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    • 47. 发明授权
    • Affinity markers for human serum albumin
    • 人血清白蛋白的亲和标记
    • US07166695B2
    • 2007-01-23
    • US10934841
    • 2004-09-02
    • Alexander KrantzWolin HuangArthur M. HanelDarren L. HolmesDominique P. Bridon
    • Alexander KrantzWolin HuangArthur M. HanelDarren L. HolmesDominique P. Bridon
    • C07K7/06
    • A61K49/0021A61K38/00A61K47/62A61K47/6901A61K49/0043A61K49/0056C07K14/665
    • Methods and compositions are provided for identifying compounds having affinity or complementarity to a target molecule. Compounds according to the invention may be described by the formula E-Ca—R—Cb-A, wherein E is a therapeutic or diagnostic agent, R is a reactive group, Ca and Cb are connector groups between E and R and between R and A, respectively, and A is an affinity group comprising the sequence F-1-Y-E-E. Compounds according to the invention may be used for labeling the target molecule, particularly where the target molecule is naturally found in a complex mixture, such as a physiological fluid, like blood. By affinity labeling in vivo, the lifetime of physiologically active entities can be greatly enhanced by becoming bound to long-lived blood components. The covalently bound entity may also serve as an antagonist or agonist of a particular binding protein or as an enzyme inhibitor.
    • 提供了用于鉴定与靶分子具有亲和力或互补性的化合物的方法和组合物。 根据本发明的化合物可以用下式描述:其中E是治疗剂或诊断剂,R是反应性基团,C < 分别是E和R之间以及R和A之间的连接器组,A是包含序列F-1 -YEE的亲和基团。 根据本发明的化合物可以用于标记靶分子,特别是当目标分子天然存在于复杂混合物如生理液体如血液中时。 通过体内亲和标记,生理活性实体的寿命可以通过与长寿命的血液成分结合而大大增强。 共价结合的实体也可以用作特异性结合蛋白的拮抗剂或激动剂或作为酶抑制剂。
    • 50. 发明授权
    • Method for alleviating pain or providing an analgesic effect in a patient
    • 减轻疼痛或在患者中提供镇痛作用的方法
    • US06610825B2
    • 2003-08-26
    • US09798119
    • 2001-03-01
    • Alan M. EzrinDominique P. BridonDarren L. HolmesPeter G. Milner
    • Alan M. EzrinDominique P. BridonDarren L. HolmesPeter G. Milner
    • C07K700
    • C07K14/70A61K38/00A61K47/64C07K14/665C07K2319/00
    • Conjugates are prepared from antinociceptive agents, particularly opioids or opioid analogs, more particularly dynorphins, endorphins, deltorphins, enkephalins or analogs thereof, by combining said antinociceptive agent with a material providing a functionally reactive group capable of reacting with a blood component (preferably a blood cell or protein). Said conjugates permit extension of the therapeutic life of the antinociceptive agent. They may be administered to patients to alleviate pain, produce analgesic effects, or assist in cases of narcotics withdrawal, and may also be used as probes for receptor activity. The administration to the patient may be made either in vivo or ex vivo and may be performed by either introducing the derivative including the reactive functional group into the patient's vascular system or preparing such a conjugate externally (or in vitro) and introducing that conjugate to the patient's vascular system.
    • 通过将所述抗伤害感受剂与提供能够与血液成分(优选血液)反应的功能反应性基团的材料组合,由抗伤害感受剂,特别是阿片样物质或阿片样物质类似物,更具体地说是强啡肽,内啡肽,delphphins,脑啡肽或其类似物制备缀合物 细胞或蛋白质)。 所述缀合物允许延长抗伤害感受剂的治疗寿命。 可以向患者施用以缓解疼痛,产生镇痛作用或辅助麻醉药物撤出的情况,也可用作受体活性的探针。 对患者的施用可以在体内或体外制备,并且可以通过将包含反应性官能团的衍生物引入患者的血管系统或者在外部(或体外)中制备这种缀合物并将该缀合物引入到 患者血管系统。