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    Imidazolyl-cyclic acetals
    2.
    发明授权
    Imidazolyl-cyclic acetals 有权
    咪唑基 - 环状缩醛

    公开(公告)号：US06602877B1

    公开(公告)日：2003-08-05

    申请号：US09456360

    申请日：1999-12-08

    申请人： Paul L. Bamborough ,  Alan J. Collis ,  Frank Halley ,  Richard A. Lewis ,  David J. Lythgoe ,  Jeffrey M. McKenna ,  Iain M. McLay ,  Barry Porter ,  Andrew J. Ratcliffe ,  Paul A. Wallace

    发明人： Paul L. Bamborough ,  Alan J. Collis ,  Frank Halley ,  Richard A. Lewis ,  David J. Lythgoe ,  Jeffrey M. McKenna ,  Iain M. McLay ,  Barry Porter ,  Andrew J. Ratcliffe ,  Paul A. Wallace

    IPC分类号： C07D23354

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/10 ,  C07D493/10

    摘要： Compounds of formula (I) are described in which R1 is optionally substituted heteroaryl; R2 is optionally substituted aryl or optionally substituted heteroaryl; R3 is a group —L1—R7 or —L2—R8 [where L1 is an optionally substituted alkylene linkage; R7 is hydrogen, aryl, cyano, cycloalkyl, heteroaryl, heterocycloalkyl, nitro, —S(O)nR9, —NHSO2R9, —C(═Z)OR10, —C(═Z)R10, —OR10, —N(R11)—C(═Z)R9, —NY1Y2, —SO2NY1Y2, —C(═Z)—NY1Y2, —N(R11)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)R10, —C(═NOR10)R10, —C(═Z)NR10OR12, —N(R11)—C(═NR13)—NY1Y2 or —N(R11)—C(═Z)OR11; L2 is a direct bond or a straight- or branched-carbon chain comprising from 2 to about 6 carbon atoms and contains a double or triple carbon-carbon bond; and R8 is hydrogen, aryl, cycloalkenyl, cycloalkyl, heteroaryl or heterocycloalkyl]; R4 is a group —L3—R14 [where L3 is a direct bond or an optionally substituted alkylene linkage and R14 is hydrogen, alkyl, azido, hydroxy, alkoxy, aryl, arylalkyloxy, aryloxy, carboxy (or an acid bioisostere), cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, heterocycloalkyl, heterocycloalkyloxy, nitro, —NY4Y5, —N(R10)—C(═Z)—R15; —N(R10)—C(═Z)—L4—R16, —NH—C(═Z)—NH—R15, —NH—C(═Z)—NH—L4—R16, —N(R10)—SO2—R15, —N(R10)—SO2—L4—R16, —S(O)nR9, —C(═Z)—NY4Y5 or —C(═Z)—OR9]; R5 is hydrogen, alkyl or hydroxyalkyl; or R4 and R5, when attached to the same carbon atom, may form with the said carbon atom a cycloalkyl, cycloalkenyl or heterocycloalkyl ring or a group C═CH2; R6 is hydrogen or alkyl; and m is zero or an integer 1 or 2; and N-oxides thereof, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of compounds of formula (I) and N-oxides thereof, and their prodrugs. The compounds are TNF inhibitors and are useful as pharmaceuticals.

    摘要翻译： 描述式（I）的化合物，其中R 1是任选取代的杂芳基; R2是任选取代的芳基或任选取代的杂芳基; R3是基团-L1-R7或-L2-R8 [其中L1是任选取代的亚烷基键; R 7是氢，芳基，氰基，环烷基，杂芳基，杂环烷基，硝基，-S（O）n R 9，-NHSO 2 R 9，-C（= Z）OR 10，-C（= Z）R 10，-OR 10，-N（R 11） -C（= Z）R9，-NY1Y2，-SO2NY1Y2，-C（= Z）-NY1Y2，-N（R11）-C（= Z）-NY1Y2，-N（OR10）-C（= Z）-NY1Y2 ，-N（OR 10）-C（= Z）R 10，-C（= NOR 10）R 10，-C（= Z）NR 10 OR 12，-N（R 11）-C（= NR 13）-NY 1 Y 2或-N（R 11） C（= Z）OR 11; L2是直接键或包含2至约6个碳原子并含有双或三碳 - 碳键的直链或支链碳链; 和R8是氢，芳基，环烯基，环烷基，杂芳基或杂环烷基]; R4是基团-L3-R14 [其中L3是直接键或任选取代的亚烷基键，R 14是氢，烷基，叠氮基，羟基，烷氧基，芳基，芳基烷氧基，芳氧基，羧基（或酸式生物电子等排体） 杂芳基烷氧基，杂芳氧基，杂环烷基，杂环烷氧基，硝基，-NY 4 Y 5，-N（R 10）-C（= Z）-R 15; -N（R10）-C（= Z）-L4-R

