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Title:
TERMINALLY-BRANCHED POLYMERIC LINKERS AND POLYMERIC CONJUGATES CONTAINING THE SAME
Document Type and Number:
WIPO Patent Application WO1999053951
Kind Code:
A9
Abstract:
The present invention is directed to polymeric-prodrug transport forms of formula (I), wherein: J is (1), (2) or (3), 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, (2) or (3) 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 or formula (II) wherein 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, C1-6 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; and R1 is a polymeric residue, which is optionally capped with a moiety of formula (V).

Inventors:
MARTINEZ ANTHONY J
PENDRI ANNAPURNA
GREENWALD RICHARD B
CHOE YUN H
Application Number:
US9908373W
Publication Date:
October 05, 2000
Filing Date:
April 16, 1999
Export Citation:
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Assignee:
ENZON, INC.
International Classes:
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): A61K39/385; A01N37/00; A01N43/02; A01N31/14; C08F283/00
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