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    • 91. 发明申请
    • OPTICAL SENSOR SYSTEM FOR THE DETERMINATION OF PH VALUES INDEPENDENTLY OF IONIC STRENGTH
    • 用于确定离子强度的PH值的光学传感器系统
    • WO1997015832A1
    • 1997-05-01
    • PCT/EP1996004426
    • 1996-10-11
    • NOVARTIS AGBARNARD, Steven, MarkBERGER, JosephROUILLY, MarizelWALDNER, Adrian
    • NOVARTIS AG
    • G01N33/84
    • G01N33/84C08F220/56G01N21/6428G01N2021/7786Y10T436/15
    • The invention relates to a polymer composition comprising pH-sensitive fluorescent dyes, to an ionic strength-independent optical sensor for pH value determination that contains the composition in the form of a membrane on a transparent support material, and to an optical process, according to the fluorescence method, that renders possible highly accurate pH value determination independently of the ionic strength of the test solution. The process is especially suitable for the determination of the pH value of physiological solutions, especially for the determination of the pH value of blood. The water-insoluble copolymer is composed of: a) from 39.9 to 60 % by weight of N,N-dimethylacrylamide or N,N-dimethylmethacrylamide; b) from to 60 to 39.9 % by weight of a monomer of formula (Ia) or (Ib) wherein Ra is hydrogen or C1-C6alkyl and Rb is C1-C12alkyl; c) from 0.1 to 0.7 % by weight of a proton-sensitive fluorophore which is either admixed with or covalently bonded to the polymer; and d) from 0 to 20 % by weight of a diolefinic crosslinking component, the sum of the percentage weights of a) to d) being 100 %.
    • 本发明涉及包含pH敏感性荧光染料的聚合物组合物,用于pH值测定的离子强度独立光学传感器,其包含透明载体材料上的膜形式的组合物和光学方法,根据 荧光法,其可以独立于测试溶液的离子强度使得可能的高度准确的pH值测定。 该方法特别适用于测定生理溶液的pH值,尤其适用于测定血液pH值。 水不溶性共聚物由以下组成:a)39.9〜60重量%的N,N-二甲基丙烯酰胺或N,N-二甲基甲基丙烯酰胺; b)从60至39.9重量%的式(Ia)或(Ib)的单体,其中R a是氢或C 1 -C 6烷基,R b是C 1 -C 12烷基; c)0.1至0.7重量%的质子敏感性荧光团,其与聚合物混合或共价键合; 和d)0至20重量%的二烯烃交联组分,a)至d)的百分比之和为100%。
    • 92. 发明申请
    • N-SULPHONYL AND N-SULPHINYL AMINO ACID DERIVATIVES AS MICROBICIDES
    • 作为微生物的N-磺酰基和N-磺酰氨基酸衍生物
    • WO1997014677A1
    • 1997-04-24
    • PCT/EP1996004349
    • 1996-10-07
    • NOVARTIS AGZELLER, Martin
    • NOVARTIS AG
    • C07C311/06
    • C07C311/06A01N41/06C07C307/06
    • alpha -Amino acid amides of formula (I) wherein the substituents are defined as follows: n is the number zero or one; R1 to R7 are as herein defined; R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl; R9 is C3-C8cycloalkyl; a C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl group substituted by one or more halogen atoms; or a group (a) wherein p and q are identical or different and are each independently of the other the number zero or one; and R13, R14, R15 and R16 are identical or different and are each independently of the others hydrogen or C1-C4alkyl; and X is hydrogen, in which case p and q must have the value zero; phenyl unsubstituted or mono- or poly-substituted by halogen, nitro, cyano, carboxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6haloalkyl, C3-C6alkenyloxy, C3-C6alkynyloxy, C3-C7cycloalkyl, C1-C6haloalcoxy, C1-C6alkylthio, C1-C6alcoxycarbonyl, C3-C6alkenyloxycarbonyl, C3-C6alkynyloxycarbonyl, C1-C6alkyl or by C1-C6alkoxy; cyano; -COOR17; -COR18 or a group (b) wherein R17 and R21 are each independently of the other hydrogen, C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl, and R18 is hydrogen; C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl or phenyl, unsubstituted or substituted by halogen, nitro, cyano, C1-C4alkyl or by C1-C4alkoxy, and R19 and R20 are identical or different and are each independently of the other hydrogen or C1-C4alkyl, are valuable microbicides. They can be used in plant protection in the form of suitable compositions, for example in the control of fungal diseases.
