 Ar.4 Het.15 B-690 Ar.5 Het.15 B-691 Ar.6 Het.15 B-692 Ar.7 Het.15 B-693 Ar.8 Het.15 B-694 Ar.9 Het.15 B-695 Ar.10 Het.15 B-696 Ar.ll Het.15 B-697 Ar.12 Het.15 B-698 Ar.13 Het.15 B-699 Ar.14 Het.15 B-700 Ar. 15 ' Het.15 B-701 Ar.16 Het.15 B-702 Ar_17 Het.15 B-703 Ar.18 Het.15 B-704 Ar.19 Het.15 B-705 Ar.20 Het.15 B-706 Ar.21 Het.15 B-707 Ar.22 Het.15 B-708 Ar.23 Het.15 B-709 Ar.24 Het.15 B-710 Ar.25 Het.15 編號 Ar, Het B-711 Ar.26 Het.15 B-712 Ar.27 Het. 15 B-713 Ar.28 Het.15 B-714 Ar.29 Het.15 B-715 Ar.30 Het.15 B-716 Ar.31 Het.15 B-717 Ar.32 Het.15 B-718 Ar.33 Het.15 B-719 Ar.34 Het.15 B-720 Ar.35 Het.15 B-721 Ar.36 Het.15 B-722 Ar.37 Het.15 B-723 Ar.38 Het.15 B-724 Ar.39 Het.15 B-725 Ar.40 Het.15 B-726 Ar.41 Het.15 B-727 Ar.42 Het.15 B-728 Ar.43 Het.15 B-729 Ar.44 Het.15 B-730 Ar.45 Het.15 B-731 Ar.46 Het.15 B-732 Ar.47 Het.15 B-733 Ar.48 Het.15 B-734 Ar.49 Het.15 B-735 Ar.50 Het.15 B-736 Ar.2 Het. 16 B-737 Ar.3 Het. 16 B-738 Ar.4 Het. 16 B-739 Ar.5 Het. 16 B-740 Ar.6 Het. 16 B-741 Ar.7 Het. 16 B-742 Ar.8 Het. 16 B-743 Ar.9 Het. 16 B-744 Ar.10 Het. 16[SI 149027.doc -140- 201103430 No. Ar, Het B-65 Ar.17 Het.2 B-66 Ar.18 Het.2 B-67 Ar.19 Het.2 B-68 Ar.20 Het.2 B -69 Ar.21 Het.2 B-70 Ar.22 Het.2 B-71 Ar.23 Het.2 B-72 Ar.24 Het.2 B-73 Ar.25 Het.2 B-74 Ar.26 Het.2 B-75 Ar.27 Het.2 B-76 Ar.28 Het.2 B-77 Ar.29 Het.2 B-78 Ar.30 Het.2 B-79 Ar.31 Het.2 B- 80 Ar.32 Het.2 B-81 Ar.33 Het.2 B-82 Ar.34 Het.2 B-83 Ar.35 Het.2 B-84 Ar.36 Het.2 B-85 Ar.37 Het .2 B-86 Ar.38 Het.2 B-87 Ar.39 Het.2 B-88 Ar.40 Het.2 B-89 Ar.41 Het.2 B-90 Ar.42 Het.2 B-91 Ar.43 Het.2 B-92 Ar.44 Het.2 B-93 Ar.45 Het.2 B-94 Ar.46 Het.2 B-95 Ar.47 Het.2 B-96 Ar.48 Het. 2 B-97 Ar.49 Het.2 B-98 Ar.50 Het.2 No. At' Het B-99 Ar.2 Het.3 B-100 Ar.3 Het.3 B-101 Ar.4 Het.3 B-102 Ar.5 Het.3 B-103 Ar.6 Het.3 B-104 Ar.7 Het.3 B-105 Ar.8 Het.3 B-106 Ar.9 Het.3 B-107 Ar. 10 Het.3 B-108 Ar.ll Het.3 B-109 Ar.12 Het.3 B-110 Ar.13 Het.3 B-lll Ar.14 Het.3 B-112 Ar.15 Het.3 B -113 Ar.16 Het.3 B-114 Ar.17 Het.3 B-115 Ar.18 Het.3 B-116 Ar.19 Het.3 B-117 Ar.20 Het.3 B-118 Ar.21 Het.3 B-119 Ar.22 Het.3 B-120 Ar.23 Het.3 B-121 Ar.24 Het.3 B- 122 Ar.25 Het.3 B-123 Ar.26 Het.3 B-124 Ar.27 Het.3 B-125 Ar.28 Het.3 B-126 Ar.29 Het.3 B-127 Ar.30 Het .3 B-128 Ar.31 Het.3 B-129 Ar.32 Het.3 B-130 Ar.33 Het.3 B-131 Ar.34 Het.3 B-132 Ar.35 Het.3 149027.doc -141 - 201103430 No. At, Het B-133 Ar.36 Het.3 B-134 Ar.37 Het.3 B-135 Ar.38 Het.3 B-136 Ar.39 Het.3 B-137 Ar.40 Het.3 B-138 Ar.41 Het.3 B-139 Ar.42 Het.3 B-140 Ar.43 Het.3 B-141 Ar.44 Het.3 B-142 Ar.45 Het.3 B- 143 Ar.46 Het.3 B-144 Ar.47 Het.3 B-145 Ar.48 Het.3 B-146 Ar.49 Het.3 B-147 Ar.50 Het.3 B-148 Ar.2 Het .4 B-149 Ar.3 Het.4 B-150 Ar.4 Het.4 B-151 Ar.5 Het.4 B-152 Ar.6 Het.4 B-153 Ar.7 Het.4 B-154 Ar.8 Het.4 B-155 Ar.9 Het.4 B-156 Ar.10 Het.4 B-157 Ar.ll Het.4 B-158 Ar_12 Het.4 B-159 Ar.13 Het.4 B -160 Ar.14 Het.4 B-161 Ar.15 Het.4 B-162 Ar. 16 Het.4 B-163 Ar.17 Het.4 B-164 Ar.18 Het.4 B-165 Ar.19 Het.4 B-166 Ar.20 Het.4 No. A r, Het B-167 Ar.21 Het.4 B-168 Ar.22 Het.4 B-169 Ar.23 Het.4 B-170 Ar.24 Het.4 B-171 Ar.25 Het.4 B- 172 Ar.26 Het.4 B-173 Ar.27 Het.4 B-174 Ar.28 Het.4 B-175 Ar.29 Het.4 B-176 Ar.30 Het.4 B-177 Ar.31 Het .4 B-178 Ar.32 Het.4 B-179 Ar.33 Het.4 B-180 Ar.34 Het.4 B-181 Ar.35 Het.4 B-182 Ar.36 Het.4 B-183 Ar.37 Het.4 B-184 Ar.38 Het.4 B-185 Ar.39 Het.4 B-186 Ar.40 Het.4 B-187 Ar.41 Het.4 B-188 Ar.42 Het. 4 B-189 Ar.43 Het.4 B-190 Ar.44 Het.4 B-191 Ar.45 Het.4 B-192 Ar.46 Het.4 B-193 Ar.47 Het.4 B-194 Ar .48 Het.4 B-195 Ar.49 Het.4 B-196 Ar.50 Het.4 B-197 Ar.2 Het.5 B-198 Ar.3 Het.5 B-199 Ar.4 Het.5 B-200 Ar.5 Het.5 [s] 149027.doc -142- 201103430 No. Ar, Het B-201 Ar.6 Het.5 B-202 Ar.7 Het.5 B-203 Ar.8 Het.5 B-204 Ar.9 Het.5 B-205 Ar.10 Het.5 B-206 Ar.ll Het.5 B-207 Ar.12 Het.5 B-208 Ar.13 Het.5 B-209 Ar. 14 Het.5 B-210 Ar. 15 Het.5 B-211 Ar.16 Het.5 B-212 Ar.17 Het.5 B-213 Ar.18 Het.5 B-214 Ar_19 Het.5 B-215 Ar.20 Het.5 B-216 Ar.21 Het.5 B-2 17 Ar.22 Het.5 B-218 Ar.23 Het.5 B-219 Ar.24 Het.5 B-220 Ar.25 Het.5 B-221 Ar.26 Het.5 B-222 Ar.27 Het .5 B-223 Ar.28 Het.5 B-224 Ar.29 Het.5 B-225 Ar.30 Het.5 B-226 Ar.31 Het.5 B-227 Ar.32 Het.5 B-228 Ar.33 Het.5 B-229 Ar.34 Het.5 B-230 Ar.35 Het.5 B-231 Ar.36 Het.5 B-232 Ar.37 Het.5 B-233 Ar.38 Het. 5 B-234 Ar.39 Het.5 No. At' Het B-235 Ar.40 Het.5 B-236 Ar.41 Het.5 B-237 Ar.42 Het.5 B-238 Ar.43 Het.5 B-239 Ar.44 Het.5 B-240 Ar.45 Het.5 B-241 Ar.46 Het.5 B-242 Ar.47 Het.5 B-243 Ar.48 Het.5 B-244 Ar. 49 Het.5 B-245 Ar.50 Het.5 B-246 Ar.2 Het.6 B-247 Ar.3 Het.6 B-248 Ar.4 Het.6 B-249 Ar.5 Het.6 B -250 Ar.6 Het.6 B-251 Ar.7 Het.6 B-252 Ar.8 Het.6 B-253 Ar.9 Het.6 B-254 Ar.10 Het.6 B-255 Ar.ll Het.6 B-256 Ar.12 Het.6 B-257 Ar.13 Het.6 B-258 Ar.14 Het.6 B-259 Ar.15 Het.6 B-260 Ar.16 Het.6 B- 261 Ar.17 Het.6 B-262 Ar.18 Het.6 B-263 Ar.19 Het.6 B-264 Ar.20 Het.6 B-265 Ar.21 Het.6 B-266 Ar.22 Het .6 B-267 Ar.23 Het.6 B-268 Ar.24 Het.6 149027.do C -143- 201103430 No. Ar, Het B-269 Ar.25 Het.6 B-270 Ar.26 Het.6 B-271 Ar.27 Het.6 B-272 Ar.28 Het.6 B-273 Ar. 29 Het.6 B-274 Ar.30 Het.6 B-275 Ar.31 Het.6 B-276 Ar.32 Het.6 B-277 Ar.33 Het.6 B-278 Ar.34 Het.6 B -279 Ar.35 Het.6 B-280 Ar.36 Het.6 B-281 Ar.37 Het.6 B-282 Ar.38 Het.6 B-283 Ar.39 Het.6 B-284 Ar.40 Het.6 B-285 Ar.41 Het.6 B-286 Ar.42 Het.6 B-287 Ar.43 Het.6 B-288 Ar.44 Het.6 B-289 Ar.45 Het.6 B- 290 Ar.46 Het.6 B-291 Ar.47 Het.6 B-292 Ar.48 Het.6 B-293 Ar.49 Het.6 B-294 Ar.50 Het.6 B-295 Ar.2 Het .7 B-296 Ar.3 Het.7 B-297 Ar.4 Het.7 B-298 Ar.5 Het.7 B-299 Ar.6 Het.7 B-300 Ar.7 Het.7 B-301 Ar.8 Het.7 B-302 Ar.9 Het.7 No. Ar, Het B-303 Ar.10 Het.7 B-304 Ar.ll Het.7 B-305 Ar.12 Het.7 B-306 Ar .13 Het.7 B-307 Ar.14 Het.7 B-308 Ar.15 Het.7 B-309 Ar.16 Het.7 B-310 Ar.17 Het.7 B-311 Ar.18 Het.7 B-312 Ar.19 Het.7 B-313 Ar.20 Het.7 B-314 Ar_21 Het.7 B-315 Ar.22 Het.7 B-316 Ar.23 Het.7 B-317 Ar.24 Het .7 B-318 Ar.25 Het.7 B-319 A R.26 Het.7 B-320 Ar.27 Het.7 B-321 Ar.28 Het.7 B-322 Ar.29 Het.7 B-323 Ar.30 Het.7 B-324 Ar_31 Het.7 B -325 Ar.32 Het.7 B-326 Ar.33 Het.7 B-327 Ar.34 Het.7 B-328 Ar.35 Het.7 B-329 Ar.36 Het.7 B-330 Ar.37 Het.7 B-331 Ar.38 Het.7 B-332 Ar.39 Het.7 B-333 Ar.40 Het.7 B-334 Ar.41 Het.7 B-335 Ar.42 Het.7 B- 336 Ar.43 Het.7 [si 149027.doc -144- 201103430 No. Ar' Het B-337 Ar.44 Het.7 B-338 Ar.45 Het.7 B-339 Ar.46 Het.7 B-340 Ar.47 Het.7 B-341 Ar.48 Het.7 B-342 Ar.49 Het.7 B-343 Ar.50 Het.7 B-344 Ar.2 Het. 8 B-345 Ar.3 Het. 8 B-346 Ar.4 Het.8 B-347 Ar.5 Het. 8 B-348 Ar.6 Het.8 B-349 Ar.7 Het.8 B-350 Ar.8 Het.8 B-351 Ar .9 Het.8 B-352 Ar.10 Het.8 B-353 Ar.ll Het.8 B-354 Ar.12 Het.8 B-355 Ar.13 Het.8 B-356 Ar.14 Het.8 B-357 Ar.15 Het.8 B-358 Ar.16 Het.8 B-359 Ar.17 Het.8 B-360 Ar.18 Het.8 B-361 Ar.19 Het.8 B-362 Ar. 20 Het.8 B-363 Ar.21 Het.8 B-364 Ar.22 Het.8 B-365 Ar.23 Het.8 B-366 Ar.24 Het.8 B-367 Ar.25 Het.8 B -368 Ar.26 Het.8 B-369 Ar.27 Het. 8 B-370 Ar.28 Het.8 No. Ar' Het B-371 Ar.29 Het.8 B-372 Ar.30 Het.8 B-373 Ar.31 Het.8 B-374 Ar.32 Het.8 B-375 Ar.33 Het.8 B-376 Ar.34 Het.8 B-377 Ar.35 Het.8 B-378 Ar.36 Het.8 B-379 Ar.37 Het.8 B-380 Ar. 3 8 Het.8 B-381 Ar.39 Het.8 B-382 Ar.40 Het.8 B-383 Ar.41 Het.8 B-384 Ar.42 Het.8 B-385 Ar.43 Het.8 B-386 Ar.44 Het.8 B-387 Ar.45 Het.8 B-388 Ar.46 Het.8 B-389 Ar.47 Het.8 B-390 Ar.48 Het.8 B-391 Ar. 49 Het.8 B-392 Ar.50 Het.8 B-393 Ar.2 Het.9 B-394 Ar.3 Het.9 B-395 Ar.4 Het.9 B-396 Ar.5 Het.9 B -397 Ar.6 Het.9 B-398 Ar.7 Het.9 B-399 Ar.8 Het.9 B-400 Ar.9 Het.9 B-401 Ar.10 Het.9 B-402 Ar.ll Het.9 B-403 Ar.12 Het.9 B-404 Ar.13 Het.9 149027.doc •145- 201103430 No. Ar' Het No. At' Het B-405 Ar.14 Het.9 B-439 Ar. 48 Het.9 B-406 Ar.15 Het.9 B-440 Ar.49 Het.9 B-407 Ar.16 Het.9 B-441 Ar.50 Het.9 B-408 Ar.17 Het.9 B -442 Ar.2 Het. 10 B-409 Ar.18 Het.9 B-443 Ar.3 Het. 10 B-410 Ar.19 Het.9 B-444 Ar.4 Het. 10 B-411 Ar.20 Het.9 B-445 Ar.5 Het 10 B-412 Ar.21 Het.9 B-446 Ar.6 Het. 10 B-413 Ar.22 Het.9 B-447 Ar.7 Het. 10 B-414 Ar.23 Het.9 B-448 Ar.8 Het. 10 B-415 Ar.24 Het.9 B-449 Ar.9 Het. 10 B-416 Ar.25 Het.9 B-450 Ar.10 Het. 10 B-417 Ar.26 Het. 9 B-451 Ar.ll Het. 10 B-418 Ar.27 Het.9 B-452 Ar.12 Het. 10 B-419 Ar.28 Het.9 B-453 Ar.13 Het. 10 B-420 Ar .29 Het.9 B-454 Ar.14 Het. 10 B-421 Ar.30 Het.9 B-455 Ar.15 Het. 10 B-422 Ar.31 Het.9 B-456 Ar.16 Het. 10 B-423 Ar.32 Het.9 B-457 Ar.17 Het 10 B-424 Ar.33 Het.9 B-458 Ar.18 Het. 10 B-425 Ar.34 Het.9 B-459 Ar.19 Het. 10 B-426 Ar.35 Het.9 B-460 Ar.20 Het. 10 B-427 Ar.36 Het.9 B-461 Ar.21 Het. 10 B-428 Ar.37 Het.9 B- 462 Ar.22 Het. 10 B-429 Ar.38 Het.9 B-463 Ar.23 Het. 10 B-430 Ar.39 Het.9 B-464 Ar.24 Het. 10 B-431 Ar.40 Het .9 B-465 Ar.25 Het. 10 B-432 Ar.41 Het.9 B-466 Ar.26 Het. 10 B-433 Ar.42 Het.9 B-467 Ar.27 Het. 10 B-434 Ar.43 Het.9 B-468 Ar.28 Het. 10 B-435 Ar.44 Het.9 B-469 Ar.29 Het. 10 B-436 Ar.45 Het.9 B-470 Ar.30 Het. 10 B-437 Ar.46 Het.9 B-471 Ar.31 Het. 10 B-438 Ar.47 Het.9 B-472 Ar.32 Het. 10 [si 149027.doc -146· 201103430 No. Ar' Het B -473 Ar.33 Het.10 B-474 Ar.34 Het. 10 B-475 Ar.35 Het.10 B-476 Ar.36 Het.10 B-477 Ar.37 Het.10 B-478 Ar.38 Het.10 B-479 Ar.39 Het.10 B-480 Ar.40 Het.10 B-481 Ar.41 Het.10 B-482 Ar.42 Het.10 B-483 Ar.43 Het.10 B- 484 Ar.44 Het.10 B-485 Ar.45 Het.10 B-486 Ar.46 Het.10 B-487 Ar.47 Het.10 B-488 Ar.48 Het.10 B-489 Ar.49 Het .10 B-490 Ar.50 Het.10 B-491 Ar.2 Het. 11 B-492 Ar.3 Het. 11 B-493 Ar.4 Het. 11 B-494 Ar.5 Het. 11 B-495 Ar.6 Het. 11 B-496 Ar.7 Het. 11 B-497 Ar.8 Het. 11 B-498 Ar.9 Het. 11 B-499 Ar.10 Het. 11 B-500 Ar.ll Het. 11 B-501 Ar.12 Het. 11 B-502 Ar.13 Het. 11 B-503 Ar.14 Het. 11 B-504 Ar.15 Het. 11 B-505 Ar.16 Het. 11 B-506 Ar .17 Het. 11 No. Ar, Het B-507 Ar.18 Het. 11 B-508 Ar.19 Het. 11 B-509 Ar.20 Het. 11 B-510 Ar.21 Het. 11 B-511 Ar. 22 Het. 11 B-512 Ar.23 Het. 11 B-513 Ar.24 Het. 11 B-514 Ar.25 Het. 11 B-515 Ar.26 Het. 11 B-516 Ar.27 Het. 11 B-517 Ar.28 Het. 11 B-518 Ar.29 Het. 11 B-519 Ar.30 Het. 11 B-520 Ar. 31 Het. 11 B-521 Ar.32 Het. 11 B-522 Ar.33 Het. 11 B-523 Ar.34 Het. 11 B-524 Ar.35 Het. 11 B-525 Ar.36 Het. 11 B -526 Ar.37 Het. 11 B-527 Ar.38 Het. 11 B-528 Ar.39 Het 11 B-529 Ar.40 Het. 11 B-530 Ar.41 Het. 11 B-531 Ar.42 Het 11 B-532 Ar.43 Het. 11 B-533 Ar.44 Het. 11 B-534 Ar.45 Het. 11 B-535 Ar.46 Het. 11 B-536 Ar.47 Het. 11 B-537 Ar.48 Het. 11 B-538 Ar.49 Het. 11 B-539 Ar.50 Het. 11 B-540 Ar.2 Het. 12 149027.doc -147· 201103430 No. At' Het B-541 Ar.3 Het.12 B-542 Ar.4 Het.12 B-543 Ar.5 Het.12 B-544 Ar.6 Het.12 B-545 Ar.7 Het.12 B-546 Ar.8 Het.12 B- 547 Ar.9 Het.12 B-548 Ar.10 Het.12 B-549 Ar.ll Het.12 B-550 Ar.12 Het.12 B-551 Ar.13 Het.12 B-552 Ar.14 Het .12 B-553 Ar.15 Het.12 B-554 Ar.16 Het.12 B-555 Ar.17 Het.12 B-556 Ar.18 Het.12 B-557 Ar.19 Het.12 B-558 Ar.20 Het.12 B-559 Ar.21 Het.12 B-560 Ar.22 Het.12 B-561 Ar.23 Het.12 B-562 Ar.24 Het.12 B-563 Ar.25 Het.12 B-564 Ar.26 Het.12 B-565 Ar.27 Het.12 B-566 Ar.28 Het.12 B-567 Ar. 29 Het.12 B-568 Ar.30 Het.12 B-569 Ar.31 Het.12 B-570 Ar.32 Het.12 B-571 Ar.33 Het.12 B-572 Ar.34 Het.12 B -573 Ar.35 Het.12 B-574 Ar.3 6 Het.12 No. Ar' Het B-575 Ar.37 Het.12 B-576 Ar.38 Het. 12 B-577 Ar.39 Het.12 B -578 Ar.40 Het.12 B-579 Ar.41 Het.12 B-580 Ar.42 Het.12 B-581 Ar.43 Het.12 B-582 Ar.44 Het.12 B-583 Ar.45 Het.12 B-584 Ar.46 Het.12 B-585 Ar.47 Het.12 B-586 Ar.48 Het.12 B-587 Ar.49 Het.12 B-588 Ar.50 Het.12 B- 589 Ar.2 Het. 13 B-590 Ar.3 Het. 13 B-591 Ar.4 Het. 13 B-592 Ar.5 Het. 13 B-593 Ar.6 Het. 13 B-594 Ar.7 Het 13 B-595 Ar.8 Het. 13 B-596 Ar.9 Het. 13 B-597 Ar.10 Het. 13 B-598 Ar.ll Het. 13 B-599 Ar.12 Het. 13 B-600 Ar.13 Het. 13 B-601 Ar.14 Het. 13 B-602 Ar.15 Het. 13 B-603 Ar.16 Het. 13 B-604 Ar.17 Het. 13 B-605 Ar.18 Het. 13 B-606 Ar.19 Het. 13 B-607 Ar.20 Het. 13 B-608 Ar.21 Het. 13 149027.doc -148- 201103430 At' Het B-609 Ar.22 Het.13 B-610 Ar.23 Het. 13 B-611 Ar.24 Het.13 B-612 Ar.25 Het.13 B-613 Ar.26 Het.13 B- 614 Ar.27 Het.13 B-615 Ar.28 Het.13 B-616 Ar.29 Het.13 B-617 Ar.30 Het.13 B-618 Ar.31 Het.13 B-619 Ar.32 Het .13 B-620 Ar.33 Het.13 B-621 Ar.34 Het.13 B-622 Ar.35 Het.13 B-623 Ar.36 Het.13 B-624 Ar.37 Het.13 B-625 Ar.38 Het.13 B-626 Ar.39 Het.13 B-627 Ar.40 Het.13 B-628 Ar.41 Het.13 B-629 Ar.42 Het.13 B-630 Ar.43 Het. 13 B-631 Ar.44 Het.13 B-632 Ar.45 Het.13 B-633 Ar.46 Het.13 B-634 Ar.47 Het.13 B-635 Ar.48 Het.13 B-636 Ar .49 Het.13 B-637 Ar.50 Het.13 B-638 Ar.2 Het. 14 B-639 Ar.3 Het. 14 B-640 Ar.4 Het. 14 B-641 Ar.5 Het. 14 B-642 Ar.6 Het. 14 No. Ar' Het B-643 Ar.7 Het. 14 B-644 Ar.8 Het. 14 B-645 Ar.9 Het. 14 B-646 Ar.10 Het: 14 B -647 Ar.ll Het. 14 B-648 Ar.12 Het. 14 B-649 Ar.13 Het. 14 B-650 Ar.14 Het. 14 B-651 Ar.15 Het. 14 B-652 Ar.16 Het. 14 B-653 Ar.17 Het. 14 B-654 Ar.18 Het. 14 B-655 Ar.19 Het. 14 B-656 Ar.20 Het. 14 B -657 Ar.21 Het. 14 B-658 Ar.22 Het. 14 B-659 Ar.23 Het. 14 B-660 Ar.24 Het. 14 B-661 Ar.25 Het. 14 B-662 Ar.26 Het. 14 B-663 Ar.27 Het. 14 B-664 Ar.28 Het. 14 B-665 Ar.29 Het. 14 B-666 · Ar.30 Het. 14 B-667 Ar.31 Het. 14 B -668 Ar.32 Het. 14 B-669 Ar.33 Het. 14 B-670 Ar.34 Het. 14 B-671 Ar.35 Het. 14 B-672 Ar.36 Het. 14 B-673 Ar.37 Het. 14 B-674 Ar.38 Het. 14 B-675 Ar.39 Het. 14 B-676 Ar.40 Het. 14 149027.doc •149· 201103430 No. Ar' Het B-677 Ar.41 Het. 14 B-678 Ar.42 Het. 14 B-679 Ar.43 Het. 14 B-680 Ar.44 Het. 14 B-681 Ar.45 Het. 14 B-682 Ar.46 Het. 14 B-683 Ar. 47 Het. 14 B-684 Ar.48 Het. 14 B-685 Ar.49 Het. 14 B-686 Ar.50 Het. 14 B-687 Ar.2 Het.15 B-688 Ar.3 Het.15 B -689 Ar.4 Het.15 B-690 Ar.5 Het.15 B-691 Ar.6 Het.15 B-692 Ar.7 Het.15 B-693 Ar.8 Het.15 B-694 Ar.9 Het.15 B-695 Ar.10 Het.15 B-696 Ar.ll Het.15 B-697 Ar.12 Het.15 B-698 Ar.13 Het.15 B-699 Ar.14 Het.15 B- 700 Ar. 15 ' Het.15 B-701 Ar.16 Het.15 B-702 Ar_17 Het.15 B-703 Ar.18 Het.15 B-704 Ar.19 Het.15 B-705 Ar.20 Het.15 B-706 Ar.21 Het.15 B-707 Ar.22 Het.15 B-708 Ar.23 Het. 15 B-709 Ar.24 Het.15 B-710 Ar.25 Het.15 No. Ar, Het B-711 Ar.26 Het.15 B-712 Ar.27 Het. 15 B-713 Ar.28 Het.15 B-714 Ar.29 Het.15 B-715 Ar.30 Het.15 B-716 Ar.31 Het.15 B-717 Ar.32 Het.15 B-718 Ar.33 Het.15 B-719 Ar. 34 Het.15 B-720 Ar.35 Het.15 B-721 Ar.36 Het.15 B-722 Ar.37 Het.15 B-723 Ar.38 Het.15 B-724 Ar.39 Het.15 B -725 Ar.40 Het.15 B-726 Ar.41 Het.15 B-727 Ar.42 Het.15 B-728 Ar.43 Het.15 B-729 Ar.44 Het.15 B-730 Ar.45 Het.15 B-731 Ar.46 Het.15 B-732 Ar.47 Het.15 B-733 Ar.48 Het.15 B-734 Ar.49 Het.15 B-735 Ar.50 Het.15 B- 736 Ar.2 Het. 16 B-737 Ar.3 Het. 16 B-738 Ar.4 Het. 16 B-739 Ar.5 Het. 16 B-740 Ar.6 Het. 16 B-741 Ar.7 Het 16 B-742 Ar.8 Het. 16 B-743 Ar.9 Het. 16 B-744 Ar.10 Het. 16

LSI 149027.doc -150- 201103430 編號 Ar' Het B-745 Ar.ll Het.16 B-746 Ar. 12 Het.16 B-747 Ar.13 Het.16 B-748 Ar.14 Het.16 B-749 Ar.15 Het.16 B-750 Ar.16 Het.16 B-751 Ar.17 Het.16 B-752 Ar.18 Het.16 B-753 Ar.19 Het.16 B-754 Ar.20 Het.16 B-755 Ar.21 Het.16 B-756 Ar.22 Het.16 B-757 Ar.23 Het.16 B-758 Ar.24 Het.16 B-759 Ar.25 Het.16 B-760 Ar.26 Het.16 B-761 Ar.27 Het.16 B-762 Ar.28 Het.16 B-763 Ar.29 Het.16 B-764 Ar.30 Het.16 編號 Ar, Het B-765 Ar.31 Het.16 B-766 Ar.32 Het.16 B-767 Ar.33 Het.16 B-768 Ar.34 Het.16 B-769 Ar.35 Het.16 B-770 Ar.36 Het.16 B-771 Ar.37 Het.16 B-772 Ar.38 Het.16 B-773 Ar.39 Het.16 B-774 Ar.40 Het.16 B-775 Ar.41 Het.16 B-776 Ar.42 Het.16 B-777 Ar.43 Het.16 B-778 Ar.44 Het.16 B-779 Ar.45 Het.16 B-780 Ar.46 Het.16 B-781 Ar.47 Het.16 B-782 Ar.48 Het.16 B-783 Ar.49 Het.16 B-784 Ar.50 Het.16 基團Ar.2至Ar.50對應於上文所列作為式Ar.2至Ar.50之 基團的Ar之特定實施例的基團,且基團Het.l至Het.16對應 於上文所列作為式Het.l至Het.16之基團的Het之特定實施 例的基團。 基團Ar.2至Ar.50對應於上文所列作為式Ar.2至Ar.50之 基團的Ar之特定實施例的基團。基團Het.l至Het. 16對應於 上文所列作為式Het.l至Het. 16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1.1至1.24、1.49至1.72、1.97 149027.doc -151 - 201103430 至 Ι·120、1.145 至 1.168 ; II.1 至 Π_24 及 Π·49 至 „.72 之化合 物。在此等化合物中,較佳為化合物丨丨至〗^、149至 1.60 &gt; I.97J.I.108 ^ 1.145^1.156 ; 11.1^.11.12^11.49^ ΙΙ.60。尤佳為化合物! 2、j 5〇、j 98、Ι 146、η 2及^ 式I及II之化合物可藉由一或多種下列如下文流程〗至9及 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II所定義。 式I化合物,其中R1為Him為〇(或化合,其中Ria為 )可:δ々IL程1中所概述藉由硫化相應的三哇衍生物IV來製 備。硫化反應可類似於(例如,如wo 96/41804中所述之) 已知方法來進行。舉例而言,三唾基環可首先用以下強驗 去除質子化,例如有機鋰鹼,諸如正丁基鋰、第三丁基鋰 或第二丁基鐘’二異丙胺化經、氫化鈉胺化納或與四甲 基乙一胺(TMEDA)混合之第三丁醇斜,隨後所得陰離子與 元素;’I反應 般使用粉末狀硫。反應一般在惰性溶劑, 諸如醚類(例如二乙醚、甲基第三丁基醚、四氫呋喃或二 惡烷)、一甲氧基乙烷、液氨、=甲亞砜或二曱基甲醯胺 中進订。反應溫度不是报關鍵且可在例如_7〇至+5〇。〇,較 佳-70至+0C之範圍内。或者,硫化反應可在不存在鹼之情 _ 藉由使7與元素硫在高沸點溶劑(諸如N-曱基。比嘻咬 嗣、二°惡院或Ν,Ν-二U曱醯胺)中反應同時加熱至例如 。至50 C來進行。在完成該反應之後,例如藉由添加水 °拎义諸如無機酸(例如稀硫酸或鹽酸)、乙酸或氯化 錄來水解所得混合物,得㈣合物卜LSI 149027.doc -150- 201103430 No. Ar' Het B-745 Ar.ll Het.16 B-746 Ar. 12 Het.16 B-747 Ar.13 Het.16 B-748 Ar.14 Het.16 B- 749 Ar.15 Het.16 B-750 Ar.16 Het.16 B-751 Ar.17 Het.16 B-752 Ar.18 Het.16 B-753 Ar.19 Het.16 B-754 Ar.20 Het .16 B-755 Ar.21 Het.16 B-756 Ar.22 Het.16 B-757 Ar.23 Het.16 B-758 Ar.24 Het.16 B-759 Ar.25 Het.16 B-760 Ar.26 Het.16 B-761 Ar.27 Het.16 B-762 Ar.28 Het.16 B-763 Ar.29 Het.16 B-764 Ar.30 Het.16 No. Ar, Het B-765 Ar .31 Het.16 B-766 Ar.32 Het.16 B-767 Ar.33 Het.16 B-768 Ar.34 Het.16 B-769 Ar.35 Het.16 B-770 Ar.36 Het.16 B-771 Ar.37 Het.16 B-772 Ar.38 Het.16 B-773 Ar.39 Het.16 B-774 Ar.40 Het.16 B-775 Ar.41 Het.16 B-776 Ar. 42 Het.16 B-777 Ar.43 Het.16 B-778 Ar.44 Het.16 B-779 Ar.45 Het.16 B-780 Ar.46 Het.16 B-781 Ar.47 Het.16 B -782 Ar.48 Het.16 B-783 Ar.49 Het.16 B-784 Ar.50 Het.16 The groups Ar.2 to Ar.50 correspond to the above listed formulas Ar.2 to Ar.50. a group of a specific embodiment of Ar of the group, and the groups Het.l to Het.16 correspond to The groups of the specific examples of Het listed above as groups of the formulas Het.l to Het.16. The groups Ar. 2 to Ar. 50 correspond to the groups of the specific examples of Ar listed above as the group of the formulae Ar. 2 to Ar. The groups Het.l to Het. 16 correspond to the groups of the specific examples of Het listed above as groups of the formulas Het.l to Het. Among the above compounds, preferred are compounds of the formulae 1.1 to 1.24, 1.49 to 1.72, 1.97 149027.doc - 151 - 201103430 to Ι·120, 1.145 to 1.168; II.1 to Π24 and Π·49 to „.72. Among these compounds, preferred are compounds 丨丨 to ^, 149 to 1.60 &gt; I.97J.I.108 ^ 1.145^1.156; 11.1^.11.12^11.49^ ΙΙ.60. More preferably a compound! 2 , j 5 〇, j 98, 146 146, η 2 and ^ Compounds of the formulae I and II can be prepared by one or more of the following methods and variants as described in Schemes 9 to 9 and in the synthesis details. As defined above for Formulas I and II. Compounds of Formula I wherein R1 is Him is 〇 (or compounded, wherein Ria is) can be prepared by sulfonating the corresponding tri-Wow derivative IV as outlined in δ々IL Process 1. The sulfidation reaction can be carried out analogously to the known methods (for example, as described in WO 96/41804). For example, the trisap ring can be firstly removed by protonation, such as an organolithium base, such as a positive Butyllithium, tert-butyllithium or a second butyl bell 'diisopropyl amination, sodium hydride sodium or with tetramethylethylamine (TME) DA) mixed third butanol is inclined, and then the obtained anion is reacted with the element; 'I reacts with powdered sulfur. The reaction is generally carried out in an inert solvent such as ether (for example, diethyl ether, methyl tert-butyl ether, tetrahydrofuran or two). The order of the alkylene oxide, monomethoxyethane, liquid ammonia, = sulfoxide or dimethyl carbamide is not specified. The reaction temperature is not critical and can be, for example, _7 〇 to +5 〇. -70 to +0C. Alternatively, the sulfurization reaction can be carried out in the absence of a base _ by making 7 with elemental sulfur in a high boiling solvent (such as N-fluorenyl). The reaction in Ν-di-U amide is simultaneously heated to, for example, to 50 C. After completion of the reaction, for example, by adding water, such as a mineral acid (for example, dilute sulfuric acid or hydrochloric acid), acetic acid or chlorine Hydrogenation to hydrolyze the resulting mixture to obtain (four) complex

ESI 149027.doc •152· 201103430 流程1ESI 149027.doc •152· 201103430 Process 1

如流程2中所概述,三唑化合物w可類似於已知方法(諸 如在例如EP-A-〇〇65485中所述)來製備。舉例而言,化合 物1(其中X為良好的脫離基’諸如鹵素原子,尤其c卜h 或I’苯基磺醯基氧基、對甲笨磺醯基氧基、三氟乙醯氧 基或烷基磺醯基氧基,諸如甲磺醯基氧基)可與乐 三唑化合物2(其中M為氫原子或金屬原子,尤其鹼金屬原 子,諸如Li、Na或K)反應。在MgH之情況下,反應宜在 驗,諸如驗金屬虱化物(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(例如碳 酸鈉、碳酸钾、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-二甲基甲醯胺、N,N_二曱基乙醯胺、二甲亞碼、乙 腈、苯甲腈、醚類(諸如二乙醚、二丙醚、甲基第三丁基 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、甲苯、二甲苯、氣 149027.doc •153- 201103430 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1 7〇。〇之範圍 内。反應宜在反應混合物之回流溫度下進行。 流程2As outlined in Scheme 2, the triazole compound w can be prepared analogously to known methods, such as described, for example, in EP-A-〇〇65485. For example, compound 1 (wherein X is a good leaving group such as a halogen atom, especially c b or I'phenylsulfonyloxy, p-methylsulfonyloxy, trifluoroacetoxy or An alkylsulfonyloxy group, such as a methylsulfonyloxy group, can be reacted with a triazole compound 2 (wherein M is a hydrogen atom or a metal atom, especially an alkali metal atom such as Li, Na or K). In the case of MgH, the reaction is preferably tested, such as metal halides (such as sodium hydride, potassium hydride), metal hydroxides (such as sodium hydroxide, potassium hydroxide), alkali metal carbonates (such as sodium carbonate, It is carried out in the presence of potassium carbonate, carbonic acid planing or a suitable amine such as triethylamine, triethylenediamine, piperidine, pyridine, 4-dimethylaminopyridine or 4-pyrrolidinopyridine. 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-dimethylformamide, N,N-dimercaptoacetamide, dimethyl methacrylate, acetonitrile, benzonitrile, Ethers (such as diethyl ether, dipropyl ether, methyl tert-butyl ether, tetrahydrofuran or dioxane) and the like, and can be used in combination with other less polar inert solvents such as benzene, toluene, and Toluene, gas 149027.doc • 153- 201103430 Benzene, nitrobenzene, hexane, heptane, petroleum ether and the like. The reaction temperature is not critical and can be, for example, up to 22 Torr. Preferably, it is 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 2

A 如以下流程3中所概述,化合物1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HO-A-OH較佳在形成共沸 物的化合物(諸如苯、甲苯、二甲苯、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(ketaUzati〇n reaction)。後續鹵化所得縮酮4產生縮酮1,其中χ為鹵素 原子,若需要,則其可轉化為化合物丨,其中χ為除鹵素以 外的脫離基。 流程3A, as outlined in Scheme 3 below, Compound 1 can in turn be prepared analogously to known methods, such as those described in EP-A-0 065 485 or Synthesis, 1974, I, 23. For example, ketone 3 may be reacted with the diol HO-A-OH preferably in the presence of a compound forming an azeotrope such as benzene, toluene, xylene, gas or tetra-methane, which may also act as a reaction solvent. Several hours. The ketalization reaction (ketaUzati〇n 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, wherein hydrazine is a halogen atom which, if desired, can be converted to the oxime of the compound, wherein hydrazine 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)次 [ 149027.doc -154- 201103430 得,其中X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、C卜Br或I,苯基磺醯基氧基、對甲 苯項S备基氧基、三氟乙醯氧基或烷基磺醯基氧基,諸如甲 磺醯基氧基,或反之亦然,其中X丨為良好的脫離基且父2為 基團Y-H或Y-M。在χΐ或X2為γ-Η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 一胺、。底。定、。比°定、4 -二甲基胺基〇比咬、4 -吼ρ各咬基。比。定) 存在下進行。若脫離基X1或X2為C1或ΒΙ·,則可藉由添加鹼 金屬碘化物(諸如Nal或ΚΙ)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-二曱基曱醯胺、n,N-二甲基乙醯胺、二甲亞 石風、乙腈、苯曱腈、醚類(諸如二乙醚、二丙醚、曱基第 二丁基、四氫吱喃或二惡烧)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〇至220°C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。 流程4As outlined in Scheme 4 below, the ketone 3 can be similar to known methods (such as the condensation reaction of compounds 5 and 6 as described, for example, in ΕΡ-Α-0065485) [149027.doc-154-201103430, where X Is a group γ_Η or Υ-Μ, wherein Μ is a metal atom, especially an alkali metal atom such as Li, Na or Κ, and X 2 is a good leaving group such as a halogen atom such as F, C b Br or I, phenyl Sulfhydryloxy, p-toluene, S, benzyloxy, trifluoroacetoxy or alkylsulfonyloxy, such as methylsulfonyloxy, or vice versa, wherein X is a good detachment Base and parent 2 are the group YH or YM. In the case where ruthenium or X2 is γ-Η, the reaction is preferably carried out in a base such as an alkali metal hydride (for example, sodium hydride or potassium hydride), an alkali metal hydroxide (for example, sodium hydroxide or potassium hydroxide), or an alkali metal carbonate. a salt (such as sodium carbonate, potassium carbonate, carbonic acid planing) or a suitable amine (for example, triethylamine, tri-ethylamine, succinct, stipulated, 4 - dimethylamino hydrazine, 4 -吼ρ Each bite base. The ratio is determined to exist. If the leaving group X1 or X2 is C1 or ΒΙ·, the reaction can be promoted by adding an alkali metal iodide such as Nal or hydrazine. 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-didecylguanamine, n,N-dimethylacetamide, dimethyl sulphide, acetonitrile, benzoquinone , ethers (such as diethyl ether, dipropyl ether, decyl second butyl, tetrahydrofuran or dioxo) and the like, and can be used in combination with other less polar inert solvents, such as benzene, Toluene, diphenyl, benzene, nitrobenzene, hexane, heptane, petroleum ether and the like. The reaction temperature is not critical and can be, for example, in the range of 〇 to 220 ° C and preferably 80 to 170 ° C. The reaction is preferably carried out at the reflux temperature of the reaction mixture. Process 4

149027.doc -155- 201103430 作為流程4中所iiic夕士·、+ ,, 7 it之方法的替代,如以下流程5中所概 述,酮3(其中γ立 - 3))可類似於EP-A-0065485中所述 之方法藉由碳酸酯7之脫羧反應來製備。其又可自羥基化 &quot; 來製備.备基化合物8與以下碳酸之雙官能衍生物 9諸如光氣、自素甲酸二酉旨、二院基碳酸二酷或二苯基 厌酉欠一s曰反應,且與羥基化合物1〇進一步反應。藉由在實 際上或在呵沸點惰性溶劑(諸如二苯醚或乙二醇二甲醚)中 力…7至120至220 C範圍内之溫度進行脫羧反應。 流程5 Αγ-ΟΗ 8149027.doc -155- 201103430 As an alternative to the method of iiic, +, and 7 it in Scheme 4, as outlined in Scheme 5 below, ketone 3 (where γ  3) can be similar to EP- The process described in A-0065485 is prepared by the decarboxylation reaction of carbonate 7. It can also be prepared from hydroxylation &quot;. The base compound 8 and the following bifunctional derivative of carbonic acid 9 such as phosgene, self-acid formic acid, second-complexed carbonic acid or diphenyl-anthraquinone The hydrazine reacts and further reacts with the hydroxy compound 1 hydrazine. The decarboxylation reaction is carried out by a temperature in the range of from 7 to 120 to 220 C in an inert solvent such as diphenyl ether or ethylene glycol dimethyl ether. Flow 5 Αγ-ΟΗ 8

also

ch3 • co2Ch3 • co2

作為流程2中所述方法的替代,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^ 與二醇HO_A-〇H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。As an alternative to the process described in Scheme 2, compound IV can be similar to that described in EP-A-0 065 485 by ketalization of the ketone with the diol HO_A-〇H, as outlined in Scheme 6 below. To prepare. The ketalization reaction can be carried out under the reaction conditions described in Scheme 3.

