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    5-LIPOXYGENASE INHIBITORS
    1.
    发明申请
    5-LIPOXYGENASE INHIBITORS 审中-公开
    5-LIPOXYGENASE抑制剂

    公开(公告)号：WO2009146871A1

    公开(公告)日：2009-12-10

    申请号：PCT/EP2009/003906

    申请日：2009-06-01

    Applicant: JACKSON, William Paul

    Inventor： JACKSON, William Paul

    IPC: A61K31/18 ,  C07C311/21 ,  A61P35/00

    CPC classification number: A61K31/18 ,  C07C311/21 ,  C07C311/46

    Abstract: The use of compounds of the formula (I) Ar 1 -L 1 -Ar 2 -L 2 -C(R 3 )(R 4 )N(OR 1 )C(=Y)-R 2 (I) where Y is selected from O or S; R 1 is H, a salt or readily hydrolysable substituent; R 2 is selected from H or CH 3 , CH 2 F, CF 2 H or CF 3 ; R 3 and R 4 are selected independently from H, C 1-4 alkyl or alkenyl, CF 3 , CH 2 F, CF 2 H and F, with the proviso that if either R 3 or R 4 is H, then the other is not H; L 1 is a linker group; L 2 is a linker group comprising an optionally substituted or unsubstituted unsaturated branched or straight chain alkyl group; Ar 1 is an optionally substituted or unsubstituted aryl or heterocyclic group; and Ar 2 is an optionally substituted or unsubstituted aryl or heterocyclic group, in the treatment of 5-lipoxygenase mediated cancer provide improved therapies due to the effective inhibition of 5- lipoxygenase and long duration of activity in vivo after oral administration.

    Abstract translation: 使用式（I）Ar1-L1-Ar2-L2-C（R3）（R4）N（OR1）C（= Y）-R2（I）的化合物，其中Y选自O或S; R1是H，一种盐或易水解的取代基; R2选自H或CH3，CH2F，CF2H或CF3; R 3和R 4独立地选自H，C 1-4烷基或烯基，CF 3，CH 2 F，CF 2 H和F，条件是如果R 3或R 4是H，则另一个不是H; L1是连接基团; L2是包含任选取代或未取代的不饱和支链或直链烷基的连接基团; Ar 1是任选取代或未取代的芳基或杂环基; 并且Ar2是任选取代或未取代的芳基或杂环基，在5-脂氧合酶介导的癌症的治疗中，由于在口服给药后有效抑制5-脂氧合酶和长时间的活性，提供了改善的疗法。

    FLUID RECOVERY SYSTEM AND METHOD
    2.
    发明申请
    FLUID RECOVERY SYSTEM AND METHOD 审中-公开
    流体恢复系统和方法

    公开(公告)号：WO2006104982A2

    公开(公告)日：2006-10-05

    申请号：PCT/US2006/011037

    申请日：2006-03-28

    Applicant: J & J TECHNICAL SERVICES, L.L.C. ,  JACKSON, Thomas, Roland ,  JACKSON, William, Julius

    Inventor： JACKSON, Thomas, Roland ,  JACKSON, William, Julius

    IPC: E21B43/00

    CPC classification number: E21B43/124 ,  E21B43/121

    Abstract: A fluid recovery system (10) for collecting formation fluid at the surface of a well (12) includes a downhole jet pump (20) and a surface diaphragm pump (40) having a plurality of diaphragms (42). The jet pump includes a fluid nozzle (22), an intake (24) directing the formation fluid into a jet (26), a mixing tube (28) for mixing the power fluid and the formation fluid, and a diffuser (30) for converting the velocity of the mixed fluid to pressure. A flow meter (50) and a pressure sensor (52) monitor the quantity and pressure of the power fluid to the jet pump.

    Abstract translation: 用于在井（12）的表面处收集地层流体的流体回收系统（10）包括井下喷射泵（20）和具有多个隔膜（42）的表面隔膜泵（40）。 喷射泵包括流体喷嘴（22），将地层流体引导到射流（26）的入口（24），用于混合动力流体和地层流体的混合管（28），以及用于 将混合流体的速度转换成压力。 流量计（50）和压力传感器（52）监测动力流体对喷射泵的数量和压力。

    PROCESS FOR PREPARATION OF ARYL SUBSTITUTED PROPIONATE DERIVATIVES
    5.
    发明申请
    PROCESS FOR PREPARATION OF ARYL SUBSTITUTED PROPIONATE DERIVATIVES 审中-公开
    制备芳基取代的丙酸衍生物的方法

    公开(公告)号：WO1989005298A1

    公开(公告)日：1989-06-15

    申请号：PCT/AU1988000458

    申请日：1988-11-25

    Applicant: ICI AUSTRALIA OPERATIONS PROPRIETARY LIMITED ,  FUNG, Yik, Man ,  GREDLEY, Matthew ,  JACKSON, William, Roy ,  MATTHEWS, Barry, Ross

    Inventor： ICI AUSTRALIA OPERATIONS PROPRIETARY LIMITED

    IPC: C07D317/34

    CPC classification number: C07D317/34

    Abstract: A process for the preparation of a compound of formula (I) wherein Ar is selected from the group consisting of aryl, heteroaryl, substituted aryl and substituted heteroaryl; R is a carboxylic acid or ester or a group capable of being converted to a carboxylic acid or ester group; R is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl and substituted aryl; and X is halogen; which process comprises reacting a compound of formula (III) wherein R is selected from the group consisting of alkyl, aryl, substituted alkyl and substituted aryl, with a compound of formula R R R SiX wherein R , R , and R are independently chosen from alkyl and aryl.

