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    • 71. 发明申请
    • MONOAZO DYES CONTAINING A FLUOROSULPHONYL GROUP AND USE THEREOF
    • 含有荧光素团的MONOAZO染料及其用途
    • WO1995020014A1
    • 1995-07-27
    • PCT/GB1994002831
    • 1994-12-30
    • ZENECA LIMITEDHALL, Nigel
    • ZENECA LIMITED
    • C09B62/825
    • D06P3/8233C09B29/0003C09B29/0014C09B29/0025C09B29/0811C09B29/0838C09B29/095C09B29/10C09B29/36C09B62/825D06P3/26
    • A process for colouring a synthetic textile material or fibre blend thereof which comprises applying to the synthetic textile material a compound or mixture thereof, which is free from water solubilising groups, of the Formula (1) A-N=N-D, wherein: A and D each independently is an optionally substituted heterocyclic or carbocyclic group and at least one of A or D carries directly at least one -SO2F group or carries a substituent to which at least one -SO2F group is attached except for 4-(4-fluorosulphonylphenylazo)-N,N-dimethylaniline, provided that one of A or D is not 3,5-difluorosulphonylthien-2-yl, optionally substituted 1-phenyl-pyrazol-4-yl-5-one or (a) or that one of A or D does not carry an -NCH2CH(OH)CH2Cl, -NCOCH2Cl or -NCH2CH2SO2F substituent. The presence of one or more -SO2F groups in a dye molecule generally improves the properties of that dye and confers surprisingly good wet fastness and light fastness properties.
    • 合成纺织材料或其纤维混合物的着色方法,其包括向所述合成纺织品材料施用式(1)AN = ND的无水增溶基团的化​​合物或其混合物,其中:A和D各自 独立地是任选取代的杂环或碳环基团,并且A或D中的至少一个直接携带至少一个-SO 2 F基团或携带至少一个-SO 2 F基团连接的取代基,除了4-(4-氟磺酰基苯基偶氮)-N 的N-二甲基苯胺,条件是A或D中的一个不是3,5-二氟磺酰基噻吩-2-基,任选取代的1-苯基 - 吡唑-4-基-5-酮或(a)或A或D中的一个 不携带-NCH 2 CH(OH)CH 2 Cl,-NCOCH 2 Cl或-NCH 2 CH 2 SO 2 F取代基。 染料分子中一个或多个-SO 2 F基团的存在通常改善了该染料的性质,并赋予令人惊奇的良好的耐湿牢度和耐光性能。
    • 72. 发明申请
    • FREE RADICAL POLYMERISATION PROCESS
    • 自由放射聚合过程
    • WO1995017435A1
    • 1995-06-29
    • PCT/GB1994002769
    • 1994-12-20
    • ZENECA LIMITEDHADDLETON, David, MarkMUIR, Andrew, Victor, GrahamLEEMING, Stephen, William
    • ZENECA LIMITED
    • C08F02/38
    • C07F5/022C08F2/38
    • A compound for effecting molecular weight control in polymerisation is a CoII chelate of formula (I), wherein each group R is an organic cyclic group which, independently, is a monovalent group which comprises a cyclic structure or taken together as two adjacent groups provides a divalent group, and wherein further at least one of the groups R includes at least one heteroatom selected from O, N, S, P, halogen and Si, which heteroatom provides a substituent group or part of a substituent group on the cyclic structure, or a heteroatom of a heterocyclic ring of the cyclic structure; and wherein each group Q is independently selected from F, Cl, Br, OH, C1-12 alkoxy and C1-12 alkyl; or being a CoIII analogue of the cobalt II chelate of formula (I) in which the Co atom is additionally covalently bonded to H, a halide or other anion, or a homolytically dissociable organic group. Free-radical polymerisation of at least one ethylenically unsaturated monomer is carried out in the presence of such a compound.