149027.doc -156- 201103430 如以下流程7中所概述’酮11又可類似於ep-A-0065485 中所述之方法,藉由使化合物12(其中χ為良好的脫離基, 諸如鹵素原子,尤其Cl、Br或I,苯基磺醯基氧基、對甲 苯磧醯基氧基、三氟乙醯氧基或烷基磺醯基氧基,諸如甲 石買醯氧基)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之函化反應獲 得。 流程7149027.doc -156- 201103430 As outlined in Scheme 7 below, 'ketone 11 can be similar to that described in ep-A-0065485 by compound 12 (wherein oxime is a good leaving group, such as a halogen atom, In particular, Cl, Br or I, phenylsulfonyloxy, p-tolylhydryloxy, trifluoroethyloxy or alkylsulfonyloxy, such as methyl methoxy, and triazole compounds 2 Prepared by reaction under the reaction conditions described for the reaction in Scheme 2. Compound 12 is again obtainable from the functionalization 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,尤其驗金 屬原子,諸如Li、Na或Κ,且X2為良好的脫離基,諸如鹵 素原子’尤其Cl、Br或I,笨基項醢基氧基、對甲笨確醯 基氧基、三氟乙醯氧基或烷基磺醯基氧基,諸如曱績醯基 氧基’或反之亦然’其中X1為良好的脫離基且χ2為基團γ_ Η 或 γ_Μ 〇 流程8As an alternative to the process described in Scheme 2, as outlined in Scheme 8 below, Compound IV can be similar to the process described in EP-A-0 065 485 by reacting compounds 13 and 14 in the reaction conditions described for Scheme 4. Prepared by condensation, wherein X1 is a group YH or YM, wherein ruthenium is a metal atom, especially a metal atom such as Li, Na or ruthenium, and X2 is a good leaving group such as a halogen atom 'in particular Cl, Br or I a stupid base fluorenyloxy, p-decyloxy, trifluoroacetoxy or alkylsulfonyloxy, such as fluorenyloxy or vice versa where X1 is good Detached group and χ2 is a group γ_ Η or γ_Μ 〇 Process 8

Ar-χι 13Ar-χι 13

A I49027.doc -157- 201103430 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Ιν(其中Y為〇( = 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醋 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9A I49027.doc -157- 201103430 As an alternative to the method described in Scheme 2, the compound Ιν (where Y is 〇(=IV')) can be similar to that described in EP-A-0065485, as outlined in Scheme 9 below. The process 'prepared by decarboxylation of carbonate vine 15 under the reaction conditions described for 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。 右上述反應物中之基團對各別反應呈現惰性,則其可存 在於上述反應步驟中或可在後一階段引入(例如)化合物w 中〇 式I化合物(其中R1不為氫且⑺為…可由化合物^(其中 R1==H且m=0)來製備。 式I化合物(其中111為〇且尺1為Ci_Ci〇烷基、鹵烷 基、c2-c1()稀基、c2_Cl()li 稀基、C2_Ci〇快基、C2夂^炔 基、cvc丨〇環烷基、cvCi〇鹵環烷基、苯基、苯基π”。烷 基,其中最後2個提及基團中的苯基部分可如上所述經取 代,及含有1、2或3個選自N、〇及3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DE_A_19520098 4W〇 96/418〇4中 149027.doc -158- 201103430 所述之方法,藉由使化合物I(其中m為0且R1為Η)與化合物 R -LG(其中Ri具有上述含義中之一者且lg為脫離基,諸 如齒基(例如Cl、Br、I)、曱苯磺酸酯基或甲磺酸酯基)反 應來製備。合適之鹼為例如,鹼金屬氫化物(例如氫化 納、氣化鉀)' 鹼金屬氫氧化物(例如氮氧化鈉、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(例如曱醇鈉、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 鋰及一異丙胺鋰)。一般在合適之溶劑中進行反應。合適 之/合劑為例如甲苯、N_曱基吡咯啶酮、醚類(例如二乙 醚、四氫呋喃、二噁烷、丨,2_二甲氧基乙烷)、乙腈、N,N_ 一曱基甲醯胺或二曱亞;e風。 或者,式I化合物(其中且烷基、C丨 齒烧基C2-C1G烯基、c2-C1Q鹵烯基、c2-C1()炔基、c2-C10 鹵炔基、&lt;:3-(:10環烷基、C3_Ci〇鹵環烷基、苯基、苯基 C4烷基,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,及含有1、2或3個選自Ν、Ο及s之雜原子作為 環成貝的5-或6-員飽和、部分不飽和或芳族雜環,其中雜 %可如上所述經取代)可類似於Heter〇cycles, 23(7), 1649, 1985中所述之方法,藉由在類似於針對流程1所述之 條件下使化合物IV與二硫化物Rl_s_s_Rl在強驗存在下反應 來製備。 &amp; 式I化合物(其巾爪為〇且Rl為_c(=〇)r8或件s)r8)可類似 於DE-A-19617461 中所述之 f、土 ^ . 斤迩之方法,藉由使化合物1(其中爪為 149027.doc -159- 201103430 0 且 R】為 Η)與化合物 r8_c( = 〇&gt;w、r8_c( = s) w、尺8, -N=C=0或R8,_N=C = S(其中r8具有上述含義中之,^為 G-C⑺烷基或C|_Cl0鹵烷基且w為良好的脫離基諸如鹵 基(例如CM、Br、υ、烷氧基(例如甲烧氧基、乙烷氧基鳩 五氟苯氧基)在鹼存在下反應來製備。合適之鹼為例如, 驗金屬氫化物(例如氫化鈉、氩化_)、驗金屬氫氧化物(例 如虱氧化鈉、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、曱醇鉀、乙醇 鈉、乙醇鉀、第三丁醇斜)或有機鐘驗(例如正丁基鐘、第 丁基鋰第一丁基鋰及二異丙胺鋰反應一般在合適 之溶劑中進行。合適之溶劑為例如甲苯、Ν_曱基。比㈣ 酮、醚類(例如二乙醚、四氫呋喃、二噁烷、i,2-二甲氧基 乙烷)、乙腈、N,N•二甲基甲醯胺或二甲亞砜。 式1化合物(其中m為0且為-s〇2r8)可類似於de_a_ 1962059G中所述之方法,藉由使化合物z(其中⑺為。且…為 H)與化合物R^s〇2_w(其中尺8具有上述含義中之一且w為 良好的脫離基,諸如函基(例如C卜BH氧基(例如 甲烧氧基、乙貌氧基)或五氟苯氧基)在驗存在下反應來製 備。適之驗為例如,驗金屬氫化物(例如氮化納、氫化 1甲)、驗金屬氣氧化物(例如氫氧化鈉、IL氧化钟)、驗金屬 碳酸鹽(例如碳酸鋼、碳酸_、碳酸鉋)、驗金屬醇鹽(例如 甲醇納、甲醇卸、乙醇鈉、6醇卸、第三丁醇卸)或有機 裡驗(例如正丁農相、铉_ τ^ 丞鋰、第一丁基鋰、第三丁基鋰、二異丙 胺)反應I在合適之溶劑中進行。合適之溶劑為例 [S] 149027.doc •160· 201103430 如甲苯、N-甲基吡咯啶_、醚類(例如二乙醚、四氫呋 南一惡烷、丨,2-二甲氧基乙烷)、乙腈、n,N-二曱基甲醯 胺或二曱亞石風。 弋化&amp;物(其中且R1為_CN)可類似於DE_A· 196204G7中所述之方法,藉由使化合物:(其中@為G且 Η)與化合物CN_W(其十评為良好的脫離基,諸如函基(例如 C卜Br、I))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)、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 丁土鋰第一丁基鐘、二異丙胺經)。反應一般在合適 之溶劑中進行。合適之溶劑為例如甲苯、N_甲基η比洛咬 酮、醚類(例如二乙醚、四氫。夫。南、二噁院、以-二甲氧基 乙烷)、乙腈、N,N-二甲基甲醯胺或二甲亞砜。 式I化合物(其中爪為0且Rl為M)可類似於de a i96i7282 中所述之方法’藉由使化合W (其中且r、h)與胺 NRaRbRe(其中Ra、RbA Re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化〇物(其中m為0且R1為式ΠΙ之基團)可類似於WO 97/43269中所述之方法,藉由使化合物i(其中@為〇且以 H)與齒素(尤其硬)在驗存在下反應來製備。合適之驗為例 如,鹼金^屬氫化物(例如氫化納、氫化卸)、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 149027.doc • 161 · 201103430 鈉、碳酸鉀、碳酸鉍、 金屬醇鹽(例如曱醇鈉、曱醇 鉀、乙.鈉、乙醇鉀、 基經、第二丁基鐘、第二物或有機㈣(例如正丁 般在合適之溶劑中進二、:鋰、二異丙胺鋰)。反應- 丁 0適之溶劑為例如曱苯、N-曱基 吡咯啶酮、醚類(例如二乙 « g- 7 ^ , 虱夫喃、二噁烷、i,2·二 )、乙睛、Ν,Ν·二曱基曱酿胺或二甲亞颯。 物(其中GJ·R1為·ρ(=φιλι°)可類似請 99/05149中所述之方法來製備。 1式II化合物(其中Ru不為氫)可藉由類似於化合物1(其中 , 述轉化反應使NRU基團(其中R】、H)反應變為 R不為Η之化合物來製備。 化合物Κ其中m為“戈2)可藉由氧化反應自各別化合物 K其夠來製備。或者,化合W(其中^2)可藉由首 土裒去除質子化,隨後與磺醯氣R^SC^Cl反應自 化:物IV來t備。化合物z(其中①為可藉由首先使三唾 土裒去除吳子化,隨後與硫酸氯化物或式R^OSC^Cl之硫酸 酉旨氯化物(其中R1 6 $ r K係選自虱、Ci_Ci。院基、Ci_c〗。齒烷基、 C2-C1G稀基、c2_Ci。齒烯基、c2_Ci。炔基、C2_C|❹幽炔基、 C3-c1()壞烧基、C3_Cig_環烧基、苯基、苯基_Ci_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’及含有1、2或3個選自N、〇及8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。 右個別化合物不能經由上述途徑製備,則其可藉由其他 ES3 I49027.doc •162· 201103430 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由揮 發性組份純化其。若獲得呈固體狀之_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 ΟCompounds 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. The group in the above right reactant is inert to the respective reaction, which may be present in the above reaction step or may be introduced in the latter stage, for example, in the compound w, the compound of the formula I (wherein R1 is not hydrogen and (7) is ... can be prepared from the compound ^ (wherein R1 == H and m = 0). The compound of the formula I (wherein 111 is oxime and the rule 1 is Ci_Ci 〇 alkyl, haloalkyl, c2-c1 (), c2_Cl() Li dilute, C2_Ci 〇 fast radical, C 2 夂 ^ alkynyl, cvc 丨〇 cycloalkyl, cvCi 〇 halocycloalkyl, phenyl, phenyl π". alkyl, of which the last two mentioned in the group The phenyl moiety may be substituted as described above, and a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, oxime and 3 as ring members, wherein The heterocyclic ring may be substituted as described above) and may be similar to the method described in DE _A_19520098 4W 〇 96/418 〇 4 149027. doc-158-201103430 by compound I (wherein m is 0 and R1 is Η) R-LG (wherein Ri has one of the above meanings and lg is a leaving group such as a dentate group (e.g., Cl, Br, I), an anthracenesulfonate group or a mesylate group) Suitable bases are, for example, alkali metal hydrides (e.g., sodium hydride, potassium hydride) 'alkali metal hydroxides (e.g., sodium oxynitride, potassium hydroxide), alkali metal carbonates (e.g., sodium carbonate, potassium carbonate, Barium carbonate), alkali metal alkoxide (such as sodium decoxide, potassium decoxide, sodium ethoxide, potassium ethoxide, potassium butoxide) or organic lithium base (such as n-butyl lithium, second butyl lithium, third butyl) Lithium hydride and lithium isopropylamine. Generally, the reaction is carried out in a suitable solvent. Suitable/mixtures are, for example, toluene, N-decylpyrrolidone, ethers (for example, diethyl ether, tetrahydrofuran, dioxane, hydrazine, 2 _Dimethoxyethane), acetonitrile, N,N-monomethylcarbamide or diterpenoid; e wind. Or, a compound of formula I (wherein an alkyl group, a C-dentate C2-C1G alkenyl group, c2-C1Q haloalkenyl, c2-C1()alkynyl, c2-C10 haloalkynyl, &lt;: 3-(:10 cycloalkyl, C3_Ci〇 halocycloalkyl, phenyl, phenyl C4 alkyl, The phenyl moiety in the last two of the groups mentioned may be substituted as described above, and contains 1, 2 or 3 heteroatoms selected from the group consisting of ruthenium, osmium and s as 5- or 6- a saturated, partially unsaturated or aromatic heterocyclic ring in which the % by mole may be substituted as described above) may be similar to the method described in Heter(R) cycles, 23(7), 1649, 1985, by analogous to Scheme 1 The compound IV is prepared by reacting the compound IV with the disulfide Rl_s_s_Rl in the presence of a strong test. & The compound of the formula I (the pad of which is 〇 and R1 is _c(=〇)r8 or s)r8) A method similar to that described in DE-A-19617461, in which the compound 1 (wherein the claw is 149027.doc -159-201103430 0 and R) is Η) and the compound r8_c (= 〇) &gt;w, r8_c(= s) w, ruler 8, -N=C=0 or R8, _N=C = S (where r8 has the above meaning, ^ is G-C(7) alkyl or C|_Cl0 halane The base is prepared by reacting a good cleavage group such as a carbonyl group such as CM, Br, hydrazine, alkoxy group (e.g., alkoxy group, ethaneoxyquinone pentafluorophenoxy) in the presence of a base. Suitable bases are, for example, metal hydrides (e.g., sodium hydride, argon), metal hydroxides (e.g., sodium bismuth oxide, potassium hydroxide), alkali metal carbonates (e.g., sodium carbonate, potassium carbonate, carbonic acid planing). ), an alkali metal alkoxide (such as sodium methoxide, potassium decoxide, sodium ethoxide, potassium ethoxide, butanol slant) or an organic clock (such as n-butyl quinone, butyl butyl lithium butyl lithium and diiso) The lithium propylamine reaction is generally carried out in a suitable solvent. Suitable solvents are, for example, toluene, hydrazine-hydrazine, ketone, ethers (for example, diethyl ether, tetrahydrofuran, dioxane, i,2-dimethoxyethane). , acetonitrile, N,N-dimethylformamide or dimethyl sulfoxide. The compound of formula 1 (where m is 0 and is -s〇2r8) can be similar to the method described in de_a_1962059G by making the compound z (wherein (7) is . and ... is H) and the compound R^s〇2_w (wherein the rule 8 has one of the above meanings and w is a good leaving group such as a functional group (for example, C b BHoxy group (for example, formazan) The oxy group, the ethyl oxy group) or the pentafluorophenoxy group are prepared by reacting in the presence of the test, and the test is, for example, a gold test. Hydrides (such as sodium nitride, hydrogenated 1A), metal oxides (such as sodium hydroxide, IL oxidation clock), metal carbonates (such as carbonic acid steel, carbonic acid, carbonation), metal alkoxides For example, sodium methoxide, methanol unloading, sodium ethoxide, 6 alcohol unloading, third butanol unloading) or organic testing (such as n-butylation, 铉_τ^ 丞 lithium, first butyl lithium, t-butyl lithium, two Isopropylamine) Reaction I is carried out in a suitable solvent. Suitable solvents are examples [S] 149027.doc • 160· 201103430 such as toluene, N-methylpyrrolidine _, ethers (eg diethyl ether, tetrahydrofuran) Oxane, anthracene, 2-dimethoxyethane), acetonitrile, n,N-dimercaptocarbamide or diterpene smectite. Deuteration &amp; (wherein R1 is _CN) can be similar The method described in DE_A. 196204G7, wherein the compound: (where @ is G and Η) and the compound CN_W (which is rated as a good leaving group, such as a functional group (for example, Cb Br, I)) is present in the base The reaction is prepared by the following reaction. Suitable bases are, for example, alkali metal hydrides (such as sodium hydride, potassium hydride), alkali metal hydroxides (such as hydrogen and oxygen). Sodium 'potassium hydroxide), alkali metal carbonate (such as sodium carbonate, potassium carbonate, carbonic acid planing), alkali metal alkoxide (such as sodium methoxide, potassium methoxide, sodium ethoxide, potassium ethoxide, potassium butoxide) or organolithium a base (for example, n-butyllithium, lithium butoxide, first butyl quinone, diisopropylamine). The reaction is generally carried out in a suitable solvent. Suitable solvents are, for example, toluene, N-methyl η piroxone, Ethers (eg diethyl ether, tetrahydrogen, fus. South, dioxins, with -dimethoxyethane), acetonitrile, N,N-dimethylformamide or dimethyl sulfoxide. Wherein the paw is 0 and R1 is M) can be similar to the method described in de a i96i7282 'by combining the W (wherein r, h) with the amine NRaRbRe (wherein Ra, RbA Re are as defined above) or with the metal A salt such as sodium hydroxide, potassium hydroxide or copper acetate is reacted to prepare. A quinone of the formula I (wherein m is 0 and R1 is a group of the formula )) can be similar to the method described in WO 97/43269 by making the compound i (where @ is 〇 and in H) and dentate ( Especially hard) prepared in the presence of the test. Suitable tests are, for example, alkali metal hydrides (e.g., sodium hydride, hydrogenation), alkali metal hydroxides (e.g., sodium hydroxide, potassium hydroxide), alkali metal carbonates (e.g., 149027.doc • 161 201103430 Sodium, potassium carbonate, cesium carbonate, metal alkoxide (such as sodium decoxide, potassium decoxide, sodium ethoxide, potassium ethoxide, ketone, second butyl quinone, second or organic (four) (such as n-butyl) In a suitable solvent, two: lithium, lithium diisopropylamine). The reaction - the solvent is, for example, toluene, N-decyl pyrrolidone, ether (for example, diethyl « g- 7 ^ , coward Methane, dioxane, i, 2 · 2), acetonitrile, hydrazine, hydrazine, hydrazine, dimethyl hydrazine, etc. (where GJ · R1 is · ρ (= φιλι °) can be similar to 99 Prepared by the method described in /05149. 1 compound of formula II (wherein Ru is not hydrogen) can be converted to R by a reaction similar to compound 1 (wherein the conversion reaction causes the NRU group (wherein R), H) to react It is prepared as a compound of ruthenium. Compound Κ where m is "Ge 2" can be prepared by oxidation reaction from each compound K. Alternatively, compound W (where ^ 2) The protonation can be removed by the first earthworm, and then reacted with the sulfonium gas R^SC^Cl: the compound IV is prepared. The compound z (where 1 can be removed by first removing the scorpion scorpion, followed by Sulfate chloride or barium sulfate of the formula R^OSC^Cl (wherein R1 6 $ r K is selected from the group consisting of hydrazine, Ci_Ci. Institute base, Ci_c). Tetraalkyl, C2-C1G dilute, c2_Ci. Base, c2_Ci. alkynyl, C2_C|❹, alkynyl, C3-c1(), bad alkyl, C3_Cig_cycloalkyl, phenyl, phenyl-Ci_C4, wherein the last two of the groups mentioned The phenyl moiety can be substituted as described above and a 5- or 6-membered saturated, partially unsaturated or aromatic heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, fluorene and 8. The substitution reaction as described above is carried out from the compound IV. The right individual compound cannot be prepared via the above route, and it can be derivatized by other ES3 I49027.doc •162·201103430 compounds I and II or by the synthesis route The preparation is prepared by modification. The reaction mixture is treated in a conventional manner, for example by mixing with water, separating the phases and, if appropriate, by way of example The crude product can be purified by chromatography on alumina or tannin. Some intermediates and final products in the form of colorless or light brown viscous oil can be obtained, which do not contain volatile components or are volatilized under reduced pressure and moderately high temperature. The component is purified. If a solid and a final product are obtained, it can be purified by recrystallization or decomposition. Another aspect of the present invention relates to a compound of formula IV.

其中Ar、Het、A及Y具有上述針對化合物給出之—般 或尤其較佳含義中之一者。 化合物IV—方面為化合物1及„之製備(參見上述流程)中 的有用中間物,而另-方面亦具有顯著的殺真菌活性。 尤佳之化合物IV為式1\^.1至1¥ 48之化合物,其中R2〗、 R 、R 、R及R25之組合在各情況下對應於上述表A中之 一列且Het在各情況下具有式Het」至Het 16中之一者;及 式IV.49至IV.96之化合物,其中沿1與八]:,之組合在各情況 下對應於+述表B中之一列。 149027.doc -163· 201103430Wherein Ar, Het, A and Y have one of the above-mentioned general or especially preferred meanings given to the compound. Compound IV - aspects are useful intermediates in the preparation of compounds 1 and „ (see the above scheme), and in addition have significant fungicidal activity. Particularly preferred compound IV is formula 1 \^.1 to 1 ¥ 48 a compound, wherein the combination of R2, R, R, R and R25 corresponds in each case to one of the above Table A and Het has in each case one of the formulas Het" to Het 16; and Formula IV. Compounds of 49 to IV.96, wherein the combination of 1 and VIII]: corresponds in each case to one of the columns in Table B. 149027.doc -163· 201103430

[si 149027.doc 164 201103430[si 149027.doc 164 201103430

149027.doc -165- 201103430149027.doc -165- 201103430

[si 149027.doc -166 - 201103430[si 149027.doc -166 - 201103430

在此等化合物中,較佳為化合物IV1至IV 24及IV 49至 1.72 ’更佳為化合物IV丨至卩12及〗49至16〇,且尤佳為化 合物 IV.2 及 IV.50。 本發明進一步係關於一種農業組合物,其包含至少—種 如上所疋義之式Ϊ、11及/或以之化合物或其農業上可接受 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,包括土壤 傳播真菌,尤其來源於以下類別者:根腫菌綱 (m〇di〇Ph〇romycetes)、印菌綱(peronoSp〇r〇rnyCetes,Among these compounds, preferred compounds IV1 to IV 24 and IV 49 to 1.72 ' are preferably compounds IV to 12 and 49 to 16, and more preferably compounds IV.2 and IV.50. The invention further relates to an agricultural composition comprising at least one of the formulas, 11 and/or compounds as defined above, or an agriculturally acceptable salt thereof, and a liquid or solid carrier. 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: m〇di〇Ph〇romycetes, and sinensis (peronoSp〇r〇rnyCetes,

Oomycetse)、gg 菌綱(chytridiomycetes)、接合菌綱 (Zyg〇mycetes)、子囊菌綱(八則町⑽⑷、擔子菌綱 (Basidiomycetes)及半知菌綱(Deuter〇mycetes)(同義詞,不 完全菌綱(Fungi imperfecti))。其牛一些係全身有效的且其 可作為葉面殺真菌劑、拌種(seed dressing)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&amp;物I、Π及IV及本發明組合物在防治以下大量植物致 病真菌中尤其重要:各種栽培植物上之真菌,諸如穀類, 例如小麥、裸麥、大麥、黑小麥、燕麥或稻榖;甜菜, 149027.doc •167· 201103430 例如,㈣甜菜或㈣甜菜;水果,諸如仁果、核果或軟 果(soft fnm),例如,頻果、梨、李子、桃、杏仁、樓 桃、草莓、樹莓、黑莓或醋栗;豆科植物,諸如小扁豆、 婉豆、首靖或大豆;油料作物,諸如油菜、芬末、撖:、 向曰葵、椰子、可可豆、繁麻、油棕、落花生或大豆丨瓜 類,諸如南瓜、胡瓜或甜瓜;纖維植物,諸如棉花、亞 麻、大麻或黃麻;柑桔類水果,諸如橙子、 4 丁傢、匍匈柚 或柑;蔬菜,諸如蔽菜、萬苣、產筒、甘藍菜、胡蘿葡、 洋蔥、番站、馬鈴著、瓜類或辣椒;月桂科植物,諸如鍾 梨、肉桂或樟腦,·能量及原料植物,諸如玉米、大豆、‘由 菜、甘薦或油棕;玉米;煙草;堅果卜加啡;茶香 1 ;藤本植物(鮮食葡萄及葡萄汁葡萄藤);蛇麻子;’ 皮;天然橡膠植物或觀賞植物及林業植物諸如花:灌 木、闊葉樹或常綠樹’例如針葉樹;及植物繁殖材料上^ 真菌,諸如種子,及此等植物之作物材料。 較佳地,化合物卜„及以及其組合物分別用於防治以下 各物上的大量真菌:田間作物,諸如馬鈴薯、糖用甜菜、 煙Ί麥、一裸麥、大麥、燕麥、稻毅、玉米、棉花、大 豆油菜、丑類、向日葵、咖啡或甘嚴丨水 物;觀賞植物;或蔬菜,@ h # '' 馼 疏未4如胡瓜、番茄、豆或南瓜。 應瞭解術語「植物繁碚M斗立 表示可用於繁殖植物的所 有植物生殖性部分,諸如種 植物的所 裡于及營養性植物材料,語如 插條及塊莖(例如馬铃薯)。此包括種子、根 莖、球莖、根莖、枝、幼枯βt 貝、塊 幼枝及植物之其他部分,“㈣ I49027.doc -168- 201103430 及秧苗,其係在萌芽之後或在露出土壤之後被移植。亦可 在移植之前藉由浸潰或傾注之全部或部分處理來保護此等 秩苗。 較佳地,分別以化合物I、II及IV及其組合物處理植物繁 殖材料係用於防治以下各物上之大量真菌:榖類,諸如小 麥、裸麥、大麥及燕麥;稻穀、玉米、棉花及大豆。 術語「栽培植物」應理解為包括已藉由育種、突變誘發 或遺傳工程設計經修飾之植物,包括(但不限於)市售或開 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)、乙酸化或法呢基化(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。Oomycetse), chytridiomycetes, Zyg〇mycetes, Ascomycetes (Bazuki-cho (10) (4), Basidiomycetes and Deuter〇mycetes (synonym, incomplete bacteria) (Fungi imperfecti). Some of its cattle 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 control Harmful fungi, especially fungi that occur in the roots of wood or plants. Chemicals &amp; I, sputum and IV and compositions of the invention are particularly important in controlling a large number of phytopathogenic fungi: fungi on various cultivated plants, such as cereals, for example Wheat, rye, barley, triticale, oats or rice bran; beet, 149027.doc •167· 201103430 For example, (iv) beet or (iv) beet; fruit, such as pome fruit, stone fruit or soft fruit (soft fnm), for example, frequency Fruit, pear, plum, peach, almond, peach, strawberry, raspberry, blackberry or gooseberry; legumes such as lentils, cowpea, sage or soybean; oil crops such as canola, fennel撖:, hollyhock, coconut, cocoa, 麻麻, oil palm, groundnut or soy melon, such as pumpkin, courgette or melon; fiber plant, such as cotton, linen, hemp or jute; citrus fruit, Such as oranges, 4 Dingjia, Sui Hung pomelo or mandarin; vegetables, such as vegetables, borage, barrels, kale, carrots, onions, bananas, bells, melons or peppers; laurel plants, Such as clock pear, cinnamon or camphor, energy and raw plant, such as corn, soybean, 'yield, ginseng or oil palm; corn; tobacco; nut, bake, tea, 1; vine (salty and grape juice) Rattan; hops; 'skin; natural rubber or ornamental plants and forestry plants such as flowers: shrubs, broadleaf trees or evergreen trees' such as conifers; and plant propagation materials ^ fungi, such as seeds, and crop materials of such plants Preferably, the compounds and their compositions are used to control a large number of fungi on the following crops: field crops such as potatoes, sugar beets, buckwheat, rye, barley, swallow , rice, corn, cotton, soybean rape, ugly, sunflower, coffee or Ganshui water; ornamental plants; or vegetables, @ h # '' 馼 未 不 4 such as courgettes, tomatoes, beans or pumpkins. The term "plants" refers to all plant reproductive parts that can be used to propagate plants, such as in the plant and in vegetative plant material, such as cuttings and tubers (eg potatoes). This includes seeds, Rhizomes, bulbs, rhizomes, shoots, young βt shells, young shoots and other parts of plants, "(iv) I49027.doc -168- 201103430 and seedlings, which are transplanted after germination or after exposure of the soil. These ranks can also be protected by all or part of the treatment by dipping or pouring before transplantation. Preferably, the plant propagation material is treated with Compounds I, II, and IV, and combinations thereof, respectively, for controlling a large number of fungi on the following: mites, such as wheat, rye, barley, and oats; rice, corn, cotton And soybeans. The term "cultivated plants" is understood to include plants that have been modified by breeding, mutation induction or genetic engineering, including but not limited to commercially available or developing agricultural biotechnology products (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 are not readily obtainable by cross-breeding, mutation or natural recombination in nature. Typically, one or more genes have been integrated into the genetic material of a genetically modified plant to modify certain properties of the plant. Such genetic modifications also include, but are not limited to, proteins, for example, by glycosylation or polymer addition (such as prenylated, acetated 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、WOModified plants have been designed by breeding, mutation induction or genetic engineering. Due to conventional breeding or genetic engineering methods, for example, tolerance to the application of specific classes of herbicides, such as hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor; acetaminophen lactate (ALS) inhibitor, such as sulfonylurea (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 &gt; WO 149027.doc -169- 201103430 03/13225、WO 03/14356、WO 04/16073)或咪唑啉酮(例如 參見 US 6,222,100、WO 01/82685、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 03/143 56、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);麩醯胺酸合成酶(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US 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 „米„坐琳 酮(例如曱氧咪草煙(imazamox))具财受性。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〜些植物以 商標名 RoundupReady®(财受嘉填塞,Monsanto,s A )及97/41218 'WO 98/02526, WO 98/02527, WO 04/106529, WO 05/20673, WO 03/14357 &gt; WO 149027.doc -169-201103430 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, WO 98/02527, WO 04/106529, WO 05/20673, WO 03/ 014357, WO 03/13225, WO 03/143 56, WO 04/16073); enol acetone oxalic acid-3-phosphate synthase (EPSPS) inhibitors, such as glyphosate (see, for example, WO 92/) 00377); a glutamate synthase (GS) inhibitor such as glufosinate (see, for example, EP-A 242 236, EP-A 242 246) or an oxynil herbicide (see, for example, US) 5,559,024). Conventional breeding methods (mutation induced) have rendered several cultivated plants tolerant to herbicides, such as Clearfield® Summer Canola (Canola, BASF SE, Germany) to „米„坐琳酮 (eg, Imazamox) Financial acceptability. Genetically engineered methods have been used to make cultivated plants (such as soybeans, cotton, corn, sugar beets, and canola) tolerant to herbicides (such as jiacaosai and chlorpyrifos), some of which are under the trade name RoundupReady® , Monsanto, s A ) and

LibertyLink®(而才受固殺草,Bayer CropScience,Germany) 市售》 此外,亦包括藉由使用重組DN A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 Bacillus),特別來自蘇雲金芽孢桿菌(BaeUlus thuringiensis)之蛋白,諸如δ-内毒素,例如,CryJA(b)、LibertyLink® (commercially available from Bayer CropScience, Germany) also includes plants capable of synthesizing one or more insecticidal proteins by using recombinant DN A technology, especially from the genus Bacteroides ( Genus Bacillus), especially a protein from BaeUlus thuringiensis, such as δ-endotoxin, for example, CryJA(b),

CrylA(c)、CrylF、CryIF(a2)、CryIIA(b)、CryliiA、CrylA (c), CrylF, CryIF (a2), CryIIA (b), CryliiA,

CrylllB(bl)或Cry9c ;營養期殺昆蟲蛋白(Vlp),例如 VIP1、VIP2、VIP3或VIP3A ;定殖線蟲之細菌(例如發光CrylllB (bl) or Cry9c; vegetative insecticidal protein (Vlp), such as VIP1, VIP2, VIP3 or VIP3A; colonizing nematode bacteria (eg, luminescence)

