Nektar Therapeutics

Nektar Therapeutics Al, Corporation

Shearwater Corporation

Other

Naktar Therapeutics

Xiaoming Shen

Michael David Bentley

Antoni Kozlowski

Samuel P McManus

Xuan Zhao

J Milton Harris

Sean M Culbertson

Jennifer A Riggs-Sauthier

Lihong Guo

William Dudley Battle, Iii

Wen Zhang

Zhihao Fang

Brian Bray

Tracy L Hutchison

Lin Cheng

Michael James Roberts

Tony L Sander

YongQi Mu

Neel Kumar Anand

Bo-Liang Deng

Timothy A Riley

Zhongxu Ren

Pankaj Sharma

Natalia Aurrecoechea

Donogh John Roger O'Mahony

Xuyuan Gu

Yuan Song

Xuejun Yuan

Mark A Wilson

Vijay Kumar Khatri

Michael Lixin Shen

Aleksandrs Odinecs

Daniel C Cook

Xuan Zhoa

Samuel P Mcmanus

William Dudley Battle

Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies.

Multi-arm polymeric alkanoate conjugates

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-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 instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.

Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine

The invention is directed to multi-functional N-maleimidyl polymer derivatives comprising a water soluble and non-peptidic polymer backbone having a terminal carbon, such as a poly(alkylene glycol), the terminal carbon of the polymer backbone being directly bonded to the nitrogen atom of a N-maleimidyl moiety without a linking group therebetween. The invention also provides two methods of preparing such linkerless N-maleimidyl polymer derivatives.

N-maleimidyl polymer derivatives

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Madison, AL, United States of America

Xiaoming Shen