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    Substituted dihydro, trihydro and tetrahydro cycloalkyloxazolopyrimidinones, preparation and use thereof
    2.
    发明授权
    Substituted dihydro, trihydro and tetrahydro cycloalkyloxazolopyrimidinones, preparation and use thereof 有权
    取代的二氢，三氢和四氢环烷基唑并吡咯酮，其制备和应用

    公开(公告)号：US08207181B2

    公开(公告)日：2012-06-26

    申请号：US12875700

    申请日：2010-09-03

    申请人： Raymond Walter Kosley, Jr. ,  Rosy Sher

    发明人： Raymond Walter Kosley, Jr. ,  Rosy Sher

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00

    CPC分类号： C07D498/04

    摘要： The present disclosure relates to a series of 2-substituted-di- tri or tetra-hydro-8H-cyclopentaoxazolo[3,2-a]pyrimidin-8-ones and 2-substituted-di-, tetra-, or hexa-hydro-cyclohexaoxazolo[3,2-a]pyrimidin-9-ones of formula (I): wherein p, n, A, B, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

    摘要翻译： 本公开涉及一系列2-取代二 - 二或四氢-8H-环五唑并[3,2-a]嘧啶-8-酮和2-取代二 - ，四 - 或六氢 - - 环己氧氮杂并[3,2-a]嘧啶-9-酮其中p，n，A，B，X，Y，R1，R2，R3，R4，R5，R6，R7和R8分别为 本文定义。 本发明还涉及制备这些化合物的方法，包括新型中间体。 本发明的化合物是代谢型谷氨酸受体（mGluR），特别是mGluR2受体的调节剂。 因此，本发明的化合物可用作药物，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经变性疾病，精神病，抽搐，焦虑， 抑郁症，偏头痛，疼痛，睡眠障碍和呕吐。

    Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof
    5.
    发明授权
    Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof 有权
    取代的二氢和四氢恶唑啉嘧啶酮，其制备和应用

    公开(公告)号：US08642603B2

    公开(公告)日：2014-02-04

    申请号：US12554129

    申请日：2009-09-04

    申请人： Bin Cao ,  Vieroslava Gurunian ,  Sathapana Kongsamut ,  Raymond W. Kosley, Jr. ,  Rosy Sher ,  Ryan E. Hartung

    发明人： Bin Cao ,  Vieroslava Gurunian ,  Sathapana Kongsamut ,  Raymond W. Kosley, Jr. ,  Rosy Sher ,  Ryan E. Hartung

    IPC分类号： C07D491/04 ,  A61K31/519 ,  A61P25/28 ,  A61P25/22 ,  A61P25/18 ,  A61P25/06 ,  A61P25/02

    CPC分类号： C07D498/04

    摘要： The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

    摘要翻译： 本发明涉及一系列取代的二氢和四氢恶唑啉嘧啶酮，特别涉及一系列2-取代-2,3-二氢 - 恶唑并[3,2-a]嘧啶-7-酮和2-取代-2,2-二氧杂唑并[ （I）的3,5,6-四氢恶唑并[3,2-a]嘧啶-7-酮：其中p，n，X，Y，R1，R2，R3，R4，R5，R6， R7和R8如本文所定义。 本发明还涉及制备这些化合物的方法，包括新型中间体。 本发明的化合物是代谢型谷氨酸受体（mGluR），特别是mGluR2受体的调节剂。 因此，本发明的化合物可用作药物，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经变性疾病，精神病，抽搐，焦虑， 抑郁症，偏头痛，疼痛，睡眠障碍和呕吐。

    Substituted dihydro benzocycloalkyloxymethyl oxazolopyrimidinones, preparation and use thereof
    8.
    发明授权
    Substituted dihydro benzocycloalkyloxymethyl oxazolopyrimidinones, preparation and use thereof 有权
    取代的二氢苯并环烷氧基甲基恶唑啉嘧啶酮，其制备和应用

    公开(公告)号：US09051331B2

    公开(公告)日：2015-06-09

    申请号：US13410723

    申请日：2012-03-02

    申请人： Rosy Sher ,  Raymond Walter Kosley, Jr.

