Benzodiazepines for Treating or Preventing Rsv Infection

    公开(公告)号:US20080139536A1

    公开(公告)日:2008-06-12

    申请号:US10593667

    申请日:2005-03-18

    摘要: Use of a compound which is (a) a benzodiazepine derivative of the formula (I) or an N-oxide thereof or (b) a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing an RSV infection wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6alkyl)amino, vitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″, wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; n is from O to 3; R4 represents hydrogen or C1-6 alkyl; X represents —CO—, —CO—NR′—, —S(O)— or —S(O)2—, wherein R′ is hydrogen or a C1-C6 alkyl group; and R5 represents a heteroaryl or heterocyclyl group which is substituted by a C1C6 hydroxyalkyl group or a —(C1-C4 alkyl)-X1—(C1-C4 alkyl)-X2—(C1-C4 alkyl} group, wherein X1 represents -0-, —S— or —NR′—, wherein R′ represents H or a C1-C4 alkyl group and X2 represents —CO—, —SO— or —SO2—, or R5 represents -A1-Y-A2, wherein: -A1 is an aryl, heteroaryl, carbocyclyl or heterocyclyl group; 25 —Y represents a direct bond or a C1-C4 alkylene, —SO2—, —CO—, -0-, —S— or —NR′-moiety, wherein R′ is a C1-C6 alkyl group; and -A2 is an aryl, heteroaryl, carbocyclyl or heterocyclyl group.

    Benzodiazepine derivatives and pharmaceutical compositions containing them

    公开(公告)号:US08119630B2

    公开(公告)日:2012-02-21

    申请号:US12476797

    申请日:2009-06-02

    IPC分类号: A61P31/12

    摘要: Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; -each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; -n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(0)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

    Process for Preparing Benzodiazepines
    5.
    发明申请

    公开(公告)号:US20070293482A1

    公开(公告)日:2007-12-20

    申请号:US10593665

    申请日:2005-03-21

    CPC分类号: C07D243/24 Y02P20/55

    摘要: A process for producing a compound which is a benzodiazepine derivative of formula: (I) wherein: represents or R1 represents C1-6 alkyl, aryl or heteroaryl; each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″, wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; n is from 0 to 3; X represents —NH—, —N(C1-C6alkyl)-, —CO—, —CO—NR′—, —S(O)— or —S(O)2—, wherein R′ is hydrogen or a C1-C6 alkyl group; and R4 represents hydrogen; or —CO—R4′ or —CO—NH—R4 ′, wherein R4 ′ is a C1-C6 alkyl, C1-C6 hydroxyalkyl, aryl, heteroaryl, carbocyclyl or heterocyclyl group, which group is substituted by a C1-C6 hydroxyalkyl, aryl, heteroaryl, carbocyclyl or heterocyclyl group or a —(C1-C4 alkyl)-X1—(C1-C4 alkyl)-X2—(C1-C4 alkyl) group, wherein X1 represents —O—, —S— or —NR′—, wherein R′ represents H or a C1-C4 alkyl group and X2 represents —CO—, —SO— or —SO2—; or R4 ′represents -A1-Y-A2, wherein: A1 is an aryl, heteroaryl, carbocyclyl or heterocyclyl group; Y represents a direct bond or a C1-C4 alkylene, —SO2—, —CO—, —O—, —S or —NR′—, wherein R′ is a C1-C6 alkyl group; and A2 is an aryl, heteroaryl, carbocyclyl or heterocyclyl group; or R4 is a group selected from aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— and -ZR5, wherein: Z represents —CO—, —S(O)— or —S(O)2′; and R5 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-; or a pharmaceutically acceptable salt thereof; which process comprises: (a) subjecting a racemic benzodiazepine derivative of formula: (IIa): wherein R1, R3, R4, n and X are as defined above, and R2 represents an amino protecting group, to crystallisation induced dynamic resolution to yield a benzodiazepine derivative of formula (II): wherein, R1, R2, R3, R4, n and X are as defined above; and (b) deprotecting the benzodiazepine derivative of formula (II) as defined above to yield a benzodiazepine derivative of formula (I) or a pharmaceutically acceptable form thereof as defined above.