[SJ 149027.doc -170- 201103430 \ na〇aus柳.)或嗜線蟲致病桿菌屬 咖—us spp·))之殺昆蟲蛋白;由動物產生之毒素, L蠍母素&amp;蛛,素、黃蜂毒素或其他昆蟲特異性神經 毋素’由真菌產生之毒素’諸如鏈黴菌毒素、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 如膜蛋白酶抑制劑、絲胺酸蛋白酶抑制劑、塊莖儲藏蛋白 (patatin)抑制齊卜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M麻毒素、玉蜀黍_ Rip、相思子素、絲瓜軒毒蛋白、沙泊寧(sap〇rin)或異株 腹瀉毒蛋白(bryodin);類固醇代謝酶,諸如弘羥基類固醇 氧化酶、脫皮類固醇撕-糖基轉移酶、膽固醇氧化酶、 蛻皮激素抑制劑或HMG-CoA-還原酶;離子通道阻斷劑, 諸如鈉通道或鈣通道阻斷劑;保幼激素酯酶;利尿激素受 體(異株瀉根毒蛋白受體);芪合成酶、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 質結構域之新穎级合(例如參見WO 02/015701)。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 &amp;W0 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 149027.doc 171 201103430 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(C〇le〇ptera))、兩翼昆蟲(雙翅目 altera))及蛾(鱗翅目(Lepid〇ptera)),及線蟲(線蟲綱 (Nematoda))。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Cryl Ab毒素之玉米栽培品種)、 YieldGard® Plus(產生CrylAb及Cry3BM毒素之玉米栽培品 種)、Stadink®(產生Cry9c毒素之玉米栽培品種)、[SJ 149027.doc -170-201103430 \na〇aus willow.) or the insecticidal protein of the nematophagous bacillus genus (us spp.)); the toxin produced by animals, L蝎 mother &amp; , wasp-toxin or other insect-specific neurosteroids - toxins produced by fungi such as streptomyces toxins, plant lectins such as cowpea or barley lectin; lectins; protease inhibitors such as membrane protease inhibitors, silkamine Acid protease inhibitors, patatin inhibits cis-cysteine protease inhibitors or papain inhibitors; ribosome-inactivated proteins (RIP), such as M-toxin, maize R Rip, acacia, Loofah venom protein, sap〇rin or diarrhea venom protein (bryodin); steroid metabolism enzymes, such as hydroxy steroid oxidase, dermal steroid tear-glycosyltransferase, cholesterol oxidase, ecdysone inhibition Agent or HMG-CoA-reductase; ion channel blocker, such as sodium channel or calcium channel blocker; juvenile hormone esterase; diuretic hormone receptor (heterologous genus protein receptor); Biphenyl Group synthase, chitinase (pumila chitinase and) or a glucanase. In the context of the present invention, it is also expressly understood that such insecticidal proteins or toxins are understood to be protoxins, hybrid proteins, truncated or otherwise modified proteins. Hybrid proteins are characterized by novel cascades of protein domains (see, for example, WO 02/015701). 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, Methods for producing such genetically modified plants in WO 03/18810 &amp; WO 03/52073 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 which produce such proteins 149027.doc 171 201103430 to tolerate harmful pests from all: arthropod taxa, especially beetles (Coleoptera (C〇le〇) Ptera)), two-winged insects (Diptera altera) and moths (Lepid〇ptera), and nematodes (Nematoda). Genetically modified plant lines capable of synthesizing one or more insecticidal proteins are described, for example, in the above publication, and some of them are commercially available: such as YieldGard® (a corn cultivar producing Cryl Ab toxin), YieldGard® Plus (creating CrylAb) And Cry3BM toxin corn cultivar), Stadink® (Cry9c toxin-producing corn cultivar),

Herculex® RW(產生 Cry34Abl、Cry35Abl 及酶膦萬麻鹼 _N_ 乙醯基轉移酶[PAT]之玉米栽培品種);NuC〇TN® 33B(產 生Cry 1 Ac毋素之棉栽培品種)、B〇ligard® 1(產生cryiAc 毒素之棉花栽培品種)、Bollgard® II(產生CrylAc及 Cry2Ab2毒素之棉花栽培品種);viPCOT®(產生VIP-毒素 之棉彳匕栽培品種);NewLeaf®(產生Cry3A毒素之馬鈐著栽 培品種);Bt-Xtra®、NatureGard®、KnockOut®、 BiteGard®、Protecta®、自 Syngenta Seeds SAS,France購得 之Btll(例如,Agrisure⑧CB)及Btl76(產生CrylAb毒素及 PATS# 之玉米栽培品種)、自 Syngenta Seeds SAS,France靖 得之MIR604(產生經修飾形式之Cry3A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購得之IPC 531(產 生經修飾形式之CrylAc毒素的棉花栽培品種)及自Pi〇neer Overseas Corporation,Belgium購得之 1507(產生 CrylF毒素 149027.doc -172- 201103430 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—或多 種增加彼等植物對細菌、病毒或真菌病原體之抗性或=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(path〇genesis-reiated protein)」(PR蛋白,例如參見 EP-A 392 225)、植物抗病基因(例如,馬鈴薯栽培品種, 其表現用以對抗源自墨西哥野生馬鈴薯二倍體品種 (Solanum bulbocastanum)之馬鈴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(Erwinia amylv〇ra)之細菌抗性增 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、毅粒產量、殿粉含量、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,D〇wHerculex® RW (Corn cultivar producing Cry34Abl, Cry35Abl and phosphatidylcholine _N_acetyltransferase [PAT]); NuC〇TN® 33B (Cry 1 Acetate cotton cultivar), B〇 Ligard® 1 (cotton cultivar producing cryiAc toxin), Bollgard® II (cotton cultivar producing CrylAc and Cry2Ab2 toxin); viPCOT® (cotton cultivar producing VIP-toxin); NewLeaf® (producing Cry3A toxin) Horses cultivar); Bt-Xtra®, NatureGard®, KnockOut®, BiteGard®, Protecta®, Btll available from Syngenta Seeds SAS, France (eg Agrisure 8CB) and Btl76 (corn producing CrylAb toxin and PATS#) Cultivars), from Syngenta Seeds SAS, France's MIR604 (a maize cultivar producing a modified form of Cry3A toxin' reference WO 03/018810), MON 863 purchased from Monsanto Europe SA, Belgium (to produce a Cry3Bbl toxin) Corn cultivar), IPC 531 (a cotton cultivar producing a modified form of CrylAc toxin) purchased from Monsanto Europe SA, Belgium, and from Pi〇neer Overseas Corporation, Be LG purchased 1507 (produced CrylF toxin 149027.doc -172- 201103430 and corn cultivar of PAT enzyme). Also included are plants which can be synthesized by using recombinant DNA techniques - or a plurality of proteins which increase the resistance or resistance of their plants to bacterial, viral or fungal pathogens. Examples of such proteins are the so-called "path 〇 genesis-reiated proteins" (PR proteins, see for example EP-A 392 225), plant disease resistance genes (for example, potato cultivars, which are used for Against a resistance gene derived from the potato Phytophthora in the wild potato diploid species (Solanum bulbocastanum) or T4-lysozyme (for example, a potato cultivar capable of synthesizing such proteins, such as against pear fire damage (Erwinia amylv) 〇ra) increased bacterial resistance). 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, powder 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 including varying amounts of inclusions or novel inclusions by using recombinant DNA technology, for example, produce long-chain ω_3 fatty acids or unsaturated ω which promote health. -9 fatty acid oil crops (eg, Nexera® canola, D〇w

Agro Sciences,Canada) 〇 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 149027.doc -173- 201103430 物,例如,產生增加量之支鏈澱粉的馬鈴薯(例如, Amflora®馬鈴薯,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: 白銹病菌屬(Albugo spp.)(白銹病):於觀賞植物、蔬菜 (例如’油菜白錄病菌(A. Candida))及向曰婆(例如,婆羅 門白錢病菌(A. tragopogonis))上;交鏈孢菌屬(Aiternaria spp.)(黑斑病(Alternaria leaf spot)):於蔬菜、油菜(芸苔交 鍵孢菌(A. brassicola或brassicae))、糖用甜菜(細交鏈抱菌 (A. tenuis))、水果、稻榖、大豆、馬鈴薯(例如,馬鈴薯交 鏈孢菌(A. soUni)或互格交鏈孢菌(A. altemata))、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 菜及蔬菜上之根腐病菌屬(Aphan〇myces spp.);榖類及蔬 菜上之輪紋病菌屬(Asc〇chyta spp ),例如小麥上之小麥 輪紋病菌(A. tritici)(炭疽病)及大麥上之大麥輪紋病菌(a hordei) ’平臍蠕孢屬(Bip〇iaris spp )及内臍蠕孢屬 (Drechslera spp.)(有性態:旋孢腔菌屬(cochHobolus spp.)),例如,玉米上之南方葉枯病(玉蜀黍長蠕孢(d. maydis))或北方葉枯病(玉米生平臍蠕孢⑺找^〇丨^),例 如,縠類上之斑點病(小麥根腐平臍蠕孢(B· s〇r〇kiniana)) 及例如稻穀及草皮上之稻平臍類(B me);縠類上(例 士】夕或大麥上)之白粉病菌(B】umeria graminis)(先前稱 為Erysiphe graminis)(白粉病);水果及聚果(例如,草 莓)、蔬菜(例如,萵苣、胡蘿S、芽菜及甘藍菜)、油菜、 [S] 149027.doc -174- 201103430 藤本植物林業植物及小麥上之灰葡萄抱(B〇trytis cinerea)(有性悲:灰黴病菌(B〇try〇tinia fuckeiiana):灰 黴),萵苣上之高苣露菌病(Bremia lactucae)(霜黴病),·闊 葉知ί及吊',亲柄上之長嗓殼屬(cerat0Cystis spp·)(同義詞長 喙黴屬(Ophiostoma spp·))(腐爛或枯萎),例如榆樹上之榆 長喙殼菌(C. uhni)(荷蘭榆樹病);葉斑病菌屬(Cerc〇sp〇ra spp.)(葉斑病):於玉米(例如,灰色葉斑病:玉米灰斑病菌 (C. zeae-maydis))、稻榖、糖用甜菜(例如,甜菜褐斑病菌 (C. beticola))、甘蔗、蔬菜、咖啡、大豆(例如,大豆灰斑 病菌(C_ sojina)或大豆紫斑病菌(c kikuchH))及稻縠上;黑 變病菌屬(Clad〇Sporium spp·):於番茄(例如,葉黑變病菌 (C. fulvum).葉黴病)及縠類上,例如小麥上之麥類黑變病 菌(C. herbarum)(黑穗病);穀類上之黑麥角菌(Claviceps pUrpUrea)(麥角症);旋孢腔菌屬(c〇cMi〇b〇lus spp )(無性 態:平臍蠕孢屬之長蠕孢(Helminthosp〇rium))(葉斑病): 於玉米(玉米旋孢腔菌(C. carbonum))、縠類(例如,禾旋孢 腔菌(C. Sativus),無性態:麥根腐平臍蠕孢菌(b sorokiniana))及稻穀(例如,宮部旋孢腔菌(c miyabeanus),無性態:水稻長蠕孢菌(H沉%“))上;刺 盤抱屬(Colletotrichum SPP.)(有性態:炭疽病菌屬 (Glomerella spp.))(炭疽病):於棉花(例如,棉刺盤孢(c g〇SSypii))、玉米(例如,禾刺盤孢(c. graminic〇la):炭疽 莖腐病)' 軟果、馬鈐薯(例如’果腐刺盤孢(c. coccodes):黑斑病)、豆(例如,菜豆刺盤孢(c. 149027.doc -175 - 201103430 Π —驗nUm))及大豆(例如,平頭刺盤孢(c加臟她) 或膠?〇炭症病菌(C. gi〇e〇sp〇ri〇ides))上;伏革菌屬 (Conic— spp.),例如,稻穀上之紋枯病菌(cϋϋ)(紋 枯病);大豆及觀賞植物上之山扁豆生棒孢菌(c〇rynesp〇ra cassiicola)(葉斑病);環錐孢菌屬(CyCl〇Conium spp.),例 如,油撖欖樹上之油橄欖環錐孢菌(c 〇leaginum);柱孢菌 屬(Cylindr〇carpon spp.)(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(Nectria spp.)或新叢赤设菌屬(Ne〇nectria spp.)):於果樹、藤本植 物(例如,鵝莩楸柱孢菌(c liriodendri),有性態:鵝掌楸 新叢赤叙菌(Neonectria liriodendri):黑腳病)及觀賞植物 上,大豆上之褐束絲菌(Dematophoranecatrix)(有性態:褐 堅座殼菌(Rosellinia neeatrix))(根腐病及莖腐病);間座殼 鹵屬(Diaporthe spp.),例如,大豆上之菜豆間座殼菌(d. phase〇l〇rum)(猝倒病);内臍蠕孢屬(同義詞長蠕孢屬,有 性態:核腔菌(Pyrenophora)):於玉米、穀類,諸如大麥 (例如,圓内臍蠕孢菌(D. teres),網斑病)及小麥(例如,黃 斑小麥内臍螺抱菌(D. tritici-repentis,褐斑病))、稻穀及 草皮上;藤本植物上之Esca(頂枯病,乾枯病),由斑點孔 菌(Formitiporia punctata,Phellinus punctata)、地中海孔 菌(F. mediterranea)、垣孢伐莫尼亞菌(Phaeomoniella chlamydospora)(早期之厚垣褐枝頂孢(Phaeoacremonium chlamydosporum))、寄生瓶黴菌(Phaeoacremonium aleophilum)及/或圓頭葡萄座腔菌(Botryosphaeria obtusa)Agro Sciences, Canada) 〇 In addition to 'specifically improving the production of raw materials' also includes plants containing varying amounts of inclusions or novel inclusions by using recombinant DNA techniques, for example, 149027.doc-173-201103430 An increased amount of amylopectin potato (eg, Amflora® potato, BASF SE, Germany). Compounds I, II and IV and their compositions are especially suitable for controlling the following plant diseases: Albugo spp. (white rust): in ornamental plants, vegetables (eg 'A. Candida') And to the aunt (for example, A. tragopogonis); Aiternaria spp. (Alternaria leaf spot): in vegetables, rape (salty moss) A. brassicola or brassicae), sugar beet (A. tenuis), fruit, rice bran, soybean, potato (for example, A. souni or A. souni) A. altemata, tomato (for example, Alternaria alternata or Alternaria alternata) and wheat; sugar beet and vegetable root rot (Aphan〇myces spp. ); Asc〇chyta spp on moss and vegetables, such as A. tritici (anthrax) on wheat and barley ring disease (a hordei) on barley Bip〇iaris spp and Drechslera spp. (sexual state: genus genus (c) ochHobolus spp.)), for example, southern leaf blight on corn (d. maydis) or northern leaf blight (corn worm (7) found ^^^), for example, on moss Spot disease (B. s〇r〇kiniana) and, for example, rice umbilical (B me) on rice and turf; on the scorpion (used on the evening or on barley) Powdery mildew (B) umeria graminis (formerly known as Erysiphe graminis) (powder disease); fruits and fruit (eg, strawberries), vegetables (eg, lettuce, carrots, sprouts and kale), canola, [ S] 149027.doc -174- 201103430 vine planting plants and wheat vines (B〇trytis cinerea) (sexual sorrow: B〇try〇tinia fuckeiiana: gray mold), lettuce Bremia lactucae (downy mildew), broadleaf and sling, cerat0Cystis spp. (synonym Ophiostoma spp.) Rotting or withering), such as C. uhni (Netherlands eucalyptus) on the eucalyptus; Cerc〇sp〇ra spp. Spot disease): in corn (for example, gray leaf spot: C. zeae-maydis), rice bran, sugar beet (for example, C. beticola), sugar cane, vegetables , coffee, soybean (for example, C_ sojina or C kikuchH) and rice blast; Clad 〇Sporium spp.: in tomato (for example, Phytophthora (C. fulvum). Foliar) and mites, such as C. herbarum (smut) on wheat; Claviceps pUrpUrea on cereals (ergots) ); genus genus (c〇cMi〇b〇lus spp) (all-sex: Helminthosp〇rium) (leaf leaf spot): in corn (corn corn snail cavity) C. carbonum), terpenoids (eg, C. sativus, asexuality: b sorokiniana) and rice (eg, uterine spore cavity) Cmiyabeanus, asexual state: Helminthosporium ssp. (H. %)); Colletotrichum SPP. (Polymorphism: Anthracnose (Glomerella) Spp.)) (anthrax): in cotton (for example, cg〇SSypii), corn (for example, c. graminic〇la: anthrax stem rot), soft fruit, Horse yam (eg 'c. coccodes: black spot disease'), beans (eg, Bean thorn spores (c. 149027.doc -175 - 201103430 Π - test nUm)) and soybeans (eg , flat head thorn spore (c plus dirty her) or glue? On C. gi〇e〇sp〇ri〇ides); Cono-spp., for example, Rhizoctonia solani (cϋϋ) on rice paddy; Sheath blight; Soybean And ornamental plants on the genus C. rynesp〇ra cassiicola (leaf leaf spot); Cyclabium conium spp., for example, the Phytophthora indicum on the eucalyptus c 〇leaginum); Cylindr 〇carpon spp. (eg, fruit squamous cell carcinoma or vine decline) 'sexual state: Nectria spp. or new plexus Ne〇nectria spp.): in fruit trees, vines (for example, c liriodendri, having a sexual state: Neonectria liriodendri: blackfoot disease) On ornamental plants, Dematophoranecatrix (sexual state: Rosallian neeatrix) (root rot and stem rot); Diaporthe spp. For example, d. phase〇l〇rum (dumping disease) on soybean; Helminthosporium (synonym Having a sexual state: Pyrenophora: in corn, cereals, such as barley (for example, D. teres, net spot disease) and wheat (for example, umbilical cord blood snail) (D. tritici-repentis, brown spot), rice and turf; Esca (top blight, dry blight) on vines, by Listpipora punctata (Phellinus punctata), Mediterranean bacterium (F. Mediterranea), Phaeomoniella chlamydospora (early Phaeoacremonium chlamydosporum), Phaeoacremonium aleophilum and/or Botryosphaeria obtusa

[SI 149027.doc -176· 201103430 所引起,癖囊腔菌屬(Elsinoe spp.):於仁果(梨癌囊腔菌 (E. pyri))、軟果(懸鈴木痂囊腔菌(E veneta).:炭疽病)及 藤本植物(葡萄痂囊腔菌(Ε· ampelina):炭疽病)上;稻穀 上之稻葉黑腫病菌(Entyloma oryzae)(葉黑穗病);小麥上 黑附球菌屬(Epicoccum spp.)(黑黴病);白粉病菌屬 (Erysiphe spp.)(白粉病):於糖用甜菜(甜菜白粉病菌(E betae))、蔬菜(例如,豌豆白粉病菌(E. pisi))、諸如瓜類 (例如’ 一孢白粉病菌(E· cichoracearum))、甘藍菜、油菜 (例如’十子^匕白粉病菌(E. cruciferarum))上;於果樹、藤 本植物及觀員植物樹木上之多,彎孢殼菌(Eutypa iata)(葡萄 癌腫病或頂枯病,無性態:多殼囊孢菌(Cyt〇sp〇rina Uu) (同義5司百肋匕盤針抱菌(Libertella blepharis)));於玉米 (例如’大斑突臍蠕孢菌(E turcicum))上之突臍孢菌屬 (Exserohilum spp. ’同義詞長蠕孢屬);各種植物上之鐮孢 菌屬(Fusarium spp.)(有性態:赤黴菌屬(Gibberella spp.))[SI 149027.doc -176· 201103430 caused by the genus Elsinoe spp.: in the fruit of the fruit (E. pyri), soft fruit (P. sylvestris (E veneta) ): anthracnose) and vines (Ε·ampelina: anthracnose); Entyloma oryzae (leaf smut) on rice; (Epicoccum spp.); Erysiphe spp. (powder disease): in sugar beet (E. beetiae), vegetables (eg, pea powdery mildew (E. pisi) ), such as melons (such as 'E. cichoracearum), cabbage, rapeseed (such as 'E. cruciferarum'); in fruit trees, vines and plant trees There are many, Eutypa iata (Cell cancer or top blight, asexuality: Cyt〇sp〇rina Uu) (synonymous 5 Division 百 匕 匕 匕 抱 ( Libertella blepharis))); Exaserohilum spp. 'synonymous on maize (eg 'E turcicum') Helminthosporium); various kinds of Fusarium on plants (Fusarium spp) (sexual stage: the genus Fusarium (Gibberella spp))

(&gt;周萎病、根腐病或莖腐病),諸如榖類(例如小麥或大麥) 上之禾秋鐮抱菌(F graminearum)或黃色鐮抱菌(F CUlm〇rUm)(根腐病、瘡痂病或赤黴病(head blight))、番茄 上之錘形鐮孢菌(F· oxysporum)、大豆上之茄鐮孢菌(F_ S〇lani)及玉米上之輪枝鐮孢菌(F. verticillioides);榖類(例 士 ]麥或大麥)及玉米上之禾頂囊殼菌(Gaeumann〇myCes graminis)(全蝕病);赤黴菌屬(GibbereUa spp.):於榖類(例 如玉米根腐赤黴菌(G. zeae))及稻榖(例如藤倉赤黴菌(G. fujikuroi) ’惡苗病)上;藤本植物仁果及其他植物上之 149027.doc -177- 201103430 炭疽病菌(Glomerella cingulata)及棉花上之棉炭疽病菌(g. gossypii);稻穀上之格蘭染色複合物(Grainstaining complex),藤本植物上之葡祠球座菌(Guignardia bidwellii)(黑腐病);薔薇科植物及刺柏上之膠鏽菌屬 (Gymnosporangium spp.),例如梨上之薩賓膠鏽菌(G sabinae)(銹病);玉米、榖類及稻榖上之長螺孢屬(同義詞 内臍蠕孢,有性態:旋孢腔菌);鏽菌屬(Hemileia spp.), 例如咖啡上之聪孢鏽菌(Hemileia vastatrix)(咖啡葉錄病); 藤本植物上之葡萄褐斑病菌(Isariopsis clavispora)(同義詞 葡萄黑變病菌(Cladosporium vitis));大豆及棉花上之菜豆 殼球孢菌(Macrophomina phaseolina,Macrophomina phaseoli)(根腐病及莖腐病);榖類(例如小麥或大麥)上之 雪腐微結節菌(Microdochium nivale)(同義詞雪腐鐮抱菌 (Fusarium nivale))(雪黴病);大豆上之黃華彼散又絲殼 (Microsphaera diffusa)(白粉病);褐腐病菌屬(Monilinia(&gt;Peripheral rot, root rot or stem rot), such as F graminearum or F CUlm〇rUm on roots (such as wheat or barley) (root rot) Disease, scab or head blight), F. oxysporum on tomato, Fusarium oxysporum on soybean, and Fusarium oxysporum on corn (F. verticillioides); apes (salmon) wheat or barley) and Gaeumann〇myCes graminis on corn (total eclipse); Gibbere Ua spp.: in mites ( For example, G. zeae (G. zeae) and rice blast (such as G. fujikuroi 'mycosis); vines and other plants 149027.doc -177- 201103430 anthracnose (Glomerella cingulata) and cotton anthracnose (g. gossypii); Granstaining complex on rice, Guignardia bidwellii (black rot) on vine; Genus plants and the genus Gymnosporangium spp., such as Sabine rust on pears (G sab Inae) (rust); Helminthosporium on corn, alfalfa and rice blast (synonym umbilical umbilical cord, sexual state: Helminthosporium); Helicobacter spp. Hemileia vastatrix (coffee leaf disease); Isariopsis clavispora on the vine (synonym Cladosporium vitis); Soybean and cotton on the genus Macrophomina Phaseolina, Macrophomina phaseoli); Microdochium nivale (synonymous with Fusarium nivale) on moss (eg wheat or barley) (snow mold) ); on the soybean, Huanghua and silk shell (Microsphaera diffusa) (powder disease); brown rot fungus (Monilinia)

spp.) ’例如,核果及其他薔薇科植物上之核果褐腐病菌 (M. laxa)、美澳型核果褐腐病菌(m. fructicola)及仁果褐腐 病菌(M. fructigena)(花腐病及枝枯病(bl〇〇m and twig blight)、褐腐病);穀類、香蕉、軟果及落花生上之球腔菌 屬(Mycosphaerella spp.) ’諸如小麥上之禾球腔菌(M graminicola)(無性態.小麥殼針孢菌(sept〇ria tritici),殼 針孢菌斑病(Septoria blotch)),或香蕉上之斐濟球腔菌(μ. fijiensis)(黑香蕉葉斑病);霜黴菌屬(per〇n〇Sp〇ra Spp )(霜 黴病).於甘藍菜(例如芸苔霜徽病(p. brassicae))、油菜(例Spp.) 'For example, M. laxa on the fruit and other Rosaceae plants, m. fructicola and M. fructigena (flower rot) Disease and blight (bl〇〇m and twig blight), brown rot); cereals, bananas, soft fruits and groundnuts (Mycosphaerella spp.) 'such as wheat on the bacterium (M. Graminicola) (sexless state. Sept〇ria tritici, Septoria blotch), or Filipino bacterium (μ. fijiensis) on banana (black banana leaf spot) ); downy mildew (per〇n〇Sp〇ra Spp) (downy mildew). in cabbage (such as mossy rose disease (p. brassicae), rapeseed (example)

[SI 149027.doc -178- 201103430 如寄生霜黴菌(p_ parasitica))、洋蔥(例如毁壞霜黴菌(p. destructor))、煙草(煙草霜黴菌(p仏以以⑽》及大豆(例如 大豆霜黴菌(P. manshurica))上;大豆上之豆薯層鏽菌 (Phakopsora pachyrhizi)及山馬蝗層鏽菌(p meibomiae)(大 豆銹病)’瓶黴菌屬(Phialophora spp.):例如於藤本植物 (例如管胞瓶黴菌(P. tracheiphila)及四孢瓶黴菌(p tetraspora))及大豆(例如大豆莖瓶黴菌(p gregata):莖腐 病)上;油菜及甘藍菜上之黑脛莖點黴菌(ph〇ma lingam)(根腐病及莖腐病),及糖用甜菜上之甜菜莖點黴菌 (P. betae)(根腐病、葉斑病及立枯病);擬莖點黴菌屬 (Phomopsis spp.):於向日葵、藤本植物(例如葡萄生擬莖 點黴菌(P_ viticola):葉斑病(can and leaf spot))及大豆(例 如莖腐病.菜豆擬莖點黴菌(P. phase〇li),有性態:菜豆 間座殼菌(Diaporthe phaseolorum))上;玉米上之玉米節壺 菌(Physoderma maydis)(褐斑病);以下各種植物上之疫黴 菌屬(Phytophthora 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. capsici))、大豆(例如 大豆疫黴菌(P. megasperma,P. sojae))、馬鈐薯及番茄(例 如致病疫黴菌(P. infestans):晚疫病)及闊葉樹(例如多枝 疫黴菌(P. ramorum):橡樹突死);甘藍菜、油菜、蘿蔔及 其他植物上之芸苔根腫菌(plasm〇di〇phora brassicae)(根腫 病);單軸徽菌屬(Plasmopara spp.),例如藤本植物上之葡 萄生單軸黴菌(P. viticola)(葡萄藤霜黴病),及向日葵上之 霍爾斯單軸黴菌(p. halstedii);薔薇科植物、蛇麻子、仁 •179· 149027.doc 201103430 果及軟果上之叉絲單囊殼菌屬(p〇d〇sphaera -)(白粉 病)’例如頻果上之白又絲單囊殼菌(p leuc〇tricha);多黏 菌屬(Polymyxa SPP.),例如在穀類(諸如大麥及小麥)(禾多 黏菌〇&gt;· graminis))及糖用甜菜(甜菜多黏菌(p 上, 及由此傳播之病毒疾病;榖類(例如小麥或大麥)上之蔓毛 殼假尾孢(pseud〇cercosporeUa herp〇trich〇ides)(輪紋病, 有性態:Tapesia yaUundae);各種植物上之假霜黴菌 (PSeUd〇peronospora)(霜黴病),例如瓜類上之南瓜假霜黴 菌(P. cubensis)或蛇麻子上之葎草假霜黴菌(p. humiH);藤 本植物上之葡萄角斑葉焦病菌(Pseud〇pezicuia tracheiphilaK 紅火病(red fire disease)或 r〇tbrenner,,無性 態:瓶黴菌(Phialophora));各種植物上之柄鏽菌屬 (Puccinia spp.)(銹病),例如穀類(例如小麥、大麥或黑麥) 上之小麥柄鏽菌(P. triticina)(褐銹病或葉銹病)、條形柄鏽 菌(P. striiformis)(條銹病或黃銹病)、麥芽柄鏽菌(p hordei)(矮銹病(dwarf rust))、禾柄鏽菌(p graminis)(莖銹 病或黑銹病)或隱匿柄鏽菌(P. recondita)(褐銹病或葉錄 病)’及產筍上之柄鏽菌屬(例如蘆筍柄鏽菌(P. asparagi));小麥上之黃斑小麥核腔菌(Pyren〇ph〇ra tritiCirepentis)(無性態:黃斑小麥内臍蠕孢菌(Drechslera triticirepentis))(褐斑病)或大麥上之圓核腔菌(P teres)(網 斑病);梨孢菌屬(Pyricularia spp.),例如稻穀上之水稻梨 孢菌(P. oryzae)(有性態:稻盘菌(Magnaporthe grisea),稻 癌病)及草皮及穀類上之灰梨孢菌(P. grisea);草皮、稻 149027.doc -180· 201103430 縠、玉米、小麥、棉花、油菜、向日葵、大豆、糖用甜 菜、蔬菜及各種其他植物上之腐徽菌屬(Pythium spp.)(立 枯病)(例如終末腐黴菌(P. ultimum)或瓜果腐黴菌(P. aphanidermatum)),柱隔孢菌屬(Ramuiaria spp·),例如大 麥上之克樂希柱隔孢菌(R. collocygni)(柱隔孢菌葉斑病, 生理性葉斑病)及糖用甜菜上之甜菜枉隔孢菌(R beticola);棉花、稻縠、馬鈴薯、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 (Rhizoctonia spp_) ’例如大豆上之茄絲核菌(R. s〇iani)(根 腐病及莖腐病)、稻榖上之茄絲核菌(紋枯病)或小麥或大麥 上之禾毀絲核菌(R. cerealis)(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(Rhizopus stolonifer)(黑黴病、軟腐病);大麥、 黑麥及黑小麥上之黑麥嗓孢菌(Rhynchosporium secalis)(褐 斑病)’相穀上之稻帚梗柱孢菌(Sarocladium oryzae)及長 管帚梗柱孢菌(S. attenuatum)(鞘腐病);核盤菌屬 (Sclerotinia spp.)(莖腐病或白黴病):於蔬菜及田間作物, 诸如油菜、向日凑(例如菌核核盤菌(S. sclerotiorum))及大 豆(例如齊整核盤菌(s r〇lfsii)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(s glycines)(褐斑病)、小麥上之小麥殼針孢菌(8 uhici)(殼針 孢菌斑病)及毀類上之穎枯殼針抱菌(S. n〇d〇rum)(同義詞穎 枯殼多孢菌(Stagonospora nodorum))(殼多抱菌斑病);藤 本植物上之葡萄鉤絲殼菌(Uncinula necator)(同義詞葡萄白 149027.doc -181 - 201103430 粉病菌(Erysiphe necator))(白粉病,無性態:托氏粉孢菌 (Oidium tuckeri));刺球腔菌屬(Setospaeria spp·)(葉枯 病)·於玉米(例如大斑刺球腔菌(S· turcicum),同義詞大斑 長螺孢菌(Helminthosporium turcicum))及草皮上;黑穗病 菌屬(Sphacelotheca spp.)(黑穗病):於玉米(例如玉米絲黑 穗病菌(S. reiliana):絲黑穗病(head smut))、高粱及甘荒 上’瓜類上之蒼耳單絲殼菌(Sphaerotheca fuliginea)(白粉 病)’馬铃薯上之馬鈴薯粉病菌(Sp〇ng〇spora subterranea)(白痂病)及由此傳播之病毒疾病;穀類上之殼 多抱菌屬,例如小麥上之穎枯殼多孢菌(S. nod〇rurn)(;殼多 抱菌斑病,有性態:穎枯小球腔菌(Lept〇sphaeria nodorum)[同義詞穎枯殼針孢菌(phae〇sphaeria nodorum)]);馬鈐薯上之内生集壺菌(Synchytrium end〇bi〇ticum)(馬鈴薯癌腫病);外囊菌屬(Taphrina spp ), 例如桃上之畸形外囊菌(T. def0rmans)(縮葉病)及李子上之 李外囊菌(T. pruni)(李囊果病);煙草、仁果、蔬菜、大豆 及棉花上之根串珠徽菌屬(Thielaviopsis spp_)(黑根腐病), 例如煙草根串珠黴菌(T. basicola)(同義詞優雅橫節黴菌 (Chalara elegans));縠類上之腥黑穗病菌屬(TiUetia SPP_)( *見之黑穗病或腥黑穗病(stinking smut)),諸如小麥 上之小麥腿黑穗病菌(T. tritici)(同義詞網腥黑穗病菌(τ. caries),小麥黑穗病)及錄腫黑穗病菌(τ controversa)(矮 黑穗病);大麥或小麥上之紅核瑚菌(Typhula incarnata)(灰 雪Μ病)’條黑穗病菌屬(Urocystis spp.),例如黑麥上之專 [ 149027.doc •182- 201103430 麥桿黑稳病菌(u. occulta)(莖黑穗病);蔬菜上之單孢鏽菌 屬(Uromyces spp.)(銹病),諸如於豆(例如疣頂單孢鏽菌 (u. appendiculatus),同義詞菜豆單孢鏽菌(u phase〇H))及 糖用甜菜(例如甜菜單孢鏽菌(u betae))上;黑穗病菌屬 (Ustilago spp.)(散黑穗病(i〇〇se smut》:於榖類(例如裸黑 穗病菌(U. nuda)及燕麥黑穗病菌(u avaenae))、玉米(例如 玉蜀黍黑穗病菌(U. maydis) _·玉米黑穗病菌)及甘蔗上; 黑星菌屬(Venturia spp.)(瘡痂病):於蘋果(例如蘋果黑星 菌(V· inaeqUaiis))及梨上;及各種植物(諸如水果及觀賞植 物、藤本植物、軟果、蔬菜及田間作物)上之半身萎凋病 菌屬(Verticillium spp〇(凋萎病),例如草莓、油菜、馬鈐 薯及番茄上之大理菊萎凋病菌(v dahliae)。 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」應理解為表示保護以下技術及非生物材料來對抗有害 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(Ophiostoma spp.)、青變真菌屬(Ceratocystis spp.)、 出芽短梗黴(Aureobasidium pullulans)、擬莖點黴屬 (Sclerophoma spp.)、毛殼菌屬(Chaetomium spp.)、腐瘦菌 屬(Humicola spp.)、彼得殼屬(Petriella spp·)、毛束徽屬 (Trichurus spp.);擔子菌綱,諸如粉孢革菌屬(Coniophora 149027.doc •183- 201103430 spp.)、革蓋菌屬(Coriolus spp.)、褐褶菌屬(Gl〇e〇phyllum spp.) ' 香疏屬(Lentinus spp.)、側耳屬(pieur〇tus spp.)、茯 苓屬(Poria spp.)、蟠龍介屬(Serpula spp.)及乾酪菌屬 (Tyromyces spp.);半知菌綱’諸如麴菌屬(Aspergillus SPP.)、黑變病菌屬、青Μ菌屬(Penicillium spp.)、木黴菌 屬(Trichoderma spp.)、交鏈孢菌屬、擬青黴屬 (Paecilomyces spp.)及接合菌綱,諸如毛黴菌屬(Muc〇r 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(Candida spp.)及釀酒酵母菌 (Saccharomyces cerevisae) 〇 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」)]、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性。以上鑑別出之植物健 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[SI 149027.doc -178- 201103430 such as parasitic downy mildew (p_parasitica), onions (such as p. destructor), tobacco (tobacco downy mildew (p仏 to (10)" and soy (such as soy cream) P. manshurica; Phakopsora pachyrhizi and p meibomiae (soybean rust) 'Phialophora spp.: for example, vines (eg, P. tracheiphila and p tetraspora) and soybeans (eg, p gregata: stem rot); black stalks on rapeseed and kale Mold (ph〇ma lingam) (root rot and stem rot), and P. betae (root rot, leaf spot and blight) on sugar beet; Phomopsis spp.: in sunflowers, vines (eg P_ viticola: can and leaf spot) and soybeans (eg stem rot. Phytophthora sojae (P) Phase〇li), sexual state: Diaporthe phaseolorum; jade on corn Physoderma maydis (brown spot disease); Phytophthora spp. (wild 'root' leaf, fruit and stem rot) on various plants: such as peppers and melons (eg peppers) P. capsici), soybean (eg P. megasperma (P. sojae)), horse yam and tomato (eg P. infestans: late blight) and broadleaf trees (eg P. ramorum: oak tree death; plasm〇di〇phora brassicae (root swollen disease) on cabbage, rapeseed, radish and other plants; (Plasmopara spp.), for example, P. viticola (vine vine downy mildew) on vines, and p. halstedii on sunflower; Rosaceae, snake麻子,仁•179· 149027.doc 201103430 The fruit and soft fruit on the genus Pseudomonas (p〇d〇sphaera -) (powder disease), such as the white fruit of the genus Pseudomonas sinensis (p Leuc〇tricha); Polymyxa SPP., for example in cereals (such as barley and wheat) 〇 〇 · gram gram gram ( 及 及 及 及 及 及 及 ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ps ps ps ps ps ps ps ps ps ps 〇trich〇ides) (rotary disease, sexuality: Tapesia yaUundae); Pseudomonas spp. (Pythromycin) on various plants, such as P. cubensis on melons Or P. humiH on hops; Pseud〇pezicuia tracheiphilaK red fire disease or r〇tbrenner, asexual: bottle mold (Phialophora)); Puccinia spp. (rust) on various plants, such as P. triticina (brown rust or leaf rust) on cereals (eg wheat, barley or rye) ), P. striiformis (strip rust or yellow rust), P hordei (dwarf rust), p graminis (stem rust or Black rust) or P. recondita (brown rust or leaf recorded disease) and on bamboo shoots Puccinia genus (such as P. asparagi); Pyren〇ph〇ra triti Cirepentis on wheat (disorder: Drechslera triticirepentis) (Brown spot) or Pteres on barley (net spot disease); Pyricularia spp., such as P. oryzae on rice (sexual state) : Magnaporthe grisea, rice cancer) and P. grisea on turf and cereals; turf, rice 149027.doc -180· 201103430 縠, corn, wheat, cotton, rape, sunflower Pythium spp. (Pythium blight) (such as P. ultimum or P. aphanidermatum) on soybeans, sugar beets, vegetables, and various other plants. Ramuiaria spp., such as R. collocygni on barley (Saccharomyces cerevisiae leaf spot, physiological leaf spot) and sugar beet on sugar beet R beticola; cotton, rice bran, potato, turf, corn, canola, potato, sugar Rhizoctonia spp_ on sugar beets, vegetables and various other plants such as R. s〇iani (root rot and stem rot) on soybean, and stalk core on rice blast Phytophthora (strain) or R. cerealis (spring blight) on wheat or barley; lychee on strawberries, carrots, kale, vines and tomatoes Rhizopus stolonifer (black mold, soft rot); Rhizochasporium secalis (brown spot) on barley, rye and black wheat Sarocladium oryzae) and S. attenuatum (sheath rot); Sclerotinia spp. (stalk rot or white mold): in vegetables and field crops, such as rapeseed, On the day (such as S. sclerotiorum) and soybeans (such as Sr〇lfsii or Sclerotinia sclerotiorum); Saccharines (brown spots) on wheat, and 8 uhici on wheat (shell needles) Plaque disease) and S. n〇d〇rum (synonym Stagonospora nodorum) (shell occidentosis); vines Uncinula necator (synonym grape white 149027.doc -181 - 201103430 Erysiphe necator) (powder disease, asexuality: Oidium tuckeri); Genus (Setospaeria spp.) (leaf blight) · in corn (such as S. turcicum, synonym Helminthosporium turcicum) and turf; Sphacelotheca Spp.) (Smut): in the corn (such as S. reiliana: head smut), sorghum and sorghum on the melon (Sphaerotheca fuliginea) (Spear white) "Sp〇ng〇spora subterranea" (white sputum) and viral diseases transmitted thereby; the genus of the genus Bacillus on cereals, such as wheat S. nod〇rurn (S. nod 〇 urn ( ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; Lept〇sphaeria nodorum) [synonym phae〇sphaeria nodorum]; Synchytrium end〇bi〇ticum (potato cancer); (Taphrina spp), such as T. def0rmans on the peach (throat leaf disease) and T. pruni on the plum (risk fruit); tobacco, pome fruit, vegetables, Thielaviopsis spp_ (black root rot) on soybean and cotton, such as T. basicola (synonym Chalara elegans); black stalk on scorpion Phytophthora (TiUetia SPP_) (* see smut or stinking smut), such as T. tritici on wheat (synonym τ. τ. caries) , wheat smut) and ta controversa (dwarf smut); Typhula incarnata (grey ferrets) on barley or wheat 'Urocystis Spp.), for example, on rye [ 149027.doc •182- 201103430 Helicobacter pylori (u. occulta) (stem Ear disease); Uromyces spp. (rust) on vegetables, such as beans (eg, u. appendiculatus, synonym for u phase〇H) And sugar beet (for example, u betae); Ustilago spp. (i〇〇se smut): in scorpion (such as smut) (U. nuda) and O. avaenae, corn (such as U. maydis _ · Maize smut) and sugar cane; Ventrica spp. Disease): Verticillium on apples (such as V. inaeq Uaiis) and pears; and various plants (such as fruits and ornamental plants, vines, soft fruits, vegetables, and field crops) Spp〇 (wild wilt), such as strawberry, canola, horse yam and tomato dahliae on the tomato. Compounds I, II and IV and combinations thereof are also suitable for controlling harmful fungi, respectively, in protecting stored products or harvests and protective materials. The term "protective material" is understood to mean the protection of the following technical and non-biological materials against the infestation and destruction of harmful microorganisms such as fungi and bacteria: such as adhesives, glues, wood, paper and cardboard, textiles, leather. , paint dispersions, plastics, cooling lubricants, fibers or fabrics. Regarding the protection of wood and other materials, special attention should be paid to the following harmful fungi: Ascomycetes, such as Ophiostoma spp., Ceratocystis spp., Aureobasidium pullulans, and stalks Sclerophoma spp., Chaetomium spp., Humicola spp., Petriella spp., Trichurus spp.; Basidiomycetes Such as, for example, Conophora 149027.doc •183-201103430 spp., Coriolus spp., Gl〇e〇phyllum spp. 'Lentinus Spp.), Pleurotus spp., Poria spp., Serpula spp., Tyromyces spp., Deuteromycete, such as genus Aspergillus SPP.), Helicobacter genus, Penicillium spp., Trichoderma spp., Alternaria, Paecilomyces spp., and zygomycetes, such as hair Muc〇r spp·' and in addition to protect stored products and harvests, care should be taken to Yeast fungi: Candida and Saccharomyces cerevisiae (Saccharomyces cerevisae) square Compounds I, II and IV, respectively, and combinations thereof may be used to improve the health of plants (Candida spp.). The present invention also relates to a method for improving the health of plants by treating plants, their propagation materials and/or the plants where they are grown or to be grown, in an effective amount of Compounds I, II and/or IV and combinations thereof, respectively. method. The term "phyto-health condition" is understood to mean the condition of a plant and/or its product, 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, improved plant growth and/or greener leaves ("greening effect"), quality (eg, improved content or composition of certain ingredients) and resistance to abiotic and/or biological stresses Receptive. The indicators of the above identified plant health conditions may be interdependent or may be mutually causal. The compounds of formulae I, II and IV may exist in different crystalline variants which may differ in biological activity. It is also the subject matter of the invention. When treating fungi or plants by means of a fungicidal effective amount of active substance