    发明人： Rosy Sher ,  Raymond Walter Kosley, Jr.

    IPC分类号： C07D491/048 ,  C07D498/04 ,  A61K31/519 ,  A61K31/522

    CPC分类号： C07D498/04 ,  A61K31/519 ,  A61K31/522

    摘要： The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I): Wherein n, R1, R2, R3, R4, R5 and R6 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

    摘要翻译： 本发明涉及式（I）的一系列取代的二氢苯并环烷基 - 氧甲基恶唑啉嘧啶酮：其中n，R1，R2，R3，R4，R5和R6如本文所定义。 本发明还涉及制备这些化合物的方法，包括新型中间体。 本发明的化合物是代谢型谷氨酸受体（mGluR），特别是mGluR2受体的调节剂。 因此，本发明的化合物可用作药剂，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经变性疾病，精神病，认知缺陷障碍， 惊厥，焦虑，抑郁，偏头痛，疼痛，睡眠障碍和呕吐。

    SUBSTITUTED DIHYDRO BENZOCYCLOALKYLOXYMETHYL OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
    9.
    发明申请
    SUBSTITUTED DIHYDRO BENZOCYCLOALKYLOXYMETHYL OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF 有权
    取代二氢苯并二氧杂环戊烯甲氧基亚胺基嘧啶，其制备及其用途

    公开(公告)号：US20120184566A1

    公开(公告)日：2012-07-19

    申请号：US13410723

    申请日：2012-03-02

    申请人： Rosy SHER ,  Raymond Walter KOSLEY, JR.

    发明人： Rosy SHER ,  Raymond Walter KOSLEY, JR.

    IPC分类号： A61K31/519 ,  A61P25/22 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  A61P25/08 ,  C07D498/04 ,  A61P25/06

    CPC分类号： C07D498/04 ,  A61K31/519 ,  A61K31/522

    摘要： The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I): Wherein n, R1, R2, R3, R4, R5 and R6 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

    摘要翻译： 本发明涉及式（I）的一系列取代的二氢苯并环烷基 - 氧甲基恶唑啉嘧啶酮：其中n，R1，R2，R3，R4，R5和R6如本文所定义。 本发明还涉及制备这些化合物的方法，包括新型中间体。 本发明的化合物是代谢型谷氨酸受体（mGluR），特别是mGluR2受体的调节剂。 因此，本发明的化合物可用作药剂，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经变性疾病，精神病，认知缺陷障碍， 惊厥，焦虑，抑郁，偏头痛，疼痛，睡眠障碍和呕吐。

    Dipyrazole compounds and their use as central nervous system agents
    10.
    发明授权
    Dipyrazole compounds and their use as central nervous system agents 失效
    二吡唑类化合物及其作为中枢神经系统药物的用途

    公开(公告)号：US08053458B2

    公开(公告)日：2011-11-08

    申请号：US11855521

    申请日：2007-09-14

    申请人： Raymond W. Kosley ,  Douglas MacDonald ,  Rosy Sher

    发明人： Raymond W. Kosley ,  Douglas MacDonald ,  Rosy Sher

    IPC分类号： A61K31/455 ,  C07D231/26

    CPC分类号： C07D401/14 ,  C07D231/22 ,  C07D231/26

    摘要： The present invention is directed to dipyrazole compounds of formula I and their pharmaceutically acceptable salts, stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I. The compounds of this invention modulate AMPA and NMDA receptor function, and therefore are useful as pharmaceutical agents, especially for the treatment of neuropsychiatric disorders.

    摘要翻译： 本发明涉及式I的二吡唑化合物及其药学上可接受的盐，立体异构体，互变异构体或溶剂化物。 新型化合物包括式I化合物。本发明化合物调节AMPA和NMDA受体功能，因此可用作药剂，特别是用于治疗神经精神障碍。