    Routing in an asymmetrical link wireless network
    6.
    发明申请
    Routing in an asymmetrical link wireless network 审中-公开
    路由在不对称链路无线网络中

    公开(公告)号:US20050249186A1

    公开(公告)日:2005-11-10

    申请号:US11063290

    申请日:2005-02-22

    IPC分类号: H04L1/00 H04L1/18 H04L1/20

    摘要: A method for directing packets in a radio network includes, at each node of the network, maintaining link data characterizing reliability of transmissions between neighboring nodes and that node based on received radio transmissions at that node, and distributing the link data to one or more of the neighboring nodes.

    摘要翻译: 用于在无线电网络中引导分组的方法包括:在网络的每个节点处,基于在该节点处的接收到的无线电传输来维护表征相邻节点和该节点之间的传输的可靠性的链接数据,并将链接数据分发到 相邻节点。

    Cooling system, a motor handling system, and a method of positioning a motor in a cooling system
    9.
    发明授权
    Cooling system, a motor handling system, and a method of positioning a motor in a cooling system 有权
    冷却系统,电动机处理系统以及将电动机定位在冷却系统中的方法

    公开(公告)号:US08446057B2

    公开(公告)日:2013-05-21

    申请号:US13011561

    申请日:2011-01-21

    IPC分类号: H02K9/00

    CPC分类号: F16M7/00

    摘要: A cooling system, a motor handling system, and a method of positioning a motor in a cooling system are disclosed. The motor handling system includes a suspension feature configured to engage a support member, the support member positioned partially below a cooler. The motor handling system permits positioning of a motor in a first position and re-positioning of the motor to a second position. The cooling system includes a cooler, a support member positioned partially below the cooler, and a motor handling system. The method of positioning includes engaging a support member of a cooling system with a suspension feature, positioning the motor at a first position, and re-positioning the motor at a second position.

    摘要翻译: 公开了一种冷却系统,电动机处理系统以及将电动机定位在冷却系统中的方法。 马达处理系统包括悬挂特征,其构造成与支撑构件接合,所述支撑构件部分地位于冷却器下方。 电动机处理系统允许将电动机定位在第一位置并将电动机重新定位到第二位置。 冷却系统包括冷却器,部分位于冷却器下方的支撑构件和电动机处理系统。 定位方法包括将冷却系统的支撑构件与悬挂特征接合,将电动机定位在第一位置,并将电动机重新定位在第二位置。

    COOLER, COOLER PLATFORM ASSEMBLY, AND PROCESS OF ADJUSTING A COOLER PLATFORM
    10.
    发明申请
    COOLER, COOLER PLATFORM ASSEMBLY, AND PROCESS OF ADJUSTING A COOLER PLATFORM 审中-公开
    冷却器,冷却器平台组件和调节冷却器平台的过程

    公开(公告)号:US20130012118A1

    公开(公告)日:2013-01-10

    申请号:US13542947

    申请日:2012-07-06

    IPC分类号: F24F7/00 F24F7/007

    CPC分类号: F24F13/20 F24F2013/205

    摘要: A cooler, a cooler platform assembly, and a process of adjusting a cooler platform are disclosed. The cooler includes a cooling region, a discharge region, and a cooler platform positioned in the discharge region and proximal to a sloped interior section of the cooler. The cooler platform assembly includes a cooler platform, a sloped interior section of a cooler proximal to a first end of the cooler platform, and a vertical wall proximal to a second end of the cooler platform. The process includes adjusting a cooler platform from a retracted position substantially parallel to a vertical wall of a cooler to a deployed position substantially perpendicular to the vertical wall.

    摘要翻译: 公开了一种冷却器,冷却器平台组件和调节冷却器平台的过程。 冷却器包括冷却区域,排放区域和位于排放区域中并且靠近冷却器的倾斜内部部分的冷却器平台。 冷却器平台组件包括冷却器平台,靠近冷却器平台的第一端的冷却器的倾斜内部部分和靠近冷却器平台的第二端的垂直壁。 该过程包括从大致平行于冷却器的垂直壁的缩回位置到基本上垂直于垂直壁的展开位置调节冷却器平台。