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51. 发明申请

WO1996025452A1 PRODUCTION OF A POLYMER COMPOSITION 审中-公开
标题翻译：生产聚合物组合物
公开(公告)号：WO1996025452A1
公开(公告)日：1996-08-22
申请号：PCT/GB1996000305
申请日：1996-02-12
申请人： ZENECA LIMITED , LIDDELL, John, Macdonald , GEORGE, Neil , TURNER, Peter, Deryck
发明人： ZENECA LIMITED
IPC分类号： C08J03/03
CPC分类号： C12P7/625 , C08G63/89 , C08J3/07 , C08J2367/04
摘要： A process of making a polyhydroxyalkanoate PHA latex comprises making a liquid-form solution of such PHA in a water soluble liquid and contacting that solution with water under shear. Suitably the solution is prepared at a temperature between the boiling point of water and 10 DEG C below the melting point of the PHA as measured by DSC for example by melt separating PHA from a microbiologicalsuspension thereof, dissolving it in the water soluble liquid, and then contacting the solution at over 100 DEG C with water at 50-95 DEG C. The water-soluble liquid may be for example 1,2-propandiol or a liquid more volatile than water such as ethanol, propanol or tertiary butanol. A surfactant may be present or added after contacting, for example one providing steric stabilisation such as an acrylic graft copolymer emulsifier.
摘要翻译：制备聚羟基链烷酸酯PHA胶乳的方法包括将这种PHA的液体形式的溶液制成水溶性液体，并在剪切下使该溶液与水接触。适当地，溶液在沸点水和低于PHA熔点10℃之间的温度下制备，例如通过DSC测量，例如通过将PHA与其微生物悬浮液熔融分离，将其溶解在水溶性液体中，然后在100℃以上的溶液与水在50-95℃下接触。水溶性液体可以是例如1,2-丙二醇或比水如乙醇，丙醇或叔丁醇更易挥发的液体。在接触之后可以存在或加入表面活性剂，例如提供空间稳定剂的表面活性剂，例如丙烯酸接枝共聚物乳化剂。

52. 发明申请

WO1996023812A1 PROLINE DERIVATIVES USEFUL AS INHIBITORS OF HUMAN LEUKOCYTE ELASTASE 审中-公开
标题翻译：丙泊酚衍生物作为人类白细胞抗原的抑制剂有用
公开(公告)号：WO1996023812A1
公开(公告)日：1996-08-08
申请号：PCT/GB1996000193
申请日：1996-01-30
申请人： ZENECA LIMITED
发明人： ZENECA LIMITED , BERNSTEIN, Peter, Robert , VEALE, Chris, Allan , DAVIES, Elwyn, Peter
IPC分类号： C07K05/083
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to particular forms of a novel 1-substituted-N-[2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide of formula (I) which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes pharmaceutical compositions containing such forms, processes for preparing the forms and intermediates useful in the synthesis of the forms.
摘要翻译：本发明涉及作为人类白细胞弹性蛋白酶（HLE）抑制剂的式（I）的新的1-取代-N- [2-甲基-1-（三氟乙酰基）丙基]吡咯烷-2-甲酰胺的具体形式，被称为人嗜中性粒细胞弹性蛋白酶（HNE），使得它们在需要这种抑制时是有用的，例如用于药物，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。本发明还包括含有这种形式的药物组合物，用于制备可用于合成形式的形式和中间体的方法。

53. 发明申请

WO1996022334A1 MONOAZO PIGMENTS 审中-公开
标题翻译： MONOAZO颜料
公开(公告)号：WO1996022334A1
公开(公告)日：1996-07-25
申请号：PCT/GB1995002833
申请日：1995-12-05
申请人： ZENECA LIMITED , CHORLTON, Alan, Patrick , MASON, James
发明人： ZENECA LIMITED
IPC分类号： C09B63/00
CPC分类号： C09B69/045 , C09B29/366 , C09B63/005 , C09B67/0029 , Y10S534/04
摘要： An azo pyrazolone compound of formula (1) in the form of a salt, and its use as a pigment.
摘要翻译：盐形式的式（1）的偶氮吡唑啉酮化合物及其作为颜料的用途。

