Nektar Therapeutics

Trimeris, Inc.

Brian Bray

Antoni Kozlowski

Samuel P McManus

Xiaoming Shen

Tracy L Hutchison

John R Handley

Anthony G Schaefer

Tony L Sander

Seoju Lee

Bhalchandra V Joshi

Myung-Chol Kang

Gene Merutka

Patrick Spence

Ryan Odom

Patrick L Spence

Shaoyong Nie

Anthony O Chong

Greg Lavaty

David Swallow

Sachin Tipnis

Catherine Mader

Maynard Lichty

Samuel Mcmanus

Among other aspects, provided herein is a mixed-acid salt of a water-soluble polymer-drug conjugate, along with related methods of making and using the same. The mixed-salt acid salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding predominantly pure acid salt or free base forms of the polymer-drug conjugate. The mixed acid salt is reproducibly prepared and recovered, and provides surprising advantages over non-mixed acid salt forms of the water-soluble polymer drug conjugate.

Acid salt forms of polymer-drug conjugates and alkoxylation methods

Among other aspects, provided herein is a hydrohalide salt of a multi-arm water-soluble polyethylene glycol-drug conjugate, along with related methods of making and using the same. The hydrohalide salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding free base form of the conjugate.

Salt form of a multi-arm polymer-drug conjugate

Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.

Intermediates useful in the preparation of maleimide functionalized polymers

Methods for preparing polymeric reagents bearing a maleimide are provided. Also provided are related compositions.

Method for preparing polymer maleimides

Methods for preparing conjugates using polymeric reagents bearing a maleimide are provided. Also provided are compositions comprising the conjugates.

Method for preparing conjugates using polymer maleimides

Methods for preparing polymeric reagents bearing a maleimide are provided. Also provided are compositions comprising the polymeric reagents, and conjugates prepared by polymeric reagents obtained by the described methods.

Method of preparing maleimide functionalized polymers

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Huntsville, AL, United States of America

Brian Bray