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    NOVEL COMPOUNDS
    4.
    发明申请
    NOVEL COMPOUNDS 审中-公开
    新型化合物

    公开(公告)号：US20080306123A1

    公开(公告)日：2008-12-11

    申请号：US12124755

    申请日：2008-05-21

    申请人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Deborah Jane Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    发明人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Deborah Jane Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    IPC分类号： A61K31/4468 ,  A61P13/00 ,  A61P29/00 ,  A61P15/00 ,  A61P25/24

    CPC分类号： C07D207/14

    摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S or O; Y is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

    摘要翻译： 式（I）化合物及其药学上和/或兽医学上可接受的衍生物，其中R 1是H，C 1-6烷基，-C（X）Y，C 3-8环烷基，芳基，het，芳基-C 1-4烷基或叔丁基 其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基 - C 1-6烷基和C 1-4烷基-S-C 1-4烷基; R 2是芳基或杂芳基，各自任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1 -4-烷基-S-C 1-4烷基; R 3为C 1-6烷基，C 3-8环烷基，C 3-8环烷基-C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔-C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个取代基取代 独立地选自C 1-6烷基，C 1-6烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基; X是S或O; Y是H，C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基C 1-4烷基; n为1或2，条件是当n为1时，m为0或1，当n为2时，m为0，其中如果m为0，则*表示手性中心。 本发明的化合物表现出5-羟色胺和去甲肾上腺素再摄取抑制剂的活性，因此可用于各种治疗领域，例如尿失禁。

    Compounds
    5.
    发明授权
    Compounds 失效

    公开(公告)号：US07378436B2

    公开(公告)日：2008-05-27

    申请号：US10872160

    申请日：2004-06-17

    申请人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    发明人： Paul Vincent Fish ,  Michael Jonathan Fray ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Alistair Whitlock ,  Mark David Andrews ,  Alan Daniel Brown ,  Mark Ian Lansdell

    IPC分类号： A61K31/40 ,  C07D295/10

    CPC分类号： C07D207/14

    摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy-C1-6alkyl and C1-4alkyl-S—C1-4alkyl; R3 is C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy —C1-6alkyl and C1-4alkyl-S—C1-4alkyl; X is S or O; Y is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

    Quinoxalinediones
    6.
    发明授权
    Quinoxalinediones 失效
    喹喔啉

    公开(公告)号：US06376490B1

    公开(公告)日：2002-04-23

    申请号：US09157806

    申请日：1998-09-04

    申请人： David John Bull ,  Christopher Lee Carr ,  Michael Jonathan Fray ,  Elisabeth Colette Louise Gautier ,  Charles Eric Mowbray ,  Alan Stobie

    发明人： David John Bull ,  Christopher Lee Carr ,  Michael Jonathan Fray ,  Elisabeth Colette Louise Gautier ,  Charles Eric Mowbray ,  Alan Stobie

    IPC分类号： A61K315377

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： The invention provides compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 5-membered ring heteroaryl group containing 3 or 4 nitrogen heteroatoms which is linked to the quinoxalinedione ring by a ring carbon or nitrogen atom said group being optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by 1 or 2 substituents each independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, C3-C7 cycloalkyloxy, —COOH, C1-C4 alkoxycarbonyl, —CONR3R4, —NR3R4, —S(O)p(C1-C4 alkyl), —SO2NR3R4, aryl, aryloxy, aryl(C1-C4)alkoxy, and het, said C1-C4alkyl being optionally substituted by C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, halo(C1C4)alkoxy, C3-C7 cycloalkyloxy, C3-C7 cycloalkyl (C1-C4) alkoxy, —COOH, C1-C4 alkoxycarbonyl, —CONR3R4, —NR3R4,—S(O)p(C1-C4 alkyl), —SO2(aryl), —SO2NR3R4 morpholino, aryl, aryloxy, aryl(C1-C4)alkoxy or het, and said C2-C4 alkenyl being optionally substituted by aryl; and R1 and R2 are each independently selected from H, fluoro, chloro, bromo, C1-C4 alkyl and halo(C1-C4)alkyl. The compounds are useful as NDMA receptor antagonists for treating acute neurodegenerative and chronic neurological disorders.

    摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中R是含有3或4个氮杂原子的5元环杂芳基，其通过环碳或氮原子与喹喔啉二酮环连接，所述基团为 任选地苯并稠合并任选被取代的，包括在苯并稠合部分中的1或2个独立地选自C 1 -C 4烷基，C 2 -C 4烯基，C 3 -C 7环烷基，卤素，羟基，C 1 -C 4烷氧基，C 3 -C（C 1 -C 4）烷氧基，-COOH，C 1 -C 4烷氧基羰基，-CONR 3 R 4，-NR 3 R 4，-S（O）p（C 1 -C 4烷基），-SO 2 NR 3 R 4，芳基，芳氧基，芳基（C 1 -C 4）烷氧基， 任选被C 3 -C 7环烷基，卤素，羟基，C 1 -C 4烷氧基，卤代（C 1 -C 4）烷氧基，C 3 -C 7环烷基氧基，C 3 -C 7环烷基（C 1 -C 4）烷氧基，-COOH，C 1 -C 4烷氧基羰基 ，-CONR 3 R 4，-NR 3 R 4，-S（O）p（C 1 -C 4烷基），-SO 2（芳基），-SO 2 NR 3 R 4吗啉代，芳基，芳氧基，芳基（C 1 -C 4）烷氧基或杂原子， 任选地被取代 由芳基 并且R 1和R 2各自独立地选自H，氟，氯，溴，C 1 -C 4烷基和卤代（C 1 -C 4）烷基。 该化合物可用作治疗急性神经变性和慢性神经障碍的NDMA受体拮抗剂。

    Quinoxalinedione NMDA receptor antagonists
    7.
    发明授权
    Quinoxalinedione NMDA receptor antagonists 失效
    喹喔啉酮NMDA受体拮抗剂

    公开(公告)号：US5783572A

    公开(公告)日：1998-07-21

    申请号：US793896

    申请日：1997-03-12

    申请人： Charles Eric Mowbray ,  Alan Stobie ,  Michael Jonathan Fray ,  David John Bull ,  Christopher Lee Carr

    发明人： Charles Eric Mowbray ,  Alan Stobie ,  Michael Jonathan Fray ,  David John Bull ,  Christopher Lee Carr

    IPC分类号： C07D401/14 ,  A61K31/495 ,  A61K31/535 ,  A61P25/08 ,  A61P25/20 ,  A61P25/28 ,  A61P43/00 ,  C07D403/06 ,  A61K31/55

    CPC分类号： C07D403/06

    摘要： Compounds of formula (I): ##STR1## and their pharmaceutically acceptable salts, wherein R.sup.1 and R.sub.2 are each independently Cl, Br, CH.sub.3, CH.sub.2 CH.sub.3 or CF.sub.3 ; R.sup.3 is H, CH.sub.3 or CH.sub.2 CH.sub.3 ; and X is a 5-membered heterocyclic group containing up to four nitrogen atoms, attached via a nitrogen atom, the said group being optionally substituted by C.sub.1 -C.sub.6 alkyl or (CH.sub.2).sub.n NR.sup.4 R.sup.5, wherein n is an integer from 1 to 5 and R.sup.4 and R.sup.5 are each independently H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or C.sub.1 -C.sub.4 alkyl substituted by phenyl or pyridyl, or R.sup.4 and R.sup.5 are linked to form, together with the nitrogen atom to which attached, a pyrrolidine, piperidine, piperazine, N-(C.sub.1 -C.sub.4 alkyl) piperazine, morpholine or azepine group, or, when X is triazolyl, said group may optionally be benzofused, are NMDA antagonists of value in the treatment of acute neurodegenerative disorders, e.g. arising from stroke or traumatic head injury and in chronic neurological disorders, e.g. senile dementia and Alzheimer's disease.

    摘要翻译： PCT No.PCT / EP95 / 03483第 371日期1997年3月12日 102（e）1997年3月12日PCT PCT 1995年9月1日PCT公布。 公开号WO96 / 08485 日本公报（I）的化合物：其中R 1和R 2各自独立地为Cl，Br，CH 3，CH 2 CH 3或CF 3; R3是H，CH3或CH2CH3; 并且X是含有至多四个氮原子的五元杂环基，其通过氮原子连接，所述基团任选被C 1 -C 6烷基或（CH 2）n NR 4 R 5取代，其中n是1至5的整数，R 4 R 5和R 5各自独立地为H，C 1 -C 6烷基，C 3 -C 6环烷基或被苯基或吡啶基取代的C 1 -C 4烷基，或者R 4和R 5与连接的氮原子一起形成吡咯烷，哌啶， 哌嗪，N-（C 1 -C 4烷基）哌嗪，吗啉或吖庚因基，或者当X是三唑基时，所述基团可以任选地被苯并稠合，是治疗急性神经变性疾病的NMDA拮抗剂，例如 由中风或创伤性头部损伤和慢性神经障碍引起的，例如， 老年痴呆和阿尔茨海默病。