54. 发明申请

WO1996022023A1 COMPOSITION AND USE 审中-公开
标题翻译：组成和使用
公开(公告)号：WO1996022023A1
公开(公告)日：1996-07-25
申请号：PCT/GB1995002951
申请日：1995-12-18
申请人： ZENECA LIMITED , AUSTIN, Peter, William
发明人： ZENECA LIMITED
IPC分类号： A01N43/80
CPC分类号： C07D275/04 , A01N43/80 , C08K5/0058 , C08K5/47
摘要： The use of a 2-(C3-5-alkyl)-BIT or 2-aralkyl-BIT such as 2-phenylethyl-BIT as a fungicide for plastics materials. 2-n-butyl-BIT is preferred.
摘要翻译：使用2-（C 3-8 - 烷基）-BIT或2-芳烷基-BIT如2-苯基乙基-BIT作为塑料材料的杀真菌剂。 2-正丁基-BIT是优选的。

55. 发明申请

WO1996020011A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO1996020011A1
公开(公告)日：1996-07-04
申请号：PCT/GB1995002991
申请日：1995-12-21
申请人： ZENECA LIMITED , TAYLORSON, Christopher, John , EGGELTE, Hendrikus, Johannes , TARRAGONA-FIOL, Antonio , RABIN, Brian, Robert , BOYLE, Francis, Thomas , HENNAM, John, Frederick , BLAKEY, David, Charles , MARSHAM, Peter, Robert , HEATON, David, William , DAVIES, David, Huw , SLATER, Anthony, Michael , HENNEQUIN, Laurent, François, André
发明人： ZENECA LIMITED
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K47/6899 , C12N9/48
摘要： Improved systems for targetted enzyme prodrug therapy, especially antibody directed enzyme prodrug therapy (ADEPT), in which the enzyme used is a mutated form of a host enzyme in which the natural host enzyme, such as ribonuclease, recognises its natural substrate by an ion pair interaction and this interaction is reversed ("reversed polarity") in the design of mutated enzyme and complementary prodrug.
摘要翻译：用于靶向酶前药治疗的改进的系统，特别是抗体定向酶前药治疗（ADEPT），其中使用的酶是宿主酶的突变形式，其中天然宿主酶如核糖核酸酶通过离子对识别其天然底物在突变酶和互补前药的设计中，相互作用被逆转（“反极性”）。

56. 发明申请

WO1996016960A1 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO1996016960A1
公开(公告)日：1996-06-06
申请号：PCT/GB1995002768
申请日：1995-11-28
申请人： ZENECA LIMITED , BARKER, Andrew, John
发明人： ZENECA LIMITED
IPC分类号： C07D403/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention concerns quinazoline derivatives of formula (I) wherein m is 1 or 2; each R includes hydrogen, halogeno, (1-4C)alkyl and (1-4C)alkoxy; n is 1, 2 or 3; each R includes hydrogen, hydroxy, halogeno and (1-4C)alkyl; and Ar is a 5- or 9-membered nitrogen-linked heteroaryl moiety containing up to four nitrogen heteroatoms, or Ar is a 5-, 6-, 9- or 10-membered nitrogen-linked unsaturated heterocyclic moiety containing up to three nitrogen heteroatoms which bears one or two substituents selected from oxo and thioxo; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物，其中m为1或2; 每个R 1包括氢，卤代，（1-4C）烷基和（1-4C）烷氧基; n为1,2或3; 每个R 2包括氢，羟基，卤代和（1-4C）烷基; 并且Ar是含有至多四个氮杂原子的5-或9-元含氮连接的杂芳基部分，或Ar是含有至多三个氮杂原子的5-，6-，9-或10-元含氮连接的不饱和杂环部分其具有一个或两个选自氧代和硫代的取代基; 或其药学上可接受的盐; 其制备方法，含有它们的药物组合物以及该化合物的受体酪氨酸激酶抑制性质用于治疗增殖性疾病例如癌症的用途。

