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    Compounds which potentiate glutamate receptor and uses thereof in medicine
    1.
    发明授权
    Compounds which potentiate glutamate receptor and uses thereof in medicine 失效
    增强谷氨酸受体的药物及其在药物中的应用

    公开(公告)号：US07572819B2

    公开(公告)日：2009-08-11

    申请号：US11673044

    申请日：2007-02-09

    申请人： Daniel Marcus Bradley ,  Kevin Michael Thewlis ,  Simon Edward Ward

    发明人： Daniel Marcus Bradley ,  Kevin Michael Thewlis ,  Simon Edward Ward

    IPC分类号： A61K31/445 ,  C07D213/56

    CPC分类号： C07D213/64 ,  C07D213/42 ,  C07D213/50 ,  C07D213/61 ,  C07D213/84 ,  C07D213/85 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D333/20

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of C1-6alkyl, C1-6alkoxy, acetyl, halogen, haloC1-6alkyl, cyano, nitro, amino, monoC1-4alkylamino and diC1-4alkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.

    摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，溶剂合物或前体药物：其中R 1是C 1-6烷基，卤代C 1-6烷基，C 2-6烯基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; R 2和R 3可以相同或不同，为氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; 每个R 4可以相同或不同，为C 1-6烷基，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，硝基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; p为0,1或2; n为1或2; R 5和R 6可以相同或不同，为氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; 并且Het是噻吩基，吡啶基，嘧啶基，哒嗪基，嘧啶基，吡嗪基，咪唑基，吡唑基，吡咯基，喹啉基，噻唑基或呋喃基，其各自可以被一个或多个独立地选自C 1-6烷基， 1-6烷氧基，乙酰基，卤素，卤代C 1-6烷基，氰基，硝基，氨基，单C 1-4烷基氨基和二C 1-4烷基氨基。 还公开了化合物的制备方法及其在药物中的用途，例如精神分裂症的治疗。

    Compounds which potentiate glutamate receptor and uses thereof in medicine
    4.
    发明授权
    Compounds which potentiate glutamate receptor and uses thereof in medicine 失效
    增强谷氨酸受体的药物及其在药物中的应用

    公开(公告)号：US07741351B2

    公开(公告)日：2010-06-22

    申请号：US11573368

    申请日：2005-08-05

    申请人： Kevin Michael Thewlis ,  Simon Edward Ward

    发明人： Kevin Michael Thewlis ,  Simon Edward Ward

    IPC分类号： A61K31/425 ,  A61K31/40 ,  A61K31/275 ,  A61K31/17

    CPC分类号： C07D207/27 ,  C07C311/07 ,  C07C311/08 ,  C07C311/37 ,  C07C317/28 ,  C07C2602/08 ,  C07D275/02

    摘要： This case discloses compounds of formula (I) wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano or amino; each R4, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; p is 0, 1 or 2; each R5, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; q is 0, 1 or 2; R6 is —NR6aSO2R6b, —NR6aC(═O)R6b, —NR6a(C═O)N(R6c)2, —(C═O)R6d, —CH2NR6aSO2R6b, —CH2NR6aC(═O)R6b, CH2NR6a(C═O)N(R6c)2 or —CH2(C═O)R6d; where R6a and each R6c, which may be the same or different, is hydrogen or C1-6alkyl; R6b and R6d are C1-6alkyl or haloC1-6alkyl; or R6a and R6b, or R6a and R6c, together with the interconnecting atoms, may form a 5- or 6-membered ring; n is 1 or 2; and R7 and R8, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano or amino. It also discloses methods for preparing the compounds and their use in therapy such as treating schizophrenia.

    摘要翻译： 本例公开了式（I）的化合物，其中R 1是C 1-6烷基，卤代C 1-6烷基，C 2-6烯基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; R 2和R 3可以相同或不同，是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基或氨基; 每个R 4可以相同或不同，为C 1-6烷基，卤素，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，硝基或氨基; p为0,1或2; 每个R 5可以相同或不同，是C 1-6烷基，卤素，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，硝基或氨基; q是0,1或2; R6是-NR6aSO2R6b，-NR6aC（= O）R6b，-NR6a（C = O）N（R6c）2， - （C = O）R6d，-CH2NR6aSO2R6b，-CH2NR6aC（= O）R6b，CH2NR6a ）N（R6c）2或-CH2（C = O）R6d; 其中R 6a和R 6c可以相同或不同，是氢或C 1-6烷基; R6b和R6d是C1-6烷基或卤代C 1-6烷基; 或R6a和R6b或R6a和R6c与互连原子一起可以形成5-或6-元环; n为1或2; 和可以相同或不同的R 7和R 8是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基或氨基。 它还公开了制备化合物的方法及其在诸如治疗精神分裂症的治疗中的用途。

