Phosphonomethoxy carbocyclic nucleosides and nucleotides
    1.
    发明授权
    Phosphonomethoxy carbocyclic nucleosides and nucleotides 失效
    膦基甲氧基碳环核苷酸和核苷酸

    公开(公告)号:US5744600A

    公开(公告)日:1998-04-28

    申请号:US357561

    申请日:1994-12-16

    CPC分类号: C07F9/65121

    摘要: A compound of the Formula I or Formula II ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, hydroxy, chlorine, fluorine, bromine, or an organic substituent having 1 to 5 carbon atoms and selected from acyloxy having a hydrocarbon stem of 1 to 4 carbon atoms, alkoxy, alkylthio, amino, alkylamino and dialkylamino; R.sup.3 and R.sup.4 are independently hydrogen, or organic phosphonic ester substituents having 1 to 12 carbon atoms and selected from alkyl, alkenyl, aryl, and aralkyl; and B is a heterocyclic group selected from the group consisting of pyrimidine, purine, triazine, deazapurine, and triazole, attached through a ring nitrogen atom thereof optionally substituted with 1 to 3 substituents selected from the group consisting of hydroxy, mercapto, amino, hydrazino, fluoro, chloro, bromo, iodo, C.sub.1 to C.sub.3 alkyl, C2-C3 alkenyl, C2-C3 haloalkenyl, C1-C3 alkoxy, and C1-C3 alkylthio; and the pharmaceutically acceptable acid addition, metal, and amine salts thereof. The compositions of the invention are useful for, among other things, antiviral agents.

    摘要翻译: 式I或式II的化合物其中R 1和R 2独立地是氢,羟基,氯,氟,溴或具有1至5个碳原子并且选自具有烃的酰氧基的有机取代基 1至4个碳原子的烷氧基,烷硫基,氨基,烷基氨基和二烷基氨基; R3和R4独立地是氢,或具有1至12个碳原子并且选自烷基,烯基,芳基和芳烷基的有机膦酸酯取代基; 并且B是选自嘧啶,嘌呤,三嗪,脱氮嘌呤和三唑的杂环基,其通过环氮原子连接,任选被1-3个选自羟基,巯基,氨基,肼基的取代基取代 ,氟,氯,溴,碘,C 1至C 3烷基,C 2 -C 3烯基,C 2 -C 3卤代烯基,C 1 -C 3烷氧基和C 1 -C 3烷硫基; 及其药学上可接受的酸加成盐,金属盐和胺盐。 本发明的组合物尤其可用于抗病毒剂。

    Inhibitors of cyclin dependent kinases
    5.
    发明授权
    Inhibitors of cyclin dependent kinases 失效
    细胞周期蛋白依赖性激酶抑制剂

    公开(公告)号:US5733920A

    公开(公告)日:1998-03-31

    申请号:US551031

    申请日:1995-10-31

    摘要: The invention provides novel inhibitors of cyclin-dependent kinases, in particular inhibitors of the CDK/cyclin complexes such as CDK4/cyclin D1. The novel compounds are analogs of chromones. These compounds can be used for inhibiting excessive or abnormal cell proliferation. Thus, the novel compounds are useful for treating a subject with a disorder associated with excessive cell proliferation, such as cancer.

    摘要翻译: 本发明提供细胞周期蛋白依赖性激酶的新型抑制剂,特别是CDK /细胞周期蛋白复合物例如CDK4 /细胞周期蛋白D1的抑制剂。 新化合物是色酮的类似物。 这些化合物可用于抑制细胞增殖过多或异常。 因此,新化合物可用于治疗与过度细胞增殖相关的疾病如癌症的受试者。