发明名称 OLIGOMER-CALCIUM CHANNEL BLOCKER CONJUGATES
摘要 The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
申请公布号 US2014323529(A1) 申请公布日期 2014.10.30
申请号 US201414266317 申请日期 2014.04.30
申请人 NEKTAR THERAPEUTICS 发明人 Ren Zhongxu;Deng Bo-Liang;Riggs-Sauthier Jennifer;Harvey Micah
分类号 A61K47/48;A61K31/4418 主分类号 A61K47/48
代理机构 代理人
主权项 1. A compound comprising a calcium channel blocker residue covalently attached via a stable or degradable linkage to a water-soluble, non-peptidic oligomer, wherein the calcium channel blocker residue is a residue of a calcium channel blocker having the formulawherein: R is hydrogen or lower alkyl; R1 and R2 are each independently selected from the group consisting of hydrogen, substituted lower alkyl, unsubstituted lower alkyl, and —YOYNR6R7, where each Y is independently lower alkylene and R6 and R7 are each independently selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, cycloalkyl, aryl and alkylaryl; R3 and R4 are each independently selected from the group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, and —YNR6R7, where Y is lower alkylene and R6 and R7 are each independently selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, cycloalkyl, aryl and alkylaryl; and each R5 is independently selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, chloro, fluoro and nitro,wherein the water-soluble, non-peptidic oligomer is made of 2 to 30 monomers,or pharmaceutically acceptable salts thereof.
地址 San Francisco CA US
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