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    Imidazole derivatives and their use as hypercholesterolemia and hyperlipoproteinemia agents
    2.
    发明授权
    Imidazole derivatives and their use as hypercholesterolemia and hyperlipoproteinemia agents 失效
    咪唑衍生物及其用作高胆固醇血症和高脂蛋白血症的药物

    公开(公告)号：US5013749A

    公开(公告)日：1991-05-07

    申请号：US415917

    申请日：1989-10-02

    申请人： Nigel S. Watson ,  Chuen Chan ,  Barry C. Ross

    发明人： Nigel S. Watson ,  Chuen Chan ,  Barry C. Ross

    IPC分类号： C07D233/64 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61P3/00 ,  A61P9/00 ,  A61P9/10 ,  C07D233/54 ,  C07D233/60 ,  C07D401/04 ,  C07D405/06 ,  C07D405/14

    CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D405/06 ,  Y02P20/55

    摘要： Compounds of formula ##STR1## wherein R.sup.1 or R.sup.2 represents a C.sub.1-6 alkyl group optionally substituted by one to three halogen atoms and the other represents a phenyl or pyridyl ring or N-oxide thereof optionally substituted by one or more substituents selected from halogen atoms and hydroxyl, C.sub.1-3 alkyl, C.sub.1-3 alkoxy and trifluoromethyl groups; wherein R.sup.3 represents a phenyl or pyridyl ring or N-oxide thereof optionally substituted by one or more substituents selected from halogen atoms and hydroxyl, C.sub.1-3 alkyl, C.sub.1-3 alkoxy and trifluoromethyl groups with the proviso that only one of the groups R.sup.1, R.sup.2 or R.sup.3 represents an optionally substituted pyridyl ring; X represents --CH.dbd.CH--; and Z represents ##STR2## wherein R.sup.4 represents a hydrogen atom, a carboxyl protecting group or a cation; and R.sup.5 represents a hydrogen atom or a C.sub.1-3 alkyl group; a solvate thereof, or acid addition salts of compounds wherein R.sup.4 represents a hydrogen atom or a carboxyl protecting group; for use in the treatment and/or prevention of diseases associated with hypercholesteroloma and hyperlipoproteinemia.

    摘要翻译： 式（I）的化合物，其中R 1或R 2表示任选被一至三个卤素原子取代的C 1-6烷基，另一个表示任选被一个或多个取代基所取代的苯基或吡啶环或N-氧化物 卤素原子和羟基，C 1-3烷基，C 1-3烷氧基和三氟甲基; 其中R 3表示任选被一个或多个选自卤素原子和羟基，C 1-3烷基，C 1-3烷氧基和三氟甲基的取代基取代的苯基或吡啶环或N-氧化物，条件是只有一个基团R 1， R2或R3表示任选取代的吡啶环; X表示-CH = CH-; Z表示（a）或（b）其中R 4表示氢原子，羧基保护基或阳离子; R5代表氢原子或C1-3烷基; 其溶剂合物或其中R4表示氢原子或羧基保护基的化合物的酸加成盐; 用于治疗和/或预防与高胆固醇血症和高脂蛋白血症相关的疾病。

    Imidazole derivatives, pharmaceutical compositions and use
    3.
    发明授权
    Imidazole derivatives, pharmaceutical compositions and use 失效
    咪唑衍生物，药物组合物和用途

    公开(公告)号：US5112819A

    公开(公告)日：1992-05-12

    申请号：US593954

    申请日：1990-10-09

    申请人： Barry C. Ross ,  Barrie E. Kirk ,  Michael G. Lester ,  Panayiotis A. Procopiou ,  Nigel S. Watson

    发明人： Barry C. Ross ,  Barrie E. Kirk ,  Michael G. Lester ,  Panayiotis A. Procopiou ,  Nigel S. Watson

    IPC分类号： A61K31/415 ,  A61P3/06 ,  A61P9/10 ,  C07D233/54 ,  C07D233/64 ,  C07D401/04 ,  C07D405/06 ,  C07D413/06 ,  C07D413/14

    CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D405/06 ,  C07D413/06 ,  C07D413/14 ,  Y02P20/55

