发明名称 NOVEL POLYMERS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF SYNTHESIZING THE SAME
摘要 Novel methods to prepare novel polymers are disclosed. Oxazolidinyl compounds according to formula IV:;;are also disclosed as intermediate compounds that can be reacted with an acid to form a polymer of formula I.
申请公布号 US2015299254(A1) 申请公布日期 2015.10.22
申请号 US201514688026 申请日期 2015.04.16
申请人 Kirshenbaum Kent;Levine Paul;Craven Timothy 发明人 Kirshenbaum Kent;Levine Paul;Craven Timothy
分类号 C07K7/06;C07K17/08 主分类号 C07K7/06
代理机构 代理人
主权项 1. A process for preparing a polymer according to formula I: or a pharmaceutically acceptable salt, stereoisomer, isotopic variant or tautomer thereof; comprising the steps of A1) providing a compound of formula II: A2) reacting the compound of formula II with a polypeptide of formula III: to form the oxazolidine compound of formula IV:  and A3) reacting the oxazolidine compound of formula IV with an acid to form the polymer of formula I; wherein AG is a) a moiety comprising polyethylene glycol; or AG is -(L1-O)m-LINK-; LINK is an alkylene linker; the subscript m is an integer from 2-200; L1 is substituted or unsubstituted alkylene; and Y is hydroxy, protected hydroxyl, amino or protected amino; or Y is —O—R2, —O—C(O)—R2, —NH—C(O)—R2 or —NH—C(O)—O—R2;b) a biotin moiety; and Y is absent;c) a folate moiety; and Y is absent;d) a fluorescein moiety; and Y is absent;e) a lipid moiety; and Y is absent;f) a carbohydrate moiety; and Y is absent;g) a doxorubicin moiety; and Y is absent;h) a small molecule therapeutic moiety, wherein the small molecule therapeutic moiety comprises at least one carboxylic group; and Y is absent;i) a naproxen moiety; and Y is absent;j) an ibuprofen moiety; and Y is absent;k) a small molecule hormone moiety, wherein the small molecule hormone moiety comprises at least one carboxylic group; and Y is absent;l) a thyroxine moiety; and Y is absent; orm) a small molecule imaging agent moiety, wherein the small molecule imaging agent moiety comprises at least one carboxylic group; and Y is absent; X is hydroxyl, alkoxy, amino or substituted amino; R1 is H or methyl; each R2 is independently H, alkyl, or aryl; each R4 is independently H or substituted or unsubstituted alkyl; and the subscript t is 1, 2, 3, or 4.
地址 New York NY US