[SI 149027.doc 201103430 物繁殖材料(諸如種子、土壤、表s、材料或房間)以使其 免受真菌侵襲時,化合物I、^及…係按原狀使用或以組合 物形式使用。在植物、植物繁殖材料(諸如種子、土壤、 表面、材料或房間)受到真菌感染之前及之後均可施用。 - 可在種植或移植之時或之前以化合物I、II及/或以按原 • 狀或以包含至少一種化合物I、π及/或1¥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 I、II及/或IV之農用化學組合物及用於防治有害真菌之用 途。 農用化學組合物包含殺真菌有效量之化合物b ^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J、π及/或1¥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 • 纟物’例如溶液、乳液、懸浮液、粉劑、散劑、糊狀物及 ; 齡。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。 組〇物類型之貫例為懸浮液(sc、〇D、Fs)、可乳化濃 縮物㈣、乳液(EW、E〇、ES)、糊狀物、片劑、可濕潤 散劑或粉劑(WP、SP、ss、ws、Dp、DS)或顆粒(GR、 149027.doc -185. 201103430 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(GF)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, 1 967 年 1 2 月 4 日,147-48,Perry's Chemical Engineer’s Handbook,第 4 版,McGraw-Hill,New York, 1963,第 8-57 頁,以下各頁,w〇 91/13546、US 4,172,714、US 4,144,050、US 3,920,442、US 5,180,587、 US 5,232,701 ' 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[SI 149027.doc 201103430 When materials such as seeds, soils, tables, materials or rooms are protected from fungal attack, the compounds I, ^ and ... are used as they are or in the form of a composition. It can be applied before and after infection with plants, plant propagation materials such as seeds, soil, surfaces, materials or rooms. - The plant propagation material can be treated prophylactically with the compounds I, II and/or in the original form or with a composition comprising at least one compound I, π and/or 1 ¥ at or before the planting or transplanting. The invention also relates to agrochemical compositions comprising a solvent or solid carrier and at least one compound I, II and/or IV and for the use in the control of harmful fungi. The agrochemical composition comprises a fungicidally effective amount of the compound b^ and/or IV. The term "effective amount" means an amount of the composition or compound J, π and/or 1 of the compound I, II and / or IV which is sufficient to control harmful fungi or protective materials on cultivated plants and which does not substantially impair the treated plant. . 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. Compounds I, II and IV and their salts can be converted into agrochemical groups of the customary type: 纟 ’ such as solutions, emulsions, suspensions, powders, powders, pastes, and ages. 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. The examples of the type of loquat are suspension (sc, 〇D, Fs), emulsifiable concentrate (4), emulsion (EW, E〇, ES), paste, tablet, wettable powder or powder (WP, SP, ss, ws, Dp, DS) or granules (GR, 149027.doc - 185. 201103430 FG, GG, MG), which may be water soluble or wettable, and used to treat plant propagation material (such as seeds) Gel (GF) Formulations The type of composition (eg, 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, 1 February 4, 147-48, Perry's Chemical Engineer's Handbook , 4th edition, McGraw-Hill, New York, 1963, pp. 8-57, following pages, w〇91/13546, US 4,172,714, US 4,144,050, US 3,920,442, US 5,180,587, US 5,232,701 ' 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))。 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〉谷劑、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、防凍劑、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)。 [S3 149027.doc -186- 201103430 :適,溶劑為水;有機溶劑’諸如中至高沸點之礦物油 β刀諸如煤油或柴油;此外有煤焦油及植物或動物來源 之油,脂族、環狀及芳族煙,例如甲苯、二甲苯、石蝶、 四氣化蔡、⑦基化萘或其衍生物;醇類,諸如甲醇:乙 . #、丙醇、丁醇及環已醇;二醇類;酮類,諸如環己酮及 • γ-丁内醋;脂肪酸二甲醯胺、脂肪酸及脂肪酸酷及強極性 溶劑’例如胺’諸如N_f基吡咯啶酮。 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、白要、紅玄武土、黃土、黏土、白雲 石、矽溱土、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。 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®型, Borregard,Norway)、酚磺酸、萘磺酸(M〇rwet®型,Akz〇 Nobel,U.S.A)、二丁基萘磺酸(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、爿θ肪醇硫酸鹽,及硫酸化十六烧醇、十七烧醇及十八 烷醇之鹽、硫酸化脂肪醇二醇醚、此外有萘或萘續酸與苯 酚及甲醛之縮合物、聚氧乙烯辛基苯基醚、乙氧基化異辛 基酚、辛基酚、壬基酚、烷基苯基聚乙二醇醚、三丁基苯 基聚乙二醇醚、二硬脂酿基苯基聚乙二醇喊、烧基芳基聚 149027.doc -187- 201103430 醚醇、醇及脂肪醇/環氧乙烷縮合物、乙氧基化蓖麻油' 聚氧乙烯院基醚、乙氧基化聚氧丙烯、月桂醇聚乙二醇醚 縮酸、山梨糖醇酯、木質素亞硫酸鹽廢液及蛋白質、變性 蛋白質、多酿(例如’曱基纖維素)、疏水性改質澱粉、聚 乙稀醇(Mowiol® 型,ciariant,Switzerland)、聚缓酸酯 (Sokolan®型’ BASF,Germany)、聚烷氧基化物、聚乙烯胺 (Lupasol型’ BASF,Germany)、聚乙烯吡咯啶酮及其共聚 物0 稍化劑之貫例(亦即,賦予組合物以改良的流動性之化 合物’亦即在靜態條件下之高黏度及在振盪期間之低黏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 carrier 'dispersants or emulsifiers (such as 'other granules, protective colloids, surfactants and binders), organic and inorganic thickeners, bactericides, antifreeze Agents, defoamers, (if appropriate) colorants and tackifiers or binders (for example, for seed treatment formulations). [S3 149027.doc -186- 201103430: suitable, the solvent is water; organic solvent 'such as medium to high boiling mineral oil β knife such as kerosene or diesel; in addition to coal tar and oil of plant or animal origin, aliphatic, ring And aromatic smoke, such as toluene, xylene, stone butterfly, tetra-gasification, 7-based naphthalene or its derivatives; alcohols, such as methanol: B. #, propanol, butanol and cyclohexanol; diol Ketones such as cyclohexanone and • γ-butane vinegar; fatty acid dimethylamine, fatty acids and fatty acids and strong polar solvents such as amines such as N_f-pyrrolidone. The solid carrier is mineral soil, such as citrate, tannin, talc, kaolin, limestone, lime, white, red basalt, loess, clay, dolomite, alumina, calcium sulfate, magnesium sulfate, magnesium oxide; Grinding synthetic materials, fertilizers 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 solids Carrier. Suitable surfactants (adjuvants, wetting agents, tackifiers, dispersants or emulsifiers) are aromatic sulfonic acids (eg lignin sulfonic acid (B〇rresperse® type, Borregard, Norway), phenolsulfonic acid, naphthalene Sulfonic acid (M〇rwet® type, Akz〇Nobel, USA), dibutylnaphthalenesulfonic acid (Nekal® type, basf, Germany)) and alkali metal salts, alkaline earth metal salts and ammonium salts of fatty acids; alkane-sulfonate Acid salt, alkyl aryl sulfonate, alkyl sulfate, lauryl ether sulfuric acid salt, 爿 肪 肪 alcohol sulfate, and sulfated hexadecanol, heptadecyl alcohol and stearyl alcohol, Sulfated fatty alcohol glycol ether, in addition to condensate of naphthalene or naphthalene acid with phenol and formaldehyde, polyoxyethylene octyl phenyl ether, ethoxylated isooctyl phenol, octyl phenol, nonyl phenol, alkane Phenyl phenyl polyglycol ether, tributyl phenyl polyglycol ether, distearyl phenyl PEG, aryl aryl group 149027.doc -187- 201103430 ether alcohol, alcohol and Fatty alcohol/ethylene oxide condensate, ethoxylated castor oil 'polyoxyethylene yard ether, ethoxylated polyoxypropylene, lauryl polyethylene glycol ether, sorbate Sugar alcohol esters, lignin sulfite waste liquids and proteins, denatured proteins, multi-flavored (eg 'mercapto cellulose'), hydrophobic modified starch, polyethylene glycol (Mowiol® type, ciariant, Switzerland), poly slow Examples of acid esters (Sokolan® type 'BASF, Germany), polyalkoxylates, polyvinylamines (Lupasol type 'BASF, Germany), polyvinylpyrrolidone and copolymers thereof 0 (ie, A compound that imparts improved fluidity to the composition', ie high viscosity under static conditions and low viscosity during oscillation

度)為多醣及有機及無機黏土 ’諸如三仙膠(Kelzan®,CPDegree) for polysaccharides and organic and inorganic clays such as Sanzan Gum (Kelzan®, CP)

Kelco, U.S.A.) ^ Rhodopol® 23(Rhodia, France) ^ Veegum® (R.T. Vanderbilt, U.S.A.)^ Attaclay®(Engelhard Corp., NJ, USA) 〇Kelco, U.S.A.) ^ Rhodopol® 23 (Rhodia, France) ^ Veegum® (R.T. Vanderbilt, U.S.A.)^ Attaclay® (Engelhard Corp., NJ, USA) 〇

可添加殺細菌劑以便保存組合物且使組合物穩定。合適 权細函知彳之實例為彼等基於雙氣盼及苯曱醇半縮甲酸(icI 之 Proxel® 或 Thor Chemie之 Acticide® RS及 Rohm &amp; Haas之A bactericide may be added to preserve the composition and stabilize the composition. Examples of suitable rights are those based on double gas and phenyl decyl hemiformic acid (ICI's Proxel® or Thor Chemie's Acticide® RS 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°塞。坐琳_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,Siiikon® SRE, Wacker,Germany 或 Rhodorsil®, Rh〇dia,France)、長鏈醇、 脂肪酸、脂肪酸鹽、氟有機化合物及其混合物。 t I49027.doc •188- 201103430 A二者色劑為低水溶性顏料及水溶性染料。所提及且 _紅1、顏料藍15:4、顏料藍15:3、顏料藍15:2、顏料藍 15]、顏料藍8G、顏料黃i、顏料黃13、顏料紅⑴、顏料 紅伙2、顏料紅48:1、顏料紅…、顏料紅加、顏料撥 43、顏料橙34、顏料橙5、顏料綠% '顏料綠7、顏料白 6、顏料棕25、鹼性紫10、鹼性紫49、酸性紅$丨、酸性紅 52、酸性紅14、酸性藍9、酸性黃23、鹼性紅1〇、鹼性红 108。 匕增黏劑或黏合劑之實例為聚乙烯料相、聚乙酸乙婦 酯、聚乙烯醇及纖維素醚(Tyl〇se®,SMnEtsu,了邛抓)。 可藉由將化合物I及(若適當)其他活性物質與至少一種固 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 石石夕凑土、硫酸妈、硫酸鎂、氧化鎮;經研磨之合成材 料,肥料,諸如硫酸敍、磷酸錢、硝酸錄、尿素·,及植物 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。 組合物類型之實例為: 1.以水稀釋之組合物類型 0水溶性濃縮物(SL、LS) 149027.doc -189- 201103430 將ι〇重量份本發明化合物!溶解於9〇重量份水中或水溶 性溶劑中。或I,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1G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j溶於7〇重量份環己酮中,同 時添加10重里伤为政劑,例如聚乙稀。比。各α定酮。以水稀 釋,產生分散液。活性物質含量為20重量%。 iii) 可乳化濃縮物(EC) 將1 5重量份本發明化合物I溶解於75重量份二甲苯中, 同時添加十二烷基苯磺酸鈣及萬麻油乙氧化物(分別為5重 量份)。以水稀釋,產生乳液。該組合物具有〖5重量%之活 性物質含量。 iv) 乳液(EW、EO、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 量份)。將此混合物藉助於乳化機(Ultraturrax)引入30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25重量%之活性物質含量。 v) 懸浮液(SC、OD、FS) 在攪動式球磨機中’將20重量份本發明化合物I艰磨, 同時添加10重量份分散劑及濕潤劑及70重量份水或有機溶 劑’得到精細的活性物質懸浮液。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20重量%。Kathon® MK) is a bactericide and an isothiazolinone derivative such as an alkyl isocyanide. Sitting on lin and benzoisothiazolone (Thutr chemie Acticide® MBS). Examples of suitable antifreeze agents are ethylene glycol, propylene glycol, urea and glycerin. Examples of antifoaming agents are polyoxynitride emulsions (such as Siiikon® SRE, Wacker, Germany or Rhodorsil®, Rh〇dia, France), long chain alcohols, fatty acids, fatty acid salts, fluoroorganic compounds, and mixtures thereof. t I49027.doc •188- 201103430 A The two colorants are low water-soluble pigments and water-soluble dyes. Mentioned and _ red 1, pigment blue 15:4, pigment blue 15:3, pigment blue 15:2, pigment blue 15], pigment blue 8G, pigment yellow i, pigment yellow 13, pigment red (1), pigment red 2, pigment red 48: 1, pigment red ..., pigment red plus, pigment dial 43, pigment orange 34, pigment orange 5, pigment green % 'pigment green 7, pigment white 6, pigment brown 25, alkaline purple 10, alkali Sexual purple 49, acid red $ 丨, acid red 52, acid red 14, acid blue 9, acid yellow 23, alkaline red 1 〇, alkaline red 108. Examples of 匕 tackifiers or binders are polyethylene phase, polyethylene acetate, polyvinyl alcohol and cellulose ether (Tyl〇se®, SMnEtsu, Scratch). Powders, dispersion materials and powders can be prepared by mixing the compound I and, if appropriate, other active substances with at least one solid carrier or with grinding. 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, sulphate, magnesium sulfate , oxidized town; ground synthetic materials, fertilizers, such as sulphate, phosphoric acid, nitric acid, urea, and plant-derived products, such as cereal meal, bark meal, wood meal and nut meal, cellulose Powder; and other solid carriers. Examples of composition types are: 1. Type of composition diluted with water 0 Water soluble concentrate (SL, LS) 149027. doc - 189 - 201103430 The amount of the compound of the invention is ι 〇! Dissolved in 9 parts by weight of water or a water-soluble solvent. Or I, add a wetting agent or other additives. Once diluted with water, the active substance dissolves. In this way, a composition having an active substance content of 1 G% by weight was obtained. Ii) Dispersible Concentrate (DC) 20 parts by weight of the compound j of the present invention is dissolved in 7 parts by weight of cyclohexanone, while adding 10 weights of a chemical agent such as polyethylene. ratio. Each alpha ketone. Dilute with water to produce a dispersion. The active substance content was 20% by weight. Iii) Emulsifiable Concentrate (EC) 15 parts by weight of the compound I of the present invention is dissolved in 75 parts by weight of xylene, and simultaneously added calcium dodecylbenzenesulfonate and eucalyptus ethoxylate (5 parts by weight, respectively) . Dilute with water to produce an emulsion. The composition has an active substance content of 5% by weight. Iv) Emulsion (EW, EO, ES) 25 parts by weight of the compound I of the invention is dissolved in 35 parts by weight of xylene, together with calcium dodecylbenzenesulfonate and castor oil ethoxylate (5 parts by weight, respectively) . This mixture was introduced into 30 parts by weight of water by means of an emulsifier (Ultraturrax) 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 the agitated ball mill '20 parts by weight of the compound I of the invention, while adding 10 parts by weight of dispersant and wetting agent and 70 parts by weight of water or organic solvent' to obtain fine Active substance suspension. Dilution with water produces a stable suspension of the active substance. The active substance content in the composition was 20% by weight.

[SI 149027.doc -190- 201103430 vi) 水分散性顆粒及水溶性顆粒(Wg、sg) 將50重罝份本發明化合物i細磨,同時添加5〇重量份分 月欠劑及濕潤劑,藉助於工業級設備(例如擠壓機、喷霧 塔、流體化床)將其製備成水分取性或水溶性顆粒。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) 水为政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〗,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) 在攪動式球磨機中,將20重量份本發明化合物〗碾磨, 同時添加10重量份分散劑、i重量份膠凝劑濕潤劑及7〇重 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2〇%(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工細磨且與95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〗細磨且與99 5重量份載劑組 149027.doc 191 - 201103430 合。當前方法為擠壓、喷霧乾燥或流體化床。此操作得到 具有0.5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丨溶於9〇重量份有機溶劑(例如 二甲苯)中。此操作得到具有1〇重量%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〇 〇1與95重量%,較佳〇丨與卯 重量%之間’最佳0.5與9〇重量%之間的活性物質。使用純 度為90%至1〇〇%,較佳95%至丨〇〇%(根據nmr光譜)之活性 物質。 為處理植物繁殖材料(尤其種子)之目的,通常使用水溶 性濃縮物(LS)、可流動濃縮物(FS)、供乾燥處理之散劑 (DS)、供㈣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)及凝膠此等組 合物可經稀釋或未經稀釋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 〇.〇1至60重,較佳〇 u4〇重量%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 物分別施用於或處理植物繁殖材料(尤其種子)之方法在此 項技術中已知,包括繁殖材料之摔藥(dressi♦包衣、丸 化撒各、浸泡及溝施方法。在一個較佳實施例中,藉由 不會誘導發芽之方法,例如藉由種子摔藥、丸化、包衣及 撒私將化合物或其組合物分別施用於植物繁殖材料上。 在-個較佳實施例中’懸浮液型(FS)組合物係用於種子[SI 149027.doc -190- 201103430 vi) Water-dispersible granules and water-soluble granules (Wg, sg) 50 parts by weight of the compound i of the present invention is finely ground, and 5 parts by weight of a monthly effluent and a wetting agent are added. It is prepared as a moisture-retaining or water-soluble granule by means of industrial grade equipment such as extruders, spray towers, fluidized beds. 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-based powder and water-soluble powder (wp, sp, SS, WS) 75 parts by weight of the compound of the 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) In an agitated ball mill, 20 parts by weight of a compound of the invention is milled while adding 10 parts by weight of a dispersant, i by weight of a gelling agent wetting agent, and 7 parts by weight of water or an organic solvent. A fine suspension of the active substance is obtained. A stable suspension of the active substance is produced by dilution to obtain a composition having 2% by weight (w/w) of the active substance. 2. Type of composition to be applied without dilution ix) Powderable powder (DP, DS) 5 parts by weight of the compound 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 invention were finely ground and combined with 99 parts by weight of the vehicle group 149027.doc 191 - 201103430. Current methods are extrusion, spray drying or fluidized beds. This operation was obtained with 0.5 weight. /. A granule that is applied without dilution of the active substance content. Xi) ULV solution (UL) 10 parts by weight of the compound of the present invention is dissolved in 9 parts by weight of an organic solvent such as xylene. This operation resulted in an undiluted composition having an active substance content of 1% by weight. The agrochemical composition typically comprises between 0.51 and 95% by weight, preferably between 0.5 and 重量 by weight, of an optimum of between 0.5 and 9% by weight. An active material having a purity of 90% to 1%, preferably 95% to 丨〇〇% (according to the nmr spectrum) is used. For the purpose of treating plant propagation materials (especially seeds), water-soluble concentrates (LS), flowable concentrates (FS), powders for drying treatment (DS), water-dispersible powders (ws) for (iv) treatment are usually used. , water-soluble powder (ss), emulsion (ES), emulsifiable concentrate (EC) and gel. These compositions can be applied to plant propagation materials either diluted or undiluted, especially in seed-related compositions at 2 to 1 〇 After the double dilution, an active substance concentration of from 1 to 60, preferably 〇u4% by weight, is obtained in the ready-to-use preparation. It can be applied before or during sowing. Methods of applying agrochemical compounds and compositions thereof to or treating plant propagation materials, particularly seeds, are known in the art, including propellant materials (dressi♦ coating, pelleting, soaking, and ditching). 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, such as by seed medicine, pelleting, coating, and spreading. - a preferred embodiment of the 'suspension type (FS) composition for seed

[SI 149027.doc -192- 201103430 g/Ι活性物質、1-200 〇至400 g/Ι黏合劑、〇 處理。通常’ FS組合物可包含l_8〇〇 g/ι界面活性劑、〇至200 g/ι防凍劑、 至200 g/Ι顏料,及至丨公升之溶劑(較佳為水卜 活性物質可以原狀或以其組合物形式,例如以直接可喷 渡溶液、㈣、懸浮液、分散液、乳液、油分散液、糊狀 物、可粉化產品、散播物質或顆粒之形式,藉由噴灑 '霧 化、撒粉、散播、刷塗、浸潰或傾注使用。施用形式完全 視所欲目的而定;意欲確保本發明之活性物質在各情況下 最細微可能的分佈。 可由乳液濃縮物、糊狀物或可濕潤散劑(可喷灑散劑, 油分散液)添加水製備含水施用形式。為製備乳液、糊狀 物或油分散液,可藉由潤濕劑、増黏劑、分散劑或乳化劑 使原狀或溶於油或溶劑中之物質在水中均質化。或者,可 能製備由活性物質、濕潤劑、增黏劑、分散劑或乳化劑及 (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當廣泛範圍内變化。 一般而言,濃度範圍為0.0001至1〇重量%,較佳0.001至i 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 性物質之量為0.001至2公斤/公項(kg/ha) ’較佳0.005至2公 I49027.doc -193- 201103430 斤/公項’更佳0.05至0.9公斤/公項,尤其〇 n75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:ϋ至 1000公克,較佳1至1000公克,更佳1至100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 施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,較佳〇 〇〇5公克至〗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 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1:1〇〇至1〇〇1,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石夕氧院,諸如 u S 240 ,醇烷氧基化物,諸如⑯、[SI 149027.doc -192- 201103430 g / Ι active substance, 1-200 〇 to 400 g / Ι binder, 〇 treatment. Typically the 'FS composition may comprise l_8〇〇g/ι surfactant, 〇 to 200 g/ι antifreeze, up to 200 g/Ι pigment, and to liters of solvent (preferably the water active substance may be as it is or a form of the composition, for example, in the form of a direct sprayable solution, (iv), a suspension, a dispersion, an emulsion, an oil dispersion, a paste, a powderable product, a dispersed material or granules, by spraying 'atomization, Powdering, spreading, brushing, dipping or pouring. The application form is entirely dependent on the intended purpose; it is intended to ensure the finest possible distribution of the active substance of the invention in each case. It may be by emulsion concentrate, paste or Wettable powder (sprayable powder, oil dispersion) is added with water to prepare an aqueous application form. To prepare an emulsion, paste or oil dispersion, it can be made by a wetting agent, a viscous agent, a dispersing agent or an emulsifier. Or a substance dissolved in an oil or a solvent is homogenized in water. Alternatively, a concentrate composed of an active substance, a wetting agent, a tackifier, a dispersing agent or an emulsifier and, if appropriate, a solvent or oil may be prepared, and such Concentrate suitable for Diluted with water. The concentration of the active substance in the ready-to-use preparation can vary over a wide range. Generally, the concentration ranges from 0.0001 to 1% by weight, preferably from 0.001 to 9% by weight of active substance. The method (ULV) successfully uses the active substance, it is possible to apply a composition comprising more than 95% by weight of active substance, or even to apply the active substance without additives. When used for plant protection, depending on the type of action desired The amount of active substance applied is 0.001 to 2 kg / part (kg / ha) 'better 0.005 to 2 public I49027.doc -193- 201103430 kg / public 'better 0.05 to 0.9 kg / public , especially 75 n75 kg / public. When treating plant propagation materials (such as seeds) by spraying, coating or soaking seeds, for example, the active mass generally needs to be in the following range: ϋ to 1000 grams, preferably 1 Up to 1000 grams, more preferably 1 to 100 grams and most preferably 5 to 1 gram per 100 kilograms of plant propagation material (preferably seeds). When used to protect materials or store products, the quality of the applied active depends on the application. Domain type Depending on the desired action, the amount conventionally used for material protection is, for example, from 0.001 to 2 kg, preferably from 5 to 8,000 kg of active substance per cubic meter of treated material. Wetting agents, adjuvants, herbicides, bactericides, other fungicides and/or insecticides are added to the active substance or compositions containing it' (if appropriate) until it is ready for use (in-tank mixing) These agents may be mixed with the composition of the invention in a weight ratio of 1:1 Torr to 1 〇〇 1, preferably 1: 10 to 10: 1. The adjuvants which may be used are especially modified organic polyliths. Oxygen hospital, such as u S 240, alcohol alkoxylate, such as 16,

MBA 1303、Plurafac lf 300®及 Lutensol ON 30® ; EO/PO 後段聚合物’例如’心他刪加^及⑹㈣^醇 乙氧基化物,諸如Lutensol xp 8〇⑯;及:辛基石黃基破拍酸 鈉’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MBA 1303, Plurafac lf 300® and Lutensol ON 30®; EO/PO back-end polymer 'for example, 'additional ^ and (6) (four) alcohol ethoxylates, such as Lutensol xp 8〇16; and: octyl stellite Sodium ate 'such as Leophen RA®. The compositions of the present 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.

[SI 149027.doc -194- 201103430 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(str〇bilurin) 亞托敏(azoxystrobin)、地莫菌胺(dimoxystr〇bin)、烯肟 菌酉曰(enestroburin)、I 氧菌胺(fiuoxastr〇bin) ' 克收欣 (kresoxim-methyl)、苯氧菌胺(met〇minostr〇bin)、奥瑞菌 月女(orysastrobin)、《&gt;定氧菌胺(piCOXyStr〇bin)、百克敏 (pyraclostrobin)、°比瑞笨卡(pyribe:ncarb) '三 氣敏 (trifloxystrobin)、2-(2-(6-(3-氯-2-曱基-苯氧基)-5-氟-嘧 啶-4-基氧基)-苯基)_2_曱氧基亞胺基曱基-乙醯胺、3 -甲 氧基-2-(2-(N-(4-曱氧基-苯基)_環丙烷-甲醯亞胺基硫基曱 基)-苯基)-丙烯酸曱酯、(2-氣-5-[l-(3-曱基苄氧基亞胺基) 乙基]苄基)胺基曱酸曱酯及2-(2-(3-(2,6-二氣苯基)-1-甲基-亞烯丙基胺基氧基曱基)-笨基)_2-曱氧基亞胺基-N-曱基-乙 醯胺; B) 羧醯胺類 - 羧醯苯胺類: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(carb〇xin)、甲呋醯胺 149027.doc -195· 201103430 (fenfuram)、環醯菌胺(fenhexamid)、氟多寧 (flutolanil)、福拉比(furametpyr)、異。比贊 (isopyrazam)、異噻菌胺(isotianil)、克拉昔 (kiralaxyl)、滅鑛胺(mepronil)、滅達樂(metalaxyl)、 滅達樂-M(甲霜靈(mefenoxam))、0夫酿胺(ofurace)、歐 殺斯(oxadixyl)、氧化萎鑪靈(ox;yCarb〇xin)、°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-曱基-噻唑-5-曱醯苯胺、2-氣-N-(1,1,3-三曱基-茚滿-4-基)-菸鹼醯胺、N-(3,,4',5,-三氟 聯苯-2-基)-3-二氟曱基-1-甲基-1H-吡唑-4-曱醯胺、Ν-Ο1-三氟 甲基硫基聯苯-2-基)-3-二 氟甲基-1-曱基-1H-&quot; 比 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N-(2-(l,3,3-三甲基-丁基)-苯基)-1,3-二曱基-5-氟-1H-d比唑-4-甲醯胺; - 叛基嗎琳類:達滅芬(dimethomorph)、敗嗎琳 (flumorph)、丁。比嗎淋(pyrimorph); - 苯甲酸酿胺:It美醯胺(flumetover)、氣°比菌胺 (fluopicolide)、敗 α比胺(fluopyram)、氣苯.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; - 其他叛酿胺:加普胺(carpropamid)、百治美特 (dicyclomet)、雙炔醯菌胺(mandiproamid)、土徽素 (oxytetracyclin)、石夕硫芬(silthiofarm)及 N-(6-甲氧基-[SI 149027.doc -194- 201103430 Only mixed (in-tank mixing). 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 is expanded or prevented. 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) str〇bilurin, azoxystrobin, and delixillamide ( Dimoxystr〇bin), enestroburin, fiuoxastr〇bin 'kresoxim-methyl, methotrexate, oryrobacter (orysastrobin), "&gt; acCOXyStr〇bin, pyracostrobin, pyrier: ncarb" trifloxystrobin, 2-(2-(6-( 3-Chloro-2-indolyl-phenoxy)-5-fluoro-pyrimidin-4-yloxy)-phenyl)_2-decyloxyimidoindolyl-acetamide, 3-methoxy 2-(N-(N-(4-decyloxy-phenyl)-cyclopropane-carboxamidothio-indenyl)-phenyl)-decyl acrylate, (2-gas-5-[ 1-(3-Mercaptobenzyloxyimino)ethyl]benzyl)amino decanoate and 2-(2-(3-(2,6-diphenyl)-1-methyl) -Allallylaminooxyindolyl)-styl)_2-decyloxyimido-N-indenyl-acetamide; B) Carboxylammonium - Carboxyanilide : Benalaxyl, Benalaxyl-M, benodanil, bixafen, boscalid, carb〇xin, methylfuran Amine 149027.doc -195·201103430 (fenfuram), fenhexamid, flutolanil, furametpyr, isoform. Isopyrazam, isotianil, kiralaxyl, mepronil, metalaxyl, methaul-M (mefenoxam), 0 Ofurace, oxadixyl, ox; yCarb〇xin, penthiopyrad, sedaxane, tecloftalam, race Thifluzamide, tiadinil, 2·amino-4-mercapto-thiazole-5-nonanilide, 2-gas-N-(1,1,3-tridecyl-indan 4-yl)-nicotine decylamine, N-(3,,4',5,-trifluorobiphenyl-2-yl)-3-difluoroindol-1-yl-1H-pyrazole- 4-decylamine, Ν-Ο1-trifluoromethylthiobiphenyl-2-yl)-3-difluoromethyl-1-indenyl-1H-&quot; Biazole-4-decylamine, N -(2-(l,3-dimercapto-butyl)-phenyl)-1,3-didecyl-5-fluoro-1H-pyrazole-4-decylamine and N-(2-( l,3,3-Trimethyl-butyl)-phenyl)-1,3-dimercapto-5-fluoro-1H-dbiazole-4-carboxamide; - Rebelism: Dimethomorph, flumorph, Ding. Pyrimorph; - benzoic acid amine: It flumetover, fluopicolide, fluopyram, zoxamide, N-( 3-ethyl-3,5,5-trimethyl-cyclohexyl)-3-mercaptoamino-2-hydroxy-benzoguanamine; - other apoemic amines: carpropamid, hundred Dicyclomet, mandiproamid, oxytetracyclin, silthiofarm and N-(6-methoxy-