    • 用于在聚合中进行分子量控制的化合物是式(I)的CoII螯合物,其中每个基团R是有机环状基团,其独立地是包含环状结构的一价基团或两个相邻的基团一起提供一个 并且其中所述基团R中的至少一个基团包含至少一个选自O,N,S,P,卤素和Si的杂原子,所述杂原子提供环状结构上的取代基或取代基的一部分,或 环状结构的杂环的杂原子; 并且其中每个基团Q独立地选自F,Cl,Br,OH,C 1-12烷氧基和C 1-12烷基; 或者是式(I)的钴II螯合物的CoIII类似物,其中Co原子另外共价键合到H,卤化物或其它阴离子或均分解离的有机基团。 至少一种烯键式不饱和单体的自由基聚合在这种化合物的存在下进行。
    • 76. 发明申请
    • FUNGICIDES
    • 杀菌剂
    • WO1995007022A1
    • 1995-03-16
    • PCT/GB1994001751
    • 1994-08-11
    • ZENECA LIMITEDCROWLEY, Patrick, JelfHEANEY, Stephen, PaulLAWSON, Kevin, RobertYOULE, David
    • ZENECA LIMITED
    • A01N37/44
    • A01N43/36A01N37/44A01N37/46A01N43/08A01N43/10A01N47/18C07C229/48C07C235/54C07C237/20C07C271/24C07C2601/08C07D207/16C07D307/24Y02P20/55
    • A method of combating fungi which comprises applying to a plant, to a seed of a plant or to the locus of a seed or plant a compound of formula (I), wherein X is O, S, SO, SO2, NR or CLM; A, B, D, E, L and M are, independently, hydrogen, halogen, alkyl, mono- or di-haloalkyl, benzyl (optionally substituted by halogen or haloalkyl) or hydroxy; A and B or D and E or L and M may together form a =S, =O or =CR R group; B and L or D and L may together form a bond; V is O or NR ; R and R are, independently, hydrogen or an amine protecting group; R , R and R are, independently, hydrogen, alkyl or benzyl; R and R are, independently, hydrogen, halogen, alkyl, phenyl, benzyl, alkoxy or acyloxy; or a salt thereof; provided that when X is CLM, R , R , R , A, M, D and E are all hydrogen, L and B are either both hydrogen or together form a bond, and V is O then the compound of formula (I) is in the form of a salt, but not a hydrochloride salt.
    • 一种防治真菌的方法,其包括向植物,植物种子或种子或植物的场所施用式(I)化合物,其中X为O,S,SO,SO 2,NR 8, 或CLM; A,B,D,E,L和M独立地为氢,卤素,烷基,单 - 或二 - 卤代烷基,苄基(任选被卤素或卤代烷基)或羟基取代; A和B或D和E或L和M可以一起形成= S,= O或= CR 6 R 7组; B和L或D和L可以一起形成键; V是O或NR 4; R 1和R 2独立地是氢或胺保护基; R 3,R 4和R 8独立地是氢,烷基或苄基; R 6和R 7独立地是氢,卤素,烷基,苯基,苄基,烷氧基或酰氧基; 或其盐; 条件是当X为CLM时,R 1,R 2,R 3,A,M,D和E均为氢,L和B均为氢或一起形成键,V为O 那么式(I)的化合物是盐的形式,而不是盐酸盐。
    • 77. 发明申请
    • FREE RADICAL POLYMERISATION PROCESS
    • 自由放射聚合过程
    • WO1995004759A1
    • 1995-02-16
    • PCT/GB1994001693
    • 1994-08-02
    • ZENECA LIMITEDHADDLETON, David, MarkMUIR, Andrew, Victor, Graham
    • ZENECA LIMITED
    • C08F02/38
    • C08F10/00C08F2/38
    • Process for the free-radical polymerisation of olefinically unsaturated monomer(s) using a free-radical initiator, wherein said polymerisation is performed in the presence of a compound for effecting molecular weight control, said molecular weight control compound being selected from Cobalt II chelates of formulae (I), (II) and (III), wherein: x and y are independently 2 to 5; each R , R , R and R is independently selected from H, C1-C12 alkyl, optionally substituted aryl, OR where R is C1 to C12 alkyl or optionally substituted aryl, CO2R , SO3H, C(=O)R , CO2H, NO2, OH, NR 2, NH2, NHR , SR , SH, CN, SO3R , halogen, 2-furyl and 3-furyl; each X is independently selected from (CR 2)n, (CR 2O)n, optionally substituted o-phenylene, and optionally substituted 1,8-naphthylene, where each R is independently selected from H and C1 to C12 alkyl, and n is 1 to 10; and wherein said cobalt chelates of formulae (I) and (II) possess a positive charge of 2 and are associated with an anion or anions for balancing the positive charge, while that of formula (III) is neutral; and also Co III analogues of said cobalt (II) chelates of formulae (I), (II) and (III) in which the Co atom is additionally covalently bonded, in a direction at right angles to the macrocyclic chelate ring system, to H, a halide ion or other anion, or a homolytically dissociatable organic group.
