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    Benzodiazepines for Treating or Preventing Rsv Infection
    4.
    发明申请
    Benzodiazepines for Treating or Preventing Rsv Infection 审中-公开

    公开(公告)号：US20080139536A1

    公开(公告)日：2008-06-12

    申请号：US10593667

    申请日：2005-03-18

    申请人： Verity Dowdell ,  Richard Kelsey ,  Malcolm Carter ,  Dagmar Alber ,  Elisa Henderson

    发明人： Verity Dowdell ,  Richard Kelsey ,  Malcolm Carter ,  Dagmar Alber ,  Elisa Henderson

    IPC分类号： A61K31/5513 ,  C07D243/24 ,  A61P31/12

    CPC分类号： C07D403/12 ,  A61K31/5513 ,  C07D243/24 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/393

    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.

    Process for Preparing Benzodiazepines
    5.
    发明申请
    Process for Preparing Benzodiazepines 审中-公开

    公开(公告)号：US20070293482A1

    公开(公告)日：2007-12-20

    申请号：US10593665

    申请日：2005-03-21

    申请人： Verity Dowdell ,  Richard Kelsey ,  Malcolm Carter ,  Elisa Henderson

    发明人： Verity Dowdell ,  Richard Kelsey ,  Malcolm Carter ,  Elisa Henderson

    IPC分类号： A61K31/5513 ,  A61P31/12 ,  C07D243/24 ,  C07D243/26

    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.

    Benzodiazepine derivatives and pharmaceutical compositions containing them
    6.
    发明申请
    Benzodiazepine derivatives and pharmaceutical compositions containing them 失效

    公开(公告)号：US20060040923A1

    公开(公告)日：2006-02-23

    申请号：US10528250

    申请日：2003-09-22

    申请人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

    发明人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

    IPC分类号： A61K31/5513 ,  C07D243/12

    CPC分类号： C07D401/12 ,  C07D243/24 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    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(O)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)-.

    Benzodiazepine Derivatives and Pharmaceutical Compositions Containing Them
    7.
    发明申请
    Benzodiazepine Derivatives and Pharmaceutical Compositions Containing Them 失效

    公开(公告)号：US20100015063A1

    公开(公告)日：2010-01-21

    申请号：US12476797

    申请日：2009-06-02

    申请人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

    发明人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

    IPC分类号： A61K9/12 ,  A61K38/20 ,  A61K31/56 ,  A61K31/5513 ,  C07D243/24

    CPC分类号： C07D401/12 ,  C07D243/24 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    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)-.

    Benzodiazepine derivatives and pharmaceutical compositions containing them
    8.
    发明授权
    Benzodiazepine derivatives and pharmaceutical compositions containing them 失效

    公开(公告)号：US08119630B2

    公开(公告)日：2012-02-21

    申请号：US12476797

    申请日：2009-06-02

    申请人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

    发明人： Malcolm Carter ,  Elisa Henderson ,  Richard Kelsey ,  Lara Wilson ,  Phil Chambers ,  Debra Taylor ,  Stan Tyms

    IPC分类号： A61P31/12

    CPC分类号： C07D401/12 ,  C07D243/24 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    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)-.

    Routing in an asymmetrical link wireless network
    9.
    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

    申请人： Richard Kelsey ,  Matteo Paris ,  Andrew Wheeler

    发明人： Richard Kelsey ,  Matteo Paris ,  Andrew Wheeler

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

    CPC分类号： H04L1/18 ,  H04L1/203 ,  H04L2001/0093 ,  H04W40/14

    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。