[SI 149027.doc -196· 201103430 吡啶-3-基)環丙烷甲酸醯胺; C) °坐類 -三0坐類:阿紮康0坐(azaconazole)、比多農(bitertanol)、 溴克 °坐(bromuconazole)、環克《•坐(cyproconazole)、苯 趟甲環0坐(difenoconazole)、二石肖康》坐(diniconazole)、 二石肖康α坐-Μ、氟環°坐(epoxiconazole)、芬布康唾 (fenbuconazole)、氟奎康。坐(fluquinconazole)、氟石夕《•坐 (flusilazole)、護汰芬(flutriafol)、六康 〇坐 (hexaconazole)、亞胺。坐(imibenconazole)、依普克 〇坐 (ipconazole)、葉菌唾(metconazole)、麥環丁尼 (myclobutanil)、嗯口米口坐(oxpoconazole)、巴克素 (paclobutrazole)、潘康唾(penconazole)、丙環唾 (propiconazole)、丙石荒醇克嗤(prothioconazole)、石夕氤 。坐(simeconazole)、得克利(tebuconazole)、敗趟唾 (tetraconazole)、三泰芬(triadimefon)、三泰隆 (triadimenol)、環菌嗤(triticonazole)、烯效唾 (uniconazole)、1-(4-氯-苯基)-2-([1,2,4]三嗤-1-基)-環 庚醇; - 味°坐類:赛座滅(cyazofamid)、依滅列(imazalil)、稻痕 醋(pefurazoate)、撲克拉(prochloraz) ' 賽福座 (triflumizole); - 苯并咪唑類:苯菌靈(benomyl)、貝芬替 (carbendazim)、麥穗靈(fuberidazole)、°塞苯味嗤 (thiabendazole); 149027.doc -197- 201103430 ~ 其他:乙°塞博胺(ethaboxam)、依得利(etridiazole)、°惡 黴靈(hymexazole)及 2-(4-氣-苯基)-N-[4-(3,4-二曱氧基-苯基)-異噁唑-5-基]-2-丙-2-炔氧基-乙醯胺; D)雜環化合物 -。比咬類: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]比啶、3-[5-(4-曱基-苯基)-2,3-二曱基-異噁唑啶-3-基]比啶、 2,3,5,6-四-氣-4-曱磺醢基-。比啶、3,4,5-三氣吡啶-2,6-二-甲腈、N-(l-(5-溴-3-氣-吡啶-2-基)-乙基)-2,4-二氯 菸鹼醯胺、N-[(5-溴-3-氯-吡啶-2-基)-甲基]-2,4-二氣-菸鹼醯胺; -。密 D定類:績。密菌靈(bupirimate)、西波定(cyprodinil)、 二氟林(diflumetorim)、芬瑞莫(fenarimol)、°密菌月宗 (ferimzone)、米潘尼比林(mepanipyrim)、氣0定 (nitrapyrin)、I苯。密咬醇(nuarim〇l)、比利美沙尼 (pyrimethanil); - 派唤類:賽福寧(triforine); -°比 B各類:拌種 17各(fenpiclonil)、護汰寧(fludioxonil); • 嗎琳類:阿迪嗎琳(aldimorph)、嗎菌靈(dodemorph)、 乙酸嗎菌靈、粉鑛琳(fenpropimorph) '十三嗎琳 (tridemorph); - 派°定類:苯鑛°定(fenpropidin); - 二甲醯亞胺:氟醯亞胺(fluoroimid)、依普同 (iprodione)、撲滅寧(procymi done)、免克寧 [S1 149027.doc -198- 201103430 (vinclozolin); - 非芳私5-貝雜環:„惡。坐菌酮(fainoxad〇ne)、0米0坐菌酮 (fenamidone)、敗多寧(fiutianii)、辛 0塞酮 (octhilinone)、〇塞菌靈(pr〇benazole)、5-胺基-2-異丙 基-3-側氧基-4-鄰-甲苯基_2,3_二氫-吡唑-1-硫代甲酸S- 稀丙S旨, -其他:酸化苯并噻二唑-S-曱酯(acibenzolar_s_ methyl) 、 α引唾續菌胺(amisulbrom)、敵菌靈 (anilazin)、殺稻瘦素 _s(blasticidin-S)、四氯丹 (captafol)、篕普丹(captan)、滅蜗猛 (chinomethionat)、邁隆(dazomet) 、 °米菌威 (debacarb) 噠菌清(diclomezine)、苯敵快 (difenzoquat)、苯敵快-曱基硫酸鹽、禾草靈 (fenoxanil)、福爾培(Folpet)、歐索林酸(〇x〇linic acid)、粉病靈(piperalin)、普奎那兹(proquinazid)、百 快隆(pyroquilon)、快諾芬(quinoxyfen)、咪唑嗪 (triazoxide)、三赛唑(tricyclazole)' 2-丁氧基-6-碘-3-丙基咬稀-4-酮、5-氯-1-(4,6-二甲氧基-嘧咬-2-基)-2-曱 基-1H-苯并咪唑、5-氣-7-(4-曱基哌啶-1-基)_6-(2,4,6-三氟苯基)-[1,2,4]三唑并[1,5-&amp;]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 - 硫代胺基甲酸酯及二硫代胺基曱酸酯,福美鐵 (ferbam)、代森锰鋅(mancozeb)、代森猛(maneb)、威 149027.doc -199- 201103430 百故(metam)、績菌威(methasulphocarb)、代森聯 (metiram)、丙森鋅(pr0pineb)、福美雙(thiram)、代森 鋅(zineb)、福美鋅(zirarn); - 胺基曱酸醋:苯π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(vaiiphenal) 及N-(l-(l-(4-氰基-苯基)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)、多寧游離驗、雙胍辛 (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:春日黴素(kasugamycin)、春日黴素鹽酸鹽水 合物、鍵徽素(streptomycin)、多氧菌素(polyoxine)、 有效黴素 A(validamycin A); - 硝基苯基衍生物:百蜗克(binapacryl)、大脫蜗 (dinobuton)、白粉克(dinocap)、酞菌酯〇1如1^1-isopropyl)、四氣硝基苯(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); - 有機構化合物:護粒松(edifenphos)、三乙膦酸 (fosetyl)、三乙膦酸銘(fosetyl-aluminum)、丙基喜樂 [S3 149027.doc -200- 201103430 松(iprobenfos)、亞磷酸及其鹽、白粉松(pyraz〇ph〇〇、 脫克松(tolclofos-methyl); - 有機氯化合物:百菌清(chlorothalonil)、益發靈 (dichlofluanid)、雙氯酌·(dichlorophen)、I 硫滅 (flusulfamide)、六氣苯、賓克隆(penCyCUron)、五氯齡 及其鹽、苯酞(phthalide)、奎脫辛(quintozene)、曱基 多保淨 (thiophanate-methyl)、 曱基益發靈 (tolylfluanid)、N-(4-氣-2-硝基-苯基)-N-乙基-4-曱基 _ 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、演硝醇(bronopol) 、α塞芬胺 (cyflufenamid)、霜脲氰(cymoxanil)、二苯胺、美曲芬 諾(metrafenone)、滅粉黴素(mildiomycin) ' 經基啥咐 銅(oxin-copper)、調環酸約(prohexadione-calcium)、螺 環菌胺(spiroxamine)、甲基益發靈(tolylfluanid)、N-(環丙基甲氧基亞胺基_(6-二氟-曱氧基-2,3-二氟-苯基)-曱基)-2-苯基乙酿胺、N1-(4-(4·-氣-3-三氣曱基-苯氧 基)-2,5-二曱基-笨基乙基-N-甲基甲脒、Ν·-(4-(4-氟-3-三氟甲基-苯氧基)_2,5-二甲基-苯基)-Ν-乙基-Ν-甲 基甲脒、:ΝΓ-(2-甲基-5-三氟甲基-4-(3·三曱基矽烷基-丙 氧基)-苯基)-Ν-乙基-Ν-甲基甲脒、Ν·-(5-二氟甲基-2-曱基-4-(3-三甲基矽烷基-丙氧基)-苯基)-Ν-乙基-Ν-甲 基曱脒、2-{1-[2-(5-甲基-3-三氟甲基-吡唑-1-基)-乙醯 149027.doc -201 - 201103430 基]-哌啶-4-基}-噻唑-4-曱酸曱基-(1,2,3,4-四氫-萘-ΐ· 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-曱酸甲基-(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-啥 啉-4-基酯。 G)生長調節劑 脫落酸、呋喃丹(amidochlor)、三環苯嘧醇 (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)、環烧基醯苯胺(cyclanilide)、丁, 醯餅·(daminozide)、敵草克(dikegulac)、°塞節因 (dimethipin)、2,6-二曱基°比咬、益收生長素 (ethephon) 敗印胺(flumetralin)、吱 °密醇 (flurprimidol)、噠草氟(fluthiacet)、氯吡脲 (forchlorfenuron)、赤黴酸(gibberellic acid)、依納素 (inabenfide)、吲哚-3-乙酸、順丁烯二醯肼(maleic hydrazide)、氟續醯草胺(mefluidide)、壯棉素 (mepiquat)(壯棉素氯化物)、萘乙酸、N-6-苄基腺嗓 呤、巴克素、調環酸(調環酸鈣)、茉莉酸丙酯 (prohydrojasmon)、°塞苯隆(thidiazuron)、抑芽唾 (triapenthenol)、三丁基三硫磷酸酯、2,3,5-三碘苯甲 酸、抗倒酯(trinexapac-ethyl)及稀效°坐; [S1 149027.doc -202- 201103430 Η)除草劑 - 乙酸胺類:乙草胺(acetochlor)、曱草胺(alachlor)、去 草胺(butachlor)、二甲草胺(dimethachlor)、二甲0塞草 胺(dimethenamid)、氟嗔草胺(flufenacet)、苯°塞酸草胺 (mefenacet)、異丙甲草胺(metolachlor)、°比草胺 (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)、丁基賽 伏草(cyhalofop-butyl)、°惡 °坐禾草靈(fenoxaprop)、口比 氟禾草靈(fluazifop)、°比氟氯禾靈(haloxyfop)、。惡唾醯 草胺(metamifop)、普拔草(propaquizafop)、啥禾靈 (quizalofop)、11奎禾靈糠醋(quizalofop-P-tefuryl); - 聯°比11定類:敵草快(diquat)、百草枯(paraquat); -(硫代)胺基曱酸酯類:亞速爛(asulam)、蘇達滅 (butylate)、卡草胺(carbetamide)、甜菜安 (desmedipham)、派草丹(dimepiperate)、撲草滅 (eptam ,EPTC)、戊草丹(esprocarb)、得草滅 (molinate)、坪草丹(orbencarb)、甜菜寧 (phenmedipham)、苄草丹(prosulfocarb)、稗草畏 149027.doc -203 - 201103430 (pyributicarb)、殺丹(thiobencarb)、野麥畏(triallate); - 環己二鲷類:丁苯草酮(butroxydim)、克草同 (clethodim)、環殺草(cycloxydim)、環苯草酮 (profoxydim)、西殺草(sethoxydim)、得殺草 (tepraloxydim)、苯草 _(tralkoxydim); - 二确基苯胺類··倍尼芬(benfluralin)、乙丁烯氟靈 (ethalfluralin)、安項靈(oryzalin)、二甲戊樂靈 (pendimethalin)、胺氟樂靈(prodiamine)、氟樂靈 (trifluralin); - 二苯謎類:三氣叛草醚(acifluorfen)、苯草鍵 (aclonifen)、必芬諾(bifenox)、禾草靈(diclofop)、氣 氟草醚(ethoxyfen)、氟續胺草醚(fomesafen)、乳氟禾 草靈(lactofen)、乙氧氟草趟(oxyfluorfen); - 經基苯曱腈類:漠苯腈(bomoxynil)、二氣苯腈 (dichlobenil)、峨苯精; - 咪°坐琳酮類·· p米草醋(imazamethabenz)、甲氧咪草煙 (imazamox)、曱咪0坐煙酸(imazapic)、滅草煙 (imazapyr)、滅草嗜(imazaquin)、。米草煙 (imazethapyr); - 苯氧基乙酸類:稗草胺(clomeprop)、2,4-二氯苯氧乙 酸(2,4-D)、2,4-DB、滴丙酸(dichlorprop)、MCPA、 MCPA-硫乙基、MCPB、2-曱-4-氯丙酸(Mecoprop); -°比嗪類:氣草敏(chloridazon)、氟建嗓草醋(flufenpyr-ethyl) 、 °塞乙草 S旨(fluthiacet)、氣草敏[SI 149027.doc -196· 201103430 pyridin-3-yl)cyclopropanecarboxylic acid decylamine; C) ° sitting class - three 0 sitting class: Azacon 0 sitting (azaconazole), than donut (bitertanol), brom ° bromuconazole, cyproconazole, difenoconazole, dichoxon, diniconazole, dioxin, ketone, epoxiconazole, fenbux芬buconazole, fluoroquine. Fluquinconazole, flusilazole, flutriafol, hexaconazole, imine. Ibibenconazole, ipconazole, metconazole, myclobutanil, oxpoconazole, paclobutrazole, penconazole , propiconazole, prothioconazole, and stone scorpion. Simeconazole, tebuconazole, tetraconazole, triadimefon, triadimenol, triticonazole, uniconazole, 1-(4- Chloro-phenyl)-2-([1,2,4]triin-1-yl)-cycloheptanol; - taste ° sitting class: cyazofamid, imazalil, rice mark Peacheazoate, prochloraz 'triflumizole'; - benzimidazoles: benomyl, carbendazim, fuberidazole, ° benzophene (thiabendazole); 149027.doc -197- 201103430 ~ Others: ethaboxam, etridiazole, hymexazole and 2-(4-gas-phenyl)-N -[4-(3,4-Dimethoxy-phenyl)-isoxazol-5-yl]-2-prop-2-ynyloxy-acetamide; D) Heterocyclic compound-. Specific biting: fluazinam, pyrifenox, 3-[5-(4-gas-phenyl)-2,3-dimethyl-isoxazodin-3-yl] Bisidine, 3-[5-(4-indolyl-phenyl)-2,3-dimercapto-isoxazodin-3-yl]pyridinium, 2,3,5,6-tetra-gas- 4-sulfonyl-based. Bisidine, 3,4,5-tripyridine, 2,6-di-carbonitrile, N-(l-(5-bromo-3-a-pyridin-2-yl)-ethyl)-2,4 - Dichloronicotinium amide, N-[(5-bromo-3-chloro-pyridin-2-yl)-methyl]-2,4-diqi-nicotinium amide; D D class: performance. Bupirimate, cyprodinil, diflumetorim, fenarimol, ferimzone, mepanipyrim, gas Nitrapyrin), I benzene. Niarim〇l, pyrimethanil; - dispatching class: triforine; -° ratio B: seed dressing 17 (fenpiclonil), defensive ning (fludioxonil) • 琳琳类: adimorph (aldimorph), morphine (dodemorph), acetaminophen, fenpropimorph 'tridemorph'; - 派 ° class: benzene ore (fenpropidin); - dimethylimine: fluoroimid, iprodione, procymi done, konken [S1 149027.doc -198- 201103430 (vinclozolin); Non-aromatic 5-pentene heterocycle: „恶. fainoxad〇ne, quinamidone, fiutianii, octhilinone, acesulfame (pr〇benazole), 5-amino-2-isopropyl-3-oxooxy-4-o-tolyl-2,3-dihydro-pyrazole-1-thiocarboxylic acid S-sodium propyl S Purpose, - Others: acidified benzothiadiazole-S-decyl ester (acibenzolar_s_methyl), alpha azulbrom, azilzin, blasticidin-S, Captafol, captan "chinomethionat", "dazomet", "debacarb", diclomezine, difenzoquat, benzoic acid-sulfonate, fenoxanil, Folpet, 〇x〇linic acid, piperalin, proquinazid, pyroquilon, quinoxyfen, imidazolium Triazoxide), tricyclazole '2-butoxy-6-iodo-3-propyl benzo-4-one, 5-chloro-1-(4,6-dimethoxy-pyrimidine) 2-yl)-2-mercapto-1H-benzimidazole, 5-gas-7-(4-mercaptopiperidin-1-yl)-6-(2,4,6-trifluorophenyl)-[ 1,2,4]triazolo[1,5-&amp;]pyrimidine and 5-ethyl-6-octyl-[1,2,4]triazolo[l,5-a]pyrimidin-7- Base amine; E) urethane-thiocarbamate and dithioamino phthalate, ferbate, mancozeb, maneb, wei 149027.doc -199- 201103430 Metha, methasulphocarb, metiram, pr0pineb, thiram, zineb, thiram ( Zirarn); - Amino citrate: benthiavalicarb, diethofencarb, iprovalicarb, propamocarb, chlorfenapyr hydrochloride, vaiiphenal And N-(l-(l-(4-cyano-phenyl)ethanesulfonyl)-butan-2-yl)amino decanoic acid _ (4-fluorophenyl) ester; F) other active substances - Anthraquinones: sputum, dodine, tannin free test, guazatine, bismuth octanoic acid acetate, iminoctadine, gram heat triacetate, gram heat (alkylbenzene sulfonic acid) Salt); - Antibiotics: kasugamycin, kasugamycin hydrochloride, streptomycin, polyoxine, validamycin A; - nitrophenyl Derivatives: binapacryl, dinobuton, dinocap, sputum ester 〇1 such as 1^1-isopropyl, tetrakis nitrobenzene (tecnazen); organometallic compounds: three Fentin salts, such as triphenyltin sulphate, triphenyltin or fentin hydroxide; - sulfur-containing heterocyclic compounds: dithianon, rice stalk (isoprothiolane); - Institutional compounds: edifenphos, triethylphosphonic acid (fosetyl), triethylphosphonic acid (fosetyl-aluminum), propyl joy [S3 149027.doc -200- 201103430 pine (iprobenfos ), phosphorous acid and its salts, white pine (pyraz〇ph〇〇, tolclofos-methyl; - organochlorine compounds: chlorothalonil, dichlofluanid, dichlorophen ), I sulfsulfamide, hexa-benzene, penced culron, pentachlorocyl and its salts, phthalide, quintozene, thiophanate-methyl, Tolylfluanid, N-(4-Gas-2-nitro-phenyl)-N-ethyl-4-mercapto-benzenesulfonamide; - Inorganic active substance: Bordeaux mixture , copper acetate, copper hydroxide, copper oxide, basic copper sulfate, sulfur; - other · biphenyl, bronopol, cyflufenamid, cymoxanil, diphenylamine , metrafenone, mildiomycin 'oxin-copper' Prohexadione-calcium, spiroxamine, tolylfluanid, N-(cyclopropylmethoxyimino)-(6-difluoro-decyloxy-2, 3-difluoro-phenyl)-indenyl)-2-phenylethylamine, N1-(4-(4·-gas-3-tris-methoxy-phenoxy)-2,5-diindole Base-stylethyl-N-methylformamidine, Ν-(4-(4-fluoro-3-trifluoromethyl-phenoxy)_2,5-dimethyl-phenyl)-indole- Ethyl-hydrazine-methylformamidine: ΝΓ-(2-methyl-5-trifluoromethyl-4-(3·tridecylfluorenyl-propoxy)-phenyl)-fluorene-ethyl -Ν-methylformamidine, Ν·-(5-difluoromethyl-2-indolyl-4-(3-trimethyldecyl-propoxy)-phenyl)-indole-ethyl-hydrazine -methyl hydrazine, 2-{1-[2-(5-methyl-3-trifluoromethyl-pyrazol-1-yl)-acetamidine 149027.doc -201 - 201103430 yl]-piperidine- 4-yl}-thiazole-4-decanoate-(1,2,3,4-tetrahydro-naphthalene-fluorenyl)-decylamine, 2-{1-[2-(5-methyl- 3-trifluoromethyl-pyrazol-1-yl)·ethinyl]-piperidin-4-yl}-thiazole-4-furoic acid methyl-(R)-l,2,3,4-tetra Hydrogen_naphthalen-1-yl-decylamine, acetic acid 6-t-butyl-8-fluoro-2,3-dimercaptoquinoline-4-yl ester and decyloxy-acetic acid 6-t-butyl - 8-Fluoro-2,3-dimercapto-indololin-4-yl ester. G) growth regulators abscisic acid, amidochlor, ancymidol, 6-benzylamine hydrazine, brassinolide, butralin, gramme (chlormequat) (chlormequat chloride), choline chloride, cyclanilide, diced, daminozide, dikegulac, ° plug Dimethipin, 2,6-dimercapto ratio bite, ethephon flumetralin, flurprimidol, fluthiacet, chlorpyrifos (forchlorfenuron) ), gibberellic acid, inabenfide, indole-3-acetic acid, maleic hydrazide, mefluidide, mepiquat (strong cotton chloride), naphthaleneacetic acid, N-6-benzyl adenine, bucksin, cyclamate (calcium cyclate), propyl jasmonate (prohydrojasmon), ° thidiazuron, Triapenthenol, tributyltrithiophosphate, 2,3,5-triiodobenzoic acid, trinexapac-ethyl and dilute °Sit; [S1 149027.doc -202- 201103430 Η) Herbicide - Acetone: acetochlor, alachlor, butachlor, dimethachlor, Dimethenamid, flufenacet, mefenacet, metolachlor, metazachlor, naphthylamine (napropamide), naproanilide, pethoxamid, pretilachlor, propachlor, thenylchlor; - amino acid derivatives: bilapia Bilanafos), glyphosate, glufosinate, sulfosate; - aryloxyphenoxypropionates: clodinafop, cyhalofop-butyl ), ° 恶 ° sitting on the grass fenoxaprop (fenoxaprop), mouth than fluazifop (fluazifop), ° than haloxyfop (haloxyfop). Metaamifop, propaquizafop, quizalofop, quizalofop-P-tefuryl; - ratio of 11 to 11: diquat (diquat) ), paraquat; -(thio)amino phthalate: asulam, butarate, carbeamide, desmedipham, peltani (dimepiperate), eptam (EPTC), esprocarb, molinate, orbencarb, phenmedipham, prosulfocarb, valerian 149027.doc -203 - 201103430 (pyributicarb), thiobencarb, triallate; - cycloheximide: butroxydim, clethodim, ringworm Cycloxydim), profoxydim, sethoxydim, tepraloxydim, tralkoxydim; - dibasic aniline · benfluralin, ethylene butene Ethalfluralin, oryzalin, pendimethalin, prodiamine, trifluralin Ifluralin); - Diphenyl mystery: acifluorfen, aclifen, bifenox, diclofop, ethoxyfen, flunarizine Fomesafen, lactofen, oxyfluorfen; - benzoquinones: bomoxynil, dichlobenil, terpene ; - 咪 ° sitin ketone · · p rice vinegar (imazamethabenz), imazamox (imazamox), azomic acid (imazapic), imazapyr (imazapyr), imazaquin (imazaquin) ,. Imazethapyr; - phenoxyacetic acid: clomeprop, 2,4-dichlorophenoxyacetic acid (2,4-D), 2,4-DB, dichlorprop , MCPA, MCPA-thioethyl, MCPB, 2-曱-4-chloropropionic acid (Mecoprop); -° ratio: chloridazon, flufenpyr-ethyl, °乙草斯的(fluthiacet), 禾草敏

E SI 149027.doc -204- 201103430 (norflurazon)、唾草特(pyridate); -。比D定類:氯胺°比咬酸(aminopyralid)、畢克草 (clopyralid)、。比氟草胺(diflufenican)、氟硫草定 (dithiopyr) ' It °定草酮(Huriclone) 、 It 草煙 (fluroxypyr)、毒赛定(picloram)、氟 °比草胺 (picolinafen)、°塞草咬(thiazopyr); - 石黃醢脲類:醯°密續隆(amidosulfuron)、四吐痛續隆 (azimsulfuron)、苄&quot;密績隆(bensulfuron)、乙基氯《•密橫 隆(chlorimuron-ethyl)、氣績隆(chlorsulfuron)、喊罐隆 (cinosulfuron)、環丙 °密績隆(cyclosu+lfamuron)、乙氧密 石黃隆(ethoxysulfuron)、°密咬石黃隆(flazasulfuron)、氣口比 石黃隆(flvicetosulfuron)、氟_ 咬嘴續隆(flupyrsulfuron)、 曱酿喷石黃隆(foramsulfuron)、 氯°比醚績隆 (halosulfuron)、〇坐 〇比嘴績隆(imazosulfuron)、換曱續 隆(iodosulfuron)、甲績胺續隆(mesosulfuron)、甲基曱 石黃隆(metsulfuron-methyl)、煙 °密績隆(nicosulfuron)、 環氧 β密石黃隆(oxasulfuron)、氟 °密續隆(primisulfuron)、 氟石黃隆(prosulfuron)、D比嘴續隆(pyrazosulfuron)、礙0密 續隆(rimsulfuron)、曱口密石黃隆(sulfometuron)、續0密續 隆(sulfosulfuron)、°塞吩續隆(thifensulfuron)、鍵苯績 隆(triasulfuron)、苯確隆(tribenuron)、三氟咬確隆 (trifloxysulfuron)、氟胺石黃隆(triflusulfuron)、三氟曱 石黃隆(tritosulfuron)、1-((2-氯-6-丙基-咪。坐并[l,2-b]噠 嗪-3-基)磺醯基)-3-(4,6-二甲氧基-嘧啶-2-基)脲; 149027.doc -205 - 201103430 - 三唤類:莠滅淨(ametryn)、莠去津(atrazine)、氰草津 (cyanazine)、異戊乙淨(dimethametryn)、乙嗪草酿| (ethiozin)、六 °秦同(hexazinone)、笨0秦草酿I (metamitron)、赛克津(metribuzin)、撲草淨 (prometryn)、西瑪津(simazine)、特 丁津 (terbuthylazine)、特丁淨(terbutryn)、三喚敦草胺 (triaziflam); - 脲類:綠麥隆(chlorotoluron)、殺草隆(daimuron)、敵 草隆(diuron)、伏草隆(fluometuron)、 異丙隆’ (isoproturon)、利榖隆(linuron)、甲苯 D塞隆 (methabenzthiazuron)、丁 口塞隆(tebuthiuron); - 其他乙醯乳酸合成酶抑制劑:雙草醚-鈉(bispyribac-sodium) '曱基氣自旨石黃草胺(cloransulam-methyl)、雙氣 績草胺(diclosulam)、雙氣續草胺(florasulam)、氣酮續 隆(flucarbazone)、β坐嘯確草胺(flumetsulam)、確草0坐 胺(metosulam)、嘲苯胺罐隆(ortho-sulfamuron)、五氟 績草胺(penoxsulam)、丙氧績隆(propoxycarbazone)、 丙醋草鍵(pyribambenz-propyl)、嘴咬肪草謎 (pyribenzoxim)、環酯草趟(pyriftalid)、曱基0^ 草醚 (pyriminobac-methyl)、喊沙泛(pyrimisulfan)、嘴硫草 醚(pyrithiobac)、普羅蘇芬(pyroxasulfone)、曱氧石黃草 胺(pyroxsulam); - 其他:胺°圭草_ (amicarbazone)、胺基三°坐、莎稗構 (anilofos)、氣丁醯草胺(beflubutamid)、草除靈乙醋E SI 149027.doc -204- 201103430 (norflurazon), pyridate (pyridate); Compared with D: chloramine ° than amino acid (aminopyralid), clopyralid (clopyralid). Diflufenican, dithiopyr 'It °Hurclone, It's fluroxypyr, picloram, picolinafen, ° Straw (thiazopyr); - scutellaria 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 ami ami ami ami ami ami ami ami ami ami ami Ethyl), chlorsulfuron, cinosulfuron, cyclosu+lfamuron, ethoxysulfuron, flazasulfuron, vent Flvicetosulfuron, fluorine_flupyrsulfuron, foramsulfuron, halosulfuron, halosulfuron, imazosulfuron Iotosulfuron, mesosulfuron, metsulfuron-methyl, nicosulfuron, oxasulfuron, fluorine Primisulfuron, fluorite yellow, prosulfuron, D Pyrazosulfuron, rimsulfuron, sulfometuron, sulfosulfuron, thifensulfuron, triasulfuron, Tribenuron, trifloxysulfuron, triflusulfuron, tritosulfuron, 1-((2-chloro-6-propyl-mi). And [l,2-b]pyridazin-3-yl)sulfonyl)-3-(4,6-dimethoxy-pyrimidin-2-yl)urea; 149027.doc -205 - 201103430 - III Calling class: ametryn, atrazine, cyanazine, dimethametryn, thiazinine, (ethiozin), hexazinone, stupid 0 Immamitron, metribuzin, prometryn, simazine, terbuthylazine, terbutryn, triaziflam ) - Urea: chlorotoluron, daimuron, diuron, fluometuron, isoproturon, linuron Toluene D-sialon (methabenzthiazuron), tebuthiuron; - other acetamidine lactate synthase inhibitor: bispyribac-sodium 曱 气 气 clo clo clo clo clo clo clo ), diclosulam, florasulam, flucarbazone, flumetsulam, metosulam, benzylamine tank Ortho-sulfamuron, penoxsulam, propoxycarbazone, pyribambenz-propyl, pyribenzoxim, pyrifalid , pyridylbac-methyl, pyrimisulfan, pyrithiobac, pyroxasulfone, pyroxsulam; - other: amine °圭草_ _ (amicarbazone), amine-based three-degree sitting, anthonyfoss (anilofos), flubendiamide (beflubutamid), herbicide vinegar

