Pegylation reagents and compounds formed therewith

Biologically active conjugates are disclosed which are formed by reaction of a thiol moiety of a biologically active molecule with a non-peptidic polymer having an active sulfone moiety. Also disclosed are compounds having the formula R1-X-R2 wherein at least one of R1 and R2 is a biologically activ...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: THOMPSON ROBERT C, KOHNO TADAHIKO, BREWER MICHAEL T
Format: Patent
Sprache:eng
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Beschreibung
Zusammenfassung:Biologically active conjugates are disclosed which are formed by reaction of a thiol moiety of a biologically active molecule with a non-peptidic polymer having an active sulfone moiety. Also disclosed are compounds having the formula R1-X-R2 wherein at least one of R1 and R2 is a biologically active molecule having a reactive thiol moiety which forms a covalent bond with X, a Michael acceptor-activated non-peptidic polymer. Further disclosed are methods of making the conjugates and compounds of the present invention as well as pharmaceutical compositions containing them. In addition, activated polymers suitable for attachment to a variety of molecules and surfaces are disclosed.