    • 使用自由基引发剂使烯属不饱和单体自由基聚合的方法,其中所述聚合在化合物存在下进行以进行分子量控制,所述分子量控制化合物选自钴 式(I),(II)和(III),其中:x和y独立地为2至5; 每个R 1,R 2,R 3和R 4独立地选自H,C 1 -C 12烷基,任选取代的芳基,OR 5,其中R 5是C 1至C 12烷基或 任选取代的芳基,CO 2 R 5,SO 3 H,C(= O)R 5,CO 2 H,NO 2,OH,NR 5,NH 2,NHR 5,SR 5,SH,CN,SO 3 R 卤素,2-呋喃基和3-呋喃基; 每个X独立地选自(CR 6)n,(CR 6 O)n,任选取代的邻亚苯基和任选取代的1,8-亚萘基,其中每个R 6独立地选自H 和C 1〜C 12烷基,n为1〜10; 并且其中所述式(I)和(II)的钴螯合物具有2的正电荷并且与用于平衡正电荷的阴离子相关联,而式(III)的中性; 以及所述式(I),(II)和(III)的所述钴(II)螯合物的Co III类似物,其中所述Co原子在与大环螯合环体系成直角的方向上额外共价键合至H ,卤化物离子或其它阴离子,或同解离的有机基团。
    • 79. 发明申请
    • ANILINE DERIVATIVES
    • 苯胺衍生物
    • WO1994029291A1
    • 1994-12-22
    • PCT/EP1994001808
    • 1994-06-03
    • ZENECA LIMITEDZENECA-PHARMA S.A.EDWARDS, Philip, Neil
    • ZENECA LIMITEDZENECA-PHARMA S.A.
    • C07D309/10
    • C07D405/12C07D309/10
    • The invention concerns an aniline derivative of formula (I) wherein R includes hydrogen and (1-4C)alkyl; R includes hydrogen and (1-4C)alkyl; R is hydrogen or (1-4C)alkyl; X includes a group of the formula CR R wherein R is hydrogen or (1-4C)alkyl and R is hydrogen or (1-4C)alkyl; A includes a direct link to X ; X includes thio and sulphonyl; Ar includes phenylene, which may be optionally substituted; R includes hydrogen and (1-4C)alkyl; and R and R together form a ring having 5 to 6 ring atoms including one oxygen atom, and which ring may bear one, two or three substituents, including methyl alpha to the oxygen atom; or a pharmaceutically acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    • 本发明涉及式(I)的苯胺衍生物,其中R 4包括氢和(1-4C)烷基; R 5包括氢和(1-4C)烷基; R 6是氢或(1-4C)烷基; X 3包括式CR 7 R 8的基团,其中R 7是氢或(1-4C)烷基,R 8是氢或(1-4C)烷基; A <1>包括与X <1>的直接链接; X 1包括硫代和磺酰基; Ar包括可以任选取代的亚苯基; R 1包括氢和(1-4C)烷基; 并且R 2和R 3一起形成具有5至6个环原子的环,包括一个氧原子,并且该环可以带有一个,两个或三个取代基,包括氧原子的甲基α; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物及其作为5-脂肪氧合酶抑制剂的用途。
    • 80. 发明申请
    • FLUORESCENCE ENERGY TRANSFER SUBSTRATES
    • 荧光能量转移基板
    • WO1994028166A1
    • 1994-12-08
    • PCT/GB1994001153
    • 1994-05-27
    • ZENECA LIMITEDGARMAN, Andrew, John
    • ZENECA LIMITED
    • C12Q01/37
    • G01N33/533C12Q1/37Y10S435/968
    • A method for the preparation of a fluorescence resonance energy transfer (FRET) substrate having donor and acceptor species on opposite sides of a proteolytic cleavage site and wherein the donor and/or acceptor species are attached via the side chain(s) of amino acid(s) therein. The method comprises contacting a reactive donor or acceptor species with a polypeptide substrate having the side chain(s) of amino acid(s) therein adapted for reaction with the reactive species and then contacting the substrate so obtained with a corresponding reactive donor or acceptor species. Novel FRET substrates so prepared and their use in assays to identify modulators of protease activity.
    • 一种用于制备在蛋白水解切割位点的相对侧具有供体和受体物质的荧光共振能量转移(FRET)底物的方法,其中供体和/或受体物质通过氨基酸的侧链( s)。 该方法包括使反应性供体或受体物质与其中具有适于与反应物质反应的氨基酸侧链的多肽底物接触,然后将如此获得的底物与相应的反应性供体或受体物质 。 新型FRET底物如此制备,并在测定中用于鉴定蛋白酶活性的调节剂。