[SI 149027.doc -206- 201103430 (benazolin)、苯卡巴腙(bencarbazone)、°夫草石黃 (benfluresate)、。比草 g同(benzofenap)、苯達松 (bentazone)、苯雙 ο塞隆(benzobi.cyclon)、除草定 (bromacil)、;臭丁 酿草胺(br〇mobutide)、氣丙。密草醋 (butafenacil)、抑草磷(butamifos) '唑草胺 (cafenstrole)、唾酮草酿(carfentrazone)、°引 α朵酮草酉旨 (cinidon-ethlyl)、敵草索(chl〇rthal)、環庚草醚 (cinmethylin)、可滅蹤(clomazone)、苄草隆 (cumyluron)、噻普磺醯胺(Cyprosulfaniide)、麥草畏 (dicamba)、苯敵快(difenzoquat)、二氟。比隆 (diflufenzopyr)、稗内臍蠕孢菌(Drechslera monoceras)、 草哆嘴(endothal)、 乙0夫草石黃 (ethofumesate)、乙氧苯草胺(etobenzanid)、四。坐酸草 胺(fentrazamide)、戊基氟胺草醋(flumiclorac-pentyl)、 丙炔氟草胺(flumioxazin)、氟胺草唾(flupoxam)、氟洛 草酮(flurochloridone)、。夫草酮(flurtamone)、茚草酮 (indanofan)、異。惡草胺(isoxaben)、異°惡。坐草酮 (isoxaflutole)、環草定(lenacil)、敵裨(propanil)、戊快 草胺(propyzamide)、二氯啥嚇·酸(quinclorac)、喧草酸 (quinmerac)、甲基續草酮(mesotrione)、曱基胂酸、萘 草胺(naptalam)、丙炔β惡草酮(oxadiargyl)、°惡草酮 (oxadiazon)、°惡嗪草酮(oxazic丨omefone)、環戊°惡草酉同 (pentoxazone) .、a坐淋草酯(pinoxaden)、雙吐草腈 (卩7^〇1〇1^1)、乙基°比草醚(卩}^3£11^611-6化)^1)、°比續托利 149027.doc -207- 201103430 (pyrasulfotole)、节草。坐(pyrazoxyfen)、比拉 〇坐諾 (pyrazolynate)、滅蒸酿(quinoclamine)、痛咬月亏草醚 (saflufenacil)、續草酿j (sulcotrione)、曱石夤草胺 (sulfentrazone)、特草定(terbacil)、特伏曲酮 (tefuryltrione)、替莫曲酮(tembotrione)、°塞吩卡巴腙 (thiencarbazone)、拓普美膝(topramezone)、4-^. -3- [2-(2-曱氧基-乙氧基曱基)-6-三氟曱基-η比啶-3-羰基]- 雙環[3.2.1]辛-3-烯-2-酮、(3-[2-氣-4-氟-5-(3-甲基 _2,6_ 二側氧基-4-三氟曱基-3,6-二氫-2H-嘧啶-1-基)-苯氧 基]-吡啶-2-基氧基)-乙酸乙酯、6-胺基-5-氯-2-環丙基_ 嘧啶-4-甲酸甲酯、6-氯-3-(2-環丙基-6-曱基-苯氧基)_ 噠嗪-4-醇、4-胺基-3-氣-6-(4-氯-苯基)-5-氟-吡啶-2-曱 酸、4 -胺基-3-氣- 6- (4 -氣-2-說-3-曱氧基-苯基)-«·比〇定_2~ 甲酸甲酯及4-胺基-3-氣-6-(4-氣-3-二曱基胺基-2-氟-苯 基)-吡啶-2-曱酸曱酯。 I)殺蟲劑 - 有機(硫代)破酸鹽類:歐殺松(acephate)、曱基°比咬石粦 (azamethiphos)、曱基穀硫石粦(azinphos-methyl)、毒死 蜱(chlorpyrifos)、曱基毒死蜱(chlorpyrifos-methyl)、 氯芬碌(chlorfenvinphos)、二。秦農(diazinon)、敵敵畏 (dichlorvos)、百治麟(dicrotophos)、大滅松 (dimethoate)、二硫松(disulfoton)、愛殺松(ethion)、撲 滅松(fenitrothion)、芬殺松(fenthion)、加福松 (isoxathion)、馬拉松(malathion)、達馬松 [S] 149027.doc •208 - 201103430 (methamidophos)、滅大松(methidathion)、甲基巴拉松 (methyl-parathion)、美文松(mevinphos)、亞素靈 (monocrotophos)、滅多松(oxydemeton-methyl)、巴拉 奥克松(paraoxon)、巴拉松(parathion)、赛達松 (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); - 胺基甲酸酯類: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)、芬諾克 (fenoxycarb)、呋線威(furathiocarb)、滅蟲威 (methiocarb)、納乃得(methomyl) ' 歐殺滅(oxamyl)、 抗蚜威(pirimicarb)、殘殺威(propoxur)、硫雙威 (thiodicarb)、唑蚜威(triazamate); - 擬除蟲菊酯:丙烯除蟲菊(allethrin)、畢芬寧 (bifenthrin)、賽扶寧(cyfluthrin)、赛洛寧 (cyhalothrin)、賽酚寧(cyPhenothrin)、赛滅寧 (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 149027.doc • 209- 201103430 (fenpropathrin)、芬化利(fenvalerate)、依普寧 (imiprothrin)、λ-赛洛寧(iarnbda-cyhalothrin)、百滅寧 (permethrin)、普亞列寧(pranethrin)、除蟲菊精 (pyrethrin)I及II、異列滅寧(resrnethrin)、氣石夕菊醋 (silafluofen)、τ-福化利(tau_fiuvalinate)、七敗菊酉旨 (tefluthrin)、四曱司林(tetramethrin)、泰滅寧 (tralomethrin)、拜富寧(transfiuthrin)、丙 IL 菊酉旨 (profluthrin)、四氟曱醚菊酯(dimefluthrin); -昆蟲生長調節劑:a)甲殼素合成抑制劑:苯甲醯基脲 (benzoylureas).克福隆(chi〇rfiuazuron)、赛滅淨 (cyramazin) 一 福隆(diflubenzuron)、福環脈 (flucycloxuron)、敦芬隆(nufen〇xur〇n)、六伏隆 (hexaflumuron)、祿芬隆(lufenuron)、諾瓦隆 (novaluron)、付福隆(teflubenzuron) 、三 福隆 (triflumuron),布芬淨(buprofezin)、笨蟲驗 (diofenolan)、合赛多(hexythiazox)、依殺蜗 (etoxazole)、克务蜗(ei〇fentazjne) ; b)蜆皮激素抄抗 劑.合务隆 (halofenozide)、 滅芬嗜 (methoxyfenozide)、得芬諾(tebufen〇zide)、印楝素 (azadirachtin) ; c)保幼激素類似物:百利普芬 (pyriproxyfen)、美賜平(meth〇prene)、芬諾克;勾脂質 生物合成抑制劑.螺蜗酉旨(Spir〇diclofen)、螺曱蜗酉旨 (spiromesifen) ' 螺蟲乙 g旨(Spir〇tetramat); - 菸鹼樣受體促效藥/拮抗劑化合物:可尼丁 149027.doc •210· 201103430 (clothianidin) 、 11夫蟲胺(dinotefuran)、益達胺 (imidacloprid)、α塞蟲嗓(thiamethoxam)、稀 σ定蟲胺 (nitenpyram) 、 β定蟲脉(acetamiprid) 、 °塞蟲琳 (thiacloprid)、1-(2 -氣-〇塞唾-5-基曱基)-2 -石肖基亞胺基_ 3,5-二甲基-[1,3,5]三嗪; -GABA括抗劑化合物: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-l-(2,6 -二氣-4-甲基-苯基)-4-胺亞續酿基-1 Η - °比唾-3 -硫代 甲酸醯胺; - 大環内酯殺蟲劑: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:亞酉昆瞒(acequinocyl)、福希普 (fluacyprim)、伏礒腙(hydramethylnon); - 解偶聯劑:蟲蜗腈(chlorfenapyr); - 氧化碌酸化抑制劑:環己錫(cyhexatin)、汰芬隆 (diafenthiuron)、' 芬布賜(fenbutatin oxide)、跋瞒多 (propargite); 149027.doc -211 · 201103430 - 蛻皮破裂劑化合物:賽滅淨(cryomazine); - 混合功能氧化酶抑制劑:胡椒基丁醚(piperonyl butoxide); - 鈉通道阻斷劑:茚蟲威(indoxacarb)、美氟膝 (metaflumizone); - 其他:本克°塞(benclothiaz)、畢芬載(bifenazate)、殺琪 丹(cartap)、 氣尼胺(flonicamid)、咬蟲丙醚 (pyridalyl).、派滅淨(pymetrozine)、硫、硫賜安 (thiocyclam)、福本胺(flubendiamide)、氯鄰胺基苯曱 普(chlorantraniliprole)、 魚尼汀受體抑制劑 (cyazypyr,HGW86)、塞諾 °比芬(cyenopyrafen)、°比氣 硫峨(flupyrazofos)、噻氟美芬(cyflumetofen)、醯胺氟 美(amidoflumet)、咪克芬(imicyafos)、雙三氟蟲脲 (1^1;1^1111*〇11)及 °比氟嗤腙(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1)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、π及/或 IV及至少一種來自如上所述之群八)至〇之殺真菌劑的混合 物對抗有害真菌比以個別化合物j、π或1¥或來自群Α)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 149027.doc •212- 201103430 1、π及/或IV連同至少一種來自群…至^之活性物質,可獲 〜協同放應,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I、II及/或IV連同至少另一種 活性物質應理解為表示至少一種式卜Η及/或…之化合物 及至少另-種活性物質以殺真菌有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,諸如受感染植 物植物%殖材料(尤其種子)、表面、材料或土壞以及經 保護以免受真菌侵襲之植物、植物繁殖材料(尤其種子)、 土壌、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〖、π&amp;/4ΐν及至 J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 性物質之時仍以足夠量出現在作用點。施用順序對本發明 之實施並不重要。 在二凡混合物(亦即包含一種化合物[、卩或〗^(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)中’組们與組份2之重量比—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10:1之範圍内且尤其在^至夂丨之範圍内。 在三元混合物(亦即包含一種化合(組份1}及第一其他 活性物質(組份2)及第二其他活性物質(組份3)(例如,來自 群A)至I)之兩種活性物質)的本發明組合物)中,組份1與組 149027.doc -213· 201103430 份2之重量比視所用活性物質之性質而定,較佳在1:5 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1:5〇至5〇:1之範圍内且尤其在1:1〇至 10:1之範圍内。 5亥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组合組合物(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—起或預調配。在套組中提供兩種以」 組份之彼等實施例中,可將組份合併在一起,因而包裝方 單個容器(諸如小瓶、瓶子、罐子、小袋、袋子或小罐 中。在其他實施例中,可分別包裝套組之兩種或兩種以」 伤’亦即不進行預調配。因而,套組可包括一或多個為 獨=谷②’諸如小舨、罐子、瓶子、小袋、袋子或小罐, 各谷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—起施心 作為用於製備本發明組合物的本發明組合組合物之組份3} 施用。 、背負式喷霧器、喷淋槽或噴 。此處’以水及/或緩衝液使 需施用濃度,適當時可能添加 使用者通常由預劑量裝置 灑飛機來施用本發明組合物 農用化學紐合物補足達到所 t S1 149027.doc -214- 201103430 2他助劑’由此獲得本發明之即用型噴灑液或農用化學組 口物通吊,每公頃農業有效面積施用50至500公升即用 型喷灑液,較佳100至400公升。 根據一實施例,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 之卩刀)且(右適當)可添加其他助劑(槽内混合)。 在另一實施例中,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Ϊ、 Π及/或IV及/或來自群A)至〗)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组份或部分預混合組份(例 如,包含化合物I、^及/或1¥及/或來自群⑷至^之活性物 質的組份)。 亦权佳為包含化合物I、/或IV(組份i)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 及聘菌醋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、異吡贊、甲霜靈、呋醯胺、達 滅芬、氟嗎啉、氟吼菌胺(匹克苯甲咪)、氣苯醯胺、加普 胺、雙炔醯菌胺(mandipropamid)及义(3,,4,,5,-三氟聯笨-2-基)-3-二氟曱基-1-曱基_1H-叱唑-4-曱醯胺的活性物質之混 149027.doc -215- 201103430 合物。 較佳為包含式I、Π及/或IV之化合物(組份1)及至少一種 選自群C)之哇類(組份2)且尤其選自環克唑、苯醚曱環唑、 氟環唑、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、氟醚唑、環菌唑、撲克拉、赛座滅、苯菌靈、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/或以(組份丨)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 f、嗎菌靈 '粉鏽淋、十三嗎琳、笨鏽咬、依普同、免克 寧、噁唑菌酮、咪唑菌酮、噻菌靈、普奎那茲、酸化苯并 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]三唑幷[15-a]嘧啶_7_基胺的活性物質之 混合物。 亦較佳為包含化合物I、Π及/或1¥(組份1}及至少—種選 自群E)之胺基甲酸酯(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1¥(組份丨)及至少—種選 自群F)令給出之殺真菌劑(組份2)且尤其選自腈硫醌、二〜 —本 錫鹽(諸如三苯醋錫)、三乙膦酸、三乙膦酸鋁、Hjo及 其鹽、百菌清、益發靈、甲基多保淨、乙酸銅、氫氣化 銅、氯氧化銅、硫酸銅、硫、霜脲氰、美曲芬諾及螺枣菌 [S] 149027.doc •216· 201103430 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、II及/或IV(組份 1)及另一活性物質(組份2)之組合物,該另一活性物質係選 自表C之C-1至C-346列之「組份2」行。 另一實施例係關於表C中所列之組合物C-1至C-346,其 中表C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及/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C :包含一種個別化化合物I、II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 C-1 一種個別化化合物I、II或IV 亞托敏 C-2 一種個別化化合物I、II或IV 地莫菌胺 C-3 一種個別化化合物I、II或IV 烯肟菌酯 C-4 一種個別化化合物I、II或IV 氟氧菌胺 C-5 一種個別化化合物I、II或IV 克收欣 C-6 一種個別化化合物I、II或IV 苯氧菌胺 C-7 一種個別化化合物I、II或IV 奥瑞菌胺 C-8 一種個別化化合物I、II或IV 啶氧菌胺 C-9 一種個別化化合物I、II或IV 百克敏 C-10 一種個別化化合物I、II或IV η比瑞苯卡 C-11 一種個別化化合物I、II或IV 三氟敏 C-12 一種個別化化合物I、II或IV 2-(2-(6-(3-氯-2-曱基-苯氧基)-5-氟-嘧 。定-4-基氧基)-苯基)-2-甲氧基亞胺基~N-甲基-乙醯胺 C-13 一種個別化化合物I、II或IV 2-(鄰-((2,5-二曱基苯基-氧亞曱基)笨 基)-3 -甲氧基-丙稀酸(acrylsSure)甲6旨 149027.doc -217- 201103430 混合物 組份1 組份2 ~ C-14 一種個別化化合物I、II或IV 3-甲氧基-2-(2-(Ν-(4·甲氧基-笨基 烷曱醯亞胺基硫基甲基)-苯基)·丙歸酸 曱酯 C-15 一種個別化化合物I、II或IV 2-(2-(3-(2,6-二氯苯基)-1-曱基-亞稀丙 基胺基氧基甲基)-苯基)-2-甲氧基亞胺 基·Ν·甲基·乙酿胺 C-16 一種個別化化合物I、II或IV 苯霜靈 C-17 一種個別化化合物I、II或IV 苯霜靈-Μ C-18 一種個別化化合物I、II或IV 麥鏽靈 C-19 一種個別化化合物I、II或rv 必殺吩 C-20 一種個別化化合物I、II或IV 博克利 C-21 一種個別化化合物I、II或IV 萎鏽靈 C-22 一種個別化化合物I、II或IV 曱呋醯胺 C-23 一種個別化化合物I、Π或IV 環醯菌胺 C-24 一種個別化化合物I、II或IV 氟多寧 C-25 一種個別化化合物I、II或IV 福拉比 C-26 一種個別化化合物I、II或rv 異0比贊 C-27 一種個別化化合物I、Π或IV 異噻菌胺 C-28 一種個別化化合物I、II或IV 克拉昔 C-29 一種個別化化合物I、II或IV 滅鏽胺 C-30 一種個別化化合物I、II或rv 滅達樂 C-31 一種個別化化合物I、Π或IV 滅達樂-Μ C-32 一種個別化化合物I、II或IV 呋醯胺 C-33 一種個別化化合物I、II或rv 歐殺斯 C-34 一種個別化化合物I、II或IV 氧化萎鏽靈 C-35 一種個別化化合物I、II或IV 吡噻菌胺 C-36 一種個別化化合物I、II或IV 森達先 C-37 一種個別化化合物I、II或rv 克枯爛 C-38 一種個別化化合物I、II或IV 赛氟滅 C-39 一種個別化化合物I、II或IV 汰敵寧 C-40 一種個別化化合物I、Π或IV 2·胺基-4-曱基塞嗤-5·曱醯苯胺 149027.doc -218- [si 201103430[SI 149027.doc -206- 201103430 (benazolin), bencarbazone, benfluresate, benfluresate. More than benzofenap, bentazone, benzobi.cyclon, bromacil, bromo mobutide, aerobic. Butafenacil, butamifos, cafenstrole, carfentrazone, cinidon-ethlyl, enemies (chl〇rthal) ), cinmethylin, clomazone, cumyluron, cyprosulfaniide, dicamba, difenzoquat, difluoro. Diflufenzopyr, Drechslera monoceras, endothal, ethofumesate, etobenzanid, IV. Sitting on fentrazamide, flumiclorac-pentyl, flumioxazin, flupoxam, flurochloridone. Flurtamone, indanofan, and different. Isoxaben, heterosexual. Isoxaflutole, lenacil, propanil, propyzamide, quinclorac, quinmerac, methyl oxaloacetone Mesotrione), mercaptoic acid, naptalam, acetylene beta oxadiargyl, oxadiazon, oxazic丨omefone, cyclopentazone With (pentoxazone), a sitpox (pinoxaden), bisoxaquinonitrile (卩7^〇1〇1^1), ethyl ° 草 草 ether (卩}^3£11^611-6) ^1), ° than continued Toli 149027.doc -207- 201103430 (pyrasulfotole), grass. Pyrazoxyfen, pyrazoonate, quinoclamine, saflufenacil, sulcotrione, sulfentrazone, special grass Terbacil, tefuryltrione, tembotrione, thiencarbazone, topramezone, 4-^. -3- [2-(2 -methoxy-ethoxymethyl)-6-trifluoromethyl-n-pyridyl-3-carbonyl]-bicyclo[3.2.1]oct-3-en-2-one, (3-[2- Gas 4-fluoro-5-(3-methyl-2,6-di-oxo-4-trifluoromethyl-3,6-dihydro-2H-pyrimidin-1-yl)-phenoxy]- Pyridin-2-yloxy)-ethyl acetate, 6-amino-5-chloro-2-cyclopropyl-pyrimidine-4-carboxylic acid methyl ester, 6-chloro-3-(2-cyclopropyl-6 -mercapto-phenoxy)-pyridazin-4-ol, 4-amino-3-gas-6-(4-chloro-phenyl)-5-fluoro-pyridine-2-decanoic acid, 4-amine Base-3-gas-6-(4- gas-2-say-3-methoxy-phenyl)-«·比〇定_2~ methyl formate and 4-amino-3-gas-6- (4-Gas-3-didecylamino-2-fluoro-phenyl)-pyridine-2-decanoate. I) Insecticides - Organic (thio) salts: acephate, azamethiphos, azinphos-methyl, chlorpyrifos , chlorpyrifos-methyl, chlorfenvinphos, two. Diazinon, dichlorvos, dicrotophos, dimethoate, disulfoton, ethion, fenitrothion, fenthion ), isoxathion, malathion, damasson [S] 149027.doc •208 - 201103430 (methamidophos), methadinion, methyl-parathion, meson pine Mevinphos), monocrotophos, oxydemeton-methyl, paraoxon, parathion, phenthoate, phosalone, benefit Phosmet, phosphamidon, phorate, phoxim 'pirimiphos-methyl, profenofos prothiofos, killer ( Sulprophos), tetrachlorvinphos, terbufos, triazophos, trichlorfon; - urethanes: alanycarb, aldicarb , bendicarb (bendiocarb), free gram (benfuracar b), carbaryl, carbofuran, carbosulfan, fenoxycarb, furathiocarb, meticarb, nanet ( Methomyl) 'oxamyl, anti-pirimicarb, propoxur, thiodicarb, triazamate; - pyrethroid: pyrethrum (allethrin) ), bifenthrin, cyfluthrin, cyhalothrin, cyPhenothrin, cypermethrin, α-赛灭宁, β_赛灭宁, ζ_赛Zeta-cypermethrin, deltamethrin, esfenvalerate, etofenProx, fenpenin 149027.doc • 209- 201103430 (fenpropathrin), fenvalerate, fen Imiprothrin, iarnbda-cyhalothrin, permethrin, pranethrin, pyrethrin I and II, resrnethrin, gas Silafluofen, tau_fiuvalinate, and tefluthr In), tetramethrin, trolomethrin, transfiuthrin, pro-IL-profluthrin, dimefluthrin; - insect growth regulator: a) Chitin synthesis inhibitors: benzoylureas. Chi〇rfiuazuron, cyramazin, diflubenzuron, flucycloxuron, Dunferon ( Nufen〇xur〇n), hexaflumuron, lufenuron, novaluron, teflubenzuron, triflumuron, buprofezin, stupid Insect test (diofenolan), hexythiazox, etoxazole, ei〇fentazjne; b) ecdysone retinoic acid agent. haofofozide, methoxyfenozide ), tebufen〇zide, azadirachtin; c) juvenile hormone analogues: pyriproxyfen, meth〇prene, fenolect; Synthetic inhibitors. Spir〇diclofen, spiromesifen 'spiders B g(Spir〇tetramat); - nicotinic receptor agonist/antagonist compound: cotinine 149027.doc •210· 201103430 (clothianidin), 11 dinotefuran, imidacloprid , thiamethoxam, nitenpyram, acetamiprid, thiacloprid, 1-(2-gas-pyrene-5-yl fluorenyl) -2 - schlossylidene _ 3,5-dimethyl-[1,3,5]triazine; -GABA inhibitor compound: endosulfan, ethiprole, fenapini (fipronil), vaniliprole, pyrafluprole, pyriprole, 5-amino-l-(2,6-dioxa-4-methyl-phenyl)-4 - Amines - 1 - 比 - ° than salivation - 3 - thioglycolate; - Macrolides: aba, ab (abamectin), emmeectin (ememectin), metostatin (milbemectin), lepimectin, spinosad, spinetoram; - mitochondrial electron transport inhibitor (METI) I acaricide: fenazaquin (pyridaben), defenfen (tebufenpyrad), off Tolfenpyrad, flufenerim; -METI II and III compounds: acequinocyl, fluacyprim, hydramethylnon; - uncoupling agent: worm Nitroxide (chlorfenapyr); - oxidative acidification inhibitors: cyhexatin, diafenthiuron, 'fenbutatin oxide, propargite; 149027.doc -211 · 201103430 - Clay rupture agent compound: cryomazine; - mixed functional oxidase inhibitor: piperonyl butoxide; - sodium channel blocker: indoxacarb, metaflumizone; - Others: Benclothiaz, bifenazate, cartap, flonicamid, pyridalyl, pymetrozine, sulfur, Thiocyclam, flubendiamide, chlorantraniliprole, chlorinated receptor inhibitor (cyazypyr, HGW86), cyenopyrafen, ° sulphur Flupyrazofos, cyflumetofe n), amidoxime (amidoflumet), imicyafos, imipenem (1^1; 1^1111*〇11) and °pyrfluquinazon. The invention further relates to an agrochemical composition comprising at least one compound I, II and/or IV (component 1) and at least one other active substance suitable for plant protection (for example selected from group 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 solvent or mixture of 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, a mixture of compounds I, π and/or IV and at least one fungicide from group VIII) to cockroaches as described above against harmful fungi than individual compounds j, π or 1 ¥ or from group Α to F Individual fungicides are more effective against their fungi. By applying the compound 149027.doc •212-201103430 1, π and/or IV together with at least one active substance from the group ... to ^, a synergistic ration can be obtained, that is, a simple phase obtained not only by individual effects Add (collaboration mixture). According to the invention, the administration of the compounds I, II and/or IV together with at least one further active substance is understood to mean that at least one compound of the formula and/or ... and at least one further active substance are present simultaneously in a fungicidal effective amount. Point (ie, 'a harmful fungus that is controlled or its habitat, such as infected plants, % of materials (especially seeds), surfaces, materials or soil damage, and plants, plant propagation materials that are protected from fungal attack (especially Seed), bandits, surfaces, materials or rooms). This can be done by simultaneously (in combination (for example in the form of a mixed formulation in the tank) or separately) or by the continuous application of the compound [, π &amp; /4ΐν and to the other active substance, the time interval between the individual applications in # The choice is made to ensure that the active substance applied first occurs at a point of action in a sufficient amount when the other active substance is applied. The order of administration is not critical to the practice of the invention. In a mixture of the invention (ie, a composition of the invention comprising a compound [, hydrazine or hydrazine (component 1) and another active substance (component 2) (eg, active material from group VIII (4))) 'The weight ratio of the group to the 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 It is more preferably in the range of 1:10 to 10:1 and especially in the range of ^ to 在 in the range of 1:2 〇 to 2 〇:1. In a ternary mixture (ie, comprising one compound (component 1} and the first other active material (component 2) and a second other active material (component 3) (eg, from group A) to I) In the active substance) composition of the invention, the weight ratio of component 1 to group 149027.doc -213·201103430 part 2 depends on the nature of the active substance used, preferably in the range of 1:5 〇 to 50:1. Within the range of 1:10 to 10:1, and the weight of component 1 and component 3 is preferably in the range of 1:5〇 to 5〇:1 and especially in the range of 1:1〇 to 10: Within the scope of 1. The components such as 5H can be used individually or partially or completely mixed with each other to prepare the composition 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 in a pre- or pre-provisioning. In embodiments in which two components are provided in a kit, the components may be combined together so that the package is in a single container (such as a vial, bottle, can, pouch, bag or canister. In other implementations) In the example, two or two sets of packages may be separately packaged to "injury", that is, no pre-distribution may be performed. Thus, the kit may include one or more of two types such as a small bowl, a can, a bottle, a pouch. , bag or small can, each bar contains a separate component of the agrochemical composition. In both forms, the components of the kit can be separated from other components or together with other components - as a preparation for the preparation The composition of the composition of the invention of the composition of the invention 3} is applied, a knapsack sprayer, a spray tank or a spray. Here, the concentration to be applied is set with water and/or buffer, and a user may be added as appropriate. The ready-to-use spray or agrochemical group of the present invention is usually obtained by spraying a pre-dosing device onto the aircraft to apply the agrochemical compound of the composition of the present invention to make up the S_149027.doc-214-201103430 2 Hanging through the mouth, every hectare of agriculture has Applying 50 to 500 liters of ready-to-use spray fluid, preferably 100 to 400 liters. According to an embodiment, the individual components of the composition of the invention (such as a portion of a kit or A binary or ternary mixture of trowels) and (right appropriate) additional additives (in-tank mixing) may be added. In another embodiment, the individual components of the composition of the invention may be mixed by a user in a spray tank. Or a partially pre-mixed component (for example, a component comprising the compound Ϊ, Π and/or IV and/or from Group A) to ???) and (if appropriate) additional auxiliaries and additives may be added (in the tank) mixing). 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, ^, and/or 1 ¥ and / Or a component from the active substance of group (4) to ^). Also preferred is a compound I, / or IV (component i) and at least one selected from the group A) of esculine (component 2) and especially selected from the group consisting of atropine, tilmus, oxyfluoride A mixture of the active substances of bacteriocin, kexinxin, oriprozamide, oxystrobin, pyraclostrobin and vinegar. • It is also preferred to include compounds I, II and/or IV (component 1) and at least one carboxamide selected from group B) (component 2) and in particular selected from the group consisting of chlorhexidine, bokley, and sender , cycloheximide, chlorhexidine, isopyrazine, metalaxyl, furosemide, damiden, flumorph, flufenamide (p-benzophenone), benzophenone, gupamine, Mandipropamid and (3,4,5,-trifluorobi-2-yl)-3-difluoroindol-1-yl-1H-indazole-4-indole Mixture of active substances of guanamine 149027.doc -215-201103430. Preference is given to compounds comprising the formula I, hydrazine and/or IV (component 1) and at least one group selected from the group C) (component 2) and especially selected from the group consisting of cycloxazole, difenoconazole, fluorine Cycloazol, fluconazole, flucarbazole, dimethoate, meconazole, madridin, panconazole, propiconazole, propylthioglycol, trimethoate, three tailong, dekli, fluoride A mixture of active substances of ethiazole, cycloxazole, poker, cyanobacteria, benomyl, befenfen and ethipramine. Also preferably, it comprises a compound I, hydrazine and/or (component hydrazine) and at least one heterocyclic compound selected from group D) (component 2) and is especially selected from the group consisting of gibberidine, simboldine and fenremore. , 米潘尼比林, 比利美沙尼,赛福宁,护护f, 菌菌灵' powder rust, thirteen lin, stupid rust bite, yiputong, kekening, famoxadone, Imidazolone, thiabendazole, puquinaz, acidified benzothiadiazole-S-methyl ester, tetradone, fore, phlorin, vebufen and 5_ethyl-6-octyl- [1,2,4] A mixture of active substances of triazolium [15-a]pyrimidin-7-ylamine. Also preferred is a urethane comprising a compound I, hydrazine and/or 1 (component 1} and at least one selected from the group E) (component 2) and especially selected from the group consisting of mancozeb, dysen A mixture of active substances of hydrazine, propyl sulphate, thiram, carbendazim, phenthiali and propamocarb. It is also preferred to include the compound I, π and/or 1 ¥ (component 丨) and at least one selected from the group F) to give the fungicide (component 2) and especially selected from the group consisting of nitrile sulphide, two 〜 - Benxi salt (such as triphenyl vinegar), triethylphosphonic acid, aluminum triethylphosphinate, Hjo and its salts, chlorothalonil, Yifaling, methylpolybao, copper acetate, copper hydride, chlorine oxidation Copper, copper sulphate, sulphur, cymoxanil, mebendazole and snails [S] 149027.doc • 216· 201103430 A mixture of active substances of amines. Accordingly, the present invention is further directed to compositions comprising Compounds I, II and/or IV (Component 1) and another active substance (Component 2) selected from Table C, C-1 to The "Component 2" line listed in C-346. Another embodiment relates to compositions C-1 to C-346 listed in Table C, wherein one of the tables C corresponds in each case to a compound comprising an individualized formula I, II and/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 C: Composition mixture comprising an individual compound I, II or IV and another active substance from groups A) to I) Component 1 Component 2 C-1 An individualized compound I, II or IV MinC-2 An individualized compound I, II or IV Dimethoprim C-3 An individualized compound I, II or IV enestrobin C-4 An individualized compound I, II or IV fluoxetine C -5 an individualized compound I, II or IV kexin C-6 an individualized compound I, II or IV phenoxystrobin C-7 an individualized compound I, II or IV oriprosamine C-8 Individualized compound I, II or IV oxystrobin C-9 An individualized compound I, II or IV 100 g-sensitive C-10 an individualized compound I, II or IV η ribitola C-11 an individualized compound I, II or IV trifluoro-sensitive C-12 an individualized compound I, II or IV 2-(2-(6-(3-chloro-2-indolyl-phenoxy)-5-fluoro-pyrimidine -4-yloxy)-phenyl)-2-methoxyimino-N-methyl-acetamide C-13 An individualized compound I, II or IV 2-(o-((2, 5-dimercaptophenyl-oxoarhenyl)acyl-acrylic acid (acrylsSure) 6 149027.doc -217- 201103430 Mixture component 1 Component 2 ~ C-14 An individualized compound I, II or IV 3-methoxy-2-(2-(Ν-(4.methoxy)- Styloalkyl sulfoximine iminothiomethyl)-phenyl) propyl decyl C-15 An individualized compound I, II or IV 2-(2-(3-(2,6-dichloro) Phenyl)-1-fluorenyl-siallylaminooxymethyl)-phenyl)-2-methoxyiminoamine·Ν·methyl·ethnamine C-16 an individualized compound I , II or IV Benzophene C-17 An individualized compound I, II or IV phenhydryl-oxime C-18 An individualized compound I, II or IV Malacic C-19 An individualized compound I, II or Rv must kill C-20 An individualized compound I, II or IV Berkeley C-21 An individualized compound I, II or IV Rustone C-22 An individualized compound I, II or IV furosemide C- 23 An individualized compound I, hydrazine or IV Cyclosporin C-24 An individualized compound I, II or IV Fluorine C-25 An individualized compound I, II or IV Furabi C-26 An individualization Compound I, II or rv iso 0 to Z-27 An individualized compound I, guanidine or IV isothiazide C-28 An individualized compound I, II or IV Carrageen C-29 An individualized compound I, II or IV rust-killing amine C-30 An individualized compound I, II or rv Destroy C-31 An individualization Compound I, hydrazine or IV statin- Μ C-32 an individualized compound I, II or IV furosemide C-33 an individualized compound I, II or rv octopus C-34 an individualized compound I, II or IV oxidized rust rust C-35 An individualized compound I, II or IV pirfenamide C-36 An individualized compound I, II or IV Sentence C-37 An individualized compound I, II or rv克枯烂C-38 An individualized compound I, II or IV cyprofen C-39 An individualized compound I, II or IV steroidal C-40 An individualized compound I, hydrazine or IV 2 amine- 4-曱基塞嗤-5· anthranil 149027.doc -218- [si 201103430

