发明名称 Controlled release of thioamide moiety-containing therapeutic agents
摘要 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.
申请公布号 US6468522(B1) 申请公布日期 2002.10.22
申请号 US20000621109 申请日期 2000.07.21
申请人 UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY;RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY 发明人 STEIN STANLEY;ZHANG GUOBAO;QIU BO
分类号 A61K47/48;(IPC1-7):A61K31/74;A61K39/44;A61K9/14 主分类号 A61K47/48
代理机构 代理人
主权项
地址