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    Benzodiazepine derivatives and pharmaceutical compositions containing them
    2.
    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
    3.
    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
    4.
    发明授权
    Benzodiazepine derivatives and pharmaceutical compositions containing them 失效

    公开(公告)号：US07582624B2

    公开(公告)日：2009-09-01

    申请号：US10528250

    申请日：2003-09-22

    申请人： Malcolm Carter ,  Philip Chambers ,  Verity Dowdell ,  Elisa Ann Henderson ,  Richard David Kelsey ,  Debra Taylor ,  Stanley Tyms ,  Lara Wilson

    发明人： Malcolm Carter ,  Philip Chambers ,  Verity Dowdell ,  Elisa Ann Henderson ,  Richard David Kelsey ,  Debra Taylor ,  Stanley Tyms ,  Lara Wilson

    IPC分类号： C07D243/24 ,  C07D409/12 ,  C07D405/12 ,  C07D403/12 ,  A61K31/5513

    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)-.

    Benzodiazepines for Treating or Preventing Rsv Infection
    7.
    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.

    Benzanilide derivatives
    10.
    发明授权
    Benzanilide derivatives 失效
    苯甲酰苯胺衍生物

    公开(公告)号：US5510350A

    公开(公告)日：1996-04-23

    申请号：US237297

    申请日：1994-05-03

    申请人： Alexander W. Oxford ,  William L. Mitchell ,  John Bradshaw ,  John W. Clitherow ,  Malcolm Carter

    发明人： Alexander W. Oxford ,  William L. Mitchell ,  John Bradshaw ,  John W. Clitherow ,  Malcolm Carter

    IPC分类号： A61K31/495 ,  A61K20060101 ,  A61K31/165 ,  A61K31/41 ,  A61K31/496 ,  A61K31/53 ,  A61P5/00 ,  A61P9/12 ,  A61P15/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D20060101 ,  C07D249/04 ,  C07D249/06 ,  C07D249/08 ,  C07D249/14 ,  C07D271/06 ,  C07D271/07 ,  C07D271/08 ,  C07D271/10 ,  C07D271/107 ,  C07D285/06 ,  C07D285/08 ,  C07D285/10 ,  C07D285/12 ,  C07D285/125 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

    CPC分类号： C07D249/08 ,  C07D249/06 ,  C07D271/06 ,  C07D271/07 ,  C07D271/107 ,  C07D285/06 ,  C07D285/08 ,  C07D285/12

    摘要： The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a hydrogen atom or a halogen atom or a group selected from C.sub.1-6 alkyl and C.sub.1-6 alkoxy;R.sup.2 represents a phenyl group substituted by a group selected from ##STR2## and optionally further substituted by one or two substituents selected from halogen atoms, C.sub.1-6 alkoxy, hydroxy, and C.sub.1-6 alkyl;R.sup.3 represents the group ##STR3## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a group selected from hydroxy, C.sub.1-6 alkoxy and C.sub.1-6 alkyl;R.sup.6 represents a hydrogen atom or a group selected from --NR.sup.9 R.sup.10 and a C.sub.1-6 alkyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkoxy, hydroxy, C.sub.1-6 acyloxy and --SO.sub.2 R.sup.11 ;R.sup.7, R.sup.8 and R.sup.9, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-6 alkyl group;R.sup.10 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.1-6 acyl, benzoyl and --SO.sub.2 R.sup.11 ;R.sup.11 represents a C.sub.1-6 alkyl group or a phenyl group;Z represents an oxygen atom or a group selected from NR.sup.8 and S(O).sub.k ; andk represents zero, 1 or 2.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.

    摘要翻译： 本发明提供式（I）化合物：其中R 1表示氢原子或卤素原子或选自C 1-6烷基和C 1-6烷氧基的基团;或其生理学上可接受的盐或溶剂化物。 R 2表示被选自下列基团取代的苯基，并任选进一步被一个或两个选自卤素原子，C 1-6烷氧基，羟基和C 1-6烷基的取代基取代; R 3表示基团R 4和R 5可以相同或不同，各自独立地表示氢原子或卤素原子或选自羟基，C 1-6烷氧基和C 1-6烷基的基团。 R6表示氢原子或选自-NR9R10和任选被一个或两个选自C 1-6烷氧基，C 1-6酰氧基和-SO 2 R 11的取代基取代的C 1-6烷基的基团; R 7，R 8和R 9可以相同或不同，各自独立地表示氢原子或C 1-6烷基; R 10表示氢原子或选自C 1-6烷基，C 1-6酰基，苯甲酰基和-SO 2 R 11的基团; R11表示C1-6烷基或苯基; Z表示氧原子或选自NR8和S（O）k的基团; 并且k代表0,1或2.化合物可用于治疗或预防抑郁症和其它CNS疾病。