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66 条记录 (耗时 0.042 秒)

    Method of using p-acylaminophenoxycarbamates and derivatives as analgesics
    2.
    发明授权
    Method of using p-acylaminophenoxycarbamates and derivatives as analgesics 失效
    使用对氨基苯氧基氨基甲酸酯和衍生物作为止痛剂的方法

    公开(公告)号：US5214061A

    公开(公告)日：1993-05-25

    申请号：US837190

    申请日：1992-02-18

    申请人： Richard C. Allen ,  Raymond W. Kosley, Jr. ,  Bettina Spahl

    发明人： Richard C. Allen ,  Raymond W. Kosley, Jr. ,  Bettina Spahl

    IPC分类号： C07C271/40 ,  C07C271/44 ,  C07D213/54 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07C271/40 ,  C07C271/44 ,  C07D213/54 ,  C07D233/56 ,  C07D249/08

    摘要： This invention relates to p-acylaminophenoxycarbamates having the formula ##STR1## where R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl, aryl and arylloweralkyl; R.sub.3 is hydrogen, loweralkyl, arylloweralkyl; R.sub.4 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkyl, phenylcarbonyl, arylloweralkylcarbonyl, substituted phenylcarbonyl, pyridylcarbonyl, and substituted pyridylcarbonyl with the proviso that if R.sub.4 contains a carbonyl group directly attached to the oxygen of the N-O moiety, R.sub.3 cannot be hydrogen; or R.sub.3 and R.sub.4 taken together from a heterocyclic ring selected from the group consisting of imidazole or loweralkylimidazole; X is hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; and p is an integer selected from 0 and 1; the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics.

    摘要翻译： 本发明涉及具有式“IMAGE”的对酰氨基苯氧基氨基甲酸酯，其中R 1和R 2各自独立地为氢，低级烷基，芳基和芳基低级烷基; R3是氢，低级烷基，芳基低级烷基; R4是氢，低级烷基，甲酰基，烷基羰基，芳基低级烷基，苯基羰基，芳基低级烷基羰基，取代的苯基羰基，吡啶基羰基和取代的吡啶基羰基，条件是如果R4含有直接键合在N-O部分的氧上的羰基，则R3不能是氢; 或者R 3和R 4一起选自咪唑或低级烷基咪唑的杂环; X是氢，卤素，羟基，低级烷基，低级烷氧基，硝基，氨基或三氟甲基; 并且p是选自0和1的整数; 其药学上可接受的酸加成盐，以及适用的几何和立体异构体及其外消旋混合物。 本发明化合物显示出作为止痛剂的效用。

    [1-indanon-2-yl]methylpiperidines
    8.
    发明授权
    [1-indanon-2-yl]methylpiperidines 失效
    [1-茚满酮-2-基]甲基哌啶

    公开(公告)号：US06413986B1

    公开(公告)日：2002-07-02

    申请号：US08435079

    申请日：1995-05-08

    申请人： Raymond W. Kosley, Jr. ,  Bettina Spahl ,  Richard C. Effland

    发明人： Raymond W. Kosley, Jr. ,  Bettina Spahl ,  Richard C. Effland

    IPC分类号： A61K31445

    CPC分类号： C07D213/50 ,  C07D211/32

    摘要： Novel [[(aminocarbonyloxy)-1-indan]-2-yl]methylpiperidines of the formula wherein R is hydrogen, loweralkyl, or a group of the formula R1 is hydrogen or a group of the formula W, X and Y are hydrogen, loweralkyl, loweralkoxy, halogen, nitrogen, or trifluoromethyl; n is 1 or 2; the pharmaceutically acceptable acid addition salts thereof intermediates of the formula and process for the preparation thereof, and a method of relieving memory dysfunction, employing compounds and compositions thereof are disclosed.

    摘要翻译： 式（Ⅳ）的新型[[（氨基羰氧基）-1-茚满] -2-基]甲基哌啶是氢，低级烷基或式R 1的基团是氢或式W的基团，X和Y是氢，低级烷基，低级烷氧基 ，卤素，氮或三氟甲基; n为1或2; 公开了其药学上可接受的酸式加成盐及其制备方法及其制备方法，以及使用化合物及其组合物缓解记忆功能障碍的方法。

    Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof
    10.
    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。