公开(公告)号：WO2011063156A2

公开(公告)日：2011-05-26

申请号：PCT/US2010057289

申请日：2010-11-18

Applicant: NEKTAR THERAPEUTICS ,  CHONG ANTHONY O ,  LEE SEOJU ,  JOSHI BHALCHANDRA V ,  BRAY BRIAN ,  NIE SHAOYONG ,  SPENCE PATRICK ,  KOZLOWSKI ANTONI ,  MCMANUS SAMUEL ,  TIPNIS SACHIN ,  LAVATY GREG ,  SWALLOW DAVID

Inventor： CHONG ANTHONY O ,  LEE SEOJU ,  JOSHI BHALCHANDRA V ,  BRAY BRIAN ,  NIE SHAOYONG ,  SPENCE PATRICK ,  KOZLOWSKI ANTONI ,  MCMANUS SAMUEL ,  TIPNIS SACHIN ,  LAVATY GREG ,  SWALLOW DAVID

IPC: A61K47/48 ,  A61P35/00

CPC classification number: C08G65/331 ,  A61K31/4745 ,  A61K47/60 ,  C07C51/412 ,  C07C53/18 ,  C07D491/22 ,  C08G65/329 ,  C08G65/33396 ,  C08G65/48 ,  C08L2203/02

Abstract: 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-sail 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.

Abstract translation: 在其他方面中，本文提供了水溶性聚合物 - 药物缀合物的混合酸盐以及制备和使用它们的相关方法。 混合帆酸盐是稳定形成的，并且似乎比聚合物 - 药物缀合物的相应主要纯酸盐或游离碱形式更耐水解降解。 混合酸盐可重现地制备和回收，并且与非混合酸盐形式的水溶性聚合物药物缀合物相比，提供了令人惊讶的优点。

公开(公告)号：WO2011063158A1

公开(公告)日：2011-05-26

申请号：PCT/US2010/057292

申请日：2010-11-18

Applicant: NEKTAR THERAPEUTICS ,  CHONG, Anthony, O. ,  LEE, Seoju ,  JOSHI, Bhalchandra, V. ,  BRAY, Brian ,  NIE, Shaoyong ,  SPENCE, Patrick ,  KOZLOWSKI, Antoni ,  MCMANUS, Samuel ,  TIPNIS, Sachin ,  LAVATY, Greg ,  SWALLOW, David

Inventor： CHONG, Anthony, O. ,  LEE, Seoju ,  JOSHI, Bhalchandra, V. ,  BRAY, Brian ,  NIE, Shaoyong ,  SPENCE, Patrick ,  KOZLOWSKI, Antoni ,  MCMANUS, Samuel ,  TIPNIS, Sachin ,  LAVATY, Greg ,  SWALLOW, David

IPC: A61K47/48 ,  A61P35/00

CPC classification number: C08G65/331 ,  A61K31/4745 ,  A61K47/60 ,  C07C51/412 ,  C07C53/18 ,  C07D491/22 ,  C08G65/329 ,  C08G65/33396 ,  C08G65/48 ,  C08L2203/02

Abstract: 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.

Abstract translation: 在其它方面，本文提供了多臂水溶性聚乙二醇 - 药物偶联物的氢卤酸盐，以及制备和使用它们的相关方法。 氢卤酸盐稳定地形成，似乎比结合物的相应游离碱形式更耐水解降解。

公开(公告)号：WO2011063156A3

公开(公告)日：2011-05-26

申请号：PCT/US2010/057289

申请日：2010-11-18

Applicant: NEKTAR THERAPEUTICS ,  CHONG, Anthony, O. ,  LEE, Seoju ,  JOSHI, Bhalchandra, V. ,  BRAY, Brian ,  NIE, Shaoyong ,  SPENCE, Patrick ,  KOZLOWSKI, Antoni ,  MCMANUS, Samuel ,  TIPNIS, Sachin ,  LAVATY, Greg ,  SWALLOW, David

Inventor： CHONG, Anthony, O. ,  LEE, Seoju ,  JOSHI, Bhalchandra, V. ,  BRAY, Brian ,  NIE, Shaoyong ,  SPENCE, Patrick ,  KOZLOWSKI, Antoni ,  MCMANUS, Samuel ,  TIPNIS, Sachin ,  LAVATY, Greg ,  SWALLOW, David

IPC: A61K47/48 ,  A61P35/00 ,  C08G65/08 ,  C08G65/14 ,  C08G65/26

Abstract: 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-sail 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.