公开(公告)号：US20010016624A1

公开(公告)日：2001-08-23

申请号：US09824395

申请日：2001-04-02

Applicant: Debio Recherche Pharmaceutique S.A.

Inventor： J. Milton Harris ,  Xuan Zhao

IPC: C08H001/00 ,  C08G065/00 ,  C08L089/00 ,  C08G065/32 ,  C08F283/00 ,  C08F283/06 ,  A61K009/14 ,  C07C033/025

CPC classification number: C08L71/02 ,  A61K47/60 ,  C08G65/329 ,  C08G65/3322 ,  C08L2203/02 ,  Y10S530/81 ,  Y10S530/816 ,  C08L2666/04

Abstract: A heterobifunctional poly(ethylene glycol) is provided having a hydrolytically degradable linkage, a first terminus comprising an acrylate group, and a second terminus comprising a target such as a protein or pharmaceutical agent or a reactive moiety capable of coupling to a target. Hydrogels can be prepared. The hydrogels can be used as a carrier for a protein or a pharmaceutical agent that can be readily released in a controlled fashion.

Abstract translation: 提供具有水解可降解键的异双功能聚（乙二醇），包含丙烯酸酯基的第一末端，和包含诸如蛋白质或药物的靶的第二末端或能够与靶偶合的反应性部分。 水凝胶可以制备。 水凝胶可用作可以以受控方式容易地释放的蛋白质或药剂的载体。

公开(公告)号：US20030202955A1

公开(公告)日：2003-10-30

申请号：US10389560

申请日：2003-03-14

Applicant: Debio Recherche Pharmaceutique S.A.

Inventor： J. Milton Harris

IPC: A61K031/785 ,  A61K031/765 ,  C08G063/48 ,  C08G063/91

CPC classification number: G01N33/528 ,  A61K47/56 ,  A61K47/60 ,  A61K47/6903 ,  B01L3/508 ,  B01L99/00 ,  Y10S424/13 ,  Y10S530/816

Abstract: A degradable PEG hydrogel is described that, upon hydrolysis, releases conjugates of substantially non-peptidic polymers and biologically active molecules. For example, PEG and protein conjugates can be released in vivo from the hydrogels for therapeutic application.

公开(公告)号：US20040086992A1

公开(公告)日：2004-05-06

申请号：US10684946

申请日：2003-10-14

Applicant: Debio Recherche Pharmaceutique S.A.

Inventor： J. Milton Harris ,  Xuan Zhao

IPC: C12N011/00 ,  C12N011/16

CPC classification number: C08L71/02 ,  A61K47/60 ,  C08G65/329 ,  C08G65/3322 ,  C08L2203/02 ,  Y10S530/81 ,  Y10S530/816 ,  C08L2666/04

Abstract: A heterobifunctional poly(ethylene glycol) is provided having a hydrolytically degradable linkage, a first terminus comprising an acrylate group, and a second terminus comprising a target such as a protein or pharmaceutical agent or a reactive moiety capable of coupling to a target. Hydrogels can be prepared. The hydrogels can be used as a carrier for a protein or a pharmaceutical agent that can be readily released in a controlled fashion.

公开(公告)号：US20040086991A1

公开(公告)日：2004-05-06

申请号：US10684692

申请日：2003-10-14

Applicant: Debio Recherche Pharmaceutique S.A.

Inventor： J. Milton Harris ,  Xuan Zhao

IPC: C12N011/00 ,  C12N011/16

CPC classification number: C08L71/02 ,  A61K47/60 ,  C08G65/329 ,  C08G65/3322 ,  C08L2203/02 ,  Y10S530/81 ,  Y10S530/816 ,  C08L2666/04

Abstract: A heterobifunctional poly(ethylene glycol) is provided having a hydrolytically degradable linkage, a first terminus comprising an acrylate group, and a second terminus comprising a target such as a protein or pharmaceutical agent or a reactive moiety capable of coupling to a target. Hydrogels can be prepared. The hydrogels can be used as a carrier for a protein or a pharmaceutical agent that can be readily released in a controlled fashion.

Abstract translation: 提供具有水解可降解键的异双功能聚（乙二醇），包含丙烯酸酯基的第一末端，和包含诸如蛋白质或药物的靶的第二末端或能够与靶偶合的反应性部分。 水凝胶可以制备。 水凝胶可用作可以以受控方式容易地释放的蛋白质或药剂的载体。

公开(公告)号：US20040076602A1

公开(公告)日：2004-04-22

申请号：US10684893

申请日：2003-10-14

Applicant: Debio Recherche Pharmaceutique S.A.

Inventor： J. Milton Harris

IPC: A61K048/00 ,  A61K031/765

CPC classification number: C08G65/329 ,  A61K47/10 ,  A61K47/34

Abstract: This invention relates to hydrolytically degradable gels of crosslinked poly(ethylene) glycol (PEG) structures. Addition of water causes these crosslinked structures to swell and become hydrogels. The hydrogels can be prepared by reacting two different PEG derivatives containing functional moietes at the chain ends that react with each other to form new covalent linkages between polymer chains. The PEG derivatives are chosen to provide covalent linkages within the crosslinked structure that are hydrolytically degradable. Hydrolytic degradation can provide for dissolution of the gel components and for controlled release of trapped molecules, including drugs. Reageants other than PEG can be avoided. The hydrolysis rates can be controlled by varying atoms adjacent to the hydrolytically degradable functional groups to provide substantially precise control for drug delivery in vivo.

Abstract translation: 本发明涉及交联的聚乙二醇（PEG）结构的水解可降解凝胶。 加入水使这些交联结构溶胀并变成水凝胶。 水凝胶可以通过使两个不同的PEG衍生物在链端反应而制备，所述PEG衍生物在链端彼此反应以在聚合物链之间形成新的共价键。 选择PEG衍生物以在交联结构内提供可水解降解的共价键。 水解降解可以提供凝胶组分的溶解和用于控制捕获的分子（包括药物）的释放。 除PEG以外的其他药物可以避免。 可以通过改变与水解可降解官能团相邻的原子来控制水解速率，从而为体内药物递送提供基本精确的控制。