发明名称 Water-soluble polymer alkanals
摘要 The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.
申请公布号 US8853325(B2) 申请公布日期 2014.10.07
申请号 US201113301715 申请日期 2011.11.21
申请人 Nektar Therapeutics 发明人 Kozlowski Antoni
分类号 C08G63/48;C08G63/91;C08G65/26;C07C45/30;C07C47/198;C07C43/315;A61K47/48;C08G65/329;C08G10/00;C08G12/00 主分类号 C08G63/48
代理机构 McDermott Will & Emery LLP 代理人 McDermott Will & Emery LLP ;Evans Susan T.
主权项 1. A conjugate having the following structure: wherein: POLY is CH3O—CH2CH2—O—(CH2CH2O)n-1—CH2CH2— and n is 3 to about 4,000;X′ is —O—;z′ is an integer from 2 to about 21;R1, in each occurrence, is independently H or an organic radical selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, and substituted aryl;R2, in each occurrence, is independently H or an organic radical selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, and substituted aryl; and—“NH-biologically active agent” represents a biologically active agent comprising an amino group, and further where the following apply: when POLY is linear: (a) the total number of carbonyls present in the polymer is 0 or 2 or greater except when X′ comprises one or more contiguous (—CH2CH2O—) segments, and (b) when X′ is oxygen or comprises at least one (—CH2CH2O—) segment and z′ is from 2 to 12, then at least one of R1 or R2 in at least one occurrence is an organic radical as defined above, when POLY is branched, (c) either (i) at least one of R1 or R2 in at least one occurrence is an organic radical as defined above or (ii) X′ includes —(CH2CH2O)b— where b is from 1 to about 20 in the instance where POLY comprises a lysine residue, and (d) when POLY possesses two polymer arms, then neither polymer arm comprises oxygen as the only heteroatom in the instance where POLY comprises “C—H” as a branch point.
地址 San Francisco CA US