57. 发明申请

WO1996015127A1 PYRIDAZINOQUINOLINE COMPOUNDS 审中-公开
标题翻译：吡啶并喹啉化合物
公开(公告)号：WO1996015127A1
公开(公告)日：1996-05-23
申请号：PCT/GB1995002613
申请日：1995-11-08
申请人： ZENECA LIMITED , BARE, Thomas, Michael , CHAPDELAINE, Marc, Jerome , DAVENPORT, Timothy, Wayne , EMPFIELD, James, Roy , GARCIA-DAVENPORT, Laura, Enid , JACKSON, Paul, Francis , McKINNEY, Jeffrey, Alan , McLAREN, Charles, David , SPARKS, Richard, Bruce
发明人： ZENECA LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to pyridazinoquinoline coumpounds of formulae A and A', wherein: ring A is chosen from an ortho fused aromatic or heteroaromatic five- or six-membered ring; R is selected from the group consisting of halo, (1-4C)alkyl, NO2, CN, (C1-3)perfluoroalkyl, OH, OCF3, (2-4C)alkenyl, (2-4C)alkynyl, O(1-4C)alkyl, NR'R", SO2NR'R", or SOmR'; R is selected from H, (1-6C)alkyl, or -(CH2)nL; R is selected from H or -(CH2)nL; L is a variety of substituents including phenyl, heterocyclic groups and heteroaryl; n is 0-6; m is 0-2, R is selected from H, (1-6C)alkyl or (1-6C)alkylaryl; R is selected from H or -(CO)R wherein R is selected from a variety of substituents including hydrogen, (1-12C)alkyl, pyridyl, phenyl, pyridyl (1-12C)alkyl and phenyl (1-4C)alkyl; and R' and R" are selected from H, (1-4C)alkyl, (3-6C)cycloalkyl, phenyl (0-4)alkyl-, heterocycle (0-4C)alkyl- or heteroaryl (0-4C)alkyl- to pharmaceutical compositions containing them and to methods for the treatment of neurological disorders utilizing them.
摘要翻译：本发明涉及式A和A'的哒嗪喹啉基团，其中：环A选自邻近稠合芳族或杂芳族五元或六元环; R 4选自卤素，（1-4C）烷基，NO 2，CN，（C 1-3）全氟烷基，OH，OCF 3，（2-4C）烯基，（2-4C）炔基，O （1-4C）烷基，NR'R“，SO2NR'R”或SOmR'; R 1选自H，（1-6C）烷基或 - （CH 2）n L; R 2选自H或 - （CH 2）n L; L是各种取代基，包括苯基，杂环基和杂芳基; n为0-6; m为0-2，R 5选自H，（1-6C）烷基或（1-6C）烷基芳基; R 3选自H或 - （CO）R 6，其中R 6选自多种取代基，包括氢，（1-12C）烷基，吡啶基，苯基，吡啶基（1-12C）烷基和苯基（1-4C）烷基; 并且R'和R“选自H，（1-4C）烷基，（3-6C）环烷基，苯基（0-4）烷基 - ，杂环（0-4C）烷基 - 或杂芳基（0-4C）烷基 - 含有它们的药物组合物和用于治疗利用它们的神经障碍的方法。

58. 发明申请

WO1996015116A1 HERBICIDAL PYRAZOLES 审中-公开
标题翻译：除草剂PYRAZOLES
公开(公告)号：WO1996015116A1
公开(公告)日：1996-05-23
申请号：PCT/GB1995002459
申请日：1995-10-18
申请人： ZENECA LIMITED , CHRYSTAL, Ewan, James, Turner , BARNETT, Susan, Patricia
发明人： ZENECA LIMITED
IPC分类号： C07D231/20
CPC分类号： C07D231/22 , A01N43/56
摘要： Compounds of formula (I) wherein: R is hydrogen, alkyl, alkenyl or alkynyl, any of which may optionally be substituted; R is alkyl, alkenyl or alkynyl, any of which may optionally be substituted, or OR or SOmR ; R is H, halogen, cyano, optionally substituted alkyl, alkenyl or alkynyl or OR or CO2R ; R is H, alkyl, alkenyl or alkynyl, any of which may optionally be substituted, halogen, cyano, nitro, CO2R , OR , NR R , NR SO2R , OSO2R or OmSR R R ; R , R and R are each independently H or alkyl, alkenyl or alkynyl, any of which may optionally be substituted; Y is halogen or cyano; each X is independently halogen, cyano, nitro, hydroxy, alkyl, alkoxy, alkylthio, alkoxyalkyl, SOmalkyl, CONR R or heterocyclyl or, alternatively, two X groups together or an X group and R may form a further ring; m is 0, 1 or 2; n is 0, 1 or 2; R and R are each independently hydrogen or lower alkyl; are active as herbicides.
摘要翻译：式（I）的化合物，其中：R 1是氢，烷基，烯基或炔基，其中任何一个可以任选被取代; R 2是烷基，烯基或炔基，其中任何一个可任选被取代，或OR 5或SOmR 5; R 3是H，卤素，氰基，任选取代的烷基，烯基或炔基或OR 5或CO 2 R 5; R 4是H，烷基，烯基或炔基，其中任何一个可以任选被取代，卤素，氰基，硝基，CO 2 R 5，OR 5，NR 5 R 6，NR 5 SO 2 R 6，OSO 2 R 5或OmSR 5 R 6 R 7; R 5，R 6和R 7各自独立地为H或烷基，烯基或炔基，其中任何一个可任选被取代; Y是卤素或氰基; 每个X独立地是卤素，氰基，硝基，羟基，烷基，烷氧基，烷硫基，烷氧基烷基，SOm烷基，CONR 8 R 9或杂环基，或者两个X基团或X基团和R 4可以形成另一个戒指; m为0,1或2; n为0,1或2; R 8和R 9各自独立地为氢或低级烷基; 作为除草剂具有活性。

