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    Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof
    1.
    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。

    Galanthamine derivatives as acetylcholinesterase inhibitors
    4.
    发明授权
    Galanthamine derivatives as acetylcholinesterase inhibitors 失效
    Galanthamine衍生物作为乙酰胆碱酯酶抑制剂

    公开(公告)号：US06316439B1

    公开(公告)日：2001-11-13

    申请号：US08137444

    申请日：1993-10-15

    申请人： Raymond W. Kosley, Jr. ,  Larry Davis ,  Veronica Taberna

    发明人： Raymond W. Kosley, Jr. ,  Larry Davis ,  Veronica Taberna

    IPC分类号： C07D49106

    CPC分类号： C07D491/10

    摘要： This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12)alkylcarbonyl, (C1-C12)alkoxycarbonyl, aryl(C1-C12)alkylaminocarbonyl, mono(C1-C18)alkylaminocarbonyl or di(C1-C8)alkylaminocarbonyl; R2 is (C1-C12)alkylcarbonyloxy, aryl(C1-C4)alkylcarbonyloxy, (C1-C12)alkoxycarbonyloxy, arylcarbonyloxy, hydroxy, (C1-C6)alkoxycarbonyl(C1-C6)alkoxy or hydroxy(C1-C10)alkoxy; R3 is hydrogen or halo; and pharmaceutically acceptable addition salts; with the proviso that when R2 is hydroxy, R1 and R3 are not both hydrogen or when R2 is hydroxy and R3 is hydrogen, R1 is not methylcarbonyl; which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.

    摘要翻译： 本申请涉及式（Ⅳ）化合物，其中R1是氢，（C1-C12）烷基羰基，（C1-C12）烷氧基羰基，芳基（C1-C12）烷基氨基羰基，单（C1-C18）烷基氨基羰基或二（C1-C8）烷基氨基羰基; R2是（C1-C12）烷基羰基氧基，芳基（C1-C4）烷基羰基氧基，（C1-C12）烷氧基羰氧基，芳基羰基氧基，羟基，（C1-C6）烷氧羰基（C1-C6）烷氧基或羟基（C1-C10） 是氢或卤素; 和药学上可接受的加成盐; 条件是当R 2是羟基时，R 1和R 3不是氢或当R 2是羟基且R 3是氢时，R 1不是甲基羰基;这些化合物可用于治疗以胆碱能功能降低为特征的记忆功能障碍，含有 化合物的制备和使用方法。