    Antimicrobial agents
    5.
    发明授权
    Antimicrobial agents 失效
    抗微生物剂

    公开(公告)号：US07323596B2

    公开(公告)日：2008-01-29

    申请号：US10433625

    申请日：2001-12-21

    申请人： Barry Porter ,  Paul Gane ,  Raymond Beckett ,  Kenneth Keavey ,  Jac Wijkmans ,  Lydia Saroglou

    发明人： Barry Porter ,  Paul Gane ,  Raymond Beckett ,  Kenneth Keavey ,  Jac Wijkmans ,  Lydia Saroglou

    IPC分类号： C07C239/00 ,  C07C259/00 ,  C07C303/00 ,  C07C307/00 ,  C07C309/00 ,  C07C311/00

    CPC分类号： C07D285/10 ,  C07C259/06 ,  C07C311/19 ,  C07D209/18 ,  C07D215/56 ,  C07D217/22 ,  C07D263/12 ,  C07D311/12 ,  C07D491/04

    摘要： Compounds of formula (I) and (IA) have antibacterial or antiprotozoal activity: formula (1) formula (2) wherein: Z represents a radical of formula N(OH)CH(═O) or of formula C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl, or, except when Z is a radical of formula N(OH)CH(═O), a hydroxy or amino group; R2 represents a radical of formula R10—(X)n-(ALK)m- wherein R10 represents hydrogen, or an optionally substituted c1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 ?alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent NH—, —O— or S— linkages, X represents NH—, —O— or S—, and m and n are independently 0 or 1; R3 represents hydrogen, C1-C6alkyl, or benzyl; and R4 is as defined in the specification.

    摘要翻译： 式（I）和（IA）的化合物具有抗菌或抗原虫活性：式（1）式（2）其中：Z表示式N（OH）CH（-O）或式C（-O）NH （哦）; R 1表示氢，甲基或三氟甲基，或除Z是式N（OH）CH（-O），羟基或氨基基团时; R 2表示式R 10 - （X）n - （ALK）m - 的基团，其中R C 1 -C 10烷基，C 2 -C 6烷基，C 2 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 6个烯基，C 2 -C 6炔基，环烷基，芳基或杂环基，ALK表示直链或支链二价C 1 - “C” - “C” - “00”“”=“2.46mm”wi =“1.44mm”file = “US07323596-20080129-P00001.TIF”alt =“自定义字符”img-content =“character”img-format =“tif”/> 6亚链烯基或C 2 -C 6个亚炔基，并且可以被一个或多个不相邻的NH-，-O-或S-键间隔，X表示NH-，-O-或S-，m和n独立地为0或 1; R 3表示氢，C 1 -C 6烷基或苄基; R 4和R 4如本说明书中所定义。

    Handheld spray receptor
    6.
    发明授权
    Handheld spray receptor 有权
    手持式喷雾受体

    公开(公告)号：US07798429B1

    公开(公告)日：2010-09-21

    申请号：US10179088

    申请日：2002-06-25

    申请人： Barry Porter

    发明人： Barry Porter

    IPC分类号： B05B7/02 ,  B05B7/30

    CPC分类号： B05B7/2427 ,  B65D83/202

    摘要： The handheld spray receptor provides an apparatus which, when used with a supply of a liquid under pressure, dispenses a liquid material in a pattern that is controlled by an inexpensive and disposable actuator. Such actuators are employed as an industry standard part that would be found on any aerosol spray can, and feature small cylindrical actuators that may be easily interchanged, so as to provide varied spray patterns. A purging model provides for a quick and convenient method of purging liquid from the actuator, so as to prevent hardening of liquid material exposed to the atmosphere, and a subsequent clogging of the receptor. When used with a supply of liquid under pressure and access to a propellant, the handheld spray receptor significantly reduces the amount of hazardous waste, in the form of partially consumed aerosol cans, that would otherwise enter landfills or hazardous waste recycling facilities.

    摘要翻译： 手持式喷雾式接收器提供了一种在压力下与液体供应一起使用的设备，其以由便宜且一次性的致动器控制的图案分配液体材料。 这种致动器被用作可以在任何气溶胶喷雾罐上发现的工业标准部件，并且具有可以容易地互换的小型圆柱形致动器，以便提供各种喷射模式。 吹扫模型提供了从致动器清洗液体的快速方便的方法，以防止暴露于大气中的液体材料的硬化以及随后的受体堵塞。 当与压力下的液体供应和进入推进剂一起使用时，手持式喷雾受体显着减少部分消耗的气溶胶罐形式的危险废物的数量，否则这些废物将进入垃圾填埋场或危险废物回收设施。

    Reusable chemical caddie
    7.
    发明授权
    Reusable chemical caddie 失效
    可重复使用的化学品球罐

    公开(公告)号：US06279837B1

    公开(公告)日：2001-08-28

    申请号：US09539001

    申请日：2000-03-30

    申请人： Barry Porter

    发明人： Barry Porter

    IPC分类号： B05B900

    CPC分类号： B05B9/0805 ,  B05B1/3046 ,  B05B9/01

    摘要： This multipurpose device for dispensing paints or chemicals replaces aerosol cans and custom equipment for spraying paint. Constructed of stainless steel, brass, and Teflon®, the reusable chemical caddie can be used to dispense solvents, paints, and a broad range of materials which will not corrode stainless steel. The reusable chemical caddie eliminates the contamination of the atmosphere with traditional propellants, utilizing compressed air as a propellant. The reusable nature of the reusable chemical caddie eliminates the contamination that results from residual toxic materials and that are invariably discarded when traditional spray cans are discarded into landfills. It is portable, and with an increased capacity as compared to traditional spray cans, is ideally suited for commercial applications.

