Nektar Therapeutics

Baxalta Gmbh

Baxter International Inc.

Baxter Healthcare Sa

Sean M Culbertson

Samuel P McManus

Antoni Kozlowski

Michael David Bentley

Xiaoming Shen

Jennifer A Riggs-Sauthier

Stephanie Allums-Donald

Tony Drew Vinson

Mary J Bossard

Timothy A Riley

Dennis G Fry

Mark A Wilson

Peter Turecek

Zhihao Fang

Ping Zhang

Hanspeter Rottensteiner

Alfred Weber

Katalin Varadi

Harold Zappe

Heinz Anderle

Dawei Sheng

Xuejun Yuan

Patrick D Youso

Vidula R Dixit

Gerald Schrenk

Venkata Ravidnranadh Somu

Samuel P Mcmanus

Samuel Mcmanus

Vidula Dixit

The instant disclosure provides (among other things) improved methods of preparing fluorenyl-based polymeric reagents, methods of recovering and purifying such polymeric reagents, methods of reducing unwanted impurities in a fluorenyl-based polymeric reagent, fluorenyl-based polymeric reagents prepared by the methods described herein, and conjugates prepared by reaction with fluorenyl-based polymeric reagents prepared by the methods described herein.

Method of making releasable polymeric reagents

Provided herein are polymeric &#x3b1;-hydroxy aldehyde or &#x3b1;-hydroxy ketone reagents which can be conjugated to amine-containing compounds to form stable conjugates in a single-step reaction. In selected embodiments, the polymeric reagent itself incorporates an internal proton-abstracting (basic) functional group, to promote more efficient reaction. The substituent is appropriately situated, via a linker if necessary, to position the group for proton abstraction, preferably providing a 4- or 5-bond spacing between the abstracting atom and the hydrogen atom on the &#x3b1;-carbon. Also provided are methods of using the reagents and stable, solubilized conjugates of the reagents with biologically active compounds. In preferred embodiments, the polymeric component of the reagent or conjugate is a polyethylene glycol.

Polymeric alpha-hydroxy aldehyde and ketone reagents and conjugation method

The invention relates to (among other things) polymer-sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over sunitinib in unconjugated form.

Polymer-sunitinib conjugates

The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form.

Polymer-des-ethyl sunitinib conjugates

The present invention provides conjugates having a degradable linkage and polymeric reagents useful in preparing such conjugates. The conjugates as well as the polymeric reagents used to form the conjugates include at least one of each the following: an aromatic moiety comprising an ionizable hydrogen atom, a spacer moiety, and a water-soluble polymer. Methods of making polymeric reagents and conjugates, as well as methods for administering conjugates and compositions, are also provided.

Conjugates having a degradable linkage and polymeric reagents useful in preparing such conjugates

The invention relates to (among other things) polymer-semaxanib moiety conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over the semaxanib moiety in unconjugated form.

Polymer-semaxanib moiety conjugates

Composition comprising a polymeric reagent

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Gurley, AL, United States of America

Sean M Culbertson