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    • 71. 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。
    • 72. 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。
    • 73. 发明申请
    • POLYESTER COMPOSITION
    • 聚酯组合物
    • WO1994028061A1
    • 1994-12-08
    • PCT/GB1994001184
    • 1994-06-01
    • ZENECA LIMITEDHAMMOND, TimothyLIGGAT, John, JamiesonMONTADOR, James, HenryWEBB, Andrew
    • ZENECA LIMITED
    • C08K05/00
    • C08K5/0016C08L67/02C08L67/04C08L2666/02
    • Polyester composition comprising a biodegradable polyester and a plasticising quantity of at least one plasticiser selected from the group: high-boiling esters of polybasic acids; phosphoric acid drivatives; phosphorous acid derivatives; phosphonic acid derivatives; substituted fatty acids; high-boiling glycols, polyglycols, polyoxyalkylenes and glycerol each optionally substituted and optionally terminally esterified; pentaerythritols and derivatives; sulphonic acid derivatives; epoxy derivatives; chlorinated paraffins; polymeric esters; Wolflex-But3; provided that citrates does not include doubly esterified hydroxycarboxylic acids having at least 3 ester groups in its molecule and further provided that glycerols do not include glycerol triacetate and glycerol diacetate.
    • 包含可生物降解的聚酯和增塑量的至少一种增塑剂的聚酯组合物,其选自多元酸的高沸点酯; 磷酸驱动剂; 亚磷酸衍生物; 膦酸衍生物; 取代脂肪酸; 高沸点二醇,聚二醇,聚氧化烯和甘油,各自任选被取代并任选地被酯化; 季戊四醇及其衍生物; 磺酸衍生物; 环氧衍生物; 氯化石蜡; 聚合酯; Wolflex-But3; 条件是柠檬酸盐不包括其分子中具有至少3个酯基的双酯化羟基羧酸,并且进一步提供甘油不包括甘油三乙酸酯和甘油二乙酸酯。
    • 75. 发明申请
    • BICYCLIC ETHER DERIVATIVES AND THEIR USE AS 5-LIPOXYGENASE INHIBITORS
    • 双相醚衍生物及其作为5-LIPOXYGENASE抑制剂的用途
    • WO1994027999A1
    • 1994-12-08
    • PCT/EP1994001805
    • 1994-06-03
    • ZENECA LIMITEDZENECA-PHARMA S.A.EDWARDS, Philip, Neil
    • ZENECA LIMITEDZENECA-PHARMA S.A.
    • C07D493/08
    • C07D495/08
    • The invention concerns a bicyclic ether derivative of formula (I), wherein Ar is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur; A is a direct link to the group X or A is (1-4C)alkylene; X is oxy, thio, sulphinyl or sulphonyl; Ar is phenylene, pyridinediyl, pyrimidinediyl, thiophendiyl, furandiyl or thiazolediyl; and R is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; 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)的双环醚衍生物,其中Ar 1是苯基或萘基,或含有一个或两个氮杂原子并任选地含有另外选自氮,氧和硫的杂原子的10元双环杂环部分 ; A是直接连接到X基团或A是(1-4C)亚烷基; X是氧基,硫基,亚磺酰基或磺酰基; Ar 2是亚苯基,吡啶二基,嘧啶二基,噻吩二基,呋喃二基或噻唑二基; 并且R 1是(1-4C)烷基,(3-4C)烯基或(3-4C)炔基; 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
