Terminally-branched polymeric linkers and polymeric conjugates containing the same

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United States of America Patent

PATENT NO 6395266
SERIAL NO

09293624

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention is directed to polymeric-prodrug transport forms of the formula: ##STR1## wherein: ##STR2## E.sub.1-4 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls, substituted C.sub.1-6 heteroalkyls, C.sub.1-6 alkoxy, phenoxy, C.sub.1-6 heteroalkoxy, ##STR3## and at least one of E.sub.1-4 includes a B moiety, wherein B is a leaving group, OH, a residue of a hydroxyl-or amino-containing moiety or ##STR4## wherein J.sub.1 is the same as J, or another member of the group defining J and E.sub.5 is the same as E.sub.1-4, or another member of the group defining E.sub.1-4 ; Y.sub.1-2 are independently O, S or NR.sub.9 ; 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(=Y.sub.2); R.sub.2-5 and R.sub.7-9 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-16 heteroalkyls, substituted C.sub.1-6 heteroalkyls, C.sub.1-6 alkoxy, phenoxy and C.sub.1-6 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 R.sub.1 is a polymeric residue. which is optionally capped with a moiety of the formula: ##STR5##

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Patent Owner(s)

  • ENZON, INC.

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Choe, Yun H Piscataway, NJ 14 818
Greenwald, Richard B Somerset, NJ 79 5036
Martinez, Anthony J Hamilton Square, NJ 21 1495
Pendri, Annapurna Middletown, CT 54 2240

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