    • 式(I)的α-氨基酰胺,其中取代基定义如下:n是数字0或1; R1至R7如本文所定义; R8是C1-C6烷基,C3-C6链烯基或C3-C6炔基; R9为C3-C8环烷基; 被一个或多个卤素原子取代的C 1 -C 6烷基,C 3 -C 6烯基或C 3 -C 6炔基; 或其中p和q相同或不同并且各自独立于数字零或一个的基团(a); R 13,R 14,R 15和R 16相同或不同,各自独立地为氢或C 1 -C 4烷基; 并且X是氢,在这种情况下,p和q必须具有零值; 未被取代或被卤素,硝基,氰基,羧基,C 2 -C 6烯基,C 2 -C 6炔基,C 1 -C 6卤代烷基,C 3 -C 6烯氧基,C 3 -C 6炔氧基,C 3 -C 7环烷基,C 1 -C 6卤代烷氧基,C 1 -C 6烷硫基, C 1 -C 6烷氧基羰基,C 3 -C 6烯氧基羰基,C 3 -C 6炔氧基羰基,C 1 -C 6烷基或C 1 -C 6烷氧基; 氰基; -COOR17; -COR 18或其中R 17和R 21各自独立地为其它氢,C 1 -C 6烷基,C 3 -C 6烯基或C 3 -C 6炔基的基团(b),R 18为氢; C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基或苯基,未被取代或被卤素,硝基,氰基,C 1 -C 4烷基或C 1 -C 4烷氧基取代,R 19和R 20相同或不同,各自独立地为氢或 C1-C4烷基是有价值的杀菌剂。 它们可以以合适的组合物的形式用于植物保护,例如用于控制真菌疾病。
    • 94. 发明申请
    • IMPROVED INTEGRATION OF EXOGENOUS DNA DELIVERED TO EUKARYOTIC CELLS
    • 改进了提供给原核细胞的异源DNA的整合
    • WO1997012046A1
    • 1997-04-03
    • PCT/EP1996004006
    • 1996-09-12
    • NOVARTIS AGHANSEN, GenevièveCHILTON, Mary-Dell
    • NOVARTIS AG
    • C12N15/82
    • C12N15/8207C12N15/8201
    • The present invention provides an improved method for achieving stable integration of an exogenous DNA fragment in intact form into the genome of a eukaryotic cell, particularly a plant cell. The method comprises providing the exogenous DNA together with one or more proteins which promote integration of the exogenous DNA to the eukaryotic cell targeted for transformation, wherein the proteins are provided in the form of a chimeric gene or translatable RNA capable of expression in the eukaryotic cell. The method is particularly applied to plant cells to achieve stable integration of an exogenous DNA fragment bounded by T-DNA borders in intact form using integration-promoting proteins derived from Agrobacterium. Transgenic cultures, tissues and whole organisms, particularly transgenic plants, can be generated from cells transformed according to the method of the invention.
    • 本发明提供了一种改进的方法,用于将完整形式的外源DNA片段稳定整合到真核细胞,特别是植物细胞的基因组中。 该方法包括提供外源DNA与一种或多种促进外源DNA整合到靶向转化的真核细胞的蛋白质,其中蛋白质以能够在真核细胞中表达的嵌合基因或可翻译RNA的形式提供 。 该方法特别适用于植物细胞,以使用来自农杆菌的整合促进蛋白质以完整形式实现由T-DNA边界限制的外源DNA片段的稳定整合。 可以从根据本发明的方法转化的细胞产生转基因培养物,组织和整个生物,特别是转基因植物。
    • 95. 发明申请
    • NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES
    • 新的2,3-二氧代-1,2,3,4-四氢喹啉衍生物
    • WO1997008155A1
    • 1997-03-06
    • PCT/EP1996003644
    • 1996-08-19
    • NOVARTIS AGACKLIN, PierreALLGEIER, HansAUBERSON, YvesBIOLLAZ, MichelMORETTI, RobertOFNER, SilvioVEENSTRA, Siem, Jacob
    • NOVARTIS AG
    • C07D241/44
    • C07D401/06C07D241/44C07D401/12C07D417/12C07F9/650994
    • 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N (R8)(R9)-X-R7A (Id), -alk-O-X-R7 (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R7 and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.
