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    • 81. 发明授权
    • PDK-1/Akt signaling inhibitors
    • PDK-1 / Akt信号传导抑制剂
    • US08541460B2
    • 2013-09-24
    • US12118788
    • 2008-05-12
    • Ching-Shih Chen
    • Ching-Shih Chen
    • A61K31/415C07D231/10
    • C07D231/12
    • Use of a new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I for inducing apoptosis in unwanted rapidly proliferating cells, for treating, inhibiting, or delaying the onset of cancer, and for preventing restenosis in a subject that has undergone an angioplasty or stent: wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, C1-C4 haloalkyl, azido, C1-C4 azidoalkyl, aryl, akylaryl, haloaryl, haloalkylaryl, and combinations thereof; and R is selected from the group consisting of nitrile, acetonitrile, ethylnitrile, propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine, aminoacetamide, guanidine, and urea.
    • 使用新一类式I的磷酸肌醇依赖性激酶-1(PDK-1)抑制剂用于诱导不期望的快速增殖细胞中的凋亡,用于治疗,抑制或延迟癌症的发作,以及用于预防受试者的再狭窄 已经经历了血管成形术或支架:其中X选自烷基和卤代烷基; Ar是选自苯基,联苯基,萘基,蒽基,菲基和芴基的芳基; 并且其中Ar任选被一个或多个选自卤素,C 1 -C 4烷基,C 1 -C 4卤代烷基,叠氮基,C 1 -C 4叠氮基烷基,芳基,烷基芳基,卤代芳基,卤代烷基芳基及其组合的基团取代。 并且R选自腈,乙腈,乙腈,丙腈,甲酰胺,脒,四唑,肟,腙,乙脒,氨基乙酰胺,胍和脲。
    • 90. 发明申请
    • PDK-1/AKT SIGNALING INHIBITORS
    • PDK-1 / AKT信号抑制剂
    • US20090281328A1
    • 2009-11-12
    • US12476772
    • 2009-06-02
    • Ching-Shih Chen
    • Ching-Shih Chen
    • C07D403/12C07D231/12
    • C07D231/12
    • A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I: wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, C1-C4 haloalkyl, azido, C1-C4 azidoalkyl, aryl, alkylaryl, haloaryl, haloalkylaryl, and combinations thereof; and R is selected from the group consisting of nitrile, acetonitrile, ethylnitrile, propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine, aminoacetamide, guanidine, and urea. Also provided are methods of using the compounds for the treatment and prevention of cancer in humans.
    • 新型的式I的磷酸肌醇依赖性激酶-1(PDK-1)抑制剂:其中X选自烷基和卤代烷基; Ar是选自苯基,联苯基,萘基,蒽基,菲基和芴基的芳基; 并且其中Ar任选被一个或多个选自卤素,C 1 -C 4烷基,C 1 -C 4卤代烷基,叠氮基,C 1 -C 4叠氮基烷基,芳基,烷基芳基,卤代芳基,卤代烷基芳基及其组合的基团取代。 并且R选自腈,乙腈,乙腈,丙腈,甲酰胺,脒,四唑,肟,腙,乙脒,氨基乙酰胺,胍和脲。 还提供了使用该化合物治疗和预防人类癌症的方法。