    摘要： Certain novel imidazole derivatives N-substituted by a vinyl group itself carrying a mevalonic acid derivative or corresponding lactone are inhibitors of HMG-CoA reductase and are useful for lowering blood plasma cholesterol levels.The compounds are of general formula (I): ##STR1## in which one of the groups R.sup.1 and R.sup.2 represents a C.sub.1-6 alkyl group optionally substituted by one to three halogen atoms and the other represents a phenyl ring optionally substituted by one to five substituents selected from halogen atoms and hydroxyl, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, S(O).sub.n C.sub.1-3 alkyl, (CH.sub.2).sub.m NR.sup.a R.sup.b, (CH.sub.2).sub.m NR.sup.c COR.sup.d and trifluoromethyl groups;R.sup.3 represents a phenyl ring optionally substituted by one to five substituents selected from halogen atoms and hydroxyl, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, S(O).sub.n C.sub.1-3 alkyl, (CH.sub.2).sub.m NR.sup.a R.sup.b, (CH.sub.2).sub.m NR.sup.c COR.sup.d and trifluoromethyl groups; with the proviso that at least one of the groups R.sup.1, R.sup.2 and R.sup.3 contains an S(O).sub.n C.sub.1-3 alkyl, (CH.sub.2).sub.m NR.sup.a R.sup.b or (CH.sub.2).sub.m NR.sup.c COR.sup.d substituent;X represents --CH.dbd.CH--;Z represents ##STR2## and physiologically acceptable solvates, physiologically acceptable acid addition salts thereof when R.sup.4 represents hydrogen or a physiologically acceptable and metabolically labile carboxyl protecting group when Z is (a), and quaternary ammonium derivatives thereof.

    Cyclic ketal derivatives
    4.
    发明授权
    Cyclic ketal derivatives 失效
    环状缩酮衍生物

    公开(公告)号：US5409950A

    公开(公告)日：1995-04-25

    申请号：US141061

    申请日：1993-10-26

    申请人： Michael J. Dawson ,  Allan Baxter ,  Robert M. Tait ,  Nigel S. Watson ,  David Noble ,  Alan Shuttleworth ,  Howard G. Wildman ,  Michael V. Hayes

    发明人： Michael J. Dawson ,  Allan Baxter ,  Robert M. Tait ,  Nigel S. Watson ,  David Noble ,  Alan Shuttleworth ,  Howard G. Wildman ,  Michael V. Hayes

    IPC分类号： A61K31/34 ,  A61P3/06 ,  A61P9/08 ,  A61P9/10 ,  A61P31/04 ,  C07D493/08 ,  C12N1/00 ,  C12N9/99 ,  C12P17/18 ,  C12R1/00 ,  A61K31/335 ,  C07D311/00

    CPC分类号： C07D493/08 ,  C12P17/181 ,  Y10S435/911

    摘要： Compounds are described of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a hydroxyl group or a group selected from --OCOCH.dbd.CHCH(CH.sub.3)(CH.sub.2).sub.3 CH.sub.3, --OCOCH.dbd.CHC(CH.sub.3).dbd.CHCH(CH.sub.3)--CH.sub.2 CH.sub.3, or --OCO--X--CH.sub.2 CH(CH.sub.3)CH.sub.2 CH.sub.3 [where X is --CH.dbd.CHCH(CH.sub.3)--, --CH.sub.2 CH(OH)CH(CH.sub.3)--, --CH.dbd.CHC(OH)(CH.sub.3)--, --CH.sub.2 CH(OH)CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH(CH.sub.3)--)];R.sub.2 represents a hydrogen atom or a hydroxyl group;R.sub.3 represents a group selected from --C(.dbd.CH.sub.2)CH(OR.sub.7)CH(CH.sub.3)CH.sub.2 Ph (where R.sub.7 is a hydrogen atom or an acetyl group), --C(CH.sub.3).dbd.CHCH(CH.sub.2 R.sub.8)CH.sub.2 Ph (where R.sub.8 is a hydrogen or a hydroxyl group), --C(CH.sub.2 OH).dbd.CHCH(CH.sub.3)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(OH)CH(CH.sub.2 OH)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(NHCOCH.sub.3)CH(CH.sub.3)CH.sub.2 Ph, --C(CH.sub.2 NHCOCH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph or ##STR2## R.sub.4, R.sub.5 and R.sub.6 may each independently represent a hydrogen atom or a methyl group and salts thereof; with the proviso that when either of R.sub.1 and R.sub.2 represents a hydrogen atom R.sub.3 is a group selected from --C(.dbd.CH.sub.2)CH(OR.sub.7)CH(CH.sub.3)CH.sub.2 Ph and --C(CH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph and when both of R.sub.1 and R.sub.2 represent hydrogen atoms R.sub.3 represents --C(CH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph.These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.

