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    Bisphenyl inhibitors of farnesyl-protein transferase
    8.
    发明授权
    Bisphenyl inhibitors of farnesyl-protein transferase 失效
    法呢基蛋白转移酶的二苯基抑制剂

    公开(公告)号：US5710171A

    公开(公告)日：1998-01-20

    申请号：US648330

    申请日：1996-05-15

    申请人： Christopher J. Dinsmore ,  Suzanne C. MacTough ,  Gerald E. Stokker ,  Theresa M. Williams

    发明人： Christopher J. Dinsmore ,  Suzanne C. MacTough ,  Gerald E. Stokker ,  Theresa M. Williams

    IPC分类号： A61K31/33 ,  A61K31/4164 ,  A61P13/12 ,  A61P31/10 ,  A61P31/12 ,  A61P35/00 ,  A61P43/00 ,  C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D521/00 ,  A61K31/415 ,  C07D233/56 ,  C07D233/60 ,  C07D403/02

    CPC分类号： C07D233/64

    摘要： The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzene and analine analogs, further substituted with a second phenyl ring attached via a bond, a heteroatom linker or an aliphatic linker. 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： 本发明包括拟肽化合物，其包含适当取代的氨基烷基苯和分析物类似物，进一步被通过键连接的第二苯环，杂原子连接体或脂族连接体取代。 本发明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。