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    Novel compounds
    13.
    发明申请
    Novel compounds 失效

    公开(公告)号：US20050137229A1

    公开(公告)日：2005-06-23

    申请号：US10872160

    申请日：2004-06-17

    Applicant: Paul Fish ,  Michael Fray ,  Deborah Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    Inventor： Paul Fish ,  Michael Fray ,  Deborah Lovering ,  Alan Stobie ,  Florian Wakenhut ,  Gavin Whitlock

    IPC: A61P13/00 ,  A61P25/24 ,  A61P29/00 ,  C07D207/14 ,  C07D211/06 ,  A61K31/445 ,  C07D211/56

    CPC classification number: C07D207/14

    Abstract: 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.

    Quinoxaline derivatives useful in therapy
    14.
    发明授权
    Quinoxaline derivatives useful in therapy 失效
    喹喔啉衍生物可用于治疗

    公开(公告)号：US5863917A

    公开(公告)日：1999-01-26

    申请号：US938230

    申请日：1997-09-26

    Applicant: Charles Eric Mowbray ,  Alan Stobie

    Inventor： Charles Eric Mowbray ,  Alan Stobie

    IPC: A61K31/495 ,  A61K31/498 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  C07D241/44 ,  C07D403/12 ,  C07D413/06 ,  C07D413/12 ,  C07D241/52

    CPC classification number: C07D403/12 ,  A61K31/498 ,  C07D241/44 ,  C07D413/06 ,  Y02P20/55

    Abstract: The invention provides compounds of formula I, ##STR1## wherein R.sup.1 and R.sup.2 independently represent Cl or C.sub.1-6 alkyl;R.sup.3 represents XCO.sub.2 R.sup.4, XCONHSO.sub.2 R.sup.5, YNHSO.sub.2 R.sup.5 or XR.sup.6 ;R.sup.4 represents H or C.sub.1-6 alkyl (optionally substituted by aryl or heterocyclyl);R.sup.5 represents CF.sub.3, heterocyclyl or C.sub.1-6 alkyl (optionally substituted by aryl or heterocyclyl);R.sup.6 represents an acidic heterocycle;X represents a C.sub.1-6 alkyl diradical (optionally subsituted by aryl or heterocyclyl); andY represents a C.sub.2-6 alkyl diradical (optionally substituted by aryl or heterocyclyl); provided that when R.sup.1 and R.sup.2 each represent Cl, then R.sup.3 does not represent CH.sub.2 CO.sub.2 H, CH.sub.2 CO.sub.2 CH.sub.3, CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3 or 5-tetrazolylmethyl; and pharmaceutically acceptable salts thereof.The compounds are indicated as anxiolytics, anticonvulsants, analgesics and neuroprotectives.

    Abstract translation: 本发明提供式I化合物，其中R 1和R 2独立地表示C 1或C 1-6烷基; R3表示XCO2R4，XCONHSO2R5，YNHSO2R5或XR6; R 4表示H或C 1-6烷基（任选被芳基或杂环基取代）; R5代表CF3，杂环基或C1-6烷基（任选被芳基或杂环基取代）; R6表示酸性杂环; X表示C 1-6烷基双基（任选被芳基或杂环基取代）; Y代表二价C 2-6烷基（任选被芳基或杂环基取代）; 条件是当R 1和R 2各自表示Cl时，则R 3不表示CH 2 CO 2 H，CH 2 CO 2 CH 3，CH 2 CH 2 NHSO 2 CF 3或5-四唑基甲基; 及其药学上可接受的盐。 化合物表示为抗焦虑药，抗惊厥药，止痛剂和神经保护剂。

    Quinoxalinedione NMDA receptor antagonists
    15.
    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

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

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

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

    CPC classification number: C07D403/06

    Abstract: 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.

    Abstract translation: 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。

    Compounds
    17.
    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

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

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

    IPC: A61K31/40 ,  C07D295/10

    CPC classification number: C07D207/14

    Abstract: 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.

    Imidazopyridine compounds as 5-HT4 receptor modulators
    19.
    发明授权
    Imidazopyridine compounds as 5-HT4 receptor modulators 失效
    咪唑并吡啶化合物作为5-HT4受体调节剂

    公开(公告)号：US06624162B2

    公开(公告)日：2003-09-23

    申请号：US10251109

    申请日：2002-09-20

    Applicant: Chikara Uchida ,  Hirohide Noguchi ,  Alan Stobie ,  Geoffrey Gymer ,  David Fenwick

    Inventor： Chikara Uchida ,  Hirohide Noguchi ,  Alan Stobie ,  Geoffrey Gymer ,  David Fenwick

    IPC: A61K31437

    CPC classification number: C07D471/04

    Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein R1 is hydrogen, halo or alkyl; R2 and R3 are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R2 and R3 taken together with the nitrogen atom to which they are attached may form hetrocyclic; R4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R5 is hydrogen, halo, alkyl alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R6 is hydrogen, alkyl or alkoxyalkyl; X is NR9 wherein R9 is hydrogen or alkyl; and Y is (CR7R8)n wherein n is an integer from 0 to 5. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, Functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

    Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐，其中R 1是氢，卤素或烷基; R 2和R 3独立地是氢，烷基，烯基，炔基，氨基烷基或羟烷基; 或R 2和R 3与它们所连接的氮原子一起可以形成环状的; R 4是氢，卤素，酰基，氨基，酰氨基，芳基，芳基烷基或杂芳基; R 5是氢，卤素，烷基烯基，炔基，酰基，氨基，酰氨基，芳基，芳基烷基或杂芳基; R 6是氢，烷基或烷氧基烷基; X是NR 9，其中R 9是氢或烷基; 并且Y是（CR 7 R 8）n，其中n是0至5的整数。这些化合物具有5-HT 4受体结合活性，因此可用于治疗胃食管反流病，非溃疡性消化不良 ，功能性消化不良，肠易激综合征等。 本发明还提供了包含上述化合物的药物组合物。

    Quinoxalinediones
    20.
    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

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

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

    IPC: A61K315377

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

    Abstract: 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.

    Abstract translation: 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。

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