利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

56 条记录 (耗时 0.045 秒)

    Benzamide-containing inhibitors of farnesyl-protein transferase
    12.
    发明授权
    Benzamide-containing inhibitors of farnesyl-protein transferase 失效
    含有苯甲酰胺的法呢基蛋白转移酶抑制剂

    公开(公告)号：US5578629A

    公开(公告)日：1996-11-26

    申请号：US413137

    申请日：1995-03-29

    申请人： Terrence M. Ciccarone ,  Theresa M. Williams ,  Suzanne C. MacTough

    发明人： Terrence M. Ciccarone ,  Theresa M. Williams ,  Suzanne C. MacTough

    IPC分类号： C07C323/59 ,  C07D233/54 ,  C07D277/04 ,  C07C237/20 ,  C07C321/10 ,  C07C323/29 ,  C07D277/12

    CPC分类号： C07D233/64 ,  C07C323/59

    摘要： The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors differ from those previously described as inhibitors of farnesyl-protein 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： 本发明包括含有适当取代的氨基烷基苯甲酰胺部分的拟肽化合物。 本化合物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。 此外，法呢基蛋白转移酶抑制剂与先前描述为法呢基蛋白转移酶抑制剂的不同之处在于它们不具有硫醇部分。 缺乏硫醇在改善动物药代动力学行为方面提供独特的优势，防止硫醇依赖的化学反应，如快速自身氧化和内源性硫醇形成二硫键，并减少全身毒性。 本发明还包含含有这些法呢基转移酶抑制剂的化疗组合物及其生产方法。

    CGRP receptor antagonists
    14.
    发明授权
    CGRP receptor antagonists 有权
    CGRP受体拮抗剂

    公开(公告)号：US07632832B2

    公开(公告)日：2009-12-15

    申请号：US11795678

    申请日：2006-01-13

    申请人： Christopher S. Burgey ,  Theresa M. Williams ,  Zhengwu J. Deng ,  Craig A. Stump

    发明人： Christopher S. Burgey ,  Theresa M. Williams ,  Zhengwu J. Deng ,  Craig A. Stump

    IPC分类号： C07D401/14 ,  A61K31/4745 ,  A61P25/06

    CPC分类号： C07D401/14

    摘要： Compounds of Formula I: (where variables R1, R2, R3, R7, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache, and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

    摘要翻译： 式I化合物（其中变量R1，R2，R3，R7，G，J，Q，T，W，X和Y如本文所定义）可用作CGRP受体的拮抗剂，可用于治疗或预防 CGRP涉及，如头痛，偏头痛和丛集性头痛，以及包含这些化合物的药物组合物，以及这些化合物和组合物在预防或治疗CGRP所涉及的疾病中的用途。

    Benzodiazepine CGRP receptor antagonists
    16.
    发明授权
    Benzodiazepine CGRP receptor antagonists 有权
    苯二氮卓CGRP受体拮抗剂

    公开(公告)号：US07196079B2

    公开(公告)日：2007-03-27

    申请号：US10562298

    申请日：2004-06-24

    申请人： Christopher S. Burgey ,  Craig A. Stump ,  Theresa M. Williams

    发明人： Christopher S. Burgey ,  Craig A. Stump ,  Theresa M. Williams

    IPC分类号： C07D401/14 ,  A61K31/55 ,  A61P25/06

    CPC分类号： C07D401/14

    摘要： The present invention is directed to compounds of Formula I: (where variables R1, R2, R3, R6, R7, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.

    摘要翻译： 本发明涉及式I化合物：