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12 条记录 (耗时 0.018 秒)

    2-SUBSTITUTED PROLINE BIS-AMIDE OREXIN RECEPTOR ANTAGONISTS
    3.
    发明公开
    2-SUBSTITUTED PROLINE BIS-AMIDE OREXIN RECEPTOR ANTAGONISTS 审中-公开
    2-取代的脯氨酸双酰胺食欲素受体拮抗剂

    公开(公告)号：EP2049526A2

    公开(公告)日：2009-04-22

    申请号：EP07810508.7

    申请日：2007-07-13

    申请人： Merck & Co., Inc.

    发明人： COX, Christopher, D. ,  WHITMAN, David, B. ,  BRESLIN, Michael, J.

    IPC分类号： C07D403/06

    CPC分类号： C07D403/06 ,  C07D403/12 ,  C07D403/14

    摘要： The present invention is directed to 2-substituted proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

    DIAZASPIRODECANE OREXIN RECEPTOR ANTAGONISTS
    4.
    发明公开
    DIAZASPIRODECANE OREXIN RECEPTOR ANTAGONISTS 审中-公开
    DIAZASPIRODECAN食欲肽受体拮抗剂

    公开(公告)号：EP1922071A2

    公开(公告)日：2008-05-21

    申请号：EP06802269.8

    申请日：2006-08-24

    申请人： Merck & Co., Inc.

    发明人： BRESLIN, Michael, J. ,  COX, Christopher, D. ,  WHITMAN, David, B.

    IPC分类号： A61K31/4747 ,  C07D471/10

    CPC分类号： C07D471/10

    摘要： The present invention is directed to diazaspirodecane compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

    MITOTIC KINESIN INHIBITORS
    5.
    发明公开
    MITOTIC KINESIN INHIBITORS 审中-公开
    MITOTIC KINESIN抑制剂

    公开(公告)号：EP1851213A2

    公开(公告)日：2007-11-07

    申请号：EP06734469.7

    申请日：2006-02-06

    申请人： Merck & Co., Inc.

    发明人： BRESLIN, Michael, J. ,  WHITMAN, David, B. ,  NEILSON, Lou Anne ,  COX, Christopher, D. ,  COLEMAN, Paul, J.

    IPC分类号： C07D405/12 ,  C07D207/50 ,  A61K31/40 ,  A61K31/4025

    CPC分类号： C07D491/052

    摘要： The present invention relates to tricyclic pyrazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

    摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，治疗与KSP驱动蛋白活性有关的病症和用于抑制KSP驱动蛋白的三环吡唑类。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

    INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
    8.
    发明公开
    INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 失效
    法尼蛋白转移酶抑制剂

    公开(公告)号：EP0783318A1

    公开(公告)日：1997-07-16

    申请号：EP95933956.0

    申请日：1995-09-25

    申请人： Merck & Co., Inc.

    发明人： BRESLIN, Michael, J. ,  deSOLMS, S., Jane ,  GRAHAM, Samuel, L. ,  HUTCHINSON, John, H. ,  STOKKER, Gerald, E.

    IPC分类号： A61K38 ,  A61P35 ,  A61P43 ,  C07C229 ,  C07C237 ,  C07C255 ,  C07C323 ,  C07K5

    CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07K5/0808

    摘要： The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogs differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

    摘要翻译： 本发明包括被体内法尼基化修饰的蛋白质Ras的CAAX基序的类似物。 这些CAAX类似物抑制Ras的法尼基化。 此外，这些CAAX类似物不同于之前描述为Ras法尼基转移酶抑制剂的那些，因为它们不具有硫醇部分。 缺乏巯基在改善动物中的药代动力学行为，防止巯基依赖性化学反应如快速自动氧化和与内源硫醇形成二硫化物以及降低全身毒性方面提供了独特优势。 本发明还包含含有这些法尼基转移酶抑制剂的化学治疗组合物及其制备方法。