Terminally-branched polymeric linkers and polymeric conjugates containing the same

US6153655A · kind A · utility

Assignee

• Enzon, Inc. · US

Inventors

• Anthony J. Martinez · Hamilton Square, US
• Annapurna Pendri · South Glastonbury, US
• Richard B. Greenwald · Cambridge, US
• Yun H. Choe · Green Brook, US

Key dates

• Filing date: Apr 17, 1998
• Grant date: Nov 28, 2000
• Expiry date: Apr 17, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C08F283/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention is directed to polymeric- prodrug transport forms of the formula: ##STR1## wherein: B is a leaving group, OH, a residue of a hydroxyl-containing moiety or ##STR2## wherein B.sub.1 is a leaving group, OH or a residue of a hydroxyl-containing moiety; PA1 Y.sub.1-2 are independently O or S; PA1 M is 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(.dbd.Y.sub.2); R.sub.2-5 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 and substituted C.sub.1-6 heteroalkyls; PA1 (m) is zero or one; PA1 (n) is a positive integer; PA1 (p) is zero or a positive integer; PA1 Z is an electron withdrawing group; and PA1 R.sub.1 is a polymeric residue which is optionally capped with a moiety of the Formula (v) ##STR3##