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39 条记录 (耗时 0.023 秒)

    SPIRO-PIPERIDINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
    17.
    发明公开
    SPIRO-PIPERIDINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 失效
    螺哌啶衍生物及其作为药物

    公开(公告)号：EP0912579A1

    公开(公告)日：1999-05-06

    申请号：EP97928357.0

    申请日：1997-06-24

    申请人： MERCK SHARP & DOHME LTD.

    发明人： CURTIS, Neil, Roy ,  HUSCROFT, Ian, Thomas ,  KULAGOWSKI, Janusz, Jozef ,  SWAIN, Christopher, John

    IPC分类号： H04L12 ,  A61K31 ,  C07D491

    CPC分类号： C07D491/10 ,  A61K31/438

    摘要： The present invention relates to compounds of formula (I), wherein R is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalyklC1-4alkyl, which groups are optionally substituted by hydroxy, C1-4alkoxy or NRaRb, where R?a and Rb¿ each independently represent hydrogen or C¿1-4?alkyl; or R is C1-4alkyl substituted by Ar, and optionally further substituted by one or both of R?4 and R5; R1, R2 and R3¿ represent a variety of substituents; R?9 and R10¿ are each hydrogen, halogen, C¿1-6?alkyl, CH2OR?e¿, oxo, CO¿2R?a or CONRaRb where Re represents hydrogen, C¿1-6?alkyl or phenyl; X is -CH2, or -CH2CH2-; Y is -CH=, -CH2-, -CH2CH= or -CH2CH2-, with the proviso that the sum total of carbon atoms in X+Y is 2 or 3; and when Y is -CH= or -CH2CH=, the broken line is a double bond; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

    SPIRO-KETAL DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
    18.
    发明公开
    SPIRO-KETAL DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 失效
    螺 - 酮衍生物及其作为治疗剂的用途

    公开(公告)号：EP0880528A1

    公开(公告)日：1998-12-02

    申请号：EP97903437.0

    申请日：1997-02-12

    申请人： MERCK SHARP & DOHME LTD.

    发明人： ELLIOTT, Jason, Matthew ,  KELLEHER, Fintan ,  SWAIN, Christopher, John

    IPC分类号： A61K31 ,  A61P1 ,  A61P11 ,  A61P19 ,  A61P25 ,  A61P29 ,  A61P43 ,  C07D498

    CPC分类号： C07D498/10

    摘要： The present invention relates to compounds of formula (I), wherein R?1, R2, R4, R5 and R6¿ represent a variety of substituents; R3 represents an optionally substituted 5- or 6- membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur. R?9a and R9b¿ each independently represent hydrogen or C¿1-4?alkyl, or R?9a and R9b¿ are joined so, together with the carbon atoms to which they are attached, there is formed a C¿5-7? ring; m is zero, 1, 2 or 3; and n is zero, 1, 2 or 3; with the proviso that the sum total of m and n is 2 or 3; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

    摘要翻译： 本发明涉及式（I）的化合物，其中R 1，R 2，R 4，R 5和R 6'代表多种取代基; R 3代表任选取代的含有1,2,3或4个选自氮，氧和硫的杂原子的5-或6-元芳族杂环基团。 R 9a和R 9b各自独立地代表氢或C 1-4烷基，或者R 9a和R 9b连接在一起，与它们所连接的碳原子一起形成C 5-7 ？ 环; m是0,1,2或3; 并且n是0,1,2或3; 条件是m和n的总和为2或3; 或其药学上可接受的盐。 该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。