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    • 32. 发明申请
    • HERBICIDAL COMPOSITIONS
    • 除草剂组合物
    • WO1996011574A1
    • 1996-04-25
    • PCT/EP1995003935
    • 1995-10-05
    • CIBA-GEIGY AGGLOCK, JuttaHUDETZ, ManfredKERBER, Elmar
    • CIBA-GEIGY AG
    • A01N43/90
    • A01N43/56A01N43/90A01N43/42A01N25/32A01N2300/00
    • Selective herbicidal compositions for controlling grasses and weeds in crops of cultivated plants, comprising: a) a herbicidally effective amount of a compound of formula (I), wherein R1 is the (i), (ii) or (iii) group; the substituents R4 are each independently of one another halogen, nitro, cyano, C1-C4alkyl, C1-C4haloalkyl, C1-C10alkoxy, C1-C4haloalkoxy, C3-C6alkenyloxy, C1-C4alkoxy-C2-C4alkoxy, C3-C6alkynyloxy, C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, C1-C4alkylthio, C1-C4alkylsulfinyl, C1-C4alkylsulfonyl, amino, C1-C4alkylamino or di-C1-C4alkylamino; R5 is the (iv) or (v) group; n is 0, 1, 2, 3 or 4; m is 0 or 1, the sum of m and n being 0, 1, 2, 3 or 4; q is 0, 1, 2 or 3; X1 is oxygen, sulfur, -CH2- or -N(R7)-; the substituents R6 are each independently of one another C1-C4alkyl, halogen, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy, nitro, cyano, C1-C4alkoxycarbonyl, amino, C1-C4alkylamino or di-C1-C4alkylamino; R7 is hydrogen, C1-C4alkyl, formyl or C1-C4alkylcarbonyl; A and B are each independently of one another hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl or cycloalkyl, or substituted or unsubstituted aryl; or A and B, taken together, form the divalent radical of a saturated or unsaturated and unsubstituted or substituted mono-, bi-, tri- or polycyclic system; G is hydrogen or a group -CO-R18 (a), (b), -SO2-R20 (c), (d), (e) or X (f); L and M are each independently of the other oxygen or sulfur; R18 is halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, polyalkoxyalkyl or cycloalkyl, which may contain hetero atoms; unsubstituted or substituted phenyl, unsubstituted or substituted phenylalkyl, substituted heteroaryl, substituted phenoxyalkyl, or substituted heteroaryloxyalkyl; R19 is halogen-substituted alkyl, alkenyl, alkoxyalkyl or polyalkoxyalkyl, or unsubstituted or substituted phenyl or benzyl; R20, R21 and R22 are each independently of one another unsubstituted or halogen-substituted alkyl, alkoxy, alkylamino, dialkylamino, alkylthio, alkenylthio, alkynylthio or cycloalkylthio, or unsubstituted or substituted phenyl, phenoxy or phenylthio; R23 and R24 are each independently of the other hydrogen, unsubstituted or halogen-substituted alkyl, alkenyl, alkoxy or alkoxyalkyl, unsubstituted or substituted phenyl or benzyl; or R23 and R24, taken together, form an alkenyl radical, which may contain oxygen as hetero atom; and X is a metal ion equivalent or an ammonium ion; as well as salts and diastereoisomers of the compounds of formula (I); and b) to antagonise the herbicide, an antidotally effective amount of either a quinoline derivative of formula (IIa), wherein R10 is hydrogen, C1-C8alkyl, or C1-C8alkyl which is substituted by C1-C6alkoxy or C3-C6alkenyloxy; and X2 is hydrogen or chloro; of a 1-phenylazole-3-carboxylic acid derivative of formula (IIb), wherein E is nitrogen or methine; R11 is -CCl3 or unsubstituted or halogen-substituted phenyl; R12 and R13 are each independently of the other hydrogen or halogen; and R14 is C1-C4alkyl, are particularly suitable for controlling weeds in crops of cultivated plants, in particular maize and cereals.