    Compounds which potentiate glutamate receptor and uses thereof in medicine
    6.
    发明授权
    Compounds which potentiate glutamate receptor and uses thereof in medicine 失效

    公开(公告)号：US07618969B2

    公开(公告)日：2009-11-17

    申请号：US11573370

    申请日：2005-08-05

    申请人： Daniel Marcus Bradley ,  Kevin Michael Thewlis ,  Simon Edward Ward

    发明人： Daniel Marcus Bradley ,  Kevin Michael Thewlis ,  Simon Edward Ward

    IPC分类号： A61K31/44 ,  C07D213/02

    CPC分类号： C07D213/64 ,  C07D213/42 ,  C07D213/50 ,  C07D213/61 ,  C07D213/84 ,  C07D213/85 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D333/20

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of C1-6alkyl, C1-6alkoxy, acetyl, halogen, haloC1-6alkyl, cyano, nitro, amino, monoC1-4alkylamino and diC1-4alkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.

    4-PHENYL-3-(2-PROPYLSULFONYLAMINO) TETRAHYDROFURAN DERIVATIVES WHICH POTENTIATE GLUTAMATE RECEPTORS AND ARE USEFUL IN THE TREATMENT OF SCHIZOPHRENIA
    9.
    发明申请
    4-PHENYL-3-(2-PROPYLSULFONYLAMINO) TETRAHYDROFURAN DERIVATIVES WHICH POTENTIATE GLUTAMATE RECEPTORS AND ARE USEFUL IN THE TREATMENT OF SCHIZOPHRENIA 审中-公开
    4-硝基-3-（2-丙磺酰氨基）四氢呋喃衍生物，它们是可溶性谷氨酸受体，并且有助于治疗精神病药

    公开(公告)号：US20090221643A1

    公开(公告)日：2009-09-03

    申请号：US12278602

    申请日：2007-02-06

    申请人： Kevin Michael Thewlis ,  Simon Edward Ward

    发明人： Kevin Michael Thewlis ,  Simon Edward Ward

    IPC分类号： A61K31/4439 ,  C07D405/10 ,  A61P25/18 ,  C07D307/22 ,  A61K31/341 ,  C07D325/00 ,  A61K31/357 ,  C07D409/10 ,  A61K31/381

    CPC分类号： C07D307/22 ,  C07D405/10 ,  C07D407/10 ,  C07D409/10

    摘要： Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl and thienyl optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, cyano, C(O)C1-4alkyl, NHSO2C1-4alkyl, NMeSO2C1-4alkyl, NHCOC1-4alkyl, NMeCOC1-4alkyl, SOC1-4alkyl, SO2C1-4alkyl and CO2C1-4alkyl, or two Y groups together form a cyclic group —O(CH2)O—. Processes for preparation, and uses thereof in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.

    摘要翻译： 提供式（I）化合物，其盐和溶剂化物：其中Ar选自苯基，吡啶基和任选被一个或多个Y基团取代的噻吩基; 并且每个Y基团独立地选自：卤素，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，氰基，C（O）C 1-4烷基，NHSO 2 C 1-4烷基，NMeSO 2 C 1-4烷基，NHCOC 1-4烷基，NMeCOC 1 - 烷基，SO1-4烷基，SO2C1-4烷基和CO2C1-4烷基，或两个Y基团一起形成环状基团-O（CH 2）O-。 还公开了制备方法及其用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症的用途。

    COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE
    10.
    发明申请
    COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE 失效

    公开(公告)号：US20080194648A1

    公开(公告)日：2008-08-14

    申请号：US11673044

    申请日：2007-02-09

    申请人： Daniel Marcus Bradley ,  Kevin Michael Thewlis ,  Simon Edward Ward

    发明人： Daniel Marcus Bradley ,  Kevin Michael Thewlis ,  Simon Edward Ward

    IPC分类号： A61K31/44 ,  A61P25/18 ,  C07D211/84

    CPC分类号： C07D213/64 ,  C07D213/42 ,  C07D213/50 ,  C07D213/61 ,  C07D213/84 ,  C07D213/85 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D333/20

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of C1-6alkyl, C1-6alkoxy, acetyl, halogen, haloC1-6alkyl, cyano, nitro, amino, monoC1-4alkylamino and diC1-4alkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.