Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents

US6180095A · kind A · utility

Assignee

• Enzon, Inc. · US

Inventors

• Richard B. Greenwald · Cambridge, US
• Annapurna Pendri · South Glastonbury, US
• Yun H. Choe · Green Brook, US

Key dates

• Filing date: Oct 30, 1998
• Grant date: Jan 30, 2001
• Expiry date: Oct 30, 2018

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric prodrugs are preferably of the formula: ##STR1## wherein: L.sub.1 is a bifunctional linking moiety; G is H or ##STR2## where B is H, a leaving group, a residue of an amine-containing moiety, or a residue of a hydroxyl-containing moiety; Y.sub.1-4 are independently, O, S, or NR.sub.12 ; R.sub.1, R.sub.4, R.sub.9, R.sub.10, and R.sub.12, 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; R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.1-6 alkoxy, phenoxy, C.sub.1-8 heteroalkyls, C.sub.1-8 heteroalkoxy, substituted C.sub.1-6 alkyls, C.sub.3-8 cycloalkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, halo-, nitro-, cyano-, carboxy-, C.sub.1-6 carboxyalkyls and C.sub.1-6 alkyl carbonyls; Ar is a moiety which when included in Formul…