    Abstract translation: 一种制备式（I）化合物的方法，其中Ar选自芳基，杂芳基，取代的芳基和取代的杂芳基; R是羧酸或酯或能够转化成羧酸或酯基的基团; R 1选自氢，烷基，取代的烷基，芳基和取代的芳基; X为卤素; 该方法包括使其中R 2选自烷基，芳基，取代的烷基和取代的芳基的式（III）化合物与式R 3 R 4 R 5的化合物反应， 其中R 3，R 4和R 5独立地选自烷基和芳基。

    AMIDINE COMPOUNDS
    7.
    发明申请
    AMIDINE COMPOUNDS 审中-公开
    氨基化合物

    公开(公告)号：WO2004033458A1

    公开(公告)日：2004-04-22

    申请号：PCT/AU2003/001329

    申请日：2003-10-09

    Applicant: MONASH UNIVERSITY ,  POLYCHIP PHARMACEUTICALS PTY LTD ,  JACKSON, William, Roy ,  SUBASINGHE, Kamani, Rupika

    Inventor： JACKSON, William, Roy ,  SUBASINGHE, Kamani, Rupika

    IPC: C07D489/02

    CPC classification number: C07D489/02

    Abstract: Amidine derivatives of opioids of the formula YN-X-(NH)n-C(=NR)-R' in which YN is a morphine-like opioid radical; X is a direct bond, a substituted or unsubstituted, branched, straight-chained or cyclic alkylene having from 1 to 6 carbon atoms, optionally containing one or two heteroatoms in the alkyl chain, or an optionally substituted, branched or straight-chained alkenylene having from 4 to 10 carbon atoms; R and R' are independently hydrogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, substituted alkyne, aryl, substituted aryl, heterocycle, substituted heterocycle or cyano; and n is 0 when X is said direct bond, or n is 1 when X is said alkylene or alkenylene. The compounds are effective in treating pain, and have effect in the peripheral nervous system, with comparably less or no activity in the central nervous system.

    Abstract translation: 式YN-X-（NH）n-C（= NR）-R'的阿片样物质的脒衍生物，其中YN是吗啡样阿片样物质; X是直接键，具有1至6个碳原子的取代或未取代的，支链的，直链或环状的亚烷基，任选地在烷基链中含有一个或两个杂原子，或任选取代的支链或直链亚烯基，其具有 4至10个碳原子; R和R'独立地是氢，烷基，取代的烷基，烯烃，取代的烯烃，炔烃，取代的炔烃，芳基，取代的芳基，杂环，取代的杂环或氰基; 当X为直接键时，n为0，X为所述亚烷基或亚烯基时，n为1。 这些化合物在治疗疼痛方面是有效的，并且在周围神经系统中具有作用，在中枢神经系统中具有相当少或没有活性。

    NOVEL BENZOTHIOPHENE COMPOUNDS AND METHODS
    10.
    发明申请
    NOVEL BENZOTHIOPHENE COMPOUNDS AND METHODS 审中-公开
    新型苯并噻吩化合物和方法

    公开(公告)号：WO1996028156A1

    公开(公告)日：1996-09-19

    申请号：PCT/US1996003350

    申请日：1996-03-12

    Applicant: ELI LILLY AND COMPANY ,  CARLSON, Donald, G. ,  CULLINAN, George, J. ,  FAHEY, Kennan, J. ,  JACKSON, William, T. ,  ROEHM, Neal, W. ,  SPAETHE, Stephen, M.

    Inventor： ELI LILLY AND COMPANY

    IPC: A61K31/38

    CPC classification number: C07D333/56 ,  A61K31/381

    Abstract: A method of inhibiting 5-lipoxygenase comprising administering to a mammal in need thereof an effective amount of a compound having formula (I), wherein R1 and R2 are independently hydrogen or C1-C6 alkyl; R3 is hydrogen, or a group of formula (a), wherein R4 is phenyl, substituted phenyl, naphthyl or substituted naphthyl, with the proviso that when R1 and R2 are both C1-C6 alkyl, R3 is not hydrogen; and pharmaceutically acceptable salts thereof.

    Abstract translation: 一种抑制5-脂氧合酶的方法，包括向有需要的哺乳动物施用有效量的具有式（I）的化合物，其中R 1和R 2独立地是氢或C 1 -C 6烷基; R 3是氢或式（a）的基团，其中R 4是苯基，取代的苯基，萘基或取代的萘基，条件是当R 1和R 2都是C 1 -C 6烷基时，R 3不是氢; 及其药学上可接受的盐。

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