Bicyclic aminoimidazoles
    2.
    发明授权
    Bicyclic aminoimidazoles 失效
    双环氨基咪唑

    公开(公告)号:US06218549B1

    公开(公告)日:2001-04-17

    申请号:US09441721

    申请日:1999-11-16

    IPC分类号: C07D40500

    摘要: The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a tetrahydropurine compound. The subject invention also provides for processes for preparing the compounds.

    摘要翻译: 本发明提供双环氨基咪唑化合物,羟烷基氨基咪唑化合物,双环吡咯化合物,hymenin化合物,醛氨基咪唑化合物,缩酮氨基咪唑化合物,三环化合物和四氢嘌呤化合物。 本发明还提供了制备化合物的方法。

    Syntheses and methods of use of new antimitotic agents
    3.
    发明授权
    Syntheses and methods of use of new antimitotic agents 失效
    新型抗有丝分裂剂的合成和使用方法

    公开(公告)号:US06673937B2

    公开(公告)日:2004-01-06

    申请号:US09910195

    申请日:2001-07-19

    IPC分类号: C07D40500

    摘要: Oxidative cyclization of bis-naphthyl ethers allows concise total syntheses of palmarumycin CP1 and deoxypreussomerin A in 8-9 steps and 15-35% overall yield from 5-hydroxy-8-methoxy-1-tetralone. A small library of palmarumycin analogs was created. Biological evaluation of these naphthoquinone spiroketals against MCF-7 and MDA-MB-231 human breast cancer cells revealed several low-micromolar growth inhibitors. A number of the analogs inhibit the thioredoxin—thioredoxin reductase system.

    摘要翻译: 双萘基醚的氧化环化允许8-9步骤中棕榈霉素CP1和脱氧阿司咪霉素A的简明综合,5-羟基-8-甲氧基-1-四氢萘酮的总产率为15-35%。 创建了一个古老的棕榈霉素类似物库。 这些萘醌螺旋酮对MCF-7和MDA-MB-231人乳腺癌细胞的生物学评价显示出几种低微摩尔生长抑制剂。 许多类似物抑制硫氧还蛋白硫氧还蛋白还原酶系统。

    Synthesis and clinical uses of D,&agr;-tocopherol nicotinate compounds
    4.
    发明授权
    Synthesis and clinical uses of D,&agr;-tocopherol nicotinate compounds 失效
    D,α-生育酚烟酸酯化合物的合成和临床应用

    公开(公告)号:US06423847B1

    公开(公告)日:2002-07-23

    申请号:US09532658

    申请日:2000-03-20

    IPC分类号: C07D40500

    CPC分类号: C07D405/12

    摘要: A process of synthesis of D,&agr;-tocopherol nicotinate compounds is presented. Therapeutic uses for this compound are described. The active agents are demonstrated to be complementary in their physiological functions especially as these relate to cellular and endothelial biochemistry and physiology and, ultimately to vascular health. The active components of the invention are selected for inclusion in a unique combination that clinically reduces risks of vasculopathy, DNA strand breakage and neuronal excitotoxicity in various diseases. In addition to the systemic vascular benefits acquired, improvement of the vascular health of the eye reduces the risk of glaucomatous optic nerve atrophy with its accompanying visual field loss and potential blindness and reduces conditions of risk for macular degeneration.

    摘要翻译: 提出了合成D,α-生育酚烟酸酯化合物的方法。 描述了该化合物的治疗用途。 证明活性剂在其生理功能上是互补的,特别是因为这些涉及细胞和内皮生物化学和生理学,最终涉及血管健康。 选择本发明的活性组分以包含在临床上降低各种疾病中血管病变,DNA链断裂和神经元兴奋性毒性的风险的独特组合中。 除了所获得的全身血管益处之外,眼睛血管健康状况的改善降低了青光眼性视神经萎缩的风险及伴随的视野丧失和潜在的失明,并减少了黄斑变性的风险。