    摘要翻译： 描述式（I）的化合物，其中R 1表示氢原子，羟基或选自-OCOCH = CHCH（CH 3）（CH 2）3 CH 3，-OCOCH = CHC（CH 3）= CHCH（CH 3） ）-CH 2 CH 3或-OCO-X-CH 2 CH（CH 3）CH 2 CH 3 [其中X是-CH = CHCH（CH 3） - ， - CH 2 CH（OH）CH（CH 3） - ， - CH = CHC（OH） ，-CH 2 CH（OH）CH 2 - 或-CH 2 CH 2 CH（CH 3） - ）]; R2表示氢原子或羟基; R3表示选自-C（= CH2）CH（OR7）CH（CH3）CH2Ph（其中R7为氢原子或乙酰基），-C（CH3）= CHCH（CH2R8）CH2Ph（其中R8为 氢或羟基），-C（CH2OH）= CHCH（CH3）CH2Ph，-C（= CH2）CH（OH）CH（CH2OH）CH2Ph，-C（= CH2）CH（NHCOCH3）CH（CH3） ，-C（CH 2 NHCOCH 3）= CHCH（CH 3）CH 2 Ph或R 4，R 5和R 6可各自独立地表示氢原子或甲基及其盐; 条件是当R 1和R 2中的任一个表示氢原子时，R 3是选自-C（= CH 2）CH（OR 7）CH（CH 3）CH 2 Ph和-C（CH 3）= CHCH（CH 3）CH 2 Ph的基团，当两者 的R 1和R 2表示氢原子，R 3表示-C（CH 3）= CHCH（CH 3）CH 2 Ph。 这些化合物抑制角鲨烯合酶和/或用于制备抑制酶角鲨烯合酶的化合物的中间体。 本发明的化合物可以配制用于各种病症，其中动物血浆中胆固醇水平的降低将是有益的并且用于抵抗动物中的真菌感染。

    Valve with different configurations for different uses
    7.
    发明授权
    Valve with different configurations for different uses 有权
    不同配置的阀门用于不同用途

    公开(公告)号：US6065487A

    公开(公告)日：2000-05-23

    申请号：US197789

    申请日：1998-11-23

    申请人： Nigel S. Watson

    发明人： Nigel S. Watson

    IPC分类号： F16K31/42 ,  F16K11/02

    CPC分类号： F16K31/426 ,  Y10T137/5283 ,  Y10T137/86614 ,  Y10T137/8671

    摘要： A valve having a valve body with an elongated opening therein and having a first end and a second end. A valve member is slidably disposed in the elongated opening. First, second and third ports are in fluid communication with the opening in the valve body at times. One of the first, second and third ports have a supply of fluid under pressure connected thereto. A first passage is disposed in the valve body and leads from the first port to the second end thereof. A second passage is disposed in the valve body and leads from the second port to the second end thereof. A third passage is disposed in the valve body and leads from the third port to the second end thereof. An actuator body is adapted to be connected to the valve body and has a cavity therein. The actuator body has a first end adjacent to the second end of the valve body. An actuator is disposed in the cavity. The actuator has a first side and a second side and is moveable between a first and a second position thereof for moving the valve member. A fluid passageway is disposed in the actuator body and leads from the first end of the actuator body to a position on the second side of said actuator and is adapted to be selectively connected in one of a first, second and third configuration at any one time to one of the first, second and third passages and is adapted to be connected to any one of the first, second and third passages of a user's choosing.

