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15 条记录 (耗时 0.044 秒)

    Prodrugs of inhibitors of farnesyl-protein transferase
    7.
    发明授权
    Prodrugs of inhibitors of farnesyl-protein transferase 失效
    法呢基蛋白转移酶抑制剂的前药

    公开(公告)号：US5534537A

    公开(公告)日：1996-07-09

    申请号：US412830

    申请日：1995-03-29

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

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

    IPC分类号： C07C323/59 ,  C07D233/54 ,  C07D233/56 ,  A61K31/41 ,  C07D403/12

    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。

    Peptides having ANF activity
    10.
    发明授权
    Peptides having ANF activity 失效
    具有ANF活性的肽

    公开(公告)号：US5091366A

    公开(公告)日：1992-02-25

    申请号：US534001

    申请日：1990-06-04

    申请人： Ruth F. Nutt ,  Terrence M. Ciccarone ,  Stephen F. Brady ,  Daniel F. Veber

    发明人： Ruth F. Nutt ,  Terrence M. Ciccarone ,  Stephen F. Brady ,  Daniel F. Veber

    IPC分类号： A61K38/00 ,  C07K14/58

    CPC分类号： C07K14/58 ,  A61K38/00

    摘要： Analogs of the 17-membered ring portion of ANF wherein the cysteine moiety is replaced with dipeptidyl moieties, specifically, Phe-Pro, NMP-Pro, Pro-Pro, Val-Pro, Lys-Pro, Ile-Pro, Arg-Pro, HAr-Pro, Dly-Pro, Arg-Pro, Lys-BAr, Arg-Pro, CyA-CyA, Cys-Cys, or with .alpha.-aminoheptanoic acid result in analogs of ANF having increased potencies and metabolic stability.

    摘要翻译： ANF的17-元环部分的类似物，其中半胱氨酸部分被二肽基部分，特别是Phe-Pro，NMP-Pro，Pro-Pro，Val-Pro，Lys-Pro，Ile-Pro，Arg-Pro， HAr-Pro，Dly-Pro，Arg-Pro，Lys-BAr，Arg-Pro，CyA-CyA，Cys-Cys或α-氨基庚酸导致ANF的类似物具有增加的效力和代谢稳定性。