混合物 組份1 組份2 C-41 一種個別化化合物I、Π或IV 2-氯二甲基·節滿-4-基)-於驗 醯胺 C-42 一種個別化化合物I、π或IV N-(3',4f,5 -二·氟聯本-2-基)-3-二氣甲基-卜甲基-1H-吡唑-4-曱醯胺 C-43 一種個別化化合物I、II或IV Ν-(4·-三氟曱基硫基聯笨-2-基)-3-二氟 甲基-1-曱基-1H-吡唑-4-曱醯胺 C-44 一種個別化化合物I、Π或IV N-(2-(l,3-二曱基-丁基)-苯基)-1,3-二甲 基-5-氟-1H-吡唑-4-甲醯胺 C-45 一種個別化化合物I、Π或IV N-(2-(l,3,3-三 f 基-丁基)-苯基)-i,3-二 甲基-5-氟-1H-吡唑-4-甲醯胺 C-46 一種個別化化合物I、II或IV 達滅芬 C-47 一種個別化化合物I、II或IV 氟嗎啉 C-48 一種個別化化合物I、II或IV 丁 &quot;比嗎淋 C-49 一種個別化化合物I、Π或IV 氟美醯胺 C-50 一種個別化化合物I、II或IV 氟°比菌胺 C-51 一種個別化化合物I、II或IV 氟吡胺 C-52 一種個別化化合物I、II或IV 氣苯醯胺 C-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-甲醯 基胺基-2-羥基-苯甲醯胺 C-54 一種個別化化合物I、II或IV 加普胺 C-55 一種個別化化合物I、II或IV 二氣西莫(dic.locymet) C-56 一種個別化化合物I、II或IV 雙炔醯菌胺 C-57 一種個別化化合物I、II或IV 土黴素 C-58 一種個別化化合物I、II或IV 妙硫分 C-59 一種個別化化合物I、II或IV N-(6-甲氧基-吡啶-3-基)環丙烷曱酸 醯胺 C-60 一種個別化化合物I、II或IV 阿紮康嗤 C-61 一種個別化化合物I、II或IV 比多農 C-62 一種個別化化奋物I、II或IV 溴克唾 C-63 一種個別化化合物I、II或IV 環克唑 C-64 一種個別化化合物I、II或IV 苯醚曱環唑 C-65 一種個別化化合物I、II或IV 二硝康唑 C-66 一種個別化化合物I、II或IV 二硝康唑-M 149027.doc •219- 201103430 混合物 組份1 組份2 C-67 一種個別化化合物I、II或IV 氣環β坐 C-68 一種個別化化合物I、II或IV 芬布康唑 C-69 一種個別化化合物I、Π或IV 氟奎康唑 C-70 一種個別化化合物I、II或IV 氟矽唑 C-71 一種個別化化合物I、Π或IV 護汰芬 C-72 一種個別化化合物I、II或IV 六康坐 C-73 一種個別化化合物I、Π或IV 亞胺D坐 C-74 一種個別化化合物I、II或IV 依普克。坐 C-75 一種個別化化合物I、π或IV 葉菌α坐 C-76 一種個別化化合物I、II或IV 麥環丁尼 C-77 一種個別化化合物I、Π或IV 嗯咪β坐 C-78 一種個別化化合物I、II或IV 巴克素 C-79 一種個別化化合物I、II或IV 潘康唑 C-80 一種個別化化合物I、II或IV 丙環唾 C-81 一種個別化化合物I、II或IV 丙硫醇克吐 C-82 一種個別化化合物I、II或IV 矽氟唑 C-83 一種個別化化合物I、II或IV 得克利 C-84 一種個別化化合物I、π或IV 氟醚唾 C-85 一種個別化化合物I、II或IV 三泰芬 C-86 一種個別化化合物I、Π或IV 三泰隆 C-87 一種個別化化合物I、II或IV 環菌°坐 C-88 一種個別化化合物I、II或IV 缔效°坐 C-89 一種個別化化合物I、II或IV Κ4-氣-苯基)-2-([1,2,4]三唑-1-基)-環 庚醇 C-90 一種個別化化合物I、II或IV 賽座滅 C-91 一種個別化化合物I、II或IV 依滅列 C-92 一種個別化化合物I、II或IV 依滅列硫酸鹽 C-93 一種個別化化合物I、II或IV 稻盘酯 C-94 一種個別化化合物I、II或IV 撲克拉 C-95 一種個別化化合物I、II或IV 赛福座 C-96 一種個別化化合物I、II或IV 苯菌靈 149027.doc •220· [si 201103430 混合物 組份1 組份2 C-97 —種個別化化合物I、II或IV 貝芬替 C-98 一種個別化化合物I、II或IV 麥穗靈 C-99 一種個別化化合物I、II或IV 噻苯咪唑 C-100 一種個別化化合物I、II或IV 乙噻博胺 C-101 一種個別化化合物I、II或IV 依得利 C-102 一種個別化化合物I、II或IV 噁黴靈 C-103 一種個別化化合物I、II或IV 2-(4-氣-苯基)-N-[4-(3,4-二曱氧基-苯 基)-異α惡嗤-5-基]-2-丙-2-快基氧基-乙 醯胺 C-104 一種個別化化合物I、II或IV 扶吉胺 C-105 一種個別化化合物I、II或IV 比芬諾 C-106 一種個別化化合物I、II或IV 3-[5-(4-氣-苯基)-2,3-二甲基-異噁唑啶-3-基]比π定 C-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-異噁唑 淀·3·基]·π比'^定 C-108 一種個別化化合物I、II或IV 2,3,5,6-四氯__4-曱石黃醯基-°比〇定 C-109 一種個別化化合物I、II或IV 3,4,5-二氯-〇比〇定-2,6-二甲腈 C-110 一種個別化化合物I、II或IV N-(l-(5-&gt;臭-3 -氣-σ比咬-2-基)-乙基)-2,4_ 二氣-終驗醯胺 C-lll 一種個別化化合物I、II或IV Ν-((5-溴-3-氣比啶-2-基)-甲基)-2,4-二 氣-於驗醯胺 C-112 一種個別化化合物I、II或IV 磺嘧菌靈 C-113 一種個別化化合物I、II或IV 西波定 C-114 一種個別化化合物I、II或IV 二氟林 C-115 —種個別化化合物I' II或IV 芬瑞莫 C-116 一種個別化化合物I、II或IV 嘧菌腙 C-117 一種個別化化合物I、II或IV 米潘尼比林 C-118 一種個別化化合物I、II或IV 氯咬 C-119 一種個別化化合物I、II或IV 氟苯嘧啶醇 C-120 一種個別化化合物I、II或IV 比利美沙尼 C-121 一種個別化化合物I、II或IV 賽福寧 C-122 一種個別化化合物I、II或IV 拌種咯 C-123 一種個別化化合物I、II或IV 護汰寧 149027.doc -221 - 201103430 混合物 組份1 組份2 C-124 一種個別化化合物I、Π或IV 阿迪嗎啉 C-125 一種個別化化合物I、II或IV 嗎菌靈 C-126 一種個別化化合物I、II或IV 乙酸嗎菌靈 C-127 一種個別化化合物I、II或IV 粉鑛说 C-128 一種個別化化合物I、Π或IV 十三嗎°林 C-129 一種個別化化合物I、II或IV 笨鏽啶 C-130 一種個別化化合物I、π或rv 氟醢亞胺 C-131 一種個別化化合物I、II或IV 依普同 C-132 一種個別化化合物I、II或IV 撲滅寧 C-133 一種個別化化合物I、π或rv 免克寧 C-134 一種個別化化合物I、II或IV 。惡。坐菌酮 C-135 一種個別化化合物I、II或IV °米坐菌酮 C-136 一種個別化化合物I、II或IV 氟多寧 C-137 一種個別化化合物I、Π或IV 辛。塞明 C-138 一種個別化化合物I、Π或IV 噻菌靈 C-139 一種個別化化合物I、Π或IV 5-胺基-2-異-丙基-4-鄰-曱笨基-2,3- — 氫·。比嗤-1-硫代曱酸S-稀丙S旨 C-140 一種個別化化合物I、Π或IV 酸化苯并噻二唑-S-曱酯 C-141 一種個別化化合物I、II或rv 吲唑磺菌胺 C-142 一種個別化化合物I、π或rv 敵菌靈 C-143 一種個別化化合物I、II或IV 殺稻瘟素-S C-144 一種個別化化合物I、II或IV 四氣丹 C-145 一種個別化化合物I、Π或IV 蓋普丹 C-146 一種個別化化合物I、II或IV 滅瞒猛 C-147 一種個別化化合物I、II或IV 邁隆 C-148 一種個別化化合物I、II或IV 咪菌威 C-149 一種個別化化合物I、II或IV 噠菌清 C-150 一種個別化化合物I、II或IV 苯敵快 C-151 一種個別化化合物I、II或rv 曱基硫酸苯敵快 C-152 一種個別化化合物I、II或IV 禾草靈 C-153 一種個別化化合物I、II或IV 福爾培 149027.doc • 222 - [si 201103430 混合物 組份1 組份2 C-154 一種個別化化合物I、II或IV 草酸(OxolinsSure) C-155 一種個別化化合物I、II或IV 粉病靈 C-156 一種個別化化合物I、II或IV 普奎那茲 C-157 一種個別化化合物I、II或IV 百快隆 C-158 一種個別化化合物I、II或IV 快諾芬 C-159 一種個別化化合物I、II或IV °米唾嘻 C-160 一種個別化化合物I、II或IV 三賽唑 C-161 一種個別化化合物I、II或IV 2· 丁氧基·6·峨-3-丙基-P克唏-4-画同 C-162 一種個別化化合物I、II或IV 5-氣-1-(4,6-二曱氧基-嘧啶_2_基)-2-曱 基-1H-苯并味»坐 C-163 一種個別化化合物I、II或IV 5-氣-7-(4-曱基-哌啶_1_基)_6-(2,4,6-三 氟-笨基)-[1,2,4]三峻并[i,5-a]嘧咬 C-164 一種個別化化合物I、II或IV 5-乙基·6-辛基-[1,2,4]三唑并[l,5-a]嘧 啶-7-基胺 C-165 一種個別化化合物I、Π或IV 福美鐵 C-166 一種個別化化合物I、II或IV 代森猛辞 C-167 一種個別化化合物I、Π或IV 代森錳 C-168 一種個別化化合物I、Π或IV 威百欲 C-169 一種個別化化合物I、Π或IV 續菌威 C-170 —種個別化化合物I、Π或IV 代森聯 C-171 一種個別化化合物I、Π或IV 丙森鋅 C-172 一種個別化化合物I、II或IV 福美雙 C-173 一種個別化化合物I、II或IV 代森鋅 C-174 一種個別化化合物I、II或IV 福美鋅 C-175 一種個別化化合物I、II或IV 乙黴威 C-176 一種個別化化合物I、II或IV 笨噻瓦利 C-177 一種個別化化合物I、II或IV 纈黴威 C-178 一種個別化化合物I、II或IV 霜黴威 C-179 一種個別化化合物I、II或IV 霜黴威鹽酸鹽 C-180 一種個別化化合物I、π或IV 威立芬那 C-181 一種個別化化合物I、II或IV N-(l-(l-(4-氰基笨基)乙磺醯基)-丁 -2-基)胺基曱酸-(4-氟苯基)酯 •223· 149027.doc 201103430 混合物 組份1 組份^ ~~ ' C-182 一種個別化化合物I、Π或IV 多寧 — C-183 一種個別化化合物I、II或IV C-184 一種個別化化合物I、Π或IV 雙胍辛 ---- C-185 一種個別化化合物I、II或IV 雙胍辛乙酸鹽 - C-186 一種個別化化合物I、II或IV 雙胍辛胺 - C-187 一種個別化化合物I、II或IV 雙胍辛胺三乙酸鹽 C-188 一種個別化化合物I、Π或IV 克熱淨(烧笨確酸鹽) C-189 一種個別化化合物I、Π或IV 春曰黴素 — C-190 一種個別化化合物I、Π或IV 春曰黴素鹽酸鹽水合物 C-191 一種個別化化合物I、Π或IV 夕氧菌素 C-192 一種個別化化合物I、Π或IV 鏈黴素 C-193 一種個別化化合物I、Π或IV 有效黴素A ' C-194 一種個別化化合物I、II或IV 百蟎克 C-195 一種個別化化合物I、π或rv 氣硝胺(Dicloran) C-196 一種個別化化合物I、II或IV 大脫蟎 C-197 一種個別化化合物I、Π或IV 白粉克 C-198 一種個別化化合物I、II或IV 酞菌酯 C-199 一種個別化化合物I、Π或IV 四氣硝基苯 C-200 一種個別化化合物I、II或IV 三笨錫鹽 C-201 一種個別化化合物I、II或IV 腈硫醌 C-202 一種個別化化合物I、Π或IV 稻瘟靈 C-203 一種個別化化合物I、π或rv 護粒松 C-204 一種個別化化合物I、π或rv 三乙膦酸、三乙膦酸鋁 C-205 一種個別化化合物I、II或IV 丙基喜樂松 C-206 一種個別化化合物I、II或rv 磷酸(H3P〇3)及衍生物 C-207 一種個別化化合物I、Π或IV 白粉松 C-208 一種個別化化合物I、II或IV 脫克松 C-209 一種個別化化合物I、II或IV 百菌清 C-210 一種個別化化合物I、Π或IV 益發靈 C-211 一種個別化化合物I、II或IV 雙氣酚 C-212 一種個別化化合物I、II或IV 氟硫滅 [si 149027.doc -224- 201103430 混合物 組份1 組份2 C-213 一種個別化化合物I、II或IV 六氣苯 C-214 —種個別化化合物I、II或IV 賓克隆 C-215 一種個別化化合物I、II或IV 五氣酚及其鹽 C-216 一種個別化化合物I、II或IV 苯欧 C-217 一種個別化化合物I、II或IV 奎脫辛 C-218 一種個別化化合物I、II或IV 甲基多保淨 C-219 一種個別化化合物I、II或IV 甲基益發靈 ^ C-220 —種個別化化合物I、II或IV N-(4-氣-2-硝基-苯基)-N-乙基-4-甲基- 苯磺醯胺 C-221 一種個別化化合物I、II或IV 波爾多液 C-222 一種個別化化合物I、II或IV 乙酸銅 C-223 —種個別化化合物I、II或IV 氫氧化銅 C-224 一種個別化化合物I、II或IV 氣氧化銅 C-225 一種個別化化合物I、II或IV 驗式硫酸銅 C-226 —種個別化化合物I、II或IV 硫 C-227 。一種個別化化合物I、II或IV 聯苯 C-228 一種個別化化合物I、II或IV 溴硝醇 C-229 —種個別化化合物I、II或IV 噻芬胺 C-230 一種個別化化合物I、II或IV 霜脲氰 C-231 一種個別化化合物I、II或IV 二苯胺 C-232 —種個別化化合物I、II或IV 美曲芬諾 C-233 —種個別化化合物I、II或IV 滅粉黴素 C-234 一種個別化化合物I、II或IV 羥基喹啉鋼 C-235 一種個別化化合物I、II或IV 調環酸鈣 C-236 一種個別化化合物I、II或IV 螺環菌胺 C-237 —種個別化化合物I、II或IV 曱基益發靈 C-238 —種個別化化合物I、II或IV N-(環丙基曱氧基亞胺基-(6-二氟甲氧 基-253-一 Hr苯基)-曱基)_2·苯基乙酿胺 C-239 —種個別化化合物I、II或IV N_-(4-(4-氣-3-三氟曱基-笨氧基)_2,5_二 甲基-笨基)-N-乙基-N-曱基甲脒 C-240 一種個別化化合物I、ΓΙ或IV N'-(4-(4-1-3-三氣曱基-苯氧基)_2,5-二 甲基-苯基)-N-乙基-N-甲基甲脒 -225 - 149027.doc 201103430 混合物 組份1 組份2 C-241 一種個別化化合物I、II或IV 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-曱 基曱脒 C-242 一種個別化化合物I、π或rv NH5-二氟曱基-2-曱基-4-(3-三曱基 梦烧基-丙氧基)-苯基)_N-乙基-N-甲 基曱脒 C-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-甲酸曱 基-(1,2,3,4-四氮-奈-1-基),酸月安 C-244 一種個別化化合物I、II或IV 2-{ 1-[2-(5-曱基-3-三氟曱基-吡唑-1-基)-乙醯基]-哌啶-4-基}-噻唑-4-甲酸曱 基-(R)-l,2,3,4-四氮-奈-1-基-Sfe胺 C-245 一種個別化化合物I、II或IV 乙酸6-第三丁基-8-氟-2,3-二甲基-喹啉-4-基S旨 C-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-2,3-二曱 基-啥淋-4-基酉旨 C-247 一種個別化化合物I、II或IV 加保利 C-248 一種個別化化合物I、II或IV 加保扶 C-249 一種個別化化合物I、II或IV 丁基加保扶 C-250 一種個別化化合物I、II或IV 納乃得硫雙威 C-251 一種個別化化合物I、II或IV 畢芬寧 C-252 一種個別化化合物I、II或IV 賽扶寧 C-253 一種個別化化合物I、II或IV 赛滅寧 C-254 一種個別化化合物I、II或IV 亞滅寧 C-255 一種個別化化合物I、II或rv ζ-氯氰菊酯 C-256 一種個別化化合物I、II或IV 第滅寧 C-257 一種個別化化合物I、II或IV 益化利 C-258 —種個別化化合物I、II或IV λ-赛洛寧 C-259 —種個別化化合物I、II或IV 百滅寧 C-260 一種個別化化合物I、II或rv 七氟菊酯 C-261 一種個別化化合物I、II或IV 二福隆 C-262 一種個別化化合物I、II或IV 氟芬隆 C-263 一種個別化化合物I、II或IV 祿芬隆 C-264 一種個別化化合物I、II或IV 得福隆 [s] 149027.doc -226· 201103430 混合物 組份1 組份2 C-265 一種個別化化合物I、II或IV 螺蟲乙酯 C-266 一種個別化化合物I、II或IV 可尼丁 C-267 一種個別化化合物I、II或IV α夫蟲胺 C-268 一種個別化化合物I、II或IV 益達胺 C-269 一種個別化化合物I、II或IV 噻蟲。秦 C-270 一種個別化化合物I、II或IV σ疋蟲脉 C-271 一種個別化化合物I、II或IV D塞蟲琳 C-272 一種個別化化合物I、II或IV 硫丹 C-273 一種個別化化合物I、II或IV 芬普尼 C-274 一種個別化化合物I、II或IV 阿巴汀 C-275 一種個別化化合物I、II或IV 因滅汀 C-276 一種個別化化合物I、II或IV 賜諾殺 C-277 一種個別化化合物I、II或IV 斯平托蘭 C-278 一種個別化化合物I、II或IV 伏蟻腙 C-279 一種個別化化合物I、II或IV 蟲蜗猜 C-280 一種個別化化合物I、II或IV 芬布賜 C-281 一種個別化化合物I、II或IV 茚蟲威 C-282 一種個別化化合物I、II或IV 美H月宗 C-283 一種個別化化合物I、II或IV IL尼胺 C-284 一種個別化化合物I、II或IV 福本胺 C-285 一種個別化化合物I、II或IV 氣鄰胺基苯甲普 C-286 一種個別化化合物I、II或IV 魚尼汀受體抑制劑(HGW86) C-287 一種個別化化合物I、II或IV 嗟氟美芬 C-288 一種個別化化合物I、II或IV 乙草胺 C-289 一種個別化化合物I、II或IV 二甲噻草胺 C-290 一種個別化化合物I、II或IV 異丙甲草胺 C-291 一種個別化化合物I、II或IV 。比草胺 C-292 一種個別化化合物I、II或IV 嘉磷塞 C-293 一種個別化化合物I、II或IV 固殺草 C-294 一種個別化化合物I、II或IV 硫復松 C-295 一種個別化化合物I、II或IV 炔草酸 -227- 149027.doc 201103430 混合物 組份1 組份2 C-296 一種個別化化合物I、II或IV 噁唑禾草靈 C-297 一種個別化化合物I、II或IV 0比氟禾草靈 C-298 一種個別化化合物I、II或IV 11比氟氣禾靈 C-299 一種個別化化合物I、II或IV 百草枯 C-300 一種個別化化合物I、II或IV 甜菜寧 C-301 一種個別化化合物I、II或IV 克草同 C-302 一種個別化化合物I、II或IV 環殺草 C-303 一種個別化化合物I、II或IV 環苯草酮 C-304 一種個別化化合物I、II或IV 西殺草 C-305 一種個別化化合物I、II或IV 得殺草 C-306 一種個別化化合物I、II或IV 二甲戊樂靈 C-307 一種個別化化合物I、II或IV 胺氟樂靈 C-308 一種個別化化合物I、II或IV 氟樂靈 C-309 一種個別化化合物I、II或IV 三氟羧草醚 C-310 一種個別化化合物I、II或IV 溴苯腈 C-311 一種個別化化合物I、II或IV 咪草酯 C-312 一種個別化化合物I、II或IV 曱氧η米草煙 C-313 一種個別化化合物I、II或IV 甲D米σ坐煙酸 C-314 一種個別化化合物I、II或IV 滅草煙 C-315 一種個別化化合物I、II或IV 滅草喹 C-316 一種個別化化合物I、II或IV 咪草煙 C-317 一種個別化化合物I、II或IV 2,4-二氣苯氧基乙酸(2,4-D) C-318 一種個別化化合物I、II或IV 氣草敏 C-319 一種個別化化合物I、II或IV 畢克草 C-320 一種個別化化合物I、II或IV 氟草煙 C-321 一種個別化化合物I、II或IV 毒赛定 C-322 一種個別化化合物I、II或IV 氟°比草胺 C-323 一種個別化化合物I、π或rv 苄嘧磺隆 C-324 一種個別化化合物I、II或IV 乙基氣嘧磺隆 C-325 一種個別化化合物I、II或IV 環丙嘧磺隆 C-326 一種個別化化合物I、II或IV 碘曱磺隆 149027.doc -228- [si 201103430 混合物 組份1 組份2 C-327 一種個別化化合物I、II或IV 甲磺胺磺隆 C-328 一種個別化化合物I、II或IV 甲基甲·磺隆 C-329 一種個別化化合物I、II或IV 煙,項隆 C-330 一種個別化化合物I、II或IV 艰嘧磺隆 C-331 一種個別化化合物I、II或IV 氟胺磺隆 C-332 一種個別化化合物I、II或IV 莠去津 C-333 一種個別化化合物I、II或IV 六嗪同 C-334 一種個別化化合物I、II或IV 敵草隆 C-335 一種個別化化合物I、II或IV 雙氟磺草胺 C-336 一種個別化化合物I、II或IV 普羅蘇芬 C-337 一種個別化化合物I、II或IV 苯達松 C-338 一種個別化化合物I、II或IV 吲哚酮草酯 C-339 一種個別化化合物I、II或IV 環庚草醚 C-340 一種個別化化合物I、II或IV 麥草畏 C-341 一種個別化化合物I、II或IV 二氟吡隆 C-342 一種個別化化合物I、II或IV 二氣喹啉酸 C-343 一種個別化化合物I、II或IV 喹草酸 C-344 一種個別化化合物I、II或IV 曱基磺草酮 C-345 一種個別化化合物I、II或IV 嘧啶肟草醚 C-346 一種個別化化合物I、II或IV 拓普美月宗 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 ; 149027.doc -229· 201103430 DE 19650197 ; DE 10021412 ; DE 102005009458 ; US 3,296,272 ; US 3,325,503 ; WO 98/46608 ; WO 99/14187 ;Mixture component 1 component 2 C-41 an individualized compound I, hydrazine or IV 2-chlorodimethylindophthyl-4-yl)--prolineamine C-42 an individualized compound I, π or IV N-(3',4f,5-di-fluorobenz-2-yl)-3-dimethylmethyl-bumethyl-1H-pyrazole-4-decylamine C-43 an individualized compound I, II Or IV Ν-(4·-trifluoromethylsulfanylbiphenyl-2-yl)-3-difluoromethyl-1-indolyl-1H-pyrazole-4-decylamine C-44 Compound I, hydrazine or IV N-(2-(l,3-dimercapto-butyl)-phenyl)-1,3-dimethyl-5-fluoro-1H-pyrazole-4-carboxamide C-45 An individualized compound I, hydrazine or IV N-(2-(l,3,3-trif-butyl-phenyl)-phenyl)-i,3-dimethyl-5-fluoro-1H- Pyrazole-4-carboxamine C-46 An individualized compound I, II or IV daxanphene C-47 an individualized compound I, II or IV flumorpholine C-48 an individualized compound I, II or IV Ding &quot; 比吗淋C-49 An individualized compound I, hydrazine or IV flumetamide C-50 An individualized compound I, II or IV fluoropyramine C-51 an individualized compound I, II or IV flupirtine C-52 an individualized compound I, II or IV gas benzene Amine C-53 An individualized compound I, II or IV N-(3-ethyl-3,5,5-trimethyl-cyclohexyl)-3-carboxyamino-2-hydroxy-benzamide Amine C-54 an individualized compound I, II or IV gupamine C-55 an individualized compound I, II or IV dioxo (dic.locymet) C-56 an individualized compound I, II or IV Alkyomycin C-57 An individualized compound I, II or IV oxytetracycline C-58 an individualized compound I, II or IV wonderful sulfur C-59 an individualized compound I, II or IV N-(6 -Methoxy-pyridin-3-yl)cyclopropanoic acid decylamine C-60 An individualized compound I, II or IV Azakol 嗤C-61 An individualized compound I, II or IV than donut C- 62 An individualized excimer I, II or IV Bromogram C-63 An individualized compound I, II or IV cycloxazole C-64 an individualized compound I, II or IV difenoconazole C-65 An individualized compound I, II or IV dinitroconazole C-66 an individualized compound I, II or IV dinitroconazole-M 149027.doc • 219-201103430 mixture component 1 component 2 C-67 an individual Compound I, II or IV gas ring β sitting C-68 Individualized compound I, II or IV fenbuconazole C-69 an individualized compound I, hydrazine or IV fluconazole C-70 an individualized compound I, II or IV flucarbazole C-71 Compound I, hydrazine or IV Hydrazine C-72 An individualized compound I, II or IV hexahydrate C-73 An individualized compound I, hydrazine or IV imine D sits C-74 an individualized compound I, II Or IV Epke. Sit C-75 An individualized compound I, π or IV Phytophthora α sit C-76 An individualized compound I, II or IV Maidinidin C-77 An individualized compound I, Π or IV 咪咪β sits C -78 An individualized compound I, II or IV Bark C-79 An individualized compound I, II or IV Penconazole C-80 An individualized compound I, II or IV Propyl-salt C-81 An individual compound I, II or IV propyl thiol ketone C-82 an individualized compound I, II or IV oxime azole C-83 an individualized compound I, II or IV Dekley C-84 an individualized compound I, π or IV fluoroether salivary C-85 an individualized compound I, II or IV trimethoprim C-86 an individualized compound I, hydrazine or IV tri-teronol C-87 an individualized compound I, II or IV ring bacteria ° C -88 an individualized compound I, II or IV. Effect C-89 An individualized compound I, II or IV Κ4-a-phenyl)-2-([1,2,4]triazole-1- ))-cycloheptanol C-90 An individualized compound I, II or IV 赛赛灭C-91 An individualized compound I, II or IV 灭列列 C-92 An individualized compound I, II or IV Column Acidate C-93 An individualized compound I, II or IV rice sulphate C-94 An individualized compound I, II or IV Poker La C-95 An individualized compound I, II or IV Safford C-96 Individualized compound I, II or IV benomyl 149027.doc • 220· [si 201103430 mixture component 1 component 2 C-97 - individualized compound I, II or IV befenfen C-98 an individualized compound I, II or IV Maishenling C-99 an individualized compound I, II or IV thiabendazole C-100 an individualized compound I, II or IV ethipramine C-101 an individualized compound I, II or IV 依得利 C-102 An individualized compound I, II or IV carbendazim C-103 an individualized compound I, II or IV 2-(4-a-phenyl)-N-[4-(3, 4-Dimethoxy-phenyl)-iso-oxo-5-yl]-2-propan-2-freeoxy-acetamide C-104 An individualized compound I, II or IV edugalamine C-105 An individualized compound I, II or IV Tefino C-106 an individualized compound I, II or IV 3-[5-(4-a-phenyl)-2,3-dimethyl-iso Oxazolidine-3-yl] than π-C-107 An individualized compound I, II or IV 3-[5- (4-Methyl-phenyl)-2,3-dimethyl-isoxazole Dang·3·yl]·π ratio '^定C-108 An individualized compound I, II or IV 2,3,5 ,6-tetrachloro__4-曱石黄醯基-°比定定C-109 An individualized compound I, II or IV 3,4,5-dichloro-indole 〇定定-2,6-dicarbonitrile C -110 an individualized compound I, II or IV N-(l-(5-&gt; odor-3 - gas-σ ratio -2-yl)-ethyl)-2,4_diox-final amine C-lll An individualized compound I, II or IV Ν-((5-bromo-3-apiridin-2-yl)-methyl)-2,4-digas--proline amine C-112 Individualized compound I, II or IV sulfamethoxazole C-113 an individualized compound I, II or IV simboldine C-114 an individualized compound I, II or IV diflurine C-115 - an individualized compound I' II or IV fenrimyl C-116 an individualized compound I, II or IV azoxystrobin C-117 an individualized compound I, II or IV rice penicillin C-118 an individualized compound I, II Or IV Chloride C-119 An Individualized Compound I, II or IV Fluoropyrimidinol C-120 An Individualized Compound I, II or IV Bilimecin C-121 An Individualized Compound I, II or IV Funing C-122 An individualized compound I, II or IV Seed dressing C-123 An individualized compound I, II or IV NING 149027.doc -221 - 201103430 Mixture component 1 Component 2 C-124 Individualized compound I, hydrazine or IV adimorpholine C-125 an individualized compound I, II or IV carbendazim C-126 an individualized compound I, II or IV acetaminophen C-127 an individualized compound I , II or IV fine ore, said C-128, an individualized compound I, hydrazine or IV, thirteen, C, 129, an individualized compound I, II or IV, pyridine, C-130, an individualized compound I, π or Rv Fluoroquinone C-131 An individualized compound I, II or IV Escherichia C-132 An individualized compound I, II or IV Fighting C-133 An individualized compound I, π or rv Free Kein C -134 An individualized compound I, II or IV. evil. Phytosinone C-135 An individualized compound I, II or IV ° acetaminophen C-136 An individualized compound I, II or IV Fludonine C-137 An individualized compound I, hydrazine or IV octane. Seming C-138 An individualized compound I, hydrazine or IV thiabendazole C-139 An individualized compound I, hydrazine or IV 5-amino-2-iso-propyl-4-o-indole-based-2 , 3- — Hydrogen·.嗤-1-thio decanoic acid S- succinyl S-C-140 An individualized compound I, hydrazine or IV acidified benzothiadiazole-S- decyl ester C-141 An individualized compound I, II or rv Oxazone C-142 An individualized compound I, π or rv carbendazim C-143 an individualized compound I, II or IV blasticidin-S C-144 an individualized compound I, II or IV Tetragen C-145 An individualized compound I, hydrazine or IV Cappuccine C-146 An individualized compound I, II or IV cockroach C-147 An individualized compound I, II or IV Mailon C-148 An individualized compound I, II or IV imiprozil C-149 an individualized compound I, II or IV sputum C-150 an individualized compound I, II or IV benzoin C-151 an individualized compound I , II or rv thiol sulfonate fast C-152 an individualized compound I, II or IV oxacillin C-153 an individualized compound I, II or IV Forpe 149027.doc • 222 - [si 201103430 mixture Component 1 Component 2 C-154 An individualized compound I, II or IV Oxolins Sure C-155 An individualized compound I, II or IV powder disease C-156 An individualized compound I, II or IV Puccinaz C-157 An individualized compound I, II or IV Hundred Kelvin C-158 An individualized compound I, II or IV veprofen C-159 an individualized compound I , II or IV ° m. saliva C-160 an individualized compound I, II or IV trioxazole C-161 an individualized compound I, II or IV 2 · butoxy · 6 · indole-3-propyl - P克唏-4-画同C-162 An individualized compound I, II or IV 5-gas-1-(4,6-dimethoxy-pyrimidin-2-yl)-2-indenyl-1H- Benzoin»Sit C-163 An individualized compound I, II or IV 5-gas-7-(4-mercapto-piperidinyl-1-yl)_6-(2,4,6-trifluoro-phenyl )-[1,2,4]三峻和[i,5-a] pyrimidine C-164 an individualized compound I, II or IV 5-ethyl·6-octyl-[1,2,4] Triazolo[l,5-a]pyrimidin-7-ylamine C-165 an individualized compound I, hydrazine or IV ferrocene C-166 an individualized compound I, II or IV Individualized compound I, hydrazine or IV mancozegan C-168 An individualized compound I, hydrazine or IV 百 欲 C-169 An individualized compound I, hydrazine or IV Continuum C-170 - individualized I, Π or IV 森森联 C-171 An individualized compound I, hydrazine or IV propyl zinc C-172 An individualized compound I, II or IV thiram C-173 An individualized compound I, II or IV Dessert Zinc C-174 An Individualized Compound I, II or IV Fumei Zinc C-175 An Individualized Compound I, II or IV. Ethylcarbamate C-176 An Individualized Compound I, II or IV Stupid Tully C- 177 An individualized compound I, II or IV 缬 威 C C-178 An individualized compound I, II or IV. Mildew C-179 An individualized compound I, II or IV. Individualized compound I, π or IV Willinphenine C-181 An individualized compound I, II or IV N-(l-(l-(4-cyanophenyl)ethenyl)-but-2- Amino phthalic acid-(4-fluorophenyl) ester • 223· 149027.doc 201103430 Mixture component 1 Component ^ ~~ ' C-182 An individualized compound I, Π or IV 宁宁 — C-183 An individualized compound I, II or IV C-184 an individualized compound I, hydrazine or IV bisindole---- C-185 an individualized compound I, II or IV bisindole acetate - C-186 Compound I, II or IV Bis-octylamine-C-187 An individualized compound I, II or IV Bis-octylamine triacetate C-188 An individualized compound I, hydrazine or IV gram of heat (burning acid salt) C-189 An individualized compound I, hydrazine or IV vincomycin - C-190 An individualized compound I, hydrazine or IV Phytomycin hydrochloride hydrate C-191 An individualized compound I, hydrazine or IV An individual compound I, hydrazine or IV streptomycin C-193 An individualized compound I, hydrazine or IV tyrosin A ' C-194 An individualized compound I, II or IV克C-195 An individualized compound I, π or rv Dicloran C-196 An individualized compound I, II or IV Largely deuterated C-197 An individualized compound I, hydrazine or IV white powder gram C- 198 an individualized compound I, II or IV trifloxystrobin C-199 an individualized compound I, hydrazine or IV tetranitrobenzene C-200 an individualized compound I, II or IV tristinyl salt C-201 Individualized compound I, II or IV nitrile sulfonium C-202 An individualized compound I, hydrazine or IV Indigo C-203 An individualized I, π or rv granules C-204 an individualized compound I, π or rv triethylphosphonic acid, aluminum triethylphosphonate C-205 an individualized compound I, II or IV propyl chelsson C-206 An individualized compound I, II or rv phosphoric acid (H3P〇3) and a derivative C-207 an individualized compound I, hydrazine or IV white pine C-208 An individualized compound I, II or IV Dexon C-209 An individualized compound I, II or IV chlorothalonil C-210 an individualized compound I, hydrazine or IV effluent C-211 an individualized compound I, II or IV bisphenol C-212 an individualized compound I, II or IV fluorosulfurization [si 149027.doc -224- 201103430 Mixture component 1 component 2 C-213 an individualized compound I, II or IV hexabenzene benzene C-214 - individualized compound I, II or IV Binclones C-215 An individualized compound I, II or IV Pentaphenol and its salt C-216 An individualized compound I, II or IV Benzene C-217 An individualized compound I, II or IV quetiacin C -218 An individualized compound I, II or IV methylpolysafe C-219 An individualized compound I, II or IV methyl valproate ^ C-2 20-An individualized compound I, II or IV N-(4-Gas-2-nitro-phenyl)-N-ethyl-4-methyl-benzenesulfonamide C-221 An individualized compound I, II or IV Bordeaux C-222 An individualized compound I, II or IV Copper acetate C-223 - Individualized compound I, II or IV Copper hydroxide C-224 An individualized compound I, II or IV C-225 An individualized compound I, II or IV of copper sulfate C-226 - an individualized compound I, II or IV sulfur C-227. An individualized compound I, II or IV biphenyl C-228 an individualized compound I, II or IV bromoxynol C-229 - an individualized compound I, II or IV thiafenac C-230 an individualized compound I , II or IV sulphonic acid cyanide C-231 an individualized compound I, II or IV diphenylamine C-232 - an individualized compound I, II or IV melfene C-233 - an individualized compound I, II or IV Dictomycin C-234 An individualized compound I, II or IV hydroxyquinoline steel C-235 An individualized compound I, II or IV calcium cyclamate C-236 An individualized compound I, II or IV snail Cyclosporin C-237 - an individualized compound I, II or IV thiol valproate C-238 - an individualized compound I, II or IV N-(cyclopropyl decyloxyimino-(6-di Fluoromethoxy-253-Hrphenyl)-indenyl)_2-phenylethylamine C-239 - Individualized compound I, II or IV N_-(4-(4-gas-3-trifluoro) Indole-stupyloxy)_2,5-dimethyl-phenyl)-N-ethyl-N-mercaptomethylhydrazine C-240 An individualized compound I, hydrazine or IV N'-(4-(4 -1-3-triseodecyl-phenoxy)_2,5-dimethyl-phenyl)-N-ethyl-N-methylformamidine-225 - 149027.doc 201103430 Mixture component 1 Component 2 C-241 An individualized compound I, II or IV N'-(2-methyl-5-trifluoromethyl-4-(3-trimethyldecyl)- Propoxy)-phenyl)-N-ethyl-N-mercaptopurine C-242 An individualized compound I, π or rv NH5-difluorodecyl-2-mercapto-4-(3-tri An individualized compound I, II or IV 2-{1-[2-(5-fluorenyl) -3-trifluoromethyl-pyrazol-1-yl)-ethinyl]-piperidin-4-yl}-thiazole-4-carboxylic acid decyl-(1,2,3,4-tetrazine-na -1-yl), acid sulphate C-244 an individualized compound I, II or IV 2-{ 1-[2-(5-fluorenyl-3-trifluoromethyl-pyrazol-1-yl)- Ethyl]-piperidin-4-yl}-thiazole-4-carboxylic acid decyl-(R)-l,2,3,4-tetrazine-n-yl-Sfeamine C-245 Compound I, II or IV Acetic acid 6-Terbutyl-8-fluoro-2,3-dimethyl-quinolin-4-yl S. C-246 An individualized compound I, II or IV oxime- Acetic acid 6-t-butyl-8-fluoro-2,3-didecyl-indole-4-ylindole C-247 an individualized compound I, II or IV plus Poly C-248 an individualized compound I , II or IV plus C-249 An individualized compound I, II or IV butyl plus Bao C-250 An individualized compound I, II or IV Na Nade thiodicarb C-251 An individualized compound I, II or IV Bifenin C- 252 An individualized compound I, II or IV Safranine C-253 An individualized compound I, II or IV Saining C-254 An individualized compound I, II or IV Sub-Ning C-255 An individual compound I, II or rv ζ-cypermethrin C-256 An individualized compound I, II or IV fentanyl C-257 an individualized compound I, II or IV 益化利 C-258 - an individualized compound I, II or IV λ-赛洛宁 C-259 — Individualized compound I, II or IV 百灭宁 C-260 An individualized compound I, II or rv Tefluthrin C-261 An individualized compound I, II or IV二福隆C-262 An individualized compound I, II or IV Flufuron C-263 An individualized compound I, II or IV Lucendron C-264 An individualized compound I, II or IV Defolon [s ] 149027.doc -226· 201103430 Mixture Component 1 Component 2 C-265 An Individualized Compound I, II or IV Spirotetramat C-266 Individualized compound I, II or IV Cotinine C-267 An individualized compound I, II or IV α-clavamide C-268 An individualized compound I, II or IV etadamine C-269 An individual compound I, II or IV worms. Qin C-270 An individualized compound I, II or IV σ 疋 脉 C C-271 An individualized compound I, II or IV D cecutin C-272 An individualized compound I, II or IV endosulfan C-273 An individualized compound I, II or IV Fenpney C-274 An individualized compound I, II or IV Abatatin C-275 An individualized compound I, II or IV Inhibitor C-276 An individualized compound I , II or IV. C-277 An individualized compound I, II or IV Spinoline C-278 An individualized compound I, II or IV Volt C-279 An individualized compound I, II or IV Insect C. C-280 An Individualized Compound I, II or IV Fenbu C-281 An Individualized Compound I, II or IV Indoxacarb C-282 An Individualized Compound I, II or IV. -283 An individualized compound I, II or IV IL nitramine C-284 An individualized compound I, II or IV Fubenamine C-285 An individualized compound I, II or IV gaseous o-aminobenzamide C-286 An individualized compound I, II or IV nicotinin receptor inhibitor (HGW86) C-287 an individualized compound I, II or IV flumazum C -288 An individualized compound I, II or IV Acetochlor C-289 An individualized compound I, II or IV Methifen C-290 An individualized compound I, II or IV Metolachlor C- 291 An individualized compound I, II or IV. Butachlor C-292 An individualized compound I, II or IV jiaphosphonate C-293 An individualized compound I, II or IV. C-294 An individualized compound I, II or IV thiolopine C- 295 An individualized compound I, II or IV acetyl oxalic acid -227-149027.doc 201103430 Mixture component 1 Component 2 C-296 An individualized compound I, II or IV Oxazolicide C-297 An individual compound I, II or IV 0 is better than fluoxacillin C-298. An individualized compound I, II or IV 11 is more specific than the fluorine gas C-299. An individualized compound I, II or IV Paraquat C-300 An individual compound I, II or IV beetine C-301 an individualized compound I, II or IV gram of grass with C-302 an individualized compound I, II or IV cyclosporin C-303 an individualized compound I, II or IV ring Benzolidone C-304 An individualized compound I, II or IV Pseudomonas C-305 An individualized compound I, II or IV. A herbicide C-306 An individualized compound I, II or IV Pendimethalin C-307 An individualized compound I, II or IV Amphetamine C-308 An individualized compound I, II or IV Trifluralin C- 309 An individualized compound I, II or IV Acifluorfen C-310 An individualized compound I, II or IV bromoxynil C-311 An individualized compound I, II or IV Imazethin C-312 An individual Compound I, II or IV 曱 η 草 草 C C-313 An individualized compound I, II or IV A D σ 坐 nicotinic acid C-314 An individualized compound I, II or IV imazapyrine C-315 An individualized compound I, II or IV imazaquin C-316 an individualized compound I, II or IV imazethapyr C-317 an individualized compound I, II or IV 2,4-diphenoxyacetic acid ( 2,4-D) C-318 An individualized compound I, II or IV Aerosol sensitive C-319 An individualized compound I, II or IV Biekgrass C-320 An individualized compound I, II or IV Fluorine Tobacco C-321 An individualized compound I, II or IV toxin C-322 An individualized compound I, II or IV Fluoropyramine C-323 An individualized compound I, π or rv Bensulfuron-C -324 An individualized compound I, II or IV Ethylsulfuron-C-325 An individualized compound I, II or IV Cyclopropsulfuron-C-326 An individualized compound I II or IV Iodosulfuron 149027.doc -228- [si 201103430 Mixture Component 1 Component 2 C-327 An Individualized Compound I, II or IV Sulfasulfuron-C-328 An Individualized Compound I, II or IV Methylsulfuron C-329 An individualized compound I, II or IV smoke, a long-term C-330, an individualized compound I, II or IV, an imidazosulfuron C-331, an individualized compound I, II or IV flucarbazone C-332 an individualized compound I, II or IV atrazine C-333 an individualized compound I, II or IV hexazine with C-334 an individualized compound I, II or IV diuron C-335 An individualized compound I, II or IV diflufenacil C-336 An individualized compound I, II or IV Prosufene C-337 An individualized compound I, II or IV bentazon C-338 An individualized compound I, II or IV ketoxime C-339 An individualized compound I, II or IV cycloheptyl ether C-340 An individualized compound I, II or IV dicamba C-341 Compound I, II or IV diflupiron C-342 an individualized compound I, II or IV dihaloquinoic acid C-343 Compound I, II or IV Quinoxalic Acid C-344 An Individualized Compound I, II or IV Sulfosyl Ketone C-345 An Individualized Compound I, II or IV Pyrimidinol C-346 An Individualized Compound I , II or IV Topex is known as the active substance of component 2, its preparation and its activity against harmful fungi are known (see, http://www.alanwood.net/pesticides/); Other substances 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; 149027.doc-229·201103430 DE 19650197; DE 10021412; DE 102005009458; US 3,296,272; US 3,325,503; 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 03/1 1853 ; 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、II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、π 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 03/1 1853; 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 ). Mixtures of the active substances may be prepared in the form of compositions by a conventional method, for example, by a method of the compositions of the compounds I, II and/or IV, which compositions comprise at least one inert ingredient in addition to the active ingredient. Ingredients. With regard to the common ingredients of such compositions, reference is made to the explanations for compositions containing compounds I, π and/or IV. Mixtures of the active substances according to the invention are suitable as fungicides. 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. Compounds I, II and IV and their pharmaceutically acceptable salts are also suitable for treatment

ί SI 149027.doc -230- 201103430 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 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 受之鹽,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、Ci_ CU烷基磺酸(諸如甲磺酸)、芳族磺酸(諸如苯磺酸及甲苯磺 酸)、草酸、順丁烯二酸、反丁烯二酸、乳酸、酒石酸、 己二酸及笨甲酸。其他合適之酸係描述於例wF〇rtsch出te der Arzneimittelforschung,第 10 卷,第 224 ff.頁, Birkhauser 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 剑賦形劑、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、„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I、II及/或IV之化合物或 149027.doc 231 201103430 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卜π及/或1¥之化合物或 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。SUb ’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、_、腸、前 列腺、皮膚(黑色素瘤)、腎臟、膀胱、口腔”侯、食道、 月卵巢、騰腺、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用 於治療以下動物之病毒感染:温血脊椎動物,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 諸如狗m努動物(牛、綿羊、山'羊、野牛 等)、馬’及鳥類,諸如雞、火雞、鴨、鶴'珠雞及其類 似物。其適用於治療病毒感染,例如反轉錄病毒感染,諸 如mV及HTLV、流感病毒感染、鼻病毒感染、癌療及其 類似感染。 例如經口、靜脈 本發明之化合物可以習用方式投與 J49027.doc •232· f S3 201103430 内肌肉内或皮下。對於經口投與而言,可將活性化合物 與例如惰性稀釋劑或可食用載劑混合;可將其包埋於硬質 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錠 劑、口腔欽劑、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1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 勝;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 椒薄荷、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 齊J丸劑及勝囊可經蟲膠(schellack)、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曱酯或對羥基苯曱 酉λ丙Sa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。 149027.doc -233 - 201103430 亦可非經腸或腹膜内投與 潤劑ί諸^,性化合物。可使用合適之濕 溶液或懸变、y ,、)^水來製備活性化合物或其鹽之 之3八队+ 甘油、液態聚乙二醇及其於油中SI SI 149027.doc -230- 201103430 Human and animal diseases, 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" and refers to an agent used against animal pathogenic or human pathogenic fungi, that is, for combating animals, especially mammals (including humans). An agent for fungi in 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 especially the physiologically tolerated salts of Compound I, in particular, physiologically acceptable acid addition salts of acids. Examples of suitable organic and inorganic acids are hydrochloric acid, hydrobromic acid 'phosphoric acid, sulfuric acid, Ci_ CU alkyl sulfonic acid (such as methanesulfonic acid), aromatic sulfonic acids (such as benzenesulfonic acid and toluenesulfonic acid), oxalic acid, cis. Butenedioic acid, fumaric acid, lactic acid, tartaric acid, adipic acid and benzoic acid. Other suitable acid systems are described in the example of WF Artzneimittelforschung, Vol. 10, page 224 ff., Birkhauser Verlag, Basle and Stuttgart, 1966, the entire contents of which are expressly incorporated herein by reference. in. Suitable carriers are, for example, those commonly used in pharmaceutical formulations, sacrificial excipients, binders, and the like, which are described below in an exemplary manner for the particular mode of administration. Another aspect of the invention relates to the use of the compound I, „ and Iv or a pharmaceutically acceptable salt thereof for the preparation of an antifungal 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 pertains to a compound of formula I, II and/or IV or 149027.doc 231 201103430 a pharmaceutically acceptable salt thereof for use in the treatment of cancer Use of the agent for use. Another aspect of the invention relates to the use of a compound of the formula π and/or 1 or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment or prevention of a viral infection. The compounds of I, II and IV and/or their pharmaceutically acceptable salts are suitable for the treatment, inhibition or control of the growth and/or proliferation of tumor cells and the conditions associated therewith. SUb 'is suitable for cancer therapy of the following animals: Warm-blooded vertebrates 'for example, mammals and birds, especially males, and other mammals' are particularly useful livestock, such as dogs, cats, pigs, ruminants (bovine, sheep, goats, bison, etc.), horses, and birds. , such as chicken , turkey, duck, goose, guinea fowl and the like. The compounds of formulas I, II and IV and/or their pharmaceutically acceptable salts are suitable for the treatment of cancer or cancerous disorders of the following organs: breast, _ , intestine, prostate, skin (melanoma), kidney, bladder, oral cavity, esophagus, ovary, gonad, liver and brain or CNS. The compounds of the formulae I, II and IV and/or their pharmaceutically acceptable salts are suitable for the treatment of viral infections in the following animals: warm-blooded vertebrates, for example mammals and birds, especially males, and other mammals, especially useful Houses such as dog mnu (bovine, sheep, mountain 'sheep, bison, etc.), horse' and birds, such as chicken, turkey, duck, crane 'beads and their analogues. It is useful for treating viral infections such as retroviral infections such as mV and HTLV, influenza virus infections, rhinovirus infections, cancer treatments and the like. For example, the compound of the present invention can be administered intramuscularly or subcutaneously in a conventional manner by J49027.doc • 232· f S3 201103430. For oral administration, the active compound may be mixed with, for example, an inert diluent or an edible carrier; it may be enclosed in a hard or soft gelatin capsule which may be compressed into a lozenge or may be administered directly Food / feed mix. The active compound may be mixed with excipients and administered in the form of indigestible lozenges, oral solutions, tablets, pills, capsules, suspensions, liquids, syrups and the like. These preparations should contain at least 0.1% active compound. The composition of the formulation may of course vary. The dosage unit usually comprises from 2 to 60% by weight of the active compound. The preferred formulation of the compound 1 of the invention comprises from 10 to 1000 mg of active compound per oral dosage unit. The agent, the pill 'capsule and the like may comprise the following components: a binder such as tragacanth, acacia, corn starch or Mingsheng; an excipient 'such as calcium hydrogen phosphate; a disintegrating agent 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 peppermint, vanilla and the like. Containing a liquid carrier. Other substances which modify the nature of the dosage unit may also be used. For example, the ingot J pellet and the capsule may be coated with schellack, sugar or a mixture thereof. In addition to the active compound, the syrup Or the drink may also contain sugar (or other sweetener), a hydroxybenzoate or a p-hydroxybenzoquinone gamma-Sa coloring agent and/or flavoring agent as a preservative. Of course, the active compound The components of the formulation must be pharmaceutically pure and non-toxic in the amounts used. In addition, the active compound may be formulated as a formulation for controlling the release of the active compound, such as a delayed release formulation. 149027.doc -233 - 201103430 Intestinal or intraperitoneal administration of emollients, compounds, can be prepared using a suitable wet solution or suspension, y, ,) water to prepare the active compound or its salt of the eight teams + glycerol, liquid polyethylene Glycol and its oil

之混合物來製備分散液 T 止微生物生長。 匕專版劑常另外包含防腐劑以防 欲供注射用之製劑包 ^ .、'、菌水溶液及分散液以及用於製 備無菌溶液及分散液 农 …、菌叔末。製劑必須具有足夠流動 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 水、乙醇、多元醇(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】 由以下非限制性貫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1及11之化合物的殺真菌作用: Α)微量滴定試驗 活性物質於二曱亞砜(DMSO)中單獨地調配成儲備溶 液’濃度為10 000 ppm。 使用實例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農 度。隨後添加致病疫黴菌之遊走孢子水性懸浮液。將盤置 149027.doc -234- 201103430 於溫度為18。(: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Μτρ。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_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 之稻瘟病病原體的活性 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 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(=1〇〇%)之生長進行比較且與= 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。/〇。 使用實例3 :在微量滴定試驗中對抗由小麥殼針抱菌所引 起之殼針抱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(=1〇〇%)之生長進行比較i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 I49027.doc -235· 201103430 體在個別活性物質中之相對生長%。 B)溫室試驗 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/或二曱亞石風(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酚之潤濕 劑)之混合物以溶劑/乳化劑99:1之體積比將其補足至10 ml。隨後使用水將該溶液補足至1 〇〇 ml。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。 使用貫例4 以保護性施用對抗由致病疫黴菌所引起之番 茄早疫病之活性 使番%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。在接種之 後’將試驗植物立即轉移至潮濕室内。在置於丨8至2(rc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。 使用實例5 :對抗小麥上之隱匿柄鏽菌(小麥褐銹病)的治療 性作用 以小麥褐銹病(隱匿柄鏽菌)之孢子懸浮液喷灑栽培品種 「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20-221之室内24小時。在此期間,孢子發 芽且芽管透入葉片組織中。次曰’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。 【S1 149027.doc • 236· 201103430 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7〇%之相對大氣濕度下再培養7天。 隨後目測葉上之銹病進展程度。 使用實例6 :對抗小麥上之隱匿柄鏽菌(小麥褐銹病)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噴灑栽培 種Kanzler」之盆:栽小麥幼苗葉直至溢流點為止。次 日,以小麥褐銹病(隱匿柄鏽菌)之孢子懸浮液噴灑處理組 植物。隨後將植物置於高大氣濕度(9〇至95%)&amp;2〇_22t2 室内24小時。在此期μ,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2〇與22。〇之間的溫 度及65至7G%之相對大氣濕度下再培養7天。隨後目測葉 上之錢病進展程度。 使用實例7·.對抗小麥上之小麥白粉病菌(小麥白粉病)的保 護性作用 口以具有下文規定之活性物質濃度之水性懸浮液喷灑栽培 種Kanzler」之盆栽小麥幼苗葉直至溢流點為止。次 日’以小麥白粉病(小麥白粉病菌)之孢子懸浮液喷麗處理 組植物。隨後使植物返回溫室中且在2(&gt;與抑之間的溫度 及60至90%之招對大氣濕度下再培養了天。隨後目測葉片 上之白粉病進展程度。 使用實例8:對抗胡瓜上之蒼耳單絲殼菌(胡瓜白粉病)的保 護性作用 、八有下文規&amp;之活性物質濃度之水性m喷灑盆栽 149027.doc -237· 201103430 胡瓜幼苗(處於胚層階段)葉直至溢流點。次日’以胡瓜白 粉病(蒼耳單絲殼菌)之孢子懸浮液噴灑處理組植物❶隨後 使植物返回溫室中 相對大氣濕度下再 展程度。 且在20與24°C之間的溫度及60至80%之 。養7天。隨後目測子葉上之白粉病進The mixture is prepared to prepare a dispersion T to stop microbial growth. The 匕 special edition agent often additionally contains a preservative to prevent the preparation of the preparation for injection, ', the aqueous solution and dispersion of the bacteria, and the preparation of the sterile solution and the dispersion liquid. The formulation must be sufficiently mobile to 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 water, ethanol, polyol (for example, 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 1 and 11 was demonstrated by the following experiment: Α) Microtiter test The active substance was separately formulated into a stock solution in disulfoxide (DMSO). 'The concentration is 10 000 ppm. Use Example 1: Activity against Phytophthora infestans in a microtiter test against a pathogen of late blight. Store the stock solution in a microtiter plate (MTP) and dilute it to the specified active substance using a pea juice-based aqueous nutrient medium for fungi. Agricultural degree. An aqueous suspension of zoospores of Phytophthora infestans is then added. Place the plate at 149027.doc -234- 201103430 at a temperature of 18. (: In a room where water vapor is saturated. Using an absorption photometer, Μτρ is measured at 405 nm on the 7th day after inoculation. The measured parameters are compared with the control variant without active substance (=1%%) The growth was compared and compared to the blank test values without the true and active substances to determine the relative growth % of the pathogen in the individual active substances. Example 2: In the microtiter test against P. Activity of the caused rice blast pathogen The stock solution is inhaled into a microtiter plate (MTp) and diluted to the specified active substance concentration using a malt-based aqueous nutrient medium for fungi. Subsequently, an aqueous suspension of spores of P. sphaeroides is added. The plate was placed in a water vapor-saturated chamber 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 not active. The growth of the control variants (= 1%) was compared and compared to the blank test values for fungi and active substances to determine the relative growth of the pathogen in the individual active substances. Example 3: In the microtiter test against the activity of the sclerotium plaque pathogen caused by the bacterium of the bacterium, the stock solution was inhaled into the microtiter plate (MTp) and the malt base for fungi was used. The aqueous nutrient medium is diluted to the specified active substance concentration. Subsequently, an aqueous suspension of spores of S. cerevisiae is added. The dish is placed in a water vapor-saturated chamber at a temperature of 18 ° C. Inoculation is carried out using an absorption photometer. The microtiter plate was then measured at 405 nm on day 7. The measured parameters were compared to the growth of the control variant (=1〇〇%) without active substance i and the blank without fungi and active substances The test values were compared to determine the relative growth % of the pathogen I49027.doc -235· 201103430 in individual active substances. B) Greenhouse test The active substance was formulated separately or together to form a stock solution containing 25 mg of active substance. / or a mixture of bismuth stone (DMSO) and emulsifier Wettol EM 3 1 (ethoxylated phenol based humectant with emulsification and dispersion) as solvent / emulsifier 99:1 Ratio thereof to make up 10 ml. The solution was then made up to 1 〇〇 ml with water. This stock solution was diluted with the solvent/emulsifier/water mixture to the concentration of active material given below. Use of Example 4 for protective application against the activity of P. oxysporum caused by Phytophthora infestans causes the growth of the plant seedlings in the pot. The plants are sprayed with an aqueous suspension containing the active substance concentrations specified below until overflowing. The next day, the treatment group was inoculated with an aqueous suspension of the Phytophthora infestans sporangia. Immediately after inoculation, the test plants were transferred to a humid chamber. After 6 days at a relative humidity of 丨8 to 2 (rc and close to 100%), the degree of fungal attack on the leaves was visually evaluated, expressed as % of diseased leaf area. Example 5: Against Puccinia striiformis on wheat (Therapeutic effect of wheat 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 high atmospheric humidity (90 to 95%). And indoors of 20-221 for 24 hours. During this period, the spores germinate and the germ tube penetrates into the leaf tissue. The secondary sputum sprays the infected plants with an aqueous suspension having the concentration of the active substance specified below until the overflow point. [S1 149027.doc • 236· 201103430 After drying the sprayed suspension, the test plants are 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 7 %. The degree of rust progression on the leaves was then visually observed. Use Example 6: Protective effect against Puccinia glabrata (wheat brown rust) on wheat Spray cultivar Ka with an aqueous suspension having the concentration of active substance specified below The basin of the "nzler": the leaves of the wheat seedlings were planted until the overflow point. The next day, the plants were sprayed with the spore suspension of wheat brown rust (Puccinia recondita). The plants were then placed in high atmospheric humidity (9〇 to 95). %)&amp;2〇_22t2 indoor 24 hours. In this period μ, spores germinate and the germ tube penetrates into the leaf tissue. The next day, the test plants are returned to the greenhouse and the temperature between 2〇 and 22. 65 to 7G% of the relative atmospheric humidity for another 7 days. Then visually measure the degree of progress of the disease on the leaf. Use Example 7 to protect the protective effect of wheat powdery mildew (wheat powdery mildew) on wheat with the following provisions The aqueous suspension of the active substance concentration is sprayed on the potted wheat seedling leaves of the cultivar Kanzler until the overflow point. The next day, the spore suspension of wheat powdery mildew (wheat powdery mildew) is sprayed with the plants, and then the plants are planted. Return to the greenhouse and the temperature between 2 (&gt; and depression) and 60 to 90% of the strokes were further incubated for the day under atmospheric humidity. Then the degree of powdery mildew progress on the leaves was visually observed. Example 8: Against the sage of the squash Ear monofilament The protective effect of the fungus (courgette powdery mildew), the water content of the active substance concentration of the following regulations &spray; spray pot 149027.doc -237· 201103430 The leaves of the cucurbit seedlings (at the stage of the germ layer) until the overflow point. The treated group of plants is sprayed with a spore suspension of the squash powdery mildew (Spirulina solani) and the plants are then returned to the greenhouse for re-expansion at relative atmospheric humidity. The temperature between 20 and 24 ° C and 60 to 80 %. Raise for 7 days. Then visually measure the powdery mildew on the cotyledons.

