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    • 32. 发明授权
    • Controlled release of thioamide moiety-containing therapeutic agents
    • 含硫酰胺部分的治疗剂的控制释放
    • US06468522B1
    • 2002-10-22
    • US09621109
    • 2000-07-21
    • Stanley SteinGuobao ZhangBo Qiu
    • Stanley SteinGuobao ZhangBo Qiu
    • A61K3174
    • A61K47/60Y10S424/16
    • This invention pertains to disulfide-linked conjugates of therapeutic agents containing at least one thioamide group with polymer comprising at least one thiol group, so as to provide a controlled release pharmaceutical composition for administration to animals for the prophylaxis or treatment of various conditions or diseases. The therapeutic agent conjugate may comprise an inactive or weakly active prodrug form which may be converted into the original therapeutic compound by the natural action of reducing agents in vivo. The composition may comprise a mixture of polymers each with a different thioamide-containing agent attached, or a polymer conjugated with a mixture of thioamide-containing agents. Modified properties of the therapeutic compound potentially provided by the polymer itself, as well as by other compounds also appended to the polymer, include but are not limited to greater water solubility, longer in-vivo half-life (due to larger size of the conjugate), slower release from a sustained-release depot (due to larger size of the conjugate), better oral bioavailability and tissue-specific targeting.
    • 本发明涉及含有至少一种硫代酰胺基团的治疗剂与包含至少一种硫醇基团的聚合物的二硫键连接的缀合物,以提供用于预防或治疗各种病症或疾病的用于给予动物的控释药物组合物。 治疗剂缀合物可以包含无活性或弱活性的前药形式,其可以通过体内还原剂的天然作用转化为原始治疗化合物。 组合物可以包含各自与不同含硫代酰胺的试剂连接的聚合物的混合物,或与含硫代酰胺的试剂的混合物缀合的聚合物。 由聚合物本身以及也附加到聚合物上的其它化合物可以提供的治疗化合物的改性特征包括但不限于更大的水溶性,更长的体内半衰期(由于缀合物的较大尺寸 ),缓释片段的释放缓慢(由于缀合物的尺寸较大),更好的口服生物利用度和组织特异性靶向。