    摘要翻译： 这种用于分配油漆或化学品的多用途装置取代喷雾罐和用于喷涂油漆的定制设备。 可重复使用的化学品罐由不锈钢，黄铜和特氟龙（R）构成，可用于分配溶剂，涂料和不腐蚀不锈钢的各种材料。 可重复使用的化学玩具消除了传统推进剂对空气的污染，利用压缩空气作为推进剂。 可重复使用的化学品罐头的可重复使用性质消除了由残留的有毒物质引起的污染物，当传统喷雾罐被丢弃到垃圾填埋场时，这些污染物总是被丢弃。 它是便携式的，与传统喷雾罐相比具有增加的容量，非常适合商业应用。

    HANDHELD SPRAY RECEPTOR
    8.
    发明申请
    HANDHELD SPRAY RECEPTOR 审中-公开
    手持喷雾受体

    公开(公告)号：US20100181347A1

    公开(公告)日：2010-07-22

    申请号：US12749562

    申请日：2010-03-30

    申请人： Barry Porter

    发明人： Barry Porter

    IPC分类号： B65D83/16

    CPC分类号： B05B7/2427 ,  B65D83/202

    摘要： The handheld spray receptor provides an apparatus which, when used with a supply of a liquid under pressure, dispenses a liquid material in a pattern that is controlled by an inexpensive and disposable actuator. Such actuators are employed as an industry standard part that would be found on any aerosol spray can, and feature small cylindrical actuators that may be easily interchanged, so as to provide varied spray patterns. A purging model provides for a quick and convenient method of purging liquid from the actuator, so as to prevent hardening of liquid material exposed to the atmosphere, and a subsequent clogging of the receptor. When used with a supply of liquid under pressure and access to a propellant, the handheld spray receptor significantly reduces the amount of hazardous waste, in the form of partially consumed aerosol cans, that would otherwise enter landfills or hazardous waste recycling facilities.

    摘要翻译： 手持式喷雾式接收器提供了一种在压力下与液体供应一起使用的设备，其以由便宜且一次性的致动器控制的图案分配液体材料。 这种致动器被用作可以在任何气溶胶喷雾罐上发现的工业标准部件，并且具有可以容易地互换的小型圆柱形致动器，以便提供各种喷射模式。 吹扫模型提供了从致动器清洗液体的快速方便的方法，以防止暴露于大气中的液体材料的硬化以及随后的受体堵塞。 当与压力下的液体供应和进入推进剂一起使用时，手持式喷雾受体显着减少部分消耗的气溶胶罐形式的危险废物的数量，否则这些废物将进入垃圾填埋场或危险废物回收设施。

    Bacterial enzyme inhibitors
    9.
    发明授权
    Bacterial enzyme inhibitors 失效
    细菌酶抑制剂

    公开(公告)号：US07241921B2

    公开(公告)日：2007-07-10

    申请号：US10497494

    申请日：2002-11-27

    申请人： Paul Gane ,  Barry Porter ,  Henriette Willems ,  Raymond Paul Beckett ,  Kenneth Keavey

    发明人： Paul Gane ,  Barry Porter ,  Henriette Willems ,  Raymond Paul Beckett ,  Kenneth Keavey

    IPC分类号： C07C259/04 ,  A61K31/19

    CPC分类号： C07D213/40 ,  C07C275/24 ,  C07C2601/08 ,  C07D295/215

    摘要： Compounds of formula (I) are antibacterial agents: wherein: Z is —N(OH)CH(═O) or —C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl or, except when Z is a radical of formula —N(OH)CH(═O), a hydroxy, halo or amino group; R2, R3 and R4 independently represents hydrogen or a group R10—(D)n—(ALK)m— wherein R10, D, n, m and ALK are as defined in the claims; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted monocyclic heterocyclic ring containing from 5 to 7 ring atoms, one of which is the nitrogen atom to which R4 and R5 are attached and the remaining ring atoms being selected from compatible combinations of carbon, oxygen, sulfur and nitrogen

    摘要翻译： 式（I）化合物是抗菌剂：其中：Z是-N（OH）CH（-O）或-C（-O）NH（OH）; 除了当Z是式-N（OH）CH（-O），羟基，卤素或氨基基团时，R 1表示氢，甲基或三氟甲基。 R 2，R 3和R 4独立地表示氢或基团R 10 - （D）