    • 选择性除草组合物,用于控制栽培植物作物中的草和杂草,包括:a)除草有效量的式(I)化合物,其中R1是(i),(ii)或(iii)基团; 取代基R 4各自独立地为卤素,硝基,氰基,C 1 -C 4烷基,C 1 -C 4卤代烷基,C 1 -C 10烷氧基,C 1 -C 4卤代烷氧基,C 3 -C 6烯氧基,C 1 -C 4烷氧基-C 2 -C 4烷氧基,C 3 -C 6炔氧基,C 1 -C 4烷基羰基 C1-C4烷氧基羰基,C1-C4烷硫基,C1-C4烷基亚磺酰基,C1-C4烷基磺酰基,氨基,C1-C4烷基氨基或二C1-C4烷基氨基; R5是(iv)或(v)组; n为0,1,2,3或4; m为0或1,m和n的和为0,1,2,3或4; q为0,1,2或3; X1是氧,硫,-CH2-或-N(R7) - ; 取代基R6各自独立地为C1-C4烷基,卤素,C1-C4卤代烷基,C1-C4烷氧基,C1-C4卤代烷氧基,硝基,氰基,C1-C4烷氧基羰基,氨基,C1-C4烷基氨基或二C1-C4烷基氨基; R 7是氢,C 1 -C 4烷基,甲酰基或C 1 -C 4烷基羰基; A和B各自独立地为氢,烷基,烯基,炔基,烷氧基烷基,烷硫基烷基或环烷基,或取代或未取代的芳基; 或A和B一起形成饱和或不饱和和未取代或取代的单,双,三或多环体系的二价基团; G是氢或-CO-R18(a),(b),-SO2-R20(c),(d),(e)或X(f) L和M各自独立地为其它氧或硫; R18是可以含有杂原子的卤素取代的烷基,烯基,烷氧基烷基,烷硫基烷基,聚烷氧基烷基或环烷基; 未取代或取代的苯基,未取代或取代的苯基烷基,取代的杂芳基,取代的苯氧基烷基或取代的杂芳基烷基; R19是卤素取代的烷基,烯基,烷氧基烷基或聚烷氧基烷基,或未取代或取代的苯基或苄基; R20,R21和R22各自独立地为未取代的或卤素取代的烷基,烷氧基,烷基氨基,二烷基氨基,烷硫基,烯硫基,炔硫基或环烷硫基,或未取代或取代的苯基,苯氧基或苯硫基; R 23和R 24各自独立地为氢,未取代或卤素取代的烷基,烯基,烷氧基或烷氧基烷基,未取代或取代的苯基或苄基; 或R 23和R 24一起形成可以含有氧作为杂原子的烯基; X为金属离子当量或铵离子; 以及式(I)化合物的盐和非对映异构体; 和b)拮抗除草剂,一种解药有效量的式(IIa)的喹啉衍生物,其中R 10是氢,C 1 -C 8烷基或被C 1 -C 6烷氧基或C 3 -C 6烯氧基取代的C 1 -C 8烷基; X2是氢或氯; 的式(IIb)的1-苯基唑-3-羧酸衍生物,其中E是氮或次甲基; R 11是-CCl 3或未取代的或卤素取代的苯基; R 12和R 13各自独立地为氢或卤素; 和R14是C1-C4烷基,特别适用于控制栽培植物,特别是玉米和谷类作物的杂草。
    • 34. 发明申请
    • MONONUCLEOTIDE AND DINUCLEOTIDE ANALOGUES AND INTERMEDIATES THEREFOR
    • 单核苷酸和胆固醇类似物及其中间体
    • WO1996007666A1
    • 1996-03-14
    • PCT/GB1995001986
    • 1995-08-21
    • CIBA-GEIGY AGIRVING, EdwardBAXTER, Anthony, DavidCOLLINGWOOD, Stephen, PaulTAYLOR, Roger, John
    • CIBA-GEIGY AG
    • C07H19/04
    • C07H23/00C07H19/06C07H21/00C07H21/04Y02P20/55
    • A compound of formula (I) or a pharmaceutically acceptable salt thereof, where R is hydrogen, R a or a group of formula (II), R a b or a protecting group Q, R b is C1-C20 alkyl, C2-C20 alkenyl, C3-C10 cycloalkyl, C6-C15 aryl, C7-C16 aralkyl or a 5- or 6- membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R is hydrogen, R a or -OR , provided that when R is hydrogen, R is R a or -OR , R a is a C1-C20 aliphatic group, a C3-C10 cycloaliphatic group, a C6-C15 aromatic group, a C7-C16 araliphatic group, or a 5- or 6- membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R is hydrogen, halogen, hydroxy, R , -OR , OSO2R , OCOR or tri(C1-C15 hydrocarbyl) silyloxy, R is R a or together with R denotes a valence bond, R a is hydrogen, halogen or R , R is hydrogen, halogen, hydroxy, R , -OR , -OCOR , OSO2R , or tri(C1-C15 hydrocarbyl) silyloxy, R is hydrogen, halogen or R , or together with R denotes a valence bond, R is hydrogen, or an atom or group capable of terminating a replicating strand of a nucleic acid or of inhibiting viral DNA synthesis, other than a group connected to the indicated furanose ring through an oxygen atom, or together with R denotes a valence bond, R is R a, or together with R denotes a valence bond, R a is hydrogen, halogen, hydroxy, R , -OR , -OCOR , -OSO2R or tri(C1-C15 hydrocarbyl) silyloxy, R is a monovalent nucleoside base radical, R is hydrogen or R a, R a is R , -COR , -SO2R or tri(C1-C15 hydrocarbyl)silyl, R is hydrogen, halogen, hydroxy, R , -OR , -OCOR , -OSO2R or Z, R is hydrogen, halogen or R . R is hydrogen or R a, R a is halogen, hydroxy, R , -OR , -OCOR , -OSO2R or tri(C1-C15 hydrocarbyl)silyloxy, R is a monovalent nucleoside base radical, R is hydrogen or R a, R a is a C1 to C10 aliphatic group, a C3 to C8 cycloaliphatic group, a C6 to C15 aromatic group or a C7 to C16 araliphatic group, R , R , R , R , R , R , R , R and R are independently a C1 to C10 aliphatic group, a C3 to C10 cycloaliphatic group, a C6 to C15 aromatic group or a C7 to C30 araliphatic group, and Z is substituted or unsubstituted C6 to C10 aryloxythiocarbonyloxy.
    • 式(I)化合物或其药学上可接受的盐,其中R 1是氢,R 1a或式(II)的基团,R 1'> a <= R 1> b或 保护基Q,R 1b是C 1 -C 20烷基,C 2 -C 20烯基,C 3 -C 10环烷基,C 6 -C 15芳基,C 7 -C 16芳烷基或被碳原子连接的5-或6-元杂环基 在指定的磷原子的杂环基中,R 2是氢,R 2 a或-OR 15,条件是当R 1是氢时,R 2是R 2 a或 -OR 15,R 2a是C 1 -C 20脂族基团,C 3 -C 10脂环族基团,C 6 -C 15芳族基团,C 7 -C 16芳脂族基团或5-或6-元杂环基团 通过杂环基中的碳原子与指定的磷原子连接,R 3是氢,卤素,羟基,R 16,-OR 16,OSO 2 R 16,OCOR 16或三(C 1 -C 6) -C 15烃基)甲硅烷氧基,R 4是R 4 a或与R 6一起代表价键,R 4是氢,卤素或R 17,R 5是氢, 卤素,羟基,R 18,-OR 18,-OCOR 18 ,OSO 2 R 18或三(C 1 -C 15烃基)甲硅烷氧基,R 6是氢,卤素或R 19,或与R 4一起代表价键,R 7是氢,或 可以终止核酸的复制链或抑制病毒DNA合成的原子或基团,除了通过氧原子与所示的呋喃糖环连接的基团,或与R 8一起,表示价键, R 8是R 8,或与R 7一起代表价键,R 8 a是氢,卤素,羟基,R 20,-OR 20,-OCOR 20, -OSO 2 R 20或三(C 1 -C 15烃基)甲硅烷氧基,R 9是一价核苷碱基,R 10是氢或R 10a,R 10a是R 21, -COR 21,-SO 2 R 21或三(C 1 -C 15烃基)甲硅烷基,R 11是氢,卤素,羟基,R 22,-OR 22,-OCOR 22, OSO 2 R 22或Z,R 12是氢,卤素或R 23。 