59. 发明申请

WO1996014043A1 RESERVOIRS AND DELIVERY DEVICES 审中-公开
标题翻译：储存和运输设备
公开(公告)号：WO1996014043A1
公开(公告)日：1996-05-17
申请号：PCT/GB1995002564
申请日：1995-11-01
申请人： ZENECA LIMITED , GRAY, John, Martyn
发明人： ZENECA LIMITED
IPC分类号： A61J01/00
CPC分类号： A61J1/10 , A61J2205/10 , A61J2205/60 , A61J2205/70 , B65D33/004 , B65D2203/10 , G06K19/04 , G08B13/2408 , G08B13/2434 , G08B13/2471 , Y10S128/24
摘要： A passive reservoir for medicament in the form of a plastics bag (1), has a hanging eyelet (2) at its upper end and a lower outlet nozzle (3). The plastics bag (1) has bottom corners (4, 5), the left-hand right-angled corner (5) of which encapsulates a data carrier means (6) which carries data relating to a medicament contained or to be contained within the bag (1). The data carrier means is in the form of an electrically and/or magnetically operable device which can emit the data it is carrying in response to activation by a suitable field applied by an external reading device, which can cooperate with a delivery device to control the delivery to a patient of medicament when contained in the bag (1).
摘要翻译：用于塑料袋（1）形式的药物的被动储存器在其上端具有悬挂孔眼（2）和下出口喷嘴（3）。塑料袋（1）具有底角（4,5），其左角直角（5）封装了数据载体装置（6），该数据载体装置（6）承载与包含或包含在包（1）。数据载体装置是电和/或磁可操作装置的形式，其能够响应于由外部读取装置施加的合适的领域的激活而发射其携带的数据，该外部读取装置可与输送装置配合以控制当包装在袋（1）中时递送给患者药物。

60. 发明申请

WO1996010022A1 AMINOHETEROCYCLIC DERIVATIVES AS ANTITHROMBOTIC OR ANTICOAGULANT AGENTS 审中-公开
标题翻译：作为抗生素或抗凝剂的氨基酸衍生物
公开(公告)号：WO1996010022A1
公开(公告)日：1996-04-04
申请号：PCT/GB1995002285
申请日：1995-09-25
申请人： ZENECA LIMITED , FAULL, Alan, Wellington , MAYO, Colette, Marie , PRESTON, John , STOCKER, Andrew
发明人： ZENECA LIMITED
IPC分类号： C07D401/04
CPC分类号： C07D213/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
摘要： The invention concerns compounds of formula (I), wherein each of G , G and G is CH or N; m is 1 or 2; R includes hydrogen, halogeno and (1-4C)alkyl; M is a group of formula: NR -L -T R , in which R and R together form a (1-4C)alkylene group, L includes (1-4C)alkylene, and T is CH or N; A may be a direct link; M is a group of the formula: (T R )r-L -T R in which R is 0 or 1, each of T and T is CH or N, each of R and R is hydrogen or (1-4C)alkyl, or R and R together form a (1-4C)alkylene group, and L includes (1-4C)alkylene; M may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocyclic moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.
摘要翻译：本发明涉及式（I）化合物，其中G 1，G 2和G 3各自为CH或N; m为1或2; R 1包括氢，卤素和（1-4C）烷基; M 1是下式的基团：NR 2 -L 1 -T 1 R 3，其中R 2和R 3一起形成（1-4C）亚烷基，L 1包括（1-4C）亚烷基，T 1是CH或N; A可能是直接链接; M 2是下式的基团：（T 2 R 4）r L 2 -T 3 R 5其中R是0或1，每个T 2和T R 3和R 5分别是氢或（1-4C）烷基，或者R 4和R 5一起形成（1-4C）亚烷基，和L 2包括（1-4C）亚烷基; M 3可以直接连接到X; X包括磺酰基; 且Q包括萘基和杂环部分; 或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其作为抗血栓形成或抗凝血剂的用途。

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