[SI 149027.doc 238[SI 149027.doc 238

Claims (1)

201103430 七、申請專利範圍: 1.式I及11之二π坐化合物,201103430 VII. Patent application scope: 1. Formula I and 11 bis π sitting compounds, A 其中 Ar Het 為可具有1、2、3 含有1、2或3個選 的 3- 、 4- 、 5- 、 6-雜環,其中該雜 R3 ; 或5個取代基R2之苯基,或為 =N、Ο及S之雜原子作為環成員 或?,員飽和、部分不飽和或芳族 了具有1、2、3或4個取代基 員有1 2或3個選自N、◦及S之雜原子作為環成 員的 3-、4-、5-、6 。 -或7-員飽和、部分不飽和或芳 族雜環,其中該雜環 _ .. ^ . 衣』具有1、2、3或4個取代基 R4 ; A 為可經1、2、3或4個取代基R5取代之直鏈 烷基橋; Y 為 0、S 或 NR6 ; R 係選自氫、α-(:10烷基、Cl_c10鹵烷基、匚2-(:10烯 基、C2-Ci〇鹵坤基、C2'Ci〇快基、C2_Ci〇齒快基、 環烷基、C3_C1()ii環烷基、苯基、苯基_Ci_ C4烷基,其中最後2個提及之基團中的苯基部分可 149027.doc 201103430 具有:、2、3、4或5個取代基R'及含有卜2或3 個選自及S之雜原子作為環成㈣5_或6_員飽 和、部为不飽和或芳族雜 a y 其中該雜環可具有 1、2或3個取代基1^ ;或 m為〇之情況下,亦可選 自-C(=0)R、-C(=s)r8、 R9R丨0、Μ及式in之基團 -CN、-P( Q)A wherein Ar Het is a 3-, 4-, 5-, 6-heterocyclic ring which may have 1, 2 or 3, wherein the heterocyclic R 3 ; or 5 substituent R 2 is phenyl, Or is the hetero atom of =N, Ο, and S as a ring member or? , saturated, partially unsaturated or aromatic, having 1, 2, 3 or 4 substituents having 12 or 3 heteroatoms selected from N, ◦ and S as ring members 3-, 4-, 5 -, 6 . a 7-membered saturated, partially unsaturated or aromatic heterocyclic ring wherein the heterocyclic ring has a 1, 2, 3 or 4 substituent R4; A is 1, 2, 3 or 4 linear alkyl bridges substituted with substituent R5; Y is 0, S or NR6; R is selected from hydrogen, α-(:10 alkyl, Cl_c10 haloalkyl, 匚2-(:10 alkenyl, C2 -Ci〇 〇 坤, C2'Ci 〇 fast radical, C2_Ci 〇 fast radical, cycloalkyl, C3_C1 () ii cycloalkyl, phenyl, phenyl _Ci_ C4 alkyl, of which the last two are mentioned The phenyl moiety in the group may be 149027.doc 201103430 having: 2, 3, 4 or 5 substituents R' and containing 2 or 3 heteroatoms selected from and S as a ring (4) 5_ or 6_ member Saturated, partially unsaturated or aromatic, ay, wherein the heterocyclic ring may have 1, 2 or 3 substituents; or m is oxime, may also be selected from -C(=0)R, -C (=s)r8, R9R丨0, Μ and the group of the formula in-CN, -P(Q) A (III) 其中 Ar、Het、A及Y係如式1及„中所定義;及 #為連接至分子其餘部分之連接點.A (III) wherein Ar, Het, A and Y are as defined in Formula 1 and „; and # is the point of attachment to the rest of the molecule. 係選自氫、CVCw烷基 Ci-C10 鹵烷基、C2_Cl〇烯 基、c2-c1G _烯基、c2_Cig快基、c2_CiG齒炔基、 匸3-匸10環烷基、(:3-(:1〇鹵環烷基、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r7,含有〖、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個取代基尺7,-^:^^!]^、 ^:”…、- S(0)2R8、-CN、-P(=Q) r9ri〇及 M ; LSI 149027.doc 201103430 各R2獨立地選自鹵素、〇H、SH、NO〗、CN、(:丨-(:4烷 基、CVC4鹵烷基、C2-C4烯基、C2-C4鹵烯基、c2-匚4快基、C2-C4 _快基、C3-C8環娱•基、C3-C8彘環 烷基、CVC4烷氧基、C「C4鹵烷氧基、CVC4烯氧 基、C1-C4鹵稀氧基、C1-C4炔氧基、(^-〇4鹵快氧 基、c3-c8環烷氧基、c3-c8鹵環烷氧基、Cl-C4烷 硫基、C1-C4鹵烧硫基、C1-C4稀硫基、C1-C4 1¾快 石·》»基、本基、苯基七丨-匚4烧基、苯基院氧 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ru ;含有 1、2或3個選自N、〇及8之雜原子作為環成員的% 4 5 或員飽和、部分不飽和或最大不飽 和雜環,其中該雜環可具有i、2或3個取代基尺11丨 C〇R 、COORl2、CONR13R14、NRnR14 及 s(o)pRU,其中上述基團中之脂族 或3個取代基r15 ^ 兵1P上述基團中之環脂族部分可 具有1、2或3個取代基尺10 ;或 連接於相鄰碳環历工l 衣原子上之兩個基團R2連同其所連 接之叙核原子— .6 .7 D 起形成部分不飽和或最大不飽和5- 或7-貝碳環, ^ μ ^ V. . . 5 3有i、2或3個選自0、S及Ν 〈雜原子作為環出 '6-^7 I μ 的部分不飽和或最大不飽和5- &amp;次7-員雜環;其 成 3個取代基R11 . 、 兔核或雜環可具有1、2或 各R3獨立地選自南素、 、SH ' N02、CN、C】_C4烷 I49027.doc 201103430 基、C1-C4鹵炫基、C2-C4稀基、C2-C4鹵歸基、匸 C4炔基、C2-C4鹵炔基、C3-C8環烷基、C3-c8 _環 炫基、C】-C4炫氧基、C1-C4鹵烧氧基、(^-〇4稀氣 基、C1-C4鹵稀氧基、C1-C4快氧基、C1-C4鹵炔氣 基、C3-C8環炫*氧基、C3-C8鹵環烧氧基、 硫基、C1-C4鹵院硫基、C1-C4稀硫基、齒休 硫基、苯基、苯基-C1-C4烧基、笨基燒氣 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R11 ;含有 1、2或3個選自N、Ο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’其中該雜環可具有1、2或3個取代基r 11 . COR12 ' COOR12 . conr13r14 . NR13R14AS(〇) R12,其中上述基團中之脂族部分可具有i、2或3個 取代基R15,其中上述基團中之環脂族部分可具有 1、2或3個取代基;或Is selected from the group consisting of hydrogen, CVCw alkyl Ci-C10 haloalkyl, C2_Cl nonenyl, c2-c1G-alkenyl, c2_Cig fast radical, c2_CiG alkynyl, 匸3-匸10 cycloalkyl, (: 3-( : 1 〇 halocycloalkyl, phenyl, phenyl _c "C4 alkyl, wherein the phenyl moiety in the last two mentioned groups may have 1, 2, 3, 4 or 5 substituents r7, containing 2, or 3, 5 or 6-membered saturated, partially unsaturated or aromatic heterocyclic rings selected from the group consisting of N, anthracene and S, wherein the heterocyclic ring may have 1, 2 or 3 substituents. Base rule 7, -^:^^!]^, ^:"..., -S(0)2R8, -CN, -P(=Q) r9ri〇 and M; LSI 149027.doc 201103430 Each R2 is independently selected from Halogen, hydrazine H, SH, NO, CN, (: 丨-(: 4 alkyl, CVC4 haloalkyl, C2-C4 alkenyl, C2-C4 haloalkenyl, c2-匚4 fast radical, C2-C4 _ fast base, C3-C8 ring entertainment base, C3-C8 fluorene cycloalkyl, CVC4 alkoxy, C "C4 haloalkoxy, CVC4 alkenyloxy, C1-C4 halooxy, C1-C4 alkyne Oxy, (^-〇4 halooxy, c3-c8 cycloalkoxy, c3-c8 halocycloalkoxy, Cl-C4 alkylthio, C1-C4 halogen-sulphur, C1-C4 sulfur Base, C1-C4 13⁄4 fast stone ·》» , a phenyl phenyl sulfonium group, a phenyl alkoxy group, a phenoxy group, a phenylthio group, wherein the phenyl moiety in the last five mentioned groups may have 1, 2, 3, 4 Or 5 substituents ru; % 4 5 or a saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, fluorene and 8 as ring members, wherein the heterocyclic ring may be Having i, 2 or 3 substituent bases 11丨C〇R, COORl2, CONR13R14, NRnR14 and s(o)pRU, wherein the aliphatic or the three substituents in the above group r15^兵1P are in the above group The cycloaliphatic moiety may have 1, 2 or 3 substituents of the base 10; or two groups R2 attached to the adjacent carbon ring calendar atom together with the nucleus to which it is attached - .6 .7 D Forming a partially unsaturated or maximally unsaturated 5- or 7-shell carbocyclic ring, ^ μ ^ V. . . 5 3 having i, 2 or 3 selected from 0, S and Ν <heteroatom as ring-out '6- ^7 I μ of partially unsaturated or maximally unsaturated 5 - &amp; 7-membered heterocyclic ring; which is 3 substituents R11 . , rabbit nucleus or heterocyclic ring may have 1, 2 or each R 3 independently selected from the south , SH, N02, CN, C] _C4 alkane I490 27.doc 201103430, C1-C4 halo, C2-C4, C2-C4 halo, 匸C4 alkynyl, C2-C4 haloalkynyl, C3-C8 cycloalkyl, C3-c8 _ ring Hyun, C]-C4 methoxy, C1-C4 halooxy, (^-〇4 dilute gas, C1-C4 halooxy, C1-C4 oxy, C1-C4 haloalkyne , C3-C8 cyclodextro-oxy, C3-C8 halocycloalkyloxy, thio, C1-C4 halogen thio, C1-C4 disulfide, dentate, phenyl, phenyl-C1- a C4 alkyl group, a phenoxy group, a phenoxy group, a phenylthio group, wherein the phenyl moiety in the last five mentioned groups may have 1, 2, 3, 4 or 5 substituents R11; 2 or 3 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or maximally unsaturated heterocyclic rings selected from heteroatoms of N, hydrazine and S as ring members wherein the heterocyclic ring may have 1 , 2 or 3 substituents r 11 . COR12 'COOR12 . conr13r14 . NR13R14AS(〇) R12, wherein the aliphatic moiety of the above group may have i, 2 or 3 substituents R15, wherein the ring in the above group The aliphatic moiety can have 1, 2 or 3 substituents; or SH、N〇2、CN、CVQ烷 烯基、c2-c4鹵烯基、c2- 149027.doc 201103430 C4炔基、c2-c4自炔基、(:3-(:8環烷基、c3-c8鹵環 炫基、c丨-C4烷氧基、Cl_C4鹵烷氧基、c丨-C4烯氧 基、Cnc4鹵烯氧基、Cl-c4炔氧基、C/C4鹵炔氧 基、c3-c8環烷氧基、c3-c8鹵環烷氧基、C〗-C4烧 碰基 C1-C4鹵院硫基、C1-C4婦硫基、(1:1-〇14_块 硫基、苯基、笨基-Cl-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 笨基部分可具有1、2、3、4或5個取代基R1!;含有 1、2或3個選自N、〇及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,其中該雜環可具有1、2或3個取代基Rn ;SH, N〇2, CN, CVQ alkenyl group, c2-c4 haloalkenyl group, c2-149027.doc 201103430 C4 alkynyl group, c2-c4 alkynyl group, (: 3-(:8-cycloalkyl group, c3- C8 halocyclyl, c丨-C4 alkoxy, Cl_C4 haloalkoxy, c丨-C4 alkenyloxy, Cnc4 haloalkenyloxy, Cl-c4 alkynyloxy, C/C4 haloalkoxy, c3 -c8 cycloalkoxy, c3-c8 halocycloalkoxy, C--C4 alkyl group C1-C4 halogen thiol, C1-C4 thiol, (1:1-〇14_block thio, Phenyl, phenyl-Cl-C4 alkyl, phenyl-Cl_C4 alkoxy, phenoxy, phenylthio, wherein the stupid moiety in the last five mentioned groups may have 1, 2, 3, 4 Or 5 substituents R1!; 3, 4, 4, 5, 6 or 7 containing 1, 2 or 3 heteroatoms selected from N, 〇 and S as ring members saturated, partially unsaturated or maximal a saturated heterocyclic ring wherein the heterocyclic ring may have 1, 2 or 3 substituents Rn; 1、2或3個取代基R16 ;或1, 2 or 3 substituents R16; or 各尺5獨立地選自鹵素、OH c】-c4齒炫基' C2-C4稀基' c 基、Ρr 甘Each ruler 5 is independently selected from the group consisting of halogen, OH c]-c4 dentate 'C2-C4 dilute base' c base, Ρr gan ,丞 ' 婦基、C2_Cj C1-C4炫氧基、c 、C1-C4鹵燒氧 c2-c4 _ 炔基、 I49027.doc 201103430 1 c4院硫基及CVC4南炫硫基’其中上述基團 中之脂族部分可具有i、2或3個取代基Rl5,·或 連接於兩個相鄰碳原子上的兩個基團R5連同其所 連接之碳原子-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j、 2、或3個選自〇、之雜原子作為環成員的3-、 6或7-員飽和、部分不飽和或最大不餘和 雜裱,其中該碳環或雜環可具有丨、2或3個取代基 R11 : R6係選自氫、CN、Cl_c4院基、Ci_c4 _院基、c2_c4 烯基、cvcu稀基、c2_c4炔基、c2_C4i炔基、 Cl_C4烷氧基、C1_C4鹵烷氧基、苯基、苯基 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&quot; ; c:〇R〗2、c〇〇Ri2、 C〇NRuR14及 s(〇)p r丨2 ; 各r7獨立地選自鹵素、OH、SH、NR丨3R14、CN、N02、 烧基、Ci-CUil 烧基、c2-C4 烯基、C2-C4 鹵烯 基、C2-C4块基、c2-C4齒炔基、CVC4炫氧基、CV 烧氧基、(VC4烷硫基&amp;(ν(: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 R15 ; R 係選自氫、C|'C10烷基、CVC丨〇鹵烷基、(^-(^烷 氧基、CVCk鹵烷氧基、CVCM胺基烷基、C3-C10 環烧基、C:3-C丨〇鹵環烷基、苯基、苯基 149027.doc [S1 201103430 基,其中最後2個提及基團中的笨基部分可具有 卜二小⑷個取代基^含有卜如個選自 N、0及S之雜原子作為環成員的5_或6•請和、部 分不飽和或芳族雜環,其中該雜環可具有i、… 個取代基R7,及NR13R14 ; R9及R1G彼此獨立地選自q-Cw烷基 Cl-Cl〇 鹵烧基、C,- c10稀基、c2-c10㈣基、c2_Ci〇块基、C2_Ci〇南快 基、c3-c1G環烷基、c3_ClQ_環烷基、燒氧 基、CVCw鹵烧氧基、Cl_c道敦基_CiCi。烧基、 Ci-C^烧氧基-Ci-Cio烧氧基、Cl_CiQ炫硫基、c〗_Ca 齒烧硫基、〇2-(:10烯氧基、c2_Ci〇稀硫基、c 炔氧基、c2-c1()炔硫基、c3_ClG環烧氧基、c3_Cic 環烷硫基、苯基、苯基-C^C:4烷基、苯硫基 '苯 基-CVC4烷氧基及NRnR14 ; 各R獨立地選自鹵素、OH、SH、NR13R14、CN、N〇2、 Ci-C4烧基、基、c2-c4烯基、c2-c4 齒烯 基、c2-c4炔基、c2-c4鹵炔基' CVCU烷氧基、CV C4鹵烷氧基、Ci-q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 R15 ; 各汉12獨立地選自氫、c〗-c4烷基、Ci-C4鹵烷基、c2-c4烯 基、c2-c4鹵烯基、CVC4胺基烷基、苯基、苯基-C1-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,及含有1、2或3 149027.doc 201103430 個選自N、0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 ; 各R13獨立地選自氫及&lt;^-(:8烷基; 各R14獨立地選自氫、C,-C8烷基、苯基及苯基_Ci_c4烷 基; 或R及R —起形成直鏈或Cs伸烷基橋或基團 -CH2CH2OCH2CH2-5t-CH2CH2NRI7CH2CH2-; 各R獨立地選自確基、CN、oh、、COR12、 COOR12、C0NRnRH ; nr13rI4、C3_c6環烧基、 (VC:6鹵環烷基、(:丨-(:4烷氧基、c丨_C4鹵烷氧基、 Cs-C6環烧氧基(cyci〇ai〇xy)、苯基及苯氧基; 各R獨立地選自石肖基、Cn、〇H、SH、COR丨2、 COOR·2、C0NRnRl4、nr13r14、Ci C4⑦基、^ C4鹵烷基、(:3-(:6環烷基、C3_C6鹵環烷基、Ci_C4 烷氧基、CrC4鹵烷氧基、c3-C6環烷氧基、苯基及 苯氧基; 各R丨7獨立地選自氫及Ci_c4烷基; Q 為〇或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、C「 c 10院基、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:函素、CN、硝基、烷基、C/C4鹵烷 149027.doc 14 201103430 m 基、(VC4院氧基、函燒氧基及取13Ri 為〇、1或2 ;及 P 為1或2 ; 及其農業上可接受之鹽。 2. 如請求们之式!及„之化合物,其中^為可具有卜2、 3“或5個取代基以之苯基,或為含有卜⑻個選自 N、〇及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R3。 3. 如請求項2之式认此化合物,其中^為可具有1、2、 3、4或5個’較佳丨、2或3個取代基以之苯基,或為選自 :比啶基、嘧啶基、吱痛基、噻吩基、吡咯基、吡唾基、 味唑基: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1、2、3或4 個,較佳1或2個取代基R3。 4·如請求項3之式1及II之化合物,其中Ar為可具有卜2、 :、4或5個’較佳丨、2或3個取代駐2之苯基,或為選自 基、噻吩基及噻唑基之5_或6_員雜芳環,較佳為吡 二Γ:該雜芳環可具有Η。或4個,較佳1或2個 5.=述請求項中任—項之式則之化合物,其中此為 3。 、2或3個選自Ν、Ο及S之雜原子作為環成員的5_或 6:貝雜芳環,其中該雜芳環可具有1、2、3或4個取代某 R 。 土 6·如請求項5之式咖之化合物,其中Het為選自^定基、 149027.doc 201103430 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弘戋 6-員雜芳環,其中該雜芳環可具有丨、2、3或4個,較佳工 或2個取代基R4。 7_如請求項6之式I及II之化合物,其中Het為選自吡啶基、 噻吩基及噻唑基之5-或6-員雜芳環,較佳為吡啶基,其 中痒雜芳環可具有1、2、3或4個,較佳丨或2個取代基 R4。 8. 如前述請求項中任一項之式1及π之化合物其中R2、r3 及R4彼此獨立地且每次出現時獨立地選自鹵素、OH、 SH、N〇2、CN、Ci-C^烧基、C^-C*函烧基、烧氧 基-C^C^烧基、C|-C4烧氧基、C|-C4烧氧基烧氧基 及CVC41|烷氧基,較佳選自氫、氟、氣、溴、Ci_c4^ 基、CVC4鹵烷基、(^-(^烷氧基及C|-c4鹵烷氧基。 9. 如前述請求項中任一項之式I及π之化合物,其中Rs係選 自c丨-c4烷基、c丨-c2鹵烷基、C〗-C4烷氧基、Ci-C2鹵烷氧 基、苯基、苯氧基及NR13R14,其中R13為氫,R&quot;係選自 氫、c「c4烷基及苯基,或及r&quot;均為Ci_c4烷基。 10. 如前述請求項中任一項之式1&amp;π之化合物,其中Rl係選 自氫、C〗-C4烷基、_C(=〇)R8、-S(0)2R8、_CN、Μ及式 ΠΙ之基團,較佳選自氫、曱基、乙基、丙基、異丙 基、-c(=〇)ch3、-C(==0)0CH3、_C(=0)N(CH3)2、CN、 式III之基團、鹼金屬陽離子及cu2+。 n_如前述請求項中任一項之式I及II之化合物,其中1113係選 [S] 149027.doc -10· 201103430 自氫、Crq烷基、_S(0)2R8及-C(=0)R8。 12_如前述請求項中任一項之式化合物,其中八為直 鏈C2或C3伸烷基橋’其中該伸烷基橋之丨或2個氫原子可 經1或2個取代基r5置換,其中各R5獨立地選自^-^烷 基、c丨-c4_烷基、Cl_C4烷氧基、Ci_C4烷氧基_c丨^烷 乳基及C!-C4鹵烧氧基’較佳選自甲基、乙基、曱氧基、 乙氧基及甲氧基曱氧基,或連接於相鄰碳原子上的兩個 取代基R5連同其所連接之碳原子一起形成環戊基或環己 基環。 13_如前述請求項中任一項之式I及化合物,其中γ為 0。 14.如前述請求項中任一項之式1及11之化合物,其中爪為〇。 15· —種式IV之化合物,, 丞' gynecological, C2_Cj C1-C4 decyloxy, c, C1-C4 halogenated oxygen c2-c4 _ alkynyl, I49027.doc 201103430 1 c4 hospital thiol and CVC4 sulphide thiol ' among the above groups The aliphatic moiety may have i, 2 or 3 substituents Rl5, or two groups R5 attached to two adjacent carbon atoms together with the carbon atom to which they are attached - form 3_, 4_, 5_, 6 _ or 7 members of saturated or unsaturated carbon rings, or containing 1, 2, or 3 heteroatoms selected from ruthenium, as a ring member, 3-, 6 or 7-member saturated, partially unsaturated or maximal And the heterocyclic ring, wherein the carbocyclic or heterocyclic ring may have an anthracene, 2 or 3 substituents R11: R6 is selected from the group consisting of hydrogen, CN, Cl_c4, Ke_c4 _ 院, c2_c4 alkenyl, cvcu, C2_c4 alkynyl, c2_C4i alkynyl, Cl_C4 alkoxy, C1_C4 haloalkoxy, phenyl, phenylalkyl, wherein the phenyl moiety in the last two mentioned groups may have 1, 2, 3, 4 or 5 substituents R&quot;; c: 〇R 〖2, c〇〇Ri2, C〇NRuR14 and s(〇)pr丨2; each r7 is independently selected from halogen, OH, SH, NR丨3R14, CN, N02 , burning base, Ci-CUil burning , c2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 block, c2-C4 alkynyl, CVC4 methoxy, CV alkoxy, (VC4 alkylthio &amp; (ν(:4) a haloalkylthio group wherein the aliphatic moiety of the above group may have 1, 2 or 3 substituents R15; R is selected from the group consisting of hydrogen, C|'C10 alkyl, CVC丨〇 haloalkyl, (^-( Alkoxy, CVCk haloalkoxy, CVCM aminoalkyl, C3-C10 cycloalkyl, C:3-C丨〇halocycloalkyl, phenyl, phenyl 149027.doc [S1 201103430 base, wherein The stupid base moiety in the last two mentioning groups may have a small (4) substituent, a hetero atom containing N, 0 and S as a ring member, or a partial or not a saturated or aromatic heterocyclic ring, wherein the heterocyclic ring may have i, ... substituents R7, and NR13R14; R9 and R1G are independently of each other selected from the group consisting of q-Cw alkyl Cl-Cl〇 haloalkyl, C, -c10 dilute Base, c2-c10(tetra)yl, c2_Ci〇 block, C2_Ci〇南快基, c3-c1G cycloalkyl, c3_ClQ_cycloalkyl, alkoxy, CVCw halooxy, Cl_cDowyl-CiCi. Ci-C^ alkoxy-Ci-Cio alkoxy group, Cl_CiQ sulphur group, c〗 _Ca tooth sulphur group, hydrazine 2-(:10 alkenyloxy, c2_Ci〇 dilute thio, c alkynyloxy, c2-c1()alkynylthio, c3_ClG cycloalkoxy, c3_Cic cycloalkylthio, phenyl, phenyl-C^C : 4 alkyl, phenylthio 'phenyl-CVC4 alkoxy and NRnR14; each R is independently selected from the group consisting of halogen, OH, SH, NR13R14, CN, N〇2, Ci-C4 alkyl, ke, c2-c4 Alkenyl, c2-c4 alkenyl, c2-c4 alkynyl, c2-c4 haloalkynyl CVCU alkoxy, CV C4 haloalkoxy, Ci-q alkylthio and (^-(:4halane) a thio group, wherein the aliphatic moiety in the above group may have 1, 2 or 3 substituents R15; each han 12 is independently selected from the group consisting of hydrogen, c--c4 alkyl, Ci-C4 haloalkyl, c2-c4 Alkenyl, c2-c4 haloalkenyl, CVC4 aminoalkyl, phenyl, phenyl-C1-C4 alkyl, wherein the phenyl moiety in the last two mentioned groups may have 1, 2, 3, 4 Or 5 substituents R11, and 5 or 6 membered saturated, partially unsaturated or aromatic heterocyclic rings containing 1, 2 or 3 149027.doc 201103430 heteroatoms selected from N, 0 and S as ring members The heterocyclic ring may have 1, 2 or 3 substituents R11; each R13 is independently selected from hydrogen and &lt;^-(:8 alkyl; each R14 is independently selected from hydrogen C,-C8 alkyl, phenyl and phenyl-Ci_c4 alkyl; or R and R together form a straight or Cs alkyl bridge or group -CH2CH2OCH2CH2-5t-CH2CH2NRI7CH2CH2-; each R is independently selected from Base, CN, oh, COR12, COOR12, C0NRnRH; nr13rI4, C3_c6 cycloalkyl, (VC: 6 halocycloalkyl, (: 丨-(:4 alkoxy, c丨_C4 haloalkoxy, Cs) -C6 cycloalkoxy (cyci〇ai〇xy), phenyl and phenoxy; each R is independently selected from the group consisting of schlossyl, Cn, 〇H, SH, COR丨2, COOR·2, C0NRnRl4, nr13r14, Ci C47 , C 4 haloalkyl, (: 3-(:6 cycloalkyl, C3_C6 halocycloalkyl, Ci_C4 alkoxy, CrC4 haloalkoxy, c3-C6 cycloalkoxy, phenyl and phenoxy) Each R丨7 is independently selected from hydrogen and Ci_c4 alkyl; 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, C"10 10, phenyl and benzyl, wherein the phenyl moiety of the last two mentioned groups may have 1, 2 or 3 substituents independently selected from the group consisting of: Nitro, alkyl, C/C4 halo 149027.doc 14 201103430 m base, (VC4, oxy, alkoxy and 13Ri are 〇, 1 or 2; and P is 1 or 2; and agriculturally acceptable salts thereof. 2. As requested! And a compound of „, wherein ^ is a phenyl group which may have 2, 3" or 5 substituents, or 5_ or 6_ containing a hetero atom selected from N, oxime and S as a ring member A heteroaromatic ring wherein the heteroaromatic ring may have 1, 2, 3 or 4 substituents R3. 3. Recognizing the compound as claimed in claim 2, wherein ^ is 1, 2, 3, 4 or 5 'preferably fluorene, 2 or 3 substituents phenyl, or selected from: pyridine Base, pyrimidinyl, anthraquinone, thienyl, pyrrolyl, pyridyl, oxazolyl: oxazolyl, isoxazolyl, thiazolyl, isothiazolyl and triazolyl 5- or 6-membered An aromatic ring wherein the heteroaryl ring may have 1, 2, 3 or 4, preferably 1 or 2 substituents R3. 4. A compound of formula 1 and II according to claim 3, wherein Ar is a phenyl group which may have 2, :, 4 or 5 'preferred oximes, 2 or 3 substituted groups 2, or selected from the group consisting of The 5- or 6-membered heteroaryl ring of the thienyl group and the thiazolyl group is preferably pyridinium: the heteroaryl ring may have an anthracene. Or 4, preferably 1 or 2 5. The compound of the formula of any one of the claims, wherein this is 3. And 2 or 3 5- or 6: bet-heterocyclic rings selected from the group consisting of a hetero atom of ruthenium, osmium and S as a ring member, wherein the heteroaromatic ring may have 1, 2, 3 or 4 substituents R. Soil 6. The compound of claim 5, wherein Het is selected from the group consisting of 149027.doc 201103430 pyrimidinyl, furyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isomer A 6-membered heteroaryl ring of oxazolyl, thiazolyl, isothiazolyl and triazolyl, wherein the heteroaryl ring may have fluorene, 2, 3 or 4, preferably 2 or 2 substituents R4. 7) A compound of the formulae I and II according to claim 6, wherein Het is a 5- or 6-membered heteroaryl ring selected from the group consisting of pyridyl, thienyl and thiazolyl, preferably pyridyl, wherein the itch heteroaryl ring is There are 1, 2, 3 or 4, preferably oxime or 2 substituents R4. 8. The compound of formula 1 and π according to any of the preceding claims, wherein R2, r3 and R4 are independently of each other and are each independently selected from the group consisting of halogen, OH, SH, N〇2, CN, Ci-C. ^Acetyl, C^-C* functional base, alkoxy-C^C^ alkyl, C|-C4 alkoxy, C|-C4 alkoxy alkoxy and CVC41|alkoxy Preferably, it is selected from the group consisting of hydrogen, fluorine, gas, bromine, Ci_c4^, CVC4 haloalkyl, (^-(^ alkoxy and C|-c4 haloalkoxy). 9. Formula according to any of the preceding claims a compound of I and π, wherein Rs is selected from the group consisting of c丨-c4 alkyl, c丨-c2 haloalkyl, C-C4 alkoxy, Ci-C2 haloalkoxy, phenyl, phenoxy and NR13R14 Wherein R13 is hydrogen, R&quot; is selected from the group consisting of hydrogen, c"c4 alkyl and phenyl, or r&quot; are both Ci_c4 alkyl. 10. A compound of formula 1 &amp; π according to any of the preceding claims, Wherein R1 is selected from the group consisting of hydrogen, C-C4 alkyl, _C(=〇)R8, -S(0)2R8, _CN, hydrazine and a hydrazine group, preferably selected from the group consisting of hydrogen, fluorenyl and ethyl. Propyl, isopropyl, -c(=〇)ch3, -C(==0)0CH3, _C(=0)N(CH3)2, CN, a group of formula III, an alkali metal cation, and cu2+. _ as requested above A compound of any of formulas I and II, wherein 1113 is selected from the group consisting of [S] 149027.doc -10·201103430 from hydrogen, Crq alkyl, _S(0)2R8 and -C(=0)R8. A compound of any one of the preceding claims, wherein the eighth is a linear C2 or C3 alkylene bridge, wherein the alkyl or two hydrogen atoms of the alkylene bridge may be replaced by one or two substituents r5, wherein each R5 Independently selected from the group consisting of ^-^alkyl, c丨-c4_alkyl, Cl_C4 alkoxy, Ci_C4 alkoxy-c丨^alkanyl and C!-C4 halooxyl is preferably selected from methyl The ethyl, decyloxy, ethoxy, and methoxymethoxy groups, or the two substituents R5 attached to adjacent carbon atoms, together with the carbon atom to which they are attached, form a cyclopentyl or cyclohexyl ring. The compound of the formula I and the compound of any one of the preceding claims, wherein γ is 0. 14. The compound of the formulae 1 and 11 according to any of the preceding claims, wherein the paw is ruthenium. Compound, 其中Ar、Het、Α及Υ係如請求項1至8及12至14中任一項 所定義。 16. —種農業組合物,其包含至少一種如請求項丨至丨5中任 一項之式I、II及/或IV之化合物或其農業上可接受之鹽 及液體或固體載劑。 17. —種如請求項ii15中任一項之式卜或…之化合物 149027.doc -11 - 201103430 的用途,其用於防治有害真菌。 〗8· 一f防治有害真菌之方法’其中該真菌、其棲息地或經 :、蒦乂免又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II及/或IV之化合物處理, 其中化合物I、II及工V係如請求項i至J 5令任一項所定 義。 、 19· -種種子,每100公斤種子包含〇1公克至1〇公斤量的至 J 一種式I、II及/或IV之化合物,其中化合物J、MW 係如請求項1至15中任一項所定義。 20. —種醫藥組合物,其包含至少一種如請求項丨至^中任 一項之式I、II及/或IV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。 21. —種如請求項1至15中任一項之式卜π&amp;/或^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。 2 2. —種治療癌症或病毋感染或對抗動物致病性或人類致病 性真菌之方法’其包含以至少一種如請求項1至15中任 一項之式I、II及/或IV之化合物、至少一種其醫藥學上 可接受之鹽或如請求項20之醫藥組合物治療有此需要之 個體。 149027.doc •12- 201103430 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 Ar, Het, Α and Υ are as defined in any one of claims 1 to 8 and 12 to 14. 16. An agricultural composition comprising at least one compound of formula I, II and/or IV according to any one of claims 1 to 5, or an agriculturally acceptable salt thereof, and a liquid or solid carrier. 17. The use of a compound of the formula ii15 or a compound of 149027.doc -11 - 201103430 for the control of harmful fungi. 〗 〖8. A method for controlling harmful fungi, wherein the fungus, its habitat or by:, remedy and fungal attack material or plant, or soil or reproductive material is at least an effective amount of Treatment with a compound of IV or IV, wherein compounds I, II and V are as defined in any one of claims i to J5. a seed containing from 1 g to 1 kg per 100 kg of seed to a compound of formula I, II and/or IV, wherein compound J, MW is as claimed in any of claims 1 to 15. Defined by item. 20. A pharmaceutical composition comprising at least one compound of formula I, II and/or IV according to any one of claims 1-4, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable Carrier. 21. The use of a compound of the formula π&amp;/or ^ or a pharmaceutically acceptable salt thereof according to any one of claims 1 to 15 for the preparation of a medicament for the treatment of cancer or a viral infection or For the preparation of anti-mold agents. 2 2. A method of treating a cancer or a disease infection or combating an animal pathogenic or human pathogenic fungus comprising at least one of formulas I, II and/or IV according to any one of claims 1 to 15. A compound, at least one pharmaceutically acceptable salt thereof, or a pharmaceutical composition according to claim 20, is used to treat an individual in need thereof. 149027.doc •12- 201103430 IV. Designated representative map: (1) The representative representative of the case is: (none) (2) The symbol of the symbol of the representative figure is simple: 5. If there is a chemical formula in this case, please reveal the best display. Chemical formula of the inventive feature: LSI 149027.docLSI 149027.doc
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