R 13是氢或R 13 a,R 13是卤素,羟基,R 24,-OR 24,-OCOR 24,-OSO 2 R 24或三(C1- C 15烃基)甲硅烷氧基,R 14是单价核苷碱基,R 15是氢或R 15 a,R 15是C 1至C 10脂族基团,C 3至C 8脂环族基团, C 6至C 15芳族基团或C 7至C 16芳脂基基团,R 16,R 17,R 18,R 19,R 20,R 21,R 22, 23>和R 24独立地为C 1至C 10脂族基团,C 3至C 10脂环族基团,C 6至C 15芳族基团或C 7至C 30芳脂族基团,Z为取代或未取代的C 6至C 10芳氧基硫代羰基氧基。
    • 39. 发明申请
    • PROCESS FOR THE PREPARATION OF SPHERICAL MICROPARTICLES CONTAINING BIOLOGICALLY ACTIVE COMPOUNDS
    • 制备含有生物活性化合物的球形微生物的方法
    • WO1996003040A1
    • 1996-02-08
    • PCT/EP1995002727
    • 1995-07-12
    • CIBA-GEIGY AGNASTKE, RudolfNEUENSCHWANDER, Ernst
    • CIBA-GEIGY AG
    • A01N25/28
    • A01N25/28
    • The invention relates to a process for encapsulating biologically active compounds in the form of substantially spherical microparticles, comprising the steps of a) preparing an aqueous solution of surfactants, catalysts and monomers or prepolymers which are suitable for forming a crosslinked polycondensate, b) forming an emulsion of the substantially water-insoluble biologically active compound or mixture thereof in the solution a) by adding said solution under high shear force, and c) forming a solid capsule wall around the biologically active compound or mixture thereof by heating the reaction mixture to a temperature at which the crosslinking reaction takes place, which process comprises fusing the biologically active compound or mixture thereof and adding the melt to the aqueous reaction mixture at a temperature which is higher than the temperature of the reaction mixture. The invention further relates to the use of the microparticles for the preparation of a composition for controlling plant pests, weeds or animal parasites, as well as to aqueous spray mixtures, water-dispersible granulates or water-dilutable powders containing the claimed microparticles.
    • 本发明涉及以基本上为球形的微粒形式包封生物活性化合物的方法,其包括以下步骤:a)制备适于形成交联缩聚物的表面活性剂,催化剂和单体或预聚物的水溶液,b)形成 基本上不溶于水的生物活性化合物或其混合物在溶液中的乳液a)通过在高剪切力下加入所述溶液,和c)在生物活性化合物或其混合物周围形成固体胶囊壁,将反应混合物加热至 交联反应发生的温度,该方法包括熔融生物活性化合物或其混合物,并在高于反应混合物温度的温度下将熔体加入到水性反应混合物中。 本发明还涉及微粒用于制备用于防治植物害虫,杂草或动物寄生虫的组合物以及含有所要求保护的微粒的水性喷雾混合物,水分散性颗粒或水可稀释粉末的用途。