公开(公告)号：US20180282476A1

公开(公告)日：2018-10-04

申请号：US16000561

申请日：2018-06-05

申请人： Nektar Therapeutics

发明人： J. Milton Harris ,  Antoni Kozlowski ,  Lihong Guo

IPC分类号： C08G63/91 ,  C08F261/04 ,  C08F265/00 ,  C08F271/00 ,  C08G65/334 ,  C08F289/00 ,  C08F291/00 ,  C08F251/00 ,  C08G65/332 ,  C08F283/06 ,  A61K31/765 ,  C08G65/30

摘要： Methods for preparing water soluble, non-peptidic polymers carrying carboxyl functional groups, particularly carboxylic acid functionalized poly(ethylene glycol) (PEG) polymers are disclosed, as are the products of these methods. In general, an ester reagent R(C═O)OR′, wherein R′ is a tertiary group and R comprises a functional group X, is reacted with a water soluble, non-peptidic polymer POLY-Y, where Y is a functional group which reacts with X to form a covalent bond, to form a tertiary ester of the polymer, which is then treated with a strong base in aqueous solution, to form a carboxylate salt of the polymer. Typically, this carboxylate salt is then treated with an inorganic acid in aqueous solution, to convert the carboxylate salt to a carboxylic acid, thereby forming a carboxylic acid functionalized polymer.

公开(公告)号：US10011682B2

公开(公告)日：2018-07-03

申请号：US13922020

申请日：2013-06-19

申请人： Nektar Therapeutics

发明人： J. Milton Harris ,  Antoni Kozlowski ,  Lihong Guo

IPC分类号： C08G63/91 ,  C08G65/332 ,  C08G65/334 ,  A61K31/765 ,  C08F251/00 ,  C08F261/04 ,  C08F265/00 ,  C08F271/00 ,  C08F283/06 ,  C08F289/00 ,  C08F291/00 ,  C08G65/30

CPC分类号： C08G63/91 ,  A61K31/765 ,  C08F251/00 ,  C08F261/04 ,  C08F265/00 ,  C08F271/00 ,  C08F283/06 ,  C08F289/00 ,  C08F291/00 ,  C08G65/30 ,  C08G65/332 ,  C08G65/3322 ,  C08G65/3346

摘要： Methods for preparing water soluble, non-peptidic polymers carrying carboxyl functional groups, particularly carboxylic acid functionalized poly(ethylene glycol) (PEG) polymers are disclosed, as are the products of these methods. In general, an ester reagent R(C═O)OR′, wherein R′ is a tertiary group and R comprises a functional group X, is reacted with a water soluble, non-peptidic polymer POLY-Y, where Y is a functional group which reacts with X to form a covalent bond, to form a tertiary ester of the polymer, which is then treated with a strong base in aqueous solution, to form a carboxylate salt of the polymer. Typically, this carboxylate salt is then treated with an inorganic acid in aqueous solution, to convert the carboxylate salt to a carboxylic acid, thereby forming a carboxylic acid functionalized polymer.

公开(公告)号：US11111335B2

公开(公告)日：2021-09-07

申请号：US16000561

申请日：2018-06-05

申请人： Nektar Therapeutics

发明人： J. Milton Harris ,  Antoni Kozlowski ,  Lihong Guo

IPC分类号： C08G65/332 ,  C08G63/91 ,  C08G65/334 ,  A61K31/765 ,  C08F251/00 ,  C08F261/04 ,  C08F265/00 ,  C08F271/00 ,  C08F283/06 ,  C08F289/00 ,  C08F291/00 ,  C08G65/30

摘要： Methods for preparing water soluble, non-peptidic polymers carrying carboxyl functional groups, particularly carboxylic acid functionalized poly(ethylene glycol) (PEG) polymers are disclosed, as are the products of these methods. In general, an ester reagent R(C═O)OR′, wherein R′ is a tertiary group and R comprises a functional group X, is reacted with a water soluble, non-peptidic polymer POLY-Y, where Y is a functional group which reacts with X to form a covalent bond, to form a tertiary ester of the polymer, which is then treated with a strong base in aqueous solution, to form a carboxylate salt of the polymer. Typically, this carboxylate salt is then treated with an inorganic acid in aqueous solution, to convert the carboxylate salt to a carboxylic acid, thereby forming a carboxylic acid functionalized polymer.