公开(公告)号：US20080139703A1

公开(公告)日：2008-06-12

申请号：US12029324

申请日：2008-02-11

Applicant: Te-Wei Lee ,  Shu-Pei Chiu ,  Chiu-Yu Yu ,  Tsui-Jung Chang ,  Chih-Hsien Chang

Inventor： Te-Wei Lee ,  Shu-Pei Chiu ,  Chiu-Yu Yu ,  Tsui-Jung Chang ,  Chih-Hsien Chang

IPC: C08L89/00

CPC classification number: A61K9/1271 ,  A61K9/1278 ,  A61K47/62 ,  A61K47/6911 ,  C07K14/6555 ,  Y02P20/55

Abstract: The present invention discloses a method for preparing lipid-spacer-reactive functional group-peptide, wherein the peptide consists of 3 to 16 amino acid residues in which at least one amino acid residue is lysine (Lys), the reactive functional group is a formula of —X—CO—Y—CO—, wherein X represents an oxygen atom or a nitrogen atom, and Y represents C1-6 alkylene which may be interrupted by one or two oxygen or nitrogen atom(s), the spacer is a hydrophilic polymer, and the lipid is phosphatidylethanoaminecarbonyl represented by the formula (I): R1 and R2 are the same or different and individually represent linear or branch C7-30 alkyl or linear or branch C7-30 alkenyl; which is characterized in that the reaction is carried out in a liquid phase and comprises the following steps of (a) firstly protecting Lys amino acid residue in the peptide through a protection group; (b) subsequently reacting the peptide with the lipid-spacer-reactive functional group; and (c) finally removing the protection group from Lys amino acid residue in the peptide.

Abstract translation: 本发明公开了一种制备脂质 - 间隔物反应性官能团肽的方法，其中肽由3至16个氨基酸残基组成，其中至少一个氨基酸残基为赖氨酸（Lys），反应性官能团为式 的-X-CO-Y-CO-，其中X表示氧原子或氮原子，Y表示可被一个或两个氧或氮原子间隔的C 1-6亚烷基（ s），间隔基是亲水性聚合物，并且脂质是由式（I）表示的磷脂酰硫代氨基羰基：R 1和R 2都相同或不同，并且各自代表 直链或支链C 7-30烷基或直链或支链C 7-30链烯基; 其特征在于反应在液相中进行，并包括以下步骤：（a）首先通过保护基保护肽中的Lys氨基酸残基; （b）随后使肽与脂质 - 间隔物反应性官能团反应; 和（c）最后从肽中的Lys氨基酸残基中除去保护基团。

公开(公告)号：US20080102110A1

公开(公告)日：2008-05-01

申请号：US11608836

申请日：2006-12-10

Applicant: Te-Wei Lee ,  Shu-Pei Chiu ,  Chiu-Yu Yu ,  Tsui-Jung Chang ,  Chih-Hsien Chang

Inventor： Te-Wei Lee ,  Shu-Pei Chiu ,  Chiu-Yu Yu ,  Tsui-Jung Chang ,  Chih-Hsien Chang

IPC: A61K9/127 ,  C07K7/08 ,  C07K7/06

CPC classification number: A61K9/1271 ,  A61K9/1278 ,  A61K47/62 ,  A61K47/6911 ,  C07K14/6555 ,  Y02P20/55

Abstract: The present invention discloses a method for preparing lipid-spacer-reactive functional group-peptide, whereinthe peptide consists of 3 to 16 amino acid residues in which at least one amino acid residue is lysine (Lys), the reactive functional group is a formula of —X—CO—Y—CO—, wherein X represents an oxygen atom or a nitrogen atom, and Y represents C1-6 alkylene which may be interrupted by one or two oxygen or nitrogen atom(s), the spacer is a hydrophilic polymer, and the lipid is phosphatidylethanoaminecarbonyl represented by the formula (I): R1 and R2 are the same or different and individually represent linear or branch C7-30 alkyl or linear or branch C7-30 alkenyl; which is characterized in that the reaction is carried out in a liquid phase and comprises the following steps of (a) firstly protecting Lys amino acid residue in the peptide through a protection group; (b) subsequently reacting the peptide with the lipid-spacer-reactive functional group; and (c) finally removing the protection group from Lys amino acid residue in the peptide.