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    SUBSTITUTED DIHYDRO AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
    1.
    发明申请
    SUBSTITUTED DIHYDRO AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF 审中-公开
    取代的二羟基和四氢呋喃氧杂二恶嗪，其制备和使用

    公开(公告)号：WO2008112483A3

    公开(公告)日：2009-01-15

    申请号：PCT/US2008056002

    申请日：2008-03-06

    Applicant: SANOFI AVENTIS ,  CAO BIN ,  GURUNIAN VIEROSLAVA ,  KONGSAMUT SATHAPANA ,  KOSLEY JR RAYMOND W ,  SHER ROSY ,  HARTUNG RYAN E

    Inventor： CAO BIN ,  GURUNIAN VIEROSLAVA ,  KONGSAMUT SATHAPANA ,  KOSLEY JR RAYMOND W ,  SHER ROSY ,  HARTUNG RYAN E

    IPC: C07D498/04 ,  A61K31/519 ,  A61P25/06 ,  A61P25/18 ,  A61P25/24 ,  A61P29/00

    CPC classification number: C07D498/04

    Abstract: 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.

    Abstract translation: 本发明涉及一系列取代的二氢和四氢恶唑啉嘧啶酮，具体地涉及一系列2-取代-2,3-二氢 - 恶唑并[3,2-a]嘧啶-7-酮和2-取代-2,4-二氢吡喃并[ （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 AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
    5.
    发明申请
    SUBSTITUTED DIHYDRO AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF 审中-公开
    取代的二羟基和四氢呋喃氧杂二恶嗪，其制备和使用

    公开(公告)号：WO2008112483A2

    公开(公告)日：2008-09-18

    申请号：PCT/US2008/056002

    申请日：2008-03-06

    Applicant: SANOFI-AVENTIS ,  CAO, Bin ,  GURUNIAN, Vieroslava ,  KONGSAMUT, Sathapana ,  KOSLEY, Jr., Raymond, W. ,  SHER, Rosy ,  HARTUNG, Ryan E.

    Inventor： CAO, Bin ,  GURUNIAN, Vieroslava ,  KONGSAMUT, Sathapana ,  KOSLEY, Jr., Raymond, W. ,  SHER, Rosy ,  HARTUNG, Ryan E.

    CPC classification number: C07D498/04

    Abstract: 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, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 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.

    Abstract translation: 本发明涉及一系列取代的二氢和四氢恶唑啉嘧啶酮，具体地涉及一系列2-取代-2,3-二氢 - 恶唑并[3,2-a]嘧啶-7-酮和2-取代-2,4-二氢吡喃并[ （I）的3,5,6-四氢恶唑并[3,2-a]嘧啶-7-酮：其中p，n，X，Y，R 1， R 3，R 3，R 4，R 5，R 6，R 6， R 7和R 8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。

    METHOD OF TREATING SCHIZOPHRENIA AND/OR GLUCOREGULATORY ABNORMALITIES
    6.
    发明申请
    METHOD OF TREATING SCHIZOPHRENIA AND/OR GLUCOREGULATORY ABNORMALITIES 审中-公开
    治疗嗜酸性粒细胞减少症和/或葡萄糖不育症的方法

    公开(公告)号：WO2005097122A2

    公开(公告)日：2005-10-20

    申请号：PCT/US2005/011107

    申请日：2005-04-01

    Applicant: AVENTIS PHARMACEUTICALS INC. ,  SMITH, Craig, P. ,  RAMPE, David, E. ,  BOROWSKY, Beth ,  KONGSAMUT, Sathapana

    Inventor： SMITH, Craig, P. ,  RAMPE, David, E. ,  BOROWSKY, Beth ,  KONGSAMUT, Sathapana

    IPC: A61K31/4439

    CPC classification number: A61K31/4439

    Abstract: The present invention provides methods of treating schizophrenia and/or glucoregulatory abnormalities in a patient in need thereof comprising administering to said patient a therapeutically effective amount of a compound of formula (I) wherein m is 0, 1 or 2; n is 0, 1 or 2; p is 0 or 1; each R is independently hydrogen, halogen, trifluoromethyl, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, benzyloxy, hydroxy, nitro or amino; each R 1 is independently hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkenyl, C 1 -C 6 alkanoyl, halogen, cyano, -C(O) C 1 -C 6 alkyl, -C 1 -C 6 alkyleneCN, -C 1 -C 6 alkyleneNR’R” wherein R’ and R” are each independently hydrogen or C 1 -C 6 alkyl, -C 1 -C 6 alkyleneOC(O)C 1 -C 6 alkyl, or -CH(OH)R 4 wherein R 4 is hydrogen or C 1 -C 6 alkyl; R 2 is hydrogen, C 1 -C 6 alkyl optionally substituted with halogen, hydroxy or benzyloxy, C 1 -C 6 alkenyl, C 1 -C 6 alkynyl, -CO 2 C 1 -C 6 alkyl, or -R 5 -NR’R” wherein R 5 is C 1 -C 6 alkylene, C 1 -C 6 alkenylene or C 1 -C 6 alkynylene and R’ and R” are each independently hydrogen, C 1 -C 6 alkyl or alternatively the group -NR’R” as a whole is 1-pyrrolidinyl; and R 3 is hydrogen, nitro, amino, halogen, C 1 -C 6 alkoxy, hydroxy or C 1 -C 6 alkyl or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明提供在有需要的患者中治疗精神分裂症和/或葡萄糖调节异常的方法，包括向所述患者施用治疗有效量的式（I）化合物，其中m为0,1或2; n为0,1或2; p为0或1; 每个R独立地是氢，卤素，三氟甲基，C 1 -C 6烷基，C 1 -C 6烷氧基，苄氧基，羟基，硝基或氨基; 每个R 1独立地是氢，C 1 -C 6烷基，C 1 -C 6烯基，C 1 -C 6烷酰基，卤素，氰基，-C（O）C 1 -C 6烷基，-C 1 -C 6亚烷基基团，-C 1 -C 6亚烷基NR'R“，其中R'和R” 各自独立地是氢或C 1 -C 6烷基，-C 1 -C 6亚烷基OC（O）C 1 -C 6烷基或-CH（OH）R 4，其中R 4是氢或C 1 -C 6烷基; R 2是氢，任选地被卤素，羟基或苄氧基取代的C 1 -C 6烷基，C 1 -C 6烯基，C 1 -C 6炔基，-CO 2 C 1 -C 6烷基或-R 5 -NR'R“，其中R 5是C 1 -C 6亚烷基， C 6亚炔基和R'和R“各自独立地为氢，C 1 -C 6烷基或者基团-NR'R”整体上为1-吡咯烷基; R 3为氢，硝基，氨基，卤素，C 1 -C 6烷氧基，羟基或C 1 -C 1-6烷基或其药学上可接受的盐。

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