发明名称 Terminally-branched polymeric linkers and polymeric conjugates containing the same
摘要 The present invention is directed to polymeric-prodrug transport forms of the formula:wherein:E1-4 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy, C1-6 heteroalkoxy,and at least one of E1-4 includes a B moiety, wherein B is a leaving group, OH, a residue of a hydroxyl-or amino-containing moiety orwherein J1 is the same as J, or another member of the group defining J and E5 is the same as E1-4, or another member of the group defining E1-4;Y1-2 are independently O, S or NR9;M is a heteroatom selected from either X or Q; wherein X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(=Y2);R2-5 and R7-9 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-16 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy;(m1) and (m2) are independently zero or one;(n1), (n2), (p1), (p2) and (q) are independently zero or a positive integer,Z is an electron withdrawing group; andR1 is a polymeric residue.which is optionally capped with a moiety of the formula:
申请公布号 US6395266(B1) 申请公布日期 2002.05.28
申请号 US19990293624 申请日期 1999.04.16
申请人 ENZON, INC. 发明人 MARTINEZ ANTHONY J.;PENDRI ANNAPURNA;GREENWALD RICHARD B.;CHOE YUN H.
分类号 A61K47/34;A61K47/48;A61P1/00;A61P9/08;A61P15/08;A61P15/18;A61P25/04;A61P25/22;A61P25/28;A61P29/00;C07D491/22;C07H15/252;C08F283/00;C08G65/329;C08G85/00;(IPC1-7):A61K31/785;A61K47/30;A61K31/44;A61K31/21 主分类号 A61K47/34
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