    摘要翻译： 一种具有在其中具有细长开口的阀体并具有第一端和第二端的阀。 阀构件可滑动地设置在细长开口中。 首先，第二和第三端口有时与阀体中的开口流体连通。 第一，第二和第三端口中的一个具有与其连接的压力下的流体供应。 第一通道设置在阀体中并从第一端口引导到第二端。 第二通道设置在阀体中并从第二端口引导到其第二端。 第三通道设置在阀体中并从第三端口引导到第二端。 致动器主体适于连接到阀体并且在其中具有空腔。 致动器主体具有与阀体的第二端相邻的第一端。 致动器设置在空腔中。 致动器具有第一侧和第二侧，并且可在其第一和第二位置之间移动，用于移动阀构件。 流体通道设置在致动器主体中并且从致动器本体的第一端引导到所述致动器的第二侧上的位置，并且适于在任何一个时间选择性地连接在第一，第二和第三构造之一中 到第一，第二和第三通道中的一个，并且适于连接到用户选择的第一，第二和第三通道中的任何一个。

    System for holding a linear motion guide track to a support base and method therefor
    8.
    发明授权
    System for holding a linear motion guide track to a support base and method therefor 有权
    用于将直线运动导轨保持在支撑座上的系统及其方法

    公开(公告)号：US08608383B2

    公开(公告)日：2013-12-17

    申请号：US12939804

    申请日：2010-11-04

    申请人： Nigel S. Watson

    发明人： Nigel S. Watson

    IPC分类号： F16C19/00

    CPC分类号： F16C29/004 ,  F16C29/005 ,  F16C29/045 ,  Y10T29/49826 ,  Y10T403/7064

    摘要： A system for securing a linear motion guide track (1010) to a support extrusion (1030) comprises an elongated wedge (1040) having a protrusion configured for insertion in a slit in one side of the well of the support extrusion for positioning the wedge in the well, the wedge having deformable teeth on a side opposite the protrusion such that insertion of the guide track in the well deforms the teeth of the wedge thereby securely holding the guide track in the support extrusion.

    摘要翻译： 用于将直线运动导轨（1010）固定到支撑挤压件（1030）的系统包括细长楔形物（1040），其具有突出部，该突起被构造成用于插入在支撑挤压件的孔的一侧中的狭缝中，用于将楔定位在 井，在与突起相对的一侧具有可变形的齿，使得导轨在井中的插入使楔的齿变形，从而将导轨牢固地保持在支撑挤压中。

    System, Method, and Apparatus for Holding a Track to a Base
    9.
    发明申请
    System, Method, and Apparatus for Holding a Track to a Base 有权
    用于将轨道保持在基座上的系统，方法和装置

    公开(公告)号：US20110110616A1

    公开(公告)日：2011-05-12

    申请号：US12939804

    申请日：2010-11-04

    申请人： Nigel S. Watson

    发明人： Nigel S. Watson

    IPC分类号： F16C29/00 ,  F16C33/10 ,  F16C43/04 ,  F16C33/30 ,  F16B7/04 ,  B23P11/00

    CPC分类号： F16C29/004 ,  F16C29/005 ,  F16C29/045 ,  Y10T29/49826 ,  Y10T403/7064

    摘要： An assembly for coupling a track with a base extrusion via a support extrusion and a wedge assembly. A double-edged support extrusion for coupling a track with a guide wheel via a wedge assembly according to some embodiments of the invention. Methods for assembling an assembly for coupling a track with a base extrusion via a support extrusion and a wedge assembly and a double-edged support extrusion for coupling a track with a guide wheel via a wedge assembly.

    摘要翻译： 一种用于通过支撑挤压件和楔形组件将轨道与基座挤压件联接的组件。 根据本发明的一些实施例的用于通过楔组件将轨道与导轮联接的双刃支撑挤压件。 用于组装用于通过支撑挤出机将轨道与基座挤出件联接的组件的方法，以及用于通过楔组件将轨道与导轮联接的双刃支撑挤压件。