发明名称 Omega-functionalized polymers, junction-functionalized block copolymers, polymer bioconjugates, and radical chain extension polymerization
摘要 Polymeric compounds having spatially controlled bioconjugation sites are described. Functionalization is achieved by selective ω-terminal chain extension of polymer chains by radical polymerization, such as reversible addition-fragmentation chain transfer (RAFT) polymerization.
申请公布号 US9593169(B2) 申请公布日期 2017.03.14
申请号 US200913133355 申请日期 2009.12.08
申请人 University of Washington;PhaseRx, Inc. 发明人 Stayton Patrick S.;Hoffman Allan S.;Convertine Anthony J.;Henry Scott M.;Overell Robert W.;Johnson Paul H.
分类号 C07D345/00;C07D517/00;C08F2/38;A61K47/48;C08F220/54;C08F293/00;C12N15/11 主分类号 C07D345/00
代理机构 Christensen O'Connor Johnson Kindness PLLC 代理人 Christensen O'Connor Johnson Kindness PLLC ;Renzoni George;Zheng Juan
主权项 1. A compound of formula IA:wherein Pn is a polymer chain, E is a chain extension residue corresponding to formula E3 j, k and l are each independently selected integers, where j ranges from 0 to 9, k is >1, l ranges from 0 to 9, and the sum (j+k+l) is <10, L is a linking moiety, Q is a biomolecular agent covalently bonded through L to R5 of chain extension residue E, the biomolecular agent being a therapeutic agent, a targeting agent, a diagnostic agent, or an analytical agent, R1 and R4 are each hydrogen, R2, N—R5, and R3 together form an N-substituted imidyl moiety represented by the formula —C(O)NR5C(O)—, R5 is a C1-C20 moiety comprising a functional group or comprising a functional group covalently coupled to the biomolecular agent, Q, through a linking moiety, L, wherein the C1-C20 moiety is selected from the group consisting of hydrocarbyl, substituted hydrocarbyl, hetero-hydrocarbyl, substituted hetero-hydrocarbyl, carbocyclic, substituted carbocyclic, heterocyclic, substituted heterocyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and fused-multiring structures comprising one or more of the foregoing, and wherein the functional group is selected from the group consisting of amino, ammonio, imino, amido, imidyl, nitrile, azo, azido, cyano, cyanato, isocyanato, isothiocyanto, hydrazide, nitro, nitroso, nitrosooxy, pyridyl, hydroxyl, alkoxy, carboxyl, ester, acyl, halo, haloformyl, phosphino, phosphoric, phospho, sulfide, di-sulfide, thio, thiol, sulfonyl, sulfo, sulfinyl, alkenyl, alkynl, allenyl, and silyl, and Y is a thiocarbonylthio moiety having a formula —SC(═S)Z, where Z is an activating group.
地址 Seattle WA US