    • 式(I)的2,3-二氧代-1,2,3,4-四氢 - 喹喔啉基衍生物,其中基团R 1和R 2之一是基团R 5,另一个是式-CH(R 6) -alk-R7(Ia),-alk-CH(R6-R7(Ib))-alk-N(R8)-X-R7(Ic),-alk-N +(R8)(R9)-X -R7A - (Id),-alk-OX-R7(Ie)或-alk-SX-R7(If),R3,R4和R5各自独立地为氢,低级烷基,卤素,三氟甲基,氰基 或硝基,R 6是未取代的或低级烷基化的和/或低级烷酰基化的氨基,R 7是氢;脂族,脂环族或杂环脂族基团;氰基;衍生自碳酸的酰基或来自碳酸的半酯或半酰胺, 脂族或芳族磺酸或磷酸或膦酸酯;未取代或脂族或芳烃取代和/或被脂族或芳族酰基取代的氨基;或芳族或杂芳族基团,R 8为氢; 脂肪族或芳脂族辐射 CAL; 或衍生自脂族或芳脂族羧酸的酰基或来自碳酸或R 7和R 8的脂族或芳脂肪族半酯与X以及键合R 8和X的氮原子形成未取代或取代的单 - 或二 - 氮杂环烷基的酰基, 氮杂环烷基,氮杂环烷基或任意氧化的经氮原子键合的硫代环烷基,或未取代或取代的,任选部分羟基化的芳基或杂芳基,R 9为脂族或芳脂族基,或者R 7,R 8和R 9与X和氮原子键合 R8,R9和X形成通过季氮原子键合的未取代或取代的季杂芳基,A 1是质子酸的阴离子,alk是低级亚烷基和X(除非与R 7和R 8一起 键合R8和X的氮原子或与R8,R9和X键合的氮原子一起形成所述环系中一个的一部分)是二价脂族,脂环族或芳族 脂肪族基团或直接键合,并且其药学上可接受的盐可用于制备用于治疗对阻断NMDA受体的AMPA,红藻氨酸和/或甘氨酸结合位点有反应的病理状况的药物。
    • 98. 发明申请
    • O-BENZYL OXIME ETHER DERIVATIVES AS PECTICIDES
    • WO1998028262A1
    • 1998-07-02
    • PCT/EP1997007122
    • 1997-12-18
    • NOVARTIS AGHÜTER, Ottmar, FranzFAROOQ, SaleemTRAH, StephanSZCZEPANSKI, Henry
    • NOVARTIS AG
    • C07C251/60
    • C07C251/40C07C251/34C07C251/38C07C251/60
    • Compounds of formula (I), wherein either X is CH or N, Y is OR1 and Z is O, or X is N, Y is NHR8 and Z is O, S or S(=O); U is (a) or (b); R1 is H or C1-C4alkyl; R2 is, for example, H, C1-C4alkyl or halo-C1-C4alkyl; R3 and R4 are, for example, H, C1-C4alkyl or C1-C4alkoxy; l is 0, 1 or 2; R5 and R6 are, for example, C1-C6alkyl, halo-C1-C6alkyl, C3-C6cycloalkyl, C3-C6cycloalkenyl, halo-C3-C6cycloalkyl, C1-C6alkoxy, halo-C1-C6alkoxy or C1-C6alkylthio; R55 is, for example, C1-C6alkyl, halo-C1-C6alkyl, C3-C6cycloalkyl or C3-C6cycloalkenyl; R66 is, for example, hydrogen, C1-C6alkyl, halo-C1-C6alkyl, C3-C6cycloalkyl, C3-C6cycloalkenyl, halo-C3-C6cycloalkyl, C1-C6alkylsulfinyl or halo-C1-C6alkylsulfinyl; m is 0, 1, 2, 3, 4, or 5; n is 0, 1, 2, 3 or 4; q is 0, 1, 2, 3 or 4; A is a direct bond, C1-C10alkylene, -C(=O)-, -C(=S)- or halo-C1-C10alkylene and R7 is a radical R10; or A is, for example, C1-C10alkylene and R7 is -CN, OR10, N(R10)2 or -S(=O)pR10; R8 is H or C1-C4alkyl; R9 is methyl, fluoromethyl or difluoromethyl; R10 is, for example, H, C1-C6alkyl, C2-C8alkenyl, C2-C8alkynyl or C3-C6cycloalkyl; and, where applicable, their possible E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in salt form, can be used as agrochemical active ingredients.
    • 式(I)化合物,其中X为CH或N,Y为OR 1,Z为O,X为N,Y为NHR 8,Z为O,S或S(= O); U是(a)或(b); R1是H或C1-C4烷基; R2是例如H,C1-C4烷基或卤代-C1-C4烷基; R3和R4是例如H,C1-C4烷基或C1-C4烷氧基; l为0,1或2; R 5和R 6是例如C 1 -C 6烷基,卤代-C 1 -C 6烷基,C 3 -C 6环烷基,C 3 -C 6环烯基,卤代-C 3 -C 6环烷基,C 1 -C 6烷氧基,卤代-C 1 -C 6烷氧基或C 1 -C 6烷硫基; R 55是例如C 1 -C 6烷基,卤代-C 1 -C 6烷基,C 3 -C 6环烷基或C 3 -C 6环烯基; R 66是例如氢,C 1 -C 6烷基,卤代-C 1 -C 6烷基,C 3 -C 6环烷基,C 3 -C 6环烯基,卤代-C 3 -C 6环烷基,C 1 -C 6烷基亚磺酰基或卤代-C 1 -C 6烷基亚磺酰基; m为0,1,2,3,4或5; n为0,1,2,3或4; q是0,1,2,3或4; A是直接键,C 1 -C 10亚烷基,-C(= O) - , - C(= S) - 或卤代-C 1 -C 10亚烷基,R 7是基团R 10; 或A为例如C 1 -C 10亚烷基,且R 7为-CN,OR 10,N(R 10)2或-S(= O)p R 10; R8是H或C1-C4烷基; R9是甲基,氟甲基或二氟甲基; R 10是例如H,C 1 -C 6烷基,C 2 -C 8烯基,C 2 -C 8炔基或C 3 -C 6环烷基; 并且如果适用,其可能的E / Z异构体,E / Z异构体和/或互变异构体的混合物,在每种情况下为游离形式或盐形式,可用作农业化学活性成分。