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56 条记录 (耗时 0.037 秒)

    Phenyl-protein transferase inhibitors
    1.
    发明授权
    Phenyl-protein transferase inhibitors 失效
    苯基蛋白转移酶抑制剂

    公开(公告)号：US06333335B1

    公开(公告)日：2001-12-25

    申请号：US09609205

    申请日：2000-06-30

    申请人： Christopher J. Dinsmore ,  Samuel L. Graham ,  Theresa M. Williams

    发明人： Christopher J. Dinsmore ,  Samuel L. Graham ,  Theresa M. Williams

    IPC分类号： A61K31437

    CPC分类号： C07D471/04

    摘要： The present invention is directed to tetrahydro-imidazopyridinyl compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

    摘要翻译： 本发明涉及抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的四氢 - 咪唑并吡啶基化合物。 本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。

    Inhibitor of farnesyl-protein transferase
    3.
    发明授权
    Inhibitor of farnesyl-protein transferase 失效
    法呢基蛋白转移酶抑制剂

    公开(公告)号：US5703241A

    公开(公告)日：1997-12-30

    申请号：US729265

    申请日：1996-10-10

    申请人： S. Jane deSolms ,  Samuel L. Graham

    发明人： S. Jane deSolms ,  Samuel L. Graham

    IPC分类号： A61K38/00 ,  C07K5/06 ,  A61K31/415 ,  C07D403/02

    CPC分类号： C07K5/06026 ,  A61K38/00

    摘要： The present invention comprises an analog of the CA.sub.1 A.sub.2 X motif of the protein Ras that is modified by farnesylation in vivo. This CA.sub.1 A.sub.2 X analog inhibits the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, this CA.sub.1 A.sub.2 X analog differs from most compounds previously described as inhibitors of farnesyl-protein transferase in that it does 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. The compound of the instant invention also incorporates a cyclic amine moiety in the A.sup.1 position of the motif. Further contained in this invention are chemotherapeutic compositions containing this farnesyl transferase inhibitor and methods for its production.

    摘要翻译： 本发明包括通过体内法尼基化修饰的蛋白Ras的CA1A2X基序的类似物。 该CA1A2X类似物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。 此外，该CA1A2X类似物与先前描述为法呢基 - 蛋白转移酶抑制剂的大多数化合物不同，因为其不具有硫醇部分。 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。 本发明的化合物还在基序的A1位置加入环胺部分。 本发明还包含含有该法呢基转移酶抑制剂的化疗组合物及其生产方法。

    Bicyclic spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease
    10.
    发明授权
    Bicyclic spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease 有权
    双环哌啶哌啶β-分泌酶抑制剂用于治疗阿尔茨海默病

    公开(公告)号：US08377954B2

    公开(公告)日：2013-02-19

    申请号：US12522056

    申请日：2007-12-28

    申请人： Shaun R. Stauffer ,  Samuel L. Graham

    发明人： Shaun R. Stauffer ,  Samuel L. Graham

    IPC分类号： C07D401/14 ,  A61K31/438

    CPC分类号： C07D471/20

    摘要： The present invention is directed to bicyclic spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

    摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病如阿尔茨海默病的式（I）的双环螺哌啶化合物。 本发明还涉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治疗涉及β-分泌酶的疾病中的用途。