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    • 3. 发明授权
    • Hydrazone-based and oxime-based fluorescent and chromophoric/pro-fluorescent and pro-chromophoric reagents and linkers
    • 腙基和肟基荧光和发色/前荧光和原色发色试剂和接头
    • US08541555B2
    • 2013-09-24
    • US11787932
    • 2007-04-18
    • David A. SchwartzLeopoldo Mendoza
    • David A. SchwartzLeopoldo Mendoza
    • C07K16/00C07H21/04C07D235/02
    • G01N33/582C07D303/02
    • Conjugationally extended hydrazine compositions of the formula (RR2)N(H)n(NH2)n, fluorescent hydrazone compositions of the formula (RR2)NN═C(R1R2), methods of the formation of hydrazones from the reaction of conjugationally extended hydrazines with conjugationally extended carbonyls and methods of their use in assays systems are described. Use of these conjugationally extended hydrazine and oxime compositions for direct calorimetric and fluorometric assays wherein a chromophore or the fluorophore is incorporated into the linker that is positioned between a reactive linking moiety and a biotin molecule. More specifically the linker comprises one molecule of a high affinity binding pair such as for example biotin of the biotin/avidin high affinity binding pair, connected to a spacer molecule such as for example a length of polyethyleneglycol followed by a pro-chromophoric, chromophoric, pro-fluorescent or fluorescent moiety connected to an amino-, thiol- or carbohydrate-reactive moiety such as for example succinimidyl, maleimido or aminoxy group respectively, that may covalently link to a biomolecule.
    • 式(RR2)N(H)n(NH2)n的共轭延伸的肼组合物,式(RR2)NN = C(R1R2)的荧光腙组合物,从共轭延伸的肼与 描述了缀合扩展的羰基及其在测定系统中的用途。 使用这些共轭延伸的肼和肟组合物用于直接量热和荧光测定,其中发色团或荧光团被引入位于反应性连接部分和生物素分子之间的连接体中。 更具体地,接头包含一个高亲和力结合对分子,例如生物素/抗生物素蛋白高亲和力结合对的生物素,连接到间隔分子,例如长度的聚乙二醇,随后是发色团,发色团, 分别连接到可以共价连接到生物分子的氨基,硫醇或碳水化合物反应性部分的前荧光或荧光部分,例如琥珀酰亚胺基,马来酰亚胺基或氨氧基。
    • 5. 发明授权
    • Type 2 methionine aminopeptidase (MetAP2) inhibitors and uses thereof
    • 2型甲硫氨酸氨基肽酶(MetAP2)抑制剂及其用途
    • US06566541B2
    • 2003-05-20
    • US09813555
    • 2001-03-21
    • Jun O. LiuEric C. GriffithZhuang Su
    • Jun O. LiuEric C. GriffithZhuang Su
    • C07D30308
    • C07D495/04C07D303/02C07D303/14
    • Novel compounds that are anti-angiogenic or immunosuppressive are described. Also described are methods for determining if an animal is at risk for a disease involving abnormal angiogenesis or an immune reaction resulting in pathology comprising evaluating an aspect of MetAP2 metabolism or structure; methods for identifying agents that are anti-angiogenic or immunosuppressive comprising evaluating the effect of the agent on an aspect of MetAP2 metabolism; methods for treating a cell having an abnormality in metabolism or structure of MetAP2; and methods for treating abnormal angiogenesis or an immune reaction which results in pathology in an animal. Pharmaceutical compositions are also provided.
    • 描述了抗血管生成或免疫抑制的新型化合物。 还描述了用于确定动物是否处于涉及异常血管发生的疾病或导致病理学的免疫反应的风险的方法,包括评估MetAP2代谢或结构的一个方面; 用于鉴定抗血管生成或免疫抑制剂的试剂的方法,包括评估试剂在MetAP2代谢方面的作用; 用于治疗MetAP2的代谢异常或结构异常的细胞的方法; 以及用于治疗导致动物病理学的异常血管生成或免疫反应的方法。 还提供药物组合物。
    • 6. 发明申请
    • Type 2 methionine aminopeptidase (MetAP2) inhibitors and uses thereof
    • 2型甲硫氨酸氨基肽酶(MetAP2)抑制剂及其用途
    • US20010034455A1
    • 2001-10-25
    • US09813555
    • 2001-03-21
    • Jun O. LiuEric C. GriffithZhuang Su
    • C07D303/36
    • C07D495/04C07D303/02C07D303/14
    • Novel compounds that are anti-angiogenic or immunosuppressive are described. Also described are methods for determining if an animal is at risk for a disease involving abnormal angiogenesis or an immune reaction resulting in pathology comprising evaluating an aspect of MetAP2 metabolism or structure; methods for identifying agents that are anti-angiogenic or immunosuppressive comprising evaluating the effect of the agent on an aspect of MetAP2 metabolism; methods for treating a cell having an abnormality in metabolism or structure of MetAP2; and methods for treating abnormal angiogenesis or an immune reaction which results in pathology in an animal. Pharmaceutical compositions are also provided.
    • 描述了抗血管生成或免疫抑制的新型化合物。 还描述了用于确定动物是否处于涉及异常血管发生的疾病或导致病理学的免疫反应的风险的方法,包括评估MetAP2代谢或结构的一个方面; 用于鉴定抗血管生成或免疫抑制剂的试剂的方法,包括评估试剂在MetAP2代谢方面的作用; 用于治疗MetAP2的代谢异常或结构异常的细胞的方法; 以及用于治疗导致动物病理学的异常血管生成或免疫反应的方法。 还提供药物组合物。