    • SUBSTITUTED FUSED PYRAZOLO COMPOUNDS AND THEIR USE AS HERBICIDES
    • 取代的FUSED PYRAZOLO化合物及其作为除草剂的用途
    • WO1994017062A1
    • 1994-08-04
    • PCT/GB1994000067
    • 1994-01-13
    • ZENECA LIMITED
    • ZENECA LIMITEDMICHAELY, William, JamesCURTIS, Jeff, KimoKNUDSEN, Christopher, Glade
    • C07D471/04
    • C07D471/04A01N43/90C07D487/04
    • Novel substituted pyrazolo-rings fused to nitrogen containing heterocyclic rings having formula (I) in which at least one of Y, Z or W is N or N-O and the remainder of Y, Z or W is C-R wherein R is hydrogen; halogen; nitro; cyano; alkyl; alkoxymethyl; acetoxymethyl; hydroxymethyl; haloalkyl; formyl; alkylcarbonyl; carboxy and its salts; COO alkyl; azido (N3); amino; substituted amino wherein the substituents are alkyl, alkoxy, hydroxy, formyl, alkylcarbonyl, alkoxycarbonylalkyloxy, alkoxycarbonylalkylthio, alkoxycarbonylalkylidenecarbonyl, hydroxycarbonylalkoxy, hydroxycarbonylthio, cyanoalkoxy, hydroxycarbonylalkyledinecarbonyl, alkylsufonyl, haloalkylsulfonyl, aminocarbonyl, (di)alkylaminocarbonyl, alkoxycarbonyl, alkoxyalkyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, and amino; carboxyamido; substituted carboxyamido wherein said substituents can be selected from alkyl, alkylsulfonyl, and haloalkylsulfonyl; sulfonamido wherein the N is substituted with hydrogen and/or alkyl; YR wherein Y is O and S(O)m and R is selected from the group hydrogen, alkyl, haloalkyl, cyanolalkyl, alkoxycarbonylalkyl, hydroxycarbonylalkyl and aminocarbonylalkyl wherein the N is substituted with hydrogen and/or alkyl; m is 0 to 2; R is hydrogen and halogen; R is hydrogen, nitro, halogen, cyano, alkylthio, alkylsulfinyl, alkylsulfonyl, and alkoxy; R is halogen, haloalkyl, cyano, alkylthio, alkylsulfinyl, and alkylsulfonyl; R is hydrogen and halogen; X is N or C-R ; wherein R is hydrogen, haloalkyl, halogen, cyano, nitro, alkylthio, alkylsulfinyl, alkylsulfonyl, and alkoxy; and agriculturally acceptable salts thereof.
    • 与式(I)的含氮杂环稠合的新型取代的吡唑并环,其中Y,Z或W中的至少一个为N或N-O,Y,Z或W的其余部分为C-R,其中R为氢; 卤素; 硝基; 氰基; 烷基; 烷氧基; 乙酰氧基; 羟甲基; 卤代; 甲酰基; 羰基; 羧基及其盐; COO烷基; 叠氮(N 3); 氨基; 取代的氨基,其中取代基是烷基,烷氧基,羟基,甲酰基,烷基羰基,烷氧基羰基烷氧基,烷氧基羰基烷硫基,烷氧基羰基亚烷基羰基,羟基羰基烷氧基,羟基羰基硫基,氰基烷氧基,羟基羰基烷基羰基,烷基磺酰基,卤代烷基磺酰基,氨基羰基,(二)烷基氨基羰基,烷氧基羰基,烷氧基烷基,羟基羰基烷基,烷氧基羰基烷基和 氨基; 羧酰胺; 取代的羧酰胺基,其中所述取代基可以选自烷基,烷基磺酰基和卤代烷基磺酰基; 其中N被氢和/或烷基取代; YR 6其中Y是O且S(O)m和R 6选自氢,烷基,卤代烷基,环烷醇烷基,烷氧基羰基烷基,羟基羰基烷基和氨基羰基烷基,其中N被氢和/或烷基取代; m为0〜2; R 1是氢和卤素; R 2是氢,硝基,卤素,氰基,烷硫基,烷基亚磺酰基,烷基磺酰基和烷氧基; R 3是卤素,卤代烷基,氰基,烷硫基,烷基亚磺酰基和烷基磺酰基; R 4是氢和卤素; X是N或C-R 5; 其中R 5是氢,卤代烷基,卤素,氰基,硝基,烷硫基,烷基亚磺酰基,烷基磺酰基和烷氧基; 和其农业上可接受的盐。